The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor for treating novel coronavirus infections (COVID-19).
The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor for treating novel coronavirus infections (COVID-19).
A pharmaceutical composition for treating novel coronavirus infections (COVID-19) is provided, the composition containing, as an active ingredient, a complex that contains:
a compound represented by Formula (I):
The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor for treating novel coronavirus infections (COVID-19).
A pharmaceutical composition for treating novel coronavirus infections (COVID-19) is provided, the composition containing, as an active ingredient, a complex that contains:
a compound represented by Formula (I):
The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor for treating novel coronavirus infections (COVID-19).
A pharmaceutical composition for treating novel coronavirus infections (COVID-19) is provided, the composition containing, as an active ingredient, a complex that contains:
a compound represented by Formula (I):
and
fumaric acid.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
The purpose of the present invention is to provide a novel polynucleotide that efficiently expresses the HIV Tat protein or an antigenic fragment thereof and has an excellent ability to induce an anti-Tat antibody, and to provide a pharmaceutical composition containing the polynucleotide. Disclosed is a novel polynucleotide encoding a polypeptide comprising: (a) the HIV Tat protein or an antigenic fragment thereof; and (b) a signal peptide. The pharmaceutical composition containing the polynucleotide can be used for the treatment and/or prevention of HIV-related diseases.
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Provided is a compound represented by Formula (I):
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Provided is a compound represented by Formula (I):
wherein Ring A is a ring represented by:
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Provided is a compound represented by Formula (I):
wherein Ring A is a ring represented by:
wherein X is a single bond or the like, R2 is substituted or unsubstituted aromatic carbocyclyl or the like, R3c is substituted or unsubstituted aromatic carbocyclyl or the like, R3 is substituted or unsubstituted aromatic carbocyclyl or the like, R3a is a hydrogen atom or the like, R3b is a hydrogen atom, R8a is substituted or unsubstituted aromatic carbocyclyl or the like, and R8b is a hydrogen atom or the like,
R1 is a substituted or unsubstituted aromatic heterocyclyl, m is 0 or the like, R5a is each independently a hydrogen atom or the like, R5b is each independently a hydrogen atom or the like, R6 is cyano or the like, and R7a and R7b are each independently a hydrogen atom or the like, or a pharmaceutically acceptable salt of the compound.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
4.
SYSTEM, METHOD, AND NON-TRANSITORY COMPUTER-READABLE RECORDING MEDIUM
A system has an output for outputting an acoustic signal generated by amplitude modulation, the acoustic signal having an amplitude change corresponding to the frequency of gamma waves, a memory for storing information of the acoustic signal output by the output, and a transmission for transmitting a notification based on the information stored by the memory to a apparatus external to the system.
Provided are a new pharmaceutical composition and a method for treating and/or preventing autism spectrum disorder, fragile X syndrome, and/or an autism spectrum disorder-like symptom. A pharmaceutical composition for the treatment and/or prevention of autism spectrum disorder, fragile X syndrome, and/or an autism spectrum disorder-like symptom, comprising buprenorphine or a pharmaceutically acceptable salt thereof and/or morphine or a pharmaceutically acceptable salt thereof.
Provided is a pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition having an excellent ACC2-selective inhibitory effect and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
Provided is a pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition having an excellent ACC2-selective inhibitory effect and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition comprising a compound represented by Formula (I):
Provided is a pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition having an excellent ACC2-selective inhibitory effect and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition comprising a compound represented by Formula (I):
wherein R1 is haloalkyl or non-aromatic carbocyclyl,
R2 is a hydrogen atom or halogen,
R3 is halogen,
ring A is a group represented by the formula:
Provided is a pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition having an excellent ACC2-selective inhibitory effect and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing at least one of heart diseases, heart disease complications, skeletal muscle diseases, and skeletal muscle conditions, the pharmaceutical composition comprising a compound represented by Formula (I):
wherein R1 is haloalkyl or non-aromatic carbocyclyl,
R2 is a hydrogen atom or halogen,
R3 is halogen,
ring A is a group represented by the formula:
—L1-is —O—(CH2)2, —(CH2)2—, or the like,
R4 is alkyl or haloalkyl, and
R5 is alkylcarbonyl or carbamoyl,
or a pharmaceutically acceptable salt thereof.
The present invention provides a compound showing coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. A compound represented by formula (I) [in the formula: ring A is a ring represented by formula (I-A) (wherein X is a single bond, etc., R2 is a substituted or unsubstituted aromatic carbocyclic group, etc., and R3c is a substituted or unsubstituted aromatic carbocyclic group, etc.); R1 is a substituted or unsubstituted aromatic heterocyclic group; m is 0, etc.; R5as are independently a hydrogen atom, etc.; R5bs are independently a hydrogen atom, etc.; R6 is cyano, etc.; and R7a and R7b are independently a hydrogen atom, etc.], or a pharmaceutically acceptable salt thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C12N 7/06 - Inactivation or attenuationProducing viral sub-units by chemical treatment
C12N 9/99 - Enzyme inactivation by chemical treatment
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
8.
SPIROHETEROCYCLE DERIVATIVE HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
wherein R1 is a hydrogen atom or the like; A1 is each independently CR2R2′; A2 is each independently CR3R3′, R2 is each independently a hydrogen atom or the like; R2′ is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; R3′ is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
wherein R1 is a hydrogen atom or the like; A1 is each independently CR2R2′; A2 is each independently CR3R3′, R2 is each independently a hydrogen atom or the like; R2′ is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; R3′ is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
wherein R1 is a hydrogen atom or the like; A1 is each independently CR2R2′; A2 is each independently CR3R3′, R2 is each independently a hydrogen atom or the like; R2′ is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; R3′ is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:
or the like
wherein R4 is a group represented by Formula:
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
wherein R1 is a hydrogen atom or the like; A1 is each independently CR2R2′; A2 is each independently CR3R3′, R2 is each independently a hydrogen atom or the like; R2′ is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; R3′ is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:
or the like
wherein R4 is a group represented by Formula:
Provided are compounds having a serotonin 5-HT2A receptor antagonism and/or inverse agonism, pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising thereof.
A compound represented by Formula (I):
wherein R1 is a hydrogen atom or the like; A1 is each independently CR2R2′; A2 is each independently CR3R3′, R2 is each independently a hydrogen atom or the like; R2′ is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; R3′ is each independently a hydrogen atom or the like; m and n are each independently 1 or the like; ring B is a ring represented by Formula:
or the like
wherein R4 is a group represented by Formula:
or the like
wherein A3 is each independently CR13R13′; A4 is each independently CR14R14′; R13 is each independently a hydrogen atom or the like; R13′ is each independently a hydrogen atom or the like; R14 is each independently a hydrogen atom or the like; R14′ is each independently a hydrogen atom or the like; q and r are each independently 1 or the like; R10 and R11 are each independently substituted or unsubstituted aromatic carbocyclyl or the like; R8 is a hydrogen atom or the like, or a pharmaceutically acceptable salt thereof.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
The present invention provides a medicament useful in treatment and/or prevention, etc. of COVID-19.
The present invention provides a medicament useful in treatment and/or prevention, etc. of COVID-19.
Provided is a medicament characterized by combining (A) a compound represented by Formula (I):
The present invention provides a medicament useful in treatment and/or prevention, etc. of COVID-19.
Provided is a medicament characterized by combining (A) a compound represented by Formula (I):
wherein Y is N; R1 is substituted or unsubstituted aromatic heterocyclyl; R2 is substituted or unsubstituted 6-membered aromatic carbocyclyl; R3 is substituted or unsubstituted aromatic heterocyclyl; —X— is —NH—; m is 0 or 1; R5a is a hydrogen atom; R5b is a hydrogen atom; n is 1; R4a is a hydrogen atom; and R4b is a hydrogen atom, or a pharmaceutically acceptable salt thereof; and
(B) a COVID-19 exacerbation suppressant.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
Provided is a novel method for producing a uracil derivative. A method for producing a compound represented by formula (III) (in the formula, R1 represents a halogen or the like, each R2 is independently a halogen or the like, Z is CH or the like, and n is an integer of 1-5), or a salt thereof, characterized by reacting a compound represented by formula (I) (symbols in the formula are as defined above), or a salt thereof, with a compound represented by formula (II) (symbols in the formula are as defined above), or a salt thereof, in the presence or absence of a base and in the presence of a condensing agent selected from the group consisting of T3P (registered trademark) and the like.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C12N 9/99 - Enzyme inactivation by chemical treatment
The present invention provides a pharmaceutical composition containing a compound that exhibits coronavirus growth–inhibiting activity. Provided is a pharmaceutical composition containing a compound represented by formula (I-1) or a pharmaceutically acceptable salt thereof.
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention provides a preparation (pharmaceutical composition) containing, as an active ingredient, a uracil derivative exhibiting coronavirus 3 CL protease inhibitory activity, a pharmaceutically acceptable salt thereof, or a solvate thereof. The present invention also provides crystals of a uracil derivative exhibiting coronavirus 3 CL protease inhibitory activity, a pharmaceutically acceptable salt thereof, or a solvate thereof.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C12N 9/99 - Enzyme inactivation by chemical treatment
13.
BISPECIFIC ANTIBODY THAT RECOGNIZES CCR8 AS ANTIGEN
Disclosed is a bispecific antibody that recognizes CCR8 as an antigen. It was found that the bispecific antibody has cytotoxic activity against CCR8-expressing cells.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Taoda, Yoshiyuki
Uehara, Shota
Sako, Yuseke
Hirai, Keiichiro
Abstract
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Provided is a compound represented by Formula (I):
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
Provided is a compound represented by Formula (I):
wherein carbon atom a and carbon atom b are each a carbon atom constituting ring A, the ring A is substituted aromatic carbocycle or the like, R1 is substituted or unsubstituted aromatic heterocyclyl or the like, R2 is substituted or unsubstituted 6-membered aromatic carbocyclyl or the like, m is 1 or the like, R5as are each independently a hydrogen atom or the like, R5bs are each independently a hydrogen atom or the like, n is 1 or the like, R4a is a hydrogen atom or the like, and R4a is a hydrogen atom or the like. Alternatively, provided is a pharmaceutically acceptable salt of the compound.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
15.
MEDICINE FOR PREVENTION AND TREATMENT OF DISEASES LINKED TO ANTI-OBESITY ACTIVITY
A pharmaceutical preparation characterized by combination of (A) and (B) is useful for the prevention and treatment of a disease related to anti-obesity effect, wherein
(A) is a compound represented by formula:
A pharmaceutical preparation characterized by combination of (A) and (B) is useful for the prevention and treatment of a disease related to anti-obesity effect, wherein
(A) is a compound represented by formula:
or a pharmaceutically acceptable salt thereof, and
(B) is at least one agent selected from the group consisting of agents having anti-obesity action, agents for controlling blood glucose level, agents for controlling cholesterol and/or triglyceride in blood, and agents for controlling blood pressure.
A61K 31/499 - Spiro-condensed pyrazines or piperazines
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention provides a preparation that is minimally colored through irradiation with light by coating a preparation containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a crystal thereof with a light stabilizing substance and a polymer, particularly with one or more of titanium oxide and talc used as the light stabilizing substance and hypromellose used as the polymer.
The purpose of the present invention is to provide a pharmaceutical composition containing a novel Nav1.7 monoclonal antibody. Disclosed is a pharmaceutical composition comprising a Nav1.7 monoclonal antibody having a specific CDR or a specific heavy chain variable region/light chain variable region, or an antibody fragment thereof. This pharmaceutical composition can be used for the treatment or prevention of pain, pruritis, and the like.
The present invention provides a compound represented by Formula (I):
The present invention provides a compound represented by Formula (I):
The present invention provides a compound represented by Formula (I):
wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
The present invention accurately predicts the magnitude of a subject's future psychological stress. A prediction system (100) comprises: a first extraction unit (42) that extracts a group of similar workers from a plurality of workers (W) on the basis of the degree of similarity of the work patterns of the plurality of workers (W) to the work pattern of a subject (O) during a first period; a first model generation unit (43) that generates a first prediction model (57) through machine learning using, as learning data, first information including at least work pattern information, measurement information, behavioral record information, and psychological stress information of each worker (W) included in the group of similar workers; and a first prediction unit (44) that predicts the magnitude of psychological stress of the subject (O) by entering input data, including at least work pattern information, measurement information, and behavioral record information of the subject (O), into the first prediction model (57).
G06Q 10/06 - Resources, workflows, human or project managementEnterprise or organisation planningEnterprise or organisation modelling
G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
20.
SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES AND PRODRUGS THEREOF
The present inventon provides the following compounds having anti-viral activity.
The present inventon provides the following compounds having anti-viral activity.
A1 is CR1AR1B, S or O;
A2 is CR2AR2B, S or O;
A3 is CR3AR3B, S or O;
A4 is CR4AR4B, S or O;
the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2;
R1A and R1B are each independently hydrogen, halogen, alkyl, or the like;
R2A and R2B are each independently hydrogen, halogen, alkyl, or the like;
R3A and R3B are each independently hydrogen, halogen, alkyl, or the like;
R4A and R4B are each independently hydrogen, halogen, alkyl, or the like;
R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle;
X is CH2, S or O;
R1 is each independently halogen, hydroxy, or the like;
m is any integer of 0 to 2; and
n is any integer of 1 to 2.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
21.
FUSED RING DERIVATIVE HAVING MGAT-2 INHIBITORY ACTIVITY
The present invention provides the compound represented by the following formula (I):
The present invention provides the compound represented by the following formula (I):
wherein a moiety represented by formula:
The present invention provides the compound represented by the following formula (I):
wherein a moiety represented by formula:
The present invention provides the compound represented by the following formula (I):
wherein a moiety represented by formula:
or the like;
y is 0 or 1; R1 is hydrogen or the like; R2a and R2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R3a is hydrogen or the like; R3b is hydrogen or the like; R4a is represented by formula:
The present invention provides the compound represented by the following formula (I):
wherein a moiety represented by formula:
or the like;
y is 0 or 1; R1 is hydrogen or the like; R2a and R2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R3a is hydrogen or the like; R3b is hydrogen or the like; R4a is represented by formula:
The present invention provides the compound represented by the following formula (I):
wherein a moiety represented by formula:
or the like;
y is 0 or 1; R1 is hydrogen or the like; R2a and R2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R3a is hydrogen or the like; R3b is hydrogen or the like; R4a is represented by formula:
L1 is a single bond or the like; L2 is —C(═O)— or the like; La is a single bond or the like; R7 is substituted or unsubstituted alkyl or the like; R4b is substituted or unsubstituted alkyl or the like; R4c is each independently halogen or the like.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
22.
TREATING INFLUENZA USING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES AND PRODRUGS THEREOF IN A SUBJECT HAVING INFLUENZA AND A SEVERE INFLUENZA CONDITION
A method for treating an influenza virus infection is described. The disclosed method generally involves administering an effective amount of a compound (A), for example baloxavir marboxil, and a compound (B), for example a neuraminidase inhibor, to a subject that (1) has an influenza virus infection, (2) has been symptomatic of the influenza virus infection for no more than 96 hours, and (3) further has at least one severe influenza condition selected from the following: (a) being hospitalized due to severe influenza virus infection, (b) requiring an extension of hospitalization because of the influenza virus infection during the hospitalization, (c) having a National Early Warning Score 2 of four or more, (d) being on support for respiration, and (e) having at least one complication attributable to the influenza virus infection that necessitates hospitalization.
Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a pharmaceutical composition containing the same, particularly an anti-HIV pharmaceutical composition.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
The present invention provides a solid dosage form having good stability, suspensibility in water and fluidity by preparing a solid dosage form containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a stabilizer, a sugar alcohol and/or a sugar, a water-soluble polymer and an inorganic substance.
A method for treating an influenza virus infection is described. The disclosed method generally involves administering an effective amount of a compound, for example baloxavir marboxil, to a subject having an influenza virus infection and at least one complication risk factor. Generally, the amount is effective such that a reduction in a time to improvement of at least one symptom of an influenza virus infection is statistically significant as compared to that of a non-treated subject.
The present invention relates to a compound that has GLP-1 receptor agonist activity and is useful as a therapeutic or prophylactic agent for diseases associated with the GLP-1 receptor, or a pharmaceutically acceptable salt thereof, and relates to a pharmaceutical composition containing the compound or its pharmaceutically acceptable salt.
The present invention relates to a compound that has GLP-1 receptor agonist activity and is useful as a therapeutic or prophylactic agent for diseases associated with the GLP-1 receptor, or a pharmaceutically acceptable salt thereof, and relates to a pharmaceutical composition containing the compound or its pharmaceutically acceptable salt.
Provided is a compound represented by formula (I):
The present invention relates to a compound that has GLP-1 receptor agonist activity and is useful as a therapeutic or prophylactic agent for diseases associated with the GLP-1 receptor, or a pharmaceutically acceptable salt thereof, and relates to a pharmaceutical composition containing the compound or its pharmaceutically acceptable salt.
Provided is a compound represented by formula (I):
wherein A1 is C(R5) or the like, A2 is C(R6) or the like, A3 is C(R7) or the like, R5, R6, and R7 are each independently a hydrogen atom or the like, R1 is carboxy or the like, R2 is substituted or unsubstituted alkyl or the like, —X— is —O— or the like, the ring represented by:
The present invention relates to a compound that has GLP-1 receptor agonist activity and is useful as a therapeutic or prophylactic agent for diseases associated with the GLP-1 receptor, or a pharmaceutically acceptable salt thereof, and relates to a pharmaceutical composition containing the compound or its pharmaceutically acceptable salt.
Provided is a compound represented by formula (I):
wherein A1 is C(R5) or the like, A2 is C(R6) or the like, A3 is C(R7) or the like, R5, R6, and R7 are each independently a hydrogen atom or the like, R1 is carboxy or the like, R2 is substituted or unsubstituted alkyl or the like, —X— is —O— or the like, the ring represented by:
is a ring represented by:
The present invention relates to a compound that has GLP-1 receptor agonist activity and is useful as a therapeutic or prophylactic agent for diseases associated with the GLP-1 receptor, or a pharmaceutically acceptable salt thereof, and relates to a pharmaceutical composition containing the compound or its pharmaceutically acceptable salt.
Provided is a compound represented by formula (I):
wherein A1 is C(R5) or the like, A2 is C(R6) or the like, A3 is C(R7) or the like, R5, R6, and R7 are each independently a hydrogen atom or the like, R1 is carboxy or the like, R2 is substituted or unsubstituted alkyl or the like, —X— is —O— or the like, the ring represented by:
is a ring represented by:
and the like
wherein
R10 is each independently halogen or the like,
s is 0 or the like,
R13 is each independently a hydrogen atom or the like, and R3 is substituted or unsubstituted aromatic carbocyclyl or the like, or
a pharmaceutically acceptable salt thereof.
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
The purpose of the present invention is to provide a capsule or granules containing a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate of the same. Provided are a capsule or granules that contain, e.g., a compound represented by formula (I) and have excellent elution properties because of containing a surfactant.
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
28.
CHIMERIC ANTIGEN RECEPTOR THAT RECOGNIZES CCR8 AS ANTIGEN
The chimeric antigen receptor that recognizes CCR8 as an antigen of the present invention has cytotoxic activity against CCR8-expressing cells by being expressed in effector cells.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention provides a compound having an antagonist and/or inverse agonist action on the serotonin 5-HT2A receptor as well as an antagonist and/or inverse agonist action on the serotonin 5-HT2C receptor, or a pharmaceutically acceptable salt thereof. The present invention also provides a pharmaceutical composition containing the same. Provided is a compound represented by formula 1, or a pharmaceutically acceptable salt thereof. (In the formula: R1is a substituted or unsubstituted 6-membered aromatic heterocyclic group or the like; A1is CR2or the like; A2is CR3or the like; A3is CR4or the like; R2, R3, and R4are each independently a hydrogen atom or the like; R5is a substituted or unsubstituted aromatic heterocyclic group or the like; R15and R16are each independently a hydrogen atom or the like; and R17and R18 are each independently a hydrogen atom or the like.)
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention provides novel cationic lipids having excellent encapsulation and delivery stability of nucleic acid medicines. Provided is a compound represented by Formula (I) or a pharmacologically acceptable salt thereof. In the Formula (I), R1 is a substituted or unsubstituted formula: (CH2)a—L1—(CH2)b—CH3; R2 is a substituted or unsubstituted C5-C20 alkyl group or a substituted or unsubstituted formula: —(CH2)c—L2—(CH2)a—CH3; L1 and L2 are each independently —C(═O)O—, —OC(═O)—, or —OC(═O)O—; a, b, c, and d are each independently an integer of at least 1, and the total of a and b and the total of c and d are each an integer of 5 to 25; R3 to R7 are each independently a hydrogen atom, a substituted or unsubstituted C1-C6 alkyl group, or the like; R8, R9, and R10 are each a hydrogen atom; the constituent atoms in the Formula (I) may form a ring; Z is —OC(═O)—, —C(═O)O—, —OC(═O)O—, or the like; and X is O or S.
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 47/16 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen
C07C 229/24 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one carboxyl group bound to the carbon skeleton, e.g. aspartic acid
C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
32.
USE OF PYRIDINE DERIVATIVE WHICH IS TRPV1 ANTAGONIST
The present invention provides a novel pharmaceutical composition and a method for treating and/or preventing social impairment, such as autism spectrum disorder, fragile X syndrome, and/or autism spectrum-like symptoms. Specifically, provided is a pharmaceutical composition for the treatment and/or prevention of social impairment, the pharmaceutical composition comprising a compound represented by formula (I) (in the formula, R1is a substituted or unsubstituted alkyl; R2is a hydrogen atom or the like; A is N or the like; the dashed line represents the presence or absence of a bond; R3is a substituted or unsubstituted alkyl or the like; m is 0 or 1; and R4and R5 each independently represent a hydrogen atom or the like) or a pharmaceutically acceptable complex thereof.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Shionogi & Co., Ltd. (Japan)
Inventor
Kitajima, Masaaki
Iwamoto, Ryo
Masago, Yusaku
Hayase, Shin
Katayama Adachi, Yuka
Abstract
The present invention provides a method for quantitatively detecting virus-derived RNA and/or DNA in an environmental sample or a fecal sample with high sensitivity, and a kit for quantitatively detecting virus-derived RNA and/or DNA in an environmental sample or a fecal sample with high sensitivity.
C12Q 1/70 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving virus or bacteriophage
C12Q 1/689 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for detection or identification of organisms for bacteria
NATIONAL UNIVERSITY CORPORATION KOCHI UNIVERSITY (Japan)
SHIONOGI & CO., LTD. (Japan)
Inventor
Aoyama, Bun
Kawano, Takashi
Abstract
The purpose of the present invention is to provide a preparation that can effectively suppress post-operative delirium. A post-operative delirium suppressant according to the present invention is characterized by containing a GABA-A receptor selective positive allosteric modulator as an active ingredient.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
36.
MONOCYCLIC COMPOUND HAVING GLP-1 RECEPTOR AGONIST ACTIVITY
11 is C(R522 is C(R633 is C(R7) or N, R5, R6, and R7are each independently a hydrogen atom or the like, R2is a substituted or unsubstituted alkyl or the like, R3is a phenyl or the like that may be substituted with a substituent from group F, which includes halogens, cyanos, alkyls, haloalkyls, alkyloxys, and haloalkyloxys, and, in the formulas for -L-, R1is a hydrogen atom or the like, R8is a hydrogen atom or the like, each R10 is independently a cyano group or the like, and m is an integer from 1 to 3.)
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
11 is C(R1), etc.; R1is a hydrogen atom, etc.; R811 is CH, etc.; R10is cyano, etc. R3is a phenyl group optionally substituted with a group of substituents F, etc.; the group of substituents F: halogen, cyano, alkyl, haloalkyl, alkyloxy and haloalkyloxy; Q is a substituted or unsubstituted benzene ring, etc.; R2 is a substituted or unsubstituted alkyl, etc.; and -L- is a group represented by the formula, etc.].
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A condensed heterocyclic compound has a sepiapterin reductase inhibitory action and is particularly useful for treatment of a pain. The condensed heterocyclic compound represented by Formula (I) below (R1 represents a hydrocarbon group or the like; R2 and R3 represent a hydrogen atom or the like; R4, X, and Y represent defined substituents), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of any of these.
A condensed heterocyclic compound has a sepiapterin reductase inhibitory action and is particularly useful for treatment of a pain. The condensed heterocyclic compound represented by Formula (I) below (R1 represents a hydrocarbon group or the like; R2 and R3 represent a hydrogen atom or the like; R4, X, and Y represent defined substituents), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of any of these.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
A compound represented by Formula (I):
Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
A compound represented by Formula (I):
wherein R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or the like; a combination of (L1, L2) is (NH, N) or the like; R4 is a group represented by Formula:
Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
A compound represented by Formula (I):
wherein R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or the like; a combination of (L1, L2) is (NH, N) or the like; R4 is a group represented by Formula:
wherein p and q are each independently 2 or the like; Ra is substituted or unsubstituted alkyl or the like; Xb is each independently CRbRb′; Rb is each independently a hydrogen atom or the like; Rb′ is each independently a hydrogen atom or the like; Xc is each independently CRcRc′; Rc is each independently a hydrogen atom or the like; Rc′ is each independently a hydrogen atom or the like; Xd is CRd or the like; and Rd is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; and R7 is a group represented by Formula:
Provided are a compound having serotonin 5-HT2A receptor antagonism and/or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and/or inverse agonism comprising them.
A compound represented by Formula (I):
wherein R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or the like; a combination of (L1, L2) is (NH, N) or the like; R4 is a group represented by Formula:
wherein p and q are each independently 2 or the like; Ra is substituted or unsubstituted alkyl or the like; Xb is each independently CRbRb′; Rb is each independently a hydrogen atom or the like; Rb′ is each independently a hydrogen atom or the like; Xc is each independently CRcRc′; Rc is each independently a hydrogen atom or the like; Rc′ is each independently a hydrogen atom or the like; Xd is CRd or the like; and Rd is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; and R7 is a group represented by Formula:
wherein A is CR11 or the like; R9 is substituted or unsubstituted alkyloxy or the like; R10 is a hydrogen atom or the like; and R11 is each independently a hydrogen atom or the like; or a pharmaceutically acceptable salt thereof.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention provides a pharmaceutical composition containing a compound represented by formula (I), a salt thereof, or a solvate thereof. The present invention uses, as a disintegrant, a partially pregelatinized starch, carmellose calcium, a low-substituted hydroxypropyl cellulose, carmellose, and/or crospovidone, and uses D-mannitol as an excipient. As a result, it is possible to produce a pharmaceutical composition in which a change in contents, an increase in analogs, and a change in color tone occur less.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
41.
SIGNAL PROCESSING DEVICE, CONGNITIVE FUNCTION IMPROVEMENT SYSTEM, SIGNAL PROCESSING METHOD, AND PROGRAM
A signal processing device according to an embodiment of the present disclosure has: a reception means for receiving an input acoustic signal; a generation means for performing a modulation process including amplitude modulation on the input acoustic signal received by the reception means, and thereby generating a modulated acoustic signal having a change in amplitude corresponding to the frequency of gamma waves; and an output means for outputting content that includes the modulated acoustic signal generated by the generation means, and modulation information relating to the modulation process performed in order to generate the modulated acoustic signal, in association with each other.
A61M 21/00 - Other devices or methods to cause a change in the state of consciousnessDevices for producing or ending sleep by mechanical, optical, or acoustical means, e.g. for hypnosis
42.
SIGNAL PROCESSING DEVICE, EARPHONE EQUIPPED WITH MICROPHONE, SIGNAL PROCESSING METHOD, AND PROGRAM
A signal processing device according to one embodiment of the present disclosure comprises: an acquisition means for acquiring an input acoustic signal based on a sound picked up by a microphone disposed in the vicinity of a user's ear; a generation means for generating an output acoustic signal having a variable volume corresponding to the frequency of a gamma wave by performing modulation processing, including amplitude modulation, on the input acoustic signal acquired by the acquisition means; and an output means for outputting the output acoustic signal generated by the generation means to a speaker from which a sound is emitted toward the user's ear.
A signal processing device according to an aspect of the present disclosure comprises: an output means that outputs an acoustic signal which is generated by amplitude modulation and has an amplitude change corresponding to the frequency of a gamma wave; a storage means in which information of the acoustic signal output by the output means is stored; and a transmission means that transmits a notification based on the information stored in the storage means to an external device.
Provided is a crystal of a dihydropyridinone derivative or a solvate thereof. The present invention relates to: a crystal of a compound represented by the formula, or a solvate thereof; and a pharmaceutical composition containing the same.
The purpose of the present invention is to provide a novel antibody or antibody fragment thereof that binds to cannabinoid type 1 (CB1) receptors. Disclosed is a CB1 receptor antibody having six specific CDRs (heavy-chain CDR1 to CDR3 and light-chain CDR1 to CDR3) or a specific heavy-chain variable region/light-chain variable region, or an antibody fragment thereof. The antibody, etc., can be used in the treatment or prevention of obesity, diabetes, non-alcoholic steatohepatitis, and the like.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
The present invention provides a compound represented by formula (I):
The present invention provides a compound represented by formula (I):
wherein the dashed line indicates the presence or absence of a bond; R1 is carboxy or the like; L is substituted or unsubstituted non-aromatic carbocyclyldiyl or the like; R2 is substituted or unsubstituted alkyl; R3 is a hydrogen atom or the like; X is ═CRX— or ═N—; Y is ═CRY— or ═N—; U is —CRU═ or —N═; V is —CRV═ or —N═; W is ═CRW— or ═N—; ZA is —C═ or —N—; ZB is —CR5R6— or the like; ZC is —CR7R8— or the like; RX, RY, RV and RW are each independently a hydrogen atom or the like; RU is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; R7 and R8 are each independently a hydrogen atom or the like; R4 is substituted or unsubstituted alkyloxy or the like,
or a pharmaceutically acceptable salt thereof, having an antiviral activity; and a pharmaceutical composition comprising the same.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
NATIONAL UNIVERSITY CORPORATION NARA INSTITUTE OF SCIENCE AND TECHNOLOGY (Japan)
Inventor
Yoshida, Yuki
Kiguchi, Ryo
Fujita, Satoki
Hata, Ayano
Furukawa, Toshiaki
Tajika, Aran
Yoshimoto, Junichiro
Abstract
The purpose of the present invention is to accurately predict re-occurrence and worsening of a depressive symptom beforehand. An information processing system (100) is provided with: a clustering unit (52) which inputs behavior record information of a user (U) into a clustering model for classifying behavior patterns into a plurality of clusters, to classify a behavior pattern of the user (U) into one of the plurality of clusters; a first feature generation unit (53) which generates a first feature indicating an activity state of the user U; and an estimation unit (55) which estimates the magnitude of a psychological stress of the user (U) on the basis of subject information including attribute information of a subject, the cluster into which the behavior pattern of the subject has been classified, and the first feature.
G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
Provided are novel anti-CCR8 antibodies. Said antibodies detect CCR8 expressed in tumor invasive Treg cells or the like and are useful for cancer diagnosis or companion diagnostics.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention provides: a compound that exhibits a coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the same. The compound is represented by formula (I) (where: ring A is represented by formula (I-A) (where: X is a single bond or the like; R2is a substituted or unsubstituted aromatic carbocyclic group or the like; R3cis a substituted or unsubstituted aromatic carbocyclic group or the like; R3is a substituted or unsubstituted aromatic carbocyclic group or the like; R3ais a hydrogen atom or the like; R3bis a hydrogen atom; R8ais a substituted or unsubstituted aromatic carbocyclic group or the like; and R8bis a hydrogen atom or the like); R1is a substituted or unsubstituted aromatic heterocyclic group; m is 0 or the like; R5ais each independently a hydrogen atom or the like; R5bis each independently a hydrogen atom or the like; R6is cyano or the like; and R7aand R7b are each independently a hydrogen atom or the like) or pharmaceutically acceptable salt thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C12N 7/06 - Inactivation or attenuationProducing viral sub-units by chemical treatment
C12N 9/99 - Enzyme inactivation by chemical treatment
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
50.
URACIL DERIVATIVE HAVING VIRAL GROWTH INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
The present invention provides a compound showing coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. A compound represented by formula (I) [in the formula: ring A is a ring represented by formula (I-A) (wherein X is a single bond, etc., R2is a substituted or unsubstituted aromatic carbocyclic group, etc., and R3cis a substituted or unsubstituted aromatic carbocyclic group, etc.); R1is a substituted or unsubstituted aromatic heterocyclic group; m is 0, etc.; R5as are independently a hydrogen atom, etc.; R5bs are independently a hydrogen atom, etc.; R6is cyano, etc.; and R7aand R7b are independently a hydrogen atom, etc.], or a pharmaceutically acceptable salt thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C12N 7/06 - Inactivation or attenuationProducing viral sub-units by chemical treatment
C12N 9/99 - Enzyme inactivation by chemical treatment
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
By administering a liposome formulation in which an antibacterial agent is bound to a liposome, in particular, a lipid-soluble side chain of the antibacterial agent is bound to a lipid of the liposome, and the antibacterial agent extends outward from a surface of the liposome, it is possible to provide a liposome formulation in which blood retention of an active ingredient is increased, an amount of the active ingredient taken by a reticuloendothelial system such as a liver is reduced, an amount of the active ingredient transferred into a kidney is reduced, and antibacterial activity can also be increased with little resistance.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY (Japan)
Inventor
Uchiumi Takaoki
Ota Norio
Inoue Youko
Nishi Hiroshi
Shimosako Kenichi
Nishibori Masahiro
Morimatsu Hiroshi
Abstract
The problem to be solved by the invention is to provide monoclonal antibodies that can specifically detect and capture HRG in a test sample, a set (or combination) thereof, and an HRG measuring method using these antibodies. As a result of extensive research, the present inventors discovered antibodies that can detect and capture HRG in test samples with good sensitivity and specificity, a set of these antibodies, and an HRG measuring method using these antibodies. The present invention is a result of this discovery.
ESTIMATION SYSTEM, ESTIMATION METHOD, PROGRAM, ESTIMATION MODEL, BRAIN ACTIVITY TRAINING APPARATUS, BRAIN ACTIVITY TRAINING METHOD, AND BRAIN ACTIVITY TRAINING PROGRAM
ADVANCED TELECOMMUNICATIONS RESEARCH INSTITUTE INTERNATIONAL (Japan)
SHIONOGI & CO., LTD. (Japan)
Inventor
Ogawa, Takeshi
Tamano, Ryuta
Kawanabe, Motoaki
Kawato, Mitsuo
Abstract
An estimation system obtains brain wave measurement data and functional magnetic resonance imaging measurement data simultaneously measured from a subject, calculates first functional connectivity for each channel combination based on correlation between channels included in the brain wave measurement data, calculates second functional connectivity for each brain network based on correlation between regions of interest included in the functional magnetic resonance imaging measurement data, calculates a disorder-likelihood label by calculating a score representing disorder-likelihood to be estimated with the use of a plurality of second functional connectivities, and determines an estimation model for estimating disorder-likelihood based on prescribed first functional connectivity by machine learning using the first functional connectivity for each channel combination and the disorder-likelihood label.
A61B 5/055 - Detecting, measuring or recording for diagnosis by means of electric currents or magnetic fieldsMeasuring using microwaves or radio waves involving electronic [EMR] or nuclear [NMR] magnetic resonance, e.g. magnetic resonance imaging
ADVANCED TELECOMMUNICATIONS RESEARCH INSTITUTE INTERNATIONAL (Japan)
HIROSHIMA UNIVERSITY (Japan)
SHIONOGI & CO., LTD. (Japan)
Inventor
Kashiwagi, Yuto
Tokuda, Tomoki
Takahara, Yuji
Kawato, Mitsuo
Yamashita, Ayumu
Yamashita, Okito
Sakai, Yuki
Yoshimoto, Junichiro
Okada, Go
Abstract
There is provided a therapy selection support device that generates a discriminator (identifier) as a diagnostic marker or a classifier as a stratification marker through machine learning on the basis of measurement data on brain activities and that uses the discriminator or the classifier as a biomarker.
There is provided a therapy selection support device that generates a discriminator (identifier) as a diagnostic marker or a classifier as a stratification marker through machine learning on the basis of measurement data on brain activities and that uses the discriminator or the classifier as a biomarker.
A therapy selection support system 300a, 300b, 500 includes a clustering device 300b that executes stratification in which the results of measurement of brain functional connectivity correlation values acquired from a plurality of second subjects are divided into a plurality of clusters through a clustering process. The therapy selection support system further includes: a database device 5100 that stores clusters obtained as a result of stratification by a clustering classifier and corresponding predetermined therapy information in association with each other; and a support information providing device 300a that receives an input of the results of measurement of brain activities of a first subject and that outputs corresponding therapy information in accordance with the results of classification by the clustering classifier for the measurement results.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
By administering a PLGA preparation in which an antimicrobial is bonded outwardly to the surface of PLGA particles, the antimicrobial is less likely to be taken up by the reticuloendothelial system, the toxicity can also be reduced, residence in the blood can be maintained, and the antimicrobial action can be heightened.
A61K 47/59 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
B25J 9/10 - Programme-controlled manipulators characterised by positioning means for manipulator elements
56.
NOVEL ACRIDINIUM SALT AND METHOD FOR PRODUCING SAME
The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.
The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.
The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.
wherein R1 is C1-C6 alkyl or C1-C6 alkyloxy; R2 is hydrogen or C1-C6 alkyloxy; R3 is hydrogen, halogen, C1-C6 alkyl or C1-C6 alkyloxy; R4 is hydrogen, C1-C6 alkyloxy, halo C1-C6 alkyloxy or C1-C6 alkylamino; R5 is C1-C3 alkyl; and X− is an anion.
C07D 219/02 - Heterocyclic compounds containing acridine or hydrogenated acridine ring systems with only hydrogen, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
57.
PROGRAM GENERATION ASSISTING SYSTEM FOR ASSISTING GENERATION OF PROGRAM FOR ANALYZING CLINICAL TRIAL
The purpose of the present disclosure is to assist automation of programming for automatic generation of an analysis material prepared by analysis work in a clinical trial during pharmaceutical development. Using the format information, the layout information, and the image data of an image/table analysis plan, this program generation assisting system performs form pattern prediction by two approaches: micro rule-based prediction and macro CNN-based prediction. In addition, the program generation assisting system performs model data/variable prediction by using the format information and the layout information of the image/table analysis plan, an ADaM specification, and ADaM/variable association information, and presents a combination of the model data/variable prediction and the pattern prediction.
G06V 10/82 - Arrangements for image or video recognition or understanding using pattern recognition or machine learning using neural networks
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
58.
COMBINED USE OF ANTI-CCR8 ANTIBODY AND CHEMOTHERAPEUTIC AGENT
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
SHIONOGI & CO., LTD. (Japan)
Inventor
Nagata Satoshi
Kamada Haruhiko
Ise Tomoko
Furukawa Kentaro
Takahashi Tatsuya
Shishido Takao
Fukao Keita
Yoshikawa Mai
Ota Takeshi
Takayama Masahiro
Tsugawa Yoji
Ogura Keiji
Maeda Kousuke
Abstract
The purpose of the present invention is to provide: a novel monoclonal antibody against S2 subunit of a spike protein of SARS-CoV-2; and a pharmaceutical composition containing said antibody for prevention or treatment of corona virus infectious diseases. An antibody according to the present invention was found by producing various antibodies using the S2 subunit of the spike protein of SARS-CoV- 2 as an antigen, which led to the completion of the present invention. This monoclonal antibody can be used for prevention or treatment of corona virus infectious diseases.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
61.
LYOPHILIZED FORMULATION CONTAINING CEPHALOSPORIN HAVING CATECHOL GROUP AND THE MANUFACTURING METHOD
The present invention relates to a method for manufacturing a lyophilized formulation which comprises a compound represented by Formula (I) shown below, or its pharmaceutically acceptable salt, wherein the water content is controlled and the reconstitution time is short; and a lyophilized formulation. With a method for manufacturing a lyophilized formulation comprising: 1) cooling a liquid comprising the compound represented by Formula (I) or its pharmaceutically acceptable salt in a chamber of a lyophilizer, to a determined cooling temperature, and 2) spraying mist into the chamber, a lyophilized formulation having a specific surface area of 0.6 to 1.1 m2/g can have a water content of 0.5% or less, and a reconstitution time can be 30 seconds or less.
The present invention relates to a method for manufacturing a lyophilized formulation which comprises a compound represented by Formula (I) shown below, or its pharmaceutically acceptable salt, wherein the water content is controlled and the reconstitution time is short; and a lyophilized formulation. With a method for manufacturing a lyophilized formulation comprising: 1) cooling a liquid comprising the compound represented by Formula (I) or its pharmaceutically acceptable salt in a chamber of a lyophilizer, to a determined cooling temperature, and 2) spraying mist into the chamber, a lyophilized formulation having a specific surface area of 0.6 to 1.1 m2/g can have a water content of 0.5% or less, and a reconstitution time can be 30 seconds or less.
A61K 9/19 - Particulate form, e.g. powders lyophilised
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Tachibana, Yuki
Uehara, Shota
Unoh, Yuto
Nakahara, Kenji
Taoda, Yoshiyuki
Yamatsu, Yukiko
Ando, Shigeru
Sasaki, Michihito
Abstract
The present invention provides a compound exhibiting coronavirus 3 CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.
A compound represented by Formula:
or a pharmaceutically acceptable salt thereof.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
63.
PHARMACEUTICAL COMPOSITION FOR TREATING FATTY LIVER DISEASE
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
wherein
R1 is haloalkyl or non-aromatic carbocyclyl,
R2 is a hydrogen atom or halogen,
R3 is halogen,
ring A is a group represented by the formula:
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
wherein
R1 is haloalkyl or non-aromatic carbocyclyl,
R2 is a hydrogen atom or halogen,
R3 is halogen,
ring A is a group represented by the formula:
-L1- is —O—(CH2)—, —(CH2)2—, or the like,
R4 is alkyl or haloalkyl, and
R5 is alkylcarbonyl or carbamoyl,
or a pharmaceutically acceptable salt thereof.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
64.
USE OF OPIOID FOR TREATMENT OF AUTISM SPECTRUM DISORDERS
Provided are a novel pharmaceutical composition and method for treating and/or preventing autism spectrum disorders, fragile X syndrome, and/or autism spectrum disorder-like symptoms. Specifically provided is a pharmaceutical composition for treating and/or preventing autism spectrum disorders, fragile X syndrome, and/or autism spectrum disorder-like symptoms, the composition containing: buprenorphine or a pharmaceutically acceptable salt thereof; and/or morphine or a pharmaceutically acceptable salt thereof.
The signal processing apparatus receives an input acoustic signal, and amplitude-modulates the received input acoustic signal to generate an output acoustic signal having an amplitude change corresponding to a frequency of a gamma wave, and outputs the generated output acoustic signal.
G10H 7/02 - Instruments in which the tones are synthesised from a data store, e.g. computer organs in which amplitudes at successive sample points of a tone waveform are stored in one or more memories
66.
SIGNAL PROCESSING APPARATUS AND SIGNAL PROCESSING METHOD
A signal processing apparatus receives an input acoustic signal, acquires a first acoustic signal having a periodic variation corresponding to the frequency of gamma waves, and outputs an output acoustic signal based on the acquired first acoustic signal and the second acoustic signal. The second acoustic signal is based on the input acoustic signal.
A61B 5/374 - Detecting the frequency distribution of signals, e.g. detecting delta, theta, alpha, beta or gamma waves
G10H 7/02 - Instruments in which the tones are synthesised from a data store, e.g. computer organs in which amplitudes at successive sample points of a tone waveform are stored in one or more memories
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
09 - Scientific and electric apparatus and instruments
10 - Medical apparatus and instruments
30 - Basic staples, tea, coffee, baked goods and confectionery
31 - Agricultural products; live animals
32 - Beers; non-alcoholic beverages
35 - Advertising and business services
40 - Treatment of materials; recycling, air and water treatment,
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Acids; salts [chemical preparations]; salts [fertilisers];
salts for industrial purposes; alkalies; bleaching
preparations, not for laundry use; bleaching preparations
[decolorants] for industrial purposes; gum arabic; gum
arabic for industrial purposes; glue for industrial
purposes; phosphorus; ethyl alcohol; glycerine; glycerine
for industrial purposes; sulfur; oxygen; oxygen for
industrial purposes; enzymes for industrial purposes;
camphor; camphor oil for industrial purposes; camphor, for
industrial purposes; distilled water; carbonic acid gas;
peppermint oil for industrial purposes; disinfectants for
industrial purposes; biological preparations, other than for
medical or veterinary purposes; dendrimer-based polymers for
use in the manufacture of capsules for pharmaceuticals;
chemicals; industrial chemicals; chemical preparations for
scientific purposes, other than for medical or veterinary
use; vitamins for use in the manufacture of pharmaceuticals;
plant extracts for use in the manufacture of
pharmaceuticals; antioxidants for use in the manufacture of
pharmaceuticals; preservatives for use in the pharmaceutical
industry; proteins for use in the manufacture of food
supplements; chemical reagents kit; glue and adhesives for
industrial purposes; plant growth regulating preparations;
plant food; ceramic glazings; oil cement [putty]; higher
fatty acids; non-metallic minerals; chemical compositions
for use in developing photographs; reagent paper [not for
medical purposes]; artificial sweeteners; flour and starch
for industrial purposes; unprocessed plastics in primary
form; groundwood pulp or chemical pulps for manufacturing
purposes; detergents for industrial use as part of
manufacturing operations; chemicals used in horticulture. Soaps and detergents; shampoos; facial washes; skin
cleansers; non-medicated skin care preparations; gargles,
not for medical purposes; mouthwashes, not for medical
purposes; hand cleaning preparations; preparations for
cleaning dentures; detergents, other than for use in
manufacturing operations and for medical purposes;
preparations for laundry sterilization; cosmetic
preparations; cosmetic preparations for hair care and scalp
care; hair nourishers; cosmetic scalp care preparations
having hair-growing effect; dentifrices; perfume and flavour
materials; incense; perfumes; natural perfumery prepared
from vegetables; natural perfumery prepared from animals;
synthetic perfumery; blended perfumery; food flavorings
prepared from essential oils; laundry fabric conditioner;
laundry bleaching preparations; antistatic preparations for
household purposes; degreasing preparations for household
purposes; rust removing preparations; stain removing
benzine; adhesives for affixing false hair; starch for
laundry purposes; seaweed gelatine for laundry use;
adhesives for affixing false eyelashes; breath freshening
preparations; deodorants for animals; paint removing
compositions; shoe and boot cream; shoe black [shoe polish];
polishing powder; abrasive paper; abrasive cloth; abrasive
sand; pumice stone; polishing paper; false nails; false
eyelashes; cotton sticks for cosmetic purposes; hair tonic. Pharmaceutical preparations and other preparations for
destroying vermin, fungicides, herbicides; medicines for
human purposes; drugs for medical purposes; pharmaceutical
preparations and substances; pharmaceutical preparations and
other preparations for destroying vermin, fungicides,
herbicides in the form of jelly; pharmaceutical products for
the treatment of COVID-19; vaccines against COVID-19;
vaccines; antivirals; anti-cancer preparations; vitamin
preparations and substances; chemico-pharmaceutical
preparations; biological preparations for medical purposes;
biological preparations for veterinary purposes; detergents
for medical purposes; medicated toiletry preparations;
nutritional supplements for boosting energy; liquid
nutritional supplements for boosting energy; disinfectants;
bactericides; sterilizing preparations other than for
industrial and laundry purposes; wet wipes impregnated with
sterilizing preparations; sanitizers for hands and fingers;
medicinal preparations for stimulating hair growth;
medicinal hair growth preparations; diagnostic reagent kit
for medical use; quinine for medical purposes; analgesic
preparations; tinctures for medical purposes; syrup for
pharmaceutical purposes; decoctions for pharmaceutical
purposes; medicinal infusions; medical plasters; crude
drugs, charred drugs and moxa; lime-based pharmaceutical
preparations; flowers of sulfur for pharmaceutical purposes;
sulfur sticks for use as disinfectants; antiseptics [only
for agricultural purposes]; deodorants, other than for human
being and for animals; antiparasitics; chemical reagents for
medical or veterinary purposes; reagent paper for medical
purposes; oiled paper for medical purposes; adhesive tapes
for medical purposes; drug delivery agents in the form of
edible wafers for wrapping pharmaceuticals; drug delivery
agents in the form of edible jelly for wrapping
pharmaceuticals; drug delivery agents in the form of edible
liquid for wrapping pharmaceuticals; gauze for dressings;
empty capsules for pharmaceuticals; eyepatches for medical
purposes; ear bandages; menstruation bandages; sanitary
tampons; sanitary napkins; sanitary panties; adhesive
plasters; absorbent cotton; materials for dressings; liquid
bandages; breast-nursing pads; cotton swabs for medical use;
cotton sticks for medical purposes; dental materials;
surgical implants comprised of living tissues; denture
adhesive; diapers; diaper covers; fly catching paper;
mothproofing paper; lacteal flour for babies; dietary
supplements consisting of amino acids and vitamins in the
form of balls, powder, granules, particulate, tablets,
capsules, liquid, cream, paste, gel, jelly, solid, plates,
and sheets, or filled capsules; dietary supplements
consisting of green juice in the form of balls, powder,
granules, particulate, tablets, capsules, liquid, cream,
paste, gel, jelly, solid, plates, and sheets, or filled
capsules; dietary supplements consisting of mushroom extract
in the form of balls, powder, granules, particulate,
tablets, capsules, liquid, cream, paste, gel, jelly, solid,
plates, and sheets, or filled capsules; dietary and
nutritional supplements; dietary supplements for humans;
dietary supplements in the form of jelly; dietary fiber;
dietetic beverages adapted for medical purposes; dietetic
foods adapted for medical purposes; beverages for babies;
food for babies; dietary supplements for animals; semen for
artificial insemination; bacterial preparations for medical
and veterinary use; first-aid boxes, filled; menthol
[peppermint]; throat lozenge. Graduated glassware; laboratory apparatus and instruments;
research laboratory analyzers for measuring, testing and
analyzing blood and other bodily fluids; chemistry apparatus
and instruments; measuring or testing machines and
instruments; water meters; precision measuring machines and
instruments; measuring instruments; nanoparticle size
analysers; dosage dispensers; dosimeters; optical machines
and apparatus; photographic apparatus and instruments;
cinematographic apparatus and instruments; humanoid robots
with artificial intelligence for use in scientific research;
phase modifiers; power distribution or control machines and
apparatus; rotary converters; solar cells; electrical cells
and batteries; electric or magnetic meters and testers;
conductors, electric; electrical communication machines and
instruments; personal digital assistants; straps for
personal digital assistants; computers and their
peripherals; computer programs; software as a medical device
[SaMD], downloadable; computer operating programs, recorded;
computer software, recorded; computer software applications,
downloadable; computer programs, recorded; computer
programs, downloadable; computer software in the field of
artificial intelligence; computers with artificial
intelligence and their parts and fittings; computers
[including for use in robots] with artificial intelligence
and their parts and fittings; teaching robots; telepresence
robots; humanoid bipedal robots for use in scientific
research; mouse pads; ozonisers [ozonators]; electrolysis
apparatus for laboratory use; fire extinguishers; fire
hoses; fire hose nozzles; sprinkler systems for fire
protection; fire alarms; gas leak alarm systems; burglar
alarms; safety helmets; electrodes; magnetic cores;
resistance wires; dust masks; gas masks; welding masks;
disaster prevention hoods; fireproof garments; gloves for
protection against accidents; eyewear; consumer video game
programs; electronic circuits and CD-ROMs recorded with
programs for hand-held games with liquid crystal displays;
sound recordings, music, graphics, images, motion pictures
and text data downloadable via the Internet; still and
moving images for stickers downloadable via the Internet;
audio and video recordings; recorded video discs and video
tapes; electronic publications; electronic publications,
downloadable; exposed cinematographic films; slide film,
exposed; slide film mounts; ear plugs for swimmers; ear
plugs for divers; egg-candlers; blueprint apparatus; cash
registers; coin counting or sorting machines; photocopying
apparatus; mathematical instruments; time and date stamping
machines; time clocks [time recording devices]; punched card
office machines; voting machines; postage stamp checking
apparatus; coin-operated mechanisms for operating gates for
car parking lots; life-saving apparatus and equipment;
railway signals; vehicle breakdown warning triangles; road
signs, luminous or mechanical; breathing apparatus for
underwater swimming; weight belts for divers; compressed air
bailout units for diving, not for sports; diving goggles;
diving helmets; buoyancy compensator devices for divers, not
for sports; nose clips for divers, not for sports; game
programs for arcade video game machines; vehicle driving
simulators for training purposes; sports training
simulators; fire boats; satellites for scientific purposes;
fire trucks; protective helmets for sports; sports whistles;
weight belts for scuba diving; air tanks [for scuba diving];
snorkels; regulators for scuba diving; metronomes;
electronic circuits and CD-ROMs recorded with automatic
performance programs for electronic musical instruments;
electric and electronic effects units for musical
instruments. Medical apparatus and instruments; apparatus for DNA and RNA
testing for medical purposes; apparatus for use in medical
analysis; diagnostic apparatus for medical purposes in a
form of testing kit; water ionizers for medical purposes;
sanitary masks; pacifier clips; ice bag pillows for medical
purposes; triangular bandages; support bandages; catgut;
feeding cups for medical purposes; dropping pipettes for
medical purposes; teats; nipples for baby bottles; medical
ice bags; medical ice bag holders; baby bottles; nursing
bottles; contraceptive devices; artificial tympanic
membranes; prosthetics or fillings materials, not for dental
use; ear plugs for sleeping; ear plugs for protection
against noise; ear plugs [hearing protection devices];
esthetic massage apparatus for commercial use; facial
aesthetic treatment apparatus using ultrasonic waves for
household purposes; electric massage apparatus for household
purposes; gloves for medical purposes; urinals for medical
purposes; bed pans; ear picks. Cereals, processed; granola; noodles; oat flakes; oatmeal;
couscous; croutons; corn flakes; cereal bars; pasta; crumb;
tea; tea beverages; tea substitutes; flowers or leaves for
use as tea substitutes; coffee; instant coffee; coffee
beverages; coffee substitutes; cocoa; binding agents for ice
cream; meat tenderizers for household purposes; preparations
for stiffening whipped cream; aromatic preparations for
food; essences for foodstuffs, except etheric essences and
essential oils; ice; grain based, chocolate based sweets,
desserts and snacks other than fruit-based, vegetable-based,
bean-based or nut-based; jelly confectionery; confectionery;
bread; sandwiches; steamed buns stuffed with minced meat
[chuka-manjuh]; hamburgers [sandwiches]; fresh pizzas; hot
dogs [sandwiches]; meat pies; cereal-based snack food;
rice-based snack food; chips [cereal products]; seasonings
[other than spices]; natural sweeteners; spices; ice cream
mixes; sherbet mixes; unroasted coffee; chocolate spread;
garden herbs, preserved [seasonings]; fruit coulis [sauces];
Chinese stuffed dumplings; Chinese steamed dumplings; sushi;
fried balls of batter mix with small pieces of octopus
[takoyaki]; boxed lunches consisting of rice, with added
meat, fish or vegetables; ravioli; yeast powder; koji
[fermented malted rice]; yeast; baking powder; malt for
human consumption; malt extract for food; instant
confectionery mixes; pasta sauce; by-product of rice for
food [sake lees]; propolis; royal jelly; rice; husked oats;
husked barley; wheat germ for human consumption; gluten for
food; flour; soya flour. Edible aquatic animals, live; fish, live; fish spawn;
shellfish, live; edible seaweeds, unprocessed; seaweed,
unprocessed, for human or animal consumption; vegetables,
fresh; sugar crops; fruit, fresh; nuts, unprocessed; malt;
foxtail millet, unprocessed; proso millet, unprocessed;
sesame, unprocessed; buckwheat, unprocessed; maize; corn
[unprocessed grain]; corn [fresh vegetables]; maize cake for
cattle; Japanese barnyard millet, unprocessed; wheat, barley
and oats, unprocessed; rice, unprocessed; sorghum; wreaths
of natural flowers for ceremonies or funerals; fishing
baits; hops; protein foodstuffs for animal consumption;
animal foodstuffs; seeds and bulbs; cereal seeds,
unprocessed; plants; trees; grasses [plants]; turf, natural;
dried flowers; flowers, dried, for decoration; seedlings;
saplings; flowers [natural]; pasture grass; natural bonsai
trees; live mammals, fish [not for food], birds and insects;
silkworm eggs; cocoons for egg production; eggs for
hatching; urushi tree seeds; rough cork; palm fronds;
undressed timber; trunks of trees; malt for brewing and
distilling; straw litter. Soft drinks; carbonated drink mixes; soft drinks in the form
of jelly; table waters; drinking water; non-alcoholic fruit
extracts; fruit beverages and fruit juices; fruit beverages
and fruit juices in the form of jelly; vegetable juices
[beverages]; vegetable beverages and vegetable juices in the
form of jelly; syrups for beverages; energy drinks;
protein-enriched sports beverages; soya-based beverages,
other than milk substitutes; soda water; pastilles for
effervescing beverages; powders for effervescing beverages;
green juice bases in the form of powder; green vegetables
based green juices; fruit juice concentrates; concentrated
fruit juices; concentrates for making fruit drinks;
concentrates used in the preparation of soft drinks; whey
beverages; whey beverages in the form of jelly;
non-alcoholic beverages flavored with coffee; non-alcoholic
beverages flavored with tea; cocktails, non-alcoholic;
non-alcoholic beverages; preparations for making
non-alcoholic beverages; beers; extracts of hops for making
beer; starch-based dry mixes for beverage preparation;
non-alcoholic essences for making beverages. Office functions; data processing services [office
functions]; business invoicing services; office functions
for others; copying of documents; office functions, namely
filing, in particular documents or magnetic tapes;
compilation of information into computer databases;
management of computerised digital data files; import-export
agency services; advertising and publicity services; rental
of advertising space and advertising material; rental of
advertising space; rental of sales stands; online
advertising on a computer network; conducting of commercial
events; organization of trade fairs; promoting the goods and
services of others through the administration of sales and
promotional incentive schemes involving trading stamps;
business management of sports people; administrative
services for medical referrals; administration of business
affairs; provision of business information; providing
commercial and business contact information; providing
business information via a website; business consulting
services for digital transformation; merchandising;
administrative processing of orders; providing information
concerning commercial sales; provision of an online
marketplace for buyers and sellers of goods and services;
advisory and information services relating to commercial
transactions; commercial intermediation services; business
management analysis or business consultancy; marketing
research or analysis; market intelligence services;
sponsorship search; presentation of goods on communication
media, for retail purposes; promoting the sale of goods and
services of others; marketing in the framework of software
publishing; promotion of goods and services through
sponsorship of sports events; marketing services; job
placement services; medical doctor referral; nurse referral;
dentist referral; midwife referral; pharmacist referral;
referral of scientific or technological experts; providing
commercial information and advice for consumers in the
choice of products and services; providing employment
information; news clipping services to provide information
about newspaper articles; rental of vending machines;
preparation of financial statements; conducting of auction
sales; arranging newspaper subscriptions for others;
shorthand secretarial services; transcription; providing
business assistance to others in the operation of data
processing apparatus namely, computers, typewriters, telex
machines and other similar office machines; reception
services for visitors in buildings [office functions];
rental of typewriters, copying machines; retail services or
wholesale services for pharmaceutical, veterinary and
sanitary preparations and medical supplies; retail services
or wholesale services for electrical machinery and
apparatus; retail services or wholesale services for woven
fabrics and bedding; retail services or wholesale services
for clothing; retail services or wholesale services for
diapers; retail services or wholesale services for footwear;
retail services or wholesale services for bags and pouches;
retail services or wholesale services for wet paper wipes;
retail services or wholesale services for non-woven hand
wipes [used as paper wipes]; retail services or wholesale
services for wet non-woven wipes [used as wet paper wipes];
retail services or wholesale services for personal articles;
retail services or wholesale services for combs and hair
tinting brushes; retail services or wholesale services for
hair dye gloves; retail services or wholesale services for
food and beverages; retail services or wholesale services
for dietary supplements; retail services or wholesale
services for processed seafood products; retail services or
wholesale services for edible shavings of dried kelp
[tororo-kombu]; retail services or wholesale services for
mushroom extract for food and culinary purposes; retail
services or wholesale services for cosmetics, toiletries,
dentifrices, soaps and detergents; retail services or
wholesale services for bladed or pointed hand tools, hand
tools and metal hardware; retail services or wholesale
services for kitchen equipment, cleaning tools and washing
utensils; retail services or wholesale services for printed
matter; retail services or wholesale services for paper and
stationery; retail services or wholesale services for sports
goods; retail services or wholesale services for toys,
dolls, game machines and apparatus; retail services or
wholesale services for clocks, watches, spectacles,
eyeglasses and goggles; retail services or wholesale
services for tobacco and smokers' articles; online retail
services for downloadable and pre-recorded music and movies;
online retail services for downloadable digital music;
retail services or wholesale services for automobiles;
retail services or wholesale services for two-wheeled motor
vehicles; retail services or wholesale services for
bicycles; retail services or wholesale services for
furniture; retail services or wholesale services for joinery
fittings; retail services or wholesale services for tatami
mats; retail services or wholesale services for ritual
equipment; retail services or wholesale services for
agricultural machines, implements and supplies; retail
services or wholesale services for flowers [natural] and
trees; retail services or wholesale services for fuel;
retail services or wholesale services for musical
instruments and records; retail services or wholesale
services for photographic machines and apparatus and
photographic supplies; retail services or wholesale services
for building materials; retail services or wholesale
services for semi-wrought precious stones and their
imitations; retail services or wholesale services for pets. Custom manufacture of pharmaceuticals; custom manufacturing
of make-up; custom manufacture of medical devices for
others; custom assembling of materials for others; custom
manufacture of biopharmaceuticals; processing of medicinal
materials; processing of chemicals and petrochemicals;
processing of chemical reagents; chemical encapsulation and
dispersion of hazardous chemicals; custom manufacture of
products for the pharmaceutical, chemical and food
industries by compressing and compacting powders and
granules; custom manufacturing of dietary supplements for
humans; providing material treatment information; processing
of bamboo, tree barks, rattan, vines or other mineral
vegetable materials, other than processing of ingredients;
processing of raw materials for the manufacture of food and
beverages; food processing; processing of artificial limbs
or artificial teeth, including processing of medical
materials; recycling of chemicals; processing and recycling
of waste and trash; treatment of waste and harmful
substances; sorting and disposal of waste and trash; removal
of radiation rays; consultancy or providing information
relating to removal of radiation rays; rental of industrial
robots for use in manufacturing; drying of cloth, clothing
or fur; treatment or processing of cloth, clothing or fur,
including drying; application of coatings using chemical,
mechanical, thermal or thermomechanical processes;
metalworking; processing of rubber; processing of plastics;
ceramic processing; timber processing; paper treating and
working; stone treating; custom 3D printing for others;
waste water reprocessing; water treating; printing; offset
printing; photogravure printing; screen printing;
lithographic printing; letterpress printing; customized
printing of company names and logos for promotional and
advertising purposes on the goods of others; rental of
chemical processing machines and apparatus; rental of
knitting machines; rental of sewing machines; rental of
printing machines and apparatus; sewing; embroidering;
taxidermy; processing of cinematographic films; photographic
enlarging; photographic printing; processing of photographic
films; bookbinding; reprocessing of nuclear fuels; engraving
of sealing stamps; photogravure; rental of machines and
apparatus for treating textiles; rental of machines and
apparatus for film development, photograph printing,
photograph enlargement or photograph finishing; rental of
metal treating machines and tools; rental of bookbinding
machines; rental of machines and apparatus for processing
foods or beverages; rental of machines and apparatus for
lumbering, wood-working, or veneering or plywood making;
rental of machines and apparatus for pulp-making,
papermaking or paper-working; rental of water purifying
apparatus; rental of waste compacting machines and
apparatus; rental of waste crushing machines and apparatus;
rental of glassware manufacturing machines and apparatus;
rental of machines for making shoes; rental of tobacco
processing machines; rental of 3D printers; rental of
air-conditioning apparatus for household purposes; rental of
humidifier for household purposes; rental of air purifiers
for household purposes; rental of electricity generators;
rental of boilers; rental of humidifier for industrial
purposes; rental of air purifiers for industrial purposes;
rental of air conditioners for industrial purposes. Pharmaceutical training and teaching; medical training and
teaching; vocational education and training services;
teaching; educational and instruction services relating to
arts, crafts, sports or general knowledge; providing
information in the field of education; tutoring; arranging,
conducting and organization of seminars; arranging and
conducting of seminars; arranging, conducting and
organization of symposiums; arranging and conducting of
in-person educational forums; organization, arranging and
conducting of seminars, workshops, in-person educational
forums, symposiums, conferences, academic conferences and
study groups; publishing services; publication of journals,
books and handbooks in the field of medicine; publication of
scientific papers in relation to medical technology;
publication of the results of clinical trials for
pharmaceutical preparations; on-line publication of
electronic books and periodicals; providing information on
donation of human corpses for medical education; arranging
of donation of human corpses for medical education;
providing electronic publications; reference libraries of
literature and documentary records; book rental; providing
online electronic publications, not downloadable; providing
information in the field of entertainment; arranging and
planning of movies, shows, plays or musical performances;
movie theatre presentations or movie film production and
distribution; providing online music, not downloadable;
providing online videos, not downloadable; providing films,
not downloadable, via video-on-demand transmission services;
providing television programs, not downloadable, via
video-on-demand services; providing online non-downloadable
music, audio, videos, images and texts via the internet;
presentation of live show performances; direction or
presentation of plays; presentation of musical performances;
production of radio or television programs; video
production; production of videotape film in the field of
education, culture, entertainment or sports [not for movies
or television programs and not for advertising or
publicity]; directing of radio and television programs;
operation of video and audio equipment for the production of
radio and television programs; arranging and conducting of
sports events; sporting activities; organization of
entertainment events excluding movies, shows, plays, musical
performances, sports, horse races, bicycle races, boat races
and auto races; providing audio or video studio services;
providing exercise facilities; providing amusement
facilities; game services provided online from a computer
network; providing facilities for movies, shows, plays,
music or educational training; photography; language
interpretation; language translation; rental of cameras;
rental of cinematographic apparatus; rental of binoculars
for watching sports events; rental of telescopes for leisure
activities; lottery services; dubbing; animal training;
plant exhibitions; animal exhibitions; art exhibitions;
providing gardens for public admission; caves for public
admission; organization, arranging and conducting of horse
races; organization, arranging and conducting of bicycle
races; organization, arranging and conducting of boat races;
organization, arranging and conducting of motorcycle races;
booking of seats for shows; rental of cinematographic
apparatus; rental of cine-films; rental of musical
instruments; rental of sports equipment; rental of
television sets; rental of radio sets; rental of records or
sound-recorded magnetic tapes; rental of image-recorded
magnetic tapes; rental of film negatives; rental of reversal
film; toy rental; rental of amusement machines and
apparatus; rental of game machines and apparatus; rental of
paintings and calligraphic works. Development of pharmaceuticals and providing information
relating thereto; pharmaceutical research services and
providing information relating thereto; stability testing,
inspection or research of pharmaceutical products and
providing information relating thereto; quality testing,
inspection or research of pharmaceutical products and
providing information relating thereto; physicochemical
testing, inspection or research of pharmaceutical products
and providing information relating thereto; microbial
testing, inspection or research of pharmaceutical products
and providing information relating thereto; testing,
inspection or research of materials, intermediates and final
products of pharmaceutical products and providing
information relating thereto; testing, inspection or
research of analysis method of pharmaceutical products and
providing information relating thereto; testing, inspection
or research of pharmaceutical products and providing
information relating thereto; testing, inspection or
research of surface analysis of pharmaceutical products and
providing information relating thereto; testing, inspection
or research of chemicals, pharmaceuticals, agrochemicals,
cosmetics and foodstuffs and providing information relating
thereto; pharmaceutical product evaluation and providing
information relating thereto; providing information about
medical and scientific research in the field of
pharmaceuticals; medical research and providing information
relating thereto; research and development of medical
technology and providing information relating thereto;
scientific and medical research and development and
providing information relating thereto; scientific research
and development; technological research; research in the
fields of chemistry, biology and physics; chemical testing,
inspection, analysis or research; agrochemical research
services; research and development of new products; product
quality testing; quality control; conducting technical
project studies; technical writing; technical measuring and
testing services; research and development services relating
to measuring and regulating technology; development of
measuring and testing methods; calibration of medical
apparatus; testing or research on machines, apparatus and
instruments; design services; industrial design; packaging
design; designing of machines, apparatus, instruments
[including their parts] or systems composed of such
machines, apparatus and instruments; design and development
of medical diagnostic apparatus; architectural design;
engineering; plant engineering; information technology [IT]
consultancy; surveying; geological surveys or research;
consultancy in the field of scientific and industrial
research; computer software design, computer programming, or
maintenance of computer software; computer system analysis;
design, programming and maintenance of computer software;
rental of computer software; computer programming in the
medical field; design and development of computer software
for use with medical technology; advisory services relating
to computer software; technological advice relating to
computers, automobiles and industrial machines; testing or
research on prevention of pollution; research on building
construction or city planning; testing or research on
electricity; testing or research on civil engineering;
research in the field of environmental protection; material
testing; water analysis; testing, inspection or research on
agriculture, livestock breeding or fisheries; rental of
measuring apparatus; electronic storage of medical records;
rental of computers; providing computer programs on data
networks; software as a service [SaaS]; platform as a
service [PaaS]; cloud computing; rental of laboratory
apparatus and instruments; rental of technical drawing
instruments; providing meteorological information; rental of
word processors. Provision of medical information; providing information to
patients in the field of administering medication; health
care; consultancy, advisory and information services
relating to healthcare; providing information relating to
medical practice; providing information relating to
dentistry; providing information relating to the preparation
and dispensing of medications; pharmacy advice; providing
information and advice relating to pharmaceuticals;
providing information and advice relating to pharmaceuticals
and medical products; medical treatment; consultancy,
advisory and information services relating to medical
treatment; paramedical services; consultancy, advisory and
information services relating to paramedical services;
medical diagnostic services [testing and analysis]; medical
diagnostic services of virus infectious disease; medical
counseling and diagnostic services provided via Internet;
testing and analysis of human blood and feces for clinical
laboratory purposes; cultured cell bank services for medical
transplantation and providing information relating thereto;
remote monitoring of medical data for medical diagnosis and
treatment and providing information relating thereto; blood
bank services and providing information relating thereto;
medical analysis services for diagnostic and treatment
purposes provided by medical laboratories and providing
information relating thereto; palliative care; consultancy,
advisory and information services relating to palliative
care; human tissue bank services and providing information
relating thereto; therapy services; consultancy, advisory
and information services relating to therapy services;
alternative medicine services; consultancy, advisory and
information services relating to alternative medicine
services; rehabilitation for substance abuse patients;
consultancy, advisory and information services relating to
rehabilitation for substance abuse patients; physical
examination and providing information relating thereto;
dietary and nutritional guidance and providing information
relating thereto; advisory services relating to nutrition;
postnatal care services; consultancy, advisory and
information services relating to postnatal care services; in
vitro fertilisation services and providing information
relating thereto; artificial insemination services and
providing information relating thereto; rental of medical
machines and apparatus; rental of ultrasonic diagnostic
apparatus; rental of medical X-ray apparatus; rental of
surgical robots; beauty treatment services and providing
information relating thereto; barbershops and providing
information relating thereto; massage and therapeutic
shiatsu massage and providing information relating thereto;
chiropractic and providing information relating thereto;
moxibustion and providing information relating thereto;
treatment for dislocated joints, sprain, bone fractures
[judo-seifuku] and providing information relating thereto;
bodywork therapy and providing information relating thereto;
acupuncture and providing information relating thereto;
nursing care and providing information relating thereto;
animal breeding and providing information relating thereto;
veterinary services and providing information relating
thereto; animal grooming and providing information relating
thereto; pet grooming and providing information relating
thereto; veterinary assistance and providing information
relating thereto; provision of bath houses and providing
information relating thereto; garden tree planting and
providing information relating thereto; garden or flower bed
care and providing information relating thereto; spreading
of fertilizers and providing information relating thereto;
weed control and providing information relating thereto;
vermin exterminating [for agriculture, aquaculture,
horticulture or forestry] and providing information relating
thereto; rental of potted plants; rental of fishing
equipment and instruments for commercial fishing purposes;
rental of machines and apparatus for use in beauty salons or
barbers' shops; rental of lawnmowers; farming equipment
rental; landscape design.
68.
AROMATIC HETEROCYCLIC DERIVATIVE HAVING GLP-1 RECEPTOR AGONIST ACTIVITY
The present invention pertains to: a compound, or a pharmacologically acceptable salt thereof, having GLP-1 receptor agonist activity and offering utility as an agent for treating or preventing diseases involving GLP-1 receptors; and a pharmaceutical composition containing the compound and the pharmacologically acceptable salt. A compound or a pharmaceutically acceptable salt thereof, the compound being represented by formula (IA) (where: R1is an optionally substituted alkyl group; R2is a group represented by BB; X is N, etc.; L is a group represented by CC (where: R8is a hydrogen atom, etc.; R9is a halogen, etc.; each of Z1and Z2is independently N, etc.; the atom labelled a bonds to a group represented by DD; and the atom labelled b bonds to a group represented by EE); W is N, etc.; R11is a hydrogen atom, etc.; each of R12and R13is independently a hydrogen atom, etc.; and each of R14and R15 is independently a hydrogen atom, etc.).
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
69.
PHARMACEUTICAL COMPOSITION IN WHICH PRODUCTION OF IMPURITIES IS SUPPRESSED
By wet-pulverizing a compound represented by Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (hereinafter referred to as a compound represented by Formula (I) or the like), it is possible to provide a crystal of the compound represented by Formula (I) or the like and a pharmaceutical composition containing the same having excellent stability.
By wet-pulverizing a compound represented by Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (hereinafter referred to as a compound represented by Formula (I) or the like), it is possible to provide a crystal of the compound represented by Formula (I) or the like and a pharmaceutical composition containing the same having excellent stability.
In addition, by wet-kneading and/or wet-granulating the compound represented by Formula (I) or the like, it is possible to provide a pharmaceutical composition containing the compound represented by Formula (I) or the like having excellent stability.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A pharmaceutical composition containing the substance according to any one of the following (a) to (c), an organic acid, a metal salt of an organic acid, and a sugar and/or a sugar alcohol, wherein when the pharmaceutical composition is dissolved in distilled water for injection, a pH of the pharmaceutical composition is 3.0 to 4.5, the substance according to any one of the following (a) to (c) can be stabilized;
(a) an HMGB1 fragment peptide comprising the amino acid sequence set forth in SEQ ID NO: 1 or an acid addition salt thereof;
(b) a peptide comprising an amino acid sequence having substitution, deletion, insertion or addition of one or more amino acids in the amino acid sequence set forth in SEQ ID NO: 1, and having an activity of stimulating migration of a cell, or an acid addition salt thereof; and
(c) a peptide comprising an amino acid sequence having about 80% or more of sequence identity to the amino acid sequence set forth in SEQ ID NO: 1, and having an activity of stimulating migration of a cell, or an acid addition salt thereof.
The present invention provides a medicine useful for treating and/or preventing COVID-19. Provided is a medicine characterized by combining: (A) a compound represented by formula (I) (where: Y is N; R1represents an optionally substituted aromatic heterocyclic group; R2represents an optionally substituted 6-membered aromatic carbon ring group; R3represents an optionally substituted aromatic heterocyclic group; -X- is -NH-; m is 0 or 1; R5arepresents a hydrogen atom; R5brepresents a hydrogen atom; n is 1; R4arepresents a hydrogen atom; and R4b represents a hydrogen atom) or a pharmaceutically acceptable salt thereof; and (B) a COVID-19 aggravation inhibitor.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to a pharmaceutical composition comprising a P2X3 and/or P2X2/3 receptor antagonist for the treatment of neuropathic pain, nociceptive pain or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome.
The present invention relates to a pharmaceutical composition comprising a P2X3 and/or P2X2/3 receptor antagonist for the treatment of neuropathic pain, nociceptive pain or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome.
It is a pharmaceutical composition for treating and/or preventing neuropathic pain, nociceptive pain, or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome, comprising a compound represented by Formula (I):
The present invention relates to a pharmaceutical composition comprising a P2X3 and/or P2X2/3 receptor antagonist for the treatment of neuropathic pain, nociceptive pain or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome.
It is a pharmaceutical composition for treating and/or preventing neuropathic pain, nociceptive pain, or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome, comprising a compound represented by Formula (I):
The present invention relates to a pharmaceutical composition comprising a P2X3 and/or P2X2/3 receptor antagonist for the treatment of neuropathic pain, nociceptive pain or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome.
It is a pharmaceutical composition for treating and/or preventing neuropathic pain, nociceptive pain, or visceral pain, as well as interstitial cystitis and/or bladder pain syndrome, comprising a compound represented by Formula (I):
or a pharmaceutically acceptable salt thereof.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 25/04 - Centrally acting analgesics, e.g. opioids
73.
PHARMACEUTICAL FOR TREATING HEART DISEASE OR SKELETAL MUSCLE DISEASE
Provided is a pharmaceutical composition for treating and/or preventing at least one among heart disease, heart disease complications, skeletal muscle disease, and skeletal muscle disease conditions, the pharmaceutical composition having excellent ACC2-selective inhibitory action without accompanying side effects such as an increase in plasma triglycerides or a decrease in platelet concentration. The pharmaceutical composition for treating and/or preventing at least one among heart disease, heart disease complications, skeletal muscle disease, and skeletal muscle disease conditions, the pharmaceutical composition containing the compound represented by formula (I) or a pharmaceutically acceptable salt thereof. Formula (I): chemical formula 1 (in the formula, R1is a haloalkyl or non-aromatic carbocyclic group, R2is a hydrogen atom or a halogen, R3is a halogen, ring A is a group represented by formula: chemical formula 2, －L12222－, etc., R4is an alkyl or a haloalkyl, and R5 is alkylcarbonyl or carbamoyl).
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
74.
HETEROAROMATIC DERIVATIVES HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
A composition comprising the compounds of Formula (I):
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
A composition comprising the compounds of Formula (I):
or pharmaceutically acceptable salts thereof,
wherein: R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or 2; R4 is substituted or unsubstituted non-aromatic nitrogen-containing heterocyclyl or the like; L is —NR8— or the like; R8 is a hydrogen atom or the like; R8 is each independently a hydrogen atom or the like; R8 is each independently a hydrogen atom or the like; p is 1 or 2; and R7 is a group represented by Formula:
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
A composition comprising the compounds of Formula (I):
or pharmaceutically acceptable salts thereof,
wherein: R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or 2; R4 is substituted or unsubstituted non-aromatic nitrogen-containing heterocyclyl or the like; L is —NR8— or the like; R8 is a hydrogen atom or the like; R8 is each independently a hydrogen atom or the like; R8 is each independently a hydrogen atom or the like; p is 1 or 2; and R7 is a group represented by Formula:
wherein R9 is substituted or unsubstituted alkyloxy or the like; R10 is a hydrogen atom or the like; R11 is halogen or the like; and m is 0 or 1.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The purpose of the present invention is to provide a novel Nav1.7 monoclonal antibody. Disclosed is a Nav1.7 monoclonal antibody having a specific CDR or a specific heavy chain variable region/light chain variable region, or an antibody fragment thereof. The monoclonal antibody, etc., can be used in the treatment or prevention of pain, pruritus, etc.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The purpose of the present invention is to provide a novel Nav1.7 monoclonal antibody. Disclosed is a Nav1.7 monoclonal antibody having a specific CDR or a specific heavy chain variable region/light chain variable region, or an antibody fragment thereof. The monoclonal antibody, etc., can be used in the treatment or prevention of pain, pruritus, etc.
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
77.
SIGNAL PROCESSING DEVICE, COGNITIVE FUNCTION IMPROVEMENT SYSTEM, SIGNAL PROCESSING METHOD, AND PROGRAM
This signal processing device comprises: a means for receiving an input acoustic signal; a means for generating an output acoustic signal in which the rise and fall of an envelope of an amplitude waveform are asymmetric, the output acoustic signal having a change in amplitude corresponding to the frequency of a gamma wave as a result of performing amplitude modulation of the received input acoustic signal; and a means for outputting the generated output acoustic signal.
This signal processing device comprises: a means for receiving an input acoustic signal; a means for acquiring a first acoustic signal having periodic changes corresponding to the frequency of a gamma wave; and a means for outputting an output acoustic signal based on a second acoustic signal based on the acquired first acoustic signal and the input acoustic signal.
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Tachibana, Yuki
Uehara, Shota
Unoh, Yuto
Nakahara, Kenji
Taoda, Yoshiyuki
Kasamatsu, Koji
Yamatsu, Yukiko
Ando, Shigeru
Iimuro, Atsuhiro
Suto, Takahiro
Sasaki, Michihito
Abstract
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.
A compound represented by Formula (I):
The present invention provides a compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same. Furthermore, the present invention provides a crystalline form useful as an active pharmaceutical ingredient, and a pharmaceutical composition comprising the same.
A compound represented by Formula (I):
wherein Y is N or the like; R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is substituted or unsubstituted aromatic carbocyclyl or the like; R3 is substituted or unsubstituted aromatic heterocyclyl or the like; —X— is —NH— or the like; m is 1 or the like; R5a is each independently a hydrogen atom or the like; R5b is each independently a hydrogen atom or the like; n is 1 or the like; R4a is each independently a hydrogen atom or the like; and R4b is each independently a hydrogen atom or the like,
or a pharmaceutically acceptable salt thereof.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
NATIONAL UNIVERSITY COPORATION HOKKAIDO UNIVERSITY (Japan)
SHIONOGI & CO., LTD. (Japan)
Inventor
Ishii, Akihiro
Sato, Akihiko
Kawai, Makoto
Taoda, Yoshiyuki
Abstract
The present invention provides a compound having antiviral activity, especially having arenavirus proliferation inhibitory activity, and/or a medicament comprising the compound. More preferably, the present invention provides a compound having proliferation inhibitory activity on the Old World arenaviruses such as Luna virus, Lassa virus, and lymphocytic choriomeningitis virus and/or the New World arenaviruses such as Junin virus, and/or a medicament comprising the compound.
An arenavirus proliferation inhibitor comprising a compound represented by Formula (I) or a prodrug thereof or a pharmaceutically acceptable salt thereof:
11 are each independently a hydrogen atom, carboxy, cyano, alkyl optionally substituted with Substituent group F, or the like).
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
wherein the group represented by Formula:
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
wherein the group represented by Formula:
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
wherein the group represented by Formula:
is a group represented by Formula:
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
wherein the group represented by Formula:
is a group represented by Formula:
A novel compound having HDAC2 inhibitory activity is provided. A compound represented by Formula (I):
wherein the group represented by Formula:
is a group represented by Formula:
or the like, wherein R3 is each independently amino or the like, and n is an integer of 0 to 4, X1 is N or the like, X2 is N or the like, R4 and R5 are each independently a hydrogen atom or the like, R1 is substituted with Substituent group C or unsubstituted non-aromatic carbocyclyl or the like, Substituent group C is halogen or the like, and R2 is a hydrogen atom, or a pharmaceutically acceptable salt thereof.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor in order to treat a novel coronavirus (COVID-19) infection. Provided is a pharmaceutical composition for treating a novel coronavirus (COVID-19) infection, said pharmaceutical composition containing, as an effective ingredient, a composite that includes a compound represented by formula (I) and fumaric acid.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
83.
PHARMACEUTICAL FOR TREATING NOVEL CORONAVIRUS INFECTION
The present invention provides a pharmaceutical composition containing a coronavirus 3CL protease inhibitor in order to treat a novel coronavirus (COVID-19) infection. Provided is a pharmaceutical composition for treating a novel coronavirus (COVID-19) infection, said pharmaceutical composition containing, as an effective ingredient, a composite that includes a compound represented by formula (I) and fumaric acid.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Tachibana, Yuki
Uehara, Shota
Unoh, Yuto
Nakahara, Kenji
Taoda, Yoshiyuki
Kasamatsu, Koji
Yamatsu, Yukiko
Ando, Shigeru
Fukao, Keita
Nobori, Haruaki
Kuroda, Takayuki
Toba, Shinsuke
Uemura, Kentaro
Maruyama, Yuki
Sasaki, Michihito
Sawa, Hirofumi
Abstract
The present invention provides a pharmaceutical composition containing a compound that exhibits a coronavirus growth inhibitory activity. A pharmaceutical composition containing a compound represented by the formula (wherein: Y is N; R1 represents an optionally substituted aromatic heterocyclic group; R2 represents an optionally substituted 6-membered aromatic carbon ring group; R3 represents an optionally substituted aromatic heterocyclic group; -X- is -NH-; m is 0 or 1; R5a represents a hydrogen atom; R5b represents a hydrogen atom; n is 1; R4a represents a hydrogen atom; and R4b represents a hydrogen atom) or a pharmaceutically acceptable salt thereof.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Tachibana Yuki
Uehara Shota
Unoh Yuto
Nakahara Kenji
Taoda Yoshiyuki
Kasamatsu Koji
Yamatsu Yukiko
Ando Shigeru
Fukao Keita
Nobori Haruaki
Kuroda Takayuki
Toba Shinsuke
Uemura Kentaro
Maruyama Yuki
Sasaki Michihito
Sawa Hirofumi
Abstract
The present invention provides a pharmaceutical composition containing a compound that exhibits a coronavirus growth inhibitory activity. A pharmaceutical composition containing a compound represented by the formula (wherein: Y is N; R1represents an optionally substituted aromatic heterocyclic group; R2represents an optionally substituted 6-membered aromatic carbon ring group; R3represents an optionally substituted aromatic heterocyclic group; -X- is -NH-; m is 0 or 1; R5arepresents a hydrogen atom; R5brepresents a hydrogen atom; n is 1; R4arepresents a hydrogen atom; and R4b represents a hydrogen atom) or a pharmaceutically acceptable salt thereof.
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, diabetes, obesity, cancer, endocrine disorders, hormonal diseases and disorders, urological disorders, sexual dysfunction, HIV and AIDs, central nervous systems diseases and disorders, peripheral nervous system diseases and disorders, osteoporosis, rheumatism, neurological disorders, pain, gastrointestinal disorders, respiratory diseases and disorders, allergies, bacterial disorders, viral disorders, fungal disorders, infectious diseases, inflammationn and inflammatory diseases, sepsis, immunological disorders, musculoskeletal disorders, thrombocytopenia, disease and disorders of the liver, and opioid-induced constipation; pharmaceutical preparations for treating allergic rhinitis
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, diabetes, obesity, cancer, endocrine disorders, hormonal diseases and disorders, urological disorders, sexual dysfunction, HIV and AIDs, central nervous systems diseases and disorders, peripheral nervous system diseases and disorders, osteoporosis, rheumatism, neurological disorders, pain, gastrointestinal disorders, respiratory diseases and disorders, allergies, bacterial disorders, viral disorders, fungal disorders, infectious diseases, inflammationn and inflammatory diseases, sepsis, immunological disorders, musculoskeletal disorders, thrombocytopenia, disease and disorders of the liver, and opioid-induced constipation; pharmaceutical preparations for treating allergic rhinitis
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, diabetes, obesity, cancer, endocrine disorders, hormonal diseases and disorders, urological disorders, sexual dysfunction, HIV and AIDs, central nervous systems diseases and disorders, peripheral nervous system diseases and disorders, osteoporosis, rheumatism, neurological disorders, pain, gastrointestinal disorders, respiratory diseases and disorders, allergies, bacterial disorders, viral disorders, fungal disorders, infectious diseases, inflammationn and inflammatory diseases, sepsis, immunological disorders, musculoskeletal disorders, thrombocytopenia, disease and disorders of the liver, and opioid-induced constipation; pharmaceutical preparations for treating allergic rhinitis
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, diabetes, obesity, cancer, endocrine disorders, hormonal diseases and disorders, urological disorders, sexual dysfunction, HIV and AIDs, central nervous systems diseases and disorders, peripheral nervous system diseases and disorders, osteoporosis, rheumatism, neurological disorders, pain, gastrointestinal disorders, respiratory diseases and disorders, allergies, bacterial disorders, viral disorders, fungal disorders, infectious diseases, inflammationn and inflammatory diseases, sepsis, immunological disorders, musculoskeletal disorders, thrombocytopenia, disease and disorders of the liver, and opioid-induced constipation; pharmaceutical preparations for treating allergic rhinitis
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, diabetes, obesity, cancer, endocrine disorders, hormonal diseases and disorders, urological disorders, sexual dysfunction, HIV and AIDs, central nervous systems diseases and disorders, peripheral nervous system diseases and disorders, osteoporosis, rheumatism, neurological disorders, pain, gastrointestinal disorders, respiratory diseases and disorders, allergies, bacterial disorders, viral disorders, fungal disorders, infectious diseases, inflammationn and inflammatory diseases, sepsis, immunological disorders, musculoskeletal disorders, thrombocytopenia, disease and disorders of the liver, and opioid-induced constipation; pharmaceutical preparations for treating allergic rhinitis
95.
SPIROHETEROCYCLE DERIVATIVE HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
The present invention provides: a compound having a serotonin 5-HT2A receptor antagonist and/or inverse agonist activity or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing same. A compound represented by formula (I) (in the formula, R1represents a hydrogen atom or the like, each A1independently represents CR2R2', each A2independently represents CR3R3', each R2independently represents a hydrogen atom or the like, each R2'independently represents a hydrogen atom or the like, each R3independently represents a hydrogen atom or the like, each R3'independently represents a hydrogen atom or the like, m and n each independently represent 1 or the like, ring B represents a ring represented by formula (II) or the like (in the formula, R4represents a group represented by formula (III) or the like (in the formula, each A3independently represents CR13R13', each A4independently represents CR14R14', each R13independently represents a hydrogen atom or the like, each R13'independently represents a hydrogen atom or the like, each R14independently represents a hydrogen atom or the like, each R14'independently represents a hydrogen atom or the like, q and r each independently represent 1 or the like, and R10and R11each independently represent a substituted or unsubstituted aromatic carbocyclic group or the like), and R8 represents a hydrogen atom or the like)), or a pharmaceutically acceptable salt thereof.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
A61P 43/00 - Drugs for specific purposes, not provided for in groups
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Kawaguchi Yoshimasa
Ueda Taichi
Yamada Toru
Kusumoto Yoshifumi
Sano Masayuki
Sanaki Takao
Toba Shinsuke
Sasaki Michihito
Abstract
The present invention provides a compound having a corona virus proliferation inhibition activity, and/or a pharmaceutical composition containing the compound having a corona virus proliferation inhibition activity. A compound represented by (I) (in the formula, R1represents a hydrogen atom or the like, R2represents a group or the like represented by formula: -(CR2aR2b)t2-Y2, R2'represents a hydrogen atom or the like, R3represents a hydrogen atom or the like, R4represents a substituted or unsubstituted alkyl, R4'represents a hydrogen atom, R5represents a hydrogen atom, R6represents a group or the like represented by formula: -(CR6aR6b)t6-Y6, R6'represents a hydrogen atom or the like, R7represents a hydrogen atom or the like, R8represents a group represented by formula: -(CR8aR8b)t8-Y8, R8'represents a hydrogen atom, R9represents a hydrogen atom or the like, R10represents a substituted or unsubstituted alkyl or the like, R10'represents a hydrogen atom or the like, R11represents a hydrogen atom or the like, R12represents a group or the like represented by formula: -(CR12aR12b)t12-Y12, R12'represents a hydrogen atom or the like, R13represents a substituted or unsubstituted alkyl, R13'represents a hydrogen atom, R14represents a hydrogen atom, R15represents a substituted or unsubstituted alkyl or the like, R15'represents a hydrogen atom or the like, R16represents a hydrogen atom, R17represents a group represented by formula: -(CR17aR17b)t17-Y17, R17'represents a hydrogen atom, R18represents a hydrogen atom, R19represents a substituted or unsubstituted alkyl, R19'represents a hydrogen atom or the like, R20represents a hydrogen atom, R21represents a group or the like represented by formula: -(CR21aR21b)t21-Y21, R21'represents a hydrogen atom, R22 represents a hydrogen atom or the like, -L- represents -S- or the like, and X represents a lipid-modifying residue), or a pharmaceutically acceptable salt thereof.
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Taoda Yoshiyuki
Uehara Shota
Sako Yusuke
Hirai Keiichiro
Abstract
The present invention provides: a compound having coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing same. Provided is a compound represented by formula (I) (in the formula, each of carbon atom a and carbon atom b is a carbon atom constituting ring A, ring A is a substituted aromatic carbon ring or the like, R1is a substituted or unsubstituted aromatic heterocyclic group or the like, R2is a substituted or unsubstituted 6-membered aromatic carbon ring group or the like, m is 1 or the like, R5ais each independently a hydrogen atom or the like, R5bis each independently a hydrogen atom or the like, n is 1 or the like, R4ais a hydrogen atom or the like, and R4b is a hydrogen atom or the like), or a pharmaceutically acceptable salt thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 451/04 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring system
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07K 14/165 - Coronaviridae, e.g. avian infectious bronchitis virus
The present invention provides a medicine characterized by the combination of: a compound represented by (A) or a pharmaceutically acceptive salt thereof; and (B) at least one drug selected from the group consisting of drugs having exhibiting anti-obesity activity, drugs for controlling blood sugar level, drugs for controlling blood cholesterol and/or triglycerides, and drugs for controlling blood pressure. The medicine is useful for the prevention and treatment of diseases linked to anti-obesity activity.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
99.
MEDICINE FOR PREVENTION AND TREATMENT OF DISEASES LINKED TO ANTI-OBESITY ACTIVITY
The present invention provides a medicine characterized by the combination of: a compound represented by (A) or a pharmaceutically acceptive salt thereof; and (B) at least one drug selected from the group consisting of drugs having exhibiting anti-obesity activity, drugs for controlling blood sugar level, drugs for controlling blood cholesterol and/or triglycerides, and drugs for controlling blood pressure. The medicine is useful for the prevention and treatment of diseases linked to anti-obesity activity.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
100.
BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVE HAVING VIRUS GROWTH INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
Inventor
Unoh Yuto
Yoshida Shuhei
Nakahara Kenji
Kojima Eiichi
Sasaki Yoshikazu
Miyagawa Masayoshi
Abstract
The present invention provides a compound that exhibits an inhibitory activity against coronavirus 3CL protease or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same. A compound represented by formula (I) (in the formula; X represents -NH-, etc.; Y represents =N-, etc.; Z represents -NR1-, etc.; W represents =N-, etc.; R1represents a substituted alkyl, a substituted or unsubstituted aromatic heterocyclic group, etc.; R2arepresents a substituted or unsubstituted aromatic carbon cyclic group, etc.; R2brepresents a hydrogen atom, etc.; n represents 1, etc.; R4arepresents a hydrogen atom, a substituted or unsubstituted alkyl, etc.; and R4b represents a hydrogen atom, etc.), or a pharmaceutically acceptable salt thereof.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
