Provided is a method for producing a substance related to 2-alkylcarbonylnaphtho[2,3-b]furan-4,9-dione that is suitable for industrial production. The present disclosure provides: a method for producing two production intermediates for 2-alkylcarbonyl[2,3-b]furan-4,9-dione by reacting commercially available 2-hydroxy-1,4-naphthoquinone with equally inexpensive, commercially available induced N,N-substituted formamide dimethyl acetal, and further reacting the product with an inexpensive commercially available 2-halo-1,4-diketone compound in the presence of water; and a substance related to the same.
The present disclosure provides a method for treating a microsatellite stable cancer patient with a specific combination of medical agents or a composition or combination therefor. Specific combinations of medical agents include a combination of a cancer stem cell inhibitor (e.g., napabucasin) and an immune checkpoint inhibitor (e.g., pembrolizumab). The MSS patient can be selected by determining if the patient has one or more patient characteristics. Another aspect of the disclosure provides a method for predicting responsiveness of a patient to a cancer treatment based on one or more patient characteristics.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
[Problem] To provide an assistance system for a person requiring nursing care enabling efficient collection of stimulus information. [Solution] The assistance system comprises: a stimulus information storing means that stores stimulus information regarding a stimulus to at least one of the five senses of a person requiring nursing care; and a value exchanging means that provides a stimulus information provision compensation to a provider who has provided new stimulus information additionally stored in the stimulus information storing means.
G06Q 50/22 - Social work or social welfare, e.g. community support activities or counselling services
G16H 40/00 - ICT specially adapted for the management or administration of healthcare resources or facilitiesICT specially adapted for the management or operation of medical equipment or devices
4.
SIGHTLINE-POSITION DETERMINATION DEVICE, SIGHTLINE-POSITION DETERMINATION METHOD, AND TRAINING METHOD
NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY (Japan)
SUMITOMO DAINIPPON PHARMA CO., LTD. (Japan)
Inventor
Nakaguchi, Toshiya
Shimizu, Eiji
Hirano, Yoshiyuki
Sutoh, Chihiro
Shiraiwa, Naomi
Ikeda, Yuki
Saito, Shunsuke
Abstract
A sightline-position determination device according to the present invention is provided with: a sightline-position input unit via which the position of a sightline of a user is input; a determination-area setting unit that sets a determination area; a determination unit that determines whether or not the position of the sightline, input via the sightline-position input unit, falls within the determination area; and an output unit that outputs feedback to the user when it is determined by the determination unit that the position of the sightline falls within the determination area.
A61B 10/00 - Instruments for taking body samples for diagnostic purposesOther methods or instruments for diagnosis, e.g. for vaccination diagnosis, sex determination or ovulation-period determinationThroat striking implements
A61B 3/113 - Objective types, i.e. instruments for examining the eyes independent of the patients perceptions or reactions for determining or recording eye movement
G06F 3/01 - Input arrangements or combined input and output arrangements for interaction between user and computer
The purpose of the present invention is to increase the amount of oligonucleic acid transported into the cytoplasm by bringing about an efficient interaction of a cell uptake promoter with a target cell. An oligonucleic acid conjugate according to the present invention comprises a dendritic polymer, a plurality of oligonucleic acids, one or a plurality of cell uptake promoters, and one or a plurality of hydrophilic linkers. Each oligonucleic acid is bonded to the dendritic polymer directly or through a linker, and each cell uptake promoter is bonded to the dendritic polymer through the hydrophilic linker.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
The present invention provides a compound that has an inhibitory effect on DYRK and is represented by general formula (I) (in the formula, A1, A2, L, R1, and R2 are as described in the specification).
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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 31/454 - 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 31/4743 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having sulfur as a ring hetero atom
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
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
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 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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
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 7/10 - Compounds having one or more C—Si linkages containing nitrogen
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
C07F 9/6584 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
The invention of the present application provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1) (see the description with respect to A1, A2, L1, L2, X, Z, R1and R4 in the formula), or a pharmaceutically acceptable salt thereof.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 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 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/00 - Drugs for disorders of the nervous system
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
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 purpose of the present invention is to provide a medium suitable for subretinal transplantation of retinal tissue for treating of retinal degenerative disease such as retinitis pigmentosa, and a transplantation composition that contains retinal tissue and said medium. The medium for transplantation according to the present invention is for subretinal transplantation of retinal tissue, has a viscosity of 5-500 mPa•s when shear speed (1/s) is 2 at 25°C, and contains hyaluronic acid and a pharmaceutically acceptable aqueous liquid. The transplantation composition according to the present invention contains retinal tissue for transplantation and the medium for transplantation according to the present invention.
The purpose of the present invention is to provide a complex containing two or more neural retina-containing cell aggregates and a matrix, and a method for manufacturing the same. The complex according to the present invention contains two or more cell aggregates, which contain pluripotent stem cell-derived neural retinas, and a matrix, where the two or more cell aggregates are disposed inside the matrix. The method for manufacturing the complex according to the present invention is a method for manufacturing a complex in which two or more neural retina-containing cell aggregates are disposed inside a matrix, the method including: (1) a first step for producing the two or more neural retina cell aggregates from pluripotent stem cells, and (2) a second step for making the matrix into a gel by causing the two or more cell aggregates to come into contact with the matrix or a matrix precursor in a prescribed arrangement.
A61L 27/44 - Composite materials, i.e. layered or containing one material dispersed in a matrix of the same or different material having a macromolecular matrix
A compound represented by formula (2): [in the formula, R1represents a hydrogen atom, etc., R2represents a methoxy group, etc., R3represents a hydrogen atom, etc., R41-61-6 alkyl group, etc., m represents 0, 1, or 2, n represents 0, 1, 2, or 3, L1represents -NH-C(=O)-, -C(=O)-NH-, etc., L2 represents a single bond, etc., X represents an optionally substituted phenyl, etc., Y represents an optionally substituted phenyl, etc., where X and Y are bonded by carbon atoms on their respective rings] or a pharmaceutically acceptable salt thereof.
C07C 235/38 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 235/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
NATIONAL UNIVERSITY CORPORATION EHIME UNIVERSITY (Japan)
SUMITOMO DAINIPPON PHARMA CO., LTD. (Japan)
Inventor
Tsuboi, Takafumi
Takashima, Eizo
Nagaoka, Hikaru
Fukushima, Akihisa
Abstract
The present disclosure comprises: a monoclonal antibody or an antibody fragment that binds to an epitope consisting of 5-20 consecutive amino acids in an amino acid sequence of SEQ ID NO: 1; and a method for detecting or quantifying a malaria vaccine antigen derived from Ripr, the method including bringing the antibody into contact with a sample.
The present disclosure provides a therapeutic agent useful for the treatment of motor fluctuations (e.g., wearing-off) in Parkinson's disease. In particular, the present disclosure provides: a composition characterized by containing tandospirone or a pharmaceutically acceptable salt or prodrug thereof for treating, ameliorating, inhibiting the progression of, or preventing motor complications, particularly, motor fluctuations, of Parkinson's disease; and a method characterized in that the tandospirone or the pharmaceutically acceptable salt thereof is parenterally administered.
NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER (Japan)
SUMITOMO DAINIPPON PHARMA CO., LTD. (Japan)
Inventor
Iwata, Yuko
Yoshida, Kozo
Hasezaki, Takuya
Takada, Yoshinori
Hashimoto, Masakazu
Abstract
The present invention provides an anti-human TRPV2 antibody, which recognizes an extracellular domain of human TRPV2 as an epitope, or a fragment thereof.
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
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 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
The present invention relates to a treatment agent for various diseases of the nervous system and mental illnesses which contains the compound represented in formula (1) or a pharmaceutically acceptable salt thereof as the active component (in the formula, R1represents a hydrogen, etc., R2represents a halogen, etc., and R3, R4, R5and R6 represent a hydrogen, etc.).
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 25/04 - Centrally acting analgesics, e.g. opioids
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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Pre-erythrocytic malaria vaccines with good preservation stability and immunostimulatory action are provided. According the present invention, combination use of a pharmaceutical composition comprising (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaeneamide, or a pharmaceutically acceptable salt thereof, as a vaccine adjuvant with enhanced specific immune response against antigens and good preservation stability and a malaria vaccine with biological activity allow for the provision of pre-erythrocytic malaria vaccines with good preservation stability and immunostimulatory action.
The present invention relates to a compound that is useful as a vaccine adjuvant, a method for producing the same, a pharmaceutical composition that contains the compound, and use of the compound as a vaccine adjuvant.
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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
INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC. (Japan)
Inventor
Goto, Masashi
Suginobe, Natsuko
Nakamura, Megumi
Abstract
The present disclosure includes a pharmaceutical composition for treating cancer in an HLA-A*02:07, HLA-A*03:01, HLA-B*15:01 or HLA-B*27:05-positive subject, said pharmaceutical composition comprising a cancer antigen peptide derived from WT1 or a peptide conjugate containing the same, etc.
An information processing device according to the present invention is equipped with a means for acquiring audio collected by a plurality of microphones. The information processing device is equipped with a means for estimating an arrival direction of the acquired audio. The information processing device is equipped with a means for generating a text image corresponding to the acquired audio. The information processing device is equipped with a means for referencing the estimated arrival direction and determining a presentation mode for the text image. The information processing device is equipped with a means for presenting the text image in the determined presentation mode.
G10L 15/10 - Speech classification or search using distance or distortion measures between unknown speech and reference templates
G10L 15/22 - Procedures used during a speech recognition process, e.g. man-machine dialog
G10L 15/28 - Constructional details of speech recognition systems
G10L 25/51 - Speech or voice analysis techniques not restricted to a single one of groups specially adapted for particular use for comparison or discrimination
G06F 3/01 - Input arrangements or combined input and output arrangements for interaction between user and computer
Provided are a system, a device, a program, and a method capable of objectively evaluating three-dimensional cognitive ability using quantification and the like. A three-dimensional cognitive ability of a subject is evaluated by: acquiring the position of a moving object that can specify the distance between the moving object and the subject; receiving the subject's active response which is responsive to the three-dimensional position of the object recognized by the subject; and determining whether the acquired position of the object and the input response correspond correctly. The present invention can also be configured such that: the moving object can be provided in virtual reality by means of a virtual reality headset; a moving image, when the object moves from a movement start position to a movement termination position in a direction approaching a predetermined viewpoint along a predetermined movement path when viewed in a predetermined viewpoint, is displayed in the virtual reality; and the three-dimensional cognitive ability is evaluated by a response to the position of the object.
G09B 19/00 - Teaching not covered by other main groups of this subclass
A61B 3/11 - Objective types, i.e. instruments for examining the eyes independent of the patients perceptions or reactions for measuring interpupillary distance or diameter of pupils
A61B 3/113 - Objective types, i.e. instruments for examining the eyes independent of the patients perceptions or reactions for determining or recording eye movement
G06F 3/01 - Input arrangements or combined input and output arrangements for interaction between user and computer
A61B 5/11 - Measuring movement of the entire body or parts thereof, e.g. head or hand tremor or mobility of a limb
The present invention addresses the problem of providing a 2-heteroarylaminoquinazolinone derivative. The present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof [in the formula, X1represents CR1or N; X2represents CR2or N; X3represents CR3or N; X4represents CR41-63-106-106-10 aryl group, or an optionally substituted 5 to 10-membered heteroaryl group; Z represents an optionally substituted 6 to 10-membered heteroaryl group; and each of R1, R2, R3, and R41-61-61-6 alkoxy group, or the like].
C07D 239/95 - QuinazolinesHydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 25/00 - Drugs for disorders of the nervous system
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 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 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 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 413/12 - 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
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 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
NATIONAL UNIVERSITY CORPORATION EHIME UNIVERSITY (Japan)
SUMITOMO DAINIPPON PHARMA CO., LTD. (Japan)
Inventor
King, C. Richter
Wu, Yimin
Plieskatt, Jordan Lee
Lee, Shwu-Maan
Wu, Chia-Kuei
Tsuboi, Takafumi
Fukushima, Akihisa
Abstract
Malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action are provided. According the present invention, combination use of a pharmaceutical composition comprising (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaeneamide, or a pharmaceutically acceptable salt thereof, as a vaccine adjuvant with enhanced specific immune response against antigens and good preservation stability and a malaria vaccine with non-glycosylation, homogeneity, and biological activity allow for the provision of malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action.
The present invention relates to the compound represented in formula (1) or a pharmaceutically acceptable salt thereof (in the formula, Q1represents a halogen, Q2represents a hydrogen, etc., X, Y and Z represent a nitrogen atom or an oxygen atom, and R1 represents a prescribed structure), and the present invention further relates to a therapeutic and/or prophylactic agent for disease such as epilepsy that contains these.
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
C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
23.
REGULATOR OF EXPRESSION AND/OR FUNCTION OF SCN1A GENE
A single-stranded antisense oligonucleotide or pharmaceutically acceptable salt thereof for promoting expression and/or regulating functioning of the voltage-dependent sodium channel α1 subunit gene, wherein the single-stranded antisense oligonucleotide includes a gap region, a 3' wing region bonded to the 3' end of the gap region, and a 5' wing region bonded to the 5' end of the gap region, the gap region being a 5-20 mer nucleic acid in which the sugar part is deoxyribose, the 3' wing region and the 5' wing region each being a 1-5 mer modified nucleic acid, and the modified nucleic acid in each of the 3' wing region and the 5' wing region including at least one selected from the group consisting of AmNA, GuNA, and scpBNA.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61P 25/00 - Drugs for disorders of the nervous system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
24.
CDK9 INHIBITOR PRODRUG AND LIPOSOME INCLUDING THE SAME
Provided is a novel CDK9 inhibitor prodrug and a liposome that includes the same. The present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, and a liposome that includes the same. [In the formula, A1, A2and A322E, or a hydrogen atom or the like; E is a group represented by formula (E); the * in the formula indicates a bonding location. X is an optionally-substituted 3- to 12-membered monocyclic or polycyclic divalent heterocyclic group or the like; Y is a single bond or the like; and Z is an optionally-substituted 5- to 10-membered heteroaryl group or the like.]
A61P 35/02 - Antineoplastic agents specific for leukemia
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 451/02 - 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
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
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
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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
25.
OPTICALLY RESOLVED TROLOX INTERMEDIATE AND METHOD FOR PRODUCING SAME
The present invention provides a method for chiral resolution of Trolox. The present disclosure relates to a method for producing a solid salt of a compound of formula I, wherein an amide-based solvent is added to a sample, which contains a compound of formula I, while being assumed to contain a compound of formula II, in the presence of an optical resolution agent. Formula I: (R)-6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-carboxylic acid (hereinafter referred to R Trolox) Formula II: (S)-6-hydroxy-2, 5, 7, 8-tetramethylchroman-2-carboxylic acid (hereinafter referred to S Trolox)
C07D 311/66 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 235/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
The present invention pertains to a transdermal absorption preparation that is capable of maintaining a blood concentration sufficient to exert the medicinal effect of tandospirone and that has excellent storage stability against heat, humidity and light. The present invention makes it possible to provide a transdermal absorption preparation characterized by comprising tandospirone or a pharmaceutically acceptable salt thereof and levulinic acid. This transdermal absorption preparation of tandospirone exhibits high skin permeability of tandospirone or a pharmaceutically acceptable salt thereof contained in the preparation and has excellent storage stability against heat and light.
The present invention addresses the problem of providing a virtual reality video play device that can cause a viewer to experience a disorder caused by a disease such as diabetes with a strong sense of immersion. This virtual reality video play device executes a filtering process that simulates a visual disorder caused by diabetes in a predetermined region of an image included in a virtual reality video that displays a virtual reality content, and displays the result on an electronic display included in a virtual reality headset.
The present invention provides a kit which is used to determine tauopathy and dementia-related diseases (here, Alzheimer's disease is excluded), and which comprises an antibody that recognizes a polypeptide consisting of: (1) the amino acid sequence represented by SEQ ID NO: 1; or (2) an amino acid sequence obtained by substituting, deleting, adding, or inserting one or more amino acids in the amino acid sequence represented by SEQ ID NO: 1.
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 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
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
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
The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I) (in the formula, Q, R1, R2, and R3 are as defined in the description).
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
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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
Provided are: a heterocyclic derivative and/or a pharmaceutically acceptable salt thereof that can serve as a therapeutic agent and/or a prophylactic agent for a disease in which the sodium channel (Nav) is involved and for various central nervous system disorders; and a pharmaceutical agent that includes the heterocyclic derivative and/or a pharmaceutically acceptable salt thereof as an active ingredient. Also provided are: a heterocyclic derivative and/or a pharmaceutically acceptable salt thereof that can serve as a therapeutic agent and/or a prophylactic agent for tauopathy, the agents functioning by activating Nav; and a pharmaceutical agent that includes the heterocyclic derivative and/or a pharmaceutically acceptable salt thereof as an active ingredient. Further provided is a heterocyclic derivative and/or a pharmaceutically acceptable salt thereof that can serve as a pharmaceutical agent and that is represented by formula (I) [in the formula, Y1, Y2, Y3, M1, and M2 are as defined in this description]; and a therapeutic agent and/or a prophylactic agent that includes the heterocyclic derivative and/or a pharmaceutically acceptable salt thereof as an active ingredient, and that is for a disease in which the sodium channel is involved, for various central nervous system disorders, and/or for tauopathy.
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
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 401/06 - 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 401/12 - 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 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 409/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 413/06 - 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 carbon chain containing only aliphatic carbon atoms
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
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5395 - 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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
Provided is a therapeutic agent and/or prophylactic agent for tauopathies that is based on the activation of voltage-gated sodium channels (Nav). The therapeutic agent and/or prophylactic agent for tauopathies has an Nav activator as an active ingredient.
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
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 401/06 - 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 401/12 - 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 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 403/06 - 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 403/12 - 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 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 405/06 - 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
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 409/14 - 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 413/06 - 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 carbon chain containing only aliphatic carbon atoms
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
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
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 31/4375 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged 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
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
2A77 receptors; or a pharmaceutically acceptable salt of the compound. (In the formula, Z is a nitrogen atom or the like; Y is carbonyl and the like; m and n are 1 and the like; R1athrough R1d, R2athrough R2d, and R4athrough R4dare a hydrogen atom and the like; R3 is an alkyl and the like; and Q is a specific bicyclic group.)
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
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
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 413/04 - 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 directly linked by a ring-member-to-ring- member bond
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The present invention addresses the problem of providing a culturing method and a production method for hematopoietic stem cells which can be used for hematopoietic stem cell transplantation. The method for culturing hematopoietic stem cells according to the present invention comprises culturing a cell population including hematopoietic stem cells in a medium containing at least one compound represented by formula (1) or a salt thereof.
[Problem] To provide a method which is for preparing a peptide emulsion formulation and by which a desired peptide emulsion formulation can be prepared. [Solution] A method for preparing a peptide emulsion formulation includes: a step for mixing an oily formulation and an aqueous solution containing a compound consisting of an amino acid sequence represented by formula (1) or a pharmaceutically acceptable salt of the compound, and a peptide consisting of an amino acid sequence represented by WAPVLDFAPPGASAYGSL (SEQ ID NO: 1) or a pharmaceutically acceptable salt of the peptide, and then subjecting the resultant mixture to vibration stirring; and a membrane emulsification step for causing a premixed solution, which has been subjected to the vibration stirring, to pass through a membrane filter to perform emulsification.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/16 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
B01J 13/00 - Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided forMaking microcapsules or microballoons
35.
SMALL-SIZED TABLET HAVING EXCELLENT PRODUCIBILITY AND ELUTION PROPERTIES
The present invention relates to: a small-sized oral preparation, which contains imeglimin or a pharmaceutically acceptable salt thereof, a binding agent, and a disintegrating agent, is produced according to a fluidized bed granulation method, and has excellent elution properties; and a method for producing the small-sized oral preparation.
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
The present invention pertains to a therapeutic agent or preventative agent against diseases involving an orexin receptor, and specifically, an orexin type-2 receptor, said agent containing a novel compound having a urea skeleton or a pharmaceutically acceptable salt thereof as an active ingredient. Specifically, the present invention pertains to a therapeutic agent or preventative agent against diseases such as narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, and the like.
C07D 211/16 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
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 31/495 - 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
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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
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
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
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 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 11/00 - Drugs for disorders of the respiratory system
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/04 - Centrally acting analgesics, e.g. opioids
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 35/02 - Antineoplastic agents specific for leukemia
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 401/12 - 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 413/04 - 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 directly linked by a ring-member-to-ring- member bond
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 417/04 - 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 directly linked by a ring-member-to-ring- member bond
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
Provided is a method for freezing a cell aggregate that includes neural cells. Provided is a method for freezing a cell aggregate that includes neural cells having a three-dimensional structure, said method including the following step (1) and step (2): (1) a step in which, prior to freezing, the cell aggregate that includes the neural cells having the three-dimensional structure is brought into contact with a preservation liquid at 0°C to 30°C, and a preservation liquid-soaked cell aggregate is prepared; and (2) a step in which the preservation liquid-soaked cell aggregate that was obtained in step (1) is cooled at an average temperature reduction speed of 2-7°C/min, at least from a temperature that is approximately 5°C above the freezing point of the preservation liquid to a temperature that is approximately 5°C below said freezing point, and is thus made to freeze.
Provided is a method for freezing cell aggregates including nervous cells. Provided is a method for freezing cell aggregates including nervous cells and having a three-dimensional structure, the method comprising the following step (1) and step (2): step (1) for immersing, in a cryopreservation solution, cell aggregates including nervous cells at a temperature of 0 °C to 30 °C before freezing, and preparing the cell aggregates immersed in the cryopreservation solution; and step (2) for freezing the cell aggregates including nervous cells under a gaseous phase condition of a liquid nitrogen container having a temperature of at most -150 °C.
The present invention provides a novel compound having an excellent β-lactamase inhibitory effect. The present invention provides: a compound which has an excellent β-lactamase inhibitory effect, and is represented by formula (1a), (1b) or (11); or a pharmaceutically acceptable salt thereof. This compound provides a prophylactic or therapeutic agent effective for bacterial infections when used in combination with β-lactam-based drugs or used as a single agent. The present invention also provides a prophylactic or therapeutic agent effective for treating various diseases, by being used in combination with β-lactam-based drugs.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
A61K 31/407 - 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 heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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
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
This RI-labeled anti-MUC5AC humanized antibody is a complex of a radionuclide-chelated chelating agent and an antibody (the radionuclide is a metal nuclide that emits α-rays or positrons, and the antibody is a humanized antibody that binds specifically to MUC5AC) and is very useful in the treatment and/or diagnosis of diseases in which MUC5AC is overexpressed, especially cancer, due to excellent specificity for MUC5AC and ability to accumulate in tumors.
A61K 51/10 - Antibodies or immunoglobulinsFragments thereof
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
The purpose of the present invention is to provide a humanized antibody or an antigen-binding fragment thereof that has stable physical properties, that demonstrates excellent tumor accumulation, and that is capable of binding to mucin subtype 5AC. To solve the foregoing, the present invention provides a humanized antibody, or an antigen-binding fragment thereof, that has a heavy chain variable region composed of an amino acid sequence represented by SEQ ID NOs: 1-4 or a variant thereof and a light chain variable region composed of an amino acid sequence represented by SEQ ID NOs: 5-8 or a variant thereof, and that is capable of binding to mucin subtype 5AC.
The present invention pertains to a compound represented by formula (1a) [in the formula: p represents 1 or 2; R1to R4 represent a hydrogen atom, etc.; ring A represents a cycloalkylene, etc.; L represents a single bond, etc.; and R represents methyl, etc.] or a pharmaceutically acceptable salt thereof. This compound exerts an anticancer effect by inhibiting the binding of an MLL fusion protein fused with a typical fusion partner gene inducing MLL leukemia, for example AF4 or AF9, to menin.
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
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
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 31/4545 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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
43.
METHOD FOR PRODUCING CELL AGGREGATE INCLUDING GLIAL PROGENITOR CELLS
This method for producing a cell aggregate including glial progenitor cells comprises: (1) a step for forming a cell aggregate by subjecting pluripotent stem cells to a suspension culture for 5-10 days in an embryoid body-forming medium containing at least one SMAD signaling inhibitor and at least one Wnt signaling activator, in the absence of feeder cells; (2) a step for subjecting the cell aggregate obtained in (1) to a suspension culture in an embryoid body-forming medium containing retinoic acid; (3) a step for subjecting the cell aggregate obtained in (2) to a suspension culture in an embryoid body-forming medium or nerve and glia-proliferating medium, which contains retinoic acid and at least one SHH signaling activator; and (4) a step for subjecting the cell aggregate obtained in (3) to a suspension culture in a nerve and glia-proliferating medium which does not contain retinoic acid and contains at least one SHH signaling activator.
C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving viable microorganisms
C12Q 1/04 - Determining presence or kind of microorganismUse of selective media for testing antibiotics or bacteriocidesCompositions containing a chemical indicator therefor
This disclosure provides: a method for treating a patient with microsatellite stable cancer using a specific combination of drugs; and a composition or combination therefor. An example of the specific combination of drugs is a combination of a cancer stem cell inhibitor (e.g., napabucasin) and an immune checkpoint inhibitor (e.g., pembrolizumab). The MSS patient may be selected on the basis of having one or more patient characteristics. Another aspect of the present disclosure is a method for predicting the responsiveness of the patient to cancer treatment on the basis of the one or more patient characteristics.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention provides a 2-aminoquinazolinone derivative. The present invention is a compound represented by formula (1) [wherein X1represents CR1or N, X2represents CR2or N, X3represents CR36-106-106-10 aryl, RA1-61-61-61-6 alkoxy, and R1, R2, and R31-61-61-6 alkoxy] or a pharmaceutically acceptable salt thereof.
A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 39/06 - Free radical scavengers or antioxidants
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 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 405/12 - 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 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 239/95 - QuinazolinesHydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
Provided are a ring-fused pyrazole derivative, which is useful as a therapeutic agent and/or a preventive agent for diseases associated with Nav1. 1 and various central nervous system diseases, and/or a pharmaceutically acceptable salt thereof, and a pharmaceutical comprising the same as an active ingredient. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof. [In the formula: Y1, Y2and Y3independently represent N or CR2; R1is a hydrogen atom, etc.; R2is a hydrogen atom, etc.; M14-124-12 carbocyclic group, etc.; M2is a group represented by formula (2a) or (2b), etc.; and X1a, X1b, X1c, X2, X3, X4, X5, X6, X7, X8, A1and A2 are as stated in the description.]
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 43/00 - Drugs for specific purposes, not provided for in groups
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 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
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 31/4545 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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
47.
PHARMACEUTICAL COMPOSITION FOR THERAPY AND/OR PROPHYLAXIS OF COLORECTAL CANCER
The present disclosure provides a pharmaceutical composition or method for therapy and/or prophylaxis of cancer, or a screening method for screening for a substance or a factor for therapy and/or prophylaxis of cancer. The present disclosure provides a pharmaceutical composition that is for therapy and/or prophylaxis of cancer accompanied by chronic inflammation, and that contains an NFKBIZ inhibitor. Examples of the NFKBIZ inhibitor include substances that inhibit the expression and/or function of NFKBIZ. The cancer accompanied by chronic inflammation is preferably an enterocolitis-associated cancer observed in ulcerative colitis.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Provided is a method for producing a substance related to 2-alkylcarbonylnaphtho[2,3-b]furan-4,9-dione that is suitable for industrial production. The present disclosure provides: a method for producing two production intermediates for 2-alkylcarbonyl[2,3-b]furan-4,9-dione by reacting commercially available 2-hydroxy-1,4-naphthoquinone with equally inexpensive, commercially available induced N,N-substituted formamide dimethyl acetal, and further reacting the product with an inexpensive commercially available 2-halo-1,4-diketone compound in the presence of water; and a substance related to the same.
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C07C 225/24 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones the carbon skeleton containing carbon atoms of quinone rings
Provided is a composite that includes a neural retina, a retinal pigment epithelial cell sheet, and a hydrogel, wherein: the neural retina and the retinal pigment epithelial cell sheet are derived from human pluripotent stem cells; in the neural retina, a neural retina layer including at least a photoreceptor cell layer is formed; the photoreceptor cell layer includes at least one type selected from photoreceptor cells, photoreceptor precursor cells, and retina precursor cells; the melting point of the hydrogel is 20-40ºC; the neural retina and the retinal pigment epithelial cell sheet are entirely embedded in the hydrogel; the direction of a tangent to the surface of the neural retina and that of the retinal pigment epithelial cell sheet are almost parallel; and the top end surface of the neural retina faces the top end surface of the retinal pigment epithelial cell sheet, and both are separated from each other by the hydrogel and are not in contact with each other.
The present invention provides a therapeutic drug that is useful for levodopa induced dyskinesia in Parkinson's disease. In particular, the present invention provides a composition and method for treating, improving, suppressing the progression, or preventing motor complications associated with levodopa therapy for Parkinson's disease, especially levodopa induced dyskinesia (PD-LID), comprising tandospirone or a pharmaceutically acceptable salt or prodrug thereof, wherein the tandospirone or a pharmaceutically acceptable salt or prodrug thereof is parenterally administered.
The present invention provides a method in which when using (+)-dibenzoyl-D-tartaric acid to optically divide (±)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone, an ether-based solvent is added and an extremely high yield of (R)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone (+)-dibenzoyl-D-tartrate is thereby obtained, a slurry thereof is treated with a base, a "three-dimensionally bulky reducing agent" is subsequently used, and cis-(-)-fluocino piperidol is thereby produced with surprisingly high selectivity.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations; antitumor drugs; pharmaceutical
preparations for the diagnosis, prevention and treatment of
cancer; biological preparations for the treatment of cancer. Testing, inspection or research of pharmaceuticals; testing,
inspection or research of pharmaceuticals for the diagnosis,
prevention and treatment of cancer. Providing medical information; providing information in the
field of cancer prevention, screening, diagnosis and
treatment; health care services for treating cancer.
53.
WATER SOLUBLE ADJUVANT AND COMPOSITION CONTAINING SAME
The present invention pertains to a compound useful as a vaccine adjuvant for a cancer vaccine, a method for producing said compound, a medicinal composition containing said compound, and a use of said compound as a vaccine adjuvant for a cancer vaccine.
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
The present invention pertains to a compound useful as a vaccine adjuvant for a cancer vaccine, a method for producing said compound, a medicinal composition containing said compound, and a use of said compound as a vaccine adjuvant for a cancer vaccine.
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
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 47/26 - 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
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
C07D 239/49 - Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
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
This method for evaluating the quality of a transplant neural retina includes: extracting, as a quality evaluation sample, a portion of or all of a cell aggregate that contains a neural retina having an epithelial structure derived from pluripotent stem cells; detecting, in the quality evaluation sample, the expressions of genes related to neural-retina-based cells and genes related to non-neural-retina-based cells; and, in the case in which the expressions of the genes related to the neural-retina-based cells are recognized and the expressions of the genes related to the non-neural-retina-based genes are not recognized, determining that it is possible to use, as the transplant neural retina, (1) a neural retina (transplant neural retina) in a cell aggregate that is the same as the cell aggregate that contains the quality evaluation sample as a portion thereof, (2) a neural retina (transplant neural retina) in a cell aggregate of the same lot as the cell aggregate that contains the quality evaluation sample as a portion thereof, or (3) a neural retina (transplant neural retina) in a cell aggregate of the same lot as the cell aggregate the entirety of which is the quality evaluation sample. The genes related to non-neural-retina-based cells are one or more types of genes selected from the group consisting of cerebrospinal tissue marker genes and eye-related tissue marker genes.
The present invention provides an aqueous suspension-type pharmaceutical preparation containing (1) (3aR, 4S, 7R, 7aS)-2-{(1R, 2R)-2-[4-(1,2-benzoisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindol-1,3-dione (compound 1), a pharmaceutically acceptable acid addition salt thereof, or a mixture of these and (2) one or more chlorides selected from inorganic chlorides or C4-12 quaternary ammonium chlorides that masks the bitterness to improve the ease of administration and has good drug absorption, wherein the aqueous suspension-type pharmaceutical preparation has characteristic (I) or (II): (I) D90 of the suspended particles is 1-50 μm when the particle size distribution of the suspended particles in the preparation is unimodal; (II) D90 of the suspended particles is 1-100 μm when the particle size distribution of the suspended particles in the preparation is bimodal or multimodal.
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
Provided is a method for preparing an influenza HA split vaccine which produces an antibody that binds to an HA stem region of influenza, wherein it is difficult for the HA stem region to produce an antigenic variant. Acidic treatment is performed on the influenza HA split vaccine. By performing the acidic treatment, the influenza HA split vaccine is obtained which produces an antibody that binds to an LAH of an HA stem region. This influenza HA split vaccine has good protective ability against infection from other influenza viruses having different antigenicities.
INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC. (Japan)
Inventor
Yamakawa Erina
Goto Masashi
Abstract
Disclosed is a method for selecting a subject likely benefiting from a pharmaceutical composition for treating or preventing cancer, said method comprising: a step for identifying the presence or absence of a mutation in Tumor Protein p53 (TP53) gene and/or BCL6 co-repressor (BCOR) gene with the use of a sample collected from the subject; and a step for, when TP53 wild type and/or BCOR wild type are identified, then providing an indication that this subject likely benefits from the pharmaceutical composition.
C12Q 1/04 - Determining presence or kind of microorganismUse of selective media for testing antibiotics or bacteriocidesCompositions containing a chemical indicator therefor
A compound or represented by formula (1) or a salt thereof (in the formula, R1 represents a hydrogen atom or a sulfonyl group, and Z represents a group represented by formula (Z-1), etc.).
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
C07K 5/065 - Dipeptides the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
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 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
An agent for eliminating pluripotent stem cells that comprises an antibody-drug conjugate or a salt thereof, said antibody-drug conjugate releasing a compound represented by formula (1-1) [wherein: b represents an integer of 1-5; and Z represents a group represented by formula (Z-1) or formula (Z-2)].
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 207/416 - 2,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
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
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
A61K 35/12 - Materials from mammalsCompositions comprising non-specified tissues or cellsCompositions comprising non-embryonic stem cellsGenetically modified cells
A compound represented by formula (1) or a salt thereof. [In formula (1), b is an integer of 1-5, X represents -NH- or -CO-, Z represents a group represented by, for example, formula (Z-1), R1mm, AB represents a specific amino acid residue, and when two or more AB moieties are present, then the AB moieties may be the same or different and have been bonded to each other by an amide linkage, m is an integer of 1-9, R2gg, AC represents a specific amino acid residue, and when two or more AC moieties are present, then the AC moieties may be the same or different and have been bonded to each other by an amide linkage, and g is an integer of 1-9.]
Provided is a method for producing a 2-alkylcarbonylnaphtho[2,3-b]furan-4,9-dione-related substance, which is suitable for the production on an industrial scale. The present invention provides: a method for producing an intermediate for the production of a 2-alkylcarbonyl[2,3-b]furan-4,9-dione, which comprises reacting a 1-butyne derivative in which a ketone or an alcohol is protected with a 2-hydroxy-1,4-naphthoquinone derivative having a leaving group at position-3 in a solvent in the presence of a metal or a metal compound and a base; and a substance relating to the intermediate.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Anti-cancer preparations; pharmaceutical preparations for the diagnosis, prevention and treatment of cancer; biological preparations for the treatment of cancer Testing, inspection or research of pharmaceuticals; testing, inspection or research of pharmaceuticals for the diagnosis, prevention and treatment of cancer Providing medical information; providing information in the field of cancer prevention, screening, diagnosis and treatment; health care services for treating cancer
Provided is a composition that is useful as a vaccine adjuvant and has excellent storage stability and immunostimulatory activity. Specifically provided is a freeze-dried preparation that has high storage stability, said preparation containing a (4E, 8E, 12E, 16E, 20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexane-3-yl]amino}-6-methylpyrimidine-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaenamide, squalene, a hydrophilic surfactant, and an oleophilic surfactant, and being characterized by containing an ascorbic acid-based antioxidant and an excipient.
Provided is a cancer treatment pharmaceutical composition that contains a CDK inhibitor. A pharmaceutical composition that includes a CDK inhibitor and is for treating cancers that demonstrate resistance to androgen removal therapy. The CDK inhibitor includes alvocidib or a pharmaceutically acceptable salt thereof. The cancers are cancers that demonstrate treatment resistance to androgen receptor antagonists and/or androgen synthesis inhibitors. A cancer treatment composition that includes alvocidib or a pharmaceutically acceptable salt thereof as an active ingredient and is to be administered to subjects that have enhanced androgen receptor phosphorylation.
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
The purpose of the present invention is to provide a novel compound that has an excellent β-lactamase inhibitory activity. The present invention provides: a compound that has an excellent β-lactamase inhibitory activity and is represented by formula (1a), (1b) or (11); or a pharmaceutically acceptable salt thereof. The compound provides a prophylactic or therapeutic agent that is useful for bacterial infection when used in combination with a β-lactam drug or used alone. The present invention also provides a prophylactic or therapeutic agent that is useful for treating a variety of diseases in combination with a β-lactam drug.
A61K 31/407 - 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 heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
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
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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 9/00 - Drugs for disorders of the cardiovascular system
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention pertains to a therapeutic drug for diseases accompanied by disorders in retinal system cells or a retinal tissue, the drug containing a non-autologous retinal tissue having a steric structure. The intended patients for the therapeutic drug administration are those who are affected with diseases accompanied by disorders in retinal system cells or a retinal tissue and who would not receive systemic administration of an immune-suppressive agent used for the purpose of preventing any rejection reaction caused by transplant for at least a month after the therapeutic drug was administered.
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 45/00 - Medicinal preparations containing active ingredients not provided for in groups
The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.
C07B 63/02 - PurificationSeparation specially adapted for the purpose of recovering organic compoundsStabilisationUse of additives by treatment giving rise to a chemical modification
C07C 43/20 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
C07C 45/65 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by splitting-off hydrogen atoms or functional groupsPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by hydrogenolysis of functional groups
The present invention addresses the problem of providing a formulation for applying a semaphorin inhibitor without surgery to remove the dura mater. Provided is a sheet formulation for treating spinal cord injury or brain injury by epidural administration, the sheet formulation including a semaphorin inhibitor.
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
71.
THERAPEUTIC AGENT FOR CENTRAL NERVOUS SYSTEM DISEASE INCLUDING TIPEPIDINE
The present invention relates to: a therapeutic agent or a prophylactic agent for a central nervous system disease, in which tipepidine or a pharmaceutically accepted salt thereof and CYP2D6 inhibitor are used in combination; or a therapeutic agent or a prophylactic agent, in which tipepidine alone is used, for Parkinson's disease, Parkinson's disease syndrome caused by the use of an antipsychotic drug, sleep disorders, chronic fatigue syndrome, and also for fatigue, compulsive eating, addiction, or fibromyalgia associated with nerve degeneration and central nervous system disorder, or emotional trauma and stressor-related disorders.
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
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
Provided is a method for producing particles coated by a coatable first polymer and a lubricant. A method for producing particles coated by a first polymer and a lubricant, wherein the production method is characterized by: including a step for adding a first polymer and a lubricant to core particles that include a target component and a second polymer, and coating while rolling the mixture and spraying a solvent capable of dissolving the first polymer; and the particles coated by the first polymer and lubricant being target-component-containing hollow particles.
A61K 8/81 - Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
Provided is a method for assessing the correlation of respective preventive interventional actions with, and impact thereof on, health in a health domain of interest, on the basis of biological information acquired over time. This method comprises: acquiring an individual's biological information over time; assessing the individual's health over time on the basis of the acquired biological information; acquiring respective intervention quantities of one or more preventive interventional actions over time; establishing correlation of the intervention quantities over time of each of the preventive interventional actions with, and impact thereof on, the individual's health over time; and determining one of the one or more preventive interventional actions that has a correlation of a predetermined value or higher to be a relevant preventive interventional action of interest.
G16H 20/00 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance
INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC. (Japan)
SUMITOMO DAINIPPON PHARMA CO., LTD. (Japan)
Inventor
Sugiyama Haruo
Abstract
1263535 helper peptide. In another aspect, provided are WT1 peptide-specific CTLs, a method for inducing WT1-specific helper T cells and a method for inducing dendritic cells presenting a WT1 peptide.
The present invention pertains to a lyophilized preparation to be used in a cancer peptide vaccine therapy, said lyophilized preparation comprising two or more kinds of WT1 protein-derived cancer antigen peptides having cytotoxic T cell induction activity.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 47/69 - 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
The present invention pertains to a compound represented by formula (1a) [wherein: p represents 1 or 2; R1to R4 represent a hydrogen atom, etc.; and a to d represent 1 or 2] or a pharmaceutically acceptable salt thereof, said compound inhibiting the binding of an MLL-fusion protein, which carries a typical fusion partner gene such as AF4 or AF9 inducing MLL leukemia fused therewith, to menin and thus exerting an anticancer effect.
The present invention relates to a compound or a pharmaceutically acceptable salt thereof that exhibits an anti-cancer effect by inhibiting binding between menin and an MLL fusion protein in which a representative fusion partner gene such as AF4 or AF9, which induces MLL leukemia, is fused, the compound being represented by formula (1a) [wherein a to d and p represent 1 or 2, R1to R4represent a hydrogen atom or the like, and R1833].
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
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
The present invention provides a polypeptide comprising any of the following amino acid sequences that are useful for diagnosing Alzheimer's disease: (1) an amino acid sequence expressed by SEQ ID NO: 1; or (2) an amino acid sequence in which one or several amino acids of the amino acid sequence expressed by SEQ ID NO:1 are substituted, deleted, added or inserted.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
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
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
The present invention relates to a therapeutic agent for neuropsychiatric disorders containing a compound represented by formula (1) or a pharmaceutically acceptable salt thereof an active ingredient.
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
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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
Provided are: a pyridazinone derivative and/or a pharmaceutically acceptable salt thereof, which is useful as a therapeutic agent and/or a prophylactic agent for diseases in which Nav1.1 is involved and various central nervous system diseases; and a medicine containing the pyridazinone derivative and/or the pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof. [In the formula, M14-124-12 carbocyclic group or the like; R1and R2independently represent a hydrogen atom or the like; M2represents a group represented by formula (2a) or the like; X1a, X1band X1cindependently represent N or the like; X2, X3and X4independently represent CR3or the like; A1and A2independently represent N or the like; and R3 represents a hydrogen atom or the like.]
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
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
A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
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
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 403/14 - 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 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 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
The present invention pertains to a drug for the treatment and/or prevention of pain, more specifically to a medicinal preparation for external use to treat and/or prevent peripheral neuropathic pain, the medicinal preparation containing as an active ingredient N2-{[1-ethyl-6-(4-methylphenoxy)-1H-benzimidazol-2-yl]methyl}-L-alaninamide.
The present invention addresses the problem of providing: a dispersion of pluripotent stem cells and a pluripotent stem cell product, each of which can be stored, can be distributed on the market, and has quality suitable for the use as a medicine or a raw material for a medicine; and a method for producing the pluripotent stem cell product. The method for producing a pluripotent stem cell product according to the present invention comprises the steps of: (1) culturing pluripotent stem cells in an undifferentiated cell maintenance culture medium; (2) suspending the pluripotent stem cells cultured in step (1) in a first cell suspension medium containing a ROCK inhibitor; (3) replacing the cell suspension medium in the suspension obtained in step (2) by a cryopreservation medium to produce a cell dispersion composed of the cryopreservation medium and the pluripotent stem cells dispersed in the cryopreservation medium; and (4) filling the cell dispersion obtained in step (3) in an air-tight container in an air-tight state.
The present disclosure relates to a solid oral dosage form comprising: (i) (S)-4-amino-5-chloro-N-[{4-[(1-hydroxyacetyl-4-piperidinyl)methyl]-2-morpholinyl}methyl]-2-methoxybenzamide, a pharmaceutically acceptable salt thereof, or a hydrate or solvate of the same; (ii) a disintegrating agent; and (iii) a water-soluble polymer binder. The present disclosure also relates to a medicinal composition, a therapeutic agent and/or a preventive agent, which comprise the medicine according to the present disclosure, for treating and/or preventing digestive diseases, digestive symptoms, psychoneurological diseases or urinary diseases, a preferable example thereof being a solid oral dosage form.
Provided is a novel compound that has an excellent β-lactamase inhibitory effect. More specifically, provided is a compound represented by formula (1a), (1b) or (11) having an excellent β-lactamase inhibitory effect or a pharmaceutically acceptable salt thereof. By using this compound either in combination with a β-lactam drug or alone, a useful preventive or therapeutic agent for bacterial infections is provided. Also provided are useful preventive or therapeutic agents for treating various diseases with the combined use of the aforesaid compound and β-lactam drugs.
A61K 31/407 - 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 heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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 11/00 - Drugs for disorders of the respiratory system
A61P 11/04 - Drugs for disorders of the respiratory system for throat disorders
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
The present invention pertains to a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, said compound inhibiting the binding of an MLL fusion protein, in which a typical fusion partner gene such as AF4 or AF9 inducing MLL leukemia is fused, to menin and thus exerting an antitumor effect. [In the formula: p represents 1 or 2; R133, etc.; R2a, R2b, R3aand R3b represent a hydrogen atom, etc.; and X represents -C(=O)-, etc.]
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
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof, the compound or salt being useful as a novel antitumor agent targeting CSC, which is suggested to be significantly involved in the sustained growth of malignant tumors, cancer metastasis, recurrence, and resistance to antitumor agents. [In the formula, R1A, R1B, R1C, and R1Dare hydrogen atoms, etc.; R2Aand R2Bare hydrogen atoms, etc.; R3A, R3B, R3C, and R3D1-61-6 alkylene, and Q represents an optionally substituted imidazole.]
A61K 31/436 - 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 oxygen as a ring hetero atom, e.g. rapamycin
The present invention provides an aqueous suspension-type pharmaceutical preparation that, even when administered orally, suppresses premature dissolution and absorption, has a relatively low risk of onset of unexpected side effects caused by temporary increase in concentration in the blood, and contains (1)–(4). (1) A (3aR, 4S, 7R, 7aS)–2–{(1R, 2R)–2–[4–(1, 2–benzisothiazole–3–yl) piperazine–1–ylmethyl] cyclohexylmethyl} hexahydro–4, 7 – methano–2H–isoindole–1,3–dione, a pharmaceutically acceptable acid addition salt thereof, or a mixture of these; (2) xantham gum; (3) a dispersant; and (4) water.
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
The present invention provides an aqueous suspension-type pharmaceutical preparation that does not cause premature dissolution or absorption even when administered orally, exhibits gastric solubility corresponding to the drug characteristics, is capable of suppressing particle growth and particle aggregation, contains (1)–(4), and has a pH of 2.5–5.5. (1) A (3aR, 4S, 7R, 7aS)–2–{(1R, 2R)–2–[4–(1, 2–benzisothiazole–3–yl) piperazine–1–ylmethyl] cyclohexylmethyl} hexahydro–4, 7 – methano–2H–isoindole–1,3–dione, a pharmaceutically acceptable acid addition salt thereof, or a mixture of these; (2) at least one type of chloride selected from an inorganic chloride or a C4–12 quaternary ammonium chloride; (3) a dispersant; and (4) water.
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
90.
DIBENZAZEPINE DERIVATIVE HAVING NITROGEN-CONTAINING HETEROCYCLIC RING
The present invention provides a compound represented by formula (1), which is useful as a therapeutic and/or prophylactic agent for central nervous system diseases, or a pharmaceutically acceptable salt thereof. (In the formula, each of ring Q1and ring Q2independently represents an optionally substituted benzene ring or an optionally substituted pyridine ring; Ra1-61-6 alkyl group which may be substituted by the same or different 1-3 halogen atoms; n represents 0, 1 or 2; m represents 1, 2, 3 or 4; and, in cases where a plurality of Rbmoieties are present, each of the Rb1-61-6 alkyl group which may be substituted by the same or different 1-3 halogen atoms.)
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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
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
91.
METHOD FOR MANUFACTURING DRUG-CONTAINING PARTICLES
The present invention relates to an efficient method for manufacturing drug-containing particles. This method for manufacturing hollow particles that each comprise a shell and a hollow portion, with the shell containing a drug and a polymer, is characterized by including a step of using a container rotating stirring device to add a polymer and a solvent capable of dissolving the polymer to drug-containing powder while rotating a container and stirring blades, and then rotating the container and the stirring blades to form the particles, wherein the average particle size of the polymer used as a source material is five or more times the average particle size of the drug used as a source material.
A61J 3/02 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of powders
The purpose of the present invention is to provide: a cell aggregate containing dopamine-producing neural precursor cells suitable for transplantation; a mixture thereof; and a method for preparing the same. This cell aggregate contains FOXA2 positive nervous system cells or TUJ1 positive nervous system cells, and contains 1000 or more cells.
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 21/02 - Muscle relaxants, e.g. for tetanus or cramps
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
INTERNATIONAL INSTITUTE OF CANCER IMMUNOLOGY, INC. (Japan)
Inventor
Ban, Hitoshi
Takanashi, Yosuke
Abstract
The present disclosure relates to a compound represented by formula (1) [wherein the cancer antigen peptide A represents a MHC class I restricted peptide made of 7 to 30 amino acid residues including at least one cysteine residue; the cysteine residue of the cancer antigen peptide A is bonded to R1by a disulfide bond; R1is a hydrogen atom, a group represented by formula (2) (wherein Xaand Yaindependently represent a single bond or a divalent group of a peptide made of 1 to 4 amino acid residues, the sum of the number of amino acid residues in Xaand the number of amino acid residues in Yais an integer of from 0 to 4, the cancer antigen peptide B represents a MHC class II restricted peptide made of 9 to 30 amino acid residues, the amino group of the N-terminal amino acid of the cancer antigen peptide B bonds with Yain formula (2), the carbonyl group of the C-terminal amino acid of the cancer antigen peptide B bonds with the hydroxyl group in formula (2), and formula (1) and formula (2) are bonded by a disulfide bond), a group represented by formula (3) (wherein Xband Ybindependently represent a single bond or a divalent group of a peptide made of 1 to 4 amino acid residues, the sum of the number of amino acid residues in Xband the number of amino acid residues in Ybis from 0 to 4, the cancer antigen peptide C represents a MHC class II restricted peptide made of 9 to 30 amino acid residues, the carbonyl group of the C-terminal amino acid of the cancer antigen peptide C bonds with Xbin formula (3), the amino group of the N-terminal amino acid of the cancer antigen peptide C bonds with the hydrogen atom in formula (3), and formula (1) and formula (3) are bonded by a disulfide bond), or a cancer antigen peptide D; the cancer antigen peptide D represents a MHC class II restricted peptide made of 9 to 30 amino acid residues including at least one cysteine residue; and the cysteine residue of the cancer antigen peptide D is bonded to R1 by a disulfide bond], or a pharmaceutically acceptable salt of said compound.
Provided are: bitterness-masked drug-containing particles; and a bitterness-masked formulation which uses said drug-containing particles to maintain drug absorption. This invention pertains to: drug-containing particles which have the outer layer thereof coated with sodium stearyl fumarate, and containing (S)-4-amino-5-chloro-N-[{4-[(1-hydroxyacetyl-4-piperidinyl)methyl]-2-morpholinyl}methyl]-2-methoxybenzamide or a pharmacologically acceptable salt thereof, a hydrate thereof or a solvate thereof; and a formulation containing said drug-containing particles.
A61K 47/46 - Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Provided is a method for manufacturing a particle coated with fine particles capable of coating. A method for manufacturing a particle coated with fine particles capable of coating, the manufacturing method characterized by including a step for adding fine particles capable of coating to an inner core including a polymer and a target component, and, while rolling the mixture, performing coating while spraying a solvent capable of dissolving the polymer, the particle coated with fine particles capable of coating being a target-component-containing hollow particle which is coated.
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
The present invention provides an effector memory T cell inducer or MHC class I inducer that is to be used in combination with an immune checkpoint inhibitor, includes a TLR7 agonist, and is for treating or preventing cancer. The present invention also provides a cancer treatment agent or prevention agent that is to be used in combination with an immune checkpoint inhibitor and includes a TLR7 agonist.
Provided are: a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. (In the formula, R1and R21−4 6−106−10 aromatic carbon ring group, a 4 to 10 membered saturated heterocyclic group or the like; R3and R41−61−41−4 alkoxy or the like; R5and R61−61−61−6 alkoxy, an −NRaRbor the like; Raand Rb1−4 1−4 alkyl or the like; X represents a nitrogen atom or a −CRe−; and Re1−61−6 alkyl or the like).
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
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
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
98.
ADAPTER FOR CELL DRUG VESSEL, MULTI-PASSAGE ADAPTER FOR CELL DRUG VESSEL, AND CELL DRUG TRANSFER SYSTEM AND TRANSFER METHOD USING SAME
A cell drug transfer system (10) comprises: an adapter (1) for a cell drug vessel, said adapter (1) comprising a first passage (11) and a second passage (12), both passages allowing the passage of liquids and cells therethrough; a cell drug vessel (2) to which the adapter (1) is installed and which accommodates a cell drug to be transferred; an administration medium accommodation vessel (3) which communicates with the first passage (11) and accommodates an administration medium; a retrieval vessel (4) which is for retrieving the cell drug and communicates with the second passage (12) comprised by the adapter (1); and a powering means (5) which provides power for transferring the administration medium from the administration medium accommodation vessel (3) to the cell drug vessel (2) via the first passage (11), and for transferring the cell drug and the administration medium from the cell drug vessel (2) to the retrieval vessel (4) via the second passage (12).
The present invention provides: a compound (In the formula: R1and R21-46-106-10 aromatic carbon ring or the like; R3, R4and R51-61-41-4 alkoxy, or the like; ring B represents a 5- to 10-membered heteroaromatic ring or the like; R6, R7and R81-61-6 alkyl, -NRaRbor the like; and Raand Rb1-41-4 alkyl or the like) represented by formula (1') which is useful as a therapeutic agent against diseases associated with group II mGlu receptors, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing said compound.
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
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
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
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
The present application provides a substituted purine compound represented by formula (1) and a pharmaceutically acceptable salt thereof, which exhibit a TLR7-inhibiting effect and are useful for therapy, etc., of autoimmune diseases. [In the formula: R11-61-6 alkoxy or the like; R21-61-6 alkyl or the like; ring Q1represents an aromatic carbon ring group or the like; W11-41-4 alkylene or the like; n represents 1, 2, 3, or 4; R3represents a hydrogen atom, a halogen atom, or the like; Q1-X1represents Q12mm-O- or the like, m represents 0, 1, or 2; W2represents a single bond or the like; R4represents an optionally substituted 4- to 10-membered saturated hetero ring or the like; X2represents a single bond or the like; and R51-81-8 alkyl, an optionally substituted 4- to 10-membered saturated heterocyclic group, or the like]
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
