NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Watanabe, Naoki
Satou, Youhei
Takeda, Shin'Ichi
Nagata, Tetsuya
Abstract
The present invention provides a pharmaceutical composition which causes skipping of the 53rd exon in the human dystrophin gene with a high efficiency. The present invention provides an oligomer which efficiently enables to cause skipping of the 53rd exon in the human dystrophin gene.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
2.
CRYSTALLINE SUBSTITUTED PYRAZINES AS PGI2 RECEPTOR AGONISTS
A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as “Compound B”). A form-I crystal of Compound B, which shows peaks at diffraction angles (2θ) of 6.4°, 8.1°, 9.5°, 10.9°, 13.2°, 15.7°, 17.0°, 19.5°, 20.3°, 21.0°, and 22.8° in a powder X-ray diffraction spectrum obtained using a Cu-Kα radiation (λ=1.54 Å). A form-II crystal of Compound B, which shows peaks at diffraction angles (2θ) of 9.6°, 11.4°, 11.7°, 16.3°, 17.5°, 18.5°, 18.7°, 19.9°, 20.1°, 21.0°, and 24.6° in a powder X-ray diffraction spectrum obtained using a Cu-Kα radiation (λ=1.54 Å).
C07D 241/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
National University Corporation Gunma University (Japan)
Inventor
Nakagawa, Shinichiro
Tagaya, Mitsuhiro
Himoto, Takuya
Kiyama, Kaname
Tojo, Akari
Kamitani, Wataru
Abstract
The present specification provides an antisense oligonucleotide or a pharmaceutically acceptable salt or hydrate thereof targeting a particular region in genomic RNA of SARS-CoV-2, a pharmaceutical composition comprising the antisense oligonucleotide or the pharmaceutically acceptable salt or hydrate thereof, etc.
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Aoki, Yoshitsugu
Kunitake, Katsuhiko
Abstract
Disclosed are a cell population of human urine-derived cells positive for CD90, a cell population of myotubes induced from the cell population of the human urine-derived cells positive for CD90, and a method for producing a myotube derived from the human urine-derived cell, comprising a step of separating the human urine-derived cells positive for CD90.
The present invention relates to a method for producing guaiazulene, the method comprising a process for reacting a compound represented by formula (1) or a compound represented by formula (2) in a solvent in the presence of a palladium catalyst, wherein the solvent is composed of at least one substance that is selected from among triglyme, tetraglyme, N-methyl pyrrolidone (NMP), and the like.
C07C 1/24 - Preparation of hydrocarbons from one or more compounds, none of them being a hydrocarbon starting from organic compounds containing only oxygen atoms as hetero atoms by elimination of water
C07C 13/47 - Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with a bicyclo ring system containing ten carbon atoms
C07C 303/04 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof by substitution of hydrogen atoms by sulfo or halosulfonyl groups
C07C 309/25 - Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
12.
METHOD FOR ESTIMATING MICROBIAL GROWTH RATE IN FOOD, METHOD FOR EVALUATING SHELF LIFE OF FOOD, AND SYSTEM FOR ESTIMATING MICROBIAL GROWTH RATE IN FOOD
For providing a method for estimating a microbial growth rate in food that is capable of rapidly and non-destructively evaluating shelf life of food (e.g., best-by date) and the like while reducing cost and labor associated with the evaluation, the present disclosure includes: a step of placing a hydrophilic membrane filter on a surface of a food sample, and inoculating microorganisms on the hydrophilic membrane filter; a step of imaging the microorganisms growing on the hydrophilic membrane filter over time using a microscope; a step of digitizing area of the microorganisms from the image taken over time; and a step of estimating a growth rate of the microorganisms based on the digitized data.
C12Q 1/04 - Determining presence or kind of microorganismUse of selective media for testing antibiotics or bacteriocidesCompositions containing a chemical indicator therefor
C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for the treatment of Duchenne Muscular Dystrophy; Medicines for human purposes; Drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of Duchenne Muscular Dystrophy, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of Duchenne Muscular Dystrophy, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of Duchenne Muscular Dystrophy, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of Duchenne Muscular Dystrophy, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of Duchenne Muscular Dystrophy, both prescription and over-the-counter, for use in connection with humans
27.
ANTISENSE OLIGONUCLEOTIDE TARGETING ATN1 MRNA OR PRE-MRNA
The present invention provides an antisense oligonucleotide that is formed of 15-22 nucleotides and that is complementary to a nucleic acid including at least 15 consecutive bases in a specific target region of a base sequence of SEQ ID NO: 471, or a pharmaceutically acceptable salt thereof, or hydrates of those.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
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
In one embodiment, the object of the present invention is to provide a nephrotoxicity reducing agent for a pharmaceutical composition comprising an antisense oligomer, and a method for reducing nephrotoxicity of the pharmaceutical composition. In one embodiment, the present invention relates to a nephrotoxicity reducing agent for a pharmaceutical composition comprising an antisense oligomer, wherein the nephrotoxicity reducing agent comprises a non-glucose sugar and is used in an amount such that the concentration of the sugar in the pharmaceutical composition is 1 mg/ml to 400 mg/mL.
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Tone, Yuichiro
Aoki, Yoshitsugu
Motohashi, Norio
Abstract
Herein, a combination of antisense oligomers or pharmaceutically acceptable salts thereof, or hydrates thereof which cause simultaneous skipping of any two or more numerically consecutive exons selected from the group consisting of the 45th exon to the 55th exon in human dystrophin pre-mRNA is provided.
National University Corporation Kobe University (Japan)
Inventor
Sonoke, Satoru
Fujiwara, Kae
Satou, Youhei
Wakayama, Tatsushi
Masuda, Hirofumi
Seki, Ryosuke
Matsubara, Takuma
Numakura, Yuki
Okamoto, Kentaro
Toda, Tatsushi
Ikeda, Mariko
Kobayashi, Kazuhiro
Abstract
In one embodiment, the object of the present invention is to provide a nephrotoxicity reducing agent for a pharmaceutical composition comprising an antisense oligomer, and a method for reducing nephrotoxicity of the pharmaceutical composition. In one embodiment, the present invention relates to a nephrotoxicity reducing agent for a pharmaceutical composition comprising an antisense oligomer, wherein the nephrotoxicity reducing agent comprises a sugar alcohol and is used in an amount such that the concentration of the sugar alcohol in the pharmaceutical composition is 1 mg/ml to 400 mg/mL.
In one embodiment, the object of the present invention is to provide a precipitation suppressing agent for an antisense oligomer in urine of a subject to whom a pharmaceutical composition comprising an antisense oligomer has been administered, and a method for suppressing precipitation of an antisense oligomer in urine, in a subject to whom the pharmaceutical composition has been administered. In one embodiment, the present invention relates to a precipitation suppressing agent for an antisense oligomer in urine of a subject to whom a pharmaceutical composition comprising an antisense oligomer has been administered, wherein the precipitation suppressing agent comprises a sugar other than glucose and is used in an amount such that the concentration of the sugar in the pharmaceutical composition is 0.5 mg/mL to 3000 mg/mL.
The present invention relates to a method for producing an oligonucleic acid compound, the method being characterized by (1) treating a compound represented by formula [A-1] and a compound represented by formula [B-1] with a condensation agent in the presence of a base and then (2) treating the compounds with an oxidizing agent and an organic amine to produce a compound represented by formula [C-1] (in the formulae, each symbol is as defined in the description).
The present invention relates to a method for producing an oligonucleic acid compound, the method being characterized by (1) treating a compound represented by formula [A-1] and a compound represented by formula [B-1] with a condensation agent in the presence of a base and then (2) treating the compounds with an oxidizing agent and an organic amine to produce a compound represented by formula [C-1] (in the formulae, each symbol is as defined in the description).
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
National University Corporation Gunma University (Japan)
Inventor
Nakagawa, Shinichiro
Tagaya, Mitsuhiro
Himoto, Takuya
Kamitani, Wataru
Abstract
An object of the present invention is to provide an antiviral nucleic acid, etc. against SARS-COV-2 SARS-COV-2, SARS-COV-1, or MERS-COV and/or a method for treating and/or preventing viral infection using the nucleic acid, etc. The present invention relates to, for example, an antiviral nucleic acid or a pharmaceutically acceptable salt or hydrate thereof targeting a sequence in at least one target region selected from the group consisting of 5′ UTR region, nsp3 region, 3C-like proteinase region, nsp9 region, RNA-dependent RNA polymerase region, helicase region, 3′-to-5′ exonuclease region, 2′-O-ribose methyltransferase region, S region including S1 region and S2 region, E region, M region, and N region in genomic RNA of SARS-COV-2, wherein the virus is SARS-COV-2, SARS-COV-1, or MERS-COV.
HEAT-RESISTANT MOLD GROWTH INHIBITOR, FOOD AND DRINK IN WHICH GROWTH OF HEAT-RESISTANT MOLD IS INHIBITED, AND METHOD FOR INHIBITING GROWTH OF HEAT-RESISTANT MOLD
For providing a heat-resistant mold growth inhibitor capable of inhibiting growth of heat-resistant mold without performing heat treatment at a high temperature, food and drink in which the growth of heat-resistant mold is inhibited, and a method for inhibiting the growth of heat-resistant mold, the heat-resistant mold growth inhibitor according to the present disclosure contains diethyl fumarate and/or 2-decenoic acid as an active component.
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
A represents NR6 and R6 represents a hydrogen atom, alkyl, or the like;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
A represents NR6 and R6 represents a hydrogen atom, alkyl, or the like;
D represents alkylene or alkenylene optionally substituted with hydroxy;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
A represents NR6 and R6 represents a hydrogen atom, alkyl, or the like;
D represents alkylene or alkenylene optionally substituted with hydroxy;
E represents phenylene or a single bond;
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
A represents NR6 and R6 represents a hydrogen atom, alkyl, or the like;
D represents alkylene or alkenylene optionally substituted with hydroxy;
E represents phenylene or a single bond;
G represents O, S, or the like; and
The present invention relates to a therapeutic agent for gait disturbance in a patient with ischemic disease, containing, as an active ingredient, a heterocyclic derivative represented by formula (1) or a pharmaceutically acceptable salt thereof:
wherein R1 and R2 are the same or different and each represents optionally substituted aryl;
R3 and R4 are the same or different and each represents a hydrogen atom or alkyl;
R5 represents a hydrogen atom, alkyl, or a halogen atom;
Y represents N or N->0;
A represents NR6 and R6 represents a hydrogen atom, alkyl, or the like;
D represents alkylene or alkenylene optionally substituted with hydroxy;
E represents phenylene or a single bond;
G represents O, S, or the like; and
Q represents carboxy, alkoxycarbonyl, or the like.
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
A pill container includes a plurality of pill accommodation portions each extending in a first direction and having a volume allowing a predetermined plurality of pills to be accommodated therein. The plurality of pill accommodation portions each include a pair of wall portions extending in the first direction and placed so as to oppose each other. At least one of the pair of wall portions is formed in a corrugated plate shape in which a plurality of mountain portions projecting inwardly toward the other wall portion and a plurality of outwardly recessed valley portions are alternately repeated along the first direction.
A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
A61J 7/00 - Devices for administering medicines orally, e.g. spoonsPill counting devicesArrangements for time indication or reminder for taking medicine
A measuring container comprises a storage container and a storage section selector. The storage container includes storage sections each capable of storing a predetermined number of tablets. The storage section selector is attached to the storage container and has a second path that allows the tablets to pass through from one end to an other end. The one end of the second path is connected to an outside, and the other end is selectively connected to one of the storage sections.
B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, spherical or like small articles, e.g. tablets or pills
38.
COMPOUND SERVING AS DDR1 KINASE INHIBITOR, AND MEDICINE
Provided is a compound having DDR1 inhibitory activity and represented by general formula (I), or a pharmaceutically acceptable salt or solvate thereof, and pharmaceutical use of the same.
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
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 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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
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 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 35/02 - Antineoplastic agents specific for leukemia
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 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention relates to a composition containing an antisense oligonucleotide, and the use thereof to treat Duchenne muscular dystrophy. The present invention particularly relates to the above-described composition that is effective for the treatment of Duchenne muscular dystrophy when it is administered at a dose for the treatment, and the use thereof.
A flow liquid separation device comprising: an inlet through which a liquid mixture of a first liquid and a second liquid that are phase-separable from each other is supplied; a body that stores the liquid mixture; a phase separation unit that has a first outlet which is connected to the body and through which the first liquid can be discharged, and a second outlet which is connected to the body and is located upstream of the first outlet, and through which the second liquid is allowed to overflow; and an interface adjustment unit that is connected to one of the first and second outlets, and that adjusts the position of the interface between the first and second liquids that are phase-separated from each other in the phase separation unit, wherein the position of the interface is adjusted between the first and second outlets in the vertical direction.
B01D 17/032 - Separation of non-miscible liquids by gravity, in a settling tank provided with special equipment for removing at least one of the separated liquids
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
Provided are: a solid dispersion comprising at least one compound selected from the group consisting of a hetero ring derivative represented by general formula [1], a tautomer of the hetero ring derivative, and a pharmaceutically acceptable salt of the hetero ring derivative or the tautomer, and a pharmaceutically acceptable polymer; and a pharmaceutical preparation containing the solid dispersion.
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 31/423 - Oxazoles condensed with carbocyclic rings
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
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 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
The present invention provides a pharmaceutical composition containing a pharmaceutically acceptable salt of (2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (compound B) with good storage stability. The present invention is a pharmaceutical composition containing the following components: (A) a pharmaceutically acceptable salt of (2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid; (B) a buffering agent 1 having a buffering capacity in a basic region, and a buffering agent 2 having a buffering capacity in a neutral region, or a buffering agent 3 having a buffering capacity in a basic region to a neutral region; and (C) a pH-adjusting agent.
In the description of the present invention, provided is an antisense oligonucleotide, or a pharmaceutically acceptable salt thereof, which comprises 15-22 nucleotides, and which is complementary to a nucleic acid including at least 15 consecutive bases in a target region selected from the group consisting of, from 5' end of the base sequence of SEQ ID NO: 1, position 1 to position 102, position 159 to position 842, position 879 to position 1822, and position 1874 to position 4182.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
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
47.
COMPOUND SERVING AS DDR1 KINASE INHIBITOR, AND MEDICINE
The present invention provides a compound represented by general formula[1] and having a DDR1 kinase inhibitory activity, a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt (in the formula, R1represents a hydrogen atom, a halogen atom, an optionally substituted alkyl group; Het represents a 5- to 10-membered heteroaryl group; L1represents -CO-NH- or -CRa=CRb-; X represents C-Rc; R216166 haloalkyl group; R3, R4366 cycloalkyl group or an optionally substituted heterocycloalkyl group).
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/34 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
The purpose of the present invention is to provide a method for estimating the rate of microbial growth in a food that enables non-destructive and quick evaluation of the shelf life (for example, best before date), etc. of the food while reducing the cost and labor required for the evaluation. To solve this problem, provided is a method comprising: a step for placing a hydrophilic membrane filter 6 on the surface of a food sample 5 and inoculating a microorganism 7 on the hydrophilic membrane filter 6; a step for imaging the microorganism 7 growing on the hydrophilic membrane filter 6 over time using a microscope; a step for quantifying the area of the microorganism 7 from the images taken over time; and a step for estimating the growth rate of the microorganism 7 on the basis of the quantified data.
A form-II crystal of Compound B, which shows peaks at diffraction angles (2θ) of 9.6°, 11.4°, 11.7°, 16.3°, 17.5°, 18.5°, 18.7°, 19.9°, 20.1°, 21.0°, and 24.6° in a powder X-ray diffraction spectrum obtained using a Cu-Kα radiation (λ=1.54 Å).
C07D 241/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
The present invention relates to a novel therapeutic agent for high-risk myelofibrosis, said agent containing a compound represented by general formula [1] (in the formula, R1, R2, R3, R4, R5, and X are as defined in the description) or a pharmaceutically acceptable salt thereof as an active ingredient.
The present invention relates to a novel therapeutic agent for high-risk myelofibrosis, said agent containing a compound represented by general formula [1] (in the formula, R1, R2, R3, R4, R5, and X are as defined in the description) or a pharmaceutically acceptable salt thereof as an active ingredient.
In the present description, there are provided; a nucleic acid having a carrier peptide linked thereto, or a pharmaceutically acceptable salt of the nucleic acid, or a hydrate of the nucleic acid or the pharmaceutically acceptable salt; and others. The nucleic acid having a carrier peptide linked thereto or the pharmaceutically acceptable salt of the nucleic acid or the hydrate of the nucleic acid or the pharmaceutically acceptable salt comprises: a nucleic acid capable of regulating the splicing of pre-mRNA or inhibiting the function of targeted RNA or a target region in the RNA or a pharmaceutically acceptable salt of the nucleic acid or a hydrate of the nucleic acid or the pharmaceutically acceptable salt; and a carrier peptide that is linked to the nucleic acid, the pharmaceutically acceptable salt of the nucleic acid or the hydrate of the nucleic acid or the pharmaceutically acceptable salt and comprises the amino acid sequence represented by the formula KKRTLRKSNRKKR (SEQ ID NO:1) or an amino acid sequence having such a structure that one or two amino acid residues in SEQ ID NO:1 are added, deleted or substituted (provided that an amino acid sequence in which both of amino acid residues located at position-8 and position-9 from the N-terminal of SEQ ID NO:1 are substituted is excluded). In the nucleic acid having a carrier peptide linked thereto, or a pharmaceutically acceptable salt of the nucleic acid, or a hydrate of the nucleic acid or the pharmaceutically acceptable salt, the nucleic acid is selected from the group consisting of an antisense oligomer, siRNA and shRNA.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 31/80 - Polymers containing hetero atoms not provided for in groups
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 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
C12N 15/87 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY (Japan)
Inventor
Nakagawa Shinichiro
Tagaya Mitsuhiro
Himoto Takuya
Kamitani Wataru
Abstract
The present specification provides an antisense oligomer that has a length of 15-30 bases and that has a base sequence complementary to the base sequence of a target region, a pharmaceutically acceptable salt thereof, or a hydrate of the same. The target region has: a base sequence that is consecutive by at least 10 times and that is in at least one region selected from the group consisting of the 5' UTR region, the nsp1 region, the nsp10 region, the RNA-dependent RNA polymerase region, the ORF10 region, and the 3' UTR region in the genome RNA of SARS-CoV-2; or a sequence complementary to said base sequence. The antisense oligomer, or the pharmaceutically acceptable salt thereof, or the hydrate of the same has an antiviral effect with respect to a virus selected from the group consisting of SARS-CoV-2, SARS-CoV-1, and MERS-CoV.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
A main object of the present invention is to provide new crystals of (S)-N2-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter, referred to as “compound A”). A Form-I crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu Kα radiation (λ=1.54 Å). A Form-II crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ: 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu Kα radiation (λ=1.54 Å).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention provides a compound indicated by general formula (1) and having mPGES-1 inhibitory activity, a pharmaceutically acceptable salt thereof, or a solvate thereof (in the formula, R1and R2each independently indicate hydrogen, halogen, or a substitutable alkyl, R322R5or –COR5, R4indicates a substitutable alkyl, cycloalkyl, aryl, heteroaryl, saturated heterocyclic group, or arylalkyl, and R5 indicates a substitutable alkyl, cycloalkyl, aryl, heteroaryl, saturated heterocyclic group, alkenyl, or arylalkyl.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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 31/454 - 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 31/501 - 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
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 9/00 - Drugs for disorders of the cardiovascular system
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 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 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/04 - 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 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
The present invention relates to a method for producing a morpholino nucleic acid oligomer (each symbol is as defined in the description), the method including a step for treating a compound of formula (II) using a solution that contains an acid and a scavenger in an elongation reaction of a morpholino nucleic acid oligomer represented by the formula and removing R1 from the compound of formula (II) to produce a compound of formula (III).
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of myelofibrosis, eosinophilic granulomatosis with polyangiitis and endometriosis, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of myelofibrosis, eosinophilic granulomatosis with polyangiitis and endometriosis, both prescription and over-the-counter, for use in connection with humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medical and pharmaceutical preparations, for the treatment of myelofibrosis, eosinophilic granulomatosis with polyangiitis and endometriosis, both prescription and over-the-counter, for use in connection with humans
60.
ANTISENSE OLIGONUCLEOTIDE TARGETING ATN1 MRNA OR PRE-MRNA
The present invention provides an antisense oligonucleotide that is formed of 15-22 nucleotides and that is complementary to a nucleic acid including at least 15 consecutive bases in a specific target region of a base sequence of SEQ ID NO: 471, or a pharmaceutically acceptable salt thereof, or hydrates of those.
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
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
61.
HEAT-RESISTANT MOLD GROWTH INHIBITOR, FOOD AND DRINK IN WHICH GROWTH OF HEAT-RESISTANT MOLD IS INHIBITED, AND METHOD FOR INHIBITING GROWTH OF HEAT-RESISTANT MOLD
In order to provide a heat-resistant mold growth inhibitor capable of inhibiting the growth of heat-resistant mold without carrying out heat treatment at a high temperature, food and drink in which the growth of heat-resistant mold is inhibited, and a method for inhibiting the growth of heat-resistant mold, a heat-resistant mold growth inhibitor according to the present invention comprises, as active components thereof, diethyl fumarate and/or 2-decenoic acid.
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Watanabe, Naoki
Satou, Youhei
Takeda, Shin'Ichi
Nagata, Tetsuya
Abstract
The present invention provides an oligomer which efficiently enables to cause skipping of the 53rd exon in the human dystrophin gene. Also provided is a pharmaceutical composition which causes skipping of the 53rd exon in the human dystrophin gene with a high efficiency.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
63.
ANTISENSE NUCLEIC ACID INDUCING SKIPPING OF EXON 51
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Honda, Yu
Muchima, Kaname
Fukui, Takahiro
Hasegawa, Saki
Takeda, Shin'Ichi
Aoki, Yoshitsugu
Abstract
The present specification provides a drug that causes highly-efficient skipping of exon 51 in the human dystrophin gene. The present specification provides an antisense oligomer having an activity to induce skipping of exon 51 in the human dystrophin gene.
NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY (Japan)
Inventor
Nakagawa Shinichiro
Tagaya Mitsuhiro
Himoto Takuya
Muchima Kaname
Tojo Akari
Kamitani Wataru
Abstract
In the present description, provided are an antisense oligonucleotide targeting a specific region of the genomic RNA of SARS-CoV-2, a pharmaceutically acceptable salt thereof or a hydrate of the same, a pharmaceutical composition containing the antisense oligonucleotide, a pharmaceutically acceptable salt thereof or a hydrate of the same, etc.
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.
The compound of the present invention has an inhibitory activity against the PDGF receptor kinase. In addition, since the compound of the present invention has an inhibitory activity against the PDGF receptor kinase, it is useful as a therapeutic agent for respiratory diseases, cancers, smooth muscle proliferative diseases, vasoproliferative diseases, autoimmune/inflammatory diseases, metabolic diseases, vasoocclusive diseases, and the like.
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 263/34 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring 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 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon 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
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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 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 413/12 - 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
A61P 11/00 - Drugs for disorders of the respiratory system
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Honda, Yu
Muchima, Kaname
Fukui, Takahiro
Hasegawa, Saki
Takeda, Shin'Ichi
Aoki, Yoshitsugu
Abstract
The present specification provides a drug that causes highly-efficient skipping of exon 51 in the human dystrophin gene. The present specification provides an antisense oligomer having an activity to induce skipping of exon 51 in the human dystrophin gene.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
67.
PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR CHRONIC PROSTATITIS/CHRONIC PELVIC PAIN SYNDROME
The present invention relates to a prophylactic and/or therapeutic agent for chronic prostatitis/chronic pelvic pain syndrome, the agent containing an mPGES-1 inhibitor as an active ingredient.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations; pharmaceutical preparations for the treatment of Duchenne muscular dystrophy; medicines for human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes; reagent paper
for medical purposes; dental materials; diapers; diaper
covers; fly catching paper; mothproofing paper; lacteal
flour for babies; dietary supplements for humans; dietetic
beverages adapted for medical purposes; dietetic foods
adapted for medical purposes; beverages for babies; food for
babies; dietary supplements for animals; semen for
artificial insemination; dietary fiber.
70.
ANTISENSE NUCLEIC ACID THAT INDUCES SKIPPING OF EXON 50
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Enya, Yukiko
Sunadoi, Yuta
Waki, Reiko
Muchima, Kaname
Takeda, Shin'Ichi
Aoki, Yoshitsugu
Abstract
The present specification provides a drug that causes highly-efficient skipping of exon 50 in the human dystrophin gene. The present specification provides an antisense oligomer which induces skipping of exon 50 in the human dystrophin gene.
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Watanabe, Naoki
Tone, Yuichiro
Takeda, Shin'Ichi
Aoki, Yoshitsugu
Abstract
The present specification provides an antisense oligomer capable of causing simultaneous skipping of a plurality of exons in pre-mRNA of interest, and a pharmaceutical composition comprising the oligomer. The present specification also provides an antisense oligomer or a pharmaceutically acceptable salt thereof, or hydrate thereof which causes simultaneous skipping of two or more numerically consecutive exons from pre-mRNA of interest, the antisense oligomer comprising a base sequence complementary to a base sequence of a region including the vicinity of a donor of any intron in the pre-mRNA of interest, or a region including the vicinity of an acceptor of any intron in the pre-mRNA of interest, or a partial base sequence thereof.
The present invention relates to a prophylactic and/or therapeutic agent for cancer containing an mPGES-1 inhibitor as an active ingredient, the agent being useful in combination with an immune checkpoint inhibitor, and the invention has industrial applicability.
The present invention relates to a method for producing a compound [C] of the general formula [C] by subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a phosphorous atom-containing substituent group of the general formula [1] to a condensation reaction, characterized in that the method is carried out in the presence of at least one reaction accelerator selected from the group consisting of a quaternary ammonium salt, a quaternary imidazolium salt, a quaternary morpholinium salt, a quaternary phosphonium salt, a quaternary piperidinium salt, a quaternary pyridinium salt, a quaternary pyrrolidinium salt and a quaternary sulfonium salt.
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C07H 1/00 - Processes for the preparation of sugar derivatives
The present invention relates to a method for producing a compound represented by general formula [C-1-1], which comprises: a step for reacting a compound represented by general formula [B-1-1] with a compound represented by general formula [P] to form a compound represented by general formula [B-1-2]; and a step for reacting the compound represented by general formula [B-1-2] with a compound represented by general formula [A-1] to form the compound represented by general formula [C-1-1].
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
[Problem] In one embodiment, the present invention addresses the problem of providing: a nephrotoxicity reducing agent for a pharmaceutical composition containing an antisense oligomer; and a method for reducing nephrotoxicity of said pharmaceutical composition. [Solution] In one embodiment, the present invention pertains to a nephrotoxicity reducing agent that is for an pharmaceutical composition containing an antisense oligomer and that contains a sugar which is not glucose and which is contained at a concentration of 1-400 mg/mL in the pharmaceutical composition.
[Problem] In one embodiment, the present invention addresses the problem of providing: a nephrotoxicity reducing agent for a pharmaceutical composition containing an antisense oligomer; and a method for reducing nephrotoxicity of said pharmaceutical composition. [Solution] In one embodiment, the present invention pertains to a nephrotoxicity reducing agent that is for an pharmaceutical composition containing an antisense oligomer and that contains a sugar which is not glucose and which is contained at a concentration of 1-400 mg/mL in the pharmaceutical composition.
[Problem] In an embodiment, the present invention addresses the problem of providing a precipitation inhibitor for antisense oligomers in the urine for a subject to whom an antisense oligomer-containing drug composition has been administered, and providing a method for inhibiting the precipitation of antisense oligomers in the urine in a subject to whom said drug composition has been administered. [Solution] In an embodiment, the present invention relates to a precipitation inhibitor for antisense oligomers in the urine for a subject to whom an antisense oligomer-containing drug composition has been administered, wherein the precipitation inhibitor contains a sugar that is not glucose and is used in an amount that gives a sugar concentration in the drug composition of 0.5-3000 mg/mL.
NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY (Japan)
Inventor
Sonoke Satoru
Fujiwara Kae
Satou Youhei
Wakayama Tatsushi
Masuda Hirofumi
Seki Ryosuke
Matsubara Takuma
Numakura Yuki
Okamoto Kentaro
Toda Tatsushi
Ikeda Mariko
Kobayashi Kazuhiro
Abstract
[Problem] In an embodiment, the present invention addresses the problem of providing a nephrotoxicity reducing agent for a medical composition including an antisense oligomer, and a method for reducing nephrotoxicity of said medical composition. [Solution] In an embodiment, the present invention relates to a nephrotoxicity reducing agent for a medical composition including an antisense oligomer, the nephrotoxicity reducing agent including a sugar alcohol and being used in an amount such that the concentration of the sugar alcohol in the medical composition is 1-400 mg/mL.
[Problem] In an embodiment, the present invention addresses the problem of providing a precipitation suppressing agent for antisense oligomers in the urine for a subject to whom an antisense oligomer-containing drug composition has been administered, and providing a method for suppressing the precipitation of antisense oligomers in the urine in a subject to whom said drug composition has been administered. [Solution] In an embodiment, the present invention relates to a precipitation suppressing agent for antisense oligomers in the urine for a subject to whom an antisense oligomer-containing drug composition has been administered, wherein the precipitation suppressing agent contains a sugar that is not glucose and is used in an amount that gives a sugar concentration in the drug composition of 0.5-3000 mg/mL.
The purpose of the present invention is to provide a compound having M3 PAM activity.
The purpose of the present invention is to provide a compound having M3 PAM activity.
Examples of the present invention include azabenzimidazole compounds represented by the following formula [1] and pharmaceutically acceptable salts thereof.
The purpose of the present invention is to provide a compound having M3 PAM activity.
Examples of the present invention include azabenzimidazole compounds represented by the following formula [1] and pharmaceutically acceptable salts thereof.
The purpose of the present invention is to provide a compound having M3 PAM activity.
Examples of the present invention include azabenzimidazole compounds represented by the following formula [1] and pharmaceutically acceptable salts thereof.
The compounds of the present invention have M3 PAM activity. In addition, since the compounds of the present invention have M3 PAM activity, the compounds of the present invention are useful as preventive agents or therapeutic agents for urination disorders and urine collection disorders in underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, and neurogenic bladder.
A novel prophylactic agent or therapeutic agent for functional gastrointestinal disorders or xerostomia is provided. The present invention is a therapeutic agent or prophylactic agent for functional gastrointestinal disorders, containing an azabenzimidazole compound represented by the following formula [1] (each symbol in the formula is as described in the specification), or a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient.
A novel prophylactic agent or therapeutic agent for functional gastrointestinal disorders or xerostomia is provided. The present invention is a therapeutic agent or prophylactic agent for functional gastrointestinal disorders, containing an azabenzimidazole compound represented by the following formula [1] (each symbol in the formula is as described in the specification), or a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient.
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Tone, Yuichiro
Aoki, Yoshitsugu
Motohashi, Norio
Abstract
In the present description, provided is a combination of antisense oligomers, which induce simultaneous skipping of any two or more exons, said exons being consecutive in numerical order, selected from the group consisting of the 45th exon to the 55th exon in the human dystrophin pre-mRNA, pharmaceutically acceptable salts thereof or hydrates of the same.
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
A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
A61K 31/7125 - Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Tone Yuichiro
Aoki Yoshitsugu
Motohashi Norio
Abstract
In the present description, provided is a combination of antisense oligomers, which induce simultaneous skipping of any two or more exons, said exons being consecutive in numerical order, selected from the group consisting of the 45th exon to the 55th exon in the human dystrophin pre-mRNA, pharmaceutically acceptable salts thereof or hydrates of the same.
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
A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
A61K 31/7125 - Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
In order to provide a nutritional composition that has a shape that is easy to administer or ingest, that does not exhibit a marked reduction in viscosity under acidity (when mixed with gastric juices), and that has excellent nutrients, the nutritional composition according to one embodiment of the present invention includes casein, collagen, and a thickener, where the thickener does not have a gelling property that is exhibited when cooled after heating, and is soluble in an acid.
A23L 29/238 - Foods or foodstuffs containing additivesPreparation or treatment thereof containing gelling or thickening agents of vegetable origin from seeds, e.g. locust bean gum or guar gum
A23L 29/256 - Foods or foodstuffs containing additivesPreparation or treatment thereof containing gelling or thickening agents of vegetable origin from seaweeds, e.g. alginates, agar or carrageenan
A23L 29/269 - Foods or foodstuffs containing additivesPreparation or treatment thereof containing gelling or thickening agents of microbial origin, e.g. xanthan or dextran
The present invention relates to a novel cytokine storm inhibitor containing, as an active ingredient, a compound represented by general formula [1]: [in the formula, R1R2, R3, R4, R5, and X are as defined in the description], or a pharmacologically acceptable salt thereof.
The present invention relates to a method for producing an oligonucleic acid compound, the method being characterized by (1) treating a compound represented by formula [A-1] and a compound represented by formula [B-1] with a condensing agent in the presence of a base and then (2) treating the compounds with an oxidizing agent and an organic amine to produce a compound represented by formula [C-1] (in the formulae, each symbol is as defined in the description).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY (Japan)
Inventor
Nakagawa Shinichiro
Tagaya Mitsuhiro
Himoto Takuya
Kamitani Wataru
Abstract
The present invention addresses the problem of providing: an antiviral nucleic acid, etc., against SARS-CoV-2 SARS-CoV-2, SARS-CoV-1, or MERS-CoV; and/or a method for treating and/or preventing a viral infection using the nucleic acid, etc. The present invention relates to an antiviral nucleic acid that targets a sequence in at least one target region selected from the group consisting of the 5' UTR region, nsp3 region, 3C-like proteinase region, nsp9 region, RNA-dependent RNA polymerase region, helicase region, 3'-to-5' exonuclease region, 2'-O-ribose methyltransferase region, S region including S1 region and S2 region, E region, M region, and N region in the genomic RNA of SARS-CoV-2, or a pharmacologically acceptable salt thereof or a hydrate of these, etc., wherein the virus is SARS-CoV-2, SARS-CoV-1, or MERS-CoV.
The present invention relates to a method for producing an oligonucleic acid compound, the method being characterized by (1) treating a compound represented by formula [A-1] and a compound represented by formula [B-1] with a condensing agent in the presence of a base and then (2) treating the compounds with an oxidizing agent and an organic amine to produce a compound represented by formula [C-1] (in the formulae, each symbol is as defined in the description).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
89.
Antisense nucleic acid that induces skipping of exon 50
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY (Japan)
Inventor
Enya, Yukiko
Sunadoi, Yuta
Waki, Reiko
Muchima, Kaname
Takeda, Shin'Ichi
Aoki, Yoshitsugu
Abstract
The present specification provides a drug that causes highly-efficient skipping of exon 50 in the human dystrophin gene. The present specification provides an antisense oligomer which induces skipping of exon 50 in the human dystrophin gene.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
The present invention relates to a therapeutic agent for a gait disturbance of a patient associated with an ischemic disease, the therapeutic agent containing, as an active ingredient, a heterocyclic derivative represented by general formula (1) or a pharmaceutically acceptable salt thereof. In formula (1), R1 and R2, which may be the same or different, each represent aryl that may be substituted; R3 and R4, which may be the same or different, each represent a hydrogen atom or alkyl; R5 represents a hydrogen atom, alkyl or a halogen atom; Y represents N or N?O; A represents NR6 and R6 represents a hydrogen atom, alkyl or the like; D represents alkylene or alkenylene that may be substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, or the like; and Q represents carboxy, alkoxycarbonyl, or the like.
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
The present invention relates to a therapeutic agent for a gait disturbance of a patient associated with an ischemic disease, the therapeutic agent containing, as an active ingredient, a heterocyclic derivative represented by general formula (1) or a pharmaceutically acceptable salt thereof. In formula (1), R1and R2, which may be the same or different, each represent aryl that may be substituted; R3and R4, which may be the same or different, each represent a hydrogen atom or alkyl; R5represents a hydrogen atom, alkyl or a halogen atom; Y represents N or N→O; A represents NR6and R6 represents a hydrogen atom, alkyl or the like; D represents alkylene or alkenylene that may be substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, or the like; and Q represents carboxy, alkoxycarbonyl, or the like.
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
The present invention relates to a novel salt of 2-(4-(5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (hereinafter referred to as “Compound B”) and a crystal of the salt thereof.
C07D 241/28 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes; reagent paper
for medical purposes; dental materials; diapers; diaper
covers; fly catching paper; mothproofing paper; lacteal
flour for babies; dietary supplements for humans; dietetic
beverages adapted for medical purposes; dietetic foods
adapted for medical purposes; beverages for babies; food for
babies; dietary supplements for animals; semen for
artificial insemination; dietary fiber.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
the treatment of Duchenne muscular dystrophy; medicines for
human purposes; drugs for medical purposes; reagent paper
for medical purposes; dental materials; diapers; diaper
covers; fly catching paper; mothproofing paper; lacteal
flour for babies; dietary supplements for humans; dietetic
beverages adapted for medical purposes; dietetic foods
adapted for medical purposes; beverages for babies; food for
babies; dietary supplements for animals; semen for
artificial insemination; dietary fiber.
