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公开(公告)号：US10980825B2
公开(公告)日：2021-04-20
申请号：US16185258
申请日：2018-11-09
发明人： Masato Yoshikawa , Morihisa Saitoh , Taisuke Kato , Yayoi Nakayama , Tomohiro Seki , Yasuo Nakagawa , Yusuke Tominari , Masaki Seto , Akito Shibuya , Kosuke Hidaka , Zenyu Shiokawa , Yoshihisa Nakada , Michiyo Mochizuki
IPC分类号： A61K31/7084 , A61K31/7076 , A61K47/68 , A61P35/00 , C07H21/00 , C07H21/02
摘要： The present disclosure provides a compound having a STING agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases.
The present disclosure relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.-
公开(公告)号：US20210052600A1
公开(公告)日：2021-02-25
申请号：US16958394
申请日：2018-12-27
发明人： Izumi Kamo , Nele MUELLER-PLOCK
IPC分类号： A61K31/553 , A61K31/55 , A61P1/00 , A61P13/00
摘要： The present invention provides a medicament for use in treating stress urinary incontinence with fewer adverse effects including a body weight lowering effect. The present invention also provides a medicament for use in treating a disease such as incontinence of feces and further provide a medicament for use in treating a disease such as incontinence of feces with fewer adverse effects including a body weight lowering effect.
A medicament for use in treating stress urinary incontinence, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug. A medicament for use in treating incontinence of feces, etc., comprising a 5-HT2C receptor agonist. A medicament for use in treating incontinence of feces, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug.-
公开(公告)号：USRE48334E1
公开(公告)日：2020-12-01
申请号：US15445251
申请日：2017-02-28
发明人： Junya Shirai , Hideyuki Sugiyama , Taku Kamei , Hironobu Maezaki
IPC分类号： C07D401/04 , C07D207/14 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/06 , C07D413/08 , C07D413/14 , C07D417/08
摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.
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公开(公告)号：US10787462B2
公开(公告)日：2020-09-29
申请号：US15769201
申请日：2016-10-21
发明人： Takatoshi Yogo , Masato Yoshikawa , Morihisa Saitoh , Taisuke Katoh , Tomohiro Seki , Yoshihisa Nakada
IPC分类号： C07D519/00 , C07D487/04 , C07D471/04 , C07D513/04 , A61K31/55 , A61K31/553 , A61K31/554 , A61P31/12 , A61P13/12 , A61P1/16 , A61P25/00
摘要： The present invention provides a heterocyclic compound having an RIP1 kinase inhibitory action, which is useful for the prophylaxis or treatment of Gaucher's disease, Niemann-Pick disease, inflammatory bowel disease, multiple sclerosis, chronic kidney disease, acute kidney injury, acute hepatic failure, autoimmune hepatitis, hepatitis B, hepatitis C, alcohol steatohepatitis, non-alcohol steatohepatitis and the like.The present invention relates to a compound represented by the following formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
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公开(公告)号：US10786506B2
公开(公告)日：2020-09-29
申请号：US16065362
申请日：2016-12-21
IPC分类号： A61K31/517 , A61K31/519 , A61P9/04
摘要： The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.
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公开(公告)号：US10745397B2
公开(公告)日：2020-08-18
申请号：US15746828
申请日：2016-07-26
发明人： Dinesh Barawkar , Anil M Deshpande , Santosh Patil , Yogesh Waman , Anil Panmand , Dilip Jadhav , Bheemashankar Kulkarni
IPC分类号： C07D498/04 , C07D471/04 , C07D513/04 , A61P19/02
摘要： The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.
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公开(公告)号：US20200255439A1
公开(公告)日：2020-08-13
申请号：US16651840
申请日：2018-09-27
发明人： Makoto KAMATA , Hideyuki SUGIYAMA , Minoru NAKAMURA , Masataka MURAKAMI , Shuhei IKEDA , Tomohiro OKAWA , Hidekazu TOKUHARA
IPC分类号： C07D487/10 , A61P25/28 , A61K9/48 , A61K9/20
摘要： The present invention provides a compound having an MAGL inhibitory action, and expected to be useful as an agent for the prophylaxis or treatment of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis etc.), anxiety disorder, pains (e.g., inflammatory pain, cancerous pain, neurogenic pain etc.), epilepsy, depression and the like.The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.
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公开(公告)号：US10710989B2
公开(公告)日：2020-07-14
申请号：US16488770
申请日：2018-02-27
IPC分类号： C07D405/14 , C07D231/12 , C07D405/10
摘要： The present invention provides a method of producing a heterocyclic compound useful as an agent for the prophylaxis and/or treatment of Alzheimer's disease and the like. The present invention relates to a method of producing 1,5-anhydro-2,4-dideoxy-2-(4-fluoro-5-methyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-threo-pentitol or a salt thereof, which comprises reacting 4-fluoro-3-hydroxy-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one or a salt thereof, 3-fluoro-2-formyl-4-methyl-5-[4-(1H-pyrazol-1-yl)benzyl]benzoic acid or a salt thereof, or a mixture thereof, with 2-amino-1,5-anhydro-2,4-dideoxy-L-threo-pentitol.
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公开(公告)号：US10668260B2
公开(公告)日：2020-06-02
申请号：US14774385
申请日：2014-03-11
摘要： The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections 4 erected on one support sheet, each microprojection 4 having a drug layer 5 soluble in vivo at its top part and having an intermediate layer 6 under the drug layer 5, the intermediate layer 6 containing a polymeric substance for adhesion of the drug layer 5 to the support sheet, the drug layer 5 at the top part of the microprojection 4 containing a single drug, the microprojections 4 holding difference types of drugs being arranged together on the support sheet 2.
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公开(公告)号：US20200148637A1
公开(公告)日：2020-05-14
申请号：US16739707
申请日：2020-01-10
发明人： TAKASHI OUCHI , GIHO GOH , SUNMI KIM , JINSOON CHOI , HUNSOO PARK
IPC分类号： C07D207/36 , B01J23/44 , C07B61/00 , C07C253/30 , C07C255/42 , C07D401/12 , C07D207/34 , B01J8/02 , B01J21/04 , B01J29/08 , C07B31/00 , C07B41/06 , C07C255/28
摘要： The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.
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