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公开(公告)号:US09808445B2
公开(公告)日:2017-11-07
申请号:US15303322
申请日:2015-04-10
发明人: Isao Sakurada , Tomokazu Hirabayashi , Yoshitaka Maeda , Hiroshi Nagasue , Takashi Mizuno , Jiayi Xu , Ting Zhang , Cameron Smith , Dann Parker
IPC分类号: A61K31/501 , A61K31/439 , C07D413/14 , C07D261/20 , C07D413/04 , C07D498/04 , C07D209/52 , C07D519/00 , A61K31/444 , A61K31/506 , A61K45/06
CPC分类号: A61K31/439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/52 , C07D261/20 , C07D413/04 , C07D413/14 , C07D498/04 , C07D519/00
摘要: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
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公开(公告)号:US09708308B2
公开(公告)日:2017-07-18
申请号:US14652237
申请日:2013-12-16
发明人: Cameron James Smith , John Qiang Tan , Ting Zhang , James Balkovec , William John Greenlee , Liangqin Guo , Yi-Heng Chen , Yili Chen , Jiayi Xu , Samuel Chackalamannil , Tomokazu Hirabayashi , Hiroshi Nagasue , Kouki Ogawa
IPC分类号: C07D471/04 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
CPC分类号: C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
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公开(公告)号:US20170027916A1
公开(公告)日:2017-02-02
申请号:US15303322
申请日:2015-04-10
发明人: Isao Sakurada , Tomokazu Hirabayashi , Yoshitaka Maeda , Hiroshi Nagasue , Takashi Mizuno , Jiayi Xu , Ting Zhang , Cameron Smith , Dann Parker
IPC分类号: A61K31/439 , A61K45/06 , A61K31/444 , A61K31/506 , A61K31/501 , C07D519/00 , C07D413/14 , C07D498/04
CPC分类号: A61K31/439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/52 , C07D261/20 , C07D413/04 , C07D413/14 , C07D498/04 , C07D519/00
摘要: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译: 在其许多实施方案中,本发明提供了由式(I)表示的新一类苯甲酰胺化合物或其药学上可接受的盐或溶剂化物,或包含一种或多种所述化合物或其药学上可接受的盐或溶剂化物的药物组合物,以及使用 所述化合物或其药学上可接受的盐或溶剂合物用于治疗或预防血栓形成,栓塞,高凝状态或纤维变性。
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公开(公告)号:US10399945B2
公开(公告)日:2019-09-03
申请号:US16138369
申请日:2018-09-21
发明人: Fumihiko Saitoh , Hiroshi Nagasue
IPC分类号: C07D213/89 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , A61P17/06 , A61P25/00 , A61P35/00 , C07D213/75 , A61K31/4418 , A61K31/506 , A61K31/4439 , A61K31/444 , C07D213/84 , A61K31/4433 , C07D405/14 , C07D213/81 , C07D413/12 , A61K45/06 , A61K45/00 , C07C213/10 , C07C215/44 , A61P1/16 , A61P1/02 , A61P31/00 , A61P3/06 , A61P3/04 , A61P1/00 , A61P21/02 , A61P13/02 , A61P11/00 , A61P37/06 , A61P25/24 , A61P15/00 , A61P29/02 , A61P13/10 , A61P25/04 , A61P25/16 , A61P25/20 , A61P21/00 , A61P9/06 , A61P9/00 , A61P25/28 , A61P29/00 , A61P5/14 , A61P35/02 , A61P19/10 , A61P1/18 , A61P37/00 , A61P13/08 , A61P31/18 , A61P11/04 , A61P17/00 , A61P13/12 , A61P11/06 , A61P11/02 , A61P1/04 , A61P19/02 , A61P43/00 , A61P7/00 , A61P9/12 , A61P25/08 , A61P3/10
摘要: The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound represented by formula (I):
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公开(公告)号:US11325895B2
公开(公告)日:2022-05-10
申请号:US16647223
申请日:2018-09-13
发明人: Yuji Kawada , Fumihiko Saitoh , Hiroshi Nagasue , Tsutomu Satoh
IPC分类号: C07D401/04
摘要: Provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea which are useful as bulk pharmaceutical crystals. Also provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea having excellent TrkA inhibitory effect, medicines and medicinal composition containing these crystals, and a method for producing these crystals.
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公开(公告)号:US10669239B2
公开(公告)日:2020-06-02
申请号:US16514835
申请日:2019-07-17
发明人: Fumihiko Saitoh , Hiroshi Nagasue
IPC分类号: C07D213/75 , C07D401/04 , C07D405/04 , C07D413/06 , C07D417/04 , A61P25/04 , A61K31/4418 , A61K31/506 , A61K31/4439 , A61K31/444 , C07D213/84 , A61K31/4433 , C07D405/14 , C07D213/81 , C07D413/12 , A61K45/06 , A61P37/00 , A61P1/02 , A61P7/00 , A61P13/08 , A61P21/00 , A61P25/20 , A61P25/28 , A61P31/00 , A61P43/00 , A61P1/16 , A61P9/00 , A61P9/06 , A61P11/06 , A61P37/06 , A61P1/18 , A61P3/04 , A61P3/06 , A61P11/04 , A61P17/00 , A61P19/02 , A61P29/02 , A61P31/18 , A61P35/02 , A61P3/10 , A61P9/12 , A61P13/02 , A61P13/10 , A61P13/12 , A61P21/02 , A61P25/24 , A61P1/00 , A61P11/00 , A61P15/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P29/00 , A61P1/04 , A61P5/14 , A61P11/02 , A61P19/10 , A61P35/00 , A61K45/00 , C07C213/10 , C07C215/44 , C07C271/24
摘要: The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound
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