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公开(公告)号:EP3131896B1
公开(公告)日:2019-01-30
申请号:EP15779184.9
申请日:2015-04-10
Inventor: SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC: C07D413/14 , C07D261/20 , C07D207/02 , A61K31/439
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公开(公告)号:EP3229801A1
公开(公告)日:2017-10-18
申请号:EP15866965.5
申请日:2015-12-07
Inventor: ZHANG, Ting , CHEN, Yi-Heng , GUO, Liangqin , HRUZA, Alan , JIAN, Tianying , LI, Bing , MENG, Dongfang , PARKER, Dann, L., Jr. , SHERER, Edward, C. , WOOD, Harold, B. , SAKURADA, Isao
IPC: A61K31/4184 , C07D235/04
Abstract: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
Abstract translation: 本发明提供式I化合物和包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防不稳定心绞痛,难治性心绞痛,心肌梗塞,短暂性脑缺血发作,心房纤颤,血栓性中风,栓塞 中风,深静脉血栓形成,弥散性血管内凝血,纤维蛋白的眼部积聚以及再通血管的再闭塞或再狭窄。 这些化合物是选择性因子IXa抑制剂。
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公开(公告)号:EP2934537A1
公开(公告)日:2015-10-28
申请号:EP13866418.0
申请日:2013-12-16
Inventor: SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , CHEN, Yi-Heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , KATSUNO, Mika
IPC: A61K31/5377 , C07D413/12
CPC classification number: C07D413/14 , C07D413/12 , C07D513/04
Abstract: The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently 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, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
Abstract translation: 本发明提供式(I)(结构表示)的化合物,其中R 1,R 2,R 3和R 4独立地为H或C 1-6烷基,条件是当R 1,R 2和R 3为H时,R 4为C 1-6烷基 当R 1,R 2和R 4是H时,R 3是C 1-6烷基,并且当R 1,R 3和R 4是H时,R 2是C 1-6烷基,并且当R 2,R 3和R 4是H时,R 1是 C 1-6烷基; 以及包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防血栓形成,栓塞,高凝状态或纤维化改变的方法。
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公开(公告)号:EP3131897A1
公开(公告)日:2017-02-22
申请号:EP15780578.9
申请日:2015-04-10
Inventor: SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC: C07D413/14 , C07D261/20 , C07D207/02
CPC classification number: C07D413/14 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K45/06 , C07D413/04 , C07D417/14 , C07D471/04 , C07D498/04 , C07D519/00
Abstract: 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.
Abstract translation: 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合物,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合物的药物组合物,以及使用 所述化合物或其药学上可接受的盐或溶剂化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:EP3229801B1
公开(公告)日:2020-04-01
申请号:EP15866965.5
申请日:2015-12-07
Inventor: ZHANG, Ting , CHEN, Yi-Heng , GUO, Liangqin , HRUZA, Alan , JIAN, Tianying , LI, Bing , MENG, Dongfang , PARKER, Dann, L., Jr. , SHERER, Edward, C. , WOOD, Harold, B. , SAKURADA, Isao
IPC: A61K31/4184 , C07D235/04
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公开(公告)号:EP2934537B1
公开(公告)日:2018-04-04
申请号:EP13866418.0
申请日:2013-12-16
Inventor: SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , CHEN, Yi-Heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , KATSUNO, Mika
IPC: A61K31/5377 , C07D413/12 , C07D413/14 , C07D513/04
CPC classification number: C07D413/14 , C07D413/12 , C07D513/04
Abstract: The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently 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, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
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公开(公告)号:EP3131896A1
公开(公告)日:2017-02-22
申请号:EP15779184.9
申请日:2015-04-10
Inventor: SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC: C07D413/14 , C07D261/20 , C07D207/02
CPC classification number: A61K31/439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/52 , C07D261/20 , C07D413/04 , C07D413/14 , C07D498/04 , C07D519/00
Abstract: 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.
Abstract translation: 在其许多实施方案中,本发明提供了一类由式(I)表示的新型苯甲酰胺化合物或其药学上可接受的盐或溶剂合物,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化物用于治疗或预防血栓形成,栓塞,高凝状态或纤维化改变。
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公开(公告)号:EP2934538A1
公开(公告)日:2015-10-28
申请号:EP13873301.9
申请日:2013-12-16
Inventor: SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , XU, Jiayi , CHEN, Yi-heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , NAGASUE, Hiroshi , OGAWA, Kouki
IPC: A61K31/5377 , C07D413/12
CPC classification number: C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: 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.
Abstract translation: 本发明提供式(I)(结构表示)的化合物,其中R 1为H或C 1-6烷基,R 2为H或C 1-6烷基或CH 2 OH,R 3为H或C 1-6烷基,且R 4为H或 条件是当R 1,R 2和R 3是H时,R 4是C 1-6烷基,并且当R 1,R 2和R 4是H时,则R 3是C 1-6烷基,并且当R 1,R 3和 R 4是H,R 2是C 1-6烷基或-CH 2 OH,并且当R 2,R 3和R 4是H时,则R 1是C 1-6烷基; A为1)具有1-3个独立地选自N,S和O的杂原子的9-10元双环杂环,该9-10元双环杂环为未取代的或被R5取代且未被取代或被R6取代且未被取代或被NH2取代 或2)未被取代或被R 5取代的未被取代或被R 6取代且未被取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 且B为1)具有1或2个独立地选自N,S或O的杂原子的5-或6-元单环杂环,其未被取代或在碳或氮原子上被R7取代,未被取代或在碳或氮上被取代 原子与R8取代,并且未被取代或在碳或氮原子上被R9取代,或2)具有1,2或3个氮原子的8-或9-元稠合双环杂环,其未被取代或在碳或氮原子上被 R7,并且未被取代或在碳或氮原子上被R8取代; 和包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防血栓形成的方法。
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9.
公开(公告)号:EP3484464B1
公开(公告)日:2020-10-28
申请号:EP17770855.9
申请日:2017-03-17
Applicant: Merck Sharp & Dohme Corp.
Inventor: ROECKER, Anthony, J. , LAYTON, Mark, E. , GRESHOCK, Thomas, J. , PERO, Joseph, E. , KELLY, Michael, J., III , ZHANG, Ting
IPC: A61K31/426 , A61K31/433 , C07D277/52 , C07D285/08 , A61K31/18 , A61K31/635 , A61K31/427 , C07F7/08
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公开(公告)号:EP3390374B1
公开(公告)日:2020-08-26
申请号:EP16820497.2
申请日:2016-12-14
Applicant: Merck Sharp & Dohme Corp.
Inventor: GRESHOCK, Thomas, J. , MULHEARN, James , ZHENG, Junying , KIM, Ronald, M. , ZHANG, Ting , ROECKER, Anthony, J. , WON, Walter , NANTERMET, Philippe , ANAND, Rajan , ZHOU, Gang , WANG, Deping , GUO, Liangqin
IPC: C07D285/08 , C07D417/12 , C07D277/52 , A61K31/4168 , A61K31/4178 , A61K31/4196 , A61K31/551 , A61P29/00 , A61P11/14
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