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1. 发明公开

EP2934536A4 FACTOR IXa INHIBITORS 有权转让
公开(公告)号：EP2934536A4
公开(公告)日：2016-09-21
申请号：EP13863880
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： HIRABAYASHI TOMOKAZU , KATSUNO MIKA , SMITH CAMERON JAMES , SHERER EDWARD , CAMPEAU LOUIS-CHARLES , BALKOVEC JAMES , GREENLEE WILLIAM JOHN , LI DERUN , GUO LIANGQIN , CHAN TIN YAN , CHEN YI-HENG , CHEN YILI , CHACKALAMANNIL SAMUEL , TAN JOHN QIANG
IPC分类号： C07D413/12 , A61K31/5377
CPC分类号： C07D513/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, 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.

2. 发明公开

EP3131897A4 FACTOR IXA INHIBITORS 有权转让
公开(公告)号：EP3131897A4
公开(公告)日：2018-01-03
申请号：EP15780578
申请日：2015-04-10
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： SAKURADA ISAO , HIRABAYASHI TOMOKAZU , MAEDA YOSHITAKA , NAGASUE HIROSHI , MIZUNO TAKASHI , XU JIAYI , ZHANG TING , SMITH CAMERON , PARKER DANN
IPC分类号： C07D413/14 , C07D207/02 , C07D261/20
CPC分类号： 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
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.

3. 发明公开

EP3131896A4 FACTOR IXA INHIBITORS 有权转让
公开(公告)号：EP3131896A4
公开(公告)日：2018-01-10
申请号：EP15779184
申请日：2015-04-10
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： SAKURADA ISAO , HIRABAYASHI TOMOKAZU , MAEDA YOSHITAKA , NAGASUE HIROSHI , MIZUNO TAKASHI , XU JIAYI , ZHANG TING , SMITH CAMERON , PARKER DANN
IPC分类号： C07D413/14 , A61K31/439 , C07D207/02 , C07D261/20
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.

4. 发明公开

EP2934538A4 FACTOR IXA INHIBITORS 有权转让
标题翻译： FAKTOR-IXA-缝边
公开(公告)号：EP2934538A4
公开(公告)日：2016-06-08
申请号：EP13873301
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： 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分类号： C07D413/12 , A61K31/5377 , A61P7/02
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.
摘要翻译：本发明提供式（I）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，R 4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为H时，R 3为C 1-6烷基，当R 1，R 3和R 4为H ，R2是C1-6烷基或-CH2OH，当R2，R3和R4是H时，R1是C1-6烷基; A是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，其中9-10元双环杂环是未取代的或被R 5取代且未被取代或被R 6取代且未取代或被NH 2取代，或2）未被取代或被未取代或被R 6取代的R 5取代的未取代或被-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，其未取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代具有R 8的未取代或取代的碳原子或氮原子上的取代基，或2）具有1,2或3个氮原子的8或9元稠合双环杂环，其未被取代或在碳原子或氮原子上被取代， R7，并且在碳或氮原子上未被取代或取代为R8; 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。

5. 发明公开

EP2934537A4 FACTOR IXA INHIBITORS 有权转让
标题翻译：因子IXA-缝边
公开(公告)号：EP2934537A4
公开(公告)日：2016-05-25
申请号：EP13866418
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： 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分类号： A61K31/5377 , C07D413/12 , C07D413/14 , C07D513/04
CPC分类号： C07D413/14 , C07D413/12 , C07D513/04
摘要： 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.
摘要翻译：本发明提供式（I）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，中，R 2和R 4为H，R 3为C 1-6烷基，当R 1，R 3和R 4为H时，R 2为C 1-6烷基，当R 2，R 3和R 4为H时，R为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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