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公开(公告)号：EP4422746A1
公开(公告)日：2024-09-04
申请号：EP22830974.6
申请日：2022-10-28
发明人： SU, Shun , BILDER, Donna M. , CLARKE, Adam James , FINLAY, Heather , FRIENDS, Todd J. , MATHUR, Arvind , MYERS, Michael C. , LAWRENCE, R. Michael , LI, Jianqing , PINTO, Donald J.P. , ORWAT, Michael J. , PABBISETTY, Kumar Balashanmuga , SHAW, Scott A. , SMITH II, Leon M. , TORA, George O. , VOKITS, Benjamin P. , O'MALLEY, Daniel , WURTZ, Nicholas R. , BHOGADI, Vikram , PASUNOORI, Laxman , SRINIVAS, Pitani Veera Venkata , KUMAR, Sreekantha Ratna , POTTURI, Hima Kiran , HEGDE, Subramanya
IPC分类号： A61P1/16 , A61P13/12 , C07C237/38 , C07C255/60 , C07C311/46 , C07D207/09 , C07D213/56 , C07D249/04 , C07D261/20 , C07D275/06 , C07D277/28 , C07D285/12 , C07D307/87 , C07D309/08 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04 , C07D493/04 , C07D498/04 , A61K31/4409
CPC分类号： C07D471/04 , C07D498/04 , C07D261/20 , C07D309/08 , C07D417/12 , C07D275/06 , C07D285/12 , C07D413/12 , C07C311/46 , C07C255/60 , C07C237/38 , C07D307/87 , C07D207/09 , C07D413/06 , C07D493/04 , C07D249/04 , C07D277/28 , C07D213/56 , A61P1/16 , A61P13/12
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公开(公告)号：EP4286372A3
公开(公告)日：2024-02-21
申请号：EP23185426.6
申请日：2015-07-29
发明人： DILGER, Andrew K. , CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , PABBISETTY, Kumar Balashanmuga , EWING, Willam R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH II, Leon M.
IPC分类号： C07D471/18 , A61K31/4162 , A61P7/02
摘要： The present invention provides a compound which is (9 R ,13 S )-13-{4-[5-chloro-2-(4-chloro-1 H -1,2,3-triazol-1-yl)phenyl]-6-oxo-1,6-dihydropyrimidin-1-yl}-3-(difluoromethyl)-9-methyl-3,4,7,15-tetraazatricyclo[12.3.1.0 2,6 ]octadeca-1(18),2(6),4,14,16-pentaen-8-one trifluoroacetate, or a stereoisomer or tautomer thereof. This invention also relates to pharmaceutical compositions comprising this compound and their use in the treatment of thromboembolic disorders.
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公开(公告)号：EP3988549A1
公开(公告)日：2022-04-27
申请号：EP21192647.2
申请日：2015-01-30
发明人： CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , DILGER, Andrew K. , PABBISETTY, Kumar Balashanmuga , EWING, William R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH, Leon M. II
IPC分类号： C07D471/08 , C07D487/08 , A61K31/529 , A61P7/00
摘要： The present invention provides compounds of Formula (I):
or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and these compounds for use in therapy.-
公开(公告)号：EP3828186A3
公开(公告)日：2021-07-28
申请号：EP20197284.1
申请日：2015-07-29
发明人： DILGER, Andrew K. , CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , PABBISETTY, Kumar Balashanmuga , EWING, William R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH II, Leon M.
IPC分类号： C07D471/18 , A61K31/4162 , A61P7/02 , C07D213/61 , C07D239/36 , C07D403/10 , C07D239/34
摘要： The present invention provides compounds of the following formulae:
or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and synthetic intermediates for preparing the same.-
公开(公告)号：EP4448484A1
公开(公告)日：2024-10-23
申请号：EP22859562.5
申请日：2022-12-14
IPC分类号： C07C233/00 , C07D231/12 , C07D261/08 , C07D261/20 , C07D275/02 , C07D309/08 , C07D498/04 , A61K31/167 , A61P9/00
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公开(公告)号：EP4286372A2
公开(公告)日：2023-12-06
申请号：EP23185426.6
申请日：2015-07-29
发明人： DILGER, Andrew K. , CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , PABBISETTY, Kumar Balashanmuga , EWING, Willam R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH II, Leon M.
IPC分类号： C07D239/34
摘要： The present invention provides a compound which is (9 R ,13 S )-13-{4-[5-chloro-2-(4-chloro-1 H -1,2,3-triazol-1-yl)phenyl]-6-oxo-1,6-dihydropyrimidin-1-yl}-3-(difluoromethyl)-9-methyl-3,4,7,15-tetraazatricyclo[12.3.1.0 2,6 ]octadeca-1(18),2(6),4,14,16-pentaen-8-one trifluoroacetate, or a stereoisomer or tautomer thereof. This invention also relates to pharmaceutical compositions comprising this compound and their use in the treatment of thromboembolic disorders.
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公开(公告)号：EP3293186B1
公开(公告)日：2020-09-23
申请号：EP17189935.4
申请日：2015-07-29
发明人： DILGER, Andrew K. , CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , PABBISETTY, Kumar Balashanmuga , EWING, William R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH II, Leon M.
IPC分类号： C07D471/18 , A61K31/4162 , A61P7/02
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公开(公告)号：EP2766345A1
公开(公告)日：2014-08-20
申请号：EP12778912.1
申请日：2012-10-12
发明人： ORWAT, Michael J. , PINTO, Donald J.P. , SMITH II, Leon M. , SRIVASTAVA, Shefali , CORTE, James R.
IPC分类号： C07D217/26 , C07D401/10 , C07D401/14 , C07D403/14 , C07D471/04 , C07D487/04 , A61K31/4725 , A61P7/02 , A61K31/437 , A61K31/4375
CPC分类号： C07D401/10 , C07D217/26 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of Formula (IX): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
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公开(公告)号：EP4423094A1
公开(公告)日：2024-09-04
申请号：EP22813058.9
申请日：2022-10-28
发明人： PINTO, Donald J.P. , SU, Shun , MATHUR, Arvind , MYERS, Michael C. , LI, Jianqing , PABBISETTY, Kumar Balashanmuga , SHAW, Scott A.
IPC分类号： C07D498/04 , C07C235/40 , C07C275/34 , A61K31/42 , A61P9/10
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公开(公告)号：EP3828186A2
公开(公告)日：2021-06-02
申请号：EP20197284.1
申请日：2015-07-29
发明人： DILGER, Andrew K. , CORTE, James R. , DE LUCCA, Indawati , FANG, Tianan , YANG, Wu , WANG, Yufeng , PABBISETTY, Kumar Balashanmuga , EWING, William R. , ZHU, Yeheng , WEXLER, Ruth R. , PINTO, Donald J.P. , ORWAT, Michael J. , SMITH II, Leon M.
IPC分类号： C07D471/18 , A61K31/4162 , A61P7/02 , C07D213/61 , C07D239/36 , C07D403/10 , C07D239/34
摘要： The present invention provides compounds of the following formulae:
or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and synthetic intermediates for preparing the same.
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