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1.发明申请MACROCYCLES WITH HETROCYCLIC P2' GROUPS AS FACTOR XIA INHIBITORS 审中-公开作为因子XIA抑制剂的HETROCYCLIC P2'组合物公开(公告)号：US20170002006A1
公开(公告)日：2017-01-05
申请号：US15115327
申请日：2015-01-30
发明人： James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Andrew K. Dilger , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J.P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07D471/18 , C07D487/08
CPC分类号： C07D471/08 , C07D403/06 , C07D403/14 , C07D471/18 , C07D487/08
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 methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译： 本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性因子XIa抑制剂或FXIa和血浆激肽释放酶的双重抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
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公开(公告)号：US20200055854A1
公开(公告)日：2020-02-20
申请号：US16451873
申请日：2019-06-25
发明人： Andrew K. Dilger , James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J.P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07D471/18 , C07F7/08 , C07D519/00 , C07D471/08 , C07D487/08
摘要： The present invention provides compounds of Formula (1): 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 methods of treating thromboembolic and/or inflammatory disorders using the same.
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公开(公告)号：US10336754B2
公开(公告)日：2019-07-02
申请号：US15903671
申请日：2018-02-23
发明人： Andrew K. Dilger , James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J. P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07F7/08 , C07D519/00 , C07D471/18 , C07D487/08 , C07D471/08
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 methods of treating thromboembolic and/or inflammatory disorders using the same.
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公开(公告)号：US20170342071A1
公开(公告)日：2017-11-30
申请号：US15680729
申请日：2017-08-18
发明人： Andrew K. Dilger , James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J.P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07D471/18 , C07D487/08
CPC分类号： C07D471/18 , C07D487/08
摘要： The present invention provides compounds of Formula (Ia): 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 methods of treating thromboembolic and/or inflammatory disorders using the same.
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公开(公告)号：US20220356179A1
公开(公告)日：2022-11-10
申请号：US17349980
申请日：2021-06-17
发明人： Peter W. Glunz , Vladimir Ladziata , Indawati De Lucca , George O. Tora , Tarun Kumar Maishal , Raghuram Tangirala , Kamalraj Thiyagarajan
IPC分类号： C07D417/12 , C07D401/14 , C07D403/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D495/04 , C07D519/00
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 ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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公开(公告)号：US20210147406A1
公开(公告)日：2021-05-20
申请号：US16629717
申请日：2018-07-11
发明人： Peter W. Glunz , Vladimir Ladziata , Indawati De Lucca , George O. Tora , Tarun Kumar Maishal , Raghuram Tangirala , Kamalraj Thiyagarajan
IPC分类号： C07D417/12 , C07D471/04 , C07D519/00 , C07D495/04 , C07D491/052 , C07D403/12 , C07D401/14 , C07D417/14
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 ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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公开(公告)号：US20200131200A1
公开(公告)日：2020-04-30
申请号：US16739363
申请日：2020-01-10
发明人： Leon M. Smith, II , Vladimir Ladziata , Indawati De Lucca , Donald J.P. Pinto , Michael J. Orwat , Andrew K. Dilger , Kumar Balashnmuga Pabbisetty , Wu Yang , Scott A. Shaw , Peter W. Glunz , Manoranjan Panda
IPC分类号： C07D513/04 , A61P9/10 , A61P15/10 , C07D213/64 , C07D231/12 , C07D401/14 , C07D231/54 , C07D401/12 , C07D413/12 , C07D471/12 , C07D471/04 , C07D231/18
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 ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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公开(公告)号：US20170096429A1
公开(公告)日：2017-04-06
申请号：US15115314
申请日：2015-01-30
发明人： James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Andrew K. Dilger , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J.P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07D471/08 , C07D403/14 , C07D471/18 , C07D487/08
CPC分类号： C07D471/08 , C07D403/06 , C07D403/14 , C07D471/18 , C07D487/08
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 methods of treating thromboembolic and/or inflammatory disorders using the same.
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公开(公告)号：US20170057961A1
公开(公告)日：2017-03-02
申请号：US15115319
申请日：2015-01-30
发明人： Andrew K. Dilger , James R. Corte , Indawati De Lucca , Tianan Fang , Wu Yang , Yufeng Wang , Kumar Balashanmuga Pabbisetty , William R. Ewing , Yeheng Zhu , Ruth R. Wexler , Donald J.P. Pinto , Michael J. Orwat , Leon M. Smith, II
IPC分类号： C07D471/18 , C07D487/08
CPC分类号： C07D471/18 , C07D487/08
摘要： The present invention provides compounds of Formula (Ia): 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 methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译： 本发明提供式（Ia）化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性因子XIa抑制剂或FXIa和血浆激肽释放酶的双重抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
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公开(公告)号：US11673886B2
公开(公告)日：2023-06-13
申请号：US17349980
申请日：2021-06-17
发明人： Peter W. Glunz , Vladimir Ladziata , Indawati De Lucca , George O. Tora , Tarun Kumar Maishal , Raghuram Tangirala , Kamalraj Thiyagarajan
IPC分类号： C07D417/12 , C07D401/14 , C07D403/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D519/00 , C07D491/052
CPC分类号： C07D417/12 , C07D401/14 , C07D403/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D495/04 , C07D519/00
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 ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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