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![CRYSTALLINE FORMS OF (9R, 135S)-13- {4-[5-CHLORO-2-(4-CHLORO-1H,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](data:image/svg+xml,%3Csvg xmlns='http://www.w3.org/2000/svg' width='200' height='200' viewBox='0 0 200 200'%3E%3Crect width='100%25' height='100%25' fill='%23eee'%3E%3C/rect%3E%3Ctext x='50%25' y='50%25' dominant-baseline='middle' text-anchor='middle' fill='%23333333' font-family='Helvetica' font-size='20' font-weight='bold'%3ENo Pic%3C/text%3E%3C/svg%3E)
公开(公告)号：US20230151010A1
公开(公告)日：2023-05-18
申请号：US17995848
申请日：2021-04-09
Applicant: Bristol-Myers Squibb Company , Janssen Pharmaceutica NV
Inventor： Andrew K. Dilger , Michael A. Galella , Daniel Smith , Theresa M. Ziemba , David Lüdeker , Christos XIOURAS , Dipali AHUJA , Dirk Angelina J. CLEEREN
IPC: C07D471/18
CPC classification number: C07D471/18 , C07B2200/13
Abstract: Disclosed are crystalline forms of Compound (I). Compound (I) is useful as an anti-thromboembolic agent in the treatment of cardiovascular diseases.
![CRYSTALLINE FORMS OF (9R, 135S)-13- {4-[5-CHLORO-2-(4-CHLORO-1H,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](/docs/US/2023-05-18/US20230151010A1/abs.jpg.600x600.jpg)
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公开(公告)号：US10676477B2
公开(公告)日：2020-06-09
申请号：US15747867
申请日：2016-07-28
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Yeheng Zhu , Andrew K. Dilger , William R. Ewing , Michael J. Orwat , Donald J. P. Pinto
IPC: C07D487/04 , C07D403/14 , C07D401/14 , C07D403/12 , A61P7/02
Abstract: 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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3.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
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： 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: C07D471/18 , C07D487/08
CPC classification number: C07D471/08 , C07D403/06 , C07D403/14 , C07D471/18 , C07D487/08
Abstract: 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.
Abstract translation: 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：US20250049765A1
公开(公告)日：2025-02-13
申请号：US18718484
申请日：2022-12-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Andrew K. Dilger , Leon M. Smith ll , Michael J. Orwat , Donald J.P. Pinto
IPC: A61K31/423 , A61K31/27 , C07C237/24 , C07D261/04 , C07D261/20
Abstract: The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
![BICYCLO [3.2.0] HEPTANE BIS(AMIDE) RXFP1 AGONISTS](/docs/US/2025-02-13/US20250049765A1/abs.jpg.600x600.jpg)
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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
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： 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: C07D513/04 , A61P9/10 , A61P15/10 , C07D213/64 , C07D231/12 , C07D401/14 , C07D231/54 , C07D401/12 , C07D413/12 , C07D471/12 , C07D471/04 , C07D231/18
Abstract: 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：US20180162821A1
公开(公告)日：2018-06-14
申请号：US15837034
申请日：2017-12-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： James R. Corte , Andrew K. Dilger , William R. Ewing , Donald J.P. Pinto , Wu Yang
IPC: C07D225/06 , C07D403/04 , C07D401/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07D245/06 , A61P7/02
CPC classification number: C07D225/06 , A61P7/02 , C07D245/06 , C07D401/04 , C07D403/04 , C07D471/04 , C07D471/08 , C07D487/08
Abstract: The present invention provides compounds of Formula (I): P-Ma (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：US20170096429A1
公开(公告)日：2017-04-06
申请号：US15115314
申请日：2015-01-30
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： 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: C07D471/08 , C07D403/14 , C07D471/18 , C07D487/08
CPC classification number: C07D471/08 , C07D403/06 , C07D403/14 , C07D471/18 , C07D487/08
Abstract: 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
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： 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: C07D471/18 , C07D487/08
CPC classification number: C07D471/18 , C07D487/08
Abstract: 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.
Abstract translation: 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：US10287288B2
公开(公告)日：2019-05-14
申请号：US15747818
申请日：2016-07-28
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Kumar Balashanmuga Pabbisetty , James R. Corte , Andrew K. Dilger , William R. Ewing , Yeheng Zhu
IPC: A61K31/16 , C07C211/33 , C07D471/04 , C07D403/12 , C07D403/14 , C07D471/06 , C07D471/20 , C07D491/20 , A61P7/02
Abstract: 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：US10273236B2
公开(公告)日：2019-04-30
申请号：US15946837
申请日：2018-04-06
Applicant: Bristol-Myers Squibb Company
Inventor： 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: C07D471/18 , C07D487/08
Abstract: 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.
