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公开(公告)号：US09617224B2
公开(公告)日：2017-04-11
申请号：US14722434
申请日：2015-05-27
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC: C07D249/08 , C07D249/12 , C07D233/64 , C07D235/16 , C07D231/12 , C07D233/68 , C07D263/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D235/08 , C07D263/32 , C07D263/12
CPC classification number: C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
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2.发明授权公开(公告)号：US09493412B2
公开(公告)日：2016-11-15
申请号：US14346751
申请日：2012-09-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jennifer X. Qiao , Heather Finlay , Ji Jiang , John Lloyd , Carol Hui Hu , Zulan Pi , George O. Tora , James Neels , Jon J. Hangeland , Todd J. Friends
IPC: C07D207/38 , C07D409/12 , C07D471/04 , C07D401/12 , C07D413/12 , C07D417/12 , C07D403/12 , C07D401/04 , C07D405/12 , C07F7/08
CPC classification number: C07D207/38 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07F7/0812
Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
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3.发明申请公开(公告)号：US20140213588A1
公开(公告)日：2014-07-31
申请号：US14346747
申请日：2012-09-26
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Lynn Abell , Leonard Adam , Cullen L. Cavallaro , Heather Finlay , Todd J. Friends , Jon J. Hangeland , Ji Jiang , R. Michael Lawrence , Jennifer X. Qiao , Carol Hui Hu , Tammy C. Wang
IPC: C07D417/06 , C07D417/04 , C07D409/04 , C07D413/06 , C07D405/06 , C07D233/61 , C07D401/06 , C07D207/277 , C07D405/04
CPC classification number: C07D207/277 , C07D207/28 , C07D207/38 , C07D233/61 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/06 , C07D417/04 , C07D417/06
Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
Abstract translation: 本发明提供式（I）化合物：如说明书中所定义和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。 本公开还提供了一种通过使用根据式（II）的化合物来治疗与内皮脂肪酶活性相关的疾病或病症的新方法：如说明书中所定义和包含任何化合物的组合物。
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公开(公告)号：US09901572B2
公开(公告)日：2018-02-27
申请号：US15488642
申请日：2017-04-17
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Huji Turdi , Jon J. Hangeland , R. Michael Lawrence , Saleem Ahmad , Wei Meng , Robert Paul Brigance , Pratik Devasthale , Guohua Zhao
IPC: C07D211/90 , C07D401/04 , A61K31/4439 , A61K31/438 , A61K31/675 , A61K31/4418 , C07D413/04 , C07D221/20 , C07D413/14 , A61K31/5377 , C07F9/59 , C07D401/14 , A61K45/06 , C07D401/10 , C07D401/12 , C07D407/14 , C07D413/12 , C07D417/04 , C07D417/14 , C07D211/86 , C07F9/535 , C07F9/40 , C07D405/14
CPC classification number: A61K31/438 , A61K31/4418 , A61K31/4439 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D211/86 , C07D211/90 , C07D221/20 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/4006 , C07F9/5352 , C07F9/59
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
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公开(公告)号：US09079860B2
公开(公告)日：2015-07-14
申请号：US14219311
申请日：2014-03-19
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC: C07D403/04 , C07D235/16 , C07D235/08 , C07D231/12 , C07D233/64 , C07D233/68 , C07D249/08 , C07D263/12 , C07D263/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D263/32
CPC classification number: C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
Abstract translation: 本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法： 其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂的化合物。 本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。
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Patent Agency Ranking
公开(公告)号：US20210161869A1
公开(公告)日：2021-06-03
申请号：US17177327
申请日：2021-02-17
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Huji Turdi , Jon J. Hangeland , R. Michael Lawrence , Saleem Ahmad , Wei Meng , Robert Paul Brigance , Pratik Devasthale , Guohua Zhao
IPC: A61K31/438 , C07D405/14 , C07D221/20 , C07D401/12 , A61K31/4418 , C07D211/90 , C07D417/04 , C07D407/14 , A61K31/675 , C07D401/04 , C07D417/14 , C07D413/12 , A61K45/06 , C07D211/86 , C07F9/40 , C07D413/14 , C07D413/04 , A61K31/4439 , C07F9/535 , C07D401/14 , A61K31/5377 , C07D401/10 , C07F9/59
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
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公开(公告)号：US10966967B2
公开(公告)日：2021-04-06
申请号：US16879810
申请日：2020-05-21
Applicant: Bristol-Myers Squibb Company
Inventor： Huji Turdi , Jon J. Hangeland , R. Michael Lawrence , Saleem Ahmad , Wei Meng , Robert Paul Brigance , Pratik Devasthale , Guohua Zhao
IPC: A61K31/438 , A61K31/675 , C07D211/90 , A61K31/4418 , C07D401/04 , A61K31/4439 , C07D413/04 , C07D221/20 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K45/06 , C07D401/10 , C07D401/12 , C07D407/14 , C07D413/12 , C07D417/04 , C07D417/14 , C07F9/59 , C07F9/40 , C07D211/86 , C07F9/535 , C07D405/14
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
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公开(公告)号：US20150259297A1
公开(公告)日：2015-09-17
申请号：US14722434
申请日：2015-05-27
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC: C07D233/64 , C07D263/32 , C07D401/12 , C07D403/04 , C07D417/04
CPC classification number: C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
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9.发明申请公开(公告)号：US20140206706A1
公开(公告)日：2014-07-24
申请号：US14219311
申请日：2014-03-19
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC: C07D417/04 , C07D263/32 , C07D231/12 , C07D403/04 , C07D235/08 , C07D233/64 , C07D401/12 , C07D249/08
CPC classification number: C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
Abstract translation: 本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法： 其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂的化合物。 本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。
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10.发明申请ARYL DIHYDROPYRIDINONE AND PIPERIDINONE MGAT2 INHIBITORS 有权ARYL DIHYDROPRIDINONE和PIPERIDINONE MGAT2 INHIBITORS公开(公告)号：US20130143843A1
公开(公告)日：2013-06-06
申请号：US13688584
申请日：2012-11-29
Applicant: Bristol-Myers Squibb Company
Inventor： Huji Turdi , Jon J. Hangeland , R. Michael Lawrence , Dong Cheng , Saleem Ahmad , Wei Meng , Robert Paul Brigance , Pratik Devasthale
IPC: A61K31/675 , A61K31/4418 , C07D401/04 , A61K31/4439 , C07D413/04 , A61K45/06 , A61K31/438 , C07D413/14 , A61K31/5377 , C07F9/59 , C07D401/14 , C07D211/90 , C07D221/20
CPC classification number: A61K31/438 , A61K31/4418 , A61K31/4439 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D211/86 , C07D211/90 , C07D221/20 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/4006 , C07F9/5352 , C07F9/59
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
Abstract translation: 本发明提供式（I）化合物或其立体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。 这些化合物是可用作药物的单酰基甘油酰基转移酶2型（MGAT2）抑制剂。
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