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公开(公告)号：US20180282320A1
公开(公告)日：2018-10-04
申请号：US15756378
申请日：2016-08-30
发明人： Scott A. Shaw , Joanne M. Smallheer
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) 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
发明人： 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分类号： C07D233/64 , C07D263/32 , C07D401/12 , C07D403/04 , C07D417/04
CPC分类号： 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
摘要： 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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公开(公告)号：US20150112058A1
公开(公告)日：2015-04-23
申请号：US14578846
申请日：2014-12-22
发明人： James R. Corte , Tianan Fang , Carl P. Decicco , Donald J.P. Pinto , Karen A. Rossi , Zilun Hu , Yoon Jeon , Mimi L. Quan , Joanne M. Smallheer , Yufeng Wang , Wu Yang
IPC分类号： C07D498/06 , C07D487/16 , C07D487/06
CPC分类号： C07D487/04 , C07D471/14 , C07D471/18 , C07D487/06 , C07D487/08 , C07D487/14 , C07D487/16 , C07D487/18 , C07D498/04 , C07D498/06 , C07D498/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt 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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4.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
发明人： 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分类号： C07D417/04 , C07D263/32 , C07D231/12 , C07D403/04 , C07D235/08 , C07D233/64 , C07D401/12 , C07D249/08
CPC分类号： 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
摘要： 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.
摘要翻译： 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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公开(公告)号：US11008317B2
公开(公告)日：2021-05-18
申请号：US16083958
申请日：2017-03-16
发明人： Ellen K. Kick , Joanne M. Smallheer , Scott A. Shaw , Benjamin P. Vokits , Andrew K. Dilger , Charles G. Clark , Meriah Neissel Valente , Sutjano Jusuf , Nicholas R. Wurtz
IPC分类号： C07D471/04 , C07D519/00
摘要： The present invention provides compounds of Formula (I); wherein the substituents are each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
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公开(公告)号：US10407422B2
公开(公告)日：2019-09-10
申请号：US15756367
申请日：2016-08-30
IPC分类号： C07D471/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
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公开(公告)号：US10214527B2
公开(公告)日：2019-02-26
申请号：US15756378
申请日：2016-08-30
发明人： Scott A. Shaw , Joanne M. Smallheer
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04
摘要： The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
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公开(公告)号：US20230250063A1
公开(公告)日：2023-08-10
申请号：US18004722
申请日：2021-07-08
发明人： James A. Johnson , Zulan Pi , Nicholas R. Wurtz , Joanne M. Smallheer , Meriah Neissel Valente , Ellen K. Kick , Charles G. Clark , Pravin Sudhaka Shirude , Balaji Kumar Seshadri , Amit Kumar Chattopadhyay
IPC分类号： C07D231/50 , C07D405/14 , C07D401/14 , C07D451/02 , C07D413/14 , C07D401/04
CPC分类号： C07D231/50 , C07D405/14 , C07D401/14 , C07D451/02 , C07D413/14 , C07D401/04
摘要： The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
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公开(公告)号：US20200291015A1
公开(公告)日：2020-09-17
申请号：US16083951
申请日：2017-03-10
发明人： Joanne M. Smallheer , Carol Hui HU , Meriah Neissel Valente , Scott A. Shaw , Benjamin P. Vokits , Oz Scott Halpern
IPC分类号： C07D471/04
摘要： The present invention provides compounds of Formula (I). wherein A and Z are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
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公开(公告)号：US10577383B2
公开(公告)日：2020-03-03
申请号：US16099010
申请日：2017-06-26
发明人： Joanne M. Smallheer , Ellen K. Kick , Meriah Neissel Valente , Carol Hui Hu , Oz Scott Halpern , Sutjano Jusuf
IPC分类号： C07D519/00 , A61P9/10
摘要： The present invention provides compounds of Formula (I): wherein the substituents are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, and may be useful for for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
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