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61. 发明授权

US10081617B2 Factor XIa inhibitors 有权
公开(公告)号：US10081617B2
公开(公告)日：2018-09-25
申请号：US15565748
申请日：2016-04-11
申请人： MERCK SHARP & DOHME CORP.
发明人： Eric Mertz , Scott D. Edmondson , Sung-Sau So , Wanying Sun , Weiguo Liu , Santhosh F. Neelamkavil , Ying-Duo Gao , Alan Hruza , Yi Zang , Amjad Ali , Rudrajit Mal , Jiafang He , Rongze Kuang , Heping Wu , Anthony K. Ogawa , Andrew F. Nolting
IPC分类号： C07D401/14 , C07D413/14 , C07D409/14
摘要： The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

62. 发明授权

US09868727B2 Factor XIa inhibitors 有权
公开(公告)号：US09868727B2
公开(公告)日：2018-01-16
申请号：US15329634
申请日：2015-07-23
申请人： Merck Sharp & Dohme Corp.
发明人： Weiguo Liu , Scott D. Edmondson , Zhuyan Guo , Sung-Sau So , Anthony K. Ogawa , Rongze Kuang , Heping Wu , Amjad Ali , Ying-Duo Gao , Yu Jiang , Chunsing Li , Tingting Yu
IPC分类号： C07D409/14 , C07D417/14 , C07D413/14 , C07D401/14 , C07D401/06 , A61K31/4439 , A61K31/444
CPC分类号： C07D409/14 , A61P7/02 , C07D401/06 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

63. 发明授权

US09783530B2 Factor Xla inhibitors 有权
公开(公告)号：US09783530B2
公开(公告)日：2017-10-10
申请号：US15312839
申请日：2015-05-22
申请人： Merck Sharp & Dohme Corp.
发明人： Weiguo Liu , Scott D. Edmondson , Zhuyan Guo , Eric Mertz , Anthony K. Ogawa , Sung-Sau So , Wanying Sun , Linda L. Brockunier , Amjad Ali , Rongze Kuang , Heping Wu
IPC分类号： C07D417/10 , C07D401/10 , C07D213/89 , C07D401/12 , C07D401/14 , C07D413/10
CPC分类号： C07D417/10 , C07D213/89 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10
摘要： The present invention provides a compound of Formula I (The chemical formula should be inserted here.) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

64. 发明申请

US20160304486A1 INDOLINE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：吲哚酚化合物作为醛固酮合成酶抑制剂
公开(公告)号：US20160304486A1
公开(公告)日：2016-10-20
申请号：US15197957
申请日：2016-06-30
申请人： Merck Sharp & Dohme Corp. , ElexoPharm GmbH
发明人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lina Yin , Rolf Hartmann , Qingzhong Hu , Ralf Heim , Christina Zimmer
IPC分类号： C07D401/04 , A61K31/4439 , C07D409/14 , A61K31/4725
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D409/14 , A61K2300/00
摘要： This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
摘要翻译：或其药学上可接受的盐，其中变量在本文中定义。本发明化合物选择性地抑制醛固酮合酶。本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

65. 发明申请

US20140088048A1 DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES 有权
标题翻译：二氮杂环丁烷衍生物
公开(公告)号：US20140088048A1
公开(公告)日：2014-03-27
申请号：US14115139
申请日：2012-04-27
申请人： Merck Sharp & Dohme Corp.
发明人： Amjad Ali , Michael Man-Chu Lo , Lin Yan
IPC分类号： C07C247/06 , C07D231/12 , C07D249/04 , C07D317/72
CPC分类号： C07C247/06 , C07B2200/07 , C07C245/24 , C07C291/08 , C07C2601/14 , C07D231/12 , C07D249/04 , C07D317/72
摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R6 is hydrogen, —OH, —C1-6alkyl, —OC1-6alkyl, aryl, or halogen, or together with R7, forms an oxo group, or together with R7 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms, wherein alkyl and aryl are unsubstituted or independently mono-, di-, or tri-substituted with R14; R7 is hydrogen, C1-6alkyl, —CF3, aryl, —O-aryl, —O—C1-6alkyl, —C(O)OC1-6alkyl, —C(R15R16)OH, a 5-7-membered heteroaryl having 1, 2, 3 or 4 nitrogen atoms, or halogen, or together with R6, forms an oxo group, or together with R6 and the atom to which they are attached, form a 5-7-membered carbocycle ring or a 5-7-membered heterocyclic ring having 1, 2, or 3 heteroatoms wherein alkyl, aryl and heteroaryl are unsubstituted or independently mono-, di- or tri-substituted with R14; R12 is hydrogen, C1-6alkyl, or —(CH2)1-2OH, or together with R13 and the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or independently mono-, di- or tri-substituted with halogen or —C1-6alkyl; R13 is —C1-6alkyl or —(CH2)1-2OH, or together with R12 and the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or independently mono-, di- or tri-substituted with halogen or —C1-6alkyl.
摘要翻译：具有结构或其药学上可接受的盐的化合物，其中R 6是氢，-OH，-C 1-6烷基，-OC 1-6烷基，芳基或卤素，或与R 7一起形成氧代基，或与R 7和它们连接的原子形成5-7元碳环或具有1,2或3个杂原子的5-7元杂环，其中烷基和芳基是未取代的或独立地是单 - ，二 - 或用R14三取代; R 7是氢，C 1-6烷基，-CF 3，芳基，-O-芳基，-O-C 1-6烷基，-C（O）OC 1-6烷基，-C（R 15 R 16）OH，5- ，2,3或4个氮原子，或卤素，或与R6一起形成氧代基团，或与R6及其连接的原子一起形成5-7元碳环或5-7元碳环，其中烷基，芳基和杂芳基是未取代的或独立地被R 14取代或被二取代或三取代的杂环基; R 12是氢，C 1-6烷基或 - （CH 2）1-2 OH，或者与R 13和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧的4-至7-元杂环原子，其中所述环是未取代的或独立地被卤素或-C 1-6烷基单，二或三取代; R 13是-C 1-6烷基或 - （CH 2）1-2 OH，或与R 12和它们所连接的氮原子一起形成含有一个氮原子和0或1个氧原子的4-至7-元杂环，其中所述环是未取代的或独立地被卤素或-C 1-6烷基单，二或三取代。

66. 发明申请

US20220235033A1 FACTOR XI ACTIVATION INHIBITORS 有权
公开(公告)号：US20220235033A1
公开(公告)日：2022-07-28
申请号：US17613988
申请日：2020-05-26
申请人： Merck Sharp & Dohme Corp.
发明人： Jacqueline D. Hicks , John S. Debenham , Amjad Ali , Lan Wei , Tianying Jian , Dexi Yang , Anthony K. Ogawa , Wenlang Fu , Matthew Lombardo , Rongze Kuang , Meng Yang , Sung-Sau So , Kenneth Ellsworth , Peter Nizner , Daniel A. Tatosian , Robert R. Wilkening , Jun Wang
IPC分类号： C07D401/14 , C07D405/14 , C07D471/04 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

67. 发明授权

US11312719B2 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use 有权
公开(公告)号：US11312719B2
公开(公告)日：2022-04-26
申请号：US16695367
申请日：2019-11-26
申请人： Merck Sharp & Dohme Corp.
发明人： Matthew A. Larsen , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Andrew J. Hoover , Ping Liu , Kun Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang , Yonglian Zhang
IPC分类号： C07D487/04 , C07K16/28
摘要： In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

68. 发明申请

US20210355131A1 Factor XIa Inhibitors 有权
公开(公告)号：US20210355131A1
公开(公告)日：2021-11-18
申请号：US17286525
申请日：2019-10-21
申请人： Merck Sharp & Dohme Corp.
发明人： Amjad Ali , John S. Debenham , Cheng Zhu
IPC分类号： C07D487/08
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

69. 发明授权

US10093683B2 Factor XIa inhibitors 有权
公开(公告)号：US10093683B2
公开(公告)日：2018-10-09
申请号：US15305421
申请日：2015-04-21
申请人： Merck Sharp & Dohme Corp.
发明人： Yeon-Hee Lim , Zhuyan Guo , Amjad Ali , Scott D. Edmondson , Weiguo Liu , Gioconda V. Gallo-Etienne , Heping Wu , Ying-Duo Gao , Andrew W. Stamford , Younong Yu , Nancy J. Kevin , Rajan Anand , Deyou Sha , Santhosh F. Neelamkavil , Zahid Hussain , Puneet Kumar , Remond Moningka , Joseph L. Duffy , Jiayi Xu , Yu Jiang , Anjan Chakrabarti , Hiroki Sone
IPC分类号： C07D498/20 , C07F9/6561 , C07D487/10 , C07D498/10 , C07D471/10
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

70. 发明授权

US10011585B2 Factor XIa inhibitors 有权
公开(公告)号：US10011585B2
公开(公告)日：2018-07-03
申请号：US15329635
申请日：2015-07-23
申请人： Merck Sharp & Dohme Corp.
发明人： Weiguo Liu , Scott D Edmondson , Zhuyan Guo , Alan Hruza , Sung-Sau So , Wanying Sun , Amjad Ali , Rongze Kuang , Ying-Duo Gao , Anthony K Ogawa
IPC分类号： C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

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