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公开(公告)号:US20220235041A1
公开(公告)日:2022-07-28
申请号:US17619338
申请日:2020-06-02
申请人: Brendan M. CROWLEY , Philippe NANTERMET , David OLSEN , Takao SUZUKI , Merck Sharp & Dohme Corp.
IPC分类号: C07D413/14 , C07D413/12 , C07D417/10 , A61K31/422 , A61K31/541 , C07D471/04 , A61K31/437 , C07D413/10 , A61K45/06 , A61P31/06 , A61P31/08
摘要: Disclosed are dihydroisoxazole compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. Also disclosed are compositions which comprise at least one of these dihydroisoxazole compounds, methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of these dihydroisoxazole compounds and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
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公开(公告)号:US20220081403A1
公开(公告)日:2022-03-17
申请号:US17422308
申请日:2019-12-19
申请人: Randall R. MILLER , Joseph A. KOZLOWSKI , Philippe NANTERMET , David B. OLSEN , Jing SU , Uihu YANG , Takao SUZUKI , Brendan M. CROWLEY , Nengxue WANG , Lanying YOU , Merck Sharp & Dohme Corp.
发明人: Randall R. Miller , Joseph A. Kozlowski , Philippe Nantermet , David B. Olsen , Jing Su , Lihu Yang , Takao Suzuki , Brendan Crowley , Negxue Wang , Lanying You
IPC分类号: C07D263/06 , C07D471/04 , C07D413/12 , C07D495/04 , C07F9/653 , C07F9/6553 , A61K31/422 , A61K31/421 , A61K31/437 , A61K31/498 , A61K31/4439 , A61K31/541 , A61P31/06 , A61K45/06
摘要: The present invention discloses oxazolidinone compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A and E, are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
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公开(公告)号:US20170283416A1
公开(公告)日:2017-10-05
申请号:US15505620
申请日:2015-10-26
申请人: Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Takao Suzuki , Joseph P. Vacca , Shouning Xu , Merck Sharp & Dohme Corp.
发明人: Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Takao Suzuki , Joseph P. Vacca , Shouning Xu
IPC分类号: C07D471/10 , A61K31/444 , A61K31/501 , A61K31/435
CPC分类号: C07D471/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/444 , A61K31/501 , A61K31/55 , A61K2300/00
摘要: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号:US09650375B2
公开(公告)日:2017-05-16
申请号:US14769159
申请日:2014-03-10
申请人: Merck Sharp & Dohme Corp. , John J. Acton, III , Rajan Anand , Ashok Arasappan , Qun Dang , Iyassu Sebhat , Zhifa Pu , Takao Suzuki
发明人: John J. Acton, III , Rajan Anand , Ashok Arasappan , Qun Dang , Iyassu Sebhat , Zhifa Pu , Takao Suzuki
IPC分类号: C07D209/04 , C07D471/04 , A61K31/404 , C07D209/12 , C07D209/30 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/04 , C07D413/10 , C07D493/04 , C07D209/18 , C07D519/00 , C07D209/08
CPC分类号: C07D471/04 , A61K31/366 , A61K31/397 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/04 , C07D413/10 , C07D493/04 , C07D519/00 , A61K2300/00
摘要: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
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公开(公告)号:US10208064B2
公开(公告)日:2019-02-19
申请号:US15323989
申请日:2015-07-09
申请人: MERCK SHARP & DOHME CORP. , Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
发明人: Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC分类号: C07D513/10 , C07D519/00 , A61K45/06 , A61K31/435 , A61K31/4745 , A61K31/4375
摘要: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号:US20170197989A1
公开(公告)日:2017-07-13
申请号:US15323989
申请日:2015-07-09
申请人: Alexander PASTERNAK , Ian DAVIES , Fa-Xiang DING , Jinlong JIANG , Shuzhi DONG , Xin GU , Takao SUZUKI , Joseph P. VACCA , Zhifa PU , Shouning XU , Merck Sharp & Dohme Corp.
发明人: Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC分类号: C07D519/00 , A61K31/4745 , A61K31/4375 , A61K31/435
CPC分类号: C07D519/00 , A61K31/435 , A61K31/4375 , A61K31/4745 , A61K45/06
摘要: The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号:US20160324833A1
公开(公告)日:2016-11-10
申请号:US15101481
申请日:2014-12-19
申请人: Shuzhi DONG , Alexander PASTERNAK , Xin GU , Qinghong FU , Jinlong JIANG , Fa-Xiang DING , Haifeng TANG , Reynalda K. DEJESUS , Takao SUZUKI , MERCK SHARP & DOHME CORP.
发明人: Shuzhi Dong , Alexander Pasternak , Xin Gu , Qinghong Fu , Jinlong Jiang , Fa-Xiang Ding , Haifeng Tang , Reynalda K. DeJesus , Takao Suzuki
IPC分类号: A61K31/435 , C07D471/10 , A61K31/444 , A61K31/506 , A61K31/438 , C07D498/10 , A61K31/537 , A61K31/497 , C07D519/00 , A61K31/437 , A61K45/06 , A61K31/501
CPC分类号: A61K31/435 , A61K31/437 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/537 , A61K45/06 , C07D471/10 , C07D498/10 , C07D519/00 , A61K2300/00
摘要: Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.
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公开(公告)号:US20180016263A1
公开(公告)日:2018-01-18
申请号:US15545891
申请日:2016-02-08
申请人: Alexander PASTERNAK , Jessica FRIE , Shuzhi DONG , Takao SUZUKI , Shouning XU , Merck Sharp & Dohme Corp.
发明人: Alexander Pasternak , Jessica Frie , Shuzhi Dong , Takao Suzuki , Shouning Xu
IPC分类号: C07D405/14 , A61K31/496 , C07D413/14
CPC分类号: C07D405/14 , A61K31/496 , A61K2300/00 , A61P9/00 , C07D413/14
摘要: The present invention provides compounds of Formula (I); and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号:US09850245B2
公开(公告)日:2017-12-26
申请号:US15505277
申请日:2015-10-26
申请人: Merck Sharp & Dohme Corp. , Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Haifeng Tang , Xin Gu , Reynalda K. DeJesus , Jessica Frie , Qinghong Fu , Takao Suzuki , Zhifa Pu
发明人: Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Haifeng Tang , Xin Gu , Reynalda K. DeJesus , Jessica Frie , Qinghong Fu , Takao Suzuki , Zhifa Pu
IPC分类号: C07D471/10 , A61K31/499 , C07D498/10 , A61K31/5386 , A61K31/55 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K45/06
CPC分类号: C07D471/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/499 , A61K31/537 , A61K31/5386 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/10 , C07D498/10 , C07D498/20 , A61K2300/00
摘要: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号:US20160002224A1
公开(公告)日:2016-01-07
申请号:US14769159
申请日:2014-03-10
申请人: John J. ACTON, III , Rajan ANAND , Ashok ARASAPPAN , Qun DANG , Iyassu SEBHAT , Zhifa PU , Takao SUZUKI , MERCK SHARP & DOHME CORP.
发明人: John J. Acton, III , Rajan Anand , Ashok Arasappan , Qun Dang , Iyassu Sebhat , Zhifa Pu , Takao Suzuki
IPC分类号: C07D471/04 , A61K31/404 , A61K31/437 , A61K31/4985 , A61K31/4439 , A61K31/366 , A61K31/397 , C07D209/08 , C07D401/10
CPC分类号: C07D471/04 , A61K31/366 , A61K31/397 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/04 , C07D413/10 , C07D493/04 , C07D519/00 , A61K2300/00
摘要: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译: 结构式(I)的新型化合物是AMP-蛋白激酶的活化剂,可用于治疗,预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病,高血糖症,代谢综合征,肥胖症,高胆固醇血症和高血压。
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