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公开(公告)号：US10000484B2
公开(公告)日：2018-06-19
申请号：US15101467
申请日：2014-12-16
申请人： MERCK SHARP & DOHME CORP. , Harry Chobanian , Barbara Pio , Yan Guo , Fa-Xiang Ding , Shuzhi Dong , Shawn P. Walsh , Jinlong Jiang , Dooseop Kim
发明人： Harry Chobanian , Barbara Pio , Yan Guo , Fa-Xiang Ding , Shuzhi Dong , Shawn P. Walsh , Jinlong Jiang , Dooseop Kim
IPC分类号： A61K31/4355 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/55 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/401 , A61K31/4178 , A61K31/424 , A61K31/4422 , A61K31/496 , A61K31/4965 , A61K31/585 , A61K45/06
CPC分类号： C07D471/04 , A61K31/401 , A61K31/4178 , A61K31/424 , A61K31/437 , A61K31/4422 , A61K31/496 , A61K31/4965 , A61K31/4985 , A61K31/519 , A61K31/55 , A61K31/585 , A61K45/06 , C07D487/04 , C07D498/04 , A61K2300/00
摘要： The present invention provides compounds of Formula (I) (Formula (I)) including 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：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：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：US20200375987A1
公开(公告)日：2020-12-03
申请号：US16769670
申请日：2018-12-20
申请人： Alexander PASTERNAK , Shuzhi DONG , Jack D. SCOTT , Haiqun TANG , Zhiqiang ZHAO , Dexi YANG , Li XIAO , Xin GU , Merck Sharp & Dohme Corp.
发明人： Alexander Pasternak , Shuzhi Dong , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Dexi Yang , Li Xiao , Xin Gu , Jinlong Jiang
IPC分类号： A61K31/4985 , C07D487/04 , C07D471/04 , A61K31/4439 , A61K31/519 , A61K31/4188 , C07D513/04 , C07D403/10 , A61K31/4178 , A61K31/407 , A61K31/496 , A61K31/165 , A61K31/7048 , A61K31/546 , A61P31/04
摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein RA, R1, and Z are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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公开(公告)号：US20170275283A1
公开(公告)日：2017-09-28
申请号：US15505277
申请日：2015-10-26
申请人： Alexander PASTERNAK , Fa-Xiang DING , Shuzhi DONG , Jinlong JIANG , Haifeng TANG , Xin GU , Reynalda K. DEJESUS , Jessica FRIE , Qinghong FU , Takao SUZUKI , Zhifa PU , Merck Sharp & Dohme Corp.
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 , C07D498/10 , A61K31/5386 , A61K45/06 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K31/499 , A61K31/55
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：US20160304515A1
公开(公告)日：2016-10-20
申请号：US15101467
申请日：2014-12-16
申请人： Harry CHOBANIAN , Barbara PIO , Yan GUO , Fa-Xiang DING , Shuzhi DONG , Shawn P. WALSH , Jinlong JIANG , Dooseop KIM , MERCK SHARP & DOHME CORP.
发明人： Harry Chobanian , Barbara Pio , Yan Guo , Fa-Xiang Ding , Shuzhi Dong , Shawn P. Walsh , Jinlong Jiang , Dooseop Kim
IPC分类号： C07D471/04 , A61K45/06 , A61K31/55 , C07D487/04 , A61K31/4985 , C07D498/04 , A61K31/519 , A61K31/437
CPC分类号： C07D471/04 , A61K31/401 , A61K31/4178 , A61K31/424 , A61K31/437 , A61K31/4422 , A61K31/496 , A61K31/4965 , A61K31/4985 , A61K31/519 , A61K31/55 , A61K31/585 , A61K45/06 , C07D487/04 , C07D498/04 , A61K2300/00
摘要： The present invention provides compounds of Formula (I) (Formula (I)) including 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：US20160024091A1
公开(公告)日：2016-01-28
申请号：US14774390
申请日：2014-03-10
申请人： Alexander PASTERNAK , Fa-Xiang DING , Shuzhi DONG , Haifeng TANG , Jinlong JIANG , Cangming YANG , Dipshikha BISWAS , MERCK SHARP & DOHME CORP.
发明人： Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Dipshikha Biswas , Haifeng Tang , Jinlong Jiang , Cangming Yang , Xin Gu
IPC分类号： C07D471/10 , A61K31/444 , A61K31/506 , A61K31/435 , A61K31/5386 , A61K31/501 , C07D471/20 , A61K31/4995 , C07D498/20 , A61K45/06 , A61K31/497
CPC分类号： C07D471/10 , A61K31/24 , A61K31/401 , A61K31/403 , A61K31/405 , A61K31/407 , A61K31/41 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/444 , A61K31/472 , A61K31/4965 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5386 , A61K31/55 , A61K31/551 , A61K31/554 , A61K31/585 , A61K31/675 , A61K45/06 , C07D471/20 , 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.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 这些化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭和慢性肾脏疾病以及与过量的盐和水保留有关的病症的医学病症。
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公开(公告)号：US20170275302A1
公开(公告)日：2017-09-28
申请号：US15505266
申请日：2015-10-09
申请人： Alexander PASTERNAK , Barbara PIO , Harry R. CHOBANIAN , Zhi-Cai SHI , Shuzhi DONG , Yan GUO , Shawn P. WALSH , Zhiqiang GUO , Ronald D. FERGUSON , Brian CATO , Merck Sharp & Dohme Corp.
发明人： Alexander Pasternak , Barbara Pio , Harry Chobanian , Zhi-Cai Shi , Shuzhi Dong , Yan Guo , Shawn P. Walsh , Zhiqiang Guo , Ronald D. Ferguson II , Brian Cato
IPC分类号： C07D519/00 , A61K31/4985 , C07D471/10 , A61K31/435 , C07D498/10 , A61K31/519 , A61K31/437 , A61K31/4365 , A61K31/4375 , A61K31/4355 , A61K45/06 , A61K31/5025
CPC分类号： C07D519/00 , A61K31/401 , A61K31/407 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4422 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/55 , A61K45/06 , C07D471/10 , C07D498/10 , 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：US09062070B2
公开(公告)日：2015-06-23
申请号：US14239649
申请日：2012-08-16
申请人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
发明人： Alexander Pasternak , Timothy Blizzard , Harry Chobanian , Reynalda de Jesus , Fa-Xiang Ding , Shuzhi Dong , Candido Gude , Dooseop Kim , Haifeng Tang , Shawn Walsh , Barbara Pio , Jinlong Jiang
IPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
CPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
摘要： The present invention provides compounds of Formula Ia 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 conditions associated with excessive salt and water retention.
摘要翻译： 本发明提供式Ia化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 该化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和水滞留有关的病症的医学病症。
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