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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：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：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：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：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：US20160002259A1
公开(公告)日：2016-01-07
申请号：US14768245
申请日：2014-02-12
申请人： Alexander PASTERNAK , Reynalda Keh DE JESUS , Fa-xiang DING , Shuzhi DONG , Jessica FRIE , Xin GU , Jinlong JIANG , Aurash SHAHRIPOUR , Barbara PIO , Haifeng TANG , Shawn WALSH , MERCK SHARP & DOHME CORP.
发明人： Alexander Pasternak , Reynalda Keh DeJesus , Fa-Xiang Ding , Shuzhi Dong , Jessica L. Frie , Xin Gu , Jinlong Jiang , Aurash Shahripour , Barbara Pio , Haifeng Tang , Shawn Walsh
IPC分类号： C07D498/04 , A61K45/06 , A61K31/4985 , A61K31/5383 , C07D487/04
CPC分类号： C07D498/04 , A61K31/401 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/4985 , A61K31/5383 , A61K31/55 , A61K31/675 , A61K45/06 , C07D487/04 , C07D519/00 , 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, kidney disease, edema, 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。 该化合物可以用作利尿剂和/或利尿钠剂，并用于治疗和预防包括心血管疾病如高血压，心力衰竭，肾脏疾病，水肿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：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：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：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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