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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
Applicant: Shuzhi DONG , Alexander PASTERNAK , Xin GU , Qinghong FU , Jinlong JIANG , Fa-Xiang DING , Haifeng TANG , Reynalda K. DEJESUS , Takao SUZUKI , MERCK SHARP & DOHME CORP.
Inventor： Shuzhi Dong , Alexander Pasternak , Xin Gu , Qinghong Fu , Jinlong Jiang , Fa-Xiang Ding , Haifeng Tang , Reynalda K. DeJesus , Takao Suzuki
IPC: 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 classification number: 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
Abstract: 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：US20170275283A1
公开(公告)日：2017-09-28
申请号：US15505277
申请日：2015-10-26
Applicant: 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.
Inventor： 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: C07D471/10 , C07D498/10 , A61K31/5386 , A61K45/06 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K31/499 , A61K31/55
CPC classification number: 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
Abstract: 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
Applicant: 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
Inventor： 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: C07D471/10 , A61K31/499 , C07D498/10 , A61K31/5386 , A61K31/55 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K45/06
CPC classification number: 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
Abstract: 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：US10513518B2
公开(公告)日：2019-12-24
申请号：US15544295
申请日：2016-01-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Reynalda K. deJesus , Qinghong Fu , Jinlong Jiang , Haifeng Tang
IPC: A61K31/435 , A61K31/55 , A61K31/5386 , A61K31/424 , C07D471/10 , C07D487/10 , C07D498/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/439 , A61K31/4422 , A61K31/4523 , A61K31/5377 , C07D471/20 , A61K31/444 , A61K31/46 , A61K45/06 , C07D451/00
Abstract: The present invention provides compounds of Formula I (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：US20180009807A1
公开(公告)日：2018-01-11
申请号：US15544295
申请日：2016-01-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Reynalda K. deJesus , Qinghong Fu , Jinlong Jiang , Haifeng Tang
IPC: C07D471/10 , C07D487/10 , C07D451/00 , A61K31/55 , A61K31/435 , A61K31/5386 , A61K31/46 , A61K31/444 , C07D498/10 , A61K45/06
Abstract: The present invention provides compounds of Formula I (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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Patent Agency Ranking
公开(公告)号：US20170275298A1
公开(公告)日：2017-09-28
申请号：US15505254
申请日：2015-10-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Shuzhi Dong , Xin Gu , Jinlong Jiang , Zhi-Cai Shi , Shawn P. Walsh , Zhicai Wu , Yang Yu , Ronald Ferguson, II , Zhiqiang Guo , Jessica Frie , Takao Suzuki , Timothy A. Blizzard , Qinghong Fu , Kelsey F. Vangelder
IPC: C07D498/10 , A61K31/435 , A61K31/501 , A61K31/506 , A61K31/444 , A61K31/5386 , A61K31/497 , A61K31/41 , A61K31/4184 , A61K31/4178 , A61K31/4422 , A61K31/55 , A61K31/401 , A61K31/675 , A61K31/551 , A61K31/4965 , A61K31/585 , C07D471/10
CPC classification number: C07D498/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/444 , A61K31/4965 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5386 , A61K31/55 , A61K31/551 , A61K31/585 , A61K31/675 , A61P3/14 , A61P7/10 , A61P9/12 , C07D471/10 , C07D497/10 , A61K2300/00
Abstract: 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：US09951052B2
公开(公告)日：2018-04-24
申请号：US15032174
申请日：2014-10-27
Applicant: Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Haifeng Tang , Jessica Frie , Ronald Dale Ferguson , Zhiqiang Guo , Zhi-Cai Shi , Brian Cato , Qinghong Fu
IPC: C07D405/06 , A61K31/4525 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K45/06
CPC classification number: C07D405/06 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
Abstract: 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：US09839629B2
公开(公告)日：2017-12-12
申请号：US15101481
申请日：2014-12-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： Shuzhi Dong , Alexander Pasternak , Xin Gu , Qinghong Fu , Jinlong Jiang , Fa-Xiang Ding , Haifeng Tang , Reynalda K. DeJesus , Takao Suzuki
IPC: C07D471/10 , C07D498/10 , A61K31/4545 , A61K31/537 , A61K31/4745 , A61K31/435 , A61K31/497 , A61K31/501 , A61K31/506 , C07D519/00 , A61K31/437 , A61K31/438 , A61K31/444 , A61K45/06
CPC classification number: 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
Abstract: 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：US20160257670A1
公开(公告)日：2016-09-08
申请号：US15032174
申请日：2014-10-27
Applicant: Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Haifeng Tang , Jessica Frie , Ronald Dale Ferguson , Zhiqiang Guo , Zhi-Cai Shi , Brian Cato , Qinghong Fu
IPC: C07D405/06 , A61K31/427 , C07D471/04 , C07D513/04 , C07D417/14 , A61K45/06 , A61K31/4525 , A61K31/4545 , C07D405/14 , A61K31/433 , A61K31/4439 , A61K31/454 , C07D413/14
CPC classification number: C07D405/06 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
Abstract: 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：US20140235628A1
公开(公告)日：2014-08-21
申请号：US14344681
申请日：2012-09-10
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Shawn Walsh , Alexander Pasternak , Brian Cato , Paul E. Finke , Jessica Frie , Qinghong Fu , Dooseop Kim , Barbara Pio , Aurash Shahripour , Zhi-Cai Shi , Haifeng Tang
IPC: C07D401/10 , C07D211/28 , C07D487/04 , C07D405/14 , C07D211/48 , C07D471/08 , C07D211/62 , C07D413/14
CPC classification number: C07D401/10 , C07D211/28 , C07D211/48 , C07D211/62 , C07D403/10 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D471/08 , C07D487/04
Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
Abstract translation: 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。
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