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公开(公告)号：US20150099729A1
公开(公告)日：2015-04-09
申请号：US14569858
申请日：2014-12-15
Applicant: Merck Sharp & Dohme Corp.
Inventor： Fa-Xiang Ding , Shuzhi Dong , Jessica Frie , Xin Gu , Jinlong Jiang , Alexander Pasternak , Haifeng Tang , Zhicai Wu , Yang Yu , Takao Suzuki
IPC: C07D498/20 , C07D471/20 , C07D471/10
CPC classification number: C07D498/20 , A61K31/435 , A61K31/46 , A61K31/4995 , A61K31/5386 , A61K45/06 , C07D451/00 , C07D471/10 , C07D471/20 , C07D519/00
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 conditions associated with excessive salt and water retention.
Abstract translation: 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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公开(公告)号：US20140031349A1
公开(公告)日：2014-01-30
申请号：US13951096
申请日：2013-07-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Fa-Xiang Ding , Shuzhi Dong , Jessica Frie , Xin Gu , Jinlong Jiang , Alexander Pasternak , Haifeng Tang , Zhicai Wu , Yang Yu , Takao Suzuki
IPC: A61K31/5386 , A61K31/435 , C07D451/00 , A61K45/06 , C07D471/20 , A61K31/4995 , C07D498/20 , C07D471/10 , A61K31/46
CPC classification number: C07D498/20 , A61K31/435 , A61K31/46 , A61K31/4995 , A61K31/5386 , A61K45/06 , C07D451/00 , C07D471/10 , C07D471/20 , C07D519/00
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 conditions associated with excessive salt and water retention.
Abstract translation: 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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公开(公告)号：US10208064B2
公开(公告)日：2019-02-19
申请号：US15323989
申请日：2015-07-09
Applicant: 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
Inventor： Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC: C07D513/10 , C07D519/00 , A61K45/06 , A61K31/435 , A61K31/4745 , A61K31/4375
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：US20180244656A1
公开(公告)日：2018-08-30
申请号：US15737351
申请日：2016-06-24
Applicant: Merck Sharp & Dohme Corp.
Inventor： Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu
IPC: C07D403/10 , A61K31/4184 , C07D401/10 , A61K31/4709 , A61K31/416 , C07D413/10 , A61K31/423 , C07D417/10 , A61K31/428 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/454 , C07D471/04 , C07D495/08 , C07D487/10 , A61K31/541 , C07D493/04 , C07D493/08 , C07D453/02 , C07D403/14 , C07D405/14 , A61K31/41 , A61K31/4245 , A61K31/4192 , A61K31/421 , A61K31/4196 , A61K31/198 , A61K31/431 , A61K31/546 , A61K31/4545 , A61K31/439 , A61K31/407 , A61P31/04
CPC classification number: C07D403/10 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/431 , A61K31/437 , A61K31/4375 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/546 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-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：US09765074B2
公开(公告)日：2017-09-19
申请号：US14774390
申请日：2014-03-10
Applicant: Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Dipshikha Biswas , Haifeng Tang , Jinlong Jiang , Cangming Yang , Xin Gu
IPC: A61K31/24 , C07D471/10 , A61K31/401 , C07D471/20 , A61K31/403 , A61K31/405 , A61K31/407 , A61K31/41 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/472 , A61K31/4965 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/554 , A61K31/585 , A61K31/675 , A61K31/435 , A61K31/444 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5386 , A61K45/06 , C07D498/20
CPC classification number: 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
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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Patent Agency Ranking
公开(公告)号：US09718808B2
公开(公告)日：2017-08-01
申请号：US15106847
申请日：2015-01-05
Applicant: Merck Sharp & Dohme Corp.
Inventor： Dipshikha Biswas , Fa-Xiang Ding , Shuzhi Dong , Xin Gu , Jinlong Jiang , Alexander Pasternak , Takao Suzuki , Joseph Vacca , Shouning Xu
IPC: A61K31/501 , A61K31/403 , A61K31/4439 , A61K31/497 , A61K31/437 , A61K31/427 , A61K31/41 , C07D405/14 , C07D487/04 , C07D413/14 , C07D471/04 , C07D417/14 , A61K31/506 , A61K45/06
CPC classification number: C07D405/14 , A61K31/403 , A61K31/41 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , 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：US20170197989A1
公开(公告)日：2017-07-13
申请号：US15323989
申请日：2015-07-09
Applicant: 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.
Inventor： Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC: C07D519/00 , A61K31/4745 , A61K31/4375 , A61K31/435
CPC classification number: C07D519/00 , A61K31/435 , A61K31/4375 , A61K31/4745 , A61K45/06
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：US09604998B2
公开(公告)日：2017-03-28
申请号：US14768245
申请日：2014-02-12
Applicant: MERCK SHARP & DOHME CORP.
Inventor： 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: A61K31/401 , C07D498/04 , A61K31/5383 , C07D487/04 , C07D519/00 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/4985 , A61K31/55 , A61K31/675 , A61K45/06
CPC classification number: 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
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, kidney disease, edema, 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
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：US20160002259A1
公开(公告)日：2016-01-07
申请号：US14768245
申请日：2014-02-12
Applicant: 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.
Inventor： 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: C07D498/04 , A61K45/06 , A61K31/4985 , A61K31/5383 , C07D487/04
CPC classification number: 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
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, kidney disease, edema, and conditions associated with excessive salt and water retention.
Abstract translation: 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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