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公开(公告)号：US20200281913A1
公开(公告)日：2020-09-10
申请号：US16631673
申请日：2018-07-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Shuzhi Dong , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Dexi Yang , Xin Gu , Jinlong Jiang , Li Xiao
IPC: A61K31/454 , C07D401/10 , C07D401/14 , C07D413/10 , C07D498/10 , C07D471/10 , C07D403/10 , C07D403/14 , C07D471/08 , C07D405/14 , A61K31/41 , A61K31/5377 , A61K31/5386 , A61K31/438 , A61K31/55 , A61K31/496 , A61K31/439 , A61K31/551 , A61K31/407 , A61K31/198 , A61P31/04
Abstract: The present invention relates to metallo-β-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-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：US20190144432A1
公开(公告)日：2019-05-16
申请号：US16244876
申请日：2019-01-10
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 , A61K31/198 , C07D403/12 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08 , A61K31/407 , A61K31/5025 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , C07D487/04 , A61K31/506 , C07D471/04 , C07D417/14 , C07D417/10 , C07D413/10 , C07D407/14 , C07D403/14 , C07D401/10 , C07D413/14 , A61K31/41
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-β-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-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：US10221163B2
公开(公告)日：2019-03-05
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: C07D403/14 , C07D403/10 , C07D403/12 , C07D413/14 , C07D401/10 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D487/04 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , 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：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：US20170037037A1
公开(公告)日：2017-02-09
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: C07D405/14 , A61K31/501 , A61K31/403 , A61K31/4439 , C07D487/04 , C07D413/14 , A61K31/497 , C07D471/04 , A61K31/437 , C07D417/14 , A61K31/427 , A61K45/06 , A61K31/41
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.
Abstract translation: 本发明提供了作为ROMK（Kir1.1）通道抑制剂的式（I）化合物及其药学上可接受的盐。 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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Patent Agency Ranking
公开(公告)号：US09206198B2
公开(公告)日：2015-12-08
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: C07D471/20 , A61K31/435 , A61K31/46 , A61K31/5386 , C07D471/10 , A61K45/06 , C07D498/20 , A61K31/4995 , C07D451/00 , C07D519/00
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.
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公开(公告)号：US10544130B2
公开(公告)日：2020-01-28
申请号：US16244876
申请日：2019-01-10
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 , C07D403/12 , C07D413/14 , C07D401/10 , C07D403/14 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D487/04 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
Abstract: The present invention relates to metallo-β-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-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：US20180179190A1
公开(公告)日：2018-06-28
申请号：US15737334
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 , David Hunter , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu , Yunfeng Bai , Zhixiang Zheng , Xu Zhang
IPC: C07D403/14 , A61K45/06 , A61K31/4184 , C07D401/14 , A61K31/454 , C07D471/04 , A61K31/437 , A61K31/4545 , C07D487/04 , A61K31/5025 , C07D403/10 , A61K31/416 , A61K31/4439 , C07D417/14 , A61K31/428 , A61K31/4375 , C07D413/14 , A61K31/423 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/506 , A61K31/498 , A61K31/5377 , 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-β-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and RB 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：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：US09708336B2
公开(公告)日：2017-07-18
申请号：US15110431
申请日：2015-01-16
Applicant: Merck Sharp & Dohme Corp.
Inventor： Mihir Mandal , Haifeng Tang , Li Xiao , Jing Su , Guoqing Li , Shu-Wei Yang , Weidong Pan , Haiqun Tang , Reynalda DeJesus , Jacqueline Hicks , Matthew Lombardo , Hong Chu , William Hagmann , Alex Pasternak , Xin Gu , Jinlong Jiang , Shuzhi Dong , Fa-Xiang Ding , Clare London , Dipshikha Biswas , Katherine Young , David N. Hunter , Zhiqiang Zhao , Dexi Yang
IPC: C07D491/048 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D401/04 , C07D409/10 , C07D487/04 , C07D471/10 , C07D471/04 , C07D451/04 , C07D417/14 , C07D417/10 , C07D413/10 , C07D401/14 , C07D405/12 , C07D405/10 , C07D403/10 , C07D401/10 , C07D413/14 , C07D405/14 , A61K31/41 , C07D257/04 , A61K31/197 , A61K31/407 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427
CPC classification number: C07D491/048 , A61K31/197 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D257/04 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , Y02A50/473 , A61K2300/00
Abstract: The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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