Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Bristol-Myers Squibb Pharma Company

Merck Sharp & Dhome Corp.

Xin Gu

Shuzhi Dong

Alexander Pasternak

Jinlong Jiang

Fa-Xiang Ding

Sherman Tim Waddell

Haifeng Tang

James M Balkovec

Takao Suzuki

Li Xiao

Haiqun Tang

Zhiqiang Zhao

Dexi Yang

Jack D Scott

Donald W Graham

Milana M Maletic

Nancy J Kevin

Jessica Frie

Susan D Aster

Katherine Young

Gina M Santorelli

Aaron H Leeman

Frank W Bennett

Jianmin Fu

Yuhua Huang

Zhibo Zhang

Dipshikha Biswas

Joseph P Vacca

Zhicai Wu

Ian W Davies

Qinghong Fu

Yang Yu

Zhifa Pu

Shouning Xu

David N Hunter

Reynalda K DeJesus

Xu Zhang

Jinglan Zhou

William K Hagmann

Barbara A Pio

Mitree M Ponpipom

Shawn P Walsh

Guoqing Li

Ying-Duo Gao

Jing Su

Clare London

Weidong Pan

Jacqueline D Hicks

Aurash Shahripour

Gool F Patel

Mihir Mandal

Xu Bai

Shu-Wei Yang

Zhixiang Zheng

Cangming Yang

Hong Dong Chu

Yunfeng Bai

Matthew Lombardo

Reynalda Keh Dejesus

Reynalda DeJesus

Leslie Ann Robinson

Jinglong Jiang

Alex Pasternak

Nikolaus M Gubernator

Eddine Saiah

David Hunter

Reynalda Dejesus

Reynalda K Dejesus

Reynalda Keh De Jesus

Zhieai Wu

The present invention relates to metallo-&#x3b2;-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, R, X, Xand Rare as defined herein. The present invention also relates to compositions which comprise a metallo-&#x3b2;-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 &#x3b2;-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. 

Metallo-beta-lactamase inhibitors and methods of use thereof

The present invention relates to metallo-&#x3b2;-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, R, X, Xand Rare as defined herein. The present invention also relates to compositions which comprise a metallo-&#x3b2;-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 &#x3b2;-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.

Metallo-beta-lactamase inhibitors

The present invention relates to metallo-&#x3b2;-lactamase inhibitor compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, wherein Z, R, X, Xand Rare as defined herein. The present invention also relates to compositions which comprise a metallo-&#x3b2;-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 &#x3b2;-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. 

Metallo-&#x3b2;-lactamase inhibitors

The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, R, X, Xand Rare 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 &#x3b2;-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. 

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. 

Inhibitors of the renal outer medullary potassium channel

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. 

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. 

The present invention relates to compounds of formula (I) that are metallo-&#x3b2;-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with &#x3b2;-lactam antibiotics for overcoming resistance. 

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.

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.

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase Type 1 enzyme (11&#x3b2;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&#x3b2;-HSD-1.

Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

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Scotch Plains, NJ, United States of America

Xin Gu