Merck Sharp + Dohme Corp.

Aventis Pharmaceuticals Inc.

Fa-Xiang Ding

Jinlong Jiang

Shuzhi Dong

Haifeng Tang

Alexander Pasternak

Xin Gu

Takao Suzuki

Hubert B Josien

Thomas Joseph Tucker

Hong Shen

Jian Liu

Harold B Wood

Jing Su

Joseph P Vacca

Barbara A Pio

Elisabetta Bianchi

Yusheng Xiong

Shawn P Walsh

Yan Guo

William K Hagmann

Xianhai Huang

Dong-Ming Shen

Steven L Colletti

Ling Tong

Michael Man-Chu Lo

Zhicai Wu

Dooseop Kim

Liangqin Guo

Guoqing Li

Ian W Davies

Li Xiao

Subharekha Raghavan

Harry R Chobanian

Wanying Sun

John P Caldwell

Christina B Madsen-Duggan

Linda Brockunier

Darby Schmidt

Tesfaye Biftu

Rose Yen

Jianming Bao

Thomas H Graham

Rui Liang

Zhi-Cai Shi

James R Tata

Helen Y Chen

Anthony K Ogawa

Yeon-Hee Lim

Clare London

Christopher W Plummer

Timothy A Blizzard

Abbas M Walji

Sookhee Nicole Ha

Jessica Frie

Mihir Mandal

Shu-Wei Yang

Weidong Pan

Angela Dawn Kerekes

Danila Branca

Chengwei Wu

Dipshikha Biswas

Shouning Xu

Weiguo Liu

Marc A Labroli

Ginny Dai Ho

Haiqun Tang

Dexi Yang

Anilkumar G Nair

Qinghong Fu

Yang Yu

William Arthur Metz, Jr

Christine Yang

Zheng Tan

Hongwu Wang

Reynalda Keh Dejesus

Zhifa Pu

Sandra J Koseoglu

Sang Ho Lee

Zhiqiang Zhao

Min K Park

Jacqueline D Hicks

John E Stelmach

Raffaele Ingenito

Jianping Pan

Timothy Allen Blizzard

Yuhua Huang

Sobhana Babu Boga

Aurash Shahripour

Katherine Young

Yi Zang

Hyewon Youm

Jian Guo

Alessia Santoprete

Cangming Yang

Keith Rosauer

Rudrajit Mal

Hong Dong Chu

Candido Gude

James Patrick Roane

Jonathan A Groeper

Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

Diacylglyceride O-acyltransferase 2 inhibitors

Disclosed are compounds of Formula I, or a salt thereof:

PCSK9 antagonist compounds

Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R, and Rare as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic.

Oxazolidinones as TarO inhibitors

Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R, Rand Rare as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.

Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R, and Rare as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions 

PCSK9 antagonists bicyclo-compounds

The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, Q, A, M, W, Rand Rare as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic. 

Oxazolidinones as taro inhibitors

The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 ('DGAT2') and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. 

Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2

The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, L, M, W, X, Y, Z, Rand Rare as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds. 

Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

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) (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. 

Inhibitors of the renal outer medullary potassim 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. 

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Staten Island, NY, United States of America

Fa-Xiang Ding