Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Ra Pharmaceuticals, Inc.

Quixgen, Inc.

Merck Sharpe & Dohme Corp.

Elexopharm Gmbh

Yusheng Xiong

Clare London

Scott B Hoyt

Hyewon Youm

Angela Dawn Kerekes

Thomas Joseph Tucker

Elisabetta Bianchi

Danila Branca

Chengwei Wu

Rui Liang

Bheemashankar A Kulkarni

Andrew John Cooke

Sookhee Nicole Ha

Emma Louise Carswell

Paul David Ratcliffe

Jerry Andrew Taylor

D Jonathan Bennett

Raffaele Ingenito

Jason Eugene Imbriglio

Swapan Kumar Samanta

Jaiqiang Cai

Alonso Ricardo

Nicolas Cedric Boyer

Min K Park

Aurash Shahripour

Jian Guo

Willy Costantini

Hubert B Josien

Emma R Parmee

Zhijian Lu

Fa-Xiang Ding

James R Tata

Linda Brockunier

John K MacLean

Abbas M Walji

Alessia Santoprete

John MacLean

Hong-Ping Guan

Ming You

Amjad Ali

Ling Tong

Zhong Ma

Mark W Embrey

Arthur A Patchett

Suresh B Singh

Frank W Bennett

Jian Liu

Kevin Tyler Chapman

Eric J Gilbert

Harold B Wood

Ketki Ashok Dhamnaskar

Anilkumar G Nair

Immacolata Conte

Stefania Colarusso

Rohit Saxena

Joseph R Stringer

Derek M LaPlaca

Whitney Lane Petrilli

Roberto Costante

Wenjun Huang

Michael Man-Chu Lo

Zhicai Wu

Songnian Lin

Derun Li

Subharekha Raghavan

Timothy J Henderson

Wonsuk Chang

Rolf Wolfgang Hartmann

Tanweer A Khan

Harry R Davis

Brent Whitehead

Pengcheng Patrick Shao

Sobhana Babu Boga

Feng Ye

Jiaqiang Cai

Claire Lankin

Andrew Cooke

Yang Yu

Ralf Heim

Jose M Castro-Perez

Qingmei Hong

Lina Yin

Qingzhong Hu

Emmanuel Bey

Kenneth Marby

Zhe Feng

George Scott Tria

Michael Lo

Archana Gupta

Tiebang Wang

Venukrishnan Komanduri

Samuel S Engel

Anthappan Tony Kurissery

Samuel E Engel

Douglas G Johns

Stephen F Previs

Thomas P Roddy

Liangsu Wang

Sheng-Ping Wang

The present invention relates to Compounds of Formula I: and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment of cardiometabolic diseases including high blood pressure, heart failure, kidney disease, and diabetes in a subject.

Natriuretic peptide receptor a agonists useful for the treatment of cardiometabolic diseases, kidney disease and diabetes

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

PCSK9 antagonist compounds

Provided herein are spirolactone compounds of Formula I that are useful as inhibitors of ACC1 and/or ACC2. The spirolactone compounds described herein can be used for treating a disease or disorder associated with aberrant ACC1 and/or ACC2 activities, for example, non-alcoholic steatohepatitis (NASH), acne, obesity, diabetes, and cancer. Also provided herein are pharmaceutical compositions comprising the spirolactone compound of Formula I, or pharmaceutically acceptable salt thereof.

Spirolactone compounds

Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.

Cyclic polypeptides for PCSK9 inhibition

Provided herein are spirolactone compounds of Formula I that are useful as inhibitors of ACC1 and/or ACC2. The spirolactone compounds described herein can be used for treating a disease or disorder associated with aberrant ACC1 and/or ACC2 activities, for example, non-alcoholic steatohepatitis (NASH), acne, obesity, diabetes, and cancer. Also provided herein are pharmaceutical compositions comprising the spirolactone compound of Formula I, or pharmaceutically acceptable salt thereof. 

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

Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.

Methods of treating diabetes by administering a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor

The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X, X, Y, R, R, R, Rand n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples. 

Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as PCSK9 allosteric binders

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, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. 

Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2

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, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. 

This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

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Plainsboro, NJ, United States of America

Yusheng Xiong