Merck Sharp + Dohme Corp.

Ra Pharmaceuticals, Inc.

Chengwei Wu

Thomas Joseph Tucker

Elisabetta Bianchi

Yusheng Xiong

Angela Dawn Kerekes

Danila Branca

Sookhee Nicole Ha

Raffaele Ingenito

Hyewon Youm

Alonso Ricardo

Nicolas Cedric Boyer

Aurash Shahripour

Willy Costantini

Hubert B Josien

Fa-Xiang Ding

Abbas M Walji

Alessia Santoprete

Ling Tong

Jian Liu

Harold B Wood

Eric J Gilbert

Zhong Ma

Mark W Embrey

Ketki Ashok Dhamnaskar

Anilkumar G Nair

Immacolata Conte

Stefania Colarusso

Joseph R Stringer

Derek M LaPlaca

Roberto Costante

Ravi P Nargund

Anandan Palani

Antonello Pessi

Qiaolin Deng

Sobhana Babu Boga

Federica Orvieto

Paul E Carrington

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

PCSK9 antagonist 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

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

Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

Co-agonists of the glucagon and GLP-1 receptors

Growing community of inventors

Ambler, PA, United States of America

Chengwei Wu