Merck Sharp + Dohme Corp.

Sanofi

Ra Pharmaceuticals, Inc.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Indiana University

Merck + Co., Inc.

Medimmune Limited

Janssen Biotech, Inc.

Eniricerche S.p.a.

Ambrx, Inc.

Protagonist Therapeutics, Inc.

Msd Italia S.r.l.

Whitehead Institute for Biomedical Research

Cambridge Antibody Technology Limited

Merck Sharp & Dohme LLC

Elisabetta Bianchi

Antonello Pessi

Raffaele Ingenito

Thomas Joseph Tucker

Danila Branca

Alessia Santoprete

Chengwei Wu

Yusheng Xiong

Angela Dawn Kerekes

Sookhee Nicole Ha

Federica Orvieto

Anandan Palani

Hyewon Youm

Alonso Ricardo

Olivier Duclos

Qiaolin Deng

Sergio Mallart

Nicolas Cedric Boyer

Aurash Shahripour

Ravi P Nargund

Hubert B Josien

Fa-Xiang Ding

Abbas M Walji

Richard Dennis DiMarchi

Ling Tong

Nick Knudsen

Tomi K Sawyer

Jian Liu

Harold B Wood

Eric J Gilbert

Robert M Garbaccio

Mark W Embrey

David L Smiley

Andreas Evers

Zhong Ma

Ketki Ashok Dhamnaskar

Frank Marguet

Anilkumar G Nair

Wolfgang Seghezzi

Yun-Ping Zhou

Michael D Miller

Ashok Bhandari

Brian Troy Frederick

Jonathan Wesley Day

Armin Lahm

Peter S Kim

Nis Halland

Yuping Zhu

Sobhana Babu Boga

John W Shiver

Debra Muir Eckert

Daria Hazuda

Joseph M Metzger

Maria A Bednarek

Paul E Carrington

Paolo Ingallinella

Stéphane Illiano

Claire Minoletti-Hochepied

Paola Magotti

Willy Costantini

Donald J Marsh

George J Eiermann

Ranabir Sinha Roy

Dennis P Gately

Immacolata Conte

Yingjun Mu

Stefania Colarusso

Anthony Manibusan

Grigori Ermakov

Joseph R Stringer

Derek M LaPlaca

Roberto Costante

Chunhui Huang

Brian P Ward

Licia Tomei

Philip Janiak

Raffaele De Francesco

Giampietro Corradin

Michael J Root

Ralf Elvert

Romas Geleziunas

Sandeep Somani

Chengzao Sun

Denis Brasseur

Raymond Patch

Stephanie A Barros

David Bramhill

Simon N Lennard

Daniela Fattori

Christian Steink&uuml;hler

Andrea Urbani

Marina Taliani

Frank Narjes

Anna Demartis

Ziyu Li

Alessandro Pocai

Elena Capito

Philippe Beauverger

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

PCSK9 antagonist compounds

The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases.

Peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory diseases

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

Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog 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 agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

Antibody peptide conjugates that have agonist activity at both the glucagon and glucagon-like peptide 1 receptors

A biologically active single chain Relaxin peptide having the formula N-Ac-L-E-G-R-E-K-V-R-A-X-I-X-X-E-G-X-S-T-F-S-X-R-A-X-NH-C, or a salt of solvate thereof, is described.

Modified lipidated relaxin B chain peptides and their therapeutic use

Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

Long-acting co-agonists of the glucagon and GLP-1 receptors

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

Provided is a biologically active single chain Relaxin peptide having the following formula (I):N-Ac-(E)-X-E-G-R-E-X-V-R-X-X-I-X-X-E-G-X-S-X-X-X-X-R-(X)-(X)-(K)-(X)-(gE)-X-C; or a salt or solvate thereof. Also provided is a pharmaceutical composition comprising at least one peptide of the invention, and the peptide or the pharmaceutical composition for its use as a medicament.

Modified lipidated Relaxin B chain peptides and their therapeutic use

Provided is a biologically active single chain Relaxin peptide having the following formula (I): N-X-(E)-X-E-G-R-E-X-V-R-X-X-I-X-X-E-G-X-S-X-X-X-X-R-(X)-(X)-(X)-NH-C. Also provided is a pharmaceutical composition comprising at least one peptide of the invention, or a pharmaceutically acceptable salt or a solvate thereof. Further provided is the peptide, a pharmaceutically acceptable salt or solvate thereof, or the pharmaceutical composition for use as a medicament.

Modified relaxin B chain peptides and their therapeutic use

Provided is a biologically active single chain Relaxin peptide having the following formula (I) (SEQ ID NO 105): N-Ac-X-E-G-R-E-X-V-R-X-X-I-X-X-E-G-X-S-X-X-X-X-X-X-X-NH-Cor a salt or solvate thereof. Also provided is a pharmaceutical composition comprising at least one biologically active single chain Relaxin peptide. Uses of the peptide or the pharmaceutical composition as a medicament are also provided.

Growing community of inventors

Pomezia, Italy

Elisabetta Bianchi