Merck Sharp + Dohme Corp.

Ra Pharmaceuticals, Inc.

Agency for Science, Technology and Research

Msd International Gmbh (Singapore Branch)

Sookhee Nicole Ha

Thomas Joseph Tucker

Elisabetta Bianchi

Yusheng Xiong

Angela Dawn Kerekes

Danila Branca

Chengwei Wu

Nicolas Cedric Boyer

Fa-Xiang Ding

Alonso Ricardo

Jing Su

Christina B Madsen-Duggan

John P Caldwell

Marc A Labroli

Ginny Dai Ho

Raffaele Ingenito

Aurash Shahripour

Mihir Mandal

Hyewon Youm

Shu-Wei Yang

Christine Yang

Zheng Tan

Willy Costantini

Sandra J Koseoglu

Hao Wang

Christopher Michael Tan

Terry Roemer

Sang Ho Lee

Scott D Edmondson

Gregori J Morriello

Cheng Zhu

Bing Li

Ihor E Kopka

Richard Berger

Liping Wang

Stephen D Goble

Lehua Chang

Nam Fung Kar

Chris Moyes

Hubert B Josien

Dong-Ming Shen

Ling Tong

Jian Liu

Haifeng Tang

Harold B Wood

Eric J Gilbert

Zhong Ma

Mark W Embrey

Weidong Pan

Ketki Ashok Dhamnaskar

Jianping Pan

Anilkumar G Nair

Abbas M Walji

Alessia Santoprete

Immacolata Conte

Stefania Colarusso

Joseph R Stringer

Derek M LaPlaca

Charles J Gill

Reynalda De Jesus

Roberto Costante

Tomi K Sawyer

Helen Y Chen

Timothy A Blizzard

Sobhana Babu Boga

Nelo R Rivera

Chunhui Huang

Jason Eugene Imbriglio

Ian Mangion

Charles William Johannes

Candido Gude

Jane Yang Wu

Jeffrey Donald Hermes

Michael Shevlin

Seongkon Kim

Tsz Ying Yuen

Rebecca T Ruck

Christopher J Mortko

Ding-Ming Shen

Michael B Garrigou

Pietro Aronica

Srinivasaraghavan Kannan

Anthony W Partridge

Chris R Moyes

The invention provides compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein the variables are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (K-Ras) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Macrocyclic peptides as potent inhibitors of K-RAS G12D mutant

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

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.

Benzimidazoles and indoles as taro inhibitors

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.

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 provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of &#x3b2;3-adrenoceptor. 

Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists

Hydroxymethyl pyrrolidines as &#x3b2;3 adrenergic receptor agonists

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Warren, NJ, United States of America

Sookhee Nicole Ha