Merck Sharp + Dohme Corp.

Schering Corporation

Msd R&d (china) Co., Ltd.

Other

Southern Research Institute

Merck Msd (r&d) China Co., Ltd.

Msd R&d Co., Ltd.

Ling Tong

Joseph A Kozlowski

Bandarpalle B Shankar

Brian J Lavey

Wensheng Yu

Neng-Yang Shih

Dansu Li

M Arshad Siddiqui

Janeta Popovici-Muller

Vincent Stewart Madison

Michael Man-Chu Lo

Zhuyan Guo

Robert D Mazzola, Jr

Jianming Bao

Melissa S Egbertson

Michael T Rudd

Craig Alan Coburn

Ronald L Wolin

Bin Hu

Harold B Wood

Hubert B Josien

Thomas Joseph Tucker

Fa-Xiang Ding

Elisabetta Bianchi

Yusheng Xiong

F George Njoroge

Michael P Dwyer

Frank W Bennett

David James Witter

Xianhai Huang

Lei Chen

Ashok Arasappan

Jack D Scott

Jian Liu

Joey Lee Methot

Qin-Yi Tong

Jongwon Lim

Kevin J Wilson

Srikanth Venkatraman

John A Secrist, Iii

David L Sloman

Malcolm Maccoss

Ping Liu

Phieng Siliphaivanh

Christopher W Boyce

Thomas H Graham

Solomon D Kattar

Wei Wei

Raman Kumar Bakshi

Subramaniam Ananthan

Jason W Skudlarek

Izzat Tiedje Raheem

Michael K C Wong

Guowei Zhou

De-Yi Yang

Razia Rizvi

Seong Heon Kim

Vinay M Girijavallabhan

Kristin E Rosner

Chaoyang Dai

Peter Orth

Chunsing Li

David M Tellers

Xiaolei Gao

Sandra Lee Knowles

John J Acton, Iii

Scott T Harrison

Umar Faruk Mansoor

Timothy J Henderson

Zhaoyang Meng

Dahai Wang

Fengqi Zhang

Bin Zhong

Richard J Friary

Qiaolin Deng

Angela Dawn Kerekes

Sookhee Nicole Ha

Anilkumar G Nair

Abbas M Walji

Deyou Sha

Milana M Maletic

Santhosh Francis Neelamkavil

Kartik M Keertikar

Matthew H Daniels

Blair T Lapointe

Takao Suzuki

Peter H Fuller

Wei Zhou

Weiguo Liu

Francisco Velazquez

Joseph A Maddry

James J Mulhearn

Hakan Gunaydin

Feng Geng

Vishal Verma

Vladimir Simov

Yuhua Huang

Sobhana Babu Boga

Tao Ji

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

PCSK9 antagonist compounds

The present invention is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor

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.

The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved. 

Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof

The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

5-(pyridin-3-yl)oxazole allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention is directed to 6,6-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

6,6-fused heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention relates to novel Chromane-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', RR, Rand Rare as defined herein. The present invention also relates to compositions comprising a Chromane-Substituted Tetracyclic Compound, and methods of using the Chromane-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient. 

Chromane-substituted tetracyclic compounds and uses thereof for the treatment of viral diseases

The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', RRand Rare as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient. 

Heterocycle-substituted tetracyclic compounds and methods of use thereof for the treatment of viral diseases

The present invention relates to novel Fused Tetracyclic Heterocyclic Compounds of Formula I: (I), wherein A, A', R, R, R, R, R, and Rare defined herein. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The present invention also relates to pharmaceutical compositions comprising at least one Fused Tetracyclic Heterocyclic Compound, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines, and methods of using the Fused Tetracyclic Heterocyclic Compounds for treating or preventing HCV infection in a patient. 

Fused tetracyclic heterocyclic compounds and methods of use thereof for the treatment of viral diseases

The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', RR, Rand R are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient. 

The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R, X, Y, Z, R, R, R, R, R, R, R, R, R, Rand n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. 

Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). 

Compounds that are ERK inhibitors

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Warren, NJ, United States of America

Ling Tong