Merck Sharp + Dohme Corp.

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

Elexopharm Gmbh

Nicox S.a.

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

Nicox

Msd R&d Co., Ltd.

Michael Man-Chu Lo

Amjad Ali

Robert D Mazzola, Jr

Timothy J Henderson

Xiaolei Gao

Sandra Lee Knowles

Chunsing Li

Jianming Bao

Edward Metzger

Ling Tong

Lin Yan

Yeon-Hee Lim

Brent Whitehead

Andrew William Stamford

Rongze Kuang

David M Tellers

Heping Wu

Scott T Harrison

Christopher L Franklin

Ravi P Nargund

Melissa S Egbertson

Pauline C Ting

Michael T Rudd

Iyassu Sebhat

Nicoletta Almirante

Qiaolin Deng

Paul Tempest

John J Acton, Iii

Fengqi Zhang

Oleg B Selyutin

Silvia Stefanini

Xianhai Huang

Dong Xiao

Younong Yu

Ennio Ongini

Rolf Wolfgang Hartmann

Zhaoyang Meng

Stefano Biondi

Jae-Hun Kim

Gioconda V Gallo

Ronald Dale Ferguson, Ii

Ralf Heim

Lina Yin

Qingzhong Hu

Meng Na

Shrenik K Shah

Hubert B Josien

Michael Berlin

Thomas Joseph Tucker

Jian Liu

Fa-Xiang Ding

Christopher W Boyce

Robert K Baker

Liangqin Guo

Harold B Wood

Rajan Anand

Manuel De Lera Ruiz

Tao Yu

Jayaram R Tagat

Junying Zheng

Laura Storoni

Nicolas Zorn

Walter Won

Abbas M Walji

Gang Zhou

Debra L Ondeyka

Zhiqiang Guo

Christina Zimmer

Chris Franklin

Kevin D McCormick

Kathleen M Rupprecht

Joseph Michael Kelly

Yusheng Xiong

Purakkattle J Biju

Bheemashankar A Kulkarni

Takao Suzuki

Clare London

Tanweer A Khan

Wei Zhou

Yonglian Zhang

James J Mulhearn

Scott B Hoyt

Pei Huo

Jerry Andrew Taylor

Xiaohong Zhu

Jianhua Cao

Vanessa L Rada

Swapan Kumar Samanta

Joe F Lee

Jun Wang

Sylvia Joanna Degrado

Jie Wu

Jeffrey W Schubert

Rohit Saxena

Jenny Miu-Chun Wai

Emmanuel Bey

James Dellureficio

Liwu Hong

Whitney Lane Petrilli

Ali Amjad

Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, 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 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

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 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.

Heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention is directed to 6,5-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.

6,5-fused heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of Areceptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which Areceptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which Areceptors are involved.

2,2-difluorodioxolo Areceptor antagonists

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 is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A-receptor is involved. The invention further involves use of the compounds as an A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases. 

Substituted aminoquinazoline compounds as Aantagonist

The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one 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.

6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor

6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor

The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. 

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Edison, NJ, United States of America

Michael Man-Chu Lo