Merck + Co., Inc.

Merck Sharp + Dohme Corp.

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

Other

The Rockefeller University

Sunesis Pharmaceuticals, Inc.

Msd R&d Co., Ltd.

Melissa S Egbertson

George D Hartman

Mark E Duggan

Wasyl Halczenko

John S Wai

Steven D Young

Nathan C Ihle

Linghang Zhuang

William F Hoffman

Mark W Embrey

William L Laswell

Laura M Vassallo

Laura M Turchi

Harold G Selnick

Jianming Bao

Ling Tong

Michael Man-Chu Lo

Robert D Mazzola, Jr

David M Tellers

Xiaolei Gao

John J Acton, Iii

Thorsten E Fisher

Scott T Harrison

Chunsing Li

Oleg B Selyutin

H Marie Langford

Ben C Askew

Michael T Rudd

John D Prugh

Sandra Lee Knowles

Zhaoyang Meng

Robert J Gould

James P Guare

Fengqi Zhang

Joseph P Vacca

Julio Cesar Medina

Neville J Anthony

Craig Alan Coburn

Wenjin Yang

Shawn J Stachel

Shaun R Stauffer

Robert P Gomez

Timothy J Henderson

Terry A Lyle

Qiaolin Deng

Donnette D Staas

David Louis Clark

Lou Anne Neilson

Lekhanh O Tran

Catherine M Wiscount

David B Whitman

Vanessa L Rada

Boyoung Kim

Debra S Perlow

Georgia B McGaughey

Ronald Dale Ferguson, Ii

Wei Han

David A Claremon

John Howard Hutchinson

John M Sanders

Yimin Qian

Mark T Bilodeau

Samuel L Graham

William C Lumma, Jr

Dong-Ming Shen

James C Barrow

Juan Carlos Jaen

Dansu Li

James J Perkins

Deping Wang

Philippe G Nantermet

Mark E Layton

Michelle R Machacek

David Askin

Ulf H Dolling

XiaoXia Qian

Anthony J Roecker

Richard Berger

Takao Suzuki

Philip J Pye

Xuanjia Peng

Jules A Shafer

Christopher Joseph Sinz

James J Mulhearn

Linda S Payne

Shimin Xu

Hemaka Anthony Rajapakse

R Scott Hoerrner

Zhi-Qiang Yang

Kenneth E Rittle

Melody McWherter

Yiwei Li

Bart Harper

Edward J Brnardic

Meng Yang

John C Hartnett

Ming Wang

Jonathan E Wilson

Mark Cameron

Bohumil Bednar

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.

Pyranoyrazoles and pyrazolopyridines of formula I or formula II are disclosed:  These compounds inhibit Coagulation Factor XIIa in the presence of thrombin and other coagulation factors. They are useful to treat autoimmune diseases.

Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases

2-Acylindazole compounds of formula I or formula II are disclosed: These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.

Aminoacylindazole immunomodulators for treatment of autoimmune diseases

Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof. 

Pyrimidone carboxamide compounds as PDE2 inhibitors

Disclosed are compounds of Formula A-a, or a salt thereof: Where 'B' and 'R' through &#x201c;R&#x201d; are as defined herein, which compounds have properties for blocking Na1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same. 

Bicycloamine-substituted-N-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels

The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C. 

TrkA kinase inhibitors, compositions and methods thereof

The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

TRPA1 antagonists

The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Quinolinone PDE2 inhibitors

The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease

Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

HIV integrase inhibitors

Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R, R, R, R, R, Rand Rare defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

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Ambler, PA, United States of America

Melissa S Egbertson