Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Canada Inc.

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

Msd R&d Co., Ltd.

Peter D Williams

Roger M Freidinger

John A McCauley

Christopher James Bungard

David Jonathan Bennett

Catherine M Wiscount

Mark G Bock

Daniel F Veber

Ben E Evans

John S Wai

Terry A Lyle

Satyanarayana Tummanapalli

Philippe G Nantermet

Oscar Miguel Moradei

Thomas J Greshock

Donnette D Staas

Vouy Linh Truong

Christian Beaulieu

Carmela Molinaro

Kenneth E Rittle

Sheldon N Crane

Harold G Selnick

Ian M Bell

Philip E Sanderson

M Katharine Holloway

Thorsten E Fisher

Douglas J Pettibone

Kevin F Gilbert

Debra S Perlow

Matthew M Morrissette

Kenneth J Stauffer

Doug W Hobbs

Joseph M Pawluczyk

Daniel Mckay

Michelle A Sparks

Craig Alan Coburn

Michael P Dwyer

Bin Hu

James C Barrow

Sherman Tim Waddell

Gregori J Morriello

Xin-Jie Chu

Mark W Embrey

Kartik M Keertikar

Lehua Chang

Tao Ji

Bin Zhong

Lekhanh O Tran

H Marie Loughran

H Marie Langford

J Christopher Culberson

Jesse J Manikowski

Mary Beth Young

William J Greenlee

Roger D Tung

Scott D Kuduk

Joseph P Vacca

Brian Alexander McKittrick

Linghang Zhuang

Thomas Allen Miller

Dong-Ming Shen

Jason D Brubaker

Elizabeth M Smith

Craig A Stump

Joey Lee Methot

Phieng Siliphaivanh

Christopher S Burgey

Shankar Venkatraman

Wayne J Thompson

Thomas S Reger

Dai-Shi Su

Ralph A Rivero

Christian Fischer

Peter Emmanuel Maligres

Zhiguo Jake Song

Tanweer A Khan

Richard Wayne Heidebrecht, Jr

Andrew John Cooke

Paul S Anderson

William D Shipe

Nicolas Zorn

James P Guare

Ronald K Chang

Tao Pei

Edward C Sherer

Alejandro Crespo

Elizabeth Helen Kelley

Rachel Nicola MacCoss

Boyoung Kim

Jingjun Yin

Karin M Otte

David C Dubost

Richard C A Isaacs

Neil A Strotman

Michael Shevlin

William Colby Brown

Richard G Ball

Stephanie Lessard

Matthew L Maddess

The present invention is directed to compounds of Formula (I), pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. 

Heterocyclic compounds as HIV protease inhibitors

The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. 

Piperazine derivatives as HIV protease inhibitors

The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z, Z, V, V, V, R, R, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

HIV protease inhibitors

The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The present invention is directed to 4-fluoropiperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.

4-fluoropiperidine orexin receptor antagonists

The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative &#x3b3;-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Diaryl ether derivatives as notch sparing gamma secretase inhibitors

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, 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.

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z, R, R, 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.

8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I), wherein 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described. 

Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors

Bicyclic pyrazoles of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z is O or N(R); n is an integer equal to zero or 1; and R, 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.

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)&#x2014;N(R)CH(R)&#x2014; wherein the nitrogen atom is attached to R, and Rand Rare independently selected from the group consisting of hydrogen, Ccycloalkyl, and Calkyl, or 2) wherein the nitrogen atom is attached to R, and m is 0, 1, or 2 

Thrombin inhibitors

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Harleysville, PA, United States of America

Peter D Williams