Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Intervet Inc.

Msd R&d Cn Co., Ltd

Cardiome International Ag

Jingjun Yin

Artis Klapars

Kevin Campos

Kevin Michael Belyk

Tetsuji Itoh

Wensong Xiao

Jacob M Janey

John S Wai

Peter D Williams

Shankar Venkatraman

Gregory Hughes

Wayne J Thompson

Richard John Varsolona

Dai-Shi Su

Mark W Embrey

Peter Emmanuel Maligres

Zhiguo Jake Song

Mark A Huffman

Hallena Strotman

Zhuqing Liu

Fred J Fleitz

Edward Cleator

Jianguo Yin

Gregory L Beutner

John Limanto

Thorsten E Fisher

Tao Pei

Alexei Kalinin

Ji Qi

Michel Journet

Harald Schmitt

Cheol Keun Chung

Yonggang Chen

Qinghao Chen

Zhijian Liu

Bangping Xiang

Ian Mangion

Louis-Charles Campeau

Matthew D Truppo

David C Dubost

Michael Shevlin

Jeffrey T Kuethe

Eric Ashley

Neil A Strotman

Richard C A Isaacs

Alan Michael Hyde

Richard G Ball

Dietrich P Steinhuebel

Matthew L Maddess

Melodie Deniz Christensen

Eric J Choi

Aaron M Dumas

Matthew Thomas Tudge

Hongming Li

Andrew Brunskill

Lichen Song

Brendan Grau

Daniel Salanta

Claudia Scheipers

Thomas Dahmen

Neil Campbell

Sarah L Trice

Hallena R Strotman

Eric R Ashley

Matthew Maddess

The application relates to processes for the preparation of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide (I) which include (i) a synthesis for bromo and iodo pyridine intermediates, (ii) a synthesis of a pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I).

Process for preparing 1-([3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide

The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention. 

Process for preparing substituted tetracyclic heterocycle compounds

The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X, X, R, Rand Rare defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.

Process for making tetracyclic heterocycle compounds

The present invention is directed to processes for preparing an intermediate for a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.

Process for the preparation of an intermediate for an orexin receptor antagonist

The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates. 

Process for preparing aminocyclohexyl ether compounds

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

The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Process for making hydroisoindoline tachykinin receptor antagonists

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Green Brook, NJ, United States of America

Jingjun Yin