Merck Sharp + Dohme Corp.

Bristol-myers Squibb Compnay

Neil A Strotman

Benjamin Cohen

Jun Li

John S Wai

Peter D Williams

Shankar Venkatraman

Wayne J Thompson

Dai-Shi Su

Mark W Embrey

Peter Emmanuel Maligres

Zhiguo Jake Song

Yi Xiao

Martin D Eastgate

Edward Cleator

Qi Gao

Gregory L Beutner

Thorsten E Fisher

Victor W Rosso

Michael Shawn Lawler

Bin Zheng

Michael J Smith

Tao Pei

Ke Chen

Nicolas Cuniere

Christopher S Regens

Faye Sheen

Jingjun Yin

Jianji Wang

Thorsten Rosner

Eric M Simmons

David C Dubost

Junying Fan

Peng Geng

Shane W Krska

Gavin William Stewart

Carl A Baxter

Lopa V Desai

Joerg Deerberg

Amanda J Rogers

Paul C Lobben

Richard C A Isaacs

Carolyn S Wei

Michael Shevlin

Timothy James Wright

Matthew L Maddess

Dietrich P Steinhuebel

Keming Zhu

Daniel S Treitler

Tamas Benkovics

Richard G Ball

Debra J Wallace

Dimitri Skliar

Alina Borovika

Dong Lin

Michael Dummeldinger

Bahar Inankur

Maxime C D Soumeillant

Eric J Choi

Jason Michael Stevens

Monica Fitzgerald

Michael Bryan Hay

Sarah L Trice

Neil Campbell

Sergei V Kolotuchin

Matthew Maddess

Edward Cleartor

Timothy Wright

Steven Tymonko

Disclosed is a process for preparing (S)-4-(3-(but-2-ynamido)piperidin fluoro-2,3-dimethyl-1H-indole-7-carboxamide, comprising the steps of: preparing a compound of Formula (III); converting the compound of Formula (III) to a compound of Formula (V); and reacting the compound of Formula (V) with a compound of Formula (VI) to provide (S)-4-(3-(but-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide. 

Process for preparing indole carboxamide compounds

The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis. 

Process for the preparation of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide

The present invention is directed to processes for preparing 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. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.

Process for the preparation of an orexin receptor antagonist

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

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Flemington, NJ, United States of America

Neil A Strotman