Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Aicuris Anti-infective Cures Gmbh

Msd R&d Cn Co., Ltd

Kevin Michael Belyk

Guy R Humphrey

Mark E Scott

John Limanto

Alexander Pasternak

Barbara A Pio

Haifeng Tang

Shawn P Walsh

Kevin Campos

Edward Cleator

Jianguo Yin

Aurash Shahripour

Hsien-Hsin Tung

Philip Jones

Lihu Yang

Nobuyoshi Yasuda

Wilfried Schwab

Dooseop Kim

Vincenzo Summa

Zhi-Cai Shi

Richard John Varsolona

Helen Y Chen

Harry R Chobanian

Yan Guo

Shen-Chun Kuo

Peter Emmanuel Maligres

Philip J Pye

Zhuqing Liu

Artis Klapars

Lushi Tan

Cheol Keun Chung

Bangping Xiang

Paul Gerard Bulger

William R Leonard

Jingjun Yin

Amar J Mahajan

Daniel J Kumke

Tetsuji Itoh

Vanessa Pruzinsky

Lawrence Wai

Henry G Morrison

Yuping Zhu

Jessica Frie

David L Hughes

Timothy Allen Blizzard

Nelo R Rivera

Alexei Kalinin

Regina M Black

Ji Qi

Yonggang Chen

Brian Cato

Qinghao Chen

Reynalda Keh Dejesus

Louis-Charles Campeau

Burkhard Klenke

Dean R Bender

Alan Michael Hyde

Remy Angelaud

Reynalda K DeJesus

Wensong Xiao

Michael R Luzung

Danny Mancheno

Andrew Brunskill

Aaron M Dumas

Melodie Deniz Christensen

Hongming Li

Matthew Thomas Tudge

Stephen Mark Dalby

Naoki Yoshikawa

Tom Moody

Gareth Brown

V Brett Cooper

Enrique Vazquez

Benjamin Dorner

A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

Regioselective N-2 arylation of indazoles

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 a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I). 

Process for making substituted quinazoline compounds

The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine, utilizing a highly effective spiroacid synthesis.

Process for making CGRP receptor antagonists

This invention relates to compounds of Formula I-VI having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

Inhibitors of the Renal Outer Medullary Potassium channel

This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure. 

Inhibitors of the renal outer medullary potassium channel

Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

Process for preparing N-alkylated hydroxypyrimidinone compounds

An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1'-carbonyldiimidazole ('CDI') as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.

Process for the preparation of CGRP antagonist

Potassium salt of an HIV integrase inhibitor

This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.

Echinocandin process

There is disclosed a novel process for preparing aza cyclohexapeptides of the formula ##STR1## where all variables are defined herein.

Process for preparing certain aza cyclohexapeptides

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Metuchen, NJ, United States of America

Kevin Michael Belyk