Merck + Co., Inc.

David Askin

Ralph P Volante

Paul J Reider

Kai Rossen

Ichiro Shinkai

Richard John Varsolona

Kan K Eng

Peter Emmanuel Maligres

Kenneth M Wells

Steven A Weissman

R Scott Hoerrner

Robert A Reamer

Todd K Jones

J Christopher McWilliams

Jess Sager

Marjorie See Waters

Jennifer A Cowen

Robert M Purick

Daisy Joe

Sander G Mills

Linghang Zhuang

Melissa S Egbertson

John S Wai

Thomas R Verhoeven

Zhijian Lu

Yuan Cheng

David M Tschaen

Ulf H Dolling

Kevin Tyler Chapman

James R Tata

Subharekha Raghavan

Michel M Chartrain

Philip J Pye

Kenneth M Ryan

Joseph Leslie Duffy

Nancy J Kevin

Thomas A Rano

Fengqi Zhang

Richard Desmond

Mark Cameron

Debra S Perlow

Joseph D Armstrong, Iii

Wei Han

Jaemoon Lee

Veena Upadhyay

Remy Angelaud

Steven J Cianciosi

Robert S Hoerrner

Brian Anthony Kirk

Fred Fleitz

Daniel E Petrillo

Danny Mancheno

Tracy Huening

Michael A Wallace

Rowena D Ruzek

Bruce S Foster

Stephanie Lewis

Thoa Hoang

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

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Process for the synthesis of (2S)-phenyl-3-piperidone

The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I):

Process for synthesizing biaryl inhibitors of farnesyl-protein transferase

The present invention is directed to a process for synthesizing substituted piperazinones, which are useful intermediates for making farnesyl-protein transferase inhibitors, using a Mitsunobu reaction.

Process for the synthesis of substituted piperazinones via Mitsunobu

The present invention is directed to a process for synthesizing 1,5-disubstituted imidazoles, which are useful in the preparation of farnesyl-protein transferase inhibitors.

Process for making 1,5-disubstituted imidazoles

This invention relates to a sulfate salt of an HIV protease inhibitor, Compound A, of formula: ##STR1## Compound A is useful in the treatment of AIDS, ARC or HIV infection in adults and children. Processes for making the sulfate salt of Compound A are also disclosed.

HIV protease inhibitor

The present invention is concerned with a novel process for the preparation of a compound of the formula: ##STR1## This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Process for the preparation of (S)-3-carbethoxy-3-benzylpiperidine

Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Process for making HIV protese inhibitors

A process for synthesizing the epoxide of the formula ##STR1## consists of, at a minimum, formation of a halohydrin from the allyl acetonide reactat, followed by base-induced cyclization, the epoxide product I being useful as an intermediate for the synthesis of inhibitors of renin or HIV protease or other proteases.

Process for making an epoxide

An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butyl-carboxamide, an intermediate for an HIV protease inhibitor.

Process for preparing

Process for making HIV protease inhibitors

A process for racemization of optically pure or enriched piperazine-2-tert-butylcarboxamide and its derivatives comprising reacting the optically pure or enriched piperazine compound with a racemizing agent selected from a strong base, an anhydrous metal salt or a carboxylic acid, in a solvent at a temperature range of between room temperature and 250.degree. C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.

A process is disclosed for making a chiral compound of the formula ##STR1## comprising reacting an epoxide compound of the formula ##STR2## and an amide of the formula ##STR3## in the presence of a strong base at a low temperature.

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Warren, NJ, United States of America

David Askin