Merck + Co., Inc.

Debra S Perlow

John S Wai

Peter D Williams

Ian M Bell

Neville J Anthony

Roger M Freidinger

Linghang Zhuang

Melissa S Egbertson

Steven D Young

Robert P Gomez

Mark W Embrey

Michelle A Sparks

Michelle Sparks Kuo

Mark G Bock

Daniel F Veber

Samuel L Graham

William C Lumma, Jr

S Jane deSolms

Anthony W Shaw

David Askin

Ulf H Dolling

Philip J Pye

Thorsten E Fisher

Jacob M Hoffman

R Scott Hoerrner

James P Guare

Lekhanh O Tran

Mark Cameron

H Marie Langford

Doug W Hobbs

Kenneth J Stauffer

Wei Han

Joseph M Pawluczyk

Jeffrey Y Melamed

Samson M Jolly

Jennifer J Bennett

Remy Angelaud

James B Hoffman

Danny Mancheno

Rowena D Ruzek

Bruce S Foster

Jill M Erb

Timothy W Funk

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

Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or 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 also described.

Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors

The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Inhibitors of prenyl-protein transferase

This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.

Tocolytic oxytocin receptor antagonists

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Inhibitors of farnesyl-protein transferase

This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery. A typical compound is as follows: ##STR1##

The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

Piperazinylcamphorsulfonyl oxytocin antagonists

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East Greenville, PA, United States of America

Debra S Perlow