Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Robert P Gomez

Neville J Anthony

Steven D Young

John S Wai

Theresa M Williams

Samuel L Graham

Gerald E Stokker

S Jane deSolms

Kelly Michelle Solinsky

John Howard Hutchinson

Christopher J Dinsmore

Mark W Embrey

Thorsten E Fisher

Jennifer J Bennett

Samson M Jolly

Ian M Bell

Melissa S Egbertson

Jeffrey M Bergman

Lekhanh O Tran

Debra S Perlow

Suzanne C MacTough

Chrisopher J Dinsmore

Michelle Sparks Kuo

George D Hartman

Linghang Zhuang

William C Lumma, Jr

Wasyl Halczenko

Thomas Joseph Tucker

Anthony W Shaw

Dai-Shi Su

Victor M Garsky

Terrence M Ciccarone

James P Guare

John T Sisko

Catherine M Wiscount

Robert M Tynebor

H Marie Langford

Jeffrey Y Melamed

John Jin Lim

Charles A Omer

Elizabeth A Giuliani

Timothy W Funk

John Lim

Heteroaromatic compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, R, R, R, R, R, R, R, R, Rand Rare defined herein. The compounds of Formula I and their pharmaceutically acceptable salts and prodrugs are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts and prodrugs can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

Non-nucleoside reverse transcriptase inhibitors

Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R, R, R, R, R, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

N-(Sulfonyloxybiarylmethyl) aminocyclopropanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Sulfonyl substituted n-(biarylmethyl) aminocyclopropanecarboxamides

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

Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds 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

Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds 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 intergrase inhibitors

The present invention is directed to compounds which inhibit farnesyl-protein transferas (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

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.

Biaryl substituted imidazole compounds useful as farnesyl-protein

Substituted imidazole compounds useful as farnesyl-protein transferase

The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Arylheteroaryl inhibitors of farnesyl-protein transferase

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Perkasie, PA, United States of America

Robert P Gomez