Merck + Co., Inc.

Terry A Lyle

Philip E Sanderson

Donnette D Staas

Peter D Williams

Joseph P Vacca

Bruce D Dorsey

Matthew M Morrissette

Kenneth J Stauffer

Roger M Freidinger

Craig Alan Coburn

William C Lumma, Jr

John S Wai

Thomas Joseph Tucker

Stephen F Brady

Thorsten E Fisher

Lekhanh O Tran

Catherine M Wiscount

Harold G Selnick

Matthew G Stanton

Linghang Zhuang

Melissa S Egbertson

Ruth F Nutt

James C Barrow

Philippe G Nantermet

Mark W Embrey

Dong-Mei Feng

Adel M Naylor-Olsen

Boyoung Kim

Daniel F Veber

Theresa M Williams

Christopher S Burgey

Wayne J Thompson

Richard John Varsolona

Lou Anne Neilson

Susan F Britcher

Kenneth E Rittle

Sandor L Varga

Mary Beth Young

Richard Saperstein

Theresa R Lamanec

Kyle A Robinson

Kelly L Savage

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z, R, R, R, R, R, R, R, Rand Rare 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

Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R, R, R, R, R, Rand Rare 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. 

Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R, R, R, R, R, R, Rand Rare 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. 

Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)&#x2014;N(R)CH(R)&#x2014; wherein the nitrogen atom is attached to R, and Rand Rare independently selected from the group consisting of hydrogen, Ccycloalkyl, and Calkyl, or 2) wherein the nitrogen atom is attached to R, and m is 0, 1, or 2 

Thrombin inhibitors

Pyrazinone thrombin inhibitors

A compound which inhibits human thrombin and where has the structure ##STR1##

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##

Pyridinone thrombin inhibitors

Piperidine and hexahydropyridazine thrombin inhibitors

Compounds of the invention have the following structure: ##STR1## for example ##STR2## These compounds inhibit thrombin and associated thrombosis.

Pyrrolidine thrombin inhibitors

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Lederach, PA, United States of America

Terry A Lyle