Merck + Co., Inc.

Kenneth J Stauffer

Philip E Sanderson

Terry A Lyle

Roger M Freidinger

Peter D Williams

Joseph P Vacca

Harold G Selnick

William C Lumma, Jr

James C Barrow

Thomas Joseph Tucker

Philippe G Nantermet

Stephen F Brady

Dong-Mei Feng

Donnette D Staas

Ian M Bell

Catherine M Wiscount

Lekhanh O Tran

Kenneth E Rittle

Debra S Perlow

Matthew M Morrissette

Mary Beth Young

Michelle A Sparks

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

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

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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Souderton, PA, United States of America

Kenneth J Stauffer