Merck + Co., Inc.

Roger M Freidinger

Mark G Bock

Ben E Evans

Daniel F Veber

Peter D Williams

Robert M DiPardo

Douglas J Pettibone

Harold G Selnick

Ian M Bell

Michael A Patane

Terry A Lyle

Kenneth J Stauffer

Michelle A Sparks

David A Claremon

Joseph P Vacca

Nigel J Liverton

William C Lumma, Jr

Otto D Hensens

Thomas Joseph Tucker

Philip E Sanderson

Stephen F Brady

Dong-Mei Feng

Paul S Anderson

Debra S Perlow

Cheryl D Schwartz

Garry R Smith

Doug W Hobbs

Rose Ann Ponticello

John J Baldwin

George D Hartman

Roger D Tung

Richard L Tolman

David C Remy

Deborah L Zink

Ruth F Nutt

James C Barrow

Philippe G Nantermet

Joshua S Boger

Jerrold M Liesch

John Hannah

Victor M Garsky

Jeffrey M Bergman

Raymond S Chang

Yiu-kuen T Lam

James P Guare

Steven M Pitzenberger

Michael A Goetz

Kevin F Gilbert

Thomas M Connolly

Lawrence R Koupal

Joseph M Pawluczyk

George F Lundell

Randall C Newton

Richard Saperstein

James B Hoffman

Robert B Stein

Thrombin receptor antagonists

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

Alpha 1a adrenergic receptor antagonists

This invention relates to certain novel piperazine 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.

Piperazine oxytocin receptor antagonists

Imidazolinobenzodiazepines

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##

Piperidine and hexahydropyridazine thrombin inhibitors

This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.

N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides

N-(2,4-dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-yl)-3-amides

Compounds of the formula ##STR1## X is --O--, --NH-- and --NR.sup.8 --; Y is --CH.sub.2 --, --CHR.sup.8 -- and --C(R.sup.8).sub.2 --; R.sup.1 is camphor-10-yl, C.sub.1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R.sup.4, and unsubstituted or substituted phenyl where the substituents on phenyl are R.sup.5, R.sup.6 and R.sup.7 ; R.sup.2 is hydrogen, C.sub.1-5 alkoxy, C.sub.1-5 alkyl, amino, C.sub.1-5 alkylcarbonylamino, nitro or halogen; R.sup.3 is hydrogen, C.sub.1-5 alkoxycarbonyl, cyano or carbamoyl; R.sup.4 is one to two of hydrogen, oxo, hydroxy, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonylamino-C.sub.1-5 alkyl and amino-C.sub.1-5 alkyl; R.sup.5, R.sup.6 are each independently selected from hydrogen, halogen, C.sub.1-5 alkyl, hydroxyl and C.sub.1-5 alkoxy; R.sup.7 is ##STR2## W is CO or SO.sub.2 ; and m is an integer from 0 to 1. Such compounds as useful as oxytocin and vasopressin receptor antagonists.

Benzoxazinone and benzopyrimidinone piperidinyl tocolytic oxytocin

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Alpha-1a adrenergic receptor antagonists

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

Pyrrolidine thrombin inhibitors

Imidazobenzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

Antiarrhythmic benzodiazepines

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Lansdale, PA, United States of America

Roger M Freidinger