Syntex (u.s.a.) Inc.

Genelabs Technologies, Inc.

Other

Joseph M Muchowski

Robert J Greenhouse

Angel Guzman

Arthur F Kluge

Robin D Clark

Peter H Nelson

Jack Ackrell

Lawrence Emerson Fisher

Natalia Dyatkina

Jacob Berger

Christopher Don Roberts

Alexander Khorlin

John O Gardner

Dong-Fang Shi

Roberto P Rosenkranz

Janos Botyanszki

Mark Douglas Velligan

Wentao Zhang

Sebastian Johannes Reinhard Liehr

Deborah L McClelland

Fang-Ting Chiu

John H Fried

Jurg R Pfister

Anthony C Allison

Elsie M Eugui

John M Young

In-Seop Cho

D V Murthy

Edvige Galeazzi

Michael C Venuti

Stefan H Unger

L David Waterbury

Klaus K Weinhardt

Joan Marie Caroon

William L Smith

Tsung-tee Li

Richard M Eglen

Tsung-Tee Li

Maria T Lara

Joan Huguet

Ruth S Romero

Fidencio Franco

Armando C Castaneda

The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.

Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity

The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I):Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.

Compounds possessing antibacterial, antifungal or antitumor activity

.alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

Serotonergic alpha-oxoacetamides

Compounds of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;

Bis(benzylpyrrolidine) derivatives useful for treating congestive heart

Compound of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;

Bis(benzylpyrrolidine) derivatives as dopamine agonists

Dopamine agonist compounds disclosed are useful in treating hypertension and congestive heart failure in mammals. The compounds have the following general formula (I) ##STR1## wherein: X is nitrogen or CH;

Benzylpyrrolidine derivatives as dopamine agonists

5-Aroyl-2,3-dihydro-1H-pyrrolizine-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-aroylpyrroles. Hydrolysis and mono-decarboxylation of these compounds affords ketorolac and related compounds.

Process for preparing

This invention is directed to compounds of formula (I): ##STR1## wherein R.sup.1 is thiocyano, --CH.sub.2 CN, --NH.sub.2, --NHR.sup.5, or --CH.sub.2 OR.sup.5 where R.sup.5 is lower alkyl;

Pyrrolo(1,2-a)pyrazines as inhibitors of gastric acid secretion

5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-halopyrroles. Hydrolysis and .beta.-decarboxylation of these compounds affords ketorolac and related compounds.

Intermediates for preparing

A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: A is oxygen or sulfur;

Mycophenolic acid derivatives in the treatment of rheumatoid arthritis

3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkanoyl]-pyrroles and their de-oxy analogs, for example, 3-(3,5-di-t-butyl-4-hydroxybenzyl)pyrrole, 2-chloro-4-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole, 3-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole and 3-[2-(3,5-di-t-butyl-4-hydroxyphenyl)-1-oxoethyl]pyrrole, have high pharmacological potency as anti-inflammatory, analgesic and antipyretic agents.

3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkyl]pyrroles, and

Novel 13,14-dihydroprostaglandin derivatives of the formula ##STR1## wherein: m is 1 or 3;

13,14-dihydroprostaglandin C-type derivatives

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Sunnyvale, CA, United States of America

Joseph M Muchowski