Abbott Laboratories Corporation

James B Summers, Jr

Steven K Davidsen

George S Sheppard

Dee W Brooks

Douglas H Steinman

James H Holms

George M Carrera, Jr

Paul D May

Daisy Pireh

Bruce P Gunn

Denise E Guinn

James G Phillips

H Robin Heyman

Andrew O Stewart

Joseph F Dellaria, Jr

Alan S Florjancic

Jimmie L Moore

Karen E Rodriques

Michael B Martin

Lianhong Xu

Stephen W Fesik

Robert B Garland

Yan Guo

Michael L Curtin

Daniel Joseph Kerkman

Michael R Michaelides

Robert G Maki

Jonathan G Martin

Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.

Macrocyclic inhibitors of matrix metalloproteinases and TNF.alpha.

Compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof inhibit matrix metalloproteinases and TNF.alpha. secretion and are useful in the treatment of inflammatory disease states. Also disclosed are matrix metalloproteinases and TNF.alpha. secretion inhibiting compositions and a method for inhibiting matrix metalloproteinases and TNF.alpha. secretion.

Biphenyl hydroxamate inhibitors of matrix metalloproteinases

The present invention provides compounds of formula ##STR1## wherein Y is &gt;C.dbd.O or &gt;S(O).sub.t wherein t is 1 or 2 and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, rhinitis, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Indole piperazine platelet activating factor antagonists

The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, rhinitis, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Indole cyclohexyl platelet activating factor antagonists

The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Indole-3-carbonyl and indole-3-sulfonyl derivatives as platelet

The present invention relates to compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Platelet activating factor antagonists: imidazopyridine indoles

Platelet activating factor antagonists

Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.

Indole-,benzofuran-,and benzothiophene-containing

Compounds of the formula: ##STR1## wherein R.sub.1 is selected from (1) hydrogen; (2) --NR.sub.2 R.sub.3, --OR.sub.2 or --SR.sub.2 where R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, aryl and alkylaryl; and (3) optionally substituted C1-C8 alkyl, C2-C8 alkenyl, arylalkyl or cycloalkyl;

Lipoxygenase-inhibiting compounds derived from non-steroidal

Urea based lipoxygenase inhibiting compounds

Lipoxygenase inhibiting compounds

Benzoylphenyl derivatives of 2-(3-pyridinyl)-3-alkyl-4-thiazolidinecarboxamide, 2-(3-pyridinyl)-thiazolid-4-ylacetamide, 2-(3-pyridinyl)-4-dithiolanecarboxamide or 2-(3-pyridinyl)dithiolan-4-yl]urea-group are potent inhibitors of PAF and are useful in the treatment of PAF-related disorders including anaphylactic shock, respiratory distress syndrome, acute inflammation, delayed cellular immunity, parturtition, fetal lung maturation, and cellular differentiation.

Platelet activating antagonists

Benzoylphenyl derivatives of 2-(3-pyridinyl)-3-alkyl-4-thiazolidinecarboxamide, 2-(3-pyridinyl)-thiazolid-4-ylacetamide, 2-(3-pyridinyl)-4-dithiolanecarboxamide or 2-(3-pyridinyl)dithiolan-4-yl] urea are potent inhibitors of PAF and are useful in the treatment of PAF-related disorders including anaphylactic shock, respiratory distress syndrome, acute inflammation, delayed cellular immunity, parturtition, fetal lung maturation, and cellular differentiation.

Benzoylphenyl pyridinylthiazolidine compounds as platelet activating

Indole compounds substituted at the 1- or 3 position by a (pyrid-3 yl)thiazolid-4-yl)alkyl-, (pyrid-3-yl)thiazolid-4-oyl)-, (pyrid-3-yl)dithiolan-4-yl)alkyl- or (pyrid-3-yl) dithiolan-4-ol)- group are potent inhibitors of PAF and are useful in the treatment of PAF-related disorders including anaphylactic shock, respiratory distress syndrome, acute inflammation, delayed cellular immunity, parturtition, fetal lung maturation, and cellular differentiation.

Growing community of inventors

Libertyville, IL, United States of America

James B Summers, Jr