American Home Products Corporation

Ayerst, Mckenna & Harrison, Inc.

Christopher A Demerson

Leslie G Humber

Ivo L Jirkovsky

Thomas A Dobson

Andre A Asselin

Dominick Mobilio

Alan Howard Katz

Jean-Marie Ferland

George Santroch

John H Musser

Amedeo A Failli

Anthony F Kreft, Iii

Nedumparambil A Abraham

James Albert Nelson

Uresh Shantilal Shah

Adolf H Philipp

Joseph P Sabatucci

Amadeo A Failli

Wilbur Lippman

This invention relates to substituted indole derivatives possessing lipoxygenase inhibitory, phospholipase A.sub.2 inhibitory and leukotriene antagonist activity, which are useful as anti-inflammatory, antiallergic and cytoprotective agents.

Substituted indole-, indene-, pyranoindole- and

There are disclosed compounds of the formula

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at positions 5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

Substituted 1,3,4,9-tetrahydropyrano(3,4-b)indole-1-acetic acids

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing substituents in position 1-,5-,6-, 7- and 8- are disclosed. The derivatives are useful anti-inflammatory and/or analgesic agents. Methods for their preparation and use are also disclosed.

Substituted-8-alkenyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic

Production of indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at positions 5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

Production of substituted 1,3,4,9-tetrahydropyrano(3,4-B)indole-1-acetic

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing substituents in position 1-, 5-, 6-, 7- and 8- are disclosed. The derivatives are useful anti-inflammatory and/or analgesic agents. Methods for their preparation and use are also disclosed.

Substituted-8-alkenyl-1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1,5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

Substituted 1,3,4,9-tetrahydropyrano[3,4,-b]indole-1-acetic acids,

Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation. The compounds are useful analgesic and anti-inflammatory agents.

Production of substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid

Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful analgesic and antiinflammatory agents.

Process for preparing substituted

Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid

Substituted 1,3,4,9-tetrahydropyrano(3,4-B)indole-1-acetic acids

Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives,

Mixtures of racemic (+)pyrano[3,4-b]indole-1-acetic acids are resolved with (-)-borneol to obtain the substantially pure (+) and (-)-enantiomers. The resolution involves the formation of a mixture of the diastereoisomeric pyrano[3,4-b]indole-1-acetic acid, (-)-borneol esters, separation of the diastereoisomeric esters, and hydrolysis of the latter esters.

Process for the resolution of pyrano[3,4-b]indole-1-acetic acids

A process for preparing 1,8-diethyl-1,3,4,9-tetrahydro[3,4-b]-indole-1-acetic acid (etodolac) is disclosed. Etodolac is a useful antiinflammatory and analgesic agent.

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Montreal, Canada

Christopher A Demerson