Wyeth

American Home Products Corporation

Other

Eric Gould Gundersen

John Anthony Butera

Scott Christian Mayer

Hassan Mahmoud Elokdah

Lisa Marie Havran

Craig E Caufield

Robert E McDevitt

Alexander Greenfield

Alan Howard Katz

Joseph R Lennox

David LeRoy Crandall

Russell Graceffa

Russell F Graceffa

Dominick Anthony Quagliato

Douglas John Jenkins

Madelene M Antane

Geraldine Ruth McFarlane

Bradford H Hirth

David R Herbst

David Leroy Crandall

This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R, R, R, and Rare each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; Ris H, alkyl, perfluoroalkyl, aryl optionally substituted with R, alkanoyl, aroyl optionally substituted with R; Ris H, alkyl, alkylaryl, benzyl optionally substituted with R, alkanoyl, aroyl optionally substituted with R; Ris H, alkyl, alkylaryl, aryl optionally substituted with R; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SOH, POH, tetronic acid, etc.; Ris H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)

The present invention relates generally to substituted phenyl indoles and methods of using them, for example as PAI-1 inhibitors.

Substituted phenyl indoles

The present invention relates to substituted aryl oximes and methods of using them.

Substituted aryloximes

The present invention relates to substituted indole oximes and methods of using them.

Substituted indole oximes

This invention provides compounds of Formula I having the structureor a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

2,3,5-substituted biphenyls useful in the treatment of insulin resistance and hyperglycemia

This invention provides PAI-1 inhibiting compounds of Formula I:wherein: R, R, R, and Rare each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; Ris H, alkyl, perfluoroalkyl, aryl optionally substituted with R, alkanoyl, aroyl optionally substituted with R; Ris H, alkyl, alkylaryl, benzyl optionally substituted with R, alkanoyl, aroyl optionally substituted with R; Ris H, alkyl, alkylaryl, aryl optionally substituted with R; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SOH, POH, tetronic acid, etc.; Ris H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor Type-1 (PAI-1)

This invention provides compounds of Formula I having the structure

The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.6 is methyl, fluoro, chloro, or methoxy; or a pharmaceutically acceptable salt thereof, relax smooth muscles.

Substituted N-arylmethylamino derivatives of cyclobutene-3, 4-diones

The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.

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Royersford, PA, United States of America

Eric Gould Gundersen