American Home Products Corporation

Wyeth

Other

Thomas Joseph Commons

Donald P Strike

Richard Eric Mewshaw

Susan Christman

Richard Page Woodworth, Jr

Andrew Fensome

Casey Cameron McComas

Gavin David Heffernan

Edward George Melenski

Michael Byron Webb

Michael Anthony Marella

Christa M LaClair

Ronald Charles Bernotas

Hassan Mahmoud Elokdah

Eugene John Trybulski

John R Potoski

David LeRoy Crandall

Susan Christman Croce

Jerauld S Skotnicki

Douglas John Jenkins

Christa L Musial

Richard Page Woodworth

The present invention relates to oxazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.

Oxazolo-naphthyl acids

Compounds of the following structure are described: wherein R-R, R, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Imidazolidin-2-one derivatives useful as PR modulators

Compounds of the following structure are described: wherein R-R, m, V, W, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Oxazolidine derivatives as PR modulators

Compounds of the following structure are described: wherein R, R, R, R, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Oxazolidone derivatives as PR modulators

Compounds of the following structure are described: wherein R-R, R, m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Tricyclic oxazolidone derivatives useful as PR modulators

The present invention relates to thiazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.

Thiazolo-naphthyl acids

Compounds of the following structure are described: wherein R-R, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Oxazinan-2-one derivatives useful as PR modulators

The present invention relates generally to substituted biphenyloxy acids (such as 4'-aryl-amido-biphenyl-4(3)-yloxy-acids and 4&#x2032;-aryl-amidomethyl-biphenyl-4(3)-yloxy-acids) and methods of using them, for example, as PAI-1 inhibitors.

Biphenyloxy-acids

The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.

Pyrrolo-naphthyl acids and methods for using them

6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)

Elevation of HDL cholesterol by 4-&lsqb;(aminothioxomethyl)-hydrazono&rsqb;-N-(substituted)-4-arylbutanamides

Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the &ldquo;good&rdquo; cholesterol and as such may be useful for treating diseases such as atherosclerosis. These compounds are represented by the formula

Elevation of HDL cholesterol by 4-&lsqb;(Aminothioxomethyl)-hydrazono&rsqb;-N-(substituted)-4-arylbutanamides

This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;

Elevation of HDL cholesterol by N-[2-[(aminothioxomethyl)

This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;

Elevation of HDL cholesterol by N-[4-[(aminothioxomethyl)

This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.10 alkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, furanyl, pyridinyl or thienyl, and Ar.sup.1 is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; and Ar is phenyl, napthyl, furanyl, pyridinyl or thienyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.

Growing community of inventors

Wayne, PA, United States of America

Thomas Joseph Commons