American Home Products Corporation

Wyeth

Kenneth L Kees

John H Musser

Diane Barbara Hauze

Jay Edward Wrobel

John P Yardley

Arie Zask

Anthony F Kreft, Iii

Jeffrey Claude Pelletier

Richard Dale Coghlan

Charles William Mann

James J Bicksler

Daniel Michael Green

John Francis Rogers, Jr

Joseph Theodore Lundquist, Iv

Winifred P Howse

Robert S Cheeseman

John Francis Mehlmann

Lloyd Michael Garrick

Compounds of Formula I, useful as Gonadotropin Releasing Hormone ('GnRH') (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists, are disclosed. 

Gonadotropin releasing hormone receptor antagonists

Bicyclic antagonists selective for the &agr;v&bgr;3 integrin

This invention provides compounds of Formula I having the structure

(2-Acylaminothiazole-4-yl)acetic acid derivative

This invention relates to compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 and R.sup.2 form a bond;

Unsaturated fatty acyl derivatives of 2-aminothiazoleacetic acid and

The compounds of the formulae: ##STR1## in which R.sup.1 is alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy of 1 to 6 carbon atoms, alkylthio, perfluoroalkylthio, alkylsulfinyl, alkylamino, halo, alkanoyl, 1-hydroxyalkyl or 1-(hydroxyimino) alkyl;

Trifluoromethyl substituted 1H-pyrazoles and derivatives thereof

The compound of the formula: ##STR1## in which the dotted lines represent two sites of unsaturation appropriately located based on the identity of R.sup.2, R.sup.3 and R.sup.4 and, R.sup.1 is alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, alkylthio, perfluoroalkylthio, alkylsulfinyl, alkylamino, halo, alkanoyl, 1-hydroxyalkyl or (1-hydroxyimino) alkyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or alkyl; R.sup.4 is hydrogen or alkyl; n is 0 or 1; or a pharmaceutically acceptable salt thereof, are antihyperglycemic agents.

Process for treating hyperglycemia using trifluoromethyl substituted

The compounds of the formula: ##STR1## in which the dotted lines represent optional unsaturation when n is 1 or 2 and X is CR.sup.5, Y is CR.sup.6 or X or Y are N; R.sup.1 is hydrogen, alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, alkyl, aryl or arylalkyl; R.sup.3 is alkyl, perfluoromethyl or alkoxy; R.sup.4 is halogen, alkyl or alkoxy; X is CR.sup.5, O, S or N, in which R.sup.5 is hydrogen, halogen, alkyl, or alkoxy; Y is CR.sup.6, O, S or N, in which R.sup.6 is hydrogen, halogen, alkyl or alkoxy; n is one of the integers 0, 1 or 2; m is one of the integers 0, 1, 2, or 3; or a pharmaceutically acceptable salt thereof, with the provisos that one of X and Y is O,S or N and R.sup.3 is other than alkyl when n and m are 0 and X and Y are O, are useful hypolglycemic agents in the treatment of non-insulin dependent diabetes melitus.

4-arylmethyl-5-alkyl-3h-pyrazol-3-ones

The compounds of the formula: ##STR1## in which the dotted lines represent optional unsaturation when X is CR.sup.5, Y is CR.sup.6 or X or Y are N; R.sup.1 is hydrogen, alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, alkyl, aryl or arylalkyl; R.sup.3 is alkyl, perfluoromethyl or alkoxy; R.sup.4 is halogen, alkyl or alkoxy; X is CR.sup.5, O, S or N, in which R.sup.5 is hydrogen, halogen, alkyl, or alkoxy; Y is CR.sup.6, O, S or N, in which R.sup.6 is hydrogen, halogen, alkyl or alkoxy; n is one of the integers 0, 1 or 2; m is one of the integers 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof, are useful hypoglycemic agents in the treatment of non-insulin dependent diabetes mellitus.

4-arylmethyl-5-alkyl-3H-pyrazol-3-ones and hypoglycemic use

Compounds of the formula: ##STR1## in which R is a substituted or unsubstituted monocyclic or bicyclic alkyl group containing from 3 to 8 ring carbon atoms, wherein any substituent is alkyl of 1 to 3 carbon atoms, oxo, hydroxy, carboxy or when the hydroxy and carboxy substituents taken together they form a 1,3-carbonyloxy lactone ring closed structure;

Tetrazoles and their use as hypoglycemic agents

Compounds of the formula: ##STR1## where R is hydrogen or A--(CF.sub.2).sub.m --CH.sub.2 --; A is --F or --H; n is an integer from 1 to 10, inclusive; m is an integer from 0 to 9, inclusive; p is an integer from 0 to 4, inclusive; and Y is hydrogen, halo, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or hydroxy; or a pharmaceutically acceptable salt thereof. The compounds are useful as anti-hyperglycemic and anti-hyperinsulinemic agents.

N-(1H-tetrazol-5-yl-alkylphenyl)polyfluoroalkanamides

There are disclosed compounds having the formula ##STR1## wherein X is CR or N when n=1; or

Novel substituted naphthyloxymethyl quinoline derivatives as

The compounds: ##STR1## in which R is hydrogen, lower alkyl, phenyl or benzyl, and R.sup.2 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, are useful hypoglycemic and hypoinsulinemic agents for the treatment of diabetes mellitus and cardiovascular disease states involved in elevated insulin levels such as atherosclerosis.

Hypoglycemic thiazolidinediones

There are disclosed compounds of the formula ##STR1## wherein X is OR.sup.2, SR.sup.2, N(R.sup.2).sub.2 or halo;

Growing community of inventors

West Chester, PA, United States of America

Kenneth L Kees