American Cyanamid Company

Wyeth

Other

Minu D Dutia

Jonathan D Bloom

Thomas H Claus

Dan Maarten Berger

Vern G DeVries

Jo A Dolan

Joseph William Epstein

Rolf Paul

Dennis W Powell

Gary H Birnberg

William A Hallett

Allan Wissner

Diane H Boschelli

Hwei-Ru Tsou

Nan Zhang

Dennis William Powell

Biqi Wu

Fei Ye

Elwood Eugene Largis

Frenel Fils DeMorin

Gary E Walker

This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

Tricyclic protein kinase inhibitors

Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.

MDR reversal agents

The invention is antiobesity/antidiabetes beta-3 agonists of the formula: ##STR1## wherein Ar, X, R.sub.2, R.sub.3, Y and n are as defined in the specification.

.beta..sub.3 -adrenergic agents, benzodioxole dicarboxylates and their

The invention is antiobesity/antidiabetic/beta-3 agonists of the formula ##STR1## wherein the substituents R.sub.o, R.sub.1, R.sub.4, R.sub.4 ', R.sub.5, R.sub.6 or n are as defined in the specification.

Aminocycloalkanobenzodioxoles as beta-3 selective adrenergic agents

.beta..sub.3 -adrenergic agents benzodioxole dicarboxylates and their

The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.

Substituted 5-(2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodioxoles

A process is disclosed for obtaining the R,R isomer of: ##STR1## wherein R.sub.1 and R.sub.2 may be one or more groups which may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxy, halogen, trifluoromethyl, carboxy, hydroxyalkyl, alkoxycarbonyl, C.sub.1 to C.sub.4 thioalkyl, sulfonyl and sulfinyl; X is a divalent radical consisting of ##STR2## wherein R' is hydrogen; R.sub.2 and R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1 to C.sub.4 alkyl; R.sub.5 and R.sub.6 are selected from the group consisting of hydrogen, carboxy, alkoxycarbonyl, hydroxymethyl, --CH.sub.2 OCH.sub.2 COOR.sub.7 and --CH.sub.2 OCH.sub.2 CH.sub.2 OR.sub.7 where R.sub.7 is hydrogen or C.sub.1 to .sub.4 alkyl; except that R.sub.5 and R.sub.6 may not both be hydrogen; and the asterisks denote asymmetric carbon atoms; said process comprising the steps of:

Substituted 5-(2-(2-aryl-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxoles

New thioester and ester, amide and ketone isostere analogs of oleoyl coenzyme A, useful as antiatherosclerotic agents, are provided. The compounds have the formula: ##STR1## wherein A is selected from the group consisting of ##STR2## Y is selected from the group consisting of --S--, --O--, --NH-- and (--CH.sub.2 --).sub.n wherein n=1 to 4; and Z is selected from the group consisting of alkyl (C.sub.1 -C.sub.6), ##STR3## wherein R=Hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 acyl, and ##STR4##

Simplified thioester and isostere analogs of oleoyl coenzyme A as

Method of increasing lean meat in edible animals

Growing community of inventors

West Nyack, NY, United States of America

Minu D Dutia