Bristol-myers Squibb Compnay

Bristol-myers Company

Bristol-myers Squibb

Ivo Monkovic

David Willner

Takushi Kaneko

Robert S Greenfield

Gary R Braslawsky

Graham Johnson

Ronnie R Crenshaw

Graham S Poindexter

Jaswant S Gidda

Michael R Kozlowski

Charles P Sloan

Marc A Bruce

Karen LeBoulluec

Ramakrishna Seethala

Lotte Wang

A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Dihydropyridine npy antagonists: piperazine derivatives

The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-substituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the preferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.

Bifunctional linking compounds, conjugates and methods for their

This invention relates to a compound of formula I ##STR1## wherein p is 1 to 3;

Dibenz[b,f][1,4]oxazepin-11(10H)-ones for multidrug resistance reversing

The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-subhstituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the perferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.

Novel substituted benzamides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.

Pharmacologically active substituted benzamides

The present invention provides a method for treating gastrointestinal motility disorders and thiadiazole oxide compounds for use in the method.

Thiadiazole oxides for treating gastrointestinal motility disorders

Anti-emetic quinuclidinyl benzamides

Histamine H.sub.2 -antagonists of the formula: ##STR1## wherein m is an integer of from 0 to 2 inclusive;

Growing community of inventors

Durham, CT, United States of America

Ivo Monkovic