Bristol-myers Squibb Compnay

Bristol-myers Company

Bristol-myers Squibb

Pierre Dextraze

Piyasena Hewawasam

Edward H Ruediger

Joseph P Yevich

Jie Chen

Gene G Kinney

Jean-Paul Daris

Steven Dworetzky

Ashvinikumar V Gavai

Dolatrai M Vyas

Yong-Jin Wu

Harold A Mastalerz

Valentin K Gribkoff

Katherine S Takaki

David W Smith

Guifen Zhang

Alexandre L'Heureux

Huan He

Marco Dodier

Jonas A Gylys

Li-Quang Sun

Carola Solomon

Philippe Lapointe

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Pyrrolotriazine compounds

Cinnamide derivatives as KCNQ potassium channel modulators

Fluoro oxindole derivatives as modulators if KCNQ potassium channels

There is provided a novel series of cis cyclopropane compounds of Formula I

Heterocyclic cis cyclopropane derivatives as melatonergic agents

A series of novel 5-cyclobutenedione derivatives of indolylalkylpiperazinyl pyridines and pyrimidines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1##

Antimigraine cyclobutenedione derivatives of indolylalkyl-pyridinyl and

A series of 5-halopyrimidin-2-ylpiperazinylalkyl derivatives having useful anti-ischemic properties for treatment and prevention of dirorders resulting from brain and/or spinal cord anoxia.

Agents for treatment of brain ischemia

This invention provides novel azetidinone intermediates having the formulas: ##STR1## wherein R.sup.1 is hydrogen, or a conventional hydroxy-protecting groups; R.sup.2, R.sup.4, and R.sup.5 are independently selected from the group consisting of hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; spirocycloalkyl having 3-6 carbon atoms; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; or various heterocyclic moieties; and R.sup.6 is methanesulfonyl or p-toluenesulfonyl; which are useful in the preparation of carbapenem antibiotics.

Synthesis of carbapenems using N-substituted azetidinones

A novel series of carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which n has a value of 1, 2 or 3; R.sup.5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroaraliphatic, heterocyclyl or heterocyclylaliphatic radical; and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle bonded to the group --S--(CH.sub.2)n--S-- via a ring carbon atom.

Carbapenems with quaternized heterothioalkylthio substitution at

A novel process is disclosed for converting known 3,4-disubstituted azetidinones to carbapenems. The process proceeds through novel N-substituted intermediates and then cyclizes to the 4-position of the azetidinone to form the carbapenem.

Synthesis of carbapenems using n-substituted azetidinones

Growing community of inventors

La Prairie, Canada

Pierre Dextraze