Bayer Aktiengesellschaft

Bayer Corporation

Osi Pharmaceuticals, Inc.

Bayer Pharmaceuticals Corporation

Pfizer Corporation

Richard D Connell

Hilmar Bischoff

Dirk Denzer

Siegfried Goldmann

Stefan Wohlfeil

Martin Beuck

Ulrich E Muller

Rudi Grutzmann

Timothy G Lease

Ulrich M&uuml;ller

Stefan Lohmer

Rudi Gr&uuml;tzmann

Gaetan H Ladouceur

Anke Domdey-Bette

Jeremy L Baryza

Martin H Osterhout

Klaus-Helmut Mohrs

Ann-Marie Campbell

Siegfried Raddatz

Michael Matzke

Timothy Norris

Jeffrey W Raggon

James H Cook, Ii

James Dale Moyer

Shama Kajiji

Sandra Leta Silberman

Karen J Ferrante

Michael J Morin

Barbara A Foster

Rolf Angerbauer

Matthias Muller-Gliemann

John Charles Kath

Ulrich Niewohner

Samit Kumar Bhattacharya

Goss S Kauffman

Jinshan Michael Chen

Joel Morris

Ulrich Müller

Blaise S Lippa

Rudi Gru Tzmann

Rudi Grützmann

The invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R, R, R, R, N, Z, A, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Substituted heterocylces for the treatment of abnormal cell growth

A method of monotherapy for a subject suffering from abnormal cell growth expressing the epidermal growth factor receptor (EGFR) which comprises orally administering to the subject a therapeutically effective amount of a crystalline polymorph of the hydrochloride salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine so as to treat the subject.

Treating abnormal cell growth with a stable polymorph of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride

This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.

Sulfonamide substituted chroman derivatives

The present invention relates to a stable crystalline form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride designated the B polymorph, its production in essentially pure form, and its use. The invention also relates to the pharmaceutical compositions containing the stable polymorph B form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride, as well other forms of the compound, and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.

Stable polymorph on N-(3-ethynylphenyl)-6, 7-bis (2methoxyethoxy)-4-quinazolinamine hydrochloride, methods of production, and pharmaceutical uses thereof

Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Cycloalkano-indole and -azaindole derivatives

This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.

Carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists

Cycloalcanoindole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with anmines. The cycloahloanindole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Amide derivatives and methods of administering the compositions to mammals to treat disorders such as obesity that are mediated by NPY and especially those mediated by NPY via the Y5 receptor.

Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists

The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.

Hetero-linked phenylglycinolamides

The heterocyclically substituted phenylglycinolamides are obtained by reaction of heterocyclically substituted phenylacetic acids with appropriate phenylglycinols. The heterocyclically substituted phenylglycinolamides are suitable as active compounds in medicaments, in particular in antiatherosclerotically active medicaments.

Heterocyclically substituted phenylglycinolamides

Cycloakano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carbonylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

&agr;-alkoxy and &agr;-thioalkoxyamide compositions and methods of administering the compositions to mammals to treat disorders such as obesity that are mediated by NPY and especially those mediated by NPY via the Y5 receptor.

NPY5 receptor antagonists and methods for using same

The indolyl-substituted phenylacetic acid derivatives are prepared by reacting the corresponding phenylacetic acids with the required amines. The indolyl-substituted phenylacetic acid derivatives are suitable as active compounds in medicaments, in particular in antiarteriosclerotic medicaments.

Indolyl-substituted phenylacetic acid derivatives

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Trumbull, CT, United States of America

Richard D Connell