Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Pamela Loreen Rossman

Sung-Sau So

Kin-Chun Thomas Luk

Yi Heng Chen

Paul Gillespie

Apostolos Dermatakis

Kevin W Anderson

Jefferson Wright Tilley

Dennis D Keith

Stefan Scheiblich

Manfred Weigele

Robert Alan Goodnow, Jr

Nancy-Ellen Haynes

Nader Fotouhi

Jin-Jun Liu

Norman Kong

Xin-Jie Chu

Sherrie Lynn Pietranico-Cole

Kevin Richard Guertin

Christophe Michoud

Kshitij Chhabilbhai Thakkar

David Joseph Bartkovitz

Nathan Robert Scott

Lida Qi

Nicholas J S Huby

John Lawson Roberts

Harry A Albrecht

Marek Michal Kabat

Qiang Zhang

Frederick M Konzelmann

Michael Paul Myers

Yi Chen

Kevin William DrANDERSON

Kevin William Anderson

The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.

Sultam derivatives

There are provided compounds of the formula wherein R, R, R, X, ring A and ring B are as described. The compounds exhibit anticancer properties.

Substituted thieno[3,2-C]pyridine carboxylic acid derivatives

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.

Adamantyl-pyrazole carboxamides as inhibitors of 11&#x3b2;-hdroxysteroid dehydrogenase

Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Pyrimido compounds having antiproliferative activity

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

There are presented antibacterial cephalosporine having broad antimicrobial activity, having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group: R.sub.1 represents a substituted piperazinyl group of formula ##STR2## or a substituted pyrrolidinylamino group of formula ##STR3## or a substituted pyrrolidinylmethylamino group of formula ##STR4## where the piperazinyl or pyrrolidinyl group may be optionally substituted with one or more lower alkyl groups, and where Q represents a substituted quinolinyl or naphthyridinyl group: R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group: and m is 0, 1 or 2, but preferably 0; as well as the corresponding readily hydrolyzable esters. pharmaceutically acceptable salts and hydrates of these compounds.

Antibacterial cephalosporin compounds

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Nutley, NJ, United States of America

Pamela Loreen Rossman