Vertex Pharmaceuticals, Inc.

Cephalon, Inc.

Ignyta, Inc.

Sanofi Pharmaceuticals, Inc.

Mark A Ator

Roland Ellwood Dolle

Tina Morgan Ross

James M Rinker

Stanley J Schmidt

Denton W Hoyer

Robert L Hudkins

Joseph M Salvino

Prasad V Chaturvedula

Catherine P Prouty

Jasbir Singh

Irennegbe K Osifo

Eric P Lodge

Bruce D Dorsey

Lawrence I Kruse

Sankar Chatterjee

Thomas D Gordon

Derek D Dunn

Ron H Bihovsky

Teruna J Siahaan

Bruce A Ruggeri

Mohamed M Awad

Mohamed M A Awad

James Arthur Gainor

Thelma S Angeles

Barry Arnold Morgan

Mangeng M Cheng

Ron Bihovsky

This application describes the use of the compound (I) or a salt thereof, either alone or in combination with other therapeutically active agents, for the treatment of particular cancers, including any solid or hematological cancer in which AXL or c-Met is over-expressed. 

Methods of treating various cancers using an AXL/cMET inhibitor in combination with other agents

The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.

Multicyclic compounds and the use thereof

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof:wherein

4-pyridazinecarboxamides and esters as interleukin-1&#x3b2;  converting enzyme inhibitors

Pyridazines as interleukin-1&bgr; converting enzyme inhibitors

Disclosed are compounds, compositions, and methods for inhibiting interleukin-1&bgr; protease activity, wherein the compounds are &agr;-substituted methyl ketones having formula (I) as set forth herein. These compounds are inhibitors of IL-1&bgr; converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Peptide analogs as irreversible interleukin-1&bgr; protease inhibitors

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate;

Pyridazines as interleukin-1.beta. converting enzyme inhibitors

Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Peptide analogs as irreversible interleukin-1.beta. protease inhibitors

Peptides or peptides having an amino acid-like moiety in place of an amino acid moiety thereof immobilized on glass beads, especially controlled-pore glass beads, by a C-terminal .alpha.-carboxyl-.omega.-amino linker and .alpha.-silyl-.omega.-amino anchor, especially wherein the anchor has the structural formula

N-terminal-marked peptides immobilized on glass beads and method of

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Paoli, PA, United States of America

Mark A Ator