Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Glaxo Inc.

Michael Robert Peel

Philip Anthony Harris

Mui Cheung

David Kendall Jung

Brian Alvin Johns

Karen Elizabeth Lackey

Stanley Dawes Chamberlain

Kristjan S Gudmundsson

Scott Howard Dickerson

James Marvin Veal

Robert Walton McNutt, Jr

Robert Neil Hunter, Iii

Michael John Alberti

Jennifer Gabriel Badiang

Daniel D Sternbach

Jennifer Badiang Stanford

Jeffrey Alan Stafford

Michael Luzzio

Francis Xavier Tavares

Lee Frederick Kuyper

Edgar Raymond Wood, Iii

Tara Renae Rheault

M Ross Johnson

Jeffrey M Besterman

Michael G Evans

Gregory Pacofsky

Kirk Stevens

Robert N Hunter

F Leslie Boyd

Matthew Lee Brown

Michael John Reno

Cassandra Gauthier

Connie Jo Sexton

Fused pyradazine derivatives which are usefule as CDK inhibitors are described herein. The described invention alos includes methods of making such fused pyradazine derivatives as wells as methods of using the same in the treatment of hyperproliferative diseases.

Pyrazolopyridazine derivatives

Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

1,3-Oxazole compounds for the treatment of cancer

The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

Pyrazolopyridinyl pyrimidine therapeutic compounds

Pyrazolopyridines, process for their preparation and use as therapeutic compounds

Pyralopyridines, process for their preparation and use as therapeutic compounds

The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.

Oxindole derivatives

Compounds of general formula (I) wherein: R,is H or optionally joined with R,to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R,and R,are independently H, HET, aryl, C,aliphatic, CN, NO,, halogen, R,, &mdash;OR,, &mdash;SR,, &mdash;S(O)R,, &mdash;SO,R,, &mdash;NR,R,, &mdash;NR,R,, &mdash;NR,COR,, &mdash;NR,CO,R,, &mdash;NR,CONR,R,, &mdash;NO,SO,R,, &mdash;NR,C(NR,)NHR,, &mdash;COR,, &mdash;CO,R,, &mdash;CONR,R,, &mdash;SO,NR,R,, &mdash;OCONR,R,, C(NR,)NR,R,, R,and R,are independently halogen, CN, NO,, &mdash;CONR,R,, &mdash;SO,NR,R,, &mdash;NR,R,, or &mdash;OR,, where R,and R,are as defined below; R,is OH, NHSO,R,or NHCOCF,; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.

Benzylidene-1,3-dihydro-indol-2-one derivatives a receptor tyrosine kinase inhibitors, particularly of Raf kinases

The present invention relates to water soluble, camptothecin derivatives of formula (I). ##STR1## wherein A represents a moiety of the formula (IIA), (IIB) or (IIC): ##STR2## X is selected from the group consisting of alkyl, aryl, (CH.sub.2).sub.m OR.sup.1, (CH.sub.2).sub.m SR.sup.1 and (CH.sub.2).sub.m NR.sup.1 R.sup.2 wherein m is an integer of 0 to 6, and R.sup.1 and R.sup.2 are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.

Water soluble camptothecin derivatives

This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-amino-1,9-dihydro-9[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-p urin-6-one, an antiviral agent.

Process for the synthesis of cyclopentene derivatives of purines

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Durham, NC, United States of America

Michael Robert Peel