Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Robert Neil Hunter, Iii

Philip Anthony Harris

Scott Howard Dickerson

James Marvin Veal

Michael Luzzio

Karen Elizabeth Lackey

Stephen Thomas Davis

Lee Frederick Kuyper

Duncan Herrick Walker

Stephen V Frye

Michael Robert Peel

Jeffrey Alan Stafford

Mui Cheung

David Harold Drewry

Robert Walton McNutt, Jr

Gregory Pacofsky

Matthew Lee Brown

David Kendall Jung

Cassandra Gauthier

Benzimidazolyl-pyridine derivatives, which are useful as SGK-1 inhibitors are described herein. The described invention also includes methods of making such benzimidazolyl-pyridine derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate SGK-1 activity.

Chemical compounds

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

Compounds of formula (I): wherein X is N, CH, CCF, or C(Caliphatic); Ris sulfonic acid, Caliphatic-sulfonyl, sulfonyl-Caliphatic, Caliphatic-sulfonyl-Caliphatic, Caliphatic-amino, R-sulfonyl, Rsulfonyl-Caliphatic, R-aminosulfonyl, R-aminosulfonyl-Caliphatic, R-sulfonylamino, R-sulfonylamino-Caliphatic, aminosulfonylamino, di-Caliphatic amino, di-Caliphatic aminocarbonyl, di-Caliphatic aminosulfonyl, di-Caliphatic amino, di-Caliphatic aminocarbonyl, di-Caliphatic aminosulfonyl-Caliphatic, (R)-Arylamino, (R)-Arylsulfonyl, (R)-Aryl-aminosulfonyl, (R)-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, Ris hydrogen; and further wherein Rand Rare optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects

Compounds of formula (I): wherein X is N, CH, CCF , or C(C aliphatic); R is sulfonic acid, C aliphatic-sulfonyl, sulfonyl-C aliphatic, C aliphatic-sulfonyl-C aliphatic, C aliphatic-amino, R -sulfonyl, R sulfonyl-C aliphatic, R -aminosulfonyl, R -aminosulfonyl-C aliphatic, R -sulfonylamino, R -sulfonylamino-C aliphatic, aminosulfonylamino, di-C aliphatic amino, di-C aliphatic aminocarbonyl, di-C aliphatic aminosulfonyl, di-C aliphatic amino, di-C aliphatic aminocarbonyl, di-C aliphatic aminosulfonyl-C aliphatic, (R ) -Arylamino, (R ) -Arylsulfonyl, (R ) -Aryl-aminosulfonyl, (R ) -Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R is hydrogen; and further wherein R and R are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors

The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of such kinases as well as protecting a patient undergoing chemotherapy from chemotherapy induced alopecia.

Substituted oxidole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors

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

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Durham, NC, United States of America

Robert Neil Hunter, Iii