Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Duncan Herrick Walker

James Marvin Veal

Michael Luzzio

Philip Anthony Harris

Stephen Thomas Davis

Scott Howard Dickerson

Lee Frederick Kuyper

Robert Neil Hunter, Iii

Karen Elizabeth Lackey

Stephen V Frye

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

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Summit, NJ, United States of America

Duncan Herrick Walker