Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Glaxosmithkline LLC

Scott Howard Dickerson

Philip Anthony Harris

James Marvin Veal

Michael Luzzio

Robert Neil Hunter, Iii

William Pendergast

Karen Elizabeth Lackey

Lee Frederick Kuyper

Stephen Thomas Davis

Duncan Herrick Walker

Michael Robert Peel

Robert Ferone

Julius Vass Johnson

Francis Xavier Tavares

Alex Gregory Waterson

Stephen V Frye

David Harold Drewry

David Edward Uehling

Tara Renae Rheault

Kirk Stevens

Jeffrey Alan Stafford

Jerry Leroy Adams

Mui Cheung

Brian Edward Marron

Neil W Johnson

David Kendall Jung

Xinrong Tian

Marc W Andersen

George Adjabeng

David Norman Deaton

David John Cowan

Robert Walton McNutt, Jr

John Stellwagen

Joseph Wendell Wilson

Jeffrey M Ralph

Edgar Raymond Wood, Iii

Robert Carl Andrews

Kevin Kuntz

Robert Dale Hubbard

Jennifer Gabriel Badiang

Gregory Pacofsky

Douglas McCord Sammond

Michael David Gaul

Michael Howard Rabinowitz

Keith Hornberger

Holly Kathleen Emerson

Brian Wilson

Matthew Lee Brown

Kimberly Petrov

Robert N Hunter

Huiqiang Zhou

James Andrew Linn

Cassandra Gauthier

Michael John Reno

Gregory Schaaf

The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.

Benzene sulfonamide thiazole and oxazole compounds

The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors

The present invention relates to pyrazaolpyradazine derivatives that inhibit GSK3 (glycogen synthase kinase), pharmaceutical compositions containing these derivatives, and methods for their use in the treatment of disorder characterized by misregulation of GSK3.

Pyradazine compounds as GSK-3 inhibitors

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

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

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.

Substituted oxindole derivatives as tyrosine kinase inhibitors

Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R , R , R and R are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O) R wherein n is the integer 0, 1 or 2 and R is halo or alkyl or a group NR R wherein R and R are both hydrogen, a group NR R wherein R and R are the same or different and each is hydrogen or alkyl, a group OR wherein R is hydrogen or C of alkyl optionally substituted by halo; a C aliphatic group optionally substituted by a group OR or NR R wherein R and R are the same or different and each is hydrogen or alkyl; or two of R to R are linked together to form a benzo group, or one of R to R is a group X&mdash;Y&mdash;R wherein X is CH , NR , CO or S(O) and Y is CH , NR , O or S(O) , or X&mdash;Y is O, NR , &mdash;CH&boxH;CH&mdash; or N&boxH;N&mdash;, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.

Pharmaceutically active benzoquinazoline compounds

Oxindole derivatives, specifically pyrrolo&lsqb;3,2-f&rsqb;quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Oxindole derivatives

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 formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R,is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R,, R,, R,and R,are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O),R,wherein n is the integer 0, 1 or 2 and R,is halo or alkyl or a group NR,R,wherein R,and R,are both hydrogen, a group NR,R,wherein R,and R,are the same or different and each is hydrogen or alkyl, a group OR,wherein R,is hydrogen or C,of alkyl optionally substituted by halo; a C,aliphatic group optionally substituted by a group OR,or NR,R,wherein R,and R,are the same or different and each is hydrogen or alkyl; or two of R,to R,are linked together to form a benzo group, or one of R,to R,is a group X&mdash;Y&mdash;R,wherein X is CH,, NR,, CO or S(O),and Y is CH,, NR,, O or S(O),, or X&mdash;Y is O, NR,, &mdash;CH&boxH;CH&mdash; or N&boxH;N&mdash;, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.

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

A family of compounds having the general structural formula

Formamides as therapeutic agents

Growing community of inventors

Durham, NC, United States of America

Scott Howard Dickerson