Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Versi Group, LLC

Delta Pharmaceuticals Ltd.

Robert Walton McNutt, Jr

Karen Elizabeth Lackey

Kwen-Jen Chang

Lee Frederick Kuyper

William Pendergast

Philip Anthony Harris

Michael Robert Peel

Grady Evan Boswell

Dulce Garrido Bubacz

Ann O Davis

Kestutis P Biciunas

Klim King

Kimberley Caroline Glennon

Mark Allan Collins

James Marvin Veal

Scott Howard Dickerson

Robert Neil Hunter, Iii

Edgar Raymond Wood, Iii

Shyi-Tai Jan

Robert N Hunter

Shyi-Tan Jan

David Kendall Jung

Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.

Delta opioid receptor agonist compounds

Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.

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

3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors

The present invention relates generally to novel amine 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 general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. 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 tumor-related angiogenesis.

3-(anilinomethylene) oxindoles

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 method for the treatment or prophylaxis of one or more conditions or disorders selected from the group consisting of physiological pain, diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depressioysema, apnea, cognitive disorders and gastrointestinal disorders, comprising administration to a subject in need of such treatment or prophylaxis, of a diarylmethylpiperazine or piperidine opioid compound.

Opioid diarylmethylpiperazines and piperidines

Opioid diarylmethylpiperazines and piperdines

Growing community of inventors

Durham, NC, United States of America

Robert Walton McNutt, Jr