Janssen Pharmaceutica Nv

Richard William Connors

Dana L Johnson

Tianbao Lu

Kristi A Leonard

Maxwell David Cummings

Thomas P Markotan

Robert W Tuman

Richard Scott Alexander

Jan L Sechler

Robert A Galemmo

Anna C Maroney

Jeremy Mark Travins

Heather Rae Hufnagel

Ehab Khalil

Eddy Jean Edgard Freyne

Li Liu

Donald William Ludovici

Chih Yung Ho

Jean Fernand Armand Lacrampe

Steven J Coats

Bart L De Corte

Mark J Schulz

Peter Jacobus Johannes Buijnsters

Alan Richardson

Annette Cornelia Bakker

The invention is directed to triazolopyridazine compounds of Formula I: where R, R, R, R, R, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Triazolopyridazine compounds

Triazolopyridazines as kinase modulators

The invention is directed to acylhydrazones compounds of Formula I: where R, Rand A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Acylhydrazones as kinase modulators

The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases. 

Triazolopyrimidine derivatives

The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m, n, R, R, R, Rand Rare as defined herein, the use of such compounds as inhibitors of cyclin-dependent serine/threonine kinases (Cdks), as well as kinases and phosphatases involved in cell cycle regulation such as the tyrosine kinases Wee1, Mik1 and Myt1 or the tyrosine dephosphatases such as Cdc25 and Pyp3. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating cell proliferative disorders such as atherosclerosis, restenosis and cancer.

3-furanyl analogs of toxoflavine as kinase inhibitors

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Harleysville, PA, United States of America

Richard William Connors