Bristol-myers Squibb Compnay

Methylgene, Inc.

Carl Thibault

Rejean Ruel

John E Macor

R Michael Lawrence

Edward H Ruediger

Daniel Delorme

Graham S Poindexter

Guixue Yu

George C Morton

Timothy F Herpin

Elie Abou-Khalil

Alexandre L'Heureux

Rico Lavoie

James Clifford Sutton

Rajeev S Bhide

Zulan Pi

Patrick Y S Lam

Rico C Lavoie

The invention relates to the inhibition of histone deactylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Inhibitors of histone deacetylase

The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Yreceptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Yreceptor activity.

[object Object]

Compounds having the formula (I), G is a novel side chain selected from Calkenyl, A-aryl, &#x2014;OR, heteroaryl, A-cyano, A&#x2014;OR, A&#x2014;C(&#x2550;O)R, A&#x2014;COR, A&#x2014;C(&#x2550;O)NRR, A&#x2014;OC(&#x2550;O)R, A&#x2014;NRC(&#x2550;O)R, A&#x2014;OC(&#x2550;O)NRR, A&#x2014;NRCOR, A&#x2014;NRSOR, A&#x2014;SOR, A&#x2014;NRC(&#x2550;O)NRR, and A&#x2014;SR; or when y is 0 or when W is not NHR, G may be A-heterocyclo, wherein Ais a bond, Calkylene or C-alkenylene, Ais Calkylene or Calkenylene, and Ais Calkenylene; W is selected from &#x2014;NRR, &#x2014;OR, &#x2014;NRC(&#x2550;O)R, &#x2014;NRCOR, amidino, guanidino, or a heteroaryl, heterocyclo or Ccycloalkyl as defined in the specification, and X and Rthrough Rare as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.

Compounds useful as modulators of Melanocortin Receptors and pharmaceutical compositions comprising same

Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof,in which E isX is N or CH, W is &#x2014;NRR, &#x2014;NRC(&#x2550;O)R, &#x2014;NRCOR, &#x2014;OR, or a heteroaryl or heterocyclo group as defined in the specification, and Rthrough R, R, R, R, R, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and MC-4R.

Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same

The present invention provides compounds of formula I,and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Azaindole kinase inhibitors

The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Growing community of inventors

Mascouche, Canada

Carl Thibault