Bayard D Clarkson, Age 98223 Piping Rock Rd, Muttontown, NY 11545

2005000, Jan 13, 2005

Jan 5, 2004

10/751703

Darren Veach - New York NY, US
William Bornmann - New York NY, US
Bayard Clarkson - New York NY, US
Nikolas Bubonoff - Munich, DE
Justus Duyster - Munich, DE

A61K031/519
C07D487/02

514264110, 544280000

The present invention provides compounds of formula (0): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (0) and provides methods of treating cancer comprising administering a compound of formula (0).

6100386, Aug 8, 2000

Jan 22, 1997

8/787091

Nicholas A. Carpino - Memphis TN
Ryuji Kobayashi - Syosset NY
David G. Wisniewski - Staten Island NY
Annabel O'C. Strife - New York NY
Bayard D. Clarkson - New York NY

Cold Spring Harbor Laboratory - Cold Spring Harbor NY
Sloan-Kettering Institute for Cancer Research - New York NY

C07H 2104
C12N 1563
C12P 2100

536 231

Characteristic of chronic myelogenous leukemia (CML) is the presence of the chimeric p120. sup. bcr-abl protein possessing elevated protein tyrosine kinase activity relative to normal c-abl tyrosine kinase. Hematopoietic progenitors isolated from CML patients in the chronic phase contain a constitutively tyrosine phosphorylated protein that migrates at approximately 62 kDa by SDS-PAGE and associates with the p120 ras GTPase-activating protein (GAP). This novel protein, called p62. sup. dok (p62 protein downstream of tyrosine kinases), was isolated from a hematopoietic cell line expressing p120. sup. bcr-abl. Association of p62. sup. dok with GAP correlates with its tyrosine phosphorylation. p62. sup. dok is rapidly tyrosine phosphorylated upon activation of the c-kit receptor, implicating it as a component of a signal transduction pathway downstream of receptor tyrosine kinases.