Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.
Type:
Grant
Filed:
January 24, 2001
Date of Patent:
December 20, 2005
Assignee:
Kinacia Pty. Ltd.
Inventors:
Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yap, Hishani Parbaharan, Phil Thompson