Abstract: The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
Type:
Grant
Filed:
July 27, 1999
Date of Patent:
December 18, 2001
Assignees:
University of California, Yissum Research Development Company of the Hebrew University
of Jerusalem, Biosignal LTD, Sugen, Inc., Max-Planck-Gesellschaft zur Forderung der Wissenschaften
E.V.
Inventors:
Klaus P. Hirth, Elaina Mann, Laura K. Shawyer, Axel Ullrich, Istvan Szekely, Tamas Bajor, Janis Haimichael, Laszlo Orfi, Alex Levitzki, Aviv Gazit, Peng Cho Tang, Reiner Lammers