Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
Type:
Grant
Filed:
February 6, 2009
Date of Patent:
September 20, 2011
Assignee:
OSI Pharmaceuticals, LLC
Inventors:
An-Hu Li, Arno G. Steinig, Andrew Kleinberg, Qinghua Weng, Mark J. Mulvihill, Jing Wang, Xin Chen, Ti Wang, Hanqing Dong, Meizhong Jin
Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.
Type:
Grant
Filed:
November 9, 2005
Date of Patent:
August 23, 2011
Assignee:
OSI Pharmaceuticals, LLC
Inventors:
Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
Abstract: The present invention provides methods of identifying an agents that inhibit tumor cells from undergoing an epithelial to mesenchymal transition, impair tumor cell mobility, and thus inhibit tumorigenicity. The present invention also provides compositions comprising said agents, and methods for their preparation and use. The present invention also provides methods for inhibiting tumor cells in a patient from undergoing an epithelial to mesenchymal transition by administration of inhibitors of PAK2 kinase, that optionally also inhibit PAK1 kinase. Such methods may be employed in combination with other anti-cancer agents such as EGFR or IGF-1R kinase inhibitors.
Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and cisplatin combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and cisplatin combination in combination with a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as Tarceva™).