Claims for Patent: 9,586,940

Summary for Patent: 9,586,940

Title:	Methods for treatment of breast cancer nonresponsive to trastuzumab
Abstract:	The present invention provides a method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of compound N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydro- cyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof.
Inventor(s):	Waksal; Samuel (New York, NY), Chiang; Lillian (Princeton, NJ)
Assignee:	KADMON CORORATION, LLC (New York, NY)
Application Number:	14/801,335
Patent Claims:	1. A method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound of Formula 1 ##STR00003## or a pharmaceutically acceptable salt thereof. 2. The method of claim 1, wherein the compound, or a pharmaceutically acceptable salt thereof, is a stereoisomer selected from the group consisting of N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclop- enta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine and N-(3,4-dichloro-2-fluorophenyl)-7-({[(3 aR, 5 s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy- )quinazolin-4-amine, or a pharmaceutically acceptable salt of the stereoisomer. 3. The method as in claim 1 or 2, wherein the pharmaceutically acceptable salt is the salt of p-toluenesulfonic acid. 4. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer has not been treated with trastuzumab. 5. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer has been treated with trastuzumab. 6. The method as in claim 1, 2 or 3, comprising co-administering the compound of Formula 1 and trastuzumab. 7. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer is PTEN-negative. 8. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer is positive for mutations in the PIK3CA gene. 9. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer expresses a truncated ErbB2 receptor that lacks the extracellular domain to which trastuzumab binds. 10. The method as in claim 1, 2 or 3, wherein the subject is human and the breast cancer overexpresses one or more RTKs selected from the group consisting of EGFR family members, IGF-1R and HGFR.

Details for Patent 9,586,940

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2031-12-27
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2031-12-27
Genentech, Inc.	HERCEPTIN HYLECTA	trastuzumab and hyaluronidase-oysk	Injection	761106	02/28/2019		2031-12-27