Claims for Patent: 9,175,009

Summary for Patent: 9,175,009

Title:	Benzoxepin PI3K inhibitor compounds and methods of use
Abstract:	Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z.sup.1 is CR.sup.1 or N; Z.sup.2 is CR.sup.2 or N; Z.sup.3 is CR.sup.3 or N; Z.sup.4 is CR.sup.4 or N; and where (i) X.sup.1 is N and X.sup.2 is S, (ii) X.sup.1 is S and X.sup.2 is N, (iii) X.sup.1 is CR.sup.7 and X.sup.2 is S, (iv) X.sup.1 is S and X.sup.2 is CR.sup.7; (v) X.sup.1 is NR.sup.8 and X.sup.2 is N, (vi) X.sup.1 is N and X.sup.2 is NR.sup.8, (vii) X.sup.1 is CR.sup.7 and X.sup.2 is O, (viii) X.sup.1 is O and X.sup.2 is CR.sup.7, (ix) X.sup.1 is CR.sup.7 and X.sup.2 is C(R.sup.7).sub.2, (x) X.sup.1 is C(R.sup.7).sub.2 and X.sup.2 is CR.sup.7; (xi) X.sup.1 is N and X.sup.2 is O, or (xii) X.sup.1 is O and X.sup.2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. ##STR00001##
Inventor(s):	Blaquiere; Nicole (San Francisco, CA), Do; Steven (San Jose, CA), Dudley; Danette (Pacifica, CA), Folkes; Adrian (Berkshire, GB), Goldsmith; Richard (Belmont, CA), Heald; Robert (Harlow, GB), Heffron; Timothy (Burlingame, CA), Kolesnikov; Aleksandr (San Francisco, CA), Ndubaku; Chudi (San Francisco, CA), Olivero; Alan G. (Half Moon Bay, CA), Price; Stephen (Harlow, GB), Staben; Steven (San Francisco, CA), Wei; BinQing (Belmont, CA)
Assignee:	GENENTECH, INC. (South San Francisco, CA)
Application Number:	14/565,669
Patent Claims:	1. A method of treating a hyperproliferative disease comprising administering a pharmaceutical composition comprised of a therapeutically effective amount of 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dih- ydrobenzo[b]thieno[2,3-d]oxepine-8-carboxamide and a pharmaceutically acceptable carrier, glidant, diluent, or excipient to a patient having said hyperproliferative disease, wherein the hyperproliferative disease is cancer selected from breast, colon, glioma, lung, melanoma, ovarian and prostate cancer. 2. The method of claim 1 wherein the pharmaceutical composition is administered to the patient by injection. 3. The method of claim 1 wherein the patient is further treated with ranibizumab or bevacizumab. 4. A method of inhibiting PI3K and/or mTOR in a patient, the method comprising administering a therapeutically effective amount of 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dih- ydrobenzo[b]thieno[2,3-d]oxepine-8-carboxamide together with a pharmaceutically acceptable carrier, glidant, diluent, or excipient to the patient. 5. A process for making 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dih- ydrobenzo[b]thieno[2,3-d]oxepine-8-carboxamide comprising reacting 2-[5-amino-2-(2,4-difluoro-phenyl)-2H-[1,2,4]triazol-3-yl]-4,5-dihydro-6-- oxa-1-thia-benzo[e]azulene-8-carboxylic acid and methylamine hydrochloride.

Details for Patent 9,175,009

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004		2039-02-26
Genentech, Inc.	LUCENTIS	ranibizumab	Injection	125156	06/30/2006		2039-02-26
Genentech, Inc.	LUCENTIS	ranibizumab	Injection	125156	08/10/2012		2039-02-26
Genentech, Inc.	LUCENTIS	ranibizumab	Injection	125156	10/13/2016		2039-02-26
Genentech, Inc.	LUCENTIS	ranibizumab	Injection	125156	03/20/2018		2039-02-26