Claims for Patent: 8,614,330

Summary for Patent: 8,614,330

Title:	Substituted benz-azoles and methods of their use as inhibitors of RAF kinase
Abstract:	New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Inventor(s):	Amiri; Payman (Walnut Creek, CA), Fantl; Wendy (San Francisco, CA), Hansen; Teresa (Danville, CA), Levine; Barry Haskell (Lafayette, CA), McBride; Christopher (Oakland, CA), Poon; Daniel J. (Oakland, CA), Ramurthy; Savithri (Walnut Creek, CA), Renhowe; Paul A. (Danville, CA), Shafer; Cynthia M. (El Sobrante, CA), Subramanian; Sharadha (San Ramon, CA), Sung; Leonard (Irvine, CA)
Assignee:	Novartis Vaccines and Diagnostics, Inc. (Emeryville, CA)
Application Number:	12/723,483
Patent Claims:	1. A compound selected from the group consisting of: (a) (4-{2-[(4-bromophenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))-N-methylcar- boxamide; (b) (4-{2-[(4-chlorophenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))-N-methylca- rboxamide; (c) N-methyl(4-{2-[(4-methylphenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))car- boxamide; (d) N-methyl[4-(2-{[4-(trifluoromethoxy)phenyl]amino}benzothiazol-5-yloxy)(2-- pyridyl)]carboxamide; (e) (4-{2-[(4-butylphenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))-N-methylcar- boxamide; (f) N-methyl[4-(2-{[4-(methylethyl)phenyl]amino}benzothiazol-5-yloxy)(2-pyrid- yl)]carboxamide; (g) (4-{2-[(3,4-dichlorophenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))-N-meth- ylcarboxamide; (h) (4-{2-[(4-bromophenyl)amino]benzothiazol-5-yloxy}(2-pyridyl))-N-(2-morpho- lin-4-ylethyl)carboxamide; (i) N-((3R)pyrrolidin-3-yl)(4-{2-[(4-bromophenyl)amino]benzothiazol-5-yloxy}(- 2-pyridyl))carboxamide; and (j) N-[(3R,5R)-5-(methoxymethyl)pyrrolidin-3-yl](4-{2-[(4-bromophenyl)amino]-- benzothiazol-5-yloxy}(2-pyridyl))carboxamide. 2. A composition comprising an amount of a compound of claim 1 effective to inhibit Raf activity in a human or animal subject when administered thereto, together with a pharmaceutically acceptable carrier. 3. A composition of claim 2 which further comprises at least one additional agent for the treatment of cancer. 4. A composition of claim 3 in which the at least one additional agent for the treatment of cancer is selected from irinotecan, topotecan, gemcitabine, 5-fluorouracil, leucovorin carboplatin, cisplatin, taxanes, tezacitabine, cyclophosphamide, vinca alkaloids, imatinib, anthracyclines, rituximab and trastuzumab.

Details for Patent 8,614,330

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2022-03-29
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2022-03-29
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2022-03-29
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2022-03-29
Genentech, Inc.	RITUXAN HYCELA	rituximab and hyaluronidase human	Injection	761064	06/22/2017		2022-03-29
Genentech, Inc.	HERCEPTIN HYLECTA	trastuzumab and hyaluronidase-oysk	Injection	761106	02/28/2019		2022-03-29