IP Library Granted Patent US 9,296,732
Granted Patent B2
US 9,296,732 · App. 14/391,690 · Granted Mar 29, 2016

Substituted benzamides and their uses

Inventors: Amato Giaccia (Palo Alto, CA); Edwin Lai (Santa Clara, CA); Olga Razorenova (Irvine, CA); Denise Chan (San Francisco, CA); Michael Patrick Hay (Auckland, NZ); Muriel Bonnet (Auckland, NZ); Connie Sun (Palo Alto, CA); Ray Tabibiazar (Portola Valley, CA); Po-wai Yuen (Ann Arbor, MI)
Assignees: The Board of Trustees of the Leland Stanford Junior University; Auckland UniServices, Limited; Ruga Corporation
C07D413/12C07D213/75C07D263/62C07D401/12C07D405/12C07D409/12C07D417/12
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Quick Facts
Patent No.
US 9,296,732
App. No.
14/391,690
Granted
Mar 29, 2016
Kind
B2
Abstract

Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.

Claims (20)

1. A compound selected from the group consisting of

4-(5-methyl-4-((piperazin-1-ylsulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(5-methyl-4-((4-methylpiperazin-1-ylsulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-((4-isobutylpiperazin-1-ylsulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-((4-tert-butylpiperazin-1-ylsulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-((4-cyclopropylpiperazin-1-ylsulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(5-methyl-4-((4-(2,2,2-trifluoroethyl)piperazin-1-ylsulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(5-methyl-4-(morpholinosulfonylmethyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-((4-isopropylpiperazin-1-ylsulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(5-methyl-4-(((4-neopentylpiperazin-1-yl)sulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-(((4-ethylpiperazin-1-yl)sulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

4-(4-(((4-cyclobutylpiperazin-1-yl)sulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide, and

4-(5-methyl-4-((thiomorpholinosulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide,

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein the compound is 4-(5-methyl-4-((piperazin-1-ylsulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide.

3. The compound of claim 1 wherein the compound is 4-(5-methyl-4-((4-methylpiperazin-1-ylsulfonyl)methyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide.

4. The compound of claim 1 wherein the compound is 4-(4-((4-isobutylpiperazin-1-ylsulfonyl)methyl)-5-methyloxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide.

5. The compound of claim 1 wherein the compound is 4-(5-methyl-4-(morpholinosulfonylmethyl)oxazol-2-yl)-N-(pyridin-3-ylmethyl)benzamide.

6. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

7. A method for treating renal carcinoma mediated by HIF-1α and/or HIF-2α, the method comprising administering to a subject a compound as defined in claim 1 .

Assignments (4)
CHANGE OF NAME Recorded Nov 17, 2016
From: RUGA CORPORATION
To: ARAVIVE BIOLOGICS, INC.
Reel/Frame 040645/0147 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2015
From: HAY, MICHAEL PATRICK; BONNETT, MURIEL
To: AUCKLAND UNISERVICES LIMITED
Reel/Frame 035839/0989 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2015
From: SUN, CONNIE L.; TABIBIAZAR, RAY; YUEN, PO-WAI
To: RUGA CORPORATION
Reel/Frame 035910/0871 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2015
From: GIACCIA, AMATO; LAI, EDWIN; RAZORENOVA, OLGA; CHAN, DENISE
To: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Reel/Frame 035915/0486 →
Continuity (3)
Provisional Application 61791823 · Mar 15, 2013
Provisional Application 61623517 · Apr 12, 2012
Related Publication 20150072976A1 · Mar 12, 2015