IP Library › Granted Patent US 9,617,242
Granted Patent B2
US 9,617,242 · App. 14/653,818 · Granted Apr 11, 2017

Histone demethylase inhibitors

Inventors: Toufike Kanouni (La Jolla, CA); Jeffrey Alan Stafford (San Diego, CA); James Marvin Veal (Apex, CA); Michael Brennan Wallace (San Diego, CA)
Assignee: CELGENE QUANTICEL RESEARCH, INC.
C07D401/12C07D401/14C07D403/12C07D405/14C07D413/12C07D413/14C07D471/04
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Quick Facts
Patent No.
US 9,617,242
App. No.
14/653,818
Granted
Apr 11, 2017
Kind
B2
Abstract

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Claims (25)

1. A compound, or pharmaceutically acceptable salt thereof, chosen from:

3-({5-fluoro-1-[2-(4-methylmorpholin-2-yl)ethyl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

3-{[5-chloro-1-(3,3,3-trifluoropropyl)-1H-indol-3-yl]amino}pyridine-4-carboxylic acid,

3-({5-fluoro-1-[(3S)-pyrrolidin-3-yl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

3-({5-fluoro-1-[(3R)-pyrrolidin-3-yl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

3-{[5-fluoro-1-(tetrahydro-2H-pyran-4-yl)-1H-indazol-3-yl]amino}pyridine-4-carboxylic acid,

3-{[5-fluoro-1-(tetrahydro-2H-pyran-3-yl)-1H-indazol-3-yl]amino}pyridine-4-carboxylic acid,

3-{[1-(4,4-difluorocyclohexyl)-5-fluoro-1H-indazol-3-yl]amino}pyridine-4-carboxylic acid,

3-{[1-(tetrahydrofuran-3-yl)-4,5,6,7-tetrahydro-1H-indazol-3-yl]amino}pyridine-4-carboxylic acid,

3-({5-fluoro-1-[(3S)-tetrahydrofuran-3-yl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

3-({5-fluoro-1-[(3R)-tetrahydrofuran-3-yl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

3-{[5-fluoro-1-(tetrahydrofuran-3-yl)-1H-indol-3-yl]amino}pyridine-4-carboxylic acid,

3-{[5-chloro-1-(tetrahydrofuran-3-yl)-1H-indazol-3-yl]amino}pyridine-4-carboxylic acid,

N-cyano-3-({5-fluoro-1-[(3S)-tetrahydrofuran-3-yl]-1H-indazol-3-yl}amino)pyridine-4-carboxamide,

3-({1-[2-(3,3-difluoropyrrolidin-1yl)ethyl]-5-fluoro-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

N-cyano-3-({1-[2-(3,3-difluoropyrrolidin-1 yl)ethyl]-5-fluoro-1H-indazol-3-yl}amino)pyridine-4-carboxamide,

3-({1-[2-(4,4-difluoropiperidin-1 yl)ethyl]-5-fluoro-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid,

N-cyano-3-({1-[2-(4,4-difluoropiperidin-1 yl)ethyl]-5-fluoro-1H-indazol-3-yl}amino)pyridine-4-carboxamide,

N-cyano-3-{[5-fluoro-1-(2-methylpropyl)-1H-indazol-3-yl]amino}pyridine-4-carboxamide,

N-cyano-3-({1-[4-(dimethylamino)butyl]-5-fluoro-1H-indazol-3-yl}amino)pyridine-4-carboxamide,

N-cyano-3-({5-fluoro-1-[2-(pyrrolidin-1-yl)ethyl]-1H-indazol-3-yl}amino)pyridine-4-carboxamide,

3-({5-chloro-1-[2-(pyrrolidin-1-yl)ethyl]-1H-indazol-3-yl}amino)pyridine-4-carboxylic acid, and

N-cyano-3-({5-chloro-1-[2-(pyrrolidin-1-yl)ethyl]-1H-indazol-3-yl}amino)pyridine-4-carboxamide.

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

3. A method for treating cancer in a subject in need thereof, comprising administering to the subject a composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 8, 2016
From: QUANTICEL PHARMACEUTICALS, INC.
To: CELGENE QUANTICEL RESEARCH, INC.
Reel/Frame 038399/0685 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2015
From: KANOUNI, TOUFIKE; STAFFORD, JEFFREY ALAN; VEAL, JAMES MARVIN; WALLACE, MICHAEL BRENNAN
To: QUANTICEL PHARMACEUTICALS, INC.
Reel/Frame 036200/0038 →
Continuity (3)
Provisional Application 61792930 · Mar 15, 2013
Provisional Application 61739521 · Dec 19, 2012
Related Publication 20160060247A1 · Mar 3, 2016