IP Library › Granted Patent US 9,447,045
Granted Patent B2
US 9,447,045 · App. 14/740,143 · Granted Sep 20, 2016

Histone demethylase inhibitors

Inventors: Young K. Chen (San Marcos, CA); Toufike Kanouni (La Jolla, CA); Zhe Nie (San Diego, CA); Jeffrey Alan Stafford (San Diego, CA); James Marvin Veal (Apex, NC); Michael Brennan Wallace (San Diego, CA)
Assignee: Celgene Quanticel Research, Inc.
C07D213/74C07D213/79C07D213/81C07D237/24C07D401/04C07D401/12C07D405/12C07D405/14C07D409/12C07D409/14
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Quick Facts
Patent No.
US 9,447,045
App. No.
14/740,143
Granted
Sep 20, 2016
Kind
B2
Abstract

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine 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 (24)

1. A compound of Formula (I), or pharmaceutically acceptable salt thereof,

wherein, R is hydrogen or alkyl;

G is —X—Y;

X is unsubstituted —C1-C5 alkylene, unsubstituted —(C1-C5 alkylene)—Z—(C1-C5 alkylene)—, or unsubstituted —(C1-C5 alkylene)—Z—;

Y is unsubstituted carbocyclyl, unsubstituted heterocyclyl, unsubstituted aryl, or unsubstituted heteroaryl; and

 and n is 0, 1, 2, or 3;

Z is unsubstituted

with the provision:

G is not

2. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is a C1 alkylene.

3. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is a C2 alkylene.

4. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is a C3 alkylene.

5. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is —(C1-C5 alkylene)—Z—.

6. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is —(C1 alkylene)—Z—.

7. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein X is —(C1 alkylene)—Z—, and n is 0, 1 or 2.

8. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein Y is carbocyclyl.

9. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein Y is heterocyclyl.

10. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein Y is aryl.

11. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein Y is heteroaryl.

12. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein R is hydrogen.

13. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein R is alkyl.

14. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of Formula (I) as described in claim 1 , or pharmaceutically acceptable salt thereof.

15. A method of inhibiting a histone demethylase enzyme comprising contacting the histone demethylase enzyme with a compound of Formula (I) as described in claim 1 .

16. A method of treating cancer in a subject in need thereof comprising administering to the subject a composition comprising a compound of Formula (I) as described in claim 1 , or 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 13, 2015
From: CHEN, YOUNG K.; KANOUNI, TOUFIKE; NIE, ZHE; STAFFORD, JEFFREY ALAN; VEAL, JAMES MARVIN; WALLACE, MICHAEL BRENNAN
To: QUANTICEL PHARMACEUTICALS, INC.
Reel/Frame 036073/0615 →
Continuity (5)
Continuation 14592830 · Jan 8, 2015
Division 14139197 · Dec 23, 2013
Provisional Application 61785380 · Mar 14, 2013
Provisional Application 61745246 · Dec 21, 2012
Related Publication 20150291529A1 · Oct 15, 2015