IP Library › Granted Patent US 9,738,637
Granted Patent B2
US 9,738,637 · App. 14/774,329 · Granted Aug 22, 2017

Histone demethylase inhibitors

Inventors: Young K. Chen (San Marcos, CA); Michael Brennan Wallace (San Diego, CA)
Assignee: Celgene Quantical Research, Inc.
C07D471/04
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Quick Facts
Patent No.
US 9,738,637
App. No.
14/774,329
Granted
Aug 22, 2017
Kind
B2
Abstract

The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of 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 (15)

1. A compound having the structure of Formula (II),

or a pharmaceutically acceptable salt thereof, wherein,

R 1 is hydrogen or alkyl;

G is X-R 2 or X 1 -alkyl, wherein

X is a bond, alkyl, alkyl-O—, —C(O)—, —C(O)—NH—, —NH—, —NH—C(O)—, —O—, —S—, or —SO 2 ;

R 2 is selected from monocyclic or bicyclic carbocyclyl, heterocyclyl, aryl, or heteroaryl, optionally substituted with at least one alkyl, phenyl, halogen, hydroxyl, —CF 3 , —CN, NH—C(O), —O-alkyl, —O-carbocyclyl, —O-alkyl-CF 3 , or —O—CF 3 ;

X 1 is a bond, —C(O)—, —C(O)—NH—, —NH—, —NH—C(O), —O—, —S—, or —SO 2 —; and

R 3 is hydrogen, halogen or alkyl.

2. The compound of claim 1 , wherein R 1 is hydrogen.

3. The compound of claim 1 , wherein R 3 is hydrogen.

4. The compound of claim 1 , wherein G is X—R 2 .

5. The compound of claim 4 , wherein X is a bond and R 2 is monocyclic or bicyclic aryl.

6. The compound of claim 4 , wherein X is alkyl and R 2 is monocyclic or bicyclic aryl.

7. The compound of claim 4 , wherein X is a bond and R 2 is monocyclic or bicyclic heteroaryl.

8. The compound of claim 4 , wherein X is alkyl and R 2 is monocyclic or bicyclic heteroaryl.

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 Sep 23, 2015
From: CHEN, YOUNG K.; WALLACE, MICHAEL BRENNAN
To: QUANTICEL PHARMACEUTICALS, INC.
Reel/Frame 036638/0931 →
Continuity (2)
Provisional Application 61778193 · Mar 12, 2013
Related Publication 20160194315A1 · Jul 7, 2016