IP Library Granted Patent US 9,096,549
Granted Patent B2
US 9,096,549 · App. 14/169,732 · Granted Aug 4, 2015

Selective HDAC3 inhibitors

Inventors: John H. van Duzer (Georgetown, MA); Ralph Mazitschek (Belmont, MA)
Assignee: ACETYLON PHARMACEUTICALS, INC.
C07D241/44C07D209/34C07D215/38C07D215/54C07D217/26C07D231/56C07D235/06C07D471/04
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Quick Facts
Patent No.
US 9,096,549
App. No.
14/169,732
Granted
Aug 4, 2015
Kind
B2
Abstract

Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.

Claims (37)

1. A compound of Formula II:

or a pharmaceutically acceptable salt thereof,

wherein

A is bicyclic heteroaryl or bicyclic heterocycloalkyl selected from the group consisting of

R 1 is halo;

R 3 is heterocycloalkyl, or C 1-6 -alkyl-heterocycloalkyl wherein the heterocycloalkyl or C 1-6 -alkyl-heterocycloalkyl groups are optionally substituted with C 1-4 -alkyl;

R 4 and R 5 are each independently selected from H, C 1-6 -alkyl, C 2-6 -alkenyl, C 2-6 -alkynyl, C 3-6 -cycloalkyl, C 1-6 -alkyl-C 3-6 -cycloalkyl, heterocycloalkyl, C 1-6 -alkyl-heterocycloalkyl, NR 6 R 7 , O—C 1-6 -alkyl-OR 8 , C 1-6 -alkyl-OR 8 , aryl, C 1-6 -alkyl-aryl, heteroaryl, C 1-6 -alkyl-heteroaryl, C(O)N(R 6 )-heteroaryl, C(O)N(R 6 )-heterocycloalkyl, C(O)N(R 6 )-aryl, C(O)—NR 6 R 7 , C(O) -heteroaryl, C(O)-heterocycloalkyl, C(O)-aryl, C(O)—C 1-6 -alkyl, CO 2 -heteroaryl, CO 2 -heterocycloalkyl, CO 2 -aryl, CO 2 -C 1-6 -alkyl, or C(O)—C 1-6 -alkyl-heterocycloalkyl, wherein the cycloalkyl, heterocycloalkyl, aryl, or heteroaryl groups are optionally substituted with C 1-4 -alkyl, CO 2 R 8 , C(O)R 8 , or C 1-6 -alkyl-OR 8 ;

R 6 and R 7 are each independently selected from H, C 1-6 -alkyl, C 1-6 -alkyl-OR 8 , CO 2 R 8 , or C 1 -C 6 -alkyl-aryl; and

R 8 is H or C 1-6 -alkyl.

2. The compound of claim 1 , wherein R 3 is piperazinyl or piperazinyl-CH 3 .

3. The compound claim 1 , wherein R 3 is CH 2 CH 2 -morpholinyl.

4. The compound of claim 1 ,

wherein

R 4 is independently selected from H, C 3-6 -cycloalkyl, C 1-6 -alkyl-C 3-6 -cycloalkyl, heterocycloalkyl, or C 1-6 -alkyl-heterocycloalkyl.

5. The compound claim 4 , wherein R 4 is H or C 3-6 -cycloalkyl.

6. The compound of claim 5 , wherein R 4 is cyclopropyl.

7. A compound of Formula IV:

or a pharmaceutically acceptable salt thereof,

wherein

A is bicyclic heteroaryl or bicyclic heterocycloalkyl selected from the group consisting of

R 1 is H or halo;

R 3 is heterocycloalkyl, or C 1-6 -alkyl-heterocycloalkyl;

R 4 is selected from C 3-6 -cycloalkyl, C 1-6 -alkyl-C 3-6 -cycloalkyl, heterocycloalkyl, C 1-6 -alkyl-heterocycloalkyl, aryl, C 1-6 -alkyl-aryl, heteroaryl, C 1-6 -alkyl-heteroaryl wherein the cycloalkyl, heterocycloalkyl, aryl, or heteroaryl groups are optionally substituted with C 1-4 -alkyl, CO 2 R 8 , C(O)R 8 , or C 1-6 -alkyl-OR 8 ; and

R 8 is H or C 1-6 -alkyl.

8. The compound of claim 7 , wherein R 1 is halo.

9. The compound of claim 7 , wherein R 3 is heterocycloalkyl.

10. The compound of claim 7 , wherein R 4 is cycloalkyl.

11. The compound of claim 1 , selected from the following:

or pharmaceutically acceptable salts thereof.

12. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

13. The compound of claim 1 , wherein R 1 is fluoro.

14. The compound claim 7 , wherein R 1 is fluoro.

15. The compound of claim 7 , wherein R 3 is piperazinyl.

16. The compound of claim 7 , wherein R 4 is cyclopropyl.

17. The compound of claim 7 , which is:

or a pharmaceutically acceptable salt thereof.

18. A pharmaceutical composition comprising a compound of claim 7 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2017
From: ACETYLON PHARMACEUTICALS INC
To: REGENACY PHARMACEUTICALS, LLC
Reel/Frame 044032/0220 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2014
From: VAN DUZER, JOHN H.; MAZITSCHEK, RALPH
To: ACETYLON PHARMACEUTICALS, INC.
Reel/Frame 033173/0958 →
Continuity (3)
Provisional Application 61759732 · Feb 1, 2013
Provisional Application 61923023 · Jan 2, 2014
Related Publication 20140243345A1 · Aug 28, 2014