IP Library Granted Patent US 10,385,031
Granted Patent B2
US 10,385,031 · App. 15/820,827 · Granted Aug 20, 2019

Substituted piperazines as selective HDAC1,2 inhibitors

Inventors: John H. van Duzer (Georgetown, MA); Ralph Mazitschek (Belmont, MA)
Assignee: REGENACY PHARMACEUTICALS, LLC
C07D295/155A61P7/00A61P35/00A61P35/02C07D213/40C07D213/82C07D215/48C07D263/48C07D277/56C07D307/52C07D333/20C07D401/04C07D401/12C07D401/14C07D405/12C07D405/14C07D409/12C07D409/14C07D413/04C07D413/12C07D417/12C07D417/14
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Quick Facts
Patent No.
US 10,385,031
App. No.
15/820,827
Granted
Aug 20, 2019
Kind
B2
Abstract

Provided herein are compounds of Formula II, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity

Claims (28)

1. A compound of Formula (II):

or a pharmaceutically acceptable salt thereof,

wherein:

R 3 is furyl, pyridyl, phenyl or thienyl, wherein phenyl is optionally substituted with one or more halogens;

R 4 is H or C 1-4 alkyl, wherein the C 1-4 alkyl is optionally and independently substituted one or more times with one or more substituents selected from the group consisting of halogen, —CN, —NO 2 , C 1-6 alkoxy, C 1-6 alkyl, C 1-6 haloalkyl and C(O)—C 1-6 alkyl; and

B is pyrazyl, oxazolyl, thienyl or thiazolyl, wherein the thiazolyl is optionally substituted with CH 3 .

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is furyl, pyridyl or thienyl; and

B is oxazolyl, thienyl or thiazolyl.

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is H or CH 3 .

4. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

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

8. A method for inhibiting the activity of histone deacetylase 1 and/or histone deacetylase 2 in a subject, comprising administering to a subject in need thereof a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the subject is a human.

10. The method of claim 8 , wherein the subject has a disease selected from the group consisting of sickle cell disease, beta thalassemia, myelodysplastic syndrome, acute myelogenous leukemia, neuroblastoma and acute megakaryocytic leukemia.

11. The method of claim 8 , wherein the subject has a disease mediated by histone deacetylase 1 and/or histone deacetylase 2.

12. The method of claim 11 , wherein the disease is a myelodysplastic syndrome.

13. The method of claim 11 , wherein the disease is a hemoglobinopathy.

14. The method of claim 13 , wherein the hemoglobinopathy is sickle-cell disease or beta-thalassemia.

15. The method of claim 11 , wherein the disease is a cancer.

16. The method of claim 15 , wherein the cancer is lung cancer, colon cancer, breast cancer, neuroblastoma, leukemia or lymphoma.

17. The method of claim 15 , wherein the cancer is acute myelogenous leukemia or acute megakaryocytic leukemia.

18. The method of claim 15 , wherein the cancer is neuroblastoma.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 12, 2019
From: VAN DUZER, JOHN H.; MAZITSCHEK, RALPH
To: REGENACY PHARMACEUTICALS, LLC
Reel/Frame 048868/0168 →
Continuity (3)
Provisional Application 62425938 · Nov 23, 2016
Provisional Application 62506344 · May 15, 2017
Related Publication 20180141923A1 · May 24, 2018