IP Library Granted Patent US 10,968,180
Granted Patent B2
US 10,968,180 · App. 16/433,386 · Granted Apr 6, 2021

Piperidine derivatives as HDAC1/2 inhibitors

Inventors: John H. van Duzer (Concord, MA); Ralph Mazitschek (Weston, MA)
Assignee: Regenacy Pharmaceuticals, LLC
C07D211/58C07D401/12C07D401/14C07D409/12C07D409/14
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,968,180
App. No.
16/433,386
Granted
Apr 6, 2021
Kind
B2
Abstract

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

Claims (23)

1. A compound of Formula III:

or a pharmaceutically acceptable salt thereof;

wherein,

X 1 is N;

X 2 is N;

R 1 is selected from the group consisting of H and C 1 -C 6 -alkyl;

R 2 is selected from the group consisting of H, C 1 -C 6 -alkyl, and C 6 -aryl;

R 3 is selected from the group consisting of H, C 1 -C 6 -alkyl, and C 6 -aryl;

or R 2 and R 3 together form a C 2 -C 6 -heterocyclyl;

R 4 is H; and

R 5 is C 1 -C 6 -alkyl;

or R 4 and R 5 together form a C 2 -C 6 -heterocyclyl, wherein heterocyclyl is optionally substituted by 1 or 2 of C 1 -C 6 -alkyl, halo, or hydroxy.

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

3. The compound of claim 1 , wherein R 3 is H, methyl, or isopropyl.

4. The compound of claim 1 , wherein R 4 and R 5 together form a heterocyclyl selected from the group consisting of morpholinyl, piperidinyl, piperazinyl, and pyrrolidinyl, wherein the morpholinyl, piperidinyl, piperazinyl, and pyrrolidinyl are optionally substituted by 1 or 2 of C 1 -C 6 -alkyl, halo, or hydroxy.

5. The compound of claim 1 , wherein

R 1 is H;

R 2 is H;

R 3 is H or C 1 -C 4 -alkyl; and

R 4 and R 5 together form a heterocyclyl selected from the group consisting of morpholinyl, piperidinyl, piperazinyl, and pyrrolidinyl, wherein the morpholinyl, piperidinyl, piperazinyl, and pyrrolidinyl are optionally substituted by 1 or 2 of C 1 -C 6 -alkyl, halo, or hydroxy.

6. The compound of claim 1 , selected from:

or pharmaceutically acceptable salts thereof.

7. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2019
From: VAN DUZER, JOHN H.; MAZITSCHEK, RALPH
To: ACETYLON PHARMACEUTICALS, INC.
Reel/Frame 051188/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2019
From: ACETYLON PHARMACEUTICALS, INC.
To: REGENACY PHARMACEUTICALS, LLC
Reel/Frame 051190/0745 →
Continuity (5)
Continuation 15700998 · Sep 11, 2017
Division 14966556 · Dec 11, 2015
Provisional Application 62238931 · Oct 8, 2015
Provisional Application 62091221 · Dec 12, 2014
Related Publication 20190359569A1 · Nov 28, 2019