IP Library Granted Patent US 10,377,726
Granted Patent B2
US 10,377,726 · App. 16/173,871 · Granted Aug 13, 2019

3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors

Inventors: Xiaozhang Zheng (Lexington, MA); Pui Yee Ng (Waltham, MA); Bingsong Han (Westwood, MA); Jennifer R. Thomason (Clinton, MA); Mary-Margaret Zablocki (Revere, MA); Cuixian Liu (Madison, CT); Aleksandra Rudnitskaya (Roslindale, MA); David R. Lancia, Jr. (Boston, MA); David S. Millan (Watertown, MA); Matthew W. Martin (Arlington, MA)
Assignee: Forma Therapeutics, Inc.
C07D267/14C07D243/14C07D267/12C07D291/08C07D401/06C07D401/10C07D403/06C07D403/10C07D405/06C07D413/04C07D413/06C07D413/08C07D413/12C07D413/14C07D417/04C07D471/04C07D491/107C07D493/08C07D495/10C07D498/04C07D498/08
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Quick Facts
Patent No.
US 10,377,726
App. No.
16/173,871
Granted
Aug 13, 2019
Kind
B2
Abstract

The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , and Y 4 are described herein.

Claims (18)

1. A compound:

or a pharmaceutically acceptable salt thereof.

2. A composition, comprising a compound:

or a pharmaceutically acceptable salt thereof.

3. The composition of claim 2 , wherein the composition further comprises an ester:

4. The composition of claim 3 , wherein the composition further comprises an amine:

5. The composition of claim 4 , wherein the composition further comprises an aryl halide:

6. The composition of claim 2 , further comprising at least one compound selected from:

7. A process for preparing a compound:

or a pharmaceutically acceptable salt thereof,

comprising a step of treating an ester:

with hydroxylamine and a first base to form the compound:

8. The process of claim 7 , wherein the process further comprises a step of treating an amine:

with an acyl halide in the presence of a second base to form the ester:

9. The process of claim 8 , wherein the process further comprises a step of cyclizing an aryl halide:

in the presence of a catalytic amount of a metal catalyst to form the amine:

10. The process of claim 9 , wherein the process further comprises a step of treating (S)-2-amino-2-phenylethan-1-ol with a benzylic halide:

to form the aryl halide:

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Oct 17, 2023
From: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
To: VALO HEALTH, INC.; VALO HEALTH, LLC
Reel/Frame 065255/0660 →
SECURITY INTEREST Recorded Jul 6, 2023
From: VALO HEALTH, LLC; VALO HEALTH, INC.
To: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
Reel/Frame 064207/0957 →
MERGER Recorded Sep 8, 2021
From: VALO EARLY DISCOVERY, INC.
To: VALO HEALTH, INC.
Reel/Frame 057438/0025 →
CHANGE OF NAME Recorded Sep 16, 2020
From: INTEGRAL EARLY DISCOVERY, INC.
To: VALO EARLY DISCOVERY, INC.
Reel/Frame 053787/0138 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2020
From: FORMA THERAPEUTICS, INC.
To: INTEGRAL EARLY DISCOVERY, INC.
Reel/Frame 053402/0298 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 31, 2018
From: ZHENG, XIAOZHANG; NG, PUI YEE; HAN, BINGSONG; THOMASON, JENNIFER R.; ZABLOCKI, MARY-MARGARET; LIU, CUIXIAN; RUDNITSKAYA, ALEKSANDRA; LANCIA, DAVID R., JR; MILLAN, DAVID S.; MARTIN, MATTHEW W.
To: FORMA THERAPEUTICS, INC.
Reel/Frame 047369/0765 →
Continuity (4)
Continuation 15013816 · Feb 2, 2016
Provisional Application 62205438 · Aug 14, 2015
Provisional Application 62110716 · Feb 2, 2015
Related Publication 20190062288A1 · Feb 28, 2019
Cited By (6)
US 12,201,617 US 12,213,969 US 12,264,137 US 12,304,904 US 12,312,345 US 12,564,880