IP Library Granted Patent US 10,370,343
Granted Patent B2
US 10,370,343 · App. 16/003,861 · Granted Aug 6, 2019

[6,6] Fused bicyclic HDAC8 inhibitors

Inventors: Xiaozhang Zheng (Lexington, MA); Pui Yee Ng (Waltham, MA); Jennifer R. Thomason (Clinton, MA); Mary-Margaret Zablocki (Revere, MA); Bingsong Han (North Haven, CT); Nicholas Barczak (Waterford, CT); Cuixian Liu (Madison, CT); Aleksandra Rudnitskaya (Roslindale, MA); David R. Lancia, Jr. (Boston, MA); Kenneth W. Bair (Wellesley, MA)
Assignee: FORMA Therapeutics, Inc.
C07D265/36C07D265/34C07D279/14C07D279/16C07D401/04C07D413/06C07D413/10C07D413/12C07D417/06C07D471/04C07D487/04C07D491/107C07D513/04
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Quick Facts
Patent No.
US 10,370,343
App. No.
16/003,861
Granted
Aug 6, 2019
Kind
B2
Abstract

The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R 1 , R 2 , R 2 ′, L, X, W, Y 1 , Y 2 , Y 3 , and Y 4 are described herein.

Claims (38)

1. A composition comprising a compound selected from:

or a pharmaceutically acceptable salt thereof.

2. The composition of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

3. The composition of claim 2 , further comprising the compound:

or a pharmaceutically acceptable salt thereof.

4. The composition of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

5. The composition of claim 4 , further comprising the compound:

or a pharmaceutically acceptable salt thereof.

6. A composition comprising a compound selected from:

or a pharmaceutically acceptable salt thereof,

wherein the compound is obtained by a process comprising a step of treating a compound:

with hydroxylamine and a first base to form a compound:

wherein R 1 is selected from the group consisting of:

7. The composition of claim 6 , wherein the first base comprises a hydroxide ion.

8. The composition of claim 7 , wherein the first base is NaOH.

9. The composition of claim 6 , wherein the process further comprises a step of treating a compound:

with R 1 —X′, wherein X′ is halogen, and a second base to form the compound:

10. The composition of claim 9 , wherein the second base is NaH, K 2 CO 3 , or Cs 2 CO 3 .

11. The composition of claim 9 , wherein X′ is Cl or Br.

12. The composition of claim 6 , wherein the composition comprises:

or a pharmaceutically acceptable salt thereof,

wherein the compound is obtained by a process, comprising the step of treating the compound:

with hydroxylamine and a first base to form the compound:

13. The composition of claim 12 , wherein the process further comprises the step of treating the compound:

with R 1 —X′, wherein X′ is halogen, and a second base to form the compound:

14. The composition of claim 6 , wherein the composition comprises:

or a pharmaceutically acceptable salt thereof,

wherein the compound is obtained by a process, comprising the step of treating the compound:

with hydroxylamine and a first base to form the compound:

15. The composition of claim 14 , wherein the process further comprises the step of treating the compound:

with R 1 —X′, wherein X′ is halogen, and a second base to form the compound:

16. A composition comprising a first compound selected from:

and

a second compound:

17. The composition of claim 16 , wherein the first compound is:

18. The composition of claim 16 , wherein the first compound is:

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 Jun 28, 2018
From: ZHENG, XIAOZHANG; NG, PUI YEE; THOMASON, JENNIFER R.; ZABLOCKI, MARY-MARGARET; HAN, BINGSONG; BARCZAK, NICHOLAS; LIU, CUIXIAN; RUDNITSKAYA, ALEKSANDRA; LANCIA, DAVID R., JR.; BAIR, KENNETH W.
To: FORMA THERAPEUTICS, INC.
Reel/Frame 046226/0926 →
Continuity (3)
Continuation 15255817 · Sep 2, 2016
Provisional Application 62214101 · Sep 3, 2015
Related Publication 20180354919A1 · Dec 13, 2018