IP Library Granted Patent US 10,508,088
Granted Patent B2
US 10,508,088 · App. 16/202,207 · Granted Dec 17, 2019

Methods using HDAC11 inhibitors

Inventors: Jennifer Lee (Arlington, MA); Nicholas Barczak (Waterford, CT); Jaime A. Escobedo (Natick, MA); Chiara Conti (Belmont, MA); Bingsong Han (Westwood, MA); David R. Lancia, Jr. (Boston, MA); Cuixian Liu (Madison, CT); Matthew W. Martin (Arlington, MA); Pui Yee Ng (Waltham, MA); Aleksandra Rudnitskaya (Roslindale, MA); Jennifer R. Thomason (Clinton, MA); Xiaozhang Zheng (Lexington, MA)
Assignee: FORMA Therapeutics, Inc.
C07D263/58A61K31/403A61K31/404A61K31/4178A61K31/4184A61K31/4188A61K31/4192A61K31/422A61K31/423A61K31/427A61K31/428A61K31/4245A61K31/435A61K31/437A61K31/438A61K31/4439A61K31/4709A61K31/4985A61K31/506A61K31/52A61K31/5377A61K31/5383A61K45/06A61P35/00C07C53/06C07D209/40C07D209/54C07D221/20C07D235/30C07D277/82C07D401/04C07D401/06C07D401/14C07D403/04C07D403/06C07D405/04C07D413/06C07D413/12C07D413/14C07D417/06C07D473/00C07D487/04C07D491/056C07D491/107C07D498/04
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Quick Facts
Patent No.
US 10,508,088
App. No.
16/202,207
Granted
Dec 17, 2019
Kind
B2
Abstract

The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.

Claims (25)

1. A compound of Formula I-A or a pharmaceutically acceptable salt thereof,

wherein:

X 1 , X 2 , X 3 , and X 4 are each independently, at each occurrence, N or CR 1 ;

wherein

(i) X 1 and X 4 are both N, and X 2 and X 3 are each independently CR 1 ;

(ii) X 2 and X 4 are both N, and X 1 and X 3 are each independently CR 1 ;

(iii) X 1 is N and X 2 , X 3 , and X 4 are each independently CR 1 ; or

(iv) X 1 , X 2 , X 3 , and X 4 are each CR 1 ;

R 1 is independently, at each occurrence, —H, —R 3 , —R 4 , —C 1 -C 6 alkyl, —C 2 -C 6 alkenyl, —C 4 -C 8 cycloalkenyl, —C 2 -C 6 alkynyl, —C 3 -C 8 cycloalkyl, heterocyclyl, aryl, heteroaryl containing 1-5 heteroatoms selected from the group consisting of N, S, P and O, —OH, —OR 3 , halogen, —NO 2 , —CN, —NHC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl) 2 , —S(O) 2 NH 2 , —S(O) 2 N(C 1 -C 6 alkyl) 2 , —N(C 1 -C 6 alkyl)S(O) 2 R 5 , —S(O) 2 (C 1 -C 6 alkyl), —(C 1 -C 6 alkyl)S(O) 2 R 5 , —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl)S(O) 2 C 1 -C 6 alkyl, or —(CHR 5 ) p NR 3 R 4 , wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more —OH, halogen, —NO 2 , oxo, —CN, —R 3 , —R 5 , —SR 3 , —OR 3 , —NHR 3 , —NR 3 R 4 , —S(O) 2 N(R 3 ) 2 —, —S(O) 2 R 5 , —C(O)R 5 , —C(O)OR 5 , —NR 3 S(O) 2 R 5 , —S(O)R 5 , —S(O)NR 3 R 4 , —NR 3 S(O)R 5 , heterocycle, aryl, or heteroaryl;

or two occurrences of R 1 , when on adjacent atoms, can combine to form a cycloalkyl, a heterocycle, aryl, heteroaryl containing 1-5 heteroatoms selected from the group consisting of N, S, P and O, or a cycloalkenyl, each optionally substituted with one or more independent occurrences of R 3 and R 4 ;

R 3 and R 4 are independently, at each occurrence, —H, —C 1 -C 6 alkyl, —C 2 -C 6 alkenyl, —C 4 -C 8 cycloalkenyl, —C 2 -C 6 alkynyl, —C 3 -C 8 cycloalkyl, heterocyclyl, aryl, heteroaryl containing 1-5 heteroatoms selected from N, S, P, and O, —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 (C 1 -C 6 alkyl), —(C 1 -C 6 alkyl)S(O) 2 R 5 , —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, oxo, or —(CHR 5 ) p N(C 1 -C 6 alkyl) 2 , wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is optionally substituted with one or more substituents selected from —OH, halogen, —NO 2 , oxo, —CN, —R 5 , —O(C 1 -C 6 )alkyl, —NH(C 1 -C 6 )alkyl, —N(C 1 -C 6 alkyl) 2 , —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 NHC 1 -C 6 alkyl, —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl)S(O) 2 C 1 -C 6 alkyl, —S(O)R 5 , —S(O)N(C 1 -C 6 alkyl) 2 , —N(C 1 -C 6 alkyl)S(O)R 5 , heterocycle, aryl, or heteroaryl;

R 5 is independently, at each occurrence, —H, —C 1 -C 6 alkyl, —C 2 -C 6 alkenyl, —C 4 -C 8 cycloalkenyl, —C 2 -C 6 alkynyl, —C 3 -C 8 cycloalkyl, heterocyclyl, aryl, heteroaryl containing 1-5 heteroatoms selected from N, S, P and O, —OH, halogen, —NO 2 , —CN, —N(C 1 -C 6 alkyl) 2 , —S(O) 2 NH(C 1 -C 6 alkyl), —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 C 1 -C 6 alkyl, —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl)SO 2 C 1 -C 6 alkyl, —S(O)(C 1 -C 6 alkyl), —S(O)N(C 1 -C 6 alkyl) 2 , —N(C 1 -C 6 alkyl)S(O)(C 1 -C 6 alkyl) or —(CH 2 ) p N(C 1 -C 6 alkyl) 2 ;

R 6 is —H, —C 2 -C 6 alkenyl, —C 4 -C 8 cycloalkenyl, —C 2 -C 6 alkynyl, —C 3 -C 8 cycloalkyl, heterocyclyl, aryl, heteroaryl containing 1-5 heteroatoms selected from the group consisting of N, S, P and O, —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 (C 1 -C 6 alkyl), —(C 1 -C 6 alkyl)S(O) 2 R 5 , —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, or —(CHR 5 ) p NR 3 R 4 wherein each alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl is optionally substituted with one or more substituents selected from —OH, halogen, —NO 2 , oxo, —CN, —R 5 , —O(C 1 -C 6 )alkyl, —NH(C 1 -C 6 )alkyl, —N(C 1 -C 6 alkyl) 2 , —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 NHC 1 -C 6 alkyl, —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl)S(O) 2 C 1 -C 6 alkyl, —S(O)R 5 , —S(O)N(C 1 -C 6 alkyl) 2 , —N(C 1 -C 6 alkyl)S(O)R 5 , heterocycle, aryl, or heteroaryl;

and

p is 0, 1, 2, 3, 4, 5, or 6.

2. The compound of claim 1 , wherein X 1 , X 2 , X 3 , and X 4 are each CR 1 .

3. The compound of claim 2 , wherein each R 1 is independently H, halogen, —CF 3 , —OH, —CN, —SO 2 (C 1 -C 3 alkyl), phenyl, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, pyridyl, —C(O)C 1 -C 3 alkyl, —OC 1 -C 3 alkyl, —(C 1 -C 3 alkyl)O(C 1 -C 3 alkyl), —OCF 3 or —OCH 2 phenyl.

4. The compound of claim 3 , wherein each R 1 is independently H or halogen.

5. The compound of claim 1 , wherein R 6 is H, —(CHR 5 ) p NR 3 R 4 , or —C 1 -C 6 alkyl optionally substituted with one or more substituents selected from —OH, halogen, —NO 2 , oxo, —CN, —R 5 , —O(C 1 -C 6 )alkyl, —NH(C 1 -C 6 )alkyl, —N(C 1 -C 6 alkyl) 2 , —S(O) 2 N(C 1 -C 6 alkyl) 2 , —S(O) 2 NHC 1 -C 6 alkyl, —C(O)C 1 -C 6 alkyl, —C(O)OC 1 -C 6 alkyl, —N(C 1 -C 6 alkyl)S(O) 2 C 1 -C 6 alkyl, —S(O)R 5 , —S(O)N(C 1 -C 6 alkyl) 2 , or —N(C 1 -C 6 alkyl)S(O)R 5 .

6. The compound of claim 5 , wherein R 6 is H.

7. A compound selected from

8. The compound of claim 7 , wherein the compound is selected from:

9. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier.

10. A pharmaceutical composition comprising a compound of claim 7 , or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier.

11. A pharmaceutical composition comprising a compound of claim 8 , or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier.

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 Dec 3, 2018
From: LEE, JENNIFER; BARCZAK, NICHOLAS; CONTI, CHIARA; ESCOBEDO, JAIME A.; HAN, BINGSONG; LANCIA, DAVID R., JR; LIU, CUIXIAN; MARTIN, MATTHEW W.; NG, PUI YEE; RUDNITSKAYA, ALEKSANDRA; THOMASON, JENNIFER R.; ZHENG, XIAOZHANG
To: FORMA THERAPEUTICS, INC.
Reel/Frame 047660/0510 →
Continuity (5)
Continuation 15789869 · Oct 20, 2017
Provisional Application 62410767 · Oct 20, 2016
Provisional Application 62410766 · Oct 20, 2016
Provisional Application 62410768 · Oct 20, 2016
Related Publication 20190084945A1 · Mar 21, 2019
Cited By (1)
US 12,479,807