IP Library Granted Patent US 9,115,053
Granted Patent B2
US 9,115,053 · App. 13/554,670 · Granted Aug 25, 2015

Activators of class I histone deacetlyases (HDACS) and uses thereof

Inventors: Li-Huei Tsai (Cambridge, MA); Ling Pan (Charlestown, MA); Stephen J. Haggarty (Dorchester, MA); Debasis Patnaik (Quincy, MA)
Assignees: Massachusetts Institute of Technology; The General Hospital Corporation
C07C219/28C07C217/58C07D307/40C07D307/52C07D405/12C07D409/12C07D411/12C07D487/04
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Quick Facts
Patent No.
US 9,115,053
App. No.
13/554,670
Granted
Aug 25, 2015
Kind
B2
Abstract

The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).

Claims (20)

1. A compound of Formula (C-VII):

or a pharmaceutically acceptable salt, tautomer, stereoisomer, or prodrug thereof, wherein:

each instance of R C1 and R C2 is independently selected from the group consisting of halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —OR C2a , —N(R C2b ) 2 , —SR C2a , —C(═O)R C2a , —C(═O)OR C2a , —C(═O)SR C2a , —C(═O)N(R C2b ) 2 , —OC(═O)R C2a , —OC(═O)OR C2a , —OC(═O)SR C2a , —OC(═O)N(R C2b ) 2 , —NR C2b C(═O)R C2b , —NR C2b C(═O)OR C2a , —NR C2b C(═O)SR C2a , —NR C2b C(═O)N(R C2b ) 2 , —SC(═O)R C2a , —SC(═O)OR C2a , —SC(═O)SR C2a , —SC(═O)N(R C2b ) 2 , —C(═NR C2b )R C2a , —C(═NR C2b )OR C2a , —C(═NR C2b )SR C2a , —C(═NR C2b )N(R C2b ) 2 , —OC(═NR C2b )R C2a , —OC(═NR C2b )OR C2a , —OC(═NR C2b )SR C2a , —OC(═NR C2b )N(R C2b ) 2 , —NR C2b C(═NR C2b )R C2b , —NR C2b C(═NR C2b )OR C2a , —NR C2b C(═NR C2b )SR C2a , —NR C2b C(═NR C2b )N(R C2b ) 2 , —SC(═NR C2b )R C2a , —SC(═NR C2b )OR C2a , —SC(═NR C2b )SR C2a , —SC(═NR C2b )N(R C2b ) 2 , —C(═S)R C2a , —C(═S)OR C2a , —C(═S)SR C2a , —C(═S)N(R C2b ) 2 , —OC(═S)R C2a , —OC(═S)OR C2a , —OC(═S)SR C2a , —OC(═S)N(R C2b ) 2 , —NR C2b C(═S)R C2b , —NR C2b C(═S)OR C2a , —NR C2b C(═S)SR C2a , —NR C2b C(═S)N(R C2b ) 2 , —SC(═S)R C2a , —SC(═S)OR C2a , —SC(═S)SR C2a , —SC(═S)N(R C2b ) 2 , —S(═O)R C2a , —SO 2 R C2a , —NR C2b SO 2 R C2a , —SO 2 N(R C2b ) 2 , —CN, —SCN, and —NO 2 , wherein each occurrence of R C2a is independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl, and each occurrence of R C2b is independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, or a nitrogen protecting group, or two R C2b groups are joined to form an optionally substituted heterocyclic ring;

q is 0, 1, 2, 3, or 4; and

v is 0, 1, 2, or 3;

provided that the compound is not of the formula:

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable excipient.

3. The compound of claim 1 , wherein the compound is of the formula:

or a pharmaceutically acceptable salt, tautomer, stereoisomer, or prodrug thereof.

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

or a pharmaceutically acceptable salt, tautomer, stereoisomer, or prodrug thereof.

5. The compound of claim 1 , wherein at least one R C1 is C 1-6 alkyl.

6. The compound of claim 1 , wherein at least one R C1 is methyl.

7. The compound of claim 1 , wherein q is 0.

8. The compound of claim 1 , wherein q is 1.

9. The compound of claim 1 , wherein at least one R C2 is halogen.

10. The compound of claim 1 , wherein at least one R C2 is —OR C2a .

11. The compound of claim 10 , wherein R C2a is hydrogen.

12. The compound of claim 1 , wherein v is 1.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 16, 2014
From: TSAI, LI-HUEI; PAN, LING
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 032681/0759 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2014
From: HAGGARTY, STEPHEN J.; PATNAIK, DEBASIS
To: THE GENERAL HOSPITAL CORPORATION D/B/A MASSACHUSETTS GENERAL HOSPITAL
Reel/Frame 032659/0533 →
CONFIRMATORY LICENSE Recorded Aug 22, 2012
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 028826/0127 →
Continuity (2)
Provisional Application 61510885 · Jul 22, 2011
Related Publication 20130096129A1 · Apr 18, 2013