Activators of class I histone deacetlyases (HDACS) and uses thereof
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-487/04
C07C-219/28
C07D-307/52
C07D-405/12
C07D-409/12
C07C-217/58
C07D-411/12
C07D-307/40
출원번호
US-0554670
(2012-07-20)
등록번호
US-9115053
(2015-08-25)
발명자
/ 주소
Tsai, Li-Huei
Pan, Ling
Haggarty, Stephen J.
Patnaik, Debasis
출원인 / 주소
Massachusetts Institute of Technology
대리인 / 주소
Wolf, Greenfield & Sacks, P.C.
인용정보
피인용 횟수 :
1인용 특허 :
59
초록▼
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 pr
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).
대표청구항▼
1. A compound of Formula (C-VII): or a pharmaceutically acceptable salt, tautomer, stereoisomer, or prodrug thereof, wherein: each instance of RC1 and RC2 is independently selected from the group consisting of halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substit
1. A compound of Formula (C-VII): or a pharmaceutically acceptable salt, tautomer, stereoisomer, or prodrug thereof, wherein: each instance of RC1 and RC2 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, —ORC2a, —N(RC2b)2, —SRC2a, —C(═O)RC2a, —C(═O)ORC2a, —C(═O)SRC2a, —C(═O)N(RC2b)2, —OC(═O)RC2a, —OC(═O)ORC2a, —OC(═O)SRC2a, —OC(═O)N(RC2b)2, —NRC2bC(═O)RC2b, —NRC2bC(═O)ORC2a, —NRC2bC(═O)SRC2a, —NRC2bC(═O)N(RC2b)2, —SC(═O)RC2a, —SC(═O)ORC2a, —SC(═O)SRC2a, —SC(═O)N(RC2b)2, —C(═NRC2b)RC2a, —C(═NRC2b)ORC2a, —C(═NRC2b)SRC2a, —C(═NRC2b)N(RC2b)2, —OC(═NRC2b)RC2a, —OC(═NRC2b)ORC2a, —OC(═NRC2b)SRC2a, —OC(═NRC2b)N(RC2b)2, —NRC2bC(═NRC2b)RC2b, —NRC2bC(═NRC2b)ORC2a, —NRC2bC(═NRC2b)SRC2a, —NRC2bC(═NRC2b)N(RC2b)2, —SC(═NRC2b)RC2a, —SC(═NRC2b)ORC2a, —SC(═NRC2b)SRC2a, —SC(═NRC2b)N(RC2b)2, —C(═S)RC2a, —C(═S)ORC2a, —C(═S)SRC2a, —C(═S)N(RC2b)2, —OC(═S)RC2a, —OC(═S)ORC2a, —OC(═S)SRC2a, —OC(═S)N(RC2b)2, —NRC2bC(═S)RC2b, —NRC2bC(═S)ORC2a, —NRC2bC(═S)SRC2a, —NRC2bC(═S)N(RC2b)2, —SC(═S)RC2a, —SC(═S)ORC2a, —SC(═S)SRC2a, —SC(═S)N(RC2b)2, —S(═O)RC2a, —SO2RC2a, —NRC2bSO2RC2a, —SO2N(RC2b)2, —CN, —SCN, and —NO2, wherein each occurrence of RC2a 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 RC2b 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 RC2b groups are joined to form an optionally substituted heterocyclic ring;q is 0, 1, 2, 3, or 4; andv 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 RC1 is C1-6 alkyl. 6. The compound of claim 1, wherein at least one RC1 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 RC2 is halogen. 10. The compound of claim 1, wherein at least one RC2 is —ORC2a. 11. The compound of claim 10, wherein RC2a is hydrogen. 12. The compound of claim 1, wherein v is 1.
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