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    • 9. 发明授权
    • Histone deacetylase inhibitors
    • 组蛋白脱乙酰酶抑制剂
    • US07399884B2
    • 2008-07-15
    • US11557402
    • 2006-11-07
    • Jerome C. BressiSheldon X. CaoJeffrey A. StaffordPhong H. Vu
    • Jerome C. BressiSheldon X. CaoJeffrey A. StaffordPhong H. Vu
    • C07C259/04C07C229/34C07D231/16C07D239/22C07D241/36
    • C07C259/06C07D231/16C07D239/38C07D241/44
    • Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen;R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl;M is a substituent capable of complexing with a protein metal ion; andL is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
    • 提供组蛋白脱乙酰酶抑制剂及其用途,其具有以下通式:其中R 1,R 2,R 3和R 4, / SUB>各自独立地选自氢,取代或未取代的直链C 1-12烷基,C 2-12-12氨基烷基或C 1 -C 12烷基, 2-12个氧杂烷基,以及取代和未取代的3,4,5,6,7或8元环,条件是R 3和R 4 不是氢; R 5选自羰基,取代或未取代的C 1-3烷基,取代或未取代的C 1-3烷基, 烷基-C(O),取代或未取代的-C(O)-C 1-3烷基和取代或未取代的-C(O)C(O)C 1-3烷基; M是能与蛋白质金属离子络合的取代基; L是包含连接M取代基与L取代基的α原子的3-12个原子的链的取代基。