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    NOVEL MOLECULES THAT SELECTIVELY INHIBIT HISTONE DEACETYLASE 6 RELATIVE TO HISTONE DEACETYLASE 1
    6.
    发明公开
    NOVEL MOLECULES THAT SELECTIVELY INHIBIT HISTONE DEACETYLASE 6 RELATIVE TO HISTONE DEACETYLASE 1 审中-公开
    的新分子FOR组蛋白脱乙酰6的相对于组蛋白脱乙酰1选择性抑制

    公开(公告)号：EP2763531A1

    公开(公告)日：2014-08-13

    申请号：EP12838935.0

    申请日：2012-10-03

    申请人： The Trustees of Columbia University in the City of New York ,  Sloan Kettering Institute For Cancer Research

    发明人： BRESLOW, Ronald ,  MARKS, Paul, A.

    IPC分类号： A01N37/18

    CPC分类号： C07C259/10 ,  C07C259/06 ,  C07C275/64 ,  C07C2602/10 ,  C07D209/08 ,  C07D209/18 ,  C07D209/24 ,  C07D209/42 ,  C07D215/06 ,  C07D215/40 ,  C07D235/06

    摘要： This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(═O)—R6, —NH—C(═O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(═S)R7, —C(═O)—NR5R6, —CH2—C(═O)—NR5R6, —C(═NR5)R6, —P(═O)(OR5)(OR6), —P(OR5)(OR6), —C(═S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(═O)OR8, C(═O)R8, —C(═O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or absent, and when present is —O—, —S—, —CH2—, —C(O)——NH—, —NH—NH—, —NHC(═O)—, —C(═O)NH—, —NHC(═O)CH2NH—, —NHC(═O)CH2C(═O)—, —N(OH)—, —CH2CH2— or —NHC(═O)CH═CH—; and R4 is alkyl, —OR11 or —NH—OR11, wherein R11 is H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, aryl, heteroaryl, or heterocyclyl, and when Q is —Ar1—Z—, Z is absent, Ar1 is phenyl, R2 and R3 are H, n=1, and R4 is —NHOH, then R1 is other than carbazole, tetrahydro-&bgr;-carboline, tetrahydro-γ-carboline, —C(═O)—NR5R6 and —NR5—C(═O)—R6, wherein one of R5 or R6 is quinoline and the other of R5 or R6 is H; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供具有以下结构的化合物：其中R1是H，卤素，-NR 5 R 6，-NR 5 C（= O）-R 6，-NH-C（= O）-OR 7，-OR 7，-NO 2，-CN， -SR 7，-SO 2 R 7，-CO 2 R 7，CF 3，-SOR7，-POR7，-C（= S）R 7，-C（= O）-NR 5 R 6，-CH 2 -C（= O）-NR5R6，（-C═NR5 （）R 6，-P = O）（OR 5）（OR 6），P（OR 5）（OR 6）， - C（= S）R 7，C 1-5烷基，C 2-5烯基，C 2-5炔基，芳基， 杂芳基，或杂环基，worin R5，R6，和R7和各自独立地为H，C 1-5烷基，C 2-5烯基，C 2-5炔基，杂烷基，环烷基，杂环，芳基或杂芳基; m是从0至2的整数; R2和R3是各自独立地为H，卤素，-NH 2，-CX 3，-C（= O）OR 8，C（= O）R8，-C（= O）NR 9 R 10，C 1-10烷基，C 2-10烯基 ，C 2-10炔基，杂烷基，芳基，杂芳基，或杂环基; 其中X是Cl，Br或F; R8，R9和R10各自独立地为H，C 1-5烷基，C 2-5烯基，C 2-5炔基，杂烷基，环烷基，杂环，芳基或杂芳基; Q是-Ar1-Z或-Z-AR1-Z，worin Ar 1是芳基或杂芳基; 和Z在每次出现时独立地为存在或不存在，并且当存在时是-O - ， - S - ， - CH 2 - ， - C（O） - NH - ， - NH-NH - ， - NHC（= O） - ，-C（= O）NH-，-NHC（= O）CH 2 NH-，-NHC（= O）CH 2 C（= O） - ， - N（OH） - ，-CH 2 CH 2或-NHC（= O）CH = CH-; 且R 4是烷基，-OR 11或-NH-OR11，R11 worin是H，C 1-10烷基，C 2-10烯基，C 2-10炔基，芳基，杂芳基，或杂环基，并且当Q是-Ar1-Z-， Z不存在; Ar 1为苯基，R 2和R 3是H，n = 1时，R4为-NHOH，那么R 1不是咔唑，四氢-β-咔啉，四氢γ咔啉，-C其他（= O） -NR5R6和-NR 5 C（= O）-R 6，worin R5或R6中的一个是喹啉和其它R5或R6是H; 或其药学上可接受的盐。