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    N-HYDROXYACRYLAMIDE COMPOUNDS
    4.
    发明申请
    N-HYDROXYACRYLAMIDE COMPOUNDS 审中-公开
    N-羟基丙烯酰胺化合物

    公开(公告)号：US20100069388A1

    公开(公告)日：2010-03-18

    申请号：US12517290

    申请日：2007-12-14

    申请人： Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Fumiyuki Shirai

    发明人： Yoshikazu Inoue ,  Yoshiteru Eikyu ,  Fumiyuki Shirai

    IPC分类号： A61K31/5377 ,  C07D211/72 ,  C07D241/02 ,  C07D413/12 ,  A61K31/44 ,  A61K31/4965 ,  A61P3/10

    CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D405/12

    摘要： A compound having the following formula (I): wherein —R1 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with —OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

    摘要翻译： 具有下式（I）的化合物：其中-R 1是氢，任选取代的低级烷基，环（低级）烷基，环（高级）烷基，任选取代的芳基，任选取代的杂环基或芳基稠合的环（低级）烷基 R 2为氢或卤素，Z为CH或N，X为式（II）R 3为可被-OH或任选取代的芳基或低级烷酰基取代的低级烷基，R 4为氢或低级烷基，Y为任选取代的 低级亚烷基或其盐。 该化合物可用作组蛋白脱乙酰酶抑制剂。

    Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
    5.
    发明授权
    Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
    噻唑衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US5371097A

    公开(公告)日：1994-12-06

    申请号：US80051

    申请日：1993-06-22

    申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

    发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P1/04 ,  A61P43/00 ,  C07D277/48 ,  C07D417/04 ,  C07D417/14 ,  C07D521/00

    CPC分类号： C07D417/04 ,  C07D277/48 ,  C07D417/14

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, acylamino, cyclo(lower)alkenylamino having amino and oxo, imido, triazolylamino, benzoisothiazolylamino, wherein each of said heterocyclicamino groups may be substituted by one or more substituent(s) selected from the group consisting of lower alkyl, amino and oxo, 2-cyano-3-lower alkylguanidino, 2-acyl-3-lower alkylguanidino, 2-acylguanidino, (1-lower alkylamino-2-nitrovinyl)amino, hydroxy, halogen, cyano, acyl, benzimidazolylthio, triazolyl substituted with amino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, cyano, or acyl, andR.sup.5 is amino or lower alkoxy,R.sup.2 and R.sup.3 are each hydrogen, acyl or lower alkyl which may have halogen; orR.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen or halogen, andA is lower alkylene, or pharmaceutically acceptable salt thereof.

    摘要翻译： 下式的化合物，其中R 1是氨基，酰氨基，具有氨基和氧代的环（低级）烯基氨基，亚氨基，三唑基氨基，苯并异噻唑基氨基，其中每个所述杂环氨基可以被一个或多个被选择的取代基取代 由2-烷基氨基和氧代低级烷基，2-氰基-3-低级烷基胍基，2-酰基-3-低级烷基胍基，2-酰基胍基，（1-低级烷基氨基-2-硝基乙烯基）氨基，羟基，卤素， 氰基，酰基，苯并咪唑硫基，被氨基取代的三唑基或下式的基团：其中R 4是氢，氰基或酰基，R 5是氨基或低级烷氧基，R 2和R 3各自是氢，酰基或更低级 可以具有卤素的烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢或卤素，A是低级亚烷基或其药学上可接受的盐。