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    Tricyclic hydroxamate and benzaminde derivatives, compositions and methods
    47.
    发明公开
    Tricyclic hydroxamate and benzaminde derivatives, compositions and methods 审中-公开
    Tricyclische Hydroxamat-和Benzamid-Derivate，Zusammensetzungen und Methoden

    公开(公告)号：EP1541549A1

    公开(公告)日：2005-06-15

    申请号：EP03293143.8

    申请日：2003-12-12

    申请人： Exonhit Therapeutics S.A.

    发明人： Leblond, Bertrand ,  Beausoleil, Eric

    IPC分类号： C07C259/10 ,  C07C233/80 ,  C07C259/06 ,  A61K31/167 ,  A61P35/00

    CPC分类号： C07C259/10 ,  C07C233/80 ,  C07C259/06 ,  C07C2602/10

    摘要： The present invention relates to compounds and methods for inhibiting histone deacetylase enzymatic activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit histone deacetylases (HDACs), and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, and also central nervous system diseases. It further deals with processes for preparing said compounds.

    摘要翻译： 本发明涉及抑制组蛋白脱乙酰酶酶活性的化合物和方法。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制组蛋白脱乙酰酶（HDAC），以及在治疗HDAC介导的病症，癌症，增殖性病症 ，牛皮癣以及中枢神经系统疾病。 它还涉及制备所述化合物的方法。

    VERFAHREN ZUR HERSTELLUNG VON N-ALKOXY-N-ALKYLAMIDEN
    48.
    发明授权
    VERFAHREN ZUR HERSTELLUNG VON N-ALKOXY-N-ALKYLAMIDEN 有权
    工艺生产N-烷氧基的N-烷基酰胺

    公开(公告)号：EP1250316B1

    公开(公告)日：2004-12-29

    申请号：EP01913765.2

    申请日：2001-01-24

    申请人： Lonza AG

    发明人： HANSELMANN, Paul ,  HILDBRAND, Stefan ,  STERREN, Etienne

    IPC分类号： C07C259/06 ,  C07C259/10 ,  C07D307/68

    CPC分类号： C07D307/68 ,  C07C259/06 ,  C07C259/10

    摘要： The invention relates to a method for producing N -alkoxy- N -alkylamides of general formula (I), wherein R represents C1-10 alkyl, cyclo-C5-7 alkyl, cyclo-C5-7 alkenyl, C2-10 alkenyl, aryl, aryl C1-3 alkyl, heteroaryl, heteroaryl C1-3 alkyl or heterocyclyl; and R2 represents C1-6 alkyl. The inventive compounds are characterized in that an ester of general formula (II): R COOR , wherein R has the above-mentioned meaning, and R represents C1-6 alkyl, 4-nitrophenyl, 2,4-dinitrophenyl, succinimido or benzotriazole-1-yl, is reacted with hydroxylamine, a hydroxylamine derivative or with a hydroxylammonium salt, and the reaction product is alkylated in the presence of a phase transfer catalyst.