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199 条记录 (耗时 0.067 秒)

    N-substituted tetrahydroisoquinoline benzamides/benzene sulfonamides as anti-cancer agents
    43.
    发明授权
    N-substituted tetrahydroisoquinoline benzamides/benzene sulfonamides as anti-cancer agents 有权
    N-取代四氢异喹啉苯甲酰胺/苯磺酰胺作为抗癌剂

    公开(公告)号：US08889713B1

    公开(公告)日：2014-11-18

    申请号：US13960886

    申请日：2013-08-07

    申请人： Florida A&M University

    发明人： Kinfe Ken Redda ,  Madhavi Gangapuram

    IPC分类号： C07D217/08 ,  A61K31/472 ,  C07D417/12

    CPC分类号： C07D217/08 ,  C07D417/12

    摘要： The compounds herein disclosed are N-substituted tetrahydroisoquinoline benzamide and benzene sulfonamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6- to 10-fold less than the IC50 of Tamoxifen.

    摘要翻译： 本文公开的化合物是通过引入具有各种电子性质的基团在苯环上具有修饰的N-取代的四氢异喹啉苯甲酰胺和苯磺酰胺化合物。 N-取代的四氢异喹啉化合物的这些衍生物已被证明对细胞具有抗增殖活性。 特别地，发现这些化合物在抑制癌细胞（例如起源于乳腺组织的癌细胞）的增殖方面是有效的。 另外，已经显示新化合物对乳腺癌细胞的IC 50值比他莫昔芬的IC50低6-10倍。

    N- (2 -AMINOPHENYL) BENZAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
    45.
    发明申请
    N- (2 -AMINOPHENYL) BENZAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
    N-（2-氨基苯基）苯甲酸衍生物作为脱乙酰壳多糖酶抑制剂

    公开(公告)号：US20140135327A1

    公开(公告)日：2014-05-15

    申请号：US14130703

    申请日：2012-07-06

    申请人： Ronald Ernest Grigg ,  Martyn Inman ,  Graham Packham

    发明人： Ronald Ernest Grigg ,  Martyn Inman ,  Graham Packham

    IPC分类号： C07D413/06 ,  C07D401/06 ,  C07D217/14 ,  C07D217/16 ,  G01N33/50 ,  C07D217/24

    CPC分类号： C07D413/06 ,  C07D217/08 ,  C07D217/14 ,  C07D217/16 ,  C07D217/24 ,  C07D401/06 ,  G01N33/5008

    摘要： This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.

    摘要翻译： 本发明涉及具有HDAC抑制活性的新化合物或其药学上可接受的盐的发现。 特别地，本发明的化合物显示对I类HDAC酶的选择性，因此预期其可用于其抗增殖活性和治疗人或动物体的方法，例如用于预防或抑制肿瘤生长和 癌转移。 本发明还涉及制备本文定义的化合物或其药学上可接受的盐的方法，其含有它们的药物组合物及其在制备药物中的用途，所述药物用于在温暖的生产中产生抗增殖作用， 流血的动物如人。