Gossypol co-crystals and the use thereof
    72.
    发明授权
    Gossypol co-crystals and the use thereof 有权
    棉酚共晶及其用途

    公开(公告)号:US07432300B2

    公开(公告)日:2008-10-07

    申请号:US11818766

    申请日:2007-06-15

    CPC classification number: A61K31/11

    Abstract: This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

    Abstract translation: 本发明涉及包含( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体的组合物,其可用作 Bcl-2家族蛋白。 本发明还涉及( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体用于诱导细胞凋亡 细胞和致敏细胞诱导凋亡细胞死亡。

    ErbB-2 selective small molecule kinase inhibitors
    73.
    发明授权
    ErbB-2 selective small molecule kinase inhibitors 失效
    ErbB-2选择性小分子激酶抑制剂

    公开(公告)号:US07427689B2

    公开(公告)日:2008-09-23

    申请号:US10343267

    申请日:2001-07-30

    CPC classification number: A61K31/216 A61K31/00 A61K31/192

    Abstract: A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.

    Abstract translation: 化合物的erbB-2激酶抑制的新方法通过计算建模和数据处理鉴定,和/或合理和从头药物设计提供了化合物结合erbB-2激酶分子,并且其可以用作erbB-2激酶激动剂或拮抗剂 。 这些化合物特别用于治疗癌症,特别是乳腺癌,并且可以单独使用或与其它化学治疗剂,特别是与赫氏原,人源化抗HER-2抗体或放射治疗组合使用。 例示的具体化合物是“化合物B17”=甲基 - (对硝基苯基)-2-丙炔酸酯。

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