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11 条记录 (耗时 0.02 秒)

    Anticancer agents and use
    2.
    发明授权
    Anticancer agents and use 失效
    抗癌剂及用途

    公开(公告)号：US07737134B2

    公开(公告)日：2010-06-15

    申请号：US11544474

    申请日：2006-10-06

    申请人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    发明人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    IPC分类号： A01N43/00 ,  A61K31/33 ,  C07D513/00

    CPC分类号： C07D513/08 ,  C07D277/28 ,  C07D277/56

    摘要： Provided herein are compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drug mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evaluation of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.

    摘要翻译： 本文提供了组合物，所有相关的立体异构体以及作为百日咳胺A的简化类似物提供的药学上可接受的盐，其中类似物通常缺少C3-氨基和C5-甲基，也称为脱甲基，脱氨基 - 胺甲胺 合适的类似物通过本文所述的用于百日咳胺A的新型药物作用机制体内和体外提供抗癌和抗增殖作用，包括抑制eIF4A依赖性翻译起始。 如同本文所述的胺甲胺A，合适的类似物引起细胞周期停滞或诱导转化细胞中的细胞凋亡。 然而，这些化合物对生长缓慢的正常细胞的毒性低。 此外，类似物类似物，如百草胺A，靶翻译起始因子，并且可用作有需要的受试者中的抗癌和抗增殖剂。 此外，类似物，如数位胺A，是用于评估真核翻译起始的有价值的分子探针，以及用于开发改良抗癌剂的铅化合物。

    Potent immunosuppressive agents, derivatives and uses
    4.
    发明授权
    Potent immunosuppressive agents, derivatives and uses 有权
    强效免疫抑制剂，衍生物和用途

    公开(公告)号：US08841285B2

    公开(公告)日：2014-09-23

    申请号：US12813858

    申请日：2010-06-11

    申请人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    发明人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    IPC分类号： A61K31/33 ,  C07D291/00

    CPC分类号： C07D513/08 ,  C07D277/28 ,  C07D277/56

    摘要： Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evaluation of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.

    摘要翻译： 本文提供的组合物，所有相关立体异构体以及作为百日咳胺A的简化类似物提供的药学上可接受的盐，其中类似物通常缺少C3-氨基和C5-甲基，也称为去甲基脱氨基 - 胺甲胺A 合适的类似物在体内和体外通过本文所述的用于百日咳素A的新药作用机制提供抗癌和抗增殖作用，包括eIF4A依赖性翻译启动的抑制。 如同本文所述的胺甲胺A，合适的类似物引起细胞周期停滞或诱导转化细胞中的细胞凋亡。 然而，这些化合物对生长缓慢的正常细胞的毒性低。 此外，类似物类似物，如百草胺A，靶翻译起始因子，并且可用作有需要的受试者中的抗癌和抗增殖剂。 此外，类似物，如数位胺A，是用于评估真核翻译起始的有价值的分子探针，以及用于开发改良抗癌剂的铅化合物。

    POTENT IMMUNOSUPPRESSIVE AGENTS, DERIVATIVES AND USES
    7.
    发明申请
    POTENT IMMUNOSUPPRESSIVE AGENTS, DERIVATIVES AND USES 有权
    POTENT免疫抑制剂，衍生物和用途

    公开(公告)号：US20110053994A1

    公开(公告)日：2011-03-03

    申请号：US12813858

    申请日：2010-06-11

    申请人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    发明人： Daniel Romo ,  Jun Liu ,  Nam Song Choi ,  Zonggao Shi ,  Woon-Kai Low ,  Yongjun Dang ,  Tilman Schneider-Poetsch

    IPC分类号： A61K31/431 ,  G01N33/50 ,  C07D513/08 ,  A61P35/00

    CPC分类号： C07D513/08 ,  C07D277/28 ,  C07D277/56

    摘要： Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof. Moreover, the analogs, like pateamine A, are valuable molecular probes for evalutaion of eukaryotic translation initiation and as lead compounds for development of improved anticancer agents.

    摘要翻译： 本文提供的组合物，所有相关立体异构体以及作为百日咳胺A的简化类似物提供的药学上可接受的盐，其中类似物通常缺少C3-氨基和C5-甲基，也称为去甲基脱氨基 - 胺甲胺A 合适的类似物在体内和体外通过本文所述的用于百日咳素A的新药作用机制提供抗癌和抗增殖作用，包括eIF4A依赖性翻译启动的抑制。 如同本文所述的胺甲胺A，合适的类似物引起细胞周期停滞或诱导转化细胞中的细胞凋亡。 然而，这些化合物对生长缓慢的正常细胞的毒性低。 此外，类似物类似物，如百草胺A，靶翻译起始因子，并且可用作有需要的受试者中的抗癌和抗增殖剂。 此外，类似物，如胺甲胺A，是用于评价真核翻译起始的有价值的分子探针，也是用于开发改良抗癌剂的铅化合物。