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    C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
    1.
    发明授权
    C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity 有权

    公开(公告)号：US10098896B2

    公开(公告)日：2018-10-16

    申请号：US15159117

    申请日：2016-05-19

    申请人： The University of Maryland, Baltimore

    发明人： Angela Brodie ,  Vincent C. O. Njar

    IPC分类号： A61K31/58 ,  C07J43/00

    摘要： Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

    NOVEL C-17-HETEROARYL STEROIDAL CYP17 INHIBITORS/ANTIANDROGENS, IN VITRO BIOLOGICAL ACTIVITIES, PHARMACOKINETICS AND ANTITUMOR ACTIVITY
    2.
    发明申请
    NOVEL C-17-HETEROARYL STEROIDAL CYP17 INHIBITORS/ANTIANDROGENS, IN VITRO BIOLOGICAL ACTIVITIES, PHARMACOKINETICS AND ANTITUMOR ACTIVITY 审中-公开
    新C-17-异氟醚CYP17抑制剂/抗生素，体外生物活性，药物动力学和抗肿瘤活性

    公开(公告)号：US20140288036A1

    公开(公告)日：2014-09-25

    申请号：US14081910

    申请日：2013-11-15

    申请人： the University of Maryland, Baltimore

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： C07J43/00

    CPC分类号： A61K31/58 ,  C07J43/003

    摘要： Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

    摘要翻译： 描述的是甾体C-17苯并唑，嘧啶并唑（氮杂苯并唑）和二嗪。 还描述了它们的合成方法，其包括具有3'-乙酰氧基-17-氯-16-甲酰基雄甾-5,16-二烯或其类似物和苯并唑或嘧啶并咪唑的亲核乙烯基“加成 - 消除”取代反应步骤的方法 亲核试剂和方法具有钯催化的17-碘雄甾-5,16-二烯-3β-醇或其类似物与三丁基甲锡烷基二嗪的交叉偶联反应。 这些化合物是人CYP17酶的有效抑制剂，以及野生型和突变雄激素受体（AR）的有效拮抗剂。 该化合物可用于治疗人类前列腺癌。