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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
    C-17-杂芳基甾族CYP17抑制剂/抗雄激素，体外生物活性，药代动力学和抗肿瘤活性

    公开(公告)号：US07875599B2

    公开(公告)日：2011-01-25

    申请号：US11817550

    申请日：2006-03-02

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： A61K31/58

    CPC分类号： 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 CYP 17 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，以及野生型和突变体雄激素受体（AR）的有效拮抗剂。 该化合物可用于治疗人类前列腺癌。

    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
    新型C-17-杂芳基类甾体Cyp17抑制剂/抗雄激素，体外生物活性，药代动力学和抗肿瘤活性

    公开(公告)号：US20100048914A1

    公开(公告)日：2010-02-25

    申请号：US12577096

    申请日：2009-10-09

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： C07D235/12

    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 CYP 17 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，以及野生型和突变体雄激素受体（AR）的有效拮抗剂。 该化合物可用于治疗人类前列腺癌。

    Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
    3.
    发明申请
    Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity 审中-公开

    公开(公告)号：US20100048912A1

    公开(公告)日：2010-02-25

    申请号：US12577091

    申请日：2009-10-09

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： C07D235/12

    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.

    ANDROGEN RECEPTOR INACTIVATION CONTRIBUTES TO ANTITUMOR EFFICACY OF CYP17 INHIBITORS IN PROSTATE CANCER
    8.
    发明申请
    ANDROGEN RECEPTOR INACTIVATION CONTRIBUTES TO ANTITUMOR EFFICACY OF CYP17 INHIBITORS IN PROSTATE CANCER 审中-公开
    雄激素受体灭活对CYP17抑制剂在前列腺癌中的抗肿瘤效果的贡献

    公开(公告)号：US20110105445A1

    公开(公告)日：2011-05-05

    申请号：US12921932

    申请日：2009-03-12

    申请人： Vincent C.O. Njar ,  Angela Brodie

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

    IPC分类号： A61K31/58 ,  A61P35/00

    CPC分类号： A61K31/58 ,  A61K31/568

    摘要： Provided are methods of inhibiting CYP17 in a mammal, such as a human, that include administering an effective amount of at least one CYP17 inhibitor, such as VN/124-1, VN/125-1, VN/85-1, VN/87-1 and/or VN/108-1 to the mammal. Also provided are methods of down regulating androgen receptor (AR) protein expression and methods of antagonizing AR in a mammal that include administering to the mammal an effective amount of at least one active ingredient selected from VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Also provided are methods of treating prostate cancer and methods of suppressing or preventing prostate tumor growth by administering such compounds to a mammal.

    摘要翻译： 提供了抑制哺乳动物（例如人）中的CYP17的方法，其包括施用有效量的至少一种CYP17抑制剂，例如VN / 124-1，VN / 125-1，VN / 85-1，VN / 87-1和/或VN / 108-1。 还提供了下调哺乳动物的雄激素受体（AR）蛋白表达和拮抗AR的方法，其包括向哺乳动物施用有效量的至少一种选自VN / 124-1，VN / 125-1的活性成分 ，VN / 85-1，VN / 87-1和VN / 108-1。 还提供了通过向哺乳动物施用这种化合物来治疗前列腺癌的方法和抑制或预防前列腺肿瘤生长的方法。