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    Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens: Synehesis, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
    1.
    发明申请
    Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens: Synehesis, 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：合成，体外生物活性，药代动力学和抗肿瘤活性

    公开(公告)号：US20100137269A1

    公开(公告)日：2010-06-03

    申请号：US12623257

    申请日：2009-11-20

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： A61K31/58 ,  A61K31/56 ,  C07J1/00

    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。

    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：US20100047338A1

    公开(公告)日：2010-02-25

    申请号：US12577090

    申请日：2009-10-09

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： C07J43/00 ,  A61K31/58 ,  A61K9/20 ,  A61K9/48

    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。

    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 有权
    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：US20080280864A1

    公开(公告)日：2008-11-13

    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 ,  C07J43/00 ,  A61P35/00

    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3β-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唑亲核试剂的亲核乙烯基“加成 - 消除”取代反应步骤的方法 以及具有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钯催化交叉偶联反应的方法。 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。

    HDAC inhibitors and hormone targeted drugs for the treatment of cancer
    7.
    发明授权
    HDAC inhibitors and hormone targeted drugs for the treatment of cancer 失效
    HDAC抑制剂和激素靶向药物治疗癌症

    公开(公告)号：US08110550B2

    公开(公告)日：2012-02-07

    申请号：US12134717

    申请日：2008-06-06

    申请人： Angela Brodie ,  Vincent Njar ,  Gauri Sabnis ,  Lalji Gediya

    发明人： Angela Brodie ,  Vincent Njar ,  Gauri Sabnis ,  Lalji Gediya

    IPC分类号： A61P35/00 ,  A61K38/00 ,  A61K39/00 ,  G01N33/574 ,  C07K16/28

    CPC分类号： A61K31/44 ,  A61K31/10 ,  A61K31/196 ,  A61K31/4196 ,  A61K31/495 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy.

    摘要翻译： 本发明涉及例如治疗内分泌调节癌症的方法，包括激素抵抗性癌症。 更具体地，本发明涉及增加激素抵抗性癌症对激素治疗剂的敏感性的方法。 在具体实施方案中，本发明涉及将组蛋白脱乙酰酶抑制剂和激素靶向药物递送至具有癌症的个体。 在具体实施方案中，组蛋白脱乙酰酶抑制剂和激素靶向药物协同作用以治疗癌症，包括克服对癌症治疗的抗性。

    Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
    9.
    发明申请
    Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity 审中-公开
    新型C-17-杂芳基甾体CYP17抑制剂/抗雄激素;合成体外生物活性，药代动力学和抗肿瘤活性

    公开(公告)号：US20100048524A1

    公开(公告)日：2010-02-25

    申请号：US12577092

    申请日：2009-10-09

    申请人： Angela Brodie ,  Vincent Njar

    发明人： Angela Brodie ,  Vincent Njar

    IPC分类号： A61K31/58 ,  C12N5/071 ,  A61P35/00

    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。

    C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
    10.
    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。