发明授权
US07875599B2 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
- 专利标题： C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
- 专利标题（中）： 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
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申请号： US11817550申请日： 2006-03-02
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公开(公告)号： US07875599B2公开(公告)日： 2011-01-25
- 发明人: Angela Brodie , Vincent Njar
- 申请人： Angela Brodie , Vincent Njar
- 申请人地址： US MD Baltimore
- 专利权人： University of Maryland
- 当前专利权人： University of Maryland
- 当前专利权人地址： US MD Baltimore
- 代理机构： Wilson Sonsini Goodrich & Rosati
- 国际申请： PCT/US2006/007143 WO 20060302
- 国际公布： WO2006/093993 WO 20060908
- 主分类号： A61K31/58
- IPC分类号： A61K31/58
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.
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