Novel C-17- heteroaryl steroid CYP17 inhibitors / antiandrogens: synthesis, in vitro biological activity, pharmacokinetics and anti-tumor activity

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专利权人:

オブ;ユニバーシティ;メリーランド，ボルティモア;ユニバーシティ オブ メリーランド,ボルティモア

发明人:

ブローディー，アンジェラ,ヌジャー，ビンセント,ブローディー,アンジェラ,ヌジャー,ビンセント

申请号：

JP2007558143

公开号：

JP5130453B2

申请日:

2006.03.02

申请国别(地区):

JP

年份:

2013

代理人:

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 3²-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-3²-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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中国工程科技知识中心

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http://www.ckcest.cn/home/