Invention Grant
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
- Patent Title: C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
- Patent Title (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
-
Application No.: US11817550Application Date: 2006-03-02
-
Publication No.: US07875599B2Publication Date: 2011-01-25
- Inventor: Angela Brodie , Vincent Njar
- Applicant: Angela Brodie , Vincent Njar
- Applicant Address: US MD Baltimore
- Assignee: University of Maryland
- Current Assignee: University of Maryland
- Current Assignee Address: US MD Baltimore
- Agency: Wilson Sonsini Goodrich & Rosati
- International Application: PCT/US2006/007143 WO 20060302
- International Announcement: WO2006/093993 WO 20060908
- Main IPC: A61K31/58
- IPC: A61K31/58
Abstract:
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.
Public/Granted literature
Information query
