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    • 10. 发明授权
    • 20-fluoro-17(20)-vinyl steroids
    • 20-氟-17(20) - 乙烯基类固醇
    • US06413951B2
    • 2002-07-02
    • US09886818
    • 2001-06-21
    • Norton P. PeetPhilip M. WeintraubJoseph P. BurkhartCynthia A. Gates
    • Norton P. PeetPhilip M. WeintraubJoseph P. BurkhartCynthia A. Gates
    • A61K3156
    • C07J13/007
    • The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formulae:
    • 本发明涉及20和xgr-氟孕烷-4,17(20) - 二烯-21-蓖麻油酸乙酯,20&xgr-氟-3β-羟基孕烯-5,17(20) - 二烯-21-酸 (20) - 二烯-3-酮,20和xgr-氟孕烷-5,17(20) - 二烯-3β,21-二醇及相关化合物,并与 掺入这些化合物的组合物以及C17,20裂解酶,5α-还原酶和C17-羟化酶的抑制,以及这些化合物在治疗雄激素和雌激素介导或依赖性疾病(包括良性前列腺增生症,前列腺癌)中的用途 ,乳腺癌和DHT介导的疾病如痤疮和多毛症。 还包括治疗与过度合成皮质醇有关的疾病,例如库欣综合征。 雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。 本发明化合物具有以下通式: