The invention related to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-4,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17(20)-dien-3-one, 20&xgr;-fluoropregna-4,17(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: chemistry chemdraw filechemistry mol file展开▼
机译：本发明涉及20-xgr-氟代孕烯-4,17（20）-二烯-3-基-油酸乙酯，20x--氟代三酚-b-羟基丁烯-4,17（20）-dien-21-油酸乙酯，20x-氟-21-羟基孕烯-4,17（20）-dien-3-one，20xgr-氟pregna-4,17（20）-dien-3＆bgr，21-二醇及相关化合物以及掺入这些化合物的组合物，以及对C 17,20 裂解酶，5α-还原酶和C 17 -羟化酶的抑制作用，以及这些化合物的用途在雄激素和雌激素介导或依赖性疾病的治疗中，包括良性前列腺增生，前列腺癌，乳腺癌和DHT介导的疾病，例如痤疮和多毛症。还包括与皮质醇过度合成有关的疾病的治疗，例如库欣氏综合症。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，例如氟他胺的组合疗法。本发明的化合物具有以下通式： <图像文件=“ US20020019548A1-20020214-C00001.GIF” he =“ 118.58805” id =“ EMI-C00001” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 139.22685“ /> 化学化学绘图文件 化学mol文件
展开▼
