首页> 外国专利> 17-BETA-CYCLOPROPYL(AMINO/OXY) 4-AZA STEROIDS AS ACTIVE INHIBITORS OF TESTOSTERONE 5-ALPHA REDUCTASE AND C17-20-LYASE

17-BETA-CYCLOPROPYL(AMINO/OXY) 4-AZA STEROIDS AS ACTIVE INHIBITORS OF TESTOSTERONE 5-ALPHA REDUCTASE AND C17-20-LYASE

机译:17-BETA-环丙基(氨基/氧)4-AZA甾体作为睾丸甾酮5-α还原酶和C17-20-裂解酶的活性抑制剂

摘要

The invention related to 4-aza-17 beta -(cyclopropoxy)-androst-5 alpha -androstan-3-one, 4-aza-17 beta -(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5 alpha -reductase and C17 alpha -hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis 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 general formula (I).
机译:本发明涉及4-氮杂-17β-(环丙氧基)-rost-5-α-雄烷-3-酮,4-氮杂17β-(环丙基氨基)-androst-4-en-3-one及相关化合物和掺入这些化合物的组合物,以及对C17-20裂合酶,5α-还原酶和C17α-羟化酶的抑制作用,以及这些化合物在雄激素和雌激素介导的疾病(包括良性前列腺增生和雄激素介导的疾病)的治疗中的用途前列腺癌,雌激素介导的乳腺癌以及DHT介导的疾病(例如痤疮)。还包括与皮质醇过度合成有关的疾病,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通式(I)。

著录项

  • 公开/公告号HU9900955A3

    专利类型

  • 公开/公告日2000-06-28

    原文格式PDF

  • 申请/专利权人 HOECHST MARION ROUSSEL INC. CINCINNATI OHIO;

    申请/专利号HU19990000955

  • 发明设计人

    申请日1997-01-09

  • 分类号C07J73/00;A61K31/59;

  • 国家 HU

  • 入库时间 2022-08-22 01:56:13

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