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发明授权
CN1878786B 新的I型17β-羟化类固醇脱氢酶抑制剂 失效 - 权利终止

新的I型17β-羟化类固醇脱氢酶抑制剂
摘要：
本发明涉及作为I型17β-羟化类固醇脱氢酶(17β-HSD1)抑制化合物的新的3,15取代的雌酮衍生物，它们的盐，含这些化合物的药物制剂以及这些化合物的制备方法。此外，本发明还涉及所述新的3,15取代的雌酮衍生物的治疗应用，尤其在治疗或预防类固醇激素依赖性疾病或病症，例如需要抑制I型17β-羟化类固醇脱氢酶和/或需要降低内源性17β-雌二醇浓度的类固醇激素依赖性疾病或病症中的应用。另外，本发明涉及选择性I型17β-羟化类固醇脱氢酶抑制剂的一般用途，它另外对雌激素受体不具有或仅具有单纯的拮抗结合亲和力，以治疗和预防良性妇科疾病，尤其是子宫内膜异位。
摘要（英）：

The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17beta-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17beta-estradiol concentration. In addition, the present invention relates to the general use of selective 17beta-hydroxysteroid dehydrogenase type I inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.

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