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2. 发明申请

WO2005047303A3 NOVEL 17beta HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 审中-公开
标题翻译：新型17β羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：WO2005047303A3
公开(公告)日：2005-08-25
申请号：PCT/EP2004052925
申请日：2004-11-11
申请人： SOLVAY PHARM GMBH
发明人： MESSINGER JOSEF , THOLE HEINRICH-HUBERT , HUSEN BETTINA , VAN STEEN BARTHOLOMEUS JOHANNE , SCHNEIDER GYULA , HULSHOF JOHANNES BERNARDUS EVE , KOSKIMIES PASI , JOHANSSON NINA , ADAMSKI JERZY
IPC分类号： A61K31/565 , C07J1/00
CPC分类号： C07J1/0059 , C07J1/00
摘要： 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 1 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.
摘要翻译：本发明涉及将17β-羟基类固醇脱氢酶I型（17β-HSD1）的抑制性化合物与其盐形成含有这些化合物的药物制剂的新型3,15取代的雌酮衍生物以及这些化合物的制备方法。此外，本发明涉及所述新型3,15取代的雌酮衍生物的治疗用途，特别是其用于治疗或预防类固醇激素依赖性疾病或病症（例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症） I型酶和/或需要降低内源性17β-雌二醇浓度。此外，本发明涉及选择性17β-羟类固醇脱氢酶1型抑制剂的一般用途，其具有对雌激素受体没有或仅有纯的拮抗性结合亲和力，用于治疗和预防良性妇科疾病，特别是子宫内膜异位症。

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