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TETRALONE OR BENZOPYRANONE DERIVATIVES, METHOD OF THEIR SYNTHESIS AND DRUG

机译:替拉酮或苯并吡喃酮衍生物,其合成方法和药物

摘要

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes the novel tetralone or benzopyranone derivatives and method of their synthesis that can be used as therapeutic drug for prophylaxis and treatment of patients with hormone-depending diseases. New tetralone and benzopyranone derivatives have the general formula (I) where each of R1 and R2 means hydrogen atom, hydroxyl-group, alkoxy-group, respectively; each of R3-R7 means hydrogen atom, hydroxyl-group, direct or branched alkyl, alkylhydroxy-group containing 1-6 carbon atoms, halogen atom, amino-group or alkylenedihydroxy-group bound respectively by the point R3 and R4, R4 and R5, R5 and R6 or R6 and R7 and A means methylene-group or oxygen atom. Compounds show inhibiting effect on activity of 17-17-hydroxysteroid dehydrogenase and therefore these derivatives can be used for preparing therapeutic agent used for prophylaxis and/or treatment of patients with androgen- and estrogen-dependent diseases, in part, prostate gland cancer, prostate benign hyperplasia, virilism. breast cancer, mastopathy, uterus cancer, ovary cancer and so on. EFFECT: improved method of synthesis, enhanced anticancer activity of compounds. 4 cl, 3 dwg
机译:领域:有机化学,化学技术,药学。物质:本发明描述了可以用作预防和治疗激素依赖性疾病患者的治疗药物的新型四氢萘酮或苯并吡喃酮衍生物及其合成方法。新的四氢萘酮和苯并吡喃酮衍生物具有通式(I)其中每个R 1 和R 2 分别是指氢原子,羟基和烷氧基; R 3 -R 7 分别表示氢原子,羟基,直链或支链烷基,含1-6个碳原子的烷基羟基,卤素原子,氨基R 3 和R 4 ,R 4 和R 5 ,R分别键合的烷基或亚烷基二羟基 5 和R 6 或R 6 和R 7 ,A表示亚甲基或氧原子。化合物显示出对17-17-羟类固醇脱氢酶活性的抑制作用,因此这些衍生物可用于制备用于预防和/或治疗雄激素和雌激素依赖性疾病(部分是前列腺癌,前列腺癌)的患者的治疗剂。良性增生,男性主义。乳腺癌,乳腺疾病,子宫癌,卵巢癌等。效果:改进的合成方法,增强了化合物的抗癌活性。 4 cl,3 dwg

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