首页> 外国专利> USE OF 2-ALPHA-CYANO-4-ALPHA, 5-ALPHA-EPOXYANDROSTAN-17-BETA-OL-3-ONE DERIVATIVES FOR LOWERING LEVELS OF SERUM CORTISOL AND FOR THE TREATMENT OF CLINICAL CONDITIONS ASSOCIATED THEREOF

USE OF 2-ALPHA-CYANO-4-ALPHA, 5-ALPHA-EPOXYANDROSTAN-17-BETA-OL-3-ONE DERIVATIVES FOR LOWERING LEVELS OF SERUM CORTISOL AND FOR THE TREATMENT OF CLINICAL CONDITIONS ASSOCIATED THEREOF

机译:2-α-氰基-4-α,5-α-环氧雄酮-17-BETA-OL-3-ONE衍生物用于降低血清皮质醇水平和治疗相关的临床状况

摘要

Use of a compound of formula (I) or a 3-enol C1-4 alkanoate ester thereof inthe manufacture of a medicament for the intermittent treatment of a conditionof a human or non-human mammal in which said mammal has an abnormally highserum concentration of an adrenal hormone: Wherein R1, R2, R5, and R6 are thesame or different and each is hydrogen or C1 to 4 alkyl; R3 is hydrogen, C1 to4 alkyl, C1 to 4 alkenyl or C1 to 4 alkynyl; R4, is hydroxy, C1 to 4alkanoyloxy, a group of formula (II) or (III) Wherein R7 is (CH2)n, where n isan integer of from 0 to 4, R8 is hydrogen, C1 to 4 alkyl, hydroxy or NH2 andR9 and R10 are the same or different and each is hydrogen or C1 to 4 Alkyl; orR3 and R4 together are oxo, ethylenedioxy or propylenedioxy. The invention haspractical benefits for the treatment of man and other animals with diseasesassociated with abnormal production of adrenal steroids. The invention alsoshows that sustained suppression of the adrenal hormones is not required toachieve relief of symptoms in these conditions.
机译:式(I)的化合物或其3-烯醇式C1-4链烷酸酯的用途间歇性疾病治疗药物的生产人类或非人类哺乳动物的特征,其中所述哺乳动物异常高肾上腺激素的血清浓度:其中R1,R2,R5和R6为相同或不同,各自为氢或C 1-4烷基; R3是氢,C1为4个烷基,C 1-4烯基或C 1-4炔基; R4是羟基,C1至4烷酰氧基,式(II)或(III)的基团,其中R 7为(CH 2)n,其中n为0至4的整数,R8是氢,C1至4烷基,羟基或NH2,并且R9和R10相同或不同,分别为氢或C1-4烷基。要么R3和R4一起是氧代,乙二氧基或丙二氧基。本发明具有治疗人类和其他动物疾病的实际好处与肾上腺类固醇异常产生有关。本发明也表明不需要持续抑制肾上腺激素在这些情况下可以缓解症状。

著录项

  • 公开/公告号CA2443633C

    专利类型

  • 公开/公告日2010-06-22

    原文格式PDF

  • 申请/专利权人 STEGRAM PHARMACEUTICALS LIMITED;

    申请/专利号CA20022443633

  • 发明设计人 WOOD CHRISTOPHER;MARGETTS GEORGE;

    申请日2002-04-09

  • 分类号A61K31/56;A61K31/57;A61K31/575;A61K31/58;A61P5/46;

  • 国家 CA

  • 入库时间 2022-08-21 18:42:46

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