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-环氧雄烷-17-β-醇-3-酮衍生物在降低血清皮质醇水平和治疗与其相关的临床病症中的用途

摘要

Disclosed herein is a use of a compound of formula (I) or a 3-enol C1-4 alkanoate ester thereof in the manufacture of a medicament for effecting endocrinological cure, without extirpation of the source of increased cortisol production, of a condition selected from Alopecia X in dogs, laminitis in horses, Cushing's Syndrome, pseudo-Cushing's Syndrome, hypercortisolaemia associated with insulin dependant diabetes, hypercortisolaemia associated with aging, or hypercortisolaemia associated with depression, schizophrenia, Alzheimer's disease, Parkinson's disease, alcoholism, anorexia nervosa, bulimia or addiction, wherein R1, R2, R5, and R6 are the same or different and each is hydrogen or C1 to 4 alkyl; R3 is hydrogen, C1 to 4 alkyl, C1 to 4 alkenyl or C1 to 4 alkynyl; R4, is hydroxy, C1 to 4 alkanoyloxy, a group of formula (II) or (III) Wherein R7 is (CH2)n, where n is an integer of from 0 to 4, R8 is hydrogen, C1 to 4 alkyl, hydroxy or NH2 and R9 and R10 are the same or different and each is hydrogen or C1 to 4 alkyl; or R3 and R4 together are oxo, ethylenedioxy or propylenedioxy. These medicaments are for the treatment of man and other animals with diseases associated with abnormal production of adrenal steroids. The use of these medicaments also shows that sustained suppression of the adrenal hormones is not required to achieve relief of symptoms in these conditions.
机译:本文公开了式(I)的化合物或其3-烯醇式C1-4链烷酸酯在制备用于内分泌治疗的药物中的用途,所述内分泌治疗选自以下条件:犬X型脱发症,马椎板炎,库欣综合症,假库欣综合症,与胰岛素依赖型糖尿病相关的高皮质醇血症,与衰老相关的高皮质醇血症或与抑郁症,精神分裂症,阿尔茨海默氏病,帕金森氏病,酒精中毒,厌食症或神经性厌食症相关的高皮质醇血症R 1,R 2,R 5和R 6相同或不同,且各自为氢或C 1-4烷基; R 3为氢,C 1-4烷基,C 1-4烯基或C 1-4炔基; R 4是羟基,C 1-4烷氧基,式(II)或(III)的基团,其中R 7是(CH 2)n,其中n是0至4的整数,R 8是氢,C 1-4烷基,羟基NH 2与R 9和R 10相同或不同,分别为氢或C 1-4烷基;或或R 3和R 4一起是氧代,乙二氧基或丙二氧基。这些药物用于治疗患有与肾上腺类固醇异常产生有关的疾病的人和其他动物。这些药物的使用还表明,在这些情况下,不需要持续抑制肾上腺激素即可缓解症状。

著录项

  • 公开/公告号NZ529141A

    专利类型

  • 公开/公告日2005-09-30

    原文格式PDF

  • 申请/专利权人 STEGRAM PHARMACEUTICALS LIMITED;

    申请/专利号NZ20020529141

  • 发明设计人 WOOD CHRISTOPHER;MARGETTS GEORGE;

    申请日2002-04-09

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

  • 国家 NZ

  • 入库时间 2022-08-21 22:16:53

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