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STEROID COMPOUND HAVING CONTRACEPTIVE ACTIVITY AND ANTIOSTEOPOROSIS ACTIVITY

机译:具有避孕作用和抗骨质疏松作用的类固醇化合物

摘要

PROBLEM TO BE SOLVED: To obtain the subject new compound consisting of a specific steroid compound, having contraceptive activity and antiosteoporosis activity and useful e.g. for the prevention and treatment of menopausal symptom caused by estrogen deficiency, osteoporosis, arteriosclerosis, Alzheimer's disease, etc. SOLUTION: The objective compound is a new steroid compound expressed by the formula [R3 is =O, OH, =NOR (R is a 1-6C alkyl), OR or OOCR; R6 is H, =CH2 or (CH2 )m H ((m) is 1 or 2); R7 is H, a (substituted)1-4C alkyl, a (substituted)2-4C alkenyl, etc.; R11 is H, a (substituted)1-4C alkyl, a (substituted)1-6C alkylidene, etc.; E forms a 4 to 7-membered ring taking -configuration relative to the ring D together with 16 and 17-site C atoms of the ring D; RE is H, a 1-6C alkyl, a 2-6C alkenyl, OR, SR, etc.; R17 is OH, OCH2 OR, OR, etc.] and is useful e.g. for the prevention and treatment of diseases caused by estrogen deficiency. The compound can be produced by bonding an alkenyl chain to the 16, 17 sites of a 17-ketosteroid of the formula II and cyclizing the product in the presence of a catalyst.
机译:要解决的问题:为了获得主题的新化合物,其由特定的类固醇化合物组成,具有避孕活性和抗骨质疏松活性,并且例如用于预防和治疗由雌激素缺乏,骨质疏松,动脉硬化,阿尔茨海默氏病等引起的更年期症状。解决方案:目标化合物是一种新的类固醇化合物,其化学式为[R3为= O,OH,= NOR(R为1-6C烷基),OR或OOCR; R6为H,= CH2或(CH2)mH((m)为1或2); R 7为H,(取代的)1-4C烷基,(取代的)2-4C烯基等。 R11为H,(取代的)1-4C烷基,(取代的)1-6C亚烷基等。 E相对于环D与环D的16和17位C原子一起形成4至7元环。 RE是H,1-6C烷基,2-6C烯基,OR,SR等。 R 17是OH,OCH 2 OR,OR等],并且例如对R 17是有用的。用于预防和治疗由雌激素缺乏引起的疾病。该化合物可以通过将烯基链键合至式II的17-酮类固醇的16、17位点并在催化剂的存在下使产物环化来制备。

著录项

  • 公开/公告号JPH10273499A

    专利类型

  • 公开/公告日1998-10-13

    原文格式PDF

  • 申请/专利权人 AKZO NOBEL NV;

    申请/专利号JP19980039455

  • 发明设计人 LOOZEN HUBERT JAN JOZEF;

    申请日1998-02-20

  • 分类号C07J53/00;A61K31/56;

  • 国家 JP

  • 入库时间 2022-08-22 03:08:44

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