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REMEDY FOR SLEEP DISTURBANCE

机译:睡眠障碍的补救措施

摘要

Agents for treating and preventing sleep disorders comprise new and known opioid receptor-like 1 receptor (ORL-1) agonists. Agents for treating and preventing sleep disorders comprise new and known opioid receptor-like 1 receptor agonists. An independent claim is also included for new acenaphthene derivatives of formula (I) and their racemates, enantiomers and salts. [Image] R 1H, A, lower alkyl, lower alkenyl, CO 2H, COA, COOA, COPh, COOA, COOPh, PhCOA, ACOOA, lower alkenyl-COOA, ACONR 3R 4, SO 2A, SO 2Ph, ASA, ASOA, ASO 2A, ASO 2NR 3R 4, Ph or CH 2Ph; A : lower alkyl; Ph : phenyl (optionally substituted by A, halo, OA, phenoxy or benzyloxy); R 2H, A, halo, OA, phenoxy, benzyloxy, CF 3, NO 2, NH 2 or CN; R 3, R 4H, A or lower alkenyl; or NR 3R 4saturated heterocyclyl optionally substituted by A, halo, OA, phenoxy or benzyloxy; and X : O or S. ACTIVITY : CNS-Gen.; Hypnotic. In circadian rhythm sleep tests on rats administration of (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,4-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide (Ia) at 3 mg/kg orally advanced the Zeitgeber time by 3 hours compared to a control. MECHANISM OF ACTION : ORL-Agonist.
机译:用于治疗和预防睡眠障碍的药物包括新的和已知的类阿片受体样1受体(ORL-1)激动剂。用于治疗和预防睡眠障碍的药物包括新的和已知的类阿片受体样1受体激动剂。还包括对式(I)的新衍生物及其外消旋物,对映异构体和盐的独立权利要求。 [图片] R 1H,A,低级烷基,低级烯基,CO 2H,COA,COOA,COPh,COOA,COOPh,PhCOA,ACOOA,低级烯基-COOA,ACONR 3R 4,SO 2A,SO 2Ph,ASA,ASOA, ASO 2A,ASO 2NR 3R 4,Ph或CH 2Ph; A:低级烷基; Ph:苯基(任选地被A,卤素,OA,苯氧基或苄氧基取代); R 2H,A,卤素,OA,苯氧基,苄氧基,CF 3,NO 2,NH 2或CN; R 3,R 4H,A或低级烯基;或任选被A,卤素,OA,苯氧基或苄氧基取代的NR 3R 4饱和杂环基;或活动:CNS-Gen。; X:O或S。催眠。在昼夜节律睡眠试验中,对大鼠施用(R)-2- {3- [1-(ac啶-1-基)哌啶-4-基] -2,4-二氢-2-氧代苯并咪唑-1-基与对照组相比,口服3 mg / kg的N-甲基乙酰胺(Ia)可使Zeitgeber时间延长3小时。作用机理:ORL激动剂。

著录项

  • 公开/公告号PT1491212E

    专利类型

  • 公开/公告日2012-11-16

    原文格式PDF

  • 申请/专利权人 MITSUBISHI TANABE PHARMA CORPORATION;

    申请/专利号PT20030715566T

  • 发明设计人 KOJI TESHIMA;MASANORI MINOGUCHI;

    申请日2003-03-28

  • 分类号A61K31/454;A61K31;A61K31/527;A61P25/20;C07D235/26;C07D235/28;C07D401/04;

  • 国家 PT

  • 入库时间 2022-08-21 16:40:09

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