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    • 1. 发明授权
    • Substituted imidazolidinone derivatives
    • 取代的咪唑啉酮衍生物
    • US06699880B1
    • 2004-03-02
    • US10110638
    • 2002-04-15
    • Takeru YamakawaMakoto AndoSeita KoitoKenji OhwakiToshifumi KimuraToshihiko SaekiMitsuru MiyajiYuki IwahoriToru FujikawaNorikazu OtakeKazuhito Noguchi
    • Takeru YamakawaMakoto AndoSeita KoitoKenji OhwakiToshifumi KimuraToshihiko SaekiMitsuru MiyajiYuki IwahoriToru FujikawaNorikazu OtakeKazuhito Noguchi
    • A61K31445
    • C07D401/14
    • This invention relates to the compounds represented by the general formula [I], [in which A—D signify optionally substituted methine group(s) or nitrogen atom; E signifies oxygen or sulfur atom; signify optionally substituted mono- or bi-cyclic aliphatic nitrogen-containing heterocyclic group(s); R1 signifies lower alkenyl, lower alkynyl, cyclo(lower alkyl), lower alkanoyl, lower alkoxycarbonyl, optionally substituted lower alkyl and the like; and R2 signifies lower alkyl]. The compounds of the present invention exhibit an action to stimulate muscarinic acetylcholine receptors M4, and are useful as analgesic for diseases accompanying pain such as cancerous pain, migraine, gout, chronic rheumatism, chronic pain or neuralgia; or as agents for treating tolerance to narcotic analgesics represented by morphine, dependence on narcotic analgesics represented by morphine, itching, dementia, irritable bowel syndrome, schizophrenia, glaucoma, pollakiuria, urinary incontinence, cholelithiasis, cholecystitis, functional dyspepsia and reflux esophagitis.
    • 本发明涉及由通式[I]表示的化合物,其中A-D表示任选取代的次甲基或氮原子; E表示氧或硫原子;表示任选取代的单环或双环脂族含氮杂环基; R 1表示低级烯基,低级炔基,环(低级烷基),低级烷酰基,低级烷氧基羰基,任意取代的低级烷基等; 本发明化合物表现出刺激毒蕈碱性乙酰胆碱受体M4的作用,可作为镇痛药用于伴随疼痛的疾病,例如癌性疼痛,偏头痛,痛风,慢性风湿病,慢性疼痛或慢性疼痛。 神经痛; 或作为治疗由吗啡代表的麻醉止痛药的耐受性的药剂,以吗啡,瘙痒,痴呆,肠易激综合征,精神分裂症,青光眼,尿频尿症,尿失禁,胆石病,胆囊炎,功能性消化不良和反流性食管炎为代表的麻醉止痛药的依赖。