1-[1-(1-methoxycarbonylpiperidin-4-yl)piperidin-4-yl]-3-(methylsulfonyl)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 1-[1-(1-methoxycarbonylpiperidin-4-yl)piperidin-4-yl]-3-(methylsulfonyl)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one
• 英文别名: 1-[1-(1-methoxycarbonylpiperidin-4-yl)-piperidin-4-yl]-3-(methylsulfonyl)-1,3-dihydro-2H-imidazo-[4,5-b]pyridin-2-one；methyl 4-[4-(3-methylsulfonyl-2-oxoimidazo[4,5-b]pyridin-1-yl)piperidin-1-yl]piperidine-1-carboxylate
• 化学式: C₁₉H₂₇N₅O₅S
• 分子量: 437.52
• InChiKey: XGEIVRANTROKON-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.63
• 拓扑面积：
  112
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1-[1-(1-methoxycarbonylpiperidin-4-yl)-piperidin-4-yl]-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one 生成 1-[1-(1-methoxycarbonylpiperidin-4-yl)piperidin-4-yl]-3-(methylsulfonyl)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one
  参考文献：
  名称：

  SUBSTITUTED IMIDAZOLIDINONE DERIVATIVES

  摘要：

  公开号：

  EP1221443B1

文献信息

• Substituted imidazolidinone derivatives
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US06699880B1

  公开（公告）日：2004-03-02

  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.

  本发明涉及由一般式[I]表示的化合物，其中A-D表示可选择取代的亚甲基组或氮原子；E表示氧原子或硫原子；表示可选择取代的单环或双环脂肪族含氮杂环基团；R1表示较低的烯基、较低的炔基、环状（较低的烷基）、较低的烷酰基、较低的烷氧羰基、可选择取代的较低烷基等；R2表示较低的烷基。本发明的化合物表现出刺激肌动蛋白酸乙酰胆碱受体M4的作用，可用作治疗伴随疼痛的疾病的镇痛剂，例如癌症疼痛、偏头痛、痛风、慢性风湿病、慢性疼痛或神经痛；或作为治疗对吗啡类镇痛剂的耐受性、依赖性、瘙痒、痴呆、肠易激综合征、精神分裂症、青光眼、尿频、尿失禁、胆石症、胆囊炎、功能性消化不良和反流性食管炎的药物。
• US6699880B1
  申请人：——

  公开号：US6699880B1

  公开（公告）日：2004-03-02
• SUBSTITUTED IMIDAZOLIDINONE DERIVATIVES
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP1221443B1

  公开（公告）日：2004-09-01