pyridin-3-yl 4-(1H-indole-2-carbonyl)piperazine-1-carboxylate | 1225282-03-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: pyridin-3-yl 4-(1H-indole-2-carbonyl)piperazine-1-carboxylate
• CAS: 1225282-03-0
• 化学式: C₁₉H₁₈N₄O₃
• 分子量: 350.377
• InChiKey: JJQQRZPJCUSOIC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  78.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• CARBAMATE COMPOUND OR SALT THEREOF
  申请人：Ishii Takahiro

  公开号：US20110212973A1

  公开（公告）日：2011-09-01

  [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention. The carbamate compound of the present invention has an excellent FAAH inhibitory activity and can be used as an agent for preventing and/or treating FAAH-related diseases, particularly nocturia, interstitial cystitis, painful bladder syndrome, or chronic non-bacterial prostatitis/chronic pelvic pain syndrome.

  [问题] 提供了一种作为治疗FAAH相关疾病药物组合物活性成分的化合物。 [解决方法] 现有发明人对具有FAAH抑制活性的化合物进行了广泛的研究，结果发现，一种哌嗪-1-羧酸盐化合物，在其中苯并咪唑-2-基甲酰基，苯并呋喃-2-基甲酰基或类似物与哌嗪的4-位结合，具有出色的FAAH抑制活性，并进一步具有增加有效膀胱容量的作用，改善睡眠障碍的作用，抗利尿作用和对包括膀胱疼痛在内的下尿路疼痛的镇痛活性，从而完成了本发明。本发明的氨基甲酸酯化合物具有出色的FAAH抑制活性，可用作预防和/或治疗FAAH相关疾病的药物，特别是夜尿症，间质性膀胱炎，疼痛性膀胱综合征或慢性非细菌性前列腺炎/慢性盆腔疼痛综合征的药物。