2,6-dimethylpyridin-3-yl 4-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]piperidine-1-carboxylate | 1205634-48-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2,6-dimethylpyridin-3-yl 4-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]piperidine-1-carboxylate
• 英文别名: 2,6-dimethylpyridin-3-yl 4-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]piperidine--carboxylate；(2,6-Dimethylpyridin-3-yl) 4-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]piperidine-1-carboxylate
• CAS: 1205634-48-5
• 化学式: C₂₁H₂₀F₂N₄O₃
• 分子量: 414.412
• InChiKey: XJFRLBKSPDZTGG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  81.4
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• PROPHYLACTIC OR THERAPEUTIC AGENT FOR DISEASES ASSOCIATED WITH PAINS IN URINARY ORGANS
  申请人：Astellas Pharma Inc.

  公开号：EP2564849A1

  公开（公告）日：2013-03-06

  Disclosed is a prophylactic or therapeutic agent for diseases associated with pains in urinary organs. It is confirmed that a pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate compound or a salt thereof has an effective bladder capacity increasing activity and also has an analgesic activity on pains in the bladder and the testis, which rely on a FAAH inhibiting activity thereof. Therefore, a pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate compound or a salt thereof can be used for the prevention or treatment of interstitial cystitis/bladder pain syndrome and/or chronic non-bacterial prostatitis/chronic pelvic pain syndrome.

  本发明公开了一种预防或治疗与泌尿器官疼痛相关疾病的药物。经证实，一种吡啶基非芳香族含氮杂环-1-羧酸盐化合物或其盐类具有有效的膀胱容量增加活性，并且对膀胱和睾丸疼痛也具有镇痛活性，这依赖于其 FAAH 抑制活性。因此，吡啶基非芳香族氮化杂环-1-羧酸酯化合物或其盐可用于预防或治疗间质性膀胱炎/膀胱疼痛综合征和/或慢性非细菌性前列腺炎/慢性盆腔疼痛综合征。
• AZOLE COMPOUND
  申请人：Astellas Pharma Inc.

  公开号：EP2308869B1

  公开（公告）日：2012-09-19
• AGENT FOR PREVENTING OR TREATING DISEASES ACCOMPANIED BY URINARY PAIN
  申请人：Someya Akiyoshi

  公开号：US20130030006A1

  公开（公告）日：2013-01-31

  [Problem] Provided is an agent for preventing or treating diseases accompanied by urinary pain. [Means for Solution] A pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof was confirmed to have not only an action of increasing effective bladder capacity but also an analgesic action against bladder pain and testis pain, based on FAAH inhibitory action. Accordingly, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or a salt thereof can be used for preventing or treating interstitial cystitis/bladder pain syndrome and/or chronic nonbacterial prostatitis/chronic pelvic pain syndrome.
• US8207199B2
  申请人：——

  公开号：US8207199B2

  公开（公告）日：2012-06-26
• [EN] AZOLE COMPOUND<br/>[FR] COMPOSÉ AZOLE
  申请人：ASTELLAS PHARMA INC

  公开号：WO2010007966A1

  公开（公告）日：2010-01-21

  【課題】神経因性疼痛治療用医薬組成物の有効成分として有用な化合物を提供する。 【解決手段】発明者等は、FAAH阻害活性を有する化合物について鋭意検討した結果、N-(ピリジン-3-イル)オキシカルボニル-ピペリジン-4-イル基及びフェニル基で置換されたアゾール化合物又はその製薬学的に許容される塩が優れたFAAH阻害活性を示すことを知見し、本発明を完成させた。 　本発明化合物は、優れたFAAH阻害活性を有し、ラット神経因性疼痛モデルにおいて抗アロディニア効果が確認できたことから、神経因性疼痛の予防剤及び/又は治療剤として有用である。