Benzimidazol-2-N-piperazinylcarboxamid | 73903-20-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: Benzimidazol-2-N-piperazinylcarboxamid
• 英文别名: 1-(1H-benzimidazole-2-carbonyl)-piperazine；1H-Benzimidazol-2-yl-1-piperazinylmethanone；1H-benzimidazol-2-yl(piperazin-1-yl)methanone
• CAS: 73903-20-5
• 化学式: C₁₂H₁₄N₄O
• 分子量: 230.269
• InChiKey: CPSXHDNWKIRHJV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  61
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Benzimidazol-2-N-piperazinylcarboxamid 、 N,N-二乙基氯甲酰胺 以90%的产率得到
  参考文献：
  名称：

  RASTOGI R.; SHARMA S.; IYER R. N., INDIAN J. CHEM., 1979, B 18, NO 5, 464-467

  摘要：

  DOI：
• 作为产物：
  描述：

  4-(1H-benzoimidazole-2-carbonyl)-piperazine-1-carboxylic acid ethyl ester 、 盐酸 以50%的产率得到
  参考文献：
  名称：

  RASTOGI R.; SHARMA S.; IYER R. N., INDIAN J. CHEM., 1979, B 18, NO 5, 464-467

  摘要：

  DOI：

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。
• [EN] HETEROCYCLIC COMPOUNDS<br/>[FR] COMPOSES HETEROCYCLIQUES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004022060A2

  公开（公告）日：2004-03-18

  (1H-Benzoimidazol-2-YL)-(Piperazinyl)-Methanone derivatives of formula (I) and related compounds as histamine H4-receptor antagonists for the treatment of inflammatory and allergic disorders (I) wherein B and B1 are C or up to one of B and B1 may be N; Y is O, S or NR2, where R2 is H or C1-4alkyl; Z is O or S; R8 is H and R9 is (a), where R10 Is H or C1-4alkyl, or R8 and R9 are taken together with their N of attachment to form (b); n is 1 or 2; m is 1 or 2; n + m is 2 or 3; other substituents as defined in claim 1.

  (1H-苯并咪唑-2-基)-(哌嗪基)-甲酰胺类化合物(I)及其相关化合物，作为组胺H4受体拮抗剂用于治疗炎症性和过敏性疾病。 其中，B和B₁是C，或者B和B₁中至多一个为N；Y是O、S或NR₂，其中R₂是H或C₁₋₄烷基；Z是O或S；R₈是H，且R₉是(a)，其中R₁₀是H或C₁₋₄烷基，或者R₈和R₉与它们的连接N原子一起形成(b)；n是1或2；m是1或2；n + m是2或3；其他取代基如权利要求1所述。
• [EN] (1H-BENZOIMIDAZOL-2-YL)-(PIPERAZINYL)-METHANONE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H4-RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS<br/>[FR] COMPOSES HETEROCYCLIQUES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004022060A3

  公开（公告）日：2004-07-08
• RASTOGI R.; SHARMA S.; IYER R. N., INDIAN J. CHEM., 1979, B 18, NO 5, 464-467
  作者：RASTOGI R.、 SHARMA S.、 IYER R. N.

  DOI：——

  日期：——