(9H-Fluoren-9-yl)methyl 4-(aminomethyl)piperidine-1-carboxylate

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: (9H-Fluoren-9-yl)methyl 4-(aminomethyl)piperidine-1-carboxylate
• 英文别名: 9H-fluoren-9-ylmethyl 4-(aminomethyl)piperidine-1-carboxylate
• 化学式: C₂₁H₂₄N₂O₂
• 分子量: 336.4
• InChiKey: KKDUEQBKFRCXSH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] BIS(PENTAHYDROXYHEXYL)AMINO SUBSTITUTED 2-{[(3-AMINO-PYRAZIN-2-YL)FORMAMIDO]METHYL}-1H-1,3-BENZODIAZOL-3-IUM DERIVATIVES AS ENAC INHIBITORS FOR TREATING RESPIRATORY DISEASES<br/>[FR] DÉRIVÉS DE 2-{[(3-AMINO-PYRAZIN-2-YL)FORMAMIDO]MÉTHYL}-1H-1,3-BENZODIAZOL-3-IUM SUBSTITUÉS PAR BIS(PENTAHYDROXYHEXYL)AMINO UTILISÉS EN TANT QU'INHIBITEURS D'ENAC POUR LE TRAITEMENT DE MALADIES RESPIRATOIRES
  申请人：ENTERPRISE THERAPEUTICS LTD

  公开号：WO2019077340A1

  公开（公告）日：2019-04-25

  The present invention discloses bis(pentahydroxyhexyl)amino substituted 2-[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3- benzodiazol-3-ium derivatives of formula (I) as inhibitors of ENaC and are of use in the treatment of respiratory diseases and conditions, skin conditions or ocular conditions, wherein the respiratory disease or condition is e.g. cystic fibrosis, chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchiectasis, including non-cystic fibrosis bronchiectasis, and asthma; the skin condition is e.g. psoriasis, atopic dermatitis and ichthyosis; and the ocular condition is e.g. dry eye disease.

  本发明公开了式(I)的双(戊糖基己基)氨基取代的2-[(3-氨基吡嗪-2-基)甲酰胺基]甲基}-1H-1,3-苯二唑-3-ium衍生物作为ENaC的抑制剂，并用于治疗呼吸道疾病和症状、皮肤病或眼部病症，其中呼吸道疾病或症状例如囊性纤维化、慢性阻塞性肺病（COPD）、慢性支气管炎、肺气肿、支气管扩张症，包括非囊性纤维化支气管扩张症和哮喘；皮肤病例如银屑病、特应性皮炎和鱼鳞病；眼部病症例如干眼症。
• COMPOUNDS
  申请人：Enterprise Therapeutics Limited

  公开号：US20210188855A1

  公开（公告）日：2021-06-24

  Compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

  通式（I）中R1、R2、R3、R4和X的化合物是上皮钠通道（ENaC）的抑制剂，可用于治疗或预防呼吸道疾病和状况、皮肤状况和眼部状况。
• [EN] BENZODIAZOLIUM COMPOUNDS AS ENAC INHIBITORS<br/>[FR] COMPOSÉS DE BENZODIAZOLIUM EN TANT QU'INHIBITEURS D'ENAC
  申请人：ENTERPRISE THERAPEUTICS LTD

  公开号：WO2018096325A1

  公开（公告）日：2018-05-31

  Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

  通式（I）中R1、R2、R3、R4、R5和X的化合物是上皮钠通道（ENaC）的抑制剂，可用于治疗或预防呼吸道疾病和状况、皮肤状况和眼部状况。
• Substituted benzodiazoliums as ENaC inhibitors
  申请人：ENTERPRISE THERAPEUTICS LIMITED

  公开号：US10941149B2

  公开（公告）日：2021-03-09

  Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

  其中 R1、R2、R3、R4、R5 和 X 如本文所定义的通式（I）化合物是上皮钠通道（ENaC）的抑制剂，可用于治疗或预防呼吸系统疾病、皮肤病和眼部疾病。
• Bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives as ENaC inhibitors for treating respiratory diseases
  申请人：ENTERPRISE THERAPEUTICS LIMITED

  公开号：US11370778B2

  公开（公告）日：2022-06-28

  The present invention discloses bis(pentahydroxyhexyl)amino substituted 2-[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives of formula (I) as inhibitors of ENaC and are of use in the treatment of respiratory diseases and conditions, skin conditions or ocular conditions, wherein the respiratory disease or condition is e.g. cystic fibrosis, chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchiectasis, including non-cystic fibrosis bronchiectasis, and asthma; the skin condition is e.g. psoriasis, atopic dermatitis and ichthyosis; and the ocular condition is e.g. dry eye disease.

  本发明公开了式(I)的双(五羟基己基)氨基取代的2-[(3-氨基吡嗪-2-基)甲酰氨基]甲基}-1H-1,3-苯并二唑-3-鎓衍生物，作为ENaC的抑制剂，可用于治疗呼吸系统疾病和病症、皮肤病症或眼部病症，其中呼吸系统疾病或病症为如.如囊性纤维化、慢性阻塞性肺病（COPD）、慢性支气管炎、肺气肿、支气管扩张症（包括非囊性纤维化支气管扩张症）和哮喘；皮肤状况如银屑病、特应性皮炎和鱼鳞病；眼部状况如干眼症。