N-[(1-ethylpyrrolidin-2-yl)methyl]-6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: N-[(1-ethylpyrrolidin-2-yl)methyl]-6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide
• 化学式: C₂₀H₂₆N₄O₃
• 分子量: 370.4
• InChiKey: GKOIVPDQQHRBHI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  79.5
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] NOVEL DIHYDROINDENO[1,2-C]PYRAZOLE-3-CARBOXAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEVELOPMENTAL DISORDERS OR NEURODEGENERATIVE DISEASES, COMPRISING SAME<br/>[FR] NOUVEAU DÉRIVÉ DE DIHYDRO-INDÉNO[1,2-C]PYRAZOLE-3-CARBOXAMIDE ET COMPOSITION PHARMACEUTIQUE POUR LA PRÉVENTION OU LE TRAITEMENT DE TROUBLES NEURODÉVELOPPEMENTAUX OU DE MALADIES NEURODÉGÉNÉRATIVES LE COMPRENANT<br/>[KO] 신규한 디히드로인데노[1,2-c]피라졸-3-카복사미드 유도체 및 이를 포함하는 신경발달장애 또는 신경퇴행성 질환의 예방 또는 치료용 약학 조성물
  申请人：KOREA RES INST CHEMICAL TECH

  公开号：WO2021133129A2

  公开（公告）日：2021-07-01

  [EN] The present invention relates to a novel dihydroindeno[1,2-c]pyrazole-3-carboxamide derivative and a pharmaceutical composition for the prevention or treatment of neurodevelopmental disorders or neurodegenerative diseases, the pharmaceutical composition comprising same as an active ingredient. The present invention can provide a compound which has excellent GSK3β inhibitory activity and excellent efficacy of inhibiting NFκB activity and activating the Wnt/β-catenin signaling pathway in MeCP2-depleted cells, and thus is effective as a composition for the prevention or treatment of neurodevelopmental disorders or neurodegenerative diseases.
  [FR] La présente invention concerne un nouveau dérivé de dihydro-indéno[1,2-c]pyrazole-3-carboxamide et une composition pharmaceutique pour la prévention ou le traitement de troubles neurodéveloppementaux ou de maladies neurodégénératives, la composition pharmaceutique le contenant en tant que substance active. La présente invention concerne un composé qui a une excellente activité inhibitrice de GSK3β et une excellente efficacité d'inhibition de l'activité de NFκB et d'activation de la voie de signalisation Wnt/β-caténine dans des cellules appauvries en MeCP2, et est donc efficace en tant que composition pour la prévention ou le traitement de troubles neurodéveloppementaux ou de maladies neurodégénératives.
  [KO] 본 발명은 신규한 디히드로인데노[1,2-c]피라졸-3-카복사미드 유도체 및 이를 유효성분으로 포함하는 신경발달장애 또는 신경퇴행성 질환의 예방 또는 치료용 약학 조성물에 관한 것으로, GSK3β 저해 활성이 우수하며 MeCP2가 제거된 세포에서의 NFκB 활성 억제 및 Wnt/β-카테닌 신호전달계 활성화 효능이 우수하여 신경발달장애 또는 신경퇴행성 질환 예방 또는 치료용 조성물로 유용한 화합물을 제공할 수 있다.