(-)-(R)-6-{2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl}-3,4-dihydro-2(1H)-quinolinone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (-)-(R)-6-{2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl}-3,4-dihydro-2(1H)-quinolinone
• 英文别名: (R)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydroquinolin-2(1H)-one；(R)-6-(2-(4-(3-fluorophenyl)-4-hydroxypiperidin-1-yl)-1-hydroxyethyl)-3,4-dihydroquinolin-2(1H)-one；6-[(1R)-2-[4-(3-fluorophenyl)-4-hydroxypiperidin-1-yl]-1-hydroxyethyl]-3,4-dihydro-1H-quinolin-2-one
• 化学式: C₂₂H₂₅FN₂O₃
• 分子量: 384.451
• InChiKey: ZTOSZJPNPROTBL-FQEVSTJZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  72.8
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] AZASPIRO DERIVATIVES AS TRPM8 ANTAGONISTS<br/>[FR] DÉRIVÉS AZASPIRO EN TANT QU'ANTAGONISTES DE TRPM8
  申请人：RAQUALIA PHARMA INC

  公开号：WO2015136947A1

  公开（公告）日：2015-09-17

  The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

  本发明涉及式(I)的氮杂环螺环衍生物或其药用可接受盐或前药，其制备方法，含有它们的药物组合物以及它们在治疗通过TRPM8受体介导的各种疾病中的应用。
• 3, 4-dihydroquinolin-2(1H)-one compounds as NR2B receptor antagonists
  申请人：——

  公开号：US20030216430A1

  公开（公告）日：2003-11-20

  This invention provides a compound which is (R)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof. The compound is useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, stroke, traumatic brain injury, Parkinson's disease, Alzheimer's disease, depression, anxiety, migraine, or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

  这项发明提供了一种化合物，即(R)-6-[2-[4-(3-氟苯基)-4-羟基-1-哌啶基]-1-羟乙基]-3,4-二氢-2(1H)-喹啉酮或其药学上可接受的酯，或其药学上可接受的盐。该化合物可用于治疗由NMDA NR2B受体过度活化引起的疾病症状，如疼痛、中风、创伤性脑损伤、帕金森病、阿尔茨海默病、抑郁症、焦虑症、偏头痛等哺乳动物，特别是人类。这项发明还提供了包含上述化合物的药物组合物。
• [EN] IMIDAZOLINONE DERIVATIVES AS TRPM8 ANTAGONISTS<br/>[FR] DÉRIVÉS D'IMIDAZOLINONE UTILISÉS EN TANT QU'ANTAGONISTES DE TRPM8
  申请人：RAQUALIA PHARMA INC

  公开号：WO2017043092A1

  公开（公告）日：2017-03-16

  The present invention relates to imidazolinone derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

  本发明涉及式(I)的咪唑啉酮衍生物或其药用可接受的盐或前药，其制备方法，含有它们的药物组合物以及它们在治疗通过TRPM8受体介导的各种疾病中的应用。
• Azaspiro derivatives as TRPM8 antagonists
  申请人：RaQualia Pharma Inc.

  公开号：US10093678B2

  公开（公告）日：2018-10-09

  The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

  本发明涉及式（I）的氮杂螺衍生物或其药学上可接受的盐或其原药、其制备工艺、含有它们的药物组合物以及它们在治疗通过 TRPM8 受体介导的各种疾病中的用途。
• 3, 4-DIHYDROQUINOLIN-2(1H)-ONE COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS
  申请人：PFIZER INC.

  公开号：EP1499606B1

  公开（公告）日：2006-05-03