8-benzhydryl-N-[(2-methoxyphenyl)methyl]-7-azatricyclo[4.3.1.03,7]decan-9-amine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 8-benzhydryl-N-[(2-methoxyphenyl)methyl]-7-azatricyclo[4.3.1.03,7]decan-9-amine
• 化学式: C₃₀H₃₄N₂O
• 分子量: 438.6
• InChiKey: LJKDZSJYYRZNMT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Novel medical use for tachykinin antagonists
  申请人：GLAXO GROUP LIMITED

  公开号：EP0533280A1

  公开（公告）日：1993-03-24

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R¹ is selected from halogen atoms and C₁₋₄alkyl, C₁₋₄alkoxy, trifluoromethyl, and S(0)nC₁₋₄alkyl groups; R² and R³, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C₁₋₄alkyl, C₁₋₄alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗呃逆中的应用。本发明还描述了式 (I) 的新型速激肽拮抗剂、其制备工艺、含有它们的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R¹ 选自卤素原子和 C₁₋₄烷基、C₁₋₄烷氧基、三氟甲基和 S(0)nC₁₋₄ 烷基； R² 和 R³（可以相同或不同）各自独立地选自氢和卤素原子以及 C₁₋₄烷基、C₁₋₄烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis
  申请人：GLAXO GROUP LIMITED

  公开号：EP0916346A2

  公开（公告）日：1999-05-19

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗呃逆中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4烷基、C1-4烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• NK-1 receptor antagonist and a systemic antiinflammatory corticosteroid for the treatment of emesis
  申请人：GLAXO GROUP LIMITED

  公开号：EP0919245A2

  公开（公告）日：1999-06-02

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗呃逆中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4烷基、C1-4烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• NK1 Antagonists for the treatment of depression
  申请人：GLAXO GROUP LIMITED

  公开号：EP1082959A1

  公开（公告）日：2001-03-14

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of depression. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1- 4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗抑郁症中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4 烷基、C1-4-烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• QUINUCLIDINE DERIVATIVES
  申请人：PFIZER INC.

  公开号：EP0540526B1

  公开（公告）日：1994-12-28