2,3,4,5-tetrahydro-2-[(5-methyl-1 H-imidazol-4-yl)methyl]-5-propyl-1 H-pyrido[4,3-b]indol-1-one | 122852-37-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 2,3,4,5-tetrahydro-2-[(5-methyl-1 H-imidazol-4-yl)methyl]-5-propyl-1 H-pyrido[4,3-b]indol-1-one
• 英文别名: 2-[(5-methyl-1H-imidazol-4-yl)methyl]-5-propyl-3,4-dihydropyrido[4,3-b]indol-1-one
• CAS: 122852-37-3
• 化学式: C₁₉H₂₂N₄O
• 分子量: 322.41
• InChiKey: HRLHPVVRDWUEJP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  53.9
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Use of serotonin antagonists in the treatment of cognitive disorders
  申请人：GLAXO GROUP LIMITED

  公开号：EP0357415A2

  公开（公告）日：1990-03-07

  The invention relates to the use of compounds of formula wherein Im represents an imidazolyl group of formula: and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl,C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵); one of the groups represented by R², R³ and R⁴ is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenylC₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group; and n represents 2 or 3, and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.

  本发明涉及式化合物的用途 其中 Im 代表式中的咪唑基团： 且 R¹ 代表氢原子或选自 C₁₋₆烷基、C₃₋₆烯基、C₃₋₁₀alkynyl、C₃₋₇cycloalkyl,C₃₋₇cycloalkylC₁₋₄alkyl、苯基的基团、苯基、C₁₋₃烷基、苯甲氧基甲基、苯氧基乙基、苯氧基甲基、-CO₂R⁵、-COR⁵、-CONR⁵R⁶或-SO₂R⁵（其中R⁵ 和R⁶可以相同或不同、各自代表氢原子、C₁₋₆烷基或 C₃₋₇环烷基，或苯基或苯基 C₁₋₄ 烷基，其中苯基任选被一个或多个 C₁₋₄ 烷基取代、C₁₋₄烷氧基或羟基或卤素原子取代，但当 R¹ 代表-CO₂R⁵或-SO₂R⁵基团时，R⁵不代表氢原子；） R²、R³和R⁴所代表的基团之一是氢原子或C₁₋₆烷基、C₃₋₇环烷基、C₃₋₆烯基、苯基或苯基 C₁₋₃烷基，而另外两个基团（可以相同或不同）分别代表氢原子或 C₁₋₆烷基； n 代表 2 或 3、 及其生理上可接受的盐和溶液，用于制造治疗认知障碍的药物。
• Use of serotonin antagonists in the treatment of depression
  申请人：GLAXO GROUP LIMITED

  公开号：EP0357414A2

  公开（公告）日：1990-03-07

  The invention relates to the use of compounds of formula (I) wherein Im represents an imidazolyl group of formula: and R¹ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₃₋₆alkenyl, C₃₋₁₀alkynyl, C₃₋₇cycloalkyl, C₃₋₇cycloalkylC₁₋₄alkyl, phenyl, phenylC₁₋₃alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO₂R⁵, -COR⁵, -CONR⁵R⁶ or -SO₂R⁵ (wherein R⁵ and R⁶, which may be the same or different, each represents a hydrogen atom, a C₁₋₆alkyl or C₃₋₇cycloalkyl group, or a phenyl or phenylC₁₋₄alkyl group, in which the phenyl group is optionally substituted by one or more C₁₋₄alkyl, C₁₋₄alkoxy or hydroxy groups or halogen atoms, with the proviso that R⁵ does not represent a hydrogen atom when R¹ represents a group -CO₂R⁵ or -SO₂R⁵); one of the groups represented by R², R³ and R4 is a hydrogen atom or a C₁₋₆alkyl, C₃₋₇cycloalkyl, C₃₋₆alkenyl, phenyl or phenylC₁₋₃alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C₁₋₆ alkyl group; and n represents 2 or 3, and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of depression.

  本发明涉及式（I）化合物的用途 其中 Im 代表式中的咪唑基团： 且 R¹ 代表氢原子或选自 C₁₋₆烷基、C₃₋₆烯基、C₃₋₁₀alkynyl、C₃₋₇cycloalkylC₁₋₄烷基、苯基的基团、C₁₋₃烷基、苯甲氧基甲基、苯氧乙基、苯氧甲基、-CO₂R⁵、-COR⁵、-CONR⁵R⁶或-SO₂R⁵（其中 R⁵ 和 R⁶可以相同或不同、各自代表氢原子、C₁₋₆烷基或 C₃₋₇环烷基，或苯基或苯基 C₁₋₄ 烷基，其中苯基任选被一个或多个 C₁₋₄ 烷基取代、C₁₋₄烷氧基或羟基或卤素原子取代，但当 R¹ 代表-CO₂R⁵或-SO₂R⁵基团时，R⁵不代表氢原子；） R²、R³ 和 R4 所代表的基团之一是氢原子或 C₁₋₆烷基、C₃₋₇环烷基、C₃₋₆烯基、苯基或苯基 C₁₋₃烷基，而另外两个基团（可以相同或不同）分别代表氢原子或 C₁₋₆烷基； n 代表 2 或 3、 及其生理上可接受的盐和溶液，用于制造治疗抑郁症的药物。
• Use of 5-hydroxytryptamine-antagonists in the treatment of mental disorders originating in childhood
  申请人：GLAXO GROUP LIMITED

  公开号：EP0450757A2

  公开（公告）日：1991-10-09

  The invention relates to the use of a compound which acts as an antagonist of 5-HT at 5-HT₃ receptors in the treatment of autism or another disorder originating in childhood in which there is mental retardation.

  本发明涉及一种在 5-HT₃ 受体上作为 5-HT 拮抗剂的化合物在治疗自闭症或另一种源于儿童期的精神发育迟滞疾病中的应用。
• Lactam derivatives
  申请人：GLAXO GROUP LIMITED

  公开号：EP0306323B1

  公开（公告）日：1994-09-21
• US5221687A
  申请人：——

  公开号：US5221687A

  公开（公告）日：1993-06-22