(8S,11R,15R)-8-methyl-7,10-diazatetracyclo[8.5.1.05,16.011,15]hexadeca-1,3,5(16)-triene

• 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: (8S,11R,15R)-8-methyl-7,10-diazatetracyclo[8.5.1.05,16.011,15]hexadeca-1,3,5(16)-triene
• 化学式: C₁₅H₂₀N₂
• 分子量: 228.33
• InChiKey: FGDVGQYZEYBKIK-ZKYQVNSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives
  申请人：Sabb Louise Annmarie

  公开号：US20050004101A1

  公开（公告）日：2005-01-06

  This invention provides compounds of the formulae: wherein: R 1 is hydrogen, —C(O)CH 3 or alkyl of 1-6 carbon atoms; R 2 and R 3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH 2 OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R 4 and R 5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R 6 and R 7 are each independently hydrogen, C 1 -C 6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

  本发明提供了以下式的化合物：其中：R1是氢，—C（O）CH3或1-6碳原子的烷基；R2和R3各自独立地是氢、1-6碳原子的烷基、环烷基、1-6碳原子的烷氧基、—CH2OH、氟代烷基、1-6碳原子的烷基磺酰胺、1-6碳原子的烷基酰胺、氨基、1-6碳原子的烷基氨基、每个烷基基团的1-6碳原子的二烷基氨基、1-6碳原子的氟代烷氧基、2-7碳原子的酰基、芳基或芳酰基；R4和R5各自独立地是氢、1-6碳原子的烷基、1-6碳原子的烷氧基、卤素、氟代烷基、—CN、1-6碳原子的烷基磺酰胺、1-6碳原子的烷基酰胺、氨基、1-6碳原子的烷基氨基、每个烷基基团的1-6碳原子的二烷基氨基、1-6碳原子的氟代烷氧基、2-7碳原子的酰基或芳酰基；R6和R7各自独立地是氢、C1-C6烷基或环烷基；或其药学上可接受的盐，以及含有这些化合物的制药组合物和它们的使用方法，包括治疗强迫症、惊恐障碍、抑郁症、焦虑、广泛性焦虑障碍、精神分裂症、偏头痛、睡眠障碍、进食障碍、肥胖症、癫痫和脊髓损伤。
• PROCESS FOR PREPARATION OF CYCLOPENTA [B] [1,4] DIAZEPINO [6,7,1-HI] INDOLE DERIVATIVES
  申请人：American Home Products Corporation

  公开号：US20020055630A1

  公开（公告）日：2002-05-09

  The present invention provides processes for the preparation of 1, 2, 3, 4, 8, 9, 10, 10 a -octahydro-7bH-cyclopenta[b][1, 4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: 1 wherein: R is H, alkyl, acyl, or aroyl; R 1 , R 2 , R 4 and R 5 are H, OH, alkyl, cycloalkyl, alkoxy s, halogen, fluorinated alkyl, —CN, —NH—SO 2 -alkyl, -SO 2 —NH-alkyl, alkyl amide, amino, alkylamino s, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; R 3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO 2 -alkyl, -SO 2 —NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of central nervous system disorders.

  本发明提供了一种制备1,2,3,4,8,9,10,10a-八氢-7bH-环戊[b][1,4]二氮杂-6,7,1-咪唑[6,7,1-hi]吲哚衍生物的方法，其一般式为：1其中：R为H、烷基、酰基或芳基；R1、R2、R4和R5为H、OH、烷基、环烷基、烷氧基、卤素、氟代烷基、—CN、—NH—SO2-烷基、-SO2—NH-烷基、烷基酰胺、氨基、烷基氨基、二烷基氨基、氟代烷氧基、酰基、芳基或芳基酰基；R3为H、烷基、环烷基、烷氧基、氟代烷基、—NH—SO2-烷基、-SO2—NH-烷基、烷基酰胺、氨基、烷基氨基、二烷基氨基、氟代烷氧基、酰基、芳基或芳基酰基；或其药学上可接受的盐，其用于治疗中枢神经系统疾病。
• CYCLOPENTA[b][1,4]DIAZEPINO[6,7,1-hi]INDOLES AND DERIVATIVES
  申请人：Sabb Louise Annmarie

  公开号：US20080009480A1

  公开（公告）日：2008-01-10

  This invention provides compounds of the formulae: wherein: R 1 is hydrogen, —C(O)CH 3 or alkyl of 1-6 carbon atoms; R 2 and R 3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH 2 OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R 4 and R 5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R 6 and R 7 are each independently hydrogen, C 1 -C 6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

  这项发明提供了以下式子的化合物：其中：R1为氢、—C（O）CH3或1-6个碳原子的烷基；R2和R3各自独立地为氢、1-6个碳原子的烷基、环烷基、1-6个碳原子的烷氧基、—CH2OH、氟代烷基、1-6个碳原子的烷基磺酰胺、1-6个碳原子的烷基酰胺、氨基、1-6个碳原子的烷基氨基、每个烷基成分的1-6个碳原子的双烷基氨基、1-6个碳原子的氟代烷氧基、2-7个碳原子的酰基、芳基或芳酰基；R4和R5各自独立地为氢、1-6个碳原子的烷基、1-6个碳原子的烷氧基、卤素、氟代烷基、—CN、1-6个碳原子的烷基磺酰胺、1-6个碳原子的烷基酰胺、氨基、1-6个碳原子的烷基氨基、每个烷基成分的1-6个碳原子的双烷基氨基、1-6个碳原子的氟代烷氧基、2-7个碳原子的酰基或芳酰基；R6和R7各自独立地为氢、C1-C6烷基或环烷基；或其药学上可接受的盐，以及包含这些化合物的制药组合物和它们的使用方法，包括治疗强迫症、恐慌症、抑郁症、焦虑症、广泛性焦虑症、精神分裂症、偏头痛、睡眠障碍、进食障碍、肥胖症、癫痫和脊髓损伤。
• CYCLOPENTA[B][1,4] DIAZEPINO[6,7,1-HI]INDOLES AS 5HT2C ANTAGONISTS
  申请人：Wyeth

  公开号：EP1330457B1

  公开（公告）日：2004-10-20
• Methods for modulating bladder function
  申请人：Jacobson William

  公开号：US20070225274A1

  公开（公告）日：2007-09-27

  This invention provides methods and pharmaceutical compositions for modulating bladder function, and in particular for maintaining bladder control or treating urinary incontinence.