Benzamide, 3,4-dichloro-N-methyl-N-(2-(1-pyrrolidinyl)cyclohexyl)-, cis- | 92953-43-0

• 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: Benzamide, 3,4-dichloro-N-methyl-N-(2-(1-pyrrolidinyl)cyclohexyl)-, cis-
• 英文别名: 3,4-dichloro-N-methyl-N-[(1R,2S)-2-pyrrolidin-1-ylcyclohexyl]benzamide
• CAS: 92953-43-0
• 化学式: C₁₈H₂₄Cl₂N₂O
• 分子量: 355.3
• InChiKey: JUBNVWGVNWIXMB-SJORKVTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Cis-N-[(2-aminocycloaliphatic)benzene acetamide and -benzamide anticonvulsants
  申请人：THE UPJOHN COMPANY

  公开号：EP0222533A1

  公开（公告）日：1987-05-20

  Certain cis-N-(2-amino-cycloaliphatic)benzeneacetamide and -benz­amides of the formula where m is 0 or 1, n is 1 or 2, R is hydrogen or alkyl, R₁ and R₂ are separately alkyl, or, taken together with the nitrogen denote a pyrrolidine ring, and X and Y are hydrogen, fluorine, chlorine or bromine or one of X and Y is trifluoromethyl, e.g., cis-3,4-dichloro-­N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzamide and salts thereof, have been found to have CNS seizure blocking or preventing drug action, e.g., anti-convulsant drug properties with little or no analgesic properties. Some of these compounds are new.

  某些顺式-N-(2-氨基环脂族)苯乙酰胺和-苯甲酰胺，其式为 其中m为0或1，n为1或2，R为氢或烷基，R₁和R₂分别为烷基，或与氮一起表示吡咯烷环，X和Y为氢、氟、氯或溴，或X和Y之一为三氟甲基，例如已发现顺式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)环己基]苯甲酰胺及其盐类具有中枢神经系统癫痫发作阻断或预防药物作用，例如抗惊厥药物特性，但几乎没有镇痛特性。其中一些化合物是新化合物。
• N-/Arylethyl/-N-alkyl-2-(1-pyrrolidinyl)ethylamine derivatives for CNS disorders
  申请人：G.D. Searle & Co.

  公开号：EP0518216A2

  公开（公告）日：1992-12-16

  Certain N-[arylethyl]-N-alkyl-2-(1-pyrrolidinyl)ethylamine compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula wherein R1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R2 and R3 is independently selected from hydrido and loweralkyl; wherein each of R4 through R9 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein m is a number selected from one through three; wherein n is a number selected from four through seven; wherein p is a number selected from zero through four; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

  某些 N-[芳基乙基]-N-烷基-2-(1-吡咯烷基)乙胺化合物用于治疗中枢神经系统疾病，如脑缺血、精神障碍、抽搐和帕金森病。特别值得关注的化合物为以下式子 其中 R1 选自水合烷基、低级烷基、4 至 6 个碳原子的环烷基烷基和低级烯基烷基；其中 R2 和 R3 各自独立地选自水合烷基和低级烷基；其中 R4 至 R9 各自独立地选自水合烷基、羟基、低级烷基、苄基、苯氧基、苄氧基和卤代低级烷基；其中 m 是选自 1 至 3 的数字；其中 n 是选自 4 至 7 的数字；其中 p 是选自 0 到 4 的数字；其中 A 选自苯基、萘基和噻吩基；其中任何上述 A 基团可进一步被一个或多个取代基取代，这些取代基独立地选自肼基、羟基、低级烷基、低级烷氧基、卤代、卤代低级烷基、氨基、单低级烷基氨基和稀释低级烷基氨基；或其药学上可接受的盐。
• CIS-N-(2-AMINOCYCLOALIPHATIC)BENZENE ACETAMIDE AND -BENZAMIDE ANTICONVULSANTS
  申请人：THE UPJOHN COMPANY

  公开号：EP0248824A1

  公开（公告）日：1987-12-16
• Use of CIS-N-(2 Aminocycloaliphatic) benzene acetamide and Benzamide for the manufacture of anticonvulsants
  申请人：THE UPJOHN COMPANY

  公开号：EP0248824B1

  公开（公告）日：1990-01-17
• NITROGEN-CONTAINING CYCLOHETERO CYCLOALKYLAMINOARYL DERIVATIVES FOR CNS DISORDERS
  申请人：G.D. Searle & Co.

  公开号：EP0594597A1

  公开（公告）日：1994-05-04