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    • 3. 发明申请
    • Methods and compositions for production, formulation and use of 1-aryl-3-azabicyclo[3.1.0]hexanes
    • 用于生产,配制和使用1-芳基-3-氮杂双环[3.1.0]己烷的方法和组合物
    • US20060223875A1
    • 2006-10-05
    • US11371178
    • 2006-03-07
    • Phil SkolnickAnthony BasileZhengming Chen
    • Phil SkolnickAnthony BasileZhengming Chen
    • A61K31/403C07D209/00
    • C07D209/52
    • The invention provides novel 1-aryl-3-azabicyclo[3.1.0]hexanes that are active for modulating biogenic amine transport, along with compositions and methods for using these compounds to treat central nervous system disorders. Certain 1-aryl-3-azabicyclo[3.1.0]hexanes are provided that have at least one substituent on the aryl ring. In other embodiments 1-aryl-3-azabicyclo[3.1.0]hexanes are provided that have a substitution on the nitrogen at the ‘3’ position. In additional embodiments 1-aryl-3-azabicyclo[3.1.0]hexanes are provided which have one substitution on the aryl ring, as well as a substitution on the nitrogen at the ‘3’ position. The invention also provides novel methods of making aryl- and aza-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, including synthetic methods that form novel intermediate compounds of the invention for producing aryl- and aza-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes.
    • 本发明提供了用于调节生物胺转运的新型1-芳基-3-氮杂双环[3.1.0]己烷,以及使用这些化合物治疗中枢神经系统疾病的组合物和方法。 提供在芳基环上具有至少一个取代基的某些1-芳基-3-氮杂双环[3.1.0]己烷。 在其它实施方案中,提供1-氮杂双环[3.1.0]己烷,其在“3”位上在氮上具有取代基。 在另外的实施方案中,提供1-芳基-3-氮杂双环[3.1.0]己烷,其在芳基环上具有一个取代基,以及在“3”位置的氮上进行取代。 本发明还提供制备芳基和氮杂取代的1-芳基-3-氮杂双环[3.1.0]己烷的新方法,包括形成本发明的新型中间体化合物的合成方法,用于制备芳基和氮杂取代的1-芳基 -3-氮杂双环[3.1.0]己烷。