SKOLNICK, PHIL,CHEN, ZHENGMING,BASILE, ANTHONY,EPSTEIN, JOSEPH W
申请号:
NZ59283606
公开号:
NZ592836A
申请日:
2006.07.25
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
592836 Disclosed are derivatives of 1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane and 1-(naphthalen-1-yl)-3-aza-bicyclo[3.1.0]hexane as represented by the general formulae (II) and (III), and enantiomers and pharmaceutically acceptable salts thereof, wherein: R1 and R2 are independently selected from hydrogen, unsubstituted alkyl, alkenyl and alkynyl, and substituted alkyl, alkenyl and alkynyl R3 is selected from hydrogen, alkyl, alkoxycarbonyl, alkanoyl, cycloalkyl, cycloalkanoyl, aryl, heteroaryl, saturated heterocyclic, alkenyl, alkynyl, and substituted alkyl, alkenyl and alkynyl and R4 and R5 are independently hydrogen or 1-4 substituents independently selected from halogen, alkyl, alkenyl, alkynyl, haloalkyl, cyano, hydroxy, cycloalkyl, alkoxy, alkoxyalkyl, carboxyalkyl, alkanoyl, haloalkoxy, nitro, amino, alkylamino, and dialkylamino and wherein the remaining substituents are as defined herein. Representative compounds include 1-(2-methoxynaphthalen-6-yl)-3-methyl-3-aza-bicyclo[3.1.0]hexane, (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane, (1S,5R)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane, (1R,5S)-3-methyl-1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane, (1S,5R)-3-methyl-1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane, 3-isopropyl-1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane, 3-ethyl-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane, 1-(naphthalen-1-yl)-3-aza-bicyclo[3.1.0]hexane, (1R,5S)-1-(naphthalen-1-yl)-3-azabicyclo[3.1.0]hexane, (1R,5S)-3-methyl-1-(naphthalen-1-yl)-3-aza-bicyclo[3.1.0]hexane, 1-(1-fluoronaphthalen-4-yl)-3-aza-bicyclo[3.1.0]hexane and 1-(1-methylnaphthalen-4-yl)-3-aza-bicyclo[3.1.0]hexane. Further disclosed is a pharmaceutical composition comprising an effective amount of a compound as defined above and a pharmaceutical acceptable carrier or vehicle therefor, for treating or preventing a central nervous system (CNS) disorder such as depression, an anxiety disorder, or an attention deficit disorder.