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US 2018/0000777 A1Published application
Novel 1-Aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders
AssigneeNeurovance, Inc.
InventorsPhil SKOLNICK, Anthony BASILE, Zhengming CHEN, Joseph W. EPSTEIN
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Abstract
The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
Claims25
1-93. (canceled)
A method of making a 1-aryl-3-azabicyclo[3.1.0]hexane of Formula IV
- or a pharmaceutically acceptable salt thereof, wherein Ar is an unsubstituted naphthyl group or a naphthyl group having 1-4 substituents independently selected from halogen, C1-3 alkyl, C2-4 alkenyl, C2-4 alkynyl, halo(C1-3)alkyl, cyano, hydroxy, C3-5 cycloalkyl, C1-3 alkoxy, C1-3 alkoxy(C1-3)alkyl, carboxy(C1-3)alkyl, C1-3 alkanoyl, halo(C1-3)alkoxy, nitro, amino, C1-3 alkylamino, and di(C1-3)alkylamino, comprising cyclizing a compound of formula (iii)
- wherein Ar is as defined above.
A method of making a 1-aryl-3-azabicyclo[3.1.0]hexane of Formula V
- or a pharmaceutically acceptable salt thereof, wherein Ar is an unsubstituted naphthyl group or a naphthyl group having 1-4 substituents independently selected from halogen, C1-3 alkyl, C2-4 alkenyl, C2-4 alkynyl, halo(C1-3)alkyl, cyano, hydroxy, C3-5 cycloalkyl, C1-3 alkoxy, C1-3 alkoxy(C1-3)alkyl, carboxy(C1-3)alkyl, C1-3 alkanoyl, halo(C1-3)alkoxy, nitro, amino, C1-3 alkylamino, and di(C1-3)alkylamino, and R is hydrogen, methyl, ethyl, isopropyl or a nitrogen protecting group, comprising reducing a compound of formula (ix)
- wherein Ar and R are as defined above.
Dependencies are inferred from the claim text.