Methods and compositions for production, formulation and use...

A - Human Necessities – 61 – K

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A61K 31/40 (2006.01) A61K 31/4015 (2006.01) C07C 69/76 (2006.01) C07C 211/17 (2006.01) C07D 207/444 (2006.01) C07D 209/52 (2006.01)

Patent

CA 2640120

The invention provides novel l-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 l-aryl-3-azabicyclo¢3.1.0! hexanes are provided that have at least one substituent on the aryl ring. In other embodiments l-aryl-3-azabicyclo¢3.1.0! hexanes are provided that have a substitution on the nitrogen at the '3' position. In additional embodiments l-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 l-aryl-3-azabicyclo¢3.1.0! hexanes, including synthetic methods that form novel intermediate compounds of the invention for producing aryl- and aza-substituted l-aryl-3- azabicyclo¢3.1.0! hexanes.

L'invention porte sur de nouveaux l-aryl-3-azabicyclo[3.1.0] hexanes et sur des compositions et méthodes d'utilisation de ces composés pour traiter les troubles du SNC. Certains de ces l-aryl-3-azabicyclo[3.1.0] hexanes présentent au moins une substitution sur le cycle aryle. D'autres de ces l-aryl-3-azabicyclo[3.1.0] hexanes présentent une substitution sur l'azote à la position '3'. Dans d'autres variantes, ces l-aryl-3-azabicyclo[3.1.0] hexanes présentent une substitution sur le cycle aryle, et une substitution sur l'azote à la position '3'. L'invention porte également sur de nouveaux procédés d'obtention d'l-aryl-3-azabicyclo[3.1.0] hexanes à substitution aryle et aza, dont des procédés de synthèse des nouveaux composés intermédiaires de l'invention permettant d'obtenir des l-aryl-3-azabicyclo[3.1.0] hexanes à substitution aryle et aza.

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