1-aza-bicyclo[3.3.1]nonanes

摘要

The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.;

主权项

1. A compound of formula I wherein A represents O; Y represents a group of formula wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted phenyl, napthyl or heteroaryl, a group N(R1)(R4) or a group N(R2)(CHR3R4); wherein said heteroaryl is a 5-6 membered monocyclic ring or a 9 membered bicyclic ring wherein said ring has from one to three heteroatoms each independently selected from the group consisting of N, O and S; wherein said phenyl, napthyl, or heteroaryl are optionally substituted with 1-3 substituents selected from the group consisting of amino, C1-C4alkyl amino, di(C1-C4alky)-amino, C3-C5cycloalkyl amino, di(C3-C5)cycloalkyl amino, N—C1-C4alkyl-N—C3-C5cycloalkyl amino, halogen C1-C4alkyl, C4-C6cycloalkyl, hydroxy, C1-C4alkoxy, C3-C5cycloalkyloxy, C1-C4alkoxy C1-C4alkoxy, di(C1-C4alkyl)-amino C1-C4alkoxy, carbamoyl, N—C1-C4alkyl-carbamoyl, N,N-di(C1-C4alkyl)-carbamoyl, nitro, cyano, carboxy, C1-C4alkoxy carbonyl, C1-C4alkanoyloxy, benzoyl, amidino, guanidino, ureido, mercapto, C1-C4alkylthio, pyridyl, phenyl, phenoxy, C1-C4alkoxy phenyl, phenylthio, phenyl-C1-C4alkylthio, C1-C4alkylsulfonyl, phenylsulfonyl, C1-C4alkylphenylsulfonyl, C1-C4alkenyl, C1-C4alkanoyl, C1-C4alkylene dioxy bound at adjacent C-atoms of the ring, and C1-C4alkyl, which is substituted by halogen, hydroxy, C1-C4alkoxy, nitro, cyano, carboxy, C1-C4alkoxy carbonyl, C1-C4alkanoyl or C1-C4alkanoyloxy; wherein said C1-C4alkyl is optionally substituted by halogen; R1 represents hydrogen; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents phenyl, napthyl or heteroaryl, wherein said heteroaryl is a 5-6 membered monocyclic ring or a 9 membered bicyclic ring wherein said ring has from one to three heteroatoms each independently selected from the group consisting of N, O and S; wherein said phenyl, napthyl, or heteroaryl are optionally substituted with 1-3 substituents selected from the group consisting of halogen, NO2, CN, C1-C4alkoxy, C1-C4alkyl; wherein said C1-C4alkyl is optionally substituted by halogen; in free base or acid addition salt form.