| 摘要 |
The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.;In formula I, the variables have the following meanings:m is 1 or 2,n is 1 or 2,A is selected from the group consisting of CH2, CH2CH2, CHFCH2 and CF2CH2,R1 is an oxygen containing cyclic radical selected such as C3-C6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, and a carbonyl oxygen,R2 is selected from the group consisting of hydrogen, OH and fluorine,R3a is selected from the group consisting of hydrogen and methyl,R3b is selected from the group consisting of hydrogen and methyl,R4 is branched C4-C6 alkyl or branched fluorinated C4-C6 alkyl, andR5 is inter alia C1-C6 alkyl, fluorinated C1-C3 alkyl, C1-C2-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkyl, fluorinated hydroxy-C1-C4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C5 cycloalkyl, fluorinated C3-C5 cycloalkyl, etc. |
| 主权项 |
1. A compound of the formula I where m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH2, CH2CH2, CHFCH2 and CF2CH2, R1 is an oxygen containing cyclic radical selected from oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, and a carbonyl oxygen, and which may additionally carry 1 or 2 radicals selected from fluorine, C1-C2-alkyl and fluorinated C1-C2-alkyl; R2 is selected from the group consisting of hydrogen and fluorine, R3a is selected from the group consisting of hydrogen and methyl, R3b is selected from the group consisting of hydrogen and methyl, R4 is branched C4-C6 alkyl or branched fluorinated C4-C6 alkyl, and R5 is selected from the group consisting of C1-C6 alkyl, fluorinated C1-C3 alkyl, C1-C2-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkyl, fluorinated hydroxy-C1-C4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C5 cycloalkyl, fluorinated C3-C5 cycloalkyl, C3-C5 cycloalkyl-C1-C4-alkyl, fluorinated C3-C5 cycloalkyl-C1-C4-alkyl, C3-C5 cycloalkoxy-C1-C4-alkyl and fluorinated C3-C5 cycloalkoxy-C1-C4-alkyl, where the cycloalkyl moiety in the last six mentioned groups of radicals may carry 1 or 2 radicals selected from hydroxyl, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, C1-C2-alkyl and fluorinated C1-C2-alkyl, where the cycloalkoxy moiety in the last two mentioned radicals may carry 1 or 2 radicals selected from hydroxyl, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, C1-C2-alkyl and fluorinated C1-C2-alkyl, the N-oxides, the prodrugs and the pharmaceutically acceptable salts of these compounds. |
