Pyrimidine derivatives for the treatment of diseases of the nerve system mediated by gamma-aminobutyric acid B (GABA B)

摘要

1. The compound of the formula! ! in the form of a free base or in the form of an acid addition salt, where! R1 is an alkyl, haloalkyl, alkoxy group, haloalkoxy group, alkylthio group, haloalkylthio group, alkylamino group or haloalkylamino group; ! R2 is halogen, hydroxy or a substituted amino group, wherein the substituent (s) is selected from the group consisting of hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted adamantyl, unsubstituted or substituted alkyl (CO), unsubstituted or substituted cycloalkyl (CO), unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted aralkyl, unsubstituted or ameschenny heteroarylalkyl and unsubstituted or substituted heterocyclylalkyl; ! R3 is halogen, haloalkyl, nitro, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl; ! R4 is hydrogen, halogen, hydroxy, alkynyl, trialkylsilylalkynyl or a substituted amino group, wherein the substituent (s) is selected from the group consisting of hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkyl (CO), unsubstituted or substituted cycloalkyl (CO), unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted aralkyl, unsubstituted or substituted heteroarylalkyl and unsubstituted or substituted heterocyclylalkyl; and! A is a bond, alkanediyl, alkenediyl and