ISOQUINOLINE COMPOUNDS HAVE STRONG AFFINITY FOR MELATONIN RECEPTOR AND SELECTIVITY FOR ONE OR ANOTHER OF THE MELATONINERGIC RECEPTOR SUB-TYPES, PREPARATION PROCESS THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

摘要

PURPOSE: Isoquinoline compounds, a preparation process thereof and pharmaceutical compositions containing the same are provided. The isoquinoline compounds have strong affinity for melatonin receptor and selectivity for one or another of the melatoninergic receptor sub-types, and are thus useful for treatment of disease associated with melatoninergic system. CONSTITUTION: The isoquinoline compounds represented by formula (I), enantiomers and diastereoisomers thereof, or addition salts thereof with a pharmaceutically acceptable acid or base are provided, wherein n is 1, 2 or 3; A is NRCZR', CZNRR' or NRCZNR'R"; Z is sulphur or oxygen; R and R''are the same or different, and are independently hydrogen or linear or branched (C1-C6)alkyl; R' is linear or branched (C1-C6)alkyl, linear or branched (C2-C6)alkenyl, linear or branched (C2-C6)alkynyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, aryl, aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, heteroaryl or heteroaryl(C1-C6)alkyl in which the alkyl moiety is linear or branched; X is nitrogen or N-R1; R1 is hydrogen or linear or branched (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, aryl, aroyl, aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, heteroaryl, heteroaroyl or heteroaryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched; and R2 is linear or branched (C1-C6)alkoxy, (C3-C8)cycloalkyloxy or (C3-C8)cycloalkyl-(C1-C6)alkyloxy in which the alkyloxy moiety is linear or branched.