Medicaments containing 2-aryl-8-oxodihydropurine derivatives as the active ingredient for treating dementia, dsmnesia, learning deficit and higher brain dysfunction

摘要

A 2-aryl-8-oxodihydropurine derivative of formula (I) wherein: W is H; C1-6alkyl; halogen; C1-6alkoxy; amino; a mono- or di(C1-4alkyl)amino; or phenyl which may optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl)amino, cyano and nitro; X is H; C1-6alkyl; C3-8cycloalkyl-C1-4alkyl; C1-4alkyl substituted by a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl)amino, cyano and nitro; C3-6alkenyl; carbamoyl; di(C1-4alkyl) carbamoyl; or a group of the formula [Q]: -CH(R3)CON(R1)(R2) Y is H; C1-6alkyl; C3-8cycloalkyl; C3-8cycloalkyl-C1-4alkyl; C3-6alkenyl; a C1-4alkyl substituted by a phenyl group which may be optionally substituted with 1 or 2 with halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl)amino, cyano and nitro; or a group of the formula [Q]: -CH(R3)CON(R1)(R2); A is a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl)amino, cyano and nitro; or a monocyclic 5- or 6-membered heteroaryl group or a bicyclic heteroaryl group composed of 5- or 6-membered heteroaryls which have at least one heteroatom selected from a N, O or S and is optionally substituted by a C1-3alkyl or trifluoromethyl; R1 is a C1-6alkyl; C3-6alkenyl; C3-8cycloalkyl; C3-8cycloalkyl-C1-4alkyl; or a hydroxy-C1-4 alkyl; R2 is C1-6alkyl; C3-8cycloalkyl; a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6 alkyl, C1-6 alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl) amino, cyano and nitro; C1-4alkyl substituted by a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, mono- or di(C1-4alkyl)amino, cyano and nitro; or a monocyclic 5- or 6-membered heteroaryl group or a bicyclic heteroaryl group composed of 5- or 6-membered heteroaryls which have at least one heteroatom selected from N, O or S and is optionally substituted by a C1-3alkyl or trifluoromethyl; or R1 and R2 may optionally be taken together with the adjacent nitrogen to form a piperidine ring, a pyrrolidine ring, a morpholine ring or a piperazine ring, which may optionally be substituted by 1 or 2 C1-6alkyls respectively; R3 is H, C1-6alkyl or hydroxy-C1-4alkyl; with the proviso that either X or Y is a group of the formula [Q], and when X is a group of the formula [Q], then Y is H; C1- 6alkyl; C3-8cycloalkyl; C3-8cycloalkyl-C1-4alkyl; C3-6alkenyl; or C1-4alkyl group substituted by a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, mono- or di(C1-4alkyl) amino, cyano and nitro, and when Y is a group of the formula [Q], then X is H; C1-6alkyl; C3-8cycloalkyl- C1-4alkyl; C1-4alkyl substituted by a phenyl group which may be optionally substituted with 1 or 2 halogen, C1-6alkyl, C1-6alkoxy, trifluoromethyl, hydroxy, amino, a mono- or di(C1-4alkyl)amino, cyano and nitro; C3-6alkenyl; a carbamoyl group; or a di(C1-4alkyl)carbamoyl group, or a pharmaceutically acceptable acid addition salt thereof is used in the manufacture of a medicament for treating or preventing dementia, learning deficit, dysmnesia, disorientation based in dysmnesia or intellectual dysfunction.