Dementia remedies containing 2-aryl-8-oxodihydropurine derivatives as the active ingredient
View Patent ↗Medicines for treatment or prevention of dementia comprising 2-aryl-8-oxodihydropurine derivatives of the formula (I): wherein W is H, C 1-6 alkyl, halogen, C 1-6 alkoxy, or the like; X is H, C 1-6 alkyl, a group of the formula (Q): —CH(R 3 )CON(R 1 ) (R 2 ) (wherein R 1 is a C 1-6 alkyl or the like; R 2 is phenyl-substituted C 1-4 alkyl or the like; and R 3 is H or the like); Y is H, C 1-6 alkyl, a group of the above formula (Q), or the like; and A is substituted phenyl or the like, with the proviso that one of X and Y is a group of the formula (Q) and the other is a group selected from those defined for X or Y except the groups (Q), or pharmaceutically acceptable acid addition salts thereof. The above compounds exhibit an extremely potent ameliorating effect on learning disorder and/or dymnesia and thus are useful in the treatment or prevention of Alzheimer-type dementia, cerebrovascular dementia, senile dementia, etc.
1. A method for the treatment of Alzheimer-type dementia which comprises administering an effective amount of a 2-aryl-8-oxodihydropurine derivative of the formula (Ia):
wherein:
R 12 and R 22 are the same or different and are an ethyl group, a propyl group or a butyl group; or R 12 is a methyl group, an ethyl group or a propyl group, and R 22 is a phenyl group, a halogenophenyl group, a methoxyphenyl group, a benzyl group, a halogenobenzyl group or a methoxybenzyl group;
R 32 is a hydrogen atom;
Y 1 is a hydrogen atom, a methyl group or an ethyl group;
R 42 is a hydrogen atom, a halogen atom, a methyl group, a methoxy group, a nitro group or a trifluoromethyl group,
or a pharmaceutically acceptable acid addition salt thereof, to a mammal in need of such treatment of Alzheimer-type dementia.
2. A method for the treatment of Alzheimer-type dementia which comprises administering an effective amount of a 2-aryl-8-oxodihydropurine derivative of the formula (Ib):
wherein:
X 1 is a hydrogen atom, a methyl group, an ethyl group or a propyl group;
R 13 and R 23 are the same or different and are an ethyl group, a propyl group or a butyl group; or R 13 is a methyl group, an ethyl group or a propyl group, and R 23 is a phenyl group, a halogenophenyl group, a methoxyphenyl group, a benzyl group, a halogenobenzyl group or a methoxybenzyl group;
R 33 is a hydrogen atom;
R 43 is a hydrogen atom, a halogen atom, a methyl group, a methoxy group, a nitro group or a trifluoromethyl group,
or a pharmaceutically acceptable acid addition salt thereof, to a mammal in need of such treatment of Alzheimer-type dementia.
3. A method for the treatment of Alzheimer-type dementia which comprises administering an effective amount of a compound which is selected from the following compounds,
N-(4-methoxyphenyl)-7,8-dihydro-7-methyl-N-methyl-8-oxo-2-phenyl-9H-purin-9-acetamide,
N-benzyl-N-ethyl-8,9-dihydro-9-methyl-8-oxo-2-phenyl-7H-purin-7-acetamide,
N-ethyl-8,9-dihydro-9-methyl-8-oxo-2-phenyl-N-phenyl-7H-purin-7-acetamide, and
N-benzyl-7-ethyl-N-ethyl-7,8-dihydro-8-oxo-2-phenyl-9H-purin-9-acetamide,
or a pharmaceutically acceptable acid addition salt thereof, to a mammal in need of such treatment of Alzheimer-type dementia.
4. A method for the treatment of Alzheimer-type dementia which comprises administering an effective amount of N-benzyl-N-ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-acetamide, or a pharmaceutically acceptable acid addition salt thereof, to a mammal in need of such treatment of Alzheimer-type dementia.