Patent ID: 6372740
Filing Date: 2002-04-16
Classification: A61P,C07D

Abstract:
A 2-aryl-8-oxodihydropurine derivative of the following formula wherein:W is a hydrogen atom, a lower alkyl group, a halogen atom, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group, or a phenyl group which may optionally be substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group; X is a hydrogen atom, a lower alkyl group, a cycloalkyl-lower alkyl group, an alkyl group having 1 to 4 carbon atoms which is substituted by a phenyl group being optionally substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group, a lower alkenyl group, a carbamoyl group, a di-lower alkylcarbamoyl group, or a group of the formula (Q): â€”CH(R3)CON(R1)(R2)â€ƒâ€ƒ(Q) â€ƒwherein: R1 is a lower alkyl group, lower alkenyl group, a cycloalkyl group, a cycloalkyl-lower alkyl group, or a hydroxyl-lower alkyl group, R2 is a lower alkyl group, a cycloalkyl group, a phenyl group which may optionally be substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group, an alkyl group having 1 to 4 carbon atoms which is substituted by a phenyl group being optionally substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group, or a 5-membered or 6-membered monocyclic heteroaryl group or a bicyclic heteroaryl group, each ring having 5 or 6 members, which heteroaryl group may optionally be substituted by a C1-C3 alkyl group or a trifluoromethyl group, and has at least one of a nitrogen atom, an oxygen atom and a sulfur atom, or R1 and R2 may combine together with the adjacent nitrogen atom to form a piperidine ring, a pyrrolidine ring, a morpholine ring or a piperazine ring, and these rings may optionally be substituted by one or two lower alkyl groups, and R3 is a hydrogen atom, a lower alkyl group, or a hydroxy-lower alkyl group; Y is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkyl-lower alkyl group, a lower alkenyl group, an alkyl group having 1 to 4 carbon atoms which is substituted by a phenyl group being optionally substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group, or a group of the formula (Q): â€ƒâ€”CH(R3)CON(R1)(R2)â€ƒâ€ƒ(Q)wherein R1, R2 and R3 are the same as defined above; and A is a phenyl group which may optionally be substituted by one or two groups selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group, a hydroxyl group, an amino group, a mono- or di-lower alkylamino group, a cyano group and a nitro group, or a 5-membered or 6-membered monocyclic heteroaryl group or a bicyclic heteroaryl group, each ring having 5 or 6 members, which heteroaryl group may optionally be substituted by a C1-C3 alkyl group or a trifluoromethyl group, and has at least one of a nitrogen atom, an oxygen atom and a sulfur atom; provided that one of X and Y of the above formula(I) is the group of the formula (Q), and the other is not the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof.