2-aryl-8-oxodihydropurine derivatives, process for producing...

C - Chemistry – Metallurgy – 07 – D

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C07D 473/00 (2006.01) A61K 31/52 (2006.01)

Patent

CA 2312885

The present invention is directed to 2-aryl-8-oxodihydropurine derivatives of the following formula (I): (see formula I) wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di- lower alkylamino, or substituted or unsubstituted phenyl; X is H, lower alkyl, cycloalkyl-lower alkyl, substituted or unsubstituted phenyl-lower alkyl, lower alkenyl, carbamoyl, di-lower alkylcarbamoyl, or a group of the formula (Q): -CH(R3)CON(R1)(R2); Y is H, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, lower alkenyl, substituted or unsubstituted phenyl-lower alkyl, or a group of the formula (Q): -CH(R3)CON(R1)(R2); A is substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; provided that one of X and Y of the above formula (I) is the group of the formula (Q), and the other is chosen from the groups for X or Y as described above, except fro the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof. These compounds are useful for the prophylaxis or treatment of central nervous system disorders such as anxiety-related diseases (neurosis, somatoform disorders, anxiety disorders, and others), depression, epilepsy, etc., or circulatory organs disorders such as angina pectoris, and hypertension.

Cette invention se rapporte à des dérivés de 2-aryl-8-oxodihydropurine, représentés par la formule générale (I) ou à des sels d'addition d'acide de ces dérivés, acceptables sur le plan pharmaceutique. Ces composés sont utiles comme remèdes et comme prophylactiques contre les maladies associées à l'anxiété (névrose, troubles psychophysiologiques, troubles de l'anxiété, etc.), contre les maladies du système nerveux central, telles que la dépression et l'épilepsie, et contre les maladies circulatoires telles que l'angine de poitrine et l'hypertension. Dans cette formule, A représente phényle éventuellement substitué ou hétéroaryle éventuellement substitué; et soit X soit Y représente [Q]:-CH(R<3>)CON(R<1>)(R<2>).

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