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    • 3. 发明授权
    • 2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof
    • 2-芳基-8-氧代二氢嘌呤衍生物,其制备方法,含有它们的药物组合物及其中间体
    • US06372740B1
    • 2002-04-16
    • US09555490
    • 2000-06-01
    • Teruya MurataKaoru MasumotoKatsunori KondoKiyoshi FurukawaMakoto Oka
    • Teruya MurataKaoru MasumotoKatsunori KondoKiyoshi FurukawaMakoto Oka
    • C02D47300
    • C07D473/00
    • 2-Aryl-8-oxodihydropurine derivative of the following 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 when one of X and Y of the above formula (I) is the group of the formula (Q), then the other is the same groups for X or Y as described above except for 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 disorders such as anxiety-related diseases (neurosis, somatoform disorders, anxiety disorders, and others), depression, epilepsy, etc., or circulatory organs disorders such as angina pectoris, hypertension.
    • 下式(I)的2-芳基-8-氧代二氢嘌呤衍生物:其中W是H,低级烷基,卤素,低级烷氧基,氨基,一或二低级烷基氨基或取代或未取代的苯基; X为H,低级烷基,环烷基 - 低级烷基,取代或未取代的苯基 - 低级烷基,低级烯基,氨基甲酰基,二低级烷基氨基甲酰基或式(Q)基团:-CH(R3)CON(R1) R2); Y为H,低级烷基,环烷基,环烷基 - 低级烷基,低级烯基,取代或未取代的苯基 - 低级烷基或式(Q)基团:-CH(R3)CON(R1)(R2) A是取代或未取代的苯基,或取代或未取代的杂芳基; 条件是当上述式(I)的X和Y之一是式(Q)的基团时,另一个是与上述相同的X或Y基团,除了式(Q), 或其药学上可接受的酸加成盐。 这些化合物可用于预防或治疗诸如焦虑相关疾病(神经症,躯体形式障碍,焦虑障碍等),抑郁症,癫痫等中枢神经障碍或循环器官疾病如心绞痛,高血压。