发明名称 [1,2,4]Triazolo[1,5-c]pyrimidine derivatives and pharmaceutical use as adenosine A2A receptor antagonists
摘要 A [1,2,4]triazolo[1,5-c]pyrimidine derivative of formula (I) is disclosed, wherein: R1 represents substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R2 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; na and nb are the same or different, and each represents an integer of 0 to 4; Q represents a hydrogen atom or 3,4-dimethoxybenzyl; R6 represents a hydrogen atom, substituted or unsubstituted lower alkyl, halogen, or hydroxy; R3 represents (i) hydroxy, (ii) hydroxy-lower alkyl, (iii) substituted or unsubstituted lower alkoxy, or (iv) a group selected from the group consisting of substituted or unsubstituted imidazo[1,2-a]pyridyl, substituted or unsubstituted imidazo[1,2-a]pyrazinyl, substituted or unsubstituted imidazo[1,2-a]pyrimidinyl, substituted or unsubstituted benzimidazolyl; substituted or unsubstituted benzothiazolyl, substituted or unsubstituted benzo-2,1,3-thiadiazolyl, substituted or unsubstituted isoxazolyl, and substituted or unsubstituted 3-oxo-3,4-dihydro-2H-benzo[1,4]oxazinyl; and when R3 represents hydroxy, hydroxy-lower alkyl, or substituted or unsubstituted lower alkoxy, R4 and R5 are the same or different, and each represents substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl, or R4 and R5 form a substituted or unsubstituted saturated carbocycle together with the adjacent carbon atom, and when R3 represents a group selected from the group consisting of substituted or unsubstituted imidazo[1,2-a]pyridyl, substituted or unsubstituted imidazo[1,2-a]pyrazinyl, substituted or unsubstituted imidazo[1,2-a]pyrimidinyl, substituted or unsubstituted benzimidazolyl, substituted or unsubstituted benzothiazolyl, substituted or unsubstituted benzo-2,1,3-thiadiazolyl, substituted or unsubstituted isoxazolyl, and substituted or unsubstituted 3-oxo-3,4-dihydro-2H-benzo[1,4]oxazinyl, R4 and R5 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or substituted or unsubstituted aryl, or R4 and R5 form a substituted or unsubstituted saturated carbocycle together with the adjacent carbon atom; or a pharmaceutically acceptable salt thereof. [1,2,4]triazolo[1,5-c]pyrimidine derivative of formula (I) may be used for preventing or treating disease induced by hyperactivity of an adenosine A2A receptor.
申请公布号 NZ510629(A) 申请公布日期 2003.04.29
申请号 NZ19990510629 申请日期 1999.09.22
申请人 KYOWA HAKKO KOGYO CO 发明人 KANDA, TOMOYUKI;KUWANA, YOSHIHISA;SHIMADA, JUNICHI;IMMA, HIRONORI;OSAKADA, NAOTO;SHIOZAKI, SHIZUO
分类号 A61P25/24;A61P25/28;C07D487/04;(IPC1-7):C07D487/04;A61K31/519 主分类号 A61P25/24
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