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公开(公告)号:EP1116722A1
公开(公告)日:2001-07-18
申请号:EP99944771.7
申请日:1999-09-22
发明人: SHIMADA, Junichi , IMMA, Hironori , OSAKADA, Naoto , SHIOZAKI, Shizuo , KANDA, Tomoyuki , KUWANA, Yoshihisa
IPC分类号: C07D487/04 , A61K31/505
CPC分类号: C07D487/04
摘要: [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by the general formula (I)
or pharmacologically acceptable salts thereof which show adenosine A 2A receptor antogonism, wherein R 1 represents heteroaryl, etc.; R 2 represents hydrogen, etc.; na and nb represent each an integer of 0 to 4; Q represents hydrogen, etc.; R 4 and R 5 represent each lower alkyl or aryl, or R 4 form together with the adjacent carbon atom a saturated carbon ring when R 3 is any of (i) to (iii); or R 4 represent each hydrogen, lower alkyl or aryl, or R 4 and R 5 form together with the adjacent carbon atom a saturated carbon ring when R 3 is (iv).摘要翻译: 由通式(I)表示的Ä1,2,4'-三唑并[1,5-c]嘧啶衍生物或其药理学上可接受的盐,其显示腺苷A2A受体阴性,其中R 1表示杂芳基等; R 2表示氢等; na和nb表示0〜4的整数, Q表示氢等。 当R 3是(i)至(iii)中的任何一个时,R 4和R 5各自表示低级烷基或芳基,或R 4与相邻碳原子一起形成饱和碳环。 或R 4表示当R 3为(ⅳ)时,每个氢,低级烷基或芳基,或R 4和R 5与相邻碳原子一起形成饱和碳环。
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公开(公告)号:EP1116722B1
公开(公告)日:2005-01-12
申请号:EP99944771.7
申请日:1999-09-22
发明人: SHIMADA, Junichi , IMMA, Hironori , OSAKADA, Naoto , SHIOZAKI, Shizuo , KANDA, Tomoyuki , KUWANA, Yoshihisa
IPC分类号: C07D487/04 , A61K31/505 , C07D519/00
CPC分类号: C07D487/04
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公开(公告)号:EP0976753B1
公开(公告)日:2004-01-02
申请号:EP98909835.5
申请日:1998-03-24
发明人: TSUMUKI, Hiroshi , SHIMADA, Junichi , IMMA, Hironori , NAKAMURA, Akiko , NONAKA, Hiromi , SHIOZAKI, Shizuo , ICHIKAWA, Shunji , KANDA, Tomoyuki , KUWANA, Yoshihisa , ICHIMURA, Michio , SUZUKI, Fumio
IPC分类号: C07D487/04 , A61K31/505
CPC分类号: C07D487/04
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公开(公告)号:EP0976753A1
公开(公告)日:2000-02-02
申请号:EP98909835.5
申请日:1998-03-24
发明人: TSUMUKI, Hiroshi , SHIMADA, Junichi , IMMA, Hironori , NAKAMURA, Akiko , NONAKA, Hiromi , SHIOZAKI, Shizuo , ICHIKAWA, Shunji , KANDA, Tomoyuki , KUWANA, Yoshihisa , ICHIMURA, Michio , SUZUKI, Fumio
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof are provided, which have adenosine A 2A receptor antagonism and are useful for the treatment or prevention of various diseases induced by hyperactivity of adenosine A 2A receptors (for example, Parkinson's disease or senile dementia):
wherein R 1 represents substituted or unsubstituted aryl, or the like; R 2 represents hydrogen, halogen, lower alkyl, substituted or unsubstituted aryl, or the like; R 3 represents hydrogen, halogen, XR 10 (wherein X represents O or S; and R 10 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic ring, substituted or unsubstituted aralkyl, lower alkyl, or hydroxy lower alkyl), or the like; and Q represents hydrogen or 3,4-dimethoxybenzyl.摘要翻译: 提供了由式(I)表示的三氮唑-1,5-c嘧啶衍生物或其药学上可接受的盐,其具有腺苷A2A受体拮抗作用,并且可用于治疗或预防腺苷A2A受体多动症诱导的各种疾病(对于 例如,帕金森病或老年痴呆):
其中R 1表示取代或未取代的芳基等; R 2表示氢,卤素,低级烷基,取代或未取代的芳基等; R 3表示氢,卤素,XR 10(其中X表示O或S; R 10表示取代或未取代的芳基,取代或未取代的芳族杂环,取代或未取代的芳烷基,低级烷基或羟基 低级烷基)等; Q表示氢或3,4-二甲氧基苄基。
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