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    • 9. 发明公开
    • HIV 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체
    • 具有艾滋病毒整合的抑制活性的多环碳酰胺基衍生物
    • KR1020080064182A
    • 2008-07-08
    • KR1020087012320
    • 2006-10-26
    • 시오노기세야쿠 가부시키가이샤
    • 요시다,히로시카와스지,타카시타이시,테르히코타오다,요시유키
    • C07D471/14C07D498/14C07D471/20A61K31/4985
    • C07F9/6561C07D471/04C07D471/14C07D471/20C07D498/14
    • Disclosed is a novel compound having an anti-viral activity, particularly an inhibitory activity on HIV integrase. Also disclosed is a pharmaceutical, particularly an anti-HIV agent, comprising the compound. The compound is represented by the formula (I): (I) wherein R1 represents a hydrogen or a lower alkyl; X represents a lower alkylene or the like; R2 represents an aryl which may be substituted; R3 represents a hydrogen, a halogen, a hydroxy, or the like; R4 represents a hydrogen, a lower alkyl group which may be substituted or the like; the broken line represents the presence or absence of a bond; one of B1 and B2 represents CR20R21 and the other represents NR22 wherein no broken line is present, or B1 and B2 independently represent C, CR23 or N wherein the B1 moiety and the B2 moiety may together form a heterocyclic ring which may be substituted; and R20, R21, R22 and R23 independently represent a hydrogen, a lower alkyl which may be substituted, a cycloalkyl which may be substituted, a cycloalkyl(lower)alkyl which may be substituted or the like.
    • 公开了具有抗病毒活性的新型化合物,特别是对HIV整合酶的抑制活性。 还公开了包含该化合物的药物,特别是抗HIV剂。 该化合物由式(I)表示:(I)其中R 1表示氢或低级烷基; X表示低级亚烷基等; R2代表可被取代的芳基; R 3表示氢,卤素,羟基等; R4代表氢,可被取代的低级烷基等; 虚线代表债券的存在与否; B1和B2之一表示CR20R21,另一个表示NR22,其中不存在虚线,或B1和B2独立地表示C,CR23或N,其中B1部分和B2部分可以一起形成可被取代的杂环; 并且R 20,R 21,R 22和R 23独立地表示氢,可以被取代的低级烷基,可被取代的环烷基,可被取代的环烷基(低级)烷基等。