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    • 25. 发明授权
    • Antiviral pyrimidinedione derivatives and process for the preparation thereof
    • 抗病毒嘧啶二酮衍生物及其制备方法
    • US06987114B1
    • 2006-01-17
    • US09719282
    • 2000-04-08
    • Eui-Hwan ChoSun-Gan ChungSun-Hwan LeeHo-Seok KwonJae-Eung LeeJeong-Ho Joo
    • Eui-Hwan ChoSun-Gan ChungSun-Hwan LeeHo-Seok KwonJae-Eung LeeJeong-Ho Joo
    • C07D239/54C07D239/60A61K31/513
    • C07D239/54C07D239/60C07D401/06C07D403/06C07D405/06C07D413/06
    • The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.
    • 本发明涉及下列通式(I)的嘧啶二酮衍生物,其可用作抗病毒剂,特别是作为治疗AIDS的药物,其药学上可接受的盐,其制备方法和含有该化合物的药物组合物,其中R代表环丙基; 环丁基 环己基 未取代的或具有选自羟基,C 1 -C 4 -C 4烷基,C 1 -C 3烷基的单 - ,二 - 或三取代苯基, 烷氧基,卤素,三氟甲基,氰基和氨基; 1-或2-萘基; 9-蒽基; 2-蒽醌; 未取代或取代的具有选自C 1 -C 4烷基,C 1 -C 4烷氧基的基团的吡啶基 ,氰基和卤素; 2-,3-或4-喹啉基; 环氧乙烷基 1-苯并三唑基; 2-苯并恶唑基; 被C 1 -C 4烷氧基羰基取代的呋喃基; C 1 -C 4烷基羰基; 或苯甲酰基,R 1表示卤素或C 1 -C 4烷基,R 2和R 2, 3独立地表示氢或C 1 -C 4烷基,X表示氧原子,Y表示氧原子,硫原子或羰基。