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公开(公告)号:US20050025774A1
公开(公告)日:2005-02-03
申请号:US10493280
申请日:2002-10-21
申请人: Benedetta Crescenzi , Cristina Gardelli , Ester Muraglia , Federica Orvieto , Paola Pace , Giovanna Pescatore , Alessia Petrovich , Marco Poma , Michael Rowley , Rita Scarpelli , Vincenzo Summa , Emanuela Nizi
发明人: Benedetta Crescenzi , Cristina Gardelli , Ester Muraglia , Federica Orvieto , Paola Pace , Giovanna Pescatore , Alessia Petrovich , Marco Poma , Michael Rowley , Rita Scarpelli , Vincenzo Summa , Emanuela Nizi
IPC分类号: C07D239/46 , A61K20060101 , A61K31/513 , A61K31/515 , A61K31/5377 , A61K39/00 , A61P31/18 , A61P43/00 , C07D20060101 , C07D239/54 , C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D513/04
CPC分类号: C07D239/557 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D513/04
摘要: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula (I): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译: 描述了式(I)的N-取代的5-羟基嘧啶-6-酮-4-甲酰胺:描述为HIV整合酶的抑制剂和HIV复制抑制剂,其中R 1,R 2,R 3和R <4>在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防,延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。 还描述了预防,治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。