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    • 2. 发明授权
    • Anti-viral compounds
    • 抗病毒化合物
    • US06358971B1
    • 2002-03-19
    • US09674037
    • 2000-12-04
    • Jesus Ezquerra-CarreraJoseph Michael GruberChafiq Hamdouchi HamdouchiRichard Elmer HolmesWayne Alfred Spitzer
    • Jesus Ezquerra-CarreraJoseph Michael GruberChafiq Hamdouchi HamdouchiRichard Elmer HolmesWayne Alfred Spitzer
    • A61K31437
    • C07D471/04
    • The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1 is hydrogen, halo, CN, C1-C4 alkyl, —C≡CH, CO(C1-C4 alkyl), CO2(C1-C4 alkyl), or CONR2R3; R2 and R3 are independently hydrogen or C1-C4 alkyl; A′ is hydrogen, halo, C1-C6 alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4 is C1-C6 alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5 is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6 is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4 alkyl, or CO2(C1-C4 alkyl), C1-C4 alkoxy; or a pharmaceutically acceptable salt thereof.
    • 本发明涉及抑制小核糖核酸病毒,肝病毒,肠病毒,心脏病毒,脊髓灰质炎病毒,A组和B组柯萨克病毒,回波病毒和孟戈病毒的生长的下列式(I)的化合物。其中A是苯基,吡啶基 取代的苯基,取代的吡啶基或苄基; R是氢,COR4或COCF3; X是N-OH,O或CHR1; R1是氢,卤素,CN,C1-C4烷基,-C = CH, C1-C4烷基),CO2(C1-C4烷基)或CONR2R3; R2和R3独立地是氢或C1-C4烷基; A'是氢,卤素,C1-C6烷基,苄基,萘基,噻吩基,呋喃基,吡啶基 ,吡咯烷基,COR4,S(O)nR4或式R4的基团是C1-C6烷基,苯基或取代的苯基; n是0,1或2; R5各自独立地为氢或卤素; m为 1,2,3或4; 或者其药学上可接受的盐,R 6是氢,卤素,CF 3,OH,CO 2 H,NH 2,NO 2,CONHOCH 3,C 1 -C 4烷基或CO 2(C 1 -C 4烷基),C 1 -C 4烷氧基。