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    • 8. 发明申请
    • 1-THIA-2,4A-DIAZA-CYCLOPENTA[B]NAPHTHALENE-3,4-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
    • 1-THIA-2,4A-DIAZA-CYCLOPENTA [B]萘普生-3,4-二酮及相关化合物作为抗感染剂
    • WO2006074317A1
    • 2006-07-13
    • PCT/US2006/000371
    • 2006-01-05
    • ACHILLION PHARMACEUTICALS, INC.BRADBURY, Barton, JamesWILES, Jason, Allan
    • BRADBURY, Barton, JamesWILES, Jason, Allan
    • C07D513/14A61P31/00
    • C07D513/14
    • The invention provides compounds and salts of Formula (I) and Formula (II) which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
    • 本发明提供具有抗微生物活性的式(I)和式(II)的化合物和盐。 本发明还提供了可用于制备式(I)和式(II)的化合物的新型合成中间体。 变量A 1,A 8,R 2,R 3,R 5,/ 3 >,R 6,R 7和R 9在本文中定义。 本文公开的某些式(I)和式(II)化合物是细菌DNA合成和细菌复制的有效和选择性抑制剂。 本发明还提供包含一种或多种式(I)或式(II)化合物和一种或多种载体,赋形剂或稀释剂的抗微生物组合物,包括药物组合物。 这样的组合物可以含有作为唯一活性剂的式(I)或式(II)的化合物或可以含有式(I)或式(II)的化合物与一种或多种其它活性剂的组合。 本发明还提供了治疗动物微生物感染的方法。