4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION
    5.
    发明申请
    4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 审中-公开
    4-氨基-4-氧杂多酚类环状类似物,病毒复制抑制剂

    公开(公告)号:US20100152103A1

    公开(公告)日:2010-06-17

    申请号:US12635049

    申请日:2009-12-10

    IPC分类号: A61K38/12 C07K5/12 A61P31/12

    摘要: The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof.The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.

    摘要翻译: 本发明提供了式I的4-氨基-4-氧代丁酰基肽及其环状类似物及其药学上可接受的盐。 变量在此定义。 某些式I化合物可用作抗病毒剂。 本文公开的4-氨基-4-氧代丁酰基肽环类似物是病毒复制,特别是丙型肝炎病毒复制的有效和/或选择性抑制剂。 本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽环状类似物和一种或多种药学上可接受的载体的药物组合物。 这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽环类似物作为唯一的活性剂,或者可以含有4-氨基-4-氧代丁酰基肽环类似物和一种或多种其它药物活性剂的组合。 本发明还提供了用于治疗患者中的病毒感染(包括丙型肝炎感染)的方法。

    4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
    10.
    发明申请
    4-SUBSTITUTED-1H-ISOTHIAZOLO[5,4-B][1,4]OXAZINO[2,3,4-IJ]QUINOLINE-7,8(2H,9H)-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS 审中-公开
    4-取代的1H-异亮氨酸[5,4-B] [1,4]氧杂嗪[2,3,4-I]喹啉-7,8(2H,9H) - 和相关化合物作为抗感染剂

    公开(公告)号:US20090012071A1

    公开(公告)日:2009-01-08

    申请号:US12108106

    申请日:2008-04-23

    CPC分类号: C07D513/16

    摘要: The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted-1H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.

    摘要翻译: 本发明提供具有抗微生物活性的具有下式的化合物。 本文提供的某些化合物具有有效的抗细菌,抗原生动物或抗真菌活性。 本文提供的具体化合物也是微生物DNA合成和繁殖的有效和/或选择性抑制剂。 本发明提供包含本发明化合物和一种或多种或多种载体的抗微生物组合物,包括药物组合物。 本发明提供含有4-取代-1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7,8(2H,9H) - 二酮或相关 化合物作为唯一的活性剂或与一种或多种其它活性剂组合。 本发明通过施用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij],提供了治疗或预防微生物感染,优选动物的方法。 喹啉-7,8(2H,9H) - 二酮或相关化合物与患有或易感微生物感染的生物体接触。 本发明还提供了通过应用有效量的4-取代的1H-异噻唑并[5,4-b] [1,4]恶嗪并[2,3,4-ij]喹啉-7 ,8(2H,9H) - 二酮或相关化合物。