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    Substituted phenylindoles for the treatment of HIV
    47.
    发明授权
    Substituted phenylindoles for the treatment of HIV 有权
    用于治疗HIV的取代的苯基吲哚

    公开(公告)号：US07365090B2

    公开(公告)日：2008-04-29

    申请号：US10637949

    申请日：2003-08-07

    申请人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

    发明人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

    IPC分类号： A61K31/405 ,  C07D209/14

    CPC分类号： C07D403/04 ,  C07D209/42 ,  C07D403/12

    摘要： This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4′ and 5′, 5′ and 6′ or the 5′ and 7′ positions, optionally in combination with disubstitution at positions 3″ and 5″ on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF3, methoxy, CN, and NO2.

    摘要翻译： 本发明在可用于治疗HIV感染的苯基吲哚的区域中，特别是对抗HIV抗性菌株显示出显着活性的苯基吲哚。 苯吲哚在吲哚官能团的苯并环上具有至少两个除氢之外的取代基，优选在4'和5'，5'和6'或5'和7'位置，任选地与3位的取代基组合 “和5”，化合物的吲哚基上的位置-2的含羧酰胺的部分。 甲基是在苯环上取代的优选基团。 吲哚官能团的苯并环的优选取代基包括但不限于氯，氟，溴，碘，CF 3，甲氧基，CN和NO 2。

    BETA-L-2' DEOXYNUCLEOSIDES FOR THE TREATMENT OF RESISTANT HBV STRAINS AND COMBINATION THERAPIES
    48.
    发明申请
    BETA-L-2' DEOXYNUCLEOSIDES FOR THE TREATMENT OF RESISTANT HBV STRAINS AND COMBINATION THERAPIES 有权
    用于治疗耐药性HBV菌株和组合治疗的BETA-L-2'脱氧核糖核酸

    公开(公告)号：US20110172178A1

    公开(公告)日：2011-07-14

    申请号：US13052750

    申请日：2011-03-21

    申请人： David Standring ,  Jean-Pierre Sommadossi ,  April L. Patty ,  Maria Seifer

    发明人： David Standring ,  Jean-Pierre Sommadossi ,  April L. Patty ,  Maria Seifer

    IPC分类号： A61K31/7072 ,  A61K31/7068 ,  A61P31/20

    CPC分类号： A61K45/06 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K38/21

    摘要： It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a β-L-2′-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.

    摘要翻译： 已经发现，-L-2'-脱氧核苷对具有突变的耐药性乙型肝炎病毒具有活性。 提供了一种治疗宿主中拉米夫定耐药HBV（M552V）的方法，其包括施用一种β-2'-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 另外，提供了一种用于预防在初始宿主中发生拉米夫定耐药性HBV（M552V）突变的方法，其包括施用一种β-2'-脱氧核苷或其药学上可接受的盐，酯或前药。 还提供了用于预防和/或抑制宿主中HBV双突变体（L528M / M552V）的出现的方法，其包括施用＆bgr。-L-2'-脱氧核苷或其药学上可接受的盐，酯或前药。