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59 条记录 (耗时 0.226 秒)

    Viral polymerase inhibitors
    45.
    发明授权
    Viral polymerase inhibitors 有权

    公开(公告)号：US06448281B1

    公开(公告)日：2002-09-10

    申请号：US09898297

    申请日：2001-07-03

    申请人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    IPC分类号： A81K314184

    CPC分类号： C07D401/04 ,  C07D235/18 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D417/14 ,  C07D471/04 ,  Y10S514/894

    摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

    Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
    48.
    发明授权
    Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them 失效
    哌嗪衍生物，含有这些化合物的药物组合物，其用途和制备方法

    公开(公告)号：US5700801A

    公开(公告)日：1997-12-23

    申请号：US572256

    申请日：1995-12-13

    申请人： Helmut Pieper ,  Volkhard Austel ,  Frank Himmelsbach ,  Gunter Linz ,  Brian Guth ,  Johannes Weisenberger

    发明人： Helmut Pieper ,  Volkhard Austel ,  Frank Himmelsbach ,  Gunter Linz ,  Brian Guth ,  Johannes Weisenberger

    IPC分类号： C07D295/18 ,  A61K31/495 ,  A61P7/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/34 ,  C07D211/58 ,  C07D213/74 ,  C07D213/78 ,  C07D401/12 ,  C07D211/18

    CPC分类号： C07D213/74 ,  C07D211/34 ,  C07D211/58 ,  C07D401/12

    摘要： Piperazine derivatives useful in the treatment or prevention of inflammation, bone degradation, thrombosis and tumor metastasis. Exemplary species are: (a) �4-trans-�3-�4-(4-Pyridyl)-piperazin-1-yl!propionyl!amino!-cyclohexanecarboxylic acid, (b) 3-�4-trans-�4-(4-Pyridyl)-piperazin-1-yl!carbonylamino!-cyclohexylpropionic acid, (c) 3-�4-trans-�4-(4-Pyridyl)-piperazin-1-yl!malonylamino!cyclohexylcarboxylic acid, (d) Methyl �4-trans-�3-�4-(4-pyridyl)-piperazin-1-yl!-propionyl!-amino!cyclohexane carboxylate, (e) Methyl 3-�4-trans-�4-(4-pyridyl)-piperazin-1-yl!-carbonylamino!cyclohexyl propionate, (f) Methyl �4-trans-�4-(4-pyridyl)-piperazin-1-yl!-malonylamino!-cyclohexyl carboxylate, (g) Cyclohexyl �4-trans-��4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate, and (h) Isobutyl �4-trans-��4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate.

    摘要翻译： 哌嗪衍生物可用于治疗或预防炎症，骨退化，血栓形成和肿瘤转移。 示例性物质是：（a）[4-反式 - [3- [4-（4-吡啶基） - 哌嗪-1-基]丙酰基]氨基] - 环己烷甲酸，（b）3- [4-反式 - [4 - （4-吡啶基） - 哌嗪-1-基]羰基氨基] - 环己基丙酸，（c）3- [4-反式 - [4-（4-吡啶基） - 哌嗪-1-基]丙二酰氨基]环己基羧酸， d）[4-反式 - [3- [4-（4-吡啶基） - 哌嗪-1-基] - 丙酰基] - 氨基]环己烷羧酸甲酯，（e）3- [4-反式 - [4- 4-吡啶基） - 哌嗪-1-基] - 羰基氨基]环己基丙酸酯，（f）[4-反式 - [4-（4-吡啶基） - 哌嗪-1-基] - 丙酰基氨基] ）[4-反式 - [[4-（4-吡啶基） - 哌嗪-1-基] - 乙酰基] - 氨基] - 环己烷羧酸环己酯和（h）[4-反式 - [[4- 吡啶基） - 哌嗪-1-基] - 乙酰基] - 氨基] - 环己烷羧酸酯。