公开(公告)号：US20110112100A1

公开(公告)日：2011-05-12

申请号：US12868342

申请日：2010-08-25

申请人： Jared Bruce John Milbank ,  David Cameron Pryde ,  Thien Duc Tran

发明人： Jared Bruce John Milbank ,  David Cameron Pryde ,  Thien Duc Tran

IPC分类号： A61K31/498 ,  C07D241/36 ,  A61P31/14

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07F5/025 ,  C07F7/0812

摘要： The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.

摘要翻译： 本发明涉及含有这些化合物的组合物以及使用这些化合物作为HCV复制抑制剂的式（I）化合物及其药学上可接受的盐。

公开(公告)号：US20110039884A1

公开(公告)日：2011-02-17

申请号：US12914530

申请日：2010-10-28

申请人： Peter H. Jones ,  David Cameron Pryde ,  Thien Duc Tran

发明人： Peter H. Jones ,  David Cameron Pryde ,  Thien Duc Tran

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P31/12 ,  A61P31/22 ,  A61P31/14

CPC分类号： C07D471/04 ,  C07D405/14

摘要： The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases.We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is —O—; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.

摘要翻译： 本发明涉及咪唑并吡啶酮，其在医药中的用途，含有它们的组合物，其制备方法和用于此类方法的中间体。 通过激活TLRs，应该可以诱导或刺激免疫细胞以产生免疫应答。 特别地，TLR7涉及病毒感染（例如HCV或HBV），癌症和肿瘤以及T2辅助细胞（TH2）介导的疾病，因此TLR7激动剂潜在地用于治疗这些疾病。 我们现在发现了一系列作为TLR7激动剂的咪唑并吡啶酮。 提供式（I）化合物或其药学上可接受的盐或溶剂合物，其中R1是3-8元饱和杂环基，其中一个环成员是-O-; 且R 2为苯基或吡啶基，各自任选被C 1 -C 6烷基取代。

公开(公告)号：US07691877B2

公开(公告)日：2010-04-06

申请号：US11675667

申请日：2007-02-16

申请人： Peter Jones ,  David Pryde ,  Thien Duc Tran

发明人： Peter Jones ,  David Pryde ,  Thien Duc Tran

IPC分类号： C07D513/02 ,  C07D515/02 ,  A01N43/42 ,  A61K31/44

CPC分类号： C07D213/80 ,  C07D213/75 ,  C07D471/04

摘要： The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.

摘要翻译： 本发明涉及通过激动作用选择性地作用于Toll样受体（TLR）的式（I）的免疫应答调节剂，其用途，其制备方法，用于其制备的中间体和含有所述抑制剂的组合物。 这些抑制剂可用于各种治疗领域，包括治疗感染性疾病如肝炎（如HCV，HBV），遗传相关的病毒感染和癌症。

公开(公告)号：US20090221631A1

公开(公告)日：2009-09-03

申请号：US12184494

申请日：2009-05-15

申请人： Peter H. JONES ,  David Cameron Pryde ,  Thien Duc Tran

发明人： Peter H. JONES ,  David Cameron Pryde ,  Thien Duc Tran

IPC分类号： A61K31/437 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D405/14

摘要： The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases.We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is —O—; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.

摘要翻译： 本发明涉及咪唑并吡啶酮，其在医药中的用途，含有它们的组合物，其制备方法和用于此类方法的中间体。 通过激活TLRs，应该可以诱导或刺激免疫细胞以产生免疫应答。 特别地，TLR7涉及病毒感染（例如HCV或HBV），癌症和肿瘤以及T2辅助细胞（TH2）介导的疾病，因此TLR7激动剂潜在地用于治疗这些疾病。 我们现在发现了一系列作为TLR7激动剂的咪唑并吡啶酮。 提供式（I）化合物或其药学上可接受的盐或溶剂合物，其中R1是3-8元饱和杂环基，其中一个环成员是-O-; 且R 2为苯基或吡啶基，各自任选被C 1 -C 6烷基取代。

公开(公告)号：US20070197478A1

公开(公告)日：2007-08-23

申请号：US11675667

申请日：2007-02-16

申请人： Peter Jones ,  David Pryde ,  Thien Duc Tran

发明人： Peter Jones ,  David Pryde ,  Thien Duc Tran

IPC分类号： A61K31/675 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D213/80 ,  C07D213/75 ,  C07D471/04

摘要： The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.

摘要翻译： 本发明涉及通过激动作用选择性地作用于Toll样受体（TLR）的式（I）的免疫应答调节剂，其用途，其制备方法，用于其制备的中间体和含有所述抑制剂的组合物。 这些抑制剂可用于各种治疗领域，包括治疗感染性疾病如肝炎（如HCV，HBV），遗传相关的病毒感染和癌症。

公开(公告)号：US20120302598A1

公开(公告)日：2012-11-29

申请号：US13302085

申请日：2011-11-22

申请人： Peter H. Jones ,  David Cameron Pryde ,  Thien Duc Tran

发明人： Peter H. Jones ,  David Cameron Pryde ,  Thien Duc Tran

IPC分类号： A61K31/437 ,  A61P31/14 ,  A61P31/22 ,  C07D471/04 ,  A61P31/20

CPC分类号： C07D471/04 ,  C07D405/14

摘要： The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases.We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is O; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.

摘要翻译： 本发明涉及咪唑并吡啶酮，其在医药中的用途，含有它们的组合物，其制备方法和用于此类方法的中间体。 通过激活TLRs，应该可以诱导或刺激免疫细胞以产生免疫应答。 特别地，TLR7涉及病毒感染（例如HCV或HBV），癌症和肿瘤以及T2辅助细胞（TH2）介导的疾病，因此TLR7激动剂潜在地用于治疗这些疾病。 我们现在发现了一系列作为TLR7激动剂的咪唑并吡啶酮。 提供式（I）化合物或其药学上可接受的盐或溶剂化物，其中R1为3-8元饱和杂环基，其中一个环成员为O; 且R 2为苯基或吡啶基，各自任选被C 1 -C 6烷基取代。