利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

23 条记录 (耗时 0.032 秒)

    Hydroxylated nebivolol metabolites
    12.
    发明申请
    Hydroxylated nebivolol metabolites 审中-公开
    羟基化的奈比洛尔代谢物

    公开(公告)号：US20070014733A1

    公开(公告)日：2007-01-18

    申请号：US11342497

    申请日：2006-01-30

    申请人： John O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw ,  Jinn Wu

    发明人： John O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw ,  Jinn Wu

    IPC分类号： A61K31/353 ,  A61L9/04

    CPC分类号： C07D311/58 ,  A61K31/353

    摘要： Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

    摘要翻译： 急性给药后羟化的奈比洛尔代谢物以浓度依赖的方式增加人内皮细胞制剂的NO释放。 此外，羟基化的奈比洛尔代谢物，包括但不限于4-羟基-6,6'-二氟 - ，4-羟基-5-苯酚-6,6'-二氟和4-羟基-8-苯基-6,6 “二氟”具有增加慢性给药后人体内皮细胞NO释放能力的能力。 本发明提供羟基化的奈比洛尔代谢物和包含奈比洛尔和/或至少一种羟基化的奈必洛尔代谢物和/或用于治疗心血管疾病的至少一种另外的化合物或其药学上可接受的盐的组合物。 此外，本发明提供了治疗和/或预防血管疾病的方法，其通过施用能够将治疗有效量的一氧化氮释放到受血管疾病影响的靶位点的奈比洛尔的羟基化代谢物。 此外，本发明涉及治疗和/或预防给予至少一种羟基化的奈必洛尔代谢物的偏头痛。 本发明还可以与代谢综合征病症联合使用或作为单一治疗代用综合征病症使用。

    Glucuronidated nebivolol metabolites
    16.
    发明申请
    Glucuronidated nebivolol metabolites 审中-公开
    葡萄糖醛酸化的奈比洛尔代谢物

    公开(公告)号：US20070014734A1

    公开(公告)日：2007-01-18

    申请号：US11342889

    申请日：2006-01-30

    申请人： John O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw

    发明人： John O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw

    IPC分类号： A61K31/7048 ,  A61L9/04

    CPC分类号： A61K45/06 ,  A61K31/7012 ,  A61K31/7048 ,  A61K2300/00

    摘要： This invention provides glucuronidated nebivolol metabolites and pharmaceutical compositions of glucuronidated nebivolol metabolites for treatment of cardiovascular diseases. In addition, this invention also provides compositions comprising nebivolol and/or at least one glucuronidated metabolite of nebivolol and/or at least one other active compound in a pharmaceutically acceptable carrier. This invention also provides methods of treating and/or preventing vascular diseases, by administering at least one glucuronidated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one glucuronidated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

    摘要翻译： 本发明提供了用于治疗心血管疾病的葡糖醛酸化奈必洛尔代谢物和葡糖苷酸化奈必洛尔代谢物的药物组合物。 此外，本发明还提供在药学上可接受的载体中包含奈比洛尔和/或至少一种葡萄糖醛酸化的奈必洛尔代谢物和/或至少一种其它活性化合物的组合物。 本发明还提供了治疗和/或预防血管疾病的方法，其通过施用能够将治疗有效量的一氧化氮释放到受血管疾病影响的靶位的奈比洛尔的至少一种葡糖醛酸化代谢物。 此外，本发明涉及治疗和/或预防给予至少一种奈非洛尔的葡糖醛酸化代谢物的偏头痛。 本发明还可以与代谢综合征病症联合使用或作为单一治疗代用综合征病症使用。

    HYDROXYLATED NEBIVOLOL METABOLITES
    20.
    发明申请
    HYDROXYLATED NEBIVOLOL METABOLITES 审中-公开
    羟化的NEBIVOLOL代谢物

    公开(公告)号：US20110065783A1

    公开(公告)日：2011-03-17

    申请号：US12908336

    申请日：2010-10-20

    申请人： John P. O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw ,  Jinn Wu

    发明人： John P. O'Donnell ,  Walter Owens ,  Joseph Duncan ,  Andrew Shaw ,  Jinn Wu

    IPC分类号： A61K31/353 ,  A61P9/12

    CPC分类号： C07D311/58 ,  A61K31/353

    摘要： Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.

    摘要翻译： 急性给药后羟化的奈比洛尔代谢物以浓度依赖的方式增加人内皮细胞制剂的NO释放。 此外，羟基化的奈比洛尔代谢物，包括但不限于4-羟基-6,6'-二氟 - ，4-羟基-5-苯酚-6,6'-二氟和4-羟基-8-苯基-6,6 “二氟”具有增加慢性给药后人体内皮细胞NO释放能力的能力。 本发明提供羟基化的奈比洛尔代谢物和包含奈比洛尔和/或至少一种羟基化的奈必洛尔代谢物和/或用于治疗心血管疾病的至少一种另外的化合物或其药学上可接受的盐的组合物。 此外，本发明提供了治疗和/或预防血管疾病的方法，其通过施用能够将治疗有效量的一氧化氮释放到受血管疾病影响的靶位点的奈比洛尔的羟基化代谢物。 此外，本发明涉及治疗和/或预防给予至少一种羟基化的奈必洛尔代谢物的偏头痛。 本发明还可以与代谢综合征病症联合使用或作为单一治疗代用综合征病症使用。