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1. 发明申请

WO2006083779A3 PHARMACEUTICAL COMPOSITION COMPRISING HYDROXYLATED NEBIVOLOL 审中-公开
标题翻译：包含羟化的NEBIVOLOL的药物组合物
公开(公告)号：WO2006083779A3
公开(公告)日：2006-11-23
申请号：PCT/US2006003252
申请日：2006-01-30
申请人： MYLAN LAB INC , O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW , WU JINN
发明人： O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW , WU JINN
IPC分类号： A61K31/353 , A61P9/00 , A61P9/08 , C07D311/58
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 have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites to treat cardiovascular diseases. 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.
摘要翻译：在急性给药后，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，具有增加慢性给药后人体内皮细胞中NO释放能力的能力。本发明提供了治疗心血管疾病的羟基化奈比洛尔代谢物。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。

2. 发明申请

WO2006083780A3 GLUCURONIDATED NEBIVOLOL 审中-公开
公开(公告)号：WO2006083780A3
公开(公告)日：2006-11-23
申请号：PCT/US2006003253
申请日：2006-01-30
申请人： MYLAN LAB INC , O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW
发明人： O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW
IPC分类号： C07H7/033 , A61K31/7012 , A61P9/00 , A61P9/08
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 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.
摘要翻译：本发明提供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。

3. 发明专利

AP2672A Glucuronidate nebivoloi metabolites 未知
公开(公告)号：AP2672A
公开(公告)日：2013-05-23
申请号：AP2007004104
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： DUNCAN JOSEPH , O'DONNELL JOHN , OWENS WALTER
IPC分类号： A61K31/7048 , A61L9/04
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.

4. 发明专利

CA2596428A1 GLUCURONIDATED NEBIVOLOL 未知
公开(公告)号：CA2596428A1
公开(公告)日：2006-08-10
申请号：CA2596428
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： SHAW ANDREW , DUNCAN JOSEPH , OWENS WALTER , O'DONNELL JOHN P
IPC分类号： C07H15/26 , A61K31/7048 , A61K45/06 , A61P9/00
摘要： This invention provides glucuronidated nebivolol metabolites and pharmaceutical compositions of glucuronidated nebivolol 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.

5. 发明专利

SG175477A1 HYDROXYLATED NEBIVOLOL METABOLITES 未知
公开(公告)号：SG175477A1
公开(公告)日：2011-11-28
申请号：SG2010030559
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW , WU JINN
摘要： HYDROXYLATED NEBIVOLOL METABOLITESHydroxylated nebivolol metabolites increase NO release from human endothelialcell preparations in a concentration dependent fashion following acuteadministration. In addition, hydroxylated nebivolol metabolites, including but notlimited to 4-hydroxy- 6,6'difluoro have the ability to increase the capacity for NOrelease in human endothelial cells following chronic administration. Thisinvention provides hydroxylated nebivolol metabolites to treat cardiovasculardiseases. In addition, this invention provides methods of treating and/orpreventing vascular diseases by administering at least one hydroxylatedmetabolite of nebivolol that is capable of releasing a therapeutically effectiveamount of nitric oxide to a targeted site affected by the vascular disease.Figure: None

6. 发明专利

SG175476A1 GLUCURONIDATED NEBIVOLOL METABOLITES 未知
公开(公告)号：SG175476A1
公开(公告)日：2011-11-28
申请号：SG2010030542
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW
摘要： GLUCURONIDATED NEBIVOLOL METABOLITESThis invention provides glucuronidated nebivolol metabolites and pharmaceuticalcompositions of glucuronidated nebivolol for treatment of cardiovascular diseases.In addition, this invention also provides compositions comprising nebivolol and/orat least one glucuronidated metabolite of nebivolol and/or at least one other activecompound in a pharmaceutically acceptable carrier. This invention also providesmethods of treating and/or preventing vascular diseases, by administering at leastone glucuronidated metabolite of nebivolol that is capable of releasing atherapeutically effective amount of nitric oxide to a targeted site affected by thevascular disease.Figure: None

7. 发明专利

NZ560386A Pharmaceutical composition comprising hydroxylated nebivolol 未知
公开(公告)号：NZ560386A
公开(公告)日：2009-12-24
申请号：NZ56038606
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： O'DONNELL JOHN P , OWENS WALTER , DUNCAN JOSEPH , SHAW ANDREW , WU JINN
IPC分类号： A61K31/353 , A61P9/00 , A61P9/08 , C07D311/58
摘要： Disclosed is a pharmaceutical composition comprising at least one stereoisomer of a hydroxyl substituted metabolite of nebivolol as defined in formula I, wherein one or more of positions 3-5, 7, 8 and 3'-5', 7', 8' is substituted with a hydroxyl group, or a pharmaceutically acceptable salt thereof, and a pharmaceutically-acceptable carrier. Also disclosed is the use of at least one stereoisomer of a hydroxyl substituted metabolite of nebivolol as defined above, and at least one other active agent in the preparation of a medicament for treating and/or preventing a cardiovascular disorder. The use of the medicament for improving NO release in a black patient is also disclosed.

8. 发明专利

CA2596426A1 PHARMACEUTICAL COMPOSITION COMPRISING HYDROXYLATED NEBIVOLOL 未知
公开(公告)号：CA2596426A1
公开(公告)日：2006-08-10
申请号：CA2596426
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： WU JINN , DUNCAN JOSEPH , SHAW ANDREW , O'DONNELL JOHN P , OWENS WALTER
IPC分类号： A61K31/353 , A61P9/00 , A61P9/08 , C07D311/58
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.

9. 发明专利

AU2006210953A1 Glucuronidated nebivolol 未知
公开(公告)号：AU2006210953A1
公开(公告)日：2006-08-10
申请号：AU2006210953
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： SHAW ANDREW , O'DONNELL JOHN P , DUNCAN JOSEPH , OWENS WALTER
IPC分类号： C07H7/033 , A61K31/7012 , A61P9/00 , A61P9/08
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.

10. 发明专利

AP2764A Hydroxylated nebivolol metabolites 未知
公开(公告)号：AP2764A
公开(公告)日：2013-09-30
申请号：AP2007004089
申请日：2006-01-30
申请人： MYLAN LAB INC
发明人： DUNCAN JOSEPH , O'DONNELL JOHN P , OWENS WALTER
IPC分类号： A61K31/353 , A61P9/00 , A61P9/08
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.

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