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Hydroxylated nebivolol metabolites
专利权人:
MYLAN LABORATORIES INC
发明人:
DUNCAN JOSEPH,O'DONNELL JOHN P,OWENS WALTER
申请号:
AP200704089
公开号:
AP2764A
申请日:
2006.01.30
申请国别(地区):
AP
年份:
2013
代理人:
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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