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。

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。

公开(公告)号：US20120273373A1

公开(公告)日：2012-11-01

申请号：US13456581

申请日：2012-04-26

申请人： Gene Kai Jinn WU

发明人： Gene Kai Jinn WU

IPC分类号： A47G33/00

CPC分类号： A47G33/002 ,  A47G19/2205

摘要： The present invention is a single-use ergonomic chalice that has the ability to store both a liquid and a wafer commonly served during the religious ceremony known as Communion. The present invention comprises an ergonomic cup and a cup lid. The ergonomic cup is shaped to easily fit into the fingers or the hand of an individual using the ergonomic cup. Also, the fluid is stored within the ergonomic cup. The cup lid should store the wafer. The present invention may comprise multiple embodiments. Each embodiment is configured to have the cup lid attach to the ergonomic cup. A first embodiment has each the cup lid and the ergonomic cup hermetically sealed with only a single seal. A second embodiment has a seal for each the cup lid and the ergonomic cup. The cup lid may also serve as a supplemental base support for the ergonomic cup.

摘要翻译： 本发明是一种单次使用的符合人体工程学的圣杯，其具有存储在称为圣餐的宗教仪式期间通常服务的液体和晶片的能力。 本发明包括符合人体工程学的杯和杯盖。 符合人体工学的杯子的形状可以很容易地使用人体工学的杯子装入手指或个人的手中。 此外，流体存储在符合人体工程学的杯子内。 杯盖应存放晶片。 本发明可以包括多个实施例。 每个实施例被配置为使杯盖附接到人体工程学杯。 第一实施例具有每个杯盖和符合人体工程学的杯，仅用一个密封密封。 第二实施例具有用于每个杯盖和人体工程学杯的密封。 杯盖也可用作人体工程学杯的补充基座支架。