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1. 发明申请

WO2006119168A2 USE OF CAROTENOIDS AND/OR CAROTENOID DERIVATIVES/ANALOGS FOR REDUCTION/INHIBITION OF CERTAIN NEGATIVE EFFECTS OF COX INHIBITORS 审中-公开
标题翻译：用于减少/抑制COX抑制剂某些负面影响的CAROTENOIDS和/或CAROTENOID衍生物/模拟物
公开(公告)号：WO2006119168A2
公开(公告)日：2006-11-09
申请号：PCT/US2006016590
申请日：2006-05-02
申请人： HAWAII BIOTECH INC , LOCKWOOD SAMUEL F , MASON R PRESTON
发明人： LOCKWOOD SAMUEL F , MASON R PRESTON
CPC分类号： A61K31/415 , A61K31/015 , A61K31/196 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： Administering carotenoids, and in particular xanthophyll carotenoids, or analogs or derivatives of astaxanthin, lutein, zeaxanthin, lycoxanthin, lycophyll, or lycopene to a subject undergoing treatment with COX-2 inhibitor drugs may reduce at least a portion of the adverse side effects associated with administration of COX-2 selective inhibitor drugs. The carotenoids, or analogs or derivatives thereof may be administered to a subject prior to, at the same time as, or after the commencement of COX-2 selective inhibitor drug therapy. The carotenoids, or analogs or derivatives thereof may be administered to a subject concurrently with COX-2 selective inhibitor drugs therapy. The carotenoids, or analogs or derivatives thereof may be incorporated into pharmaceutical preparation in combination with the COX-2 selective inhibitor drug or may be administered separately. Administration of the analogs or derivatives described herein may reduce peroxidation of LDL and other lipids in the serum and plasma cell membranes of subjects undergoing COX-2 selective inhibitor drug therapy. Administration of the analogs or derivatives described herein may reduce the incidence of deleterious clinical cardiovascular events undergoing COX-2 selective inhibitor drug therapy.
摘要翻译：将类胡萝卜素，特别是叶黄素类胡萝卜素或虾青素，叶黄素，玉米黄质，lycoxanthin，番茄红素或番茄红素的类似物或衍生物施用于用COX-2抑制剂药物治疗的受试者可以减少至少一部分与给予COX-2选择性抑制药物。类胡萝卜素或其类似物或衍生物可以在COX-2选择性抑制剂药物治疗开始之前，同时或之后施用于受试者。类胡萝卜素或其类似物或衍生物可以与COX-2选择性抑制剂药物治疗同时给予受试者。类胡萝卜素或其类似物或衍生物可以与COX-2选择性抑制剂药物组合引入药物制剂中，或者可以分开施用。本文所述的类似物或衍生物的施用可以减少经历COX-2选择性抑制剂药物治疗的受试者的血清和浆细胞膜中LDL和其它脂质的过氧化。本文所述的类似物或衍生物的给药可以降低经历COX-2选择性抑制剂药物治疗的有害临床心血管事件的发生率。

2. 发明申请

WO2006071351A2 SYNERGISTIC EFFECT OF AMLODIPINE AND ATORVASTATIN ON AORTIC ENDOTHELIAL CELL NITRIC OXIDE RELEASE 审中-公开
标题翻译： AMLODIPINE和ATORVASTATIN对动物内皮细胞氧化氮释放的协同作用
公开(公告)号：WO2006071351A2
公开(公告)日：2006-07-06
申请号：PCT/US2005039534
申请日：2005-10-28
申请人： MASON R PRESTON
发明人： MASON R PRESTON
IPC分类号： A61K31/44 , A61K31/40 , A61K31/401
CPC分类号： A61K31/401 , A61K31/198 , A61K31/40 , A61K31/44 , A61K45/06 , A61K2300/00
摘要： The combination of amlodipine and atorvastatin act to synergistically synthesize NO production. Moreover, the addition of a tertiary compound complements this combination of amlodipine and atorvastatin in NO production.
摘要翻译：氨氯地平和阿托伐他汀的组合起协同合成NO产生作用。此外，加入叔胺化合物可补充氨氯地平和阿托伐他汀在NO生产中的组合。

3. 发明申请

WO0064443A9 SYNERGISTIC EFFECTS OF AMLODIPINE AND ATORVASTATIN 审中-公开
标题翻译：阿米膦酸和阿托伐他汀的协同作用
公开(公告)号：WO0064443A9
公开(公告)日：2002-08-29
申请号：PCT/US0010465
申请日：2000-04-18
申请人： MASON R PRESTON
发明人： MASON R PRESTON
IPC分类号： C07D211/84 , A61K31/40 , A61K31/44 , A61K31/4422 , A61P3/06 , A61P9/00 , A61P9/10 , A61P9/12 , C07D207/34 , A61K31/4418
CPC分类号： A61K31/44 , A61K31/40 , A61K2300/00
摘要： The combination of amlodipine with either atorvastatin or atorvastatin metabolite shows a synergistic antioxidant effect on lipid peroxidation in human low-density lipoproteins and membrane vesicles enriched with polyunsaturated fatty acids. Inhibition of oxy-radical damage by this drug combination was observed at therapeutic levels in a manner that could not be reproduced by the combination of amlodipine with other statins or the natural antioxidant, vitamin E. The basis for this potent activity is attributed to the chemical structures of these compounds and their molecular interactions with phospholipid molecules, as determined by x-ray diffraction analyses. This combination therapy can be used to treat cardiovascular disorders, especially coronary artery disease, by increasing the resistance of low-density lipoproteins and vascular cell membranes against oxidative modification.
摘要翻译：氨氯地平与阿托伐他汀或阿托伐他汀代谢物的组合在人类低密度脂蛋白和富含多不饱和脂肪酸的膜囊泡中显示出对脂质过氧化的协同抗氧化作用。在治疗水平下，以不能通过氨氯地平与其他他汀类药物或天然抗氧化剂维生素E的组合复制的方式观察到这种药物组合的氧自由基损伤的抑制。该有效活性的基础归因于化学这些化合物的结构及其与磷脂分子的分子相互作用，通过X射线衍射分析测定。这种联合治疗可以通过增加低密度脂蛋白和血管细胞膜对氧化修饰的抵抗力来治疗心血管疾病，特别是冠状动脉疾病。

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