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91. 发明授权

US08377918B2 Apigenin for chemoprevention, and chemotherapy combined with therapeutic reagents 有权
标题翻译：芹菜素进行化学预防，化疗联合治疗试剂
公开(公告)号：US08377918B2
公开(公告)日：2013-02-19
申请号：US11344725
申请日：2006-01-31
申请人： Bing-Hua Jiang , Jing Fang
发明人： Bing-Hua Jiang , Jing Fang
IPC分类号： A01N43/00 , A01N43/16
CPC分类号： A61K31/353
摘要： Apigenin is a nontoxic compound. The present invention is appropriate for apigenin use in people who have a high risk of getting cancer, and in people who have cancer through chemoprevention and chemotherapy, respectively. We showed that apigenin inhibited cancer cell proliferation, tumor growth and angiogenesis. Apigenin selectively inhibited proliferation and induced apoptosis of cancer cells, enhanced the sensitivity of different cancer cells to different therapeutic drugs including cisplatin and taxol. Apigenin also inhibits angiogenesis and tumor growth in human cancers, and inhibits angiogenic inducers such as hypoxia-inducible factor 1 (HIF-1) and vascular endothelial growth factor (VEGF). Apigenin inhibited expression of HIF-1 and VEGF through PI3K, AKT, p70S6K1 and HDM2 pathways, which are commonly observed in all kinds of human cancers. Thus, our results indicate that apigenin can be applied to various human cancers for chemoprevention, and for chemotherapy when combined with other therapeutic reagents.
摘要翻译：芹菜素是无毒化合物。本发明分别适用于具有高癌风险的人群和通过化学预防和化学治疗癌症的人中的芹菜素。我们显示芹菜素抑制癌细胞增殖，肿瘤生长和血管生成。芹菜素选择性抑制增殖并诱导癌细胞凋亡，增强不同癌细胞对不同治疗药物（包括顺铂和紫杉醇）的敏感性。芹菜素还抑制人类癌症中的血管发生和肿瘤生长，并抑制血管生成诱导因子如缺氧诱导因子1（HIF-1）和血管内皮生长因子（VEGF）。芹菜素通过PI3K，AKT，p70S6K1和HDM2途径抑制HIF-1和VEGF的表达，这些通常在各种人类癌症中观察到。因此，我们的研究结果表明，芹菜素可以应用于各种人类癌症用于化学预防，并且与其他治疗试剂组合时可用于化疗。

92. 发明授权

US08367652B2 Methods of treating hypertriglyceridemia 有权
公开(公告)号：US08367652B2
公开(公告)日：2013-02-05
申请号：US13610247
申请日：2012-09-11
申请人： Mehar Manku , Ian Osterloh , Pierre Wicker , Rene Braeckman , Paresh Soni
发明人： Mehar Manku , Ian Osterloh , Pierre Wicker , Rene Braeckman , Paresh Soni
IPC分类号： A61K9/48 , A61K31/33 , A61K31/02 , A01N43/00 , A01N37/06
CPC分类号： A61K31/232 , A61K31/202 , A61K45/06 , G06F19/00
摘要： In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.

93. 发明授权

US08367651B2 Solid ganaxolone formulations and methods for the making and use thereof 有权
标题翻译：固体加诺沙酮制剂及其制备和使用方法
公开(公告)号：US08367651B2
公开(公告)日：2013-02-05
申请号：US13052798
申请日：2011-03-21
申请人： Kenneth Shaw , Mingbao Zhang
发明人： Kenneth Shaw , Mingbao Zhang
IPC分类号： A01N43/00 , A61K31/33
CPC分类号： A61K31/573 , A61K9/0019 , A61K9/10 , A61K9/143 , A61K9/145 , A61K9/146 , A61K9/1676 , A61K9/2054 , A61K9/2059 , A61K9/2077 , A61K9/282 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4891 , A61K9/5026 , A61K9/5078 , A61K9/5084 , A61K31/57 , A61K47/02 , A61K47/26 , Y10S977/773 , Y10S977/775 , Y10S977/906 , Y10S977/915
摘要： In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
摘要翻译：在某些实施方案中，本发明涉及包含稳定的颗粒的组合物，所述稳定颗粒包含加纳西酮，其中颗粒的体积加权中位数直径（D50）为约50nm至约500nm。

94. 发明授权

US08367105B2 Compressed solid dosage form manufacturing process well-suited for use with drugs of low aqueous solubility and compressed solid dosage forms made thereby 有权
公开(公告)号：US08367105B2
公开(公告)日：2013-02-05
申请号：US10986494
申请日：2004-11-10
申请人： Ilan Zalit , Fanny Leska , Mali Kadosh , Dorit Marco , Yonit Messer-Triger
发明人： Ilan Zalit , Fanny Leska , Mali Kadosh , Dorit Marco , Yonit Messer-Triger
IPC分类号： A61K31/55 , A61K31/445 , A61K9/20 , A61K9/64 , A01N43/00 , A01N43/40 , A01N43/36
CPC分类号： A61K9/2077 , A61K9/2059 , A61K31/445 , A61K31/55
摘要： A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.

95. 发明授权

US08343951B2 Volatile sulfide production inhibitor and method for inhibiting the production of volatile sulfide using the inhibitor 有权
标题翻译：挥发性硫化物生成抑制剂和抑制剂抑制挥发性硫化物生成的方法
公开(公告)号：US08343951B2
公开(公告)日：2013-01-01
申请号：US12280470
申请日：2007-02-21
申请人： Kazuyuki Oku , Mayumi Kurose , Hiroto Chaen , Toshio Miyake
发明人： Kazuyuki Oku , Mayumi Kurose , Hiroto Chaen , Toshio Miyake
IPC分类号： A01N43/00 , A61K31/33 , C12P19/60
CPC分类号： A61K8/676 , A23B4/20 , A23B5/14 , A23B9/26 , A23C3/08 , A23L3/3562 , A23L5/20 , A23L5/27 , A23L13/428 , A23L15/30 , A23L17/00 , A23L27/60 , A23L33/18 , A23V2002/00 , A61K8/602 , A61K9/0014 , A61K47/22 , A61K2800/52 , A61Q19/00 , A23V2200/15 , A23V2250/708 , A23V2250/61
摘要： The object of the present invention is to establish a volatile sulfide production inhibitor that can inhibit the production of volatile sulfides from a composition and to provide a method for inhibiting the production of volatile sulfides from a composition by using the inhibitor. The object are solved by providing a volatile sulfide production inhibitor comprising L-ascorbic acid 2-glucoside as an effective ingredient and a method for inhibiting the production of volatile sulfides from a composition by incorporating the volatile sulfide production inhibitor into the composition.
摘要翻译：本发明的目的是建立一种挥发性硫化物生成抑制剂，其可以抑制组合物中挥发性硫化物的产生，并提供通过使用该抑制剂从组合物中抑制挥发性硫化物生成的方法。该目的通过提供一种包含L-抗坏血酸2-葡萄糖苷作为有效成分的挥发性硫化物生成抑制剂和通过将挥发性硫化物生成抑制剂掺入组合物中来抑制从组合物中产生挥发性硫化物的方法来解决。

96. 发明授权

US08338404B2 Composition and method for reducing allergen 失效
标题翻译：降低过敏原的组合物和方法
公开(公告)号：US08338404B2
公开(公告)日：2012-12-25
申请号：US11853401
申请日：2007-09-11
申请人： Tetsuo Nakano , Hideo Kawabe , Keiichirou Inui , Kouichi Waki
发明人： Tetsuo Nakano , Hideo Kawabe , Keiichirou Inui , Kouichi Waki
IPC分类号： A01N43/00 , A61K31/33
CPC分类号： A61K31/401
摘要： This invention relates to an allergen-reducing composition comprising a hydroxyproline derivative, a polymer thereof, or a salt of such a derivative or polymer, which is capable of reducing the allergenicity of mites, pollens, or other allergens and is capable of imparting functions of reducing allergenicity to fibers or textiles such as a carpet, a tatami mat, a bed cloth, a curtain, clothing, a stuffed animal, a mask, a filter material, or a dust bag for an electric vacuum cleaner without discoloration; and a method for reducing allergens using such composition.
摘要翻译：本发明涉及包含羟脯氨酸衍生物，其聚合物或这种衍生物或聚合物的盐的变应原减少组合物，其能够降低螨虫，花粉或其它过敏原的变应原性，并且能够赋予减轻对诸如地毯，榻榻米，床布，窗帘，衣物，填充动物，面罩，过滤材料或用于电动吸尘器而不变色的防尘袋的纤维或纺织品的变应原性; 以及使用这种组合物减少过敏原的方法。

97. 发明授权

US08318721B2 Topical pharmaceutical composition comprising a cholinergic agent or a calcium channel blocker 有权
标题翻译：包含胆碱能药物或钙通道阻断剂的局部药物组合物
公开(公告)号：US08318721B2
公开(公告)日：2012-11-27
申请号：US13178567
申请日：2011-07-08
申请人： Michael A. Kamm , Robin K. S. Phillips
发明人： Michael A. Kamm , Robin K. S. Phillips
IPC分类号： A01N43/00 , A61K31/55 , A61K31/13
CPC分类号： A61K31/554 , A61K9/0031 , A61K31/27 , A61K31/55 , A61K31/573 , A61K47/10 , A61K47/14 , A61K47/20 , A61K2300/00
摘要： A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers.
摘要翻译：提供了用于治疗肛门直肠疾病和控制与之相关的疼痛的方法和组合物。该方法包括向需要这种治疗的受试者施用单独或与一氧化氮供体一起治疗有效量的钙通道阻断剂。氨氯地平，阿尼膦平，阿维地平，地西泮，依替地平，非洛地平，伊立替尼，伊西地平，非洛地平，伊立平，拉西地平，替卡西汀，利多匹嗪，马尼地平，米替尼滨，尼卡地平，硝苯地平，尼洛地平，尼伐地平，尼莫地平，尼索地平，尼群地平，其药学上可接受的盐是合适的钙通道阻断剂。

98. 发明授权

US08318715B2 Methods of treating hypertriglyceridemia 有权
公开(公告)号：US08318715B2
公开(公告)日：2012-11-27
申请号：US13282145
申请日：2011-10-26
申请人： Mehar Manku , Ian Osterloh , Pierre Wicker , Rene Braeckman , Paresh Soni
发明人： Mehar Manku , Ian Osterloh , Pierre Wicker , Rene Braeckman , Paresh Soni
IPC分类号： A01N43/00 , A01N37/06 , A61K31/33 , A61K31/02 , A61K9/48
CPC分类号： A61K31/232 , A61K31/202 , A61K45/06 , G06F19/00
摘要： In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.

99. 发明授权

US08318713B2 Potentiation of cancer chemotherapy by 7-(2, 5-dihydro-4-imidazo [1, 2-A] pyridine-3-yl-2,5-Dioxo-1H-pyrrol-3-yl)-9-fluoro-1,2,3,4 tetrahydro-2-(1-piperidinyl-carbonyl)-pyrrolo [3,2,1-jk] [1,4] benzodiazepine 有权
标题翻译： 7-（2,5-二氢-4-咪唑并[1,2-A]吡啶-3-基-2,5-二氧代-1H-吡咯-3-基）-9-氟-1 ，2,3,4四氢-2-（1-哌啶基 - 羰基） - 吡咯并[3,2,1-jk] [1,4]苯并二氮杂
公开(公告)号：US08318713B2
公开(公告)日：2012-11-27
申请号：US12664664
申请日：2008-06-20
申请人： Marcio Chedid , Thomas Albert Engler
发明人： Marcio Chedid , Thomas Albert Engler
IPC分类号： A01N43/00 , A01N43/62 , A61K31/33 , A61K31/55
CPC分类号： A61K31/724 , A61K31/4745 , A61K31/4985 , A61K31/513 , A61K31/5517 , A61K31/555 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K2300/00
摘要： A method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions comprising 7-(2,5-dihydro-4-imidazo[1,2-a]pyridine-3-yl-2,5-dioxo-IH-pyrrol-3-yl)-9-fluoro-1,2,3,4-tetrahydro-2-(1-piperidinyl-carbonyl)-pyrrolo[3,2,1-jk][1,4]benzodiazepine, useful for the method and a process for preparing said compositions.
摘要翻译：描述了一种治疗患者的胃癌，卵巢癌，非小细胞肺癌或结肠直肠癌的方法，以及包含7-（2,5-二氢-4-咪唑并[1,2-a ]吡啶-3-基-2,5-二氧代-1H-吡咯-3-基）-9-氟-1,2,3,4-四氢-2-（1-哌啶基 - 羰基） - 吡咯并[3， 2,1-jk] [1,4]苯并二氮杂，可用于该方法和制备所述组合物的方法。

100. 发明授权

US08288434B2 Topical pharmaceutical formulations containing a low concentration of benzoyl peroxide in suspension in water and a water-miscible organic solvent 有权
标题翻译：在水中悬浮液中含有低浓度过氧化苯甲酰和水混溶性有机溶剂的局部药物制剂
公开(公告)号：US08288434B2
公开(公告)日：2012-10-16
申请号：US12455525
申请日：2009-06-03
申请人： Yunik Chang , Gordon J. Dow
发明人： Yunik Chang , Gordon J. Dow
IPC分类号： A01N43/36 , A01N43/00 , A01N31/00 , A61K31/40 , A61K31/33 , A61K31/075
CPC分类号： A61K31/7056 , A61K8/0241 , A61K8/042 , A61K8/044 , A61K8/345 , A61K8/38 , A61K8/55 , A61K9/0014 , A61K9/14 , A61K31/075 , A61K31/235 , A61K31/327 , A61K45/06 , A61K47/10 , A61K47/32 , A61K2800/33 , A61K2800/413 , A61Q19/00 , A61K2300/00
摘要： An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea.
摘要翻译：用于局部施用于皮肤的水性制剂，包括水，水混溶性有机溶剂和过氧化苯甲酰，其中有机溶剂的浓度足以提供过氧化苯甲酰在水性制剂中的稳定悬浮液，而不包含表面活性剂在制剂中，其中制剂中水和有机溶剂的浓度的比例足以在施用于皮肤后将过氧化苯甲酰保持在制剂中饱和溶解度，并且其中制剂中过氧化苯甲酰的浓度小于5.0 ％和至少1.0％w / w。制剂还可以含有除了过氧化苯甲酰之外的化学化合物，其有效治疗痤疮。本发明的水性制剂可用于治疗痤疮和痤疮性红斑痤疮。

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