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    • 5. 发明申请
    • Sweet Gum Fruit Extract as a Therapeutic Agent
    • 甜胶提取物作为治疗剂
    • US20100189830A1
    • 2010-07-29
    • US12600751
    • 2008-05-21
    • Zhijun LiuPeiying YangRobert A. Newman
    • Zhijun LiuPeiying YangRobert A. Newman
    • A61K36/185A61P25/28A61P9/10A61P9/12A61P3/10A61P37/06
    • A61K36/185A61K45/06
    • Sweet gum (Liquidambar styraciflua L., family Hamamelidaceae) fruit extract was discovered to possess potent activities against multiple targets of the PBK (phosphatidylinositide 3-kinase) pathway, especially the PI3K/Akt and mTOR pathways. At a very low concentration of 1.85 μg/ml (IC50), sweet gun extract showed the ability of simultaneously blocking the pathways of PI3K/Akt (upstream), mTOR (mammalian target of rapamycin) (downstream), as well as its downstream protein products S6K and S6. It was also able to block 5-HETE, a lipoxygenase product that contributes to inflammation and activation of PI3K/Akt. The sweet gum fruit extract was prepared with 50% methanol (47:1; raw to extract) and concentrated to an organic fraction (210:1 raw to extract) referred as LIS-100 via reverse-phase column chromatography using a bioassay directed fractionation approach. The extract is a new targeted therapeutic agent for numerous disorders known to be treated by mTOR inhibitors, including cancer, diabetes, obesity, and inflammation.
    • 发现甜口香糖(枫香香a,,家amel科)水果提取物具有针对PBK(磷脂酰肌醇3-激酶)途径的多个靶点,特别是PI3K / Akt和mTOR途径的有效活性。 在1.85μg/ ml(IC 50)的非常低的浓度下,甜枪提取物显示同时阻断PI3K / Akt(上游),mTOR(雷帕霉素的哺乳动物靶标)(下游)以及其下游蛋白的途径的能力 产品S6K和S6。 它还能够阻断5-HETE,一种有助于PI3K / Akt的炎症和活化的脂氧合酶产物。 用50%甲醇(47:1,未加萃取物)制备甜口香糖果提取物,并通过反相柱色谱法使用生物测定方向分馏法浓缩成称为LIS-100的有机级分(210:1原始提取物) 方法 提取物是已知用mTOR抑制剂治疗的许多病症的新靶向治疗剂,包括癌症,糖尿病,肥胖症和炎症。
    • 6. 发明申请
    • Sweet Gum Fruit Extract as a Therapeutic Agent
    • 甜胶提取物作为治疗剂
    • US20150110862A1
    • 2015-04-23
    • US14590033
    • 2015-01-06
    • Zhijun LiuPeiying YangRobert A. Newman
    • Zhijun LiuPeiying YangRobert A. Newman
    • A61K36/185A61K45/06
    • A61K36/185A61K45/06
    • Sweet gum (Liquidambar styraciflua L., family Hamamelidaceae) fruit extract was discovered to possess potent activities against multiple targets of the PI3K (phosphatidylinositide 3-kinase) pathway, especially the PI3K/Akt and mTOR pathways. At a very low concentration of 1.85 μg/ml (IC50), sweet gun extract showed the ability of simultaneously blocking the pathways of PI3K/Akt (upstream), mTOR (mammalian target of rapamycin) (downstream), as well as its downstream protein products S6K and S6. It was also able to block 5-HETE, a lipoxygenase product that contributes to inflammation and activation of PI3K/Akt. The sweet gum fruit extract was prepared with 50% methanol (47:1; raw to extract) and concentrated to an organic fraction (210:1 raw to extract) referred as LIS-100 via reverse-phase column chromatography using a bioassay directed fractionation approach. The extract is a new targeted therapeutic agent for numerous disorders known to be treated by mTOR inhibitors, including cancer, diabetes, obesity, and inflammation.
    • 发现甜口香糖(Liquidambar styraciflua L.,家amel科)水果提取物具有针对PI3K(磷脂酰肌醇3-激酶)途径的多个靶点的有效活性,特别是PI3K / Akt和mTOR途径。 在1.85μg/ ml(IC 50)的非常低的浓度下,甜枪提取物显示同时阻断PI3K / Akt(上游),mTOR(雷帕霉素的哺乳动物靶标)(下游)以及其下游蛋白的途径的能力 产品S6K和S6。 它还能够阻断5-HETE,一种有助于PI3K / Akt的炎症和活化的脂氧合酶产物。 用50%甲醇(47:1,未加萃取物)制备甜口香糖果提取物,并通过反相柱色谱法使用生物测定方向分馏法浓缩成称为LIS-100的有机级分(210:1原始提取物) 方法 提取物是已知用mTOR抑制剂治疗的许多病症的新靶向治疗剂,包括癌症,糖尿病,肥胖症和炎症。
    • 8. 发明授权
    • Natural composition to decrease effects of a high fat diet
    • 天然成分降低高脂肪饮食的作用
    • US09072762B2
    • 2015-07-07
    • US13746630
    • 2013-01-22
    • Zhijun LiuPeiying Yang
    • Zhijun LiuPeiying Yang
    • A61K31/704A61K31/192A61K31/366
    • A61K31/704A61K31/192A61K31/366A61K2300/00
    • The combination of gallic acid, ellagic acid, and rubusoside was shown to inhibit angiogenesis by inhibition of pro-angiogenic factors. These three compounds were shown to be absorbed from the intestine making the compounds orally bioavailable. The ratio of the three compounds in the composition was a weight ratio of approximately 1:1.7:17.0 of gallic acid, ellagic acid, and rubusoside, respectively, resulting in a composition with 5% w/w gallic acid, 9% w/w ellagic acid, and 86% w/w rubusoside. This combination was also shown to reduce weight gain, fat accumulation, and serum cholesterol in mammals fed a high fat diet. It also reduced serum triglycerides and tended to reduce blood glucose in mammals on both normal and high fat diets. This three-compound composition (“GER”) can be used to treat diseases associated with angiogenesis and to decrease effects of a high fat diet.
    • 没食子酸,鞣花酸和罗红糖苷的组合显示通过抑制促血管生成因子抑制血管生成。 这三种化合物被显示为从肠中吸收,使化合物口服生物可利用。 组合物中三种化合物的比例分别为没食子酸,鞣花酸和罗红糖苷的约1:1.7:17.0的重量比,得到具有5%w / w没食子酸的组成,9%w / w 鞣花酸和86%w / w的Rubusoside。 这种组合也显示出降低饲喂高脂肪饮食的哺乳动物体重增加,脂肪积累和血清胆固醇。 它还减少血清甘油三酯,并倾向于降低哺乳动物在正常和高脂肪饮食中的血糖。 这种三重化合物(“GER”)可用于治疗与血管生成相关的疾病,并降低高脂肪饮食的作用。
    • 9. 发明申请
    • Natural Composition to Decrease Effects of a High Fat Diet
    • 天然成分降低高脂肪饮食的影响
    • US20140206634A1
    • 2014-07-24
    • US13746630
    • 2013-01-22
    • Zhijun LiuPeiying Yang
    • Zhijun LiuPeiying Yang
    • A61K31/704A61K31/366A61K31/192
    • A61K31/704A61K31/192A61K31/366A61K2300/00
    • The combination of gallic acid, ellagic acid, and rubusoside was shown to inhibit angiogenesis by inhibition of pro-angiogenic factors. These three compounds were shown to be absorbed from the intestine making the compounds orally bioavailable. The ratio of the three compounds in the composition was a weight ratio of approximately 1:1.7:17.0 of gallic acid, ellagic acid, and rubusoside, respectively, resulting in a composition with 5% w/w gallic acid, 9% w/w ellagic acid, and 86% w/w rubusoside. This combination was also shown to reduce weight gain, fat accumulation, and serum cholesterol in mammals fed a high fat diet. It also reduced serum triglycerides and tended to reduce blood glucose in mammals on both normal and high fat diets. This three-compound composition (“GER”) can be used to treat diseases associated with angiogenesis and to decrease effects of a high fat diet.
    • 没食子酸,鞣花酸和罗红糖苷的组合显示通过抑制促血管生成因子抑制血管生成。 这三种化合物被显示为从肠中吸收,使化合物口服生物可利用。 组合物中三种化合物的比例分别为没食子酸,鞣花酸和罗红糖苷的约1:1.7:17.0的重量比,得到具有5%w / w没食子酸的组成,9%w / w 鞣花酸和86%w / w的Rubusoside。 这种组合也显示出降低饲喂高脂肪饮食的哺乳动物体重增加,脂肪积累和血清胆固醇。 它还减少血清甘油三酯,并倾向于降低哺乳动物在正常和高脂肪饮食中的血糖。 这种三重化合物(“GER”)可用于治疗与血管生成相关的疾病,并降低高脂肪饮食的作用。
    • 10. 发明申请
    • Natural Composition for Anti-Angiogenesis and Anti-Obesity
    • 抗血管生成和抗肥胖的天然成分
    • US20110039796A1
    • 2011-02-17
    • US12761798
    • 2010-04-16
    • Zhijun LiuPeiying Yang
    • Zhijun LiuPeiying Yang
    • A61K31/704A61P35/00A61P3/04A61P3/00
    • A61K45/06A61K31/192A61K31/366A61K31/704Y02A50/401A61K2300/00
    • The combination of gallic acid, ellagic acid, and rubusoside was shown to inhibit angiogenesis by inhibition of pro-angiogenic factors. These three compounds were shown to be absorbed from the intestine making the compounds orally bioavailable. The ratio of the three compounds in the composition was a weight ratio of approximately 1:1.7:17.0 of gallic acid, ellagic acid, and rubusoside, respectively, resulting in a composition with 5% w/w gallic acid, 9% w/w ellagic acid, and 86% w/w rubusoside. This combination was also shown to reduce weight gain, fat accumulation, and serum cholesterol in mammals fed a high fat diet. It also reduced serum triglycerides and tended to reduce blood glucose in mammals on both normal and high fat diets. This three-compound composition (“GER”) can be used to treat diseases associated with angiogenesis and to decrease effects of a high fat diet.
    • 没食子酸,鞣花酸和罗红糖苷的组合显示通过抑制促血管生成因子抑制血管生成。 这三种化合物被显示为从肠中吸收,使化合物口服生物可利用。 组合物中三种化合物的比例分别为没食子酸,鞣花酸和罗红糖苷的约1:1.7:17.0的重量比,得到具有5%w / w没食子酸的组成,9%w / w 鞣花酸和86%w / w的Rubusoside。 这种组合也显示出降低饲喂高脂肪饮食的哺乳动物体重增加,脂肪积累和血清胆固醇。 它还减少血清甘油三酯,并倾向于降低哺乳动物在正常和高脂肪饮食中的血糖。 这种三重化合物(“GER”)可用于治疗与血管生成相关的疾病,并降低高脂肪饮食的作用。