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    • 2. 发明专利
    • Gynosaponins and their preparations
    • 青蒿素及其制剂
    • JPS5758699A
    • 1982-04-08
    • JP13468480
    • 1980-09-27
    • Nippon Shoji KkTsunematsu Takemoto
    • TAKEMOTO TSUNEMATSUARIHARA SHIGENOBUNAKASHIMA TADASHIOKUDAIRA MEGUMI
    • C07J17/00A61K31/575A61K31/70A61K36/42A61P3/06C07J9/00
    • NEW MATERIAL:A gynosaponin shown by the formula[when R
      3 is H, R
      1 is β-D- xylopyranosyl(1→2)-β-D-glucopyranosyl and R
      2 is β-D-xylopyranosyl(1→6)-β-D-glucopyranosyl, etc.; when R
      3 is OH, R
      1 is β-D-glucopyranosyl(1→2)-β-D-glycopyranosyl and R
      2 is α-L-rhamnopyranosyl(1→6)-β-D-glucopyranosyl, etc.].
      EXAMPLE: 20S, 26-Hydroxyprotopanaxadiol-3-0-[β-D-glucopyranosyl(1→2)-β-D- glucopyranoside]20-0-[α-L-rhamnopyranosy(1→6)-β-D-glucopyranoside]: gynosaponin P.
      USE: A lipometabolism agent.
      PROCESS: Gynostemma pentaphyllum Makino is extracted with water or water- containing alcohol, the extracted solution is treated with a nonionic adsorbing resin, eluted with a lower alcohol, absorbed on alumina, and eluted with a lower alcohol to give the titled compounds.
      COPYRIGHT: (C)1982,JPO&Japio
    • 新材料:由式[当R 3是H时,R 1是β-D-吡喃木糖基(12)-β-D-吡喃葡萄糖基并且R 2是β-D-吡喃木糖基( 1 6)-β-D-吡喃葡萄糖基等; 当R 3为OH时,R 1为β-D-吡喃葡萄糖基(12)-β-D-吡喃葡萄糖基,R 2为α-L-鼠李糖吡喃糖基(16)-β-D-吡喃葡萄糖基, 等等。]。 实施例:20S,26-羟基新戊二醇-3-0- [β-D-吡喃葡萄糖基(12)-β-D-吡喃葡萄糖苷] 20-0- [α-L-鼠李糖吡喃糖(16)-β-D-吡喃葡萄糖苷] :gynosaponin P.使用:脂代谢剂。 方法:用水或含水醇提取绞股蓝绞肉提取液,用非离子吸附树脂处理提取液,用低级醇洗脱,吸附在氧化铝上,用低级醇洗脱,得到标题化合物。
    • 3. 发明专利
    • Pfaffic acid and derivative thereof
    • 食用酸及其衍生物
    • JPS5910548A
    • 1984-01-20
    • JP11887282
    • 1982-07-07
    • Toshio OdajimaRooto Seiyaku KkTsunematsu Takemoto
    • TAKEMOTO TSUNEMATSUODAJIMA TOSHIOHAYASHI SHINICHINISHIMOTO KIJIYUUNAKAI SHIROUTAKAGI NORIKO
    • C07C69/013A61K31/19A61K31/215A61P35/00C07C51/00C07C51/42C07C62/32C07C67/00C07C69/757
    • NEW MATERIAL:Pfaffic acid and its derivative of the formula (R
      1 is H or acyl; R
      2 is H or alkyl).
      USE: An antitumor agent, capable of exhibiting improved inhibitory activity against melanoma cells, cervical cancer cells, cancer cells of the lung, etc. in a concentration as low as 4W6μg/ml, and administered in 10mgW1g, preferably about 100mg daily dose in the form of a powder, granule, capsule, solution, etc.
      PROCESS: The root of a dried Pfaffia paniculate Kuntze is pulverized and extracted with an alcohol, and sulfuric acid is then added to the resultant extract solution and refluxed under heating to distill away the solvent. The residue obtained by the distillation is then passed through a column packed with silica gel, and eluted with a mixture of chloroform with methanol at (50:1)W(20:1) ratio. The solvent is then distilled from the eluted fraction to recrystallize the residue from the alcohol and give the aimed pfaffic acid of the formula. The pfaffic acid of the formula is a crystalline substance having specific ≤29C skeleton, and stable to acids and alkalis with 285W286°C melting point.
      COPYRIGHT: (C)1984,JPO&Japio
    • 新物质:Pfaffic酸及其衍生物(R1为H或酰基; R2为H或烷基)。 用途:能够以低至4-6mug / ml的浓度显示出对黑素瘤细胞,宫颈癌细胞,肺癌细胞等的改善的抑制活性的抗肿瘤剂,并以10mg-1g,优选约100mg 粉末,颗粒,胶囊,溶液等形式的日剂量。方法:将干燥的Pfaffia paniculate Kuntze的根粉碎并用醇萃取,然后将硫酸加到得到的提取液中,加热回流 蒸馏除去溶剂。 然后将通过蒸馏得到的残余物通过填充有硅胶的柱,并用氯仿与甲醇(50:1) - (20:1)比例的混合物洗脱。 然后从洗脱的级分中蒸馏出溶剂,使来自醇的残余物重结晶,得到下式的目标化合物。 该配方酸是具有特定<= 29C骨架的结晶物质,对酸和碱稳定,具有285-286摄氏度的熔点。
    • 4. 发明专利
    • Remedy for tragomaschalia
    • 补救措施
    • JPS6176412A
    • 1986-04-18
    • JP19902984
    • 1984-09-21
    • Rooto Seiyaku KkTsunematsu Takemoto
    • TAKEMOTO TSUNEMATSUHAYASHI SHINICHINISHIMOTO KIJU
    • A61K8/00A61K8/11A61K8/97A61Q15/00
    • PURPOSE: To remedy for tragomaschalia that contains, as an active ingredient, an essence of AMACHAZURU (Gynostemma pentaphyllum Makino), thus showing treating effect by oral administration with low toxicity.
      CONSTITUTION: The objective remedy is obtained by using, as an active ingredient, an essence of AMACHAZURU. The essence is obtained by extracting the whole plant with hot water or by drying the plant and crushing it into a powder. when the essence is orally given by 0.05W5g/day, preferably 0.1W2g/day for 6 months, the effect is developed. Since the toxicity of the essence is very low, it can be given for a long period of time.
      COPYRIGHT: (C)1986,JPO&Japio
    • 目的:治疗含有AMACHAZURU(绞股蓝绞股蓝)的精华作为活性成分的疟原虫,因此通过口服低毒处理效果显着。 构成:通过使用AMACHAZURU的精华作为活性成分,获得客观的补救。 通过用热水提取整个植物或通过干燥植物并将其粉碎成粉末获得本质。 当精华以0.05-5g /天,优选0.1-2g /天口服给药6个月时,发挥作用。 由于本质的毒性非常低,可以长时间给予。
    • 8. 发明专利
    • Anticancer agent composition containing dammarane based compound
    • 含有DAMMARANE的化合物的反应剂组合物
    • JPS59181217A
    • 1984-10-15
    • JP5467883
    • 1983-03-30
    • Toshio OdajimaRooto Seiyaku KkTsunematsu Takemoto
    • TAKEMOTO TSUNEMATSUARIHARA SHIGENOBUODAJIMA TOSHIOHAYASHI SHINICHINISHIMOTO KIJIYUUTAKAGI NORIKOWATANABE YOSHIE
    • C07J17/00A61K31/58A61K31/704A61P35/00
    • PURPOSE: A low toxic anticancer agent composition, containing one or more specific dammarane based compounds, including novel compounds, and capable of inhibiting tumorous cells in a very small amount without damaging cells in the inhibitory concentration thereof.
      CONSTITUTION: An anticancer agent composition containing one or more of compound expressed by formula I (glu is β-D-glucopyranosyl), formula II, III or IV. The compounds expressed by formulas I WIV are found to have powerful antitumor activity in prosapogenin and sapogenin obtained by hydrolyzing dammarane based sepogenin contained in Hydrangeae serrata Seringe var. thunbergii Sugimoto. The compounds expressed by formulas I WIV are capable of inhibiting remarkably the multiplication of uterine neck cancer calls or melanoma cells, etc. in an amount of ≤10μg/ml concentration and scarcely damaging the cell in the concentration. The agent is applicable to cancers in the skin, liver and stomach, etc. The compound of formula III is a novel compound and designated as Mh-2.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:一种低毒性抗癌剂组合物,其含有一种或多种特异性抗坏血酸基化合物,包括新型化合物,并且能够以非常少的量抑制肿瘤细胞,而不会以抑制浓度破坏细胞。 构成:含有一种或多种由式I表示的化合物(glu是β-D-吡喃葡萄糖基),式II,III或IV的抗癌剂组合物。 发现由式I -IV表达的化合物在通过水解包含在绣球花serrata Seringe var中的基于dammarane的sepogenin获得的促生长素和皂甙元中具有强大的抗肿瘤活性。 杉木杉杉本 由式I -IV表达的化合物能够显着地抑制子宫颈癌调用或黑素瘤细胞等的增殖,其量为<= 10mug / ml浓度,并且几乎不破坏浓度的细胞。 该药剂适用于皮肤,肝,胃等癌症。式Ⅲ化合物为新化合物,称为Mh-2。