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    • 3. 发明申请
    • Extract from plant of japanese parsley family and process for producing the same
    • 从日本欧芹系列植物提取物及其生产方法
    • US20070092587A1
    • 2007-04-26
    • US10561431
    • 2004-06-18
    • Hiromu OhnogiKatsumi SugiyamaNobuko MurakiTatsuji EnokiHiroaki SagawaIkunoshin Kato
    • Hiromu OhnogiKatsumi SugiyamaNobuko MurakiTatsuji EnokiHiroaki SagawaIkunoshin Kato
    • A61K36/232
    • A61K36/232A23L2/02A23V2002/00A23V2250/21A23V2200/328
    • The present invention provides an extract obtainable by extracting a plant belonging to Umbelliferae, or a processed product thereof, with a water-containing alcohol; a process for preparing the extract; a therapeutic agent or prophylactic agent for a disease accompanying an abnormality in an amount of insulin or insulin response and/or diabetic complications, characterized in that the therapeutic agent or prophylactic agent comprises as an effective ingredient the extract as defined above; an agent for an insulin-mimetic action, characterized in that the agent comprises as an effective ingredient the extract as defined above; a food, beverage or feed, comprising the extract as defined above; an agent for enhancing glucose uptake into a cell, characterized in that the agent comprises as an effective ingredient the extract as defined above; to an agent for inducing differentiation into an adipocyte, characterized in that the agent comprises as an effective ingredient the extract as defined above; and an inhibitory agent for aldose reductase, characterized in that the agent comprises as an effective ingredient the extract as define above.
    • 本发明提供通过用含水醇提取属于伞形赤霉属的植物或其加工产物而获得的提取物; 一种制备提取物的方法; 用于伴随胰岛素或胰岛素反应量和/或糖尿病并发症的异常的疾病的治疗剂或预防剂,其特征在于所述治疗剂或预防剂包含作为有效成分的上述提取物; 用于胰岛素模拟作用的药剂,其特征在于所述药剂包含如上所定义的提取物作为有效成分; 包含上述提取物的食品,饮料或饲料; 用于增强葡萄糖摄入细胞的药剂,其特征在于所述药剂包含如上所定义的提取物作为有效成分; 涉及诱导分化为脂肪细胞的药剂,其特征在于所述药剂包含如上所定义的提取物作为有效成分; 以及醛糖还原酶抑制剂,其特征在于,所述药剂含有作为有效成分的上述定义的提取物。
    • 9. 发明授权
    • Method for reductive elimination of protecting groups
    • 还原消除保护基团的方法
    • US4564471A
    • 1986-01-14
    • US188107
    • 1980-09-17
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • C07B31/00C07B51/00C07C67/00C07C227/00C07C227/16C07C227/18C07C227/20C07C231/00C07K1/06C07K1/12C07K5/075C07C101/02
    • C07K1/12C07K5/0613Y02P20/55
    • The invention provides a novel and efficient method for the elimination of protecting groups, e.g. benzyloxycarbonyl group, from a protected amino acid, peptide or derivative thereof having at least one functional group protected by a protecting group, e.g. a lower alkyl ester of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine by catalytic hydrogen reduction to produce free amino acid, peptide or derivative thereof. In contrast to the conventional procedures in which the reaction is carried out in a solvent dissolving both the starting compound and the product compound or a solvent dissolving the starting compound but not dissolving the product compound, the inventive method utilizes a binary two-phase reaction medium composed of water and an organic solvent not freely miscible with water such as toluene. The reaction takes place in the organic phase containing the starting compound dissolved and the catalyst dispersed therein whereas the reaction product which is water-soluble is smoothly and successively transferred into the aqueous phase so that advantages are obtained in the unexpectedly high yield of the product as well as in the easiness of handling the reaction mixture after completion of the reaction.
    • 本发明提供了一种用于消除保护基团的新型和有效的方法,例如, 苄氧羰基,被保护的氨基酸,具有至少一个被保护基保护的官能团的肽或衍生物。 N-苄氧羰基-α-L-天冬氨酰基-L-苯丙氨酸的低级烷基酯通过催化氢还原反应产生游离氨基酸,肽或其衍生物。 与在溶解起始化合物和产物化合物的溶剂或溶解起始化合物但不溶解产物化合物的溶剂中进行反应的常规方法相反,本发明的方法利用二元二相反应介质 由水和不能与水如甲苯自由混溶的有机溶剂组成。 反应发生在含有溶解的起始化合物和分散在其中的催化剂的有机相中,而水溶性的反应产物顺利地依次转移到水相中,从而获得了产品出乎意料的高产率的优点, 以及在反应完成后容易处理反应混合物。
    • 10. 发明授权
    • Method of producing .alpha.-L-aspartyl-L-phenylalanine methyl ester
hydrochloride
    • 生产α-L-天冬氨酰-L-苯丙氨酸甲酯盐酸盐的方法
    • US5225587A
    • 1993-07-06
    • US864133
    • 1992-04-06
    • Katsumi SugiyamaKiyo AdachiToshihide Yukawa
    • Katsumi SugiyamaKiyo AdachiToshihide Yukawa
    • C07K5/072C07K5/075
    • C07K5/0613
    • A method of purifying .alpha.-L-aspartyl-L-phenylalanine methyl ester as a hydrochloride salt thereof which comprises:i) contacting a mixture of .alpha.-L-aspartyl-L-phenylanaline methyl ester and .beta.-L-aspartyl-L-phenylalanine methyl ester with an aqueous medium containing (a) hydrogen chloride in an amount not more than ca. 2 mol., per liter of said aqueous medium, but not less than 1 mol., per mole of said of said mixture of .alpha.-L-aspartyl-L-phenylalanine methyl ester and .beta.-L-aspartyl-L-phenylalanine methyl ester, and (b) an inorganic chloride selected from the group consisting of NaCl, KCl, NH.sub.4 Cl, CaCl.sub.2, and ZnCl.sub.2 in an amount of at least ca. 50 g., per liter of said aqueous medium, to form crystals of .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride, andii) recovering the .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride crystals therefrom.
    • 纯化α-L-天冬氨酰基-L-苯丙氨酸甲酯盐酸盐的方法,其包括:i)使α-L-天冬氨酰基-L-苯亚胺甲酯与β-L-天冬氨酰基-L-苯丙氨酸的混合物 甲酯与含有(a)氯化氢的含水介质的量不大于约 每摩尔所述所述α-L-天冬氨酰基-L-苯丙氨酸甲酯和β-L-天冬氨酰-L-苯丙氨酸甲酯的混合物每升所述水性介质2摩尔,但不小于1摩尔 ,和(b)选自NaCl,KCl,NH 4 Cl,CaCl 2和ZnCl 2的无机氯化物,其量至少约为。 50升,每升所述水性介质中,形成α-L-天冬氨酰基-L-苯丙氨酸甲酯盐酸盐的晶体,和ii)从其中回收α-L-天冬氨酰基-L-苯丙氨酸甲酯盐酸盐晶体。