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    • 3. 发明授权
    • Synthesis of a derivative of GRF and intermediate peptides
    • GRF和中间体肽衍生物的合成
    • US4774319A
    • 1988-09-27
    • US119279
    • 1987-11-09
    • Keiichi OnoYoshiyuki KaiYoshiaki TakebayashiAkihiko SanoKazushi Suwa
    • Keiichi OnoYoshiyuki KaiYoshiaki TakebayashiAkihiko SanoKazushi Suwa
    • A61K38/00C07K14/60C07K7/06C07K7/08C07K7/10
    • C07K14/60A61K38/00Y02P20/55Y10S930/12
    • A process for the manufacture of a polypeptide (I) having the formula: ##STR1## which comprises steps of: (a) coupling, successively and in the order of the sequence of the polypeptide (I), the four protected fragments A, B, C and D or five protected fragments A, B, C, E and F,said fragment A by the formula, Leu-Gin-Asp-Ile-Met-Ser-Arg-NH.sub.2said fragment B by the formula, Gln-Leu-Ser-Ala-Arg-Lys-Leusaid fragment C by the formula, Arg-Lys-Val-Leu-Glysaid fragment D by the formula, Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyrsaid fragment E by the formula, Ile-Phe-Thr-Asn-Ser-Tyrand said fragment F by the formula, Tyr-Ala-Asp-Ala being represented, respectively, and(b) eliminating, at the end of sequence, all the protecting groups to provide the polypeptide (I) which is active on the stimulation of the release of the growth hormone and thus is very useful as medicine for treatment of growth hormone deficiency disease and the like.
    • 一种制备具有下式的多肽(I)的方法:其包括以下步骤:(a)依次和按照多肽(I ),四个保护的片段A,B,C和D或五个保护的片段A,B,C,E和F,所述片段A通过式Leu-Gin-Asp-Ile-Met-Ser-Arg-NH2表示 片段B由式Gln-Leu-Ser-Ala-Arg-Lys-Leu表示,由式Arg-Lys-Val-Leu-Gly表示的片段C表示下式的Tyr-Ala-Asp-Ala- Ile-Phe-Thr-Asn-Ser-Tyr分别表示分子式为Ile-Phe-Thr-Asn-Ser-Tyr的片段E和由式Tyr-Ala-Asp-Ala表示的所述片段F,以及 (b)在序列结束时,除去所有保护基以提供在刺激生长激素释放方面具有活性的多肽(I),因此作为治疗生长激素缺乏症的药物非常有用, 类似。
    • 5. 发明授权
    • Sustained-release drug formulations
    • 持续释放药物制剂
    • US07601363B2
    • 2009-10-13
    • US11688082
    • 2007-03-19
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • A61K9/14A61F2/00A61F13/00
    • A61K9/0024A61K47/02
    • The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
    • 本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。 制剂包含组合(a),(b)和(c)中的一种,以及包含疏水性聚合物的载体,其中所述颗粒组合分散在载体中:(a)包含活性成分的颗粒, 碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳(物质如酸)的物质的颗粒; (b)包含活性成分和碳酸酯的颗粒,以及包含物质如酸的颗粒; 和(c)包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。
    • 6. 发明授权
    • Sustained-release drug formulations for implantation
    • 用于植入的持续释放药物制剂
    • US07247312B1
    • 2007-07-24
    • US10089694
    • 2000-10-31
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • A61F13/00A61F2/00A61K9/14
    • A61K9/0024A61K47/02
    • The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
    • 本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。 制剂包含组合(a),(b)和(c)中的一种,以及包含疏水性聚合物的载体,其中所述颗粒组合分散在载体中:(a)包含活性成分的颗粒, 碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳(物质如酸)的物质的颗粒; (b)包含活性成分和碳酸酯的颗粒,以及包含物质如酸的颗粒; 和(c)包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。
    • 7. 发明申请
    • SUSTAINED-RELEASE DRUG FORMULATIONS
    • 持续释放药物制剂
    • US20070166377A1
    • 2007-07-19
    • US11688082
    • 2007-03-19
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • Akihiko SanoMasako KajiharaHiroo Maeda
    • A61K39/00A61K9/46
    • A61K9/0024A61K47/02
    • The present invention relates to a formulation for implantation having a novel constitution, which accomplishes controlled releases of active ingredients. The formulation comprises one of combinations (a), (b) and (c), as well as a carrier comprising a hydrophobic polymer, wherein the particle combination is dispersed into the carrier: (a) particles comprising an active ingredient, particles comprising a carbonate, and particles comprising a substance which is reacted with the carbonate in an aqueous solution to generate carbon dioxide (substance such as an acid); (b) particles comprising an active ingredient and a carbonate, and particles comprising a substance such as an acid; and (c) particles comprising a carbonate, and particles comprising an active ingredient and a substance such as an acid.
    • 本发明涉及具有实现活性成分控制释放的新颖结构的植入制剂。 制剂包含组合(a),(b)和(c)中的一种,以及包含疏水性聚合物的载体,其中所述颗粒组合分散在载体中:(a)包含活性成分的颗粒, 碳酸盐和包含与碳酸盐在水溶液中反应产生二氧化碳(物质如酸)的物质的颗粒; (b)包含活性成分和碳酸酯的颗粒,以及包含物质如酸的颗粒; 和(c)包含碳酸盐的颗粒和包含活性成分和物质如酸的颗粒。