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    • 6. 发明申请
    • PROCESS FOR PRODUCING URINARY TRYPSIN INHIBITOR AND DOMAINS THEREOF, NOVEL POLYPEPTIDE RELATED TO THE BOTH, AND PROCESS FOR PRODUCING THE POLYPEPTIDE
    • 用于生产尿素抑制剂及其领域的方法,与两相关的新型多肽,以及生产多肽的方法
    • WO1996003503A1
    • 1996-02-08
    • PCT/JP1995001449
    • 1995-07-21
    • THE GREEN CROSS CORPORATIONIDENO, ShojiGOTO, TakashiHORII, Hajime
    • THE GREEN CROSS CORPORATION
    • C12N15/12
    • C07K14/8103A61K38/00
    • A process for producing a urinary human trypsin inhibitor (UTI) and domains thereof by using a yeast of the genus Pichia as the host cell; an expression system related thereto; a novel polypeptide at least having the amino acid sequence represented by formula (I) in the specification; a DNA coding for the same; an expression vector containing the DNA; a transformant containing the vector; and a process for producing the polypeptide. The above UTI, expression system of each domain thereof, and process for producing the UTI and domains thereof enable UTI and domains thereof to be mass-produced readily and efficiently. The use of the expression system facilitates the preparation of variants or derivatives of UTI and so forth and contributes to the development of novel medicines such as a protease inhibitor. The invention also provides a novel useful polypeptide which is more excellent in elastase inhibitory activity than natural UTI and can be mass-produced.
    • 通过使用毕赤酵母属的酵母作为宿主细胞来制备尿胰蛋白酶抑制剂(UTI)及其结构域的方法; 与此有关的表达制度; 至少具有说明书中由式(I)表示的氨基酸序列的新型多肽; 编码相同的DNA; 含有DNA的表达载体; 含有载体的转化体 以及产生该多肽的方法。 上述UTI,其每个结构域的表达系统,以及UTI及其结构域的制备方法使得UTI及其结构域容易且有效地批量生产。 表达系统的使用促进了UTI等变体或衍生物的制备,并有助于新型药物如蛋白酶抑制剂的开发。 本发明还提供了一种与天然UTI相比弹性蛋白酶抑制活性更优异的新型有用多肽,可以批量生产。
    • 7. 发明申请
    • SUCCINAMIC ACID COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
    • 磺胺酸化合物,其生产方法及其用途
    • WO1995007898A1
    • 1995-03-23
    • PCT/JP1994001266
    • 1994-08-01
    • SENJU PHARMACEUTICAL CO., LTD.THE GREEN CROSS CORPORATIONHOSONO, HiroshiNISHIO, ToshiyukiISHIKAWA, HiromichiNAKAMURA, YoshiyukiMATSUI, Tetsuo
    • SENJU PHARMACEUTICAL CO., LTD.THE GREEN CROSS CORPORATION
    • C07D277/64
    • C07D277/64
    • A novel succinamic acid compound represented by general formula (1) or a pharmaceutically acceptable salt thereof; a preventive and/or a remedy for complications of diabetes containing the compound or the salt as the active ingredient; an aldose reductase inhibitor containing the compound or the salt as the active ingredient; and a process for producing the compound or the salt. In said formula, R represents alkyl or lower alkenyl, and R represents carboxyl which may be esterified. The invention compound (1) and the salt have a potent aldose reductase inhibitor activity on mammals including humans and an excellent safety, and hence are useful as a remedy for therapeutic treatment of complications of diabetes, such as failure of corneal lesion union, cataract, neurosis, retinopathy and nephropathy, especially cataract and neurosis. The invention process can provide the invention compounds having such a usefulness efficiently.
    • 一种由通式(1)表示的新型琥珀酰胺酸化合物或其药学上可接受的盐; 包含化合物或盐作为活性成分的糖尿病并发症的预防和/或补救措施; 含有该化合物或该盐作为有效成分的醛糖还原酶抑制剂; 以及该化合物或其盐的制造方法。 在所述式中,R 1表示烷基或低级烯基,R 2表示可被酯化的羧基。 本发明化合物(1)和盐具有对包括人类在内的哺乳动物有效的醛糖还原酶抑制剂活性,并且具有优异的安全性,因此可用作治疗糖尿病并发症的治疗方法,例如角膜损伤联合失败,白内障, 神经症,视网膜病变和肾病,特别是白内障和神经症。 本发明方法可以有效地提供具有这种有效性的本发明化合物。