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Growth hormone releasing factor analogs their preparation and pharmaceutical compositions containing them

机译:生长激素释放因子类似物的制备及其包含它们的药物组合物

摘要

Novel growth hormone releasing factor analogs are presented having a sequence of twenty-nine to forty-four amino acids (SEQ ID NO: 6) wherein Xaa at position 1 is His, 3-MeHis, desNH2His, Tyr, or desNH2Tyr; Xaa at position 2 is Val, Leu, Ile, Ala, D-Ala, N-Methyl-D-Ala, Gly, Nle, or Nval; Xaa at position 8 is Gln, Ser, or Thr; Xaa at position 15 is Ala or Leu; Xaa at position 27 is Met, Nle or Leu; Xaa at position 28 is Ser or Asn; Xaa at position 29 is an amino acid residue sequence (SEQ ID NO: 7) or fragments thereof where the fragment is reduced in number by one to fifteen amino acid residues from the carboxyl-terminus, where the carboxyl terminus can be the free carboxylic acid or the corresponding amide, and the pharmaceutically acceptable acid or base addition salts thereof. The novel growth hormone releasing factor analogs have enhanced potency for the release of growth hormone and enzymatic stability, improved half-life stability in aqueous solution, and can be administered to a subject having a deficiency of growth hormone or for improvement of growth performance in livestock and other warm blooded animals and in fish and other cold blooded marine animals.
机译:提出了新的生长激素释放因子类似物,其序列具有29至44个氨基酸(SEQ ID NO:6),其中位置1的Xaa是His,3-MeHis,desNH2His,Tyr或desNH2Tyr; 2位上的Xaa是Val,Leu,Ile,Ala,D-Ala,N-甲基-D-Ala,Gly,Nle或Nval;第8位的Xaa是Gln,Ser或Thr;第15位的Xaa是Ala或Leu;第27位的Xaa是Met,Nle或Leu;第28位的Xaa是Ser或Asn;第29位的Xaa是氨基酸残基序列(SEQ ID NO:7)或其片段,其中该片段的数目从羧基末端减少了1至15个氨基酸残基,其中羧基末端可以是游离羧酸或其相应的酰胺,及其药学上可接受的酸或碱加成盐。新型生长激素释放因子类似物具有增强的生长激素释放能力和酶稳定性,改善了在水溶液中的半衰期稳定性,并且可以施用于缺乏生长激素的受试者或用于改善家畜的生长性能。和其他温血动物以及鱼类和其他冷血海洋动物。

著录项

  • 公开/公告号IL101452A

    专利类型

  • 公开/公告日1996-11-14

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号IL19920101452

  • 发明设计人

    申请日1992-04-02

  • 分类号C07K14/60;A61K38/25;

  • 国家 IL

  • 入库时间 2022-08-22 03:26:50

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