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    • 58. 发明申请
    • HISTIDINE SUBSTITUTED GROWTH HORMONE RELEASING FACTOR ANALOGS
    • HISTIDIN取代生长激素释放因子模拟
    • WO1992000095A1
    • 1992-01-09
    • PCT/US1991004606
    • 1991-06-27
    • HOFFMANN-LA ROCHE INC.
    • HOFFMANN-LA ROCHE INC.FELIX, Arthur, MartinHEIMER, Edgar, Philip
    • A61K37/36
    • C07K14/60A61K38/00
    • Novel growth hormone releasing factor analogs are presented having formula (I), wherein R1 is His, 3-MeHis, desNH2His, Tyr, or desNH2Tyr; R2 is Val, Leu, or Ile; R3 is Ala; R4 is Met, Leu, Ile, or Nle; R5 is Ser or Asn; R6 is an amino acid residue sequence selected from Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu or fragments thereof where the fragment is reduced in number by one to fifteen amino acid residues from the amino acid residue which carries the substituent X; and X is either OH or NH2, and the pharmaceutically acceptable acid or base addition salts thereof. The novel growth hormone releasing factor analogs demonstrate enhanced potency for the released growth hormone, have enhanced enzymatic stability, and can be administered to a subject having a deficiency of growth hormone or for improvement of growth performance in livestock.
    • 呈现新型生长激素释放因子类似物具有式(I),其中R 1是His,3-MeHis,desNH 2 His,Tyr或desNH 2 Tyr; R2是Val,Leu或Ile; R3是Ala; R4是Met,Leu,Ile或Nle; R5是Ser或Asn; R6是选自Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu或其片段数目减少的片段的氨基酸残基序列 来自携带取代基X的氨基酸残基的1至15个氨基酸残基; 并且X是OH或NH 2,以及其药学上可接受的酸或碱加成盐。 新生长激素释放因子类似物表现出增强的释放的生长激素的效力,具有增强的酶稳定性,并且可以施用于具有生长激素缺乏或用于改善家畜生长性能的受试者。