发明名称 ANTAGONISTIC ANALOGUES OF GROWTH HORMONE RELEASING-HORMONE (GH-RH) INHIBITING INSULIN-LIKE GROWTH FACTORS (IGF-I AND -II)
摘要 FIELD: medicine, oncology, chemistry of peptides. ^ SUBSTANCE: invention relates to peptide taken among the group of the formula: X-R1-R2-Asp-Ala-R-Thr-R8-R-R10-Arg-R12-R13-R14-R15-R16-Leu-R18-R19-Arg-R21-R22-Leu-Gln-Asp-Ile-R27-R28-R29-NH2 wherein X means PhAc, IndAc or Nac; R1 means Tyr or His; R2 means D-Arg; R5 means Ile or Val; R6 means Phe or Phe(Cl); R8 means Asn, Gln, Ala or D-Asn; R9 means Arg, Har, Lys, Orn, D-Arg, D-Har, D-Lys, D-Orn, Cit, Nle, Tyr(Me), Ser, Ala or Aib; R10 means Tyr or Tyr(Me); R12 means Lys; R13 means Val or Nle; R14 means Leu or Nle; R15 means Gly, Ala, Abu, Nle or Gln; R16 means Gln or Arg; R18 means Ser or Nle; R19 means Ala; R21 means Lys; R22 means Leu, Ala or Aib; R27 means Met, Leu, Nle, Abu or D-Arg; R28 means Arg, D-Arg or Ser; R29 means Arg, D-Arg, Har or D-Har under condition that if R9 and R28 mean Ser then R29 is not Arg or Har, and its pharmaceutically acceptable salts. Compounds are antagonists of the growth hormone releasing hormone and elicit the enhanced affinity for receptor. Invention describes also a method for suppression of excessive levels of the growth hormone in a patient, method for treatment of malignant tumor and method for inhibition of levels of IGF-II in tumors. ^ EFFECT: valuable medicinal properties of analogues. ^ 11 cl, 9 tbl, 5 dwg, 4 ex
申请公布号 RU2235099(C2) 申请公布日期 2004.08.27
申请号 RU20010117218 申请日期 1999.11.23
申请人 发明人 SHEHLLI EHNDRJU V.;VARGA DZHOZEF;ZARANDI MARTA
分类号 A61K38/00;A61K38/27;A61P5/08;A61P35/00;C07K14/60 主分类号 A61K38/00
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