发明名称 SOMATOSTATIN RECEPTOR ANTAGONISTS
摘要 organic chemistry, biochemistry, peptide hormones. SUBSTANCE: invention describes novel compounds of the general formula (I): (R1, R2)A1-A2-A3-A4-Lys-A6-A7-A8-R3 where A1 means D- or L-isomer of aromatic amino acid; A2 means D-isomer taken among the group including Cys, Pen, aromatic amino acid or aliphatic amino acid; A3 means aromatic amino acid; A4 means D-Trp; A6 means Thr, Thr(Bzl), Gly, Ser or aliphatic amino acid; A7 means Cys, Pen or aromatic or aliphatic amino acid; A8 means D- or L-isomer taken among the group including Thr, Ser, aromatic amino acid or aliphatic amino acid; each of R1 and R2 means independently H or E, SO2 or E, CO where E1 means heterocycle, lower alkyl substituted by heterocycle with hydroxy-lower alkyl; R3 means NH2 under condition that if A2 is D-Cys or D-Pen and A7 is Cys or Pen then side chains A2 and A7 are bound by disulfide bond; and if A1 is p-HO2-Phe, A2 means D-Cys, A3 means Phe or Tyr, A6 means Thr or Val and A7 means Cys then A8 means beta-Nal. new compounds are antagonists of somatostatin receptors and can be used for treatment of patients with diseases and disorders when activation of growth hormone or insulin secretion is necessary, for example, in methods of radiotreatment. EFFECT: new compounds indicated above, valuable medicinal properties. 19 cl, 1 tbl
申请公布号 RU2179172(C2) 申请公布日期 2002.02.10
申请号 RU19990114018 申请日期 1997.12.04
申请人 NTIFIK S.A. (S.K.R.A.S.);DZE ADMINISTREJTORS OF DZE T'JULEJN EHD'JUKEJSHNL;UNIV TULANE;FAND 发明人 MORGAN BEHRRI;MERFI VILL'JAM;KOJ DEHVID KH.
分类号 A61K38/18;A61P5/02;C07K7/06;C07K14/655;(IPC1-7):C07K7/06 主分类号 A61K38/18
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