发明名称 GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES
摘要 GLP-2 analogues are disclosed which comprise one of more substitutions as compared to h[Gly2]GLP-2 and which may have the property of an altered GLP-1 activity, and their medical use. The analogues are particularly useful for the prophylaxis treatment or ameliorating of the gastro-intestinal associated side effects of diabetes.
申请公布号 US2016355563(A1) 申请公布日期 2016.12.08
申请号 US201615238126 申请日期 2016.08.16
申请人 Zealand Pharma A/S 发明人 JUST Rasmus;BOVBJERG Kirsten Lindegaard;RIBER Ditte;RUSSELL Wayne Shaun
分类号 C07K14/605 主分类号 C07K14/605
代理机构 代理人
主权项 1. A GLP-2 analogue represented by the general Formula I:R1-His-X2-X3-Gly-X5-Phe-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16-X17-Ala-X19-X20-X21-Phe-Ile-X24-Trp-Leu-X27-X28-X29-X30-X31-X32-X33-X34-R2 (I) or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen, C1-4 alkyl (e.g. methyl), acetyl, formyl, benzoyl or trifluoroacetyl; X2 is Gly, Ala or Aib; X3 is Glu, Gln or Asp; X5 is Ser or Thr; X7 is Ser or Thr; X8 is Asp, Glu or Ser, X9 is Glu or Asp; X10 is Met, Val, Leu or Tyr; X11 is Asn, Ser or Ala; X12 is Thr, Ser or Lys; X13 is Ile, Leu, Val, Tyr, Phe or Gln; X14 is Leu or Met; X15 is Asp or Glu; X16 is Asn, Gln, Gly, Ser, Ala, Glu or Lys; X17 is Gln, Lys, Arg, His or Glu; X19 is Ala or Val; X20 is Arg, Lys or His; X21 is Asp, Glu or Leu; X24 is Asn, Ala, Glu or Lys; X27 is Ile, Leu, Val, Glu or Lys; X28 is Gln, Asn, Lys, Ser, Gly, Y1 or absent; X29 is Thr, Ala, Y1 or absent; X30 is Lys, Y1 or absent X31 is Ile, Pro, Y1 or absent; X32 is Thr, Y1 or absent; X33 is Asp, Asn, Y1 or absent; Y1 is Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser, or Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser, and R2 is NH2 or OH; wherein the GLP-2 analogue contains no more than one Y1; if any of X28 to X33 is Y1, those positions X29 to X34 downstream of that Y1 are absent; if any of X28 to X33 is absent, those positions X29 to X33 downstream of that position are also absent; and with the proviso that the GLP-2 analogue of Formula I is notHGDGSFSDEMNTILDGQAARDFINWLIQTKITD;HGDGSFSDEMNTILDNQAARDFINWLIQTKITD; orHGDGSFSDEMNTILDSQAARDFINWLIQTK.
地址 Glostrup DK