发明名称 GIP-GLP-1 DUAL AGONIST COMPOUNDS AND METHODS
摘要 The present invention relates to truncated GIP analogues which comprise one or more substitutions as compared to wild-type GIP and which may have the property of an altered, preferably increased GLP-1 activity, e.g. as assessed in in vitro efficacy assays. The invention provides GIP-GLP-1 dual agonist compounds and associated methods.
申请公布号 US2015299281(A1) 申请公布日期 2015.10.22
申请号 US201314398260 申请日期 2013.05.03
申请人 Zealand Pharma A/S/ 发明人 JUST Rasmus;RIBER Ditte;SHELTON Anne Pernille Tofteng;ØSTERLUND Torben;HANSEN Kate;JESSEN Lene
分类号 C07K14/575 主分类号 C07K14/575
代理机构 代理人
主权项 1. A GIP analogue represented by the general Formula I′:(SEQ 10 NO: 61)R1-Tyr-X2-X3-Gly-Thr-Phe-X7-Ser-X9-X10-X11-X12- X13-X14-X15-X16-Lys-Ala-X19-X20-X21-X22-X23-X24- Trp-Leu-X27-X28-X29-X30-X31-X32-X33-X34-X35- X36-X37-X38-X39-X40-X41-X42-R2 or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is Hy-, Ac or pGlu; X2 is Ala, Aib or Gly; X3 is Glu or Asp; X7 is Thr, Ser, or Ile; X9 is Asp or Glu; X10 is Tyr, Leu or Ser; X11 is Ser or Leu; X12 is Ile or Lys; X13 is Ala, Tyr or Aib; X14 is Met, Leu or Ser; X15 is Asp or Glu; X16 is Lys, Gly, Ser or Glu; X19 is Gln, Ala, Glu or Lys; X20 is Gln, Lys, Arg or His; X21 is Asp, Ala or Glu; X22 is Phe or 1 Nal; X23 is Val, Ile or Leu; X24 is Asn, Glu, Arg or Lys; X27 is Leu, Val, Ile, Lys, Glu or Ser; X28 is Ala, Ser, Arg or Aib; X29 is Gln, Aib, Lys, Gly or Ala; X30 is Lys, Gly, Pro or absent; X31 is Gly, Pro, Ser, Glu or absent; X32 is Lys, Ser or absent; X33 is Lys, Ser, Glu or absent; X34 is Asn, Gly, Ala, Lys or absent; X35 is Asp, Ala, Pro, Glu or absent; X36 is Trp, Pro, Lys or absent; X37 is Lys, Pro, Glu or absent; X38 is His, Pro, Ser, Lys or absent; X39 is Asn, Ser or absent; X40 is Ile or absent; X41 is Thr or absent; X42 is Gin or absent; and R2 is —NH2 or —OH.
地址 Glostrup DK