Patent ID: 6184201
Filing Date: 2001-02-06
Classification: A61K,A61P,C07K,G01N

Abstract:
A GLP-2 analog, or a pharmaceutically acceptable salt thereof, which has intestinotrophic activity and which has the formula (SEQ ID NO: 1):R1-(Y1)m-X1-X2-X3-X4-Ser5-Phe6-Ser7-Asp8-(P1)-Leu14-Asp15-Asn16-Leu17-Ala18 -X19-X20-Asp21-Phe22-(P2)-Trp25-Leu26-Ile27-Gln28-Thr29-Lys30-(P3)-(Y2)n-R2 ,wherein:X1 is His or Tyr X2 is Ala or an Ala-replacement amino acid which confers on the analog or salt resistance to cleavage by human DPP-IV enzyme; X3 is Pro or HPro; X4 is Gly or Ala; P1 is Glu-X10-Asn-Thr-Ile (SEQ ID NO. 3) or Tyr-Ser- Lys-Tyr (SEQ ID NO. 4); X10 is Met or an oxidatively stable Met-replacement amino acid; X19 is Ala or Thr; X20 is Arg, Lys, His or Ala; P2 is Ile-Asn, Ile-Ala or Val-Gln; P3 is a covalent bond, or is Ile, Ile-Thr or Ile-Thr-Asp; R1 is H or an N-terminal blocking group; R2 is OH or a C-terminal blocking group; Y1 is one or two amino acids selected from the group consisting of Arg, Lys and His; Y2 is one or two amino acids selected from the group consisting of Arg, Lys and His; m and n, independently, are 0 or 1