Patent ID: 6034056
Filing Date: 2000-03-07
Classification: A61K,A61P,C07K

Abstract:
A cyclic peptide of formula 1 ##STR174## wherein AA1 is an L or D amino acid selected from the group consisting of Ile, Leu, Pro, Gly, Tic, Val, tert-Leu, tert-butyl-Ala, Phe, Nle, Met, Arg, Lys and Ala;AA2 is an L amino acid selected from Leu, Ile, Phe, Val, tert-Leu, Nle, Cha and tert-butyl-Ala;AA3 is an L amino acid selected from Asp or Glu;AA4 is an L amino acid selected from Val, Leu, Ile, Phe, Cha, Nle and Nva;wherein each amino acid of AA1, AA2, AA3 and AA4 is optionally independently alkylated with a C.sub.1-4 alkyl group;LINKER represents a linking moiety for linking N terminus of AA1 to C terminus of AA4 to form a cyclic peptide containing a heterocyclic ring having 17 to 30 members;the cyclic peptide having an IC.sub.50 of <20 .mu.M in the MOLT-4 cell/fibronectin assay described herein and/or;the cyclic peptide having an IC.sub.50 of <100 .mu.M in the MOLT-4 cell/recombinant soluble VCAM-1 assay described herein and;AA1-4 have the general formula 2 ##STR175## wherein R1 is the amino acid side chain and R2 and R3, which may be the same or different for each AA1-AA4, independently represent H or C.sub.1-4 alkyl;or a salt thereof.