Patent ID: 6117840
Filing Date: 2000-09-12
Classification: A61K,A61P,C07K

Abstract:
A peptide of formula AX--B--Asp--Z Awherein B is an .alpha.-hydrophobic amino acid residue whose side chain has a length of about 2 to about 5 methylene groups;X is a group amide-linked to the nitrogen atom of B, said group having a ring structure bonded to the carbonyl carbon of said amide-linkage by a spacer having a length of zero to about two methylene groups, said ring structure being a 5-, 6-, fused 6,6- or fused 6,5-membered ring which, optionally, contains one or more nitrogen, sulfur and oxygen atoms, the length of X, including said spacer and carbonyl carbon, being about that of 3-quinolinecarbonyl or smaller, unless: (I) said ring structure of X is substituted with a C.sub.1 -C.sub.2 alkyl or hydroxyl group, (ii) the .alpha.-amino group of the X amino acid residue is acylated with a C.sub.1 -C.sub.6 acyl group or (iii) X together with the nitrogen atom of said Leu forms a phthalimido, a 1,2,3,4-tetrahydroquinazoline-2,4-dione-3-yl or 5-phenylhydantoin-3-yl group; andZ is p1 Xaa--NCy.sup.1 where Xaa is Val, Ile, Leu or an amino acid residue having a side chain that contains one or two fused aromatic rings and NCy.sup.1 is a cyclic ring-containing group having a ring nitrogen atom that forms an amide bond with the .alpha.-carboxyl group of Xaa, and whose cyclic ring contains 5- or 6-atoms including said ring nitrogen atom, wherein the cyclic ring of NCy.sup.1 is optionally substituted with one or two substituent groups selected from the group consisting of carboxyl, C.sub.1 -C.sub.4 alkylenecarboxyl, carboxamide, C.sub.1 -C.sub.4 alkylenecarboxamide, hydroxyl, hydroxymethyl, (CH.sub.2 CH.sub.2 O).sub.n H, where n is 1, 2 or 3, and C.sub.1 -C.sub.4 alkyl.