Patent ID: 6096712
Filing Date: 2000-08-01
Classification: A61K,A61P,C07C,C07K

Abstract:
A kininogenase inhibiting peptide having an in vitro Ki values of 10.sup.-3 to 10.sup.-9 M in a kininogenase inhibition assay and having the structure ##STR6## wherein: A is an .alpha.-amino acid of D- or L-configuration or an .alpha.-imino acid of D- or L-configuration;B is an .alpha.-amino add of D or L configuration selected from the group consisting of: Ada; Aha; Cha; 1-Dhn; 2-Dhn; homo-1-Dhn; Hch; Leu; 1-Nal; 2-Nal; homo-1-Nal; Nse; Phe; 4-F-Phe; pentafluoro -Phe; Ser(O.sup.n Bu); Ser(OBn); Trp; 1-Tna; and homo-1-Tna;Y is selected from --H, --NO.sub.2, and --CN;Z is selected from --CH.sub.2 --, 13 NH--, --S-- and --O--;R.sup.7 is independently selected from H and C.sub.1 to C.sub.6 alkyl;R.sup.5 and R.sup.6 are independently selected from H and C.sub.1 to C.sub.6 alkyl; andR.sup.1, R.sup.2, R.sup.3, R.sup.4, are independently selected from H, C.sup.1 to C.sub.6 alkyl, --OH, and C.sub.1 to C.sub.6 alkoxy; or either one of CR.sup.1 R.sup.2 or CR.sup.3 R.sup.4 constitutes a carbonyl group or a C.sub.3 -C.sub.6 cycloalkyl group.