Back to results
US 5,508,385 AGranted
Tripeptide derivatives containing pyroglutamic acid residue
AssigneeNitto Boseki Co., Ltd.
InventorsYoshihito Abe, Takeshi Nagasawa, Katsumasa Kuroiwa, Katsuhiro Yaginuma
Life of this patent
Estimating the term…
Abstract
Novel tripeptide derivatives having a pyroglutamic acid residue strongly inhibit a plurality of trypsin-like serine proteases such as plasmin, thrombin, trypsin, kallikrein, factor Xa and urokinase. The compounds of the present invention can inhibit various trypsin-like serine proteases and are expected to show remarkable effects as novel protease inhibitors for the treatment of pancreatitis, inflammantion, ulcer, etc.
Claims2
A tripeptide derivative represented by the formula:
- X--A.sub.1 --A.sub.2 --A.sub.3 --H
- wherein X is bound to the secondary amino group of A.sub.1 and is selected from the group consisting of a hydrogen atom, an arenesulfonyl group, an alkanesulfonyl group, an aroyl group, an acyl group, and an alkyloxycarbonyl group;
- A.sub.1 is L- or D-pyroglutamic acid;
- A.sub.2 is selected from the group consisting of glycine, L-alanine, L-valine, L-isoleucine, L-serine, L-threonine, L-lysine, L-proline, L-pipecolinic acid and L-phenylalanine;
- and A.sub.3 is an L-, D- or DL-arginal residue or a pharmaceutically acceptable acid addition salt thereof.
2 more elements
Dependencies are inferred from the claim text.