Inhibitors of trypsin-like enzymes
AssigneeTrigen Limited
InventorsGoran Claeson, Manfred Hans Wilhelm Philipp, Rainer Metternich
Life of this patent
Estimating the term…
Abstract
Pharmaceutical compositions comprising compounds of the formula: ##STR1## in which X.dbd.H or is an N-protecting group; Y is 1-10 .alpha.-amino acids; Q1 and Q2 taken together represent the residue or a diol; R is C.sub.1-4 alkyl; and the asymmetric carbon atom marked * may have the D- or L-configuration, are useful in therapeutic methods of inhibiting thrombin.
Claims12
A method of inhibiting thrombin in the treatment of disease comprising administering to a mammal a therapeutically effective amount of a compound of the formula:
- ##STR19## in which X.dbd.H or is an N-protecting group;
- Y is a sequence of 2-10 .alpha.-amino acids, wherein D-Phe-Pro is attached to --NH;
- Q1 and Q2 taken together represent the residue of a diol;
- R is C.sub.1-4 alkyl;
- and the asymmetric carbon atom marked * may have the D- or L- configuration, wherein the compound has affinity for the active site of thrombin.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of the formula:
- ##STR20## in which X.dbd.H or is an N-protecting group;
- Y is a sequence of 1-10 .alpha.-amino acids;
- Q1 and Q2 taken together represent the residue of a diol;
- R is C.sub.1-4 alkyl;
- and the asymmetric carbon atom marked * may have the D- or L- configuration, wherein the compound has affinity for the active site of thrombin.
Dependencies are inferred from the claim text.