Back to results
US 5,328,900 AGranted
Anti-thrombotic peptide and pseudopeptide derivatives
AssigneeRhone-Poulenc Rorer Pharmaceuticals Inc.
InventorsScott I. Klein, Bruce F. Molino
Life of this patent
Estimating the term…
Abstract
Disclosed are novel peptide and pseudopeptide derivatives and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
Claims16
A compound of the formula ##STR20## wherein:
- X is H, amidino, ##STR21## Y is --OR.sub.1, ##STR22## a D- or L-amino acid or its corresponding carboximide, a synthetic amino acid of the formula ##STR23## a dipeptide or a dipeptide isostere of the formula ##STR24## R.sub.1 and R.sub.2 are independently H, alkyl, aryl, aralkyl, or allyl;
- R.sub.3 is H, --CO.sub.2 H, --CO.sub.2 R.sub.1, --CONH.sub.2, ##STR25## R.sub.4 and R.sub.5 are independently H, alkyl, cycloalkyl, cycloalkylmethyl, ##STR26## p is 0 to 8;
- R.sub.6 and R.sub.7 form a ring with the nitrogen to which they are attached and are --(CH.sub.2).sub.4 --, (CH.sub.2).sub.5 --, --(CH.sub.2).sub.6 --, --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 NR.sub.1 CH.sub.2 -- or ##STR27## X.sub.2 is H, Cl, Br, F, --OR.sub.1, --NO.sub.2, ##STR28## --SR.sub.1, C.sub.1 -C.sub.5 alkyl, phenyl, --CO.sub.2 R.sub.1, ##STR29## --CF.sub.3 or --NHSO.sub.2 R.sub.1 ;
- V.sub.1 is ##STR30## --(CH.sub.2).sub.n --, --CH.dbd.CH--, --CH.sub.2 --NH--, --CH.sub.2 --O--, --CH.sub.2 --S-- or ##STR31## m is 0, 1 or 2;
- n is 0, 1, 2 or 3;
- and
- p is 0, 1, 2 or 3;
- or
- pharmaceutically acceptable salts thereof.
6 more elements
A compound according to claim I selected from the group consisting of:
- pyrrolidine-3-carboxyl-prolyl-aspartyl-leucine;
- pyrrolidine-3-carboxyl-prolyl-aspartyl-isoleucine;
- pyrrolidine-3-carboxyl-piperidine-2-carboxyl-aspartyl-valine;
- and
- pyrrolidine-3-carboxyl-piperidine-2-carboxyl-aspartyl-leucine.
2 more elements
Dependencies are inferred from the claim text.