Abstract: A method of inhibiting thrombin is disclosed, as well as a method of treating or preventing thrombosis and hypercoaguability. The methods employ compounds of the formula ##STR1## stereoisomers thereof and physiologically acceptable salts thereof.

Abstract: The invention relates to new competitive inhibitors of thrombin, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for prophylaxis and treatment of thromboembolic diseases, according to the formula ##STR1## wherein A represents a methylene group, an ethylene group or a propylene group, which may be substituted orA represents --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --S--CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 --, orA represents --CH.sub.2 --O--, --CH.sub.2 --S--, --CH.sub.2 --SO--, with the heteroatom functionality in position 4, orn is an integer 2 to 6; andB represents --N(R.sup.6)--C(NH)--NH.sub.2, wherein R.sup.6 is H or a methyl group, orB represents --S--C(NH)--NH.sub.2, or --C(NH)--NH.sub.2.

Abstract: A method is disclosed for treatment or prophylaxis of arterial thrombosis employing the compound HOOC-CH.sub.2 -(R)Cha-Pic-Nag or a stereoisomer thereof or a physiologically acceptable salt thereof.