Prodrugs of thrombin inhibitors
AssigneeAstra AB
InventorsDavid Gustafsson, Jan-Erik Nystrom, Henrik Sorensen, Mikael Sellen
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Abstract
There is provided compounds of formula I, R.sup.1 O(O)C--CH.sub.2 --(R)Cgl-Aze-Pab-R.sup.2 I wherein R.sup.1 and R.sup.2 have meanings given in the description, which are useful as prodrugs of inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (eg thrombosis) or as anticoagulants.
Claims38
A compound of the formula I,
- R.sup.1 O(O)C--CH.sub.2 --(R)Cgl-Aze-Pab-R.sup.2 I
- wherein
- R.sup.1 represents H or C.sub.1-10 alkyl;
- R.sup.2, which replaces one of the hydrogen atoms in the amidino unit of Pab-H, represents OH;
- or a pharmaceutically-acceptable salt thereof.
MeOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
EtOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
nPrOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
iPrOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
tBuOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
HOOCCH.sub.2 --(R)Cgl-Aze-Pab-OH.
Dependencies are inferred from the claim text.