| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel compounds of the general formula (I): R 1 -O(O)C-CH 2 -(R)Cgl-Aze-Pab-R 2 where R 1 means -R 3 or -A 1 -C(O)N-(R 4 )R 5 or -A 1 -C(O)O-R 4 ; A 1 means C 1-5 -alkylene; R 2 (that replaces one of hydrogen atom in amidine unit in Pab-H) means OH, OC(O)-R 6 , C(O)O-R 7 or C(O)OCH((R 8 ))OC(O)-R 9 ; R 3 means H, C 1-10 -alkyl or C 1-3 -alkyl-phenyl (being the latter group is substituted possibly with C 1-6 -alkyl); R 4 and R 5 mean independently H, C 1-6 -alkyl or when R 1 means -A 1 -C(O)N-(R 4 )R 5 in common with nitrogen atom to which they are bound mean pyrrolidinyl group; R 6 means C 1-17 -alkyl or phenyl; R 7 means phenyl, C 1-3 -alkylphenyl (being two latter groups are substituted possibly with C 1-6 -alkyl, C 1-6 -alkoxy-group or nitro-group) or C 1-12 -alkyl (being the latter group is substituted possibly with C 1-6 -alkoxy-group or halogen atom); R 8 means H or C 1-4 -alkyl and R 9 means phenyl or C 1-8 -alkyl being alkyl groups that can be presented by R 3 ,R 4 ,R 5 ,R 6 ,R 7 and R 9 can be linear ones or in the case of sufficient amount of carbon atoms they can be branched, cyclic or partially cyclic, saturated or unsaturated ones and can be broken by oxygen atom under condition that when R 1 means R 3 then R 3 means benzyl, methyl, ethyl, n-butyl or n-hexyl group and R 2 means C(O)O-R 7 and then R 7 does not mean benzyl; or its pharmaceutically acceptable salt. New compounds relate to pharmaceutically useful prodrugs of pharmaceutically active compounds that are competitive inhibitors of trypsin-like serine proteases, especially, thrombin. EFFECT: new compounds indicated above, valuable medicinal properties. 66 cl, 1 tbl, 70 ex |