PRODRUGS OF THROMBIN INHIBITORS Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel compounds of the general formula (I): R¹-O(O)C-CH₂-(R)Cgl-Aze-Pab-R² where R¹ means -R³ or -A¹-C(O)N-(R⁴)R⁵ or -A¹-C(O)O-R⁴; A¹ means C_1-5-alkylene; R² (that replaces one of hydrogen atom in amidine unit in Pab-H) means OH, OC(O)-R⁶, C(O)O-R⁷ or C(O)OCH((R⁸))OC(O)-R⁹; R³ means H, C_1-10-alkyl or C_1-3-alkyl-phenyl (being the latter group is substituted possibly with C_1-6-alkyl); R⁴ and R⁵ mean independently H, C_1-6-alkyl or when R¹ means -A¹-C(O)N-(R⁴)R⁵ in common with nitrogen atom to which they are bound mean pyrrolidinyl group; R⁶ means C_1-17-alkyl or phenyl; R⁷ 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); R⁸ means H or C_1-4-alkyl and R⁹ means phenyl or C_1-8-alkyl being alkyl groups that can be presented by R³,R⁴,R⁵,R⁶,R⁷ and R⁹ 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 R¹ means R³ then R³ means benzyl, methyl, ethyl, n-butyl or n-hexyl group and R² means C(O)O-R⁷ and then R⁷ 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