| 摘要 |
FIELD: organic chemistry, peptides. SUBSTANCE: invention relates to group of novel individual compounds of the formula (I): where: R is optionally substituted aryl, aryl-(lower)-alkyl, (lower)-alkenyl, (lower)- alkynyl or N-containing heterocyclyl; R2 and R3 each independently each of other means hydrogen atom or optionally substituted (lower)-alkyl, aryl-(lower)-alkyl, cycloalkyl-(lower)-alkyl; or R2 and R3 mean in common (lower)-alkylene by so that in common with carbon atom with which they are bound form a ring; R4 and R5 each independently each of other is H or optionally substituted (lower)-alkyl, aryl-(lower)-alkyl; or R4 and R5 in common mean (lower)-alkylene by so that in common with carbon atom with which they are bond form a ring; or R4 is H and R5 means substituents of the formula -X2--Ar-Z where: X2 means C2-C7-alkylene containing O, S or CON in chain; Ar means arylene; Z means carboxyl or esterified carboxyl; X1 means -C(O)- or -S(O)2-; Y means oxygen atom; L means optionally substituted -Het-, -Het-CH2- or -CH2- Het- where Het means heteroatom taken among O and N and x = 0 or 1; in the above given values aryl is carbocyclic or heterocyclic aryl, its physiologically acceptable and cleaving ester or salt. Invention relates also to method of synthesis of compounds of the formula (I) by claim 1 that are effective inhibitors of cysteine cathepsins. EFFECT: improved method of synthesis, valuable biochemical properties of compounds. 10 cl, 11 tbl
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