NEW ANTI-DIABETIC AGENTS

FIELD: organic chemistry, medicine, endocrinology, pharmacy. ^ SUBSTANCE: invention relates to compounds of the formula (1) or its pharmaceutical salts wherein A means ^ R1 means hydrogen atom (H), (C1-C6)-alkyl (including branched alkyl and cycloalkyl), -(CH2)aNHW1, -(CH2)bCOW2, -(CH2)cOW3, -CH(Me)OW4, -(CH2)d-C6H4-W5, -(CH2)eSW6 wherein a = 2-5; b = 1-4; c = 1-2; d = 1-2; e = 1-3; W1 means -COW6, -CO2W6, -SO2W6; W2 means -OH, -NH2, -OW6, -NHW6; W3 means hydrogen atom (H), W6; W4 means H, W6; W5 means H, -OH, -OMe; W6 means (C1-C6)-alkyl, benzyl, optionally substituted phenyl wherein optional substitutes (up to two groups) are taken among (C1-C3)-alkyl, (C1-C3)-alkoxy-group, fluorine (F) and/or chloride (Cl) atoms; R2 means H, -(CH2)nNH-C5H3N-Y wherein n = 2-4; Y means H, F, Cl atoms, -NO2 and -CN; or R1 and R2 represent in common -(CH2)p- wherein p = 3 or 4; X is taken among: (i) one L-alpha-aminoacyl group taken among Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val, or two such groups that represent Arg and Ile; (ii) groups -R3CO wherein R3 represents H, (C1-C6)-alkyl (including branched alkyl and cycloalkyl) or phenyl; (iii) groups -R4COOC, -(R5)(R6)OCO wherein R4 means H, (C1-C6)-alkyl (including branched alkyl and cycloalkyl), benzyl or optionally substituted phenyl wherein substituted (up to two groups) are taken among (C1-C3)-alkyl, (C1-C3)-alkoxy-group, F and Cl atoms; each R5 and R6 means independently H or (C1-C6)-alkyl; or R5 and R6 mean in common -(CH2)m- wherein m means a whole number 4-6; and (iv) methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl groups; R7 is taken among pyridyl and optionally substituted phenyl wherein substitutes (up to two groups) are taken among (C1-C3)-alkyl, (C1-C3)-alkoxy-group, F, Cl atoms, -NO2, -CN and -CO2H; R8 means H or (C1-C3)-alkyl; R9 means H, (C1-C6)-alkyl, phenyl or (C1-C6)-alkoxy-group and under condition that indicated compound doesn't represent N(Z-Val)-2-cyanopyrrolidine. Compounds of the formula (1) are inhibitors of DP-IV and can be used in pharmaceutical compositions in treatment of the tolerance disturbances to glucose and diabetes mellitus of type 2. ^ EFFECT: valuable medicinal properties of compounds and compositions. ^ 26 cl, 2 tbl, 19 ex