INHIBITORS OF PROCESSES ASSOCIATED WITH DP-IV Russian patent published in 2000 - IPC

FIELD: organic chemistry. SUBSTANCE: invention describes inhibitors of process associated with DP-IV taken among compounds of the general formula: A-B (group I) where B means formula (I) ; n = 1 or 2; m = 0, 1 or 2; X means CH₂, S, SO, SO₂, O; Y means N; R means H, CN, CHO, B(OH)₂; A is bound to Y and a) when R means H, then A is alpha-aminoacyl group obtained from alpha-amino acid carrying cycloaliphatic side chain or beta-aminoacyl group of the general formula (II) where p = 1-6 and in any case ring can contain unsaturated bonds and/or substitution with heteroatom; b) when R means CN then A corresponds to definition given in (a) and except for it can be obtained from any L-alpha-amino acid carrying lipophilic side chain and c) when R means CHO or B(OH)₂ then A means beta-aminoacyl group determined in (a); (group II): B, n, m, X as indicated above; R means H, CN; A is bound to Y and A means (i) where a = 1-5; D means G-(CH₂)_b-(R₄)-R₃; G means NH or NMe; b = 1-12; g = 0 or 1; R₄ means Z-NH-(CH₂)_c or NH-Z-(CH₂)_c- where c = 1-12; Z means CO, CH₂; R₃ is CO₂H or its ester, CONH₂, CONR₅R₆, SO₂NH₂, SO₂NR₅R₆, OH, OR₅, substituted or unsubstituted aryl, NH₂, NR₅R₆, NHCOR₅, NHSO₂R₅, NH-CH(:NR₅)NR₅R₆; R₅ and R₆ are taken independently each of other among H, lower alkyl, fluoroalkyl groups or R₅ and R₆ in common with nitrogen atom to which they are bound form the chain C₃-C₈ or A means (ii) where R¹ is H, Me; E is J-(CH₂)_b-(R₄)_q-R₃; J is CO; a, b, q, R₃ and R₄ correspond to definition given in (i); or it means (III) where R² is H, Me; L means (CH₂)_d-(CO)_r-(CH₂)_b-(R₄)_q-R₃ where r = 1; d = 1-4; b, q, R₃ and R₄ correspond to definition given in (i). The above described inhibitors are highly active competitive inhibitors of DP-IV (values K are in the range from 10^-6 to 10^-10) and they exhibit chemical stability (t_1/2 > 24 h). EFFECT: inhibitors indicated above, valuable chemical properties. 4 cl, 8 tbl, 7 ex