| 摘要 |
FIELD: organic chemistry, chemical technology, pharmacy. ^ SUBSTANCE: invention relates to new five-member heterocyclic compounds of the general formula (I): ^ ^ wherein W means R1-A-C(R13); Y means carbonyl group; Z means N(R0); A means phenylene; E means R10CO; B means (C1-C6)-alkylene that can be unsubstituted or substituted with (C1-C6)-alkyl; R0 means if necessary (C6-C14)-aryl-(C1-C8)-alkyl substituted in aryl residue; R means hydrogen atom (H) or (C1-C6)-alkyl; R1 means X-NH-C(=NH)-(CH2)p wherein p = 0; X means hydrogen atom, hydroxyl group (-OH), (C1-C6)-alkoxycarbonyl or if necessary phenoxycarbonyl or benzyloxycarbonyl substituted in aryl residue; R2, R2a and R2b mean hydrogen atom; R3 means R11NH- or CO-R5-R6-R7; R4 means bivalent (C1-C4)-alkylene residue; R5 means bivalent residue of natural or non-natural amino acid with lipophilic by-side chain taken among the group consisting of (C1-C6)-alkyl residues, (C6-C12)-aryl-(C1-C4)-alkyl residues that can be substituted if necessary in aryl residue and if necessary substituted (C6-C12)-aryl residues; R6 means a single bond; R7 means Het; R10 means hydroxyl or (C1-C6)-alkoxy-group; R11 means R12-NH-C(O), R12-NH-C(S) or R14a-O-C(O) wherein R12 means (C6-C14)-aryl-(C1-C6)-alkyl substituted if necessary in aryl residue; R13 means (C1-C6)-alkyl; R14a means if necessary substituted heteroaryl, heteroaryl-(C1-C6)-alkyl substituted if necessary in heteroaryl residue or R15 wherein R15 means R16 or R16-(C1-C6)-alkyl; R16 means residue of 3-12-membered monocyclic or 6-24-membered bicyclic, or 6-24-membered tricyclic ring; Het means 5-7-membered monocyclic residue of heterocycle bound through nitrogen atom in ring and comprising if necessary another heteroatom among the group consisting of nitrogen atom (N), oxygen atom (O) or sulfur atom (S); g and h mean 0 or 1 in all their stereoisomeric forms and their mixtures and their physiologically acceptable salts also. Also, invention relates to pharmaceutical preparation eliciting ability to inhibit adhesion. ^ EFFECT: improved preparing method, valuable medicinal properties of compounds. ^ 13 cl, 5 ex |
