HETEROCYCLES AS INHIBITORS OF LEUKOCYTE ADHESION AND VLA-4-ANTAGONISTS Russian patent published in 2004 - IPC

Abstract RU 2220977 C2

FIELD: organic chemistry, heterocyclic compounds, medicine, pharmacy. SUBSTANCE: invention relates to agent used for inhibition of adhesion or migration of leukocytes or for inhibition of VLA-4-receptor. Agent represents heterocycles of the general formula (I) wherein W means R1-A-C; R13 Y means carbonyl; Z means N(R0); A means bivalent phenylene residue, bivalent residue (C1-C6)-alkylene; B means bivalent residue (C1-C6)-alkylene that can be substituted with (C1-C8)-alkyl; D means C(R2)(R3), E means R10CO, R and R0, mean independently of one another hydrogen atom, substituted (C6-C14)-aryl if necessary, substituted heteroaryl if necessary, (C6-C14)-aryl- (C1-C6)-alkyl substituted in aryl residue if necessary or heteroaryl-(C1-C6)-alkyl substituted in heteroaryl residue if necessary; R1 means hydrogen atom, Het, residue R28N(R21)- C(O)-; R2 means hydrogen atom; R3 means CONHR4, R11NH,; R4 means (C1-C28)-alkyl that can be mono- or multiple substituted with similar or different residues if necessary taken among of row hydroxycarbonyl, (C1-C6)-alkoxycarbonyl and R5 wherein R5 means substituted (C6-C14)-aryl if necessary; R10 means hydroxyl or (C1-C6)-alkoxy-group; R11 means R12CO,; R12 means R15-O-; R13 means (C1-C6)-alkyl; R15 means R16-(C1-C6)-alkyl; wherein R16 means 7-12-membered bicyclic or tricyclic residue, saturated or partially unsaturated that can be substituted with one or some similar or different (C1-C4)-alkyl residues; R21 means hydrogen atom; R28 means R21; Het means mono- or polycyclic, 4-14-membered, aromatic or nonaromatic cycle that can comprise 1, 2, 3 or 4 nitrogen atoms; b, c, d and f mean independently of one another 0 or 1, however, they can not mean 0 simultaneously; e, g and h mean independently of one another 0, 1, 2, 3, 4, 5 or 6 in all their stereoisomeric forms and as their mixtures in any ratios, and their physiologically acceptable salts also. Invention describes pharmaceutical preparations comprising these compounds also. EFFECT: valuable biological and medicinal properties of heterocyclic compounds. 37 cl, 1 tbl, 1 sch, 4 ex

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RU 2 220 977 C2

Authors

Shtil'Ts Khans Ul'Rikh

Vener Fol'Kmar

Khjul'S Kristof

Zajffge Dirk

Dates

2004-01-10Published

1997-11-13Filed