FIELD: organic chemistry, pharmaceuticals.
SUBSTANCE: invention relates to new imidazolydine derivatives of formula I wherein A is cyclopropylmethyl or isobuthyl; E is -CO-R6 or -CH2-O-R7; Z is oxygen; R1 is hydrogen or methyl; R2 is phenyl, pyridyl or C1-C4-alkyl; R3 and R4 are methyl or trifluorometyl; R5 is hydrogen or C1-C4-alkyl; R6 is hydroxyl; R7 is hydrogen; or R- or S-stereomeres, or R/S-stereomere mixture, or physiologically acceptable salts thereof. Said derivatives represent valuable pharmaceutically active compounds, useful in treatment of e.g. rheumatoid arthritis or allergic diseases. Derivatives of formula I are inhibitors of leukocyte adhesion and migration and/or antagonists of VLA-4 adhesion receptor from integrine group. Said derivatives are useful in treatment of diseases associated with undesired leukocyte adhesion and/or migration, as well as diseases mediated by intracellular interaction or cell-matrix interaction. Method for production of compound of formula I and pharmaceutical agent based on the same also are disclosed.
EFFECT: new imidazolydine derivatives useful as pharmaceutical agents.
14 cl, 23 ex
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Authors
Dates
2007-07-27—Published
2002-02-23—Filed