| 摘要 |
FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention relates to novel derivatives of azethedine of the formula (I): in free form or as a salt wherein Ar means phenyl optionally substituted with one or some substitutes chosen from halogen atom, (C1-C8)-alkyl, cyano-group; R1 means hydrogen atom (H), (C1-C8)-alkyl optionally substituted with hydroxy-, (C1-C8)-alkoxy-, (C1-C8)-alkylcarbonyloxy-group, halogen atom, carboxy-group, (C1-C8)-alkoxycarbonyl; R2 means H, (C1-C8)-alkyl, (C3-C10)-cycloalkyl; R3 means (C1-C8)-alkyl substituted with phenyl, phenoxy-, (C1-C8)-alkylcarbonyloxy-group, naphthyl; or R2 represents (C3-C10)-cyclalkyl optionally comprising benzo-group, condensed benzo-group, 5-6-membered heterocyclic group comprising 1-3 different heteroatoms chosen from nitrogen (N), oxygen (O) and sulfur (S), or up to 4 N atoms, or it means 5-6-membered heterocyclic group comprising 1 or 2 ring O or N atoms and optionally substituted with substitutes enumerated in the formula; or R3 means phenyl or naphthyl wherein indicated phenyl, phenoxy- or naphthyl group is substituted optionally with one or some substitutes chosen from halogen atom, cyano-, hydroxy-group, (C1-C8)-alkylcarbonyl, -SO2NH2, (C1-C8)-alkyl, optionally substituted (C1-C8)-alkoxy-, (C1-C8)-alkylthio-group, -SO2-(C1-C8)-alkyl, (C1-C8)-alkoxycarbonyl, (C1-C8)-acylamino-group substituted optionally with (C1-C8)-alkyl by nitrogen atom, (C1-C8)-alkylamino-group, aminocarbonyl, (C1-C8)-alkylaminocarbonyl, di-(C1-C8-alkyl)amino-group, di-(C1-C8-alkyl)aminocarbonyl, di-(C1-C8-alkyl)aminocarbonylmethoxy-group; X means -C(=O)-, -O-, -CH2- or -CH(OH); Y means O, S; m means 1, 2, 3 or 4; each n, p and q means 0 or 1, n + p + q = 1, n + q = 1 and p+ q = 1 and when n means 0 then p means 0. Compounds of the formula (I) inhibit binding eotaxine with CCR-3 receptor that allows their using as component of pharmaceutical composition and for preparing a medicinal agent used in inflammatory or allergic state. ^ EFFECT: valuable medicinal properties of compounds and pharmaceutical composition. ^ 15 cl, 5 tbl, 201 ex |
