FIELD: organic chemistry, chemical technology, medicine, pharmacy.
SUBSTANCE: invention relates to new physiologically active compounds of the formula (I), its N-oxides, ester derivatives and their pharmaceutically acceptable salts and solvates also that elicit valuable pharmaceutical properties, in particular, the ability to control the interaction of VCAM-1 and fibronectin with integrin VLA-4 (α4β1) and they can be used in treatment of inflammatory diseases and asthma. In compound of the general formula (I):
X1 and X2 mean independently CR10; R4 means hydrogen atom or (C1-C4)-alkyl group; R10 means hydrogen atom, (C1-C4)-alkyl, (C1-C4)-alkoxy-group, (C1-C4)-alkylthio-group, (C1-C4)-alkylsulfinyl group or (C1-C4)-alkylsulfonyl group; R12 means hydrogen atom, (C1-C4)-alkyl or benzyl; R13 means (C1-C6)-alkyl optionally substituted with carboxy-group, (C1-C4)-alkoxyalkoxy-group, -OCH2CO2H, -NY1Y2 or with one or more hydroxy-groups; heteroaryl taken among imidazolyl, oxazolyl, pyridyl, thienyl and pyridazinyl each of that is substituted optionally with carboxy-group or (C1-C4)-alkyl; heterocycloalkyl, such as tetrahydropyranyl; or aryl taken among phenyl and naphthyl each of that can be substituted with carboxy-group, -NY4Y5 or one or more (C1-C4)-alkoxy-group wherein Y4 and Y5 represent independently (C1-C)-alkyl; R15 means -N(R12)-C(=O)-R13, -N(R12)-SO2-R13 or -NY1Y2 wherein Y1 and Y2 represent independently hydrogen atom, (C1-C4)-alkyl or aryl-(C1-C4)-alkyl, or the group -NY1Y2 can form 5-6-membered cyclic amine that can comprise additional heteroatom taken among oxygen atom or NY3 [wherein Y3 means -C(=O)-OR14 (wherein R14 means (C1-C4)-alkyl) or (C-C4)-alkyl]; Ar1 means unsubstituted phenylene. Invention relates also to a pharmaceutical composition and a method for treatment using compounds of the present invention.
EFFECT: improved treatment method, valuable medicinal properties of compounds.
16 cl, 51 ex
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|
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| 0 |
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SU542474A3 |
