| 摘要 |
FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of isoxazole of the formula (1) where D means hydrogen atom; one of A and B means group (1) -E-N= C(NR25R26)NR27R28 where E means a single bond or alkylene group; R25 and R26 each means independently hydrogen atom, C1-4-alkyl, -(CH2)n-CO2R32 where n is a whole number 1-3; R32 means hydrogen atom, C1-4-alkyl, -(CH2)m-CO2R35 where m = 2 or 3; R35 means hydrogen atom, C1-4-alkyl, -(CH2)m where m is given above or -(CH2)n-C(O)R36 where n is given above; R36 means hydrogen atom, C1-4-alkyl and so on; or taken in common they form with nitrogen atom 5-7-membered saturated nitrogen-containing heterocyclic group that can be substituted with one or two substituted taken among alkyl group, hydroxyl group and oxo-group; R27 and R28 each means independently hydrogen atom, -(CO)O-R32 where R32 means C1-4-alkyl; or R26 and R27 form with two nitrogen atoms and one carbon atom 5-7-membered saturated nitrogen-containing heterocyclic group that can be substituted with one or two substitutes taken among alkyl group, -(CH2)m-; R25 and R26 mean independently hydrogen atom, C1-3-alkyl or -(CH2)m-OH-OH and so on; (2) -E-N(R45)C(NR46R47)=NR48 where R45 means hydrogen atom, C1-4-alkyl, -(CO)O-R32; R48 means hydrogen atom, benzyl group and so on; and R47 each means hydrogen atom, C1-4-alkyl, -(CO)O-R32; or taken in common they form with nitrogen atom 5-7-membered saturated nitrogen-containing heterocyclic group and so on; one of A and B means group of the formula -J-G where G means phenyl, biphenyl, benzoylphenyl and so on; J means -C(R8R9)- or -C(=CR8R9)-, where R8 and R9 mean independently hydrogen atom, lower alkoxy-group, lower alkyl group and so on; or their pharmaceutically acceptable salts. Invention relates also to pharmaceutical composition used for treatment of autoimmune diseases or inflammatory diseases and comprising derivative of isoxazole of the formula (1) or its pharmaceutically acceptable salt as active component in common with pharmaceutically acceptable carrier. Invention relates also to method of treatment of autoimmune diseases or inflammatory diseases involving administration of derivative of isoxazole of the formula (1) or its pharmaceutically acceptable salt in effective amount in human body. EFFECT: new isoxazole derivatives, valuable medicinal properties of compounds. 12 cl, 1 dwg, 4 tbl |
