DIPHENYLAZETHIDINONES SUBSTITUTED WITH ACIDIC GROUPS, METHOD FOR THEIR PREPARING, MEDICINAL AGENT COMPRISING THEREOF AND THEIR USING

FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention relates to novel diphenylazethidinones substituted with acidic groups of the formula (I): , wherein one R1 or R2 means hydrogen atom (H) and another means atoms F, Cl, Br, J, -O-(C1-C6)-alkyl, (C0-C30)-alkylene-LAG wherein one or s...

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Hauptverfasser: LINDENSHMIDT ANDREAS, SHEFER KHANS-LJUDVIG, FLOR SHTEFANI, KRAMER VERNER, JENE GERKHARD, FRIK VENDELIN, GLOMBIK KHAJNER, KHOJER KHUBERT
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention relates to novel diphenylazethidinones substituted with acidic groups of the formula (I): , wherein one R1 or R2 means hydrogen atom (H) and another means atoms F, Cl, Br, J, -O-(C1-C6)-alkyl, (C0-C30)-alkylene-LAG wherein one or some carbon atoms in alkylene residue can be substituted for -O-, -NH-, -(C=O)-, -N(C1-C6)-alkyl-; LAG means -(CH2)1-10-SO3H, -(CH2)0-10-COOH; one R3 or R4 means H and another means atoms F, Cl, Br, J, (C0-C30)-alkylene-LAG wherein one or some carbon atoms in alkylene residue can be substituted for -O-, -NH-, -(C=O)-, -N-(C1-C6)-alkyl-; LAG means -(CH)1-10-SO3H, -(CH)0-10-P(O)(OH)2, -(CH2)0-10-O-P(O)(OH)2. -(CH2)0-10-COOH; n = 1-2; one R5 or R6 means H and another means atoms F, Cl, Br, J, and their pharmaceutically acceptable salts but compound 2-{[4-(4-{1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxypropyl]-4-oxoazethidine-2-yl}phenoxy)-butyl]methylamino}ethanesulfoacid and compounds wherein residues R1-R4 mean -O-(CH2)1-10-COOH, (C1-C6)-alkylene-COOH or -COOH are excluded. Compounds of the formula (I) possess the effect decreasing the cholesterol level and can be used as component of a medicinal agent. ^ EFFECT: improved preparing method, valuable medicinal properties of compounds and medicinal agents. ^ 7 cl, 1 tbl, 13 ex