| 摘要 |
Leukotriene-B4 derivatives have the formula (1), in which R1 stands for CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 represents together with R2 a carbonyl group; R2 and R3 are different or the same and stand for H or an organic acid residue with 1-15 C atoms; R4 stands for H, C1-C10-alkyl, possibly substituted one or several times by chlorine or bromine, C3-C10-cycloalkyl, a C6-C10-aryl residue possible independently substituted one or several times by chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy or a 5-6 membered aromatic heterocyclic ring with at least 1 heteroatom; R5 stands for hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, an aryl residue possibly substituted by 1-3 chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, CH2-CO-(C6-C10)aryl or a 5-6 membered ring with at least 1 heteroatom; A stands for a trans, trans-CH=CH-CH=CH, -CH2CH2-CH=CH- or a tetramethylene group; B stands for a straight or branched chain C1-C10alkylene group, possibly substituted with fluorine or the group (a); D is a direct bond, oxygen, sulphur, -C?C-, -CH = CR8 or it may represent together with B a direct bond: R6 and R7 are different or the same and stand for H or C1-C4-alkyl or R7 stands for H and R6 stands for C1-C10-alkanoyl or C1-C10-alkansulphonyl; R8 stands for H, C1-C5-alkyl, chlorine, bromine; m stands for the digits 1 or 4 and n equals 3-5. Also disclosed are the salts of these derivatives with physiologically tolerable bases, when R5 stands for hydrogen, and their cyclodextrine clathrates.
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