| abstract |
Leukotriene-B4 derivatives correspond to formula (I), in which R1 denotes CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 denotes with R2 a carbonyl group; R2 and R3 are the same or different and denote H or an organic acid residue having 1 to 15 carbon atoms; R4 denotes H, C1-C10 alkyl, optionally substituted one or more times with chlorine or bromine, C3-C10 cycloalkyl, a C6-C10 aryl residue optionally substituted independently of one another one or more times with chlorine, bromine, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or a 5 or 6-membered aromatic heterocyclic ring having at least 1 heteroatom; R5 denotes hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl residue substituted where appropriate by 1-3 chlorine, bromine, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, aryl CH2CO- (C6-C10) or a 5 or 6-membered ring having at least one heteroatom; A denotes a tetramethylene group, trans, trans-CH = CH-CH = CH-, or -CH2CH2-CH = CH-; B denotes a C1-C10 alkylene group with a straight or branched chain, optionally substituted by fluorine, or group (a); D denotes a direct bond, oxygen, sulfur, -C = C-, -CH = CR8 or can represent with B a direct bond; R6 and R7 are the same or different and denote H or C1-C4 alkyl, or else R7 denotes H and R6 denotes C1-C10 alkanoyl or C1-C10 alkansulfonyl; R8 denotes H, C1-C5 alkyl, chlorine, bromine; m denotes the figures 1 or 4 and n is between 3 and 5. The invention also relates to the salts of these derivatives with physiologically tolerable bases, when R5 denotes hydrogen, as well as their cyclodextrin clathrates. |