| abstract |
Described are pharmacologically active leukotriene B4 derivatives of general formula (I) in which R1 is CH2OH, CH3, CF3, COOR4 or CONR5R6, R2 is H or an organic-acid group with 1 to 15 C-atoms, R3 is H, a C1-C14 alkyl group, optionally with one or more substituents, a C3-C10 cycloalkyl group, a C6-C10 aryl group optionally substituted, independently of each other, with one or more halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy groups or R3 is a 5- to 6-membered aromatic heterocyclic ring with at least one hetero atom, R4 is H, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl group optionally substituted with 1 to 3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy groups or R4 is CH2-CO-(C6-C10) aryl or a 5- to 6-membered ring with at least one hetero atom, A is a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B is a straight-chain or branched-chain C1-C10 alkylene group, which may be substituted with fluorine, or the group (a), D is a direct bond, oxygen, sulphur, -CC- or -CH=CR7 or, together with B, may also form a direct bond, R5 and R6 which may be the same or different, are H or C1-C4 alkyl, or R6 is H and R5 is C1-C15 alkanoyl or R8SO2-, R5 and R6 being optionally substituted with OH, R7 is H, C1-C5 alkyl, chlorine or bromine, R8 is defined in the same way as R3, n is 2 to 5 plus, when R4 is hydrogen, salts of these compounds with physiologically tolerated bases, as well as their cyclo-dextrin clathrates. |