NEW LEUKOTRIENE B 4? DERIVATIVES, METHOD FOR PREPARING THEM AND THEIR USE AS DRUGS.

摘要

Leukotriene-B4 derivatives of formula I (I) are described, in which R1 means CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 together with R2 means a carbonyl group, R2 and R3 are the same or different and represent H or an organic acid radical with 1-15 C atoms, R4 symbolizes H, C1-C10 alkyl optionally substituted once or several times by chlorine or bromine, C3-C10 cycloalkyl, C6-C10 aryl radical optionally substituted, independent from one another, once 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 means hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C10 aryl radical optionally 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 56-membered ring with at least 1 heteroatom, A symbolizes a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B symbolizes a C1-C10 straight-chain or branched-chain alkylene group, which optionally can be substituted by fluorine or the group , D can mean a direct bond, oxygen, sulfur, -C?C-, -CH=CR8 or together with B can also mean a direct bond, R6 and R7 are the same or different and represent H or C1-C4 alkyl or R7 represents H and R6 represents C1-C10 alkanoyl or C1-C10 alkanesulfonyl, R8 means H, C1-C5 alkyl, chlorine, bromine, n is 3-5 as well as, if R5 means hydrogen, their salts with physiologically compatible bases and their cyclodextrin clathrates.