申请人:Schering Aktiengesellschaft
公开号:US06340706B1
公开(公告)日:2002-01-22
The invention relates to leukotriene B4 derivatives of general formula (I) in which R1 stands for CH2OH, CH3, CF3, COOR4, CONR5R6; R2 stands for H or an organic acid radical with 1-15 C atoms; R3 stands for H; R4 is hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical optionally substituted by 1-3 halogen, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or CH2—CO—(C6-C10) aryl, or a 5-6 link ring with at least 1 heteroatom; A is a trans-, trans-CH═CH—CH═CH, a —CH2CH2—CH═CH— or a tetramethylene group; B is a C1-C10 linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, —C≡C—, —CH═CR7, or a direct bonding with B. The invention also relates to salts thereof, having physiologically compatible bases and their cyclodextrin clathrates. The inventive substances can be used as pharmaceutical preparations
该发明涉及一般式(I)的白三烯B4衍生物,其中R1代表CH2OH、CH3、CF3、COOR4、CONR5R6;R2代表H或具有1-15个碳原子的有机酸基团;R3代表H;R4为氢、C1-C10-烷基、C3-C10-环烷基、一个C6-C10-芳基,可选择地被1-3个卤素、苯基、C1-C4-烷基、C1-C4-烷氧基、氟甲基、氯甲基、三氟甲基、羧基或羟基取代,或CH2—CO—(C6-C10)芳基,或至少含有1个杂原子的5-6环;A为反式、反式-CH═CH—CH═CH、—CH2CH2—CH═CH—或四亚甲基基团;B为C1-C10直链或支链烷基基团或组(a)或(b);D为直接键合、氧、硫、—C≡C—、—CH═CR7,或与B直接键合。该发明还涉及其盐,具有生理兼容的碱和其环糊精包合物。这些创新物质可用作制药制剂。