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 OH、
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、— —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。