申请人:Schering Aktiengesellschaft
公开号:US05183925A1
公开(公告)日:1993-02-02
The invention relates to leukotriene-B.sub.4 derivatives of formula I, ##STR1## in which n=1-10, R.sub.1 means radical CH.sub.2 OH, radical COOR.sub.4, radical CONHR.sub.5 or radical CONR.sub.6 R.sub.7, A means a cis, trans or trans, trans--CH.dbd.CH--CH.dbd.CH group or tetramethylene group, B means an alkylene group with up to 10 C atoms, D means a direct compound, oxygen, sulfur, a --C.tbd.C group or a --CH.dbd.CR.sub.8 group, B and D together mean a direct bond, R.sub.2 means a hydrogen atom or an acid radical of an organic acid with 1-15 C atoms and R.sub.3 means a hydrogen atom, an optionally substituted alkyl radical with 1-10 C atoms, a cycloalkyl radical with 3-10 C atoms, an optionally substituted aryl radical with 6-10 C atoms or a 5-6 member heterocyclic radical and if R.sub.4 means a hydrogen atom, their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their pharmaceutical use.
本发明涉及化合物I的白三烯-B.sub.4衍生物,其中:##STR1## 其中n = 1-10,R.sub.1表示基团CH.sub.2 OH、基团COOR.sub.4、基团CONHR.sub.5或基团CONR.sub.6R.sub.7,A表示顺式、反式或反式,反式-CH.dbd.CH-CH.dbd.CH基团或四亚甲基基团,B表示最多有10个C原子的烷基基团,D表示直接化合物、氧、硫、-C.tbd.C基团或-CH.dbd.CR.sub.8基团,B和D一起表示直接键,R.sub.2表示氢原子或具有1-15个C原子的有机酸的酸基基团,R.sub.3表示氢原子、可选择取代的1-10个C原子的烷基基团、3-10个C原子的环烷基团、6-10个C原子的可选择取代的芳基基团或5-6个成员的杂环基团,如果R.sub.4表示氢原子,则它们与生理兼容的碱盐和它们的环糊精包合物,以及它们的制备方法和药物用途。