申请人:CIBA-GEIGY AG
公开号:EP0475895A1
公开(公告)日:1992-03-18
The invention relates to novel polycyclic derivatives of rifamycins of the formula
and the salts thereof, in which the structural elements -A₁-A₂-, -A₃-A₄- and -A₅-A₆- each denote ethylene or vinylene or the elements -A₁-A₂- and -A₃-A₄- each denote ethylene and -A₅-A₆- denotes vinylene; X represents
and R₆ denotes hydrogen or alkyl; A denotes a bivalent aliphatic hydrocarbon radical, a bond, or, if X represents
represents the structural element -X₁-A₁- in which X₁ denotes -O-, -S(O)n- or -C(R₆)- n being 0, 1 or 2 and R₆ being hydrogen or alkyl and in which A₁ denotes a bivalent aliphatic hydrocarbon radical; R₁ denotes hydrogen or acyl; R₂ denotes acyl or an aliphatic radical; and R₃ and R₃′ represent a common bond; or R₃ denotes hydrogen, acyl or an aliphatic radical, and R₃′ is hydrogen or an aliphatic radical; R₄ denotes hydrogen, optionally substituted cycloalkyl in which a C-atom is optionally replaced by -O- or -S(O)n and n is 0, 1 or 2, aryl or heteroaryl; R₅ denotes hydrogen or acetyl; R₇ denotes hydrogen or alkyl; the preparation and use thereof, and pharmaceutical products and the preparation thereof.
本发明涉及一种新的利福霉素的多环衍生物及其盐,其化学式中结构元素-A₁-A₂-,-A₃-A₄-和-A₅-A₆-分别表示乙烯或乙烯基,或元素-A₁-A₂-和-A₃-A₄-表示乙烯,而-A₅-A₆-表示乙烯基;X代表,R₆代表氢或烷基;A表示二价脂肪族碳氢化合物基、键或,如果X表示结构元素-X₁-A₁-,其中X₁表示-O-,-S(O)n-或-C(R₆)-,n为0、1或2,R₆为氢或烷基,而A₁表示二价脂肪族碳氢化合物基;R₁表示氢或酰基;R₂表示酰基或脂肪基;R₃和R₃′表示共价键;或R₃表示氢、酰基或脂肪基,而R₃′表示氢或脂肪基;R₄表示氢、可选取代的环烷基,其中一个C原子可选地被-O-或-S(O)n替换,n为0、1或2,芳基或杂环芳基;R₅表示氢或乙酰基;R₇表示氢或烷基;其制备和用途以及制备的药物产品。