申请人:Ciba-Geigy Corporation
公开号:US05149717A1
公开(公告)日:1992-09-22
Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.
通式为##STR1##的烷基酮衍生物,其中 R.sub.1 为未取代或氟代的较低烷基,R.sub.2 为氢,或未取代或氟代的较低烷基或较低烯基,X 为较低烷基,氧,硫或直接键,alk 为较低烷基,n 为1或2,R.sub.3 为未取代的苯基或被未取代或氟代的较低烷基、醚化或酯化的羟基、未取代或较低烷基化的氨基和/或自由、酯化或酰胺化的羧基取代的苯基,或未取代的较低烷基,被氟和氯取代或被自由酯化或酰胺化的羧基取代,R.sub.4 为自由、酯化或酰胺化的羧基或5-四唑基,R.sub.5 为氢或较低烷基,具有白三烯拮抗性质,可用作药物中的抗过敏活性成分。