申请人:Leif Lundblad
公开号:US04990510A1
公开(公告)日:1991-02-05
Substituted indoloquinoxalines of the general formula I ##STR1## wherein R.sub.1 represents one of several, preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, prefrably Br, lower alkyl/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group; X is a group --(CH.sub.2).sub.n--R.sub.2 wherein R.sub.2 represents a nitrogen containing basic residue such as NH.sub.2, NHR.sub.4 or NR.sub.5 R.sub.6 wherein R.sub.4, R.sub.5 and R.sub.6 independently are lower alkyl or cykloalkyl and n is an integer of from 1 to 4 and R.sub.3 represents hydrogen, lower alkyl/cykloalkyl group having not more than 4 carbon atoms, and the physiologically acceptable addition products of the compounds with acids and halogen adducts, preferably adducts with iodine, iodine monochloride or iodine monobromide. Also methods for preparing said compounds by reacting a compound of the formula II ##STR2## with a reactive compound containing the residue --CHR.sub.3 R.sub.7 or by rearranging a compound the formula III by heating are described. The novel indoloquinoxalines have antiviral effect and have effect against cancer.
通式I的吲哚喹喔啉衍生物,其中R.sub.1代表1-4个相似或不同的取代基之一,在位置1-4和/或7-10,选择自卤素,优选溴,碳原子不超过4个的低烷基/烷氧基团,三氟甲基团,三氯甲基团;X是一个基团--(CH.sub.2).sub.n--R.sub.2,在其中R.sub.2代表氮含基团,如NH.sub.2,NHR.sub.4或NR.sub.5 R.sub.6,其中R.sub.4,R.sub.5和R.sub.6独立地是低烷基或环烷基,n是1到4的整数,R.sub.3代表氢,碳原子不超过4个的低烷基/环烷基团,以及所述化合物与酸和卤素加合物的生理上可接受的加合物,优选与碘,一氯化碘或溴化碘的加合物。还描述了通过将通式II的化合物与含有残基--CHR.sub.3 R.sub.7的反应性化合物反应或通过加热重排通式III的化合物来制备所述化合物的方法。新型吲哚喹喔啉具有抗病毒作用和对抗癌症的作用。