申请人:Egis Gyogyszergyar
公开号:US04921854A1
公开(公告)日:1990-05-01
The compounds of the general formula I ##STR1## and pharmaceutically acceptable acid addition salts and hydrates thereof possess useful immunostimulant properties and can be used in therapy. In the general Formula I A stands for --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 CH.sub.2 --or --CH.dbd.CH--; R.sub.4 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl; r is 0, 1, 2, 3 or 4; R.sub.1 stands for hydrogen of C.sub.1-5 alkanoyl; R.sub.2 represents hydrogen, C.sub.1-5 alkanoyl or a group of the general formula (a) ##STR2## wherein R stands for hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, phenyl or phenyl-C.sub.1-3 alkyl and R.sub.3 stands for hydrogen. The compounds of the general Formula I can be prepared by reacting a 2-mercapto-4,6-diamino-pyrimidine of the general Formula II ##STR3## with a dihalo compound of the general Formula III ##STR4## (wherein Y and Z are halogen).
通用式I的化合物及其药学上可接受的酸盐和水合物具有有用的免疫刺激性质,并可用于治疗。在通用式I中,A代表--CH.sub.2--CH.sub.2--, --CH.sub.2--CH.sub.2--CH.sub.2--, --CH.sub.2--CH.sub.2--CH.sub.2CH.sub.2--或--CH.dbd.CH--; R.sub.4为氢、C.sub.1-4烷基或可选择地取代的苯基;r为0、1、2、3或4;R.sub.1代表氢或C.sub.1-5烷酰基;R.sub.2代表氢、C.sub.1-5烷酰基或通用式(a)的基团 ##STR2## 其中R代表氢、C.sub.1-4烷基、C.sub.2-4烯基、苯基或苯基-C.sub.1-3烷基,R.sub.3代表氢。通用式I的化合物可通过将通用式II的2-巯基-4,6-二氨基嘧啶与通用式III的二卤化合物反应而制备(其中Y和Z为卤素)。