申请人:Farmitalia Carlo Erba S.r.l.
公开号:US05656654A1
公开(公告)日:1997-08-12
Arylidene and heteroarylidene oxindole derivatives of formula (I) ##STR1## wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline; R is hydrogen or an oxo (.dbd.O) group when Y is tetralin; or R is hydrogen when Y is naphthalene, quinoline or isoquinoline; each of R.sup.1 and R.sup.2 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; m is zero, 1 or 2; n is zero, 1, 2 or 3; each of R.sup.3 and R.sup.4 independently is hydrogen, halogen, cyano, C.sub.1 -C.sub.6 alkyl, carboxy, nitro or --NR.sup.6 R.sup.7 in which each of R.sup.6 and R.sup.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.
Arylidene和heteroarylidene氧吲哚衍生物的化学式(I)如下:其中,对于规定,Y是选择自萘、四氢萘、喹啉和异喹啉的双环环系统;当Y是四氢萘时,R是氢或氧代(.dbd.O)基团;或当Y是萘、喹啉或异喹啉时,R是氢;R.sup.1和R.sup.2中的每一个独立地是氢、C.sub.1-C.sub.6烷基或C.sub.2-C.sub.6烷酰基;m为零、1或2;n为零、1、2或3;R.sup.3和R.sup.4中的每一个独立地是氢、卤素、氰基、C.sub.1-C.sub.6烷基、羧基、硝基或--NR.sup.6 R.sup.7,其中R.sup.6和R.sup.7中的每一个独立地是氢或C.sub.1-C.sub.6烷基;R.sup.5是氢或C.sub.1-C.sub.6烷基;以及它们的药学上可接受的盐,用作酪氨酸激酶抑制剂。