| 摘要 |
A 3-cyano-quinoline derivative has the formula (I) or a pharmaceutically acceptable salt thereof wherein: X is optionally alkyl substituted cycloalkyl or optionally substituted pyrimidinyl or phenyl; Z is NH, O, S or NR; R is alkyl or carboalkyl; G1, G2, R1 and R4 are independently H, halo, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxy, alkoxymethyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulphonamido, alkenylsulphonamido, alkynylsulphonamido, hydry, CF3, CF3O, NO2, carboxy, carbalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, alkoxyamino, alkylamino, dialkylamino, N- alkylcarbamoyl, N-dialkylcarbamoyl, N-alkyl-N-alkenylamino, dialkenylamino, phenylamino, benzylamino, R8R9-CH-M- (C(R6)2)k-Y-, a group of formula (II), R7-(C(R6)2)g-Y-, R7- (C(R6)2)p-M-(C(R6)2)k-Y- or Het-(C(R6)2)q-W-(C(R6)2)k-Y- provided that either G1 or G2 must be R8R9-CH-M-(C(R6)2)k-Y- , a group of formula (II), R7-(C(R6)2)g-Y-, R7-(C(R6)2)p-M- (C(R6)2)k-Y-, Het-(C(R6)2)q-W-(C(R6)2)k-Y or -N(H)-R2; n is 0 or 1 and R2, R7 to R9, k, p, g, Y, Het, and q are as defined in the specification. The compounds are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
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