| 摘要 |
<p>The present invention relates to compounds useful as tyrosine kinase inhibitors, having general formula (I) wherein one of the groups X?1, X2, X3, X4¿ is N and the others are CH; R is a group of formula (a), (b), (c) or (d) each of R?1 and R3¿ independently is hydrogen, amino, carboxy, cyano, -SO¿3?R?4. -SO¿2NHR5. (1), -COOR6, -CONH(CH¿2?)oPh, -CONHCH2(CHOH)nCH2OH, (2), -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NHC(NH2)=NH, -NHCO(CHOH)nCH2OH, (3), -NHSO2R?7¿, -OCH¿2?(CHOH)nCH2OH, -OOC(CHOH)nCH2OH, -OPO(OH)2, -OCH2SO2NH2, -CH2NH2, -C(NH2)=NH, -CH2NHC(NH2)=NH, (4), -CH2OH, -CH2OOC(CHOH)nC2OH, -CH2OPO(OH)2, -PO(OH)2; R?2¿ is H, C¿1?-C6 alkyl, C2-C6 alkanoyl, -CH2OH, -CH2CH2CONH2, -SO2Me, -COCH2SO2NH2; R?4¿ is H, -CH¿2?(CHOH)nCH2OH, C1-C6 alkyl; R?5¿ is H, C¿1?-C6 alkyl, -CH2(CHOH)nCH2OH, -(CH2)mNMe2; R?6 is C¿1-C6 alkyl, unsubstituted or substituted by phenyl, -CH2(CHOH)nCH2OH; R7 is Me, -C¿6?H4Me; Z is CH2, O, NH, NCH2CH2OH; n is 0 or 1; m is 2 or 3; o is 0, 1, 2 or 3; p is 1, 2 or 3; provided that when R is (a), (b), or (c) then R?1¿ is not H and when R is (d) then one of R?1 and R3¿ is not H; and the pharmaceutically acceptable salts thereof.</p> |
