SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION

摘要

The present invention relates to compounds useful as tyrosine kinase inhibitors, having general formula (I) wherein one of the groups X<1>, X<2>, X<3>, X<4> is N and the others are CH; R is a group of formula (a), (b), (c) or (d) each of R<1> and R<3> independently is hydrogen, amino, carboxy, cyano, -SO3R<4>. -SO2NHR<5>. (1), -COOR<6>, -CONH(CH2)oPh, -CONHCH2(CHOH)nCH2OH, (2), -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NHC(NH2)=NH, -NHCO(CHOH)nCH2OH, (3), -NHSO2R<7>, -OCH2(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, C1-C6 alkyl, C2-C6 alkanoyl, -CH2OH, -CH2CH2CONH2, -SO2Me, -COCH2SO2NH2; R<4> is H, -CH2(CHOH)nCH2OH, C1-C6 alkyl; R<5> is H, C1-C6 alkyl, -CH2(CHOH)nCH2OH, -(CH2)mNMe2; R<6> is C1-C6 alkyl, unsubstituted or substituted by phenyl, -CH2(CHOH)nCH2OH; R<7> is Me, -C6H4Me; 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 R<3> is not H; and the pharmaceutically acceptable salts thereof.