发明名称 SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION.
摘要 <p>The present invention relates to compounds useful as tyrosine kinase inhibitors, having general formula (I) wherein one of the groups X1, X2, X3, X4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) each of R1 and R3 independently is hydrogen, amino, carboxy, cyano, -SO3R4. -SO2NHR5. (1), -COOR6, -CONH(CH2)oPh, -CONHCH2(CHOH)nCH2OH, (2), -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NHC(NH2)=NH, -NHCO(CHOH)nCH2OH, (3), -NHSO2R7, -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; R2 is H, C1-C6 alkyl, C2-C6 alkanoyl, -CH2OH, -CH2CH2CONH2, -SO2Me, -COCH2SO2NH2; R4 is H, -CH2(CHOH)nCH2OH, C1-C6 alkyl; R5 is H, C1-C6 alkyl, -CH2(CHOH)nCH2OH, -(CH2)mNMe2; R6 is C1-C6 alkyl, unsubstituted or substituted by phenyl, -CH2(CHOH)nCH2OH; R7 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 R1 is not H and when R is (d) then one of R1 and R3 is not H; and the pharmaceutically acceptable salts thereof.</p>
申请公布号 MX9600686(A) 申请公布日期 1997.06.28
申请号 MX19960000686 申请日期 1995.05.30
申请人 PHARMACIA S.P.A. 发明人 FRANCO BUZZETTI;MARIA GABRIELLA BRASCA;ANTONIO LONGO;DARIO BALLINARI
分类号 A61K31/435;A61K31/445;A61K31/495;A61K31/535;A61K45/06;A61P35/00;C07D471/04;C07F9/6561;(IPC1-7):C07D471/04;C07F09/656 主分类号 A61K31/435
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