发明公开
EP0715628A1 SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
失效
取代AZAINDOLYLIDENDERIVATE及其制备方法
- 专利标题: SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
- 专利标题(中): 取代AZAINDOLYLIDENDERIVATE及其制备方法
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申请号: EP95921777.0申请日: 1995-05-30
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公开(公告)号: EP0715628A1公开(公告)日: 1996-06-12
- 发明人: BUZZETTI, Franco , BRASCA, Gabriella, Maria , LONGO, Antonio , BALLINARI, Dario
- 申请人: PHARMACIA S.p.A.
- 申请人地址: Via Robert Koch, 1.2 I-20152 Milano IT
- 专利权人: PHARMACIA S.p.A.
- 当前专利权人: PHARMACIA S.p.A.
- 当前专利权人地址: Via Robert Koch, 1.2 I-20152 Milano IT
- 代理机构: Ferrario, Vittorino, et al
- 优先权: GB19940012719 19940624
- 国际公布: WO1996000226 19960104
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61K45 ; A61P35 ; C07D471 ; C07F9
摘要:
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.
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