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    SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
    1.
    发明公开
    SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION 失效
    取代AZAINDOLYLIDENDERIVATE及其制备方法

    公开(公告)号：EP0715628A1

    公开(公告)日：1996-06-12

    申请号：EP95921777.0

    申请日：1995-05-30

    申请人： PHARMACIA S.p.A.

    发明人： BUZZETTI, Franco ,  BRASCA, Gabriella, Maria ,  LONGO, Antonio ,  BALLINARI, Dario

    IPC分类号： A61K31 ,  A61K45 ,  A61P35 ,  C07D471 ,  C07F9

    CPC分类号： C07D471/04 ,  C07F9/6561

    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.

    SUBSTITUTED BETA-ARYL AND BETA-HETEROARYL-ALPHA-CYANOACRYLAMIDE DERIVATIVES AS TYROSINE KINASE INHIBITORS
    2.
    发明公开
    SUBSTITUTED BETA-ARYL AND BETA-HETEROARYL-ALPHA-CYANOACRYLAMIDE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效
    N-取代的BETA-ARYL IN BETA-HETEROARYL-ALPHA-CYAMOACRYLAMIDDERIVATE ALS TYROSINE KINASE INHIBITOREN

    公开(公告)号：EP0700388A1

    公开(公告)日：1996-03-13

    申请号：EP95910542.0

    申请日：1995-03-02

    申请人： PHARMACIA S.p.A.

    发明人： BUZZETTI, Franco ,  CRUGNOLA, Angelo ,  LONGO, Antonio ,  BRASCA, Gabriella, Maria ,  BALLINARI, Dario

    IPC分类号： A61K31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07C255 ,  C07D209 ,  C07D213 ,  C07D215 ,  C07D217 ,  C07D401

    CPC分类号： C07D401/12 ,  C07C255/41 ,  C07C2602/10 ,  C07D209/12 ,  C07D209/18 ,  C07D215/12 ,  C07D215/26 ,  C07D217/14 ,  C07D217/16

    摘要： The present invention relates to new compounds of formula (I), wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole; B is an R2 substituted benzene ring or an unsubstituted pyridine or thiphene ring; R is hydrogen, C¿1?-C6 alkyl, halogen, nitro, cyano, carboxy or a group NR?3R4¿, wherein each of R?3 and R4¿ is independently hydrogen or C¿1?-C6 alkyl; R?1¿ is hydrogen, C¿1?-C6 alkyl or C1-C6 alkanoyl; R?2¿ is hydrogen, C¿1?-C6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C1-C6 alkoxy, C1-C6 alkanoyloxy or a group NR?3R4¿, wherein R?3 and R4¿ are as defined above; n is zero or an integer of 1 to 2; x is zero or an integer of 1 to 5; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful as tyrosine kinase inhibitors.

    摘要翻译： PCT No.PCT / EP95 / 00758 Sec。 371日期：1995年11月21日 102（e）1995年11月21日日期PCT 1995年3月2日PCT公布。 WO95 / 26341 PCT出版物 日期：1995年10月5日本发明涉及新的式（I）化合物，其中A是选自萘，四氢萘，喹啉，异喹啉和吲哚的双环。 B是R2取代的苯环或未取代的吡啶或噻吩环; R是氢，C 1 -C 6烷基，卤素，硝基，氰基，羧基或NR 3 R 4基团，其中R 3和R 4各自独立地是氢或C 1 -C 6烷基; R1是氢，C1-C6烷基或C1-C6烷酰基; R 2是氢，C 1 -C 6烷基，卤素，硝基，氰基，羧基，羟基，C 1 -C 6烷氧基，C 1 -C 6烷酰氧基或NR 3 R 4基团，其中R 3和R 4如上定义; n为0或1〜2的整数; x为0或1〜5的整数; 及其药学上可接受的盐。 本发明的化合物可用作酪氨酸激酶抑制剂。

    SUBSTITUTED 3-ARYLIDENE-7-AZAOXINDOLE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
    3.
    发明公开
    SUBSTITUTED 3-ARYLIDENE-7-AZAOXINDOLE COMPOUNDS AND PROCESS FOR THEIR PREPARATION 失效
    取代的3- ARYLIDINENE-7氮杂吲哚化合物和工艺及其

    公开(公告)号：EP0741726A1

    公开(公告)日：1996-11-13

    申请号：EP95937030.0

    申请日：1995-10-30

    申请人： Pharmacia S.p.A.

    发明人： BUZZETTI, Franco ,  BRASCA, Gabriella, Maria ,  LONGO, Antonio ,  BALLINARI, Dario

    IPC分类号： A61K31 ,  A61P9 ,  A61P35 ,  A61P43 ,  C07D471 ,  C07D519

    CPC分类号： C07D471/04

    摘要： The present invention relates to compound of formula (I) wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole; R1 is -H, -CN, -SO3R4, -SO2NHR5, (i), -COOR6, -CONHCH2(CHOH)nCH2OH, (ii), -NR7R8, -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NH-C(NH2)=NH, -NHCO(CH)OH)nCH2OH, (iii), -NHSO2R9, -OR10, -OCH2(CHOH)nCH2OH, -OOC(CHOH)nCH2OH, -OPO(OH)2, -CH2NH2, -C(NH2)=NH, -CH2NHC(NH2)=NH, (iv), -CH2OH, -CH2OOC(CHOH)nCH2OH, -CH2OPO(OH)2 or -PO(OH)2; R2 is C1-C6 alkyl, halogen, or hydroxy; R3 is -H or C1-C6 alkyl; R4 is -H, C1-C6 alkyl or -CH2(CHOH)nCH2OH; R5 is -H, C1-C6 alkyl, -CH2(CHOH)nCH2OH or -(CH2)mNMe2; R6 is -H, C1-C6 alkyl or -CH2(CHOH)nCH2OH; each of R7 and R8 independently is -H or C1-C6 alkyl; R9 is methyl or tolyl; R10 is -H, C1-C6 alkyl or C2-C6 alkanoyl; Z is ⊃CH2, ⊃0, ⊃NH or ⊃NCH2CH2OH; n is zero or 1; m is 2 or 3; p is 1, 2 or 3; q is zero, 1 or 2; and the pharmaceutically acceptable salt thereof, for use as tyrosine kinase inhibitors.