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    SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
    2.
    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
    3.
    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
    4.
    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.

    BIOLOGICALLY ACTIVE 3-SUBSTITUTED OXINDOLE DERIVATIVES USEFUL AS ANTI-ANGIOGENIC AGENTS
    7.
    发明公开
    BIOLOGICALLY ACTIVE 3-SUBSTITUTED OXINDOLE DERIVATIVES USEFUL AS ANTI-ANGIOGENIC AGENTS 失效
    生物活性3-取代羟吲哚类USED AS抗血管生成活性。

    公开(公告)号：EP0684820A1

    公开(公告)日：1995-12-06

    申请号：EP94931583.0

    申请日：1994-11-08

    申请人： PHARMACIA S.p.A.

    发明人： BUZZETTI, Franco ,  LONGO, Antonio ,  BRASCA, Maria Gabriella ,  ORZI, Fabrizio ,  CRUGNOLA, Angelo ,  BALLINARI, Dario ,  MARIANI, Mariangela

    IPC分类号： C07D401 ,  A61K31 ,  A61K38 ,  A61P27 ,  A61P29 ,  A61P35 ,  C07D209

    CPC分类号： A61K31/70 ,  A61K31/40 ,  A61K31/47 ,  A61K31/475 ,  A61K31/505 ,  A61K31/675 ,  A61K38/04 ,  Y10S514/825 ,  Y10S514/863 ,  Y10S514/866 ,  Y10S514/886 ,  Y10S514/908 ,  A61K2300/00

    摘要： The new use of a compound of formula (I) wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole; n is zero or an integer of 1 to 3; R1 is hydrogen, C1-C6 alkyl or C2-C6 alkanoyl; R2 is hydrogen, halogen, C1-C6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R4 is hydrogen, hydroxy, C1-C6 alkoxy, C2-C6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above; R5 is hydrogen, C1-C6 alkyl or halogen; or a pharmaceutically acceptable salt thereof; and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR1, R2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin; and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R2 is hydrogen, halogen, cyano or C1-C6 alkyl and R3, R4 and R5 are hydrogen; whereas when Y is indole, then R2 is hydrogen, halogen, C1-C6 alkyl, cyano, carboxy, nitro or -NHR, in which R is as defined above, R3 is hydrogen or C1-C6 alkyl, R4 is hydrogen, hydroxy, C1-C6 alkoxy, C2-C6 alkanoyloxy, carboxy, nitro or -NHR, wherein R is as defined above, and R5 is hydrogen, halogen or C1-C6 alkyl; as anti-angiogenic agent is disclosed.