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    Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents
    7.
    发明授权
    Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents 失效
    用作抗血管生成剂的生物活性3-取代羟吲哚衍生物

    公开(公告)号：US5576330A

    公开(公告)日：1996-11-19

    申请号：US354215

    申请日：1994-12-12

    申请人： Franco Buzzetti ,  Antonio Longo ,  Maria G. Brasca ,  Fabrizio Orzi ,  Angelo Crugnola ,  Dario Ballinari ,  Mariangela Mariani

    发明人： Franco Buzzetti ,  Antonio Longo ,  Maria G. Brasca ,  Fabrizio Orzi ,  Angelo Crugnola ,  Dario Ballinari ,  Mariangela Mariani

    IPC分类号： C07D401/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/475 ,  A61K31/505 ,  A61K31/675 ,  A61K31/70 ,  A61K38/04 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  C07D209/34 ,  A61K31/015

    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

    摘要： The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 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 OR.sub.1, R.sub.2 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 R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl and R.sub.3, R.sub.4 and R.sub.5 are hydrogen; whereas when Y is indole, then R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro or --NHR, in which R is as defined above, R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, carboxy, nitro or --NHR, wherein R is as defined above, and R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;as anti-angiogenic agent is disclosed.

    摘要翻译： 式（I）化合物（I）的新用途其中Y是选自萘，四氢化萘，喹啉，异喹啉和吲哚的双环; n为0或1〜3的整数， R1是氢，C1-C6烷基或C2-C6烷酰基; R2是氢，卤素，C1-C6烷基，氰基，羧基，硝基或NHR，其中R是氢或C1-C6烷基; R3是氢或C1-C6烷基; R 4是氢，羟基，C 1 -C 6烷氧基，C 2 -C 6烷酰氧基，羧基，硝基或NHR，其中R如上定义; R5是氢，C1-C6烷基或卤素; 或其药学上可接受的盐; 当Y为萘时，n为0或1〜3的整数，Y为四氢化萘，喹啉，异喹啉或吲哚时，n为0,1或2。 并且其中当双环Y为萘，喹啉，异喹啉或吲哚时，则所述取代基OR 1，R 2和羟吲哚基中的每一个可以独立地表示在所述二环的芳基或杂芳基部分上，而只有苯部分被取代， Y是四氢化萘; 其中当Y为萘，四氢化萘，喹啉或异喹啉时，则R2为氢，卤素，氰基或C1-C6烷基，R3，R4和R5为氢; 而当Y为吲哚时，R 2为氢，卤素，C 1 -C 6烷基，氰基，羧基，硝基或-NHR，其中R如上定义，R 3为氢或C 1 -C 6烷基，R 4为氢，羟基， C 1 -C 6烷氧基，C 1 -C 6烷酰氧基，羧基，硝基或-NHR，其中R如上所定义，R 5是氢，卤素或C 1 -C 6烷基; 作为抗血管生成剂被公开。