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    Arylidene-heterocyclic derivatives and process for their preparation
    1.
    发明授权
    Arylidene-heterocyclic derivatives and process for their preparation 失效
    亚芳基杂环衍生物及其制备方法

    公开(公告)号：US5587385A

    公开(公告)日：1996-12-24

    申请号：US452288

    申请日：1995-05-26

    申请人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria G. Brasca ,  Sergio Penco

    发明人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria G. Brasca ,  Sergio Penco

    IPC分类号： C07D217/24 ,  C07D275/06 ,  C07D401/06 ,  C07D417/06 ,  A61K31/47 ,  A61K31/475 ,  C07D401/08

    CPC分类号： C07D275/06 ,  C07D217/24 ,  C07D401/06 ,  C07D417/06

    摘要： The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

    摘要翻译： 本发明涉及式（I）的化合物，其中Ar是选自苯，萘，四氢萘，喹啉和吲哚的单环或双环体系; Het是R 3是氢或C 1 -C 6烷基的氢，卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3; R 1是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如上所定义; R2是氢，卤素，羟基或C1-C6烷基; 并且其中当同时（Ar）R 1 R 2基团表示未取代的苯基或4-氯 - ，4-氰基 - ，4-氨基 - 或3,4-二甲氧基 - 苯基且Het为 4-高邻苯二甲酰亚胺基，则R不是氢，其可用作抗增殖剂。

    3-aryl-glycidic ester derivatives
    2.
    发明授权
    3-aryl-glycidic ester derivatives 失效
    3-芳基 - 缩水甘油酯衍生物

    公开(公告)号：US5436235A

    公开(公告)日：1995-07-25

    申请号：US16980

    申请日：1993-02-12

    申请人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    发明人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    IPC分类号： A61K31/335 ,  A61K31/336 ,  A61K31/40 ,  A61K31/47 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07D303/48 ,  C07D405/04 ,  C07D27/56

    CPC分类号： C07D405/04 ,  C07D303/48

    摘要： The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.

    摘要翻译： 本发明涉及式为“IMAGE”的3-芳基 - 环氧乙烷衍生物，其中Ar为4'-喹啉或5'-喹啉; R和R 1各自独立地是氢或C 1 -C 6烷氧基; X和Y中的一个是氢，氰基，-COOR 2或-CONR 3 R 4，X和Y中的另一个是氰基，-COOR 2或-CONR 3 R 4，其中R 2是C 1 -C 6烷基，R 3和R 4各自独立地是氢或C 1 -C6烷基和其药学上可接受的盐，其可用于治疗作为酪氨酸激酶抑制剂，特别是作为抗增殖剂（通常作为抗癌剂）用于治疗牛皮癣和抑制动脉粥样硬化斑块发展。

    Arylidene-heterocyclic derivatives and process for their preparation
    3.
    发明授权
    Arylidene-heterocyclic derivatives and process for their preparation 失效
    亚芳基杂环衍生物及其制备方法

    公开(公告)号：US5639884A

    公开(公告)日：1997-06-17

    申请号：US400113

    申请日：1995-03-06

    申请人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria Gabriella Brasca ,  Sergio Penco

    发明人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria Gabriella Brasca ,  Sergio Penco

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00 ,  A61P43/00 ,  C07D217/24 ,  C07D275/06 ,  C07D401/06 ,  C07D417/06 ,  C12N9/99

    CPC分类号： C07D275/06 ,  C07D217/24 ,  C07D401/06 ,  C07D417/06

    摘要： The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar)R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

    摘要翻译： 本发明涉及式（I）的化合物，其中Ar是选自苯，萘，四氢萘，喹啉和吲哚的单环或双环体系; Het是R 1是氢或C 1 -C 6烷基的氢，卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3; R 1是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如上所定义; R2是氢，卤素，羟基或C1-C6烷基; 其中当（Ar）R 1 R 2基团同时表示未取代的苯基或4-氯 - ，4-氰基 - ，4-氨基 - 或3,4-二甲氧基 - 苯基且Het为 4-高邻苯二甲酰亚胺基，则R不是氢，它们可用作抗增殖剂。