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    1H-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors
    1.
    发明授权
    1H-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors 有权
    可用作激酶抑制剂的1H-噻吩并[2,3-c]吡唑化合物

    公开(公告)号：US07943654B2

    公开(公告)日：2011-05-17

    申请号：US11988528

    申请日：2006-07-10

    申请人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tizizno Bandiera

    发明人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tizizno Bandiera

    IPC分类号： A01N43/56 ,  A01N43/06 ,  A61K31/415 ,  A61K31/38 ,  C07D487/02 ,  C07D231/54 ,  C07D333/00

    CPC分类号： C07D495/04

    摘要： There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR5 is at the ortho position to the CONH linker; R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; R5 is hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

    摘要翻译： 提供式（I）的噻吩并[2,3-c]吡唑衍生物，其中A是芳基或杂芳基环，取代基-NHZR5在其上与CONH连接体的邻位; R1和R2相同或不同，彼此独立地表示氢原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; R5是氢或有机基团; 或异构体，互变异构体，载体，代谢物，前药和药物上可接受的盐。 还公开了其制备方法和包含它们的药用组合物; 本发明的化合物在治疗与失调的蛋白激酶活性相关的疾病（例如癌症）中可能是有用的。

    1H-Thieno[2,3-c]Pyrazole Compounds Useful as Kinase Inhibitors
    2.
    发明申请
    1H-Thieno[2,3-c]Pyrazole Compounds Useful as Kinase Inhibitors 有权
    可用作激酶抑制剂的1H-噻吩并[2,3-c]吡唑化合物

    公开(公告)号：US20090149457A1

    公开(公告)日：2009-06-11

    申请号：US11988528

    申请日：2006-07-10

    申请人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tiziano Bandiera

    发明人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tiziano Bandiera

    IPC分类号： A61K31/5377 ,  C07D231/54 ,  A61K31/4162 ,  C12N9/99 ,  A61P35/00 ,  A61P37/00 ,  A61P25/00 ,  C07D409/14 ,  A61K31/496 ,  C07D413/14

    CPC分类号： C07D495/04

    摘要： There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR5 is at the ortho position to the CONH linker; R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; R5 is hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

    摘要翻译： 提供式（I）的噻吩并[2,3-c]吡唑衍生物，其中A是芳基或杂芳基环，取代基-NHZR5在其上与CONH连接体的邻位; R1和R2相同或不同，彼此独立地表示氢原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C-O或-C（-O）NH-; R5是氢或有机基团; 或异构体，互变异构体，载体，代谢物，前药和药物上可接受的盐。 还公开了其制备方法和包含它们的药用组合物; 本发明的化合物在治疗与失调的蛋白激酶活性相关的疾病（例如癌症）中可能是有用的。

    1H-FURO[3,2-C]PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS
    3.
    发明申请
    1H-FURO[3,2-C]PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS 有权
    1H-FURO [3,2-C]吡唑化合物作为激酶抑制剂有用

    公开(公告)号：US20090239924A1

    公开(公告)日：2009-09-24

    申请号：US12302569

    申请日：2007-05-25

    申请人： Daniele Fancelli ,  Maurizio Pulici ,  Jurgen Moll ,  Tiziano Bandiera

    发明人： Daniele Fancelli ,  Maurizio Pulici ,  Jurgen Moll ,  Tiziano Bandiera

    IPC分类号： A61K31/4162 ,  C07D491/048 ,  A61P35/00 ,  A61P35/04

    CPC分类号： C07D491/048

    摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.

    摘要翻译： 如描述中定义的式（I）的呋喃并[3,2-c]吡唑衍生物及其药学上可接受的盐，其中A是芳基或杂芳基环，-NHZR5位于与CONH接头的邻位; -R 1和R 2相同或不同，彼此独立地表示氢原子或有机残基; R3是氢或卤素原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C-O或-C（-O）NH-; -R5是氢或任选取代的有机基团或其异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。 公开了其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性，特别是Aurora激酶活性或IGF-1R活性相关的疾病，如癌症。

    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
    4.
    发明授权
    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors 有权
    可用作激酶抑制剂的1H-呋喃并[3,2-C]吡唑化合物

    公开(公告)号：US08119641B2

    公开(公告)日：2012-02-21

    申请号：US12302569

    申请日：2007-05-25

    申请人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    发明人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    IPC分类号： A61K31/4162 ,  A61K31/427 ,  A61K31/496 ,  C07D491/048 ,  C07D277/44 ,  C07D295/135 ,  C07D417/10 ,  C07D403/14

    CPC分类号： C07D491/048

    摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.

    摘要翻译： 如描述中定义的式（I）的呋喃并[3,2-c]吡唑衍生物及其药学上可接受的盐，其中A是芳基或杂芳基环，-NHZR5位于与CONH接头的邻位; -R 1和R 2相同或不同，彼此独立地表示氢原子或有机残基; R3是氢或卤素原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; -R5是氢或任选取代的有机基团或其异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。 公开了其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性，特别是Aurora激酶活性或IGF-1R活性相关的疾病，如癌症。