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    1H-FURO[3,2-C]PYRAZOLE COMPOUNDS USEFUL AS KINASE INHIBITORS
    52.
    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。

    Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
    57.
    发明申请
    Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开
    作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物

    公开(公告)号：US20060135508A1

    公开(公告)日：2006-06-22

    申请号：US10522253

    申请日：2003-07-16

    申请人： Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

    发明人： Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

    IPC分类号： A61K31/55 ,  A61K31/4745 ,  C07D487/02 ,  C07D471/02

    CPC分类号： C07D487/04 ,  A61K31/415 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

    摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrrolo-pyrazole or pyrazolo-azepine. The invention also provides specific pyrrolo-pyrazoles and pyrazolo-azepines, useful intermediates, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.

    摘要翻译： 本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡咯并吡唑或吡唑并氮。 本发明还提供特定的吡咯并吡唑和吡唑并氮杂，有用的中间体，包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由和/或 与改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫疾病和神经变性疾病有关。

    Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
    59.
    发明申请
    Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开
    作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物

    公开(公告)号：US20060100233A1

    公开(公告)日：2006-05-11

    申请号：US10522254

    申请日：2003-07-01

    申请人： Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

    发明人： Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrazole-tetrahydro pyridine derivative. The invention also provides specific pyrazole-tetrahydro pyridines, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.

    摘要翻译： 本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡唑 - 四氢吡啶衍生物。 本发明还提供特异性的吡唑 - 四氢吡啶，其中包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由改变的蛋白激酶引起的和/或与其相关的疾病 活动如癌症，细胞增殖性疾病，病毒感染，自身免疫性疾病和神经变性疾病。

    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis
    60.
    发明授权
    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis 失效
    氨基蒽环类衍生物及其在治疗淀粉样变性中的应用

    公开(公告)号：US06268362B1

    公开(公告)日：2001-07-31

    申请号：US09622921

    申请日：2000-09-07

    申请人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    发明人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    IPC分类号： A61K315377

    CPC分类号： C07D405/06 ,  C07D211/70

    摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

    摘要翻译： 式（1）的化合物，其中R 1表示氢，羟基，式OR 7的基团，其中R 7是C 1 -C 6烷基，C 2 -C 6烯基; R2代表氢，羟基，二乙基氨基，哌啶子基，四氢吡啶基或吗啉代，独立的R 3独立地代表氢或羟基，独立地，R 4和R 5独立地表示氢，羟基或与碳原子一起代表 羰基; 或R 3和R 4一起表示式（A）的基团，其中R 8和R 9表示C 1 -C 6烷基，R 5表示氢; R6代表氢或任选被甲基，甲氧基或卤素取代的苯基及其药物上可接受的盐，可用于治疗淀粉样变性。 还描述了制备方法和药物组合物。