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6 条记录 (耗时 0.045 秒)

    Pyrazolo-quinazolines
    3.
    发明授权
    Pyrazolo-quinazolines 有权
    吡唑并喹唑啉

    公开(公告)号：US08846701B2

    公开(公告)日：2014-09-30

    申请号：US13001331

    申请日：2009-06-17

    申请人： Marina Caldarelli ,  Mauro Angiolini ,  Riccardo Colombo ,  Teresa Disingrini ,  Stefano Nuvoloni ,  Helena Posteri ,  Matteo Salsa ,  Marco Silvagni

    发明人： Marina Caldarelli ,  Mauro Angiolini ,  Riccardo Colombo ,  Teresa Disingrini ,  Stefano Nuvoloni ,  Helena Posteri ,  Matteo Salsa ,  Marco Silvagni

    IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D239/70

    CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D239/70

    摘要： The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecule framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

    摘要翻译： 本发明涉及吡唑并 - 喹唑啉，其特征在于在8位上具有邻位取代的芳基氨基，杂环基氨基或C3-C7环烷基氨基残基，芳基，杂环基或C3-C7环烷基作为分子3位的羧酰胺的取代基 框架。 本发明的化合物调节蛋白激酶的活性，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是MPS1 / TTK。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。

    PYRAZOLO--QUINAZOLINES
    4.
    发明申请
    PYRAZOLO--QUINAZOLINES 有权
    PYRAZOLO - QUINAZOLINES

    公开(公告)号：US20110105542A1

    公开(公告)日：2011-05-05

    申请号：US13001331

    申请日：2009-06-17

    申请人： Marina Caldareli ,  Mauro Angiolini ,  Riccardo Colombo ,  Teresa Disingrini ,  Stefano Nuvoloni ,  Helena Posteri ,  Matteo Salsa ,  Marco Silvagni

    发明人： Marina Caldareli ,  Mauro Angiolini ,  Riccardo Colombo ,  Teresa Disingrini ,  Stefano Nuvoloni ,  Helena Posteri ,  Matteo Salsa ,  Marco Silvagni

    IPC分类号： A61K31/519 ,  C07D239/00 ,  A61P35/00

    CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D239/70

    摘要： The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

    摘要翻译： 本发明涉及吡唑并 - 喹唑啉，其特征在于在8位的邻位取代的芳基氨基，杂环基氨基或C3-C7环烷基氨基残基，作为分子3位的羧酰胺取代基的芳基，杂环基或C 3 -C 7环烷基 框架。 本发明的化合物调节蛋白激酶的活性，因此可用于治疗由失调的蛋白激酶活性引起的疾病，特别是MPS1 / TTK。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。

    Tricyclopyrazole derivatives
    5.
    发明授权
    Tricyclopyrazole derivatives 有权
    三环吡唑衍生物

    公开(公告)号：US09127015B2

    公开(公告)日：2015-09-08

    申请号：US13512904

    申请日：2010-11-24

    申请人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    发明人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    IPC分类号： A61K31/437 ,  C07D471/14 ,  C07D487/14

    CPC分类号： C07D487/14 ,  C07D207/34 ,  C07D471/14

    摘要： Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

    摘要翻译： 公开了作为三环吡唑衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

    TRICYCLOPYRAZOLE DERIVATIVES
    6.
    发明申请
    TRICYCLOPYRAZOLE DERIVATIVES 有权
    三甲基吡唑衍生物

    公开(公告)号：US20120277214A1

    公开(公告)日：2012-11-01

    申请号：US13512904

    申请日：2010-11-24

    申请人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    发明人： Teresa Disingrini ,  Sergio Mantegani ,  Mario Varasi

    IPC分类号： C07D487/14 ,  C40B40/04 ,  A61K31/55 ,  A61K31/551 ,  A61K31/437 ,  A61P25/28 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02 ,  A61P31/18 ,  A61P31/12 ,  A61P37/06 ,  C07D471/14 ,  A61K31/496

    CPC分类号： C07D487/14 ,  C07D207/34 ,  C07D471/14

    摘要： Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

    摘要翻译： 公开了作为三环吡唑衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。