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    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
    1.
    发明授权
    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法

    公开(公告)号：US08592583B2

    公开(公告)日：2013-11-26

    申请号：US13505357

    申请日：2010-10-27

    Applicant: Matteo D'Anello ,  Marco Re

    Inventor： Matteo D'Anello ,  Marco Re

    IPC: C07D401/00

    CPC classification number: C07D403/04 ,  C07D207/34

    Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

    3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases
    2.
    发明授权
    3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases 有权
    3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮衍生物，用于调节蛋白激酶的活性

    公开(公告)号：US08394802B2

    公开(公告)日：2013-03-12

    申请号：US13119849

    申请日：2009-09-17

    Applicant: Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

    Inventor： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

    IPC: A61K31/495

    CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D487/04

    Abstract: Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds with the formula 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.

    Abstract translation: 具有下式或其药学上可接受的盐的3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物，其制备方法和包含它们的药物组合物是 披露; 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。

    3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
    6.
    发明授权
    3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 有权
    作为激酶抑制剂活性的3,4-二氢-2H-吡嗪并[1,2-A]吲哚-1-酮衍生物，其制备方法和包含它们的药物组合物

    公开(公告)号：US08513241B2

    公开(公告)日：2013-08-20

    申请号：US13482626

    申请日：2012-05-29

    Applicant: Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Barbara Salom

    Inventor： Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Barbara Salom

    IPC: A61K31/5355 ,  A61K31/501 ,  C07D413/14 ,  C07D241/04

    CPC classification number: C07D487/04

    Abstract: Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one 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.

    Abstract translation: 公开了3,4-二氢-2H-吡嗪并[1,2-a]吲哚-1-酮衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物的化合物。 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。

    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-羧酸的方法

    公开(公告)号：US20120220771A1

    公开(公告)日：2012-08-30

    申请号：US13505357

    申请日：2010-10-27

    Applicant: Matteo D'Anello ,  Marco Re

    Inventor： Matteo D'Anello ,  Marco Re

    IPC: C07D403/04 ,  C07D207/34

    CPC classification number: C07D403/04 ,  C07D207/34

    Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

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