公开(公告)号：US09284298B2

公开(公告)日：2016-03-15

申请号：US14110596

申请日：2012-04-03

申请人： Francesco Casuscelli ,  Maria Gabriella Brasca ,  Marina Caldarelli ,  Giovanni Cervi ,  Teresa Disingrini ,  Francesca Quartieri

发明人： Francesco Casuscelli ,  Maria Gabriella Brasca ,  Marina Caldarelli ,  Giovanni Cervi ,  Teresa Disingrini ,  Francesca Quartieri

IPC分类号： A61K45/06 ,  A61K31/506 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D403/04 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.

摘要翻译： 本发明涉及调节蛋白激酶活性的吡唑基 - 嘧啶衍生物，因此可用于治疗由失调的蛋白激酶活性引起的疾病。 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，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。

公开(公告)号：US20140051708A1

公开(公告)日：2014-02-20

申请号：US14110596

申请日：2012-04-03

申请人： Francesco Casuscelli ,  Maria Gabriella Brasca ,  Marina Caldarelli ,  Giovanni Cervi ,  Teresa Disingrini ,  Francesca Quartieri

发明人： Francesco Casuscelli ,  Maria Gabriella Brasca ,  Marina Caldarelli ,  Giovanni Cervi ,  Teresa Disingrini ,  Francesca Quartieri

IPC分类号： C07D403/04 ,  A61K45/06 ,  C07D401/14 ,  A61K31/506

CPC分类号： C07D403/04 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

摘要： The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.

摘要翻译： 本发明涉及调节蛋白激酶活性的吡唑基 - 嘧啶衍生物，因此可用于治疗由失调的蛋白激酶活性引起的疾病。 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，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物。

公开(公告)号：US08981092B2

公开(公告)日：2015-03-17

申请号：US13747859

申请日：2013-01-23

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

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

IPC分类号： C07D241/38 ,  A61K31/4985 ,  C07D487/04 ,  A61K45/06

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, 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。 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。

公开(公告)号：US08394802B2

公开(公告)日：2013-03-12

申请号：US13119849

申请日：2009-09-17

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

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

IPC分类号： A61K31/495

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20110251179A1

公开(公告)日：2011-10-13

申请号：US13119849

申请日：2009-09-17

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

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

IPC分类号： A61K31/4985 ,  C40B40/04 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61P35/02 ,  C12N9/99 ,  A61P35/00 ,  A61P31/12 ,  A61P31/18 ,  A61P37/06 ,  A61P25/28 ,  C07D487/04 ,  A61K31/551

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, 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。 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。

公开(公告)号：US20130137696A1

公开(公告)日：2013-05-30

申请号：US13747859

申请日：2013-01-23

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

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

IPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

CPC分类号： A61K31/4985 ,  A61K45/06 ,  C07D487/04

摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, 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。 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。

公开(公告)号：US08946250B2

公开(公告)日：2015-02-03

申请号：US13970854

申请日：2013-08-20

申请人： Maurizio Pulici ,  Fabio Zuccotto ,  Gabriella Traquandi ,  Sonia Biondaro ,  Paolo Trifiro′ ,  Alessandra Badari ,  Stefano Nuvoloni ,  Giovanni Cervi ,  Chiara Marchionni ,  Michele Modugno

发明人： Maurizio Pulici ,  Fabio Zuccotto ,  Gabriella Traquandi ,  Sonia Biondaro ,  Paolo Trifiro′ ,  Alessandra Badari ,  Stefano Nuvoloni ,  Giovanni Cervi ,  Chiara Marchionni ,  Michele Modugno

IPC分类号： A01N43/54 ,  A61K31/505 ,  A01N43/40 ,  A61K31/44 ,  C07D239/02 ,  C07D401/00 ,  C07D401/04 ,  C07D403/04 ,  C07D407/14 ,  C07D409/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/635 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D513/14

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/635 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D513/14

摘要： 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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, like cancer.

摘要翻译： 公开了说明书中定义的式（I）的3,4-二芳基吡唑衍生物及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; 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相关的疾病，如癌症。

公开(公告)号：US20140005150A1

公开(公告)日：2014-01-02

申请号：US13970854

申请日：2013-08-20

申请人： Maurizio Pulici ,  Fabio Zuccotto ,  Gabriella Traquandi ,  Sonia Biondaro ,  Paolo Trifiro' ,  Alessandra Badari ,  Stefano Nuvoloni ,  Giovanni Cervi ,  Chiara Marchionni ,  Michele Modugno

发明人： Maurizio Pulici ,  Fabio Zuccotto ,  Gabriella Traquandi ,  Sonia Biondaro ,  Paolo Trifiro' ,  Alessandra Badari ,  Stefano Nuvoloni ,  Giovanni Cervi ,  Chiara Marchionni ,  Michele Modugno

IPC分类号： C07D401/04 ,  A61K45/06 ,  C07D405/14 ,  C07D413/14 ,  A61K31/635 ,  C07D409/14 ,  C07D401/14 ,  A61K31/444 ,  A61K31/4545 ,  C07D403/04 ,  A61K31/506 ,  A61K31/4439 ,  C07D513/14

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/635 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D513/14

摘要： 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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, like cancer.

摘要翻译： 公开了说明书中定义的式（I）的3,4-二芳基吡唑衍生物及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; 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相关的疾病，如癌症。

公开(公告)号：US20120157454A1

公开(公告)日：2012-06-21

申请号：US13320969

申请日：2010-05-19

申请人： Gianluca Mariano Enrico Papeo ,  Jay Aaron Bertrand ,  Giovanni Cervi ,  Barbara Forte ,  Rosita Lupi ,  Alessia Montagnoli ,  Alessandra Scolaro ,  Fabio Zuccotto ,  Paolo Orsini ,  Helena Posteri

发明人： Gianluca Mariano Enrico Papeo ,  Jay Aaron Bertrand ,  Giovanni Cervi ,  Barbara Forte ,  Rosita Lupi ,  Alessia Montagnoli ,  Alessandra Scolaro ,  Fabio Zuccotto ,  Paolo Orsini ,  Helena Posteri

IPC分类号： A61K31/472 ,  A61K31/4725 ,  C07D413/12 ,  A61K31/5377 ,  G01N21/64 ,  A61P35/00 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  C07D217/24 ,  C07D401/12

CPC分类号： C07D217/24 ,  C07D221/18 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  Y10T436/145555

摘要： There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. 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. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.

摘要翻译： 提供了选择性地抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的取代的异喹啉-1（2H） - 酮衍生物。 因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。 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。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。

公开(公告)号：US20060264493A1

公开(公告)日：2006-11-23

申请号：US10545768

申请日：2004-02-03

申请人： Ermes Vanotti ,  Giovanni Cervi ,  Maurizio Pulici ,  Maria Menichincheri ,  Mario Varasi ,  Paola Vianello

发明人： Ermes Vanotti ,  Giovanni Cervi ,  Maurizio Pulici ,  Maria Menichincheri ,  Mario Varasi ,  Paola Vianello

IPC分类号： A61K31/4162 ,  C07D487/02

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K45/06 ,  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 tetracyclic pyrazole. The invention also provides specific tetracyclic pyrazole derivatives, 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，该方法包括向有需要的哺乳动物施用有效量的四环吡唑。 本发明还提供具体的四环吡唑衍生物，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，其可用于治疗由改变的和/或与之相关的疾病 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。