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公开(公告)号：EP2324008B1
公开(公告)日：2012-05-09
申请号：EP09780990.9
申请日：2009-07-23
发明人： PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
IPC分类号： C07D401/04 , C07D403/04 , C07D407/14 , C07D409/14 , A61K31/4439 , A61P35/00
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.
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2.发明公开3,4-DIHYDRO-2H-PYRAZINOÝ1,2-A¨INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权3,4-二氢-2H-吡嗪并[1,2-a]吲哚-1-酮衍生物作为激酶抑制剂，其制备方法和药物制剂
公开(公告)号：EP2254886A2
公开(公告)日：2010-12-01
申请号：EP09724061.8
申请日：2009-03-27
IPC分类号： C07D405/12 , C07D417/12 , A01N43/40 , A01N43/78
CPC分类号： C07D487/04
摘要： 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 ofdiseases 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.
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公开(公告)号：EP2702055A1
公开(公告)日：2014-03-05
申请号：EP12717627.9
申请日：2012-04-03
发明人： CASUSCELLI, Francesco , BRASCA, Maria Gabriella , CALDARELLI, Marina , CERVI, Giovanni , DISINGRINI, Teresa , QUARTIERI, Francesca
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P37/00 , A61P31/12
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.
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公开(公告)号：EP4217354A1
公开(公告)日：2023-08-02
申请号：EP21773829.3
申请日：2021-09-15
发明人： BINDI, Simona , BUFFA, Laura , CERVI, Giovanni , D ALESSIO, Roberto , MENICHINCHERI, Maria , MODUGNO, Michele
IPC分类号： C07D403/04 , C07D403/14 , A61P35/00 , A61K31/415 , A61K31/506
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5.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3,4-二氢-2H-吡嗪并[1,2-a]吲哚-1-酮衍生物作为激酶抑制剂，其制备方法和药物制剂
公开(公告)号：EP2254886B1
公开(公告)日：2016-05-25
申请号：EP09724061.8
申请日：2009-03-27
IPC分类号： C07D405/12 , C07D417/12 , A01N43/40 , A01N43/78
CPC分类号： C07D487/04
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公开(公告)号：EP2376492A1
公开(公告)日：2011-10-19
申请号：EP09783126.7
申请日：2009-09-17
发明人： MIRIZZI, Danilo , CERVI, Giovanni , D'ANELLO, Matteo , PAPEO, Gianluca Mariano Enrico , FERGUSON, Ron , CASUSCELLI, Francesco
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： A61K31/4985 , A61K45/06 , C07D487/04
摘要： Compounds which are 4,7-disubstituted derivatives of3,4-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.
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公开(公告)号：EP2432765B1
公开(公告)日：2016-03-02
申请号：EP10723046.8
申请日：2010-05-19
发明人： PAPEO, Gianluca Mariano Enrico , BERTRAND, Jay Aaron , CERVI, Giovanni , FORTE, Barbara , LUPI, Rosita , MONTAGNOLI, Alessia , SCOLARO, Alessandra , ZUCCOTTO, Fabio , ORSINI, Paolo , POSTERI, Helena
IPC分类号： C07D217/24 , C07D401/04 , A61K31/472 , A61K31/4725 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D217/24 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , Y10T436/145555
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公开(公告)号：EP2376492B1
公开(公告)日：2015-04-08
申请号：EP09783126.7
申请日：2009-09-17
发明人： MIRIZZI, Danilo , CERVI, Giovanni , D'ANELLO, Matteo , PAPEO, Gianluca Mariano Enrico , FERGUSON, Ron , CASUSCELLI, Francesco
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： A61K31/4985 , A61K45/06 , C07D487/04
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公开(公告)号：EP2432765A1
公开(公告)日：2012-03-28
申请号：EP10723046.8
申请日：2010-05-19
发明人： PAPEO, Gianluca Mariano Enrico , BERTRAND, Jay Aaron , CERVI, Giovanni , FORTE, Barbara , LUPI, Rosita , MONTAGNOLI, Alessia , SCOLARO, Alessandra , ZUCCOTTO, Fabio , ORSINI, Paolo , POSTERI, Helena
IPC分类号： C07D217/24 , C07D401/04 , A61K31/472 , A61K31/4725 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00
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.
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公开(公告)号：EP2324008A1
公开(公告)日：2011-05-25
申请号：EP09780990.9
申请日：2009-07-23
发明人： PULICI, Maurizio , ZUCCOTTO, Fabio , BADARI, Alessandra , NUVOLONI, Stefano , CERVI, Giovanni , TRAQUANDI, Gabriella , BIONDARO, Sonia , TRIFIRO', Paolo , MARCHIONNI, Chiara , MODUGNO, Michele
IPC分类号： C07D401/04 , C07D403/04 , C07D407/14 , C07D409/14 , A61K31/4439 , A61P35/00
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.
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