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1.发明公开
公开(公告)号：EP2004180A2
公开(公告)日：2008-12-24
申请号：EP07727513.9
申请日：2007-03-29
发明人： FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
IPC分类号： A61K31/4162 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/454 , A61K31/496 , A61K31/5377
摘要： The invention provides low molecular weight compounds, namely tetrahydropyrrolo[3,4-c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor-resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
摘要翻译： 本发明提供低分子量化合物，即四氢吡咯并[3,4-c]吡唑，其显示出对ABL酪氨酸激酶的ATP袋的高亲和力。 因此，这些化合物也是ATP竞争性酪氨酸激酶抑制剂，并且特别是对BCR-ABL抑制剂抗性T315I ABL突变体显示出显着的抑制效力。 本发明的化合物可用于治疗抗BCR-ABL抑制剂的ABL介导的疾病，例如耐伊马替尼的慢性粒细胞性白血病。 此外，本发明提供了用于鉴定能够结合激酶蛋白质的ATP袋，特别是T315I突变体ABL激酶的化合物的筛选方法。
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2.发明公开
公开(公告)号：EP2007380A2
公开(公告)日：2008-12-31
申请号：EP07727485.0
申请日：2007-03-29
发明人： FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
IPC分类号： A61K31/4162 , A61K31/44 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/44
摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3- c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor- resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
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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：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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5.发明授权
公开(公告)号：EP2007380B1
公开(公告)日：2011-09-14
申请号：EP07727485.0
申请日：2007-03-29
发明人： FANCELLI, Daniele , ISACCHI, Antonella , MODUGNO, Michele , MOLL, Jurgen , RUSCONI, Luisa , SONCINI, Chiara , LUPI, Rosita
IPC分类号： A61K31/4162 , A61K31/44 , A61P35/02
CPC分类号： A61K31/4162 , A61K31/44
摘要： The invention provides low molecular weight compounds, namely 1H-thieno[2,3- c]pyrazoles, showing a high affinity for the ATP pocket of ABL tyrosine kinase. These compounds are thus ATP-competitive tyrosine kinase inhibitors displaying a significant inhibitory potency also, and in particular, towards BCR-ABL inhibitor- resistant T315I ABL mutants. The compounds of the invention find a useful application in the treatment of BCR-ABL inhibitor-resistant ABL-mediated diseases, such as Imatinib-resistant chronic myelogenous leukemia. Moreover, the invention provides a screening method for the identification of compounds capable of binding the ATP pocket of a kinase protein, in particular of the T315I mutant ABL kinase.
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