发明名称 |
USE OF A KINASE INHIBITOR FOR THE TREATMENT OF PARTICULAR RESISTANT TUMORS |
摘要 |
<p>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.</p> |
申请公布号 |
EP2004180(A2) |
申请公布日期 |
2008.12.24 |
申请号 |
EP20070727513 |
申请日期 |
2007.03.29 |
申请人 |
NERVIANO MEDICAL SCIENCES S.R.L. |
发明人 |
FANCELLI, DANIELE;ISACCHI, ANTONELLA;MODUGNO, MICHELE;MOLL, JURGEN;RUSCONI, LUISA;SONCINI, CHIARA;LUPI, ROSITA |
分类号 |
A61K31/454;A61K31/4162;A61K31/496;A61K31/5377;A61P35/02 |
主分类号 |
A61K31/454 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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