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. |
申请人 |
NERVIANO MEDICAL SCIENCES S.R.L.;FANCELLI, DANIELE;ISACCHI, ANTONELLA;MODUGNO, MICHELE;MOLL, JURGEN;RUSCONI, LUISA;SONCINI, CHIARA;LUPI, ROSITA |
发明人 |
FANCELLI, DANIELE;ISACCHI, ANTONELLA;MODUGNO, MICHELE;MOLL, JURGEN;RUSCONI, LUISA;SONCINI, CHIARA;LUPI, ROSITA |