The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Dec. 27, 2011
Filed:
Mar. 29, 2007
Daniele Fancelli, Milan, IT;
Antonella Isacchi, Milan, IT;
Michele Modugno, Cernusco sul Naviglio, IT;
Juergen Moll, Appiano Gentile, IT;
Luisa Rusconi, Milan, IT;
Chiara Soncini, Piacenza, IT;
Rosita Lupi, Milan, IT;
Daniele Fancelli, Milan, IT;
Antonella Isacchi, Milan, IT;
Michele Modugno, Cernusco sul Naviglio, IT;
Juergen Moll, Appiano Gentile, IT;
Luisa Rusconi, Milan, IT;
Chiara Soncini, Piacenza, IT;
Rosita Lupi, Milan, IT;
Nerviano Medical Sciences S.r.l., Nerviano (MI), IT;
Abstract
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.