Use of a kinase inhibitor for the treatment of particular...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S407000

Reexamination Certificate

active

08084455

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.

REFERENCES:
patent: WO 2005/005427 (2005-01-01), None
Carter T.A. et al., “Inhibition of Drug-Resistant Mutants of ABL, KIT, and EGF Receptor Kinases”,Proceedings of the National Academy of Sciences 102(31):11011-11016 (2005), XP-002440841.
Gumireddy K. et al., “A Non-ATP-Competitive Inhibitor of BCR-ABL Overrides Imatinib Resistance”,Proceedings of the National Academy of Sciences 102(6):1992-1997 (2005), XP-002405719.

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