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

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

A - Human Necessities

61

K

A61K 31/4162 (2006.01) A61P 35/02 (2006.01)

Patent

CA 2647186

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.

La présente invention concerne des composés de faible poids moléculaire, à savoir des tétrahydropyrrolo[3,4-c]pyrazoles, présentant une grande affinité pour une poche ATP de la tyrosine kinase ABL. Ces composés sont donc des inhibiteurs de la tyrosine kinase "ATP-compétitifs" qui présentent également une puissance inhibitrice considérable, notamment vis-à-vis des mutants T315I ABL résistant à un inhibiteur BCR-ABL. Les composés selon l'invention sont très utiles pour traiter des maladies à médiation ABL résistant à un inhibiteur BCR-ABL, telles qu'une leucémie myélogène chronique résistant à Imatinib. De plus, cette invention a pour objet une méthode de criblage servant à identifier des composés capables de se lier à la poche ATP d'une protéine kinase, plus spécifiquement la kinase ABL du mutant T315I.

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