2-pyrimidineamine derivatives and processes for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/505 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2269095

Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group -X1- R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.

L'invention concerne des composés représentés par la formule générale (1), dans laquelle Ar est un groupe aromatique facultativement substitué; R<2> est un atome d'hydrogène ou d'halogène ou un groupe -X<1>-R<2a> dans lequel X<1> est une liaison directe ou un atome ou un groupe lieurs et R<2a> est un groupe alkyle, alcényle ou alkynyle à chaîne droite ou ramifiée facultativement substitué; R<3> est un groupe hétérocycloalkyle facultativement substitué, l'invention concernant également les sels, les solvates, les hydrates et les N-oxydes desdits composés. Lesdits composés sont des inhibiteurs sélectifs de tyrosine-kinase, en particuliers des kinases ZAP-70 et syk, et sont utilisés dans le traitement préventif et curatif de maladies immunitaires ou allergiques et de maladies entraînant une mauvaise activation plaquettaire.

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