Use of pyrazolo ¢3,4-b! pyridine as cyclin dependent kinase...

Details Use of pyrazolo ¢3,4-b! pyridine as cyclin dependent kinase... Use of pyrazolo ¢3,4-b! pyridine as cyclin dependent kinase...

A - Human Necessities

61

K

A61K 31/44 (2006.01) A61K 31/437 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2314355

Compounds of formula (I) and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein: X is O, S(O)m; Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl; R1 is hydrogen or lower alkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocloalkylalkyl, -O-alkyl, -O-aryl, - NR4R5; R3 is hydrogen or lower alkyl; R4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -O-alkyl, -O-aryl; R5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, -O-alkyl, -O-aryl; and m is 0, 1 or 2. The compounds of formula (I) are proteinkinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.

L'invention concerne des composés de formule (I), ainsi que des sels pharmaceutiquement acceptables de ceux-ci, destinés à être utilisés en tant qu'inhibiteurs de kinase dépendant de la cycline. Dans cette formule: X représente O, S(O)¿m?; Y représentant alkyle, aryle, arylalkyle, hétéroaryle, hétéroarylalkyle, cycloalkyle, cycloalkylalkyle, hétérocycloalkyle, hétérocycloalkylalkyle; R¿1? représente hydrogène ou alkyle inférieur; R¿2? représente alkyle, aryle, arylalkyle, hétéroaryle, hétéroarylalkyle, cycloalkyle, cycloalkylalkyle, hétérocycloalkyle, hétérocycloalkylalkyle, -O-alkyle, -O-aryle, -NR¿4?R¿5?; R¿3? représente hydrogène ou alkyle inférieur; R¿4? représente hydrogène, alkyle, aryle, arylalkyle, hétéroaryle, hétéroarylalkyle, cycloalkyle, cycloalkylalkyle, hétérocycloalkyle, hétérocycloalkylalkyle, -O-alkyle, -O-aryle; R¿5? représente hydrogène, alkyle, aryle, alkylaryle, hétéroaryle, alkylhétéroaryle, cycloalkyle, alkylcycloalkyle, hétérocycloalkyle, alkylhétérocycloalkyle, -O-alkyle, -O-aryle; et m est égal à 0, 1, ou 2. Ces composés de formule I constituent des inhibiteurs de la protéine kinase et sont utiles au traitement et à la prévention de maladies prolifératives, par exemple le cancer, les inflammations, et l'arthrite. Ces composés peuvent en outre être utiles au traitement des maladies neurodégénératives telles que la maladie d'Alzheimer et les maladies cardiovasculaires, virales et fongiques.

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