Quinazolines and their use for inhibiting cyclin-dependent...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/84 (2006.01) A61K 31/517 (2006.01) C07D 239/78 (2006.01) C07D 239/80 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2386955

This invention provides quinazolines that are useful for treating cell proliferative diseases and disorders, such as cardiovascular diseases, infections, cancers, autoimmune diseases, gout, kidney disease, and neurodegenerative diseases and disorders such as Alzheimer's disease. We have now discovered a group of 2-arylamino-quinazolines (I) and (II) that are potent inhibitors of cyclin-dependent kinases (cdks). The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention also provides pharmaceutical formulations comprising at least one of the quinazoline compounds together with a pharmaceutically acceptable carrier, diluent, or excipient therefor. The invention further provides useful intermediates generated during the production of the quinazoline compounds.

Cette invention porte sur des quinazolines qui sont utiles pour traiter des pathologies et états induisant la prolifération cellulaire tels que les maladies cardio-vasculaires, les infections, les cancers, les maladies auto-immunes, la goutte, les maladies du foie et les maladies et états dégénératifs tels que la maladie d'Alzheimer. Nous avons maintenant découvert un groupe de 2-arylamino- quinazolines (I) et (II) qui sont de puissants inhibiteurs des kinases dépendant de la cycline (cdks). Les composés sont facilement synthétisés et peuvent être administrés de différentes manières, y compris par voie orale, et ont une biodisponibilité suffisante. Cette invention porte également sur des formulations pharmaceutiques comprenant au moins un des composés de quinazoline et un support acceptable d'un point de vue pharmaceutique, un diluant ou un excipient de celui-ci. L'invention porte en outre sur des intermédiaires utiles générés au cours de la production des composés de quinalozine.

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