1,3-diaryl substituted ureas as modulators of kinase activity

Details 1,3-diaryl substituted ureas as modulators of kinase activity 1,3-diaryl substituted ureas as modulators of kinase activity

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/404 (2006.01) A61P 35/04 (2006.01)

Patent

CA 2594449

Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non- covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck sguamous cell carcinoma. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom

L'invention porte: sur certaines entités chimiques de formule (I) et leurs sels, solvates, formes cristallines, chélates, complexes non covalents, prodrogues, pharmacocompatibles, et leurs mélanges; sur des préparations pharmaceutiques comprenant au moins l'une de ces entités et un ou des véhicules choisis parmi des vecteurs, adjuvants et excipients; sur leur utilisation pour traiter des patients souffrant de maladies ou troubles réagissant à la modulation de la kinase angiogène tels que des cancers, dont ceux du sein, de l'endomètre, du colon, et le carcinome squameux du col, consistant à leur administrer une dose d'au moins une de ces entités pour en réduire les signes ou les symptômes; et sur une méthode permettant de déterminer la présence ou l'absence d'une kinase angiogène dans un échantillon, consistant à mettre l'échantillon en contact avec l'une au moins desdites entités dans des conditions permettant de détecter l'activité de ladite kinase et son niveau.

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