Pyrazolo[3,4-d]-pyramidine derivatives as antiproliferative...

Details Pyrazolo[3,4-d]-pyramidine derivatives as antiproliferative... Pyrazolo[3,4-d]-pyramidine derivatives as antiproliferative...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2694666

The present invention is directed to novel pyrazolo[3,4-d]pyrimidine derivatives of the formula (I), and pharma-ceutically-acceptable salts and esters thereof, wherein R, Ring A, L, and Ring B are as described herein. These compounds and their pharmaceutically-acceptable salts and esters inhibit Raf kinase and have antiproliferative activity. As such, they are useful in the treatment or control of proliferative disorders such as cancer, in particular solid tumors, more particularly breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.

La présente invention porte sur de nouveaux dérivés de pyrazolo[3,4-d]pyrimidine de la formule (I), et sur des sels et esters pharmaceutiquement acceptables de ces dérivés. Dans la formule (I), R, le noyau A, L et le noyau B sont tels que décrits présentement. Ces composés et leurs sels et esters pharmaceutiquement acceptables inhibent la Raf kinase et ont une activité antiproliférative. En tant que tels, ils sont utiles dans le traitement ou la lutte contre les troubles prolifératifs tels que le cancer, en particulier les tumeurs solides, plus particulièrement la tumeur du sein, la tumeur du côlon, la tumeur du poumon, la tumeur de la prostate et le mélanome. L'invention porte également sur une composition et une formulation posologique unitaire comprenant un tel composé, ou un sel ou ester pharmaceutiquement acceptable de celui-ci, sur des procédés de fabrication de tels composés et sur des procédés d'utilisation de tels composés, ou leurs sels ou esters pharmaceutiquement acceptables, dans le traitement de troubles prolifératifs.

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