Thiazoliopyrimidines and their use as inhibitors of...

C - Chemistry – Metallurgy – 07 – D

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C07D 513/04 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2692050

Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; and R4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110.delta. isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

La présente invention concerne des thiazolopyrimidines de formule (I) : dans laquelle W représente un cycle thiazole; R1 et R2 forment, conjointement avec l'atome d'N auquel ils sont liés, un groupe ayant la formule (Ha) : dans laquelle A représente : un système cyclique; m est égal à 0, 1 ou 2; R3 représente H ou alkyle en C1- C6; et R4 représente un groupe indole substitué ou non; et leurs sels pharmaceutiquement acceptables, qui sont des inhibiteurs de la PI3K et sont sélectifs de l'isoforme p110d, qui est une PD kinase de classe Ia, par rapport aux deux autres kinases de classe Ia et Ib. Les composés peuvent être utilisés pour traiter des maladies et des troubles résultant d'une croissance, fonction ou comportement cellulaire anormaux associés à la PI3 kinase tels que cancer, troubles immunitaires, maladie cardiovasculaire, infection virale, inflammation, des troubles du métabolisme ou de la fonction endocrine et troubles neurologiques.

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