Quinazoline derivatives as medicaments

Details Quinazoline derivatives as medicaments Quinazoline derivatives as medicaments

C - Chemistry, Metallurgy

07

D

C07D 239/91 (2006.01) A61K 31/47 (2006.01) A61K 31/505 (2006.01) A61P 29/00 (2006.01) C07D 215/00 (2006.01) C07D 239/72 (2006.01) C07D 239/94 (2006.01) C07D 401/12 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2342250

The invention is directed to methods to inhibit TGF-.beta. and/or p38-.alpha. kinase using compounds of formula (1) or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar' is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

L'invention concerne des procédés relatifs à l'inhibition du TGF-bêta et/ou de la p38-.alpha. kinase au moyen des composés représentés par la formule (1), y compris les sels pharmaceutiquement acceptables desdits composés. Dans ladite formule, R?3¿ est un substituant sans activité interférentielle; chaque élément Z est CR?2¿ ou N, sachant qu'au maximum deux positions Z dans le cycle A correspondent à N, et que deux positions adjacentes Z dans ledit cycle ne peuvent pas correspondre à N; chaque élément R?2¿ est indépendamment un substituant sans activité interférentielle; L est un élément de liaison; n vaut 0 ou 1; et Ar' est le résidu d'une fraction cyclique aliphatique, cyclique hétéroaliphatique, aromatique ou hétéroatomique éventuellement substituée par les substituants 1-3 sans activité interférentielle.

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