Indol derivative and their use as inhibitors of p38 kinase

Details Indol derivative and their use as inhibitors of p38 kinase Indol derivative and their use as inhibitors of p38 kinase

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/404 (2006.01) A61P 43/00 (2006.01) C07D 209/24 (2006.01) C07D 209/42 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2429605

The invention is directed to methods to inhibit p38-.alpha. kinase using compounds of formula (I) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein ---- represents a single or double bond; B is Wi-COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 A, and each of i and j is independently 0 or 1; each R3 is independently a noninterfering substituent, wherein n is 0-3; Z3 is NR7 or O; wherein R7 is H or a noninterfering substituent; one Z2 is C or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; wherein A is (II) such that Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; each R4 is independently a noninterfering substituent where m is 0-4; each of L1 and L2 is a linker; and the distance between the atom of Ar linked to L2 and the center of the .beta. ring is a 4.5-24A.

L'invention concerne des procédés pour inhiber p38-.alpha. kinase en utilisant des composés de la formule (I) et leurs sels pharmaceutiquement acceptables ou une composition pharmaceutique à base de ces composés; dans cette formule, ---- représente une liaison simple ou double; B est W¿i?-COX¿j?Y, où Y est COR?2¿ ou son isostère et R?2¿ est hydrogène ou un substituant sans activité interférentielle, chacun des W et X est un espaceur of 2-6 A, et chacun parmi i et j est indépendamment 0 ou 1; chacun R?3¿ est indépendamment un substituant sans activité interférentielle, où n est 0-3; Z?3¿ est NR?7¿ ou O; où R?7¿ est H ou un substituant sans activité interférentielle; un Z?2¿ est C ou CR?8¿A et l'autre est CR?1¿, CR?1¿¿2?, NR?6¿ ou N où chacun R?1¿, R?6¿ et R?8¿ est indépendamment hydrogène ou substituant sans activité interférentielle; où un est (II) de sorte que Z?1¿ soit CR?5¿ ou N où R?5¿ soit hydrogène ou un substituant sans activité interférentielle; chacun parmi 1 et k est entier entre 0-2 où la somme de 1 etk est 0-3; Ar est groupe aryle substitué avec 0-5 substituants sans activité interférentielle; chacun R?4¿ est indépendamment un substituant sans activité interférentielle où m est 0-4; chacun parmi L?1¿ et L?2¿ est un lieur. Enfin, la distance entre l'atome de Ar lié à L2 et le centre du noyau .beta. est de 4,5-24.ANG..

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