Compounds and compositions as protein kinase inhibitors

Details Compounds and compositions as protein kinase inhibitors Compounds and compositions as protein kinase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/519 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2553785

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 and c-Met kinases. The novel class of compounds is a compound of Formula Ia: (see formula Ia) in which: n is selected from 0, 1 and 2; W is selected from -NR4-, -S-, -O-, -S(O)- and -S(O)2-; wherein R4 is selected from hydrogen and C1-6alkyl; R1 is selected from C6-10aryl-C0-4alkyl, C5-10heteroaryl-C0-4alkyl, C3-12cycloalkyl-C0-4alkyl and C3-8heterocycloalkyl-C0-4alkyl; wherein any arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl of R1 is optionally substituted by 1 to 3 radicals independently selected from halo, nitro, cyano, C6-10aryl, C5-10heteroaryl, C3-12cycloalkyl, C3-8heterocycloalkyl, C1-6alkyl, C1-6alkoxy, halo-substituted-C1-6alkyl, halo-substituted-C1-6alkoxy, -XNR5R5, -XNR5XNR5R5, -XNR5XOR5, -XOR5, -XSR5, -XS(O)R5, -XS(O)2R5, -XC(O)NR5R5, -XOXR6 and -XC(O)R6; wherein X is a bond or C1-6alkylene; R5 is selected from hydrogen, C1-6alkyl and C3-12cycloalkyl-C0-4alkyl; and R6 is selected from C3-8heterocycloalkyl-C0-4alkyl and C5-10heteroaryl-C0-4alkyl optionally substituted by 1 to 3 radicals selected from C1-6alkyl and -C(O)OH; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl substituent of R1 is further optionally substituted by 1 to 5 radicals independently selected from C1-6alkyl and C1- 6alkoxy; R2 is selected from C6-10aryl-C0-4alkyl, C5-10heteroaryl-C0-4alkyl, C3-12cycloalkyl-C0-4alkyl and C3-8heterocycloalkyl-C0-4alkyl; wherein any arylalkyl, heteroarylalkyl, cycloalkylalkyl or heterocycloalkylalkyl of R2 is optionally substituted by 1 to 3 radicals independently selected from halo, nitro, cyano, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6alkoxy, halo-substituted-C1-6alkyl, halo-substituted-C1-6alkoxy, C3-8heteroarylC0-4alkyl, -XNR5R5, -XOR5, -XSR5, -XS(O)R5, -XS(O)2R5, -XSNR5R5, -XS(O)NR5R5, -XS(O)2NR5R5, -XC(O)OR5, -XOC(O)R5, -XC(O)R5, -XC(O)NR5XNR5R5, -XC(O)NR5R5, -XC(O)NR5XC(O)OR5, -XC(O)NR5XNR5C(O)R5, -XC(O)NR5XNR5C(O)OR5, -XC(O)NR5XOR5, -XC(O)N(XOR5)2, -XNR5C(O)R5, -XC(O)NR5R6, -XC(O)R6, -XR7, -XC(O)R7, -XR6 and -XC(O)NR5XR7; wherein X is a bond or C1-6alkylene; and R5 is selected from hydrogen, C1-6alkyl and C3-12cycloalkyl-C0-4alkyl; R6 is selected from C3-8heterocycloalkyl-C0-4alkyl and C5-10heteroaryl-C0-4alkyl optionally substituted by 1 to 3 radicals selected from C1-6alkyl and -C(O)OH; and R7 is selected from halo and cyano; R3 is selected from halo, hydroxy, -XSR5, -XS(O)R5, -XS(O)2R5, -XC(O)R5 and -XC(O)OR5; wherein X is a bond or C1-6alkylene; and R5 is selected from hydrogen, C1-6alkyl and C3-12cycloalkyl-C0-4alkyl; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof.

Une nouvelle classe de composés, de compositions pharmaceutiques comprenant de tels composés et des procédés d'utilisation des composés afin de traiter ou éviter les maladies ou les troubles associés à une activité anormale ou déréglée de la kinase, plus particulièrement à des maladies ou à des troubles impliquant une activation anormale de FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 et c-Met kinases.

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