QUINOLINE AND QUINOXALINE DERIVATIVES AS INHIBITORS OF KINASE ENZYMATIC ACTIVITY

摘要

Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y¹, L¹ and z are as defined in the claims; R₆ is C₁-C₄alkoxy, hydrogen or halo; W represents a bond, -CH₂-, -O-, -S-, -S(=O)₂-, or -NR₅- where R₅ is hydrogen or C₁-C₄ alkyl; Q is =N-, =CH- or =C(X¹)- wherein X¹ is cyano, cyclopropyl or halo; linker radicals L² are as defined in the claims; R is a radical of formula (X) or (Y): wherein R₁ is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R₄ is hydrogen; or optionally substituted C₁-C₆ alkyl, C₃-C₇ cycloalkyl, aryl, aryl(C₁-C₆ alkyl)-, heteroaryl, heteroaryl(C₁-C₆ alkyl)-, -(C=O)R₃, -(C=O)OR₃, or -(C=O)NR₃ wherein R₃ is hydrogen or optionally substituted (C₁-C₆)alkyl, C₃-C₇ cycloalkyl, aryl, aryl(C₁-C₆ alkyl)-, heteroaryl, or heteroaryl(C₁-C₆ alkyl)-; R₄