The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R2 is H; halogen; C1-6alkyl; C1-6 alkoxy; C1-6 alkoxyalkyl; or C3-6cycloalkyl; R1 is formula (a); —CN; or formula (b); R is H; C6-14aryl unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; 5-15 membered heterocyclic group unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; or —(CH2)n—CHR4R5. The present invention relates to a pharmaceutical composition for treating caspase-associated diseases by inhibiting the activity of caspase-3 which comprises the compound of formula (1) or its pharmaceutically acceptable salt. ##STR1##

 
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