C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/54 (2006.01) A61K 31/4706 (2006.01) A61K 31/4709 (2006.01) A61K 31/5377 (2006.01) C07D 215/42 (2006.01) C07D 215/44 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01)
Patent
CA 2484959
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; C 1-6 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.
L'invention porte sur de nouveaux dérivés de la quinoline de formule (1) ou leurs sels pharmacocompatibles qui présentent une activité inhibitrice de la caspase-3, et sur leurs procédés de préparation. Dans la formule (1): R¿2? est H; halogène, C¿1-6 ?alkyle, C ¿1-6? alkoxy, C¿1-6 ?alkoxyalkyle, ou C¿3-6 ?cycloalkyle; R¿1? est la formule (a), -CN, ou la formule (b); R est H, C¿6-14 ?aryle substitué ou non par halogène, C¿1-6? alkyle, C¿1-6? alkoxy ou amino, un groupe hétérocyclique à 5 - 15 éléments substitué ou non par halogène, C¿1-6? alkyle, C¿1-6? alkoxy ou amino, ou -(CH¿2?)¿n?-CHR¿4?R¿5?. Ladite invention porte également sur des préparations pharmaceutiques traitant les maladies associées à la caspase par inhibition de l'activité de la caspase-3 et comprenant les composés de formule (1) ou leurs sels pharmacocompatibles.
Jung Yoon-Sung
Kim Sung-Gyu
Kong Jae-Yang
Park Woo-Kyu
Korea Research Institute Of Chemical Technology
Ridout & Maybee Llp
Yungjin Pharmaceutical Co. Ltd.
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