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    ISOQUINOLINE DERIVATIVES AND THEIR USE FOR THE TREATEMTN OF OPHTHALMIC DISORDERS
    1.
    发明公开
    ISOQUINOLINE DERIVATIVES AND THEIR USE FOR THE TREATEMTN OF OPHTHALMIC DISORDERS 审中-公开

    公开(公告)号：EP3505513A1

    公开(公告)日：2019-07-03

    申请号：EP18214556.5

    申请日：2018-12-20

    申请人： Industrial Technology Research Institute

    发明人： Chen, Chih-Hung ,  Chen, Yi-Hsun ,  Huang, Jui-Wen ,  Huang, Kuo-Kuei ,  Liu, Chih-Peng ,  Hwang, Chrong-Shiong

    IPC分类号： C07D217/02 ,  A61K31/472 ,  A61P27/02

    摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof is provided. In formula (I), Ar is indazole, 5-isoquinoline, 6-isoquinoline, or their N-oxide. X is -C(=Z)-, wherein Z is N-CN, NH, NR 4 , NCOR 4 , NCONR 4 R 5 , NCO-aryl, S, or O. Y and J are independently H, alkyl, aryl, aminoalkyl, -NH 2 , -CN, -OH, -O-alkyl, -O-aryl, -COOH, -COOR 4 , -CONHR 4 , -CONHCH 2 -aryl, -CONR 4 CH 2 -aryl,-NHCOR 4 , halogen, halogened alkyl, -alkyl-OR 4 , -O-alkyl-OR 4 , -alkyl-ONO 2 , O-alkyl-ONO 2 , -OCOOR 4 , -O(C=O)-aryl, -CHR 4 OH, -CH 2 OH, -CH 2 O(C=O)-aryl,-CH 2 O(C=O)-R 4 , -CHR 4 O(C=O)-aryl, -CHR 4 O(C=O)-R 4 , unsaturated carboxylic ester, substituted alkynyl, -NHSO 2 R 4 , -SR 4 , -SO 2 R 4 , -SO 2 NHR 4 , or -SO 2 NR 4 R 5 , or Y and J bond together to form a carbocylic or aromatic ring, wherein R 4 and R 5 are independently H, substituted C1-C6 alkyl, substituted aryl, cycloalkyl, alkylaryl,-alkyl-NR 6 R 7 , -alkyl-OR 6 , -alkyl-ONO 2 , -S(O) 0-2 -(alkyl-NR 6 R 7 ). R 1 , R 2 and R 3 are H, C1-C6 alkyl, cycloalkyl, aryl, alkylaryl, alkylheteroaryl, alkylheterocycle, wherein any one thereof is optionally substituted with one or more of OH, NO 2 , or NR 8 R 9 .