(19)
(11)EP 4 257 192 A3

(12)EUROPEAN PATENT APPLICATION

(88)Date of publication A3:
18.10.2023 Bulletin 2023/42

(43)Date of publication A2:
11.10.2023 Bulletin 2023/41

(21)Application number: 23191923.4

(22)Date of filing:  20.12.2018
(51)International Patent Classification (IPC): 
C07D 217/02(2006.01)
A61P 27/02(2006.01)
A61K 31/472(2006.01)
(52)Cooperative Patent Classification (CPC):
A61K 9/0048; A61K 9/08; A61K 31/472; A61K 31/4725; A61P 27/02; C07D 217/02
(84)Designated Contracting States:
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

(30)Priority: 26.12.2017 US 201762610446 P
30.11.2018 US 201816206000

(62)Application number of the earlier application in accordance with Art. 76 EPC:
18214556.5 / 3505513

(71)Applicant: Industrial Technology Research Institute
Chutung, Hsinchu 310401 (TW)

(72)Inventors:
  • CHEN, Chih-Hung
    730 Tainan City (TW)
  • CHEN, Yi-Hsun
    300 Hsinchu City (TW)
  • HUANG, Jui-Wen
    302 Zhubei City (TW)
  • HUANG, Kuo-Kuei
    302 Zhubei City (TW)
  • LIU, Chih-Peng
    300 Hsinchu City (TW)
  • HWANG, Chrong-Shiong
    300 Hsinchu City (TW)

(74)Representative: Michalski Hüttermann & Partner Patentanwälte mbB 
Kaistraße 16A
40221 Düsseldorf
40221 Düsseldorf (DE)

  


(54)ISOQUINOLINE DERIVATIVES AND THEIR USE FOR THE TREATEMTN OF OPHTHALMIC DISORDERS


(57) 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, NR4, NCOR4, NCONR4R5, NCO-aryl, S, or O. Y and J are independently H, alkyl, aryl, aminoalkyl, -NH2, -CN, -OH, -O-alkyl, -O-aryl, -COOH, -COOR4, -CONHR4, -CONHCH2-aryl, -CONR4CH2-aryl,-NHCOR4, halogen, halogened alkyl, -alkyl-OR4, -O-alkyl-OR4, -alkyl-ONO2, O-alkyl-ONO2, -OCOOR4, -O(C=O)-aryl, -CHR4OH, -CH2OH, -CH2O(C=O)-aryl,-CH2O(C=O)-R4, -CHR4O(C=O)-aryl, -CHR4O(C=O)-R4, unsaturated carboxylic ester, substituted alkynyl, -NHSO2R4, -SR4, -SO2R4, -SO2NHR4, or -SO2NR4R5, or Y and J bond together to form a carbocylic or aromatic ring, wherein R4 and R5 are independently H, substituted C1-C6 alkyl, substituted aryl, cycloalkyl, alkylaryl,-alkyl-NR6R7, -alkyl-OR6, -alkyl-ONO2, -S(O)0-2-(alkyl-NR6R7). R1, R2 and R3 are H, C1-C6 alkyl, cycloalkyl, aryl, alkylaryl, alkylheteroaryl, alkylheterocycle, wherein any one thereof is optionally substituted with one or more of OH, NO2, or NR8R9.







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Search report