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ISOQUINOLINE DERIVATIVES AND METHODS OF USE
专利权人:
ABBOTT LABORATORIES;GENENTECH, INC.; INC.;THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH;GENENTECH
发明人:
BAELL, JONATHAN, BAYLDON,BUI, CHINH, THIEN,COLMAN, PETER,CZABOTAR, PETER,DUDLEY, DANETTE, A,FAIRBROTHER, WAYNE, J,FLYGARE, JOHN, A,LESSENE, GUILLAUME, LAURENT,NDUBAKU, CHUDI,NIKOLAKOPOULOS, GEORGE,SLE
申请号:
NZ59353709
公开号:
NZ593537A
申请日:
2009.12.17
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Disclosed herein are isoquinoline compounds of formula I-a, wherein the substituents are as defined within the specification, processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful in the treatment or prevention of a disease or condition caused, exacerbated by or resulting from an excess of, or undesired activation of, platelets in a patient, as such is useful for treating essential thrombocythemia, polycythemia vera, restenosis, perioperative antiplatelet therapy and device-associated thrombi and also small cell lung cancer. Examples of particularly preferred compounds include: 2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylic acid; 5-(3-(4-aminophenoxy)propyl)-2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylic acid; 5-(3-(1H-imidazol-1-yl)propyl)-2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylic acid; 5-((4-(5-amino-4-cyano-1H-pyrazol-3-yl)phenoxy)methyl)-2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylic acid; 2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(4-cyanothiophen-3-yl)phenoxy)propyl)thiazole-4-carboxylic acid; 5-(3-(4-((1S,2S,5R)-9-aminobicyclo[3.3.1]nonan-2-yl)phenoxy)propyl)-2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylic acid; 6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-3-(3-(4-(5-(2-(dimethylamino)ethoxy)pyridin-2-yl)phenoxy)propyl)picolinic acid; 2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)-N-hydroxythiazole-4-carboxamide.
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