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TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS
专利权人:
SANOFI-AVENTIS
发明人:
HEINELT, UWE,WEHNER, VOLKMAR,HERRMANN, MATTHIAS,SCHOENAFINGER, KARL,STEINHAGEN, HENNING
申请号:
NZ58714209
公开号:
NZ587142A
申请日:
2009.01.23
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are triazolo compounds of formula I, stereoisomers, tautomers and salts thereof, and methods for their preparation. Specific examples of compounds of formula I include: 1-{ 2-[3-acetylamino-5-(pentafluorosulfanyl)phenyl]-2-oxoethyl} -3-amino-6-ethoxy-[1,2,4]triazolo[4,3-b]pyridazin-1-ium trifluoroacetate, 3-amino-1-[2-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxoethyl]-6-trifluoromethyl-[1,2,4]triazolo[4,3-a]pyridin-1-ium, 3-amino-1-[2-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxoethyl][1,2,4]triazolo[4,3-a]pyridin-1-ium, 3-amino-1-[2-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-oxoethyl]-6-trifluoromethyl-[1,2,4]triazolo[4,3-a]pyridin-1-ium, and 3-amino-1-[2-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-oxoethyl]-5-methyl-7-trifluoromethyl-[1,2,4]triazolo[4,3-a]pyridin-1-ium. Also disclosed is the use of compounds of formula I for treating disorders associated with thromboses, embolisms, hypercoagulability, fibrotic changes or inflammatory disorders, such as myocardial infarction, angina pectoris and other types of acute coronary syndrome, stroke, peripheral vascular disorders, deep vein thrombosis, pulmonary embolism, embolic or thrombotic events caused by cardiac arrhythmias, cardiovascular events such as restenosis following revascularization and angioplasty and similar procedures such as stent implantations and bypass operations or reduction of the risk of thrombosis following surgical procedures such as knee and hip joint operations or procedures leading to contact of blood with foreign surfaces, such as for dialysis patients and patients with indwelling catheters or disseminated intravascular coagulation, sepsis and other intravascular events associated with inflammation, atherosclerosis, diabetes and the metabolic syndrome and the sequelae thereof, tumor (tumour) growth and tumor metastasis, inflammatory and degenerative articular disorders such as rheumatoid arthritis and arthrosis, impairments of the hemostatic system such as fibrin deposits, fi
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