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Urethanes, ureas, amidines and related inhibitors of factor xa
专利权人:
PHARMADIALL LTD.
发明人:
MALAKHOV DMITRY VIKTOROVICH,TOVBIN DMITRY GENNADIEVICH,TARASOV DMITRY NIKOLAEVICH
申请号:
NZ60276911
公开号:
NZ602769A
申请日:
2011.03.02
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed are betrixaban analogues as represented by formula (I), wherein: R1 is selected from H, -Cl, -F, -Br, -OH, -Me, -OMe; R2 is selected from CH and N; R3 and R4 are each independently selected from H, -Cl, -F, -Br, -OH, -Me, -OMe; R5 is selected from H or alkyl which is optionally substituted with a hydroxyl, carboxylic acid or a carboxylic acid ester group; R6 is a imine or amide containing group as defined herein; R8, R9 and R10 are each independently selected from H, -Cl, -F, -Br, -OH, -Me, -OMe; R7 is selected from group H, -Cl, -F, -Br, -OH, -Me, -OMe or an optionally substituted aminoalkoxy moiety as defined herein. Representative compounds include N-(5-chloropyridin-2-yl)-2-([4-(N-methyl-N-acetamidino)benzoyl]amino)-5-methoxybenzamide, N-(5-chloropyridin-2-yl)-2-([4-(N-methyl-N-acetamidino)benzoyl]amino)-5-methyl-benzamide, N-(5-chloropyridin-2-yl)-5-chloro-2-([2-fluoro-4-(N-methyl-N-acetamidino)benzoyl]amino)-benzamide and N-(5-chloropyridine-2-yl)-2-[4-(ethaneimidoylmethylamino)-2-(3-aminopropoxy)-6-fluorophenylcarbonylamino]-5-methylbenzamide. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above for use in preventing or treating a condition in a mammal characterized by undesired thrombosis, including conditions such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, occlusive coronary thrombus occurring post-thrombolytic therapy or post-coronaryangioplasty, a thrombotically mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, transient ischemic attacks, venous thrombosis, deep venous thrombosis, pulmonary embolus, coagulopathy, disseminated intravascular coagulation, thrombotic thrombocytopenic purpura, thromboangiitis obliterans, thrombotic disease associated with heparin-induced thrombocytopenia, thrombotic complications associated with extracorporeal circulation, and thrombotic complications associated with fitting of pro
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