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analogues of arylpropionamide, arylacrylamide, arylpropinamide, or arylmethylurea analogues, processes for their preparation, pharmaceutical composition and use thereof

机译:芳基丙酰胺,芳基丙烯酰胺,芳基丙酰胺或芳基甲基脲类似物,其制备方法,药物组合物及其用途

摘要

ANALOG COMPOUNDS OF ARILPROPIONAMIDE, ARILACRILAMIDE, ARILPROPINAMIDE, OR ARYLMETHYLERIA, PROCESS FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION AND USE OF THE SAME. The present invention provides compounds according to Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L ~ 1, M and R 11 are as defined. on here. The compounds according to Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and / or contact activation system; for example thrombin, factor Xa, factor Xla, factor IXa, factor VIla and / or plasma kallikrein. In particular, it refers to compounds which are selective factor X1a inhibitors or dual plasma inhibitors of fX1a and kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and / or inflammatory disorders using them.
机译:模拟化合物丙戊酰胺,芳基酰胺,芳基丙酰胺或芳菊酯的制备,药物组成和用途相同。本发明提供了根据式(I)的化合物:或其立体异构体,互变异构体,药学上可接受的盐或溶剂化物形式,其中变量A,L〜1,M和R 11如上所定义。在这。根据式(I)的化合物是凝血级联和/或接触活化系统的丝氨酸蛋白酶的选择性抑制剂;例如凝血酶,因子Xa,因子Xla,因子IXa,因子VIIa和/或血浆激肽释放酶。特别地,它是指作为fX1a和激肽释放酶的选择性因子X1a抑制剂或双重血浆抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物以及使用它们治疗血栓栓塞性和/或炎性疾病的方法。

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