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Pyrimidinone derivatives as therapeutic agents for acute and chronic inflammation, ischemia and remodeling processes

机译:嘧啶酮衍生物作为急性和慢性炎症,局部缺血和重塑过程的治疗剂

摘要

Compounds of formula (I) and salts, hydrates and/or solvates thereof and their tautomeric forms in which A is an aryl or heteroaryl ring, each of R1, R2 and R3 are independently H or various substituents, R4, R5, R6 and R7 are various substituents and each of Y1, Y2 Y3, Y4, and Y5 are independently CH or N so that the ring contains 0, 1 or 2 nitrogen atoms. In particular, A is a phenyl ring, each of Y1-Y5 is CH and R4 is an alkoxycarbonyl residue. The compounds may be inhibitors of human leukocyte elastase (HLE, also known as human neutrophil elastase or HNE) and as such may be useful in the treatment of chronic obstructuive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
机译:式(I)的化合物及其盐,水合物和/或溶剂化物及其互变异构形式,其中A为芳基或杂芳基环,R 1,R 2和R 3各自独立地为H或各种取代基R 4,R 5,R 6和R 7是各种取代基,并且Y 1,Y 2 Y 3,Y 4和Y 5各自>独立地为CH或N,使得该环含有0、1或2个氮原子。特别地,A为苯环,Y 1 -Y 5各自为CH,R 4为烷氧羰基残基。所述化合物可以是人白细胞弹性蛋白酶(HLE,也称为人嗜中性粒细胞弹性酶或HNE)的抑制剂,因此可以用于治疗慢性阻塞性肺疾病,急性冠状动脉综合征,急性心肌梗塞和心力衰竭。

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