首页> 外国专利> 1-{N-2-(DIETHYLAMINO)ETHYL-N-4-(4-TRIFLUOROMETHYLPHENYL)-BENZYLAMINOCA RBONYLMETHYL}-2-(4-FLUOROBENZYL)THIO-5,6-TRIMETHYLENEPYRIMIDINE-4-ONE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHOD FOR PREPARING AND PHARMACEUTICAL COMPOSITION

1-{N-2-(DIETHYLAMINO)ETHYL-N-4-(4-TRIFLUOROMETHYLPHENYL)-BENZYLAMINOCA RBONYLMETHYL}-2-(4-FLUOROBENZYL)THIO-5,6-TRIMETHYLENEPYRIMIDINE-4-ONE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHOD FOR PREPARING AND PHARMACEUTICAL COMPOSITION

机译:1- {N- [2-(二乙基氨基)乙基] -N- [4-(4-三氟甲基苯基)-苄基]氨酰氨基苯甲基} -2-(4-氟联苯基)硫基-5,6-三甲基乙炔基-4-一个或其药学上可接受的盐,制备方法和药物组合物

摘要

FIELD: organic chemistry, chemical technology, medicine, pharmacy.;SUBSTANCE: invention relates to new 1-{N-[2-(diethylamino)ethyl]-N-[4-(4-trifluoromethylphenyl)-benzyl]aminocarbonylmethyl}-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidine-4-one of the formula (I):; ;or its pharmaceutically acceptable salt that elicit properties of inhibitor of enzyme Lp-PLA2 and can be used for treatment or prophylaxis of morbidity state associated with activity of indicated enzyme. Such disease can be atherosclerosis and also diabetes, hypertension, stenocardia, reprefusion, ischemia, rheumatoid arthritis, Alzheimer's disease, myocardium infarction, sepsis, acute and chronic inflammation and psoriasis. Compounds can be used, in particular, for preparing a medicinal agent used for primary and secondary prophylaxis of acute coronary attacks. Compound of the formula (I) is prepared by interaction of compound of the formula (II):; ;with compound of the formula (III): ;under conditions of amide formation. Invention relates also to a pharmaceutical composition.;EFFECT: improved preparing method, valuable medicinal properties of compound.;20 cl, 1 sch, 8 ex
机译:技术领域:本发明涉及新的1- {N- [2-(二乙氨基)乙基] -N- [4-(4-三氟甲基苯基)-苄基]氨基羰基甲基} -2 -式(I)的-(4-氟苄基)硫基-5,6-三亚甲基嘧啶-4-之一: ;或其可药用的盐,可激发Lp-PLA 2 抑制剂的性质,可用于治疗或预防与所示酶活性有关的发病状态。这种疾病可以是动脉粥样硬化,也可以是糖尿病,高血压,狭窄性心动过速,再灌注,局部缺血,类风湿性关节炎,阿尔茨海默氏病,心肌梗塞,败血症,急慢性炎症和牛皮癣。化合物尤其可以用于制备用于急性和急性冠脉发作的一级和二级预防的药物。式(I)的化合物通过式(II)的化合物的相互作用制备: ;具有式(III)的化合物:;在以下条件下酰胺的形成。本发明还涉及药物组合物。效果:改进的制备方法,该化合物的有价值的医学性质。20 cl,1 sch,8 ex

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