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
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Authors
Dates
2004-09-10—Published
2001-02-13—Filed