DERIVATIVES OF PYRIMIDINONE AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS, WHICH HAS PROPERTIES OF HUMAN NEUTROPHIL ELASTASE INHIBITOR

FIELD: medicine. ^ SUBSTANCE: invention is related to new heterocyclic compounds of common formula (I), and also their pharmaceutically acceptable salts, hydrates and/or solvates, possessing properties of human neutrophil elastase. In common formula (I) , A means phenyl or pyridyl cycle, R1 and R3 e...

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Hauptverfasser: SHLEMMER KARL-KHAJNTS, GILEN-KHEHRTVIG KHAJKE, MIN-JIAN LI FOL'KKHART, TILEHN LEHJLA, AL'BREKHT BARBARA, ROZENTRETER UL'RIKH, ALLERKHAJLIGEN SVEN, NEHSH KEVIN, KEL'DENIKH JORG, MOJRER DIRK, BEHRFAKER LARS, FITTSDZHERALD MEHRI F
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Sprache:eng ; rus
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Zusammenfassung:FIELD: medicine. ^ SUBSTANCE: invention is related to new heterocyclic compounds of common formula (I), and also their pharmaceutically acceptable salts, hydrates and/or solvates, possessing properties of human neutrophil elastase. In common formula (I) , A means phenyl or pyridyl cycle, R1 and R3 each means atom of hydrogen, R2 means atom of fluorine, chlorine, bromine, nitro group or cyano group, R4 means cyano group, alkyl carbonyl group with number of carbon atoms in alkyl residue from one to four, or alkoxycarbonyl group with number of carbon atoms in alkoxyl residue from one to four, besides alkoxycarbonyk group with number of carbon items in alkoxyl residue from one to four, may be substituted with substituent, which is selected from the group that includes hydroxyl group, alkoxygroup with number of carbon atoms from one to four, alkoxycarbonyl group with number of carbon atoms in alkoxyl residue from one to four, mono- or dialkylaminogroup, with number of carbon atoms in each of alkyl residues from one to four, 5-6-member heteroaryl group, which contains from 1 to 4 heteroatoms in heteroaryl ring, selected from nitrogen, oxygen or sulfur, possibly susbstituted with alkyl group, which contains from 1 to 4 atoms of carbon and possibly condensed with benzene ring, and 5-8 member heterocyclyl group, which contains from 1 to 3 heteroatoms from group of nitrogen, oxygen or sulfur, or SO, SO2 possibly substituted with ketogroup, R5 means methyl group, R6 means atom of hydrogen, alkyl group with number of carbon atoms from one to four, mono- or dialkylaminocarbonyl group with number of carbon atoms in each of alkyl residues from one to four, etc., Y1, Y2, Y3, Y4 and Y5 each means CH-group. Invention is also related to pharmaceutical composition. ^ EFFECT: possibility of application for treatment of chronic obstructive lung diseases, acute coronary syndrome, acute myocardial infarction and progressing cardiac decompensation. ^ 8 cl, 1 dwg, 111 ex Изобретение относится к новым гетероциклическим соединениям общей формулы (I), а также их фармацевтически приемлемым солям, гидратам и/или сольватам, обладающим свойствами ингибитора нейтрофильной эластазы человека, которые могут найти применение для лечения хронических обструктивных легочных заболеваний, острого коронарного синдрома, острого инфаркта миокарда и прогрессирующей сердечной недостаточности. В общей формуле (I) ! , ! где А означает фенильный или пиридильный цикл, R1 и R3 каждый означает атом водорода,