DERIVATIVES OF PYRIMIDINONE AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS, WHICH HAS PROPERTIES OF HUMAN NEUTROPHIL ELASTASE INHIBITOR Russian patent published in 2009 - IPC C07D239/22 C07D401/04 C07D401/12 C07D403/12 C07D403/08 C07D405/08 C07D413/04 C07D417/04 A61K31/513 A61K31/5377 A61P9/00 

Abstract RU 2376295 C9

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

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RU 2 376 295 C9

Authors

Gilen-Khehrtvig Khajke

Min-Jian Li Fol'Kkhart

Rozentreter Ul'Rikh

Shlemmer Karl-Khajnts

Allerkhajligen Sven

Tilehn Lehjla

Behrfaker Lars

Kel'Denikh Jorg

Fittsdzherald Mehri F.

Nehsh Kevin

Al'Brekht Barbara

Mojrer Dirk

Dates

2009-12-20Published

2003-08-28Filed