HETEROCYCLIC COMPOUNDS, INHIBITORS OF NEUTROPHILE ELASTASE AND PHARMACEUTICAL COMPOSITIONS BASED ON THEREOF Russian patent published in 2004 - IPC

FIELD: chemistry of heterocyclic compounds, biochemistry, pharmacy. SUBSTANCE: invention relates to new heterocyclic compounds of the general formula (I-a) where sign * means carbon atom labeled as * and represents asymmetric carbon atom; A and B are similar or different and each represents lower alkylene group optionally substituted with oxo-group; D represents heteromonocyclic group of the formula (a) wherein D¹ represents methylene or ethylene group and these groups are optionally substituted with oxo-group; ring G represents 5- or 6-membered saturated or unsaturated heteromonocyclic group optionally containing nitrogen atom; indicated heterocyclic group can be optionally substituted with substituent T¹ wherein T¹ represents 1-3 similar or different groups taken among: (i) oxo-group; (ii) lower alkyl group; R¹ and R² are similar or different and each represents lower alkyl group; R³ and R⁴ differ of one another and each represents hydrogen atom or hydroxy-group, or both in common form oxo-group; R⁵ represents group of the formula (b) ; X¹ and X² are halogen atom; Y¹ is halogen atom, lower alkoxycarbonyl group, aralkylaminocarbonyl group or group of the formula c) wherein U is oxygen atom; Q represents unsubstituted ortho-phenylene group; n = 0 or 1; m = 0; or their esters, or salts. Inhibitor of human neutrophile elastase comprises compound of the formula (I-b) as an active component. Invention relates also to pharmaceutical composition eliciting inhibitory effect with respect to human neutrophile elastase comprising compound of the formula (I-b) as an active component or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier or excipient. Invention provides preparing heterocyclic compounds eliciting inhibitory effect on activity of human neutrophile elastase. EFFECT: valuable medicinal and biochemical properties of compounds. 8 cl, 9 tbl