PYRIMIDINE DERIVATIVES AND USING THEM IN TREATING RESPIRATORY DISEASES, SUCH AS COPD Russian patent published in 2016 - IPC C07D487/04 A61K31/519 A61P11/00 A61P11/12 A61P1/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) or their pharmaceutically acceptable salt, which are neutrophil elastase (hNE) inhibitors. The compounds can be applicable for treating a disease or condition, which involves hNE, or in producing a medicinal agent. This disease or condition can be presented by chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary fibrosis, pneumonia, acute respiratory distress syndrome (ARDS), pulmonary emphysema, emphysema caused by smoking, or mucoviscidosis, asthma, rhinitis, psoriasis, atopic dermatitis, non-atopic dermatitis, Crohn's disease, nonspecific ulcerative colitis or irritable bowel disease. In formula (I)

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A represents C-R¹; R¹ and R² represent hydrogen; R⁴ represents hydrogen; R³ and R⁵ are independently specified in hydrogen and C₁-C₆-alkyl, which can be additionally substituted by halogen; R⁶ represents -CO₂R¹¹; -X¹-X²- represents -NR¹⁹-CO-; R¹¹ represents a radical of formula -[Alk¹]_p-[Alk²]_q-Z, wherein p and q independently mean 0 or 1 provided, p and q does not mean 0 at the same time; each Alk¹ and Alk² independently represent C₁-C₆-alkylene radical; Z represents (1) -N(R^A)(R^B), wherein R^A and R^B independently represent hydrogen or C₁-C₆-alkyl group; or (2) -N⁺(R^A)(R^B)(R^C), wherein R^A, R^B and R^C independently represent C₁-C₆-alkyl group; R¹⁹ is specified in hydrogen and (C₁-C₆)alkyl; optionally in the form of a pharmaceutically acceptable salt.

EFFECT: compounds can be applicable for treating a disease or condition, which involves hNE, or in producing a medicinal agent.

14 cl, 3 ex