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

Abstract RU 2604719 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, having inhibitory activity on human neutrophil elastase (HNE). In formula (I) , A is C-R1; R1 and R2 are hydrogen; R4 is hydrogen; R3 and R5 are independently selected from hydrogen and C1-C6-alkyl, which can be substituted with halogen; R6 is selected from -COOH, -COORA, -CONH2, -CONHRA and -CONRARB, where RA and RB independently represent (C1-C6)alkyl; -X1-X2- is -CR15=N- or -NR19-CO-; R15 and R19, each independently, represent a radical of formula -[Y]m-[Alk1]p-[Alk2]q-Z, where Y is -(C=O)NRE- or -NRE(C=O)-, where RE is hydrogen or C1-C6-alkyl; m, p, q are independently equal to 0 or 1; provided that m, p and q are not simultaneously equal to 0, when -X1-X2- is -CR15=N-; Alk1 and Alk2, each independently, denote C1-C6-alkylene radical; Z is -N(RA)(RB), where RA and RB independently represent hydrogen or C1-C6-alkyl group.

EFFECT: compounds can be used for treating a disease or condition, which is a chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary fibrosis, pneumonia, acute respiratory distress syndrome (ARDS), emphysema, emphysema caused by smoking, or mucoviscidosis, asthma, rhinitis, psoriasis, atopic dermatitis, non-atopic dermatitis, Crohn's disease, ulcerative colitis or irritable bowel disease.

14 cl, 4 ex

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RU 2 604 719 C2

Authors

Eduards Kristin

Kulagovski Janush

Finch Garri

Dates

2016-12-10Published

2011-03-10Filed