Known potassium canal activating heterocyclic cpds. - can be used in the prophylaxis of obstructive and inflammatory respiratory tract problems esp. asthma, pneumonoconiosis and morning dipping

摘要

Heterocyclic cpds. of formula (I) and their N-oxides, pharmaceutically acceptable acid addn. salts or quat. ammonium salts can be used in the prepn. of pharmaceuticals for the prophylaxis of obstructive or inflammatory problems of the respiratory tract. aa) V = R1C, T = R2C and W = CH; bb) V = N, T = R2C and W = CH; cc) V = R1'C, T = CH and W = N; dd) V = N, T = CH and W = N; R1 = H, halogen ethynyl, OH, CN, NR6R8,COOR6 or CONR6R7; R2 = H, halogen, 1-4C alkoxy, OH or NR6R8 or one of R1 and R2 = NO2 and the other gp. is defined as above; R1' = H, CN or NO2; R3 and R4 = each H or 1-4C alkyl or R3 and R4 together form -(CH2)n; R5 = H or OR8; R6 and R7 = each H or 1-4C alkyl; R8 = H, 1-4C alkyl, formyl, ethanoyl or trifluoroethanoyl; R9 and R10 = each H or Me or together form oxo or thio; n = 2-5; m = 1-3; X = O or NR11; Y = CH, C-halogen, N, C-formyl or C-hydroxymethyl, Z = CH2, O, S, CH halogen or NR6; R11 = H, 1-4C alkyl, formyl, ethanoyl or hydroxymethyl. USE/ADVANTAGE - (I) are known to have an opening effecting on K+ canals and are usually used in the cardiovascular region e.g. as vasodilators and also as bronchodilators e.g. in the symptomatic treatment of asthma. It is now found that (I) suppress, reduce or remove the basal pathology of obstructive or inflammatory problems of the respiratory tract by suppressing, reducing or removing the hyperactivity of the respiratory tract or the collection of pulmonary eosinophilic cells which are the origins of these problems. Thus (I) can be used prophylactically, in marked contrast to previously used medicaments which are used symptomatically and have no influence on the pathology of the disease. (I) can also be used in the prophylaxis of pneumoconiosis and Morning dipping. Suitable daily doses are 0.1-2 mg p.o. or 50-500 mg/day when inhaled.