| abstract |
Compounds having the formula:n and their pharmaceutically acceptable salts and acid- addition salts, are antagonists of leukotrienes of C 4 , D 4 and E 4 , the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-Inflammatory agents and cytoprotective agents. n In the formula, each R, independently of the others, is hydrogen, hydroxy, C 1-6 alkyl, C 2-6 alkenyl, trifluoromethyl, C 1-6 alkoxy, mercapto, C 1-6 thioalkyl, phenyl, phenyl substituted by C 1-3 alkyl or by halogen, benzyl, phenethyl, halogen, amino, N(R 3 ) 2 , COOR 3 , CH 2 0R 3 , formyl, cyano, trifluoromethylthio or nitro;n each R', independently of the others, R 3 or R 4 , or R' and R' together are an oxo or methylene group; each R 1 , independently of the others, is hydrogen or C 1-4 alkyl; R 2 is C 1-6 alkyl or C 3-6 alkenyl; each R 3 , independently of any others, is hydrogen or C 1-6 alkyl; R 4 is hydrogen, C 1-6 alkyl or C 1-6 alkoxy; R 6 is hydrogen, C 1-6 alkyl, R 3 CO- or R 3 0CH 2 -; each R 6 , independently of any others, is R 3 or is such that HNR 6 -(CR 6 R 6 )-COOR 3 is an amino acid or amino acid ester; each of X 1 and X 2 , independently of the other, is oxygen, sulfur, sulfoxide, sulfone;n Z is 0, S or NR 3 ; each n, independently of any others, is 0 or an integer from 1 to 6. |