Leukotriene antagonist

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514445, 514447, 514570, 549 63, 549 66, 549 68, 549 79, 562426, 562429, 562430, A61K 3138, C07D33336, C07D33332, C07D33324

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active

047300051

ABSTRACT:
The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.2 is hydrogen, bromo, chloro, methyl, trifluoromethyl, hydroxy, methoxy or nitro; or R.sub.1 is hydrogen and R.sub.2 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxy(pentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl-C.sub.4 to C.sub.10 alkyl or ##STR4## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and p is 0 or 1, with the proviso that R is not a thiophene radical and any of R.sub.1 and R.sub.2 above are not thioalkyl or phenylthioalkyl when p is 1; and pharmaceutically acceptable salts thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.

REFERENCES:
patent: 3078290 (1963-02-01), Hechenbleikner
patent: 4111873 (1978-09-01), Cordes
patent: 4134879 (1979-01-01), Schmidt
patent: 4269731 (1981-05-01), Mack
patent: 4348383 (1982-09-01), Bouillon
Kogo et al. Chem. Abst. 89:130417 (1978).
Chemical Abstracts, vol. 85, 1976, 32188 No. 32190h, Pesek.
Chemical Abstracts, vol. 71, 1969, 74821 No. 74808g, Canonne

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