This invention relates to a novel aminostyryl compound having leukotriene antagonistic action and a leukotriene antagonistic composition containing the same as the active ingredient.
For prophylaxis or therapy of allergic diseases, there are the method which inhibits liberation of the mediator of anaphylaxis and the method which permits an antagonist to act on the mediator liberated. Disodium cromoglycate [The Merck Index, ninth edition 2585 (1976)] and Tranirast [Journal of Japanese Pharmacology, 74, 699 (1978)] are typical drugs belonging to the former and those belonging to the latter may include drugs antagonistic to hystamine which is one of the mediators of allergic reactions such as diphenhydramine, chlorophenylamine, astemizole, terfenadine, clemastine, etc., as well known drugs. However, a substance which cannot be antagonized with an anti-hystamine agent, namely SRS (Slow Reacting Substance) has been suggested to be liberated from the lung of a bronchial asthma patient [Progr. Allergy, 6, 539 (1962)], and recently these SRS [leukotriene C.sub.4 (LTC.sub.4), leukotriene D.sub.4 (LTD.sub.4) and leukotriene E.sub.4 (LTE.sub.4)] are comprehensively called SRS [Proc. Natl. Acad. Sci. U.S.A., 76, 4275 (1979) and 77, 2014 (1980); Nature, 285, 104 (1980)] and considered as the important factor participating in human asthma attack [Proc. Natl. Acad. Sci. U.S.A., 80, 1712 (1983)].
Some leukotriene antagonists have been known in patents or literatures. For example, there have been known FPL-55712 [Agents and Actions, 9, 133 (1979)] represented by the following formula: ##STR2## KC-404 [Jap. J. Pharm., 33, 267 (1983)] represented by the following formula: ##STR3## KZ-111 [Chem. Abst, registration number 72637-30-0] represented by the following formula: ##STR4## and the compound represented by the following formula (U.S. Pat. No. 4,296,129): represented by the following formula: ##STR5## wherein R.sub.1 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a group represented by the following formula: ##STR6## (wherein R.sub.3 and R.sub.4 each represent an alkyl group having 1 to 3 carbon atoms); R.sub.2 represents an alkyl group having 8 to 15 carbon atoms or a cycloalkyl group having 6 to 12 carbon atoms; R.sub.5 and R.sub.6 each represent a hydrogen atom or a methyl group.
However, none of these have been clinically applied.
As aminostyryl compounds, there have been known compounds (West Germany Pat. No. 23 31 444) represented by the following formulas: ##STR7## and a compound [Arzneim Forsch, 19, 719 (1969)] represented by the following formula: ##STR8## However, in any of these literatures or patents, nothing is mentioned about the leukotriene antagonistic action.
Further, a compound represented by the following formulas: ##STR9## was disclosed in Japanese Unexamined Patent Publication No. 142968/1980, as a novel compound having the antiallergic action and the anti-inflammatory action. However, there is no description about the leukotriene antagonistic action.