Quinolylbenzofuran derivatives as leukotriene antagonists

Details Quinolylbenzofuran derivatives as leukotriene antagonists Quinolylbenzofuran derivatives as leukotriene antagonists

1994-08-02

1997-08-26

Haley, Jacqueline

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546167, A61K 3147, C07D40104

Patent

active

056611595

DESCRIPTION:

BRIEF SUMMARY
This is a National State application of PCT/JP93/00198 filed Feb. 18, 1993, published as WO93/17013 on Sep. 2, 1993.


TECHNICAL FIELD

This invention relates to new quinolylbenzofuran derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament.


BACKGROUND ART

Some quinolylbenzofuran derivatives have been known as described, for example, in J. Chem. Soc., 1964, 173 and Chim. Ther., 6, 159 (1971).


DISCLOSURE OF INVENTION

This invention relates to new quinolylbenzofuran derivatives and pharmaceutically acceptable salts thereof.
More particularly, it relates to new quinolylbenzofuran derivatives and pharmaceutically acceptable salts thereof which have activities as leukotriene and Slow Reacting Substance of Anaphylaxis (hereinafter, SRS-A) antagonists or inhibitors, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or treatment of allergy or inflammation in human beings or animals, and more particularly to methods for prevention and/or treatment of asthma, psoriasis, hepatitis, pancreatitis, arthritis, nephritis, inflammatory bowel disease, septic Shock, arteriosclerosis, myocardial infarction, cerebral vasospasm, rhinitis, conjunctivitis, dermatitis, rheumatism, peptic ulcer, gout and the like.
One object of this invention is to provide new and useful quinolylbenzofuran derivatives and pharmaceutically acceptable salts thereof which possess activities as leukotriene and SRS-A antagonists or inhibitors.
Another object of this invention is to provide processes for the preparation of said derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said quinolylbenzofuran derivatives and pharmaceutically acceptable salt thereof.
Still further object of this invention is to provide a therapeutical method for the prevention and/or treatment of allergy or inflammation, and more particularly of asthma, psoriasis, hepatitis, pancreatitis, arthritis, nephritis, inflammatory bowel disease, septic shock, arteriosclerosis, myocardial infarction, cerebral vasospasm, rhinitis, conjunctivitis, dermatitis, rheumatism, peptic ulcer, gout and the like, using said quinolylbenzofuran derivatives and pharmaceutically acceptable salts thereof.
The object quinolylbenzofuran derivatives of this invention are new and can be represented by the following general formula (I) : ##STR2## wherein R.sup.1 is hydrogen; halogen; lower alkyl optionally substituted with halogen, lower alkylamino or lower alkyl(acyl)amino; cyclo(lower)alkyl; tricycloalkyl; aryl optionally substituted with lower alkoxy; or a heterocyclic group; hydroxy(lower)-alkyl, halo(lower)alkyl, cyano(lower)alkyl, heterocyclic(lower) alkyl or acyl; or lower alkyl which may be substituted with substituent(s) selected from the group consisting of halogen, cyano, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, acyl, lower alkylthio, acyl(lower)alkylthio, heterocyclic(lower)alkylthio and aryl optionally substituted with halo(lower)alkyl, cyano(lower)alkyl, heterocyclic(lower)alkyl, cyano, acyl, acyl(lower)alkyl or a heterocyclic group; hydrogen, A is a single bond and X is a single bond, then R.sup.1 is halogen; lower alkyl substituted with halogen, lower alkylamino or lower alkyl(acyl)amino; cyclo(lower)alkyl; tricycloalkyl; aryl substituted with lower alkoxy; or a heterocyclic group;
The object compound (I) or its salt can be prepared by processes as illustrated in the following reaction schemes. ##STR3## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, A, X and Y are each as defined above, substituent(s) selected from the group consisting of halogen, cyano, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, acyl, lower alkylthio, acyl(lower)alkylthio, heterocyclic(lower)-alkylthio, and aryl optionally substituted with halo(lower)alkyl, cyano(lower)alkyl, heterocyclic(lower)alkyl, cyano, acyl, acyl(lower)alkyl or a heterocyclic group, select

REFERENCES:
Chemical Abstracts, vol. 72, 1970, abstract 31573e.
Musser, J.H. Journal of Medicinal Chemistry, vol. 33, No. 1 1990, pp. 240-245.
Shaw, A. Journal of Medicinal Chemistry, vol. 34, NO. 4 1991, pp. 1235-1242 .

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