Thiazolylbenzofuran derivatives and pharmaceutical compositions

Details Thiazolylbenzofuran derivatives and pharmaceutical compositions Thiazolylbenzofuran derivatives and pharmaceutical compositions

1998-07-21

1999-11-30

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548181, 548205, C07D41704, A01K 3142

Patent

active

059943785

DESCRIPTION:

BRIEF SUMMARY
This invention relates to novel compounds and pharmaceutically acceptable salts thereof.
More particularly, it relates to new thiazolylbenzofuran 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.
One object of this invention is to provide new and useful thiazolylbenzofuran 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 thiazolylbenzofuran 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, bronchitis, gastritis, esophagitis, pancreatitis, arthritis, nephritis, inflammatory bowel disease, shock [e.g., septic shock, anaphylactic shock, etc.], arteriosclerosis, myocardial infarction, cerebral vasospasm, rhinitis, conjunctivitis, eczema, ischemic cerebral disease, chronic obstructive lung disease, cerebral edema, adult respiratory distress syndrome, neonatal pulmonary hypertension, Chrohn's disease, dermatitis (e.g., atopic dermatitis, etc.), rheumatism, gastric ulcer, peptic ulcer, gout or the like, using said thiazolylbenzofuran derivatives and pharmaceutically acceptable salts thereof.
Some thiazolylbenzofuran derivatives have been known as described, for example, in J. Heterocycl. Chem., 16, 97(1979), Chemical Abstract, 70, 11630b and 90, 152062t, and European Patent Application Publication No. 0 528 337.
The object thiazolylbenzofuran derivatives of this invention are new and can be represented by the following general formula (I): ##STR1## wherein R.sup.1 is lower alkyl, L is single bond or lower alkylene optionally substituted with aryl, oxo or hydroxy, and substituent(s); or suitable substituent(s) and at least one of which is lower alkoxy optionally substituted with cyano, protected carboxy, carboxy, lower alkylene, a heterocyclic group optionally substituted with oxo, or amidino optionally substituted with hydroxy or lower alkoxy,
One preferable genus within the embodiment described in general formula (I) is the compound of the formula (II): ##STR2## wherein --A.sup.1 --A.sup.2 --A.sup.3 -- is (a) --CR.sup.2 .dbd.CR.sup.3 --X--, (b) --N.dbd.N--NR.sup.4 -- or (c) --NR.sup.5 --N.dbd.N--, hydrogen or suitable substituent, taken together with the carbon atoms to which they are attached, they form an aromatic ring optionally substituted with one or more suitable substituent(s).
Within this genus is the preferable sub-genus of the compound of formula (II) wherein from the group consisting of acyl; carboxy; protected carboxy; aryl; and lower alkyl optionally substituted with acyl, carboxy, protected carboxy, halogen, a heterocyclic group or cyano, is optionally substituted with carboxy or protected carboxy, and
A preferable second genus within the embodiment described in general formula (I) is the compound of the formula (III) ##STR3## wherein Y is CR.sup.10 or N, and R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are each independently hydrogen or suitable substituent, taken together with the vicinal carbon atoms to which they are attached, they form an aromatic ring optionally substituted with one or more suitable substituent(s).
Within this genus is the preferable sub-genus of the compound of formula (III) wherein which they are attached, and R.sup.7 and R.sup.8 are represented by the structure: heterocyclic group; lower alkyl optionall

REFERENCES:
patent: 5296495 (1994-03-01), Matsuo et al.

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