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US 5,296,495 AGranted
Thiazolylbenzofuran derivatives and pharmaceutical composition comprising the same
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsMasaaki Matsuo, Kazuo Okumura, Shinji Shigenaga, Hiroshi Matsuda
Life of this patent
Estimating the term…
Abstract
Compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A, X and Y are as defined and pharmaceutically acceptable salts thereof; which have activities as leukotriene and Slow Reacting Substance of Anaphalaxis (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 inflamation in human beings or animals.
Claims8
A compound of the formula:
- ##STR6## wherein R.sup.1 is lower alkyl optionally substituted with halogen, lower alkylamino or lower alkyl(acyl)amino;
- cyclo(lower)alkyl;
- tricycloalkyl;
- aryl optionally substituted with lower alkoxy;
- thienyl;
- or pyridyl;
- R.sup.2 is hydrogen or halogen, or
- R.sup.1 and R.sup.2 are taken together with the adjacent atoms to form cycloalken ring or tetrahydroazepine optionally substituted with acyl,
- R.sup.3 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,
- R.sup.4 is hydrogen;
- acyl;
- cyano;
- aryl optionally substituted with hydroxy(lower)alkyl, halo(lower)alkyl, cyano(lower)alkyl, tetrazolyl(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, acyl(lower)alkylthio and aryl optionally substituted with halo(lower)alkyl, cyano(lower)alkyl, tetrazolyl(lower)alkyl, cyano, acyl, acyl(lower)alkyl, tetrazolyl or (lower alkylsulfinyl)(lower alkylthio)lower alkenyl;
- wherein in R.sup.1, R.sup.1 and R.sup.2 taken together, and R.sup.4 acyl is selected from the group consisting of carboxy, esterified carboxy, carbamoyl optionally substituted with lower alkyl arylsulfonyl, lower alkylsulfonyl, lower alkanoyl, aroyl and heterocycliccarbonyl,
- A is lower alkylene, lower alkenylene or a single bond,
- X is a single bond, O or S, and
- Y is O or S,
- provided that A or X is not a single bond when R.sup.1 is lower alkyl or aryl and R.sup.2 is hydrogen, or pharmaceutically acceptable salts thereof.
16 more elements
Dependencies are inferred from the claim text.