Substituted isoxazoles for the treatment of inflammation

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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548182, 548186, 548190, 548193, 548202, 548203, 548225, 548228, 548229, 548232, 548234, 548235, 548243, 548245, 548247, 548248, 5462721, 544405, 514255, 514340, 514365, 514369, 514370, 514374, 514376, 514377, 514380, C07D26106, C07D26110, C07D26112, C07D26114, A61K 3142

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056332726

ABSTRACT:
A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.

REFERENCES:
patent: 5310926 (1994-05-01), Hagiwara et al.
patent: 5318970 (1994-06-01), Suzuki et al.
Ichiro Yamawaki et al, Chem. Pharm. Bull., 36:3142-3146 @(1988).
Umezawa et al, Bull. Chem. Soc. Jpn vol. 36, No. 9, pp. 1150-1154 Sep. (1963).
Descamps et al, Bull. Soc. Chim. Belg., 73:459-82 (1964).
Hagiwara et al. CA 114:42776k, @1991.
Nagai et al., CA 117:212485w, @1992.

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