Antiarthritic isoxazole-4-carboxamides

Details Antiarthritic isoxazole-4-carboxamides Antiarthritic isoxazole-4-carboxamides

1988-01-26

1990-06-19

Sutto, Anton H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548248, 560124, 564190, A61K 3142, C07D26104

Patent

active

049354345

ABSTRACT:
Disclosed herein are isoxazole-4-carboxamides having the formula ##STR1## wherein R.sup.1 is C.sub.3-6 cycloalkyl and R.sup.2 is selected from the group consisting of C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.2-5 alkynyl, C.sub.3-6 cycloalkyl, phenyl, and phenyl substituted with at least one group selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, and halo-substituted C.sub.1-5 alkyl; with the proviso that when R.sup.1 is cyclopropyl, R.sup.2 is not methyl, ethyl, or cyclobutyl; or R.sup.1 is C.sub.1-5 alkyl and R.sup.2 is phenylmethyl wherein the ring portion is opt. substituted with a halo-substituted C.sub.1-5 alkyl group. These compounds have antiinflammatory and antiarthritic activities and are also useful as intermediates in the preparation of .beta.-ketonitriles.

REFERENCES:
patent: 4087535 (1978-05-01), Heubach
patent: 4284785 (1981-08-01), Hanifin, Jr. et al.
patent: 4284786 (1981-08-01), Kammerer et al.
Doyle et al., J. Chem. Soc., 1963, p. 5845.
Hiroshi et al., Chemical Abstracts, vol. 96, No. 122673(1982).
Abstract for JP 45/7054 (3/11/70).

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