N-hydroxyamide, N-hydroxythioamide, hydroxyurea, and N-hydroxythiourea derivatives of selected nsaids as antiinflammatory agents
AssigneeWarner-Lambert Company
InventorsThomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
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Abstract
The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxygenase.
Claims22
A compound of the formula (I) ##STR40## and a pharmaceutically acceptable acid addition or base salt thereof;
- wherein Ar is (1) ##STR41## wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, fluoro, chloro, bromo, iodo, CF.sub.3, lower alkyl, CN, hydroxy, lower alkoxy, --S(O)q-lower alkyl wherein q is an integer of 0, 1, or 2, NO.sub.2 or NR.sub.4 R.sub.5 wherein R.sub.4 or R.sub.5 are independently hydrogen, lower alkyl, lower acyl;
- ##STR42## Y is O or S;
- W is lower alkyl, aryl, aralkyl, lower alkoxy, NR.sub.6 R.sub.7, (CH.sub.2).sub.n CO.sub.2 R.sub.7, NH(CH.sub.2).sub.m CO.sub.2 R.sub.7, NH(CH.sub.2).sub.p NR.sub.6 R.sub.7, or NHCH.sub.2 CH.dbd.CH.sub.2
- wherein R.sub.5 is independently as defined above, R.sub.6 and R.sub.7 are independently hydrogen or lower alkyl, n is an integer of from 0 to 3, m is an integer of from 0 to 3;
- and p is an integer of 2 or 3;
- with the proviso that Y cannot be sulfur when n is 0.
A compound which is N-hydroxy-9H-fluoren-2-methanamine.
A compound which is N-hydroxy-.alpha.-methyl-9H-fluorene-2-methanamine.
Dependencies are inferred from the claim text.