Patent ID: 6090824
Filing Date: 2000-07-18
Classification: A61P,C07D

Abstract:
A compound of formula XVI: R.sup.1 is independently selected from the group consisting of hydroxy, dimethylamino, acetamido, phenyl, methyl-sulphinyl-phenyl, 2-oxo-perhydro-pyrimidinyl, piperidino, 2-oxo-piperidino, carbamoyl, N-methyl-carbamoyl, and 2-oxo-2,3-dihydro-benzimidazolyl;R.sup.2 is independently selected from the group consisting of H, hydroxy, dimethylamino, acetamido, phenyl, methyl-sulphinyl-phenyl, 2-oxo-perhydro-pyrimidinyl, piperidino, 2-oxo-piperidino, carbamoyl, N-methyl-carbamoyl, and 2-oxo-2,3-dihydro-benzimidazolyl;X and Y are independently selected from the group consisting of H, halogen, and hydroxy, provided that X or Y is halogen;Z is selected from the group consisting of --OC(.dbd.O)NR.sup.3.sub.2, --N(R.sup.4)C(.dbd.O)OR.sup.3, --N(R.sup.4)C(.dbd.O)NR.sup.3.sub.2, --N(R.sup.4)C(.dbd.O)SR.sup.3, --SC(.dbd.O)NR.sup.3.sub.2, --N(R.sup.4)C(.dbd.O)R.sup.3, and --OC(.dbd.O)R.sup.3 ; whereinR.sup.3 at each occurrence is independently selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl, heteroaryl, aryl-C.sub.1 -C.sub.3 -alkyl, heteroaryl-C.sub.1 -C.sub.3 -alkyl, and a radical of formula XV, ##STR3## where any aryl or heteroaryl group or radical of R.sup.3 may be mono-, di- or tri-substituted with substituents independently selected from the group consisting of halo, trifluoromethyl, hydroxy, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkyl, cyano, and methylenedioxy, and further wherein any arylethyl, arylpropyl, heteroarylethyl or heteroarylpropyl group may be substituted at the position .alpha. to the aryl or heteroaryl group by an oxo group; andwhere, in a radical of formula XV, E is selected from --O--, --S--, --N(R.sup.3)--, --S(.dbd.O)-- and --SO.sub.2 --; m is 1, 2, or 3; and R.sup.3 is as heretofore defined;R.sup.4 at each occurrence is independently selected from hydrogen or C.sub.1 -C.sub.3 -alkyl;or, any of the foregoing compounds having an N-oxide at the piperidino nitrogen in formula XVI;or, a pharmaceutically-acceptable salt of any of the foregoing compounds.