Patent ID: 6214991
Filing Date: 2001-04-10
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR37##or a pharmaceutically acceptable salt thereof whereinA is a C.sub.1 -C.sub.4 alkylene group unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl or mono- or disubstituted with halogen;Z is a bond, O, S, C(O)NH, or C.sub.1 -C.sub.3 alkylene unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl;R.sub.1 is hydrogen, alkyl having 1-6 carbon atoms, halogen, 2-, 3-, or 4-pyridyl, or phenyl, where the phenyl or pyridyl is unsubstituted or substituted with up to three groups selected from halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, nitro, amino, or mono- or di(C.sub.1 -C.sub.6)alkylamino;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, nitro, or an alkyl group of 1-6 carbon atoms unsubstituted or substituted with one or more halogens;OR.sub.7, SR.sub.7, S(O)R.sub.7, S(O).sub.2 N(R.sub.7).sub.2, C(O)N(R.sub.7).sub.2, or N(R.sub.7).sub.2, wherein each R.sub.7 is independently hydrogen, an alkyl group of 1-6 carbon atoms unsubstituted or substituted with one or more halogens, or benzyl, where the phenyl portion is unsubstituted or substituted with up to three groups independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, and mono- or di(C.sub.1 -C.sub.6)alkylamino;phenyl or heteroaryl, each of which phenyl or heteroaryl is unsubstituted or substituted with up to three groups independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, and mono- or di(C.sub.1 -C.sub.6)alkylamino;phenoxy where the phenyl portion is unsubstituted or substituted with up to three groups independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, and mono- or di(C.sub.1 -C.sub.6)alkylamino; ora group of the formula ##STR38##whereJ is a bond, CH.sub.2, oxygen, or nitrogen; andeach r is independently 2 or 3;R.sub.6 is hydrogen, benzyl, di(C.sub.1 -C.sub.6)alkylaminoethyl, acetoxymethyl, pivaloyloxymethyl, phthalidoyl, ethoxycarbonyloxyethyl, 5-methyl-2-oxo-1,3-dioxol-4-yl methyl, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by N-morpholino, or di(C.sub.1 -C.sub.6)alkylamino;R.sub.a is hydrogen, C.sub.1 -C.sub.6 alkyl, fluoro, or trifluoromethyl;and Ar representsa heterocyclic 5-membered ring having one nitrogen, oxygen or sulfur, one nitrogen and either one oxygen or one sulfur, two nitrogens, two nitrogens and either one oxygen or one sulfur, or three nitrogens said heterocyclic 5-membered ring being condensed with benzo, where the benzo is unsubstituted or substituted by one of iodo, cyano, nitro, perfluoroethyl, trifluoroacetyl, or (C.sub.1 -C.sub.6)alkanoyl, one or two of fluoro, chloro, bromo, hydroxy, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylthio, trifluoromethoxy, trifluoromethylthio, (C.sub.1 -C.sub.6)alkylsulfinyl, (C.sub.1 -C.sub.6)alkylsulfonyl or trifluoromethyl, or two fluoro or two trifluoromethyl with one hydroxy or one (C.sub.1 -C.sub.6)alkoxy, or one or two fluoro and one trifluoromethyl, or three fluoro, said pyridyl, furyl or thienyl unsubstituted or substituted in the 3-position by fluoro, chloro, bromo, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkoxy;a heterocyclic 6-membered ring having one to three nitrogen atoms, or one or two nitrogen atoms and one oxygen or sulfur said heterocyclic 6-membered ring being condensed with benzo which is unsubstituted or substituted by one of iodo or trifluoromethylthio, or one or two of fluoro, chloro, bromo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylthio, (C.sub.1 -C.sub.6)alkylsulfinyl, (C.sub.1 -C.sub.6)alkylsulfonyl, or trifluoromethyl, and said pyridyl, furyl or thienyl unsubstituted or substituted in the 3-position by fluoro, chloro, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkoxy;said benzo-condensed heterocyclic 5-membered or 6-membered rings being unsubstituted or substituted in the heterocyclic 5-membered or 6-membered ring by one of fluoro, chloro, bromo, methoxy, or trifluoromethyl.