Patent ID: 6306876
Filing Date: 2001-10-23
Classification: A61P,C07D

Abstract:
A compound of Formula (I): ##STR14##wherein:R.sup.1 is a substituent selected from the group consisting of hydrogen, (C.sub.1-8)alkyl, (C.sub.2-6)alkenyl, (C.sub.3-7)cycloalkyl, (C.sub.3-6)cycloalkyl(C.sub.1-3)alkyl, (C.sub.1-6)alkoxy(C.sub.1-3)alkyl, 4-(C.sub.1-4)alkyl-4,5-dihydro-5-oxo-1H-tetrazol-1-yl(C.sub.1-4)alkyl, 2-thienyl(C.sub.1-4)alkyl, 3-thienyl(C.sub.1-4)alkyl, 2-furanyl(C.sub.1-4)alkyl, 3-furanyl(C.sub.1-4)alkyl, 2-pyrrolyl(C.sub.1-4)alkyl, 3-pyrrolyl(C.sub.1-4)alkyl, 2-pyridinyl(C.sub.1-4)alkyl, 3-pyridinyl(C.sub.1-4)alkyl, 4-pyridinyl(C.sub.1-4)alkyl, 3-pyrazolyl(C.sub.1-4)alkyl, 4-pyrazolyl(C.sub.1-4)alkyl, 5-pyrazolyl(C.sub.1-4)alkyl, 2-pyrimidinyl(C.sub.1-4)alkyl, 4-pyrimidinyl(C.sub.1-4)alkyl, 5-pyrimidinyl(C.sub.1-4)alkyl, 6-pyrimidinyl(C.sub.1-4)alkyl, 2-thiazolyl(C.sub.1-4)alkyl, 4-thiazolyl(C.sub.1-4)alkyl, 5-thiazolyl(C.sub.1-4)alkyl, 2-oxazolyl(C.sub.1-4)alkyl, 4-oxazolyl(C.sub.1-4)alkyl, 5-oxazolyl(C.sub.1-4)alkyl, phenyl(C.sub.1-4)alkyl and phenyl(C.sub.2-4)alkenyl; wherein the foregoing thienyl, furanyl, pyrrolyl, thiazolyl, oxazolyl, pyrazolyl, pyridinyl, pyrimidinyl and phenyl substituents are optionally substituted with one to three substituents independently selected from the group consisting of hydroxy, halogen, (C.sub.1-3)alkyl, (C.sub.2-3)alkenyl, (C.sub.1-3)alkoxy, (C.sub.1-3)acyl, (C.sub.1-10)acyloxy, cyano, amino, (C.sub.1-3)acylamino, (C.sub.1-3)alkylamino, di(C.sub.1-3)alkylamino, (C.sub.1-3)alkylthio, (C.sub.1-3)alkylsulfonyl, --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O--, trifluoromethyl and trifluoromethoxy;R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, (C.sub.1-8)alkyl (optionally substituted with one to three halogen substituents), (C.sub.2-6)alkenyl, (C.sub.3-7)cycloalkyl, phenyl (wherein phenyl is optionally substituted with one to three substituents independently selected from the group consisting of halogen, (C.sub.1-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.3-7)cycloalkyl, --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O-- and trifluoromethyl), benzyl (wherein benzyl is optionally substituted with one to three substituents independently selected from the group consisting of halogen, (C.sub.1-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.1-6)alkoxy, (C.sub.3-7)cycloalkyl, --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O-- and trifluoromethyl), hydroxy(C.sub.1-4)alkyl, (C.sub.1-6)alkoxy(C.sub.1-4)alkyl and trifluoro(C.sub.1-4)alkoxy; alternatively, R.sup.2 and R.sup.3 may form a single fused moiety selected from the group consisting of 1,4-butylene, 1,5-pentylene, 1,5-(3-oxapentylene) and 1,5-(3-azapentylene); wherein the moiety is optionally substituted with one to four substituents independently selected from the group consisting of (C.sub.1-6)alkyl, (C.sub.2-6)alkenyl and (C.sub.3-7)cycloalkyl;the moiety --C(.dbd.X)Z is substituted on phenyl at the 3 or 4 position; wherein X is selected from the group consisting of S and O; Z is selected from the group consisting of N and O; and, Z is optionally substituted with one to two substituents independently selected from the group consisting of R.sup.2 and R.sup.3 ;with the proviso that:if Z is O, then Z is optionally substituted with one substituent selected from R.sup.2 ;n is selected from 0 or 1;Ar is selected from the group consisting of phenyl, 1-naphthyl and 2-naphthyl; wherein Ar is optionally substituted with from one to three substituents independently selected from R.sup.4 ; and,R.sup.4 is independently selected from the group consisting of hydroxy, halogen, (C.sub.1-3)alkyl, (C.sub.2-3)alkenyl, (C.sub.1-3)alkoxy, (C.sub.1-3)acyl, (C.sub.1-10)acyloxy, cyano, amino, (C.sub.1-3)acylamino, (C.sub.1-3)alkylamino, di(C.sub.1-3)alkylamino, (C.sub.1-3)alkylthio, (C.sub.1-3)alkylsulfonyl, --OCH.sub.2 O--, --O(CH.sub.2).sub.2 O--, trifluorcimethyl and trifluoromethoxy; and, alternatively, two adjacent R.sup.4 groups may form a single fused moiety, wherein the moiety is selected from the group consisting of --(CH.sub.2).sub.3-5 -- and --O(CH.sub.2).sub.1-3 O--;and pharmaceutically acceptable diastereomers and salts thereof.