Patent ID: 6277878
Filing Date: 2001-08-21
Classification: A61P,C07D,Y02P

Abstract:
A compound of the following formula: ##STR19##or the pharmaceutically acceptable salts thereof whereinR.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is C(=L')R.sup.3 or SO.sub.2 R.sup.4 ; Y is a direct bond or C.sub.1-4 alkylene; L and L' are independently oxygen or sulfur;Q is selected from the following:(Q-a) C.sub.1-6 alkyl,(Q-b) halo-substituted C.sub.1-4 alkyl,(Q-c) C.sub.3-7 cycloalkyl optionally substituted with one or two substituents independently selected from C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy and halo,(Q-d) phenyl or naphthyl, the phenyl and naphthyl being optionally substituted with one, two or three substituents independently selected from halo, C.sub.1-4, alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, halo-substituted C.sub.1-4 alkoxy, S(O).sub.m R.sup.5, SO.sub.2 NH.sub.2, SO.sub.2 N(C.sub.1-4 alkyl).sub.2, amino, C.sub.1-4 alkylamino, di-(C.sub.1-4 alkyl)amino, NR.sup.1 C(O)R.sup.5, CN, C.sub.1-4 alkyl-OH and C.sub.1-4 alkyl-OR.sup.5,(Q-e) a 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, and said monocyclic armomatic group being optionally substituted with one, two or three substituents independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkoxy, amino, C.sub.1-4 alkylamino, di-(C.sub.1-4 alkyl)amino, C.sub.1-4 alkyl-OH and C.sub.1-4 alkyl-OR.sup.5, and(Q-f) a 6-membered monocyclic aromatic group containing one nitrogen atom and optionally containing one, two or three additional nitrogen atom(s), and said monocyclic armomatic group being optionally substituted with one, two or three substituents independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkoxy, amino, C.sub.1-4 alkylamino, di-(C.sub.1-4 alkyl)amino, C.sub.1-4 alkyl-OH and C.sub.1-4 alkyl-OR.sup.5 ;R.sup.3 is --OR.sup.6, --NR.sup.7 R.sup.8, N(OR.sup.1)R.sup.7 or a group of formula: ##STR20##Z is a direct bond, oxygen, sulfur or NR.sup.5 ;R.sup.4 is C.sub.1-6 alkyl, halo-substituted C.sub.1-4 alkyl, C.sub.1-4 alkyl-OH, --NR.sup.7 R.sup.8, phenyl or naphthyl, the phenyl and naphthyl being optionally substituted with one, two or three substituents independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy and halo-substituted C.sub.1-4 alkoxy;R.sup.5 is C.sub.1-4 alkyl or halo-substituted C.sub.1-4 alkyl;R.sup.6 is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.1-4 alkyl-C.sub.3-7 cycloalkyl, halo-substituted C.sub.1-4 alkyl, C.sub.1-4 alkyl-phenyl or phenyl, the phenyl moiety being optionally substituted with one, or two substituents independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, amino, di-(C.sub.1-4 alkyl)amino and nitro;R.sup.7 and R.sup.8 are independently selected from the following:(a) hydrogen,(b) C.sub.1-6 alkyl optionally substituted with a substituent independently selected from halo, hydroxy, C.sub.1-4 alkoxy, amino, C.sub.1-4 alkylamino and di-(C.sub.1-4 alkyl)amino,(c) C.sub.3-7 cycloalkyl optionally substituted with a substituent independently selected from hydroxy, C.sub.1-4 alkyl and C.sub.1-4 alkoxy,(d) C.sub.1-4 alkyl-C.sub.3-7 cycloalkyl optionally substituted with a substituent independently selected from hydroxy, C.sub.1-4 alkyl and C.sub.1-4 alkoxy, and(f) C.sub.1-4 alkyl-phenyl or phenyl, the phenyl moiety being optionally substituted with one or two substituents independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, nitro, amino, di-(C.sub.1-4 alkyl)amino and CN;X is independently selected from halo, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, nitro, amino, di-(C.sub.1-4 alkyl)amino and CN;m is 0, 1 or 2; n is 0, 1, 2 or 3; and r is 1, 2 or 3.