Patent ID: 6235742
Filing Date: 2001-05-22
Classification: A61P,C07D

Abstract:
A compound of the formula (I) ##STR146##whereinR.sub.a is C.sub.3 -C.sub.6 alkyl;R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;each of R.sub.2 and R.sub.3 is independently selected from H and C.sub.1 -C.sub.4 alkyl, orR.sub.2 is H or C.sub.1 -C.sub.4 alkyl and R.sub.3 is OH, C.sub.2 -C.sub.4 alkanoyloxy or fluoro, orR.sub.2 and R.sub.3 when taken together represent C.sub.2 -C.sub.6 alkylene, orR.sub.2 and R.sub.3 when taken together with the carbon atom to which they are attached represent a carbonyl group;Ar is either (a) ##STR147##wherein each of R.sub.4, R.sub.5 and R.sub.6 is independently selected fromH,C.sub.1 -C.sub.4 alkyl,C.sub.1 -C.sub.4 alkoxy,C.sub.1 -C.sub.4 alkoxy-Z--,halo,halo(C.sub.1 -C.sub.4)alkyl,phenoxy, optionally substituted by up to three substitutents each of which substituent is independently selected from halo, C.sub.1 -.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy,nitro,hydroxy,hydroxy-Z--,C.sub.2 -C.sub.4 alkanoyl,amino,amino-Z--,(C.sub.1 -C.sub.4 alkyl)NH,(C.sub.1 -C.sub.4 alkyl).sub.2 N--,(C.sub.1 -C.sub.4 alkyl)NH--Z--,(C.sub.1 -C.sub.4 alkyl).sub.2 N--Z--,--COOH,--Z--COOH,--COO(C.sub.1 -C.sub.4 alkyl),--Z--COO(C.sub.1 -C.sub.4 alkyl)C.sub.1 -C.sub.4 alkanesulphonamido,C.sub.1 -C.sub.4 alkanesulphonamido-Z--,halo(C.sub.1 -C.sub.4)alkanesulphonamido,halo(C.sub.1 -C.sub.4)alkanesulphonamido-Z--,C.sub.1 -C.sub.4 alkanamido,C.sub.1 -C.sub.4 alkanamido-Z--,HOOC--Z--NH--,HOOC--Z--NH--Z--,(C.sub.1 -C.sub.4 alkyl)OOC--Z--NH--,(C.sub.1 -C.sub.4 alkyl)OOC--Z--NH--Z--,C.sub.1 -C.sub.4 alkyl-NH--SO.sub.2 --NH--,C.sub.1 -C.sub.4 alkyl-NH--SO.sub.2 --NH--Z--,(C.sub.1 -C.sub.4 alkyl).sub.2 --N--SO.sub.2 --NH--,(C.sub.1 -C.sub.4 alkyl).sub.2 --N--SO.sub.2 --NH--Z--,C.sub.1 -C.sub.4 alkoxy CH.dbd.CH--Z--CONH--,C.sub.1 -C.sub.4 alkoxy CH.dbd.CHCONHC.sub.1 -C.sub.4 alkyl-SO.sub.2 --N(C.sub.1 -C.sub.4 alkyl)-,C.sub.1 -C.sub.4 alkyl-SO.sub.2 --N(C.sub.1 -C.sub.4 alkyl)--Z--,(C.sub.1 -C.sub.4 alkyl)NH--Z--SO.sub.2 --NH--,(C.sub.1 -C.sub.4 alkyl).sub.2 N--Z--SO.sub.2 --NH--,(C.sub.1 -C.sub.4 alkyl)NH--Z--SO.sub.2 --NH--Z--,(C.sub.1 -C.sub.4 alkyl).sub.2 N--Z--SO.sub.2 --NH--Z--,benzenesulphonamido, optionally ring substituted by up to three substitutents each of which is independently selected from halo, C.sub.1 -.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy,C.sub.1 -C.sub.4 alkanoyl-N(C.sub.1 -C.sub.4 alkyl)-,C.sub.1 -C.sub.4 alkanoyl-N(C.sub.1 -C.sub.4 alkyl)-Z--,C.sub.1 -C.sub.4 alkoxycarbonyl-CH(CH.sub.2 OH)NHSO.sub.2 --,--SO.sub.3 H,--SO.sub.2 NH.sub.2,H.sub.2 NOC--CH(CH.sub.2 OH)--NHSO.sub.2 --,HOOC--Z--O--, and(C.sub.1 -C.sub.4 alkyl)OOC--Z--O--,or optionally one of R.sub.4, R.sub.5 and R.sub.6 is a G-Het group and wherein the others of R.sub.4, R.sub.5 and R.sub.6 are independently selected from the R.sub.4, R.sub.5 and R.sub.6 subsituents listed above;Z is C.sub.1 -C.sub.4 alkylene,G is a direct link, Z, O, --SO.sub.2 NH--, SO.sub.2, or --Z--N(C.sub.1 -C.sub.4 alkyl)SO.sub.2 --,Het is a 5- or 6-membered heterocyclic group containing heteroatoms selected from the groups consisting of 1, 2, 3 or 4 nitrogen heteroatoms; and 1 or 2 nitrogen heteroatoms and 1 sulphur heteroatom or 1 oxygen heteroatom; or the heterocyclic group is furanyl or thiophenyl; wherein the Het group is saturated or partially or fully unsaturated and optionally substituted by up to 3 substituents, wherein each substituent is independently selected from C.sub.1 -C.sub.4 alkyl, oxo, hydroxy, halo, and halo(C.sub.1 -C.sub.4) alkyl;or (b) any one of the following bicyclic groups:benzodioxolanyl,benzodioxanyl,benzimidazolyl,quinolinyl,indolyl,quinazolinyl,isoquinolinyl,benzotriazolyl,benzofuranyl,benzothiophenyl,quinoxalinyl, orphthalizinyl,wherein said bicyclic Ar groups are linked to the neighbouring --C(R.sub.2 R.sub.3)-- group via the benzo ring portion,and wherein the heterocyclic portion of said bicyclic Ar group is optionally partially or fully saturated, said group being optionally substituted by one or more of C.sub.1 -C.sub.4 alkyl, halo, hydroxy, oxo, amino, and C.sub.1 -C.sub.4 alkoxy;or a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable solvate of the compound or the salt.