Patent ID: 6174889
Filing Date: 2001-01-16
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR21##or a salt or solvate thereof;wherein X is N;Y is a group W(CH.sub.2), (CH.sub.2)W, or W, in which W is 0, S(O).sub.m wherein m is 0, 1 or 2, or NR.sup.a wherein R.sup.a is hydrogen or a C.sub.1-8 alkyl group;eithern is 1, p is 0 and R"" is selected from the group consisting of phenyl, furan, thiophene, pyridine, pyrimidine, pyrazine, pyrrole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, triazole, tetrazole, and imidazole or a hydrogenated derivative thereof, said group being optionally substituted by one or more R.sup.1 groups; wherein R.sup.1 is eitherselected from M.sup.1 -M.sup.2 -M.sup.3 -M.sup.4, M.sup.1 -M.sup.5 or M.sup.1 -M.sup.2 -M.sup.3' -M.sup.6, or jselected from the group consisting of amino, hydrogen, halogen, hydroxy, hydroxy-C.sub.1-4 alkyl, formyl, carboxy, cyano, nitro, C.sub.1-8 alky, C.sub.1-8 alkoxy, C.sub.1-8 alkylthio, C.sub.1-8 alkylsulphinyl, C.sub.1-8 alkylsulphonyl, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, dioxolanyl, or hydroxy-C.sub.1-4 alkanoyl-(C.sub.1-4 alkyl)-amino; orn is 0, p is 0, 2, or 3 and each R.sup.1 is selected from the group consisting of amino, hydrogen, halogen, hydroxy, hydroxy-C.sub.1-4 alkyl, formyl, carboxy, cyano, nitro, C.sub.1-8 alkyl, C.sub.1-8 alkoxy, C.sub.1-8 alkylthio, C.sub.1-8 alkylsulphinyl, C.sub.1-8 alkylsulphonyl, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, dioxolanyl, benzyloxy, or hydroxy-C.sub.1-4 alkanoyl-amino; or when p is 2 or 3, two adjacent R.sup.1 groups together form an optionally substituted methylenedioxy or ethylenedioxy group; orn is 0, p is 1 and R.sup.1 isselected from M.sup.1 -M.sup.2 -M.sup.3 -M.sup.4, M.sup.1 -M.sup.5 or M.sup.1 -M.sup.2 -M.sup.3' -M.sup.6 ; orselected from the group consisting of amino, hydrogen, halogen, hydroxy, hydroxy-C.sub.1-4 alkyl, formyl, carboxy, cyano, nitro, C.sub.1-8 alkyl, C.sub.1-8 alkylthio, C.sub.1-8 alkylsulphinyl, C.sub.1-8 alkylsulphonyl, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, dioxolanyl, benzyloxy, or hydroxy-C.sub.1-4 alkanoyl-(C.sub.1-4 alkyl)-amino;M.sup.1 represents a C.sub.1-4 alkyl group, wherein optionally a CH.sub.2 group is replaced by a CO group;M.sup.2 represents a NR.sup.12 or CR.sup.12 R.sup.13, in which R.sup.12 and R.sup.13 each independently represent H or C.sub.1-4 alkyl;M.sup.3 represents a C.sub.1-4 alkyl group;M.sup.3' represents a C.sub.1-4 alkyl group or is absent;M.sup.4 represents CN, NR.sup.12 S(O).sub.m R.sup.13, S(O).sub.m NR.sup.14 R.sup.15, CONR.sup.14 R.sup.15, S(O).sub.m R.sup.13 or CO.sub.2 R.sup.13, in which R.sup.12, R.sup.13 and m are as hereinbefore defined and R.sup.14 and R.sup.15 each independently represent H or C.sub.1-4 alkyl, or R.sup.14 and R.sup.15 together with the nitrogen atom to which they are attached represent a 5- or 6-membered ring optionally containing 1 or 2 additional heteroatoms selected from N, O or S(O).sub.m in which ring any nitrogen atom present may optionally be substituted with a C.sub.1-4 alkyl group;M.sup.5 represents the group NR.sup.14 R.sup.15 or the group ##STR22##andM.sup.6 represents a C.sub.3-6 cycloalkyl group, the group NR.sup.14 R.sup.15 or a 5- or 6-membered heterocyclic ring system containing 1 to 4 heteroatoms selected from N, O or S;R.sup.2 represents hydrogen;U represents an indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazoylyl, 1H-benzimidazoylyl, 2,3-dihydro-1H-benimidazoylyl or 1H-benzotriazoylyl group which is substituted by at least one independently selected R.sup.6 group and is optionally substituted by at least one independently selected R.sup.4 group, each R.sup.4 is independently hydrogen, hydroxy, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylamino, di-amino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkylcarbamoyl, di-carbamoyl, carbamyl, C.sub.1-4 alkoxycarbonyl, cyano, nitro or trifluoromethyl;each R.sup.6 is independently benzyl, halo-, dihalo- and trihalobenzyl, .alpha.-methylbenzyl, phenyl, halo-, dihalo-, and trihalophenyl, pyridyl, pyridylmethyl, pyridyloxy, pyridylmethoxy, thienylmethoxy, dioxolanylmethoxy, cyclohexylmethoxy, phenoxy, halo-dihalo-, and trihalophenoxy, phenylthio, benzyloxy, halo-, dihalo-, trihalobenzyloxy, C.sub.1-4 alkoxybenzoyloxy, phenyloxalyl or benzenesulphonyl; and A represents ##STR23##