Patent ID: 6268391
Filing Date: 2001-07-31
Classification: A61P,C07D

Abstract:
A compound of formula (I) ##STR138##whereinR.sup.1 is H or is optionally joined with R.sup.2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, said heteroaryl or said heterocyclyl rings having one to three heteroatoms where zero to three of said heteroatoms are N and zero to 1 of said heteroatoms are O or S and where said fused ring is optionally substituted by one to three of R.sup.9, where R.sup.2 and R.sup.9 are as defined below;R.sup.2 and R.sup.3 are independently H, HET, aryl, C.sub.1-12 aliphatic, CN, NO.sub.2, halogen, R.sup.10, --OR.sup.10, --SR.sup.10, --S(O)R.sup.10, --SO.sub.2 R.sup.10, --NR.sup.10 R.sup.11, --NR.sup.11 R.sup.12, --NR.sup.12 COR.sup.11, --NR.sup.12 CO.sub.2 R.sup.11, --NR.sup.12 CONR.sup.11 R.sup.12, --NR.sup.12 SO.sub.2 R.sup.11, --NR.sup.12 C(NR.sup.12)NHR.sup.11, --COR.sup.11, --CO.sub.2 R.sup.11, --CONR.sup.12 R.sup.11, --SO.sub.2 NR.sup.12 R.sup.11, --OCONR.sup.12 R.sup.11, C(NR.sup.12)NR.sup.12 R.sup.11 where said C.sub.1-12 aliphatic optionally bears one or two insertions of one to two groups selected from C(O), O, S, S(O), SO.sub.2 or NR.sup.12 ; with said HET, aryl or C.sub.1-12 aliphatic being optionally substituted by one to three of R.sup.10 ; and where R.sup.2 is optionally joined with R.sup.3 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, said heteroaryl or said heterocyclyl rings having zero to three heteroatoms where zero to three of said heteroatoms are N and zero to one of said heteroatoms are O or S and where said fused ring is optionally substituted by one to three of R.sup.9 ; where HET, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 are as defined below;or R.sup.2 and R.sup.3 are independently --R.sup.12 NH.sub.2, --R.sup.12 -halogen, --COR.sup.11 NR.sup.12 R.sup.11, --C(NH)R.sup.11, where R.sup.11 is as defined below, and R.sup.12 is H, C.sub.1-6 aliphatic, NO.sub.2, C.sub.1-6 alkoxy, halogen, aryl or HET, said C.sub.1-6 aliphatic optionally substituted by one to three of halogen or OH, where HET is as defined below;R.sup.4 is H, halogen, NO.sub.2 or CN;R.sup.5 is H or C.sub.1-12 aliphatic optionally substituted by one to three of halo, hydroxyl, or aryl;R.sup.6 and R.sup.7 are independently bromo or chloro;R.sup.8 is OH;each R.sup.9 is independently halogen, C.sub.1-12 aliphatic, CN, --NO.sub.2, R.sup.10, --OR.sup.11, --SR.sup.11, --S(O)R.sup.10, --SO.sub.2 R.sup.10, --NR.sup.10 R.sup.11, --N.sup.11 R.sup.12, --NR.sup.12 COR.sup.11, --NR.sup.12 CO.sub.2 R.sup.11, --NR.sup.12 CONR.sup.11 R.sup.12, --NR.sup.12 SO.sub.2 R.sup.11, --NR.sup.12 C(NR.sup.12)NHR.sup.11, --CO.sub.2 R.sup.11, --CONR.sup.12 R.sup.11, --SO.sub.2 NR.sup.12 R.sup.11, --OCONR.sup.12 R.sup.11 or C(NR.sup.12)NR.sup.12 R.sup.11, where R.sup.10, R.sup.11 and R.sup.12 are as defined below;each R.sup.10 is independently H, halogen, C.sub.1-12 aliphatic, aryl or HET, where said C.sub.1-12 aliphatic optionally bears an inserted one to two groups selected from O, S, S(O), SO.sub.2 or NR.sup.12, where said C.sub.1-12 aliphatic, aryl or HET is optionally substituted by one to three of halo, another HET, aryl, CN, --SR.sup.12, --OR.sup.12, --N(R.sup.2).sub.2, --S(O)R.sup.12, --SO.sub.2 R.sup.12, SO.sub.2 N(R.sup.12).sub.2, --NR.sup.12 COR.sup.12, --NR.sup.12 CO.sub.2 R.sup.12, --NR.sup.12 CON(R.sup.12).sub.2, --NR.sup.12 (NR.sup.12)NHR.sup.12, --CO.sub.2 R.sup.12, --CON(R.sup.12).sub.2, --NR.sup.12 SO.sub.2 R.sup.12, --OCON(R.sup.12).sub.2, where HET and R.sup.12 are as defined below;or each R.sup.10 is independently C.sub.1-6 aliphatic, aryl or HET optionally substituted by one to three of NO.sub.2, R.sup.12, --R.sup.12 N(R.sup.12).sub.2 or trifluoro, where R.sup.12 is H, C.sub.1-6 aliphatic, NO.sub.2, C.sub.1-6 alkoxy, halogen, aryl or HET, said C.sub.1-6 aliphatic optionally substituted by one to three of halogen or OH, where HET is as defined below;or each R.sup.10 is oxo, cyano or amino;or each R.sup.9 is --COR.sup.10, where R.sup.10 is H, C.sub.1-6 aliphatic or amino;R.sup.11 is H or R.sup.10 ;R.sup.12 is H, C.sub.1-12 aliphatic or HET, said C.sub.1-12 aliphatic optionally substituted by one to three of halogen or OH where HET is as defined below; or R.sup.12 is NO.sub.2, C.sub.1-6 alkoxy, halogen or aryl;HET is a five to ten-membered saturated or unsaturated heterocyclic ring selected from the group consisting of benzofuran, benzoxazole, dioxin, dioxane, dioxolane, dithiane, dithiazine, dithiazole, dithiolane, furan, imidazole, indole, indazole, morpholine, oxazole, oxadiazole, oxathiazole, oxathiazolidine, oxazine, oxiadiazine, piperazine, piperidine, pyran, pyrazine, pyrazole, pyridine, pyrimidine, pyrrole, pyrrolidine, quinoline, quinazoline, tetrahydrofuran, tetrazine, tetrazole, thiophene, thiadiazine, thiadiazole, thiatriazole, thiazine, thiazole, thiomorpholine, thianaphthalene, thiopyran, triazine, and triazole;or R.sup.12 is (R.sup.11).sub.2 N--C.sub.1-6 aliphatic, where R.sup.11 is H, C.sub.1-6 aliphatic, hydroxy-C.sub.1-6 aliphatic, phenyl, phenyl-C, aliphatic or HET, where HET is oxazole, pyridine, tetrazole or thiazole; andand the pharmaceutically acceptable salts or solvates thereof.