Patent ID: 6218382
Filing Date: 2001-04-17
Classification: A61K,A61P,C07K

Abstract:
A compound having the formula: ##STR100##Wherein:R.sup.1 and R.sup.2 are independently selected from the group consisting of H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-3 alkylaryl, C.sub.1-3 alkyl-C.sub.3-8 cycloalkyl and aryl;R.sup.3 is H, C.sub.1-6 alkyl, or R.sup.2 and R.sup.3 are taken together to form a carbocyclic ring;q is an integer equal to 1;r is an integer from 0-4;s is an integer from 0-1;t is an integer from 0-4;A is selected from the group consisting of R.sup.8, --NR.sup.8 R.sup.9, ##STR101##where R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are independently selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylawyl; R.sup.12 is selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl, or can be taken together with R.sup.10 or R.sup.11 to form a 5-6 membered ring; and R.sup.13 is selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl, or can be taken together with R.sup.11 to form a 5-6 membered ring;D is selected from the group consisting of a direct link, C.sub.3-8 cycloalkyl, C.sub.1-6 alkenyl, C.sub.1-6 alkenylaryl, aryl and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S;E is selected from the group consisting of a direct link, --CO--, --SO.sub.2 --, --O--CO--, --NR.sup.14 --SO.sub.2 -- and --NR.sup.14 --CO--, where R.sup.14 is selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl;G is selected from the group consisting of a direct link, C.sub.3-8 cycloalkyl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from the group consisting of N, O and S;J is selected from the group consisting of R.sup.15, --NR.sup.15 R.sup.16, ##STR102##where R.sup.15, R.sup.16, R.sup.17 and R.sup.18 are independently selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl; R.sup.19 is selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl, or can be taken together with R.sup.17 or R.sup.18 to form a 5-6 membered ring; and R.sup.20 is selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl, or can be taken together with R.sup.18 to form a 5-6 membered ring; with the proviso that when J is R.sup.15, then G must contain at least one N atom;K', K"", K'"" and K"""" are each --CH--;Q is selected from the group consisting of H, ##STR103##where R.sup.21 and R.sup.22 are independently selected from the group consisting of H, C.sub.1-3 alkyl and aryl; and T is selected from the group consisting of H, --COOR.sup.23, --CONR.sup.23 R.sup.24, --CF.sub.3, --CF.sub.2 CF.sub.3 and a group having the formula: ##STR104##where: R.sup.23 and R.sup.24 are independently selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl; U' and U"" are independently selected from the group consisting of --O--, --S--, --N-- and --NH--; with the proviso that at least one of U' or U"" is --N-- or --NH--; R.sup.25 is selected from the group consisting of H, C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.0-6 alkylaryl, C.sub.2-6 alkenylaryl, C.sub.0-6 alkylheterocyclo, C.sub.2-6 alkenylheterocyclo, --CF.sub.3 and --CF.sub.2 CF.sub.3 ; V is selected from the group consisting of --S--, --SO--, --SO.sub.2 --, --O-- and --NR.sup.26 --, where R.sup.26 is selected from the group consisting of H, C.sub.1-6 alkyl and benzyl; and W is selected from the group consisting of: ##STR105##a C.sub.6-10 heterocyclic ring system substituted by R.sup.29 and R.sup.30 and containing 1-4 heteroatoms selected from N, S and O; where: a is an integer from 0-2; R.sup.27 and R.sup.28 are independently selected from the group consisting of H, C.sub.1-6 alkyl, aryl, C.sub.1-6 alkylaryl, --COOR.sup.31, --CONR.sup.31 R.sup.32, --CN and --CF.sub.3 ; and R.sup.29 and R.sup.30 are independently selected from the group consisting of H, C.sub.1-6 alkyl, aryl, C.sub.1-6 alkylaryl, C.sub.1-4 alkyloxy, halogen, --NO.sub.2, --NR.sup.31 R.sup.32, --NR.sup.31 COR.sup.32, --OR.sup.31, --OCOR.sup.31, --COOR.sup.31, --CONR.sup.31 R.sup.32, --CN, --CF.sub.3, --SO.sub.2 NR.sup.31 R.sup.32 and C.sub.1-6 alkyl--OR.sup.31 ; where R.sup.31 and R.sup.32 are independently selected from the group consisting of H, C.sub.1-6 alkyl, C.sub.1-3 alkylaryl and aryl; or all pharmaceutically acceptable salts or optical isomers thereof.