Patent ID: 6211183
Filing Date: 2001-04-03
Classification: A61P,C07D

Abstract:
A compound having the formula: ##STR285##wherein:R.sup.1 is 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 and R.sup.2 is H, or R.sup.1 and R.sup.2 are taken together to form a carbocyclic ring;m is an integer from 0-2;n is an integer from 0-6;p is 1;q is 1;r is an integer from 0-4;s is an integer from 0-1;A is selected from the group consisting of R.sup.3, --NR.sup.3 R.sup.4, ##STR286##where R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl; R.sup.7 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.5 or R.sup.6 to form a 5-6 membered ring; and R.sup.8 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.6 to form a 5-6 membered ring;Q is selected from the group consisting of a direct link, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 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;D is selected from the group consisting of a direct link, --CO--, --SO.sub.2 --, --DECO--, --NR.sup.9 --SO.sub.2 -- and --NR.sup.9 --CO--, where R.sup.9 is selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl;E 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;G is selected from the group consisting of R.sup.10, --NR.sup.10 R.sup.11, ##STR287##where R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are independently selected from the group consisting of H, --OH, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl; R.sup.14 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.sub.12 or R.sup.13 to form a 5-6 membered ring; and R.sup.15 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.13 to form a 5-6 membered ring; with the proviso that when G is R.sup.10, then E must contain at least one N atom;X and Y are independently selected from the group consisting of O and H.sub.2 ;W is selected from the group consisting of H, ##STR288##where R.sup.16 and R.sup.17 are independently selected from the group consisting of H, C.sub.1-3 alkyl and aryl; anti Z is selected from the group consisting of H, --COOR.sup.18, --CONR.sup.18 R.sup.19, --CF.sub.3, --CF.sub.2 CF.sub.3 and a group having the formula: ##STR289##where:R.sup.18 and R.sup.19 are independently selected from the group consisting of H, C.sub.1-6 alkyl, aryl and C.sub.1-4 alkylaryl;U is selected from the group consisting of --O--, --S--, --N-- and --NH--; andV is selected from the group consisting of --O--, --S--, --N-- and --NH--; with the proviso that at least one of U or V is --N-- or --NH--;R.sup.20 is selected from the group consisting of H, C.sub.1-6 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 ;J is selected from the group consisting of --S--, --SO--, --SO.sub.2 --, --O-- and --NR.sup.21 --, where R.sup.21 is selected from the group consisting of H, C.sub.1-6 alkyl and benzyl; andL is selected from the group consisting of: ##STR290##a C.sub.6-10 heterocyclic ring system substituted by R.sup.24 and R.sup.25 and containing 1-4 heteroatoms selected from N, S and O;where t is an integer from 0-2;R.sup.22 and R.sup.23 are independently selected from the group consisting of H, C.sub.1-6 alkyl, aryl, C.sub.1-6 alkylaryl, --COOR.sup.26, --CONR.sup.26 R.sup.27, --CN and --CF.sub.3 ;R.sup.24 and R.sup.25 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.26 R.sup.27, --NR.sup.26 COR.sup.27, --OR.sup.26, --OCOR.sup.26, --COOR.sup.26, --CONR.sup.26 R.sup.27, --CN, --CF.sub.3, --SO.sub.2 NR.sup.26 R.sup.27 and C.sub.1-6 alkyl-OR.sup.26 ; andR.sup.26 and R.sup.27 are independently selected from the group consisting of H, C.sub.1-6 alkyl, C.sub.1-3 alkylaryl and aryl; and all pharmaceutically acceptable salts and optical isomers thereof.