Patent ID: 6066657
Filing Date: 2000-05-23
Classification: A61P,C07D

Abstract:
A compound of formula (i) ##STR7## wherein Z is CO or CS;R.sub.1 is selected from the group consisting of OH, alkoxy optionally substituted with one or more halogens, and thioalkyl optionally substituted with one or more halogens;R.sub.3 is selected from the group consisting of H, alkyl, and halogen;R.sub.4 is H or alkyl;R.sub.5 is aryl or heteroaryl, either of which may be substituted at any position with one or more substitutents R.sub.14 or alkyl-R.sub.14 ;R.sub.14 is selected from the group consisting of alkyl optionally substituted with one or more halogens, aryl, heteroaryl, heterocyclo, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, SO.sub.2 NR.sub.9 R.sub.10, OR.sub.11, halogen, CN, NR.sub.8 R.sub.12, COR.sub.13, S(O).sub.p R.sub.13, and NHSO.sub.2 CF.sub.3 ;p is 0-2;R.sub.8 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, and heterocycloalkyl;R.sub.9 and R.sub.10 are the same different and selected from the group consisting H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, and heterocycloalkyl, or NR.sub.9 R.sub.10 represents a heterocyclic ring;R.sub.11 is selected from the group consisting of H, alkyl optionally substituted with one or more halogens, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, and heterocycloalkyl;R.sub.12 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, heterocycloalkyl, alkylcarbonyl, alkoxycarbonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl, alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, and heterocyclosulphonyl;R.sub.13 is selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, cycloalkylalkyl, arylalkyl, heteroarylalkyl, and heterocycloalkyl;R.sub.2 is selected from the group consisting of alkyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, and heterocycloalkyl, any of which can be attached at any position on the alkyl portion to A and through the same different position to the benzofuran ring wherein the aryl or heteroaryl group is optionally substituted at any position by one or more substitutents R.sub.14 or alkyl-R.sub.14, and the cycloalkyl or heterocycloalkyl group is optionally substituted at any position with one or more substituents R.sub.7 or alkyl-R.sub.7, or R.sub.2 is absent;R.sub.7 is selected from the group consisting of carbonyl oxygen, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, SO.sub.2 NR.sub.9 R.sub.10, NR.sub.8 R.sub.12, OR.sub.11, alkyl optionally substituted with one or more halogens, halogen, CN, NHSO.sub.2 CH.sub.3, tetrazolyl, and heterocyclo;A is selected from the group consisting of --O--, --O--(C(R.sub.15).sub.2).sub.n --, --O--(C(R.sub.15).sub.2).sub.n --C(.dbd.O)--(C(R.sub.15).sub.2).sub.m --, --O--(C(R.sub.15).sub.2).sub.n --SO.sub.q --(C(R.sub.15).sub.2).sub.m --, --NR.sub.6 --, --NR.sub.6 --(C(R.sub.15).sub.2).sub.n --, --NR.sub.6 --(C(R.sub.15).sub.2).sub.m --C(.dbd.O)--(C(R.sub.15).sub.2).sub.m --, --NR.sub.6 --(C(R.sub.15).sub.2).sub.n --SO.sub.q --(C(R.sub.15).sub.2).sub.m --, --SO.sub.q --, --SO.sub.q --(C(R.sub.15).sub.2).sub.m --, and --SO.sub.q NR.sub.6 --;R.sub.6 is H or alkyl;n is 1-4;m is 0-4;q is 1 or 2;R.sub.15 is H or alkyl; andB is selected from the group consisting of H, a heterocyclic ring optionally substituted at any position with one or more substitutents R.sub.7 or alkyl-R.sub.7, and alkyl, aryl, or heteroaryl, any of which can be optionally substituted at any position with one or more substituents R.sub.14 or alkyl-R.sub.14 ;provided that B is H only when R.sub.2 is cycloalkylalkyl and A is --O--, and that B is substituted when R.sub.2 is not cycloalkylalkyl and A is selected from the group consisting of --O--, --O--(C(R.sub.15).sub.2).sub.n, --O--(C(R.sub.15).sub.2).sub.n --C(.dbd.O)--(C(R.sub.15).sub.2).sub.m --, --NR.sub.6 --, --NR.sub.6 --(C(R.sub.15).sub.2).sub.n --, and --NR.sub.6 --(C(R.sub.15).sub.2).sub.n --C(.dbd.O)--(C(R.sub.15).sub.2).sub.m --;or a N-oxide or pharmaceutically acceptable salt thereof.