Patent ID: 6262030
Filing Date: 2001-07-17
Classification: C07H

Abstract:
A compound of the formula 1 ##STR56##or a pharmaceutically acceptable salt thereof, wherein:X is --O--, --NR.sup.5 --, or (CR.sup.5 R.sup.6).sub.g, wherein g is 0 or 1 and wherein, when X is --NR.sup.5 --, R.sup.5 and R.sup.2 are taken together to form --(CR.sup.7 R.sup.8)--;or X is taken together with R.sup.1 to form --N.dbd.CR.sup.7 R.sup.8 ;or X and R.sup.1 are taken together to form a heterocyclic ring of the formula XI ##STR57##wherein in said ring of formula XI, r and p are each independently an integer ranging from 1 to 3, q is 0 or 1, and R.sup.9 is --CH.sub.2 --, O, S, --C(O)--, --C(S)--, --SO.sub.2 --, --CH.dbd.CH--, --CH(OH)CH(OH)--, or --NH--; and wherein the (CH.sub.2).sub.r and (CH.sub.2).sub.p portions of said ring of formula XI are optionally substituted by 1 to 4 substituents and wherein each hydrogen atom of R.sup.9 when R.sup.9 is --CH.sub.2 --, --CH.dbd.CH--, --CH(OH)CH(OH)--, or --NH is optionally substituted by one substituent, said optional substituents being independently selected from the group consisting of --C(O)OR.sup.10, --OR.sup.10, --C(O)R.sup.10, halo, nitro, cyano, 4-10 membered heterocyclic, --R.sup.10, --NR.sup.10 R.sup.11, --NHC(O)R.sup.10, --NHC(O)NR.sup.10 R.sup.11, C.sub.6 -C.sub.10 aryl, 4-10 membered heterocyclic, --S(O).sub.n R.sup.10, and --SO.sub.2 NR.sup.10 R.sup.11, wherein n is an integer ranging from 0 to 2;Y is R.sup.7 or --(CR.sup.5 R.sup.6).sub.m R.sup.12, wherein m is an integer ranging from 0 to 6; and R.sup.5 and R.sup.6 may each independently vary when m is greater than 1;R.sup.1 is H, R.sup.7, --C(O)R.sup.7, --C(O)R.sup.12, --C(O)OR.sup.7, --C(O)OR.sup.12, or --(CR.sup.5 R.sup.6).sub.m R.sup.12, wherein m is an integer ranging from 0 to 6;R.sup.2 is H or C.sub.1 -C.sub.12 alkyl, wherein one or two carbons of said alkyl are optionally replaced by a heteroatom selected from the group consisting of O, S and N, and are optionally substituted by 1 to 3 substituents selected from the group consisting of --C(O)OR.sup.10, --OR.sup.10, --C(O)R.sup.10, halo, nitro, cyano, 4-10 membered heterocyclic, --R.sup.10, --NR.sup.10 R.sup.11, --NHC(O)R.sup.10, --NHC(O)NR.sup.10 R.sup.11, C.sub.6 -C.sub.10 aryl, 4-10 membered heterocyclic, --S(O).sub.n R.sup.10, and --SO.sub.2 NR.sup.10 R.sup.11, wherein n is an integer ranging from 0 to 2;each R.sup.3 is independently selected from the group consisting of H, --C(O)R.sup.12 or C.sub.1 -C.sub.18 alkanoyl, wherein in the alkyl portion of said alkanoyl one or two carbons optionally may be replaced by a heteroatom selected from O, S and N;each R.sup.5 and R.sup.6 is independently H, halo, or C.sub.1 -C.sub.10 alkyl and R.sup.5 and R.sup.6 may each independently vary when m is greater than 1;each R.sup.7 and R.sup.8 is independently selected from H and C.sub.1 -C.sub.18 alkyl, wherein one or two carbons of said alkyl are optionally replaced by a heteroatom selected from the group consisting of O, S and N, and are optionally substituted by 1 to 3 substituents selected from the group consisting of --C(O)OR.sup.10, --OR.sup.10, --C(O)R.sup.10, halo, nitro, cyano, 4-10 membered heterocyclic, --R.sub.01, --NR.sup.10 R.sup.11, --NHC(O)R.sup.10, --NHC(O)NR.sup.10 R.sup.11, C.sub.6 -C.sub.10 aryl, 4-10 membered heterocyclic, --S(O)n R10 and --SO.sub.2 NR.sup.10 R.sup.11, wherein n is an integer ranging from 0 to 2;each R.sup.10 and R.sup.11 is independently H or C.sub.1 -C.sub.10 alkyl; and,R.sup.12 is a 4-10 membered heterocycyl or C.sub.6 -C.sub.10 aryl, wherein said heterocycyl and aryl groups are optionally substituted by 1 to 3 substituents independently selected from the group consisting of --C(O)OR.sup.10, --OR.sup.10, --C(O)R.sup.10, halo, nitro, cyano, 4-10 membered heterocyclic, --R.sup.10, --NR.sup.10 R.sup.11, --NHC(O)R.sup.10, --NHC(O)NR.sup.10 R.sup.11, C.sub.6 -C.sub.10 aryl, 4-10 membered heterocyclic, --S(O).sub.n R.sup.10, and --SO.sub.2 NR.sup.10 R.sup.11, wherein n is an integer ranging from 0 to 2.