Patent ID: 6235929
Filing Date: 2001-05-22
Classification: A61K,C07C,C07D,C07K

Abstract:
A compound of the formula:M.sub.1 --AA.sup.1 --AA.sup.2 --AA.sup.3 --CO--NR.sub.3 R.sub.4or a pharmaceutically acceptable salt, whereinM.sub.1 represents H, NH.sub.2 --CO--, NH.sub.2 --CS--, NH.sub.2 --SO.sub.2 --, X--NH--CO--, X.sub.2 N--CO--, X--NH--CS--, X.sub.2 N--CS--, X--NH--SO.sub.2 --, X.sub.2 N--SO.sub.2 --, X--CO--, X--CS--, X--SO.sub.2 --, X--O--CO, X--O--CS--;X is selected from the group consisting of C.sub.1-10 alkyl, C.sub.1-10 fluoroalkyl, C.sub.1-10 alkyl substituted with J, C.sub.1-10 fluoroalkyl substituted with J, 1-admantyl, 9-fluorenyl, phenyl, phenyl substituted with K, phenyl disubstituted with K, phenyl tisubstituted with K, naphthyl, naphthyl substituted with K, naphthyl disubstituted with K, naphthyl trisubstituted with K, C.sub.1-10 alkyl with an attached phenyl group substituted with K, C.sub.1-10 alkyl with two attached phenyl groups substituted with K, C.sub.1-10 alkyl with an attached phenoxy group, and C.sub.1-10 alkyl with an attached phenoxy group substituted with K on the phenoxy group;J is selected from the group consisting of halogen, COOH, OH, CN, NO.sub.2, NH.sub.2, C.sub.1-10 alkoxy, C.sub.1-10 alkylamine, C.sub.2-12 dialkylamine, C.sub.1-10 akyl--O--CO--, C.sub.1-10 alkyl--O--CO--NH--, and C.sub.1-10 alkyl--S--;K is selected from the group consisting of halogen, C.sub.1-10 alkyl, C.sub.1-10 perfluoroalkyl, C.sub.1-10 alkoxy, NO.sub.2, CN, OH, CO.sub.2 H, amino, C.sub.1-10 alkylamino, C.sub.2-12 dialkylamino, C.sub.1-10 acyl, and C.sub.1-10 alkoxy--CO--, and C.sub.1-10 alkyl--S--;AA.sup.1 and AA.sup.2 are the same or different and are side chain blocked or unblocked amino acids with the L configuration, D configuration, or no chirality at the a-carbon selected from the group consisting of alanine, valine, leucine, isoleucine, glycine, serine, aspartic acid, and glutamic acid;AA.sup.3 is selected from the group consisting of aspartic acid and glutamic acid;R.sub.3 is selected from the group consisting of C.sub.2-3 alkyl with a phenyl group attached to the C.sub.2-3 alkyl, C.sub.3-20 cyclized alkyl with an attached phenyl group, C.sub.1-20 alkyl with an attached phenyl group substituted with K, C.sub.1-20 alkyl with an attached phenyl group disubstituted with K, C.sub.1-20 alkyl with an attached phenyl group trisubstituted with K, C.sub.3-20 cyclized alkyl with an attached phenyl group substituted with K, --NH--CH.sub.2 CH.sub.2 --(4-hydroxyphenyl), and --NH--CH.sub.2 CH.sub.2 --(3-indolyl); andR.sub.4 is selected from the group consisting of H, C.sub.3-20 alkyl, cyclized alkyl, C.sub.1-20 alkyl with a phenyl group attached to the C.sub.1-20 alkyl, C.sub.3-20 cyclized alkyl with an attached phenyl group, C.sub.1-20 alkyl with an attached phenyl group substituted with K, C.sub.1-20 aLkyl with an attached phenyl group disubstituted with K, C.sub.1-20 alkyl with an attached phenyl group trisubstituted with K, C.sub.3-20 cyclized alkyl with an attached phenyl group substituted with K, --NH--CH.sub.2 CH.sub.2 --(4-hydroxyphenyl), and --NH--CH.sub.2 CH.sub.2 --(3-indolyl).