Patent ID: 6291640
Filing Date: 2001-09-18
Classification: A61K,A61P,C07K

Abstract:
A compound of formula I:##STR116##wherein z is C or P;when z is C, then X is CF.sub.3 ; C.sub.2 F.sub.5 ; benzothiazole; oxazolo[4,5b]pyridine; or benzoxazole-R.sub.7 wherein R.sub.7 is H or methyl;or X is CF.sub.2 CONH-R.sub.6 or C(O)NH-R.sub.6,wherein R.sub.6 is selected from:C.sub.0-10 alkyl optionally substituted with phenyl or cyclohexyl, said phenyl or cyclohexyl ring being optionally substituted with Me, halogen, --CF.sub.3,--CH(Me)--C(O)--OBn; --C(O)NH.sub.2 ; or --C(O)-morpholino, said phenyl or cyclohexyl ring optionally fused with a phenyl ring;(CH.sub.2).sub.1-3 --O--(CH.sub.2).sub.1-3 -phenyl, said phenyl optionally substituted with halogen;(CH.sub.2).sub.1-3 -2-benzimidazole;(CH.sub.2).sub.1-3 -(3,4-methylenedioxybenzene); or(CH.sub.2).sub.1-3 --O--C(O)--OCH.sub.2 CH.dbd.CH.sub.2 ;or, when z is P, then X is --(OPh).sub.2 ;R.sub.1 is H, Me, or Et;R.sub.2 is CH.sub.2 --SO.sub.2 NH.sub.2 ; --(C.sub.1-6 alkyl)thiazolo; --CH.sub.2 C(O)--(C.sub.1-6 alkyl); --CH.sub.2 C(O)-pyrrolidino; --CH.sub.2 C(O)-morpholino; --(C.sub.1-6 alkyl)amino; --(C.sub.1-6 alkyl)amido optionally mono- or di-substituted with C.sub.1-6 alkyl, said alkyl optionally substituted with pyridino;W is NH, CH.sub.2 or CH(CH.sub.3);R.sub.3 is --C.sub.1-12 alkyl; --(C.sub.1-6 alkyl)C(O)OH; or adamantyl;n is 0 or 1,R.sub.4, when n is 1, is --C.sub.1-6 alkyl or --(C.sub.1-6 alkyl)-aryl wherein said aryl is optionally substituted with OH;m is 0 or 1,R.sub.5, when m is 1, is H or --CH.sub.2 OH;andY is H; (CH.sub.2).sub.2 -t-Bu; or an acyl of formula:--C(O)--(CH.sub.2).sub.1-6 --C(O)OH;--C(O)--(CH.sub.2).sub.1-6 -Ph wherein Ph is optionally substituted with OH;--C(O)--CH.sub.2 N(CH.sub.3).sub.2 ;--C(O)--R.sub.9 ; --C(O)O--R.sub.9 ; or --C(O)NH--R.sub.9 wherein R.sub.9 is C.sub.1-6 alkyl; or--C(O)--(CH.sub.2).sub.1-6 --NH.sub.2 wherein the NH.sub.2 group is optionally protected with an amino protecting group.