Patent ID: 6103739
Filing Date: 2000-08-15
Classification: A61K,A61P,C07K

Abstract:
A compound of formula (I) ##STR31## wherein X is a group of formula (II) ##STR32## R.sub.2 is a group --(Alk).sub.m --(Q).sub.n --Z wherein m and n are independently 0 or 1,Alk represents (C.sub.1 -C.sub.6)alkyl,Q represents --O--, --S--, --SO-- or SO.sub.2 --, andZ represents hydrogen, or an optionally substituted (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, or phenyl group;R.sub.1 is hydrogen or a group R.sub.20 C(O)-- where R.sub.20 is a (C.sub.1 -C.sub.6)alkyl;R.sub.21 is hydrogen or a phthalimido(C.sub.1 -C.sub.4)alkyl- or optionally methyl-substituted 2,5-dioxo-1-imidazolidinyl(C.sub.1 -C.sub.6)alkyl group;R.sub.3 is the side chain of a natural .alpha.-amino acid in which any functional groups may be protected, or a group selected from 4-chlorophenylmethyl, 2-thienylmethyl, iso-butyl or 1-benzylthio-1-methylethyl, benzyl, t-butyl or 1-mercapto-1-methylethyl,R.sub.4 is a phenyl or pyridyl, thiazolyl, or quinolyl ring wherein any ring nitrogen atom may be oxidized as an N-oxide, and wherein any of the rings may be optionally substituted by:(a) one or more substituents independently selected from hydroxyl, halogen, --CN, --CO.sub.2 (C.sub.1 -C.sub.6)alkyl, --(C.sub.1 -C.sub.6)alkyl-CO.sub.2 (C.sub.1 -C.sub.6)alkyl, --CONH.sub.2, --CONH(C.sub.1 -C.sub.6)alkyl, --CON(C.sub.1 -C.sub.6)alkyl).sub.2, --CHO, --CH.sub.2 OH, --(C.sub.1 -C.sub.4)perfluoroalkyl, --O(C.sub.1 -C.sub.6)alkyl, --S(C.sub.1 -C.sub.6)alkyl, --SO(C.sub.1 -C.sub.6)alkyl, --SO.sub.2 (C.sub.1 -C.sub.6)alkyl, --NO.sub.2, NH.sub.2 --NH(C.sub.1 -C.sub.6)alkyl, --N((C.sub.1 -C.sub.6)alkyl).sub.2, and --NHCO(C.sub.1 -C.sub.6)alkyl, or(b) a group selected from (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.4 -C.sub.8)cycloalkenyl, phenyl, benzyl, heteroaryl or heteroarylmethyl any of which groups may be optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, carboxyl, (C.sub.1 -C.sub.4)perfluoroalkyl, (C.sub.1 -C.sub.6)alkyl, --O(C.sub.1 -C.sub.6)alkyl or --S(C.sub.1 -C.sub.6)alkyl;R.sub.5 is hydrogen or a (C.sub.1 -C.sub.6)alkyl group;or a salt, hydrate or solvate thereof.