Peptide derivatives and peptidomimetic (D) and their stereoisomer forms, E/Z-isomers, enantiomers, enantiomeric mixture, diastereomers, diastereomeric mixture, racemates, tautomers, anomers, keto-enol-forms, betaine forms, prodrugs, solvate, hydrate or their salts, are new. Peptide derivatives and peptidomimetic (D) of formula (I-III), and their stereoisomer forms, E/Z-isomers, enantiomers, enantiomeric mixture, diastereomers, diastereomeric mixture, racemates, tautomers, anomers, keto-enol-forms, betaine forms, prodrugs, solvate, hydrate or their salts, are new, where (I) excludes compounds having X and X1a are hydrogen and Y 1>；is hydroxy. MS : acceptor substituted olefin of formula (-CH(R 1>；)(R 2>；)-CH(R 3>；)(R 4>；)-(CO) m-CH(Z 3>；)=C(Z 1>；)(Z 2>；))； E : e.g. -CH 2-, -CF 2-, -C 2H 4-, -CH 2-CF 2-, -CF 2-CH 2-, -CH=CH-, -CH(OH)-CH 2-, -C(=O)-CH 2-, -CH 2-NH-, -CH 2-O-, -CH(OH)-CH 2-NH-, -P(=O)(OH)-NH-, -P(=O)(OH)-O- or -P(=O)(OH)-S-； m : 0 or 1； either Z 1>；-Z 3>；e.g. CO-(1-6C-alkyl), -COO-(1-6C-alkyl) (both preferred), -CO-R 6>；, -CO-R 7>；, -CO-(1-6C-haloalkyl), -CO-(3-10C-heteroaryl), -CO-(6-15C-aryl), -COO-(1-6C-haloalkyl), -COO-(3-10C-heteroaryl), -COO-(6-15C-aryl), -CN, -F, -Cl, -COOH, -CO-NH(1-6C-alkyl), -CO-N(1-6C-alkyl)(1-6C-alkyl), -CO-NH 2, -CH 2CN, -CH 2F, -CHF 2, -CF 3, -OCF 3, -CH 2-CF 3, -CF 2-CF 3, -NO 2, -CS-(1-6C-alkyl), -CS-N(1-6C-alkyl)(1-6C-alkyl), -OS-NH 2, -SO-N(1-6C-alkyl)(1-6C-alkyl), -SO 2-N(1-6C-alkyl)(1-6C-alkyl), SO 2-OH, -O-P(O)(OH) 2, -O-P(O)(O-1-6C-alkyl)(O-1-6C-alkyl), -P(O)(O-1-6C-alkyl)(O-1-6C-alkyl) or -CF 2-P(O)(O-1-6C-alkyl)(O-1-6C-alkyl)； or Z 2>；+Z 3>；e.g. -CO-O-CH 2-, -CO-O-CO- or -CO-NH-CO-； either Q, Q 1>；a side chain residue of a natural amino acid； or Q+X1a, Q 1>；+X1b : a propylenyl group； Y 1>；e.g. OH, amino, 1-6C-alkylamino, 1-6C-dialkylamino, 1-6C-alkoxy, 1-6C-alkyl, 1-6C-haloalkyl, 3-10C-heteroaryl, 6-15C aryl, a peptidomimetic group of up to 60 carbon atoms or amine bond bounded pe
