Patent ID: 8445484

Claim:
A compounds of formula (I) wherein: R1 is —CH(R)COR5; R is an α-amino acid side chain; R2 is H, alkyl, aryl, alkylaryl; R3 and R4 are independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, alkylaryl, aryl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, and —CH(α-amino acid side chain)CH 2 OH; R3 and R4 together with the nitrogen atom to which they are connected can form a ring, selected from the group consisting of piperidine, 4-hydroxyethyl-piperazine, 4-methyl-piperazine, 4-carboethoxy-piperazine, 4-phenylethyl-piperazine, 4-benzyl-piperazine, and morpholine; R5 is selected from the group consisting of -Oalkyl, -Oaryl, -NHalkyl, NHaryl, and amino acid; comprising all the possible combination of stereoisomers. the term “amino acid” includes every natural α-amino acids of the L or D series having as “side chain”: —H for glycine; —CH3 for alanine; —CH(CH 3 ) 2 for valine; —CH 2 CH(CH 3 ) 2 for leucine; —CH(CH 3 )CH 2 CH 3 for isoleucine; —CH 2 OH for serine; —CH(OH)CH 3 for threonine; —CH 2 SH for cysteine; —CH 2 CH 2 SCH 3 for methionine; —CH 2 -(fenil) for phenylalanine; —CH 2 -(fenil)-OH for tyrosine; —CH 2 -(indole) for tryptophan; —CH 2 COOH for aspartic acid; —CH 2 C(O)(NH 2 ) for asparagine; —CH 2 CH 2 COOH for glutamic acid; —CH 2 CH 2 C(O)NH 2 for glutamine; —CH 2 CH 2 CH 2 —N(H)C(NH 2 )NH for arginine; —CH 2 -(imidazole) for hystidine; —CH 2 (CH 2 ) 3 NH 2 for lysine, comprising the same side chains of amino acids bearing suitable protecting groups; and the term “amino acid” includes non natural amino acids, such as ornitine (Orn), norleucine (Nle), norvaline (NVa), β-alanine, L or D α-phenylglycine (Phg), diaminopropionic acid, diaminobutyric acid, aminohydroxybutyric acid, and other well known in the state of the art of peptide chemistry.