申请人:Farmitalia Carlo Erba S.p.A.
公开号:US04350627A1
公开(公告)日:1982-09-21
There is disclosed biologically active peptides of the formula ##STR1## where X is a hydrogen atom, an N-terminus protecting group (any of an acyl-type protecting group, an aromatic urethane-type protecting group, an alkyl-type protecting group, or an alkyl urethane type protecting group), or a residue of a natural L-amino acid or a dipeptide formed of two natural L-amino acids, wherein the free amino group may be replaced by any of the foregoing N-terminus protecting groups; Y is a hydrogen atom or a protecting group for the phenolic hydroxyl group of tyrosine; A is a D-amino acid residue with a lower (thio) alkyl side chain; B is a neutral L-amino acid residue, a glycine residue, or an N-methyl amino acid residue; C is a direct bond or an amino acid or di-or tripeptide residue; and W is OH, OR, NH.sub.2, NHR, N(R).sub.2, NH-NH.sub.2, where R is an alkyl, cycloalkyl or aralkyl group of 1 to 7 carbon atoms or NHNHR' where R' is a hydrogen atom, linear or branched alkyl, cycloalkyl; alkenyl, a linear or branched or cyclic aliphatic urethane-type group, an aromatic urethane-type group normally used in polypeptide chemistry, a residue of an .alpha.-amino; .alpha.-imino, or .beta.-amino acid, or a di-or tripeptide residue, where the -NHR' bond is an amidic linkage and the amino group is free or protected by an N-terminus protecting group. The peptides have central nervous system activity and are useful as analgesics, psychotics, and neuroendocrinologicals.
本发明公开了具有生物活性的肽的公式##STR1##其中X是氢原子,N-末端保护基(包括酰基保护基,芳香族脲基保护基,烷基保护基或烷基脲基保护基)或由两个天然L-氨基酸形成的二肽的残基,其中自由氨基可以被上述N-末端保护基之一所取代;Y是氢原子或酪氨酸酚羟基的保护基;A是具有较低(硫)烷基侧链的D-氨基酸残基;B是中性的L-氨基酸残基,甘氨酸残基或N-甲基氨基酸残基;C是直接键或氨基酸或二肽或三肽残基;W是OH,OR,NH.sub.2,NHR,N(R).sub.2,NH-NH.sub.2,其中R是1至7个碳原子的烷基,环烷基或芳基烷基,或NHNHR',其中R'是氢原子,线性或支链烷基,环烷基,烯基,线性或支链或环状脂肪族脲基,通常用于多肽化学中的芳香族脲基,α-氨基酸残基,α-亚氨基酸残基或β-氨基酸残基,或二肽或三肽残基,其中-NHR'键是酰胺键,氨基可以是自由的或由N-末端保护基保护的。这些肽具有中枢神经系统活性,可用作镇痛剂,精神药物和神经内分泌药物。