公开(公告)号：US4350627A

公开(公告)日：1982-09-21

申请号：US212586

申请日：1980-12-03

申请人： Roberto de Castiglione ,  Fiorenzo Faoro ,  Giuseppe Perseo ,  Silvano Piani ,  Francesco Santangelo

发明人： Roberto de Castiglione ,  Fiorenzo Faoro ,  Giuseppe Perseo ,  Silvano Piani ,  Francesco Santangelo

IPC分类号： A61K38/00 ,  C07K5/107 ,  C07K14/665 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K14/665 ,  C07K5/1016 ,  A61K38/00 ,  Y02P20/55 ,  Y10S514/809

摘要： 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; andW 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.

摘要翻译： 公开了式（I）的生物活性肽，其中X是氢原子，N末端保护基（酰基型保护基，芳族氨基甲酸酯型保护基，烷基型 保护基或烷基氨基甲酸酯型保护基）或由两种天然L-氨基酸形成的天然L-氨基酸或二肽的残基，其中游离氨基可以被任何前述N-末端替代 保护团体 Y是氢原子或酪氨酸酚羟基的保护基; A是具有低级（硫代）烷基侧链的D-氨基酸残基; B是中性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 - 或三肽残基; 并且W是OH，OR，NH 2，NHR，N（R）2，NH-NH 2，其中R是1至7个碳原子的烷基，环烷基或芳烷基或NHNHR'，其中R'是氢原子，直链或 支链烷基，环烷基; 链烯基，直链或支链或环状脂族氨基甲酸酯基，通常用于多肽化学的芳族氨基甲酸酯基，α-氨基的残基; α-亚氨基或β-氨基酸，或二 - 或三肽残基，其中-NHR'键是酰胺键，氨基由N-末端保护基游离或保护。 肽具有中枢神经系统活性，可用作止痛药，精神药物和神经内分泌学。