Biologically active peptides

专利名称：Biologically active peptides发明人：Roberto de Castiglione,Fiorenzo

Faoro,Giuseppe Perseo,SilvanoPiani,Francesco Santangelo

申请号：US06/212586申请日：19801203公开号：US04350627A公开日：19820921

摘要：There is disclosed biologically active peptides of the formula ##STR1## where Xis a hydrogen atom, an N-terminus protecting group (any of an acyl-type protectinggroup, an aromatic urethane-type protecting group, an alkyl- type protecting group, oran alkyl urethane type protecting group), or a residue of a natural L-amino acid or adipeptide formed of two natural L-amino acids, wherein the free amino group may bereplaced by any of the foregoing N- terminus protecting groups;

Y is a hydrogen atom or a protecting group for the phenolic hydroxyl group oftyrosine;

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 acidresidue;

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, cycloalkylor 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, aresidue of an &agr;-amino; &agr;-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 byan N- terminus protecting group. The peptides have central nervous system activity andare useful as analgesics, psychotics, and neuroendocrinologicals.

申请人：FARMITALIA CARLO ERBA S.P.A.

代理机构：Stevens, Davis, Miller & Mosher

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