Imperial Chemical Industries Limited

Zeneca Limited

Michael Brian Giles

Anand Swaroop Dutta

Ronald Cotton

David Timms

Barrington John Furr

A process for the solid phase synthesis of peptides containing a C-terminal aza-amino acid, for example the decapeptide goserelin, which comprises:

Process for making peptides

Compounds of the formula: ##STR1## wherein R.sup.1 stands for an alk-2-enyl radical of not more than 5 carbon atoms or a furylmethyl radical, R.sup.2 stands for an alk-2-enyl or alkyl radical of not more than 5 carbon atoms or a furylmethyl radical, &gt;N--A, B, D, E and F stand for defined amino acid or aza-amino-acid residues, and in particular one or both of B and D stand(s) for an amino acid residue of the formula --NH.C(1-3C alkyl)(1-3C alkyl).CO-- or a similar residue, and X stands for --OR.sup.7 or --NR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, stand for hydrogen or a (1-4C)alkyl radical, and wherein the linkages are all conventional peptide linkages or in the case of D-E the peptide linkage is replaced by the group --CH.sub.2 S--, and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutically-acceptable diluent or carrier. The compounds are selective opiate .delta.-receptor antagonists.

Peptide and pseudopeptide derivatives

The disclosure relates to novel polypeptides which are analogues of luliberin and which possess luliberin antagonist activity, to processes for their manufacture and to compositions containing them. Typical of the polypeptides disclosed is ##STR1## in which A is D-Phe, D-Trp or a direct bond.

Luliberin analogs

The disclosure relates to novel luliberin analogues which possess luliberin agonist activity, to processes for their manufacture and to compositions containing them. Typical of the peptides disclosed is ##STR1## in which A is D-Phe, D-Tyr(Me) or D-Ser(Bu.sup.t).

Growing community of inventors

Macclesfield, United Kingdom

Michael Brian Giles