G.d. Searle & Company

James M Schlatter

Robert H Mazur

David A Jones, Jr

Donald W Hansen, Jr

Richard A Mikulec

Judith A Reuter

Arthur H Goldkamp

Owen Goodmonson

The invention relates to tetrapeptides of the formula I: ##STR1## which are useful as renin inhibition/antihypertensive agents.

Tetrapeptide amides in the treatment of hypertension

The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.

Enkephalin analogs

Methionine.sup.5 -enkephalin sulfoxides and sulfones having agonist activity at opiate receptors are disclosed herein. These sulfoxides and sulfones are useful as analgesics, non-addicting narcotic antagonists and anti-diarrheal agents.

Methionine.sup.5 -enkephalin sulfoxides and sulfones

An improved process for cleaving peptides bound to a polymer by way of a benzylester linkage during solid phase peptide synthesis, the improvement comprising hydrogenolysis of said linkage by catalytic hydrogenation using a palladium (II) salt with a weak acid anion as the catalyst.

Method for cleaving the peptide-resin bond in solid phase peptide

Analogs of methionine.sup.5 -enkephalin and leucine.sup.5 -enkephalin wherein the L-phenylalanyl residue in position 4 has been substituted by various other amino acid residues are disclosed herein. These analogs exhibit agonist activity at opiate receptor sites and are thus useful as analgesics, non-addicting narcotic antagonists and anti-diarrheal agents.

4-Substituted enkephalin derivatives

Fragments of secretin are disclosed herein. The compounds disclosed contain the amino acid fragments of secretin having the 1-15 amino acid sequence through those having the 1-19 amino acid sequence. Also disclosed are the above secretin fragments having a protecting group on the first amino acid. The compounds are useful as gastric antisecretory agents.

Fragments of secretin

Analogs of enkephalin having agonist activity at opiate receptors are disclosed herein. These analogs are useful as analgesics, non-addicting narcotic antagonists and anti-diarrheal agents.

2 AND 3-SUBSTITUTED ENKEPHALINS

3-Amino-N-substituted succinamic acids, prepared by coupling of a protected L-aspartic acid derivative with the appropriate amine followed by cleavage of the protecting groups, are potent sweetening agents and also exhibit pharmacological, e.g. anti-inflammatory, properties.

3-Amino-N-substituted succinamic acids

The above-captioned compounds, prepared by coupling of a protected L-aspartic acid derivative with the appropriate amine followed by cleavage of the protecting groups, are potent sweetening agents and exhibit also pharmacological, e.g. anti-inflammatory, properties.

3-Amino-N-substituted succinamic acids and intermediates thereto

Treatment of an alkyl ester of DL-phenylalanine with an N-acyl-D-phenylalanine results in the formation of the corresponding insoluble salt of L-phenylalanine alkyl ester and N-acyl-D-phenylalanine. The salt is purified by recrystallization in the presence of an added quantity of the alkyl ester of DL-phenylalanine or the alkyl ester of L-phenylalanine. The isolated, purified salt is decomposed to afford the desired L-phenylalanine alkyl ester, which is an important starting material in the preparation of artificial sweetening agents.

Growing community of inventors

Glenview, IL, United States of America

James M Schlatter