Usv Pharmaceutical Corporation

Rorer Pharmaceutical Corporation

Armour Pharmaceutical Company

David Stevenson

Laurence L Ho

Robert C Liu

John T Suh

Edward S Neiss

Howard Jones

Everett Flanigan

Charles D Bossinger

Stephen M Coutts

Mohammad A Islam

Karl Lederis

Donald B Olsen

New peptides are disclosed which have biological activity of the same type as known calcitonins and which are amide analogs of natural calcitonins.

Amide analogs of calcitonin

Peptides, such as calcitonin, having two cysteine residues connected by a disulfide bond are prepared by a process which includes the step of cyclizing the cysteines at a pH of 8.5 to 9.0, and a concentration of 0.4 to 1.8 mg of peptide per ml of solution. These novel conditions produce rapid cyclization with an unforeseen improvement in yield.

Process for the preparation and purification of peptides

Compounds of the structure ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sub.1 and R.sub.2 are independently H, OH, lower alkyl, lower alkoxy, aryloxy, heteroaryloxy, heteroaryl lower alkoxy, aryl, heteroaryl, aryl-lower alkyl, aryl-lower alkoxy, halogenated aryl-lower alkoxy, lower alkenyl, lower alkynyl, lower alkenoxy, lower alkynoxy, halogen or trifluoromethyl;

Phenylacetamides as anti-allergy, anti-asthma and anti-inflammatory

The yield of peptide synthesis processes of the type in which a protected intermediate resin peptide of the formula Resin--CH.sub.2 --O--Phe--X, Resin--CH.sub.2 --O--Gly--X, Resin--CH.sub.2 --O--Ala--X, or Resin--CH.sub.2 --O--Leu--X is deprotected, and successively protected amino acids are coupled to the resin peptide and deprotected, is increased significantly by deprotecting the first residue with trifluoroacetic acid and deprotecting the other residues with hydrogen chloride.

Synthesis of hormone fragments

Antihypertensive polypeptides

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Scarsdale, NY, United States of America

David Stevenson