Ferring Ab

Ferring B.v.

Jan-Ake Skoldback

Birgitta Mornstam

Krister Larsson

Jan Roschester

Thomas Mellbrand

Lars Henrik Andersson

Jens-Peter No Slashedrgaard

Ragner Asplund

A process for preparing and purifying cyclic peptides having disulfide moieties in a two step processing operation including reverse phase chromatography which simplifies synthesis and reduces production costs, yet produces high, quality yield. The improved process is particularly useful for the preparation of vasopressin and oxytocin and their respective derivatives and analogs.

Synthesis of cyclic peptides

A process for the manufacture of high purity desmopressin produced in single batches of substantial size and a method of treating nocturia, incontinence and enuresis with the high purity desmopressin produced therefrom.

Desmopressin for nocturia, incontinence and enuresis

A process for the manufacture of high purity desmopressin produced in single batches of substantial size and a method of treating diabetes insipidus with the high purity desmopressin produced therefrom.

High-purity desmopressin produced in large single batches

A process for preparing and purifying cyclic peptides having disulfide moieties in a single processing operation which simplifies synthesis and reduces production costs, yet produces high, quality yield. Higher yields are obtained by isolating the desired cyclic compound through direct ion exchange chromatography as an integral part of the single process. The improved process is particularly useful for the preparation of vasopressin and oxytocin and their respective derivatives and analogs.

High purity desmopressin produced in large single batches

A process for the manufacture of 1-deamino-8-D-arginine vasopressin (DDAVP) comprising, condensing a preparation of Mpa(R.sup.1)-Tyr-Phe-Gln-Asn-Cys(R.sup.2)-Pro-OH (SEQ ID NO: 1), where R.sup.1 and R.sup.2 are sulfhydryl-protecting groups, with the dipeptide (R.sup.3)-D-Arg(HCl)-Gly-NH.sub.2, where R.sup.3 is an acid-sensitive amino-protecting group, to form Mpa(R.sup.1)-Tyr-Phe-Gln-Asn-Cys(R.sup.2)-Pro-D-Arg(HCl)-Gly-NH.sub.2 (SEQ ID NO: 1), which is oxidized with iodine in a protic solvent. The reaction mixture containing the oxidized product can be purified by ion exchange chromatography on a cation exchange resin equilibrated with acid. Also disclosed is high-purity DDAVP obtained by this process and its use for treating diurea.

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Malmo, Sweden

Jan-Ake Skoldback