Ciba-geigy Corporation

Ucp Gen-pharma Ag

Werner Rittel

Bruno Kamber

Peter Sieber

Bernhard Riniker

Max Brugger

Hendrik M Greven

Albert Hartmann

Hans Rink

Hans Fritz

Sefik Alkan

Manfred Liersch

Leo Geller

Francois Meyer

Robert Neher

Walter M&auml;rki

Friedrich Werner Kahnt

Ursula Seem&uuml;ller

Herbert Zuber

The invention relates to DNA sequences which code an eglin, expression plasmids containing such DNA sequences, hosts transformed with such expression plasmids, novel eglin compounds produced from such transformed hosts, monoclonal antibodies against eglins, hybridoma cells which produce such antibodies, and test kits for immunoassays containing such antibodies, and furthermore the processes for their preparation and a process for the preparation of eglins with the aid of the transformed hosts. The eglins which can be prepared according to the invention have useful pharmacological properties.

Process for preparing recombinant eglin, protease inhibitor

The invention concerns an improved process for the manufacture of cystine-containing peptides from cysteine-containing aminoacid sequences whose mercapto groups are protected by trityl groups, wherein the S-trityl cysteine-containing sequences are directly oxidized with iodine to yield the cystine disulfide bond.

Process for the manufacture of cystine-containing peptides

The new hypocalcaemically active peptides of formula I ##STR1## and corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.

Peptides and process for their manufacture

Process for the manufacture of peptides which contain more than one disulphide bond characterized in that in one or two aminoacid sequences containing cysteine, in which disulphide bonds are to be produced, two cysteine radicals which are to be linked are protected by a mercapto-protective group R.sub.1 of the aralkyl type, two further cysteine radicals are protected by an acylaminomethyl group R.sub.2, the protective groups R.sub.1 are removed by treatment with iodine in the presence of a polyhalogenated lower aliphatic hydroxy compound or oxo compound, or a corresponding lower alkanoic acid lower alkyl ester, at the same time forming the disulphide bond between these cysteine radicals, which are protected by R.sub.1, and at any desired point after removal of the polyhalogenated compound the second disulphide bridge is formed in the usual manner.

Process for the manufacture of peptides containing cystine

Synthetic hypocalcaemic dotriacontapeptide of the formula

Hypocalcaemic peptides and processes for their manufacture

Pharmaceutical preparations containing acid addition salts of ACTH-peptides with saturated or unsaturated fatty acids of chain length 12-36 carbon atoms.

Salts of ACTH-peptides and processes for their manufacture

Peptides of the calcitonin type when obtained by synthesis can be purified in a simple manner by forming inner salts, which precipitate from aqueous solutions of salts of the peptides with acids or bases when these solutions are adjusted to the isoelectric range. Impurities remain in solution, while the inner salts separate practically quantitatively. The precipitation is completed after several hours. The peptides can then be recuperated by treatment with an acid, especially a therapeutically suitable acid. The process affords products which are superior to those obtained by purification methods hitherto known and gives higher yields. Other long-chain peptides such as ACTH, insulin or glucagon cannot be purified in this manner.

Process for the purification of synthetic calcitonins

The new hypocalcaemically active peptides of formula I

Growing community of inventors

Basel, Switzerland

Werner Rittel