Hoechst Aktiengesellschaft

Heochst Aktiengesellschaft

Dominique Tripier

Paul Habermann

Peter Crause

Klaus Sauber

Gerhard Schmid

Wolfgang Ulmer

Martin Kramer

Arno Schulz

Rainer Obermeier

Klaus Bartsch

Gerhard Seipke

Gerd Johnscher

Laszlo Vertesy

Werner Bonin

Stefan Mullner

Max Hropot

Gunter Muller

Matthias Scharf

Joachim Engels

Jurgen Ludwig

Harald Ritzel

Werner Badziong

Elisabet Wohner

Hirudin derivatives can be prepared by the selective enzymic replacement of a part of the molecule with an amino derivative. The hirudin derivatives are suitable for preparing pharmaceuticals having an anticoagulatory effect.

Hirudin derivatives and a process for their preparation

Phosphoinositol-glycan-peptide with insulin-like action Phosphoinositol-glycan-peptides obtainable by cleavage of adenosine 3',5'-cyclic monophosphate-binding protein, which contain glucosamine, galactose, mannose, inositol, phosphoric acid, ethanolamine and a peptide with the sequence Asx-Cys-Tyr, the preparation and use thereof for the treatment of diabetes mellitus and non-insulin-dependent diabetes are described.

Phosphoinositol-glycan-peptide with insulin-like action

The invention relates to novel synthetic isohirudins which have improved stability owing to exchange in the region of the Asp-Gly motif. This results, on the one hand, in an increase in the yield during workup and, on the other hand, in making possible pharmaceutical formulation as directly injectable solution ready for use.

Synthetic isohirudins with improved stability

The present invention relates to hirudin derivatives which are formed from hirudin or the physiologically acceptable salt thereof and a carrier, to a process for the preparation thereof, and to the use thereof as thrombin inhibitor.

Hirudin derivatives with delayed action

Thrombin inhibitors from the hirudin family which differ from the previously known hirudins by mutation in the protein chain, and a process for their preparation are described. The novel hirudins are distinguished by a high specific activity, high stability and good pharmacokinetics.

Isohirudins

Novel synthetic isohirudins with improved stability The invention relates to novel synthetic isohirudins which have improved stability owing to exchange in the region of the Asp-Gly motif. This results, on the one hand, in an increase in the yield during workup and, on the other hand, in making possible pharmaceutical formulation as directly injectable solution ready for use.

A hirudin derivative which has the N-terminal amino acid sequence Leu-Thr-Tyr-Thr-Asp shows high biological activity. Moreover, this hirudin derivative can be obtained very efficiently by genetic engineering preparation in yeasts.

Hirudin derivative

A new transaminase has been isolated from E. coli DH-1 (ATCC 33849). It is possible to use the transaminase with great efficiency to prepare L-phosphinothricin and gamma-aminobutyric acid from appropriate precursors by transferring an amino group from glutamate.

Transaminase from E. coli DH-1 (ATCC 33849)

A process for the preparation of a purified transaminase having a molecular weight of 20,000 to 250,000 daltons, an isoelectric point at a pH between 3.0 and 8.0, a pH optimum in a range from 5.0 to 10.0 and a substrate specificity for the transamination of (3-carboxy-3-oxo-propyl)-methyl-phosphinic acid or the esters thereof. The production of the enzyme comprises cultivating E. coli ATCC 33849, disrupting the cultivated E. coli ATCC 33849, obtaining a supernatant therefrom containing the enzyme and isolating the transaminase by heating the supernatant at a temperature and for a time sufficient to denature proteins other than the transaminase and than finally removing the denatured proteins from the supernatant.

Process for producing transaminase from E. coli ATCC 33849

The invention relates to a process for the isolation and purification of hirudin from complex and salt-containing solutions by hydrophobic chromatography, using as stationary phase porous adsorber resins and as mobile phase organic solvents which are miscible with water.

Process for the isolation and purification of hirudin

The invention relates to a new active substance--amblyommin--for anticoagulant therapy and to a process for the isolation thereof from hard ticks. The isolated protein having a thrombin-inhibitory action has a molecular weight of 20000 to 30000 dalton, an isoelectric point between 5.05 and 5.65 and the partial amino acid sequences

Tick-derived amblyommin and method of antithrombin therapy

The invention relates to a polypeptide of the formula ##STR1## in which R represents phenoloic hydrogen or a phenolic ester group and m, n, X, Z, A, B, C, D, E, F, G, I and J have the meanings given, and in which the 6 Cys radicals are linked in pairs via disulfide bridges, processes for the preparation or isolation thereof, their use and agents containing them.

Novel polypeptides with a blood coagulation-inhibiting action, processes

The invention relates to polypeptides of the formula I ##STR1## in which m denotes 0-50, n denotes 0-100 and R denotes the phenolic hydrogen or a phenol ester group, X represents identical or different residues of naturally occurring .alpha.-amino acids, Y denotes Val, Ile, Thr, Leu or Phe, and Z represents identical or different residues of naturally occurring .alpha.-amino acids, and in which the Cys residues are linked pairwise via disulfide bridges, to a process for preparing or obtaining them and to agents containing them.

Polypeptides with an anticoagulant action, a process to prepare or

Cyclic polypeptides of the formula I ##STR1## in which Z, S, Y and AS have the meanings given, a process for their preparation and their use are described. The compounds have an .alpha.-amylase-inhibiting action.

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Eppstein/Taunus, Germany

Dominique Tripier