摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
The present invention relates to a process for inactivating Carboxypeptidase Y (CPY) in a hirudin-containing culture broth produced by fermenting a transformed yeast. It has been found that inactive precursors of CPY are activated at a temperature 70.degree. C. and that the active peptidases will further degrade hirudin when the two proteins are present together in a composition. The present invention overcomes the CPY activation problem by heating a broth containing hirudin and CPY to a temperature of about 80.degree.-100.degree. C. in about one minute or less.
摘要:
Substituted thiophenesulfonylureas and -thioureas I ##STR1## wherein R(1) is selected from the group consisting of hydrogen, halogen, alkyl having 1 or 2 carbon atoms, alkoxy having 1 or 2 carbon atoms, mercaptoalkyl having 1 or 2 carbon atoms, fluoroalkoxy having 1 or 2 carbon atoms, and fluoroalkyl having 1 or 2 carbon atoms; R(2) is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms such as methyl, alkoxy having 1 or 2 carbon atoms, and trifluoromethyl; X is selected from the group consisting of oxygen (compounds Ia) or sulfur (compounds Ib); Y and Z are identical or different and are selected from the group consisting of hydrogen, F, Cl, Br, I, alkyl having 1 or 2 carbon atoms and alkoxy having 1 or 2 carbon atoms.