201results about "Leech-based protease inhibitors" patented technology

The invention belongs to the technical field of polypeptide medicament preparation methods, and in particular relates to a preparation method for bivalirudin. The preparation method for the bivalirudin comprises solid phase polypeptide synthesis for preparing bivalirudin resin, acid hydrolysis of the bivalirudin resin to obtain a crude bivalirudin product, and purification of the crude bivalirudin product to obtain a purified bivalirudin product, wherein the solid phase polypeptide synthesis for preparing the bivalirudin resin comprises the following steps of: sequentially connecting corresponding Fmoc- protected amino acids in the following sequences to Fmoc-Leu-carrier resin by a solid phase coupling synthesis method: R1-D-Phe-Pro-Arg(Pbf)-Pro-X-Asn(R2)-Gly-Asp(OtBu)-, Phe-Glu(OtBu)-Glu(OtBu)-Ile-Pro-Glu(OtBu)-Glu(OtBu)- and Tyr(tBu)-Leu-resin, and thus obtaining the bivalirudin resin; and when the X fragment is connected, only one times of solid phase coupling synthesis reaction is used, and the corresponding Fmoc- protected amino acid is Fmoc-Gly-Gly-Gly-Gly-OH. The purity of the bivalirudin is more than 99.5 percent, and the single impurity is less than 0.2 percent.

The invention relates to methods for the preparation of highly purified peptides. The peptides are prepared in high optical purity of at least about 98.5%, and preferably at least about 99%. Specifically, Nesiritide (SEQ. ID NO. 1) having a purity of at least 99% as measured by HPLC and containing about 0.05% to about 0.5% [D-His]-Nesiritide (SEQ. ID NO. 1) as measured by chiral GC / MS.

An aliphatic polyester polymer for stent coating is described.

The invention discloses a preparation method of polypeptide solid-phase synthesis bivalirudin crude product. The preparation method comprises the following steps of: (1) mixing Fmoc-amino-acid resin or Fmoc-polypeptide resin and an unprotecting agent and removing Fmoc protecting group; (2) in the existence of a condensing agent, leading amino acid with Fmoc or Boc and amino acid or polypeptide onthe resin to carry out condensation; (3) repeating the step (1) and step (2) and obtaining polypeptide resin shown as formula II; and (4) in the existence of a cutting agent, leading the polypeptide and the resin on the polypeptide resin to be separated, and obtaining bivalirudin shown as formula I. The unprotecting agent contains 3 to 20 percent of piperidine and 0.5 to 10 percent of bicyclic amidine by total volume.

The present invention relates to a process for the production of bivalirudin, a 20-mer peptide of formula H-D-Phe1-Pro-Arg-Pro-Gly5-Gly-Gly-Gly-Asn-Gly10-Asp-Phe-Glu-Glu-lle15-Pro-Glu-Glu-Tyr-Leu20-OH (I) via a convergent five-fragment synthesis, and to several peptide intermediates thereof.

The complement system plays an important role in providing resistance to infections and in the pathogenesis of tissue injury. Yet an inappropriate activation of complement can result in a variety of disorders. The present invention provides C1s catalytic site-directed moieties, C1s exosite binding moieties, and bivalent polypeptide inhibitors comprising such moieties, which can be used to treat conditions characterized by inappropriate complement activation.

Aryl sulfonic pyridoxine compounds with inhibition of serine protease activity and antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related diseases are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxines.