42 results about "Teriparatide" patented technology

The present invention relates to a novel method for purifying teriparatide, a therapeutically active polypeptide fragment of full-length human parathyroid hormone. The method is based on ion exchange chromatography and is effective in separating the therapeutically active polypeptide from undesirable variants, such as truncated polypeptides. The method of the invention can be used at a preparative scale which allows it to be implemented into the production process for teriparatide. Accordingly, the invention also provides a method for the production of teriparatide which includes a step in which teriparatide is purified by the novel ion exchange chromatography method of the invention.

The invention discloses novel parathyroid hormone (PTH) (1-34) mimetic peptide based on protein domain reconstruction.; The mimetic peptide contains peptide fragment repeats at 29-34th positions, andthe 34th position of the mimetic peptide and the last amino acid of the peptide fragment repeats at 29-34th positions are changed into tyrosine (Tyr, Y) from phenylalanine (Phe, F), so that MY-3 peptide is formed; preclinical experiments show that the MY-3 mimetic peptide can promote osteoblast differentiation, and has a very good effect of treating osteoporosis and promoting bone growth; the anti-osteoporosis effect of the MY-3 mimetic peptide is better than that of the PTH (1-34) (a product on the market is named as Forteo or Teriparatide), so that the MY-3 mimetic peptide has a significantclinical application prospect.

The present invention relates to an oral pharmaceutical composition and a preparation method therefor, the oral pharmaceutical composition comprising an ionic bond complex consisting of teriparatide, deoxycholic acid, N [alpha]-deoxycholyl-L-lysyl methyl ester (N [alpha]-deoxycholyl-L-lysyl methyl ester, DCK), and D-[alpha]-tocopherol polyethylene glycol 1000 succinate (D-[alpha]-tocopherol polyethylene glycol 1000 succinate), the ionic bond complex comprising at least one compound selected from the group consisting of N [alpha]-deoxycholyl-L-lysyl methyl ester, N [alpha]-tocopherol polyethylene glycol 1000 succinate, N [alpha]-tocopherol polyethylene glycol 1000 succinate, N [alpha]-tocopherol polyethylene glycol 1000 succinate, N [alpha]-tocopherol polyethylene glycol 1000 succinate, N [alpha]- The oral pharmaceutical composition provided by the invention can improve the intestinal mucosa permeability and oral administration bioavailability of teriparatide and improve patient compliance, and can be used for treating osteoporosis.

The invention relates to the field of medicine synthesis, and discloses a method for synthesizing teriparatide. The method comprises the following steps: performing esterification reaction between Phe coupled with a protecting group at an N end and HMP Linker resin under the action of a coupling reagent and an activating reagent to obtain peptide resin 1; and performing one-by-one extension coupling on the rest protective amino acids under the reaction of a condensation reagent and an activating reagent according to a sequence from a C end to the N end of a teriparatide amino acid sequence to obtain corresponding peptide resin after each extension coupling and finally obtain teriparatide resin, performing acid hydrolysis to obtain a teriparatide crude product, and purifying the teriparatide crude product into acetate so as to obtain a teriparatide pure product. According to the method disclosed by the invention, a suitable synthesis scheme is selected, the HMP Linker resin is used as carrier resin, the whole synthesis process is optimized, a high-purity product is obtained, the total yield of the teriparatide is improved, and the method is harmless to any environment.

The present invention relates to a method for preparing teriparatide. The specific steps of the present invention are: A) in the presence of an activator system, coupling the resin solid phase carrier and Fmoc-Phe-OH to obtain Fmoc-Phe-resin; B ) Through the solid-phase synthesis method, amino acids with N-terminal Fmoc protection and side chain protection are sequentially coupled according to the peptide sequence of the teriparatide main chain. The amino acid at position 16-17 of the peptide sequence is a pseudo-proline dipeptide Fmoc-Asn ( Trt)-Ser(ψMe,Me Pro)-OH replaces the original two amino acids at 16-17 positions for coupling; C) Peptide resin cleavage uses NH-containing 4 I / Me 2 The lysate of the TFA system of S, the crude product was purified by HPLC and freeze-dried to obtain teriparatide, whose process impurity Met 8 (O)‑Teriparatide content is less than 0.1%. The invention provides a teriparatide preparation process with high purity, low cost and suitable for large-scale production. This process can effectively control Met 8 (O)-Teriparatide content does not affect the overall yield of teriparatide.

The invention relates to the application of higenamine hydrochloride in the preparation of medicines for treating osteoporosis, and belongs to the technical field of chemical medicine development. The present invention discovers for the first time that higenamine hydrochloride can target IQGAP1 protein, activate Smad2 / 3 pathway, promote Smad2 / 3 phosphorylation, thereby promoting osteogenic differentiation, and has the potential to become a new drug for treating osteoporosis. At present, the clinical treatment of osteoporosis is mainly based on anti-bone resorption drugs: such as bisphosphonates, etc., but with the different causes of osteoporosis and the development of the disease course, simple anti-bone resorption drugs can no longer meet the needs of patients , and the only bone-promoting drug, teriparatide, has long-term osteosarcoma risk and other side effects and limitations, while higenamine hydrochloride has the characteristics of oral and injectable, small side effects, and obvious osteogenesis-promoting effect. Treating osteoporosis offers new options.