5 results about "Daclatasvir" patented technology

Compositions and treatment methods for cancer, such as enzalutamide resistant cancers, using one or more alternatives to daclatasvir (DCV). DCV has been shown to inhibit the Tribbles homolog 2 (TRIB2) pseudokinase encoded in humans by the TRIB2 gene, but more potent compounds are described herein that bind and inhibit the TRIB2 pseudokinase with greater affinity. TRIB2 is a target for several types of very aggressive cancers, such as castration resistant prostate cancer (CRPC), small cell lung cancer (SCLC), pancreatic neuroendocrine cancer (PNEC), triple negative breast cancer (TNBC), sarcomatoid kidney cancer, and melanoma.

The present invention discloses a method for detecting an antiviral component and an application thereof. The detection method can detect five antiviral components, namely, monolavir, oseltamivir, daclatasvir, nematevir and ritonavir, at one time, with high sensitivity, strong specificity and good repeatability. The detection limit concentration of the five representative components is about 0.3 μg / ml, and the quantitative limit concentration is about 1 μg / ml. In addition, the recovery rate and the recovery of the spiked product are good. The method is simple and suitable for the rapid detection of antiviral components in medicines, is beneficial to the supervision and inspection of antiviral medicines, ensures the drug safety of consumers, and has broad application prospects.

The RBC is the main host cell for Plasmodium falciparum. The release into the blood circulation is concomitant with an increase in infected RBC deformability allowing mature gametocytes to circulate through the spleen. The inventors showed that nine NS5A inhibitors display measurable IC50 on asexual stage of Plasmodium falciparum. Four of them have IC50 lower than 2 µM (ravidasvir, daclatasvir, velpatasvir, elbasvir). Ravidasvir, velpatasvir, and elbasvir are as effective on either P. falciparum artemisinin-sensitive (F-32TEM, NF54) and artemisinin-resistant (F32-ART) strains. Ravidasvir exhibits the widest therapeutic window: serum peak after a single dose of 200-300 mg (3.33 - 7.16 µM) compared to the IC50 (1.08-1.4 mM). Finally, there is a stiffening effect of ravidasvir on mature gametocytes of P. falciparum with an IC50 value= 0.99 µM. The present invention thus relates to the use of ravidasvir, velpatasvir, and elbasvir for blocking transmission of Plasmodium gametocytes.

The application discloses a synthesis method of daclatasvir hydrochloride. The daclatasvir hydrochloride is obtained from biphenyl as a starting material through a Friedel-Crafts acylation reaction, a condensation cyclization reaction, an amide hydrolysis reaction, a condensation reaction, salt formation and the like. The synthesis method has the advantages of low synthesis cost, simple post-treatment method, high yield, industrial production, reduced solvent and catalyst use, reduced reaction by-products and pollution, conformity to the development trend of green chemistry, maximized reduction of the production cost of the overall process and high application value.

The present invention discloses a detection method and application of ultra-high performance liquid chromatography-tandem mass spectrometry. The method of the present invention adopts ultra-high performance liquid chromatography-tandem mass spectrometry, first with 0.1% (V / V) formic acid aqueous solution and methanol as mobile phase gradient elution, and then in electrospray positive ion mode, using multiple reaction monitoring mode and secondary full scan analysis scanning. The linearity of three antiviral drug components, namatevir, monoclavir and daclatasvir, detected by the detection method of the present invention is good; the average recovery rate of spiked is 80% to 91.6%, and the precision is less than 5%. The method of the present invention is sensitive, rapid and reliable, and can be used for the qualitative and quantitative analysis of the drug components namatevir, monoclavir and daclatasvir in preparations.