40 results about "Peramivir" patented technology

The present invention provides a dual release solid dosage form containing a first composition that releases a neuraminidase inhibitor, such as oseltamivir, zanamivir, or peramivir, in a controlled manner and a second composition that releases an H1 antagonist in a rapid and / or immediate manner. A wide range of H1 antagonist antihistamines, especially fexofenadine and loratadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. The device is useful for the treatment of respiratory congestion and other viral infection associated symptoms.

The present invention relates to a novel process for preparing peramivir formula (I) or a pharmaceutically acceptable salt thereof, and to intermediates used therein.

The invention relates to a peramivir solution inhalation and a preparation method thereof, wherein the solution inhalation is made of peramivir, an osmotic pressure regulator, a pH regulator and water, wherein the concentration of peramivir Greater than 15 mg / ml, the concentration of the osmotic pressure regulator is less than 8 mg / ml, the pH value of the solution-type inhalation is 5.0-6.0, and no heat sterilization is used, and the osmotic pressure regulator is selected from sodium chloride or glucose . The solution-type inhalation has better stability and excellent lung-targeting effect, which significantly improves the effectiveness and safety of the drug.

The invention discloses a method for detecting a peramivir intermediate I by reversed-phase high performance liquid chromatography. The method comprises the following steps: preparing a test sample solution, detecting a test sample by reversed-phase high performance liquid chromatography, and calculating the contents of single impurities and total impurities in the test sample according to an area normalization method. According to the method, the intermediate I is completely separated from chromatographic peaks of various impurities by changing a mobile phase, a ratio, the wavelength of an ultraviolet absorption detector and the like; and the detection time is short, the detection specificity, accuracy and sensitivity are high, and more accurate detection and quality control can be carried out on the peramivir intermediate I.

The invention discloses a preparation method of a key intermediate (3aR, 4R, 6S, 6As)-4-[[(1, 2, 3, 4-triazole-3-yl)-1, 3, 4-triazole-3-yl]-1, 3, 4-triazole-3- The invention relates to a synthesis method of (1S, 4R)-(-)-[[(1, 1-dimethyl ethyoxyl) carbonyl] amino]-3-(1 '-ethyl propyl)-3a, 5, 6, 6a-tetrahydro-4H-cyclopenta [d] isoxazole-6-carboxylic acid methyl ester, which comprises the following steps: taking (1S, 4R)-(-)-[[(1, 1-dimethyl ethyoxyl) carbonyl] amino] cyclopent-2-ene-1-carboxylic acid methyl ester as an initial raw material; the preparation method comprises the following steps: under the catalysis of triethylamine, carrying out cyclization reaction on (3aR, 4R, 6S, 6As)-4-[[(1, 2, 4-triazine-2-yl)-1, 3-diketone]-1, 3-diketone and a toluene solution containing 2-ethyl-N-hydroxybutyrimidyl chloride, and directly obtaining (3aR, 4R, 6S, 6As)-4-[[(1, 2, 4-triazine-2-yl)-1, 3-diketone]-1, 3-diketone through solvent treatment, impurity removal and Compared with the prior art, the preparation method disclosed by the invention has the advantages that the yield is high, the operation is safe and simple, the purity of a finished product is high, and industrial large-scale production is convenient to realize. The preparation method disclosed by the invention has the advantages that the preparation method disclosed by the invention can be used for preparing the 3-(1, 1-dimethyl ethyoxyl) carbonyl] amino]-3-(1 '-ethyl propyl)-3a, 5, 6, 6a-tetrahydro-4H-cyclopenta [d] isoxazole-6-carboxylic acid methyl ester.

A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

The invention discloses an application of peramivir in preparing a medicine for treating an inflammatory storm caused by an infectious disease, wherein the infectious disease is an infection caused by a virus, chlamydia, mycoplasma, bacteria or parasite, and the inflammatory storm is Infectious diseases cause the rapid and massive production of various cytokines in the body, and the various cytokines in the body are TNFα, IL-6, IL-1β, IL-12, IFNα and IFN-γ. The present invention proves for the first time that peramivir has the effect of treating inflammatory storm caused by infectious disease, can be used for preparing the therapeutic drug for inflammatory storm caused by infectious disease, and provides a new anti-inflammatory scheme for clinical treatment.

The invention relates to a synthesis method of peramivir trihydrate, an anti-influenza medicine. The present invention uses (3aR,4R,6S,6aS)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3-(1'-ethylpropyl)-3a,5, 6,6a-tetrahydro-4H-cyclopenta[d]isoxazole-6-carboxylic acid 1,1-dimethylethylammonium (compound I, prepared by referring to CN101367750B method) as raw material, through five steps Synthetic procedure Preparation of peramivir trihydrate. Compared with the methods reported in existing documents, the present invention designs a shorter, more effective and practical process route, and the total yield of finished product preparation is significantly improved.

The invention discloses a synthesis method of a 3+2 closed ring. According to the method, chiral induction is enhanced under the spatial steric effect of bridge ring molecules, so that a ring closingreaction has efficient spatial selectivity. The method is applied to synthesis of peramivir and has the characteristics that the synthesis route is short, the stereoselectivity is high and the operation procedure is convenient.

The invention relates to an anhydrous peramivir crystal compound and a preparation method thereof, and further discloses a pharmaceutical composition comprising the same and the application thereof in the preparation of medicaments for treating the influenza virus and the Avian influenza virus.

The invention provides a peramivir hydrate crystal, a preparation method for the crystal, a medical compound containing the crystal and the application of the crystal in preparing the drugs for resisting influenza virus. The structural formula of the peramivir is shown in the description.

The present invention relates to a method for producing peramivir trihydrate, which is an inhibitor of neuraminidase infection, as an anti-influenza agent. According to the production method of the present invention, peramivir trihydrate can be produced with high yield and stability through a process suitable for producing excellent pharmaceuticals and quality control standards (GMP) without using highly-toxic methanol and activated carbon.

The invention discloses a new method for preparing a peramivir key intermediate. According to the new method for preparing the peramivir key intermediate, an intermediate (II) is taken as a raw material; and after reductive ring opening, post-processing of a reaction system is not required, and an acetylating agent is added by a one-pot method so as to obtain a peramivir intermediate (I) (1S, 2S, 3S, 4R, 1'S)-3-(1-acetamido-2-ethylbutyl)-4-(Boc)-amino-2-hydroxy-cyclopentane-1-carboxylate. Through the adoption of the method, a middle complicated post-processing process is omitted and the acetylating agent is directly used for quenching and acetylating, so that the method is simple in operation and the yield is greater than 80%.