-4-[6-(purine-6-ylamino)hexanoyl]-3,4-dihydro-3-methyl-7,8-difluor-2h-[1,4]benzoxazine and (3r)-4-[6-(purine-6-ylamino)hexanoyl]-3,4-dihydro-3-methyl-7,8-difluor-2h-[1,4]benzoxazine with antiviral activity

FIELD: pharmacology.

SUBSTANCE: invention relates to new purine derivatives of the formulas: .

EFFECT: new derivatives possessing selective antiviral activity against herpes simplex viruses 1 and acting on viral strains with drug resistance to acyclovir and related compounds are obtained.

3 cl, 1 tbl, 3 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: co-crystals possess firstly the anti-inflammatory, antipyretic and analgesic action and are applicable to produce pharmaceutical preparations. The co-crystal of diflunisal and theophylline has an endothermal peak from 183 to 195°C according to the measured data by differential scanning calorimetry and peaks at 2θ(°) 5.2, 10.3, 11.9, 18.18, 23.5, 26.4 according to the measured data of X-ray powder diffraction, while the co-crystalline form of diclofenac and theophylline has an endothermal peak from 186 to 198°C according to the measured data by differential scanning calorimetry and peaks at 2θ(°) 7.6, 12.2, 16.7, 17.4, 20.1, 27.0 according to the measured data of X-ray powder diffraction. The co-crystals can be presented in the solid phase and in the solution.

EFFECT: co-crystal enables increasing water-solubility for diflunisal and for diclofenac as compared to the unformulated solubility.

12 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to cyclohexylammonium salt of [3-methyl-1-n-propyl-7-(1-oxothietanyl-3)xanthinyl-8-thio]acetic acid of formula .

EFFECT: what is prepared and described is a new compound which can find application in medicine as an antiaggregation and anticoagulation agent.

3 cl, 2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention relates to a benzylammonium and cyclohexylammonium salt of [3-methyl-1-n-propyl-7-(1,1-dioxothietanyl-3)xanthinyl-8-thio]acetic acid of formula Ia,b, where B+=H3N+-CH2 (la), H3N+) (Ib).

EFFECT: novel compounds which can be used in medicine as proaggregant agents are obtained and described.

4 cl, 1 tbl, 4 ex

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of xanthine of the formula (I): possessing inhibitory effect on activity of phosphoenolpyruvate carboxykinase. In compound of the formula (I) R1 is chosen from group consisting of lower alkenyl, lower alkynyl, lower alkenyl substituted with halogen atom, phenyl and phenyl substituted with one or two substitutes chosen independently from group comprising halogen atom, hydroxy-group, lower alkoxy-group, nitro-group, amino-group or 5- or 6-membered aromatic heterocyclic ring comprising 1, 2, 3 or 4 nitrogen atoms added to phenyl by ring carbon atom; R2 is chosen from group comprising unsubstituted lower alkyl, lower alkyl substituted with lower alkoxy-group or hydroxy-group, lower alkenyl, phenyl, -(CH2)n-unsubstituted lower cycloalkyl and -(CH2)n-lower cycloalkyl substituted with at least one substitute chosen from group comprising carboxy-group, lower alkyl, carboxy-lower alkyl and lower alkyl substituted with hydroxy-group, -(CH2)n-C(O)Rb wherein Rb is chosen from group comprising hydroxyl, lower alkoxy-group, hydrogen atom, benzyl, lower alkyl and -NHRb wherein Rb is chosen from group comprising lower alkoxy-group, -NHRc wherein Rc is chosen from group comprising hydrogen atom, benzyl, lower alkyl and -NHRd wherein Rd is chosen from group comprising hydrogen atom and carboxy-lower alkyl; -(CH2)n-unsubstituted aromatic 5-membered heterocyclic ring comprising one oxygen or sulfur atom, -(CH2)-aromatic 5-membered heterocyclic ring comprising one oxygen or sulfur atom wherein ring is substituted with carboxylic acid residue, -(CH2)n-unsubstituted aromatic 5-membered heterocyclic ring comprising 1, 2 or 3 nitrogen atoms, -(CH)n-nonaromatic 5- or 6-membered heterocyclic ring comprising at least one oxygen atom and two nitrogen atoms or not comprising nitrogen atoms wherein nonaromatic heterocyclic ring has no substitutes or comprises one ring carbon atom as carbonyl, and wherein R3 means: and others. Also, invention relates to pharmaceutically acceptable salts of compounds, pharmaceutical composition based on thereof, using and inhibition of activity of PEPCK.

EFFECT: improved method of synthesis, valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

32 cl, 1 tbl, 125 ex

The invention relates to new compounds of formula I and Ia in all their stereoisomeric forms or their mixtures in all ratios, and their pharmaceutically acceptable salts, which has antagonistic activity against vitronectin receptor

The invention relates to new derivatives of purine of formula I, II, III and IV, pharmaceutical compositions and method of treatment of a pathological state characterized by thrombotic activity

The invention relates to new derivatives of substituted purine with immune modulating, in particular immunostimulatory activity in vivo and in vitro and does not exhibit toxicity, to pharmaceutical compositions and method of slowing tumor growth

The invention relates to medicine and organic chemistry and relates to the problem of creating new drugs, inhibiting the proliferation of lymphocytes

The invention relates to analogues of nucleosides dimethoxyaniline

The invention relates to a method for producing analogues of nucleosides dimethoxyaniline

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to biotechnology. There are presented a vaccine composition containing Bordetella bronchiseptica and a recovered pertactin antigen, and the use of the vaccine composition for treating and preventing a complex of infectious respiratory diseases in dogs. The presented vaccine containing a combination of a bacterin or a bacterial extract of Bordetella bronchiseptica and the recovered protein pertactin enables preventing the complex of infectious respiratory diseases in dogs caused both by Bordetella bronchiseptica, and such pathogens, as the canine parainfluenza virus, canine adenovirus-2, canine respiratory coronavirus and canine influenza virus.

EFFECT: vaccine composition can be used to prevent and treat the above infections in veterinary science.

16 cl, 4 tbl, 5 ex

FIELD: pharmacology.

SUBSTANCE: invention relates to the field of pharmaceutical industry, specifically to a new derivative of 1,3-adamantandiacetic acid with amino acid residue of ethyl alcohol of threonine of the formula specified below. The compound may be used to create new anti-virus preparations. .

EFFECT: compound has selective anti-virus activity in respect to virus of flu A and acts at strains resistant to effect of remantadin hydrochloride.

2 cl, 3 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: presented invention refers to immunology. There are presented versions of antibodies neutralising a subtype group 1 and subtype group 2 influenza A virus infection. The antibody is characterised by: either a set of 3 CDR of a light and 3 CDR of a heavy chain, or the presence of variable regions of the light and heavy chains. There are disclosed: a nucleic acid molecule coding the antibody; a cell expressing the antibody; as well as a method for the attenuation of the influenza A virus infection or reducing a risk thereof with the use of the antibody in a therapeutically or preventatively effective amount.

EFFECT: using the invention provides the antibodies neutralising the influenza A virus, which can find application in medicine in treating subtypes H1, H2, H3, H5, H7, H9 influenza.

18 cl, 6 tbl, 2 ex

FIELD: biotechnology.

SUBSTANCE: strain of bacteria Serratia plymuthica B-1288, a strain of bacteria Serratia plymuthica B-1297, a strain of bacteria Serratia plymuthica B-1296 and a strain of bacteria Serratia plymuthica B-1285 are proposed. These strains are deposited in the collection of bacteria, bacteriophages and fungi of the Federal State Institution of Science "State Research Centre of Virology and Biotechnology "Vector". When using the preparations on the basis of the proposed strains the neutralisation index of influenza virus o type A is 2.5-6.5 lg with the initial concentration of the virus of 102.5-6.5 lg TCD50/ml.

EFFECT: strains have antiviral activity against influenza virus of type A.

4 cl, 5 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to immunology, and can be used for preventing influenza. That is ensured by combined single administration of cytokine that is ensured by interferon gamma, and an inactivated anti-influenza vaccine. Interferon gamma is administered intermuscularly or subcutaneously in a dose of 0.5 ml 100,000 International Units±10% into the upper one-third of one shoulder; then the inactivated anti-influenza vaccine 0.5ml based on vaccine influenza viral strains (H5N1) Orniflue containing heamagglutinin in a minimum dose of 15 mcg/dose for this vaccine is administered intramuscularly into the upper one-third of the other shoulder.

EFFECT: method enables increasing immunogenicity and protective activity of the vaccine ensured by single vaccination and reducing side effects on the antigen by the immune response modulation.

9 tbl, 1 ex

Antiviral agent // 2542488

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to an antiviral agent and aims at inactivating a wide range of viruses. The antiviral agent contains an active agent presented by particles of at least one type of iodide formed by iodine and an element formed in 4-6th periods of the 8-10th or 12-15th groups of the periodic table, Cu or Au. The above element found in the 4-6th periods of the 8-10th or 12-15th groups of the periodic table represents Sb, Ir, Ge, Sn, Tl, Pt, Pd, Bi, Fe, Co, Ni, Zn, In or Hg. What is also presented is the antiviral agent containing particles of at least one type of a cuprous compound as an active ingredient. The above cuprous compound represents chloride, acetate, sulphide, iodide, bromide, peroxide, oxide or thiocyanide.

EFFECT: using the group of inventions provides the agent having the high antiviral activity; the above agent is able to exhibit and maintain its antiviral activity easily since it requires no preparation or special washing.

5 cl, 4 tbl, 27 ex

FIELD: medicine.

SUBSTANCE: invention represents a drug preparation for treating influenza and respiratory viral infections containing 3,3-diindolylmethane, cod liver oil type A and Polysorbate 80 in the following proportions, wt %: 3,3-diindolylmethane 9-20, cod liver oil type A 1-10, Polysorbate 80 - the rest. The invention also concerns using this drug preparation for treating influenza and respiratory viral infections.

EFFECT: higher clinical effectiveness.

3 cl, 2 dwg, 7 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to virology and implies using the similar mini-antibodies for the prevention and therapy of influenza. What is declared is a similar mini-antibody specifically binding to a certain epitope of influenza A (H5N2) hemagglutinin and suppressing the influenza A (H5N2) infection. What is created is an adenovirus viral vector expressing the similar mini-antibody, which can effectively bind to the certain epitope of influenza hemagglutinin and thereby block the influenza progression. What is presented is a composition containing an effective amount of the similar mini-antibody and the viral vector expressing this similar mini-antibody.

EFFECT: what is presented is a method for the prevention and therapy of the influenza A (H5N2) infection providing administering the preventive or therapeutic effective amount of the pharmaceutical composition intranasally in the form of drops or spray into the patient in need thereof.

9 cl, 10 dwg, 2 tbl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to biotechnology and virology. An influenza virus contains 6 internal genome segments of one or more virus donors and genome segments coding an NA polypeptide, and the NA polypeptide. The NA polypeptide comprises the amino acid sequence SEQ ID NO:6. There are also described immunogenic composition and vaccine containing the above virus, as well as using it for preparing a therapeutic agent. The invention can be used in medicine.

EFFECT: what is described is an influenza reassortant virus.

16 cl, 4 dwg, 3 tbl

FIELD: medicine.

SUBSTANCE: chicken embryos are infected; a virus-containing allantoic fluid (VAF) is collected, and the VAF is purified by microfiltration. The VAF is purified with the use of polyethylene glycol of the molecular weight of 6000 in the concentration of 1.5% and microfiltered on depth filters having pore diameters of 1.0 mcm and 10.0 mcm. Further, the purified VAF is concentrated by ultrafiltration on membranes with the molecular weight cut 100 kD, and the prepared concentrate is purified in a sucrose gradient by ultracentrifugation.

EFFECT: using the method enables the higher quality of virion purification, as well as the higher number of viral antigens recovered from one chicken embryo.

1 tbl, 1 dwg, 6 ex

FIELD: medicine.

SUBSTANCE: method involves removing an epithelial layer, exposing a cornea by saturating it through multiple instillations of 0.1% riboflavin followed by the ultraviolet exposure. After the epithelial layer has been removed, a ring made of an ultraviolet-protected contact lens is applied on a surface of the eyeball perilimbally. An outer diameter of the ring covers the limb by no more than 2 mm, whereas an inner diameter of the ring is equal to a basic diameter of the keratoconus. The whole duration of the ultraviolet exposure involves additional instillations of riboflavin on the cornea every 3-4 minutes. The exposure is characterised by wavelength 365 nm, power 3.0 mWt/cm2 at 50 mm for 30 minutes with the ring to be removed after the exposure is completed.

EFFECT: method is easy to implement, involves no difficulties for specialists, providing higher clinical effectiveness by limiting the ultraviolet exposure area, preventing the ultraviolet involvement of the limb and reducing a risk of postoperative complications.

1 ex

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