Immunomodulatory and anti-infectious composition

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics. A composition contains nanosized silver powder, nanosized aluminium powder and nanosized diamond powder in the following proportions, wt %: nanosized silver powder - 40, aluminium powder -30, nanosized diamond powder -30.

EFFECT: composition shows a combined immunomodulatory and antibacterial effect, low toxicity.

3 tbl, 1 ex

 

The invention relates to compositions having biological activity, in particular immunomodulatory and antibacterial properties, and can be used in medical and veterinary practice for the treatment and prevention of infectious diseases, accompanied by changes in the immune status of the organism.

Known patent RU No. 2203068, publ. 27.04.2003, "Biologically active ultradispersed diamonds of detonation synthesis", which has antitumor activity in the absence of adverse toxic effects (substance to treat class 4 toxicity). The disadvantage of this arrangement is the lack of antibacterial activity.

The famous "Biologically active agent" (patent RU №2123329, publ. 20.12.1998), representing a mixture of ultrafine powders of heavy metals: (UDP) copper, silver, platinum, iron, zinc. The purpose of this tool is closest to the claimed composition and selected as a prototype.

The disadvantage of the prototype is that it has toxic side effects on the body, primarily immunotoxic effect.

An object of the invention is to develop new effective compositions involving nanosized powders of diamond, aluminum and silver, and with increased biological activity, and is about obtaining low-toxic drug, have immunomodulatory properties in combination with antibacterial activity.

The problem is solved by using not previously used compositions, namely nanosized silver powder (particle size of 80-100 nm), nano-diamond powder (particle size 4-7 nm) and nano aluminium powder (particle size of 80-100 nm) in a quantitative ratio, wt.%: 40:30:30.

The composition is selected based on the specifics of the biological activity of the components.

Example. Nanosized powder of silver 0.4 g mixed with nano-sized powder of aluminum in the amount of 0.3 g and nano-size diamond powder in the amount of 0.3 g Of the obtained mixture to prepare a suspension in 100 ml of distilled water.

Freshly prepared according to the example of the suspension was used to test the reaction of blast transformation of human lymphocytes (rbtl).

With this purpose, conducted the analysis of the action of drugs on immune cells stimulated by phytohemagglutinin (PHA) after the action of drugs in the concentration range from 0.001 to 1 mg/ml assessing the impact of drugs on lymphocyte proliferative activity in spontaneous and induced PHA test conducted in accordance with the methodological recommendations of farmkomiteta of the RF Ministry of health (Vedomosti of the pharmacological Committee, 1999, No. 1).

The result of the testing of drugs in the reaction rbtl presented in table 1.

The testing established that the claimed composition does not have a dampening effect on PHA induced lymphocyte proliferative activity. From table 1 we see that the claimed composition in all investigated concentrations, has a stimulating effect on the activity of lymphocytes in the test spontaneous proliferation (without the stimulus impact PHA) in comparison with the prototype.

Freshly prepared according to example suspension was used to study the antibacterial activity of the claimed composition. Antibacterial activity was determined by serial dilution method in bacterial cultures at a concentration of 1.0 mg/ml, 0.5 mg/ml and 0.1 mg/ml the results of the experiments after 24 hours the growth of microorganisms at 37°C are presented in table 2. From the table it follows that the claimed composition has a strong bactericidal effect on microorganisms, causing 100% mortality.

Studies the influence of the composition (freshly prepared in example suspension) on the functional activity of polymorphonuclear leukocytes in the peripheral blood of donors in a wide range of concentrations. Used are known from the literature, the modeling technique of phagocytosis using Staphylococcus aureus N-209 (D.K. Novikov, V.N. Novikov. Assessment of immune status. Moscow Is-Vitebsk 1996, 281 C.). Counts the percentage of active neutrophils (PAN), the percentage of completed phagocytosis (NRF) in the control test without the influence of drugs and adsorption capacity of neutrophils. The results are presented in table 3, which shows that in the area studied concentrations after exposure of the composition increases the percentage of completed phagocytosis, the percentage of active neutrophils and phagocytic activity in comparison with the prototype.

Table No. 1
Immunomodulatory and anti-infective composition
Dose, mg/mlSpontaneous proliferationProliferation with phytohemagglutinin (PHA)
The placeholderTrackThe placeholderTrack
control779494
0,5the cytolysis of all cells140
0,05348095
0,005679294

Table 2
Immunomodulatory and anti-infective composition
MedicationDose, mg/mlE. coliStaphylococcus aureusThe control strain without the drug)
The placeholder1100% growth inhibition100% growth inhibitionActive growth of colonies
0,5100% growth inhibition100% growth inhibition
0,1100% growth inhibition100% suppression of Rho is the
The claimed composition1100% growth inhibition100% growth inhibitionActive growth of colonies
0,5100% growth inhibition100% growth inhibition
0,1100% growth inhibition100% growth inhibition

Table 3
Immunomodulatory and anti-infective composition
Dose, mg/mlThe percentage of active neutrophils (PAN)The percentage of completed phagocytosis (NRF)Adsorption capacity of neutrophils
The placeholderTrackThe placeholderTrack The placeholderTrack
control3232535355
0,51237305824
0,052040477036
0,0052942506435

Immunomodulatory and anti-infective composition comprising nano-sized powder of silver, characterized in that it further comprises a nano-sized powder of aluminum and nano-diamond powder, in the following ratio, wt.%:

nanosized powder of silver40
on oratory powder aluminum 30
nano diamond powder30



 

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3 ex, 1 tbl

FIELD: chemistry.

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23 cl, 3 tbl, 34 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pyridine derivatives of formula

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20 cl, 244 ex, 2 tbl

FIELD: medicine, pharmaceutics.

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25 cl, 6 tbl, 16 dwg

FIELD: medicine.

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14 cl, 1 ex

FIELD: medicine.

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1 dwg, 4 tbl, 5 ex

FIELD: chemistry.

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25 cl, 1 tbl, 41 ex

FIELD: medicine, pharmaceutics.

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8 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

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2 cl, 3 ex, 3 tbl

FIELD: medicine.

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12 cl, 13 ex, 9 dwg

FIELD: chemistry.

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13 cl, 2 ex, 3 tbl, 11 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to azabenzofuranyl compounds of formula I and salts thereof, where: Z1 denotes CR1, Z2 denotes N, Z3 denotes CR3, Z4 denotes CR4, R1, R3 and R4 are independently selected from H, halogen, CN, -(CR14R15)nC(=Y)OR11, - (CR14R15)nOR11, C1-C12 alkyl; W denotes or R5 and R6 are independently selected from H or C1-C12 alkyl; X1 is selected from R11, -OR11 and -S(O)2R11; if X1 denotes R11 or -OR11 from X1 and -R5 optionally taken together with a nitrogen atom with which they are bonded form a 4-6-member saturated or unsaturated ring containing 0-2 additional heteroatoms selected from O, S, where said ring is optionally substituted with one or more groups selected from oxo, -(CR19R20)nNR16R17, -(CR19R20)nOR16, (CR19R20)nS(O)2R16 and R21; X is selected from aryl, where said aryl is optionally substituted with one or more groups selected from halogen, CN, -Si(C1-C6alkyl), -(CR19R20)nOR16, -(CR19R20)nSR16, C1-C12alkyl; R11, R12 and R13 independently denote H, C1-C12alkyl, aryl, azetidine, pyrrolidinyl, piperidinyl, tetrahydropyranyl; R14 and R15 are independently selected from H or C1-C12 alkyl; n is independently selected from 0, 1; Y independently denotes O; where each of said alkyl, alkenyl, aryl and heteroaryl from R1, R2, R3, R4, R5, R6, X1, X2, R11, R12, R13, R14 and R15 is independently and optionally substituted with one or more groups independently selected from -(CR19R20)nC(=Y')OR16, -(CR19R20)nNR16R17, -(CR19R20)nOR16, -(CR19R20)nNR16C(=Y')R17, -(CR19R20)nNR16C(=Y')OR17, - (CR19R20)nNR17SO2R16 and R21; each R16, R17 independently denotes H, C1-C12 alkyl, C2-C8alkenyl, aryl, or pyridinyl, where said alkyl, alkenyl or aryl is optionally substituted with one or more groups selected from -OH; R19 and R20 are independently selected from H, C1-C12 alkyl; R21 denotes C1-C12 alkyl, aryl, imidazolyl, pyridinyl, pyrazolyl, pyrrolidinyl, 2-oxo-pyrrolidinyl, piperidinyl, or 2,2-dimethyl-1,3-dioxolanyl; each Y' independently denotes O. The invention also relates to specific compounds, a pharmaceutical composition based on the disclosed compounds, a method of inhibiting anomalous cell growth or a method of treating hyperproliferative disorders, inflammatory diseases and other diseases.

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23 cl, 3 tbl, 34 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biotechnology, specifically to obtaining PEGylated interferon alpha (IFN-alpha), and can be used in medicine. A conjugate of IFN-alpha with monomethoxypolyethylene glycol, bonded to N-terminal IFN-cysteine alpha of general formula , is obtained, where: n is a whole number from 454 to 1000; m is a whole number ≥4; NαH-IFN is interferon-α-2b, having interferon alpha activity.

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23 cl, 9 dwg, 6 tbl, 20 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to the use of pteridines of formula (I), including new pteridine derivatives of formula (VII), their pharmaceutically acceptable salts or esters as HCV-replication inhibitors. The invention also refers to pharmaceutical compositions based on the compounds stated above and a method for HCV-replication inhibition. In general formula

R1 independently means hydrogen; L means -NR8-, -NR8-C1-6alkandiyl or

wherein a cycle indicated by a dashed line together with N and Z forms a cycle containing 5-8 members, and can be substituted by an aromatic monocyclic heterocycle having 6 members in a cycle which contains as cycle members one heteroatom specified in nitrogen, wherein said L cycle is attached to a pteridine cycle by a nitrogen atom; Z means N or CH; R2 means hydroxyC1-6alkyl, phenyl, Het2, wherein said phenyl and Het2 are independently optionally substituted by one or more substitutes specified in a group consisting of C1-4alkyl, -COOR7, morpholin-4-yl, -CONR4aR4b, wherein R4a and R4b represent hydrogen, Het1-C1-4alkyl; or NR4aR4b, wherein R4a and R4b represent hydrogen, hydroxy C1-4alkyl, or can optionally form together with a nitrogen atom whereto attached, a 5-6-members saturated cycle, optionally containing an oxygen atom; R3 means phenyl, Het2 . The other radical values are specified in the patent claim.

EFFECT: preparing the compounds applicable as HCV-replication inhibitors.

16 cl, 1 dwg, 4 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, more specifically to an antiviral and interferonogenic amison preparation. The offered drug preparation is presented in the form of a capsule and contains the active substance amison (55.0-85.0 wt %) and target additives: lactose (11.0-44.0 wt %), aerosil (0.1-1.0 wt %), magnesium or calcium stearate (0.5-1.2 wt %) and talc (0-3.0 wt %).

EFFECT: invention provides the oral dosage form of amison for the first time presented in the form of capsules, storage-stable and enabling fast and complete release of the active substance.

1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutics, specifically to a tabletted antiviral agent. The agent contains, wt %: as an active substance - 2-methyl-6-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazin-7-one sodium salt, dehydrate (60.0-90.0), as an excipient - potato starch and/or lactose (1.0-20.0), as an aerating agent - low-substituted hydroxypropyl cellulose and/or microcrystalline cellulose (0.5-20.0), as antifriction substances - talc (0.2-2.5) and aerosil (0.2-3.0), as a greasing ingredient - magnesium stearate (0.2-3.0), as an agent forming a protective coating - hypromellose (1.0-10.0). The declared agent exhibits virus-inhibiting activity with respect to avian influenza virus, Rift Valley fever viruses, parainfluenza virus, Aujeszky's disease virus, western equine sleeping sickness virus, Venezuelan sleeping sickness virus, respiratory syncytial virus. What is also presented is a method for preparing said tabletted agent.

EFFECT: group of inventions provides the extended range of antiviral preparations due to preparing the tabletted agent having manifested virus-inhibiting action and improved organoleptic properties.

10 cl, 2 dwg, 6 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to biotechnology, particularly to a method for preparing a combined bivalent, tissue-culture, inactivated, concentrated, purified vaccine for preventing hemorrhagic fever and renal syndrome (HFRS). Substance of the invention involves reproduction of strains "ПУУ-ТКД/VERO" and "ДОВ-ЕАТ/VERO" of PUUMALA and DOBRABA viruses in a multilayer passaged culture of VERO-line grivet monkey's kidneys involving microfiltration of a virus-containing culture fluid to remove cell debris, virus inactivation by formalin, concentration by ultrafiltration and chromatography purification of the inactivated concentrated from ballast proteins, aluminium hydroxide sorption.

EFFECT: provided creation of the vaccine to be applied in European Russia and other European countries.

8 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared group of inventions relates to medicine. What is offered is using the Enterococcus faecium M (All-Russian collection of industrial microorganisms B-3490) and/or Enterococcus faecium M-3185 (VKPM B-3491) strains for preparing a composition, an agent or a preparation for treating viral hepatitis. The composition, the agent or the preparation for treating viral hepatitis contains an effective amount of the Enterococcus faecium M (All-Russian collection of industrial microorganisms B-3490) strain and/or an amount of the Enterococcus faecium M-3185 (All-Russian collection of industrial microorganisms B-3491) strain, and a pharmaceutically acceptable carrier. The composition, the agent or the preparation based on the Enterococcus faecium M (All-Russian collection of industrial microorganisms B-3490) and/or Enterococcus faecium M-3185 (All-Russian collection of industrial microorganisms B-3491) strains are administered orally in an effective single dose one to three times a day for 10-180 days.

EFFECT: compositions and methods have high therapeutic effectiveness, the patients show no such intoxication symptoms as dizziness and sleepiness; general state of health is normalised more rapidly.

2 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and concerns an interferon-inducing agent for treating acute respiratory viral infections and represents 1-{[6-brom-1- methyl-5-methoxy-2-phenylthiomethyl-1-n-indol-3-yl]carbonyl}-4-benzylpiperazine hydrochloride.

EFFECT: invention provides the agent showing interferonogenic action and applicable for treating acute respiratory viral infections (ARVIs).

12 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: disclosed is an agent which is 1,5-bis-(4-dodecyl-1,4-diazoniabicyclo[2.2.2]octan-1-yl)pentane dichloride dibromide with a structural formula shown on dwg. 1, which can be used to treat viral diseases of animals (e.g., bovine virus diarrhoea), accompanied by bacterial infections. Synthesis of the disclosed compound takes place in methanol as a solvent in 20-24 hours with molar ratio of the following components: 1-dodecyl-4-aza-1-azoniabicyclo[2.2.2]octane chloride to 1,5-dibromopentane equal to 1:(2.0-2.16), with 80.4-83.7% output of the end product.

EFFECT: agent has low toxicity, is stable during storage at room temperature for 3 years, has marked antibacterial action on pathogenic strains of microorganisms.

1 cl, 2 dwg, 3 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing concentrates of nanodispersions of zerovalent metals such as silver, gold, copper, palladium, platinum and mercury, which have antiseptic properties. Said method involves mixing a solution of a soluble metal salt in a solvent with ammonia to obtain a complex which is then mixed with alkalnolamine to form a solution. The obtained solution is mixed with a solution of a polymer stabiliser to obtain a stabilised metal cation which is then reduced by adding to the solution an organic or inorganic reducing agent to form a stable dispersion of metal nanoparticles. The disclosed method is realised at a defined ratio of components for 10-60 minutes in an air atmosphere at temperature of up to 100°C.

EFFECT: invention is aimed at obtaining metal dispersions with high sedimentation and chemical resistance and high antiseptic power, which are compatible with a physiological NaCl solution; the method also cuts duration of synthesis and considerably simplifies the process, increases efficiency and complete conversion of cationic metal into a zerovalent metal.

38 cl, 3 tbl, 104 ex

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