Drugs for immunological or allergic disorders (A61P37)

A   Human necessities(312083)
A61P37                 Drugs for immunological or allergic disorders(1768)

Recombinant chimerical ntbi polypeptide-immunogen with ability to induce neutralizing antibodies to type 1 human immunodeficiency virus and intended for use as component of vaccine against hiv-1 // 2642258
FIELD: medicine.SUBSTANCE: recombinant chimerical polypeptide-immunogen is proposed, including conservative T- and B-cell epitopes of HIV-1 and consecutive peptide fragments of p24, gp41, gp120 proteins, recognizable by wide-neutralizing 10e8, 2F5, VRC01 antibodies.EFFECT: improved HIV-specific immune response due to the inclusion of unique linear conformational epitopes imitators, recognizable by wide-neutralizing antibodies into the polypeptide-immunogen nTBI.6 dwg, 5 ex
ethod for endometritis treatment in cows // 2642251
FIELD: veterinary medicine.SUBSTANCE: ozonized autoblood as an immunomodulating and etiotropic agent is infused intramuscularly for four times in increasing-decreasing doses of 50, 75, 100, 75 ml at an interval of 48 hours, after obtaining from a vein, the blood is prepared by mixing in a syringe with 15 mg of sodium citrate and 10 mg of ozone in a ratio of 1:1 for 25 seconds, and Endometramag K is injected intramuscularly in an amount of 100.0 ml at an interval of 48 hours until recovery.EFFECT: increased effectiveness of therapeutic measures in case of endometritis and reduced period of the disease.2 tbl
Application of fullerene c60 aqueous solution as therapeutic agent at atopic dermatitis disease // 2641091
FIELD: pharmacology.SUBSTANCE: invention is application of a therapeutic agent for parenteral administration in atopic dermatitis, which is a water-salt solution consisting of fullerene C60, pluronic F-127 and physiological saline, where the components in the agent are in a certain ratio per ml of solution.EFFECT: reduction of allergic inflammation, skin regeneration improvement.1 tbl, 5 dwg
New compounds // 2640200
FIELD: pharmacology.SUBSTANCE: invention relates to a new compound of the formula (I) or a pharmaceutically acceptable salt thereof having interferon α (IFN-α) and tumour necrosis factor α (TNF-α) inducer properties. The compounds may be useful as vaccine adjuvants. In the formula (I) R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl; m is an integer having a value of 1 to 4.EFFECT: compounds can be used for treatment of allergic diseases and inflammatory conditions, for example, allergic rhinitis and asthma, infectious diseases and cancer.15 cl, 7 ex

Cd89 activation in therapy // 2640082
FIELD: pharmacology.SUBSTANCE: for CD89 activation neutrophil therapy, inflammations previously activated by a stimulus, are brought into contact with an effective dose of molecules that activate CD89 and contain Fc-alpha.EFFECT: CD89 activation increases apoptosis in neutrophils, which provides inhibition of inflammation in autoimmune and inflammatory diseases.18 cl, 13 dwg, 8 ex
Phenyl derivative // 2639875
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) having a high antagonistic activity with respect to human S1P2, and can be used to prepare a drug for treatment of a disease mediated by S1P2, such as a disease caused by vasoconstriction, fibrosis and respiratory disease.EFFECT: compound application efficiency increase.14 cl, 2 tbl, 9 ex
Hetero-aromatic methylic derivative of cyclic amine // 2639869
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (IA), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; Y is any structure from the following group of formulas (a); n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group; R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 an alkyl group; or a pharmaceutically acceptable salt thereof. The invention also relates to a compound represented by the formula (I), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; any one of Y1 and Y2 is a nitrogen atom, and the other is CH; n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group;R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 alkyl group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are intended for the production of a pharmaceutical composition having antagonistic activity against OX1 and OX2 orexin receptors.EFFECT: hetero-aromatic methyl derivative of cyclic amine, which has antagonistic activity against OX1 and OX2 orexin receptors.9 cl, 6 tbl, 85 ex

ethod for gm-csfrα inhibition in patient // 2639546
FIELD: medicine.SUBSTANCE: method for inhibition or neutralisation of the alpha chain activity of the colony-stimulating granulocyte/macrophage (GM-CSFRα) factor in a patient, comprising administration of a composition containing an effective amount of an antibody to human GM-CSFRα. In addition, methods for treatment of rheumatoid arthritis, asthma, chronic obstructive pulmonary disease or myeloid leukaemia in a patient are contemplated. This invention may find use in the therapy of other diseases associated with GM-CSFRα.EFFECT: increased efficiency of treatment.12 cl, 9 dwg, 5 tbl

Analogues of complement factor b and their application // 2639521
FIELD: biotechnology.SUBSTANCE: invention can be used in medicine to treat a disease mediated by activation of an alternative complement pathway. A polypeptide consisting of hfB3-292S (amino acids 1-764 or 26-764 in SEQ ID NO: 2), hfB3-292SN480 (amino acids 1-480 or 26-480 in SEQ ID NO: 2) or hfB3-292S-Fc (amino acids 1-990 or 26-990 in SEQ ID NO: 22) is obtained.EFFECT: invention allows to effectively inhibit the activity of the alternative complement pathway when using the resulting polypeptide, coding its nucleic acid or expression vector.12 cl, 14 dwg, 6 tbl, 19 ex

Immunity inducing agent // 2639518
FIELD: medicine.SUBSTANCE: invention refers to the immunity inducing agent containing the effective number of at least one polypeptide with inducing immune system activity, which induces cytotoxic t-cells capable to destroy tumour cells expressing polypeptide CAPRIN-1. Also, method is represented to obtain the selected antigen-presenting cell in vitro, which presents polypeptide fragment CAPRIN-1 for class I molecule RENAMO t-cells, as well as in vitro method for obtaining selected cytotoxic t-cells specific to protein CAPRIN-1. The invention also relates to a method of induction of immunity, including the introduction of individual effective amount of at least one polypeptide with inducing immune system activity, which induces cytotoxic t-cells capable to destroy tumour cells expressing polypeptide CAPRIN-1.EFFECT: effectively destroys tumour cells expressing the CAPRIN-1 polypeptide.13 cl, 5 dwg, 6 ex

Virions and virus-like particles of alternanthera mosaic virus as amplifiers of immune response // 2639491
FIELD: medicine.SUBSTANCE: virus-like particles are produced in vitro from the protein of the alternanthera mosaic virus (AMV) coat in the absence of RNA. The virus-like particles are produced under physiological conditions by incubating the AMV coat protein in 0.15 M NaCl at pH 7.0-7.5. The group of inventions also relates to a method for enhancing an immune response to an antigen when immunizing animals or human with a mixture of an antigen and an adjuvant, wherein the virus-like AMV particles obtained by the above mentioned method are used as an adjuvant.EFFECT: use of this group of inventions allows to obtain stable and highly immunogenic virus-like particles which do not differ in size and morphology from full-fledged viral particles, while the AMV coat protein under in vitro physiological conditions can be repolymerised into long spiral structures in the absence of RNA.2 cl, 6 ex, 6 dwg
ethod of treatment of ifn-alpha-connected states // 2639135
FIELD: medicine.SUBSTANCE: immunogenic product comprising IFNα coupled to a molecule of keyhole limpet hemocyanin (KLH), is used in therapeutically effective amount that is administered to a specified subject in one introduction which is more than 30 micrograms, and the ratio of IFNα to KLH by weight is from 0.06 to 0.6. The group of inventions also refers to a unit dosage drug form containing more than 30 μg of immunogenic product, as well as a kit for treating IFN-associatedα state of the subject in need thereof.EFFECT: neutralisation of IFNα in vivo, when more than 30 μg of the immunogenic product is used, increase of the production of IFN-binding antibodies in patients in response to the above immunogenic product.15 cl, 11 ex, 8 tbl, 5 dwg
ethod for obtaining of herbal agent with immunostimulating activity // 2639132
FIELD: pharmacology.SUBSTANCE: method for obtaining of an agent with an immunostimulating effect from the aerial part of the cold gentian by extracting the herbal material, wherein the ground herbal material is mixed with 70% ethanol, the mixture is ultrasonicated, the mixture is filtered and washed on a filter with an additional volume of 70% ethanol, then the remainder of the herbal material after ethanol extraction is mixed with water, the mixture is subjected to ultrasonic treatment, the mixture is filtered and washed on the filter with an additional volume of water, the ethanol extraction is concentrated, the aqueous extraction is concentrated, the concentrated ethanol and aqueous extracts are combined, dried and ground under certain conditions.EFFECT: agent obtained by the above-described method has a pronounced immunostimulating effect.5 tbl, 3 ex
ethod for anal fissure treatment // 2639039
FIELD: medicine.SUBSTANCE: for treatment of a chronic anal fissure, it is excised along with the surrounding scar tissue and the guard tubercle by two half-moon incisions within healthy tissues. 0.1-0.2 ml doses of autoplasma, enriched with platelet growth factors, is injected into the wound walls and bottom with a grid of 3-4 mm. Wound edges are separated by a rectal mirror. A film of enriched autoplasm is applied to the wound bottom. Enriched autoplasm in a volume of 1 ml is injected under the wound, to a depth of 5-7 mm. Botulinum toxin A at a dose of 15-20 units is injected into the inner sphincter at three points to a depth of 5-7 mm. In case of back fissure, botulinum toxin is administered at 5, 7 and 12 hours, in case of front fissure - at 11, 1 and 6 hours. On the 4th day, the introduction of autoplasm is repeated.EFFECT: reduces postoperative pain syndrome, increases the effectiveness of anal fissure treatment, reducing the risk of postoperative complications.2 ex
Application of cxcr4 antagonists // 2638802
FIELD: pharmacology.SUBSTANCE: for the treatment or prevention of WHIM syndrome in a person diagnosed with WHIM syndrome, this person is administered a CXCR4 antagonist in an amount effective to treat or prevent WHIM syndrome. The CXCR4 antagonist is 1,1'-[1,4-phenylene-bis (methylene)]-bis-1,4,8,11-tetraazacyclotetradecane or a pharmaceutically acceptable salt or metal complex thereof. A pharmaceutical composition for the treatment or prevention of WHIM syndrome in humans as well as the treatment or prevention of a disorder or condition independently selected from WHIM syndrome, hypogammaglobulinemia, myelocatex, neutropenia, leukopenia or lymphopenia in a person diagnosed with WHIM syndrome is also provided.EFFECT: effective treatment of these conditions in the patient.39 cl, 2 dwg, 1 ex

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex
Pyrazolo [3,4-c] pyridines and methods of application thereof // 2638116
FIELD: pharmacology.SUBSTANCE: subject of the invention is pyrazolo [3,4-c] pyridines of the formula I ,including their stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts, wherein R1 and R2 have the values disclosed in the claims. These compounds are useful for inhibiting Pim-kinases and for treating disorders such as cancer, mediated by Pim-kinase. Methods for using compounds of formula I for in vitro, in situ and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells or related pathological conditions are disclosed.EFFECT: increased application effeciency.4 cl, 3 tbl, 328 ex
Inhibitors of lrrk2 kinases activity // 2637936
FIELD: pharmacology.SUBSTANCE: R1, R2, R3 and R4 values are defined in the claims of this invention. Compounds of the formula (I) inhibit the LRRK2 activity. In addition, the invention relates to particular compounds as defined in claim 14. The invention also relates to a pharmaceutical composition comprising the compounds of the invention and to a method for neurodegenerative diseases treatment, for example those in which the disease is represented by α-synucleinopathy and in particular to a method for treatment of various diseases of the Parkinson's disease type, as well as a method for treatment of autoimmune diseases, such as Crohn's disease or ulcerative colitis.EFFECT: new method for neurodegenerative diseases treatment.22 cl, 10 tbl, 15 ex
Immunodepressant // 2637643
FIELD: medicine.SUBSTANCE: as an immunosuppressant, 2-(ethylthiomethylene)-3,3-dimethyl-1,3-oxazolidinium chloride compounds are used. Application of 2-(ethylthiomethylene)-3,3-dimethyl-1,3-oxazolidinium chloride compounds, formerly known as antibacterial agent, as an immunosuppressant in medicine can be used as a basis for the creation of drugs for the treatment of autoimmune and allergic diseases.EFFECT: increased efficiency of treatment.3 tbl, 3 ex
Immunodepressant // 2637642
FIELD: pharmacology.SUBSTANCE: application of 2-(isopropylthiomethylene)-3-methyl-3-(2-hydroxyethyl)-1,3-oxazolidinium chloride as an immunosuppressant is proposed. The technical result is compound in doses far from toxic (LD50 at intraperitoneal introduction to mice - 2000 mg/kg), has an in vitro selective antiproliferative effect on actively fissionable lymphoid cells, but not on tumour cells.EFFECT: invention will allow to create medicaments for treatment of autoimmune and allergic diseases based on the said compound.2 tbl, 1 ex
ethod for reconstruction of immunological disorders in newborn calves // 2636491
FIELD: veterinary medicine.SUBSTANCE: method includes application of xymedone in combination with L-ascorbic acid and saline solution and additionally OCC "Furor" as follows: on day 1, 2 and 7 of life: IM xymedone in combination with L-ascorbic acid and saline solution at the following component ratio, wt %: xymedone - 13.22, L-ascorbic acid - 4.13, saline -the rest at a dose of 52.5 mg/kg of body weight, OCC "Furor" starting from the second day of life for 10 days inside with milk or colostrum at a dose of 0.3 ml/kg of body weight.EFFECT: increased serum bactericidal activity and serum lysozymic activity, increased number of T-and B-lymphocytes, phagocytic activity of blood neutrophils, adaptation to environmental changes and high antigen load, greater resistance to gastrointestinal diseases.7 tbl, 3 ex

Targeted/immunomodulating fusion proteins and methods for their obtaining // 2636342
FIELD: biotechnology.SUBSTANCE: chimeric fusion protein containing a targeting moiety for cancer cell targeting, an immunomodulating moiety that counteracts the immune tolerance of cancer cells, and an amino acid spacer is prepared recombinantly.EFFECT: invention allows to increase the effectiveness of cancer diseases treatment.9 cl, 65 dwg, 1 tbl, 12 ex

Compositions for inhibition of masp-2-dependent complement activation // 2636038
FIELD: medicine.SUBSTANCE: isolated human monoclonal antibody and its antigen-binding fragment that bind to human MASP-2 are disclosed. In addition, a nucleic acid molecule encoding the amino acid sequences of the variable regions of the antibody and an antigen-binding fragment are examined; an expression cassette; a cell and a method for production of an isolated anti-MASP-2 antibody or an antigen-binding fragment thereof. A composition for treatment of a condition associated with MASP-2-dependent complement activation; application of an anti-MASP-2 antibody for drug preparation, and an industrial product for treatment of a condition associated with MASP-2-dependent complement activation are also described.EFFECT: can find further application in the therapy of complement-mediated diseases.19 cl, 24 dwg, 30 tbl, 12 ex

Antibodies to pd-l1 and their application for t-cells function strengthening // 2636023
FIELD: biotechnology.SUBSTANCE: isolated antibody to PD-L1 and its antigen-binding fragment, characterized by amino acid sequences of hypervariable regions (HVR) in the heavy chain and light chain variable regions, are proposed. In addition, an isolated nucleic acid encoding the antibody; an expression vector; a host cell and a method for production of an antibody or an antigen-binding fragment thereof are described. Also a composition comprising an effective amount of the antibody to PD-L1 or the antigen-binding fragment; a product of manufacture comprising a container with a therapeutically effective amount of the composition; and methods for malignant tumour and infection treatment are considered.EFFECT: invention can find further application in therapy.60 cl, 11 dwg, 4 tbl, 11 ex
ethod for treatment and prevention of allergic spectrum states // 2635968
FIELD: medicine.SUBSTANCE: use of a peptide, which is sodium gamma-D-glutamyl-D-tryptophan as an antiallergic drug for treatment or prevention of pathological conditions with allergic syndrome, selected from at least one: allergic rhinitis, allergic conjunctivitis, allergic bronchial asthma, is proposed.EFFECT: relief of residual manifestations in the disease remission.3 cl, 1 tbl, 6 ex
Drug based on 5-amino-2,3-dihydrophthalazine-1,4-dione as quick-soluble film for transbuccal introduction // 2635769
FIELD: pharmacology.SUBSTANCE: drug in the form of easily soluble biocompatible film for transbuccal application includes a therapeutically effective amount of pharmacologically active agent, such as a salt of alkaline or alkaline-earth metal 5-amino-2.3-dihydrophthalazine-1.4-dione as a waterless salt or its monohydrate or dihydrate, or their mixtures, mucoadhesive film forming polymer plasticiser and taste flavour, represented by a mixture of β-cyclodextrin or modified β-cyclodextrin with sorbitol when their mass ratio of 4:1-1:2, the content of the specified mixture in the film is 15-40 wt % of the weight of the entire film.EFFECT: increased release speed of the pharmacologically active agent when applying the film, increased transparency, uniformity and stability in storage while retaining elasticity and strength.16 cl, 5 tbl
ethod for obtaining of peptide immunity stimulator (versions) and baa based thereon // 2635625
FIELD: pharmacology.SUBSTANCE: raw materials are defrost, ground, extracted with 3% acetic acid solution, the supernatant is obtained and separated, the final product is isolated. The raw material is extracted for 35-48 hours with stirring for 15 minutes every 1.5 hours, then basified with sodium bicarbonate solution to pH of 8.0-8.5, 0.3% chitosan solution in 3% acetic acid is added, the resulting mass is centrifuged on a centrifuge at 5000 rpm for 20 minutes, ammonium sulfate is added to the supernatant to 30% of the solution concentration, kept with stirring for two hours, centrifuged again at 5000 rpm for 20 minutes, the supernatant is diafiltered at the checkout counter hydrochloric membrane with a separation limit of 1000 Da four times with distilled water addition to the resulting concentrate with a concentrate: water ratio of 1:2 to obtain a solution with a final substance of 1000 to 15000 Da. Also biologically active additive is proposed.EFFECT: increased biological activity by increasing the content of peptides with an immunostimulating effect.7 cl, 2 tbl, 6 ex

ethod for treating autoimmune disease using biocompatible bioabsorbable nanosphere // 2635537
FIELD: medicine.SUBSTANCE: composition for preventing or treating an autoimmune disease comprising antigen-MHC polypeptide complexes function-associated with biocompatible bioadsorbable nanospheres forming a population of nanospheres with polypeptide complexes connected thereto, wherein the ratio of the plurality of polypeptide complexes is greater than 50 to 200 per nanosphere having a size of less than 14 nm. The group of inventions also includes the application of this composition for the treatment of an autoimmune disorder, wherein the composition is administered in an amount sufficient to proliferate antipathogenic autoreactive T-cells. The application of this group of inventions provides significant proliferation of CD8+ T-cells due to the use of antigen-MHC polypeptide complexes associated with biocompatible bioadsorbable nanospheres, wherein a plurality of polypeptide complexes is more than 50 to 200 per nanosphere having a size of less than 14 nm.EFFECT: directional binding of a plurality of pMHCs to the surface of the nanoparticles through their carboxy-ends results in stabilization of the coated nanoparticles, obtaining a high concentration of particles without disturbing the monodispersity and their stability.34 cl, 4 ex, 4 tbl, 9 dwg
ethod for treatment of chronic endometritis with autoimmune endometrium disorders // 2635518
FIELD: medicine.SUBSTANCE: for treatment of chronic endometritis with autoimmune endometrium disorders, a sterile and warmed to a body temperature of 36.6-37°C 0.02% solution of gepon (2.0 ml) is prescribed intrauterinely once a day for 10 days as pathogenetic treatment of chronic autoimmune endometritis from the 5th day of the menstrual cycle.EFFECT: invention provides relief of the inflammatory process, restoration of endometrium sensitivity to its own hormones and restoration of the endometrium glandulocyte secretory activity.1 ex
Bruton's tyrosine kinase inhibitors // 2634723
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of general formula I: , as well as to pharmaceutical compositions based thereon, and to application for treatment of inflammatory or autoimmune diseases associated with aberrant B-cell proliferation.EFFECT: new compounds with inhibitory activity against Btk are obtained.27 cl, 2 tbl, 34 ex
ethod for immunodeficient conditions correction by "alloplant" biomaterial // 2634631
FIELD: medicine.SUBSTANCE: method is based on subcutaneous injection of dispersed "Alloplant" biomaterial, diluted in physiological solution at a ratio of 30-50 mg of biomaterial per 12 ml of solution into biologically active points. To ensure the neurohumoral regulation, points GB 8, GV 14, GV 20, GV 23 are affected. For immunoregulation, points BL 11, GV 13, CV 19, CV 21 are affected. For restorative and harmonizing action, points LI 4, LI 11, ST 36, CV 12, BL 24, CV 4, CV 6, are used. Introduction is performed as 0.5-1.0 ml in one injection. At that, injections are performed by sessions of 1-10 per course with an interval of 1-5 days.EFFECT: effective correction of the immune system disorders, no adverse reactions, well tolerated by patients.1 dwg, 2 ex
Filler for capsular inhaler // 2634258
FIELD: pharmacology.SUBSTANCE: filler contains timodepressin in the form of fine particles of respirable size in the amount of 8.5-11.5 wt % and an inert carrier - inhalation lactose - the rest.EFFECT: expanded arsenal of drugs for inhalation in the treatment of autoimmune diseases, ensuring drug delivery to the blood in unchanged form.3 dwg, 3 ex
ethod for immune response stimulation and preparation for its implementation // 2634247
FIELD: pharmacology.SUBSTANCE: preparation includes an adjuvant and an inactivated antigenic material, with fatty (C12-C22) acid and fatty (C12-C22) acid N,N-dimethylaminopropylamide mixture in an 1:1 molar ratio used as an adjuvant, and the preparation includes the following components (wt %): a mixture of a fatty (C12-C22) acid and fatty (C12-C22) acid N,N-dimethylaminopropylamide (in a molar ratio of 1:1) to 0.01-10; aqueous inactivated antigenic material in an amount sufficient to induce an immune response - up to 100. The group of inventions also includes a method for immune response stimulation, comprising administration of the above preparation.EFFECT: application of this group of inventions allows to stimulate the immune response when using a mixture of fatty acid and fatty acid N,N-dimethylaminopropylamide as an adjuvant.2 cl, 6 tbl

Aptamer against ngf and its application // 2633510
FIELD: biotechnology.SUBSTANCE: invention relates to an aptamer specifically binding to a nerve growth factor (NGF), and can be used in medicine as an anti-inflammatory or analgesic. The invention allows to obtain an aptamer capable of forming a secondary structure represented by the formula (I), where N is nucleotid selected from the group consisting of A, G, C and U. Each of N14 and N24, N31 and N41, and N39 and N49 forms a Watson-Cric base pair, and the remaining nucleotides of formula (I) are capable of forming a stalk structure.EFFECT: invention provides an aptamer capable of inhibiting NGF activity at IC50 1 nM or less.5 cl, 5 dwg, 5 tbl, 18 ex
edicinal for vaginal application, with antiviral, antimicrobial, antifungal, antiprotozoal, antiinfectious, immunomodulating and antiinflammatory action, as ointment, gel, suppository // 2633056
FIELD: pharmacology.SUBSTANCE: medicament is presented comprising active substances, excipients and a consistently-forming base, characterized by comprising fluconazole, metronidazole, alpha- or beta- or gamma-recombinant interferon as active substances, disodium edetate and boric acid as adjuvants, and substances selected from the group: macrogol 400, macrogol 1500, macrogol 4000, vitepsol, glycerin, cocoa butter, paraffin, lanolin, vaseline, acetylphthalyl, GL type solid fat as a consistently forming base, wherein the drug components are in a specific ratio in g per 1 g of the agent.EFFECT: high therapeutic effect ensures rapid substances entry into the blood.1 cl

Dyetered diaminopyrimidine compounds and pharmaceutical compositions containing such connections // 2632907
FIELD: pharmacology.SUBSTANCE: invention relates to novel deuterated diaminopyrimidines of the general formula (I) and their pharmaceutically acceptable salts. In the general formula (I) R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9, R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a and R20b independently hydrogen or deuterium; R5 is hydrogen, deuterium or halogen, R8 Represents a halogen; Provided that at least four of R1a, R1b, R1c, R2a, R2b, R2c, R3, R12, R13a, R13b, R13c, R14a, R14b, R14c, R19a, R19b, R20a or R20b are deuterium. The invention also relates to a process for the preparation of compounds of general formula (I) by reacting compound A6 with compound XV and to intermediates A6 and XV. In this case, in compound A6 R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a or R20b are independently selected from deuterium or hydrogen and at least one of them is deuterium; In compound XV R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9 are independently selected from hydrogen or deuterium and at least one of them is deuterium; and R5 is hydrogen, deuterium or halogen; and R8 represents a halogen; X2 is selected from F, Cl, Br, I.EFFECT: compounds have ALK protein kinase inhibitory properties and can be used to treat or prevent cancer, impair cell proliferation, cardiovascular diseases, inflammation, infection, autoimmune diseases, organ transplantation, viral diseases, cardiovascular diseases or metabolic diseases.18 cl, 4 dwg, 1 tbl
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 ex
Tricyclic heterocyclic compounds and jak inhibitors // 2632870
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula : , where the Aa ring is represented by the following formula , where T1a is a nitrogen atom, U1a is a nitrogen atom, Xa is CR9a (where R9a represents a hydrogen atom), Ya a is CR10a (where R10a is a hydrogen atom), R1a is a hydrogen atom, ring Ba is C4-7cycloalkane, benzene or a 4 to 6-membered non-aromatic heterocycle containing 1 heteroatom selected from a nitrogen atom, L1a is a single bond, L2a is a single bond, C1-3 is an alkylene group (C1-3 alkylene group is unsubstituted or substituted by a cyano group) or C1-3 halogenoalkylene group, L3a is a single bond or is represented by any of the following formulas: na is 0 or 1, R3a is a hydroxy group, a halogen atom, a cyano group or a methyl group, the remaining radicals are as defined in the claims. The invention also relates to a compound represented by the formula (Ib), to a JAK inhibitor containing the compound of the invention, to a preventive, therapeutic or improving agent for diseases in which JAK inhibition is effective, to a drug.EFFECT: new compounds with inhibitory activity against JAK are obtained.36 cl, 236 tbl, 611 ex

odified biotin-binding protein, fusion proteins based thereon and their application // 2632651
FIELD: biotechnology.SUBSTANCE: fusion biotin-binding protein is obtained which comprises a soluble biotin-binding protein and an antigenic protein or peptide, the fusion protein does not include amino acids 1-44 of the wild-type Rizavidin protein.EFFECT: invention allows to express fusion biotin-binding proteins in soluble form and at a high yield, to increase the efficiency of formation of complexes of biotin-binding proteins and protein antigens.18 cl, 14 dwg, 5 tbl, 7 ex

ethod for graft-versus-host reaction identification or treatment // 2632434
FIELD: pharmacology.SUBSTANCE: group of inventions refers to medicine, namely, to transplantology and immunology, and can be used to prepare a pharmaceutical composition for treatment of the graft-versus-host reaction. A pharmaceutical composition for graft-versus-host reaction treatment comprising an anti-CCL8 antibody as an active ingredient. The group of inventions also relates to a method of graft-versus-host reaction treatment comprising anti-CCL8 antibody administration to a subject.EFFECT: use of this group of inventions provides prevention of organ damage in patients with GVHD with the use of CCL8 antibodies.2 cl, 9 ex, 17 dwg

Treatment of malignant and non-malignant diseases with ras antagonists // 2632097
FIELD: pharmacology.SUBSTANCE: group of inventions is a Ras antagonist represented by the formula R1-R2-R3-R4, where: R3 is S; R4 is farnesyl or geranyl-geranyl, wherein geranyl-geranyl has the structure :R2 is a 5-membered heterocyclic ring containing one S heteroatom; R1 is C(=O)R5, CO2M; R5 is hydroxyl; M is a salt forming an organic or inorganic counterion; and R8is hydrogen or C1-C4 alkyl; and pharmaceutically acceptable salts thereof; or R1 is a 5-membered heterocyclic ring containing 2-4 N heteroatoms and R2 is a phenyl ring; or R2 is a 5-membered heterocyclic ring containing three heteroatoms selected from N and S, and R1 is C(=O)R10, and R10 is hydrogen, hydroxyl or C1-C4 alkyloxy. The invention also relates to a method for inhibition of Ras-induced cell proliferation associated with a malignant or non-malignant disease, comprising Ras antagonist administration to a patient.EFFECT: increased efficiency of treatment.20 cl, 9 ex, 7 dwg

Coagulation factor viii with reduced immunogenicity // 2631801
FIELD: biotechnology.SUBSTANCE: method comprises: (a) identification of at least one epitope of NKT cells, wherein the motif of the said NKT cell epitope is [FWTHY]-X2X3-[ILMV]-X5X6-[FWTHY], wherein at least one NKT cell epitope is in SEQ ID NO: 1 and (b) modification of the said epitope(s) by replacing at least one hydrophobic amino acid residue at position P1 and P7 with one amino acid other than F, W, T, H, Y.EFFECT: invention allows to obtain an active molecule of factor VIII, which has a reduced ability to activate NKT cells due to reduced binding to the CD1d molecule.6 cl, 6 dwg, 1 tbl, 7 ex
Water-dispersible desloratadine pill and method for its manufacture // 2631619
FIELD: pharmacology.SUBSTANCE: invention describes a pharmaceutical composition in the form of a dispersible pill comprising desloratadine and a method for its manufacture. A water-dispersible desloratadine pill is prepared by compressing the active ingredient in an amount of 2.5 or 5.0 mg with processing aids and pharmaceutically acceptable excipients and is capable of dispersing in water for 3 minutes to form a dispersion consisting of particles smaller than 710 mcm. The obtained pill possesses high stability and physical preservation, good mechanical properties in combination with fast disintegration in water solutions.EFFECT: experimentally selected composition allows for high processability of the dispersible pill manufacturing process.2 ex, 2 tbl

Composition // 2631482
FIELD: pharmacology.SUBSTANCE: compound and its pharmaceutically acceptable salts are inducers of human interferon. Some discrete and single doses of the compound (I) may be particularly useful for treatment of various disorders, for example, allergic rhinitis and allergic asthma.EFFECT: invention provides treatment at a stated dose of 10 to 20 ng, it is possible to avoid the unpleasant side effects.5 cl, 4 dwg
Dimethylamide 7-cyclopentyle-2-(5-piperazin-1-il-pyridine-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carbonic acid salt (salts) and method for their production // 2631243
FIELD: pharmacology.SUBSTANCE: invention relates to a new succinate salt of dimethylamide 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid represented by the formula (II) in a hydrated and non-hydrated form. The compound can be used to treat a disease impaired by cyclin-dependent kinases activity inhibition, in particular, CDK1, CDK2, CDK3, CDK4 CDK5, CDK6 and CDK9 kinases. Such a disease can be represented by breast cancer, genitourinary cancer, lung cancer, pancreatic cancer, etc. The succinate salt corresponds to the structural formula given below.EFFECT: increased efficiency of treatment.5 cl, 6 dwg, 2 tbl, 7 ex

Fusion proteins for application as immunogenic amplifying agents to induce antigen-specific t-cell response // 2631002
FIELD: biotechnology.SUBSTANCE: invention relates to fusion proteins for application as an immunogenic enhancing agent to enhance antigen-specific T-cell responses, and can be used in medicine. A fusion protein is produced recombinantly, which comprises: (a) a binding domain with an antigen-presenting cell (APC) or a binding domain with the CD91 receptor; (b) a protein transduction domain; (c) a pathogenic antigen. The binding domain with the antigen-presenting cell (APC) or the binding domain with the CD91 receptor is located at the N-terminus of the fusion protein, and the pathogenic antigen is located at the C-terminus of the protein transduction domain.EFFECT: invention allows to obtain an enhanced antigen-specific T-cell response against a viral pathogen and cancer cell.16 cl, 15 dwg, 2 tbl, 6 ex
Nitrogen-containing spirocyclic compound and its application in medicine // 2630694
FIELD: pharmacology.SUBSTANCE: compounds can be used to prepare a medicament for treatment or prevention of a disease selected from the group consisting of organ transplant rejection, graft versus host transplantation, autoimmune disease, allergic diseases and chronic myeloproliferative disease. The disease can be selected from rheumatoid arthritis, psoriasis, atopic dermatitis or a disease caused by dry eyes. In the general formula Ra is the same or different and each represents (1) C1-6 alkyl or (2) a halogen atom, n1 is an integer selected from the integers from 0 to 2, Rb are the same or different and each represents (1) C1-6 alkyl or (2) halogen atom, n2 is an integer selected from the integers from 0 to 2, m1 is an integer selected from the integers from 0 to 3, m2 is an integer selected from the integers from 1 to 4, Xa=Xb is (1) CH=CH, (2) N=CH or (3) CH=N, X is (1) a nitrogen atom or (2) C-Rd, where Rd is a hydrogen atom or halogen atom, Rc is a group selected from the following groups (1)-(6): (1) a hydrogen atom, (2) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, (3) -C(=O)-Rc1, (4) -C(=O)-O-Rc2, (5) -C(=O)-NRc3Rc4, where Rc1, Rc2, Rc3, Rc4 are the same or different and each represents (i) a hydrogen atom or (ii) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, or (6) a group of the following formula in which Ya is a group selected from the following groups (i) to(iii) (i) C1-6 alkylene, (ii) -C(=O)- or (iii) -S(=O)-O-, ring T is (i) a phenyl, (ii) C3-10 cycloalkyl or (iii) a saturated monoheterocyclyl, which contains 1 nitrogen atom and carbon atoms, and the number of atoms, constituting the ring, is 3-7, Rc5 is the same or different and each represents (i) cyano, or (ii) a nitro group, p is an integer selected from the integers from 0 to 1, group A is a group, consisting of (a) a hydroxyl, (b) C1-6 alkoxy, (c) a cyano, (d) C1-6 alkoxycarbonyl, (e) C1-6 alkylcarboxylic and (f) C2-6 alkenylacyl.EFFECT: increased efficiency of treatment.60 cl, 33 tbl, 8 ex

Hybrid polypeptide, presenting amino acid sequences, and its application // 2630660
FIELD: biotechnology.SUBSTANCE: hybrid polypeptides are produced, that are capable of inducing an immune response against X1 in an animal other than a human, according to formula I and II NH2-S2-X1-COOH (formula I) NH2-S4-X2-S3-S2-X1-S1-S0-COOH (formula II), where X1 contains an amino acid sequence that is a target antigen or an immunogenic sequence and optionally includes a linker or adapter sequence, denotes a peptide bond, S1 and S2 are a pair of sequences of SEQ ID NO: 3 and 2, respectively.EFFECT: invention allows to effectively achieve an immune response to the target antigen and to obtain antibodies to the target antigen.14 cl, 40 dwg, 2 tbl, 17 ex

Hybrid peptide carrying proteins as vaccines against allergy // 2630652
FIELD: biotechnology.SUBSTANCE: invention relates to polypeptides for treatment or prevention of allergies to pollen Ph1P1, birch Betv1 pollen and Derp2 home dust mite allergens, which can be used in medicine. The recombinantly obtained polypeptides of SEQ ID NO: 14-19 and 149-152 are used in vaccine compositions intended to treat or prevent response to corresponding allergens.EFFECT: decreased number of side effects when vaccinated with Ph1P1, Betv1 and Derp2 allergens.33 cl, 20 dwg, 7 tbl, 27 ex

Compositions, method and kits for mucosal immune system stimulation // 2630299
FIELD: biotechnology.SUBSTANCE: nutritional compositions for stimulating mucosal immune system, method of manufacturing and applying them are proposed. The composition comprises a milk or cereal product fermented with probiotic bacterium Lactobacillus paracasei (CBA L74) BCCM/LMG LMG P-24778. Alternatively, the composition comprises L. paracasei LMG P-24778 in amount of from about 1×102 CFU/g to about 1012 CFU/g of bacteria on 1 gram of dry mass and a physiologically acceptable carrier. The method of manufacturing the composition comprises combining the food product with an effective amount of Lactobacillus paracasei LMG P-24778 and incubating the mixture at a temperature and for a time sufficient for fermentation. Nutritional kits are proposed, comprising compositions based on L. paracasei LMG P-24778 or fermented milk or grain product and one or more items, selected from group consisting of a packaging material, a package insert including instructions for use, a sterile liquid, and a sterile container.EFFECT: proposed compositions of the invention may be administered to a patient having gastrointestinal disorders or the risk their development, which refers to an inadequate development of immune system, infection or disease, to stimulate immunomodulatory reaction in mucosal immune system.30 cl, 34 dwg, 20 ex
 
2551062.
Up!