Drugs for disorders of the metabolism (A61P3)

A   Human necessities(312083)
A61P3                 Drugs for disorders of the metabolism (of the blood or the extracellular fluid a61p0007000000)(10709)
Forzicyaside sulfate and its derivatives, method for its production and its application // 2642784
FIELD: pharmacology.SUBSTANCE: invention relates to forzicyaside sulfate and its derivative represented by the following formula , wherein R is Na+, K+ or NH+, and a method for their preparation, as well as an antiviral drug based on them and its use.EFFECT: increased efficiency of agents.10 cl, 9 tbl, 2 dwg
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex
ethod for increase of organism resistance to combined toxic action of nanoparticles of copper, zinc and lead oxides // 2642674
FIELD: medicine.SUBSTANCE: method for reduction of the adverse effects of combined effects of copper (CuO), zinc (ZnO) and lead (PbO) oxides nanoparticles on organism in risk groups covering individuals exposed to such effects under production conditions. Method includes prescription of a complex of biologically active drugs: glutaminic acid, glycine, N-acetylcysteine, pectin enterosorbent, fish oil preparation rich in unesterified omega-3 fatty acids, Vitamins A, C, D3, E, selenium, iron and iodized preparations. This complex is taken by repeated courses 1-2 times a year for 4-6 weeks daily at doses providing daily intake of 300 mg of glycine, 600 mg of cysteine, 4 g of glutaminic acid, 25 ml of fish oil with 12-15% content of polyunsaturated omega-3 fatty acids, 4-5 grams of pectin, as well as selenium, iron, iodine and these vitamins in doses that provide the normal physiological needs of the organism.EFFECT: reduction of all three metals in the blood, improved elimination function of the liver and kidneys, reduced integral signs of chronic intoxication, including signs of neurotoxicity, and genotoxic combined action of copper, zinc and lead oxides nanoparticles on the body.6 tbl
Packaged product of solid preparation containing 5-hydroxy-1h-imidazole-4-carboxamide, or its salt, or its hydrate // 2642670
FIELD: medicine.SUBSTANCE: invention relates to a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate and a medium regulating agent, as well as a method for solid preparation stabilizing. The packaged product of the present invention is characterized by the colour differences of the solid preparation being no more than 3, when evaluating the solid preparation surface before and after storage for 3 months under conditions of 40°C and relative humidity of 75%, or for four weeks under conditions of 60°C.EFFECT: invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate, with excellent stability of solid preparation during storage.6 cl, 1 tbl, 15 ex

Compositions of long-term action insulins // 2642662
FIELD: pharmacology.SUBSTANCE: group of inventions refers to an aqueous pharmaceutical composition containing 270-330 U/ml of glargine insulin [equimolar to 270-330 IU of human insulin], wherein the composition containing 300 U/ml of glargine insulin is excluded, for treatment of type I and II diabetes.EFFECT: application of these inventions allows to provide a basal insulin reserve within 24 hours after a subcutaneous injection of a single dose.16 cl, 9 dwg, 12 tbl, 18 ex

Concentrated therapeutic phospholipide compositions // 2642653
FIELD: pharmacology.SUBSTANCE: composition for treatment or prevention of cardiometabolic disorders, a metabolic syndrome, neurodegenerative disorders comprises a concentrated therapeutic phospholipid extract comprising compounds of Formula I wherein the total amount of the phospholipid compounds of Formula I from the extract is in a concentration of 60 wt % to 90 wt % of the total weight of the composition and the extract includes astaxanthin; to a capsule containing a concentrated therapeutic extract of krill oil that contains the phospholipid compounds of Formula I and the extract includes astaxanthin; to application of a composition that includes a concentrated therapeutic phospholipid extract containing compounds of Formula I for preparation of therapeutic compositions for serum triglyceride levels lowering; to application of a concentrated therapeutic phospholipid extract that contains compounds of Formula I for preparation of pharmaceutical compositions for treatment of cardiovascular diseases.EFFECT: increased mass percentage of phospholipids in the composition.20 cl, 35 dwg, 2 tbl, 7 ex
Processing of fish population by lufenuron // 2642637
FIELD: veterinary medicine.SUBSTANCE: drug is applied by oral administration of daily doses of 1 lufenuron to 30 mg/kg of fish biomass within a period of 3 to 14 days, while the total number of lufenuron used during the specified interval of time is from 7 up to 350 mg/kg of fish biomass.EFFECT: invention is suitable for treating salmon and provides continued effective protection against sea lice in the sea.10 cl, 6 tbl, 2 ex

Improved synergic antidiabetic compositions // 2642633
FIELD: pharmacology.SUBSTANCE: composition comprising inulin with a degree of polymerization (DP) below about 25, and a sulfonylurea and/or a derivative thereof, or a combination thereof, wherein the composition is synergic when used to treat or delay the onset of type 2 diabetes, and wherein the composition contains 5 mg to 50 g of inulin and 0.5 mg to 2000 mg of sulfonylurea and/or a derivative thereof, or a combination thereof. A method for treatment or delaying of the onset of type 2 diabetes. A method for treatment of hyperglycemia associated with type 2 diabetes. A method for prevention of development or alleviation of a side effect in a subject having type 2 diabetes treated with sulfonylurea and/or a derivative thereof or a combination thereof, wherein the side effect arises or is aggravated by treatment with sulfonylurea and/or a derivative thereof or a combination thereof. A method for prevention of development or alleviation of a pathological condition in a subject having type 2 diabetes or hyperglycemia associated with type 2 diabetes. A method for treatment or delaying of the onset of type 2 diabetes or treatment of hyperglycemia in a subject with type 2 diabetes.EFFECT: composition is effective for treatment or delaying of the onset of type 2 diabetes and acts synergistically.22 cl, 13 dwg, 13 tbl, 12 ex
Complex preparation for treatment of acute and chronic otites of parasitary, bacterial and fungical origin in dogs, cats, fur-bearing animals and rabbits // 2642617
FIELD: veterinary science.SUBSTANCE: this invention relates to veterinary medicine and can be used in the treatment of acute and chronic otitis of parasitic, bacterial and fungal origin in dogs, cats, fur-bearing animals and rabbits. Complex preparation in the form of eardrops contains levofloxacin, clotrimazole, dexamethasone, moxidectin, and also targeted additives.EFFECT: invention provides 100 % therapeutic efficacy for parasitizing of ear mites and 98–100 % efficacy for otites of bacterial and/or fungal etiology.1 cl, 4 ex
Cyclopropane carboxylate ethers of purine analogues // 2642463
FIELD: pharmacology.SUBSTANCE: invention relates to new cyclopropane carboxylate esters of purine analogues of the formula (T) or pharmaceutically acceptable salts thereof, which can be used for treatment of herpesvirus infections. Herpesvirus infection is an infection caused by the herpes simplex virus, infection of herpes zoster, or cytomegalovirus infection. In the compound of the formula (T) each Rx and Rz is independently hydrogen or (C1-C6)alkyl, or Rx is hydrogen and Rz is (C1-C6)alkyl, or Rx is (C1-C6)alkyl and Rz is hydrogen; and Ry is (C1-C6)alkyl, halo (C1-C6)alkyl, C6aryl, haloC6aryl or (C4-C5)heteroaryl with one heteroatom selected from nitrogen and oxygen in the ring.EFFECT: increased efficiency of compounds application.7 cl, 5 dwg, 3 tbl, 16 ex
Amide derivatives as grp119 agonists // 2642429
FIELD: pharmacology.SUBSTANCE: invention relates to an amide derivative of the following formula 1, its stereoisomers or its pharmaceutically acceptable salts of formula 1, wherein X1, X2, X3, X4, X5, X6, X7 and X8 each independently is C or N; R1 is -F or -C1-3-perfluorinated alkyl; R2 and R3 each is independently selected from the group consisting of halogen, -C1-5-alkyl and C3-6-cycloalkyl, wherein -C1-5-alkyl and C3-6cycloalkyl independently of one another may be unsubstituted or substituted by halogen, -CN, -OC1-5-alkyl or-C1-5-alkyl, or R2 and R3 together with the carbon atom to which they are attached, can form C3-6-cycloalkyl, where C3-6cycloalkyl may be unsubstituted or substituted by halogen, -OC1-5-alkyl or -C1-5-alkyl; R4 and R5 each independently is H, halogen or -C1-5-alkyl; R6 and R7 each independently is H, halogen, -C1-5-alkyl or -CN; R8 means methyl; R9 means H, halogen or OH; and m is 1 or 2. The invention also relates to individual compounds and to a pharmaceutical composition.EFFECT: new compounds of formula 1 are obtained that have the properties of GPR119 agonists, which can be used in diabetes mellitus treatment.7 cl, 15 tbl
N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines with antibacterial activity and method for their obtaining // 2642428
FIELD: pharmacology.SUBSTANCE: invention relates to new N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines of general formula I , where a: R1=R2=R3=H; b: R2=CH3, R1=R3=H; c: R2= OCH3, R1=R3=H; d: R1=R2=R3=OCH3 and a method for their preparation, in which 5-bromo-4-(5-nitrofuran-2-yl)pyrimidine (6) is mixed with the corresponding arylamine taken in 1.5 times excess, palladium (II) acetate and 1,1'-bis (diphenylphosphino)ferracene taken in catalytic amounts and potassium phosphate taken in 2.5-fold excess, the resulting mixture is dissolved in degassed 1,4-dioxane and heated at 85°C with vigorous stirring for at least 15 hours, followed by solvent distillation on a rotary evaporator under reduced pressure, and the resulting residue is subjected to chromatographic separation on a silica gel column with a ratio of ethyl acetate: hexane components of 1:3 in the eluent.EFFECT: highly effective method is proposed for the preparation of a compound that has a broad spectrum of antibacterial activity against coccal infections caused by gonococci or staphylococcus aureus, as well as purulent inflammatory infectious diseases of skin and mucous membranes caused by staphylococci and streptococci.2 cl, 1 tbl, 4 ex
1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2h-chromen-3-yl)-1,4-dihydroquinoline-3-carboxylic acid with anti-tubercular activity // 2642426
FIELD: pharmacology.SUBSTANCE: invention relates to a fluoroquinolone carboxylic acid derivative, namely 1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2H-chromen-3-yl)-1,4-dihydroquinoline-3 carboxylic acid of formula .EFFECT: high antitubercular activity, including that with respect to strains of mycobacteria with multiple drug resistance.2 tbl, 1 ex
ethod for prevention and treatment of dangerous neuroviral infections // 2642312
FIELD: medicine.SUBSTANCE: for treatment of dangerous neuroviral infections, mice are injected with Moliksan® in a single dose of 20.0 mg/kg of body weight immediately after infection and after 24, 48, 72 hours.EFFECT: increased effectiveness of combating diseases caused by pathogens of dangerous neuroviral infections.6 tbl

Cancer treatment using targeted antibodies in vivo // 2642305
FIELD: biotechnology.SUBSTANCE: antibody binding to claudine 6 (CLDN6) and inhibiting tumor growth in vivo is claimed. The antibody can be used as part of a pharmaceutical composition, in a method for treatment of tumor related to cells expressing CLDN6. The invention also relates to hybridomas producing antibodies to CLDN6 deposited under the accession numbers DSM ACC3059 (GT512muMAB 36A), DSM ACC3058 (GT512muMAB 27A), DSM ACC3057 (GT512muMAB 5F2D2).EFFECT: invention effectively inhibits the growth of CLDN6-positive germ cell tumors, improves survival and prolongs life of patients with tumors.17 cl, 18 dwg, 5 ex

Immunotherapeutic compositions on the basis of yeast-muc1 and methods of their use // 2642300
FIELD: biotechnology.SUBSTANCE: fusion protein is produced which contains the MUC1 antigen having an amino acid sequence that is at least 85% identical to the sequence of SEQ ID NO: 25 or at least 95% identical to the positions 92-566 of the sequence of SEQ ID NO: 25, and where MUC1 antigen contains 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 of the following amino acids L184, Y232, L233, V240, V241, L242, Y483, V497, L335, F536 and Y551.EFFECT: invention allows to effectively treat Mucin-1-expressing carcinomas, and also to prevent their metastatic progression.14 cl, 3 dwg, 5 tbl, 10 ex

P53 peptidomimetic macrocycles // 2642299
FIELD: biotechnology.SUBSTANCE: stable cross-linked p53 peptidomimetic macrocycle, a method for its preparation and its use are proposed. The p53 peptidomimetic macrocycle has a structure represented in the formula, and interferes with binding of p53 to MDM2 and/or p53 to MDMX. The P53 peptidomimetic macrocycle can be used to prepare pharmaceutical compositions for treatment of cancer characterized by undesirably low or low p53 activity and/or for the treatment of cancer characterized by undesirably high levels of MDM2 or MDMX activity.EFFECT: proposed cross-linked p53 macrocycle has cell permeability that is at least twice as high as that of the corresponding macrocycle without cross-links.50 cl, 7 dwg, 9 tbl, 22 ex

Hpv chimeric particle // 2642287
FIELD: biotechnology.SUBSTANCE: chimeric virus-like particle (VLP) of human papilloma virus (HPV), and method for its production and extraction, methods for prevention or treatment of HPV infection or cervical cancer, and for induction of an immune response in the patient, including the administration of proposed HPV VLP, as well as the application of the proposed HPV VLP in these methods and in production of pharmaceuticals to implement these methods, are proposed. The proposed chimeric HPV VLPS has a diameter of about 30 nm and contains a chimeric polypeptide HPV 16 L1/L2, which consists of a polypeptide HPV 16 L1, in which the peptide HPV 16 L2 from the amino acid residue 414 is inserted. The peptide contains from 13 to 26 amino acids. The amino acids of the inserted HPV 16 L2 peptide replace the corresponding amino acids of the HPV 16 L1 polypeptide. A method is also provided for the production of said HPV VLP in a plant in which successful assembly of small chimeric HPV VLPs, having a diameter of 30 nm, takes place.EFFECT: proposed group of inventions can be used in medicine for the prevention or treatment of HPV infection or in antitumor therapy for cervical cancer.28 cl, 32 dwg, 11 tbl, 3 ex

Composition for hyperlipidemia treatment containing oxyntomodulin derivative // 2642267
FIELD: biotechnology.SUBSTANCE: oxyntomodulin derivative with SEQ ID NO: 24, 25 or 26 fused to the Fc region of the immunoglobulin via a non-peptidyl polymer that covalently binds the oxyntomodulin derivative and the immunoglobulin Fc region is obtained.EFFECT: invention allows to obtain a conjugate of a oxyntomodulin derivative with a high ability to activate the GLP-1 receptor and a glucagon receptor compared to natural oxyntomodulin and to effectively lower the levels of total cholesterol, low density cholesterol and triglycerides in blood that have been elevated due to a high fat diet and to raise high-density cholesterol levels and high-density cholesterol - low-density cholesterol ratios.13 cl, 10 dwg, 3 tbl, 6 ex

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
Application of composition in medical products or drug manufacture for prevention and treatment of leukopenia caused by radiation and chemotherapy // 2642256
FIELD: pharmacology.SUBSTANCE: invention relates to application of a composition made from raw materials consisting of Radix Panacis Quinquefolii Ganoderma, or Radix Et Rhizoma Ginseng and fermented Cordyceps synesis powder and/or from Cordyceps, taken in a certain amount, in manufacture of medical products or drugs for prevention and treatment of radiation therapy or chemotherapy induced leukopenia in which the composition is obtained by raw materials mixing and extracting them with water and/or alcohol (versions).EFFECT: compositions described above are effective in the manufacture of medical products or drugs for prevention and treatment of radiotherapy or chemotherapy-induced leukopenia.25 cl, 36 tbl, 56 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
Compositions, synthesis and methods for application of phenylcycloalkylmethylamine derivatives // 2642074
FIELD: pharmacology.SUBSTANCE: invention relates to new phenylcycloalkylmethylamine derivatives of structural formula (I), or enantiomers or optically active isomers, or pharmaceutically acceptable salts having affinity for the binding of dopamine (DAT), the carrier of norepinephrine (NET) and the serotonin transporter (SERT). The compounds may find use in treatment and/or prevention of obesity, as well as depression 1. In the structural formula (I) ,n is 1; SP is a spacer, wherein the said spacer is C4 alkylene; X is O or S; R1 and R2 are independently H, C1-6 alkyl, C1-6 alkoxy, halogen; R3 is C1-6 alkyl; R4 is H or C1-6 alkyl; R5 is C1-6 alkyl; and * represents a carbon atom that can be optically active.EFFECT: improved composition properties.12 cl, 1 tbl, 86 ex
N-pyperonyl derivatives of daunorubicine, with antiprofliferative properties // 2642068
FIELD: pharmacology.SUBSTANCE: invention relates to the N-piperonyl derivatives of daunorubicine, which can be used in medicine, of general formula I where R=H, OCH3.EFFECT: new daunorubicine derivatives with antiproliferative properties and relatively low acute toxicity are proposed for cancer treatment, including non-small cell lung cancer, rhabdomyosarcoma, bowel carcinoma, breast adenocarcinoma.2 cl, 1 tbl, 2 ex
4-amino-3-methoxymethyl-5-phenyl-1h-pyrazole // 2642060
FIELD: pharmacology.SUBSTANCE: invention relates to preparation of new 4-amino-3-methoxymethyl-5-phenyl-1H-pyrazole previously not described. 4-amino-3-methylamide-5-phenyl-1H-pyrazole that has the following equation, derived from cycloaromatization of isonitrosodiketone and restoration of a new, not previously described intermediate - 4-nitroso-3-methylamide-5-phenyl-1H-pyrazole. The resulting target compound shows high antibacterial activity against E. coli (Escherichia coli strain ATCC 25822, sensitive to antibiotics) that allows its use in pharmacology to create antibacterial drugs. .EFFECT: increased efficiency of compounds application.2 ex
ethod for treatment of mouth cavity candidosis with lizobakt and cyclopheron by using removable orthopedic constructions // 2642053
FIELD: medicine; dentistry.SUBSTANCE: invention refers to medicine, namely to dentistry. In method of oral candidiasis treatment in patients with removable orthopedic structures, including correction of the prosthesis basis, as well as treatment of inflamed areas of the soft tissues of the prosthetic bed with a 3 % solution of hydrogen peroxide, followed by application to the treated areas of 10 % methyluracil emulsion, according to the invention, additionally, the lysobact is given topically 1 tablet 3 times a day, slowly dissolving the drug, at the time of using the drug, the orthopedic structures are removed; 1 pill of tsikloferon taken orally once a day 30 minutes before eating; duration of the therapy course is two weeks.EFFECT: method allows to eliminate the phenomena of hyperemia, swelling and soreness, thereby improving the patients life quality with complete or partial absence of teeth.1 cl, 1 tbl
ethod of prevention and treatment of nutritional disorders and increasing the resistance of cow organism // 2642052
FIELD: veterinary medicine.SUBSTANCE: invention relates to veterinary medicine, in particular to methods for normalizing metabolism and enhancing resistance in ruminant animals. Method includes intraperitoneal administration of an immunomodulator for treatment on the first day after calving, three times within 72 hours at intervals of 6–8 hours at a rate of 1 ml per 1 kg of live weight, as a prevention, the immunomodulator is administered at a dose of 1 ml per 1 kg of live weight for 3 days. Immunomodulator is a preparation in which glucose is used, bidistilled water as a solvent, and magnesium chloride, hexahydrate, potassium chloride, calcium chloride and sodium chloride as an active ingredient.EFFECT: invention provides improved metabolism, increased overall resistance and normalization of reproductive function of the organism of highly productive cows.1 cl, 1 ex, 3 tbl
ethod for morphological evaluation of influence of various dosage forms of iron for enternal application on small intestine in experimental animals // 2641979
FIELD: medicine.SUBSTANCE: pathohistological examination of the small intestine tissues is performed. Morphological criteria are determined: desquamation of the mucosal epithelium, necrosis of the mucous membrane, arterial-venous hyperemia, hemorrhage, mucosal edema, hemosiderosis of enterocytes, hemosiderosis of phagocytes. Further, the criteria are scored. The degree of influence of medicinal forms of iron on the small intestine (SPK) is calculated according to the claimed formula. The value of SPK from 0 to 1.2 points inclusive is assessed as a mild injury. SPK from 1.3 to 1.9 points inclusive - as an average injury. SPK from 2.0 to 3.0 points inclusive - as a serious injury.EFFECT: method allows to accurately and simply perform a morphological evaluation of the effect of various medicinal forms of iron for enteral administration on the small intestine in experimental animals by determining the most significant morphological criteria.2 tbl
Liquid stable viral vaccines // 2641970
FIELD: veterinary medicine.SUBSTANCE: liquid stable vaccine comprises a live attenuated canine virus, 10-30% (w/v) of saccharic adjuvant, and an amino acid, wherein the liquid stable vaccine has pH value from 6.0 to 8.0. The amino acid is selected from the group consisting of arginine and methionine; if the amino acid is arginine, then its final concentration in the liquid stable vaccine is from 0.15 to 0.6 M. If the amino acid is methionine, its final concentration in the liquid stable vaccine is from 0.025 to 0.3 M. A live attenuated canine virus is selected from the group consisting of the canine distemper virus, canine adenovirus of the 2 type, canine parvovirus and canine parainfluenza virus, or any combination thereof.EFFECT: usage of the above-mentioned stabilization principle allows to produce liquid stable composition for a live attenuated canine distemper virus, canine adenovirus of the 2 type, canine parvovirus and canine parainfluenza virus.12 cl, 2 ex, 5 tbl
Injectable veterinary composition // 2641962
FIELD: veterinary medicine.SUBSTANCE: to treat bacterial infection, an injectable veterinary composition containing quinolone and cephalosporin or their pharmaceutically acceptable salts with propylene glycol with dicaprilocaprate and/or glycerylcaprilocaprate in an oil suspension is administered to the animal. An injectable veterinary composition for bacterial infection treatment in an animal, comprising at least one other therapeutic agent in an oil suspension, is also provided.EFFECT: group of inventions allows treatment of bacterial infection in pigs or cattle.13 cl, 3 tbl, 3 dwg, 3 ex
3-aminocyclopentancarboxamide derivatives // 2641913
FIELD: chemistry.SUBSTANCE: invention relates to the individual compounds selected from the group: 4-(1,3-benzoxazole-2-yl)]-N-[(1R,3S)-3-(ethylcarbamate)cyclopentyl]-N-methylbenzamide, N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methyl-4-(1-methyl-1H-benzoimidazol-2-yl)-benzamide, 4-benzothiazol-2-yl-N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methylbenzamide, ((1R,3S)-3-ethylcarbamoylcyclopentyl)-methylamide4'-[(R)-(tetrahydrofuran-3-yl)oxy]-biphenyl-4-carbon acid, 4-benzoxazole-2-yl-N-((1R,3S)-3-isopropylcyclopentadienyl)-N-methylbenzamide, and other compounds that are specified in the claims. The invention also relates to medicinal means having an inhibiting activity against fatty acid synthase (FAS) containing therapeutically effective amount of the compound of the invention.EFFECT: new compounds are obtained that have an inhibiting activity against the synthesis of fatty acids.2 cl, 2 tbl, 12 ex
New semi-synthetic eremomycine derivative and its application // 2641912
FIELD: pharmacology.SUBSTANCE: invention relates to a new semi-synthetic derivative of glycopeptide eremomycine antibiotic, which is eremomycine tetramethylenimide of formula , and its pharmaceutically acceptable salts. A method for production of eremomycine tetramethylenimide of formula 2, its pharmaceutical compositions and their use for treatment of mammalian infections caused by gram-positive bacteria, including insensitive or low-sensitive to other antibiotics.EFFECT: compound efficiency increase.6 cl, 4 tbl, 6 ex

Crystalline forms of complexes useful as sglt2 inhibitors, and methods of their obtaining // 2641905
FIELD: chemistry.SUBSTANCE: invention relates to the crystalline form of the complex (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-ylpropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, bis(L-proline) characterized by an X-ray powder diffraction pattern comprising peaks at 4.08, 17.19, and 21.12 degrees 2θ (±0.05 degrees 2θ), wherein the said X-ray powder diffraction pattern is obtained using CuKα1 radiation.EFFECT: provided complex has an inhibitory effect on the sodium-dependent SGLT transporter.7 cl, 1 tbl, 3 dwg, 7 ex

New salicylic acid derivatives, their pharmaceutically acceptable salt, compositions and method for application // 2641903
FIELD: pharmacology.SUBSTANCE: invention relates to a number of other similar specific compounds, pharmaceutical compositions, comprising these compounds and their application to obtain a drug to inhibit the STAT3 and/or STAT5 activity or to treat cancer, where the cancer cells contain activated STAT3 or STAT5. , , , .EFFECT: preparation of a drug for STAT3 and STAT5 activity inhibition or for cancer treatment where the cancer cells contain activated STAT3 or STAT5.20 cl, 21 dwg, 6 tbl, 76 ex
N-[3-oxolup-20(29)-ene-28-oil]-2,2,6,6-tetramethylpiperidine-4-ylamine with cytotoxic activity in respect of human tumour cells // 2641900
FIELD: pharmacology.SUBSTANCE: invention relates to N-[3-oksolup-20(29)-ene-28-oil]-2.2,6,6-tetramethylpiperidine-4-ylamine of the structural formula with cytotoxic activity against human tumour cells.EFFECT: new compound is obtained that has an ability to suppress the growth of human tumour cells.2 tbl, 3 ex
Heterocyclic pyrimidine analogues as tyk2 inhibitors // 2641895
FIELD: pharmacology.SUBSTANCE: compounds possess the properties of the inhibitor of the non-responsive tyrosine Tyk2 kinase and selective inhibitory action against JAK1, JAK2, JAK3 Janus kinases. The compounds can be used in a method for treatment or prevention of immunological, inflammatory, autoimmune, allergic disorder or graft rejection or graft-versus-host diseases. In the formula (I) , R1 is H; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R3, which are the same or different. At that, C 1-6 alkyl containing a hydroxy group may be deuterated; R3 represents halogen; CN; C(O)OR4; OR4; C(O)R4; (O)N(R4R4a); S(O)2R4; S(O)R4; or T1; R4, R4a, R4b are independently selected from the group consisting of H; T1; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R5, which are the same or different; R5 represents halogen; CN; OR6; or T1; R6 is H; T1 is C3-7 cycloalkyl; 4-7 membered heterocyclyl with 1 to 2 heteroatoms in the ring selected from nitrogen, oxygen or sulfur; or a 7-8 membered heterobicyclyl, optionally spyrocondensed, with two heteroatoms in the cycle, selected from nitrogen or nitrogen and oxygen, where T1 is optionally substituted by one or more R7 , which are the same or different; R7 is halogen; CN; C(O)OR8 ; oxo (= O), wherein the ring is at least partially saturated; C 1-6 alkyl; R 8 are independently selected from the group consisting of H; C1-6 alkyl; X1 is C(R11a) or N; X2 is C(R11b) or N; X3 is C(R11c) or N; X4 is C(R11d) or N; X5 is C(R11e) or N, provided that no more than two of X1, X2, X3, X4, X5 are N; R11a, R11c, R11e are independently selected from the group consisting of H; halogen; CN; OR12; C(O)N(R12 R12a); S(O)2N (R12R12a); S(O)2R12; T2; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R11b, R11d are independently selected from the group consisting of H; halogen; CN; OR12; S(O)2N (R12R12a); S(O)R12; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R12, R12a are independently selected from the group consisting of H and C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; T2 is a 5-membered heterocycle with two nitrogen atoms in the ring; R13 is halogen; CN; OR14; C(O)N (R14R14a); S(O)2N(R14R14a); S(O)2R14; S(O) R14; N(R14) S(O)2N(R14aR14b); N(R14)S(O)N(R14aR14b); SR14; N(R14R14a); NO2; OC(O)R14; N(R14)S(O)2R14a; R14, R14a, R14b are independently selected from the group consisting of H or C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R15, which are the same or different; R15 is halogen.EFFECT: increased efficiency.18 cl, 13 tbl, 480 ex
Azole derivatives of benzene // 2641891
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 means OR, NRR', which can form a ring, or SR. Wherein R and R' independently mean hydrogen atom, linear, cyclic or branched alkyl containing 1-8 carbon atoms, and optionally substituted by one or more linear, circular, or branched alkoxygroup containing 1-8 carbon atoms, halogen atoms or hydroxyl groups, monocyclic or bicyclic aryl containing 6-10 carbon atoms, optionally substituted by one or more linear, cyclic or branched alkyl containing 1-8 carbon atoms, linear, cyclic or branched alkoxygroup containing 1-8 carbon atoms, or halogen atoms, where the term "NRR' forms a ring" means that R and R' join to form pyrrolidine-1-yl group; R2 means a hydrogen atom or a linear, cyclic or branched alkyl containing 1-8 carbon atoms; X1, X2 and X3 mean independently CR3 or a nitrogen atom, or X1 means CR3 or a nitrogen atom, and X2 and X3 together form a benzene ring. Moreover, R3 means a hydrogen atom or a linear, cyclic or branched alkyl having 1-8 carbon atoms. The invention also relates to specific compounds corresponding to formula (I). The invention relates to an intermediate compounds represented by the formulas, and , where R1, R2, X1, X2 and X3 correspond to the values given for compounds of formula (I) and R4 means protective group of the carboxylic group, selected from methyl, ethyl, isopropyl, heptyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, propanol and benzyl, and R5 means a protective group of phenolic hydroxyl group selected from methyl, isopropyl, allyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, 1-ethoxyethyl, benzyl, 4-methoxybenzyl, acetyl, trimethylsilyl, t-butyldimethylsilyl. The compounds of the invention of formula (I) have an inhibitory activity against xanthine oxidase.EFFECT: azole derivatives of benzene as inhibitors of xanthine oxidase.19 cl, 15 tbl, 58 ex

Polymeric hydrogels and methods for their preparation // 2641749
FIELD: pharmacology.SUBSTANCE: invention relates to a polymeric hydrogel comprising carboxymethyl cellulose and citric acid. This citric acid participates in the formation of cross-links in carboxymethylcellulose, wherein the said polymeric hydrogel has a swelling ratio of 50 to 300. The invention also relates to application of said hydrogel for use in the treatment of obesity in a patient in need thereof, as well as for the manufacture of a medicament for obesity treatment in a patient in need thereof.EFFECT: increased application efficiency.12 cl, 2 dwg, 8 tbl
5-(pyridine-2-ylamino)-pyrasin-2-carbonitrile compounds and their therapeutic application // 2641693
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula , as well as to pharmaceutical compositions based thereon for use in the treatment of a disease or condition mediated by SNK1.EFFECT: new compounds are obtained that inhibit the kinase function of kinase 1 of the control point.37 cl, 2 dwg
New anti-invasive compounds // 2641650
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, which can be used to prevent, and/or inhibit, and/or treat cancer. In formula (I) A and A' independently represent phenyl or pyridylene group; R2 represents a hydrogen or alkyl group (C1-C4); R3 represents a 2-pyridyl group, 3-pyridyl group, 4-pyridyl group, 2-pyrimidinyl group, 4-pyrimidinyl group or 5-pyrimidinyl group; R4 represents a carbonyl group or sulfonyl group; R5 is a -NH-(CH2)(a)-NR6R7 group or a 4-methylpiperazinyl group and a is an integer from 1 to 4, R6 and R7 independently represent a nalkyl group (C1-C4) or R6 R7 together with nitrogen atom they are bounded to form a heterocyclic group selected from 4-methylpiperazinyl group, morpholine group, pyrrolidinyl group and piperidine group. The invention also relates to a method for preparation of compounds of formula (I) and a pharmaceutical composition containing them.EFFECT: improved compounds properties.16 cl, 6 tbl, 17 ex
ethod for complex empirical antibacterial therapy of implant-associated orthopedic infections // 2641608
FIELD: medicine.SUBSTANCE: for complex empirical antibacterial therapy of implant-associated orthopedic infections, bone defect replacement with a cement spacer is performed. Then the wound is sutured. Antibacterial therapy is prescribed, which has simultaneous local and systemic effect on the focus of infection. At that, an antibacterial drug is added to the cement when the spacer is mixed and injected systemically after the operation. This antibacterial drug is allowed for regular use and is characterized by the presence of a freeze-dried form, thermostability, water solubility, a wide range of activity, including methicillin-resistant Staphylococcus. Moreover, the systemic therapy is complemented with an antibiotic having a synergic action in terms of leading pathogens of the implant-associated infection, but belonging to another group.EFFECT: invention allows to increase the effectiveness of etiotropic antibacterial therapy for implant-associated orthopedic infections.1 ex
Antimicrobial composition for use in otorhinolaryngology // 2641607
FIELD: pharmacology.SUBSTANCE: antimicrobial composition for use in otorhinolaryngology containing hydroxymethylquinoxaline dioxide, polyvinylpyrrolidone and dexamethasone is described, with the following component ratio, wt %: polyvinylpyrrolidone 45.0-55.0, hydroxymethylquinoxaline dioxide solution 10 mg/ml 30.0-33.0, dexamethasone solution 4 mg/ml 12.0-25.0.EFFECT: antimicrobial composition has a prolonged action due to its high viscosity and adsorption capacity, providing long-term exposure to active substances and reducing the incidence of invasive procedures in otorhinolaryngology.2 ex
Antiseptic drug // 2641309
FIELD: pharmacology.SUBSTANCE: invention relates to the organic heterocyclic compounds chemistry, namely a new quaternary ammonium salt containing a fragment of a vitamin B6 derivative of formula I , which exhibits antibacterial, antimycotic, antiviral and antiprotozoal properties.EFFECT: compound can be used in medicine and veterinary medicine.2 cl, 2 dwg, 16 tbl

Cyclohexanoxycarbonyl-dipeptide and its antiviral activity against hepatitis c virus // 2641297
FIELD: pharmacology.SUBSTANCE: invention relates to new synthetic compounds, namely to the N-acyl derivative of dipeptide, which is cyclohexyloxycarbonyl-prolyl-tryptophan (Cho-Pro-Trp-OH). Cho-Pro-Trp-OH inhibits reproduction of the hepatitis C virus (HCV), and also has a virucidal effect against HCV. The compound has a low toxic effect on the monolayer of the transplantable kidney cell line in the pig embryo (SPEV). .EFFECT: compound can be recommended for creation of new antiviral drugs, used both as an individual agent and as part of compositions for hepatitis C treatment.3 cl, 6 dwg, 3 tbl, 5 ex

Pharmaceutical composition for cancer treatment and prevention // 2641260
FIELD: pharmacology.SUBSTANCE: invention relates to an antibody or a binding fragment thereof that specifically binds to the CAPRIN-1 protein and has immunological reactivity to the partial CAPRIN-1 polypeptide. Also a conjugate, as well as a pharmaceutical composition and a pharmaceutical combination for treatment or prevention of a malignant tumour expressing CAPRIN-1 are disclosed. The invention also relates to a method for treatment or prevention of a cancer expressing CAPRIN-1 using the above antibody or a fragment thereof, a conjugate, a composition or a combination.EFFECT: invention enables efficient treatment or prevention of cancer expressing CAPRIN-1.19 cl, 12 ex

Glp-1 peptides compositions and their production // 2641198
FIELD: pharmacology.SUBSTANCE: group of inventions concerns pharmaceutical compositions for treatment of diabetes or obesity, containing the first type of granules and the second type of granules, where the specified first type of granules contains the salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and does not contain GLP-1 peptide, and where the specified second type of granules contains GLP-1 peptide and does not contain the salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, and also refers to methods for composition production and application in medicine.EFFECT: improving the bioavailability of the GLP-1 peptide.33 cl, 10 ex, 12 tbl

ethod of obtaining supramolecular hydrogel // 2641111
FIELD: chemistry.SUBSTANCE: method of obtaining supramolecular hydrogels includes mixing an aqueous solution of L-cysteine with the silver acetate aqueous solution so that the concentration of L-cysteine in the mixture is in the range of 1.0 to 6.0 mmol, and the ratio of molar concentrations of silver acetate to L-cysteine in the mixture is in the range of 1.23 to 1.33, where the mixture is left in a dark place at room temperature for 4 hours for the formation of the L-cysteine-silver solution. Then, the mature L-cysteine-silver solution is mixed with an aqueous solution of sulfate with a cation from the series Na+, K+, Cu2+, Fe2+, Mg2+, Zn2+, Al3+, Ni2+, Co2+, Mn2+ at a concentration of sulfate in the mixture in the range of 0.075-0.750 mmol, after a certain time, depending on the concentration of sulphate and the type of cation, after which the liquid system becomes a gel.EFFECT: improved method.2 tbl, 6 dwg

Salt of nitrogen-containing heterocyclic compound or its crystalline form, pharmaceutical composition and flt3 inhibitor // 2641106
FIELD: pharmacology.SUBSTANCE: invention relates to new salts of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide selected from succinate, fumarate, pamoate, hydrochloride, phosphate, sulfate and hydrobromide, as well as crystalline salt forms. The compounds possess the properties of FLT3 (Fms-like tyrosine kinase 3) inhibitor and can be used to treat blood carcinoma including various forms of leukemia, for example acute lymphatic leukemia (ALL), acute myeloid leukemia (AML), acute promyelocytic leukemia (APL), chronic lymphocytic leukemia (CLL), and others. Crystalline α succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 10.5, 17.1, 19.1 and 22.4°; crystalline β succinate of this compound demonstrates diffraction peaks at diffraction angles of (2θ) 12.8, 16.1, 21.4 and 28.0°. Crystalline fumarate of the said compound on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 8.6, 13.7, 17.8 and 23.0°.EFFECT: salts have storage stability or high solubility.9 cl, 6 dwg, 10 tbl, 13 ex
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
Biaryl derivatives as agonists gpr120 // 2641003
FIELD: pharmacology.SUBSTANCE: invention relates to diaryl derivatives of the formula 1 , or their pharmaceutically acceptable salts or isomers of formula 1, wherein A and B are independently phenyl or pyridine provided that when B is phenyl, -G-COOR7 is substituted in the para-position of phenyl and, when B is pyridine, -G-COOR7 is substituted in position 3 of pyridine, any of R1-D and R2-E may be absent, D and E are independently carbon, nitrogen, oxygen or sulfur, or represent a direct bond, and any of R1 and R2 may be absent, or R1 is a halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted by C3-C10-alkylsilanyloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted by C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl, R2 is hydrogen, halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted with C3-C10-alkylsilaniloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted with C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl and, when D and E represent nitrogen or carbon, R1 and R2 may represent two or three groups, which may be the same or different, isolated from C1-C6-alkyl or phenyl, G is -J-(CR5C6)p, where J is oxygen or sulfur, R5 and R6 independently represent hydrogen, C1-C6-alkyl or C3-C10-cycloalkyl and R5 and R6, substituted in the one and the same or different carbon atoms, may be bound producing C3-C10-cycloalkyl, R1 and R4 independently from each other may be absent depending on m and n value or independently represent hydrogen, halogen or C1-C6-alkyl, or C1-C6-alkoxy, R7 is hydrogen or C1-C6-alkyl, m and n independently represent an integral number from 0 to 5 and p is an integral number from 2 to 6, where heterocycloalkyl and heteroaryl contain at least one heteroatom, isolated from N, O, and S, to the pharmaceutical composition, containing them, and method of its production.EFFECT: stimulates the formation of GLP-1 in the gastrointestinal tract and improves insulin resistance in the liver or muscles, effective prevention or treatment of diabetes, complications of diabetes, obesity, non-alcoholic fatty hepatosis, steatohepatitis, osteoporosis or inflammation.6 cl, 1 tbl, 279 ex
 
2550932.
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