Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics (A61P31)

A   Human necessities(312709)
A61P31                 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics(3672)
A61P31/02 - Local antiseptics(137)
A61P31/04 - Antibacterial agents(1186)
A61P31/06 - For tuberculosis(306)
A61P31/08 - For leprosy(15)
A61P31/10 - Antimycotics(279)
A61P31/12 - Antivirals(672)
A61P31/14 - For rna viruses(147)
A61P31/18 - For hiv(228)
A61P31/20 - For dna viruses(44)
A61P31/22 - For herpes viruses(121)

ethods of glycogonjugation and composition // 2645071
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, namely to vaccine prevention, and discloses a method for preparing a glycoconjugate comprising bacterial capsular polysaccharide conjugated to a carrier protein via (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, glycoconjugate, and the immunogenic composition containing said glycoconjugate.EFFECT: inventions allow to obtain suitably blocked conjugates based on a carrier protein, which maintain the functional properties of the carrier and the conjugate itself retains the ability to induce the desired immune response.16 cl, 15 tbl, 9 ex, 8 dwg

ethod for treatment of patients with hemorrhagic fever with renal syndrome in case of liver dysfunction development // 2645067
FIELD: medicine.SUBSTANCE: invention is designed to treat patients with hemorrhagic fever with renal syndrome (HFRS), accompanied by liver dysfunction. As part of basic therapy, intravenous dropwise introduction of 400 ml of remaxol is provided once a day for 10 days. Additionally, as a part of complex therapy, cytoflavin is administered orally twice a day (2 pills) and 250 mg of methionine hepatoprotector is introduced 3 times a day for 20 days.EFFECT: method allows reduce the duration of the disease, reduce manifestations of intoxication and cytolytic syndromes, and improve the quality of life of patients.8 tbl, 1 ex
-4-[6-(purine-6-ylamino)hexanoyl]-3,4-dihydro-3-methyl-7,8-difluor-2h-[1,4]benzoxazine and (3r)-4-[6-(purine-6-ylamino)hexanoyl]-3,4-dihydro-3-methyl-7,8-difluor-2h-[1,4]benzoxazine with antiviral activity // 2644351
FIELD: pharmacology.SUBSTANCE: invention relates to new purine derivatives of the formulas: .EFFECT: new derivatives possessing selective antiviral activity against herpes simplex viruses 1 and acting on viral strains with drug resistance to acyclovir and related compounds are obtained.3 cl, 1 tbl, 3 ex
Drug with activity against gram-positive bacteria, microbacteria and fungi // 2644250
FIELD: pharmacology.SUBSTANCE: drug is a compound of the perimidinone class of the derivatives of salicylic aldehyde and perhydropyrimidine-2,4,6-trions of the general formula 1, where X1, X3 are selected from the group: H, halogen, NO2; X2, X4 represent H; Z is selected from the group: O, NNH2, NOH, perhydropyrimidin-5-ylidene-2,4,6-trione, substituted on the nitrogen atom by a methyl, allyl, methoxybenzyl, phenyl group; Y is selected from the group: H, Na, Li, K.EFFECT: invention implementation allows to obtain new chemical compounds with a high antibacterial activity and a greater range of action.4 ex, 3 tbl

Compositions containing secretor-like immunoglobulins // 2644240
FIELD: biotechnology.SUBSTANCE: method for in vitro preparation of a composition comprising a secretor-like immunoglobulin comprising the steps of production of a protein composition isolated from blood containing an immunoglobulin containing a J-chain in a crude form and mixing of the composition of step (a) with a secretory component. A composition for use in medicine comprising secretor-like IgA and/or secretor-like IgM or a combination thereof obtained by the described method is provided.EFFECT: increased efficiency of composition application.17 cl, 8 dwg, 5 ex

Single-domain antibodies to ebola virus gp protein for immunotherapy of ebola fever // 2644202
FIELD: biotechnology.SUBSTANCE: presented single-domain and oligomeric antibodies contain an antigen-binding amino acid sequence, selected from a group consisting of sequences SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, on the basis of which compositions, intended for the prevention and treatment of infection of mammals caused by Ebola virus, are created.EFFECT: proposed antibodies bind to the GP protein of the Ebola virus and have a virus-neutralizing activity and protect against infection and development of the infection in vivo.6 cl, 10 dwg, 4 tbl, 9 ex
Prodrug of polymerase ns5b hcv inhibitor, method for its preparation and application // 2644156
FIELD: medicine; pharmaceuticals.SUBSTANCE: present invention relates to a novel prodrug which is cyclobutyl (S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-ylmethoxy]phenoxy-phosphorylamino}-propanoate of general formula 1, its stereoisomer, or polycrystalline form. Stereoisomers of this compound are cyclobutyl (S)-2-{(S)-[(2R,3R,4R,5R)-5-(3,4-dihydro-2,4-dioxo-2H-pyrimidin-1-yl)-3-hydroxy-4-methyl-4-fluoro-tetrahydrofuran-2-ylmethoxy]-phenoxy-phosphorylamino}-propanoate of formula 1.1 or cyclobutyl (S)-2-{(R)-[(2R,3R,4R,5R)-5-(3,4-dihydro-2,4-dioxo-2H-pyrimidin-1-yl)-3-hydroxy-4-methyl-4-fluoro-tetrahydrofuran-2-ylmethoxy]-phenoxy-phosphorylamino}-propanoate of formula 1.2. Polycrystalline form of these compounds is a mixture of rhombic and monoclinic forms. Crystalline form is a rhombic form. Method for preparation of the prodrug of formulas 1, 1.1 and 1.2 is the reaction of cyclobutyl (S)-2-(pentafluorophenyloxy-phenoxy-phosphorylamino)-propionate of formula 2 or cyclobutyl (S)-2-((S)-pentafluorophenyloxy-phenoxy-phosphorylamino)-propionate of formula 2.1 or cyclobutyl (S)-2-((R)-pentafluorophenyloxy-phenoxy-phosphorylamino)-propionate of formula 2.2 with tert-butyl(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl)-2-(hydroxymethyl)-4-methyl-4-fluoro-tetrahydrofuran-3-yl carbonate of formula 7 in the presence of an alkyl magnesium halide, followed by deprotection. EFFECT: prodrug has the properties of a polymerase NS5B HCV inhibitor and can be used in treatment of hepatitis C.10 cl, 10 ex, 3 tbl
Composition for prevention and treatment of aids and method of its production // 2643919
FIELD: pharmaceutics.SUBSTANCE: present invention relates to pharmaceutical composition, namely to agent for preventing and treating AIDS. Composition for prevention and treatment of AIDS, characterized by that the active components of the composition consist of aqueous and/or ethanol extracts of the following raw materials: 5–200 parts by weight of Ganoderma, 5–150 parts by weight of Radix Panacis Quinquefolii or Radix Et Rhizoma Ginseng, 1–90 parts by weight of powder fermented with Cordyceps sinensis and/or 1–120 parts by weight of Cordyceps. Composition for prevention and treatment of AIDS, characterized by that the active components of the composition consist of aqueous and/or ethanol extracts of the following raw materials: i) 5–200 weight parts of Ganoderma, ii) 5–150 parts by weight of Radix Panacis Quinquefolii or Radix Et Rhizoma Ginseng, iii) 1–90 parts by weight of powder fermented with Cordyceps sinensis and/or 1–120 parts by weight of Cordyceps and iv) one or any combination of: 5–90 parts by weight of Flos Rosae Rugosae, 5–150 parts by weight of Ganoderma spore powder, 10–400 parts by weight of Radix Pseudostellariae, 3–400 parts by weight of Radix Codonopsis and 3–400 parts by weight of Radix Astragali. Method for preparing the composition (variants). Use of the composition in preparation of a medical product, drug or product for prevention and treatment of AIDS.EFFECT: compositions described above are effective for prevention and treatment of AIDS.18 cl, 45 ex, 1 tbl

Polyethylene glycol compositions for control of relapses of labial herpes, genital herpes and herpes zoster // 2643763
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry, namely to method for reducing the frequency of relapses of labial herpes in patient, which comprises topical administration of therapeutically effective amount of polyethylene glycol (PEG) as an active agent, which is either (i) PEG with average molecular weight of 200–800, or (ii) mixture of (a) PEG with average molecular weight of 200–800 and (b) PEG with average molecular weight of 1000–15000, wherein the weight ratio (a) to (b) ranges from 3:1 to 20:1, wherein said method is performed for at least 4 weeks; topical administration is carried out 1–5 times a day on the lips and/or around the lips of the patient.EFFECT: invention provides reduction or prevention of relapses of labial herpes.53 cl, 1 ex, 9 tbl, 1 dwg
eans for cattle treatment at necrobacteriosis // 2643592
FIELD: veterinary medicine.SUBSTANCE: agent contains magnesium sulfate - 29.0; sodium sulfate - 30,0; copper sulfate 5.0; zinc sulphate - 5.0; polyvinyl alcohol (powder) - 30.5-32.0; novocaine powde - 0.5.EFFECT: invention provides creation of an agent for cattle treatment at necrobacteriosis, which allows to increase the therapeutic effect by expanding the spectrum of bactericidal action and relieving pain in sick animals.3 ex, 2 tbl
ethod for preparation of ethyl 3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,5,10-trioxo-10b-phenyl-1,2,3,5,10,10b -hexagydro-3ah-naphto [2',3':4,5]furo[3,2-b]pyrrol-3a-carboxylates // 2643372
FIELD: pharmacology.SUBSTANCE: invention relates to a method for preparation of new compounds - ethyl 3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,5,10-trioxo-10b-phenyl-1,2,3,5,10,10b-hexahydro-3aH-naphtho[2',3':4,5]furo[3,2-b]pyrrole-3a-carboxylates of the general formula I , where R=CH2Ph(a), C6H11-c(b), Ph(c), C6H4OMe-4 (d), C6H4Me-4 (e), C6H4Cl-4 (f), Me(g) by reacting 5-phenyl-4-ethoxycarbonyl-1H-pyrrole-2,3-dione with 2-hydroxynaphthalene-1,4-dione in a 1:2 ratio in the presence of acetic acid in an inert aprotic solvent environment.EFFECT: obtaining of new compounds that can be used as ingredients for synthesis of new heterocyclic systems and in pharmacology as having antimicrobial activity.3 cl, 1 tbl, 2 ex
New compounds // 2643371
FIELD: pharmaceutics.SUBSTANCE: invention refers to the new compound of formula (I) or its pharmaceutically acceptable salt possessing the properties of interferon inducer α (IFN-α) and tumor necrosis factor α (TNF-α). In the formula (I) R1 it represents n-C3-6alkyl; R2 represents hydrogen or methyl; R3 is hydrogen or C1-6alkyl; m is an integer that has the value from 0 to 3.EFFECT: compounds can be applied for the treatment of allergic diseases and inflammatory states, infectious diseases and cancer.15 cl, 3 ex
Injectable antibiotic formulations and methods of their use // 2643327
FIELD: chemistry.SUBSTANCE: group of inventions refers to chemical-pharmaceutical industry and presents a ready-to-use antimicrobial composition comprising penetamate (PNT) or a pharmaceutical equivalent thereof and at least one oily vehicle, a non-gelling, caking-inhibiting agent, wherein the composition is formulated in such a way, that the viscosity of the composition is below 3000 mPa∙s at a temperature of 20 °C, and a way of its manufacturing. Group of inventions also includes a method of treating an animal with a composition as described above, for treating or preventing mastitis, wherein the method comprises intramuscular or subcutaneous injection.EFFECT: group of inventions allows to provide a long-term stability of the oil-based composition during storage, as well as a rapid release of the injectable active agent.22 cl, 16 dwg, 8 tbl, 6 ex

Lyophilized drug nanosuspensions // 2643062
FIELD: pharmacology.SUBSTANCE: present invention relates to a lyophilized (also known as freeze-dried) drug nanosuspension comprising of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile or its stereoisomeric form or its pharmaceutically acceptable salt and a steric stabiliser, which is a solid at room temperature, and polyvinyl pyrrolidone.EFFECT: according to the present invention the composition of the lyophilized drug nanosuspension has an acceptable stability of grain-size composition in storage, including long-term storage.25 cl, 6 dwg, 7 tbl, 2 ex
Application of cyclohexanol derivatives as antimicrobial active compounds // 2642987
FIELD: pharmacology.SUBSTANCE: application of at least one cyclohexanol derivative of the formula (Ia) and/or (Ib) as an antimicrobial active compound is proposed, application of the same compounds as an anti-acne, antiperspirant, antiperspirant or deodorant active compound, a drug with antimicrobial action comprising at least one cyclohexanol derivative of formula (Ia) and/or (Ib), with exception of 2-hydroxycyclohexane-1-carboxylic acid, individual cyclohexanol derivatives of formula (Ia) and/or (Ib).EFFECT: bacteriostatic action of compounds against Staphylococcus epidermidis, suppression of growth and reproduction of other gram-positive and gram-negative bacteria, yeast, fungi or viruses.15 cl, 16 ex
Selective antibacterial agents, represented by 3-(azol-1-yl)-6-amino-substituted 1,2,4,5-tetrazines // 2642882
FIELD: pharmacology.SUBSTANCE: invention relates to 3-(azol-1-yl)-6-amino substituted 1,2,4,5-tetrazines of the formula: , where Het = imidazol-1-yl, NHR = allylamino (Ia); Het = 4-methylimidazol-1-yl, NHR = allylamino (Ib); Het = benzimidazol-1-yl, NHR = allylamino (Ic); Het = indazol-1-yl, NHR = allylamino (Id); Het = imidazol-1-yl, NHR = propargylamino (Ie); Het = 4-methylimidazol-1-yl, NHR = propargylamino (If); Het = benzimidazol-1-yl, NHR = propargylamino (Ig); Het = indazol-1-yl, NHR = propargylamino (Ih). The invention also relates to antibacterial agents.EFFECT: new compounds of formula I, active against gram-negative bacteria Neisseria gonorrhoeae and clinically relevant pathogenic and opportunistic microorganisms, are obtained.2 cl, 2 tbl, 8 ex
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
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
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
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
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
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
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
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

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
Combination of fulvic acid and antibiotic for suppression of growth of bacteria resistant to majority of drugs, or treatment of infections caused by them // 2640928
FIELD: pharmacology.SUBSTANCE: invention relates to combinations for treatment of infections caused by gram-negative bacteria positive for NDM-1 producing carbapenemase. The combination includes fulvic acid or a salt thereof as an active ingredient and meropenem.EFFECT: increased effectiveness of treatment, while the synergistic effect of fulvic acid and meropenem is observed.6 cl, 2 dwg, 5 tbl, 2 ex

Therapeutic application of compounds // 2640596
FIELD: pharmacology.SUBSTANCE: invention refers to the application of a compound of formula R1-COOH (I), where R1 is an alkyl group with a main chain of 7-11 carbon atoms, possibly branched in any position of the carbon atom in the main chain, where branching is a side C1-6 alkyl group. The alkyl group of the main chain and/or the side alkyl groups optionally contain one or more heteroatoms. The specified compound is selected from 4-ethyl octanoic acid, 2-butyl octanoic acid, 4-methyl nonanoic acid and 3-methyl undecanoic acid or its pharmaceutically acceptable salt, amide or ester, for treatment or prevention of disease or biomedical state, selected from disorders associated with cramps.EFFECT: increased efficiency of the composition and treatment method.2 cl, 9 dwg, 3 tbl
Antiseptic composition intended for application in oral cavity, for treatment of oral mucositis // 2640301
FIELD: pharmacology.SUBSTANCE: application of antiseptic composition is proposed. The composition is in the form of a solution for local administration in the mouth cavity, and the composition contains one antiseptic agent, isolated from a group, consisting of hydrogen peroxide and carbamide peroxide and their mixture, cetylpyridinium chloride, or their mixtures; ether oil, isolated from eugenol; phenolic antiseptic agent, isolated from vapour chlorophenol; agent having antiseptic properties, isolated from camphor; plant extract, isolated from wild chamomile, and auxiliary substances. In addition, in this invention a method for treatment of oral mucositis and stomatitis is proposed. It is associated with anticancer therapy, including production of the antiseptic composition and administration of the composition, designed for use in mouth cavity, in the mouth cavity of the patient, who needs it.EFFECT: effective prevention and improvement of the condition of the patient, suffering from oral mucositis or stomatitis, without any side effects.9 cl, 5 ex, 1 tbl

eans and methods of predicting response to treatment of hepatitis b // 2640256
FIELD: biotechnology.SUBSTANCE: invention relates to a method of determining whether a patient with hepatitis b (HBV) has an increased probability of a positive outcome of hepatitis B treatment compared to the average probability in a population of patients with hepatitis B. The proposed method includes establishing whether the sample with nucleic acid of specified patient with hepatitis B, associated with positive result of G allele of SNP rs 12356193.EFFECT: invention allows you to determine whether a patient with HBV will respond to HBV therapy prior to therapy, and gives the possibility to avoid unnecessary expenditure and the emergence of side-effects and complications during treatment.9 cl, 24 dwg, 3 tbl, 4 ex

Bis-met-histones // 2640247
FIELD: biotechnology.SUBSTANCE: nucleic acid molecule encodes a polypeptide consisting of two methionine residues as the first and second N-terminal amino acid residues linked through a peptide bond to the mature eukaryotic histone H1. 3. A polypeptide is prepared by culturing a host cell transformed with an expression vector comprising the said nucleic acid molecule. The polypeptide is used as part of a pharmaceutical composition for treatment of cancer, bacterial, viral or fungal infections. Also, the polypeptide is used as part of a composition for diagnosing a patient with respect to the presence of a response to a pharmaceutical composition containing the said polypeptide, or with respect to curability thereof.EFFECT: invention allows to increase the efficiency of recombinant expression and facilitate the determination of the said polypeptide in the presence of endogenous histones while maintaining biological activity of the mature eukaryotic histone.16 cl, 3 dwg, 6 tbl, 7 ex
Composition for topical application, containing glycerin and tannin // 2640020
FIELD: pharmacology.SUBSTANCE: invention relates to a topical formulation for treatment of skin and mucosal infections comprising glycerin in an amount of 30 to 99.99% v/v and plant proanthocyanidins; to a method for maintaining of a glycerin film on a biological surface by preparing the formulation and its application to a biological surface; to a method for skin and mucosal infections treatment, comprising the step of composition application; to a method for production of the claimed composition.EFFECT: formation of a long-term high-osmotic film on damaged surfaces, thereby keeping the lesions clean from all free contaminants.11 cl, 9 dwg, 11 ex
Active biological substance "ingaliptum active plus", local action preparation obtained on its basis // 2639562
FIELD: pharmacology.SUBSTANCE: invention relates to a biologically active substance for inhibition of the growth activity of Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Bacillus subtilis ATCC 6633 and Candida albicans ATCC 653/885 strains. The biologically active substance for inhibition of the growth activity of Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Bacillus subtilis ATCC 6633 and Candida albicans ATCC 653/885 strains contains thymol, eucalyptus oil, peppermint oil, eucalyptus extract, polysorbate 80, benzalkonium chloride at a certain ratio of components. The local action preparation for inhibition of the growth activity of Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Bacillus subtilis ATCC 6633 and Candida albicans ATCC 653/885 strains contains the biologically active substance, glycerin and purified water at a certain ratio of components. The above-described substance and preparation are effective for inhibition of the growth activity of Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Bacillus subtilis ATCC 6633 and Candida albicans ATCC 653/885 strains.EFFECT: increased preparation efficiency.6 cl, 2 tbl, 2 ex

Peptides suppressing respiratory viruse infections, their application and methods for obtaining // 2639559
FIELD: pharmacology.SUBSTANCE: inventions relate to a peptide synthesized chemically or genetically engineered, compositions comprising such a peptide, DNA coding a polypeptide, vector incorporating such a DNA, a host cell for expression of the peptide, a peptide screening Kit, capable of suppressing a respiratory virus infection and a method for screening of a peptide capable of suppressing a respiratory virus infection. The presented peptide contains 5 or more essential amino acids, 2 or more of these essential amino acids are located in the N-terminal or C-terminal region, and the N-terminal region contains a sequence of no more than 10 amino acids from the peptide N-terminal amino acid and the C-terminal region contains a sequence of no more than 10 amino acids from the peptide C-terminal amino acid, while the peptide consists of a sequence of amino acids, at least 90% identical to SEQ ID NO: 10.EFFECT: possibility of application of inventions to block infections of respiratory viruses such as influenza viruses or coronaviruses in the target cells for prevention and treatment of these infections.23 cl, 10 dwg, 3 tbl, 1 ex

Computer-optimized antigens with wide reactivity spectrum for influenza viruses of h5n1 and h1n1 // 2639551
FIELD: biotechnology.SUBSTANCE: recombinant influenza hemagglutinin (HA) polypeptide to elicit an immune response to the H5N1 influenza virus containing the amino acid sequence from residues 2-568 of SEQ ID NO: 1 encoding its nucleic acid containing the proposed polypeptide fusion protein and virus-like particle (VLP) to elicit a response to the H5N1 influenza virus, an expression vector containing the nucleic acid, and an isolated cell containing it, a composition and method for eliciting an immune response to the H5N1 influenza virus, and a method for immunizing a subject are proposed. The proposed group of inventions can be used in medicine for immunization against the H5N1 influenza virus.EFFECT: proposed protein, VLP, and compositions are capable of eliciting an immune response with a wide range of reactivity to the H5N1 influenza virus.19 cl, 8 dwg, 5 ex

Dosing modes for echinocandine class compounds // 2639483
FIELD: medicine.SUBSTANCE: aqueous solution is applied that includes compound 22 having the structural formula or its pharmaceutically acceptable salt, which is administered to the patient in the form of intravenous infusion, intravenous bolus or subcutaneously, or a pharmaceutical composition containing an effective amount of compound 22, while the specified composition is either dried or is an aqueous solution.EFFECT: increased efficiency of fungal infection treatment with reduced dosage and frequency of drug administration due to the improved pharmacokinetic profile of the compound.15 cl, 22 dwg, 14 tbl, 13 ex

Composition for viral hepatitis c therapy // 2639388
FIELD: medicine.SUBSTANCE: invention can be used to treat an infection caused by the hepatitis C virus (HCV). A composition for HCV infection treatment of by the RNAi mechanism consists of complexes of lipopeptides of the OrnGlu (C16H33)2 composition, serving as a carrier, and siRNA molecules represented by 5'-AAAUCUCCAGGCAUUGAGCtt-3' (SEQ ID NO 1). Composition application on a transplantable cell culture of human hepatoma Huh-7, expressing the subgenomic replicon of HCV, causes a significant decrease in viral replicon expression by 20%.EFFECT: high bioavailability with subcutaneous administration of the composition.2 cl, 8 dwg, 4 tbl, 5 ex
Ethyl (3s,4r,5s)-4-acetamido-5-amino-3-(1-ethyl propoxy) cyclohex-1-en-1-carboxylate etoxy succinate as anti-viral drug and method for its production // 2639158
FIELD: pharmacology.SUBSTANCE: invention relates to ethyl (3S,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)cyclohex-1-en-1-carboxylate ethoxy succinate having antiviral activity. The compound of the invention is prepared by ethyl(3S,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)cyclohex-1-en-1-carboxylate treatment with ethoxysuccinic acid in ethyl acetate. .EFFECT: improvement of the method.2 cl, 1 tbl, 2 ex
Tricyclic benzoxaboral compound, method for its production and its application // 2639153
FIELD: pharmacology.SUBSTANCE: invention relates to a new tricyclic benzoxaboral compound represented by chemical formula 1, its isomer or a pharmaceutically acceptable salt thereof. Chemical formula 1 Also, methods of preparation of the said compound and a pharmaceutical composition are provided.EFFECT: new tricyclic benzoxaboral compound has antibiotic activity against gram-negative bacteria, including against gram-negative bacteria with multiple drug resistance.14 cl, 3 tbl, 12 ex
Preparation for infectious inflammatory diseases treatment and/or prevention // 2639129
FIELD: pharmacology.SUBSTANCE: invention relates to an antiseptic preparation in the form of a gel that contains chlorhexidine gluconate-0.01-0.5 g, methyl-4-hydroxybenzoate-0.01-0.1 g, ethyl 4-hydroxybenzoate-0.01-0.1 g, propyl-4-hydroxybenzoate-0.01-0.1 g, propylene glycol 5-70 g, hydroxyethylcellulose – 1.5-5 g and water - up to 100 g.EFFECT: creation of a new drug that is effective against pathogens that cause sexually transmitted diseases and is not toxic and irritating.3 cl, 8 ex, 2 tbl
ethod for obtaining means with antimicrobial activity // 2639119
FIELD: pharmacology.SUBSTANCE: method for obtaining of a means with antimicrobial activity, incudes combination of dried leaves of wild apple with wild apple fruit pulp obtained after mechanical juice squeezing and subsequent drying, crushing, extraction with ethanol, filtering, the residue is extracted with 95% ethanol, infused, filtered and the obtained extractions are combined under certain conditions.EFFECT: means obtained by the above-described method has a pronounced antimicrobial effect.1 tbl
Indasole inhibitors of wnt signal path and their therapeutic applications // 2638932
FIELD: medicine.SUBSTANCE: invention relates to a indasole derivative that has the following formula , or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing it. The invention relates to methods for treatment of disorders characterized by the activation of Wnt-signalling pathways (e.g., cancer, abnormal cell proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), including introduction of a therapeutically effective amount of this compound or pharmaceutically acceptable salt thereof. This compound can also be used in modulation of cellular events, mediated by Wnt-signalling, as well as for treatment of genetic diseases and neurological conditions/disorders/diseases due to mutations or disregulation of the Wnt pathway and/or one or more components of Wnt-signalling.EFFECT: inhibits the Wnt signalling pathway and can be used to treat various diseases and pathologies.28 cl, 8 tbl, 8 ex
Derivatives of 1h-pyrazolo [3,4-d] pyrimidine and method of their production // 2638928
FIELD: chemistry.SUBSTANCE: invention relates to novel derivatives of 1H-pyrazolo [3.4-d] pyrimidine of the general formula I , where: R=CH3, R1=C(O)NH (Ia); R=CH3, R1=C(NH)NH2 (Ib); R=naphthylmethyl, R1=C(O)NH2 (Ic); R=naphthylmethyl, R1=C(NH)NH2 (Ir). Derivatives of 1H-pyrazolo[3,4-d]pyrimidine presented in the formula I, are produced by the interaction of 4,6-dichloro-2-S-(substituted) pyrimidine-5-carbaldehyde dissolved in tetragidrofurane, with the addition of the calculated derived quantities of hydrazine and triethylamine in a molar ratio of 1:1:2, the mixture is mixed on the magnetic agitator for 12 h at room temperature. The resulting precipitate is poured with water and stirred at room temperature for 3 hours. The regenerated precipitate is filtered.EFFECT: production of new compounds that can be used for the synthesis of heterocyclic compounds and in medicine as antimicrobial agents.2 cl, 2 tbl, 5 ex
 
2550854.
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