For tuberculosis (A61P31/06)

A   Human necessities(312083)
A61P31/06                     For tuberculosis(306)
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
New inhibitors of serine-threonine kinases, including for treatment of oncological diseases and tuberculosis // 2633032
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula or n=0-2; A is independently selected and is a 5-7-membered aromatic heterocycle containing 1-2 N atoms and 0-1 S atom; A contains 0-2 R substituents; R is independently selected and represents methyl or ethyl; B is independently selected and represents phenyl, 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; B contains 0-3 R1 substituents; C is independently selected and represents phenyl, -NH2, -NH-C1-3-alkyl, -NH (C1-3-alkyl) C1-3-alkyl, a 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or a 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; C contains 0-3 R1 substituents; R1 is independently selected and represents -C1-6-alkyl, halogen, phenyl, -C5-7-heteroaryl containing 1-2 N atoms and 0-1 S atom, -COOH, -CONH2, -NH2 or -NHR2; R2 is independently selected and represents -C1-6-alkyl, -C (O) -C1-8-alkyl; the linker X is independently selected and is -CH2-, -C(=O)-CH2- or -CH2-O-group; the linker Q is independently selected and represents -NH- or -NH-C(O) -group; the Y linker is independently selected and represents -O-(CH2) m or -C(O)-NH-(CH2)m, where m=1-3; Z is independently selected and represents -CH2- group or an oxygen atom.EFFECT: compounds are prospective for use in the therapy of diseases associated with the activity of serine-threonine kinases.13 cl, 2 tbl, 16 ex
Quaternary ammonium derivatives of 2-aminothiophen-3-carboxylates having anti-tuberculosis activity // 2629369
FIELD: pharmacology.SUBSTANCE: invention relates to the new quaternary ammonium salts of 2-aminothiophene-3-carboxylic acid derivatives having anti-tuberculosis activity of general formula I and formula II where X is absent or is -CH2-, -(CH2)2-, CH3CH-, -N(R4)-; R1 is CN, C(O)OR5, C(O)NHR6; R4 are aliphatic saturated, unbranched or branched C1-C5 hydrocarbon, benzyl; R5 are aliphatic saturated, unbranched or branched C1-C5 hydrocarbon; R6 are H, aliphatic saturated, unbranched or branched C1-C5 hydrocarbons, cyclic hydrocarbons C3-C7.EFFECT: increased efficiency.2 cl, 2 tbl, 12 ex
ethod for pressing the growth of mycobacterium tuberculosis polyresistent stamps in experiment // 2628624
FIELD: biotechnology.SUBSTANCE: in order to suppress the growth of multidrug resistant strains of Mycobacterium tuberculosis, a photodynamic effect is carried out in the experiment. As a photosensitizer, photoditazine at a concentration of 4⋅10-5 Mol/l. The irradiation is carried out with a low-intensity Azor-2K-02 laser with a wavelength of 660 nm, an output power of 25 mW emitting in a constant mode for 40 minutes at a power density of 0.32 mW/cm2 And an energy density of 0.76 J/cm2.EFFECT: method provides simple, reliable and effective inhibition of the growth of mycobacterium tuberculosis culture due to an additional inhibitory effect and enhancement of the bacteriostatic effect of laser irradiation of the cell culture treated with a photosensitizer.1 tbl
Antituberculosis pharmaceutical composition containing thioacetazone // 2627611
FIELD: pharmacology.SUBSTANCE: compositions for tuberculosis treatment include thioacetazone s active ingredient, as well as lactose, starch, talc and stearic acid and/or a salt thereof, at a certain quantitative ratio.EFFECT: invention allows to obtain a composition characterized by high solubility, bioavailability and efficacy.8 tbl, 6 ex
ethod for obtaining of rifampicine polymeric complexes with reduced toxicity and high antituberculosis activity // 2623877
FIELD: pharmacology.SUBSTANCE: invention relates to medicine and is a method for production of rifampicine polymeric complexes with reduced toxicity and high antituberculosis activity by rifampicine complexing with anionic polyelectrolyte in its aqueous solution. Poly-2-acrylamido-2-methylpropanesulphonic acid with a molecular weight of 20,000-40,000 is used as an anionic polyelectrolyte, complexation is performed at a weight ratio of polymer:antibiotic equal to 1.9-4.0.EFFECT: decreased rifampicin toxicity while preserving high level of anti-TB activity.1 tbl, 4 ex
Agent with isoniazid-containing liposomes // 2622755
FIELD: pharmacology.SUBSTANCE: capsules for oral use comprise liposomes prepared by mixing egg lecithin, PEG 2000 and Tween-80 at the ratio of 6:2:1 at a temperature of 40°C, followed by hydration, encapsulated for oral use, wherein liposomes comprise isoniazid as an active agent in the following ratio of liposome components, g per 1 capsule: isoniazid - 0.3; a mixture of phospholipid, PEG 2000 and Tween-80 - 0.22. Number 0 capsules with a diameter of 7.65 mm, length of 21.7 mm, filling volume of 0.68 ml are additionally used.EFFECT: agent has antiphthisic effect, as well as constant-rate release of active agents and pronounced prolonged action, it is convenient for using by patients themselves.3 tbl, 3 ex
Pill with isoniazid and ofloxacin for tuberculosis treatment // 2622754
FIELD: pharmacology.SUBSTANCE: proposed pill comprises isoniazid and ofloxacin as active agents, a mixture of milk sugar, potato starch 1500 and crospovidone Polyplasdone as auxiliary agents for core cladding at the ratio of 2:1:1; 7% aqueous solution of potato starch as a humidifier 1; 3% aqueous solution of povidone (Plasdone C) 2 as a humidifier 2; alcohol solution containing 5 wt % of acetylphthalylcellulose and 2 wt % of Tween-80 as a acido-resistant coating - humidifier 3; a mixture of 64% sugar syrup solution and 1.5% aqueous solution of kollidon 25 at the ratio of 5:1 as a humidifier 4 at a certain ratio of the components.EFFECT: use of the invention ensures preparation of a new domestically produced drug in the form of a pill comprising isoniazid and ofloxacin having antiphthisic effect, with release of active agents within 1-2 hours.2 cl, 2 dwg, 4 ex
ethod of treating patients suffering pulmonary tuberculosis // 2621875
FIELD: medicine.SUBSTANCE: antibacterial therapy is conducted in accordance to standard conditions. From the first day of treatment, also inject Wobenzym daily 1 tablet 30 minutes before meals 2 times a day for 60 days. Additionally, 10 intravenous drip infusions of the drug Reamberin are included in the course of treatment from the first day. Infusions are performed once a day every other day at a dose of 400 ml per infusion.EFFECT: reduction of the periods of resorption of infiltration, closure of cavities of decay, abacillation, reduction in the frequency of formation of adverse hepatotoxic reactions.1 tbl, 2 ex

Synergic anti-tuberculosis pharmaceutical composition containing cycloserine and zinc containing connection // 2620857
FIELD: pharmacology.SUBSTANCE: invention relates to a synergistic pharmaceutical composition with anti-tuberculosis activity, containing cycloserine and a zinc-containing compound as active principle.EFFECT: composition of the invention is characterized by increased anti-tuberculosis activity, pharmacokinetics and reduced toxicity.17 cl, 6 ex, 12 tbl, 2 dwg

Diflunisal co-crystalline form // 2617849
FIELD: pharmacology.SUBSTANCE: diflunisal co-crystalline form with isoniazid is disclosed, wherein the molar ratio of diflunisal to isoniazid is 1:1, wherein the cocrystal has an endothermic spike from 148 to 152°C, according to measurement by differential scanning calorimetry, and spikes at 2θ(°) 5.9, 7.5, 8.5, 11.6, 15.1, 18.5, 26.6, according to measurement by powder X-ray diffraction.EFFECT: diflunisal co-crystalline form is obtained, suitable for use in the pharmaceutical industry as a pharmaceutical preparation component, used to relieve pain accompanied by inflammation, and symptomatic treatment of rheumatoid arthritis and osteoarthritis, with increased level of solubility in water by more than 5 times for diflunisal compared with values in pure form.7 dwg, 2 ex
Chloride 4-[(1e)-1-(6-chloro-4-oxo-4n-chromen-3-yl)-4-methylpent-1-en-3-yl]morpholine-4-yl, method of producing thereof and its antituberculosis effect // 2613633
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to chloride 4-[(1E)-1-(6-chloro-4-oxo-4H-chromen-3-yl)-4-methylpent-1-en-3-yl]morpholine-4-yl of formula I and method of producing thereof.EFFECT: new heterocyclic compound, may be used as a potential antituberculosis drug.3 cl, 5 dwg, 2 tbl, 2 ex
ethod of increasing the efficiency of treatment of patients with tuberculosis // 2611398
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to phthisiology, and can be used to improve the efficiency of treatment of patients with tuberculosis. Method includes the determination of the degree of patient’s medication adherence through his questioning, which is performed at the beginning of the main course of treatment. Stens are determined and after its determination diagnose the factors affecting the level of adherence, and then the prediction of medication adherence is determined: if total score is from 35 points and more, 1–2 stens mark the unsatisfactory medication adherence, if it is 16–34 points, 3–5 stens mark satisfactory medication adherence, if it is 4–15 points, 6–8 stens mark good medication adherence, if it is up to 3 points, 9–10 stens mark medication adherence. In case of unfavorable prognosis at 1–5 stens prescribe cycloferon immunomodulator and methods of psychotherapy, as well as the chemotherapy regimen correction is carried out by changing the method of administration of etiotropic drugs, and at a satisfactory medication adherence etiotropic drugs are administered parenterally, and at unsatisfactory medication adherence etiotropic drugs are administered parenterally and inhalationly.EFFECT: use of invention improves efficiency of treatment of patients with tuberculosis by determining the degree of patient’s medication adherence for further treatment correction.1 cl, 2 ex
ethod for treatment of patients with pulmonary tuberculosis // 2611391
FIELD: medicine, pharmacy.SUBSTANCE: invention refers to medicine, namely to phthisiology, and can be used in complex treatment of patients with pulmonary tuberculosis (PT). Pulmonary tuberculosis patients receive a course of treatment according to standard regimes. Starting from the first day of treatment, the patient receives Wobenzym orally during 60 days of daily dose of 1 tablet 2 times a day 30 minutes before eating. Additionally, the treatment includes oral administration of Tubosan, 1 capsule of 200 mg 1 time a day after meal, once in two days during 60 days. After 60 days from the start of treatment, Wobenzym and Tubosan are canceled, and the course of TB treatment is continued according to standard regimes.EFFECT: increased efficiency of treatment by reducing infiltration resorption periods, decay cavity closure, abacillation and normalization of immune and cytokine status, reduction of frequency of common residual changes.4 tbl, 2 ex

Imidazo[1,2-a]pyridine compounds, synthesis thereof and methods of using same // 2608611
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to novel imidazole derivatives of formula given below or pharmaceutically acceptable salt thereof, where Y denotes CH or N; R1 is: -alkyl containing 1-2 carbon atoms; - substituted alkyl containing 1-3 carbon atoms, which includes 1-3 substitutes, selected from a heteroaryl (selected from pyridine, thiazole furan), phenyl, halogen, wherein said heteroaryl and phenyl are substituted with 1-3 substitutes, selected from halogen, -OQ10, methylsulphonyl group, fluorophenox group and Q15; wherein Q10 is an alkyl containing 1-3 carbon atoms, and Q15 is hydrogen, alkyl containing 1-2 carbon atoms, which can be substituted with three halogen atoms; - cycloalkyl containing 3-6 carbon atoms; - amide (-CONH2) or alkyne containing 2-4 carbon atoms; -halogen; -phenyl; -substituted phenyl, containing 1-2 substitutes, selected from trifluoromethylphenoxy group, -OQ10, halogen, thiomorpholine; wherein Q10 is an alkyl, containing one carbon atom; -benzotriazole; R2 is: -alkyl, containing one carbon atom; -substituted alkyl, containing one carbon atom, containing 1-3 substitutes, selected from halogen and phenyl; -phenyl; R3 is -COW, where W is OR1, NHR1 or NR1R2. Invention also relates to a pharmaceutical composition based on a condensed imidazole derivative and use of said compound.EFFECT: technical result is obtaining novel condensed imidazole derivatives, useful in treatment or prevention of tuberculosis.19 cl, 4 dwg, 5 tbl
Drug of anti-tuberculosis action on the basis of d-cycloserine in the form of a lyophilisate and method of producing a medicinal preparation // 2606839
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and medicine and represents a drug of anti-tuberculosis action in the form of a lyophilisate for oral application weight 2.0±0.20 g, containing D-cycloserine 12.5±1.25 wt%, polymer PLGA 50/50 50±5.0 wt%, polyvinyl alcohol 12.5±1.25 wt% and D-mannitol 25±2.5 wt%, with content of D-cycloserine from 0.225 to 0.275 g, which when diluted with water in amount of 100±10 ml forms a suspension of particles with size of not more than 800 nm, components of not less than 90 %.EFFECT: invention provides high stability under conditions of long-term storage at temperature 5±3 °C for 18 months and accelerated storage at temperature 25±2 °C for 184 days, high bioavailability, including high tissue bioavailability in target organs of the infectious process, and low toxicity, neurotoxicity.6 cl, 3 ex, 5 tbl

Oral solid preparation of compound antituberculosis drug and preparation method thereof // 2605388
FIELD: medicine.SUBSTANCE: oral solid preparation of a compound anti-tubercular drug is disclosed, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride in weight ratio of 150:75:400:275, respectively. Compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not come to contact with each other directly. In the coated tablet with coated core in the inner core contains isoniazid or rifampicin and polymer, which is quickly destroyed and is quickly increased in volume during absorption of water, or rifampicin in the inner core is in the form of enteric solid dispersion. In the coated three-layer tablet the top layer and bottom layer separately and independently comprise a layer of rifampicin, including polymer which is quickly destroyed and is quickly increased in volume during absorption of water, and a layer of isoniazid/pyrazinamide, and a central layer is a layer of ethambutol hydrochloride including an inhibitor, which retains fast disintegration or release of ethambutol hydrochloride, or in the layer containing rifampicin, rifampicin is in form of enteric solid dispersion, where the weight ratio of rifampicin and enteric solid carrier is from 2:1 to 1:3.EFFECT: compound oral solid preparation according to the invention is characterized by high stability, higher bioavailability of rifampicin, that enhances treatment efficacy and reduces a probability of drug resistance.19 cl, 11 dwg, 11 tbl, 11 ex

N-(2-aminopurin-6-yl)glycyl-(s)-glutamic acid, having anti-tuberculosis activity // 2604068
FIELD: chemistry.SUBSTANCE: invention relates to a novel N-(2-aminopurin-6-yl)glycyl-(S)-glutamic acid, having high anti-tuberculosis activity, including with respect to mycobacteria strains with multiple drug resistance. N-(2-aminopurin-6-yl)glycyl-(S)-glutamic acid corresponds to formula .EFFECT: development of new drugs.1 cl, 1 tbl

tb-c vaccine against asthma // 2602771
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and describes the agent for the treatment or prevention of an allergic condition. Agent, which is a liposome formulation comprising: (a) fragments of a Mycobacterium tuberculosis-complex (MTB-C) strain, (b) a liposome-forming agent, (b) 1 to 20 % sucrose. Also a liposomal agent is offered, where z-average particle size is equal to 150 nm or less, and a pharmaceutical composition comprising the specified agent.EFFECT: group of inventions provides the prevention and treatment of asthma in a mammal, attenuates airway hyperresponsiveness, eosinophilia level and lymphocytosis in the airways of sensitized animals, due to content of 1-20 % weight/volume of sucrose and specific particle size (less than 150 nm) in liposomal agent.32 cl, 15 dwg, 10 tbl, 10 ex

Agent exhibiting bacteriostatic activity on multiresistant mycobacterium tuberculosis strains in experiment // 2602450
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to medicine and pharmaceutical industry and represents an agent exhibiting bacteriostatic activity on multiresistant Mycobacterium tuberculosis strains in experiment, representing a water fotoditazin solution in concentration of 4·10-5 mol/l.EFFECT: invention provides wider range of medicinal agents used to inhibit growth of Mycobacterium tuberculosis.1 cl, 1 tbl

ethod for prevention of complications induced by isoniazid // 2597788
FIELD: medicine.SUBSTANCE: invention refers to medicine, namely to therapy, and can be used for prevention of complications induced by isoniazid. For this purpose, along with introduction of isoniazid, amaranth seed oil is used produced by cold pressing of germs and shells of amaranth seeds in the dose of 600 mg 1 time a day 1 hour prior to the meal before noon daily as per the therapeutic course of 3-4 weeks, at extension of the anti-tuberculosis therapy the said is used as continuous assistance with the interval between courses of 1 month.EFFECT: invention ensures reduction of severity of metabolic and morphological hepatic disorders in acute disorders induced by isoniazid, reduction of intensity of pathological changes in the cardiovascular system and the central nervous system.1 cl, 2 dwg, 3 tbl, 3 ex

Use of nanophospholipid composition of rifampicine together with protionamide or its nanophospholipid form in treatment of tuberculosis // 2595881
FIELD: medicine.SUBSTANCE: invention refers to medicine and pharmacology and concerns using of nanophospholipid composition of rifampicine together with protionamide or its nanophospholipid form for treatment of tuberculosis.EFFECT: invention provides reducing of collateral toxic damage.1cl, 1 tbl

Use of ammonium salts of trifluorborane as an antibacterial and anti-mitotic agent // 2595037
FIELD: chemistry.SUBSTANCE: present invention relates to the use of ammonium salts of trifluoroborane of formula I for preparing a drug possessing antibacterial (bactericidal) and antimycotic (antifungal, fungicidal) activity against Salmonella r. B, Candida Albicans, Pseudomonas aeruginosa. Ammonium salts of trifluoroborane correspond the general formula I , where R denotes h-C-8H17; n-(C)10H21, n-C12H25; n-C14H29; n-C16H33, n-C-18H37.EFFECT: compounds are characterised by a broad temperature stability interval up to 250-300 °C in the form of liquid crystals and can be used in medicine, veterinary science, agriculture.1 cl, 1 tbl, 7 ex

Α,ω-bis(amide- and hydrazide methyl sulfinyl- and sulphonyl) alkanes having anti-tuberculosis activity, and α,ω-bis(methoxy carbonyl methyl sulfinyl- or sulphonyl) alkanes for production thereof // 2591256
FIELD: chemistry.SUBSTANCE: invention relates to sulphur-containing dicarboxylic acids of formula (1) wherein: X=NH2, m=1, n=2, 3, 4, 5, 6, 7, 8, 10; X=NH2, m=2, n=1, 2, 3, 4, 5, 6, 7, 8, 10; X=NHNH2, m=1, n=1, 2, 3, 5, 6, 7, 8, 10; X=NHNH2, m=2, n=1, 2, 3, 4, 5, 6, 7, 8, 10. Invention also relates to sulphur-containing dicarboxylic acids of formula (2) wherein: m=1, n=2, 3, 4, 5, 6, 7, 8, 10; m=2, n=3, 4, 5, 6, 7, 8, 10; used for producing compounds of formula (1).EFFECT: compounds of formula (1) have high tuberculostatic activity, including in relation to multi-drug resistant Mycobacteria strains, low toxicity and simplicity of synthesis.3 cl, 2 tbl, 59 ex

Derivatives of 6-methyl-4-phenyl-5-(phenyl or cycloalkyl)-carbamoyl-1,2,3,4-tetrahydropyrimidin-2-one as antituberculous agents // 2590163
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of general formula 1 having anti-tuberculosis activity, and a method for production thereof. In general formula 1 R represents H, halogen, digalogen, R1 represents chlorophenyl, nitrophenyl, dichlorophenyl, cyclohexyl, X is O or S, compounds are selected from: N-(3-chlorophenyl)-4-(3-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, N-(2,3-dichlorophenyl)-4-(3-chlorophenyl) 6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, N-(4-nitrophenyl) -4-(3-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide), N-(4-nitrophenyl)-6-methyl-4-phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, N-(4-nitrophenyl)-4-(2,4-dichlorophenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, N-cyclohexyl-4-(2,4-dichlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide. Method of producing compounds of formula 1 comprises a) mixing substituted acetoacetanilide, substituted aldehyde and urea, in molar ratio 1:1:1.5 in a solvent, preferably absolute ethanol; b) heating reaction mixture obtained at step (a), at temperature within range of 60-100 °C for a period of time in range of 4-8 hours; c) adding p-TSA (p-toluenesulphonic acid) to reaction mixture obtained at step (b), with subsequent boiling with reflux condenser at temperature within range of 60-100 °C for a period of time in range of 4-8 hours; d) cooling reaction mixture obtained at step (c), followed by separation of solid substances by filtration, flushing of alcohol.EFFECT: disclosed compounds exhibit anti-tuberculosis activity towards mycobacteria, both in active phase and at rest, which increases efficiency of reducing rate of tuberculosis and allows to reduce morbidity and mortality from said disease.9 cl, 1 dwg, 3 tbl, 27 exФормула 1 - Formula 1

ethod of treating patients with destructive forms of pulmonary tuberculosis // 2587332
FIELD: medicine.SUBSTANCE: invention can be used in integrated treatment of patients with destructive forms of pulmonary tuberculosis. For this purpose, on background of course of anti-tuberculosis therapy according to standard conditions from first day in therapeutic course includes Thiotriazoline preparation, and patient is orally administered 200 mg of Tubosan 1 time a day after meals. Thiotriazoline is administered as follows: first 15 days intravenously in dose 4.0 ml diluted in 200.0 ml of 0.9 % sodium chloride, from 16th to 60th day orally in a dose of 100 mg 1 time a day after meals. Tubosan and Thiotriazoline preparations are withdrawn, and course of anti-tuberculosis therapy according to standard conditions is continued.EFFECT: method enables to reduce time of resorption infiltration, cavity closure and abacillation, improves parameters of immune and cytokine status, free-radical oxidation with reduction of frequency of adverse reactions on antituberculous preparations.1 cl, 6 tbl, 2 ex

Aromatic butan-2-ol compounds, preparation and use thereof // 2580551
FIELD: medicine.SUBSTANCE: present invention relates to novel aromatic butan-2-ol compounds of formula I, methods for preparation thereof, a pharmaceutical composition and use to obtain a medicament for treating and/or preventing a disease or disorder caused by tubercle bacillus infection. A compound of formula I of the present invention has advantages in the treatment and/or prevention of a disease or disorder caused by tubercle bacillus infection. In the compound of formula I: R1 is hydrogen, fluorine, chlorine, bromine, iodine or methoxy; R2 is hydrogen, fluorine, chlorine, bromine or iodine; R3 is hydrogen, fluorine, chlorine, bromine, iodine or C1-8-alkyl, inserted in the o-, m- or p-position of the phenyl ring; R4 is phenyl, substituted phenyl or naphthyl and R5 is hydroxy or methoxy.EFFECT: prevention of a disease or disorder caused by tubercle bacillus infection.11 cl, 3 tbl, 46 ex

Antiinfective compounds // 2576662
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to heterocyclic compounds of formula Ib and its pharmaceutically acceptable salts, wherein X, Y and Z represent CH; o is equal to 1; n is equal to 0; m is equal to 1 or 2; A represents C=O; W represents NH; in each specific case, R2 is independently specified in a group consisting of C1-C10 alkyl; in each specific case, R3 is independently specified in a group consisting of halogen, C1-C10 alkyl optionally substituted by halogen; OR6, -NO2, heteroaryl representing pyridyl; in each specific case, R6 is independently specified in a group consisting of C1-C10 alkyl and C1-C10 halogenalkyl; R10 represents a fragment specified in a group consisting of wherein m' is equal to 0, 1, 2, 3 or 4; in each specific case, R11 is independently specified in a group consisting of hydrogen and C1-C10 alkyl; in each specific case, R12 is independently specified in a group consisting of hydrogen, C1-C10 alkyl optionally substituted by OR8 group, heterocyclyl representing morpholinyl, or by hydroxyl; C3-C10 cycloalkyl, C1-C10 halogenalkyl, hydroxyl, -OR14, C(O)R14, -C(O)N(R14)2, phenyl optionally substituted by halogen, -N(R8)C(O)R8 group or OR8 group; benzyl optionally substituted by halogen or OR8 group; in each specific case, R14 is independently specified in a group consisting of hydrogen, C1-C8 alkyl; phenyl optionally substituted by halogen, C1-C3 halogenalkyl or OR8 group, benzyl optionally substituted by halogen; in each specific case, R8 is independently specified in a group consisting of hydrogen, C1-C10 alkyl, C1-C3 halogenalkyl, C3-C7 cycloalkyl, phenyl substituted by halogen or OR8 group. The invention also refers to specific compounds, using the above compounds, a pharmaceutical composition based on the compound of formula EFFECT: activity of certain known compounds has been examined, and the new compounds possessing inhibitory activity on mycobacterial growth have been produced.10 cl, 3 dwg, 2 tbl, 3 ex

N-(2-acetamidopurin-6-yl)glycine, which has anti-tuberculosis activity // 2570113
FIELD: chemistry.SUBSTANCE: invention relates to novel N-(2-acetamidopurin-6-yl)glycine of lower given formula , which has anti-tuberculosis activity, including with respect to strains of mycobacteria with multi-drug-resistance. Invention can be applied in medicine and veterinary.EFFECT: increase of compound activity.1 tbl, 1 ex
ethod of specific prevention of tuberculosis // 2562550
FIELD: veterinary medicine.SUBSTANCE: immunisation is carried out to cattle from 10-20 day-old with the specific immunomodulator KIM-M2 subcutaneously at a dose of 20 µg of protein per 1 kg of animal weight. Then young animals are immunised every 6 months, and cows - in 12 months until recovery of the farm (estation). Tuberculosis test of the immunised animals is carried out with allergic skin reaction in 6 months.EFFECT: invention enables to create in the animals of immunity against tuberculosis.8 tbl, 3 ex

Antituberculosis composition, containing oxazole compounds // 2560676
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to field of pharmaceutics and medicine and deals with anti-tumour medication, containing (R)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxy)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazo[2,1-b]oxazole and anti-HIV medication. Anti-HIV medication is selected from the following: (a) nucleic acid-based reverse transcriptase inhibitor, (b) non-nucleic acid based reverse transcriptase inhibitor or (c) protease inhibitor. Invention also discloses set for treating tuberculosis.EFFECT: medication possesses higher activity.5 cl, 2 dwg, 2 tbl

ethod of complex treatment and prevention of recurrences of muscular-non-invasive forms of urinary bladder cancer // 2560314
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to oncology and oncological surgery, and can be used for complex endourethral treatment and prevention of recurrences of muscular non-invasive forms of urinary bladder cancer. For this purpose bilpolar transurethral resection of urinary bladder tumour in physiological solution is performed. After that, on 25-30 day once per week carried out is 1.5-2 month long induction course of intravesical immunotherapy with medicinal composition, which is prepared immediately before introduction into urinary bladder by mechanical mixing of 100-120 mg of BCG Imuron vaccine and 10 g of Tizol gel in 50 g of physiological solution. Time of exposure of medicinal composition in urinary bladder constitutes 30 minutes. 1 month after break in case of absence of tumour recurrence and satisfactory tolerance of treatment first course of supporting intravesical therapy with said medicinal composition is carried out once monthly with 12 month duration. When first course is completed, 1-month break is made. In case of absence of tumour recurrence and satisfactory tolerance of treatment second course of supporting intravesical therapy is carried out once monthly with 12 month duration.EFFECT: method provides increase of recurrence-free period duration and improvement of patients' life quality with reduction of treatment toxicity and reduction of complications of performed drug therapy.2 dwg, 5 tbl, 2 ex
ethod of treating tuberculosis with multiple drug resistance // 2554753
FIELD: medicine.SUBSTANCE: invention refers to a method of treating tuberculosis with multiple drug resistance characterised by prescribing a combination of six anti-tuberculosis preparations in the intensive phase of chemotherapy and five preparations - in the phase of the 20-month therapy continuation, wherein the intensive phase duration makes at least 8 months until obtaining four negative culture results every month in tuberculosis with multiple drug resistance and until obtaining two negative culture results in all other cases of tuberculosis with multiple drug resistance, the phase of the therapy continuation makes 12 months.EFFECT: higher clinical effectiveness.1 tbl, 9 ex
Capsular form of clofazimine // 2553310
FIELD: medicine.SUBSTANCE: invention concerns a simplified capsular form of clofazimine, containing clofazimine, bee wax, soya bean lecithin, butylhydroxy toluene, soya bean oil, gelatine, glycerol, sorbitol, methylparabene, propylparabene, titanium dioxide, brown chocolate and purified water with preserving high efficacy.EFFECT: simplifying the form.4 tbl, 3 ex
ethod of treating pulmonary tuberculosis // 2549485
FIELD: medicine.SUBSTANCE: invention refers to medicine, namely to phthisiology, and can be used in treating pulmonary tuberculosis accompanied by tuberculosis intoxication. To this effect, administering anti-tuberculosis preparations is combined with the additional intravenous drop-by-drop administration of Reamberin, Heptral and antitoxic polyvalent antigangrenous serum (AGS) preceded by the administration of heparin 50 units/kg; Reamberin is administered in an amount of 400 ml on the first and second day for 2 hours; Heptral is introduced in an amount of 400 ml from the first to the fifth day; AGS is administered on the third day in an amount of 30 thousand International Units, on the fourth day in an amount of 60 thousand International Units, in case of a destructive process - in an amount of 60 thousand International Units on the fifth day; AGS is administered in normal saline NaCl 400 ml, and the first 1 ml of the solution is administered for 5 minutes, the rest amount - for 1.5-2 hours.EFFECT: method enables increasing the clinical effectiveness of pulmonary tuberculosis as soon as possible by binding and neutralising microbial exo- and endotoxins by serum antibodies with no side effects and reduced financial expenses.4 tbl, 3 ex
eans, possessing anti-tuberculosis action // 2549477
FIELD: medicine.SUBSTANCE: means represents a dry extract of leaves and flowers of Gratiola officinalis, obtained by milling the leaves and flowers of Gratiola officinalis, extraction with 96% alcohol on a water bath to boiling and boiling, evaporation, dilution of the evaporated residue first with distilled water, then by the addition of chloroform, cooling to room temperature and centrifuging with the following separation of a water fraction and drying it under specified conditions.EFFECT: means is non-toxic, has an expressed anti-tuberculosis action.2 tbl, 2 ex
Combined antituberculous drugs // 2545731
FIELD: medicine.SUBSTANCE: agent is presented in the form of a tablet, contains isoniazid and a substance which reduces its toxicity; as the substance which reduces the isoniazid toxicity, it contains thiotriazolin. The isoniazid/thiotriazolin ratio makes 4:1.EFFECT: combined antituberculous drug ensures reducing toxicity as compared to the known ones and increasing its pharmacological activity.2 cl, 1 ex, 1 tbl

Antituberculous therapeutic agent: composition of imidazo[1,2-b]tetrazine and pyrazinamide // 2545458
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a chemical compound of formula wherein R=benzyl and to an antituberculous therapeutic agent representing a composition of imidazo[1,2-b][1,2,4,5]tetrazine derivative of formula I, wherein R=benzyl, isopropyl or phenyl and the known antituberculous preparation pyrazinamide with the ingredients in mole ratio 1:1.EFFECT: there are prepared new antituberculous therapeutic agents.2 cl, 2 tbl, 6 ex

Nitroimidazooxazine and nitroimidazooxazole analogues and use thereof // 2540860
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to nitroimidazooxazine derivatives of general formula I, where n equals 1, V and W independently denote H or CH3, and one of X and Y is H and the other is one of the formulae and , where formula IIa includes a single ring labelled at position 3 and position 4 and containing R1 as a substitute, and formula IIb includes a first ring labelled at position 3 and position 4 and containing as substitutes both R2 and a terminal ring, labelled at position 4 and containing R1 as a substitute, where the single ring of formula IIa and the first ring and the terminal ring of formula IIb include C, CH, or N at each ring position, where the single ring of formula IIa and the first ring and the terminal ring of formula IIb independently contain no more than two nitrogen atoms; Z in formulae IIa and IIb is CH2 or a direct bond, R1 is independently any one or two of H, F, C1, CF3, OCF3 or OCH2Ph, and R2 is H. The invention also relates to a pharmaceutical composition based on the compound of formula I, a method of preventing and treating a microbial infection based on use of the compound of formula , and specific nitroimidazooxazine derivatives.EFFECT: obtaining novel compounds with useful biological activity.7 cl, 21 dwg, 3 tbl

Preventive or therapeutic polyepitopic anti-tuberculosis vaccine construction providing induction of cellular immune response of cd4+ or cd8+ t-lymphocytes // 2539035
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of genetic engineering, molecular biology and vaccinology. Claimed is polyepitopic anti-tuberculosis vaccine construction for formation of immune response, which provides induction of immune response of CD8+ T-lymphocytes, consisting of universal polyepitopic immunogen, containing CTL-epitopes, selected from immunodominant antigens of M. tuberculosis, fused from N-end with ubiquitin, and having amino acid sequence SEQ ID NO: 1.EFFECT: vaccine construction provides achievement of effective therapeutic T-cell immune response not only due to antigenspecific cytotoxic CD8+ T-lymphocytes but also intensive response of CD4+ T-lymphocytes.1 tbl, 11 dwg

Furilidene furanone derivatives of usnic acid as new antituberculosis agents // 2533707
FIELD: medicine.SUBSTANCE: invention concerns Mycobacterium tuberculosis growth inhibitors representing (+) and (-)-enantiomers of derivatives of usnic acid containing a furilidene furanone fragment, namely (10R,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4a and (10S,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4b EFFECT: inhibitors possess the high antimicrobial activity.2 tbl, 7 ex

Quinoline derivatives, particularly 6,7-substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ols, method for production thereof and use of compounds to treat infectious mycobacterial dieseases, particularly tuberculosis // 2530493
FIELD: chemistry.SUBSTANCE: invention relates to novel derivatives of 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ol of general formula I or their pharmaceutically acceptable salts with acids, where R1 denotes H, R2+R3 denotes -O-(CH2)n-O-, where n=1-2, which forms additional dioxane and 1,3-dioxolane rings. The invention also relates to a method of producing a compound of formula I and to use of the compound of formula I in treating infectious mycobacterial diseases.EFFECT: obtaining novel compounds with useful biological activity.4 cl, 2 tbl, 3 ex
ethod of treating patients with pulmonary tuberculosis with accompanying non-specific bronchites // 2526121
FIELD: medicine.SUBSTANCE: for treatment of patients with pulmonary tuberculosis with accompanying non-specific bronchitis at the background of carrying out standard anti-tuberculosis therapy from the first day of treatment additionally daily for 3 months the preparation Wobenzym is introduced in a dose of 1 tablet 2 times per day, 30 minutes before meal, and inhalation with a solution of the preparation Hixozide in a dose of 350 mg in 10 ml of water for injections is performed 2 times per week, the course constitutes 24 procedures.EFFECT: method makes it possible to increase treatment efficiency by indices of infiltration resorption, closing of the decay cavities and abacillation.1 tbl, 2 ex
ethod of complex therapy of fist time identified pulmonary tuberculosis // 2525580
FIELD: medicine.SUBSTANCE: for complex therapy of the first time identified pulmonary tuberculosis traditional anti-tuberculosis therapy is carried out. After two weeks of anti-tuberculosis chemotherapy, complex physiotherapy is performed. In the morning 40-60 minutes after meal ultrasound inhalation with an inhibitor of proteases contrykal in a dose of 5000 UNITS, diluted in 3-4 ml of an isotonic solution of sodium chloride is carried out. Inhalation is carried out at a temperature of the solution of 35°C for 10 minutes on the apparatus "Vulkan-1". 20 minutes after inhalation magnetic infrared laser therapy (MIL-therapy) is performed from the apparatus "Rikta-04/4" on affected zones of the lungs by contact method of the application of the apparatus emitter. Frequency of the laser impact constitutes 5-50 Hz. Average power of infrared light-diode radiation is 60±30 mW, an impact with constant magnetic field is realised with induction 35±10 mT for 1-5 min. The course of treatment constitutes 30-40 daily procedures as well.EFFECT: enhancement of infiltration resorption, closing decay cavities in the shorter period, arrest of intoxication symptoms by the end of the first month of treatment, reduction of terms of elimination of clinical and laboratory manifestations of tuberculosis.3 cl, 2 ex

Drug preparation for treating tuberculosis // 2523792
FIELD: medicine.SUBSTANCE: drug preparation for treating tuberculosis contains an active substance isoniaside, and a pharmaceutical carrier tiozol gel with the isoniaside concentration of 5.7-54.5 wt % and the tiozol gel concentration of 45.5-94.3 wt %.EFFECT: higher clinical effectiveness in tuberculosis and lower toxicity.2 cl, 2 tbl

Cocrystalline form of fenbufen // 2521572
FIELD: chemistry.SUBSTANCE: claimed is a cocrystalline form of fenbufen with pyrazinamide, where molar ratio of fenbufen with pyrazinamide constitutes 1:1, which has an endothermal peak from 148 to 152°C by the data of measurements by means of differential scanning calorimetry and peaks at 2θ(°) 7.38, 10.43, 11.04, 21.67 by the data of measurement of polycrystal X-ray radiation diffraction.EFFECT: increased rate and level of solubility of the crystalline form of fenbufen and its suitability for application in the pharmaceutical industry.2 ex, 7 dwg
ethod of treating patients with destructive forms of pulmonary tuberculosis // 2521197
FIELD: medicine.SUBSTANCE: with underlying antituberculous therapy from the first day of treatment, a therapeutic course is added with an oral administration of preparations Wobenzym and Thiotriazoline; Wobenzym is administered for 4 months in a dose of 1 tablet once a day 30 minutes before breakfast, while Thiotriazoline is administered for the first 15 days in a dose of 100 mg 2 times a day, from the 16th to 45th day in a dose of 100 mg 1 time a day, on the 46th day, Thiotriazoline is withdrawn.EFFECT: method enables higher clinical effectiveness and reduced rate of an adverse hepatotoxic response to the antituberculous preparations due to improving the immune status and peroxidation values.6 tbl, 2 ex

ethod for preparing high-bioavailability rifabutin composition, pharmaceutical composition and method of treating mycobacteriosis // 2520603
FIELD: medicine.SUBSTANCE: rifabutin is dissolved in a water-miscible solvent which dissolves rifabutin better than water does; a rifabutin solution is prepared; gelatin is dissolved in water to prepare a gelatin solution; the rifabutin solution is slowly added to the gelatin solution while stirring to prepare a semi-product. The semi-product is dried in a spray drier or lyophilised to prepare a product. The prepared product is used as a part of a pharmaceutical composition for treating mycobacteriosis and Helicobacter pylori infection.EFFECT: higher bioavailability of rifabutin.46 cl, 8 tbl, 5 ex, 7 dwg

Selective anti-tuberculosis agents, representing 3-aminosubstituted 6-(3,5-dimethylpyrazol-1-yl)-1,2,4,5-tetrazines // 2519218
FIELD: chemistry.SUBSTANCE: invention represents 3-aminosubstituted 6-(3,5-dimethylpyrazol-1-yl)-1,2,4,5-tetrazines, which applied as anti-tuberculosis medications make it possible to increase activity and specificity of antimicrobacterial action, extend its spectrum (impact on atypical strains of mycobacteria) as well as reduce toxicity in comparison with analogues.EFFECT: toxicity of claimed compounds is 10-20 times lower than toxicity of anti-tuberculosis medications applied in medicine.5 tbl, 16 ex
ethod of treating patients with chronic forms of pulmonary tuberculosis // 2519140
FIELD: medicine.SUBSTANCE: in an intensive phase of the therapeutic course, a conventional anti-tuberculosis therapy is added with the oral preparation Thiotriazoline 100 mg 2 times a day daily for 45 days. Besides, pulmonary administration of the preparation Hixozide 350 mg dissolved in 10 ml of water for injection every second day in the number of 20 procedures is added.EFFECT: infiltrate resolution, cavity closure and abacillation with no hepatotoxic reaction ensured by creating high concentrations of drug preparations directly in the lesion and increased activity of the immune system.2 ex, 3 tbl
 
2551054.
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