Drugs for disorders of the respiratory system (A61P11)

A   Human necessities(312083)
A61P11                 Drugs for disorders of the respiratory system(1221)
A61P11/04 - For throat disorders(67)
A61P11/06 - Antiasthmatics(363)
A61P11/08 - Bronchodilators(124)
A61P11/10 - Expectorants(16)
A61P11/12 - ucolytics(21)
A61P11/14 - Antitussive agents(35)
Composition for prevention or treatment of chronic obstructive pulmonary diseases containing monoacethyldiglycerol compounds as active ingredient // 2642631
FIELD: pharmacology.SUBSTANCE: compounds of this invention reduce the expression level of CXCL-1, TNF-α or MIP-2, and thus do not have the side effects of the currently used therapeutic agents for chronic obstructive pulmonary disease treatment, are non-toxic and have an excellent therapeutic effect, so that they can be useful as a composition for prevention, treatment and reduction of chronic obstructive pulmonary diseaseseverity.EFFECT: prevention of chronic obstructive pulmonary disease containing monoacetyl diacylglycerin as an active ingredient.10 cl, 6 ex, 8 tbl
Pharmaceutical composition // 2642624
FIELD: pharmacology.SUBSTANCE: version 1 of the composition contains maleate indacaterol in an amount of 20-1200 μg in combination with fluticasone furoate in an amount of 0.5-800 μg or ciclesonide in an amount of 20-800 μg, lactose and optionally one or more pharmaceutically acceptable excipients. Version 2 of the composition contains maleate indacaterol in an amount of 20-1200 μg in combination with fluticasone furoate in an amount of 0.5-800 μg and tiotropium in an amount of 2.25-30 μg, lactose and optionally one or more pharmaceutically acceptable excipients. The composition is in a form suitable for administration once a day.EFFECT: composition according to the invention simplifies the mode of drug administration in the treatment of respiratory, inflammatory or obstructive airway diseases.2 cl, 49 ex
Quinine compounds, method for their production and their medical application // 2641285
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt or optical isomer thereof, wherein, in formula I, n is selected from 1 to 7, R1 means C3-C7 hydrocarbyl, which may be unsubstituted or optionally substituted by halogen, alkoxy, alkoxycarbonyl, heterocyclyl or aryl; R2 is aryl or heteroaryl containing one or more heteroatoms selected from N, O or S which may be unsubstituted or optionally substituted by one or more substituents of halogen, phenyl, -OR6, -SR6, -NR6R7, -NHCOR6, -CONR6R7, -CN, -NO2, -COOR6, -CF3 or linear or branched C1-C4 hydrocarbyl, R6 and R7 can denote a hydrogen atom or linear or branched C1-C4 hydrocarbyl; R3 is hydroxyl, halogen, alkoxy or acyloxy. Alkoxy or acyloxy may be unsubstituted or optionally substituted by halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl; R4 and R5 may or may not be present, and, independently, can mean, without limitation, a substituent such as halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl when these radicals are present. Y is linear or branched C1-C7 alkyl or - (CH2-O-CH2)m-, which may be optionally substituted by halogen, hydroxyl, alkoxy, alkoxyalkyl, unsaturated hydrocarbyl, cyclic hydrocarbyl or heterocyclyl. M is 1-3; X- means an acid residue or hydroxyl, the said compounds having a selective antagonistic effect on the M1 and M3 receptors subtypes, but insignificantly affect the M2 receptor subtype.EFFECT: compound application efficiency increase.24 cl, 5 tbl, 33 ex

Cations of monovalent metals of dry powders for inhalations // 2640921
FIELD: pharmacology.SUBSTANCE: dry powders for treatment of respiratory diseases, consisting of inhaled dry particles, including salts of monovalent metals in quantities of at least 3% of the weight of dry particles and a pharmaceutically active substance, which represents an antibiotic, LABA, LAMA, a corticosteroid or a combination thereof. At that, dry particles in the dry powders are characterized by a volume geometric mean diameter of 5 mcm or less, tundish density between 0.45 g/cm3 and 1.2 g/cm3 and ratio of the volumetric mean geometric diameter measured at a dispersion pressure of 1 bar divided by the volumetric mean geometric diameter measured at a dispersion pressure of 4 bar is less than 1.5. Also, dry powders application for the manufacture of drugs for treatment and prevention of respiratory diseases and their exacerbations are disclosed.EFFECT: due to high dispersibility of dry particles, the group of inventions allows treatment and prevention of respiratory diseases through dry powders inhalation into the lungs of the patient, using only the energy of inhalation, without application of carrier particles or active inhalers.22 cl, 20 dwg, 28 tbl, 17 ex
odulators of atp-binding cartridge transporters // 2640420
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula II , where R is H, OH, OCH3, or two R taken together form -OCH2O- or -OCF2O-; R1 is H or up to two C1-C6alkyls; R2 is H or halogen; and R3 is H or C1-C6 alkyl; R3 is H or C1-C6 alkyl; Y is O or NR4; and R4 is H or C1-C6 alkyl, and their pharmaceutical compositions useful as modulators of ATP-binding cassette ("ABC") transporters, or fragments thereof, including a cystic fibrosis transmembrane conduction regulator ("CFTR"). This invention also relates to methods for treatment of diseases mediated by ABC transporters using the compounds of the invention.EFFECT: increased efficiency of treatment.19 cl, 2 tbl, 1 ex
New compounds // 2640200
FIELD: pharmacology.SUBSTANCE: invention relates to a new compound of the formula (I) or a pharmaceutically acceptable salt thereof having interferon α (IFN-α) and tumour necrosis factor α (TNF-α) inducer properties. The compounds may be useful as vaccine adjuvants. In the formula (I) R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl; m is an integer having a value of 1 to 4.EFFECT: compounds can be used for treatment of allergic diseases and inflammatory conditions, for example, allergic rhinitis and asthma, infectious diseases and cancer.15 cl, 7 ex
Liquid marker for determination of respiratory epithelial clearance speed of nasal mucosa and maxillary sinus // 2640174
FIELD: medicine.SUBSTANCE: liquid marker for determination respiratory epithelial clearance speed of the nasal mucosa and maxillary sinus contains methylene blue, anesthesin, saccharin, sodium laurisulfate and distilled water. The ingredients are used in the declared amounts.EFFECT: application of the invention allows to determine the speed of mucus transport over the surface of the mucosa and gives a characterization of the human respiratory epithelial clearance system as a whole.1 ex

Transmucosal introducting system of pharmaceutical drug // 2639369
FIELD: pharmacology.SUBSTANCE: transmucosal introducing system of the pharmaceutical active agent is described, comprising a suspension containing 30-60 wt % of the active agent selected from the group consisting of idebenone, decilubihinone and ubiquinone, and 40-70 wt % of polyalcohol and/or a cellulose derivative as a carrier, wherein the system is a mucoadhesive film dissolved in the mouth.EFFECT: idebenone concentration in blood after introduction via the tunica mucosa of mouth is significantly higher compared to the oral introduction.15 cl, 1 dwg, 4 tbl, 2 ex
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
ethod for treatment of olfactory dysfunction in patients with acute rhinosinusitis // 2638688
FIELD: medicine.SUBSTANCE: method includes application of local decongestants, irrigation, anti-inflammatory and mucolytic therapy. After acute manifestations of the disease subside, multichannel electrical stimulation is performed on the areas of the chewing muscles, nose wings muscles, the circular muscle of the mouth and the trapezium from both sides. Electrical stimulation is carried out by bipolar-pulse current with a trapezoidal envelope by a premise and a pause of 2 s, with a frequency of 20-120 MHz, current strength to low vibration of muscles under the electrodes. Exposure duration is 10-15 minutes. After this, a leech is placed on the lateral wall of the nose vestibule on one side for 10-12 minutes. The course of physiotherapeutic treatment is 4-5 combined weekly procedures.EFFECT: increased effectiveness of olfactory dysfunction treatment in patients with acute rhinosinusitis due to a multifactorial sequential action on all segments of the olfactory analyzer and the autonomic nervous system.1 ex
Enzymes inhibition // 2638537
FIELD: pharmacology.SUBSTANCE: invention relates to the compound of the formula or its pharmaceutically acceptable salt. In the formula (I) R1 represents -CN; R2 is selected from (C1-C4)haloalkyl, (C1-C4)haloalkoxy; W represents the (i) 5-membered heteroaryl ring, where two or three ring-atoms represent the hetero-atom N, optionally substituted by one group, which is selected from the (C1-C4) alkyl, the group -NHR18, and from the group -COOR28; or (iii) phenyl group; R3 represents the group -CH2-R23; R5 represents the hydrogen; R6 represents the hydrogen; A1 represents the group -CR7=; A2 represents the group =CR8- or the group =N-; A3--A4 represents the group, which is selected from the group -CR4=N-, the group -CR4=CR9- and the group NR17-CO-; R4 represents the group, which is selected from the hydrogen, the (C1-C4) alkyl, -NR10R11, -NHCOR12, -NHCOO-R13, -NHCONR27-R14, the (C1-C4)alkoxy, -NH(CH2)n-SO2(C1-C4)alkyl, -(NH)q(CH2)n-(C6H4)-SO2(C1-C4)alkyl, -NHSO2(C1-C4) alkyl and -(NH)r(CH2)nCONR15R16; the other chemical groups value is indicated in the invention formula. The invention also relates to the pharmaceutical composition and to the method of the disease or state treatment, where HNE is implicated.EFFECT: there are new compounds of the formula that offer the inhibitors' properties of the human neutrophil elastase.14 cl, 97 ex
Derivatives of 1-phenyl-2-pyridinyl-alkyl alcohols as phosphodiesterase inhibitors // 2637945
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula (I) , where R1 and R2 are different or identical and are independently selected from the group consisting of: - H; -(C1-C6)haloalkyl; -(C1-C6)alkyl optionally substituted by one or more substituents selected from (C3-C7)cycloalkyl; and -(C3-C7)cycloalkyl; A is a monocyclic heteroaryl ring system selected from the group consisting of radicals , , , and , n is 0, 1 or 2; R3 is a possible substituent, which in each case is selected from the group consisting of: -(C1-C6)alkyl, optionally substituted by (C3-C7)cycloalkyl; -OR4, (the meaning of the remaining radicals is given in claim 1), its corresponding N-oxide over the pyridine ring and pharmaceutically acceptable salts or solvates thereof. The compounds obtained are inhibitors of the phosphodiesterase 4 (PDE4) enzyme.EFFECT: increased efficiency.14 cl, 8 tbl, 19 ex
ethod for indirect endolymphatic therapy in case of bronchopneumonia in dogs // 2637645
FIELD: veterinary medicine.SUBSTANCE: invention concerns a method for treatment of dogs with bronchopneumonia characterized by appointment freshly prepared drug mixture in conjunction with conventional therapy by a complex of lymph-stimulating injections into the thickness of interspinous ligament of spine at the T10-T12 level; the mixture contains 32 U of Lydazum, 2 ml (6 mg) of Polyoxidonium®-vet, 4 ml of 5% novocaine solution and 4 ml of 40% glucose solution, in a dose of 1 ml per 1 kg of animal weight 5 times with an interval of 24 hours.EFFECT: improved effectiveness of dogs therapy in case of bronchopneumonia by accelerating the seizure of inflammatory edema of respiratory organs, improving tissue oxygenation and accelerating the excretion of toxic products of inflammation by improving lymphovenous relationship in the respiratory region and stimulation of contractile and deposition ability of the ymphatic channel, increased overall immunological reactivity due to polyoxidonium introduction into the therapeutic scheme, shortened treatment.1 ex, 1 tbl
eans for nasal cavity, nasopharynx and oral cavity rinsing // 2637438
FIELD: pharmacology.SUBSTANCE: invention is a means for nasal cavity, nasopharynx and oral cavity rinsing on the basis of natural raw materials, including sodium (Na+), potassium (K+), calcium (Ca2+), magnesium (Mg2), chlorine (Cl-) and bromine (Br-) ions, characterized by containing an aqueous solution of a dry concentrate of salt lake brine with concentration ranging from 0.5 to 10%, with pH ranging from 7.2 to 8.3, osmolarity of 276-278 mOsm/l, with a certain ionic composition in terms of mg/ml as the natural raw material.EFFECT: improved overall health of children and adults and provision of an opportunity to reduce the incidence of influenza during the epidemic.2 cl, 10 ex

Composition for asthma prevention or treatment containing monoacethyldiacyl glycerine compound as active ingredient // 2636615
FIELD: pharmacology.SUBSTANCE: monoacetyl diacylglycerin according to the invention is a natural substance isolated from deer antlers. The monoacetyl diacylglycerols of the invention inhibit the expression of interleukin-4 (IL-4) in mouse T-cell lymphoma cells (EL-4), reduce airway hyperreactivity in experimental induced asthma in animals, and inhibit inflammatory cells penetration into the bronchial tree. In addition, the compounds of the invention reduce the immunoglobulin E (IgE) content in the blood serum and in the fluid obtained from bronchoalveolar lavage; have a pronounced effect of suppressing the expression of cytokines produced by Th2 cells (IL-4, IL-5 and IL-13) in the lungs, and have no side effects, are not toxic, and have an effective therapeutic effect.EFFECT: asthma prevention or treatment.9 cl, 7 dwg, 7 tbl, 8 ex
ethod for extension of drug action during intralacunar introduction into tonsils // 2636611
FIELD: medicine.SUBSTANCE: invention is intended for palatine tonsils sanation during local treatment of chronic tonsillitis in persons with contradictions to administration of drugs to the palatine tonsil by phonophoresis. In the local treatment of chronic tonsillitis, a glycerol-containing drug is injected into the open mouths of lacunae treated with physiological solution, after closing of the lacunae mouths, an aseptic adhesive gum balm is applied to them. As a glycerol-containing drug, Candide solution is used. Also, a mixture of levomycetin, glycerin and physiological sodium chloride solution is used for preparation of which 4.0 ml of eyedrops "Levomycetin 0.25%", 0.2 ml of glycerol for external and topical administration and 0.8 ml of 0.9% physiological solution of sodium chloride are mixed, or these substances are mixed in other amounts, multiple thereof.EFFECT: long drug depot in the palatine tonsils lacunae, which ensures a prolonged drug contact with the epithelial surface of the tonsil mucosa in the lacunae.3 cl, 2 ex

Carboxylic acids compounds // 2636146
FIELD: pharmacology.SUBSTANCE: compounds may find use in the treatment of a disease mediated by TLR7. This disease can be a cancer selected from bladder cancer, head and neck cancers, prostate cancer, breast cancer, lung cancer, uterine cancer, pancreatic cancer, liver cancer, kidney cancer, ovarian cancer, colon cancer, stomach cancer, skin cancer, brain tumour, myeloma and lymphoproliferative tumours, such a disease or condition can also be represented by asthma, COPD (chronic obstructive pulmonary disease), allergic rhinitis, allergic conjunctivitis, allergic dermatitis, hepatitis B, hepatitis C, HIV, HPV (human papillomavirus), bacterial infection, or dermatosis. In the formula ,n is equal to 0, 1 or 2; m is 1 or 2; p is 1, 2 or 3, provided that when X is oxygen, p is 2 or 3, and when X is a single bond, p is 1; X is oxygen or a single bond; R1 is chosen from C1-4 alkyl group, C1-3alkyl-(CH2)group, in which C1-3 alkyl functional group is substituted by 1, 2 or 3 fluorine atoms, and C1-4 an alkylcarbonyl group; R2 is hydrogen; or R1 and R2 together with the nitrogen and carbon atoms to which they are attached form a saturated or unsaturated 5-membered heterocyclic ring optionally containing an additional heteroatom selected from N; R3 is selected from hydrogen, hydroxymethyl and 2-hydroxyethyl. The invention also relates to a method for preparation of a compound of formula (I) and to an intermediate of formula wherein n, p, X, R1, R2 have the above values, Y is a hydroxy or substituted group selected from mesitylenesulfonyloxy, or tri(isopropyl)phenylsulfonyloxy; and PG1 is a carboxylic acid protecting group selected from C1-4 alkyl; or a salt thereof.EFFECT: compound application efficiency increase.37 cl, 13 dwg, 7 tbl, 30 ex

Alpha-1 proteinase inhibitor for delay of beginning or progress of pulmonary exacerbations // 2635482
FIELD: medicine.SUBSTANCE: methods are proposed comprising administration of an effective amount of an alpha1 proteinase inhibitor purified by chromatography (A1PI-HC) to the subject by daily inhalation for a long-term period of time (from 21 days to 10 years). For one version of the method, A1PI-HC is aerosolized and administered using an inhaler in an effective amount of A1PI-HC from about 25 to about 750 mg per day, or from about 0.5 to about 15 mg/kg/day. The patient's age should be at least 12 years. Pulmonary disorder or disease is fibro-cystic degeneration, chronic obstructive pulmonary disease (COPD), deficiency of alpha1 proteinase (A1PI deficiency), emphysema, asthma, mycobacterial infection, pneumonia, bronchiectasis or chronic bronchitis. A version of the method including preliminary identification of subjects with an increased risk of pulmonary diseases exacerbations acceptable for A1PI maintenance therapy is also proposed. The method includes evaluating one or more subject criteria, such as (a) age; (b) history of exacerbations; (c) lungs function (FEV1); (d) chronic productive cough (with phlegm); (e) infectious load by the upper and lower respiratory tract pathogen; (f) inflammation markers of the respiratory tract of exhaled gas; (g) response to exogenous provocation for airways hyperreactivity research; (h) number and classes of concomitant medications; (i) the profile of genetic risk for respiratory disease; (j) environmental risk factors, such as smoking history, allergies, occupational risk factors and/or air pollution effects. It is then determined whether or not the subject is a candidate for A1PI maintenance therapy based on the above criteria, and an effective amount of A1PI-HC is administered to the subject by daily inhalation for a long-term period from 21 days to 10 years. For another version of the method, the above-mentioned inhaled administration of A1PI-HC is performed using an aerosol generated by the inhaler one or more times per day. The cumulative effective dose of A1PI-HC is from about 25 to about 750 mg once a day.EFFECT: group of inventions provides effective prevention and treatment of pulmonary diseases and their exacerbations associated with alpha1-proteinase deficiency due to drug administration directly into the lower parts of the respiratory tract at low therapeutic doses.12 cl, 3 tbl, 3 dwg, 4 ex
Filler for capsular inhaler // 2634258
FIELD: pharmacology.SUBSTANCE: filler contains timodepressin in the form of fine particles of respirable size in the amount of 8.5-11.5 wt % and an inert carrier - inhalation lactose - the rest.EFFECT: expanded arsenal of drugs for inhalation in the treatment of autoimmune diseases, ensuring drug delivery to the blood in unchanged form.3 dwg, 3 ex
Heterocyclic amines and their application // 2632900
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (III) or a pharmaceutically acceptable salt thereof, wherein W is S; Y is N; X is N; R1 is selected from (a) C1-C6 alkyl optionally substituted with amino, methylamino, dimethylamino, C1-C6 alkoxy or isoindolyl; (B) -NR8R7, -CH2NR7R8, where R7 and R8 are joined to form optionally substituted C3-C7 non-aromatic ring which is pyrrolidine, morpholine, piperazine, piperidine, 1,4-diazepane, azepane, azetidine, 2-azabicyclo[2.2.1]heptane or 2,5-diazabicyclo[2.2.1]heptane and optionally substituted by one or more C1-C6alkyl, C1-C6alkoxy, methoxyethyl, 1-methoxypropane, isopropyloxymethyl, isopropyloxyethyl, -C(O(CH2)-methyl, -C(O)(CH2)-O-isopropyl, C1-C6haloalkyl, -S(O)2-methyl, -S(O)2-isopropyl, oxo, -C(O)(C1-C2)alkyl-N(methyl)2, -C(O)(C2)alkyl-(pyrrolidine), t-butyl-C(O)- or phenyl; or (c) -O-(tetrahydro-2H-pyran); each of R2, R3 and R5 are hydrogen; R4 is selected from C3-C6cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and optionally substituted heteroaryl selected from pyridine, pyrazole, pyridazine, pyrimidine. The said heteroaryl is optionally substituted with 1 to 2 substituents selected from C1-C6 alkyl and CN. The invention also relates to specific compounds as defined in the claims. The compounds of the invention are intended for the manufacture of a pharmaceutical composition having an inhibitory activity against an interleukin 1 receptor associated kinase 1 (IRAK-1) and an interleukin 1 receptor associated kinase 4 (IRAK-4). The compounds of the invention are also useful in a method for treatment of a disorder sensitive to inhibition of IRAK-1-mediated signalling.EFFECT: heterocyclic amines having inhibitory activity against an interleukin 1 receptor associated kinase 1 and interleukin 1 receptor associated kinase 4.24 cl, 4 tbl, 431 ex
Substituted derivatives of 3-heteroaroylaminopropionic acid and their application as drugs // 2632897
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I in any of its stereoisomeric forms or a physiologically acceptable salt thereof, wherein A is selected from the group consisting of C(R1) and N; D is selected from the group consisting of C(R2) and N; E is selected from the group consisting of C(R3) and N; L is selected from the group consisting of C(R4); where at least one and not more than two of A, D, E or L is N; G is selected from the group consisting of R71-O-C(O)-;R1 is selected from the group consisting of hydrogen, halogen; R2 is selected from the group consisting of hydrogen, halogen, (C1-C7)-alkyl, Het2 and Ar-CsH2s-, where s is 0; R3 is selected from the group consisting of hydrogen, Het2, R11-O-; R4 and R10 are selected from the group consisting of hydrogen, halogen; provided that one of the R2, R3 is a cyclic substituent; R11 is selected from the group consisting of hydrogen, R14; R12 and R13 are hydrogen; R14 is (C1-C10)-alkyl optionally substituted by one substituent, which is an oxo group; R30 is selected from the group consisting of R31, R32-CuH2u-, where u is 0; R31 is (C1-C10)-alkyl; R32 is phenyl, wherein phenyl is optionally substituted by one or more identical or different substituents selected from the group consisting of halogen, (C1-C6)-alkyl, (C1-C6)-alkyl-O-, CF3-; R40, R50, R60 and R71 are hydrogen; Ar, independently of other Ar groups, is selected from the group consisting of phenyl and aromatic 5-membered or 6-membered monocyclic heterocycle which includes one, two or three identical or different ring heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and is bonded through the carbon atom of the ring, wherein phenyl and heterocycle are optionally substituted by one or more identical or different substituents selected from the group consisting of halogen, (C1-C6)-alkyl, HO-(C1-C6)-alkyl, Het4, (C1-C6)-alkyl-O-, -CF3, -CO-(C1-C6)-alkyl, -CO-NR12R13 and NC-; and wherein phenyl can be substituted with -CH=CH-CH=CH-, -O-CH2-O-, -O-CH2-CH2-O-, -O-CF2-O- or -N((C1-C3)-alkyl) -CH=CH-; Het2 is a saturated 5-membered - 6-membered monocyclic heterocycle that includes a nitrogen atom in the ring through which Het2 is attached and optionally one other ring heteroatom selected from the group consisting of nitrogen and oxygen; Het4, regardless of other Het4 groups, is a saturated or unsaturated 4-membered to 5-membered monocyclic heterocycle that includes one to three ring heteroatoms selected from the group consisting of nitrogen and oxygen which is optionally substituted by one or more identical or different substituents selected from the group consisting of (C1-C4)-alkyl, HO-, (C1-C4)-alkyl-O-. Compounds of formula are obtained by the reaction of a compound of formula II with a compound of formula III, where the A, D, E, L, G, R10, R30, R40, R50 and R60 groups such as defined above for compounds of formula I, and additional functional groups may be present in protected form or in the form of a precursor group, and group J in the compound of formula II is HO-, (C1-C4)alkyl-O- or halogen.EFFECT: substituted derivatives of 3-heteroaroylaminopropionic acid for application as a pharmaceutical agent for catheptase protease A inhibition.10 cl, 1 tbl, 620 ex
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 ex
ethod for prevention of complications in postoperative period in case of nasal septum surgical treatment in children // 2632117
FIELD: medicine.SUBSTANCE: for prevention of complications in the postoperative period in case of surgical treatment of nasal septum deformities in children, the cavity is washed with an octenicept solution diluted with distilled water in a volume ratio of 1:7. After this, endonasal ionophoresis is carried out using fermenkol. Then, tamponade of the reconstructed nasal cavity is performed by turundas impregnated with fermenkol-gel.EFFECT: invention can reduce inflammation, prevent adhesions and scars formation in the nasal cavity, accelerate mucous membrane epithelialization.5 cl, 3 ex

Composition // 2631482
FIELD: pharmacology.SUBSTANCE: compound and its pharmaceutically acceptable salts are inducers of human interferon. Some discrete and single doses of the compound (I) may be particularly useful for treatment of various disorders, for example, allergic rhinitis and allergic asthma.EFFECT: invention provides treatment at a stated dose of 10 to 20 ng, it is possible to avoid the unpleasant side effects.5 cl, 4 dwg
[1,2,4] triazolopiridines and their application as inhibitors of phosphodiesterase // 2630699
FIELD: chemistry.SUBSTANCE: invention relates to a compound of general formula (I) in which R is a branched butyl. The invention also relates to a pharmaceutical composition having a phosphodiesterase inhibitory activity, to the use of a compound for the preparation of a pharmaceutical composition, and to a method of treating or reducing the intensity of a disease, disorder or condition susceptible to a PDE4 inhibitory activity.EFFECT: new compound of general formula I, having a phosphodiesterase inhibitory activity, was obtained.10 cl, 4 ex

Pharmaceutical composition // 2630617
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for treatment of cyclooxygenase-2 mediated diseases is described. The said composition includes, (2S)-7-tret-butyl-6-chloro-2- (trifluoromethyl)-2H-chromene-3-carboxylic acid as the active substance and a filler selected from tromethamine or meglumine. The filler is used in an amount of 0.5 wt % to 70 wt %. Two versions of the method for preparation of this composition and its application are also described.EFFECT: increased dissolution rate and oral bioavailability of the said composition, including the free form of the said compound.9 cl, 5 dwg, 16 tbl, 6 ex
Combination of traditional chinese medicine for immune function regulation and method for its production // 2630056
FIELD: pharmacology.SUBSTANCE: composition of traditional Chinese medicine for immunity regulation, which contains the following raw materials in parts by weight: 1-100 parts of Radix Panacis Quinquefolii, 1-100 parts of Ganoderma, 1-60 parts of Cordyceps sinensis fermented powder, 1-60 parts of Flos Rosae Rugosae and 1-60 parts of Rhizoma Anemarrhenae or one or more of their extracts. A composition of traditional Chinese medicine for immunity regulation. containing the following raw materials in parts by weight: (i) 1-100 parts of any of Radix Et Rhizoma Ginseng, Radix Codonopsis, Radix Pseudostellariae or Radix Astragali, or any of Radix Et Rhizoma Ginseng extract, Extract of Radix Codonopsis, extract of Radix Pseudostellariae or extract of Radix Astragali; (ii) 1-100 parts of Gandorema; (iii) 1-60 parts of Cordyceps or Cordyceps extract; (iv) 1-60 parts of Flos Rosae Rugosae and (v) 1-60 parts of Rhizoma Anemarrhenae. Method for obtaining of a composition of traditional Chinese medicine. Use of the composition in the manufacture of a medicament for allergic diseases prevention and treatment. Allergic diseases include allergic rhinitis, allergic asthma, atopic dermatitis and/or urticaria. Composition application in the manufacture of a medicament for viral diseases prevention and treatment. Viral diseases include hepatitis B and/or AIDS. Composition application for manufacture of a medicament that is effective in increasing of the leukocytes number. Composition application for manufacture of a medicament for radiation injury prevention and treatment. Composition application for manufacture of a medicament to reduce toxic and/or side effects resulting from radiation therapy and chemotherapy. Composition application for manufacture of a medicament for male sexual function improvement. Composition application for manufacture of a medicament for human body immunity enhancement. Composition application for production of a dietary food product or a medicament to alleviate physical fatigue.EFFECT: compositions described above are effective for immunity regulation.18 cl, 19 ex, 13 tbl

Dry powder compositions represented as particles which contain two or more active ingredients for treatment of obstructive or inflammatory diseases of respiratory ways // 2629333
FIELD: pharmacology.SUBSTANCE: dry powder inhalation compositions containing spray-dried particles and their use for treatment of obstructive or inflammatory respiratory disease are described. Each particle has a core of the first active ingredient in a substantially crystalline form that is coated by a layer of the second active ingredient in a substantially amorphous form that is dispersed in a pharmaceutically acceptable hydrophobic excipient. The hydrophobic excipient is a phospholipid in an amount of 40 to 99 wt % of the composition. A method for preparation of such compositions and a delivery system comprising an inhaler and a dry powder composition are also described.EFFECT: invention solves the problem of co-formulating two or more pharmaceutically active agents in a single powder dosage form that is suitable for inhalation, with improved aerosol characteristics.15 cl, 3 dwg, 9 tbl, 7 ex

Aminomethyl quinolones useful ifor treatment of jnk-mediated disorder // 2629111
FIELD: chemistry.SUBSTANCE: invention relates to new aminomethyl quinolone derivative of formula (I) or its pharmaceutically acceptable salt, where R is -C(=O)A, -C(=O)OA, -C(=O)NHA, -C(=N-C≡N)A, -C(=N-C≡N)NHA or A; A is C1-6-alkyl, phenyl, lower cycloalkyl, adamantyl, heterocycloalkyl selected from benzodioxin, pyrrolidine, piperidine, morpholine or piperazine, heteroaryl selected from pyridine, pyrazole, thiazole, triazole or pyrimidine or bicyclic heteroaryl selected from quinoline, quinazoline, indole, benzothiazole, benzoimidazole or imidazopyridine optionally substituted with one or two A1; each A1 independently represents A2 or A3; each A2 is independently halo or oxo; each A3 is independently C1-6-alkyl, C1-6-alkoxy, phenyl, benzyl, heterocycloalkyl selected from morpholine, piperidine, diazepane, pyrrolidine, azepane or piperazine, bicyclic heterocycloalkyl selected from benzodioxole or diazobicycloheptane, heteroaryl selected from oxazole, triazole, pyrazole, imidazole, thiadiazole, oxadiazole, thiazole or tetrazole, amino, C1-6-alkylamino, C1-6-dialkylamino, amido, C1-6-alkyl ester group, sulfonyl, sulfonamido, -C(=O) or -C(═O)O, optionally substituted by one, two or three groups, selected from halo, hydroxy, C1-6-alkylamino, C1-6-alkyloxy, C1-6-alkyl, C1-6-alkoxy, phenyl, hydroxycycloalkyl wherein cycloalkyl is adamantyl, amino, C1-6-alkylamino, C1-6-dialkylamino, t-butyl complex of carbamic acid ester, (C1-6-alkyl) sulfonyl-piperidinyl or hydroxy- (C1-6-alkyl); R' is H or methyl; X is CX'; X' is H or halo; X1 is H, 2-oxazolyl, dimethylamido or C1-6-alkyl ester group; Y is CH or N; and Y1 is H, halo, C1-6- alkoxy or halo (C1-6alkyl). The invention also relates to particular aminomethyl quinolone derivatives and to the use of said aminomethyl quinolone derivatives.EFFECT: obtained new aminomethyl quinolone derivatives, useful in the treatment of JNK-mediated disorder.15 cl, 2 tbl, 211 ex

Crystalline micro particles of beta-agonist, coated with fatty acid // 2629085
FIELD: chemistry.SUBSTANCE: crystalline microparticles consisting of formoterol or its pharmaceutically acceptable salts and myristic acid in amount of 1.0 to 2.0% by weight are described. Myristic acid forms continuous film on surface of microparticles. Crystalline microparticles are used in production of pharmaceutical aerosol compositions in the form of suspension in liquefied propellant gas or in the form of powder compositions. Method of producing microparticles and metered-dose inhaler under pressure filled with aerosol composition has been also described. Crystalline microparticles are used for prevention and/or treatment of respiratory disease, such as asthma or chronic obstructive pulmonary disease.EFFECT: crystalline microparticles of the invention are characterized by improved stability and composition of such particles with improved aerosol characteristics.9 cl, 1 dwg, 4 tbl, 6 ex
Pyperidinyl naphthyluxic acids // 2628083
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I): , as well as to pharmaceutically acceptable salts, pharmaceutical compositions and application thereof.EFFECT: new compounds that are CRTH2 receptor antagonists have been obtained that can be useful for respiratory diseases treatment or prevention.20 cl, 2 tbl, 37 ex
Hinuclidine ethers of 1-azaheterocylic acetic acid as antimuscarine means, method for their production and their drug compositions // 2628082
FIELD: pharmacology.SUBSTANCE: invention relates to formula compounds, where A can be a single bond, a double bond, O, S, NR3, C(R3)R4, CO, C(O)N(R3), N(R3)C(O) and C(R3)-(CH2)-C(R4); m is an integer from 1 to 4; N is 0 or an integer from 1 to 4; R1 is selected from the group consisting of phenyl and 5-member heteroaryl containing one S heteroatom optionally substituted by one or more substituents selected from the group consisting of halogen atoms, (C1-C6)alkyl and (C1-C6)alkoxy; X is a physiologically acceptable anion; R2 is a group of the formula (Y), where p is 0 or an integer from 1 to 4; Q is 0 or an integer from 1 to 4; P is absent or selected from the group consisting of CO, N(R3)C(O) and C(O)N(R3); W is selected from the group consisting of H, (C1-C10)alkoxyl, phenyl, heteroaryl optionally substituted with one or more substituents selected from the group consisting of halogen atoms, OH, oxo (=O), CO2R3, (C1-C6)alkyl, (C1-C6)alkoxyl and phenyl; wherein heteroaryl is a mono- or bicyclic ring system having from 5 to 9 ring atoms and from 1 to 3 heteroatoms selected from N, O and S; R3 and R4 are independently selected from the group consisting of H, halogen atoms, CONH2, (C1-C6)alkyl, (C1-C6)alkanoyl and (C3-C8)cycloalkyl, as selective M3 receptor antagonists, to a method for their preparation, to compositions containing them, and to their therapeutic use for treatment of a respiratory disease such as asthma and chronic obstructive pulmonary disease (COPD).EFFECT: increased composition application efficiency.14 cl, 2 tbl, 34 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex
ethod of prevention of respiratory diseases in group keeping of calves // 2627461
FIELD: veterinary medicine.SUBSTANCE: method of preventing respiratory diseases of calves includes the use of a medicinal product based on vegetable raw materials, is characterized by the fact that before the formation of groups at an early stage of cultivation, in group of animals the calves are given a mixture of infusions of motherwort and pion in a ratio of 2:1 with milk at a dose of 2.5-3 ml.EFFECT: method allows to successfully prevent respiratory diseases of calves, increases the safety of animals and shortens the duration of the disease.3 cl, 2 tbl, 1 ex
ethod of treatment of obstructive bronchitis in dogs // 2627446
FIELD: veterinary medicine.SUBSTANCE: method involves the treatment with Vasotop P, a course of 1-2 months. Treatment of obstructive bronchitis with bacterial, viral and parasitic etiology is carried out in two stages, including the use of immunostimulants in the first stage with the administration of etiotropic therapy with antibiotics and/or antiparasitic drugs; in the second stage, the use of bronchodilators with the simultaneous use of Vasotop P at a dose of 0.125 mg per 1 kg Mass of the animal, and in the presence of relapse - for life. In another embodiment, the method comprises using Veroshpiron in capsules at a dose of 100 mg per dog 20 kg Course 5-7 days; Vasotope P at a dose of 0.125 mg per 1 kg Weight of the animal, course 1-2 months, and at the terminal stage of life and Riboxin + glucose of 2.5 ml per dog 20 kg 1 time per day, 3 days, intravenously.EFFECT: highly effective treatment of dogs with obstructive bronchitis on the background of chronic cardiac and renal insufficiency.2 cl, 1 dwg, 1 ex
ethod for respiratory disorders syndrome prevention for newborns // 2627441
FIELD: medicine.SUBSTANCE: for prevention of respiratory disorders syndrome in newborns, the patients receive Dexamethazon intramuscularly, 8 mg №3 in 8:00 hours on 25(0)-27(6) week of pregnancy, the course is repeated in 7 days with the total dose of 48 mg.EFFECT: invention provides prolongation of pregnancy, complicated by fetal bladder prolapse or premature amniotic fluid discharge.2 dwg, 3 ex
Bicyclic heterocyclic derivatives, their production and application // 2627269
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of general formula (I) , as well as to a method for their preparation, pharmaceutical compositions based thereon, and their application.EFFECT: new compounds have been obtained that can be used to treat or prevent pathology for which it is necessary to inhibit the mTOR kinase.20 cl, 4 tbl, 30 ex
Aza-aryl-1-h-pyrazol-1-yl-sulphonamides // 2627268
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) ,in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists.EFFECT: increased efficiency of compounds application.26 cl, 2 tbl, 33 ex

1-phenyl-2-pyridinylalkyl alcohols derivatives as phosphodiesterase inhibitors // 2626956
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of general formula , where: R1 is selected from the group consisting of: methyl; trifluoromethyl; R2 is selected from the group consisting of: methyl optionally substituted with cyclopropyl; cyclopentyl; or R1 and R2, together with their interconnecting atoms, form a 2,2-difluoro-1,3-dioxolane ring of formula (q) condensed with a phenyl group that carries -OR1 and -OR2 groups, where the asterisks indicate carbon atoms shared by such phenyl ring: , R19 is hydrogen; R3 is one or more substituents independently selected from halogen atoms; Z represents a -(CH2)n- group, where n is 0 or 1; A is a saturated and monocyclic (C3-C7) heterocycloalkylene group selected from the following list of di-radicals: , , , , , , , , , , where symbols [3] and [4] indicate the points of group A attachment to groups Z and K, respectively; K is selected from the group consisting of: -(CH2)mC(O)R4, where m can be 0 or 1; -C(O)(CH2)jR4, where j can be 1 or 2; -SO2(CH2)pR4, where p can be 0, 1 or 2; -(CH2)ySO2R4, where y can be 1 or 2; -(CH2)zR4, where z can be 1; and -C(O)(CH2)2SO2R4; R4 is a ring system which is a mono- or bicyclic ring which may be saturated, partially unsaturated or fully unsaturated, selected from phenyl, (C3-C8) cycloalkyl, (C3-C7) heterocycloalkyl where at least one ring carbon atom is replaced by a heteroatom selected from N, NH and O or heteroaryl, such ring is optionally substituted with one or more R5, which may be the same or different and which are independently selected from the group consisting of: (C1-C6) alkyl, optionally substituted with one or more groups independently selected from the list consisting of: -OH; (C3-C7) heterocycloalkyl(C1-C4)alkyl where at least one ring carbon atom is replaced by a heteroatom selected from N, NH, O; 5-6 member heteroaryl where at least one ring carbon atom is replaced by a heteroatom selected from N and O; -OR6 group, where R6 is selected from the group consisting of (C1-C6) haloalkyl; -SO2R7 group, where R7 is (C1-C4) alkyl; and methyl optionally substituted with one or more (C3-C7) cycloalkyls; halogen atoms; CN; NR8R9, where R8 and R9 are different or identical and independently selected from the group consisting of: H; (C1-C4) alkylen-NR13 R14, where R13 and R14 are different or identical and independently selected from the group consisting of: a (C1-C6) alkyl, or they form a saturated (C3-C7) heterocyclic ring together with the nitrogen atom to which they are attached; -SO2R15 group, where R15 is selected from the group consisting of: (C1-C4) alkyl; -C(O)OR17 group, where R17 is selected from the group consisting of: (C1-C6) alkyl; or they form, together with the nitrogen atom to which they are attached, a saturated or partially saturated heterocyclic ring which is optionally substituted by one or more (C1-C6) alkyl; (C1-C2) alkylene-NR8R9, as mentioned above; COR10, where R10 is (C1-C6) alkyl; oxo; -SO2R11, where R11 is (C1-C4) alkyl or NR8R9, where R8 and R9 are as above; -COOR12, where R12 is H, (C1-C4) alkyl or (C1-C4) alkylene-NR8R9, where R8 and R9 are as above; and -CONR8R9, where R8 and R9 are as above; where R6, R8, R9, R10, R11, R12, R13, R14, R15, R17 and R19 groups in each case may have the same or different value if more than one group is present; and their N-oxide derivatives on the pyridine ring or their pharmaceutically acceptable salts. The compound is a phosphodiesterase 4 (PDE4) enzyme inhibitors.EFFECT: improved properties.19 cl, 26 tbl, 36 ex
Adamantyl derivatives useful for treatment of jnk-mediated disorder // 2626890
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the heterocyclic compound of I formula or a pharmaceutically acceptable salt thereof, wherein R represents phenyl optionally substituted with one or more R'; R' is halo or methoxy; X represents CH; X1 represents C(=O)OCH3; Y represents N; Y1 It is OH, N(Y1')2, NHS(=O)2Y1', NHC(=O)Y1', NHC(=O)C(CH3)2OH or NHC(=O)C(CH3)2OC(=O)Y1'; each Y1' independently represents H, C1-6-alkyl or lower cycloalkyl; Y2 It is H. The invention also relates to formula I based on the compound of the pharmaceutical composition and the use thereof.EFFECT: new heterocyclic compounds useful for treating JNK-mediated disorder are obtained.12 cl, 5 tbl, 31 ex

ethods of production isoquinolinones and solid forms isoquinolinones // 2626883
FIELD: chemistry.SUBSTANCE: invention relates to new polymorphic forms of the compounds of formula (I), having inhibitory action against phosphoinositide 3-kinase (PI3K). The compounds may be used to treat cancer, such as leukemia, lymphoma, inflammatory disease and autoimmune disease. The polymorphic forms of the compound of formula (I) is the polymorphic form C of the hydrate of the compound of formula (I), which has characteristic peaks in the x-ray powder diffraction pattern (XRPD) 2θ=10.4°(±0.2°), 13.3°(±0.2°) and 24.3°(±0.2°); Polymorph A, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 12.2°(±0.2°), and 18.3°(±0.2°); Polymorph B, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=7.9°(±0.2°), 13.4°(±0.2°), and 23.4°(±0.2°); polymorphic form D, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=11.4°(±0.2°), 17.4°(±0.2°), and 22.9°(±0.2°); polymorphic form E, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=6.7°(±0.2°), 9.3°(±0.2°) and 24.4°(±0.2°); Polymorphic form F, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 17.3°(±0.2°), and 24.6°(±0.2°); Polymorphic form G which is the solvate of the tert-butyl methyl ether of the compound of formula (I) and has characteristic peaks in the powder XRPD pattern 2θ=6.7°(±0.2°), 9.5°(±0.2°) and 19.0°(±0.2°); Polymorphic form H, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=8.9°(±0.2°), 9.2°(±0.2°) and 14.1°(±0.2°); Polymorphic Form I, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.7°(±0.2°), 19.3°(±0.2°), and 24.5°(±0.2°), and the polymorphic form J, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.1°(±0.2°), 17.3°(±0.2°) and 18.3°(±0.2°). The invention also relates to a process of preparing form C. For example, mentioned process comprising (i) exposure of the medium containing water, a composition comprising at least one polymorphic form, not a form of a compound of formula (I), for a period time sufficient for the transformation, preferably for 18-24 hours, at least 50% of the total amount of the polymorphic form (s) a non-form C; and (ii) recovering mentioned polymorph form C.EFFECT: high effectiveness of compounds.84 cl, 31 dwg, 16 tbl, 42 ex
eans for polyps treatment in sinuses and prevention of their repeated growth, and method of its application // 2626829
FIELD: medicine.SUBSTANCE: method for polyps treatment in the sinuses is proposed. The method is characterized by application of aqueous solutions of acetic acid in concentrations of 3-6% as means or drug component for the treatment of polyps in the nose sinuses, and 1-2 drops of solution are injected into each sinus within 1-2 weeks, 3-5 times a day.EFFECT: improved safety and effectiveness of polyps treatment in the sinuses, prevention of repeated growth, reduced duration and costs of treatment.3 ex
eans for emergency voice recovery at flash aphonia // 2625766
FIELD: medicine.SUBSTANCE: invention is a means for emergency recovery of voice in sudden aphonia, intended for inhalation, comprising lidocaine hydrochloride in an amount of 1.2-1.5% by weight, sodium bicarbonate in an amount of 0.5% by weight and water doubly-modified - the rest, at pH 8.4 and osmotic activity of 280-330 mOsmol/l of water.EFFECT: invention provides an emergency recovery of the suddenly lost voice, reduces the symptoms of inflammation of the vocal cords, has an anesthetic effect on the larynx, has a sedative effect without irritating, cauterizing and toxic action.1 cl
Application of pyrazole derivative in treatment of acute attacks of chronic obstructive pulmonary disease // 2625762
FIELD: pharmacology.SUBSTANCE: 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof are applied. Application of a single dose of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methyl-benzamide or a pharmaceutically acceptable derivative thereof, using 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methyl-benzamide in the drug manufacture, method of treating acute attacks of chronic obstructive pulmonary disease, a drug for oralinjection comprising 3-[5-amino-4-(3-cyanobenzoyl)-pirasol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof are also proposed.EFFECT: treatment of acute attacks of chronic obstructive pulmonary disease.17 cl, 5 tbl, 1 ex
Water-based liquid composition with bromfenac possessing preservative effectiveness // 2625755
FIELD: chemistry.SUBSTANCE: invention represents the use of bromfenac or its salt to improve the preservative effectiveness of the water-based liquid composition, comprising (a) bromfenac or its salt and (b) benzalkonium chloride, and c) at least one agent selected from the group consisting of nonionic surfactant and water-soluble polymer. The invention also relates to a method of improving the preservative effectiveness of the aqueous solution described above, which comprises adding of bromfenac or its salt in an amount of 0.1 w/v % to the solution.EFFECT: invention enables to obtain a composition with imroved preservative activity, wherein there are low concentrations of benzalkonium chloride preserving agent.10 cl, 21 tbl, 4 ex
Kinase inhibitors // 2623734
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof which have an inhibitory activity against p38 MAP kinase. In formula (I), W is NH, Y is selected from the -O (CR3R4)n- group, where n is 0, R1 is (IIb) group , X1 is -(CH)-, R9 is C1-C6alkyl, C3-C6cycloalkyl or phenyl optionally substituted with halogen atoms, R12 is a hydrogen atom, A is a bivalent cycloalkylene radical having 5, 6 or 7 ring atoms, wherein the said cycloalkylene ring is attached to W and Y and fused to a phenyl ring, wherein such phenyl ring is optionally substituted with one or two R27 groups, R27 is selected from halogen, R2 is a radical of formula (IVb) or (IVc) where R17 is selected from a single electron pair, hydrogen or aryl, where any such aryl may be optionally substituted by a C1-C6alkyl or C3-C7cycloalkyl; or R17th is a group of general formula (V) R20 is selected from the group consisting of -CH3 or -C2H5; R21 is -CH3 or -C2H5; R18 is selected from the group consisting of a single electron pair, hydrogen, aryl, heteroaryl, -(C1-6alkyl), -(C3-C7cycloalkyl), -(C3-C7heterocycloalkyl), (C5-C7heterocycloalkyl)-(C1-C6alkyl) and (C5-C7heterocycloalkyl)-(C3-C6cycloalkyl) group, R19 Is selected from -CF3, z1, z2, z3 and z4 are independently selected from the group consisting of C, N, O, -CH- and -NH- groups, in such combination that the resulting ring is an aromatic system, T is -CR28=; R28 is halogen; R22 is H or halogen. The invention also relates to a pharmaceutical composition comprising the said compounds, a method for treatment of diseases which benefit from p38 MAP kinase inhibition, and their application for manufacture of a medicament for treatment of such diseases.EFFECT: increased efficiency of compounds application.14 cl, 2 tbl, 35 ex
Tetrahydrotriazolopyrimidine derivatives as inhibitors of human neutrophil elastase // 2622643
FIELD: pharmacology.SUBSTANCE: invention compounds have the properties of human neutrophil elastase (HNE) inhibitors. In formula I A represents CH; R1 is selected from hydrogen; a (C1-C6) alkyl; a (C1-C6)alkylNR7R8group; a (C1-C4)alkenyl; a (C1-C6)alkylphenyl, where the phenyl ring is possibly substituted by a (C1-C6)alkylNR15R16 group or a (C1-C6)alkylN+R15R16R17group; a -(CH2)nCONR5R6group; a -CH2-(CH2)nNR5SO2R6group; a -(CH2)t-(C6H4)-SO2(C1-C4)alkyl group; a -(CH2)rSO2(C1-C4)alkyl group, wherein such (C1-C4)alkyl is possibly substituted by a -N+R15R16R17group; a -SO2-phenyl group. Such phenyl ring is possibly substituted by a (C1-C6)alkylNR7R8group; and a -(CH2)n-W group, where W represents a 6-membered heteroaryl ring with one heteroatom N, which is possibly substituted by a group -SO2(C1-C4)alkyl; n means 1; t means zero, 1; r means 2, 3; R5 is selected from the group consisting of hydrogen, a (C1-C6)alkyl, a (C1-C6)alkylNR16R15group and a (C1-C6)alkylN+R17R15R16group; R6 represents hydrogen or a (C1-C6)alkyl; R7 is selected from the group consisting of a (C1-C6)alkyl, a carbonyl(C1-C6)alkyl group, a -SO2(C1-C4)alkyl group and a (C1-C6)alkylNR16R15group; R8 represents a (C1-C6 )alkyl; alternatively, R7 and R8 can form, together with the nitrogen atom to which they are attached, a (C5-C7)heterocycloalkyl ring system, which is possibly substituted by oxo; R16 represents a (C1-C6)alkyl; R15 represents a (C1-C6)alkyl; R17 represents a (C1-C6)alkyl; R2 represents hydrogen or -SO2R4, where R4 is selected from a (C1-C6)alkyl; R14 represents a cyano group or a -C(O)-XR3group; X is a divalent group selected from -O- and -NH-; R3 represents a group selected from hydrogen; a (C1-C6)alkyl; a group of formula -[Alk1]-Z, where Alk1 represents a (C1-C4)alkylene radical, and Z represents NR9R10, where R9 and R10 independently represent a (C1-C6)alkyl. The invention also relates to pharmaceutical compositions and to a method of treating a disease or a condition in which HNE is involved.EFFECT: new formula compounds obtained, having the properties of human neutrophil elastase inhibitors.16 cl, 1 tbl, 39 ex
ethod for regenerative treatment of patients with bronchial asthma and obesity // 2622610
FIELD: medicine.SUBSTANCE: basic therapy is carried out and electric stimulation is performed transcranially by pulsed current with pulse width of 4-5 ms, frequency of 76 Hz, amperage from 0.5 mA to 2.75 mA. Procedure duration is 30 minutes. The course of treatment consists of 10 daily treatments in the morning. At that, starting from the second procedure, the current strength is increased by 0.25 mA and duration of each subsequent treatment is increased by 1 minute.EFFECT: method allows to improve the rehabilitation treatment efficiency and to increase the remission period, which is achieved by the developed mode of transcranial electrostimulation.4 cl, 3 tbl, 3 ex
ethod for lung ventilation during thoracic surgery in lung cancer patients with concomitant chronic obstructive pulmonary disease // 2621381
FIELD: medicine.SUBSTANCE: high-frequency mechanical ventilation is provided. At that, high-frequency ventilation is performed using oxygen in catheter ventilation mode at a frequency of 90-95 cycles per 1 min at gas flow rate of 5-7 l per 1 min. Additionally, via a micro pump nebulizer, embedded into the breathing system, Spiriva bronchial spasmolytic is injected into the independent lung during the main phase of surgical intervention at a dose of 18 g, dissolved in 4 ml of physiological solution, in two steps by 2 ml of the prepared solution for 15 min with 60 min intervals between introductions.EFFECT: method allows to increase the effectiveness of ventilation support in patients with lung cancer and COPD due to bronchospasm reduction and improvement of capillary-alveolar gas exchange.1 ex, 2 tbl, 1 dwg
Antifibrolytic means // 2621299
FIELD: pharmacology.SUBSTANCE: digitoxin application is described.EFFECT: digitoxin effectively reduces TGF-β-induced differentiation of myofibroblasts and can be used to treat idiopathic pulmonary fibrosis with a reduction in the number of complications.2 dwg
 
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