(A61K31/4965)

2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex

Amide compounds, methods for production, application as means for treatment and prevention of diseases caused by rna-containing viruses // 2628800
FIELD: pharmacology.SUBSTANCE: compounds of the invention are intended for manufacture of a pharmaceutical composition, kit or drug. The invention also relates to a process for preparation of compounds of the invention (versions). Compounds of the invention are intended for use in the prevention or treatment of diseases caused by RNA-containing viruses belonging to enteroviruses, metapneumoviruses or pneumoviruses.EFFECT: amide compounds for treatment or prevention of diseases caused by RNA-containing viruses.26 cl, 8 tbl, 5 ex
Inhibitors of nonprilyzine // 2622288
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula , wherein R1 is selected from -OR7 and -NR8R9; R2 is H; X is -C1-9heteroaryl, selected from pyrazole, imidazole, triazole, benzotriazole, furan, tetrazole, pyrazine, thiophene, oxazole, isoxazole, thiazole, oxadiazole, pyridazine, pyridine, pyrimidine, benzoxazole, pyridylimidazole and pyridyltriazole; R3 is absent or is selected from H; Halogen; -C0-5alkylene-OH; -NH2; -C1-6alkyl; -CF3; -C3-7cycloalkyl; -C0-2alkylene-O-C1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C (O) NR22R23; -NHC(O)R24; =O; -NO2; -C(CH3) =N(OH); Phenyl optionally substituted with one or two groups independently selected from halogen, -OH, -CF3, -OCH3, -NHC(O)CH3 and phenyl; Naphthalenyl; Pyridinyl; Pyrazinyl; Pyrazolyl optionally substituted with methyl; Thiophenyl, optionally substituted by methyl or halogen; Furanyl; and -CH2-morpholinyl; and R3, when present, is attached to a carbon atom; R4 is absent or is selected from H; -HE; -C1-6alkyl; -C1-2alkylene-COOR35; -OCH2 O(O)CH (R36)NH2; -OCH2O(O)CH3; -CH2CH(OH)CH2OH; and phenyl or benzyl optionally substituted with 1 to 3 groups selected from halogen, -COOR35, -OCH3, -OCF3 and -SCF3; and R4, when present, is attached to a carbon or nitrogen atom; or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-; A is 0 or 1; R5 is halogen; B is 0 or an integer of 1 to 3; Each R6 is independently selected from halogen, -OH, -CH3 and -OCH3; R7 is selected from H, -C1-8alkyl, -[(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl and the structure of formula (a); R10 is -O-C3-7cycloalkyl; and R32 is -C1-6alkyl; R8 and R9 are H; R20, R21 and R35 are independently selected from H and -C1-6alkyl; R22 and R23 are independently selected from H, -C1-6alkyl, -CH2COOH, -(CH2)2OH, -(CH2)2OCH3, - (CH2)2SO2NH2, -(CH2)2N(CH3)2, -C0-1alkylene-C3-7-cycloalkyl and -(CH2)2-imidazolyl; or R22 and R23 are taken together to form a ring; R24 is selected from -C1-6alkyl; -C0-1alkylene-O-C1-6alkyl; Phenyl optionally substituted by halogen or -OCH3; and pyridinyl; and R36 is -CH (CH3) 2; and wherein the methylene linker on the biphenyl is optionally substituted with one or two -C1-6 alkyl groups; or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are prepared by combining a compound of formula with a compound of formula 2 to provide a compound of formula I; Where P1 is also H. Also, the invention relates to an intermediate of formula 1, wherein P1 is H. The compounds of formula (I) are intended for the preparation of a medicament or pharmaceutical composition having inhibitory activity against non-prolamin (NEP). (a).EFFECT: compounds that have a non-lysine inhibitory enzyme activity.28 cl, 61 tbl, 25 ex
ethod of treating and preventing chronic inflammatory diseases of nasopharynx associated with inhalation exposure to benzene and formaldehyde in children // 2618469
FIELD: medicine.SUBSTANCE: invention can be used to treat and prevent chronic inflammatory diseases of nasopharynx (CIDN) in children aged 4 through 10 years old, living in area of industrial enterprises impact in conditions of atmospheric air pollution with benzene and formaldehyde. Treatment is carried out by combined administration of the following medicinal products to children: "Tonsilgon N" preparation orally in a dose for children aged 4 through 6 years old - 10 drops 3-4 times a day; for children over 6 years - 1 pill 3-4 times a day, for 21 days course; "Multi-Tabs Junior" 1 tablet once a day for 21 days; "Eslidine" 1 capsule twice a day before meals in the morning and evening for 21 days; "Zodac" preparation 5 mg once a day in a dose for children aged 4 through 6 years old; 10 mg once a day for children over 6 years old, for 21 days course, and simultaneously with children medical treatment, starting from the third day of drug administration, pulsed low-frequency magnetotherapy is employed for 10 minutes daily or every other day for 10 days course on nose sinuses or submandibular regions in the form of two-inductor technique with transverse arrangement of inductors and feedback sensor position at right supraclavicular region.EFFECT: invention provides treatment and prevention of chronic inflammatory disease of nasopharynx associated with exposure to benzene and formaldehyde in children.5 cl, 5 tbl

Arry-520 application for treatment of cancer for patients with low acs // 2617392
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, namely to oncology and can be used to treat cancer for patients with low concentrations of human α 1-acid glycoprotein (ACS). The methods of the invention include biological sample obtaining from a patient to determine the concentration of ACG and ARRY-520 administration to a patient with low concentration of ACG.EFFECT: increased efficiency of treatment due to a better response to the introduction of ARRY-520 at low ACG.57 cl, 6 tbl, 10 dwg, 10 ex

ethod of using 4-((1r,3s)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine and salts thereof in treating schizophrenia // 2613177
FIELD: medicine.SUBSTANCE: group of inventions relates to treating central nervous system diseases. Use of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine or its salt is disclosed for treating schizophrenia, schizophreniform disorder, schizo-affective disorder, delusional disorder, short-term psychotic disorder, induced psychotic disorder or bipolar disorder, every week or twice a week in form of immediate release composition (IR-composition), long, controlled or delayed release for peroral administration in dose of 20 mg/week up to 50 mg/week in terms of free base of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine and application of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine (cikronapine) or its salt for preparing drug for above treatment.EFFECT: introduction 1 time a week of declared dose is effective in reducing total PANSS score relative to daily administration of 10 mg; it can lead to increase of consent of patient.10 cl, 1 dwg, 1 tbl
Novel pyrazine derivatives // 2612138
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) modulate activity of cannabinoid receptor 2 (CB2). . In formula (I) R1 is a halophenyl or C3-C6-cycloalkyl-C1-C6-alkoxy; R2 is a C3-C6-cycloalkyl, azetidinyl or difluoroazetidinyl; one of R3 and R4 is hydrogen, and other is -(CR5R6)-R7 or -A-R7; or R2 is a C3-C6-cycloalkyl, and R3 and R4 together with a nitrogen atom, to which they are bonded, form piperidinylamine; R5 and6 are independently selected from hydrogen, C1-C6-alkyl, halogen-C1-C6-alkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C6-alkyl, phenyl, phenyl-C1-C6-alkyl and halophenyl; or R5 and6 together with carbon atom, to which they are bonded, form C3-C6-cycloalkyl or oxetanyl; R7 is cyano, carboxy, 5-methyl-[1,2,4]oxadiazol-3-yl, 5-amino-[1,2,4]oxadiazol-3-yl, thiazolyl, C1-C6-alkylthiazolyl, pyridinyl, C1-C6-alkylaminocarbonyl, hydroxy-C1-C6-alkyl, C1-C6-alkoxy-C1-C6-alkyl, aminocarbonyl, C1-C6-alkoxycarbonyl, di-C1-C6-alkylaminocarbonyl, phenyl-C1-C6-alkyl, pyridinyl-C1-C6-alkyl, halogen-C1-C6-alkylaminocarbonyl, 5-phenyl-2-methyl-oxazol-4-yl-alkyl, aminocarbonyl-C1-C6-alkyl or halogen; and A is cyclohexyl or thiophenyl, under condition specified in patent claim. Invention also relates to individual compounds, pharmaceutical composition, use of compounds and to a method of modulating CB2 receptor activity.EFFECT: technical result is obtaining novel compounds of formula (I) modulating activity of cannabinoid receptor 2 (CB2).19 cl, 111 ex

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

Form of pharmaceutical composition multi-layer coating for oral administration containing omega-3 fatty acid or its alkyl ester, as well as medicinal agent based on statin // 2600804
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutics. Pharmaceutical composition for oral administration is described containing: gelatine capsule core, coated with first and second layers of coating. Gelatine capsule core contains omega-3 fatty acid or its alkyl ester. First coating layer contains hydroxypropyl methylcellulose and copolymer of butyl methacrylate, (2-dimethylaminoethyl)methacrylate and methyl methacrylate with weight ratio of 1:2:1; where weight ratio of hydroxypropyl methylcellulose to said copolymer ranges from 1:0.8 to 1:10. Second coating layer contains medicinal agent based on statin as inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase.EFFECT: invention prevents sticking of gelatine capsules' cores to each other and deformation of gelatin capsules' cores, which can occur in process of aqueous coating application, invention also provides pharmaceutical composition disintegration and stability requirements compliance.13 cl, 9 tbl, 7 ex

Prognostic factors for treating cancer // 2600026
FIELD: medicine.SUBSTANCE: invention refers to medicine and represents a method for prediction of response of oncological patient with non-Hodgkin's lymphoma to anticancer therapy, including bortezomib and rituximab, characterized by that the method involves determination of level or amount of first prognostic factor and determination of presence or amount of second prognostic factor, wherein low level of CD68 or polymorphism of PSMB1 (P11A) correlates with, at least, one positive result. Invention also relates to a diagnostic kit for detecting oncological patients with non-Hodgkin's lymphoma, which are candidates for treating cancer with bortezomib and rituximab, as well as method of treating cancer in oncological patients with non-Hodgkin's lymphoma.EFFECT: invention implementation enables predicting positive response of oncology patient to combination therapy of bortezomib and rituximab.7 cl, 5 ex, 25 tbl, 8 dwg

Novel cyclopentane derivatives // 2572555
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to compounds of formula where A1 and R1, R2, R3, R4 and R5 are determined in invention formula, which are preferable inhibitors of cathepsin cycteinprotease, in particular cathepsin S or L cycteinprotease, which makes them useful as medications, especially for treatment of diabetes, atherosclerosis, aneurism of abdominal aorta, peripheral arterial disease or diabetic nephropathy.EFFECT: invention relates to methods of obtaining claimed compounds, thereof-containing pharmaceutical composition and thereof application.24 cl, 1 tbl, 255 ex

Cyclopentylacrylamide derivative // 2565070
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound, represented by general formula or its pharmaceutically acceptable salt, in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy- C1-C6alkylsulphonyl group, and A is selected from group which includes: thiazolyl group, 1,2,4-thiadiazolyl group, pyrazolyl group, pyridyl group, pyrazinyl group, isooxazolyl group, benzothiazolyl group and thiazolo[5,4-b]pyridyl group, and A can be mono-substituted by substituent, selected from group, which includes halogen atom; C1-C6alkyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C6alkoxyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C3alkoxy-C1-C2alkoxyl groups; C1-C3alkoxycarbonyl-C1-C2alkoxyl groups; C1-C6alkylsulphanyl groups; C1-C6amino-alkylsulphanyl group, optionally substituted with C1-C3alkyl group; C1-C6alkylsulphanyl-C1-C6alcoxyl groups; phenyl group; 1,3-dipxolane, substituted with two C1-C6alkyl groups; piperazinesulphonyl is substituted with methyl group; 1,3-dioxolanemethyl, substituted with two methyl groups; piperazinemethyl, substituted with methyl group; tetrahydropyranyloxy-C1-C3alkoxy group; aminosulphonyl groups, optionally substituted with C1-C3alkyl group; C1-C6 hydroxyalkylsulphanyl groups; -(O)(CH2)C(O)O-C1-C6alkyl group; -C(O)O-C1-C6 alkyl group; as well as groups, represented by general formula -(CH2)mP(O)R4R5 (where R4 and R5 independently represent C1-C3alkoxyl group; m is integer number from 0 to 1). Compound of formula (1) is intended, as active ingredient, for production of pharmaceutical composition, which has effect for activation of glucokinase (GK) or hypoglycaemic action. Invention also relates to intermediate compounds, represented by formula in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy-C1-C6alkylsulphonyl group.EFFECT: acrylamide compounds as glucokinase activator for treatment of diabetes.21 cl, 38 tbl, 55 ex

Synergic combination of proteasome inhibitor and vitamin k for inhibition of growth and proliferation of tumour cells, pharmaceutical composition and thereof-based anti-tumour medication // 2563986
FIELD: medicine, pharmaceutics.SUBSTANCE: group of inventions relates to medicine and deal with synergic combination of proteasome inhibitor bortezomib in quantity from 0.05 mg to 10 mg and vitamin K analogue sodium 2,3-dihydro-2-methyl-1,4-naphthoquinone-2-culphonate in amount from 2 mg to 100 mg for inhibition of growth and proliferation of tumour cells, pharmaceutical composition based on said combination and anti-tumour medication, including bortezomib and said vitamin K analogue. Invention can be used for treatment of hepatocellular carcinoma, melanoma, mammary gland carcinoma, thyroid gland carcinoma, multiple myeloma and other malignant neoplasms.EFFECT: synergism of claimed combination and sharp reduction of bortezomib toxicity in comparison with its independent application are demonstrated.9 cl, 8 tbl, 8 ex

Crystals // 2556206
FIELD: medicine, pharmaceutics.SUBSTANCE: invention describes crystals of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide ("compound A"), as a form I of the compound A crystal, which shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in its power X-ray diffraction spectrum, as a form II of the compound A crystal, which shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in its power X-ray diffraction spectrum, as a form III of the compound A crystal, which shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in its power X-ray diffraction spectrum. There are also described methods for producing the forms I, II and III of the compound A crystal, based pharmaceutical composition and PGI2 receptor agonist agent, an accelerating agent for angiogenic therapy, gene engineering or autoimmune bone marrow transplantation, and an accelerating agent for angiogenesis for peripheral artery recovery or angiogenic therapy on the basis thereof; there are also described a preventive or therapeutic agent for a wide range of diseases and conditions.EFFECT: preparing the new therapeutic agent for the wide range of diseases and conditions.11 cl, 6 dwg, 6 tbl, 5 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

New phenol derivatives and their pharmaceutical or cosmetic application // 2540858
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of structural formula (I), which can be used for treating diseases mediated by an androgen receptor. In formula (I), R1 means (C2-6)alkyl, (C1-6)alkyloxy, -S(O)m-(C1-6)alkyl, (C1-6)fluoroalkyl, CN or halogen, R2 and R3 are identical or different and mean a hydrogen atom or (C1-9)alkyl, R4, R5, R6, R7 are identical or different and mean a hydrogen or halogen, X means CH or N, Y means either a nitrogen atom, or a carbon atom substituted by (C1-6)alkyl, (C1-6)alkyloxy, (C1-6)fluoroalkyl, a hydrogen atom or halogen; m is equal to 0, 1 or 2.EFFECT: invention refers to using the compounds for preparing a therapeutic agent for preventing and/or treating hirsutism, androgenetic alopecia, hypertrichosis, atopic dermatitis, disordered sebaceous gland, such as hyperseborrhea, acne, greasy skin or seborrheic dermatitis.8 cl, 2 tbl, 26 ex

N-pyridin-3-yl or n-pyrazin-2-yl carboxamides as agents increasing level of hdlp cholesterol // 2540069
FIELD: chemistry.SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compounds of formula I and to their pharmaceutically acceptable salts, where A is selected from CH or N; R1 is selected from the group, consisting of C3-6-cycloalkyl, C3-6-cycloalkyl-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, halogen-C1-7-alkyl; R2 and R6 independently on each other represent hydrogen of halogen; R3 and R5 independently on each other are selected from the group, consisting of hydrogen, C1-7-alkyl and halogen; R4 is selected from the group, consisting of hydrogen, C1-7-alkyl, halogen and amino; R7 is selected from the group, consisting of C1-7-alkyl, C1-7alkoxy-C1-7-alkyl, C1-7-alkoxyimino-C1-7-alkyl, 4-6-membered heterocyclyl, containing one heteroatom O, phenyl, with said phenyl being non-substituted or substituted with one hydroxy group, and 5-10-membered heteroaryl, containing 1-3 heteroatoms, selected from N, S and O, said heteroaryl is not substituted or is substituted with one or two groups, selected from the group, consisting of C1-7-alkyl, hydroxy, C1-7-alkoxy, cyano, C1-7-alkylaminocarbonyl and halogen. Invention also relates to pharmaceutical composition based on formula I compound and to method of obtaining formula I compound.EFFECT: obtained are novel heterocyclic compounds, which are agents, increasing level of LDLP.17 cl, 2 tbl, 89 ex
ethod of preventing cerebral form of radiation sickness // 2537170
FIELD: medicine.SUBSTANCE: invention relates to medical radiology and can be used for prevention of cerebral form of acute radiation sickness. Claimed is application of officinal drug pyrazinamide as medication for prevention of cerebral form of acute radiation sickness. Pyrazinamide has been used for treating tuberculosis.EFFECT: preventing in 100% of cases development of early temporary incapacity in case of irradiation in dose 200 Gy, improvement of indices of behavioral and research activities in irradiated animals, in reduction of frequency of motor disorders, reduction of frequency and expression of convulsive-hyperkinetic syndrome and 9,5 fold increase of average life expectancy of irradiated animals Pyrazinamide is not inferior to drug - nicotinamide prototype in efficiency of radioprotective action.4 tbl, 4 ex

Compositions for treating abuse with substances causing painful addiction, and improvement of behaviour associated with abuse // 2535046
FIELD: medicine, pharmaceutics.SUBSTANCE: group of inventions relates to medicine, in particular to a composition, the application of the composition and a method of treating abuse with substances, causing painful addiction in a subject. The composition contains a carbamoyl compound, or its pharmaceutically acceptable salt, or an ester as an active ingredient and the method includes the introduction of a therapeutically effective quantity of the carbamoyl compound, or its pharmaceutically acceptable salt, or the ester.EFFECT: composition is used for the treatment of abuse with substances, causing painful addiction in a subject, as well as to an improvement of behaviour associated with the abuse.14 cl, 1 tbl, 3 ex

Pharmaceutical compositions // 2532330
FIELD: medicine, pharmaceutics.SUBSTANCE: what is presented is a group of inventions involving a pharmaceutical composition for preventing or treating diabetes mellitus, diseases related to diabetes mellitus, or complications of diabetes mellitus containing a combination of (A) (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol, or its salt, hydrate or hydrate salt, and (B) metformine or an agent intensifying insulin secretion, and a combination of the same formulation and for the same application.EFFECT: in addition to the pronounced blood plasma glucose reduction, the synergetic effect is ensured in inhibiting the plasma insulin level; what is also shown is inhibiting the side effect of glimepiride that is a body weight increase.16 cl, 20 tbl

Stable formulations of bortezomib // 2529800
FIELD: medicine, pharmaceutics.SUBSTANCE: storage-stable pharmaceutical composition represents a liquid formulation containing bortezomib and a system of anhydrous solvents and applicable for injection. A primary ingredient of the system of anhydrous solvents is propylene glycol. Bortezomib is found in the concentration of at least 1 mg/ml. The pharmaceutical composition contains a total amount of aqueous buffer of 10 vol. % or more.EFFECT: stable pharmaceutical composition according to invention maintains bortezomib degradation at the level of not less than 10 wt % when keeping the liquid formulation for at least three months in the ambient environment.9 cl, 10 tbl

Tablets and granulated powders containing 6-fluor-3-hydroxy-2-pyrazincarboxamide // 2527766
FIELD: medicine, pharmaceutics.SUBSTANCE: invention discloses a tablet for treating or preventing viral infections which contains 50-95% of 6-fluor-3-hydroxy-2-pyrazincarboxamide or its salt; it has a size facilitating ingestion; it possesses excellent release characteristics of the active principle and has hardness.EFFECT: method enables the tablet maintaining stability when applying a film coating, packing and transporting.16 cl, 19 ex, 4 tbl

Benzene or thiophen derivative and using it as vap-1 inhibitor // 2526256
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound presented by formula , wherein A1 means benzene or heterocycle specified in a group consisting of pyridine, pyrazine, imidazole, thiazole, pyrimidine, thiophen, pyridazine, benzoxazine and oxobenzoxazine; A2 means benzene, if needed substituted by fluorine, or thiophen; B1 means hydrogen, lower alkyl, if needed substituted by piperazinyl or morpholino, halogen-substituted lower alkyl, lower alkoxy substituted by carbamoyl, acylamino, carbamoyl or lower alkylcarbonyloxy (provided A1 means thiazole, B1 does not mean acylamino); B2 means hydrogen or a functional group containing at least one nitrogen atom specified in a group consisting of acylamino, pyrrolidinyl, morpholino, piperidinyl, if needed substituted by acyl, piperazinyl, if needed substituted by lower alkyl or acyl, pyrazolyl, diazabicyclo[2.2.1]heptyl, if needed substituted by acyl, and di-(lower alkyl)amino, if needed substituted by amino or acylamino (provided A1 means thiazole, B2 does not mean acylamino); Y means a group presented by formula , wherein J means ethylene or lower alkynylene; L means a bond; M means a bond; X means -(CH2)m-, -(CH2)m-O- or -(CH2)m-NR2- (wherein m is an integer of 0 to 3, and R2 means hydrogen); D means -NR3-, wherein R3 means hydrogen; and E means amino, or its pharmaceutically acceptable salt. The compounds of formula (I) are used for preparing a pharmaceutical agent or a pharmaceutical composition for treating or preventing the VAP-1 related diseases.EFFECT: benzene or thiophen derivative as a VAP-1 inhibitor.13 cl, 25 tbl, 125 ex

Diaminoheterocyclic carboxamide compound // 2526253
FIELD: medicine, pharmaceutics.SUBSTANCE: compounds can find application for preventing or treating cancer, lung cancer, non-small cells lung cancer, small-cell lung cancer, EML4-ALK hybrid polynucleotide-positive cancer, EML4-ALK hybrid polynucleotide-positive lung cancer or EML4-ALK hybrid polynucleotide-positive non-small cells lung cancer. In formula (I) -X-: group of formula , A represents chlorine, ethyl or isopropyl; R1 represents phenyl wherein carbon in the 4th position is substituted by the group -W-Y-Z, and carbon in the 3rd position can be substituted by a group specified in a group consisting of halogen, R00 and -O-R00; R00: lower alkyl which can be substituted by one or more halogen atoms; -W-: a bond, piperidine-1,4-diyl or piperazine-1,4-diyl; -Y- represents a bond; Z represents a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more substitutes R00; R2 represents (i) an optionally bridged saturated C3-10cycloalkyl which can be substituted by one or more groups specified in -N(lower alkyl)2, lower alkyl, -COO-lower alkyl, -OH, -COOH, -CONH-RZB and morpholinyl, or (ii) a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more groups specified in a group consisting of lower alkyl, -CO-lower alkyl, oxo, -CO-RZB and benzene; and RZB: phenyl which can be substituted by a group consisting of halogen and -O-lower alkyl; R3 represents -H.EFFECT: invention refers to new compounds of formula or their pharmaceutically acceptable salts possessing the properties of a selective inhibitor of EML4-ALK hybrid protein kinase activity.16 cl, 201 tbl, 582 ex

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

Therapeutic compositions containing macitentan // 2519161
FIELD: medicine, pharmaceutics.SUBSTANCE: there are presented: a product for treating pulmonary arterial hypertension containing macitentan or its pharmaceutically acceptable salt in a combination with a prostacyclin receptor (IP) agonist specified in iloprost, beraprost, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulphonyl)acetamide, {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid or their pharmaceutically acceptable salt (versions), a pharmaceutical composition for the same application and formulation of the active agents. What is also presented is using macitentan or its salt in a combination with the above agonist for preparing the therapeutic agent for treating pulmonary arterial hypertension.EFFECT: what is shown is synergic action (double effect) of the declared combinations 10 cl, 1 tbl, 1 ex

Using pentaaminofullerenes as antimicrobial agents and antimicrobial composition based thereon // 2501785
FIELD: chemistry.SUBSTANCE: in formula 1 , X denotes a negative charge which is localised on a fullerene skeleton, a chlorine atom bonded to a carbon skeleton or a hydrogen atom; the NR1R2 moiety denotes an amine residue, where R1 and R2 are hydrogen atoms or linear or branched alkyl radicals (CmH2m+1; n=1-20) that are substituted with protonated (NH3 +) or unprotonated (NH2) amine groups, or a piperazine residue of general formula 1c-1 , where R, R'1, R'2, R'3 and R'4 are hydrogen atoms or linear or branched alkyl (CmH2m+1; n=1-20) radicals, as well as residues of aliphatic alcohols -(CH2)nOH, ethers -(CH2)nOR'5, thiols -(CH2)nSH, acids -(CH2)nCOOH, esters thereof -(CH2)nCOOR'5 or amides -(CH2)nCONR'5R'6, for which n=0-20, R'5 and R'6 are hydrogen atoms or linear alkyl (CmH2m+1; n=1-20) radicals.EFFECT: stronger or prolonged antibacterial action.2 cl, 2 dwg, 2 tbl, 3 ex

Fibrosis inhibitor // 2497525
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pharmaceutics and medicine and concerns a fibrosis inhibitor containing 2-{4-N-(5,6-diphenyl-pyrazin-2-yl)-N-isopropylamino]butyloxy}acetic aci or a pharmaceutically acceptable salt thereof or 2-{4-[N-(5,6-diphenyl-pyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide or a pharmaceutically acceptable salt thereof as an active ingredient for treating interstitial pneumonia, pulmonary fibrosis, scleroderma or hepatic cirrhosis.EFFECT: inhibitor provides high efficacy.6 cl, 0 dwg, 6 ex

Novel compounds, use and production thereof // 2493152
FIELD: chemistry.SUBSTANCE: invention relates to a compound, which is N3-1H-indol-5-yl-5-pyridin-4-ylpyrazine-2,3-diamine, or a pharmaceutically acceptable salt thereof, which can act as inhibitors of protein kinase, especially FLT3 tyrosine kinase. The invention also relates to a pharmaceutical composition which contains said compound in combination with another molecularly directed (target) agent, which is a traditional cytotoxic agent or a compound used after chemotherapy, supporting therapy targeted on stem cells and in case of MLL rearrangement acute lymphoblastic leukaemia in children.EFFECT: obtaining a novel compound which can be used in medicine for preventing or treating haematological malignant growths such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative diseases, autoimmune diseases and skin diseases, such as psoriasis and atopic dermatitis.16 cl, 2 tbl, 26 ex

Combined therapy of tuberculosis // 2484819
FIELD: medicine, pharmaceutics.SUBSTANCE: group of inventions refers to medicine and aims at therapy of tuberculosis. What is used is a combination of formula (I), (S)-N-[[3-[3-fluor-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-xazolidinyl]methyl]cetamide, or a pharmaceutically acceptable salt thereof in combination with at least two agents, for preparing a therapeutic agent for treating tuberculosis after the individual has undergone the initial therapeutic phase.EFFECT: use of the declared group of inventions provides a high therapeutic effect of treating tebrculosis.12 tbl, 8 ex, 10 cl

Pyrazinone derivatives and use thereof in treatment of lung diseases // 2479580
FIELD: chemistry.SUBSTANCE: invention relates to pyrazinone derivatives of formula (I): , where R1, R2, R3, R4, R5, R and R7 are as defined in claim 1 of the invention. The invention also describes a crystalline form, compounds of formula I, use of the compound of formula I in producing a medicinal agent for treating chronic obstructive pulmonary disease. A pharmaceutical composition and a pharmaceutical product are also described. Methods of obtaining compounds of formula I are also described.EFFECT: novel compounds which can be used in therapy are obtained and described.20 cl, 334 ex, 15 tbl, 12 dwg

Pharmaceutical anti-tuberculosis combined composition // 2478389
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of medicine and deals with combined pharmaceutical composition, which possesses anti-tuberculosis action. Composition is made in form of solid drug form, which contains combination of levofloxacin, protionamide, pyrazinamide, ethambutol hydrochloride and pyridoxine hydrochloride ad active ingredient, and pharmaceutically acceptable auxiliary substances.EFFECT: composition is characterised by high therapeutic activity.10 cl, 2 tbl, 4 ex

Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme // 2474576
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, where Q is phenyl or pyridinyl; A is pyrazolyl or triazolyl, where each A is independently additionally unsubstituted or substituted with 1 or 2 substitutes represented by Ra, or A is formula (a); Va is C(R4), Vb is N or C(R5) and Vc is N; or Va is N, Vb is C(R5) and Vc is N or C(R6); R4 is hydrogen, R5 is hydrogen, C1-6alkyl, -ORb, -SRb, aryl, selected from phenyl, heteroaryl, selected from thienyl, or cycloalkyl, selected from cyclopropyl; R6 is hydrogen or aryl, selected from phenyl; R7 is hydrogen or C1-6alkyl; R3 is hydrogen, C1-3alkyl, -OH, -S(O)2R1, or heteroaryl, selected from tetrazolyl, where the heteroaryl is bonded to a nitrogen atom through a ring carbon atom; Rb, Rx, Ry, Rza, Rzb, Rw, Re, Rk, Rm, Rn, Rq and R1, in each case, are independently hydrogen, C1-3alkyl or C1-3haloalkyl; and Rf, in each case, is independently hydrogen, C1-3alkyl or -OH (the rest of the substitutes assume values given in the claim). The invention also relates to a pharmaceutical composition, having inhibiting action on DGAT-1, which contains a compound of formula (I), and a treatment method.EFFECT: compounds of formula (I) as DGAT-1 inhibitors are provided.16 cl, 9 dwg, 1 tbl, 127 ex

Piperidine/piperazine derivatives // 2470017
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to DGAT inhibitor of formula (I), its N-oxide, pharmaceutically acceptable salt and solvate, based on it pharmaceutical composition and its application for treatment of diseases, mediated by DGAT activity, such as obesity and diabetes. In general formula (I) A represents CH or N; X represents -C (=O)-C(=O); -O-C(=O)-; -NRX-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(O)-; -C(O)-Z1-; -NRx-C(O)-Z1-; -S(=O)p-; -NRX-C(=S) -; Y represents NRx-C(=O)-Z2-; -NRx-C(=O)-Z2-NRy-; -NR*-C(=O)-Z2-NRy-C(=O)-; -NRx-C(=O)-Z2-NRy-C(=O)-O-; -NRx-C(O)-Z2-O-; -NRx-C(=O)-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-O-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy-C(=O)-NRy-, -C(<))-Z2-; -C(=O)-NRx-Z2-; -C(=O)-NRx-Z2-O-; R1 represents C1-12alkyl, optionally substituted with cyano, C1-4alkyloxy, C1-4alkyloxy C1-4alkyloxy, C3-6cycloalkyl or aryl; C2-6alkenyl, C2-6alkinyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or HetC1-6alkyl, on condition that when Y represents -NRxC(=O)-Z2-; -NRx-C(=O)-Z2-NRy; -NRx-C(=O)-Z2-C(=O)-NRy-, -C(=O)Z2-; -NRx-C(=O)-Z2-NRy-C(=O)-NRy-; -C(=O)-NRx-Z2-; -C(=O)-NRx-O-Z2- or -C(=O)-NRx-Z2-NRy-; then R1 can also represent hydrogen; R2 represents R3; R3 represents phenyl, naphthalenyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle, containing 1 or 2 N atoms, where each of said cycles can optionally be substituted with, at least, one substituent, in particular, one-five substituents, said substituents represent halogen, C1-6alkyl, optionally substituted with hydroxy, polyhalogen C1-6alkyl, C1-6alkylthio, polyhalogen-C1-6alkyloxy, carboxyl, hydroxyl, C1-6alkylcarbonyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, nitro, R5R4N-C(=O)-; R5R4N-C1-6alkyl; HetC1-4alkyl, Het-C(=O)-C1-4alkyl, Het-C(=O)-; R8 represents hydrogen, halogen, C1-4alkyl, substituted with hydroxyl Values of other radicals are given in invention formula.EFFECT: obtaining pharmaceutical composition for treatment of diseases, mediated by DGAT activity, such as obesity and diabetes.31 cl, 5 tbl, 352 ex

Pharmaceutical composition for prevention and treatment of diabetes mellitus and obesity containing compound inhibiting activity of dipeptidylpeptidase-iv, and other antidiabetic agents or antiobesity agents as active ingredients // 2466727
FIELD: medicine.SUBSTANCE: invention refers to a pharmaceutical composition for prevention and treatment of diabetes mellitus and obesity containing as active ingredients a compound inhibiting activity of dipeptidylpeptidase-IV (DPP-IV), its pharmaceutically acceptable salt, its hydrate or its solvate, and one or more other antidiabetic agents or antiobesity agents.EFFECT: pharmaceutical composition shows excellent improvement of glucose tolerance and may be used in prevention and treatment of diabetes mellitus, obesity and similar diseases, effectively reducing blood glucose level and weight.25 cl, 8 dwg, 17 tbl, 32 ex

Pharmaceutical composition containing pyrazine derivative and method for using pyrazine derivative in combination // 2463051
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a pharmaceutical combination and to its use for treating an infection caused by influenza virus. The declared composition contains a pyrazine derivative of formula wherein R1 and R2 are identical or different, and each represents a hydrogen atom or a halogen atom; and R3 represent a hydrogen atom or a protective group for amino group or its salt, and, and a neuraminidase inhibitor. The neuraminidase inhibitor is specified in oseltamivir, zanamivir, peramivir or CS-8958.EFFECT: invention provides preparing the combination which shows strong antiviral activity, smaller side effects and applicable for treating influenza.12 cl, 8 tbl, 4 ex

3-pyridine carboxamide and 2-pyrazine carboxamide derivatives as hdl-cholesterol raising agents // 2454405
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I: , where A denotes CH or N; R1 is selected from a group consisting of: cycloalkyl which is unsubstituted or substituted with hydroxy, lower hydroxyalkyl or lower alkoxy, 1-hydroxy-2-indanyl, lower hydroxyalkyl, lower hydroxy haloalkyl, lower hydroxy alkoxyalkyl, CH2-CR9R10-cycloalkyl and -CR11R12- COOR13; R9 denotes hydrogen or lower alkyl; R10 denotes hydrogen, hydroxy or lower alkoxy; R11 and R12 independently denote hydrogen or lower alkyl; R13 denotes lower alkyl; R2 denotes hydrogen; or R1 and R2 together with the nitrogen atom with which they are bonded form a morpholinyl ring; R15 is selected from a group consisting of lower alkoxyalkyl, cycloalkyl and furanyl, substituted with halogen; R17 is selected from a group consisting of hydrogen, lower alkyl and lower haloalkyl; R4 and R8 independently denote hydrogen or halogen; R5 and R7 are independently selected from a group consisting of hydrogen, lower alkyl, lower alkoxy, halogen, lower haloalkyl, lower haloalkoxy and cyano; R6 is selected from a group consisting of hydrogen, lower alkoxy, halogen, lower haloalkyl, lower haloalkoxy and cyano; and pharmaceutically acceptable salts thereof. The invention also relates to use of said compounds to produce medicinal agents for treating and/or preventing diseases which can be cured by HDL-cholesterol raising agents and to a pharmaceutical composition based on said compounds.EFFECT: novel compounds which can be useful in treating diseases which can be treated with HDL-cholesterol raising agents are obtained and described.36 cl, 164 ex

2,3-substituted pyrazine sulphonamides as crth2 inhibitors // 2453540
FIELD: chemistry.SUBSTANCE: invention relates to 2,3-substituted pyrazine sulphonamides of formula (I), use thereof in treating allergic diseases, inflammatory dermatosis, immonological disorders and neurodegenerative disorders, as well as pharmaceutical compositions, having CRTH2 receptor inhibiting action and inhibiting chemoattractant receptor, homologous to the molecule expressed on T-helpers 2. in general formula . A is selected from a group consisting of , n denotes an integer independently selected from 0, 1, 2, 3 or 4; m equals 1 or 2; B is selected from a group consisting of phenyl or piperazinyl; R1 denotes hydrogen; R2 denotes phenyl, where R2 is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C1-C6)alkyl; R3 is selected from a group consisting of (C1-C6)alkyl, aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl and (C3-C8)heterocycloalkyl, where each of said (C1-C6)alkyl, aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl and (C3-C8)heterocycloalkyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C1-C6)alkyl, (C1-C6)alkoxy, heteroaryl, aryl, thioalkoxy and thioalkyl, or where said aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl or (C3-C8)heterocycloalkyl can be condensed with one or more aryl, heteroaryl, (C3-C8)cycloalkyl or (C3-C8)heterocycloalkyl groups and can be substituted with one or more substitutes selected from a group consisting of (C1-C6)alkyl, alkoxy, aryl, heteroaryl, carboxyl, cyano, halogen, hydroxy, amino, aminocarbonyl, nitro, sulphoxy, sulphonyl, sulphonamide and trihaloalkyl; R7 is selected from a group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, aryl, heteroaryl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, carboxyl, cyano, amino and hydroxy; aryl is selected from phenyl or naphthyl; and heteroaryl is selected from pyridyl, indolyl, 3H-indolyl, benzimidazolyl, quinolizinyl.EFFECT: high efficiency of using the compounds.4 cl, 10 dwg, 46 ex

Compounds and compositions as gpr119 activity modulators // 2443699
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof, in which Q is a divalent or trivalent radical selected from C6-10aryl and heteroaryl; where said aryl or heteroaryl in Q is optionally substituted up to 3 times with radicals independently selected from halogen, C1-6 alkyl, C1-6 alkyl substituted with halogen, C1-6 alkoxy group, C1-6 alkoxy group substituted with halogen, -C(O)R20 and -C(O)OR20; where R20 is selected from hydrogen and C1-6 alkyl; and where optionally, the carbon atom neighbouring W2 can be bonded through CR31 or O with a carbon atom of Q to form a 5-member ring condensed with A and Q rings; where R31 is selected from hydrogen and C1-6 alkyl; W1 and W2 are independently selected from CR21 and N; where R21 is selected from hydrogen and -C(O)OR25; where R25 denotes hydrogen; ring A can contain up to 2 carbon ring atoms substituted with a group selected from -C(O)-, -C(S)- and -C(=NOR30)- and can be partially unsaturated and contain up to 2 double bonds; where R30 denotes hydrogen ; L is selected from C1-6alkylene, C2-6alkenylene, -OC(O)(CH2)n-, -NR26(CH2)n- and -O(CH2)n-; where R26 is selected from hydrogen and C1-6 alkyl; where n is selected from 0, 1, 2, 3 and 4; q is selected from 0 and 1; t1, t2, t3 and t4 are each independently selected from 0, 1 and 2; R1 is selected from -X1S(O)0-2X2R6a, -X1S(O)0-2X2OR6a, -X1S(O)0-2X2C(O)R6a, -X1S(O)0-2X2C(O)OR6a, -X1S(O)0-2X2OC(O)R6a and -X1S(O)0-2NR6aR6b; where X1 is selected from a bond, O, NR7a and C1-4alkylene; where R7a is selected from hydrogen and C1-6alkyl; X2 is selected from a bond and C1-6alkylene; R6a is selected from hydrogen, cyanogroup, halogen, C1-6alkyl, C2-6alkenyl, C6-10aryl, heteroaryl, heterocycloalkyl and C3-8cycloalkyl; where said aryl, heteroaryl, cycloalkyl and heterocycloalkyl in R6a is optionally substituted with 1-3 radicals independently selected from hydroxy group, halogen, C1-6alkyl, C1-6alkyl substituted with a cyano group, C1-6alkoxy group and C6-10aryl-C1-4alkoxy group; and R6b is selected from hydrogen and C1-6alkyl; R3 is selected from hydrogen, halogen, hydroxy group, C1-6alkyl, C1-6alkyl substituted with halogen, C1-6alkyl substituted with a hydroxy group, C1-6alkoxy group, C1-6alkoxy group substituted with halogen, -C(O)R23 and -C(O)OR23; where R23 is selected from hydrogen and C1-6alkyl; R4 is selected from R8 and -C(O)OR8; where R8 is selected from C1-6alkyl, heteroaryl, C3-8cycloalkyl and heterocycloalkyl; where said heteroaryl, cycloalkyl or heterocycloalkyl in R8 is optionally substituted with 1-3 radicals independently selected from halogen, C1-6alkyl, C3-8cycloalkyl and C1-6alkyl substituted with halogen; R5 is selected from hydrogen, C1-6alkyl substituted with a hydroxy group, and a C1-6alkoxy group; heteroaryl denotes a monocyclic or condensed bicyclic aromatic ring complex containing 5-9 carbon atoms in the ring, where one or more ring members are heteroatoms selected from nitrogen, oxygen and sulphur, and heterocycloalkyl denotes a saturated monocyclic 4-6-member ring in which one or more said carbon atoms in the ring are substituted with a group selected from -O-, -S- and -NR-, where R denotes a bond, hydrogen or C1-6alkyl. The invention also relates to pharmaceutical compositions containing said compounds, and methods of using said compounds to treat or prevent diseases or disorders associated with GPR119 activity, such as obesity, type 1 diabetes, type 2 sugar diabetes, hyperlipidemia, type 1 autopathic diabetes, latent autoimmune diabetes in adults, type 2 early diabetes, child atypical diabetes, adult diabetes in children, malnutrition-associated diabetes and diabetes in pregnant women.EFFECT: improved properties of compounds.27 cl

Substituted methyl-amines, serotonin 5-ht6 receptor antagonists, methods of production and use // 2443697
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted methyl-amines of general formula 1, having serotonin 5-HT6 receptor antagonist properties. In formula 1 , W is naphthalene, indolysin or quinoline; R1 is hydrogen, fluorine, chlorine, methyl; R2 is hydrogen, fluorine, methyl, phenyl, thiophen-2-yl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 is methyl; or W is benzene, R3 assumes the value given above; R1 is 3-Cl, R2 is 3-piperazin-1-yl or 3-(4-methylpiperazin-1-yl); or R1 is hydrogen, R2 is phenyl or pyridyl; or R1 is hydrogen, fluorine, chlorine, methyl; R2 is 4-piperazin-1-yl or 4-(4-methylpiperazin-1-yl); or W is oxazole, R3 is optionally substituted methyl; R1 is chlorine or fluorine, R2 is methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is piperazin-1-yl, 4-methylpiperazin-1-yl, or R1 is chlorine, fluorine or methyl; R2 is furan-2-yl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is furan-2-yl, R3 is (tetrahydrofuran-2-yl)methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is thiophen-2-yl, R3 is 2-methoxyethyl, or R1 is chlorine or fluorine, R2 is thiophen-2-yl, R3 is methyl.EFFECT: compounds can be used to treat central nervous system (CNS) diseases, such as psychiatric disorders, schizophrenia, anxiety disorders, as well as for improving mental capacity, for treating obesity or for studying the molecular mechanism of inhibiting serotonin 5-HT6 receptors.15 cl, 27 dwg, 2 tbl, 25 ex
Coformulated antituberculous drug // 2430724
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to medicine, and concerns a coformulated drug exhibiting antituberculous action and representing a solid dosage form which contains as an active principle a formulation of rifampicin, isoniazid, pyrazinamide, and a zinc-containing compound, and pharmaceutically acceptable excipients. The zinc-containing compound is zinc salt, preferentially zinc sulphate.EFFECT: pharmaceutical composition under the invention is characterised by high efficacy and provides synergetic antimycobacterial activity when using the formulation of rifampicin, isoniasid, pyrazinamide and zinc sulphate as an antituberculous drug as compared with a formulation of standard antituberculous drugs.9 cl, 3 ex
urrain virus drug for pig or sheep family animals, and methods for murrain prevention and treatment in pig or sheep family animals // 2428187
FIELD: medicine, pharmaceutics.SUBSTANCE: group of inventions refers to animal breeding and veterinary science. There are declared an antiviral agent for animals, animal feedstuff, and a method for murrain treatment and prevention in animals. The antiviral agent and feedstuff contain 3-oxo-3,4-dihydro-2-pyrazinecarboxamide or its salt. The method for murrain prevention and treatment includes prescription of 3-oxo-3,4-dihydro-2-pyrazinecarboxamide or its salts.EFFECT: group of inventions is effective for murrain prevention and treatment in pig and sheep family animals.10 cl, 5 tbl, 6 ex

Heterocyclylamide-substituted thaizoles, pyrroles and thiophenes // 2425829
FIELD: chemistry.SUBSTANCE: compound of formula (I) has antiviral activity toward the human cytomegalovirus (HCMV) or some other representative of the Herpes virida group. In formula (I) , R1 is a group of formula , where * denotes the point of bonding to a carbonyl group, R3 denotes a pyridyl which can be substituted with a substitute independently selected from a group comprising C1-C6alkyl or a cyano group, R5 and R6 independently denote hydrogen, R2 denotes a phenyl which can be substituted with a substitute selected from a group comprising a trifluoromethoxy group, a difluoromethoxy group and a monofluoromethoxy group, A is a group of formula or , where * denotes the point of bonding to the carbonyl group, # denotes the point of bonding to the nitrogen atom of urea, R7 denotes C1-C6alkyl which can be substituted with a substitute selected from a group comprising C3-C6cycloalkyl, R8 and R9 independently denote hydrogen, halogen or C1-C6alkyl. The invention also relates to a method of producing a compound of formula (I) from a compound of formula , a method of producing a compound of formula (V), a medicinal agent containing the disclosed compound, use of the compound in preparing a medicinal agent and a method of fighting viral infections, among them human cytomegalovirus (HCMV) or some other representative of the Herpes viridae group.EFFECT: high antiviral activity.9 cl, 1 tbl, 39 ex

Novel piperazines as antimalarial agents // 2423358
FIELD: chemistry.SUBSTANCE: invention relates to compounds selected from a group comprising piperazine compounds of formula I: , where X is -CH2- or a bond; n equals 1; R1 is alkyl; cycloakyl; hydroxyethyl; benzo[1,3]dioxolyl; phenyl, which can be mono-substituted with a halide, alkyl, alkoxy, -CF3 or alkylcarbonyl; or phenyl which is di- or tri-substituted with substitutes independently selected from alkyl and halide; pyridyl which can be mono-substituted with a halide, alkyl or -CF3; furanyl which can be mono-substituted with methyl, hydroxymethyl or bromine, or furanyl which is disubstituted with an alkyl; thienyl which can be mono-substituted with methyl or chromium; pyrimidinyl; isoquinolinyl; benzhydryl; imidazolyl optionally mono-substituted with an alkyl; or thiazolyl; or X is -C(=O)- and R1 is hydrogen; R2 is indolyl, imidazolyl optionally mono-substituted with alkyl; phenyl which can be mono-substituted with a halide, alkyl, hydroxy or cyano, or phenyl which is disubstituted with a halide; pyridyl; benzothienyl; thiazolyl or thienyl; R3 is indolyl, pyridyl which can be mono-substituted with alkoxy, alkoxyalkoxy, NR31R32, morpholine, piperadine, oxopiperidinyl, oxopyrrolidinyl, pyridyl or phenyl; or phenyl which is mono-substituted with phenyl, pyridyl, alkyl, alkoxy, dialkylamino, morpholine, N-benzyl-N-alkylamino, (dialkylamino)alkoxy, phenylalkoxy or tetrahydroisoquinolinyl; or R3 denotes the group: , where Z is phenyl or pyridyl; R31 is 2-C1-C5alkoxyethyl, phenyl, pyridyl, phenylalkyl, hydroxyalkylcarbonyl, alkylcarbonyl, cycloalkylcarbonyl or phenylcarbonyl; R32 is hydrogen or methyl; R35 is alkyl, alkylcarbonyl, phenyl, pyridyl or pyrimidinyl; and R4 is phenyl-CH=CH-, where the phenyl can be mono-, di- or tri-substituted with substitutes independently selected from halide, alkyl, alkoxy and -CF3; or phenyl-CH2-CH2, where the phenyl is disubstituted with -CF3; and to optically pure enantiomers thereof, mixtures of enantiomers, such as, for example, racemates, optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and mesoforms, such as salts of such compounds. The invention also relates to a pharmaceutical composition, as well as to use of compounds in any of claims 1-4.EFFECT: obtaining novel biologically active compounds with antimalarial activity.8 cl, 138 ex, 1 tbl

New antagonists nk1 and nk2 // 2419609
FIELD: medicine, pharmaceutics.SUBSTANCE: there are described compounds of 3-cyanonaphthalene-1-carboxylic acid and perhydroxyalkylmethylpiperazine of formula , where R1 means C1-C4alkyl, R2 and R3 mean halogen, R4 is selected from the group consisting of 2-furanyl, 3-furanyl, 2-thiophen, 3-thiophen, phenyl, benzyl, 2-benzofuranyl, etc., R5 is selected from the group consisting of hydrogen and R6, R6 means a subgroup of general formula which are antagonists of tachykinin receptors. Also, there are described pharmaceutical compositions containing such compounds, and methods for making such compounds and intermediate products for making the compounds according to said methods.EFFECT: preparation of new compounds.

Some substituted amides, method of their obtaining and method of their application // 2418788
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula 2: and to its pharmaceutically acceptable salts and their mixtures, where values of R, M, Q, Z, W, D radicals are described in i.1 of the invention formula. Invention also relates to pharmaceutical compositions, which possess inhibiting activity with respect to Btk, based on formula 2 compounds.EFFECT: obtained are novel compounds and based on them pharmaceutical compositions which can be applied in medicine for treatment of patients with diseases associated with inhibiting Btk activity and/or B-cell activity.55 cl, 19 ex

Pharmacological composition with anti-tuberculosis action // 2412715
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to chemical-pharmaceutical industry and medicine, in particular to composition, which possesses bacteriostatic and bactericidal action and is intended for treatment of tuberculosis diseases. Pharmacological composition with anti-tuberculosis action contains active substances - anti-tuberculosis medications (ethambutol, isoniazid, rifampicin, pirazinamide) and as potentiating agent of synergetic action, enhancing impact of chemical preparations, stabilised nanoparticles of silver.EFFECT: invention possesses properties allowing to inhibit medication-resistant strains of tuberculosis mycobacteria.5 ex, 1 tbl

Pharmaceutical compositions, containing glucagon-like peptide (glp-1) // 2409349
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to the field of medicine. Composition containing microparticles of glucagons-like peptide 1 (GLP-1) in combination with diketopiperazine (DKP) is stable in vitro and in vivo. Composition may be used as pharmaceutical preparation to treat diseases or conditions, including, but not limited to, diabetes, cancer and obesity.EFFECT: invention provides for minimum risk in case of intrapulmonic administration.24 cl, 31 dwg, 20 ex

Pyrazine-2-carboxamide derivatives as mglur5 antagonists // 2407739
FIELD: chemistry.SUBSTANCE: invention relates to novel pyrazine-2-carboxamide derivatives of general formula , where R1 denote a 5- or 6-member ring, having a formula given in claim 1, R2 denotes H or C1-C7-alkyl; R3 denotes phenyl, pyridinyl or pyrimidinyl, possibly substituted with the following substitutes: Cl, F or Br; R4 denotes H, CI, F, Br, CF3 or C1-C7-alkyl; R5 denotes C1-C7-alkyl; as well as pharmaceutically acceptable salts thereof. Disclosed compounds are metabotropic glutamate receptor (mGLUR 5) antagonists. The invention also pertains to a medicinal agent based on disclosed compounds.EFFECT: improved method.17 cl, 23 ex

Crystalline modifications of n-α-(2,4,6-triisopropylphenylsulphonyl)-3-hydroxyamidino-(l)-phenylalanine-4-ethoxycarbonyl piperazide and/or salts thereof // 2388754
FIELD: chemistry.SUBSTANCE: invention relates to new crystalline modifications of N-α-(2,4,6-triisopropylphenylsulphonyl)-3-hydroxyamidino-(L)-phenylalanine-4-ethoxycarbonyl piperazide and/or its salts. Such crystalline modifications have high stability particularly at low hygroscopicity compared to known amorphous forms of the compound.EFFECT: invention relates to a method of obtaining such new crystalline modifications, to pharmaceutical compositions containing these new crystalline modifications and their use as an anti-tumour agent.26 cl, 7 tbl, 13 ex, 20 dwg
 
2550920.
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