(A61K31/498)

Antimicrobial composition for use in otorhinolaryngology // 2641607
FIELD: pharmacology.SUBSTANCE: antimicrobial composition for use in otorhinolaryngology containing hydroxymethylquinoxaline dioxide, polyvinylpyrrolidone and dexamethasone is described, with the following component ratio, wt %: polyvinylpyrrolidone 45.0-55.0, hydroxymethylquinoxaline dioxide solution 10 mg/ml 30.0-33.0, dexamethasone solution 4 mg/ml 12.0-25.0.EFFECT: antimicrobial composition has a prolonged action due to its high viscosity and adsorption capacity, providing long-term exposure to active substances and reducing the incidence of invasive procedures in otorhinolaryngology.2 ex
Derivatives of 1,4-dioxide of quinoxaline-2-carbonitrile inhibiting tumour cells growth // 2640304
FIELD: pharmacology.SUBSTANCE: invention relates to derivatives of 1,4-dioxide of quinoxaline-2-carbonitrile, corresponding to the formula: , as well as pharmaceutical compositions based on them.EFFECT: new compounds are obtained that have antiproliferative activity and can be used to inhibit the growth of tumour cells.9 cl, 2 tbl, 48 ex

Derivatives of azaindasole or diazaindasole type for pain treatment // 2640046
FIELD: pharmacology.SUBSTANCE: invention relates application of a compound of formula for treatment or prevention of pain associated with at least one Trk protein. The radicals and symbols in formula (I) have the definitions indicated in the claims. The invention also relates to a pharmaceutical composition comprising a compound of formula (I) as an active substance.EFFECT: compound application efficiency increase.15 cl, 6 dwg, 1 tbl, 35 ex
Anti-cancer benzopyrazines acting through fgfr-kinases inhibition // 2639863
FIELD: pharmacology.SUBSTANCE: invention relates to benzopyrazine derivatives of the general formula (I) , including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein W is -N(R3)-; R2 is C1-4alkoxy; Y is -CR18=N-OR19 or -E-D; E is bond, C2-4alkynediyl, -CO-(CR22R23)s-, -NR22-(CR22R23)s-, -(CR22R23)s-CO-NR22-(CR22R23)s- or -(CR22R23)s-NR22-CO-(CR22R23)s-; D is phenyl, 3-6 membered cycloalkyl or 5-9 membered mono- or bicyclic saturated, partially saturated or aromatic heterocyclyl containing 1-4 heteroatoms selected from N, O or S, wherein the said phenyl, cycloalkyl and heterocyclyl can each optionally being substituted with 1-2 R1-groups; with the exception of the compounds indicated in the formula; R1 is halogen, cyano, C1-6alkyl, C1-6alkoxy, -C(=O)-O-C1-6alkyl, hydroxyC1-6alkyl, -NR4R5 , C1-6alkyl substituted by -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by -NR4R5, -C(=O)-NR4R5, R6, C1-6alkyl substituted by R6, -C(=O)-R6; R3 is halogenC1-6alkyl, optionally substituted by -O-C(=O)-C1-6alkyl, hydroxyC1-6alkyl, hydroxyhalogenC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group or -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by R9, C2-6alkynyl substituted with R9, C1-6alkyl substituted by -NR10R11, C1-6alkyl substituted by -O-C(=O)-NR10R11; R4 and R5 are hydrogen, C1-6alkyl, C1-6alkyl substituted by -NR14R15, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group, -C(=O)-NR14R15, -C(=O)-O-C1-6alkyl, -C(=O)-R13; R6 is a 6-membered saturated or aromatic monocyclic heterocyclyl having 1 to 2 heteroatoms selected from N or O; the said heterocyclyl is optionally substituted by 1 substituent selected from C1-6alkyl, halogen, C1-6alkyl-O-C(=O)-; R9 is C3cycloalkyl or 3-6 membered monocyclic saturated, partially saturated or aromatic heterocyclyl containing 1-2 heteroatoms selected from N or O, the said heterocyclyl is optionally substituted by 1 substituent selected from =O, hydroxyC1-4alkyl, C1-4alkyl-C(=O)-, C1-4alkyl substituted by -NR14R15, C1-4alkoxy; R10 and R11 are hydrogen, C1-6alkyl, halogen C1-6alkyl, hydroxyC1-6alkyl or C1-6alkyl substituted by carboxyl; R13 is a saturated 6-membered monocyclic heterocyclyl containing 1-2 heteroatoms selected from N and O; R14 and R15 are hydrogen or C1-4alkyl; R18 and R19 are C1-6alkyl; R22 and R23 are hydrogen; n=2; s=0, 1, 2, or 3. Invention also relates to a pharmaceutical composition and a product based thereon, the use of a compound of formula (I) and a method of prevention or treatment of conditions mediated by FGFR kinase.EFFECT: new derivatives of benzopyrazine, useful for cancer treatment.28 cl, 4 tbl, 54 ex
Spirocyclic pyrrolopyrazine(piperidine)amides as ionic channels modulators // 2634900
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula or its pharmaceutically acceptable salts. In formula I R1 is C1-C8alkyl, C1-C8hydroxyalkyl, CO2R8, or two R1 together form an oxo group, or a 3- to 7-membered fused cycloalkyl ring; R2 is halogen, C1-C8haloalkyl, C1-C8hydroxyhaloalkyl, CN, SO2CH3, CO2R8, CON(R8)2 or COR8; R3 is H, C1-C8alkyl, C3-C8cycloalkyl, CO2R8, COR8, CON(R8)2, CF3, CH2CF3, CH2CHF2, CH2-phenyl, CH2-CN, CH2-CO2R8, CH2-CON(R8)2, CH2-C3-C8cycloalkyl, C1-C8alkoxy-C1-C8alkyl or C1-C8hydroxyalkyl; R4 is C1-C8alkyl or halogen; A is phenyl substituted by 1 to 2 substituents; or 5-membered heteroaryl, wherein the three ring atoms are N, substituted by fluorophenyl-C1-C8alkyl; or 6-membered heteroaryl, wherein one ring atom is N substituted by 1 to 2 substituents; or a 9-10 membered bicyclic heteroaryl, wherein 2 to 3 ring atoms are independently heteroatoms selected from N, O, optionally substituted by 1 to 2 substituents; m is an integer from 1 to 2; n is an integer from 1 to 2; and o is an integer from 0 to 1; the values of the remaining substituents are indicated in the claims. The invention also relates to pharmaceutical compositions, to methods for inhibition of a potential-dependent sodium ion channel, to methods of treatment, to individual compounds.EFFECT: new compounds having inhibitory activity with respect to the potential-dependent sodium ion channel are obtained.42 cl, 3 tbl, 752 ex

New compounds - neurokinin 1 receptor antagonizer // 2631319
FIELD: pharmacology.SUBSTANCE: in formula n=1 or 2; R1 and R2, independently of each other, are hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or halogen; R3 is hydrogen or C1-4 alkyl optionally substituted with hydroxy; R4 is hydrogen or oxo; R5 and R6, independently of one another, are hydrogen, C(=O)OR7, C(=O)NR8R9, C1-4 alkyl, wherein the said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-member heterocyclic ring with 1-4 heteroatoms selected from O and N, wherein the said 5- or 6-member heterocyclic ring is optionally substituted with C1-4 alkyl or C(=O)R7; or R5 and R6 together with the carbon atom to which they are attached form =CH2 or 5- or 6-member heterocycloalkyl with 1-4 heteroatoms selected from O and N, wherein the said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are, independently of each other, hydrogen or C1-4 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a 5- or 6-membered heterocyclic ring with 1-4 heteroatoms selected from O and N. The invention also relates to a pharmaceutical composition, a method for prevention, treatment or alleviation of the severity of conditions accompanied by skin pruritus, application of the said compounds in the manufacture of a medicament for prevention, treatment or alleviation of the said diseases, and to intermediates of general formula wherein R10 is selected from the group consisting of hydrogen and C(O)OR14; R11 is selected from the group consisting of hydrogen and oxo; R12 and R13 are independently selected from the group consisting of hydrogen, C1-C4 alkyl, allyl and C(O)O(C1-C4alkyl); R14 is selected from the group consisting of C1-C4-alkyl; n is 1 or 2.EFFECT: possibility to use the compounds for prevention, treatment or alleviation of conditions accompanied by skin pruritus.27 cl, 3 dwg, 1 tbl, 122 ex
eans for treatment of animals with postoperative and bitten wounds // 2630984
FIELD: veterinary medicine.SUBSTANCE: means for animals treatment consists of dioxidine, xeroform, anestesin, dimedrol and starch. Dioksidin - 7.0 wt % and xeroform - 7.0 wt % are used as antimicrobial agents, anesthesin - 3.0 wt % is used as an analgesic agent, dimedrol - 3.0 wt % is used as an antipruritic agent, and starch is used as a coating and drying agent, comprising the rest to 100 wt %.EFFECT: invention shows antimicrobial action, promotes damaged tissues regeneration due to drying, astringent, anesthetic and antiallergic properties and allows effective treatment of postoperative and fresh bitten wounds in animals.4 tbl, 2 ex

Bicyclic piperazine compounds // 2628616
FIELD: pharmacology.SUBSTANCE: invention relates to new bicyclic piperazine compounds of formula , as well as to pharmaceutically acceptable salts thereof.EFFECT: new compounds of formula I have been obtained that have modulating activity against Bruton tyrosine kinase, that can be used to prepare pharmaceutical compositions, as well as for treatment of immune disorders such as inflammation mediated by kinase.17 cl, 15 dwg, 2 tbl, 131 ex
Piperazino[1,2-a]indole-1-ones and [1,4] diazeptino[1,2-a]indole-1-one // 2628126
FIELD: medicine.SUBSTANCE: invention relates to application of compounds of general formula I .EFFECT: new compounds, as well as pharmaceutical compositions based thereon, are obtained, that can be used to treat schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorder, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down's syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and violations resulting from radiation therapy, chronic stress or abuse of neuroactive drugs, such as alcohol, opiates, methamphetamine, phencyclidine or cocaine.11 cl, 1 tbl, 46 ex
Tricyclic nitrogen-containing derivatives of imidazo[4,5-c]pyridine, having inhibiting activity in response to hystamine 4 receptor (hh4r) // 2628074
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of formula 1 , or to a racemate, isomer, or pharmaceutically acceptable salt thereof, wherein X1 and X2 are C; each of X3 and X4 is independently C or N, provided that one of X3 and X4 is N; R1 is a saturated 4-9 member mono- or bi-heterocyclyl containing 1-2 heteroatoms (where the heteroatoms are N), where R1 is unsubstituted or substituted by 1 to 3 substituents selected from -NR6R7 and R8; or R1 is selected from -NR6R7 and R8; R2, R3, R4 and R5 may be the same or different; and each is independently selected from -H; -C1-C6alkyl; -C1-C6haloalkyl; -C1 -C6perhaloalkyl; -halogen (-F, -Cl, -Br, -I); -CN; -C1-C6talkoxy; -C1-C6haloalkoxy; -C1-C6perhaloalkoxy; C2alkenyl; -C2-C3alkynyl; -amino; -OH; -nitro (-NO2); -C6-C1aryl; and furan; provided that, when X3 is N, R4 is absent; and when X4 is N, R5 is absent, each of Y1, Y2, Y3, Y4 and Y5 is independently C or a heteroatom (preferably a heteroatom independently selected from N, O and S), provided that at least two of Y1, Y2, Y3, Y4 and Y5 are heteroatoms independently selected from N and O; each of Y2 and Y3 can be independently substituted by R9; Y4 may be substituted with -H or -C1-C6alkyl; each of R6 and R7 is independently selected from -H; -C1-C6alkyl; and -carboxyl (-COOH); R8 is -C1-C6alkyl or -C3cycloalkyl; and R9 is selected from -H; -C1-C6alkyl; and -C3cycloalkyl; wherein the alkyl and heterocyclyl may be independently unsubstituted or substituted by one or more substituents (for example, 1 to 3 substituents) selected from the group consisting of -C1-C4alkyl, -C1-C4alkoxy and -OH. The invention also relates to particular compounds and a pharmaceutical composition based on the said compounds.EFFECT: new heterocyclic compounds useful for human histamine receptor 4 inhibition are obtained.13 cl, 13 tbl, 144 ex
Compound as wnt signal inhibitor, its compositions and application // 2627712
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where 0 or 1 of X1-X4 can be N; Y1, Y2 and Y3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein each of C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl and 6-member heteroaryl may be optionally substituted with one R4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5, C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with 1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 and X8, is: or The invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 cl
Starch-free soft chewing gums // 2627420
FIELD: pharmacology.SUBSTANCE: group of inventions refers to a soft chewing gum, which comprises: (a) a pharmaceutically effective amount of at least one active ingredient; (b) a flavoring agent of animal origin; (c) at least 10 wt % of a disintegrating agent in the final composition, which is selected from the group consisting of i) carmellose calcium, ii) directly compressible mannitol, and iii) a mixture or combination of croscarmellose sodium and directly compressible mannitol; (d) at least 10 wt % of a wetting agent in the final composition; (e) a binding agent; (f) an antioxidant; (g) optionally, a preservative; and (h) water; where the soft chewing gum contains less than about 2 wt % of each of polyethylene glycol (PEG), propylene glycol, starch, soy products and wax. Also, the group of inventions refers to a method for the said soft chewing gum production.EFFECT: short time of soft chewing gum decomposition, retained even after prolonged storage at elevated temperature.11 cl, 1 ex, 4 tbl, 3 dwg
2-aryl-2,4-dihydroxy-2,5-dihydro-3-heteryl-5-oxo-1h-pyrrol-1-yl-4-methyl benzenesulphanolamides with analgesic activity // 2626650
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the new methylbenzenesulfonamide derivatives of the formula (I) , where X=O, Ar=4-Me-C6H4 (a); X=O, Ar=4-Cl-C6H4 (b); X=NH, Ar=4-Cl-C6H4 (c).EFFECT: new compounds having analgesic activity were obtained.2 tbl, 4 ex

New pyrazole derivative // 2625790
FIELD: pharmacology.SUBSTANCE: in particular, invention relates to a compound represented by the following general formula (I): [wherein Ar1 is 2-methoxy-4-(2-pyridylmethoxy)phenyl, etc. and Ar2 is 1H-indole-6-yl group, etc.] or to salt thereof.EFFECT: increased efficiency of treatment.19 cl, 4 dwg, 1 tbl, 112 ex
Hydinine derivatives as inheritors of ferment pde10a // 2624440
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to heterocyclic compounds selected from 7-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)ethyl]-2,3-dihydro[1,4]dioxino[2,3-g]quinoline and 6-[2-(5,8-dimethyl[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-ethyl]-[1,3]dioxolo[4,5-g]quinoline and the pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions on the basis of one of these compounds and the use of these compounds.EFFECT: obtained new heterocyclic compounds useful in the treatment of a neurodegenerative or psychiatric disorder.10 cl, 1 tbl, 2 ex

ethod and improved pharmaceutical composition for acceleration of pde-5 inhibitor transdermal delivery // 2618462
FIELD: medicine, pharmacy.SUBSTANCE: invention refers to medicine and is a transdermal pharmaceutical composition in the form of gel or patch that contains vardenafil, enhancer selected from the group consisting of sodium lauroamphoacetate, quaternium-60, izostearamidopropil morpholine lactate and combinations thereof, and a pharmaceutically acceptable excipient. The enhancer accelerates the kinetics of transdermal absorption of vardenafil. Vardenafil and enhancer are present in the composition in a ratio from 20:1 to 2:1 by weight. The invention also relates to the method of acceleration of the transdermal delivery of vardenafil.EFFECT: invention provides transdermal delivery acceleration due to the vardenafil enhancer.8 cl, 2 ex, 2 dwg

Pyridone and aza-pyridone compounds and methods of use // 2617405
FIELD: chemistry.SUBSTANCE: invention relates to a compound selected from formula I, or its stereoisomers, or pharmaceutically acceptable salts thereof, where R1 is optionally substituted C1-C3 alkyl; R2, R3 and R4 are independently selected from H, F, Cl; R5 is selected from (i) optionally substituted C6-C20 aryl, selected from phenyl; (ii) optionally substituted C5-C20 heteroaryl, selected from pyrazolyl, pyridinyl, pyrimidinyl, tetrahydroisoquinolinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazinyl, 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazinyl, 4,6,7-trihydropyrazolo[3,2-c][1,4]oxazinyl, 5,6,7,8-tetrahydro-1,6-naphthyridinyl, 2,3-dihydro-1H-isoindolyl, 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridinyl; (iii) optionally substituted -(C6-C20 aryl)-(C3-C20 heterocyclyl), where heterocyclyl is selected from azetidinyl, piperidinyl, morpholino, piperazinyl; (iv) optionally substituted -(C5-C20 heteroaryl)-(C3-C20 heterocyclyl), where heteroaryl is selected from pyridinyl and pyridazinyl and heterocyclyl is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 1,4-diazepanyl, 2,6-diazaspiro[3.3]heptanyl, 7,9-diazabicyclo[3.3.1]nonanyl, hexahydropyrrolo[3,4-c]pyrrolyl, morpholino; (v) optionally substituted -(C5-C20 heteroaryl)-(C1-C6 alkyl), where heteroaryl is selected from pirazolyl and pyridinyl; or (vi) optionally substituted -(C5-C20 heteroaryl)-C(=O)-(C3-C20 heterocyclyl), selected from (pyridinyl)-C(=O)-(morpholino); R6 represents H or C1-C3 alkyl; Y1 and Y2 are independently selected from CR6 and N; where C1-C3 alkyl, C3-C20 heterocyclyl, C6-C20 aryl and C5-C20 heteroaryl optionally substituted with one to three groups, independently selected from D, F, Cl, Br, I, -CH3, -CH2CH3, -CH2CH(CH3)2, -CH2OH, -CH2CH2OH, -C(CH3)2OH, -CH2F, -OC(O)CH3, -COCH3, -NHCH3, -N(CH3)2, =O, -OH, -OCH3, -OCH2CH2N(CH3)2, -OP(O)(OH)2, -CH2OCH3, cyclopropyl, azetidinyl, 1-(methylazetidin-3-yl)oxy, N-methyl-N-oxetan-3-ylamino, azetidin-1-ylmethyl, oxetanyl and morpholino; where group (a), formed Z1, Z2, Z3, Z4, Z5, X and NC(O), forms structure, given in claim, and wherein wavy line indicates bonding point. Invention relates to a pharmaceutical composition for treating a condition, mediated by Bruton's tyrosine kinase, containing a compound of formula (I) and a pharmaceutically acceptable carrier, lubricant, a diluent or filler. Compounds of formula (I) are intended for use as a drug for treating cancer, mediated by Bruton's tyrosine kinase.EFFECT: pyridone and aza-pyridone compounds for treating disorders mediated by Bruton's tyrosine kinase (Btk).20 cl, 9 dwg, 4 tbl, 907 ex (а)
Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as inhibitors // 2617401
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula (I) (I), where: R1 and R2, which can be identical or different, independently selected from a group consisting of: - (C1-C6)alkyl, optionally substituted (C3-C7)cycloalkyl; - (C1-C6)halogenalkyl; - (C3-C7)cycloalkyl and - (C3-C7)heterocycloalkyl, containing heteroatom O; R3 represents hydrogen, (C1-C6)alkyl or (C1-C3)alkylthio(C1-C6)alkyl; A is a partially unsaturated or unsaturated bicyclic ring system consisting of two condensed monocyclic ring systems B and C, presented in cl. 1 of formula, where ring C is a monocyclic aryl or monocyclic heteroaryl ring system, ring B is a 5- or 6-member heterocycloalkyl group, zero of Y groups is bonded to ring C, n of groups Y is bonded to ring B, and n is an integer from 1 to 3; and where ring B and C optionally contains additional heteroatoms in amount of 1 to 4, selected from N, O or S; p is an integer from 0 to 3; Y denotes oxo group; K is selected from a group consisting of: - (C1-C6)alkyl, optionally substituted with one (C3-C7)cycloalkyl group; - (C3-C6)heterocycloalkyl(C1-C4)alkyl containing 1 or 2 heteroatoms selected from N or O; - (C3-C6)heterocycloalkyl containing 1 or 2 heteroatoms selected from N or O, optionally substituted with one or more (C1-C6)alkyl group; - (C1-C4)halogenalkyl; - OR4, where R4 selected from a group consisting of: - H; - (C1-C6)alkyl, optionally substituted (C3-C7)cycloalkyl or heteroaryl; - halogen atoms; - CN; - NO2; - NR5R6, where R5 and R6, which can be identical or different, independently selected from a group consisting of: - H; - OH; - (C1-C4)alkyl-NR7R8, where R7 and R8, which can be identical or different, independently selected from a group consisting of: H; (C1-C6)alkyl, possibly substituted (C1-C6)alkoxyl; and (C1-C6)alkyl-NR9R10, where R9 and R10, which can be identical or different, represent H or (C1-C6)alkyl; or they form together with a nitrogen atom to which they are bonded, (C3-C6)heterocycloalkyl ring containing 1 or 2 heteroatoms, selected from N, O or S, optionally substituted (C1-C6)alkyl or (C1-C6)alkylcarbonyl group; -(C1-C6)alkyl, optionally substituted with (C1-C6)alkoxyl or heteroaryl, (C3-C6)heterocycloalkylcarbonyl containing 1 or 2 heteroatoms selected from N or O, heteroarylcarbonyl, wherein all of them may further be substituted with one or more (C1-C6)alkyl, (C1-C6)halogenalkyl or (C1-C6)alkoxyl groups, which are identical or different and are selected independently; - SO2R11, where R11 represents (C1-C6)alkyl; - C(O)R12, where R12 is (C1-C6)alkyl, optionally substituted with (C1-C6)alkoxyl; - (C1-C4)alkyl-NR13R14, where R13 and R14, which can be identical or different, are independently selected from a group consisting of groups: - SO2(C1-C6)alkyl, H, (C1-C6)alkyl and (C3-C7)heterocycloalkyl(C1-C4)alkyl containing 1 or 2 heteroatoms selected from N or O; and - SO2NR15R16, where R15 and R16, which can be identical or different, independently represent H or (C1-C6)alkyl; where groups with R4 at R16 have similar or different values in each case, if they are present in more than one group; and where heteroaryl is a mono- or bicyclic ring system with 5–10 ring atoms, containing 1 or 2 heteroatoms selected from N, O or S; or its pyridine-N-oxides, pharmaceutically acceptable salts or solvates. As well as to methods of producing such compounds, compositions containing them and their therapeutic application as inhibitors of phosphodiesterase 4 (PDE4) enzyme.EFFECT: disclosed are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as inhibitors.16 cl, 16 tbl, 52 ex

Pharmaceutical composition based on β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-n,n'-dioxide and method for obtaining thereof // 2614736
FIELD: chemistry.SUBSTANCE: group of inventions relates to medicine. Disclosed a pharmaceutical composition containing crystalline modification of β2,3-bis-(hydroxymethyl)quinoxaline-N,N'-dioxide, characterised by a number of diffraction peaks (d, Ǻ) and their intensity (Irel., %), and silver nanoparticles. Disclosed production process. Antimicrobial, antibacterial and bactericidal pharmaceutical composition, comprising crystalline β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-N,N'-dioxide, characterised by a number of diffraction peaks (d, Ǻ) and their intensity (Irel., %), and silver nanoparticles, constitutes a light fluffy powder of yellowish to light-brown colour, non-odorous.EFFECT: disclosed the said pharmaceutical composition and method for obtaining thereof.7 cl, 6 dwg, 4 ex

Pharmaceutical composition for treating, preventing or relieving movement disorders and its application // 2611376
FIELD: medicine.SUBSTANCE: group of inventions relates to treatment of movement disorders. Application of composition is proposed, which contains zolmitriptan or its pharmaceutically acceptable salt and 5-HT-receptor agonist buspirone or its pharmaceutically acceptable salt for treating, preventing or relieving movement disorders and use of set containing pharmaceutical composition of zolmitriptan or its salt and pharmaceutical composition of 5-HT-receptor agonist buspirone or its salt, at same prescription.EFFECT: technical result is increased efficiency of combined treatment in part of manifestations of delayed dyskinesia and relief of symptoms of Parkinson's disease in its model in rats.13 cl, 4 dwg, 9 ex
Pharmaceutical preparation for local application, containing b220 // 2608909
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical composition for local application for preventing or treating herpes virus infection in humans. Above composition contains 2,3-dimethyl-6-(N,N-dimethylaminoethyl)-6H-indolo-(2,3-b)quinoxaline (B-220) or its pharmaceutically acceptable salt in amount of 0.1–10 wt/wt% in pharmaceutically acceptable carrier.EFFECT: invention provides evident therapeutic effect of herpetic infection.5 cl, 1 ex

Quinoline and quinoxaline derivatives effective as cysteinyl-leukotriene antagonists // 2605929
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a heterocyclic compound of formula (IA) or to a pharmaceutically acceptable salt thereof, where in each case R1 and R3 are independently selected from a group comprising hydrogen, halogen, -OH, -C1-2alkyl, -O-C1-2alkyl, -O-C1halogenalkoxy, -N(C1alkyl)2; R2 represents hydrogen; W represents a group selected from -CH= or -N=; X represents a group selected from -CH=CH- or -N=CH-, where nitrogen from -N=CH- is directly bonded with ring 'a'; Y represents a group selected from -CH=CH- or -C≡C-; Z denotes a bond or group selected from -(CH2)n- and -CH=CH-; A is a group selected from -OR, -O(CH2)nphenyl, -O(CH2)nthiophene; P is selected from a group comprising -O-; Q is a group selected from -COOH; where R is selected from a group comprising hydrogen, -C1-6alkyl, -C3-6cycloalkyl, -C1alkyl (C3-6cycloalkyl), -C3-6alkenyl and -C3-6alkynyl; 'n' in each case represents an integer, selected from 1, 2 or 3; 'm' in each case represents an integer, selected from 0-3, inclusive. Invention also relates to a compound of formula (Id), where radicals are described in patent claim.EFFECT: obtaining novel heterocyclic compounds effective as antagonists of cysteinyl-leukotriene.9 cl, 1 dwg, 2 tbl, 67 ex

Pharmaceutical composition for treating addiction in humans // 2605283
FIELD: medicine.SUBSTANCE: invention relates to medicine and is presented by pharmaceutical composition for treating addiction in humans. Composition contains two active agents: compound with antagonistic activity on 5-HT2 serotonin receptors, selected from cyproheptadine; and compound with antagonistic activity on alpha-1-noradrenergic receptors, selected from prazosin, alfuzosin, terazosin, tamsulosin, silodosin and doxazosin. Invention also relates to combined pharmaceutical product for simultaneous introduction of said agents for treating addiction in humans.EFFECT: technical result consists in reduction of risk of side effects, simultaneous antagonist activity in relation to alpha-1-noradrenergic receptors and 5-HT2 serotonin receptors, maintaining efficiency, unexpected synergism between agents and stable effect in time.12 cl, 4 ex, 7 tbl

Azaindazole or diazaindazole derivatives as medicine // 2600976
FIELD: chemistry.SUBSTANCE: invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt thereof, in which radicals and symbols assume values given in patent claim. Compound of formula (I) is a kinase inhibitor, such as ALK Abl and/or c-Src.EFFECT: invention also relates to its use as a drug for treating cancer, inflammation and neurodegenerative diseases, such as Alzheimer's disease, to its use as an inhibitor of said kinases, to a pharmaceutical composition containing said compound, and to methods of its production.16 cl, 20 tbl, 35 ex

Imidazopyrazines // 2600327
FIELD: pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula I and pharmaceutically acceptable salts thereof, in which values for groups R1, R2, R3, R4 and X are defined in patent claim. Invention also relates to pharmaceutical compositions, having activity of inhibitor of Fms-like tyrosine 3 (FLT3) containing said compounds and pharmaceutically acceptable salts thereof.EFFECT: invention relates to use of said compounds and pharmaceutical compositions for treating, controlling or relieving symptoms of AML (acute myeloid leukaemia).35 cl, 93 ex, 1 tbl

Extended-release formulation for reducing the frequency of urination and method of use thereof // 2599017
FIELD: medicine.SUBSTANCE: group of inventions relates to methods and compositions for inhibiting the contraction of muscles and, in particular, to methods and compositions for inhibiting the contraction of smooth muscles of the urinary bladder. Method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising acetaminophen and one or more additional active ingredients selected from a group, comprising of α-blockers and 5α-reductase inhibitors. Group of inventions also relates to pharmaceutical compositions containing acetaminophen and one or more αblocker or acetaminophen and one or more 5α-reductase inhibitor, in which acetaminophen is made for prolonged release, and one or more αblockers and one or more 5α-reductase inhibitors - for immediate release.EFFECT: this allows to reduce a rate of urination due to inhibition of smooth muscle contraction of the urinary bladder.36 cl, 9 tbl, 8 ex, 2 dwg

2-arylimidazo[1,2-b]pyridazine,2-phenylimidazo[1,2-a]pyridine and 2-phenylimidazo[1,2-a]pyrazine derivatives // 2598385
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula or a pharmaceutically acceptable salt thereof. Disclosed compounds have inhibitory activity on Hedgehog pathway activation and can be effective in treating pancreatic cancer or prostate cancer. In formula R1 is a pyridyl, optionally substituted in position where substitution is possible with one or more R8; R2 is CN, C1-C6 alkyl, C3-C-8 cycloalkyl, phenyl, 5-6-member heteroaryl, where 1-2 members are heteroatoms selected from N and O, 4-5-member heterocyclyl, where 1 member is a heteroatom selected from a group consisting of N, where each alkyl, cycloalkyl, phenyl or heterocyclyl group is optionally substituted in position where substitution is possible with one or more R10; R3 is halogen, C1-C-6 alkyl, C1-C6 haloalkyl or C3-C8 cycloalkyl; A is a bond,-N(R7)-, -N(R7)C(O)-, N(R7)C(O)N(R7)-, -C(O)O-, -S(O)2N(R7)- or-N(R7)S(O)2-; each R5 is independently hydrogen, C1-C6 alkyl; each Z is independently CR6; each R6 is independently hydrogen, halogen. Invention also relates to a pharmaceutical composition containing disclosed compound, a method of inhibiting Hedgehog signaling pathway and use of compounds.EFFECT: technical result is obtaining novel compounds having inhibitory activity on Hedgehog pathway activation.19 cl, 3 dwg, 5 tbl, 706 ex

Phenicol antibacterial agents // 2593204
FIELD: chemistry. SUBSTANCE: invention relates to a compound of formula I or its pharmaceutically acceptable salts, where grouping Het denotes a pyridinyl or thiazolyl; each of R1 and R2 represents H; each R3 and R4 independently denotes H, -C1-8alkyl or R3 and R4, taken together, form C3-6cycloalkyl; W represents -H, -PO(OH)2 or -CH2OPO(OH)2; each of X and Y denotes chlorine or each of X and Y denotes fluorine, and Z is H. EFFECT: compounds of formula I are used in method of controlling and treating infections in livestock, which involves administering animal with therapeutically effective amount of compound of formula I or its pharmaceutically acceptable salt. 8 cl, 3 tbl, 161 ex

Quinoxalines and azaquinoxalines as crth2 receptor modulators // 2589709
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (IC) and pharmaceutically acceptable salts thereof. Disclosed compounds have properties of CRTH2 receptor modulators. In formula (IC) R1 represents -C(O)-N(R6a)(R6b); I) R6a is H, and R6b represents a) -Q-RAH, where RAH is phenyl, and where RAH is unsubstituted or substituted with one fragment R8, selected from group consisting of fluorine and -CN; Q is selected from group consisting of (i) link; (ii) , where Re denotes H, and R(f) is H or methyl; b) -Q-RHC, where RHC is C5-C6 cycloalkyl, where said C5-C6 cycloalkyl forms condensed cycle with benzene ring and where RHC is unsubstituted or substituted with 1-2 fragments of R12, independently selected from group consisting of halogen and -CN; II) or R6a and R6b together with N atom to which they are bonded form R6h, where R6h is pyrrolidinyl, piperidinyl or piperazinyl, where R6h is substituted with -Z-RCY, Z is bond and RCY is unsubstituted phenyl or phenyl, substituted with 1-2 fragments of R10, selected from group consisting of halogen and -CN; R6H optionally substituted with 1-2 fragments in R9, where each fragment R9 is independently C1-C3 alkyl, halogen or -CN, and R2 is unsubstituted phenyl. Invention also relates to pharmaceutical composition for treating asthma or allergic rhinitis and method of treating asthma or allergic rhinitis.EFFECT: technical result is obtaining novel compounds which can be used to treat asthma or allergic rhinitis.10 cl, 2 tbl, 44 ex

ethod of preventing or treating skin tumour // 2587041
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and provides methods for preventing formation of skin tumors or inhibiting progression of existing skin tumors caused by UV irradiation, comprising applying a composition containing brimonidine or brimonidine tartrate. Also described is a method of protecting skin and lips from damaging effects of UV radiation, comprising applying a composition containing brimonidine or brimonidine tartrate.EFFECT: group of inventions provides noninvasive means to effectively prevent formation of, or reduce spread of skin cancer caused by UV radiation.13 cl, 4 dwg, 5 ex, 12 tbl

Derivatives of 6,7-dihydro-3h-oxazolo[3,4-α]pyrazine-5,8-dione // 2581831
FIELD: chemistry.SUBSTANCE: invention relates to the derivatives of 6,7-dihydro-3H-oxazolo[3,4-α]pyrazine-5,8-dione of formula (I), where R1 represents an indole group, R2 represents methylene-3,4-dioxyphenyl group, R3 represents hydrogen, halogen, C1-6 halogenalkyl, C1-3 heteroalkyl or C1-3 alkyl and R4 represents hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkinyl, C1-6 halogenalkyl, C3-8 cycloalkyl or C3-8-cycloalkyl-C1-3-alkyl, and their pharmaceutically acceptable salts. The invention also relates to the pharmaceutical composition, containing the compounds of formula , and to a method for obtaining the formula compound.EFFECT: improvement of the properties of derivatives.8 cl, 3 dwg, 2 ex

Compounds applicable for treating aids // 2575845
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to using a compound of formula or any of its pharmaceutically acceptable salts, wherein means an aromatic ring, wherein V represents C or N, and when V represents N, V is found in meta- or para-position to Z, R independently represents a hydrogen atom, halogen atom or group specified in -CN group, hydroxyl group, -COOR1 group, (C1-C3)fluoralkyl group, (C1-C3)fluoralkoxy group, -NO2 group, -NR1R2 group, (C1-C4)alkoxy group, phenoxy group and (C1-C3)alkyl group, wherein the above alkyl is optionally monosubstituted by a hydroxyl group, R1 and R2 independently represent a hydrogen atom or (C1-C3)alkyl group, n is equal to 1, 2 or 3, n′ is equal to 1 or 2, R′ represents a hydrogen atom, halogen atom or group specified in (C1-C3)alkyl group, -NO2 group, -NR1R2 group, morpholinyl group, N-methylpiperazinyl group, (C1-C3)fluoralkyl group and (C1-C4)alkoxy group, R″ represents a hydrogen atom, Z, Y, X, W, T and U represent N or C, and wherein at most four of V, T, U, Z, Y, X and W groups represent N, and at least one of T, U, Y, X and W groups represents N, for producing a medicinal preparation for preventing, inhibiting or treating AIDS. The invention also refers to using specific compounds, new quinoline derivatives, a pharmaceutical composition based on the new quinoline derivatives.EFFECT: new quinoline derivatives are produced, and new biological activity of known compounds is stated.15 cl, 2 tbl, 11 ex

N-[(1h-pyrazol-1-yl) aryl]-1h-indole or 1h-indazole-3-carboxamide derivatives, producing and using them as p2y12 antagonists // 2572593
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to compounds characterised by general formula (I), wherein A represents an aromatic diradical specified in groups having formulas such as below whereas the other radical and groups have values presented in the patent claim.EFFECT: invention refers to methods for producing the compounds of formula (I) , pharmaceutical composition containing them, and using them as P2Y12 antagonists for treating cardiovascular diseases.14 cl, 16 tbl, 21 ex

1-arylpyrrolo[1,2a]pyrazine-3-carboxamides with neuropsychotropic activity // 2572076
FIELD: chemistry.SUBSTANCE: invention relates to novel group of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides of formula (1), where R1 can be hydrogen or methal group, R2 can be (C1-C4)-alkyl or benzyl group and R3 can be hydrogen or halogen atom. Invention also relates to particular compounds, methods for obtaining formula (1) compound, methods for treating anxiety disorders. Novel 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides, possessing useful biological activity have been obtained.EFFECT: increased biological activity.15 cl, 13 tbl, 11 ex

Gel compositions with brimonidine and methods of application // 2571277
FIELD: medicine.SUBSTANCE: group of inventions relates to gel composition for local application, which contains from 0.05 to 0.20 wt % of methylparaben as preservative; one or more additional preservatives; from 0.80 to 1.50 wt % of carbomer; from 9.0 to 13.0 wt % of the total content of polyatomic alcohols, in particular propyleneglycol and glycerol; active ingredient, containing agonist of alpha-adrenergic receptors or its pharmaceutically acceptable salt, in particular brimonidine tartrate, and purified water, in which the total quantity of all ingredients equals 100%, composition pH constitutes from 4.5 to 7.5, and where when methylparaben concentration is higher than 0.15 wt %, carbomer concentration constitutes less than 1.25 wt %, and to method of treatment or prevention of skin disease in patient.EFFECT: creation of improved gel composition for local application, which in fact does not contain methylparaben crystals and possesses microbiological purity.15 cl, 2 ex, 3 tbl

Imidazopyrrolopyrazine derivatives, useful for treatment of diseases, caused by abnormal activity of proteinkinases jak1, jak3 or syk // 2570416
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to the field of organic chemistry, namely to a novel imidazopyrrolopyrazine derivative of formulaand to its pharmaceutically acceptable salt, stereoisomer or isomer, where R1, R2 and R5 represent H; R3 represents (C3-C6)cycloalkyl, substituted with one group, independently selected from CH2NH2 or NH2; or R3 represents -A-D-E-G, where: A represents a bond or -N(Ra)C(O)-Re-; D represents (C1-C3)alkylene, bound by a bridge bond (C8)cycloalkylene, (C4-C6)cycloalkylene, substituted with one substituent, selected from (C1-C3)alkyl; (C4-C5)monoheterocyclylene, optionally substituted with one substituent, selected from (C1-C3)alkyl, where monoheterocyclylene contains 1-2 heteroatoms, independently selected from carbon or oxygen atoms; E represents a bond, -Re, -Re-C(O)-Re-, -Re-O-Re-, -Re-N(Ra)-Re-, -Re-N(Ra)C(O)-Re-, -ReC(O)N(Ra)Re-, -Re-N(Ra)S(O)2-Re- or -Re-N(Ra)S(O)2N(Ra)-Re-; where in all cases E is bound either with a carbon atom or with a nitrogen atom in D; G represents hydrogen, -N(Ra)(Rb), -(C1-C6)alkyl, optionally substituted with 1-3 substituents, independently selected from a halogen, hydroxyl or cyano; (C3-C6)monocycloalkyl, optionally substituted with 1-2 substituents, independently selected from a halogen, cyano, monocyclic (C3-C5)heteroaryl, optionally substituted with one substituent, independently selected from cyano, where heteroaryl contains 2 heteroatoms, independently selected from nitrogen atoms; (C3-C5)monoheterocyclyl, optionally substituted with 1 or 2 substituents, independently selected from methyl, -CF3, halogen or CH2CN, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen atoms; (C6)aryl, optionally substituted with 1-2 substituents, independently selected from a halogen or cyano; where in the fragment, containing -N(Ra)(Rb), nitrogen, Ra and Rb can form a ring in such a way that -N(Ra)(Rb) represents C4monoheterocyclyl, where monoheterocyclyl contains 1-2 heteroatoms, independently selected from nitrogen or oxygen; R4 represents hydrogen or -(C1-C6)alkyl; Ra and Rb, each independently represent hydrogen, (C1-C6)alkyl, oxetane; and Re for each case independently represents a bond or -(C1-C4)alkylene. The invention also relates to particular imidazopyrrolopyrazine derivatives, a pharmaceutical composition, based on the claimed compound and to the application of the claimed compound.EFFECT: invention provides obtaining novel imidazopyrrolopyrazine derivatives, useful in the treatment of conditions, mediated by the activity of Jak1, Jak3 and Syk proteinkinases.23 cl, 54 tbl, 690 ex

Substituted pyridopyrazines as novel syk inhibitors // 2569635
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I), their racemic mixture, enantiomers, diastereomers and pharmaceutically acceptable salts, possessing properties of Syk inhibitor, pharmaceutical composition and medication based thereof, thereof application, methods of inhibiting and method of treatment with thereof application. In general formula (I) R1 represents hydrogen or C1-C6alkyl, R2 represents phenyl, benzo[d][1,3]dioxolyl, 2,3-dihydrobenzo[b][1,4]dioxinyl, or 5-10-membered heteroaryl, containing 1-2 heteroatoms, selected from N and O, which is optionally substituted with one or several groups, selected from halogen, -NR5R6, -OR7, -S(O)nR8, -C(O)R9, -CN, -C(O)NR5R6, -NR5C(O)R9, -NR5S(O)nR8, -S(O)nNR5R6, C1-C6alkyl, optionally substituted with one, two or three groups, selected from halogen, -OH, -OC1-C4alkyl, -NH2, -NH(C1-C4alkyl), -N(C1-C4alkyl)(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), or 5-8-membered heterocycle, containing 1-2 heteroatoms, selected from N, O, and S, optionally substituted with -SO2(C1-C4alkyl), C3-C6cycloalkyl, 5-8-membered heterocycle, containing 1-2 heteroatoms, selected from N, O and S, optionally substituted with one, two, or three groups, selected from halogen, -OH, C1-C4alkyl, -C1-C4alkyl-OH, ketogroup(oxo), -C(O)C1-C4alkyl, -C(O)C3-C6cycloalkyl, -C(O)C3-C6cycloalkyl-CN, -C(O)C3-C6cycloalkylhalogen, -C(O)NH2, -C(O)NH(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), -C(O)(C1-C4alkyl)-OH, -C(O)(C1-C4alkyl)-O(C1-C4alkyl), -C(O)C1-C4halogenalkyl, -C(O)(C1-C4alkyl)-CN, -C(O)(C1-C4alkyl)-C(O)NH2, -C(O)(C1-C4alkyl)C3-C6cycloalkyl, -C(O)(C1-C4alkyl)-oxetane, C(O)-furanyl, -C(O)-tetrahydrofuranyl, -C(O)(C1-C4alkyl)-SO2(C1-C4alkyl), -O(C1-C4alkyl)-OH, -SO2(C1-C4alkyl), -SO2NH(C1-C4alkyl), -SO2(C1-C4alkyl)(C1-C4alkyl), -SO2C3-C6cycloalkyl, -N(C1-C4alkyl)C(O)(C1-C4alkyl), and 5-6-membered heteroaryl, containing 1-2 nitrogen atoms, optionally substituted with C1-C4alkyl, R3 and R4 are independently selected from hydrogen, C1-C6alkyl, C3-C6cycloalkyl, phenyl, 1,3-dihydroisobenzofuranyl, and 5-6-membered heterocycle, containing 1 nitrogen atom, each of which, except hydrogen, is optionally substituted with one or several groups, selected from halogen, -NR5R6, -OR7, -C(O)OR7, -CN, -C(O)NR5R6, -S(O)nNR5R6, C1-C6alkyl, C3-C6cycloalkyl, 5-6-membered heteroaryl, containing 1-2 nitrogen atoms, and 4-7-membered heterocycle, containing 1-2 heteroatoms, selected from N, O, and S, optionally substituted with one, two or three groups, selected from halogen, hydroxyl, ketogroup(oxo) C1-C4alkyl, -C1-C4alkyl-OH, -C1-C4halogenalkyl, -C(O)NH2, -C(O)NH(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), -C(O)C1-C4alkyl, -C(O)(C1-C4alkyl)-C3-C6cycloalkyl, -C(O)C3-C6cycloalkyl, -C(O)C1-C4halogenalkyl, -C(O)(C1-C4alkyl)-CN, -C(O)(C1-C4alkyl)-OH, -C(O)(C1-C4alkyl)-O-(C1-C4alkyl), -C(O)(C1-C4alkyl)N(C1-C4alkyl)2, -C(O)(C1-C4alkyl)-SO2-(C1-C4alkyl), -C(O)(C1-C4alkyl)-C3-C6cycloalkyl, -SO2(C1-C4alkyl), -SO2(C1-C4halogenalkyl), -SO2C3-C6cycloalkyl, -SO2NH2 and pyrimidinyl, or R3 and R4 together with N atom, which they bind to, can form 5-10-membered monocyclic, fused bicyclic or spirocyclic ring, optionally containing 1 additional nitrogen atom, which is optionally substituted with one or several groups, selected from -NR5R6, -C(O)OR7, -C(O)NR5R6, -NR5S(O)nR8, -NR5C(O)NR10R11, and C1-C6alkyl optionally substituted with hydroxyl, amino, -NHSO2(C1-C4alkyl), -NH(C1-C4alkyl), -N(C1-C4alkyl)(C1-C4alkyl), or -NHC(O)NH2, m equals 0 or 1, n equals 2.EFFECT: obtaining novel compounds.28 cl, 3 ex

Compounds suitable for cancer treatment // 2567752
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to application of formulacompound,where stands for aromatic ring, where V represents C or N and, where V represents N, V is in meta- or para-position to Z, R independently represents hydrogen atom, halogen atom or group, selected from group -CN, hydroxyl group, group -COOR1, (C1-C3)fluoroalkyl group, (C1-C3)fluoroalkoxy group, group -NO2, group -NR1R2, (C1-C4)alkoxy group, phenoxy group and (C1-C3)alkyl group, where said alkyl is possibly monosubstituted with hydroxyl group, R1 and R2 independently represent hydrogen atom or (C1-C3)alkyl group, n equals 1, 2 or 3, n' equals 1 or 2, R' represents hydrogen atom, halogen atom or group, selected from (C1-C3)alkyl group, group -NO2, group -NR1R2, morpholinyl group, N-methylpiperazinyl group, (C1-C3)fluoroalkyl group and (C1-C4)alkoxy group, R" represents hydrogen atom, Z, Y, X, W, T, U independently represent N or C, and where maximum four of groups V, T, U, Z, Y, X and W represent N, and at least one of groups T, U, Y, X and W represents N, or any of its pharmaceutically acceptable salts for obtaining medication for prevention, inhibition or treatment of cancer. Invention also relates to application of particular compounds, to novel quinoline and isoquinoline derivatives, pharmaceutical composition based on novel quinoline and isoquinoline derivatives.EFFECT: obtained are novel quinoline and isoquinoline derivatives, and novel biological activity of known compounds is discovered.10 cl, 2 tbl, 6 ex

4-phenoxy-nicotanimides or 4-phenoxy-pyrimidine-5-carboxamides // 2565077
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula I wherein A1 represents CR13; A2 represents CR14 or N; R1 and R2 are independently specified in hydrogen, halogen, and halogen-C1-7-alkyl; R13 and R14 are independently specified in hydrogen, C1-7-alkyl, halogen, halogen-C1-7-alkyl and C1-7-alkoxy; R3 is specified in hydrogen, C1-7-alkyl, halogen, C1-7-alkoxy, piperidinyl and -NR15R16, wherein R15 and R16 are independently specified in hydrogen, C1-7-alkyl and C3-7-cycloalkyl; R4 is specified in hydrogen and C1-7-alkyl; or R3 and R4 or R3 and R14 together represent -X-(CR17R18)n- and form a part of the ring, wherein X is specified in -CR19R20- and -NR21-; R17, R18, R19, R20 are hydrogen; R21 is specified in hydrogen, C1-7-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-7-alkyl, wherein C3-7-cycloalkyl is substituted or not by C1-7-alkoxycarbonyl, and C1-7-alkylsulphonyl; and n represents 1, 2 or 3; B1 represents N or N+-O-; B2 represents CR7 or N; R5, R6 and R7 are independently specified in hydrogen, halogen and C1-7-alkyl; and R8, R9, R10, R11 and R12 are those as presented in the patent claim. The compound also refers to pharmaceutically acceptable salts of the compounds of formula I and to pharmaceutical compositions possessing GPBAR1 receptor agonist activity.EFFECT: compounds of formula I as GPBAR1 agonists.20 cl, 85 ex

Crystalline β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-n,n'-dioxide, method of thereof obtaining and thereof-based pharmaceutical composition // 2563256
FIELD: chemistry.SUBSTANCE: invention relates to crystalline β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-N,N'-dioxide (dioxidine), method of its obtaining and its application for preparation of pharmaceutical composition, possessing antimicrobial, antibacterial and bactericidal activity.EFFECT: crystalline dioxidine β-modification possesses increased antimicrobial, antibacterial and bactericidal activity in comparison with activity of initial dioxidine substance.3 cl, 8 dwg, 4 tbl, 4 ex

New nicotinamide derivative or salt thereof // 2560163
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to nicotinamide derivatives of formula (I) exhibiting the property of Syk-kinase inhibitor and to a based pharmaceutical composition. In general formula R1 means halogen atom; R2 means a substitute presented by formula as follows and R3 means a pyridyl group presented by formulas as follows (VIII-1) or (VIII-2); R4 and R5 mean hydrogen atom. The other radicals are presented in the patent claim.EFFECT: producing new nicotinamide derivatives.13 cl, 2 dwg, 25 tbl, 47 ex

8-methyl-1-phenylimidazo[1,5-a]pyrazine compounds // 2560162
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel 8-methyl-1-phenylimidazo[1,5-a]pyrazine derivatives of formula or pharmaceutically acceptable salts thereof, where R1 is 1-2 groups independently selected from hydrogen, hydroxy, (1-6C)alkoxy, halogen; R2 is H or (1-6C)alkyl; R3 is (R31)(R32)CH-O; or (1-6C)alkoxy; or heteroaryl, which is an indole, pyrrole, indazole, pyrrolopyridine, thienopyrrole, optionally substituted with 1-2 groups selected from R34, R35, R36, halogen, hydroxy; R31 is (1-5C)alkyl, optionally substituted with one hydroxy; R32 is (1-5C)alkyl; R34 is (1-6C)alkyl; R35 is (1-6C)alkoxy; R36 is hydrogen or (1-6C)alkyl; R4 is or or R4 is (1-4C)alkyl, independently substituted with 1 substitute selected from R8, hydroxy; where m, n, r equals 1 or 2; Y is CR5 or N; X is O, CHR6, C(R66)(R67), NR7, C=O; Z is O or Z forms with R9 a 5-member heterocyclyl substituted with R91; R5 is H or (1-6C)alkyl; R6 is R61, R62, R63, R65, H, hydroxy; R7 is R71, R72, R73, R74, H; R8 is imidazole; R9: H or (1-6C)alkyl, optionally substituted with one or more fluorine atoms; R61 is amino(1-4C)alkyl, [(1-6C)alkyl]amino(1-4C)alkyl, (di)[(1-6C)alkyl]amino(1-4C)alkyl, [(1-4C)alkylcarbonyl]amino(1-4C)alkyl, [(1-4C)alkoxycarbonyl]amino(1-4C)-alkyl; R62 is (1-4C)alkylcarbonyloxy, (3-6C)cycloalkylaminocarbonyloxy; R63 is amino, [(1-6C)alkyl]amino, (di)[(1-6C)alkyl]amino, [(1-6C)alkoxy(2-6C)alkyl]amino, [(1-6C)alkyl][(1-6C)alkoxy(2-6C)alkyl]amino, [(1-6C)-alkylcarbonyl][(1-6C)alkoxy(2-6C)alkyl]amino; all alkyl groups in R63 are optionally substituted with 2 fluorine atoms; R65 is an N-bonded heterocyclyl, which is pyrazine, azetidine, morpholine, optionally substituted with 1 oxo group, or 2 fluorine atoms or one R651 group; R66 is [(1-6C)alkyl]amino(1-4C)alkyl; R67 is hydroxy; R71 is (1-6C)alkyl; R72 is (1-4C)alkyl, substituted with 1 R725 group; R73 is R732carbonyl, R733carbonyl or R735carbonyl; R74 is a heterocyclyl which is tetrahydropyran or piperidine, optionally substituted with one R741 group; R91 is (1-6C)alkyl, substituted with 3 fluorine atoms; R651 is (1-4C)alkyl, (1-4C)alkylcarbonyl; R725 is (di)[(1-6C)alkyl]-aminocarbonyl; R732 is (1-4C)alkyl, amino(1-4C)alkyl, (di)[(1-6C)alkyl]-amino(1-4C)alkyl, hydroxy(1-4C)alkyl, (1-6C)alkoxy(1-4C)alkyl; R733 is (1-6C)alkoxy; R735 is amino; R741 is (1-4C)alkylcarbonyl. The invention also relates to use of the compound of formula I.EFFECT: obtaining novel 8-methyl-1-phenylimidazo[1,5-a]pyrazine derivatives which are useful in treating an Lck-mediated condition.14 cl, 1 t bl, 77 ex

4,10-bis((±)-5-benzoyl-2,3-dihydro-1h-pyrrolo[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane as analgetic means and method of its obtaining // 2558148
FIELD: chemistry.SUBSTANCE: invention relates to a novel chemical substance - 4,10-bis((±)-5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane The invention also relates to a method of its obtaining, which consists in the acylation of 2,6,8,12-tetraacetyl-2,4,6,8,10,12- hexaazatetracyclo [5,5,0,03,11,05,9]dodecane by chloranhydride 5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.EFFECT: novel compound, which has analgetic activity, is obtained.2 cl, 1 tbl, 2 ex
ethod of treating radiation and interstitial cystitis // 2557949
FIELD: medicine.SUBSTANCE: method involves instilling the Colegel ADL gel preparation every second day from the 1st to 20th day, and then Colegel DNK L two times a week from the 21st to 56th day.EFFECT: invention enables relieving pain symptomatic, reducing the rate and length of recurrences in the patients.3 ex

ethods of obtaining and purification of heteroaryl compounds // 2557242
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to methods of obtaining heteroaryl compounds, represented by structural formulae (I) or (II): where R1-R4 have values, given in subcl. 1,14 of the formula.EFFECT: compounds can be used for treatment or prevention of cancer, inflammatory states, immunological states, etc.29 cl, 20 ex
ethod of treating chronic opisthorchiasis in patients with rosacea // 2555351
FIELD: medicine.SUBSTANCE: praziquantel is administered in a single dose of 20 mc/kg for the first day of treatment in the daytime, and withdrawn; on the following day, the conducted therapy is added with introducing Gelmicide, a biologically active food supplement, in a dose of 2 capsules with meals for 21 days; the course is repeated 10 days later in a dose of 2 capsules 2 times a day with meals for 14 days.EFFECT: reducing the rate of complications and increasing the high dishelminthisation efficacy.1 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

ethod for overcoming gentamycin resistance in methicillin-resistant s. aureus strains // 2553601
FIELD: medicine.SUBSTANCE: invention refers to medicine, namely to clinical microbiology and antimicrobial chemotherapy, and concerns developing and creating new combinations providing potentiating bactericidal action and effectively inhibiting the purulent infection caused by methicillin-resistant S. aureus by using two classes of compounds possessing the essentially different mechanism of antimicrobial action.EFFECT: developing and creating the new combinations providing potentiating bactericidal action and effectively inhibiting the purulent infection.2 dwg, 6 tbl
Capsular form of clofazimine // 2553310
FIELD: medicine.SUBSTANCE: invention concerns a simplified capsular form of clofazimine, containing clofazimine, bee wax, soya bean lecithin, butylhydroxy toluene, soya bean oil, gelatine, glycerol, sorbitol, methylparabene, propylparabene, titanium dioxide, brown chocolate and purified water with preserving high efficacy.EFFECT: simplifying the form.4 tbl, 3 ex
Condensed heteroaryls and their application // 2552114
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula (1) and/or to their pharmaceutically acceptable salts, where A1 represents CH; A4and A5 independently represent CR2 or N; A2 and A3 together with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected from where t represents 1 or 2; and R3 is independently selected from H, C1-C6 alkyl, C6-aryl, C3-C6-membered cycloalkyl, C(O)NRcRd, -ORb, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C1-C6 alkyl, possibly substituted with one substituent, selected from -CONMe2, C3-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)Ra; -CN; -C(O)NRcRd; -NRcRd; -ORb; -S(O)nRe; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when A4 represents CR2, A2 and A3 together with ring B are selected from structure (3), (5) or (6); represents single bond or double bond; R1 represents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from C1alkyl, C2alkinyl, -NRcRd, -NRcS(O)nRe, -ORb, halogen, halogenalkyl; R2 is independently selected from H; each Ra, Rb, Rc, Rd, and Re is independently selected from H; C1-C4alkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH2, -NMe2, C3-cycloalkyl; C2-C3alkenyl; C3alkinyl; C6aryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C3-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rc and Rd together with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex
 
2551153.
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