(A61K31/4709)

ultifunctional quinoline derivatives as antineurodegenerative agents // 2642466
FIELD: chemistry.SUBSTANCE: invention relates to a hydroxy-derived quinoline of the formula (I) or to a pharmaceutically acceptable salt thereof, (I) wherein R1 is hydrogen, (C1-C3)alkyl, (C1)alkylene(C3)cycloalkyl, (C1)haloalkyl or (C1)alkylene(C6)aryl; R2 is hydrogen or halogen; R3 is hydrogen, halogen, (C1)alkyl or (C1)alkoxy; R4 is hydrogen, halogen, (C1)alkyl, (C1)alkoxy or (C1)haloalkyl; R5 and R6 are hydrogen; and R7 is (C9-C15)alkanol, (C1)alkylenepiperazinyl(C1-C2)alkanol, (C1-C8)alkylenepiperazinyl (C1-C2)alkyl, (C10-C13)alkylene OCOCH3, (C1)alkylene(C1)alkylamino(C3)alkynyl, (C1)alkyleneamino(C8)alkanol or (C1)alkyleneamino(C6)alkanol(C1)alkylene(8-methoxyquinolin-2-yl); or (II), where R1, R2, R3, R4 and R6 each is as described in (I) above; R5 is (C11-C12)alkanol, and R7 is hydrogen. The invention also relates to a pharmaceutical composition based on the formula (I) compounds, a method for treatment of Alzheimer's disease, traumatic brain injury and/or damage to the spinal cord and a method for improvement of the ability of learning and/or memory in a patient suffering from Alzheimer's disease, based on the formula (I) compound.EFFECT: new hydroxy derivatives of quinoline have been obtained that have useful biological properties.13 cl, 13 dwg, 9 ex
1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2h-chromen-3-yl)-1,4-dihydroquinoline-3-carboxylic acid with anti-tubercular activity // 2642426
FIELD: pharmacology.SUBSTANCE: invention relates to a fluoroquinolone carboxylic acid derivative, namely 1-ethyl-6-fluoro-4-oxo-7-(8-ethoxy-2-oxo-2H-chromen-3-yl)-1,4-dihydroquinoline-3 carboxylic acid of formula .EFFECT: high antitubercular activity, including that with respect to strains of mycobacteria with multiple drug resistance.2 tbl, 1 ex
Partly saturated nitrogen-containing heterocyclic compound // 2641291
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the formula (I'), (wherein W represents the formula -CR11R12CR13R14-; R11 represents a hydrogen atom, a fluorine atom, C1-4 alkyl or phenyl; R12 represents a hydrogen atom, a fluorine atom or C1-4 alkyl; provided that R11 and R12, together with the adjacent carbon atom, optionally form C3-8 cycloalkane or tetrahydropyran; R13 represents a hydrogen atom, a carbamoyl, C1-4 alkyl (C1-4 alkyl is optionally substituted by one group selected from the group consisting of hydroxy, C1-3 alkoxy and di-C1-3 alkylamino), halo-C1-4 alkyl, phenyl, pyridyl, benzyl or phenethyl; R14 represents a hydrogen atom, C1-4 alkyl or halogen-C1-4 alkyl; Y represents a single bond or C1-6 alkanediyl (C1-6 alkanediyl is optionally substituted by one hydroxy group and one of the carbon atoms in C1-6 alkanediyl is optionally substituted by cycloalkpropane-1,1-diyl); R2 represents a hydrogen atom, C1-6 alkyl, C3-8 cycloalkyl {C3-8 cycloalkyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl (C1-6 alkyl is optionally substituted by one phenyl group), phenyl (phenyl is optionally substituted by one halogen atom), C1-6 alkoxy [C1-6 alkoxy is optionally substituted by one group selected from the group consisting of C3-8 cycloalkyl, phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom and C1-6 alkyl) and pyridyl (pyridyl is optionally substituted by one halogen atom)], C3-8 cycloalkoxy, phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl) and pyridyloxy (pyridyloxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl)}, phenyl (phenyl is optionally substituted by one to three groups that are the same or different and which are selected from the group of α3 substituents), naphthyl, indanyl, tetrahydronaphthyl, pyrazolyl [pyrazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl (phenyl optionally substituted by one C1-6 alkyl)], imidazolyl [imidazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl], isoxazolyl [isoxazolyl is optionally substituted by one phenyl group (phenyl is optionally substituted by one halogen atom)], oxazolyl [oxazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl and phenyl], thiazolyl [thiazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl, phenyl and morpholino], pyridyl (pyridyl is optionally substituted by one or two groups that are are the same or different and are selected from the group of α5 substituents), pyridazinyl [pyridazinyl is optionally substituted by one C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl group)], pyrimidinyl [pyrimidinyl is optionally substituted by one group selected from the group consisting of halogen-C1-6 alkyl, C3-8 cycloalkyl, phenyl and phenoxy (phenoxy is optionally substituted by one C1-6 alkyl)], pyrazinyl [pyrazinyl is optionally substituted by one group selected from the group consisting of C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl), and phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl and C3-8 cycloalkyl)], benzothiophenyl, quinolyl, methylenedioxyphenyl (methylenedioxyphenyl is optionally substituted by one or two fluorine atoms), azetidinyl (azetidinyl is optionally substituted with one pyrimidinyl group), piperidinyl (piperidinyl is optionally substituted by one group selected from the group consisting of pyrimidinyl, phenyl-C1-3 alkyl, C3-8 cycloalkyl-C1-3 alkylcarbonyl and phenyl-C1-3 alkoxycarbonyl) or the following formula (I") -CONR5CH2-R6 (I") [wherein in formula (I") R5 represents a hydrogen atom or C1-3 alkyl and R 6 is phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom, halogen-C1-6 alkyl and phenyl)], Y4 represents C1-4 alkanediyl; R3 represents a hydrogen atom or methyl; R4 represents -COOH or -CONHOH).EFFECT: compound has a superior PHD2 inhibitory effect.16 cl, 28 tbl, 11 ex
Heterocyclic compounds, effective for kinase inhibition // 2640862
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein Q is O; W is phenyl; X is absent; Y is NH; Z1 and Z2 are N; Z3 is NR5, where R5 is hydrogen; R1 is pyridine or pyrimidine; optionally substituted with C1-C6alkyl, C1-C6alkoxy, -NR10R11 or -SOmR12, where R10 and R11 are hydrogen, R12 is C1-C6alkyl; and m is 0; R3 is C1-C6alkyl; R2 is C1-C6alkyl when p is 1; or one R2 is C1-C6alkyl and one R2 is halogen when p is 2; or one R2 and R3 combined with formation of a five- to seven-membered carbocycle; R4 is hydrogen; p=1 or 2; and n is 1.EFFECT: heterocyclic compounds designed for cancer treatment.12 cl, 1 tbl, 8 ex

New glp-1 receptor modulators // 2634896
FIELD: pharmacology.SUBSTANCE: compounds can be used in combination to reduce glucose with exenatide. In the formula IR or IS , A is a heteroaryl selected from imidazole, oxadiazole, thiadiazole, thiazole, oxazole, pyridine, pyrimidine, pyridazine, triazine; B is a heterocyclyl selected from isoxazole, oxazole, pyrimidine, pyrazole, thiazole, thiophenyl, thiadiazole, azepine, optionally fused to another nitrogen-containing 6-membered heterocyclic ring; C is an aryl selected from phenyl and naphthyl, benzyl; Y1 and Y2 are absent; Z is -C(O)-; each R1 is independently H or C1-4 alkyl; R2 is -O-R8, -N(R1)-SO2-R8, -NR41R42, -N(R1)-(CRaRb)m-COOH, -N(R1)-(CRaRb)m-CO-N(R1)-heterocyclyl, -N(R1)-(CRaRb)m-CO-N(R1)(R7) or -N(R1)-heterocyclyl, wherein R2 is not -OH or -NH2, and heterocyclyl is a 5-6 membered heterocyclyl containing 1 to 3 heteroatoms selected from N and S; each R3 and R4 is independently halogen, C1-C4alkyl, C1-C4alkyl substituted with R31, C1-C4alkoxy, halogenC1-C4alkyl, perhalogenC1-C4alkyl, halogenC1-C4alkoxy, -OH, -NR1R8, -C(O)R8, -C(O)NR1R8, -S(O)2R8, -OS(O)2R8, -(CRaRb)mNR1R8, -(CRaRb)mO(CRaRb)mR8; or any two R3 or R4 groups on the same carbon atom, taken together, form oxo, values of R31, R40, R41, R42 are indicated in the claims; W1 is absent; each Ra and Rb have values indicated in the claims; R5 is R7, -(CH2)m-L2-(CH2)m-R7 or -(-L3-(CRaRb)r-)s-L3-R7; R7, R8 have values indicated in the claims; L2 is independently, from the near to the far end of the structure of the formula I-R or I-S, absent or -O-; each L3 is independently absent, -O- or -N(R1)-, each m is independently 0, 1, 2, 3, 4, 5 or 6; each n is independently 0, or 1, or 2; P is 0, 1, 2, or 3; Q is 0, 1, 2, or 3.EFFECT: compounds have activity for glucagon-like peptide 1 and can be used to treat diseases for which modulation or potentiation of GLP-1R is prescribed, particularly for the treatment of diabetes.8 cl, 2 tbl, 381 ex
Analgesic means // 2634618
FIELD: pharmacology.SUBSTANCE: invention relates to an analgesic means in which individual substituted quinoline-4(1H)-ones of general formula 1 their salts or compositions based on them are active substances, and which can be used as an anesthetic to treat humans and animals, where R1 = phenyl unsubstituted or substituted by one substituent selected from alkyl (C1-C4), alkoxy (OC1-OC4), halogen; phenyl substituted by two substituents selected from methyl, ethyl, methoxy, ethoxy or halogen; unsubstituted naphthyl, unsubstituted thienyl or thienyl substituted by one substituent selected from methyl or halogen; unsubstituted furyl, C4-alkyl, OMe; R2+R3 = =O, =NOMe, R4=H, COOMe, COOH; R5= H, Me; R6th= H, Me, OMe, Et, halogen; R7th= H, halogen, CN; R8= H, alkyl (C1-C4), halogen, CN.EFFECT: expansion arsenal of anesthetic means.2 tbl, 7 ex
Fluoroquinolones based on 4-deoxypyridoxine // 2634122
FIELD: pharmacology.SUBSTANCE: invention relates to new fluoroquinolone derivatives of the general formula (I), where R1 = ; R2 = H; R3 = ; or R1 = C2H5; R2 = H; R3 = ; or R1 = C2H5; R2 = F; R3 = ; or R1 = ; R2 = OCH3; R3 = .EFFECT: new fluoroquinolone derivatives with antibacterial activity.2 tbl, 6 ex
Pill containing methanesulfonate hydrate of 1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-1-methyl-2,3-dihydro-1h-isoindole-5-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid // 2633477
FIELD: pharmacology.SUBSTANCE: dosage form in the form of a pill according to this invention has a percentage of methanesulfonate hydrate of 1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-isoindole-5-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid from 80 wt % to 97.5 wt %.%. The pill has a size smaller than 200 mg of the commercially available Geninax pill.EFFECT: compliance with the drug regimen is improved, washability is high, crushing strength and abrasion resistance are high, the invention withstands film coating and transportation and is suitable as a methanesulfonic acid hydrate pill of chemical compound A.13 cl, 29 ex, 6 tbl

Crystalline form i of tyrosine kinase inhibitor dicaletat and method for its preparation // 2631321
FIELD: pharmacology.SUBSTANCE: invention relates to the crystalline form I of (R,E)-N-(4-(3-chloro-4-(pyridin-2-yl-methoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide dimaleate, a method for its preparation, a pharmaceutical composition based thereon, and its use.EFFECT: resulting crystalline form I of dimaleate has good crystal stability and chemical stability and can be used to prepare drugs for treatment of diseases associated with EGFR tyrosine protein kinase or HER-2 receptor tyrosine protein kinase.7 cl, 4 dwg, 2 tbl, 7 ex

Pharmaceutical compositions for treatment of skin diseases and conditions containing 7-(1h-imidazol-4-ylmethyl)-5,6,7,8-tetrahydroquinoline // 2630978
FIELD: pharmacology.SUBSTANCE: invention is a method for skin conditions treatment in a patient suffering therefrom, comprising administration of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-imidazol-4-ylmethyl)-5,6,7,8-tetrahydroquinoline or pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients, wherein the condition is selected from rosacea, rapid rosacea, sunburn, psoriasis, flushing and redness associated with hot flashes, erythema associated with hot flashes, photoaging, face telangiectasia, tingling or burning sensation, skin erythema and skin hyperactivity with skin blood vessels dilation.EFFECT: extension of the arsenal of agents for treatment of rosacea, rapid rosacea, sunburn, psoriasis, flushing and redness associated with hot flashes, erythema associated with hot flashes, photoaging, face telangiectasia, tingling or burning sensation, skin erythema and skin hyperactivity with skin blood vessels dilation.11 cl, 7 dwg, 3 ex

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

Derivatives of hinoline, visualizing tau protein // 2627694
FIELD: pharmacology.SUBSTANCE: invention relates to a new quinoline derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is or , R1 is halogen or , in which R4 and R5 each independently represents hydrogen, a lower alkyl group, or R4, R5 and the nitrogen atom to which they are attached together form a 6-member nitrogen-containing aliphatic ring (where the nitrogen atom may be substituted by a lower alkyl group), or R4 and the nitrogen atom to which it is attached together with ring A form a 10-membered nitrogen-containing fused bicyclic ring (one carbon atom constituting the nitrogen-containing condensed bicyclic ring can be replaced by the oxygen atom), and R5 is a lower alkyl group where a line crossed by a dashed line means a bond of the above general formula with another structural moiety, R2 or R3 each independently represents NRaRb or -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy groups), ring A is unsubstituted or substituted by R6 (where R6 is one substituent selected from halogen and an -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy, Ra and Rb each represents hydrogen or a lower alkyl group, m and n denote an integer from 0 to 1, wherein at least one of R2, R3 and R6 is an -O-lower alkyl group substituted with one hydroxy group and one halogen. The invention also relates to a pharmaceutical composition, a composition for conformational disease diagnosis, treatment or prevention, a diagnostic kit based on a compound of formula (I), a method of treatment, a method for detection or staining of a protein-layer β-structure, a process for preparation of a compound of formula (I) and intermediates.EFFECT: new compounds are obtained that can be used to diagnose and treat conformational diseases, in particular, a disease having such a cardinal symptom as intracerebral accumulation of tau protein, for example, Alzheimer's disease.17 cl, 29 dwg, 26 tbl, 2 ex
Aza-aryl-1-h-pyrazol-1-yl-sulphonamides // 2627268
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) ,in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists.EFFECT: increased efficiency of compounds application.26 cl, 2 tbl, 33 ex
Adamantyl derivatives useful for treatment of jnk-mediated disorder // 2626890
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the heterocyclic compound of I formula or a pharmaceutically acceptable salt thereof, wherein R represents phenyl optionally substituted with one or more R'; R' is halo or methoxy; X represents CH; X1 represents C(=O)OCH3; Y represents N; Y1 It is OH, N(Y1')2, NHS(=O)2Y1', NHC(=O)Y1', NHC(=O)C(CH3)2OH or NHC(=O)C(CH3)2OC(=O)Y1'; each Y1' independently represents H, C1-6-alkyl or lower cycloalkyl; Y2 It is H. The invention also relates to formula I based on the compound of the pharmaceutical composition and the use thereof.EFFECT: new heterocyclic compounds useful for treating JNK-mediated disorder are obtained.12 cl, 5 tbl, 31 ex
Quinolines as fgfr kinase modulators // 2625303
FIELD: pharmacology.SUBSTANCE: invention related to a new quinoline derivative of formula (I), where W us -N(R3)- or -C(R3aR3b)-; each R2 is independently selected from halogen, C1-4alkoxy, Y is -E-D; D is phenyl or 5-6-membered monocyclic heterocyclyl, containing one or two heteroatoms selected from N or O, wherein the mentioned heterocyclyl can be optionally substituted with one group of R1; E is a link; R1 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyl which is substituted with -S(=O)2-C1-6alkyl, R6; R3a is hydroxyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, C1-6alkyl which is substituted with -NR10R11, C1-6alkyl which is substituted with -C(=O)-NR10R11; R3b is hydrogen; or R3a and R3b are combined to obtain =O or to obtain =CH-C0-4alkyl which is substituted with R3c; R3c is cyano; R3 is C2-6alkynyl, hydroxyC1-6alkyl, hydroxyhaloC1-6alkyl, C1-6alkyl which is substituted with R9, C2-6alkynyl which is substituted with R9, C1-6alkyl which is substituted with -NR10R11; R6 is 6-membered monocyclic heterocyclyl, containing one O atom; R9 is 5- or 6-membered monocyclic heterocyclyl, containing one or two heteroatoms, seleceted from N or O, each is optionally and each is independently substituted with substitute selected from =O, C1-4alkyl, C1-4alkoxy, S(=O)2-NR14R15, C1-4alkyl which is substituted with -NH-S(=O)2-haloC1-4alkyl, 6-membered aromatic monocyclic heterocyclyl, containing two N atoms, wherein the mentioned heterocyclyl is optionally substituted with R16; each R10 and R11 independently represent hydrogen, C1-6alkyl, haloC1-6alkyl; each R14 and R15 independently represent C1-4alkyl; R16 is C1-4alkoxy; n independently represent a whole number equal to 2, 3 or 4; as well as to its pharmaceutically acceptable salt and to any tautomeric or stereochemically isomeric form thereof. The invention also relates to pharmaceutical compositions based on compound of formula (I), application of the compound of formula (I), method for the prevention or treatment of a disease and product based on the compound of formula (I).EFFECT: new quinoline derivatives are obtained, useful in the treatment of diseases mediated by FGFR kinase.30 cl, 2 tbl, 35 ex

2-quinaldicarboxylic acid derivatives and their anti-influenza activity // 2624906
FIELD: pharmacology.SUBSTANCE: agent is amino acid derivatives of 2-quinaldicarboxylic acid: 2-quinaldine-seryl methyl ester (Qln-Ser), 2-quinaldine-tryptophanyl methyl ester (Qln-Trp) and 2-quinaldine-alanyl-proline-1(1-adamantyl)ethylamide (Qln-APR), and can be used for development of new antiviral drugs. The invention also relates to a new compound - 2-quinaldine-alanyl-proline-1(1-adamantyl)ethylamide (Qln-APR).EFFECT: increased antiviral activity of derivatives against influenza A viruses and acting on strains resistant to rimantadine and amantadine.3 cl, 7 dwg, 4 tbl, 6 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
Heterocyclic compounds and their application as glycogen synthase kinase-3 inhibitors // 2623427
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula , where A represents NRB, where RB represents hydrogen; X1 and X2 represent CR2 and X3, X4, X5 and X6 represent CR3 or CR4, or X1 and X2 represent CR2, X3 represent N, and X4, X5 and X6 represent CR3; Y1, Y2, Y3 and Y4 represent CR4 or CR5 or Y2 represents N, and Y1, Y3 and Y4 represent CR5; provided that no more than one of Y1, Y2, Y3 and Y4 represents CR4; and provided that one of Y1, Y2, Y3 and Y4 represents CR4 or C-CF3, if none of X3, X4, X5 and X6 represents CR4; R1 represents hydrogen; each R2 represents hydrogen; each R3 is independently selected from the group consisting of hydrogen, CN, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy and C1-C6-haloalkoxy; R4 represents a C-linked saturated or partially unsaturated monocyclic 5- or 6-member heterocyclic ring containing one heteroatom selected from O and N, as ring members, wherein the heterocyclic ring optionally has one N-linked substituent R8; R5 is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-haloalkyl and C3-C7-cycloalkyl; and R8 is selected independently on the case from the group consisting of C1-C6-alkyl, C1-C6-haloalkyl and C1-C6-alkoxycarbonyl. The invention also relates to pharmaceutical compositions based on a formula (I) compound, formula (I) compound application, a method of treatment of diseases susceptible to treatment by a compound that modulates the activity of 3β glycogen synthase kinase.EFFECT: new heterocyclic compounds useful for treatment of neurodegenerative disorders or inflammatory diseases are obtained.25 cl, 2 tbl, 70 ex
Heterobicyclic derivatives as hcv inhibitors // 2621734
FIELD: chemistry.SUBSTANCE: invention relates to heterocyclic compound of formula (I) or to pharmaceutically acceptable salt thereof, wherein Y is CH, N or CR4; W is carbonyl, sulfonyl or CR5R6; is or is independently selected from the group containing R and R' independently selected from -CR1R2R3, where R1 is selected from C1-4alkyl; R2 is C1-4alkyloxycarbonylamino; R3 is hydrogen; R4 is hydrogen or fluorine; CR5R6 together form oxetane. The invention also relates to pharmaceutical composition based on compound of formula (I), its use and product on its base.EFFECT: obtaining novel heterocyclic compounds, useful in the treatment of HCV infections.14 cl, 2 tbl

aleate salts of (e)-n-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and their crystal form // 2621719
FIELD: chemistry.SUBSTANCE: method of increasing neratinib oral absorption incudes neratinib administering to a patient in the form of maleate salt, where the neratinib maleate salt is a crystalline monohydrate of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide maleate (Form II). The invention also relates to a method for cancer treatment including neratinib administering to a patient in the form maleate salt (Form II).EFFECT: increased oral absorption and cancer treatment based on the use of a crystal form of neratinib maleate salt.7 cl, 8 dwg, 11 tbl, 2 ex
Amorphous (5-fluoro-2-methyl-3-quinolin-2-ylmethylindol-1-yl)-acetic acid // 2616000
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a stable solid dispersion (5-fluoro-2-methyl-3-quinolin-2-ylmethylindol-1-yl)-acetic acid (Compounds 1), containing amorphous (5-fluoro-2-methyl-3-quinolin-2-ylmethylindol-1-yl)-acetic acid (Compound 1) or its pharmaceutically or veterinarily acceptable salt and polymer, selected from polyvinylpyrrolidone (PVP), polyvinylpyrrolidone-vinyl acetate copolymer (PVP-VA), hydroxypropyl methylcellulose (HPMC) and hypromellose acetate succinate (HPMC AS) and their mixtures. Invention also relates to a method of producing said stable solid dispersion, its application, method of treating said diseases and pharmaceutical composition based on stable solid dispersion.EFFECT: obtaining a stable solid dispersion based on amorphous compound 1 and polymer, useful for treating or preventing diseases mediated by prostaglandin D2 (PGD2) or other agonists, acting on CRTH2 receptor.22 cl, 17 dwg, 15 tbl, 13 ex

7-{(3s,4s)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal // 2615509
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular, to a hydrochloride salt crystal, a hydrochloride salt hydrate crystal and methane sulphonate salt crystal 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid. Invention also relates to an antibacterial pharmaceutical preparation based on said crystal, a method of producing said crystals.EFFECT: technical result: obtained crystals have high solubility in water, as well as high storage stability.19 cl, 6 dwg, 4 tbl, 13 ex
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 ex
Compounds having antagonistic activity towards muscarinic receptors and agonist activity to beta2-adrenoreceptors // 2606121
FIELD: chemistry.SUBSTANCE: present invention relates to compounds of general formula (I), acting as muscarinic receptors antagonists or beta2-adrenoreceptors agonists, as well as to pharmaceutical compositions based thereon and to therapeutic applications for preparing a medicine to prevent and treat diseases, such as asthma, chronic bronchitis, etc.EFFECT: obtained are novel compounds of formula (I) having activity towards muscarinic receptors or beta2-adrenoreceptors.13 cl, 5 tbl, 39 ex, 2 dwg

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

3-carboxy-4-aminoquinoline derivates, useful as sweet taste modifiers // 2605549
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel quinoline derivatives of general formula (IIIb) or ingestible salt thereof, where A is NH2; B is C1-C4 alkyl; C is -CO2R7; R7 is hydrogen; L1 is C1-C8 alkylene, C6-cycloalkylene or -CH2-C6-cycloalkylene; L2 is -O-, NR34-C(O)-, -C(O)-NR34-, -(3-6-member heterocyclylene-C(O))-group, where heterocyclylene contains one nitrogen atom; R33 is C1-C6 alkyl, optionally substituted C1-C6 alkoxy or hydroxy, C3-C10 carbocyclyl, optionally substituted with one C1-C6 alkoxy, C6-C10 aryl, optionally substituted with one or two substitutes, selected from -OH, halogen, -C(=O)NH2, -C(=O)NHC1-6 alkyl, C1-C6 alkoxy, C1-C6 alkyl-OH and O-C1-C6 alkyl-OH, C6-C10 aryl C1-C4 alkyl, optionally substituted C1-C6 alkoxy, 5-10-member heterocyclyl containing 1 or 2 oxygen atoms, pyridine or pyridine-C1-C4 alkyl; and R34 is hydrogen. Invention also relates to quinoline derivatives of formula (IIIc) and (IIIc'), specific quinoline derivatives, ingestible composition based on compounds of formula (IIIb), (IIIc) and (IIIc'), method of enhancing sweet taste of ingestible composition, method of producing intermediate compounds of formulae (IV) and (IVc).EFFECT: novel quinoline derivatives, useful as sweet taste modifiers.23 cl, 23 tbl, 133 ex, , ,

New derivatives of 3,3-dimethyltetrahydroquinoline // 2603276
FIELD: chemistry.SUBSTANCE: invention is related to organic chemistry and specifically to new tetrahydroquinolin derivatives of general formula (I) or pharmaceutically acceptable salts or esters where R1 represents hydrogen, halogen, carboxyl, alkoxycarbonyl, alkilsulphonylaminocarbonyl or cycloalkylalkilsulphonylaminocarbonyl; R2 represents hydrogen, halogen or carboxyl; R3 represents hydrogen, halogen, carboxyl, halogenalkyl, cyano, alkoxycarbonyl, alkylsulphonyl, alkylsulphonylaminocarbonyl, cycloalkylalkilsulphonylaminocarbonyl, carboxylalkylamino(alkyl)carbonyl, alkyl(hydroxy)pyrrolidinylcarbonyl or carboxylpyrrolydincarbonyl; R4 is hydrogen, carboxyl, alkilsulphonylaminocarbonyl or cycloalkylalkilsulphonylaminocarbonyl; R5 is pyridinyl, substituted pyridinyl, morphonylpyrinidil, phenyl or substituted phenyl, where substituted pyridinyl and substituted phenyl represent pyridinyl and phenyl, substituted with one or two substitutes given in the patent claim; where the alkyl, one or in combination, is saturated alkyl group with linear or branched chain containing 1 to 6 carbon atoms; alkoxy, one or in combination, denotes a group of alkyl-O-, where the alkyl such as defined above; cycloalkyl, one or in combination, relates to saturated carbon ring, containing from 3 to 6 carbon atoms; provided that 3,3-dimethyl-2-phenyl-1,2,3,4,6-hydroxyl-2,2,4-trimethyl-1,2,3,4-tetrahydroquinline is excluded. Invention is also related to specific compounds, pharmaceutical composition based on compound of formula (I), use of formula (I) and a method of treating or preventing diseases based on use of compounds of formula (I).EFFECT: technical result is obtaining novel tetrahydroquinolin derivatives, useful as activator AMR-activated protein kinase (AMPK).17 cl, 236 ex

Cyanoquinoline derivatives // 2600928
FIELD: chemistry.SUBSTANCE: invention relates to novel cyanoquinoline derivatives of general formula I, as well as to stereoisomers, cis-trans-isomers or pharmaceutically acceptable salts thereof, where R1 is selected from a group consisting of 4-bromobut-2-enamide, 4-(dimethylamino)but-2-enamide, acrylamido, but-2-enamide, 3-methylbut-2-enamide, 2-(1-tert-butoxycarbonylpiperidin-4-ylidene) acetamide, 2-(piperidin-4-ylidene)acetamide, 2-(1-methylpiperidin-4-ylidene) acetamide, 2-(1-ethylpiperidin-4-ylidene) acetamide, 2-(1-benzylpiperidin-4-ylidene) acetamide, 2-(1-(2-methoxyethyl) piperidin-4-ylidene)acetamide, 2-(1-(2-methoxycarbonylmethylene)piperidin-4-ylidene)acetamide, 2-(1-isopropylpiperidin-4-ylidene) acetamide, 2-(1-(2-hydroxyethyl)piperidine-4-ylidene)acetamide, 2-(pyrrolidin-3-ylidene)-acetamide, N-(N-(2-(2-(dimethylamino)ethoxy)ethyl)amino)fumaramide, 2-(1-(2-(2-(2-hydroxyethoxy)ethylamino)acetyl) piperidin-4-ylidene)acetamide, 2-((1-methylsulphonyl)piperidin-4-ylidene) acetamide, 4-(piperidin-1-yl)but-2-enamide, 4-(morpholin-4-yl)but-2-enamide, 4-(tert-butylamino)but-2-enamide, 4-(benzylamino)but-2-enamide, 4-(6-hydroxyhexylamino)but-2-enamide, 4-(N-methylbenzylamino)but-2-enamide, 4-(diethylamino)but-2-enamide, 4-(2-methoxyethylamino)but-2-enamide, 4-(diethanolamino)but-2-enamide, 4-(N-methylmethoxyethylamino) but-2-enamide, 4-(N-methyl-ethanolamino)but-2-enamide, 4-(dimethoxyethylamino)but-2-enamide, 4-(N-methyl-6-amino-1-hexanolyl)but-2-enamide and propylamide; one of R2 and R3 is H, while other is selected from unsubstituted C6-aryl-C1-2-alkyl, substituted with 1-2 substitutes or unsubstituted C6-aryl and substituted with 1 substitute or unsubstituted 6-9-member heteroaryl, where, when R2 or R3 is selected from a substituted C6-aryl, substitute is selected from C2-C6-alkynyl, halogen, C6-aryl-C1-alkyloxy (where said C6-aryl can be substituted with 1 substitute selected from halogen, cyano, C1-C6 alkyl, C1-C-6 alkoxy), and 6-member heteroaryl-C-1-alkyloxy, and when R2 or R3 are selected from a substituted heteroaryl, substitute is selected from a group comprising C6-aryl-C1-alkyl (where said C6-aryl is optionally substituted with 1 substitute selected from halogen and cyano, methoxy group), C6-arylamido (where the said C6-aryl can be unsubstituted or substituted with 1 dimethylamino group), C6-arylsulphonylamino, C5-heteroarylamido, C6-cycloalkylamido, C6-arylaminocarbonyl (where said C6-aryl is substituted with 1 methoxy group), C6-aryl-C1-alkyloxy and C6-aryloxy; or R2 and R3, together with a nitrogen atom to which they are bonded, form a substituted or unsubstituted 9-10-member heterocyclyl, where heterocycyl substitutes are selected from halogen, C1-C-6 alkyl, CF3, C6-aryl-C1-alkoxy, -COOMe, -CH2OH and pyrrolyl; and R4 is substituted with 1 methyl or unsubstituted 5-6-member heterocyclyl or unsubstituted 6-member heteroaryl. Invention also relates to specific compounds, pharmaceutical composition based on compound of formula I and use of formula I.EFFECT: technical result is obtaining novel cyanoquinoline derivatives which are useful in treating tumours.33 cl, 20 tbl, 228 ex

New substituted quinoline compounds as inhibitors of s-nitrozoglutation-reductase inhibitors // 2599144
FIELD: chemistry.SUBSTANCE: invention is related to organic chemistry and specifically to novel quinoline derivatives of general formula I or pharmaceutically acceptable salts, stereoisomers or N-oxides, where m = 0 and 1; R1 is independently selected from a group consisting of chlorine, fluorine and bromine; R2b and R2 c are independently selected from a group, consisting of hydrogen, halogen, C1-C3 alkyl, fluorinated C1-C3alkyl, cyano and N (CH3)2; X is selected from a group consisting of n is selected from a group consisting of 0 and 1; R3 is independently selected from a group consisting of halogen, C1-C3 alkyl, fluorinated with1-C3 alkyl, cyano, C1-C3alkoxy and NR4R4′, where R4 and R4′ are independently selected from a group consisting of C1-C3 alkyl; and a is selected from a group consisting of .Invention is also related to the use of formula I, pharmaceutical composition based on the compound of formula I, method of treating pulmonary disorders and inflammatory diseases based on use of the compound of formula I, and a method of producing a pharmaceutical composition based on the compound of formula I.EFFECT: technical result is obtaining novel quinoline derivatives, useful as inhibitors of S-nitrozoglutation reductase (GSNOR).17 cl, 64 ex

Triazolopyrine compounds as kinase inhibitors pim // 2598846
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I, their stereoisomers and pharmaceutically acceptable salts thereof, in which R1, R2, R3, R4 and R10 assume values given in the patent claim. Declared compounds are inhibitors of kinase tyrosine kinases PIM-1, and/or PIM-2, and/or PIM-3 and can be used in treating diseases mediated by said kinase. Invention also relates to a pharmaceutical composition based on them, methods of producing the declared compounds and an intermediate compound used in production of the declared compounds.EFFECT: disclosed are compounds of Formula I, their stereoisomers and pharmaceutically acceptable salts.56 cl, 6 tbl, 11 ex biological researches (A-K), 6 receptions of, 328 ex

Quinoline-2-amine derivatives, useful for treating aids // 2598845
FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry, namely to new quinoline-2-amine derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where X represents CR0 or N, i.e. together with the ring it belongs to it forms respectively a benzene or a pyridine group, R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom , a halogen atom or a group selected from a (C1-C5)alkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a -NRaRb group, a -NRa-SO2-NRaRb group, a -NRa-SO2-Ra group and may additional represent a group selected from (IIa) or (IIIa); A represents an oxygen atom, B is a covalent bond, n equals 1, 2 or 3, m equals 1, 2 or 3, R, R′, Rand R andb independently represent a hydrogen atom or (C1-C5)alkyl group, R and R′ can further form with a nitrogen atom, to which they are bonded, saturated 5-or 6-member heterocycle, possibly containing one more heteroatom O, R5 is a hydrogen atom or (C1-C5)alkyl group, R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom under the conditions specified in CL. 1. Invention also relates to specific quinoline-2-amine derivatives and a pharmaceutical composition based on the compound of formula (I).EFFECT: technical result: there are new quinoline-2-amine derivatives, useful for treating AIDS.14 cl, 2 tbl, 6 ex , ,

Substituted benzamide derivatives // 2595902
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (I), where R is hydrogen or C1-7alkyl; R1 represents -(CH2)n-(O)o-5-7-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, except for piperazine, where said heterocycloalkyl group optionally substituted with C1-7alkyl, hydroxy or halogen; n equals to 0, 1 or 2; o equals to 0 or 1; R2 represents CF3, C3-6-cycloalkyl, possibly substituted C1-7alkoxy or halogen, or represents indane-2-yl, or is 6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, optionally substituted with pyrimidinyl, or is 5-6 mono- or 9-10-member bicyclic heteroaryl containing 1-2 heteroatoms selected from N, O and S, where the heteroaryl is not thiazol and where said aromatic ring, is possibly substituted with one or two substitutes selected from C1-7alkyl, halogen, 5-6-member heteroaryl containing 1-2 heteroatoms selected from N and O, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2Cl)(CH3), S-C-1-7alkyl, C1-7alkoxy, CH2-C-1-7alkoxy, C2-7alkynyl or cyano, or substituted with -C(O)-phenyl, -O-phenyl, -O-CH2-phenyl, phenyl, and where said phenyl ring may be substituted with halogen, -C(O)OH or -C(O)O-C-1-7alkyl, or said aromatic ring, is possibly substituted with 5-6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, OCH2-oxetane-3-yl or O-tetrahydropyran-4-yl, possibly substituted C1-7alkyl; X is bond, -CH2NH-, -CHR″-, -(CHR″)q-O-, -O-(CHR″)q- or -(CH2)2-; Y is bond; R″ is hydrogen, C1-7alkyl, CF3, C1-7alkoxy; q is equal to 0, 1, 2 or 3; or pharmaceutically acceptable acid addition salt thereof, except for compounds specified in patent claim. Invention also relates to specific compounds specified in patent claim. Compounds are intended for producing medicinal agents, showing affinity to TAAR1.EFFECT: technical result: benzamide derivatives having high affinity to receptors associated with TAAR1 trace amines.9 cl, 1 tbl, 323 ex

Substituted 2-oxy-quinoline-3-carboxamides as kcnq2/3 modulators // 2595894
FIELD: chemistry.SUBSTANCE: invention relates to substituted 2-oxy-quinoline-3-carboxamides of general formula (I) in form of free compounds or salts of physiologically acceptable acids or bases, where R1 is C1-6-aliphatic residue; 6-member unsubstituted or mono- or disubstituted aryl or unsubstituted 5-member heteroaryl, selected from a thienyl; R2 is CF3; C1-4-aliphatic residue; O-C1-4-aliphatic residue; R3, R4, R5 and R6 each independently represent H; F; Cl; Br; I; CN; CF3; R7 is C1-6-aliphatic residue, unsubstituted or mono- or trisubstituted; where "aliphatic residue" in each case may be branched or straight, saturated, where "mono- or trisubstituted" with respect to "aliphatic residue" relates, in relation to corresponding residues, to substitution of one or three hydrogen atoms, each independently from other, with at least one substitute selected from a group which includes F, Cl, Br, I, OH, O-C1-4-aliphatic residue, where "mono- or disubstituted" with respect to "aryl" relates, in relation to corresponding residues, to substitution of one or two hydrogen atoms, each independently from other, with at least one substitute selected from a group which includes F, Cl, Br, I, OH, O-C1-4-aliphatic residue C1-4-aliphatic residue. Invention also relates to a pharmaceutical composition based on compound of formula (I) and a method of treating and/or preventing diseases mediated by channels KCNQ2/3 K+.EFFECT: obtaining novel 2-oxy-quinoline-3-carboxamide derivatives having useful biological activity.8 cl, 2 tbl, 53 ex

Pi3-kinase inhibitors and use thereof // 2595718
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds which are irreversible PI3-kinase inhibitors, and conjugates containing one or more PI3-kinases, containing cysteine residue, which is covalently and irreversibly boned with PI3-kinase inhibitor. Invention also discloses pharmaceutical compositions containing said compounds.EFFECT: compounds are intended for treating disorders and diseases associated with PI3-kinase.19 cl, 16 dwg, 26 tbl, 52 ex

Catechol-o-methyl transferase inhibitors and use thereof in treating psychotic disorders // 2586974
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to derivatives of 4-pyridinone formula I or pharmaceutically acceptable salts thereof, where A is hydrogen, B(OH)2, halogen, C(O)NH(CH2)nC(O)N(R3)2; X is hydrogen or halogen; Y denotes phenyl, benzimidazolil, benztiazolil, benzoksazolil, benzpiperidinil, quinolyl, indolyl, indazolyl or pyridyl, each optionally substituted with 1-3 groups Ra, provided that Y denotes phenyl, then at least one of said Ra selected from OCF3, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)n(C)6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, where said heterocyclic ring and aryl optionally substituted with 1-3 groups Rb; R1 represents hydrogen, NR2R3, Si(CH3)3, (CH2)nC6-10aryl, C2alkenyl or C1-4alkyl, said alkyl and alkenyl optionally substituted with 1-3 groups of halogen, OH, C1-6alkyl, O-C1-6alkyl, NR2R3, SOR2, NHSO2R2, CF3, C6-10aryl, heterocyclyl, -C≡C-C6-10aryl, C(O)NR2R3, wherein said aryl and heterocyclyl optionally substituted with 1-2 groups Ra; R2 and R3 independently denote H, C1-6alkyl, (CH2)nheterocyclyl, (CH2)nC6-10aryl, wherein said aryl optionally substituted by group Ra or R2 and R3 together with nitrogen atom to which they are bonded, form a 6-member ring, which contains oxygen; Ra is C1-6alkyl, halogen, CF3, OCF3, C3-6cycloalkyl, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, CN, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)nC6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, wherein said heterocyclyl and aryl optionally substituted with 1-3 groups Rb; Rb is C1-6alkyl, halogen, CHF2, oxo (=O), N(R2)2, CH2OH, S(O)2NR2R3, (CH2)nC6-10aryl, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, OR2, C3-6cycloalkyl, CF3 or CN; and n equals 0-3; and where heterocycle is aromatic or saturated or partially saturated monocyclic or bicyclic ring containing 5-10 atoms, among which 1-4 atoms are heteroatoms selected from nitrogen, oxygen and sulphur. Invention also relates to pharmaceutical composition based on compound of formula I, method of treating and/or preventing neurological and psychiatric disorders and method of intensifying action of antipsychotic agent based on use of compound of formula I.EFFECT: new compounds are prepared effective in treating diseases associated with catechol-O-methyltransferase (COMT).52 cl, 1 tbl, 17 ex

Synthesis and anticancer activity of derivatives of aryl and heteroaryl quinolines // 2584688
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I and pharmaceutically acceptable salts thereof , where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 is (C1-C6)alkoxy, hydroxyl or OR8; R6 is hydroxyl or (C1-C6)alkoxy; R7 represents hydrogen, hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents a RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion; or where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 represents hydrogen, (C1-C6)alkoxy, hydroxyl or OR8; R6 is (C1-C6)alkoxy; R7 is hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents PO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion. Disclosed compounds have anti-cancer activity. Invention also relates to compounds of formula I, radicals of which are presented in patent claim and to using pharmaceutical composition containing effective amount of compound of invention for treating cancer.EFFECT: technical outcome is new compounds possessing anticancer activity.17 cl, 23 dwg, 7 tbl, 4 ex

Pharmaceutically acceptable salt (e)-n-[4-[[3-chloro-4-(2-pyridylmethoxy) phenyl] amino] -3-cyano-7-ethoxy-6-quinolyl] -3-[(2r)- 1- methylpyrrolidin-2-yl] prop-2-enamide, method for production and use thereof in treating cancer // 2583056
FIELD: pharmaceutics.SUBSTANCE: invention relates to a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide (formula (I)), where n equals 1, 2 or 3; and M is a molecule of acid, where said salt is selected from group consisting of hydrochloride, para-toluene sulphonate, methanesulphonate, maleate, succinate and L-malate. Invention also relates to method of producing salt of formula (I), pharmaceutical composition based on salt compound of formula (I) and use of salt compound of formula (I).EFFECT: novel salt of compound of formula (I) effective in treating cancer.10 cl, 7 tbl, 13 ex
Heteroarylsulphonamide derivatives, production and use thereof for human treatment // 2582995
FIELD: chemistry.SUBSTANCE: invention relates to geteroarilsulfonamide derivatives of formula I, where R1 is a substituent of the phenyl nucleus X selected from the group consisting of: hydrogen, F, Cl, Br, trifluoromethyl, trifluoromethoxy group, a linear or branched C1-C4-alkyl, linear or branched C1-C4 alkoxy group; n is 0, 1 or 2; A is oxygen or sulfur; D is -C (=O)-, -CH2O- or -O-; B is a nitrogen atom if n = 1 or 2, and D is -C(=O) -, or B is CH, if n = 0, and Dis -CH2O-, or if n = 1, D is -O-; R2 is hydrogen, and HetAr is pyridyl or quinolyl, optionally containing a substituent which is a linear or branched C1-C4-alkyl or trifluoromethyl; or pharmaceutically acceptable salts thereof. Invention also relates to the methods for producing compounds of formula I and to the pharmaceutical composition containing a therapeutically effective amount of the compound of formula I. EFFECT: technical result is geteroarilsulfonamide derivatives of formula I, with blocking activity to Kv1,5 potassium channels.12 cl, 1 tbl, 35 ex
Quinoline derivatives and melk inhibitors containing same // 2582610
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to a heterocyclic compound of general formula (I) or its pharmaceutically acceptable salt thereof, where: R1 is C1-C6 alkyl sulphonyl or -CO-R5, where R5 is C1-C-6 alkyl or C3-C5 cycloalkyl; R2 represents phenyl which can contain group substitute selected from group of substitutes C, or -NR6AR7A, where R6A is hydrogen atom and R7A is -(CH2)n-R10A (where n equals whole number from 0 to 2 and R10A represents mono- or tricyclic C3-C10 cycloalkyl, which can contain group substitute selected from group of substitutes D, phenyl, which can contain group substitute selected from a group of substitutes E, aliphatic heterocyclic group which is selected from piperidinil, piperazinil and azabicyclooctanil and can be substituted C1-C-6 alkyl, aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl and pirazolil and can contain group substitute selected from a group of substitutes I), or R6A and R7A is formed with adjacent nitrogen atom aliphatic heterocyclic group that is selected from piperidinil and piperazinil and may contain group substitute selected from a group of substitutes F; R3 is C6-C10 aryl, which can contain group substitute selected from a group of substitutes G, or aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl, tiofenil, isoxazolyl, pyrrolyl and pirazolil and can contain group substitute selected from a group of substitutes H; R4 is hydrogen atom or halogen; R is hydrogen atom or halogen; and R101 is hydrogen atom; where said substitutes C - I are one-three substitutes are given in claim. Invention also relates to pharmaceutical composition, an inhibitor of MELK, agent, which simulates the expression MELK, anticancer agent based on compounds of formula (I), method of treating and/or preventing diseases, which includes MELK overexpression, using compound of formula (I).EFFECT: obtained are novel heterocyclic compounds effective as anti-tumour agent.19 cl, 4 tbl, 1200 ex

Substituted 2-oxo- and 2- thioxo- dihydroquinoline-3-carboxamides as kcnq2/3 modulators // 2581362
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to organic chemistry, namely to derivative 2-oxo- and 2-thioxodihydroquinoline-3-carboxamides of formula in the form of free compounds, or in the form of salts of physiologically acceptable acids or bases, wherein X means O or S, R1 represents an unsubstituted C1-7-aliphatic residue; or aryl specified in phenyl unsubstituted or monosubstituted by at least one substitute specified in a group, which contains F, Cl, Br; R2 represents CF3; C1-4-aliphatic residue or O-C1-4-aliphatic residue, wherein C1-4 aliphatic residue in each case is unsubstituted; each R3, R4, R5 and R6 independently represents H; F; Cl; Br; CN; CF3; OCF3; provided at least one of R3, R4, R5 and R6 does not represent H; R7 represents C1-7-aliphatic residue unsubstituted, or mono- or disubstituted; or 6-merous heterocycloaliphatic residue specified in tetrahydropyrane; wherein the 'aliphatic residue' in each case can be branched or unbranched, saturated; wherein 'mono- or disubstituted' in relation to the 'aliphatic residue' refers in the view of respective residues or groups, to substitution of one or two hydrogen atoms specified in one or two hydrogen atoms, each independently, by at least one substitute specified in a group, which contains OH, O-C1-4-aliphatic residue, COOH or C(=O)-O-C1-4-aliphatic residue. The invention also refers to a pharmaceutical composition based on the compound of formula (I).EFFECT: new compounds effective in treating and/or preventing diseases mediated by KCNQ2/3 K+ canals are produced.8 cl, 2 tbl, 45 ex

Eye medicinal film with moxifloxacin // 2581025
FIELD: medicine.SUBSTANCE: invention refers to medicine, particularly to ophthalmology, and can be used in preoperative and postoperative prevention and treatment of infectious inflammatory complications following abdominal operations on eyeball. Eye film comprises polyvinyl alcohol, dihydroquercetin as an active substance of vegetable origin, moxifloxacin as an antibiotic. Invention increases range of therapeutic action of film by giving it strong antioxidant, anti-inflammatory, immunomodulatory properties, provides long-term effect eye film.EFFECT: eye medicinal films with moxifloxacin are easy to use, have prolonged antimicrobial, antioxidant, immunomodulatory, anti-inflammatory properties.1 cl, 1 dwg

Aminopyrazole derivative // 2580543
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound, which has formula presented below, or a pharmaceutically acceptable salt thereof. This compound can inhibit fibroblast growth factor receptor (FGFR) kinases in tumour tissues. In formula (I) A means a heteroaryl specified in indole, azaindole, benzofuran, benzothiophene, benzorhiazole, quinoline and pyrrole, or a benzene ring; R1 particularly means hydrogen, hydroxy, halogen, cyano, C1-4 haloalkyl, C1-6 alkyl, C2-6 alkinyl; R2 particularly means hydrogen, hydroxy, halogen, cyano, C1-4 haloalkyl, C1-6 alkyl, C2-6 alkinyl, C3-7 cycloalkyl, phenylC1-4 alkyl, or R1 and R2 together with a nitrogen atom connected thereto form a 5-6-merous heterocyclyl group containing two oxygen atoms optionally substituted by a halogen; R3 means H, C1-5 alkyl group, phenylC1-5 alkyl group or C1-4 haloalkyl group; and R4 means H or halogen.EFFECT: invention refers to a pharmaceutical composition and an agent for FGFR inhibition, an agent for preventing or treating a malignant new growth, a method for preventing or treating malignant new growths, and the use of the compounds for producing a medicinal agent for preventing or treating malignant new growths.10 cl, 35 tbl, 246 ex

1-hydroxyimino-3-phenyl-propanes // 2579114
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to 1-hydroxyimino-3-phenyl-propane derivatives of formula I, wherein R1 represents -(CH2)m-phenyl, m is equal to 0, and phenyl is substituted by 1-3 groups independently specified in C1-7-alkyl or hydroxy, or -(CH2)n-heteroaryl, wherein n is equal to 0 or 1, and heteroaryl is specified in pyridine, 1H-pyridin-2-one, 1-oxy-pyridine, 1H-pyrimidin-2-one, quinoline and pyrazine, and is ubsubstituted or substituted by 1-3 groups specified in the patent claim; R2 represents hydrogen or C1-7-alkyl, or when R4 represents hydrogen, R2 represents phenyl optionally substituted by C1-7-alkyl; R3 represents hydrogen; R5 represents hydrogen or hydroxy; or R3 and R5 are substituted by a double bond; R4 is specified in a group consisting of C1-7-alkyl, C3-7-cycloalkyl, C2-7-alkenyl, halogen-C1-7-alky, optionally substituted phenyl, optionally substituted phenyl-C1-7-alkyl, 5-9-merous heteroaryl containing 1-2 heteroatoms specified in N and S optionally substituted by C1-7-alkyl or oxo, and piperidinyl optionally substituted by C1-7-alkyl, or R4 and R5 together with a carbon atom to which they are attached, form a C3-7-cycloalkyl ring; R6 represents hydrogen halogen; or R4 and R6 together with a carbon atom to which they are attached, form a cyclic group G , wherein m represents 0 or 2; R7 - R9 are those as specified in the patent claim; R10 is specified in hydrogen, halogen and C1-7-alkyl; or their pharmaceutically acceptable salts. The invention also refers to specific compounds specified in cl. 19 of the patent claim, a method for producing the compounds I, a pharmaceutical composition, a method of treating diabetes and using the compounds for producing a medicinal agent.EFFECT: 1-hydroxyimino-3-phenyl-propane derivatives possessing GPBAR1 agonist activity and effective in treating diabetes.26 cl, 516 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

Aryl-substituted carboxamide derivatives as calcium or sodium channel blockers // 2575168
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to aryl-substituted carboxamide derivatives of formula (I)or their pharmaceutically acceptable salts, wherein in formula (I) R represents hydrogen; R1 is independently specified in a group consisting of: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -On-C1-6 alkyl, wherein alkyl is unsubstituted or substituted by one or more substitutes optionally specified in R7, (5) -On-heterocylic group specified in piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl and oxetanyl; n has the value of 0 or 1; when n has the value of 0, a chemical bond is present instead of On; p has the value of 1 or 2; when p is equal to two, R1 can be identical or different from each other; R2 represents C1-6 alkyl, which is unsubstituted or substituted by one or more substitutes, independently specified in R7; or R2 together with R1 forms C3-C6 cycloalkyl; X represents 1,2-C3 cycloalkylene; W, Y and Z are independently specified in nitrogen atom or carbon atom; at least one of W, Y and Z represents nitrogen, and simultaneously W, Y and Z are other than carbon; R3, R4, R5 and R6 are such as presented in the patent claim; Ar means aryl, which represents mono- or bi-carbocyclic or mono or bi-heterocyclic ring containing 0-3 heteroatoms specified in O, N and S, including phenyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyridyl, piperidinyl, pyrimidinyl, isooxazolyl, triazolyl, tetrahydronaphthyl, benzofuranyl, benzothiophenyl, indolyl, benzoimidazolyl, quinolyl, isoquinolyl, quinoxalinyl, pyrazolo [1,5-a] pyridyl, thieno [3,2-b] pyrrolyl, wherein aryl is optionally substituted by 1-3 substitutes specified in the patent claim. Also the invention refers to compounds of formula (II)and their aryl-substituted carboxamide derivatives specified in cl. 3 of the patent claim, a pharmaceutical composition, a method of treating and using.EFFECT: aryl-substituted carboxamide derivatives exhibiting blocking activity on T-type calcium channels or voltage-dependent channels.10 cl, 6 tbl, 464 ex

Pharmaceutically active compounds as axl inhibitors // 2573834
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound of structural formula (I) possessing inhibitory activity on the TAM family of receptor tyrosine kinases (RTKs). In formula (I) A represents C-R10; B represents C-R11, N; R1, R4 are independently specified in -H, -F, -Cl, -Br, -I, -OH, -NH2, -OCH3, -OC2H5, -OC3H7, -OCH(CH3)2, -NO2, -CHO, -COCH3, -COC2H5, -COC3H7, -O-cyclo-C3H5, -OCH2-cyclo-C3H5, -O-C2H4-cyclo-C3H5, -OCF3, -OC2F5, -CH2F, -CHF2, -CF3, -CH2Cl, -CH2Br, -CH2I, -CH2-CH2F, -CH2-CHF2, -CH2-CF3, -CH2-CH2Cl, -CH2-CH2Br, -CH2-CH2I, cyclo-C3H5, -CH2-cyclo-C3H5, -CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -CH=CH2, -CH2-CH=CH2, -C(CH3)=CH2, -CH=CH-CH3; R2 are R3 are independently specified in -O-R18, -O-CR73R74-R18, -O-CR73R74-CR75R76-R18, -O-CR73R74-CR75R76-CR77R78-R18, -O-CR73R74-CR75R76-CR77R78-CR79R80-R18; R5 and R6 represent -H; R7, R8, which can be identical or different from each other, represent -H, -F, -Cl, -Br, -I, -CN, -NO2, -CH3, -C2H5, -C3H7, -CH(CH3)2, cyclo-C3H5, -CH2-cyclo-C3H5, -OCH3; R9 represents -H. The radical values D, R10, R11, R18, R73-R80 are presented in the patent claim. The invention also refers to a pharmaceutical composition containing the above compound.EFFECT: producing the compounds possessing the inhibitory activity on the TAM family of receptor tyrosine kinases (RTKs).14 cl, 3 tbl, 106 ex

Quinolyl-containing compound of hydroxamic acid, method for thereof obtaining and application in treatment of diseases, caused by abnormal proteinkinase and/or hystone deacetylase activity // 2573633
FIELD: chemistry.SUBSTANCE: claimed invention relates to field of organic chemistry, namely to novel quinolyl-containing compounds of hydroxamic acid of general formula (I), wherein each of V1 and V2 independently represents halogen; one of R and R' represents group Q, containing hydroxamic acid, and the other represents methoxy, wherein group Q, containing hydroxamic acid, is represented by formula ; A represents O; L represents C1-6alkyl; J represents NH, piperidinyl, or J is absent; X is absent; Y represents C1-6alkyl, or Y is absent. The invention also relates to method for obtaining formula (I) compound, pharmaceutical composition, based on formula (I) compound and its application for treatment of diseases, caused by proteinkinase and/or histone deacetylase activity.EFFECT: novel compounds, which can be applied in cancer treatment, have been obtained.25 cl, 7 dwg, 7 tbl, 45 ex

Derivatives of (4-methylsulphonylaminophenyl)-quinoline, useful in treatment of hepatitis c // 2572835
FIELD: chemistry.SUBSTANCE: invention relates to field of organic chemistry, namely to compound, selected from the group of N-{4-[7-tert-butyl-8-methoxy-5-(2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]phenyl}-methanesulphonamide; N-{4-[7-tert-butyl-8-methoxy-5-(6-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]-phenyl}- methanesulphonamide; and N-{4-[7-tert-butyl-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-8-methoxy-quinolin-2-yl]-phenyl}- methanesulphonamide; or to its pharmaceutically acceptable salt. The invention also relates to application of said compound for treatment or prevention of infection with hepatitis C virus (HCV) and for manufacturing thereof based medication.EFFECT: novel compounds, possessing useful biological activity have been obtained.5 cl, 2 tbl, 6 ex

Oxazoline derivatives for treating cns disorders // 2569887
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound of formulawherein Ra represents hydrogen or C1-7alkyl; R1 represents groups and or may be specified in a group consisting of , wherein R8 represents hydrogen, halogen or aryl optionally substituted by halogen; X represents a bond, -(CH2)n-, -CHRCH2-, -CHR(CH2)2-, -O-CHRCH2- or -(C3cyclopropyl)-CH2-CH2-, and R represents C1-7alkyl or C1-7alkyl substituted by halogen; R2 represents a) C1-7alkyl; b) hydrogen; c) NH-phenyl optionally substituted by one or more substitutes specified in halogen or C1-7alkyl substituted by halogen; d) NH-6-merous heteroaryl containing 1 or 2 heteroatoms N optionally substituted by one or more substitutes specified in halogen or C1-7-alkyl substituted by halogen; e) (CR'R")m-C3-6-cycloalkyl optionally substituted by halogen, C1-7alkyl, C1-7alkyl substituted by halogen, halogen-substituted phenyl or heteroaryl, which represents pyridine; f) 6-merous heterocycloalkyl containing 1 or 2 heteroatoms specified in N and O, optionally substituted by halogen or C1-7alkyl substituted by halogen; g) (CR'R")m-5-6-merous monocyclic or 9-10-mrous bicyclic heteroaryl containing 1-3 heteroatoms specified in N, S and O, optionally substituted by halogen, C1-7alkoxy, C1-7alkyl, substituted by halogen, C1-7alkoxy substituted by halogen, C1-7alkyl, C3-6-cycloalkyl, NHC(O)-C1-7alkyl, cyano, S(O)2-C1-7alkyl, NR6R7 or 5-6-merous heteroaryl containing 1 or 2 heteroatoms, N or 6-merous heterocyclyl containing 1 or 2 heteroatoms specified in N, O and S, wherein S is optionally specified by two oxygen molecules, which is optionally substituted by halogen; h) (CR'R")m-phenyl optionally substituted by halogen, C1-7alkyl substituted by halogen, C1-7-alkoxy substituted by halogen, C1-7alkyl, C2-7alkinyl, C1-7alkoxy, CH2-C1-7alkoxy or cyano; i) -O(CH2)o-phenyl optionally substituted by halogen, C1-7alkoxy or C1-7alkyl substituted by halogen; R' and R" independently represent hydrogen, C1-7alkoxy or C1-7alkyl; or together with atom C may form C3-6-cycloalkyl group; R3 represents phenyl or 10-merous heteroaryl containing 1 heteroatom N, wherein the above aromatic rings are optionally substituted by one or more substitutes specified in halogen or C1-7alkoxy; R4 represents C1-7alkyl, phenyl or 6-merous heteroaryl containing 1 heteroatom N, wherein the above aromatic rings are optionally substituted by one or more substituted specified in halogen, cyano or C1-7alkoxy; R5 represents hydrogen, C1-7alkyl or phenyl substituted by halogen; R6/R7 independently represent hydrogen, C1-7alkyl or (CH2)2-O-C1-7alkyl; m equals to 0, 1 or 2; n equals to 1, 2 or 3; o equals to 0 or 1; p equals to 0, 1 or 2; or their pharmaceutically acceptable acid addition salt. The invention also refers to compounds which represent 4-[2-((S)-2-amino-4,5-dihydrooxazol-4-yl)-ethyl]-N-(4-chlor-phenyl)-benzamide or (S)-4-(2-(2-amino-4,5-dihydrooxazol-4-yl)-ethyl)-N-(5-ethynylpyridin-2-yl)benzamide. The compositions according to the invention are applicable to produce a pharmaceutical composition having a high affinity to trace amine associated receptors.EFFECT: oxazoline derivatives applicable in treating depression, bipolar disorder, attention deficit/hyperactivity syndrome (ADHD), psychotic disorders, schizophrenia, Parkinson's disease, migraine and addictive substance abuse.23 cl, 1 tbl, 233 ex

Pharmaceutical compositions // 2568882
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to the pharmaceutical industry and represents a pharmaceutical composition for the treatment of a respiratory, inflammatory or obstructive disease of the respiratory tract, containing R(+) budesonide and one or more beta2-agonists, selected from albuterol, levoalbuterol, terbutaline, pirbuterol, procaterol, metaproterenol, fenoterol, bitolterol, mesylate, ritodrine, arformoterol, carmoterol, bambuterol, clenbuterol, indacaterol, milveterol, vilanterol or olodanterol, and optionally one or more pharmaceutically acceptable excipients.EFFECT: introduction of the claimed combination one time per day and reduction of side effects in the treatment of respiratory, inflammatory or obstructive diseases of the respiratory tract are provided.39 cl, 30 ex
 
2550907.
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