Quinolines and isoquinolines (A61K31/47)

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
ethod for treatment of mouth cavity candidosis with lizobakt and cyclopheron by using removable orthopedic constructions // 2642053
FIELD: medicine; dentistry.SUBSTANCE: invention refers to medicine, namely to dentistry. In method of oral candidiasis treatment in patients with removable orthopedic structures, including correction of the prosthesis basis, as well as treatment of inflamed areas of the soft tissues of the prosthetic bed with a 3 % solution of hydrogen peroxide, followed by application to the treated areas of 10 % methyluracil emulsion, according to the invention, additionally, the lysobact is given topically 1 tablet 3 times a day, slowly dissolving the drug, at the time of using the drug, the orthopedic structures are removed; 1 pill of tsikloferon taken orally once a day 30 minutes before eating; duration of the therapy course is two weeks.EFFECT: method allows to eliminate the phenomena of hyperemia, swelling and soreness, thereby improving the patients life quality with complete or partial absence of teeth.1 cl, 1 tbl
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
Bicyclic compound // 2640416
FIELD: pharmacology.SUBSTANCE: in the general formula (1) (1), A is an unbranched C1-C3 alkylene group, wherein one methylene group is optionally substituted with O or S; n is an integer from 3 to 5; each of X1 and X2 is independently CH or N; each of W1 and W2 is independently a carboxyl group or W1 is a carboxyl group and W2 is a tetrazolyl group; V is a linear or branched C1-C8 alkylene group in which one methylene group is optionally substituted by O or S; R is a group selected from the following , , where R1, R2, R3, R4 and R5 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may have a substituent group, a C1-C6 alkoxy group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkoxy group, a halogen C1-C4 alkyl group, a halogen C1-C4 vinyl group which may have a substituent group, an ethynyl group which may have a substituent group, a phenyl group which may have a substituent group on the aromatic ring, a phenoxy group which may have a substituent group on the aromatic ring, a benzyl group, which may have a substituent group on the benzene ring, a phenethyl group which may have a substituent group on the benzene ring, a benzyloxy group which may have a substituent group on the benzene ring, a benzylsulfanyl group which may have a substituent group on the benzene ring, a benzylamino group which may have a substituent group on the benzene ring, a phenyloxymethyl group which may have a substituent group on the benzene ring, a phenylsulfanylmethyl group which may contain a substituent group on the benzene ring, or a phenylaminomethyl group which may have a substituent group on the benzene ring, wherein the substituent group is indicated in the claims, m is an integer of 1 or 2 and each of Y1 and Y2 independently represents methylene, O or S, provided that they both do not represent S.EFFECT: compounds can be used to prevent or treat disorders associated with soluble guanylate cyclase, such as hypertension, pulmonary hypertension, heart failure, endothelial dysfunction, atherosclerosis, peripheral vascular disease, angina pectoris, thrombosis, myocardial infarction, erectile dysfunction or impaired renal function.9 cl, 41 tbl, 213 ex

Azadecalins condensed with heteroarylketones - glucocorticoid receptor modulators // 2639867
FIELD: medicine.SUBSTANCE: invention provides azadecalin compounds of formula ondensed with heteroarylketones, which are modulators of glucocorticoid receptors. The radicals and symbols in formula I have the definitions given in the claims. In some embodiments of the present invention, pharmaceutical composition is provided comprising a pharmaceutically acceptable excipient and a compound of formula (I). In some embodiments of the present invention, a method is provided for modulation of glucocorticoid receptors that comprises glucocorticoid receptors contacting with a compound of formula I, thereby modulating the glucocorticoid receptors, as well as a method for treatment of diseases by glucocorticoid receptors modulation, which comprises administration of a therapeutically effective amount of a formula I compound to a subject in need thereof, as a result, disease treatment takes place.EFFECT: increased efficiency of treatment.24 cl, 2 dwg, 1 tbl, 22 ex
Derivatives of 6,7-double substituted izochinolin and their application in treatment of medicinal dependence and cns diseases // 2636938
FIELD: pharmacology.SUBSTANCE: invention relates to an isoquinoline derivative of the general formula and to a pharmaceutically acceptable salt thereof a dotted bond is denoted as a possible bond; R' is H or absent, and the dotted bond is denoted as a bond; R1 and R4 are each independently selected from the group including H, halogen; R2 and R3 are both F or R2 or R3 is F, then the other radical is a lower alkyl or trifluoromethyl; and R5 is selected from the group including halogen, or when the dotted bond is denoted as a bond, then R5 can also be represented as H; with the exception of 6,7-difluoro-1,2,3,4-tetrahydro-1-methyl-isoquinoline. The invention also relates to a pharmaceutical composition based on a compound according to p.1 or 6,7-difluoro-1,2,3,4-tetrahydro-1-methyl-isoquinoline and their application.EFFECT: compounds have been obtained which are useful in the treatment of drug dependence, alcoholism or diseases of the central nervous system.13 cl, 5 ex

ethods and applications of inhibitors of proprotein convertase subtilisin/kexin, type 9 (pcsk9) // 2636820
FIELD: medicine.SUBSTANCE: proprotein convertase subtilisin/kexin 9 (PCSK9) is administered to a subject in need thereof, wherein the PCSK9 inhibitor is an antibody or an antigen-binding fragment thereof. Also, PCSK9 application is proposed for manufacture of a medicament for sepsis or septic shockr treatment. A pharmaceutical composition and a commercial package containing the PCSK9 inhibitor.EFFECT: possibility of treatment of a patient with sepsis or septic shock at doses suitable for intensive care.21 cl, 5 dwg, 7 tbl
Antibacterial agents on basis of ciprofloxacin derivatives // 2636751
FIELD: pharmacology.SUBSTANCE: invention relates to the new ciprofloxacin derivatives of a general formula (I) , having antibacterial properties.EFFECT: new ciprofloxacin derivatives of a general formula I that can be used in the function of the antibacterial agents are obtained.2 cl, 3 tbl, 14 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
Oral pharmaceutical composition for prevention or treatment of "dry eye" syndrome containing rebamipid or its precursor // 2632107
FIELD: pharmacology.SUBSTANCE: oral pharmaceutical composition for "dry eye" syndrome prevention or treatment, comprising a renamipide precursor or a pharmaceutically acceptable salt thereof in an amount of 0.5 to 1 wt % as an active ingredient. The composition is in the form of a suspension. Also an oral pharmaceutical preparation, a method for "dry eye" syndrome prevention or treatment and application of a renimidine precursor for pharmaceutical drug preparation are described. These rebamipide precursors can treat the "dry eye" syndrome with oral route of administration.EFFECT: safety and ease of use compared with conventional eye drops.10 cl, 15 dwg, 1 tbl, 28 ex

Kinases modulation and indications for its use // 2631487
FIELD: medicine.SUBSTANCE: invention can be used to treat a subject suffering from acute myeloid leukemia (AML), mediated by FMS-like tyrosine kinase 3 (Flt3) gene with internal tandem duplications (ITD) mutation. The specified subject receives an effective number of PLX3397 compound or its salts.EFFECT: invention provides treatment of patients with AML due to effective inhibition of tumour cell proliferation, activated by a mutant FLT3.10 cl, 4 tbl, 7 ex

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

Pharmaceutical composition // 2630617
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for treatment of cyclooxygenase-2 mediated diseases is described. The said composition includes, (2S)-7-tret-butyl-6-chloro-2- (trifluoromethyl)-2H-chromene-3-carboxylic acid as the active substance and a filler selected from tromethamine or meglumine. The filler is used in an amount of 0.5 wt % to 70 wt %. Two versions of the method for preparation of this composition and its application are also described.EFFECT: increased dissolution rate and oral bioavailability of the said composition, including the free form of the said compound.9 cl, 5 dwg, 16 tbl, 6 ex

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

New derivative of 3-(4-(benzyloxy)phenyl)hex-4-ine acid, method for its production and pharmaceutical composition for metabolic disease prevention and treatment including it as effective ingredient // 2628077
FIELD: pharmacology.SUBSTANCE: invention relates to a compound represented by formula 1, its optical isomer or a pharmaceutically acceptable salt thereof: [Formula 1] , as well as to methods for its preparation and a pharmaceutical composition based on it.EFFECT: new connections are obtained, with the ability to activate the GPR40 enzyme, suitable for use for metabolic disease prevention or treatment.10 cl, 7 tbl, 77 ex, 2 dwg
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

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
8-carbamoyl-2-(2,3-di-substituted pyrid-6-yl)-1,2,3,4-tetrahydroisoquinoline derivatives as apoptosis-inducing agents for cancer treatment // 2625315
FIELD: pharmacology.SUBSTANCE: invention relates to organic chemistry, namely a heterocyclic compound of formula (I) or to a therapeutically acceptable salt thereof, where X is benzo[d]thiazolyl, thiazolo[5,4-b]pyridinyl, thiazolo[4,5-c]pyridinyl, imidazo[1,2-a]pyridinyl, thiazolo[5,4-c]pyridinyl, thiazolo[4,5-b]pyridinyl, imidazo[1,2-a]pyrazinyl or imidazo[ 1,2-b]pyridazinyl; Y1 means pyrrolyl, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with 1 or 2 substituents independently selected from R5, CN and Cl; L1 is selected from (CR6R7)q, (CR6R7)s-O-(CR6R7)r, (CR6R7)s-S-(CR6R7)r, (CR6R7)s-S(O)2-(CR6R7)r and (CR6R7)s-NR6A-(CR6R7)r; Y2 means mono- or tricyclic C8-C10-cycloalkyl, spiro[2.5]octyl, spiro[3.5]nonyl, oxatricyclo[3.3.1.13,7]decyl or azabicyclo[3.2.1]octyl; where Y2 is optionally substituted with 1, 2 or 3 substituents independently selected from R8, OR8, SO2R8, CO(O)R8, OH and Br; Z1 is selected from , R1 and R3 are absent; R2 is deuterium or C1-C6-alkyl; R5 is C1-C6-alkyl; R6A is selected from hydrogen and C1-C6-alkyl; each R6 and R7 are hydrogen; R8 is selected from the group consisting of C1-C3-alkyl, morpholinyl and dioxydothiomorpholinyl; where R8, meaning C1-C6-alkyl, is optionally substituted with a substituent selected from R16, OR16, SO2R16 and NHR16; Rk is selected from C1-C6-alkyl, morpholinyl, cyclopropyl and C1-haloalkyl; R16 Is selected from C1-C4-alkyl, phenyl, morpholinyl and tetrahydropyranyl; where R16, meaning C1-C4-alkyl, is optionally substituted with 1 substituent selected from OCH3, OCH2CH2OCH3 and OCH2CH2NHCH3; q is 1 or 2; s, m and p is 0; r is 0 or 1; N is 0, 1, or 2. The invention also relates to specific compounds, pharmaceutical compositions based on these compounds and a method for treatment of these diseases.EFFECT: new heterocyclic compounds are obtained, that are useful for treatment of some cancers.16 cl, 3 tbl, 86 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

Combined composition of substances with complex pharmacological activity // 2622991
FIELD: pharmacology.SUBSTANCE: invention relates to a combined composition having radioprotective and antiradiation activity. This composition contains (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide and (3aS)-2-[(3S)-1-azabicyclo-[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1H-benz[de]isoquinoline.EFFECT: invention provides an expressed decrease in the manifestation of primary radiation exposure symptoms when affected by various doses of ionizing radiation.2 cl, 2 dwg, 7 tbl, 7 ex
Azole derivatives // 2622639
FIELD: pharmacology.SUBSTANCE: invention relates to azole derivative of formula (I) or its pharmaceutically acceptable salt, wherein R1 is hydrogen atom or C1-5alkyl; R2 is hydrogen atom or C1-5alkyl; R3 is phenyl or pyridyl (where phenyl or pyridyl is optionally substituted with one or two fragments selected from the group consisting of C1-5alkoxy, halogen and trifluoromethyl atoms); each of R4 and R5, which can be the same or different, represent hydrogen atom or C1-5alkyl (where C1-5alkyl is optionally substituted with one fragment selected from the group consisting of hydroxy and C1-5alkoxy), or R4 and R5 together with nitrogen atom joining them form 4-7-membered saturated or unsaturated heterocycle, optionally compirsing one cyclic nitrogen, oxygen or sulfur atom, aside from the mentioned above joining nitrogen atom (where 4-7-membered saturated and unsaturated heterocycle is optionally substituted with one or two fragments, selected from the group consisting of hydroxy C1-5alkyl (where C1-5 alkyl is optionally substitued with one or two hydroxyl group), C1-5alkoxy, halogen atoms, cyano, C2-5alkanoyl, aminocarbonyl, mono-C1-5alkylaminocarbonyl, di-C1-5 alkylaminocarbonyl, trifluoromethyl, amino, mono-C1-5alkylamino, di-C1-5alkylamino and C2-5alkylamino, wherein the mentioned 4-7-membered saturated or unsaturated heterocycle optionally has C1-5alkylene fragment, joining two different cyclic carbon atoms), or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; azole cycle represented by formula (α) has any structure of group (II) formula, contained in invention formula, and wherein Ry is hydrogen atom or C1-5alkyl; X1 and X2 are such that: (i) if X1 means an ordinary link or fragment -CO-, X2 means -C1-5alkylene- or -O-C1-5alkylene-; and (ii) if X1 means a fragment -CONRx1-, X2means an ordinary link; Rx1 is hydrogen atom or C1-5alkyl; and cycle A is benzol cycle, pyridine cycle (where benzol cycle is optionally substituted with one or two fragments, selected from the group consisting of halogen atoms and C1-5alkoxy), 5-6-membered saturated or partly unsaturated heterocycle, containing one or two nitrogen atoms (where 5-6-membered saturated or unsaturated heterocycle is optionally substituted with one oxo group) or C3-7cycloalkane. The invention also relates to a pharmaceutical composition having antagonistic effect against V1b arginine-vasopressin receptor, and to agent for treating or preventing mood disorders, anxiety disorders or drug addiction, comprising azole derivative of formula (I) or its pharmaceutically acceptable salt as an active agent.EFFECT: azole derivative having antagonistic effect against V1b arginine-vasopressin receptor.12 cl, 22 tbl, 361 ex

Crystalline form of compound used as a mineralocorticoid receptor antagonist and the method of its production // 2622105
FIELD: chemistry.SUBSTANCE: invention relates to crystalline forms I and II of compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxy-1-carbonyl)-3,3a, 4.5-tetrahydro-2H-pyrazolo[3.4-f]quinolin-2-yl]benzonitrile of formula (I), used as a mineralocorticoid receptor antagonist. Crystalline forms have characteristic peaks of powder X-ray diffraction pattern specified in the claims. The invention also relates to processes for preparing crystalline forms I and II and the use of the obtained crystal forms in the manufacture of medicaments for the treatment and/or prevention of kidney damage or cardiovascular diseases.EFFECT: obtained crystalline form the compound of formula amorphous form of its superior stability, not only at high temperature and humidity, and light conditions.16 cl, 4 dwg, 4 tbl, 10 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
Pharmaceutical compositions comprising camptothecin derivative // 2620331
FIELD: pharmacology.SUBSTANCE: composition comprising 7-tret-butoxyiminomethyl camptothecin, as an active agent, and a carrier comprising a lipophilic component, a surfactant, a hydrophilic component and a co-solvent. The lipophilic component is a propylene glycol monoester of caprylic acid. The surfactant is vitamin E TPGS. The hydrophilic component is PEG 400. The co-solvent is ethanol. Also, a method for composition preparation and a method of treatment are disclosed.EFFECT: increased bioavailability of 7-tret-butoxyiminomethyl camptothecin.5 cl, 6 ex
ethod for neuralgia treatment // 2619344
FIELD: medicine.SUBSTANCE: for neuralgia treatment, a drug complex is used, where one of non-steroidal anti-inflammatory compounds drugs is applied as the basic analgesic agents, namely - ketorolac tromethamine at a dose of 15-75 mg, or sodium metamizole at a dose of 500-2500 mg, or the ketoprofen at a dose of 50-250 mg, or dexketoprofen at a dose of 25-125 mg, or lornoxicam at a dose of 4-20 mg, cyanocobalamin at a dose of 500-2500 mcg is used as an adjuvant analgesic agent, and drotaverine hydrochloride at a dose of 10-50 m is used as a myotropic spasmolytic action, that are administered intravenously with distribution of the said doses by one or two daily injectios, course of treatment lasts 1-10 days.EFFECT: method allows to ensure complete elimination of the pain syndrome after the course of treatment, the possibility of pain syndrome elimination with a single administration of drugs with obtaining of a momentary stable analgesic effect by eliminating the protective muscular tension in the affected nerve zone at method safety.2 tbl, 125 ex

Crystalline solvates of hydrochloride 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one // 2619129
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular to crystalline dihydrate 6-(piperidin-4-yloxy)-2H-isoquinolin-1-one of formula and a solid pharmaceutical composition thereof.EFFECT: obtained crystalline hydrochloride dihydrate, having better stability and hygroscopicity, which is preferable in obtaining the medicinal product based on it.16 cl, 14 dwg, 1 tbl

N-piperidin-3-yl-benzamide derivatives for cardiovascular diseases treatment // 2618628
FIELD: pharmacology.SUBSTANCE: invention relates to substituted amide compounds of formula pharmaceutical compositions containing such compounds and application of such compounds for lowering plasma lipid levels, such as low density lipoprotein cholesterol (LDL-cholesterol) and triglycerides, and thus, for treatment of diseases exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in mammals, including humans.EFFECT: increased efficiency of compounds application.42 cl, 10 dwg, 55 ex
4-aminoquinoline-3-carboxylic acid derivatives and compositions containing them for enhancing sweet taste // 2617700
FIELD: chemistry.SUBSTANCE: invention relates to a new derivative of quinoline of formula (I) (I)or its salt suitable for internal use, where R1 and R2 represents hydrogen; L represents a C1-C7 alkylene, C3-C6 cycloalkylene or -(CH2)1-3-(C3-C6) cycloalkylene; M represents -NR4-C(O)- or -C(O)-NR4-; when M represents -NR4-C(O)-, R4 represents hydrogen; or alternatively R4 represents a C1-C3 alkilinity linker, where the specified alkilinity linker and from 2 to 5 atoms of L, together with the nitrogen to which they are attached, form a 5-8-membered monocyclic, bicyclic or bridged heterocyclic ring that is optionally substituted and contains one hetero-atom representing a nitrogen atom; and R3 represents a C1-C6 alkyl, a substituted C1-C3 alkyl, a C3-C6 cycloalkyl, a substituted C3-C6 cycloalkyl, a 6-membered heterocyclyl containing one oxygen atom, or a substituted 6-membered heterocyclyl containing one nitrogen atom; when M represents -C(O)-NR4-, R4 represents hydrogen; or alternatively R4 and R3 together with the nitrogen to which they are attached form a 5-6-membered monocyclic heterocyclic ring which contains one nitrogen atom; where in the group indicated as substituted, one substituent is selected from the group consisting of the following substituents: -NH2, a hydroxyl, a C1-6 alkoxy, a C1-6 alkyl, a 6-membered heterocyclyl containing one or two atoms selected from N and O, a C3-4 cycloalkyl, and C(=O)NRaRa, where each Ra independently means hydrogen or a C3-6 cycloalkyl; provided that the compounds of the formula (I) cannot represent compounds mentioned in claim 1. The invention also relates to a composition based on a compound of the formula (I) and methods for enhancing the sweet taste.EFFECT: new quinoline derivatives useful as sweet taste modifiers are obtained.31 cl, 24 tbl, 24 ex
Solid dosage forms with choline-positive action based on 9-butylamino-3,3-dimethyl-1,2,4-trihydroacridine // 2616247
FIELD: pharmacology.SUBSTANCE: solid dosage form comprising of 9-butylamino-3,3-dimethyl-1,2,4-trihydroacridine, calcium stearate, dicalcium phosphate dihydrate, polyvinyl pyrrolidone, sodium dodecyl sulfate, talc, milk sugar in a certain weight ratio is described. A method for preparing said solid dosage form is shown.EFFECT: invention provides a high tablet hardness, required disintegration and high bioavailability of the active ingredient, ease of manufacture of proposed tablets.1 tbl
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
Tetrahydroquinoline derivatives as activators of ampk // 2615758
FIELD: chemistry.SUBSTANCE: invention relates to a new tetrahydroquinoline derivative of formula or its pharmaceutically acceptable salt, wherein R1: hydrogen, lower alkyl, halogen or carboxy; R2: hydrogen, lower alkyl, halo-lower alkyl, halogen, cyano, or carboxy; R3 and R4: lower alkyl; R5 and R6 are selected from hydrogen, carboxy-lower alkylamino, carboxycyclopropylamino, lower alkylsulfonylamino, phenylsulfonylamino, halophenylsulfonylamino, lower alkylphenylsulfonylamino, halophenylkarbonilamino, piridinilsulfonilamino, lower alkylaminosulfonyl and halophenylaminosulfonyl; with the provision that both R5 and R6 do not simultaneously represent hydrogen; R7: hydrogen or lower alkyl. The invention also relates to the pharmaceutical composition based on the compound of the formula (I) and to the application of the compound of the formula (I).EFFECT: invention provides obtaining new tetrahydroquinoline derivatives useful as an activator of AMP-activated protein kinase (AMPK).20 cl, 1 tbl, 94 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

Stable pharmaceutical composition for oral administration comprising levocetirizine, or pharmaceutically acceptable salt thereof and montelukast or pharmaceutically acceptable salt thereof // 2614382
FIELD: medicine, pharmacy.SUBSTANCE: this present invention relfers to a pharmaceutical composition in the form of a capsule for oral administration for asthma or allergic rhinitis prevention or treatment. The composition comprises: (a) the first fraction of particles in the form of mini-pill comprising levocetirizine, or pharmaceutically acceptable salt thereof and organic acid; and (b) the second fraction of particles in the form of mini-pill comprising montelukast or pharmaceutically acceptable salt thereof. The organic acid is citric acid, tartaric acid, succinic acid or ascorbic acid. The organic acid is present in the amount of 100 parts by weight per 100 parts of levocetirizine. The said first and second particle fractions are physically separated and filled into the capsule. A method for pharmaceutical capsule composition production is also described. The pharmaceutical composition of this invention inhibits the production of related contaminants of levocetirizine and montelukast and provides good stability.EFFECT: invention expands the product range of drugs for allergic rhinitis or asthma prevention or treatment.9 cl, 3 dwg, 4 tbl, 6 ex
Gelatine capsule of selective vessel destruction in tumours // 2613146
FIELD: medicine.SUBSTANCE: gelatine capsule of selective vessel destruction in tumours relates to field of pharmaceutics and medicine, in particular to oncology, and deals with novel medications, mechanism of action of which consists in their destruction of already existing vessels inside tumour, preventing in such way supply of blood and oxygen, vital for survival of solid tumours with dimensions exceeding 1 mm. The capsule contains approximately 250-900 mg of pharmaceutical composition, which contains anti-tumour compound 7-methoxy-4-nitro-3-(p-methoxyphenyl)isoquinolinone 16-18 wt %, crospovidone 5-8 wt %, hypromellose 2-3 wt %, polysorbate 80 - 1-2 wt %, sodium laurylsulphate 0.7-1.2 wt %, the remaining part - mannitol, in gelatine capsule.EFFECT: invention solves the task of creating novel peroral anti-tumour medication for prevention or treatment of benign or malignant tumours, independently on their origin or size, within the framework of treating mammals, in particular humans, resistant to traditional treatment.3 cl, 1 tbl

New rebamipide prodrugs, method for their preparation and application // 2612509
FIELD: biotechnology.SUBSTANCE: invention relates to a compound of formula 1 that is a new rebamipide prodrug, and to the pharmaceutical composition thereof.EFFECT: new rebamipide prodrug with absorption rate 25 times higher than that of rebamipide, which can be used for prevention or treatment of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.7 cl, 3 tbl, 204 ex, 1 dwg
ethod of increasing the efficiency of treatment of patients with tuberculosis // 2611398
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to phthisiology, and can be used to improve the efficiency of treatment of patients with tuberculosis. Method includes the determination of the degree of patient’s medication adherence through his questioning, which is performed at the beginning of the main course of treatment. Stens are determined and after its determination diagnose the factors affecting the level of adherence, and then the prediction of medication adherence is determined: if total score is from 35 points and more, 1–2 stens mark the unsatisfactory medication adherence, if it is 16–34 points, 3–5 stens mark satisfactory medication adherence, if it is 4–15 points, 6–8 stens mark good medication adherence, if it is up to 3 points, 9–10 stens mark medication adherence. In case of unfavorable prognosis at 1–5 stens prescribe cycloferon immunomodulator and methods of psychotherapy, as well as the chemotherapy regimen correction is carried out by changing the method of administration of etiotropic drugs, and at a satisfactory medication adherence etiotropic drugs are administered parenterally, and at unsatisfactory medication adherence etiotropic drugs are administered parenterally and inhalationly.EFFECT: use of invention improves efficiency of treatment of patients with tuberculosis by determining the degree of patient’s medication adherence for further treatment correction.1 cl, 2 ex
ethod for production of antiparasitic long acting preparation for animals // 2611387
FIELD: veterinary medicine.SUBSTANCE: praziquantel, ivermectin, copolymer of lactic and glycolic acids are mixed with a solvent with the following ingredient ratio (in wt %): praziquantel - 1.0-15.0, ivermectin - 0.5-8.0, copolymer of lactic and glycolic acids - 6.0-16.5, solvent - the rest. At that,praziquantel and ivermectin are the first to be dissolved in the solvent. The solution is then purged with argon or nitrogen and placed in an ultrasonic bath. The mixture is kept in the ultrasonic bath for 50-60 minutes till complete dissolution of the components. Then the copolymer of lactic and glycolic acids is added. For complete copolymer dilution, the obtained mixture is kept for 4-5 hours with occasional stirring at the rotation speed of 1600-2000 rpm. Then, the resulting solution is subjected to sterile filtration, dispensed into vials and sealed.EFFECT: method can reduce loss of active ingredients during manufacture and provide a harmless, non-toxic, sterile and effective long-acting drug for treating animals against a wide range of parasitic infections.5 cl, 8 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
 
2551190.
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