Drugs for disorders of the nervous system (A61P25)

A   Human necessities(312083)
A61P25                 Drugs for disorders of the nervous system(3218)
Comt inhibitors // 2642779
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of the formula (I) and their pharmaceutically acceptable salts which have the properties of a catechol-O-methyltransferase (COMT) inhibitor. In the compound of the formula (I) , where R1 is hydrogen, methyl, Br, F or Cl; R2 is hydrogen, lower alkyl, Br, I, C3-6cycloalkyl, C(O)O-lower alkyl, C(O)NH-lower alkyl substituted by halogen, C(O)(morpholine) or is 3,4-dihydronaphthalen-2-yl optionally substituted by lower alkyl, 1,2,3,4-tetrahydronaphthalen-2-yl, 2,3-dihydrobenzofuran-6-yl, 1-methyl-2,3-dihydro-1H-indolin-5-yl, 1-methylindolin-5-yl, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl, 2-isopropyl-1,2,3-tetrahydroisoquinolin-5-yl, 2,3-dihydro- dimethyl[1,4]dioxin-6-yl, benzo[1,3]-dioxol-5-yl, 1,2,3,4-tetrahydroisoquinolin-7-yl optionally substituted by lower alkyl, cyclohexenyl, morpholinyl, 4-methylpiperazinyl, naphthalen-1-yl, naphtalen-2-yl, or represents (CHR)n-phenyl optionally substituted by one to five substituents R4, where R4 is F, Cl, CN, CH2-CN, lower alkyl, hydroxy, lower alkyl, substituted hydroxy, lower alkoxy, (CH2)1.2-lower alkoxy, S-lower alkyl, (CH2)1.2-S-lower alkyl, -CH2)1.2-S (O)2-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkylamino, -S(O)2-piperidinyl, lower alkyl substituted by halogen, -N=N-phenyl, di-lower alkylamino, (CH2)1.2-di-lower alkylamino, (CH2)2-NH-lower alkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, CH(CH3) C(O)O-lower alkyl, O-phenyl, O-benzyl, phenyl, optionally substituted CF3, SF5, benzyl, C(O)-lower alkyl, C(O)-phenyl, C(O)-morpholinyl, C(O)-4-methylpiperazinyl, C(O)-di-oxothiomorpholinyl, C(O)-piperidinyl, optionally substituted by F, C(O)-NH-(CH2)2-morpholinyl, C(O)-NR-(CH2)2-NR2, C(O)-N-di-lower alkyl, CH2-O-(CH2)2-4-methylpiperazinyl, CH2-O-(CH2)2-di-alkylamino, CH2-O-(CH2)2-pyrrolidinyl, CH2-O-(CH2)2-morpholinyl, CH2-O-(CH2)2-piperidinyl optionally substituted by lower alkyl substituted by halogen or lower alkyl, (CH2)3,4-pyrrolidinyl, (CH2)2,3-di-lower alkylamino, morpholinyl, CH2-morpholinyl, CH2-piperazine substituted by lower alkyl, -S(O)2-piperazine substituted by lower alkyl, CH2-O-C(O)-piperazine substituted by lower alkyl, pyrazolyl or (CH2)1,2-lower alkoxy; R is hydrogen, lower alkyl or hydroxyl; n is 0, 1, 2, or 3; or R2 is C(O)-phenyl optionally substituted by lower alkyl; or is -O-phenyl optionally substituted by F; or is CH=CH-phenyl optionally substituted by lower alkyl; or is C≡C-phenyl; or R2 is a heteroaryl selected from the group consisting of pyrazolyl, thiazolyl, pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl, isothiazolyl, thiophenyl, 1-thia-3,4-diazolyl, imidazo[1,2-a]pyridinyl, indazolyl, quinolinyl or isoquinolinyl, and the said groups are optionally substituted by R5, where R5 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, hydroxy, (CH2)1.2-lower alkoxy, CH2-di-lower alkylamino, di-lower alkylamino, morpholinyl, piperazinyl, pyrrolidin-1-yl, C(O)-piperidinyl, C(O)-4-methylpiperazinyl, phenyl optionally substituted by halogen, pyridinyl, S(O)2N(CH3)2, C(O)O-lower alkyl, NHC(O)-lower alkyl, or is C(O)-heteroaryl selected from pyridinyl and thiophenyl, where heteroaryl groups are optionally substituted by lower alkyl, n is 0, 1, 2 or 3; R3 is hydrogen, methyl, Br, F, Cl, CF3, nitro, amino, cyano, NHC(O)-phenyl, or is 1-methyl-1,2,3,6-tetrahydropyridinyl, or is pyridinyl optionally substituted by methyl or morpholinyl, or is phenyl optionally substituted by methyl , SO2CH3, CF3, CN, F or C(O)N (di-lower alkyl).EFFECT: compounds can be used to treat Parkinson's disease, depression, cognitive impairment and motor symptoms, resistant depression, cognitive impairment, mood and negative symptoms of schizophrenia.16 cl, 2 tbl, 256 ex
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex

Concentrated therapeutic phospholipide compositions // 2642653
FIELD: pharmacology.SUBSTANCE: composition for treatment or prevention of cardiometabolic disorders, a metabolic syndrome, neurodegenerative disorders comprises a concentrated therapeutic phospholipid extract comprising compounds of Formula I wherein the total amount of the phospholipid compounds of Formula I from the extract is in a concentration of 60 wt % to 90 wt % of the total weight of the composition and the extract includes astaxanthin; to a capsule containing a concentrated therapeutic extract of krill oil that contains the phospholipid compounds of Formula I and the extract includes astaxanthin; to application of a composition that includes a concentrated therapeutic phospholipid extract containing compounds of Formula I for preparation of therapeutic compositions for serum triglyceride levels lowering; to application of a concentrated therapeutic phospholipid extract that contains compounds of Formula I for preparation of pharmaceutical compositions for treatment of cardiovascular diseases.EFFECT: increased mass percentage of phospholipids in the composition.20 cl, 35 dwg, 2 tbl, 7 ex
eans for correction of psychoemotical status of organism based on astragalus herbs extract // 2642595
FIELD: pharmacology.SUBSTANCE: means for correction of the psychoemotional status of the organism, with antistress, antidepressant, anxiolytic and nootropic action, which is an aqueous or hydroalcoholic extract of Astragalus vulpinus Willd., containing flavonoids, ascorbic acid, saponins and tannins in a certain quantity.EFFECT: drug has a pronounced anti-stress, antidepressant, anxiolytic and nootropic effect, restores psychoemotional state of the organism.5 ex
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
Application of probiotic strain of enterococcus faecium l-3 microorganism for neurodegenerative diseases treatment // 2642246
FIELD: medicine.SUBSTANCE: probiotic strain of Enterococcus faecium L-3 is used. Therapy is carried out by short courses (up to a month) with interruptions under the control of the intestinal microbiota composition and the populations of circulating T cells. In case of exacerbations, traditional therapy with copaxone can be used (the use of a probiotic should be stopped for this period).EFFECT: method allows to increase the effectiveness of treatment by stimulating the production of anti-inflammatory cytokine.5 dwg
Compositions, synthesis and methods for application of phenylcycloalkylmethylamine derivatives // 2642074
FIELD: pharmacology.SUBSTANCE: invention relates to new phenylcycloalkylmethylamine derivatives of structural formula (I), or enantiomers or optically active isomers, or pharmaceutically acceptable salts having affinity for the binding of dopamine (DAT), the carrier of norepinephrine (NET) and the serotonin transporter (SERT). The compounds may find use in treatment and/or prevention of obesity, as well as depression 1. In the structural formula (I) ,n is 1; SP is a spacer, wherein the said spacer is C4 alkylene; X is O or S; R1 and R2 are independently H, C1-6 alkyl, C1-6 alkoxy, halogen; R3 is C1-6 alkyl; R4 is H or C1-6 alkyl; R5 is C1-6 alkyl; and * represents a carbon atom that can be optically active.EFFECT: improved composition properties.12 cl, 1 tbl, 86 ex
Derivatives of 1-(4,5-dihydroimidazole)-isochromane or 1-(4,5-dihydro)-isothiochromane, which are useful as agonists of alpha2 adrenoreceptors // 2642065
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the formula or a pharmaceutically acceptable salt thereof, wherein X is O or S; R1 is hydroxyhalogen, (C1-C6)alkyl, halogen(C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, cyclo(C3-C6)alkyl, (C1-C6)alkoxy, halogen(C1-C6)alkoxy, hydroxy(C1-C6)alkyl, cyano, (R6)2N-(C=O)-, (C1-C6)alkyl-S-, or furanyl; R2 is H or (C1-C6)alkyl; R3 is H, (C1-C6)alkyl, halogen(C1-C6)alkyl or (C1-C6)alkoxy(C1-C6)alkyl; R4 is H or (C1-C2)alkyl; R5 is H, hydroxy, halogen, (C1-C6)alkyl or (C1-C6)alkoxy; R6 is H; or R1 and R2 form rings together with carbon atoms, to which they are attached, a fused 6- or 7-membered saturated or unsaturated carbocyclic ring. The invention also relates to a pharmaceutical composition based on a compound of formula (I).EFFECT: new isochromane or isothiochromane derivatives, useful as alpha2 adrenoreceptor agonists, have been obtained.10 cl, 1 tbl, 106 ex
Polycyclic compounds and methods for their use // 2641648
FIELD: pharmacology.SUBSTANCE: invention relates to a compound having the formula or a pharmaceutically acceptable salt or stereoisomer thereof. In the formula (IVa): (i) R1 and R3 together with the atoms to which they are attached form an optionally substituted 3-20 membered heterocyclyl and R4 is hydrogen; or (ii) R3 and R4 together form a double bond and together with R1 and the atoms to which they are attached form an optionally substituted 5-20 membered heteroaryl; R2 is hydrogen, C1-6alkyl or absent; R5 is hydrogen; R6 and R7 are hydrogen; m is 0; n is 1; and wherein heterocyclyl or heteroaryl may be substituted by one or more substituents selected from C1-6alkyl. And heterocyclyl is a monocyclic or polycyclic ring system, which contains at least one non-aromatic ring containing one or more heteroatoms, selected from N, and the rest of the ring atoms are carbon atoms, heteroaryl is a monocyclic or polycyclic ring system, which contains at least one aromatic ring containing one or more heteroatoms, independently selected from S and N. A pharmaceutical composition and a method for neurological disorder treatment are also proposed.EFFECT: compound of the formula is used to treat neurological disorders.31 cl, 2 tbl

Therapeutic agent for diseases based on inhibiting action on microphaging migration inhibition factor // 2641301
FIELD: pharmacology.SUBSTANCE: invention relates to an inhibitor of a migration inhibition factor for macrophages containing a benzopyran derivative represented by the general formula [1] or a salt thereof, wherein R1 is a C1-6 alkyl group; one of R2 and R3 is a hydrogen atom and the other of R2 and R3 is a hydrogen atom, an amino group, an acylamino group, a carbamoyl group or an aryl group, as well as a drug against neuropathic pain, excluding the symptoms of allodynia in neuropathic pain, based on the compounds of formula I.EFFECT: increased means effeciency.9 cl, 4 tbl, 1 dwg

Benzofurazan antimyloid compounds and methods // 2641293
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula I , where R11 is selected from the group consisting of benzylamino, N-methylbenzylamino, N-methyl(4-fluorobenzyl)amino, N-methyl(4-methoxybenzyl)amino, N-methyl(3,5-dimethoxybenzyl)amino, N-methyl(pyridine-2-yl)amino, N-methyl(pyridin-3-yl)amino, piperidino, 4-methylpiperazin-1-yl, morpholino, thiomorpholino, pyrrolidino, 3-methoxypyrrolidin-1-yl, pyrrolidin-3-ol-1-yl, 2-(2-methanol-1-yl)pyrrolid-1-yl, 2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl, 2-(2-propanol-2-yl)pyrrolidin-1-yl, isoindolin-2-yl, 4-(pyrrolidin-1-yl)piperidin-1-yl, N,N-diethylamino, N-methyl-N-ethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-ethynylamino, N-(thiazol-2-ylmethyl)-N-methylamino, azetidin-1-yl, 3-methyl-3-ol-azetidin-1-yl, 3-(ethanol-2-yl)azetidin-1-yl, 3-methoxyazetidin-1-yl, 3-hydroxyazetidin-1-yl, 3-ethoxyazetidin-1-yl, 3-isopropoxyazetidin-1-yl, 3-(2-propanol-2-yl)azetidin-1-yl, 3-(morpholinomethyl)azetidin-1-yl, 3-morpholinoazetidin-1-yl, 3-(pyrrolidin-1-yl)azetidin-1-yl, 3-(pyrrolidin-1-ylmethyl)azetidin-1-yl, 3-(1-methoxyethyl)azetidin-1-yl, N-(3-(N,N-dimethylamino)propyl)-N-methylamino and 4-(N,N-dimethylamino)piperidin-1-yl; R13 is selected from the group consisting of 3-(ethanol-1-yl)phenyl, 3-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 2-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 4-(1-ol-2,2,2-trifluoroethan-1-yl)phenyl, 3-(3-ol-oxetan-3-yl)phenyl, 3-((piperazin-1-yl)methanon-2-yl)phenyl, 3-((morpholin-1-yl)methanon-2-yl)phenyl, 3-((pyrrolidin-1-yl)methanon-2-yl)phenyl, 3-((N-cyclopropyl)amide-2-yl)phenyl, 3-ol-oxetan-3-yl, 2-ol-but-3-en-4-yl and 2-ol-2-trifluoromethyl-(1,1,1-trifluoro)but-3-en-4-yl; and R12 and R14 each independently is hydrogen.EFFECT: new compounds are obtained that are useful for treatment of an amyloid disease, such as Alzheimer's disease.11 cl, 2 tbl, 7 dwg
ethod for treatment of sustainable paroxismal states and generalized myoclonia in patients with consequences of heavy damage to brain // 2641163
FIELD: medicine.SUBSTANCE: patients subjected to medical anaesthesia. The trachea is intubated and the patient is transferred to artificial lung ventilation. At that, after trachea intubation and transfer to artificial lung ventilation, medical anaesthesia is performed, including inhalation anaesthesia with Sevoflurane at a dose of 2.0-3.0 vol % MAC 0.8-0.9 for 24-48 hours and additional intravenous infusion of Ketamine in a dose of 1-2 mg/kg-h for 2 hours, starting from the 2nd hour of medical anaesthesia. Artificial lung ventilation is carried out on a semi-closed contour in the "Pressure control" or "Pressure support" mode under the control of capnometry and arterial blood gases analysis.EFFECT: method allows to increase the effectiveness of treatment of paroxysmal and persistent generalized myoclonia in patients with consequences of heavy brain damage due to the lasting effect of seized paroxysms and hyperkinesia after termination of medical anaesthesia with application of Sevoflurane and Ketamine.1 ex

Acyl derivative of aminophenol as type a monoamine oxidase activator // 2641112
FIELD: pharmacology.SUBSTANCE: invention refers to the type a monoamine oxidase activator with reduced activity at pathologies, and may find applications in biochemistry when examining the properties of various monoamine oxidases and in medicine when examining development neurodegenerative diseases and cancer processes. The activator is a derivative of 2-aminophenol(N-acetylacetamido)phenyl acetate of the structural formula (a), which is reversible and has mixed nature interactions with the enzyme.EFFECT: improved properties of the derivative.3 dwg
New water-soluble salicylamide derivative with neuroprotective action in case of cerebral circulation insufficiency // 2641102
FIELD: pharmacology.SUBSTANCE: invention relates to the dipotassium salt of 4-[(4'-salicyloylamino)butanoylamino]butanoic acid, of the following formula .EFFECT: neuroprotective action.2 tbl, 4 ex

Therapeutic application of compounds // 2640596
FIELD: pharmacology.SUBSTANCE: invention refers to the application of a compound of formula R1-COOH (I), where R1 is an alkyl group with a main chain of 7-11 carbon atoms, possibly branched in any position of the carbon atom in the main chain, where branching is a side C1-6 alkyl group. The alkyl group of the main chain and/or the side alkyl groups optionally contain one or more heteroatoms. The specified compound is selected from 4-ethyl octanoic acid, 2-butyl octanoic acid, 4-methyl nonanoic acid and 3-methyl undecanoic acid or its pharmaceutically acceptable salt, amide or ester, for treatment or prevention of disease or biomedical state, selected from disorders associated with cramps.EFFECT: increased efficiency of the composition and treatment method.2 cl, 9 dwg, 3 tbl
Benzisoxazole modulators of neurogenesis // 2640590
FIELD: pharmacology.SUBSTANCE: new compounds are obtained that can be used to treat schizophrenia, obsessive-compulsive personality disorders, major depression, bipolar disorders, anxiety, normal aging, epilepsy, retinal degeneration, traumatic brain damage, spinal cord injuries, posttraumatic stress, panic disorders, Parkinson's disease , dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down's syndrome, diseases from the autism spectrum, and loss of hearing, ringing in the ears, spinal-cerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuroactive substances such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.EFFECT: increased efficiency of treatment.12 cl, 44 ex
odulators of atp-binding cartridge transporters // 2640420
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula II , where R is H, OH, OCH3, or two R taken together form -OCH2O- or -OCF2O-; R1 is H or up to two C1-C6alkyls; R2 is H or halogen; and R3 is H or C1-C6 alkyl; R3 is H or C1-C6 alkyl; Y is O or NR4; and R4 is H or C1-C6 alkyl, and their pharmaceutical compositions useful as modulators of ATP-binding cassette ("ABC") transporters, or fragments thereof, including a cystic fibrosis transmembrane conduction regulator ("CFTR"). This invention also relates to methods for treatment of diseases mediated by ABC transporters using the compounds of the invention.EFFECT: increased efficiency of treatment.19 cl, 2 tbl, 1 ex

Cystathionine-g-lyase (cse) inhibitors // 2640418
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the Formula (I) or their pharmaceutically acceptable salts inhibiting the activity of cystathionine-gamma-lyase (CSE). In Formula (I) A is or -CONHSO2R4, where R4 is independently unsubstituted alkyl or unsubstituted aryl; X is CR1 or N; R1 is H; each R2 and R3 is H. The invention also relates to a pharmaceutical composition comprising the said compounds and a method for treatment or prevention of various diseases associated with CSE activity.EFFECT: increased efficiency of the composition and treatment method.13 cl, 11 dwg, 2 tbl, 17 ex
ulti-substituted aromatic compounds as thrombin inhibitors // 2639876
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the formula: , and also to pharmaceutical compositions and methods for treatment and prevention of a disease such as thrombotic one.EFFECT: new compounds capable of inhibiting the protease activity of thrombin.15 cl, 3 tbl, 85 ex
Hetero-aromatic methylic derivative of cyclic amine // 2639869
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (IA), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; Y is any structure from the following group of formulas (a); n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group; R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 an alkyl group; or a pharmaceutically acceptable salt thereof. The invention also relates to a compound represented by the formula (I), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; any one of Y1 and Y2 is a nitrogen atom, and the other is CH; n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group;R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 alkyl group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are intended for the production of a pharmaceutical composition having antagonistic activity against OX1 and OX2 orexin receptors.EFFECT: hetero-aromatic methyl derivative of cyclic amine, which has antagonistic activity against OX1 and OX2 orexin receptors.9 cl, 6 tbl, 85 ex
Prodrug of fluorine-containing amino acid // 2639868
FIELD: pharmacology.SUBSTANCE: in formula (I) R1 and R2 each represents a hydrogen atom, formula -(CR4R4')-O-CO-R5, or -(CR6R6')-O-CO-OR7, or formula (IIa) or (IIb), R3 represents a hydrogen atom, formula -(AA)n-H, -CO-O-(CR9R9')-O-CO-R10, or -CO-O-(CR9R9')-O-CO-OR11, or formula (III), R4 and R4' each represents a hydrogen atom or a C1-6alkyl group, R5 is a C1-10alkyl, adamantyl or phenyl group, R6 and R6'each represents a hydrogen atom or C1-6alkyl group, R7 is a C1-10alkyl, C3-8cycloalkyl or adamantyl group, R8 is a C1-6alkyl group, R9 and R9' each represents a hydrogen atom or C1-6alkyl group, R10 is a C1-10alkyl group, R11 is a C3-8cycloalkyl group, R12 is a C1-6alkyl group, AA is an aminoacyl group and n is an integer from 1 to 3.EFFECT: application of compounds for prevention or treatment of the diseases listed above.17 cl, 7 tbl, 42 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

Composition for prevention or treatment of amyotrophic lateral sclerosis using two or more hepatocytes growth factor isophorms // 2639582
FIELD: medicine.SUBSTANCE: pharmaceutical composition for prevention or treatment of amyotrophic lateral sclerosis containing a hepatocyte growth factor (HGF) isoforms or a polynucleotide, containing isoforms, and a method for prevention or treatment of amyotrophic lateral sclerosis including introduction of the specified composition to a mammal are proposed.EFFECT: prevention or treatment of amyotrophic lateral sclerosis.12 cl, 8 dwg, 6 ex

Phospho-specific antibodies recognizing tau // 2639537
FIELD: medicine.SUBSTANCE: antibody and its fragment that bind to the phospho-epitope on the Tau protein, as well as the polynucleotides encoding them, are provided; cell lines that produce antibodies; a vector, its host cell and a method for production of the antibody and its functional fragment are proposed. In addition, a pharmaceutical composition, a method for treatment, alleviation or protection against taupathy; a method for induction of a passive immune response in an animal; a method for diagnosis of a protein tau-related disease, disorder or condition, or a predisposition to a protein tau-related disease; a method for monitoring of a minimal residual disease in a patient after treatment with an anti-tau antibody; a method for prediction of patient's response to treatment with an anti-tau antibody; methods for detection of phospho-Tau multimers (pTau) in a brain sample, including postmortem detection; a diagnostic set are proposed.EFFECT: invention can find further application in the diagnosis and therapy of diseases associated with Tau-protein.42 cl, 10 dwg, 15 tbl, 11 ex

Liposomes containing oligopeptide fragments of myelin basic protein, pharmaceutical composition and method for multiple sclerosis treatment // 2639497
FIELD: biotechnology.SUBSTANCE: invention relates to the production of liposomes with a peptide of the myelin basic protein (MBP), and can be used in medicine for multiple sclerosis treatment. A composition is prepared containing the MBP peptide with SEQ ID NO: 11 or SEQ ID NO: 12 bound to the first vector, wherein the vector comprises a liposome having a surface exposed to the target portion that contains a mannose residue or a mannose derivative.EFFECT: invention provides greater therapeutic benefit than copaxone, therapeutically approved for the treatment of relapsing-remitting multiple sclerosis.18 cl, 14 dwg, 14 tbl, 14 ex
Application of lithium ascorbate for prevention and treatment of chronic alcoholic intoxication // 2639496
FIELD: pharmacology.SUBSTANCE: invention relates to application of lithium ascorbate in a dose of at least 5 mg/kg as an agent for prevention and treatment of chronic alcoholic intoxication. Application, among all, is characterized by protection of brain neurons and reduction of demyelinating complications.EFFECT: expanded arsenal of means for the specified purpose.4 cl, 1 ex, 3 tbl, 10 dwg

Pharmaceutical composition containing biotin and method for its production // 2639488
FIELD: pharmacology.SUBSTANCE: group of inventions refers to pharmaceutical compositions for polyneuropathy prevention and treatment as a solid dosage form with extended release, comprising Biotin - 40-60 wt % as an active agent, as well as Methocel K100 LV - 14-21 wt %, Methocel K4M - 5-10 wt %, microcrystalline cellulose (MCC) - 7-18 wt %, copovidone - 1.5-3 wt %, colloidal silicon dioxide - 0.4-1 wt % and a pharmaceutically acceptable stearic acid salt - 0.6-1 wt %, as well as to a method for its production, according to which Biotin, Methocel K4M, Methocel K100 LV, MCC and copovidone are sieved and mixed until homogeneous, stearic acid salt, colloidal silicon dioxide are mixed, the mixture is compacted by rolling, colloidal silicon dioxide is added and mixed together with pre-compacted grains, followed by addition of stearic acid salt, stirring and formation a solid dosage form.EFFECT: creation of a new medicinal composition with high technological properties, high stability and reproducible kinetics of active agent release.9 cl, 8 ex, 5 tbl, 1 dwg
Solid oral pharmaceutical composition of s1p agonist or its pharmaceutically acceptable salt, method for its production and methods for treatment and reduction of frequency of clinical exacerbations of multiple sclerosis // 2639424
FIELD: pharmacology.SUBSTANCE: solid oral pharmaceutical composition consists of phignolimide hydrochloride in an amount of 0.4-0.65 mg, pregelatinized starch in an amount of 145-155 mg and magnesium stearate in an amount of 1.0-2.0 mg. The composition can be presented in the form of a pill or a capsule. The composition intended for treatment of relapsing-remitting multiple sclerosis, to reduce the frequency of clinical exacerbations of the disease and reduce the risk of disability progression in relapsing-remitting multiple sclerosis. The composition is administered orally in a dose of 500 μg, once a day.EFFECT: composition according to the invention is characterized by a high homogeneity of the active substance dosage, stability for prolonged storage and is capable of disintegrating and releasing the active substance rapidly during oral administration.5 cl, 10 tbl, 8 ex
Introduction mode for nitrocatechols // 2639131
FIELD: pharmacology.SUBSTANCE: method of prevention or treatment of a disorder of the central and peripheral nervous system, comprising administration of a therapeutically effective amount of 5-[3-(2,5-dichloro-4,6-dimethyl-1-hydroxypyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol compound or pharmacologically acceptable salts, esters, carbamates and phosphates thereof in combination with catecholamine levodopa drug to a patient suffering from the said disorder, in the form of a single daily dose at least for an hour or an hour after the last daily dose of levodopa. A method for prevention or treatment of a disorder of the central and peripheral nervous system, comprising administration of a therapeutically effective amount of 5-[3-(2,5-dichloro-4,6-dimethyl-1-hydroxypyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol compound or pharmacologically acceptable salts, esters, carbamates and phosphates to a patient suffering from the said disorder without food and/or between meals. A method for prevention or treatment of a disorder of the central and peripheral nervous system, comprising administration of a therapeutically effective amount of 5-[3-(2,5-dichloro-4,6-dimethyl-1-hydroxypyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol compound or pharmacologically acceptable salts, esters, carbamates and phosphates thereof, in combination with catecholamine levodopa drug to a patient suffering from the said disorder, wherein the said compound is administered once a day at least 1 hour after the introduction of the last daily dose of levodopa, and less than 90 minutes before going to bed, or upon sleep time occurrence. A method for Parkinson's disease prevention or treatment, comprising administration of a therapeutically effective amount of 5-[3-(2,5-dichloro-4,6-dimethyl-1-hydroxypyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol compound or pharmacologically acceptable salts, esters, carbamates and phosphates thereof, in combination with catecholamine levodopa drug to a patient suffering the from said disease, wherein the said compound is administered once daily at least 1 hour after administration of the last daily dose of catecholamine drug and less than 90 minutes before going to bed, or at the onset of sleep time and at least 1 hour after the last meal and at least 1 hour before the next meal.EFFECT: methods are effective for prevention or treatment of disorders of the central and peripheral nervous system.19 cl, 3 dwg, 4 tbl, 3 ex

Treatment using eslicarbazepine acetate or eslicarbazepine // 2639120
FIELD: pharmacology.SUBSTANCE: method of partial-onset seizure treatment is offered. It is for the patient, which suffers from the absence seizures or is vulnerable to absence seizures. The method comprises the intake of the harmless and effective quantity of the eslicarbazepine acetate (or the intake of the containing it pharmaceutical composition - version), where the partial-onset seizures are accompanied by or go without the secondary generalization, where the vulnerable to absence seizures patient is a child or a teenager (versions).EFFECT: decrease of the critical calcium current on the cells HEK-293, spontaneous absence seizures reduction and absence of GABA current amplification in contrast with the carbamazepine, which increases the absence seizures and causes the worsening of the absence seizures in rats.18 cl, 4 tbl, 3 dwg, 4 ex
Indasole inhibitors of wnt signal path and their therapeutic applications // 2638932
FIELD: medicine.SUBSTANCE: invention relates to a indasole derivative that has the following formula , or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing it. The invention relates to methods for treatment of disorders characterized by the activation of Wnt-signalling pathways (e.g., cancer, abnormal cell proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), including introduction of a therapeutically effective amount of this compound or pharmaceutically acceptable salt thereof. This compound can also be used in modulation of cellular events, mediated by Wnt-signalling, as well as for treatment of genetic diseases and neurological conditions/disorders/diseases due to mutations or disregulation of the Wnt pathway and/or one or more components of Wnt-signalling.EFFECT: inhibits the Wnt signalling pathway and can be used to treat various diseases and pathologies.28 cl, 8 tbl, 8 ex

edicinal dosage form, which contains 6'-fluor-(n-methyl-or n,n-dimethyl)-4-phenyl-4,9'-dihydro-3'n-spiro[cyclohexane-1,1'-pyrano[3,4, b]indole]-4-amine for neuropathic pain treatment // 2638818
FIELD: pharmacology.SUBSTANCE: method comprises oral administration of a dosage form containing a pharmacologically active agent according to the general formula wherein R is -H or -CH3, or a physiologically acceptable salt thereof, once a day, to a subject in need thereof. The dosage form provides immediate in vitro release of the pharmacologically active agent, which is contained in a dose of 40 to 190 μg, and the pharmacokinetic parameter tmax is in the range of 4 to 6 hours.EFFECT: good bioavailability and sufficiency of pain relief, high tolerability and safety.12 cl, 5 dwg, 15 tbl, 3 ex

Recognition improvement // 2638809
FIELD: pharmacology.SUBSTANCE: invention is a composition comprising one or more omega-3 fatty acids selected from the group consisting of docosahexaenoic acid, eicosapentaenoic acid and docosapentaenoic acid, and a uridine source selected from uridine, deoxyuridine, uridine phosphate, uracil, acylated uridine and cytidine for improved recognition and/or for use in the treatment or prevention of impaired recognition function in a subject, where the composition additionally comprises choline or its salts or esters and one or more components/ingredients are selected from the group consisting of phospholipids, vitamin E, vitamin C, selenium, vitamin B12, vitamin B6 and folic acid, where the mentioned subject has one or more symptoms of Alzheimer's disease, vascular dementia, frontal-temporal dementia, semantic dementia or dementia with Lewy bodies or a prodromal form of dementia, or a prodromal form of Alzheimer's disease or a subject has a score of 20-26 by Mini Mental State Examination.EFFECT: improved recognition of Alzheimer's disease at early stages, high tolerability and relatively low side effects.11 cl, 2 ex, 2 dwg
Biotin tablets with delayed release and method for obtaining thereof // 2638803
FIELD: pharmacology.SUBSTANCE: invention is a pharmaceutical composition in the form of a pill that contains biotin as an active ingredient with a delayed release, and excipients, containing the following components, wt %: biotin 50-60, stabiliser 15-21, emulsifier 6-10, thickener 16.5-17, binder 1.5-3, debonder 0.4-1, lubricant 0.6-1.EFFECT: invention provides controlled release of the pharmaceutical composition of biotin in the presence of stable technological properties and stability.3 cl, 1 tbl, 5 ex
ethod for treatment of myophascal neck muscle ache after gurov-levin // 2638784
FIELD: medicine.SUBSTANCE: trigger zone in neck muscles are identified and myofascial blocks are held by traumel-c drug. The drug is injected in quantity of 2.2 ml into identified trigger zones of neck muscles. After that, breath is delayed inspiratorily on the phase of "breathing in" for 9-10 seconds, while the doctor fixes the interested muscle from two sides, combines his/her breath patient's breathing and, when the patient breaths out calmly, carries out traction of this muscle with minimal effort. This complex method is repeated 5-6 times on the muscle concerned, after which the patient rests with calm rhythm of breathing for 4-5 minutes.EFFECT: method provides effective treatment of myofascial aches due to the complex - medicamental and manual effects on the background of inspiratory delay of breathing.2 ex

Casmylate salt // 2638175
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely, to camsylate salt of (1r,1'R,4R)-4-methoxy-5"-methyl-6'-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3'H-dispyro[cyclohexane-1,2'-indene-1'2'-imidazole]-4"-amine. The invention also relates to a pharmaceutical composition comprising this salt and a method of treatment based on the use of said camsylate salt. .EFFECT: new salt is produced, useful in the treatment of Aβ pathologies, such as Alzheimer's disease, Down's syndrome, β-amyloid angiopathy.10 cl, 1 dwg, 2 tbl, 7 ex
Pyrazolo [3,4-c] pyridines and methods of application thereof // 2638116
FIELD: pharmacology.SUBSTANCE: subject of the invention is pyrazolo [3,4-c] pyridines of the formula I ,including their stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts, wherein R1 and R2 have the values disclosed in the claims. These compounds are useful for inhibiting Pim-kinases and for treating disorders such as cancer, mediated by Pim-kinase. Methods for using compounds of formula I for in vitro, in situ and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells or related pathological conditions are disclosed.EFFECT: increased application effeciency.4 cl, 3 tbl, 328 ex
Pyrazolaminopirimidine derivatives as leucine-repeating kinase 2 (lrrk2) modulators for treatment of parkinson disease // 2637948
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula or to their pharmaceutically acceptable salts, wherein X, R1, R2, R3 and A are as defined in the claims. The compounds of formula (I) are modulators of leucine-repeating kinase 2 (LRRK2) modulators.EFFECT: application fortreatment of diseases associated with the LRRK2 receptor, such as Parkinson's disease.20 cl, 2 tbl, 53 ex
Pyrazolaminopirimidine derivatives as modulators of leucine-repeating kinase 2 // 2637947
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazolaminopyrimidine derivatives listed in claim 1 which are modulators of leucine-repeating kinase 2 (LRRK2), a pharmaceutical composition containing them, application of these compounds for treatment of diseases associated with the LRRK2 receptor such as Parkinson's disease, and to a method for Parkinson's disease treatment.EFFECT: higher efficacy of compound application.6 cl, 4 tbl, 52 ex
Triazolcarboxamide derivatives // 2637938
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula I. In formula IR1 is phenyl or pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl, substituted halogen, and lower alkoxy substituted by halogen; X1 is -N = or CH; X2 is a CR2 or =N-; X3 is -N= or CH; provided that only two of X1, X2 or X3 are nitrogen; where is a triazole group selected from , or ; R2 is hydrogen or lower alkyl; Z is a bond, -O- or -CH2-. The compounds of the invention possess affinity for the receptors associated with trace amines (TAAR). The invention also relates to pharmaceutical compositions and to application of a compound for drug manufacture.EFFECT: new compounds of formula I are obtained that have a high affinity for the receptors associated with trace amines, especially TAAR1.12 cl, 1 tbl, 36 ex
Inhibitors of lrrk2 kinases activity // 2637936
FIELD: pharmacology.SUBSTANCE: R1, R2, R3 and R4 values are defined in the claims of this invention. Compounds of the formula (I) inhibit the LRRK2 activity. In addition, the invention relates to particular compounds as defined in claim 14. The invention also relates to a pharmaceutical composition comprising the compounds of the invention and to a method for neurodegenerative diseases treatment, for example those in which the disease is represented by α-synucleinopathy and in particular to a method for treatment of various diseases of the Parkinson's disease type, as well as a method for treatment of autoimmune diseases, such as Crohn's disease or ulcerative colitis.EFFECT: new method for neurodegenerative diseases treatment.22 cl, 10 tbl, 15 ex
Arylcycloalkylamines derivatives neuroprotector (versions), substances with combined neuroprotector, analgetic and antidepressive action, pharmaceutical compositions based thereon // 2637928
FIELD: pharmacology.SUBSTANCE: invention relates to new arylcycloalkylamines of the general formula . In the general formula (I), R1, R2 are H, linear or branched alkyl (C1-C4), linear or branched alkoxy (C1-C4), halogen; Y is -CH2-O-CH2-, - (CH2)n-, where n: 1-3; X is -CO-NH-(CH2)6-, -CO-(CH2)k-, -CH2-NH-(CH2)6-, -CH(CH3)-NH-(CH2)6-, -(CO)p-(CHR5)m, where p, m-: 0, 1, k: 2, 4-7, R5: H, linear alkyl C1-C5; R3, R4 are H, linear alkyl C1-C4, -CH2-C≡CH, -(CH2)2-O-(CH2)2-NH2, cyclopropyl, cyclopropylmethyl; 4-pyridinyl, an amino acid residue of a proteinogenic acyclic or aromatic α-amino acids, γ-aminobutyric acid, ε-aminocaproic acid, β-alanine; -CHR6-CH2-OR7, where R6: H or a linear or branched alkyl C1-C4, benzyl, R7: H, linear alkyl C1-C4, or R3, R4 together with the nitrogen to which they are attached, form a pyrrolidine, 2-(hydroxymethyl) pyrolidine, 4-aminopyridinium ring; G is (C1-C4) carboxylic acid, methanesulfonic acid or a mineral acid or water. As an acyclic or aromatic α-amino acid residue, they contain a proteinogenic α-amino acid residue. As (C1-C4) carboxylic acid, they contain at least one compound from the group consisting of acetic, fumaric, succinic, tartaric, malic and maleic acids. As a mineral acid, they contain at least one compound from the group consisting of hydrochloric, phosphoric, sulfuric acids. The preferred compounds are arylcycloalkylamine derivatives of the general formula , wherein Y: -CH2-O-CH2-, -(CH2)2-. The invention also relates to a pharmaceutical composition which can be a combination of arylcycloalkylamine derivatives and at least one substance from the group comprising levodopa, palmitoyle ethanolamide, N-(2-aminoethyl) palmitamide hydrochloride, rasagiline, risperidone, toloxaton, quetiapine, gamma-aminobutyric acid, sodium valproate, amitriptyline, clomepramine, fluoxetine, paroxetine, sertraline, phenylephrine, dexamethasone, prednisolone. The composition may be in the form of a tablet, capsule, pellet, powder for preparation of a solution for enteral administration, a solution for parenteral administration, a powder for preparation of a solution for parenteral administration.EFFECT: neuroprotective, analgesic and antidepressant action.11 cl, 13 tbl, 96 ex
Compounds of thienopyrimidine // 2637925
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I: , where group A is independently monocyclic or bicyclic aryl or heteroaryl optionally substituted by one or more A'; each group A' is independently C1-6 alkyl, halogen, cyano or heteroaryl; group R1 is tetrahydropyranyl substituted with an amino group; or pharmaceutically acceptable salts thereof, which are SYK inhibitors and are useful for treatment of autoimmune and inflammatory diseases.EFFECT: increased efficiency of treatment.10 cl, 2 tbl, 25 ex
ethod of obtaining conditioned media with regenerative potential for intranasal introduction in treatment of diseases of central nervous system // 2637407
FIELD: medicine.SUBSTANCE: conditioned media is obtained by laboratory processing and cultivation of type 2 macrophages obtained from the adherent fraction of peripheral blood mononuclear cells of the patient or his immediate relative by cultivation for 7-8 days in a nutrient medium supplemented with 2-3% autologous plasma in the presence of granulocyte-macrophagal colony-stimulating factor, as a result of which the bioactive factors are secreted to conditioned media, selected from the group consisting of erythropoietin [EPO], insulin-like growth factor-1 [IGF-1], interleukin-6 [IL-6], brain-derived neurotrophic factor [BDNF], epidermal growth factor [EGF], basic fibroblast growth factor [FGF-basic]. Conditioned media is used in the form of intranasal inhalations according to the individual course program, depending on the patient's initial condition and the features / severity of the disease.EFFECT: conditioned medium obtained by the proposed method has a regenerative potential in the treatment of functional disorders of central nervous system and the consequences of organic brain damages.3 cl, 4 ex

ethod for control functions improvement // 2637089
FIELD: pharmacology.SUBSTANCE: 24-week use of a composition for control functions improvement in a subject with Alzheimer's disease or dementia, including their prodromal forms, is proposed. Control functions include speed of information processing, cognitive and mental flexibility, scanning and/or change of cognitive tasks, the specified composition contains (in a daily dose of 125 ml): 300 mg of eicosapentaenoic acid, 1200 mg of docosahexaenoic acid, 106 mg of phospholipids, 400 mg of choline, 625 mg of UMP (uridine monophosphate), 40 mg of vitamin E (alpha-TE), 80 mg of vitamin C, 60 μg selenium, 3 μg of vitamin B12, 1 mg of vitamin B6 and 400 µg of folic acid.EFFECT: composition improves all of the above impaired cognitive functions in Alzheimer's disease.4 cl, 2 dwg, 1 tbl, 2 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
ethod for prevention of early postoperative cognitive dysfunction in patients with digestive organs pathology // 2636867
FIELD: medicine.SUBSTANCE: preliminary study of the cognitive and psychological status of the patient is performed. Combined anaesthesia is performed, including inhalation endotracheal sevoflurane anaesthesia and prolonged epidural analgesia. In this case, when a patient is diagnosed with initial cognitive impairment, chronic pain syndrome, anxiety and depression, a potentized anaesthetic with sevoflurane at a dose of 1.8-2.0% in oxygen is performed in the preoperative period. Immediately after trachea intubation, micro-jet infusion of dexmedetomidine is added at a dose of 0.4-0.8 mcg/kg/h, which is continued until suturing of the postoperative wound begins. The bispectral index of the electroencephalogram during the operation is maintained in the range of 40-60%.EFFECT: method allows to increase the effectiveness of prevention of early POCD development in patient subject to surgery due to GIT cancer, to reduce the opioids dose, to exclude the risk of application of excessively high doses of anaesthesia drugs.2 ex
Combined drug for primary neuroprotection // 2636616
FIELD: pharmacology.SUBSTANCE: drug containing glycine and thiotriazoline is presented.EFFECT: high primary neuroprotective activity due to mutually reinforcing action, which are part of the preparations, and a wide range of biological effects.3 cl, 4 tbl
Composition containing alpha-lipoic acid and honokiol, for treatment of neuropathies // 2636613
FIELD: pharmacology.SUBSTANCE: invention relates to a composition comprising alpha-lipoic acid or a salt thereof and honokiol, wherein the amount of honokiol is 1% to 30% by weight based on the total weight of honokiol and alpha-lipoic acid. A pharmaceutical preparation and a dietary preparation for oral administration are also described. The preparations may be in the form of pills or capsules.EFFECT: drug is effective for treatment or prevention of peripheral neuropathies.17 cl, 2 dwg, 3 tbl, 3 ex
Compositions containing vortioxetine and donepezil // 2635528
FIELD: pharmacology.SUBSTANCE: invention is a pharmaceutical composition comprising vortioxetine and donepezil together with a pharmaceutically acceptable excipient, the composition is for treatment of a disease selected from cognitive dysfunction, dementia in Alzheimer's disease, dementia of vascular genesis, dementia in Pick's disease, dementia in Creutzfeldt-Jakob disease, dementia in Huntington's disease, dementia in Parkinson's disease, dementia in the human immunodeficiency virus, dementia in persons abusing alcohol or medication, moderate cognitive impairment, cognitive dysfunction associated with depression, and cognitive dysfunction associated with schizophrenia.EFFECT: invention provides a synergistic increase in the extracellular level of acetylcholine in the brain.12 cl, 5 ex, 1 tbl, 6 dwg
 
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