Heterocyclic compounds (C07D)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D              Heterocyclic compounds (macromolecular compounds c08)(22987)

Fluorine-9-methyl-β-carbolines // 2642785
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) , where R1 is -F, and R2 is -H or -F, or R1 is -H, and R2 is -F; which can be used as a medicine for treatment of diseases and/or injuries of the inner ear.EFFECT: increased efficiency of compounds.10 cl, 30 dwg, 1 tbl, 9 ex
Forzicyaside sulfate and its derivatives, method for its production and its application // 2642784
FIELD: pharmacology.SUBSTANCE: invention relates to forzicyaside sulfate and its derivative represented by the following formula , wherein R is Na+, K+ or NH+, and a method for their preparation, as well as an antiviral drug based on them and its use.EFFECT: increased efficiency of agents.10 cl, 9 tbl, 2 dwg
New benzoazepine derivative and its medical application // 2642783
FIELD: pharmacology.SUBSTANCE: invention relates to a new benzoazepine derivative of formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a hydroxyl group, a lower alkoxy group or , where A is absent or a lower alkylene group which may be substituted by a lower alkyl group; R6 represents a hydrogen atom or a lower alkyl group; R7 represents a hydrogen atom, a hydroxyl group, a five-membered aromatic heterocyclic group containing 3 heteroatoms selected from nitrogen and oxygen which may be substituted by a lower alkyl group, a five-membered non-aromatic heterocyclic group containing one nitrogen atom which may be substituted by an oxo group or a carbamoyl group , which may be substituted by a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 is a lower alkyl group which may be substituted by 1 to 3 fluorine atoms or a halogen atom; R4 represents a lower alkoxy group which may be substituted by 1 to 3 halogen atoms, a five-membered aromatic monocyclic heterocyclic group or a five-membered non-aromatic monocyclic heterocyclic group (provided that each of these heterocyclic groups contains one nitrogen atom, two nitrogen atoms or one nitrogen atom and one oxygen atom in the ring, and may contain a lower alkyl group); and R5 represents a hydrogen atom, a lower alkyl group or a halogen atom. The invention also relates to a pharmaceutical composition based on a compound of the formula and intermediates of the formulas and .EFFECT: new benzoazepine derivatives having V2 receptor agonist activity are obtained.14 cl, 12 tbl, 128 ex
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
ethod for obtaining of 1-r-indole-3-ylsulfanylacetates of (2-hydroxyethyl)ammonium // 2642778
FIELD: pharmacology.SUBSTANCE: invention relates to a method for the preparation of indole-1-H-, 1-methyl-, 1-benzylindole-3-ylsulfanylacetate of (2-hydroxyethyl)ammonium heterocyclic compounds that have a broad spectrum of action, for example, selective erythropoiesis and immunomodulators with a minimum potential for undesirable effects on various body systems, and can be used to prevent and treat immune-dependent lesions that occur with anaemia, cancer and inflammatory diseases, complications with organs and bone marrow transplantation, protection against cardiogenic shock, stresses, etc. The method consists in the reaction of 1-R-indole-3-ylsulfanyl acetic acids with (2-hydroxyethyl)amines - triethanolamine, methyldiethanolamine, dimethylethanolamine without solvent upon heating to 60-65°C for 0.5-1 hour, with washing of the resulting salt with ether. The yield is 92-99%. The initial 1-R-indole-3-ylsulfanyl acetic acids (compounds 2) are obtained for this reaction from 1-H- or 1-methyl-or 1-benzylindole with thiourea, bromine, potassium bromide, taken in the molar ratios of 1:2:1:1, respectively, in a water medium at a temperature of 30-40°C for 3 h in inert gas, with subsequent processing of the reaction mass by an aqueous solution of sodium hydroxide, then an aqueous solution of monochloroacetic acid taken in the molar ratios of indole, sodium hydroxide, acid 1:(4-5):(1-1.2), heating of the reaction mixture at 90-100°C for 3 h at a pH of 9-10 with subsequent acidification with hydrochloric acid until pH=1 with a yield of 92-95%. Purity is 98.7-99.7. Replacement of scarce and expensive iodine and potassium iodide in alcohol solution with a more accessible aqueous solution of bromine and sodium bromide, excluding toxic hydrazine hydrate and toxic solvent (alcohol) from the process leads to a decrease in product cost and an increase in environmental fire safety, since the reaction is carried out in an aquatic environment. , R=H, CH3, CH2C6H5; R1, R2=H, CH3, CH2CH2OH; n=1-3.EFFECT: increased efficiency of compounds application.2 cl, 2 dwg, 8 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
ethod of producing trans-1,4,5,8-tetranitroso-1,4,5,8-tetraazadecalin // 2642470
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing trans-1,4,5,8-tetranitroso-1,4,5,8-tetraazadecalin by the condensation of glyoxal with ethylenediamine in the presence of sodium nitrite and acetic acid with subsequent dosage of the reaction mixture in dilute mineral acid, in which 30-40% sulfuric acid is used as mineral acid, and p-toluensulfonate is introduced into a mixture of glyoxal, ethylene diamine, sodium nitrite, acetic acid.EFFECT: development of highly effective environmentally safe way of obtaining a compound.2 cl, 1 tbl, 8 ex
ethod of producing nitronylnitroxyl radical 2-(5-methyl-1n-imidazole-4-yl)-4,5-bis(spiropentane)-4,5-dihydro-1n-imidazol-3-oxid-1-oxyl // 2642468
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing nitronylnitroxyl radical 2-(5-methyl-1N-imidazole-4-yl)-4.5-bis(spiropentane)-4.5-dihydro-1N-imidazole-3-oxide-1-oxyl, which consists in interacting 1.1'-dihydroxylation-bicyclopentyl produced by the neutralisation of the alkaline agent to the corresponding sulfate salt of 1,1'-dihydroxylation-bicyclopentyl, 4-methylimidazole-5-carbaldehydes in an aqueous solution when heated, and by the oxidation of the resulting product with sodium periodate, with the subsequent release of the specified nitronylnitroxide radical. .EFFECT: application as an effective and low-toxic contrast agent for MR-tomography of living organisms.2 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
Cyclopropane carboxylate ethers of purine analogues // 2642463
FIELD: pharmacology.SUBSTANCE: invention relates to new cyclopropane carboxylate esters of purine analogues of the formula (T) or pharmaceutically acceptable salts thereof, which can be used for treatment of herpesvirus infections. Herpesvirus infection is an infection caused by the herpes simplex virus, infection of herpes zoster, or cytomegalovirus infection. In the compound of the formula (T) each Rx and Rz is independently hydrogen or (C1-C6)alkyl, or Rx is hydrogen and Rz is (C1-C6)alkyl, or Rx is (C1-C6)alkyl and Rz is hydrogen; and Ry is (C1-C6)alkyl, halo (C1-C6)alkyl, C6aryl, haloC6aryl or (C4-C5)heteroaryl with one heteroatom selected from nitrogen and oxygen in the ring.EFFECT: increased efficiency of compounds application.7 cl, 5 dwg, 3 tbl, 16 ex
ethod for obtaining of n-aryl-substituted 3h-imidazo[4,5-b] pyridines // 2642456
FIELD: pharmacology.SUBSTANCE: invention relates to a method of obtaining N-aryl-substituted 3H-imidazo[4,5-b] pyridines, formula shown below, where R=H, OCH3, CH3, Cl, involving nucleophilic substitution of the chlorine atom in 2-chloro-3-nitro-6-R-pyridine in a reaction with imidazole, deoxidizing isomerization recycling of N-(3-nitro-6-R-pyrid-2-yl) benzimidazoles. Nucleophilic substitution is carried out in DMF in the presence of K2CO3 for 1 hour at a temperature of 50°C and molar ratio of 2-chloro-3-nitro-6-R-pyridine:benzimidazole:K2CO3=1:1:1.5, deoxidizing isomerization recycling of N-(3-nitro-6-R-pyrid-2-yl)benzimidazoles is performed by SnCl2⋅2H2O at a temperature of 80°C for 20 h in a mixture of isopropanol and 18% hydrochloric acid taken in a volumetric ratio of 1:1, and molar ratio of 1-(3-nitro-6-R-pyridine-2-yl)-1H-benzimidazole : SnCl2⋅2H2O=1:3.5.EFFECT: method is developed for preparation of these derivatives, which can be used as precursors for drugs.8 ex

7-(4-methoxyphenyl)-5-phenyl-4,5-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine as activator of glucokinase and inhibitor of dipeptidyl peptidase of type 4 and method of its production // 2642432
FIELD: chemistry.SUBSTANCE: invention relates to 7-(4-methoxyphenyl)-5-phenyl-4,5-dihydro-[1,2,4]triazolo [1,5-a]pyrimidine as an activator of glucokinase and an inhibitor of dipeptidyl peptidase of type 4: . The invention also relates to the method of its production.EFFECT: new compound is produced that can be used as an activator of glucokinase and an inhibitor of dipeptidyl peptidase of type 4.2 cl, 3 dwg, 3 ex
Amide derivatives as grp119 agonists // 2642429
FIELD: pharmacology.SUBSTANCE: invention relates to an amide derivative of the following formula 1, its stereoisomers or its pharmaceutically acceptable salts of formula 1, wherein X1, X2, X3, X4, X5, X6, X7 and X8 each independently is C or N; R1 is -F or -C1-3-perfluorinated alkyl; R2 and R3 each is independently selected from the group consisting of halogen, -C1-5-alkyl and C3-6-cycloalkyl, wherein -C1-5-alkyl and C3-6cycloalkyl independently of one another may be unsubstituted or substituted by halogen, -CN, -OC1-5-alkyl or-C1-5-alkyl, or R2 and R3 together with the carbon atom to which they are attached, can form C3-6-cycloalkyl, where C3-6cycloalkyl may be unsubstituted or substituted by halogen, -OC1-5-alkyl or -C1-5-alkyl; R4 and R5 each independently is H, halogen or -C1-5-alkyl; R6 and R7 each independently is H, halogen, -C1-5-alkyl or -CN; R8 means methyl; R9 means H, halogen or OH; and m is 1 or 2. The invention also relates to individual compounds and to a pharmaceutical composition.EFFECT: new compounds of formula 1 are obtained that have the properties of GPR119 agonists, which can be used in diabetes mellitus treatment.7 cl, 15 tbl
N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines with antibacterial activity and method for their obtaining // 2642428
FIELD: pharmacology.SUBSTANCE: invention relates to new N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines of general formula I , where a: R1=R2=R3=H; b: R2=CH3, R1=R3=H; c: R2= OCH3, R1=R3=H; d: R1=R2=R3=OCH3 and a method for their preparation, in which 5-bromo-4-(5-nitrofuran-2-yl)pyrimidine (6) is mixed with the corresponding arylamine taken in 1.5 times excess, palladium (II) acetate and 1,1'-bis (diphenylphosphino)ferracene taken in catalytic amounts and potassium phosphate taken in 2.5-fold excess, the resulting mixture is dissolved in degassed 1,4-dioxane and heated at 85°C with vigorous stirring for at least 15 hours, followed by solvent distillation on a rotary evaporator under reduced pressure, and the resulting residue is subjected to chromatographic separation on a silica gel column with a ratio of ethyl acetate: hexane components of 1:3 in the eluent.EFFECT: highly effective method is proposed for the preparation of a compound that has a broad spectrum of antibacterial activity against coccal infections caused by gonococci or staphylococcus aureus, as well as purulent inflammatory infectious diseases of skin and mucous membranes caused by staphylococci and streptococci.2 cl, 1 tbl, 4 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 of producing 6-ethoxycarbonyl-7- (thien-2-yl) -5-methyl-4,7-dihydro-1,2,4-triazolo [1,5-a]pyrimidine that has high tuberculostatic activity // 2642420
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing 6-ethoxycarbonyl-7-(thien-2-yl)-5-methyl-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidine having tuberculostatic activity of the formula , which consists in interaction of 2-thiophenaldehyde, acetoacetic ester and 3-amino-1,2,4-triazole by heating in a solvent, where water is used as the solvent, with a molar ratio water: 2-thiophenaldehyde: acetoacetic ester: 3-amino-1,2,4-triazole is 55:1:1:1.EFFECT: new simple technological method of obtaining a compound that does not require special equipment and acids and large volumes of organic solvents is developed.3 ex
ethod for production of hydroxylated cyclopentapyrimidine compounds and their salts // 2642311
FIELD: biotechnology.SUBSTANCE: method for production of a formula III compound or a salt thereof, . The compound of formula or its salt is brought into contact with ketoreductase or alcohol dehydrogenase enzyme.EFFECT: invention allows stereoselective reduction of a compound of formula II or a salt thereof to a compound of formula III or a salt thereof that is suitable for further synthesis of ACT protein kinase activity inhibitors.15 cl, 3 dwg, 2 tbl, 6 ex
Spiro-fused piperidine derivatives for application as inhibitors of external medullar layer potassium channel // 2642066
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula I .EFFECT: new compounds of formula I are obtained which are inhibitors of the ROMK channel and which can be used in hypertension treatment.11 cl, 5 tbl, 85 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
4-amino-3-methoxymethyl-5-phenyl-1h-pyrazole // 2642060
FIELD: pharmacology.SUBSTANCE: invention relates to preparation of new 4-amino-3-methoxymethyl-5-phenyl-1H-pyrazole previously not described. 4-amino-3-methylamide-5-phenyl-1H-pyrazole that has the following equation, derived from cycloaromatization of isonitrosodiketone and restoration of a new, not previously described intermediate - 4-nitroso-3-methylamide-5-phenyl-1H-pyrazole. The resulting target compound shows high antibacterial activity against E. coli (Escherichia coli strain ATCC 25822, sensitive to antibiotics) that allows its use in pharmacology to create antibacterial drugs. .EFFECT: increased efficiency of compounds application.2 ex
Heterocyclic compounds as pesticides // 2641916
FIELD: chemistry.SUBSTANCE: non-therapeuticuse of heterocyclic compounds of the formula for controlling animal pests, including arthropods, insects, and nematodes.EFFECT: invention allows to realise the specified purpose.18 cl, 5 tbl, 48 ex
3-aminocyclopentancarboxamide derivatives // 2641913
FIELD: chemistry.SUBSTANCE: invention relates to the individual compounds selected from the group: 4-(1,3-benzoxazole-2-yl)]-N-[(1R,3S)-3-(ethylcarbamate)cyclopentyl]-N-methylbenzamide, N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methyl-4-(1-methyl-1H-benzoimidazol-2-yl)-benzamide, 4-benzothiazol-2-yl-N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methylbenzamide, ((1R,3S)-3-ethylcarbamoylcyclopentyl)-methylamide4'-[(R)-(tetrahydrofuran-3-yl)oxy]-biphenyl-4-carbon acid, 4-benzoxazole-2-yl-N-((1R,3S)-3-isopropylcyclopentadienyl)-N-methylbenzamide, and other compounds that are specified in the claims. The invention also relates to medicinal means having an inhibiting activity against fatty acid synthase (FAS) containing therapeutically effective amount of the compound of the invention.EFFECT: new compounds are obtained that have an inhibiting activity against the synthesis of fatty acids.2 cl, 2 tbl, 12 ex

Crystalline forms of complexes useful as sglt2 inhibitors, and methods of their obtaining // 2641905
FIELD: chemistry.SUBSTANCE: invention relates to the crystalline form of the complex (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-ylpropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, bis(L-proline) characterized by an X-ray powder diffraction pattern comprising peaks at 4.08, 17.19, and 21.12 degrees 2θ (±0.05 degrees 2θ), wherein the said X-ray powder diffraction pattern is obtained using CuKα1 radiation.EFFECT: provided complex has an inhibitory effect on the sodium-dependent SGLT transporter.7 cl, 1 tbl, 3 dwg, 7 ex
Connection of spatially hindered phenol, its obtaining and its application as antioxidant // 2641904
FIELD: chemistry.SUBSTANCE: invention relates to a novel compound of the sterically hindered phenol of the formula (I) , wherein the groups R and R' are defined in the invention formula that is used as an antioxidant, a method for its preparation, its use as an antioxidant and a lubricating oil composition.EFFECT: expansion of the application field.20 cl, 18 tbl, 67 ex

New salicylic acid derivatives, their pharmaceutically acceptable salt, compositions and method for application // 2641903
FIELD: pharmacology.SUBSTANCE: invention relates to a number of other similar specific compounds, pharmaceutical compositions, comprising these compounds and their application to obtain a drug to inhibit the STAT3 and/or STAT5 activity or to treat cancer, where the cancer cells contain activated STAT3 or STAT5. , , , .EFFECT: preparation of a drug for STAT3 and STAT5 activity inhibition or for cancer treatment where the cancer cells contain activated STAT3 or STAT5.20 cl, 21 dwg, 6 tbl, 76 ex
Heterocyclic pyrimidine analogues as tyk2 inhibitors // 2641895
FIELD: pharmacology.SUBSTANCE: compounds possess the properties of the inhibitor of the non-responsive tyrosine Tyk2 kinase and selective inhibitory action against JAK1, JAK2, JAK3 Janus kinases. The compounds can be used in a method for treatment or prevention of immunological, inflammatory, autoimmune, allergic disorder or graft rejection or graft-versus-host diseases. In the formula (I) , R1 is H; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R3, which are the same or different. At that, C 1-6 alkyl containing a hydroxy group may be deuterated; R3 represents halogen; CN; C(O)OR4; OR4; C(O)R4; (O)N(R4R4a); S(O)2R4; S(O)R4; or T1; R4, R4a, R4b are independently selected from the group consisting of H; T1; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R5, which are the same or different; R5 represents halogen; CN; OR6; or T1; R6 is H; T1 is C3-7 cycloalkyl; 4-7 membered heterocyclyl with 1 to 2 heteroatoms in the ring selected from nitrogen, oxygen or sulfur; or a 7-8 membered heterobicyclyl, optionally spyrocondensed, with two heteroatoms in the cycle, selected from nitrogen or nitrogen and oxygen, where T1 is optionally substituted by one or more R7 , which are the same or different; R7 is halogen; CN; C(O)OR8 ; oxo (= O), wherein the ring is at least partially saturated; C 1-6 alkyl; R 8 are independently selected from the group consisting of H; C1-6 alkyl; X1 is C(R11a) or N; X2 is C(R11b) or N; X3 is C(R11c) or N; X4 is C(R11d) or N; X5 is C(R11e) or N, provided that no more than two of X1, X2, X3, X4, X5 are N; R11a, R11c, R11e are independently selected from the group consisting of H; halogen; CN; OR12; C(O)N(R12 R12a); S(O)2N (R12R12a); S(O)2R12; T2; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R11b, R11d are independently selected from the group consisting of H; halogen; CN; OR12; S(O)2N (R12R12a); S(O)R12; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R12, R12a are independently selected from the group consisting of H and C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; T2 is a 5-membered heterocycle with two nitrogen atoms in the ring; R13 is halogen; CN; OR14; C(O)N (R14R14a); S(O)2N(R14R14a); S(O)2R14; S(O) R14; N(R14) S(O)2N(R14aR14b); N(R14)S(O)N(R14aR14b); SR14; N(R14R14a); NO2; OC(O)R14; N(R14)S(O)2R14a; R14, R14a, R14b are independently selected from the group consisting of H or C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R15, which are the same or different; R15 is halogen.EFFECT: increased efficiency.18 cl, 13 tbl, 480 ex
Azole derivatives of benzene // 2641891
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 means OR, NRR', which can form a ring, or SR. Wherein R and R' independently mean hydrogen atom, linear, cyclic or branched alkyl containing 1-8 carbon atoms, and optionally substituted by one or more linear, circular, or branched alkoxygroup containing 1-8 carbon atoms, halogen atoms or hydroxyl groups, monocyclic or bicyclic aryl containing 6-10 carbon atoms, optionally substituted by one or more linear, cyclic or branched alkyl containing 1-8 carbon atoms, linear, cyclic or branched alkoxygroup containing 1-8 carbon atoms, or halogen atoms, where the term "NRR' forms a ring" means that R and R' join to form pyrrolidine-1-yl group; R2 means a hydrogen atom or a linear, cyclic or branched alkyl containing 1-8 carbon atoms; X1, X2 and X3 mean independently CR3 or a nitrogen atom, or X1 means CR3 or a nitrogen atom, and X2 and X3 together form a benzene ring. Moreover, R3 means a hydrogen atom or a linear, cyclic or branched alkyl having 1-8 carbon atoms. The invention also relates to specific compounds corresponding to formula (I). The invention relates to an intermediate compounds represented by the formulas, and , where R1, R2, X1, X2 and X3 correspond to the values given for compounds of formula (I) and R4 means protective group of the carboxylic group, selected from methyl, ethyl, isopropyl, heptyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, propanol and benzyl, and R5 means a protective group of phenolic hydroxyl group selected from methyl, isopropyl, allyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, 1-ethoxyethyl, benzyl, 4-methoxybenzyl, acetyl, trimethylsilyl, t-butyldimethylsilyl. The compounds of the invention of formula (I) have an inhibitory activity against xanthine oxidase.EFFECT: azole derivatives of benzene as inhibitors of xanthine oxidase.19 cl, 15 tbl, 58 ex

ethod of producing (1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid // 2641699
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the method of producing (1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolo [3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid of the formula (6), which comprises adding tert-butyl octahydro-1H-pyrrolo [3,4b] pyridine-1-carboxylate into a compound of the formula to form a compound of the formula , reacting the compound (2) with triethylorthoformate in acetic anhydride to form a compound of the formula , attaching a cyclic amine to the compound of the formula (3) to form a compound of the formula ; cyclizing a compound of the formula (4) under alkaline conditions to form a compound of the formula ; cleaving the Boc protecting group from the compound of the formula (5) to form the final compound of the formula .EFFECT: improved method of producing acid of the formula, the method is characterized by its simplicity, economy, and low environmental risk.5 cl, 5 dwg, 5 ex
5-(pyridine-2-ylamino)-pyrasin-2-carbonitrile compounds and their therapeutic application // 2641693
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula , as well as to pharmaceutical compositions based thereon for use in the treatment of a disease or condition mediated by SNK1.EFFECT: new compounds are obtained that inhibit the kinase function of kinase 1 of the control point.37 cl, 2 dwg
New anti-invasive compounds // 2641650
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, which can be used to prevent, and/or inhibit, and/or treat cancer. In formula (I) A and A' independently represent phenyl or pyridylene group; R2 represents a hydrogen or alkyl group (C1-C4); R3 represents a 2-pyridyl group, 3-pyridyl group, 4-pyridyl group, 2-pyrimidinyl group, 4-pyrimidinyl group or 5-pyrimidinyl group; R4 represents a carbonyl group or sulfonyl group; R5 is a -NH-(CH2)(a)-NR6R7 group or a 4-methylpiperazinyl group and a is an integer from 1 to 4, R6 and R7 independently represent a nalkyl group (C1-C4) or R6 R7 together with nitrogen atom they are bounded to form a heterocyclic group selected from 4-methylpiperazinyl group, morpholine group, pyrrolidinyl group and piperidine group. The invention also relates to a method for preparation of compounds of formula (I) and a pharmaceutical composition containing them.EFFECT: improved compounds properties.16 cl, 6 tbl, 17 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
Antiseptic drug // 2641309
FIELD: pharmacology.SUBSTANCE: invention relates to the organic heterocyclic compounds chemistry, namely a new quaternary ammonium salt containing a fragment of a vitamin B6 derivative of formula I , which exhibits antibacterial, antimycotic, antiviral and antiprotozoal properties.EFFECT: compound can be used in medicine and veterinary medicine.2 cl, 2 dwg, 16 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
eans for combating pests // 2641295
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the general formula (I) , where R1 represents a halogen atom, an amino group, a hydroxyl group, a mercapto group, a cyano group, a nitro group, a (C1-C6) alkyl group, a (C2-C6) alkenyl group, a (C2-C6) alkynyl group, a (C3-C6) cycloalkyl group, a (C1-C6) a halogen alkyl group, a (C1-C6) alkoxy group, a (C2-C6) alkenyloxy group, a (C2-C6) alkynyloxy group, a (C3-C6) cycloalkoxy group, a (C1-C6) halogen alkoxy group, a (C1-C6) alkylthio group, a (C2-C6) alkenylthio group, a (C2-C6) alkynylthio group, a (C3-C6) cycloalkylthio group, a (C1-C6) halogen alkylthio group, a (C1-C6) alkylamino group, a (C2-C6) alkenylamino group, a (C2-C6) alkynylamino group, a di (C1-C6) alkylamino group, a di (C2-C6) alkenylamino group, a di (C2-C6) alkynylamino group, a (C1-C6) alkylsulfinyl group, a (C2-C6) alkenylsulfinyl group, a (C2-C6) alkynylsulfinyl group, a (C3-C6) cycloalkylsulfinyl group, a (C1-C6) halogen alkylsulfinyl group, a (C1-C6) alkylsulfonyl group, a (C2-C6) alkenylsulfonyl group, a (C2-C6) alkynylsulfonyl group, a carboxyl group, a (C1-C6) alkylcarbonyl group, a (C1-C6) alkoxycarbonyl group, a (C1-C6) alkylaminocarbonyl group, a di (C1-C6) alkylaminocarbonyl group, a (C1-C6) alkylcarbonyloxy group, a (C1-C6) alkylcarbonylamino group, or a (C1-C6) alkylcarbonyl group, a (C1-C6) alkylamino group; R2 is a halogen atom, a hydroxyl group, a mercapto group, a nitro group, a (C1-C6) alkyl group, a (C2-C6) alkenyl group, a (C2-C6) alkynyl group, a (C1- C6) halogen alkyl group, a (C1-C6) alkoxy group, a (C2-C6) alkenyloxy group, a (C2-C6) alkynyloxy group, a (C1-C6) alkylthio group, a (C2-C6) alkenylthio group, a (C2-C6) alkynylthio group, a (C1-C6) alkylamino group, a (C2-C6) alkenylamino group, a (C2-C6) alkynylamino group, a di (C1-C6) alkylamino group, a di (C2-C6) alkenylamino group, a di (C2-C6) alkynylamino group, a (C1-C6) alkylsulfinyl group, a (C2-C6) alkenylsulfinyl group, a (C2-C6) alkynylsulfinyl group, a (C1-C6) alkylsulfonyl group, a (C2-C6) alkenylsulfonyl group, a (C2-C6) alkynylsulfonyl group, a (C1-C6) alkyloxy (C1-C6) alkyl group, a (C1-C6) alkylthio group (C1-C6) alkyl group, a (C1-C6) alkylamino (C1-C6) alkyl group, a di (C1-C6) alkylamino (C1-C6) alkyl group, a hydroxy (C1-C6) alkyl group, a carboxyl group, a (C1-C6) alkylcarbonyl group, a (C1-C6) alkylaminocarbonyl group, a di (C1-C6) alkylaminocarbonyl group, a (C1-C6) alkylcarbonyloxy group, a (C1-C6) alkylcarbonylthio group, a (C1-C6) alkylcarbonylamino group, or a di (C1-C6) alkylcarbonylamino group; W is CH or a nitrogen atom; n is an integer from 1 to 4; or its salt, which is used as an insecticide or means for the destruction of animal pests.EFFECT: increasing the efficiency of the means.5 cl, 3 tbl, 12 ex

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
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
Quinine compounds, method for their production and their medical application // 2641285
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt or optical isomer thereof, wherein, in formula I, n is selected from 1 to 7, R1 means C3-C7 hydrocarbyl, which may be unsubstituted or optionally substituted by halogen, alkoxy, alkoxycarbonyl, heterocyclyl or aryl; R2 is aryl or heteroaryl containing one or more heteroatoms selected from N, O or S which may be unsubstituted or optionally substituted by one or more substituents of halogen, phenyl, -OR6, -SR6, -NR6R7, -NHCOR6, -CONR6R7, -CN, -NO2, -COOR6, -CF3 or linear or branched C1-C4 hydrocarbyl, R6 and R7 can denote a hydrogen atom or linear or branched C1-C4 hydrocarbyl; R3 is hydroxyl, halogen, alkoxy or acyloxy. Alkoxy or acyloxy may be unsubstituted or optionally substituted by halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl; R4 and R5 may or may not be present, and, independently, can mean, without limitation, a substituent such as halogen, hydroxyl, alkoxy, hydrocarbyl, alkoxyhydrocarbyl, heterocyclyl or aryl when these radicals are present. Y is linear or branched C1-C7 alkyl or - (CH2-O-CH2)m-, which may be optionally substituted by halogen, hydroxyl, alkoxy, alkoxyalkyl, unsaturated hydrocarbyl, cyclic hydrocarbyl or heterocyclyl. M is 1-3; X- means an acid residue or hydroxyl, the said compounds having a selective antagonistic effect on the M1 and M3 receptors subtypes, but insignificantly affect the M2 receptor subtype.EFFECT: compound application efficiency increase.24 cl, 5 tbl, 33 ex
ethod for producing 1-phenyl-3-(4h-1,2,4-triazol-4-yl) urea // 2641109
FIELD: chemistry.SUBSTANCE: invention relates to the method of producing 1-phenyl-3-(4H-1,2,4-triazol-4-yl) urea of the formula I , which is carried out by reacting (4H-1,2,4-triazol-4-yl) amine and 1,3-diphenylurea in a molar ratio of 3:1 to 4:1 at a temperature of 170-182°C under vacuum with distillation of aniline.EFFECT: new method for preparing a compound of formula I without the use of toxic starting materials and solvents is developed.1 dwg, 4 ex
Sodium salt of 3-nitro-4-oxo-1,4-dihydropyrazolo[5,1-c]-1,2,4-triazine-8-carboxylic acid, dihydrate // 2641107
FIELD: chemistry.SUBSTANCE: invention relates to sodium salt of 3-nitro-4-oxo-1,4-dihydropyrazolo[5,1-c]-1,2,4-triazine-8-carboxylic acid, dihydrate, .EFFECT: new compound showing antiglating properties is produced.2 tbl, 3 ex

Salt of nitrogen-containing heterocyclic compound or its crystalline form, pharmaceutical composition and flt3 inhibitor // 2641106
FIELD: pharmacology.SUBSTANCE: invention relates to new salts of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide selected from succinate, fumarate, pamoate, hydrochloride, phosphate, sulfate and hydrobromide, as well as crystalline salt forms. The compounds possess the properties of FLT3 (Fms-like tyrosine kinase 3) inhibitor and can be used to treat blood carcinoma including various forms of leukemia, for example acute lymphatic leukemia (ALL), acute myeloid leukemia (AML), acute promyelocytic leukemia (APL), chronic lymphocytic leukemia (CLL), and others. Crystalline α succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 10.5, 17.1, 19.1 and 22.4°; crystalline β succinate of this compound demonstrates diffraction peaks at diffraction angles of (2θ) 12.8, 16.1, 21.4 and 28.0°. Crystalline fumarate of the said compound on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 8.6, 13.7, 17.8 and 23.0°.EFFECT: salts have storage stability or high solubility.9 cl, 6 dwg, 10 tbl, 13 ex
ethod of producing 2,3-disubstituted 1-hydroxy-1h-indole-5,6-dicarbonitriles // 2641006
FIELD: chemistry.SUBSTANCE: invention relates to the method of prosucing novel 2,3-disubstituted 1-hydroxy-1H-indole-5,6-dicarbonitriles in which R1=C6H5, or 4-CH3C6H4, or 4-OCH3C6H4, or 2-thienyl, R2=CH3, or C2H5, or C3H7, which can be used as precursors for the synthesis of biologically active substances, drugs, phthalocyanines, hexazocyclones. The method of producing 2,3-disubstituted 1-hydroxy-1H-indole-5,6-dicarbonitriles involves two steps. At the first step, 2-substituted 1-hydroxy-1 h-indole-5,6-dicarbonitriles interact with aliphatic acid anhydrides of carboxylic acids (acetic, propionic, oil anhydride) in the presence of boron-fluoride-three etherate (BF3Et2O). At the second step, obtained corresponding 3-acetamidine 2-aryl(heteryl)-1H-indole-5,6-dicarbonitriles interact with potassium carbonate in the environment of isopropyl alcohol, followed by acidification and production of the desired 2,3-disubstituted 1-hydroxy-1H-indole-5,6-dicarbonitriles. .EFFECT: new compound is produced that has high energy characteristics.8 ex
Biaryl derivatives as agonists gpr120 // 2641003
FIELD: pharmacology.SUBSTANCE: invention relates to diaryl derivatives of the formula 1 , or their pharmaceutically acceptable salts or isomers of formula 1, wherein A and B are independently phenyl or pyridine provided that when B is phenyl, -G-COOR7 is substituted in the para-position of phenyl and, when B is pyridine, -G-COOR7 is substituted in position 3 of pyridine, any of R1-D and R2-E may be absent, D and E are independently carbon, nitrogen, oxygen or sulfur, or represent a direct bond, and any of R1 and R2 may be absent, or R1 is a halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted by C3-C10-alkylsilanyloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted by C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl, R2 is hydrogen, halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted with C3-C10-alkylsilaniloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted with C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl and, when D and E represent nitrogen or carbon, R1 and R2 may represent two or three groups, which may be the same or different, isolated from C1-C6-alkyl or phenyl, G is -J-(CR5C6)p, where J is oxygen or sulfur, R5 and R6 independently represent hydrogen, C1-C6-alkyl or C3-C10-cycloalkyl and R5 and R6, substituted in the one and the same or different carbon atoms, may be bound producing C3-C10-cycloalkyl, R1 and R4 independently from each other may be absent depending on m and n value or independently represent hydrogen, halogen or C1-C6-alkyl, or C1-C6-alkoxy, R7 is hydrogen or C1-C6-alkyl, m and n independently represent an integral number from 0 to 5 and p is an integral number from 2 to 6, where heterocycloalkyl and heteroaryl contain at least one heteroatom, isolated from N, O, and S, to the pharmaceutical composition, containing them, and method of its production.EFFECT: stimulates the formation of GLP-1 in the gastrointestinal tract and improves insulin resistance in the liver or muscles, effective prevention or treatment of diabetes, complications of diabetes, obesity, non-alcoholic fatty hepatosis, steatohepatitis, osteoporosis or inflammation.6 cl, 1 tbl, 279 ex

Salts of 4-((2-(6-(4-methylpiperazine-1-carbonyl)-naphthalen-2-yl)ethyl) amino)quinazoline-6-carbonitrile and pharmaceutical composition // 2641001
FIELD: pharmacology.SUBSTANCE: invention relates to the salts of 4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile, which have the properties of a cyclin-dependent CDK8/CDK19 kinase inhibitor, and to pharmaceutical compositions comprising these salts, and to the use of such salts or such compositions for treatment of diseases or disorders mediated by the cyclin-dependent CDK8/19 kinase.EFFECT: new salts are obtained, which have improved solubility compared to the free base.13 cl, 5 tbl, 23 ex, 5 dwg
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

Chiral diacylhydrazine ligands for modulation of exogenous genes expression by ecdysone-receptor complex // 2640807
FIELD: biotechnology.SUBSTANCE: invention relates to a method for preparation of an enantiomerically enriched compound with Formula III , wherein A is (C1-C6)alkyl-O-, phenyl- C1-C6)alkyl-O-; aryl selected from phenyl, naphthyl, benzo 1,3]dioxole, 2,3-benzo[1,4]dioxin which is optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6) alkyl, (C3-C7) cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo; or heteroaryl having four or five carbon atoms and one heteroatom selected from oxygen, nitrogen and sulfur, which is optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo; B is phenyl optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo; and R1 and R2 independently represent (C1-C6)alkyl, phenyl-(C1-C6)alkyl-, hydroxy-(C1-C6)alkyl, (C3-C7)cycloalkyl, (C2-C6)alkenyl or (C2-C6)alkynyl; provided that R1 differs from R2; where the absolute configuration of the asymmetric carbon atom carrying R1 and R2, is an R-configuration; including (a) reaction of Formula XI acylhydrazine with Formula XII ketone to form a compound of Formula XIII , where R1 differs from R2, (b) reduction of the Formula XIII compound in the presence of a chiral catalyst to form a Formula R-XIV compound and (c) reaction of the Formula R-XIV compound with the Formula B-CO-LG compound, wherein LG is a leaving group, forming a compound with Formula III.EFFECT: chiral diacylhydrazine ligands for genome modulation.6 cl, 25 dwg, 11 tbl
ethod for obtaining isothiazol derivative // 2640806
FIELD: chemistry.SUBSTANCE: invention relates to a method for obtaining an isothiazol derivative represented by the general formula (3), wherein R is a cyano group, a carboxy group or an alkoxycarbonyl group; and X represents a fluorine atom, a chlorine atom, a bromine atom or an iodine atom. The method is carried out by heating a nitrile compound represented by the general formula (1) and sulfur. The reaction is then carried out between the nitrile compound represented by the general formula (1), sulfur and halogen represented by the general formula (2), where R and X are as defined above. The nitrile compound and sulfur are heated to a temperature in the range of 70 to 180°C. The reaction between the nitrile compound represented by the general formula (1), sulfur and halogen represented by the general formula (2) is carried out by charging the nitrile compound and sulfur and then halogen is introduced.EFFECT: providing a safe industrial manufacturing process by eliminating the simultaneous use of an aprotic polar solvent such as N,N-dimethylformamide, and chlorine.30 cl, 10 ex
ethod for isolating caprolactam from caprolactam- and its oligomer-containing polymers // 2640657
FIELD: chemistry.SUBSTANCE: method for isolating caprolactam from caprolactam- and its oligomer-containing polymers, consists in the process of removing caprolactam and drying the polyamide-6 granulate using nitrogen as a caprolactam transfer agent in a laminar mode. Polyamide-6 is treated with a stream of nitrogen heated to a temperature of 140-160°C, with a feed rate of 14-40 l/h.EFFECT: elimination of the oligomer losses with simultaneous improvement of the process due to the elimination of contamination of the pipelines by the crystallized oligomers.2 cl, 1 tbl, 12 ex
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
Catalysts for producing mould polyamide, method of their production and their application // 2640589
FIELD: chemistry.SUBSTANCE: invention relates to a catalyst for producing mould polyamides comprising a) at least, one lactamate, b) at least, one salt of a heteroatom-substituted organic acid selected from the group consisting of aminocaproates and/or amino-laurates of alkali and/or alkaline-earth metals and, if necessary c) lactam or a mixture of several lactams. The invention also relates to the method of producing the claimed catalyst, mould polyamide and the method of its production.EFFECT: improving the quality of mould polyamides.9 cl, 1 tbl, 1 ex
Pyridine derivative // 2640588
FIELD: pharmacology.SUBSTANCE: invention relates to a pyridine derivative of formula (I) , a prodrug thereof, wherein A is a single bond or an oxygen atom; R1 represents a nitrogen atom or CH; one of X1-X5 is a nitrogen atom, and the remaining four are CR2; R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a nitro group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which optionally can form a ring, a formyl group, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, a phenyl group, a cyclohexyl group and a halogen atom), an alkylthio group having 1 to 6 carbon atoms, a phenyl a group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom) or a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, and a halogen atom), provided that when two CR2 are located side by side, two R2 substituents can be optionally combined with cycle formation; R3 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which can optionally form a ring, an imidazole ring, a pyrazole ring, a pyrrolidine ring, a piperidine ring, a morpholine ring and a piperazine ring (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms and alkylsulfonyl group containing from 1 to 6 carbon atoms), an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group and a halogen atom), an alkylcarbonyl group having 2-7 carbon atoms, an alkylthio group having 1-6 carbon atoms, an alkylsulfinyl group having 1-6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, a phenyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a pyridyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a carboxyl group, or -CO2 R5; R4 represents a carboxyl group, a tetrazolyl group, -CONHSO2R5, -CO2R5 or any of the following substituents: , provided that when R3 represents an alkyl group having 1 to 6 carbon atoms substituted by a hydroxyl group, and when R4 represents a carboxyl group, then R3 and R4 can optionally be combined to form a lactone cycle; R5 in R3 and R4 each independently represents an alkyl group having 1 to 6 carbon atoms; Z is any of the following substituents, designated as Z1-Z7 (their meanings are defined in claim 1) that can be used to treat or prevent diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.EFFECT: compound application efficiency increase.23 cl, 55 tbl, 303 ex
 
2551299.
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