Fluorated 4-furfuryl-3,4-dihydro-2h-benzo[1,4]thiazine-1,1-dioxides with high arrythmic activity

FIELD: pharmacology.

SUBSTANCE: invention relates to new fluorinated 4-furyl-3,4-dihydro-2H-benzo[1,4]thiazine-1,1-dioxides of general formula .

EFFECT: new compounds of formula 1 are obtained, which have high antiarrhythmic activity.

1 tbl, 5 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula:

I

where (a) X is N or CR8; (b) R1 is H, F, Cl, Br; (c) R2 is H; (d) R3 is H, F, Cl, Br; (e) R4 is H, F, Cl, Br, I, CN, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C6-aryl, SR9, where each of said R4, which is substituted, contains one or more substitutes selected from F, Cl, Br; (f) R5 is H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, C(=X1)R9, C(=X1)OR9, C1-C6alkylC6-aryl (where the aryl can be substituted or unsubstituted), R9X2C(=X1)R9, R9X2R9, C(=O)(C1-C6alkyl)S(O)n(C1-C6alkyl), C(=O)(C1-C6alkyl)C(=O)O(C1-C6alkyl), (C2-C6alkenyl)C(=O)O(C1-C6alkyl), SR9, R9S(O)nR9; where each of said R5, which is substituted, contains one substitute selected from F, Cl, Br, C3-C10cycloalkyl, OR9, optionally, R5 and R7 can be bonded to form a C3 cyclic system; (g) R6 is O, S, NR9; (h) R7 is substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C6-aryl, substituted or unsubstituted C1-C20heterocyclyl, selected from thiazole, oxazole, isothiazole, thiophene, pyrroidine, furan, tetrahydrothiophene, pyridazine, piperdine, pyrazole, OR9, OR9S(O)nR9, C(=X1)R9, R9C(=X1)OR9, N(R9)2, N(R9)(R9S(O)nR9), SR9, R9S(O)nR9, C1-C6alkylC1-C20heterocyclyl (where the heterocyclyl is selected from triazole and pyrazole), C1-C6alkylS(=N-CN)(C1-C6alkyl), C1-C6alkylS(O)(=N-CN)(C1-C6alkyl), C1-C6alkylNH(C(=O)OC1-C6alkyl), C1-C6 alkylC(=O)OC1-C6alkyl, C1-C6alkyl(C6-aryl)NH(C(=O)OC1-C6alkyl), C1-C6alkyl(S-C1-C6alkyl)NH(C(=O)OC1-C6alkyl), C1-C6alkyl(S-C1-C6alkyl-C6-aryl)NH(C(=O)OC1-C6alkyl), C1-C6 alkyl(NHC(=O)OC1-C6alkylC6-aryl)NH(C(=O)OC1-C6alkyl), C1-C6alkyl(OC1-C6alkylC6-C20aryl)NH(C(=O)OC1-C6alkyl), C1-C6alkylNH(C1-C6alkyl)(C(=O)OC1-C6alkyl), C1-C6alkylNH(C1-C6alkyl), C1-C6alkylN(C1-C6 alkyl)(S(O)nC1-C6alkyl), C1-C6alkylN(C1-C6alkyl)(S(O)nC1-C6alkenylC6-aryl), C1-C6alkylN(C1-C6alkyl)(C(=O)C1-C20heterocyclyl) (where the heterocyclyl is selected from pyrazole or thiophene), C1-C6alkylN(C1-C6alkyl)(C(=O)OC1-C6alkylC6-aryl), NH(C1-C6alkylS(O)nC1-C6alkyl), where each of said R7, which is substituted, contains one or more substitutes selected from F, Cl, Br, C1-C6 alkyl, C3-C10 cycloalkyl, C(=X1)R9, C(=X1)OR9, =X2, S(=X2)nR9; (i) R8 is H, F, Cl, Br, I, CN, unsubstituted C1-C6alkoxy, C(=X)OR9, S(O)nR9; (j) R9 (each independently) is H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C2-C6alkenyloxy, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C6-aryl, where each of said R9, which is substituted, contains one or more substitutes selected from F, Cl, Br, C1-C6alkyl, OC1-C6 alkyl, C6-aryl; (k) n equals 0, 1 or 2; (l) X1 is (each independently) O; (m) X2 is (each independently) O. The invention also relates to versions of the compound of formula (I). Compounds of formula (I) are intended for pest control and seed treatment.

EFFECT: thiazole derivatives for pest control.

12 cl, 2 tbl, 83 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a sodium salt of formula I compound in the solid amorphous form. The sodium salt of formula (I) compound is obtained by (a) the preparation of a mixture of the formula I compound in a non-aqueous solvent and a water solution of sodium hydroxide; and (b) drying by spraying of the mixture (a) in a spray-drying device. The stage (a) includes mixing the sodium hydroxide solution with the said solvent and further addition of the formula I compound. The solvent is represented by halogen-containing hydrocarbon. The invention also relates to a pharmaceutical composition, possessing HCV inhibiting properties, including sodium salt of the formula I compound in the amorphous form, and a pharmaceutically acceptable carrier.

EFFECT: sodium salt of the formula (I) compound for application as HCV inhibitor and medication for HCV treatment.

10 cl, 7 dwg, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining 3-hetaryl-1,5,3-dithiazocinanes, which consists in the interaction of N1,N1,N7,N7-tetramethyl -2,6-dithiaheptane -1,7-diamine with hetarylamine in the presence of a catalyst CuCl2 in a molar ratio N1,N1,N7,N7-tetramethyl -2,6-dithiaheptane -1,7-diamine:hetarylamine:CuCl2=10:10:(0.3-0.7) at a temperature of 55-65C and atmospheric pressure in chloroform as a solvent for 60-90 min. The output of respective 3-hetaryl-1,5,3-dithiazocinanes constitutes 68-90%. .

EFFECT: method improvement.

1 tbl, 16 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining 3-pyridinyl-1,5,3-dithiazocinanes of formula I . The essence of the method consists in the interaction of N,N-bis(methoxymethyl)-N-pyridineamine with 1,3-propanedithiol in the presence of a catalyst CuCl2 in a molar ratio N,N-bis(methoxymethyl)-N-pyridineamine: 1,3-propanedithiol: CuCl2=10:10:(0.3-0.7) at room temperature and atmospheric pressure in chloroform for 120-150 minutes. The output of respective 3-pyridinyl-1,5,3-dithiazocinanes constitutes 54-77%.

EFFECT: method improvement.

1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a crystalline form of a solid-state compound of formula

having an X-ray powder diffraction characterised by peaks as follows: (i) 8.50.2, 10.70.2, 13.70.2, 14.80.2 and 17.10.2 at a diffraction angle, two theta (form I); (ii) 4.60.2, 6.50.2, 10.20.2, 12.90.2 and 14.40.2 at a diffraction angle, two theta (form II); (iii) 6.50.2, 9.80.2 and 17.80.2 at a diffraction angle, two theta (form III); (iv) 5.60.2, 9.60.2, 11.80.2, 15.90.2 and 17.10.2 at a diffraction angle, two theta (form IV); (v) 9.60.2 and 19.00.2 at a diffraction angle, two theta (form V); (vi) 4.40.2, 6.50.2, 9.90.2, 10.50.2 and 12.90.2 at a diffraction angle, two theta (form VI). The invention also refers to a mixture of two or more crystalline forms I, II, III, IV, V and VI of the compound of formula (I) for treating HCV and to a mixture of two or more crystalline forms I, II, III, IV, V and VI of the compound of formula (I) and an amorphic form of the compound of formula (I) for treating HCV. The crystalline form (I) is prepared by: a) boiling the mixture of polymorphs I and II in 1-butanol or 2-propanol in a back flow condenser to produce a transparent solution; and b) spontaneous cooling of the solution to a room temperature while stirring, and then filtering and recovering crystalline form I. The method for preparing crystalline form II involves: a) preparing a suspension of the amorphic form of the compound of formula (I) in isopropanol; b) mixing the suspension at a room temperature; and c) fusing the suspension with fusing crystals of form II or form I while stirring, then filtering and drying at 60C. There are also presented versions of the method for preparing the crystalline form (I) and (II) and forms (III), (IV) (V) and (VI). Besides, the invention refers to a pharmaceutical composition for treating HCV containing the crystalline form of the compound of formula (I), the mixture of two or more crystalline forms of the compound of formula (I) and a pharmaceutically acceptable excipient.

EFFECT: crystalline form of the hepatitis C virus (HCV) serine protease inhibitor.

19 cl, 15 dwg, 6 tbl, 12 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining 3-pyridinyl-1,5,3-dithiazepinanes of formula I. The essence of the method consists in the interaction of respective N,N-bis(methoxymethyl)-N-pyridinamine with 1,2-ethanedithiol in the presence of the catalyst CuCl2 in a molar ratio N-bis(methoxymethyl)-N-pyridinamine: 1,2-ethanedithiol: CuCl2=10:10:(0,3-0,7) at room temperature and atmospheric pressure in chloroform for 120-150 minutes. The output of respective 3-pyridinyl-1,5,3-dithiazepinanes of general formula (1) constitutes 68-89% (a); (b); (c); (d).

EFFECT: improvement of the method.

1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, in particular to method of obtaining 3-hetaryl-1,5,3-dithiazepinanes of general formula (1) , where ; ; ; ; ; ; ; ; , consisting in the following: N1,N1,N6,N6-tetramethyl-2,5-dithiahexane-1,6-diamine is subjected to interaction with hetarylamine [2-pyridinamine, 3-pyridinamine, 5-bromo-2-pyridinamine, 5-methyl-2-pyridinamine, 4-pyridinylmethylamine, 5-nitro-1,3-thiazol-2-amine, 6-nitro-1,3-benzothiazol-2-amine, 2-91h-indol-3-yl)-1-ethanamone, 5-methyl-1H-pyrazol-3-amine] in presence of catalyst CuCl2 in molar ratio N1,N1,N6,N6-tetramethyl-2,5-dithiahexane-1,6-diamine:hetarylamine: CuCl2=10:10:(0.3-0.7) at temperature 55-65C and atmospheric pressure in chloroform as solvent for 50-80 minutes.

EFFECT: elaborated is method of obtaining 3-hetaryl-1,5,3-dithiazepinanes, which can be applied as biologically active substances.

1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound presented by formula

,

wherein A1 means benzene or heterocycle specified in a group consisting of pyridine, pyrazine, imidazole, thiazole, pyrimidine, thiophen, pyridazine, benzoxazine and oxobenzoxazine; A2 means benzene, if needed substituted by fluorine, or thiophen; B1 means hydrogen, lower alkyl, if needed substituted by piperazinyl or morpholino, halogen-substituted lower alkyl, lower alkoxy substituted by carbamoyl, acylamino, carbamoyl or lower alkylcarbonyloxy (provided A1 means thiazole, B1 does not mean acylamino); B2 means hydrogen or a functional group containing at least one nitrogen atom specified in a group consisting of acylamino, pyrrolidinyl, morpholino, piperidinyl, if needed substituted by acyl, piperazinyl, if needed substituted by lower alkyl or acyl, pyrazolyl, diazabicyclo[2.2.1]heptyl, if needed substituted by acyl, and di-(lower alkyl)amino, if needed substituted by amino or acylamino (provided A1 means thiazole, B2 does not mean acylamino); Y means a group presented by formula

,

wherein J means ethylene or lower alkynylene; L means a bond; M means a bond; X means -(CH2)m-, -(CH2)m-O- or -(CH2)m-NR2- (wherein m is an integer of 0 to 3, and R2 means hydrogen); D means -NR3-, wherein R3 means hydrogen; and E means amino, or its pharmaceutically acceptable salt. The compounds of formula (I) are used for preparing a pharmaceutical agent or a pharmaceutical composition for treating or preventing the VAP-1 related diseases.

EFFECT: benzene or thiophen derivative as a VAP-1 inhibitor.

13 cl, 25 tbl, 125 ex

Organic compounds // 2518462

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

and

,

where X represents S or O, one of X1 and X2 represents CR3' and second represents N or independently CR3', n represents integer number 1, 2 or 3; R1 represents C1-6 halogenalkyl, R2 is selected from halogen and C1-C6-halogenalkyl; R3' represents H, C1-C6-alkyl, halogen, cyanogroup, or phenyl, non-substituted or substituted with halogen, C1-C6-alcoxygroup, C1-C6-halogenalcoxygroup, C1-C6-halogenalkyl group; Z represents halogen, Q radical or group -C(O)-NR5R6; R5 represents H or C1-C4-alkyl, R6 represents H; Q', C1-C6-alkyl, non-substituted or substituted with halogen, cyanogroup, C1-C4-alcoxygroup, C1-C4-alkoxycarbonyl, C2-C4-alkanoyl, aminocarbonyl, N-mono- or N,N-di-C1-C2-alkylaminocarbonyl, C1-C4-alkylthiogroup, group -C(O)NHR7 or radical Q"; or C3-C6-cycloalkyl, substituted with group -C(O)NHR7; or C2-C4-alkinyl; Q, Q' and Q" are such as given in the invention formula; R7 represents C1-C6-alkyl, which is non-substituted or substituted with halogen, cyanogroup, pyridyl; or represents C2-C4-alkinyl. Invention also relates to composition for fighting ectoparasites, containing compound of formula (Ia) or (Ib), and to application of compounds of formula (Ia) or (Ib) for composition production.

EFFECT: compounds of formula (Ia) and (Ib), possessing activity against ectoparasites.

11 cl, 4 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: described are heterobicyclic derivatives of formula (I)

, in which V denotes -C(R7)-; W denotes a single bond or -C(R8R9)-; X denotes O, S, SO, SO2 or N(R10); Y denotes -C(R11R12)-, -C(R11R12)C(R13R14)C(R11R12)C(R13R14)C(R15R16)-, -C(R11R12)C(R13R14)C(R15R16)C(R17R18)- or- C(R11)=C(R12)-; R1, R2, R3, R4 and R5 independently denote hydrogen, halogen, (lower)alkyl, fluoro(lower)alkyl, (lower)alkoxy group, fluoro(lower)alkoxy group, NH2-C(O); R6 denotes a phenyl, pyridyl, pyrazolyl or thiazolyl group, where the group is optionally substituted with 1-4 substitutes selected from a group consisting of halogen, cyano group, (lower)alkyl, (lower)alkoxy group, COOH, 1H-tetrazol-5-yl, 5-oxo-4H-[1,2,4]oxadiazol-3-yl, where (lower)alkyl is optionally substituted with COOH. A pharmaceutical composition is also described.

EFFECT: said compounds inhibit L-CPT1 and can be used as medicinal agents.

27 cl, 120 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there is described a compound of formula [I]: where A cycle represents a benzene cycle optionally having substitute(s) different from R1, R1 represents a group of formula RaSO2NH-, RaSO2NH-CH2- or (Rb)(Rc)NSO2-, Ra represents C1-C6 alkyl group, C3-C10cycloalkyl group, an amino group, 6-10-member monocyclic or bicyclic aryl group or 5-10-member monocyclic or bicyclic heteroaryl group containing 1-2 heteroatoms, chosen from oxygen, sulphur and nitrogen atoms, Rb and Rc are identical or different, and each represents hydrogen atom, C1-C6alkyl group or C3-C10cycloalkyl group, one of R2 and R3 represents hydrogen atom, halogen atom or C1-C6alkyl group, and the other represents hydrogen atom, C1-C6alkyl group, C1-C6alkoxycarbonyl group or phenyl group, or both are combined with each other together with the neighbouring carbon atom to form C3-C10cycloalkyl group, X represents oxygen atom, sulphur atom, or formula group of -NR4-; Y represents a group of formula -C(=O)-, -C(=S)- or CH(R5)-; Ar represents optionally substituted 6-10-member monocyclic or bicyclic aryl group or 5-10-member monocyclic or bicyclic group; Q represents a simple bond, C1-C6alkylene group or C2-C6alkenylene group, or its pharmaceutically acceptable salts There are described specific compounds of formula [I], and also intermediate compounds.

EFFECT: presented compounds exhibit affinity to mineralocorticoid receptor (MR) and are applicable for prevention or treatment of various diseases or diseased states associated with such receptor.

11 cl, 54 tbl, 410 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to substituted bicyclic heterocyclic compounds of the formula (I): their tautomeric forms, stereoisomers, polymorphous forms, pharmaceutically acceptable salts and pharmaceutically acceptable solvates wherein groups R1, R2, R3 and R4, and groups R5 and R6 when they are bound with carbon atom they represent hydrogen, halogen atom, hydroxy-group, alkyl, alkoxy-group; R5 and R6 as a single group or both can represent also an oxo-group when they are bound with carbon atom; when R5 and R6 are bound with nitrogen atom then they represent hydrogen atom, hydroxy-group or such unsubstituted groups as alkyl, alkoxy-group, aralkyl. X means oxygen or sulfur atom; Ar means phenylene, naphthylene or benzofuryl. Proposed compounds can be used against obesity and hypercholesterolemia. Also, the invention describes methods for preparing compounds, pharmaceutical compositions, method for treatment and using compounds proposed.

EFFECT: valuable medicinal properties of compounds and compositions.

52 cl, 77 ex

FIELD: organic chemistry, technology of organic compounds.

SUBSTANCE: invention relates to heterocyclic o-dicarbonitriles. Invention describes heterocyclic o-dicarbonitriles of the general formula: wherein R means the following compounds: . Heterocyclic o-dicarbonitriles can be used for preparing hexazocyclanes-fluorophores as a donor-fragment used for preparing hexazocyclanes-bifluorophores and hexazocyclanes-trifluorophores. Invention provides preparing new compounds possessing valuable properties.

EFFECT: valuable properties of compounds.

2 tbl, 10 ex

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of aryl carboxylic acids and describes a compound of the formula (I):

, wherein groups R1, R2, R3, R4 and groups R5 and R6 when they are joined to carbon atom can be similar or different and mean hydrogen, halogen atom, hydroxy-group or optionally substituted group taken among alkyl, alkoxy-group, phenyl, carboxylic acid or sulfonic acid; one or both substitutes R5 and R6 can mean oxo-group also if they are joined to carbon atom; if R5 and R are joined to nitrogen atom then they mean hydrogen atom, hydroxy-group or optionally substituted alkyl or benzyl; X means heteroatom taken among oxygen and sulfur atom or NH; Ar means optionally substituted bivalent a single or condensed aromatic or heterocyclic group wherein aromatic ring represents phenyl, naphthyl and heterocyclic group represents furan; R7 means hydrogen, halogen atom, alkoxy-group, alkyl, or it forms a bond with the adjacent group R8; R8 means hydrogen atom, hydroxy-, alkoxy-group, alkyl or optionally substituted benzyl; or R8 forms a bond in common with R7; R9 means hydrogen atom or optionally substituted group taken among alkyl, phenyl or benzyl group; R10 means hydrogen atom or optionally substituted group taken among alkyl, phenyl or benzyl group; Y means oxygen atom or NR12 wherein R12 means hydrogen atom, alkyl or benzyl; R10 and R12 can form in common five- or six-membered cyclic structure comprising carbon atoms that involves optionally one or some heteroatoms taken among oxygen, sulfur or nitrogen atoms; a binding group represented by the formula: -(CH2)n-(O)m- can be joined through nitrogen atom or through carbon atom and wherein n means a whole number from 1 to 4; m means a whole number from 0 to 1 under condition that when a binding group is joined through carbon atom then R5 either R6 represents oxo-group; Y means oxygen atom; R9 doesn't mean hydrogen atom; or its derivatives, analogs, its tautomeric forms, its stereoisomers, its polymorphic forms, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates. Also, invention describes methods for preparing compounds of the general formula (I), intermediate compounds and methods for their preparing, a pharmaceutical composition eliciting activity with respect to hPPRα, hPPRγ and inhibitory activity with respect to HMG-CoA-reductase and involving compound of the formula (I). Also, invention relates to methods for prophylaxis and treatment of different diseases caused by above said activity, a method for reducing the total cholesterol level and a method for reducing the glucose level. Invention provides preparing new compounds eliciting valuable biological properties.

EFFECT: improved preparing methods, valuable medicinal properties of compounds.

27 cl, 64 ex

The invention relates to a derivative of methotrexate, more specifically, to novel derivatives of methotrexate suitable as an Antirheumatic agent, agent, healing psoriasis, and cancerostatic agent

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to quinolines substituted by phosphorus-containing group of formula and applicable in medicine, wherein Z represents V1 and V2 are independently specified in hydrogen or halogen; one of R and R` represent phosphorus-containing substitute Q; the other one is specified in hydrogen or methoxyl; wherein the phosphorus-containing substitute Q represents A represents O; L represents C1-6alkyl; J represents NH or C3-6heterocycloalkyl and J is optionally substituted by G3; X is absent or represents -C(=O)-; X is absent or represents C1-6alkyl; each of R1 and R2 are independently specified in C1-6alkyl or C1-6alkoxy; G3 represents C1-6alkyl, R3S(=O)m-, R5C(=O)- or R3R4NC(=O)-; R3, R4 and R5 are independently specified in 3 or C1-6alkyl; m is equal to 0-2.

EFFECT: there are presented new protein kinase inhibitors effective for treating the diseases associated with abnormal protein kinase activity.

20 cl, 42 ex, 8 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new N-[2-(adamant-2-yl)aminocarbonylmethyl]-N'-(dialkylamino)alkylnitrobenzamide of general formula and their physiologically acceptable salts, preferentially hydrochlorides, which possess antiarhythmic action. In formula I, R can be hydrogen, alkyl (C1-C6) or cycloalkyl; R1 can be hydrogen or aliphatic residue (C1-C2); R2 can be alkyl (C1-C2) or saturated heterocycle together with nitrogen with one or two heteroatoms, such as morpholine, pyrrolidine, piperidine; "n" can have a value of 2 or 3; a nitro group in benzamide can be found in any position of the cycle.

EFFECT: invention refers to a method for preparing the compounds of general formula I, specific compounds of formula I, as well as to using them antiarhythmic, particularly antifibrillation agents.

8 cl, 11 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: presented is using 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine hydrobromide as an agent changing the total spectrum power of the heart rate variability and possessing anti-bradycardia properties. The effect of the invention can be used if it is necessary to increase the heart rate if it has dipped down, which can constitute an immediate risk of loss of the individual's life caused by a high risk of cardiac arrest emergency.

EFFECT: reducing the power of a high-frequency component of the cardiac rhythm spectrum by several times, reducing a RR interval variability factor by reducing the regulatory effect of the parasympathetic nervous system on the cardiac rhythm.

8 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to pharmaceutical compositions possessing prolonged antiarrhythmic actions and applicable to correct the cardiac arrhythmia, including that of the ischemic origin. What is presented is a pharmaceutical composition with the prolonged antiarrhythmic acitivity containing bis[2-(diethylamino)]-N-(2,6-dimethylphenyl)acetamide L-glutaminate, L-glutamic acid, 2-aminoethane sulpho-acid and excipients.

EFFECT: prolonged antiarrhythmic action and stability of the dosage form (tablets, capsules for oral application or solution for injections).

3 cl, 4 tbl

Up!