Active subctances, pharmaceutical composition, method of their production and application

FIELD: chemistry.

SUBSTANCE: invention relates to application of the substituted esters of 1,2,3,7-tetrahydro-pyrrolo [3,2-f][1,3]benzoxazine-5-carboxylic acid of general formula 1 or their racemoids, or their pharmaceutically acceptable and/or hydrates as substances of pharmaceutical compositions having anti-influenza virus activity: , where: R1 and R4 independently represent amines substitute selected from hydrogen, optionally substituted by liner or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted aryl, and probably, annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring, with one or several heteroatoms selected from nitrogen, oxygen or sulphur or their oxides; R2 represents alkyl substitute selected from hydrogen, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl; R5 represents substitute of the cyclic system selected from hydrogen, optionally substituted linear or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms optionally substituted aryl or optionally substituted and optionally substituted annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides; R6 represents substitute of cyclic system selected from hydrogen, halogen atom, cyano group, optionally substituted aryl or optionally substituted annelated heterocycle, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides.

EFFECT: production of the pharmaceutical compositions having anti-influenza virus activity.

12 cl, 2 dwg, 2 tbl, 5 ex

 

The text descriptions are given in facsimile form.

1. Use as substances of pharmaceutical compositions having activity against influenza viruses, substituted esters 1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1 or their racemates, or optical isomers, or their pharmaceutically acceptable salts and/or hydrates

where R1and R4independently from each other represent a Deputy amino group selected from hydrogen, optionally substituted linear or branched alkyl containing 3 to 12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted aryl or optionally substituted and may annulirovano heterocyclyl, which can be aromatic or non-aromatic and may contain from 3 to 10 atoms in the ring, with one or more heteroatoms selected from nitrogen, oxygen, or sulfur, or their oxides;

R2is an alkyl substituent selected from hydrogen, optionally substituted mercaptopropyl, optionally substituted amino, long is Ino substituted hydroxyl;

R3represents lower alkyl;

R5is a Deputy cyclic system selected from hydrogen, optionally substituted linear or branched alkyl containing 3 to 12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted aryl or optionally substituted and optionally annulirovano heterocyclyl, which can be aromatic or non-aromatic and may contain from 3 to 10 atoms in the ring, with one or more heteroatoms selected from nitrogen, oxygen, or sulfur, or their oxides;

R6is a Deputy cyclic system selected from hydrogen, halogen atom, ceanography, optionally substituted aryl or optionally substituted and optionally annulirovano heterocyclyl, which can be aromatic or non-aromatic and may contain from 3 to 10 atoms in the ring, with one or more heteroatoms selected from nitrogen, oxygen, or sulfur, or their oxides.

2. The use according to claim 1 ethyl esters of 9-aryl(or heterocyclyl)-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1.1 or their racemates, or optical isomers, or their pharmaceutically acceptable salts and/or hydrates

where R1, R2, R4and R5have the above meanings; Ar represents an aryl or 5-6-membered heterocyclyl comprising at least one heteroatom selected from N, O or S.

3. The use according to claim 1 ethyl esters of 9-aryl(or pyridyl)-7-methyl-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1.2 or their racemates, or optical isomers, or their pharmaceutically acceptable salts and/or hydrates

where R2, R4and R5have the above meanings; Ar1represents an aryl or pyridyl.

4. The use according to claim 3 ethyl esters of 6-aminomethyl-9-aryl(or pyridyl)-7-methyl-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1.3

where R4, R5and Ar1have the above meanings; R34and R44independently from each other represent a Deputy amino group selected from hydrogen, optionally substituted alkyl containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted phenyl or optionally substituted 5-6-membered azaheterocyclic or R34and R44together with the volume of nitrogen, with which they are linked, form a through R34and R44optionally substituted 5-7-membered azaheterocyclic may contain an additional nitrogen atom or oxygen in the loop, or guanidyl.

5. The use according to claim 4 ethyl esters of 9-aryl(or pyridyl)-6-dimethylaminomethyl-7-methyl-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1.4

where R4, R5and Ar1have the above values.

6. The use according to claim 5 ethyl esters of 9-aryl(or pyridyl)was 3.7-dimethyl-6-dimethylaminomethyl-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acids of General formula 1.5

where Ar1have the above values.

7. The use according to claim 6 ethyl ester of 3,7-dimethyl-6-dimethylaminomethyl-9-(3-pyridyl)-1,2,3,7-tetrahydro-pyrrolo[3,2-f][1,3]benzoxazine-5-carboxylic acid of the formula 1.5.1

8. Pharmaceutical composition having activity against influenza viruses containing as active substance an effective amount of at least one compound according to any one of claims 1 to 7.

9. The method of obtaining the pharmaceutical composition of claim 8 mixing an effective amount of the active substance with an inert filler and/or a solution of the holder characterized in that the active substance is used, at least one compound according to any one of claims 1 to 7.

10. The drug is in the form of tablets, capsules, or injections, placed in pharmaceutically acceptable packing for the prevention and treatment of influenza, obtained on the basis of the pharmaceutical composition of claim 8.

11. The method of prevention and treatment of influenza introduction to patient medications on item 10.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention pertains to non-peptide antagonists GnRH, with general formula 1 , where each of A1, A2 and A3 are independently chosen from A5 and A6; and A4 represents either a covalent bond, or A5; under the condition that, if A4 is a covalent bond, then one of A1-A3 represent A6, and the other two represent A5, and that, if A4 represents A5, then all of A1-A3 represent A5; A5 is chosen from C-R13 and N; A6 is chosen from N-R14, S and O; R1 is chosen from H, NHY1 and COY2, and R2 represents H; or and R1, and R2 represents methyl or together represent =O; each of R3, R4 and R5 independently represents H or low alkyl; each of R6, R7, R8, R9, R10, R11 and R12 are independently chosen from H, NH2, F, CI, Br, O-alkyl and CH2NMe2; R13 is chosen from H, F, CI, Br, NO2, NH2, OH, Me, Et, OMe and NMe2; R14 is chosen from H, methyl and ethyl; W is chosen from CH and N; X is chosen from CH2, O and NH; Y1 is chosen from CO-low alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3; Y2 is chosen from OR15, NRI6R17 and NH(CH2)cCOY3; Y3 is chosen from alkyl, OR15 and NR16R17; R15 represents H; each of R16 and R17 is independently chosen from H, low alkyl and (CH2)aR18, or together represent -(CH2)2-Z-(CH2)2-; R18 is chosen from OH, pyridyl, pyrizinyl and oxadiazolyl; Z represents NH; a represents 0-4; and b and c represent 1-3. The invention also relates to use of formula 1 a compound as a therapeutic agent and pharmaceutical composition, with antagonistic effect to GnRH receptor. Description is also given of the method of obtaining compounds with the given formula.

EFFECT: obtaining new compounds, with useful biological properties.

27 cl, 70 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of the formula (1a) or its pharmaceutically acceptable salt, esters or imides where A is a thiophenyl group containing, probably, substitution, the thiophenyl group A containing, probably, substitution with one or several groups as follows: alkyl, halo or arylalkyl, Y is O, S or NR2 where R2 is hydrogen or alkyl group containing 1 to 6 carbon atoms, and R1 is an non-ramified alkyl group containing 6 to 25 carbon atoms, ramified alkyl group containing 6 to 25 carbon atoms, aryl alkyl group where the alkyl group contains 2 to 25 carbon atoms or phenyl group containing substitution with one or several groups as follows: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16- phenyl, NR16CO-phenyl or NR16 -phenyl containing, probably, substitution where R16 is hydrogen or alkyl group containing 1 to 4 carbon atoms, the groups phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl containing, probably, substitution with one or several groups as follows: halo, alkyl, alkylhalo or phenyl group containing substitution with one or several groups or alkyl groups provided the above compound is not 5-methyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on, 6-amyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on or 6-amyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on Invention also relates to method of obtaining compounds of the formula (Ia) or (IIa), to pharmaceutical compound and application, as well as cosmetic technique.

EFFECT: obtaining of new biologically active compounds and pharmaceutical compounds based on them.

27 cl, 4 ex, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): , wherein X represents heteroatom, such as oxygen (O) or sulfur (S) atoms; X and Z mean independently of one another one or some identical or different substitutes bound any available carbon atom and they can represent hydrogen atom or halogen atom; R1 represents a substitute of the formula (II): , wherein R2 and R3 can represent simultaneously or independently of one another hydrogen atom or (C1-C4)-alkyl, or R1 can represent hydrogen, halogen atom, (C1-C7)-alkyl, -CHO, -(CH2)2COOH, -(CH2)2CO2Et, (CH2)mL wherein L means -OH or bromine atom (Br); m represents a whole number from 1 to 3; n represents a whole number from 0 to 3; Q1 and Q2 represent independently of one another oxygen atom or group of the formula: wherein substitutes y1 and y2 represent hydrogen atom, and to their pharmacologically acceptable salts. Also, invention relates to use of these compounds as intermediate substances used in synthesis of novel compounds of dibenzoazulene class, and to their using for preparing drugs.

EFFECT: valuable medicinal properties of compounds.

9 cl, 4 tbl, 13 ex

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

SUBSTANCE: invention relates to novel substituted esters of 1,2,3,7-tetrahydropyrrolo[3,2-f][1,3]benzoxazin-5-carboxylic acids of the general formula (1): or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and/or hydrates possessing the antiviral effect. In compounds of the general formula (1) each R1 and R4 represents independently of one another a substitutes of amino group chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and possibly an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R2 represents alkyl substitute chosen from hydrogen atom, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl or cycloalkyl; R5 represents a substitute of cyclic system chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and optionally an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R6 represents a substitute of cyclic system chosen from hydrogen atom, halogen atom, cyano group, optionally substituted aryl or optionally substituted and optionally annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides. Also, invention relates to methods for treatment, drugs and pharmaceutical compositions using compounds of this invention. Proposed compounds can be used as active components of drugs used in treatment of such diseases as infectious hepatitis, human immunodeficiency, atypical pneumonia and avian influenza.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods of synthesis.

22 cl, 3 tbl, 6 dwg, 7 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods for synthesis and preparing.

35 cl, 16 sch, 13 tbl, 43 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula 1 (G1 is group of general formulae 2 G1 is group of general formulae ; meanings of the rest substituents are as described in specification) or pharmaceutically acceptable salts thereof and use thereof in srug production. Said compounds are useful in treatment of male and female sexual disorders.

EFFECT: new oxytocin antagonists.

30 cl, 177 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula I and pharmaceutically acceptable salt thereof, wherein R1, R3, R4, R5, and R10 are independently H, halogen, C1-C4-alkyl, etc.; R2 is H, halogen, NO2, etc.; R6 is H, C1-C6-alkyl, C1-C6-alkoxy-substituted C1-C4-alkyl, etc.; R7 is H, C1-C4-alkyl or C2-C4-alkenyl, optionally substituted with halogen; R8 and R9 are H, R11 and R12; meanings of the rest substituents are as define in specification.

EFFECT: new compounds with value biological properties and useful as drug having activity in relates to progesterone receptor.

15 cl, 3 tbl, 80 ex

FIELD: organic chemistry.

SUBSTANCE: invention relates to new method for production of E-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones of general formula I wherein R represents H, methyl, Cl. Claimed method includes interaction of 5-aryl-2,3-dihydro-2,3-furandiones with N-phenylanthranyl acid amide in medium of inert aprotic solvent (preferably benzene) followed by isolation of target products. Process is carried out preferably at 79-80°C. Claimed compounds have fluorescent properties and are useful in labeling and copying agents, intermediates for synthesis of new heterocyclic compounds, etc.

EFFECT: new fluorescent compounds.

3 cl, 1 dwg, 3 ex

FIELD: organic chemistry, antibacterial agents.

SUBSTANCE: invention relates to an agent used against acid-resistant microorganisms containing derivative of pyridone carboxylic acid as an active component, its pharmaceutically acceptable salt or its hydrate that elicits high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms. Invention describes agent used against acid-resistant microorganisms containing compound represented by the following formula (I) its salt or its hydrate as an active component wherein R1 represents cyclic alkyl group comprising 3-6 carbon atoms that can comprise substitute(s) chosen from halogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; A1 represents incomplete structure represented by the formula (2): wherein X2 represents halogen atom, alkyl group comprising 1-6 carbon atoms or alkoxy-group comprising 1-6 carbon atoms; A1, A2 and A3 form incomplete structure of the formula: in common with carbon atoms combined with them; X1 represents halogen atom; Y represents hydrogen atom; Z represents phenylpiperazine substitute. Invention provides synthesis of pyridone carboxylic acid eliciting high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms in combination with good pharmacokinetics indices and safety.

EFFECT: valuable biological property of agent.

10 cl, 9 tbl, 10 ex

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

SUBSTANCE: invention relates to a synthetic quinolone agent that is effective as medicinal agents, veterinary preparations, drugs used in fishing industry or as antibacterial preserving agents. Invention describes compound represented by the following general formula (I): as its separate isomers or their mixture, its salt and their hydrates wherein R1 represents cyclic alkyl group comprising 3-6 carbon atoms that can comprise a substitute chosen from halogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; R4 represents hydrogen atom, amino-group, hydroxyl group; A represents nitrogen atom or part of structure as given in the invention claim; each R5 and R6 represents independently alkyl group comprising 1-6 carbon atoms or hydrogen atom; n means a whole number 1 or 2. Also, invention describes antibacterial agent and therapeutic agent based on compounds of the formula (I) used in treatment of infectious disease, a method for preparing antibacterial agent, a method for preparing a medicinal agent used in treatment of infectious disease and using compound of the formula (I) for preparing an antibacterial agent and using compound of the formula (I) for preparing a medicinal agent used in treatment of infectious disease. Invention provides novel compounds possessing useful biological properties.

EFFECT: improved preparing method of agents, valuable medicinal properties of compounds and agents.

35 cl, 2 tbl, 15 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the new derivative 4-aminomethyl-5-hydroxyindole-3-carboxylate of the general formula I: where; R indicates cyclohexyl, cycloheptyl; R1 indicates C1-C3-alkyl, -CH2-X-phenyl; X indicates NH, O, S; R2 indicates C1-C5-alkyl, R3, R4 have identical value and are selected from C1-C3-alkyl, predominantly, CH3, or R3 and R4 together with a nitrogen atom form -5-10- member heterocycle, which contains 1-2- heteroatom selected from N, O, S or their pharmaceutically acceptable salts, with the exception of 6-bromine-5-hydroxy-4-dimethylaminomethyl-2-phenylthiomethyl-1-cyclohexyl-3-ethoxycarbonylindole, 6-bromine-5-hydroxy-4-dimethylaminomethyl-2-methyl-1-cyclohexyl-3-ethoxycarbonylindole, 6-bromine-5-hydroxy-4-dimethylaminomethyl-2-(piperidinomethyl)-1-cyclohexyl-3-ethoxycarbonylindole, 6-bromine-5-hydroxy-4-dimethylaminomethyl-2-(pirrolidinemethyl)-1-cyclohexyl-3-ethoxycarbonylindole and methyl-1-cyclohexyl-4-piperidinomethyl-6-bromine-5-hydroxy-2-methyl-indole-3-carboxylate. The methods of obtaining compound I are described.

EFFECT: exhibit antiviral activity and can be used for treating influenza of the type A.

5 cl, 2 dwg, 2 tbl, 8 ex

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

SUBSTANCE: invention relates to novel substituted esters of 1,2,3,7-tetrahydropyrrolo[3,2-f][1,3]benzoxazin-5-carboxylic acids of the general formula (1): or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and/or hydrates possessing the antiviral effect. In compounds of the general formula (1) each R1 and R4 represents independently of one another a substitutes of amino group chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and possibly an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R2 represents alkyl substitute chosen from hydrogen atom, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl or cycloalkyl; R5 represents a substitute of cyclic system chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and optionally an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R6 represents a substitute of cyclic system chosen from hydrogen atom, halogen atom, cyano group, optionally substituted aryl or optionally substituted and optionally annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides. Also, invention relates to methods for treatment, drugs and pharmaceutical compositions using compounds of this invention. Proposed compounds can be used as active components of drugs used in treatment of such diseases as infectious hepatitis, human immunodeficiency, atypical pneumonia and avian influenza.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods of synthesis.

22 cl, 3 tbl, 6 dwg, 7 ex

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

SUBSTANCE: invention relates to novel substituted esters of 1H-indol-3-carboxylic acids of the general formula (1): or their racemates, or their optical isomers, or their pharmaceutical acceptable salts and/or hydrates. Compounds can be used in treatment of such diseases as infectious hepatitis, human immunodeficiency, atypical pneumonia and avian influenza. In compound of the general formula (1) R1, R41 and R42 each represents independently of one another a substitute of amino group chosen from hydrogen atom, optionally linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and possibly an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 carbon atom in ring with one or some heteroatoms chosen from nitrogen oxygen or sulfur atoms; or R41 and R42 in common with nitrogen atom to which they are bound form 5-10-membered azaheterocycle or guanidyl through R41 and R42; R2 represents an alkyl substitute chosen from hydrogen atom, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl; R5 represents a substitute of cyclic system chosen from hydrogen atom, halogen atom, cyano group, optionally substituted aryl or optionally substituted and possibly an annelated heterocycle that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms. Also, invention relates to methods for treatment, drugs and pharmaceutical compositions using compounds of this invention.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of synthesis.

22 cl, 3 tbl, 8 dwg, 6 ex

FIELD: medicine.

SUBSTANCE: method involves administering dry inhalation with essential oils in closed room. Eucalyptus and fir oils are used as essential oils. Inhalation is carried out in three stages. The first stage involves applying essential oil of eucalyptus 8 days long with 5 days long inhalation period, 3 days long pause and 3 days long inhalation period. Room saturation with applying essential oil of eucalyptus is started with 5 min a day adding 5 min every following day bringing total inhalation time to 40 min at the eighth day. Eucalyptus oil is applied at a dose of 6 drops per 15 m2. The second stage involves carrying out dry inhalation with two types of essential oils adding inhalation with fir oil. Two days combined inhalation is carried out and then 2 days is pause and 5 days of combined inhalation. Room saturation with fir oil is started with 5 min a day adding 5 min every following day bringing total inhalation time to 35 min at the seventh day. Room saturation with eucalyptus oil is started with 35 min a day subtracting 5 min every following day bringing total inhalation time to 5 min at the seventh day. Saturation with fir oil starts immediately after eucalyptus oil bringing total inhalation time to 40 min per day. Fir oil is used in the amount of 3 drops per 15 m2. The third stage involves carrying out dry inhalation with fir oil only 5 days long. Room saturation with fir oil is started with 40 min a day subtracting 5 min every following day bringing total inhalation time to 20 min at the fifth day.

EFFECT: optimum dose for treating children; improved individual tolerance.

1 dwg, 2 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a pharmaceutical composition for its using in treatment of symptoms of catarrhal diseases and influenza, or as an analgesic drug. Composition represents a single dose as an aqueous medicinal formula of the total volume less 100 ml and containing paracetamol and a masking component that attenuates or masks its bitter taste and consisting of at least two components chosen from the following groups (i)-(vi): (i) magnesium chloride, gluconate, hydroxide, carbonate or hydrocarbonate, and/or a mixture of magnesium chloride and magnesium sulfate in the molar ratio from 0.0001:1 to 0.01:1 measured as the ratio magnesium atoms : paracetamol; (ii) gingerin and/or ginger oil in the weight ratio from 1:20000 to 1:10000 with respect to paracetamol; (iii) sweetening agent of the sustained onset effect and prolonged effect chosen from taumatin, neohesperidin DC and/or glycyrrhizin taken in the weight ratio from 1:20000 to 1:100 with respect to paracetamol; (iv) soluble starch taken in the weight ratio from 1:10 to 1:1 with respect to paracetamol; (v) sucrose ester having value of hydrophilic-lipophilic balance (HLB) above 10 and taken in the weight ratio from 1:10 to 2:1 with respect to paracetamol, and (vi) glycine taken in the molar ratio from 1:4 to 2:1 with respect to paracetamol. Proposed composition provides effective taste masking or bitterness of paracetamol being especially in liquid preparations containing less 100 ml of water, and in using the combination of different masking agents also.

EFFECT: improved and valuable properties of composition.

10 cl, 3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying a preparation for preventing and treating influenza that contains methyl-1-adamantyl-methylamine hydrochloride, 2-ethylthiobenzimidazole hydrobromide and a pharmaceutically acceptable filler; moreover, it is of high curative effect and, also, increases protective body functions, endurance and recovery period by not deepening pathogenetic mechanisms caused by influenza virus at the following ratio of ingredients, weight%: methyl-1-adamantyl-methylamine hydrochloride 5-15; 2-ethylthiobenzimidazole hydrobromide 15-50; a filler- the rest.

EFFECT: higher efficiency of prophylaxis and therapy.

1 cl, 5 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: the suggested compound being 3,6-dioxocyclohexa-1,4-dien-1,2,4,5-sodium tetra-sulfonate is of antihypoxic and cytoprotector action. Moreover, the composition has been suggested being of anti-grippe action. The composition declared includes remantadin and 3,6-dioxocyclohexa-1,4-dien-1,2,4,5- sodium tetrasulfonate.

EFFECT: the compound mentioned enables to decrease remantadin toxicity during its usage at high dosage during treating the grippe infection.

4 cl, 6 dwg

FIELD: medicine, virology, pharmacy.

SUBSTANCE: invention relates to using derivatives of dithiocarbamate of the formula: R1R2NCS2H and oxidized forms of these compounds, in particular, their dimmers and their pharmaceutically compatible salts for preparing an agent used in treatment or prophylaxis of infection caused by RNA-containing viruses that damage respiratory tract and inducing disease. Also, invention relates to a disinfecting agent containing dithiocarbamate compound and a method for disinfection of surfaces, media and cell cultures.

EFFECT: valuable medicinal properties of compounds.

19 cl, 14 dwg, 14 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a cycloferon-containing medicinal agent used in prophylaxis and treatment of influenza and acute respiratory diseases, herpetic infection, chronic viral hepatitis B and C and prophylaxis of oncological diseases. Agent comprises a physiological solution in the following ratio of components: 10-29 - 10-2 mg of cycloferon in 1 ml of physiological solution. Also, invention relates to a method for preparing this medicinal agent. Proposed medicinal agent enhances antiviral and antitumor activity of natural killers by 1.8-fold, not less.

EFFECT: improved preparing and using method, valuable medicinal properties of agent.

7 cl, 1 dwg, 19 ex

FIELD: biotechnology.

SUBSTANCE: claimed strain is obtained by hybridization of epidemic virus with cold adapted and temperature sensitive virus, which represents attenuation donor and is harmless for adults, and infants of 3-14 years old. Said virus makes it possible to obtain reassortant vaccine strains from new epidemic viruses. Strain is effectively cultivated in germinative hen embryos at 32°C, and has temperature sensitivity and cold adaptation. Reassortant has two genes derived from epidemic virus encoding surface proteins (hemagglutinin and neuroamidinase) and six genes derived from attenuation donor encoding non-glycosilated proteins. Strain has no reactogenicity in relation to adults and infants of 3-14 years old at intranasal application.

EFFECT: strain for living influenza intranasal vaccine with good biological properties and reactogenicity.

3 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the new pyrazole derivatives of formula (IIa) or their pharmaceutically acceptable salts, where: Rx and Ry banded with intervening atoms while deriving benzol or cyclohexylene rings, optionally substituted by R3; R1 represents T-(ring D); ring D represents phenyl, optionally substituted by 1-2 groups R5, or naphtyl or imidazolyl or benzymidazolyl, optionally substituted by C1-C6alkyl group; T represents the linking; R2 represents hydrogen, C1-C6alkyl or C3-C6cycloalkyl; R2' represents hydrogen, or R2 and R2' is banded with their intervening atoms while deriving phenyl ring; R3 is selected from C1-C6alkyl, hydrogen, halogen, -OH, -NH2, -NHOH, -NO2, C1-C6alkoxy, optionally substituted -N(R4)2; each R4 independently selected from C1-C6alkyl, -CO2C1-C6alkyl or two R4 at the same nitrogen atom joined with nitrogen atom while deriving morpholine ring; each R5 represents one or two substitutes, independently selected from C1-C6alkyl, halogen, OH, -NH2, -CF3, C1-C6alkoxy, -COOH, -CO2C1-C6alkyl, -NHCO-C1-C6aliphatic group, NHCO(C1-C6alkyl)N(R4)2, -CONHC1-C6alkyl, -CONH(C1-C6alkyl)N(R4)2, and -NHSO2C1-C6alkyl. The compounds are useful as inhibitors of protein kinase, in particular as inhibitors Aurora-2 and GSK-3 for the treatment of cancer, diabetes and Alzheimer's disease. The subjects matter is also pharmaceutical composition on basis of their compounds and methods of the treatment of diseases mediated by the protein kinase.

EFFECT: production of new pyrazole derivatives - inhibitors of protein kinase.

25 cl, 12 tbl, 292 ex

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