Stimulator of plant growth and fungicide

 

(57) Abstract:

Usage: in agriculture, in particular as a fungicide and growth promoting substances. The inventive product is N-( 2-furfuryl)-1,3-oxazolidin and his 2-phenylpropane. The compounds were tested at a concentration of 1-10mg/l seed treatment beet it oats. Fungicidal properties tested for sulfate-reducing bacteria (Desulfovibrio desulfuricaus) and fungi (Penicillium chrisogenium) at a concentration of 150-2000 mg/l table 4.

The invention relates to agriculture and can be used in plant breeding to accelerate growth and increase crop yields.

Known compounds of similar structure:

N-glycidyl-1,3-oxazolidin and its derivatives

ONCH2-CHH2where R is H; C1-C4-Alk, Bz panaftel or menaphthyl used as additives for improving the adhesion properties of polymers, and as promoters of vulcanization of polymers based on isocyanates and polymers containing anhydrite fragments [1]

Also known connection R - where R1-C8-alkyl, phenyl or phenoxy1-C5-alkyl, C2-C5alkenyl,3-C5-cycloalkyl, benzylic or cyano, Y is hydrogen or chlorine [2]

These compounds possess herbicide activity.

Known compound 3-(3,5-dichlorophenyl)-5,5-dimethyloxazolidine-2,4-(DIH - lanolin)-fungicide to combat Munstereifel mushrooms. Rate it 2.5 kg/ha [3] the Disadvantage of this fungicide is a narrow spectrum of action.

The aim of the invention is to increase plant growth and fungicidal action.

This goal is achieved by the use of N-(2'-furfuryl)-2-R-1,3-oxazolidine General formula

OCHNO where R is H, C6H5as a fungicide and poststimulatory. These compounds are known and used to produce polymeric materials [4]

P R I m e R 1 Seeds beetroot for 8 h were soaked in aqueous solutions of preparations in a concentration of 10 mg/l Treated seeds were sown on vegetation beds. As a growth-stimulating indicators took into account the germination, growth energy and biomass tuber and haulm 45 days after sowing. The results are given in table.1.

P R I m m e R 2. Seed oats for 8 h were soaked in aqueous solutions of preparations in a concentration of 1 mg/l and then were sown in vessels with a diameter of 25 cm, Repeated 6 times. The results of the structure to sulfate-reducing bacteria (SRB) Desulfovibrio desulfuricaus anaerobic corrosionand microorganisms (strain WCMW-1388). The drugs were tested at a concentration of 150-1000 mg/l Solutions were decanted into vials of 20 ml and was inoculable two-day culture of Desulfovibrio desulfuricaus. Then the drugs within 24 h was thermostatically at 30aboutC. Upon expiration of this period was carried out transfer 2.5 ml inoculated solution in the vial containing 9 ml of culture medium of Postgate C. Repeated 4 times. The vials were thermostatically at 30aboutC for 15 days. About the effectiveness was judged by the presence or absence of black amorphous precipitate of iron sulfide. The data are given in table.3. These connections provide suppressing activity of bacteria at a concentration of 200 and 350 mg/l, whereas the prototype that operates at a concentration of 500 mg/L.

P R I m e R 4. The fungicidal activity of the compounds was determined on the livelihoods of fungi Penicillium Chrisogenium. The working concentrations of 1000-2000 mg/L. the Solution was poured into 20 ml vials and inoculable 1 ml of activated culture of Penicillium Chrisogenium. Then the vials thermostatically during the day when 30aboutC. Then produced reseeding vials with a nutrient medium of čapek and thermostatically them within 15 days at 70aboutC. the Results are given in table.4. Complete inhibition of isnide the opportunity to say, that the claimed compounds have fungicidal and astragalina activities. High activity in the claimed substances in relation to safety, making them promising in terms of practical use.

The use of N-(2-furfuryl)-1,3-oxazolidine and its derivative of General formula

< / BR>
where R is hydrogen or phenyl,

as a stimulator of plant growth and fungicide.

 

Same patents:

- aminoacyl)-5,10-dihydro-11h-dibenzo[b, e] [1,4]- diazepin-11-ons or their salts, possess antiarrhythmic activity" target="_blank">

The invention relates to the field of chemistry, particularly to the new series of compounds - 5-(-aminoacyl)-5,10-dihydro-11N - dibenzo [b,e]-[1,4]-diazepin-11-Onam General formula

where R1is a hydrogen atom or chlorine;

R2is a hydrogen atom or a C1-C2-alkyl;

R3- C1-C2-alkyl or cyclohexyl, or R2and R3together with the nitrogen atom can be morpholinyl or N-methylpiperazine balance; provided that, if R2is a hydrogen atom, R3can be1-C3-alkyl or cyclohexyl,

n=3-6;

m = 0-1; X=Cl or Br

The invention relates to new biologically active chemical compounds, namely, to derive a cyclic amide of the formula I

R1-(CH2)n-Z,

where R1group cyclic amide, such as 2H-3,4-dihydro-1,3-benzoxazin-2-she, 2H-3,4-dihydro-1,3-benzoxazin-2,4-dione, and 1,2,3,4-tetrahydroquinazoline-2,4-dione, and 1,2,3,4-tetrahydroquinazolin-2-it, 1,2,3,4-tetrahydropyrido(3,2-d)-pyrimidine-2,4 - dione, and 1,2,3,4-tetrahydropyrido(3,2-d)pyrimidine-2-it, 1,2,3,4-tetrahydropyrimidine-2,4-dione, pyrrolidin-2-it, 1,2,3,4 - tetrahydropyridine-2-it, 5H-6,7,8,9-tetrahydropyrido(3,2-b)azepin-6-she N-5,6,7,8-tetrahydropyrido(2,3-b)azepin - 8-she, 2H-3,4-dihydropyrido(2,3-e)-1, 3-oxazin-2-thione or 2-she pyrrolidine (3,4-b)-pyrazin-5-she 1H-2,3,4,5-tetrahydrothieno(2,3-b)indol-2-it, 8H-4,5,6,7-tetrahydrothieno(2,3-b)thiophene-7-she 4H-pyrazolo(5,4-f)benzazepin-9-it, isoindoline-1,3-dione, benzoxazolyl-2-it, unsubstituted or substituted lower alkyl, lower alkoxy, halogen, the nitro-group, carboxy, benzoyl or benzyl, n is zero or an integer from 1 to 6, Z is a group of formula (A) or (B):

N-(CH2)mR2(A) or -(CH2)p, dioxolane, furan, tetrahydrofuran, methylfuran or thiophene, m is an integer from 1 to 3; R3is lower alkyl; R4is phenyl or a radical of dioxolane, furan or thiophene, p = 1, provided that when R1radical 1,2,3,4-tetrahydrobenzo-2-or 1,2,3,4-tetrahydroquinazoline-2,4-dione, R2and R4are not phenyl or substituted by a halogen phenyl, or their pharmacologically acceptable salts with antiacetylcholinesterase activity

FIELD: chemistry.

SUBSTANCE: proposed hydrogen sulphide and/or low-molecular mercaptan remover is in form of amino esters with general formula: (R-)nN(-CH2-O-R')m, where R is alkyl, isoalkyl C1-C14 or cyclohexyl, or benzyl, or a bivalent group with formula - CH2-O-CH2-CH2-, bonded to a nitrogen atom of an amino ester, with formation of five-member heterocyclic ring; R' - alkyl, isoalkyl or alkenyl, preferably C1-C4; n=1 or 2, m=3-n. The invention also pertains to the method of purifying oil, water-oil emulsions, oil products, hydrocarbon gases, stratal water and process liquids from hydrogen sulphide and/or low-molecular mercaptans by treating the starting material using the above described remover. The proposed remover and a composition based on it have higher reaction capacity compared to hydrogen sulphide, light mercaptans and provides for their effective neutralisation in aqueous and non-aqueous media at normal and high temperatures (10-90°C and above). The proposed remover also has bactericidal activity towards sulphate reducing bacteria and anti-corrosion activity in hydrogen sulphide-containing media, and can be used as a bactericide-inhibitor of hydrogen sulphide corrosion in oil-field media.

EFFECT: improved properties of the remover.

4 cl, 9 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method for synthesis of N-nitro-5-azido-methyloxazolidine-1,3 which can be used as an energetic plasticiser for polymers. The starting compounds used are potassium sulphamate and epichlorohydrin. The reaction for bonding potassium sulphamate to epichlorohydrin takes place at 50…53°C and holding time of 50…55 hours with threefold excess of potassium sulphamate. Without extraction, the formed N-(3-chloro-2-hydroxypropyl)-potassium sulphamate is condensed in form of a water-alcohol solution with formaldehyde and the water-alcohol solution of N-(5-chloro-methyloxazolidine1,3)-potassium sulphamate obtained after evaporation is suspended in acetic anhydride without extraction from the reactor and nitrated with nitric acid at 10…25°C. The formed N-nitro-5-chloromethyl-oxazolidine-1,3 is extracted with organochlorine solvents, purified by treating with aqueous sodium hydroxide solution at 70…75°C and undergoes azidation with sodium azide in dimethyl formamide medium in the presence of activated carbon at 100°C.

EFFECT: improved method.

1 cl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to chemistry and the technology of producing heterocyclic compounds of the oxazolidine family, specifically N-nitro-5-azidomethyloxazolidine-1,3 which is extensively studied under the name MANO-5 as an energetic polymer plasticiser. The method of producing N-nitro-5-azidomethyloxazolidine-1,3 is realised via successive reaction of a sulphamate with epichlorohydrin and formaldehyde, followed by nitration in an acetic anhydride medium and azidation in a solvent medium. The sulphamate used is triethylammonium sulphamate and the formaldehyde source used is a mixture of paraformaldehyde and acetic acid. Azidation is carried out in the presence of a phase-transfer catalysts in an aqueous medium. Triethylammonium sulphamate and epichlorohydrin react in equimolar ratios without using a solvent. The phase-transfer catalyst used is tretralkylammonium salts, e.g., tetrabutylammonium bromide or triethylbenzylammonium chloride.

EFFECT: easy implementation of the process.

5 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing N-nitro-5-chloromethyloxazolidine-1,3, which is used as a primary product in synthesis of energetic polymer plasticisers - N-nitro-5-nitroxymethyl- and N-nitro-5-azidomethyloxazolidine-1,3, and can also be used in synthesis of biologically active substances. The method of producing N-nitro-5-chloromethyloxazolidine-1,3 is realised via successive reaction of a sulphamate with epichlorohydrin and aqueous formaldehyde solution, followed by separation of N-(5-chloromethyl-oxazolidine-1,3)-sulphamate by vacuum stripping and nitration thereof with nitric acid in the presence of acetic anhydride. The sulphamate used is a triethylammonium salt. An alcohol solution of formaldehyde is used for the cyclisation reaction. The product of cylisation of the triethylammonium salt of N-(5-chloromethyloxazolidine-1,3)-sulphamic acid is treated with an alcohol solution of potassium hydroxide; the precipitated potassium N-(5-chloromethyloxazolidine-1,3)-sulphamate is separated by filtration, dissolved in glacial acetic acid and nitrated with nitric acid in the presence of acetic anhydride at temperature 20…25°C.

EFFECT: easy implementation of the process.

1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, particularly to a method of producing 3-(2-alkynyl)-1,3-oxazolidines of formula (1) where R1=R2=H; R3=n-Pr(a), n-Bu (b), Ph (c); R1=CH3, R2=H, R3=n-Pr (d), n-Bu (e), Ph (f); R1=H, R2=CH2CH3, R3=n-Pr (g), n-Bu (h), Ph (i); R1=Ph, R2=H, R3=Ph (k), which can be used as universal precursors for fine organic synthesis and biologically active compounds. The method is carried out by reacting monoethanolamine of general formula HO(R1)CHCH(R2)NH2 (where R1=R2=H; R1=CH3, R2=H; R1=H, R2=CH2CH3; R1=Ph, R2=H) with paraform while boiling in benzene for 5 hours, followed by evacuating benzene and adding alkyl(phenyl)acetylene-1 of general formula R3-C≡CH (where R3=C3H5, C4H9, Ph) in toluene and a CuCl catalyst. The reaction mass is mixed in an argon atmosphere at 80°C and atmospheric pressure for 5-7 hours. The reaction is carried out in molar ratio HO(R1)CHCH(R2)NH2: (CH2O)n: R3-C≡CH: CuCl=2:3:1:(0.03-0.07).

EFFECT: selective production of said compounds.

1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining chiral heterocyclic ligands based on 1,2-diaminocyclohexane, which contain heterocyclic fragments: thienyl-2-, thienyl-3-, furyl-2-, 5-methylfuryl-2-, (2,2'-bithiophen)-5-yl-, 5-(4'-methylcyclohex-1'-en-1'-yl)thiophene-2-, which can be included into a structure of complexes for carrying out enantioselective reactions and asymmetric catalysis, as well as possess luminescence properties. The method is realised due to the application of available reagents, application of an acceptable molar ratio of reagents, considerable reduction of the total time of the reaction, the reduction of production costs is achieved due to the simplification of the reactor scheme and the time of the reaction carrying out.

EFFECT: simplification of the technological process.

2 ex

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds: 5 ; 10 ; which can be used for preparing a medicinal preparation for treating hyperalgesia, tolerance, withdrawal and/or subject to addictive drugs.

EFFECT: obtaining of medicinal preparation.

5 cl, 10 dwg, 9 tbl, 136 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an intermediate compound, i. e. tert.-butyl-(E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5-yl}-(4R,6S)-2,2-dimethyl[1,3]dioxane-4-yl]acetate that can be used in synthesis of compound of the formula (IV)

eliciting inhibitory effect on activity of HMG-CoA-reductase and, therefore, can be used for preparing pharmaceutical agents for treatment, for example, hypercholesterolemia, hyperproteinemia and atherosclerosis. Also, invention relates to a method for preparing indicated intermediate compound by reaction of the new parent compound - diphenyl-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-ylmethyl]phosphine oxide with tert.-butyl-2-[(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-yl]acetate in the presence of a strong base in simple ether or aromatic solvents or their mixtures at temperature in the range from -200C to -900C. Also, invention relates to a method for preparing of compound of the formula (IV) wherein R1 means hydrogen atom or pharmaceutically acceptable cation and to a method for preparing intermediate compounds of the formula (VI):

wherein each P1 and P2 represents independently (C1-C4)-alkyl or group:

and wherein P3 represents (C1-C8)-alkyl. Applying new intermediate compounds and proposed methods provide enhancing quality and yield of compounds.

EFFECT: improved preparing methods.

9 cl, 1 tbl, 8 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a new method for preparing 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxotetrahydropyran-2-yl)ethyl]-2-isopropyl-4-phenyl-1H-pyrrol-3-carboxylic acid phenylamide that involves conversion of methylcyano acetate to the end compound for 8 or less stages. Also, invention relates to value intermediate compounds that are synthesized as result of realization of above indicated stages of the claimed method. 5-(4-Fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxotetrahydropyran-2-yl)ethyl]-2-isopropyl-4-phenyl-1H-pyrrol-3-carboxylic acid phenylamide is a value intermediate compound used in synthesis of the drug atorvastatin calcium that is used as hypolipidemic and/or hypocholesterolemic agent. Proposed method allows avoiding usage of expensive chiral parent substances and to reduce the synthesis process time.

EFFECT: improved preparing method.

12 cl, 3 ex

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

SUBSTANCE: invention describes derivatives of benzodiazepine of the general formula (I)

and their pharmaceutically acceptable acid-additive salts wherein X means a ordinary bond or ethynediyl group; when X means ordinary bond then R1 means halogen atom, (lower)-alkyl, (lower)-alkylcarbonyl, (lower)-cycloalkyl, benzoyl, phenyl substituted optionally with halogen atom, hydroxyl, (lower)-alkyl, (lower)-alkoxy-group, halogen-(lower)-alkoxy-group or cyano-group; styryl, phenylethyl, naphthyl, diphenyl, benzofuranyl, or 5- or 6-membered heterocyclic ring representing thiophenyl, furanyl, pyridinyl, dihydropyridinyl, tetrahydropyridinyl which are optionally substituted; when X means ethynediyl group then R1 means hydrogen atom, (lower)-alkyl substituted optionally with oxo-group; (lower)-cycloalkyl substituted with hydroxyl; (lower)-cycloalkenyl substituted optionally with oxo-group; (lower)-alkenyl, optionally substituted phenyl; 5- or 6-membered heterocyclic ring representing thiophenyl, thiazolyl, pyridinyl, dihydropyridinyl, tetrahydropyridinyl or dihydropyranyl and substituted optionally; R3 means phenyl, pyridyl, thiophenyl or thiazolyl which are substituted optionally. These compounds can be used for treatment or prophylaxis of acute and/or chronic neurological diseases, such as psychosis, schizophrenia, Alzheimer's disease, disorder of cognitive ability and memory disorder. Also, invention describes a medicinal agent based on these compounds and a method for preparing compounds of the formula (I).

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

10 cl, 1 tbl, 173 ex

New compounds // 2258703

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compounds of the general formula (I):

wherein R1 is taken among phenyl or pyridinyl and wherein each phenyl ring R1 or pyridinyl ring R1 can be substituted additionally and independently with chlorine, fluorine, bromine and iodine atom at any position of indicated ring, and also to their pharmaceutically acceptable salts. Also, invention relates to pharmaceutical composition based on these compounds eliciting δ-agonistic activity and to a method for pain treatment. Invention provides preparing new compounds of the formula (I) used in applying for pain treatment and for manufacturing drugs for this purpose.

EFFECT: valuable medicinal properties of new compounds.

8 cl, 3 tbl, 4 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes derivatives of benzodiazepines of the general formula (I):

wherein X means ordinary bond or ethynediyl group wherein if X mean ordinary bond then R1 means halogen atom or phenyl substituted with halogen atom optionally or (C1-C7)-alkyl group; in case when X means ethynediyl group then R1 mean phenyl substituted with halogen atom optionally; R2 means halogen atom, hydroxy-group, lower alkyl, lower alkoxy-group, hydroxymethyl, hydroxyethyl, lower alkoxy-(ethoxy)n wherein n = 1-4, cyanomethoxy-group, morpholine-4-yl, thiomorpholine-4-yl, 1-oxothiomorpholine-4-yl, 1,1-dioxothiomorpholine-4-yl, 4-oxopiperidine-1-yl, 4-(lower)-alkoxypiperidine-1-yl, 4-hydroxypiperidine-1-yl, 4-hydroxyethoxypiperidine-1-yl, 4-(lower)-alkylpiperazine-1-yl, lower alkoxycarbonyl, 2-di-(lower)-alkylaminoethylsulfanyl, N,N-bis-(lower)-alkylamino-(lower)-alkyl, (lower)-alkoxycarbonyl-(lower)-alkyl, (lower)-alkylcarboxy-(lower)-alkyl, lower alkoxycarbonylmethylsulfanyl, carboxymethylsulfanyl, 1,4-dioxa-8-azaspiro[4,5]dec-8-yl, carboxy-(lower)-alkoxy-group, cyano-(lower)-alkyl, 2-oxo[1,3]dioxolane-4-yl-(lower)-alkoxy-group, 2,2-dimethyltetrahydro[1,3]dioxolo[4,5-c]pyrrole-5-yl, (3R)-hydroxypyrrolidine-1-yl, 3,4-dihydroxypyrrolidine-1-yl, 2-oxooxazolidine-3-yl, carbamoylmethyl, carboxy-(lower)-alkyl, carbamoylmethoxy-, hydroxycarbamoyl-(lower)-alkoxy-, lower alkoxycarbamoyl-(lower)-alkoxy-, (lower)-alkylcarbamoylmethoxy-group; R3 means phenyl, thiophenyl, pyridinyl that are substituted with halogen atom, cyano-group, carbamoyl, imidazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl or isoxazolyl wherein groups of 1,2,3-triazolyl, 1,2,4-triazolyl or isoxazolyl are substituted optionally with (C1-C7)-alkyl or (C1-C7)-alkylsulfanyl, and to their pharmaceutically acceptable salts. Also, invention describes a medicinal agent that is antagonist of mGlu receptors of the group II based on compound of the formula (I). The medicinal agent can be used in treatment and prophylaxis of acute and/or chronic neurological disturbances including psychosis, schizophrenia, Alzheimer's disease, disturbances in cognitive ability and memory damage.

EFFECT: valuable medicinal properties of compounds.

7 cl, 1 tbl, 98 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a prophylactic or therapeutic agent used against hyperlipidemia and comprising as an active component the heterocyclic compound of the formula [1]:

or its pharmaceutically acceptable salt wherein R1 represents aryl optionally substituted with similar or different one-three groups taken among alkyl, halogenalkyl, trihalogen alkyl, alkoxy-group and halogen atom; Het represents bivalent aromatic heterocyclic group of the formula [5]:

wherein X represents oxygen, sulfur atom or NR6 wherein R6 represents hydrogen atom or alkyl; R2 represents hydrogen atom, alkyl or trihalogenalkyl; D represents alkylene and alkenylene; E represents group of the formulae [3] or [4] wherein Y represents oxygen or sulfur atom; R3 and R4 are similar or different and each represents hydrogen atom or alkyl; p = 1; Z represents carboxy-group, alkoxycarbonyl, cyano-group or 1H-5-tetrazolyl. Also, invention relates to new compounds belonging to group of above enumerated heterocyclic compounds of the formula [1] that show effect reducing blood triglycerides level, low density lipoprotein cholesterol, glucose and insulin or effect enhancing high density lipoprotein cholesterol and effect reducing the atherogenic effect. Therefore, these compounds can be used in prophylaxis or treatment of hyperlipidemia, arteriosclerosis, heart ischemic disease, brain infarction, rheocclusion after percutaneous intraluminal coronary angioplasty, diabetes mellitus and obesity.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

29 cl, 1 tbl, 170 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to new 5-aryl-1-phenyl-4-heteroyl-3-hydroxy-3-pyrroline-2-ones of the formula:

wherein (1) X means sulfur atom (S); R means (CH3)2CH; (2) X means sulfur atom (S); R means (CH3)3C; (3) X means oxygen atom (O); R means (CH3)3C. Compounds of the formula (I) are prepared by interaction of the corresponding heteroylpyruvic acid methyl ester with mixture of aniline and aromatic aldehyde in acetic acid medium at short-time heating. Compounds elicit an anti-bacterial activity with value MIC = 3.9-7.8 mcg/ml as compared with 62-1000 mcg/ml for analogue.

EFFECT: valuable properties of compounds.

1 tbl, 3 ex

FIELD: organic chemistry, medicine, hormones.

SUBSTANCE: invention describes imidazole derivatives of the formula (I) , racemic-diastereomeric mixtures and optical isomers, pharmaceutical salts wherein ---- represents an optional bond; R1 represents hydrogen atom (H), -(CH2)m-C(O)-(CH2)m-Z1, -(CH2)m-Z1; R2 represents hydrogen atom (H), or R1 and R2 are joined with nitrogen atoms to which they are bound forming compounds represented by formulae (Ia), (Ib) or (Ic) wherein R3 represents -(CH2)m-E-(CH2)m-Z2; R4 represents hydrogen atom (H) or -(CH2)m-A1; R5 represents (C1-C12)-alkyl, (C0-C6)-alkyl-C(O)-NH-(CH2)m-Z3 and optionally substituted phenyl; R6 represents hydrogen atom (H); R7 represents (C1-C12)-alkyl or -(CH2)m-Z4; m = 0 or a whole number from 1 to 6; n is a whole number from 1 to 5. Proposed compounds bind with subtypes of somatostatin receptors selectively.

EFFECT: valuable properties of compounds.

20 cl, 13776 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new substituted indole compounds of Mannich bases of the formula (I):

wherein R1 means hydrogen atom (H), (C1-C10)-alkyl, unsubstituted phenyl or naphthyl bound through (C1-C2)-alkylene group or that monosubstituted at least with hydroxy group (-OH), halogen atom, -CF3, -CN, (C1-C6)-alkyl, (C1-C6)-alkoxy group; R2 means atoms H, F, Cl, Br, groups -CF3, -CN, -OR10, -CO(OR11), -CH2CO(OR12), -COR19, (C1-C10)-alkyl, unsubstituted phenyl or naphthyl, or that monosubstituted at least with -OH, halogen atom, -CF3, -CN, (C1-C6)-alkyl and (C1-C6)-alkoxy group; R3 means -CH(R13)N(R14)(R15); R4, R5, R6 and R7 can have similar or different values and mean atoms H, F, Cl, Br and groups -CF3, -CN, -NO2, -OR10 and others; R10 means H, -COR17, (C1-C6)-alkyl and others; R13 means unsubstituted phenyl or phenyl monosubstituted with at least (C1-C4)-alkyl, halogen atom, -CF3, -CN and -OH; R14 and R15 can have similar or different values and mean unbranched or branched (C1-C6)-alkyl, or R14 and R15 represent in common (CH2)n wherein n means a whole number from 3 to 6, or (CH2)O(CH2)2; R17 means (C1-C6)-alkyl; R19 means -NHR20, (C1-C6)-alkyl and others; R20 means H, (C1-C6)-alkyl and others, and/or their racemates, enantiomers, diastereomers and/or corresponding bases, and/or corresponding salts of physiologically acceptable acids with exception of racemates of some compounds given in claim 1. Also, invention describes method for their preparing and using as a medicinal agent possessing analgesic effect.

EFFECT: valuable medicinal properties of compounds.

42 cl, 2 dwg, 3 tbl, 103 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of imidazole of the formula (I):

or its pharmaceutically acceptable salts wherein X represents -CH2-(CH2)p-, -O-; R1 represents phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (C3-C7)-cycloalkyl wherein indicated phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (C3-C7)-cycloalkyl are substituted optionally with 1-3 substitutes taken independently among halogen atom, -OH, halogen-(C1-C6)-alkyl, (C1-C6)-alkyl, (C1-C6)-alkoxy group and OH-(C1-C6)-alkyl; R2 represents hydrogen atom (H) or (C1-C6)-alkyl; R3 represents H or (C1-C6)-alkyl; R4 represents H or (C1-C6)-alkyl; R5 represents H, or R5 and R7 form in common a bond; each R6 represents independently halogen atom, -OH, halogen-(C1-C6)-alkyl, (C1-C6)-alkyl, (C1-C6)-alkoxy group or OH-(C1-C6)-alkyl; R7 represents H, or R7 and R5 form in common a bond; each R8 represents independently -OH, (C1-C6)-alkyl, halogen-(C1-C6)-alkyl or (C1-C6)-alkoxy group; m = 0, 1, 2 or 3; n = 0 or 1; p = 0 or 1; r = 0 or 1; t = 0. Also, invention relates to a method for preparing compounds of the formula (I) and to a pharmaceutical composition showing affinity to alpha-2-adrenoceptors based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof used in aims for treatment of neurological disturbances, psychiatric disorders or disturbances in cognitive ability, diabetes mellitus, lipolytic diseases, orthostatic hypotension or sexual dysfunction.

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

25 cl, 1 tbl, 14 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes N-substituted azaheterocyclic carboxylic acids and their esters of the formula (I):

wherein R1 and R2 represent independently hydrogen, halogen atom, NR6R7 or (C1-C6)-alkyl; Y represents >N-CH2 or >C=CH2- wherein only underlined atom is a component of the ring system; X represents -O-, -S-, -CH2CH2- wherein R6 and R7 represent independently (C1-C6)-alkyl; r = 1, 2 or 3; Z represents heterocycle taken among formulas (a), (b), (c), (d), (f), (k), (g) and (j) given in the invention claim. Also, invention relates to a method for their preparing and pharmaceutical composition based on compounds of the formula (I). Invention describes a method for inhibition of neurogenous pain, inflammation and blood glucose level increase to patient by administration to patient the effective dose of compound of the formula (I). Compounds of the formula (I) elicit ability to inhibit the neurogenous pain and blood glucose enhanced level.

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

13 cl, 1 tbl, 30 ex

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