4,6-bis-(morpholyl)-2-[2'-ethoxyacetyltetrazolyl)-5'-yl]-1,3,5-triazine as antidote

FIELD: organic chemistry, agriculture.

SUBSTANCE: invention describes a new compound 4,6-bis-(morpholyl)-2-[(2'-ethoxyacetyltetrazolyl)-5'-yl]-1,3,5-triazine of the formula: that represents an antidote against phytotoxic effect of herbicide 2,4-dichlorophenoxyacetic acid on germinating sunflower seeds and seedlings.

EFFECT: valuable properties of compound.

2 cl, 2 tbl, 3 ex

 

The invention relates to the field of chemistry and agriculture, specifically to the derived series of 1,3,5-triazine as a compound that protects against fetotoksicheskoe actions of herbicides in the cultivation of sunflower (antidote).

Known 2-methoxy-4-morpholin-6-[(4'-phenylcarbamoyl-5'-methyl-1',2',3'-triazole)-1'-yl]-1,3,5-triazine (MFT) formula:

which is the antidote from fetotoksicheskoe action of the herbicide 2,4-D on the germinating seeds and seedlings of sunflower [see Pat of the Russian Federation No. 2230066; IPC707 D 403/04, A 01 N 43/68; Snehalata Ask, Ightmare, Avezov, Nscontrol, Vinsanity 2-Methoxy-4-morpholin-6-[(4'-phenylcarbamoyl-5'-methyl-1',2',3'-triazole)-1'-yl]-1,3,5-triazine as an antidote. Bull. Fig. 2004, No. 16]. The disadvantage of its use is relatively low activity in reducing fetotoksicheskoe action of the herbicide 2,4-D on seeds and seedlings of sunflower.

Technical solution to the problem is more active antidotes series of 1,3,5-triazine and an effective increase in the length of roots and hypocotyls of seedlings of sunflower in the background fetotoksicheskoe of herbicides, as well as extending the range of known antidotes.

This object is achieved by obtaining a new connection 4,6-bis (morpholin)-2-[(2'-ethoxyethylacetate)-5'-yl]-1,3,5-triazine (DEET) formula:

which can be used as an effective antidote, from fetotoksicheskoe action of the herbicide 2,4-dichlorphenoxy acid in sunflower.

The novelty of the claimed proposal is seen that a new, more active connection of a series of 1,3,5-triazine as antidotes vegetative plants of sunflower, which allows to increase the length of the roots and hypocotyls of seedlings of sunflower.

In this case the claimed connection get known method the interaction of the corresponding 4,6-bis(dimorphic)-2-[(2'-tetrazol(2 N)-5'-yl]-1,3,5-triazine with equimolar amount of ethyl ester of 2-bromatology acid in abs. ethanol in the presence of metallic sodium at the boiling temperature of the solvent [see General organic chemistry /edited by Dbarton and Udelays. - M.: Chemistry. 1981, vol. 1, s]. The original 2-cyano-4,6-disubstituted 1,3,5-triazine also get a known method [see Weigand-Hilgetag. Methods experiment in organic chemistry. - M.: Chemistry, 1969. s].

Used ethyl ester 2-bromatology acid and ethanol immediately before use purified by fractional distillation and ethanol dehydrated over anhydrous copper sulfate and dispersed according to the method [see Agordon, Rford. Satellite chemist. M: Peace. 1976. - 541 S.].

Examples of execution of the announced proposals to provide the Lena river below.

Example 1. 4,6-Bis(morpholin)-2-[(2'-ethoxyethylacetate)-5'-yl]-1,3,5-triazine (GATT). To a solution of 2.64 g (0.01 mol) of 2-cyano-4,6-bis(dimorpholino)-1,3,5-triazine in 10 ml of dry and cleaned dimethylformamide under stirring at a temperature of 20-25°C, are added dropwise separately prepared solution of a mixture of 0.65 g (0.01 mol) of sodium azide and 0.54 g (0.01 mol) of dry ammonium chloride in 10 ml of dimethylformamide. The reaction mixture was refluxed for 8-10 h and cooled to 20°C. the Mixture under stirring, a squirt poured into 100 ml of chilled 10°With water. The resulting white precipitate is filtered off, washed with water of residual solvent and ammonium chloride and dried at 20-25°C. Obtain 1.56 g (59,0%) GATT in the form of a white powder with TPL 189-190°insoluble in water, but soluble in polar organic solvents.

Found,%: C 49,35; N 7,41; N 43,10. With12H21N9. Calculated,%: C 49,46; N 7,26; N 43,27.

X νcm-1(group): 3250-3450 USS NH; 1630, 1560, 1530 S.(C=C, C=N, N=N - t. and cyanurates cycle.);

TMR, δ, ppm (group): 16,20-16,50 (1H USS NH); 3,50-of 3.80 (8H, m, NCH2); 1,15-1,25 (10H, m, NCH2CH3).

Mol. ion (mass by a spectroscope) 291.

To a solution of 0.04 g (to 0.016 mol) of metallic sodium in 10 ml of absolute ethanol is added dropwise a solution obtained as described above 0.5 g (to 0.016 mol) of 4,6-bis(dimorpholino-2-[(2'-tetrazol(2 N)-5'-yl]-1,3,5-triazine in 5 ml of abs. of ethanol. While boiling under reflux to the mixture is added dropwise 0.27 g (0,016 mol) ethyl ester 2-bromatology acid and continue boiling 10-11 hours Then the solvent is distilled to dryness in a water-jet pump vacuum at 20-25°and the dry residue repeatedly washed with water, filtered and dried at 40-50°C. Obtain 0.34 g (53,0%) DEATH in the form of a white powder with TPL 119-120°insoluble in water, but soluble in polar organic solvents.

Found, %: C 47,26; N By 5.87; N 30,96. C16H23N9O4. Calculated,%: C 47,40; N To 5.57; N 31,10.

X νcm-1(group):

TMR, δ, ppm (group):

Mol. ion (mass by a spectroscope) 405.

Example 2. 4,6-Bis(morpholin)-2-[(2'-ethoxyethylacetate)-5'-yl]-1,3,5-triazine (DEET). Under conditions analogous to example 1, 0.04 g (to 0.016 mol) of metal hydroxide, 0.5 g (to 0.016 mol) of 4,6-bis(dimorphic)-2-[(2'-tetrazol(2 N)-5'-yl]-1,3,5-triazine and 0.27 g (0,016 mol) ethyl ester 2-bromatology acid, with the only difference that the boiling continue 9-10 h obtain 0.34 g (53,0%) DEATH in the form of a white powder with TPL 119-120°insoluble in water but soluble in polar organic solvents.

Found,%: C 47,26; N By 5.87; N 30,96. C16H23N9O4. Calculated,%: C 47,40; N To 5.57; N 31,10.

X νcm-1(group):

TMR, δ, ppm (group):

Mol. ion (m is CC-by a spectroscope) 405.

Received DEATH used as an antidote to reduce fetotoksicheskoe action of the herbicide 2,4-D on the sprouted seeds (sprouts) podsolnechnika in laboratory experience. While preparing for his workers aqueous solutions of concentrations from 0.01 to within 0.00001 wt.% and treated germinated sunflower seeds varieties VNIIMK 8883, pre-sprayed with a water dispersion of 2,4-D (standard) as described below in example 3. For comparison, using an aqueous solution MFT (prototype). Due to the poor solubility in water, used MFT, DEATH and 2,4-D pre "podrastet" in a small amount of alcohol. As a control, use the option of processing water.

Example 3. In laboratory experience, couched in constantly moist filter paper in a Petri dish sunflower seeds (25 seeds per Cup in five replicates) after 4 days from the beginning of germination at 23°subjected to sequential exposure to aqueous dispersions of the herbicide 2,4-D, and after 1 h in an aqueous solution of the stated DEATH a given concentration. Continue germination under the same conditions for another 3 days. and determine the root length of seedlings (data bring to the table). The decrease in root length and hypocotyl in the advanced options in comparison with control (Amindin % is determined by the formula:

Andmind.=(O/C)·100,

where and is the length of the prophetic is Dow in the control and experimental variants, respectively.

Examples 4-9 carry out strictly the same experience 3 way. To control spending experience 4 using only water (control), as well as experience using only the herbicide 2,4-D in the specified concentrations (reference). For comparison, in similar conditions and conduct experiments using as an antidote known connections MFFT.

All experimental data are subjected to statistical analysis using t-student test at a confidence level of 0.95.

As can be seen from table 1, the application on the background of the impact of the herbicide 2,4-D proposed connection DEET as antidote provides in comparison with the standard increase in root length of seedlings of sunflower 54.8-87,1% (48-58 mm instead of 31 mm in the case of the standard), while the use of known means MFT provides an increase of only 23.1-46,0% (32-38 mm instead of 26 mm in the case of the standard). It is also clear that if as a result of fetotoksicheskoe steps of the standard length of the hypocotyl of seedlings is reduced in comparison with control 54.5%, (30 mm instead of 66) the use of the claimed DIET reduces fetotoksicheskoe herbicide action and the length of the hypocotyl is increased in comparison with the standard to 48.3-68,3% (44,5-50,5 mm), while the application of the known compounds of the prototype MFT reduces this figure only 8.9-14.3 per cent.

Thus, the application States the military connection as antidote allows background fetotoksicheskoe impact of herbicide to increase the length of the roots and hypocotyls of seedlings, and also to expand the range of known antidotes.

Table 2

Antidote activity of the synthesized compounds in relation to the length of the hypocotyl
ConnectionThe length of the hypocotyl, mm2,4-D + safener in concentration, wt.%
Control (water)2,4-D (standard)10-210-310-410-5
Root length, mm% benchmark*Root length, mm% benchmark*Root length, mm% benchmark*Root length, mm% benchmark*
Examples:456789
74353911,44014,339,512,838,18,9
66 304550.0a 50.568,34860,044,548,3

4,6-Bis(morpholin)-2-[(2'-ethoxyethylacetate)-5 '-yl]-1,3,5-triazine of the formula

which is the antidote from fetotoksicheskoe action of the herbicide 2,4-dichlorophenoxyacetic acid on the germinating seeds and seedlings of sunflower.



 

Same patents:

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new nitrogen-containing aromatic derivatives of the general formula:

wherein Ag represents (1) group of the formula:

; (2) group represented by the formula:

or ; (3) group represented by the formula:

; Xg represents -O-, -S-, C1-6-alkylene group or -N(Rg3)- (wherein Rg3 represents hydrogen atom); Yg represents optionally substituted C6-14-aryl group, optionally substituted 5-14-membered heterocyclic group including at least one heteroatom, such as nitrogen atom or sulfur atom, optionally substituted C1-8-alkyl group; Tg1 means (1) group represented by the following general formula:

; (2) group represented by the following general formula: . Other radical values are given in cl. 1 of the invention claim. Also, invention relates to a medicinal agent, pharmaceutical composition, angiogenesis inhibitor, method for treatment based on these compounds and to using these compounds. Invention provides preparing new compounds and medicinal agents based on thereof in aims for prophylaxis or treatment of diseases wherein inhibition of angiogenesis is effective.

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

40 cl, 51 tbl, 741 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new substituted derivatives of pyrrole of the formula (I): wherein R1 and R1' mean independently hydrogen atom (H) or (lower)-alkyl, unsubstituted or substituted (lower)-alkoxy-group; R2 means hydrogen atom (H), nitro-group (-NO2), cyano-group (-CN), halogen atom, unsubstituted (lower)-alkyl or substituted with halogen atom or (lower)-alkoxy-group; R2' means thiazolyl, thiophenyl, isothiazolyl, furanyl and pyrazolyl that is unsubstituted or substituted with (lower)-alkyl, pyrimidinyl, unsubstituted morpholinyl, unsubstituted pyrrolidinyl and imidazolyl that is unsubstituted or substituted with (lower)-alkyl, unsubstituted piperidinyl or piperazinyl that is unsubstituted or substituted with (lower)-alkyl, or ethoxy-group substituted with imidazolyl, or its pharmaceutically acceptable salt. Compounds of the formula (I) inhibit cell proliferation in G2/M phase of mitosis that allows their using in the pharmaceutical composition.

EFFECT: valuable biological properties of compounds.

36 cl, 4 sch, 1 tbl, 21 ex

FIELD: organic chemistry, heterocyclic compounds, medicine.

SUBSTANCE: invention relates to derivatives of piperazine and piperidine of the formula (I): wherein ---Z represents =C or -N; Q means benzyl or 2-, 3- or 4-pyridylmethyl that can be substituted with one or more substitutes taken among group comprising halogen atom, cyano-group, (C1-C3)-alkoxy-group, CF3, OCF3, SCF3, (C1-C4)-alkyl, (C1-C3)-alkylsulfonyl and their salts, and to a method for their preparing also. It has been found that these compounds elicit valuable pharmacological properties owing to combination of (partial) agonism with respect to members of dopamine receptors subtype and affinity with respect to corresponding serotonin and/or noradrenergic receptors and can be useful in preparing compositions used in treatment of fear and/or depression or Parkinson's disease.

EFFECT: valuable medicinal properties of compounds.

7 cl, 1 tbl, 3 ex

FIELD: organic chemistry, medicinal biochemistry, pharmacy.

SUBSTANCE: invention relates to substituted benzimidazoles of the formula (I): and/or their stereoisomeric forms, and/or their physiologically acceptable salts wherein one of substitutes R1, R2, R3 and R4 means a residue of the formula (II): wherein D means -C(O)-; R8 means hydrogen atom or (C1-C4)-alkyl; R9 means: 1. (C1-C6)-alkyl wherein alkyl is linear or branched and can be free of substituted by one-, bi- or tri-fold; Z means: 1. a residue of 5-14-membered aromatic system that comprises from 1 to 4 heteroatoms as members of the cycle that represent nitrogen and oxygen atoms wherein aromatic system is free or substituted; 1.1 a heterocycle taken among the group of oxadiazole or oxadiazolone that can be unsubstituted or substituted; 2. (C1-C6)-alkyl wherein alkyl is a linear or branched and monosubstituted with phenyl or group -OH; or 3. -C(O)-R10 wherein R10 means -O-R11, -N(R11)2 or morpholinyl; or R8 and R9 in common with nitrogen atom and carbon atom with that they are bound, respectively, form heterocycle of the formula (IIa): wherein D, Z and R10 have values given in the formula (II); A means a residue -CH2-; B means a residue -CH-; Y is absent or means a residue -CH2-; or X and Y in common form phenyl. The cyclic system formed by N, A, X, Y, B and carbon atom is unsubstituted or monosubstituted with (C1-C8)-alkyl wherein alkyl is monosubstituted with phenyl, and other substitutes R1, R2, R3 and R4 mean independently of one another hydrogen atom, respectively; R5 means hydrogen atom; R6 means the heteroaromatic cyclic system with 5-14 members in cycle that comprises 1 or 2 nitrogen atoms and can be unsubstituted or substituted. Also, invention relates to a medicinal agent for inhibition of activity of IkB kinase based on these compounds and to a method for preparing the indicated agent. Invention provides preparing new compounds and medicinal agents based on thereof for aims for prophylaxis and treatment of diseases associated with the enhanced activity of NFkB.

EFFECT: valuable medicinal properties of compounds and composition.

4 cl, 7 tbl, 224 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of azole of the formula:

wherein R1 represents (1) halogen atom; (2) nitrogen-containing 5- or 6-membered heterocyclic group comprising from 1 to 4 nitrogen atoms as atoms of ring system in addition to carbon atoms, and group with condensed rings comprising nitrogen-containing 5- or 6-membered heterocyclic group comprising 1-2 nitrogen atoms as atoms of ring system in addition to carbon atoms, and benzene ring wherein nitrogen-containing 5- or 6-membered heterocyclic group and group with condensed rings can comprise optionally from 1 to 3 substituted taken among group consisting of: (i) aliphatic hydrocarbon group comprising from 1 to 15 carbon atoms; (ii) (C6-C14)-aryl group, and (iii) carboxy-group that can be in form of group of (C1-C6)-alkyl ester wherein above indicated substitutes (i)-(iii) can have from 1 to 3 substituted additionally taken among group consisting of: (a) carboxyl group and (b) hydroxy-group; (3) (C1-C10)-alkylsulfanyl group that can be substituted with hydroxy-group; (4) heteroarylsulfanyl group taken among pyridylsulfanyl, imidazolylsulfanyl and pyrimidinylsulfanyl, or (5) amino-group that can be mono- or di-substituted optionally with substitutes(substitutes) among group consisting of: (i) (C1-C10)-alkyl group that can be substituted with hydroxy-group, and (ii) (C7-C10)-aralkyl group; Ab represents aryloxy-group that is substituted with alkyl group and can be substituted with halogen atom, (C1-C4)-alkoxy-group, (C1-C4)-alkyl group, hydroxy-group or (C1-C6)-alkylcarbonyloxy-group additionally; B represents (C6-C14)-aryl group or thienyl group each of that can has optionally from 1 to 4 substitutes taken among halogen atom, (C1-C6)-alkoxy-group and (C1-C6)-alkyl group that can has optionally from 1 to 3 halogen atoms; Y represents saturated aliphatic bivalent group with direct or branched chain and having from 1 to 7 carbon atoms, or to its salt. Also, invention relates to a pharmaceutical composition that elicits activity for promoting production/secretion of neurotrophine, and to methods for prophylaxis and treatment based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof used for prophylaxis and treatment of neuropathy.

EFFECT: improved and valuable medicinal properties of agent, improved methods for treatment.

19 cl, 1 dwg, 5 tbl, 122 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new piperidine compounds of the general formula (I) wherein A means preferably ring of the formula:

wherein R1 means hydrogen atom (H), cyano-group (CN), (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C8)-cycloalkyl, (C3-C8)-cycloalkenyl, (C1-C6)-alkoxy-, (C1-C6)-alkylthio-group; W means (C1-C6)-alkylene that can be substituted, ordinary bond; Z means optionally substituted aromatic hydrocarbon cyclic (C6-C14)-group; l means a number from 0 to 6. Compounds show the excellent activity directed for inhibition of sodium channels and selective inhibition of potassium channels.

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

26 cl, 4 tbl, 476 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes derivative of aroylpiperazine of the formula (I):

wherein Y means lower alkylene; R1 means phenyl with 1 or 2 substitutes taken among group consisting of trihalogen-(lower)-alkyl, halogen atom, lower alkylamino-, di-(lower)-alkylamino- and nitro-group; R2 means phenyl or indolyl and each comprises 1 or 2 substitutes taken among group consisting of lower alkyl, trihalogen-(lower)-alkyl, lower alkylene dioxy-, hydroxy-group, hydroxy-(lower)-alkyl, lower alkoxy- lower alkylamino- and di-(lower)-alkylamino-group; R3 means hydrogen atom; R4 means morpholinyl-(lower)-alkyl comprising 1 or 2 substitutes taken among group consisting of ethyl, hydroxy-(lower)-alkyl, halogen-(lower)-alkyl and lower alkoxy-(lower)-alkyl, or morpholinyl-(lower)-alkynyl that can comprise 1 or 2 substitutes taken among group consisting of ethyl, propyl, isopropyl, isobutyl, spirocyclo-(lower)-alkyl, lower alkoxy-(lower)-alkyl, hydroxy-(lower)-alkyl, carboxy-(lower)-alkyl, di-(lower)-alkyl-carbamoyl, lower alkoxycarbonyl and halogen-(lower)-alkyl. Also, invention relates to a method for preparing, pharmaceutical composition based on these compounds and a method for treatment of tachykinine-mediated diseases, such as respiratory diseases, ophthalmic, cutaneous, inflammatory diseases, and as analgetic agents. Describes compounds are antagonists of tachykinine.

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

8 cl, 94 ex

FIELD: organic chemistry, chemical technology, agriculture.

SUBSTANCE: invention describes substituted azadioxocycloalkenes of the general formula (I): wherein A means unsubstituted or methyl-substituted dimethylene; Ar means unsubstituted or fluorine-substituted ortho-phenylene, thiophendiyl or pyridindiyl; E means group of the formula: wherein G means oxygen atom, groups -O-CH2-, -CH2-O- or -C(CH3)=N-O-CH2-; Z means unsubstituted or substituted phenyl, pyrimidinyl or thiadiazolyl, or naphthyl. Invention describes 4 methods for preparing compounds of the formula (I), 5 species of intermediate compounds used for preparing compounds of the formula (I), fungicide agents comprising compound of the formula (I) as an active substance, a method for preparing fungicide agents, method for control of harmful fungi using compound of the formula (I). Compounds of the formula (I) show fungicide properties and therefore they can be used in agriculture.

EFFECT: improved preparing methods, valuable properties of compounds.

13 cl, 5 tbl, 18 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of cyclic amide of the formula (I)

or its salt, or hydrate, or solvate wherein X represents (C1-C6)-alkyl, (C1-C6)-alkyl substituted with phenyl, (C2-C6)-alkenyl substituted with phenyl or halogenphenyl, (C2-C6)-alkynyl substituted with phenyl, phenyl that can be substituted with (C1-C6)-alkyl; one or more halogen atom, nitro-group, phenyl, (C1-C6)-alkoxy-group, halogen-(C1-C6)-alkyl, halogen-(C1-C6)-alkoxy-group, phenyl-(C1-C6)-alkyl, (C1-C6)-alkoxyphenyl-(C1-C6)-alkyl, amino-group, optionally substituted with (C1-C6)-alkyl, acetyl, (C1-C6)-alkoxy-group, substituted with phenyl, phenylcarbonyl, furanyl; 1- or 2-naphthyl, monocyclic (C3-C8)-cycloalkyl, amino-group substituted with one or more substitutes taken among phenyl, halogenphenyl, (C1-C6)-alkoxyphenyl, (C1-C6)-alkyl, halogen-(C1-C6)-alkyl, phenyl-(C1-C6)-alkyl; 5- or 6-membered monocyclic heterocyclic group comprising 1 or 2 heteroatoms, such as nitrogen (N), oxygen (O), sulfur (S) atom optionally substituted with halogenphenyl, halogen atom, benzyl, (C1-C6)-alkyl, phenyl; 8-10-membered bicyclic heteroaryl group comprising 1 or 2 heteroatoms taken among N, O and optionally substituted with halogen atom; 8-10-membered polycyclic cycloalkyl group; Q means -CH2-, -CO-, -O-, -S-, -CH(OR7)- or -C(=NR8)- wherein R7 means hydrogen atom (H), (C1-C6)-alkyl; R8 means OH, (C1-C)-alkoxy-group, acylamino-group, (C1-C6)-alkoxycarbonylamino-group, phenyl-(C1-C6)-alkoxy-group; n = 0-5; B represents group or wherein each among R3, R4, R5 and R6 represents independently substitute taken among group consisting of hydrogen atom (H), halogen atom, NO2 (nitro-group), (C1-C6)-alkoxy-group, CN (cyano-group); m = 1 or 2; ring represents 5- or 6-membered aromatic heterocyclic ring comprising one or two heteroatoms taken among O, S, N. Compound of the formula (I) elicit activity inhibiting binding sigma-receptors that allows their using as component of medicinal agent.

EFFECT: valuable medicinal properties of compounds.

21 cl, 2 sch, 4 tbl, 183 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of tetrahydroisoquinoline of the formula [I] wherein R1 represents hydrogen atom or lower alkyl; R2 represents alkyl having optionally a substitute taken among alkoxycarbonyl and carboxy-group, cycloalkyl, cycloalkylalkyl, aryl having optionally a substitute taken among lower alkyl, arylalkyl having optionally a substitute taken among lower alkyl, lower alkoxy-group, halogen atom and acyl, alkenyl, alkynyl, or monocyclic heterocyclylalkyl wherein indicated heterocycle comprises 5- or 6-membered ring comprising nitrogen atom and having optionally a substitute taken among lower alkyl; R3 represents hydrogen atom or lower alkoxy-group; A represents a direct bond or >N-R5 wherein R5 represents lower alkyl; B represents lower alkylene; Y represents aryl or monocyclic or condensed heterocyclyl comprising at least one heteroatom taken among oxygen atom and nitrogen atom and having optionally a substitute taken among lower alkyl, carboxy-group, aryl, alkenyl, cycloalkyl and thienyl, or to its pharmaceutically acceptable salt. Also, invention relates to pharmaceutical composition eliciting hypoglycaemic and hypolipidemic effect based on these derivatives. Invention provides preparing new compounds and pharmaceutical agents based on thereof, namely, hypoglycaemic agent, hypolipidemic agent, an agent enhancing resistance to insulin, therapeutic agent used for treatment of diabetes mellitus, therapeutic agent against diabetic complication, agent enhancing the tolerance to glucose, agent against atherosclerosis, agent against obesity, an anti-inflammatory agent, agent for prophylaxis and treatment of PPAR-mediated diseases and agent used for prophylaxis and treatment of X-syndrome.

EFFECT: valuable medicinal properties of compounds and composition.

13 cl, 7 tbl, 75 ex

FIELD: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention describes a composition showing the selective effect and comprising as conventional inert adjuvants and the following mixture as an active component: a) effective amount of compound of the formula (I): as a herbicide wherein each R1 and R3 means independently of one another (C1-C4)-alkyl; R4 and R5 mean the group: -C-R14(R15)-C-R16(R17)-O-R18(R19)-C-R20(R21)-(Z2) wherein R14, R15, R16, R17, R18, R19, R20 and R21 mean hydrogen atom; G means hydrogen atom, -C(X1)-R30, alkaline metal cation, earth-alkaline metal cation, sulfonium or ammonium cation; X1 means oxygen atom; R30 means hydrogen atom, (C1-C10)-alkyl, and salts and diastereomers of compounds of the formula (I) under condition that R1 and R3 don't methyl group simultaneously; b) effective amount of protective agent (antidote) for prevention of hazard effect of herbicide wherein antidote is taken among the group comprising clochintocet, clochintocet with alkaline metal cation, earth-alkaline metal cation, sulfonium or ammonium cation, clochintocet-mexil, mefenpir, mefenpir with alkaline metal cation, earth-alkaline metal cation, sulfonium or ammonium cation and mefenpir-diethyl, and c) additive comprising (C8-C22)-saturated acids alkyl ester or emulsified vegetable oil, or mineral oil taken in the amount 0.01-2% as measured to the spraying mixture mass. Also, invention describes a method for selective control of weed and grassy plants in cultural plant plantings that involves using the abovementioned composition for treatment. Invention provides the selective effect in control of weed and grassy plants, in particular, in cereals crops plantings.

EFFECT: improved control method, valuable agricultural properties of composition.

3 cl, 8 tbl, 2 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: invention relates to selective herbicidal compositions, containing customary auxiliary substances, as well as: a) herbicidal effective amount of compound of formula I or agriculture acceptable salt thereof wherein R are independently C1-C6-alkyl, C1-C6-haloalkyl, C1-C4-alcoxy-C1-C4-alkyl, or C1-C4-alcoxy-C1-C4-alcoxy-C1-C4-alkyl; m = 2; Q is group of formula wherein R23 is hydroxyl and Y is C1-C4-alkylen bridge; and b) synergetically effective amount of one or more herbicides; and methods for controlling of undesired plants in tame cultures using the said composition. Also disclosed is composition containing customary auxiliary substances, as well as herbicidal and synergetically effective amount of 4-hydroxy-3-(2-methyl-6-trifluoromethylpyridine-3-carbonyl)bicyclo[3.2.1]octo-3-ene-2-one of formula 2.2 and herbicidal antagonistically effective amount of antidote of formula 3.1. Compositions based on 4-hydroxy-3-(2-methyl-6-trifluoromethylpyridine-3-carbonyl)bicyclo[3.2.1]octo-3-ene-2-one and herbicidal antagonistically effective amount of antidote, as well as methods for controlling of weeds and cereal grasses in tame cultures also are described.

EFFECT: compositions useful in effective controlling of many weeds both in pre-spring and post-spring phases.

5 cl, 63 tbl, 12 ex

FIELD: agriculture.

SUBSTANCE: invention describes a chitosan-base composition reducing the content of nitrates in plant growing production. The composition comprises chitosan of molecular mass 20-150 kDa, organic acids - mixture of succinic, ascorbic and sorbic acids in the mass ratio = 2:1:1, respectively, activating agents of nitrate and nitrite reductases - iron nitrate, ammonium molybdate, indolyl acetic acid and ethylenediaminetetraacetic acid in the mass ratio = 20:5:1:1, respectively; or iron nitrate, ammonium molybdate, indolyl acetic acid and N,N-dicarboxymethylglutamic acid in the mass ratio = 20:5:1:1, respectively, and substances enhancing synthesis of chlorophyll - 2-oxoglutaric acid and L-glutamic acid in the mass ratio = 30:1, and a surface-active substance also in the following ratio of above indicated components, wt.-%: chitosan, 15-25; organic acids, 15-25; activators of nitrate and nitrite reductases, 25-30; enhancers of chlorophyll synthesis, 29-35, and surface-active substance, 1-3. The composition provides enhancing assimilation of inorganic nitrogen in plant and reduces the content of nitrates in plant growing productions.

EFFECT: valuable properties of composition.

5 tbl

FIELD: agriculture.

SUBSTANCE: invention relates to application of 2-chloro-4,6-bis[thiophenyl]-1,3,5-triazine as antidote to reduce phytotoxic action of 2,4-dichlorophenoxyacetic acid butyl ester thereof to sunflower germs end vegetating plants.

EFFECT: effective increase of root length and sunflower yield.

2 tbl, 8 ex

FIELD: organic chemistry, agriculture, herbicide composition.

SUBSTANCE: invention relates to herbicide composition, containing conventional inert additives and mixture of a) herbicidically effective amount of substance satisfying the formula I [in formula R1 and R3 are the same or different C1-C4-alkyl; R4 and R5 together form groups of formulae: -C-R6(R7)-O-C-R8(R9)-C-R10(R11)-C-R12(R13)-(Z1), -C-R14(R15)-C-R16(R17)-O-C-R18(R19)-C-R20(R21)-(Z2), or -C-R22(R23)-C-R24(R25)-C-R26(R27)-O-C-R28(R29)-(Z3), wherein each R6-R29 is hydrogen; G is hydrogen or -C(X2)-X3-R31; X2 and X3 independently are oxygen; R31 is C1-C10-alkyl]; b) herbicidic synergic amount of at least one herbicide selected from group containing sulfonylureas, phenoxyacetic acids, as well as florsulam, tralcoxidim, klodinafol-propargil, phenoxaprop-P-ethyl, trifluramine, pendimethaline, picolinafen, etc. Composition also may contain safety effective amount of protective agent, such as chloquintocet-mexyl and additive (e.g., mineral oil or C8-C22-fat acid alkyl esters) in amount of 0-2 mass %. Also disclosed is method for selective controlling of weeds and grassy plants in cultural plants by treatment of cultural plants, seeds or seedlings thereof, or vegetation area thereof with claimed composition.

EFFECT: effective composition and method for weed controlling.

5 cl, 11 tbl, 7 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: claimed mixture from herbicides and antidotes contains (A) herbicidically active substance based on phenylsulfonylureas of formula I and salts thereof (in formula R1 is hydrogen or C1-C6-alkyl; R2 is C1-C3-alkyl; R3 is C1-C3-alkoxy; R4 is hydrogen or C1-C4-alkyl; Hal is fluorine, chlorine, bromine, or iodine); and (B) antidote of formulae II or III , wherein X is hydrogen, halogen, C1-C4-alkyl; C1-C4-alkoxy, nitro or C1-C4-haloalkyl; Z is hydroxyl, C1-C8-alkoxy, C3-C6-cycloalkoxy, C2-C8-alkenyloxy, C2-C8-alkynyloxy; R5 is C1-C2-alkandiyl chain optionally substituted with one or two C1-C4 alkyl residues or (C1-C3-alcoxy)carbonyl; W is bivalent heterocyclic residue; n = 1-5; in weight ratio herbicide/antidote of 100:1-1:100. Also disclosed is method for protection of cultural plants against phytotoxic side effect of herbicidically active substance of formula I. Claimed method includes antidote application of formulae II or III on plant, plant parts, plant seeds or seeding areas before or together with herbicidically active substance in amount of 0.005-0.5 kg/hectare in weight ratio of 100:1-1:100.

EFFECT: mixture for effective selective weed controlling in cultural plant, particularly in maize and grain cultures.

8 cl, 2 ex, 7 tbl

FIELD: agriculture, plant science, plant protection.

SUBSTANCE: the suggested herbicidal composition of selective action contains, except generally accepted additional substances for the composition, a mixture as an active substance including a) herbicidally efficient quantity of compound of formula (I) , where R1 and R3 each independently means ethyl, ethynyl, C1- or C2alkoxy; R4 and R5 forms together the group Z2-CR14(R15)-CR16(R17)-O-CR18(R19)-CR20(R21)-(Z2); R14, R15, R16, R17, R18, R19, R20 and R21 means hydrogen; G means hydrogen, -C(X1)-R30, -C(X2)-X3-R31; X1, X2, X3 means oxygen; R30, R31 each independently means C1-C10alkyl, or salts or diastereoisomer of compound of formula (I), and b) efficient quantity of antidote of formula IIa to prevent harmful action of herbicide, where R22 means hydrogen, alkaline-earth metal or ethyl, or of formula IIb , where R23 means hydrogen, alkaline-earth metal or ethyl, and method for selective control for weed plants and grasses in cultivated plants. Thus, the antidote decreases the damage of cultivated plants induced by herbicide of formula (I).

EFFECT: higher efficiency of plant protection.

3 cl, 4 ex, 4 tbl

FIELD: agriculture, insecticides.

SUBSTANCE: invention relates to insecticide covers for seeds that comprise one or some binding substances taken among the group including polymers and copolymers of polyvinyl acetate, methylcellulose, polyvinyl alcohol, vinylidene chloride, acryl, cellulose, polyvinylpyrrolidone and polysaccharide, and insecticide and a filling agent also. A binding agent forms matrix for insecticide and a filling agent. Also, invention relates to a method for control of insect-pests that involve applying a cover on seeds. Also, invention relates to a method for preparing seeds with cover that involves mixing a binding agent, carrier and insecticide, applying a mixture of seed, drying and applying an additional filming cover. Method for protecting the germinating seedlings involves applying the insecticide cover on seeds. Invention provides reducing the phytotoxic effect of insecticide on seeds.

EFFECT: valuable agricultural properties of insecticide cover.

24 cl, 5 tbl, 5 ex

The invention relates to agriculture and to the chemistry of biologically active substances

FIELD: agriculture, insecticides.

SUBSTANCE: invention relates to insecticide covers for seeds that comprise one or some binding substances taken among the group including polymers and copolymers of polyvinyl acetate, methylcellulose, polyvinyl alcohol, vinylidene chloride, acryl, cellulose, polyvinylpyrrolidone and polysaccharide, and insecticide and a filling agent also. A binding agent forms matrix for insecticide and a filling agent. Also, invention relates to a method for control of insect-pests that involve applying a cover on seeds. Also, invention relates to a method for preparing seeds with cover that involves mixing a binding agent, carrier and insecticide, applying a mixture of seed, drying and applying an additional filming cover. Method for protecting the germinating seedlings involves applying the insecticide cover on seeds. Invention provides reducing the phytotoxic effect of insecticide on seeds.

EFFECT: valuable agricultural properties of insecticide cover.

24 cl, 5 tbl, 5 ex

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