Herbicide composition

 

(57) Abstract:

Usage: agriculture, chemical means of plant protection. The inventive composition comprises a derivative of uracil 1, where R1- trifluoromethyl or pentafluoroethyl; R2group of the formula 2 and 3, where R4is hydrogen, fluorine, chlorine A2is hydrogen, C1-C3- alkyl, alpil, propargyl, 1-methylpropenyl, cyanomethyl; methoxymethyl, benzyl, o-methylbenzyl, p-methylbenzyl, picolyl, R6the group of formulas 4 and 5, SCH2CO2CH3or N(R8)SO2R7where R7- straight or branched C1-C4-alkyl, 3-chloropropyl or 2, 2, 2-triptorelin R8is hydrogen, C1-C2-alkyl or methylsulphonyl in an amount of 0.1-90 wt. % ; additives target - the rest. 14 table. , , , ,

The invention relates to herbicide compositions exhibiting selectivity and containing uracile derivative as an active ingredient.

A huge variety of herbicides was obtained and used in practice for the protection of important crop plants, such as rice, soybeans, wheat, corn, cotton, beet and others , from weeds and to increase the productivity of these agriculture is sdelete on the following three types: (1) a herbicide for upland crops, (2) herbicides for rice fields, and (3) and herbicides for non-arable lands. Each type of herbicides might be further subdivided into subclasses, such as the herbicide is the type of soil, preschoolage type of processing and post-harvest processing type (leaves) in accordance with the method of application.

As such herbicides are required substances, which can satisfy the following requirements.

Herbicide effect is high when the use of small quantities. (It is necessary, especially from the point of view of environmental protection to eliminate weeds when applied, as smaller quantities of herbicides).

Residual action is appropriate (recently mentioned problem related to the fact that the chemicals that preserve their action in the soil for a long time, cause damage to subsequent plants. Thus, it is important that the chemical was retained after applying the proper residual effect).

Weeds after application are destroyed quickly. (Provided the opportunity to conduct the seeding and transplant subsequent crops in a short time the Noi. (For selskohozaystvennih or agriculturists very important that the multiplicity of works for the destruction of weeds was reduced to the limit).

It is important that the contingent weeds, destroy or suppress one herbicide, was wide. (Preferably using one of the herbicides could be destroyed or suppressed various weeds such as broadleaf weeds, grassy weeds and perennial weeds).

The processing method must be diverse. (Herbicide effect is intensified when the herbicide can be applied in various ways, such as soil treatment, treatment of foliage and other ).

It is important to not prejudiced in any harm to cultivated plants. (On the cultivated fields, where coexist and cultivated plants and weeds, it is desirable to use herbicide selectively destroyed only weeds).

However, all is not yet available herbicides, which could satisfy all of these requirements.

Well-known I-substituted orally (I) represented by the following formula:

O= where each of R and R1is hydrogen, stands or ethyl;

R2is lower alkyl, lower alcohol is anilam, lowest alkoxycarbonyl, lower haloalkoxy, cycloalkyl, cycloalkenyl, lower haloalkylthio, lower alkenyl or lower quinil;

R3is hydrogen or is independently selected from the values of R2;

R4 is hydrogen or is independently selected from the values of R2;

X is hydrogen, carbamoyl or cyano;

Y is zero, one, two, or three.

Also known (2)1-C4-alkyl, C2-C4alkenyl and C3or4-quinil analogue ethers, 3-aelurillus formula

where R1means1-C3-alkyl, C2-C6alkenyl,2-C6-quinil,2-C8-alkoxyalkyl;

R2means halogen or cyano;

R3means hydrogen or halogen;

R4means hydrogen, fluorine or1-C4-alkyl;

R5means1-C4-alkyl or C1-C4-haloalkyl;

R4and R5together signify tri - or tetramethylene;

R6and R7each independently mean C1-C4-alkyl;

m denotes 1 or 2 and

X means 0,0-s(0), 0-C(0)-0 or C(0)-0.

Known connection if and exhibit only weak herbicide to satisfy the above requirements, namely herbicide, which shows selectivity in activity without fear of harm to cultivated plants (i.e. corrupt culture), finds excellent herbicide effect at a low dose for a wide variety of weeds, and also able to show the desired effect, as in tillage, and the processing of the leaves.

In the research it was found that derivatives of uracil, having a halogen-alkyl group in the 6-position and a phenyl group at the 3-position, which has a special Deputy, which are represented by the General formula (I) have activity penetrating translocation (movement) and very high herbicide activity, and compared with conventional herbicide compounds listed brazillia derivatives can be used for treatment or soil or foliage, and have in this quick and highly effective herbicide action even at very low doses against a wide variety of weeds, including perennial weeds, and possess the property of residual effect during the relevant time period. According to the invention offers a herbicide composition containing 0.1 to 90 wt. % uracil derivative as active increditable, represented by the General formula I

(I) in which R1represents trifluoromethyl or pentafluoroethyl;

R2represents a group of the formula

(I-A)or(I-B)where R4represents hydrogen, fluorine or chlorine;

AND2represents a hydrogen: WITH1-C3alkyl, allyl, propargyl, 1-methylpropenyl, cyanomethyl, methoxymethyl, benzyl, o-methylbenzyl, p-methylbenzyl or picolyl;

R6group of the formula:

CH2CO2CH3or

SO2R7where R7- C1-C4the normal alkyl or isotrate, 3-chloropropyl or 2,2,2-triptorelin,

R8is hydrogen, C1-C2-alkyl or methylsulphonyl.

Of these brazilina derivatives represented by the formula (I), preferred are compounds represented below:

O

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R1where D1- represents the group:

-SO2R7< / BR>
Brazillia derivatives included in the composition of the invention are new and can be synthesized using various methods. Hereinafter in the description of examples are given to illustrate these methods.

Herbicide compositions of the invention can be applied to dry poly low doses against, for example, weeds of arable land, such as broadleaf weeds family Selanan Rosaceae such as Solanum nigrum and Dotura shamonium, weeds family Maluaceae such as abutilon theophrasti and Side spinosa, weeds Sonvolvulaceae such as Ipomaca PPPs or Ipomaca purpurea, and Calystegia PPPs, weeds family Amaranthaceal such as Amaranthus lividus and Amaranhthus retroflebvas, Compositae weeds such as Xarthium ponsylvamium abmrosia cortemisaefolie ttelianthus annuus, Golinsoga ei liata, liratum arvense seneria vulgaris Erigeron annuus Bdens pilasa, weeds Cruciferea such as Rorippa indica, Sinapis arvensis u Capsella Bursapastnis, weeds Polygonaceae such as Polygonum Blume and Polygonum comolvulus, weeds family Portulacoceae such as Portulaca oleracea family Chenopodiaceae such as Chemopodium album, Chenopodiumficifolum and Kochias coparia family Coryophyllacece such as Stellaria media, family Sorophularkkki aceae such as Veronica pessica, weeds of the family Commelinaceae such as Commelina commuuis, weeds Zabiatae, such as Lanuumamplea'caule and Lamium purpureum weeds Enphorbia Rosaceae such as Enphorbia sapina and Enphorbia maculata, weeds Rubiaceae such as Galium spurium, Galium opirine and Rubinakane, weeds Violaceae such as Viola arvensis and weeds Leguminisae, such as Sesbania ecaltata and Cassis pbtusifolia; weeds of the family of Graminaceous such as Sorgham bicolos Panicum dichotomi florum, Sorghus halepenge, Echinochloa crus-dalli Digitario adscendens, avenaftia, Eleusine indica Setaria viridis u alopecurus aigualis; weeds Cyperaeous such as Cyperus rotindius and Cyperus esculentus, and weed the rice paddies, family alismatocea kurogamai weeds Serothulariaceae such as Lindencia puriadasia weed family Potenderiaceae such as Monochoria vaginalis, weeds Potomogetenaceae such as Potamogeton distinctus weeds Lythraceae such as Rotalia indica and weeds Gramincae such as Echinoohloa crus-galli. Absolutely wonderful is that brazillia derivatives of the invention do not cause harm such important crops as wheat, corn, barley, soybeans, rice. In particular, insofar as brazillia derivative (1-a) of the invention do not exhibit phytotoxicity and soil, and when processing through the seal into the soil, and high herbicide activity at very low doses against weed Abutilon theophrasti, Xanthum pensylvanium, Ipomoea PPPs, Ipomoea purpurea Calystagia PPPs. Amaranthus retrofflexus, Polyponum Blume. Polygonum convolvulus, Portulaca oleracea, Chenopdium album, Dature stramonium, Ambrosia artemisiaefolia, Bidens pilosa, Side spinose, Sebsania exaltata and Solanum nigrum.

In the compositions of the invention are active brazillia derivatives are mixed with a carrier, for example, with a solid carrier such as clay, talc, bentonite, lacomba earth and white carbon (fine-disperse powder of silicon dioxide), or a liquid carrier such as water, alcohols (isopropanol, butanol, benzyl alcohol, furfuryl alcohol, and others ), aromatic hydrocarbons (toluene, xylene, and others ), ethers (anisole and others ), Katie halogenated hydrocarbons (chlorobenzene, etc. ). If necessary, these may be joined by suitable adjuvants or adjuvants, such as surfactants, emulsifiers, dispersing agents, penetration agents, distribution agents or spreaders, thickeners, antifreeze agents, agents for preventing coagulation, stabilizers and similar connections may be offered for practical use in a variety of finished drug forms, such as liquid formulation, emulsifiable concentrate, wettable powder, dry flowable drug, fluid forms, dusty and granules.

In the herbicide composition of the invention, the amount of the active ingredient is 0.1-90 o'clock mass, and the number herbicide-acceptable carrier or diluent is in the range of 10-99,9 o'clock by weight per 100'clock mass herbicide composition.

More specifically, the preferred amount of the composition (per 100'clock mass herbicide composition) brazilero derived in each preparative form below.

Wettable powder, wt. including :

Uracile manufac - tion according to the invention 5-80 Solid media 10-85 Surfactant 1-10 the Other carries the strong production - tion according to the invention 1-30 carrier Liquid 30-95 Surfactant 5-15 Fluid preparative form, wt. hours : Uracile manufac - tion according to the invention 570 carrier Liquid 565 "Surfactant 512" Other media 530 " (e.g., antifreeze agent, a thickener, etc. )

Granular wettable powder (dry flowable form), wt. h: Uracile derivative according to the invention 2090 Solid media 1060 Surfactant 120 Granules, wt. h: Uracile derivative according to the invention 0,110 Solid media 9099,99 Other media 15

The composition of the invention can be mixed if necessary with other herbicides, various insecticides, fungicides, agents regulating the growth of plants, agents synergies and similar in the course of obtaining or during the application of preparative forms.

As an additional herbicides that can be included in the compositions of the invention, especially in the case of application to soybeans, preferably can be named trifluralin, pendimethalin, alachlor, metolachlor, metribuzin, benuron, chlorimuron ethyl, imazighen, imazethapyr, cenoses, bifenox and clomazone.

P R I m e R a-1. Synthesis of 3-/7-fluoro-3-oxo-4-propargyl-2H-1,4-benzoxazin-6-yl/-1-methyl - 6-trifluoromethyl-2,4/1H, 3H/-pyrimidinedione (compound a-1).

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P R I m e R a-3. Synthesis of 3-/7-fluoro-3-oxo-4-/2-pyridylmethyl/-2H-1,4-benzoxa - Zin-6-yl/-1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione (compound a-3).

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0.20 g of 3-/7-fluoro-3-oxo-2H-1,4-benzoxazin-6-yl/-1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione was added at room temperature to N, N-dimethylformamide solution (5 ml) suspended in it, 0.05 g of sodium hydride (purity: 55% ). After standing for 20 min to the solution was added 0.09 g of the hydrochloride of 2-chloromethylpyridine and the solution was mixed for 4 hours Then the SJ saturated aqueous floristeria and dried over anhydrous sodium sulfate, and then the ethyl acetate was distilled, yielding the crude product. This product was purified using preparative thin-layer chromatography using a mixture of hexane/ethyl acetate (2: 3) as developing solvent, giving 0.09 g of the target compound as pale yellow crystals.

P R I m e R a-4. Synthesis of 3-/7-fluoro-3-oxo-2H-1,4-benzoxazin-6-yl/-1-methyl-6-three - vermeil - 2,4/1H, 3H/-pyrimidinedione (compound a-4).

0,85 g 3-/7-fluoro-3-oxo-2H-1,4-benzoxazin-6-yl/-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione was dissolved in 8.5 ml of N, N-dimethylformamide. Then was added 0.17 g of anhydrous potassium carbonate and 0.15 ml of methyliodide, and the mixed solution was mixed for 4 hours After the reaction was completed, N, N-dimethylformamide was distilled and the residue was extracted with ethyl acetate by adding water. The extract was washed with a saturated aqueous solution of sodium chloride and dried nadaswaram sodium sulfate, and then ethyl acetate was distilled, yielding the crude product. This product was purified using chromatography on a column using chloroform as a developing solvent, giving of 0.53 g of the target compound as pale yellow crystals.

P R I m e R-1. Synthesis of 3-/4-chloro-2-fluoro-5-marks the AI 0.16 g of sodium hydride (purity 55% ) in 5 ml of dimethylformamide is added dropwise at room temperature was added a solution of 1.5 g of 3-/4-chloro-2-fluoro-5-methoxycarbonylaminophenyl/-6-trifluoromethyl - 2,4(1H, 3H)-pyrimidinedione in 10 ml of dimethylformamide. After the evolution of hydrogen had ceased, was added 0,59 g dimethylsilanol acid, and the resulting solution stirred at room temperature for 3 hours, the Reaction mixture was poured into 300 ml of water and extracted twice with ethyl acetate. The extract was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate, and then ethyl acetate was distilled, yielding the crude product. The obtained product was purified using preparative thin-layer chromatography (manifesting solvent: l3), and then using preparative liquid chromatography high resolution (eluent: CHCN) H2O (5: 1), yielding 0.1 g of target compound in the form of a viscous oil.

P R I m e R s-1. Synthesis of 3-/4-chloro-2-fluoro-5-/5-methyl-1,3,4-oxadiazol-2-yl/Fe - Nile/-1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione (compound C-1)-

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K suspension of 0.31 g of sodium hydride (oil, purity: 55% ) in 13 ml of dimethylformamide was added dropwise at 25aboutWith a solution of 2.5 g of 3-/4-chloro-2-fluoro-5-/5-methyl-1,3,4-oxadiazol-2-yl/phenyl/-6-trifluoromethyl - 2,4/1H, 3H/-pyrimidinedione in 20 ml of N, N-dimethylformamide. After the evolution of hydrogen has ceased, until the Oh temperature for 2 h and was extracted with ethyl acetate by adding water. The extract was dried over anhydrous sodium sulfate. The solvent is then distilled, and the residue was purified using preparative liquid chromatography high resolution using a mixture of acetonitrile/water (5: 1) as eluent, giving 0,78 g of target compound.

P R I m e R s-3. Synthesis of 3-/4-chloro-3-ethanolgasoline/-1-methyl-6-trifluoromethyl-2,4/1H, 3H/-pyrimidine-she (compound C-5).

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0.50 g of 3-/3-amino-4-chlorophenyl/-1-methyl-6-trifluoromethyl-2,4/1H, 3H/-pyrimide - it was dissolved in 5 ml of pyridine. To the resulting solution was added 0.16 ml of acanaloniidae dropwise at a temperature not higher than 5aboutWith, and the mixed solution was mixed for 2 hours After the reaction was completed, pyridine was distilled, and the residue was dissolved in ethyl acetate. The solution was washed with water, diluted hydrochloric acid and saturated aqueous sodium chloride and dried over anhydrous sodium sulfate, and then ethyl acetate was distilled, yielding the crude product. The resulting product was filtered diisopropyl ether, giving of 0.37 g of the desired product as light brown crystals.

P R I m e R s-4. Synthesis of 3-/4-chloro-3-N-methyl/ethanolgasoline/-1-me - til-6-trifluoromethyl - ormetal-2,4/1H, 3H/- pyrimidinedione was dissolved in 3 ml of dimethylformamide. To the resulting solution was added 0.17 g of anhydrous potassium carbonate and 0.08 ml of methyl iodide, and the mixed solution is stirred over night at room temperature. After the dimethylformamide was distilled, the residue was dissolved in ethyl acetate. The resulting solution was washed with water and saturated aqueous sodium chloride and dried over anhydrous sodium sulfate. Then the ethyl acetate was distilled, yielding the crude product. The obtained product was purified using preparative thin-layer chromatography (manifesting solvent: hexane: ethyl acetate to 3: 2, giving 0.18 g of target compound as white crystals.

P R I m e R s-5. Synthesis of 3-/4-chloro-2-fluoro-5-bis/methanesulfonyl/phenil/-1-methyl-6 - trifluoromethyl-2,4(1H, 3H/-pyrimidinedione (compound C-10).

To a suspension of 0.05 g of sodium hydride (purity 60% ) and 5 ml of tetrahydrofuran at 0aboutWith added 0.5 g of 3-/4-chloro-2-fluoro-5-methanesulfonylaminoethyl/-1-methyl-6 - trifluoromethyl-2,4(1H, 3H)-pyrimidinedione. Then to the resulting suspension was added dropwise to 0.11 ml methanesulfonanilide. After stirring for 7 h, the reaction mixture was poured into ice water and was extracted with what has uchilsa over anhydrous sodium sulfate. Then the ethyl acetate was distilled, yielding the crude product. The obtained product was washed with diethyl ether, yielding 0.50 g of the desired product as white crystals.

P R I m e R s-7. Synthesis of 3-/4-chloro-2-fluoro-5-isopropylcyclopentadienyl/-1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione (compound C-13). -

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of 0.47 g of the obtained 3-/4-chloro-2-fluoro-5-/N-acetyl/isopropylbenzylamine - nil/1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione was dissolved in 5 ml of tetrahydrofuran. To the resulting solution was added 0.04 g of sodium hydroxide and 0.06 ml of water, and the mixed solution was mixed for 4 hours After the reaction was completed, the reaction mixture was poured into diluted hydrochloric acid and was extracted with ethyl acetate. An ethyl acetate extract layer was washed with water and saturated aqueous sodium chloride and dried over anhydrous sodium sulfate. Then the ethyl acetate was distilled, yielding the crude product. The obtained product was purified using preparative thin-layer chromatography (manifesting solvent: hexane: ethyl acetate = 3: 1, giving 0,29 g of target compound in the form of a colorless viscous oil.

P R I m e R s-9. Synthesis of 3-/2,4-dichloro-5-ethanolgasoline/-1-methyl-6 - trifloromethyl/amino-2,4-dichlorophenyl/-1-methyl-6-triptime - Teal -2,4/1H, 3H/-pyrimidinedione and 0.12 g of hydrocity sodium (93% ), and to the resulting solution were added 2 ml of water. After the mixed solution was mixed for 4 h, it was added diluted hydrochloric acid for acidification of the resulting solution. The reaction mixture was extracted with ethyl acetate. The extract obtained an ethyl acetate layer was washed with water and saturated aqueous solution of chlorethane, and dried over anhydrous sodium sulfate. Then the ethyl acetate was distilled, yielding the crude product. The obtained product was purified using preparative thin-layer chromatography (manifesting solvent hexane: ethyl acetate = 3: 2, giving and 0.46 g of the desired product as white crystals.

P R I m e R s-10.

Synthesis of 3-/5-bis/methanesulfonyl/amino-4-chloro-2-forfinal/-1-methyl-6 - trifluoromethyl-2,4/1H, 3H/-pyrimidinedione (compound C-10).

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To a mixture of 1.00 g of 3-/5-amino-4-chloro-2-forfinal/-1-methyl-6-trifluoromethyl - 2,4/1H, 3H)-pyrimidinedione, 0,63 g of triethylamine and 10 ml of dichloromethane was added to 0.48 g methanesulfonanilide at a temperature of not more than 5aboutC. the resulting mixture was stirred over night. After twice washing the reaction mixture with water, the reaction mixture was filtered by us is, the Lord of the crude product. The resulting product was filtered diisopropyl ether, giving of 1.36 g of the desired product as white crystals.

Examples of specific brazilina derivatives included in compositions of the invention, shown in the table. 1-3.

The following are examples of compositions in the form of ready preparative forms of the invention. In the following formulation all parts are expressed by weight, unless otherwise indicated.

P R I m e R 1 the preparative form. Wettable powder, wt. including :

The compound a-1 infusion embracing of the invention 50 Gilit PFP (kaolin clay type, manufactured by the firm of Jclic industries Co. Co., Ltd. ) 43 Sobol 5050 (anionic surfactant manufactured by Toho chemical Co. Co., Ltd. 2 Rooks 1000 C (anionic surfactant manufactured by Toho chemical Co. Co., Ltd. ) 3 Corplex N 80 (antifreeze) (white coal manufacturers conducted by the firm of Singi pharmaceutical Co. Co., Ltd. ) 2.

P R I m m e R 2 the preparative form. Emulsifiable concentrate, wt. hours : Compound a-1 of invention 3 Xylene 76 Isophorone 15 Sobol 3005 X (mixture of nonionic surfactants and anion - based surfactant, manufactured by Toho chemical Co. Co., Ltd. ) 6

P R I m e R 3 the preparative form. Fluid drug Marianne PAV= manufactured by Toho chemical Co., 0 co., Ltd.) 0.5 to 1% Rhodopol water (thickener, manufactured by Rhone Poulenc 20 ethylene Glycol (antifreeze) 8 Water 28,5

P R I m e R 4 the preparative form. Granular wettable powder (dry flowable preparation), wt. h:

The compound a-1 of the invention 75

Isobar N 1 (anyoneeven produced Kuraray Isoprene chemical Co. Co., Ltd. ) 10 Unilex N (anionic surfactant manufactured by San Kokusaku pulp K. K. ) 5 Corplex # 80 (white carbon, manufactured by Shionogi Pharma - ceutical To. Co., Ltd. ) 10

P R I m e R 5 the preparative form. Wetting the powder, by weight. hours : Compound B-1 of the invention 50 Gilit PFP (kaolin clay type, manufactured by the firm of Jclic ind. To. Co., Ltd. ) 43 Sobol 5050 (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. 2 Rooks 1000 C (anionic surfactant manufactured by Toho chemical Co. Co., Ltd. ) 3 Corplex 80 (antifreeze, white coal, output by firm Shionogi Pharm. Co. Co., Ltd. ) 2

P R I m e R 6 the preparative form. Emulsifiable concentrate, wt. hours : Connection-1 of invention 3 Xylene 76 Isophorone 15 Sobol 3005 X (mixture of nonionic surfactants and anion aqueous surfactant manufactured by Toho chemical Co. Co., Ltd. ) 6

P R I m e R 7 the preparative form. Fluid product, wt. hours : Compound B-1 of the invention 35 Agrisol S-711 (nonionic surfactant, Strait water (gel former; it - tel, produced by firms my Rhone Poulenc) 20 ethylene Glycol (antifreeze) 8 Water 28,5

P R I m e R 8 the preparative form. Granules, wt. hours : Compound B-1 of the invention 0.1 Bentonite 55,0 Talc 44,9

P R I m e R 9 the preparative form. Granular wettable powder (dry flowable preparation), wt. hours : Compound B-1 of the invention 75 Isobar N 1 (anionic surfactant manufactured by Kuraray Isoprene chemical Co. Co., Ltd. ) 10 Unilex N(anionic surfactant manufactured by San Kokusaku pulp K. K. ) 5 Corplex # 80 (white carbon, manufactured by Shionogi Pharm. Co. Co., Ltd. ) 10

P R I m e R 10 the preparative form. Wettable powder, wt. hours : Compound C-1 of the invention 50 Gilit PFP (kaolin clay type, manufactured by the firm of Jclic industries Co. Co., Ltd. ) 43 Sobol 5050 (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. 2 Rooks 1000 C (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. ) 3 Corplex N 80 (antifreeze) (white coal output by firm Shionogi Pharm. Co. Co., Ltd. ) 2

P R I m e R 11 the preparative form. Emulsifiable concentrate, wt. hours : Compound C-1 of invention 3 Xylene 76 Isophorone 15 Sobol 3005 X (mixture of nonionic surfactant and anionic surfactant production by the company Toho chemical Co. Co., Ltd. ) 6

P R I m e R 12 the preparative form. Fluid preparation - tion of surfactants, performance - my company Toho chemical Co. Co., Ltd. ) 0.5 to 1% Rhodopol water (gel former; it - tel made of fir - my Rhone Poulenc) 20 ethylene Glycol (antifreeze) 8 Water 28,5

P R I m e R 13 the preparative form. Granules, wt. hours : Compound C-1 of the present invention 0.1 Bentonite 55,0 Talc 44,9

P R I m e R 14 the preparative form. Granular wettable powder (dry flowable preparation), wt. h: Compound C-1 of the invention 75 Isobar N 1 (anionic surfactant manufactured by Kuraray Isoprene chemical Co. Co., Ltd. ) 10 Unilex N (anionic surfactant manufactured by firms my Dignity Kokusaku pulp K. K. ) 5 Corplex 80 (white carbon, manufactured fir - my Shionogi Pharm. Co. Co., Ltd. ) 10

P R I m e R 15 the preparative form. Wettable powder, wt. hours : Compound C-7 of the invention 50 Gilit PFP (kaolin clay type, manufactured by the firm of Jclic industries Co. Co., Ltd. ) 43 Sobol 5050 (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. 2 Rooks 1000 C (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. ) 3 Corplex 80 (antifreeze, white coal, output by firm Shionogi Pharm. Co. Co., Ltd. ) 2

P R I m e R 16 the preparative form. Emulsifiable concentrate, wt. hours : Compound C-7 of the present invention 3 Xylene 76 Isophorone 15 Sobol 3005 X (mixture of nonionic surfactants and anion - aqueous surfactants, poutinerie C-7 of the invention 35 Agrisol S-711 (nonionic surfactant, produced by firms my Kao Building. ) 8 Rooks 1000 C (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. ) 0,5

1% Rhodopol water (gel former; it - tel, manufactured by Rhone-Poulenc) 20 ethylene Glycol (antifreeze) 8 Water 20,5

P R I m e R 18 preparative forms: Granules, wt. hours : Compound C-7 of the present invention 0.1 Bentonite 55,0 Talc 44,9

P R I m e R 19 the preparative form. Granular wettable powder (dry flowable preparation), wt. hours : Compound C-7 of the invention 75 Isobar N 1 (anion - deficient surfactant, manufactured by Kuraray Isoprene chemical Co. Co., Ltd. ) 10 Unilex N(anionic surfactant manufactured by firms my Dignity Kokusaku pulp K. K. ) 5 Corplex 80 (white carbon, manufactured by Shionogi farm, Co. Co., Ltd. ) 10

P R I m e R 20 the preparative form. Wettable powder, wt. hours : Compound C-11 of the invention 50 Gilit PFP (kaolin clay type, manufactured by the firm of Jclic industries Co. Co., Ltd. ) 43 Sobol 5050 (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. 2 Rooks 1000 C (anionic surfactant manufactured by firms my Toho chemical Co. Co., Ltd. ) 3 Corplex 80 (antifreeze, white coal produced by the company Shionogi Pharm. Co. Co., Ltd. ) 2

P R I m e R 21 the preparative form. Emulsifiable concentrate, wt. h : Link With-11 from the hiccuping, Co. Co., Ltd. ) 6

P R I m e R 22 the preparative form. Fluid product, wt. including :

Connection-11 of the invention 35 Agrisol S-711 (naion - ing surfactant, manufactured by Kao Corp. ) 8 Rooks 1000 C (anionic surfactant manufactured by Toho chemical Co. , Ltd.) 0.5 to 1% Rhodopol water (gel former; it - tel made of fir - my Rhone Poulenc) 20 ethylene Glycol (antifreeze) 8 Water 28,5

P R I m e R 23 the preparative form. Granules, wt. hours : Compound C-11 of the invention 0.1 Bentonite 55,0 Talc 44,9

P R I m e R 24 the preparative form. Granular wettable powder (dry flowable preparation), wt. hours : Compound C-11 of the present invention 75 Isobar N 1 (anionic surfactant manufactured by Kuraray Isoprene chemical Co. Ltd.) 10 Unilex N (anionic surfactant manufactured by San Kokusaku pulp K. K. ) 5 Corplex 80 (white carbon, manufactured by Shionogi Pharm. Co. Co., Ltd. ) 10

For practical use of the described preparative forms in the case of wettable powder, emulsifiable concentrate, flowable product and a granular wettable powder, these forms are diluted in 50-1000 times with water and then applied so that the active ingredient was delivered at a dose of 0.0001 to 10 kg per hectare.

The usefulness of the compositions of the invention will be clear from idee action when tillage.

Sterilizovanny deluvial soil was placed in a plastic box measuring 15 cm x 22 cm x 6 cm, Then the box was sown in a mixture of seeds of barnyard grass Echinochloa crusgalli, Rosicky blood (Digitaria adscendens), annual sedges (Cyperus microiria), black nightshade (Solanum nigrum), galinsoga hairy (Galinsoga ciliate), garesnica Indian (Rorippa indica), rice (Oryzo sativa), maize (Zea mays), wheat (Triticum aestivum), soybean (Glycine max) and cotton (Cossipium herbaceum) and covered by a soil layer of thickness about 1 cm, and then test the herbicide was sprayed uniformly on the soil surface using a small sprayer so that the active ingredient was applied at a predetermined rate. Each test liquid herbicide were prepared by dilution with water formulation obtained according to the relevant examples preparative forms described above. Three weeks after application (spraying) of the test liquid herbicide was tested herbicide action them on these different types of weeds and crops, and were evaluated in accordance with the following standard grading scale. The results are shown in tables 4-8.

Standard grading scale

5: degree of suppression of the growth is more than 90% of

2: the Degree of suppression of the growth of 20-40% .

1: degree of suppression of the growth is 5-20% .

0: the Degree of suppression of the growth is less than 5% .

(almost not effective).

The degree of inhibition of growth was determined by the following formula after measuring the weight of the ground part of the plants in the treated area and weight on the raw site:suppression= / 1 -

P R I m m e R 2 tests: Test for herbicide action in the processing of the leaves.

In a plastic box measuring 15 cm x 22 cm x 6 cm, containing sterilized deluvial soil were inoculated spots seeds of barnyard grass (Echinochloa crus-galli, Rosicky blood (Digitaria adscendens), annual sedges (Cyperus microria), black nightshade (Solanum nigrum), galinsoga hairy (Galinsoga ciliate), garesnica Indian (Rorippa indica), rice (Oryza sativa), maize (Zea mays), wheat (Triticum aestivum), soybean (Glycine max), cotton (Cosspium herbaceum) and sugar beet (Beta vulgaris) and was covered with soil to a thickness of about 1 cm When the plants have grown to the stage of 2-3 leaves, the test liquid herbicide evenly sprayed on the foliage of plants so that the active ingredient was applied with a specified rate of application.

Each test liquid herbicide were prepared using Sannam above, and was sprayed on the entire foliage of the weeds using a small sprayer. Four weeks after spraying, the test liquid herbicide repeated his herbicide effect on these types of weeds and useful plants and were evaluated on the same scale that was used in test example 1. The results are shown in table. 9-13.

P R I m e R and s p s g t I o n 3: Test for herbicide action in the irrigated field.

Alluvial soil were placed in pots Wagner area of 1/5000 ar, and then they poured water for kneading the soil and formation of miniature models, resembling jelly rice field with a layer of water above the soil depth of 2 cm Then these pots were inoculated mixture of seeds of barnyard grass (Echinochloa crus-galli), Monochoria (Monochoria vaginalis), rotary Indian (Rotala indica) and bulrush (Scirpus juncoides). In the soil layer was placed such tubers of perennial sedge (Cyperus serotinus) and arrowhead (Sagittaria pugmaca), and then transplanted the seedlings of rice in stage 2.5 leaves. The pots were placed in a greenhouse with a temperature of 25-30aboutTo ensure normal plant growth. On day 2 after seeding diluted liquid herbicide under test was added in drops on the surface of the water in each of GORS is after applying liquid herbicide was tested herbicide his action figure and these types of weeds and were evaluated on the same scale, as used in test example 1. The results are shown in table. 14.

The underlined symbols in the table indicate the following:

N: barnyard grass (Echinochloa crus-galli)

M: weed blood (Digitaria adscendens)

K: annual sedge (Gyperus microiria)

H: black nightshade (Solanum nigrum)

D: galinsoga hairy (Galinsoga ciliate)

I: gershnik Indian (Rorippa indica)

P: rice (Oryza sativa)

T: corn (Zea mays)

W: wheat (Triticum aestivum)

S: soybean (Glycine max)

C: cotton (Cossipium herbaceum)

B: sugar beet (Beta vulgaris)

As control compounds were used bromacil having the following structure:

(56) U.S. Patent N 4266056, CL 544-311, 1985.

U.S. patent N 4812164, CL 71-92, 1987.

HERBICIDE COMPOSITION containing derivatives of uracil and target additives, characterized in that as a derivative of uracil it contains a compound of General formula

(I)

where R1- trifluoromethyl or pentafluoroethyl;

R2group of General formula

or< / BR>
where R4is hydrogen, fluorine or chlorine;

A2is hydrogen, C1- C3- alkyl, allyl, propargyl, 1-methylpropenyl, cyanomethyl, methoxymethyl, benzyl, o-methylbenzyl, p-methylbenzyl, picolyl;

< / BR>
< / BR>
SCH2CO2
R8is hydrogen, C1- C2-alkyl or methylsulphonyl,

in an amount of 0.1 - 90 wt. % , the rest of the target additives.

 

Same patents:

The invention relates to methods of producing derivatives of 2-anilinopyrimidines or acid additive salts of novel biologically active compounds, which can find application in agriculture

The invention relates to derivatives of 2,4-bis-(pyridine)hintline, which can find application in agriculture for cotton defoliation

The invention relates to chemical means of plant protection specifically to the herbicide agent on the basis of sulfonylurea derivatives and method of weed control using herbicide tools

Fungicidal tool // 2002416

FIELD: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention describes substituted benzoylcyclohexanediones of the general formula (I):

wherein m = 0 or 1; n = 0 or 1; A means a single bond or alkanediyl (alkylene) with 1-4 carbon atoms; R1 means hydrogen atom or unsubstituted alkyl with from 1 to 6 carbon atoms; R2 means methyl; R3 means hydrogen atom, nitro-, cyano-group, halogen atom, alkyl with from 1 to 4 carbon atoms substituted with halogen atom, alkoxy-group with from 1 to 4 carbon atoms or alkyl sulfonyl with from 1 to 4 carbon atoms; R4 means nitro-group, halogen atom, unsubstituted alkyl with from 1 to 4 carbon atoms of that substituted with halogen atom; Z means heterocycle, and herbicide agent based on thereof. Also, invention describes substituted derivatives of benzoic acid of the general formula (III):

wherein values n, A, R3, R4 and Z are given above. These compounds represent the parent substances used for preparing compound of the formula (I). Compounds of the formula (I) elicit high and selective herbicide activity.

EFFECT: valuable properties of compounds.

7 cl, 8 tbl, 7 ex

FIELD: agriculture, in particular herbicide compositions.

SUBSTANCE: invention relates to weed controlling method for tolerant cotton crops using (A) road spectrum herbicides selected from group (A1) glufosinate (salt) and related compounds; (A2) glyphosate (salt) and related compounds; and (B) herbicides selected from group containing diurone, trifluraeline, linuron, and pendimethalin; lactofen, oxyfluoren, bispiribac and salts thereof, pyrithiobac and salts thereof; setoxydim, cyclosidim, and cletodim; wherein components (A) and (B) are used in synergistically effective ratio. Also are described herbicide compositions containing compound from group (A1) or (A2) and herbicide from group (B).

EFFECT: effective controlling of weeds in cotton crops.

9 cl, 12 tbl, 3 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: method involves carrying out a seasonal single treatment of plant leaves with asymmetrical derivative of 4,6-bis-(aryloxy)pyrimidine of the formula: wherein X means chlorine atom (Cl), nitro- or cyano-group. Invention provides enhancing the long-term time of plants protection.

EFFECT: enhanced effectiveness and valuable properties of compounds.

6 cl, 6 tbl

FIELD: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention relates to new derivatives of uracil of the formula [I] eliciting the herbicide effect, herbicide composition based on thereof and a method for suppression of weed growth. In the formula [I] W means oxygen (O), sulfur (S) atom or imino-group; Y means oxygen atom (O) or sulfur atom (S); R1 means (C1-C3)-alkyl or (C1-C3)-halogenalkyl; R2 means (C1-C3)-alkyl; R4 means hydrogen atom (H) or methyl; R5 means (C1-C6)-alkyl, (C1-C6)-halogenalkyl, (C3-C6)-alkenyl, (C3-C6)-halogenalkenyl, (C3-C6)-alkynyl or (C3-C6)-halogenalkynyl; X1 means halogen atom, cyano- or nitro-group; X2 means hydrogen atom (H) or halogen atom; each among X3 and X4 means independently hydrogen atom (H), halogen atom, (C1-C6)-alkyl, (C1-C6)-halogenalkyl, (C3-C6)-alkenyl, (C3-C6)-halogenalkenyl, (C3-C6)-alkynyl, (C3-C6)-halogenalkynyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-alkoxy-, (C1-C6)-halogenalkoxy-, (C1-C6)-alkoxycarbonyl-(C1-C6)-alkoxy- or cyano-group. Also, invention relates to new intermediate substances used for preparing compounds of the formula [I] corresponding to formulae [VII] , [XXXIV] and [XXXIII] wherein in compound of the formula [VII] W means oxygen (O), sulfur (S) atom or imino-group; Y means oxygen (O) or sulfur atom (S); in compounds of formulae [XXXIV] and [XXXIII] W means oxygen atom (O); R17 means oxygen atom (O); R4 means hydrogen atom (H) or methyl. Also, invention relates to methyl- or ethyl-[2-(5-amino-2-chloro-4-fluorophenoxy)phenoxy]acetate not early described in the literature.

EFFECT: valuable herbicide properties of compounds.

23 cl, 17 sch, 9 tbl, 11 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: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention elates to novel derivatives of uracil of the formula [I] possessing herbicide activity, a herbicide composition based on thereof and to a method for control of weeds. In derivatives of uracil of the formula [I] the group Q-R3 represents a substituted group taken among:

wherein a heterocyclic ring can be substituted with at least a substitute of a single species taken among the group involving halogen atom, (C1-C6)-alkyl-(C1-C6)-alkoxy; Y represents oxygen, sulfur atom, imino-group or (C1-C3)-alkylimino-group; R1 represents (C1-C3)-halogenalkyl; R2 represents (C1-C3)-alkyl; R3 represents OR7, SR8 or N(R9)R10; X1 represents halogen atom, cyano-group, thiocarbamoyl or nitro-group; X2 represents hydrogen or halogen atom wherein each among R7, R8 and R10 represents independently carboxy-(C1-C6)-alkyl and other substitutes given in the invention claim; R9 represents hydrogen atom or (C1-C6)-alkyl. Also, invention relates to intermediate compounds used in preparing uracil derivatives.

EFFECT: improved preparing method, valuable properties of compounds.

40 cl, 16 sch, 12 tbl, 65 ex

FIELD: organic chemistry, chemical technology, herbicides, agriculture.

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

and their salt wherein A represents substituted or unsubstituted benzene ring or 5-membered, or 6-membered substituted or unsubstituted heteroaromatic ring taken among the group comprising thienyl, pyrazolyl, imidazolyl, pyridyl wherein optional substitutes are taken among the group consisting of halogen atom, substituted or unsubstituted (C1-C4)-alkyl, unsubstituted or substituted (C1-C4)-alkoxy-group, nitro-group, phenyl, phenoxy-group, benzoyl and (C1-C4)-alkylcarboxylate when any alkyl fragment in the latter indicated substituted is substituted with one or some halogen atoms, (C1-C4)-alkoxy-groups, cyano-group and phenyl; Q represents -O-, -S- or group of the formula: -CXX' wherein X and X' can be similar or different and each represents hydrogen atom, halogen atom, cyano-group, alkyl comprising 1-8 carbon atoms, or the group -ORa, -SRa; or one of X and X' represents hydroxy-group and another has values determine above; Ra means (C1-C8)-alkyl, phenyl; Rb means (C1-C8)-alkyl, phenyl; Y means nitrogen atom or the group CR9; R1 means unsubstituted (C1-C8)-alkyl or that substituted with halogen atom, cyano-group, phenyl or (C1-C4)-alkoxycarbonylamino-group, or it represents phenyl; R2 means hydrogen atom (H), (C1-C4)-alkyl; R3 and R4 can be similar or different and each represents (C1-C4)-alkyl, (C1-C4)-alkoxy-group, halogen atom; R9 means hydrogen atom (H) under condition that when Q represents oxygen atom (O) or -S- then ring A represents 5-membered substituted or unsubstituted heteroaromatic ring and determined above. Compounds of the formula (I) possess the herbicide activity that allows their using for eradication of weeds. Also, invention describes a method for preparing compounds of the formula (I).

EFFECT: improved preparing method, valuable properties of compounds.

9 cl, 5 tbl, 18 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: invention relates to pest controlling agents containing compound of formula I in mixture with active fungicidal material selected from azoxystrobin, tebuconazol, prothioconazol etc., in mass ratio of formula I/active fungicidal material providing marked synergic action.

EFFECT: enhanced assortment of pest controlling agents based on nitromethylene derivatives.

2 cl, 15 tbl, 9 ex

FIELD: agriculture, fungicides.

SUBSTANCE: claimed method includes treatment of contaminated cultural plants or cultivation area thereof with effective amount of composition, containing A) N-sulfonylvaline amide of formula I 1, wherein R1 represents hydrogen or haloprenyl; and R1 represents C1-C4-alkyl, in combination with B) methalaxyl, or fluozinam, or mancoceb, or chlorithalonyl, or strobyluzine, or pyraclostrobine, or acibenzolar-S-methyl, or dimethoform, or fludioxonyl, or cimoxanyl, or imazalyl in synergistically effective amounts. Fungicide composition containing effective combination of A and B in synergistically effective amounts in combination with agriculturally acceptable carrier and optionally with surfactant.

EFFECT: composition of increased fungicidal action due to synergic effect.

8 cl, 12 ex

Herbicidal agent // 2271659

FIELD: organic chemistry, agriculture, herbicides.

SUBSTANCE: invention relates to herbicidal agent containing compound of general formula I wherein X represents residue X1 or X2 and Z, R1 and R2 are as defined in claim of invention, and additional active substance selected from group containing bromoxynil, dicamba, flufenacete, metolachlor, atrazine, pendimethaline, imazetapir, iodosulfuron, nicosulfuron, 2-amino-4-(1-fluoro-1-methyl)-6-(3-phenyl-1-cyclobuthyl-1-propylamino)-1,3,5-triazine and N-[(4,6-dimethoxy-pyrimidine-2-yl)-aminocarbonyl]-2-dimethylamino-carbonyl-5-formyl-benzenesulfonamide. Compound of formula I and additional active substance are taken in mass ratio of 1:20-10:1, respectively.

EFFECT: agent of high herbicidal activity.

6 cl, 15 ex

FIELD: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention relates to new derivatives of uracil of the formula [I] eliciting the herbicide effect, herbicide composition based on thereof and a method for suppression of weed growth. In the formula [I] W means oxygen (O), sulfur (S) atom or imino-group; Y means oxygen atom (O) or sulfur atom (S); R1 means (C1-C3)-alkyl or (C1-C3)-halogenalkyl; R2 means (C1-C3)-alkyl; R4 means hydrogen atom (H) or methyl; R5 means (C1-C6)-alkyl, (C1-C6)-halogenalkyl, (C3-C6)-alkenyl, (C3-C6)-halogenalkenyl, (C3-C6)-alkynyl or (C3-C6)-halogenalkynyl; X1 means halogen atom, cyano- or nitro-group; X2 means hydrogen atom (H) or halogen atom; each among X3 and X4 means independently hydrogen atom (H), halogen atom, (C1-C6)-alkyl, (C1-C6)-halogenalkyl, (C3-C6)-alkenyl, (C3-C6)-halogenalkenyl, (C3-C6)-alkynyl, (C3-C6)-halogenalkynyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-alkoxy-, (C1-C6)-halogenalkoxy-, (C1-C6)-alkoxycarbonyl-(C1-C6)-alkoxy- or cyano-group. Also, invention relates to new intermediate substances used for preparing compounds of the formula [I] corresponding to formulae [VII] , [XXXIV] and [XXXIII] wherein in compound of the formula [VII] W means oxygen (O), sulfur (S) atom or imino-group; Y means oxygen (O) or sulfur atom (S); in compounds of formulae [XXXIV] and [XXXIII] W means oxygen atom (O); R17 means oxygen atom (O); R4 means hydrogen atom (H) or methyl. Also, invention relates to methyl- or ethyl-[2-(5-amino-2-chloro-4-fluorophenoxy)phenoxy]acetate not early described in the literature.

EFFECT: valuable herbicide properties of compounds.

23 cl, 17 sch, 9 tbl, 11 ex

FIELD: organic chemistry, microbiology.

SUBSTANCE: invention relates to new synthetic biologically active derivatives of pyrimidine, namely to 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)imino-1,3-pyrimidine potassium, sodium or ammonium salt of the general formula: wherein X is taken among the group: Na+, K+, NH+4. The claimed substance shows expressed antibacterial activity directed mainly against different fungi, bacteria, protozoan and viruses.

EFFECT: valuable biological properties of compounds.

13 tbl, 13 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel 4-pyrimidinyl-N-acyl-L-phenylalanines of the formula (I)

or their pharmaceutically acceptable salts possessing ability to inhibit binding VCAM-1 with integrin VLA-4 (α4β1) or with cells expressing VLA-4 and useful in preparing medicinal agents used in treatment of, for example, rheumatic arthritis, cerebrospinal sclerosis, intestine inflammation and asthma. In compound of the formula (I) R1 means group of the formula (Y-1): wherein R22 and R23 mean independently hydrogen atom, lower alkyl, lower alkoxy-group, halogen atom or perfluoro-lower alkyl and at least one among R22 and R23 doesn't mean hydrogen atom; R24 means hydrogen atom, lower alkyl, lower alkoxy-group; or R1 means group of the formula (Y-3) that means 3-7-membered cycle of the formula (Y-3): wherein R25 means group of the formula: R26-(CH2)e- wherein R26 means lower alkoxy-group; Q means -(CH2)fN(R27)-, -(CH2)f- wherein R27 means hydrogen atom (H) or lower alkoxycarbonyl, and carbon atoms in cycle are unsubstituted; e means a whole number from 1 to 4; f means a whole number from 1 to 3; R2 means hydrogen atom or lower alkyl; R3 means hydrogen atom or lower alkyl; R4 means hydrogen atom, lower alkyl, lower alkyl substituted with halide; R5 means hydrogen atom or lower alkyl; R6 means hydrogen atom, lower alkyl, lower alkylcarbonyloxy-lower alkyl, or R6 means group of the formula (P-3): wherein R32 means hydrogen atom; R33 means lower alkyl; R34 means lower alkyl wherein R32 means hydrogen atom; R33 means lower alkyl; R34 means lower alkyl; h means a whole number from 0 to 2; g means a whole number from 0 to 2; h + g = 1-3; or R6 means group of the formula (P-4):

wherein R32, g and h have values given above; Q' means oxygen atom (O). Also, invention relates to pharmaceutical compositions.

EFFECT: valuable medicinal properties of compounds and compositions.

37 cl, 8 sch, 3 tbl, 42 ex

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention proposes compound of the formula (1) in free form or as a salt wherein R1, R2, R3, R4 and R5 have values given in the invention claim. The claimed compounds are selective inhibitors of enzyme PDE-5 and show the high selectivity in inhibition of activity of 3',5'-cycloguanosine monophosphate phosphodiesterase being activity of PDE-5 first of all.

EFFECT: valuable biochemical properties of derivatives.

6 cl, 3 tbl, 87 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to compounds of the formula (I): and their salts, to methods for their preparing, compositions containing thereof and their using in medicine, in particular, for prophylaxis or treatment of clinical state wherein a selective agonist of β2-adrenoceptors is prescribed.

EFFECT: valuable medicinal properties of compound and compositions.

32 cl, 4 dwg, 82 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to benzenesulphonamide derivatives of formula I and to their salts applied in agriculture. In formula I

X1 represents hydrogen or halogen; X2 chlorine; X3 represents hydrogen; Y represents group -C(A)B; A represents oxygen; B represents oxygen; R1 represents C1-C6-alkyl, which can be optionally substituted with C1-C6-alkoxyl, C1-C6-alkylcarbonyl, C3-C7-cycloalkyl, phenyl-C1-C4-alkyl; Q represents residue Q21; A8, A9 represent oxygen; R29 represents C1-C6-alkyl; R30, R31 represent hydrogen, C1-C6-halogenalkyl.

EFFECT: elaboration of method for obtaining benzenesulphonamide derivatives of formula I, herbicidal preparation based on them, method of obtaining herbicidally active preparations, method used to fight undesirable plant growth, application as herbicides and to benzenesulphonylisocyanates of formula II.

8 cl, 4 tbl, 6 ex

FIELD: pharmacology.

SUBSTANCE: invention concerns novel compounds of formula (1a) or (1b) or their pharmaceutically acceptable salts with inhibition effect on matrix metalloproteinases (MMP). In formula

or T is absent; G1 and G2 is independently CH or N; A is C1-6alkyl; B is a link; D is a link; E is phenyl substituted by condensed heterocyclic ring in the form of nitrogen-containing ring which can be substituted by carbonyl groups; or substituted 6-membered heteroaryl or bicyclic heteroaryl where second ring in bicyclic system is benzene ring, and heteroaryl is 5-6-membered ring containing 1, 2 or 3 nitrogen heteroatoms, and heteroaryl is substituted by 1, 2 and 3 groups selected out of oxo and C1-6alkyl-; R16 is C1-6alkyl; R18 is halogeno, cyano, nitro, OR16 , OCF3, SR16 or COR16; m is 0 or integer 1 or 2; n is 0.

EFFECT: obtaining compounds and pharmaceutical composition based on them.

13 cl, 18 ex

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