(57) Abstract:Usage: agriculture, composition, intended for combating weeds in crops of fine-grained cereals. The inventive composition comprising derivatives of sulfobetaine f-ly 1, where Q is - CH = CH-, sulphur, R - C1-C3-alkyl, X is methyl, methoxy, in the amount of 0.2 to 80 wt. % of the target additive and the rest. 2 C. p. F.-ly, 5 PL. f-La 1 The invention relates to chemical means of protection of plants, particularly to herbicide compositions on the basis of sulfonylureas.Already know the use of heterocyclic derivatives of sulfonylurea, for example, N-(2-chloro-phenylsulfonyl)-N-(4-methoxy-6-methyl-1,3,5-triazine-2-yl) urea (trade name "clay") and methyl-3-(4-methoxy-6-methyl-1,3,5-triazine-2-yl-carbamoylmethyl)- 2-thiophenecarboxylate (trade name "harmony") as herbicides. However, these compounds do not exhibit high activity against grassy weeds.The aim of the invention is the enhancement of herbicide action.This goal is achieved by the use of compositions containing a compound of formula I where Q represents-CH= CH-, sulfur,
R-C1In composition, we used the following connection.P R I m e R 1. N-(2-Ethylsulfonyl)/1,2-a/pyridine-3-ylsulphonyl)- N-(4,6-dimethoxy-2-pyrimidyl)urea (compound 2).To a suspension of 2-ethylsulfonyl /1,2-a/pyridine-3-sulfonamida (20.5 g) and phenyl-N-(4,6-dimethoxypyrimidine)-2-yl)carbonate (20,0 g) in 250 ml of acetonitrile under ice cooling was added DWI (11,0 g), and the mixture was stirred 3 h at room temperature.Then the mixture was poured into water (2 l), neutralized with hydrochloric acid (to pH 2-3), and the precipitated crystals were collected by filtration, washed with water and dried, resulting in a received 28.6 g (yield of 91.3% ) of target compound as a white crystal.
So pl. 197-199aboutWITH
NMR (DMSO-d6)b: 1,29(so 3H), 3,23 (sq. 2H), 3,95 (C, 6N), 5,96(s, 1H), 7,11-7,31(m, 1H), 7,47-7,81 (m, 2H), of 8.92 (d, 1H), 10,51 (s, 1H) 12,91 (s, 1H).In accordance with the procedure described in example 1 was received connection sulfonylureas, are presented in table. 1 and 2.Derivatives of sulfonylurea of the formula
Derivatives of sulfonylurea of the formula
The compounds of formula 1 can be used in the following formulation.Wettable powders Connection 2 5 wt. % Simple ents are thoroughly mixed and grinded (composition used after appropriate dilution with water)
P R I m e R 3.Emulsifiable concentrate Compound 2 3 wt. % Xylan 75 wt. % Formamide 18 wt. % A simple ester of polyoxyethylene (Nopipol 85TM) 5 wt. %
The ingredients are thoroughly mixed (the song used after dilution with water)
P R I m e R 4 Suspension concentrate. Connection 6 2 wt. % Formaldehyde allyl - phenyl ester polyoxyethylene condensate (hew Calgen E-300TM) 3 wt. % Sulfate phenylphenolate ether of polyoxyethylene L(Agrizol FL-20FATM) 2 wt. % Is a special polymer that contains several substituted hydrogen atoms (Ag rizol FL-GATM) 15 wt. % White black 2 wt. % Ethylene glycol 10 wt. % Water and 66 wt. %
The ingredients were mixed and wet crushed, resulting received a suspended fluid mixture (composition applied after dilution with water). P R I m e R 5. Granules Connection 1 0.2 wt. % Ligninsulfonate sodium 5 wt. % Bentonite to 94.8 wt. %
The ingredient was mixed with water, thoroughly stirred and granulated.P R I m e R 6. Wettable powders. The compound N 2 10 wt. % Tween-20TM20 wt. % White carbon black 40 wt. % Clay 30 wt. %
The ingredients are thoroughly mixed and grinded (composition used after dilution with water).P R and the s 3 wt. % Clay 15 wt. %
The ingredients are thoroughly mixed and crushed (composition used after dilution with water)
P R I m e R 8. Selectivity for wheat (pre-emergence treatment).Pots with a diameter of 10 cm was filled with soil (about 300 g, sterilized by steam) and the corresponding individual pots were planted 20 seeds of weeds (including 10 seeds of white mustard) and 10 wheat seeds, and then covered by soil layer thickness of about 1 cm Then on the soil surface of each pot was sprayed diluted compositions containing compound 1 in an amount up to 1 or 0.25 g on ar (0.01 ha).Each connection (1 or 0.25 g) used in the test series, was dissolved in a solution of acetone (500 ml) containing 2% wt. % . (Tween-20TM(SAS) and diluted with water to 5 l to a final volume.4 weeks after treatment, herbicide and toxic effect sootvetstvuyuschih tested ingredients to the appropriate group of plants was assessed visually by comparing with the control group.The results of the evaluation are presented in table. 4, the experiments were conducted in the greenhouse. The degree of growth inhibition and adverse effects were evaluated according to the following scale (this scale is also used in the annual processing).In separate pots (10 cm in diameter) filled with soil (about 300 g), sterilized by steam), planted 20 seeds of weeds (including 10 seeds of white mustard) and 10 wheat seeds, and covered the top soil layer thickness of about 1 cm Then, when cereal weeds have reached the stage of development of 1-1,5 leaf and broadleaf weeds have reached the stage from 2 to 6 leaves in each pot was left 10 of the same seedlings, and the rest were removed (except that in the case of white mustard, remains 5).When the wheat has reached the stage of 2-3 leaves, each pot was left for 5 seedlings. Then the seedlings in each of the pots were sprayed compositions with test compounds (1), at a dose volume of 1 or 0.25 g on ar.Each connection (1 or 0.25 g) used in the test series, was dissolved in acetone (500 ml) containing 2 wt. % /about Tween-20TM(SAS), and diluted with water to 5 l to a final volume. 4 weeks after treatment, the herbicide and the harmful effects of the respective subjects of the ingredients in the appropriate groups of plants were estimated by a method similar to that described in Experimental example 8.The results are presented in table. 5. Testing was performed in a greenhouse with reg 491/04, 1985.European patent N 238070, C 07 D 491/04, 1987. 1. HERBICIDE COMPOSITION comprising heterocyclic derivative sulfonylureas and target additives, characterized in that as heterocyclic derivative sulfonylureas used as a compound of General formula
< / BR>where Q is-CH= H- , sulfur;
X is methyl, methoxy,
in amount of 0.2 - 80,0 wt. % , special supplements - the rest.2. The composition according to p. 1, characterized in that it is designed for controlling weeds in crops of fine-grained cereals
FIELD: organic chemistry, herbicides, agriculture.
SUBSTANCE: invention describes a synergistic composition of herbicides comprising components (A) and (B) wherein (A) represents herbicide taken among the group of the formula (I):
wherein R1 means (C1-C4)-alkyl; R2 means (C1-C4)-alkyl; R3 means hydrogen atom; X and Y mean (C1-C4)-alkoxy-group; (B) represents one or two herbicides taken among the group of compounds or their acceptable forms: alachlor, metolachlor, acetochlor, dimetenamide, atrazine, cyanasin, metribusin, fluthiamide, nicosulfuron, rimsulfuron, primisulfuron, pendimetalin, sulcotrion, dicamba, mesotrion, isoxachlortol, metosulam, anilofos, fenoxaprop-ethyl, setoxydim, diclofop-methyl, MCPA, bromoxynil, pyridat, clopyralid, iodosulfuron-methyl, ethoxysulfuron, amidosulfuron, gluphosinat-amminium, isopropylammonium-glyphosate, imasetapir wherein components (A) and (B) are taken in the effective doses. Also, invention describes a method for control of weeds by using above indicated herbicide composition. Invention provides the development of the synergistic herbicide composition eliciting high activity.
EFFECT: improved method for control, valuable properties of composition.
6 cl, 26 tbl, 3 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, in particular herbicide compositions.
SUBSTANCE: invention relates to weed controlling method for tolerant grain crops using (A) road spectrum herbicides selected from group (A1) glufosinate (salt) and related compounds; (A2) glyphosate (salt) and related compounds; and (B) one or more herbicides selected from group containing (B1) herbicides selectively effecting in grain crops especially against monocotyledonous weeds effecting on folia and/or soil (residual benefit); or (B2) herbicides selectively effecting in grain crops against monocotyledonous or dicot weeds effecting especially on folia; or (B3) herbicides selectively effecting in grain crops against monocotyledonous or dicot weeds effecting on folia or soil; or (B4) herbicides selectively effecting in grain crops against monocotyledonous or dicot weeds effecting on folia; wherein components (A) and (B) are used in synergic ration. Also are described herbicide compositions containing (A1) ) glufosinate (salt) and related compounds and herbicide from group (B); as well as herbicide compositions containing(A2) glyphosate (salt) and related compounds and herbicide from group (B); wherein components (A) and (B) are used in synergically effective ration.
EFFECT: effective controlling of weeds in grain crops.
6 cl, 70 tbl, 3 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: agriculture, in particular method for controlling of weeds.
SUBSTANCE: claimed method for controlling of weeds in tolerant maize cultures includes application of composition comprising (A) road spectrum herbicide from group (A1) glufosinate (salt) and analogs, (A2) glyfosate (salt) and analogs; (B) one or more herbicides from group (B1) cyanazin, alachlor, nicosulfurone, rimsulfurone, sulkotrion, mesotrion, and penthoxamid; (B2) pendimethalyne, methosulam, isoxaflutol, metribuzin, chloransulam, flumetsulam, linuron, florasulam, and isoxachlorotol; and (B3) bromoxinyl, chlorpyralid, tifensulfuron, MCPA (2-methyl-4-chlorophenoxyacetic acid), halosulfuron, and sulfosulfuron, wherein (A) and (B) components are in synergic effective ration. Also disclosed are herbicidal compositions including compound from group (A1) or )F2) and herbicide from group (B).
EFFECT: effective controlling of weeds in tolerant maize cultures.
6 cl, 55 tbl, 3 ex
FIELD: organic chemistry, agriculture.
SUBSTANCE: invention relates to new substituted thienyl(amino)sulfonylureas of formula I ,
wherein A represents nitrogen or methane; Q represents direct bond or imino; R1 represents fluorine, chlorine, bromine, unsubstituted C1-C4-alkyl, C1-C4-alkoxyl optionally substituted with halogen, unsubstituted C1-C4-alkylthio, or di(C1-C4-alkyl)amino; R2 represents hydrogen or C1-C4-alkyl. Compounds of present invention are useful as herbicide agents.
EFFECT: new compounds with herbicide activity.
5 cl, 11 tbl, 5 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: agriculture, herbicides.
SUBSTANCE: invention relates to herbicide composition based on derivative of sulfonylurea that comprises non-ionogenic surface-active substance, lignosulfonates as anion-active surface-active substance and highly dispersed amorphous silica as a carrier. Composition comprises chlorsulfuron as derivative of sulfonylurea and triethanolamine or diethanolamine additionally, and potassium dihydrogen phosphate as a stabilizing agent in the following ratio of components, wt.-%: chlorsulfuron, 18-22; non-ionogenic surface-active substance, 3-5; potassium dihydrogen phosphate, 9-12; triethanolamine or diethanolamine, 9-11; lignosulfonates, 3-10, and highly dispersed amorphous silica, the balance. Method involves mixing components in indicated ratios by steps for 3 stages. At the 1-st stage triethanolamine or diethanolamine is applied on surface of highly dispersed amorphous silica, at the 2-d stage - chlorsulfuron, and at 3-d stage - potassium dihydrogen phosphate, lignosulfonates and non-ionogenic surface-active substance. After keeping for 24 h at the room temperature mixing products from all three stages are combined. Invention provides enhancing stability of chlorsulfuron and biological activity of preparation based on thereof. Invention is designated for applying in agriculture.
EFFECT: valuable properties of herbicide composition.
4 cl, 2 tbl, 9 ex
FIELD: agriculture, in particular chemical agents for plant protection.
SUBSTANCE: sulfonylaminourea and phenoxyacetic acid derivatives-based herbicidal composition contains nonionic surfactant, anion-active surfactant sulfonol, kaolin as carrier, and carbon white. As sulfonylaminourea and phenoxyacetic acid derivatives it contains 3-(6-methyl-4-methoxy-1,3,5-triazinyl-2-)-1-(2-chlorophenylsulphonyl)urea and 2-methyl-4-chlorophenoxyacetic acid sodium salt, respectively. Additionally composition contains triethanolamine or diethanolamine, disubstituted potassium phosphate as stabilizer in the component ratio of (mass %): 2-methyl-4-chlorophenoxyacetic acid sodium salt 55-72; 3-(6-methyl-4-methoxy-1,3,5-triazinyl-2-)-1-(2-chlorophenylsulphonyl)urea 0.3-0.4; nonionnic surfactant 0.05-0.15; sulfonol 0.05-0.15; triethanolamine or diethanolamine 0.15-0.2; carbon white 0.37-1.5; disubstituted potassium phosphate 1.0-2.0; and balance: kaolin. Composition components are separately applied on carrier surface. More specifically triethanolamine or diethanolamine is separately mixed with kaolin; 3-(6-methyl-4-methoxy-1,3,5-triazinyl-2-)-1-(2-chlorophenylsulphonyl)urea, and carbon white are separately mixed with kaolin; disubstituted potassium phosphate, nonionic surfactant, and sulfonol are separately mixed with kaolin; and 2-methyl-4-chlorophenoxyacetic acid sodium salt also is separately mixed with kaolin. Mixtures are conditioned for 24 h at room temperature and then are blended to provide mentioned above component ratio in product.
EFFECT: herbicidal composition of increased activity and deferred hydrolysis in wetted powder.
3 cl, 6 ex, 2 tbl
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, chemical technology, medicine, pharmacy.
SUBSTANCE: invention relates to new derivatives of piperazinylalkylthiopyrimidine of the formula (I): wherein R1 represents hydrogen atom, (C1-C4)-alkyl, (C1-C4)-alkanoyl or di-(C1-C4-alkyl)-amino-(C1-C4-alkyl); R2 means hydrogen atom or benzyl substituted with 1-3 substitutes taken among the group consisting of (C1-C4)-alkyl, (C1-C4)-alkoxy-group, di-(C1-C4-alkyl)-amino-group, hydroxyl group and halogen atom; n = 2, 3 or 4, and to its pharmaceutically acceptable acid addition salt. Also, invention describes a method for preparing compounds and pharmaceutical composition based on thereof. Compounds are useful for treatment of diseases arising as result of the central nervous system injury.
EFFECT: improved preparing method, valuable medicinal properties of compounds.
14 cl, 3 tbl, 26 ex
FIELD: organic chemistry, heterocyclic compounds, medicine, pharmacy.
SUBSTANCE: invention relates to nitrogen-containing heterocyclic derivatives of the formula (I): A-B-D-E (I) wherein A means 5- or 6-membered heteroaryl comprising one or two nitrogen atoms in ring; B means ethenylene; D mean phenylene; E means group -N(COR)-SO2-G wherein G means phenyl; R means 5- or 6-membered heteroaryl or heteroarylmethyl comprising one or two nitrogen atoms in ring, or group -(CH2)n-N(R5)R6 wherein n means a whole number from 1 to 5; R5 and R6 are similar or different and mean: hydrogen atom, (C1-C6)-alkyl, hydroxyalkyl, aminoalkyl; or R5 and R6 in common with nitrogen atom can form 5-7-membered cyclic amino-group -N(R5)R6 that can comprise, except for nitrogen atom, also oxygen, sulfur or nitrogen atom as a component forming the ring, or their N-oxides. Compounds of the formula (I) elicit anticancer activity and can be used in medicine.
EFFECT: valuable medicinal properties of compounds.
10 cl, 1 tbl, 24 ex
FIELD: organic chemistry, biochemistry, pharmacy.
SUBSTANCE: invention relates to new compounds of the formula (I):
eliciting inhibitory activity with respect to metalloproteinases and wherein R1 means phenoxy-group wherein phenyl residue can be substituted with one or some halogen atoms, hydroxy-, (C1-C6)-alkoxy-group, (C1-C6)-alkyl, cyano- or nitro-group; R2 means pyrimidine, pyrazine or its N-oxide or phenyl substituted with -SO2NR3R4 wherein R3 and R4 can be similar or different and mean hydrogen atom, direct-chain or branch-chain (C1-C6)-alkyl that can be substituted once or some times with the group OH, N(CH3)2, or it can be broken by oxygen atom, or it represents COR5 wherein R5 means (C1-C)-alkyl group that can be substituted with NH2. Also, invention relates to a pharmaceutical composition comprising above said compounds.
EFFECT: valuable biochemical properties of compounds and composition.
5 cl, 1 sch, 1 tbl, 10 ex
FIELD: organic chemistry, pharmaceutical composition.
SUBSTANCE: new isoindoline-1-on-glucokinase activators of general formula I , as well as pharmaceutically acceptable salts or N-oxide thereof are disclosed. In formula A is phenyl optionally substituted with one or two halogen or one (law alkyl)sulfonyl group, or nitro group; R1 is C3-C9cycloalkyl; R2 is optionally monosubstituted five- or six-membered heterocyclic ring bonded via carbon atom in cycle to amino group, wherein five- or six-membered heteroaromatic ring contains one or two heteroatoms selected form sulfur, oxygen or nitrogen, one of which is nitrogen atom adjacent to carbon atom bonded to said amino group; said cycle is monocyclic or condensed with phenyl via two carbon atoms in cycle; said monosubstituted with halogen or law alkyl heteroaromatic ring has monosubstituted carbon atom in cycle which in not adjacent to carbon atom bonded to amino group; * is asymmetric carbon atom. Claimed compounds have glucokinase inhibitor activity and useful in pharmaceutical composition for treatment of type II diabetes.
EFFECT: new isoindoline-1-on-glucokinase activators useful in treatment of type II diabetes.
23 cl, 3 dwg, 43 ex
FIELD: organic chemistry, medicine, hormones, pharmacy.
SUBSTANCE: invention relates to new biologically active compounds that act as agonists of peptide hormone vasopressin. Invention describes the compound of the general formula (1) or its pharmaceutically acceptable salt wherein V represents a covalent bond or NH; X is taken among CH2, oxygen atom (O) and N-alkyl; Z represents sulfur atom (S) or -CH=CH-; R1 and R2 are taken independently among hydrogen (H), fluorine (F), chlorine (Cl), bromine (Br) atom and alkyl; R3 is taken among hydroxyl group (OH), O-alkyl and NR4R5 wherein each R4 and R5 represents independently hydrogen atom (H) or alkyl, or both represent -(CH2)q-; p = 0, 1, 2, 3 or 4; q = 4 or 5. Also, invention describes a pharmaceutical composition eliciting agonistic activity with respect to V2-receptors, a method for treatment of enuresis, nicturia and diabetes insipidus, method for control of enuresis and a method for treatment of enuresis and a method for treatment of diseases associated with damage in blood coagulability. Invention provides preparing new compounds eliciting useful biological properties.
EFFECT: valuable medicinal properties of compounds.
17 cl, 31 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new compound of the formula (I) or its pharmaceutically acceptable salt or solvate wherein X represents CH or nitrogen atom (N); Z represents CH; R1 represents hydrogen atom; R2 and R3 can be similar or different and represent (C1-C6)-alkoxy-group that is optionally substituted with halogen atom, hydroxyl, (C1-C4)-alkoxycarbonyl, amino-group wherein one or two hydrogen atom are optionally replaced for (C1-C4)-alkyl that is optionally substituted with hydroxyl or (C1-C4)-alkoxy-group, the group R12R13N-C(=O)-O- wherein R12 and R13 can be similar or different and represent hydrogen atom or (C1-C4)-alkyl substituted optionally with (C1-C4)-alkoxy-group or the group R14-(S)m- wherein R14 represents phenyl or saturated or unsaturated 5-7-membered heterocyclic group substituted optionally with (C1-C4)-alkyl; m = 0 or 1; R4 represents hydrogen atom; R5, R6, R7 and R8 can be similar or different and represent hydrogen atom, halogen atom, (C1-C4)-alkyl, (C1-C4)-alkoxy-group or nitro-group under condition that R5, R6, R7 and R don't represent hydrogen atom simultaneously; R9 represents hydrogen atom, (C1-C6)-alkyl or (C1-C4)-alkylcarbonyl wherein alkyl fragment of indicated (C1-C6)-alkyl or (C1-C4)-alkylcarbonyl is optionally substituted with (C1-C4)-alkoxy-group; R10 represents hydrogen atom or (C1-C6)-alkyl; R11 represents (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-alkynyl (wherein each (C1-C6)-alkyl, (C2-C6)-alkenyl and (C2-C6)-alkynyl is substituted optionally with halogen atom or (C1-C6)-alkoxy-group), or R15-(CH2)n- wherein n is a whole number from 0 to 3; R15 represents naphthyl or 6-membered saturated or unsaturated carbocyclic or saturated or unsaturated 5-7-membered heterocyclic group that are substituted optionally with halogen atom, (C1-C6)-alkyl or (C1-C6)-alkoxy-group. Also, invention relates to variants of compounds of the formula (I). Compounds elicit antitumor activity and don't effect on cytomorphosis. Also, invention relates to pharmaceutical composition based on above described compounds, to a method for treatment of such diseases as malignant tumor, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and to a method for inhibition of vascular vessels angiogenesis.
EFFECT: valuable medicinal properties of compounds and composition.
22 cl, 4 tbl, 186 ex
FIELD: organic chemistry, insecticides, chemical technology.
SUBSTANCE: invention describes derivative of 1-aryl-3-cyano-5-heteroarylalkylaminopyrazole of the general formula (1): wherein A means: (A-1) , (A-2) , (A-3) and (A-4) and wherein X represents C-halogen; R1 represents (C1-C4)-alkyl group or halogen-(C1-C4)-alkyl group; A represents any group among (A-1) - (A-4) wherein R4 represents hydrogen atom or (C1-C4)-alkyl group; n = 0, 1 or 2 under condition that R1 represents halogen-(C1-C4)-alkyl group with exception for perhalogenalkyl group when A represents (A-1) and n = 0, and that n doesn't equal 0 when A represents (A-4). Also, invention describes derivative of pyrazole of the formula (2): wherein A means: (A-1) and Y means: (Y-1) , (Y-2) and (Y-3) wherein X, R2, R3 and R4 have values given above; R5 represents hydrogen atom; A represents (A-1); Y means any group among (Y-1) - (Y-3); Z represents halogen atom that are intermediate compounds used for synthesis of the compound (1). Invention describes methods for preparing compounds of the formula (1) and (2) and insecticide comprising compound of the formula (1) as an active component. Insecticide shows high systemic activity, high safety and reduced harmful effect on environment in vicinity areas of its applying.
EFFECT: improved methods for preparing, valuable insecticide properties of compound.
11 cl, 9 tbl, 19 ex