Derivatives arylpropionate having fungicidal activity
(57) Abstract:Usage: as compounds having fungicidal activity. The inventive product is derived arylpropionate f-ly 1, R-C-or 1, Y is C-C dichloroethyl , nitropyridine pyrimidinyl - 2, Si(CHJ, D, D-Ct-C Reagent 1:4 - 3 - (4 - hydroxyphenyl) - 2 - methylpropyl-2.6 - dimethylmorpholine Reagent 2: G-(CH). where G is halogen reaction Conditions: heat. 3 table. Structural formula SN Il About N-CH - CH R - CH R 2 SN (X
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
FIELD: organic chemistry, herbicides.
SUBSTANCE: invention describes a synergetic composition with the effective content of components (A) and (B) wherein (A) means herbicide chosen from the group of compounds of the formula (I): wherein R1, R2, R, X, Y and Z have values given in the invention claim or their salts; (B) means one or some herbicides among the following groups: (B1) selective herbicides with activity in some dicotyledonous cultures against monocotyledonous and dicotyledonous weeds; (B2) selective herbicides with activity in some dicotyledonous cultures against dicotyledonous weeds; (B3) selective herbicides with activity in some dicotyledonous cultures with preferable effect against monocotyledonous weeds. Also, invention describes a method for control against weeds using the proposed composition. Using the combination of proposed herbicides results to the synergetic effect.
EFFECT: valuable herbicide properties of composition.
3 cl, 7 tbl, 2 ex
FIELD: organic chemistry, insecticides.
SUBSTANCE: invention describes dialkylamide derivatives of pyrethroid acids of the general formula (III): wherein R1 and R2 represent organic radicals and each radical represents ethyl, or they both can be bound and in common with nitrogen atom represent piperidide, hexamethyleneimide, morpholide. Represented compounds are used as chemical agents for control of insect-pests in agriculture, veterinary science and cattle breeding.
EFFECT: valuable properties of compounds.
2 dwg, 4 ex
FIELD: organic chemistry, fungicides.
SUBSTANCE: invention relates to composition containing A) one arylamidine derivative of formula I , wherein R1 represents hydrogen; R2 and R3 are the same or different and represent C1-C8-alkyl; R4 represents C1-C8-alkyl; R5 represents C1-C8-alkyl; m = 1; R6 represents phenyl, substituted by the same or different substitutes selected from halogen or halo-(C1-C8)-alkyl; A represents -O-; and B) another known fungicidal agent selected from fluquinconazole and fenpropimorph, wherein mass ratio of (F) and (B) is 0.13<=A/B<=6.0. Also disclosed are method for combating of phytopathogenic fungi of agriculture cultures using effective and non-phytotoxic amount of abovementioned composition, as well as product for simultaneous, separate and alternate or sequential application of A compound and B compound in mass ratio of 0.13<=A/B<=6.0.
EFFECT: fungicidal compositions with improved and stable activity.
7 cl, 1 tbl, 1 ex
SUBSTANCE: herbicidal composition containing an inhibitor of protoporphyrinogenoxydase which is represented by lactophen or flumioxazine and SAR-inductor (an inductor of systematic acquired resistance), represented by salycilic acid, sodium salicylate or 1,2,3-benzothiadiazole-7-carbothionic acid S-methyl ester, as well as method of plant growth control by the composition are described. Method of herbicidal activity intensification of above mentioned inhibitor of protoporphyrinogenoxydase through blending the inhibitor with above mentioned SAR-inductor is described.
EFFECT: increase of composition efficiency.
5 cl, 6 tbl, 1 ex
SUBSTANCE: described is a fungicidal composition, containing (a) pyridylethylbenzamide derivative with general formula and (b) a compound, capable of inhibiting biosynthesis of ergosterol, chosen from tebuconazole, prothioconazole, propiconazole, cyproconazole, difenconazole, hexaconazole, metconazole, epoxyconazole, myclobutanil, triadimenol, fenhexamide, prochloraz, fenpropimorph, spiroxamide, triforine, bitertanol with mass ratio (a)/(b) in the interval from 0.01 to 20, as well as a method of preventive or treatment control of phytopathogenic fungi of agricultural crops using such a composition.
EFFECT: increased effectiveness of composition.
6 cl, 17 tbl, 17 ex
SUBSTANCE: invention relates to agriculture. Low temperature-stable, highly concentrated herbicide preparation contains a mixture of 1-methylheptyl ether of fluroxypyr, a surfactant or a mixture of surfactants and N-alkanoyl morpholine solvent of formula: where R is a C5-C11alkyl group. The preparation contains 430-600 g/l fluroxypyr ester, 100-200 g/l surfactant and 300-560 g/l N-alkanoyl morpholine as a solvent.
EFFECT: invention enables to obtain a preparation which exhibits high stability at low temperature at high concentrations.
2 cl, 2 ex
SUBSTANCE: invention relates to compounds of formula
where X represents S or O, one of X1 and X2 represents CR3' and second represents N or independently CR3', n represents integer number 1, 2 or 3; R1 represents C1-6 halogenalkyl, R2 is selected from halogen and C1-C6-halogenalkyl; R3' represents H, C1-C6-alkyl, halogen, cyanogroup, or phenyl, non-substituted or substituted with halogen, C1-C6-alcoxygroup, C1-C6-halogenalcoxygroup, C1-C6-halogenalkyl group; Z represents halogen, Q radical or group -C(O)-NR5R6; R5 represents H or C1-C4-alkyl, R6 represents H; Q', C1-C6-alkyl, non-substituted or substituted with halogen, cyanogroup, C1-C4-alcoxygroup, C1-C4-alkoxycarbonyl, C2-C4-alkanoyl, aminocarbonyl, N-mono- or N,N-di-C1-C2-alkylaminocarbonyl, C1-C4-alkylthiogroup, group -C(O)NHR7 or radical Q"; or C3-C6-cycloalkyl, substituted with group -C(O)NHR7; or C2-C4-alkinyl; Q, Q' and Q" are such as given in the invention formula; R7 represents C1-C6-alkyl, which is non-substituted or substituted with halogen, cyanogroup, pyridyl; or represents C2-C4-alkinyl. Invention also relates to composition for fighting ectoparasites, containing compound of formula (Ia) or (Ib), and to application of compounds of formula (Ia) or (Ib) for composition production.
EFFECT: compounds of formula (Ia) and (Ib), possessing activity against ectoparasites.
11 cl, 4 tbl, 4 ex
SUBSTANCE: invention relates to biocides. A biocidal composition contains a mixture of N-(2-nitrobutyl)morpholine, 2-ethyl-2-nitro-1,3-dimorpholinopropane and phenoxyethanol.
EFFECT: invention makes it possible to obtain the composition, stable at low temperatures.
7 cl, 7 tbl, 3 ex
SUBSTANCE: invention relates to agriculture. The invention relates to a repellent composition containing as an active ingredient at least one type of a compound selected from a heterocyclic compound of formula (1): and an auxiliary substance, as well as a method of deterring animals using the repellent composition.
EFFECT: disclosed compositions based on said compounds have an odour which induces fear in animals without animals adapting to the odour.
12 cl, 1 tbl, 5 dwg, 6 ex
FIELD: pharmaceutical chemistry, medicine.
SUBSTANCE: invention relates to new compounds of formula I ,
solvates or pharmaceutically acceptable salts having antiarrhythmic activity, including ventrical fibrillation, as well as pharmaceutical compositions containing the same. Compounds of present invention are useful in treatment or prevention of arrhythmia, modulation of ion channel activity, for topic or local anesthesia, etc. In formula I X is direct bond, -C(R6,R14)-Y- and C(R13)=CH-; Y is direct bond, O, S, and C1-C4-alkylene; R13 is hydrogen, C1-C6-alkyl, C3-C8-cycloalkyl, unsubstituted aryl or benzyl; R1 and R2 are independently C3-C8-alkoxyalkyl, C1-C8-hydroxyalkyl and C7-C12-aralkyl; or R1 and R2 together with nitrogen atom directly attached thereto form ring of formula II ,
wherein said ring is formed by nitrogen and 3-9 ring atoms selected independently from carbon, sulfur, nitrogen and oxygen, etc; R3 and R4 are independently attached to cyclohexane ring in 3-, 4-, 5-, or 6-position and represent independently hydrogen, hydroxyl, C1-C6-alkyl and C1-C6-alkoxy; and when R3 and R4 are bound with the same atom of cyclohexane ring they may form together 5- or 6-membered spiroheterocycle ring containing one or two heteroatoms selected from oxygen and sulfur; A is C5-C12-alkyl, C3-C13-carbocyclic ring, or ring structure as defined herein.
EFFECT: new antiarrhythmic drugs.
30 cl, 12 dwg, 34 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to arylsulfonyl derivatives of the formula (I): , wherein Ar means naphthyl or phenyl substituted optionally with halogen atom or (C1-C6)-alkoxy-group; R1 means (C1-C6)-alkyl; R2 means hydrogen atom or (C1-C6)-alkyl, or their pharmaceutically acceptable salts or solvates. Proposed compounds show affinity to HT6 receptors. Also, the claim describes pharmaceutical compositions comprising indicated compounds, their using as therapeutic agents and a method for their preparing. Compounds can be useful in treatment of some disturbances in the central nervous system (CNS).
EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.
12 cl, 1 tbl, 12 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel substituted derivatives of 4-aminocyclohexanol of the general formula (I) being optionally as their physiologically acceptable salts and first of all physiologically compatible acids. In compound of the general formula (I) R1 and R2 mean independently of one another hydrogen atom (H) or (C1-C8)-alkyl that can be saturated or unsaturated but both R1 and R2 can't mean simultaneously H, or residues R1 and R form a ring in common and mean (CH2)3-6; R2 means unsubstituted phenyl or phenyl substituted with halogen atom that is added through saturated or unsaturated, branched or linear (C1-C4)-alkyl group; R4 means heteroaryl chosen from 5-membered heteroaryl wherein heteroatoms are chosen from nitrogen, oxygen or sulfur atoms and each of these atoms is condensed with benzene ring and means unsubstituted or monosubstituted (C1-C8)-alkyl; -CHR6R7, -CHR6-CH2R7, -CHR6-CH2-CH2R7, -CHR6-CH2-CH2-CH2R7 wherein R6 represents H; R7 represents phenyl that can be unsubstituted or mono- either multi-substituted with halogen atoms. Also, invention relates to a method for synthesis of compounds of the formula (I) and a medicinal agent based on thereof. Synthesized compounds can be sued for preparing a medicinal agent designated for treatment of pain being first of all acute, visceral, neuropathic or chronic pain, and to a medicinal agent designated for treatment of diseases mediated by function of ORL1-receptor, for example, such as fear state, epilepsy, cardiovascular diseases.
EFFECT: improved method of synthesis, valuable medicinal properties of compounds and drug.
10 cl, 1 tbl, 21 ex
SUBSTANCE: invention relates to novel compounds of formula or to its pharmaceutically acceptable salts, where n is 0 or 1; R1 represents H or F; R2 represents C1-4alkyl; R7 represents H or C1-4alkyl; and Z represents hydroxyl C1-6alkyl or C1-6alkoxycarbonyl, or 5- or 6-member heteroaromatic ring, which belongs to aromatic rings which have given number of atoms, of which at least one is N, O or S, the remaining being carbon atoms, and which also optionally has methyl substituting group. Invention also relates to pharmaceutical composition, to application of compounds, as well as to method of obtaining formula I compounds.
EFFECT: obtaining novel biologically active compounds, possessing activity of receptor 5-HT2A antagonists.
9 cl, 25 ex
SUBSTANCE: in adamantane amino-derivatives of general formula (1), R=OH, R1=R2=R3=H, R4=C2H5, X=Cl, n=1 (I); R=Br, R1=R2=R3=H, R4=C2H5, X=Br, n=1 (II); R=OH, R1=R2=H, R3+R4=-CH2CH2CH2CH2-, X=Cl, n=1 (III); R=Br, R1=R2=H, R3+R4=-CH2CH2CH2CH2-, X=Br, n=1 (IV); R=OH, R1=R2=CH3, R3=R4=H, X=CI, n=1 (V); R=CH3, R1=-CH2OH, R2=R3=R4=H, X=Cl, n=1 (VI).
EFFECT: higher antiviral activity of derivatives towards influenza virus.
1 cl, 1 tbl, 9 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to the field of organic chemistry, namely to compounds of N-phenyl(pyperazinyl or homopyperazinyl)benzenesulphonamide or benzenesulphonylphenyl(pyperazine or homopyperazine), or to their physiologically acceptable acid addition salts, described by general formulas (I) and (I'), where X is a chemical bond or a group N-R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3alkyl, fluorine, C1-C2alkoxy or fluorinated C1-C2alkoxy; R4 is hydrogen, C1-C4alkyl or C3-C4cycloalkyl-CH2-; R5 is hydrogen, fluorine, chlorine, C1-C2alkyl, C1-C2alkoxy or fluorinated C1-C2alkoxy; R6 is hydrogen and n is 1 or 2. The invention also relates to a pharmaceutical composition based on the compound of formula
EFFECT: novel compounds, modulating activity of the 5HT6 receptor are obtained.
35 cl, 2 tbl, 105 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to compounds of formula where A1 and R1, R2, R3, R4 and R5 are determined in invention formula, which are preferable inhibitors of cathepsin cycteinprotease, in particular cathepsin S or L cycteinprotease, which makes them useful as medications, especially for treatment of diabetes, atherosclerosis, aneurism of abdominal aorta, peripheral arterial disease or diabetic nephropathy.
EFFECT: invention relates to methods of obtaining claimed compounds, thereof-containing pharmaceutical composition and thereof application.
24 cl, 1 tbl, 255 ex
SUBSTANCE: invention relates to a method of producing 1-[2-(2,4-dimethyl-phenylsulphanyl)phenyl]piperazine or its pharmaceutically acceptable salts , , , wherein method involves reaction of a compound of formula II, where X denotes Br or I, with a compound of formula III, where Y is Cl or Br, and R' is hydrogen or a metal ion, and a compound of formula IV, where R is hydrogen or a protective group, in presence of a solvent, base and a palladium catalyst, consisting of a source of palladium and phosphine ligands, at temperature from 50 to 130 C.
EFFECT: technical result is a novel method of producing 1-[2-(2,4-dimethyl-phenylsulphanyl) phenyl] piperazine derivatives with high output and purity, which makes it possible to avoid or reduce formation of impurities.
18 cl, 2 tbl, 4 ex
SUBSTANCE: invention relates to the heterocyclic compound of the formula
and its enantiomer, diastereoisomer and addition salts of the pharmaceutically acceptable bases or acids, where R1 refers to the group of -C(O)CR3R4CR5R6C(O)OH or the group of
n and m refer to 0 or 1; L1 - group C (O) -; -C (O) O- or -S (O)2-; R2 refers to the carbocyclic aromatic group having 6 members, unsubstituted or substituted with one or more substituents, identical or different, selected from the alkoxy group having 1-6 carbon atoms, linear or branched, of halogen, CF3, the cyano-group (-CN), the sulfonylmethyl group (-S (O)2-methyl); the heterocyclic aromatic group with 5 or 6 members containing 1 or 2 heteroatoms, identical or different, selected from nitrogen and sulfur; the polyheterocyclic aromatic group with 9 members, with 3 heteroatoms, identical or different, selected from nitrogen and sulfur; the L2 is - carbocyclic group, wherein the carbocycle refers to the aromatic cycle with 6 members ; or the hydrocarbon group, linear or branched, with 1 to 5 carbon atoms; L2 refers to alkyl, linear or branched, with 1 to 5 carbon atoms; R3, R4, R5 and R6 refer to hydrogen atom; R7, identical or different, refers to alkyl, linear or branched, with 1 to 5 carbon atoms. The invention also relates to the process for preparing a compound of the formula (1) and the pharmaceutical composition based on the compounds of the formula (1).
EFFECT: new heterocyclic compounds are obtained, useful in the treatment of pathologies associated with insulin resistance syndrome.
11 cl, 1 tbl 5 ex
SUBSTANCE: invention relates to a compound of formula (1), as well as to methods for its preparation, and pharmaceutical compositions based thereon.
EFFECT: new compounds have been obtained that can be used for treatment of pathologies associated with insulin resistance syndrome, for example, type 2 diabetes.
8 cl, 1 tbl, 2 ex