N-alkylsubstituted benzo- and (pyrido[2,3-b]thieno)pyrrolo[1,2-a][1,4]diazepin-6-ones - antidotes of herbicide of hormonal action 2,4-dichlorophenoxyacetic acid on sunflower
SUBSTANCE: invention relates to novel synthetic, biologically active chemical substances from series of heterocyclic compounds of formula 1
EFFECT: technical result is synthesis of novel compounds in a series of condensed pyrrolo[1,2-a][1,4]benzodiazepines of formula 1a-d in order to expand range of biologically active substances, obtained synthetically, for use in agriculture as antidotes of herbicide of hormonal action 2,4-D.
1 cl, 3 tbl, 6 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new compounds described by general formulas specified below, in the free form as pharmaceutically acceptable salts possessing anticancer activity and may be applicable in medical practice as a therapeutic agent for treating cancer. The compounds under the present invention are described by one of structure formulas: or wherein Ar represents Ph or 4-NO2-C6H4.
EFFECT: presented compounds enable reducing or eliminating completely tumour cell growth by disturbing cell division at the level of enzyme inhibition.
1 tbl, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel derivatives of diazepane of formula , where A, X, R3, R4, R5, R6, R8, R9, R10, R11, R12, R13, n and m have values, given in description and formula of invention, as well as their physiologically acceptable salts. Said compounds are antagonists of chemokine receptors CCR-2, CCR-5 and/or CCR-3 receptor and can be used in medicine as medications.
EFFECT: obtaining novel diazepane derivatives.
20 cl, 505 ex, 4 tbl
FIELD: organic chemistry, biochemistry, pharmacy.
SUBSTANCE: invention relates to new heterocyclylsulfonyl alkylcarboxylic acids and their derivatives of the general formula (1): or their pharmaceutically acceptable salts, N-oxides or hydrates possessing the inhibitory effect on kinase activity and to the focused library for search of active leader-compounds comprising at least abovementioned compound. In the general formula 91) W represents optionally substituted heterocyclic radical, among them: pyrrole-3-yl, thiophene-2-yl, isooxazole-4-yl, pyrazole-4-yl, imidazole-4-yl, pyridine-3-yl, 1H-2,4-dioxopyrimidine-5-yl, 2,3-dihydro-1H-indole-5-yl, 2,3-dihydro-1H-indole-7-yl, 1,3-dihydro-2-oxoindole-5-yl, 2,3-dioxo-1H-indole-5-yl, 2-oxo-3H-benzoxazole-6-yl, benzothiazole-6-yl, 1H-benzimidazole-5-yl, benzo[1,2,5]oxadiazole-4-yl, benzo[1,2,5]thiadiazole-4-yl, 1,2,3,4-tetrahydroquinoline-6-yl, 3,4-dihydro-2-oxo-1H-quinoline-6-yl, quinoline-8-yl, 1,4-dihydro-2,3-dioxoquinoxaline-6-yl, 3-oxo-4H-benzo[1,4]oxazine-7-yl, 3-oxo-4H-benzo[1,4]thiazine-7-yl, 2,4-dioxo-1H-quinazoline-6-yl, 2,4-dioxo-1,5-dihydrobenzo[b][1,4]diazepine-7-yl or 2,5-dioxo-3,4-dihydrobenzo[b][1,4]diazepine-7-yl; Y represents optionally substituted methylene group; R1 represents chlorine atom, optionally substituted hydroxyl group, optionally substituted amino-group, optionally substituted azaheterocyclyl; n = 1, 2 or 3; or Yn represents carbon atom of optionally substituted (C3-C7)-cycloalkyl or optionally substituted (C4-C7)-heterocyclyl. Also, invention relates to a pharmaceutical composition in form of tablets, capsules or injections placed into pharmaceutically acceptable package.
EFFECT: valuable properties of compounds.
5 cl, 3 sch, 5 tbl, 6 ex
FIELD: organic chemistry, madicine.
SUBSTANCE: tricyclic benzodiazepines of formula I as well as their pharmaceutical acceptable salts, pharmaceutical composition containing the same and methods for hypertension treatment are disclosed. In formula A is -C(O)-; Y is CH2 or CH as olefinic site; X is CH2 or CH as olefinic site S, O or NR3 (R3 is C1-C8-alkyl) with the proviso that when Y is CH, X also is CH; Z is N or CH; R1 is hydrogen, C1-C8-alkyl, C1-C8-alkoxy or halogen; R2 is NR4COAr (R4 is hydrogen; Ar is phenyl optionally substituted with 1-3 substitutes independently selected from C1-C8-alkyl, halogen, hydroxyl, fluorinated C1-C8-alkylthio and another phenyl optionally substituted with substitute selected from C1-C4-alkyl, halogen, and hydroxyl); R5 is hydrogen, C1-C4-alkyl, C1-C4-alkoxy, fluorine, chlorine, hydroxyl or di-(C1-C4)-alkylamino.
EFFECT: improved pharmaceutical composition for hypertension treatment.
12 cl, 5 tbl, 52 ex
FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel anellated carbamoylazaheterocycles of the general formula (1) that possess inhibitory property of kinase activity and eliciting, for example, an anticancer activity. Also, compounds can be used as agonists, antagonists, receptor modulating agents, antiparasitic and antibacterial agents. Also, invention relates to a method for synthesis of compounds of the formula (1), a pharmaceutical composition based on thereof and a focused library for assay of leader-compounds. In compounds of the general formula (1) W represents 6-oxopiperazine, [1,4]-thiazepane, [1,4]-oxazepane or [1,4]-diazepane cycle anellated with at least one optionally substituted and optionally condensed heterocycle or carbocycle Q; Q represents optionally substituted thiophene, optionally substituted pyrrole, optionally substituted imidazole, optionally substituted thiazole, optionally substituted pyrrolidine, optionally substituted indole, optionally substituted benzofuran, optionally substituted pyridine, optionally substituted quinoline, optionally substituted benzene or optionally substituted naphthalene cycle; R1, R2 and R represent independently of each another hydrogen atom, inert substitute, optionally substituted (C1-C6)-alkyl, optionally substituted (C3-C8)-cycloalkyl, optionally substituted phenyl, optionally substituted aryl, optionally substituted heterocyclyl.
EFFECT: improved preparing method, valuable biological and medicinal properties of compounds and pharmaceutical composition.
15 cl, 5 tbl, 6 ex
(I) where R is hydrogen, halogen, lower alkyl or lower alkoxygroup;
And group O or S;
In group-CH2-CH2or СНR1where R1means hydrogen, lower alkyl or hydroxyl;
X is oxygen or the group NH
The Y group of the formula)qwhere R2means lower alkyl, q is 2 or 3, and their salts, in particular physiologically tolerable salts, which possess pharmacological activity, in particular activity antimuskarinovoe act occurs, and therefore can be used to treat diseases of the gastrointestinal tract and respiratory tract
SUBSTANCE: invention relates to agriculture. The composition for protecting wheat and barley from harmful effects of 6-amino-2-(substituted phenyl)-5-substituted-4-pyrimidine carboxylate herbicide of formula wherein Q is C2-C4alkenyl or C1-C4alkoxy; X is H or halogen; Y is H, halogen, C1-C4alkoxy or -NR1R2; Z is halogen, C1-C4alkyl or C1-C4haloalkyl and R1 and R2 are independently H or C1-C4alkyl; or an agriculturally acceptable salt, ester or amide derivative thereof. The composition additionally contains an antidote. The antidote is cloquintocet, cloquintocet-mexyl, fenchlorazole, fenchlorazole-ethyl mefenpyr or mefenpyr-diethyl or a mixture thereof. The weight ratio of the antidote to the 6-amino-2-(substituted phenyl)-5-substituted-4-pyrimidine carboxylate herbicide is in the range of 1:16 to 4:1.
EFFECT: invention reduces damage to wheat and barley caused by the herbicide.
17 cl, 24 tbl
SUBSTANCE: invention relates to agriculture, particularly to weed control. The herbicidal/fungicidal composition contains a component (a) based on a pyridine carboxylic acid of formula (I) and a fungidical component (b) of formula (II) .
EFFECT: composition provides synergetic control of selected weeds.
8 cl, 38 tbl
SUBSTANCE: invention relates to agriculture. To protect vegetating sunflower plants from injuring impact of 2,4-dichlorophenoxyacetic acid they are treated with 2-triphenylmethylthio-4,6-dimethyltriazolo-[1,5-a]pyrimidine in amount 200 g/ha one day after herbicide application.
EFFECT: invention makes it possible to increase sunflower yield.
SUBSTANCE: method of destruction of isomers of organochlorine pesticide of hexachlorocyclohexane is that detoxicant is used as vermicompost from buckwheat husk in a dose of 9 t/ha. Adding of vermicompost from buckwheat husk in the recommended dose reduces the concentration of hexachlorocyclohexane isomers, including the most toxic γ-hexachlorocyclohexane.
EFFECT: environmentally safe, biologically active substrate - vermicompost from buckwheat husk is not only effective detoxifier, but also improver of soil properties that contribute to creation of safe and optimal conditions for sprouting plants.
2 tbl, 3 ex
SUBSTANCE: invention relates to agriculture. Paddy rice sown into water and as seedlings is protected from harmful effects of penoxsulam and its derivative salts, suitable for agricultural purposes, with the application of clomazone directly to the water as an antidote.
EFFECT: invention enables to implement the said purpose of the method.
2 cl, 3 tbl
SUBSTANCE: method implies using Cytoflavinum 10 ml in physiological saline 200 ml twice a day every 12 hours for 3 preoperative days and once intraoperatively. The above therapeutic regimen enables correcting endogenous intoxication effectively and compensating underlying respiratory disorders in the patients suffering colorectal cancer.
EFFECT: reducing rate and intensity of the respiratory disorders with underlying reduced degree of endogenous intoxication in the patients prior to the coming surgical management of colorectal cancer.
SUBSTANCE: invention relates to field of biotechnology, in particular to veterinary liquid external composition for local trasderamal treatment or prevention of parasite infections of animals, in particular, ruminant animals, such as cattle and sheep. Claimed veterinary composition includes effective quantity of clorsulon, macrocyclic lactone, selected from ivermectin or eprinomectin, glycol ether, propyleneglycol dicaprylate/dicaprinate, stearylstearate, palmitate and myristate, as well as stability enhancer, which represents glycerolformal or PEG.
EFFECT: invention makes it possible to obtain veterinary composition, which has increased stability and ensures improved bioavailability of active substances in case of local application.
5 cl, 9 dwg, 15 tbl, 4 ex
SUBSTANCE: invention relates to agriculture. 2-(1N-benzimidazol-2-yl)-5'-nitrobenzoic acid of formula 1 is antidote for protection of sunflower seedlings from negative action of herbicide of 2,4-dichlorophenoxyacetic acid: Interaction of o-phenylenediamine with 2-formyl-5-nitrobenzoic acid in ratio 1:1 in acetic acid at room temperature for 1.5 hour is carried out.
EFFECT: invention makes it possible to reduce temperature mode and reduce reaction time.
2 cl, 4 tbl, 2 ex
SUBSTANCE: invention relates to agriculture. In order to protect vegetative sunflower plants from the damaging effect of 2,4-dichlorophenoxy acetic acid, said plants are treated with benzyl ether (4,6-dimethyltriazolo-[1,5-a]pyrimidyl-2-sulphanyl)-acetic acid of formula I: in amount of 200 g/ha, three days after applying the herbicide.
EFFECT: invention increases sunflower yield.
SUBSTANCE: invention relates to the field of agriculture and land reclamation. The method includes preparation of activated carbon, its application into the soil and embedding at a depth of 1-3 seeding depth. And the granular activated carbon is prepared by fractionation 0.2-0.8 mm with the micropore size of 0.6-0.8 nm and the micropore volume of 0.36-0.50 cm3/g, and then it is applied to the soil at the dose of 100 kg/ha and mixed.
EFFECT: method enables to restore the fertility of soils contaminated with residues of pesticides resistant to degradation.
FIELD: agriculture, insecticides.
SUBSTANCE: invention relates to insecticide covers for seeds that comprise one or some binding substances taken among the group including polymers and copolymers of polyvinyl acetate, methylcellulose, polyvinyl alcohol, vinylidene chloride, acryl, cellulose, polyvinylpyrrolidone and polysaccharide, and insecticide and a filling agent also. A binding agent forms matrix for insecticide and a filling agent. Also, invention relates to a method for control of insect-pests that involve applying a cover on seeds. Also, invention relates to a method for preparing seeds with cover that involves mixing a binding agent, carrier and insecticide, applying a mixture of seed, drying and applying an additional filming cover. Method for protecting the germinating seedlings involves applying the insecticide cover on seeds. Invention provides reducing the phytotoxic effect of insecticide on seeds.
EFFECT: valuable agricultural properties of insecticide cover.
24 cl, 5 tbl, 5 ex