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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 44549. Отображено 100.
12-01-2012 дата публикации

Pest controlling composition

Номер: US20120010251A1
Принадлежит: Sumitomo Chemical Co Ltd

The present invention provides a pest controlling composition comprising, as active ingredients, an amide compound of the formula (I) and a pyrethroid compound; and so on.

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26-01-2012 дата публикации

Platinum (ii) tetradentate oncn complexes for organic light-emitting diode applications

Номер: US20120018711A1
Принадлежит: University of Hong Kong HKU

Described are novel platinum (II) containing organometallic materials. These materials show green to orange emissions with high emission quantum efficiencies. Using the materials as emitting materials; pure green emitting organic light-emitting diodes can be fabricated. Since the novel platinum (II) containing organometallic materials are soluble in common solvents, solution process methods such as spin coating and printing can be used for device fabrication.

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26-01-2012 дата публикации

Method for producing 2,2 difluoroethylamine derivatives by imine hydrogenation

Номер: US20120022264A1
Автор: Norbert Lui, Stefan Antons
Принадлежит: Bayer CropScience AG

Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are hydrogenated to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A, R 1 and R 2 radicals are each as defined in the description:

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09-02-2012 дата публикации

Pest control composition

Номер: US20120035218A1
Автор: Kaori Ikari
Принадлежит: Sumitomo Chemical Co Ltd

[Object] A composition having an excellent control activity on pests is provided. [Means of Achievement] A pest control composition comprising (i) a hydrazide compound shown by the following formula (1) [wherein G, M, Q 1 , Q 2 , Q 3 , Q 4 , R 2 , R 4 , R 5 , R 6 , and m have the meanings listed in the specification, and (ii) pyriproxyfen. A pest control method comprising a step of applying effective amounts of (i) a hydrazide compound shown by the following formula (1) and (ii) pyriproxyfen to pests or pest habitats. [Selected Drawing] None

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16-02-2012 дата публикации

Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs

Номер: US20120040995A1
Принадлежит: University of Illinois

Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.

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15-03-2012 дата публикации

Insect repellent composition

Номер: US20120065229A1
Автор: Marc Esculier
Принадлежит: Dakem SA

The present invention relates to an insect repellent composition containing the following active insect-repellent material in a physiologically acceptable medium: at least 1-methylpropyl(2-(2-hydroxyethyl)piperidine-1-carboxylate, said active material being used with at least one copolymer of vinylpyrrolidone and of a linear alkyl, having at least 16 carbon atoms, as a film-forming agent. The invention also relates to an insect-repelling method using said composition.

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12-04-2012 дата публикации

Combined use of two insecticides

Номер: US20120087987A1
Принадлежит: ECOLAB USA INC

The present disclosure relates to the combined use of two pesticides. A first pesticide composition provides an initial contact kill, and may form a barrier when applied to greasy surfaces. A second pesticide composition provides residual pesticidal activity on the surface. Methods of making and using the pesticide compositions are also provided.

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17-05-2012 дата публикации

Pesticide compositions including polymeric adjuvants

Номер: US20120122687A1
Автор: John Larry Sanders
Принадлежит: SPECIALTY FERTILIZER PRODUCTS LLC

Pesticidal compositions of improved effectiveness are provided, including a pesticide (e.g., an insecticide or herbicide) together with a copolymer adjuvant or additive selected from the group consisting of acid or salt copolymers containing individual quantities of maleic and itaconic moieties. The compositions of the invention provide multiple-fold increases in effectiveness, as compared with an equal amount of the pesticide in the absence of the copolymer.

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14-06-2012 дата публикации

Multifunctional linkers and methods for the use thereof

Номер: US20120149653A1
Принадлежит: RGo Bioscience LLC

In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.

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21-06-2012 дата публикации

Microcapsule and production method thereof

Номер: US20120156303A1
Автор: Mayuko Ozawa, Naoki Tsuda
Принадлежит: Sumitomo Chemical Co Ltd

A microcapsule in which a liquid droplet is coated with a resin, wherein in the droplet, a pesticidally active solid ingredient is suspended in a compound of formula (I), wherein R represents a C1-C5 alkyl group, is useful as a formulation of a pesticidally active solid ingredient.

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26-07-2012 дата публикации

Process for the preparation of 4-amino-3-chloro-5-fluoro-6-(substituted) picolinates

Номер: US20120190858A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, reaction with hydrazine, halogenation, hydrolysis and esterification, and transition metal assisted coupling.

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26-07-2012 дата публикации

Process for the preparation of 4-amino-5-fluoro-3-halo-6-(substituted)picolinates

Номер: US20120190860A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinates by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation and transition metal assisted coupling.

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13-09-2012 дата публикации

Pharmaceutical, dietary supplement, and food grade salts of anatabine

Номер: US20120232115A1
Принадлежит: Rock Creek Pharmaceuticals Inc

Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.

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11-10-2012 дата публикации

Stabilized polymeric thiol reagents

Номер: US20120258985A1
Принадлежит: Nektar Therapeutics

Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A] x , where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp 3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.

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01-11-2012 дата публикации

Insecticidal Compositions Suitable for Use in Preparation of Insecticidal Granular Fertilizer and Insecticidal Formulations

Номер: US20120277103A1
Принадлежит: FMC Corp, Scotts Co LLC

Insecticidal compositions suitable for use in preparation of insecticidal granular fertilizer and insecticidal formulations comprising a pyrethroid and a glycol present in a concentration of from 40.0% by weight to 99.0% by weight based upon the total weight of all components in the composition is disclosed.

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08-11-2012 дата публикации

Method for synthesizing bio-based pyridine and picolines

Номер: US20120283446A1
Принадлежит: Arkema France SA

The present invention relates to a method for synthesizing bio-based pyridine and picolines, said method including at least the following steps: a first step involving subjecting a glycerol filler, created from the methanolysis of vegetable oils or animal fats, to a dehydration reaction leading to acrolein; a second step involving partial condensation of the effluent from the first step so as to separate a water-rich flow as well as an acrolein-rich flow; and a third step involving reacting the acrolein from the preceding step with acetaldehyde in the presence of ammonia so as to obtain, by means of a condensation reaction, the biobased pyridine and picolines.

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29-11-2012 дата публикации

Herbicidal mixtures

Номер: US20120302441A1
Принадлежит: BASF SE

A synergistic herbicidal mixture comprising A) picolinafen; or one of its environmentally compatible salts; and B) a synergistically effective amount of at least a sulfonylurea of formula II wherein the variables A, B, X and R 1 to R 3 have the meanings given in the specification; and, if desired, C) at least a safener. Compositions comprising these mixtures, processes for the preparation of these compositions and their use for controlling undesired plants.

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13-12-2012 дата публикации

Metal complex, and adsorbent, occlusion material and separator material made from same

Номер: US20120312164A1
Принадлежит: Kuraray Co Ltd

This invention provides a metal complex having a gas adsorption capability, a gas storing capability, and a gas separation capability. The present invention attained the above object by a metal complex comprising: a dicarboxylic acid compound (I) represented by the following General Formula (I), wherein R 1 , R 2 , R 3 , and R 4 are as defined in the specification; at least one metal ion selected from ions of a metal belonging to Group 2 and Groups 7 to 12 of the periodic table; and an organic ligand capable of bidentate binding to the metal ion, the organic ligand belonging to the D ∞h point group, having a longitudinal length of not less than 8.0 Å and less than 16.0 Å, and having 2 to 7 heteroatoms.

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03-01-2013 дата публикации

3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinates and their use as herbicides

Номер: US20130005574A1

3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.

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17-01-2013 дата публикации

Deuterated pirfenidone

Номер: US20130018193A1
Автор: Julie F. Liu, Yong Dong
Принадлежит: Concert Pharmaceuticals Inc

This invention relates to novel substituted pyridinones, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a TNF (tumor necrosis factor)-alpha production inhibitor/TGF (transforming growth factor)-beta inhibitor.

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07-02-2013 дата публикации

Process for Preparing Form A of Atazanavir Sulfate

Номер: US20130035493A1
Автор: Ai-Hua KAO, Chia-Ying Lee
Принадлежит: Scinopharm Taiwan Ltd

A process of making Form A of atazanavir sulfate comprises: a) mixing atazanavir free base with a solvent selected from the group consisting of methanol (MeOH), ethanol (EtOH), isopropanol (IPA), N-methylprrolidone (NMP) and combinations thereof; b) reacting sulfuric acid with the atazanavir free base in the mixture formed in step a) to form a reaction solution comprising atazanavir sulfate; c) mixing an antisolvent with the reaction solution; d) seeding the mixture formed in step c) with an effective amount of Form A of atazanavir sulfate to form a seeded mixture comprising Form A of atazanavir sulfate; and e) isolating Form A of atazanavir sulfate in solid form from the seeded mixture; wherein the antisolvent is selected from the group consisting of methyl tert-butyl ether (MTBE), ethyl acetate (EtOAc), acetonitrile (MeCN), isopropyl acetate (IPAc), cyclohexane, and combinations thereof. In one alternative, step c) may be performed before step b). In another alternative, step d) may be carried out concurrent with or prior to step c).

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14-03-2013 дата публикации

Novel amides as fungicides

Номер: US20130065922A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of the general formula (I), wherein the substituents are as defined in claim 1 , are useful as fungicides.

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21-03-2013 дата публикации

PESTICIDAL COMPOSITIONS

Номер: US20130072382A1
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula I”): 3. A molecule according to wherein(a) X is CR8;(b) R1 is H;(c) R2 is H;(d) R3 is H;{'sub': 1', '3, '(e) R4 is Cor CH;'}{'sub': 1', '6, '(f) R5 is H or unsubstituted C-Calkyl;'}(g) R6 is O;{'sub': 1', '6', 'n', '1', '6', '1', '6', 'n', '1', '6', '1', '6', '1', '6, '(h) R7 is (unsubstituted C-Calkyl)S(O)(unsubstituted C-Calkyl), (unsubstituted C-Calkyl)S(O)(unsubstituted C-Calkenyl), O(unsubstituted C-Calkyl), (C-Calkyl);'}(i) R8 is H or F; and(k) n is 0, 1, or 2.4. A molecule according to or in the form of a pesticidally acceptable acid addition salt claim 2 , salt derivative claim 2 , or solvate.5. A molecule according to or having at least one H.6. A molecule according to or having at least one C.7. A molecule according to or that is a resolved stereoisomer.8. A composition comprising a molecule according to or and at least one member of the Insecticide Group claim 2 , Acaricide Group claim 2 , Nematicide Group claim 2 , Fungicide Group claim 2 , or Herbicide Group.9. A composition comprising a molecule according to or and at least one biopesticide.10. A composition comprising a molecule according to or and at least one of the following compounds:(a) 3-(4-chloro-2,6-dimethylphenyl)-4-hydroxy-8-oxa-1-azaspiro[4,5]dec-3-en-2-one;(b) 3-(4′-chloro-2,4-dimethyl[1,1′-biphenyl]-3-yl)-4-hydroxy-8-oxa-1-azaspiro[4,5]dec-3-en-2-one;(c) 4-[[(6-chloro-3-pyridinyl)methyl]methylamino]-2(5H)-furanone;(d) 4-[[(6-chloro-3-pyridinyl)methyl]cyclopropylamino]-2(5H)-furanone;(e) 3-chloro-N2-[(1S)-1-methyl-2-(methylsulfonyl)ethyl]-N1-[2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]-1,2-benzenedicarboxamide;(f) 2-cyano-N-ethyl-4-fluoro-3-methoxy-benenesulfonamide;(g) 2-cyano-N-ethyl-3-methoxy-benzene sulfonamide;(h) 2-cyano-3-difluoromethoxy-N-ethyl-4-fluoro-benzene sulfonamide;(i) 2-cyano-3-fluoromethoxy-N-ethyl-benzenesulfonamide;(j) 2-cyano-6-fluoro-3-methoxy-N,N-dimethyl-benzenesulfonamide ...

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21-03-2013 дата публикации

Pesticidal Mixtures

Номер: US20130072384A1
Принадлежит: BASF SE

The present invention relates to a mixture comprising [(3S,4R,4aR,6S,12R,12aS,12bS)-3-(cyclopropanecarbonyloxy)-6,12-dihydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,2,3,4,4a,5,6,6a,12a,12b-decahydro-11H,12H-benzo[f]pyrano[4,3-b]chromen-4-yl]methyl cyclopropanecarboxylate and a fungicidal compound II in synergistic effective amounts, to the use of this mixture for controlling pests and for improving the plant health and to plant propagation material comprising this mixture. 125-. (canceled)27. The mixture according to claim 26 , wherein the fungicidal compound II is selected from the group consisting of azoxystrobin claim 26 , coumethoxystrobin claim 26 , coumoxystrobin claim 26 , dimoxystrobin claim 26 , enestroburin claim 26 , fluoxastrobin claim 26 , kresoxim-methyl claim 26 , metominostrobin claim 26 , orysastrobin claim 26 , picoxystrobin claim 26 , pyraclostrobin claim 26 , pyrametostrobin claim 26 , pyraoxystrobin claim 26 , pyribencarb and trifloxystrobin.28. The mixture according to claim 27 , wherein the fungicidal compound II is selected from the group consisting of azoxystrobin claim 27 , dimoxystrobin claim 27 , enestroburin claim 27 , fluoxastrobin claim 27 , kresoxim-methyl claim 27 , metominostrobin claim 27 , orysastrobin claim 27 , picoxystrobin claim 27 , pyraclostrobin claim 27 , pyribencarb and trifloxystrobin.29. The mixture according to claim 28 , wherein the fungicidal compound II is selected from the group consisting of dimoxystrobin claim 28 , enestroburin claim 28 , metominostrobin and pyraclostrobin.30. The mixture according to claim 26 , wherein the fungicidal compound II is selected from the group consisting of bixafen claim 26 , boscalid claim 26 , fluxapyroxad claim 26 , isopyrazam claim 26 , penflufen claim 26 , penthiopyrad claim 26 , sedaxane claim 26 , metalaxyl and ofurace.31. The mixture according to claim 30 , wherein the fungicidal compound II is selected from the group consisting of bixafen claim 30 , fluxapyroxad claim ...

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21-03-2013 дата публикации

LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS

Номер: US20130072449A1
Принадлежит: INTERMUNE, INC.

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. 5. The compound or pharmaceutically acceptable salt of claim 2 , wherein m=1 claim 2 , and wherein Ris hydrogen and Ris selected from the group consisting of optionally substituted phenyl claim 2 , imidazole claim 2 , pyridine claim 2 , thiazole claim 2 , and oxazole.6. The compound or pharmaceutically acceptable salt thereof of claim 2 , wherein m=1 claim 2 , and wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 2 , an optionally substituted oxetane claim 2 , an optionally substituted beta-lactam claim 2 , an optionally substituted tetrahydropyran claim 2 , an optionally substituted cyclopropyl claim 2 , an optionally substituted cyclobutyl claim 2 , an optionally substituted cyclopentyl claim 2 , or an optionally substituted cyclohexyl.711.-. (canceled)13. (canceled)15. (canceled)18. (canceled)20. (canceled)21. (canceled)22. (canceled)24. The compound or salt thereof of claim 1 , selected from compounds of Table 1 claim 1 , and pharmaceutically acceptable salts thereof.25. The compound or salt thereof of claim 1 , selected from compounds of Table 2 claim 1 , and pharmaceutically acceptable salts thereof.26. The compound or salt thereof of claim 1 , selected from compounds of Table 3 claim 1 , and pharmaceutically acceptable salts thereof.28. The compound or pharmaceutically acceptable salt thereof of claim 27 , wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 27 , an optionally substituted oxetane claim 27 , an optionally substituted beta-lactam claim 27 , an optionally substituted tetrahydropyran claim 27 , an optionally ...

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21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

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21-03-2013 дата публикации

HYDROXYPYRIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC USE FOR TREATING PROLIFERATIVE DISEASES

Номер: US20130072526A1
Принадлежит: BIOTHERYX INC.

Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 2. The method of claim 1 , wherein Z is a bond.3. The method of claim 1 , wherein m is 2.4. The method of claim 1 , wherein n is 0.6. The method of claim 1 , wherein Ris Calkyl.7. The method of claim 1 , wherein Ris Caryl.8. The method of claim 7 , wherein Ris phenyl.9. The method of claim 1 , wherein Ris hydrogen.10. The method of claim 1 , wherein Ris hydrogen.11. The method of claim 1 , wherein Ris —C(R).12. The method of claim 11 , wherein Ris hydrogen.13. The method of claim 11 , wherein Ris deuterium.14. The method of claim 11 , wherein Ris fluoro.15. The method of claim 1 , wherein Ris methyl or trifluoromethyl.16. The method of claim 1 , wherein Ris hydrogen.17. The method of claim 1 , wherein Ris —C(O)Caryl; R claim 1 , R claim 1 , and Rare hydrogen; Ris Calkyl; m is 2; and n is 0; where the alkyl and aryl are optionally substituted with one or more substituents Q.18. The method of claim 1 , wherein Ris benzoyl; R claim 1 , R claim 1 , and Rare hydrogen; Ris methyl; m is 2; and n is 0; where the methyl and benzoyl are optionally substituted with one or more substituents Q.19. The method of claim 1 , wherein Ris benzoyl; R claim 1 , R claim 1 , and Rare hydrogen; Ris methyl or trifluoromethyl; m is 2; and n is 0.21. The method of claim 20 , wherein the compound is 6-cyclohexyl-4-methyl-2-oxopyridin-1(2H)-yl benzoate claim 20 , or a tautomer claim 20 , a mixture of two or more tautomer claim 20 , or an isotopic variant thereof; or a pharmaceutically acceptable salt claim 20 , solvate claim 20 , hydrate claim 20 , or prodrug thereof.22. The method of claim 1 , wherein the cancer is drug resistant.23. The method of claim 1 , wherein the cancer is leukemia.24. The method of claim 1 , wherein the cancer ...

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21-03-2013 дата публикации

NOVEL EP4 AGONIST

Номер: US20130072530A1
Принадлежит:

Provided is a compound represented by the formula (1): 110.-. (canceled)1223.-. (canceled)25. The method of for the treatment of a disease whose symptoms can be mitigated by a selective EP4 agonist action.26. The method of claim 25 , wherein the disease whose symptoms can be mitigated by a selective EP4 agonist action is an immune disease claim 25 , a cardiovascular disease claim 25 , a cardiac disease claim 25 , a respiratory disease claim 25 , an ophthalmic disease claim 25 , a renal disease claim 25 , a hepatic disease claim 25 , a bone disease claim 25 , a disease of the digestive tract claim 25 , a neurological disease or a skin disease.27. The method of claim 26 , wherein the immune disease is amyotrophic lateral sclerosis claim 26 , multiple sclerosis claim 26 , Sjogren's syndrome claim 26 , rheumatoid arthritis claim 26 , systemic lupus erythematosus claim 26 , post-transplantation rejection claim 26 , arthritis claim 26 , systemic inflammation response syndrome claim 26 , sepsis claim 26 , hemophagocytic syndrome claim 26 , macrophage activation syndrome claim 26 , Still's disease claim 26 , Kawasaki disease claim 26 , hypercytokinemia at dialysis claim 26 , multiple organ failure claim 26 , shock or psoriasis.28. The method of claim 26 , wherein the cardiovascular disease or cardiac disease is arteriosclerosis claim 26 , angina pectoris claim 26 , myocardial infarction claim 26 , brain disorder caused by cerebral hemorrhage claim 26 , brain disorder caused by cerebral infarction claim 26 , brain disorder caused by subarachnoid hemorrhage claim 26 , pulmonary arterial hypertension claim 26 , peripheral arterial obstruction or a symptom attributed to peripheral circulatory disturbance.29. The method of claim 28 , wherein the peripheral arterial obstruction is arteriosclerosis obliterans or thromboangiitis obliterans.30. The method of claim 28 , wherein the symptoms attributed to peripheral circulatory disturbance is intermittent claudication or leg numbness ...

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28-03-2013 дата публикации

NOVEL ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20130076604A1
Принадлежит: CANON KABUSHIKI KAISHA

Provided are a novel organic compound appropriate for emission of green light and an organic light-emitting device including the organic compound. Provided is a substituted or unsubstituted indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene appropriate for emission of green light. The substituents of the indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene are each independently selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group. 2. The organic compound according to claim 1 , wherein Rto Rare each independently selected from a hydrogen atom and a substituted or unsubstituted aryl group.4. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}5. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}6. The organic light-emitting device according to claim 4 , wherein the organic compound layer is a light-emitting layer.7. The organic light-emitting device according to claim 6 , wherein the organic light-emitting device emits green light.8. A display apparatus having a plurality of pixels claim 4 , each including the organic light-emitting device according to and a switching device connected to the organic light-emitting device.9. An image input apparatus comprising:an image input unit configured to input an image; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a display unit configured to display the image, the display unit having a plurality of pixels, each ...

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28-03-2013 дата публикации

PYRIDYL-2-METHYLAMINO COMPOUNDS, COMPOSITIONS AND USES THEREOF

Номер: US20130079376A1
Принадлежит:

Compounds are provided according to formula I: 2. (canceled)5. (canceled)6. (canceled)7. (canceled)8. The method according to ; wherein R′″ is H.9. The method according to ; wherein Ris H or Me.10. The method according to ; wherein Ris H.11. The method according to ; wherein Ris H.12. The method according to ; wherein Ris H.13. The method according to ; wherein Ris H.16. (canceled)17. (canceled)18. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of .19. (canceled)21. The method according to claim 1 , wherein the medical condition is selected from Alzheimer's disease claim 1 , Down's syndrome claim 1 , and Parkinson's disease.22. (canceled)23. (canceled)24. The method according to claim 1 , wherein the medical condition is associated with modulation of Aβ production.25. The method according to claim 1 , wherein the medical condition is associated with inhibition of Aβ production.26. The method according to claim 1 , wherein the medical condition is associated with modulation of APP expression or APP translation.27. A method for lowering the load of Aβ plaque claim 1 , which comprises administering to the mammal an effective treating amount of a compound according to formula I claim 1 , IVa claim 1 , IVb claim 1 , or V.28. A method for lowering the brain Aβ level claim 1 , which comprises administering to the mammal an effective treating amount of a compound according to formula I claim 1 , IVa claim 1 , IVb claim 1 , or V. The present application claims the benefit under 35 U.S.C. §119 of U.S. Provisional Application Ser. No. 61/505,511, filed Jul. 7, 2011. The content of said provisional application is hereby incorporated by reference in its entirety.Provided herein are pyridylmethylamine compounds with anti-Aβ production, aggregation, inhibition of oxidative stress, and modulation of amyloid precursor protein (APP) translation properties, and pharmaceutical compositions thereof. Also provided are ...

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28-03-2013 дата публикации

ESTER COMPOUND AND USE THEREOF

Номер: US20130079378A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

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04-04-2013 дата публикации

PESTICIDAL MIXTURES CONTAINING ISOXAZOLINE DERIVATIVES AND INSECTICIDE OR NEMATOICIDAL BIOLOGICAL AGENT

Номер: US20130085064A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A, A, R, R, R, Rand Rare as defined in claim and one of Yand Yis S, SO or SOand the other is CHand component B is an insecticide or nematicidal biological agent as defined in claim . The present invention also relates to methods of using said mixtures for the control of pests. 2. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis S and the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.3. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis SO and the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.4. A pesticidal mixture according to claim 3 , wherein the molar proportion of the cis SO compounds of formula I compared to the total amount of cis SO and trans SO compounds of formula I is greater than 50%.5. A pesticidal mixture according to claim 1 , wherein in the compound of formula I L is a direct bond or methylene; one of Yand Yis SOand the other is CH; Aand Aare C—H; Ris hydrogen or methyl; Ris trifluoromethyl; Ris 3 claim 1 ,5-dichloro-phenyl; Ris methyl; and Ris hydrogen.6. A pesticidal mixture according to claim 1 , wherein when L is a direct bond Yis CHand Yis S claim 1 , SO or SO claim 1 , and wherein when L is methylene Yis S claim 1 , SO or SOand Yis CH.8. A pesticidal mixture according to claim 1 , wherein component B is a compound selected froma) a pyrethroid selected from the group consisting of permethrin, cypermethrin, fenvalerate, esfenvalerate, deltamethrin, cyhalothrin, lambda-cyhalothrin, gamma-cyhalothrin, bifenthrin, fenpropathrin, cyfluthrin, tefluthrin, ethofenprox, ...

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11-04-2013 дата публикации

PET RADIOPHARMACEUTICALS FOR DIFFERENTIAL DIAGNOSIS BETWEEN BILATERAL AND UNILATERAL CONDITIONS OF PRIMARY HYPERALDOSTERONISM

Номер: US20130089502A1
Принадлежит:

A functional PET imaging method is disclosed for differentiation between bilateral hyperplasia and unilateral adenoma comprising (1) introducing a radioactively labelled CYP11 B2 (aldosterone synthase) inhibitor which binds selectively to CYP11 B2 (aldosterone synthase) relative to CYP11 B1 (11β-hydroxylase) into a mammal with adrenal glands and (2) conducting positron emission tomography (PET) in the region of the adrenal glands to obtain a functional PET image of the adrenal glands. Also disclosed are radioactive tracer compounds suitable for use in this method, precursors for making the same, and a process for making the radioactive tracer compounds capable of being conducted as a rapid one-pot reaction. 1. A method for making a functional image of adrenal glands comprising (1) introducing a radioactively labelled CYP11B2 (aldosterone synthase) inhibitor which binds selectively to CYP11B2 relative to CYP11B1 (11β-hydroxylase) into a mammal with adrenal glands and (2) conducting positron emission tomography (PET) in the region of the adrenal glands to obtain a functional image of the adrenal glands.2. The method according to claim 1 , wherein the radioactively labelled CYP11B2 inhibitor comprises F.7. The compound of claim 4 , wherein Rrepresents CHCHX claim 4 , Ris H and Rand Rform claim 4 , together with the pyridine ring claim 4 , an isochinoline ring system.12. A process for making a radioactive tracer comprising reacting a compound of formula (I) according to claim 4 , wherein X represents Br claim 4 , I claim 4 , tosylate or mesylate claim 4 , with F ions to obtain a radioactive tracer compound of formula (I) in which X represents F.13. The process of claim 12 , wherein the process is conducted in the presence of a cyclic crown ether compound claim 12 , a potassium salt claim 12 , and an anhydrous polar aprotic organic solvent.14. The process of claim 12 , wherein the process is conducted at a temperature in the range from 70° C. to 100° C. for a time period ...

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11-04-2013 дата публикации

ESTER COMPOUND AND USE THEREOF

Номер: US20130090363A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

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11-04-2013 дата публикации

PYRETHRINOID-TYPE ESTERS AS PESTICIDES

Номер: US20130090381A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents Rrepresents 2-propenyl or 2-propynyl; Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of ...

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18-04-2013 дата публикации

ANTIMICROBIAL COMBINATIONS OF PYRION COMPOUNDS WITH POLYETHYLENEIMINES

Номер: US20130095058A1
Принадлежит: Janssen Pharmaceutica NV

The present invention relates to combinations of the pyrion compounds sodium pyrithione and 1-hydroxy-2-pyridinone, and polyethyleneimines (PEI) which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of a pyrion compound selected from sodium pyrithione and 1-hydroxy-2-pyridinone together with polyethyleneimines; in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like. 1. A composition comprising a combination of a component (I) and a component (II) in respective proportions to provide a synergistic biocidal effect , whereby component (I) is a pyrion compound selected from sodium pyrithione (I-a) and 1-hydroxy-2-pyridinone (I-b) , andcomponent (II) are polyethyleneimines.2. The composition as claimed in wherein component (II) are polyethylene-imines with an average molecular weight between 1300 and 750000.3. The composition as claimed in wherein component (II) are polyethyleneimines with an average molecular weight of approximately 1300.4. The composition as claimed in wherein component (II) are polyethyleneimines with an average molecular weight of approximately 70000.5. The composition as claimed in wherein component (II) are polyethyleneimines with an average molecular weight of approximately 750000.6. The composition as claimed in wherein the ratio by weight of component (I) to component (II) ranges from 10:1 to 1:10.7. The composition as claimed in wherein the ratio by weight of component (I) to component (II) ranges from 4:1 to 1:4.8. The composition as claimed in wherein the ratio by weight of component (I) to ...

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18-04-2013 дата публикации

ArylSulfonamide Based Matrix Metalloprotease Inhibitors

Номер: US20130096105A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I): 2. The compound of claim 1 , wherein Ris selected from (C-C) aryl claim 1 , (5-14) membered heteroaryl claim 1 , and (4-14) membered heterocycloalkyl claim 1 , each of which is optionally substituted by one to three substituents selected from the group consisting of HC(O)— claim 1 , (5-9) membered heteroaryl claim 1 , and (4-9) membered heterocycloalkyl claim 1 , (C-C) alkyl claim 1 , (C-C) cycloakyl claim 1 , R—O— claim 1 , R—C(O)— claim 1 , R—SO— claim 1 , (R)NH—C(O)— claim 1 , and (R)(R)N— claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently (C-C) alkyl or (C-C) aryl claim 1 , each of which is further optionally substituted by one to two substituents selected from the group consisting of (C-C) alkyl claim 1 , halo claim 1 , hydroxy claim 1 , (C-C) alkoxy claim 1 , (C-C) aryl claim 1 , (C-C) dialkylamino claim 1 , and (4-9) membered heterocycloalkyl; Rand Rare independently hydrogen claim 1 , or (C-C) alkyl; X is selected from hydrogen claim 1 , amine claim 1 , cyano claim 1 , halogen claim 1 , nitro claim 1 , alkyl-S— claim 1 , alkyl-SO— claim 1 , alkyl-SO— claim 1 , HN—SO— claim 1 , R—C(O)— claim 1 , alkyl claim 1 , and R—O claim 1 , wherein Rand Rare defined above; ora pharmaceutically acceptable salt thereof, or an optical isomer thereof; or a mixture of optical isomers.4. The compound of claim 3 , wherein R′ claim 3 , is selected from (C-C) alkyl claim 3 , (C-C) cycloalkyl claim 3 , (C-C) alkoxy claim 3 , HC(O)— claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl claim 3 , or (C-C) aryl claim 3 , said (C-C) aryl claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl are optionally substituted by one or two substituents selected from hydroxy claim 3 , halo claim 3 , (C-C) alkyl claim 3 , carboxyl claim 3 , (C-C) alkoxycarbonyl claim 3 , and HC(O)—;{'sub': 2', '3, 'Rand Rare hydrogen;'}{'sub': 1', '7, 'X is ...

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18-04-2013 дата публикации

USE OF A 1-N-(HALO-3-PYRIDYLMETHYL)-N-METHYLAMINO-1-ALKYLAMINO-2-NITROETHYLENE DERIVATIVE FOR PREPARING A TOPICAL VETERINARY PHARMACEUTICAL COMPOSITION FOR COMBATING EXTERNAL PARASITES

Номер: US20130096164A1
Принадлежит: VIRBAC

The present invention relates to the use, as active ingredient, of a 1-N-(halo-3-pyridylmethyl)-N-methylamino-1-alkylamino-2-nitroethylene derivative for preparing a veterinary pharmaceutical composition for topical application in the treatment of external parasites, in particular fleas, in domestic animals, in particular in dogs and cats, intended to be applied at least every 2 weeks. 2. The method as claimed in claim 1 , wherein said composition is a collar.3. The method as claimed in claim 1 , wherein said composition is a liquid composition comprising at least one pharmaceutically acceptable liquid carrier.46. The method as claimed in claim 1 , wherein the compound(s) of formula (I) is (are) chosen from the compounds in which the halogen atom denoted Hal is located in position of the pyridyl ring and denotes a chlorine atom.5. The method as claimed in claim 1 , wherein the compound(s) of formula (I) is (are) chosen from those in which Rrepresents a hydrogen atom claim 1 , a C-Calkyl radical or a C-Ccycloalkyl radical.6. The method as claimed in claim 1 , wherein the compound(s) of formula (I) is (are) chosen from those in which Rrepresents a C-Calkyl radical or a cyclopropyl radical.7. The method as claimed in claim 1 , wherein the compound(s) of formula (I) is (are) chosen from those in which Rrepresents a hydrogen atom.8. The method as claimed in claim 1 , wherein the pharmaceutical composition comprises claim 1 , as compound of formula (I) claim 1 , (E)-N-(6-chloro-3-pyridylmethyl)-N-ethyl-N′-methyl-2-nitrovinylidenediamine (nitenpyram).9. The method as claimed in claim 1 , wherein claim 1 , within the pharmaceutical composition claim 1 , the compound(s) of formula (I) represent(s) from 5% to 20% by weight relative to the total weight of the composition.10. The method as claimed in claim 1 , wherein the compound(s) of formula (I) is (are) administered to the animal in a unit dose of between 0.1 and 200 mg/kg of body weight.11. The method as claimed in claim 3 ...

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18-04-2013 дата публикации

Method of Synthesizing the Complex [FE(NNS)2] Active Against the Malaria Parasite Plasmodium Falciparum

Номер: US20130096308A1
Автор: Enos Kiremire
Принадлежит: UNIVERSITY OF NAMIBIA

Metal complex of Iron (U) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-ER spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum . They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (FIG. 1 ).

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18-04-2013 дата публикации

Process for Preparing 4-hydroxypyridines

Номер: US20130096312A1
Принадлежит: BASF SE

The present invention relates to a process for preparing 4-hydroxypyridines of formula I 114-. (canceled)16. The process as claimed in claim 15 , wherein the base is selected from alkali metal methylates.17. The process as claimed in claim 16 , wherein the base is sodium methylate.18. The process as claimed in claim 15 , wherein the base is dissolved in a monohydric C-C-alcohol.19. The process as claimed in claim 18 , wherein the monohydric C-C-alcohol is methanol.20. The process as claimed in claim 15 , wherein in step a) claim 15 , b) and c) are carried out without isolating any intermediate compound.21. The process as claimed in claim 15 , wherein the acid is selected from mineral acids.22. The process as claimed in claim 15 , wherein the ammonia source is selected from the group consisting of aqueous ammonia solution claim 15 , ammonium halides claim 15 , ammonium carboxylates and ammonium sulfate.23. The process as claimed in claim 15 , wherein Ris hydrogen claim 15 , C-C-alkyl or C-C-haloalkyl.24. The process as claimed in claim 23 , wherein Ris C-C-perhaloalkyl.25. The process as claimed in claim 15 , wherein R claim 15 , R claim 15 , Rare hydrogen claim 15 , C-C-alkyl or C-C-haloalkyl.26. The process as claimed in claim 25 , wherein R claim 25 , R claim 25 , Rare hydrogen.28. The process of claim 27 , wherein the chlorinating agent is thionyl chloride or phosphoryl chloride. The present invention relates to a process for preparing 4-hydroxypyridines.Synthesis of substituted pyridines has been the subject of intensive investigations on account of their great versatility and their uses as components of active substances, especially of medicinal drugs and plant protection agents.The reaction of an acetylacetone enol ether with ethyl perfluoroalkanoates in the presence of the strong base potassium tert-butoxide, followed by acid catalyzed cyclization to yield substituted pyranones has been disclosed by Tyvorskii et al. (Tetrahedron 54 (1998), 2819-2826). The ...

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25-04-2013 дата публикации

Insecticidal compositions and methods of using the same

Номер: US20130101687A1
Принадлежит: Clarke Mosquito Control Products Inc

Insecticidal compositions have at least one active agent and at least one insecticide. The active agent can include perilla oil, a component found in perilla oil, or a perillaldehyde or carvone analog. The insecticide can include a pyrethrum, pyrethrin, pyrethroid, neonicotinoid, chlofenapyr, ethiprole, sulfoxoflor, carbamate, organophosphate, or organochlorine. Methods for controlling insects include contacting an insect with an effective amount of a composition described in this specification. Modified plants that produce an active agent can be contacted with an insecticide.

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25-04-2013 дата публикации

METHODS AND COMPOSITIONS FOR CONTROLLING ALGAE

Номер: US20130102638A1
Принадлежит:

Described are preferred methods and compositions for controlling algae which involve the use of bleaching pyridinecarboxamide compounds. 1. A method for control of algae in a body of water , comprising:providing in the body of water an effective algicidal concentration of a bleaching pyridinecarboxamide compound.2. The method of claim 1 , comprising maintaining in said body of water a concentration of the compound of about 1 ppb to about 80 ppb.3. The method of claim 1 , wherein said providing includes applying to said body of water an aqueous liquid formulation containing the compound.5. The method of claim 4 , wherein the compound is picolinafen.8. A method of claim 7 , wherein the compound is diflufenican.9. An algicidal concentrate composition for addition to a body of water for algae control claim 7 , comprising:a liquid carrier suitable for introduction into an aquatic environment; anda bleaching pyridinecarboxamide compound at a level constituting about 5% to about 90% of said concentrate composition.11. The composition of claim 10 , wherein said compound is picolinafen.14. The composition of claim 13 , wherein the compound is diflufenican15. A product claim 13 , comprising: a container; a composition in said container claim 13 , the composition including a bleaching pyridinecarboxamide compound; said container bearing visible indicia regarding algicidal use of the composition.17. The product of claim 16 , wherein said compound is picolinafen.20. The product of claim 19 , wherein the compound is diflufenican. The present invention relates generally to the control of algae in bodies of water such as lakes, ponds and other aqueous systems. In one particular embodiment, the present invention relates to the control of-such algae using bleaching pyridinecarboxamide compounds.As further background, undesirable growth of algal species is a continuing challenge in water bodies such as lakes, ponds and reservoirs. To date, the primary agent used to control such algal ...

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25-04-2013 дата публикации

SYNERGISTIC PESTICIDAL MIXTURES

Номер: US20130102642A1
Принадлежит: DOW AGROSCIENCES LLC

Synergistic pesticidal mixtures are provided. 1. A synergistic composition comprising(b) spirotetramat.and This applications claims priority from U.S. Provisional application 60/927,119 filed on May 1, 2007, the entire disclosure of which is hereby incorporated by reference. This application also claim priority from U.S. non-provisional application Ser. No. 12/150,801 filed May 1, 2008, the entire disclosure of which is hereby incorporated by reference. This application also claim priority from U.S. non-provisional application Ser. No. 13/096,218 filed 28 Apr. 2011, the entire disclosure of which is hereby incorporated by reference.The invention disclosed in this document is related to field of pesticides and their use in controlling pests.Pests cause millions of human deaths around the world each year. Furthermore, there are more than ten thousand species of pests that cause losses in agriculture. These agricultural losses amount to billions of U.S. dollars each year. Termites cause damage to various structures such as homes. These termite damage losses amount to billions of U.S. dollars each year. As final note, many stored food pests eat and adulterate stored food. These stored food losses amount to billions of U.S. dollars each year, but more importantly, deprive people of needed food.There is an acute need for new pesticides. Insects are developing resistance to pesticides in current use. Hundreds of insect species are resistant to one or more pesticides. The development of resistance to some of the older pesticides, such as DDT, the carbamates, and the organophosphates, is well known. But resistance has even developed to some of the newer pesticides.Therefore, a need exists for new pesticides and particularly for pesticides that have new modes of action.The examples given for the substituents are (except for halo) non-exhaustive and must not be construed as limiting the invention disclosed in this document.“alkoxy” means an alkyl further consisting of a carbon ...

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25-04-2013 дата публикации

THIONATION PROCESS AND A THIONATING AGENT

Номер: US20130102774A1
Принадлежит: Vironova AB

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline PS.2 CHN as a thionating agent. A thionating agent which is crystalline PS.2 CHN. 1. A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product , by use of crystalline PS.2 CHN as a thionating agent.2. A process according to claim 1 , wherein the thionating agent and the compound are allowed to react with each other in a liquid solvent medium for the compound and for the thionating agent.3. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , a C1-C3 alkylnitrile claim 1 , a cyclic sulfone and/or a C1-C3 dialkylsulfone.4. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , sulfolane claim 1 , dimethyl sulfone and/or acetonitrile.5. The process according to claim 1 , wherein the reaction is performed at a temperature of 60° C. to 180° C.6. The process according to claim 5 , wherein the reaction is performed at temperature of 115° C. to 175° C.7. The process according to claim 1 , wherein the compound comprises a group (I) that is present in an amide function.8. The process according to claim 1 , wherein the compound comprises a group (I) that is present in a ketone function.9. The process according to claim 1 , wherein the thionating agent is used at a molar ratio to the group (I) to be transformed of 1 mole PS.2 CHN per 1-4 moles of group (I).10. The process according to claim 1 , comprising separating the thionated reaction product from the reaction.11. The process according to claim 10 , wherein water is added to the reaction and the thionated reaction product is separated as a solid material claim 10 , by precipitation or crystallization.12. A thionating agent which is ...

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02-05-2013 дата публикации

NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS

Номер: US20130109652A1
Принадлежит:

The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) 3. The compound of claim 2 , wherein Mis a phenyl group having at least one fluoro or chloro group.4. The compound of claim 2 , wherein Mis a phenyl group having one fluoro group and one chloro group.6. The compound of claim 2 , wherein Mis a phenyl group substituted with at least one (C-C)alkyloxy.7. The compound of claim 2 , wherein Mis a phenyl group substituted with a methoxy group.8. The compound of claim 2 , wherein Mis a phenyl group substituted with at least one tetrazolyl-(C-C)alkyloxy.10. A compound according to claim 1 , or a pharmaceutically acceptable acid or base addition salt thereof claim 1 , a stereochemically isomeric form thereof and an N-oxide form thereof claim 1 , wherein said compound is:1-(2,4-difluorobenzyl)-5-(benzofuran-2-yl)pyridin-2(1H)-one;1-benzyl-5-(4-fluorophenyl)pyridin-2(1H)-one;1-(2,4-difluorobenzyl)-5-(4-fluorophenyl)pyridin-2(1H)-one;1-(3-chlorobenzyl)-5-(4-fluorophenyl)pyridin-2(1H)-one;1-benzyl-5-(4-methoxyphenyl)pyridin-2(1H)-one;1-(3-(trifluoromethyl)benzyl)-5-phenylpyridin-2(1H)-one;1-(4-methylbenzyl)-5-phenylpyridin-2(1H)-one;1-(2,4-difluorobenzyl)-5-(thiophen-2-yl)pyridin-2(1H)-one;1-benzyl-5-(4-chlorophenyl)pyridin-2(1H)-one;1-(3-(trifluoromethyl)benzyl)-5-(4-chlorophenyl)pyridin-2(1H)-one;1-(2,4-difluorobenzyl)-5-(4-chlorophenyl)pyridin-2(1H)-one;1-(2,4-dichlorobenzyl)-5-(4-methoxyphenyl)pyrimidin-2(1H)-one;1-(3-chlorobenzyl)-5-phenylpyridin-2(1H)-one;1-(3-chlorobenzyl)-5-(4-methoxyphenyl)pyridin-2(1H)-one;1-Benzyl-5-phenylpyridin-2(1H)-one;1-(2,4-difluorobenzyl)-5-phenylpyridin-2(1H)-one;1-Benzyl-5-(3-methoxyphenyl)pyridin-2(1H)-one;1-Benzyl-5-(3-chlorophenyl)pyridin-2(1H)-one;1-Benzyl-5-(4-cyanophenyl)pyridin-2(1H)-one;1-Benzyl-5-(3-nitrophenyl)pyridin-2(1H)-one;1-Benzyl-5-(2-fluorophenyl)pyridin-2(1H)-one;1-Benzyl-5-(3,4-dimethoxyphenyl)pyridin-2(1H)-one;1-Benzyl-5-(naphthalen-2-yl)pyridin-2(1H)-one;1 ...

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02-05-2013 дата публикации

ANTIMICROBIAL AGENTS

Номер: US20130109713A1
Принадлежит:

The invention provides a compound of formula I:or a salt thereof, wherein R-Rand X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents. 2. The compound of wherein:{'sup': 1', 'y', 'y, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 2', 'z', 'x, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 4', '5', '6', '7', 'd', '4', '5', '6', '7', 'p', 'p', 'p', 'g', 'h', 'g', 'h', 'a', '4', '5', '6', '7', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'at least one of RRRand Ris aryl or heteroaryl wherein each aryl or heteroaryl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and the remainder of RRRand Rare each independently H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, heteroaryloxy, (C-C)alkylthio, —S(O)R, —S(O)R, —S(O)R, —S(O)NRR, and —NRR; wherein any alkyl and any alkyl or alkanoyl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and wherein any aryl, heteroaryl, or any aryl or heteroaryl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl of RRRand Ris optionally substituted with one or more (e.g. 1, 2, 3, or 4) R;'}{'sup': 8', 'p', 'p', 'p', 'g', 'h', 'g', 'h', '8', 'a', '8', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2, 'Ris H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, ...

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09-05-2013 дата публикации

INTERMEDIATES AND PROCESS FOR PREPARING A THROMBIN SPECIFIC INHIBITOR

Номер: US20130116441A1
Принадлежит: ESTEVE QUIMICA, S.A.

Process for the preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Rand Rrepresent H; or either Rrepresents ethyl and Rrepresents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates. 3. The process according to claim 2 , wherein in step (ii) the hydrobromic acid is in 48% aqueous solution and the reaction is carried out in the presence of tetrahydrofuran.4. The process according to claim 2 , wherein the compound of formula (VII-HBr) is isolated as a solid.5. The process according to claim 4 , wherein the amount of inorganic base in step a) is 2-8% by weight in relation to the starting compound of formula (VII).6. The process according to claim 4 , wherein the inorganic base of step a) is KCOor KPO.10. A compound of formula (VII-HBr) claim 4 , which is ethyl N-(4-methylamino-3-nitrobenzoyl)-N-(2-pyridyl)-3-aminopropionate hydrobromide.11. The compound of formula (VII-HBr) according to claim 10 , which is in crystalline form.12. The compound of formula (VII-HBr) according to claim 11 , which is in crystalline form I and shows a X-Ray powder diffraction pattern comprising 2θ angle values at 8.0 claim 11 , 11.8 claim 11 , 12.1 claim 11 , 12.8 claim 11 , 14.6 claim 11 , 16.1 claim 11 , 17.6 claim 11 , 18.3 claim 11 , 20.3 claim 11 , 21.4 claim 11 , 23.8 claim 11 , 24.7 claim 11 , 25.0 and 27.3 claim 11 , measured in a X-ray diffractometer with Cu Kα radiation (1.5418 Å).13. The compound of formula (VII-HBr) according to claim 11 , which is in crystalline form II and shows a X-Ray powder diffraction pattern comprising 2θ angle values at 9.2 claim 11 , 11.8 claim 11 , 18.0 claim 11 , 19.3 claim 11 , 20.2 claim 11 , 23.5 claim 11 , 24.7 claim 11 , 26.0 claim 11 , 28.4 claim 11 , 28.8 claim 11 , 29.6 and 30.4 claim 11 , measured in a X-ray diffractometer with Cu Kα radiation (1.5418 Å).16. The process according to claim 3 , ...

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09-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF 4-CARBONYL)AMINO]-3-FLUOROPHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, ITS SALTS AND MONOHYDRATE

Номер: US20130116442A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate. 2. The process of for preparing the monohydrate of the compound of the formula (I) wherein the salt of the compound of the formula (I) is then treated with an aqueous basic solution to precipitate the monohydrate of the compound of the formula (I).3. The process of wherein the monohydrate of the compound of the formula (I) precipitates at a temperature of from 35° C. to 45° C.4. The process of or for preparing of the compound of the formula (I) wherein the monohydrate is dried under reduced pressure until the compound of the formula (I) is formed.5. The process of any of to wherein the solution comprising the solved compound of the formula (I) and what from the salt of the compound of the formula (I) precipitates is the reaction mixture or is a separate solution of the compound of the formula (I) prepared after isolation of the compound of the formula (I) from the reaction mixture.6. The process of any of to wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture a protic substance and an acid precursor.7. The process of wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture an alcohol and an acylchloride.8. The process of wherein the alcohol is ethanol and the acylchloride is acetylchloride.11. The process of or wherein the compound of the formula (II) is used in a solution of a suitable organic solvent which solution is prepared by neutralization the hydrochloric acid salt of the compound of the formula (II) with a base.12. The process of any of to wherein the compound of the formula (II) it is solved in a suitable organic solvent claim 7 , treated with an acid which is generated in situ by ...

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09-05-2013 дата публикации

METHOD FOR PRODUCING SUBSTITUTED PYRIDIN-2-ONE

Номер: US20130116443A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for the preparation of substituted 3-(2-hydroxyethyl)-1-[4-nitrophenyl]pyridin-2(1H)-ones which serve as important intermediate compounds for producing drugs. 4. The process of claim 1 , wherein Ris methyl and Ris methyl.5. The process or wherein the borane complex is borane-dimethyl sulphide claim 1 , borane-tetrahydrofuran claim 1 , borane diethylaniline or catecholborane.6. The process of wherein the borane complex is used in excess.7. The process of claim 2 , wherein the copper catalyst is provided as a bis(2-pyridinecarboxylato)copper(II) complex or a hydrate thereof claim 2 , or prepared in-situ from copper iodide claim 2 , copper chloride claim 2 , copper(II) bromide claim 2 , copper(II) triflate or copper(II) sulphate with 2-pyridinecarboxylic acid.8. The process of claim 7 , wherein the copper catalyst is provided as a bis(2-pyridinecarboxylato)copper(II) complex or a hydrate thereof.9. The process of wherein the malonic acid ester is diethylmalonic acid ester claim 2 , dibenzylmalonic acid ester claim 2 , di-tert-butylmalonic acid ester or potassium ethylmalonic acid ester.10. The process of claim 9 , wherein the malonic acid ester is diethylmalonic acid ester.11. The process of claims 2 , wherein the base is sodium or potassium tert-butylate claims 2 , potassium claims 2 , sodium or caesium carbonate claims 2 , caesium fluoride or sodium hydride.12. The process of claim 11 , wherein the base is sodium or potassium tert-butylate.14. The compound of claim 13 , wherein Ris methyl and Ris methyl.15. The process of claim 3 , wherein Ris methyl and Ris methyl.16. The process of claim 3 , wherein the copper catalyst is provided as a bis(2-pyridinecarboxylato)copper(II) complex or a hydrate thereof claim 3 , or prepared in-situ from copper iodide claim 3 , copper chloride claim 3 , copper(II) bromide claim 3 , copper(II) triflate or copper(II) sulphate with 2-pyridinecarboxylic acid.17. The process of claim 16 , wherein ...

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16-05-2013 дата публикации

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

Номер: US20130121919A1

The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject. 8. A method for screening compounds of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , the method comprising:a) administering a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) to an animal model of amyloid-beta peptide deposit accumulation; andb) selecting a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) that can modulate histone acetylation after administration of the HAT Activator compound in an animal model of amyloid-beta peptide deposit accumulation.9. A method for identifying a histone acetyltransferase (HAT) activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , wherein the method comprises selecting a HAT Activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) having one or more of the following features:{'sub': '50', 'a) the ECof the compound is no more than about 1000 nM;'}b) the histone acetylation activity in vitro targets histone protein H2, H3, and/or H4; andc) the compound penetrates the blood brain barrier; or a combination thereof.10. The method of claim 9 , wherein the compound has a molecular mass less than about 500 Da claim 9 , has a polar surface area less than about 90 Å claim 9 , has less than 8 hydrogen bonds claim 9 , or a combination thereof claim 9 , in order to penetrate the blood brain barrier.12. The method of claim 11 , wherein the subject ...

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16-05-2013 дата публикации

Novel nicotine derivatives

Номер: US20130123106A1
Автор: Gandhi Paresh T.
Принадлежит:

Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III). 2. The compound as claimed in claim 1 , which is selected from the group consisting of:3-(5-(5-acetylthiophen-2-yl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(4-fluorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(1-methyl-2-oxopyrrolidine-3-carbonyl)pyridin-3-yl)benzaldehyde;1-methyl-3-(5-m-tolylnicotinoyl)pyrrolidin-2-one;3-(5-(4-chlorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;4-(5-(1-methyl-2-oxopyrrolidine-3-carbonyl)pyridin-3-yl)benzaldehyde;3-(5-(3-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(4-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-p-tolylnicotinoyl)pyrrolidin-2-one;1-methyl-3-(5-phenylnicotinoyl)pyrrolidin-2-one;3-(5-(3-fluorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(3-nitrophenyl)nicotinoyl)pyrrolidin-2-one;3-(5-(2-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-o-tolylnicotinoyl)pyrrolidin-2-one;3-(5-(3,5-dichlorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(naphthalen-1-yl)nicotinoyl)pyrrolidin-2-one;3-(5-(3-acetylphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-cyclopropylnicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(naphthalen-2-yl)nicotinoyl)pyrrolidin-2-one;4-(5-(1-methyl- ...

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16-05-2013 дата публикации

INHIBITION OF BACTERIAL BIOFILMS WITH ARYL CARBAMATES

Номер: US20130123225A1
Принадлежит:

Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same. 8. The compound of claim 1 , wherein n=1 to 5.9. The compound of claim 1 , wherein n=1 to 5 claim 1 , saturated.11. A composition comprising a carrier and an effective amount of the compound of .12. A composition comprising the compound of and a biocide.13. A composition comprising the compound of covalently coupled to a substrate.14. The composition of claim 13 , wherein said substrate comprises a polymeric material.15. The composition of claim 13 , wherein said substrate comprises a solid support.16. The composition of claim 13 , wherein said substrate is selected from the group consisting of a drainpipe claim 13 , glaze ceramic claim 13 , porcelain claim 13 , glass claim 13 , metal claim 13 , wood claim 13 , chrome claim 13 , plastic claim 13 , vinyl claim 13 , and laminate.17. The composition of claim 13 , wherein said substrate is selected from the group consisting of shower curtains or liners claim 13 , upholstery claim 13 , laundry claim 13 , and carpeting.18. A biofilm preventing claim 13 , removing or inhibiting coating composition claim 13 , comprising:(a) a film-forming resin;(b) a solvent that disperses said resin;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(c) an effective amount of the compound of , wherein said effective amount of said compound inhibits the growth of a biofilm thereon; and'}(d) optionally, at least one pigment.19. The coating composition of claim 18 , wherein said compound is covalently coupled to said resin.20. The coating composition of claim 18 , wherein said resin comprises a polymeric material.21. A substrate coated with the coating composition of .22. A method of controlling biofilm formation on a substrate comprising the step of contacting the compound of to said substrate in an amount effective to inhibit ...

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16-05-2013 дата публикации

PYRIDINE NON-CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE

Номер: US20130123304A1

Disclosed are compounds of the formula I: 2. A method according to whereinX is selected from cycloheptyl and cyclohexyl optionally substituted with one to three groups independently selected from halo, carbonyl, hydroxyl, alkyl and alkoxy;Y is selected from carbonyl, dimethylmethylene and hydroxymethylene; andZ is selected from alkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, thiophenyl and substituted thiophenyl.3. A method according to wherein X is selected from cycloheptyl and cyclohexyl optionally substituted with carbonyl or hydroxyl.4. A method according to wherein Y is dimethylmethylene.5. A method according to wherein Z is alkyl claim 2 , phenyl or cycloalkyl.6. A method according to wherein the compound is selected froma) 3-(3-Hydroxycyclohexyl)-6-(2-methyloctan-2-yl)pyridine-2,4-diol;b) 3-(2,4-Dihydroxy-6-(2-methyloctan-2-yl)pyridin-3-yl)cyclohexanone;c) 4-(4,6-Dihydroxy-2-(2-phenylpropan-2-yl)pyridin-5-yl)-6,6-dimethylbicyclo[3.1.1]heptan-2-one;d) 4-Allyl-3-(4,6-dihydroxy-2-(2-phenylpropan-2-yl)pyridin-5-yl)cyclohexanone;e) 6-(2-Cyclohexylpropan-2-yl)-3-(5-hydroxy-2-(3-hydroxypropyl)cyclohexyl)pyridine-2,4-diol; andf) 3-(5-Hydroxy-2-(3-hydroxypropyl)cyclohexyl)-6-(2-(thiophen-2-yl)propan-2-yl)pyridine-2,4-diol. This application is a continuation of and claims priority benefit from application Ser. No. 12/579,282 filed Oct. 13, 2009, which is a continuation in-part of and claims priority benefit from application Ser. No. 12/468,776 filed May 19, 2009 which claims priority benefit from application Ser. No. 61/128,088 filed May 19, 2008, and from prior provisional application Ser. No. 61/105,143 filed Oct. 14, 2008, incorporated herein by reference in its entirety.The classical cannabinoid, delta-9-tetrahydrocannabinol (Δ-THC), is the major active constituent extracted from . The effects of cannabinoids are due to an interaction with specific high-affinity receptors. Presently, two cannabinoid receptors have been characterized: CB-1, a ...

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16-05-2013 дата публикации

METHOD TO CONTROL INSECTS RESISTANT TO COMMON INSECTICIDES

Номер: US20130123307A1
Принадлежит: DOW AGROSCIENCES LLC

N-Substituted sulfoximines are effective at controlling insects resistant to common insecticides. This application claims the benefit of U.S. Provisional Application Ser. No. 60/815,932 filed on Jun. 23, 2006, and the benefit of U.S. non-provisional application Ser. No. 11/704,824 filed on Feb. 9, 2007, now abandoned, and the benefit of U.S. non-provisional application Ser. No. 13/081,886 filed on Apr. 7, 2011, now allowed.The present invention concerns a novel method to control certain insect pests, specifically those that have developed resistance to one or more classes of insecticides, through the use of N-substituted sulfoximines.The development of resistance to insecticides in insect populations is a well recognized phenomenon and there are well documented cases of resistance for all of the major classes of insecticides (Georghiou and Saito, 1984 . Plenum Press, New York; Whalon et al., 2007 , http://www.cips.msu.edu/resistance.rmdb). The reduction in effectiveness of insecticides due to the development of resistance is one of the forces that drives the discovery and development of new insecticides.Predicting whether or not a resistance mechanism that has conferred resistance to an existing insecticide will confer resistance to a novel insecticide (i.e., cross-resistance) is not necessarily a simple matter. In the case where resistance is conferred by a change or modification in the molecular target at which the insecticide acts (i.e., target-site resistance), a novel insecticide that acts at a different target site is unlikely to be affected by the resistance mechanism. Thus, in such a case in which the target site at which a novel chemistry acts is known and the resistance mechanism of concern involves a modification to a different target site, one could predict with some confidence that the resistance mechanism would not confer resistance to the novel chemistry.In contrast to the above, the case where the target site of the novel chemistry is not known or ...

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16-05-2013 дата публикации

METHOD FOR PRODUCING CARBOXYLIC ACID AMIDE

Номер: US20130123505A1
Принадлежит:

A carboxamide can be produced in a high yield by a method for producing a carboxamide, for example, represented by formula (4): 1. A method for producing a carboxamide , the method comprising allowing a carboxylic acid ester , an amine , and a formamide compound corresponding to the amine to react in the presence of a metal alkoxide.3. The method according to claim 2 , wherein the step is a step of performing the reaction in a solvent.4. The method according to claim 3 , wherein the solvent is an alcohol solvent.5. The method according to claim 2 , wherein the metal alkoxide is an alkali metal alkoxide.6. The method according to claim 2 , wherein the step is a step performed under an increased pressure condition.7. The method according to claim 2 , wherein Rin each of formulae (2) claim 2 , (3) and (4) is a hydrogen atom or a C-Calkyl group.8. The method according to claim 2 , wherein Rin formula (1) is a C-Calkyl group.9. The method according to claim 3 , wherein the metal alkoxide is an alkali metal alkoxide.10. The method according to claim 3 , wherein the step is a step performed under an increased pressure condition. The present invention relates to a method for producing a carboxamide.Carboxamides are important compounds as a variety of chemical products such as active ingredients of medicines and pesticides, and electronic materials, and synthetic intermediates thereof (see, for example, WO2004/065374).In WO2004/065374 is disclosed a method in which ethyl 4,5-bis(4-methoxyphenyl)-1,3-oxazole-2-carboxylate, which is a carboxylic acid ester, is allowed to react with formamide in the presence of sodium methoxide, which is a metal alkoxide, to give 4,5-bis(4-methoxyphenyl)-1,3-oxazole-2-carboxamide, which is a carboxamide, in a yield of 71.9% (see Example 2).However, the method is not necessarily satisfactory in the yield of the carboxamide to be obtained.Thus, new methods by which a carboxamide can be produced from a carboxylic acid ester in a high yield have ...

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16-05-2013 дата публикации

SUBSTITUTED ENAMINOCARBONYL COMPOUNDS

Номер: US20130123506A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects. 1. A compound of formula (III){'br': None, 'sup': '1', 'sub': '2', 'HN(R)—CH-A\u2003\u2003(III)'}in whichA represents pyrid-3-yl that is optionally substituted in the 6-position by fluorine, chlorine, bromine or trifluoromethyl, or represents 1,3-thiazol-5-yl that is optionally substituted in the 2-position by chlorine; and{'sup': 1', '1, 'sub': 1', '3', '2', '3, 'Rhalo-C-C-alkyl or halo-C-C-alkenyl, with the proviso that Rmust be 2,2-difluoroethyl when A represents pyrid-3-yl that is substituted in the 6-position by chlorine.'}2. A compound of formula (III) according to claim 1 , in whichA represents 6-fluoropyrid-3-yl, 6-chloropyrid-3-yl, 6-bromopyrid-3-yl, 6-trifluoromethylpyrid-3-yl, 2-chloro-1,3-thiazol-5-yl; and{'sup': 1', '1, 'sub': 1', '3', '2', '3, 'Rrepresents fluorine-substituted C-C-alkyl or C-C-alkenyl, with the proviso that Rmust be 2,2-difluoroethyl when A represents 6-chloropyrid-3-yl.'}3. A compound which is N-[(6-chloropyridin-3-yl)methyl]-2 claim 1 ,2-difluoroethane-1-amine. This application is a continuation application of U.S. application Ser. No. 13/334,949, filed Dec. 22, 2011, which is a continuation application of U.S. application Ser. No. 12/295,355, filed Mar. 11, 2009, now U.S. Pat. No. 8,106,211, issued Jan. 31, 2012, which is a §371 National Stage Application of PCT/EP2007/002386 filed Mar. 19, 2007 which claims priority from German Application 10 2006 015 467.3 filed Mar. 31, 2006, the contents of each of these are hereby incorporated by reference in their entireties.1. Field of the InventionThe present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.2. Description of Related ...

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16-05-2013 дата публикации

Pesticidal Mixtures

Номер: US20130125267A1
Принадлежит: BASF SE

The present invention, comprising: [(3S,4R,4aR,6S,6aS,12R,12a5,12b5)-3-(cyclopropanecarbonyloxy)-6,12-dihy-droxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,2,3,4,4a,5,6,6a,12a,12b-decahydro-11H,12H-benzo[f]pyrano[4,3-b]chromen-4-yl]methyl cydopropanecarboxylate (compound II) and a pesticidal compound II; in synergistic effective amounts. 130-. (canceled)32. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of alpha-cypermethrin claim 31 , bifenthrin claim 31 , cypermethrin claim 31 , deltamethrin claim 31 , flucythrinate claim 31 , lambda-cyhalothrin claim 31 , tefluthrin and permethrin.33. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of nitenpyram claim 31 , spinosad claim 31 , spinetoram and thiacloprid.34. The mixture according to claim 31 , wherein the pesticidal compound II is ethiprole.35. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of abamectin claim 31 , emamectin benzoate claim 31 , milbemectin and lepimectin.36. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of chloranthraniliprole and cyantraniliprole.37Bacillus firmus. The mixture according to claim 31 , wherein the pesticidal compound II is CNCM 1-1582.38. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of chloranthraniliprole claim 31 , spinosad and abamectin.39. The mixture according to claim 31 , wherein the pesticidal compound II is selected from the group consisting of abamectin claim 31 , bifenthrin claim 31 , alpha-cypermethrin claim 31 , metaflumizone claim 31 , pymetrozine claim 31 , chloranthraniliprole claim 31 , cyanantraniliprole claim 31 , sulfloxaflor claim 31 , spinosad and 4-{[(6-chloropyrid-3-yl)methyl](2 claim 31 ,2-difluoroethyl)amino}furan-2(5H)-on.40. The mixture according ...

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23-05-2013 дата публикации

SYNERGISTIC HERBICIDAL COMPOSITION CONTAINING FLUROXYPYR AND PENOXSULAM, HALOSULFURON-METHYL, IMAZAMOX OR IMAZETHAPYR

Номер: US20130130900A1
Принадлежит: DOW AGROSCIENCES LLC

An herbicidal synergistic composition containing (a) fluoroxypyr and (b) an ALS inhibitor herbicide, in which the ALS inhibitor herbicide is penoxsulam, halosulfuron-methyl, imazamox or imazethapyr, provides improved post-emergence weed control in rice, cereal and grain crops, pastures, rangelands, IVM and turf. 1. A synergistic herbicidal mixture comprising a herbicidally effective amount of (a) fluoroxypyr , the acid itself , or an agriculturally acceptable salt or ester thereof , and (b) an ALS inhibitor herbicide from the sulfonylurea class of herbicides.2. The mixture of in which fluoroxypyr is the meptyl ester.3. The mixture of in which the ALS inhibitor herbicide is halosufuron-methyl.4. A synergistic herbicidal mixture comprising a herbicidally effective amount of (a) fluoroxypyr claim 1 , the acid itself claim 1 , or an agriculturally acceptable salt or ester thereof claim 1 , and (b) one or more ALS inhibitor herbicides from the imidazolinone class of herbicides.5. The mixture of in which fluoroxypyr is the meptyl ester.6. The mixture of in which the ALS inhibitor herbicides are imazamox and imazethapyr.7. A method for safening centipedegrass and sunflower from the individual harmful effects of penoxsulam and halosufuron-methyl which comprises contacting centipedegrass or sunflower with claim 4 , or applying to the area under cultivation claim 4 , a synergistic mixture of penoxsulam and halosufuron-methyl.8. An herbicidal composition comprising an herbicidally effective amount of the herbicidal mixture of and an agriculturally acceptable adjuvant and/or carrier.9. A method of controlling undesirable vegetation which comprises contacting the vegetation or the locus thereof with or applying to the soil or water to prevent the emergence or growth of vegetation an herbicidally effective amount the herbicidal mixture of .10. A method of controlling undesirable vegetation in rice claim 1 , cereal and grain crops claim 1 , pastures claim 1 , rangelands claim 1 , ...

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23-05-2013 дата публикации

Carboxamides as inhibitors of voltage-gated sodium channels

Номер: US20130131035A1
Принадлежит: AMGEN INC

The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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23-05-2013 дата публикации

NOVEL TRPV3 MODULATORS

Номер: US20130131036A1
Принадлежит: AbbVie Inc.

Disclosed herein are modulators of TRPV3 of formula (II): 2. The compound according to claim 1 , or a salt thereof claim 1 , wherein u is 0.3. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted heteroaryl or optionally substituted cycloalkyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted aryl or optionally substituted heteroaryl.'}4. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted pyridinyl, pyrimidinyl, thiazolyl, oxazolyl, or pyrazolyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted phenyl or optionally substituted pyridinyl.'}5. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '6', '1', '6', '2, 'Gis pyridinyl or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '6, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '6', '1', '6, 'Gis phenyl, pyridinyl, or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —CN, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '6', '1', '6, 'Ris C-C-alkyl or C-C-haloalkyl.'}6. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '4', '1', '4', '2, 'Gis pyridinyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '4', '1', '4, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group ...

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23-05-2013 дата публикации

CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF

Номер: US20130131085A1
Принадлежит: ABBOTT LABORATORIES

The present invention features compounds of formula I 2. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , wherein said compound is selected from the group consisting of:tert-butyl(1S,3S,4S)-3-hydroxy-5-phenyl-1-(4-pyridin-2-ylbenzyl)-4-{[(1,3-thiazol-5-ylmethoxy) carbonyl]amino}pentylcarbamate;1,3-thiazol-5-ylmethyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-4-(acetylamino)-1-benzyl-2-hydroxy-5-phenylpentyl carbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-4-amino-1-benzyl-2-hydroxy-5-phenylpentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-1-benzyl-2-hydroxy-4-[(methylsulfonyl)amino]-5-phenyl pentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-1-benzyl-4-{[(dimethylamino)carbonyl]amino}-2-hydroxy-5-phenylpentylcarbamate;methyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-1-benzyl-4-{[(dimethylamino)sulfonyl]amino}-2-hydroxy-5-phenylpentylcarbamate;tert-butyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;isobutyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;isopropyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;tert-butyl (1S,3R,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}pentylcarbamate;1,3-thiazol-4-ylmethyl (1S,3S,4S)-1-benzyl-3-hydroxy-5-phenyl-4-{[(1,3-thiazol-4-ylmethoxy)carbonyl]amino}pentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-1-benzyl-2-hydroxy-4-{[(2-isopropyl-1,3-thiazol-4-yl)acetyl]amino}-5-phenylpentylcarbamate;1,3-thiazol-5-ylmethyl (1S,2S,4S)-1-benzyl-4-{[(tert-butylamino)carbonyl]amino}-2-hydroxy-5-phenylpentylcarbamate;tert-butyl benzyl((2R,3S)-2-hydroxy-4-phenyl-3-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}butyl)carbamate;1,3- ...

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23-05-2013 дата публикации

PEST CONTROL COMPOSITION

Номер: US20130131116A1
Автор: Ikari Kaori
Принадлежит: Sumitomo Chemical Company, Limited

A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q, Q, Q, Q, R, R, R, Rand m have the same meanings described in the specification) and an ester compound shown by formula (2) below (in the formula, X, X, Xand Xhave the same meanings described in the specification) and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and the ester compound represented by formula (II) is applied to a pest or a pest habitat. 2. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , G is a group shown by G-1 claim 1 , Yis an oxygen atom claim 1 , Ris a trifluoromethyl group claim 1 , each of Q claim 1 , Q claim 1 , and Qis a CH group claim 1 , Qis a CRgroup claim 1 , Ris the group defined above claim 1 , (R)is a substituent at 3- and 5-positions claim 1 , m is 2 claim 1 , and Ris a chlorine atom.3. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom.4. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom or a methyl group.5. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a halogen atom.6. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a chlorine atom.7. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group claim 1 , a C1 to C6 haloalkyl group claim 1 , a C3 to C6 cycloalkyl group claim 1 , or a (C1 to C6 alkoxy) C1 to C6 alkyl group.8. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group.9. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C1 to C6 haloalkyl group.10. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C3 to ...

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23-05-2013 дата публикации

PEST CONTROL COMPOSITION

Номер: US20130131118A1
Автор: Ikari Kaori
Принадлежит: Sumitomo Chemical Company, Limited

A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q, Q, Q, Q, R, R, R, Rand m have the same meanings described in the specification) and an ester compound shown by formula (2) below (in the formula, X, Xand Xhave the same meanings described in the specification) and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and the ester compound represented by formula (II) is applied to a pest or a pest habitat. 2. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , G is a group shown by G-1 claim 1 , Yis an oxygen atom claim 1 , Ris a trifluoromethyl group claim 1 , each of Q claim 1 , Q claim 1 , and Qis a CH group claim 1 , Qis a CRgroup claim 1 , Ris the group defined above claim 1 , (R)is a substituent at 3- and 5-positions claim 1 , m is 2 claim 1 , and Ris a chlorine atom.3. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom.4. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom or a methyl group.5. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a halogen atom.6. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a chlorine atom.7. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group claim 1 , a C1 to C6 haloalkyl group claim 1 , a C3 to C6 cycloalkyl group claim 1 , or a (C1 to C6 alkoxy) C1 to C6 alkyl group.8. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group.9. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C1 to C6 haloalkyl group.10. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C3 to C6 ...

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23-05-2013 дата публикации

Fluro substituted Omega-Carboxyaryl Diphenyl Urea for the Treatment and Prevention of Diseases and Conditions

Номер: US20130131122A1
Принадлежит: Bayer HealthCare LLC

A compound of Formula (I): 154-. (canceled)562. A compound claim where the methylamide group is substituted with a hydroxyl group.571. A pharmaceutical composition comprising a compound of claim and a physiologically acceptable carrier.581. A pharmaceutical composition for the treatment of a cancerous cell growth comprising a compound of claim and a physiologically acceptable carrier for treating cancer.605. A compound claim where either urea nitrogen atom of the compound of formula I is substituted with a hydroxyl group.627. A compound claim where the pyridine nitrogen atom is in the n-oxide form and the methylamide functionality is substituted with a hydroxyl group. This application is a continuation application of U.S. application Ser. No. 10/895,985 filed Jul. 22, 2004 which claims the benefit of the filing date of U.S. Provisional Application Ser. No. 60/489,102 filed Jul. 23, 2003 and U.S. Provisional Application Ser. No. 60/540,326 filed Feb. 2, 2004.This invention relates to novel compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating diseases and conditions mediated by abnormal VEGFR, PDGFR, raf, p38, and/or flt-3 kinase signaling, either alone or in combination with anti-cancer agents.Activation of the ras signal transduction pathway indicates a cascade of events that have a profound impact on cellular proliferation, differentiation, and transformation. Raf kinase, a downstream effector of ras, is recognized as a key mediator of these signals from cell surface receptors to the cell nucleus (Lowy, D. R.; Willumsen, B. M. 1993, 62, 851; Bos, J. L. 1989, 49, 4682). It has been shown that inhibiting the effect of active ras by inhibiting the raf kinase signaling pathway by administration of deactivating antibodies to raf kinase or by co-expression of dominant negative raf kinase or dominant negative MEK, the substrate of raf kinase, leads to the reversion of transformed cells to the normal ...

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23-05-2013 дата публикации

PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF

Номер: US20130131350A1

The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R=H, R=H, R=CH2-COOC5H) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice. 3. The compounds as claimed in for use as anti-inflammatory agent.5. The process as claimed in claim 4 , wherein solvent used in step (ii) is selected from dry and degassed benzene or CHCl.6. The process as claimed in claim 4 , wherein olefin used in step (iv) is methyl acrylate.7. The process as claimed in step (iii) of claim 4 , wherein electric bulb of 200 watt can be used to irradiate the solution for period in the range of 8 to 10 hrs.8. The compound as claimed in for use in_inhibition of the LPS induced ICAM-1 (Intercellular cell adhesion molecule-1) expression and neutrophil adhesion on human endothelial cells with ICin the range of 50±0.84 to 178±0.81 μM and 61±0.84 to 94±0.92 μM respectively.9. The compound as claimed in for use in reduction of the neutrophil influx in the lungs in a mice model of acute lung injury at doses of 0.1 claim 2 , 1.0 and 10 mg/kg b. wt. i.p. and attenuation of the LPS-induced lung injury in mice at doses of 0.1 claim 2 , 1.0 and 10 mg/kg ...

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30-05-2013 дата публикации

HYDROPHILIZED ANTIMICROBIAL POLYMERS

Номер: US20130136783A1
Принадлежит: PURDUE RESEARCH FOUNDATION

A bactericidal or antimicrobial polymeric composition includes a hydrophilic first comonomer copolymerized to a second comonomer to produce a polymeric composition that is more hydrophilic or more bactericidal or antimicrobial in an aqueous solution than either of the comonomers alone. Methods for identifying bactericidal or antimicrobial polymers, methods for rendering materials bactericidal or antimicrobial, and methods for using bactericidal or antimicrobial compositions to kill or reduce bacterial or microbial growth are also described. Applications for the inventive compositions include their use in catheters, stents, medical devices, contact lenses; root canal fillers; fibers; paper; and/or wound dressing. 1. A device comprising a substrate having thereon a polymer represented as a free-radical copolymerization product of(a) a first monomer comprising a hydrophilic monomer having an acrylate group(b) a second monomer comprising at least one monomer selected from a pyridinium-type monomer having a quaternized nitrogen and a pyridine-type monomer having a nitrogen quaternizable with an alkyl halide, the second monomer additionally having a vinyl group(c) said polymer in quaternized form being more bactericidal in an aqueous solution than the first monomer or a homopolymer formed from the first monomer, and said polymer being more bactericidal in an aqueous solution than the second monomer or a homopolymer formed from the second monomer.2. A device according to claim 1 , wherein the second monomer comprises a member of the group consisting of vinylpyridine and quaternized vinylpyridinium.3. A device according to claim 1 , wherein the first monomer comprises at least one selected from hydroxyethylmethacylate claim 1 , polyethylene glycol) rnethacrylate and polyethylene glycol) methyl ether methacrylate.4. A device according to claim 3 , wherein the second monomer comprises a member of the group consisting of vinylpyridine and quaternized vinylpyridinium.5. A ...

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30-05-2013 дата публикации

SUB-MICRON COMPOSITIONS

Номер: US20130136849A1
Автор: Maynard Nigel Paul
Принадлежит: MATTERSMITHS TECHNOLOGIES LIMITED

The invention relates to sub-micron compositions, and methods of preparing such compositions, in particular for the treatment of substrates against biological degradation biological pests. 1. A method of preparing a composition comprising sub-micron particles , containing or coated with an active agent(s) , the method comprising at least the steps of:a) (i) dispersing sub-micron particles in a solvent(s);(ii) adding to the dispersion, a formulation containing the active agent(s) dissolved in a suitable solvent in a manner sufficient to achieve substantial uniformity of the mixture (or vice versa); orb) dispersing sub-micron particles in a solvent(s) whilst concurrently or sequentially dissolving an active agent in said solvent in a manner sufficient to achieve substantial uniformity of the mixture; andc) altering the physicochemical environment within the dispersion to cause the active agent to fall out of solution as a sub-micron layer in or on the sub-micron particles.2. The method according to claim 1 , wherein the active agent is a biocide claim 1 , colouring agent or a water repellent agent or a mixture thereof.3. The method according to claim 1 , wherein the alteration in the physicochemical environment can be by one or more of; change in pH claim 1 , introduction of another moiety which reacts with the active agent to cause precipitation claim 1 , heating which can change the isoelectric point claim 1 , heating which can remove sufficient solvent such that the solubility product of the active agent is exceeded claim 1 , addition of a non-solvent of the active agent to cause precipitation or addition of a solute which causes precipitation of the active agent.4. The method according to claim 1 , wherein the physicochemical environment is altered while agitating the result of step (a) (ii) or (b) such that the active agent precipitates as a sub-micron layer on the sub-micron particles and/or within any porosity in the sub-micron particles.5. The method according ...

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30-05-2013 дата публикации

NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS

Номер: US20130137704A1
Автор: Boléa Christelle
Принадлежит: Addex Pharma, SA

The present invention relates to novel compounds of Formula (I), wherein X, X, X, X, Aand Bare defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. 2. A compound according to claim 1 , which can exist as optical isomers claim 1 , wherein said compound is either the racemic mixture or one or both of the individual optical isomers.3. A compound according to claim 1 , wherein said compound is:N-(3-Chloro-4-(pyrimidin-2-yloxy)phenyl)picolinamideor a pharmaceutically acceptable acid or base addition salt thereof,a stereochemically isomeric form thereof and an N-oxide form thereof.4. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to to and a pharmaceutically acceptable carrier and/or excipient.5. A method of treating or preventing a condition in a mammal claim 1 , including a human claim 1 , the treatment or prevention of which is affected or facilitated by the neuromodulatory effect of mGluR4 allosteric modulators claim 1 , comprising administering to a mammal in need of such treatment or prevention claim 1 , an effective amount of a compound/composition according to to .6. A method of treating or preventing a condition in a mammal claim 1 , including a human claim 1 , the treatment or prevention of which is affected or facilitated by the neuromodulatory effect of mGluR4 positive allosteric modulators claim 1 , comprising administering to a mammal in need of such treatment or prevention claim 1 , an effective amount of a compound/composition according to to .7. A method useful for treating or preventing central nervous system disorders selected from the group consisting of: addiction claim 1 , tolerance or dependence claim 1 , affective disorders claim 1 , such as depression and anxiety claim 1 , psychiatric ...

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30-05-2013 дата публикации

ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME

Номер: US20130137731A1
Принадлежит: AstraZeneca AB

The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound. 148-. (canceled)49. 2-Methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.50. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.51. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.52. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.53. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.54. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.55. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.56. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.57. A method of treating depression in a human which comprises administering to a person in need thereof a therapeutic effective amount of a compound or a pharmaceutically acceptable salt thereof claim 49 , where the compound is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.58. A method of treating depression in a human as claimed in which comprises administering to a person in need thereof a therapeutic ...

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30-05-2013 дата публикации

ANTIMICROBIAL COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20130137732A1
Принадлежит: BYOCOAT ENTERPRISES, INC.

This disclosure provides generally for antimicrobial compositions and methods for reducing or preventing microorganism growth, viability, or survival, which are useful for treating poultry, meat, seafood, vegetables, legumes, fruit, crops, and other products for human or animal consumption. For example, the compositions can include GRAS (Generally Recognized As Safe) antimicrobial components such as ε-poly-L-lysine in combination with at least one quaternary ammonium salt, including an aliphatic heteroaryl ammonium salt such as cetylpyridinium chloride. 1. An antimicrobial composition comprising:a) ε-poly-L-lysine; andb) at least one quaternary ammonium compound.2. An antimicrobial composition according to claim 1 , wherein the ε-poly-L-lysine contains from about 20 to about 40 L-lysine residues.3. An antimicrobial composition according to claim 1 , wherein each of the at least one quaternary ammonium compound is selected independently from an aliphatic heteroaryl salt claim 1 , an aliphatic benzyl dialkyl ammonium salt claim 1 , a dialiphatic dialkyl ammonium salt claim 1 , and a tetraalkyl ammonium salt.4. An antimicrobial composition according to claim 1 , wherein each of the at least one quaternary ammonium compound is selected independently from an aliphatic heteroaryl salt and an aliphatic benzyl dialkyl ammonium salt.5. An antimicrobial composition according to claim 3 , wherein the aliphatic heteroaryl salt is selected from cetylpyridinium chloride claim 3 , cetylpyridinium bromide claim 3 , and a combination thereof.6. An antimicrobial composition according to claim 3 , wherein the aliphatic benzyl dialkyl ammonium salt is selected from alkyl dimethyl benzyl ammonium halide claim 3 , alkyl diethyl benzyl ammonium halide claim 3 , alkyl methylethyl benzyl ammonium halide claim 3 , and a combination thereof.7. An antimicrobial composition according to claim 3 , wherein the dialiphatic dialkyl ammonium salt is selected from didodecyl dimethyl ammonium halide ...

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06-06-2013 дата публикации

USE OF HISTONE ACETYLTRANSFERASE INHIBITORS AS NOVEL ANTI-CANCER THERAPIES

Номер: US20130142887A1
Принадлежит: THE JOHNS HOPKINS UNIVERSITY

The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy. 2. The method of claim 1 , wherein the p300/CBP HAT inhibitor is a p300-selective inhibitor.35.-. (canceled)6. The method of claim 1 , wherein the method further comprises administering radiation therapy or at least one additional anti-cancer agent.7. The method of claim 6 , wherein the anti-cancer agent is a DNA damaging chemotherapeutic agent.8. The method of claim 7 , wherein the DNA damaging chemotherapeutic agent is cisplatin or temozolamide.9. The method of claim 1 , wherein the cancer is leukemia claim 1 , brain cancer claim 1 , lung cancer claim 1 , central nervous system (CNS) cancer claim 1 , melanoma claim 1 , renal cancer claim 1 , prostate cancer claim 1 , colon cancer claim 1 , ovarian cancer claim 1 , or breast cancer.1011.-. (canceled)1316.-. (canceled)1716. The method of claim claim 1 , wherein the method further comprises exposing the cell to radiation therapy or contacting the cell with at least one additional anti-cancer agent.18. The method of claim 17 , wherein the anti-cancer agent is a DNA damaging chemotherapeutic agent.19. The method of claim 18 , wherein the DNA damaging chemotherapeutic agent is cisplatin or temozolamide.20. The method of claim 19 , wherein the neoplastic cell is from a leukemia claim 19 , brain cancer claim 19 , lung cancer claim 19 , CNS cancer claim 19 , melanoma claim 19 , renal cancer claim 19 , prostate cancer claim 19 , colon cancer claim 19 , ovarian cancer claim 19 , or breast cancer.21. (canceled)22. The method of claim 17 , wherein the method is carried out in vitro or in vivo.2427 ...

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06-06-2013 дата публикации

HERBICIDAL COMPOSITION CONTAINING CERTAIN PYRIDINE CARBOXYLIC ACIDS AND (2,4-DICHLOROPHENOXY)ACETIC ACID

Номер: US20130143738A1
Принадлежит: DOW AGROSCIENCES LLC

Herbicidal compositions comprising 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylic acid (I) or a derivative thereof and 2,4-D or a derivative thereof. 2. The composition of claim 1 , wherein the composition further comprises a herbicide safener.3. The composition of claim 2 , wherein the herbicide safener is cloquintocet mexyl or acid.4. The composition of claim 1 , wherein (a) is the benzyl ester claim 1 , methyl ester claim 1 , or potassium salt of the compound of formula (I).5. The composition of claim 4 , wherein (a) is the methyl ester.6. The composition of claim 4 , wherein (b) is the dimethyl amine salt of 2 claim 4 ,4 D.7. The composition of claim 5 , wherein (b) is the dimethyl amine salt of 2 claim 5 ,4 D.8. The composition of claim 1 , wherein the carboxylic acid equivalent weight ratio of the compound of formula (I) or salt claim 1 , ester or amide thereof to 2 claim 1 ,4-D or salt claim 1 , ester claim 1 , or amide thereof is from 1:100 to 1:3.5.9. The composition of claim 1 , wherein the carboxylic acid equivalent weight ratio of the compound of formula (I) or salt claim 1 , ester or amide thereof to 2 claim 1 ,4-D or salt claim 1 , ester claim 1 , or amide thereof is from 1:56 to 1:7.10. The composition of claim 5 , wherein the carboxylic acid equivalent weight ratio of the methyl ester of the compound of formula (I) to 2 claim 5 ,4-D or salt claim 5 , ester claim 5 , or amide thereof is from about 1:56 to about 1:7.11. The composition of claim 10 , wherein the carboxylic acid equivalent weight ratio is from about 1:27 to about 1:14.12. The composition of claim 4 , wherein (a) is the benzyl ester claim 4 , and the carboxylic acid equivalent weight ratio of the benzyl ester of the compound of formula (I) to 2 claim 4 ,4-D or salt claim 4 , ester claim 4 , or amide thereof is from about 1:28 to about 1:7.13. The composition of claim 4 , wherein (a) is the potassium salt claim 4 , and the carboxylic acid equivalent weight ...

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06-06-2013 дата публикации

HERBICIDAL COMPOSITION CONTAINING 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl) pyridine-2-carboxylic acid or derivative thereof AND FLUROXYPYR or derivatives thereof

Номер: US20130143739A1
Принадлежит: DOW AGROSCIENCES LLC

Herbicidal compositions comprising and methods of controlling desirable vegetation utilizing 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylic acid or an agriculturally acceptable ester, amide, or salt thereof and (b) fluroxypyr or an agriculturally acceptable ester, amide, or salt thereof. 2. The composition of claim 1 , wherein the composition further comprises a herbicide safener.3. The composition of claim 2 , wherein the safener is cloquintocet acid or cloquintocet mexyl.4. The composition of claim 1 , wherein (a) is a C-Cor benzyl ester of the compound of formula (I).5. The composition of claim 4 , wherein (a) is the methyl ester of the compound of formula (I).6. The composition of claim 5 , wherein (b) is fluroxypyr meptyl.7. The composition of claim 1 , wherein the carboxylic acid equivalent weight ratio of (a) to (b) is from about 1:1 to about 1:62.8. The composition of claim 1 , wherein the carboxylic acid equivalent weight ratio of (a) to (b) is from about 1:3 to about 1:31.9. The composition of claim 6 , wherein the carboxylic acid equivalent weight ratio of (a) to (b) is from about 1:1 to about 1:62.10. The composition of claim 6 , wherein the carboxylic acid equivalent weight ratio of (a) to (b) is from about 1:3 to about 1:31.11. The composition of claim 1 , wherein (a) is the triethylammonium salt of the compound of formula (I).12. The composition of claim 11 , wherein (b) is fluroxypyr meptyl.13. The composition of claim 12 , wherein the carboxylic acid equivalent weight ratio of (a) to (b) is from about 1:6 to about 1:17.14. The method of controlling undesirable vegetation comprising contacting the undesirable vegetation claim 1 , the area adjacent to the undesirable vegetation claim 1 , or soil a herbicidally effective amount of the composition of .15. The method of claim 14 , wherein (a) is the methyl ester of the compound of formula (I) and (b) is fluroxypyr meptyl.16. The method of claim 14 , wherein the undesirable ...

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06-06-2013 дата публикации

COMPOSITION FOR REPELLING AND DETERRING VERMIN

Номер: US20130143924A1
Принадлежит:

The present invention is directed to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I) 3. Process according to claim 2 , wherein R1 is hydrogen or halogen; m is 1 or 2 claim 2 , R2 is hydrogen claim 2 , C-C-alkyl claim 2 , or phenyl; and R4 is hydrogen or acetyl.5. Process according to claim 4 , wherein R1 is hydrogen or halogen; m is 1 or 2 claim 4 , R2 is hydrogen claim 4 , C-C-alkyl claim 4 , or phenyl; and R4 is hydrogen or acetyl.7. Process according to claim 6 , wherein R1 is hydrogen or halogen; m is 1 or 2 claim 6 , R2 is hydrogen claim 6 , C-C-alkyl claim 6 , or phenyl; and R4 is hydrogen or acetyl.9. Process according to claim 8 , wherein R1 is hydrogen or halogen; m is 1 or 2 claim 8 , R2 is hydrogen claim 8 , C-C-alkyl claim 8 , or phenyl; and R4 is hydrogen or acetyl.1012-. (canceled)13. Process according to whereby the compound of formula I is applied in the form of a pour-on or spot-on formulation.14. Process for deterring vermin from places or materials where they are not wanted claim 1 , whereby an effective amount of a compound of formula I according to is applied to the place or to the material claim 1 , at which one would like to deter insect pests claim 1 , tics or mites.15. Composition for repelling vermin claim 1 , comprising a compound of formula I according to and a spreading additive.16. Process for the preparation of a composition for repelling vermin claim 1 , whereby a compound of formula I according to is mixed with a spreading additive.1718-. (canceled) The present invention relates essentially to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula I shown below. Furthermore, it relates to corresponding vermin-repelling compositions which contain these substances as the active ingredient, to compounds of formula I for the preparation of vermin-deterring ...

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06-06-2013 дата публикации

TARGETED CORRECTION OF A GENETIC DEFECT IN CANCER THERAPY

Номер: US20130143933A1
Принадлежит: TRT Pharma Inc.

The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds. 3. The mutation-selective chemosensitizer of claim 1 , wherein said compound corrects a Keap1 mutation to restore interaction between a mutated Keap1 protein and said Nrf2 protein.10. A pharmaceutical composition for the inhibition of a Nrf2 protein which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.11. A pharmaceutical composition for overcoming drug resistance in cancer chemotherapy and for the inhibition of tumor growth which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.12. A method of treating and/or preventing a disease which involves the abnormal activation or expression of a Nrf2 protein comprising administering a therapeutically effective amount of the compound of formula (I) as defined in of .13. A method of treating a cancer in a subject in need thereof comprising administering a therapeutically effective amount of a compound of formula (I) as defined in of .14. The method of claims 13 , wherein said cancer is chosen from liver cancer claims 13 , lung cancer claims 13 , breast cancer claims 13 , prostate cancer claims 13 , colon cancer claims 13 , neuroblastoma or leukemia. This application claims priority of U.S. provisional patent application U.S. 61/557,646, filed 9 Nov. 2011, the specification of which is hereby incorporated by reference.(a) FieldThe subject matter disclosed generally relates to a mutation-selective chemosensitizer for overcoming ...

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13-06-2013 дата публикации

CATALYSED SUBSTRATE MONOLITH

Номер: US20130149221A1
Принадлежит: JOHNSON MATTHEY PUBLIC LIMITED COMPANY

A catalysed substrate monolith for use in treating exhaust gas emitted from a lean-burn internal combustion engine, which catalysed substrate monolith comprising a first washcoat coating and a second washcoat coating , wherein the first washcoat coating comprises a catalyst composition comprising at least one platinum group metal (PGM) and at least one support material for the at least one PGM, wherein at least one PGM in the first washcoat coating is liable to volatilise when the first washcoat coating is exposed to relatively extreme conditions including relatively high temperatures, wherein the second washcoat coating comprises at least one metal oxide for trapping volatilised PGM and wherein the second washcoat coating is oriented to contact exhaust gas that has contacted the first washcoat coating. 1. A catalysed substrate monolith for use in treating exhaust gas emitted from a lean-burn internal combustion engine , which catalysed substrate monolith comprising a first washcoat coating and a second washcoat coating , wherein the first washcoat coating comprises a catalyst composition comprising at least one platinum group metal (PGM) and at least one support material for the at least one PGM , wherein at least one PGM in the first washcoat coating is liable to volatilise when the first washcoat coating is exposed to relatively extreme conditions including relatively high temperatures , wherein the second washcoat coating comprises at least one metal oxide for trapping volatilised PGM and wherein the second washcoat coating is oriented to contact exhaust gas that has contacted the first washcoat coating.2. The catalysed substrate monolith according to claim 1 , wherein the at least one PGM in the first washcoat coating comprises platinum.3. The catalysed substrate monolith according to claim 2 , wherein the at least one PGM in the first washcoat coating comprises both platinum and palladium4. The catalysed substrate monolith according to claim 3 , wherein a ...

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13-06-2013 дата публикации

PHENYLTHIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Номер: US20130150381A1
Принадлежит: ARDEA BIOSCIENCE, INC.

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid. 2. (canceled)4. A compound of claim 3 , wherein{'sup': 'y', 'Ris H; and'}{'sup': 'z', 'Ris H.'}5. A compound of claim 4 , wherein Ris CN claim 4 , CHOH or C(O)NH.6. A compound of claim 5 , wherein M is H.7. A compound of claim 5 , wherein M is a pharmaceutically acceptable cation.8. A compound of claim 3 , wherein{'sup': a', 'b, 'sub': 3', '3, 'Ris CHand Ris CH; or'}{'sup': a', 'b, 'Rand Rtogether with the carbon atom to which they are attached form a cyclobutyl ring.'}9. A compound of claim 3 , wherein{'sup': 'w', 'Ris H;'}{'sup': 'x', 'sub': 2', '2, 'Ris CN, CHOH or C(O)NH;'}{'sup': 'y', 'Ris H;'}{'sup': 'z', 'Ris H;'}M is H; and{'sup': a', 'b, 'sub': 3', '3, 'Ris CHand Ris CH; or'}{'sup': a', 'b, 'Rand Rtogether with the carbon atom to which they are attached form a cyclobutyl ring.'}10. (canceled)12. (canceled)14. A compound of claim 1 , wherein{'sup': 'a', 'sub': '3', 'Ris CH; and'}{'sup': 'b', 'sub': '3', 'Ris CH.'}15. A compound of claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim 1 , 5- or 6-membered ring.17. A compound of claim 1 , wherein each R claim 1 , R claim 1 , Rand Ris H.18. A compound of claim 1 , wherein{'sup': 1', '2', '3', '4, 'each R, R, Rand Ris H;'}W is CH; and{'sup': 'x', 'X is CR.'}19. A compound of claim 1 , wherein Ris fluorine.23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. The method of claim 22 , wherein the condition is gout claim 22 , a recurrent gout attack claim 22 , gouty arthritis claim 22 , hyperuricaemia claim 22 , hypertension claim 22 , a cardiovascular disease claim 22 , coronary heart disease claim 22 , Lesch-Nyhan syndrome claim 22 , Kelley-Seegmiller syndrome claim 22 , ...

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13-06-2013 дата публикации

1,4-DISUBSTITUTED 3-CYANO-PYRIDONE DERIVATIVES AND THEIR USE AS POSITIVE MGLUR2-RECEPTOR

Номер: US20130150412A1
Принадлежит:

The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. 137-. (canceled)40. The method according to claim 38 , wherein A is pyridinyl substituted with one substituent claim 38 , said substituent is halo or Calkyl.41. The method according to claim 38 , wherein Ris Calkyl.42. The method according to claim 41 , wherein Ris 1-butyl or 3-methyl-1-butyl.43. The method according to claim 38 , wherein Ris Calkyl substituted with Ccycloalkyl.44. The method according to claim 43 , wherein Ris cyclopropylmethyl or 2-(cyclopropyl)-1-ethyl.45. The method according to claim 38 , wherein Ris hydrogen or fluoro.46. The method according to claim 38 , wherein Ris halo.47. The method according to claim 38 , wherein Ris fluoro.48. The method according to claim 38 , wherein n is 1 and Ris halo.49. The method according to claim 38 , wherein n is 2 and Ris halo.50. The method according to claim 38 , wherein the pyridinyl ring represented by A is substituted with chloro or methyl.51. The method according to claim 38 , ...

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13-06-2013 дата публикации

RATIONALLY IMPROVED ISONIAZID AND ETHIONAMIDE DERIVATIVES AND ACTIVITY THROUGH SELECTIVE ISOTOPIC SUBSTITUTION

Номер: US20130150415A1
Принадлежит:

The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including 144-. (canceled)46. The method according to wherein said NHNHgroup is isotopically labeled with two N atoms.47. The method according to wherein said compound contains at least one isotopically labeled atom selected from the group consisting of carbon-13 claim 45 , nitrogen-15 claim 45 , oxygen-17 and oxygen-18 in the exocyclic acyl hydrazide moiety of the compound.49. The method according to wherein said compound has an isotopically labeled carbon-13 claim 45 , oxygen-17 or oxygen-18 atom.50. The method according to wherein said compound has an isotopically labeled carbon-13 atom.51. The method according to wherein said compound has an isotopically labeled oxygen-17 atom.52. The method according to wherein said compound has an isotopically labeled oxygen-18 atom.53. The method according to wherein said compound has an isotopically labeled carbon-13 atom and an isotopically labeled oxygen-18 atom.54. The method according to wherein said compound has an isotopically labeled nitrogen-15 atom.55MycobacteriumMycobacterium tuberculosis.. The method according to wherein said infection is56. The method according to wherein said infection is latent.57. The method according to wherein said infection is active.58. The method according to wherein said infection is miliary.59. The method according to wherein said infection is extrapulmonary.60. The method according to wherein said infection is renal.62. The method according to wherein said compound is administered in pulmonary dosage form.63. The method according to wherein said compound is administered is oral dosage form.64. The method according to wherein said compound is administered in parenteral dosage form. This application claims the benefit of priority of U.S. provisional application Ser. No. 61/127,150, filed May 9, 2008 ...

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20-06-2013 дата публикации

HERBICIDAL COMPOSITION CONTAINING FLUROXYPYR AND GLYPHOSATE

Номер: US20130157852A1
Автор: Mann Richard K.
Принадлежит: DOW AGROSCIENCES LLC

Herbicidal compositions containing fluoroxypyr and glyphosate. 1. A herbicidal composition comprising a herbicidally effective amount of (a) fluoroxypyr or salt or ester thereof and (b) glyphosate or salt or ester thereof.2. The composition of claim 1 , wherein (a) is fluoroxypyr meptyl and (b) is glyphosate ammonium.3. The composition of claim 1 , wherein the carboxylic acid equivalent weight ratio of fluoroxypyr or salt or ester thereof to glyphosate or salt or ester thereof is from 2:1 to 1:40.4. The composition of claim 3 , wherein the carboxylic acid equivalent weight ratio is from 1:1 to 1:20.5. The composition of claim 4 , wherein the carboxylic acid equivalent weight ratio is from 1:2.5 to 1:10.6. The composition of claim 2 , wherein the carboxylic acid equivalent weight ratio of fluoroxypyr meptyl to glyphosate ammonium is from 2:1 to 1:40.7. The composition of claim 2 , wherein the carboxylic acid equivalent weight ratio of fluoroxypyr meptyl to glyphosate ammonium is from 1:1 to 1:20.8. The composition of claim 2 , wherein the carboxylic acid equivalent weight ratio of fluoroxypyr meptyl to glyphosate ammonium is from 1:2.5 to 1:10.9. The composition of claim 1 , further comprising a safener.10. The composition of claim 1 , further comprising one or more additional herbicides.11. The composition of claim 1 , wherein the composition further comprises an agriculturally acceptable adjuvant or carrier.12. A method of treating undesirable vegetation comprising contacting the vegetation claim 1 , locus of the vegetation claim 1 , soil claim 1 , or water a herbicidally effective amount of the composition of .13. A method of treating undesirable vegetation comprising contacting the vegetation claim 8 , locus of the vegetation claim 8 , soil claim 8 , or water a herbicidally effective amount of the composition of .14. A method of treating undesirable vegetation comprising contacting the vegetation claim 8 , locus of the vegetation claim 8 , soil claim 8 , or water ...

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20-06-2013 дата публикации

HERBICIDAL PICOLINIC ACID SALT COMPOSITION

Номер: US20130157862A1
Принадлежит: NUFARM AUSTRALIA LIMITED

A herbicidal concentrate composition comprising a mixture of the monomethylamine and dimethylamine salts of at least one picolinic acid herbicide of formula (Ia): wherein Xis selected from hydrogen and amino. 2. A herbicidal composition according to wherein the herbicide is clopyralid.3. A herbicidal composition according to wherein the mixture of salts is present in aqueous solution of concentration of at least 300 g/L claim 1 , based on herbicidal acid equivalent.4. A herbicidal composition according to wherein the mixture of salts is present in aqueous solution of concentration of at least 500 g/L claim 1 , based on herbicidal acid equivalent.5. A herbicidal composition according to wherein the mixture of salts is present in aqueous solution of concentration of at least 700 g/L claim 1 , based on herbicidal acid equivalent.6. A herbicidal composition according to wherein the mole ratio is in the range of 70%-90% DMA to 30%-10% MMA.7. A composition consisting essentially of:i) clopyralid in the form of the monomethylamine salt and clopyralid in the form of the dimethylamine salt wherein the molar ratio of monomethylamine to dimethylamine is preferably in the range of from 10:90 to 90:10;ii) water;iii) no more than 10% by weight based on the total weight of the composition of additives selected from surfactants and compatibility agents; andiv) wherein the concentration of picolinic acid salt herbicide in the aqueous composition is at least 500 g/L based on herbicidal acid equivalent.8. A composition according to wherein the ratio is from 70%-90% DMA to 30%-10% MMA.9. A composition according to wherein the concentration of clopyralid salt herbicide is at least 500 g/L claim 8 , based on herbicidal acid equivalent.10. A composition according to wherein the concentration of clopyralid salt herbicide is at least 700 g/L claim 9 , based on herbicidal acid equivalent.11. A composition according to wherein the composition comprises casein in an amount of from 0.01 to 5% ...

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20-06-2013 дата публикации

PIPERIDINE DERIVATIVES

Номер: US20130158050A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to a compound of formula I 2. A compound of claim 1 , wherein Ris lower alkyl.3. A compound of claim 2 , wherein the phenyl group for Ar is substituted by at least two CFgroups.4. A compound of claim 3 , selected from the group consisting ofrac-2-fluoro-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-4,6-bis-trifluoromethyl-benzamide; and2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide.5. A compound of claim 1 , wherein the phenyl group for Ar is substituted by at least one CFgroup.6. A compound of claim 5 , selected from the group consisting ofrac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-bromo-6-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-N-(1,2-dimethyl-3-phenyl-piperidin-3-yl)-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-2-cyclopropyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-(1-methyl-3-phenyl-piperidin-3-yl)-2-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-chloro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N-((S)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide; andrac-2-difluoromethoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide.7. A compound of claim 5 , selected from the group consisting ofrac-N-[3-(3-chloro-phenyl)-1-methyl- ...

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20-06-2013 дата публикации

CONJUGATES OF POLYUNSATURATED FATTY ACIDS AND AMINE-CONTAINING COMPOUNDS AND USES THEREOF

Номер: US20130158070A1
Автор: Nassar Taher
Принадлежит:

Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis. 140-. (canceled)41. A method for treating dermatitis in a subject in need comprising the step of administering the subject in need docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid linked to a hydroxyproline , thereby treating dermatitis in the subject.42. A method of synthesizing 1-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoyl-4-hydroxy-pyrrolidine-2-carboxylic acid comprising:mixing tetrahydrofurane with decosahexanoic acid;adding triethylcloroformate;adding triethylamine;stirring and filtering;adding a solution of hydroxyproline and NaOH in water;adding strong acid;adding hexane;collecting organic layer; and drying43. The method according to claim 42 , wherein the step of stirring following the addition of the hydroxyproline and NaOH in water solution claim 42 , is for at 12 hours.44. The method according to claim 42 , wherein the step of drying is over anhydrous sulfate.45. A chemical conjugate comprising a first moiety and a second moiety covalently linked therebetween claim 42 , wherein said second moiety is derived from docosa-4 claim 42 ,7 claim 42 ,10 claim 42 ,13 claim 42 ,16 claim 42 ,19-hexaenoic acid claim 42 , and wherein said first moiety is derived from a therapeutically active agent or a derivative thereof claim 42 , each independently having a functional group for forming a covalent bond with said second moiety claim 42 , with the proviso that said first moiety is not hydroxyproline claim 42 , the chemical conjugate being a cyclooxygenase-2 (COX-2) inhibitor.46. The chemical conjugate of claim 45 , being further a 5-lipoxygenase (5-LOX ...

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20-06-2013 дата публикации

Methylene Urea Derivatives

Номер: US20130158076A1
Принадлежит: Merck Patent GmBH

The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. 1. A compound of formula I{'br': None, 'A-D-B\u2003\u2003(I)'}whereinD is a bivalent methylene urea moiety, or a derivative thereof,{'sub': α', 'β', 'x', 'y', 'z, 'A is a unsubstituted or substituted moiety of up to 40 carbon atoms of the formula: -L-(M-L′), where L is a 5, 6 or 7 membered cyclic structure, selected from the group consisting of aryl, heteroaryl, arylene and heteroarylene, bound directly to D, L′ comprises an optionally substituted cyclic moiety having at least 5 members, preferably selected from the group consisting of aryl, heteroaryl, aralkyl, cycloalkyl and heterocyclyl, M is a bond or a bridging group haying at least one atom, α is an integer of from 1-4; and each cyclic structure of L and L′ contains 0-4 members of the group consisting of nitrogen, oxygen and sulfur, wherein L′ is substituted by at least one substituent selected from the group consisting of —SOR, —C(O)R, and —C(NR)R'}{'sub': 'y', 'B is a substituted or unsubstituted, up to tricyclic aryl or heteroaryl moiety of up to 30 carbon atoms, comprising at least one 5-, 6-, or 7-membered cyclic structure, a 5- or 6-membered cyclic structure, bound directly to D containing 0-4 members of the croup consisting of nitrogen, oxygen and sulfur, wherein said cyclic structure directly bound to D is selected from the group consisting of aryl, heteroaryl and heterocyclyl, Ris hydrogen or a carbon based moiety of up to 24 carbon atoms optionally containing heteroatoms selected from N, S and O and optionally halosubstituted, up to per halo,'}{'sub': 'z', 'Ris hydrogen or a carbon based moiety of up to 30 carbon atoms optionally containing heteroatoms selected from N, S ...

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20-06-2013 дата публикации

INTERMEDIATES FOR THE PREPARATION OF HMG COA REDUCTASE INHIBITORS AND PROCESSES FOR THE PREPARATION THEREOF

Номер: US20130158263A1
Принадлежит:

A compound of Formula (1), is disclosed 13. The process as claimed in step (a) of claim 12 , wherein the suitable organic solvent comprises one or more of toluene claim 12 , xylene claim 12 , ethylbenzene claim 12 , cyclohexane claim 12 , hexane claim 12 , heptane claim 12 , methylene dichloride claim 12 , ethylene dichloride claim 12 , and ethyl acetate.14. The process as claimed in step (a) of claim 12 , wherein the base comprises one or more inorganic bases selected from the group consisting of sodium hydroxide claim 12 , potassium hydroxide claim 12 , sodium bicarbonate claim 12 , potassium bicarbonate claim 12 , and sodium hydride claim 12 , or one or more organic bases selected from the group consisting of triethylamine claim 12 , diisopropylethylamine claim 12 , diisopropyl amine claim 12 , 1 claim 12 ,8-diazabicycloundec-7-ene (DBU) claim 12 , and pyridine.15. The process as claimed in step (c) of claim 12 , wherein the dialkylalkoxyborane is selected from group consisting of diethylmethoxyborane claim 12 , diethylethoxyborane claim 12 , and dimethylethoxyborane.16. The process as claimed in step (c) of claim 12 , wherein the base comprises one or more of alkali metal hydrides selected from the group consisting of sodium hydride claim 12 , potassium hydride claim 12 , lithium hydride claim 12 , sodium borohydride claim 12 , potassium borohydride claim 12 , and lithium aluminium hydride.17. The process as claimed in step (c) of claim 12 , further comprising purifying the compound of Formula (5′) in a suitable organic solvent selected from the group consisting of one or more of C-Calcohol claim 12 , water claim 12 , and aliphatic hydrocarbons.18. The process as claimed in step (d) of claim 12 , wherein the suitable reagent comprises one or more of 2 claim 12 ,2-dimethoxypropane claim 12 , 2 claim 12 ,2-dimethoxypentane claim 12 , 1 claim 12 ,1-dimethoxycyclohexane claim 12 , and 2 claim 12 ,2-dimethoxybutane.19. The process as claimed in step (d) of claim 12 , ...

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20-06-2013 дата публикации

BIVALENT LINKERS AND CONJUGATES THEREOF

Номер: US20130158271A1
Принадлежит:

Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described. 2. The compound of wherein the nucleophile is a drug claim 1 , a vitamin claim 1 , an imaging agent claim 1 , a diagnostic agent claim 1 , or another bivalent linker.4. The compound of wherein the nucleophile is a drug claim 4 , a vitamin claim 4 , an imaging agent claim 4 , a diagnostic agent claim 4 , or another bivalent linker.6. The compound of wherein the nucleophile is a drug claim 5 , a vitamin claim 5 , an imaging agent claim 5 , a diagnostic agent claim 5 , or another bivalent linker. This application claims the priority benefit under 35 U.S.C. §119(e) of U.S. provisional patent application Ser. No. 60/590,580, filed Jul. 23, 2004, the disclosure of which is incorporated herein in its entirety by reference.This invention pertains to bivalent linkers, and the synthesis and use thereof. In particular, this invention pertains to the synthesis and use of bivalent linkers in preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates.Drug, vitamin, diagnostic, and imaging agent conjugates have been used to treat, diagnose, and evaluate various disease states in humans and in animals.In many cases these drug, vitamin, diagnostic, and imaging agent conjugates include intervening linkers separating for example a targeting ligand from a drug, diagnostic agent, or imaging agent. These linkers include a wide variety of bivalent fragments that may be used separately or when linked together for inclusion in conjugates to for example space a drug, diagnostic agent, or imaging apart from other parts of the conjugate, such as for example a vitamin or other targeting ligand. These linkers may also be stable to the metabolic, physiological, or biological conditions present when they are administered to humans and animals, or alternatively these linkers may undergo various routes of cleavage and/or fragmentation under such ...

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27-06-2013 дата публикации

PEST CONTROL AGENT

Номер: US20130165482A1
Принадлежит: MEIJI SEIKA PHARMA CO., LTD.

Specific amine derivatives have been found to possess excellent activities as pest control agents. 124-. (canceled)26. The amine derivative or a salt thereof according to claim 25 , wherein Y in formula (Ie′) is a hydrogen atom or a halogen atom.27. The amine derivative or a salt thereof according to claim 25 , wherein the compound of formula (Ie′) is a compound selected from the group consisting of N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-chloro-5-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidine]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-bromopyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-(1-(6-chloropyridin-3-yl)ethyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , 2-chloro-N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , N-[1-((2-chloropyrimidin-5-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide and N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,3 claim 25 ,3 claim 25 ,3-pentafluoropropanamide.28. The amine derivative or a salt thereof according to claim 25 , which has a pest control activity on at least one type of pest selected from the group consisting of lepidopterous pests claim 25 , hemipterous pests claim 25 , thysanopterous pests claim 25 , dipterous pests claim 25 , coleopterous pests claim 25 , animal parasitic fleas and ticks claim 25 , and canine heartworms.29. A pest control agent comprising at least one amine derivative or a salt thereof according to .32. The method according to or claim 25 , wherein the pest is an agricultural/ ...

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27-06-2013 дата публикации

AROMATIC COMPOUNDS WITH SULFUR CONTAINING LIGANDS

Номер: US20130165630A1

Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: 3. The compound of wherein n=2.4. The compound of wherein R═H.5. The compound of wherein n=3.6. The compound of wherein R═H.7. The compound of wherein n=4.8. The compound of wherein R═H.10. The compound of wherein n=2.11. The compound of wherein R═H.12. The compound of wherein n=3.13. The compound of wherein R═H.14. The compound of wherein n=4.15. The compound of wherein R═H. This application is a continuation-in-part of U.S. patent application Ser. No. 13/565,047 filed 2 Aug. 2012, which is a continuation of U.S. patent application Ser. No. 12/731,415 filed on 25 Mar. 2010, the full disclosure of both is incorporated herein by reference.The present invention relates generally to novel aromatic compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or also as intermediates for producing other useful compounds of this type.Free radicals are unstable oxygen-containing molecules that negatively interact with other molecules in the body, in a process called oxidation. High levels of free radicals and oxidation can lead to oxidative stress. Moderate oxidative stress can trigger apoptosis: a genetically determined process of cell self destruction marked by fragmentation of nuclear DNA. More intensive oxidative stress may cause widespread necrosis or cell death.The body naturally fights oxidation by producing glutathione (GSH). Glutathione is a tripeptide composed of three amino acid residues: glutamic acid, cysteine and glycine. Glutathione is found in all cells in the body, including the bile, the epithial lining fluid of the lungs and in the blood. Glutathione is the smallest intracellular protein thiol molecule in the cells (that is: a molecule containing an —SH or sulfhydryl group). This characteristic emphasizes its potent antioxidant action and supports a multi- ...

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04-07-2013 дата публикации

HERBICIDAL COMPOSITIONS

Номер: US20130172188A1
Автор: BRISTOW James Timothy
Принадлежит: ROTAM AGROCHEM INTERNATIONAL CO.,LTD

A herbicidal composition comprising an aqueous suspension of microcapsules, having a capsule wall of a porous condensate polymer, and containing a solution of fluoroxypyr in a rosin solvent system comprising rosin and/or a rosin derivative. There is also provided a herbicidal composition comprising microcapsules, having a capsule wall of a porous condensate polymer, and containing fluoroxypyr and a solvent comprising rosin and/or a rosin derivative. A method of preparing a herbicidal composition is also disclosed, comprising providing a water immiscible phase comprising fluoroxypyr and an isocyanate dissolved in a rosin solvent system comprising rosin and/or a rosin derivative; providing an aqueous phase comprising one or more surfactants; combining the water immiscible phase and the aqueous phase to form a dispersion of the water immiscible phase in the aqueous phase; adding to the resulting dispersion an amine, thereby forming microcapsules of polyurea containing droplets of the water immiscible phase; and curing the microcapsules. 1. A herbicidal composition comprising an aqueous suspension of microcapsules , the microcapsules having a capsule wall of a porous condensate polymer , wherein the microcapsules contain a solution of fluoroxypyr in a rosin solvent system comprising rosin and/or a rosin derivative.2. The composition according to claim 1 , wherein fluoroxypyr is present in the composition in an amount of at least 20% by weight.3. The composition according to claim 2 , wherein fluoroxypyr is present in the composition in an amount of at least 50% by weight.4. The composition according to claim 1 , wherein the rosin solvent system consists essentially of rosin and/or a rosin derivative.5. The composition according to claim 1 , wherein the rosin solvent system comprises a rosin derivative selected from hydrogenated rosin claim 1 , polymerized rosin claim 1 , esters of rosin or hydrogenated rosin claim 1 , in particular methyl esters of rosin or of ...

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04-07-2013 дата публикации

BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA

Номер: US20130172310A1
Принадлежит:

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. 172.-. (canceled)75. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of .76. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of .77. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of .78. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of .80. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of .81. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of .83. A method for preventing or treating a condition in a mammal in need thereof characterized by undesired thrombosis comprising administering to said mammal the pharmaceutical composition of . This invention relates to novel compounds which are potent and highly selective inhibitors of isolated factor Xa or when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, fIXa) or the fibrinolytic cascades (e.g. plasminogen activators, plasmin). In another aspect, the present ...

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04-07-2013 дата публикации

PHENOXYALKYL PYRIDINIUM OXIME THERAPEUTICS FOR TREATMENT OF ORGANOPHOSPHATE POISONING

Номер: US20130172393A1
Принадлежит:

Phenoxyalkyl pyridinium oxime compounds for use in treating organophosphate poisoning. 2. The composition of claim 1 , wherein R is methyl claim 1 , ethyl claim 1 , phenyl claim 1 , methoxy claim 1 , ethoxy claim 1 , trimethyl claim 1 , methylchloro claim 1 , diethyl claim 1 , diethylchloro claim 1 , ethylchloro claim 1 , phenoxy claim 1 , acetyl claim 1 , benzoyl claim 1 , bromo claim 1 , chloro claim 1 , iodo claim 1 , dichloro claim 1 , or trichloro.3. The composition of claim 1 , wherein R is one of the following substituents:{'sub': '3', '4-CH—;'}{'sub': 3', '2', '2, '2,6-([CH]CH)—;'}{'sub': '3', '4-CH—O;'}4-Cl—;4-Br—;{'sub': '2', '4-ON—;'}{'sub': '2', '3-ON—;'}{'sub': '3', '4-CHCO—;'}{'sub': 3', '2, '4-CHCHCO—;'}3-CHCH═CHCH-4;4-Ph;{'sub': 3', '3, '2,3,5-(CH)—;'}{'sub': 3', '3, '2,4,6-(CH)—;'}{'sub': '3', '3-CH-4-Cl—;'}4-Ph-CO—;{'sub': '2', '2,5-Cl—;'}4-Ph-O—;{'sub': '2', '4-Ph-CH—;'}{'sub': '2', '4,Ph-CH—O—;'}{'sub': '3', '2,4,5-Cl)—;'}{'sub': '2', '4-Ph-CHCO—;'}{'sub': '3', '2,4,6-Cl—;'}{'sub': '2', '3,4-Cl—;'}{'sub': 2', '2, '2,6-Cl-4-ON—;'}{'sub': 3', '2, '4-Cl-3,5-(CH)—;'}3-Ph-;{'sub': 3', '2, '3-CHCH-4-Cl—;'}{'sub': '3', '3-O—C(:O)—CH═C(CH)-4;'}{'sub': 3', '3', '3, '2-CH-4-(CH)C—;'}{'sub': 3', '3', '2, '2,4-[(CH)C—]—;'}{'sub': 3', '2', '3', '2, '4-CHCHC(CH)—;'}{'sub': 3', '3', '2', '2', '2, '4-(CH)CCHC(CH)—;'}2-Br-4-Cl—;2-Cl-4-Br—;{'sub': '3', '2-Br-4-CH—;'}{'sub': 3', '2, '4-Br-3,5-(CH)—;'}{'sub': 3', '2', '6, '4-CH(CH)—O—;'}{'sub': 3', '2, '4-Ph-C(CH)—;'}{'sub': 3', '2', '2, '4-CH—O—CHCH—; or'}{'sub': '2', '2,4-Cl—.'}43. The composition of any of - claims 1 , wherein X is halo claims 1 , optionally bromo.54. The composition of any of - claims 1 , wherein the composition comprises a pharmaceutically acceptable excipient in combination with the compound.65. A method of reactivating phosphorylated brain acetylcholinesterase that has been inhibited by at least one organophosphorous compound claims 1 , the method comprising administering to a subject in need ...

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04-07-2013 дата публикации

METHOD FOR OXIDIZING ALCOHOLS

Номер: US20130172543A1
Принадлежит: TOHOKU UNIVERSITY

A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant. 2. The method according to claim 1 , wherein the alcohol is a secondary alcohol.3. The method according to claim 1 , wherein the bulk oxidant is a peracid claim 1 , hydrogen peroxide claim 1 , a hypohalogen acid or a salt thereof claim 1 , a perhalogen acid or a salt thereof claim 1 , a persulfuric acid salt claim 1 , a halogenating agent such as a halide and N-bromosuccinimide claim 1 , a trihalogenated isocyanuric acid claim 1 , a diacetoxyiodoallene claim 1 , a dialkyl azodicarboxylate claim 1 , oxygen claim 1 , air claim 1 , or a mixture thereof.4. The method according to claim 1 , wherein the bulk oxidant is air.5. The method according to claim 2 , wherein the bulk oxidant is a peracid claim 2 , hydrogen peroxide claim 2 , a hypohalogen acid or a salt thereof claim 2 , a perhalogen acid or a salt thereof claim 2 , a persulfuric acid salt claim 2 , a halogenating agent such as a halide and N-bromosuccinimide claim 2 , a trihalogenated isocyanuric acid claim 2 , a diacetoxyiodoallene claim 2 , a dialkyl azodicarboxylate claim 2 , oxygen claim 2 , air claim 2 , or a mixture thereof.6. The method according to claim 2 , wherein the bulk oxidant is air. The present invention relates to a method for oxidizing an alcohol utilizing an organic catalyst.Oxidation reactions of alcohols constitute one class of important reactions as methods for chemical conversion of compounds, and are frequently used in syntheses of organic compounds with high added values such as medicaments and agricultural chemicals and the like. Therefore variety of methods have been developed so far. However, many of those methods use explosive reagents, highly toxic metals and the ...

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04-07-2013 дата публикации

Process for Preparing Carbamolypyridone Derivatives and Intermediates

Номер: US20130172551A1
Принадлежит:

The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates. 8. The method of wherein the hydrolyzing reagent is LiOH.10. The method of wherein the Lewis acid is a magnesium halide or a lithium halide.15. The method of wherein the Lewis acid is a magnesium halide or a lithium halide. The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates which are useful as HIV integrase inhibitors.Compounds having HIV integrase inhibitory activity are described in WO 2006/116764 (corresponding to U.S. Ser. No. 11/919386 assigned to Shionogi & Co. Ltd.). The compounds are disclosed as polycyclic carbamoylpyridone deriviatives. Processes for making them are also disclosed. Among the examples of these compounds, the following polycyclic carbamoylpyridone derivatives are included:The processes disclosed for preparing these compounds are quite arduous, involving as many as 14 steps. It would therefore be an advance in the art to find ways of making these compounds with greater efficiency.The present invention provides an improved process for preparing the following compounds:In one aspect, the present invention is a method comprising contacting methyl 3-{[2,2-bis(methyloxy)ethyl]amino}-2-[(methyloxy)acetyl]-2-propenoate (formula I):with an oxalate ester of formula II:in the presence of MOR, where R is alkyl, aryl, or benzyl; and M is an alkali metal cation; to form a pyridinone of formula III:In a second aspect, the present invention method comprising selectively hydrolyzing a pyridinone of formula III:where R is alkyl, aryl, or benzyl with a selective hydrolyzing reagent to form a pyridinone carboxylic acid of formula IV where R is alkyl, aryl, or benzyl:with greater than 90% selectivity.In a third aspect, the present invention is a method comprising contacting a compound of formula VII:with a magnesium or lithium cation and a nucleophilic anion to form a compound of formula VIII:In a fourth aspect, ...

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04-07-2013 дата публикации

PHENOL DERIVATIVES AND PHARMACEUTICAL OR COSMETIC USE THEREOF

Номер: US20130172564A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): 2. The compound as defined by claim 1 , wherein:{'sub': '1', 'Rrepresents a halogen, a methyl, an ethyl, an isopropyl, a trifluoromethyl, a nitrile, a nitro, a methoxy, an ethoxy, an isopropoxy, a thiomethyl, a thioethyl, or a thioisopropyl group.'}3. The compound as defined by claim 2 , wherein the Rgroup represents a halogen claim 2 , a methoxy claim 2 , an ethoxy claim 2 , a thiomethyl claim 2 , a thioethyl or a trifluoromethyl group.4. The compound as defined by claim 1 , wherein the Rgroup is a hydrogen atom.5. The compound as defined by wherein the Rgroup is a hydrogen atom or a Calkyl group.6. The compound as defined by claim 1 , wherein the compound is selected from the group consisting of:2-[(5-Bromopyridin-3-ylamino)methyl]phenol;2-[(5-Bromopyridin-3-ylamino)methyl]-3-fluorophenol;2-[(5-Bromopyridin-3-ylamino)methyl]-4-fluorophenol;2-[(5-Methylpyridin-3-ylamino)methyl]phenol;2-[(5-Bromopyridin-3-ylamino)methyl]-5-fluorophenol;2-[(5-Bromopyridin-3-ylamino)methyl]-3,5-dichlorophenol;2-[(5-Bromopyridin-3-ylamino)methyl]-4-chlorophenol;2-[(5-Bromopyridin-3-ylamino)methyl]-4,6-difluorophenol;2-[1-(5-Bromopyridin-3-ylamino)propyl]phenol;2-[1-(5-Bromopyridin-3-ylamino)ethyl]-4-fluorophenol;2-[(5-Methoxypyridin-3-ylamino)methyl]phenol;2-[1-(5-Bromopyridin-3-ylamino)ethyl]phenol;2-[(5-Bromopyridin-3-ylamino)methyl]-3,4-difluorophenol;5-(2-Hydroxybenzylamino)nicotinonitrile;2-[(5-Chloropyridin-3-ylamino)methyl]phenol;5-(2-Hydroxybenzylamino)nicotinonitrile;2-[(5-Chloropyridin-3-ylamino)methyl]phenol;2-[1-(5-Bromopyridin-3-ylamino)butyl]phenol;2-[1-(5-Bromopyridin-3-ylamino)pentyl]phenol;2-[(5-Bromo-6-methylpyridin-3-ylamino)methyl]phenol;2-[(5-Bromo-6-methoxypyridin-3-ylamino)methyl]phenol;5-(2-Hydroxybenzylamino)-3-methylpyridine-2-carbonitrile;2-[(6-Methoxy-5-methylpyridin-3-ylamino)methyl]phenol;2-[(6-Chloro-5-methylpyridin-3-ylamino)methyl] ...

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04-07-2013 дата публикации

METHODS OF PRODUCING METHYL 4-AMINO-3-CHLORO-6-(4-CHLORO-2-FLUORO-3-METHOXYPHENYL)PYRIDINE-2-CARBOXYLATE

Номер: US20130172566A1
Принадлежит: DOW AGROSCIENCES LLC

Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. 1. A method of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxy-phenyl)pyridine-2-carboxylate , comprising:adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxy-phenylboronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxy-phenylboronic acid and an aqueous phase;separating the organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid from the aqueous phase;reacting the 4-chloro-2-fluoro-3-methoxyphenylboronic acid with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate; anddeacetylating the methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.2. The method of claim 1 , wherein adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenylboronic acid comprises forming the organic phase comprising methyl isobutyl ketone and the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and the aqueous phase comprising water and ...

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04-07-2013 дата публикации

METHOD FOR PRODUCTION OF F-18 LABELED AMYLOID BETA LIGANDS

Номер: US20130172620A1
Принадлежит: PIRAMAL IMAGING SA

This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives. 2. A method according to claim 1 , wherein PG is selected from the group consisting of:a) Boc,b) Trityl andc) 4-Methoxytrityl.3. A method according to claim 1 , wherein LG is selected from the group consisting of:a) Halogen andb) Sulfonyloxy,Wherein Halogen is chloro, bromo or iodo.4. A method according to claim 3 , wherein Sulfonyloxy is selected from the group consisting of:a) Methanesulfonyloxy,b) p-Toluenesulfonyloxy,c) (4-Nitrophenyl)sulfonyloxy,d) (4-Bromophenyl)sulfonyloxy.5. A method according to claim 1 , wherein n=3 and X═CH.6. A method according to claim 1 , wherein n=3 claim 1 , X═CH claim 1 , R=Boc claim 1 , and LG=Methanesulfonyloxy.7. A method according to claim 1 , wherein the radiofluorination reaction is carried out in a mixture of acetonitrile and co-solvents claim 1 , wherein the percentage of acetonitrile is at least 50%.8. A method according to claim 7 , wherein the radiofluorination reaction is carried out in a mixture of acetonitrile and co-solvents claim 7 , wherein the percentage of acetonitrile is at least 70%.9. A method according to claim 7 , wherein the radiofluorination reaction is carried out in a mixture of acetonitrile and co-solvents claim 7 , wherein the percentage of acetonitrile is at least 90%.10. A method according to claim 1 , wherein 1.5-75 μmol claim 1 , preferably 10-30 μmol and even more preferably 12-25 μmol of compound of Formula II are used in Step 1.11. A method according to claim 1 , wherein the method is performed as a fully automated process.12. A kit claim 1 , comprising a sealed vial comprising a predetermined quantity of a compound of formula II of and a sealed vial comprising acetonitrile or acetonitrile and a co-solvent.13. A method according to claim 1 , wherein Step 3 comprises a purification by HPLC.14. A method according to claim 13 , wherein the HPLC solvent used in ...

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11-07-2013 дата публикации

HERBICIDAL COMPOSITIONS

Номер: US20130178365A1
Автор: BRISTOW James Timothy
Принадлежит: ROTAM AGROCHEM INTERNATIONAL CO., LTD.

A herbicidal composition comprising microcapsules containing a solution of at least one herbicidally active compound that is solid at room temperature and with a melting point below 190° C., other than a sulfonylurea, preferably fluroxypyr, in a polyhydric alcohol ester solvent system; suspended in a continuous phase having suspended therein finely divided particles of one or more sulfonylureas. A method for preparing the composition comprising i) providing a water-immiscible liquid phase comprising a polyhydric alcohol ester, an active compound that is solid at room temperature and with melting point below 190° C., and a first wall forming component; ii) providing an aqueous phase comprising water and, optionally, one or more surface active agents; iii) combining the water immiscible phase with the aqueous phase to form a dispersion of the water-immiscible phase in the continuous aqueous phase; iv) adding a second wall forming component to the resulting mixture, causing interfacial polymerization of the first and second wall forming components and encapsulating droplets of the water-immiscible phase; v) providing a suspension of a sulfonylurea in a polyhydric alcohol ester, optionally with one or more dispersants; and vi) combining the composition prepared in step (iv) with the composition prepared in step (v). 1. A herbicidal composition comprising microcapsules containing a solution of at least one herbicidally active compound that is solid at room temperature and with a melting point below 190° C. , said herbicidally active compound being other than a sulfonylurea , in a polyhyrdric alcohol ester solvent system; the microcapsules being suspended in a continuous phase of a polyhydric alcohol solvent system having suspended therein finely divided particles of one or more sulfonylureas.2. The herbicidal composition according to claim 1 , wherein the polyhydric alcohol ester solvent system consists essentially of one or more polyhydric alcohol esters.3. The ...

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18-07-2013 дата публикации

SYNERGISTIC PESTICIDE COMPOSITIONS

Номер: US20130183390A1
Принадлежит: BAYER CROPSCIENCE LP

The present invention relates to compositions that include a combination of one or more pesticides and one or more adjuvants. 1. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and dibutyl sebacate.2. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and oleic acid.3. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and benzenepropanoic acid.4. A composition consisting of an active ingredient comprising a pyrethrum and/or a pyrethroid and methyl oleate.5. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and methyl linoleate.6. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and butylated hydroxyanisole (BHA).7. A composition comprising an active ingredient comprising a pyrethrum and/or a pyrethroid and two or more sebacates , wherein the sebacates are hindered amine light stabilizers and wherein said composition does not include an attractant.8. The composition of claim 7 , wherein the sebacates are bis(1 claim 7 ,2 claim 7 ,2 claim 7 ,6 claim 7 ,6-pentamethyl-4-piperidinyl)sebacate and methyl(1 claim 7 ,2 claim 7 ,2 claim 7 ,6 claim 7 ,6-pentamethyl-4-piperidinyl)sebacate.9. The composition of claim 1 , wherein the pyrethrum comprises pyrethrin.10. The composition of claim 1 , wherein pyrethroid comprises deltamethrin claim 1 , permethrin claim 1 , β-cyfluthrin claim 1 , bifenthrin claim 1 , and/or resmethrin.1110. A method for controlling or preventing a pest infestation comprising administering the composition of anyone of - to a place in need thereof. This application is a Divisional of U.S. application Ser. No. 12/410,840, filed Mar. 25, 2009, the contents of which is incorporated by reference herein in its entirety, which claims priority to U.S. Provisional Application No. 61/163,206, filed Mar. 25, 2009 and U.S. Provisional Application No. 61/072,778, filed Apr. ...

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18-07-2013 дата публикации

METHOD FOR PREPARATION OF NICOTINIC ACID COPPER CHLORIDE COMPLEX, AND ITS PHARMACEUTICAL USES

Номер: US20130184247A1
Принадлежит:

A method for preparation pharmaceutical compounds in large quantities consists of copper (I) halide, preferably the chloride complex of nicotinic acid characterized by elemental analysis, spectroscopy and crystallographic methods, used for treatment of muscular dystrophy, myopathy, myasthenia gravis, parkinsonism, Chronic Fatigue Syndrome, Male Infertility and post stroke muscle weakness. 1. The method for preparation of nicotinic acid copper chloride complex , the method for which comprises adding , drop wise , a suspension of copper (I) chloride in aqueous alcohol , to nicotinic acid dissolved in aqueous alcohol to obtain a reactant solution , from which develops a clear reddish precipitate of the nicotinic acid copper (I) chloride complex , having the empirical chemical formula:{'br': None, 'sub': 12', '12', '2', '5, 'CHClCuNO.'}2. In the method according to the final mixture was allowed to stand over several hours until the crystalline precipitate was formed.3. In the method according to . the precipitate was filtered utilizing a pump and washed with ascorbic acid solution in alcohol claim 2 , the solution comprising 70-90% ascorbic acid claim 2 , further washings with ethanol 70-99% claim 2 , acetone and dried under vacuum.4. In the method according to where the reactant solution is subject to boiling.5. A nicotinic acid copper (I) chloride complex prepared in accordance with the method of claim 1 , having the chemical formula:{'br': None, 'sub': 12', '10', '2', '4', '2, 'CHClCuNO.HO'}6. A pharmacologically active composition for the treatment of patients suffering from muscular dystrophy claim 1 , the composition comprising a unit dosage amount of a nicotinic acid copper (I) chloride monohydrate complex claim 1 , and a physiologically suitable carrier.7. The pharmacologically active composition for the treatment of patients suffering from muscular dystrophy according to claim 6 , comprising in addition to the physiologically suitable carrier a material ...

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18-07-2013 дата публикации

Novel Phenylamino Isonicotinamide Compounds

Номер: US20130184314A1
Принадлежит: Merck Patent GmBH

The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. 113-. (canceled)15. A method for treating hyperproliferative diseases related to the hyperactivity of MEK as well as diseases modulated by the MEK cascade in mammals , comprising administering to a subject a compound according to in which radicals not designated in greater detail have the meaning indicated for the Formula (I) according to but in which:in Subformula IAX is NH,{'sup': '1', 'Ris Hal, methyl or ethyl,'}{'sup': '2', 'Ris hydrogen, Hal, methoxy or acetylene,'}{'sup': '3', 'Ris hydrogen or Hal,'}{'sup': '4', 'Ris hydrogen or Hal,'}{'sup': 5', '6, 'R, Rare OH,'}Hal is F, Cl, Br or I,in Subformula IBX is NH,{'sup': '1', 'Ris Hal,'}{'sup': '2', 'Ris hydrogen or Hal,'}{'sup': '3', 'Ris hydrogen or Hal,'}{'sup': '4', 'Ris hydrogen or Hal,'}{'sup': 5', '6, 'R, Rare OH,'}Hal is F, Cl, Br or I,in Subformula ICX is NH,{'sup': '1', 'Ris F, Cl, methyl or ethyl,'}{'sup': '2', 'Ris hydrogen, I, Br, methoxy or acetylene,'}{'sup': '3', 'Ris hydrogen or Hal,'}{'sup': '4', 'Ris hydrogen or Hal,'}{'sup': 5', '6, 'R, Rare OH,'}Hal is F, Cl, Br or I,in Subformula IDX is NH,{'sup': '1', 'Ris F, Cl, methyl or ethyl,'}{'sup': '2', 'Ris hydrogen, I, Br, methoxy or acetylene,'}{'sup': '3', 'Ris hydrogen or F,'}{'sup': '4', 'Ris hydrogen or Cl'}{'sup': 5', '6, 'R, Rare OH,'}in Subformula IEX is NH,{'sup': '1', 'Ris F or Cl,'}{'sup': '2', 'Ris I or Br,'}{'sup': '3', 'Ris hydrogen or F,'}{'sup': '4', 'Ris hydrogen or Cl'}{'sup': 5', '6, 'R, Rare OH,'}in Subformula IFX is NH,{'sup': '1', 'Ris F or Cl,'}{'sup': '2', 'Ris I or Br,'}{'sup': '3', 'Ris hydrogen or F,'}{'sup': '4', 'Ris hydrogen or Cl,'}{'sup': 5', '6, 'R, Rare OH,'}in Subformula IGX is NH,{'sup': '1', 'Ris F or Cl,'}{'sup': '2', 'Ris I or Br,'}{'sup': '3', 'Ris hydrogen,'}{'sup': '4', 'Ris hydrogen,'}{'sup': 5', '6, 'R, Rare OH,'}and in ...

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