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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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Применить Всего найдено 9894. Отображено 100.
27-07-2006 дата публикации

ТЕХНОЛОГИЧЕСКАЯ ЛИНИЯ ПОЛУЧЕНИЯ N`-МЕТИЛ-1-ФЕНИЛ-1-N, N-ДИЭТИЛАМИНОМЕТАНСУЛЬФОНАМИДА (ВАРИАНТЫ)

Номер: RU0000054940U1
Автор: Иванов Владимир Борисович, Савельчев Алексей Петрович, Шарипов Эдуард Нависович
Принадлежит: Общество с ограниченной ответственностью "ФОСФОРОС" (ООО "ФОСФОРОС")

1. Технологическая линия получения N'-метил-1-фенил-1-N,N-диэтиламинометансульфонамида, включающая последовательно соединенные: реактор для получения раствора комплекса диэтиламина с SO, оборудованный устройством для подачи газообразного SO, дозаторами для подачи диэтиламина и растворителя, мерник для дозирования раствора комплекса диэтиламина с SO, реактор для синтеза N'-метил-1-фенил-1-N,N-диэтиламинометансульфонамида, оборудованный мерниками для подачи бензальметиламина и воды, охлаждаемый реактор интенсивного смешения, подогреваемый реактор интенсивного смешения. 2. Технологическая линия получения N'-метил-1-фенил-1-N,N-диэтиламинометансульфонамида, включающая последовательно соединенные: реактор для получения раствора комплекса диэтиламина с SO, оборудованный устройством для подачи газообразного SO, дозаторами для подачи диэтиламина и растворителя, мерник для дозирования раствора комплекса диэтиламина с SO, реактор для синтеза N'-метил-1-фенил-1-N,N-диэтиламинометансульфонамида, оборудованный мерниками для подачи бензальметиламина и воды, охлаждаемый реактор интенсивного смешения, реактор-перекристаллизатор, оборудованный мерником для подачи растворителя, устройство для фильтрования, имеющее три выхода, соединенные с емкостью для отстоя, устройством для регенерации растворителя и подогреваемым реактором интенсивного смешения. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 54 940 (13) U1 (51) МПК C07C 311/03 C07C 311/05 C07C 311/32 (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2005138221/22 , 22.11.2005 (24) Дата начала отсчета срока действия патента: 22.11.2005 (45) Опубликовано: 27.07.2006 (73) Патентообладатель(и): Общество с ограниченной ответственностью "ФОСФОРОС" (ООО "ФОСФОРОС") (RU) U 1 5 4 9 4 0 R U дозаторами для подачи диэтиламина и растворителя, мерник для дозирования раствора комплекса диэтиламина с SO2, реактор для синтеза N'-метил-1-фенил ...

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Номер записи: 1
26-01-2012 дата публикации

Fluorine-containing n-alkylsulfonylimide compound, manufacturing method therefor, and method of manufacturing an ionic compound

Номер: US20120022269A1
Автор: Daisuke Takano, Hiroyuki Yatsuyanagi, Takashi Konishi, Tsunetoshi Honda
Принадлежит: Mitsubishi Materials Corp, Mitsubishi Materials Electronic Chemicals Co Ltd

According to the method for producing fluorine-containing N-alkylsulfonylimide compound, the fluorine-containing N-alkylsulfonylimide compound can be produced safely with a high recovery rate by alkylating fluorine-containing sulfonylimide acid or fluorine-containing sulfonylimide acid salt with dialkylsulfuric acid or dialkylcarbonic acid.

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Номер записи: 2
23-02-2012 дата публикации

Process for preparing organic compounds by a transition metal-catalysed cross-coupling reaction of an aryl-x, heteroaryl-x, cycloalkenyl-x or alkenyl-x compound with an alkyl, alkenyl, cycloalkyl or cycloalkenyl halide

Номер: US20120046471A1
Автор: Axel Jacobi von Wangelin, Mark Sundermeier, Matthias Gotta, Waldermar Maximilian Czaplik
Принадлежит: Saltigo GmbH

This invention relates to a process for preparing functionalized aryl, heteroaryl, cycloalkenyl, or alkenyl compounds, by a transition-metal-catalyzed cross-coupling reaction of a substituted or unsubstituted aryl-X, heteroaryl-X, cycloalkenyl-X or alkenyl-X compound with an alkyl, alkenyl, cycloalkyl or cycloalkenyl halide, where X is a halide, diazonium, tosylate (p-toluenesulphonate), mesylate (methanesulphonate) or triflate (trifluoromethanesulphonate) leaving group.

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Номер записи: 3
22-03-2012 дата публикации

Liquid agricultural formulations of improved stability

Номер: US20120071320A1
Автор: Franklin N. Keeney, John M. Atkinson, LEI Liu, Melissa G. Olds
Принадлежит: DOW AGROSCIENCES LLC

Agricultural oil dispersions of improved stability and processes to make and methods to use such compositions are disclosed. The compositions are comprised of an active ingredient coated with one or more non-oil soluble polymers that hinder degradation of the active ingredient by other ingredients.

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Номер записи: 4
05-04-2012 дата публикации

Novel Compounds, Pharmaceutical Compositions Containing Same, Methods of Use for Same, and Methods for Preparing Same

Номер: US20120083471A1
Автор: Craig A. Townsend, Edward Wydysh, Francis Kuhajda, Gabriele Valeria Ronnett
Принадлежит: JOHNS HOPKINS UNIVERSITY

The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).

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Номер записи: 5
17-05-2012 дата публикации

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

Номер: US20120122920A1
Автор: David Enrique MIGUEL CENTENO, Josep Castells Boliart, Marta Pascual Gilabert
Принадлежит: Institut Universitari de Ciencia i Tecnologia

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

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Номер записи: 6
28-06-2012 дата публикации

Methods for producing bis(sulfonyl)imide ammonium salt, bis(sulfonyl)imide and bis(sulfonyl)imide lithium salt

Номер: US20120165571A1
Автор: Masao Iwaya, Ryuji Seki, Shouji Furuta
Принадлежит: Asahi Glass Co Ltd

To provide methods for producing a bis(sulfonyl)imide ammonium salt, a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt simply and in good yield. A method for producing a bis(sulfonyl)imide ammonium salt, which comprises reacting a compound of the formula R—CHF—SO 2 X (wherein R is a C 1-4 fluorinated alkyl group which may contain an etheric oxygen atom, or a fluorine atom, and X is a fluorine atom or a chlorine atom) with ammonia in the absence of a catalyst. Further, methods for producing a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt by using the bis(sulfonyl)imide ammonium salt.

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Номер записи: 7
29-11-2012 дата публикации

Herbicidal mixtures

Номер: US20120302441A1
Автор: Adam F. Burnhams, Andress Landes, Bernd Sievernich, Cyrill Zagar, Herve R. Vantieghem, Peter Dombo
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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Номер записи: 8
14-03-2013 дата публикации

Method for manufacturing fluorine-containing imide compound

Номер: US20130066110A1
Автор: Noriaki Matsumura, Tsunetoshi Honda
Принадлежит: Mitsubishi Materials Corp

With this method for manufacturing fluorine-containing imide compounds, a method for manufacturing a fluorine-containing imide compound ((Rf 1 SO 2 )(Rf 2 SO 2 )NH) is selected which includes reaction of a fluorine-containing sulfonic acid (Rf 1 SO 3 H) and a fluorine-containing sulfonamide (Rf 2 SO 2 NH) in the presence of thionyl chloride. Wherein, Rf 1 and Rf 2 are fluorine, or straight-chain or branched perfluoroalkyl groups with a carbon number of 1-4.

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Номер записи: 9
21-03-2013 дата публикации

ANTI-DIABETIC COMPOSTIONS AND METHODS

Номер: US20130072454A1
Автор: Afkham Mahnoosh, Gorgani Nick Naser
Принадлежит: OZSTAR THERAPEUTICS PTY LTD

The present invention is concerned with synergistic compositions effective in the treatment of diabetes. In particular, the present invention is concerned with synergistic compositions comprising inulin, or a suitable source thereof, and Sulphonylureas used in the treatment of type-2 Diabetes Mellitus (T2DM) and hyperglyacemia. 1. Method of treating diabetes comprising the administration to a subject requiring such treatment of a composition comprising inulin , or a source thereof , and a sulphonylurea , in the amount and for a time sufficient to reduce , regulate or normalize blood glucose concentration.2. Method of improving efficacy of sulphonylurea treatment of diabetes in a subject receiving a sulphonylurea anti-diabetic therapy , comprising administration to said subject , a composition comprising inulin or a source thereof.3. A method of or , wherein diabetes is Type-2 diabetes mellitus.4. Method of treating hyperglycemia comprising the administration to a subject requiring such treatment of a composition comprising inulin , or a source thereof , and a sulphonylurea , in the amount and for a time sufficient to reduce , regulate or normalize blood glucose concentration.5. Method of preventing the development of , or ameliorating , hypoglycaemia in a subject treated with a sulphonylurea , comprising the administration to a subject requiring such treatment of a composition comprising inulin or a source of inulin , in the amount and for a time sufficient to prevent or ameliorate hypoglycemia.6. A method of any one of to , wherein inulin , or a source thereof , is administered simultaneously or sequentially , in any order , with the sulphonylurea.7. A method of any one of to , wherein the source of inulin is a plant or part thereof.8. A method of claim 7 , wherein the plant or part thereof is selected from onion claim 7 , leek claim 7 , garlic claim 7 , artichoke claim 7 , salsify claim 7 , agave and chicory.9. A method according to claim 8 , wherein the source of ...

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Номер записи: 10
04-04-2013 дата публикации

Herbicidal composition

Номер: US20130085065A1
Автор: Hiroshi Kikugawa, Ryu Yamada, Takashi Terada, Tomoaki Kezuka
Принадлежит: Ishihara Sangyo Kaisha Ltd

At present, many herbicidal compositions have been developed and used, but there are a variety of types of weeds to be controlled, and their development lasts for a long period of time. Thus, a high active and long-residual herbicidal composition having a broad herbicidal spectrum has been desired. The present invention provides a synergistic herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one urea compound selected from the group consisting of tebuthiuron, diuron and metobromuron or its salt. According to the synergistic herbicidal composition of the present invention, a high active and long-residual herbicidal composition having a broad-spectrum can be provided.

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Номер записи: 11
11-04-2013 дата публикации

NOVEL SPECIFIC CASPASE-10 INHIBITORS

Номер: US20130090385A1
Автор: Convard Thierry, LARDY Claude, LECOMTE Marc, VIDAL Catherine
Принадлежит: Merck Patent Gesellschaft Mit Beschrankter Haftung

The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy. 128.-. (canceled)301. A method according to Claim , in which R1 represents a phenyl group optionally substituted by one or more groups , which may be identical or different , chosen from a halogen atom and an -alkyl , —O-alkyl , —CO-alkyl , —NO , —O-perhaloalkyl , —S(O)-alkyl or -perhaloalkyl group , or two substituents together form a phenyl or pyridyl group fused to the phenyl nucleus to which they are attached; or R1 represents a cycloalkyl , heteroaryl or alkyl group.311. A method according to Claim , in which R1 represents a phenyl group substituted by at least one halogen atom.321. A method according to Claim , in which R2 and R3 together form a cycloalkyl group , optionally substituted by one or more alkyl groups; or R2 and R3 together form a heterocyclyl group.331. A method according to Claim , in which R5 represents a hydrogen atom or an alkyl group , optionally substituted by one or more cycloalkyl groups.341. A method according to Claim , in which R and R′ , which may be identical or different , independently represent a hydrogen atom or an alkyl group.351. A method according to Claim , in which i=2.361. A method according to Claim , in which j=0.371. A method according to Claim , in which the group —(CH)R4 is in the para position.391. A method according to Claim , wherein the compound is administered to a newly diagnosed diabetic patient and/or a patient suffering from early retinopathy and which comprises specifically inhibiting caspase-10 in the patient.4140. A compound of the formula (I) according to Claim , for which R1 represents a phenyl group optionally substituted by one or more groups , which may be identical or different , chosen from a halogen atom and an -alkyl , —O-alkyl , —CO-alkyl , —NO , —S(O)-alkyl , ...

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Номер записи: 12
18-04-2013 дата публикации

METHOD FOR PRODUCING 1-AMINO-1-ALKOXYCARBONYL-2-VINYLCYCLOPROPANE

Номер: US20130096339A1
Автор: Asada Kuniko, Asuma Yuuki, DEKISHIMA Yasumasa, HIDAKA Tsugihiko, Kawabata Hiroshi, Miyake Ryoma, Suzuki Tatsuya, Takehara Jun
Принадлежит: API Corporation

It is an object of the present invention to provide a novel method for producing (1R,2S)/(1S,2R)-1-amino-1-alkoxycarbonyl-2-vinylcyclopropane which is useful as a synthetic intermediate of therapeutic agents for hepatitis C and a synthetic intermediate thereof. According to the present invention, when a trans-2-butene derivative having a leaving group at each of the 1- and 4-positions is reacted with a malonic ester in the presence of a base, a specific amount of an alkali metal alkoxide or an alkali metal hydride is used as the base, and further a specific amount of a malonic ester is used to produce a cyclopropane diester, and further, chiral or achiral 1-amino-1-alkoxy-carbonyl-2-vinylcyclopropane and a salt thereof are synthesized using the cyclopropane diester. 3. The method according to claim 1 , which comprises a step of purifying the compound represented by the formula (4) after performing the step (i).5. The method according to claim 4 , wherein the step (vi) is a step (vi-1) of allowing the compound represented by the formula (4) claim 4 , which has been obtained by the step (v) claim 4 , to react with an enzyme claim 4 , cells containing the enzyme claim 4 , a preparation of the cells claim 4 , or a culture solution obtained by culturing the cells claim 4 , so as to produce an optically active compound represented by the formula (5).8. The method according to claim 4 , wherein the absolute stereochemistry of the compound represented by the formula (5) is (1S claim 4 ,2S).10. The method according to claim 9 , wherein claim 9 , in the step (vii-1) claim 9 , the reaction intermediate is allowed to react with a metal azide compound or a trialkylsilyl azide in the presence of an acid.11. The method according to claim 9 , wherein the absolute stereochemistry of the compound represented by the formula (5) is (1S claim 9 ,2S) claim 9 , and the absolute stereochemistry of each of the compounds represented by the formula (6) claim 9 , the formula (7) and the ...

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Номер записи: 13
23-05-2013 дата публикации

DEFOLIANT COMPOSITION AND METHOD

Номер: US20130130901A1
Автор: Gaytan Jesse H., Hickey Joseph A., IV Osborn J., Turner
Принадлежит: ARYSTA LIFESCIENCE NORTH AMERICA, LLC

An aqueous suspension or slurry (suspension concentrate) contains a synergistic amount of thidiazuron, diuron and surfactants. The aqueous suspension contains surfactants in amounts to obtain a stable suspension or slurry without the use of organic solvents. 1. A composition for controlling vegetation comprising an aqueous suspension or slurry of thidiazuron , diuron , and at least one surfactant in an amount sufficient to maintain thidiazuron and diuron in suspension in an aqueous matrix.2. The composition of claim 1 , wherein said thidiazuron and diuron are present in a ratio of about 5:1 by weight.3. The composition of claim 1 , wherein said diuron is present in a synergistic amount to enhance the efficacy of the thidiazuron.4. The composition of claim 1 , wherein the composition further includes at least one component selected from the group consisting of emulsifiers claim 1 , wetting agents claim 1 , thickening agents claim 1 , dispersing agents claim 1 , and mixtures thereof.5. (canceled)6. The composition of claim 1 , wherein the composition is a suspension concentrate.7. The composition of claim 6 , wherein the concentrate includes about 10 wt % to about 40 wt % thidiazuron and about 5 wt % to about 20 wt % diuron based on the total weight of the concentrate.8. The composition of claim 6 , wherein the concentrate includes about 35 wt % to about 40 wt % thidiazuron and about 15 wt % to about 20 wt % diuron based on the total weight of the concentrate.9. The composition of claim 6 , further comprising a dispersing agent.10. The composition of claim 9 , wherein the thidiazuron and diuron have a median particle diameter of not greater than about 5 μm.11. The composition of claim 9 , wherein the concentrate comprises about 10 wt % to about 40 wt % thidiazuron claim 9 , about 5 wt % to about 20 wt % diuron claim 9 , a surfactant claim 9 , a dispersing agent and the balance water claim 9 , where the percentages are based on the total weight of the concentrate.12. ...

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Номер записи: 14
13-06-2013 дата публикации

MODULATORS OF RETINOID-RELATED ORPHAN RECEPTOR GAMMA

Номер: US20130150333A1
Автор: Babine Robert, Li Xiaolin, Thacher Scott, Tse Bruno
Принадлежит: ORPHAGEN PHARMACEUTICALS

Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor γ (RORγ) activity. This modulation has numerous effects, including inhibition of T-17 cell function and/or T-17 cell activity, and inhibition of re-stimulation of T-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of RORγ results in stimulation of T-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines). 1. A method of inhibiting T-17 cell differentiation , function or activity in an individual afflicted with multiple sclerosis , psoriasis , Crohn's disease , asthma , rheumatoid arthritis , uveitis or psoriatic arthritis , comprising administering to said individual an effective amount of a small organic molecule antagonist of RORγ , wherein said small organic molecule antagonist has a molecular weight of less than about 600 daltons , wherein the ability of said small organic molecule to act as a RORγ antagonist is demonstrable by its ability to inhibit transcription through the RORγ ligand binding domain and to regulate the affinity of the RORγ ligand binding domain with a coregulatory peptide at concentrations of 1 μM or less.2. The method of claim 1 , wherein said T-17 cell function or activity is release of a cytokine.3. The method of claim 2 , wherein said cytokine is interleukin-17 or interleukin-22.4. The method of claim 1 , wherein the RORγ antagonist is orally administered.5. The method of wherein the RORγ antagonist is locally administered.6. The method of wherein said effective amount of a RORγ antagonist is administered on a daily basis without resulting in weight loss or hypertriglyceridemia.7. The method of claim 1 , wherein the coregulatory peptide binding is measured by a method selected from the group consisting of fluorescence resonance energy transfer (FRET) claim 1 , fluorescence polarization claim 1 , time-resolved FRET (TR-FRET) and Alpha Screen.8. A method of ...

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Номер записи: 15
04-07-2013 дата публикации

PROCESS FOR PREPARATION OF HIV PROTEASE INHIBITORS

Номер: US20130172295A1
Автор: Crawford Kenneth R., DOWDY Eric D., Gutierrez Arnold, Polniaszek Richard P., Yu Richard Hung Chiu
Принадлежит: Gilead Sciences, Inc.

A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed 4. The process of claim 1 , where the reaction is carried out at a temperature of between about 0° C. to about 100° C.5. The process of claim 1 , where the reaction is carried out in the presence of a catalyst comprising a lanthanide or transition metal complexed to a chiral ligand.7. The process of claim 1 , which is carried out in the presence of a solvent.8. The process of claim 7 , where the solvent is a polar aprotic solvent.9. The process of claim 8 , where the solvent is methyl-t-butyl-ether claim 8 , dichloromethane or a mixture thereof.10. The process of claim 1 , which is carried out in the presence of excess 2 claim 1 ,3-dihydrofuran as a solvent.11. The process of claim 1 , where the catalyst comprises Sc.12. The process of claim 1 , where the catalyst comprises Yb.18. The process of claim 17 , where the deprotection is accomplished by combining the compound of Formula M with a deprotecting agent which is selected from trifluoroacetic acid claim 17 , hydrochloric acid claim 17 , toluenesulfonic acid claim 17 , methanesulfonic acid claim 17 , benzenesulfonic acid claim 17 , or hydrobromic acid.20. The process of claim 19 , where the reduction is accomplished by contacting the compound of Formula C with a reducing agent which is lithium aluminum hydride claim 19 , sodium borohydride claim 19 , lithium borohydride claim 19 , sodium trisacetoxyborohydride claim 19 , sodium cyanoborohydride claim 19 , potassium triisopropoxy borohydride or diisobutyl aluminum hydride28. A pharmaceutical composition comprising the salt of and an excipient claim 27 , diluent or carrier.29. A method for the treatment or prophylaxis of a retrovirus infection in a patient claim 27 , comprising administering to the patient a therapeutically effective amount of the salt of .30. The method of claim 29 , where the retrovirus is human ...

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Номер записи: 16
04-07-2013 дата публикации

NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES

Номер: US20130172388A1
Автор: FENG Rentian, XIE Xiang-qun, YANG Peng
Принадлежит: University of Pittsburgh -- Of The Commonwealth System of Higher Education

Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: 3. The compound according to claim 2 , wherein R′″ is (C-C)heterocycloalkyl.4. The compound according to claim 3 , wherein R′″ is oxetanyl claim 3 , tetrahydrofuranyl claim 3 , tetrahydropyranyl claim 3 , oxepanyl claim 3 , tetrahydrothiophenyl claim 3 , tetrahydrothiopyranyl claim 3 , 1 claim 3 ,3-dioxanyl claim 3 , oxazolidinyl claim 3 , azetidinyl claim 3 , pyrrolidinyl claim 3 , piperidinyl claim 3 , azepinyl claim 3 , piperazinyl claim 3 , morpholinyl claim 3 , tetrahydrothiopyranyl-1-oxide claim 3 , tetrahydrothiopyranyl-1 claim 3 ,1-dioxide claim 3 , pyrrolidinonyl claim 3 , piperidinonyl claim 3 , azepinonyl claim 3 , piperazidinonyl claim 3 , oxazidilinonyl claim 3 , azetidinonyl claim 3 , or morpholinonyl.7. (canceled)8. The compound according to claim 1 , wherein the compound conforms to Formula I′ and whereinD is H;D′ is phenyl;{'sub': 1', '6, 'B and Q are independently (C-C)alkylene;'}e is 0 and each of f and g is 1; and{'sup': a′', 'a″', 'a′″, 'sub': 1', '6, 'each of R, R, and R is independently selected from the group consisting of H, and straight or branched chain (C-C)alkyl.'}10. (canceled)12. The compound according to claim 11 , wherein subscripts h and k independently are 0 and subscript j is 1.14. (canceled)16. The compound according to claim 15 , wherein substituent X is N claim 15 , T and R are each independently S(O)— and Q′ is (C-C)alkyl.17. The compound according to claim 15 , wherein substituent X is CH— and each of Q′ claim 15 , R and T are independently —O—(CH)—O— claim 15 , —OC(O)— or (CH)—OC(O)—.2022-. (canceled)23. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.24. (canceled)25. A method for treating multiple myeloma or osteoporosis in a subject by ...

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Номер записи: 17
25-07-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130190338A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris H, halogen or Calkyl; and'}{'sup': '8', 'Ris H or CN.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methyl propionate, methyl-2-benzoic acid, methyl-2-methylbenzoate, methyl-3-methylphenylacetamide, methyl-3-methylphenylsulfonamide, methyl acetic acid, methyl-2-methylphenylcarboxylate or propionic acid;'}{'sup': '5', 'sub': '2', 'Ris —S(O)—, S or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '7', 'Ris chlorine, ...

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Номер записи: 18
25-07-2013 дата публикации

Novel Tetrahydronaphalene Antagonists to the Thromboxane A2 (TP) Receptor

Номер: US20130190370A1
Автор: Ballatore Carlo, Brunden Kurt R., Hogan Anne-Marie, Huryn Donna M., Lee Virginia M.Y., PISCITELLI Francesco, Smith Amos B., Trojanowski John Q.
Принадлежит: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental. 1. A composition comprising a TP receptor antagonist , wherein said antagonist comprises the chemical structures set forth in , a salt thereof , a prodrug thereof , and combinations thereof.2. The composition of claim 1 , wherein said antagonist binds to a TP receptor or a TP-like receptor.3. The composition of claim 1 , wherein said antagonist inhibits activation of a TP receptor or a TP-like receptor.4. The composition of claim 1 , wherein said antagonist is able to cross the blood brain barrier of a mammal.5. The composition of claim 1 , wherein said antagonist is not able to cross the blood brain barrier of a mammal.6. The composition of claim 1 , wherein said antagonist is selected from the group consisting of CNDR-51418 claim 1 , CNDR-51281 claim 1 , CNDR-51354 and CNDR-51414.7. A method of treating a disorder associated with activation of a TP receptor in a mammal in need thereof claim 1 , said method comprising administering to said mammal a therapeutically effective amount of a compound claim 1 , wherein said compound comprises a TP receptor antagonist claim 1 , wherein said antagonist comprises the chemical structures set forth in claim 1 , a salt thereof claim 1 , a prodrug thereof claim 1 , and combinations thereof.8. The method of claim 7 , wherein said antagonist is able to cross the blood brain barrier of said mammal.9. The method of claim 7 , wherein said antagonist is not able to cross the blood brain barrier of said mammal.10. The method of claim 7 , wherein said mammal is a human.11. The method of claim 7 , wherein said disorder associated with activation of a TP receptor is a neurodegenerative disorder.12. The method of claim 11 , wherein said neurodegenerative disorder is ...

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Номер записи: 19
25-07-2013 дата публикации

NOVEL SULFONAMIDE COMPOUNDS FOR INHIBITION OF METASTATIC TUMOR GROWTH

Номер: US20130190396A1
Автор: Carta Fabrizio, DEDHAR Shoukat, McDonald Paul C., Supuran Claudiu
Принадлежит: METASIGNAL THERAPEUTICS INC.

Therapeutic ureido-sulfonamide compositions having compounds with the formula 1. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of Formula (I){'br': None, 'sub': 2', '2, 'R-Q-Ar—SONH\u2003\u2003Formula (I)'}wherein,R is an aryl, heteroaryl, aralkyl, alkyl or cycloalkyl group, with or without a substituent;{'sub': 2', 'n, 'Q is -L(CH)—, wherein n=0, 1 or 2;'}{'sub': '2', 'L is —NHC(X)NH—, —NHC(S)SNH—, —NHC(O)NHC(S)NH—, or —SONH—;'}X is O or S; and{'sub': 6', '10, 'Ar is a C-Caryl or a heteroaryl that contains at least one heteroatom of oxygen, nitrogen or sulphur, provided that the compound of Formula (I) is not'}4-[(anilinocarbonyl)amino]benzenesulfonamide;4-{[(Pentafluorophenyl)carbamoyl]amino}benzenesulfonamide;4-{[(4′-Acetylphenyl)carbamoyl]amino}benzenesulfonamide;4-{[(4′-Chlorophenyl)carbamoyl]amino}benzenesulfonamide; or4-{[([4′-(Trifluoromethyl)phenyl]aminocarbonyl)amino]}benzenesulfonamide.2. The pharmaceutical composition of wherein Q is —NHC(O)NH— claim 1 , Ar is phenyl claim 1 , and R is PhCH claim 1 , PhCH claim 1 , 4-FCH claim 1 , 4-ClCH claim 1 , 4-BrCH claim 1 , CF claim 1 , 2-MeOCH claim 1 , 4-AcCH claim 1 , 2-i-PrCH claim 1 , 4-i-PrCH claim 1 , 4-n-BuCH claim 1 , 4-n-BuOCH claim 1 , 4-n-octyl-CH claim 1 , 4-NCCH claim 1 , 2-NCCH claim 1 , 4-PhOCH claim 1 , 2-PhCH claim 1 , 3-ONCH claim 1 , 4-MeO-2-MeCH claim 1 , Cyclopentyl claim 1 , Indan-5-yl claim 1 , 3 claim 1 ,5-MeCH claim 1 , 4-CFCH claim 1 , or 3 claim 1 ,5-(CF)CH.3. The pharmaceutical composition of wherein the compound of Formula (I) is4-{[(Benzylamino)carbonyl]amino}benzenesulfonamide;4-{[(Benzhydrylamino)carbonyl]amino}benzenesulfonamide;4-{[(4′-Fluorophenyl)carbamoyl]amino}benzenesulfonamide;4-{[(4′-Bromophenyl)carbamoyl]amino}benzenesulfonamide;4-{[(2′-Methoxyphenyl)carbamoyl]amino}benzenesulfonamide;4-{[(2′-iso-Propylphenyl)carbamoyl]amino}benzenesulfonamide;4-{[(4′-iso-Propylphenyl)carbamoyl]amino}benzenesulfonamide;4-{[(4′-n-Butylphenyl ...

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Номер записи: 20
01-08-2013 дата публикации

METHOD OF INCREASING CROP YIELD AND CONTROLLING THE GROWTH OF WEEDS USING A POLYMER COMPOSITE FILM

Номер: US20130196851A1
Автор: DUJARDIN Ralf, PARRISH Mark
Принадлежит: BAYER INNOVATION GMBH

Methods of protecting a crop from weed infestation, controlling weed growth, reducing fumigant dosage in crop protection, and reducing the growth of weeds by applying a polymer composite material with or without a biocide to soil, a crop, a vegetable, a weed, or combinations thereof are provided. In an aspect, the disclosure provides for a polymer composite material including a base polymer coated with: 1. A method of protecting a crop from weed infestation comprising applying a polymer composite material to soil , a crop , a weed , or combinations thereof , wherein said polymer composite material comprises a base polymer compound coated with(1) a first barrier layer;(2) a second layer comprising a biocide; and(3) a third protective layer.2. The method of claim 1 , wherein the weed is nutsedge.3. The method of claim 1 , wherein said first layer comprises a polyacrylate claim 1 , said second layer comprises gelatin claim 1 , and said third layer comprises gelatin and a hardener.4. The method of claim 1 , wherein said biocide comprises halosulfuronmethyl or ethoxysulfuron.5. The method of claim 1 , wherein crop safety is increased relative to a conventional plastic mulch film or virtually impenetrable film (VIF) with a biocide.6. The method of claim 5 , wherein the increased crop safety is more effective as compared to a conventional plastic mulch film or VIF applied over an equal area to which the same biocide active ingredient has been spray applied pre-emergence in the same amount as that present in the polymer composite material.7. The method of claim 1 , wherein crop yield is increased.9. The method of claim 8 , wherein the weed is nutsedge.10. The method of claim 8 , wherein the polymer composite material without a biocide reduces the growth of nutsedge at least 20% as compared to a conventional plastic mulch film or VIF without a biocide.11. The method of claim 8 , wherein said polymer composite material does not include a fumigant.12. The method of claim 8 , ...

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Номер записи: 21
01-08-2013 дата публикации

Novel Benzyl Sulfonamide Derivatives Useful As MOGAT-2 Inhibitors

Номер: US20130197039A1
Автор: Fernandez Maria Carmen, Gonzalez-Garcia Maria Rosario, Pfeifer Lance Allen
Принадлежит: ELI LILLY AND COMPANY

The present invention provides compounds of Formula below: 2. A compound according to wherein R1 is —CH.3. A compound according to wherein R1 is —CF.4. A compound according to claim 1 , wherein R2 is selected from: H claim 1 , —CH claim 1 , —CHOCH.5. A compound according to wherein R2 is H.6. A compound according to wherein R3 is selected from: H claim 1 , —CH claim 1 , —CHOCH claim 1 , and —CHOCHCH.7. A compound according to wherein R3 is selected from: H claim 6 , —CHOCH claim 6 , and —CHOCHCH.8. A compound according to wherein R3 is —CHOCH.9. A compound according to wherein R4 is selected from: H and F.10. A compound according to wherein R4 is F.11. A compound according to wherein R5 is H.12. A compound according to wherein A is selected from CH or CF.13. A compound according to wherein A is N.14. A compound according to wherein X is CF or N.15. A compound according to wherein X is CH.16. A compound of according to wherein the pharmaceutically acceptable salt is a hydrogen chloride addition salt.17. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one of a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , or excipient.19. A compound which is N-[(1S)-2 claim 1 ,2 claim 1 ,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-methoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide hydrochloride.20. A pharmaceutical composition comprising N-[(1S)-2 claim 1 ,2 claim 1 ,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-ethoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one of a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , or excipient.21. A compound which is N-[(1S)-2 claim 1 ,2 claim 1 ,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-ethoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide hydrochloride salt in crystalline form ...

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Номер записи: 22
01-08-2013 дата публикации

METHYLIDENE MALONATE PROCESS

Номер: US20130197264A1
Автор: Gondi Vijaya Bhasker, Reid John Gregory
Принадлежит: OptMed, Inc.

An improved process for the production of methylidene malonates is attained by use of select iminium salt reactants. 2. The method of wherein R claim 1 , R claim 1 , Rand Rare each independently H or an alkyl claim 1 , aryl claim 1 , alkenyl or alkynyl.3. The method of wherein X is a halogen claim 1 , a non-nucleophilic anion claim 1 , and/or acidic anion.4. The method of wherein X is a halogen claim 1 , a carboxylate or a sulfonate.5. The method of wherein X is selected from chloride claim 1 , bromide claim 1 , iodide claim 1 , AsF claim 1 , SbF claim 1 , PF claim 1 , BF claim 1 , CHSO claim 1 , CFSO claim 1 , benzenesulfonate claim 1 , para-toluenesulfonate claim 1 , acetate claim 1 , propionate claim 1 , isobutyrate claim 1 , pivalate claim 1 , sufate claim 1 , bisulfate claim 1 , perchlorate claim 1 , SbCl claim 1 , SbCl claim 1 , and SnCl7. The method of wherein Rand Rare both hydrocarbon and/or heterohydrocarbon groups and represent a Cto Clinear or branched alkyl group claim 6 , a Cto Calicyclic group claim 6 , a Cto Calkenyl group claim 6 , or a Cto Calkynyl group claim 6 , either or both of which may be substituted with or contain an ether claim 6 , epoxide claim 6 , halo claim 6 , ester claim 6 , cyano claim 6 , aldehyde claim 6 , keto or aryl group.8. The method of wherein both Rand Rare hydrocarbon or heterohydrocarbon groups wherein at least one contains an ester linkage.11. The method of wherein Ris independently a Cto Clower alkyl and n is 1 or 2.12. The method of wherein the equivalent weight of iminium salt to malonic acid ester is from 1:1 to 10:1.13. The method of wherein the equivalent weight of iminium salt to malonic acid ester is from 1:1 to 6:1.14. The method of wherein the equivalent weight of iminium salt to malonic acid ester is from 1:1 to 4:1.15. The method of wherein the iminium salt is formed in-situ and the malonic acid ester is directly added to the iminium reaction product.16. The method of wherein the in-situ reaction involves an ...

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Номер записи: 23
15-08-2013 дата публикации

MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR

Номер: US20130211045A1
Автор: Marsault Éric, St-Louis Carl
Принадлежит: TRANZYME PHARMA INC.

The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders. 2. The pharmaceutically acceptable salt of claim 1 , wherein the salt is an amorphous form.3. The pharmaceutically acceptable salt of claim 1 , wherein the salt is a crystalline form.4. The pharmaceutically acceptable salt of claim 1 , wherein the salt is a hydrochloride claim 1 , hydrobromide or hydroiodide salt.5. The pharmaceutically acceptable salt of claim 1 , wherein the salt is the hydrochloride salt.7. The process of further comprising:(a) dissolving the precipitated salt from (d) in a hot mixture of an alcohol and water to form solution C;(b) cooling solution C; and(c) separating a precipitated salt from solution C.8. The process of claim 6 , wherein the alcohol is ethanol.9. The process of claim 6 , wherein the acid is hydrochloric acid.10. The process of claim 6 , wherein the precipitated salt is an amorphous form.11. The process of claim 6 , wherein the precipitated salt is the hydrochloride salt.12. The process of claim 7 , wherein the alcohol is ethanol.13. The process of claim 7 , wherein the precipitated salt is a crystalline form.14. The process of claim 7 , wherein the precipitated salt is the hydrochloride salt.15. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) a ...

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Номер записи: 24
29-08-2013 дата публикации

SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN

Номер: US20130225621A1
Автор: Gunning Patrick, Turkson James
Принадлежит:

In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 5. The compound of claim 1 , wherein the compound exhibits inhibition of STAT with an ICof less than about 300 μM.6. The compound of claim 1 , wherein the compound exhibits inhibition with an Kof less than about 300 μM.7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of and a pharmaceutically acceptable carrier.12. The method of claim 8 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.13. The method of claim 8 , wherein the disorder is selected from psoriasis and pulmonary arterial hypertension.14. The method of claim 8 , wherein the disorder is a disease of uncontrolled cellular proliferation.15. The method of claim 14 , wherein the disease of uncontrolled cellular proliferation is a cancer selected from cancers of the head claim 14 , neck claim 14 , pancreas claim 14 , brain claim 14 , colon claim 14 , rectum claim 14 , skin claim 14 , ovary claim 14 , kidney claim 14 , prostate claim 14 , breast claim 14 , lung claim 14 , colon claim 14 , uterus claim 14 , and liver.18. The method of claim 16 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.19. The method of claim 16 , wherein the disorder is a disease of uncontrolled cellular proliferation.20. The method of claim 19 , ...

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Номер записи: 25
12-09-2013 дата публикации

Use of Compounds for Inducing Differentiation of Mesenchymal Stem Cells to Chondrocytes

Номер: US20130236969A1
Автор: Han Gyoon Hee, Hwang Ki Chul, Jang Yang Soo
Принадлежит: Industry-Academic Cooperation Foundation, Yonsei University

Use of a compound of Formula 1 for inducing differentiation of mesenchymal stem cells to chondrocytes, and a pharmaceutical composition for treating a cartilage disease, which includes chondrocytes in which differentiation from mesenchymal stem cells is induced by the compound of Formula 1, are provided. Differentiation of the mesenchymal stem cells treated with the compound of Formula 1 to chondrocytes is specifically induced, and thus the compound can be used to effectively treat a cartilage disease such as arthritis, cartilage damage, and a cartilage defect. 2. The method of claim 1 , wherein Rto Rare each independently hydrogen claim 1 , phenyl claim 1 , Calkyl claim 1 , or halogen claim 1 , or Rand Ror Rand Rare joined together to form a pyridine or benzene ring;{'sub': 4', '5', '1-4, 'Rand Rare each independently hydrogen, Calkyl, or halogen;'}{'sub': 6', '3-12', '1-4, 'Ris phenyl, naphthalyl, Ccycloalkyl, or Calkyl substituted with phenyl;'}{'sub': 7', '1-4, 'Ris hydrogen or Calkyl, and'}{'sub': 1', '6', '1-4', '1-4, 'Rto Ris each independently unsubstituted, or further substituted with at least one substituent selected from the group consisting of Calkyl, hydroxyl, hydroxyl Calkyl, nitro, carboxyl, and halogen.'}3. The method of claim 1 , wherein Rand Rare each independently hydrogen claim 1 , or are joined together to form a pyridine ring;{'sub': 3', '1-4', '2, 'Ris hydrogen, phenyl, or Calkyl, or is joined together with Rto form a benzene ring;'}{'sub': 4', '5, 'Rand Rare each independently hydrogen,'}{'sub': 6', '5-10', '1-4, 'Ris phenyl, naphthalyl, Ccycloalkyl, or Calkyl group substituted with phenyl,'}{'sub': 7', '1-4, 'Ris hydrogen or Calkyl, and'}{'sub': 1', '6', '1-4', '1-4, 'Rto Ris each independently unsubstituted, or further substituted with at least one substituent selected from the group consisting of Calkyl, hydroxyl, hydroxyl Calkyl, nitro, carboxyl, and halogen.'}4. The method of claim 1 , wherein the compound of Formula 1 is at least one ...

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Номер записи: 26
12-09-2013 дата публикации

ARYLOXY PHENOXY ACRYLIC COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT

Номер: US20130237542A1
Автор: Chung Kyung Sook, Jin Yinglan, KIM Bo Kyung, KIM Hwan Mook, Lee Chang Woo, Lee Jung Joon, LEE Ki Hoon, Lee Kiho, LEE Kyeong, LEE SEUNG-HEE, Park Song Kyu, Won Mi Sun
Принадлежит:

The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases. 5. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound represented by formula 1 is selected from the group consisting of(E)-3-[3-(4-adamantan-1-yl-phenoxy)-acryloylamino]-benzoic acid methylester,(E)-3-(3-(4-t-butylphenoxy)acrylamido)benzoic acid methylester,(E)-3-(3-(4-(2,4,4-trimethylpentan-2-yl)phenoxy)acrylamido)benzoic acid methylester,(E)-3-(3-(4-adamantan-1-yl-2-methylphenoxy) acrylamido)benzoic acid methylester,(E)-4-(3-(4-adamantan-1-yl-phenoxy)acrylamido)benzoic acid methylester,(E)-3-(4-adamantan-1-yl-phenoxy)-N-(3-sulfamoylphenyl) acrylamide,(E)-3-(4-adamantan-1-ylphenoxy)-N-(3-(methylsulfonyl)phenyl)acrylamide,(E)-5-[3-(4-adamantan-1-yl-phenoxy)-acryloamino]-2-hydroxy-benzoic acid methylester,(E)-3-[3-(4-adamantan-1-yl-phenoxy)-acryloylamino]-benzoic acid,(E)-3-(3-(4-adamantan-1-yl-phenoxy)acrylamido)benzoic acid ethylester,(E)-3-(3-(4-adamantan-1-ylphenoxy)acrylamido)benzoic acid 2-methoxyethylester,(E)-3-(3-(4-adamantan-1-yl-phenoxy)acrylamido) ...

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Номер записи: 27
19-09-2013 дата публикации

Aryl-Phenyl-Sulfonamido-Cycloalkyl Compounds and Their Use

Номер: US20130245018A1
Автор: "Van t Hof Robert Jurgen", Clase Juha Andrew, Fisher Raymond, Greig Iain Robert, Sheridan Rose Mary, Smith Andrew, Tozer Matthew John, Tuffnell Andrew Robert
Принадлежит: PIMCO 2664 LIMITED

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. 1289-. (canceled)291. A compound according to claim 290 , wherein ═W— is —CH═ and —Y═ is —CH═.292. A compound according to claim 290 , wherein ═W— is —CH═ and —Y═ is —N═.293. A compound according to claim 291 , wherein -Dis cyclohexane-1 claim 291 ,4-di-yl.294. A compound according to claim 292 , wherein -Dis cyclohexane-1 claim 292 ,4-di-yl.295. A compound according to claim 291 , wherein -Dis 4-methyl-cyclohexane-1 claim 291 ,4-di-yl;296. A compound according to claim 292 , wherein -Dis 4-methyl-cyclohexane-1 claim 292 ,4-di-yl;297. A compound according to claim 293 , wherein —Ris —F; and —Ris —F.298. A compound according to claim 294 , wherein —Ris —F; and —Ris —F.299. A compound according to claim 295 , wherein —Ris —F; and —Ris —F.300. A compound according to claim 296 , wherein —Ris —F; and —Ris —F.301. A compound according to claim 293 , wherein —Ris —Cl; and ...

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Номер записи: 28
26-09-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130252984A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris 4-chloro-3-trifluoromethylphenyl;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and,'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris 4-chloro-3-trifluoromethylphenyl;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris halogen or Calkyl; and,'}{'sup': '8', 'Ris H.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris benzyl, methyl-4-benzoic acid, tert-butyl 2-(4-methylbenzamido)acetate, tert-butyl 2-(4-methyl benzamido)acetic acid, methyl-3-methylbenzoate, 4-methyl-N-(2-(pyrrolidin-1-yl)ethyl)benzamide, 4-methyl-N-(2-(1-oxipyrrolidin-1-yl)ethyl)benzamide, 3-methyl-N-(2-(pyrrolidin-1-yl)ethyl)benzamide, methyl-2-methylbenzoate, methyl-2-benzoic acid, N,N- ...

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Номер записи: 29
26-09-2013 дата публикации

Method of Treating Skin with microRNA Modulators

Номер: US20130253053A1
Автор: Khusial Permanan Raaj, Lyga John W., Santhanam Uma
Принадлежит: AVON PRODUCTS, INC.

Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that suppress or down-regulate microRNA expression in dermal fibroblast, resulting in enhanced production of collagen, elastin and/or fibrillin in the skin. Also provided are methods for screening for activity against specific microRNAs and the methods of using active agents identified by the screening protocol in the treatment of skin. 2. The method according to claim 1 , wherein said active agent suppresses miR-29a.3. The method according to claim 1 , wherein said active agent suppresses miR-29b.4. The method according to claim 1 , wherein said active agent suppresses miR-29a and miR-29b.5. The method according to claim 1 , wherein R claim 1 , when not hydrogen claim 1 , is alkyl claim 1 , aryl claim 1 , arylalkyl claim 1 , or alkylaryl.6. The method according to claim 5 , wherein Ris hydrogen.7. The method according to claim 1 , wherein R claim 1 , Rand Rare independently a group R claim 1 , where R is selected from alkyl claim 1 , aryl claim 1 , arylalkyl claim 1 , and alkylaryl claim 1 , each being optionally substituted with 1-12 heteroatoms selected from halogen claim 1 , O claim 1 , N and S.8. The method according to claim 1 , wherein Ris a Cto Calkyl.9. The method of claim 5 , wherein Rand Rindependently is a C1 to C4 alkyl or phenyl claim 5 , and Ris hydrogen or a Cto Calkyl.11. The method according to claim 1 , wherein said aesthetic improvement of said skin is selected from the group consisting of:(a) treatment, reduction, and/or prevention of fine lines or wrinkles,(b) reduction of skin pore size,(c) improvement in skin thickness, plumpness, and/or tautness;(d) improvement in skin suppleness and/or softness;(e) improvement in skin tone, radiance, and/or clarity;(f) improvement in maintenance and remodeling of elastin;(g) improvement in skin texture and/or promotion of retexturization;(h) improvement in skin barrier repair and/or ...

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Номер записи: 30
17-10-2013 дата публикации

METHODS AND COMPOSITIONS FOR DIAGNOSING AND TREATING MUSCLE MYOPATHY DISORDERS

Номер: US20130273181A1
Автор: HANSON MARTIN GARTZ, NISWANDER LEE
Принадлежит:

Embodiments herein generally relate to methods and compositions for diagnosing and treating congenital muscle diseases (e.g. muscle myopathy disorders). In certain embodiments, methods and compositions generally relate to treating a subject having a muscle myopathy disorder with a dietary supplement and/or sulfonylurea agent. 1. A method for treating a muscle myopathy disorder in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a sulfonylurea agent or an agent that inhibits sulfonylurea receptor 1 (SUR1) and treating the muscle myopathy disorder in the subject.2. The method of claim 1 , wherein the sulfonylurea agent is selected from the group consisting of Carbutamide claim 1 , Acetohexamide claim 1 , Chlorpropamide claim 1 , Tolbutamide claim 1 , Tolazamide claim 1 , Glipizide claim 1 , Gliclazide claim 1 , Glyburide (also known as Glibenclamide) claim 1 , Glibornuride claim 1 ,Gliquidone, Glisoxepide, Glyclopyramide, and Glimepiride.3. The method of claim 1 , wherein the sulfonylurea agent is Glyburide.4. The method of claim 1 , wherein the sulfonylurea agent is administered orally to the subject.5. The method of claim 4 , wherein the sulfonylurea agent is administered at about 0.1 mg to about 10 mg.6. The method of claim 1 , wherein myopathy disorders comprise any muscle myopathy disorder claim 1 , any congenital muscle myopathy disorder claim 1 , central core disease (CCD) claim 1 , multi mini core disease claim 1 , hypokalemic periodic paralysis claim 1 , nemaline myopathy claim 1 , myotubular myopathy claim 1 , centronuclear myopathy claim 1 , congenital fiber-type disproportion myopathy claim 1 , hyaline body myopathy and malignant hyperthermia (MH).7. The method of claim 1 , wherein the muscle myopathy comprises central core disease (CCD).8. A method for assessing presence of a muscle myopathy disorder in a subject comprising:a. analyzing a muscle sample obtained from the subject for expression levels ...

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Номер записи: 31
17-10-2013 дата публикации

PROCESS AND INTERMEDIATES FOR PREPARING MACROLACTAMS

Номер: US20130274463A1
Автор: Chen Cheng, Dolman Sarah, Humphrey Guy, Kong Jongrock, Li Hongmei, Tudge Matthew T., Xiang Bangping, Yong Kelvin, Zacuto Michael
Принадлежит:

The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof. 7. The method of claim 6 , wherein Ris Calkyl and Ris a H or Calkyl.10. The method of claim 9 , wherein said Step C coupling is performed using EDC and pyridine or a pyridine derivative.13. The method of claim 8 , wherein Ris either H or Calkyl.17. The method of claim 13 , wherein Ris either H or Calkyl.19. The method of claim 8 , wherein said ring closure is performed by slow addition of catalyst and the compound of Formula IIa to a solvent at approximately the same time claim 8 , wherein:said solvent is provided at about 5-25 liters per Kg of substrate;said catalyst is provided at a concentration of about 250 ml to 3 L per Kg of catalyst;said compound is provided at a concentration of about 500 ml to 6 L per Kg of substrate; andsaid compound-solution, said catalyst-solution and said solvent are combined together over a period of 0.5-2.5 hrs.2122-. (canceled) The present invention relates to method and compounds that can be used to produce macrolactams, and modify macrolactams. One use of the methods and compounds described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity.Hepatitis C virus (HCV) infection is a major health problem that leads to chronic liver disease, such as cirrhosis and hepatocellular carcinoma, in a substantial number of infected individuals. Current treatments for HCV infection include immunotherapy with recombinant interferon-α alone or in combination with the nucleoside analog ribavirin. Several virally-encoded ...

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Номер записи: 32
31-10-2013 дата публикации

Substituted pyridines having herbicidal activity

Номер: US20130288899A1
Автор: Andree Van Der Kloet, Gilbert Besong, Helmut Kraus, Jens Lerchl, Johannes Hutzler, Klaus Grossmann, Klaus Kreuz, Liliana Parra Rapado, Matthias Witschel, Michael Rack, Richard Roger Evans, Ruediger Reingruber, Thomas Seitz, Trevor William Newton, William Karl Moberg
Принадлежит: BASF SE

The present invention provides substituted pyridine compounds of the formula I or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridines of formula I are useful as herbicides.

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Номер записи: 33
14-11-2013 дата публикации

SYNTHESIS OF METHYLENE MALONATES SUBSTANTIALLY FREE OF IMPURITIES

Номер: US20130303719A1
Автор: Chen Yangbin, Dey Tanmoy, Malofsky Bernard M., Malofsky Bernard Miles, Sullivan Jeffrey M., Wojciak Stanley C.
Принадлежит: BIOFORMIX, LLC

The present invention provides improved methods for the chemical synthesis of methylene malonates using the Knovenagel synthesis reaction. The method of the invention provides for improved methylene malonates by significantly reducing or eliminating the formation of alternative and/or deleterious side products, significantly reducing or eliminating unwanted consumption of methylene malonates, and significantly reducing or eliminating the degradation of methylene malonates. These advantages result in methylene malonates, which upon recovery, are of higher quality, greater purity, improved yield and possess overall improved performance characteristics (e.g., improved cure speed, retention of cure speed, improved shelf-life and/or stability). 158-. (canceled)59. A method of making a methylene malonate monomer comprising:(a) reacting a malonic acid ester with a source of formaldehyde in the presence of an acidic or basic catalyst and optionally in the presence of an acidic or non-acidic solvent, to form a reaction complex;(b) optionally, inactivating the catalyst; and(c) recovering methylene malonate monomer from the reaction complex.60. The method according to claim 59 , wherein inactivating the catalyst comprises forming an insoluble precipitate of the catalyst and removing the precipitate from the reaction mixture.61. The method according to claim 60 , wherein the precipitate is formed by reducing the solubility of the catalyst in the reaction mixture.62. The method according to further comprising:(d) minimizing the recovery of volatile latent acid forming impurities from the reaction complex.63. The method according to claim 62 , wherein the step of minimizing the recovery of volatile latent acid forming impurities comprises:(a) adding to the reaction mixture water and an acid having a pKa range of −8 to 5;(b) adding to the reaction mixture a sterically hindered organic acid; or(c) adding to the reaction mixture a non-volatile organic acid,or any combination of (a), ...

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Номер записи: 34
21-11-2013 дата публикации

Sulfonamide-Containing Compounds

Номер: US20130310384A1
Автор: Augelli-Szafran Corinne E., Lu Dai, Selkoe Dennis J., Wei Hanxun, Wolfe Michael S., Zhang Jing
Принадлежит: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.

This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of γ-secretase. 2. The compound of claim 1 , wherein W claim 1 , W claim 1 , W claim 1 , and Ware defined according to definition (A).3. (canceled)4. The compound according to claim 1 , wherein each of W claim 1 , W claim 1 , W claim 1 , and Wis CH.512-. (canceled)13. The compound according to claim 1 , wherein Ris selected from —COH; —C(O)OR; —NHC(O)OR; —N(CH)C(O)OR; —C(O)N(R)(R); —C(O)R; —CN; and —SO(R).14. The compound according to claim 13 , wherein Ris —COH.15. The compound according to claim 13 , wherein Ris —COR.16. (canceled)17. The compound according to claim 13 , wherein Ris —SO(R).18. (canceled)19. The compound according to claim 13 , wherein Ris —C(O)N(R)(R).2027-. (canceled)28. The compound of claim 1 , wherein Ris C-Caryl claim 1 , which is optionally substituted with from 1-3 independently selected R.29. The compound of claim 28 , wherein Ris phenyl claim 28 , which is optionally substituted with from 1-3 independently selected R.30. The compound of claim 29 , wherein claim 29 , Ris unsubstituted phenyl.31. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , which is optionally substituted with a substituent selected from —OH and —CN.32. The compound of claim 31 , wherein Ris —CHCHor —CH.3338-. (canceled)39. The compound according to claim 1 , wherein the carbon attached to Rand Rhas the S configuration.40. The compound according to claim 1 , wherein Ris C-Caryl claim 1 , which is optionally substituted with from 1-3 independently selected R.41. (canceled)42. The compound of claim 40 , wherein Ris 4-chloro-phenyl claim 40 , 4-fluoro-phenyl claim 40 , or 2 claim 40 ,4-difluorophenyl.4346-. (canceled)47. The compound according to claim 1 , wherein A is CH.48. A pharmaceutical composition comprising a compound of formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , as claimed in claim 1 , and a pharmaceutically ...

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Номер записи: 35
05-12-2013 дата публикации

PREPARATION METHOD FOR FLUORINE-CONTAINING OLEFINS HAVING ORGANIC-GROUP SUBSTITUENTS

Номер: US20130324757A1
Автор: Adachi Kenji, NAGAI Takabumi, OGOSHI Sensuke, OHASHI Masato, Shibanuma Takashi
Принадлежит:

An object of the present invention is to provide a method that enables the easy and efficient (high yield, high selectivity, low cost) preparation of a fluorine-containing olefin substituted with an organic group or groups from a fluorine-containing olefin. 1. A method for preparing a fluorine-containing olefin substituted with an organic group or groups ,the method comprising a step of reacting a fluorine-containing olefin (excluding chlorotrifluoroethylene) with an organic boron compound in the presence of an organic transition metal catalyst containing at least one transition metal selected from the group consisting of nickel, palladium, platinum, rhodium, ruthenium, and cobalt.2. The method according to claim 1 , wherein the fluorine-containing olefin is an olefin substituted with one or more fluorine atoms.3. The method according to claim 1 , wherein the transition metal is at least one member selected from the group consisting of nickel and palladium.5. The method according to claim 4 , wherein R is an optionally substituted monocyclic claim 4 , bicyclic claim 4 , or tricyclic aryl.6. The method according to claim 4 , wherein at least one of fluorine atoms claim 4 , each of which is bonded to an sphybridized carbon atom of the fluorine-containing olefin claim 4 , is substituted with a group represented by R.7. The method according to claim 1 , wherein the step is performed in the presence of a base.8. The method according to claim 1 , wherein the step is performed in the absence of a base.9. The method according to claim 1 , wherein the organic transition metal catalyst is an organic nickel complex.10. The method according to claim 1 , wherein the organic transition metal catalyst is an organic palladium complex. The present invention relates to a method for preparing a fluorine-containing olefin substituted with an organic group or groups.1-Substituted fluorine-containing olefins, such as 1,1,2-trifluorostyrene, are useful for, for example, polyelectrolyte ...

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Номер записи: 36
12-12-2013 дата публикации

HERBICIDAL COMPOSITION

Номер: US20130331264A1
Автор: Okamoto Hiroyuki, Terada Takashi, Yamada Ryu
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

Many herbicidal compositions have been developed and are presently used. However, weeds to be controlled are various in types and their emergence extends over a long period. Accordingly, it is desired to develop a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long lasting effect. The present invention provides a herbicidal composition comprising, as active ingredients, (a) flazasulfuron or its salt, and (b) amicarbazone or its salt. 1. A herbicidal composition comprising , as active ingredients , (a) flazasulfuron or its salt , and (b) amicarbazone or its salt.2. A method for controlling noxious plants , which comprises applying a herbicidally effective amount of a herbicidal composition comprising , as active ingredients , (a) flazasulfuron or its salt , and (b) amicarbazone or its salt , to the noxious plants or to a place where they grow3. A method for controlling noxious plants , which comprises applying a herbicidally effective amount of (a) flazasulfuron or its salt , and a herbicidally effective amount of (b) amicarbazone or its salt , to the noxious plants or to a place where they grow.4. The composition according to claim 1 , wherein the mixing ratio of (a) to (b) is from 1:2 claim 1 ,000 to 5:1 claim 1 , by the weight ratio.5. The method according to claim 2 , wherein (a) is applied in an amount of from 2 to 250 g/ha claim 2 , and (b) is applied in an amount of from 50 to 4 claim 2 ,000 g/ha.6. The method according to claim 2 , wherein the noxious plants are weeds having sensitivity to a sulfonylurea type compound lowered.7. The method according to claim 2 , wherein the noxious plants are convolvulaceae claim 2 , cyperaceae or gramineae.8. The method according to claim 3 , wherein (a) is applied in an amount of from 2 to 250 g/ha claim 3 , and (b) is applied in an amount of from 50 to 4 claim 3 ,000 g/ha.9. The method according to claim 3 , wherein the noxious plants are weeds having sensitivity to a sulfonylurea type ...

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Номер записи: 37
12-12-2013 дата публикации

METHOD FOR CONTROLLING WEEDS IN PADDY RICE CULTIVATION

Номер: US20130331266A1
Автор: IKEDA Hajime, Inaba Junko
Принадлежит: Sumitomo Chemical Company, Limited

The present invention provides a method for controlling weeds in paddy rice cultivation, which comprises steps of: 1. A method for controlling weeds in paddy rice cultivation , which comprises steps of:after sowing paddy rice seeds or transplanting paddy rice plants in a paddy field, applying a water-diluted solution comprising one or more herbicidal compounds selected from the group consisting of1-(2-chloro-6-propylimidazo[1,2-b]pyridazin-3-ylsulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea,(RS)-2′-[(4,6-dimethoxypyrimidin-2-yl)(hydroxy)methyl]-1,1-difluoro-6′-(methoxymethyl)methanesulfonanilide,1-{3-chloro-1-methyl-4-[(5RS)-5,6-dihydro-5-methyl-1,4,2-dioxazin-3-yl]pyrazol-5-ylsulfonyl}-3-(4,6-dimethoxypyrimidin-2-yl)urea, and2′-[(4,6-dimethoxy-1,3,5-triazin-2-yl)carbonyl]-1,1,6′-trifluoro-N-methylmethanesulfonanilideto the weeds or the paddy field where weeds grow or are to emerge; andflooding the paddy field within the first week after the application of the herbicidal compound.2. A method for controlling weeds in paddy rice cultivation , which comprises steps of:after sowing paddy rice seeds or transplanting paddy rice plants in a paddy field, applying a water-diluted solution comprising one or more herbicidal compounds selected from the group consisting of1-(2-chloro-6-propylimidazo[1,2-b]pyridazin-3-ylsulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea,(RS)-2′-[(4,6-dimethoxypyrimidin-2-yl)(hydroxy)methyl]-1,1-difluoro-6′-(methoxymethyl)methanesulfonanilide,1-{3-chloro-1-methyl-4-[(5RS)-5,6-dihydro-5-methyl-1,4,2-dioxazin-3-yl]pyrazol-5-ylsulfonyl}-3-(4,6-dimethoxypyrimidin-2-yl)urea, and2′-[(4,6-dimethoxy-1,3,5-triazin-2-yl)carbonyl]-1,1,6′-trifluoro-N-methylmethanesulfonanilide,to the weeds or the paddy field where weeds grow or are to emerge; andflooding the paddy field until the first three days after the application of the herbicidal compound.3. A method for controlling weeds in paddy rice cultivation , which comprises steps of:after sowing paddy rice seeds or ...

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Номер записи: 38
12-12-2013 дата публикации

CLASS II HMG-COA REDUCTASE INHIBITORS AND METHODS OF USE

Номер: US20130331450A1
Автор: JR. Calvin Nicklaus, Lipton Mark Alfred, Rodwell Victor W., Saleem Mohamed Naguieb, Schmidt Tim Jonathan, Stauffacher Cynthia, Steussy
Принадлежит: PURDUE RESEARCH FOUNDATION

Disclosed are compositions and methods for treating bacterial infections. 2. The inhibitor of claim 1 , wherein Ror Ris a linear or branched alkyl having from to 14 carbon atoms.3. The inhibitor of claim 1 , wherein Ris OH.4. The inhibitor of claim 1 , wherein Ris —O—(CO)NHor —OCH(CO)NH.5. The inhibitor of claim 1 , wherein Ris —OCH(CO)NH.6. The inhibitor of claim 1 , wherein A claim 1 , B claim 1 , D and E are part of a benzene ring structure.7. The inhibitor of selected from 2f claim 1 , 2l claim 1 , 2j claim 1 , and 2e claim 1 , and pharmaceutically acceptable salts thereof.8. An inhibitor according to claim 1 , the inhibitor having antimicrobial activity against one or more bacterial or fungal pathogens.9. The inhibitor of claim 1 , wherein the bacterial pathogen is a Gram-positive pathogen.10Bacillus anthracis, Bacillus subtilis, Bacillus cereus, Listeria monocytogenes, Brucella abortus, Candida albicans, Staphylococcus aureus, Enterococcus faecalisStreptococcus pneumoniae.. The inhibitor of claim 8 , wherein the pathogen is selected from the group consisting of and11. The inhibitor according to claim 8 , wherein the pathogen is resistant to vancomycin and/or methicillin.12. An inhibitor according to claim 1 , wherein the inhibitor exhibits no toxicity or low toxicity toward mammalian cells.13. An pharmaceutical composition comprising:a pharmaceutically acceptable excipient; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound according to or 5-(N-(4-butylphenyl)sulfamoyl)-2-hydroxybenzoic acid.'}14. A method of treating a multicellular organism infected with a bacterial or fungal pathogen comprising administering to the organism the pharmaceutical composition of in an amount effective to kill or inhibit growth of the pathogen.15. The method of claim 14 , wherein the organism is a human.16. A biocide comprising:a diluent; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound according to or 5-(N-(4-butylphenyl)sulfamoyl)-2-hydroxybenzoic ...

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Номер записи: 39
12-12-2013 дата публикации

INHIBITORS OF VIRAL ENTRY INTO MAMMALIAN CELLS

Номер: US20130331456A1
Автор: Basu Arnab, Bowlin Terry L., Li Bing, Mills Debra M., Peet Norton P., Williams John D.
Принадлежит:

The present invention is related to the development of compounds and methods for inhibiting viral infection in a mammal. A pseudotype virus was developed for use in a high throughput assay for identifying nonpeptidic small molecule inhibitors that prevent viral entry into a host cell. 2. The method according to claim 1 , wherein said compound if effective to inhibit viral entry into a host cell.3. The method according to claim 1 , wherein said pharmaceutically acceptable carrier or excipient is selected from binding agents claim 1 , fillers claim 1 , lubricants claim 1 , disintegrants claim 1 , wetting agents claim 1 , suspending agents claim 1 , emulsifying agents claim 1 , non-aqueous vehicles claim 1 , and preservatives.4. The method according to claim 1 , wherein said compound is effective to inhibit influenza infection.5. The method according to claim 4 , wherein said influenza is avian influenza.6. The method according to claim 5 , wherein said avian influenza is the H5N1 subtype.7. The method according to claim 1 , wherein said compound is effective to inhibit ebola infection.8. The method according to claim 1 , wherein said compound is effective to inhibit vesicular stomatitis virus infection.9. The method according to claim 1 , wherein said mammal is a human.10. The method according to claim 1 , wherein said composition is administered via a route selected from intradermally claim 1 , transdermally claim 1 , intramuscularly claim 1 , intraperitoneally claim 1 , intravenously claim 1 , or orally.11. The method according to claim 10 , wherein said composition is administered orally.12. The method of claim 11 , wherein said oral administration is selected from the group consisting of a tablet claim 11 , gelatin capsule claim 11 , microcapsule claim 11 , and liquid formula.14. The composition according to claim 13 , wherein said compound is effective to inhibit viral entry into a host cell.15. The composition according to claim 13 , wherein said ...

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Номер записи: 40
12-12-2013 дата публикации

PRODUCTION PROCESS FOR FLUOROSULFONYLIMIDE AMMONIUM SALT

Номер: US20130331609A1
Автор: Aiura Yasuyuki, Maruyama Michiaki, SUZUKI Toru, Tsubokura Shiro
Принадлежит: NIPPON SODA CO., LTD.

A compound [II] such as ammonium N,N-di(fluorosulfonyl)imide is obtained by reacting a compound [I] such as N,N-di(chlorosulfonyl)imide and NHF (HF). A compound [IV] such as an N,N-di(fluorosulfonyl)imide alkali metal salt is obtained by reacting the obtained compound [II] and an alkali metal compound or the like. 3. The process for producing a fluorosulfonylimide salt according to claim 2 , wherein the at least one compound is selected from the group consisting of alkali metal compounds claim 2 , onium compounds and organic amine compounds. The present invention relates to a process for producing a fluorosulfonylimide ammonium salt. More specifically, the present invention relates to a process for producing a fluorosulfonylimide ammonium salt with good efficiency and maximum suppression of the contamination of metal impurities that degrade electrolyte properties and the like.Priority is claimed on Japanese Patent Application No. 2011-046738, filed Mar. 3, 2011, the content of which is incorporated herein by reference.Fluorosulfonylimide salts are useful compounds in a wide variety of fields, and are used as electrolytes, as additives added to the electrolytes of fuel cells, and as selective electron withdrawing materials and the like (see Patent Document 1). Fluorosulfonylimide alkali metal salts and various fluorosulfonylimide onium salts can be obtained by cation exchange reactions using an alkali metal compound or an onium compound. Fluorosulfonylimide ammonium salts are useful as production intermediates for fluorosulfonylimide alkali metal salts and fluorosulfonylimide onium salts other than ammonium salts.Various methods have been proposed for synthesizing fluorosulfonylimide ammonium salts. For example, Non-Patent Document 1 discloses a method of synthesizing a di(fluorosulfonyl)imide ammonium salt from di(fluorosulfonyl)imide and ammonia.Patent Document 2 discloses a method of synthesizing a bis[di(fluorosulfonyl)imide] onium salt by reacting di( ...

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Номер записи: 41
12-12-2013 дата публикации

Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates

Номер: US20130331610A1
Автор: Anglada Luis, Guglietta Antonio, Palomer Albert
Принадлежит: Ferrer Internacional, S.A.

The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves. 2. The process of wherein the hydride compound is sodium hydride and Z is iodine.6. An intermediate enaminone compound which is selected from the group consisting of:N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide;N-[2-chloro-5-(3-dimethylamino-acryloyl)-phenyl]-N-methyl-acetamide;N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-methanesulfonamide;N-[2-chloro-5-(3-dimethylamino-acryloyl)-phenyl]-N-methyl-methanesulfonamide; andN-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-prop-2-ynyl-methanesulfonamide. This application is a Divisional Application of U.S. patent application Ser. No. 11/922,602, filed Apr. 30, 2009, which is the U.S. National Phase of PCT/EP2006/063243, filed Jun. 15, 2006, which claims benefit of Provisional Application No. 60/692,866 filed on Jun. 21, 2005. This application also claims priority under 35 U.S.C. §119(a) to European Patent Application No. 05105478.1, filed in Europe on Jun. 21, 2005, the entire contents of which are hereby incorporated by reference.This invention is directed to agents with affinity for GABAreceptor, specifically to halogenated pyrazolo[1,5-a]pyrimidines, and more specifically to [7-(3-amino-4-halophenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]-thiophen-2-yl-methanone acyl and sulfonyl compounds.GABAreceptor (γ-aminobutyric acid) is a pentameric protein which forms a membrane ion channel. GABAreceptor is implicated in the regulation of sedation, anxiety, muscle tone, epileptogenic ...

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Номер записи: 42
02-01-2014 дата публикации

Liquid sulfonylurea herbicide formulations

Номер: US20140005051A1
Автор: George B. Beestman, James J. Reap
Принадлежит: EI Du Pont de Nemours and Co

Disclosed are single liquid-phase herbicide compositions comprising by weight, from 0.1 to 20% of one or more sulfonylurea herbicides, from 0 to 40% of one or more biologically active agents other than sulfonylurea herbicides, from 0.1 to 20% of one or more lignosulfonates, from 0 to 99.8% of one or more fatty acid esters of C 1 -C 4 alkanols, and from 0 to 50% of one or more additional formulating ingredients.

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Номер записи: 43
09-01-2014 дата публикации

POLYMERIZABLE MONOMER, POLYMERIC COMPOUND, CHARGE CONTROL AGENT CONTAINING THE POLYMERIC COMPOUND, AND DEVELOPER BEARING MEMBER AND TONER WHICH CONTAIN THE CHARGE CONTROL AGENT

Номер: US20140011129A1
Автор: Hirose Masashi, Inoue Kei, Murai Yasuaki, Murayama Ryuji, Sato Kazuyuki
Принадлежит: CANON KABUSHIKI KAISHA

A polymerizable monomer is provided which is represented by the following formula (1): 4. The polymeric compound according to claim 3 , wherein the unit represented by the formula (4) is a styrene derivative unit or an acrylate derivative unit.5. The polymeric compound according to claim 2 , which has a weight-average molecular weight of from 3 claim 2 ,000 to 100 claim 2 ,000.6. A charge control agent comprising the polymeric compound according to .7. A developer bearing member comprising in a surface layer thereof the charge control agent according to .8. A toner comprising a binder resin claim 6 , a colorant and the charge control agent according to .9. The toner according to claim 8 , which is produced by a suspension polymerization process.10. The toner according to claim 8 , which is produced by a suspension granulation process. The present invention relates to a novel polymerizable monomer having a salicylic acid unit, and a polymeric compound produced by polymerizing the same. The present invention also relates to a charge control agent used in recording methods making use of electrophotography or the like, and a developer bearing member and a toner which contain the same.In image forming methods as typified by an electrophotographic recording method, a developer charged electrostatically (hereinafter “toner”) flies to the surface of a photosensitive member by electrostatic force which accords with potential differences on the photosensitive member surface, and develops electrostatic latent images formed on the photosensitive member surface. Hence, it is necessary and indispensable to control charge characteristics of the toner. Then, as a method for providing the toner with proper charge characteristics, a method is known in which a binder resin of a developer bearing member (hereinafter also “developing roller”) is incorporated with a charge control agent or a method in which a charge control agent capable of providing the toner with positive charges or ...

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Номер записи: 44
09-01-2014 дата публикации

NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Номер: US20140011881A1
Автор: Choi Jin Kyu, Jeong Yeon Su, Kim Jin Kwan, KIM Sun-Young, KOH Hyun-Ju, LEE Ki-Wha, Lim Kyung Min, MOH Joo-Hyun, PARK Young-ho, Shin Song Seok, WOO Byoung young
Принадлежит: AMOREPACIFIC CORPORATION

This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. 115-. (canceled)17. The pharmaceutical composition according to claim 16 , for preventing or treating a condition associated with the pathological stimulation and/or aberrant expression of vanilloid receptors.18. The pharmaceutical composition according to claim 16 , for treating a condition selected from the group consisting of pain claim 16 , inflammatory disease of the joints claim 16 , neuropathies claim 16 , HIV-related neuropathy claim 16 , nerve injury claim 16 , neurodegeneration claim 16 , stroke claim 16 , urinary bladder hypersensitivity including urinary incontinence claim 16 , cystitis claim 16 , stomach duodenal ulcer claim 16 , irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD) claim 16 , fecal urgency claim 16 , gastro-esophageal reflux disease (GERD) claim 16 , Crohn's disease claim 16 , asthma claim 16 , chronic obstructive pulmonary disease claim 16 , cough claim 16 , neurotic/allergic/inflammatory skin disease claim 16 , psoriasis claim 16 , pruritus claim 16 , prurigo claim 16 , irritation of skin claim 16 , eye or mucous membrane claim 16 , hyperacusis claim 16 , tinnitus claim 16 , vestibular hypersensitivity claim 16 , episodic vertigo claim 16 , cardiac diseases such as myocardial ischemia claim 16 , hair growth-related disorders such as effluvium claim 16 , alopecia claim 16 , rhinitis claim 16 , and pancreatitis.19. The pharmaceutical composition according to claim 18 , wherein the pain is or is associated with a condition selected from the group consisting of osteoarthritis claim 18 , rheumatoid arthritis claim 18 , ankylosing spondylitis claim 18 , diabetic neuropathic pain claim 18 , post-operative pain claim 18 , dental pain claim 18 , non-inflammatory musculoskeletal pain (including ...

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Номер записи: 45
09-01-2014 дата публикации

COMPOUND

Номер: US20140012028A1
Автор: Kawata Ken, Nakata Hiyoku, WATANABE Saisuke
Принадлежит: FUJIFILM Corporation

A compound represented by following formula (I): A-L-{D-(E)-D-(B)—Z—R}. In the formula, A represents a p-valent chain or cyclic residue; L represents a single bond or a divalent linking group; p represents an integer of 2 or more; Drepresents a carbonyl group (—C(═O)—) or a sulfonyl group (—S(═O)—); Drepresents a carbonyl group (—C(═O)—), a sulfonyl group (—S(═O)—), a carboxyl group (—C(═O)O—), a sulfonyloxyl group (—S(═O)O—), a carbamoyl group (—C(═O)N(Alk)-) or a sulfamoyl group (—S(═O)N(Alk)-); E represents a divalent group; and R represents a hydrogen atom, a substituted or non-substituted Cor longer alkyl group, a perfluoroalkyl group or a trialkylsilyl group. 3. The compound according to claim 2 , wherein in formula (Z) claim 2 , Lcorresponding to Zis a single bond or a divalent connecting group composed of a combination of one or more members selected among a carbonyl group claim 2 , a sulfonyl group claim 2 , a phosphoryl group claim 2 , an oxy group claim 2 , a substituted or non-substituted amino group claim 2 , a thio group claim 2 , an alkylene group claim 2 , an alkenylene group claim 2 , an alkynylene group and an arylene group. The present application is a Divisional Application of U.S. application Ser. No. 12/935,151, filed Sep. 28, 2010, which is the National Stage of International Application No. PCT/JP2009/056367, filed Mar. 27, 2009, and claims foreign priority to Japanese Application Nos. 2008-087957 and 2008-087958, filed Mar. 28, 2008, and Japanese Application No. 2008-301654, filed Nov. 26, 2008, the entire contents of each of which are incorporated by reference herein.The present invention relates to a novel compound. The compound of the invention is useful for various technical fields inclusive of technical fields of a lubricant.For the purposes of reducing a coefficient of friction and suppressing wear in various friction-sliding places, lubricating oils have been used in every industrial machine.In general, current lubricating oils are ...

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Номер записи: 46
16-01-2014 дата публикации

Sulfonamides as hib protease inhibitors

Номер: US20140018326A1
Автор: Daniel J. Mckay, Marie-Eve Lebrun, Oscar M. Moradei, Sheldon Crane, Vouy Linh Truong
Принадлежит: Merck Canada Inc

Compounds of Formula I are disclosed: wherein L, A, R 1 , R 2 , R 3A , R 3B , R 4A , R 4B , R 5 , R 6 and R 7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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Номер записи: 47
16-01-2014 дата публикации

USE OF D-SERINE DERIVATIVES FOR THE TREATMENT OF ANXIETY DISORDERS

Номер: US20140018549A1
Автор: Higgins Guy, Isaac Methvin, Slassi Abdelmalik
Принадлежит: NPS PHARMACEUTICALS, INC.

Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias, wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R; Ris chosen from: alkyl or haloalkyl; Ris chosen from: H, C(O)R, C(O)OR, SO2Ror C(O)NRR; R, Rand Rare independently chosen from: H or alkyl; Rand Rare independently chosen from: H or alkyl; and Ris chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R, C(O)OR, SO2Ror C(O)NRR. 120-. (canceled)23. The pharmaceutical composition of claim 21 , wherein:{'sup': 2', '6', '6', '6, 'sub': '2', 'Ris chosen from: H, C(O)R, C(O)OR, or SOR;'}{'sup': 3', '4', '5, 'R, Rand Rare each H;'}{'sup': '6', 'Ris alkyl; and'}{'sup': '8', 'Ris chosen from: halo or alkyl.'}25. The pharmaceutical composition of claim 24 , wherein:{'sup': '1', 'sub': '2', 'Ris chosen from: methyl or CHF; and'}{'sup': '6', 'Ris chosen from: methyl or tert-butyl.'}26. The pharmaceutical composition of claim 24 , wherein;{'sup': '8', 'A is aryl, optionally substituted with up to 5 independently-selected groups R;'}{'sup': 2', '6, 'Ris C(O)R; and'}{'sup': '8', 'Ris halo.'}27. The pharmaceutical composition of claim 26 , wherein;{'sup': '1', 'Ris haloalkyl; and'}{'sup': '6', 'Ris methyl.'}30. The pharmaceutical composition of claim 21 , wherein the anxiety disorder is chosen from: generalized anxiety disorder (GAD) claim 21 , panic attack claim 21 , post traumatic stress disorder (PTSD) claim 21 , obsessive compulsive disorder (OCD) or social phobias. The present disclosure relates the use serine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their usefulness in the treatment of anxiety disorders.Anxiety is broadly defined as a state of unwarranted or inappropriate worry often accompanied by ...

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Номер записи: 48
16-01-2014 дата публикации

PROCESS FOR SYNTHESIZING KETO-BENZOFURAN DERIVATIVES

Номер: US20140018553A1
Автор: Grimaud Bernard, Grossi Pierre-Jean
Принадлежит: SANOFI

9. The process according to claim 1 , wherein said keto benzofuran derivative is dranedarone or the hydrochloride salt thereof. The present invention relates to keto benzofuran derivatives of general formula (I) represented below, and also to a process for synthesizing them via coupling between a quinoneimine and a keto ester, and to synthetic intermediates thereof.In the keto benzofuran derivatives of formula (I),G1 represents a linear or branched alkyl (i), haloalkyl (ii), cycloalkyl (iii), substituted or unsubstituted aryl (iv), alkene (v) or alkyne (vi) group,G3 represents (i) a group —NHSORc or (ii) a group —NHRc, in which Rc represents (a) a linear or branched alkyl group, (b) a cycloalkyl group or (c) a substituted or unsubstituted aryl group,G5 represents a halogen atom or a group —ORb in which Rb represents a hydrogen atom, an alkyl, haloalkyl, aryl, arylalkyl, heteroaryl, cycloalkyl or heterocycloalkyl group or an -alkyleneaminoalkyl group,Ra is chosen from a hydrogen atom, halogen atoms and alkyl, haloalkyl, alkoxy and alkoxyalkyl groups,na is an index equal to 0, 1, 2, 3 or 4.A particularly advantageous derivative of the keto benzofurans (I) is 2-n- butyl-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-5-methylsulfonamidobenzofuran, known under the name dronedarone. Dronedarone, of formula (D) below:may be in the form of the free base or in salt form, in particular the hydrochloride salt of 2-n-butyl-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-5-methylsulfonamidobenzofuran.Dronedarone proves to be particularly useful as an active principle in indications of cardiac arrhythmia.At the present time, dronedarone in free base form is synthesized according to the process described in EP 0 471 609 B1 via the key intermediate bearing a benzofuran nucleus, 2-butyl-5-nitrobenzofuran. In this synthetic process, the intermediate 2-butyl-5-nitrobenzofuran must be:Friedel-Crafts reaction and then a demethylation, and ending with an O-alkylationThe complexity of the technical ...

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Номер записи: 49
23-01-2014 дата публикации

INHIBITORS OF HISTONE DEACETYLASE AND PRODRUGS THEREOF

Номер: US20140024608A1
Автор: Ajamian Alain, Deziel Robert
Принадлежит: METHYLGENE INC.

The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. 134.-. (canceled)37. A composition comprising a compound of or a pharmaceutically acceptable salt thereof.38. A composition comprising a compound of or a pharmaceutically acceptable salt thereof. This application claims the benefit of priority of U.S. Application No. 60/870,768, filed Dec. 19, 2006.1. Field of the InventionThis invention relates to the inhibition of histone deacetylase. More particularly, the invention relates to compounds and prodrugs thereof that inhibit, histone deacetylase enzymatic activity. The invention also relates to methods of inhibiting histone deacetylase enzymatic activity.2. Summary of the Related ArtIn eukaryotic cells, nuclear DNA associates with histones to form a compact complex called chromatin. The histones constitute a family of basic proteins which are generally highly conserved across eukaryotic species. The core histones, termed H2A, HB, H3, and H4, associate to form a protein core. DNA winds around this protein core, with the basic amino acids of the histones interacting with the negatively charged phosphate groups of the DNA. Approximately 146 base pairs of DNA wrap around a histone core to make up a nucleosome particle, the repeating structural motif of chromatin.Csordas, 286: 23-38 (1990) teaches that histones are subject to posttranslational acetylation of the e-amino groups of N-terminal lysine residues, a reaction that is catalyzed by histone acetyl transferase (HAT1). Acetylation neutralizes the positive charge of the lysine side chain, and is thought to impact chromatin structure. Indeed, Taunton et al., 272: 408-411 (1996), teaches that access of transcription factors to chromatin templates is enhanced by histone ...

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Номер записи: 50
30-01-2014 дата публикации

HERBICIDAL COMPOSITIONS COMPRISING 4-AMINO-3-CHLORO-5-FLUORO-6-(4-CHLORO-2-FLUORO-3-METHOXYPHENYL) PYRIDINE-2-CARBOXYLIC ACID OR A DERIVATIVE THEREOF AND HALOSULFURON, PYRAZOSULFURON AND ESPROCARB

Номер: US20140031216A1
Автор: Mann Richard K., Yerkes Carla N.
Принадлежит:

Provided herein are synergistic herbicidal compositions containing and methods of controlling undesirable vegetation utilizing 2. The composition of claim 1 , wherein (a) is a Calkyl or benzyl ester of compound (I).3. The composition of claim 2 , wherein (a) is a benzyl ester of compound (I).4. The composition of claim 1 , wherein (a) is the compound of formula (I) claim 1 , which is the carboxylic acid.5. The composition of claim 1 , further comprising a herbicide safener claim 1 , adjuvant and/or carrier.6. The composition of claim 1 , wherein the weight ratio of the compound of formula (I) or agriculturally acceptable salt or ester thereof to halosulfuron-methyl or agriculturally acceptable salt or ester thereof is from about 1:70 to about 214:1.7. The composition of claim 1 , wherein the weight ratio of the compound of formula (I) or agriculturally acceptable salt or ester thereof to pyrazosulfuron-ethyl or agriculturally acceptable salt or ester thereof is from about 1:60 to about 600:1.8. The composition of claim 1 , wherein the weight ratio of the compound of formula (I) or agriculturally acceptable salt or ester thereof to esprocarb of agriculturally acceptable salt or ester thereof is from about 1:500 to about 6:1.10. The method of claim 9 , wherein the undesirable vegetation is controlled in direct-seeded claim 9 , water-seeded and transplanted rice claim 9 , cereals claim 9 , wheat claim 9 , barley claim 9 , oats claim 9 , rye claim 9 , sorghum claim 9 , corn claim 9 , maize claim 9 , sugarcane claim 9 , sunflower claim 9 , oilseed rape claim 9 , canola claim 9 , sugar beet claim 9 , soybean claim 9 , cotton claim 9 , pineapple claim 9 , pastures claim 9 , grasslands claim 9 , rangelands claim 9 , fallowland claim 9 , turf claim 9 , tree and vine orchards claim 9 , aquatics claim 9 , plantation crops claim 9 , vegetables claim 9 , industrial vegetation management (IVM) or rights of way (ROW).11. The method of claim 9 , wherein locus a flooded rice paddy. ...

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Номер записи: 51
30-01-2014 дата публикации

SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS

Номер: US20140031399A1
Автор: McQuire Leslie Wighton, Rogel Olivier, Shultz Michael, Tommasi Ruben Alberto, Weiler Sven
Принадлежит:

The present invention provides a compound of formula (I): 1. A compound or salt thereof selected from the group consisting of:(R)—N-Hydroxy-2-[(1-hydroxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[Benzyl-(7-ethoxy-naphthalene-2-sulfonyl)-amino]-N-hydroxy-3-methyl-butyramide;N-isoamyl-N-(6-ethyl naphthalene-2-sulfonyl)-D-valine hydroxamic acid;N-Hydroxy-2-[(6-hydroxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Amino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Acetylamino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;N-isoamyl-N-(6-methoxy naphthalene-2-sulfonyl)-D-valine hydroxamic acid;N-isoamyl-N-(6-hydroxy naphthalene-2-sulfonyl)-D-valine hydroxamic acid;2-[(7-Amino-naphthalene-2-sulfonyl)-(3-phenyl-propyl)-amino]-N-hydroxy-3-methyl-butyramide;(R)—N-Hydroxy-2-[(7-methoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Ethoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[Benzyl-(6-p-tolylamino-naphthalene-2-sulfonyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-3-methyl-2-[[6-(3-methyl-butoxy)-naphthalene-2-sulfonyl]-(3-methyl-butyl)-amino]-butyramide;2-[(7-Ethoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-2-[(6-isobutoxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-3-methyl-butyramide;2-[(6-Amino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Benzyloxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Acetylamino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;N-Hydroxy-3-methyl-2-{(3-methyl-butyl)-[7-(3-methyl-butylamino)-naphthalene-2-sulfonyl]-amino}-butyramide;2-[(7-Acetylamino-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N-hydroxy-3-methyl-butyramide;2-[(6-Allyloxy-naphthalene-2-sulfonyl)-(3-methyl-butyl)-amino]-N- ...

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Номер записи: 52
06-02-2014 дата публикации

METHOD FOR PRODUCING DIAMINE COMPOUND

Номер: US20140039220A1
Автор: HAKAMATA Tomohiko, Nara Hideki, TOUGE Taichiro
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention provides a method for producing a compound represented by general formula (1) (wherein R, R, R, R-R, A-A, nand nare as defined in the description), which is characterized by reacting a compound represented by general formula (2) (wherein R-R, A-A, n, nand B are as defined in the description) with a diamine compound represented by general formula (3) (wherein R-Rare as defined in the description). The present invention is a method for producing a diamine compound, which is useful for the formation of a ruthenium-diamine complex, under mild conditions, said method being able to be put in industrial practice. 2. The production method according to claim 1 , whereinthe reaction of the compound represented by the general formula (2) is reacted with the diamine compound represented by the general formula (3) at a temperature of 100° C. to 200° C. This application is a National Stage of International Application No. PCT/JP2012/061445 filed Apr. 27, 2012, claiming priority based on Japanese Patent Application No. 2011-101528 filed Apr. 28, 2011, the contents of all of which are incorporated herein by reference in their entirety.The present invention relates to a method for producing a diamine compound useful for forming a ruthenium-diamine complex important as an asymmetric reduction catalyst.Many asymmetric reactions including asymmetric reduction have been developed, and many asymmetric reactions have been reported in which asymmetric metal complexes having optically active phosphine ligands are used. On the other hand, many reports have shown that complexes in which optically active nitrogen compounds are coordinated to transition metals, such as ruthenium, rhodium, and iridium, for example, have excellent performances as catalysts for asymmetric synthesis reactions. Moreover, to enhance the performances of these catalysts, various optically active nitrogen compounds have been developed (Non Patent Literatures 1, 2, 3, 4, etc.). In particular, M. ...

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Номер записи: 53
20-02-2014 дата публикации

METHOD FOR CONTROLLING CONIFEROUS PLANTS

Номер: US20140051578A1
Автор: OLIVER Glenn W., QUICKE Harold E., Zawierucha Joseph
Принадлежит: BASF AKTIENGESELLSCHAFT

A method for controlling coniferous plants, in particular naturally seeded coniferous plants (wildling conifers), wherein an effective amount of at least one herbicide selected from the group consisting of sulfentrazone, carfentrazone, their agriculturally acceptable salts and their agriculturally acceptable derivatives is applied to the coniferous plants to be controlled or to their parts, such as roots, leaves, seeds or germinants. 1. A herbicidal composition , which comprises at least one herbicide A , which is selected from the group consisting ofA1 acetolactate synthase inhibitors (ALS inhibitors);A2 photosynthesis inhibitors;A3 enolpyruvyl shikimate 3-phosphate synthase inhibitors (EPSP inhibitors);A4 glutamine synthetase inhibitors;A5 auxin herbicides; andA6 fosamine, andat least one further herbicide B, which is selected from the group consisting of sulfentrazone, carfentrazone, their agriculturally acceptable salts and their agriculturally acceptable derivatives,except for compositions which comprise at least one herbicide A selected from chlorimuron, halosulfuron, metsulfuron, nicosulfuron, primisulfuron, prosulfuron, thifensulfuron, tribenuron, imazamethabenz, flumetsulam, pyrithiobac, atrazin, difenzoquat, paraquat, bromoxynil, pyridate, glyphosate, glufosinate, 2,4-D, MCPA, dicamba, clopyralid, fluoxazine, the agriculturally acceptable salts thereof and the agriculturally acceptable derivatives thereof, and carfentrazone, an agriculturally acceptable salt thereof or an agriculturally acceptable derivative thereof, andexcept for compositions which comprise at least one herbicide A selected from chlorimuron, rimsulfuron, tribenuron, imazethapyr, cloransulam, flumetsulam, metribuzin, qlyphosate, 2,4-D, the agriculturally acceptable salts thereof and the agriculturally acceptable derivatives thereof, and sulfentrazone, an agriculturally acceptable salt thereof or an agriculturally acceptable derivative thereof.2. The composition as claimed in claim 1 , ...

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Номер записи: 54
20-02-2014 дата публикации

KATP ANTAGONISTS (GLIBENGLAMID) FOR USE FOR PROMOTING GROWTH AND/OR TREATING HYPERGLYCAEMIA OF A PREMATURE INFANT

Номер: US20140051761A1
Автор: Polak Marianne Berdugo, Polak Michel
Принадлежит: ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS

The present invention relates to pharmaceutical compositions comprising an ATP-sensitive potassium (K ATP) channel antagonist (e.g., sulfonylureas, meglitinides) and methods for treating hyperglycaemia and/or promoting growth of a premature and/or small for gestational age infant. 113-. (canceled)14. A method for promoting growth and/or treating hyperglycaemia in preterm and/or small-for-gestational-age infant , comprising enterally administering a therapeutically effective amount of a composition comprising a therapeutically effective amount of a KATP channel antagonist to a preterm and/or small-for-gestational-age infant in need of growth promotion and/or treatment for hyperglycaemia.15. The method of claim 14 , wherein the infant weights less than 2 claim 14 ,500 g at birth.16. The method of claim 14 , wherein the infant weights less than 1 claim 14 ,500 g at birth.17. The method of claim 14 , wherein the infant is born at less than 32 weeks gestation.18. The method of claim 14 , wherein the infant is born at less than 28 weeks gestation.19. The method of claim 14 , wherein the infant is a premature appropriate-for-gestational-age infant with preterm growth restraint.20. The method of claim 14 , wherein the Kchannel antagonist is selected from the group consisting of sulfonylureas and meglitinides claim 14 , and any combination thereof.21. The method of claim 14 , wherein the Kchannel antagonist is selected from the group consisting of glibenclamide claim 14 , acetohexamide claim 14 , carbutamide claim 14 , glibornuride claim 14 , chlorpropamide claim 14 , tolbutamide claim 14 , tolazamide claim 14 , glipizide claim 14 , gliclazide claim 14 , gliquidone claim 14 , glyclopyramide claim 14 , glisoxepide claim 14 , glimepiride repaglinide claim 14 , nateglinide and mitiglinide.22. The method of claim 14 , wherein the Kchannel antagonist is glibenclamide.23. The method of claim 14 , wherein the composition is in a liquid form.24. The method of claim 14 , wherein the ...

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Номер записи: 55
06-03-2014 дата публикации

INHIBITORS OF BROMODOMAINS AS MODULATORS OF GENE EXPRESSION

Номер: US20140066410A1
Автор: KASTRINSKY David, Mujtaba Shiraz, OHLMEYER Michael, Plotnikov Alexander, Zhang Guangtao, Zhou Ming-MIng
Принадлежит: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease. 427-. (canceled)2937-. (canceled)41. The compound of claim 39 , wherein G is fused to Xor Xto form a heterocyclic ring system capable of accepting or donating a hydrogen bond.4257-. (canceled)5964-. (canceled)67. (canceled)68. A method of treating cancer in a patient claim 1 , the method comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt form thereof claim 1 , to the patient.69. (canceled)70. The method of claim 68 , wherein the method further comprises administering a therapeutically effective amount of an anticancer agent to the patient.7178-. (canceled)79. A method for treating HIV/AIDS in a patient claim 1 , the method comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt form thereof claim 1 , to the patient.8088-. (canceled)89. A method of treating an inflammatory disease or autoimmune disease in a patient claim 1 , the method comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt form thereof claim 1 , to the patient.9092-. (canceled)93. A method of treating a neurological disorder in a patient where NF-kB is implicated in the pathology of the disorder claim 1 , the method comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt form thereof claim 1 , to the patient.9498-. (canceled)99. A method for treating a retroviral infection in a patient claim 1 , the method comprising administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt form thereof claim 1 , ...

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Номер записи: 56
06-03-2014 дата публикации

ANALOGS AND PRODRUGS OF BUMETANIDE; COMPOSITIONS AND METHODS OF USE

Номер: US20140066504A1
Автор: HOCHMAN Daryl W., ORR Matthew David, SOUKRI Mustapha
Принадлежит:

Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus. 1. A compound comprising an analog or prodrug of bumetanide.3. A compound of claim 1 , comprising a 5-amido or 5-keto bumetanide derivative in which the 5-ester has been replaced by either a ketone or an amide.9. A method for the treatment and/or prophylaxis of a neurological or psychiatric disorder comprising administering a composition having one of formulas I-VI disclosed herein.10. The method of claim 9 , wherein the neurological or psychiatric disorder is selected from the group consisting of: anxiety disorders (including posttraumatic stress disorder claim 9 , generalized anxiety disorder claim 9 , panic disorder claim 9 , obsessive compulsive disorder claim 9 , specific phobia) claim 9 , epilepsy claim 9 , migraine claim 9 , seizure disorders and non-epileptic seizures claim 9 , sleep disorders claim 9 , obesity claim 9 , eating disorders claim 9 , autism claim 9 , depression claim 9 , edema claim 9 , glaucoma claim 9 , stroke claim 9 , ischemia claim 9 , neuropathic pain claim 9 , addictive disorders claim 9 , schizophrenia claim 9 , psychosis claim 9 , and tinnitus.11. The method of claim 9 , comprising administering the composition following the onset of symptoms.12. The method of claim 9 , comprising administering the composition prophylactically prior to the onset of ...

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Номер записи: 57
20-03-2014 дата публикации

FLUORESCENT DYE FOR PH SENSOR

Номер: US20140080222A1
Автор: Riechers Daniel, Wuenn Eberhard
Принадлежит: SARTORIUS STEDIM BIOTECH GMBH

The present invention relates to a new type of fluorescent with the following formula (I), its preparation process, and also an optical pH sensor which comprises this fluorescent dye immobilized on an analyte-permeable carrier. 3. The fluorescent dye of claim 2 , where n is an integer from 2 to 4.4. The fluorescent dye of claim 1 , where the fluorescent dye has two different maxima in the fluorescence emission.5. The fluorescent dye of claim 4 , where at least one of the two different maxima in the fluorescence emission has a pH-dependent intensity maximum.6. The fluorescent dye of claim 5 , where the pH-dependent fluorescent maximum is in a range of >420 nm.8. The process of claim 7 , where the compound of the formula (III) is the corresponding disodium salt.10. An optical pH sensor claim 1 , comprising an analyte-permeable carrier and the fluorescent dye of claim 1 , which is immobilized on a carrier.11. The optical pH sensor of claim 10 , where the thickness of the carrier is from 50 μm to 500 μm.12. The optical pH sensor of claim 10 , further comprising at least one coating which is provided on at least one surface of the carrier on which the fluorescent dye is immobilized.13. The optical pH sensor of claim 12 , where the coating is transparent.14. The optical pH sensor of or claim 12 , where an adhesive layer is provided on the coating.15. The optical pH sensor claim 10 , where the dynamic measurement range is in the range from pH 4.0 to pH 8.0. 1. Field of the InventionThe present invention relates to a new type of fluorescent dye, to its preparation process, and to an optical pH sensor comprising this fluorescent dye.2. Description of the Related ArtThe determination of the H+ activity in aqueous media, i.e. the measurement of the pH, using electrochemical sensors, in particular by means of pH glass electrodes, has been known for a long time. Nevertheless, the use of glass electrodes also has disadvantages in several respects, such as, for example, the ...

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Номер записи: 58
27-03-2014 дата публикации

MODULATORS OF HSP70/DNAK FUNCTION AND METHODS OF USE THEREOF

Номер: US20140087005A1
Автор: George Donna L., Leu Julia I-Ju, Murphy Maureen
Принадлежит:

Compositions and methods for modulating HSP70 function, particularly for the targeted killing of cancer cells, are disclosed. 2. The method of wherein said disease is cancer and said HSP70 function is selected from the group consisting of modulation of protein aggregation claim 1 , chaperone protein binding claim 1 , client protein binding claim 1 , modulation of cellular stress response claim 1 , modulation of autophagy claim 1 , modulation of lysosomal functions claim 1 , modulation of NFκB activity claim 1 , modulation of caspase cleavage claim 1 , modulation of the proteasome system claim 1 , reduced viability claim 1 , modulation of anoikis claim 1 , modulation of formation of detergent-insoluble subcellular complexes claim 1 , and modulation of vacuolization.3. The method of claim 2 , wherein said compound disrupts HSP70 binding to at least one chaperone protein selected from the group consisting of CHIP claim 2 , HSP40 claim 2 , and BAG-1M isoform.4. The method of claim 2 , wherein said compound disrupts HSP70 binding to at least one client protein selected from the group consisting of APAF-1 claim 2 , p53 claim 2 , LAMP-2 claim 2 , integrin α5 claim 2 , integrin β1 claim 2 , SV40 T antigen claim 2 , and HSP90 client proteins.5. The method of claim 1 , wherein Q represents —C≡C— claim 1 , and R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Reach represents hydrogen.6. The method of claim 1 , wherein the compound of formula I is pifithrin-μ.7. The method of claim 1 , wherein said disease is characterized by aberrant cell proliferation.8. The method of claim 7 , wherein said chemotherapeutic agent is an anti-neoplastic agent.9. The method of claim 1 , wherein said chemotherapeutic agent and said compound are administered simultaneously.10. The method of claim 1 , wherein said chemotherapeutic agent and said compound are administered sequentially.11. The method of claim 1 , wherein said chemotherapeutic agent and said compound are administered via a route ...

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Номер записи: 59
03-01-2019 дата публикации

SYNERGISTIC HERBICIDAL COMPOSITION AND THE METHOD OF CONTROLLING THE GROWTH OF UNDESIRED PLANTS

Номер: US20190000083A1
Автор: BRISTOW James Timothy
Принадлежит: JIANGSU ROTAM CHEMISTRY CO., LTD

A synergistic herbicidal composition comprising Pyroxasulfone and Thifensulfuron methyl as the active components, as well as the use of the synergistic herbicidal composition for controlling the growth of undesirable plants is provided. A method of controlling the growth of undesirable plants, which comprises applying the active components Pyroxasulfone and Thifensulfuron methyl of the synergistic herbicidal composition to the undesirable plants or their growing locus jointly or separately is also provided. A method of reducing or preventing harm caused by Pyroxasulfone when applied to plants, seeds or other reproductive parts of useful crops is also provided. 1. A synergistic herbicidal composition comprising Pyroxasulfone and Thifensulfuron methyl as the active components , wherein the weight ratio of Pyroxasulfone and Thifensulfuron methyl ranges from 50:1 to 1:50.2. The synergistic herbicidal composition of claim 1 , wherein the weight ratio of said Pyroxasulfone and Thifensulfuron methyl ranges from 25:1 to 1:25.3. The synergistic herbicidal composition of claim 1 , wherein the weight ratio of said Pyroxasulfone and Thifensulfuron methyl ranges from 10:1 to 1:10.4. The synergistic herbicidal composition of claim 1 , wherein the weight ratio of said Pyroxasulfone and Thifensulfuron methyl ranges from 5:1 to 1:5.5. The synergistic herbicidal composition of claim 1 , further comprising a surfactant and/or filler.6. The synergistic herbicidal composition of claim 5 , wherein said active components of Pyroxasulfone and Thifensulfuron methyl is present in the synergistic herbicidal composition in an amount of 5% to 90% by weight.7. The synergistic herbicidal composition of claim 5 , wherein said active components of Pyroxasulfone and Thifensulfuron methyl is present in the synergistic herbicidal composition in an amount of 10% to 80% by weight.8. The synergistic herbicidal composition of claim 5 , wherein said active components of Pyroxasulfone and Thifensulfuron ...

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Номер записи: 60
07-01-2016 дата публикации

HERBICIDAL COMPOSITION

Номер: US20160000085A1
Автор: Okamoto Hiroyuki, Terada Takashi, Yamada Ryu
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

At present, many herbicidal compositions have been developed and used, but they are not necessarily sufficient to control undesired plants such as weeds to be controlled in some cases, and a herbicidal composition having high activity has been desired. 1. A herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one herbicidal compound selected from the group consisting of imazapic , hexazinone , mesotrione and their salts.2. The composition according to claim 1 , wherein the mixing ratio of (A) to (B) is from 1:0.2 to 1:50 by the weight ratio.3. The composition according to claim 2 , wherein the mixing ratio of (A) to (B) is from 1:1 to 1:30 by the weight ratio.4. The composition according to claim 3 , wherein (B) is at least one member selected from the group consisting of imazapic claim 3 , hexazinone claim 3 , mesotrione claim 3 , and wherein the mixing ratio of (A) to (B) imazapic is from 1:1 to 1:15 by the weight ratio claim 3 , the mixing ratio of (A) to (B) hexazinone is from 1:2 to 1:30 by the weight ratio claim 3 , and the mixing ratio of (A) to (B) mesotrione is from 1:1 to 1:20 by the weight ratio.5. The composition according to claim 4 , wherein (A) is flazasulfuron claim 4 , (B) is imazapic claim 4 , and their mixing ratio is from 1:1 to 1:15 by the weight ratio.6. The composition according to claim 4 , wherein (A) is flazasulfuron claim 4 , (B) is hexazinone claim 4 , and their mixing ratio is from 1:2 to 1:30 by the weight ratio.7. The composition according to claim 4 , wherein (A) is flazasulfuron claim 4 , (B) is mesotrione claim 4 , and their mixing ratio is from 1:1 to 1:20 by the weight ratio.8. A method for controlling undesired plants or inhibiting their growth claim 4 , which comprises applying a herbicidally effective amount of (A) flazasulfuron or its salt and a herbicidally effective amount of (B) at least one herbicidal compound selected from the group consisting of imazapic claim 4 , hexazinone claim 4 , ...

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Номер записи: 61
04-01-2018 дата публикации

LIQUID SULFONYLUREA-CONTAINING HERBICIDAL COMPOSITIONS

Номер: US20180000069A1
Автор: Egan Oliver, Goldsmith Andrew
Принадлежит:

This invention relates to a liquid herbicidal composition comprising a non-aqueous solvent system, at least one sulfonylurea herbicide and at least one inorganic salt selected from the metal carbonates and metal phosphates. The invention also relates to the use of an inorganic salt selected from the metal carbonates and metal phosphates to improve chemical stabilisation of a sulfonylurea herbicide in a liquid composition comprising a non-aqueous solvent system. 1. A liquid herbicidal composition comprising:a non-aqueous solvent system;at least one sulfonylurea herbicide; andat least one inorganic salt selected from the metalcarbonates and metal phosphates.2. The composition according to claim 1 , wherein the inorganic salt is selected from alkali metal phosphates and alkali metal carbonates.3. The composition according to claim 1 , wherein the inorganic salt comprises a metal selected from Na claim 1 , K claim 1 , Ca claim 1 , Mg or Al.4. The composition according to any one of to claim 1 , wherein the inorganic salt is selected from NaPO claim 1 , KPO claim 1 , Mg(PO) claim 1 , AlPO claim 1 , and NaCO.5. The composition according to any one of to claim 1 , which is formulated as an oil dispersion (OD) claim 1 , a dispersible concentrate (DC) claim 1 , an emulsifiable concentrate (EC) claim 1 , or a soluble concentrate (SL).6. The composition according to any one of to claim 1 , which is formulated as an oil dispersion (OD) and wherein at least one sulfonylurea is suspended in the non-aqueous solvent system.7. The composition according to any one of to claim 1 , wherein at least one inorganic salt is suspended in the non-aqueous solvent system.8. The composition according to any one of to claim 1 , wherein the sulfonylurea herbicide is selected from amidosulfuron claim 1 , azimsulfuron claim 1 , bensulfuron claim 1 , chlorimuron claim 1 , chlorsulfuron claim 1 , cinosulfuron claim 1 , cyclosulfamuron claim 1 , ethametsulfuron claim 1 , ethoxysulfuron claim 1 , ...

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Номер записи: 62
04-01-2018 дата публикации

PREVENTION OF HYPOGLYCAEMIA IN DIABETES MELLITUS TYPE 2 PATIENTS

Номер: US20180000902A1
Автор: BOKA Gabor, MIOSSEC Patrick, SILVESTRE Louise
Принадлежит:

A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering (a) desProExendin-4(1-39)-Lys-NHor/and a pharmaceutically acceptable salt thereof, and (b) a sulfonyl urea or/and a pharmaceutically acceptable salt thereof, to a subject in need thereof. 1. A method for improving glycemic control in a type 2 diabetes mellitus patient comprising administering to the patient in need thereof:lixisenatide or a pharmaceutically acceptable salt thereof;wherein the patient is currently receiving treatment with a sulfonylurea.2. The method of claim 1 , wherein the lixisenatide or a pharmaceutically acceptable salt thereof is administered as a daily dose of 10 μg to 20 μg.3. The method of claim 1 , wherein the patient is not adequately controlled by treatment with the sulfonylurea.4. The method of claim 1 , wherein the type 2 diabetes mellitus patient is currently receiving treatment with a sulfonylurea and metformin.5. The method of claim 4 , wherein the patient is not adequately controlled by treatment with sulfonylurea and metformin.6. The method as in or claim 4 , wherein the patient has a HbAvalue in the range of about 8% to about 10% with current treatment.7. The method of claim 1 , wherein the lixisenatide or pharmaceutically acceptable salt thereof is administered as an add-on therapy to the patient's current treatment.8. The method of claim 7 , further comprising:administering the sulfonylurea to the patient at a reduced dose if the patient has an increased risk of hypoglycemia.9. The method of claim 7 , further comprising:administering the sulfonylurea to the patient at a reduced dose if the patient has previously experienced a hypoglycemic event.10. The method of claim 1 , wherein the sulfonylurea is glibenclamide claim 1 , glibenclamide MR claim 1 , gliclazide claim 1 , gliclazide LM claim 1 , glimepiride claim 1 , glipizide claim 1 , glipizide XL claim 1 , gliquidone claim 1 , or tolbutamide.11. A method for improving glycemic ...

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Номер записи: 63
07-01-2016 дата публикации

UV-ABSORBING COMPOUNDS WITH AT LEAST ONE REACTIVE HYDROGEN

Номер: US20160002154A1
Автор: Buron Christophe, Nacharaju Krishnamurthy, Tallon Michael A., Toney Christopher J.
Принадлежит: ISP Investments Inc.

UV-absorbing compounds are provided that have at least one reactive hydrogen. These compounds have structures: wherein the generic notations have meanings as described herein. Also provided are formulations comprising a UV-absorbing compounds. 3. The compound according to wherein said Q is a residue of a compound selected from the group consisting of: diols claim 2 , diamines claim 2 , thio alcohols claim 2 , amino alcohols claim 2 , polyols claim 2 , polyether polyols claim 2 , polyacetal polyethers claim 2 , polyalkylene polyamines claim 2 , polyetheramines claim 2 , polyalkylene imines claim 2 , polysaccharides claim 2 , and combinations thereof.7. The compound according to wherein said Q is a residue of a compound selected from the group consisting of: diols claim 6 , diamines claim 6 , thio alcohols claim 6 , amino alcohols claim 6 , polyols claim 6 , polyether polyols claim 6 , polyacetal polyethers claim 6 , polyalkylene polyamines claim 6 , polyetheramines claim 6 , polyethylene imines claim 6 , polysaccharides claim 6 , and combinations thereof.11. The compound according to wherein said Q is a residue of a compound selected from the group consisting of: diols claim 10 , amino alcohols claim 10 , polyols claim 10 , polyether polyols claim 10 , polyacetal polyethers claim 10 , polyalkylene polyamines claim 10 , polyetheramines claim 10 , polyethylene imines claim 10 , polysaccharides claim 10 , and combinations thereof.13. A formulation comprising at least one compound of .14. The formulation according to that is a personal care formulation claim 13 , pharmaceutical claim 13 , food claim 13 , adhesive claim 13 , coating claim 13 , electronic claim 13 , ink claim 13 , paper claim 13 , paint claim 13 , polish claim 13 , printing claim 13 , construction claim 13 , energy claim 13 , oilfield claim 13 , lubricant claim 13 , industrial claim 13 , biocide claim 13 , preservative claim 13 , agrochemical claim 13 , or wood-care formulation.15. The formulation ...

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Номер записи: 64
07-01-2016 дата публикации

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20160002155A1
Автор: Last Stefaan Julien, Raboisson Pierre Jean-Marie Bernard, Vandyck Koen
Принадлежит: JANSSEN SCIENCES IRELAND UC

Inhibitors of HBV replication of Formula (I) 2. The compound according to claim 1 , wherein the C-Calkyl group as defined in Rrepresents a branched C-Calkyl.4. A compound according to claim 3 , wherein Ris selected from the group consisting of C-Calkyl optionally substituted with —C≡CH claim 3 , —CN claim 3 , —OH claim 3 , C-Calkyloxy claim 3 , —C(═O)O—R claim 3 , —C(═O)N(R) claim 3 , —N(R) claim 3 , —NHC(═O)—Rand —NHC(═O)O—R.5. A compound according to claim 1 , wherein at least one Ris —OH.6. A compound according to claim 3 , wherein at least one Ris C-Calkyl substituted with OH.7. A method of treating an HBV infection claim 1 , comprising administering a therapeutically effective amount of at least one compound according to .8. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier.9. (canceled)10. The pharmaceutical composition of claim 8 , further comprising a second HBV inhibitor.11. A method of treating an HBV infection claim 8 , comprising administering the pharmaceutical composition of .12. A method of treating an HBV infection claim 10 , comprising administering the pharmaceutical composition of . The Hepatitis B virus (HBV) is an enveloped, partially double-stranded DNA (dsDNA) virus of the Hepadnavirus family (Hepadnaviridae). Its genome contains 4 overlapping reading frames: the precore/core gene; the polymerase gene; the L, M, and S genes, which encode for the 3 envelope proteins; and the X gene.Upon infection, the partially double-stranded DNA genome (the relaxed circular DNA; rcDNA) is converted to a covalently closed circular DNA (cccDNA) in the nucleus of the host cell and the viral mRNAs are transcribed. Once encapsidated, the pregenomic RNA (pgRNA), which also codes for core protein and Pol, serves as the template for reverse transcription, which regenerates the partially dsDNA genome (rcDNA) in the nucleocapsid.HBV has caused epidemics in parts of Asia and Africa, and it is endemic in ...

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Номер записи: 65
07-01-2016 дата публикации

N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS

Номер: US20160002156A1
Автор: BROOKFIELD Frederick Arthur, Cohen Andrew D., COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Toscano John P.
Принадлежит:

The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives. 2. The compound of claim 1 , wherein Ris H.3. The compound of claim 1 , wherein each Rand Ris independently selected from the group consisting of Cl claim 1 , F claim 1 , I claim 1 , Br claim 1 , SOCH claim 1 , SONHOH claim 1 , CF claim 1 , CH claim 1 , NO claim 1 , phenyl claim 1 , CN claim 1 , OCH claim 1 , OCF claim 1 , t-Bu claim 1 , O-iPr claim 1 , 4-nitrophenyloxy (OPh4-NO) claim 1 , propane-2-thiyl (SCH(CH)) claim 1 , propane-2-sulfinyl (S(O)CH(CH)) claim 1 , morpholino claim 1 , N-methyl-piperazino claim 1 , dimethylamino claim 1 , piperidino claim 1 , cyclohexyloxy claim 1 , cyclopentylsulfanyl claim 1 , phenylsulfanyl and phenylsulfinyl.4. The compound of claim 1 , wherein the compound is of the formula (I).5. The compound of wherein the compound is of the formula (I) and at least one of Rand Ris other than H.6. The compound of claim 4 , wherein the compound is of the formula (I) and at least one of Rand Ris an electron withdrawing group.7. The compound of claim 4 , wherein the compound is of the formula (I) and R claim 4 , R claim 4 , R claim 4 , Rand Rare independently selected from the group consisting of H claim 4 , halo claim 4 , alkylsulfonyl claim 4 , N-hydroxylsulfonamidyl claim 4 , perhaloalkyl claim 4 , nitro claim 4 , aryl claim 4 , cyano claim 4 , alkoxy claim 4 , perhaloalkoxy claim 4 , alkyl claim 4 , substituted aryloxy claim 4 , alkylsulfanyl claim 4 , alkylsulfinyl claim 4 , heterocycloalkyl ...

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Номер записи: 66
07-01-2016 дата публикации

PLANT GROWTH REGULATING COMPOUNDS

Номер: US20160002161A1
Автор: DE MESMAEKER Alain, Jung Pierre Joseph Marcel, LACHIA Mathilde Denise, SCREPANTI Claudio, Wolf Hanno Christian
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds. 2. The compound according to wherein R1 and R2 are independently selected from H claim 1 , methyl claim 1 , ethyl claim 1 , halogen or methoxy or form a C6 cycloalkyl claim 1 , preferably unsubstituted.3. The compound according to wherein R1 and R2 are independently selected from H and methyl.4. The compound according to wherein R1 and R2 are both methyl.5. The compound according to wherein one of R1 and R2 is hydrogen and the other is methyl.6. The compound according to wherein R3 is selected from H claim 1 , C1-C6 alkyl optionally substituted by one to five R4 claim 1 , methoxy claim 1 , ethoxy claim 1 , cyano claim 1 , acetyl claim 1 , acetoxy claim 1 , cyclopropyl optionally substituted with R4 claim 1 , C1-C6 alkenyl optionally substituted by one to five R4 claim 1 , C1-C6 alkynyl optionally substituted by one to five R4; and wherein each R4 is preferably independently halogen claim 1 , methoxy or cyano.7. The compound according to wherein R3 is selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , butyl claim 1 , isopropyl claim 1 , trifluoromethyl claim 1 , trifluoroethyl claim 1 , methoxymethyl claim 1 , methoxyethyl claim 1 , methoxy claim 1 , ethoxy claim 1 , cyano claim 1 , acetyl claim 1 , acetoxy claim 1 , cyclopropyl claim 1 , allyl claim 1 , propargyl claim 1 , phenyl claim 1 , benzyl claim 1 , pyridyl or thiazolyl.8. The compound according to wherein X is selected from H claim 1 , methyl claim 1 , ethyl claim 1 , iso-propyl claim 1 , halogen claim 1 , alkoxy claim 1 , alkoxyalkyl claim 1 , haloalkyl claim 1 , cyano claim 1 , nitro claim 1 , acetylene claim 1 , acetoxy claim 1 , acetyl claim 1 , carboxyl claim 1 , methoxycarbonyl claim 1 , or from unsubstituted ...

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Номер записи: 67
02-01-2020 дата публикации

Process for Preparing Pentenoate

Номер: US20200002263A1
Автор: Kohls Paul, Pöchlauer Peter, Schuster Christian, Steinhofer Stefan
Принадлежит: PATHEON AUSTRIA GMBH & CO KG

The invention pertains to a process for preparing a compound of formula (1) 3. The process according to claim 2 , wherein step (c) is conducted in continuous mode.5. The process according to claim 4 , wherein step (d) is conducted in continuous mode.10. The process according to claim 8 , wherein step (d) is conducted in continuous mode.11. The process according to claim 9 , wherein step (d) is conducted in continuous mode. The present invention relates to processes for preparing pentenoate and pentenoate-like compounds. The invention further provides a process for preparing propenals.Synthetic routes for the preparation of pentenoate and pentenoate-like compounds are known in the art. Kelly et al (in Tetrahedron Letters, vol. 40, Iss. 16 (1999), pp. 3251-3254) discloses the synthesis of pentenoate by the reaction of bromo acetate derivatives and propenal derivatives in the presence of a Zinc-based catalyst. A further synthesis uses the condensation of acetate derivatives as described by Dewi-Wuelfling et al. (in Synlett, nb. 3 (2006), pp. 487-489). These reactions are exothermic and is consequently difficult to control and obtain high yields. Moreover, propenals, in particular acrolein, have a tendency to polymerize, rendering these compounds difficult to store and/or transport without substantial deterioration of the required propenal. Using such propenals to produce pentenoate or pentenoate-like compounds leads to an even lower yield and presence of (more) undesirable by-products.The objective of the present invention is to provide a novel process as well as an improved process to prepare pentenoate and pentenoate-like compounds.The present invention pertains to a process for preparing a compound of formula (1)wherein Ris independently chosen from C-Calkyl, cycloalkyl, aralkyl and aryl, and R, Rand Rare independently chosen from hydrogen and C-Calkyl, cycloalkyl, aralkyl and aryl;which process comprises the steps of:a) contacting a compound of formula (2)wherein ...

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Номер записи: 68
07-01-2021 дата публикации

HEAT SENSITIVE RECORDING MATERIAL AND COLOR DEVELOPER

Номер: US20210002215A1
Автор: "ONeil Robert Montgomery", BACHMANN Frank, Feiler Leonhard, KOLAMBKAR Prachin, Kulkarni Priti, WAKHARE Vilas
Принадлежит: SOLENIS TECHNOLOGIES CAYMAN, L.P.

The presently claimed invention relates to a color developer, a process for its manufacture and its use as a component in heat sensitive recording material. The heat sensitive recording material is useful for thermographic printing. 40. The compound according to claim 3 , wherein the compound is a crystalline polymorph form α that is characterized by an X-ray powder diffraction pattern comprising 2Θ reflections claim 3 , plus or minus 0.2 degrees 2Θ claim 3 , at 5.5 claim 3 , 6.1 claim 3 , 6.4 claim 3 , 12.1 claim 3 , 16.1 claim 3 , 16.8 claim 3 , 17.1 claim 3 , 18.3 claim 3 , 19.1 claim 3 , 19.9 claim 3 , 20.2 claim 3 , 21.4 claim 3 , 22.1 claim 3 , 22.7 claim 3 , 23.3 claim 3 , 24.3 claim 3 , 24.7 claim 3 , 25.0 claim 3 , 26.4 claim 3 , 27.7 and 29.3.5. The compound according to claim 3 , wherein the compound is a crystalline polymorph form β that is characterized by an X-ray powder diffraction pattern comprising 2Θ reflections claim 3 , plus or minus 0.2 degrees 2Θ claim 3 , at 6.2 claim 3 , 8.1 claim 3 , 10.1 claim 3 , 11.8 claim 3 , 12.2 claim 3 ,13.4 claim 3 , 14.1 claim 3 , 15.3 claim 3 , 16.1 claim 3 ,17.2 claim 3 ,18.4 claim 3 , 19.1 claim 3 , 20.6 claim 3 , 21.4 claim 3 , 22.4 claim 3 , 24.5 claim 3 , 25.0 claim 3 , 25.9 claim 3 , 26.2 claim 3 , 26.9 and 28.4.7. The process according to claim 6 , wherein the chlorination agent is selected from the group of thionyl chloride claim 6 , POCl claim 6 , PCland oxalyl chloride.8. The process according to claim 6 , wherein acid chloride (IVb) is 5-sulfonylchloride-isophthalic acid dichloride.10. The process according to claim 6 , wherein step c. comprises reacting the acid chloride of formula (IVb) with an amine RNHto obtain compound of formula (I) claim 6 , wherein Ris identical to R.11. The process according to claim 6 , wherein the amine is m-toluidine.13. (canceled)15. The heat sensitive recording material according to claim 14 , wherein the weight ratio of color developer to color former is in the range of 1. ...

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Номер записи: 69
01-01-2015 дата публикации

POLYMORPHS OF N- (2 -METHOXYBENZOYL) -4- [ (METHYLAMINOCARBONYL) AMINO] BENZENESULFONAMIDE

Номер: US20150005166A1
Автор: George Neil, HONE John, JONES Ian Kevin
Принадлежит: SYNGENTA LIMITED

The present invention relates to solid forms of herbicide safeners, to processes for their preparation, compositions comprising the solid forms and methods of their use as safeners 1. A crystalline polymorph of the compound of formula I , which has the following lattice parameters: a=19.38(5) , b=7.34(5) , c=22.95(5) , α=90.00 , β=90.00 , γ=90.00 and volume=3264.8(5) Å.2. The crystalline polymorph of claim 1 , wherein the polymorph is characterised by a powder X-ray diffraction pattern expressed in terms of 2θ angles claim 1 , wherein the powder X-ray diffraction pattern comprises:(a) at least one 2θ angle value at 9.0±0.2; and(b) one 2θ angle value at 21.7±0.2; and(c) at least three 2θ angle values selected from the group comprising 7.7±0.2, 11.9±0.2, 13.4±0.2, 15.0±0.2, 15.6±0.2, 16.1±0.2 and 18.0±0.2.3. The crystalline polymorph of which has a melting point of 216° C.±5° C.4. A crystalline polymorph of the compound of formula I claim 1 , wherein the polymorph is characterised by a powder X-ray diffraction pattern expressed in terms of 2θ angles claim 1 , wherein the powder X-ray diffraction pattern comprises:(a) at least one 2θ angle value at 9.0±0.2; and(b) one 2θ angle value at 21.7±0.2; and(c) at least three 2θ angle values selected from the group comprising 7.7±0.2, 11.9±0.2, 13.4±0.2, 15.0±0.2, 15.6±0.2, 16.1±0.2 and 18.0±0.2.5. The crystalline polymorph of which has a melting point of 216° C.±5° C.6. A crystalline polymorph of the compound of formula I which has the following lattice parameters: a=7.96(5) claim 4 , b=23.56(5) claim 4 , c=9.11(5) claim 4 , α=90.00 claim 4 , β=92.58(5) claim 4 , γ=90.00 and volume=1708.2(5) Å.7. The crystalline polymorph of claim 6 , wherein the polymorph is characterised by a powder X-ray diffraction pattern expressed in terms of 2θ angles claim 6 , wherein the powder X-ray diffraction pattern comprises(a) one 2θ angle value at 16.9±0.2; and(b) one 2θ angle value at 18.9±0.2; and(c) at least three 2θ angle values selected ...

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Номер записи: 70
12-01-2017 дата публикации

BENZENDE SULFONAMIDE DERIVATIVES AS HIV INTEGRASE INHIBITORS

Номер: US20170008839A1
Автор: WANG Xiang Simon
Принадлежит: HOWARD UNIVERSITY

Methods for treating retroviral infection or inhibiting HIV integrase in target cells or in a patient involve administering to target cells or to a patient in need of treatment an effective amount of at least one having a disulfonamide scaffold which is represented by the formula: 2. A method for inhibiting HIV integrase according to claim 1 , wherein X and Y independently represent lower alkyl.3. A method for inhibiting a HIV integrase according to claim 2 , wherein X and Y independently represent C-Calkyl.4. A method for inhibiting a HIV integrase according to claim 1 , wherein one of X and Y is lower alkyl and the other is halogeno claim 1 , amine or substituted amine.5. A method for inhibiting HIV integrase according to claim 1 , wherein n is 1 and m is 1 claim 1 , X and Y are independent of one another and represent para-substitutents.6. A method for inhibiting HIV integrase according to claim 1 , wherein R represents alkylene.7. A method for inhibiting HIV integrase according to claim 1 , wherein R represents an alkylene group having one to seven carbon atoms.8. A method for inhibiting HIV integrase according to claim 1 , wherein X and Y are independent of one another and represent para-substitutents and R represents an alkylene group having one to seven carbon atoms.9. A method for inhibiting HIV integrase according to claim 8 , wherein R represents —(CH)—.10. A method for inhibiting a HIV integrase according to claim 8 , wherein one of X and Y is lower alkyl and the other is halogeno.11. A method for inhibiting a HIV integrase according to claim 8 , wherein at least one X and Y is halogeno.12. A method for inhibiting a HIV integrase according to claim 1 , wherein at least one of X and Y is amine.13. A method for inhibiting a HIV integrase according to claim 1 , wherein when n is 1 and m is 2 claim 1 , one Y is substituted amino and the other Y is amino. For this application priority is claimed to U.S. Provisional Application 61/944990, filed Feb. 26, 2014, ...

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Номер записи: 71
09-01-2020 дата публикации

NOVEL IMAGING COMPOSITION AND USES THEREOF

Номер: US20200009090A1
Автор: DONNELLY Paul Stephen, Rudd Stacey Erin, Williams Spencer John
Принадлежит:

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The conjugate of claim 1 , wherein L is OR.3. The conjugate of claim 2 , wherein R is Cto Calkyl.4. The conjugate of claim 2 , wherein OR is selected from O-p-toluenesulfonate claim 2 , O-methanesulfonate claim 2 , O-trifluoromethanesulfonate claim 2 , O-benzenesulfonate claim 2 , and O-m-nitrobenzenesulfonate.5. The conjugate of claim 1 , wherein the target molecule is a polypeptide.6. The conjugate of claim 5 , wherein the polypeptide is an antibody.7. The conjugate of claim 6 , wherein the antibody is selected from trastuzumab claim 6 , rituximab and cetuximab.8. The conjugate of claim 1 , wherein the target molecule is a peptide.9. The conjugate of claim 8 , wherein the peptide is a targeting peptide.10. The conjugate of claim 9 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 9 , bombesin and glu-N(CO)N-lys PSMA. This application is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting ...

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Номер записи: 72
10-01-2019 дата публикации

METHOD FOR DECOLORING IONIC LIQUID

Номер: US20190009243A1
Автор: Kim Ki-hyun, OH Yong-Taeg, SHIN Dong-Chan
Принадлежит: Industry-Academic Cooperation Foundation Chosun University

A method of decoloring an ionic liquid includes preparing a discolored ionic liquid, and decoloring the discolored ionic liquid through irradiation with UV rays. An ionic liquid that is discolored due to heat treatment upon purification is decolored and can thus be reused. The method of decoloring the ionic liquid is effective because an ionic liquid, which is discolored due to heat treatment upon purification, can be decolored in a simple manner and also because an ionic liquid, which is discolored and is thus difficult to apply to the purification of an organic material, can be decolored in a simple manner, and can thus be reused in the form of a high-purity ionic liquid. 1. A method of decoloring an ionic liquid , comprising:preparing a discolored ionic liquid from an ionic liquid; anddecoloring the discolored ionic liquid through irradiation with UV rays.3. The method of claim 2 , wherein the ionic liquid includes at least one anion selected from the group consisting of Cl claim 2 , Br claim 2 , NO claim 2 , BF claim 2 , PF claim 2 , AlCl claim 2 , AlCl claim 2 , AcO claim 2 , CHCOO claim 2 , CFCOO claim 2 , CHSO claim 2 , CFSO claim 2 , (CFSO)N claim 2 , (CFSO)C claim 2 , (CFCFSO)N claim 2 , CFSO claim 2 , CF7COO claim 2 , (CFSO)(CFCO)N claim 2 , CFN claim 2 , CFNOS claim 2 , CFNOS claim 2 , CFNOS claim 2 , CFSO claim 2 , CFSO claim 2 , CFSO claim 2 , CFSO claim 2 , PF claim 2 , CHNOS claim 2 , CFNOS claim 2 , (CFSO)N claim 2 , and CHCH(OH)CO.4. The method of claim 1 , wherein the decoloring of the discolored ionic liquid is performed by irradiating the discolored ionic liquid with the UV rays in a UV range corresponding to an absorption wavelength of a cation contained in the ionic liquid before discoloration.5. The method of claim 2 , wherein the decoloring of the discolored ionic liquid is performed by irradiating the discolored ionic liquid with the UV rays in a UV range corresponding to an absorption wavelength of the cation contained in the ionic liquid ...

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Номер записи: 73
08-01-2015 дата публикации

HERBICIDAL COMPOSITION COMPRISING NICOSULFURON OR ITS SALT AND S -METOLACHLOR OR ITS SALT

Номер: US20150011391A1
Автор: Okamoto Hiroyuki, Terada Takashi, Yamada Ryu
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

At present, various herbicidal compositions have been developed and use, but there are a variety of types of weeds to be controlled, and their development lasts for a long period of time. Thus, a herbicidal composition having a broad herbicidal spectrum, having high activity and having a long-lasting effect has been desired. 1. A herbicidal composition comprising , as active ingredients , (a) nicosulfuron or its salt and (b) S-metolachlor or its salt.2. A method for controlling undesired plants or inhibiting their growth , which comprises applying a herbicidally effective amount of (a) nicosulfuron or its salt and a herbicidally effective amount of (b) S-metolachlor or its salt , to the undesired plants or to a place where they grow.3. The herbicidal composition according to claim 1 , wherein the weight ratio of (a) to (b) is within a range of from 1:1.3 to 1:800.4. The method according to claim 2 , wherein (a) is applied in an amount of from 5 to 150 g/ha claim 2 , and (b) is applied in an amount of from 200 to 4 claim 2 ,000 g/ha.5. The herbicidal composition according to claim 1 , which further contains claim 1 , as an active ingredient claim 1 , (c) at least one member selected from the group consisting of terbuthylazine claim 1 , mesotrione claim 1 , prosulfuron claim 1 , bicyclopyrone and their salts.6. The method according to claim 2 , wherein a herbicidally effective amount of (c) at least one member selected from the group consisting of terbuthylazine claim 2 , mesotrione claim 2 , prosulfuron claim 2 , bicyclopyrone and their salts is further applied to the undesired plants or to a place where they grow.7. The herbicidal composition according to claim 5 , wherein the weight ratio of (a) to (b) is within a range of from 1:1.3 to 1:800 claim 5 , and the weight ratio of (a) to (c) is within a range of from 1:0.006 to 1:400.8. The method according to claim 6 , wherein (a) is applied in an amount of from 5 to 150 g/ha claim 6 , (b) is applied in an amount of ...

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Номер записи: 74
09-01-2020 дата публикации

COVALENT PEPTIDE BINDERS

Номер: US20200010411A1
Автор: Hoppmann Christian, Wang Lei
Принадлежит:

There are provided, inter alia, compositions and methods for covalently binding peptides to proteins. 2. The compound according to claim 1 , wherein said Lis substituted or unsubstituted alkyl.3. The compound according to claim 2 , wherein said Lis substituted or unsubstituted C-Calkyl.4. The compound according to claim 3 , wherein said Lis unsubstituted C-Calkyl.5. The compound according to claim 4 , wherein said Lis methylene.6. The compound according to claim 1 , wherein said Lis substituted or unsubstituted heteroalkyl.7. The compound according to claim 6 , wherein said Lis substituted or unsubstituted 2 to 10 membered heteroalkyl.8. The compound according to claim 7 , wherein said Lis unsubstituted 2 to 10 membered heteroalkyl.9. The compound according to claim 7 , wherein said Lis oxo substituted 2 to 10 membered heteroalkyl.10. The compound according to claim 9 , wherein said Lis —(CH)—NH—C(O)— claim 9 , wherein n is an integer in the range 1-10.11. The compound according to claim 10 , wherein n is 1.13. The compound according to claim 1 , wherein Ris hydrogen.14. The compound according to claim 1 , wherein Ris an amino protecting group.15. The composition according to claim 14 , wherein said amino protecting group is tert-butyloxycarbonyl (tBoc) claim 14 , 9H-fluoren-9-ylmethoxycarbonyl (Fmoc) claim 14 , benzyloxy-carbonyl (Z) claim 14 , allyloxycarbonyl (Alloc) claim 14 , 4-methyltrityl (Mtt) claim 14 , 1-(4 claim 14 ,4-Dimethyl-2 claim 14 ,6-dioxocyclohex-1-ylidene)-3-ethyl (Dde) claim 14 , or 1-(4 claim 14 ,4-Dimethyl-2 claim 14 ,6-dioxocyclohex-1-ylidene)-3-methylbutyl (ivDde).16. The composition according to claim 15 , wherein said amino protecting group is Fmoc.18. The compound according to claim 17 , wherein said Lis substituted or unsubstituted alkyl.19. The compound according to claim 18 , wherein said Lis substituted or unsubstituted C-Calkyl.20. The compound according to claim 19 , wherein said Lis unsubstituted C-Calkyl.21. The compound according ...

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Номер записи: 75
09-01-2020 дата публикации

METHOD FOR PREPARING 3,7-BIS(DIMETHYLAMINO)PHENOTHIAZIN-5-YLIUM IODIDE

Номер: US20200010438A1
Автор: Feraud Michel, LAURENT Marina, QUERU Stéphane, Sayah Babak
Принадлежит: PROVEPHARM LIFE SOLUTIONS

Method for preparing 3,7-bis(dimethylamino)phenothiazin-5-ylium iodide, the method resulting in a high purity while being very simple to implement and producing high yields. The method uses phenothiazine as a starting material and includes the following steps: a) treating phenothiazine with diiodine, b) treating the reaction medium directly obtained from step a) with dimethylamine. 111-. (canceled)12. A process for preparing 3 ,7-bis(dimethylamino)phenothiazin-5-ylium iodide , this process using phenothiazine as starting product and comprising the following steps:a) treating phenothiazine with diiodine,b) treating the reaction medium directly resulting from step a) with dimethylamine.13. The process as claimed in claim 12 , wherein the treatment with diiodine is carried out with an amount of diiodine claim 12 , relative to the phenothiazine claim 12 , ranging from 2.5 molar equivalents to 3.5 molar equivalents.14. The process as claimed in claim 12 , wherein claim 12 , before step b) claim 12 , the reaction medium resulting from step a) is conditioned at a temperature ranging from 5° C. to 50° C.15. The process as claimed in claim 12 , wherein the treatment with dimethylamine is carried out with at least 7 molar equivalents of dimethylamine relative to the phenothiazine.16. The process as claimed in claim 12 , wherein claim 12 , in step a) claim 12 , the solvent is chosen from: an aromatic solvent or acetonitrile claim 12 , or mixtures thereof.17. The process as claimed in claim 16 , wherein in step a) claim 16 , the solvent is chosen from: toluene or acetonitrile claim 16 , or mixtures thereof.18. The process as claimed in claim 12 , wherein claim 12 , in step b) claim 12 , the dimethylamine is introduced into the reaction medium in the form of a solution in water.19. The process as claimed in claim 12 , wherein a precipitate forms at the outcome of the treatment of step b) claim 12 , said precipitate being recovered by filtration.20. The process as claimed in ...

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Номер записи: 76
17-01-2019 дата публикации

THIDIAZURON MIXTURES AND USES THEREOF

Номер: US20190014784A1
Автор: Belkind Benjamin A., Fritts Robert, Huang Zhengyu, Petracek Peter D., Silverman Franklin Paul, Woolard Derek D.
Принадлежит:

The present invention relates to thidiazuron mixtures. The present invention further relates to methods of promoting or synchronizing bud break in woody perennial plants by applying thidiazuron mixtures of the present invention. The present invention further relates to methods of promoting plant growth in woody perennial plants by applying thidiazuron mixtures of the present invention. 1. An agricultural composition for breaking bud dormancy of woody perennial plants comprising a mixture of an effective amount of thidiazuron and an effective amount of a second active agent selected from the group consisting of 17-0-0 fertilizer , 15-0-0 fertilizer and 1-aminocyclopropane-1-carboxylic acid , wherein the amount of thidiazuron and the second active agent is at a ratio from about 1:0.3 to about 1:3 ,000.2. The composition of claim 1 , wherein the second active agent is 15-0-0 fertilizer and the amount of thidiazuron and 15-0-0 fertilizer is at a ratio from about 1:100 to about 1:3 claim 1 ,000.3. The composition of claim 1 , wherein the second active agent is 15-0-0 fertilizer and the amount of thidiazuron and 15-0-0 fertilizer is at a ratio from about 1:500 to about 1:1 claim 1 ,500.4. The composition of claim 1 , wherein the second active agent is 17-0-0 fertilizer and the amount of thidiazuron and 17-0-0 fertilizer is at a ratio from about 1:100 to about 1:1 claim 1 ,00.5. The composition of claim 1 , wherein the second active agent is 17-0-0 fertilizer and the amount of thidiazuron and 17-0-0 fertilizer is at a ratio from about 1:400 to about 1:700.6. The composition of claim 1 , wherein the second active agent is 1-aminocyclopropane-1-carboxylic acid and the amount of thidiazuron and 1-aminocyclopropane-l-carboxylic acid is at a ratio from about 1:1 to about 1:10.7. The composition of claim 1 , wherein the second active agent is 1-aminocyclopropane-1-carboxylic acid and the amount of thidiazuron and 1-aminocyclopropane-l-carboxylic acid is at a ratio from about 1:2 ...

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Номер записи: 77
21-01-2016 дата публикации

METHODS FOR PHOSPHINE OXIDE REDUCTION IN CATALYTIC WITTIG REACTIONS

Номер: US20160016860A1
Автор: OBRIEN Christopher
Принадлежит:

A method for increasing the rate of phosphine oxide reduction, preferably during a Wittig reaction comprising use of an acid additive is provided. A room temperature catalytic Wittig reaction (CWR) the rate of reduction of the phosphine oxide is increased due to the addition of the acid additive is described. Furthermore, the extension of the CWR to semi-stabilized and non-stabilized ylides has been accomplished by utilization of a masked base and/or ylide-tuning.

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Номер записи: 78
21-01-2016 дата публикации

SUBSTITUTED BIARYL SULFONAMIDES AND THE USE THEREOF

Номер: US20160016899A1
Автор: Chan Kyle W.H., Fung Leah M., Sullivan Robert W., Swindlehurst Cathy A.
Принадлежит:

Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.

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Номер записи: 79
15-01-2015 дата публикации

CONTROL OF AQUATIC WEEDS WITH ENDOTHALL AND ALS-INHIBITING AGENT

Номер: US20150018213A1
Автор: Koschnick Tyler J., Tarver David P.
Принадлежит:

Described are preferred methods and compositions for controlling aquatic weeds that involve the use of an ALS-inhibiting herbicidal agent such as penoxsulam in combination with endothall. Preferred herbicidal combinations allow for enhanced control when treating a body of water to control a target weed population, such as hydrilla. 1. A method for controlling aquatic weeds in a body of water , comprising:providing in the body of water an herbicidal combination including penoxsulam and endothall, so as to control the aquatic weeds.2. The method of claim 1 , wherein the aquatic weeds include hydrilla.3. The method of claim 1 , wherein said providing comprises applying the endothall and penoxsulam to the body of water within 24 hours of one another.4. The method of claim 1 , wherein said providing comprises applying the endothall and penoxsulam at least 24 hours apart from one another.6. The method of claim 1 , wherein the penoxsulam is applied to the body of water at a level of about 2.5 to 50 ppb.7. The method of claim 1 , wherein the endothall is applied to the body of water at a level of about 0.1 to 3.5 ppm a.e.8. An herbicidal composition claim 1 , comprising:an herbicidal combination including penoxsulam and endothall.9. The herbicidal composition of claim 8 , wherein the penoxsulam and endothall are present in a ratio of about 1:2 to about 1:200 claim 8 , respectively.10. A multi-pack herbicide product claim 8 , comprising:a first container containing an ALS-inhibiting herbicide;a second container containing endothall; anda package holding said first container and second container.11. The product of claim 10 , wherein the ALS-inhibiting herbicide is penoxsulam.12. The product of claim 10 , wherein the ALS-inhibiting herbicide is imazamox.13. The product of claim 10 , wherein the ALS-inhibiting herbicide is bensulfuron-methyl.14. A method for controlling aquatic weeds in a body of water claim 10 , comprising:providing in the body of water an herbicidal ...

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Номер записи: 80
15-01-2015 дата публикации

HERBICIDAL COMPOSITION

Номер: US20150018214A1
Автор: Okamoto Hiroyuki, Terada Takashi, Yamada Ryu
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

To provide a high active herbicidal composition having a broad herbicidal spectrum. 1. A herbicidal composition comprising synergistically effective amounts of (A) pyridate or its salt and (B) at least one sulfonylurea compound selected from the group consisting of flazasulfuron , nicosulfuron , trifloxysulfuron , chlorimuron and its alkyl ester , halosulfuron and its alkyl ester , and their salts.2. The herbicidal composition according to claim 1 , wherein the mixing ratio of (A) to (B) is from 500:1 to 1:2.5 by the weight ratio.3. A method for controlling undesired plants or inhibiting their growth claim 1 , which comprises applying the herbicidal composition as defined in in synergistically effective amounts to the undesired plants or to a place where they grow.4. The method according to claim 3 , wherein (A) is applied in an amount of from 200 to 5 claim 3 ,000 g/ha and (B) is applied in an amount of from 10 to 500 g/ha.5kyllinga.. The method according to claim 3 , wherein the undesired plant is green6kyllinga. The method according to claim 3 , wherein the undesired plant is green having lowered sensitivity to herbicides.7kyllingakyllinga. A method for controlling green or inhibiting its growth claim 3 , which comprises applying a herbicidally effective amount of (A) pyridate or its salt to the green or to a place where it grows.8kyllingakyllinga. The method according to claim 7 , wherein the green is green having lowered sensitivity to herbicides.9. The method according to claim 7 , wherein (A) pyridate or its salt is applied in an amount of from 200 to 5 claim 7 ,000 g/ha. The present invention relates to a herbicidal composition and a method for controlling undesired plants.Patent Document 1 discloses a herbicidal composition comprising nicosulfuron and a specific known herbicide, and discloses pyridate as an example of the known herbicide.However, it has not been known that a herbicidal composition comprising synergistically effective amounts of (A) pyridate ...

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Номер записи: 81
21-01-2021 дата публикации

Method of Manufacturing an antiviral super treatment

Номер: US20210015837A1
Автор: Stafford Vivi R.
Принадлежит:

Method of Manufacturing an antiviral super pill or syrup for the treatment of viral infection such as SARS-CoV-2 (Covid 19). A cyclin antibiotic as well as a macrolide antibiotic are combined within the same compounded pill or capsule for the treatment of viruses. Doxycycline, a cyclin, binds to the 30S ribosomal subunit, and presumably to the 50S ribosomal subunit, thereby blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex, Azithromycin, a macrolide, reversibly binds to the 50S ribosomal subunit of the 70S ribosome of sensitive microorganisms, thereby inhibiting the translocation step of protein synthesis, wherein a newly synthesized peptidyl tRNA molecule moves from the acceptor site on the ribosome to the peptidyl (donor) site, and consequently inhibiting RNA-dependent protein synthesis leading to cell growth inhibition and cell death. As a result, this combination can provide immunity from certain viruses, such as Coronavirus 2019 (Covid 19) when given at the same time of a nasopharyngeal exposure to virus particles within numbers greater or less than 1000 virions, as a treatment regimen for a cure or as a prophylaxis for those exposed or were presumably exposed. 1. Compounding together for a cyclin such as Doxycycline 25 to 100 mg twice a day for the treatment of viral infections including Coronavirus or Covid 19 in combination with a Macrolid such as Azithromycin 250 mg daily either in a tablet , capsule , liquid suspension or packet.2. Vaccination of humans infected with a virus including SARS-CoV-19 through the intentional exposure to a patient of virions simultaneously or followed by the administration of a cyclin such as Doxycyline and a macrolid such as Azithromycin.3. Compounding of a cyclin such as Doxycycline and a macrolid such as Azithromycins for biofilm treatment such as an approach in decreasing the incidence of drug resistant strands to germs. Method of Manufacturing an antiviral super pill or syrup for the treatment of viral ...

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Номер записи: 82
26-01-2017 дата публикации

Fumarate compounds, pharmaceutical compositions thereof, and methods of use

Номер: US20170020837A1
Автор: Mark Quang NGUYEN
Принадлежит: Individual

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.

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Номер записи: 83
28-01-2016 дата публикации

METHOD FOR HANDLING SOLIDS CAPABLE OF DEFLAGRATION

Номер: US20160023178A1
Автор: MORHENN Heinrich, SALG Steffen
Принадлежит: BAYER TECHNOLOGY SERVICES GMBH

Method of processing and handling solids and mixtures capable of deflagration, in particular of processing materials capable of deflagration in the chemical and pharmaceutical industry, wherein the processing and handling is carried out in an environment under a reduced pressure of ≦500 mbara and the processing and/or handling comprises one or more process steps selected from the group consisting of filtration, milling, sieving, mixing, homogenization, granulation, compacting, packaging, drying, storage and transport in a transport container and other steps in apparatuses having mechanical internals. 1: Method of processing and/or handling solids and mixtures capable of deflagration , wherein the processing and/or handling is carried out in an environment under a reduced pressure of ≦500 mbara and the processing and/or handling comprises one or more process step selected from the group consisting of filtration , milling , sieving , mixing , homogenization , granulation , compacting , packaging , drying , storage and transport in a transport container and other steps in apparatuses having mechanical internals.2: Method according to claim 1 , wherein the process step is transport in transport screws or by means of star feeders.3: Method according to claim 1 , wherein the process step is carried out in a ploughshare mixer claim 1 , screw mixer or another mixer having mechanical mixing and/or chopping tools.4: Method according to claim 1 , wherein the process step is carried out in a flat-bed filter claim 1 , an oscillating sieve claim 1 , a rotational sieve and/or another filtration or sieving device having mechanical tools.5: Method according to claim 1 , wherein the process step is carried out in a roller crusher claim 1 , spiked roller crusher or toothed roller crusher mill or another comminution apparatus.6: Method according to claim 1 , wherein the process step is carried out in a paddle dryer claim 1 , plate dryer or fluidized-bed dryer.7: Method according to ...

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Номер записи: 84
22-01-2015 дата публикации

Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia

Номер: US20150024032A1
Автор: David J. Tweardy, Marvin X. Xu, Moses M. Kasembeli, Thomas Kristian Eckols
Принадлежит: Baylor College of Medicine

Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

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Номер записи: 85
26-01-2017 дата публикации

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Номер: US20170022153A1
Автор: Nguyen Mark Quang
Принадлежит:

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein each Ris independently chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , and benzyl.3. The compound according to claim 1 , wherein each Ris independently chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , and phenyl.4. The compound according to claim 1 , wherein each Ris independently chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , and phenyl.5. The compound according to claim 1 , wherein each Wis independently chosen from —S(O)N(R)— claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , and tert-butyl.6. The compound according to claim 1 , wherein each Wis —S(O)NH—.7. The compound according to claim 1 , wherein each Xis independently chosen from methane-diyl claim 1 , ethane-1 claim 1 ,1-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,3-diyl claim 1 , 2-methylpropane-1 claim 1 ,1-diyl claim 1 , 2-methylpropane-1 claim 1 ,2-diyl claim 1 , 2 claim 1 ,2-dimethylpropane-1 claim 1 ,3-diyl claim 1 , butane-1 claim 1 ,2-diyl claim 1 , butane-1 claim 1 ,3-diyl claim 1 , butane-1 claim 1 ,4-diyl ...

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Номер записи: 86
17-04-2014 дата публикации

HERBICIDAL COMPOSITION

Номер: US20140106971A1
Автор: Kezuka Tomoaki, Kikugawa Hiroshi, Terada Takashi, Yamada Ryu
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

At present, many herbicidal compositions have been developed and used, but there are a variety of types of weeds to be controlled, and their development lasts for a long period of time. Thus, a high active and long-residual herbicidal composition having a broad herbicidal spectrum has been desired. 1. A method for controlling undesired plants or inhibiting their growth , which comprises applying a synergistic herbicidally effective amount of (A) flazasulfuron or its salt and (B) duiron or its salt , to the undesired plants or to a place where they grow.2. The method according to claim 1 , wherein (A) is applied in an amount of from 10 to 150 g/ha claim 1 , and (B) is applied in an amount of from 150 to 5 claim 1 ,000 g/ha.3. The method according to claim 1 , wherein (A) is applied in an amount of from 30 to 50 g/ha claim 1 , and (B) is applied in an amount of from 1 claim 1 ,100 to 2 claim 1 ,000 g/ha. The present application is a continuation of U.S. application Ser. No. 13/700,769, which is a National Stage of International Patent Application No. PCT/JP2011/063625 filed Jun. 8, 2011, which claims priority to Japanese Application No. 2010-135400, filed Jun. 14, 2010 and Japanese Application No. 2010-229645 filed Oct. 12, 2010. The disclosures of U.S. application Ser. No. 13/700,769 and International Patent Application No. PCT/JP2011/063625 are incorporated by reference herein in their entireties.The present invention relates to a synergistic herbicidal composition comprising (A) flazasulfuron or its salt (hereinafter referred to as compound A) and (B) at least one urea compound selected from the group consisting of tebuthiuron, diuron and metobromuron or its salt (hereinafter referred to as compound B).Various heribicidal compositions have been studied to control undesired plants (hereinafter simply referred to as weeds) in agricultural fields and non-crop land. For example, Patent Document 1 discloses a mixture comprising a sulfonylurea herbicide, diuron and ...

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Номер записи: 87
25-01-2018 дата публикации

CRYSTALLINE MODIFICATION OF N-(2-(3-PHENYLUREIDO)PHENYL)BENZENESULFONAMIDE AND RECORDING MATERIAL USING SAME

Номер: US20180022136A1
Автор: KINOSHITA Shuntaro, Sakai Hiroshi
Принадлежит: NIPPON SODA CO., LTD.

The disclosure provides a novel crystal form of N-(2-(3-phenylureido)phenyl)benzenesulfonamide, which is crystalline modification thereof specified by an X-ray diffraction diagram having peaks at diffraction angles (2θ±0.1°) of 23.60°, 20.80°, 12.24° and 13.80° in a powder X-ray diffractometry using Cu-Kα ray. 1. A crystalline modification of N-(2-(3-phenylureido)phenyl)benzenesulfonamide specified by an X-ray diffraction diagram having peaks at diffraction angles (2θ±0.1°) of 23.60° , 20.80° , 12.24° and 13.80° in a powder X-ray diffractometry using Cu-Kα ray.2. The crystalline modification of N-(2-(3-phenylureido)phenyl)benzenesulfonamide according to claim 1 , wherein a melting point is 160-162° C.3. A recording material comprising a color former claim 1 , wherein the recording material comprises the crystalline modification of N-(2-(3-phenylureido)phenyl)benzenesulfonamide according to .4. A recording sheet having a recording material layer formed from the recording material according to .5. A recording material comprising a color former claim 2 , wherein the recording material comprises the crystalline modification of N-(2-(3-phenylureido)phenyl)benzenesulfonamide according to .6. A recording sheet having a recording material layer formed from the recording material according to . The present invention relates to a novel crystal form of N-(2-(3-phenylureido)phenyl)benzenesulfonamide. The present application claims priority of Japanese Patent Application No. 2015-035568 filed on Feb. 25, 2015 and priority of Japanese Patent Application No. 2015-065613 filed on Mar. 27, 2015, the contents of which are incorporated herein by reference.The recording material employing color development through a reaction between a color former and a color-developing agent, since record may be made by a relatively simple apparatus in a short time without applying a complicated treatment such as development and fixation, are widely used in e.g., thermal recording paper for output- ...

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Номер записи: 88
10-02-2022 дата публикации

FLUORINATED AMINE OXIDE SURFACTANTS

Номер: US20220040655A1
Автор: Kehren Jason M., Savu Patricia M., Untiedt Nicholas L.
Принадлежит:

Compositions including one or more fluorochemical surfactants of the formula: (I) where Ris a perfluoroalkyl group, each of R, Rand Rare C-Calkyl, alkoxy, or aryl; and Ris alkylene, arylene of a combination thereof. Ris preferably an alkylene of 1-20 carbons that may be cyclic or acyclic, may optionally contain catenated or terminal heteroatoms selected from the group consisting of N, O, and S. Most preferably Ris an alkylene of 2-10 carbon atoms. Described are anionic N-substituted fluorinated amine oxide surfactants, and use thereof in cleaning and in acid etch solutions. The cleaning and etch solutions are used with a wide variety of substrates, for example, in the cleaning and etching of silicon oxide-containing substrates. 2. The composition of claim 1 , wherein Ris from 3 to 5 carbon atoms.3. The composition of claim 1 , wherein the surfactant is present at a concentration of at least 0.001 wt. % of the composition.4. The composition of claim 1 , wherein the surfactant is present at a concentration of up to 1 weight percent of the composition.5. The composition of having less than 500 ppb of ionic contaminants.6. The composition of claim 1 , wherein the optional solvent is a water-soluble organic solvent.7. The composition of comprising less than 1 wt % organic solvent.8. The composition of claim 1 , wherein said composition further comprises iii) one or more additives selected from the group consisting of abrasive particles claim 1 , other acids claim 1 , oxidizing agents claim 1 , etchants claim 1 , corrosion inhibitors claim 1 , chelating agents claim 1 , electrolytes claim 1 , surfactants claim 1 , brighteners claim 1 , and levelers.9. A composition comprising: a) at least 0.001 weight percent of the surfactant of ; b) optional aqueous solvent; and c) oxidizing agent.10. The composition of claim 9 , wherein said oxidizing agent is selected from the group consisting of nitric acid claim 9 , HNO claim 9 , HO claim 9 , Fe(NO) claim 9 , O claim 9 , and ...

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Номер записи: 89
24-01-2019 дата публикации

COMPOUND HAVING ENHANCING ACTIVITY FOR GLUCAGON-LIKE PEPTIDE-1 RECEPTOR ACTIONS

Номер: US20190022039A1
Автор: FUJII Tomohiro, KITAHARA Yoshiro, Kitajima Seiji, Ohsumi Koji
Принадлежит: AJINOMOTO CO., INC.

Compounds represented by formula (I): 2. The compound or salt according to claim 1 , wherein{'sub': '6-14', 'A is a Caryl group or a 5- or 6-membered monocyclic aromatic heterocyclic group, each of which is optionally further substituted,'}L is a bond or a methylene group,Q is an oxygen atom,{'sup': 4', '5, 'sub': '1-6', 'Rand Rare the same or different and are each independently a hydrogen atom or an optionally substituted Calkyl group, and'}n is 1 or 2.3. The compound or salt according to claim 1 , wherein{'sub': 1-6', '1-6', '1-6', '1-3', '1-6', '1-6', '1-6', '1-3, 'A is a phenyl group optionally further substituted by the same or different 1 to 5 substituents selected from the group consisting of a halogen atom, a hydroxy group, a carboxy group, a sulfanyl group, an optionally substituted Calkyl group, an optionally substituted Calkoxy group, an optionally substituted amino group, a Calkylthio group optionally substituted by a halogen atom, and a Calkylenedioxy group, or a pyridyl group optionally further substituted by the same or different 1 to 4 substituents selected from the group consisting of a halogen atom, a hydroxy group, a carboxy group, a sulfanyl group, an optionally substituted Calkyl group, an optionally substituted Calkoxy group, an optionally substituted amino group, a 4- to 7-membered monocyclic non-aromatic heterocyclic group, a Calkylthio group optionally substituted by a halogen atom, and a Calkylenedioxy group,'}{'sub': 1-6', '1-6', '1-6', '1-3, 'B is a benzene ring optionally further substituted by the same or different 1 to 4 substituents selected from the group consisting of a halogen atom, a hydroxy group, a sulfanyl group, an optionally substituted Calkyl group, an optionally substituted Calkoxy group, an optionally substituted amino group, a Calkylthio group optionally substituted by a halogen atom, a Calkylenedioxy group, and a 4- to 7-membered monocyclic non-aromatic heterocyclic group,'}L is a bond or a methylene group,{'sup': '1', ...

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Номер записи: 90
17-04-2014 дата публикации

CCR9 INHIBITORS AND METHODS OF USE THEREOF

Номер: US20140107160A1
Автор: Chen B. Shaowu, FLEMING PAUL E., Harriman Geraldine C.B., Shi Zhan
Принадлежит: Millennium Pharmaceuticals, Inc.

The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods. 2. The compound of claim 1 , wherein Aris a substituted or unsubstituted group selected from pyrid-4-yl claim 1 , N-oxido pyrid-4-yl claim 1 , pyrimidinyl claim 1 , and pyrazinyl.4. The compound of claim 3 , wherein Aris a substituted or unsubstituted group selected from phenyl claim 3 , naphthyl claim 3 , thienyl claim 3 , and thianaphthenyl.5. The compound of claim 3 , wherein Aris a substituted or unsubstituted group selected from phenyl and pyridyl.6. The compound of claim 3 , wherein Aris a substituted or unsubstituted group selected from phenyl and thienyl.7. The compound of claim 3 , wherein Aris unsubstituted or is substituted with one or more substituents selected from substituted aliphatic claim 3 , unsubstituted aliphatic claim 3 , aryl claim 3 , arylalkyl claim 3 , substituted alkoxy claim 3 , unsubstituted alkoxy claim 3 , aryloxy claim 3 , arylalkoxy claim 3 , alkylthio claim 3 , halo claim 3 , nitro claim 3 , cyano claim 3 , S(O)-(aliphatic) claim 3 , S(O)-(aliphatic) claim 3 , NRS(O)-(aliphatic) claim 3 , C(O)N(R) claim 3 , C(O)R claim 3 , N(R) claim 3 , NRC(O)R claim 3 , and NRC(O)R claim 3 , wherein Rfor each occurrence is independently H or an aliphatic group claim 3 , and Ris an aliphatic group.8. The compound of claim 3 , wherein Aris unsubstituted or is substituted with one or more substituents selected from aliphatic claim 3 , alkoxy claim 3 , and haloalkoxy.9. The compound of claim 3 , wherein one or both rings A and B are unsubstituted or are independently substituted with a substituent selected from halo claim 3 , aliphatic claim 3 , alkoxy claim 3 , and haloalkyl.10. The compound ...

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Номер записи: 91
25-01-2018 дата публикации

PROCESS FOR FLUORINATION OF SULPHONYL HALIDE COMPOUNDS

Номер: US20180022694A1
Автор: METZ François
Принадлежит:

The present disclosure relates to the preparation of a compound of formula (I) comprising an —SOF function, R—SOF, by reacting a compound of formula (II), R′—SOX, with a fluorinating agent, the process carried out in the liquid phase in the presence of hydrofluoric acid using an antimony-based fluorination catalyst, wherein R, R′, and X are described herein. 1. A non-electrochemical process for preparing a fluorinated compound of formula (I) comprising at least one —SOF function , wherein the compound of formula (I) is prepared by reacting a compound of formula (II) with at least one fluorinating agent , wherein the process is carried out in the liquid phase in the presence of hydrofluoric acid using an antimony-based fluorination catalyst:{'br': None, 'sub': '2', 'R—SOF \u2003\u2003(I)'}where R is selected from the group consisting of R1, R2 and R3:{'sub': n', 'a', 'b, 'R1=—CHFwith n=1-10, a+b=2n+1, b≧1;'}{'sub': x', 'y', 'z', '2, 'R2=—CHF—SOF with x=1-10, y+z=2x and z≧1;'}{'sub': c', 'h', 'f, 'claim-text': {'br': None, 'sub': '2', 'R′—SOX \u2003\u2003(II)'}, 'R3=Φ-CHFwith c=1-10; h+f=2c and f≧1; Φ denoting a phenyl group;'}where R′ is selected from the group consisting of R′1, R′2 and R′3:{'sub': n', 'a', 'b, 'R′1=—CHXwith n=1-10, a+b=2n+1, b≧1;'}{'sub': x', 'y', 'z', '2, 'R′2=—CHX—SOX with x=1-10, y+z=2x and z≧1;'}{'sub': c', 'h', 'f, 'R′3=Φ-CHXwith c=1-10; h+f=2c and f≧1; Φ denoting a phenyl group;'}X is a halogen atom selected from the group consisting of chlorine and bromine.2. The preparation process as claimed in claim 1 , wherein the radicals R1 and R′1 are perhalogenated so that b=3 and a=0.3. The preparation process as claimed in claim 1 , wherein the radical R of the compound (I) is the radical R1 wherein n=1 claim 1 , a=0 and b=3 claim 1 , or n=1 claim 1 , a=1 claim 1 , b=2 or else n=1 claim 1 , a=2 and b=1.4. The preparation process as claimed in claim 1 , wherein the compound of formula (II) is obtained by radical halogenation of a compound of formula ...

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Номер записи: 92
22-01-2015 дата публикации

BISARYLSULFONAMIDES USEFUL IN THE TREATMENT OF INFLAMMATION AND CANCER

Номер: US20150025068A1
Автор: Faernegardh Katarina, Joensson Mattias, Martinsson Jessica, Ringom Rune
Принадлежит:

A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. 2. A compound according to claim 1 , wherein{'sup': 4', '4', '4, 'A is O, S, —CR═CR— or —CR═N—; and'}{'sup': 4', '4', '4', '2', '3', '5', '2', '3', '5, 'when A is —CR═CR— or —CR═N—, one of Rand Ris selected from carbocyclyl-C0-C3 alkyl; carbocyclyl-C2-C3 alkenyl; heterocyclyl-C0-C3 alkyl; and heterocyclyl-C2-C3 alkenyl; wherein any carbocyclyl or heterocyclyl is 5- or 6-membered monocyclyl or 9- or 10-membered bicyclyl; and any carbocyclyl or heterocyclyl is optionally substituted with at least one R; or Rand Rform, together with the carbon atoms to which they are attached, a 5- or 6-membered carbocyclic or heterocyclic ring, which ring is optionally substituted with at least one R;'}or a pharmaceutically acceptable salt thereof.3. A compound according to claim 2 , wherein{'sup': 4', '4', '4, 'A is O, S, —CR═CR— or —CR═N—; and'}{'sup': 4', '4', '4', '2', '3', '2', '3', '5, 'when A is —CR═CR— or —CR═N—, Ris selected from carbocyclyl-C0-C3 alkyl; carbocyclyl-C2-C3 alkenyl; heterocyclyl-C0-C3 alkyl; and heterocyclyl-C2-C3 alkenyl; wherein any carbocyclyl or heterocyclyl is 5- or 6-membered monocyclyl or 9- or 10-membered bicyclyl; and Ris selected from H; halogen; and C1-C6 alkyl, optionally substituted with at least one halogen; or Rand Rform, together with the carbon atoms to which they are attached, a 5- or 6-membered carbocyclic or heterocyclic ring, which ring is optionally substituted with at least one R;'}or a pharmaceutically acceptable salt thereof.4. A compound according to claim 1 , wherein{'sup': 4', '4', '4, 'A is O, S, —CR═CR— or —CR═N—; and'}{'sup': 2', '3, 'when A is O or S, Rand Rare each independently selected from H; halogen; C1-C6 alkyl; C1-C6 alkoxy; carbamoyl; secondary or tertiary C1-C6 alkylamido; carbocyclylcarbonylamino-C0-C2 alkyl; 5- or 6-membered cyclic aminocarbonyl optionally ...

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Номер записи: 93
22-01-2015 дата публикации

SULFONYLUREA-TOLERANT SUNFLOWER PLANTS

Номер: US20150026836A1
Автор: GABARD JEROME M., HUBY JEAN-PIERRE
Принадлежит:

This invention relates to sunflower lines and hybrids tolerant to sulfonylurea herbicides wherein the tolerance trait is obtained using induced mutagenesis and artificial selection, and to a method for selectively controlling undesired vegetation, including parasitic weeds, by applying sulfonylurea herbicides to sulfonylurea-tolerant sunflower crops. 1. A method for producing a sunflower line containing a highly heritable trait conferring tolerance to sulfonylurea herbicides , wherein the method comprises:(a) treating sunflower seeds with a mutagenic agent;(b) growing the treated seeds into mature plants to produce second-generation seeds;(c) harvesting the second-generation seeds;(d) germinating the second-generation seeds in the presence of an selectably effective amount of a sulfonylurea herbicide to select for survival only germinated seeds containing a trait conferring tolerance to the sulfonylurea herbicide; and(e) growing a surviving germinated seed into a mature plant to produce through self-pollination seeds of the sunflower line containing the heritable trait.2. A sunflower seed containing a highly heritable trait conferring tolerance to sulfonylurea herbicides , wherein said trait is obtained through mutagenesis.3. A seed of designated sunflower line M7 claim 2 , representative seed of said line M7 having been deposited under ATCC Deposit Nos. PTA-2295 and PTA-2296.4. A seed of designated sunflower line M11 claim 2 , representative seed of said line M11 having been deposited under ATCC Deposit Nos. PTA-2767 and PTA-2768.5. A seed of designated sunflower line M12 claim 2 , representative seed of said line M12 having been deposited under ATCC Deposit Nos. PTA-2769 and PTA-2770.6. A sunflower plant claim 2 , or a part thereof claim 2 , grown from a seed of claim 2 , or .7Orobanche. A seed of further containing a trait conferring resistance to parasitism.8. A sunflower plant claim 2 , or a part thereof claim 2 , produced by growing the seed of .9. Pollen of ...

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Номер записи: 94
29-01-2015 дата публикации

Pharmaceutical Formulations of HDAC Inhibitors

Номер: US20150031770A1
Автор: Bastin Richard J., Hughes Nicholas J.
Принадлежит:

This invention pertains to pharmaceutical compositions comprising certain carbamic acid compounds (e.g., which inhibit HDAC (histone deacetylase) activity) (e.g., PXD-101, N hydroxyl-3-(3-phenylsulfamoyl-phenyl)-acrylamide)) and one or more additional ingredients selected from cyclodextrin, arginine, and meglumine. The present invention also pertains to the use of such compositions, for example, in the inhibition of HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc. 4. A pharmaceutical composition according to claim 1 , further comprising meglumine.5. A pharmaceutical composition according to claim 1 , wherein said cyclodextrin is selected from:α-cyclodextrin; β-cyclodextrin; γ-cyclodextrin;(C1-4alkyl)-α-cyclodextrin; (C1-4alkyl)-β-cyclodextrin; (C1-4alkyl)-γ-cyclodextrin;(hydroxy-C1-4alkyl)-α-cyclodextrin; (hydroxy-C1-4alkyl)-β-cyclodextrin; (hydroxy C1 4alkyl)-γ-cyclodextrin;(carboxy-C1-4alkyl)-α-cyclodextrin; (carboxy-C1-4alkyl)-β-cyclodextrin; (carboxy C1 4alkyl)-γ-cyclodextrin;saccharide ethers of α-cyclodextrin; saccharide ethers of β-cyclodextrin; saccharide ethers of γ-cyclodextrin;sulfobutyl ethers of α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin.6. A pharmaceutical composition according to claim 1 , wherein said cyclodextrin is hydroxypropyl-β-cyclodextrin.7. A pharmaceutical composition according to claim 1 , wherein the molar ratio of cyclodextrin to said HDAC inhibitor is from 0.5 to 5.8. A pharmaceutical composition according to claim 1 , which is a liquid.9. A pharmaceutical composition according to claim 1 , which comprises said HDAC inhibitor at a concentration of 0.1-1000 mg/mL.10. A pharmaceutical composition according to claim 1 , which comprises said HDAC inhibitor at a concentration of 30-300 mg/mL.11. A pharmaceutical composition according to claim 1 , which comprises said HDAC inhibitor at a concentration of 0.3-3000 mM.12. A pharmaceutical composition according to claim 1 , which ...

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Номер записи: 95
04-02-2016 дата публикации

Cycloalkyl-dione derivatives and methods of their use

Номер: US20160031805A1
Автор: Amos B. Smith, Carlo Ballatore, John Q. Trojanowski, Kurt R. Brunden, Virginia M.Y. Lee, Xiaozhao Wang
Принадлежит: University of Pennsylvania Penn

The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R 1 is H or C 1-6 alkyl and R 2 is H, C 1-6 alkyl, C 1-6 alkaryl, aryl, or heteroaryl; and X is O or NH. Tautomers, enantiomers, and diastereomers, as well as pharmaceutically acceptable salt forms, of compounds of formula I are also within the scope of the invention. Methods of preparing and using the compounds of formula I are also described. wherein A is

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Номер записи: 96
04-02-2016 дата публикации

SYNTHESIS OF TETRABUTYLAMMONIUM BIS(FLUOROSULFONYL)IMIDE AND RELATED SALTS

Номер: US20160031806A1
Автор: JOHNSON Martin Reid
Принадлежит:

The present invention is directed to methods comprising adding ammonia, either as an ammonium salt or as a gas at pressures below 0.01 MPa, to a sulfuryl fluoride solution to form the anion of bis(fluorosulfonyl)amine under conditions well suited for large-scale production. The bis(fluorosulfonyl)amine so produced can be isolated by methods described in the prior art, or isolated as an organic ion pair, such as an alkylammonium solid salt, or as an ionic liquid. 1. A process for producing a salt of bis(fluorosulfonyl) imide anion (M[(FSO)N] , wherein M is an inorganic or organic cation and x , n and m are integers from 1-4 , comprising:{'sub': 2', '2, 'adding sulfuryl fluoride (SOF) to solid ammonium fluoride in a solvent in a reactor, in the presence of an aprotic base; and'}isolating said salt.2. The process of claim 1 , wherein the step of adding sulfuryl fluoride (SOF) to solid ammonium fluoride in a solvent in a reactor claim 1 , in the presence of an aprotic base claim 1 , comprisesproviding solid ammonium fluoride to the solvent in the reactor;{'sub': 2', '2, 'providing the aprotic base and an initial amount of sulfuryl fluoride (SOF) in the reactor; and'}{'sub': 2', '2, 'continuously adding an additional amount of SOFto reach a pre-determined stoichiometry.'}3. The process of claim 2 , wherein the pre-determined stoichiometry of ammonium fluoride to SOFis in a molar ratio in the range from 1:3 to 1.1:2.4. The process of claim 1 , wherein sulfuryl fluoride (SOF) is added to a suspension claim 1 , pellet claim 1 , or other form of solid ammonium fluoride in the solvent.5. The process of claim 1 , wherein the reactor is a sealed reactor.6. The process of claim 5 , further comprising applying vacuum to the sealed reactor.7. The process of claim 1 , wherein the solvent is selected from the group consisting of acetonitrile claim 1 , propionitrile claim 1 , diethyl ether claim 1 , tetrahydrofuran claim 1 , butyronitrile claim 1 , dimethylformamide claim 1 , ...

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Номер записи: 97
31-01-2019 дата публикации

Use of Herbicide-tolerant Protein

Номер: US20190029252A1
Автор: Bao Xiaoming, DING Derong, PANG Jie, TAO Qing, XIE Xiangting
Принадлежит:

The present invention relates to the use of a herbicide-tolerant protein, wherein the method for controlling weeds comprises applying a herbicide containing an effective dose of tribenuron-methyl to a plant growth environment where at least one transgenic plant is present, wherein the transgenic plant comprises a nucleotide sequence encoding a thifensulfuron hydrolase in its genome, and compared to other plants without the nucleotide sequence encoding the hydrolase, the transgenic plant has reduced plant damage and/or an increased plant yield. The present invention discloses for the first time that a thifensulfuron hydrolase can show a high tolerance to a tribenuron-methyl herbicide, plants containing a nucleotide sequence encoding the thifensulfuron hydrolase are strongly tolerant to the tribenuron-methyl herbicide and can at least tolerate 1-fold field concentration, and thus the hydrolase has broad application prospects in plants. 1. A method for controlling weeds , characterized in that the method comprises applying a herbicide containing an effective dose of tribenuron-methyl to a plant growth environment where at least one transgenic plant is present , wherein the transgenic plant comprises a nucleotide sequence encoding a thifensulfuron hydrolase in its genome , and compared to other plants without the nucleotide sequence encoding the thifensulfuron hydrolase , the transgenic plant has reduced plant damage and/or an increased plant yield.2. (canceled)3. (canceled)4Arabidopsis thaliana. The method for controlling weeds according to claim 1 , characterized in that the transgenic plant is maize claim 1 , soybean claim 1 , claim 1 , cotton claim 1 , rape claim 1 , rice claim 1 , sorghum claim 1 , wheat claim 1 , barley claim 1 , millet claim 1 , sugar cane or oat.5. The method for controlling weeds according to claim 1 , characterized in that the amino acid sequence of the thifensulfuron hydrolase comprises an amino acid sequence as shown in SEQ ID NO: 1 claim 1 ...

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Номер записи: 98
31-01-2019 дата публикации

APPLICATION FOR HERBICIDE-TOLERANT PROTEIN

Номер: US20190029257A1
Автор: DING Derong, TAO Qing, XIE Xiangting
Принадлежит:

The present invention relates to the use of a herbicide-tolerant protein, wherein the method for controlling weeds comprises applying a herbicide containing an effective dose of halosulfuron-methyl to a plant growth environment where at least one transgenic plant is present, wherein the transgenic plant comprises a nucleotide sequence encoding a thifensulfuron hydrolase in its genome, and compared to other plants without the nucleotide sequence encoding the hydrolase, the transgenic plant has reduced plant damage and/or an increased plant yield. The present invention discloses for the first time that a thifensulfuron hydrolase can show a high tolerance to a halosulfuron-methyl herbicide, plants containing a nucleotide sequence encoding the thifensulfuron hydrolase are strongly tolerant to the halosulfuron-methyl herbicide and can at least tolerate 1-fold field concentration, and thus the hydrolase has broad application prospects in plants. 1. A method for controlling weeds , characterized in that the method comprises applying a herbicide containing an effective dose of halosulfuron-methyl to a plant growth environment where at least one transgenic plant is present , wherein the transgenic plant comprises a nucleotide sequence encoding a thifensulfuron hydrolase in its genome , and compared to other plants without the nucleotide sequence encoding the thifensulfuron hydrolase , the transgenic plant has reduced plant damage and/or an increased plant yield.2. (canceled)3. (canceled)4Arabidopsis thaliana. The method for controlling weeds according to claim 31 , characterized in that the transgenic plant is maize claim 31 , soybean claim 31 , claim 31 , cotton claim 31 , rape claim 31 , rice claim 31 , sorghum claim 31 , wheat claim 31 , barley claim 31 , millet claim 31 , sugar cane or oat.5. The method for controlling weeds according to claim 1 , characterized in that the amino acid sequence of the thifensulfuron hydrolase comprises an amino acid sequence as shown in ...

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Номер записи: 99
01-02-2018 дата публикации

HEAT-RESISTANT ALIPHATIC-CHAIN SATURATED HYDROCARBON HAVING ION PAIRS AT BOTH ENDS, AND COMPOSITION USING SAME

Номер: US20180029992A1
Автор: Miyamoto Shinpei, Nishiura Koichi, Onishi Yoshifumi
Принадлежит: KANEKA CORPORATION

An aliphatic-chain saturated hydrocarbon including an aliphatic hydrocarbon chain which is saturated and has an ion pair at each end of the aliphatic hydrocarbon chain. 1. An aliphatic-chain saturated hydrocarbon , comprising:an aliphatic hydrocarbon chain which is saturated and has an ion pair at each end of the aliphatic hydrocarbon chain.2. The aliphatic-chain saturated hydrocarbon of claim 1 , wherein the aliphatic hydrocarbon chain has 18 or more carbon atoms.3. The aliphatic-chain saturated hydrocarbon of claim 1 , wherein the aliphatic hydrocarbon chain has an onium ion at an end of the aliphatic hydrocarbon chain claim 1 , and the onium ion forms the ion pair with an anion at the end of the aliphatic hydrocarbon chain.5. The aliphatic-chain saturated hydrocarbon of claim 4 , wherein R2 is a methyl group.6. The aliphatic-chain saturated hydrocarbon of claim 4 , wherein R1 is a hydrogen atom.7. The aliphatic-chain saturated hydrocarbon of claim 4 , wherein R3 is a hydrogen atom.8. The aliphatic-chain saturated hydrocarbon of claim 4 , wherein R4 is a hydrogen atom.9. The aliphatic-chain saturated hydrocarbon of claim 4 , wherein R2 is a methyl group claim 4 , and R1 claim 4 , R3 and R4 are each a hydrogen atom.12. The thermally conductive composition of claim 11 , further comprising:at least one conductive filler selected from the group consisting of aluminum, hexagonal boron nitride, and aluminum oxide.13. The thermally conductive composition of claim 11 , wherein z is an integer of 29 or larger.14. The thermally conductive composition of claim 11 , wherein m and n are each 1.15. The thermally conductive composition of claim 11 , wherein R2 is a methyl group.16. The thermally conductive composition of claim 11 , wherein R1 is a hydrogen atom.17. The thermally conductive composition of claim 11 , wherein R3 is a hydrogen atom.18. The thermally conductive composition of claim 11 , wherein R4 is a hydrogen atom.19. The thermally conductive composition of claim ...

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Номер записи: 100