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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 67883. Отображено 100.
10-10-2001 дата публикации

ТАБЛЕТКА

Номер: RU0000019762U1

Таблетка, представляющая собой твердую лекарственную форму антигипертензивного препарата, выполненная из фармацевтической композиции, включающей капторил и целевые добавки, отличающаяся тем, что в качестве целевых добавок содержит лактозу, микрокристаллическую целлюлозу, крахмал кукурузный, кислоту стеариновую и стеарат кальция, при следующем соотношении компонентов, мас.%: Каптоприл - 23,125-26,875 Лактоза - 47,7485-55,4915 Микрокристаллическая целлюлоза - 9,25-10,75 Крахмал кукурузный - 9,6015-11,1585 Кислота стеариновая - 1,8-2,2 Стеарат кальция - 0,9-1,1 (19) RU (11) 19 762 (13) U1 (51) МПК A61K 9/20 (2000.01) C07D 207/00 (2000.01) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К СВИДЕТЕЛЬСТВУ (21), (22) Заявка: 2001116993/20 , 28.06.2001 (24) Дата начала отсчета срока действия патента: 28.06.2001 (46) Опубликовано: 10.10.2001 (72) Автор(ы): Нестерук В.В., Сыров К.К. (73) Патентообладатель(и): Нестерук Владимир Викторович, Сыров Кирилл Константинович U 1 1 9 7 6 2 R U Ñòðàíèöà: 1 U 1 (57) Формула полезной модели Таблетка, представляющая собой твердую лекарственную форму антигипертензивного препарата, выполненная из фармацевтической композиции, включающей капторил и целевые добавки, отличающаяся тем, что в качестве целевых добавок содержит лактозу, микрокристаллическую целлюлозу, крахмал кукурузный, кислоту стеариновую и стеарат кальция, при следующем соотношении компонентов, мас.%: Каптоприл - 23,125-26,875 Лактоза - 47,7485-55,4915 Микрокристаллическая целлюлоза - 9,25-10,75 Крахмал кукурузный - 9,6015-11,1585 Кислота стеариновая - 1,8-2,2 Стеарат кальция - 0,9-1,1 1 9 7 6 2 (54) ТАБЛЕТКА R U Адрес для переписки: 121059, Москва, ул.Брянская, 3А, Е.Г.Павельевой (71) Заявитель(и): Нестерук Владимир Викторович, Сыров Кирилл Константинович RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1

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19-01-2012 дата публикации

Novel inhibitors of retroviral reverse transcriptace

Номер: US20120015874A1
Принадлежит: University of Missouri System

Disclosed are nucleic acid molecules, and methods of their use, which have a specific structure including a double helical domain and a G-quadruplex domain physically connected by a linker domain which may be nucleosidic or non-nucleosidic. These aptamers demonstrate potent inhibition of phylogenetically diverse primate lentiviral reverse transcriptases, which effect is largely independent of aptamer sequence provided that the aptamer has the specified structure.

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26-01-2012 дата публикации

Organic electronic device, compounds for same, and terminal

Номер: US20120018717A1
Принадлежит: Duksan Hi Metal Co Ltd

Disclosed are an organic electronic device and a compound thereof, and a terminal.

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26-01-2012 дата публикации

Bridged compounds as hiv integrase inhibitors

Номер: US20120022045A1
Принадлежит: Individual

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. 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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26-01-2012 дата публикации

Process for Preparing Dithiine-tetracarboxy-diimides

Номер: US20120022270A1
Принадлежит: Bayer CropScience AG

The present invention relates to a new process for preparing dithiine-tetracarboxy-diimides

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26-01-2012 дата публикации

Novel method for producing optically active pyrrolidine compound

Номер: US20120022271A1
Принадлежит: Astellas Pharma Inc

[Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate. [Selected Figure] None

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02-02-2012 дата публикации

3-biphenyl-substituted-3-substituted-4-ketolactam and ketolactone and their utilization as pesticide

Номер: US20120028804A1

The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.

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09-02-2012 дата публикации

Extracellular matrix compositions for tissue regeneration

Номер: US20120034191A1
Автор: Robert G. Matheny
Принадлежит: Individual

The invention is compositions of extracellular matrix that comprise mammalian extracellular matrix from two or more tissue sources in a mammal. The invention also includes methods of using these compositions to regenerate tissue or generate new tissue at sites of defects or wounds in mammals.

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08-03-2012 дата публикации

Novel Indicator Platform

Номер: US20120058503A1
Принадлежит: Biosynth AG

A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.

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15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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05-04-2012 дата публикации

Ionic liquids, the method for preparing the same and method for removing acetylenes from olefin mixtures using the ionic liquids

Номер: US20120083642A1

There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.

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24-05-2012 дата публикации

Materials for organic electroluminescent devices

Номер: US20120126179A1
Принадлежит: Merck Patent GmBH

The present invention relates to 4,4′-substituted spirobifluorenes which are suitable, owing to excellent properties, as functional materials in organic electroluminescent devices. In addition, the present invention relates to a process for the preparation of 4,4′-substituted spirobifluorenes and to the use of these compounds in organic electroluminescent devices.

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24-05-2012 дата публикации

Novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids and their uses as cooling compounds

Номер: US20120129827A1
Автор: Arkadiusz Kazimierski

The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R 1 , R 2 , R 3 , and R 4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R 5 is hydrogen or a C 1 -C 7 linear or branched acyclic hydrocarbon group, or R 5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

Embodiments provide a light emitting device material characterized by containing an anthracene compound represented by the following general formula. where R 19 to R 37 are a hydrogen atom, alkyl group, cycloalkyl group, heterocyclic group or the like; n is 1 or 2; and A is a heteroarylene group or arylene group. Any one of the R 19 to R 27 and any one of the R 28 to R 37 are used for linking with A. The present teachings allow a light emitting device having high luminous efficiency and excellent durability.

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14-06-2012 дата публикации

Multi-layered gradient vaginal ring

Номер: US20120148655A1
Принадлежит: Population Council Inc

Multi-layered vaginal rings 2 comprising silicone elastomers and pharmaceutically active ingredients are disclosed. The rings comprise a number of layers, at least one of which contains a pharmaceutically active ingredient, and each of which is a silicone elastomer. The multiple layers preferably are produced from these layers of different compositions, including an inner layer 4, a middle layer 5, and an outer layer 6. After extrusion and simultaneous curing, however, the ring 2 includes a contiguous body which comprises a continuous silicone body providing unimpeded diffusion of the pharmaceutically active ingredient from the inner layer (s) 4 to the outer layer (s) 6. Methods of producing these vaginal rings and of using them are also disclosed.

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14-06-2012 дата публикации

Multifunctional linkers and methods for the use thereof

Номер: US20120149653A1
Принадлежит: RGo Bioscience LLC

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

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21-06-2012 дата публикации

Trihydroxy polyunsaturated eicosanoid derivatives

Номер: US20120157700A1
Автор: Nicos A. Petasis
Принадлежит: University of Southern California USC

The invention features methods for the preparation of naturally occurring trihydroxy polyunsaturated eicosanoids and their structural analogs. The invention further provides new derivatives and analogs of trihydroxy polyunsaturated eicosanoids that can be prepared according to these methods. The invention also provides compositions and methods using trihydroxy polyunsaturated eicosanoid derivatives for the prevention, amelioration and treatment of a variety of diseases or conditions associated with inflammation or inflammatory response, autoimmune diseases, rheumatoid arthritis, cardiovascular diseases, or abnormal cell proliferation or cancer.

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28-06-2012 дата публикации

Stabilized microbicidal composition

Номер: US20120165376A1
Принадлежит: Individual

A microbicidal composition having at least four components. The first component is 2-25 wt % of 2,2-dibromo-3-nitrilopropionamide. The second component is 2-30 wt % water. The third component is 5-30 wt % of an aliphatic compound having 2-6 hydroxyl groups. The fourth component is 20-70 wt % of a glycol solvent.

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12-07-2012 дата публикации

Polymerizable composition, color filter, and method of producing the same, solid-state imaging device, and planographic printing plate precursor, and novel compound

Номер: US20120176571A1
Автор: Masaomi Makino
Принадлежит: Fujifilm Corp

Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R 3 and R 4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R 3 and R 4 may form a ring with each other; and X represents OR 5 , SR 6 , or NR 17 R 18 . The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.

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12-07-2012 дата публикации

Inhibition of nfk-b mediated virus replication with specific oligosaccharides

Номер: US20120178671A1
Принадлежит: Nutricia NV

The inventors surprisingly found that specific oligosaccharides are capable of inhibiting viral replication through inhibiting NF-κB activation. The invention thus pertains to a composition comprising pectin (in the form of digalacturonic acid, trigalacturonic acid, polygalacturonic acid), Arabinoxylan from rice bran, β-glucan from bakers yeast, D-Ribose or mixtures there-of for inhibiting viral replication in a mammal with a viral disease.

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19-07-2012 дата публикации

Process for preparation of phenyl carbamate derivatives

Номер: US20120184762A1
Автор: Yong Moon Choi
Принадлежит: Bio Pharm Solutions Co Ltd

Provided are a process for the preparation of phenyl carbamate derivatives, useful in the treatment of CNS (central nervous system) disorders, an intermediate in the synthesis of the phenyl carbamate derivatives, and a process for preparation of the intermediate.

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09-08-2012 дата публикации

Treatment and prevention of hiv infection

Номер: US20120201868A1
Принадлежит: Individual

This invention relates to the long term treatment of HIV infection by intermittently administering a parenteral formulation comprising brecanavir at relatively long time intervals. This invention further concerns pharmaceutical compositions for parenteral administration, comprising micro- or nanoparticles of brecanavir, suspended in an aqueous pharmaceutically acceptable carrier, for the treatment and prophylaxis of HIV infection.

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16-08-2012 дата публикации

Modified agrin-fragment capable of restoring muscle strength for use as a medicament

Номер: US20120208765A1
Принадлежит: NEUROTUNE AG

Modified agrin fragment having in vivo activity, comprising at least the domains LG2 and LG3 of human agrin in covalently interlinked form and modified in such a way that the fragment cannot be cleaved by neurotrypsin for use as medicament.

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23-08-2012 дата публикации

Organic light emitting device and flat panel display device comprising the same

Номер: US20120211733A1
Принадлежит: Samsung Mobile Display Co Ltd

Provided are an organic light emitting device including: a substrate; a first electrode; a second electrode; and an organic layer interposed between the first electrode and the second electrode and including an emission layer, wherein one of the first electrode and the second electrode is a reflective electrode and the other is a semitransparent or transparent electrode, and wherein the organic layer includes a layer having at least one of the compounds having at least one carbazole group, and a flat panel display device including the organic light emitting device. The organic light emitting device has low driving voltage, excellent current density, high brightness, excellent color purity, high efficiency, and long lifetime.

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30-08-2012 дата публикации

Process for reduction of alpha-acyloxy sulfide derivatives

Номер: US20120220784A1
Принадлежит: Scinopharm Singapore Pte Ltd

The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding α-acyloxy sulfides.

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06-09-2012 дата публикации

Process for preparing alpha-carboxamide derivatives

Номер: US20120226053A1
Автор: Matthew Allen Zajac
Принадлежит: Convergence Pharmaceuticals Ltd

The present application provides a process for the preparation of α-carboxamide pyrrolidine derivatives of formula (I), wherein R 1 and R 2 are independently hydrogen, C 1-6 alkyl or C 3-6 cycloalkylC 1-6 alkyl; or such R 1 and R 2 , together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R 5 is independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; either R 6 or R 7 is —O—R 8 , —OCHR 9 R 8 ,—NCH 2 R 8 or —(CH 2 ) 2 R 8 wherein the other R 6 or R 7 is hydrogen or R 5 ; and wherein R 8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; and R 9 is hydrogen or C 1-3 alkyl.

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20-09-2012 дата публикации

Luminogen compounds and the use of the same for biosensing and cellular imaging

Номер: US20120237964A1

Provided herein are a luminogen compound of formula (I) including a AIE luminophore moiety conjugated with a maleimide moiety and a use of the same for detecting thiol groups in biomolecules. Also provided is a dye molecule, a biosensor or a bioprobe comprising the luminogen compound of formula (I) in use for detecting thiol groups in biomolecules. The detection method of the present subject matter not only has high thio-selectivity and sensitivity, but also is rapid, convenient and handy.

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04-10-2012 дата публикации

HUMAN LYMPHOID TISSUE INDUCER (LTi) CELL COMPOSITIONS AND METHODS OF USE

Номер: US20120251505A1

The invention provides human lymphoid tissue inducer (LTi) cells, methods of producing human lymphoid tissue inducer (LTi) cells, and methods of using human lymphoid tissue inducer (LTi) cells. Such methods include treatment of a subject that would benefit from human lymphoid tissue inducer (LTi) cells, for example, an immunocompromised or immunosuppressed subject.

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04-10-2012 дата публикации

Processes for the synthesis of bazedoxifene acetate and intermediates thereof

Номер: US20120253038A1
Принадлежит: SANDOZ AG

Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.

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25-10-2012 дата публикации

Novel Polymorphs of Efavirenz

Номер: US20120271047A1
Принадлежит: Hetero Drugs Ltd

The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.

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29-11-2012 дата публикации

Process of making alpha-aminooxyketone/alpha-aminooxyaldehyde and alpha-hydroxyketone/alpha-hydroxyaldehyde compounds and a process making reaction products from cyclic alpha, beta-unsaturated ketone substrates and nitroso substrates

Номер: US20120302792A1
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

The present invention is directed to a process of making α-aminooxyketone and α-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein X a -X c represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the α-aminooxyketone compound formed to the α-hydroxyketone compound. The present invention results in α-aminooxyketone and α-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic α,β-unsaturated ketone substrate and a nitroso substrate. This methodology generally involves reacting the cyclic α,β-unsaturated ketone substrate and the nitroso substrate in the presence of a proline-based catalyst, to provide a heterocyclic product.

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06-12-2012 дата публикации

HIV Integrase Inhibitors

Номер: US20120309698A1
Принадлежит: Bristol Myers Squibb Co

The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

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06-12-2012 дата публикации

Organic compound, anthracene derivative, and light-emitting element, light-emitting device, and electronic device using anthracene derivative

Номер: US20120309984A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

Objects of the present invention are to provide novel anthracene derivatives and novel organic compounds; a light-emitting element that has high emission efficiency; a light-emitting element that is capable of emitting blue light with high luminous efficiency; a light-emitting element that is capable of operation for a long time; and a light-emitting device and an electronic device that have lower power consumption. An anthracene derivative represented by a general formula (1) and an organic compound represented by a general formula (17) are provided. A light-emitting element that has high emission efficiency can be obtained by use of the anthracene derivative represented by the general formula (1). Further, a light-emitting element that has a long life can be obtained by use of the anthracene derivative represented by the general formula (1).

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13-12-2012 дата публикации

Novel organic compound and organic light-emitting device

Номер: US20120313085A1
Принадлежит: Canon Inc

A novel organic compound suitable for blue light emission and an organic light-emitting device containing the novel organic compound are provided. An organic compound represented by the following general formula (1) wherein R 1 to R 18 independently denote a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group.

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13-12-2012 дата публикации

Method for Producing Curing Agent Having Acidic Substituent and Unsaturated Maleimide Group, Thermosetting Resin Composition, Prepreg, and Laminate

Номер: US20120316263A1
Принадлежит: Individual

A method for producing a curing agent having an acidic substituent and an unsaturated maleimido group, including reacting, in an organic solvent, a maleimide compound (a) having at least two N-substituted maleimido groups in a molecule thereof with an amine compound (b) having an acidic substituent (represented by formula (I) below); a thermosetting resin composition containing the curing agent (A) produced through the method and a compound (B) which is cured with the curing agent, wherein a cured product of the composition has a glass transition temperature of 200° C. or higher; and a prepreg and a laminated sheet produced therefrom. The thermosetting resin composition can produce a prepreg or laminated sheet exhibiting excellent performance suitable for a printed wiring board for electronic devices and similar devices.

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20-12-2012 дата публикации

Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease

Номер: US20120321560A1

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R 1 :-alkylenyl-C(O)NH-alkylenyl-R 3 , -alkylenyl-C(O)O—R 4 , R 3 :—COOH, —OH, —SH, —NH 2 , -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R 4 : H, succinimidyl group, R 2 : —H,-alkyl. In II: R 1 : -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R 2 : -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN) 2 , —HC═CHNO 2 , -alkylenyl-NH 2 , -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

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20-12-2012 дата публикации

Development of Novel Detergents for Use in PCR Systems

Номер: US20120322066A1
Принадлежит: Life Technologies Corp

This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

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20-12-2012 дата публикации

Organosilicon compounds, production processes thereof, pressure-sensitive adhesive compositions containing the organosilicon compounds, self-adhesive polarizers and liquid crystal displays

Номер: US20120322946A1
Автор: Kazuhiro Tsuchida
Принадлежит: Shin Etsu Chemical Co Ltd

Organosilicon compounds are represented by the following formula: wherein R is a hydrolyzable group, R′ is an alkyl having 1 to 4 carbon atoms, A is an alkylene having 1 to 6 carbon atoms, X is O or S, Y is —NH— or S, L 1 and L 2 are C or N, Z and M are —NH—, O or S, R 1 to R 11 are H, alkyl having 1 to 6 carbon atoms, alkoxy or fluoroalkyl, or amino, m is 1 to 3, and n is 0 to 3. R 1 and R 2 or R 2 and R 3 may bonded together. R 5 and R 6 or R 9 and R 10 may directly bond together. R 4 and R 7 or R 8 and R 11 may form a ring skeleton. Their production processes, pressure-sensitive adhesive compositions, self-adhesive polarizers and LCDs are also disclosed.

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27-12-2012 дата публикации

Method of manufacturing epsilon-caprolactam

Номер: US20120330006A1
Автор: Hideto Nagami
Принадлежит: Sumitomo Chemical Co Ltd

An epsilon-caprolactam manufacturing method capable of manufacturing in good yield, high-quality epsilon-caprolactam containing less impurity has an epsilon-caprolactam purification step A of obtaining purified epsilon-caprolactam from raw epsilon-caprolactam by applying a drop crystallization method, a first-stage epsilon-caprolactam recovery step B of obtaining first recovered epsilon-caprolactam and a first recovered mother liquor by applying an evaporative crystallization method to a crystallization mother liquor obtained in the epsilon-caprolactam purification step A, and a second-stage epsilon-caprolactam recovery step C of obtaining second recovered purified epsilon-caprolactam by applying a melt crystallization method to the first recovered mother liquor, first recovered epsilon-caprolactam being recovered as a raw material for the epsilon-caprolactam purification step A and second recovered purified epsilon-caprolactam being recovered as a raw material for the epsilon-caprolactam purification step A and/or the first-stage epsilon-caprolactam recovery step B.

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27-12-2012 дата публикации

Method for preparing polybiotinylated compounds

Номер: US20120330028A1
Автор: Xavier Lacoux
Принадлежит: Individual

The present invention relates to a novel method for preparing compounds having the formula (I), where X is biotin or Y being biotin or Z being biotin or V being biotin or It also relates to compounds having the formula (I) and their use in clinical and industrial diagnosis.

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03-01-2013 дата публикации

Novel compound and process for producing amide compound therewith

Номер: US20130005961A1
Принадлежит: UBE Industries Ltd

The present invention provides novel cyclododecanone-O-azacyclotridecen-2-yloxime and cyclododecanone-O-azacyclotridecen-2-yloxime hydrochloride. The invention also provides a process for producing an amide compound wherein cyclododecanone-O-azacyclotridecen-2-yloxime, hydrogen chloride and/or Lewis acid or cyclododecanone-O-azacyclotridecen-2-yloxime hydrochloride are used as a rearrangement catalyst and/or a reaction starting material in a reaction step.

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07-03-2013 дата публикации

Novel methods for the preparation of p2x7r antagonists

Номер: US20130060047A1
Автор: Michael Bos
Принадлежит: Affectis Pharmaceuticals AG

Disclosed are novel methods for the synthesis of N-substituted indol-3-yl-alkylamide compounds which act as P2X7R antagonists, said methods involving the rearrangement of an oxime intermediate.

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14-03-2013 дата публикации

Method for the Manufacture of an Ammonium Sulfate Composition

Номер: US20130064755A1
Принадлежит:

The present invention describes a method manufacture of an ammonium sulfate composition having a total organic carbon (TOC) content of 1% by weight or less than 1% by weight, based on the total weight of the composition, comprising the following steps: 1. Method for the manufacture of an ammonium sulfate composition comprising the following steps: 'ii) ammonia in an amount sufficient to obtain a pH of 9.5 or higher: and', 'a) reacting i) waste sulfuric acid comprising an organic tertiary amines with'} 'wherein during the separation the pH of the reaction mixture is maintained at a pH of higher than 10.', 'b) separating the organic tertiary amine from the reaction mixture obtained in step a) to form an aqueous solution comprising the ammonium sulfate and an organic tertiary amine stream;'}2. Method according to wherein the organic tertiary amine is separated from the reaction mixture obtained in step a) in a distillation column.3. Method according to wherein during the distillation ammonia is added to the distillation column.4. Method according to wherein during the distillation ammonia is added to the distillation column in a counter flow to the reaction mixture obtained in step a).5. Method according to wherein during the distillation the reaction mixture obtained in step a) is continuously fed to the upper part of a distillation column and the ammonia is continuously fed to the lower part or the middle part of the distillation column.6. Method according to wherein the ammonia feed is placed at a position of the distillation column such that the aqueous solution claim 5 , which is essentially free of organic tertiary amine and which comprises the ammonium sulfate claim 5 , in the lower part of the column has a pH ranging from 5 to 7.7. Method according to wherein the organic tertiary amine is triethylamine.8. Method according to wherein the aqueous solution claim 1 , which is essentially free of the organic tertiary amine and which comprises the ammonium sulfate ...

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14-03-2013 дата публикации

MODULATION OF BIOACTIVE EPOXY-FATTY ACID LEVELS BY PHOSPHODIESTERASE INHIBITORS

Номер: US20130065936A1

The present invention provides method for increasing levels of epoxygenated fatty acids by administration of a phosphodiesterase inhibitor. 1. A method of increasing levels of epoxygenated fatty acids in a subject in need thereof comprising administering to the subject an inhibitor of a phosphodiesterase.2. The method of claim 1 , wherein the ratio of epoxygenated fatty acids to dihydroxy fatty acids is increased without changing the levels of dihydroxy fatty acids.3. The method of claim 1 , wherein soluble epoxide hydrolase is not inhibited.4. The method of claim 1 , wherein the inhibitor of phosphodiesterase is an inhibitor of PDE4.5. The method of claim 4 , wherein the inhibitor of PDE4 is selected from the group consisting of rolipram claim 4 , roflumilast claim 4 , cilomilast claim 4 , ariflo claim 4 , HT0712 claim 4 , ibudilast claim 4 , mesembrine claim 4 , pentoxifylline claim 4 , piclamilast claim 4 , and combinations thereof.6. The method of claim 1 , wherein the inhibitor of phosphodiesterase is an inhibitor of PDE5.7. The method of claim 1 , wherein the inhibitor of phosphodiesterase is administered in a subtherapeutic dose.8. The method of claim 1 , further comprising administration of an inhibitor of soluble epoxide hydrolase.9. The method of claim 8 , wherein the inhibitor of soluble epoxide hydrolase is administered in a subtherapeutic dose.10. The method of claim 1 , wherein the epoxygenated fatty acids are cis-epoxyeicosantrienoic acids (“EETs”) claim 1 , epoxides of linoleic acid claim 1 , epoxides of eicosapentaenoic acid (“EPA”) or epoxides of docosahexaenoic acid (“DHA”) claim 1 , or a mixture thereof.11. A method of obtaining analgesic claim 1 , anti-convulsant claim 1 , anti-depressant claim 1 , anti-inflammatory claim 1 , anti-hypertensive claim 1 , cardioprotective claim 1 , organ protective effects in a subject in need thereof claim 1 , comprising administering to the subject an inhibitor of phosphodiesterase.12. A method of reducing claim ...

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21-03-2013 дата публикации

Methods and Compositions for Treatment of Human Immunodeficiency Virus Infection with Conjugated Antibodies or Antibody Fragments

Номер: US20130071406A1
Принадлежит: Immunomedics Inc

The present invention concerns methods and compositions for treatment of HIV infection in a subject. The compositions may comprise a targeting molecule against an HIV antigen, such as an anti-HIV antibody or antibody fragment. The anti-HIV antibody or fragment may be conjugated to a variety of cytotoxic agents, such as doxorubicin. In a preferred embodiment, the antibody or fragment is P4/D10. Other embodiments may concern methods of imaging, detection or diagnosis of HIV infection in a subject using an anti-HIV antibody or fragment conjugated to a diagnostic agent. In alternative embodiments, a bispecific antibody with at least one binding site for an HIV antigen and at least one binding site for a carrier molecule may be administered, optionally followed by a clearing agent, followed by administration of a carrier molecule conjugated to a therapeutic agent.

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21-03-2013 дата публикации

PESTICIDAL COMPOSITIONS

Номер: US20130072382A1
Принадлежит: DOW AGROSCIENCES LLC

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

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21-03-2013 дата публикации

BICYCLIC TETRAHYDROPYRROLE COMPOUNDS

Номер: US20130072456A1
Принадлежит: LABORATORIOS DEL DR. ESTEVE, S.A.

The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals. 2. The method according to claim 1 , characterized in that Rrepresents a hydrogen atom; an unbranched or branched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted aliphatic radical; a saturated or unsaturated claim 1 , optionally at least mono-substituted claim 1 , optionally at least one heteroatom as ring member containing cyclyl group claim 1 , which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted; a branched or unbranched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another claim 1 , optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another claim 1 , at least mono-substituted mono- or polycyclic ring system; an optionally claim 1 , at least mono-substituted benzhydryl group; a (C═O)—Rgroup; a (C═O)—ORgroup; a (SO)—Rgroup; a (C═O)—NRRgroup;wherein the bond between Y and Z is unsaturated (Y═Z),{'sup': 6', '7', '7a', '8', '9', '10', '10a', '10', '10a, 'sub': 2', '2', '2', '2, 'with Y representing CH and Z representing C—R; C—CHRR; a C—(C═O)—Rgroup; a C—CH(SO)—Rgroup; a C—CH(SO)—NRRgroup; or a C—(C═O)—NRRgroup;'}{'sup': 2', '3', '4', '5', '5a', '6', '7', '7a', '8', '9', '10', '10a, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'R, R, R, R, R, R, R, R, R, R, Rand R, ...

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21-03-2013 дата публикации

2-PHENYL BENZOYLAMIDES

Номер: US20130072519A1
Принадлежит:

Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein. 2. A compound according to wherein Ris —C(O)—N—RRand q is 0.5. A compound according to wherein p is 0 and Ris hydrogen or (C-C)alkyl.6. A compound according to wherein Ris —C(O)—O—(C-C)alkyl.7. A compound according to wherein m and n are each independently 0 or 1 and Rand Rare each independently (C-C)alkyl claim 6 , (C-C)alkoxy or trifluoromethyl.8. The compound:Ethyl (1R)-1-({2-[3-(Dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 1-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate:Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[5-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[6-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxy-5-methylbiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl ...

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21-03-2013 дата публикации

Solid dispersion comprising an anti-hiv agent

Номер: US20130072531A1
Принадлежит: Aicuris GmbH and Co KG

The present invention relates to solid dispersions comprising a compound of formula or a salt, a solvate or a solvate of a salt thereof, dispersed in a polymeric, inert, non-toxic, pharmaceutically acceptable excipient.

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21-03-2013 дата публикации

PHARMACEUTICALLY ACCEPTABLE SALTS OF THYMODEPRESSIN AND PREOCESSES FOR THEIR MANUFACTURE.

Номер: US20130072692A1
Принадлежит: APOTEX TECHNOLOGIES INC.

The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1). 120.-. (canceled)3235.-. (canceled) The present invention relates to novel crystalline and amorphous pharmaceutically acceptable salts of D-isoglutamyl-D-tryptophan. In particular, the present invention relates to D-isog!utamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1) which have improved properties over amorphous D-isoglutamyl-D-tryptophan, crystalline D-isoglutamyl-D-tryptophan and D-isoglutamyl-D-tryptophan disodium salt. The present invention also relates to processes for the manufacture of these novel salts of D-isoglutamyl-D-tryptophan.The compound D-isoglutamyl-D-tryptophan (also known as H-D-iGlu-D-Trp-OH or Thymodepressin) is a synthetic hemoregulatory dipeptide having the following formula:Thymodepressin is the free diacid having Chemical Abstracts Service (CAS) Registry Number® of 186087-26-3. U.S. Pat. No. 5,736,519 discloses H-D-iGlu-D-Trp-OH and a process for its preparation wherein it is purified by ion exchange chromatography. It is an immunosuppressant and selectively inhibits proliferation of hemopoietic precursor cells and stimulates granulocyte and lymphocyte apoptosis (Sapuntsova, S. G., et al. (May 2002), Bulletin of Experimental ...

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28-03-2013 дата публикации

AMINOBENZENE COMPOSITIONS AND RELATED DEVICES AND METHODS

Номер: US20130075670A1
Принадлежит: Plextronics, Inc.

Oligomers and/or polymers comprising a backbone comprising arylamine and fluorinated alkyleneoxy moieties which may be crosslinked. Ink formulations and devices can be formed from the oligomers or polymers, or corresponding monomers. Doped compositions can be formed. Charge injection and transport layers can be formed. Improved stability can be achieved in organic electronic devices such as OLEDs and OPVs. 1. A composition comprising a polymeric or oligomeric backbone comprising at least one repeat moiety comprising at least one O-arylamine , and at least one repeat moiety comprising at least one fluorinated alkyleneoxy.2. The composition of claim 1 , wherein the repeat moiety comprising O-arylamine and the repeat moiety comprising fluorinated alkyleneoxy are alternating moieties.3. The composition of claim 1 , wherein the O-arylamine comprises triarylamine.4. The composition of claim 1 , wherein the O-arylamine moiety comprises at least two nitrogen atoms.5. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a C-Calkylene ether.6. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a fluorinated C-Cvinyl ether.7. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a trifluoroalkyleneoxy moiety.8. The composition of claim 1 , wherein the composition comprises a soluble claim 1 , linear polymer comprising the O-arylamine and the fluorinated alkyleneoxy.9. The composition of claim 1 , wherein the composition is crosslinked.10. An oligomer or polymer comprising repeat units represented by{'br': None, 'sup': '1', '\ue8a0O—Ar\ue8a0 and\u2003\u2003(I)'}{'br': None, 'sup': 1', '2', '2, '\ue8a0O—R—O—Ar—O—R\ue8a0\u2003\u2003(II)'}wherein,{'sup': '1', 'Arcomprises arylamine,'}{'sup': '2', 'Arcomprises an aryl, and'}{'sup': 1', '2, 'sub': 1', '10, 'Rand Rare independently selected from C-Cfluorinated alkylenes.'}11. The oligomer or polymer of claim 10 , wherein the repeat units (I) and (II) are alternating. ...

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28-03-2013 дата публикации

Aromatic Amine Compound, and Light-Emitting Element, Light-Emitting Device, and Electronic Device Using the Aromatic Amine Compound

Номер: US20130076237A1

Novel aromatic amine compounds are provided. Light-emitting elements having high emission efficiency and high reliability are provided. Further, light-emitting devices and electronic devices using the light-emitting devices are provided. Specifically, an aromatic amine compound represented by the general formula (1), and light-emitting elements, light-emitting devices and electronic devices that are formed using the aromatic amine compound represented by the general formula (1) are provided. By using the aromatic amine compound represented by the general formula (1) for light-emitting elements, light-emitting devices and electronic devices, the light-emitting elements, light-emitting devices and electronic devices can have high emission efficiency. 125-. (canceled)28. The aromatic amine compound according to claim 27 ,{'sup': 1', '1, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}30. The aromatic amine compound according to claim 29 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}32. The aromatic amine compound according to claim 31 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}34. The aromatic amine compound according to claim 33 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}37. The light-emitting element according to claim 36 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms ...

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28-03-2013 дата публикации

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

Номер: US20130076604A1
Принадлежит: CANON KABUSHIKI KAISHA

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

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28-03-2013 дата публикации

Novel Isobaric Tandem Mass Tags for Quantitative Proteomics and Peptidomics

Номер: US20130078728A1
Принадлежит:

Compositions and methods of tagging peptides and other molecules using novel isobaric tandem mass tagging reagents, including novel N,N-dimethylated amino acid 8-plex and 16-plex isobaric tandem mass tagging reagents. The tagging reagents comprise: a) a reporter group having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an amine reactive group. The tagging reagents disclosed herein serve as attractive alternatives for isobaric tag for relative and absolute quantitation (iTRAQ) and tandem mass tags (TMTs) due to their synthetic simplicity, labeling efficiency and improved fragmentation efficiency. 2. The method of further comprising identifying one or more fragments of the labeled molecule using mass spectrometry.3. The method of further comprising quantifying amounts of said one or more fragments of the labeled molecule.5. The method of wherein Ris selected from the group consisting of:{'sup': 12', '13, 'a) a methyl group containing one or more deuterium atoms and wherein the carbon is C or C;'}b) hydrogen;c) deuterium;{'sup': '13', 'd) an isopropyl group containing one or more deuterium atoms and one or more C atoms; and'}{'sup': '13', 'e) a butyl group containing one or more deuterium atoms and one or more C atoms.'}6. The method of wherein said molecule is a peptide claim 1 , metabolite or neurotransmitter.7. The method of where labeling the peptide comprises the step of reacting the amine reactive group of the tagging reagent with the N-terminus of the peptide or with an ε-amino group within peptide.8. A method of analyzing a mixture containing target molecules comprising the steps of:a) labeling target molecules within a first sample with a first tagging reagent, thereby generating first labeled target molecules;b) labeling target molecules within at least one additional sample with at least one additional tagging reagent, thereby generating ...

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28-03-2013 дата публикации

ETOMIDATE ANALOGUES THAT DO NOT INHIBIT ADRENOCORTICAL STEROID SYNTHESIS

Номер: US20130079381A1
Принадлежит:

The invention is directed to compounds according to formula (I): where Ris LC(O)OT or LC(O)OLC(O)OT; Ris a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, or R; n is an integer from 0 to 5; each Ris independently halogen or R; Rand Rare independently H, halogen, CN or CF; Land Lare each independently a bond, a substituted or unsubstituted C-Calkylene, C-Calkenylene, or C-Calkynylene; and T is H, a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition. 2. The compound of claim 1 , wherein said compound is present in the form of a pure enantiomer.3. The compound of claim 2 , wherein said enantiomer is the R enantiomer.4. The compound of claim 1 , wherein Ris LC(O)OT.5. The compound of claim 1 , wherein Ris LC(O)OLC(O)OT.6. The compound of claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCHand CHCHCH.7. The compound of claim 1 , wherein T is selected from the group consisting of H claim 1 , CH claim 1 , CHCH claim 1 , CHCH(OH)CH claim 1 , and CHCHCH.8. The compound of claim 1 , wherein n is 0 or 1.9. The compound of claim 1 , wherein Ris CH claim 1 , n is 0 claim 1 , Lis a bond claim 1 , and T is H claim 1 , CH claim 1 , CHCH claim 1 , or CHCH(OH)CH.10. The compound of claim 1 , wherein both Rand Rare H.11. The compound of claim 1 , wherein at least one of Rand Ris H and the other is Br or CN.12. The compound of claim 11 , wherein Ris H and Ris Br or CN.13. The compound of claim 11 , wherein Ris Br or CN and Ris H.15. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of and a pharmaceutically acceptable carrier.16. A method for providing anesthesia to a subject comprising administering to said ...

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28-03-2013 дата публикации

Complexes of Ruthenium, Method of Production Thereof And Use Thereof As (Pre)Catalysts of the Metathesis Reaction

Номер: US20130079515A1
Принадлежит: UMICORE AG & CO. KG

The present invention provides ruthenium complexes of the formula 111-. (canceled)13. The complex of claim 12 , wherein X and X′ are chlorine.14. The complex of claim 12 , wherein Ris hydrogen.15. The complex of claim 12 , wherein A is nitrogen.16. The complex of claim 12 , wherein A is carbon with an Rgroup.17. The method for preparing the ruthenium complex of which comprises reacting 8-ethenylquinoline with a Ru carbene catalyst.19. The method of claim 17 , wherein the Ru carbene catalyst comprises an indenylidene residue claim 17 ,20. The method according to claim 17 , wherein the reaction is conducted in the presence of a copper(I) salt.21. The method according to claim 20 , wherein the copper(I) salt is copper(I) chloride.22. The method according to claim 17 , wherein the reaction is performed in a chlorinated solvent claim 17 , an aliphatic solvent claim 17 , a cycloaliphatic solvent or an aromatic hydrocarbon solvent claim 17 , or mixtures thereof.24. An improved process for ring closing metathesis (RCM) claim 12 , wherein the improvement comprise the use of the ruthenium complex of as an initiator or (pre)catalyst.25. An improved process for ring-opening metathesis polymerization (ROMP) claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst.26. An improved process for metathesis of “alkene-alkyne” (ene-yne) type claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst. This application is a continuation application of U.S. patent application Ser. No. 12/303,615, filed Apr. 3, 2009, which in turn is a national stage application of PCT Application No. EP2007/004901, filed Jun. 1, 2007. The disclosures of the above-referenced applications are hereby incorporated by reference into the present disclosure.The invention relates to novel metal complexes with formula 1, whereCompounds of formula 1 occur as two isomers: with formula 1a, in which atoms X ...

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28-03-2013 дата публикации

Method for Separating off Tryptophan

Номер: US20130079527A1
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a method for separating off tryptophan from aqueous mixtures of matter, in particular fermentation broths that are already partially processed, using simulated countercurrent chromatography or simulated moving bed (SMB) chromatography, and a device for carrying out the method. 117.-. (canceled)18. A method for separating off tryptophan from an aqueous mixture of matter using simulated countercurrent chromatography or SMB chromatography in which , in a separation section having a column arrangement consisting of more than one series-connected columns packed with an organic polymer suitable as adsorbent , which column arrangement is subdivided into a plurality of functional zones ,a) the tryptophan-containing mixture of matter and water as desorbent are continuously fed to the column arrangement at separate points andb) at a point situated between these feeds, the tryptophan-enriched extract stream, and at a further point situated upstream of the feed of tryptophan-containing mixture of matter, a raffinate stream containing further compounds from the mixture of matter used, are taken off separately, the extract stream optionally processed further and optionallyc) the columns that are loaded with non-desorbed compounds from the mixture of matter are cleaned by extraction of said compounds.19. The method as claimed in claim 18 , in which the water is optionally desalted and is fed at a temperature of from 20 to 98° C.20. The method as claimed in claim 18 , in which a mixture of matter is used that contains tryptophan at a concentration from 0.1 to 39 g/l.21. The method as claimed in claim 18 , in which a mixture of matter is used that has a pH from 2.5 to 9.22. The method as claimed in claim 18 , in which a mixture of matter obtained by fermentation is used that claim 18 , in addition to tryptophan claim 18 , also contains phenylalanine and/or tyrosine.23. The method as claimed in claim 22 , in which the mixture of matter used is the mother ...

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28-03-2013 дата публикации

ALKOXYSILANE FUNCTIONALIZED ISOCYANATE BASED MATERIALS

Номер: US20130079538A1
Принадлежит: Huntsman Internatioanl LLC

Alkoxysilane functionalized isocyanate based materials of low viscosity prepared by reacting in any possible order of addition an organic polyisocyanate with an isocyanate-reactive compound and an amino-functional alkoxysilane of formula I 2. The process according to wherein the organic polyisocyanate is pre-reacted with the compound containing isocyanate-reactive hydrogen atoms to form a so-called isocyanate functional prepolymer.3. The process according to wherein the compound containing isocyanate-reactive hydrogen atoms has a functionality of at least 2 and a molecular weight of at least 400.4. The according to wherein the polyisocyanate is reacted with the isocyanate-reactive compound in a molar ratio NCO/OH of at least 2.5. The process according to wherein the molar ratio amine/NCO is from 1 to 100.6. The process according to wherein said polyisocyanate is a difunctional aromatic isocyanate.7. The process according to wherein said polyisocyanate is based on diphenylmethane diisocyanate.8. The process according to wherein R represents an aryl claim 1 , vinyl or carbamate group.9. The process according to wherein R is a phenyl group.10. The process according to wherein Rrepresents a linear alkylene group containing 1 to 4 carbon atoms.11. The process according to wherein both Rand Rrepresent an alkylene group having 1 to 4 carbon atoms.12. The process according to wherein x is 0 or 1.13. The process according to wherein the amino-functional alkoxysilane is gamma-N-phenylaminopropyl trimethoxysilane.14. An alkoxysilane functionalized isocyanate based material obtainable by the process of .15. An alkoxysilane functionalized isocyanate based material according to having a biuret-urea ratio of less than 0.5.16. An alkoxysilane functionalized isocyanate based material according to having a viscosity of at most 200 Pa.s.17. An alkoxysilane functionalized isocyanate based material according to wherein the alkoxysilane functionalized isocyanate based material comprises ...

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04-04-2013 дата публикации

Method for treating varicocele or male infertility using anthocyanin extracted from black soybean

Номер: US20130085114A1

The present invention relates to the therapeutic or ameliorating effects of anthocyanin extracted from black soybean on varicocele or male infertility. In particular, the present invention relates to a method for treating or ameliorating varicocele or male infertility using anthocyanin extracted from black soybean.

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11-04-2013 дата публикации

Biocidal compositions

Номер: US20130090361A1
Автор: Uhr Hermann
Принадлежит: LANXESS DEUTSCHLAND GMBH

The present invention relates to storage-stable biocidal compositions comprising at least one halogen-free isothiazolinone such as in particular 2-methyl-2H-isothiazol-3-one (MIT) and/or 1,2-benzisothiazolin-3-one (BIT) and/or salts thereof, and also stabilizing amounts of copper(II) ions, to a method for preserving technical materials by means of the aforementioned biocidal compositions, and to the technical materials treated therewith. 1. Biocidal compositions comprisingone or more isothiazolinones, where the biocidal compositions, based on their total weight fraction of isothiazolinones, comprise to at least 98.0% those isothiazolinones which are halogen-free and1 to 500 ppm by weight of copper(II) ions, based on the total weight fraction of the isothiazolinone or isothiazolinones in the biocidal composition.2. Biocidal compositions according to claim 1 , characterized in that they comprise two or more isothiazolinones.3. Biocidal compositions according to or claim 1 , characterized in that the isothiazolinones are selected from the group: 2-methyl-2H-isothiazol-3-one; 1 claim 1 ,2-benzisothiazolin-3-one or salts thereof; 2-n-octyl-4-isothiazolin-3-one claim 1 , N-butyl-1 claim 1 ,2-benzisothiazolin-3-one and 2-methyl-4 claim 1 ,5-trimethylene-4-isothiazolin-3-one.4. Biocidal compositions according to one of to claim 1 , characterized in that they comprise claim 1 , as isothiazolinones claim 1 , only 2-methyl-2H-isothiazol-3-one and 1 claim 1 ,2-benzisothiazolin-3-one and/or salts thereof.5. Biocidal compositions according to one of to claim 1 , characterized in that they are liquid.6. Biocidal compositions according to claim 5 , characterized in that they are essentially free from organic solvents.7. Biocidal compositions according to one of to claim 5 , characterized in that they further comprise at least one oxidizing agent which is selected from the group: iodate claim 5 , periodate claim 5 , perchlorate claim 5 , chlorate claim 5 , bromate and organic ...

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11-04-2013 дата публикации

GOLD COMPLEXES FOR USE IN THE TREATMENT OF CANCER

Номер: US20130090472A1
Принадлежит: UNIVERSITY OF KWAZULU-NATAL

The invention provides compounds of the Formula (I), in which W is independently selected from W, W, W, W, W, or W represents a pair of substituents independently selected from H, alkyl, aryl or amide in which the amide is optionally part of a linking chain, and the Z—Zbonds (n=4-17; n′=n+1) are optionally of any whole or partial bond order, Y is Yor Y represents a pair of substituents independently selected from H, C--Calkyl, Zor Zaryl, or Y is optionally a bridging structure that may comprise one or more C--Camide, C--Cether, or C--Cester groups, R-Rare independently selected from no substituent, a lone pair of electrons, H, halogen, C-Caryl, C- C-alkyl, amine, C--Calkylamine, C--Camide, nitro, cyano, carboxyl, C--Cester, phosphane, thiol, C--Cthioether, OR′, and suitable pairs of adjacent R groups (R-R) may optionally together form part of a Cor Caryl ring, a Zor Zring, R′ is independently selected from H, C--Calkyl, Zor Zaryl, C--Cester, poly(—CO—), amine, and C--Calkylamine, Z-Zare independently selected from C, N, P, O, and S, and X is a pharmaceutically acceptable anion, for the treatment of cancer. 2. The compound of claim 1 , in which the anion is selected from halide claim 1 , hexafluorophosphate claim 1 , nitrate claim 1 , and triflate.3. The compound of claim 1 , in which Y represents two hydrogen atoms or Y.4. The compound of claim 3 , in which Y is Yand Zand Zare N.5. The compound of claim 4 , in which Z-Zare C.6. The compound of claim 1 , in which R-Rare selected from H claim 1 , C-Calkyl claim 1 , O—C-Calkyl claim 1 , hydroxyl and halogen.7. The compound of claim 6 , in which C-Calkyl is methyl claim 6 , O—C-Calkyl is O-ethyl claim 6 , and halogen is chlorine.8. The compound of claim 1 , in which W is selected from W claim 1 , W claim 1 , WWor W.9. The compound of claim 8 , in which R-Rare selected from H claim 8 , C-Calkyl claim 8 , O—C-Calkyl and halogen.10. The compound of claim 9 , in which C-Calkyl is methyl claim 9 , O—C-Calkyl is O-ethyl and ...

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11-04-2013 дата публикации

CRYSTALLINE FORMS OF 4, 4'- [4-FLUORO-7-( ETHYNYL)-2-METHYL-1H-INDOLE-1,3-DIYL] DIBUTANOIC ACID, 4,4'-[2-METHYL-7-( ETHYNYL)-1H-INDOLE-1, 3-DIYL] DIBUTANOIC ACID, AND 4,4'-[4-FLUORO-2-METHYL-7- ( ETHYNYL)-1H-INDOLE-1, 3-DIYL] DIBUTANOIC ACID

Номер: US20130090482A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The present invention provides type C crystal of compound I, type B crystal of compound II, or type C crystal of compound III set forth in this specification. 1. A crystal of 4 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 ,3-diyl]dibutanoic acid having at least peaks of about 7.29 , 10.24 , 12.15 , 17.95 , and 18.44 at 2θ degree in powdered X-ray diffraction spectrum.2. The crystal of 4 claim 1 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 1 ,3-diyl]dibutanoic acid according to claim 1 , having peaks of about 6.41 claim 1 , 7.29 claim 1 , 9.22 claim 1 , 10.03 claim 1 , 10.24 claim 1 , 12.15 claim 1 , 12.59 claim 1 , 13.36 claim 1 , 13.88 claim 1 , 14.15 claim 1 , 14.44 claim 1 , 16.60 claim 1 , 17.33 claim 1 , 17.95 claim 1 , 18.44 claim 1 , 18.86 claim 1 , 19.27 claim 1 , 20.23 claim 1 , 21.10 claim 1 , 21.85 claim 1 , 22.26 claim 1 , 23.11 claim 1 , 23.63 claim 1 , and 24.38 at 2θ degree in powdered X-ray diffraction spectrum.3. The crystal of 4 claim 2 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 2 ,3-diyl]dibutanoic acid according to claim 2 , characterized by the chart of powdered X-ray diffraction spectrum shown in .4. A crystal of 4 claim 2 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 2 ,3-diyl]dibutanoic acid having an endothermic peak of about 157° C. in differential scanning calorimetry.5. The crystal of 4 claim 4 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 4 ,3-diyl]dibutanoic acid according to claim 4 , characterized by the chart of differential scanning calorimetry shown in .6. A crystal of 4 claim 4 ,4′-[2-methyl-7-({4-[4-(pentafluorophenyl)butoxy]phenyl}ethynyl)-1H-indole-1 claim 4 ,3-diyl]dibutanoic acid having at least peaks of about 5.12 claim 4 , 10.16 claim 4 , 10.51 claim 4 , 14.90 claim 4 , ...

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11-04-2013 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20130090483A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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18-04-2013 дата публикации

ARYLTHIAZOLYL PIPERIDINES AND RELATED COMPOUNDS AS MODULATORS OF SURVIVAL MOTOR NEURON (SMN) PROTEIN PRODUCTION

Номер: US20130096160A1
Принадлежит:

Aryl substituted thiazol-2-yl-piperidines and related compounds useful as modulators of survival motor neuron (SMN) protein production are provided herein. Without being bound to any particular theory it is believed the aryl substituted thiazol-2-yl-piperidines and related compounds provided herein act to increase production of the SMN2 form of survival motor neuron protein. These compounds are useful for treating spinal muscular atrophy. Pharmaceutical compositions containing a carrier and one or more of the aryl substituted thiazol-2-yl-piperidine or related compounds described herein are also provided. Methods of treating spinal muscular atrophy are also provided by this disclosure. 3. A compound or salt of claim 1 , wherein Ris(i) a 5-membered heteroaryl group containing 1, 2 or 3 heteroatoms chosen from N, O, and S and not more than one O or S heteroatoms:(ii) phenyl, naphthyl, or a 6-membered heteroaryl group containing one or two nitrogen atoms;(iii) a phenyl group fused to a 5, 6, or 7-membered heterocycloalkyl group containing one or two heteroatoms independently chosen from N, O, and S;(iv) a benzofuranyl, indolyl, 9H-fluorenyl, or dibenzo[b,d]thiophenyl group;each of which (i) and (ii) is substituted with 0 to 3 substituents independently chosen from:{'sub': 2', '1', '6', '1', '6', '2', '4', '1', '4', '1', '4', '1', '4', '0', '2', '1', '4', '1', '4', '1', '2', '1', '2, '(a) halogen, hydroxy, amino, cyano, nitro, oxo, —(C═O)NH, C-Calkyl, C-Calkoxy, C-Calkanoyl, C-Calkylthio, C-Calkylsulfonyl, mono- and di-(C-Calkylamino)C-Calkyl, mono- and di-(C-Calkyl)carboxamide, mono- and di-(C-Calkyl)sulfonamide, C-Chaloalkyl, and C-Chaloalkoxy, and'}{'sub': 3', '6', '0', '2', '0', '2', '0', '2', '0', '2', '1', '2', '1', '2, '(b) (C-Ccycloalkyl)C-Calkyl, (heterocycloalkyl)C-Calkyl; (phenyl)C-Calkyl, (phenyl)C-Calkoxy, and thienyl, each of which (b) is substituted with 0 to 2 substituents independently chosen from halogen, C-Calkyl, and C-Calkoxy; and'}{'sub': 1', '2', ...

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18-04-2013 дата публикации

SALALEN LIGANDS AND ORGANOMETALLIC COMPLEXES

Номер: US20130096271A1
Принадлежит: Ramot at Tel-Aviv University Ltd.

Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a Group IV metal and a salalen ligand in the polymerization of alpha-olefins, is disclosed. The alpha-olefin polymers obtained are characterized by controlled levels of tacticity. Also disclosed are novel salalen ligands and novel complexes thereof with Group IV metals. 161-. (canceled)62. A process of polymerizing an alpha-olefin , the process comprising contacting the alpha-olefin with a catalyst system which comprises:(i) a pre-catalyst comprising a Group IV metal atom and a salalen ligand complexed therewith; and(ii) a co-catalyst,thereby producing a polymer of the alpha-olefin.64. The process of claim 62 , wherein said alpha-olefin is propylene.65. The process of claim 62 , wherein said co-catalyst is an aluminoxane.67. The process of claim 63 , wherein R is alkyl.68. The process of claim 63 , wherein at least one of R-Ris an alkyl.69. The process of claim 68 , wherein said alkyl is a bulky alkyl selected from the group consisting of tert-butyl claim 68 , isobutyl claim 68 , isopropyl claim 68 , trityl claim 68 , cumyl and tert-hexyl.70. The process of claim 63 , wherein at least one of R-Ris halogen.71. The process of claim 70 , wherein each of R-Ris halogen.72. The process of claim 70 , wherein at least one of Rand Ris halogen.73. The process of claim 63 , wherein at least one of R-Ris a bulky rigid group.74. The process of claim 73 , wherein at least one of R-Ris selected from the group consisting of aryl claim 73 , heteroaryl claim 73 , cycloalkyl and heteroalicyclic claim 73 , each having at least 7 carbon atoms.75. The process of claim 63 , wherein Ris adamantyl.76. The process of claim 72 , wherein Ris adamantyl.77. A polymer of an alpha-olefin claim 62 , prepared by the process of .78. The polymer of claim 77 , characterized by at least one of:an isotacticity degree of at least 50%;{'sub': 'w', 'a molecular weight of at least M=200,000 grams/mol; and'}a molecular weight ...

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18-04-2013 дата публикации

PROCESSES AND INTERMEDIATES

Номер: US20130096277A1
Автор: Tanoury Gerald J.
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A process for preparing enantioselectively a compound of formula I-1a or I-1b: 2. The process of claim 1 , wherein ring A is Ccycloaliphatic.32. The process of - claims 1 , wherein ring A is cyclopropyl.42. The process of - claims 1 , wherein ring A is cyclopentyl.52. The process of - claims 1 , wherein ring A is 1 claims 1 ,1-dimethylcyclopropyl.9. The process of claim 1 , wherein ring B is a 5-membered heterocyclic ring.11. The process of claim 1 , wherein ring B is substituted with an aryl ring optionally substituted with 0 to 4 groups claim 1 , each independently selected from alkyl claim 1 , halo claim 1 , alkoxy claim 1 , and hydroxyl.12. The process of claim 11 , wherein the aryl ring is phenyl.1514. The process of - claims 1 , wherein Ris H.1614. The process of - claims 1 , wherein Ris Caliphatic.1714. The process of - claims 1 , wherein Ris tert-butyl.2120. The process of - claims 18 , wherein Ris Caliphatic.2220. The process of - claims 18 , wherein Ris a cycloaliphatic.2320. The process of - claims 18 , wherein Ris Caliphatic.2420. The process of - claims 18 , wherein Ris Calkyl.2520. The process of - claims 18 , wherein Ris selected from methyl claims 18 , ethyl claims 18 , n-propyl claims 18 , iso-propyl claims 18 , iso-butyl claims 18 , n-butyl claims 18 , n-pentyl claims 18 , and iso-pentyl.2620. The process of - claims 1 , wherein Ris iso-butyl.2726. The process of - claims 1 , wherein Ris tert-butyl carbamate (Boc).2827. The process of - claims 1 , wherein the carboxylation step includes treating a compound of formula II with carbon dioxide and a lithium base in the presence of an aprotic solvent.29. The process of claim 28 , wherein the aprotic solvent is toluene claim 28 , ethyl acetate claim 28 , benzene claim 28 , and methyl tert-butyl ether.30. The process of claim 28 , wherein the aprotic solvent is methyl tert-butyl ether.31. The process of claim 28 , wherein the lithium base is sec-butyl lithium.3231. The process of - claims 1 , wherein the ...

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18-04-2013 дата публикации

REDUCTION OF ALDEHYDES AND KETONES TO ALCOHOLS

Номер: US20130096317A1
Принадлежит:

The embodiments described herein provide a reduction of an aldehyde or a ketone, such as a Meerwein-Ponnorf-Verley (MPV) reaction of an aldehyde or ketone. In some embodiments, the reaction occurs in the presence of Al[OC(CH)]. In some embodiments, the reaction occurs in the presence of an aprotic solvent. In some embodiments, the aldehyde or ketone is an amino aldehyde or an amino ketone wherein the amine is group is protected such that the nitrogen of the amine has no proton. Other embodiments related to compositions and compounds related to the reduction reaction, or to the preparation or use of the aldehyde, the ketone, or the resulting alcohol. 1. A method of reducing a C═O of an aldehyde or a ketone to a CH—OH of a product alcohol comprising reacting the aldehyde or ketone in the presence of Al[OC(CH)] and a reactant alcohol which comprises a carbon atom directly bonded to both a hydroxyl group and a hydrogen atom2. A method of reducing a C═O of an aldehyde or a ketone to a CH—OH of a product alcohol comprising reacting the aldehyde or ketone in the presence of: Al(OR) , a reactant alcohol comprising a carbon atom directly bonded to both a hydroxyl group and a hydrogen atom , and an aprotic solvent , wherein each Ris independently Calkyl or optionally substituted aryl.3. The method of claim 2 , wherein the aprotic solvent comprises ethyl acetate claim 2 , tetrahydrofuran claim 2 , toluene claim 2 , dichloromethane claim 2 , or an ether.4. The method of claim 2 , wherein the volume ratio of the aprotic solvent to the reactant alcohol is at least about 1:1.7. The method of claim 5 , wherein Ris COR.12. The method of claim 11 , wherein the ratio of diastereomer 1 to diastereomer 2 is at least about 0.5.13. The method of claim 11 , wherein the ratio of diastereomer 1 to diastereomer 2 has a value in the range of about 1 to about 10 claim 11 ,000. 1. Field of the InventionThe embodiments disclosed herein relate to reduction of an aldehyde or ketone, such as by ...

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18-04-2013 дата публикации

MESO-BILIVERDIN COMPOSITIONS AND METHODS

Номер: US20130096318A1
Принадлежит: Utah State University

Methods and materials for producing meso-biliverdin are provided where the methods include reacting phycocyanobilin with an amphoteric compound in a solvent to yield meso-biliverdin. 1. A method of producing meso-biliverdin , the method comprising:reacting phycocyanobilin with an amphoteric compound to yield meso-biliverdin.2. The method of claim 1 , wherein the meso-biliverdin comprises meso-biliverdin IXα.3. The method of claim 1 , wherein the meso-biliverdin consists of meso-biliverdin IXα.4. The method of claim 1 , wherein the amphoteric compound is selected from the group consisting of sodium bicarbonate claim 1 , potassium carbonate claim 1 , and sodium carbonate.5. The method of claim 1 , wherein the amphoteric compound comprises sodium bicarbonate or potassium carbonate.6. The method of claim 1 , wherein the phycocyanobilin is reacted with the amphoteric compound in ethanol or tert-butanol.7. The method of claim 5 , wherein the phycocyanobilin is reacted with the sodium bicarbonate or the potassium carbonate in ethanol.8. The method of claim 1 , wherein the amphoteric compound is present in from 1 to 5 folds in weight compared to the phycocyanobilin by weight.9. The method of claim 1 , wherein the amphoteric compound is present in from 2 to 4 folds in weight compared to the phycocyanobilin by weight.10. The method of claim 1 , the method further comprising culturing cyanobacteria claim 1 , rhodophyte claim 1 , cryptophyte claim 1 , or mixture thereof to yield the phycocyanobilin to be reacted with the amphoteric compound.11. The method of claim 10 , wherein the cyanobacteria claim 10 , rhodophyte claim 10 , cryptophyte claim 10 , or mixture thereof are cultured in a culture media comprising waste water.12. A method of producing meso-biliverdin claim 10 , the method comprising:extracting phycocyanobilin from cyanobacteria, rhodophyte, cryptophyte, or mixture thereof; andisomerizing the extracted phycocyanobilin to form meso-biliverdin.13. The method of claim ...

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18-04-2013 дата публикации

PROCESS FOR PREPARATION OF AMISULPRIDE

Номер: US20130096319A1
Принадлежит: Lupin Limited

The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively. 1) A process for the preparation of amisulpride (I) which involves following steps:{'b': '1', ') methylation of 4-amino-salicylic-acid (VI) to 4-amino-2-methoxy methyl benzoate (VII), optionally in the presence of phase transfer catalyst,'}{'b': '2', ') conversion of 4-amino-2-methoxy methyl benzoate (VII) to 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII),'}{'b': '3', ') ethylation of 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII) to form 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X),'}the intermediate compound (X) is converted to amisulpiride (I) by two routes (a) or (b):Route (a):{'b': '4', 'i': 'a', ') hydrolysis of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX),'}{'b': '4', 'i': 'b', ') oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) with a suitable oxidizing agent in presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV),'}Route (b):{'b': '5', 'i': 'a', ') oxidation of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) with a suitable oxidizing agent,'}{'b': '5', 'i': 'b', ') hydrolysis of 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid,(IV and;'}{'b': '6', ') coupling of 2-methoxy-4-amino-5-ethyl-sulfonyl ...

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25-04-2013 дата публикации

ORGANIC PHOTOELECTRIC CONVERSION ELEMENT AND SOLAR CELL USING SAME

Номер: US20130098449A1
Автор: Okubo Yasushi, TANI Kunio
Принадлежит: KONICA MINOLTA HOLDINGS, INC.

Disclosed is an organic photoelectric conversion element which has a reverse layer structure wherein at least a first electrode, a photoelectric conversion layer and a second electrode are arranged on a substrate in this order. The organic photoelectric conversion element is characterized in that: the photoelectric conversion layer is a bulk heterojunction layer that is composed of a p-type organic semiconductor material and an n-type organic semiconductor material; and a compound that has a linear or branched fluorinated alkyl group having 6-20 carbon atoms is contained as the p-type organic semiconductor material. 1. An organic photoelectric conversion element having a reverse layer structure comprising a substrate having thereon at least a first electrode , a photoelectric conversion layer and a second electrode in this order , whereinthe photoelectric conversion layer is a bulk heterojunction layer comprising a p-type organic semiconductor material and an n-type organic semiconductor material, andthe p-type organic semiconductor material comprises a compound that has a linear or branched fluorinated alkyl group having 6 to 20 carbon atoms.2. The organic photoelectric conversion element of claim 1 , wherein the fluorinated alkyl group has 8 to 20 carbon atoms.4. The organic photoelectric conversion element of claim 3 , wherein Formula (1) meets 3≧m+n≧2.5. The organic photoelectric conversion element of claim 3 , wherein Formula (1) meets m≧1 and n≧1.7. The organic photoelectric conversion element of claim 6 , wherein claim 6 , in Formula (2) claim 6 , L represents a carbonyl group claim 6 , an ester group or an amide group.8. The organic photoelectric conversion element of wherein claim 6 , in Formula (2) claim 6 , L represents an ester group.9. The organic photoelectric conversion element of claim 1 , wherein at least one fluorinated alkyl group has 7 to 17 fluorine atoms.10. The organic photoelectric conversion element of claim 1 , wherein the compound having ...

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25-04-2013 дата публикации

BIPOLAR COMPOUND AS A HOST MATERIAL FOR ORGANIC LIGHT EMITTING DIODES

Номер: US20130099207A1

The present invention provides a bipolar compound represented by formula (I) and the derivatives thereof as a host material having excellent bipolar transporting properties for organic light-emitting diodes (OLEDs). The present invention also relates to a device including at least a layer of the bipolar compound and/or the derivatives thereof as a host material and a method of making the same. 2. The bipolar compound of claim 1 , wherein said substituted or unsubstituted alkyl group is Calkyl selected from one or more of a methyl group claim 1 , an ethyl group claim 1 , an n-propyl group claim 1 , an n-butyl group claim 1 , an n-pentyl group claim 1 , an n-hexyl group claim 1 , an n-heptyl group claim 1 , an n-octyl group claim 1 , an n-decyl group claim 1 , an iso-propyl group claim 1 , an iso-butyl group claim 1 , a sec-butyl group claim 1 , a tert-butyl group claim 1 , an iso-pentyl group claim 1 , a neopentyl group claim 1 , a tert-octyl group claim 1 , a fluoromethyl group claim 1 , a difluoromethyl group claim 1 , a trifluoromethyl group claim 1 , a 2-fluoroethyl group claim 1 , a 2 claim 1 ,2 claim 1 ,2-trifluoroethyl group claim 1 , a perfluoroethyl group claim 1 , a 3-fluoropropyl group claim 1 , a perfluoropropyl group claim 1 , a 4-fluorobutyl group claim 1 , a perfluorobutyl group claim 1 , a 5-fluoropentyl group claim 1 , a 6-fluorohexyl group claim 1 , a chloromethyl group claim 1 , a trichloromethyl group claim 1 , a 2-chloroethyl group claim 1 , a 2 claim 1 ,2 claim 1 ,2-trichloroethyl group claim 1 , a 4-chlorobutyl group claim 1 , a 5-chloropentyl group claim 1 , a 6-chlorohexyl group claim 1 , a bromomethyl group claim 1 , a 2-bromoethyl group claim 1 , an iodomethyl group claim 1 , a 2-iodoethyl group claim 1 , a hydroxymethyl group claim 1 , a hydroxyethyl group claim 1 , a cyclopropyl group claim 1 , a cyclobutyl group claim 1 , a cyclopentyl group claim 1 , a cyclohexyl group claim 1 , a cyclopentylmethyl group claim 1 , a cyclohexylmethyl ...

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25-04-2013 дата публикации

Method of manufacturing display apparatus

Номер: US20130100386A1
Принадлежит: SAMSUNG ELECTRONICS CO LTD

In a method of manufacturing a display apparatus, a first substrate including a plurality of pixels is formed, and a black column spacer is formed on the first substrate. A second substrate is formed, and a liquid crystal layer is formed between the first substrate and the second substrate. The black column spacer is formed by coating a photoresist on the first substrate, exposing the photoresist to a first light, developing the exposed photoresist and exposing the developed photoresist to a second light.

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25-04-2013 дата публикации

Treatment Methods Using Disinfecting Compositions Containing a Polymer Complex of Organic Acid

Номер: US20130101526A1
Принадлежит: Reckitt Benckiser LLC.

The present invention provides compositions which not only effectively kill a broad spectrum of microorganisms present on surfaces on contact but continue to kill microorganisms for a period of time thereafter. 1. A composition which provides an antimicrobial benefit to a surface selected from: a hard inanimate surface , a textile , a fabric , and skin , which composition comprises:(a) at least one organic acid;(b) optionally, at least one anionic surfactant;{'sup': 1', '2', '3', '1', '2', '4', '1', '2', '3', '4', '1', '2', '3, 'sub': 1-6', '1-6', '1-6', '1-6', '1-6', '1-6, '(c) at least one polymer capable of forming a complex with (a) at least one of organic acid; wherein said polymer is a copolymer of Monomer A and Monomer B wherein Monomer A is of the formula R—CH═CH—Rand wherein Monomer B is of the formula R—C(R)═C(R)—R, wherein Rand Rare independently selected from hydrogen; hydroxy; halogen; carboxy; sulfo; phenyl; phenoxy; Calkyl, Calkoxy, Caminoalkyl, Chaloalkyl wherein the halogen is selected from chlorine, bromine, iodine, and fluorine; Calkylphenyl; amino and Calkylamino, Ris an acidic group or a derivative thereof and Ris a group selected from any of the definitions given hereinbefore for R, Ror R, with the proviso that neither monomer A nor monomer B is an ester having a quaternary ammonium compound;'}(d) optionally, at least one organic solvent;(e) optionally, at least one propellant;(f) water; andoptionally, one or more further conventional constituents such as: pH buffering agents, perfumes, perfume carriers, colorants, hydrotropes, viscosity modifying agents, further germicides, fungicides, anti-oxidants, and anti-corrosion agents.2. The composition according to wherein the at least one organic acid is selected from a compound having the formula:{'br': None, 'R—COOH'}wherein R is hydrogen, lower alkyl; substituted lower alkyl; hydroxy lower alkyl; carboxy lower alkyl; carboxy, hydroxy lower alkyl; carboxy, halo lower alkyl; carboxy, dihydroxy lower ...

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25-04-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130102585A1
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 118.-. (canceled)20. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 19 , a pharmaceutically acceptable excipient and a pharmaceutically acceptable diluent.21. A pharmaceutical composition of claim 20 , wherein the composition is a solid oral dosage form.22. A pharmaceutical composition of claim 20 , wherein the composition is a syrup claim 20 , an elixir or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.Cannabis sativa has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from Cannabis sativa and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased ...

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25-04-2013 дата публикации

TARGETED NITROXIDE AGENTS

Номер: US20130102626A1
Принадлежит:

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. 45-. (canceled)6. The compound of claim 1 , in which R is Ac claim 1 , Boc claim 1 , Cbz claim 1 , or —P(O)-Ph.7. The compound of claim 1 , in which R claim 1 , R claim 1 , Rand Rare independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.8. The compound of claim 1 , wherein when X is —CH═CR— claim 1 , Ris hydrogen claim 1 , methyl or ethyl.912-. (canceled)13. The compound of in which R1 claim 1 , R2 and R3 independently are methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.1421-. (canceled)27. A method of making a targeted antioxidant compound claim 1 , comprising:{'sub': 1', '1', '1', '6', '6', '5, 'a. reacting an aldehyde of structure R—C(O)— with (R)-2-methylpropane-2-sulfinamide to form an imine, in which Ris C-Cstraight or branched-chain alkyl, optionally including a phenyl (CH) group, that optionally is methyl-, hydroxyl- or fluoro-substituted;'}{'sub': 2', '2', '2, 'b. reacting a terminal alkyne-1-ol (HCC—R—CH—OH), in which Ris not present or is branched or straight-chained alkylene, with a tert-butyl)diphenylsilane salt to produce an alkyne;'}c. ...

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25-04-2013 дата публикации

Inhibitors of protein prenyltransferases

Номер: US20130102639A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.

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25-04-2013 дата публикации

MICROBICIDAL COMPOSITION

Номер: US20130102646A1
Принадлежит: ISP Investment Inc.

The invention relates to a microbicidal composition which comprises a mixture of at least two components, the first component being 2-methyl-3-isothiazolone (MIT) and the second component being at least one active compound selected from the following groups of active compounds: 1. Microbicidal composition which comprises a mixture of at least two components , the first component being 2-methyl-3-isothiazolone and the second component being at least one active compound selected from the following groups of active compounds:a) compounds having activated methylol groupsb) quats or polyquatsc) carbamatesd) organic acidse) aromatic alcohols.2. Composition according to claim 1 , characterized in that the composition comprises one or more different solvents.3. Composition according to one or both of the preceding claims claim 1 , characterized in that water claim 1 , glycols and/or glycol ethers are provided as solvent.4. Composition according to one or more of the preceding claims claim 1 , characterized by a synergistic action of the components present in the mixture.5. Composition according to one or more of the preceding claims claim 1 , characterized by an activity enhancement by the solvent claim 1 , in particular the glycols and/or glycol ethers.6. Composition according to one or more of the preceding claims claim 1 , characterized in that bronopol claim 1 , diazolidinylurea or imidazolidinylurea are provided as compounds having activated methylol groups.7. Composition according to one or more of the preceding claims claim 1 , characterized in that polyaminopropyl biguanide claim 1 , cetrimonium bromide or benzalconium chloride are provided as quats or polyquats.8. Composition according to one or more of the preceding claims claim 1 , characterized in that iodopropynyl butylcarbamate or dithiocarbamate are provided as carbamates.9. Composition according to one or more of the preceding claims claim 1 , characterized in that dehydroacetic acid claim 1 , undecylenic ...

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25-04-2013 дата публикации

SUBSTITUTED BIARYL ALKYL AMIDES

Номер: US20130102649A1
Принадлежит: BioTheryX, Inc.

Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds. 2. The compound of claim 1 , wherein n is selected from the group consisting of 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , and 5.3. The compound of claim 2 , wherein n is 2.4. The compound of claim 1 , wherein each Ris halo.5. The compound of claim 4 , wherein each Ris chloro.6. The compound of claim 1 , wherein Z claim 1 , Z claim 1 , Zand Zare each —CH—.7. The compound of claim 1 , wherein Ris (Calkoxy)Calkyl.8. The compound of claim 7 , wherein Ris methoxymethyl or ethoxymethyl.9. The compound of claim 1 , wherein Ris (aryloxy)Calkyl.10. The compound of claim 9 , wherein Ris phenoxymethyl.11. The compound of claim 1 , wherein Ris Cheterocyclyl.12. The compound of claim 11 , wherein Ris selected from optionally substituted tetrahydrofuranyl or optionally substituted pyrrolidinyl.13. The compound of claim 12 , wherein the nitrogen atom in pyrrolidinyl is protected with a t-butyloxycarbonyl (Boc) protecting group.14. The compound of claim 1 , wherein Ris Ccycloalkyl.15. The compound of claim 14 , wherein Ris cyclopentyl.16. The compound of claim 1 , wherein Ris haloalkyl.17. The compound of claim 16 , wherein Ris selected from the group consisting of —CHCl claim 16 , —CHBr claim 16 , —CHCHCl claim 16 , —CHCHBr claim 16 , —CH(Cl)CHand —CH(Br)CH.18. The compound of claim 1 , wherein Ris optionally substituted aminoalkyl.19. The compound of claim 18 , wherein Ris selected from the group consisting of —CHNH claim 18 , —CHNH(Boc) claim 18 , —CH(NH)CH claim 18 , and —CH(Boc-NH)CH.20. The compound of claim 1 , wherein Ris —OH.22. The compound of claim 21 , wherein Ris —OH.23. The compound of claim 1 , wherein Ris selected from the group consisting of —OH claim 1 , —NHR claim 1 , an optionally substituted Calkoxy claim 1 , and an optionally ...

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25-04-2013 дата публикации

NOVEL CURING AGENTS

Номер: US20130102756A1
Автор: Cawse John
Принадлежит: Hexcel Composites Limited

A curable resin comprising a compound having the structure (I): wherein each carbon 2, together with either its carbon 1 or carbon 3, arc members of a fused cycloaliphatic ring, and when carbon 1 is a member of the ring so is N, and wherein each of the aliphatic or aromatic ring-member carbons may either be members of further fused cycloaliphatic rings or be bonded to a group selected from H or linear or branched Cto Calkyl. 2. A curable resin according to claim 1 , wherein any carbons forming part of any further fused cycloaliphatic rings are also bonded to either an H or linear or branched Cto Calkyl.3. A curable resin according to claim 1 , wherein each of the aliphatic or aromatic ring-member carbons claim 1 , which are not members of a fused cycloaliphatic ring claim 1 , are bonded to an H or linear or branched Cto Calkyl.4. A curable resin according to claim 1 , wherein the compound has a molecular weight of no greater than 600.5. A curable resin according to claim 1 , wherein the fused cycloaliphatic rings comprise five or six carbons.8. A curable resin according to claim 1 , wherein carbon 2 is a member of two fused cycloaliphatic rings claim 1 , one with carbon 1 and the other with carbon 3.9. A curable resin according to claim 1 , having a melting point of from 80° C. to 200° C.10. A curable resin according to claim 1 , wherein the resin is an epoxy or urethane.11. A curable resin according to claim 1 , comprising a fibre reinforcement.12. A curable resin according to claim 11 , which is a prepreg claim 11 ,13. A cured resin made by exposing a curable resin according to to elevated temperature.14. A cured resin according to claim 13 , which has a glass transition temperature of greater than 100° C.15. A cured resin according to which forms part of a structural member of an aerospace structure. The present invention relates to novel resin curing agents, particularly for epoxy and urethane resins.Curable resin systems are widely known and have a wide range ...

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25-04-2013 дата публикации

Substituted Tetracycline Compounds

Номер: US20130102779A1
Автор: Abato Paul
Принадлежит: PARATEK PHARMACEUTICALS, INC.

The present invention pertains to tetracycline compounds of formula (VIIa): 2. The tetracycline compound of claim 1 , wherein Ris oxazolyl.3. The tetracycline compound of claim 2 , wherein oxazolyl is substituted with methyl or isopropyl.4. The tetracycline compound of claim 1 , wherein Ris oxadiazolyl.5. The tetracycline compound of claim 4 , wherein oxadiazolyl is substituted with alkyl.6. The tetracycline compound of claim 1 , wherein Ris isoxazolyl.7. The tetracycline compound of claim 1 , wherein Ris pyrazolyl.8. The tetracycline compound of claim 7 , wherein Ris methylpyrazolyl.9. The tetracycline compound of claim 1 , wherein Ris —CONRR claim 1 , in which Ris hydrogen and Ris hydroxyl claim 1 , hydroyxalkyl claim 1 , alkoxy claim 1 , phenyl claim 1 , or alkyl.10. The tetracycline compound of claim 1 , wherein Ris wherein Ris —CONRR claim 1 , in which Ris alkyl and Ris alkyl or hydroxyl.11. The tetracycline compound of claim 1 , wherein Ris dialkylamino.12. The tetracycline compound of claim 11 , wherein Ris dimethylamino.13. The tetracycline compound of claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , and R is hydrogen.14. The tetracycline compound of claim 13 , wherein Ris dialkylamino.15. The tetracycline compound of claim 14 , wherein Ris dimethylamino.19. A pharmaceutical composition comprising a tetracycline compound of and a pharmaceutically acceptable carrier.20. A method for treating a tetracycline responsive state in a subject claim 1 , comprising administering to said subject an effective amount of a tetracycline compound of claim 1 , such that said subject is treated. This application is a divisional application of U.S. Ser. No. 11/963,540, filed on Dec. 21, 2007 and issued as U.S. Pat. No. 8,318,706 on Nov. 27, 2012, which claims priority to U.S. Provisional Patent Application No. 60/876,313, filed on Dec. 21, 2006 and U.S. Provisional Patent Application No. 60/943,003, filed Jun. 8, 2007. The contents of the foregoing applications ...

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25-04-2013 дата публикации

SYNTHETIC PROCESS FOR AMINOCYCLOHEXYL ETHER COMPOUNDS

Номер: US20130102791A1
Принадлежит: CARDIOME PHARMA CORP.

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed. 15.-. (canceled)7. The method of further comprising optionally protecting the compound of formula (4) and/or the compound of formula (6) before the reaction of compound of formula (4) with the compound of formula (6) and optionally deprotecting the compound of formula (8) after the reaction.9. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.12. The method of further comprising optionally protecting the compound of formula (71) and/or the compound of formula (6) before the reaction of compound of formula (71) with the compound of formula (6) and optionally deprotecting the compound of formula (73) after the reaction.14. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.17. The method of further comprising optionally protecting the compound of formula (72) and/or the compound of formula (6) before the reaction of compound of formula (72) with the compound of formula (6) and optionally deprotecting the compound of formula (74) after the reaction.19. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.2120. The method of any one of claim 16 , claim 16 , and claim 16 , wherein the separation step comprises crystallization claim 16 , kinetic resolution claim 16 , chemical separation claim 16 , enzymatic resolution claim 16 , and/or chromatographic resolution.22. The method of wherein said optional functionalization step comprises formation of acid addition salts of the mixture of the compound of formula (4a) and the compound of formula (5a) or the ...

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02-05-2013 дата публикации

LIGHT EMITTING ELEMENT

Номер: US20130105787A1
Принадлежит: Toray Industries, Inc.

Provided is an organic thin film light emitting element which has achieved all of improved luminous efficiency, improved driving voltage and improved durability life. Specifically provided is a light emitting element which comprises a hole transport layer and an electron transport layer between a positive electrode and a negative electrode and emits light by means of electrical energy. The light emitting element is characterized in that: the hole transport layer of the light emitting element contains a compound represented by general formula (1); the electron transport layer contains a donor compound; and the donor compound is an alkali metal, an inorganic salt containing an alkali metal, a complex of an alkali metal and an organic substance, an alkaline earth metal, an inorganic salt containing an alkaline earth metal, or a complex of an alkaline earth metal and an organic substance. (In the formula, R-Reach represents one group selected from the group consisting of hydrogen, deuterium, an alkyl group, a cycloalkyl group, an amino group, an aryl group, a heterocyclic group, a heteroaryl group, an alkenyl group, a cycloalkenyl group, an alkynyl group, analkoxy group, an alkylthio group, an arylether group, an arylthioether group, a halogen, a cyano group, a —P(═O)RRgroup and a silyl group; Rand Reach represents an aryl group or a heteroaryl group; and these substituents may be further substituted, or adjacent two substituents may combine together to form a ring. Meanwhile, R-Rmay be the same or different and each represents one group selected from the group consisting of an alkyl group, a cycloalkyl group, an aryl group and a heteroaryl group; and these substituents maybe further substituted.) 2. A light-emitting element claim 1 , according to claim 1 , wherein a hole injection layer exists between the hole transport layer and the anode and consists of an acceptor compound alone or contains an acceptor compound3. A light-emitting element claim 2 , according to claim ...

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02-05-2013 дата публикации

FAAH Inhibitors

Номер: US20130109721A1
Принадлежит: Ironwood Pharmaceuticals, Inc.

The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is an optionally substituted ring selected from the group consisting of phenyl claim 1 , pyridine claim 1 , pyrimidine claim 1 , pyrazine claim 1 , pyridazine claim 1 , pyrrole claim 1 , imidazole claim 1 , pyrazole claim 1 , furan claim 1 , thiophene claim 1 , triazole claim 1 , tetrazole claim 1 , thiazole claim 1 , oxathiazole and oxazole.3. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein ring B is an optionally substituted pyridine or an optionally substituted phenyl.45.-. (canceled)6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is selected from the group consisting of 0 and 1.7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Jis independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , cyclopropyl claim 1 , cyclopropyloxy claim 1 , Chaloalkyl claim 1 , Calkoxy and Chaloalkoxy.8. The compound according to claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein each Jis independently selected from the group consisting of halogen claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , isopropyl claim 7 , trifluoromethyl claim 7 , methoxy claim 7 , trifluoromethoxy claim 7 , ethoxy claim 7 , propyloxy and isopropyloxy.10. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein p is selected from the group consisting of 0 claim 1 , 1 and 2.11. The compound ...

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02-05-2013 дата публикации

Biocide

Номер: US20130109727A1
Автор: Carsten Berg
Принадлежит: Titan Chemicals Ltd

Aqueous solutions of the tetramethylammonium salt of 1,2-benzothiazolone stable below 0° C.

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02-05-2013 дата публикации

GPR120 RECEPTOR AGONISTS AND USES THEREOF

Номер: US20130109734A1
Принадлежит: Metabolex, Inc.

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. 125.-. (canceled)26. A compound selected from the group consisting of:3-(4-((5-fluoro-1-(methoxycarbonyl)-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid;3-(4-((5-fluoro-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid; and3-(4-((5-fluoro-1,2,2-trimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid,or a pharmaceutically acceptable salt thereof.27. A composition comprising a compound of and a pharmaceutically acceptable carrier.28. A method of treating a disease or condition selected from the group consisting of Type I diabetes claim 26 , Type II diabetes and metabolic syndrome claim 26 , said method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of .29. The method of claim 28 , wherein said disease is Type II diabetes.30. A method of lowering blood glucose in a mammal claim 26 , said method comprising administering a therapeutically effective amount of a compound of to a mammal in need of such treatment.31. The method of claim 30 , wherein said mammal is a human. Diabetes mellitus can be divided into two clinical syndromes, Type I and Type II diabetes mellitus. Type I diabetes, or insulin-dependent diabetes mellitus, is a chronic autoimmune disease characterized by the extensive loss of beta cells in the pancreatic islets of Langerhans (hereinafter referred to as “pancreatic islet cells” or “islet cells”), which produce insulin. As these cells are progressively destroyed, the amount of secreted insulin decreases, eventually leading to hyperglycemia (abnormally high level of glucose in the blood) when the amount secreted drops below the level required for euglycemia (normal blood glucose level). Although the exact trigger for this immune response is not known, patients with Type I ...

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02-05-2013 дата публикации

SALACINOL AND PONKORANOL HOMOLOGUES, DERIVATIVES THEREOF, AND METHODS OF SYNTHESIZING SAME

Номер: US20130109735A1
Принадлежит: SIMON FRASER UNIVERSITY

Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from 5. (canceled)8. (canceled)9. (canceled)13. A method of using a compound as defined in as a glycosidase inhibitor claim 1 , comprising administering said compound to a patient.14. A method for treating diabetes in an affected patient comprising the step of administering to the patient a therapeutically effective amount of a compound as defined in .15. (canceled)16. (canceled) This application claims priority to, and the benefit under 35 U.S.C. §119 of, U.S. provisional patent application No. 61/265,695 filed 1 Dec. 2009 and entitled SALACINOL HOMOLOGUES, DERIVATIVES THEREOF AND METHODS OF SYNTHESIZING SAME, the entirety of which is hereby incorporated by reference.This application relates to salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using same.Glycosidases are enzymes that are involved in the catabolism of glycoproteins and glycoconjugates and the biosynthesis of oligosaccharides. Disruption in regulation of glycosidases can lead to diseases.Over the years, glycosidase inhibitors have received considerable attention in the field of chemical and medicinal researchbecause of their effects on quality control, maturation, transport, secretion of glycoproteins, and cell-cell or cell-virus recognition processes. This principle has potential for many therapeutic applications, such as in the treatment of diabetes, cancer and other viral infections.Bioactive components isolated from medicinal plants that are used in traditional medicine or folk medicine often provide the lead structures for modern drug-discovery programs. For example, ...

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02-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF PYRROLINES FROM GAMMA-NITROKETONES. USE OF THE GAMMA-NITROKETONES AS PESTICIDAL AGENTS

Номер: US20130109757A1
Принадлежит: Bayer Intellectual Property GmbH

The invention is directed to method for the preparation of pyrrolines of the general formula (I) 2. The method according to claim 1 , wherein said elevated pressure is in a range from 2 to 100 bar.3. The method according to claim 1 , wherein the transitionmetal catalyst used comprises at least one metal selected from the group consisting of platinum, palladium, cobalt and nickel.4. The method according to claim 3 , wherein Raney-Nickel is used as transition metal catalyst in the presence of an organic sulfur-containing compound.5. The method according to claim 4 , wherein said organic sulfur-containing compound is selected from the group consisting of thiophene claim 4 , tetrahydrothiophene and 2 claim 4 ,2′-thiobisethanol.9. The nitroketone compound of formula (II) according to claim 6 , capable of being used for combating harmful invertebrate pests which occur in the agriculture or which occur in a veterinary field.10. A method for combating one or more harmful invertebrate pests which occur in the agriculture or which occur in a veterinary field comprising using a compound of to combat said pests. The present invention relates to a method (process) for the synthesis of substituted pyrrolines as well as to specific γ-nitroketones which can be used as starting materials in the process according to the invention. Pyrrolines are biological active and can thus be used as pesticides (cf. WO 2009/097992, WO 2009/112275).Several methods for the manufacturing of pyrrolines are known (cf. Cheruku, Srinivasa et al. 44 (2003), 3701-3703 and Moffett and White, J. Org. Chem. 17 (1952) 407-413)). One method is the reductive cyclization of γ-nitroketones using zinc powder together with HCOH-EtOH (1:1) which results in pyrroline N-oxides and pyrrolines (cf. Cheruku, Srinivasa et al. 44 (2003), 3701-3703).The reductive cyclization of a bromine-substituted pyrrole-γ-nitroketone is described by Laha, K. Joydev et al. in 2006, 71, pp. 4092-4102 (therein named as compound 8) using ...

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02-05-2013 дата публикации

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

Номер: US20130109866A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:a is 1 and b is 0.3. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': 5', '14, 'sub': 'n', 'Ris —S(O)R.'}4. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'sub': '3', 'Ris —CF.'}5) A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'Ris halogen.'}6. A compound according to claim 1 , wherein:a is 1 and b is 0;{'sup': 1', '11', '12', '13, 'sub': '1-8', 'Ris optionally substituted Calkyl, —NRRor —OR;'}{'sup': '2', 'sub': '1-8', 'Ris optionally substituted Calkyl;'}{'sup': 3', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 4', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 5', '14, 'sub': 3', 'n, 'Ris halogen, —CFor —S(O)R;'}n is 0, 1 or 2;{'sup': 6', '15', '13', '11', '−12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 7', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': '8', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '6-10, 'Ris hydrogen, optionally substituted Calkyl or optionally substituted Caryl;'}{'sup': '10', 'sub': '1-8', 'Ris hydrogen or optionally substituted C;'}{'sup': '11', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '12', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '13', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '14', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl; ...

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09-05-2013 дата публикации

COMPOUND HAVING CARBAZOLE RING STRUCTURE, AND ORGANIC ELECTROLUMINESCENT DEVICE

Номер: US20130112950A1
Принадлежит: HODOGAYA CHEMICAL CO., LTD.

There is provided an organic compound of excellent characteristics that exhibits excellent hole-injecting/transporting performance and has high triplet exciton confining capability with an electron blocking ability, and that has high stability in the thin-film state and high luminous efficiency. The compound is used to provide a high-efficiency, high-durability organic electroluminescent device, particularly a phosphorescent organic electroluminescent device. The present invention is a compound of the following general formula having a carbazole ring structure. The compound is used as a constituent material of at least one organic layer in an organic electroluminescent device that includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes. 3. (canceled)4. (canceled)6. An organic electroluminescent device that comprises a pair of electrodes , and one or more organic layers sandwiched between the pair of electrodes ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the compound having a carbazole ring structure of is used as a constituent material of at least one organic layer.'}7. The organic electroluminescent device according to claim 6 , wherein the organic layer is a hole transport layer.8. The organic electroluminescent device according to claim 6 , wherein the organic layer is a hole injection layer.9. The organic electroluminescent device according to claim 6 , wherein the organic layer is an electron blocking layer.10. The organic electroluminescent device according to claim 6 , further comprising a light emitting layer that contains a phosphorescent light-emitting material.11. The organic electroluminescent device according to claim 10 , wherein the phosphorescent light-emitting material is a metal complex that contains iridium or platinum.12. An organic electroluminescent device that comprises a pair of electrodes claim 10 , and one or more organic layers sandwiched between the pair of electrodes claim ...

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09-05-2013 дата публикации

Saccharide Siloxanes Stable In Aqueous Environments And Methods For The Preparation And Use Of Such Saccharide Siloxanes

Номер: US20130115184A1
Принадлежит: Dow Corning Corporation

A novel saccharide siloxane copolymer has improved stability in the presence of water as compared to certain previously known saccharide siloxanes. The saccharide siloxane copolymer is useful in personal care compositions. 1. A saccharide siloxane copolymer of formula:{'br': None, 'sup': 2', '1', '2', '1', '1', '1', '2, 'sub': a', '(3-a)', 'm', '2', 'n', 'y', '(3-a)', 'a, 'RRSiO—[(SiRRO)—(SiRO)]—SiRR; where'}{'sup': 1', '1', '3, 'claim-text': 'Q comprises an epoxy, cycloalkylepoxy, primary or secondary amino, ethylenediamine, carboxy, halogen, vinyl, allyl, anhydride, or mercapto functionality;', 'each Rcan be the same or different and each Rcomprises hydrogen, an alkyl group, an organic group, or a group of formula R-Q;'}subscripts m and n are integers from 0 to 10,000 and may be the same or different;each subscript a is independently 0, 1, 2, or 3;subscript y is an integer such that the copolymer has a molecular weight less than 1 million;{'sup': 2', '1', '2', '2, 'sub': b', 'c, 'claim-text': [{'sup': '1', 'Gis a saccharide component comprising 5 to 12 carbon atoms,'}, 'a quantity (b+c) has a value ranging from 1 to 10, and', 'subscript b or subscript c can be 0,', {'sup': '2', 'Gis a saccharide component comprising 5 to 12 carbon atoms additionally substituted with organic or organosilicon radicals,'}, {'sup': 3', '8', '4', '3', '8', '4', '3', '4', '8, 'sub': 2', '2, 'claim-text': [{'sup': 3', '4', '5', '6', '7, 'sub': r', 's', 't, 'claim-text': where at least one of subscripts r, s and t is 1, and', {'sup': 5', '7', '9, 'sub': 'p', 'each Rand each Rare independently either an alkylene group of 1 to 12 carbon atoms or a group of formula (RO), where'}, 'subscript p is an integer with a value ranging from 1 to 50, and', {'sup': '9', 'each Ris a divalent organic group, and'}, {'sup': '90', 'each Rmay be the same or different,'}, {'sup': 6', '8', '8', '3, 'each Ris —N(R)—, where Ris selected from R, a group of formula Z—X, an unsaturated hydrocarbon group, or a ...

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09-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130115676A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , ScaI claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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09-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130115677A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , ScaI claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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09-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130115679A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , ScaI claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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09-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130115680A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , ScaI claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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09-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130115681A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , ScaI claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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09-05-2013 дата публикации

(METHYLSULFONYL) ETHYL BENZENE ISOINDOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USES

Номер: US20130116204A1
Принадлежит: Celgene Corporation

Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein Ris (cyclopropyl)-C(O)—.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris methyl.6. The compound of claim 1 , wherein Ris gluc.7. The compound of claim 1 , wherein Ris hydrogen.8. The compound of claim 1 , wherein Ris ethyl.9. The compound of claim 1 , wherein Ris hydroxyl.10. The compound of claim 1 , wherein Ris —O-gluc.13. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof.14. A method of treating claim 1 , managing or preventing a disease or disorder comprising administering to a patient a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein the disease or disorder is cancer claim 1 , a disorder associated with angiogenesis claim 1 , pain claim 1 , macular degeneration or a related syndrome claim 1 , a skin disease claim 1 , a pulmonary disorder claim 1 , an asbestos-related disorder claim 1 , a parasitic disease claim 1 , an immunodeficiency disorder claim 1 , a CNS disorder claim 1 , CNS injury claim 1 , atherosclerosis or a related disorder claim 1 , dysfunctional sleep or a related disorder claim 1 , hemoglobinopathy or a related disorder claim 1 , or a TNFα related disorder. Provided herein are (methylsulfonyl)ethyl benzene isoindoline derivatives. Pharmaceutical compositions comprising the compounds and methods for treating, preventing and managing various disorders are also provided.Many cellular functions are mediated by levels of adenosine 3′,5′-cyclic monophosphate (cAMP). Such cellular functions can contribute to inflammatory ...

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09-05-2013 дата публикации

METAL COMPLEXES WITH ORGANIC LIGANDS AND USE THEREOF IN OLEDS

Номер: US20130116755A1
Принадлежит: Merck Patent GmBH

The present invention relates, inter alia, to metal complexes having improved solubility, to processes for the preparation of the metal complexes, to devices comprising these metal complexes and to the use of the metal complexes. M(L)n(L′)m formula 1 where the compound contains a moiety M(L)n of the formula (2) W is equal to the formula (3). 117-. (canceled)23. The compound according to claim 18 , wherein m is 1 claim 18 , 2 claim 18 , 3 claim 18 , or 4.28. The compound according to claim 18 , wherein M is equal to iridium.30. A formulation comprising at least one compound according to and at least one solvent.31. An electronic device which comprises the compound according to .32. The electronic device as claimed in claim 31 , wherein in the device is an organic electroluminescent device claim 31 , an organic integrated circuit claim 31 , an organic field-effect transistor claim 31 , an organic thin-film transistor claim 31 , an organic light-emitting transistor claim 31 , an organic solar cell claim 31 , an organic optical detector claim 31 , an organic photoreceptor claim 31 , an organic field-quench device claim 31 , a light-emitting electrochemical cell or an organic laser diode.33. An organic electroluminescent device which comprises the compound according to is employed as emitting compound in one or more emitting layers.34. An organic electroluminescent device which comprises the compound according to is employed as emitting compound in one or more emitting layers claim 18 , in combination with a matrix material.35. The organic electroluminescent device according to claim 34 , wherein the matrix material is a ketone claim 34 , phosphine oxide claim 34 , sulfoxide claim 34 , sulfone claim 34 , triarylamine claim 34 , carbazole derivative claim 34 , indolocarbazole derivative claim 34 , indenocarbazole derivativs claim 34 , azacarbazole derivative claim 34 , bipolar matrix material claim 34 , silane claim 34 , azaborole claim 34 , boronic ester claim 34 , ...

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16-05-2013 дата публикации

DYE FOR PHOTOELECTRIC CONVERSION, SEMICONDUCTOR ELECTRODE, PHOTOELECTRIC CONVERSION ELEMENT, SOLAR CELL, AND NOVEL PYRROLINE-BASED COMPOUND

Номер: US20130118570A1
Принадлежит: NEC Corporation

Provided is a dye for photoelectric conversion containing at least one or more kind of a compound represented by the following General Formula (1) (in Formula (1), Rand Rrepresent any one of —CN, —SOR, —COOR, and —CONR(R represents a hydrogen atom, a substituted or unsubstituted alkyl group, a cycloalkyl group, or an aryl group); Rrepresents a direct bond or a substituted or unsubstituted alkylene group; X represents an acidic group; and D represents an organic group having an electron donating substituent or a substituted or unsubstituted heterocyclic group). 2. The dye for photoelectric conversion according to claim 1 ,wherein the acidic group is a carboxy group, a hydroxy group, a sulfonic acid group, or a phosphonic acid group.3. The dye for photoelectric conversion according to claim 1 ,wherein the organic group having an electron donating substituent is an aryl group having an electron donating substituent.4. A semiconductor electrode comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a semiconductor layer onto which at least one or more kind of the dye for photoelectric conversion according to has been adsorbed.'}5. The semiconductor electrode according to claim 4 ,wherein the semiconductor layer is constituted with a semiconductor material containing titanium oxide or zinc oxide.6. A photoelectric conversion element using the semiconductor electrode according to .7. A solar cell comprising:{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'the photoelectric conversion element according to .'} The present invention relates to a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, a solar cell, and a novel pyrroline-based compound.Since a large amount of fossil fuels represented by petroleum have been used so far, the level of COhas increased. Consequently, global warming has become a serious problem, and there is a concern over the depletion of fossil fuels. Accordingly, how the demand for a large amount ...

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16-05-2013 дата публикации

PHOTOELECTRIC CONVERSION DEVICE, PRODUCTION METHOD THEREOF, PHOTOSENSOR, IMAGING DEVICE AND THEIR DRIVE METHODS

Номер: US20130122276A1
Принадлежит: FUJIFILM Corporation

A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula. 2. An electron blocking material comprising the compound according to .3. A film comprising the compound according to claim 1 , wherein the film has a thickness of 1 to 1 claim 1 ,000 nm.4. The compound according to claim 1 , wherein Rand R′in formula (F-10) are the same.5. The compound according to claim 1 , wherein Aand Ain formula (F-10) are the same.6. The compound according to claim 1 , wherein Xa in formula (A-1) represents a single bond.7. The compound according to claim 1 , wherein the compound represented by formula (F-10) has a molecular weight of 500 to 2000.8. The compound according to claim 1 , wherein the compound represented by formula (F-10) has an ionization potential of 5.8 eV or less. 1. Field of the InventionThe present invention relates to a photoelectric conversion device, a production method thereof, a photosensor, an imaging device and their driving methods.2. Description of the Related ArtAs for the solid-state imaging device, there is widely used a flat light-receiving device where photoelectric conversion sites are two-dimensionally arrayed in a semiconductor to form pixels and a signal generated by photoelectric conversion in each pixel is charge-transferred and read out through a CCD or CMOS circuit. The conventional photoelectric conversion site generally used is a photodiode part formed using PN junction in a semiconductor such as Si.In recent years, fabrication of a multipixel device is proceeding, and the pixel size and in turn, the area of a photodiode part become small, which brings about problems of reduction in the aperture ratio, reduction in the light ...

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16-05-2013 дата публикации

High Fidelity Restriction Endonucleases

Номер: US20130122568A1
Принадлежит: NEW ENGLAND BIOLABS, INC.

Compositions and methods are provided for enzymes with altered properties that involve a systematic approach to mutagenesis and a screening assay that permits selection of the desired proteins. Embodiments of the method are particularly suited for modifying specific properties of restriction endonucleases such as star activity. The compositions includes restriction endonucleases with reduced star activity as defined by an overall fidelity index improvement factor. 1. A composition , comprising: a restriction endonuclease having at least one artificially introduced mutation and an overall fidelity index (FI) improvement factor of at least 2 , the restriction endonuclease being capable of cleaving a substrate with at least a similar cleavage activity to that of the restriction endonuclease absent the artificially introduced mutation , in a predetermined buffer , wherein the artificially introduced mutation is the product of at least one of a targeted mutation , saturation mutagenesis , or a mutation introduced through a PCR amplification procedure.2. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with an oppositely charged residue at a target site in the restriction endonuclease.3. A composition claim 1 , according to claim 1 , wherein at least one of the artificially introduced mutations is a replacement of a naturally occurring residue with a residue selected from a Phenylalanine and an Alanine at a target site in the restriction endonuclease.4. A composition claim 1 , according to claim 1 , wherein the restriction enzyme absent the at least one artificially introduced mutation is selected from the group consisting of: BamHI claim 1 , EcoRI claim 1 , Scal claim 1 , SalI claim 1 , SphI claim 1 , PstI claim 1 , NcoI claim 1 , NheI claim 1 , SspI claim 1 , NotI claim 1 , SacI claim 1 , PvuII claim 1 , MfeI claim 1 , HindIII claim 1 , SbfI claim 1 , EagI claim ...

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