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

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Применить Всего найдено 11237. Отображено 100.
27-04-2014 дата публикации

УСТАНОВКА ДЛЯ ПРОИЗВОДСТВА ЭТАНОЛАМИНОВ

Номер: RU0000139878U1
Автор: Пенкин Константин Владимирович, Сажин Сергей Григорьевич
Принадлежит: федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Нижегородский государственный технический университет им. Р.Е. Алексеева" (НГТУ)

Установка для производства этаноламинов, содержащая реактор-смеситель и реактор вытеснения, соединенные между собой линией, на которой установлены технологические емкости, линии подачи в реактор-смеситель окиси этилена, аммиака, возвратного моноэтаноламина из реактора вытеснения, линию отвода из него реакционной смеси на стадию ректификации, систему управления процессом, включающую контуры регулирования подачи окиси этилена, аммиака, возвратного моноэтаноламина к реактору-смесителю и расхода пара перед реактором вытеснения с датчиками количества подаваемых и отводимых продуктов, автоматическими регуляторами, воздействующими на регулирующие клапаны, и задатчиками, отличающаяся тем, что в контур регулирования подачи в реактор-смеситель окиси этилена введена детерминированная математическая модель реактора-смесителя, выход микропроцессорного контроллера в ее составе соединен с входом задатчика расхода окиси этилена, выход задатчика соединен с входом автоматического регулятора, воздействующего на регулирующий клапан на линии подачи окиси этилена, второй вход автоматического регулятора соединен с выходом датчика расхода окиси этилена на линии его подачи, вход микропроцессорного контроллера в составе математической модели реактора-смесителя соединен с датчиком состава реакционной смеси после реактора-смесителя, в контур регулирования подачи возвратного моноэтаноламина к реактору-смесителю и расхода пара перед реактором вытеснения введена регрессионная математическая модель реактора вытеснения, выход микропроцессорного контроллера в ее составе соединен с входом задатчика расхода пара, выход задатчика соединен с входом автоматического регулятора пара, воздействующего на регулирующий клапан на линии подачи пара, второй вход автоматического регулятора соединен с выходом датчика расхода пара на линии его подачи, вход микропроцессорного контроллера в составе регрессионной математической модели соединен с датчиком состава реакционной смеси на линии отвода ее из реактора ...

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Номер записи: 1
10-05-2012 дата публикации

Sinomenine Derivatives and Processes for their Synthesis

Номер: US20120116086A1
Автор: Bobby N. Trawick, David W. Berberich, Gary L. Cantrell, John Brandt, Peter X. Wang, Subo Liao, Tao Jiang
Принадлежит: Mallinckrodt LLC

The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates.

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Номер записи: 2
31-05-2012 дата публикации

Abuse resistant opioid drug-ion exchange resin complexes having hybrid coatings

Номер: US20120135077A1
Автор: Alivia Chaudhuri, Ashok Perumal, Ketan Mehta, Yu-Hsing Tu
Принадлежит: Tris Pharma Inc

A sustained release formulation for opioid drugs is described. The formulation contains an opioid-ion exchange resin complex having a hybrid coating. The hybrid coating contains a cured polyvinylacetate polymer and a pH-dependent enteric coating layer mixed therein. Also provided are methods of making and using same.

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Номер записи: 3
07-06-2012 дата публикации

Novel formulation of meloxicam

Номер: US20120141548A1
Автор: Aaron Dodd, Adrian Russell, Felix Meiser, H William Bosvch, Marck Norret
Принадлежит: Fundacion Universidad del Norte Co

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.

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Номер записи: 4
14-06-2012 дата публикации

Trp inhibitors and uses thereof

Номер: US20120148604A1
Автор: Eric M. Ostertag, John Stuart Crawford
Принадлежит: Transposagen Biopharmaceuticals Inc

The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.

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Номер записи: 5
05-07-2012 дата публикации

Percutaneous absorption type plaster

Номер: US20120171278A1
Автор: Koji Tanaka, Yasuhiro Ikeura, Yasunori Takada
Принадлежит: Hisamitsu Pharmaceutical Co Inc

A transdermal patch comprising a backing 2 and an adhesive layer 3 laminated on the backing 2 , wherein the adhesive layer 3 comprises a rosin-based resin and petroleum resin as a tackifier, the total compounding amount of the rosin-based resin and the petroleum resin is in a range of 15% by mass to 50% by mass, and compounding amount of the petroleum resin is 1/3 times by mass to 4 times by mass as that of the rosin-based resin.

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Номер записи: 6
16-08-2012 дата публикации

Transdermal therapeutic system for administration of fentanyl or an analog thereof

Номер: US20120209223A1
Автор: Bjoern Schurad, Ingo Teutsch, Nouha Salman
Принадлежит: Acino AG

Disclosed is a transdermal therapeutic system for administering an active ingredient through the skin comprising: a) a back layer, b) a reservoir on the back layer comprising b1) a first layer containing active ingredient, at least one gel former, at least one plasticizer, and a first polyisobutylene; and b2) a second layer containing active ingredient, at least one gel former, at least one plasticizer, and a second polyisobutylene, wherein the first polyisobutylene is different from the second polyisobutylene, wherein at least the first layer contains undissolved active ingredient in the form of active ingredient particles; and wherein the active ingredient is fentanyl or an analogue of the fentanyl.

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Номер записи: 7
18-10-2012 дата публикации

Agents for enhanced charge transport across microbial membranes

Номер: US20120264649A1
Автор: Guillermo C. Bazan, James J. Sumner, Logan E. GARNER
Принадлежит: UNIVERSITY OF CALIFORNIA

The invention provides molecules useful for enhancing charge transport across membranes, such as electron transport across membranes, and methods of using such molecules, for example in improving the performance of a microbial fuel cell or in staining microbes for observation. The amphiphilic molecule comprises a conjugated core with hydrophilic groups on either end. The amphiphilic molecule inserts into the membrane of a microbe and facilitates charge transfer across the membrane of the microbe.

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Номер записи: 8
13-12-2012 дата публикации

novel polymomorph of desvenlafaxine benzoate

Номер: US20120316238A1
Автор: Dabeer Rauf Karnalkar, Girij Pal Singh, Gurvinder Pal Singh, Hemraj Mahadeorao Lande
Принадлежит: Lupin Ltd

The present invention relates to a novel crystalline form L of (±)-desvenlafaxine benzoate and process for the preparing of the same. Further, the present invention also relates to pharmaceutical composition of novel crystalline form L of desvenlafaxine benzoate and one or more pharmaceutically acceptable excipient.

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Номер записи: 9
20-12-2012 дата публикации

Methods for controlling pain in equines using a transdermal solution of fentanyl

Номер: US20120322828A1
Автор: Amy Louise Marr, Douglas Eugene Mouzin, Jane Granville Owens, Kari Lynette Riggs
Принадлежит: Eli Lilly and Co

This invention provides methods of controlling pain in an equine for an effective period of time comprising transdermally administering a composition comprising fentanyl, a penetration enhancer, and a volatile liquid, wherein the composition is a solution. The invention also provides a single unit dose of the composition.

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Номер записи: 10
24-01-2013 дата публикации

Arachidonic acid analogs and methods for analgesic treatment using same

Номер: US20130023510A1
Автор: John R. Falck, Lane Brostrom
Принадлежит: Cytometix Inc

The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.

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Номер записи: 11
21-02-2013 дата публикации

Analgesic and anti-inflammatory composition

Номер: US20130045279A1
Автор: Jeffrey D. Edwards, John Palermo
Принадлежит: CAMBRIDGE SCIENTIFIC PTY LTD

The present invention discloses a composition that contains (1) an effective amount of an analgesically and/or anti-inflammatory active fraction separated from a mixture of plasma and/or serum, and (2) at least one metal, metal ion or metal salt, in which the mixture has been denatured. Also disclosed are methods of producing the composition for treating a subject afflicted with inflammation and/or pain.

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Номер записи: 12
28-03-2013 дата публикации

PROCESS FOR THE PREPARATION OF 2-HYDROXY-4-PHENYL-3,4-DIHYDRO-2H-CHROMEN-6-YL-METHANOL AND (R)-FESO-DEACYL

Номер: US20130079532A1
Автор: Ciambecchini Umberto, De Ferra Lorenzo, TURCHETTA Stefano, ZENONI Maurizio
Принадлежит: Chemi S.P.A.

The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B. 2. Process according to claim 1 , wherein said silylating agent is selected from among RRRSiX where R claim 1 , R claim 1 , Rare C-Clinear or branched alkyl or aryl residues possibly substituted claim 1 , X is a halogen or a sulfonate group; CYCO(MeSi)═NH(MeSi) claim 1 , where Y is hydrogen or halogen; or (MeSiNH)C═O.3. Process according to claim 1 , wherein said silylating agent is used in presence of a base.4. Process according to claim 1 , wherein said selective deprotection of the phenolic hydroxyl of the compound of formula (B) is conducted in presence of a salt of alkaline metals.5. Process according to claim 1 , wherein said cyclic secondary amine is selected from among morpholine claim 1 , N-methyl-piperazine claim 1 , N-benzyl-piperazine claim 1 , pyrrolidine and piperazine.6. Process according to claim 1 , wherein said deprotection of the compound of formula (D) is conducted in presence of fluoride ion.7. Process according to claim 1 , wherein said hydrolysis occurs by mixing the reaction mixture with an aqueous solution having a pH below 1.8. Process according to claim 7 , wherein 5 to 100 volumes of aqueous solution per volume of reaction mixture are used.9. Process according to claim 1 , wherein the compounds of formula (B) claim 1 , (D) and/or (E) are not isolated.11. Process according to claim 10 , wherein said metal hydride is sodium ...

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Номер записи: 13
04-04-2013 дата публикации

AROMATIC BUTAN-2-OL COMPOUNDS AND PREPARATION AND USES THEREOF

Номер: US20130085183A1
Автор: Li Song, Li Xingzhou, Liu Ping, Wang Lili, Wang Xiaokui, Xiao Junhai, Xie Yunde, Zhao Guoming, Zheng Zhibing, Zhong Wu, Zhou Xinbo
Принадлежит: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA

Aromatic butan-2-ol compounds, preparation methods for making the compounds, and uses of the compounds are provided. Specifically, the compound of Formula I, or an optical isomer, racemate, diastereomer, pharmaceutically acceptable salt, or solvate thereof, is provided, where each of the substituents is defined. In addition, a pharmaceutical composition containing the compound, and the use of the compound in manufacture of a medicament for the treatment and/or prophylaxis of a disease or disorder caused by infection, is provided. 2. The compound of Formula I according to claim 1 , or an optical isomer claim 1 , racemate claim 1 , diastereomer claim 1 , pharmaceutically acceptable salt claim 1 , or solvate thereof claim 1 , wherein{'sub': '1', 'Rrepresents hydrogen, fluoro, chloro, bromo, iodo, or methoxy;'}{'sub': '2', 'Rrepresents hydrogen, fluoro, chloro, bromo, or iodo;'}{'sub': 3', '1-8, 'Rrepresents hydrogen, fluoro, chloro, bromo, iodo, or a Calkyl substituted at an o-, m-, or p-position of the phenyl ring;'}{'sub': '4', 'Rrepresents phenyl, substituted phenyl, or naphthyl; and'}{'sub': 5', '1-8, 'Rrepresents hydroxy, thiol, a Calkoxy, or methylthio.'}3. The compound of Formula I according to claim 2 , or an optical isomer claim 2 , racemate claim 2 , diastereomer claim 2 , pharmaceutically acceptable salt claim 2 , or solvate thereof claim 2 , wherein{'sub': '1', 'Rrepresents hydrogen, fluoro, chloro, bromo, or iodo;'}{'sub': 3', '1-6, 'Rrepresents hydrogen, fluoro, chloro, bromo, iodo, or a Calkyl substituted at an o-, m-, or p-position of the phenyl ring;'}{'sub': '4', 'Rrepresents phenyl, phenyl substituted with one or more halogens, or naphthyl; and'}{'sub': 5', '1-6, 'Rrepresents hydroxy or a Calkoxy.'}4. The compound of Formula I according to claim 3 , or an optical isomer claim 3 , racemate claim 3 , diastereomer claim 3 , pharmaceutically acceptable salt claim 3 , or solvate thereof claim 3 , wherein{'sub': '1', 'Rrepresents hydrogen, chloro, or bromo ...

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Номер записи: 14
11-04-2013 дата публикации

SOLID STATE FORMS OF TAPENTADOL SALTS

Номер: US20130090314A1
Автор: Ahirao Vikas Daulatrao, BONDGE Sandipan Prabhurao, Khunt Mayur Devjibhai, Pradhan Nitin Sharadchandra
Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt. 1. Solid state form of a salt of 3-[(1R ,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol (tapentadol salt) , wherein the salt of tapentadol is an L-(−)-camphorsulfonate salt , a dibenzoyl-(D)-tartrate salt , a malate salt , a maleate salt , or a salicylate salt.2. The solid state form of tapentadol salt of claim 1 , which is in a crystalline form or in an amorphous form claim 1 , and wherein the solid state form is anhydrous and/or solvent-free form claim 1 , or a hydrate and/or a solvate form.3. The solid state form of tapentadol salt of claim 1 , having the following characteristics claim 1 , wherein: [{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 3.93, 5.66, 14.94, 16.16 and 21.52±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional peaks at about 8.01, 11.36, 14.10, 15.27, 15.91, 16.72, 19.06, 19.88, 21.85, 22.56, 23.92 and 27.12±0.2 degrees 2-theta; and', {'figref': {'@idref': 'DRAWINGS', 'FIG. 2'}, 'iv) a differential scanning calorimetric (DSC) thermogram substantially in accordance with ;'}], 'a) the solid state form of tapentadol L-(−)-camphorsulfonate salt is characterized by one or more of the following properties [{'figref': {'@idref': 'DRAWINGS', 'FIG. 5'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 8.52, 9.39, 11.81, 12.28, 13.46, 14.06, 17.77, 17.97, 18.33, 18.79, 19.58 and 20.05±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional ...

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Номер записи: 15
18-04-2013 дата публикации

NOVEL PROCESS FOR PREPARING HIGHLY PURE TAPENTADOL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

Номер: US20130096347A1
Автор: BONDGE Sandipan Prabhurao, Khunt Mayur Devjibhai, Pagire Haushabhau Shivaji, Patil Nilesh Sudhir, Pradhan Nitin Sharadchandra
Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein is a novel, commercially viable and industrially advantageous process for the preparation of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol (Tapentadol), or a pharmaceutically acceptable salt thereof, and its intermediates, in high yield and purity. Provided also herein are novel solid state forms of tapentadol intermediates and processes for their preparation thereof. Provided further herein is a purification process for preparing highly pure tapentadol hydrochloride. 2. The process of claim 1 , wherein the first solvent used in step-(a) is selected from the group consisting of water claim 1 , an alcohol claim 1 , an ether claim 1 , a hydrocarbon claim 1 , a chlorinated hydrocarbon claim 1 , a nitrile solvent claim 1 , a polar aprotic solvent claim 1 , and mixtures thereof; wherein the second solvent used in step-(b) is selected from the group consisting of a ketone claim 1 , a cyclic ether claim 1 , an aliphatic ether claim 1 , and mixtures thereof; wherein the third solvent used in step-(c) is selected from the group consisting of water claim 1 , an alcohol claim 1 , a ketone claim 1 , an ester claim 1 , a hydrocarbon claim 1 , a chlorinated hydrocarbon claim 1 , a polar aprotic solvent claim 1 , and mixtures thereof; wherein the fourth solvent used in step-(e) is selected from the group consisting of water claim 1 , an alcohol claim 1 , a ketone claim 1 , a cyclic ether claim 1 , an aliphatic ether claim 1 , a hydrocarbon claim 1 , a chlorinated hydrocarbon claim 1 , a nitrile claim 1 , an ester claim 1 , and mixtures thereof; and wherein the fifth solvent used in step-(f) is selected from the group consisting of water claim 1 , an alcohol claim 1 , a ketone claim 1 , a cyclic ether claim 1 , an aliphatic ether claim 1 , a hydrocarbon claim 1 , a chlorinated hydrocarbon claim 1 , a nitrile solvent claim 1 , and mixtures thereof3. The process of claim 2 , wherein the first solvent used in step-(a) is selected from the group consisting ...

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Номер записи: 16
16-05-2013 дата публикации

Adhesive Compositions for Bonding Composites

Номер: US20130123513A1
Автор: Rammon Richard M., Williamson Bobby Lee
Принадлежит: GEORGIA-PACIFIC CHEMICALS LLC

The present invention relates to a non-thermosetting composition made by reacting epichlorohydrin and a primary amine, to the use of that composition for making thermosetting (curable) adhesives suitable for bonding composites, to a method of preparing composites using the thermosetting (curable) adhesives, and to the related composites bonded with the thermosetting (curable) adhesives. 1. A non-thermosetting, reaction product of (a) epichlorohydrin and (b) an amine selected from the group consisting of ammonia, a primary amine and mixtures thereof, wherein the reaction product is produced by reacting the epichlorohydrin and the amine in a ratio of 0.40 to 0.92 moles of epichlorohydrin per atom equivalent of amine hydrogen and wherein the epi-amine reaction product is produced by reacting in a serial fashion separate portions of the epichlorohydrin and separate portions of the amine at a temperature of not greater than 60° C. This application is a divisional of co-pending U.S. patent application Ser. No. 12/718,391, filed on Mar. 5, 2010, which claims the benefit of U.S. Provisional Application No. 61/158,013 filed Mar. 6, 2009, each of which is hereby incorporated by reference in its entirety.The present invention is directed to a non-thermosetting composition made by reacting epichlorohydrin and an amine, to the use of that composition for making thermosetting (curable) adhesives, particularly adhesives suitable for bonding composites, to a method of preparing composites, particularly wood composites using the thermosetting (curable) adhesives, and to the related composites bonded with the cured thermosetting (curable) adhesives.A variety of composite materials are made by bonding into a unitary product a primary constituent, often a structural or reinforcement component, using a bonding agent or matrix material, such as an adhesive resin. Composites include engineered wood products (wood-adhesive composite products), insulation products and the like.Wood-adhesive ...

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Номер записи: 17
16-05-2013 дата публикации

Methods for preparing ritodrine hydrochloride

Номер: US20130123539A1
Автор: Jacopo Zanon
Принадлежит: Lundbeck Pharmaceuticals Italy SpA

Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.

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Номер записи: 18
30-05-2013 дата публикации

Chelator Stabilized Cationic Ammonium Compounds and Compositions Comprising the Same

Номер: US20130137773A1
Автор: Au Van, MADISON Stephen Alan
Принадлежит: CONOPCO, INC., D/B/A UNILEVER

Stabilized cationic ammonium compounds are described. The compounds are stabilized with pyridine-based chelators and/or heteroketo-based chelators that impede the generation of nitrogen comprising groups from the cationic ammonium compounds. 1. A composition comprising a cationic ammonium compound and a pyridine-based chelator , a heteroketo-based chelator , or both , the chelator being one which impedes the generation of a nitrogen comprising group from the cationic ammonium compound within the composition wherein the nitrogen comprising group comprises a trimonium group.3. The composition according to wherein the anionic counterion is organic or inorganic.5. The composition according to wherein the cationic ammonium compound is a salt of hydroxypropyltri (C-Calkyl) ammonium mono-substituted-saccharide claim 2 , salts of hydroxypropyltri (C-Calkyl) ammonium mono-substituted polyols claim 2 , dihydroxypropyltri (C-Calkyl) ammonium salts claim 2 , dihydroxypropyldi (C-Calkyl) mono(hydroxyethyl) ammonium salts claim 2 , guar hydroxypropyl trimonium salts claim 2 , 2 claim 2 ,3-dihydroxypropyl tri(C-Calkyl or hydroxalkyl) ammonium salts or mixtures thereof.6. The composition according to wherein the cationic ammonium compound is 1 claim 2 ,2-dihydroxypropyltrimonium chloride.8. The composition according to wherein the composition is topically applied to the body.9. The composition according to wherein the composition is a leave-on or rinse off composition.10. The composition according to wherein the composition is a moisturizing composition.11. The composition according to wherein the cationic ammonium compound is a salt of a hydroxypropyltri (C-Calkyl) ammonium mono-substituted saccharide claim 9 , salts of hydroxypropyltri (C-Calkyl) ammonium mono-substituted polyols claim 9 , dihydroxypropyltri (C-Calkyl) ammonium salts claim 9 , dihydroxypropyldi (C-Calkyl) mono(hydroxyethyl) ammonium salts claim 9 , guar hydroxypropyl trimonium salts claim 9 , 2 claim 9 ,3- ...

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Номер записи: 19
13-06-2013 дата публикации

TARGETING OF T-LYMPHOCYTES TO TREAT AMYOTROPHIC LATERAL SCLEROSIS

Номер: US20130150454A1
Автор: Gil Alan, Lincecum John, Perrin Steven, Vieira Fernando
Принадлежит: ALS Therapy Development Institute

Methods and therapeutic compositions are disclosed for treating neurodegenerative disorders and, in particular Amyotrophic Lateral Sclerosis, using sphingosine1-phosphate receptor modulators, such as fingolimod or a pharmaceutically acceptable salt, hydrate, or solvate thereof. 2. The method of claim 1 , wherein Ris an unsubstituted straight or branched C-Calkyl claim 1 , C-Calkenyl claim 1 , or C-Calkynyl and m is 2.3. The method of claim 2 , wherein the Ris an unsubstituted straight chain Calkyl.5. The method of claim 1 , wherein both Rare OH claim 1 , both Rare P(O)(OH) claim 1 , or one Ris OH and the other Ris P(O)OH).6. The method of claim 1 , wherein the compound is a chloride salt.8. The method of claim 7 , wherein the compound a hydrochloride salt claim 7 , or a phosphate salt thereof.9. The method of claim 1 , wherein Ris a C-Calkyl wherein one or more of the carbon atoms in Ris substituted with a moiety selected from O claim 1 , S claim 1 , and phenyl claim 1 , n is 1 claim 1 , and Ris a halogen.11. The method of claim 10 , wherein the compound a hydrochloride salt claim 10 , or a phosphate salt thereof.12. The method of claim 1 , further comprises inhibiting macrophage accumulation.13. The method of claim 12 , wherein macrophage accumulation is localized in the axons of nerves innervating the skeletal muscle.14. The method of claim 12 , wherein inhibiting macrophage accumulation inhibits at least 50% compared to the macrophage population prior to administering the compound.15. The method of claim 12 , wherein inhibiting macrophage accumulation inhibits CD11b positive macrophages.16. The method of claim 1 , further comprises reducing lymphocyte proliferation.17. The method of claim 16 , wherein reducing lymphocyte proliferation comprises reducing the concentration of one or more of CD8+ T cell claim 16 , CD4+ T cell claim 16 , and CD45R+ T cell in whole blood by at least 30 percent compared to the concentration in whole blood prior to administering the ...

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Номер записи: 20
13-06-2013 дата публикации

STEREOSELECTIVE SYNTHESIS OF TAPENTADOL AND ITS SALTS

Номер: US20130150622A1
Автор: Fandrick Daniel Robert, RODRIGUEZ Sonia, YANG Bing-Shiou
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

A process for the synthesis of a salt of tapentadol. 2. The process according to claim 1 , wherein the suitable solvent of steps (a) to (g) are each organic solvents claim 1 , preferably anhydrous organic solvents.3. The process according to claim 1 , wherein the suitable solvent of step (a) is anhydrous dimethylformamide (DMF) claim 1 , anhydrous dimethylsulfoxide (DMSO) claim 1 , anhydrous dimethyl acetamide (DMAc) claim 1 , anhydrous ethanol claim 1 , anhydrous methanol claim 1 , anhydrous n-propanol claim 1 , anhydrous 2-butanol claim 1 , anhydrous 1-butanol claim 1 , anhydrous tetrahydrofuran (THF) claim 1 , anhydrous 2-methyltetrahydrofuran (2-MeTHF) claim 1 , anhydrous dioxane claim 1 , anhydrous toluene claim 1 , anhydrous ethyl acetate claim 1 , anhydrous isopropyl acetate claim 1 , or a mixture thereof.4. The process according to claim 1 , wherein the suitable solvent of step (b) is anhydrous 2-MeTHF claim 1 , anhydrous THF claim 1 , anhydrous toluene claim 1 , anhydrous dioxane claim 1 , anhydrous methyl tert-buyl ether (MTBE) claim 1 , anhydrous cyclopentyl methyl ether claim 1 , or anhydrous diethyl ether.5. The process according to claim 1 , wherein step (b) is accomplished using a suitable reducing agent claim 1 , the reducing agent preferably selected from lithium borohydride claim 1 , sodium borohydride claim 1 , lithium aluminum hydride claim 1 , disobutyl aluminum hydride claim 1 , or RedAl.6. The process according to claim 1 , wherein the suitable solvent of step (c) is THF claim 1 , 2-MeTHF claim 1 , toluene claim 1 , dioxane claim 1 , MTBE claim 1 , cyclopentyl methyl ether claim 1 , diethyl ether claim 1 , or a mixture thereof.7. The process according to claim 1 , wherein claim 1 , the organometallic catalyst of step (d) is [Ir(COD)Cl]or [Ir(COE)Cl].8. The process according to claim 1 , wherein the suitable solvent of step (d) is dichloromethane claim 1 , THF claim 1 , toluene claim 1 , dioxane claim 1 , MTBE claim 1 , cyclopentyl methyl ether ...

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Номер записи: 21
27-06-2013 дата публикации

PROCESS FOR THE PREPARATION OF EFAVIRENZ

Номер: US20130165650A1
Автор: Galvagni Marco, Leganza Alessandro
Принадлежит: F.I.S. Fabbrica Italiana Sintetici S.p.A

A process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I): This is a continuation of application Ser. No. 13/060,839, filed on Feb. 25, 2011, which is a 371 of PCT/EP09/00612, filed on Jan. 30, 2009.The present invention is directed to a process for the preparation of Efavirenz.Efavirenz is a well known non-nucleoside reverse transcriptase inhibitor (NNRTI) that is used in the antiretroviral therapy of HIV-1. Efavirenz is on the market for this use since 1998.Several processes are known in the prior art to produce this active substance that start from the intermediate of formula (II):This intermediate, (2S)-2-(2-amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yn-2-ol, as a free base, is reacted with a chloroformate derivative in basic conditions to give, after 1 to 6 hours reaction, an alkyl carbamate intermediate (reaction of the amine moiety of intermediate (II) with the chloroformate derivative) that is then cyclized to yield Efavirenz.Even if this kind of reaction allows to obtain Efavirenz with an acceptable impurities profile, it has some disadvantages due to the length of the reaction time and/or the quite complicate work-up, as the alkyl carbamate intermediate must be isolated or the reaction mixture must be at least separated and concentrated before undergoing the cyclization step. No one-step process using chloroformate derivatives has been proposed so far, nor thrichloromethylchloroformate (diphosgene) has been proposed as a reactant of choice in this process.It has now been surprisingly found that by reacting intermediate (II) with diphosgene in pretty neutral or slightly basic conditions, it is possible to obtain Efavirenz with a one-step process in a short time and with high yield and purity.A process is provided for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-214-3,1-benzoxazin-2-one, of formula ...

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Номер записи: 22
27-06-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF CHOLINE SALTS

Номер: US20130165694A1
Автор: Lustig Steven Raymond, Redder Dennis A.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

A method to synthesize choline salts to be used as inexpensive ingredients for application in ionic liquids or other applications is disclosed. 1. A process for the synthesis of one or more choline salts , comprising:(a) providing an aqueous solution of choline;(b) combining the aqueous solution of choline with a hydrophobic organic solvent and an excess of free acid to form a first acidic, solution;(c) combining the first acidic solution with one or more alcohols to form a first extraction mixture;(d) separating the first extraction mixture into a lower phase, a middle phase and an upper phase; and(e) recovering the lower phase of the first extraction mixture to provide a first aqueous solution of a choline salt.2. A process according to further comprising:(f) combining the first aqueous solution of choline salt with an excess of free acid and a hydrophobic organic solvent to form a second acidic solution;(g) combining the second acidic solution with at least one alcohol and to form a second extraction mixture;(h) separating the second extraction mixture into a lower phase, a middle phase and an upper phase; and(i) recovering the lower phase of the second extraction mixture to provide a second aqueous solution of a choline salt.3. A process according to further comprising isolating the choline salt from the first aqueous solution of choline salt.4. A process according to further comprising isolating the choline salt from the second. aqueous solution of choline salt.5. A process according to further comprising recycling the hydrophobic organic solvent for further use in the process.4. A process according to wherein the alcohol comprises at least one Cto Calcohol.5. A process according to wherein the alcohol comprises ethanol claim 1 , propanol or isopropanol.6. A process according to wherein the hydrophobic organic solvent comprises a high-boiling-point alkane.7. A process according to wherein the hydrophobic organic solvent comprises cyclohexane.8. A process ...

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Номер записи: 23
11-07-2013 дата публикации

MONOCATIONIC POLYHYDROXYL COMPOUNDS

Номер: US20130178542A1
Автор: Brehm Nicole, Deavenport Joseph
Принадлежит: Dow Global Technologies LLC

Described are novel monocationic polyhydroxyl compounds and their uses in personal care compositions. 2. The compound of claim 1 , wherein Rand Rare each H.3. The compound of claim 1 , wherein Rand Rare each H.4. The compound of claim 1 , wherein Rand Rare each —CH.5. The compound of claim 1 , wherein Rand Rare each —CHCH(OH)CHOH.6. The compound of claim 1 , wherein Rand Rare each —CHCHOH.7. The compound of claim 1 , wherein Ris —(CH)CHand Ris —CHCHOH.8. The compound of claim 1 , wherein Ris —CHOH.9. The compound of claim 1 , wherein Ris —CHCH.10. The compound of claim 1 , wherein Rand Rcooperate to form a cyclohexyl group.12. A method for providing humectancy in a personal care composition claim 1 , comprising including the compound of into the personal care composition.13. A hair care composition containing the compound of .14. A skin care composition containing the compound of . The present invention relates to novel monocationic polyhydroxyl compounds and their uses in personal care compositions.Polyhydroxyl compounds, or polyols, have a number of uses, from raw materials used in the manufacture of urethane foams to humectants for personal care products like shaving foams, lotions, and shampoos.Quaternary ammonium compounds are also useful in a number of applications, such as for disinfectants, surfactants, fabric softeners, and conditioners in shampoos.Despite the number of available conventional compounds, there is a strong need for novel compounds with properties to differentiate performance or offer synergistic effects in areas of interest, particularly in personal care compositions.In one embodiment, the present invention provides compounds, including salts, of the Formula (I):wherein:The term “optionally substituted” as used herein means that the groups in question are either unsubstituted or substituted with one or more groups, radicals or moieties, selected from halogen, hydroxy, amino or carboxy. When the groups in question are substituted with more ...

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Номер записи: 24
11-07-2013 дата публикации

NOVEL PRECURSOR OF RADIOLABELLED CHOLINE ANALOG COMPOUNDS

Номер: US20130178653A1
Автор: Aboagye Eric Ofori, ROBINS EDWARD GEORGE, Smith Graham, Zhao Yongjun
Принадлежит:

The present invention describes intermediate(s), pre-cursor(s), for the preparation of radialabelled choline analogs to be used as radiotracers for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of diseases. 2. A compound according to wherein:{'sub': 1', '2', '3', '4, 'R, R, R, and Rare each independently hydrogen;'}{'sub': 5', '6', '7', '8', '2', 'm', '8', '2', 'm', '8', '2', 'm', '8', '8', '2, 'R, R, and Rare each independently hydrogen, R, —(CH)R, —(CD)R, —(CF)R, or —CD(R);'}{'sub': 8', '3', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '6', '5, 'Ris hydrogen, —OH, —CH, —CF, —CHOH, —CHF, —CHCl, —CHBr, —CHI, —CD, —CDOH, —CDF, CDCl, CDBr, CDI, or —CH; and'}m is an integer from 1-4.3. A compound according to wherein:{'sub': 1', '2, 'Rand Rare each hydrogen;'}{'sub': 3', '4, 'Rand Rare each deuterium (D);'}{'sub': 5', '6', '7', '8', '2', 'm', '8', '2', 'm', '8', '2', 'm', '8', '2, 'sup': '8', 'R, R, and Rare each independently hydrogen, R, —(CH)R, —(CD)R, —(CF)R, or —CD(R);'}{'sub': 8', '3', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '6', '5, 'Ris hydrogen, —OH, —CH, —CF, —CHOH, —CHF, —CHCl, —CHBr, —CHI, —CD, —CDOH, —CDF, CDCl, CDBr, CDI, or —CH; and'}m is an integer from 1-4.7. A compound according to wherein Pg is a p-methoxybenyzl (PMB) claim 6 , trimethylsilyl (TMS) claim 6 , or a dimethoxytrityl (DMTr) group.8. A compound according to wherein Pg is a p-methoxybenyzl (PMB) group.10. A compound according to wherein:{'sub': 1', '2', '3', '4, 'R, R, R, and Rare each independently hydrogen;'}{'sub': 5', '6', '7, 'with the proviso that R, R, and Rare each not hydrogen.'}11. A compound according to wherein:{'sub': 1', '2', '3', '4, 'R, R, R, and Rare each deuterium (D);'}{'sub': 5', '6', '7, 'R, R, and Rare each not hydrogen.'}12. A compound according to claim 9 , wherein:{'sub': 1', '2, 'Rand Rare each hydrogen; and'}{'sub': 3', '4, 'Rand Rare each deuterium (D).'} The present invention ...

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Номер записи: 25
18-07-2013 дата публикации

ISOTOPIC CARBON CHOLINE ANALOGS

Номер: US20130183239A1
Автор: Aboagye Eric Ofori, Luthra Sajinder, ROBINS EDWARD GEORGE, Smith Graham
Принадлежит:

Novel choline-derived radiotracer (s) having an isotopic carbon for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer—primary tumor, nodal disease or metastases). 21. The compound according to Claim wherein C* is C , C , or C.31. The compound according to Claim wherein C* is C; X and Y are each hydrogen; and Z is F.41. The compound according to Claim wherein C* is C; X claim 1 , Y and Z are each hydrogen H; R claim 1 , R claim 1 , R claim 1 , and Rare each deuterium (D); and R claim 1 , R claim 1 , and Rare each hydrogen. 5. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or excipient.6. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or excipient.7. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or excipient.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or excipient. The present invention describes a novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer—primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), precursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).The biosynthetic product of choline kinase (EC 2.7.1.32) activity, phosphocholine, is elevated in several cancers and is a precursor for membrane phosphatidylcholine (Aboagye, E. O., et al., 1999; 59:80-4; Exton, J. H., 1994; 1212:26-42; George, T. P., et al., 1989; 104:283-91; and ...

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Номер записи: 26
18-07-2013 дата публикации

ANTI-MICROBIAL AND ANTI-STATIC SURFACE TREATMENT AGENT WITH QUATERNARY AMMONIUM SALT AS ACTIVE INGREDIENT AND METHOD FOR PREVENTING STATIC ELECTRICITY IN POLYMER FIBERS USING SAME

Номер: US20130183456A1
Автор: KIM Seong Cheol
Принадлежит: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YEUNGNAM UNIVERSITY

Provided are an anti-static and anti-microbial surface treatment agent including a quaternary ammonium salt compound as an active ingredient and a method of preventing a polymer fiber from developing static electricity by using the surface treatment agent. The quaternary ammonium salt compound has excellent anti-static and anti-microbial effects for the prevention or improvement of static electricity in a polymer fiber. Accordingly, the quaternary ammonium salt compound is suitable for use as a fabric softener, or an anti-static agent, and also, provides anti-microbial effects to a polymer fiber. 2. A method of preventing static electricity in a polymer fiber claim 1 , comprising treating the polymer fiber with a surface treatment agent of .3. The method of claim 1 , wherein the method comprises: dipping the polymer fiber in a solvent; and treating the polymer fiber with the surface treatment agent of and a reaction catalyst.4. The method of claim 3 , wherein the reaction catalyst is treated at room temperature.5. The method of claim 3 , further comprising claim 3 , prior to the treating the polymer fiber with the surface treatment agent of claim 3 , forming a radical of the polymer fiber by using at least one treatment selected from (i) a treatment with a reaction catalyst claim 3 , (ii) irradiation of gamma ray claim 3 , (iii) irradiation of E-beam claim 3 , (iv) irradiation of ion-beam claim 3 , (v) irradiation of deep ultra violet (UV) light claim 3 , and (vi) a plasma treatment.6. The method of claim 5 , comprisingforming a radical of the polymer fiber by using at least one treatment selected from (i) a treatment with a reaction catalyst, (ii) irradiation of gamma ray, (iii) irradiation of E-beam, (iv) irradiation of ion-beam, (v) irradiation of deep ultra violet (UV) light, and (vi) a plasma treatment; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'adding the surface treatment agent of to the radical of the polymer fiber to form a covalent bond with a ...

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Номер записи: 27
25-07-2013 дата публикации

CRYSTALS OF CARBOPROST TROMETHAMINE AND THE PREPARATION METHOD AS WELL AS THE USES THEREOF

Номер: US20130190404A1
Автор: Gao Xiaoliang, Ji Xiaoming, Li Ming, Tang Zhijun
Принадлежит: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.

Disclosed is a crystal of carboprost tromethamine as represented by Formula (I). The crystal has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 6.6±0.2°, 9.9±0.2°, 18.5±0.2° and 20.1±0.2°. Furthermore, also disclosed are preparation method and the use of the crystal. 2. The crystal of carboprost tromethamine according to claim 1 , wherein said crystal further has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 19.3±0.2° claim 1 , 19.5±0.2° claim 1 , 19.9±0.2° and 21.6±0.2°.3. The crystal of carboprost tromethamine according to claim 1 , wherein said crystal further has characteristic peaks in the X-ray diffraction pattern at the following 2θ angles: 13.3±0.2° claim 1 , 15.8±0.2° claim 1 , 16.7±0.2° claim 1 , 17.7±0.2° claim 1 , 18.1±0.2° claim 1 , 20.8±0.2° claim 1 , 21.1±0.2° claim 1 , 26.9±0.2° claim 1 , 27.6±0.2° claim 1 , 33.8±0.2° and 40.8±0.2°.4. The crystal of carboprost tromethamine according to claim 1 , wherein the maximum peak is at 103.97±5° C. in the differential scanning calorimetry (DSC).5. The crystal of carboprost tromethamine according to claim 1 , wherein the infrared Spectrum of said crystal is shown in .7. The method according to claim 6 , wherein said solvent is selected from the group consisting of acetonitrile claim 6 , acetone claim 6 , ethyl ether claim 6 , and a C1-4 straight or branched chain alcohol.8. The method according to claim 6 , wherein the temperature for dissolving the carboprost in step a is 0° C.-100° C.9. The method according to claim 6 , wherein the amount of said solvent in step (a) ranges from 1000:1 to 1:1 (ml solvent/g carboprost).10. The method according to claim 6 , wherein when adding the aqueous trometamol into said solution dropwise in step (b) claim 6 , the temperature is 20° C.-100° C.11. The method according to claim 6 , wherein claim 6 , the molar ratio of trometamol added in step (b) to carboprost ranges from 0.8:1 to 1.2:1.12. The method ...

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Номер записи: 28
01-08-2013 дата публикации

Anti-asic1 antibodies and uses thereof

Номер: US20130195878A1
Автор: Lynn Macdonald, Marc R. Morra, Michael L. LaCROIX-FRALISH, Min Gao, Nicole M. ALESSANDRI-HABER
Принадлежит: Regeneron Pharmaceuticals Inc

The present invention provides antibodies and antigen-binding fragments thereof that specifically bind to cells expressing acid-sensing ion channel-1 (ASIC1). According to certain embodiments of the invention, the antibodies inhibit acid-induced, ASIC1-mediated ion currents in cells expressing human ASIC1. The antibodies of the invention are useful for the treatment of pain, including pain associated with surgical intervention and various diseases and disorders.

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Номер записи: 29
01-08-2013 дата публикации

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

Номер: US20130197096A1
Автор: Gall Anna, Hong Feng, Kuksa Vladimir A., Little Thomas, Orme Mark W., Scott Ian L.
Принадлежит: Acucela, Inc.

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 168.-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/977,957, filed Oct. 5, 2007; U.S. Provisional Application No. 61/066,353, filed Feb. 19, 2008; U.S. Provisional Application No. 61/043,127, filed Apr. 7, 2008; U.S. Provisional Application No. 61/051,657, filed May 8, 2008; and U.S. Provisional Application No. 61/060,083, filed Jun. 9, 2008, each of which is incorporated herein by reference in its entirety.Neurodegenerative diseases, such as glaucoma, macular degeneration, and Alzheimer's disease, affect millions of patients throughout the world. Because the loss of quality of life associated with these diseases is considerable, drug research and development in this area is of great importance.Age-related macular degeneration (AMD) affects between ten and fifteen million patients in the United States, and it is the leading cause of blindness in aging populations worldwide. AMD affects central vision and causes the loss of photoreceptor cells in the central part of retina called the macula. Macular degeneration can be classified into two types: dry-form and wet-form. The dry-form is more common than the wet; about 90% of age-related macular degeneration patients are diagnosed with the dry-form. The wet-form of the disease and geographic atrophy, which is the end-stage phenotype of dry-form AMD, causes the most serious vision loss. All patients who develop wet-form AMD are believed to previously have developed dry-form AMD for a prolonged period of time. The exact causes of AMD are ...

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Номер записи: 30
01-08-2013 дата публикации

New Solid Forms of [4-(3-Fluoro-5-Trifluoromethyl-Pyridin-2-Yl)-Piperazin-1-Yl-[5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methyl-Ethoxy)-Phenyl]Methanone

Номер: US20130197225A1
Автор: Bubendorf Andre, Diodone Ralph, Dyenet-Vucenovic Annette, Grassmann Olaf, Lindenstruth Kai, Pinard Emmanuel, Rohrer Franziska E., Schwitter Urs
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease. 1. An amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2 ,2 ,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone characterized by an absence of sharp X-ray peaks in its XRPD pattern and/or by an infrared spectrum having sharp bands at 1642 , 1622 , 1599 , 1579 , 1509 , 1487 , 1399 , 1329 , 1293 , 1253 , 1159 , 1124 , 1090 , 1016 , 960 , 920 , 903 , 889 , 827 , 782 , 763 , 739 and 636 cm(±3 cm).2. An amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2 ,2 ,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone characterized by a glass transition temperature (DSC , heating rate 10 K/min , closed pan) of about 48° C. to about 65° C.3. A methylparaben cocrystal form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2 ,2 ,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone characterized by at least three peaks selected from the following X-ray diffraction peaks obtained with a CuKα radiation , expressed in degrees 2Theta=8.0 , 8.9 , 10.5 , 12.6 , 15.2 , 16.1 , 17.7 , 18.5 , 19.8 , 20.2 , 21.7 , 22.9 , 24.2 and 25.9 (±0.2).4. A methylparaben cocrystal form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2 ,2 ,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone characterized by the following X-ray diffraction peaks obtained with a ...

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Номер записи: 31
08-08-2013 дата публикации

2,4,5-TRIAMINOPHENOLS AND RELATED COMPOUNDS

Номер: US20130204041A1
Автор: Ritter Joachim C.
Принадлежит: E I DU PONT DE NEMOURS AND COMPAN

New triaminophenol compositions and related compounds are disclosed, as are processes for their preparation and for the preparation of novel salts and diacid complexes from such compounds. Polymers prepared from these compositions can be made into high strength fiber, film., and tape and are useful in applications such as protective apparel, aircraft., automotive components, personal electronics, and sports equipment. 2. The composition of wherein Ris methyl and R claim 1 , R claim 1 , RRRR claim 1 , and Rare each H.3. The composition of wherein R claim 1 , R claim 1 , R claim 1 , RRRR claim 1 , and Rare each H.5. The composition of wherein R claim 4 , R claim 4 , and Rare each independently H claim 4 , A is HCl claim 4 , and n is 2 to 4. This application claims priority under 35 U.S.C. §119(e) from, and claims the benefit of, U.S. Provisional Application No. 61/288,417, filed Dec. 21, 2009, which is by this reference incorporated in its entirety as a part hereof for all purposes,This disclosure relates to new compositions based on 2,4,5-triaminaphenols, which can be used in the manufacture of high-performance polybenzimidazole polymers.Aromatic amines and phenols are useful as monomers for high performance polymers such as aramid polymers and polybenzarenazoles. The structure of the specific monomer used greatly impacts polymer properties such as tenacity, solubility, and also the rheological behavior of the polymer during processing such as spinning. It is thought that replacing highly symmetric monomers that are currently used (e.g., 2,3,5,6-tetraamino pyridine) with asymmetric monomers would increase the solubility of the corresponding polymers and the ease with which they are processed. However, such monomers are often difficult to synthesize or are unknown. These materials are unknown and have not been synthesized.A need thus remains for asymmetric monomers that can be readily synthesized and used in the production of high performance polymers such as aramid ...

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Номер записи: 32
15-08-2013 дата публикации

Neo-tryptophan

Номер: US20130210740A1
Автор: Abdul Fauq, Bernadette Marie Cusack, Beth Marie Tyler, Daniel J. McCormick, Elliott Richelson, Mona Boules, Yuan-Ping Pang
Принадлежит: Mayo Foundation for Medical Education and Research

Methods of inducing antinociception in a human are described. The method includes the step of administering an effective dose of a polypeptide comprising L-neo-tryptophan to the human extracranially. The polypeptide containing L-neo-tryptophan could be, but is not limited to, NT64L, NT65L, NT66L, NT67L, NT69L, NT69L′, NT71, NT72, NT73, NT74, NT75, NT76, or NT77.

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Номер записи: 33
15-08-2013 дата публикации

SYNTHESIS OF BICYCLIC COMPOUNDS AND METHOD FOR THEIR USE AS THERAPEUTIC AGENTS

Номер: US20130210904A1
Автор: BOULANGER Martin J., BRANT Michael G., Bromba Caleb M., Mason Jeremy W., Wulff Jeremy E.
Принадлежит:

Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds. 2. The compound according to where the heteroatom-containing moiety is selected from aldehyde claim 1 , acyl halide claim 1 , carbonate claim 1 , carboxyl claim 1 , carboxylate claim 1 , ether claim 1 , ester claim 1 , hydroxyl claim 1 , ketone claim 1 , silyl ether claim 1 , peroxy claim 1 , hydroperoxy claim 1 , phosphate claim 1 , phosphonate claim 1 , phosphoryl claim 1 , phosphodiester claim 1 , phosphine claim 1 , pyrrole claim 1 , thiol claim 1 , thioether/sulfide claim 1 , disulfide claim 1 , sulfonyl claim 1 , sulfonyl claim 1 , carbonothioyl claim 1 , sulfino claim 1 , sulfo claim 1 , thiocyanate claim 1 , isothiocyanate claim 1 , oxazole claim 1 , oxadiazole claim 1 , imidazole claim 1 , triazole claim 1 , tetrazole claim 1 , amine claim 1 , amide claim 1 , azide claim 1 , azo claim 1 , cyano claim 1 , isocyanate claim 1 , imide claim 1 , nitrile claim 1 , isonitrile claim 1 , nitro claim 1 , nitroso claim 1 , nitromethyl claim 1 , selenol claim 1 , guanidino claim 1 , and substituted guanidino.4. The compound according to where Vis CRR claim 3 , C(R) claim 3 , or C(R) claim 3 , and any one of R claim 3 , R claim 3 , or Rtogether with Rform a lactam or lactone.5. ...

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Номер записи: 34
29-08-2013 дата публикации

ANALGESIC COMPOUNDS, METHODS, AND FORMULATIONS

Номер: US20130225679A1
Автор: CHEN Shuhui, Defauw Jean Marie, HOLMSTROM Scott Dale, Lu Lun, Ma Yujuan, PENG Xian, Wu Wentao, Zhang Yang
Принадлежит: ELI LILLY AND COMPANY

Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided. 128-. (canceled)32. The compound of wherein it is 2-dimethylaminomethyl-3-(3-methoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(3-fluoro-5-methoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(5-methoxy-2-trifluoromethoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(2-fluoro-5-methoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(4-fluoro-3-methoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(2-fluoro-3-methoxy-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(3-methoxy-5-methyl-phenyl)-bicyclo[3.2.1]octan-3-ol; 3-(2-chloro-5-methoxy-phenyl)-2-dimethylaminomethyl-bicyclo[3.2.1]octan-3-ol; 3-(3-chloro-5-methoxy-phenyl)-2-dimethylaminomethyl-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(5-methoxy-2-methyl-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(3-methoxy-4-methyl-phenyl)-bicyclo[3.2.1]octan-3-ol; 2-dimethylaminomethyl-3-(3-hydroxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(2-fluoro-5-hydroxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(3-fluoro-5-hydroxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(3-hydroxy-5-trifluoromethyl-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(5-hydroxy-2-trifluoromethoxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(3-hydroxy-4-trifluoromethyl-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(4-fluoro-3-hydroxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(2-fluoro-3-hydroxy-phenyl)-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(3-hydroxy-5-methyl-phenyl)-bicyclo[3.2.1]octan-3-ol;3-(2-chloro-5-hydroxy-phenyl)-2-dimethylaminomethyl-bicyclo[3.2.1]octan-3-ol;3-(3-chloro-5-hydroxy-phenyl)-2-dimethylaminomethyl-bicyclo[3.2.1]octan-3-ol;2-dimethylaminomethyl-3-(5- ...

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Номер записи: 35
12-09-2013 дата публикации

LEVALBUTEROL SALT

Номер: US20130236515A1
Автор: BAKALE Roger, MCGLYNN Paul, STURGE Craig
Принадлежит: Sunovion Pharmaceuticals Inc.

Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler. 117-. (canceled)18. An aerosol formulation adapted for administration using a metered dose inhaler , the formulation comprising crystalline levalbuterol L-tartrate and a propellant , wherein the formulation is configured to provide reproducible doses of levalbuterol L-tartrate when delivered using a metered dose inhaler.19. The aerosol formulation of claim 18 , wherein the crystalline levalbuterol L-tartrate is resistant to agglomeration.20. The aerosol formulation of claim 18 , wherein the crystalline levalbuterol L-tartrate has favorable aerodynamic properties.21. The aerosol formulation of claim 20 , wherein the crystalline levalbuterol L-tartrate is in the form of needle-like particles.22. The aerosol formulation of claim 18 , wherein the crystalline levalbuterol L-tartrate is stable in the presence of aerosol formulation components.23. The aerosol formulation of claim 22 , wherein the aerosol formulation components comprise ethanol.24. An aerosol formulation of claim 18 , wherein the crystalline levalbuterol tartrate is in the form of particles having an aerodynamic diameter of from 1 to 10 microns.25. An aerosol formulation of claim 24 , wherein the crystalline levalbuterol tartrate is in the form of particles having an aerodynamic diameter of from 1 to 5 microns.26. An aerosol formulation of claim 18 , wherein the crystalline levalbuterol tartrate does not substantially change in size or morphology under varying conditions of temperature and relative humidity during storage of up to six months. This application claims the benefit of U.S. provisional patent application No. 60/432,195 filed on Dec. 10, 2002, the disclosure of which is incorporated by reference herein.Levalbuterol (also known as (R)-albuterol) is a beta agonist useful as a relaxant of smooth muscle tissue, for example in the treatment of bronchospasm in patients suffering from asthma or ...

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Номер записи: 36
12-09-2013 дата публикации

AMINES HAVING SECONDARY ALIPHATIC AMINO GROUPS

Номер: US20130237681A1
Автор: BURCKHARDT Urs
Принадлежит: SIKA TECHNOLOGY AG

The present invention relates to novel amides having secondary amino groups, a process for preparing them, adducts of these amines and their uses. The amides can be prepared in a simple way from readily available starting materials. They and their adducts have, in particular, a low viscosity and are suitable as constituent of polyurethane and polyurea compositions having excellent processability and high flexibility, and also as constituent of epoxy resin compositions, in particular coatings. 2. The amine of formula (I) according to claim 1 , wherein Rand Reach stand for a methyl radical and/or Rstands for a hydrogen atom.3. The amine of formula (I) according to claim 1 , wherein Rstands for a hydrogen atom or for a hydrocarbon radical with 1 to 12 carbon atoms claim 1 , optionally containing an ether oxygen.4. The amine of formula (I) according to claim 1 , wherein Rstands for a hydrogen atom or a linear or branched alkyl radical with 1 to 11 carbon atoms claim 1 , optionally with cyclic fractions and optionally with at least one heteroatom or for a mono- or polyunsaturated linear or branched hydrocarbon radical with 5 to 11 carbon atoms or for an optionally substituted aromatic or heteroaromatic six-membered ring.5. The amine of formula (I) according to claim 1 , wherein Xstands for a phenyl claim 1 , biphenyl or naphthyl radical claim 1 , where this radical is optionally substituted claim 1 , with linear or branched alkyl radicals with 1 to 6 carbon atoms claim 1 , with alkoxy groups with 1 to 6 carbon atoms claim 1 , with ester groups with 1 to 6 carbon atoms or with nitrilo groups.7. The method of synthesis of an amine of formula (I) according to claim 6 , wherein the process is carried out in such a way that at one amine PA of formula (II) is condensed with at least one aldehyde ALD of formula (III) to form an aldimine which is then hydrogenated.8. The method according to claim 6 , wherein the amine PA of formula (II) is selected from the group consisting of 1 ...

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Номер записи: 37
19-09-2013 дата публикации

HCl Polymorphs of 3-((2-(Dimethylamino)methyl(cyclohex-1-yl))phenol

Номер: US20130245125A1
Автор: Berghausen Joerg, De PAUL Susan Margaret, Fischer Andreas, GRUSS Michael, Hell Wolfgang, KEGEL Markus, VON RAUMER Markus
Принадлежит: GRUENENTHAL GmbH

A crystalline salt of 3-[2-(dimethylamino)methyl(cyclohex-1-yl)] phenol and hydrogen chloride, preferably in a 1:1 composition, including various crystalline forms of this salt, processes for preparing the various crystalline forms of this salt, pharmaceutical compositions containing the various crystalline forms of this salt, and the use of this salt as a pharmacologically active agent in a pharmaceutical composition to treat or inhibit pain or other disorders or disease states. 1. A crystalline salt of hydrogen chloride and 3-[2-(dimethylamino)methyl-(cyclohex-1-yl)]phenol.3. A crystalline salt according to claim 1 , wherein said salt is in the form of a diastereomer or a mixture of enantiomeric diastereomers wherein the phenol ring and the dimethylaminomethyl group are in a trans configuration.4. A crystalline salt according to claim 3 , wherein said salt is in the form of an enantiomer with a (1R claim 3 ,2R) absolute configuration.5. A crystalline salt according to claim 1 , wherein said salt exhibits a characteristic X-ray diffraction pattern within the range from 2° to 35° 2θ with characteristic lines corresponding to the following 2theta values: 11.2 (w) claim 1 , 14.1 (m) claim 1 , 17.1 (w) claim 1 , 19.5 (w) claim 1 , 19.8 (vs) claim 1 , 20.5 (w) claim 1 , 21.5 (m) claim 1 , 24.1 (m) claim 1 , 26.1 (s) claim 1 , 26.8 (w) claim 1 , and 31.3 (m).6. A crystalline salt according to claim 1 , which exhibits the X-ray diffraction pattern of .7. A crystalline salt according to claim 1 , which exhibits the Raman spectrum of .8. A crystalline salt according to claim 1 , wherein said salt is crystalline form III and exhibits a characteristic X-ray diffraction pattern within the range from 2° to 35° 2θ with pronounced characteristic lines corresponding to the following 2theta values: 6.9 (s) claim 1 , 13.9 (m) claim 1 , 16.3 (m) claim 1 , 17.7 (w) claim 1 , 20.9 (vs) claim 1 , 22.1 (w) claim 1 , 22.5 (w) claim 1 , and 27.8 (w).9. A crystalline salt according to claim ...

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Номер записи: 38
19-09-2013 дата публикации

SPHINGOSINE KINASE TYPE 1 INHIBITORS

Номер: US20130245321A1
Автор: Adams Jeffrey Kroll, Spiegel Sarah, Zipkin Robert Elliot
Принадлежит:

Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM). 1104-. (canceled)106. The compound of claim 105 , wherein Ris OH.107. The compound of claim 105 , wherein Ris H.108. The compound of claim 105 , wherein Ris —NH—CH claim 105 , —NH—CO—CH claim 105 , —NH—CHCH claim 105 , or —N(CH).109. The compound of claim 105 , wherein Ris in the para position.110. The compound of claim 105 , wherein Ris —(CH)—CHor —O—(CH)—CH.111. The compound of claim 105 , wherein Ris OH.112. The compound of claim 105 , wherein Ris H.121. The compound of claim 120 , wherein R is 3 claim 120 ,4-dimethoxy.122. The compound of claim 120 , wherein R is 4-phenyl.123. The compound of claim 120 , wherein R is 3-pentyl.124. The compound of claim 105 , wherein the compound inhibits sphingosine kinase 1 greater than sphingosine kinase 2. This application is a divisional of U.S. patent application Ser. No. 12/584,131, filed Aug. 31, 2009, which is a continuation-in-part of U.S. patent application Ser. No. 12/387,228, filed Apr. 29, 2009, which claims the benefit of Provisional Application No. 61/048,638, filed Apr. 29, 2008, the contents of all of which are hereby incorporated by reference in their entirety.The invention generally relates to the field of compositions, including sphingosine analogs and inhibitors which are useful for sphingolipids mediation, regulation and inhibition. This invention also concerns compounds which preferentially inhibit or regulate sphingokinase kinase Type 1 (SphK1). These compounds are useful in a number of indications or disease conditions, including treatments for cancer, asthma, anaphylaxis, autophagy, central nervous system, including glioblastoma multiforme and others.All patents, patent applications, patent publications, ...

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Номер записи: 39
26-09-2013 дата публикации

STYRENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Номер: US20130253064A1
Автор: Gage Jennifer, Gall Anna, Jiang Qin, JR. Kevin F., JR. Thomas L., Kubota Ryo, Kuksa Vladimir Aleksandrovich, Little, McGee, Orme Mark W., Rossiter Lana Michele, Scott Ian Leslie
Принадлежит:

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 184.-. (canceled)86. The method of claim 85 , wherein Rand Rare each independently hydrogen claim 85 , halogen claim 85 , alkyl or —OR; and Rand Rare each independently hydrogen claim 85 , halogen claim 85 , alkyl or —OR claim 85 , wherein each Ris independently selected from hydrogen or alkyl.87. The method of claim 85 , wherein:t is 2 or 3;{'sup': '20', 'two adjacent R, together with the two carbon atoms to which they are attached, form a fused phenyl ring; and'}{'sup': 3', '4', '5', '6, 'R, R, Rand Rare each independently hydrogen, alkyl, halogen or fluoroalkyl.'}88. The method of claim 87 , wherein Rand Rare each independently hydrogen claim 87 , halogen claim 87 , alkyl or —OR; and Rand Rare each independently hydrogen claim 87 , halogen claim 87 , alkyl or —OR.90. The method of wherein each of Rand Ris hydrogen.91. The method of wherein:p is 0, 1, 2 or 3; and{'sup': '21', 'each Ris independently alkyl, halogen or fluoroalkyl.'}92. The method of claim 91 , wherein Rand Rare each independently hydrogen claim 91 , halogen claim 91 , alkyl claim 91 , fluoroalkyl claim 91 , —ORor —NRR; and Rand Rare each independently hydrogen claim 91 , halogen claim 91 , alkyl claim 91 , fluoroalkyl claim 91 , or —OR claim 91 , wherein each Ris independently hydrogen or alkyl; and{'sup': 18', '19, 'each Rand Rare independently hydrogen or alkyl.'}93. The method of wherein Ris alkyl and Ris hydrogen.94. The method of claim 93 , wherein Rand Rare each independently hydrogen claim 93 , halogen claim 93 , alkyl ...

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Номер записи: 40
03-10-2013 дата публикации

RADIOFLUORINATED COMPOUNDS AND THEIR PREPARATION

Номер: US20130259802A1
Автор: ARSTAD ERIK, GLASER MATTHIAS EBERHARD
Принадлежит: HAMMERSMITH IMANET LIMITED

The present invention provides a process for [F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [F]-labelled prosthetic groups. [F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided. 126-. (canceled)29. A method of wherein the diagnostic device is a Positron Emission Tomography scanner.37. Radiofluorination kit of further comprising a compound of formula (8):{'br': None, 'sup': '2', 'sub': '2', 'RNH\u2003\u2003(8)'}{'sup': '2', 'wherein Rdenotes a bio-molecule residue having at least one free amino function.'} The present invention relates to processes and reagents for [F]-fluorination, particularly of peptides. The resultant [F]-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).Compounds labelled with short-lived positron emitting radionuclides are used for in vivo studies of human and non-human physiology. In particular, radiolabelled bioactive compounds which selectively interact with specific cell types are useful for the delivery of radioactivity to target tissues. The applications of bioactive compounds such as peptides and proteins, including antibodies and fragments of peptides are useful for receptor imaging. For example, radiolabelled peptides have significant potential for the delivery of radionuclides to the receptors expressed on cells of tissues, e.g. in tumours, infarcts and infected tissues for diagnosis, radiotherapy and monitoring of treatment. PET is a high resolution, non-invasive, imaging technique which has gained increased importance in the recent years for the visualisation of human disease.In PET, F is one of the most widely used ...

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Номер записи: 41
24-10-2013 дата публикации

Highly Selective 5-HT(2C) Receptor Agonists That Show Anti-Psychotic Effects with Antagonist Activity at the 5-HT(2B) Receptor

Номер: US20130281539A1
Автор: Cho Sung Jin, Kozikowski Alan, Roth Bryan, Svennebring Andreas
Принадлежит:

Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)14. The composition of wherein the second therapeutic agent comprises a therapeutic agent useful in a treatment of a psychiatric disorder claim 13 , a metabolic disorder claim 13 , or an eating disorder.15. (canceled)17. The method of wherein the 5-HT(2C) receptors are activated.18. (canceled)19. (canceled)20. (canceled)21. The method of wherein the disease or condition is selected from the diseases and conditions disclosed in paragraphs [0100] through [0102].22. The method of wherein the disease or condition is a central nervous system disorder or a damage to the central nervous system.23. The method of wherein the central nervous system disorder is anxiety claim 22 , a panic disorder claim 22 , a schizoaffective disorder claim 22 , schizophrenia claim 22 , psychosis claim 22 , an adjustment disorder claim 22 , dystonia claim 22 , clinical depression claim 22 , bipolar disorder claim 22 , an addictive behavior claim 22 , a compound addiction claim 22 , obsessive compulsive disorder claim 22 , a movement disorder claim 22 , or a cognition disorder.24. The method of wherein the disease or condition is a metabolic or eating disorder selected from the group consisting of dyslipidemia claim 16 , Type 2 diabetes claim 16 , diabetes insipidus claim 16 , metabolic syndrome claim 16 , and obesity.25. (canceled)26. The method of wherein the disease or condition is a gastrointestinal disorder claim 16 , sleep apnea claim 16 , hypertension claim 16 , hyperlipidemia claim 16 , a cardiovascular disease claim 16 , dementia claim 16 , memory deficit claim 16 , mild ...

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Номер записи: 42
24-10-2013 дата публикации

BENZYLAMINE HYDROPHOBE

Номер: US20130281617A1
Автор: Bobsein Barrett R., Rabasco John J.
Принадлежит:

The present invention relates to a compound characterized by the following formula: 3. The compound of wherein Ris n-butyl or 2-ethylhexyl.7. The method of wherein Ris n-butyl or 2-ethylhexyl; m is 0; and p is 1. The present invention idea relates to an amine-based hydrophobe useful in preparing hydrophobically modified alkylene oxide urethane polymers, which are useful as rheology modifiers for coatings formulations.Rheology modifiers are typically designed to impart desirable rheological properties to coating formulations over a wide shear rate range. U.S. Pat. No. 7,741,402 discloses ethylene oxide urethane polymers modified with hydrophobes that contain organic bases such as secondary or tertiary amines (amine-modified HEURs), the presence of which provides for viscosity control through a pH trigger. When the pH of the HEUR composition is sufficiently low with respect to the pKof the incorporated base, the basic groups are protonated and the viscosity is relatively low; when the pH is sufficiently high, associative thickening occurs. Thus, incorporation of basic hydrophobes into the HEUR polymer allows relatively high concentration of polymer to be dissolved in water at low pH; once the solution is added to the high pH environment of paint coatings, the base is deprotonated and the associative thickening mechanism activated.Amine-modified HEURs can be sensitive to the pH of the paint formulation to which it is added. For example, the pH of the formulation, through time and heat aging, may decrease to a level below a critical pH conducive to associative thickening, thereby resulting in a poorer formulation; consequently, it would be desirable to discover a hydrophobe, more particularly an amine-based hydrophobe, that preserves the desired viscosity of the formulation in face of pH-lowering mechanisms.The present invention addresses a need by providing, in one aspect, a compound characterized by the following formula:where Ris C-C-alkyl, phenyl, naphthyl, C-C- ...

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Номер записи: 43
24-10-2013 дата публикации

FINGOLIMOD POLYMORPHS AND THEIR PROCESSES

Номер: US20130281739A1
Автор: N/A Veereshappa, Purohit Prashant, Shrawat Vimal Kumar, Singh Vinod Kumar
Принадлежит:

The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof. 1. Fingolimod hydrochloride crystalline Form-α characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2θ° peaks selected from the XRPD peak set of 10.51 , 15.20 , 19.27 , 21.77 , 23.12 , 24.91 , 26.14 , 26.46 , 29.03 , 33.47 and 35.46±0.1 2θ°.21. Fingolimod hydrochloride crystalline Form-α according to claim- , which is further characterized by DSC isotherm comprising at least three endothermic peaks ranging between—a. Peak-1—Between 40 to 43° C.b. Peak-2—Between 65 to 68° C.c. Peak-3—Between 105 to 110° C.d. Peak-4—Between 270 to 280° C.3. Fingolimod hydrochloride crystalline Form-α characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2θ° peaks selected from the XRPD peak set of 10.51 , 15.20 , 19.27 , 21.77 , 23.12 , 24.91 , 26.14 , 26.46 , 29.03 , 33.47 and 35.46±0.1 2θ° and DSC isotherm comprising the endothermic peaks ranging between 40 to 43° C. (Peak-1) , 65 to 68° C. (Peak-2) , 105 to 110° C. (Peak-3) and/or 270 to 280° C. (Peak-4).43. Fingolimod hydrochloride crystalline Form-α according to claim- , characterized by X-ray powder diffraction pattern substantially according to and DSC isothermal pattern substantially according to .5. A process for preparing Fingolimod hydrochloride crystalline Form-α comprising the steps of—a. Combining the Fingolimod hydrochloride with an organic acidb. Optionally heating up to about 40-50° C.c. cooling the solution up to about 0-5° C.d. isolating the crystalline Form-α.6. A process for preparing Fingolimod hydrochloride crystalline Form-α according to claim 5 , wherein organic acid may be selected from C1 to C4 carboxylic acids.7. Fingolimod hydrochloride crystalline Form-β characterized by X-ray powder diffraction pattern comprising at least 4 characteristic 2θ° peaks selected from the XRPD peak set of 3.54 claim 5 , 7.07 claim 5 , 10.66 ...

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Номер записи: 44
05-12-2013 дата публикации

Quaternized Polyethulenimines with a High Ethoxylation Degree

Номер: US20130324451A1
Автор: Delplancke Patrick, Di Capua Gloria, Dobrawa Rainer, Ebert Sophia, Evers Marc, Huelskoetter Frank, SCIALLA Stefano
Принадлежит: BASF SE

The present invention relates to an ethoxylated polyethylenimine polymer comprising (1) a polyethyleneimine backbone, (2) a polyoxyethylene chain wherein the polyoxyethylene chain has an average of 40 to 90 ethyleneoxide units per unit of NH in the polyethyleneimine backbone, (3) a quaternization degree of from 1% to less than 50%. 16-. (canceled)8. The ethoxylated polyethyleneimine according to claim 7 , wherein n has a value which lies in the range of from 45 to 80.9. The ethoxylated polyethyleneimine according to claim 7 , wherein n has a value which lies in the range of from 50 to 80.10. The ethoxylated polyethyleneimine according to claim 7 , wherein the polyethyleneimine backbone has a weight average molecular weight of from 400 to 10000 g/mol.11. The ethoxylated polyalkylenimine polymer according to claim 7 , wherein the polyethyleneimine backbone has a weight average molecular weight of from 400 to 6000 g/mol.12. Use of the ethoxylated polyalkylenimine polymer according to in chemical technical applications claim 7 , car wash claim 7 , cosmetics claim 7 , paper and cardboard manufacturing claim 7 , leather and textile industry. The present invention relates to an ethoxylated polyethylenimine polymer comprising (1) a polyethyleneimine backbone, (2) an ethoxylation modification consisting of the replacement of a hydrogen atom by a polyoxyethylene chain having an average of 40 to 90 ethoxy units per unit of NH in the polyethyleneimine backbone, (3) a quaternization degree of the nitrogen atoms present in the polyethyleneimine backbone which lies in the range of from 1% to less than 50%.Surface cleaning with liquid detergents poses an ongoing problem for consumers. Consumers utilizing liquid detergents as a light-duty liquid dishwashing detergent composition or as a hard surface cleaning composition frequently find surface imperfections such as soil residues, streaks, film and/or spots after washing. Besides, consumers prefer cleaning compositions to be dried ...

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Номер записи: 45
05-12-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF CHIRAL PROPARGYLIC ALCOHOLS

Номер: US20130324763A1
Автор: Brenner Meinrad, Carreira Erick M., Chinkov Nicka, Lorenzi Miriam, Warm Aleksander, Zimmermann Lothar
Принадлежит: LONZA LTD

A process for the synthesis of chiral propargylic alcohols. 2. The process of claim 1 , wherein the protic chiral auxiliary is selected from the group consisting of N claim 1 ,N-disubstituted ephedrine derivatives.3. The process of claim 1 , wherein the molar ratio of the protic chiral auxiliary to the diorganylzinc(II) compound is in the range of 1.5:1 to 1:1.4. The process of claim 1 , wherein the diorganylzinc(II) compound is selected from the group consisting of di(C-alkyl) and di(C-cycloalkyl) claim 1 , wherein the alkyl moieties are selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , isobutyl claim 1 , sec-butyl and tert-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , heptyl claim 1 , and octyl claim 1 , and wherein the cycloalkyl moieties are selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl and cyclohexyl.5. The process of claim 1 , wherein in step (i) the molar ratio of the protic chiral auxiliary to the compound of formula III is in the range of 1:1 to 1:10 claim 1 , preferably in the range of 1:2 to 1:6 claim 1 , more preferably of 1:3 to 1:6.6. The process of claim 1 , wherein in step (iii) the compound of formula II is used in a molar ratio to the compound of formula III of 1:0.6 to 1:1.3.7. The process of claim 1 , wherein the organolithium base and/or the other alkali metal organyl is added in a molar ratio to the compound of formula III from 1:0.8 to 1:1.5.8. The process of claim 1 , wherein the organolithium base is selected from the group consisting of (C-alkyl)lithium claim 1 , lithium diisopropylamide (LDA) claim 1 , lithium hexamethyldisilazide (LiHMDS) claim 1 , phenyllithium claim 1 , and naphthyllithium.9. The process of claim 8 , wherein the (C-alkyl)lithium is selected from the group consisting of methyllithium claim 8 , n-butyllithium claim 8 , sec-butyllithium claim 8 , tert-butyllithium claim 8 , and hexyllithium.10. The ...

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Номер записи: 46
19-12-2013 дата публикации

Process for the Synthesis of Aminobiphenylene

Номер: US20130338369A1
Автор: Heinrich Markus, Pratsch Gerald
Принадлежит: BASF SE

The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions. 127-. (canceled)31. The process of claim 28 , wherein the reaction is performed at a pH of 9.1 or greater32. The process of claim 28 , wherein the reaction is performed in the presence of at least one solvent.33. The process of claim 32 , wherein the solvent is an aqueous solvent.34. The process of claim 28 , wherein the reaction is performed in the presence of water and of at least one base.35. The process of claim 34 , wherein the base is selected from the group consisting of alkali metal hydroxides claim 34 , alkaline earth metal hydroxides claim 34 , alkali metal carbonates and alkali metal phosphates claim 34 , and is preferably sodium hydroxide or potassium hydroxide.36. The process of claim 28 , wherein the reaction is performed within the temperature range from 50 to 130° C.37. The process of claim 28 , wherein the compound of the formula 1 or the compound of the formula 2 or both compounds 1 and 2 are used in the reaction dispersed in an alkaline medium.38. The process of claim 37 , wherein the pH of the alkaline medium is at least 9.1.39. The process of claim 28 , wherein claim 28 , in a first step claim 28 , a compound of the formula 1 is reacted with a base in aqueous medium and claim 28 , in a second step claim 28 , the dispersion obtained is added to the compound of the formula 2.40. The process of claim 39 , wherein the pH of the dispersion obtained is at least 9.1.41. The process of claim 39 , wherein the compound 2 claim 39 , prior to addition of the dispersion claim 39 , is brought to a temperature of 50 to 130° C.42. The process of claim 28 , wherein the compound of the formula 2 is initially charged in an alkaline medium and the compound of the formula 1 is added.43. The process of claim 42 , wherein the compound of the formula 2 is initially ...

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Номер записи: 47
09-01-2014 дата публикации

Crystalline Forms of (-)-(1R, 2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride

Номер: US20140011886A1
Автор: BUSCHMANN Helmut, Fischer Andreas, GRUSS Michael, LISCHKE Dagmar
Принадлежит: GRUENENTHAL GmbH

A hitherto unknown crystalline form of (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence. 1. A process for producing a (−)-(1R ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A , said process comprising:dissolving a (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B in acetone, acetonitrile or isopropanol to form a solution;leaving the solution to crystallize andisolating crystals of (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A.2. The process of claim 1 , wherein said (−)-(1R claim 1 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of Form B is dissolved in acetonitrile claim 1 , and further comprising the steps of:stirring the solution;removing insoluble residue by filtering andevaporating the acetonitrile leaving (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of Form A to crystallize.3. The process according to claim 1 , wherein said (−)-(1R claim 1 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B is dissolved in isopropanol at temperatures above room temperature claim 1 , and after complete dissolution no further heat is provided and further comprising:adding seed crystals of (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A and then cooling the mixture down to ≦15° C.4. The process of claim 3 , wherein said (−)-(1R claim 3 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B is dissolved in isopropanol at a temperature above 65° C. but not exceeding 80° C.5. The process of claim 3 , wherein said mixture is cooled down to ≦10 ...

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Номер записи: 48
09-01-2014 дата публикации

4-PYRIDINONE COMPOUNDS AND THEIR USE FOR CANCER

Номер: US20140012007A1
Автор: Borzilleri Robert M., CAI Zhen-Wei, Gallagher William P., Livingston Robert C.
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed. 18-. (canceled)12. The compound according to claim 9 , or a salt thereof claim 9 , wherein:{'sub': '2', 'X is NO.'}15. The compound according to claim 9 , or a salt thereof claim 9 , wherein:{'sub': '2', 'X is NH.'} The present invention generally relates to processes for preparing pyridinone compounds.Met, also referred to as hepatocyte growth factor receptor (HGFR), is expressed predominantly in epithelial cells but has also been identified in endothelial cells, myoblasts, hematopoietic cells, and motor neurons. Overexpression of hepatocyte growth factor and activation of Met has been associated with the onset and progression in a number of different tumor types as well as in the promotion of metastatic disease.U.S. Patent Application Publication 2008/0114033 A1 discloses a pyridinone compound useful for treating Met-related cancers. The disclosed pyridinone compound, which comprises an amide linkage and an amine substituted pyridyl group, has the structure of Formula (Ia):The reference also discloses a multistep synthesis process for preparing the pyridinone compound. This process includes the reaction between an aniline compound and a carboxylic acid compound to form the amide linkage in the compound of Formula (Ia). The disclosed process also includes a Hofmann Rearrangement reaction to convert an amide substituent to an amine group, to provide the amine substituted pyridyl group in the structure of Formula (Ia). ...

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Номер записи: 49
09-01-2014 дата публикации

METHOD FOR PRODUCING CYCLIC SILANE COMPOUND OR SALT THEREOF, SALT HAVING CYCLIC SILANE DIANION, AND CYCLIC SILANE DIANION SALT-CONTAINING COMPOSITION

Номер: US20140012030A1
Автор: Abe Takashi, IMOTO Shin-ya, KITAMURA Morihiro, Takahashi Hikaru
Принадлежит:

An object of the present invention is to provide a production method that can efficiently produce a cyclic silane compound or a salt thereof with a high yield and to provide a novel salt having a cyclic silane dianion that is easy to handle and a cyclic silane dianion salt-containing composition. The method for producing a cyclic silane compound or a salt thereof of the present invention includes the step of allowing a halosilane compound to react in the presence of at least one of a phosphonium salt and an ammonium salt, and a compound represented by a specific formula. 2. The method for producing a cyclic silane compound or a salt thereof according to claim 1 , wherein the reaction is carried out in the presence of a basic compound.3. The method for producing a cyclic silane compound or a salt thereof according to claim 1 , wherein the phosphonium salt or the ammonium salt is a quaternary phosphonium salt or a quaternary ammonium salt.7. The cyclic silane dianion salt-containing composition according to claim 6 , wherein the salt having a cyclic silane dianion represented by the general formula (vii) is contained in an amount of 1 to 10000 parts by mass claim 6 , based on the total amount of 100 parts by mass of the salt having a cyclic silane dianion represented by the general formula (vi).8. The method for producing a cyclic silane compound or a salt thereof according to claim 2 , wherein the phosphonium salt or the ammonium salt is a quaternary phosphonium salt or a quaternary ammonium salt. (1) Field of the InventionThe present invention relates to a production method that can efficiently obtain a cyclic silane compound or a salt thereof by a simple method, a novel salt having a cyclic silane dianion, and a cyclic silane dianion salt-containing composition.(2) Description of Related ArtA silane compound is widely utilized as a raw material of silicon and silica, and a water-reactive combustible gas such as monosilane and disilane is mostly used. On the other ...

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Номер записи: 50
16-01-2014 дата публикации

Solid dosage formulations of narcotic drugs having improved buccal adsorption

Номер: US20140018392A1
Автор: Federico Stroppolo, Shahbaz Ardalan
Принадлежит: ALPEX PHARMA SA

Disclosed is a pharmaceutical composition in the form of a tablet suitable for dissolution in the buccal cavity, said composition comprising i) an effective amount of a narcotic active ingredient, and ii) a pharmaceutically acceptable amine having a pK of about 8 or greater, wherein the molar ratio of amine:active ingredient is at least about 5:1.

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Номер записи: 51
30-01-2014 дата публикации

Diamino alcohol and strong base neutralizers for low voc coating compositions

Номер: US20140031470A1
Автор: Anurima Singh, Asghar Peera, Esin Busche, Ian A. Tomlinson, John Quinn, Raymond Swedo
Принадлежит: Angus Chemical Co, Dow Global Technologies LLC

A coating composition comprising a binder, a carrier, a pigment, cations selected from the group consisting of alkali metal cations, ammonium cations, and mixtures thereof, and at least one diamino alcohol selected from the group consisting of compounds of Formula I and compounds of Formula II. The present invention also provides a method for reducing the volatile organic compound (VOC) content of a coating composition having a binder, a carrier, and a pigment, which comprises including in the coating composition the aforesaid A) cations and B) at least one diamino alcohol. The diamino alcohol may be of Formula I: wherein R 1 and R 2 are independently C 1 -C 10 alkyl, or R 1 and R 2 , together with the carbon to which they are attached, form a C 3 -C 12 cycloalkyl ring optionally substituted with C 1 -C 6 alkyl. For example, the compound of Formula I may be 2-(2-amino-2-methylpropylamino)-2-(hydroxymethyl)propane-1,3-diol. Alternatively, the diamino alcohol may be of Formula II: or salt thereof, wherein R 1 and R 2 are independently at each occurrence C 1 -C 6 alkyl; and R 3 is independently at each occurrence H or C 1 -C 6 alkyl. For example, the compound of Formula II may be 2,2′-((2-hydroxytrimethylene)diimino)bis(2-methyl-1-propanol).

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Номер записи: 52
06-02-2014 дата публикации

Analgesic method

Номер: US20140039040A1
Автор: Ping-Heng TAN
Принадлежит: I-SHOU UNIVERSITY

An analgesic medication includes an oligonucleotide being a double strand RNA comprising 18 to 70 base pairs, and a pharmaceutical acceptable vehicle for delivering the said oligonucleotide into cells, wherein a dosage of the oligonucleotide in the analgesic is 50 μg to 200 μg/kg per time, and the pharmaceutical acceptable vehicle is selected from a group of polyethyleneimine, lipofectamine and iFect.

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Номер записи: 53
06-02-2014 дата публикации

BROMFENAC ORGANIC SALTS AND PREPARATION METHOD, COMPOSITION AND USE THEREOF

Номер: US20140039056A1
Автор: Liu Jidong, Tang Hai, Wang Jiuliang, Yang Yuchun
Принадлежит: SHENYANG XINGQI PHARMACEUTICAL CO., LTD.

Provided are bromfenac organic salts and preparation method, composition and use thereof. The bromfenac organic salt has the structure as shown in the following Formula I, wherein A represents an organic base. Also provided are a method for the preparation of the bromfenac organic salt, a composition comprising the bromfenac organic salts, a use of the bromfenac organic salts or the composition thereof in manufacture of a medicament for treatment and/or prophylaxis of an inflammation or for analgesia, and a method for treatment and/or prophylaxis of an inflammation or for analgesia. 3. A method for preparing the bromfenac organic salt according to claim 1 , comprising the steps:1) dissolving bromfenac in an organic solvent, heating to dissolve, then adding an organic base in equimolar amount, stirring until the end of reaction;2) concentrating and evaporating the reaction solution to dry to obtain a light yellow or orange yellow solid; and3) recrystallizing the solid obtained in step 2) to obtain the bromfenac organic salt.4. The method according to claim 3 , wherein said organic solvent in step 1) is one or more selected from the group consisting of methanol claim 3 , ethanol claim 3 , acetone claim 3 , n-butanol and toluene; and said organic base is a nitrogen-containing organic base.5. The method according to claim 3 , wherein the temperature of heating in step 1) is 25-80° C.6. The method according to claim 3 , wherein the time for stirring and reacting in step 1) is 0.5-2 hours.7. The method according to claim 3 , wherein the recrystallization in step 3) is performed at 0° C. or below.8. The method according to claim 3 , further comprising step 4): vacuum drying the crystal obtained by recrystallizing.9. A composition claim 1 , comprising the bromfenac organic salt according to .10. (canceled)11. A method for treatment and/or prophylaxis of an inflammation or for analgesia claim 1 , comprising a step of administering an effective amount of the bromfenac organic ...

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Номер записи: 54
13-02-2014 дата публикации

Substituted n-pentanamide compounds, preparation method and the use thereof

Номер: US20140046074A1
Автор: JIANG Xiangrui, Li Jianfeng, Shen Jingshan, TIAN Guanghui, ZHANG QIANG, ZHANG Rongxia, ZHU Fuqiang
Принадлежит:

The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process. 2. The (2R claim 1 ,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compound according to claim 1 , wherein R and the phenolic hydroxyl group form an ether group or an ester group; wherein R is selected from C1-C6 linear or branched alkyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted arylalkyl claim 1 , alkylsilyl claim 1 , C1-C6 alkoxymethyl claim 1 , C1-C6 alkyloyl claim 1 , substituted or unsubstituted aryloyl; wherein the substituent is hydroxy claim 1 , halogen claim 1 , C1-C6 alkyl or C1-C6 alkoxy; said aryl is phenyl or naphthyl;wherein X is O; and Y is O;{'sub': '1', 'wherein Ris C1-C6 alkyl group, substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, wherein the substituent on phenyl or benzyl is 1 to 3 substituent(s) selected from hydroxy, halogen, C1-C6 alkyl and C1-C6 alkoxy;'}{'sub': 2', '3, 'wherein Rand Rare each independently selected from H, C1-C6 alkyl and phenyl.'}3. The (2R claim 2 ,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compound according to claim 2 ,wherein R is benzyl, methyl, t-butyl, triphenylmethyl, methoxymethyl, trimethylsilyl, t-butyldimethylsilyl, acetyl or benzoyl;wherein X is O; and Y is O;{'sub': '1', 'wherein Ris phenyl; phenyl substituted with 1 to 3 substituent(s) selected from hydroxy, halogen, C1-C6 alkyl and C1-C6 alkoxy; benzyl;'}{'sub': 2', '3, 'wherein Rand Rare each independently selected from H, C1-C6 alkyl and phenyl.'}6. The method according to claim 5 , wherein claim 5 ,said hydrocarbylation agent is any one of methyl ...

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Номер записи: 55
06-03-2014 дата публикации

CYCLOHEXANE COMPOUNDS AND THEIR USE AS ANTIBIOTICS

Номер: US20140066409A1
Автор: Luense Christina Elsbeth, Mayer Günter, Schmidt Magnus S., Wittmann Valentin
Принадлежит:

The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic. 3. The compound according to claim 1 , wherein R claim 1 , Rand Rare OH.4. The compound according to claim 1 , wherein Ris selected from the group comprising hydrogen claim 1 , C-C-alkyl preferably methyl claim 1 , ethyl or n-propyl claim 1 , benzyl claim 1 , C-C-acyl preferably C(O)CH claim 1 , C(O)CH claim 1 , C(O)n-propyl or C(O)iso-propyl claim 1 , C(O)NH claim 1 , NHand/or S(O)OH.5. The compound according to claim 1 , wherein Ris selected from the group comprising hydrogen claim 1 , P(O)(OH)and/or aryloxy phosphoramidates according to general formula (II) wherein Ris methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , cyclohexyl or benzyl claim 1 , X is methoxy and Ris methyl claim 1 , preferably Ris P(O)(OH).7. The compound according to claim 1 , wherein the compound according to general formula (I) is part of a dimer claim 1 , trimer or oligomer claim 1 , formed from one compound according to any one of the foregoing claims and at least one other compound joined together via a linker linked to element A claim 1 , preferably a linker selected from the group comprising nucleotide linkers claim 1 , polyethylene glycols claim 1 , peptide linkers and/or linear or branched claim 1 , saturated or unsaturated C-C-alkyl. The present invention relates to cyclohexane compounds according to general formula (I) and pharmaceutical compositions comprising compounds according to general formula (I). In particular, the present invention relates to the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic.Since the discovery of antibiotic substances and their use against microbes, bacteria have evolved to defend themselves by acquiring resistances. Especially in ...

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Номер записи: 56
06-03-2014 дата публикации

Novel Method

Номер: US20140066516A1
Автор: Geoffrey Douglas Clarke, Ian Burnett, Timothy James Grattan
Принадлежит: GlaxoSmithKline LLC

The present invention is directed to a novel method for reducing intrapatient variability in pharmaceutically active agent which is suitably not absorbed in the stomach, such as paracetamol, containing formulations in patients having gastric dysmotility, or a method of improving analgesia in a diabetic patient, or improving absorption of an active agent is a patient with gastric dysmotility, which methods comprises administering orally to said patient in need thereof a pharmaceutical dosage form comprising a first active agent, calcium carbonate, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, a super disintegrant, and a second active agent.

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Номер записи: 57
13-03-2014 дата публикации

ONO PINCER LIGANDS AND ONO PINCER LIGAND COMPRISING METAL COMPLEXES

Номер: US20140073800A1
Автор: "OREILLY MATTHEW", JAN MUHAMMAD TARIQ, VEIGE ADAM STEVEN
Принадлежит: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.

Embodiments of the invention are directed to ONO pincer ligands that can be in a trianionic, protonated or protonated equivalent form. The ONO pincer ligand can be combined with a transition metal comprising compound to form an ONO pincer ligand comprising transition metal complex. By choice of the ONO pincer ligand structure, the steric and electronic properties of the transition metal complexes therefrom can be controlled. The ONO pincer ligands comprise a central nitrogen atom that is disubstituted with a pair of three atom comprising bridges where the three atoms are three sphybridized carbons or the three atoms are a pair of sphybridized carbons and an sphybridized carbon or silicon. 5. A method of preparing an ONO pincer ligand precursor according to claim 1 , comprising condensing a nucleophilic oxygen or nucleophilic nitrogen comprising compound with an electrophilic carbon comprising compound further comprising the bridge structure of the resulting ONO pincer ligand.6. A trianionic ONO pincer ligand comprising transition metal complex comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one ONO trianionic pincer ligand derived from the ONO trianionic pincer ligand precursor of ; and'}a transition metal from group III through group X of the periodic table.7. The trianionic ONO pincer ligand comprising transition metal complex of claim 6 , wherein the transition metal is an early transition metal complex from group III through group VI.18. The method of preparing an ONO pincer ligand comprising transition metal complex of claim 17 , wherein the precursor metal compound further comprises a metal alkylidyne claim 17 , further comprising adding the OH or NH of the ONO pincer ligand precursor across the metal alkylidyne to form the anionic ONO pincer ligand comprising metal complex. This application is a continuation-in-part of International Patent Application No. PCT/US2012/037302, filed May 10, 2012, which claims the benefit of U.S. ...

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Номер записи: 58
13-03-2014 дата публикации

PREPARATION METHOD FOR RIVASTIGMINE, INTERMEDIATES THEREOF, AND PREPARATION METHOD FOR SAID INTERMEDIATES

Номер: US20140073809A1
Автор: Bai Hua, Chen Daoxin, Sun Rentong, Yang Chunbo, YANG Zhezhou, YANG Zhiqing, ZHANG Fuli
Принадлежит:

The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N—((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production. 113-. (canceled)21. The method according to anyone of and , wherein demethylation is performed in the presence of hydrobromic acid , aluminum chloride or concentrated sulfuric acid.2220. The method according to anyone of the - claim 17 ,wherein the methylation agents are selected from the group consisting of methyl fluoride, methyl chloride, methyl bromide, methyl iodide, dimethyl sulfate, dimethyl carbonate, methyltrifluoromethane sulfonate, and fluorine acid methyl ester;wherein the methylation is performed between 0° C.-100° C.;wherein methylation uses an inert solvent as a reaction solvent in which the inert solvent is selected from the group consisting of an ether solvent, an aromatic hydrocarbon solvent, a halogenated hydrocarbon solvent, an alcohol solvent, an amide solvent, acetonitrile, and acetone;wherein the ether solvent is selected from the group consisting of tetrahydrofuran, diethyl ether, ethylene glycol dimethyl ether, dioxane, and 2-methyltetrahydrofuran;wherein the aromatic hydrocarbon solvent is selected from the group consisting of benzene, toluene, and ...

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Номер записи: 59
13-03-2014 дата публикации

AMINODIHYDROTHIAZINE DERIVATIVES SUBSTITUTED WITH A CYCLIC GROUP

Номер: US20140073815A1
Автор: FUJIKOSHI Chiaki, Kooriyama Yuuji, Matsumoto Sae, Suzuki Shinji, Tada Yukio, TAMURA Yuusuki, UENO Tatsuhiko, YONEZAWA Shuji
Принадлежит: Shionogi & Co., Ltd.

This invention provides a compound of the formula (I): 114-. (canceled)16. The compound of wherein ring A is substituted phenyl or optionally substituted pyridine claim 15 , or a salt thereof. This application is a Continuation of application Ser. No. 13/417,786, filed Mar. 12, 2012, which is a Divisional of application Ser. No. 12/596,796, filed Dec. 3, 2009, which is a National Stage Application of PCT/JP2008/057847, filed Apr. 23, 2008, which applications are incorporated herein by reference.This invention relates to a compound having an inhibitory activity against production of amyloid β protein and useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.In the brain of Alzheimer's patient many insoluble spots (senile plaque) are found, which is formed by extraneuronal accumulation of a peptide called amyloid β protein comprised of about 40 amino acids. Neuronal death caused by the senile plaque is considered to develop Alzheimer's Disease and an enhancer of amyloid β protein decomposition or vaccine of amyloid β protein etc. are extensively studied as a remedy for Alzheimer's Disease.Secretase is an enzyme producing amyloid β protein by intracellular cleavage of a protein called amyloid β protein precursor(APP). An enzyme playing a role for producing an N-terminal of the amyloid β protein is called BACE1 (beta-site APP-cleaving enzyme) and an inhibitor of the BACE1, which will reduce production of amyloid β protein, could be a remedy for treating Alzheimers disease.Patent literature 1 discloses a compound with a chemical structure similar to that of the compound of the present invention, having an inhibitory activity of NO synthetase and effective for treating dementia.Patent literature 2-5 and non-patent literature 1-2 disclose compounds with a chemical structure similar to those of the compound of the present invention, and describe that each compound is useful as an anti-hypotensive agent, morphine-like analgesic ...

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Номер записи: 60
03-04-2014 дата публикации

Process

Номер: US20140094625A1
Автор: Sedelmeier Gottfried
Принадлежит: NOVARTIS AG

The present invention relates to improved processes for the production of 2-amino-2-[2-(4-Calkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein. 7. A process according to claim 1 , wherein Ris n-hexyl.12. The process of claim 2 , which is performed on a continuous flow. The present invention relates to processes for the production of 2-amino-2-[2-(4-C-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.2-Amino-2-[2-(4-C-alkyl-phenyl)ethyl]propane-1,3-diols are disclosed in EP-A-1627406 the relevant disclosure of which is incorporated herein by reference. On the basis of observed activity, the compounds have been found to be useful as immunosuppressants. Accordingly, the compounds may be useful in the treatment or prevention of acute allograft rejection, autoimmune diseases or xenograft rejection. A particular compound of this type is FTY720, i.e. 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol, which has the following structure:FTY720 has been found to be useful in the prevention of autoimmune diseases, such as multiple sclerosis. FTY720 is the first-in-class sphingosine 1-phosphate (SIP) receptor modulator which has been effective in clinical trials for Multiple Sclerosis.WO 00/27798 discloses various processes for the preparation of 2-amino-2-[2-(4-C-alkyl-phenyl)ethyl]propane-1,3-diols. Some of these processes are illustrated in the reaction scheme below in relation to the production of FTY720, using the reference numerals given in the publication:The above processes involve formation of intermediate 18 via acylation of compound 16. However, the acylation process results in a mixture of ortho-, meta- and para-substituted products. None all these products have biological activity. There is a need for a processes for producing 2-amino-2-[2-(4-C-alkyl-phenyl)ethyl]propane-1,3-diols, in particular FTY720 and salts thereof, which have improved regioselectivity for the para-position of the benzene ring.Furthermore the above ...

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Номер записи: 61
04-01-2018 дата публикации

POLYMORPHIC AND AMORPHOUS FORMS OF (R)-2-HYDROXY-2-METHYL-4-(2,4,5-TRIMETHYL-3,6-DIOXOCYCLOHEXA-1,4-DIENYL)BUTANAMIDE

Номер: US20180000749A1
Автор: CORNELL Christopher R., GIANNOUSIS Peter, MIRMEHRABI Mahmoud, MOLLARD Paul, SUCHIT Shazad, WESSON Kieron E.
Принадлежит:

Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms. 1. An polymorph of an anhydrate , a hydrate , or a solvate of (R)-2-hydroxy-2-methyl-4-(2 ,4 ,5-trimethyl-3 ,6-dioxocyclohexa-1 ,4-dienyl)butanamide , wherein the polymorph is selected from the group consisting of Forms I-VI as described in Table A or Tables 2-7 respectively.2. The polymorph of claim 1 , wherein the polymorph is Form I claim 1 , wherein a powder X-ray diffraction pattern for the polymorph comprises characteristic peaks at the following angular positions claim 1 , wherein the angular positions may vary by ±0.2: 12.06 claim 1 , 17.03 claim 1 , and 17.26.3. The polymorph of claim 1 , wherein the polymorph is Form I claim 1 , wherein a powder X-ray diffraction pattern for the polymorph comprises characteristic peaks at the following angular positions claim 1 , wherein the angular positions may vary by ±0.2: 12.06 claim 1 , 15.33 claim 1 , 17.03 claim 1 , 17.26 claim 1 , and 18.72.4. The polymorph of claim 1 , wherein the polymorph is Form I claim 1 , wherein the polymorph has a powder x-ray diffraction pattern substantially as shown in .5. A composition comprising the polymorph of any one of - claim 1 , wherein the composition is essentially free of Forms II-VI claim 1 , wherein Forms II-VI are described in Table A or Tables 3-7 respectively.6. A composition comprising the polymorph of any one of - claim 1 , wherein at least about 95% by mole of the composition is the polymorph Form I claim 1 , exclusive of any solvents claim 1 , carriers or excipients.7. The polymorph of claim 1 , wherein ...

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Номер записи: 62
06-01-2022 дата публикации

CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF

Номер: US20220002310A1
Автор: Ebel Heiner, Frattini Sara, GERLACH Kai, GIOVANNINI Riccardo, HOENKE Christoph, Mazzaferro Rocco, SANTAGOSTINO Marco, Scheuerer Stefan, Tautermann Christofer, Trieselmann Thomas
Принадлежит:

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 2. The method of claim 1 , wherein Li is —NH—.3. The method of claim 2 , wherein Ris —C-C-heterocyclyl substituted by one or more groups selected from among halogen claim 2 , —CF claim 2 , —OCF claim 2 , —CN claim 2 , —OH claim 2 , —O—C-C-alkyl claim 2 , and —C-C-alkyl.4. The method of claim 3 , wherein Ris phenyl optionally substituted with one or more groups selected from among —CF claim 3 , —O—CF claim 3 , —CN claim 3 , —C-C-alkyl claim 3 ,—C(CH)—CN claim 3 , and halogen.5. The method of claim 4 , wherein Ris —H claim 4 , and Ris —C-C-alkyl.6. The method of claim 5 , wherein Ris —H.8. The method of claim 1 , wherein the neurologic disease is inflammatory pain.9. The method of claim 4 , wherein the neurologic disease is inflammatory pain.10. The method of claim 7 , wherein the neurologic disease is inflammatory pain.11. The method of claim 1 , wherein the neurologic disease is neuropathic pain.12. The method of claim 4 , wherein the neurologic disease is neuropathic pain.13. The method of claim 7 , wherein the neurologic disease is neuropathic pain.14. The method of claim 11 , wherein the neuropathic pain is low back pain claim 11 , hip pain claim 11 , leg pain claim 11 , non-herpetic neuralgia claim 11 , post herpetic neuralgia claim 11 , diabetic neuropathy claim 11 , nerve injury-induced pain claim 11 , phantom limb pain claim 11 , post-surgical pain claim 11 , stump pain claim 11 , or trigeminal neuralgia.15. The method of claim 1 , wherein the neurologic disease is neuropathic pain due to chemotherapy caused nerve injury.16. The method of claim 13 , wherein the neuropathic pain is leg pain.17. The method of claim 13 , wherein the neuropathic pain is nerve injury-induced pain.18. The method of claim 13 , wherein the neuropathic pain is hip pain ...

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Номер записи: 63
07-01-2021 дата публикации

Compositions And Methods For Prophylaxis Or Treatment Of Pain

Номер: US20210000912A1
Автор: Agrez Michael Valentine
Принадлежит:

There are described methods for the prophylaxis or treatment of pain in a mammal wherein the method comprising administering to the mammal an effective amount of a pain inhibitor comprising a pain inhibiting peptide having an amino acid sequence of more than 6 contiguous arginine residues, or a physiologically acceptable salt of the peptide. The pain inhibitor can be administered in combination with at least one analgesic and/or at least one anti-inflammatory drug. Pharmaceutical compositions comprising the pain inhibitor together with at least one analgesic and/or at least one anti-inflammatory drug are also provided. The pain may, for example, be selected from one or more of neuropathic pain, inflammatory pain, idiopathic pain and nociceptive pain. 1. A method for prophylaxis or treatment of pain in a mammal , the method comprising administering to the mammal an effective amount of a pain inhibitor comprising a pain inhibiting peptide having an amino acid sequence of more than 6 contiguous arginine residues , or a physiologically acceptable salt of the peptide.2. The method according to claim 1 , wherein the peptide comprises at least 9 contiguous arginine residues.3. The method according to claim 1 , wherein the peptide comprises at least 12 contiguous arginine residues.4. The method according to claim 1 , wherein the peptide comprises 14 or more contiguous arginine residues.5. The method according to claim 4 , wherein the peptide comprises 14 contiguous arginine amino acids.6. The method according to any one of to claim 4 , wherein the peptide is C-terminal protected.7. The method according to claim 6 , wherein the peptide is amidated at its C-terminal end.8. The method according to any one of to claim 6 , wherein the peptide is an inhibitor of the activity of PKG1α.9. The method according to claim 8 , wherein the peptide is an inhibitor of PKG1α and PKG1β.10. The method according to any one of to claim 8 , wherein the peptide is an inhibitor of c-Src.11. The ...

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Номер записи: 64
04-01-2018 дата публикации

Injectable formulations of paracetamol

Номер: US20180000940A1
Автор: Asheel K. PATEL, Ketan R. Patel, Milan R. Patel, Prakashchandra J. Shah
Принадлежит: Troikaa Pharmaceuticals Ltd

The present invention relates to low volume intravenous injections of paracetamol or its pharmaceutically acceptable salt and method of preparation thereof. The formulations provide high concentration of paracetamol or its pharmaceutically acceptable salt in a solvent system of the present invention which can be administered not only through intra-muscular & intravenous infusion route but also suitable for slow IV bolus administration after dilution with aqueous fluids to final volume of not more than 20 ml. These injectable formulations remain stable and are also suitable for administration through slow intravenous route with minimized side effects (such as phlebitis, pain etc.).

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Номер записи: 65
07-01-2021 дата публикации

PROCESSES FOR REGENERATION OF ORGANOCATIONS

Номер: US20210002153A1
Автор: Gonen Yotam, Rauch Amos, Sade Rotem, Shifton Ohad
Принадлежит:

The present disclosure concerns processes for regenerating organocations from perchlorate-rich waste products, more specifically transformation of water-insoluble organocation-perchlorate salt, originating from perchlorate-removal water treatment processes, into a water-soluble perchlorate salt for reusing same. 1. A process for recovering a water-soluble organocation salt from a substantially water-insoluble organocation-perchlorate , the process comprising:(a) contacting said substantially water-insoluble organocation-perchlorate with a first solution containing a first salt dissolved in an organic solvent, the first salt consisting of a metal cation and a balancing anion, under conditions permitting precipitation of metal-perchlorate salt and formation of a second salt dissolved in said organic solvent, the second salt consisting of the organocation and the balancing anion;(b) separating the metal-perchlorate salt from the organic solvent in which the second salt is dissolved; and(c) separating the organic solvent from the second salt to obtain said second salt,said second salt being a water-soluble organocation salt.2. The process of claim 1 , wherein the separating in step (c) is carried out by evaporation of the organic solvent.3. (canceled)4. The process of claim 2 , wherein step (c) further includes condensing vapors of the organic solvent formed during evaporation or distillation to obtain a condensate of organic solvent.5. (canceled)6. The process of claim 1 , wherein said separating in step (b) is carried out by sedimentation claim 1 , decantation claim 1 , filtration claim 1 , flotation or a combination thereof.7. The process of claim 1 , wherein metal-perchlorate salt separated in step (b) is further treated to remove the organic solvent from the metal-perchlorate salt.8. The process of claim 7 , wherein the organic solvent is removed from the metal-perchlorate salt by evaporating.9. The process of claim 8 , wherein the organic solvent removed from the ...

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Номер записи: 66
07-01-2016 дата публикации

NUCLEOSIDE ANALOG SALTS WITH IMPROVED SOLUBILITY AND METHODS OF FORMING SAME

Номер: US20160002240A1
Автор: Rogers Robin D.
Принадлежит:

Disclosed are salts of nucleoside analogs and methods of forming the salts. An anion of a nucleoside analog is paired with a permanent counter cation to form a salt that has decreased melting point and increased aqueous solubility compared to the nucleoside compound prior to the salt formation. Also a cation of a nucleoside analog is paired with a permanent counter anion to form a salt that has decreased melting point and increased aqueous solubility compared to the nucleoside compound prior to the salt formation. The nucleoside analog in some embodiments has therapeutic activity such as antiviral. The permanent counter cation or anion in some embodiments has bioactivity such as antibacterial or being a vitamin. 1. A salt , comprising: at least one kind of anion that is anion of a nucleoside analog and at least one kind of cation that is a permanent counter cation , or at least one kind of cation that is a cation of a nucleoside analog and at least one kind of anion that is a permanent counter anion , wherein the aqueous solubility of the salt is greater than the aqueous solubility of the nucleoside analog.2. The salt of claim 1 , wherein the nucleoside analog comprises an ionizable purine or pyrimidine base.3. The salt of claim 1 , wherein the nucleoside analog comprises a guanosine analog antiviral drug.4. The salt of claim 3 , wherein the guanosine analog antiviral drug comprises acyclovir or a pharmaceutically effective salt thereof.5. The salt of claim 1 , wherein the cation is an aprotic cation including quaternary nitrogen or a phosphorous or sulfur-containing analog thereof.6. The salt of claim 1 , wherein the cation is an ammonium cation of the structure NRRRR claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from substituted or unsubstituted Calkyl claim 1 , substituted or unsubstituted Calkenyl claim 1 , substituted or unsubstituted Calkynyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or ...

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Номер записи: 67
04-01-2018 дата публикации

SOLID FORMS OF DESVENLAFAXINE

Номер: US20180002273A1
Автор: Domínguez Chávez Jorge Guillermo, HERNÁNDEZ ILLESCAS Javier, Herrera Ruiz Dea, Höpfl Herbert, MONDRAGÓN VÁSQUEZ Karina, Morales Rojas Hugo, REYES MARTINEZ Reyna, Senosiain Peláez Juan Pablo
Принадлежит:

The present invention refers to new amorphous and crystalline solid forms of desvenlafaxine, also known as O-desmethylvenlafaxine or desmethylvenlafaxine, and to its salts, solvates, hydrates and polymorphs thereof, as well as to their use in the manufacture of a pharmaceutical composition useful in the treatment of depression and/or as a selective serotonin and norepinephrine reuptake inhibitor and also in menopause-associated vasomotor disorders. 1. A crystalline or amorphous solid compound formed by the selective serotonin and noradrenaline reuptake inhibitor desvenlafaxine (or DSV) and a co-former X , wherein X comprises one or more hydroxyl groups and a carboxyl group , wherein desvenlafaxine and X form the solid compound through ionic interactions or non-covalent intermolecular forces; or any solvate , hydrate or polymorph of the solid compound.2. The solid compound of claim 1 , wherein X is selected from the group consisting of 2-hydroxybenzoic acid claim 1 , 3-hydroxibenzoic acid claim 1 , 4-hydroxybenzoic acid claim 1 , 2 claim 1 ,3-dihydroxybenzoic acid claim 1 , 2 claim 1 ,4-dihydroxybenzoic acid claim 1 , 2 claim 1 ,5-dihydroxybenzoic acid claim 1 , 2 claim 1 ,6-dihydroxybenzoic acid claim 1 , 3 claim 1 ,4-dihydroxybenzoic acid claim 1 , 3 claim 1 ,5-dihydroxybenzoic acid claim 1 , 3 claim 1 ,4 claim 1 ,5-trihydroxybenzoic acid; or any solvate claim 1 , hydrate or polymorph of the solid compound.3. The solid compound of claim 1 , wherein the solid compound is amorphous and wherein X is selected from the group consisting of 2-hydroxybenzoic acid claim 1 , 3-hydroxibenzoic acid claim 1 , 4-hydroxybenzoic acid claim 1 , 2 claim 1 ,3-dihydroxybenzoic acid claim 1 , 2 claim 1 ,4-dihydroxybenzoic acid claim 1 , 2 claim 1 ,5-dihydroxybenzoic acid claim 1 , 2 claim 1 ,6-dihydroxybenzoic acid claim 1 , 3 claim 1 ,4-dihydroxybenzoic acid claim 1 , 3 claim 1 ,5-dihydroxybenzoic acid claim 1 , 3 claim 1 ,4 claim 1 ,5-trihydroxybenzoic acid; or any solvate claim 1 , ...

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Номер записи: 68
03-01-2019 дата публикации

IMPROVED METHOD FOR SYNTHESISING PARTIALLY N-HYDROXYETHYLATED TERTIARY 1,6-HEXANEDIAMINES

Номер: US20190002392A1
Автор: Delfort Bruno, Grandjean Julien
Принадлежит: IFP ENERGIES NOUVELLES

The invention relates to a synthesis method for at least one nitrogen compound belonging to the family of partly N-hydroxyethylated tertiary 1,6-hexanediamines with general formula (I) as follows: 3) A method as claimed in claim 1 , wherein the first precursor compound is 1 claim 1 ,6-hexanediamine and the second precursor compound 2 PET-3256 is ethylene oxide claim 1 , said method comprising:a first reaction step between the 1,6-hexanediamine and the ethylene oxide so as to form at least one intermediate compound selected from the list including N-(2-hydroxyethyl)-1,6-hexanediamine, N,N′-di(2-hydroxyethyl)-1,6-hexanediamine, N,N-di(2-hydroxyethyl)-1,6-hexanediamine and N,N,N′-tri(2-hydroxyethyl)-1,6-hexane-diamine;a second step of methylation of the primary or secondary amine functions of said at least one intermediate compound so as to form at least one compound according to general formula (I).4) A method as claimed in claim 3 , wherein the second methylation step is carried out by reaction between said intermediate compound claim 3 , formaldehyde and hydrogen in the presence of a hydrogenation catalyst claim 3 , or by reaction between said intermediate compound claim 3 , formaldehyde and formic acid according to the Eschweiler-Clarke reaction.5) A method as claimed in claim 3 , wherein the residual 1 claim 3 ,6-hexanediamine that has not reacted at the end of the first reaction step is recycled to said first reaction step claim 3 , after separation by distillation of said 1 claim 3 ,6-hexanediamine from said at least one intermediate compound.6) A method as claimed in claim 3 , wherein the molar ratio of ethylene oxide to 1 claim 3 ,6-hexanediamine is less than or equal to 3/1 claim 3 , and preferably less than or equal to 2.5/1.7) A method as claimed in claim 3 , further comprising claim 3 , at the end of the first reaction step claim 3 , at least one separation step claim 3 , preferably by distillation claim 3 , of at least one intermediate compound so as to ...

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Номер записи: 69
07-01-2021 дата публикации

COMPOUND AND COLORED RESIN COMPOSITION

Номер: US20210002487A1
Автор: AKASAKA Tetsuo, Inoue Keisuke, KAWANISHI Yutaka
Принадлежит: Sumitomo Chemical Company, Limited

An object of the present invention is to provide a novel squarylium dye that can achieve an equivalent chromaticity value of even a colored resin composition having a low content of the squarylium dye as compared with a colored resin composition comprising a conventional squarylium dye. The present invention provides a compound represented by the formula (I) wherein Rto Reach independently represent a hydrogen atom or the like; Rto Reach independently represent a hydrogen atom or the like; Rand Reach independently represent a monovalent saturated hydrocarbon group having 1 to 20 carbon atoms or the like; Rand Reach independently represent a halogen atom or an alkyl halide group having 1 to 6 carbon atoms; and m1 and m2 each independently represent an integer of 1 to 5. 2. A colored resin composition comprising a colorant comprising a compound according to claim 1 , and a resin.3. A color filter formed from a colored resin composition according to .4. A solid-state imaging device comprising a color filter according to .6. A compound represented by the formula (IV-1) according to . The present invention relates to a novel compound and a colored resin composition.In colored curable resin compositions, it is known that squarylium dyes are used as colorants. Patent Literature 1 has proposed a squarylium dye represented by a specific general formula.Patent Literature 1: Japanese Patent Laid-Open No. 2015-86379An object of the present invention is to provide a novel squarylium dye that can achieve an equivalent chromaticity value of even a colored resin composition having a low content of the squarylium dye as compared with a colored resin composition comprising a conventional squarylium dye. Another object of the present invention is to provide a precursor of the novel squarylium dye and a method for producing the novel squarylium dye.The present invention provides the following [1] to [6]:[1] A compound represented by the formula (I):whereinRto Reach independently ...

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Номер записи: 70
14-01-2016 дата публикации

A PROCESS FOR THE PREPARATION OF 2-AMINO-1,3-PROPANE DIOL COMPOUNDS AND SALTS THEREOF

Номер: US20160009634A1
Автор: Aswathanarayanappa Chandrashekar, CHANDREGOWDA Dharshan Jakkali, Duvva Chandrasekhar, Kumar Kothakonda Kiran, PULLELA Venkata Srinivas
Принадлежит:

The present disclosure relates to processes for the preparation of 2-amino-1,3-propane diol compounds and their hydrochloride salts. Particularly, the present disclosure relates to processes for synthesizing 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol and its hydrochloride salt 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride respectively. The said process is safe, commercially feasible for large-scale synthesis and has improved efficacy along with many other advantages. The present disclosure also relates to the novel polymorphs of 2-amino-1,3-propane diol compound and its hydrochloride salt, where in 2-amino-1,3-propane diol compound is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol, and its hydrochloride salt is 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride. 2. The process as claimed in claim 1 , wherein the reaction of step (a) is carried out in presence of solvent selected from a group comprising toluene claim 1 , xylene claim 1 , heptanes claim 1 , hexanes claim 1 , diethyl ether claim 1 , methyl tertiary butyl ether and tetrahydrofuran or any combination thereof; and further comprises adding reagent selected from a group comprising alkaline metal carbonate and alkaline earth metal carbonate or a combination thereof.3. The process as claimed in claim 2 , wherein volume of the solvent ranges from about 1 to about 30 volumes; and wherein the alkaline metal carbonate and alkaline earth metal carbonate is selected from a group comprising lithium carbonate claim 2 , sodium carbonate claim 2 , potassium carbonate claim 2 , cesium carbonate claim 2 , magnesium carbonate claim 2 , calcium carbonate and barium carbonate.4. The process as claimed in claim 1 , wherein the step (a) is carried out at temperature ranging from about 10° C. to about 160° C. and for a time period ranging from about 3 hours to about 24 hours.5. The process as claimed in claim 1 , wherein the conversion of step (b) or step (c) or step (d) is carried ...

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Номер записи: 71
14-01-2016 дата публикации

PREPARATION OF (R,R)-FENOTEROL AND (R,R)-OR (R,S)-FENOTEROL ANALOGUES AND THEIR USE IN TREATING CONGESTIVE HEART FAILURE

Номер: US20160009636A9
Автор: Abernethy Darrell R., Beigi Abhari Farideh M., Chakir Khalid, Wainer Irving William, Xiao Rui-Ping, Zhu Weizhong
Принадлежит: The USA, as represented by the Secretary, Department of Health and Human Services

This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding β2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease. 3. The compound of claim 2 , wherein Ris selected from methyl claim 2 , ethyl claim 2 , n-propyl claim 2 , and isopropyl.4. The compound of claim 3 , wherein Ris methyl.6. The compound of claim 5 , wherein Ris methyl.7. The compound of claim 6 , wherein the compound is a (R claim 6 ,R′)-compound.8. The compound of claim 1 , wherein the compound is a (R claim 1 ,S′)-compound.9. A pharmaceutical composition comprising the compound of and at least one pharmaceutically acceptable carrier.10. A method for treating a pulmonary or cardiovascular disorder in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'administering a therapeutically effective amount of the compound of to the subject with the pulmonary or cardiovascular disorder.'}11. A method for treating a pulmonary or cardiovascular disorder in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'administering a therapeutically effective amount of the pharmaceutical composition of to the subject with the pulmonary or cardiovascular disorder.'}13. The method of claim 12 , wherein the compound is a (R claim 12 ,R′)-compound.14. The method of claim 12 , wherein the compound is a (R claim 12 ,S′)-compound.15. The method of claim 12 , wherein the disorder is a cardiovascular disorder.16. The method of claim 15 , wherein the cardiovascular disorder is congestive heart failure.17. The method of claim 12 , wherein the disorder is a pulmonary disorder. ...

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Номер записи: 72
09-01-2020 дата публикации

Method of Inhibiting Chronification of Pain

Номер: US20200009083A1
Автор: HAMON Michel, JAHNEL Ulrich, REINARTZ Silvia, SCHIENE Klaus, Schneider Johannes, STEIGERWALD Ilona, TZSCHENTKE Thomas
Принадлежит: Grünenthal GmbH

The use of tapentadol in the treatment of pain and/or pain chronification in a subject suffering from pain chronification and/or in the treatment of pain and inhibition of pain chronification in a subject suffering from pain and at risk of pain chronification, as well as the use of tapentadol for the treatment or inhibition of migraine. 1. A method of treating pain in a subject suffering from pain chronification or for inhibiting pain chronification in a subject suffering from pain and at risk for pain chronification , said method comprising administering to said subject an effective pain alleviating or pain chronification inhibiting amount of tapentadol.2. A method as recited in claim 1 , wherein said subject is a subject suffering from pain and at risk of pain chronification claim 1 , and the tapentadol is administered in an effective pain alleviating and pain chronification inhibiting amount.3. A method as recited in claim 1 , wherein said subject is a subject suffering from pain and pain chronification claim 1 , and the tapentadol is administered in an effective pain alleviating and pain chronification treating amount.4. A method as recited in claim 1 , wherein said subject is a subject suffering from pain claim 1 , and the tapentadol is administered in an effective pain alleviating amount.5. A method as recited in claim 1 , wherein said subject is a subject suffering from central pain.6. A method as recited in claim 1 , wherein said subject is a subject suffering from peripheral pain.7. A method as recited in claim 1 , wherein said subject is a subject suffering from acute pain.8. A method as recited in claim 7 , wherein said acute pain is selected from the group consisting of mechanical pain claim 7 , heat pain claim 7 , cold pain claim 7 , ischemic pain claim 7 , and chemical-induced pain.9. A method as recited in claim 1 , wherein said subject is a subject suffering from pain selected from the group consisting of postoperative pain claim 1 , inflammatory ...

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Номер записи: 73
27-01-2022 дата публикации

PROCESS FOR MANUFACTURING ETHYLENEAMINE COMPOUNDS

Номер: US20220024852A1
Автор: EDVINSSON Rolf Krister, EHLERS Ina, JOVIC Slavisa, KANTZER Eike Nicolas, LAKE Karl Fredrik, RAAIJMAKERS Michiel Jozef Thomas, TEN KATE Antoon Jacob Berend, VAN DAM Hendrik, VENEMAN Rens, ZUBEIR Lawien Feisal
Принадлежит: NOURYON CHEMICALS INTERNATIONAL B.V.

The present disclosure pertains to a process for manufacturing ethyleneamine compounds selected from the group of ethyleneamines and hydroxyethylethyleneamines wherein the process comprises two reaction sequences. 1. Process for manufacturing ethyleneamine compounds selected from the group of ethyleneamines and hydroxyethylethyleneamines wherein the process comprises a first and a second reaction sequences , in an adduction step, providing a CO2 adduct of a starting compound comprising a —NH—CH2-CH2-NH— moiety or a —NH—CH2-CH2-OH moiety, or HO—CH2-CH2-OH,', 'in a chain-extension step reacting a hydroxy-functional compound selected from ethanolamines and dihydroxyethane with an ethyleneamine compound, wherein at least part of a total of hydroxy-functional compounds and the ethyleneamine compound is provided in the form of a CO2 adduct, to form a CO2 adduct of a chain-extended ethyleneamine compound,', 'in an elimination step converting the CO2 adduct of the chain-extended ethyleneamine compound to the corresponding product ethyleneamine compound by removal of the carbonyl group, and, 'the first reaction sequence comprising the steps of in a ethylenedichloride reaction step reacting ethylenedichloride with at least one compound selected from the group of ammonia, an ethyleneamine and/or an ethanolamine to form a hydrochloride salt of the ethyleneamine and/or the ethanolamine,', 'in a caustic treatment step reacting a hydrochloride salt of the ethyleneamine or ethanolamine with a base to form an ethyleneamine compound and an inorganic chloride salt,', 'in a salt separation step separating the inorganic chloride salt from the ethyleneamine compound,, 'the second reaction sequence comprising the steps of effluent from a step in the first reaction sequence is provided as a starting material to a step in the second reaction sequence,', 'effluent from a step in the second reaction sequence is provided as a starting material to a step in the first reaction sequence,', 'a ...

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Номер записи: 74
14-01-2021 дата публикации

METHODS FOR PRODUCING (6S,15S)-3,8,13,18-TETRAAZAICOSANE-6,15-DIOL

Номер: US20210009504A1
Автор: Bharathkumar Padavalachandu, PATIL Rahul, Rai U Sankappa, Shanker P. Sathya, Vengatesan Selvam, Venghatraghavan Murali
Принадлежит:

The present invention provides methods of synthesizing (6S,15S)-3,8,13,18-tetraazaicosane-6,15-diol and salts thereof. 2. The method of claim 1 , wherein PG is benzyl or substituted benzyl.3. The method of claim 2 , wherein PG is benzyl claim 2 , 4-methoxybenzyl or 3 claim 2 ,4-dimethoxybenzyl.4. The method of claim 3 , wherein PG is benzyl.5. The method of claim 2 , wherein in step (e) claim 2 , the compound of Formula (VI) is deprotected by hydrogenolysis.6. The method of claim 4 , further comprising the step of reacting 1 claim 4 ,4-diaminobutane with benzaldehyde under reducing conditions claim 4 , thereby producing the compound of Formula (I).7. The method of claim 1 , wherein the reducing agent of step (b) is lithium aluminum hydride.8. The method of claim 1 , wherein the acetylating agent is acetic anhydride.9. The method of claim 1 , wherein the reducing agent of step (d) is lithium aluminum hydride.10. The method of claim 1 , wherein PG is benzyl; the reducing agent of step (b) and the reducing agent of step (d) are both lithium aluminum hydride; and the acetylating agent is acetic anhydride.11. The method of claim 1 , wherein step (a) is conducted in the presence of a base.12. The method of claim 11 , wherein the base is KCO claim 11 , NaHCOor diisopropylethylamine.13. The method of claim 11 , where step (a) is conducted in a polar organic solvent.14. The method of claim 13 , wherein the solvent is ethanol claim 13 , N claim 13 ,N-dimethylformamide claim 13 , or acetone.15. The method of claim 1 , wherein step (a) is conducted in an ethanol solution of sodium bicarbonate.16. The method of claim 1 , wherein the reducing agent in step (b) is lithium aluminum hydride or Raney nickel and ammonia.17. The method of claim 1 , wherein step (b) is conducted in tetrahydrofuran or methanolic ammonia. This application is a continuation of International Application No. PCT/US2019/015581, which designated the United States and was filed on Jan. 29, 2019, published in ...

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Номер записи: 75
14-01-2021 дата публикации

CATIONIC LIPIDS AND TRANSFECTION METHODS

Номер: US20210009505A1
Автор: Angel Matthew, KOSTAS Franklin, Rohde Christopher
Принадлежит:

The present invention relates in part to novel cationic lipids and their use, e.g., in delivering nucleic acids to cells. 2. The compound of claim 1 , wherein n is 2-15.3. The compound of claim 1 , wherein n is 2-12.12. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable carrier or excipient.13. A lipid aggregate comprising the compound of .14. The lipid aggregate of claim 13 , wherein the lipid aggregate does not comprise one or more additional lipids or polymers.15. The lipid aggregate of claim 13 , further comprising a nucleic acid claim 13 , selected from a DNA or RNA molecule. The present application claims priority to U.S. patent application Ser. No. 16/746,279, filed on Jan. 17, 2020, U.S. Provisional Application No. 62/870,245, filed on Jul. 3, 2019, U.S. Provisional Application No. 62/880,435, filed on Jul. 30, 2019, and U.S. Provisional Application No. 63/023,654, filed on May 12, 2020, the contents of which are herein incorporated by reference in their entireties.The present invention relates, in part, to various novel lipids, including methods, compositions, and products for delivering nucleic acids to cells.The instant application contains a Sequence Listing which has been submitted in ASCII format via EFS-Web and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Jul. 3, 2020, is named FAB-012US_ST25.txt and is 1,441,638 bytes in size.Lipid-based materials, such as liposomes, are used as biological carriers for pharmaceutical and other biological applications, e.g., to introduce agents into cultured cell lines. Lipids are commonly used to deliver nucleic acids to cells in vitro under low-serum or serum-free conditions, for instance in transfection. However, serum components inhibit the activity of many lipids, limiting their use in the presence of serum, both in vitro and in vivo. Improved lipid delivery systems, e.g., to achieve higher levels of transfection both in vitro and ...

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Номер записи: 76
10-01-2019 дата публикации

DEZOCINE ANALOGUE

Номер: US20190010114A1
Автор: CHEN Shuhui, FANG Yongbo, Gu Wei, Li Jian, Li Zhixiang, WANG FEI, Wu Wentao, Yang Guangwen, Zhang Tao, Zhang Yang
Принадлежит:

Disclosed in the present disclosure is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof. 2. The compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to claim 1 , wherein Ris selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , OH claim 1 , NH claim 1 , or the group consisting of Calkyl or heteroalkyl claim 1 , 3-5 membered cycloalkyl or heterocycloalkyl claim 1 , and 5-6 membered aryl or heteroaryl claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , or 3 R; and claim 1 , when X is CH claim 1 , Ris not H.5. The compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to claim 1 , wherein each of Rand Ris independently selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , OH claim 1 , NH claim 1 , or the group consisting of Calkyl or heteroalkyl claim 1 , 3-5 membered cycloalkyl or heterocycloalkyl and 5-6 membered aryl or heteroaryl claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , or 3 R.14. A method for treating pain in a subject in need thereof claim 1 , comprising: administering an effective amount of the compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to to the subject. This application is a National Stage of International Application No. PCT/CN2017/070126, filed on Jan. 4, 2017, and published in Chinese as WO2017/118375 A1 on Jul. 13, 2017. This application claims the priority to Chinese Patent Application No. 201610003868.6, filed on Jan. 4, 2016. The entire disclosures of the above applications are incorporated herein by reference.Disclosed in the present disclosure is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof. ...

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Номер записи: 77
14-01-2021 дата публикации

LINKER OF BIOPROBES

Номер: US20210011012A1
Автор: CHEN YU-CHE, LI CHING-WEN
Принадлежит:

A linker of bioprobes, suitable for immobilizing a bioprobe on a chip substrate of a sensor, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is greater than 250 nm, coverage of the linker on the chip substrate is 40%-80%. A further linker of bioprobes, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of less than 6, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is less than 250 nm, coverage of the linker on the chip substrate is 65%-100%. The optimal carbon chain length of the linker and the coverage are realized for substrates of various roughnesses, and grasping ability of an electrochemical sensor chip for a detected object are enhanced. 1. A linker of bioprobes , suitable for immobilizing a bioprobe on a chip substrate of a sensor , comprising:SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1,wherein when an average surface roughness (Ra) of the chip substrate is greater than 250 nm, a coverage of the linker on the chip substrate is in a range of 40% to 80%.2. The linker of bioprobes according to claim 1 , wherein a material of the chip substrate of the sensor is silicon claim 1 , glass claim 1 , graphene claim 1 , gold claim 1 , platinum or polymers.3. The linker of bioprobes according to claim 1 , wherein the chip substrate is subjected to surface treatment according to a proportion of 1 part of 98 wt % sulfuric acid and 3 parts of 33 wt % hydrogen peroxide claim 1 , and a specific roughness is obtained by different treatment time.4. The linker of bioprobes according to claim 1 , further comprising: soaking the chip substrate into a solution of a linker dissolved in 99.8 ...

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Номер записи: 78
03-02-2022 дата публикации

METHODS AND COMPOSITIONS FOR THE TREATMENT OF OPIOID DEPENDENCE AND FOR THE TREATMENT OF PAIN

Номер: US20220031798A1
Автор: Kuhn Cynthia, Patkar Ashwin
Принадлежит: Duke University

The present invention relates to methods of treating opioid dependence, enhancing the treatment of opioid dependence, treating opioid withdrawal, or alleviating one or more opioid withdrawal symptoms in a subject, preventing or reducing the likelihood of opioid dependence relapse in a subject treated for opioid dependence, reducing the vulnerability of a subject to develop opioid dependence in adulthood following opioid exposure during adolescence, or treating pain in a subject, comprising administering a therapeutically effective amount of a N-methyl-D-aspartate receptor (NMDA) partial agonist to the subject. The present invention further relates to compositions comprising an NMDA partial agonist for use with the aforementioned methods. 1. (canceled)2. (canceled)3. (canceled)4. A method of treating hyperalgesia in a subject , the method comprising: administering a therapeutically effective amount of a NMDA partial agonist to the subject.5. (canceled)6. (canceled)7. (canceled)8. A method of reducing the vulnerability of a subject to develop opioid dependence in adulthood following opioid exposure during adolescence , the method comprising: administering a therapeutically effective amount of a NMDA partial agonist to the subject.9. (canceled)10. The method according to wherein the NMDA partial agonist is rapastinel.11. The method according to wherein the subject is a human.12. The method according to wherein the human is an adolescent.13. A composition comprising an NMDA partial agonist and a pharmaceutically acceptable carrier.14. The composition of wherein the NMDA partial agonist is rapastinel.15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. The method according to claim 11 , wherein the human is an adult.28. The method according to claim 4 , wherein the subject has an opioid dependence.29. The method according to claim 4 , wherein the NMDA ...

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Номер записи: 79
21-01-2016 дата публикации

COMPOSITIONS COMPRISING BIOREVERSIBLE DERIVATIVES OF HYDROXY N- SUBSTITUTED-2-AMINOTETRALINS, DOSAGE FORMS, AND RELATED METHODS

Номер: US20160015684A1
Автор: Higuchi William I., Patel Firoozeh Aminian
Принадлежит:

Described are compositions that may be orally administered that comprise a bioreversible derivative of hydroxy N-substituted-2-aminotetralin or an enantiomer or salt or prodrug thereof, and a pharmaceutically acceptable carrier suitable for oral administration in the amount present, wherein the composition is orally bioavailable when administered to a subject. The bioreversible derivative has an intrinsic lipophilicity C log P value of about 7 to about 11.5. A method comprises oral administering such composition to a human subject in need of hydroxy N-substituted-2-aminotetralin therapy.

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Номер записи: 80
21-01-2016 дата публикации

NONIONIC SURFACTANT COMPOSITIONS

Номер: US20160016886A1
Автор: Elowe Paul R., Graf Irina V., Krasovskiy Arkady L., WANG Lin
Принадлежит:

The present invention provides nonionic surfactants, compositions incorporating these surfactants, and related methods of making and using such surfactants and compositions. The nonionic surfactants demonstrate excellent equilibrium and dynamic surface tension properties as well as excellent wetting properties. Further, representative embodiments of the surfactants have shown low foaming characteristics, indicating that the surfactants would be suitable in applications where resistance to foaming is desired. The surfactants can be used singly or in combination with other nonionic and/or ionic surfactants as desired. As an over view, the nonionic surfactants of the present invention have a structure in which the surfactant backbone includes one or more amine moieties. At least one, preferably two or more branched, cyclic, fused cyclic, and/or spyro hydrophobic moieties are pendant from at least one of the amine moieties. Additionally, at least one, preferably two or more hydrophilic moieties, preferably alkylene oxide (i.e., polyether) chains also are pendant from at least one of the amine moieties. 1. A method of making a nonionic surfactant , comprising the steps of:a) providing an adduct comprising at least one secondary amine moiety and at least two branched, cyclic, fused cyclic, and/or spyro hydrophobic moieties; andb) N-functionalizing at least a portion of the secondary amine moieties of the adduct under conditions effective to convert at least a portion of the secondary amine moieties to tertiary amine moieties having pendant, hydrophilic, N-ether functionality.2. The method of claim 1 , wherein step (a) comprises reacting ingredients comprising first and second compounds under conditions effective to form the adduct claim 1 , wherein the first compound comprises one or more ketone and/or aldehyde moieties and the second compound comprises one or more primary amine moieties.3. The method of claim 2 , wherein the first compound comprises one or more of methyl ...

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Номер записи: 81
21-01-2016 дата публикации

Methods of treating a subject using bioreversible derivatives of hydroxy n-substituted-2-aminotetralins

Номер: US20160016887A1
Автор: Higuchi William I., Patel Firoozeh Aminian
Принадлежит:

Described are compositions that may be orally administered that comprise a bioreversible derivative of hydroxy N-substituted-2-aminotetralin or an enantiomer or salt or prodrug thereof, and a pharmaceutically acceptable carrier suitable for oral administration in the amount present, wherein the composition is orally bioavailable when administered to a subject. The bioreversible derivative has an intrinsic lipophilicity C log P value of about 7 to about 11.5. A method comprises oral administering such composition to a human subject in need of hydroxy N-substituted-2-aminotetralin therapy.

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Номер записи: 82
21-01-2021 дата публикации

POLYMORPHIC AND AMORPHOUS FORMS OF (R)-2-HYDROXY-2-METHYL-4-(2,4,5-TRIMETHYL-3,6-DIOXOCYCLOHEXA-1,4-DIENYL)BUTANAMIDE

Номер: US20210015765A1
Автор: GIANNOUSIS Peter, MIRMEHRABI Mahmoud, MOLLARD Paul, SUCHIT Shazad
Принадлежит:

Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms. 1. A polymorph of a solvate of (R)-2-hydroxy-2-methyl-4-(2 ,4 ,5-trimethyl-3 ,6-dioxocyclohexa-1 ,4-dienyl)butanamide , wherein the polymorph is selected from the group consisting of Forms IV , V , and VI wherein a powder X-ray diffraction pattern for polymorph Form IV comprises characteristic peaks at least at the following angular positions , wherein the angular positions may vary by ±0.2: 4.31 , 12.97 , and 13.20; wherein a powder X-ray diffraction pattern for polymorph Form V comprises characteristic peaks at least at the following angular positions , wherein the angular positions may vary by ±0.2: 9.61 , 11.49 , and 15.45; and wherein a powder X-ray diffraction pattern for polymorph Form VI comprises characteristic peaks at least at the following angular positions , wherein the angular positions may vary by ±0.2: 6.27 , 9.91 , and 12.94.26.-. (canceled)7. The polymorph of claim 1 , wherein the polymorph is Form V.8. The polymorph of claim 1 , wherein the polymorph is Form V claim 1 , wherein a powder X-ray diffraction pattern for the polymorph comprises characteristic peaks at the following angular positions claim 1 , wherein the angular positions may vary by ±0.2: 9.61 claim 1 , 11.49 claim 1 , 12.93 claim 1 , 15.45 claim 1 , and 26.05.9. (canceled)10. A composition comprising the polymorph claim 7 , wherein the composition is essentially free of Forms I-IV and VI claim 7 , wherein; wherein a powder X-ray diffraction pattern for polymorph Form I comprises characteristic peaks at least at the ...

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Номер записи: 83
17-01-2019 дата публикации

Ultra bright dimeric or polymeric dyes

Номер: US20190016898A1
Автор: Michael VANBRUNT, Sharat Singh, Tracy Matray
Принадлежит: Sony Corp, Sony Corp of America

or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L1, L2, L3, L4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

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Номер записи: 84
16-01-2020 дата публикации

Catalytic Process For Preparing N,N-Dimethylglucamine From N Methylglucamine

Номер: US20200017435A1
Автор: Akgün Ertan, Klug Peter, KREUZPOINTNER Stefan, LINK Martin, RAAB Klaus, SCHEITZENEDER Karl, WERNER Sarah
Принадлежит: CLARIANT INTERNATIONAL LTD.

The invention relates to a method for preparing aqueous solutions of N,N-dimethylglucamine, characterized by first preparing an adduct of N-methylglucamine and formaldehyde in water at temperatures of between 15° C. and 40° C., and subsequently reacting said adduct to N,N-dimethylglucamine in the presence of a metal catalyst under hydrogen pressure at 20-68° C., followed by secondary hydrogenation at 70-120 bar and 70-110° C. once hydrogen absorption at 20-68° C. is completed. 1. A process for preparing N ,N-dimethylglucamine comprising the step of reacting an aqueous solution of N-methylglucamine first with an aqueous solution of formaldehyde at 15-40° C. and subsequently , at a pressure of 20-120 bar and a temperature T=30-68° C. , with hydrogen under metal catalysis , wherein , after absorption of hydrogen has completed at 20-68° C. , a further , after-hydrogenation is added at 70-120 bar and at 70-110° C.2. The process as claimed in claim 1 , wherein the metal catalyst is Raney nickel.3. The process as claimed in claim 1 , which is carried out at a hydrogen pressure of 70-110 bar.4. The process as claimed in claim 1 , wherein the hydrogenation is carried out at 35-65° C.5. The process as claimed in claim 1 , wherein the molar ratio of N-methylglucamine to formaldehyde is 1:1 to 1:1.5.6. The process as claimed in claim 1 , wherein the hydrogenation catalyst is reused more than 5 times.7. The process as claimed in claim 1 , wherein reaction takes place in a stirred reactor or loop reactor.8. The process as claimed in claim 1 , wherein the remaining N-methylglucamine content is <2 claim 1 , wt %.9. The process as claimed in claim 1 , wherein the residual formaldehyde content is <0.1 wt %.10. The process as claimed in claim 1 , in which the Hazen color number of the resulting solution of N claim 1 ,N-dimethylglucamine is <500.11. The process as claimed in claim 1 , in which the molar ratio of N-methylglucamine to formaldehyde is 1:1 to 1:1.2.12. The process as ...

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Номер записи: 85
28-01-2016 дата публикации

Novel Formulation of Indomethacin

Номер: US20160022637A1
Автор: Aaron Dodd, Adrian Russell, Felix Meiser, H. William Bosch, Marck Norret
Принадлежит: Iceutica Pty Ltd

The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

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Номер записи: 86
10-02-2022 дата публикации

OPIOID RECEPTOR MODULATOR DOSAGE FORMULATIONS

Номер: US20220040151A1
Автор: Ceulemans Jens Jozef, Costello Tim, Heyns Philip Erna H., Jans Eugeen Maria Jozef
Принадлежит:

Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations. 1. A pharmaceutical tablet comprising:about 75 mg or about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid;about 70-90% by weight of a combination of a first filler and a second filler;about 3-7% by weight disintegrant;about 0.55-0.95% by weight colloidal silicon dioxide; andabout 0.45-1% by weight lubricant;wherein the first filler is mannitol; and wherein the tablet comprises at least 10% by weight mannitol.2. The tablet of claim 1 , wherein the second filler is silicified microcrystalline cellulose.3. The tablet of claim 1 , wherein the disintegrant is crospovidone.4. The tablet of claim 1 , comprising about 5% by weight disintegrant.5. The tablet of claim 4 , comprising about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2 claim 4 ,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.6. The tablet of claim 5 , comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant claim 5 , wherein the lubricant is magnesium stearate.7. The tablet of claim 5 , wherein the disintegrant is crospovidone.8. The tablet of claim 7 , comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant.9. The tablet of claim 8 , wherein the lubricant is magnesium stearate.10. The tablet of claim 1 , comprising:about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid;about 560 mg-720 mg of the combination of the first filler and the second filler;about 24 mg-56 mg disintegrant;about 4.4 mg-7.6 mg ...

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Номер записи: 87
26-01-2017 дата публикации

ONO Pincer Ligands and ONO Pincer Ligand Comprising Metal Complexes

Номер: US20170022230A1
Автор: "OREILLY MATTHEW", VEIGE ADAM STEVEN
Принадлежит:

Embodiments of the invention are directed to ONO pincer ligands that can be in a trianionic, protonated or protonated equivalent form. The ONO pincer ligand can be combined with a metal comprising compound to form an ONO pincer ligand comprising transition metal complex. By choice of the ONO pincer ligand structure, the steric and electronic properties of the metal complexes therefrom can be controlled. The ONO pincer ligands comprise a central nitrogen atom that is disubstituted with a pair of three atom comprising bridges where the three atoms are a pair of sphybridized carbons and an sphybridized carbon. 3. A method of preparing an ONO pincer ligand precursor according to claim 1 , comprising condensing a nucleophilic oxygen or nucleophilic nitrogen comprising compound with an electrophilic carbon comprising compound further comprising the bridge structure of the resulting ONO pincer ligand.4. A trianionic ONO pincer ligand comprising metal complex comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one ONO trianionic pincer ligand derived from the ONO trianionic pincer ligand precursor of ; and'}a metal.5. The trianionic ONO pincer ligand comprising metal complex of claim 4 , wherein the metal is a transition metal from group III through group X of the periodic table.13. The method of preparing an ONO pincer ligand comprising metal complex of claim 11 , wherein the precursor metal compound further comprises a metal alkylidyne claim 11 , further comprising adding the OH or NH of the ONO pincer ligand precursor across the metal alkylidyne to form the anionic ONO pincer ligand comprising metal complex. This application is a divisional of U.S. application Ser. No. 14/077,822, filed Nov. 12, 2013, which is a continuation-in-part of International Patent Application No. PCT/US2012/037302, filed May 10, 2012, which claims the benefit of U.S. Provisional Application Ser. No. 61/484,793, filed May 11, 2011, the disclosures of which are hereby ...

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Номер записи: 88
17-04-2014 дата публикации

TRI-ARYL COMPOUNDS AND COMPOSITIONS COMPRISING THE SAME

Номер: US20140107336A1
Автор: GAZIT Aviv, PRIEL Esther, Slavin Shimon, YITZCHAK Sara
Принадлежит: Ben-Gurion University of the Negev Research and Development Authority

The present invention relates to a novel class of tri-aryl compounds, compositions comprising the same and processes for the preparation thereof. 2. The compound of claim 1 , wherein Z is nitrogen claim 1 , phosphor claim 1 , arsenic claim 1 , silicon or germanium.3. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare independently selected from the group consisting of:{'sub': 2', 'n, '—(CH)-heterocycloalkyl group;'}{'sub': 2', 'n, '—(CH)-aminoalkyl group;'}{'sub': 2', 'n, '—(CH)-dialkylamino group;'}{'sub': 2', 'n', '3', '2, '—(CH)—N(CH)group;'}{'sub': 2', 'n', '2, '—(CH)—N(Et)group;'}{'sub': 2', 'n, '—(CH)-aryl group;'}{'sub': 2', 'n, '—(CH)-heteroaryl group;'}{'sub': 2', 'n, '—(CH)-haloalkyl group; and'}{'sub': 2', 'n, 'claim-text': 'wherein n is between 1-6.', '—(CH)-cycloalkyl group,'}4. The compound of claim 1 , wherein Ris methyl.5. The compound of claim 4 , wherein Z is carbon claim 4 , R′ claim 4 , R″ claim 4 , and R′″ are hydrogen claim 4 , and R claim 4 , R claim 4 , R claim 4 , R claim 4 , Rand Rare halogen.8. The compound of claim 7 , wherein X is carbon claim 7 , Ris halogen claim 7 , Rand Rare independently hydrogen claim 7 , methyl claim 7 , alkyl or alkoxy claim 7 , and Rand Rare hydrogen.9. The compound of claim 7 , wherein X is nitrogen claim 7 , Ris nothing claim 7 , Rand Rare independently hydrogen claim 7 , methyl claim 7 , alkyl or alkoxy claim 7 , and Rand Rare hydrogen.11. A pharmaceutical composition comprising the compound of .12. A pharmaceutical composition comprising the compound of . The present invention relates to a novel class of tri-aryl compounds, pharmaceutical compositions comprising the same and methods of preparation thereof.Nucleic acid polymerases are enzymes, whose primary function is to polymerize new nucleic acids such as deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) using an existing DNA or RNA template. Polymerases typically are involved in the processes of ...

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Номер записи: 89
17-04-2014 дата публикации

DENDRIMERS AND METHODS FOR THEIR PREPARATION

Номер: US20140107376A1
Автор: Peera Asghar A., Tomlinson Ian A.
Принадлежит:

Provided are new dendrimers and processes for making them. The dendrimers are derived from a nitroalkyloxirane compound of formula (III): wherein R, R, and Rare as described herein. 2. The dendrimer of wherein the terminal residues are amine residues claim 1 , hydroxyl residues claim 1 , thiol residues claim 1 , or combinations of two or more thereof.3. The dendrimer of wherein Rand Rare each C-Calkyl.4. The dendrimer of wherein Ris H.5. The dendrimer of wherein when the core is an aliphatic acyclic residue containing 2 amine residues claim 1 , the dendrimer comprises at least 2 generations.6. The dendrimer of of the structure shown in Table 1.8. The process of wherein the terminal functional groups of the polyvalent organic molecule are amines claim 7 , hydroxyls claim 7 , thiols claim 7 , or combinations of two or more thereof.9. The process of wherein R claim 7 , Rand the nitrogen to which they are attached form a NOgroup claim 7 , and the dendrimer is further functionalized to form a functionalized dendrimer by: base catalyzed reaction with an aldehyde (Henry Reaction); base catalyzed reaction with an α claim 7 ,β-unsaturated ester or nitrile (Michael Reaction); base catalyzed reaction with an aldehyde in the presence of an amine (Mannich Reaction); strong base catalyzed reaction with an alkyl halide (alkylation); strong base catalyzed reaction with an acyl chloride or activated ester (acylation); or base catalyzed halogenation.10. The process of wherein Rand Rare H claim 7 , and the dendrimer is further functionalized to form a functionalized dendrimer by reaction with an epoxide claim 7 , acrylate claim 7 , or acid chloride.11. The process of wherein the dendrimer is further functionalized with a dye claim 9 , a drug claim 9 , or a drug targeting molecule.12. The process of wherein the functionalized dendrimer is of the structure shown in Table 2. This application claims priority from provisional application Ser. No. 61/497,551, filed Jun. 16, 2011, which is ...

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Номер записи: 90
02-02-2017 дата публикации

NOVEL TRISCATIONIC AMPHIPHILE DERIVATIVE COMPOUNDS HAVING A PENDENT ALCOHOL GROUP, COMPOSITIONS THEREOF, AND METHODS FOR MAKING SAME

Номер: US20170029363A1
Автор: Caran Kevin L., Seifert Kyle
Принадлежит:

The inventive subject matter relates to compounds of Formula I, compositions thereof, and processes for making such compounds as further described herein. The inventive compounds and compositions have antimicrobial properties and are useful as environmental disinfectants, topical cleansers such as topical personal care compositions, sanitizers, preservatives, in water treatment, as permanent or erodible coatings for medical devices and appliances, and in therapeutics. Additionally, the compounds of Formula I will serve as synthetic intermediates for making additional novel derivatives of triscationic amphiphile compounds. 2. The compound of claim 1 , wherein:{'sub': 1', 'n, 'Ris independently selected from the group consisting of straight or branched chain Calkyl; and'}{'sub': 2', 'm, 'Ris independently selected from the group consisting of straight or branched chain Calkyl.'}3. The compound of claim 2 , wherein:{'sub': 1', '2-18, 'Ris independently selected from the group consisting of straight chain Calkyl; and'}{'sub': 2', '2-18, 'Ris independently selected from the group consisting of straight chain Calkyl.'}4. The compound of claim 3 , wherein:{'sub': 1', '8-16, 'Ris independently selected from the group consisting of straight chain Calkyl; and'}{'sub': 2', '8-16, 'Ris independently selected from the group consisting of straight chain Calkyl.'}5. The compound of claim 4 , wherein:{'sub': 1', '10-14, 'Ris independently selected from the group consisting of straight chain Calkyl; and'}{'sub': 2', '10-14, 'Ris independently selected from the group consisting of straight chain Calkyl.'}6. The compound of claim 5 , wherein:{'sub': 1', '12, 'Ris Calkyl; and'}{'sub': 2', '12, 'Ris Calkyl.'}7. The compound of claim 1 , wherein X is halogen.8. The compound of claim 7 , wherein X is bromine.10. The method of claim 9 , wherein:{'sub': 1', 'n, 'Ris independently selected from the group consisting of straight or branched chain Calkyl; and'}{'sub': 2', 'm, 'Ris independently ...

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Номер записи: 91
02-02-2017 дата публикации

KINASE INHIBITOR

Номер: US20170029378A1
Автор: Fyfe Matthew Colin Thor
Принадлежит:

There is provided a compound of formula VIIa, 2. A compound of formula VIIa claim 1 , or a salt or protected derivative thereof claim 1 , as claimed in claim 1 , wherein said compound is methyl 4-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)ureido)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoate. This invention relates, inter alia, to a compound which is an antiinflammatory agent (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), for example the alpha kinase sub-type thereof; Syk kinase; and the Src family of tyrosine kinases). The invention also relates to the use of this compound in therapy, including in mono- and combination therapies, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung (such as asthma and chronic obstructive pulmonary disease (COPD)), eye (such as uveitis or keratoconjunctivitis sicca (dry eye disease, also known as xerophthalmia)) and gastrointestinal tract (such as Crohn's disease and ulcerative colitis).The listing or discussion of an apparently prior-published document in this specification should not necessarily be taken as an acknowledgement that the document is part of the state of the art or is common general knowledge.Four p38 MAPK isoforms (alpha, beta, gamma and delta respectively) have been identified, each displaying different patterns of tissue expression. The p38 MAPK alpha and beta isoforms are found ubiquitously throughout the body, are present in many different cell types and are inhibited by a number of previously described small molecular weight compounds. Early classes of inhibitors were highly toxic due to the broad tissue distribution of these isoforms which resulted in off-target effects of the compounds. Some of the more recently identified inhibitors show improved selectivity for p38 MAPK alpha and beta isoforms and have wider safety ...

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Номер записи: 92
02-02-2017 дата публикации

BIOCATALYST SOLVENT USING IONIC LIQUID, AND BIOCATALYST SOLUTION CONTAINING BIOCATALYST AND SAID SOLVENT

Номер: US20170029801A1
Автор: KANEKO Kotaro, KANEKO Nobuhiro, KAWAI Koji
Принадлежит: MIYOSHI OIL & FAT CO., LTD.

There is provided a biocatalyst solvent which is capable of dissolving a biocatalyst in a liquid state while maintaining the activity of the biocatalyst at a high concentration from a low temperature to a high temperature, and is capable of storing the biocatalyst for a long time period; and a biocatalyst solution using the biocatalyst solvent. Disclosed is a biocatalyst solvent which consists of an ionic liquid including a quaternary ammonium cation represented by the following Formula (I) and an anion: 14-. (canceled)6. The biocatalyst solvent according to claim 5 , wherein the biocatalyst solvent is capable of storing the biocatalyst while retaining the activity of the biocatalyst.7. The biocatalyst solvent according to claim 5 , wherein the quaternary ammonium cation represented by Formula (I) in the ionic liquid has a structure with n representing 1 to 3.8. The biocatalyst solvent according to claim 7 , wherein the quaternary ammonium cation represented by Formula (I) in the ionic liquid has a structure with n representing 1 to 3 claim 7 , and R's each independently representing a hydrogen atom claim 7 , a methyl group or an ethyl group.9. The biocatalyst solvent according to claim 8 , wherein the anion of the ionic liquid is at least one selected from the group consisting of a carboxylate anion claim 8 , a sulfonate anion and a phosphate anion claim 8 , and the biocatalyst is an enzyme.10. The biocatalyst solvent according to claim 8 , wherein the quaternary ammonium cation represented by Formula (I) in the ionic liquid has a structure with n representing 1 to 3 claim 8 , and R's representing a hydrogen atom.11. The biocatalyst solvent according to claim 10 , wherein the anion of the ionic liquid is at least one selected from the group consisting of a halogen-based anion claim 10 , a sulfur-based anion claim 10 , a phosphorus-based anion claim 10 , a cyan-based anion claim 10 , a boron-based anion claim 10 , a fluorine-based anion claim 10 , a nitrogen oxide- ...

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Номер записи: 93
01-02-2018 дата публикации

Ethyl Benzyl Quaternary Amines of Amido Amines for Improved Antifungal properties

Номер: US20180029972A1
Автор: Daly Thomas P.
Принадлежит:

Ethyl benzyl quaternaries having superior anti-fungal properties versus their benzyl quaternary analogs. The ethylbenzyl amidoamine quaternaries of the present invention are easily produced without significant waste and with minimal capital, while possessing improved antimicrobial properties. These molecules are useful in a range of applications such as fungicides, personal care as treatments for acne, dandruff, psoriasis and other fungal skin born conditions, as well as in feminine products where an antifungal is required that is gentle on the sensitive tissues, as well as HIV prevention. These molecules are also excellent hair conditioners and laundry fabric softeners. 2. The zwitterionic surfactant of where R═C17H35 and n=1.3. The zwitterionic surfactant of where R═C17H33 and n=1.4. The zwitterionic surfactant of where R═C17H35 and n=105. The zwitterionic surfactant of where R═C17H33 and n=06. The zwitterionic surfactant of where R═C11H23 and n=1.7. The zwitterionic surfactant of where R═C11H23 and n=0.9. The zwitterionic surfactant of where R═C17H35 and n=1 claim 8 , G═—H and J═—H.10. The zwitterionic surfactant of where R═C17H33 and n=1 claim 8 , G═—H and J═—H.11. The zwitterionic surfactant of where R═C11H23 and n=1 claim 8 , G═—H and J═—H.12. The zwitterionic surfactant of where R═C17H35 and n=0 claim 8 , G═—H and J═—H.13. The zwitterionic surfact of where R═C17H33 and n=0 claim 8 , G═—H and J═—H.14. The zwitterionic surfactant of where R═C11H23 and n=0 claim 8 , G═—H and J═—H.15. The zwitterionic surfactant of where R═C17H35 and n=1 claim 8 , G═—CH3 and J═—H.16. The zwitterionic surfactant of where R═C17H33 and n=1 claim 8 , G═—CH3 and J═—H.17. The zwitterionic surfactant of where R═C11H23 and n=1 claim 8 , G═—CH3 and J═—H.18. The zwitterionic surfactant of where R═C17H35 and n=1 claim 8 , G═—H and J═—CH3.19. The zwitterionic surfactant of where R═C17H33 and n=1 claim 8 , G═—H and J═CH3.20. The zwitterionic surfactant of where R═C11H23 and n=1 claim 8 , G═—H ...

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Номер записи: 94
01-02-2018 дата публикации

Crystalline Forms of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride

Номер: US20180029976A1
Автор: BUSCHMANN Helmut, Fischer Andreas, GRUSS Michael, LISCHKE Dagmar
Принадлежит:

A hitherto unknown crystalline form of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence. 1. A process for producing a (-)-(1R ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A , said process comprising:dissolving a (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B in acetone, acetonitrile or isopropanol to form a solution;leaving the solution to crystallize andisolating crystals of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A.2. The process of claim 1 , wherein said (-)-(1R claim 1 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of Form B is dissolved in acetonitrile claim 1 , and further comprising the steps of:stirring the solution;removing insoluble residue by filtering andevaporating the acetonitrile leaving (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of Form A to crystallize.3. The process according to claim 1 , wherein said (-)-(1R claim 1 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B is dissolved in isopropanol at temperatures above room temperature claim 1 , and after complete dissolution no further heat is provided and further comprising:adding seed crystals of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form A and then cooling the mixture down to ≦15° C.4. The process of claim 3 , wherein said (-)-(1R claim 3 ,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride of crystalline Form B is dissolved in isopropanol at a temperature above 65° C. but not exceeding 80° C.5. The process of claim 3 , wherein said mixture is cooled down to ≦10 ...

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Номер записи: 95
01-02-2018 дата публикации

CONDENSATION PRODUCT OF 1-AMINO-2-PROPANOL AND FORMALDEHYDE AND THE USE THEREOF FOR REDUCING THE AMOUNT OF HYDROGEN SULPHIDE IN LIQUIDS AND GASES

Номер: US20180030041A1
Автор: Beilfuss Wolfgang, Gradtke Ralf, Knopf Jennifer, WEBER Klaus
Принадлежит:

Disclosed is a storage-stable condensation product prepared from 1-amino-2-propanol and formaldehyde in a molar ratio in the range from 1:2.0 to 1:3.1. The condensation product contains less than 10% by weight of water. Also, disclosed is the preparation of the condensation product and the use thereof for reducing the amount of hydrogen sulphide in liquids and gases. 1. Process for preparing a condensation product , containing less than 10% by weight of water , comprising the successive steps:Step a) of reaction of 1-amino-2-propanol is reacted with formaldehyde in a molar ratio in the range from 1:2.0 to 1:3.1 and at a temperature in the range from 50° C. to 80° C. to form a product;Step b) of removal of water from the product obtained at the end of step a), under reduced pressure to form the condensation product.2. Process according to claim 1 ,wherein the molar ratio of 1-amino-2-propanol to formaldehyde is in the range from 1:2.5 to 1:3.1.3. Process according to claim 1 , wherein the reaction in step a) is carried out at a temperature in the range from 60° C. to 70° C.4. Process according to claim 1 , wherein in step a) claim 1 , formaldehyde is used in the form of paraformaldehyde.5. Process according to claim 1 , wherein claim 1 , in step a) claim 1 , 1-amino-2-propanol is initially charged and formaldehyde is added.6. Process according to claim 1 , wherein the removal of water is carried out at a temperature of from 50° C. to 80° C.7. Process according to claim 1 , wherein the removal of water is carried out at a pressure in the range from 10to 10Pa (1 to 100 mbar)8. Process according to claim 1 , wherein the condensation product contains less than 4% by weight of water.9. Condensation product obtainable by the process according to .10. A method for removing sulphur compounds from process streams claim 9 , comprising providing a condensation product containing less than 10% by weight of water claim 9 , according to claim 9 , and applying the condensation ...

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Номер записи: 96
31-01-2019 дата публикации

Process of Manufacturing a Stable, Ready to Use Infusion Bag for an Oxidation Sensitive Formulation

Номер: US20190029979A1
Автор: Sasank KUNADHARAJU, Satish Pejaver, Tushar HINGORANI, Tushar Malkan
Принадлежит: InnoPharma, Inc.

A process for minimizing formation of a highest degradation product during moist heat sterilization of a drug solution of an oxidation susceptible active pharmaceutical ingredient (API) is provided, wherein the water is not deoxygenated and a nitrogen blanket is not used during formulation, or the formulation is stored in ambient conditions in the polymer bag and autoclaved. The highest degradation product in the parenteral drug product is less than 0.1% by weight of a labeled amount of the oxidation susceptible API in the parenteral drug product.

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Номер записи: 97
30-01-2020 дата публикации

DENTAL POLYMERIZABLE MONOMERS, COMPOSITIONS, ADHESIVE DENTAL MATERIALS AND KITS

Номер: US20200030194A1
Автор: Arata Masami, KAMIMOTO Yoshihisa, KATSURA Yoshiaki, KINOSHITA Shinsuke, MITAMURA Takenori, MIYAMORI Sayaka, MURAI Hiroki, Ori Tatsuya, SHIMIZU Hirohisa, TANABE Yoshimitsu, TSUCHIKAWA Masuji, Yokoyama Takeshi, Yoshinaga Kazuhiko
Принадлежит:

A dental adhesive curable composition containing a polymerizable monomer including a polymerizable monomer represented by formula (1′) and defined amounts of an acidic group-containing polymerizable monomer, a polymerization initiator containing a peroxide and a photopolymerization initiator, and a reductant containing a sulfinic acid compound and/or a salt thereof, and a filler: 2. The dental adhesive curable composition according to wherein the content of the acidic group-containing polymerizable monomer (BC) is 1 to 10 parts by weight based on the total weight of the polymerizable monomer (III)3. A dental adhesive curable kit (αc) for preparing a dental adhesive curable composition (c) described in claim 1 , the dental adhesive curable kit (αc) comprising at least a first composition and a second composition claim 1 ,at least one of the first composition and the second composition including a polymerizable monomer (A),the first composition including a reductant (Dc),the second composition including an acidic group-containing polymerizable monomer (Bc) and a polymerization initiator (Cc).5. The dental adhesive curable composition (C) according to claim 4 , wherein the moiety of the general formula (2c) is the structure represented by the general formula (RB).7. A mobile tooth fixing material (βd) according to claim 6 ,wherein a cured product that is obtained by the following method and that is subjected to a three-point bending test exhibits a breaking energy of not less than 65 mJ,the cured product being obtained by packing the dental adhesive composition (d) into a 2×2×25 mm mold, which is brought into press contact with a polypropylene film and a glass plate, irradiating nine points on each of front and back sides with light for 10 seconds, and polishing a surface of the cured product with #320 waterproof abrasive paper,the three-point bending test being performed such that the obtained cured product is soaked in water at 37° C. overnight, and thereafter is ...

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Номер записи: 98
30-01-2020 дата публикации

NOVEL COMBINATIONS OF A H3 ANTAGONIST AND A NORADRENALINE REUPTAKE INHIBITOR, AND THE THERAPEUTICAL USES THEREOF

Номер: US20200030310A1
Автор: LANDAIS Laurent, LECOMTE Jeanne Marie, Ligneau Xavier, Perrin David, SCHWARTZ Jean Charles
Принадлежит:

The present invention relates to combinations of a H3 antagonist and an antidepressant, which exhibit a synergistic wake promoting activity. 2. The combination according to wherein said antidepressant is not venlafaxine.3. The combination according to wherein said antidepressant is a noradrenaline reuptake inhibitor chosen from duloxetine claim 1 , reboxetine claim 1 , atomoxetine claim 1 , desipramine claim 1 , desvenlafaxine.6. The combination according to claim 1 , wherein said noradrenaline reuptake inhibitors are chosen from duloxetine claim 1 , reboxetine claim 1 , atomoxetine claim 1 , desipramine.10. A pharmaceutical composition comprising a combination according to claim 1 , wherein both ingredients are administered simultaneously claim 1 , separately claim 1 , or staggered over time.11. A method for treating and/or preventing a disorder chosen from excessive daytime sleepiness claim 1 , substance such as alcohol abuse disorders claim 1 , and/or with attention and cognitive deficit claim 1 , in a patient suffering from deficient noradrenaline release claim 1 , comprising applying an effective amount of the combination of .12. The method according to claim 11 , wherein said disorder is excessive daytime sleepiness and occurs in a patient suffering from:Narcolepsy with and without cataplexy,Idiopathic hypersomnia,Daytime sleepiness disorders,Obstructive sleep apnea,Circadian rhythm sleep-wake disorders,Parkinson's disease, orPrader-Willi Syndrome.13. The method according to wherein said disorder is attention and cognitive deficit and occurs in a patient suffering from attention deficit and hyperactivity disorder (ADHD).14. The method according to wherein said disorder is excessive daytime sleepiness claim 11 , attention and cognitive deficit and occurs in a patient suffering from depression.15. The method according to wherein said disorder is chosen from substance abuse withdrawal syndromes.16. The combination according to claim 2 , wherein said ...

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Номер записи: 99
04-02-2021 дата публикации

OPIOID RECEPTOR MODULATOR DOSAGE FORMULATIONS

Номер: US20210030720A1
Автор: Ceulemans Jens Jozef, Costello Tim, Heyns Philip Erna H., Jans Eugeen Maria Jozef
Принадлежит:

Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations. 1. A tablet comprising:about 75 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid,silicified microcrystalline cellulose, colloidal silicon dioxide, crospovidone, mannitol, and magnesium stearate.2. The tablet of claim 1 , comprising about 5-15% by weight mannitol and about 0.55-0.95% by weight colloidal silicon dioxide.3. The tablet of claim 1 , comprising about 3-7% by weight crospovidone claim 1 , about 60-80% by weight silicified microcrystalline cellulose claim 1 , and about 5-15% by weight mannitol.4. The tablet of claim 1 , comprising about 5-15% by weight mannitol.5. The tablet of claim 4 , comprising about 60-80% by weight silicified microcrystalline cellulose.6. The tablet of claim 4 , comprising about 0.55-0.95% by weight colloidal silicon dioxide.7. The tablet of claim 5 , comprising about 3-7% by weight of crospovidone.8. The tablet of claim 6 , wherein extraction of the tablet with water or saline at 25° C. for 12 hours results in a concentration of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2 claim 6 ,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid of less than or approximately 4 mg/ml.9. The tablet of claim 7 , wherein extraction of the tablet with water or saline at 25° C. for 12 hours results in a concentration of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2 claim 7 ,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid of less than or approximately 4 mg/ml.10. The tablet of claim 6 , wherein extraction of the tablet at 25° C. for 12 hours in acidic solvent results in a greater ...

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Номер записи: 100