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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 8552. Отображено 100.
01-03-2012 дата публикации

Process to form a tablet and apparatus suitable for applying this process

Номер: US20120049412A1
Автор: Hans Almer Middlebeek, Jozefus A.C. Smit
Принадлежит: Intervet International BV

The present invention pertains to a process for the preparation of a fast-disintegrating tablet ( 30 ) containing a medicinal substance, comprising the steps of providing a fluid formulation comprising the medicinal substance, providing a solid element ( 100 ) having formed therein at least one cavity, ( 101 ) cooling the solid element ( 100 ) to a temperature below a freezing temperature of the formulation, filling the cavity with the fluid formulation, solidifying the formulation while present in the cavity ( 101 ) to form a solid pellet comprising the medicinal substance without actively shaping the entire surface of the pellet, taking the pellet out of the cavity and drying the pellet in a vacuum to obtain the tablet. The invention also pertains to a system for performing such a process and a package containing the resulting tablet.

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Номер записи: 1
01-03-2012 дата публикации

Alkoxylated alkylamines/alkyl ether amines with peaked distribution

Номер: US20120053054A1
Автор: Alberto Slikta, David Becher, David Eaton, Giao Nguyen, Henry Agbaje, Kha Nguyen, Michael Seitz, Shawn Zhu
Принадлежит: Akzo Nobel NV

The present invention generally relates to a process for preparing the alkoxylated alkylamines and/or alkyl ether amines. The process consists of three stages, and utilizes an alkali catalyst. The alkoxylated alkyl amines and alkoxylated alkyl ether amines prepared by the process possess the peaked distribution and contain less hazardous by-product.

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Номер записи: 2
15-03-2012 дата публикации

Delivery system for delivery of a substance into the oral cavity

Номер: US20120065160A1
Автор: Jonatan Moses
Принадлежит: NEOINVENT MEDICAL ENGR AB

A delivery system for use in the oral cavity, the system comprising a carrier for a bioactive substance. The carrier has a surface comprising oxygen-binding sites (X), and at least one link comprising a pentose group and one or more additional sugar groups, the pentose group being bonded to one of said oxygen binding sites (X) and wherein one or more bioactive molecules (R) are bonded directly to one of the sugar groups of the at least one link or to one or more substituents on one or more sugar groups in the at least one link.

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Номер записи: 3
03-05-2012 дата публикации

Process for preparing 1,4-bishydroxyethylpiperazine

Номер: US20120108816A1
Автор: Christof Wilhelm Wigbers, Johann-Peter Melder, Nina Challand, Roman Dostalek, Udo Rheude
Принадлежит: BASF SE

Process for preparing 1,4-bishydroxyethylpiperazine (BHEPIP) of the formula I wherein diethanolamine (DEOA) of the formula II is reacted in the liquid phase in a reactor at a temperature in the range from 130 to 300° C. in the presence of a copper-comprising, chromium-free heterogeneous catalyst.

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Номер записи: 4
05-07-2012 дата публикации

Compositions, Synthesis, and Methods of Using Cycloalkylmethylamine Derivatives

Номер: US20120172426A1
Автор: Kouacou Adiey, Laxminarayan Bhat
Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

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Номер записи: 5
26-07-2012 дата публикации

Tertiary Amine Salt Additives for Hydrate Control

Номер: US20120190893A1
Автор: Cheryl R. Bailey, Jun Tian
Принадлежит: Baker Hughes Inc

New tertiary amine salts are useful as gas hydrate inhibitors in oil and gas production and transportation. These tertiary amine salts give very good separation from an emulsion, are economic and have reduced toxicity concerns.

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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
23-08-2012 дата публикации

Polymers based on glycerol carbonate and an amine

Номер: US20120215020A1
Автор: Fabien Jean Brand, Roman Benedikt Raether
Принадлежит: BASF SE

The present invention relates to a polymer and the associated polymerization process, and to the use of the polymers according to the invention for example as foam suppressant, for the dispersion of solids or as surfactant for washing or cleaning purposes. The polymer is prepared by polymerization of a) at least one alkylene oxide or a cyclic carbonate of the formula (I) where n is 1 to 10, m is 0 to 3 and R 1 is C 1 -C 10 -alkyl, C 2 -C 10 -alkenyl, aryl or aralkyl, b) glycerol carbonate and c) at least one amine.

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Номер записи: 8
27-09-2012 дата публикации

Orally dispersible tablet

Номер: US20120244223A1
Автор: Naoki Nagahara, Tetsuya Matsuura, Yutaka Tanoue, Yutaka Yamagata
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

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Номер записи: 9
18-10-2012 дата публикации

Process for preparing n,n-dimethylaminoethoxyethanol

Номер: US20120264979A1
Автор: Alfred Krause, Bernd Stein, Frank Haese, Frank-Friedrich Pape, Joachim-Thierry Anders, Johann-Peter Melder
Принадлежит: BASF SE

A process for preparing N,N-dimethylaminoethoxyethanol (DMAEE), wherein a) dimethylamine and ethylene oxide are reacted, b) the resulting product mixture of N,N-dimethylethanolamine and DMAEE is separated by distillation to obtain a DMAEE-containing fraction as the bottom stream, and c) DMAEE from the fraction obtained in (b) is removed by distillation.

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Номер записи: 10
10-01-2013 дата публикации

Melt extruded nicotine thin strips

Номер: US20130011462A1
Автор: Caroline Bruce, Mark Manning
Принадлежит: NOVARTIS AG

A thin strip for oral ingestion is between 0.05 millimeters and 2.00 millimeters thick. It includes 10 to 80% by weight of polyethylene oxide having a molecular weight of from 70,000 to 300,000 daltons. It further includes 5 to 50% by weight of a sugar alcohol having a melting point in excess of 75 C and 5 to 30% by weight of polyethylene glycol having a molecular weight of from 200 to 1,000 daltons. Lastly it includes 1 to 30% by weight of a carboxy vinyl polymer cross linked with an allyl ether of pentaerythritol, and 1 to 10% by weight of an organic acid addition salt of nicotine.

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Номер записи: 11
10-01-2013 дата публикации

2,4,5-triaminophenols and related compounds

Номер: US20130012681A1
Автор: Joachim C. Ritter, Rajiv Dhawan
Принадлежит: EI Du Pont de Nemours and Co

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.

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Номер записи: 12
28-03-2013 дата публикации

AMINOBENZENE COMPOSITIONS AND RELATED DEVICES AND METHODS

Номер: US20130075670A1
Автор: Brown Christopher T., Seshadri Venkataramanan, Wang Jing
Принадлежит: Plextronics, Inc.

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

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Номер записи: 13
28-03-2013 дата публикации

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

Номер: US20130079417A1
Автор: Chen Gang, 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. 2. The compound of wherein Ris selected from the group consisting of halo claim 1 , OR claim 1 , SR claim 1 , NO claim 1 , CN claim 1 , NC claim 1 , Calkyl claim 1 , haloCalkyl claim 1 , OCF claim 1 , Cheteroalkyl claim 1 , and hydroxyCalkyl claim 1 ,and n is 0, 1, or 2.3. The compound of wherein Ris selected from the group consisting of Calkyl claim 1 , halo claim 1 ,{'sup': 'a', 'and OR, and n is 0, 1, or 2.'}4. The compound of wherein Ris selected from the group consisting of F claim 1 , Br claim 1 , Cl claim 1 , OH claim 1 , NO claim 1 , OCH claim 1 , OCF claim 1 , CF claim 1 , CH claim 1 , and CH claim 1 , and n is 0 or 1.6. The compound of wherein Ris F claim 5 , Br claim 5 , Cl claim 5 , OH claim 5 , NO claim 5 , OCH claim 5 , OCF claim 5 , CF claim 5 , CH claim 5 , or CH claim 5 ,and n is 0 or 1.7. The racemic mixture of a compound of .8. (canceled)9. The (+) enantiomer of substantially free of the (−) enantiomer.10. (canceled)11. The (−) enantiomer of substantially free of the (+) enantiomer.12. (+)-trans(S claim 1 ,S)-[2-(2-Cyclopropylmethyloxy-5-fluorophenyl)cyclopropyl]methylamine Hydrochloride claim 1 ,(+)-trans(S,S)-[2-(2-Cyclopropylmethyloxy-5-hydroxyphenyl)cyclopropyl]methylamine Hydrochloride, or a pharmaceutically acceptable salt or hydrate thereof.13. A composition comprising (a) compound of claim 1 , (b) optionally a second therapeutic agent useful in the treatment of a disease or condition wherein modulation of 5-HT(2C) provides a benefit claim 1 , and (c) an excipient and/or pharmaceutically acceptable carrier.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 ...

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Номер записи: 14
04-04-2013 дата публикации

Buccal Drug Delivery

Номер: US20130085165A1
Автор: Anders Dam, Janos Major, Peter Tasko
Принадлежит: Arrow No 7 Ltd

A lozenge is provided that has stable pH and stable levels of active ingredient over time. It comprises a combination of (i) at least one gum and (ii) at least one non-crystallising sugar or non-crystallising sugar alcohol in a matrix designed for controlled buccal delivery of a drug. The lozenge also contains water and optional components selected from flavourings, taste masking agents, colourings, buffer components, pH adjusting agents, excipients, stabilizers and sweeteners. Methods of preparing the lozenge are also provided.

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Номер записи: 15
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: 16
11-04-2013 дата публикации

Buccal Drug Delivery

Номер: US20130087946A1
Автор: Anders Dam, Janos Major, Peter Tasko
Принадлежит: Arrow No 7 Ltd

A lozenge is provided that has stable pH and stable levels of active ingredient over time. It comprises a combination of (i) at least one gum and (ii) at least one non-crystallising sugar or non-crystallising sugar alcohol in a matrix designed for controlled buccal delivery of a drug. The lozenge also contains water and optional components selected from flavourings, taste masking agents, colourings, buffer components, pH adjusting agents, excipients, stabilizers and sweeteners. Methods of preparing the lozenge are also provided.

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Номер записи: 17
11-04-2013 дата публикации

Novel Low Molecular Weight Cationic Lipids for Oligonucleotide Delivery

Номер: US20130090372A1
Автор: Budzik Brian W., Colletti Steven L., DAVIS Jennifer R., Hills Ivory D., SEIFRIED Darla Danile, Stanton Matthew G.
Принадлежит:

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A cationic lipid of Formula A according to claim 1 ,wherein:{'sup': 1', '2, 'Rand Rare each methyl;'}{'sub': 1', '4', '22', '4', '22, 'Lis selected from C-Calkyl and C-Calkenyl; and'}{'sub': 2', '3', '13', '3', '33, 'Lis selected from C-Calkyl and C-Calkenyl;'}or any pharmaceutically acceptable salt or stereoisomer thereof.3. A cationic lipid which is selected from:R—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 2);S—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 1);1-{2-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-1-[(octyloxy)methyl]ethyl}pyrrolidine (Compound 3);(2S)—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-[(5Z)-oct-5-en-1-yloxy]propan-2-amine (Compound 4);1-{2-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-1-[(octyloxy)methyl]ethyl}azetidine (Compound 5);(2S)-1-(hexyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 6);(2S)-1-(heptyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 7);N,N-dimethyl-1-(nonyloxy)-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 8);N,N-dimethyl-1-[(9Z)-octadec-9-en-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 9);(2S)—N,N-dimethyl-1-[(6Z,9Z,12Z)-octadeca-6,9,12-trien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 10);(2S)-1-[(11Z,14Z)-icosa-11,14-dien-1-yloxy]-N,N-dimethyl-3-(pentyloxy)propan-2-amine (Compound 11);( ...

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Номер записи: 18
18-04-2013 дата публикации

PROCESS FOR PREPARATION OF AMISULPRIDE

Номер: US20130096319A1
Автор: Chavan Yuvraj Atmaram, Deshpande Tushar Nandkumar, Kolekar Mahesh Ramkumar, Paghdar Dinesh Jayntibhai, Patil Suryaprakash Pandurang, Ray Purna Chandra, Singh Girij Pal
Принадлежит: Lupin Limited

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

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Номер записи: 19
25-04-2013 дата публикации

Method and agent for detecting drugs in beverages

Номер: US20130098286A1
Автор: Catherine Herry, Emmanuel Dupau, Pauline Contamin
Принадлежит: Ethypharm SAS

The present invention relates to a method for combating chemical submission, which comprises: putting into solution, in a beverage, a pharmaceutical form comprising an active ingredient and at least 0.05 mg, preferably from 0.2 to 5 mg, even more preferentially from 0.3 to 2 mg of at least one water-soluble colouring agent chosen from: indigocarmine or E 132, erythrosine or E 127, brilliant blue FCF, alphazurine FG, fast green FCF, quinzarine green SS, orange II, tartrazine and Sunset yellow FCF, detecting the pharmaceutical form, said detection being characterized by the immediate change in colour of the beverage; it also relates to the use of said colorant for combating chemical submission, and also to a non-film-coated solid pharmaceutical form comprising said colorant.

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Номер записи: 20
09-05-2013 дата публикации

INTRAORALLY DISINTEGRATING TABLET

Номер: US20130115287A1
Автор: Nakamura Kazuhiro, Ogawa Teppei
Принадлежит: TEIJIN PHARMA LIMITED

Disclosed is an orally disintegrating tablet which masks bitterness, dissolves well, and which permanently retains good oral disintegration properties immediately following manufacture. The disclosed orally disintegrating tablet is formed by compression-molding an organic acid together with particles comprising active ingredient-containing nuclear particles covered by a layer containing water-insoluble polymers and/or enteric polymers. 1. An intraorally disintegrating tablet , in which an active ingredient-containing core particle coated with a layer comprising a water insoluble polymer and/or an enteric polymer has been compression molded together with an organic acid.2. The tablet of claim 1 , wherein the content of the organic acid is 1 to 10 wt %.3. The tablet of claim 1 , wherein the organic acid is ascorbic acids and/or citric acids.4. The tablet of claim 1 , wherein the water insoluble polymer and/or the enteric polymer is a methacrylic acid copolymer.5. The tablet of claim 1 , wherein the water insoluble polymer and/or the enteric polymer is ethyl cellulose.6. An intraorally disintegrating tablet claim 1 , in which an active ingredient-containing core particle coated with a layer containing a water insoluble polymer and/or an enteric polymer and a granule obtained by coating a disintegrant-containing particle with a disintegrant have been compression molded together with an organic acid. The present invention relates to an intraorally disintegrating tablet comprising an organic acid as a disintegration accelerator.Intraorally disintegrating tablets containing organic acids such as ascorbic acids and citric acids are known. Specific examples thereof include, those containing ascorbic acid as an active ingredient (Patent Documents 1-3) and those illustrating the addition of an organic acid as a dissolution agent for an active ingredient in order to ensure absorptivity (Patent Documents 4 and 5). However, none of the above documents describe or suggest ...

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Номер записи: 21
06-06-2013 дата публикации

AMPHIPATHIC LIPID-BASED SUSTAINED RELEASE COMPOSITIONS

Номер: US20130142876A1
Автор: Howard Scott A., Purvis Troy
Принадлежит: PEGASUS LABORATORIES, INC.

Chewable sustained release compositions and their methods of production are provided. The sustained release compositions contain amphipathic lipids, which are used to encapsulate various drugs and active ingredients. 1. A composition comprising:(a) about 0.5 to about 90 weight percent of one or more active ingredients;(b) between about 0.5 to about 80 weight percent of one or more amphipathic lipids; and(c) between about 5 to about 90 weight percent of at least one bulking or spheronizing agent,wherein said at least one active ingredient being encapsulated within a matrix comprising said one or more amphipathic lipids and said at least one bulking or spheronizing agent,wherein said composition exhibits an in vitro dissolution rate of said active ingredients as measured by a USP Dissolution Apparatus II of about 10% to 50% after about 2 hours, about 25% to 90% after about 4 hours, more than about 60% after about 12 hours, and more than about 75% after about 16 hours.2. The composition according to wherein said composition comprises at least about 1 and/or no more than about 60 weight percent of said one or more active ingredients.3. The composition according to wherein said composition comprises at least about 1 and no more than about 50 weight percent of said one or more amphipathic lipids.4. The composition according to wherein said composition comprises at least about 10 and no more than about 70 weight percent of said at least one bulking or spheronizing agent.5. The composition according to wherein said composition exhibits an in vitro dissolution rate of said active ingredients as measured by a USP Dissolution Apparatus II of no more than 90% of said active ingredients released after 8 hours.6. The composition according to wherein said one or more amphipathic lipids are selected from the group consisting of phospholipids claim 1 , lecithins claim 1 , ceramides claim 1 , sphingolipids claim 1 , steroids claim 1 , and glycolipids.7. The composition according to ...

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Номер записи: 22
06-06-2013 дата публикации

Ferrimannitol-ovalbumin tablet composition

Номер: US20130143819A1
Автор: Ana Isabel Torres-Suarez, Daniel Filipe Tavares Da Silva Fernandes, Maria Esther Gil Alegre
Принадлежит: Tedec Meiji Farma SA

The invention refers to an oral pharmaceutical tableted dosage form which comprises a mixture of: a) granules comprising ferrimannitol-ovalbumin (FMOA) and at least an intragranular pharmaceutical acceptable excipient including a binder; and b) extragranular pharmaceutical excipients including a filler and a binder; which may be obtained by wet-granulation and compression.

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Номер записи: 23
06-06-2013 дата публикации

POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND

Номер: US20130143846A1
Автор: Ebdrup Soren, Greve Tanja Maria, Nielsen Kim Troensegaard
Принадлежит: LEO PHARMA A/S

The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C-Calkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C-Calkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid. 1. A crystalline form of {4-[(1R ,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.2. The crystalline form according to which belongs to the orthorhombic space group P222having unit-cell parameters a=8.7299(17) Å claim 1 , b=14.822(3) Å and c=16.353(3) Å.3. The crystalline form according to which has an X-ray powder diffraction pattern that exhibits characteristic peaks expressed in 2θ at approximately 8.0 claim 1 , 11.3 claim 1 , 11.4 claim 1 , 15.0 claim 1 , 18.2 and/or 21.5 (±0.05 degrees) (underlined primary) claim 1 , respectively.4. The crystalline form according to which has an X-ray powder diffraction pattern substantially as appears from Graph 2b.5. The crystalline form according to which has a differential scanning calorimetry curve comprising an event with an onset at about 255° C. (±2° C.).6. The crystalline form according to which has a differential scanning calorimetry curve substantially as appears from Graph 4b.7. The crystalline form according to which has Solid State NMR spectrum substantially as ...

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Номер записи: 24
06-06-2013 дата публикации

Sublingual zolpidem formulations

Номер: US20130143912A1
Автор: Ajay Kumar Narayan Sharma, Hemanth Prakash Joshi, Natarajan Mathivanan, Prasad Vure, Priyanka Sriram Pathak, Snehalatha Movva
Принадлежит: Dr Reddys Laboratories Inc, Dr Reddys Laboratories Ltd

The present disclosure provides pharmaceutical compositions for the delivery of a hypnotic agent across the oral mucosa. In particular, the compositions devoid of buffer and in the presence of alkaline oxides capable of raising the pH of saliva to a pH greater than about 7.0 thereby facilitate the substantially complete conversion of the hypnotic agent from its ionized to its un-ionized form. As a result, the dose of hypnotic agent is rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-subject variability. Furthermore, delivery of the hypnotic agent across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating sleep disorders such as insomnia are also provided.

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Номер записи: 25
13-06-2013 дата публикации

SOLID DAPOXETINE

Номер: US20130150453A1
Автор: JITHENDER Aadepu, Krishnareddy Pingili, Mohan Rao Dodda
Принадлежит: SYMED LABS LIMITED

The present invention relates to solid racemic dapoxetine, solid dapoxetine S(+)enantiomer, processes for their preparation and their use in the pharmaceutically active compound dapoxetine acid addition salt, and pharmaceutical compositions thereof. 110-. (canceled)11. A solid racemic dapoxetine.12. A process for preparing solid racemic dapoxetine comprising:a) providing a solution of racemic dapoxetine in a hydrocarbon solvent n-hexane or cyclohexane or a mixture thereof; andb) evaporating the solvent(s), or by cooling the solution obtained in step (a) to below about 30° C. to obtain a solid; andc) recovering the solid obtained in step (b) by conventional methods to afford the desired racemic dapoxetine.13. The process of claim 12 , wherein the solution in step (a) is obtained by dissolving an oily residue or crude faun of racemic dapoxetine or racemic dapoxetine obtained from a reaction mixture of racemic dapoxetine or a salt thereof in a suitable organic solvent(s).14. The process of claim 12 , wherein the solution is obtained at a temperature range from about 30° C. to about the boiling point of the solvent (s) used.15. The process of claim 12 , wherein the solid is precipitated in step b) by evaporation of the solvents from the solution of step a) at elevated temperatures under reduced pressure or by cooling the solution from about −5° C. to about 30° C.16. The process of claim 12 , wherein recovery of solid racemic dapoxetine in step c) is by a conventional method.17. The process of claim 12 , wherein the solid racemic dapoxetine obtained is dried at a temperature range from about 25° C. to about 45° C. under reduced pressure.18. The process of claim 12 , wherein the solid racemic dapoxetine obtained is optionally recrystallized from a solvent or a mixture of solvents selected from the group consisting of esters claim 12 , alcohols claim 12 , or alcohols in combination with water in any proportion.19. A solid dapoxetine S(+) enantiomer.20. process for ...

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Номер записи: 26
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: 27
13-06-2013 дата публикации

Novel Amino Alcohol Cationic Lipids for Oligonucleotide Delivery

Номер: US20130150625A1
Автор: Budzik Brian W., Colletti Steven L., SEIFRIED Darla Danile, Stanton Mathew G., Tian Lu
Принадлежит:

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is more efficacious than traditional cationic lipids. The present invention employs amino alcohols to enhance the efficiency of in vivo delivery of siRNA. 2. A cationic lipid of Formula A according to claim 1 , wherein:{'sup': 1', '2, 'Rand Rare each H;'}{'sup': '3', 'Ris H;'}{'sub': 1', '4', '22', '4', '22, 'Lis selected from C-Calkyl and C-Calkenyl; and'}{'sub': 2', '4', '22', '4', '22, 'Lis selected from C-Calkyl and C-Calkenyl;'}or any pharmaceutically acceptable salt or stereoisomer thereof.3. A cationic lipid which is selected from:2-amino-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-2-{[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]methyl)}propan-1-ol (Compound 1);2-amino-3-[(9Z)-octadec-9-en-1-yloxy]-2-{[(9Z)-octadec-9-en-1-yloxy]methyl}propan-1-ol (Compound 2);2-amino-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-2-[(octyloxy)methyl]propan-1-ol (Compound 3); and2-(dimethylamino)-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-2-{[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]methyl}propan-1-ol (Compound 4) or any pharmaceutically acceptable salt or stereoisomer thereof.4. The use of a cationic lipid according to for the preparation of lipid nanoparticles.5. The use of a cationic lipid according to as a component in a lipid nanoparticle for the delivery of oligonucleotides.6. The use according to wherein the oligonucleotides are siRNA or miRNA.7. The use according to wherein the oligonucleotides are siRNA. The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo. ...

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Номер записи: 28
20-06-2013 дата публикации

CATIONIC ALCOHOLS AND USES THEREOF

Номер: US20130156719A1
Автор: Love Kevin T., Nagamoottoo-Casse Lorna, Puerta David T.
Принадлежит: Living Proof, Inc.

Compositions are disclosed comprising novel fluorinated cationic alcohols in a cosmetically acceptable vehicle. The fluorinated compounds alter a surface property of the hair to provide hair conditioning, for example. In embodiments, the compounds have improved water solubility and deposition properties. 8. A method of treating hair claim 5 , comprising applying a cosmetic composition according to to hair.9. A method of treating hair claim 6 , comprising applying a cosmetic composition according to to hair.10. A method of treating hair claim 7 , comprising applying a cosmetic composition according to to hair. This application is a divisional of U.S. application Ser. No. 13/547,522, filed Jul. 12, 2012, which is a continuation of U.S. application Ser. No. 12/883,762, filed Sep. 16, 2010, now U.S. Pat. No. 8,242,309, which claims the benefit of U.S. Provisional Application No. 61/243,066, filed Sep. 16, 2009 and U.S. Provisional Application No. 61/320,362, filed Apr. 2, 2010, all of which are incorporated herein by reference.1. Field of the InventionThe invention is directed to cationic fluorinated alcohols, compositions containing the same, and methods for treating surfaces such as hair and skin.2. Description of Related ArtHair conditioning refers to the process of imparting attributes such as smoothness, softness, and ease of styling to hair. Conditioning may also reduce a feeling of dryness and impart shine. Both damaged and normal hair require conditioning, however, there is a greater need of conditioning for damaged hair due to the negative attributes it imparts. There is no single sensory attribute that equates with the perception of damage, rather it is associated with a combination of tactile and visual properties. For example, damaged hair in general is more hydrophilic leaving it susceptible to moisture flux which increases its propensity for swelling and breakage leading to a rough texture. Additionally, damaged hair tends to have a duller appearance due ...

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Номер записи: 29
20-06-2013 дата публикации

Composition of Antigen and Method of Sublingual Administration

Номер: US20130156812A1
Автор: Hauer Stephen, Holm Kristin
Принадлежит:

A method of sublingually administering an effective amount of an antigenic composition to a mammal in order to produce a mucosal and systemic immune response. 1. A method for the sublingual administration of a therapeutic compound to a human or animal comprising mixing an effective amount of said therapeutic compound with a pharmaceutically acceptable viscous compound and providing said mixture to said human or animal for oral consumption.2. A method according to wherein said viscous compound is spread on a serving structure such that full oral consumption by said human or animal requires repeated licking of said mixture.3. A method according to wherein said viscous compound is spread inside a serving structure such that full oral consumption by said human or animal requires repeated licking of said mixture.4. A method according to wherein said animal is a dog.5. A method according to wherein said animal is a cat.6. A method according to wherein the viscous compound is flavored to appeal to a human or animal.7. A method according to wherein said therapeutic compound contains allergenic extracts.8. A method according to wherein the viscous compound additionally contains any of a prebiotic agent and a probiotic agent.9. A method according to wherein said viscous carrier is paste.10. A method according to wherein said viscous carrier is a gel.11. A method according to wherein said composition is in the form of an aqueous solution.12. A composition comprising:a. one or more antigenic extracts; andb. a viscous compound.13. A composition according to wherein said viscous compound is a paste claim 11 , gelatin claim 11 , gum claim 11 , or cellulosic compound.14. A composition according to wherein said viscous compound is peanut butter.15. A composition according to wherein said composition additionally comprises a prebiotic.16. A composition according to wherein said composition additionally comprises a probiotic. Allergic disease is an increasingly prevalent health ...

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Номер записи: 30
04-07-2013 дата публикации

SOFT FOOD COMPOSITION WITH PROBIOTICS AND PREBIOTICS FOR MASKING MEDICATIONS

Номер: US20130171204A1
Автор: DuBourdieu Daniel J., Gor Tapan A., Lall Rajiv, Raval Devraj C., Sinha Anita K.
Принадлежит: VETS PLUS, INC.

A soft extruded food composition containing probiotics, enzymes, and vitamins for wrapping medications, such as pills or tablets, for animal consumption. The flavor of the wrapped solid medication is masked by the food composition and thus becomes more palatable to the animal while providing additional health benefits in the form of probiotics, prebiotics, enzymes, and vitamins. 1. A consumable composition for providing health benefits to an animal comprising: a carrier base comprising components selected from the group consisting of a powder, an emulsifier, a starch, an oil, a softening agent, and water in a combination and in amounts effective to confer viscoelasticity to the viscoelastic mass; and', 'an effector component selected from the group consisting of a probiotic, a prebiotic, and an enzyme selected from the group consisting of a carbohydrase, a lipase, and a protease., 'a viscoelastic mass comprising2Aspergillus, Trichoderma, Bacillus, Bacteriodies, Bifidobacterium, Lactobacillus, Leuconostoc, Streptococcus, Pediococcus, Propionibacterium, Saccharomyces, Enterococcus, Escherichia. The composition of comprising the probiotic claim 1 , wherein the probiotic is a microorganism in a genus selected from the group consisting of claim 1 , and combinations thereof.3. The composition of comprising the probiotic in an amount of from about 0.01 to about 1×10CFU/g of the viscoelastic mass.4. The composition of comprising the prebiotic claim 1 , wherein the prebiotic is selected from the group consisting of inulin claim 1 , lactulose claim 1 , lactitol claim 1 , a fructooligosaccharide claim 1 , a galactooligosaccharide claim 1 , a xylooligosaccharide claim 1 , an isomaltooligosaccharide claim 1 , a mannaoligosaccharide claim 1 , a lactosucrose claim 1 , a cereal fiber claim 1 , a soy oligosaccharide claim 1 , raffinose claim 1 , beet pulp claim 1 , psyllium claim 1 , cellulose claim 1 , gum arabic claim 1 , and combinations thereof.5. The composition of comprising ...

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Номер записи: 31
04-07-2013 дата публикации

BRANCHED HETERO POLYFUNCTIONAL POLYOXYALKYLENE COMPOUND AND INTERMEDIATE THEREOF

Номер: US20130172576A1
Автор: Kamiya Masaki, Nakamoto Ken-ichiro
Принадлежит: NOF CORPORATION

A branched hetero polyfunctional polyoxyalkylene compound represented by the following formula (1): 2. The branched hetero polyfunctional polyoxyalkylene compound according to claim 1 , wherein OAand OAare an oxyethylene group claim 1 , in the formula (1).3. The branched hetero polyfunctional polyoxyalkylene compound according to claim 1 , wherein n and r are 0 and m is 100 to 800 claim 1 , in the formula (1).4. The branched hetero polyfunctional polyoxyalkylene compound according to claim 2 , wherein n and r are 0 and m is 100 to 800 claim 2 , in the formula (1).5. The branched hetero polyfunctional polyoxyalkylene compound according to claim 1 , wherein n is 1 to 500 and m is 100 to 800 claim 1 , in the formula (1).6. The branched hetero polyfunctional polyoxyalkylene compound according to claim 1 , wherein X and Y are a functional group capable of chemically bonding to an amino group claim 1 , a mercapto group claim 1 , a carboxyl group claim 1 , an aldehyde group claim 1 , an unsaturated bond claim 1 , or an azido group claim 1 , in the formula (1).7. The branched hetero polyfunctional polyoxyalkylene compound according to claim 2 , wherein X and Y are a functional group capable of chemically bonding to an amino group claim 2 , a mercapto group claim 2 , a carboxyl group claim 2 , an aldehyde group claim 2 , an unsaturated bond claim 2 , or an azido group claim 2 , in the formula (1).8. The branched hetero polyfunctional polyoxyalkylene compound according to claim 1 , wherein X and Y are a functional group selected from a substituted active ester claim 1 , an active carbonate claim 1 , an aldehyde claim 1 , an isocyanate claim 1 , an isothiocyanate claim 1 , an epoxide claim 1 , a thiol claim 1 , a substituted maleimide claim 1 , a hydrazide claim 1 , a dithiopyridine claim 1 , a substituted sulfonate claim 1 , an amine claim 1 , an oxyamine claim 1 , an α-haloacetyl claim 1 , a carboxylic acid claim 1 , a substituted unsaturated bond claim 1 , and an azide ...

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Номер записи: 32
11-07-2013 дата публикации

METHODS OF TREATMENT USING ARYLCYCLOPROPYLAMINE COMPOUNDS

Номер: US20130178520A1
Автор: Caron Marc G., GAINETDINOV RAUL R., Gooden David M., McCafferty Dewey G., Pollock Julie A., Sotnikova Tatyana D.
Принадлежит: Duke University

Described herein are methods of treating Parkinson's disease using arylcyclopropylamine compounds. 2. The method of claim 1 , wherein R claim 1 , R claim 1 , Rand Rare hydrogen.3. The method of claim 1 , wherein Ris selected from Chaloalkyl claim 1 , halo claim 1 , Calkoxy claim 1 , and Caryloxy.4. The method of claim 1 , wherein Rand Rare taken together with the carbon atoms to which they are attached to form a Cheterocyclyl ring.5. The method of claim 4 , wherein Rand Rare taken together to form a five-membered heterocyclyl ring.6. The method of claim 1 , wherein Ris hydrogen.818.-. (canceled)20. The method of claim 19 , wherein A is a heterocyclyl ring.21. The method of claim 19 , wherein A is a bicyclic heterocyclyl ring.27. The method of claim 26 , wherein Xand Xare O.28. The method of claim 26 , wherein n is 1.2939.-. (canceled) This application claims priority to U.S. Provisional Patent Application No. 61/579,872, filed on Dec. 23, 2011, the entire contents of which are hereby incorporated by reference.This invention was made with United States Government support awarded by National Institutes of Health, Grant No. GM65539. The U.S. Government has certain rights in this invention.Although there is no known cure for Parkinson's disease (PD), one of the two most common neurodegenerative diseases of aging, dopamine (DA) replacement therapy by administration of the DA biosynthetic precursor levodopa (L-DOPA or LD) has been employed for over 40 years as the gold standard for treatment of PD-associated symptoms. However, the efficacy of this treatment may wane with time, and the drug may have a number of long-term side-effects including L-DOPA-induced dyskinesias (LIDs), fluctuations in motor performance, and hallucinations. Often these effects can become dose limiting at a time when patients are in need of more medication and not less. DA agonists, as well as several other classes of drugs directly or indirectly affecting DA function (monoamine oxidase (MAO) ...

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Номер записи: 33
11-07-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF

Номер: US20130178644A1
Автор: Bertolini Giorgio, Landoni Nicola, Motta Giuseppe, Vergani Domenico
Принадлежит: EUTICALS S.P.A.

The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. 130-. (canceled)32. The process according to claim 31 , wherein the halide is bromide and the metal is zinc or magnesium.33. The process according to claim 31 , wherein the ethyl metal halide is ethylmagnesium bromide.34. The process according to claim 32 , wherein the ethyl metal halide is used in a quantity between 1 and 5 equivalents with respect to compound (VIII).35. The process according to claim 31 , wherein the alkylation is carried out at a temperature between 0° C. and the boiling temperature of the solvent.36. The process according to claim 35 , wherein the alkylation is carried out at a temperature between 10 and 30° C.38. The process according to claim 37 , wherein the chiral acid is selected from D(−) mandelic acid claim 37 , D(−) 2-chloromandelic acid claim 37 , D(−) tartaric acid claim 37 , and (2R claim 37 ,3R)-O claim 37 ,O′-dibenzoyl tartaric acid.39. The process according to claim 38 , wherein the chiral acid is D(−) mandelic acid.40. The process according to claim 37 , wherein the polar solvent of step a′) is selected from: water claim 37 , aliphatic ketones and/or aliphatic alcohols claim 37 , used ...

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Номер записи: 34
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: 35
25-07-2013 дата публикации

ORAL PRODUCT

Номер: US20130189333A1
Автор: Atchley Frank Scott, DiNovi Christopher Joseph, Gao Feng, Gee Diane, Griscik Gregory, Hulan Phillip M., Kobal Gerd
Принадлежит: ALTRIA CLIENT SERVICES INC.

An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and an additive dispersed in the mouth-stable polymer matrix. The oral product is adapted to release the additive from the body when the body is received within the oral cavity and exposed to saliva. 1. An oral product , comprising a body that is wholly receivable in an oral cavity , the body comprising:a mouth-stable polymer matrix;cellulosic fibers embedded in the mouth-stable polymer matrix; andan additive dispersed in the mouth-stable polymer matrix such that the additive is released from the body when the body is received within the oral cavity and exposed to saliva.2. The oral product of claim 1 , wherein the mouth-stable polymer matrix comprises polyurethane.3. The oral product of claim 1 , wherein the mouth-stable polymer matrix comprises polyester.4. The oral product of claim 1 , wherein the mouth-stable polymer matrix comprises polyacrylate.5. The oral product of claim 1 , wherein the mouth-stable polymer matrix comprises apolyethylene claim 1 , SEBS claim 1 , SBS claim 1 , or another thermal plastic elastomer.6. The oral product of claim 1 , further comprising a plasticizer dispersed in the mouth-stable polymer matrix.7. The oral product of claim 6 , wherein the plasticizer is selected from the group consisting of propylene glycol claim 6 , glycerin claim 6 , vegetable oil claim 6 , triglycerides claim 6 , and combinations thereof.8. The oral product of claim 1 , further comprising a sweetener dispersed in the body.9. The oral product of claim 1 , wherein the sweetener is selected from the group consisting of saccharine claim 1 , sucralose claim 1 , aspartame claim 1 , acesulfame potassium claim 1 , and combinations thereof.10. The oral product of claim 1 , wherein the additive is selected from the group consisting of minerals claim 1 , vitamins claim 1 , dietary ...

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Номер записи: 36
25-07-2013 дата публикации

CALCIUM RECEPTOR-ACTIVE MOLECULES

Номер: US20130190407A1
Автор: Balandrin Manuel F., Del Mar Eric G., Nemeth Edward F., Van Wagenen Bradford C.
Принадлежит: NPS PHARMACEUTICALS, INC.

The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies. 76. (canceled)78. The compound of or a pharmaceutically acceptable salt thereof claim 77 , wherein Yand Yare each independently a phenyl claim 77 , or 1- or 2-napthyl.79. The compound of or a pharmaceutically acceptable salt thereof claim 78 , wherein Yis independently a phenyl or 2-napthyl; and Yis independently a phenyl or 1-naphthyl.80. The compound of or a pharmaceutically acceptable salt thereof claim 79 , wherein Ris a methyl; and Ris a hydrogen.82. The compound of or a pharmaceutically acceptable salt thereof wherein the cycloaliphatic ring is selected from the group consisting of: cyclopropyl claim 77 , cyclobutyl claim 77 , cyclopentyl claim 77 , cyclopropylmethyl claim 77 , and cyclohexyl.838284. A pharmaceutical composition comprising a pharmaceutically acceptable carrier claim 77 , and a compound of any one of - or or a pharmaceutically acceptable salt thereof.84. The compound of or a pharmaceutically acceptable salt thereof claim 77 , wherein Alkyl is a C-Chydrocarbon having spor sphybridization and further comprises linear or branched moieties claim 77 , or a combination ...

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Номер записи: 37
25-07-2013 дата публикации

PROCESS FOR PREPARING CHOLINE HYDROXIDE FROM TRIMETHYLAMINE AND ETHYLENE OXIDE

Номер: US20130190534A1
Автор: Chen Xiaoyun, Dixit Ravindra S., JR. John G., Li Ruokang, Patel Avani M., Pell Randy J., PENDERGAST
Принадлежит: DOW AGROSCIENCES LLC

Processes for preparing N,N,N-trimethylethanolammonium hydroxide (choline hydroxide) and the choline hydroxide produced are described. These processes minimize the production of byproduct mono-ethoxylated and di-ethyoxylated choline in the product choline hydroxide. The processes generally include feeding ethylene oxide, trimethylamine, and water into a first reactor to create a first reactor product under temperature controlled conditions. The product of the first reactor is fed into a second reactor to form a second reactor product under uncontrolled, adiabatic, conditions. Finally, any unreacted to trimethylamine in the second reactor product is removed to form a final product comprising choline hydroxide. Additional reactors can be used for the ethylene oxide and trimethylamine reaction. 1. A process for preparing choline hydroxide comprising:feeding ethylene oxide, trimethylamine, and water into a first reactor to create a first reactor product, wherein the first reactor temperature is maintained between 5° C. and 35° C. and the molar ratio of ethylene oxide to trimethylamine fed to the first reactor is equal to or less than one;feeding the first reactor product into a second reactor to form a second reactor product, wherein the second reactor is insulated; andremoving any unreacted trimethylamine from the second reactor product to form a final product comprising choline hydroxide.2. The process of claim 1 , wherein the choline hydroxide final product comprises less than 10 weight percent mono-ethoxylated choline and/or di-ethyoxylated choline.32. The process of any one of - claims 1 , wherein the trimethylamine and water are fed into the first reactor as a mixture.43. The process of any one of - claims 1 , wherein the residence time in the second reactor is sufficient for any unreacted ethylene oxide present in the first reactor product to react.54. The process of any one of - claims 1 , wherein adiabatic heating in the second reactor raises the temperature of ...

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Номер записи: 38
01-08-2013 дата публикации

Non-Starch Based Soft Chewables

Номер: US20130197006A1
Автор: HAMANN Hans-Juergen, KANIKANTI Venkata-Rangarao
Принадлежит: Bayer Animal Health GmbH

The present invention generally relates to soft chewables, especially suitable for delivering active ingredients to animals and processes for the preparation thereof. In various embodiments, the soft chewable comprises a pharmaceutically effective amount of at least one active ingredient, a flavoring agent, a disintegrant a humectant, an antioxidant, a preservative, and water. In accordance with preferred embodiments, the soft chewable is essentially free of starch, oil glycols, waxes, and soy products. 1. A soft chewable comprising:(a) a pharmaceutical effective amount of at least one active ingredient;(b) a flavoring agent;(c) a disintegrant;(d) a humectant;(e) a binder(f) an antioxidant;(g) optionally a preservative; and(h) water.2. The soft chewable of comprising (g) a preservative.3. The soft chewable of wherein the soft chewable disintegrates in less than about 25 minutes as determined in accordance with method 2.9.1 (Test B) of the European Pharmacopoeia 6.0.43. The soft chewable of claim to wherein the disintegrant constitutes at least about 10 wt % claim 2 , at least about 12 wt % claim 2 , at least about 15 wt % claim 2 , at least about 17 wt % claim 2 , at least about 20 wt % claim 2 , at least about 25 wt % claim 2 , at least about 30 wt %. claim 2 , at least about 40 wt % claim 2 , or at least about 50 wt % of the soft chewable.5. The soft chewable of wherein the disintegrant is selected from the group consisting of carmellose calcium claim 4 , directly compressible mannitol claim 4 , crosslinked povidone claim 4 , polyvinyl sodium claim 4 , a mixture of directly compressible mannitol and polyvinyl sodium claim 4 , and combinations thereof.6. The soft chewable of wherein the disintegrant is selected from the group consisting of a mixture of polyvinyl sodium and directly compressible mannitol claim 4 , a mixture of polyvinyl sodium and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer claim 4 , a mixture of croscarmellose sodium ...

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Номер записи: 39
08-08-2013 дата публикации

AMINE COMPOUND, ELECTROPHOTOGRAPHIC PHOTOCONDUCTOR, IMAGE FORMING METHOD, IMAGE FORMING APPARATUS, AND PROCESS CARTRIDGE

Номер: US20130202994A1
Автор: ARAI Ryota, Nomura Masayoshi, SHIMADA Tomoyuki
Принадлежит:

To provide an amine compound, represented by General Formula (I) below: 4. The electrophotographic photoconductor according to claim 3 , wherein the photoconductive layer includes a charge transport material.8. The electrophotographic photoconductor according to claim 4 , wherein the charge transport material is a polymeric charge transport material.11. The electrophotographic photoconductor according to claim 3 , wherein the electrophotographic photoconductor includes a protective layer on an outermost surface claim 3 , and the protective layer includes the amine compound represented by General Formula (I).12. The electrophotographic photoconductor according to claim 11 , wherein the protective layer includes a filler.13. The electrophotographic photoconductor according to claim 11 , wherein the protective layer includes a resin formed by curing a polymerizable monomer.15. The image forming apparatus according to claim 14 , wherein the exposure unit is any one of a laser diode and a light-emitting diode claim 14 , and the electrostatic latent image is digitally written on the electrophotographic photoconductor using the exposure unit. 1. Field of the InventionThe present invention relates to: an amine compound; an electrophotographic photoconductor including the amine compound; and an image forming method, an image forming apparatus and a process cartridge using the electrophotographic photoconductor.2. Description of the Related ArtIn recent years, development of an information-processing system device using an electrophotographic method is remarkable. In particular, a laser printer and a digital copier, which convert information to digital signals and carry out information recording with light, have improved significantly in terms of their print quality and reliability. Further, through combination with high-speed technology, they have been applied to a laser printer or a digital copier with which a full-color printing is possible. From such a background, to have ...

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Номер записи: 40
08-08-2013 дата публикации

CYCLOALIPHATIC CARBONATES AS REACTIVE DILUENTS IN EPOXY RESINS

Номер: US20130203894A1
Автор: Burton Bruce L.
Принадлежит: Huntsman Petrochemical LLC

Embodiments of the present invention disclose a method for limiting peak exotherm temperatures in epoxy systems comprising the step of: combining an amine hardener, an epoxy and a diluent to form an epoxy system, wherein the diluent is selected from the group consisting of: ethylene carbonate, propylene carbonate, butylene carbonate, delta-valerolactam, delta-valerolactone, gamma valerolactone, butyrolactam, beta butyrolactone, gamma butyrolactone, and combinations thereof. 1. A method for limiting peak exotherm temperatures in an epoxy system comprising the step of:combining an amine hardener, an epoxy, and a diluent to form an epoxy system;wherein the diluent is selected from the group consisting of: ethylene carbonate, propylene carbonate, butylene carbonate, delta-valerolactam, delta-valerolactone, gamma valerolactone, butyrolactam, beta butyrolactone, gamma butyrolactone, and combinations thereof.2. The method of wherein the diluent is propylene carbonate3. The method of wherein the diluent is selected from the group consisting of: delta-valerolactam claim 1 , delta-valerolactone claim 1 , gamma valerolactone claim 1 , butyrolactam claim 1 , beta butyrolactone claim 1 , gamma butyrolactone claim 1 , and combinations thereof.4. The method of wherein the epoxy system is substantially free of an aliphatic glycidyl ether.5. The method of wherein the aliphatic glycidyl ether comprises a diglycidyl ether of 1 claim 4 ,4-butane diol.6. The method of wherein the amine hardener comprises an aliphatic amine having an amine-hydrogen functionality greater than two amine hydrogens per molecule.7. The method of wherein the epoxy comprises a multifunctional polyglycidyl ether of dihydric phenol.8. The method of further comprising the step of heating the epoxy system.9. The method of further comprising the step of injecting claim 1 , filling claim 1 , or infusing the epoxy system into a mold.10. The method of wherein the mold is a wind blade mold.11. The method of claim 1 , ...

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Номер записи: 41
15-08-2013 дата публикации

MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR

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

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

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Номер записи: 42
22-08-2013 дата публикации

Process for the preparation of substituted n-(benzyl)cyclopropanamines by imine hydrogenation

Номер: US20130217910A1
Автор: Norbert Lui, Thomas Norbert MÜLLER, Wahed Ahmed Moradi
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(arypmethylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.

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Номер записи: 43
29-08-2013 дата публикации

QUATERNIZED POLYETHER AMINES AND THEIR USE AS ADDITIVE FOR FUELS AND LUBRICANTS

Номер: US20130225463A1
Автор: BOEHNKE Harald, Grabarse Wolfgang, HANSCH Markus, VOELKEL Ludwig, WALTER Marc
Принадлежит:

The present invention relates to novel quaternized polyetheramines and to the preparation thereof. The present invention further relates to the use of these compounds as a fuel and lubricant additive. More particularly, the invention relates to the use of these quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct injection diesel engines, especially in common rail injection systems, for reducing the fuel consumption of direct injection diesel engines, especially of diesel engines with common rail injection systems, and for minimizing power loss in direct injection diesel engines, especially in diesel engines with common rail injection systems. The invention also provides additive packages comprising these polyetheramines; and fuels and lubricants additized therewith. The invention further relates to the use of these quaternized nitrogen compounds as an additive for gasoline fuels, especially for improving the intake system cleanliness of gasoline engines. 1. A fuel composition or lubricant composition comprising , in a conventional fuel or lubricant , at least one reaction product comprising a quaternized nitrogen compound , said reaction product being obtainable by reactiona) of a polyether-substituted amine comprising at least one tertiary quaternizable amino group withb) a quaternizing agent which converts the at least one tertiary amino group to a quaternary ammonium group.2. The fuel composition or lubricant composition according to claim 1 , in which the polyether substituent comprises monomer units of the general formula Ic{'br': None, 'sub': 3', '4, '—[—CH(R)—CH(R)—O—]—\u2003\u2003(Ic)'}in which{'sub': 3', '4, 'Rand Rare the same or different and are each H, alkyl, alkylaryl or aryl.'}3. The fuel composition or lubricant composition according to claim 2 , wherein the polyether-substituted amine has a number-average molecular weight in the range from 500 to 5000.4. The fuel composition or ...

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Номер записи: 44
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: 45
29-08-2013 дата публикации

COMPOUNDS AND METHODS FOR PKC THETA INHIBITION

Номер: US20130225687A1
Автор: Ajioka Janet, Hummel Heidi S., Meyer Rich B., Swindle John
Принадлежит: Complegen Partners, LLC

The present invention provides a method of selectively inhibiting PKCθ in the presence of PKCδ, by administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula I. The present invention also provides a method of inhibiting cytokine synthesis in a T cell, a method of inhibiting T cell proliferation, and a method of inhibiting the replication of and cytokine production by T lymphocytes, while not stimulating or inhibiting the replication of B lymphocytes. 27.-. (canceled)8. The method of claim 1 , wherein Y is S.9. The method of claim 1 , wherein Y is O.10. (canceled)11. (canceled)12. The method of claim 1 , wherein each Ris independently selected from the group consisting of 4-t-butyl claim 1 , 4-cyclopentyl and 4-t-pentyl.1326.-. (canceled)27. The method of claim 1 , wherein the contacting is in vivo.28. The method of claim 1 , wherein the contacting is ex vivo. This application claims priority to U.S. Provisional Application No. 61/098,640, filed Sep. 19, 2008, which is incorporated in its entirety herein for all purposes.T lymphocytes are an essential part of the immune response as they are necessary for initiating the cellular response to pathogenic organisms, host cells that have become oncogenic and damaged tissue (see Fundamental Immunology, 6Edition, 2003, ed. Paul, Wm. Lippencott Williams & Wilkins). Functionally, T cells have been subdivided into two classes with distinct surface antigens, CD4 and CD8 and this differentiation occurs in the Thymus. CD4+ cells are helper T cells and are further divided into Th1, Th2 and Th17 (see Tesmer, L. A., et al. (2008) Immunological Reviews, 228, 87-113, Harington, L. et al. (2005) Nat. Immunol. 6, 1123) which produce distinct levels of different cytokines (see below). CD8+ cells are cytolytic cells and are involved in lysis of tumors or viral infected cells. These responses are usually initiated by the interaction of a specific surface protein of the T cell, the T cell Receptor ...

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Номер записи: 46
12-09-2013 дата публикации

Pharmaceutical Compositions Comprising Terbinafine

Номер: US20130236514A1
Автор: BONNY Jean-Daniel, EUGSTER Andreas Carl, GUITARD Patrice, Hirsch Stefan
Принадлежит: NOVARTIS AG

This invention provides a terbinafine pharmaceutical composition which is emulsifable or self-emulsifying or in form of an emulsion wherein the composition is adapted for oral administration. 1. An oral terbinafine pharmaceutical composition which is emulsifiable or self-emulsifying or in the form of an emulsion , wherein said composition comprises a lipid component that is a triglyceride of CG-12 saturated fatty acids , a surfactant and an emulsion stabilizing agent that is a mixture of sodium carboxymethylcellulose and microcrystalline cellulose.2. A pharmaceutical composition according to wherein the lipophilic component is present in an amount of 15 to 25% by weight based on total weight of composition.3. A pharmaceutical composition according to wherein the surfactant is a phospholipid.4. A pharmaceutical composition according to wherein the surfactant is present in an amount of 1.5 to 5% by weight based on total weight of composition.5. A pharmaceutical composition according to further comprising water.6. A pharmaceutical composition according to wherein the mean droplet size of lipophilic phase is of about 0.1 to 30 IJm.7. A method for the treatment of fungal infections of the human body comprising administering a pharmaceutically effective amount of a pharmaceutical composition according to to a subject in need of such treatment. The present invention relates to a pharmaceutical composition comprising terbinafine.Terbinafine may be used e.g. in free form or in acid addition salt form. An acid addition salt form may be prepared from the free base form in conventional manner and vice-versa. Examples of suitable acid addition salt form are the hydrochloride, the lactate and the ascorbate. The free base and the hydrochloride are preferred.Terbinafine is known from e.g. BE-PS-853976 and EP-A-24587. It belongs to the class of allylamine anti-mycotics. It is acknowledged in the art and is commercially available under the trade name Lamisil®.Terbinafine is highly ...

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Номер записи: 47
12-09-2013 дата публикации

LICORICE LOLLIPOP THAT INHIBITS DENTAL CARIES FORMATION

Номер: US20130236527A1
Автор: Anderson Maxwell H.
Принадлежит: INTELLIHERB, LLC

This invention pertains to the discovery that certain extracts of licorice, particularly when formulated as a candy or lollipop or other means that provides an extended release (e.g., greater than about 4 minutes) to the oral cavity significantly inhibits the formation of dental caries in a human subject. 1Glycyrrhiza. A composition for reducing dental caries in a human subject , said composition comprising a lollipop or hard candy , wherein said lollipop or hard candy is substantially sugar free , and said lollipop or hard candy comprises an extract from the root of spp. , wherein said extract comprises a glycyrrhizol.2. The composition of claim 1 , wherein said lollipop or hard candy is a lollipop.3. The composition of claim 1 , wherein said lollipop or hard candy comprises:a starch or dextrin;a flavoring;a sweetener; andsaid extract.4. The composition of claim 3 , wherein said sweetener is non-cariogenic.5. The composition of claim 3 , wherein said sweetener is a sugar alcohol.6. The composition of claim 3 , wherein said sweetener is an artificial sweetener.7. The composition of claim 3 , wherein said sweetener is selected from the group consisting of stevia claim 3 , aspartame claim 3 , saccharin claim 3 , acesulfame k claim 3 , sucralose claim 3 , and neotame.8. The composition of claim 3 , wherein said lollipop or hard candy comprises:hydrogenated starch hydrolysate;citric acid;flavoring; andacesulfame potassium.9. The composition of claim 8 , wherein said lollipop or hard candy further comprises a coloring agent.10. The composition of claim 1 , wherein said extract comprises substantially purified glycyrrhizol A claim 1 , and/or substantially purified glycyrrhizol B claim 1 , and/or substantially purified 6 claim 1 ,8-diisoprenyl-5 claim 1 ,7 claim 1 ,4′-trihydroxyisoflavone.11. The composition of claim 10 , wherein said extract comprises substantially purified glycyrrhizol A.12. The composition of claim 1 , wherein said extract consists essentially of ...

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Номер записи: 48
12-09-2013 дата публикации

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

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

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

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Номер записи: 49
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: 50
26-09-2013 дата публикации

ORAMUCOSAL PHARMACEUTICAL DOSAGE FORM

Номер: US20130252916A1
Автор: Danckwerts Michael Paul, Patel Rupal, Pillay Viness
Принадлежит: University of the Witwatersrand, Johannesburg

This invention relates to an oramucosal pharmaceutical dosage form in the form of a wafer. The wafer comprises a porous, hydroscopic, muco-adhesive polymeric matrix with at least one desired pharmaceutically active compound added thereto. The polymer is selected from a number of polymers having different dissolution rates and, in use when taken orally, the matrix adheres to an oramucosal surface to dissolve over a predetermined period of time to release the pharmaceutically active compound. The invention also extends to a method of manufacturing an oramucosal pharmaceutical dosage form in the form of a wafer which involves freeze drying or lyophilisation. 157-. (canceled)58. An oramucosal pharmaceutical dosage form comprising a porous , hydroscopic , muco-adhesive polymeric matrix comprising hydroxypropyl cellulose; excipients mannitol , lactose and glycine; and having at least one pharmaceutically active compound added thereto , the dosage form formulated into a wafer , in use the dosage form disintegrates within 30 seconds.59. The oramucosal pharmaceutical dosage form as claimed in claim 58 , wherein the pharmaceutically active compound is selected from the group consisting of: analgesics claim 58 , sedatives claim 58 , antihistamines and paediatric drugs.60. The oramucosal pharmaceutical dosage form as claimed in claim 59 , wherein the pharmaceutically active compound is an analgesic selected from the group consisting of: diclophenac claim 59 , aspirin and paracetamol.61. The oramucosal pharmaceutical dosage from as claimed in claim 59 , wherein the pharmaceutically active compound is a sedative selected from the group consisting of: diazepam claim 59 , zolpidem and zopiclone.62. The oramucosal pharmaceutical dosage form as claimed in claim 59 , wherein the pharmaceutically active compound is an antihistamine selected from the group consisting of: loratidine and chlorpheniramine.63. The oramucosal pharmaceutical dosage form as claimed in claim 59 , wherein the ...

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Номер записи: 51
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: 52
03-10-2013 дата публикации

AMPHIPATHIC LIPID-BASED SUSTAINED RELEASE COMPOSITIONS

Номер: US20130259937A1
Автор: Howard Scott A., Purvis Troy
Принадлежит:

Chewable sustained release compositions and their methods of production are provided. The sustained release compositions contain amphipathic lipids and matrix-forming polymers, which are used to encapsulate various drugs and active ingredients. The chewable sustained release compositions can maintain their sustained release properties even after being fragmented into a plurality of pieces. 1. A composition comprising:(a) one or more active ingredients;(b) one or more amphipathic lipids; and(c) at least one bulking or spheronizing agent,wherein said active ingredients being encapsulated within a matrix comprising said amphipathic lipids,wherein said composition exhibits an in vitro dissolution rate of said active ingredients as measured by a USP Dissolution Apparatus II of about 10% to 50% after about 2 hours, about 25% to 90% after about 4 hours, more than about 60% after about 12 hours, and more than about 75% after about 16 hours,wherein the average in vitro dissolution rate of said composition as measured by a USP Dissolution Apparatus II does not increase by more than 100% during the first 2 hours after said composition has been fragmented into two or more pieces.2. The composition according to wherein the average in vitro dissolution rate of said composition as measured by a USP Dissolution Apparatus II does not increase by more than 50% during the first 2 hours after said composition has been fragmented into two or more pieces.3. The composition according to wherein said composition comprises a plasticized matrix-forming polymer claim 1 , wherein said matrix encapsulating said active ingredients comprises said matrix-forming polymer.4. The composition according to wherein said matrix-forming polymer has a glass transition temperature (“Tg”) of not more than about 120° C.5. The composition according to wherein said matrix-forming polymer comprises a bulking or spheronizing agent claim 3 , a binder claim 3 , a flavoring agent claim 3 , a sustained coating ...

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Номер записи: 53
03-10-2013 дата публикации

Ibuprofen Solid Oral Dosage Composition Comprising a Methacrylic Acid Copolymer

Номер: US20130261188A1
Автор: DAS ADITYA R., HIBI TORU
Принадлежит: TEIKOKU PHARMA USA, INC.

Aspects of the invention include organoleptically acceptable solid oral dosage compositions of ibuprofen. Solid oral dosage compositions according to certain embodiments include ibuprofen and a methacrylic acid copolymer in an amount sufficient to make the composition organoleptically acceptable for administering in an oral cavity of a subject to deliver ibuprofen to the subject. Methods for preparing and using solid oral dosage compositions of the invention are also described. 1. A solid oral dosage composition comprising:ibuprofen; anda methacrylic acid copolymer in an amount sufficient to make the solid oral dosage composition organoleptically acceptable for administering in an oral cavity of a subject.34-. (canceled)5. The solid oral dosage composition according to claim 1 , wherein the amount of ibuprofen in the solid oral dosage composition ranges from 20 mg to 200 mg.67-. (canceled)8. The solid oral dosage composition according to claim 1 , wherein the amount of methacrylic acid copolymer ranges from 40 mg to 400 mg.9. (canceled)10. The solid oral dosage composition according to claim 1 , wherein the solid oral dosage composition is formulated for maintaining in an oral cavity of a subject for a predetermined amount of time to deliver ibuprofen to the subject.11. The solid oral dosage composition according to claim 10 , wherein the solid oral dosage composition is formulated to be maintained in the oral cavity of a subject for 10 minutes or more.12. (canceled)13. The solid oral dosage composition according to claim 10 , wherein the solid oral dosage composition is formulated to be disintegrated in the oral cavity by chewing.14. The solid oral dosage composition according to claim 10 , wherein the solid oral dosage composition is formulated to be dissolved in the oral cavity.15. The solid oral dosage composition according to claim 1 , wherein the solid oral dosage composition further comprises a souring agent.16. The solid oral dosage composition according to ...

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Номер записи: 54
03-10-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF IVABRADINE AND ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID

Номер: US20130261298A1
Автор: Grandjean Mathieu, LE FLOHIC Alexandre
Принадлежит: LES LABORATOIRES SERVIER

Process for the synthesis of ivabradine of formula (I): 2. The process according to claim 1 , wherein the coupling agent used to carry out the reaction for lactamisation of the compound of formula (VI) is selected from oxalyl chloride claim 1 , thionyl chloride claim 1 , N claim 1 ,N-dicyclohexylcarbodiimide (DCC) claim 1 , 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI) claim 1 , N claim 1 ,N-carbonyldiimidazole (CDI) claim 1 , 1-propanephosphonic acid cyclic anhydride (T3P) and 1-(methylsulphonyl)-1H-benzotriazole.3. The process according to claim 2 , wherein the coupling agent used to carry out the reaction for lactamisation of the compound of formula (VI) is thionyl chloride.4. The process according to claim 3 , wherein the amount of thionyl chloride used to carry out the reaction for lactamisation of the compound of formula (VI) is between 1 and 5 equivalents claim 3 , inclusive.5. The process according to claim 1 , wherein the base used to carry out the reaction for lactamisation of the compound of formula (VI) is selected from triethylamine claim 1 , diisopropylethylamine and pyridine.6. The process according to claim 5 , wherein the base used to carry out the reaction for lactamisation of the compound of formula (VI) is triethylamine.7. The process according to claim 1 , wherein the organic solvent used to carry out the reaction for lactamisation of the compound of formula (VI) is selected from dichloromethane claim 1 , tetrahydrofuran claim 1 , acetonitrile claim 1 , acetone and toluene.8. The process according to claim 7 , wherein the organic solvent used to carry out the reaction for lactamisation of the compound of formula (VI) is dichloromethane.9. The process according to claim 1 , wherein the reaction for lactamisation of the compound of formula (VI) is carried out at a temperature between 0° C. and 40° C. claim 1 , inclusive.12. The process according to claim 10 , wherein the base used to carry out the alkylation reaction between the compound of ...

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Номер записи: 55
10-10-2013 дата публикации

Laxative gel composition

Номер: US20130267607A1
Автор: Paranjothy Kanni, Veerappan Sellappan Subramanian
Принадлежит: Gavis Pharmaceuticals LLC

An edible, gel composition of a PEG and a gel forming agent wherein the composition is prepared by mixing together the PEG with gel forming agent to form the edible gel composition, and the edible gel composition has laxative properties.

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Номер записи: 56
17-10-2013 дата публикации

NOVEL FUNCTIONAL FOOD PRODUCT AND METHOD THEREOF

Номер: US20130274339A1
Автор: LURYA Leonid, NOVODVORETS Vadim
Принадлежит:

A whole impregnated freeze dried food product for delivering a material of interest comprising; 2. The method according to claim 1 , wherein said step of drying the obtained food product is performed at a temperature of about 40° C.-about 60° C. under normal pressure or under vacuum.3. The method according to claim 1 , wherein said step of freeze drying said fresh food product is performed by combining vacuum process to said food product to remove moisture content.4. The method according to claim 1 , wherein said incubation in step iii is performed under vacuum.5. The method according to claim 1 , further comprising the step of drying the soaked food product;6. The method according to claim 1 , wherein said food product is dehydrated in step (b) until the residual moisture extent is between about 0% to about 5%.7. The method according to claim 1 , wherein said residual moisture extent is selected from a group consisting of: about 0% claim 1 , about 1% claim 1 , about 2% claim 1 , about 3% claim 1 , about 4% claim 1 , about 5% of said food product volume.8. The method according to claim 1 , wherein at least one of the following is true;a. said material of interest is a natural pharmacological or bio-active material containing a definite tasteb. said material of interest includes any of phytochemicals or nutraceutical material, said nutraceutical material selected from a group consisting of; vitamins, minerals, isoflavoronals, lycopene, resveratol, indocarbonals, anthocyanins, soluble fiber, high protein rice, and soy isolate or any combination thereofc. said food product further comprises food additives selected from a group consisting of acids, acidity regulators, anticaking agents, antifoaming agents, antioxidants, bulking agents, food coloring, color retention agents, emulsifiers, flavors, flavor enhancers, flour treatment agents, glazing agents, humectants, tracer gas, stabilizers, preservatives, sweeteners, thickenersd. said taste additives are volatile ...

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Номер записи: 57
17-10-2013 дата публикации

ORALLY DISINTEGRATING TABLET

Номер: US20130274348A1
Автор: Kigoshi Makoto, Morita Hideki, Ota Motohiro, SATO Takafumi
Принадлежит: KYOWA HAKKO KIRIN CO., LTD.

It is an object of the present invention to provide an orally disintegrating tablet that has desirable oral disintegrability and excellent tablet hardness, a process for producing the same, and the like.

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Номер записи: 58
24-10-2013 дата публикации

Method of administration of active agents to non-human mammals

Номер: US20130280304A1
Автор: Douglas Kramer
Принадлежит: Individual

The present invention provides an improved method of administering a medicinal, dental or nutritional agent to a non-human animal, such as a domesticated dog or cat. The method comprises mixing a liquid composition in a mixer at various speeds and pressures for a period of time; pouring the liquid composition onto a conveyor belt propelled by polymer rollers, wherein the polymer rollers allow the components to advance on the conveyor belt without adhering to the belt; evenly distributing the composition on the belt with the use of a knife; heating the composition in one or more hot-air chambers; obtaining a film comprised of the composition; cutting the film into strips; and then administering one or more of the strips to the non-human animal by placing the strip under the tongue of the animal, i.e., by sub-lingual administration.

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Номер записи: 59
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: 60
31-10-2013 дата публикации

CYCLOPROPYLAMINE INHIBITORS OF OXIDASES

Номер: US20130289076A1
Автор: Fyfe Matthew Colin Thor, Laria Julio Castro-Palomino, Muñoz Alberto Ortega, Pedemonte Marc Murtinell, Valls Vidal Núrla
Принадлежит:

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer. 24-. (canceled)5. The compound of wherein G is aryl or heteroaryl.6. The compound of wherein G is phenyl claim 5 , indolyl or indazolyl.79-. (canceled)10. The compound of claim 1 , wherein G is phenyl.11. The compound of claim 1 , wherein E is —X═X—.12. The compound of wherein one of X claim 11 , X claim 11 , X claim 11 , and Xis N or C(R2) and the other ones of X claim 11 , X claim 11 , X claim 11 , and Xare each independently C(R2).13. The compound of claim 11 , wherein one of X claim 11 , X claim 11 , Xand Xis N and the other ones of X claim 11 , X claim 11 , Xand Xare each independently C(R2).14. The compound of wherein Xis N claim 13 , and X claim 13 , Xand Xare each independently C(R2).15. (canceled)16. The compound of claim 1 , wherein each R1 is independently chosen from lower alkyl claim 1 , lower alkynyl claim 1 , amido claim 1 , halo claim 1 , lower haloalkyl claim 1 , cyano claim 1 , hydroxyl claim 1 , or alkoxy.1718-. (canceled)19. The compound of claim 1 , wherein each R2 is —H.20. The compound of claim 1 , wherein n is 0 or 1.21. (canceled)22. The compound of claim 1 , wherein the compound of Formula (I) is in the trans configuration in respect of the substituents on the cyclopropyl ring.23. The compound of claim 1 , wherein said compound is chosen from:5-((trans)-2-aminocyclopropyl)-N-(3-chlorophenyl)pyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-(4-chlorophenyl)pyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-(4-(trifluoromethyl)phenyl)pyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-(3-methoxyphenyl)pyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-(4-methoxyphenyl)pyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-p-tolylpyridin-2-amine;5-((trans)-2-aminocyclopropyl)-N-m-tolylpyridin-2-amine;4-(5-((trans)-2-aminocyclopropyl)pyridin-2-ylamino ...

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Номер записи: 61
31-10-2013 дата публикации

FORMULATION COMPRISING ARGININE, USE AND PREPARATION THEREOF

Номер: US20130289119A1
Автор: Bosi Emanuele, Casiraghi Maria Cristina, Monti Lucilla Domenica, Pagani Maria Ambrogina, Piatti Piermarco, Quaglia Lucio, Setola Emanuela
Принадлежит:

The present invention relates to an edible formulation comprising the following ingredients (% on mix) 19 to 30 weight % of a dietary supplement comprising at least 50% of L-arginine, 20 to 35 weight % of cereal flakes, 14 to 25 weight % of puffed brown or white rice, 12 to 24 weight % of nuts, 9 to 18 weight % of orange rind (or dried fruit such as cranberries, blueberries, raspberry, blackberry) and 2 to 10 weight % of water and/or fruit juice, its use and process of preparation. 1. An edible formulation comprising the following ingredients (% on mix):19 to 30 weight % of a dietary supplement comprising at least 50% of L-arginine or a physiologically acceptable salt thereof,20 to 35 weight % of cereal flakes,14 to 25 weight % of puffed brown or white rice,12 to 24 weight % of nuts,9 to 18 weight % of orange rind (or dried fruit such as cranberries, blueberries, raspberry, blackberry), and2 to 10 weight % of water and/or fruit juice.2. The edible formulation according to comprising the following ingredients (% on mix):20 to 25 weight % of a dietary supplement comprising at least 50% of L-arginine or a physiologically acceptable salt thereof,24 to 28 weight % of cereal flakes,16 to 20 weight % of puffed brown or white rice,15 to 19 weight % of nuts,11 to 15 weight % of orange rind (or dried fruit such as cranberries, blueberries, raspberry, blackberry), and4 to 8 weight % of water and/or fruit juice.3. The edible formulation according to being in the form of a food product or a dietary supplement.4. The edible formulation according to wherein the food product is in the form of a biscuit or a bar snack.5. The edible formulation according to comprising in % wet weightat least 10 ww % of L-arginine or a physiologically acceptable salt thereof,5 to 10 ww % of proteins,25 to 32 ww % of starch,6 to 8 ww % of sugars,9 to 12 ww % of total fat, and4 to 7 ww % of total dietary fibers.6. The edible formulation according to comprising in % wet weight:11 to 15 ww % of L-arginine ...

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Номер записи: 62
07-11-2013 дата публикации

FLASHMELT ORAL DOSAGE FORMULATION

Номер: US20130296337A1
Автор: Desai Divyakant S., Kothari Sanjeev H.
Принадлежит:

There is provided granules for the production of flash-melt pharmaceutical oral dosage forms. In addition to one or more medicaments, the granules are composed of an excipient combination consisting of a superdisintegrant, a dispersing agent, a distributing agent, and a binder and may also include other conventional ingredients such as sweetening and flavoring agents. The subject granules are advantageous in that they are stable and can be prepared without the aid of solvents and without the need for special environments or handling. Dosage forms, especially tablets, prepared therefrom on conventional equipment disintegrate in the mouth in under about twenty five seconds. 1. A flash-melt pharmaceutical dosage form comprising a medicament , a superdisintegrant , a dispersing agent and a binder wherein said medicament is aripiprazole and wherein said dispersing agent is calcium silicate and wherein said superdisintegrant is selected from the group of crospovidone and croscarmellose sodium.2. A flash-melt pharmaceutical dosage form according to wherein said dispersing agent comprises from about 20 to about 70 percent by weight of said dispersing agent based on the total weight of said dosage form.3. A flash-melt pharmaceutical dosage form according to wherein said dispersing agent comprises from about 35 to about 45 percent by weight of said dispersing agent based on the total weight of said dosage form.4. A flash-melt pharmaceutical dosage form according to wherein greater than 50 percent of said dispersing agent by weight is comprised of calcium silicate.5. A flash-melt pharmaceutical dosage form according to wherein greater than 80 percent of said dispersing agent by weight is comprised of calcium silicate.6. A flash-melt pharmaceutical dosage form according to wherein said calcium silicate is orth- claim 1 , meta- or alpha triclinic-calcium silicate.7. A flash-melt pharmaceutical dosage form according to wherein said calcium silicate is comprised of a combination ...

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Номер записи: 63
07-11-2013 дата публикации

SUBLINGUAL FENTANYL SPRAY

Номер: US20130296368A1
Автор: Goskonda Venkat R., Kattookaran Linet, Kottayil S. George, Parikh Neha, Zhu Zhongyuan
Принадлежит:

The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable sale thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations. 1. A sublingual formulation comprising an effective amount of fentanyl and at least one pharmaceutically acceptable excipient , the formulation providing a mean Tof about 1.28+/−0.60 hours when a dose is administered sublingually to humans.2. The sublingual formulation of claim 1 , which provides a plasma concentration after administration to humans selected from the group consisting of: about 60% of the mean Cin about 10 minutes claim 1 , about 86% of the mean Cby about 20 minutes and a combination thereof.3. The sublingual formulation of claim 1 , that when administered to humans provides a plasma concentration that is greater than about 80% of the mean Cfor about 2 hours. This application is a continuation of U.S. patent application Ser. No. 12/221,333 filed Aug. 1, 2008, which claims the benefit of U.S. Provisional Application Nos. 60/963,076, filed on Aug. 2, 2007 and 60/963,253 filed Aug. 3, 2007; the disclosures of which are hereby incorporated by reference in their entireties.The invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable salt thereof, or derivative thereof, suitable for administration to humans, and methods for treatment with the sublingual formulations.Fentanyl is a μ-opioid receptor agonist with analgesic potency approximately 80-100 times that of morphine. In clinical settings, fentanyl exerts its principal pharmacologic effects on the central nervous system. Its primary actions are analgesic and sedation.The analgesic effects of fentanyl are related to the blood level of the drug. In general, the minimum effective concentration and the concentration at which toxicity occurs rise with increasing tolerance to any and all opioids. The rate of development of ...

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Номер записи: 64
07-11-2013 дата публикации

Fast Dissolving Tablet

Номер: US20130296385A1
Автор: Abu-Izza Khawka Abdullah, Kinter Kevin Scott, Li Vincent H., Szamosi Janos
Принадлежит:

The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided. 131-. (canceled)32. A tablet consisting of a fast dissolve granulation , an active ingredient , corn starch , one saccharide selected from the group of sorbitol , glucose , dextrose , fructose , maltose , xylitol , sucrose , lactose , glucose , galactose , mannitol , a dextrate and a maltodextrin and at least one non-saccharide containing excipient selected from the group consisting of a sowing agent , a sweetening agent , crosscarmellose sodium , a flavoring agent , a disintegrant , a glidant and a silicon dioxide ,wherein said fast dissolve granulation consists essentially of some or all of said one saccharide and one or more low melting point compound that melts or softens at or below 37° C.,wherein the said one or more low melting point compound comprises less than about 20% (wt/wt) of the fast dissolve granulation and from about 0.01% to about 2.5% (wt/wt) of the tablet, andwherein the tablet has a hardness of less than 0.5 kP.33. The tablet of wherein the one saccharide is mannitol.34. The tablet of wherein the one or more low melting point compound is one or more compounds selected from the group consisting of hydrogenated oil and partially hydrogenated oil.35. The tablet of wherein the hydrogenated oil or partially hydrogenated oil is a vegetable oil.36. A tablet consisting of a fast dissolve granulation claim 34 , an active ingredient claim 34 , corn starch claim 34 , one saccharide selected from the group of sorbitol claim 34 , glucose claim 34 , dextrose claim 34 , ...

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Номер записи: 65
07-11-2013 дата публикации

NOVEL PHOTOINITIATORS

Номер: US20130296577A1
Автор: Anderson David George, Madsen Niels Joergen, Nielsen Christian B., Sehnal Petr
Принадлежит: COLOPLAST A/S

Novel photoinitiators provide for polyurethane formation, in which a photoinitiator moiety and a tertiary amine are incorporated into the photoinitiator structure, and thus the polyurethane polymer.

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Номер записи: 66
21-11-2013 дата публикации

FAST DISSOLVING PHARMACEUTICAL COMPOSITION

Номер: US20130310319A1
Автор: Ahuja Varinder, Gunjikar Tejas, Gupta Shweta, Wannerberger Kristin
Принадлежит: FERRING B.V.

The subject invention is directed to a pharmaceutical composition comprising an open matrix network carrying a pharmaceutically active ingredient, wherein the open matrix network comprises levan. 131-. (canceled)32. A pharmaceutical composition comprising an open matrix network comprising a pharmaceutically active ingredient and levan , the pharmaceutical composition having a tensile strength of about 0.05-1.6 N/mmand a rapid dissolution rate such that at least 80% of the composition is dissolved in an aqueous medium or saliva within 30 seconds.33. A pharmaceutical composition according to wherein the composition dissolves in an aqueous medium or saliva within 10 seconds.34. A pharmaceutical composition according to claim 32 , in an oral dosage form.35. A pharmaceutical composition according to obtainable by sublimating solvent from a liquid preparation comprising the active ingredient and levan.36. A pharmaceutical composition according to wherein the active ingredient is desmopressin acetate.37. A pharmaceutical composition according to claim 32 , wherein the active ingredient is desmopressin.38. A pharmaceutical composition according to claim 32 , wherein the active ingredient is famotidine.39. A pharmaceutical composition according to claim 32 , wherein the active ingredient is montelukast sodium.40. A pharmaceutical composition according to claim 32 , wherein the active ingredient is ondansetron.41. A pharmaceutical composition according to wherein the active ingredient is loratidine.42. A pharmaceutical composition according to which is adapted for sublingual administration.43. A pharmaceutical composition according to claim 35 , wherein the sublimation is carried out by freeze drying the preparation.44. A process for preparing a pharmaceutical composition comprising at least a step of sublimating solvent from a liquid preparation comprising a pharmaceutically active ingredient and levan.45. A process according to claim 44 , comprising: (a) introducing unit ...

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Номер записи: 67
21-11-2013 дата публикации

SOLID-IN-OIL DISPERSIONS

Номер: US20130310457A1
Автор: Ramesh Niral
Принадлежит:

A grain free solid-in-oil dispersion comprising a medium chain fatty acid (MCFA), at least one polyunsaturated fatty acid (PUFA), and at least one solid, is provided. The dispersion compositions are useful for preparing dosage forms, dietary supplements and foods that provide health benefits. 1. A grain free solid-in-oil dispersion comprising at least one medium chain fatty acid (MCFA) , at least one polyunsaturated fatty acid (PUFA) , at least one solid ,wherein the dispersion is a grain free food product hat provides health benefits.2. The solid-in-oil dispersion of claim 1 , wherein the medium chain fatty acid comprises from about 35% to about 90% by weight of total fat in the dispersion claim 1 , and the polyunsaturated fatty acid (PUFA) comprises from about 10% to about 65% of by weight of total fat in the dispersion claim 1 , or acceptable salts thereof;wherein the solid is at least about 50% by weight of the dispersion composition and is an insoluble drug, an isolated protein, a flour, or acceptable salts thereof; andoptionally further comprising one or more of dietary carriers, preservative agents or adjuvants.3. The solid-in-oil dispersed composition of claim 1 , wherein the polyunsaturated fatty acid (PUFA) is ethyl eicosapentaenoic acid (Ethyl EPA) claim 1 , linolenic acid (LA) claim 1 , arachidonic acid (AA) claim 1 , docosahexaenoic acid (DHA) claim 1 , alpha-linolenic acid (ALA) claim 1 , stearadonic acid (STA) claim 1 , eicosatrienoic acid (ETA) claim 1 , docosapentaenoic acid (DPA) or a nutraceutically acceptable salt or derivative thereof.4. The solid-in-oil dispersion of claim 1 , wherein the solid is protein claim 1 , flour claim 1 , carrier or an insoluble active agent.5. The solid-in-oil dispersion of claim 1 , wherein the medium chain fatty acid is from a whole food such as coconut flour claim 1 , palm drupe flour claim 1 , or camphor drupe flour.6. The solid-in-oil dispersion of claim 1 , wherein the polyunsaturated fatty acid (PUFA) is ...

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Номер записи: 68
28-11-2013 дата публикации

ORAL ANESTHESIA APPLICATION

Номер: US20130315842A1
Автор: Skigen Andrew L.
Принадлежит:

The present invention provides methods of administering an active agent to a localized mucous membrane in the oral cavity of a mammal, as well as oral dissolving film formed therefore. 1. A method of applying an active agent to a specific site on a mammalian mucous membrane , the method comprising the steps of:selecting an oral dissolving film comprising an active agent;identifying a specific area on a mammalian mucous membrane for treatment by the active agent;placing the oral dissolving film comprising active agent on the identified area; andtreating the identified area with the active agent comprised in the oral dissolving film, wherein the treating the identified area includes an injection or incision to the mammalian mucous membrane.2. The method of wherein the identified area comprises tissue within a mammalian oral cavity.3. The method of additionally comprising the step of administering an injection into specific area.4. The method of wherein the active agent comprises a topical anesthetic and the injection comprises administration of an additional anesthetic.5. The method of wherein the active agent comprises ethyl ester of p-aminobenzoic acid.6. The method of wherein the active agent comprises benzocaine.7. The method of wherein the active agent comprises one or more of: butamben claim 1 , dibucaine claim 1 , lidocaine claim 1 , oxybuprocaine claim 1 , pramoxine claim 1 , proparacaine claim 1 , tetracaine and proxymetacaine.8. The method of claim 1 , wherein the active agent comprises a nutraceutical.9. The method of claim 1 , wherein the active agent comprises a nutrient.10. The method of claim 1 , wherein the active agent comprises one or more of: an anti-fungal agent claim 1 , an antimicrobial agent and an antibacterial agent.11. The method of wherein the oral dissolving film additionally comprises a coloring agent and the method additionally comprises the steps of:coloring mucous membrane with the coloring agent;identifying an area treated by the ...

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Номер записи: 69
28-11-2013 дата публикации

Hydroxylated Tricyclic Compounds

Номер: US20130317114A1
Автор: Deng Bo-Liang, Gursahani Hema, Riggs-Sauthier Jennifer
Принадлежит: Nektar Therapeutics

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer. 13-. (canceled)512-. (canceled)14. The compound of claim 13 , wherein m is 2.20. The compound of claim 16 , wherein the compound is the (E) isomer.21. The compound of claim 16 , wherein the compound is the (Z) isomer.22. The compound of claim 16 , wherein n is an integer from 1 to 10.23. (canceled)24. A compound claim 16 , or at least one pharmaceutically acceptable salt thereof claim 16 , selected from:{'sub': '4', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '1', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '2', '(R)-5-(3-dimethylamino-propylidene)-100 mPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '6', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '8', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '4', '(S)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '6', '(S)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '8', '(S)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-E-ene;'}{'sub': '4', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-Z-ene;'}{'sub': '6', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-Z-ene;'}{'sub': '8', '(R)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11-dihydro-5H-dibenzo[a,d]cyclohept-Z-ene;'}{'sub': '4', '(S)-5-(3-dimethylamino-propylidene)-10-OmPEG-10,11- ...

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Номер записи: 70
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: 71
12-12-2013 дата публикации

ZEAXANTHIN-ENRICHED POULTRY EGG

Номер: US20130330298A1
Автор: Ikarashi Michihisa, Kawashima Yuki, Nagai Hidetada
Принадлежит: JX NIPPON OIL & ENERGY CORPORATION

An object of the present invention is to provide zeaxanthin-enriched poultry eggs containing zeaxanthin at high concentrations. The present invention specifically relates to zeaxanthin-enriched poultry eggs obtained by feeding poultry with a poultry feedstuff containing zeaxanthin-producing bacteria. 1. A poultry egg containing zeaxanthin in yolk at 3.5 mg to 10 mg per 100 g of yolk.2. The poultry egg according to claim 1 , wherein the poultry are chickens.3. A zeaxanthin-enriched poultry egg claim 1 , which is obtained by feeding poultry with a poultry feedstuff containing zeaxanthin-producing bacteria.4Paracoccus.. The zeaxanthin-enriched poultry egg according to claim 3 , wherein the bacteria belong to the genus5. The zeaxanthin-enriched poultry egg according to claim 3 , wherein the amount of zeaxanthin in the feedstuff is 1 mg or more per 100 g of the feedstuff.6. The zeaxanthin-enriched poultry egg according to claim 3 , containing zeaxanthin in yolk at 1.5 mg to 10 mg per 100 g of yolk.7. The zeaxanthin-enriched poultry egg according to claim 3 , wherein the poultry are chickens.8. A method for producing a zeaxanthin-enriched poultry egg comprising a step of feeding poultry with a poultry feedstuff containing zeaxanthin-producing bacteria.9Paracoccus.. The method according to claim 8 , wherein the bacteria belong to the genus10. The method according to claim 8 , wherein the amount of zeaxanthin in the feedstuff is 1 mg or more per 100 g of the feedstuff.11. The method according to claim 8 , wherein the zeaxanthin-enriched poultry egg contains zeaxanthin in yolk at 1.5 mg to 10 mg per 100 g of yolk.12. The method according to claim 8 , wherein the poultry are chickens.13. A poultry feedstuff containing zeaxanthin-producing bacteria.14Paracoccus.. The poultry feedstuff according to claim 13 , wherein the bacteria belong to the genus15. The poultry feedstuff according to claim 13 , wherein the amount of zeaxanthin to be added is 1 mg or more per 100 g of the ...

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Номер записи: 72
12-12-2013 дата публикации

METHODS FOR THE TREATMENT OF THROAT DISCOMFORT

Номер: US20130330396A1
Автор: Cornec Michel, Correa Beth Ann, Harnish Michelle, Harvey Joan E., Lynch Caroline, Schwartz Danielle, Watson Deborah L.
Принадлежит: Intercontinental Great Brands LLC

The physiological cooling agent N-ethyl-2,2-diisopropylbutanamide exhibits a surprising selectivity for throat cooling over mouth cooling, especially when consumed in the form of a confection. Methods of treating throat discomfort using N-ethyl-2,2-diisopropylbutanamide are described. Also described are various confections that incorporate N-ethyl-2,2-diisopropylbutanamide, including hard candy confections, soft candy confections, and center-filled confections. 1. A method of treating throat discomfort , comprising administering to a subject in need thereof an effective amount of N-ethyl-2 ,2-diisopropylbutanamide.2. The method of claim 1 , wherein the effective amount of N-ethyl-2 claim 1 ,2-diisopropylbutanamide is administered in the form of a confection having a mass of about 2 to about 10 grams and comprising about 0.03 to about 0.4 weight percent of N-ethyl-2 claim 1 ,2-diisopropylbutanamide claim 1 , based on the weight of the confection.3. The method of claim 2 , wherein the confection further comprises at least 80 weight percent of a confectionery base.4. The method of claim 2 , wherein the confection is a hard candy confection.5. The method of claim 2 , wherein the confection further comprises about 0.005 to about 0.5 weight percent of monomenthyl glutarate claim 2 , N-ethyl-p-menthane-3-carboxamide claim 2 , or a combination thereof.6. The method of claim 5 , wherein the confection comprises monomenthyl glutarate.7. The method of claim 5 , wherein the confection comprises N-ethyl-p-menthane-3-carboxamide.8. The method of claim 2 , wherein the confection further comprises about 0.01 to about 0.2 weight percent menthol.9. The method of claim 2 , wherein the confection further comprises about 0.001 to about 0.02 weight percent eucalyptus oil.10. The method of claim 2 , wherein the confection is a hard candy confection.11. The method of claim 2 , wherein the confection is a soft candy confection.12. The method of claim 2 , wherein the confection is a center- ...

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Номер записи: 73
12-12-2013 дата публикации

AMINOTETRALINE DERIVATIVES

Номер: US20130331429A1
Автор: Gmeiner Peter, Huebner Harald, Ruberg Miriam
Принадлежит:

The present application relates generally to amino tetraline derivative compounds and methods of use, specifically, embodiments including compounds of formula (I) described herein, pharmaceutically acceptable salts and solvates. More specifically, this application relates to amino tetraline derivative compounds and uses of such compounds producing medicaments for the treatment of various disease and conditions including movement disorders and disorders of the central nervous system. 2. The method of claim 1 , wherein the movement disorder is an L-DOPA associated dyskinesia.3. The method of wherein R of the compound of formula I is OR1 claim 1 , wherein R1 is methyl claim 1 , hydrogen or a group —C(═O)R2 claim 1 , wherein R2 is (C1-C6)alkyl or (C1-C6)alkyloxy.4. The method of wherein Cy of the compound of formula I is a 5 or 6 membered aromatic or heteroaromatic ring which is selected from the group of phenyl claim 1 , thienyl claim 1 , furanyl claim 1 , imidazolyl claim 1 , 1 claim 1 ,2 claim 1 ,3-triazolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-triazolyl claim 1 , pyrazolyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , and unsubstituted or substituted with one or two groups R4.5. The method according to wherein the compound of formula I administered to a recipient is selected fromN-(8-Hydroxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,(R)—N-(8-Hydroxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,(S)—N-(8-Hydroxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,N-(8-Methoxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,(R)—N-(8-Methoxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,(S)—N-(8-Methoxytetralin-2-yl)-N-propyl-N-[2-(2-thienyl)ethyl]amine,N-[2-(4-Hydroxyphenyl)ethyl]-N-(8-hydroxytetralin-2-yl)-N-propylamine,N-[2-(4-Methoxyphenyl)ethyl]-N-(8-methoxytetralin-2-yl)-N-propylamine,N-[2-(2,5-Dimethylphenyl)ethyl]-N-(8-hydroxytetralin-2-yl)-N-propylamine,N-[2-(2,5-Dimethylphenyl)ethyl]-N-(8-methoxytetralin-2-yl)-N-propylamine,N-[2-(1- ...

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Номер записи: 74
19-12-2013 дата публикации

PROCESS FOR THE PRODUCTION OF AMINO ALCOHOLS

Номер: US20130338401A1
Автор: Tjosas Freddy
Принадлежит: BORREGAARD AS

The present invention relates to a process for the manufacture of APD and N-alkyl-APD wherein 1-CPD is reacted with aqueous ammonium or aqueous alkyl-amine under alkaline conditions and where the process is conducted in a continuous manner in a reactor comprising a tubular reactor wherein at least two reaction zones are established. 1. Process for the manufacture of APD and N—C-C-alkyl-APD wherein comprising reacting 1-CPD is reacted with aqueous ammonium or aqueous C-C-alkyl-amine under alkaline conditions , characterized in that wherein the process is conducted in a continuous manner in a reactor comprising a tubular reactor , and wherein at least two reaction zones are established.2. Process of wherein the tubular reactor is a microreactor or a millireactor3. Process of claim 1 , wherein the reactor contains two separate reaction zones.4. Process of claim 1 , wherein a first reaction zone is adapted for the formation of glycidol by the reaction of 1-CPD in alkaline conditions.5. Process of claim 4 , wherein at reactor inlets of the first reaction zone claim 4 , 1-CPD and base are injected through separate inlets into a mixing zone at injection speeds sufficient to ensure thorough mixing of the reactants.6. Process of claim 4 , wherein alkali claim 4 , is added to keep the pH of the mixture between 10 and 13.7. Process of claim 4 , wherein the temperature in the first reaction zone of the tubular reaction is above ambient temperature.8. Process of claim 7 , wherein the temperature in the first reaction zone of the tubular reactor is up to about 60° C.9. Process of claim 7 , wherein the temperature in the first reaction zone of the tubular reactor is from about 35° C. to about 45° C.10. Process of claim 1 , wherein a second reaction zone is adapted for the formation of APD or N—C-C-alkyl-APD by the reaction of glycidol with ammonium or with C-C-alkyl-amine.11. Process of wherein at least 2 moles of ammonium or C-C-alkylamine are added per mole 1-CPD.12. Process of ...

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Номер записи: 75
16-01-2014 дата публикации

POUCH CONTAINING NICOTINE IN FREE SALT FORM

Номер: US20140017286A1
Автор: Nilsson Per-Gunnar
Принадлежит: CHILL OF SWEDEN AB

The invention relates to a product for oral delivery of nicotine containing a core comprising a powder of at least one free nicotine salt, at least one pH adjusting agent and at least one filler, and a water insoluble pouch, wherein said pouch is permeable for saliva and therein dissolved parts of the powder, wherein said product upon contact with purified water gives a pH of at least 6. The invention also relates to a method to manufacture such a product. 2. The product according to claim 1 , wherein said nicotine salt is water soluble.3. The product according to claim 1 , wherein said nicotine salt is selected from the group consisting of nicotine hydrochloride claim 1 , nicotine dihydrochloride claim 1 , nicotine monotartrate claim 1 , nicotine bitartrate claim 1 , nicotine bitartrate dihydrate claim 1 , nicotine sulphate claim 1 , nicotine zinc chloride monohydrate and nicotine salicylate claim 1 , and mixtures thereof.4. The product according to claim 3 , wherein said nicotine salt is nicotine bitartrate dihydrate.5. The product according to claim 1 , wherein said pH adjusting agent is selected from the group consisting of carbonates including monocarbonate claim 1 , bicarbonate and sesquicarbonate claim 1 , acetates claim 1 , glycinates claim 1 , gluconates claim 1 , borates claim 1 , glycerophosphates or citrates of alkaline metals or ammonium claim 1 , phosphate systems including monohydrogenphosphate claim 1 , dihydrogenphosphate and trihydrogenphosphate claim 1 , metal hydroxides such as sodium hydroxide and potassium hydroxide claim 1 , and mixtures thereof.6. The product according to claim 5 , wherein said pH adjusting agent is sodium bicarbonate or sodium carbonate claim 5 , and mixtures thereof.7. The product according to claim 5 , wherein said pH adjusting agent is encapsulated or embedded.8. The product according to claim 7 , wherein said pH adjusting agent is encapsulated or embedded with a polymer which physically separates the pH adjusting agent ...

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Номер записи: 76
16-01-2014 дата публикации

GELATIN-FREE, ISOMALTULOSE-CONTAINING SOFT CARAMEL

Номер: US20140017346A1
Автор: Bernard Jorg, Jorg Kowalczyk
Принадлежит: Südzucker Aktiengesellschaft Mannheim/Ochsenfurt

Disclosed is a gelatin-free soft caramel including a soft caramel base mass that contains at least one polysaccharide hydrocolloid as texturing agent, a crystalline sweetener phase formed by isomaltulose, and a noncrystalline sweetener phase, wherein the caramel is gelatin-free. It can be made by providing a noncrystalline sweetener phase by dissolving at least one soluble sweetener in water, adding polysaccharide hydrocolloid, fat component, emulsifier and a part of the total amount of the isomaltulose to the noncrystalline sweetener phase, steam heating the mixture to a temperature of at least 100° C., adding the remaining isomaltulose to the heated mixture while stirring, incorporating air into the mixture and cooling. 1. A method for producing a gelatin free isomaltulose containing soft caramel that comprisesa) preparing a noncrystalline sweetener phase by dissolving at least one soluble sweetener in water,b) adding at least one polysaccharide hydrocolloid, at least one fat component, at least one emulsifier, and a part of the total amount of a crystalline sweetener phase to the noncrystalline sweetener phase, wherein the crystalline sweetener phase is formed by isomaltulose,c) steam heating the mixture obtained in (b) to a temperature of at least 100° C.,d) adding the remaining isomaltulose to the heated mixture while stirring,e) incorporating air into the mixture obtained in (d) andf) cooling the mixture.2. A method as in claim 1 , where 70% to 90% of the total amount of isomaltulose is added to the noncrystalline sweetener phase.3. A method as in claim 2 , where 74% to 85% of the total amount of isomaltulose is added to the noncrystalline sweetener phase.4. A method as in claim 3 , where the mixture containing the noncrystalline sweetener phase is heated to 110° C.5. A method as in claim 1 , where the mixture containing the noncrystalline sweetener phase is heated to 110° C.6. A method as in claim 1 , where after heating the mixture containing the ...

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Номер записи: 77
06-02-2014 дата публикации

METHODS FOR THE TREATMENT OF DIABETIC RETINOPATHY AND OTHER OPHTHALMIC DISEASES

Номер: US20140039048A1
Автор: Bavik Claes Olof, Henry Susan Hayes, Kubota Ryo, Kuksa Vladimir A.
Принадлежит: Acucela Inc.

Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions. 2. (canceled)3. (canceled)4. The method of claim 1 , wherein n is 0 claim 1 , 1 claim 1 , or 2.5. (canceled)6. (canceled)7. The method of claim 4 , wherein X is —C(R)—O—.8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. The method of claim 7 , wherein Y is substituted or unsubstituted carbocyclyl claim 7 , or substituted or unsubstituted C-Calkyl.13. The method of claim 12 , wherein Y is substituted or unsubstituted carbocyclyl.14. The method of claim 12 , wherein Y is substituted or unsubstituted C-Calkyl.15. The method of claim 13 , wherein the substituted or unsubstituted carbocyclyl is a substituted or unsubstituted 4- claim 13 , 5- claim 13 , 6- claim 13 , or 7-membered ring.16. The method of claim 14 , wherein the substituted or unsubstituted C-Calkyl is a substituted or unsubstituted C-Calkyl.17. The method of claim 16 , wherein the substituted C-Calkyl is substituted with an C-Calkoxy group.18. The method of claim 18 , wherein the substituted C-Calkyl is —CHCHCHOCH.19. The method of claim 15 , wherein the substituted or unsubstituted carbocyclyl is a 6-membered ring.20. The method of claim 19 , wherein the substituted or unsubstituted 6-membered ring is a substituted or unsubstituted cyclohexyl.21. (canceled)22. The method of claim 1 , wherein Ris hydrogen and Ris hydroxyl.23. The method of claim 1 , wherein Rand Rform an oxo.24. The method of claim 1 , wherein Ris hydrogen.25. The method of claim 1 , wherein Ris methyl.26. (canceled)27. ( ...

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Номер записи: 78
06-02-2014 дата публикации

PROCESS FOR PREPARING FESOTERODINE

Номер: US20140039216A1
Автор: Ladani Mahesh, Parekh Viral, Patel Ronak, Patel Samir, PATIL Chetan, Raman Jayaraman Venkat, Raval Prashant, Shah Hiral, Thakor Indrajit
Принадлежит: ALEMBIC PHARMACEUTICALS LIMITED

The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+)benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol. 2. A process according to claim 1 , wherein resolution of racemic compound of formula (III) through formation of the diastereomeric salt thereof with an optically active acid claim 1 , which may be selected from an optically active acid is an optically active carboxylic acid or sulphonic acid.3. (canceled)4. A process according to claim 2 , wherein an optically active acid is selected from (+) tartaric acid claim 2 , (−) tartaric acid claim 2 , (+) 2 claim 2 ,3-dibenzoyl-D-tartaric acid claim 2 , (−) 2 claim 2 ,3-dibenzoyl-L-tartaric acid claim 2 , mandelic acid claim 2 , 3-chloro mendalic acid claim 2 , abietic acid claim 2 , S-(+)-camphorsulfonic acid claim 2 , di-p-tolyl-D-tartaric acid and di-p-tolyl-L-tartaric acid.5. (canceled)6. A process according to claim 1 , wherein the resolution of racemic compound of formula (III) is carried out in a solvent selected from water claim 1 , a dipolar aprotic solvent claim 1 , a C3-C8 ketone claim 1 , a cyclic or acyclic ether claim 1 , an ester claim 1 , a chlorinated solvent and a polar protic solvent claim 1 , or a mixture claim 1 , of two or more typically two claim 1 , of said solvents claim 1 , more preferably isopropyl alcohol.7. (canceled)8. (canceled)10. An acid addition salt according to claim 9 , wherein said addition salt is selected from hydrochloride claim 9 , hydrobromide claim 9 , sulfate claim 9 , methanesulfonate claim 9 , phosphate claim 9 , nitrate claim 9 , benzoate claim 9 , citrate claim 9 , tartarate claim 9 , fumarate or maleate.1315.-. (canceled)17. The process of claim 16 , ...

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Номер записи: 79
20-02-2014 дата публикации

Morpholinoalkyl Fumarate Compounds, Pharmaceutical Compositions, and Methods of Use

Номер: US20140051705A1
Автор: Cundy Kenneth C., Manthati Suresh K., Wustrow David J.
Принадлежит: XenoPort, Inc.

Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 131-. (canceled)33. A compound of claim 32 , wherein n is 2.34. A compound of claim 32 , wherein Q is a morpholino group.35. A compound of claim 32 , wherein the compound is a pharmaceutically acceptable salt.36. A compound according to claim 32 , wherein the compound is a HCl salt.37. A pharmaceutical composition comprising a pharmaceutically acceptable vehicle and a therapeutically effective amount of a compound of .38. A method for treating in a mammal in need thereof a disease or condition which comprises administering to the mammal an effective disease-treating or condition-treating amount of a compound of .39. The method of claim 38 , wherein the disease or condition is selected from a neurodegenerative disease claim 38 , an inflammatory disease claim 38 , and an autoimmune disease.40. The method of claim 38 , wherein the disease or condition is selected from multiple sclerosis claim 38 , psoriasis claim 38 , irritable bowel disorder claim 38 , ulcerative colitis claim 38 , arthritis claim 38 , chronic obstructive pulmonary disease claim 38 , asthma claim 38 , Parkinson's disease claim 38 , Huntington's disease claim 38 , and amyotrophic lateral sclerosis.41. The method of claim 38 , wherein the disease or condition is multiple sclerosis.42. The method of claim 38 , wherein the disease or condition is psoriasis. This application is a continuation of U.S. patent application Ser. No. 13/761,864, filed Feb. 7, 2013, which claims the benefit of U.S. Provisional Patent Application No. 61/ ...

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Номер записи: 80
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: 81
20-03-2014 дата публикации

Suspension Pharmaceutical Formulations Comprising Low Melting Propionic Acid Derivative Particles

Номер: US20140080912A1
Автор: Murali K. Vuppala, Saumitra Bagchi
Принадлежит: McNeil PPC Inc

Low melting propionic acid derivative particles that are free flowing and have significantly reduced or eliminated throat burn are disclosed. A method of manufacturing the low melting propionic acid derivative particles; dosage forms containing the low melting propionic acid derivative particles; methods of manufacturing the dosage forms; and methods of treatment using the dosage forms are also disclosed.

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Номер записи: 82
20-03-2014 дата публикации

PROCESS FOR THE PREPARATION OF DEUTERATED COMPOUNDS CONTAINING N-ALKYL GROUPS

Номер: US20140081019A1
Автор: Atzrodt Jens, Beller Matthias, Derdau Volker, Holla Wolfgang, Michalik Dirk, Neubert Lorenz
Принадлежит: SANOFI

The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst. 1. A process for preparing a deuterated compound (II) containing at least one structural element of the formula N—C—C , which is not part of an aromatic ring system , and wherein the amount of deuterium at the carbon atom in the alpha position and/or the carbon atom in the beta position of the structural element is at least 1% , comprising reacting a compound (1) comprising a residue which contains at least one structural element N—C—C , wherein at least one H atom is at each carbon atom of the structural element and the N—C—C element is not part of an aromatic ring system , with a deuterium source in the presence of a catalyst of formula (2) 1-UH-tetra-Z-cyclopentadienyl-(tetra-Z-2 ,4-cyclopentadien-1-U)-μ-hydro-tetra-L-diruthenium(II) (2) , wherein{'sub': '5', 'UH is OH, NHR, or SH;'}{'sub': '5', 'U is O, NRor S;'}{'sub': 5', '1', '6', '2, 'Ris (C-C)alkyl, phenyl or —CH-phenyl;'}{'sub': 1', '6', '1', '6, 'Z is, independently of each other, (C-C)alkyl or phenyl, wherein each phenyl is optionally substituted by (C-C)alkyl or phenyl, wherein phenyl is optionally substituted 1 or more times by halogen, and'}L is CO, CN or COD.2. The process according to claim 1 , wherein the structural element in a compound (I) is N—C(H)—C(H)wherein m is 1 or 2 and n is 1 claim 1 , 2 or 3.3. The process according to claim 1 , wherein the structural element in a compound (I) is N—CH—CH.4. The process according to claim 1 , wherein the residue containing the structural element in compound (I) is —N(C)alkylene claim 1 , —NH(C-C)alkyl claim 1 , —N((C-C)alkyl)((C-C)alkyl) claim 1 , —(C-C)alkylene-N((C-C)alkyl) claim 1 , —(C-C)alkylene-N((C-C)alkyl)((C-C)alkyl)) or (C-C)heterocycloalkyl.5. The process according to claim 1 , wherein compound (I) is a compound of formula (I){'br': None, 'sub': 1', '1', '2', '3', '4 ...

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Номер записи: 83
20-03-2014 дата публикации

METHODS OF SYNTHESIZING 2- SUBSTITUTED-1,4-BENZENEDIAMINE

Номер: US20140081049A1
Автор: ANDERSON James S., GARDLIK John Michael, GARRETT Garry Steven, Murphy Bryan Patrick, SHUMATE Robert Edward, Zhang Guiru
Принадлежит: The Proctor & Gamble Company

Disclosed is a method of making a 2-substituted-1,4-benzenediamine by nucleophilic aromatic substitution. 2. The method of wherein the suitable alkali alkoxide is selected from the group consisting of sodium methoxide claim 1 , lithium methoxide claim 1 , potassium methoxide claim 1 , sodium ethoxide claim 1 , lithium ethoxide claim 1 , potassium ethoxide claim 1 , sodium propoxide claim 1 , lithium propoxide claim 1 , potassium propoxide and mixtures thereof.3. The method of wherein the suitable alkali hydroxide is sodium hydroxide or potassium hydroxide.4. The method of wherein the method further comprises dissolving a 4-nitro-2- (or 3-) haloalkyl moiety substituted chlorobenzene in an alcohol selected from methanol claim 1 , ethanol and propanol to form a solution and then mixing the solution with an alkali alkoxide claim 1 , alkali hydroxide and mixtures thereof.5. The method of wherein the suitable alkali alkoxide claim 4 , alkali hydroxide and mixtures thereof is present in an amount from about 10% to about 30% by weight of the solution. The subject matter of the present application relates to the synthesis of a 2-substituted-1,4-benzenediamine such as a 2-methoxymethyl-1,4-benzenediamine and physiologically compatible salts thereof.2-Substituted-1,4-benzenediamine and physiologically compatible salts thereof may be useful as primary intermediates in oxidative hair color. For example, 2-methoxymethyl-1,4-benzenediamine and physiologically compatible salts thereof are useful as primary intermediates in oxidative hair color. A current process for synthesizing 2-methoxymethyl-1,4-benzenediamine may be accomplished as discussed in U.S. Pat. No. 4,997,451 and U.S. Pat. No. 6,648,923. Such a process is illustrated by the following reaction scheme:However, it is still desired to find alternative processes that reduce costs of manufacturing the desired product. As such, there still exists a need to utilize less expensive starting materials to arrive at the desired ...

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Номер записи: 84
10-04-2014 дата публикации

POLYETHER COMPOUND, CURING AGENT USING THE POLYETHER COMPOUND, AND PRODUCING METHOD OF THE POLYETHER COMPOUND

Номер: US20140100390A1
Автор: AMAO Akihito, KITAGAWA Hirotaka
Принадлежит: FUJIFILM Corporation

Disclosed is a polyether compound which is useful as a curing agent or the like, a curing agent using the compound and a producing method of the compound. The polyether compound of the present invention is represented by the following general formula (1). 2. The polyether compound according to claim 1 , wherein Rrepresents a hydrogen atom in the general formula (1).3. The polyether compound according to claim 1 , wherein Rrepresents a hydrogen atom and Rrepresents —C(═O)—C(R)═CHin the general formula (1).4. A curing agent using the polyether compound according to .5. A curing agent using the polyether compound according to .6. A curing agent using the polyether compound according to . 1. Field of the InventionThe present invention relates to a polyether compound, a curing agent using the polyether compound and a producing method of the polyether compound.2. Description of the Related ArtAs a raw material of various kinds of polymers and curable resin compositions, a polymerizable compound which is polymerized and cured by imparting energy such as heat and light, is widely used for industrial uses such as coating materials, paints, printing inks, adhesive agents and resist materials.For example, an epoxy resin (an epoxy compound) is used in various fields such as an adhesive agent for civil engineering and constructions, a sealing agent for semiconductors, an insulating material for printed circuit boards, mold devices for high voltage power, or the like, paints for cans, automobiles, or the like due to its excellent characteristics and diversity.It is possible to improve the characteristics of an obtained molded body (a cured product) by using a polymerizable compound. For example, by the compound being polymerized to be a cured film by heating after an image is formed by using inks or paints containing a polymerizable compound which is cured by heat, an image which has an excellent weather resistance and durability can be created.Curing of the polymerizable ...

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Номер записи: 85
06-01-2022 дата публикации

Sublingual Epinephrine Compositions Including pH-Modifying Excipients And Penetration Enhancers And Methods for Use Thereof

Номер: US20220000806A1
Автор: RAWAS-QALAJI Mutasem
Принадлежит: NOVA SOUTHEASTERN UNIVERSITY

The invention provides sublingual epinephrine compositions including epinephrine fine particles formulated with pH-modifying excipients and penetration enhancers. The sublingual compositions are used to control absorption of epinephrine at the site of delivery in an oral cavity. The invention also provides methods for therapeutic use of the sublingual compositions for treatment of conditions responsive to epinephrine and/or for increasing sublingual bioavailability of epinephrine. 1. A sublingual composition formulated as a fast-disintegrating tablet , the sublingual composition comprising:epinephrine fine particles; andat least one of a pH-modifying excipient and a penetration enhancer.2. The sublingual composition according to claim 1 , wherein the epinephrine fine particles have a particle size distribution in a range (loin about 500 nm to about 2.5 μm.3. The sublingual composition according to claim 1 , wherein the epinephrine is epinephrine bitartrate.4. The sublingual composition according to claim 3 , wherein the epinephrine bitartrate is equivalent to a range of about 15 mg epinephrine to about 20 mg epinephrine.5. The sublingual composition according to claim 3 , wherein the epinephrine bitartrate is equivalent to about 15 mg epinephrine.6. The sublingual composition according to claim 3 , wherein the epinephrine bitartrate is equivalent to about 20 mg epinephrine.7. The sublingual composition according to claim 1 , wherein the epinephrine fine particles are epinephrine microparticles claim 1 , epinephrine microcrystals claim 1 , epinephrine nanoparticles claim 1 , or epinephrine nanocrystals.8. The sublingual composition according to claim 1 , wherein the pH-modifying excipient is an alkalizing excipient.9. The sublingual composition according to claim 1 , wherein the pH-modifying excipient is sodium carbonate claim 1 , sodium bicarbonate claim 1 , or calcium citrate.10. The sublingual composition according to claim 9 , wherein the pH-modifying excipient ...

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Номер записи: 86
03-01-2019 дата публикации

SELF-FILM-FORMING COMPOSITION FOR ORAL CARE

Номер: US20190000757A1
Автор: CALVO GUIRADO Jose, Cuñé Castellana Jordi, LAZARO MALLEN Elisabet, Luis, Mareque, MAREQUE BUENO Javier, SANTAS GUTIÉRREZ Jonatan
Принадлежит:

A self-film-forming composition in powder form, a reconstituted formula and a kit for oral use are provided, which allow an adequate colonization of the probiotic in the oral cavities together with a sufficient residence time to allow beneficial effects against the pathogens related with oral conditions. Thus, the items provided are useful for the prevention and/or treatment of a condition related to alterations of the oral microbiota, and specifically for peri-implantitis. The self-film-forming composition in powder form comprises at least a gelifier agent and/or at least a bioadhesive agent, and at least one lactic acid bacteria strain. 1. A self-film-forming composition in powder form , self-film-forming under agitation in the presence of a liquid medium , the composition comprising:(i) at least one gelifier agent in powder form,(ii) at least one bioadhesive agent in powder form, and(iii) at least one lactic acid bacteria strain in powder form,wherein (i), (ii) and (iii) are in a single or in separate containers;wherein the self-film-forming composition is administered topically;wherein the (i) at least one gelifier agent is in an amount to provide viscosity to the composition, and is selected from the group consisting of: (a) a starch, (b) a gum, (c) an algal polysaccharide, (d) a polysaccharide selected from the group consisting of pectin and maltodextrin, (e) a cellulose derivative, (f) a polypeptide selected from the group consisting of gelatin, collagen, and casein, and;wherein the (ii) at least one bioadhesive agent is in an amount to provide adhesiveness to the composition, and is selected from the group consisting of:(a) a gum, (b) an algal polysaccharide, (c) a cellulose derivative, (d) a polysaccharide selected from the group consisting of pectin and maltodextrin, and (e) a polymer selected from the group consisting of an acrylate-based polymer, a vinyl-based polymer and a cationic polysaccharide.2. The self-film-forming composition in powder form ...

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Номер записи: 87
03-01-2019 дата публикации

ABUSE DETERRENT SOFT CHEWABLE DRUG FORMULATIONS

Номер: US20190000766A1
Автор: Dixit Manesh A., Patel Mineshkumar, Patel Rushi, Pawar Vaibhav
Принадлежит: First Time US Generics LLC

The present disclosure relates to oral, abuse deterrent, edible soft chewable dosage forms for delivery of drugs that are susceptible to abuse to a human or animal subject. The dosage forms are provided as chewable tablets manufactured using a compression (tablet) press. The edible soft chew dosage forms can be administered to subjects that are unable to swallow conventional tablets or capsules whole. One or more abuse deterrent measures in the dosage forms prevent the conversion of the dosage form into a residue or extract suitable for non-oral administration, such as intranasal or intravenous abuse. The present disclosure also relates to processes of preparing the dosage form. Such soft chew dosage forms have hardness less than 2 kilopond, preferably less than 1 kilopond, more preferably no measurable hardness when measured with tablet hardness tester and friability less than 1%, preferably less than 0.5%, more preferably less than 0.1% for 100 rotations (per USP); 200 rotations or 300 rotations. 1. A solid , abuse-resistant , edible , semi-plastic unit dosage form comprising:a compressed tablet,said tablet including a pharmaceutically active drug substance with abuse-potential,said tablet having a hardness of less than about two kiloponds (2 kp) when measured on tablet hardness tester;said tablet having a friability of less than about one percent (1%) at one-hundred (100) rotations.2. The dosage form of as claimed in claim 1 ,said tablet including an ingredient that reduces the abuse-potential of the pharmaceutically active drug substance,said drug substance and said ingredient being conjugated.3. The dosage form of as claimed in claim 1 ,said tablet including an ingredient that regulates the: chemical stability; solubility; bioavailability; palatability; or combinations thereof of the pharmaceutically active drug substance,said pharmaceutically active drug substance and said ingredient being conjugated.4. The dosage form as claimed in claim 1 , a. at least one ...

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Номер записи: 88
04-01-2018 дата публикации

SUBLINGUAL AND BUCCAL FILM COMPOSITIONS

Номер: US20180000726A1
Автор: Bogue B. Arlie, Boone Bill J., Hariharan Madhusudan, Hilbert Samuel D., Myers Garry L., Sanghvi Pradeep
Принадлежит:

The present invention relates to products and methods for treatment of various symptoms in a patient, including treatment of pain suffered by a patient. The invention more particularly relates to self-supporting dosage forms which provide an active agent while providing sufficient buccal adhesion of the dosage form. Further, the present invention provides a dosage form which is useful in reducing the likelihood of diversion abuse of the active agent. 2. The individual film dosage units of claim 1 , wherein application of the individual dosage units to the oral mucosa results in different absorption of the agonist and the antagonist through the mucosa claim 1 , with an agonist Cmax of about 0.868 to about 6.94 ng/ml claim 1 , and an antagonist Cmax of about 32.5 to about 260 pg/ml. (put deleted into spec)3. The individual film dosage units claim 1 , wherein the polymeric matrix further comprises a cellulose selected from the group consisting of hydroxypropylmethyl cellulose claim 1 , hydroxymethyl cellulose claim 1 , hydroxypropyl cellulose claim 1 , carboxymethyl cellulose and combinations thereof.4. The individual film dosage units of claim 1 , further including a material selected from the group consisting of a sugar alcohol claim 1 , a flavor claim 1 , an acidulent claim 1 , a sweetener claim 1 , a color claim 1 , a taste-masking agent claim 1 , a controlled release agent and combinations thereof.54. The individual film dosage units of claim 1 , wherein the sugar alcohol is selected from the group consisting of maltitol claim 1 , sorbitol claim 1 , mannitol claim 1 , xylitol and combinations thereof.6. The individual film dosage units of claim 4 , wherein the acidulent is citric acid.7. The individual film dosage units of claim 4 , wherein the sweetener is selected from the group consisting of acesulfame-K claim 4 , saccharin claim 4 , aspartame claim 4 , sucralose and combinations thereof.8. The individual film dosage units of claim 4 , wherein the flavor is ...

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Номер записи: 89
04-01-2018 дата публикации

ORAL DISINTEGRATING TABLET

Номер: US20180000730A1
Автор: KAWABATA YOHEI, NAKATANI Manabu, Sawada Takeshi, Takasaki Hiroshi
Принадлежит:

A process for the preparation of an oral disintegrating tablet comprising the antihypertensive telmisartan and the tablet obtained by the process. 1. An oral disintegrating tablet having 150-740 mg comprising20-80 mg angiotensin II receptor antagonist telmisartan20-80 mg basic excipient selected from the group consisting of alkali metal hydroxides, basic amino acids and meglumine20-350 mg filler selected from the group consisting of cellulose, dibasic calcium phosphate anhydrous, erythritol, mannitol, microcrystalline cellulose, corn starch, and pregelatinized starch,20-150 mg coating agent of the first granulate selected from corn starch, pregelatinized starch, lactose, D-mannitol, erythritol or microcrystalline cellulose5-50 mg disintegrant selected from the group consisting of sodium starch glycolate, crospovidone, corn starch and pregelatinized starch2-20 mg surfactant/emulsifier poloxamer 1880.5-10 mg sweetener0.12-1.2 mg flow control agent light anhydrous silicic acid0-0.01 mg lubricant0-0.01 mg dye or pigmentwhereinthe basic excipient is meglumine;the filler is selected from the group consisting of cellulose, dibasic calcium phosphate anhydrous, erythritol, mannitol, microcrystalline cellulose corn starch and pregelatinized starch;the disintegrant is selected from the group consisting of sodium starch glycolate, crospovidone (cross-linked polyvinylpyrrolidone), corn starch and pregelatinized starch;the coating agent of the first granulate is selected from corn starch or pregelatinized starch;the lubricant is magnesium stearate;the sweetener is saccharin sodium;the dye or pigment is an iron oxide.2. The tablet of claim 1 , wherein the tablet contains 20 mg claim 1 , 40 mg or 80 mg amorphous telmisartan.3. A method of treating or preventing hypertension claim 1 , chronic stable angina claim 1 , vasospastic angina claim 1 , stroke claim 1 , myocardial infarction claim 1 , congestive heart failure claim 1 , diabetes claim 1 , dyslipidemia or dementia comprising ...

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Номер записи: 90
02-01-2020 дата публикации

Method of rapidly achieving therapeutic concentrations of triptans for treatment of migraines and cluster headaches

Номер: US20200000712A1
Автор: Donald Kellerman, Mahmoud Ameri, Peter C. Schmidt, Peter E. Daddona, Yi Ao
Принадлежит: Zosano Pharma Corp, Zp Opco Inc

Compositions, devices and methods employing therapeutic concentrations of a triptan for treatment of migraine are described.

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Номер записи: 91
02-01-2020 дата публикации

Controlled Absorption Water-Soluble Pharmaceutically Active Organic Compound Formulation for Once-Daily Administration

Номер: US20200000719A1
Автор: Counts David F., Cox Donald P., Dam Anup K., Stalhamer Michael E.
Принадлежит:

The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a watersoluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours. 126-. (canceled)27. A method of treating pain in a patient in need thereof comprising a step of administering to the patient a particulate composition comprising (i) naproxen, a pharmaceutically acceptable salt of said naproxen, or a combination thereof and', '(ii) a drug binding polymer comprising a silicified high density microcrystalline cellulose composed of 98% microcrystalline cellulose and 2% colloidal silicon dioxide, wherein said naproxen, said pharmaceutically acceptable salt of said naproxen, or said combination thereof is in reversible association with said drug binding polymer and in a weight ratio therewith of from about 20:1 to about 1:2; and, '(a) a biologically active core, said biologically active core comprising'}(b) a coat, said coat comprising a membrane-forming polymer, said membrane-forming polymer comprising ethylcellulose and surrounding said biologically active core, wherein the particulate ...

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Номер записи: 92
02-01-2020 дата публикации

CARBOXYLIC ACIDS FOR TREATING/PREVENTING NASAL CONGESTION

Номер: US20200000751A1
Автор: Ernst Bettina
Принадлежит: Proponent Biotech GmbH

The present invention relates to a pharmaceutical composition comprising a carboxylic acid or a pharmaceutically acceptable salt thereof as active ingredient for use in treating and/or alleviating and/or preventing nasal congestion, a viral infectious disease of the respiratory tract or an inflammation of the throat. Furthermore, the present invention relates to a method for treating and/or alleviating and/or preventing nasal congestion, viral infections of the respiratory tract and/or inflammation of the throat in. a patient, comprising administering an effective amount of a carboxylic acid or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a carboxylic acid or a pharmaceutically acceptable salt thereof to a patient in need thereof. In addition, the present invention relates to a method for alleviating the symptoms associated with nasal congestion, viral infections of the respiratory tract and/or inflammation of the throat comprising administering an effective amount of a carboxylic acid or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a carboxylic acid or a pharmaceutically acceptable salt thereof to a patient in need thereof. 114-. (canceled)15. A method for treating nasal congestion , viral infections of the respiratory tract , inflammation of the throat in a patient , or a combination thereof , the method comprising administering to a patient in need thereof an effective amount of a pharmaceutical composition comprising a carboxylic acid or a pharmaceutically acceptable salt thereof.1618-. (canceled)19. The method of claim 15 , wherein the carboxylic acid or a pharmaceutically acceptable salt thereof comprises between two and four carbon atoms.20. The method of claim 15 , wherein the carboxylic acid or pharmaceutically acceptable salt thereof is one or more of acetic acid claim 15 , propionic acid claim 15 , butyric acid claim 15 , isobutyric acid claim 15 , 2-hydroxyproirinic acid ...

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Номер записи: 93
02-01-2020 дата публикации

Method for Treating Epilepsy

Номер: US20200000752A1
Автор: Kang Jing-Qiong
Принадлежит:

Treatment of conditions with celastrol are disclosed herein. In particular, methods of administration of celastrol for the treatment of neurological and non-neurological disorders, including epilepsy are provided. 1. A method of treating a condition with reduced GABA , the method comprising:{'sub': 'A', 'administering celastrol to a subject in need of treatment for a condition with reduced GABA.'}2. The method of claim 1 , further comprising administering diazepam.3. The method of claim 1 , wherein the celastrol is administered orally claim 1 , intraperitoneally claim 1 , or intravenously.4. The method of claim 3 , wherein the celastrol is administered intraperitoneally in the range of 0.1 mg/kg to 0.5 mg/kg.5. The method of claim 3 , wherein the celastrol is administered orally at a daily dose of about 5-10 mg.6. The method of claim 1 , wherein the condition is epilepsy.7. The method wherein the epilepsy is selected from Dravet syndrome claim 6 , primary epilepsy or secondary epilepsy.8. The method of claim 1 , wherein the subject is an animal subject claim 1 , celastrol is provided in an animal food product claim 1 , and the administering comprises feeding the animal subject the animal food product.9. A method of treating a condition selected from neurological diseases claim 1 , central nervous system (CNS) disorders claim 1 , and inflammatory diseases claim 1 , the method comprising:administering celastrol to a subject in need of treatment for a neurological disease, a CNS disorder, or an inflammatory disease.10. The method of claim 9 , wherein the condition is selected from encephalitis claim 9 , Alzheimer's claim 9 , Parkinson's or Huntington's.11. The method of claim 9 , wherein the treatment delays seizure onset claim 9 , shortens seizure duration claim 9 , or reduces seizure severity.12. The method of claim 9 , wherein the administering comprises intermittent dosing.13. The method of claim 12 , wherein the celastrol is administered at 0.1 mg/kg to about 20 ...

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Номер записи: 94
02-01-2020 дата публикации

FAST ACTING ORALLY DISINTEGRATING FILM

Номер: US20200000773A1
Автор: LEE Catherine, WANG Chien-Chiao
Принадлежит:

A fast acting orally disintegrating film (ODF) for treatment of various medical conditions including emesis that has a simple formulation, easy to manufacture and has similar pharmacokinetic profile to currently commercially available orally administered drug products is provided. The ODF comprises an active pharmaceutical ingredient such as ondansetron or a pharmaceutical acceptable salt thereof in an amount of 2 to 24 mg, at least one hydrophilic film forming polymer in an amount of at least 8% by weight of the film, wherein the at least one hydrophilic film forming polymer is characterized by having a molecular weight of 5000 to 50000 Da, and a water soluble excipient in an amount of 10 to 30% by weight of the film. The present invention also provides a method for preparing the ODF that remains stable over a period of time under a normal pharmacologically storage condition and a method for treating or preventing various medical conditions such as nausea or vomiting or a treatment method mediated through antagonizing action of 5HT at 5-HT3 receptor by administering the ODF to a patient in need thereof. 125-. (canceled)26. An orally disintegrating film , comprising:ondansetron or a pharmaceutical acceptable salt thereof in an amount of about 2 to about 24 mg;a first hydrophilic film forming polymer in a total amount of from about 15% to about 50% by weight of said film, wherein said first hydrophilic film forming polymer is characterized by having a molecular weight of about 5000 Da to about 50000 Da and viscosity of about 3 cps or about 6 cps; anda second hydrophilic film forming polymer having a molecular weight between about 50000 Da to about 60000 Da and viscosity of about 15 cps,wherein said first hydrophilic film forming polymer is mixed with said second hydrophilic film forming polymer in a ratio from about 0.3:1 to about 7:1.27. The orally disintegrating film of claim 26 , comprising a mixture of said first hydrophilic film forming polymer to said second ...

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Номер записи: 95
07-01-2016 дата публикации

ANTIMICROBIAL COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20160002163A1
Автор: FAULKNER KATHERINE CASSIDY, Hurley Katherine Ann, WEIBEL Douglas Benjamin
Принадлежит:

Described herein are antimicrobial compounds identified via a high-throughput screen to identify compounds that produce anucleate cells in after cell division occurs. Compound 1 (5-nonyloxytryptamine) and its analogs are small molecule inhibitors of the nucleoid occlusion system and/or proteins that are responsible for maintaining the structure of the chromosome. The antimicrobial compounds are useful to treat bacterial infections as well as to inhibit bacterial growth. 2. A pharmaceutical composition comprising the antimicrobial compound of and a pharmaceutically acceptable excipient.3. The pharmaceutical formulation of claim 2 , in the form of a composition for topical administration.4. The pharmaceutical formulation of claim 2 , in the form of a composition for systemic administration.7. The method of claim 6 , wherein claim 6 , R is a substituted or unsubstituted C-Calkyl group claim 6 , a substituted or unsubstituted C-Calkenyl group claim 6 , or a substituted or unsubstituted C-Calkynyl group.8. The method of claim 7 , wherein claim 7 , R is a substituted or unsubstituted C-Calkyl group.9. The method of claim 8 , wherein R is substituted with one or more C-Calkyl groups claim 8 , C-Caryl claim 8 , and/or C-Carylalkyl groups.10. The method of claim 8 , wherein R is substituted with one or more C-Calkyl groups or a C-Caryl group.12. The method of claim 5 , wherein the bacteria causing the infection are Gram-negative bacteria claim 5 , Gram-positive bacteria claim 5 , or bacteria that are neither Gram-positive nor Gram-negative.13Escherichia coli, Pseudomonas aeruginosa, Candidatus liberibacter, Agrobacterium tumefaciens, Branhamella catarrhalis, Citrobacter diversus, Enterobacter aerogenes, Klebsiella pneumoniae, Proteus mirabilis, Salmonella typhimurium, Neisseria meningitidis, Serratia marcescens, Shigella sonnei, Shigella boydii, Neisseria gonorrhoeae, Acinetobacter baumannii, Salmonella enteriditis, Fusobacterium nucleatum, Veillonella parvula, Bacteroides ...

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Номер записи: 96
05-01-2017 дата публикации

DIETHER BASED BIODEGRADABLE CATIONIC LIPIDS FOR siRNA DELIVERY

Номер: US20170001947A1
Автор: Budzik Brian W., Colletti Steven L., Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

Disclosed herein are novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. The cationic lipids can demonstrate enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain coupled with inclusion of hydrolysable functionality in the lipid chains to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A cationic lipid of claim 1 , wherein:{'sup': 1', '2, 'Rand Rare each methyl;'}n is 0;{'sup': '5', 'sub': 4', '8', '4', '8, 'Ris independently selected from (C-C)alkylene and (C-C)alkenylene, said alkylene or alkenylene optionally substituted with one to three substituents selected from R′;'}{'sup': '6', 'sub': 1', '2, 'Ris (C-C)alkyl, said alkyl optionally substituted with one to three substituents selected from R′;'}{'sup': '2', 'Qis a bond or —C(O)O—;'}or a pharmaceutically acceptable salt or stereoisomer thereof.3. A lipid nanoparticle comprising a cationic lipid of .4. The lipid nanoparticle of claim 3 , wherein the lipid particle comprises oligonucleotides.5. The lipid nanoparticle of claim 4 , wherein the oligonucleotides are siRNA.6. A lipid nanoparticle comprising a cationic lipid of claim 1 , cholesterol claim 1 , DSPC and PEG-DMG. The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.Cationic lipids and the use of cationic lipids in lipid nanoparticles for the delivery of oligonucleotides, in particular siRNA and miRNA, have been previously disclosed. Lipid nanoparticles and use of lipid nanoparticles for the delivery of oligonucleotides, in ...

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Номер записи: 97
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: 98
01-01-2015 дата публикации

COMPOSITIONS AND METHODS OF MAKING RAPIDLY DISSOLVING IONICALLY MASKED FORMULATIONS

Номер: US20150004240A1
Автор: MCMAHEN Russell, TENGLER Mark
Принадлежит:

The present invention includes compositions and methods for reduce the taste of the drug in the drug resin complex. The composition may include one or more drug-resin complexes and a highly compressible, free-flowing pharmaceutical excipient. The resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth. 1. A taste-masked pharmaceutical composition comprising:a drug-resin complex and a highly compressible, free-flowing pharmaceutical excipient, wherein the resin is present in an amount effective to reduce the taste of the drug in the drug resin complex by more than about 15 percent relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient aids release of the drug-resin complex in the mouth.2. The composition of claim 1 , wherein the composition comprises a chewable tablet claim 1 , a solid claim 1 , a dissolvable or disintegrating tablet claim 1 , a liquid claim 1 , a gel claim 1 , a tab claim 1 , a capsule claim 1 , a powder claim 1 , a lotion claim 1 , a cream claim 1 , a gum claim 1 , a lozenge and combinations thereof.3. The composition of claim 1 , wherein the drug in the drug-resin complex comprises dextromethorphan claim 1 , codeine claim 1 , morphine claim 1 , hydrocodone claim 1 , hyoscyamine claim 1 , moguisteine claim 1 , pseudoephedrine claim 1 , chlorpheniramine claim 1 , phenylpropanolamine claim 1 , pharmaceutically acceptable salts of the same and combinations thereof.4. The composition of claim 1 , wherein the pharmaceutical composition is suitable for oral administration.5. The composition of claim 1 , further comprising one or more flavorants claim 1 , sweeteners claim 1 , coolants claim 1 , dyes claim 1 , ...

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Номер записи: 99
01-01-2015 дата публикации

ABUSE DETERRENT COMPOSITIONS AND METHODS OF USE

Номер: US20150005334A1
Автор: Aigner Stefan, Difalco Ray J., Shah Manish S.
Принадлежит:

Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties. 1. A method of treating , preventing , reducing the occurrence of , decreasing the severity or degree of , and/or reducing the signs and/or symptoms of a disease or condition in a subject in need thereof ,wherein the disease or condition is selected from the group consisting of: pain, sleep disorders, anxiety, attention deficit hyperactivity disorder, narcolepsy, and depression in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising at least one drug, at least one pH-dependent agent, and at least one pH-independent agent;wherein the composition is configured such that when a unit dosage of the composition is submerged in water and/or Simulated Gastric Fluid and kept in sustained contact with at least one other unit dosage of the composition for a time period selected from 15 minutes, 30 minutes, 1 hour, 6 hours, 12 hours, and 24 hours, the unit dosage has at least one of the following characteristics: (1) a weight gain of 0 to 25%; (2) an increase in thickness of 0 to 25%; and (3) an increase in mucoadhesive strength of 0 to 25%.2. The method of claim 1 , wherein the disease or condition is selected from the group consisting of: chronic pain or acute pain.3. The method of claim 1 , wherein the disease or condition is pain associated with claim 1 , secondary to claim 1 , or caused by osteoarthritis claim 1 , rheumatoid arthritis claim 1 , fibromyalgia claim 1 , migraine or other headache claim 1 , back-related disorder claim 1 , shingles claim 1 , stiffened joints claim 1 , physical trauma claim 1 , cardiovascular condition claim 1 , cancer claim 1 , sciatica claim 1 , kidney stones claim 1 , appendicitis claim 1 , neuralgia claim 1 , pancreatitis claim 1 , gout claim 1 , endometriosis claim 1 , stomach ulcers claim 1 , Crohn's ...

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Номер записи: 100