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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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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 72512. Отображено 100.
05-01-2012 дата публикации

Biological control of nanoparticle nucleation, shape and crystal phase

Номер: US20120003629A9
Принадлежит: University of Texas System

The present invention includes compositions and methods for selective binding of amino acid oligomers to semiconductor and elemental carbon-containing materials. One form of the present invention is a method for controlling the particle size of the semiconductor or elemental carbon-containing material by interacting an amino acid oligomer that specifically binds the material with solutions that can result in the formation of the material. The same method can be used to control the aspect ratio of the nanocrystal particles of the semiconductor material. Another form of the present invention is a method to create nanowires from the semiconductor or elemental carbon-containing material. Yet another form of the present invention is a biologic scaffold comprising a substrate capable of binding one or more biologic materials, one or more biologic materials attached to the substrate, and one or more elemental carbon-containing molecules attached to one or more biologic materials.

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12-01-2012 дата публикации

Acetals as perfuming ingredients

Номер: US20120010114A1
Принадлежит: Individual

Acetal derivatives of 2,2,3,6-tetramethyl-1-cyclohexane/ene-carbaldehyde of formula (I): for use in the perfumery industry as well as the resulting compositions or articles containing one or more of these compounds. In formula (I), one dotted line indicates the presence of a carbon-carbon single or double bond and the other dotted line indicates the presence of a carbon-carbon single bond, R 1 represents a hydrogen atom or a methyl or ethyl group; and each R, taken alone, simultaneously or independently, represents a C 1-3 alkyl or alkenyl group, or the R groups, taken together, represent a C 2-6 hydrocarbon group optionally including an oxygen atom.

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19-01-2012 дата публикации

Method of immobilizing and stretching a nucleic acid on a substrate

Номер: US20120016110A1
Принадлежит: Individual

The present invention relates to a method of immobilizing and stretching a nucleic acid on a silicon substrate, to nucleic acids and substrates prepared according to this method, to uses of the method and to uses of the nucleic acid and the substrate.

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26-01-2012 дата публикации

Derivatives of n-(arylamino)sulfonamides as inhibitors of mek

Номер: US20120022076A1
Принадлежит: Individual

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

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26-01-2012 дата публикации

Delayed release, oral dosage compositions that contain amorphous cddo-me

Номер: US20120022156A1
Принадлежит: Reata Pharmaceuticals Inc

Pharmaceutical formulations exhibit a desirably low Cmax, among other properties, that contain particles of amorphous bardoxolone methyl, either in pure form or in the form of a solid dispersion, admixed with particles of a hydrophilic binding agent. Such formulations possess the advantage of higher oral bioavailability, relative to formulations based on the crystalline form of bardoxolone methyl.

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02-02-2012 дата публикации

Nitroxide Free Radical Synergized Antineoplastic Agents

Номер: US20120029021A1
Автор: Errol V. Mathias, Yong Ba
Принадлежит: California State University

Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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23-02-2012 дата публикации

Intermediates in the enantioselective synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid

Номер: US20120046468A1

(S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration.

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15-03-2012 дата публикации

Isotopologues of thalidomide

Номер: US20120064004A1
Принадлежит: Celgene Corp

Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

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15-03-2012 дата публикации

Crystalline forms of the di-sodium salt of n-(5-chlorosalicyloyl)-8-aminocaprylic acid

Номер: US20120065128A1
Принадлежит: Emisphere Technologies Inc

The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.

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29-03-2012 дата публикации

Process for the preparation of cilastatin and sodium salt

Номер: US20120078009A1

An improved process for preparing Cilastatin Sodium including dissolving Cilastatin acid in a solvent using an organic base, adding sodium salt of a week acid and isolating Cilastatin Sodium.

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03-05-2012 дата публикации

Cross-Coupled Peptide Nucleic Acids for Detection of Nucleic Acids of Pathogens

Номер: US20120107794A1

The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

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03-05-2012 дата публикации

Disubstituted-aminodifluorosulfinium salts, process for preparing same and method of use as deoxofluorination reagents

Номер: US20120108801A1
Принадлежит: OMEGACHEM INC

The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.

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10-05-2012 дата публикации

Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid

Номер: US20120115920A1
Принадлежит: Theravance Inc

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

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17-05-2012 дата публикации

New salts

Номер: US20120122883A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

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17-05-2012 дата публикации

Polyunsaturated fatty acids for the treatment of diseases related to cardiovascular, metabolic and inflammatory disease areas

Номер: US20120122940A1
Принадлежит: Individual

The present disclosure relates to lipid compounds of the general formula (I): R1-O—C(R2)(R3)-X  (I) wherein R 1 is a C 10 -C 22 alkyl group, a C 10 -C 22 alkenyl group having 1-6 double bonds, or a C 10 -C 22 alkynyl group having 1-6 triple bonds; R 2 and R 3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic, and inflammatory disease area.

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17-05-2012 дата публикации

No-Carrier-Added Nucleophilic [F-18] Fluorination of Aromatic Compounds

Номер: US20120123120A1
Принадлежит: UNIVERSITY OF CALIFORNIA

Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.

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31-05-2012 дата публикации

Substituted acylanilides and methods of use thereof

Номер: US20120136052A1

This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

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07-06-2012 дата публикации

Targetted drug delivery to the bone

Номер: US20120142641A1
Принадлежит: NANYANG TECHNOLOGICAL UNIVERSITY

The present invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.

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07-06-2012 дата публикации

Method for synthesis of secondary alcohols

Номер: US20120142934A1
Принадлежит: National Tsing Hua University NTHU

A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.

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07-06-2012 дата публикации

Process for preparing pregabalin

Номер: US20120142949A1
Автор: B. S. Pradhan
Принадлежит: HELVETICA IND (P) Ltd

The invention relates to a process for preparing a compound of formula (I): wherein said process comprises hydrogenation of a compound of formula (II); under alkaline conditions, wherein R represents hydrogen or a labile group capable of being converted to hydrogen. The invention also relates to intermediates used in said process, to the use of said intermediates in the preparation of pregabalin and to a process for resolving racemic compounds of formula (I).

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21-06-2012 дата публикации

Trihydroxy polyunsaturated eicosanoid derivatives

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

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

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28-06-2012 дата публикации

Compounds and their use as BACE Inhibitors

Номер: US20120165347A1
Принадлежит: AstraZeneca AB

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

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05-07-2012 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20120172398A1
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.

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05-07-2012 дата публикации

Hydrophilized substrate, dispersion, and making method

Номер: US20120172611A1
Автор: Masahiro Amemiya
Принадлежит: Shin Etsu Chemical Co Ltd

A powder is hydrophilized by treating surfaces of particles with a hydrolyzable silyl group-containing acid anhydride compound, dispersing the surface treated particles in water, adding a base, and heating the dispersion for thereby hydrolyzing the acid anhydride moiety to open its ring and neutralizing the resultant carboxylic acid with the base. The hydrophilized powder is fully dispersible in aqueous media.

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19-07-2012 дата публикации

Process for preparation of phenyl carbamate derivatives

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

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

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16-08-2012 дата публикации

L-ornithine phenyl acetate and methods of making thereof

Номер: US20120208885A1
Принадлежит: Ocera Therapeutics Inc

Disclosed herein are forms of L-ornithine phenyl acetate and methods of making the same. A crystalline form may, in some embodiments, be Forms I, II, III and V, or mixtures thereof. The crystalline forms may be formulated for treating subjects with liver disorders, such as hepatic encephalopathy. Accordingly, some embodiments include formulations and methods of administering L-ornithine phenyl acetate.

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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20-09-2012 дата публикации

Iodine radiolabelling method

Номер: US20120237444A1
Автор: Michelle Avory
Принадлежит: Individual

The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.

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18-10-2012 дата публикации

Polymorphic forms of o-desmethyl-venlafaxine succinate

Номер: US20120264828A1
Принадлежит: Cadila Healthcare Ltd

The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.

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25-10-2012 дата публикации

Process for producing trans-1233zd

Номер: US20120271069A1
Принадлежит: Honeywell International Inc

Trans-1233zd, the trans-isomer of 1-chloro-3,3,3-trifluoropropene (HCFO-1233zd) can be used as blowing agents, solvents, cleaning agents, as well as monomers of macromolecule compounds, and can be prepared through the dehydrochlorination of 1,1,1-trifluoro-3,3-dichloropropane (HCFC-243fa) with the help of a catalyst. The present invention is directed to an integrated process is proposed to produce trans-1233zd from 243fa, which is consisted of the following four major unit operations: (1) Catalytic dehydrochlorination of 243fa into trans/cis-1233zd, (2) HCl recovery, (3) Catalytic isomerization of cis-1233zd into trans-1233zzd, and (4) Isolation of trans-1233zd.

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01-11-2012 дата публикации

Forms of cidofovir

Номер: US20120277191A1
Принадлежит: JOHNSON MATTHEY PLC

Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.

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08-11-2012 дата публикации

Intermediate compounds and processes for the preparation of tapentadol and related compounds

Номер: US20120283463A1
Принадлежит: Mapi Pharma Ltd

The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.

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15-11-2012 дата публикации

Method for isolating an alkanol from an aqueous biotransformation mixture

Номер: US20120285816A1
Принадлежит: BASF SE

The invention relates to the isolation of an alkanol from an aqueous biotransformation mixture, in that a) a first alkanol phase is obtained by means of distilling out an alkanol-water azeotrope from the aqueous biotransformation mixture and, if the azeotrope is a heteroazeotrope, phase separating the azeotrope and separating out an aqueous phase, b) a second alkanol phase is obtained by (i) liquid/liquid extracting the first alkanol phase using a solvent as an extracting agent, or (ii) azeotropic drying the first alkanol phase in the presence of the solvent as a carrier agent, and c) the second alkanol phase is fractionally distilled, producing a pure alkanol fraction. The biotransformation mixture is obtained, for example, by means of reducing an alkanol in the presence of an alcohol dehydrogenase. The method is adapted to the severe dilution of the products of value in the biotransformation mixture and works without long phase separation times when extracting by means of organic solvents.

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15-11-2012 дата публикации

Certain Compounds, Compositions and Methods

Номер: US20120289475A1
Принадлежит: Eisai Inc

The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

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13-12-2012 дата публикации

Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

Номер: US20120316066A1
Принадлежит: Intrexon Corp

The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.

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13-12-2012 дата публикации

Low hygroscopic aripiprazole drug substance and processes for the preparation thereof

Номер: US20120316179A1
Принадлежит: Otsuka Pharmaceutical Co Ltd

The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.

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13-12-2012 дата публикации

Forms of rifaximin and uses thereof

Номер: US20120316334A1
Принадлежит: Salix Pharmaceuticals Ltd

The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.

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13-12-2012 дата публикации

METHOD OF RESOLUTION OF (RS)- 1,1'-BI-2-NAPHTHOL FOR OBTAINING ENANTIOMERIC PURE I.E. (S)-(-)-1,1'-BI-2-NAPHTHOL AND/OR (R)-(+)-1,1'-BI-2-NAPHTHOL VIA CO-CRYSTAL FORMATION WITH OPTICALLY ACTIVE DERIVATIVES OF y -AMINO ACIDS

Номер: US20120316361A1
Принадлежит: Lupin Ltd

Novel method for synthesis of optically pure (S)-(−)-1,1′-bi-2-naphthol and/or (R)-(+)-1,1′-bi-2-naphthol via resolution of racemic (RS)-1,1′-bi-2-naphthol through formation of co-crystal with optically active derivatives of γ-amino acids.

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20-12-2012 дата публикации

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

Номер: US20120321560A1

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

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20-12-2012 дата публикации

Process for producing (3s)-i-menthyl 3-hydroxybutyrate and sensate composition

Номер: US20120321773A1
Принадлежит: Takasago International Corp

Disclosed is a cooling component or sensate component which does not have undesirable stimulus feeling, bitterness and the like and is excellent in the persistence of refresh-feeling and cool-feeling, a sensate composition which comprises the same, and various products that comprise said sensate composition. Also disclosed is a cooling agent comprising (3S)-l-menthyl 3-hydroxybutyrate represented by the following formula (I)

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20-12-2012 дата публикации

Deuterated compounds useful for treating neurodegenerative diseases

Номер: US20120322799A1
Автор: GOPAL Damodara
Принадлежит: Pharmatrophix Inc

The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

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20-12-2012 дата публикации

Purification of cis-1,1,1,4,4,4-hexafluoro-2-butene via extractive distillation

Номер: US20120323054A1
Автор: Jeffrey P. Knapp
Принадлежит: EI Du Pont de Nemours and Co

A process for separating cis-1,1,1,4,4,4-hexafluoro-2-butene from a first mixture comprising cis-1,1,1,4,4,4-hexafluoro-2-butene and at least one chlorofluoroolefin is disclosed. The process involves the steps of contacting said first mixture with at least one extractive agent, to form a second mixture, distilling said second mixture; and recovering cis-1,1,1,4,4,4-hexafluoro-2-butene substantially free of chlorofluoroolefin.

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27-12-2012 дата публикации

Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof

Номер: US20120329848A1
Принадлежит: Arena Pharmaceuticals Inc

The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

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27-12-2012 дата публикации

Method of manufacturing epsilon-caprolactam

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

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

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03-01-2013 дата публикации

Crystalline forms of neurotrophin mimetic compounds and their salts

Номер: US20130005731A1
Принадлежит: Pharmatrophix Inc

The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.

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10-01-2013 дата публикации

4-hydroxybutyric acid analogs

Номер: US20130012565A1
Принадлежит: Concert Pharmaceuticals Inc

This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.

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24-01-2013 дата публикации

Crystalline form of cyclosporine a, methods of preparation, and methods for use thereof

Номер: US20130023482A1
Принадлежит: Allergan Inc

The present invention relates generally to crystalline forms of cyclosporine A and particularly to a newly identified form of cyclosporine A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders.

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31-01-2013 дата публикации

Process for the preparation of lacosamide

Номер: US20130030216A1
Принадлежит: EUTICALS SPA

A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

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21-02-2013 дата публикации

Compositions and Methods for Enhancing Proteasome Activity

Номер: US20130045992A1
Принадлежит: Harvard College

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp 14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

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21-02-2013 дата публикации

Method for producing optically active, racemic menthol

Номер: US20130046118A1
Принадлежит: BASF SE

The present invention relates to a particularly economic overall method for producing menthol, specifically for producing optically active, essentially enantiomerically and diastereomerically pure L-menthol and racemic menthol, starting from the starting material citral which is available inexpensively on an industrial scale. The method comprises the following steps a.1) catalytic hydrogenation of neral and/or geranial to give citronellal, b.1) cyclization of citronellal to isopulegol in the presence of an acidic catalyst, c.1) purification of isopulegol by crystallization and d.1) catalytic hydrogenation of isopulegol to give menthol.

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28-02-2013 дата публикации

Dp2 antagonist and uses thereof

Номер: US20130053444A1
Принадлежит: Panmira Pharmaceuticals LLC

Described herein is the DP 2 anatgonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP 2 anatgonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP 2 anatgonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D 2 -dependent or prostaglandin D 2 -mediated diseases or conditions.

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07-03-2013 дата публикации

Therapeutic Compounds

Номер: US20130059919A1
Автор: Thomas E. Jenkins
Принадлежит: Individual

A (−)-stereoisomer of formula (I): [insert formula (I) wherein X is H or F; or a pharmaceutically acceptable salt or prodrug thereof, useful as an anesthetic.

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14-03-2013 дата публикации

Salt of naphthyridine carboxylic acid derivative

Номер: US20130065917A1
Принадлежит: LG Chemical Co Ltd

7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.

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14-03-2013 дата публикации

Process for Enantioselective Synthesis of Single Enantiomers of Modafinil by Asymmetric Oxidation

Номер: US20130066111A1
Принадлежит: CEPHALON FRANCE

The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: 1. A three-step method for preparing enantiomerically enriched modafinil , wherein the steps comprise:a) dissolving non-racemic modafinil in a solvent to form a solution;b) crystallizing a modafinil enantiomer from the solution; andc) isolating the crystallized modafinil enantiomer, wherein the isolated modafinil enantiomer has an enantiomeric excess at least about 3% higher than the non-racemic modafinil dissolved in step (a).2. The method of claim 1 , wherein the solvent comprises ethanol claim 1 , tetrahydrofuran claim 1 , acetone claim 1 , dichloromethane claim 1 , acetonitrile claim 1 , or ethyl acetate.3. The method of claim 2 , wherein the solvent comprises ethanol.4. The method of claim 2 , wherein the solvent comprises tetrahydrofuran claim 2 , acetone claim 2 , dichloromethane claim 2 , acetonitrile claim 2 , or ethyl acetate.5. The method of claim 4 , wherein the solvent comprises tetrahydrofuran.6. The method of claim 5 , wherein the solvent comprises a mixture of tetrahydrofuran and water.7. The method of claim 6 , wherein the solvent comprises a mixture of about 95/5 tetrahydrofuran/water.8. The method of claim 4 , wherein the solvent comprises dichloromethane.9. The method of claim 4 , wherein the solvent comprises acetonitrile.10. The method of claim 4 , wherein the solvent comprises ethyl acetate.11. The method of claim 10 , wherein the solvent comprises a mixture of ethyl acetate and methanol.12. The method of claim 11 , wherein the solvent comprises a mixture of about 6/1 ethyl acetate/methanol.13. The method of claim 4 , wherein the solvent comprises acetone.14. The method of claim 13 , wherein the solvent comprises a mixture of acetone and water.15. The method of claim 14 , wherein the solvent comprises a mixture of about 95/5 acetone/water.16. The method of claim 1 , ...

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21-03-2013 дата публикации

Process for Producing Aliskiren

Номер: US20130071899A1
Принадлежит: Chemo Iberica SA

A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.

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21-03-2013 дата публикации

CRYSTALLINE FORMS OF A PURINE DERIVATIVE

Номер: US20130072504A1
Принадлежит: CYCLACEL LIMITED

The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. 2. The crystalline form of which is a tartrate salt.3. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 6.67±0.2 claim 2 , 8.237±0.2 claim 2 , 9.777±0.2 claim 2 , 11.96±0.2 claim 2 , 12.38±0.2 claim 2 , 13.06±0.2 claim 2 , 13.38±0.2 claim 2 , 13.94±0.2 claim 2 , 14.90±0.2 claim 2 , 15.40±0.2 claim 2 , 15.95±0.2 claim 2 , 16.27±0.2 claim 2 , 16.54±0.2 claim 2 , 17.36±0.2 claim 2 , 17.57±0.2 claim 2 , 17.86±0.2 claim 2 , 19.64±0.2 claim 2 , 19.86±0.2 claim 2 , 20.12±0.2 claim 2 , 20.73±0.2 claim 2 , 21.14±0.2 claim 2 , 21.58±0.2 claim 2 , 22.57±0.2 claim 2 , 22.95±0.2 claim 2 , 23.29±0.2 claim 2 , 23.57±0.2 claim 2 , 24.07±0.2 claim 2 , 24.63±0.2 claim 2 , 25.30±0.2 claim 2 , 26.38±0.2 claim 2 , 27.09±0.2 claim 2 , 27.67±0.2 claim 2 , 27.97±0.2 claim 2 , 28.91±0.2 claim 2 , 29.28±0.2 claim 2 , 30.08±0.2 claim 2 , 30.41±0.2 claim 2 , 31.90±0.2 and 34.49±0.2 (Form E).45-. (canceled)6. The crystalline form of which is characterized by a differential scanning calorimetry trace recorded at a heating rate of 20° C. per minute which shows a maximum endothermic peak at a temperature between about 176° C. and about 185° C. claim 2 , or a differential scanning calorimetry trace substantially in accordance with that shown in .7. (canceled)8. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 3.82±0.2 claim 2 , 7.57±0.2 claim 2 , 8.12±0.2 claim 2 , 10.53±0.2 claim 2 , 11.39±0.2 claim 2 , 12.00±0.2 ...

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28-03-2013 дата публикации

Crystalline Diacylhydrazine and the Use Thereof

Номер: US20130079413A1
Принадлежит: Intrexon Corp

The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.

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11-04-2013 дата публикации

R(+)-n-formyl-propargyl-aminoindan

Номер: US20130089612A1
Принадлежит: Teva Pharmaceutical Industries LTD

The subject invention provides R(+)-N-formyl-propargyl-aminoindan and a composition containing N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of R(+)-N-formyl-propargyl-aminoindan.

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18-04-2013 дата публикации

Functionalized nanoparticles

Номер: US20130096241A1
Принадлежит: BASF SE

Functionalized nanoparticles, which are obtainable by combining in a first step a functionalized dyestuff, a silicon-based spacer and a catalyst, and in a second step reacting the product obtained in the first step with a co-reactive organic silicon, aluminum, zirconium or titanium compound. Optionally, the thus obtained functionalized nanoparticles can be combined or encapsulated with a polymer. The functionalized nanoparticles are useful as colorants and fluorescents in plastics, paints, inks, electronic materials, cosmetic articles, and the like.

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25-04-2013 дата публикации

Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives

Номер: US20130102794A1
Принадлежит: UCB PHARMA GMBH

The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

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09-05-2013 дата публикации

Ordered mesoporous titanosilicate and the process for the preparation thereof

Номер: US20130116453A1

The invention discloses three-dimensional, ordered, mesoporous titanosilicates wherein the Ti is in a tetrahedral geometry and exclusively substituted for Si in the silica framework. Such titanosilicates find use as catalysts for epoxidation, hydroxylation, C—H bond oxidation, oxidation of sulfides, aminolysis of epoxide and amoximation, with approx. 100% selectivity towards the products.

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16-05-2013 дата публикации

Styryl-based compound, composition containing styryl-based compound, and organic light emitting diode including styryl-based compound

Номер: US20130119355A1
Принадлежит: Samsung Display Co Ltd

A styryl-based compound represented by Formula 1, a composition containing the styryl-based compound, and an organic light-emitting diode (OLED) including the styryl-based compound: The styryl-based compound may exhibit high heat resistance and thus an OLED including the same may have low driving voltage, high brightness, high efficiency, and long lifetime.

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16-05-2013 дата публикации

Tricyclic Compounds and Methods of Making and Using Same

Номер: US20130123235A1
Принадлежит: Individual

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

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16-05-2013 дата публикации

Pyrimidine derivatives and their use in the treatment of respiratory diseases such as copd

Номер: US20130123278A1
Принадлежит: Chiesi Farmaceutici SpA

Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C—R 1 or N; -X 1 -X 2 - is CR 15 ═N— or —NR 19 —CO—; and R 1 -R 6 , R 15 and R 16 are as defined in the claims.

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16-05-2013 дата публикации

Crystal of thienopyrimidine derivative

Номер: US20130123279A1
Принадлежит: Aska Pharmaceutical Co Ltd

Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.

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23-05-2013 дата публикации

Production of renewable aromatic compounds

Номер: US20130130345A1
Принадлежит: JNF BIOCHEMICALS LLC

The invention provides a process for producing a variety renewable aromatic compounds such as benzene, toluene, xylenes, and cumene, as well as compounds derived from these including, for example, aniline, benzoic acid, cresol, cyclohexane, cyclohexanone, phenol and bisphenol A, toluene di-isocyanate, isophthalic acid, phthalic anhydride, terephthalic acid and dimethyl terephthalate. The invention also provides for renewable forms of these aromatic compounds.

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06-06-2013 дата публикации

Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Номер: US20130143881A1
Принадлежит: Exelixis Inc

This invention relates crystalline hydrates of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Compound (I). The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline hydrate of Compound (I) and a pharmaceutically acceptable excipient.

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06-06-2013 дата публикации

Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-Fluoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide

Номер: US20130143918A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.

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06-06-2013 дата публикации

Device for the synthesis of radio-labeled compounds

Номер: US20130144052A1
Автор: Marco Mueller
Принадлежит: ABX advanced biochemical compounds GmbH

The invention relates to a device for the synthesis of radio-labeled compounds, which comprises a reaction vessel for reacting a precursor compound having protective groups with a radioactive isotope to obtain a first reaction product; a first cartridge for hydrolyzing the protective groups of the first reaction product to obtain a second reaction product; and a second cartridge for purifying the second reaction product, wherein the reaction vessel, the first cartridge, and the second cartridge are connected to each other via pipelines. Here it is provided that the first cartridge contains 801 to 1200 mg of a solid carrier and/or the reaction vessel is a reaction vessel made of a temperature-resistant plastic with the plastic having a temperature resistance of at least 120° C.

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13-06-2013 дата публикации

Process for cis-1-chloro-3,3,3-trifluoropropene

Номер: US20130150632A1
Принадлежит: Honeywell International Inc

Disclosed is a process for the preparation of cis-1-chloro-3,3,3-trifluoropropene (cis-1233zd) comprising the steps of (a) providing CF 3 CHClCHCl 2 (233da), and (b) treating the 233da with a dechlorinating agent to produce a mixture of compounds including cis-1-chloro-3,3,3-trifluoropropene, preferably wherein the amount of the cis-isomer generated in the reaction is not less than 30%.

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20-06-2013 дата публикации

Method of preparing ethacrynic amide derivatives and application thereof

Номер: US20130156701A1
Принадлежит: National Tsing Hua University NTHU

The present invention provides a method for preparing [ 18 F]—N-(4-fluorobutyl)ethacrynic amide which is prepared from radiofluorination and deprotection of the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)-butyl)ethacrynic amide], obtained from ethacrynic acid via 6-step synthesis in 39% yield, in a radiochemical yield of 44%, aspecific activity of 48 GBq/μmol and radiochemical purity of 98%. The present invention further provides a composition for positron emission tomography (PET) of an animal models of a tumor liver or a liver disease, comprising [ 18 F]—N-(4-fluorobutyl)ethacrynic amide and a pharmaceutically acceptable carrier.

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27-06-2013 дата публикации

Aildenafil citrate crystal form o, preparation method and use thereof

Номер: US20130165448A1
Автор: Guikun Liu
Принадлежит: Guikun Liu

The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.

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27-06-2013 дата публикации

Zinc oxide complexes

Номер: US20130165668A1
Автор: James Swanzy
Принадлежит: Kay Mary Inc

Disclosed are compounds and methods of making said compounds comprising a zinc oxide molecule chemically bound to one or more molecules having an acidic hydrogen, such as an organic acid. The invention also provides compositions comprising such compounds and methods of preparing such compounds. The compounds of the invention may be provided in, for example, topical skin formulations, pharmaceutical compositions, or delivery systems for active ingredients.

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18-07-2013 дата публикации

Processes for Making Compounds Useful as Inhibitors of ATR Kinase

Номер: US20130184292A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.

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25-07-2013 дата публикации

Process for the preparation of amino acid derivatives

Номер: US20130190533A1
Принадлежит: UCB PHARMA GMBH

The present invention relates to a process of manufacture of compounds of formula (B) wherein R 1 , R 2 and R 3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.

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25-07-2013 дата публикации

Method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane

Номер: US20130190540A1
Принадлежит: Kowa Co Ltd

A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R 1 )(R 2 )(R 3 ) (in the formula, R 1 , R 2 , and R 3 independently represent a C 6-10 aryl group, a C 6-10 aryloxy group, a C 1-10 alkyl group, a C 1-10 alkoxyl group, a C 3-6 cycloalkyl group, or a C 3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.

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01-08-2013 дата публикации

Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

Номер: US20130196966A1
Принадлежит: Receptos LLC

Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

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01-08-2013 дата публикации

Mglu 2/3 agonists

Номер: US20130197079A1
Принадлежит: Eli Lilly and Co

The present invention provides novel mGlu2/3 agonists useful in the treatment of neurological or psychiatric disorders.

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01-08-2013 дата публикации

Short synthesis of tolterodine, intermediates and metabolites

Номер: US20130197082A1
Автор: Damjan Sterk
Принадлежит: Lek Pharmaceuticals dd

A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.

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15-08-2013 дата публикации

Compositions and Methods for Imaging

Номер: US20130209360A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.

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15-08-2013 дата публикации

Process for preparing carboxamidine compounds

Номер: US20130211130A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a process of making a compound of formula (I): Wherein, R 1 , R 2 , R 4 and X are as defined herein.

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22-08-2013 дата публикации

Organic electroluminescent element, compounds and materials used for the organic electroluminescent element, and light-emitting, display and illuminating devices using the elements

Номер: US20130214259A1
Принадлежит: UDC Ireland Ltd

An organic electroluminescent element is provided that has high luminous efficiency, and a slow luminance deterioration rate in the initial stage of lighting. The organic electroluminescent element includes a substrate; a pair of electrodes including an anode and a cathode, disposed on the substrate; and at least one organic layer including a light emitting layer, disposed between the electrodes, wherein at least one organic layer includes a compound represented by the general formula (1). (R 11 to R 15 represent hydrogen atoms, alkyl groups, or silyl groups, and any one of R 21 to R 24 represents a group represented by general formula (1A) or (1B). Ph 4 represents a p-phenylene group, and at least one of Ph 4a and Ph 4b represents a p-phenylene group.)

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29-08-2013 дата публикации

Metathesis Catalysts Containing Onium Groups

Номер: US20130225807A1
Принадлежит: Apeiron Synthesis Sp zoo

Disclosed herein is a general method for the preparation of complexes containing a quaternary onium group in an inert ligand. Some of these complexes may be represented by formula 1: Methods for the preparation of complexes of formula 1, the preparation of intermediates and the use of complexes of formula 1 in metathesis reactions and a method for conducting an olefin metathesis reaction are also described.

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19-09-2013 дата публикации

Novel compound and medical use thereof

Номер: US20130245074A1
Автор: Koji Yano, Masaya Kokubo
Принадлежит: Ono Pharmaceutical Co Ltd

Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

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19-09-2013 дата публикации

Benzothiazolone compound

Номер: US20130245080A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

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19-09-2013 дата публикации

Compound having hetero ring skeleton, and process for producing optically active compound using the aforementioned compound as asymmetric catalyst

Номер: US20130245257A1
Принадлежит: KYOTO UNIVERSITY, Sumitomo Chemical Co Ltd

The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the substituents are as defined in the specification, as well as a tautomer thereof or a salt thereof. The invention also provides asymmetric synthesis methods involving the use of such a compound, tautomer thereof, or salt thereof, as a catalyst.

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03-10-2013 дата публикации

Polymorphic Form of N-(S)-(3,4-Difluoro-2-(2-Fluoro-4-Iodophenylamino)-6-Methoxyphenyl)-1-(2,3-Dihydroxypropyl)Cyclopropane-1-Sulfonamide and uses thereof

Номер: US20130261339A1
Автор: Stuart Dimock
Принадлежит: Ardea Biociences Inc

Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.

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10-10-2013 дата публикации

Filter Media Treated with Cationic Fluorinated Ether Silane Compositions

Номер: US20130264276A1
Принадлежит: 3M Innovative Properties Co

Filter media is treated with a composition comprising cationic fluorinated ether silanes to provide durable water- and/or oil-repellency properties.

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10-10-2013 дата публикации

Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof

Номер: US20130267495A1
Принадлежит: Samumed LLC

Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

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10-10-2013 дата публикации

Ampk-activating heterocyclic compounds and methods for using the same

Номер: US20130267702A1
Принадлежит: Rigel Pharmaceuticals Inc

Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R 3 , R 4 , w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

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17-10-2013 дата публикации

Compound for organic light-emitting diode and organic light-emitting diode including the same

Номер: US20130270524A1
Принадлежит: Samsung Display Co Ltd

A compound represented by Formula 1 below may be used in an organic light emitting diode.

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31-10-2013 дата публикации

Fluorinated 2-Amino-4-(Benzylamino)Phenylcarbamate Derivatives

Номер: US20130287686A1
Принадлежит: Scifluor Life Sciences Inc

The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.

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31-10-2013 дата публикации

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20130289034A1
Принадлежит: Edison Phamaceuticals Inc

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

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31-10-2013 дата публикации

Magnetic-cored dendrimer, the method for preparing the same, and the contaminant treatment method using the same

Номер: US20130289292A1

Provided is a magnetic-cored dendrimer represented by the following Chemical Formula wherein R represents a functional group represented by the following Chemical Formula (2) or (3):

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07-11-2013 дата публикации

Process for producing a particulate composition comprising anhydrous crystalline 2-o-alpha-d-glucosyl-l-ascorbic acid

Номер: US20130295618A1
Принадлежит: Hayashibara Co Ltd

The invention provides a process for enabling the production of a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside that does not significantly cake even when the production yield of ascorbic acid 2-glucoside does not reach 35% by weight. The process for producing a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside, which comprises allowing a CGTase to act on a solution containing either liquefied starch or dextrin and L-ascorbic acid and then allowing a glucoamylase to act on the resulting solution to obtain a solution with an ascorbic acid 2-glucoside production yield of at least 27%, purifying the obtained solution to increase the ascorbic acid 2-glucoside content to a level of over 86% by weight, precipitating anhydrous crystalline ascorbic acid 2-glucoside by a controlled cooling method or pseudo-controlled cooling method, collecting the precipitated anhydrous crystalline ascorbic acid 2-glucoside, and ageing and drying the collected anhydrous crystalline ascorbic acid 2-glucoside.

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07-11-2013 дата публикации

Benzoquinoline inhibitors of vesicular monoamine transporter 2

Номер: US20130296360A1
Принадлежит: Auspex Pharmaceuticals Inc

The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.

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14-11-2013 дата публикации

Processes and intermediates for producing azaindoles

Номер: US20130303764A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).

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21-11-2013 дата публикации

Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions

Номер: US20130310555A1
Автор: Hyun-Soon Chong
Принадлежит: Illinois Institute of Technology

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

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28-11-2013 дата публикации

Novel crystalline forms

Номер: US20130316982A1
Принадлежит: Thar Pharmaceuticals Inc

Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

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