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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 54246. Отображено 100.
05-01-2012 дата публикации

Chemically stable ingredients as lemon odorant

Номер: US20120003170A1
Автор: Peter Fankhauser
Принадлежит: FIRMENICH SA

The present invention discloses certain nitrile compounds that are chemically stable and are useful as a lemon odorant or to impart a lemon odor to various consumer articles. The invention also relates to the compositions and articles that contain such compounds as well to the use of the compounds in a method of imparting a lemon odor to the compositions and articles.

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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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12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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19-01-2012 дата публикации

Method for producing oxime

Номер: US20120016161A1
Автор: Sho Tsujiuchi
Принадлежит: Sumitomo Chemical Co Ltd

The present invention provides a method for producing an oxime, comprising the step of an ammoximation reaction of a ketone with an organic peroxide and ammonia in the presence of a catalyst containing titanium and silicon oxide, wherein the catalyst containing titanium and a silicon oxide is a mesoporous silicate, and is subjected to a contact treatment with a silicon compound.

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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

3-aminoxalyl-aminobenzamide derivatives and insecticidal and miticidal agents containing same as active ingredient

Номер: US20120022263A1
Принадлежит: Agro Kanesho Co Ltd

The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R 1 and R 2 each represent, for instance, a C 1 to C 3 alkoxy group or a C 1 to C 3 haloalkoxy group; R 3 and R 4 each represent, for instance, a C 1 to C 8 alkyl group or a C 1 to C 8 haloalkyl group; R 5 represents, for instance, a C 1 to C 5 haloalkyl group; R 6 and R 7 each represent, for instance, a hydrogen atom or a C 1 to C 5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).

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26-01-2012 дата публикации

Axomadol or a Metabolite Thereof for Use in the Treatment of Irritable Bowel Syndrome

Номер: US20120022294A1
Принадлежит: GRUENENTHAL GmbH

The invention relates to axomadol or a metabolite thereof for use in the treatment of irritable bowel syndrome.

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02-02-2012 дата публикации

Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products

Номер: US20120029013A1
Принадлежит: Pierre Fabre Medicament SA

The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C 1 -C 6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C 1 -C 6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

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16-02-2012 дата публикации

Substituted acylguanidine derivatives (as amended)

Номер: US20120041036A1
Принадлежит: Astellas Pharma Inc

An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT 5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

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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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08-03-2012 дата публикации

Method for preparing a terpenylcyclohexanol

Номер: US20120059196A1
Автор: Roland Jacquot
Принадлежит: Rhodia Operations SAS

A method for preparing a terpenylcyclohexanol using a terpenylphenol is described. A method for preparing a terpenylcyclohexanol by hydrogenation of a terpenylphenol is also described wherein the method includes hydrogenating the latter in a liquid phase, in the presence of a Raney nickel catalyst including residual aluminium and doped with a mixture of iron and chromium.

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15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
Принадлежит: Cardiome Pharma Corp

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

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15-03-2012 дата публикации

Methods of making lubiprostone and intermediates thereof

Номер: US20120065409A1
Принадлежит: Apotex Pharmachem Inc

There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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29-03-2012 дата публикации

Novel plasticizer for a polyvinyl chloride resin

Номер: US20120077914A1

The present invention relates to an ester compound using alicyclic polyhydric acid and to a plasticizer for plastics, particularly, polyvinylchloride (PVC), including the ester compound More particularly, the present invention relates to a plasticizer, which is derived by the esterification reaction of alicyclic polyhydric acid and alcohol. When a polyvinylchloride resin is manufactured using the plasticizer, there are advantages in that the obtained products are excellent in terms of plasticizing efficiency, and in that their physical properties, such as hardness, tensile strength and the like, can be improved.

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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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12-04-2012 дата публикации

Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same

Номер: US20120088746A1
Принадлежит: PFIZER INC

Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

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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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03-05-2012 дата публикации

Process for preparing a phenylcyclohexane

Номер: US20120108874A1
Принадлежит: BASF SE

The present invention relates to an improved process for preparing a substituted or unsubstituted phenylcyclohexane by catalytic hydrogenation of a substituted or unsubstituted biphenyl.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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10-05-2012 дата публикации

N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation

Номер: US20120115915A1
Принадлежит: Harvard College

Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

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10-05-2012 дата публикации

Process for separating one or more aliphatic diamines from reductive amination reaction solvents and impurities

Номер: US20120116123A1
Принадлежит: Dow Global Technologies LLC

The instant invention provides a process for separating one or more aliphatic diamines from reductive amination reaction solvents and impurities, and aliphatic diamines obtained via such a process. The process for separating one or more aliphatic diamines from reductive amination reaction solvents and impurities according to the instant invention comprises the steps of: (1) feeding one or more cycloaliphatic cyanoaldehydes, hydrogen, ammonia, and optionally one or more solvents into a continuous reductive amination reactor system; (2) contacting said one or more cycloaliphatic cyanoaldehydes, hydrogen, and ammonia with each other in the presence of one or more heterogeneous metal based catalyst systems at a temperature in the range of from 80° C. to about 160° C. and a pressure in the range of from 700 to 3500 psig; (3) thereby forming a product mixture comprising one or more cycloaliphatic diamines, optionally one or more bicyclic by-products, optionally one or more cycloaliphatic aminonitriles, optionally one or more cycloaliphatic aminoalcohols, optionally one or more oligomeric by-products, ammonia, water, hydrogen, and optionally one or more solvents; (4) removing said product mixture from the reactor system; (5) removing at least a portion of said ammonia, said hydrogen, or mixture thereof from said product mixture via distillation; (6) removing at least a portion of said water and said one or more optional solvents via distillation; (7) removing at least a portion of one or more optional bicyclic by-products via distillation; (8) removing one or more optional cycloaliphatic aminonitriles, one or more optional cycloaliphatic aminoalcohols, one or more optional oligomeric by-products via distillation; and (9) thereby separating said one or more cycloaliphatic diamines from said product mixture.

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17-05-2012 дата публикации

Phenoxy substituted phenylamidine derivatives and their use as fungicides

Номер: US20120122678A1
Принадлежит: Bayer CropScience AG

The present invention relates to 3-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

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17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

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17-05-2012 дата публикации

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

Номер: US20120122920A1

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

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24-05-2012 дата публикации

Derivatives of Fluorene, Anthracene, Xanthene, Dibenzosuberone and Acridine and Uses Thereof

Номер: US20120129837A1
Принадлежит: Clinical Data Inc

Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

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24-05-2012 дата публикации

Dual-acting antihypertensive agents

Номер: US20120129900A1
Принадлежит: Theravance Inc

The invention is directed to compounds of formula I: wherein Ar, r, R 3 , X, and R 5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT 1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

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24-05-2012 дата публикации

Skin Treatments Containing Carboxylic Acid-Substituted Idebenone Derivatives and Methods of Preparation and Use Thereof

Номер: US20120130098A1
Принадлежит: Elizabeth Arden Inc

The present invention relates to novel carboxylic acid-substituted idebenone derivatives, skin treatment compositions containing these carboxylic acid-substituted idebenone derivatives, methods of treating skin changes by topical application of these carboxylic acid-substituted idebenone derivatives, and their methods of synthesis. The carboxylic acid-substituted idebenone derivatives of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the carboxylic acid-substituted idebenone derivatives of the present invention have an antioxidant effect that is useful in treating a skin change.

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24-05-2012 дата публикации

Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane

Номер: US20120130127A1
Принадлежит: Mer Pharma GmbH and Co KGaA

Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, an intermediate in the synthesis of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof, comprising step (iii): (iii) reacting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane with chloroacetonitrile in the presence of an acid, wherein 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane is employed in step (iii) as obtained in the reaction of a methylmagnesium halide with 3,3,5,5-tetramethylcyclohexanone without having been subjected to a purification step.

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31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Принадлежит: Merck and Co Inc

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

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31-05-2012 дата публикации

Fty720-derived anticancer agents

Номер: US20120136063A1

A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R 1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R 2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R 3 is independently selected from the group consisting of alkyl and cyclo-alkyl; and n is independently selected from 0 to 6. The compounds have lower immunosuppressive side effects as a result of not being phosphorylated by sphingosine kinase 2.

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31-05-2012 дата публикации

Process for improving the catalytic activity of catalyst systems for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines

Номер: US20120136173A1
Принадлежит: Dow Global Technologies LLC

The instant invention provides a process for improving catalytic activity of catalyst systems for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines. The process for improving catalytic activity of catalyst systems for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines comprises the steps of: (1) feeding ammonia, optionally hydrogen, and optionally one or more solvents over one or more heterogeneous metal based catalyst systems having a reduced catalytic activity for a period of greater than 1 hour at a temperature in the range of from 50° C. to 500° C.; wherein said one or more heterogeneous metal based catalyst systems have a yield of less than 90 percent based on the molar conversion of cyanoaldehydes to diamines; and (2) thereby improving the catalytic activity of said one or more heterogeneous metal based catalyst systems.

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07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula I wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

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07-06-2012 дата публикации

Biphenylacetamide derivative

Номер: US20120142771A1
Принадлежит: Sumitomo Dainippon Pharma Co Ltd

The present invention provides a compound of formula (I) or a salt thereof, wherein R 1 , R 2 and R 3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 4 and R 5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 6 and R 7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R 8 and R 9 are independently selected from the group consisting of hydrogen atom, C 1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

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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 The Synthesis Of (+) And (-)-1-(3,4-Dichlorophenyl)-3-Azabicycle[3.1.0]Hexane

Номер: US20120142940A1
Принадлежит: Euthymics Bioscience Inc, Merck and Co Inc

The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

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07-06-2012 дата публикации

Process for producing hydrogenolysis products of polyhydric alcohols

Номер: US20120142976A1
Принадлежит: Kao Corp

The present invention relates to a process for producing hydrogenolysis products of polyhydric alcohols with a good selectivity and a high yield, as well as hydrogenolysis catalysts used in the production process. The present invention provides (1) a process for producing a hydrogenolysis product of a polyhydric alcohol which includes the step of reacting the polyhydric alcohol with hydrogen in the presence of a catalyst containing a copper component, wherein the catalyst is a catalyst (A) containing the copper component, an iron component and an aluminum component, or a catalyst (B) containing the copper component and a silicon component; and (2) a hydrogenolysis catalyst for polyhydric alcohols which includes a copper component, an iron component and an aluminum component, and (3) a hydrogenolysis catalyst for polyhydric alcohols which includes a copper component and a silicon component.

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14-06-2012 дата публикации

Enzyme inhibitors

Номер: US20120149736A1
Принадлежит: Chroma Therapeutics Ltd

Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH 2 CH 2 —; R 1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═5)—NR′, —C(═NH)NR′ or —S(═O) 2 NR — wherein R′ is hydrogen or optionally substituted C 1 —C 6 alkyl; L 1 is a divalent radical of formula —(Alk 1 ) m ,(Q) n (Alk 2 ) p — wherein m, n, p, Q, Alk 1 and Alk 2 are as defined in the claims; X 1 represents a bond; —C(═O); or —S(═O) 2 —; —NR 4 C(═O)—, —C(═O)NR 4 —,— NR 4 C(═O)NR 5 —, —NR 4 S(═O) 2 —, or —S(═O) 2 NR 4 — wherein R4 and R5 are independently hydrogen or optionally substituted C 1 -C 6 alkyl; and z is 0 or 1.

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21-06-2012 дата публикации

Cyclic compound, process for production of the cyclic compound, radiation-sensitive composition, and method for formation of resist pattern

Номер: US20120156615A1
Принадлежит: Mitsubishi Gas Chemical Co Inc

A cyclic compound represented by formula (1): wherein L, R 1 , R′, and m are as defined in the specification. The cyclic compound of formula (1) is highly soluble to a safety solvent, highly sensitive, and capable of forming resist patterns with good profile. Therefore, the cyclic compound is useful as a component of a radiation-sensitive composition.

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21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

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21-06-2012 дата публикации

Nuclear receptor binding agents

Номер: US20120157539A1
Принадлежит: GTx Inc

The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

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28-06-2012 дата публикации

Cyclic compound, process for preparation thereof, radiation-sensitive composition, and method for formation of resist pattern

Номер: US20120164576A1
Принадлежит: Mitsubishi Gas Chemical Co Inc

A cyclic compound represented by formula (1): wherein L, R 1 , R′, and m are as defined in the specification. The cyclic compound of formula (1) is highly soluble to a safety solvent, highly sensitive, and capable of forming resist patterns with good profile. Therefore, the cyclic compound is useful as a component of a radiation-sensitive composition.

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28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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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

Compositions, Synthesis, and Methods of Using Cycloalkylmethylamine Derivatives

Номер: US20120172426A1
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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05-07-2012 дата публикации

Zinc cluster

Номер: US20120172601A1
Принадлежит: Takasago International Corp

Disclosed is a novel zinc cluster compound represented by general formula (1): Zn 4 O (OCOR) 6 (RCOOH) n , wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.

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05-07-2012 дата публикации

Continuous method for the hydrogenation of aromatic compounds

Номер: US20120172632A1
Принадлежит: AET Group

The invention relates to a continuous method for the catalytic hydrogenation of an aromatic compound into a cycloaliphatic compound, wherein said method is carried out in a piston reactor provided with a mechanical axially agitating means and comprises continuously feeding a liquid phase comprising said aromatic compound and a catalyst dispersed to the liquid phase, subjecting said liquid phase, at a temperature of between 100° C. and 300° C. and while being mechanical axially agitated, to the effects of a hydrogen pressure of between 10 and 250 bars in the presence of said catalyst dispersed in the liquid phase for a residence time of between 1 second and 10 minutes, and removing the liquid phase from the reactor.

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12-07-2012 дата публикации

Process For Producing Cyclohexylbenzene

Номер: US20120178969A1
Принадлежит: ExxonMobil Chemical Patents Inc

In a process for producing cyclohexylbenzene, benzene and hydrogen are contacted under hydroalkylation conditions with a catalyst system comprising a MCM-22 family molecular sieve and at least one hydrogenation metal. The conditions comprise a temperature of about 140° C. to about 175° C., a pressure of about 135 psig to about 175 psig (931 kPag to 1207 kPag), a hydrogen to benzene molar ratio of about 0.30 to about 0.65 and a weight hourly space velocity of benzene of about 0.26 to about 1.05 hr −1 .

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

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16-08-2012 дата публикации

Compound, resin composition, and resin molded article

Номер: US20120204755A1
Автор: Kenji Yao
Принадлежит: Fuji Xerox Co Ltd

Disclosed is a compound represented by formula (1): wherein R 1 and R 3 each independently represent an alkylene group having 1 to 10 carbon atoms or an arylene group; R 2 and R 4 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an aryl group; and l, n and m each independently represent a natural number of 1 to 3.

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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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30-08-2012 дата публикации

2-phenylethylamino derivatives as calcium and/or sodium channel modulators

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.

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06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

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11-10-2012 дата публикации

Novel ligands that modulate rar receptors

Номер: US20120258996A1
Принадлежит: Galderma Research and Development SNC

Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.

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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.

Подробнее
01-11-2012 дата публикации

Solventless Reaction Process

Номер: US20120277462A1
Принадлежит: Xerox Corp

A process including reacting at least one organic acid with at least one compound of the formula R—OH, in the presence of an optional catalyst, in a reaction mixture wherein the reaction mixture is substantially free of solvent, to form a reaction product, wherein the reaction product is an ester of citric acid or an ester of tartaric acid; optionally, heating the reaction mixture; and optionally, isolating the reaction product.

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01-11-2012 дата публикации

Novel polynuclear poly(phenol) family

Номер: US20120277479A1
Автор: Tatsuya Iwai
Принадлежит: Honshu Chemical Industry Co Ltd

Provided is a polynuclear poly(phenol)family represented by general formula (1). In general formula (1), R 1 s are each independently C 1-8 alkyl group, C 1-8 alkoxy group, an aromatic hydrocarbon group, or a C 1-8 saturated hydrocarbon group having an aromatic hydrocarbon group; n is 0 or an integer of 1 to 3; X is a hydroxyphenyl group represented by general formula (2); and A is a tetravalent carbon atom group or a tetravalent saturated hydrocarbon group having two or more carbon atoms, with the proviso that when A is a tetravalent saturated hydrocarbon group having two or more carbon atoms, two carbon atoms in the A group are each bonded to two phenyl groups.

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08-11-2012 дата публикации

Anthranilic acid derivatives

Номер: US20120283326A1
Принадлежит: Chelsea Therapeutics Inc

Compounds of formula (I) are provided, wherein X is CH═CH, CH 2 O wherein the oxygen atom is bound to ring B, or OCH 2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF 3 and OCF 3 . The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions containing the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.

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08-11-2012 дата публикации

Process for preparing alkyl hydroperoxide compounds

Номер: US20120283482A1
Принадлежит: Rhodia Operations SAS

A method for making alkyl hydroperoxide compounds, specifically the preparation of cyclohexyl hydroperoxide is described. The preparation of cyclohexyl hydroperoxide by means of the oxidation of cyclohexane by oxygen in a multi-stage reactor or in reactors connected in series is also described. In these methods, the reactor surfaces in contact with the oxidation medium can be protected by a layer of heat-resistant PFA polymer.

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08-11-2012 дата публикации

Dehydrogenation Process

Номер: US20120283494A1
Принадлежит: ExxonMobil Chemical Patents Inc

In a dehydrogenation process a hydrocarbon stream comprising at least one non-aromatic six-membered ring compound and at least one five-membered ring compound is contacted with a first catalyst comprising at least one metal component and at least one support and a second catalyst. The first catalyst is utilized to convert at least a portion of the at least one non-aromatic six-membered ring compound in the hydrocarbon stream to at least one aromatic compound and the second catalyst is utilized to convert at least a portion of the at least one five-membered ring compound in the hydrocarbon stream to at least one paraffin.

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22-11-2012 дата публикации

Catalyst and process for hydrogenating aromatics

Номер: US20120296111A1
Принадлежит: BASF SE

The present invention relates to an eggshell catalyst comprising an active metal selected from the group consisting of ruthenium, rhodium, palladium, platinum and mixtures thereof, applied to a support material comprising silicon dioxide, wherein the pore volume of the support material is 0.6 to 1.0 ml/g, determined by Hg porosimetry, the BET surface area is 280 to 500 m 2 /g, and at least 90% of the pores present have a diameter of 6 to 12 nm, to a process for preparing this eggshell catalyst, to a process for hydrogenating an organic compound which comprises at least one hydrogenatable group using the eggshell catalyst, and to the use of the eggshell catalyst for hydrogenating an organic compound.

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29-11-2012 дата публикации

Ether-amide compounds and uses thereof

Номер: US20120302791A1
Принадлежит: Individual

Novel ether-amide compounds are described. Uses of the compounds, in particular as solvents, for example in phytosanitary formulations are also described.

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29-11-2012 дата публикации

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

Номер: US20120302792A1
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

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

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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

novel polymomorph of desvenlafaxine benzoate

Номер: US20120316238A1
Принадлежит: Lupin Ltd

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

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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

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

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20-12-2012 дата публикации

4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

Номер: US20120322875A1
Принадлежит: Individual

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

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27-12-2012 дата публикации

Therapeutic compounds

Номер: US20120329866A1

The invention provides compounds of Formula (I): R 1 ≡R 2   (I) wherein R 1 and R 2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

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27-12-2012 дата публикации

Bis-phosphate compound and asymmetric reaction using the same

Номер: US20120330038A1
Принадлежит: API Corp, Tohoku University NUC

A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds. Thus, the invention enables an industrially feasible method for the production of optically active amidoaldehydes, optically active β-amino acid derivatives, optically active diamine compounds, optically active pyrrolidine derivatives and optically active dihydropyran derivatives which are useful as products such as medicines, agricultural chemicals and chemical products as well as synthesis intermediates for such products.

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17-01-2013 дата публикации

Process for preparing cycloheptene

Номер: US20130018205A1
Принадлежит: BASF SE

The present invention provides a process for preparing cycloheptene and derivatives thereof by ring-closing metathesis of unsymmetric 1,8-dienes whose C—C double bond at the 8 position is nonterminal. Cycloheptene and the cycloheptanone, cycloheptylamine, cycloheptanecarbaldehyde, cycloheptanecarboxylic acid and cycloheptanecarbonyl chloride conversion products thereof, and the derivatives thereof, are important synthesis units for active ingredient compounds. The ring-closing metathesis is preferably performed as a reactive distillation. The unsymmetric 1,8-dienes for the ring-closing metathesis can be obtained by catalytic decarbonylation or oxidative decarboxylation from the corresponding unsaturated carboxylic acids or carboxylic acid derivatives.

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24-01-2013 дата публикации

Arachidonic acid analogs and methods for analgesic treatment using same

Номер: US20130023510A1
Принадлежит: Cytometix Inc

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

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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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07-02-2013 дата публикации

Therapeutic peptides

Номер: US20130035296A1
Принадлежит: LYTIX BIOPHARMA AS

The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

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14-02-2013 дата публикации

Chemoselective enrichment for compound isolation

Номер: US20130041106A1

Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

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21-02-2013 дата публикации

Process for the production of an alkyl hydroperoxide

Номер: US20130046115A1
Принадлежит: Rhodia Operations SAS

A method for preparing an alkyl hydroperoxide obtained by the oxidation of a saturated hydrocarbon using oxygen, preferably of a saturated cyclic hydrocarbon, is described. Also described, is a method for preparing cyclohexyl hydroperoxide by oxidizing cyclohexane with molecular oxygen or a gas containing molecular oxygen preferably in the absence of a catalyst.

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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

Diazeniumdiolate cyclopentyl derivatives

Номер: US20130053352A1
Принадлежит: Merck Sharp and Dohme LLC

A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, —OH, —O—C 1-6 alkyl, ═O, or halogen; R 2 is hydrogen, C(O)OR 8 , C 6 H 5 C(O)OR 8 , (CH 2 ) 1-2 OH, CR 9 R 10 OH, C(O)O(CH 2 ) 0-2 aryl, C(O)NR 9 R 10 , C(O)SO 2 NR 9 R 10 , C 6 H 5 OR 9 , W—C(O)OR 8 , W—OR 9 , Y, or P(O)(OR 9 )(ORlO); R 3 is hydrogen or —C 1-6 alkyl; R 4 is hydrogen, —OH or —C(O)OR 9 ; R 5 is hydrogen or deuterium; R 6 and R 7 are independently —C 1-6 alkyl, fluoro-substituted —C 1-6 alkyl, deutero-substituted —C 1-6 alkyl or —(CH 2 ) 1-2 R 11 , wherein any carbon atom of the fluoro-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro; R 8 , in each instance in which it occurs, is independently hydrogen, —C 1-6 alkyl, or —(CH 2 ) 2 N + (CH 3 ) 3 ; R 9 and R 10 , in each instance in which they occur, are independently —C 1-6 alkyl; R 11 is —OH, —O—C 1-6 alkyl, -0CD3, —OC(O)OC 1-6 alkyl, —NH 2 , —C 6 H 5 , —N 3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R 6 or R 7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.

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28-02-2013 дата публикации

Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

Номер: US20130053412A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R 1 , R 2 , R 3 , LO, W, AR 1 , n are as defined in claim 1 .

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14-03-2013 дата публикации

Fluorine-Containing Sulfonate, Fluorine-Containing Sulfonate Resin, Resist Composition and Pattern Formation Method

Номер: US20130065182A1
Принадлежит: Central Glass Co Ltd

According to the present invention, there is provided a fluorine-containing sulfonate resin having a repeating unit of the following general formula (3). In order to prevent deficiency such as roughness after pattern formation or failure in pattern formation, the fluorine-containing sulfonate resin incorporates therein a photoacid generating function and serves as a resist resin in which “a moiety capable of changing its developer solubility by the action of an acid” and “a moiety having a photoacid generating function” are arranged with regularity.

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14-03-2013 дата публикации

Compounds (cystein based lipopeptides) and compositions as tlr2 agonists used for treating infections, inflammations, respiratory diseases etc.

Номер: US20130065861A1
Принадлежит: IRM LLC

The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.

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11-04-2013 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20130090483A1
Принадлежит: Cardiome Pharma Corp

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

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25-04-2013 дата публикации

Cyclohexylamines

Номер: US20130101667A1
Принадлежит: Endo Pharmaceuticals Inc

The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.

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25-04-2013 дата публикации

2-methylene-vitamin d analogs and their uses

Номер: US20130102573A1
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-vitamin D 3 and (20R)-25-hydroxy-2-methylene-vitamin D 3 , as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.

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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

Imaging Agents

Номер: US20130123618A1
Автор: Mark M. Goodman
Принадлежит: EMORY UNIVERSITY

This invention provides amino acid derivatives useful in detecting and evaluating brain and body tumors, including (1S,2S) anti-2-[ 18 F]FACPC and (1R,2R) anti-2-[ 18 F]FACPC.

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23-05-2013 дата публикации

Chain-selective synthesis of fuel components and chemical feedstocks

Номер: US20130130336A1
Автор: Edwin S. Olson

A method comprising providing a starting composition comprising a polyunsaturated fatty acid, a polyunsaturated fatty ester, a carboxylate salt of a polyunsaturated fatty acid, a polyunsaturated triglyceride, or a mixture thereof; self-metathesizing the starting composition or cross-metathesizing the starting composition with at least one short-chain olefin in the presence of a metathesis catalyst to form self-/cross-metathesis products comprising: cyclohexadiene; at least one olefin; and one or more acid-, ester-, or salt-functionalized alkene; and reacting cyclohexadiene to produce at least one cycloalkane or cycloalkane derivatives. A method for producing cycloalkanes for jet fuel by providing a starting composition comprising at least one selected from the group consisting of algal and polyunsaturated vegetable oils, subjecting the starting composition to metathesis to produce metathesis product comprising at least one olefin, cyclohexadiene, and at least one acid-, ester-, or salt-functionalized alkene, and reacting the at least one olefin and cyclohexadiene to form cycloalkane(s).

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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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23-05-2013 дата публикации

Catalysts for ring-closing metathesis

Номер: US20130131353A1

A catalyst composition is provided, which may be used for ring closing metathesis. In the composition, a catalyst is immobilized on a siliceous mesocellular foam support. A suitable catalyst for use in the composition is a Grubbs-type catalyst or a Hoveyda-Grubbs-type catalyst.

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30-05-2013 дата публикации

Cyclopropene amine compounds

Номер: US20130137575A1
Автор: Edward C. Sisler
Принадлежит: North Carolina State University

Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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04-07-2013 дата публикации

Composition for regenerating normal tissue from fibrotic tissue

Номер: US20130171127A1
Принадлежит: Nitto Denko Corp

The present invention relates to a pharmaceutical composition and a method for regenerating normal tissue from fibrotic tissue, the pharmaceutical composition and the method employing a collagen-reducing substance. In accordance with the present invention, normal tissue can be therapeutically regenerated from fibrotic tissue.

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04-07-2013 дата публикации

Cysteine protease inhibitors

Номер: US20130172232A1
Принадлежит: Medivir UK Ltd

Compounds of the formula I wherein R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a C 5 -C 10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; or R 3 is a C 2 -C 4 alkyl chain with at least 2 chloro or 3 fluoro substituents; or R 3 is C 3 -C 7 cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C 1 -C 4 alkyl, halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C 1 -C 6 alkylamino, C 1 -C 6 dialkylamino or; R 4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R 4 is Het, carbocyclyl, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

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04-07-2013 дата публикации

"process for producing cycloalkylaromatic compounds"

Номер: US20130172514A1
Автор: Teng Xu, Wenyih F. Lai
Принадлежит: ExxonMobil Chemical Patents Inc

In a process for producing a cycloalkylaromatic compound, an aromatic compound, hydrogen and at least one diluent are supplied to a hydroalkylation reaction zone, such that the weight ratio of the diluent to the aromatic compound supplied to the hydroalkylation reaction zone is at least 1:100. The aromatic compound, hydrogen and the at least one diluent are then contacted under hydroalkylation conditions with a hydroalkylation catalyst in the hydroalkylation reaction zone to produce an effluent comprising a cycloalkylaromatic compound.

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04-07-2013 дата публикации

Process for the production of hexanediols

Номер: US20130172579A1
Принадлежит: EI Du Pont de Nemours and Co

Disclosed are processes for preparing 1,2-cyclohexanediol, and mixtures of 1,2-cyclohexanediol and 1,6-hexanediol, by hydrogenating 1,2,6-hexanetriol.

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18-07-2013 дата публикации

Methods and compositions for treatment of cancer and autoimmune disease

Номер: US20130184342A1
Принадлежит: Jackson Laboratory

The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.

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18-07-2013 дата публикации

Vinyl ether functional oligomers and methods for making and using same

Номер: US20130184371A1
Автор: James V. Crivello
Принадлежит: RENSSELAER POLYTECHNIC INSTITUTE

The present invention includes vinyl ether functional oligomers and methods for their preparation, the method including alternating free radical copolymerization of a dialkyl maleate or dialkyl fumerate monomer with a multifunctional vinyl ether monomer in the presence of a solvent with a high chain transfer constant. Also within the scope of the invention are uses for the vinyl ether functional oligomers compositions of this invention, including radiation curable coatings, adhesives, printing inks and composites.

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18-07-2013 дата публикации

Oxidation Catalyst for Hydrocarbon Compound, and Method and Apparatus for Producing Oxide of Hydrocarbon Compound Using Same

Номер: US20130184494A1
Принадлежит: USE Ind Ltd

According to the first embodiment of the present invention, an oxide of a hydrocarbon compound can be produced with high yield and high productivity by oxidizing the hydrocarbon compound with molecular oxygen in the co-presence of an N-hydroxy compound, such as methyl ethyl ketone or N-hydroxysuccinimide, and a phosphate ester, such as dibutyl phosphate. According to another embodiment of the present invention, an oxide of a hydrocarbon compound can be produced with high yield by using an oxidation catalyst that comprises an oxime compound, such as methyl ethyl ketone. According to another embodiment of the present invention, an alcohol and/or a ketone can be produced with high yield by oxidizing the hydrocarbon compound at a temperature of 160° C. or less, and by decomposing the resulting hydroperoxide, for example, in a unit having an inner surface formed by a material from which no transition metal ion is generated.

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