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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 57886. Отображено 100.
05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

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12-01-2012 дата публикации

Acetylene derivatives having mglur 5 antagonistic activity

Номер: US20120010263A1
Принадлежит: Individual

The invention provides compounds of formula I wherein n, A, R, R′, R″, R O , X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

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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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26-01-2012 дата публикации

Organic electronic device, compounds for same, and terminal

Номер: US20120018717A1
Принадлежит: Duksan Hi Metal Co Ltd

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

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02-02-2012 дата публикации

Bicyclic mglur5 positive allosteric modulators and methods of making and using same

Номер: US20120028955A1

In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

Номер: US20120032158A1
Принадлежит: EI Du Pont de Nemours and Co

The present invention is directed to a photoactive device comprising an anode, a cathode, and a photoactive layer, which device further comprises an electron transport and/or anti-quenching layer which minimizes both electron transfer quenching and energy transfer quenching of the photoactive layer.

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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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01-03-2012 дата публикации

Cyanine dyes

Номер: US20120052506A1
Принадлежит: Pacific Biosciences of California Inc

The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.

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01-03-2012 дата публикации

Phospholinked dye analogs with an amino acid linker

Номер: US20120052507A1
Автор: Gene Shen
Принадлежит: Pacific Biosciences of California Inc

In various embodiments, the present invention provides fluorescent dyes that are linked to another species through an amino acid or peptide linker. In an exemplary embodiment, the dye is linked to a polyphosphate nucleic acid through an amino acid or peptide linker. These conjugates find use in single molecule DNA sequencing and other applications. In various embodiments, the dye moiety is a cyanine dye. Cyanine dyes that are highly charged, such as those including muliple sulfonate, alkylsulfonate, carboxylate and/or alkylcarboxylate moieties are examples of cyanine dyes of use in the compounds of the invention.

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08-03-2012 дата публикации

Novel Indicator Platform

Номер: US20120058503A1
Принадлежит: Biosynth AG

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

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08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
Принадлежит: Bristol Myers Squibb Co

The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

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08-03-2012 дата публикации

Carbazole carboxamide compounds useful as kinase inhibitors

Номер: US20120058996A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.

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15-03-2012 дата публикации

Peptidomimetic protease inhibitors

Номер: US20120064034A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

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22-03-2012 дата публикации

Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives

Номер: US20120070385A1
Принадлежит: Spectrum Pharmaceuticals Inc

The present specification discloses tetrahydroindolone derivatives or analogues and methods for treating cognitive/attention deficit disorders using such tetrahydroindolone derivatives and analogues.

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Принадлежит: Aragon Pharmaceuticals Inc

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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22-03-2012 дата публикации

N-[(2-azabicyclo[2.1.1]hex-1-yl)-aryl-methyl]-benzamide derivatives, preparation thereof, and therapeutic use thereof

Номер: US20120071536A1
Принадлежит: SANOFI SA

The invention relates to N-[(2-aza-bicyclo[2.2.1]hex-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C 1 -C 6 )alkyl group, (C 3 -C 7 )-cycloalkyl, optionally substituted by one or more fluorine, (C 3 -C 7 )-cycloalkyl, (C 2 -C 4 )alkenyl, phenyl, (C 1 -C 6 )alkoxy, hydroxy; R 1 is phenyl or naphtyl optionally substituted by one or more halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo-(C 1 -C 6 )alkyl, NR 4 R 5 , (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkyl-SO 2 , phenyl or heteroaryl; R 2 is one or more hydrogen or halogen atoms, halo-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )-cycloalkyl-(C 1 -C 3 )alkyl; R 3 , R 4 and R 5 are independently a hydrogen atom or a (C 1 -C 6 )alkyl group; R 6 is a (C 1 -C 6 )alkyl group; R 3 and R 4 as well as R 3 and R 6 may form, together with the atoms having them, a 5- or 6-member ring; R 4 and R 5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C 1 -C 6 )alkyl group. The invention also relates to the therapeutic use thereof and to a method for synthesizing same.

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29-03-2012 дата публикации

Methods for Synthesizing 3-(Substituted Dihydroisoindolinone-2-YL)-2, 6-Dioxopiperidine, and Intermediates Thereof

Номер: US20120077982A1

The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.

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05-04-2012 дата публикации

Photoelectric conversion element, production method thereof, photosensor, imaging device and their driving method

Номер: US20120080585A1
Принадлежит: Fujifilm Corp

To provide a photoelectric conversion element capable of functioning as a photoelectric conversion element when a compound having a specific structure is applied to the photoelectric conversion element, causing the element to exhibit a low dark current, and reducing the range of increase in the dark current even when the element is heat-treated, and an imaging device equipped with such a photoelectric conversion element. A photoelectric conversion element having a photoelectric conversion film which is sandwiched between a transparent electrically conductive film and an electrically conductive film and contains a photoelectric conversion layer and an electron blocking layer, wherein the electron blocking layer contains a compound having, as a substituent, a substituted amino group containing three or more ring structures.

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05-04-2012 дата публикации

Polymorphs of saxagliptin hydrochloride and processes for preparing them

Номер: US20120083517A1

The invention provides polymorphs of Saxagliptin hydrochloride, processes for preparing polymorphs of Saxagliptin hydrochloride, and pharmaceutical compositions of polymorphs of Saxagliptin hydrochloride.

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12-04-2012 дата публикации

Bicyclic Compounds and Methods of Making and Using Same

Номер: US20120088793A1
Принадлежит: Nanotherapeutics Inc

Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.

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19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

Номер: US20120095042A1
Автор: Stefan Michael Furrer
Принадлежит: Givaudan SA

Provided are compounds of formula (I) wherein m is 0, 1 or 2; R I is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R 2 is selected from hydrogen, methyl and ethyl; I) R 3 is hydrogen, methyl, or ethyl; and R 4 and R 5 are independently selected from ethyl and isopropyl; and R 3 , R 4 and R 5 together have at least 6 carbon atoms: or II) any two or all of R 3 , R 4 and R 5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.

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03-05-2012 дата публикации

Methods and compositions involving (s)-bucindolol

Номер: US20120108617A1
Принадлежит: Arca Biopharma Inc

Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I).

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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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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

Materials for organic electroluminescent devices

Номер: US20120126179A1
Принадлежит: Merck Patent GmBH

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

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

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

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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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28-06-2012 дата публикации

Novel azabicyclohexanes

Номер: US20120165320A1
Принадлежит: Panacea Biotec Ltd

The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

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12-07-2012 дата публикации

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

Номер: US20120176571A1
Автор: Masaomi Makino
Принадлежит: Fujifilm Corp

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

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12-07-2012 дата публикации

Pyrimidine derivatives and analogs, preparation method and use thereof

Номер: US20120178915A1
Автор: Lifeng Xu
Принадлежит: Individual

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X 1 , X 2 , X 3 , X 4 are, independently at each occurrence, C, O, S, Se, N and P elements; R 1 , R 2 , R 3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

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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

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120206037A1

Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.

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23-08-2012 дата публикации

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

Номер: US20120211733A1
Принадлежит: Samsung Mobile Display Co Ltd

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

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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

Guanidine-containing compounds useful as muscarinic receptor antagonists

Номер: US20120219509A1
Принадлежит: Theravance Inc

The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R 1-3 , R 5-7 , a, X, Y, Y′, Y″, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

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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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13-09-2012 дата публикации

Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease

Номер: US20120232070A1
Принадлежит: Laboratories Fournier SAS

Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.

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13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Принадлежит: Helsinn Therapeutics Us Inc

The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

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04-10-2012 дата публикации

Processes for the synthesis of bazedoxifene acetate and intermediates thereof

Номер: US20120253038A1
Принадлежит: SANDOZ AG

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

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08-11-2012 дата публикации

Crystal forms of saxagliptin and processes for preparing same

Номер: US20120283181A1
Принадлежит: Bristol Myers Squibb Co

Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H 2 O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H 2 O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

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08-11-2012 дата публикации

Association between 4-benzamide and an acetylcholinesterase inhibitor, and pharmaceutical compositions containing it

Номер: US20120283244A1
Принадлежит: Laboratoires Servier SAS

Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.

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08-11-2012 дата публикации

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

Номер: US20120283445A1
Принадлежит: SANOFI SA

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

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15-11-2012 дата публикации

Novel compounds with high therapeutic index

Номер: US20120289471A1
Автор: V. Ravi Chandran
Принадлежит: Signature R&D Holdings LLC

The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

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06-12-2012 дата публикации

Motion-based device operations

Номер: US20120306770A1
Принадлежит: Apple Inc

Methods, program products, and systems of motion-based device operations are described. A mobile device can coordinate operations of a motion sensor and a proximity sensor. The mobile device can determine a gesture event using the motion sensor. The mobile device can determine a proximity event using the proximity sensor. The mobile device can use the gesture event and proximity event to confirm one another, and determine that the mobile device has moved in proximity to a target object following a specified gesture. Upon confirmation, the mobile device can perform a specified task.

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06-12-2012 дата публикации

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

Номер: US20120309984A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

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

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13-12-2012 дата публикации

Novel organic compound and organic light-emitting device

Номер: US20120313085A1
Принадлежит: Canon Inc

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

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20-12-2012 дата публикации

Process and intermediate compounds useful in the preparation of statins

Номер: US20120323011A1
Принадлежит: Redx Pharna PLC

There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein R a represents an alkyl group, such as a C 1-16 alkyl group, and preferably an isopropyl group; R b represents an aryl group, preferably a 4-fluorophenyl group; R c represents hydrogen, a protecting group or an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO 2 R e group where R e is an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group.

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03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Принадлежит: Merck Sharp and Dohme LLC

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is R is —C(O)—N(R 27 )(R 28 ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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03-01-2013 дата публикации

Crystalline forms of the mono-sodium salt of d-isoglutamyl-d-tryptophan

Номер: US20130005987A1
Принадлежит: Apotex Technologies Inc

The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

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10-01-2013 дата публикации

Triterpene saponins, methods of synthesis, and uses thereof

Номер: US20130011421A1

The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.

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10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011788A1
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011793A1
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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10-01-2013 дата публикации

New biologically active compound n-[3-(4-nitrophenylamino)-indole-2-ilmethylene]aminoguanidine hydrochloride with anti-inflammatory activity

Номер: US20130012724A1
Принадлежит: INPHARMA

The present invention relates to chemical-pharmaceutical industry and medicine. The present invention relates to N-[ 3 -( 4 -nitrophenylamino)-indole- 2 -ilmethylene]aminoguanidine hydrochloride of formula ( 2 ) having anti-inflammatory and chondroprotective activity. The compound does not exhibit adverse effects.

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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

Crystalline forms of the mono-sodium salt of d-isoglutamyl-d-tryptophan

Номер: US20130045930A1
Принадлежит: Apotex Technologies Inc

The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

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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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28-02-2013 дата публикации

Substituted benzofurans, benzothiophenes, benzoselenophenes and indoles and their use as tubulin polymerisation inhibitors

Номер: US20130053351A1
Принадлежит: Bionomics Ltd

The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

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07-03-2013 дата публикации

Methods of identifying modulators of gpr17

Номер: US20130059899A1

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.

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07-03-2013 дата публикации

Novel methods for the preparation of p2x7r antagonists

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

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

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21-03-2013 дата публикации

BICYCLIC TETRAHYDROPYRROLE COMPOUNDS

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

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

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21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

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21-03-2013 дата публикации

2-PHENYL BENZOYLAMIDES

Номер: US20130072519A1
Принадлежит:

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

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21-03-2013 дата публикации

PHARMACEUTICALLY ACCEPTABLE SALTS OF THYMODEPRESSIN AND PREOCESSES FOR THEIR MANUFACTURE.

Номер: US20130072692A1
Принадлежит: APOTEX TECHNOLOGIES INC.

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

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28-03-2013 дата публикации

AMINOBENZENE COMPOSITIONS AND RELATED DEVICES AND METHODS

Номер: US20130075670A1
Принадлежит: Plextronics, Inc.

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

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28-03-2013 дата публикации

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

Номер: US20130076237A1

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

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28-03-2013 дата публикации

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

Номер: US20130076604A1
Принадлежит: CANON KABUSHIKI KAISHA

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

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28-03-2013 дата публикации

USES OF SELECTIVE INHIBITORS OF HDAC8 FOR TREATMENT OF INFLAMMATORY CONDITIONS

Номер: US20130078215A1
Принадлежит: Pharmacyclics, Inc.

Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described. 1. A method for treating an inflammatory condition in a subject in need thereof , comprising administering to the subject a composition containing a therapeutically effective amount of a selective inhibitor of histone deacetylase 8 activity.2. The method of claim 1 , wherein (a) the secretion of IL-1β in a sample taken from the subject is inhibited by at least 40% claim 1 , and/or (b) the swelling on the skin of the subject decreases by at least 30% after administering the therapeutically effective amount of the selective inhibitor of histone deacetylase 8 activity.3. The method of claim 1 , wherein the inflammatory condition is a skin inflammatory condition claim 1 , autoimmune condition claim 1 , or heteroimmune condition.4. The method of claim 1 , wherein the inflammatory condition is rheumatoid arthritis or psoriasis.5. The method of claim 1 , wherein the subject is refractory or intolerant to at least one other treatment for an inflammatory condition.6. The method of claim 1 , wherein the composition is administered in combination with an additional anti-inflammatory agent.7. The method of claim 6 , wherein the additional anti-inflammatory agent is an immunosuppressant claim 6 , glucocorticoid claim 6 , non-steroidal anti-inflammatory drug claim 6 , Cox-2 specific inhibitor claim 6 , leflunomide claim 6 , gold thioglucose ...

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28-03-2013 дата публикации

Method for Separating off Tryptophan

Номер: US20130079527A1
Принадлежит: EVONIK DEGUSSA GmbH

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

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04-04-2013 дата публикации

CATIONIC 6-AMINOINDOLINES, DYEING COMPOSITIONS CONTAINING THEM, PROCESSES AND USES THEREOF

Номер: US20130081213A1
Автор: Fadli Aziz
Принадлежит:

The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline. 2. Cationic 6-aminoindoline according to claim 1 , in which the cationic radical is a tri(hydroxy)(C-C)alkylammonium radical selected from trimethylammonium claim 1 , triethylammonium claim 1 , dimethylethylammonium claim 1 , diethylmethylammonium claim 1 , diisopropylmethylammonium claim 1 , diethylpropylammonium claim 1 , beta-hydroxyethyldiethylammonium claim 1 , dimethyl-beta-hydroxyethylammonium claim 1 , di-beta-hydroxyethylmethylammonium and tri-beta-hydroxyethylammonium radicals.3. Cationic 6-aminoindoline according to claim 1 , in which the cationic radical is a cationic heterocyclic radical selected from imidazolium claim 1 , pyridinium claim 1 , piperazinium claim 1 , pyrrolidinium claim 1 , morpholinium claim 1 , pyrimidinium claim 1 , thiazolium claim 1 , benzimidazolium claim 1 , benzothiazolium claim 1 , oxazolium claim 1 , benzotriazolium claim 1 , pyrazolium claim 1 , triazolium claim 1 , benzoxazolium and piperidinium radicals.4. Cationic 6-aminoindoline according to claim 1 , in which B represents a covalent bond or a carbonyl radical CO claim 1 , AKrepresents a saturated linear C-Chydrocarbon-based chain claim 1 , p is equal to 0 claim 1 , and CAT is selected from imidazolium claim 1 , piperazinium claim 1 , pyrrolidinium claim 1 , morpholinium or piperidinium radicals claim 1 , optionally substituted with a C-Calkyl radical; the following radicals: piperidine claim 1 , pyrrolidine claim 1 , morpholine claim 1 , substituted with a methyltrimethylammonium claim 1 , methyldiethylmethylammonium claim 1 , methyl(N-methylpyrrolidinium) or trimethylammonium radical; and trimethylammonium claim 1 , ...

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11-04-2013 дата публикации

COMPOUND FOR ORGANIC PHOTOELECTRIC DEVICE AND ORGANIC PHOTOELECTRIC DEVICE INCLUDING THE SAME

Номер: US20130087776A1
Принадлежит:

A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula 1: 2. The compound as claimed in claim 1 , wherein the Arand Arare each independently selected from the group of a substituted or unsubstituted phenyl group claim 1 , a substituted or unsubstituted naphthalenyl group claim 1 , a substituted or unsubstituted fluorenyl group claim 1 , a substituted or unsubstituted biphenyl group claim 1 , a substituted or unsubstituted dibenzofuranyl group claim 1 , a substituted or unsubstituted dibenzothiophenyl group claim 1 , a substituted or unsubstituted anthracenyl group claim 1 , a substituted or unsubstituted phenanthryl group claim 1 , a substituted or unsubstituted naphthacenyl group claim 1 , a substituted or unsubstituted pyrenyl group claim 1 , a substituted or unsubstituted biphenylyl group claim 1 , a substituted or unsubstituted p-terphenyl group claim 1 , a substituted or unsubstituted m-terphenyl group claim 1 , a substituted or unsubstituted chrysenyl group claim 1 , a substituted or unsubstituted triphenylenyl group claim 1 , a substituted or unsubstituted perylenyl group claim 1 , a substituted or unsubstituted indenyl group claim 1 , a substituted or unsubstituted furanyl group claim 1 , a substituted or unsubstituted thiophenyl group claim 1 , a substituted or unsubstituted pyrrolyl group claim 1 , a substituted or unsubstituted pyrazolyl group claim 1 , a substituted or unsubstituted imidazolyl group claim 1 , a substituted or unsubstituted triazolyl group claim 1 , a substituted or unsubstituted oxazolyl group claim 1 , a substituted or unsubstituted thiazolyl group claim 1 , a substituted or unsubstituted oxadiazolyl group claim 1 , a substituted or unsubstituted thiadiazolyl group claim 1 , a substituted or unsubstituted pyridyl group claim 1 , a substituted or unsubstituted pyrimidinyl group claim 1 , a substituted or unsubstituted pyrazinyl group claim 1 , a substituted or unsubstituted ...

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11-04-2013 дата публикации

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

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

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

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18-04-2013 дата публикации

Compounds and Methods for Altering Lifespan of Eukaryotic Organisms

Номер: US20130096175A1
Принадлежит:

Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation. 11.) The compound of claim 1 , wherein the compound is selected from the following: 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[4-(N claim 1 ,N-dimethylamino)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-methylphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-(1-methylethyl)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-chlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-isobutyryl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2-chloro-6-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[naphth-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2 claim 1 ,4-dichlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[2 claim 1 ,4 claim 1 ,5-trimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopropanecarbonyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2- ...

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18-04-2013 дата публикации

PROCESSES AND INTERMEDIATES

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

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

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18-04-2013 дата публикации

PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF

Номер: US20130096303A1
Принадлежит:

The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R—N—O—Rmoiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof. 3. The process of claim 2 , wherein the acid is selected from the group consisting of hydrochloric acid claim 2 , sulfuric acid claim 2 , phosphoric acid claim 2 , nitric acid claim 2 , acetic acid claim 2 , formic acid claim 2 , sulfonic acid claim 2 , and a mixture thereof.5. The process of claim 4 , wherein the hydrolyzing is performed by reacting the compound of Formula 6 with an alkali metal hydroxide or an alkaline earth metal hydroxide.6. The process of claim 4 , wherein the acid is selected from the group consisting of hydrochloric acid claim 4 , sulfuric acid claim 4 , phosphoric acid claim 4 , nitric acid claim 4 , acetic acid claim 4 , formic acid claim 4 , sulfonic acid claim 4 , and a mixture thereof.7. The process of claim 1 , wherein Rand Rare independently methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , or phenyl.16. The process of claim 15 , wherein the reacting is performed in the presence of a base selected from the group consisting of sodium C˜Calkoxide claim 15 , potassium C˜Calkoxide claim 15 , sodium carbonate claim 15 , potassium carbonate claim 15 , lithium carbonate claim 15 , cesium carbonate claim 15 , sodium bicarbonate claim 15 , potassium bicarbonate claim 15 , potassium phosphate claim 15 , 1 claim 15 ,8-diazabicyclo[5.4.0]undec-7-ene (DBU) claim 15 , 1 claim 15 ,4-diazabicyclo[2.2.2]octane (DABCO) claim 15 , 1 claim 15 ,5-diazabicyclo[4.3.0]non-5-ene (DBN) claim 15 , pyridine claim 15 , dimethylaminopyridine claim 15 , triethylamine claim 15 , lithium bis(trimethylsilyl)amide ...

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18-04-2013 дата публикации

REDUCTION OF ALDEHYDES AND KETONES TO ALCOHOLS

Номер: US20130096317A1
Принадлежит:

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

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25-04-2013 дата публикации

Fluorogenic ph sensitive dyes and their method of use

Номер: US20130102021A1
Принадлежит: Life Technologies Corp

A new class of pH sensitive fluorescent dyes and assays relating thereto are described. The dyes and assays are particularly suited for biological applications including phagocytosis and monitoring intracellular processes. The pH sensitive fluorescent dyes of the present invention include compounds of Formula I: wherein the variables are described throughout the application.

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25-04-2013 дата публикации

NOVEL CYCLOPROPANE INDOLINONE DERIVATIVES

Номер: US20130102604A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to a compound of formula (I) 2. A compound according to claim 1 , wherein one of Rand Ris selected from hydrogen and alkyl and the other is selected from the group consisting of: pyridinyl claim 1 , halophenyl claim 1 , alkylsulfonylphenyl claim 1 , cyanophenyl and trifluoromethylphenyl.3. A compound according to claim 1 , wherein one of Rand Ris selected from hydrogen and isopropyl and the other is selected from the group consisting of: pyridinyl claim 1 , fluorophenyl claim 1 , chlorophenyl claim 1 , cyanophenyl claim 1 , methylsulfonylphenyl and trifluoromethylphenyl.4. A compound according to wherein Ris selected from the group consisting of: pyridinyl claim 1 , carboxypyridinyl claim 1 , tetrahydropyranyl claim 1 , dialkylamino claim 1 , morpholinyl claim 1 , alkylsulfonylpiperidinyl claim 1 , alkylpiperazinyl claim 1 , dialkylaminoalkylpiperazinyl claim 1 , dialkylaminopyrrolidinyl claim 1 , carboxyalkyl-1H-imidazolyl claim 1 , carboxy-1H-imidazolyl or substituted phenyl claim 1 , wherein substituted phenyl is phenyl substituted with one or two substituents independently selected from alkyl claim 1 , halogen claim 1 , carboxy claim 1 , alkylsulfonyl claim 1 , alkylaminocarbonyl claim 1 , alkylsulfonylaminocarbonyl claim 1 , piperidinylcarbonyl claim 1 , piperazinylcarbonyl claim 1 , morpholinylcarbonyl claim 1 , pyridinylpiperazinylcarbonyl claim 1 , alkylpiperazinylcarbonyl claim 1 , alkylsulfonylpiperazinylcarbonyl claim 1 , alkylpyrrolidinylalkylaminocarbonyl claim 1 , alkyl-1H-pyrazolylaminocarbonyl claim 1 , oxo-oxazolidinyl claim 1 , oxo-pyrrolidinyl and oxo-imidazolidinyl.5. A compound according to claim 1 , wherein Ris selected from the group consisting of: carboxypyridinyl claim 1 , carboxyalkyl-1H-imidazolyl claim 1 , carboxyphenyl and phenyl substituted with carboxy and oxo-oxazolidinyl.6. A compound according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and carboxy.7. A ...

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25-04-2013 дата публикации

BIARYL OXYACETIC ACID COMPOUNDS

Номер: US20130102609A1
Принадлежит: LIGAND PHARMACEUTICALS INC.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

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25-04-2013 дата публикации

TARGETED NITROXIDE AGENTS

Номер: US20130102626A1
Принадлежит:

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

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25-04-2013 дата публикации

Method for the preparation of cis-1,2-diols in the kilogram scale

Номер: US20130102640A1
Принадлежит: Merck Patent GmBH

The present invention relates to the scale up of the preparation of cis-1,2-diols of formula I from the gram to the kilogram scale.

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25-04-2013 дата публикации

NOVEL CURING AGENTS

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

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

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25-04-2013 дата публикации

THIONATION PROCESS AND A THIONATING AGENT

Номер: US20130102774A1
Принадлежит: Vironova AB

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline PS.2 CHN as a thionating agent. A thionating agent which is crystalline PS.2 CHN. 1. A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product , by use of crystalline PS.2 CHN as a thionating agent.2. A process according to claim 1 , wherein the thionating agent and the compound are allowed to react with each other in a liquid solvent medium for the compound and for the thionating agent.3. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , a C1-C3 alkylnitrile claim 1 , a cyclic sulfone and/or a C1-C3 dialkylsulfone.4. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , sulfolane claim 1 , dimethyl sulfone and/or acetonitrile.5. The process according to claim 1 , wherein the reaction is performed at a temperature of 60° C. to 180° C.6. The process according to claim 5 , wherein the reaction is performed at temperature of 115° C. to 175° C.7. The process according to claim 1 , wherein the compound comprises a group (I) that is present in an amide function.8. The process according to claim 1 , wherein the compound comprises a group (I) that is present in a ketone function.9. The process according to claim 1 , wherein the thionating agent is used at a molar ratio to the group (I) to be transformed of 1 mole PS.2 CHN per 1-4 moles of group (I).10. The process according to claim 1 , comprising separating the thionated reaction product from the reaction.11. The process according to claim 10 , wherein water is added to the reaction and the thionated reaction product is separated as a solid material claim 10 , by precipitation or crystallization.12. A thionating agent which is ...

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02-05-2013 дата публикации

Method of ameliorating oxidative stress and supplementing the diet

Номер: US20130108605A1

A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R 1 is an aromatic backbone and R 2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R 2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

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02-05-2013 дата публикации

ACTIVATORS OF HUMAN PYRUVATE KINASE

Номер: US20130109672A1

Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A, A, L, R, Rto R, Xto X, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A-NR-L-A(I). 2. (canceled)3. The compound or salt of claim 1 , wherein the phenyl ring of the bicyclic ring of R′ is fused with an aryl claim 1 , a heteroaryl claim 1 , a cyclyl claim 1 , or a heterocyclyl claim 1 , each of which is optionally substituted with one or more substituents selected from the group consisting of aryl claim 1 , heteroaryl claim 1 , cyclyl claim 1 , alkyl claim 1 , alkoxyl claim 1 , halogen claim 1 , NH claim 1 , NH—(C-C)alkyl claim 1 , N—(C-C)alkyl-(C-C)alkyl claim 1 , (C-C)alkyl-OC— claim 1 , and heterocyclyl claim 1 , each of which other than halogen and NHis further optionally substituted with one or more substituents selected from the group consisting of NH claim 1 , OH claim 1 , NH—(C-C)alkyl and N—(C-C)alkyl-(C-C)alkyl.4. The compound or salt of claim 1 , wherein the cyclyl or heterocyclyl of R′ or R″ is a five-membered claim 1 , six-membered claim 1 , or seven-membered ring.5. The compound or salt of claim 1 , wherein the heterocyclyl contains one or two heteroatoms.6. The compound or salt of claim 1 , wherein R is methyl or H.8. The compound or salt of claim 7 , wherein one Ris at the ortho position relative to the carbon attached to the NR-L moiety.9. The compound or salt of claim 7 , wherein one Ris H claim 7 , F claim 7 , Cl claim 7 , Br claim 7 , methyl claim 7 , N(Me) claim 7 , NHMe claim 7 , 1-piperidinyl claim 7 , 2-(dimethylamino)ethyl)(methyl)amino claim 7 , pyrrolidin-1-yl claim 7 , 3-(dimethylamino)pyrrolidin-1-yl claim 7 , 2-hydroxy-2-methylpropylamino claim 7 , isopropylamino claim 7 , diethylamino claim 7 , 1-hydroxypropan-2-ylamino claim 7 , 2-hydroxyethylamino claim 7 , or phenyl.10. The compound or salt of claim 1 , wherein ...

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02-05-2013 дата публикации

ISOINDOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

Номер: US20130109686A1
Принадлежит:

The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. 2. The compound of wherein W is pyridyl claim 1 , and pharmaceutically acceptable salts thereof.3. The compound of wherein W is phenyl claim 1 , and pharmaceutically acceptable salts thereof.4. The compound of wherein R is Ccycloalkyl optionally substituted with 1 to 3 groups of R claim 1 , and pharmaceutically acceptable salts thereof.5. The compound according to wherein R is cyclohexyl or cyclohexenyl claim 4 , both optionally substituted with 1 to 3 groups of R claim 4 , and pharmaceutically acceptable salts thereof.6. The compound of wherein R is (CHR)Cheterocycle claim 1 , optionally substituted with 1 to 3 groups of R claim 1 , and pharmaceutically acceptable salts thereof.7. The compound according to wherein R is pyranyl claim 6 , tetrahydropyranyl claim 6 , or pyridyl claim 6 , all optionally substituted with 1 to 3 groups of R claim 6 , and pharmaceutically acceptable salts thereof.8. The compound according to wherein R is (CHR)Caryl claim 1 , optionally substituted with 1 to 3 groups of R claim 1 , and pharmaceutically acceptable salts thereof.9. The compound according to wherein R is phenyl optionally substituted with 1 to 3 groups of R claim 8 , and pharmaceutically acceptable salts thereof.15. A compound of formula (I) of which is found in Table 1 as well as those listed immediately below:2-[(1S,2S)-2-Hydroxycyclohexyl]-5-(4-methoxybenzyl)-1,2-dihydro-3H-benzo[e]isoindol-3-one;2-[(1S,2S)-2-Hydroxycyclohexyl]-5-[(6-methylpyridin-3-yl)methyl]-1,2-dihydro-3H-benzo[e]isoindol-3-one,2-[(1S ...

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02-05-2013 дата публикации

FAAH Inhibitors

Номер: US20130109721A1
Принадлежит: Ironwood Pharmaceuticals, Inc.

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

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02-05-2013 дата публикации

GPR120 RECEPTOR AGONISTS AND USES THEREOF

Номер: US20130109734A1
Принадлежит: Metabolex, Inc.

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

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02-05-2013 дата публикации

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

Номер: US20130109866A1
Принадлежит: ALLERGAN, INC.

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

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09-05-2013 дата публикации

Hepatitis C Virus Inhibitors

Номер: US20130115193A1
Принадлежит: Bristol Myers Squibb Co

The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

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09-05-2013 дата публикации

(METHYLSULFONYL) ETHYL BENZENE ISOINDOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USES

Номер: US20130116204A1
Принадлежит: Celgene Corporation

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

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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

ALLOSTERIC BINDING COMPOUNDS

Номер: US20130123326A1
Принадлежит:

The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. 2. The method according to claim 1 , comprising administering the compound of formula (I) wherein A is an aryl ring.35.-. (canceled)6. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 6-membered cycloalkyl claim 1 , aryl claim 1 , or heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.78.-. (canceled)9. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 5-membered heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.1011.-. (canceled)14. (canceled)15. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Lis selected from the group consisting of —O— claim 1 , —NH— claim 1 , and —NR—.16. The method according to claim 15 , wherein Ris Calkyl.17. The method according to claim 16 , wherein Ris selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , iso-butyl claim 16 , sec-butyl claim 16 , and tert-butyl.1821.-. (canceled)22. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , and —NH—Calkyl claim 1 , where any of these optionally is substituted with one or more substituents.23. (canceled)24. The method according to claim 22 , wherein Ris Calkyl claim 22 , wherein the alkyl optionally is substituted with one or more substituents.2527.-. (canceled)29. The method according to claim 28 , wherein Lis selected from the group consisting of —O— and —S—.3038.-. (canceled)39. The method ...

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16-05-2013 дата публикации

ACENAPHTHO HETEROCYCLIC COMPOUND AND APPLICATION THEREOF

Номер: US20130123492A1
Автор: Wu Guiye, Zhang Zhichao
Принадлежит: Dalian University of Technology

The present invention relates to acenaphtho heterocyclic compounds and their uses in manufacturing the BH3 mimetics as Bcl-2-like protein inhibitors. Structures are shown in the following: 2. The compound according to claim 1 , wherein the said Z is a straight or branched Calkyl which is unsubstituted or substituted.3. The compound according to claim 2 , wherein Ris (CH)Ph-(o claim 2 ,m claim 2 ,p)Z claim 2 , the said Z is a straight or branched Calkyl which is unsubstituted or substituted.4. The compound according to claim 2 , or claim 2 , wherein the said W is H claim 2 , NHor OH.5. The compound according to claim 4 , wherein the said X is O or S.6. The compound according to claim 5 , wherein Ris (CH)Y claim 5 , the said Y is selected from the group consisting of Ph claim 5 , CF claim 5 , OCH claim 5 , SCH claim 5 , NH claim 5 , Br claim 5 , isopropyl claim 5 , isobutyl and secbutyl.7. The compound according to claim 1 , selected from the group consisting of:9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(hexylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-ethoxy-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-benzoyl-9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butyl(methyl)amino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-(4-bromophenylthio)-9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-(4-bromophenylthio)-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butylamino)-3-thiomorpholino-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(3-phenylpropylamino)-3-thiomorpholino-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butylamino)-3-(4-isopropylphenoxy)-8H-acenaphtho[1,2-b]pyrrol-8-one; and3-(4-isopropylphenoxy)-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one.10. The compound according to claim 9 , wherein Ris XRand Ris H.11. The compound according to or claim 9 , wherein It is CN.12. The compound according to claim 11 , wherein Ris (CH)Ph-(0 claim 11 , m claim 11 , p)Y.13. The compound according to ...

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16-05-2013 дата публикации

Aryl urea derivatives as n-formyl peptide receptors like-1 (fprl-1) receptor modulators

Номер: US20130123496A1
Принадлежит: Allergan Inc

The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

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23-05-2013 дата публикации

Organic luminescent material and organic electroluminescent apparatus

Номер: US20130126834A1
Принадлежит: Academia Sinica, AU OPTRONICS CORP

An organic luminescent material includes a host luminescent material and a guest luminescent material. The host luminescent material includes a compound represented by formula (1), where n is 0˜8; R 2 and R 3 respectively represent H, CF 3 , CN, CH 3 or C 5 H 11 ; R 1 is CH 3 or one of substituents shown as follows:

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23-05-2013 дата публикации

CATIONIC LIPID

Номер: US20130129811A1
Принадлежит:

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 2. The cationic lipid according to claim 1 , wherein Xand Xare combined together to form a single bond or alkylene.3. The cationic lipid according to claim 1 , wherein Lis a single bond claim 1 , Ris a hydrogen atom claim 1 , methyl claim 1 , pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare —O—.4. The cationic lipid according to claim 1 , wherein Lis —CO— or —CO—O— claim 1 , Ris pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , wherein at least one of the substituents is amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare identically —CO—O— or —O—CO—.5. The cationic lipid according to any one of to claim 1 , wherein Xis absent claim 1 , or is methyl.64. The cationic lipid according to any one of to claims 1 , wherein Land Lare —O— or —O—CO— claims 1 , and Rand Rare (Z)-hexadec-6-enyl or (Z)-hexadec ...

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23-05-2013 дата публикации

NOVEL COMPOSITIONS AND METHODS FOR TREATING CANCER

Номер: US20130129812A1

Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression. 7. The compound of claim 1 , wherein{'sup': 1A', '7A', '7A, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': 1B', '7B', '7B, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': '7A', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl; and'}{'sup': '7B', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl.'}8. The compound of claim 1 , wherein{'sup': 2A', '9A', '9A, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': 2B', '9B', '9B, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': '9A', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl; and'}{'sup': '9B', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to ...

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23-05-2013 дата публикации

Novel Estrogen Receptor Ligands

Номер: US20130131061A1
Принадлежит: KARO BIO AB

The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R, R, R, Rand Rare as defined in the specification. 125.-. (canceled)27. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , Ccycloalkyl claim 26 , phenyl and benzyl.28. A method as claimed in claim 27 , in which each Rindependently represents hydrogen or Calkyl.29. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen and Calkyl.30. A method as claimed in claim 26 , in which is selected from the group consisting of OR claim 26 , N(R) claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl claim 26 , trihaloCalkyl claim 26 , haloCalkenyl claim 26 , dihaloCalkenyl claim 26 , trihaloCalkenyl claim 26 , phenyl claim 26 , and 5-6 membered heterocyclyl claim 26 , wherein said phenyl or heterocyclyl group can either be unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of OR claim 26 , halogen claim 26 , cyano claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl and trihaloCalkyl.31. A method as claimed in claim 30 , in which Ris selected from the group consisting of OR claim 30 , N(R) claim 30 , —C(O)Calkyl claim 30 , Calkyl claim 30 , Calkenyl claim 30 , Calkynyl claim 30 , phenyl claim 30 , and 5-6 membered heterocyclyl claim 30 , wherein said phenyl or ...

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