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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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Применить Всего найдено 28193. Отображено 100.
10-09-2007 дата публикации

УСТАНОВКА ДЛЯ ВЫДЕЛЕНИЯ ДИГИДРОКВЕРЦЕТИНА ИЗ ДРЕВЕСИНЫ ЛИСТВЕННИЦЫ

Номер: RU0000066199U1
Автор: Кислицын Алексей Николаевич, Мальчиков Евгений Леонидович
Принадлежит: Мальчиков Евгений Леонидович, ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "ЭЛИОР"

Установка для выделения дигидрокверцетина из древесины лиственницы, содержащая бункер-питатель, узел подачи растворителя, подогреватель, сборник экстракта-растворителя, и по меньшей мере две линии экстракт-растворителей для выделения дигидрокверцетина, каждая из которых содержит подводящие и отводящие вентили, реактор-экстрактор, и пульповый насос, отличающаяся тем, что в нее введен конденсатор паров экстракта-растворителя, а в каждой из линий установлены подогреватель и пульсатор, при этом каждый из экстракторов соединен одним из входов с выходом бункера-питателя, другим входом через первый подводящий вентиль - с узлом подачи экстракта, одним из выходов связан со входом конденсатора, выход которого через вторые подающие вентили также соединен с другим входом каждого из экстракторов, другой выход каждого из которых через последовательно соединенные подогреватель, насос, пульсатор и третий подающий вентиль связан с третьим входом каждого из экстракторов, третьи выходы которых через третий насос и четвертый вентиль соединены со сборником экстракта-растворителя. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 66 199 (13) U1 (51) МПК A61K 36/00 (2006.01) C07D 311/40 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21), (22) Заявка: 2007116823/22 , 03.05.2007 (24) Дата начала отсчета срока действия патента: 03.05.2007 (45) Опубликовано: 10.09.2007 (73) Патентообладатель(и): ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "ЭЛИОР" (RU), Мальчиков Евгений Леонидович (RU) U 1 6 6 1 9 9 R U Ñòðàíèöà: 1 U 1 Формула полезной модели Установка для выделения дигидрокверцетина из древесины лиственницы, содержащая бункер-питатель, узел подачи растворителя, подогреватель, сборник экстракта-растворителя, и по меньшей мере две линии экстракт-растворителей для выделения дигидрокверцетина, каждая из которых содержит подводящие и отводящие вентили, реактор-экстрактор, и пульповый насос, отличающаяся тем, что в нее введен ...

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Номер записи: 1
05-01-2012 дата публикации

Chroman derivatives, medicaments and use in therapy

Номер: US20120004296A1
Автор: Alan Husband, Andrew Heaton
Принадлежит: Marshall Edwards Inc

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

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Номер записи: 2
08-03-2012 дата публикации

Novel kinase modulators

Номер: US20120059001A1
Автор: Govindarajulu Babu, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka
Принадлежит: Incozen Therapeutics Pvt Ltd, Rhizen Pharmaceuticals SA

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

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Номер записи: 3
03-05-2012 дата публикации

Bait chemistries in hydrogel particles for serum biomarker analysis

Номер: US20120107959A1
Автор: Alessandra Luchini, Davide Tamburro, Lance Liotta, Virginia Espina
Принадлежит: George Mason Intellectual Properties Inc, Istituto Superiore di Sanita ISS

This invention describes the identification of novel organic dye chemistries that can be used as affinity baits to capture proteins and other biomolecules useful in the fields of medical diagnostics, environmental science, toxicology, and infectious disease. Incorporation of unique affinity dye compounds within hydrogel capture particles improves analyte yield and preanalytical precision, and stabilizes the analyte against degradation, while increasing measurement sensitivity. The particles in this invention can be used for routine clinical testing as well as for discovery of low abundance disease biomarkers. Example hydrogel particles containing new high affinity bait chemistries were used to identify a new set of human serum biomarkers.

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Номер записи: 4
10-05-2012 дата публикации

Compositions and methods for inhibiting viral and/or bacterial infections

Номер: US20120114639A1
Автор: Michelle Adair Ozbun, Zurab Surviladze
Принадлежит: STC UNM

We describe herein compositions and methods related to inferring with microbial infection. Generally, the compositions include an infection antagonist that inhibits formation of a heparin sulfonated proteoglycan (HSPG)-containing infection complex. Generally, the methods include administering to a subject an amount of a composition as described herein effective to inhibit infection by a microorganism that that infects a host through interactions that involve HSPG.

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Номер записи: 5
31-05-2012 дата публикации

Immunosuppressor based on the blockage of tcr-nck interaction

Номер: US20120135041A1
Автор: Aldo Borroto Revuelta, Angel Ramirez Ortiz, Antonio Morreale De Leon, Balbino ALARCÓN SÁNCHEZ, María del Carmen Fäbregas Cleveria, Maria Luz Ortiz
Принадлежит: Consejo Superior de Investigaciones Cientificas CSIC

The present invention relates to a compound of structural formula (I) and its derivatives for use as medicinal drugs. They are preferably immunosuppressive agents, with mechanism of action based on the blockage of TCR-Nck interaction.

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Номер записи: 6
07-06-2012 дата публикации

Chromene compound

Номер: US20120138876A1
Автор: Shinobu Izumi, Soko Kasai
Принадлежит: Individual

A chromene compound represented by the following formula (1): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.

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Номер записи: 7
21-06-2012 дата публикации

Process for the working-up of a vitamin e- and vitamin e-acetate-containing mixture or product stream

Номер: US20120156107A1
Автор: Angela Wildermann, Peter Ruckstuhl, Werner Pietzonka
Принадлежит: DSM IP ASSETS BV

A rectification column and system for the working-up of a vitamin E (VE)- and/or vitamin E acetate (VEA)-containing product stream includes purification of a vitamin E-containing product stream, acetylation of at least a part of the purified vitamin E and purification of at least a part of the acetylated vitamin E, the purification of vitamin E and vitamin E acetate preferably being effected by distillation, for example rectification.

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Номер записи: 8
05-07-2012 дата публикации

Chroman derivatives, medicaments and use in therapy

Номер: US20120172424A1
Автор: Alan Husband, Andrew Heaton
Принадлежит: Marshall Edwards Inc

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

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Номер записи: 9
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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Номер записи: 10
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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Номер записи: 11
26-07-2012 дата публикации

Treatment or prophylaxis of proliferative conditions

Номер: US20120190639A1
Автор: Saraj Ulhaq, Steven Albert Everett
Принадлежит: UNIVERSITY OF DUNDEE

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

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Номер записи: 12
06-09-2012 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes and parkinson's disease

Номер: US20120225890A1
Автор: Alan D. Snow, Beth Nguyen, Charlotte Coffen, David L. Coffen, David Larsen, Gerardo Castillo, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, Thomas Lake, Virginia Sanders
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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Номер записи: 13
20-09-2012 дата публикации

Method for the enhanced recovery of catmint oil

Номер: US20120238768A1
Автор: David L. Hallahan, Mark A. Scialdone
Принадлежит: EI Du Pont de Nemours and Co

A high yielding method is described for recovery of catmint oil from catmint plants of the genus Nepeta by improved separation of a catmint oil containing phase from the condensed steam distillate of catmint plants. Catmint oil may be obtained in quantitative yields for use in insect repellent compositions.

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Номер записи: 14
18-10-2012 дата публикации

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

Номер: US20120264736A1
Автор: Chad E. Bennett, Chad E. Knutson, David J. Cole, Dmitri A. Pissarnitski, Duane A. Burnett, Haiqun Tang, Hongmei Li, Hubert B. Josien, Jing Su, John W. Clader, Li Qiang, Mark D. Mcbriar, Martin S. Domalski, Mary Ann Caplen, Murali Rajagopalan, Ruo Xu, Thavalakulamgara K. Sasikumar, Theodros Asberom, Thomas A. Bara, Wen-Lian Wu, Zhiqiang Zhao
Принадлежит: Schering Corp

This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

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Номер записи: 15
01-11-2012 дата публикации

Chroman-derived anti-androgens for treatment of androgen mediated disorders

Номер: US20120277301A1
Автор: George Wilding, Todd A. Thompson
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Methods for the prevention and/or alleviation of androgen-mediated disorders treatable by administering a chroman-derived anti-androgen compound are provided by the present invention. The invention further provides pharmaceutical and nutraceutical compositions containing chroman-derived anti-androgen compounds useful in the prevention and/or alleviation of androgen-mediated disorders, particularly prostate cancer.

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Номер записи: 16
08-11-2012 дата публикации

Inhibition and treatment of prostate cancer metastasis

Номер: US20120283313A1
Автор: Karl A. Scheidt, Raymond C. Bergan
Принадлежит: Northwestern University

The present invention provides compounds and methods of inhibiting and treating metastatic prostate cancer. The compounds include MEK4 inhibitors. In another aspect the invention provides methods of identifying inhibitors of metastatic prostate cancer by screening for inhibitors of MEK4.

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Номер записи: 17
08-11-2012 дата публикации

Use of rylene derivatives as photosensitizers in solar cells

Номер: US20120283432A1
Автор: Alfred Kuhn, Anders Hagfeldt, Andreas Herrmann, Chen Li, Felix Eickemeyer, Gero Nordmann, Jan SCHÖNEBOOM, Jianqiang Qu, Klaus MÜLLEN, Martin KÖNEMANN, Neil Gregory Pschirer, Peter Erk, Tomas Edvinsson
Принадлежит: BASF SE, Max Planck Gesellschaft zur Foerderung der Wissenschaften eV

Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR 1 R 2   (y1) -L-Z—R 3   (y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR 1 R 2 ; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO 3 M; —PO 3 M 2 ; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR 5 ] 4 + ; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R 1 , R 2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R 3 is optionally substituted alkyl, (het)aryl; R′ is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R 5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4, 6 where: n+p=0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

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Номер записи: 18
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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Номер записи: 19
22-11-2012 дата публикации

Chromone Inhibitors of S-Nitrosoglutathione Reductase

Номер: US20120295966A1
Автор: Jan Wasley, Jian Qiu, Xicheng Sun
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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Номер записи: 20
13-12-2012 дата публикации

Rodenticidal compounds, composition including same and use thereof for controlling harmful rodents

Номер: US20120316231A1
Автор: Etienne Benoit, Philippe Berny, Romain Lasseur, Stéphane Besse
Принадлежит: Liphatech SA

A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X═H, OH, Cl, Br, F or N0 2 ; R2 is: (IV) or (V) or (VI) with X═H, OH, Cl, Br, F or NO 2 ; R3 is: O or S or (VII) with X═H, OH, Cl, Br, F or N0 2 . Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.

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Номер записи: 21
27-12-2012 дата публикации

Novel Insect-Repellent Coumarin Derivatives, Syntheses, and Methods of Use

Номер: US20120329832A1
Автор: Bruno Andrioletti, Emile Vialle, Jean Delaveau, Marc Lemaire, Stephane Pellet-Rostaing
Принадлежит: Merial Ltd

This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.

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Номер записи: 22
03-01-2013 дата публикации

Supercooling promoting agent

Номер: US20130004936A1
Автор: Hiroshi Nishioka, Keita Arakawa, Seizo Fujikawa, Yukiharu Fukiharu
Принадлежит: Hokkaido University NUC

The present invention discloses a supercooling promoting agent comprising a tannin for producing practical water which does not freeze. As the tannin, a hydrolyzable tannin such as 2,3,6-tri-O-galloyl-α,β-D-hamamelose, 1,2,6-tri-O-galloyl-β-D-glucose, and a vitrification liquid, each of which contains the supercooling promoting agent are useful as a solution or the like for storing a biological material at low temperature.

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Номер записи: 23
03-01-2013 дата публикации

Antiprotozoal compound derived from coelenterata

Номер: US20130005798A1
Автор: Noboru Inoue, Shin-ichiro Kawazu, Shintaro Ishigami, Yasuyuki Goto, Yoichi Nakao
Принадлежит: Obihiro University of Agriculture and Veterinary Medicine NUC, WASEDA UNIVERSITY

The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R 1 represents R 10 — of formula (4) or R 20 — of formula (5); R 2 represents CHO—, etc.; R 3 represents a hydrogen atom, CH 3 —C(═O)—, etc.; R 4 represents a hydrogen atom, CH 3 —C(═O)—, etc.; each of R 11 and R 12 independently represents each a hydrogen atom, a methyl group, etc.; R 13 represents —CH 2 —, —CH(—OH)— or —C(═O)—; each of R 21 and R 22 independently represents eaeh a hydrogen atom, a methyl group, etc.; R 23 represents —CH 2 —, —CH(—OH)— or —C(═0)—; and R 24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.

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Номер записи: 24
17-01-2013 дата публикации

Treatment of allodynia and hyperalgesia

Номер: US20130018091A1
Автор: Argeris Karabelas, Peter Blower
Принадлежит: Proximagen Ltd

The present invention relates to the treatment or prevention of allodynia and/or hyperalgesia, and to tonabersator an analogueof formula (1), and compositions comprising tonabersat or an analogue of formula (1) for use in said treatments.

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Номер записи: 25
31-01-2013 дата публикации

Methods and compounds for the targeted delivery of agents to bone for interaction therewith

Номер: US20130029901A1
Автор: K. Grant Taylor, Kevyn Merten, Leonard C. Waite, William M. Pierce, Jr.
Принадлежит: Pradama Inc, University of Louisville Research Foundation ULRF

Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (R T ), having an affinity for bone; a Bone Active Portion (R A ) for interacting with and affecting bone; and a Linking Portion (R L ) connecting the Bone Targeting Portion and the Bone Active Portion.

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Номер записи: 26
14-03-2013 дата публикации

Fluorescent substrate for detection of enzymatic activity of nitrile-related enzyme

Номер: US20130065263A1
Автор: Fujio Yu, Tetsuo Nagano, Tomoe Ohta, Yasuteru Urano
Принадлежит: Mitsubishi Rayon Co Ltd, University of Tokyo NUC

The object of the present invention is to provide a fluorescent substrate for detecting the enzymatic activity of a nitrile-related enzyme. The present invention provides a compound represented by formula (I) and a fluorescent substrate for detecting the enzymatic activity of a nitrile-related enzyme, which comprises the compound.

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Номер записи: 27
21-03-2013 дата публикации

SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE

Номер: US20130072483A1
Автор: Cheng Yuan, Croghan Michael, DINEEN Thomas, Hitchcock Stephen, Horne Daniel, Kaller Matthew, KREIMAN Charles, Lopez Patricia, Monenschein Holger, Nguyen Thomas, Patel Vinod F., Pennington Lewis, Xue Qiufen, Yang Bryant, ZHONG Wenge
Принадлежит: Amgen Inc.

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1a', '1b', '7, 'Rand Rtaken together with the carbon atom to which they are attached form a partially or fully saturated 4-, 5- or 6-membered ring of carbon atoms optionally including 1-2 heteroatoms selected from O, N, or S, the ring optionally substituted independently with 1-3 substituents of R; and'}{'sup': '1c', 'Ris H.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris a ring selected from phenyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , triazinyl claim 1 , thiophenyl claim 1 , furyl claim 1 , pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , tetrazolyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , isothiazolyl claim 1 , thiadiazolyl claim 1 , oxadiazolyl claim 1 , pyrrolidinyl claim 1 , oxazolinyl claim 1 , isoxazolinyl claim 1 , thiazolinyl claim 1 , pyrazolinyl claim 1 , morpholinyl claim 1 , piperidinyl claim 1 , piperazinyl and pyranyl claim 1 , said ring optionally substituted with 1-5 substituents of R.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '1', 'Ais CH;'}{'sup': 2', '6, 'Ais CR;'}{'sup': 3', '4', '6', '3', '4, 'each of Aand A, independently, is CH or CRor N, provided no more than one of Aand Ais N;'}{'sup': 1a', '7, 'sub': 1-6', '2-6', '2-6', '1-6', '1-3', '1-6', '1-3', '1-6', '2', '1-3', '1-6', '1-3', '1-3', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3, 'Ris C-alkyl, Calkenyl, C-alkynyl, Calkyl-O—C-alkyl-, C-alkyl-S—C-alkyl-, C-alkyl ...

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Номер записи: 28
28-03-2013 дата публикации

ISOFLAVONE FATTY ACID ESTER DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL USES THEREOF

Номер: US20130079393A1
Автор: Li Xiaobo, Liao Qingjiang, Ma Renling, Qian Lei, Xiang Hua, Xiao Hong, Yao Yao, You Qidong, Zhao Wei
Принадлежит: CHINA PHARMACEUTICAL UNIVERSITY

Isoflavone fatty acid ester derivatives of formula (I) or (II), the preparation method thereof and the pharmaceutical compositions containing such compounds are disclosed. The uses of such compounds in preparation of medicaments for preventing or treating hyperlipidemia, obesity or type II diabetes are also disclosed. 2. The compound according to claim 1 , wherein RCO represents a fatty acyl group formed by oleic acid claim 1 , linoleic acid claim 1 , undecylenic acid claim 1 , linolenic acid claim 1 , conjugated linoleic acid claim 1 , stearic acid claim 1 , palmitoleic acid claim 1 , eicosatetraenoic acid claim 1 , eicosapentaenoic acid claim 1 , eicosenoic acid claim 1 , docosahexaenoic acid claim 1 , lauric acid claim 1 , capric acid claim 1 , octanoic acid or hydroxy-2-decenoic acid after removal of hydroxide radical.3. The compound according to claim 2 , wherein RCO represents oleoyl claim 2 , linoleoyl claim 2 , linolenic acyl claim 2 , conjugated linoleoyl or palmitoleic acyl.4. The compound according to claim 1 , wherein Rrepresents H claim 1 , OH claim 1 , OCH claim 1 , SCH claim 1 , NHCH claim 1 , N(CH) claim 1 , NO claim 1 , halogen claim 1 , CFor C(O)CH.5. The compound according to claim 4 , wherein Rrepresents OCH.6. The compound according to claim 1 , wherein Ror Rrepresents H claim 1 , OH or OCH.7. The compound according to claim 1 , wherein Rrepresents H claim 1 , OCH claim 1 , SCH claim 1 , NHCH claim 1 , N(CH) claim 1 , NO claim 1 , halogen claim 1 , CFor C(O)CH.8. The compound according to claim 7 , wherein Rrepresents OCH.9. (canceled)10. (canceled)11. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.12. A method for preventing or treating hyperlipidemia claim 11 , obesity or type II diabetes claim 11 , comprising administering an effective amount of the pharmaceutical composition of to the subject. The present invention relates to the field of pharmaceutical chemistry, specially involving the ...

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Номер записи: 29
28-03-2013 дата публикации

FUNGICIDE N-CYCLOALKYL-N-BICYCLIC-CARBOXAMIDE DERIVATIVES

Номер: US20130079524A1
Автор: Desbordes Philippe, Gary Stephanie, Grosjean-Cournoyer Marie-Clarie, Hartmann Benoit, Hiroyuki Hadano, Rinolfi Philippe, Vors Jean-Pierre
Принадлежит:

The present invention relates N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group; T represents O, S, N-R, N—OR, N—NRRor N—CN; Zrepresents a C-C-cycloalkyl group; X represents N or a CZand Z; Z; Land Lrepresent various substituents; their process of preparation; preparation intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. 116-. (canceled)18. The compound of wherein Zis a cyclopropyl.19. The compound of wherein Zis a non-substituted cyclopropyl.20. The compound of wherein Zis a hydrogen atom.21. The compound of wherein Lis CZZ.22. The compound of wherein Lis CZZand m is 1 or 2.23. The compound of wherein Zand each Zare independently selected from the group consisting of a hydrogen atom; a halogen atom; C-C-alkyl; C-C-halogenoalkyl comprising up to 9 halogen atoms that can be the same or different; C-C-alkoxy; and C-C-halogenoalkoxy comprising up to 9 halogen atoms that can be the same or different. The present invention relates to N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.In international patent application WO-2007/014290 certain N-substituted-N-bicyclic-carboxamide or thiocarboxamide derivatives are generically embraced in a broad disclosure of numerous compounds of the following formula:wherein Wcan represent oxygen or sulphur; A can represent NH or CH; Rcan represent a phenyl or heterocyclic ring; G can represent a 5-membered heterocyclic ring, ...

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Номер записи: 30
28-03-2013 дата публикации

Process for the Rapid Extraction of Active Ingredients from Herbal Materials

Номер: US20130079531A1
Автор: Barringer Ian
Принадлежит: Rm3 Labs LLC

The invention is a process for the rapid extraction of active ingredients from herbal materials using a cold solvent and a very short mixing period in order to yield commercially desirable extracts. In particular, the process can be applied to the rapid extraction of cannabinoids from The claimed invention also includes any equipment or machine, or assemblage of equipments or machines, designed or employed to utilize this process. 1. A method for the extraction of active ingredients from herbal material comprising: (i) introducing the herbal material to a non-polar or mildly polar solvent at or below a temperature of 10 degrees centigrade and (ii) rapidly separating the herbal material from the solvent after a latency period not to exceed 15 minutes.2cannabis.. The process defined in in which the herbal material is3. The process defined in in which the combined herbal material and solvent are agitated briefly prior to the separation of the herbal material and the solvent.4. The process defined in in which the solvent claim 1 , the mixture claim 1 , the herbal material and/or all or a portion of the extraction equipment is maintained below 10 degrees centigrade throughout the extraction process.5. The process defined in in which the solvent is chilled to zero degrees centigrade or below prior to its introduction to the herbal material.6. The process defined in in which the time from the introduction of the solvent to the separation of the mixture is less than two minutes.7. The process defined in in which the separation of the solvent from the herbal material is achieved through a continuous or semi-continuous process claim 1 , such as through the use of a basket centrifuge claim 1 , pusher centrifuge claim 1 , decanter centrifuge claim 1 , screen centrifuge claim 1 , inverting bag centrifuge claim 1 , conveyor belt filter claim 1 , horizontal vacuum filter claim 1 , belt press or similar apparatus.8. The process defined in in which the separation of the solvent from ...

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Номер записи: 31
28-03-2013 дата публикации

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

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

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

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Номер записи: 32
11-04-2013 дата публикации

Fluorescent dyes

Номер: US20130089853A1
Автор: Praveen Pande, Zaiguo Li
Принадлежит: Enzo Life Sciences Inc

Provided are various compounds comprising the formula Also provided are fluorescent dyes comprising the above compound. Additionally, a fluorescence energy transfer system is provided that comprises the above-described fluorescent dye and a second dye, wherein the second dye is capable of energy transfer with the fluorescent dye. Further provided is a kit for labeling a target molecule, where the kit comprises the above-described fluorescent dye with additional reagents useful for labeling the target molecule. Additionally provided is a target molecule labeled with the above-described fluorescent dye. A method of labeling a target molecule is also provided. The method comprises contacting reactive group Z of the above-described fluorescent dye with the target molecule such that reactive group Z reacts with the target molecule to form a covalent bond between reactive group Z and the target molecule. Also, another method of labeling a target molecule is provided. The method comprises contacting the above-described fluorescent dye, which further comprises a member of a binding pair, with the target molecule, where the target molecule comprises a second member of the binding pair.

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Номер записи: 33
18-04-2013 дата публикации

LONG WAVELENGTH FLUOROGENIC INTRACELLULAR ION INDICATORS THAT ARE WELL RETAINED IN THE CYTOSOL

Номер: US20130096300A1
Автор: Gee Kyle, MARTIN Vladimir
Принадлежит: LIFE TECHNOLOGIES CORPORATION

Cell permeable metal ion indicator compounds and methods of their use and synthesis are described. The compound comprises a metal chelating moiety (M), a reporter molecule and two or more lipophilic groups (G) covalently bonded through a linker to the reporter molecule, wherein the lipophilic groups, when present in a live cell, are cleaved resulting in two or more negatively charged groups. 1. An intracellular ion indicator compound , wherein the compound comprises a metal chelating moiety (M) , a reporter molecule and two or more lipophilic groups (G) covalently bonded through a linker to the reporter molecule , wherein the lipophilic groups , when present in a live cell , are cleaved resulting in two or more negatively charged groups.245-. (canceled) The present invention provides intracellular ion indicator compounds capable of chelating and detecting metal ions in cells. The compounds generally comprise a metal chelating moiety (M), a reporter molecule and one or more lipophilic groups (G) covalently bonded to the reporter molecule, wherein the lipophilic groups, when present in a live cell, are cleaved resulting in one or more negatively charged groups.Metal ions such as calcium are involved in many cellular processes including signal transduction. Small variances in intracellular ion levels can have a major impact on cellular processes. Measurement of ion levels provides a very sensitive method for identifying various cellular activities.Several fluorescent calcium indicators known in art are employed in biological research and high throughput screening. Generally, long wavelength indicators, such as rhodamine-based compounds bear a positive charge. Positively charged molecules compartmentalize in cell mitochondria. Because calcium ion release in activated cells happens in the cytosol, positively charged indicators show a weak response to calcium ion influx. Alternatively, fluorescein-based indicators have also been described that avoid accumulation in the ...

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Номер записи: 34
18-04-2013 дата публикации

POLYMORPHIC FORMS OF LUBIPROSTONE

Номер: US20130096325A1
Автор: Ceccarelli Alfredo Paul, Kothakonda Kiran Kumar
Принадлежит: APOTEX PHARMACHEM INC.

There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone. 1. APO-II polymorphic form of Lubiprostone.2. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 8.98.3. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 13.53.4. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 18.06.5. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 20.57.6. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 20.80.7. A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at approximately 22.74.8. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 13.53.9. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 18.06.10. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 20.57.11. The crystalline form of Lubiprostone of wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 20.80.12. The crystalline form of Lubiprostone of 5 wherein the X-ray powder diffraction pattern further comprises a peak claim 2 , in terms of 2-theta claim 2 , at approximately 22.74.13. The crystalline form of Lubiprostone of wherein ...

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Номер записи: 35
25-04-2013 дата публикации

Fluorogenic ph sensitive dyes and their method of use

Номер: US20130102021A1
Автор: Aleksey Rukavishnikov, Daniel Beacham, Jeffrey Dzubay, Kyle Gee, Vladimir Martin
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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Номер записи: 36
25-04-2013 дата публикации

FUNGICIDE N-CYCLOALKYL-N-BICYCLIMETHYLENE-CARBOXAMIDE DERIVATIVES

Номер: US20130102790A1
Автор: Benting Jurgen, Dahmen Peter, Desbordes Philippe, Gary Stephanie, Genix Pierre, Hartmann Benoit
Принадлежит:

The present invention relates to N-cycloalkyl-N-bicyclicmethylene-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group, T represents O or S, Zrepresents a C-C-cycloalkyl group, X represents N or a CZand Y, Y, Z, Z, Land Lrepresent various substituents. Their process of preparation, the preparation of intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions are also disclosed. 118-. (canceled)20. The compound of wherein Yis C-C-alkyl and Yis hydrogen.21. The compound of wherein Yis methyl.22. The compound of wherein Yand Yare both C-C-alkyl.23. The compound of wherein Yand Yare both methyl.24. The compound of wherein Zis hydrogen.25. The compound of wherein Lis CZZ.26. The compound of wherein Lis CZZand m is 1 or 2.27. The compound of wherein Zand each Zare independently selected from the group consisting of a hydrogen atom claim 19 , a halogen atom claim 19 , C-C-alkyl claim 19 , C-C-halogenoalkyl comprising up to 9 halogen atoms that can be the same or different claim 19 , C-C-alkoxy claim 19 , and C-C-halogenoalkoxy comprising up to 9 halogen atoms that can be the same or different.28. The compound of wherein said compound is N-cyclopropyl-3-(difluoromethyl)-N-[1-(1-hydroxy-1 claim 19 ,2 claim 19 ,3 claim 19 ,4-tetrahydronaphthalen-1-yl)ethyl]-1-methyl-1H-pyrazole-4-carboxamide. The present invention relates to N-cycloalkyl-N-bicyclicmethylene-carboxamide or thiocarboxamide derivatives, their process of preparation, preparation of intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.In international patent application WO2007060164 ...

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Номер записи: 37
02-05-2013 дата публикации

XANTHENEDIONE DERIVATIVES FOR THE TREATMENT OF PIGMENTATION AND SKIN AGEING DISORDERS

Номер: US20130108568A1
Автор: Belaubre Françoise, Poigny Stéphane
Принадлежит: PIERRE FABRE DERMO-COSMETIQUE

The invention relates to compound of generic formula (I) in which: Rand Rrepresent: OH, a hydrogen atom, a C-Calkyl radical a C-Calkoxy radical, a halogen, or OCOR; Rrepresents: a C-Calkyl radical a C-Calkenyl radical comprising at least one unsaturation; Rrepresents: COR, a glucide substituted or not by one or more acetyl radical(s); Rrepresents: a C-Calkyl radical or a C-Calkenyl radical comprising at least one unsaturation; Rand Rrepresent:—simultaneously a hydrogen atom or a methyl radical, or—when Rrepresents a hydrogen atom, Rrepresents a C-Calkyl radical or a phenyl substituted or not by one or more C-Calkoxy radical(s) or one or more halogen(s) or—Rand Rare bonded together and form a C-Ccycloalkyl, and pharmaceutically or cosmetically acceptable salts. 2. Compound of generic formula (I) according to claim 1 , characterised in that Rand Rrepresent simultaneously or independently a hydrogen atom or a C-Calkoxy radical.3. Compound of generic formula (I) according to claim 1 , characterised in that Rrepresents COR.4. Compound of generic formula (I) according to claim 1 , characterised in that Rrepresents a C-Calkyl radical or a C-Calkenyl radical comprising from 1 to 3 unsaturations.5. Compound of generic formula (I) according to claim 1 , characterised in that Rrepresents a pyranose radical claim 1 , which may be partially or totally acetylated.6. Compound of generic formula (I) according to claim 1 , characterised in that Rand Rrepresent simultaneously a methyl radical.7. Compound of generic formula (I) according to claim 1 , characterised in that it is chosen from one of the following compounds:2-methoxy-4-(3,3,6,6-tetramethyl-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-1H-xanthen-9-yl)phenyl palmitate(9Z,12Z)-2-methoxy-4-(3,3,6,6-tetramethyl-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-1H-xanthen-9-yl)phenyl octadeca-9,1 2-dienoate(3R,4S,5S)-2-(acetoxymethyl)-6-(2-methoxy-4-(3,3,6,6-tetramethyl-1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-1H-xanthen-9-yl)phenoxy)tetrahydro-2H-pyran-3 ...

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Номер записи: 38
02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Автор: Diana Katharine Hunt, Jingye Zhou, Louis Plamondon, Robert B. Zahler, Roger B. Clark, Xiao-Yi Xiao
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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Номер записи: 39
02-05-2013 дата публикации

METHODS OF TREATING HIV INFECTION: INHIBITION OF DNA DEPENDENT PROTEIN KINASE

Номер: US20130109687A1
Автор: Cooper Arik, Nabel Gary J.
Принадлежит:

Methods of treating HIV-1 infection/AIDS in a patient infected with an HIV-1 virus comprising providing a DNA-PK inhibitor to the patient are provided herein. In one embodiment the DNA-PK inhibitor is compound of the Formula I 1. A method of treating HIV-1 infection in a patient infected with an HIV-1 virus comprising providing a therapeutically effective amount of a DNA-PK inhibitor to the patient.5. The method of claim 2 , wherein Ais N claim 2 , Ais O claim 2 , and Ais O.6. The method of claim 2 , wherein Ris hydrogen claim 2 , halogen claim 2 , C-Calkyl claim 2 , or C-Calkoxy.7. The method of wherein Ais CR claim 2 , Ais CR claim 2 , and Ais CR.8. The method of claim 7 , wherein Rand Rare independently chosen from hydrogen claim 7 , halogen claim 7 , C-Calkyl claim 7 , and C-Calkoxy.9. The method of claim 5 , wherein Rand Rare joined to form an optionally substituted phenyl ring.10. The method of claim 9 , wherein Rand Rare joined to form a phenyl ring that is unsubstituted or substituted with 1 claim 9 , 2 claim 9 , or 3 substituents independently chosen from hydrogen claim 9 , halogen claim 9 , hydroxyl claim 9 , cyano claim 9 , amino claim 9 , thiol claim 9 , C-Calkyl claim 9 , C-Calkoxy claim 9 , mono- or di-C-Calkylamino claim 9 , C-Chaloalkyl claim 9 , and C-Chaloalkoxy.11. The method of claim 9 , wherein Rand Rare joined to form an unsubstituted phenyl ring.13. The method of claim 12 , wherein Xis S.15. The method of claim 1 , wherein the DNA-PK inhibitor is provided together with instructions for treating an HIV-1 infection.16. A method of inhibiting CD4 cell death in a patient infected with HIV-1 comprisingPerforming a count of CD4 cells in the patient's blood; andAdministering an effective amount of a DNA-PK inhibitor to the patient. This application claims priority from U.S. Provisional Patent application No. 61/329,775, filed Apr. 30, 2010, which is hereby incorporated by reference in its entirety.This invention was made in part with government ...

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Номер записи: 40
09-05-2013 дата публикации

ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Номер: US20130116232A1
Автор: Govek Steven P., Kahraman Mehmet, Nagasawa Johnny Y., Smith Nicholas D.
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 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. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '1', 'sub': 1', '4, 'Ris C-Calkyl;'}{'sup': 2a', '2b, 'Rand Rare taken together with the N atom to which they are attached to form a substituted or unsubstituted monocyclic heterocycloalkyl, a substituted or unsubstituted bicyclic heterocycloalkyl, a substituted or unsubstituted monocyclic heteroaryl, or a substituted or unsubstituted bicyclic heteroaryl;'}{'sup': '3', 'sub': 1', '4', '1', '4, 'Ris C-Calkyl or C-Cfluoroalkyl;'}{'sup': 4', '9', '9', '10', '10, 'sub': 2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, —OR, —SR, —S(═O)R, —S(═O)R, C-Calkyl, C-Cfluoroalkyl, C-Cfluoroalkoxy, C-Calkoxy, and C-Cheteroalkyl;'}{'sup': 5', '9, 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, —OR, C-Calkyl, C-Cfluoroalkyl, C-Cfluoroalkoxy, C-Calkoxy, and C-Cheteroalkyl;'}{'sup': '6', 'sub': 1', '6', '1', '6', 'r', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, C-Calkyl, C-Cfluoroalkyl, CCfluoroalkoxy, and C-Calkoxy;'}{'sup': '7', 'sub': '3', 'Ris H or —CH;'}Y is —O— or —S—.46-. (canceled)7. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein:{'sup': '1', 'sub': '3', 'Ris —CH;'}{'sup': '3', 'sub': 3', '3, 'Ris —CHor —CF;'}{'sup': 2a', '2b, 'Rand Rare taken together with the N atom to which they are attached to form a substituted or unsubstituted pyrrolidinyl;'}X is —O—;Y is —O—.8. (canceled)11. (canceled)13. The compound ...

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Номер записи: 41
09-05-2013 дата публикации

IRE-1alpha INHIBITORS

Номер: US20130116247A1
Автор: PATTERSON John Bruce, Toro Andras, Wade Warren Stanfield, Wu Zhipeng, Yang Yun, ZENG Qingping, Zubovics Zoltan
Принадлежит: MANNKIND CORPORATION

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies. 114-. (canceled)16. A product comprising a compound of , wherein the product is selected from the group consisting of (a) a pharmaceutical composition comprising the compound of and a pharmaceutically acceptable vehicle; and (b) a complex comprising IRE-1α and the compound of .17. A method of inhibiting IRE-1α activity claim 15 , comprising contacting IRE-1α with a compound of or a prodrug or pharmaceutically acceptable salt thereof.18. The method of wherein the IRE-1α activity is selected from the group consisting of cleavage of RNA claim 17 , cleavage of mRNA claim 17 , RNA splicing claim 17 , and mRNA splicing.19. The method of wherein the IRE-1α activity is cleavage of mRNA and wherein the mRNA is selected from the group consisting of Blos1 mRNA claim 18 , DGAT2 mRNA claim 18 , CD59 mRNA claim 18 , and IRE-1α mRNA.20. The method of claim 18 , wherein the IRE-1α activity is inhibited to treat a disorder associated with the unfolded protein response claim 18 , comprising administering to a patient in need thereof the compound of or the prodrug or pharmaceutically acceptable salt thereof.21. The method of further comprising administering a therapeutic agent that induces or up-regulates IRE-1α expression.2202. The method of claim further comprising administering a therapeutic agent which is less effective when IRE-1α is expressed.23. The method of claim 20 , further comprising administering to the patient a proteasome inhibitor.24. The method of claim 20 , wherein the IRE-1α activity is inhibited to treat a disorder associated with a target of regulated IRE 1-dependent decay (RIDD) claim 20 , comprising administering to a patient in need ...

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Номер записи: 42
09-05-2013 дата публикации

INHIBITORS OF HIF AND ANGIOGENESIS

Номер: US20130116275A1
Автор: Van Meir Erwin G., Wang Binghe
Принадлежит:

Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided. 2. The compound of claim 1 , wherein A is —CRR—.3. The compound of claim 1 , wherein X is N claim 1 , Y is CR claim 1 , and Z is CR.4. The compound of claim 1 , wherein Y is N claim 1 , X is CR claim 1 , and Z is CR.5. The compound of claim 1 , wherein Z is N claim 1 , X is CR claim 1 , and Y is CR.6. The compound of claim 1 , wherein Ris a cyclopropyl claim 1 , cyclobutyl or cyclopentyl.7. The compound of claim 1 , wherein Rand Rare alkyl.8. The compound of claim 1 , wherein Ris alkyl other than methyl.9. The compound of claim 1 , wherein is a double bond claim 1 , E is CR claim 1 , and A is —CR═CR—.10. The compound of claim 1 , wherein Ris 4-methoxyphenyl claim 1 , 3 claim 1 ,4-dimethoxyphenyl claim 1 , or 3 claim 1 ,5-dimethylphenyl.11. The compound of selected from the group:N-cyclopentyl-N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-4-methoxy-N-phenylbenzenesulfonamide;N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,5-dimethyl-N-phenylbenzenesulfonamide;N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxy-N-phenylbenzenesulfonamide;N-cyclopentyl-N-((2,2-dimethyl-2H-pyrano[3,2-b]pyridin-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-cyclobutyl-N-((2,2-dimethyl-2H-pyrano[3,2-b]pyridin-6-yl)methyl)-3,4-dimethoxybenzenesulfonamide;N-butyl-N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxybenzenesulfonamide; andN-cyclopentyl-N-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-3,4-dimethoxybenzenesulfonamide or salts thereof.12. A pharmaceutical compositions comprising a compound as provided in or pharmaceutically acceptable salt and a pharmaceutically acceptable excipient.13. A method of treatment ...

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Номер записи: 43
09-05-2013 дата публикации

METHOD FOR ENANTIOSELECTIVE HYDROGENATION OF CHROMENES

Номер: US20130116450A1
Автор: SETCHELL Kenneth David Reginald, Sorokin Victor Dmitrievich
Принадлежит:

A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained. 2. The method according to wherein the step of providing a chromene compound further comprises the step of protecting any hydroxyl substituents among R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , or Rwith a hydroxyl protecting group.3. The method according to wherein after the step of hydrogenating claim 2 , the protecting group is removed by acidifying the product.4. The method according to wherein claim 1 , when the carbons in the 4 and 5 positions of the ligand (III) are both S configuration claim 1 , the resulting chiral carbon of compound (VI) is R configuration claim 1 , and wherein when the carbons in the 4 and 5 positions of the Ir catalyst (III) are both R configuration claim 1 , the resulting chiral carbon of compound (VI) is S configuration.5. The method according to wherein the enantiomeric chromane has the structure wherein R claim 1 , R claim 1 , R claim 1 , and Rand H claim 1 , Ris phenol claim 1 , and Ris OH.6. The method according to wherein X is O claim 1 , and Y is N.7. The method according to wherein Ris phenyl and Ris methyl.9. The method according to wherein the step of hydrogenating is conducted at 0-150 psig claim 1 , at a temperature of from about 5° C. to about room temperature claim 1 , and with a solvent selected from a lower alkyl dihalide solvent.10. The method according to wherein the concentration of the chiral Ir catalyst is between 0.1 to 10 mol % relative to the chromene.13. The method according to wherein the step of hydrogenating is conducted at about 0-150 psig claim 11 , at a temperature of about 5° C. to about room temperature claim 11 , and with a ...

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Номер записи: 44
23-05-2013 дата публикации

Process for producing refined nutraceutic extracts from artichoke waste and from other plants of the cynara genus

Номер: US20130131328A1
Автор: Annalisa Romani, Claudio Russo, Daniele Pizzichini, Massimo Pizzichini, Patrizia Pinelli
Принадлежит: ISR ECOINDUSTRIA Srl

Process for fractioning and refining natural products obtainable from waste vegetal material and particularly from artichoke ( Cynara scolymus ) production or from other plants of the Cynara genus such as the cultivated or wild cardoon. The process is based on the use of membrane separation technologies envisaging a tangential microfiltration (MF) phase on the raw decoction, followed by tangential ultrafiltration (UF) on the previous MF permeate and reverse osmosis (RO) on the UF permeate, in order to obtain a retentate rich in concentrated active ingredients and a permeate consisting of ultrapure water that is recycled for the preparation of the decoction. The process enables obtaining purified extracts of high biological valence to be used in the pharmaceutical industry, in the nutraceutic sector, in the cosmetics industry and for innovative products in the food industry.

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Номер записи: 45
30-05-2013 дата публикации

NOVEL MODULATORS OF NRF2 AND USES THEREOF

Номер: US20130137694A1
Автор: BATIST Gérald, WU Jian Hui
Принадлежит:

There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions. 1214.-. (canceled)15. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) claim 1 , (II) claim 1 , (III) claim 1 , (IV) or (V) according to claim 1 , in association with a pharmaceutically acceptable carrier.16. The pharmaceutical composition as claimed in for neuroprotection.17. The pharmaceutical composition as claimed in for the inhibition or the activation of a Nrf2 protein.18. The pharmaceutical composition as claimed in for overcoming drug resistance in cancer chemotherapy.1926.-. (canceled)27. A method for preventing or treating a disease which involves the abnormal activation and or expression level of a Nrf2 protein in a patient in need thereof claim 1 , and/or the abnormal inhibition of a Nrf2 protein claim 1 , the method comprising administering a therapeutically effective amount of a compound of formula (I) claim 1 , (II) claim 1 , (III) claim 1 , (IV) or (V) as defined in .28. (canceled)29. The method according to claim 27 , wherein said disease is an oxidative stress associated disease chosen from Parkinson's disease claim 27 , Parkinson's disease with dementia with Lewy body claim 27 , Huntington's disease claim 27 , multiple system atrophy (MSA) claim 27 , progressive supranuclear palsy (PSA) claim 27 , corticobasal degeneration (CBD) claim 27 , frontotemporal lobe degeneration claim 27 , atherosclerosis claim 27 , heart failure claim 27 , myocardial infarction claim 27 , Alzheimer's disease claim 27 , Fragile X syndrome claim 27 , and chronic fatigue.30. (canceled)31. The method of claim 27 , wherein said disease is a cancer.32. (canceled)33. The ...

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Номер записи: 46
30-05-2013 дата публикации

NEW COMPOUNDS FOR THE PREVENTION AND/OR TREATMENT OF OSTEOARTHROSIS

Номер: US20130137761A1
Автор: Prehm Peter, Stracke Dennis
Принадлежит: UNIVERSITAETSKLINIKUM MUEUENSTER

The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged. 4. The compound method according to claim 1 , wherein the compound is comprised in foodstuff.5. The method of claim 4 , wherein said foodstuff is a beverage.6. The method according to claim 1 , wherein said disease is osteoarthritis.8. The method according to wherein the disease is osteoarthritis.10. The method according to wherein the disease is osteoarthritis. The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged.Hyaluronan is the major water binding component of the extracellular matrix. It is a very large glycosaminoglycan that is exported into the extracellular matrix by fibroblasts or epithelial ...

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Номер записи: 47
06-06-2013 дата публикации

POLYMORPHIC FORMS OF WARFARIN POTASSIUM AND PREPARATIONS THEREOF

Номер: US20130143957A1
Автор: Bodhuri Prabhudas, Murthy Keshava K.S., Weeratunga Gamini
Принадлежит: APOTEX PHARMACHEM INC.

There is provided crystalline solvate forms of Warfarin potassium, termed APO-I and APO-II, and processes for making APO-I and APO-II. APO-I and APO-II are polymorphic solvate forms of Warfarin potassium. 1. APO-I polymorphic form of Warfarin potassium.2. The APO-I polymorphic form of Warfarin potassium of having a powder X-ray diffraction pattern comprising peaks claim 1 , in terms of degrees 2-theta claim 1 , at approximately 9.8 claim 1 , 15.3 claim 1 , 21.4 claim 1 , 22.3 claim 1 , 24.2 and 27.5.3. The APO-I polymorphic form of Warfarin potassium of having a powder X-ray diffraction pattern comprising peaks claim 1 , in terms of degrees 2-theta claim 1 , at approximately 9.8 claim 1 , 13.1 claim 1 , 15.3 claim 1 , 18.3 claim 1 , 19.5 claim 1 , 21.4 claim 1 , 22.3 claim 1 , 24.2 and 27.5.4. The APO-I polymorphic form of Warfarin potassium of having a 1% KBr FTIR spectrum comprising peaks claim 3 , in terms of cm claim 3 , at approximately 3454 claim 3 , 1721 claim 3 , 1622 claim 3 , 1600 and 1524.5. The APO-I polymorphic form of Warfarin potassium of having a DSC thermogram comprising an endothermic peak with a peak onset temperature of approximately 163.3° C. and a peak maximum of approximately 171.6° C.6. The APO-I polymorphic form of Warfarin potassium of having a PXRD diffractogram substantially similar to a PXRD diffractogram as depicted in .7. The APO-I polymorphic form of Warfarin potassium of having a FTIR spectrum substantially similar to a FTIR spectrum as depicted in .8. The APO-I polymorphic form of Warfarin potassium of having a DSC thermogram substantially similar to a DSC thermogram as depicted in .9. APO-II polymorphic form of Warfarin potassium.10. The APO-II polymorphic form of Warfarin potassium of having a powder X-ray diffraction pattern comprising peaks claim 9 , in terms of degrees 2-theta claim 9 , at approximately 9.7 claim 9 , 14.5 claim 9 , 21.6 claim 9 , 22.1 claim 9 , and 24.7.11. The APO-II polymorphic form of Warfarin potassium of ...

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Номер записи: 48
06-06-2013 дата публикации

DOSAGE UNIT COMPRISING A PROSTAGLANDIN ANALOG FOR TREATING CONSTIPATION

Номер: US20130143958A1
Автор: PATCHEN Myra L., UENO Ryuji
Принадлежит: SUCAMPO AG

A dosage unit for treating constipation in a human patient is described. The dosage unit of the invention includes a halogenated prostaglandin analog and a pharmaceutically suitable excipient. The dosage unit relieves constipation without substantial side effects. In particular, the dosage unit includes a prostaglandin (PG) analog represented by Formula (I) and/or its tautomers, and a pharmaceutically suitable excipient, wherein the dosage unit contains the PG analog in a range of about 6-96 μg: 2. The dosage unit of claim 1 , wherein said PG analog is the monocyclic tautomer of formula (I).3. The dosage unit of claim 1 , wherein said PG analog is the bi-cyclic tautomer of formula (I).4. The dosage unit of claim 1 , wherein said PG analog is present in the range of about 24-72 μg.5. The dosage unit of claim 3 , wherein said PG analog is present in the range of about 24-60 μg.6. The dosage unit of claim 1 , wherein said PG analog is present at about 48 μg.7. The dosage unit of claim 1 , wherein said PG analog is present at about 24 μg.8. The dosage unit of claim 1 , wherein said dosage unit is administered enough times per day so that the total daily dose of the PG analog is in the range of about 6-96 μg.9. The dosage unit of claim 1 , wherein said dosage unit is administered enough times per day so that the total daily dose of the PG analog is in the range of about 24-72 μg.10. The dosage unit of claim 1 , wherein said dosage unit is administered enough times per day so that the total daily dose of the PG analog is about 48 μg.11. The dosage unit of claim 1 , wherein said dosage unit is for single administration.12. The dosage unit of claim 1 , wherein said pharmaceutically suitable excipient is orally acceptable.13. The dosage unit of claim 1 , wherein said pharmaceutically suitable excipient is a medium chain fatty acid triglyceride.14. The dosage unit of claim 1 , wherein Aand Aare fluorine atoms.15. The dosage unit of claim 14 , wherein B is —COOH.16. The dosage ...

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Номер записи: 49
13-06-2013 дата публикации

Process for extracting materials from biological material

Номер: US20130149322A1
Автор: Frank Hollman, Geert-Jan Witkamp, Jacob Van Spronsen, Robert Verpoorte, Young Hae Choi
Принадлежит: UNIVERSITEIT LEIDEN

The invention is directed to a process for extracting materials from biological material, which process is characterized in that the naturally occurring biological material is treated with an extractant consisting of a deep eutectic solvent of natural origin or a an ionic liquid of natural origin to produce a biological extract of natural origin dissolved in the said solvent or ionic liquid.

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Номер записи: 50
13-06-2013 дата публикации

Reagents and methods for direct labeling of nucleotides

Номер: US20130150254A1
Автор: Jiang Ying, Link-Cole Ryan, Naleway John J.
Принадлежит:

The present invention provides systems and methods for production of activatable diazo-derivatives for use in labeling nucleotides. Labeling nucleotides is accomplished by contacting a stable hydrazide derivative of a detectable moiety with an activating polymer reagent which is used to directly label the nucleotide sample. Labeling occurs on the phosphate backbone of the nucleotide which does not perturb hybridization of the labeled nucleotide with its anti-sense strand. Since the method involves direct labeling, all types of nucleotides can be labeled without prior amplification or alteration. 2. The method of claim 1 , wherein the analyte is selected from the group consisting of phosphate claim 1 , carboxylic acid claim 1 , boronate claim 1 , nucleotide claim 1 , deoxynucleotide claim 1 , oligonucleotide and oligodeoxynucleotide.3. The method of claim 2 , wherein said nucleotide claim 2 , deoxynucleotide claim 2 , oligonucleotide or oligodeoxynucleotide comprises a nucleotide base selected from the group consisting of adenine claim 2 , thymidine claim 2 , cytosine claim 2 , guanine claim 2 , uridine claim 2 , purine and pyrimidine.4. The method of claim 2 , wherein said nucleotide is a constituent of a DNA or RNA polynucleotide.5. The method of claim 1 , wherein said detectable moiety is selected from the group consisting of a dye claim 1 , a fluorochrome claim 1 , an enzyme claim 1 , a chemiluminescent compound claim 1 , biotin claim 1 , digoxigenin claim 1 , avidin claim 1 , streptavidin claim 1 , an antibody and a lectin.6. The method of claim 1 , wherein said linking group comprises less than twenty carbon atoms.7. The method of claim 6 , wherein the carbon atoms of the linking group (L) are non-branched.8. The method of claim 1 , wherein said linking group comprises four carbon atoms and one heteroatom.9. The method of claim 8 , wherein the heteroatom is selected from the group consisting of oxygen and nitrogen.10. The method of claim 1 , wherein said ...

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Номер записи: 51
20-06-2013 дата публикации

TRPV1 Antagonists

Номер: US20130158067A1
Автор: Daanen Jerome F., Drizin Irene I., Gfesser Gregory A., Gomtsyan Arthur, Kort Michael E., Kym Philip R., Liu Huaqing, Mortell Kathleen H., Shrestha Anurupa, Voight Eric A., Woller Kevin R.
Принадлежит: AbbVie Inc.

Disclosed herein are compounds of formula (I): 2. The compound or salt according to claim 1 , wherein A is CH.3. The compound or salt according to claim 1 , wherein Xis O or N(R) claim 1 , and n is 2.4. The compound or salt according to claim 1 , wherein Xis O claim 1 , and n is 2.5. The compound or salt according to claim 1 , wherein Xis CH claim 1 , and n is 1.6. The compound or salt according to claim 1 , wherein L is CH.7. The compound or salt according to claim 1 , wherein L is a bond.8. The compound or salt according to claim 1 , wherein:A is CH;{'sup': 1', 'w, 'Xis O or N(R); and'}n is 2.9. The compound or salt according to claim 8 , wherein L is a bond.10. The compound or salt according to claim 8 , wherein L is CH.11. The compound or salt according to claim 10 , wherein Xis O.12. The compound or salt according to claim 1 , wherein:A is CH;{'sup': '1', 'sub': '2', 'Xis CH;'}n is 1; andLisa bond.14. The compound or salt according to claim 13 , wherein:A is CH;{'sup': 1', 'w, 'Xis O or N(R);'}n is 2; andL is a bond.15. The compound or salt according to claim 13 , wherein:A is CH;{'sup': '1', 'Xis O;'}n is 2; and{'sub': '2', 'L is CH.'}16. The compound or salt according to claim 13 , wherein:A is CH;{'sup': '1', 'sub': '2', 'Xis CH;'}n is 1; andL is a bond.18. The compound or salt according to claim 17 , wherein:A is CH;{'sup': '1', 'Xis O;'}n is 2; andL is a bond.19. The compound or salt according to claim 1 , wherein the compound is selected from the group consisting of:1-[(4R)-6,8-difluoro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-8-chloro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-2,2-dimethyl-7-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-7-chloro-2,2-bis(fluoromethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-4-yl]urea;1-[(4R)-7-fluoro-2,2- ...

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Номер записи: 52
20-06-2013 дата публикации

TOCOPHEROL DERIVATIVES AND METHODS OF USE

Номер: US20130158106A1
Автор: Breen Philip J., Compadre Cesar, Hauer-Jensen Martin, Kumar K. Sree, Varughese Kottayil
Принадлежит:

Tocol derivative compounds, compositions comprising these tocol derivatives and methods of using the tocol derivatives are provided herein. Specifically the tocol derivatives have a partially unsaturated hydrocarbon tail and are thus distinct from the tocopherols. The hydrocarbon tails do not have a trans carbon-carbon double bond in the second isoprene unit of the hydrocarbon tail and are distinct from the tocotrienols. The compounds are expected to allow improved interaction with the α-tocopherol transfer protein receptor than the tocotrienols and better bioactivity than the tocopherols. 1. A tocol derivative compound comprising a chroman group and a hydrocarbon tail , the hydrocarbon tail having three isoprene units , wherein at least one isoprene unit is unsaturated between carbon 2 and 3 of the isoprene unit and wherein the second isoprene unit in the hydrocarbon tail does not include a trans carbon-carbon double bond.23.-. (canceled)5. The compound of claim 4 , wherein the Torsion A angle between carbons 5′ claim 4 , 6′ claim 4 , 7′ claim 4 , and 8′ of the hydrocarbon tail of formula II and the Torsion B angle between carbons 6′ claim 4 , 7′ claim 4 , 8 claim 4 , and 9′ of the hydrocarbon tail of formula II can adopt conformations between 30° and 90°.6. The compound of claim 4 , wherein Z includes two double bonds.7. The compound of claim 6 , wherein Z includes a double bond between the 3′ and 4′ carbons.8. The compound of claim 4 , wherein Z includes a cis double bond between the 7′ and 8′ carbons.9. The compound of claim 8 , wherein Z includes three double bonds.10. The compound of claim 4 , wherein Z includes a cyclopropyl group including the 7′ and 8′ carbons.12. The compound of claim 1 , wherein the compound is a racemic mixture of stereoisomers.13. The compound of claim 1 , wherein either isomer is in enantiomeric excess of over 50% the compound is over 80% in the RS structure.14. The compound of claim 4 , wherein Ris an ester selected from —O(CO)CH ...

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Номер записи: 53
20-06-2013 дата публикации

RUTHENIUM-DIAMINE COMPLEXES AND METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUNDS

Номер: US20130158276A1
Автор: Hakamada Tomohiko, Nara Hideki, TOUGE Taichiro
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

Provided is a catalyst for asymmetric reduction, which can be produced by a convenient and safe production method, has a strong catalytic activity, and has excellent stereoselectivity. The present invention relates to a ruthenium complex represented by the following formula (1): wherein Rrepresents an alkyl group or the like; Y represents a hydrogen atom; X represents a halogen atom or the like; j and k each represent 0 or 1; Rand Reach represent an alkyl group or the like; Rto Reach represent a hydrogen atom, an alkyl group or the like; Z represents oxygen or sulfur; nrepresents 1 or 2; and nrepresents an integer from 1 to 3, a method for producing the ruthenium complex, a catalyst for asymmetric reduction formed from the ruthenium complex, and methods for selectively producing an optically active alcohol and an optically active amine using the catalyst for asymmetric reduction. 4. A method for producing a reduction product by reducing an organic compound in the presence of the ruthenium complex as set forth in and a hydrogen donor.5. A method for producing an optically active alcohol claim 1 , the method comprising reducing a carbonyl group of a carbonyl compound in the presence of the ruthenium complex according to and a hydrogen donor.6. A method for producing an optically active amine claim 1 , the method comprising reducing an imino group of an imine compound in the presence of the ruthenium complex according to and a hydrogen donor.7. The method according to claim 4 , wherein the hydrogen donor is selected from formic acid claim 4 , a formic acid alkali metal salt claim 4 , and an alcohol having a hydrogen atom on the α-position carbon atom substituted with a hydroxyl group.8. The method according to claim 4 , wherein the hydrogen donor is hydrogen.9. A catalyst for reduction claim 4 , comprising the ruthenium complex according to .10. The catalyst according to claim 9 , wherein the catalyst is a catalyst for asymmetric reduction. The present invention ...

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Номер записи: 54
27-06-2013 дата публикации

HYPOXIA INDUCIBLE FACTOR-1 PATHWAY INHIBITORS AND USES AS ANTICANCER AND IMAGING AGENTS

Номер: US20130164218A1
Автор: Goodman Mark M., Mun Jiyoung, Van Meir Erwin
Принадлежит: EMORY UNIVERSITY

This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein. 2. The compound of claim 1 , wherein X is OH optionally substituted with one or more claim 1 , the same or different R.3. The compound of wherein the compound comprises a carbon 11 or fluorine 18 tracer.4. The compound of selected from:N-[(2,2-Dimethyl-2H-chromen-6-yl)methyl]-N-(propan-2-yl)pyridine-2-sulfonamide;N-Cyclopropyl-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]pyridine-2-sulfonamide;N-[(2,2-Dimethyl-2H-chromen-6-yl)methyl]-N-(2-methylpropyl)pyridine-2-sulfonamide;N-(Cyclopropylmethyl)-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]pyridine-2-sulfonamide;N-(Cyclobutyl)-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]pyridine-2-sulfonamide;N-(Cyclopentyl)-N-[(2,2-dimethyl-2H-chromen-6-yl)methyl]pyridine-2-sulfonamide;N-[(8-Methoxy-2,2-dimethyl-2H-chromen-6-yl)methyl]pyridine-2-sulfonamide;N-[(2,2-Dimethyl-2H-chromen-6-yl)methyl]-N-(2-methylpropyl)pyridine-4-sulfonamide;N-[(2,2-Dimethyl-2H-chromen-6-yl)methyl]-N-(2-methylpropyl)-1-methyl-1H-imidazole-2-sulfonamide;N-[(2,2-Dimethyl-2H-chromen-6-yl)methyl]-N-(2-methylpropyl)-1,3-thiazole-2-sulfonamide;N-[(8-Hydroxy-2,2-dimethyl-2H-chromen-6-yl)methyl]-N-(propan-2-yl)pyridine-2-sulfonamide; andN-[(8-Hydroxy-2,2-dimethyl-2H-chromen-6-yl)methyl]-N-(propan-2-yl)pyridine-4-sulfonamide.5. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt and a pharmaceutically acceptable excipient.6. A method of treating cancer comprising administering an effective amount of a pharmaceutical composition of .7. The method of claim 6 , wherein the cancer is selected from glioblastoma (GBM) claim 6 , breast claim 6 , pancreatic claim 6 , colon claim 6 , metastatic lung cancers claim 6 , bladder cancer claim 6 , lung cancer claim 6 , breast cancer claim 6 , melanoma claim 6 , colon and ...

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Номер записи: 55
27-06-2013 дата публикации

TOCOTRIENOL DERIVATIVES AND ASSOCIATED METHODS

Номер: US20130165435A1
Автор: Behery Fathy A., El Sayed Khalid A., Sylvester Paul W.
Принадлежит:

Compositions of matter including (R)-2,5,6,8-tetramethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine and (R)-2,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine are disclosed herein. Further disclosed are methods of preparation of such compounds and the use of such compounds as anticancer agents. 1. A composition of matter comprising a compound selected from:(R)-2,5,6,8-tetramethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;(R)-2,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;(R)-2-allyl-5,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;(R)-2-benzyl-5,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;(R)-2-(1-benzylpiperidin-4-yl)-5,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;(R)-2-(1-benzylpiperidin-4-yl)-6,8-dimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-1,2,3,8,9,10-hexahydrochromeno[5,6-e][1,3]oxazine;2-((R)-5,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-9,10-dihydrochromeno[5,6-e][1,3]oxazin-2(1H,3H,8H)-yl)ethanol;2-((R)-6,8-dimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-9,10-dihydrochromeno[5,6-e][1,3]oxazin-2(1H,3H,8H)-yl)ethanol;2-((R)-5,7-dimethyl-7-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-8,9-dihydrochromeno[7,6-e][1,3]oxazin-3(2H,4H,7H)-yl)ethanol;3-((R)-5,6,8-trimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-9,10-dihydrochromeno[5,6-e][1,3]oxazin-2(1H,3H,8H)-yl)propan-1-ol;3-((R)-6,8-dimethyl-8-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)-9,10-dihydrochromeno[5,6-e][1,3]oxazin-2(1H,3H,8H)-yl)propan-1-ol;(R)-2-(3,3-diethoxypropyl)-5,6,8- ...

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Номер записи: 56
27-06-2013 дата публикации

ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF

Номер: US20130165479A1
Автор: Bayburt Erol K., Daanen Jerome F., Gomtsyan Arthur R., JR. Robert G., Latshaw Steven P., Lee Chih-Hung, Schmidt
Принадлежит: ABBVIE, INC.

The present application is directed to compounds that are TRPV1 antagonictc and have formula (I) 2. The compound according to wherein{'sub': 1', 'b, 'Yis —N(R)—;'}{'sub': '2', 'Yis O; and'}{'sub': 3', 'c, 'Yis —N(R)—.'}3. The compound according to claim 2 , wherein Lis cycloalkyl wherein the cycloalkyl is cyclopentyl or cyclohexyl.4. The compound of claim 3 , wherein Aris phenyl.5. The compound according to claim 4 , wherein the phenyl is unsubstituted or substituted with 1 claim 4 , 2 claim 4 , 3 claim 4 , 4 claim 4 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 4 , alkyl claim 4 , arylalkyl claim 4 , halogen claim 4 , haloalkyl claim 4 , or RRN— wherein Rand Rare each independently hydrogen claim 4 , alkyl claim 4 , or haloalkyl.6. The compound according to claim 5 , wherein{'sub': '1', 'Ris hydroxy; and'}{'sub': 2', '3', '4', '5, 'R, R, R, and Rare hydrogen.'}7. The compound according to claim 2 , wherein Lis a bond.8. The compound according to claim 7 , wherein Aris a monocyclic heterocycle fused to a phenyl.9. The compound of claim 8 , wherein{'sub': '1', 'Ris hydroxy;'}{'sub': '2', 'Ris hydrogen, and'}{'sub': '1', 'Aris 3,4-dihydro-2H-chromen-3-yl.'}10. The compound according to wherein Aris optionally substituted with 1 claim 9 , 2 claim 9 , 3 claim 9 , 4 claim 9 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 9 , alkyl claim 9 , arylalkyl claim 9 , halogen claim 9 , haloalkyl claim 9 , or RRN— wherein Rand Rare each independently hydrogen claim 9 , alkyl claim 9 , or haloalkyl.11. The compound according to claim 8 , wherein{'sub': '1', 'Ris hydroxy;'}{'sub': '2', 'Ris hydrogen; and'}{'sub': '1', 'Aris 3,4-dihydro-2H-chromen-4-yl.'}12. The compound according to wherein Aris optionally substituted with 1 claim 11 , 2 claim 11 , 3 claim 11 , 4 claim 11 , or 5 substituents as represented by Rand each Ris independently alkoxy claim 11 , alkyl claim 11 , arylalkyl claim 11 , halogen claim 11 , ...

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Номер записи: 57
27-06-2013 дата публикации

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Номер: US20130165649A1
Автор: Cazin Catherine
Принадлежит:

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

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Номер записи: 58
04-07-2013 дата публикации

METHODS FOR PURIFYING TRANS-(-)-DELTA9-TETRAHYDROCANNABINOL AND TRANS-(+)-DELTA9-TETRAHYDROCANNABINOL

Номер: US20130171259A1
Автор: Etinger Marina, Fedotev Irina, GUTMAN Arie L., Khanolkar Ram, Nisnevich Gennady A., Pertsikov Boris, Rukhman Igor, Tishin Boris
Принадлежит: Purdue Pharma L.P.

Methods for making trans-(−)-Δ-tetrahydrocannabinol and trans-(+)-Δ-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(−)-Δ-tetrahydrocannabinol composition is prepared by allowing a composition comprising (±)-Δ)-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(−)-Δ-tetrahydrocannabinol composition comprising at least about 99% by weight of trans-(−)-Δ-tetrahydrocannabinol based on the total amount of trans-(−)-Δ-tetrahydrocannabinol and trans-(+)-Δ-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(−)-Δ-tetrahydrocannabinol having a purity of at least about 98% based on the total weight of cannabinoids. 1. A trans-(−)-Δ-tetrahydrocannabinol composition comprising at least 99.0% by weight of trans-(−)-Δ-tetrahydrocannabinol and less than 0.05% of Δ-tetrahydrocannabinol acid based on the total amount of cannabinoids.2. The trans-(−)-Δ-tetrahydrocannabinol composition of claim 1 , comprising at least 99.5% by weight of trans-(−)-Δ-tetrahydrocannabinol based on the total amount of cannabinoids.3. The trans-(−)-Δ-tetrahydrocannabinol composition of claim 1 , comprising at least 99.9% by weight of trans-(−)-Δ-tetrahydrocannabinol based on the total amount of cannabinoids.4. The trans-(−)-Δ-tetrahydrocannabinol composition of claim 1 , wherein the composition comprises up to about 99.95% by weight of trans-(−)-Δ-tetrahydrocannabinol based on the total amount of cannabinoids.5. The trans-(−)-Δ-tetrahydrocannabinol composition of claim 1 , wherein the composition comprises up to about 99.98% by weight of trans-(−)-Δ-tetrahydrocannabinol based on the total amount of cannabinoids.6. A method for treating emesis claim 1 , comprising administering to a patient in need thereof an effective amount of the trans-(−)-Δ-tetrahydrocannabinol composition of .7. A method for treating loss ...

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Номер записи: 59
11-07-2013 дата публикации

EXTRACTION OF VITAMIN E FROM PLANT MATTER

Номер: US20130178519A1
Автор: Ramaswamy Kamala, Ramaswamy Rajendran
Принадлежит:

A process for the extraction of Vitamin E from annatto plant matter is disclosed wherein annatto seed matter is subjected, before extraction, to acidification using amla fruit matter. After the acidification, the mixture of the two plant matters is extracted by water. The acidification converts the vitamin E compounds in the plant matter into more water-soluble forms thus enhancing the vitamin yield. More of the vitamin is obtained in the ester form than in the form of vitamin alcohols. Processing time is reduced. 1. A process for extracting vitamin E and other nutrients and plant constituents from annatto plant matter , the process comprising the steps of:providing annatto plant matter;converting the plant matter of the providing annatto step into a form having increased contact area;providing amla plant matter;converting the plant matter of the providing amla step into a form having increased contact area;mixing the annatto form having increased contact area with the amla form having increased contact area;extracting the mixture formed in the mixing step with one of water and dilute aqueous plant extract at a predetermined temperature and for a predetermined period of time to obtain a first extract and spent plant matter; concentrating the first extract; anddrying the first extract to yield a vitamin E product.2. The process for extracting vitamin E from annatto plant matter as claimed in claim 1 , the annatto plant matter being derived from seed matter claim 1 , the amla plant matter being derived from fruit matter claim 1 , both the annatto seed and the amla fruit matters being converted into pulps and combined in the mixing step claim 1 , the mixing step producing a mixture that is more acidic than is the annatto plant matter.3. The process for extracting vitamin E from annatto plant matter as claimed in claim 2 , both said pulp matters being contacted for a length of time before being subjected to the extracting step claim 2 , said contacting being promoted by ...

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Номер записи: 60
18-07-2013 дата публикации

Novel IDO Inhibitors and Methods of Use Thereof

Номер: US20130183388A1
Автор: Malachowski William P., Muller Alexander J., Prendergast George C.
Принадлежит: LANKENAU INSTITUTE FOR MEDICAL RESEARCH

Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed. 1. (canceled)3. (canceled)4. (canceled)5. A pharmaceutical composition for the treatment of cancer comprising a pharmaceutically acceptable carrier and an effective amount at least one indoleamine 2 claim 2 ,3-dioxygenase (IDO) inhibitor claim 2 , wherein at least one of said IDO inhibitors is the compound of .616-. (canceled)17. The pharmaceutical composition of claim 5 , further comprising at least one signal transduction inhibitor (STI).18. (canceled)19. (canceled)20. The pharmaceutical composition of claim 5 , further comprising at least one chemotherapeutic agent.21. (canceled)22. (canceled)23. The pharmaceutical composition of claim 20 , wherein said at least one chemotherapeutic agent is selected from the group consisting of paclitaxel (Taxol®) claim 20 , cisplatin claim 20 , docetaxol claim 20 , carboplatin claim 20 , vincristine claim 20 , vinblastine claim 20 , methotrexate claim 20 , cyclophosphamide claim 20 , CPT-11 claim 20 , 5-fluorouracil (5-FU) claim 20 , gemcitabine claim 20 , estramustine claim 20 , carmustine claim 20 , adriamycin (doxorubicin) claim 20 , etoposide claim 20 , arsenic trioxide claim 20 , irinotecan claim 20 , and epothilone derivatives.2434.-. (canceled)35. A compound which is the hydroquinone form of the compound of .36. (canceled)37. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , and Xare H.38. The compound of claim 2 , wherein Xis R.39. The compound of claim 38 , wherein R is aryl.40. The compound of claim 37 , wherein Xis R.41. The compound of claim 39 , wherein R is aryl. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/918,516, filed on Mar. 16, 2007. The foregoing application is incorporated by reference herein.Pursuant to 35 U.S.C. Section 202(c), it is acknowledged that the United ...

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Номер записи: 61
18-07-2013 дата публикации

NOVEL DAIDZEIN ANALOGS AS TREATMENT FOR CANCER

Номер: US20130184475A1
Автор: BOUE Stephen M., BUROW Matthew E., Jiang Quan, WANG Guangdi, WIESE Thomas E.
Принадлежит:

Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth. 1. A pharmaceutical composition for use in the treatment of breast cancer , wherein said composition comprises at least one novel daidzein analog in an amount effective for the therapeutic treatment of breast cancer.2. A pharmaceutical composition for use in the treatment of any cancer , wherein said composition comprises at least one novel daidzein analog in an amount effective for the therapeutic treatment of any cancer.3. A method of minimizing or treating cancer or tumor growth in an animal in need thereof , comprising administering to said animal a composition comprising an effective amount of at least one novel daidzein analog.4. The composition of wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-8 claim 1 ,8-dimethyl-8H-pyrano[2 claim 1 ,3-f]chromen-4-one.5. The composition wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-7-methoxychromen-4-one.6. The composition of wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-7-ethoxychromen-4-one.7. The composition of wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-7-propoxychromen-4-one.8. The composition of wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one.9. The composition of wherein the at least one novel daidzein analog is the compound 7-Butoxy-3-(4-hydroxyphenyl)chromen-4-one.10. The composition of wherein the at least one novel daidzein analog is the compound 3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one.11. The composition of wherein the at least one novel daidzein analog is the compound 7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one.12. The composition of wherein the at least one novel daidzein analog is the ...

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Номер записи: 62
18-07-2013 дата публикации

PREPARATION OF LUBIPROSTONE

Номер: US20130184476A1
Автор: Dahanukar Vilas Hareshwar, Eda Vishnu Vardhana Verma Reddy, Jackson Mark, Joseph Suju Chuttippari, Ramdas Sandip Khobare
Принадлежит:

Aspects of the present application relate to process for the preparation of lubiprostone. 2. The process of claim 1 , wherein the reagent in step (a) comprises one or more of sodium carbonate claim 1 , potassium carbonate claim 1 , lithium carbonate and cesium carbonate.3. The process of claim 1 , wherein the solvent comprises any one or more of methanol claim 1 , ethanol claim 1 , 1-propanol and 2-propanol.4. The process of claim 1 , wherein the reagent in step (b) comprises one or more of pyridinium-p-toluenesulfonate claim 1 , pyridinium dichromate claim 1 , carbonyldiimidazole and dicyclohexylcarbodiimide.5. The process of claim 1 , wherein the oxidizing agent in step (g) comprises pyridine-sulfur trioxide.6. The process of claim 1 , wherein the acid in step (h) comprises one or more of hydrochloric acid claim 1 , hydrobromic acid claim 1 , and sulfuric acid. This application claims priority to Indian Provisional Application 2389/CHE/2011, filed on Jul. 13, 2011 and U.S. Provisional Application No. 61/527,737, filed on filed on Aug. 26, 2011; all of which are hereby incorporated by reference in their entirety.Aspects of the present application relates to process for the preparation of lubiprostone and intermediates thereof.Lubiprostone is chemically described as (−)-7-[(2R,4aR,5R,7aR)-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[b]pyran-5-yl]heptanoic acid. It has the structure of formula (I).Lubiprostone is a locally acting chloride channel activator and is indicated for: (a) treatment of chronic idiopathic constipation in adults; and (b) treatment of irritable bowel syndrome with constipation (IBS-C) in women 18 years old; and is contained in products sold as Amitiza®.U.S. Pat. No. 5,284,858 discloses 13,14-dihydro-15-keto-16,16-difluoro-prostaglandins. U.S. Pat. No. 7,355,064 discloses a process for the preparation of 15-keto-prostaglandin E derivatives by hydrolyzing or deprotecting the intermediate of a 15-keto-prostaglandin E derivative having ...

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Номер записи: 63
25-07-2013 дата публикации

FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS

Номер: US20130190497A1
Автор: GUBERNATOR Niko Gert, Sames Dalibor, Sulzer David, VADOLA Paul
Принадлежит: The Trustees of Columbia University in the City of New York

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; Ris —H, —OH, —O—R, —N(H)—R, —N(H)—(CH)—NH, —N(R)(R), or a piperazine cation; Ris either covalently bound to R, or is —H, or is covalently bound to Rso as to form a substituted or unsubstituted pyrrole or Ris covalently bound to Ror Ror R; or Rand Rare covalently joined to form an aromatic ring; Ris either covalently bound to Rso as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen Ris ═O; Ris, inter alia, —H, —OH, or —RNH; Ris, inter alia, —H, —OH, or —RNH, and Ris either is covalently bound to Ror is —H, or Ris covalently bound to Ror Ror R. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds. 2. (canceled)3. The compound of claim 1 , wherein W is a mono-substituted heterocyclyl group wherein the heteroatom is nitrogen.4. The compound of claim 1 , wherein W is a di-substituted heterocyclyl group wherein the heteroatoms are each nitrogen.5. The compound of claim 1 , wherein W is a piperazine group.6. (canceled)7. (canceled)8. (canceled)9. The compound of claim 1 , wherein Ris —H claim 1 , —CHCHNH claim 1 , —CHCHNHCH claim 1 , —CHCH(CH)NH claim 1 , —NHCHCHNH claim 1 , —CHNH claim 1 , or a piperazine group.10. The compound of claim 1 , wherein Ris —CHCHNH claim 1 , a piperazine group claim 1 , a piperazine cation claim 1 , a pyrrolidin-2-yl group claim 1 , a piperidinyl group.11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)18. (canceled)20. (canceled)22145.-. (canceled)146. The compound of claim 21 ,wherein{'sub': 1', '34', '2, 'claim-text': {'sub': 32', '3', '2', '3, ' ...

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Номер записи: 64
01-08-2013 дата публикации

Diarylamine-based fluorogenic probes for detection of peroxynitrite

Номер: US20130196362A1
Автор: Dan Yang, Pao Peng
Принадлежит: University of Hong Kong HKU

Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.

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Номер записи: 65
01-08-2013 дата публикации

PRODUCTION OF LIPOXYGENASE INHIBITORS VIA FUNGAL BIOSYNTHETIC PATHWAY

Номер: US20130197071A1
Автор: Chiang Yi-Ming, Oakley Berl R., Somonza Amber D., Wang Clay
Принадлежит: UNIVERSITY OF SOUTHERN CALIFORNIA

The invention provides methods for producing lipoxygenase inhibitors including the steps set forth in Schemes 2 and 3, and uses of the inhibitors produced by the methods set forth herein in to treat various disease states. 2. A method for producing lipoxygenase inhibitors comprising the steps set forth in (Scheme 3).3. The method of or , wherein compound 5 is obtained from a microbial strain.4Aspergillus nidulans.. The method of claim 3 , wherein the microbial strain is a mutant strain of5. The method of or claim 3 , wherein N-halosuccinimides is any one or more of N-Chlorosuccinimide (NCS) claim 3 , N-Bromosuccinimide (NBS) and N-Iodosuccinimide (NIS).6. The method of claim 1 , wherein the oxidizing agent is lead tetracetate.7. The method of or claim 1 , wherein the lipoxygenase is any one or more of 5-LOX claim 1 , 8-LOX claim 1 , 12-LOX and 15-LOX.8. The method of or claim 1 , wherein lipoxygenase inhibitor is an azaphilone.9. The method of claim 8 , wherein an azaphilone is sclerotiorin or analogs thereof.10. A lipoxygenase inhibitor produced by the method of or .11. The lipooxygenase inhibitor of claim 10 , wherein the inhibitor is an azaphilone or an analog thereof.12. The lipoxygenase inhibitor of claim 11 , wherein the azaphilone or analog thereof is any one or more of compounds 7 claim 11 , 8 claim 11 , 9 claim 11 , 10 claim 11 , 11 claim 11 , 12 claim 11 , 13 or 14.13. A pharmaceutical composition comprising the lipoxygenase inhibitor of claim 10 , and a pharmaceutically acceptable carrier.14. A method for treating inflammatory diseases in a subject in need thereof comprising:{'claim-ref': {'@idref': 'CLM-00010', 'claim 10'}, '(i) providing a composition comprising the lipoxygenase inhibitor of , and'}(ii) administering an effective amount of the composition to the subject, thereby treating inflammatory diseases in the subject.15. The method of claim 14 , wherein the inflammatory disease is any one or more of allergies claim 14 , asthma claim 14 , ...

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Номер записи: 66
01-08-2013 дата публикации

CYCLIZATION METHODS

Номер: US20130197241A1
Автор: Baire Beeraiah, Hoye Thomas R., Niu Dawen, Willoughby Patrick H., Woods Brian P.
Принадлежит: Regents of the University of Minnesota

The invention provides methods for cyclizing poly-yne compounds under mild conditions to provide cyclic compounds. 1. A method comprising cyclizing a tri-yne compound at a temperature below about 300° C. to provide a polycyclic compound.2. A method comprising cyclizing a nonaromatic compound comprising at least three alkyne groups at a temperature below about 300° C. to provide a polycyclic compound.3. A method comprising cyclizing a first compound that comprises two or more alkyne groups with a second compound that comprises at least one alkyne group at a temperature below about 300° C. to provide a cyclic compound.5. The method of wherein W comprises 2 claim 4 , 3 claim 4 , 4 claim 4 , or 5 alkyne groups.6. The method of wherein W comprises 2 or 3 alkyne groups.7. The method of wherein X is a linking group that comprises 2-20 carbon atoms and at least one severable group.8. The method of wherein X is a linking group that comprises 2-10 carbon atoms and at least one severable group.9. The method of wherein the severable group is selected from an ester claim 4 , an amide claim 4 , a carbonate claim 4 , a carbamate claim 4 , an ether claim 4 , a silylether claim 4 , an alkene claim 4 , a urea claim 4 , a sulfide claim 4 , a disulfide claim 4 , a borate ester claim 4 , a borinate ester claim 4 , an aluminate ester claim 4 , a silicate ester claim 4 , a hydrazine claim 4 , an azo moiety claim 4 , a sulfone claim 4 , a phosphate ester claim 4 , and a phosphonate ester.10. The method of wherein X is a non-aromatic linking group that comprises 2-20 carbon atoms.11. The method of wherein X is a non-aromatic linking group that comprises 2-10 carbon atoms.12. The method of wherein Y comprises 1 claim 4 , 2 claim 4 , 3 claim 4 , or 4 alkyne groups.13. The method of wherein Y comprises 1 or 2 alkyne groups.14. The method of wherein Y has only 1 or 2 alkyne group.15. The method of further comprising contacting the polycyclic compound or the cyclic compound with a benzyne ...

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Номер записи: 67
08-08-2013 дата публикации

Sugar plant derived by-products and methods of production thereof

Номер: US20130203688A1
Автор: Genevieve Beland, Julie Barbeau
Принадлежит: FEDERATION DES PRODUCTEURS ACERICOLES DU QUEBEC

The present document describes a nutraceutical or cosmeceutical composition for the prophylaxis of an ailment comprising a therapeutically effective amount of a sugar plant syrup filtration residue in association with a pharmaceutically acceptable carrier. The present document also describes a nutraceutical or cosmeceutical composition for improving health condition of skin. The present document describes a method of producing a sugar plant syrup-derived product; wherein the improvement is characterized in the step of: collecting a sugar plant syrup residue during the production of sugar or syrup to produce a syrup-derived by-product.

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Номер записи: 68
08-08-2013 дата публикации

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

Номер: US20130203727A1
Автор: Babaoglu Kerim, Bacon Elizabeth, Bjornson Kyla, Guo Hongyan, Halcomb Randall L., Hrvatin Paul, Link John O., Liu Hongtao, McFadden Ryan, Mitchell Michael L., Roethle Paul, Taylor James, Trenkle James D., Vivian Randall W., Xu Lianhong
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). 2. The compound of wherein Ris (C-C)alkyl claim 1 , (C-C)alkenyl or —O(C-C)alkyl wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claim 1 , halo claim 1 , oxo and —CN; and wherein Ris H.4. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —OH, —O(C-C)alkyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo;'}{'sub': 3', '14', '3', '14', '3', '7, 'sup': 1', '1, 'b) (C-C)carbocycle, wherein (C-C)carbocycle is optionally substituted with one or more Zgroups, wherein two Zgroups together with the atom or atoms to which they are attached optionally form a (C-C)carbocycle or heterocycle; and'}{'sup': 7', '1, 'c) aryl, heteroaryl and fused-heterocycle, wherein any aryl, heteroaryl and fused-heterocycle is substituted with one or more Zgroups and optionally substituted with one or more Zgroups.'}5. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and ...

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Номер записи: 69
08-08-2013 дата публикации

Compounds for Prevention of Cell Injury

Номер: US20130203830A1
Автор: HENNING Robert Henk, Talaei Fatemeh, Van der Graaf Adrianus C.
Принадлежит: SULFATEQ B.V.

The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation. 1. A compound capable of increasing or maintaining the H2S level in a cell for use in the prevention of cell injury and/or protection of a cell.2. The compound of claim 1 , wherein the increase or maintenance of the H2S level in the cell is mediated by endogenous H2S production in a cell for use in the prevention of cell injury and/or protection of a cell.3. The compound of claim 1 , wherein the compound is selected from the group consisting of serotonin claim 1 , baclofen claim 1 , dopamine claim 1 , propofol claim 1 , melatonin claim 1 , histamine claim 1 , D/L phenylserine claim 1 , trolox claim 1 , reduced trolox and/or a salt claim 1 , a derivate claim 1 , or a precursor thereof.4. The compound of claim 1 , wherein the endogenous H2S production is mediated by cystathionine beta synthase (CBS).5. The compound of claim 1 , wherein the compound is transferred into the cell via active transport.6. The compound of claim 1 , wherein the prevention of cell injury and/or the protection of a cell against injury is achieved in the treatment of subjects suffering from a disorder that mediates oxidative stress to cells.7. The compound of claim 1 , wherein the prevention of cell injury and/or protection of the cells is achieved in the treatment of subjects suffering from ischemic injury and/or reperfusion claim 1 , neuromodulation claim 1 , hypertension claim 1 , inflammation claim 1 , hemorrhagic shock claim 1 , hypothermia claim 1 , diabetes or edema.8. The compound of ...

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Номер записи: 70
15-08-2013 дата публикации

ANDROGEN INDUCED OXIDATIVE STRESS INHIBITORS

Номер: US20130210772A1
Автор: BASU Hirak S., Church Dawn R., Mehraein-Ghomi Farideh, Wilding George, ZARLING David A.
Принадлежит: COLBY PHARMACEUTICAL COMPANY

Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer. 2. The compound of wherein Ris OH.3. (canceled)4. (canceled)5. The compound of wherein Ris S(═O)OH.6. The compound of wherein Ris —N═N-aryl.7. The compound of wherein aryl is naphthyl.8. (canceled)9. The compound of wherein Ris OH.10. The compound of wherein n is 1.11. (canceled)12. The compound of wherein Ris S(═O)OH.1323.-. (canceled)24. The compound of wherein Ris —N═N-aryl.25. The compound of wherein aryl is naphthyl.2633.-. (canceled)3567.-. (canceled)69. (canceled)70. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , prodrug or metabolite thereof and a pharmaceutically acceptable binder claim 1 , excipient claim 1 , or diluent thereof.71. A method of inhibiting the growth of human prostate cancer in a subject comprising administering to a subject in need thereof an inhibitor of the JunD-AR interaction.72. The method of wherein the inhibitor of the JunD-AR interaction is a compound of .73. A method of preventing interaction of androgen receptor with other transcription factors comprising contacting a compound of with an androgen receptor and/or a transcription factor wherein the interaction of androgen receptor with other transcription factors is prevented or minimized.74. The method of wherein the transcription factor is AP-1 transcription factor JunD.75. A method of reducing oxidative stress and/or blocking androgen-induced oxidative stress in cancer cells and/or tissues comprising contacting the cancer cells and/or tissues with a compound of any of wherein the oxidative stress in the cancer cell and/or tissue is reduced or the androgen-induced oxidative stress in the cancer cell and/or tissue is blocked.76. (canceled)77. The pharmaceutical composition of for the treatment of a prostate disease or disorder.78. The pharmaceutical ...

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Номер записи: 71
15-08-2013 дата публикации

COMPOUNDS, METHODS OF PREPARATION AND USE THEREOF FOR TREATING CANCER

Номер: US20130210906A1
Автор: BIAN Zhaoxiang, CHAN Albert Sun-Chi, CHEN Kaixian, Chen Shilin, LAO Yuanzhi, TAN Hongsheng, XIA Zhengxiang, XU Hongxi, YANG Dajian
Принадлежит: HONG KONG BAPTIST UNIVERSITY

The present invention provides two compounds, namely Compound A and B, as the potential anticancer drug, and a composition comprising said Compound A and/or B for treating cancer or tumor related diseases. The present invention also relates to methods of preparing the compounds from a natural source and a composition comprising the compounds, and using the same for treating cancer or tumor related diseases. 2. The composition of claim 1 , wherein said xanthone derivatives having said formula A is 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-tetrahydroxy-3-methoxy-4 claim 1 ,7 claim 1 ,8-tri(3-methylbut-2-enyl)-xanthone.3. The composition of claim 1 , wherein said xanthone derivatives having said formula B is 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-tetrahydroxy-2 claim 1 ,3-dimethoxy-4 claim 1 ,7 claim 1 ,8-tri(3-methylbut-2-enyl)-xanthone.4. The composition of is administered to a subject in needs thereof as anti-cancer/anti-tumor drugs or treatments.5. The composition of claim 1 , wherein said xantheone derivatives having said formula A or B are extracted and separated from a natural source.6. The composition of claim 5 , wherein the natural source is a herb.7Garcinia nujiangensis.. The composition of claim 6 , wherein the herb is9. The method of claim 8 , wherein said xanthone derivatives having said formula A is 1 claim 8 ,2 claim 8 ,5 claim 8 ,6-tetrahydroxy-3-methoxy-4 claim 8 ,7 claim 8 ,8-tri(3-methylbut-2-enyl)-xanthone.10. The method of claim 8 , wherein said xanthone derivatives having said formula B is 1 claim 8 ,2 claim 8 ,5 claim 8 ,6-tetrahydroxy-2 claim 8 ,3-dimethoxy-4 claim 8 ,7 claim 8 ,8-tri(3-methylbut-2-enyl)-xanthone.11. The method of claim 8 , wherein said xanthone derivatives having said formula A or B are extracted and separated from a natural source.12. The method of claim 11 , wherein the natural source is a herb.13Garcinia nujiangensis.. The method of claim 12 , wherein the herb is15. The method of claim 14 , wherein said extraction in (a) is performed ...

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Номер записи: 72
15-08-2013 дата публикации

COUMARIN-CHALCONES AS ANTICANCER AGENTS

Номер: US20130210909A1
Автор: Kumar Abdhesh, Kumar Manoj, Sarkar Jayanta, Sashidhara Koneni Venkata, Sinha Sudhir Kumar
Принадлежит: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

The present invention relates to certain coumarin/chalcone compounds or a pharmaceutically acceptable salt thereof. The present invention particularly relates to the coumarin/chalcone compounds as anticancer agents useful for the treatment of cancer. The present invention also relates to the process of preparation of the said compounds. 2. The compound as claimed in wherein pharmaceutically acceptable salt is selected from a group consisting of solvates claim 1 , amides claim 1 , esters claim 1 , ethers claim 1 , chemically protected forms claim 1 , and prodrugs of compound of formula VI.3. The compound of formula (VI) as claimed in claim 1 , useful as an anticancer agent for the treatment or prevention of cervical carcinoma claim 1 , oral squamous cell carcinoma or lung or prostate carcinoma or brain tumor.4. The compound as claimed in wherein the compound has a ICvalue ranging between 1.53 to 146.82 μM.5. The compound as claimed in wherein the representative compounds comprising:I. Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxylate (S-009-0131)II. Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-phenylprop-1-enyl)-2H-chromene-3-carboxylate (S-009-0132)III. Methyl 8-sec-butyl-2-oxo-6-(3-oxo-3-phenylprop-1-enyl)-2H-chromene-3-carboxylate (S009-0133)IV. Ethyl 8-sec-butyl-6-(3-(4-chlorophenyl)-3-oxoprop-1-enyl)-2-oxo-2H-chromene-3-carboxylate (S-009-0135)V. Methyl 8-sec-butyl-6-(3-(4-chlorophenyl)-3-oxoprop-1-enyl)-2-oxo-2H-chromene-3-carboxylate (S-009-0136)VI. (E)-8-tert-Butyl-N,N-diethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1992)VII. (E)-8-sec-Butyl-N-methyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1994)VIII. (E)-8-sec-Butyl-N-ethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1995)IX. (E)-8-sec-Butyl-N,N-diethyl-2-oxo-6-(3-oxo-3-p-tolylprop-1-enyl)-2H-chromene-3-carboxamide (S010-1996)X. (E)-Ethyl 8-sec-butyl-2-oxo-6-(3-oxo-3-(3,4,5-trimethoxyphenyl)prop-1-enyl)-2H- ...

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Номер записи: 73
15-08-2013 дата публикации

PROCESS FOR THE MANUFACTURE OF TMHQ

Номер: US20130211080A1
Автор: Bonrath Werner, Netscher Thomas, Schutz Jan, Wüstenberg Bettina
Принадлежит: DSM IP ASSETS B.V.

The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same. 1. A process for the manufacture of 2 ,3 ,5-trimethyl-hydro-p-benzoquinone comprising the following steps:a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone;b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formaldehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone;c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone;wherein the organic solvent used in steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, methyl tert.-amyl ether, methoxycyclopentane and any mixtures thereof.2. The process according to claim 1 , wherein the organic solvent in all steps a) claim 1 , b) ...

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Номер записи: 74
15-08-2013 дата публикации

ACYLATIONS IN MICRO REACTION SYSTEMS

Номер: US20130211105A1
Автор: Bonrath Werner, Koschinski Ingo, Van Oordt Thomas
Принадлежит:

A method for acylating tertiary alcohols and phenolic compounds with carboxylic acids or their anhydrides in micro-reaction systems wherein the acylation is effected in the absence of any catalyst including water at residence times of at most 30 minutes. 1. A method for acylating tertiary alcohols and phenolic compounds with carboxylic acids or their anhydrides in micro-reaction systems characterized in that the acylation is effected in the absence of any catalyst including water at a residence time of at most 30 minutes.2. The method of claim 1 , wherein the micro-reaction system is a modular micro-reaction system.3. The method of claim 1 , wherein the tertiary alcohol is an aliphatic or araliphatic alcohol.4. The method of claim 1 , wherein the acylation is effected with an acid anhydride claim 1 , particularly with acetic acid anhydride.5. The method of claim 1 , wherein the tertiary alcohol is an allylic alcohol claim 1 , particularly linalool claim 1 , dehydrolinalool claim 1 , nerolidol or isophytol.6. The method of claim 1 , wherein the phenolic compound is a tocopherol or tocotrienol claim 1 , particularly d claim 1 ,l-alpha-tocopherol.7. The method of claim 1 , wherein the acylation is effected at a temperature in the range of 80-280° C. claim 1 , preferably of 100-250° C.8. The method of claim 1 , wherein the acylation is effected under a pressure sufficient to prevent boiling of the reaction mixture. The present invention relates to a method for acylating tertiary alcohols and phenolic compounds in modular micro-reaction systems.Acylations of alcohols, especially acetylations, are among the most important reactions in organic chemistry and useful in the preparation of commercially valuable products, e.g., pharmaceuticals, agrochemicals or flavors, and intermediates therefore.On the one hand acylations of organic hydroxy compounds can be carried out by reacting the hydroxy compound with an acid. Better yields are normally achieved if acid derivatives are ...

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Номер записи: 75
22-08-2013 дата публикации

COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR

Номер: US20130217685A1
Автор: Ryder Sean
Принадлежит: University of Massachusetts

The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders. 1. A method for treating or preventing a parasitic associated state in a subject comprising administering to said subject an effective amount of an RNA binding modulatory compound , such that said parasitic associate state is treated or prevented.3. The method of claim 1 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 1 , and pharmaceutically acceptable salts thereof.4. The method of claim 1 , wherein said subject is a plant claim 1 , an animal or a human.56-. (canceled)7. The method of claim 1 , wherein said parasitic associated state is a parasitic infestation or parasitic re-infestation or a disease caused by a parasitic infestation.8. (canceled)9. The method of claim 1 , wherein said method includes protecting plants from a parasitic infestation claim 1 , inhibiting embryogenesis in a parasite or in a subject suffering from a parasitic infestation claim 1 , or reducing parasitic burden in soil claim 1 , in plants or in an animal suffering from a parasitic infection.10. The method of claim 1 , wherein said parasite is a helminth.11. The method of claim 10 , wherein said helminth is selected from the group consisting of a cestode claim 10 , a trematode and a nematode.12. (canceled)13. A method for inhibiting embryogenesis in a parasite claim 10 , comprising contacting said parasite with an effective amount of an RNA binding modulatory compound claim 10 , such that said embryogenesis is inhibited.15. The method of claim 13 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 13 , and pharmaceutically acceptable salts thereof.16. The method of claim 13 , wherein the parasite is present in a subject.1719-. (canceled)20. The method of claim 13 , wherein said ...

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Номер записи: 76
29-08-2013 дата публикации

CHIRAL COMPOUNDS, COMPOSITIONS, PRODUCTS AND METHODS EMPLOYING SAME

Номер: US20130224136A1
Автор: Boissy Raymond, deLong Mitchell A., Kvalnes Kalla Lynn
Принадлежит: LASYA, INC.

Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein. 15. A composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) from about 0.0001% to about 99.999% of a compound according to formula (I) of ;'}{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, '(b) from about 99.999% to about 0.0001% of a compound according to formula (II) of ; and'}(c) optionally, a pharmaceutically acceptable carrier,{'sup': 1', '2', '1, 'claim-ref': [{'@idref': 'CLM-00001', 'claim 1'}, {'@idref': 'CLM-00008', 'claim 8'}], 'wherein at least one of the substituents X, X, A, B, Z and Rin the compound according to formula (I) of is different from the corresponding substituent in the compound according to formula (II) of .'}16. A product comprising a compound according to .1722-. (canceled)2318. The product according to claim claim 1 , wherein said product is a skin care composition.24. The product according to claim 23 , further comprising a dermatologically acceptable carrier.25. (canceled)26. (canceled)27. A method of lightening mammalian skin claim 1 , said method comprising topically applying a compound according to to an area of skin in need of treatment.2831-. (canceled)32. A product comprising a compound according to .33. The product according to claim 32 , wherein said product is a skin care composition.34. The product according to claim 33 , further comprising a dermatologically acceptable carrier.35. A method of lightening ...

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Номер записи: 77
29-08-2013 дата публикации

SKIN LIGHTENING COMPOSITIONS

Номер: US20130224137A1
Автор: Chambournier Gilles, deLong Mitchell A., Ewell Kevin R., Kvalnes Kalla Lynn, Witwit Moe
Принадлежит: LASYA, INC.

Compositions and methods for lightening mammalian skin are described herein. 2. The composition of claim 1 , wherein Z is O.3. The composition of claim 1 , wherein A and B are taken together with the atoms to which they are attached to form an optionally substituted ring having from 4-9 member atoms.4. The composition of claim 1 , wherein A and B are taken to taken together with the atoms to which they are attached to form a ring having 6 member atoms.12. The composition of claim 1 , wherein the compound of formula I is 4-(tetrahydro-2H-pyran-2-yloxy)phenol.13. The composition of claim 1 , wherein the compound of formula I is present in the composition at a concentration of about 0.5 wt. % to about 10 wt. %.14. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid claim 1 , tocopherol claim 1 , butylated hydroxybenzoic acid claim 1 , butylated hydroxytoluene claim 1 , butylated hydroxyanisole claim 1 , uric acid claim 1 , gallic acid claim 1 , sorbic acid claim 1 , glutathione claim 1 , and esters and salts of any thereof.15. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid or a salt thereof claim 1 , ascorbyl phosphate or a salt thereof claim 1 , ascorbyl palmitate or a salt thereof claim 1 , tocopherol or a salt thereof claim 1 , tocopheryl acetate and sodium metabisulfite.16. The composition of claim 1 , comprising at least two antioxidants.17. The composition of claim 1 , comprising at least three antioxidants.18. The composition of claim 1 , comprising at least four antioxidants.19. The composition of claim 1 , comprising at least five antioxidants.20. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant is present in an amount of about 0.01 wt. % to about 3.0 wt. %.21. The composition of claim 1 , wherein the composition comprises an antioxidant ...

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Номер записи: 78
29-08-2013 дата публикации

WOGONIN FOR THE PREVENTION AND THERAPY OF CARDIAC HYPERTROPHY

Номер: US20130225530A1
Автор: Krammer H. Peter, Li-Weber Min, Polier Gernot
Принадлежит: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM

The present invention relates to a pharmaceutical composition for use as a medicament for the treatment or prophylaxis of cardiac hypertrophy, comprising at least one compound of formula (I), wherein: Ris e.g. hydrogen, —CH, Ris e.g. hydrogen, —CH, Ris hydrogen, —OH, —NH; Ris hydrogen, —OH; Ris hydrogen, —OH; Ris e.g. —OCHor a pharmaceutically acceptable salt, and at least one pharmaceutical excipient. 3. A pharmaceutical composition for use as a medicament for the treatment and/or prophylaxis of cardiac hypertrophy claim 1 , comprising at least one compound of formula (I) claim 1 , according to claim 1 , wherein the composition comprises at least one compound of formula (I) claim 1 , in which Rdenotes —OCH claim 1 , or a pharmaceutically acceptable salt or an isomeric or polymorphic form thereof.4. A pharmaceutical composition for use as a medicament for the treatment and/or prophylaxis of cardiac hypertrophy claim 1 , according to claim 1 , comprising from 0.1 to 2000 mg of the compound Wogonin (W) and at least one pharmaceutically acceptable excipient.6. A pharmaceutical composition according to claim 5 , comprising as compound of formula (I) the drug compound Wogonin (W) and as second drug compound at least one from the following group: ACE inhibitors claim 5 , beta blockers claim 5 , anti-hypertensives claim 5 , cardiotonics claim 5 , anti-thrombotics claim 5 , vasodilators claim 5 , hormone antagonists claim 5 , ionotropes claim 5 , diuretics claim 5 , endothelin antagonists claim 5 , calcium channel blockers claim 5 , phosphordiesterase inhibitors claim 5 , angiotensin type II antagonists and cytokine inhibitors.7. A pharmaceutical composition according to claim 5 , comprising as compound of formula (I) the drug compound Wogonin (W) and as second drug compound an ACE inhibitor from the group ramipril claim 5 , alacepril claim 5 , enalapril claim 5 , captopril claim 5 , cilazapril claim 5 , delapril claim 5 , enalaprilat claim 5 , fosinopril claim 5 , ...

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Номер записи: 79
29-08-2013 дата публикации

Process for the preparation of lubiprostone

Номер: US20130225842A1
Автор: Julian Paul Henschke, Lizhen Xia, Yuanlian Liu, Yung-Fa Chen
Принадлежит: Individual

Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

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Номер записи: 80
05-09-2013 дата публикации

ALDH-2 INHIBITORS IN THE TREATMENT OF ADDICTION

Номер: US20130231325A1
Автор: Graupe Michael, Venkataramani Chandrasekar, Zablocki Jeff
Принадлежит: Gilead Sciences. Inc.

Disclosed are novel isoflavone derivatives having the structure of Formula I: 2. The compound of claim 1 , wherein Ris optionally substituted alkyl and Ris optionally substituted alkyl or optionally substituted cycloalkyl.3. The compound of claim 2 , wherein Ris alkyl of 1-6 carbon atoms optionally substituted by halo claim 2 , hydroxyl claim 2 , cyano claim 2 , optionally substituted alkoxy of 1-6 carbon atoms claim 2 , optionally substituted acyl claim 2 , optionally substituted amino claim 2 , optionally substituted carboxylalkyl claim 2 , optionally substituted carboxylcycloalkyl claim 2 , or optionally substituted alkoxycarbonylamino.4. The compound of claim 3 , wherein X claim 3 , Y and Z are —CR— and Ris hydrogen claim 3 ,{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'The compound of , selected from the group consisting ofN-(4-(7-(3-methoxyprop-1-ynyl)-4-oxo-4H-chromen-3-yl)phenyl)methanesulfonamide;N-(4-(7-(3-hydroxy-3-methylbut-1-ynyl)-4-oxo-4H-chromen-3-yl)phenyl)methanesulfonamide; andN-(4-(7-(3-methoxyprop-1-ynyl)-4-oxo-4H-chromen-3-yl)phenyl)cyclopropane-sulfonamide.5. The compound of claim 1 , wherein Ris optionally substituted cycloalkyl and Ris optionally substituted alkyl or optionally substituted cycloalkyl.6. The compound of claim 5 , wherein Ris cycloalkyl optionally substituted by halo claim 5 , hydroxyl claim 5 , cyano claim 5 , alkoxy claim 5 , optionally substituted acyl claim 5 , optionally substituted amino claim 5 , optionally substituted carboxylalkyl claim 5 , optionally substituted carboxylcycloalkyl claim 5 , or optionally substituted alkoxycarbonylamino.7. A compound of claim 6 , wherein X claim 6 , Y and Z are —CR— and Ris hydrogen claim 6 ,8. A compound of claim 1 , selected from the group consisting of:N-(4-(7-(cyclopropylethynyl)-4-oxo-4H-chromen-3-yl)phenyl)methanesulfonamide;N-(4-(7-(((1S,2R)-2-hydroxycyclopentyl)ethynyl)-4-oxo-4H-chromen-3-yl)phenyl)methanesulfonamide;N-(4-(7-((1-hydroxycyclopentyl)ethynyl)-4-oxo-4H-chromen ...

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Номер записи: 81
05-09-2013 дата публикации

FLAVONE DERIVATIVES AND THEIR PREPARATIVE METHOD AND MEDICAL USE

Номер: US20130231492A1
Автор: Chen Ying, Duan Hongquan, Jin Meina, Niu Wenyan, Qin Nan, Shi Lihuan
Принадлежит:

Flavone derivatives, preparative method of the derivatives and use thereof as medicaments for treating diabetes. The structure of the derivatives is presented by formula 1: In the structure, Rand R, which are identical or not, represent hydrogen atom, halogen, cyano, hydroxyl, trifluoromethyl, thio-methyl, benzyloxy, C1-C8 linear chain or branch chain alkyl, C1-C8 linear chain or branch chain alkoxy. The pharmacological test indicates that the flavone derivatives can significantly increase the glucose consumption of Hep-G2 cell with insulin resistance activity, promote translocation of glucose transporter 4 of skeletal muscle cells (L6GLUT4myc) at different level, and significantly increase glucose intake and utilization by cells. The test proves the fact for the first time that the flavone derivatives can significantly promote translocation of glucose transporter 4 of skeletal muscle cells, and one of the mechanisms for treating diabetes is activating the cell AMPK phosphorylation and phosphorylating the downstream ACC. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , therein R2 is hydrogen claim 1 , hydroxyl or Calkoxy in a linear or branched chain.3. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , therein R2 is hydrogen.5. A compound according to claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , therein I-3 claim 4 , I-4 claim 4 , I-6 claim 4 , I-9 claim 4 , I-10 claim 4 , and I-12 are selected.6. A compound according to claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , therein I-12 is selected.8. The preparation according to characterized as follows:{'sub': '4', '(1) To a solution of substituted benzaldehydes in acetone at room temperature was slowly added a solution of the 4N NaOH aqueous solution. The mixture was stirred at 25-40° C. in 15 min-12 h. After completion of the reaction, excess acetone was removed under reduced pressure. Adjusting ...

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Номер записи: 82
12-09-2013 дата публикации

COMPOUNDS AND MIXTURES FOR INFLUENCING INFLAMMATORY STATES

Номер: US20130236472A1
Автор: Blings Maria, Götz Marcus, Ley Jakob, Reichelt Katharina
Принадлежит: SYMRISE AG

The invention relates to certain compounds, salts of these compounds and mixtures containing or consisting of two or more such compounds, two or more such salts or one or more such compounds and one or more such salts, each for use in a method for the prophylaxis and/or treatment of inflammation, in particular of inflammation of the skin. 115-. (canceled)19. The mixture of claim 16 , containing or consisting of two or more different compounds of the formula (X) claim 16 , preferably of two claim 16 , three claim 16 , four claim 16 , five claim 16 , six claim 16 , seven claim 16 , eight claim 16 , nine or ten different compounds of the formula (X).20. The mixture of claim 18 , containing or consisting of two or more different compounds of the formula (X) selected from the group consisting of the compounds (1) to (10).22. The mixture of claim 21 , wherein the following applies: Q2 claim 21 , Q4 claim 21 , Q5 claim 21 , Q8 and Q9 represent hydrogen atoms claim 21 , Q1 claim 21 , Q3 and Q6 independently of one another are hydrogen atoms claim 21 , hydroxy or methoxy groups claim 21 , with the proviso that at least one of the residues Q1 and Q3 represents a hydroxy group and Q7 represents a hydroxy group.23. The mixture of claim 21 , containing one claim 21 , several or all compounds of the formula (Y) selected from the group consisting of homoeriodictyol claim 21 , sterubin claim 21 , eriodictyol claim 21 , hesperetin claim 21 , chrysoeriol and luteolin claim 21 , preferably comprising homoeriodictyol.24. The mixture of claim 21 , wherein the proportion of the total quantity of compounds of the formula (X) and salts of compounds of the formula (X) in the mixture claim 21 , based on the total weight of the mixture claim 21 , is 1 to 99 wt. % claim 21 ,and/orthe proportion of the total quantity of compounds of the formula (Y) and salts of compounds of the formula (Y) in the mixture, based on the total weight of the mixture, is 1 to 99 wt. %.25. The mixture of claim 21 , ...

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Номер записи: 83
19-09-2013 дата публикации

TARGETED PROBES OF CELLULAR PHYSIOLOGY

Номер: US20130244891A1
Автор: Bruchez Marcel P., Chakraborty Subhasish K., Schmidt Brigitte F., Waggoner Alan
Принадлежит: CARNEGIE MELLON UNIVERSITY

Biosensor comprising an activatable acceptor fluorogen linked via a linker to a donor which transfers energy to the fluorogen on detecting an analyte wherein the fluorogen component reacts and a 100 fold increase in intensity results when the fluorogen interacts non-covalently with an activator e.g. fluorogen activator peptide. 1. A biosensor comprising an activatable acceptor fluorogen linked by a linker to an environment-sensitive donor that interacts with an analyte , wherein the activatable acceptor fluorogen produces a fluorescence signal increase of at least 100-fold when it interacts non-covalently with an activator of the activatable acceptor fluorogen as compared to when no activator is present , and wherein the environment-sensitive donor transfers excitation energy to the activatable acceptor fluorogen such that , when activated , the activatable acceptor fluorogen produces a detectable fluorescent signal when the environment-sensitive donor is excited and the environment-sensitive donor transfers different amounts of excitation energy to the activatable acceptor fluorogen when it interacts with the analyte as compared to when no analyte is present.2. The biosensor of wherein the activator is a fluorogen activator peptide (FAP).3. The biosensor of claim 1 , wherein the activatable acceptor fluorogen and the environment-sensitive donor are covalently linked.4. The biosensor of claim 1 , wherein the environment-sensitive donor is attached to the activatable acceptor fluorogen by a molecular linker and the activatable acceptor fluorogen and the environment-sensitive donor are close enough for resonance energy transfer of excited state energy of the sensitive donor to be transferred to the activatable acceptor fluorogen with at least 50% efficiency.5. The biosensor of claim 1 , wherein the environment-sensitive donor detects an ion binding event leading to a change in the fluorescence intensity of the activatable acceptor fluorogen when it is bound to its ...

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Номер записи: 84
19-09-2013 дата публикации

ENANTIOSELECTIVE ORGANIC ANHYDRIDE REACTIONS

Номер: US20130245268A1
Автор: Connon Stephen J., Cornaggia Claudio, Manoni Francesco, Tallon Sean, Torrente Esther
Принадлежит: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD

Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C-Corganic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones. 1. An enantioselective synthetic method comprising the step of:{'sub': 4', '50, 'reacting an enolisable C-Corganic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst.'}4. A method according to claim 1 , wherein the enolisable C-Corganic anhydride is a cyclic anhydride.14. A compound according to claim 10 , wherein the compound is immobilised on a solid phase support or a magnetic nanoparticle. The present invention relates to asymmetric synthesis, and in particular the field of asymmetric catalysis. Disclosed herein are a number of novel catalysts for promoting highly useful synthetic transformations between organic anhydrides and aldehydes, ketones, and α,β-unsaturated electrophiles. The transformations of the present invention allow access to densely functionalised products in high enantiomeric excess.Privileged structures are molecular frameworks exhibited in natural products and medicinal compounds that show therapeutic activity at number of different receptor or enzyme targets. Accordingly, facile enantioselective synthetic routes to such structures are valuable and are in constant demand.Two such privileged structures are Dihydroisocoumarins (A) and Dihydroisoquinolinones (B). The asterisks denote carbon atoms that are chiral. Given the effect the chirality of these stereogenic carbons may have on the activity of these molecules, controlling the absolute stereochemistry of ...

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Номер записи: 85
19-09-2013 дата публикации

ANTI-LEISHMANIAL COMPOUND AND ANTI-LEISHMANIAL DRUG

Номер: US20130245288A1
Автор: Horie Shohei, Kimura Junji, Marushima Harumi, Matsumoto Yoshitsugu, Osada Yasutaka, Sanjoba Chizu
Принадлежит: AOYAMA GAKUIN EDUCATIONAL FOUNDATION

Provided is an anti-leishmanial compound represented by formula (1): 6. An anti-leishmanial drug comprising the anti-leishmanial compound according to or a pharmacologically acceptable salt thereof as an active ingredient.7. An anti-leishmanial drug comprising the anti-leishmanial compound according to or a pharmacologically acceptable salt thereof as an active ingredient.8. An anti-leishmanial drug comprising the anti-leishmanial compound according to or a pharmacologically acceptable salt thereof as an active ingredient.9. An anti-leishmanial drug comprising the anti-leishmanial compound according to or a pharmacologically acceptable salt thereof as an active ingredient.10. An anti-leishmanial drug comprising the anti-leishmanial compound according to or a pharmacologically acceptable salt thereof as an active ingredient. The present invention relates to an anti-leishmanial compound having a high anti-leishmanial activity, and an anti-leishmanial drug.Leishmaniasis is caused by flagellated protozoan parasites of the genus , which are obligate intracellular parasites of phagocytic macrophages. Leishmaniasis has been designated as one of six major tropical diseases by the World Health Organization (WHO). Leishmaniasis is vector-borne disease by the bite of blood-sucking female sandfly vectors, resulting in the parasite inoculation to the skin, viscera or the like of mammalian hosts. The symptoms of Leishmaniasis is fatal in severe ranging from mild to heal, but pentavalent antimony formulations have been used primarily as a treatment known to cause severe adverse side effects. Therefore, there is a demand for a new drug having a low risk of adverse side effects. And Amphotericin B was used originally as an antifungal agent, which is also used to treat leishmaniasis. Furthermore, AmBisome has been developed as a drug suppressing the adverse side effects, but this drug has a problem that the drug is expensive.On the other hand, it has been reported that marine algae- ...

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Номер записи: 86
26-09-2013 дата публикации

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

Номер: US20130251647A1
Автор: BOLLSCHWEILER Claus, PELZER Ralf, SIEGEL Wolfgang, Subkowski Thomas, WITTENBERG Jens
Принадлежит: BASF SE

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators. 123.-. (canceled)27. The method according to claim 27 , where claim 27 , in the compound of the formula (II) claim 27 , X is not a methylene or linear 1 claim 27 ,4-butylene bridge.28. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , R claim 27 , Rand Rare H and{'sub': 22', '23, 'Rand R, together with the carbon atoms to which they are bonded, form a methylenedioxy group.'}29. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , the radicals Rand R claim 27 , independently of one another claim 27 , are an in each case mononuclear aryl or heteroaryl radical or a C-C-cycloalkyl radical.31. The method according to claim 25 , where the receptor is brought into contact with at least one compound which claim 25 , in a cellular activity test using cells which recombinantly express the human TRPM8 receptor claim 25 , modulates the permeability of these cells for Ca ions.32. The method according to claim 25 , where the modulating compound has an agonistic or antagonistic effect on the cellular Ca ion permeability.33. The method according to claim 25 , where the modulating compound is a TRPM8 receptor agonist.34. The use of a compound according to the definition in for inducing a sensation of coldness in humans and/or animals claim 25 , in particular for non-therapeutic purposes.35. The use of a compound according to the definition in as active constituent of a pharmaceutical composition.36. The use of a compound according to the definition in for the treatment of prostate carcinomas claim 25 , for the treatment of bladder weakness or in pain therapy.37. The use of a compound ...

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Номер записи: 87
26-09-2013 дата публикации

Compounds and Mixtures Influencing Inflammatory States

Номер: US20130251730A1
Автор: Blings Maria, Götz Marcus, Ley Jakob, Reichelt Katharina, SOMOZA Veronika, Walker Jessica, Walker Joel Michael
Принадлежит: SYMRISE AG

Suggested is a compound of the formula (X) 130-. (canceled)34. The mixture of claim 31 , containing or consisting of two or more different compounds of the formula (X) claim 31 , preferably of two claim 31 , three claim 31 , four claim 31 , five claim 31 , six claim 31 , seven claim 31 , eight claim 31 , nine or ten different compounds of the formula (X).35. The mixture of claim 33 , containing or consisting of two or more different compounds of the formula (X) selected from the group consisting of the compounds (1) to (10).37. The mixture of claim 36 , wherein the following applies: Q2 claim 36 , Q4 claim 36 , Q5 claim 36 , Q8 and Q9 represent hydrogen atoms claim 36 , Q1 claim 36 , Q3 and Q6 independently of one another are hydrogen atoms claim 36 , hydroxy or methoxy groups claim 36 , with the proviso that at least one of the residues Q1 and Q3 represents a hydroxy group and Q7 represents a hydroxy group.38. The mixture of claim 36 , containing one claim 36 , several or all compounds of the formula (Y) selected from the group consisting of homoeriodictyol claim 36 , sterubin claim 36 , eriodictyol claim 36 , hesperetin claim 36 , chrysoeriol and luteolin claim 36 , preferably comprising homoeriodictyol.40. The mixture of claim 36 , wherein the proportion of the total quantity of compounds of the formula (X) claim 36 , compounds of the formula (Y) claim 36 , salts of compounds of the formula (X) and salts of compounds of the formula (Y) in the mixture claim 36 , based on the total weight of the mixture claim 36 , is 0.0001 to 100 wt. %.41. The mixture of claim 36 , wherein the mixture comprises a plant extract or consists thereof claim 36 , and the proportion of the total quantity of compounds of the formula (X) and salts of compounds of the formula (X) in the mixture claim 36 , based on the total weight of the mixture claim 36 , is preferably 0.1 to 100 wt. %.42Eriodictyon. The mixture of claim 36 , wherein the plant extract is an extract from ssp.43. The mixture ...

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Номер записи: 88
10-10-2013 дата публикации

TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20130267538A1
Автор: BODDUPALLI Sekhar, Miller Guy M., Walkinshaw Gail, WANG Bing
Принадлежит:

The invention relates the method of treatment or amelioration of mitochondrial disorders such as Alzheimer's disease, Parkinson's disease, Friedreich's ataxia (FRDA), cerebellar ataxias, Leber's hereditary optic neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), Myoclonic Epilepsy with Ragged Red Fibers (MERFF), amyotrophic lateral sclerosis (ALS), motor neuron diseases, Huntington's disease, macular degeneration, and epilepsy, with chroman derivatives of Formula I or Formula II as described herein. 2. The method of claim 1 , comprising administering to said subject a therapeutically effective amount of a compound of Formula I.3. The method of claim 2 , comprising administering the compound of Formula I wherein Ris hydrogen claim 2 , Calkyl claim 2 , or Calkenyl.4. The method of claim 2 , comprising administering the compound of Formula I wherein Rand Rare independently of each other Calkyl or halogen.5. The method of claim 4 , comprising administering the compound of Formula I wherein Ris Calkyl and Ris Calkyl.6. The method of claim 2 , comprising administering the compound of Formula I wherein Ris Calkyl claim 2 , and Ris Calkyl or Calkenyl.7. The method of claim 2 , comprising administering the compound of Formula I wherein Rand Rtaken together with the carbon to which they are attached form a 5-6 membered carbocyclic ring claim 2 , optionally substituted with Calkyl claim 2 , Calkoxy claim 2 , hydroxy claim 2 , carboxy claim 2 , carboxyalkyl claim 2 , alkoxycarbonyl claim 2 , alkoxycarbonylalkyl claim 2 , aminocarbonyl claim 2 , aminocarbonylalkyl claim 2 , or hydroxyalkyl.8. The method of claim 1 , comprising administering to said subject a therapeutically effective amount of a compound of Formula II.9. The method of claim 8 , comprising administering the compound of Formula II claim 8 , wherein Ris —COOH claim 8 , or —COORand Ris Calkyl.11. The method of claim 1 , comprising administering a therapeutically effective amount ...

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Номер записи: 89
10-10-2013 дата публикации

Compound

Номер: US20130267586A1
Автор: Cook Graeme James, Hartley Richard Charles, McPhail Donald Barton
Принадлежит: ANTOXIS LIMITED

The present invention provides compounds of the formula Formula I or a salt thereof: and the uses of such compounds for the treatment of a disease or disorder involving oxidative damage, for preventing UV damage to the skin of a mammal and for preventing or reversing the effects of ageing, or for treating or preventing dry skin. 2. A compound as claimed in claim 1 , wherein:{'sub': '20', 'Rrepresents H or a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D);'}{'sub': '21', 'claim-text': i) represents H;', {'sub': '22', 'sup': 1', '2, 'ii) together with Rprovides a second bond between Cand C; or'}, {'sub': 1', '1', '1-6', '21', '1, 'sup': '1', 'iii) when X is —NR— and Ris not H or Calkyl, Rtogether with Rprovides a second bond between Cand N;'}], 'R{'sub': '22', 'claim-text': i) represents H;', {'sub': '23', 'ii) together with Rforms ═O; or'}, {'sub': '21', 'sup': 1', '2, 'iii) together with Rprovides a second bond between Cand C;'}], 'R{'sub': '23', 'claim-text': i) represents H or a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D); or', {'sub': '22', 'ii) together with Rforms ═O;'}, {'sub': 20', '23, 'wherein at least one of Rand Ris a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D).'}], 'R3. (canceled)4. (canceled)5. A compound as claimed in claim 1 , wherein:{'sub': 20', '21', '22', '23, 'sup': 1', '2, 'R, R, R, and Rform part of a 5, 6 or 7 membered unsaturated ring including Cand C, which ring (Ring A) is substituted with at least one group;'}said at least one group being a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D); and{'sup': '1', 'wherein the 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D) is at the meta, para or ortho position relative to C.'}6. A compound as claimed in claim 5 , wherein the 3 claim 5 , 4 claim 5 , 5 claim 5 , 6 claim 5 , 7 or 8 membered saturated or unsaturated ring (Ring D) is at the meta position relative to C.7. A compound as claimed in claim ...

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Номер записи: 90
10-10-2013 дата публикации

PROCESS FOR THE PREPARATION OF ATOVAQUONE

Номер: US20130267717A1
Автор: Dwyer Andrew Neil, Gordon Andrew, Urquhart Michael
Принадлежит: Glaxo Group Limited

Disclosed herein is novel process for preparation of atovaquone, which process includes reacting 1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone. 6. A process as claimed in wherein the reaction proceeds in the presence of a nucleophile/base.7. A process as claimed in wherein the nucleophile/base is sodium methoxide (NaOMe).8. A process as claimed in wherein the reaction proceeds in the presence of a catalyst or a base.9. A process as claimed in wherein the catalyst or base is morpholine.10. A process as claimed in wherein the catalyst or base is isobutylamine.11. A process as claimed in wherein the hydrogenating agent is Pd/C and dry activated carbon.15. (canceled) The present invention relates to a new process for the preparation of atovaquone. In particular, the present invention relates to novel intermediates useful in the preparation of atovaquone.Atovaquone, 2-[trans-4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone (compound of formula (I))is a useful medicine for the treatment and prophylaxis of infections. Atovaquone is potently active (in animals and in vitro) against , and tachyzoite and cyst forms of . Due to its inhibitory effect in sensitive parasites, atovaquone can act by selectively affecting mitochondrial electron transport and parallel processes such as ATP and pyrimidine biosynthesis.Atovaquone is approved for marketing in the US under the tradename Mepron® as tablets of 250 mg and an oral suspension which is indicated for the treatment and prophylaxis of infection. It is also available in combination with proguanil hydrochloride under the tradename Malarone® for the treatment and prevention of malaria.European Patent No. 123238 discloses 2-substituted-3-hydroxy-1,4-naphthoquinones, including atovaquone, which are said to be active against the human malaria parasite and also against species such as and , which are ...

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Номер записи: 91
17-10-2013 дата публикации

ISOFLAVONOID COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER

Номер: US20130273177A1
Автор: Moreno Ofir
Принадлежит: MARSHALL EDWARDS, INC.

Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies. 2. The composition of claim 1 , wherein Ris hydrogen.3. The composition of claim 1 , wherein Ris methyl.4. The composition of claim 1 , wherein Ris hydrogen.5. The composition of claim 1 , wherein Ris hydrogen.6. (canceled)7. The composition of claim 1 , wherein the cyclodextrin is SBE7-β-CD.8. The composition of claim 7 , wherein the composition comprises about 22 to 37% w/v SBE7-β-CD.9. The composition of claim 1 , wherein the composition further comprises water.10. (canceled)11. The composition of claim 1 , wherein the composition comprises a compound of formula II in an amount of about 35 mg/mL.12. The composition of claim 1 , wherein the composition further comprises a chemotherapeutic agent selected from the group consisting of cisplatin claim 1 , carboplatin claim 1 , paclitaxel claim 1 , gemcitabine or doxorubicin.13. (canceled)15. The method of claim 14 , wherein the composition increases or induces sensitivity of the cancer to a chemotherapeutic agent claim 14 , anti-cancer agent claim 14 , or radiation therapy.16. The method of claim 15 , wherein the cancer had lost sensitivity to a chemotherapeutic agent claim 15 , anti-cancer agent claim 15 , or radiation therapy.17. The method of claim 14 , wherein said cancer is selected from the group consisting of bladder cancer claim 14 , breast cancer claim 14 , colon cancer claim 14 , rectal cancer claim 14 , endometrial cancer claim 14 , kidney cancer claim 14 , leukemia claim 14 , lung cancer claim 14 , melanoma claim 14 , non-Hodgkin lymphoma claim 14 , ovarian cancer claim 14 , pancreatic cancer claim 14 , prostate cancer claim 14 , thyroid cancer claim 14 , and cancers of ...

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Номер записи: 92
17-10-2013 дата публикации

Chromone Inhibitors of S-Nitrosoglutathione Reductase

Номер: US20130274320A1
Автор: Qiu Jian, Sun Xicheng, Wasley Jan
Принадлежит:

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. 2. The method of wherein Ris selected from the group consisting of CF claim 1 , CFH claim 1 , and CFCH; and Ris hydrogen.3. The method of wherein Ris selected from the group consisting of CF claim 1 , methyl claim 1 , isopropyl claim 1 , and isobutyl; and Rand Rare both hydrogen.4. The method of wherein Ris selected from the group consisting of CF claim 1 , methyl claim 1 , isopropyl claim 1 , isobutyl claim 1 , CFH claim 1 , CFCH claim 1 , and CFCHCH; and Rand Rare both hydrogen.5. The method of wherein the compound of Formula (I) or pharmaceutically salt thereof is selected from the group consisting of 4-(2-(difluoromethyl)-7-hydroxy-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-2-(methoxymethyl)-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-2-isopropyl-4-oxo-4H-chromen-3-yl)benzoic acid;4-(2-cyclopentyl-7-hydroxy-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-2-methyl-4-oxo-4H-chromen-3-yl)benzoic acid;4-(2-benzyl-7-hydroxy-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-4-oxo-2-(thiophen-2-yl)-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-4-oxo-2-(thiophen-3-yl)-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-2-isobutyl-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-2-(methylthio)-4-oxo-4H-chromen-3-yl)benzoic acid;4-(6-chloro-7-hydroxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;4-(6-fluoro-7-hydroxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;2-fluoro-4-(7-hydroxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;3-chloro-4-(7-hydroxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;4-(2-(1,1-difluoroethyl)-7-hydroxy-4-oxo-4H-chromen-3-yl)benzoic acid;4-(7-hydroxy-6-methoxy-4-oxo-2-(trifluoromethyl)-4H-chromen-3-yl)benzoic acid;2-chloro-4-(7-hydroxy-4-oxo-2-(trifluoromethyl ...

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Номер записи: 93
17-10-2013 дата публикации

Process for the Synthesis of 4,5,6,7-tetrachloro-3',6'-dihydroxy-2',4',5',7'-tetraiodo-3H-spiro[isobenzofuran-1,9'-xanthen]-3-one(Rose Bengal) and Related Xanthenes

Номер: US20130274322A1
Автор: Babiak Kevin, Lutz Marlon, Scott Timothy, Singer Jamie, Wachter Eric A.
Принадлежит:

A new process for the manufacture of iodinated xanthenes in high purity includes a cyclization step followed by an iodination step. No extraction, chromatographic or solvent concentration steps are required, and the intermediate as well as final compounds are isolated via filtration or similar means. The process requires a single organic solvent, and the steps are completed at temperatures below 100° C. The exclusion of chloride ions, of chloride free-radicals, hypochlorite ions, or hypochlorous acid as reagents or from reagents that may generate these species in situ in the presence of oxidants, prevents undesirable impurity formation. Several new compounds have been conceived and isolated using these methods. These new compounds are also formed into new medicaments. 168-. (canceled)71. The medicament of wherein said compound of Formula 4 comprises about 0.001% to less than about 20% by weight.72. The medicament of wherein said compound of Formula 4 comprises a compound selected from a group consisting of:4,4′,5,6,7-pentachloro-3′,6′-dihydroxy-2′,5′,7′-triiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;2′,4,5,6,7-pentachloro-3′,6′-dihydroxy-4′,5′,7-triiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,4′,5,5′,6,7-hexachloro-3′,6′-dihydroxy-2′,7′-diiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;2′,4,5,6,7,7′-hexachloro-3′,6′-dihydroxy-4′,5′-diiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;2′,4,5,5′,6,7-hexachloro-3′,6′-dihydroxy-4′,7′-diiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,5,6,7-tetrabromo-2′-chloro-3′,6′-dihydroxy-4′,5′,7′-triiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,5,6,7-tetrabromo-4′-chloro-3′,6′-dihydroxy-2′,5′,7′-triiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,5,6,7-tetrabromo-2′,5′-dichloro-3′,6′-dihydroxy-4′,7′-diiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,5,6,7-tetrabromo-4′,5′-dichloro-3′,6′-dihydroxy-2′,7′-diiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one;4,5,6,7-tetrabromo-2′,7′-dichloro-3′,6′-dihydroxy-4′,5′-diiodo-3H- ...

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Номер записи: 94
17-10-2013 дата публикации

Method of inhibiting abcg2 and other treatment methods

Номер: US20130274323A1
Автор: Curtis J. Henrich, Heidi R. Bokesch, James B. Mcmahon, Kentaro Takada, Kirk R. Gustafson, Laura K. Cartner, Michael C. Dean, Richard W. Fuller, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Susan E. Bates
Принадлежит: US Department of Health and Human Services

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R 1 , R 2 , R 3 , X 1 , X 2 , X 3 , a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.

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Номер записи: 95
17-10-2013 дата публикации

PROCESS FOR THE PREPARATION OF NEBIVOLOL

Номер: US20130274486A1
Автор: BARTOLI Sandra, Cipollone Amalia, Fattori Daniela
Принадлежит:

The present invention relates to a novel process for the synthesis of Nebivolol product represented in Scheme (1), comprised of a reduced number of high-yield steps, and characterized by the kinetic resolution of the two epoxide pairs diastereoisomeric therebetween (mixture 1), allowing to avoid complex chromatographic separations. 2. A process according to claim 1 , wherein R and Rare each a benzyl group.3. A process according to claim 2 , wherein the amines 2 and 3 are separated from the epoxides 4 and 5 by precipitation and filtration.4. A process according to claim 2 , wherein the sterically hindered alcohol claim 2 , defined at point a1 claim 2 , is selected from the group consisting of 2-methyl-2-butanol claim 2 , tert-BuOH claim 2 , and 2-methyl-2-pentanol.5. A process according to claim 2 , wherein the apolar solvent claim 2 , defined at point a1 claim 2 , is cyclohexane.6. A process according to claim 2 , wherein the solvents for the fractional crystallization defined at point c are 2-methyl-2-butanol and subsequently an ethyl acetate/cyclohexane mixture.7. A process according to claim 2 , wherein the deprotecting envisaged at point d is performed by catalytic hydrogenation with Pd(OH). The present invention relates to a novel process for the synthesis of Nebivolol. Nebivolol is a racemic mixture of the two enantiomers [2S[2R[R[R]]]] α,α′-[imino-bis(methylene)]bis[6-fluoro-chroman-2-methanol] and [2R[2S[S[S]]]] α,α′-[imino-bis(methylene)]bis[6-fluoro-chroman-2-methanol] (Scheme 2).In particular, it is reported the kinetic resolution of the two diastereoisomeric pairs of RS/SR and SS/RR epoxides (scheme 1, mixture 1) by treatment with an amine in a suitable solvent.Nebivolol is known as an adrenergic beta-receptor antagonist, an antihypertensive agent, a platelet aggregation inhibitor and a vasodilating agent.Nebivolol has basic properties and may be converted into an acceptable pharmaceutical salt form by treatment with an acid. The hydrochloride salt is ...

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Номер записи: 96
17-10-2013 дата публикации

METHOD FOR OBTAINING PHYTOSTEROLS AND/OR TOCOPHEROLS FROM RESIDUE OF A DISTILLATION OF THE ESTERS OF VEGETABLE OILS, PREFERABLY FROM DISTILLATION RESIDUE FROM A TRANSESTERIFICATION OF VEGETABLE OILS

Номер: US20130274489A1
Автор: Baade Nico, Lemp Joachim, Pöhls Emanuel
Принадлежит: VERBIO VEREINIGTE BIOENERGIE AG

The invention relates to a method for obtaining and purifying phytosterols and/or tocopherols from distillation residue from a transesterification of vegetable oils, in particular from the vegetable oil-based fatty acid methyl ester production for the field of use of biodiesel (FAME), comprising a first transesterification stage for converting partial glycerides contained in the distillation residue; separating the glycerin phase from a reaction mixture resulting from the first transesterification stage; a second transesterification stage for converting sterol esters contained in the reaction mixture; adding water to the reaction mixture after the second transesterification stage in order to generate a multiphase system; simultaneously or sequentially separating the phases of the multiphase system into a substantially sterol-containing phase; a substantially glycerin- and methanol-containing aqueous phase; and a tocopherol-containing methyl ester phase; and obtaining phytosterols from the sterol-containing phase; and optionally obtaining tocopherols from the tocopherol-containing methyl ester phase. The invention further relates to a method for purifying a phytosterol phase and/or phytosterols. 1. A method of obtaining phytosterols and/or tocopherols from residues of a distillation of the esters of vegetable oils , preferably from distillation residues from a transesterification of vegetable oils , in particular from the vegetable oil-based fatty acid methyl ester production for the biodiesel (FAME) field of use , wherein the method comprises a two-stage basic transesterification with an interposed separation off of the glycerin phase , wherein in particularin a first basic transesterification stage an at least far-reaching reaction of partial glycerides contained in the distillation residues is carried out;glycerin phase is separated off from a reaction mixture directly resulting from the first basic transesterification stage without any further method step; andin ...

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Номер записи: 97
24-10-2013 дата публикации

METHOD FOR DEPIGMENTING KERATIN MATERIALS USING RESORCINOL DERIVATIVES

Номер: US20130281507A1
Автор: Marat Xavier
Принадлежит: L'OREAL

The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compounds 2. The compound according to claim 1 , wherein:A is a radical selected from the group consisting of:H;{'sub': 3', '8', '3', '16', '2', '16', '1', '16, 'claim-text': —OH,', {'sub': 1', '4, 'a C-Calkoxy group,'}, {'sub': '6', '—COOR,'}, {'sub': 6', '7, '—CONRR;'}, {'sub': 1', '4, 'a phenyl group which is optionally substituted by one or more hydroxyls or one or more C-Calkoxy radicals, and'}, 'a saturated or an unsaturated heterocycle comprising from 5 to 8 members and one or more heteroatoms selected from the group consisting of O, N and S, wherein one of the 5 to 8 members is optionally a carbonyl group;, 'a C-Ccyclic, a C-Cbranched, a C-Cunsaturated, or a C-Clinear saturated alkyl group, which is optionally interrupted by one or more heteroatoms or moieties selected from the group consisting of N, O, —CO— and —NHC(O)— and is optionally substituted by one or more groups independently selected from the group consisting of{'sub': 5', '12', '1', '4', '1', '4, 'a C-Caryl group, which is optionally substituted by one or more radicals independently selected from the group consisting of OH, a C-Calkoxy group, and a C-Calkyl group;'}{'sub': 2', '3, '—NRR;'}{'sub': '4', '—OR;'}{'sub': '4', '—C(O)NHR;'}anda radical of formula (II),wherein{'sub': 2', '3, 'claim-text': H,', {'sub': 3', '8', '2', '8', '3', '8', '1', '8', '1', '4, 'a C-Ccyclic, a C-Cunsaturated, a C-Cbranched, or a C-Clinear saturated alkyl group, which is optionally interrupted by an oxygen atom and optionally substituted by a hydroxyl group or a C-Calkoxy group, and'}, {'sub': 5', '12', '1', '4, 'a C-Caryl group which is optionally substituted by one or more hydroxyls and one or more C-Calkoxy radicals;'}], 'Rand Reach are independently selected from the group consisting of{'sub': 2', '3', ...

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Номер записи: 98
24-10-2013 дата публикации

ARYL HYDROCARBON RECEPTOR (AhR) MODIFIERS AS NOVEL CANCER THERAPEUTICS

Номер: US20130281525A1
Автор: GIGUERE Joshua Robert, Haigh Molina Sarah, Pollastri Michael, Schaus Scott, Schlezinger Jennifer, Sherr David H.
Принадлежит:

Provided herein are novel agents that modulate AhR activity for use in therapeutic compositions and methods thereof for inhibiting cancer cell proliferation and tumor cell invasion and metastasis. The agents comprise AhR inhibitors or non-constitutive AhR agonists of Formula (I) and (II) for the inhibition of cancer cell growth and parameters that characterize tumor metastasis, such as tumor cell invasiveness. 152-. (canceled)56. The pharmaceutical composition of claim 53 , wherein the C at position 2 is in the S configuration and the C at position 3 is in the R configuration or wherein the C at position 2 is in the R configuration and the C at position 3 is in the R configuration or wherein the C at position 2 is in the S configuration and the C at position 3 is in the S configuration.57. The pharmaceutical composition of claim 54 , wherein in Formula (IIa):X′ is alkyl, alkoxy, aminosulfonyl;n is 0 or 1;{'sub': '2', 'Ris aryl, substituted aryl, heteroaryl, or substituted aryl; and'}{'sub': 3', '4', '5', '6, 'R, R, Rand Rare independently H, alkoxy, alkyl, or halo.'}58. A method of modulating constitutive AhR activity in a subject in need thereof claim 53 , the method comprising administering to a subject having constitutive AhR activity a therapeutically effective amount of the pharmaceutical composition of .59. A method of treating a cancer claim 53 , a cancerous condition claim 53 , or tumor by modulating AhR activity claim 53 , the method comprising administering to a subject having a cancer or cancerous condition a therapeutically effective amount the pharmaceutical composition of .60. The method of claim 59 , wherein the subject having a cancer claim 59 , cancerous condition claim 59 , or tumor has an invasive tumor.61. The method of claim 59 , further comprising the step of selecting the subject having a cancer claim 59 , a cancerous condition claim 59 , or a tumor.62. The method of claim 59 , wherein the cancer is a breast cancer claim 59 , squamous cell ...

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Номер записи: 99
24-10-2013 дата публикации

METHOD FOR PRODUCING DIHYDROQUERCETIN

Номер: US20130281717A1
Автор: Lashin Sergej Alekseevich, Ostronkov Vladimir Sergeevich
Принадлежит:

The invention relates to the chemical and pharmaceutical industry. The essence of the invention consists in that the bark is removed from Siberian or Dahurian larch wood, the wood is chopped and dried at 40-50° C. to a residual humidity of 15-25 percent. The dried wood is ground, and the soluble substances are extracted from the sawdust using a 75 percent aqueous solution of ethyl alcohol at a temperature of 40-50° C. with a ratio of raw material to extraction agent of 1:(6-7). The extraction agent is then distilled off, and the aqueous portion of the extract is cooled to 38-42° C. over a period of 20-30 minutes for the removal (sedimentation) of the heavy resinous impurities accompanying the DHQ. The resin-free aqueous DHQ extract is fed into a chromatographic column filled with the hydrophobic polyvinyl benzene-based sorbent LPS 500. The desired product is eluted with a 32-40 percent solution of ethyl alcohol. The eluate is collected in a single portion or is divided into two or three fractions, depending upon the required purity of the product obtained (DHQ). Each fraction is evaporated until the ethyl alcohol is completely removed, and the residue is crystallized from deionized water. The desired product is obtained with a purity level of 95.5-99.5 percent and a yield of 1.5-2.5 percent of the mass of absolutely dry wood. The technical effect includes simplifying the method, increasing its ecological compatibility and reducing its duration, while increasing the purity of the product obtained to 99.5 percent. 1. Method for producing dihydroquercetin , comprising extraction of dried and ground larch wood with an aqueous solution of ethyl alcohol with heating , distillation of the ethyl alcohol , and cooling of the aqueous portion of the extract for the removal of oil and resin , characterized in that the extraction of the ground larch wood is effected at a ratio of raw material to extraction agent of 1:(6-7) , wherein the aqueous portion of the dihydroquercetin ...

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Номер записи: 100