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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 8265. Отображено 100.
01-03-2012 дата публикации

Method for Producing Oxygen-Containing Compound

Номер: US20120053354A1
Автор: Masaaki Yoshida
Принадлежит: UTSUNOMIYA UNIVERSITY

[Problem] There is provided a method for producing an oxygen-containing compound safely and with improved reaction efficiency, in which an undesired peroxide is unlikely to be produced, and efficient heat exchange of the ozonization can be achieved. [Mean for solving the Problem] The method comprises an ozonization reaction step of continuously supplying, together with an organic compound, ozone having an oxygen content of less than 10% in a dissolved state in high-pressure carbon dioxide to an ozonization reaction section having a thin tubular shape, and reacting the ozone and the organic compound under conditions that suppress generation of oxygen due to thermal decomposition of the ozone, thereby continuously producing an ozonide; and a decomposition reaction step of continuously supplying the ozonide produced in the ozonization reaction step to a decomposition reaction section having a thin tubular shape, thereby continuously producing an oxygen-containing compound, the decomposition reaction step being provided in a manner continuous with the ozonization reaction step.

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Номер записи: 1
26-04-2012 дата публикации

Method for screening inhibitor for inhibiting interaction between beta-amyloid peptide and vegf and inhibitor searched by the same

Номер: US20120101284A1
Автор: Chan-Won Park, In-Cheol Kang
Принадлежит: Innopharmascreen Inc

There is provided a compound found by screening a material for inhibiting a binding between a beta-amyloid 1-42 peptide and VEGF165, in which the inhibition material screened according to the present invention can improve effectiveness as a material for treating Alzheimer's disease.

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Номер записи: 2
10-05-2012 дата публикации

Method for preparing diahydrohexitol diester compositions

Номер: US20120116101A1
Автор: Herve Wyart, Patrick Fuertes
Принадлежит: Roquette Freres SA

A dianhydrohexitol diester composition is obtained by esterifying a dianhydrohexitol composition with a carboxylic acid in the presence of an acid catalyst and hypophosphorous acid. Preferably, the hypophosphorous acid is introduced in an amount between 0.05 and 2 wt. percent of dianhydrohexitol, and in a hypophosphorous acid/acid catalyst weight ratio of less than 1/1. Dianhydrohexitol diester compositions, for example isosorbide diesters, isomannide and/or isoidide rich in diester(s), and having a low yellow index (YI), are useful in numerous industrial applications, in particular in plastic compositions.

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Номер записи: 3
07-06-2012 дата публикации

Synthesis of ttx intermediates

Номер: US20120142911A1
Автор: David Herrero, Luis Miguel Lozano Gordillo, Nuria Tabares Cantero, Pedro Noheda Marín, Raul Benito Arenas
Принадлежит: Consejo Superior de Investigaciones Cientificas CSIC

The present invention relates to the synthesis of intermediates which are useful in TTX synthesis and to the preparation thereof.

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Номер записи: 4
14-06-2012 дата публикации

Electroactive materials

Номер: US20120146013A1
Автор: Hong Meng
Принадлежит: EI Du Pont de Nemours and Co

There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO 2 , or SiR 3 ; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R 1 through R 8 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO 3 R 2 , —OPO 3 R 2 , or CN.

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Номер записи: 5
16-08-2012 дата публикации

Semiconducting composition

Номер: US20120205628A1
Автор: Anthony James Wigglesworth, Nan-Xing Hu, Ping Liu, Yiliang Wu
Принадлежит: Xerox Corp

A compound of Formula (I): wherein X, A, Y, Z, R 1 , R 2 , Ar, n and m are as described herein. The compound of Formula (I) is useful as part of a semiconducting composition to be deposited upon a surface. When heated, the compound of Formula (I) is converted to a crystalline semiconductor with high mobility.

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Номер записи: 6
01-11-2012 дата публикации

Polycyclic ring-fused compound and organic thin film transistor utilizing same

Номер: US20120273770A1
Автор: Hiroaki Nakamura, Hirofumi Kondo, Masahiro Kawamura, Masatoshi Saito, Misa Sunagawa, Naoki Kurihara
Принадлежит: Idemitsu Kosan Co Ltd

A compound for an organic thin film transistor represented by the following formula (1):

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Номер записи: 7
01-11-2012 дата публикации

Epothilone compound formulations

Номер: US20120277274A1
Автор: Aparna MULUPURU, Chandrasekhar Kocherlakota, NAGARAJU Banda, Prasad Vure, Tarun Singh
Принадлежит: Dr Reddys Laboratories Inc, Dr Reddys Laboratories Ltd

The present application relates to compositions for parenteral administration of epothilone compounds, such as ixabepilone.

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Номер записи: 8
13-12-2012 дата публикации

Synthesis of epothilones, intermediates thereto and analogues thereof

Номер: US20120316348A1
Автор: Alexey Rivkin, Ana E. Gabarda, Huajin Dong, Samuel J. Danishefsky, Ting-Chao Chou, Yoshimura Fumikiko
Принадлежит: SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

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Номер записи: 9
20-12-2012 дата публикации

Electroactive materials

Номер: US20120319571A1
Автор: Hong Meng
Принадлежит: EI Du Pont de Nemours and Co

There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO 2 , or SiR 3 ; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R 1 through R 8 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO 3 R 2 , —OPO 3 R 2 , or CN.

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Номер записи: 10
20-12-2012 дата публикации

(2's)-columbianetin isolated from corydalis heterocarpa and composition containing the same

Номер: US20120323022A1
Автор: Byul Nim Ahn, Chang Suk Kong, Jung Ae Kim, Se Kwon Kim, Young Wan Seo
Принадлежит: lndustry University Cooperation Foundation of Pukyong National University

The present invention relates to a compound of (2′S)-columbianetin having photo-protective effect isolated from Corydalis heterocarpa and a cosmetic composition containing the same, which has great effects on prevention and treatment in UVB-induced skin damage.

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Номер записи: 11
14-03-2013 дата публикации

Compounds Having Semiconducting Properties and Related Compositions and Devices

Номер: US20130062598A1
Автор: Antonio Facchetti, Damien Boudinet, Hakan Usta, Jordan Quinn
Принадлежит: Individual

Disclosed are new compounds having semiconducting properties. Such compounds can be processed in solution-phase at a temperature of less than about 50° C. into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics.

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Номер записи: 12
21-03-2013 дата публикации

PROSTAGLANDIN SYNTHESIS AND INTERMEDIATES FOR USE THEREIN

Номер: US20130072695A1
Автор: ALBERICO Dino, CLAYTON Joshua, GORIN Boris Ivanovich, OUDENES Jan
Принадлежит: Alphora Research Inc.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: 2. Compound A according to wherein R represents a substituted phenyl group.3. Compound A according to wherein R represents p-methoxyphenyl5. Compound B according to wherein R′ represents p-methoxybenzyl. This invention relates to prostaglandin analogs and their synthesis. More particularly, it relates to a novel, simplified synthesis of prostaglandin analogs, and novel chemical compounds useful as intermediates in such synthesis.Prostaglandins (PGs) are organic carboxylic acids, namely cyclopentanes carrying two side chain substituents, typically linear C6-C8 side chains, bonded to adjacent positions on the cyclopentane nucleus. One of the side chains, the α-side chain, carries a terminal carboxylic acid group. Many are natural products found in mammalian organs and tissues (primary PGs), and exhibit a variety of physiological activities. Primary PGs generally have a prostanoic acid skeleton, which forms the basis of the nomenclature:A significant number of synthetic PG analogs have been made and found to have useful pharmacological properties. These may have modified skeletons, and substituted and unsaturated side chains. PGs are characterized by a hydroxyl (or ketone) substituent on the cyclopentane nucleus, position 9.Prostaglandin analogs are difficult to synthesize. Complications arise because of the requirements of the end products to have several functional groups and two side chains of significant size and complexity. Stereospecificity is commonly required, for substituent groups and for bonds in the core. Since the products are intended for pharmaceutical use, the range of industrially acceptable reagents, solvents, catalysts, etc. which can be used in their synthesis is limited to those having pharmaceutical industry acceptability.A common starting material for PG analog ...

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Номер записи: 13
28-03-2013 дата публикации

FUNGICIDAL COMPOUNDS AND METHODS OF THEIR USE

Номер: US20130078272A1
Автор: Villas-Boas Silas Granato
Принадлежит: AUCKLAND UNISERVICES LIMITED

Antifungal compounds, an antifungal compound extracted from , also known as , methods of producing the antifungal compounds, isolates and compositions comprising the antifungal compounds, and methods of using the antifungal compounds. 137-. (canceled)38Epicoccum purpurascens. A biologically pure culture of strain SVB-F1 on deposit at the National Measurement Institute , Australia (NMI) under accession number V10/000331 , deposited 18 Mar. 2010 , or a culture having the identifying characteristics thereof , or a culture extract or isolate obtained therefrom.40. The compound of wherein Ris selected from or is substituted with alkylcarbonylalkyl claim 39 , alkylcarbonyloxyalkyl claim 39 , alkyloxyalkyl claim 39 , alkylsulfonyl claim 39 , alkylsulfinyl claim 39 , alkylthioalkyl claim 39 , hydroxyalkyl claim 39 , mono-or di(alkyl)aminoalkyl claim 39 , or wherein Ris hydrogen claim 39 , hydroxyl claim 39 , or a Cto Calkyl or alkoxy group optionally comprising one or more double bonds claim 39 , and optionally substituted with one or more groups selected from lower alkyl claim 39 , lower alkenyl claim 39 , lower alkoxy claim 39 , hydroxyl and carboxyl claim 39 , or wherein Ris a Cto Calkyl or alkoxy group comprising one or more double bonds claim 39 , and substituted with one or more groups selected from lower alkyl claim 39 , lower alkenyl claim 39 , lower alkoxy claim 39 , hydroxyl and carboxyl.41. The compound of wherein R claim 39 , R claim 39 , R claim 39 , and Rare independently selected from hydrogen claim 39 , alkyl claim 39 , substituted alkyl claim 39 , alkoxy claim 39 , substituted alkoxy claim 39 , halogen claim 39 , methyl claim 39 , methoxy and hydroxyl.44. The compound of wherein R claim 43 , R claim 43 , R claim 43 , and Rare independently selected from hydrogen claim 43 , alkyl claim 43 , substituted alkyl claim 43 , alkoxy claim 43 , substituted alkoxy claim 43 , halogen claim 43 , methyl claim 43 , methoxy and hydroxyl.45. The compound of wherein each ...

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Номер записи: 14
04-04-2013 дата публикации

COMPOSITION FOR THE TREATMENT OF ARTHRITIS CONTAINING A DIBENZO-P-DIOXIN DERIVATIVE AS THE ACTIVE INGREDIENT

Номер: US20130084330A1
Автор: Kim Seoung Ho, Lee Haeng Woo, PARK Yong Ju, Shin Hyeon Cheol
Принадлежит: LIVECHEM, INC.

Disclosed is a composition for treating arthritis containing a dibenzo-p-dioxin derivative as an active ingredient. This dibenzo-p-dioxin derivative is very effective in inhibiting NF-kB and AP-1 activity, alleviates the symptoms of degenerative arthritis and rheumatoid arthritis without irritating the skin or causing side effects, and can continue to exhibit improvement effects for a considerable period of time after discontinuation of treatment. Additionally, when the dibenzo-p-dioxin derivative is contained in liposomes, the composition of the invention exhibits much greater effects on treating arthritis by absorption through skin, and thus is useful for the treatment of degenerative arthritis and rheumatoid arthritis. 2. The method according to claim 1 , wherein each R in Formulas 1 to 10 is independently hydrogen claim 1 , methyl claim 1 , acetyl or oleoyl.3. The method according to claim 1 , wherein each R in Formulas 1 to 10 is independently hydrogen.4. The method according to claim 1 , wherein the total weight of the two or more selected compounds ranges from 0.2 to 2.0 wt % of the total weight of the composition.5. The method according to claim 1 , wherein the total weight of the two or more selected compounds ranges from 0.5 to 1.5 wt % of the total weight of the composition.6. The method according to claim 1 , wherein the composition is provided in a form selected from the group consisting of an ointment claim 1 , a lotion claim 1 , a cream claim 1 , a gel claim 1 , a skin emulsion claim 1 , a skin suspension claim 1 , a patch claim 1 , and a spray.7. The method according to claim 1 , wherein the composition further comprises a liposome carrying the composition.8. The method according to claim 7 , wherein the liposome comprises multi-lamella vesicles.9. The method according to claim 7 , wherein the liposome comprises unilamella vesicles.10. The method according to claim 1 , wherein the composition is applied in a dose of 1-1000 μg/cmper day.11. The method ...

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Номер записи: 15
04-04-2013 дата публикации

Pyripyropene Derivative Having ACAT2 Inhibiting Activity and Stable to Metabolizing Enzymes

Номер: US20130085163A1
Автор: Matsuda Daisuke, Nagamitsu Tohru, Ohshiro Taichi, Ohtawa Masaki, Omura Satoshi, Tomoda Hiroshi
Принадлежит: SCHOOL JURIDICAL PERSON KITASATO INSTITUTE

A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: 5. An ACAT2 inhibitor comprising as an active ingredient a compound as set forth in or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or hydrate thereof.6. A pharmaceutical composition for ACAT2 inhibition comprising a compound as set forth in or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or hydrate thereof in an effective amount for inhibition of ACAT2 in a patient and a pharmaceutically acceptable carrier.7. A method for prevention or treatment of a disease associated with ACAT2 in a patient comprising administering a compound as set forth in or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or hydrate thereof in an amount sufficient to achieve ACAT2 inhibition to a patient in need of such prevention or treatment.8. The method of claim 7 , wherein the disease is atherosclerosis and the amount sufficient to achieve ACAT2 inhibition is an amount sufficient to prevent or treat atherosclerosis in a patient.9. An ACAT2 inhibitor comprising as an active ingredient a compound as set forth in or a pharmaceutically acceptable salt claim 2 , solvate claim 2 , or hydrate thereof.10. An ACAT2 inhibitor comprising as an active ingredient a compound as set forth in or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , or hydrate thereof.11. An ACAT2 inhibitor comprising as an active ingredient a compound as set forth in or a pharmaceutically acceptable salt claim 4 , solvate claim 4 , or hydrate thereof.12. A pharmaceutical composition for ACAT2 inhibition comprising a compound as set forth in or a pharmaceutically acceptable salt claim 2 , solvate claim 2 , or hydrate thereof in an effective amount for inhibition of ACAT2 and a pharmaceutically acceptable carrier.13. A pharmaceutical composition for ...

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Номер записи: 16
04-04-2013 дата публикации

KETAL LACTONES AND STEREOSPECIFIC ADDUCTS OF OXOCARBOXYLIC KETALS WITH TRIMETHYLOL COMPOUNDS, POLYMERS CONTAINING THE SAME, METHODS OF MANUFACTURE, AND USES THEREOF

Номер: US20130085201A1
Автор: MULLEN Brian D., SELIFONOV Sergey, ZHOU Ning
Принадлежит: SEGETIS, INC.

Ketal lactones of and methods for making such ketal lactones are disclosed. Also described are methods for making isolated cis- and trans-stereoisomers of hydroxyester ketals of oxocarboxylic acids and polymers having ketal units of such stereoisomers within the polymer backbone. 4. A polymer composition comprising a polymer and a compound of .11. A polymer composition comprising a polymer and a compound of .14. A polymer composition comprising a polymer and a compound of .17. A polymer composition comprising a polymer and the combination of .21. A polymer of claim 18 , further comprising another polyester unit derived from a polyhydric alcohol having from 2 to 6 hydroxyl groups claim 18 , a C1-36 aliphatic or C6-36 aromatic dicarboxylic or tricarboxylic acid or its reactive derivative claim 18 , a hydroxylated carboxylic acid or its ester or lactone claim 18 , a hydroxyl-terminated linear or branched polyether claim 18 , a polyester polyol claim 18 , a polyurethane polyol claim 18 , a polysaccharide claim 18 , a poly(3-hydroxyalkanoate) claim 18 , a polylactate claim 18 , a polyglycolide claim 18 , a poly(co-lactate/glycolate) claim 18 , or a combination thereof.23. A polymer of claim 18 , comprising two to six of hydroxyl groups claim 18 , isocyanate groups claim 18 , (meth)acryloyl groups claim 18 , or (meth)allyl groups.24. A polymer of claim 18 , further comprising an additional claim 18 , different polymer claim 18 , a polymer additive claim 18 , or a combination thereof.25. An article comprising a polymer of .26. A foam comprising any of the polymers or compositions thereof of .31. A polymer composition of claim 30 , wherein the polymer further comprises units derived from the living polymerization in the further presence of another lactone claim 30 , a lactide claim 30 , glycolide claim 30 , bis-lactone claim 30 , dioxanone claim 30 , dioxepanone monomer claim 30 , trimethylene carbonate claim 30 , or dimethylene carbonate.32. An article comprising the ...

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Номер записи: 17
18-04-2013 дата публикации

FURO[3,2-G]CHROMENE COMPOUNDS AND USES THEREOF

Номер: US20130096112A1
Автор: Hu Chun, Huang Erfang, LI Dawei, Liu Xiaoping, Wang Shihui, Wang Yan
Принадлежит: SHENYANG PHARMACEUTICAL UNIVERSITY

Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators. 2. A pharmaceutical composition , comprising any one compound selected from the group consisting of a compound represented by formula I , a prodrug and a pharmaceutically active metabolite thereof , and a stereoisomer and a pharmaceutically acceptable salt thereof , as an active component; and a pharmaceutically acceptable carrier or diluent.3. Use of a compound represented by formula I or a pharmaceutical composition thereof for the preparation of a medicament useful for the treatment of a bone resorption disease , useful for the suppression of cytokine-related diseases , useful for the treatment of arthritis , or useful for the treatment or prevention of estrogen-related diseases.4. The use according to claim 3 , characterized in that the bone resorption disease is osteoporosis.5. (canceled)6. The use according to claim 3 , characterized in that the cytokine is IL-6 or GM-CSF.7. The use according to claim 3 , characterized in that the disease includes breast cancer claim 3 , prostate cancer claim 3 , colon cancer claim 3 , endometrial carcinoma claim 3 , ovary cancer claim 3 , osteosarcoma claim 3 , multiple myeloma claim 3 , renal cell carcinoma or cervical cancer.8. (canceled)9. Use of the compound according to for the modulation of gene expression in ER-expressing cells.10. The use according to claim 9 , characterized in that the ER is ERα or ERβ; the cells are cells of bone claim 9 , bladder claim 9 , uterus claim 9 , ovary claim 9 , prostate claim 9 , testicle claim 9 , epididymis claim 9 , gastrointestinal tract claim 9 , kidney claim 9 , breast claim 9 , eye claim 9 , heart claim 9 , vessel wall claim 9 , immune system claim 9 , lung claim 9 , pituitary claim 9 , hippocampus or hypothalamus.11. The use according to claim 9 , characterized ...

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Номер записи: 18
25-04-2013 дата публикации

ANTICANCER AGENT

Номер: US20130102776A1
Автор: ABE Masanao, HONMA Teruki, KOJIMA Hirotatsu, Nagano Tetsuo, Nakano Hirofumi, Okabe Takayoshi, SAITO Nae, Tanaka Akiko, Tsuganezawa Keiko, Yokoyama Shigeyuki, Yuki Hitomi
Принадлежит:

An anticancer agent comprising a compound represented by the formula (I) [Rrepresents hydrogen atom, hydroxyl group, a Calkoxy group and the like; Rand Rrepresents hydrogen atom, a halogen atom, a Calkyl group and the like; Rrepresents hydrogen atom, a Calkyl group, a Calkylsulfonyl group and the like; Rrepresents hydrogen atom or a substituent; represents a single bond or a double bond; Rand Rrepresents hydrogen atom, a Calkyl group and the like; Rrepresents hydrogen atom, a Calkyl group and the like; A represents —O—, —S—, or —CH—; D represents —C═ or —N═; X represents methylene group, —O—, or —CO—; Q represents —N═ or —C(R)═; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase. 3. The anticancer agent according to containing the compound or a physiologically acceptable salt thereof as an active ingredient claim 2 , wherein Ris hydrogen atom claim 2 , hydroxyl group claim 2 , a Calkoxy group claim 2 , an aryl-substituted Calkoxy group claim 2 , an aryloxy-substituted Calkoxy group claim 2 , a hydroxy-substituted Calkoxy group claim 2 , or a Calkoxy-substituted Calkoxy group; Ris hydrogen atom claim 2 , a halogen atom claim 2 , a Calkyl group claim 2 , a Calkoxy group claim 2 , an aryl group claim 2 , amino group claim 2 , hydroxyl group claim 2 , or a heterocyclic group claim 2 , wherein Rand Rmay bind together to form a Calkylenedioxy group; Ris hydrogen atom claim 2 , a halogen atom claim 2 , a Calkyl group claim 2 , a Calkoxy group claim 2 , an aryl group claim 2 , amino group claim 2 , hydroxyl group claim 2 , or a heterocyclic group; Ris hydrogen atom claim 2 , a Calkyl group claim 2 , an alkylsulfonyl group claim 2 , or an arylsulfonyl group; Ris hydrogen atom claim 2 , or one to four substituents substituting on the benzene ring or the pyridine ring (the substituent(s) is(are) selected from the group consisting of a halogen atom claim 2 , a Calkyl group claim 2 , a Calkenyl group claim 2 , a ...

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Номер записи: 19
02-05-2013 дата публикации

SALACINOL AND PONKORANOL HOMOLOGUES, DERIVATIVES THEREOF, AND METHODS OF SYNTHESIZING SAME

Номер: US20130109735A1
Автор: Eskarandi Razieh, Kumarasamy Jayakanthan, Mohan Sankar, Nasi Ravindranath, Pinto Brian Mario
Принадлежит: SIMON FRASER UNIVERSITY

Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from 5. (canceled)8. (canceled)9. (canceled)13. A method of using a compound as defined in as a glycosidase inhibitor claim 1 , comprising administering said compound to a patient.14. A method for treating diabetes in an affected patient comprising the step of administering to the patient a therapeutically effective amount of a compound as defined in .15. (canceled)16. (canceled) This application claims priority to, and the benefit under 35 U.S.C. §119 of, U.S. provisional patent application No. 61/265,695 filed 1 Dec. 2009 and entitled SALACINOL HOMOLOGUES, DERIVATIVES THEREOF AND METHODS OF SYNTHESIZING SAME, the entirety of which is hereby incorporated by reference.This application relates to salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using same.Glycosidases are enzymes that are involved in the catabolism of glycoproteins and glycoconjugates and the biosynthesis of oligosaccharides. Disruption in regulation of glycosidases can lead to diseases.Over the years, glycosidase inhibitors have received considerable attention in the field of chemical and medicinal researchbecause of their effects on quality control, maturation, transport, secretion of glycoproteins, and cell-cell or cell-virus recognition processes. This principle has potential for many therapeutic applications, such as in the treatment of diabetes, cancer and other viral infections.Bioactive components isolated from medicinal plants that are used in traditional medicine or folk medicine often provide the lead structures for modern drug-discovery programs. For example, ...

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Номер записи: 20
02-05-2013 дата публикации

MICHELIOLIDE DERIVATIVES, MEDICINAL COMPOSITION, PRODUCING METHOD AND USAGE THEREOF

Номер: US20130109749A1
Автор: Chen Yue, Ding Yahui, Fan Hongxia, Long Jing, Lu Yaxin, Ma Weiwei, Wang Miao, Zhai Jiadai, Zhang Haoliang, Zhang Quan
Принадлежит:

The present invention provides a compound of formula (I) 2. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises any of cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl claim 1 , heteroaryl.3. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises amino acid fragment and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid.4. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises —NRR claim 1 , and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid;{'sub': 7', '8, 'Wherein, Rand Rare any of hydrogen, alkyl, cycloalkyl, alkyl substituted by hydroxyl, alkenyl, alkynyl, aryl, alkyaryl, arylakyl, arylalkenyl, arylalkynyl, heterocyclic, trifluoromethyl, perfluoroalkyl, cyano, cyanomethyl, carboxyl, cabamate, sulfonyl, sulfonamide or aryloxyalkyl respectively.'}5. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises —NRR claim 1 , and pharmaceutically acceptable salts thereof formed with inorganic and/or organic acid;{'sub': 7', '8', '7', '8, 'Wherein, Rand Rtogether with N form a ring, and Rand Rare any of hydrogen, alkyl with 1 to 8 carbon atoms, any cycloalkyl respectively.'}6. A compound of claim 5 , wherein claim 5 , the ring comprises one or more than one substituent.7. A compound of claim 6 , wherein claim 6 , the one or more than one substituent is any of hydrogen claim 6 , alkyl claim 6 , cycloalkyl claim 6 , alkenyl claim 6 , alkynyl claim 6 , aryl claim 6 , alkyaryl claim 6 , arylakyl claim 6 , arylalkenyl claim 6 , arylalkynyl and heterocyclic.8. A compound of claim 5 , wherein claim 5 , the number of the ring is three to nine.9. A compound of claim 1 , wherein claim 1 , the substituent of the alkyl with Ccomprises quaternary ammonium salts formed by amino acid fragment or —NRRwith RZ;Wherein, Z is any of fluorine, chlorine, bromine, iodine, tosylate, ...

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Номер записи: 21
16-05-2013 дата публикации

Organic Electroluminescent Element, Material for Organic Electroluminescent Element, and Light Emitting Device, Display Device and Illumination Device Each Using the Element

Номер: US20130119359A1
Автор: KITAMURA Tetsu, Ouyang Tianhua, Sotoyama Wataru, Takaku Koji, WATANABE Toru, Yonekuta Yasunori, YOUFU Katsuyuki
Принадлежит: UDC IRELAND LIMITED

The disclosure relates to organic electroluminescent elements, materials for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): 2. The organic electroluminescent element according to claim 1 , wherein in the General Formula (1) Rto Rare each selected from a hydrogen atom claim 1 , an alkyl group claim 1 , an aryl group claim 1 , a heteroaryl group claim 1 , —NYY claim 1 , —OY claim 1 , —SY claim 1 , a halogen atom claim 1 , and a silyl group claim 1 , and{'sup': 1', '4, 'wherein Yto Yeach independently represents an alkyl group, an aryl group or a heteroaryl group, and which may further have substituents.'}6. The organic electroluminescent element according to claim 4 , wherein in the General Formula (3) Land Leach independently represents an arylene group or a heteroarylene group.14. The organic electroluminescent element according to claim 1 , wherein the light emitting layer includes an anthracene-based host material.15. The organic electroluminescent element according to claim 1 , wherein the light emitting layer is formed by a vacuum deposition process.16. The organic electroluminescent element according to claim 1 , wherein the light emitting layer is formed by a wet process.17. A light emitting device comprising the organic electroluminescent element according to .18. A display device comprising the organic electroluminescent element according to .19. An illumination device comprising the organic electroluminescent element according to . This application claims the benefit of priority to Japanese Patent Application No. 2011-250945, filed Nov. 16, 2011, which is incorporated herein by reference in its entirety.The present invention relates to an organic electroluminescent element and a material for an organic electroluminescent element which can be used in the same. The present invention also relates to a light emitting device, a display device, or an illumination device each using ...

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Номер записи: 22
16-05-2013 дата публикации

SIALIC ACID ANALOGS

Номер: US20130122094A1
Автор: JUNGLES Steven, Kakkis Emil
Принадлежит: ULTRAGENYX PHARMACEUTICAL, INC.

The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies. 3. The compound of claim 1 , wherein Ris hydrogen claim 1 , Y claim 1 , optionally substituted alkyl claim 1 , or structural formula (g).4. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris hydrogen.5. The compound of claim 4 , wherein at least two of R claim 4 , R claim 4 , and Rare hydrogen.6. The compound of claim 5 , wherein R claim 5 , R claim 5 , and Rare hydrogen.7. The compound of claim 1 , wherein Ris hydrogen.8. The compound of claim 1 , whereinm is 1;{'sup': '8a', 'Ris hydrogen; and'}{'sup': '9a', 'Ris hydrogen or lower alkyl.'}9. The compound of claim 1 , wherein{'sup': '1', 'Ris selected from structural formula (a), (b), (c), and (f); or a nucleoside phosphate moiety;'}{'sup': 2', '3', '5', '6, 'sub': '4', 'R, R, R, R, and Rare hydrogen.'}10. The compound of claim 1 , wherein{'sup': '1', 'Ris selected from structural formula (a), (b), (c), and (f); or a nucleoside phosphate moiety;'}{'sup': 2', '3', '4', '6, 'R, R, R, and Rare hydrogen;'}{'sup': '5', 'Ris optionally substituted alkyl or structural formula (g).'}11. The compound of claim 1 , wherein Ris structural formula (a); and at least one of Land Lis —O—.12. The compound of claim 11 , wherein Ris hydrogen or structural formula (g).13. The compound of claim 12 , wherein Z is hydrogen claim 12 , lower alkyl claim 12 , or structural formula (a).14. The compound of claim 11 , wherein Land Lare —O—.15. The compound of claim 11 , wherein Rand Rare independently hydrogen claim 11 , optionally substituted lower alkyl claim 11 , or optionally substituted aryl.16. The compound of claim 11 , wherein R claim 11 , R claim 11 , R claim 11 , and Rare hydrogen.17. The compound of claim 1 , wherein{'sup': '1', 'Ris structural formula (a);'}X is oxygen or sulfur;{'sup': 1', '2, 'Land Lare —O—;'}{'sup': 1a', '2a, 'Rand Rare independently hydrogen, lower alkyl, ...

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Номер записи: 23
23-05-2013 дата публикации

METHODS AND SYSTEMS FOR TREATING CELL PROLIFERATION DISORDERS WITH PSORALEN DERIVATIVES

Номер: US20130129757A1
Автор: Bourke, Gooden David, JR. Frederic A., TOONE Eric, Vo-Dinh Tuan
Принадлежит: Immunolight, LLC

Psoralen compounds of Formula (I): 7. A method for treating a cell proliferation disorder in a subject , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(1) administering to the subject one or more energy modulation agents and a psoralen compound of , that effects a predetermined cellular change when activated; and'}(2) applying an initiation energy from an initiation energy source to the subject, 'thus causing the predetermined cellular change to occur, wherein occurrence of the predetermined cellular change causes an increase in rate or decrease in rate of cell proliferation to treat the cell proliferation disorder.', 'wherein the one or more energy modulation agents convert the initiation energy applied to UV-A or visible energy, which then activates the psoralen compound in situ,'}13. The system of claim 10 , further comprising (3) one or more energy modulation agents.14. The system of claim 10 , further comprising (4) one or more plasmonics active agents.15. The system of claim 13 , further comprising (4) one or more plasmonics active agents.16. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or more psoralen compounds of ; and'}a pharmaceutically acceptable carrier.19. The pharmaceutical composition of claim 16 , further comprising one or more energy modulation agents.20. The pharmaceutical composition of claim 16 , further comprising one or more plasmonics-active agents.21. The pharmaceutical composition of claim 19 , further comprising one or more plasmonics-active agents.26. The method of claim 25 , wherein the irradiation source wavelength is a UV wavelength.27. The method of claim 25 , wherein the irradiation source wavelength is an IR wavelength and the activation of the psoralen compound takes place by a multiphoton absorption.30. The method of claim 4 , wherein the cell proliferation disorder is cancer.31. The method of claim 30 , wherein the cancer is breast cancer.32. The method of claim 7 ...

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Номер записи: 24
23-05-2013 дата публикации

Harmful organism control agent

Номер: US20130131091A1
Автор: Hiroshi Tomoda, Kazuhiko Oyama, Kimihiko Goto, Masaaki Mitomi, Masato Tani, Nobuto Minowa, Nozomu Nakanishi, Ryo Horikoshi, Satoshi Omura, Toshiaki Sunazuka, Yoshimasa Fukuda
Принадлежит: Meiji Seika Pharma Co Ltd

The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R 1 , R 2 , R 3 , R 7 , R 10a , R 10b , R 11 , and R 12 represent a hydrogen atom; R 4 , R 5 , and R 6 represent a hydrogen atom, hydroxyl, optionally substituted C 1-18 alkylcarbonyloxy, optionally substituted C 1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C 1-6 alkyloxy-C 1-6 alkyloxy, C 1-6 alkyloxy-C 1-6 alkyloxy-C 1-6 alkyloxy; R 8 represents a hydrogen atom; and R 13a , R 13b , and R 13c represent methyl.

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Номер записи: 25
23-05-2013 дата публикации

METHODS AND SYSTEMS FOR TREATING CELL PROLIFERATION DISORDERS WITH PSORALEN DERIVATIVES

Номер: US20130131429A1
Автор: Bourke, Gooden David, JR. Frederic A., TOONE Eric, Vo-Dinh Tuan
Принадлежит: lmmunolight, LLC

Psoralen compounds of Formula (I): 3. A method for treating a cell proliferation disorder in a subject , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(1) administering to the subject a psoralen compound of , that effects a predetermined cellular change when activated; and'}(2) applying an initiation energy from an initiation energy source to the subject, activating the psoralen compound in situ,thus causing the predetermined cellular change to occur, wherein occurrence of the predetermined cellular change causes an increase in rate or decrease in rate of cell proliferation to treat the cell proliferation disorder.5. A method for treating a cell proliferation disorder in a subject , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(1) administering to the subject one or more energy modulation agents and a psoralen compound of , that effects a predetermined cellular change when activated; and'}(2) applying an initiation energy from an initiation energy source to the subject, 'thus causing the predetermined cellular change to occur, wherein occurrence of the predetermined cellular change causes an increase in rate or decrease in rate of cell proliferation to treat the cell proliferation disorder.', 'wherein the one or more energy modulation agents convert the initiation energy applied to UV-A or visible energy, which then activates the psoralen compound in situ,'}7. A system for treatment of a cell proliferation disorder , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(1) an initiation energy source; and (2) one or more psoralen compounds of .'}9. The system of claim 7 , further comprising (3) one or more energy modulation agents.10. The system of claim 7 , further comprising (4) one or more plasmonics active agents.11. The system of claim 9 , further comprising (4) one or more plasmonics active agents.12. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or more psoralen ...

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Номер записи: 26
20-06-2013 дата публикации

FUSED TRICYCLIC ETHER CARBAMATES AND THEIR USE

Номер: US20130158094A1
Автор: Ghosh Arun K., Mitsuya Hiroaki, Parham Garth, Xu Chun-Xiao
Принадлежит: PURDUE RESEARCH FOUNDATION

Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described. 2. (canceled)4. (canceled)5. The compound of wherein Xis a bond.7. (canceled)9. (canceled)10. The compound of wherein Y is hydrogen.11. The compound of wherein W claim 1 , W claim 1 , and Ware oxygen.14. The compound of wherein Rand Rare each hydrogen.15. The compound of wherein Ris optionally substituted arylalkyl claim 1 , Xis a bond claim 1 , Ris hydrogen claim 1 , Xis S(O) claim 1 , Ris optionally substituted aryl claim 1 , and Ris iso-butyl.16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. The compound of wherein Ris optionally substituted arylalkyl.22. The compound of wherein Wis oxygen.23. The compound of wherein Wor Wis oxygen.24. The compound of wherein Wand one of Wor Wis oxygen.25. The compound of wherein Wand Ware oxygen.26. The compound of wherein each of W claim 1 , W claim 1 , and W3 is oxygen.27. The compound of wherein Wis optionally substituted methylene.28. (canceled)29. A pharmaceutical composition comprising one or more compounds of and further comprising one or more carriers claim 1 , diluents claim 1 , or excipients claim 1 , or a combination thereof for treating HIV infection.30. (canceled)31. A method for treating a patient in need of relieve of an HIV infection claim 1 , the method comprising the step of administering to a patient in need of relief from the HIV infection a therapeutically effective amount of one or more compounds of or a pharmaceutical composition thereof. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application Ser. No. 61/379,414 filed on Sep. 2, 2010, the entire disclosure of which is hereby incorporated by reference.This invention relates to compounds that inhibit HIV proteolytic enzymes and processes for preparing the compounds. The invention also ...

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Номер записи: 27
27-06-2013 дата публикации

PROCESS FOR THE DIRECT AMINATION OF SECONDARY ALCOHOLS WITH AMMONIA TO GIVE PRIMARY AMINES

Номер: US20130165672A1
Автор: Deutsch Jens, Haas Thomas, Klasovsky Florian, Koeckritz Angela, Martin Andreas, Pfeffer Jan Christoph, Tacke Thomas
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a process for preparing primary amines which comprises the process steps 1. A process for preparing a primary amine , the process comprising:i) providing a solution of a secondary alcohol in a fluid, nongaseous phase, free ammonia, at least one ammonia-releasing compound, or both,', 'and a homogeneous catalyst, and, 'ii) contacting the solution with'} 'wherein:', 'iii) optionally isolating the primary amine obtained in said contacting ii),'}a) a volume ratio of a liquid phase to a gas phase in said contacting ii) is greater than or equal to 0.25, orb) a molar ratio of the ammonia to hydroxyl groups in the secondary alcohol is at least 5:1, orboth a) and b).2. The process according to claim 1 , wherein the homogeneous catalyst isan alkali metal alkoxide, an aluminium alkoxide, a lanthanide alkoxide, an inorganic compound of noble metals,a monometallic or multimetallic, mononuclear or multinuclear coordination compound of at least one noble metal selected from the group consisting of ruthenium, iridium, rhodium, osmium, palladium, platinum and iron,or any mixture thereof.3. The process according to claim 1 ,whereinthe secondary alcohol comprises at least two secondary hydroxy groups.4. The process according to claim 1 ,whereinthe secondary alcohol comprises a cyclic or polycyclic carbon skeleton.5. The process according to claim 1 ,whereinthe secondary alcohol is selected from the group consisting of:2-dodecanol, cyclododecanol, 4-phenyl-2-butanol, isosorbide, isomannide, isoidite, polypropylene glycol, mannitol, sorbitol, galactitol and an alkyl glycoside.6. The process according to claim 1 ,whereinthe secondary alcohol is selected from the group consisting of an alpha-hydroxycarboxylic acid and an OH-modified, natural fatty acid.7. The process according to claim 1 ,wherein a liquid or supercritical ammonia, a solution of ammonium salts in a solvent, or both is used in said contacting ii).8. The process according to claim 1 ,whereinsaid ...

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Номер записи: 28
04-07-2013 дата публикации

Semiconducting Compounds and Related Compositions and Devices

Номер: US20130168659A1
Автор: Antonio Facchetti, Christopher Newman, Hakan Usta, He Yan, Zhihua Chen
Принадлежит: Polyera Corp

Disclosed are new semiconductor materials prepared from thienocoronene-based compounds and related heteroaromatic analogs. Such compounds can exhibit high carrier mobility and/or good current modulation characteristics. In addition, the compounds of the present teachings can possess certain processing advantages such as solution-processability and/or good stability at ambient conditions.

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Номер записи: 29
04-07-2013 дата публикации

PROCESS FOR PREPARATION OF HIV PROTEASE INHIBITORS

Номер: US20130172295A1
Автор: Crawford Kenneth R., DOWDY Eric D., Gutierrez Arnold, Polniaszek Richard P., Yu Richard Hung Chiu
Принадлежит: Gilead Sciences, Inc.

A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed 4. The process of claim 1 , where the reaction is carried out at a temperature of between about 0° C. to about 100° C.5. The process of claim 1 , where the reaction is carried out in the presence of a catalyst comprising a lanthanide or transition metal complexed to a chiral ligand.7. The process of claim 1 , which is carried out in the presence of a solvent.8. The process of claim 7 , where the solvent is a polar aprotic solvent.9. The process of claim 8 , where the solvent is methyl-t-butyl-ether claim 8 , dichloromethane or a mixture thereof.10. The process of claim 1 , which is carried out in the presence of excess 2 claim 1 ,3-dihydrofuran as a solvent.11. The process of claim 1 , where the catalyst comprises Sc.12. The process of claim 1 , where the catalyst comprises Yb.18. The process of claim 17 , where the deprotection is accomplished by combining the compound of Formula M with a deprotecting agent which is selected from trifluoroacetic acid claim 17 , hydrochloric acid claim 17 , toluenesulfonic acid claim 17 , methanesulfonic acid claim 17 , benzenesulfonic acid claim 17 , or hydrobromic acid.20. The process of claim 19 , where the reduction is accomplished by contacting the compound of Formula C with a reducing agent which is lithium aluminum hydride claim 19 , sodium borohydride claim 19 , lithium borohydride claim 19 , sodium trisacetoxyborohydride claim 19 , sodium cyanoborohydride claim 19 , potassium triisopropoxy borohydride or diisobutyl aluminum hydride28. A pharmaceutical composition comprising the salt of and an excipient claim 27 , diluent or carrier.29. A method for the treatment or prophylaxis of a retrovirus infection in a patient claim 27 , comprising administering to the patient a therapeutically effective amount of the salt of .30. The method of claim 29 , where the retrovirus is human ...

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Номер записи: 30
18-07-2013 дата публикации

Composition for Lowering Blood Lipid and Elevating High-density Lipoprotein and Method for Manufacturing the Same

Номер: US20130184473A1
Автор: Lee Chun-Lin, Pan Tzu-Ming, Wu Chen-Lun
Принадлежит: SUNWAY BIOTECH CO., LTD.

The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a fermented product with acetone for three times; elevating the concentration of the fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially. 1MonascusMonascus. A composition for lowering blood lipid and elevating high-density lipoprotein , wherein the composition comprises ankaflavin , which is a yellow pigment and extracted from a fermented product.2. The composition for lowering blood lipid and elevating high-density lipoprotein according to claim 1 , wherein an amount of the ankaflavin taken by an adult is more than 0.6 mg per day.3. A method for manufacturing a composition for lowering blood lipid and elevating high-density lipoprotein claim 1 , wherein the method comprises the steps of:{'i': 'Monascus', '(1) providing a fermented product;'}{'i': 'Monascus', '(2) treating the fermented product with acetone for three times;'}(3) elevating the concentration of the product obtained from the previous step by a process of decompress concentration in a specific temperature range;(4) separating a pigment fraction from the product obtained from the previous step by a silica gel column chromatography;(5) separating a yellow pigment fraction from the pigment fraction by a Sephadex LH-20 column chromatography;(6) separating a fraction containing monascin and ankaflavin from the yellow pigment fraction by the silica gel column chromatography; and(7) separating ankaflavin from the fraction containing monascin and ankaflavin obtained ...

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Номер записи: 31
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: 32
01-08-2013 дата публикации

SYNTHESIS OF SUBSTITUTED SALICYLALDEHYDE DERIVATIVES

Номер: US20130197223A1
Автор: Farmer Jay J., Job Gabriel E.
Принадлежит: NOVOMER, INC.

Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a). 1. A method comprising the steps of:a) providing salicylaldehyde or a derivative thereof, andb) forming an anhydro dimer of the provided salicylaldehyde compound.2. The method of claim 1 , further comprising the step of performing one or more chemical transformations on the anhydro dimer.3. The method of claim 2 , further comprising the step of hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).4. The method of claim 3 , comprising the steps of:a) dehydrating a salicylaldehyde to form an anhydro dimer;b) alkylating at least one aromatic ring of the anhydro dimer in one or more positions; andc) hydrolyzing the alkylated anhydro dimer to recover an alkylated salicyladehyde derivative.5. The method of claim 4 , wherein the step of alkylating the aromatic ring comprises reacting the anhydro dimer under Friedel Crafts alkylating conditions.6. The method of claim 5 , wherein the Friedel Crafts alkylating conditions comprise reacting the anhydro dimer with at least one compound selected from the group consisting of: alkenes claim 5 , alcohols claim 5 , alkyl halides claim 5 , and mixtures of two or more of these in the presence of a promoter selected from the group consisting of Lewis acids and proton acids.7. The method of claim 4 , wherein the alkylation occurs equally on both salicylaldhyde molecules comprising the anhydro dimer.8. The method of claim 4 , wherein the alkylation occurs at the aromatic ring position ortho to the hydroxyl group of the starting salicylaldehyde. ...

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Номер записи: 33
15-08-2013 дата публикации

Novel Derivatives Useful as Antiviral Agents

Номер: US20130210886A1
Автор: Dauzonne Daniel, LUCAS-HOURANI Marianne, Munier-Lehmann Héléne, Tangy Frederic, Vidalain Pierre-Olivier
Принадлежит:

The invention relates to compounds of formula (I) for use in the prevention and/or treatment of viral infections: Wherein X, Y, Z, T, Rand Rare as defined in claim . 2. The compound of formula (I) for use according to claim 1 , wherein X is O.3. The compound of formula (I) for use according to claim 1 , wherein is a double bond.4. The compound of formula (I) for use according to claim 1 , wherein is a single bond.5. The compound of formula (I) for use according to claim 4 , wherein Rand Rare in a trans configuration.6. The compound of formula (I) for use according to claim 1 , wherein -Z-T- is —C(R)(R)—(CH)—.7. The compound of formula (I) for use according to claim 6 , wherein n is 1.8. The compound of formula (I) for use according to claim 6 , wherein Rand Rare H.9. The compound of formula (I) for use according to claim 1 , wherein Rand Rare H.10. The compound of formula (I) for use according to claim 1 , wherein at least one of R claim 1 , R claim 1 , Ris selected from I claim 1 , Cl claim 1 , Br claim 1 , or —CH═CH claim 1 , the others being H.11. The compound of formula (I) for use according to claim 1 , which is selected from:-3-(5-chloro-2-methoxyphenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-bromophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-fluorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(4-chlorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(2-chlorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-methoxyphenyl)-6,7-dihydrobenzofuran-4(5H)-one;3-(3,5-dichlorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-nitrophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-((3-trifluoromethyl)phenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-benzyloxyphenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3,4,5-trimethoxyphenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3,4-dichlorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-iodo-4-methoxyphenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-iodophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-chlorophenyl)-6,7-dihydro-5H-benzofuran-4-one;3-(3-chlorophenyl)-6,6-dimethyl-6,7- ...

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Номер записи: 34
15-08-2013 дата публикации

Intermediates and methods for making zearalenone macrolide analogs

Номер: US20130211103A1
Автор: Charles-Andre Lemelin, Francis G. Fang, Hong Du, Jing Li, Kevin (kuo-ming) Wu, Matthew J. Schnaderbeck, Pamela Mcguinness, Roch Boivin, Silvio A. Campagna, Thomas Horstmann, Xiang Niu, Xiaojie (Jeff) Zhu
Принадлежит: Eisai R&D Management Co Ltd

Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R 1 -R 12 are as defined herein.

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Номер записи: 35
29-08-2013 дата публикации

SUBSTITUTED 4-BETA-ACRYLAMIDOPODOPHYLLOTOXIN CONGENERS AS ANTITUMOUR ANTIBIOTICS AND THE PROCESS FOR PREPARATION THEREOF

Номер: US20130225672A1
Автор: Ahmed Kamal, Banala Ashwini Kumar, Paidakula Suresh, Reddy Adla Malla, Reddy Papagiri Venkat
Принадлежит: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

The present invention provides compounds of general formula (3) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4β-acrylamidopodophyllotoxin congeners of general formula (3), wherein R and R1 are an aryl group and R is selected from 3,4,5-trimethoxyphenyl or 2-methoxy phenyl and R1 is selected from the group consisting of 4-hydroxy-3-methoxyphenyl, 3-hydroxy-4-methoxyphenyl, 4-fluoro-3-methoxyphenyl, 3-fluoro-4-methoxyphenyl, 2-fluoro-5-methoxyphenyl, 2-fluoro-4-methoxyphenyl, 4-hydroxy-3-nitrophenyl, 4-methoxy-3-nitrophenyl, 4-nitrophenyl, 3-nitrophenyl, 2-nitro phenyl, 4-methoxyphenyl, 3-methoxyphenyl and 4-hydroxyphenyl. 2. The compound of claim 1 , wherein chemical formulae of the representative compounds are:4β-(E)-3-(4-hydroxy-3-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3a);4β-(E)-3-(3-hydroxy-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3b);4β-(E)-3-(4-fluoro-3-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3c);4β-(E)-3-(3-fluoro-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3d);4β-(E)-3-(2-fluoro-5-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3e);4β-(E)-3-(2-fluoro-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3f);4β-(E)-3-(4-hydroxy-3-nitrophenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3g);4β-(E)-3-(4-methoxy-3-nitrophenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3h);4β-(E)-3-(4-nitrophenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3i);4β-(E)-3-(3-nitrophenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3j);4β-(E)-3-(2-nitrophenyl)-2-(3,4,5-trimethoxyphenyl)acrylamidopodophyllotoxin (3k);4β-(E)-2-(2-methoxyphenyl)-3-(4-nitrophenyl)acrylamidopodophyllotoxin (3l);4β-(E)-2-(2-methoxyphenyl)-3-(2-nitrophenyl)acrylamidopodophyllotoxin (3m);4β-(E)-3-(4-methoxyphenyl)-2-(3,4,5- ...

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Номер записи: 36
12-09-2013 дата публикации

INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B

Номер: US20130237711A1
Автор: Benayoud Farid, Calkins Trevor Lee, Chase Charles E., Christ William, Fang Francis G.
Принадлежит: Eisai R&D Management Co., Ltd.

Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided. 8. The compound of claim 1 , wherein the compound is of formula C claim 1 , and Ris methyl.10. The compound of claim 9 , wherein said suitable hydroxyl protecting group claim 9 , taken with the oxygen atom to which it is bound claim 9 , is selected from an ester claim 9 , a silyl ether claim 9 , an alkyl ether claim 9 , an arylalkyl ether claim 9 , and an alkoxyalkyl ether.11. The compound of claim 9 , wherein said suitable leaving group is selected from the group consisting of sulphonyloxy claim 9 , optionally substituted alkylsulphonyloxy claim 9 , optionally substituted alkenylsulfonyloxy claim 9 , optionally substituted arylsulfonyloxy claim 9 , and halogen. This application is a continuation of U.S. application Ser. No. 13/476,276, filed May 21, 2012, which is a continuation of U.S. application Ser. No. 13/171,971, filed Jun. 29, 2011, which is a continuation of U.S. application Ser. No. 11/628,396, filed Mar. 28, 2007 (U.S. Pat. No. 7,982,060), which claims priority under 35 U.S.C. §371 from International Application No. PCT/US05/019669, filed Jun. 3, 2005, which claims benefit of U.S. Provisional Patent Application Nos. 60/576,642, filed Jun. 3, 2004, 60/626,769, filed Nov. 10, 2004, and 60/663,300 filed Mar. 18, 2005, the entire contents of each of which are incorporated herein by reference.The present invention relates to compounds useful as intermediates in the synthesis of pharmaceutically active macrolide compounds.The invention relates to pharmaceutically active macrolides, synthesis thereof and intermediates thereto. Halichondrin B is a potent anticancer agent originally isolated from the marine sponge , and subsequently found in sp., , and sp. A total synthesis of Halichondrin B was published in 1992 (Aicher, T. D. et al., 114:3162-3164). Halichondrin B has demonstrated in vitro inhibition of tubulin polymerization, microtubule assembly, beta-tubulin ...

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Номер записи: 37
19-09-2013 дата публикации

PROCESS FOR THE PREPARATION OF (3R, 3AS, 6AR)-HEXAHYDROFURO [2, 3- B] FURAN-3-OL

Номер: US20130244297A1
Автор: Kothari Satish Babu, Ponnuru Anil, Sahu Arabinda, Shimpi Nitin Ashok, Vellenki Siva Rama Prasad
Принадлежит: Mylan Laboratories Ltd.

The present invention relates to a novel process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol. 127.-. (canceled)30. The process according to or , wherein the step of separating the enantiomers and diasteromers of the compound of formula IV to obtain the compound of formula I is carried out via an enzymatic or a chemical process.32. The process according to claim 31 , wherein the catalyst used in step a) is N claim 31 ,N-dimethylamino pyridine.36. The process according to further comprising resolving or separating the enantiomers of the compound of formula IV to obtain the compound of formula I.3735. The process according to claim 35 , claim 35 , claim 35 , or claim 35 , wherein the compound of formula I is used as an intermediate in the preparation of HIV protease inhibitors.38. The process according to claim 37 , wherein the HIV protease inhibitor is Darunavir. This application claims priority to Indian patent application No 3518/CHE/2010 filed on Nov. 22, 2010 the contents of which are incorporated by reference in their entirety.The present invention relates to a process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol, which is useful as an intermediate in the preparation of protease ...

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Номер записи: 38
19-09-2013 дата публикации

New Process for Preparing Cyclolignans

Номер: US20130245285A1
Автор: Axelsson Magnus, Bremberg Ulf, Linden Auri, Von Kieseritzky Fredrik
Принадлежит: Axelar AB

The invention relates to a one-pot reaction for the preparation of a compound of Formula (I). The compound of Formula (I) may be further transformed into picropodophyllin and derivatives thereof. 3. The process according to claim 1 , wherein the transition metal component is selected from the group consisting of Pd(0) claim 1 , a compound containing Pd(II) claim 1 , a compound containing Pd(0) claim 1 , a mixture of compounds containing Pd(II) and Pd(0) claim 1 , and a mixture of Pd(0) and a compound containing Pd(II) and/or Pd(0).4. The process according to claim 1 , wherein the transition metal component is Ni(0) or Ni(II).5. The process according to claim 3 , wherein the transition metal component is the Herrmann-Beller catalyst.6. The process according to claim 3 , wherein the transition metal component is Pd-118.7. The process according to claim 1 , wherein the activating group P is selected from the group consisting of trifluoromethanesulfonate claim 1 , methanesulfonate claim 1 , ethanesulfonate claim 1 , benzenesulfonate claim 1 , toluenesulfonate and 4-nitro-benzenesulfonate.8. The process according to claim 1 , wherein the base is an inorganic base.9. The process according to claim 8 , wherein the base is selected from the group consisting of KCO claim 8 , NaCO claim 8 , KHCO claim 8 , NaHCO claim 8 , NaOH claim 8 , CsCO claim 8 , KOH claim 8 , NaOH claim 8 , NaPO claim 8 , NaHPO claim 8 , KPO claim 8 , KHPO claim 8 , and NHOH.10. The process according to claim 1 , wherein the base is an amine base.11. The process according to claim 10 , wherein the amine base is selected from the group consisting of ammonia claim 10 , trimethyl amine claim 10 , triethyl and diisopropyl ethylamine.12. The process according to claim 1 , wherein the transition metal component is selected from the group consisting of Pd(dppf).DCM claim 1 , tetrakis(triphenylphosphine)Pd(0) claim 1 , Pd(dba) claim 1 , dichlorobis(triphenylphosphine)-palladium(0) claim 1 , palladium(II) acetate ...

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Номер записи: 39
10-10-2013 дата публикации

COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILIZATION

Номер: US20130267554A1
Автор: Barbaras Ronald, Dasseux Jean-Louis Henri, GEOFFROY Otto, Oniciu Daniela Carmen
Принадлежит: Cerenis Therapeutics Holding SA

The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein. 2. The compound or pharmaceutically acceptable salt of the compound of claim 1 , wherein Zis N.3. The compound or pharmaceutically acceptable salt of the compound of claim 2 , wherein Ris OH claim 2 , COOH claim 2 , or an alkyl ester group.4. The compound or pharmaceutically acceptable salt of the compound of claim 3 , wherein Ris 2-halo.5. The compound or pharmaceutically acceptable salt of claim 4 , wherein each of Rand Ris independently H or alkyl.8. The composition of claim 7 , wherein the composition is formulated for oral administration.9. The composition of claim 7 , wherein the composition is in the form of a tablet or capsule.10. The composition of claim 7 , wherein the compound or salt thereof is present in an amount of about 1 mg to about 1 claim 7 ,000 mg.11100-. (canceled) This application is a division of U.S. application Ser. No. 13/276,238, now U.S. Pat. No. 8,349,833, filed Oct. 18, 2011, which claims the benefit of U.S. Provisional Application No. 61/394,136, filed Oct. 18, 2010, and U.S. Provisional Application No. 61/444,212, filed Feb. 18, 2011, the disclosure of each of which is hereby incorporated by reference herein in its entirety.The invention provides compounds, compositions, and methods of treatment or prevention of abnormal conditions in a subject.Cholesterol circulating in the human body is carried by plasma lipoproteins, which are particles of complex lipid and protein composition that transport lipids in the blood. Two types of plasma lipoproteins that carry cholesterol are low density lipoproteins (“LDL”) and high density lipoproteins (“HDL”). LDL particles ...

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Номер записи: 40
24-10-2013 дата публикации

METHODS FOR REGULATING CELL MITOSIS BY INHIBITING SERINE/THREONINE PHOSPHATASE

Номер: US20130280210A1
Автор: KOVACH John S.
Принадлежит:

Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress N—CoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death. 3. The method of claim 2 , wherein the cancer cell does not overexpress N—CoR.5. The method of claim 4 , wherein the cancer cell does not overexpress N—CoR.6. The method of claim 1 , wherein the cancer is selected from adrenocortical cancer claim 1 , bladder cancer claim 1 , osteosarcoma claim 1 , cercial cancer claim 1 , esophageal claim 1 , gallbladder claim 1 , head and neck cancer claim 1 , Hodgkin lymphoma claim 1 , non-Hodgkin lymphoma claim 1 , renal cancer claim 1 , melanoma claim 1 , pancreatic cancer claim 1 , rectal cancer claim 1 , thyroid cancer and throat cancer.7. The method of claim 1 , wherein the cancer is selected from breast cancer claim 1 , lung cancer claim 1 , prostate cancer claim 1 , and head and neck cancer.8. The method of claim 1 , wherein the anti-cancer agent is selected from x-radiation claim 1 , ionizing radiation claim 1 , a DNA damaging agent claim 1 , a DNA intercalating agent claim 1 , a microtubule stabilizing agent claim 1 , a microtubule destabilizing agent claim 1 , a spindle toxin claim 1 , abarelix claim 1 , aldesleukin claim 1 , alemtuzumab claim 1 , alitertinoin claim 1 , allopurinol claim 1 , altretamine claim 1 , amifostin claim 1 , anakinra claim 1 , anastrozole claim 1 , arsenic trioxide claim 1 , asparaginase claim 1 , azacitidine claim 1 , bevacizumab claim 1 , bexarotene claim 1 , bleomycin claim 1 , bortezomib claim 1 , busulfan claim 1 , calusterone claim 1 , capecitabine claim 1 , carboplatin claim 1 , carmustine claim 1 , celecoxib claim 1 , cetuximab claim 1 , chlorambucil claim 1 , cisplatin claim 1 , cladribine claim 1 , clofarabine claim 1 , cyclophosphamide ...

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Номер записи: 41
24-10-2013 дата публикации

METHOD OF MAKING DIACETAL COMPOUND IN AQUEOUS MEDIUM

Номер: US20130281716A1
Автор: Aduri Pavankumar, RATNAPARKHI Uday, SAKHALKAR Mangesh, UPPARA Parasu Veera
Принадлежит: RELIANCE INDUSTRIES LIMITED

This invention is directed to a process for preparation of acetal derivatives, 1,3:2,4-bis (3,4-dimethylbenzylidene)sorbitol (DMDBS) and 1,3:2,4-bis (4-methylbenzylidene)sorbitol (MDBS) by carrying out a dehydrocondensation reaction between an aldehyde and an alditol using an aqueous ionic fluid as the acid catalyst. 1. A process for preparation of acetal derivatives selected from the group consisting of 1 ,3:2 ,4-bis(3 ,4-dimethylbenzylidene)sorbitol (DMDBS) and 1 ,3:2 ,4-bis(4-methylbenzylidene)sorbitol (MDBS) comprising the following steps:preparing an aqueous ionic fluid;carrying out a dehydrocondensation reaction by adding an aldehyde and an alditol in a mole ratio of 2:1 in the ionic fluid under continuous stirring to form a reaction mixture;stirring the resultant reaction mixture to maintain the contents in a suspension form; anddiscontinuing the stirring of the reaction mixture to allow the mass formed in the reaction mixture to settle;isolating and purifying the mass by filtering, washing and drying to obtain an acetal derivative without any free acid residue present therein.2. A process as claimed in claim 1 , wherein the aqueous ionic fluid acts as a catalyst for the dehydrocondensation reaction.3. A process as claimed in claim 1 , wherein the aqueous ionic fluid acts as a reaction medium for the dehydrocondensation reaction.4. A process as claimed in claim 1 , wherein the aqueous ionic fluid comprises an ionic compound formed by the hydrogen bonding between at least one hydrogen donor selected from the group consisting of methanesulfonic acid (MSA) claim 1 , para toluenesulfonic acid (PTSA) claim 1 , oxalic acid claim 1 , citric acid claim 1 , benzoic acid claim 1 , maleic acid and tartaric acid and at least one counter ion from at least one counter ion providing compound selected from the group consisting of cholin chloride claim 1 , sodium chloride and zinc chloride.5. A process as claimed in claim 1 , wherein the aldehyde is at least one aldehyde ...

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Номер записи: 42
24-10-2013 дата публикации

HIGH-FLUIDITY NON-CAKING DIANHYDROHEXITOL PELLETS

Номер: US20130281718A1
Автор: Ibert Mathias, Saint Pol Jerome, Wyart Hervé
Принадлежит: ROQUETTE FRERES

Dianhydrohexitol pellets, whose fluidity is preserved even after lengthy storage, include between 90% and 100%, preferably between 95% and 100%, and more preferentially between 97% and 100% of dianhydrohexitols by weight, on a dry weight basis, and have the particularity of not being subject to caking. A process for preparing the dianhydrohexitol pellets is also described. 115-. (canceled)16. High-fluidity and non-caking dianhydrohexitol pellets comprising between 90% and 100% by weight , preferably between 95% and 100% by weight and more preferably between 97% and 100% by weight of dianhydrohexitols on a dry basis.17. The dianhydrohexitol pellets as claimed in claim 16 , comprising less than 2% by weight of anticaking agent claim 16 , preferably less than 0.5% by weight and more preferably still less than 0.01% by weight on a dry basis.18. The dianhydrohexitol pellets as claimed in claim 16 , wherein said dianhydrohexitols are chosen from isosorbide claim 16 , isomannide claim 16 , isoidide and the mixtures of at least two of these products.19. The dianhydrohexitol pellets as claimed in claim 16 , said dianhydrohexitol pellets exhibiting:a bulk density of between 0.80 and 1.00 g/ml, preferably of between 0.81 and 0.85 g/ml and more preferably still of between 0.82 and 0.84 g/ml,a tapped density, evaluated according to a test A, of between 0.81 and 1.00 g/ml, preferably of between 0.82 and 0.86 g/ml and more preferably still of between 0.83 and 0.85 g/ml.20. The dianhydrohexitol pellets as claimed in claim 16 , said dianhydrohexitol pellets exhibiting a tapping claim 16 , evaluated according to the test A claim 16 , at least equal to 2% claim 16 , preferably between 0.5% and 2% and more preferably still between 0.8% and 1.6%.21. The dianhydrohexitol pellets as claimed in claim 16 , said dianhydrohexitol pellets exhibiting a compressibility claim 16 , evaluated according to a test B carried out at 20° C. claim 16 , of less than 5% claim 16 , preferably of less than 3 ...

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Номер записи: 43
31-10-2013 дата публикации

CYCLIC BRIDGEHEAD ETHER DGAT1 INHIBITORS

Номер: US20130289058A1
Автор: Chen Xin, DING Yiping, Duvadie Rohit, Gai Yu, Harrison Tyler, Larrow Jay, Lui Qian, Mao Justin, Patel Sejal, Ye Jiong, ZECRI Frederic, ZHENG Rui, Zheng Xuchun, ZHOU Yizong
Принадлежит:

The invention relates to compounds of formula (I): 5. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein p is 1.6. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein p is 2.7. The compound according to or a salt or solvate thereof claim 1 , wherein Z claim 1 , Z claim 1 , Zand Zare all CH.8. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein Zis N and Z claim 1 , Zand Zare each CH.9. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein Zis N and Z claim 1 , Zand Zare each CH.10. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein Zand Zare both N and Zand Zare both CH.11. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein L is C(O).12. The compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein L is absent.16. The compound of claim 1 , or a salt or solvate thereof claim 1 , which compound is selected from:2-(4-(4′-((5-cyclobutyl-1,3,4-thiadiazol-2-yl)amino)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(4-(4′-((5-cyclobutyl-1,3,4-oxadiazol-2-yl)amino)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(4-(4-(5-(2-methyl-5-(trifluoromethyl)oxazole-4-carboxamido)pyridin-2-yl)phenyl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(4-(4-(5-(2-ethyl-4-methyloxazole-5-carboxamido)pyridin-2-yl)phenyl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(4-(4′-(2-ethyl-4-methyloxazole-5-carboxamido)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(4-(4′-((5-(tert-butyl)-1,3,4-oxadiazol-2-yl)amino)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-1-yl)acetic acid;2-(1-(4′-((5-cyclobutyl-1,3,4-oxadiazol-2-yl)amino)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-4-yl)acetic acid;2-(1-(4′-(2-methyl-5-(trifluoromethyl)oxazole-4-carboxamido)-[1,1′-biphenyl]-4-yl)-2-oxabicyclo[2.2.2]octan-4-yl)acetic acid;2-(1-(4-(5-((5-cyclobutyl-1, ...

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Номер записи: 44
31-10-2013 дата публикации

COMPOUNDS AND METHODS FOR TREATING HIV

Номер: US20130289067A1
Автор: Chapsal Bruno D., Ghosh Arun K., Mitsuya Hiroaki
Принадлежит:

Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described. 2. The compound or salt of wherein Aris phenyl substituted with one or more methoxy claim 1 , hydroxymethyl claim 1 , fluoro or 2-(morpolino)ethoxy groups;3. The compound or salt of wherein Ris 2-fluoro-2-methylpropyl.5. The compound or salt of wherein Ris O or S; and Ris NHR; and Ris isopropyl or cyclopropyl.8. The compound or salt of wherein Aris 3-methoxyphenyl claim 7 , 4-methoxyphenyl claim 7 , 3-isopropoxyphenyl claim 7 , 4-isopropoxyphenyl claim 7 , 3-hydroxymethylphenyl claim 7 , 4-hydroxymethylphenyl claim 7 , 3-methoxymethylphenyl claim 7 , 4-methoxymethylphenyl claim 7 , 3-methoxyethylphenyl claim 7 , 4-methoxyethylphenyl claim 7 , 3-fluorophenyl claim 7 , 4-fluorophenyl claim 7 , 3-[2-(morpolino)ethoxy]phenyl claim 7 , or 4-[2-(morpolino)ethoxy]phenyl.9. The compound or salt of wherein Ris methyl claim 7 , ethyl or isopropyl.10. The compound or salt of wherein Xis O or S.11. The compound or salt of wherein Ris 2-fluoro-2-methylpropyl.13. The compound or salt of claim 7 , wherein a is 1.15. A pharmaceutical composition comprising one or more compounds of and one or more carriers claim 1 , diluents claim 1 , or excipients claim 1 , or a combination thereof.16. A method for treating a patient in need of relieve from an HIV infection claim 1 , the method comprising the step of administering to a patient in need of relief from the HIV infection a therapeutically effective amount of one or more compounds of .17. A pharmaceutical composition comprising one or more compounds of and one or more carriers claim 7 , diluents claim 7 , or excipients claim 7 , or a combination thereof.18. A method for treating a patient in need of relieve from an HIV infection claim 7 , the method comprising the step of administering to a patient in need of relief from the HIV infection a ...

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Номер записи: 45
07-11-2013 дата публикации

CHROMENE DERIVATIVES AND THEIR ANALOGA AS WNT PATHWAY ANTAGONISTS

Номер: US20130296344A1
Автор: Boutros Michael, Fuchs Florian, Gilbert Daniel, Koch Corinna, Maskey Rajendra-Prasad, Steinbrink Sandra
Принадлежит:

Compounds according to the general formula (I) wherein X, X, Xand Xindependently from each other are N or CRwherein Rmay be same or different, and wherein up to 3 of the group X, X, Xand Xmay be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis). 115-. (canceled)19. The method according to wherein A is phenyl substituted by 1 to 5 R which may be same or different and/or solvates; hydrates; and pharmaceutically acceptable salts thereof.20. The method according to wherein the cell proliferation disorder is cancer or a proliferative skin disorder.21. The method according to wherein the cancer is selected from cancers showing an increased level of beta-catenin or beta-catenin target genes in comparison to a normal tissue.22. The method according to wherein the cancer is member of the group multiple myeloma claim 20 , colon cancer claim 20 , breast cancer claim 20 , gastritic cancer claim 20 , colorectal cancer claim 20 , lung cancer claim 20 , prostate cancer claim 20 , ovarian cancer claim 20 , bladder cancer claim 20 , liver cancer claim 20 , uterine cancer claim 20 , kidney cancer claim 20 , leukaemia claim 20 , gliomas claim 20 , basal cell carcinoma claim 20 , rhabdomyosarcoma claim 20 , mesothelioma claim 20 , osteosarcoma claim 20 , medulloblastomas and other primary CNS malignant neuroectodermal tumors.23. A method for modulating the Wnt signalling pathway by using a compound as defined in .24. A pharmaceutical composition containing the ...

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Номер записи: 46
07-11-2013 дата публикации

REACTION PRODUCT FROM THE CO-DEHYDRATION OF A SUGAR ALCOHOL AND A POLYOL

Номер: US20130296451A1
Автор: ABRAHAM Timothy Walter, Ference Donald Michael, ZHANG Wei
Принадлежит: Cargill, Incorporated

A reaction product of the co-dehydration of a sugar alcohol and a reactant polyol having a number average hydroxyl functionality less than 4.0 is disclosed. In some aspects the sugar alcohol comprises mannitol, sorbitol, xylitol, erythritol, or mixtures thereof. In some preferred aspects the sugar alcohol comprises sorbitol. In some aspects the reactant polyol has an average molecular weight of from 40 to 500 Daltons. In some aspects, the reaction product may be suitable for the manufacture of polyisocyanurate foam. In some aspects the reaction product may be mixed with diluent polyols, such as diols, glycols, ethylene glycol, diethylene glycol, dipropylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol and mixtures thereof. 1. A composition comprising the reaction product of the co-dehydration of a sugar alcohol and a reactant polyol having a number average hydroxyl functionality less than 4.0.2. The composition of claim 1 , wherein the sugar alcohol comprises mannitol claim 1 , sorbitol claim 1 , xylitol claim 1 , erythritol claim 1 , or mixtures thereof.3. (canceled)4. The composition of claim 1 , wherein the sugar alcohol comprises sorbitol and the reactant polyol has a number average hydroxyl functionality of from 2.0 to 3.0.5. A composition comprising a reaction product of the acid catalyzed co-dehydration of a sugar alcohol and a polyol claim 1 , wherein the reaction product comprises from about 25 to about 65 weight percent isosorbide claim 1 , and at least 2 percent oligomers.6. The composition of claim 5 , wherein the sugar alcohol comprises sorbitol.78-. (canceled)9. The composition of claim 5 , wherein the reactant polyol has an average molecular weight of from about 50 to about 300 Daltons.10. The composition of claim 5 , wherein the reactant polyol has a molecular weight of from about 60 to about 200 Daltons.11. The composition of claim 5 , wherein the reactant polyol is selected from the group consisting of glycols claim 5 , ...

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Номер записи: 47
07-11-2013 дата публикации

Process For Preparation Of Acetals

Номер: US20130296580A1
Автор: Aduri Pavankumar, RATNAPARKHI Uday, SAKHALKAR Mangesh, UPPARA Parasu Veera
Принадлежит:

A process for the preparation of 1,3:2,4-bis (4-methylbenzylidene) sorbitol (MDBS) and 1,3:2,4-bis (3,4-dimethylbenzylidene) sorbitol (DMDBS) via a dehydrocondensation reaction is disclosed. The reaction is carried out between an aldehyde and an alditol in a mole ratio of 2:1 wherein ionic fluid is used as the acidic catalyst and/or reaction medium. The ionic fluid used in accordance with the present invention is quaternary ammonium salt based ionic liquid. 1. A process for preparation of acetal derivatives selected from the group consisting of DMDBS (1 ,3:2 ,4-bis (3 ,4-dimethylbenzylidene) sorbitol) and MDBS(1 ,3:2 ,4-bis (4-methylbenzylidene) sorbitol) comprising the following steps:preparing a quaternary ammonium salt based ionic fluid;carrying out a dehydrocondensation reaction by adding an aldehyde and an alditol in a mole ratio of 2:1 in the ionic fluid under continuous stirring to form a reaction mixture;stirring the resultant reaction mixture to maintain the contents in a suspension form; anddiscontinuing the stirring of the reaction mixture to allow the mass formed in the reaction mixture to settle and separating the supernatant ionic fluid containing mother liquor;isolating and purifying the mass by filtering, washing and drying to obtain an acetal derivative without any free acid residue present therein.2. A process as claimed in claim 1 , wherein the method step of preparing the ionic fluid comprises forming an in situ ionic compound in a solvent by adding a hydrogen donor and a ‘quaternary ammonium salt’ independently in equimolar quantities to the solvent3. A process as claimed in claim 1 , wherein the ionic fluid is prepared by reacting the equimolar quantities of para-toluene sulfonic acid and choline chloride at a temperature in the range of about 15 to about 65° C.42. A process as claimed in claim 1 , wherein the solvent is at least one selected from the group of carboxylic acids claim 1 , amides claim 1 , alcohols claim 1 , amines claim 1 , ...

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Номер записи: 48
07-11-2013 дата публикации

Process For The Preparation of Alditol Acetals

Номер: US20130296581A1
Автор: Aduri Pavankumar, UPPARA Parasu Veera
Принадлежит:

The present invention is directed to a process for the preparation of 1,3:2,4-bis (4-methylbenzylidene) sorbitol (MDBS) and 1,3:2,4-bis (4-dimethylbenzylidene) sorbitol (DMDBS) by dehydrocondensating an aldehyde and an alditol using a hydrophobic ionic liquid as an acid catalyst. The ionic liquid used in the accordance with the process of the present invention is a phosphonium ion based ionic liquid. 1. A process for preparation of acetal derivatives particularly , DMDBS and MDBS by dehydrocondensation reaction between an aldehyde and alditol which comprises the following steps:dehydrocondensating an aldehyde and an alditol dissolved in a solvent by the addition of ionic liquid which acts as a catalyst under continuous stiffing at a temperature of about 25° C. to about 80° C. to obtain a reaction mixture;subjecting the reaction mixture to filtration to obtain a solid mass and a mother liquor containing the solvent and ionic liquid; andpurifying the solid mass by washing and drying to obtain an acetal derivative without any free acid residue present therein.2. A process for preparation of acetal derivatives selected from the group consisting of DMDBS (1 ,3:2 ,4-bis (3 ,4-dimethylbenzylidene) sorbitol) and MDBS (1 ,3:2 ,4-bis (4-methylbenzylidene) sorbitol) comprising the following steps:dehydrocondensating an aldehyde and an alditol dissolved in an ionic liquid which acts as a catalyst under continuous stirring at a temperature of about 25° C. to about 80° C. to obtain a reaction mixture;subjecting the reaction mixture to filtration to obtain a solid mass and a biphasic mixture of mother liquor and water;removing water from the biphasic mixture to obtain the mother liquor; andpurifying the solid mass by washing and drying to obtain an acetal derivative without any free acid residue present therein.3. A process as claimed in claim 1 , wherein the ionic liquid acts as an acid catalyst.4. A process as claimed in claim 1 , wherein the solvent is at least one solvent ...

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Номер записи: 49
07-11-2013 дата публикации

Production of 5-Membered and 6-Membered Cyclic Esters of Polyols

Номер: US20130296584A1
Автор: Howard Stephen, Sanborn Alexandra
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

Described herein are improved methods for the preparation of 5- and 6-membered cyclic mono and diesters of sugar alcohols and anhydrosugar alcohols by reaction with an organic acid RCOOH over a solid acidic substrate. The process is adaptable to a continuous process for simultaneously making and separating the cyclic esters from the sugar alcohols and anhydrosugar alcohols under mild conditions using the solid acid substrate as both the catalyst and a chromatographic bed for separation. The reactions are performed at mild temperatures of 70° C. to 100° C. and the formation of the cyclic esters is nearly quantitative. Also described is a method for making 5- and 6-membered cyclic mono and diesters of sugar alcohols and anhydrosugar alcohols using microwave irradiation in the presence of the organic acid. 1. A method of preparing cyclic esters from 5 or 6 carbon compounds comprising , contacting a column bed containing a solid acid catalyst with at least one starting 5 or 6 carbon compound selected from the group consisting of a sugar alcohol , a monoanhydrosugar alcohol , and a dianhydrosugar alcohol in the presence of an organic acid in a single step reaction under a single set of reaction conditions for a time sufficient to form at least one of a cyclic monoester and cyclic diester derivative of at least one of the monoanhydrosugar alcohol and a dianhydrosugar alcohol.2. The method of claim 1 , wherein the bed is configured in a simulated moving bed apparatus.3. The method of claim 1 , wherein the organic acid is acetic acid.4. The method of claim 1 , wherein the starting 5 or 6 carbon compound is selected from group consisting of sorbitol claim 1 , isosorbide and sorbitan.5. The method of claim 1 , wherein the starting 5 or 6 carbon compound is selected from the group consisting of arabinitol claim 1 , ribitol claim 1 , sorbitol claim 1 , mannitol claim 1 , isomannide claim 1 , galactitol claim 1 , iditol and xylitol.6. The method of claim 1 , wherein the solid ...

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Номер записи: 50
14-11-2013 дата публикации

Oxabicycloheptanes and oxabicycloheptenes, their preparation and use

Номер: US20130302402A1
Автор: Francis Johnson, John S. Kovach
Принадлежит: Lixte Biotechnology Inc

This invention provides compounds having the structure which may be used for the treatment of tumors.

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Номер записи: 51
14-11-2013 дата публикации

Acid-Labile Lipophilic Prodrugs of Cancer Chemotherapeutic Agents

Номер: US20130303601A1
Автор: Gundluru Mahesh Kumar, Henri John T., McChesney James D., Venkataraman Sylesh Kumar
Принадлежит:

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof. 117-. (canceled)29. A pharmaceutical composition comprising: a) a therapeutically effective amount of a compound of claim 18 , in the form of a single diastereoisomer; and b) a pharmaceutically acceptable excipient.30. A method for the treatment of cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound or composition of claim 18 , to a patient in need of such treatment.31. The method of claim 30 , wherein the cancer is selected from the group consisting of leukemia claim 30 , neuroblastoma claim 30 , glioblastoma claim 30 , cervical claim 30 , colorectal claim 30 , pancreatic claim 30 , renal and melanoma.32. The method of claim 30 , wherein the cancer is selected from the group consisting of lung claim 30 , breast claim 30 , prostate claim 30 , ovarian and head and neck.34. The method of claim 33 , wherein the method provides a higher concentration of the cancer chemotherapeutic agent in a cancer cell of the patient. This application claims the benefit of U.S. Provisional Application No. 61/493,827 filed Jun. 6, 2011 and U.S. Provisional Application No. 61/496,367 filed Jun. 13, 2011, the full contents of which are incorporated herein by reference.The present invention generally relates to chemical compounds and methods for use in treating patients. More particularly, the present invention is directed to molecular conjugates for use in cancer treatment. Specifically, the present invention relates to acid-labile, lipophilic conjugates, methods and intermediates useful in the formation thereof, and methods for treating a patient therewith.A number of anti-cancer drug are currently in the market for the treatment of ...

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Номер записи: 52
14-11-2013 дата публикации

NOVEL PTEROCARPAN COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF METABOLIC DISEASE OR COMPLICATION THEREOF, OR FOR ANTIOXIDANT CONTAINING THE SAME AS AN ACTIVE INGREDIENT

Номер: US20130303602A1
Автор: JEONG Tae-Sook, PARK Ho-Yong, PARK Ki Hun
Принадлежит: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND TECHNOLOGY

The present invention relates to novel pterocarpan compound or pharmaceutically acceptable salt thereof and a composition for the prevention or treatment of metabolic disease or complications thereof comprising the same as an active ingredient. The novel pterocarpan compound of the present invention isolated from soybean leaves inhibits α-glucosidase activity and hACAT activity, and suppresses LDL-oxidation efficiently. Therefore, the compound of the present invention not only can be effectively used for the prevention or treatment of metabolic disease or complications thereof but also can be effectively used as an anti-oxidative composition owing to its excellent anti-oxidative activity. 2. The novel pterocarpan compound according to claim 1 , wherein the is single bond or double bond;{'sup': '2', 'Ris hydrogen or isobutenyl group;'}{'sup': 2', '3', '2', '3, 'Ris hydroxyl group, and Ris hydrogen or isobutenyl group, or Rand Rcan form furan ring with carbon atoms conjugated with them, and at this time the furan ring is non-replaceable or can be replaced with isopropenyl group;'}{'sup': '4', 'Ris hydrogen or methoxy group;'}{'sup': '5', 'Ris hydrogen or ═O;'}{'sup': '6', 'Ris hydrogen or hydroxyl group; and'}{'sup': '7', 'Ris hydrogen or methyl group.'}4. A pharmaceutical composition for the prevention or treatment of metabolic disease or complications thereof containing the pterocarpan compound represented by Formula 1 or the pharmaceutically acceptable salt thereof of as an active ingredient.5. The pharmaceutical composition for the prevention or treatment of metabolic disease of complications thereof according to claim 4 , wherein the metabolic disease is selected from the group consisting of diabetes claim 4 , hyperlipidemia claim 4 , atherosclerosis claim 4 , fatty liver claim 4 , and obesity; and the complication is selected from the group consisting of coronary artery disease claim 4 , angina pectoris claim 4 , carotid artery disease claim 4 , stroke claim 4 , ...

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Номер записи: 53
14-11-2013 дата публикации

Process For Preparing Alditol Acetals

Номер: US20130303787A1
Автор: Aduri Pavankumar, RATNAPARKHI Uday, SAKHALKAR Mangesh, UPPARA Parasu Veera
Принадлежит:

A process for preparing alditol Acetals via a dehydrocondensation reaction is disclosed. The reaction is carried out by adding an aldehyde and an aldiol using a metal salt based ionic liquid as an acid catalyst. The ionic liquid used in the process is prepared by dissolving a hydrogen donor and a compound providing counter ion in a solvent. 1. A process for preparation of acetal derivatives selected from the group consisting of 1 ,3:2 ,4-bis(4-methylbenzylidene) sorbitol (MDBS) and 1 ,3:2 ,4-bis(3 ,4-dimethylbenzylidene) sorbitol (DMDBS) comprising the following steps: carrying out the dehydrocondensation reaction by adding an aldehyde and an alditol in a mole ratio of 2:1 in the ionic fluid under continuous stirring to form a reaction mixture;', 'stirring the resultant reaction mixture to maintain the contents in a suspension form; and', 'discontinuing the stirring of the reaction mixture to allow the mass formed in the reaction mixture to settle;', 'isolating and purifying the mass by subjecting the reaction mixture to filtration, to obtain a mother liquor containing the ionic fluid, unconverted reactants and the solid mass;', 'washing and drying the solid mass to obtain an acetal derivative without any free acid residue present therein., 'preparing a metal salt based ionic fluid selected from a fluid containing an in situ formed ionic compound by dissolving a hydrogen donor and a counter ion providing compound in a solvent and a fluid prepared by heating a hydrogen donor and a counter ion providing compound'}2. A process as claimed in claim 1 , wherein the ionic fluid acts as an acid catalyst for the dehydrocondensation reaction.3. A process as claimed in claim 1 , wherein the ionic fluid acts as a reaction medium for the dehydrocondensation reaction.4. A process as claimed in claim 1 , wherein the metal salt based ionic fluid is prepared by mixing the equimolar quantities of the hydrogen donor and the counter ion providing compound in the solvent.5. A process as ...

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Номер записи: 54
14-11-2013 дата публикации

Pseudopolymorphic Forms Of A HIV Protease Inhibitor

Номер: US20130303790A1
Автор: Janssens Luc Donne Marie-Louise, Thone Daniel Joseph Christiaan, VERMEERSCH Hans Wim Pieter, Wigerinck Piet Tom Bert Paul
Принадлежит:

New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed. 114-. (canceled)15. An ethanolate solvate of the compound (3R ,3aS ,6aR)-hexahydrofuro[2 ,3-b]furan-3-yl(1S ,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate , in which the ratio of compound to ethanol is about 1:1. This invention relates to novel pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate, a method for their preparation as well as their use as a medicament.Virus-encoded proteases, which are essential for viral replication, are required for the processing of viral protein precursors. Interference with the processing of protein precursors inhibits the formation of infectious virions. Accordingly, inhibitors of viral proteases may be used to prevent or treat chronic and acute viral infections. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate has HIV protease inhibitory activity and is particularly well suited for inhibiting HIV-1 and HIV-2 viruses.The structure of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate, is shown below:Compound of formula (X) and processes for its preparation are disclosed in EP 715618, WO 99/67417, U.S. Pat. No. 6,248,775, and in , Vol. 8, pp. 687-690, 1998, “Potent HIV protease inhibitors incorporating high-affinity P-igands and (R)-(hydroxyethylamino)sulfonamide isostere”, all of which are incorporated herein by reference.Drugs utilized in the preparation of pharmaceutical formulations for commercial use must meet certain standards, including GMP (Good Manufacturing Practices) and ICH (International Conference on Harmonization) ...

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Номер записи: 55
28-11-2013 дата публикации

SINGLETON INHIBITORS OF SUMOYLATION ENZYMES AND METHODS FOR THEIR USE

Номер: US20130317101A1
Автор: Bobkova Ekaterina, Chen Yuan, Divlianska Daniela, Li Yi-Jia, Roth Greg
Принадлежит:

According to the embodiments described herein, a SUMOylation inhibitor compound comprising a singleton scaffold is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a singleton SUMOylation inhibitor compound. In some embodiments, the method for treating a cancer may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition. 11. The method of claim 6 , wherein the SUMOylation enzyme is SUMO E1 or SUMO E2.12. The method of claim 6 , wherein the cell is part of an in vivo population of cells in a subject.13. The method of claim 12 , wherein the population of cells is a tumor claim 12 , a population of virally infected cells claim 12 , a population of cells associated with heart disease claim 12 , a population of cells associated with a degenerative disease claim 12 , or a population of cells associated with a genetic disease.14. The method of claim 6 , wherein the cell is part of a population of cells grown in culture.15. The method of claim 14 , wherein the cell is part of a primary cell line claim 14 , a secondary cell line or an immortal cell line.16. The method of claim 15 , wherein the cell line is derived from a tumor claim 15 , a degenerative disease claim 15 , a genetic disease or a cardiovascular disease.18. The method of claim 17 , wherein the disease is a cancer claim 17 ...

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Номер записи: 56
05-12-2013 дата публикации

INHIBITORS OF FLAVIVIRIDAE VIRUSES

Номер: US20130323203A1
Автор: "Clarke Michael ONeil Hanrahan", Belmont Michael Mertzman, Canales Eda, Chong Lee S., Doerffler Edward, Lazerwith Scott E., Lew Willard, Morganelli Philip Anthony, Watkins William J.
Принадлежит: Gilead Sciences, Inc.

Provided are compounds of Formula I: 121.-. (canceled)23. The compound of claim 22 , wherein Ris optionally substituted C-Csecondary or tertiary alkyl.24. The compound of claim 22 , wherein Ris optionally substituted methylcyclohexyl or optionally substituted methylcyclohexenyl.28. The compound of claim 22 , wherein Y is —R-L-Het.29. The compound of claim 28 , wherein Ris selected from the group consisting of optionally substituted Calkylene claim 28 , Ccycloalkylene claim 28 , and 5-6 membered heterocyclylene.30. The compound of wherein Het is selected from the group consisting of optionally substituted pyridinyl claim 28 , optionally substituted pyridazinyl claim 28 , optionally substituted tetrahydro-2H-pyranyl claim 28 , optionally substituted piperidinyl claim 28 , optionally substituted pyrrolidinyl claim 28 , optionally substituted tetrahydrothiophenyl claim 28 , optionally substituted pyrazinyl claim 28 , optionally substituted 1H-tetrazolyl claim 28 , optionally substituted azetidinyl claim 28 , optionally substituted tetrahydrofuranyl claim 28 , optionally substituted tetrahydro-2H-furo[2 claim 28 ,3-b]furanyl claim 28 , optionally substituted thiazoyl claim 28 , optionally substituted 1H-imidazolyl claim 28 , optionally substituted 4H-1 claim 28 ,2 claim 28 ,4-triazolyl claim 28 , optionally substituted 1H-pyrazolyl claim 28 , optionally substituted 1 claim 28 ,3 claim 28 ,4-thiadiazolyl claim 28 , optionally substituted quinolinyl claim 28 , optionally substituted [1 claim 28 ,2 claim 28 ,4]triazolo[4 claim 28 ,3-a]pyridinyl claim 28 , optionally substituted thiophenyl claim 28 , optionally substituted 1 claim 28 ,2 claim 28 ,4-thiadiazolyl claim 28 , optionally substituted pyrimidinyl claim 28 , optionally substituted 1H-1 claim 28 ,2 claim 28 ,3-triazolyl claim 28 , optionally substituted 1 claim 28 ,3 claim 28 ,4-oxadiazolyl claim 28 , and optionally substituted imidazo[1 claim 28 ,2-b]pyridazinyl.31. The compound of wherein Y is —N(R)(R).32. The ...

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Номер записи: 57
12-12-2013 дата публикации

PROCESS FOR THE DIRECT AMINATION OF ALCOHOLS USING AMMONIA TO FORM PRIMARY AMINES BY MEANS OF A XANTPHOS CATALYST SYSTEM

Номер: US20130331580A1
Автор: Beller Matthias, Deutsch Jens, Haas Thomas, Haberland Juergen, Imm Sebastian, Klasovsky Florian, Koeckritz Angela, Martin Andreas, Pfeffer Jan Christoph, Tacke Thomas
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand. 2. The process according to claim 1 ,wherein{'sup': 1', '2', '3', '4, 'sub': 3', '2, 'R=R=R=R=phenyl, and A=—C(CH)—.'}3. The process according to claim 1 ,whereinthe xantphos ligand is carbonylchlorohydrido[9,9-dimethyl-4,5-bis(diphenylphosphino)xantheno]ruthenium(II)].4. The process according to claim 1 ,whereinthe alcohol is an aliphatic, linear ω-hydroxycarboxylic acid having a carbon chain comprising at least 8 carbon atoms.5. The process according to claim 1 ,whereinthe alcohol has a concentration of from 0.1 to 1000 mmol/l, based on the fluid phase.6. The process according to claim 1 ,wherein the contacting comprises contacting with liquid or supercritical ammonia, with a solution of ammonium salts in a solvent, or both.7. The process according to claim 1 ,wherein in the contacting,the ammonia has a molar ratio to hydroxyl groups in the alcohol of at least 5:1.8. The process according to claim 1 ,wherein the contacting is carried out at a pressure of from 1 to 1000 bar.9. The process according to claim 1 ,wherein the contacting is carried out in a temperature range of from 80 to 220° C.10. The process according to claim 1 ,whereina volume ratio of a liquid phase to a gas phase in the contacting is greater than or equal to 0.05.11. The process according to claim 1 ,wherein the process is carried out in an absence of hydrogen.12. The process according to claim 1 , wherein the alcohol has a concentration of from 0.1 to 100 mmol/l based on the fluid phase.13. The process according to claim 1 , wherein the alcohol has a concentration of from 0.1 to 10 mmol/l based on the fluid phase.14. The process according to claim 1 , wherein in the contacting claim 1 , the ammonia has a molar ratio to hydroxyl ...

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Номер записи: 58
19-12-2013 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING SUBSTITUTED HEXAHYDROFURO [2,3-b] FURANS

Номер: US20130338380A1
Автор: Ghosh Arun K., Martyr Cuthbert D.
Принадлежит: PURDUE RESEARCH FOUNDATION

The invention described herein pertains to processes and compounds useful in the preparation of bis-tetrahydrofurans. The invention described herein also pertains to compounds useful for treating HIV infections. 2. (canceled)5. (canceled)16. The process of wherein the base is a lithium alkoxide claim 1 , a sodium alkoxide claim 1 , a potassium alkoxide claim 1 , a lithium amide claim 1 , a sodium amide claim 1 , a magnesium amide claim 1 , or a potassium amide.17. The process of wherein the inverting step includes converting the free hydroxyl to an ester of a carboxylic acid.18. The process of wherein the reducing agent is selected from the group consisting of a lithium hydridoaluminate and a sodium hydridoaluminate.19. The process of wherein the reducing agent is lithium aluminum hydride or sodium bis(2-methoxyethoxo)-dihydridoaluminate.20. The process of wherein the base is potassium t-butoxide claim 1 , sodium t-amyloxide claim 1 , or lithium hexamethyldisilazide.21. The process of wherein the oxidizing agent is selected from the group consisting of ozone claim 1 , NaIO—RuO claim 1 , and NaIO—OsO.22. The process of wherein the oxidizing agent is ozone.23. (canceled)25. (canceled)27. The process of wherein n is 0.29. The process of wherein n is 0. This application claims the benefit under 35 USC §119(e) of U.S. Provisional Application Ser. No. 61/418,123 filed on Nov. 30, 2010, the entire disclosure of which is incorporated herein by reference.The invention described herein pertains to processes and compounds useful in the preparation of bis-tetrahydrofurans. The invention described herein also pertains to compounds useful for treating HIV infections.In recent years, the bis-tetrahydrofuranyl ligand has become an important ligand in the design of HIV-protease inhibitors. Since its discovery, it has been the salient feature in many drug candidates. Darunavir, (1), the first FDA approved second generation protease inhibitor, is currently being used in the treatment ...

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Номер записи: 59
19-12-2013 дата публикации

Crude Reaction Product Comprising Dianhydro Sugar Alcohol and Method for Preparing the Same

Номер: US20130338381A1
Автор: Man Suk Kim, Sang Hyun Hong, Sun Dae Kim, Sung Hee Ahn
Принадлежит: Cheil Industries Inc

A crude reaction product includes: (A) about 90 to 100% by weight of a dianhydro sugar alcohol in a solid form and (B) about 0 to about 10% by weight of a reaction byproduct in a solid form. The reaction product is prepared by the steps of (a) preparing a monoanhydro sugar alcohol by reacting a sugar alcohol in the presence of a first cyclization catalyst and (b) preparing a dianhydro sugar alcohol by reacting the monoanhydro sugar alcohol in the presence of a second catalyst.

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Номер записи: 60
26-12-2013 дата публикации

Imide compound, method for producing same, thickening agent for grease, and grease composition

Номер: US20130345102A1
Автор: Kentaro Yamaguchi, Miki Fujiwara, Osamu Kurosawa, Ryuichi Ueno
Принадлежит: JX Nippon Oil and Energy Corp

The present invention provides an imide compound represented by the following general formula (1). The imide compound of the present invention, particularly when used as a thickening agent for grease, is excellent in durability at high temperatures. [wherein X represents a tetravalent residue obtained by removing four carboxylic groups from an aromatic tetracarboxylic acid, Y represents a divalent residue obtained by removing two amino groups from an aliphatic diamine or an aromatic diamine, and R represents a residue obtained by removing an amino group from an aliphatic monoamine, an alicyclic monoamine, or an aromatic monoamine.]

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Номер записи: 61
02-01-2014 дата публикации

NOVEL HERBICIDES

Номер: US20140005389A1
Автор: Mathews Christopher John, Muehlebach Michel, Scutt James Nicholas
Принадлежит: SYNGENTA CROP PROTECTION LLC

Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides. 2. A compound according to claim 1 , wherein Ris halogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Calkenyl or C-Calkynyl.3. A compound according to claim 1 , wherein Ris hydrogen claim 1 , which means that r is 0 claim 1 , or Ris halogen or C-Calkyl.4. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand R claim 1 , independently of each other claim 1 , are hydrogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-CalkoxyC-Calkyl claim 1 , C-CalkylthioC-Calkyl claim 1 , C-CalkylsulfinylC-Calkyl claim 1 , C-CalkylsulfonylC-Calkyl; C-Ccycloalkyl or C-Ccycloalkyl substituted by C- or Calkyl or C- or Chaloalkyl and in which a methylene group is optionally replaced by an oxygen or sulfur atom or a sulfinyl or sulfonyl group; C-CcycloalkylC-Calkyl or C-CcycloalkylC-Calkyl substituted by C-Calkyl or C- or Chaloalkyl and in which a methylene group is optionally replaced by an oxygen or sulfur atom or a sulfinyl or sulfonyl group.5. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand R claim 1 , independently of each other claim 1 , are hydrogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl or C-Calkoxy-C-Calkyl.6. A compound according to claim 1 , wherein Y is O claim 1 , S or C═O.7. A compound according to claim 1 , wherein{'sup': 1', '3', '4', '5', '6', '7, 'sub': 1', '4', '1', '2, 'Ris C-Calkyl; Ris hydrogen, which means that r is 0; R, R, Rand R, independently of each other, are C-Calkyl; and Y is O.'} This application is a divisional of application Ser. No. 12/519,015, which is a 371 of International Application No. PCT/EP2007/010848 filed Dec. 12, 2007, which claims priority to GB 0624961.9 filed Dec. 14, 2006, and GB 0705044.6 filed on Mar. 15, 2007, the contents of which are incorporated herein by reference.The present invention relates to novel, herbicidally active cyclic diones, and derivatives thereof, to ...

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Номер записи: 62
02-01-2014 дата публикации

Synthetic transtaganolide and basiliolide products, derivatives thereof, and synthesis methods thereof

Номер: US20140005416A1
Автор: Brian M. Stoltz, Hosea Nelson, Jonathan R. Gordon, Kei Murakami, Scott C. Virgil
Принадлежит: California Institute of Technology CalTech

Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.

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Номер записи: 63
16-01-2014 дата публикации

GAMMA SECRETASE INHIBITORS

Номер: US20140018342A1
Автор: Burnett Duane A., Greenlee William J., Wu Wen-Lian
Принадлежит:

Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease. 3. The compound of claim 2 , wherein the halogen is fluoro.4. The compound of claim 3 , wherein Ar is selected from the group consisting of{'sub': 3', '3', '1', '6, 'p-Cl-phenyl-, p-CN-phenyl-, p-CF-phenyl, pyridyl, and pyridyl substituted with 1 or 2 substituents independently selected from the group consisting of halogen, —(C1-C6)alkyl, —CN, —CF, —O—(C1-C6)alkyl, —O-halo(C1-C6)alkyl, —C(O)—O—(C1-C6)alkyl, —OH-substituted (C1-C6)allyl, -halo(C-C)alkyl, —OH substituted (C1-C4)alkoxy and (C1-C4)alkoxy(C1-C4)alkoxy.'}5. The compound of claim 4 , wherein Ar is selected from the group consisting of p-Cl-phenyl- and p-CF-phenyl.6. The compound of claim 1 , wherein R is —(C1-C3)alkyl-R.7. The compound of claim 6 , wherein Ris —C(O)NH.8. The compound of claim 1 , wherein the (C3-C5)heterocycloalkyl of Rand Ris selected from the group consisting of piperidyl claim 1 , pyrrolidinyl claim 1 , piperazinyl claim 1 , morpholinyl claim 1 , thiomorpholinyl claim 1 , thiazolidinyl claim 1 , oxazolidinyl claim 1 , azetidinyl claim 1 , tetrahydrofuranyl claim 1 , tetrahydropyran claim 1 , oxetin claim 1 , imidazolinyl and tetrahydrothiophenyl.11. The compound of claim 10 , wherein R is —(C1-C3)alkyl-Rand Ris C(O)NH.12. The compound of claim 1 , selected from the group consisting of compounds 6a-6t claim 1 , 9a-9e claim 1 , 24a-24c claim 1 , 26e-26i claim 1 , 27a-27g claim 1 , 31b-31e claim 1 , 32-34 claim 1 , 36 claim 1 , 39a-39g claim 1 , 43a-43c claim 1 , 45 claim 1 , 46a-46d claim 1 , 47 claim 1 , 51a-51d claim 1 , 56a-56f claim 1 , 63c-63e claim 1 , 64a-64d claim 1 , 75 claim 1 , 76a claim 1 ...

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Номер записи: 64
23-01-2014 дата публикации

COMPOUNDS WITH SUPER-ASPIRIN EFFECTS

Номер: US20140024681A1
Автор: "Olynn Pat", Gilmer John Francis, Harmon Shona, Ledwidge Mark, Martin Carlos Medina, Radomski Mark
Принадлежит:

A compound having the structural formula (I) and pharmaceutically acceptable salt and/or hydrates thereof, (I) wherein Y is an arylester or an C-Calkylaryl ester, selected from the group consisting of: benzene, toluene, xylene, benzoic acid, benzoate, nicotinate, isonicotinate and halobenzene, which can be unsubstituted or substituted with at least one nitric oxide releasing group; and/or at least one of hydroxide, —Cl, —Br, a C-Calkyl, benzyl, a C-Calkoxy, benzyloxy, —NHC(O)R, —NH, —NO—ONO, —(CH)ONO, —OC(O)[(CH)]ONO, —OCOArONO, —OCOAr(CH)ONOor a C-Chaloalkyl ester, wherein R is a C-Calkyl or a C-Calkoxy group, n=1-8 and m=3-10, to produce a super-aspirin effect. 2. (canceled)3. The method of claim 1 , wherein the cancer metastasis involving tumor cell induced platelet aggregation (TCIPA) is associated with malignant mesothelioma claim 1 , gynecological malignancies claim 1 , lung claim 1 , renal claim 1 , gastric claim 1 , ovarian claim 1 , colon claim 1 , colorectal claim 1 , breast tumors or other solid tumor types.4. The method of claim 1 , wherein the CVD is coronary heart disease claim 1 , cardiomyopathy claim 1 , cardiovascular disease claim 1 , ischaemic heart disease claim 1 , heart failure claim 1 , hypertensive heart disease claim 1 , inflammatory heart disease claim 1 , valvular heart disease claim 1 , myocardial Infarction or other associated conditions caused by these CVD types.5. (canceled)6. The method of claim 1 , wherein the nitric oxide release group of the compound is a nitrate ester claim 1 , a Cto Calkyl nitrate ester claim 1 , a C-Ccycloalkyl nitrate ester or a C-Calkyl nitrate ester.7. The method of wherein the nitric oxide release group is selected from the group consisting of: —NO claim 6 , —ONO claim 6 , —(CH)ONO claim 6 , —OC(O)[(CH)]ONO claim 6 , —OCOArONO claim 6 , —OCOAr(CH)ONO.8. The method of claim 1 , wherein the arylester or the alkylaryl ester of the compound is substituted at the 2- or 3-position of the aryl ring.9. The method of ...

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Номер записи: 65
23-01-2014 дата публикации

PROCESS FOR THE HOMOGENEOUSLY CATALYZED AMINATION OF ALCOHOLS WITH AMMONIA IN THE PRESENCE OF A COMPLEX CATALYST WHICH COMPRISES NO ANIONIC LIGANDS

Номер: US20140024833A1
Автор: Brinks Marion, Melder Johann-Peter, Merger Martin, Paciello Rocco, Schaub Thomas, SCHELWIES Mathias
Принадлежит: BASF SE

The invention relates to a process for preparing primary amines by alcohol amination of alcohols with ammonia with the elimination of water, where the alcohol amination is carried out under homogeneous catalysis in the presence of at least one complex catalyst which comprises ruthenium and at least one at least bidental donor ligand, but no anionic ligands. 1. A process for preparing a primary amine , the process comprising performing alcohol amination of an alcohol with ammonia and elimination of water under homogeneous catalysis in the presence of a complex catalyst comprising ruthenium and an at least bidental donor ligand , but no anionic ligands.6. The process according to claim 2 , wherein Rand Rare unsubstituted cyclohexyl.8. The process according to claim 2 , wherein n=0 in the complex catalyst.9. The process according to claim 1 , where the alcohol has a primary or secondary alkyl group.10. The process according to claim 1 , where the primary amine is a monoamine claim 1 , an alkanolamine claim 1 , a diamine claim 1 , a triamine claim 1 , or a polyamine.11. The process according to claim 1 , where the alcohol has at least two secondary alcohol groups.12. The process according to claim 1 , where the alcohol is selected from the group consisting of isosorbide claim 1 , isomannide claim 1 , isoidide and a mixture thereof.14. The process according to claim 13 , where the ruthenium-comprising catalyst precursor is selected from the group consisting of [Ru(CO)] claim 13 , [Ru(CO)(ethylene)] claim 13 , [Ru(COD)(OAc)] claim 13 , [Ru(COD)(2-methylallyl)] claim 13 , [Ru(CO)Cl] claim 13 , [Ru(CO)Cl] claim 13 , [RuCl*HO] claim 13 , [Ru(acetylacetonate)] claim 13 , [Ru(PPh)(CO)(H)Cl] claim 13 , [Ru(PPh)(CO)Cl] claim 13 , [Ru(PPh)(CO)(H)] claim 13 , [Ru(PPh)Cl] and [Ru(COD)Cl]. This patent application claims the benefit of pending U.S. provisional patent application Ser. No. 61/674,423 filed on Jul. 23, 2012, incorporated in its entirety herein by reference.The present ...

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Номер записи: 66
30-01-2014 дата публикации

PYRAZOLE COMPOUND

Номер: US20140031406A1
Автор: NATSUTANI Itaru, SASAKI Izumi, TAKAHASHI Yoko, TOYODA Tomohiro, YOSHINAGA Hidefumi
Принадлежит: DAINIPPON SUMITOMO PHARMA CO., LTD.

The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HTantagonistic action (antidepressive and anxiolytic effects), in particular, 5-HTinverse agonistic action comprising Compound (1): 117-. (canceled)19. The method of wherein the disease is (i) depression or (ii) anxiety.20. The method of wherein the disease is (i) depressive disorders such as major depressive disorder claim 18 , dysthymic disorder claim 18 , and depressive disorders not otherwise specified claim 18 , (ii) depression claim 18 , (iii) seasonal affective disorder claim 18 , or (iv) major depressive episode in bipolar disorder.21. The method of wherein the disease is (i) panic disorder claim 18 , (ii) obsessive-compulsive disorder claim 18 , (iii) posttraumatic stress disorder claim 18 , (iv) acute stress disorder claim 18 , (v) generalized anxiety disorder claim 18 , (vi) anxiety disorder due to a general medical condition claim 18 , (vii) anxiety disorder comprising substance-induced anxiety disorder claim 18 , (viii) agoraphobia claim 18 , (ix) social phobia claim 18 , (x) avoidant personality disorder claim 18 , or (xi) psychophysiological disorder.22. The method of wherein the disease is a symptom of depression or anxiety associated with schizophrenia or dementia.23. The method of wherein the disease is (i) memory impairment claim 18 , (ii) eating behavior disorder claim 18 , (iii) obesity claim 18 , (iv) sleep disorder claim 18 , (v) schizophrenia claim 18 , (vi) addiction to drugs claim 18 , (vii) cluster headache claim 18 , (viii) migraine claim 18 , (ix) pain claim 18 , (x) Alzheimer's disease claim 18 , (xi) chronic paroxysmal hemicrania claim 18 , (xii) headache associated with vascular disorder claim 18 , (xiii) Parkinson's disease claim 18 , (xiv) endocrine abnormality claim 18 , (xv) vasospasm claim 18 , (xvi) hypertension claim 18 , (xvii) gastrointestinal disorder associated with motility and secretory change claim 18 , or (xviii) sexual ...

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Номер записи: 67
06-02-2014 дата публикации

Pharmaceutical composition for treating aging-associated diseases, containing progerin expression inhibitor as active ingredient, and screening method of said progerin expression inhibitor

Номер: US20140039010A1
Автор: Bum Joon Park, Gyu Yong Song, Ji Hyun Lee, Nam Chul Ha, Su Jin Lee, Youn Sang Jung
Принадлежит: University Industry Cooperation Foundation of Pusan National University

Disclosed are a method for treating an aging-related disease and a method for screening a therapeutic agent for an aging-related disease. The method for treating an aging-related disease includes administering to a subject a progerin expression inhibitor as an active ingredient. The method for screening a therapeutic agent for an aging-related disease includes selecting a candidate drug inhibitory of progerin expression.

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Номер записи: 68
06-02-2014 дата публикации

COMPOSITION OF MONOTERPENOIDS HAVING BACTERICIDAL PROPERTIES

Номер: US20140039045A1
Автор: Reynolds Max
Принадлежит:

A composition having bactericidal properties comprising; (a) 30%-80% of at least one compound having the formula (I) and (b) 10% to 40% of at least one compound of formula (II) 2. The composition of claim 1 , wherein the at least one compound of formula 1 is selected from the group consisting of ∝-terpineol claim 1 , β-terpineol claim 1 , γ-terpineol terpinene-4-ol claim 1 , thymol claim 1 , carvacrol claim 1 , carveol claim 1 , perillyl alcohol claim 1 , isopulegol claim 1 , limonene-10-ol claim 1 , and dihydrocarveol.3. The composition of claim 1 , wherein the at least one compound of formula 1 is terpinene-4-ol.4. The composition of claim 3 , wherein the composition comprises from 40% to 70% terpinene-4-ol.5. The composition of claim 1 , having at least two compounds of formula 1.6. The composition of claim 5 , wherein there compounds of formula 1 consist essentially of terpinene-4-ol and ∝-terpineol.7. The composition of comprising between about 40 and about 70% terpinene-4-ol and about 4 to about 15% terpinene-4-ol.9. The composition of claim 1 , wherein the composition comprises at between about 10% to about 40% claim 1 , preferably between about 15% to about 35% claim 1 , preferably between about 20% to about 30% of at least one compound of formula 2.10. The composition of claim 9 , wherein the composition comprises at least two compounds of formula 2 claim 9 , and at least one compound has 2 oxygen atoms and at least one compound has three oxygen atoms claim 9 , wherein the ratio of the at least one compound having two oxygen atoms to the at least one compound having three oxygen atoms is between about 1:1 to 5:1 claim 9 , preferably between about 1.5:1 to about 4:1 claim 9 , most preferably between about 2:1 to about 3:1.11. The composition of claim 9 , wherein the at least one compound of formula 2 comprises between about 1 to about 4% claim 9 , preferably between about 2 to about 3% 2-hydroxy-1 claim 9 ,4-cineole; between about 5% to about 15% claim 9 , ...

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Номер записи: 69
27-02-2014 дата публикации

Derivatives of englerin for the treatment of cancer

Номер: US20140057950A1
Автор: Herbert Waldmann, Hongyan Sun, Lea Radtke, Mathias Christmann, Matthieu Willot, Slava Ziegler
Принадлежит: Max Planck Gesellschaft zur Foerderung der Wissenschaften eV

The present invention relates to compounds of the general formula (I) which show a specific activity against cancer cell lines, the use of these compounds for prophylaxis and treatment of cancer as well as to pharmaceutical compositions containing at least one compound of general formula (I).

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Номер записи: 70
06-03-2014 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: C-17 HOMOLOGATED OLEANOLIC ACID DERIVATIVES

Номер: US20140066408A1
Автор: GREINER Jack, Jiang Xin, LIU Xiaofeng, SZUCS Stephen S., Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 614-. (canceled)15. The compound of claim 5 , wherein Y is alkanediylor substituted alkanediyl.1618-. (canceled)19. The compound of claim 5 , wherein Xis ORand Ris absent.20. The compound of claim 4 , wherein Xis hydrogen.21. The compound of claim 5 , wherein Ris —OH.2228-. (canceled)29. The compound of claim 5 , wherein Ris acylor substituted acyl.30. The compound of claim 29 , wherein Ris selected from the group consisting of —C(═O)OH claim 29 , —C(═O)OCH claim 29 , —C(═O)NHCH claim 29 , —C(═O)NHCHCH claim 29 , and —C(═O)NHCHCF.31. The compound of claim 5 , wherein Ris acyloxyor substituted acyloxy.3246-. (canceled)47. The compound of claim 5 , wherein Ris —CN.4850-. (canceled)51. The compound of claim 3 , wherein Ris absent.5253-. (canceled)54. The compound of claim 2 , wherein Rand Rare each methyl.55. The compound of claim 2 , wherein Rand Rare each hydrogen.56. The compound of claim 1 , wherein Rand Rare each hydrogen.57. The compound of claim 1 , wherein Rand Rare each methyl.58. (canceled)59. The compound of claim 5 , wherein the bond between carbons 9 and 11 is a single bond.60. The compound of claim 5 , wherein the bond between carbons 9 and 11 is a double bond.61137-. (canceled)138. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.139146-. (canceled)147. A therapeutic method comprising administering a pharmaceutically effective amount of a compound of to a subject.148. The method of claim 147 , wherein the subject is a human.149. (canceled)150. A method of treating cancer in a subject claim 5 , comprising administering to the subject a pharmaceutically effective amount of a compound of .151173-. (canceled)174. A method of treating or preventing a disease with an inflammatory component in a subject claim 5 , comprising administering to the subject a pharmaceutically effective amount of a ...

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Номер записи: 71
06-03-2014 дата публикации

TRITERPENOID DERIVATIVES, BENZENOID DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Номер: US20140066498A1
Автор: WU Tian-Shung
Принадлежит: NATIONAL CHENG KUNG UNIVERSITY

The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): 3. The pharmaceutical composition as claimed in claim 2 , which has anti-inflammation or cancer cell cytotoxic activity. This application claims priority to, and is a Divisional of, U.S. patent application Ser. No. 13/067,230, file on May 18, 2011, which claims the benefit of filing date of U.S. Provisional Application Ser. Nos. 61/345,603, and 61/345,606, respectively entitled “The Constituents and Biological Activities from the Fruiting Body of ”, and “Camphoratins and Derivatives as a New Class of Anticancer and Anti-inflammatory Agents”, both filed May 18, 2010 under 35 USC §119(e)(1).1. Field of the InventionThe present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same and, more particularly, to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same, which can be used as anticancer agents or anti-inflammatory agents.2. Description of Related ArtNiuchangchih also named (synonym: ) (Polyporaceae, Aphyllophorales) is a rare and very precious medical fungus in Taiwan and is called as “national treasure of Taiwan”.This microorganism, , is parasitic to the inner heart-wood wall of old hollow trunks of Hay. (Lauraceae). The growth rate of natural in the wild is very slow, and it is difficult to cultivate in a greenhouse, making fruiting bodies expensive to obtain.In traditional Taiwanese folk medicine, has been used as an important health food for treating food, alcohol, and drug intoxication, diarrhea, abdominal pain, hypertension, itching, and liver cancer. It has been proven that comprises a lot of active ...

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Номер записи: 72
06-03-2014 дата публикации

Method for Preparing Curable Bicyclic Compound Derived from Biomass

Номер: US20140066637A1
Автор: Cho Jin Ku, JUNG Jae Won, Kim Baek Jin, KIM Bo Ra, KIM Sang Yong, LEE Do Hoon, Lee Jae Soung, Lee Sang Hyeup
Принадлежит: Korea Institute of Industrial Technology

The present invention relates to a curable bicyclic compound derived from biomass, solvent-free curable composition and a method for preparing thereof. The curable compound derived from biomass according to the invention comprises a bicycle structure, to which one of two epoxide functional groups are bonded. 110-. (canceled)11. A method for preparing a curable bicyclic compound derived from biomass , the method comprising:a step of preparing a starting material by preparing furan from hemicellulose extracted from biomass, maleic anhydride from cellulose extracted from biomass, or methyl acrylate from glycerol generated from biomass;a step of preparing an intermediate compound comprising bicycle and an alcohol functional group by reacting at least two of the starting materials; anda step of preparing a curable bicyclic compound comprising bicycle and an epoxide functional group by reacting the intermediate compound and epichlorohydrin.121. The method according to claim , wherein the step of preparing an intermediate compound involves reducing the intermediate compound by hydrogenation.131. The method according to claim , wherein the step of preparing a curable bicyclic compound involves reacting a mixture comprising the intermediate compound and the epichlorohydrin using PTC (Phase Transfer Catalyst) as a catalyst in a bi-phasic solvent system where a sodium hydroxide aqueous solution is added.141. The method according to claim , wherein the step of preparing an intermediate compound prepares an intermediate compound comprising bicycle and two alcohol functional groups by reacting the furan and the maleic anhydride through Diels-Alder reaction and consecutive reduction , and the step of preparing a curable bicyclic compound prepares the curable bicyclic compound comprising bicyclic and two epoxide functional groups by reacting the intermediate compound and the epichlorohydrin.15. The method according to claim 14 , wherein the step of preparing the intermediate ...

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Номер записи: 73
06-03-2014 дата публикации

NOVEL PROCESS FOR PREPARATION OF DARUNAVIR AND DARUNAVIR ETHANOLATE OF FINE PARTICLE SIZE

Номер: US20140066638A1
Автор: AHIRE Vijay, BHATNAGAR Akshat, BHISE Nandu, DESHMUKH Amol, KUMBHAR Krishnat, SASANE Sachin, Singh Girij Pal, VERMA Devendra, Vyas Rajesh
Принадлежит: Lupin Limited

The present invention provides a novel process for preparation of darunavir that involves reduction of [(1S,2R)-3-[[(4-nitrophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, of formula (5). The present invention also provides darunavir ethanolate of particle size wherein dis less than 130 μm, dis less than 30 μm, dis less than 10 μm and process for its preparation. 2. A process according to claim 1 , wherein 0.8 to 3 molar equivalents of furanyl derivative (3) claim 1 , most preferably 1.0 to 1.2 molar equivalents is employed.3. A process according to claim 1 , wherein step (i) is carried out in a solvent selected from group consisting of lower alcohols such as methanol claim 1 , ethanol claim 1 , n-propanol claim 1 , isopropanol; ketones such as acetone claim 1 , ethylmethyl ketone claim 1 , diethyl ketone claim 1 , methylisobutyl ketone; lower aliphatic esters such as ethyl acetate claim 1 , methyl acetate; halogenated hydrocarbons such as dichloromethane claim 1 , chloroform dichloroethane; dimethylformamide claim 1 , dimethyl sulfoxide claim 1 , acetonitrile claim 1 , water or mixtures thereof.4. A process according to claim 1 , wherein step (i) is carried out in dichloromethane.5. A process according to claim 1 , wherein the base employed in step (i) is selected from organic base such as triethylamine claim 1 , diisopropylethyl amine claim 1 , pyridine and the like or an inorganic base such as hydroxides of alkali metals or alkaline earth metals such as sodium hydroxide claim 1 , potassium hydroxide claim 1 , lithium hydroxide; bicarbonates of alkali metals or alkaline earth metals such as sodium bicarbonate claim 1 , potassium bicarbonate and the like; carbonates of alkali metals or alkaline earth metals such as sodium carbonate claim 1 , potassium carbonate; ammonia or the like.6. A process according to claim 1 , wherein the base employed in step (i) is triethylamine.7. A ...

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Номер записи: 74
13-03-2014 дата публикации

DAPHNE GENKWA EXTRACTS, AND PHARMACEUTICAL COMPOSITION CONTAINING FRACTIONS OF THE EXTRACTS OR COMPOUNDS SEPARATED FROM THE EXTRACTS AS ACTIVE INGREDIENTS FOR PREVENTING OR TREATING ATOPIC DERMATITIS

Номер: US20140072664A1
Автор: AHN Kyung Seop, Go Jae Jong, Ji Da Jung, KANG Ho Bum, KIM Jae Wha, Kim Joo Heon, OH Hyun Woo, OH Sei Ryang, Song Jae Sung, Sun Jang Mi
Принадлежит: Korea Research Institute of Bioscience and Biotechnology

The present invention relates to a pharmaceutical composition for the prevention or treatment of atopy comprising the extract of , the fraction thereof, of the compound isolated from the same as an active ingredient. More precisely, the extract of , the fraction thereof, or the compound isolated from the same, genekwadapnin or yuanhuacine, of the present invention can increase the secretion of cytokine in Th1 immune cells and suppress atopy in the atopy mouse model, so that the extract of , the fraction thereof, or the compound isolated from the same of the present invention can be effectively used for the prevention or treatment of atopy. 120-. (canceled)22. The method for treating atopy according to claim 21 , wherein the extract is an extract of a single or a mixed solvent comprising at least one member selected from the group consisting of water claim 21 , Cto Clower alcohol claim 21 , and acetone.23. The method for treating atopy according to claim 22 , wherein the Cto Clower alcohol is methanol or ethanol.24Daphne genkwaDaphne genkwa.. The method for treating atopy according to claim 21 , wherein the extract of is an extract of the stems claim 21 , roots claim 21 , leaves claim 21 , floral leaves claim 21 , or buds of25Daphne genkwaDaphne genkwaDaphne genkwa.. The method for treating atopy according to claim 24 , wherein the extract of is an extract of the floral leaves of or an extract of the buds of26Daphne genkwaDaphne genkwa. The method for treating atopy according to claim 21 , wherein the fraction of extract is obtained by fractionating the extract with hexane claim 21 , chloroform claim 21 , and ethyl acetate claim 21 , stepwise.27Daphne genkwa.. The method for treating atopy according to claim 21 , wherein the compound of formula 1 is isolated from the extract of28Daphne genkwa. The method for treating atopy according to claim 21 , wherein the extract of claim 21 , the fraction thereof or the compound of formula 1 maintains homeostasis of atopic skin ...

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Номер записи: 75
13-03-2014 дата публикации

ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS

Номер: US20140073629A1
Автор: Brenneman Jehrod Burnett, GINN John, LOWE Michael D., Sarko Christopher Ronald, TASBER Edward S., Zhang Zhonghua
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of formula (I): 2. The compound according to claim 1 , wherein:{'sub': '1-3', 'A is a 5-7 membered saturated heterocyclyl group containing one nitrogen, wherein one carbon of said heterocyclyl group is optionally substituted with one or two Calkyl groups;'}{'sup': '1', 'sub': '1-3', 'Ris Calkyl;'}{'sup': '4', 'Ris selected from H and F;'}{'sup': '5', 'sub': '3', 'Ris selected from H, Cl and —CH;'}{'sup': '6', 'sub': 1-6', '2', 'n', '3-6', '1-6', '2', 'n', '2', 'n', '2', 'n', '1-6', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '1-3', '1-3', '3', '2', '3, 'Ris bonded to the nitrogen on A and is selected from H, Calkyl, —(CH)Ccycloalkyl, —C(O)Calkyl, —(CH)heterocyclyl, —(CH)aryl and —(CH)heteroaryl, wherein said Calkyl, —(CH)heterocyclyl, —(CH)cycloalkyl, —(CH)aryl and —(CH)heteroaryl are optionally substituted with one to four groups independently selected from Calkyl, halogen, Calkoxy, —CF, —OH and —SOCH; and'}{'sup': '7', 'Ris H;'}or a salt thereof.4. The compound according to claim 1 , wherein:{'sup': '2', 'sub': 3', '3, 'Ris selected from —CH, F, Cl, and —CF; and'}{'sup': '6', 'sub': 1-6', '2', '3-6', '1-6', '2', 'n', '1-6', '2', 'n', '2', 'n', '1-3', '1-3', '3', '2', '3, 'Ris selected from H, Calkyl, —(CH)—Ccycloalkyl, —C(O)Calkyl and —(CH)heterocyclyl, wherein said Calkyl, —(CH)cycloalkyl and —(CH)heterocyclyl are optionally substituted with one to four groups independently selected from Calkyl, halogen, Calkoxy, —CF, —OH and —SOCH;'}or a salt thereof.5. The compound according to claim 1 , wherein each heterocyclyl referred to in Ris selected from oxetanyl claim 1 , tetrahydrofuranyl claim 1 , tetrahydropyranyl claim 1 , 2-oxabicyclo[3.2.0]heptanyl claim 1 , [1 claim 1 ,4]dioxanyl claim 1 , 8-oxabicyclo[3.2.1]octanyl claim 1 , 1-oxaspiro[4.5]decanyl and pyrrolidin-2-one;{'sup': '6', 'each heteroaryl referred to in Ris selected from imidazolyl, isoxazolyl, pyrazinyl, pyrazolyl, pyridinyl, pyrimidinyl, thiazolyl and 4,5,6,7- ...

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Номер записи: 76
13-03-2014 дата публикации

PHOTOCURABLE DIANHYDRO-HEXANE-HEXOL DERIVATIVE, MANUFACTURING METHOD THEREOF, AND PHOTOCURABLE COMPOSITION INCLUDING SAME

Номер: US20140073716A1
Автор: Cho Jin Ku, Jeong Jae Won, Kim Baek Jin, KIM Bo Ra, KIM Sang Yong, SHIN Seung Han
Принадлежит: Korea Institute of Industrial Technology

Provided herein is a photocurable dianhydrohexanehexol derivative, a method preparing the same, and a composition including the same, for example, to a photocurable compound derived from environmentally friendly biomass, the compound having a structure where a 2-hydroxypropyl methacrylate (HPM) functional group prepared by reacting a biomass derived dianhydrohexanehexol (1,4:3,6-dianhydro-d-hexane-1,2,3,4,5,6-hexol, DHH) compound under an optimal reaction condition is combined, a preparing method thereof, and a photocurable composition comprising the photocurable compound. 3. The method according to claim 2 , wherein the compound of formula 2 is derived from carbohydrate polymer.4. The method according to claim 2 , further comprising a nonprotonic polar solvent in step a).5. The method according to claim 4 , wherein the nonprotonic polar solvent is selected from a group consisting of DMSO claim 4 , DMF claim 4 , DMA claim 4 , and NMP or any combination thereof.6. The method according to claim 2 , wherein the epihalohydrin is selected from a group consisting of epichlorohydrin claim 2 , epibromohydrin claim 2 , and epiiodohydrin or any combination thereof.7. The method according to claim 2 , wherein the dehydrator is selected from a group consisting of LiOH claim 2 , NaOH claim 2 , and KOH or any combination thereof.8. The method according to claim 2 , wherein in step a) 100 to 800 parts by weight of epihalohydrin are used for every 100 parts by weight of the compound of formula 2.9. The method according to claim 2 , wherein in step a) claim 2 , 300 to 1000 parts by weight of epihalohydrin are used for every 100 parts by weight of the compound of formula 2.10. The method according to claim 2 , wherein step a) is carried out for about 0.5 to 16 hours.11. The method according to claim 2 , wherein step a) is carried out at a temperature between about 4 to 80° C.12. The method according to claim 2 , wherein step b) further comprises triethylamine.13. The method according ...

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Номер записи: 77
27-03-2014 дата публикации

Partially Saturated Tricyclic Compounds and Methods of Making and Using Same

Номер: US20140088078A1
Автор: Cramp Susan Mary, Dyke Hazel Joan, Pallin Thomas David, Zahler Robert
Принадлежит: Zafgen, Inc.

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. 2. The tricyclic compound of claim 1 , wherein X′ is selected from the group consisting of: —O—* claim 1 , —N(R)—* claim 1 , —C(RR)—C(RR)—* claim 1 , —C(R)═C(R)—* claim 1 , —O—C(RR)—* claim 1 , —N(R)—C(RR)—* claim 1 , —O—C(O)—* claim 1 , —N(R)—C(O)—* claim 1 , —N═C(R)—* and —O—C(RR)—C(RR)—*;{'sup': '+', 'wherein the and * indicate the attachment points of X′ as indicated in Formula I.'}3. The tricyclic compound of claim 1 , wherein Xis selected from the group consisting of: —NH—* claim 1 , —O—CH—* claim 1 , —NH—CH—* claim 1 , —N═CH—* and —CH═CH—*;{'sup': '+', 'wherein the and * indicate the attachment points of X′ as indicated in Formula I.'}4. The tricyclic compound of claim 1 , wherein Xis selected from the group consisting of: —O—* claim 1 , —N(R)—* claim 1 , —C(RR)—C(RR)—* claim 1 , —O—C(RR)—* claim 1 , —N(R)—C(RR)—* claim 1 , —O—C(O)—* claim 1 , —N(R)—C(O)—* claim 1 , and —O—C(RR)—C(RR)—*; wherein the and * indicate the attachment points of Xas indicated in Formula II.5. The tricyclic compound of claim 1 , wherein Xis selected from the group consisting of: —O—CH—* and —NH—CH—*; wherein the and * indicate the attachment points of Xas indicated in Formula II.6. The tricyclic compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare independently selected for each occurrence from the group consisting of hydrogen and methyl.7. The tricyclic compound of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , Rand Rare hydrogen.8. The tricyclic compound of claim 1 , wherein R claim 1 , R claim 1 , Rand Rare independently selected for each occurrence from the group consisting of hydrogen claim 1 , fluorine claim 1 , cyano and Calkyl.9. The tricyclic compound of claim 7 , ...

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Номер записи: 78
27-03-2014 дата публикации

IMIDAZOLE DERIVATIVES

Номер: US20140088124A1
Автор: Aslanian Robert, Balkovec James, DeVita Robert J., Dykstra Kevin D., Guiadeen Deodial, He Shuwen, Hong Qingmei, Jian Tianying, Kuang Rongze, Kuethe Jeffrey T., Lai Zhong, Liu Jian, Sperbeck Donald M., Ting Pauline C., Wu Heping, Wu Zhicai, Yang Ginger Xu-qiang, Yu Yang, Zhou Gang
Принадлежит:

Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity. 5. A compound of or pharmaceutically acceptable salt thereof wherein T and X are both —CH—.6. A compound of or pharmaceutically acceptable salt thereof wherein V is —N— and W is —CH—.7. A compound of or pharmaceutically acceptable salt thereof wherein T is —N— and X is —CH—.9. A compound of or pharmaceutically acceptable salt thereof wherein Ris hydrogen or halogen.10. A compound of or pharmaceutically acceptable salt thereof wherein Ris hydrogen or halogen.11. A compound of or pharmaceutically acceptable salt thereof wherein Ris hydrogen claim 1 , methyl or halogen.12. A compound of or pharmaceutically acceptable salt thereof wherein Ris hydrogen or halogen.14. A compound of or pharmaceutically acceptable salt thereof wherein m and n are independently selected from 0 or 1.15. A compound of or pharmaceutically acceptable salt thereof wherein Ris selected from the group consisting of —OH claim 1 , —COOH claim 1 , —COOC-Calkyl claim 1 , —C-CalkylCOOC-Calkyl claim 1 , C-Calkyl or —C-CalkylCOOH.16. A compound of or pharmaceutically acceptable salt thereof wherein Ris CONHSOC-Calkyl claim 1 , CONHSOhalogen-substitutedC-Calkyl claim 1 , CONHSOC-Ccycloalkyl claim 1 , CONHSOC-CcycloalkylC-Calkyl claim 1 , CONHSOheteroaryl claim 1 , CONHSOaryl claim 1 , CONHSOhalogen-substitutedaryl and CONHSOarylhalogen-substitutedC-Calkyl.18. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.19. (canceled)20. A method for the treatment of a condition selected from the group consisting of obesity and diabetes comprising administering to an individual a pharmaceutical composition comprising the compound of . This application claims the benefit of U.S. Provisional ...

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Номер записи: 79
27-03-2014 дата публикации

METHOD FOR PREPARATION OF ANHYDROSUGAR ALCOHOLS

Номер: US20140088315A1
Автор: JUNG Young Jae, Kim Young Seok, RYU Hoon
Принадлежит: SAMYANG GENEX CORPORATION

Disclosed is a method for the preparation of an anhydrosugar alcohol using a starch-derived hexitol such as sorbitol or mannitol Anhydrosugar alcohol is in the form of a diol having two hydroxyl groups in the molecule thereof and has a very high utility value as a physical property modifier which can be used primarily in plastics. Representative examples of anhydrosugar alcohols include isosorbide and isomannide. These anhydrosugar alcohols are capable of increasing a glass transition temperature of and improving strength of PET, polyesters, polycarbonates, etc., and are therefore highly valuable as biodegradable environmentally-friendly bioplastics. 1. A method for the preparation of an anhydrosugar alcohol , comprising dehydrating hexitol with a mixed acid of first acid and second acid , wherein the first acid is sulfuric acid , and the second acid is at least one sulfur-containing acid or sulfur-containing acid salt selected from the group consisting of p-toluenesulfonic acid , methanesulfonic acid , ethanesulfonic acid , benzenesulfonic acid , naphthalenesulfonic acid and aluminum sulfate.2. A method for the preparation of an anhydrosugar alcohol , comprising dehydrating hexitol with a mixed acid of first acid and second acid to produce an anhydrosugar alcohol and purifying the anhydrosugar alcohol , wherein the first acid is sulfuric acid , and the second acid is at least one sulfur-containing acid or sulfur-containing acid salt selected from the group consisting of p-toluenesulfonic acid , methanesulfonic acid , ethanesulfonic acid , benzenesulfonic acid , naphthalenesulfonic acid and aluminum sulfate.3. The method according to claim 1 , wherein the mixed acid is added in an amount of 0.5 to 10 parts by weight based on 100 parts by weight of hexitol.4. The method according to claim 1 , wherein the ratio of first acid to second acid in the mixed acid is in the range of 1:9 to 7:3 by weight.5. The method according to claim 1 , wherein the hexitol is at least one ...

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Номер записи: 80
03-04-2014 дата публикации

Taxane and Abeo-Taxane Analogs

Номер: US20140093503A1
Автор: Gundluru Mahesh Kumar, Henry John T., McChesney James D., Venkataraman Sylesh
Принадлежит: Arbor Therapeutics, LLC

The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes. 2. The compound of claim 1 , wherein:{'sub': 1-6', '1-6', '6-10', '1-3, 'R is selected from the group consisting of Calkyl, Calkoxy- and CarylCalkoxy;'}{'sub': 1', '1-6', '6-10', '1-3, 'Ris hydrogen or R′CO—, wherein R′ is selected from the group consisting of Calkyl, Caryl and arylCalkyl-;'}{'sub': 3', '1-18', '2-6, 'Ris selected from the group consisting of Calkyl and optionally substituted Calkenyl; and'}{'sub': '3', 'R′is hydrogen.'}3. The compound of claim 1 , wherein Ris selected from the group consisting of (CH)CHCH— claim 1 , (CH)CH— claim 1 , t-butyl claim 1 , optionally substituted phenyl claim 1 , and optionally substituted heteroaryl claim 1 , R is t-butoxy claim 1 , Ris CHCO— claim 1 , Ris beta CH═CH— and R′is hydrogen.5. The compound of claim 4 , wherein:{'sub': 1-6', '1-6', '6-10', '1-3, 'R is selected from the group consisting of Calkyl, Calkoxy- and CarylCalkoxy;'}{'sub': 1', '1-6', '6-10', '1-3, 'Ris hydrogen or R′CO—, wherein R′ is selected from the group consisting of Calkyl, Caryl and arylCalkyl-;'}{'sub': 3', '1-18', '2-6, 'Ris selected from the group consisting of Calkyl and optionally substituted Calkenyl; and'}{'sub': '3', 'R′is hydrogen.'}6. The compound of claim 4 , wherein Ris selected from the group consisting of (CH)CHCH— claim 4 , (CH)CH— claim 4 , t-butyl claim 4 , optionally substituted phenyl and optionally substituted heteroaryl claim 4 , R is tert-butoxy claim 4 , Ris CHCO— claim 4 , Ris beta CH═CH— and R′is hydrogen.8. (canceled)9. The compound of claim 1 , wherein the compound is greater than 95% pure or greater than 99% pure.10. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) a therapeutically effective amount of a compound of , in the ...

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Номер записи: 81
04-01-2018 дата публикации

Methods for Making Catechin Derivatives

Номер: US20180000761A1
Автор: Leahy James William, Lemus Andrea A.
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

Disclosed herein are methods for making a catechin derivative, or a salt thereof. The methods can include: contacting an alcohol protected aromatic aldehyde and a triphenyl phosphonium ylide to make an alcohol protected aromatic olefin; hydrogenating the alcohol protected aromatic olefin to make alcohol protected aromatic compound; and deprotecting the alcohol protected aromatic compound to make the catechin derivative. 1. A method for making a catechin derivative , or a salt thereof , the method comprising:contacting an alcohol protected aromatic aldehyde and a triphenyl phosphonium ylide to make an alcohol protected aromatic olefin;hydrogenating the alcohol protected aromatic olefin to make an alcohol protected aromatic compound; anddeprotecting the alcohol protected aromatic compound to make the catechin derivative.8. The method of claim 6 , wherein the chiral catalyst is present and is selected from (DHQ)PHAL and (DHQD)PHAL.9. The method of claim 6 , wherein the free radical initiator is selected from a group consisting of: dicumyl peroxide claim 6 , di-t-butyl peroxide claim 6 , t-butylperoxybenzoate claim 6 , 2 claim 6 ,5-dimethyl-2 claim 6 ,5-di(t-butylperoxy)hexane claim 6 , t-butyl peroxyneodecanoate claim 6 , 2 claim 6 ,5-dimethyl-2 claim 6 ,5-di(t-butylperoxy)hexyne claim 6 , t-amyl peroxypivalate claim 6 , 1 claim 6 ,3-bis(t-butylperoxyisopropyl)benzene claim 6 , tert-amylperoxy 2-ethyl hexanoate claim 6 , t-butylperoxy 2-ethyl hexanoate claim 6 , t-butyl peroxy isobutyrate claim 6 , t-butylperoxy isopropyl carbonate claim 6 , t-butylperoxy 3 claim 6 ,5 claim 6 ,5-trimethylhexanoate claim 6 , 2 claim 6 ,5-dimethyl-2 claim 6 ,5-di(benzolyperoxy)hexane claim 6 , n-butyl 4 claim 6 ,4-di(t-butylperoxy)valcratic claim 6 , t-butylcumyl peroxide claim 6 , di(2-t-butylperoxy isopropyl)benzene claim 6 , t-butyl hydroperoxide claim 6 , cumyl hydroperoxide and mixtures thereof. Examples of suitable azo compounds include 2 claim 6 ,2′-azobisisopropionitrile claim 6 ...

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Номер записи: 82
05-01-2017 дата публикации

COMPOUND USEFUL FOR MANUFACTURING SALACINOL, METHOD FOR MANUFACTURING THE COMPOUND, METHOD FOR MANUFACTURING SALACINOL, METHODS FOR PROTECTING AND DEPROTECTING DIOL GROUP, AND PROTECTIVE AGENT FOR DIOL GROUP

Номер: US20170001974A1
Автор: FUJINO Yuuta, KATSUMATA Taiji, NAGASE Hisato, NAKAMURA Koki, WATANABE Katsuyuki
Принадлежит: FUJIFILM Corporation

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol. 2. The compound according to claim 1 ,{'sup': 1a', '1b, 'wherein Rand Rare the same as or different from each other and each represent a carboxy protective group.'}3. The compound according to claim 1 ,{'sup': 2', '3, 'wherein each of Rand Ris a hydroxy group.'}6. The compound according to claim 1 ,{'sup': '5', 'wherein Ris a phenyl group which may be substituted.'}7. The compound according to that is a compound selected from dimethyl 2-((4aS claim 1 ,8aR)-6-phenyltetrahydro[1 claim 1 ,3]dioxino[5 claim 1 ,4-d][1 claim 1 ,3]dioxin-2-yl)malonate claim 1 , dimethyl 2-((4R claim 1 ,5S)-5-hydroxy-4-(hydroxymethyl)-1 claim 1 ,3-dioxan-2-yl)malonate claim 1 , dimethyl 2-((4aR claim 1 ,8aS)-2 claim 1 ,2-dioxidotetrahydro[1 claim 1 ,3]dioxin[5 claim 1 ,4-d][1 claim 1 ,3 claim 1 ,2]dioxathiin-6-yl)malonate claim 1 , (4S claim 1 ,5S)-4-(((2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-dihydroxy-2-(hydroxymethyl)tetrahydro-1H-thiophen-1-ium-1-yl) methyl-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , (4S claim 1 ,5 S)-4-(((1 S claim 1 ,2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-bis(benzyloxy)-2-((benzyloxy)methyl)tetrahydro-1H-thiophen-1-ium-1-yl)methyl)-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , (4S claim 1 ,5S)-4-(((1 S claim 1 ,2R claim 1 ,3 S claim 1 ,4S)-3 claim 1 ,4-bis((4-methoxybenzyl)oxy)-2-(((4-methoxybenzyl)oxy)methyl)tetrahydro-1H-thiophen-1-ium-1-yl)methyl)-2-(1 claim 1 ,3-dimethoxy-1 claim 1 ,3-dioxopropan-2-yl)-1 claim 1 ,3-dioxan-5-yl sulfate claim 1 , diethyl 2-((4aS claim 1 ,8aR)-6-phenyltetrahydro[1 ...

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Номер записи: 83
05-01-2017 дата публикации

1-HETEROCYCLYL ISOCHROMANYL COMPOUNDS AND ANALOGS FOR TREATING CNS DISORDERS

Номер: US20170001987A1
Автор: Alexandrov Vadim, HANANIA Taleen G., Jones Philip Glyn, Powell Noel Aaron, Spear Kerry L., Xie Linghong
Принадлежит:

Disclosed are compounds of Formula (I): 6. The compound of claim 1 , wherein Z is C.7. The compound of claim 6 , wherein n2 is 0 and n3 is 0.8. The compound of claim 6 , wherein one of n2 and n3 is 0 and the other is 1.9. The compound of claim 6 , wherein n2 is 1 and n3 is 1.10. The compound of claim 1 , wherein n2 is 1 and Z is O.11. The compound of claim 10 , wherein n3 is 1.13. The compound of claim 1 , wherein n1 is 1.14. The compound of claim 1 , wherein n1 is 2.15. The compound of claim 1 , wherein n1 is 3.16. The compound of claim 1 , wherein at least two of R claim 1 , R claim 1 , R claim 1 , and Rare —H.17. The compound of claim 1 , wherein at least three of R claim 1 , R claim 1 , R claim 1 , and Rare —H.18. The compound of claim 1 , wherein the 5- or 6-membered heteroaryl has at least 1 nitrogen ring atom and is unsubstituted or substituted with 1 group selected from halo claim 1 , —OH claim 1 , —OCH claim 1 , —OCF claim 1 , —NH claim 1 , —NH(CH) claim 1 , —N(CH) claim 1 , —CH claim 1 , ethyl claim 1 , —CF claim 1 , and —CN.19. The compound of claim 18 , wherein the heteroaryl is unsubstituted pyridyl claim 18 , pyrimidinyl claim 18 , pyrrolyl claim 18 , pyrazolyl claim 18 , isoxazolyl claim 18 , imidazolyl claim 18 , or oxazolyl.20. The compound of claim 18 , wherein the heteroaryl is unsubstituted pyridyl or isoxazolyl.21. The compound of claim 1 , wherein two adjacent instances of R claim 1 , R claim 1 , R claim 1 , and Rtogether form —O—CH—O— claim 1 , —O—CH(CH)—O— claim 1 , or —O—C(CH)—O—.22. The compound of claim 21 , wherein two adjacent instances of R claim 21 , R claim 21 , R claim 21 , and Rtogether form —O—CH—O—.23. The compound of claim 1 , wherein Ris —H.24. The compound of claim 1 , wherein R is —H.25. The compound of claim 1 , wherein each instance of Ris —F or —CH.26. The compound of claim 1 , wherein each instance of Ris —F or —CH.27. The compound of claim 1 , wherein each instance of Ris —CH.28. The compound of claim 1 , wherein m is 0. ...

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Номер записи: 84
07-01-2016 дата публикации

ANTIDIABETIC BICYCLIC COMPOUNDS

Номер: US20160002255A1
Автор: Brockunier Linda L., Chen Helen, Chobanian Harry R., Clements Matthew J. H., Crespo Alejandro, DeMong Duane E., Guo Yan, Hagmann William K., Marcantonio Karen M., Miller Michael, Pio Barbara, Plummer Christopher W., Xiao Dong
Принадлежит:

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 2. The compound according to wherein “a” is a single bond; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein T is CH; U is CR; V is CR; and W is CH claim 1 , N or N-oxide; or a pharmaceutically acceptable salt thereof.4. The compound according to wherein T is CH; U is CR; V is CR; and W is CH; or a pharmaceutically acceptable salt thereof.5. The compound according to wherein T is CH; U is CR; V is CR; and W is N; or a pharmaceutically acceptable salt thereof.6. The compound according to wherein Y is selected from the group consisting of:{'sup': g', 'g, '(1) —CRR,'}(2) C═O,{'sup': 'g', 'sub': '1-6', '(3) —C(R)OCalkyl,'}{'sub': '2', '(4) —CF, and'}{'sup': 'c', '(5) —NR;'}or a pharmaceutically acceptable salt thereof.7. The compound according to wherein Y is selected from the group consisting of: —CRR; or a pharmaceutically acceptable salt thereof.8. The compound according to wherein A is selected from the group consisting of:(1) aryl, and(2) heteroaryl,{'sup': 'a', 'wherein each aryl and heteroaryl is unsubstituted or substituted with one to five substituents selected from R; or a pharmaceutically acceptable salt thereof.'}9. The compound according to wherein B is selected from the group consisting of:(1) hydrogen,(2) aryl,(3) aryl-O—,{'sub': '1-10', '(4) aryl-Calkyl-O—'}{'sub': '3-6', '(5) Ccycloalkenyl, and'}(6) heteroaryl,{'sup': 'b', 'wherein B is unsubstituted or ...

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Номер записи: 85
05-01-2017 дата публикации

Enhanced regio-selectivity in glycol acylation

Номер: US20170002018A1
Автор: Erik Hagberg, Erin ROCKAFELLOW, Kenneth STENSRUD
Принадлежит: Archer Daniels Midland Co

A method for acid-catalyzed acylation of an isohexide is described. The method involves a reaction of an isohexide and an excess of carboxylic acid in the presence of a Lewis acid or a Brønsted acid catalyst. One or more Lewis acid or Brønsted acid can facilitate conversion of isohexides to their corresponding mono and diesters with a pronounced greater regio-selectivity of exo-OH over endo-OH of the isohexide in the product. Particular catalytic acid species include zirconium chloride (ZrCl 4 ) and phosphonic acid (H 3 PO 3 ), which manifest a ratio of exo:endo regioselectivity of about 5.0≠3:1 and about 4.00.3:1, respectively.

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Номер записи: 86
05-01-2017 дата публикации

SYNTHESIS OF ISOHEXIDE ETHERS AND CARBONATES

Номер: US20170002019A1
Автор: Stensrud Kenneth, Venkitasubramanian Padmesh
Принадлежит:

A facile, straightforward method for alkylation of anhydrosugar alcohols (isohexides) using a carbonate reagent is described. The alkylation method involves: a) contacting in a solution of an isohexide with a dialkyl, diallyl, or diaryl carbonate, and the solution includes a Brønsted base; and b) producing either an alkyl ether or alkyl carbonate of the isohexide compound. The alkylation reaction is in situ, that is, performed without an extrinsic catalyst. According to the method, one can synthesize various ethers and carbonates. 1. A method of alkylating an anhydrosugar compound comprising: a) contacting an isohexide compound with a dialkyl , diallyl , or diaryl carbonate and a Brønsted base; and b) producing at least an alkyl ether or alkyl carbonate of the isohexide compound.2. The method according to claim 1 , wherein the anhydrosugar compound is at least one of: isosorbide claim 1 , isomannide claim 1 , and isoidide.3. The method according to claim 1 , wherein said dialkyl claim 1 , diallyl claim 1 , or diaryl carbonate has an R-group having 1 to 20 carbon atoms.4. The method according to claim 3 , wherein when said R-group is at least one of methyl claim 3 , ethyl claim 3 , propyl group claim 3 , said alkyl ether is produced predominantly.5. The method according to claim 3 , wherein when said R-group is at least a C-Cgroup claim 3 , said alkyl carbonate is produced predominantly.6. The method according to claim 1 , wherein said alkylated ether of said isohexide compound is at least one of: mono-ether of isoidide claim 1 , mono-ether of isomannide claim 1 , mono-ether of isosorbide claim 1 , di-ether of isoidide claim 1 , di-ether of isomannide claim 1 , and di-ether of isosorbide.7. The method according to claim 3 , wherein said alkylated isohexide compound is an ether having at least one of the following alkyl groups: a mono-methyl claim 3 , mono-ethyl claim 3 , mono-propyl claim 3 , di-methyl claim 3 , di-ethyl claim 3 , or di-propyl isohexide ether.8. The ...

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Номер записи: 87
05-01-2017 дата публикации

HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME

Номер: US20170002032A9
Автор: Duffey Matthew O., England Dylan, Freeze Scott, Hu Zhigen, Langston Steven, McIntyre Charles, Mizutani Hirotake, Ono Koji, Xu He
Принадлежит: Millennium Pharmaceuticals, Inc.

Disclosed are chemical entities which are compounds of formula (I): 3. The chemical entity of claim 1 , wherein L is —C(R)(R)— claim 1 , —S— claim 1 , —S(O)— claim 1 , —S(O)— claim 1 , —C(O)— claim 1 , —C(═CH)— claim 1 , —C(R)(R)—C(═CH)— claim 1 , —C(R)(R)—C≡C— claim 1 , —C(R)(R)—O— claim 1 , —C(R)(R)—S— claim 1 , —C(R)(R)—N(R)— claim 1 , —C(R)(R)—N(R)—CH— claim 1 , —C(R)(R)—CH— claim 1 , —C(R)(R)—CH—CH— claim 1 , or —C(O)—C(R)(R)—.4. The chemical entity of claim 1 , wherein:{'sub': 1', '2, 'sup': z3', 'z3', 'z3, 'Zis hydrogen, halogen, cyano, R, —S(O)—R, or —S(O)—R;'}{'sup': z3', 'z4, 'sub': '1-4', 'Ris a phenyl, 5- to 7-membered cycloaliphatic, 5- to 7-membered heterocyclyl, or Caliphatic, any of which may be substituted with one or more independently selected R;'}{'sup': z4', 'z5', 'z6', 'z5, 'sub': 1-4', '1-4', '1-4', '1-4', '2', '2, 'Ris hydroxyl, halogen, cyano, Caliphatic, Cfluoroaliphatic, Calkoxy, Cfluoroalkoxy, —N(R), —C(O)R, —C(O)R, 5- or 6-membered cycloaliphatic or heterocyclyl, or a phenyl optionally substituted with one or more independently selected halogens;'}{'sup': 'z5', 'sub': '1-4', 'each occurrence of Ris independently hydrogen or Calkyl; and'}{'sup': 'z6', 'sub': '1-4', 'each occurrence of Ris independently Calkyl.'}5. The chemical entity of claim 4 , wherein Zis hydrogen; halogen; cyano; phenyl optionally substituted with one or more independently selected halogens; 5- to 7-membered cycloaliphatic or heterocyclyl optionally fused to a 6-membered aryl claim 4 , wherein the 5- to 7-membered cycloaliphatic or heterocyclyl optionally fused to a 6-membered aryl is optionally substituted with one or more independently selected halogens; Cfluoroaliphatic; or a Caliphatic group optionally substituted with one or more hydroxyl claim 4 , Calkoxy claim 4 , phenyl optionally substituted with one more independently selected halogens claim 4 , 5- or 6-membered cycloaliphatic claim 4 , 5- or 6-membered heterocyclyl claim 4 , or —N(R).6. The chemical entity ...

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Номер записи: 88
05-01-2017 дата публикации

PROCESS FOR PRODUCING ISOHEXIDE GLYCIDYL ETHERS, PRODUCTS THUS OBTAINED, AND USES THEREOF

Номер: US20170002132A1
Автор: Buffe Clothilde, DOLENEC Amelie, Ibert Mathias
Принадлежит:

A process for producing bis-anhydrohexitol ether compositions and in particular isohexide glycidyl ether compositions, one of the originalities of which is azeotropic distillation carried out under reduced pressure. Such compositions are used to produce epoxy resins, the function thereof being to form a three-dimensional macromolecular network. The compositions obtained according to the process are rich in diepoxy derivatives of isosorbide to the detriment of monoepoxy derivatives, only the first participating in the formation of the three-dimensional network. The crosslinking density is therefore increased, thereby making it possible to obtain a material which is more chemically resistant and mechanically stronger and which has a higher glass transition temperature (Tg), compared with the same materials obtained with bis-anhydrohexitol ether compositions according to the prior art. 19-. (canceled)10. A process for producing bis-anhydrohexitol ether compositions , comprising the following steps:a) bringing a dianhydrohexitol into contact with an organic halide,b) placing the resulting mixture of dianhydrohexitol and organic halide under vacuum so as to obtain a negative pressure of between 100 mbar and 1000 mbar,c) heating the mixture under vacuum at a temperature of between 50° C. and 120° C. and thus carrying out an azeotropic distillation,d) then adding to said mixture a basic reagent for a period of between 1 hour and 10 hours and then continuing the azeotropic distillation,e) recovering the bis-anhydrohexitol ether composition after a filtration step, concentration of the filtering and optionally a purification step.11. The process as claimed in claim 10 , wherein the dianhydrohexitol is an isohexitol claim 10 , more preferentially chosen from isosorbide claim 10 , isomannide and isoidide claim 10 , and is claim 10 , more preferentially claim 10 , isosorbide.12. The process as claimed in claim 10 , wherein the organic halide is chosen from epibromohydrin claim ...

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Номер записи: 89
07-01-2016 дата публикации

LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20160002535A1
Автор: HUANG WAN-YU, Lee Ching-Tien, Wang Chun-Chih
Принадлежит:

A liquid crystal compound of formula (I): 2. The liquid crystal compound according to claim 1 , wherein A claim 1 , A claim 1 , and Aare each independently halogen-substituted or unsubstituted 1 claim 1 ,4-phenylene.3. The liquid crystal compound according to claim 2 , wherein A claim 2 , A claim 2 , and Aare each independently 1 claim 2 ,4-phenylene claim 2 , 2-fluoro-1 claim 2 ,4-phenylene claim 2 , 3-fluoro-1 claim 2 ,4-phenylene claim 2 , 2 claim 2 ,3-difluoro-1 claim 2 ,4-phenylene claim 2 , or 3 claim 2 ,5-difluoro-1 claim 2 ,4-phenylene.4. The liquid crystal compound according to claim 1 , wherein Ris a halogen atom claim 1 , —CN claim 1 , —CF claim 1 , —OCF claim 1 , —OCH═CF claim 1 , —OCFCF═CF claim 1 , a C1-C10 alkyl group or a C1-C10 alkoxyl group.5. The liquid crystal compound according to claim 1 , wherein Ris a hydrogen atom claim 1 , a C1-C5 alkyl group or a halogen-substituted C1-C5 alkyl group.6. The liquid crystal compound according to claim 1 , wherein Z claim 1 , Z claim 1 , and Zare each independently a single bond or —CFO—.7. The liquid crystal compound according to claim 1 , wherein: A claim 1 , A claim 1 , and Aare each independently 1 claim 1 ,4-phenylene claim 1 , 2-fluoro-1 claim 1 ,4-phenylene claim 1 , 3-fluoro-1 claim 1 ,4-phenylene claim 1 , 2 claim 1 ,3-difluoro-1 claim 1 ,4-phenylene claim 1 , or 3 claim 1 ,5-difluoro-1 claim 1 ,4-phenylene; Z claim 1 , Z claim 1 , and Zare each independently a single bond or —CFO—; n=0; and m=0 or 1.8. A liquid crystal composition comprises the liquid crystal compound according to .10. The liquid crystal composition according to claim 9 , wherein Ris a hydrogen atom claim 9 , a C1-C10 alkyl group claim 9 , and Ris a halogen atom claim 9 , —CN claim 9 , a C1-C10 alkyl group claim 9 , a C2-C10 alkenyl group claim 9 , —OCHCF claim 9 , —CF claim 9 , or —OCF.11. A liquid crystal display device comprising a liquid crystal compound according to . This application claims the priority of Taiwan application ...

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Номер записи: 90
04-01-2018 дата публикации

PARTIALLY SATURATED TRICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20180002307A1
Автор: Cramp Susan M., Dyke Hazel J., Pallin Thomas D., Zahler Robert
Принадлежит:

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. 144.-. (canceled)46. The tricyclic compound of claim 45 , wherein Ris selected from hydrogen or methyl.47. The tricyclic compound of claim 45 , wherein Ris selected from hydrogen or fluorine.48. The tricyclic compound of claim 45 , wherein Ris Calkenyl substituted by RRN—.49. The tricyclic compound of claim 45 , wherein Ris (Z)-3-(N claim 45 ,N-diethylamino)prop-1-enyl. This application is a continuation of U.S. patent application Ser. No. 15/014,524, filed Feb. 3, 2016; which is a continuation of U.S. patent application Ser. No. 14/116,023, filed Nov. 6, 2013; which is a national stage filing under U.S.C. §371 of PCT/US2012/036789, filed May 7, 2012; which claims priority to U.S. Provisional Patent Application 61/559,856, filed Nov. 15, 2011; and U.S. Provisional Patent Application 61/483,257, filed May 6, 2011; all of which are incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., diseases and other adverse health conditions associated with, exacerbated by, or precipitated by being overweight or obese. The estimated mortality from obesity-related conditions in the United States is over 300,000 annually (O'Brien et al. Amer J Surgery (2002) 184:4S-8S; and Hill et al. (1998) Science, ...

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Номер записи: 91
02-01-2020 дата публикации

PALLADIUM-MEDIATED KETOLIZATION

Номер: US20200002352A1
Автор: Kishi Yoshito, LEE Jung Hwa, Li Zhanjie, Osawa Ayumi
Принадлежит: President and Fellows of Harvard College

Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer). 1111-. (canceled)114144-. (canceled)146. The compound of claim 112 , wherein Ris optionally substituted Calkyl.147. The compound of claim 146 , wherein Ris unsubstituted Calkyl.148. The compound of claim 146 , wherein Ris methyl.150153-. (canceled)154. The compound of claim 112 , wherein Ris hydrogen.155. The compound of claim 112 , wherein Ris hydrogen.156159-. (canceled)160. The compound of claim 112 , wherein Rand Rare hydrogen.161. The compound of claim 112 , wherein R claim 112 , R claim 112 , and Rare optionally substituted Calkyl.162. The compound of claim 161 , wherein R claim 161 , R claim 161 , and Rare unsubstituted Calkyl.163. The compound of claim 161 , wherein R claim 161 , R claim 161 , and Rare methyl.164. (canceled)165. A pharmaceutical composition comprising a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 , and optionally a pharmaceutically acceptable excipient.166. A method of inhibiting mitosis in a subject in need thereof claim 112 , the method comprising administering to the subject a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 , or a pharmaceutical composition thereof claim 112 , in an amount sufficient to inhibit mitosis.167. A method of triggering apoptosis in cell of a subject claim 112 , the method comprising administering to the subject a compound of claim 112 , or a pharmaceutically acceptable salt thereof claim 112 ...

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Номер записи: 92
07-01-2021 дата публикации

ISOIDIDE DERIVATIVES AND METHODS OF MAKING AND USING SAME

Номер: US20210002291A1
Автор: SIDDURI Achyutharao
Принадлежит:

The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists. An illustrative compound is shown below: 19-. (canceled)11. The compound of claim 10 , wherein Ris H.12. The compound of claim 10 , wherein:{'sup': '1', 'Ris a substituted monocyclic or bicyclic ring having 0, 1, or 2 heteroatoms independently selected from the group consisting of N, O, or S; and'}{'sup': '2', 'sub': 1', '10, 'Ris hydroxyl or OC(O)C-Calkyl.'}16. The compound of claim 15 , wherein Ris C(O)C-Calkyl.17. A pharmaceutical composition comprising at least one compound of claim 10 , or a pharmaceutically acceptable salt or tautomer thereof claim 10 , and at least one pharmaceutically acceptable carrier.18. The pharmaceutical composition of claim 17 , further comprising one or more additional therapeutic agents. This application claims priority to U.S. application Ser. No. 15/250,336 filed on Aug. 29, 2016 which claims priority to U.S. Application 62/214,519 filed on Sep. 4, 2015, the contents of which are herein fully incorporated by reference in its entirety.The field of the embodiments of the present invention relate to compounds having improved solubility thereby increasing their bioavailability. In particular, the present invention relates to the synthesis and applications of such target compounds.Isosorbide is a heterocyclic compound derived from glucose. Isosorbide has two isomers, namely two diastereomers, isomannide and isoidide, which belong to a class of compounds called 1,4;3,6-dianhydrohexitols. Isosorbide is essentially two fused tetrahydrofuran rings having a cis-arrangement at the ring junction, providing for a wedge-shaped molecule. The compound bears two ...

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Номер записи: 93
01-01-2015 дата публикации

Active Energy Ray Curable Aqueous Emulsions

Номер: US20150005408A1
Автор: Arceneaux JoAnn, Cleymans Ruben, Hibiu Hideo, Lindekens Luc, Nagakawa Ichiro, Tanabiki Fumio
Принадлежит:

The present invention relates to (meth)acrylated compounds (A) prepared from (a) at least one cyclic ether polyol, (b) at least one linking compound (b1) and/or (b2), wherein the linking compound (b1) is selected from cyclic compounds (b11) containing at least one (I) group in the cycle where X=O or NH, from hydroxy acids (b12) and/or from alkylene oxides (b13) containing from 2 to 4 carbon atoms and the linking compound (b2) is selected from epihalohydrins or polyisocyanates, (c) a (meth)acrylating compound; and to their use in radiation curable compositions for the coatings, inks, overprint varnishes, adhesives and composites. 2. The compound according to claim 1 , wherein the cyclic ether polyol is selected from dianhydrohexitols.3. The compound according to claim 1 , wherein the cyclic ether polyol is isosorbide.4. The compound according to claim 1 , wherein the linking compound (b11) is selected from lactones claim 1 , lactides claim 1 , lactams and mixtures thereof.5. The compound according to claim 1 , wherein the linking compound (b12) is glycolic acid.6. The compound according to claim 1 , wherein the linking compound (b13) is selected from ethylene oxide claim 1 , propylene oxide and mixtures thereof.7. The compound according to claim 1 , wherein the epihalohydrin is epichlorhydrin.8. The compound according to claim 1 , wherein the polyisocyanate is selected from aliphatic polyisocyanates.9. The compound according to claim 1 , wherein the (meth)acrylating compound (c) is selected from an unsaturated acid claim 1 , an acyl halide of the unsaturated acid claim 1 , a corresponding anhydride of the unsaturated acid claim 1 , a C-Calkyl ester of the unsaturated acid (c1) claim 1 , or from compounds containing at least one reactive group capable to react with isocyanate groups as well as at least one (meth)acryloyl group (c2).10. The compound according to claim 9 , wherein the (meth)acrylating compound (c1) is selected from acrylic acid claim 9 , methacrylic ...

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Номер записи: 94
01-01-2015 дата публикации

PROCESS FOR THE PRODUCTION OF 4-SUBSTITUTED CHROMANES VIA GOLD CATALYSIS

Номер: US20150005514A1
Автор: Dattatray Ambadas Devalankar, Pandurang Vilasrao Chouthaiwale, Sudalai Arumugam
Принадлежит:

Disclosed herein is single step process for the synthesis of 4-aryl substituted chromanes of compound of formula 2 comprising subjecting 3-aryloxy-1-phenylpropan-1-ol of formula 1 to gold(III) chloride-catalyzed intramolecular Friedel-Crafts reaction to obtain 4-aryl substituted chromanes. The invention further discloses novel 4-substituted Chromane compounds. 2. The process according to claim 1 , wherein claim 1 , the process is carried out at temperature in the range of 20 to 30° C.3. The process according to claim 1 , wherein the process is carried out in presence of a solvent selected from the group consisting of halogenated hydrocarbons.4. The process according to claim 1 , wherein the molar ratios of the 3-aryloxy-1-phenylpropan-1-ol with reference to gold(III) chloride is in the range of 1:0.01.6. (canceled)7. (canceled) Present invention relates to synthesis of 4-aryl substituted chromanes by using gold (III) chloride-catalyzed intramolecular Friedel-Crafts reaction of 3-aryloxy benzyl alcohol. The invention further relates to novel 4-substituted Chromane.The structure of chromanes is abundant in natural products that possess a broad array of biological activities such as antimicrobial, antiviral, anti-proliferative and antitumor activity. Since chromanes are found in many natural products, efficient construction of this ring structure has attracted much attention in the recent past.Synthesis of Chromane Derivatives via Indium-mediated Intramolecular Allenylation and Allylation to Imines as in scheme 1 is disclosed by Han-Young Kang et al. in Bull. Korean Chem. Soc. 2004, Vol. 25, No. 11, 1627-1628. However, the reported yields are poor in the range of 70-80%.Synthesis of Chromane Derivatives by Palladium-Catalyzed Intramolecular Allylation of Aldehydes with Allylic Acetates or Chlorides using Indium and Indium( III) Chloride as in scheme 2 is reported by Van Cuong Nguyen et al. in Bull. Korean Chem. Soc. 2005, Vol. 26, No. 5, page 711-712. However, the ...

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Номер записи: 95
12-01-2017 дата публикации

Improved glycol acylation process with water-tolerant metal triflates

Номер: US20170008902A1
Автор: Erik Hagberg, Erin ROCKAFELLOW, Kenneth STENSRUD, Stephen Howard
Принадлежит: Archer Daniels Midland Co

A method for acid-catalyzed acylation of an isohexide is described. The method can enable direct alcohol acylation with carboxylic acids. In particular, the method involves reacting an isohexide and an excess of carboxylic acid, in the presence of a water-tolerant Lewis acid catalyst. Water-tolerant Lewis acid catalysts can furnish relatively high diester yields (e.g., ≧55%-60%) at lower catalyst loads. This feature, among others, is highly desirable for cost savings, and can improve process economics.

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Номер записи: 96
14-01-2016 дата публикации

HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME

Номер: US20160009744A1
Автор: Duffey Matthew O., England Dylan, Freeze Scott, Hu Zhigen, Langston Steven, McIntyre Charles, Mizutani Hirotake, Ono Koji, Xu He
Принадлежит: Millennium Pharmaceuticals, Inc.

Disclosed are chemical entities which are compounds of formula (I): 3. The chemical entity of claim 1 , wherein L is —C(R)(R)— claim 1 , —S— claim 1 , —S(O)— claim 1 , —S(O)— claim 1 , —C(O)— claim 1 , —C(═CH)— claim 1 , —C(R)(R)—C(═CH)— claim 1 , —C(R)(R)—C≡C— claim 1 , —C(R)(R)—O— claim 1 , —C(R)(R)—S— claim 1 , —C(R)(R)—N(R)— claim 1 , —C(R)(R)—N(R)—CH— claim 1 , —C(R)(R)—CH— claim 1 , —C(R)(R)—CH—CH— claim 1 , or —C(O)—C(R)(R)—.4. The chemical entity of claim 1 , wherein:{'sub': 1', '2, 'sup': z3', 'z3', 'z3, 'Zis hydrogen, halogen, cyano, R, —S(O)—R, or —S(O)—R;'}{'sup': z3', 'z4, 'sub': '1-4', 'Ris a phenyl, 5- to 7-membered cycloaliphatic, 5- to 7-membered heterocyclyl, or Caliphatic, any of which may be substituted with one or more independently selected R;'}{'sup': z4', 'z5', 'z6', 'z5, 'sub': 1-4', '1-4', '1-4', '1-4', '2', '2, 'Ris hydroxyl, halogen, cyano, Caliphatic, Cfluoroaliphatic, Calkoxy, Cfluoroalkoxy, —N(R), —C(O)R, —C(O)R, 5- or 6-membered cycloaliphatic or heterocyclyl, or a phenyl optionally substituted with one or more independently selected halogens;'}{'sup': 'z5', 'sub': '1-4', 'each occurrence of Ris independently hydrogen or Calkyl; and'}{'sup': 'z6', 'sub': '1-4', 'each occurrence of Ris independently Calkyl.'}5. The chemical entity of claim 4 , wherein Zis hydrogen; halogen; cyano; phenyl optionally substituted with one or more independently selected halogens; 5- to 7-membered cycloaliphatic or heterocyclyl optionally fused to a 6-membered aryl claim 4 , wherein the 5- to 7-membered cycloaliphatic or heterocyclyl optionally fused to a 6-membered aryl is optionally substituted with one or more independently selected halogens; Cfluoroaliphatic; or a Caliphatic group optionally substituted with one or more hydroxyl claim 4 , Calkoxy claim 4 , phenyl optionally substituted with one more independently selected halogens claim 4 , 5- or 6-membered cycloaliphatic claim 4 , 5- or 6-membered heterocyclyl claim 4 , or —N(R).6. The chemical entity ...

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Номер записи: 97
27-01-2022 дата публикации

COMPOUNDS TARGETING MUTANT CALRETICULIN

Номер: US20220024944A1
Автор: Jia Ruochen, Zagrijtschuk Oleh
Принадлежит:

The present invention relates to compounds binding to calreticulin which selectively inhibit growth of CALR mutant cells and/or exhibit selective cytotoxicity towards CALR mutant cells, to pharmaceutical compositions comprising such compounds as well as to their use in treating diseases or conditions caused by or associated with a mutation of CALR, in particular myeloid malignancies, such as myeloproliferative neoplasms or myelodysplasia syndrome. The present invention also relates to screening assays allowing the identification of such compounds. 5. The compound for use of any one of to , wherein each of rings A and B is independently selected from benzo , pyridino , pyrimidino , and hydrated forms thereof , wherein the sum of m1 and m2 is 1 to 7 , preferably the sum of m1 and m2 is 1 , 2 , 3 , 4 , 5 , or 6.7. The compound for use of any one of to , wherein each of Rand Ris independently selected from the group consisting of Calkyl , Calkenyl , Calkynyl , Ccycloalkyl , Caryl , 3- to 7-membered heterocyclyl , 3- to 7-membered heteroaryl , halogen , —CN , —NO , —OH , —O(Calkyl) , —CF , —OCF , —O(CH)(Ccycloalkyl) , —O(CH)(Caryl) , —O(CH)(3- to 7-membered heteroaryl) , —O(CH)(3- to 7-membered heterocyclyl) , —NH , —NH(Calkyl) , —N(Calkyl) , —NHS(O)(Calkyl) , —S(O)NH(Calkyl) , —C(═O)(Calkyl) , —C(═O)OH , —OC(═O)R , —C(═O)O(Calkyl) , —C(═O)NH(Calkyl) , —NHC(═O)H , —NHC(═O)(Calkyl) , —NHC(═NH)NH(Calkyl) , —N(Calkyl)C(═NH)NH(Calkyl) , and —(Calkylene)OH , wherein z is 0 , 1 , or 2; and Ris selected from the group consisting of Calkyl , Ccycloalkyl , Caryl , 3- to 7-membered heterocyclyl , and 3- to 7-membered heteroaryl , and is optionally substituted with one or two independently selected R; and/or any two Rwhich are bound to the same carbon atom of ring A may join together to form ═O and/or any two Rwhich are bound to the same carbon atom of ring B may join together to form ═O and/or any two Ron adjacent ring atoms of ring A may join together with the adjacent ring atoms ...

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Номер записи: 98
11-01-2018 дата публикации

COMPOUND USEFUL FOR MANUFACTURING SALACINOL, METHOD FOR MANUFACTURING THE COMPOUND, METHOD FOR MANUFACTURING SALACINOL, METHODS FOR PROTECTING AND DEPROTECTING DIOL GROUP, AND PROTECTIVE AGENT FOR DIOL GROUP

Номер: US20180009777A1
Автор: FUJINO Yuuta, KATSUMATA Taiji, NAGASE Hisato, NAKAMURA Koki, WATANABE Katsuyuki
Принадлежит: FUJIFILM Corporation

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol. 2. The manufacturing method according to claim 1 ,{'sup': 1a', '1b', '4a', '4b', '4c, 'wherein each of Rand Ris a carboxy protective group, and each of R, R, and Ris a hydrogen atom.'}4. The manufacturing method according to claim 3 ,{'sup': '5', 'wherein Ris a phenyl group which may be substituted.'}5. The manufacturing method according to claim 3 ,{'sup': 1a', '1b', '4a', '4b', '4c, 'wherein each of Rand Ris a carboxy protective group, and each of R, R, and Ris a hydrogen atom.'} The present application is a Divisional of U.S. application Ser. No. 15/268,829, filed Sep. 19, 2016 which is a continuation of PCT/JP2015/58197 filed on Mar. 19, 2015 and claims priority under 35 U.S.C. § 119 of Japanese Patent Application No. 57961/2014 filed on Mar. 20, 2014, the disclosures of which are incorporated herein by referenceThe present invention relates to a compound useful for manufacturing salacinol and a method for manufacturing the compound. The present invention also relates to a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group.In traditional Indian medicine, Salacia reticulata which is a climbing tree of the genus Salacia is used for treating diabetes. Salacinol is a component contained in plants of the genus Salacia such as Salacia reticulata and has a strong α-glucosidase inhibitory activity (Tetrahedron Letters, Vol. 38, No. 48., pp. 8367-8370 (1997)). Salacinol is obtained from, for example, extracts of plants of the genus Salacia (JP3030008B). However, the supply of plants of the genus Salacia is small, and it is difficult to ...

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Номер записи: 99
14-01-2021 дата публикации

Method For Preparing Hexahydrofuro-Furanol Derivative, Intermediate Thereof And Preparation Method Thereof

Номер: US20210009544A1
Автор: Chen Jianhua, Gao Zhaobo, HE Dawei, Lin Jingxin, Ma Xiaodong, Mei Yijiang, Wan Zhidong, XIANG Wei, Zhou Zengle
Принадлежит: Jiangsu Ruike Medical Science And Technology Co., Ltd.

The invention relates to the field of pharmaceutical synthesis, in particular to a preparation method of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives and their intermediates. The preparation method is carried out starting from compound Formula A1. 2. The compound according to is characterized in that the hydroxyl protective group are alkyl claim 1 , silyl claim 1 , acyl of C claim 1 , ring alkenyl of C claim 1 , aryl claim 1 , aralkyl claim 1 , aroyl claim 1 , phenyl and substituted phenyl; the silyl is tetramethyl-silyl claim 1 , trimethyl-silyl claim 1 , triethyl-silyl claim 1 , tri-butyl silyl and tert-butyl dimethyl silyl; the alkyl is alkyl of C-C claim 1 , the aromatic groups are phenyl claim 1 , furan claim 1 , thiophenyl or indole group; the substituted phenyl group is alkyl substituted phenyl group claim 1 , alkoxy alkyl substituted phenyl group claim 1 , nitro alkyl substituted phenyl group or halogen substituted phenyl group; the alkyl substituted phenyl is benzyl claim 1 , diphenyl methyl claim 1 , triphenyl methyl group; the phenyl substituted by the alkoxy alkyl group is p-methoxybenzyl; the substituted phenyl group of the nitro alkyl group is p-nitro benzyl group; the phenyl substituted by the halogen is p-chlorophenyl group.5. (canceled)10. A method for the preparation of (3R claim 3 ,3aS claim 3 ,6aR)-hexahydrofuro[2 claim 3 ,3-b]furan-3-ol claim 3 , is characterized in that the intermediate C-2 or prepared from claim 3 , is prepared by further ring-closing reaction.12. (canceled)16. According to the preparation method mentioned in claim 3 , its characteristic is that the nucleotide sequence of the aldehyde/ketone reductase gene is SEQ ID NO: 2.17. According to the preparation method mentioned in claim 3 , it is characterized in that the aldehyde/ketone reductase is the total cell of genetically engineered bacteria claim 3 , the liquid of crushing enzyme claim 3 , the freeze-dried powder or the immobilized enzyme or immobilized cell.18. ...

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Номер записи: 100