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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 3093. Отображено 100.
02-02-2012 дата публикации

Process for the synthesis of cleistanthin

Номер: US20120029179A1
Автор: Om Vir Singh, Rahul Ganpat Deshmukh, Sarika Madhusudan Tapadiya
Принадлежит: Godavari Biorefineries Ltd

The present invention relates to a process for preparing compound of formula (I) that is Cleistanthin A. The process comprises the steps of reacting compound of formula (II) with compound of formula (III) in the presence of a first solvent, quarternary ammonium salt and first alkali to form compound of formula (IV). The compound of formula (IV) is further treated with a second solvent and a second alkali to form compound of formula (I). The present invention also relates to the preparation of salt of compound of formula (IV) that is Cleistanthin A acetate.

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Номер записи: 1
07-06-2012 дата публикации

Process for preparing pregabalin

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

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

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Номер записи: 2
19-07-2012 дата публикации

Methods and compositions for making antibodies and antibody derivatives with reduced core fucosylation

Номер: US20120183997A1
Автор: Brian Toki, Dennis R. Benjamin, Django Sussman, Patrick J. Burke, Scott C. Jeffrey, Stephen C. Alley
Принадлежит: Seattle Genetics Inc

The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation.

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Номер записи: 3
09-08-2012 дата публикации

Anti-influenza agents

Номер: US20120202877A1
Автор: Jeffrey Clifford Dyason, Mark Von Itzstein, Mauro Pascolutti, Robin Thomson, Santosh Rudrawar
Принадлежит: Griffith University

The present invention relates to compounds that selectively inhibit influenza A virus group (1) sialidases and are therefore potential anti-influenza agents.

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Номер записи: 4
27-12-2012 дата публикации

Peroxide removal from drug delivery vehicle

Номер: US20120330005A1
Автор: Gunjan Junnarkar, John Patrick Carr, Michael A. Desjardin
Принадлежит: Durect Corp

The present invention is related to methods for lowering peroxide levels in sucrose acetate isobutyrate formulations and to composition used in and formed by such methods.

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Номер записи: 5
03-01-2013 дата публикации

Supercooling promoting agent

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

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

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Номер записи: 6
28-03-2013 дата публикации

SIALIC ACID (A-(2-6))-D-AMINOPYRANOSE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF

Номер: US20130079291A1
Автор: YANG Fan, Ye Xinshan, Zheng Xiujing
Принадлежит: PEKING UNIVERSITY

N-acyl modified sialic acid (α-(2→6))-D-aminopyranose derivatives, their synthesis methods and uses are disclosed. Sialic acid (α-(2→6))-D-aminopyranose derivatives represented by formula 1 are synthesized by using D-aminogalactose (glucose) and sialic acid as raw materials, which are coupled with carrier proteins or polypeptides to obtain glycoprotein (glycopeptide) conjugates. Acetyl is replaced by derivative acyl in the structures of said compounds, therefore the compounds show good activity in antitumor vaccines. 2. A glycoconjugate characterized by conjugating the sialic acid-α-(2→6)-D-aminopyranose derivative or salt of to a protein or a polypeptide.3. The sialic acid (α-(2→6))-D-aminopyranose derivative or salt claim 1 , wherein the sialic acid (α-(2→6))-D-aminopyranose derivative or salt is characterized in that the salt is formed with a base.5. The Process of claim 4 , wherein the preparation process is characterized in that the raw materials include allyl 4-O-(5-amino-3 claim 4 ,5-dideoxy-α-neuraminopyranosyl)-2-acetylamino-2-deoxy-α-D-galactopyranoside claim 4 , allyl 4-O-(5-acetylamino-3 claim 4 ,5-dideoxy-α-neuraminopyranosyl)-2-amino-2-deoxy-α-D-galactopyranoside or allyl 4-O-(5-amino-3 claim 4 ,5-dideoxy-α-neuraminopyranosyl)-2-amino-2-deoxy-α-D-galactopyranoside; the carboxylic acid anhydrides include aliphatic carboxylic acid anhydrides claim 4 , with/without fluoro claim 4 , chloro or bromo substituents; that the carboxylic acids include aliphatic acids claim 4 , with/without fluoro claim 4 , chloro or bromo substituents; that the carboxylic esters include aliphatic esters claim 4 , with/without fluoro claim 4 , chloro or bromo substituents; the promoter include organic or inorganic bases; and that the solvents include water or organic solvents.6. The Process of claim 5 , wherein the preparation process is characterized in that the carboxylic acid anhydrides include acetic anhydride claim 5 , propionic anhydride claim 5 , n-butyric anhydride claim ...

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Номер записи: 7
25-07-2013 дата публикации

Curcumin Derivatives

Номер: US20130190256A1
Автор: Alonso Alejandra, Averick Saadyah, Banerjee Probal, Corbo Christopher, Debnath Shawon, DOLAI Sukanta, Mogha Amit, Raja Krishnaswami
Принадлежит: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK

The invention relates to novel curcumin derivatives in which one or two of the phenolic groups have been modified. 2. A curcumin derivative according to claim 1 , with the proviso that if Yis —C≡CH claim 1 , then m1 is 0.3. A curcumin derivative according to claim 1 , with the proviso that if Yis —C≡CH claim 1 , then m2 is 0.7. A curcumin derivative according to claim 6 , wherein the saccharide is a monosaccharide.8. A curcumin derivative according to claim 7 , wherein the monosaccharide is glucose or galactose.12. A curcumin derivative according to claim 11 , wherein the saccharide is a monosaccharide.13. A curcumin derivative according to claim 12 , wherein the monosaccharide is glucose or galactose.14. A curcumin derivative according to claim 1 , wherein Yor Yis a saccharide.15. A curcumin derivative according to claim 1 , wherein Y or Yis a disaccharide or a trisaccharide.16. A curcumin derivative according to claim 1 , wherein the saccharide is a monosaccharide.17. A curcumin derivative according to claim 1 , wherein the monosaccharide is glucose or galactose. This application claims the benefit of U.S. Provisional Application No. 61/308,362, filed Feb. 26, 2010, which is incorporated herein by reference.There is a vital need to find drugs that halt or reverse Alzheimer's disease (AD). AD presently affects 18 million people worldwide. The human and financial costs of AD in the US is expected to exceed $150 billion in 2005. FDA approved medications treat symptoms, but do not alter AD progression.The hallmarks of AD are inter-neuronal plaques consisting of precipitates or aggregates of amyloid beta protein (Aβ), and intra-neuronal neurofibrillary tangles (NFTs) of tau protein. The major target for drug discovery for AD has been Aβ that forms insoluble senile plaques. Although the etiology of AD is not fully understood, the Aβ amyloid cascade hypothesis is the most common view of the pathological pathway of AD in which the generation of Aβ and accumulation of Aβ ...

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Номер записи: 8
01-08-2013 дата публикации

CARBOHYDRATE HAPTEN-BASED ANTI-CANCER VACCINES AND ANTIBODY DRUGS

Номер: US20130195873A1
Автор: LEE Chi-Yu Gregory
Принадлежит: Vancouver Biotech LTD.

Immunogenic compositions that contain haptens consisting of carbohydrate moieties are useful to induce an immune response to provide antibodies to epitopes contained in CA215 and also to elicit an immune response to cancers expressing these epitopes. 1. A compound selected from the group consisting of{'sub': 1', '1', '1', '1, 'GalNAcGlcNAcGalNeuAc;'}{'sub': 1', '1', '2, 'GalNAcGalNeuAc;'}{'sub': 1', '1', '2, 'GalNAcGalNeuGc;'}{'sub': 1', '1', '2', '1, 'GalNAcGlcNAcGalNeuAc; and'}{'sub': 1', '1', '2, 'GalNAcGlcNAcGalNeuGc.'}12. An immunogenic composition that contains as part of an immunogen at least one hapten consisting of a compound set forth inwherein said hapten is coupled to a heterologous protein and/or wherein the composition contains an adjuvant.13. (canceled)14. An immunogenic composition that contains at least one of the compounds set forth in in combination with at least one compound selected from the group consisting of{'sub': 5', '3', '2, 'GlcNAcManHex;'}{'sub': 2', '3, 'GlcNAcMan;'}{'sub': 4', '3', '2', '1', '1, 'GlcNAcManHexFucNeuGc;'}{'sub': 5', '3', '2', '1, 'GlcNAcManHexNeuGc;'}{'sub': 4', '3', '2', '2, 'GlcNAcManHexNeuGc;'}{'sub': 5', '3', '3', '1, 'GlcNAcManHexNeuGc;'}{'sub': 6', '3', '4, 'GlcNAcManHex;'}{'sub': 4', '3', '2', '1', '2, 'GlcNAcManHexFucNeuGc;'}{'sub': 2', '5, 'GlcNAcMan;'}{'sub': 3', '3', '1, 'GlcNAcManHex; and'}{'sub': 2', '6, 'GlcNAcMan.'}1516-. (canceled)17. The composition of wherein said compounds are coupled to positions corresponding to glycosylation sites present in an Fab region.18. A method to induce an immune response directed to a tumor in a subject bearing a cancer that expresses an epitope that comprises a moiety selected from the group consisting of{'sub': 1', '1', '1', '1, 'GalNAcGlcNAcGalNeuAc;'}{'sub': 1', '1', '2, 'GalNAcGalNeuAc;'}{'sub': 1', '1', '2, 'GalNAcGalNeuGc;'}{'sub': 1', '1', '2', '1, 'GalNAcGlcNAcGalNeuAc; and'}{'sub': 1', '1', '2, 'GalNAcGlcNAcGalNeuGc'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1 ...

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Номер записи: 9
08-08-2013 дата публикации

CHEMICAL DERIVATIVES OF JASMONATE, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20130203689A1
Автор: Flescher Eliezer, Herzberg Max, Ksshman Yoel
Принадлежит:

The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers. 2. The compound of claim 1 , wherein the heteroaryloxy is unsubstituted or substituted with one or more alkyl groups.3. The compound of claim 1 , wherein Ris quinolinyloxy.4. The compound of claim 1 , wherein Rand Rtogether with the carbons to which they are attached form a C-Ccycloalkyl substituted by halo.5. The compound of claim 1 , wherein Ris oxo.6. The compound of claim 1 , wherein the bond between Cand Cis a double bond claim 1 , and R claim 1 , R claim 1 , R claim 1 , Rand Rare each hydrogen.7. The compound of claim 1 , wherein the bond between Cand Cis a single bond claim 1 , and R claim 1 , R claim 1 , R claim 1 , Rand Rare each hydrogen.8. The compound of claim 1 , wherein Rrepresents an oxygen atom which is bonded to C claim 1 , thereby forming an oxygen-containing 5-membered heterocyclic ring.10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier claim 1 , and as an active ingredient a compound according to .11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier claim 9 , and as an active ingredient a compound according to .12. The pharmaceutical composition of claim 10 , wherein the composition is in a form suitable for topical administration claim 10 , oral administration claim 10 , intravenous administration by injection claim 10 , administration by inhalation claim 10 , or administration via a suppository.13. A method for inhibiting cancer cell proliferation claim 1 , comprising contacting said cancer cells with a therapeutically effective amount of a compound according to .14. A method for inhibiting cancer cell proliferation claim 9 , comprising contacting said cancer cells with a therapeutically effective amount of a ...

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Номер записи: 10
05-09-2013 дата публикации

POLYETHERESTER POLYOLS AND THE USE THEREOF FOR PRODUCING RIGID POLYURETHANE FOAMS

Номер: US20130231413A1
Автор: Eling Berend, FRICKE Marc, KOCH Sebastian, Koenig Christian, Kunst Andreas, SCHUETTE Markus
Принадлежит:

The invention relates to a polyetherester polyol comprising the reaction product of 1. A polyetherester polyol comprising the reaction product ofa1) 5 to 63 wt % of one or more polyols or polyamines or mixtures thereof having an average functionality of 2.5 to 8,a2) 2 to 50 wt % of one or more fatty acids, fatty acid monoesters or mixtures thereof,a3) 35 to 70 wt % of one or more alkylene oxides of 2 to 4 carbon atoms.2. The polyetherester polyol according to wherein the polyols or polyamines of component a1) are selected from the group consisting of sugars claim 1 , pentaerythritol claim 1 , sorbitol claim 1 , trimethylolpropane claim 1 , glycerol claim 1 , tolylenediamine claim 1 , ethylenediamine claim 1 , ethylene glycol claim 1 , propylene glycol and water.3. The polyetherester polyol according to wherein said component a1) comprises a mixture of glycerol and sucrose.4. The polyetherester polyol according to wherein said component a2) comprises oleic acid claim 2 , stearic acid claim 2 , palmitic acid claim 2 , linolenic acid claim 2 , their monoesters or mixtures thereof.5. The polyetherester polyol according to wherein the alkylene oxide of component a3) is propylene oxide.6. The polyetherester polyol according to wherein it has an OH number of 200 to 700 mg KOH/g.7. The polyetherester polyol according to wherein it has a functionality of 2.5 to 8.8. A process for producing rigid polyurethane foams by reaction ofA) organic or modified organic polyisocyanates or mixtures thereof,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'B) one or more polyetherester polyols according to ,'}C) optionally further polyester polyols,D) optionally polyetherol polyols,E) one or more blowing agents,F) catalysts, andG) optionally further auxiliaries and/or additives.9. A rigid polyurethane foam obtainable by the process according to .10. A polyol mixture comprising as components{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'B) one or more polyetherester polyols according ...

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Номер записи: 11
26-09-2013 дата публикации

TANNIN INHIBITORS OF HIV

Номер: US20130252909A1
Автор: Kraus George A., Maury Wendy
Принадлежит: UNIVERSITY OF IOWA RESEARCH FOUNDATION

The invention provides a method to prevent or treat HIV-infection with synthetic tannins, and pharmaceutical compositions comprising synthetic tannins. 2. The method of wherein n is 1 claim 1 , m is 1 claim 1 , and p is 1.3. The method of wherein Ris CH.4. The method of wherein Rand Rare G or H.5. The method of wherein Ris G or H.6. The method of wherein Ris H or G and Ris H or G.7. The method of wherein Rand Rare H.8. The method of wherein Ris H.11. The method of wherein n is 0.13. The method of wherein Ror Ris CH.14. The method of wherein Rand/or Rare G.15. The method of wherein n is 1 claim 1 , m is 0 and p is 0.17. The method of wherein Rand/or Rare G.18. The method of wherein Ror Rare CH.20. The method of wherein Ris G.21. The method of wherein Rand Rare H.23. The method of wherein Rand/or Rare G.24. The method of wherein Ris H. This application claims priority of U.S. provisional patent application Ser. No. 61/614,792, filed Mar. 23, 2012, which is incorporated by reference herein.This invention was made with the support of the National Institutes of Health under Grant No. P50 AT004155. The U.S. Government has certain rights in the invention.With more than 33 million people currently infected with human immunodeficiency virus (HIV) and 2 million additional individuals infected each year, there is a worldwide imperative to reduce transmission of this deadly virus. Worldwide, sexual transmission is the primary route of new virus infections. Strategies to reduce spread of this virus can be achieved by reducing virus loads in currently infected individuals (and thereby reducing levels of virus exposure) and/or by blocking sexual transmission by the use of effective and safe microbicides.Clinically useful anti-retrovirals target a number of steps of the HIV-1 life cycle including co-receptor (CCR5) binding, virus membrane/cellular membrane fusion, reverse transcription, integration and proteolytic processing. See, e.g. Martins et al., 15, 1083 (2008). Combination ...

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Номер записи: 12
17-10-2013 дата публикации

TRISACCHARIDE DERIVATES, AND THEIR USE AS ADJUVANTS

Номер: US20130273082A1
Автор: Hof Robert Patrick, Kriek Maria Aldegonda Jacoba, Schaaper Wilhelmus Martinus Maria, Schenkelaars Everardus Joannes Peter Maria, Turkstra Jouwert Anne, Van Bree Johannes Gernardus Mathias Marie
Принадлежит: IMMUNOVO B.V.

The present invention relates to the use of trisaccharide derivates comprising a substituted trisaccharide core, which trisaccharide core is fully substituted with fatty acid ester groups, and optionally one or more anionic groups as adjuvants, to the trisaccharide derivates as such, to a method for preparing such trisaccharides, to trisaccharides obtained with such method, to adjuvant compositions comprising such trisaccharide derivates and to a vaccine or kit comprising such adjuvant compositions. 138-. (canceled)39. An adjuvant composition comprising:a trisaccharide derivate as the adjuvant, which derivate comprises a substituted trisaccharide core, which trisaccharide core is fully substituted with fatty acid ester groups, and optionally one or more anionic groups; andat least one of a pharmaceutical acceptable excipient and diluent.40. The adjuvant according to claim 39 , wherein the substituted trisaccharide core is derived from raffinose claim 39 , melezitose claim 39 , maltotriose claim 39 , nigerotriose claim 39 , maltotriulose or kestose claim 39 , preferably raffinose claim 39 , melezitose or maltotriose claim 39 , most preferably raffinose or maltotriose.41. The adjuvant according to claim 39 , wherein the substituted trisaccharide core comprises one or two sulphate ester or phosphate ester groups as anionic groups.42. The adjuvant according to claim 41 , wherein the anionic group is a sulphate ester.43. The adjuvant according to claim 39 , wherein the fatty acid ester group is an ester of a straight claim 39 , branched claim 39 , saturated or unsaturated fatty acid with a chain length of 4 to 20 carbon atoms.44. The adjuvant according to claim 39 , wherein the fatty acid ester is the ester of lauric acid claim 39 , myristic acid claim 39 , palmitic acid claim 39 , stearic acid or arachidic acid.45. The adjuvant according to claim 39 , wherein the fatty acid ester groups of the substituted trisaccharide core are all identical.46. The adjuvant according ...

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Номер записи: 13
17-10-2013 дата публикации

DISACCHARIDE SYNTHETIC LIPID COMPOUNDS AND USES THEREOF

Номер: US20130273149A1
Автор: Burgess Stephen W., Hickman David T., LI Shengrong, Lopez-Deber Maria Pilar, Shaw Walter A.
Принадлежит:

Essentially pure compounds of the formulas (I) to (XX) are provided. Compositions and methods for enhancing or stimulating an immune response are also provided. The compounds, provided are advantageous in that the compounds are essentially pure and free from contaminants encountered when such compounds are purified from natural sources. 3. The essentially pure compound of claim 2 , wherein AA claim 2 , and Aare each independently Cto Cunsubstituted alkyl and Aand Aare each independently are Cto Cunsubstituted alkyl.6. The essentially pure compound of claim 5 , wherein AA claim 5 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.9. The essentially pure compound of claim 8 , wherein AA claim 8 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.11. The essentially pure compound of claim 1 , wherein the compounds is at least 95% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.12. The essentially pure compound of claim 5 , wherein the compounds is at least 99% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.15. The pharmaceutical composition of claim 14 , wherein AA claim 14 , and Aare each independently Cto Cunsubstituted alkyl and Aand Aare each independently are Cto Cunsubstituted alkyl.18. The pharmaceutical composition of claim 17 , wherein AA claim 17 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.21. The pharmaceutical composition of claim 20 , wherein AA claim 20 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.23. The pharmaceutical composition of claim 13 , wherein the compounds is at least 95% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.24. The pharmaceutical composition of claim 13 , wherein the compounds is at least 99% pure with respect to the synthetic ...

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Номер записи: 14
21-11-2013 дата публикации

Capillary Electrophoresis Method for Fine Structural Analysis of Enoxaparin Sodium

Номер: US20130309655A1
Автор: Jingwu Kang, Xueqiang Zhan
Принадлежит: HANGZHOU JIUYUAN GENE ENGR CO Ltd, Shanghai Institute of Organic Chemistry of CAS

A capillary electrophoresis method for quantitatively analyzing characteristic oligosaccharide present in enoxaparin sodium is provided in this invention. The method may be used for quantitatively determining the contents of disaccharides, trisaccharides, tetrasaccharides and in particular oligosaccharides having a 1,6-anhydro ring, which are unique compounds for enoxaparin sodium, within an exhaustively digested enoxaparin sodium sample with a mixture of heparinase I, II, and III, so as to quantitatively determine the molar percentage of oligosaccharides having 1,6-anhydro ring in enoxaparin sodium. The method may be used for the pharmaceutical quality control of enoxaparin sodium during the manufacturing process.

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Номер записи: 15
12-12-2013 дата публикации

TREHALOSE DERIVATIVES, PREPARATION METHOD AND USES THEREOF

Номер: US20130331346A1
Автор: Jiang Yongli, LIU Zhaopeng
Принадлежит: JOYOCHEM CO., LTD

The invention relates to trehalose derivatives with general formula (I), a preparation method and uses thereof, wherein 6,6′-bis(2,3-dimethoxybenzoyl)-α,α-D-trehalose has anti-colon cancer 26-L5 cell invasion activity which is better than that of a natural product Brartemicin, ICis 0.10 μg/mL (0.15 μM), and when the ICis 10 μg/mL, 6,6′-bis(2,3-dimethoxybenzoyl)-α,α-D-trehalose has no cytotoxicity, shows high-selectivity anti-tumor invasion activity and can be used for preparing medicaments for preventing and treating invasion and metastasis of colon cancer and the like. 2. The trehalose derivatives according to claim 1 , wherein the trehalose derivatives include one of the following compounds:6,6′-bis(2-methoxybenzoyl))-α,α-D-trehalose (3a),6,6′-bis(4-methoxybenzoyl))-α,α-D-trehalose (3c),6,6′-bis(2,3-dimethoxybenzoyl))-α,α-D-trehalose (3e),6,6′-bis(2,6-difluorobenzoyl))-α,α-D-trehalose (3f),6,6′-bis(3-methoxy-4-fluorobenzoyl))-α,α-D-trehalose (3h) or6,6′-bis(3,4,5-trimethoxybenzoyl))-α,α-D-trehalose (3l).4. The preparation method of the trehalose derivatives according to claim 3 , wherein the substituted benzoic acid in step (1) is 2-methoxybenzoic acid claim 3 , 4-methoxybenzoic acid claim 3 , 2 claim 3 ,3-dirnethoxybenzoic acid claim 3 , 2 claim 3 ,6-difluorobenzoic acid claim 3 , 3-methoxy-4-fluorobenzoic acid or 3 claim 3 ,4 claim 3 ,5-trimethoxybenzoic acid.5. The preparation method of the trehalose derivatives according to claim 3 , wherein the solvent in step (1) is tetrahydrofuran or methylene dichloride.6. The preparation method of the trehalose derivatives according to claim 3 , wherein the Mitsunobu reagent in step (1) is diisopropyl azodicarboxylate (DIAD).7. The preparation method of the trehalose derivatives according to claim 3 , wherein the solvent in step (2) is an ethyl acetate-ethanol mixed solution in the volume ratio of 1:1 claim 3 , and the catalyst is 10% palladium/carbon.8. (canceled)9. A pharmaceutical composition against colon cancer 26-L5 ...

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Номер записи: 16
30-01-2014 дата публикации

ANTI-CHOLESTEROLEMIC COMPOUNDS AND METHODS OF USE

Номер: US20140031304A1
Автор: Butler Mark S., Chatterjee Subroto, Somanadhan Brinda
Принадлежит:

The present invention provides novel compounds with hypocholesteremic activity from crude (EO) extracts and methods of use. The invention also provides nutraceuticals. 1. (canceled)2. A method for preventing or treating inflammation in a subject comprising administering to the subject an effective amount of one or more gallic acid derivatives , thereby preventing or treating inflammation in the subject.3. A method for preventing or treating a stress response in a subject comprising administering to the subject an effective amount of one or more gallic acid derivatives , thereby preventing or treating a stress response in the subject.4. The method of claim 2 , wherein the one or more gallic acid derivatives is administered as a nutraceutical.5. The method of claim 2 , wherein the one or more gallic acid derivatives are selected from the group consisting of: methyl gallate claim 2 , ethyl gallate claim 2 , glycerol-1-gallate claim 2 , glucose-1-gallate (GG1) claim 2 , glucose-6-gallate (GG6) claim 2 , glucose-1 claim 2 ,6-digallate (DGG16) claim 2 , mucic acid-2-gallate claim 2 , 1-methyl mucate-2-gallate claim 2 , mucic acid 1 claim 2 ,4-lactone 5-gallate claim 2 , geraniin claim 2 , corilagin claim 2 , chebilc acid claim 2 , and m-digallic acid with minor p-digallic acid.6. The method of claim 5 , wherein the one or more gallic acid derivatives are selected from the group consisting of: Compound 4+Compound 5+Compound 2a claim 5 , Compound 4+Compound 8+Compound 2a claim 5 , Compound 4+Compound 5+Compound 7 claim 5 , Compound 4+Compound 2a claim 5 , Compound 4+Compound 2b claim 5 , Compound 7+Compound 2b claim 5 , Compound 5+Compound 8 claim 5 , and Compound 5+Compound 7.714.-. (canceled)15. The method of claim 2 , wherein the at least one gallic acid derivative is present in an amount from about 10 mg-500 mg.16. The method of claim 15 , wherein the at least one gallic acid derivative is present in an amount from about 40 mg-200 mg.17. The method of claim 2 , further ...

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Номер записи: 17
30-01-2014 дата публикации

METHODS AND COMPOSITIONS FOR MAKING ANTIBODIES AND ANTIBODY DERIVATIVES WITH REDUCED CORE FUCOSYLATION

Номер: US20140031536A1
Автор: ALLEY STEPHEN C., Benjamin Dennis R., Burke Patrick J., Jeffrey Scott C., Sussman Django, Toki Brian
Принадлежит: Seattle Genetics, Inc.

The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation. 2. The culture medium of wherein Ris selected from the group consisting of —C≡CH claim 1 , —C≡CCH claim 1 , C(O)OCH claim 1 , —CHCN claim 1 , and —CHBr.3. The culture medium of wherein Ris —C≡CH and R-Ris —OAc.4. The culture medium of claim 1 , which is free of added animal protein.5. The culture medium of claim 1 , which is free of serum.6. The culture medium of claim 1 , which is free of added fucose.7. The culture medium of claim 1 , which is a powder.8. The culture medium of claim 1 , which is a liquid.9. The culture medium of claim 1 , wherein each of R-Ris independently selected from the group consisting of —OH and —OC(O)C-Calkyl.10. The culture medium of claim 1 , wherein each of R-Ris independently selected from the group consisting of —OH and —OAc.11. The culture medium of claim 1 , wherein Ris selected from the group consisting of —C≡CH and —C≡CCH.12. The culture medium of claim 1 , wherein Ris —C(O)OCH claim 1 , —CHCN claim 1 , or —CHBR.13. The culture medium of wherein the effective amount is an amount of the analog that is sufficient to decrease fucose incorporation into a complex N-glycoside-linked sugar chain of an antibody or antibody derivative by at least 90%.14. The culture medium of claim 1 , which:(i) is free of added animal protein;(ii) is free of serum;(iii) is free of added fucose; and(iv) is a powder or a liquid.15. The culture medium of claim 13 , which:(i) is free of added animal protein;(ii) is free of serum;(iii) is free of added fucose; and(iv) is a powder or a liquid.16. The culture medium of wherein the effective amount is an amount of the analog that is sufficient to decrease fucose incorporation into a complex N-glycoside-linked sugar chain of an antibody or antibody derivative by at least 90%.17. The culture medium of wherein the antibody or antibody derivative is a humanized or human antibody or ...

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Номер записи: 18
13-02-2014 дата публикации

N-SUBSTITUTED MANNOSAMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE

Номер: US20140046051A1
Автор: Dekany Gyula, Hederos Markus, Jánosi Ágnes, Röhrig Christoph, Vrasidas Ioannis
Принадлежит: GLYCOM A/S

A compound of the formula (1) wherein Ris a group removable by hydrogenolysis, and wherein Ris OH or Ris —NHRwherein Ris a group removable by hydrogenolysis. The compound can be made from fructose by a Heyns-rearrangement. The compound can be used then to make free D-mannosamine or its salts, D-mannosamine building blocks and mannosamine containing oligo- or polysaccharides, N-acetyl-D-mannosamine and its hydrates and solvates, neuraminic acid derivatives, and viral neuraminidase inhibitors. 4. A method for the preparation of a compound of formula 1B of claim 3 , comprising the steps: a) treating -fructose with R—NHand a salt thereof claim 3 , and b) separating the compound of formula 1B from the reaction mixture.5. The method according to claim 4 , wherein R—NHis benzyl amine.6. A method for the preparation of a compound of formula 1A of claim 2 , comprising the steps of: a) treating -fructose with R—NHto yield a fructosyl amine derivative; b) isolating the fructosyl amine derivative as a crude product by separating excess R—NHfrom it; and c) treating the crude fructosyl amine derivative with acid.7. The method according to claim 6 , wherein R—NHis benzyl amine claim 6 , and the reaction in step c) is conducted in methanol in the presence of glacial acetic acid.8. A method for the preparation of a compound of formula 1A of claim 6 , comprising the steps of: a) making a compound of formula 1B from D-fructose according to ; and b) and treating a compound of 1B with acid to remove the —NHRgroup.9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. A method of synthesizing D-mannosamine or a salt thereof claim 4 , comprising the steps of: a) making a compound of formula 1B from D-fructose by the method according to ; and b) hydrogenolysis of the compound of formula 1B to remove the groups Rand R.14. (canceled)15. (canceled)16. (canceled)17. A method of synthesizing N-acetyl-D-mannosamine claim 4 , comprising the steps of:{'claim-ref': {'@idref': 'CLM-00013', ' ...

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Номер записи: 19
20-02-2014 дата публикации

COMPOUNDS AND METHODS FOR CHEMICAL AND CHEMO-ENZYMATIC SYNTHESIS OF COMPLEX GLYCANS

Номер: US20140051603A1
Автор: BOONS Geert-Jan, Wang Zhen
Принадлежит: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC

The present invention provides chemical and chemo-enzymatic methods for the synthesis of a wide array of complex asymmetric multi-antennary glycans. 2. The orthogonally protected oligosaccharide of further comprising a glycosidically linked glucosamine moiety in place of X claim 1 , wherein the ring hydroxyls on the glucosamine moiety are protected claim 1 , wherein the amine at the C-2 position of the glucosamine moiety is protected claim 1 , and wherein the anomeric position at the reducing end of the glucosamine moiety comprises X as in formula (I).3. The orthogonally protected oligosaccharide of further comprising a glycosidically linked glucosamine disaccharide in place of X claim 1 , wherein the ring hydroxyls on the glucosamine disaccharide are protected claim 1 , wherein the amines at both C-2 positions of the glucosamine disaccharide are protected claim 1 , and wherein the anomeric position at the reducing end of the glucosamine disaccharide comprises X as in formula (I).4. The orthogonally protected oligosaccharide of comprising a glycosidically linked fucose moiety at position C-6 of the terminal reducing glucosamine.5. The orthogonally protected oligosaccharide of wherein the orthogonal protecting group is selected from the group consisting of levulinoyl (Lev); 9-fluorenylmethoxycarbonyl (Fmoc); allyloxycarbonyl (Alloc); 2-naphthylmethyl (Nap); 1-naphthylmethyl (1-Nap); benzoyl (Bz); difluorobenzoyl (dfBz); pivaloyl levulinoyl (PivLev); pivaloyl benzoyl (PivBz); para-methoxybenzyl ether (PMB); methoxy phenyl ether (MP); allyl ether (Allyl); chloroacetyl ester (ClAc); trichloroacetyl ester (ClAc) claim 1 , trifluoroacetyl ester (FAc); and a silyl ether.6. An orthogonally protected oligosaccharide comprising an orthogonally protected oligosaccharide of .7. A method for making an oligosaccharide comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'deprotecting the orthogonally protected oligosaccharide of by removing an orthogonal protecting group ...

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Номер записи: 20
27-02-2014 дата публикации

Catalytic hydrogenolysis of a composition of a mixture of oligosaccharide precursors and uses thereof

Номер: US20140057868A1
Автор: Andreas Schroven, Elise Champion, Gyula Dekany, Sandor Demko
Принадлежит: Glycom AS

A method for the manufacture of a mixture of human milk oligosaccharides is disclosed. The method involves the catalytic hydrogenolysis of compounds of the general formula 1 and 2. The use of compounds of general formula 1 and 2 in the manufacture of human milk oligosaccharides is also disclosed.

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Номер записи: 21
27-03-2014 дата публикации

POLYPHOSPHATE AND PYROPHOSPHATE DERIVATIVE OF SACCHARIDES

Номер: US20140088036A1
Автор: Brockman Adam H., Hey John, Jogireddy Rajamalleswaramma, Lehn Jean Marie, NICOLAU Yves Claude, Yu Yongxin
Принадлежит:

The present invention provides, among other things, phosphorylated and pyrophosphate derivatives of mono-, di- and oligosaccharides, as well as structural derivatives of these compounds. These compounds have a variety of uses including for pharmaceutical applications. Also provided are methods of use in the treatment of disease, including diseases related to oxygen delivery. 1. A pharmaceutical composition comprising a compound that is a polyphosphate or pyrophosphate derivative of a mono- , di- or oligosaccharide containing a pyranose or furanose unit , or a pharmaceutically acceptable salt thereof.2. The pharmaceutical composition of claim 1 , wherein the compound is a phosphate or polyphosphate derivative of glucose claim 1 , mannose claim 1 , or galactose.3. The pharmaceutical composition of or claim 1 , wherein the pyranose is part of an oligosaccharide comprising from 2 to 4 monosaccharide units.4. The pharmaceutical composition of claim 3 , wherein the oligosaccharide is a phosphate or polyphosphate derivative of sucrose or lactose.5. The pharmaceutical composition of any one of to claim 3 , wherein the compound comprises from 2 to about 10 phosphate or polyphosphate groups.6. The pharmaceutical composition of any one of to claim 3 , wherein the compound comprises 2 to about 10 pyrophosphate groups.7. The pharmaceutical composition of any one of to claim 3 , wherein the composition comprises at least one pyrophosphate that is an internal pyrophosphate ring.8. The pharmaceutical composition of any one of to claim 3 , wherein the pyranose further comprises a derivatized hydroxyl selected from alkoxy (—OR) or acyloxy (—OCOR) claim 3 , where R is selected from alkyl claim 3 , aryl claim 3 , acyl claim 3 , aralkyl claim 3 , alkenyl claim 3 , alkynyl claim 3 , heterocyclyl claim 3 , polycyclyl claim 3 , carbocycle claim 3 , amino claim 3 , acylamino claim 3 , amido claim 3 , alkylthio claim 3 , carbonyl claim 3 , sulfonate claim 3 , alkoxyl claim 3 , sulfonyl claim ...

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Номер записи: 22
07-01-2016 дата публикации

METHOD FOR PRODUCING a-HALO-TETRAACYL-GLUCOSE

Номер: US20160002276A1
Автор: HATSUDA Masanori, HYODO Isao, TANIMOTO Kouichi, UEDA Keita
Принадлежит: MITSUBISHI TANABE PHARMA CORPORATION

There is provided an efficient and excellent preparation method of an α-halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the α-halo-tetraacyl-glucose represented by the formula (III): 2. The method according to claim 1 , wherein the method comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative derived from a carboxylic acid represented by the formula (IV) in the presence of a metal halide represented by the formula:{'br': None, 'MX'}wherein M represents an alkali metal, and X represents a halogen atom, a Lewis acid catalyst and a phase-transfer catalyst.3. The method according to claim 2 , wherein the reactive derivative derived from the carboxylic acid (IV) is an acid halide claim 2 , and R of the acid halide is an optionally substituted methyl claim 2 , t-butyl or an optionally substituted phenyl.4. The method according to or claim 2 , whereinthe metal halide MX is selected from the group consisting of lithium halide and sodium halide,the Lewis acid catalyst is selected from the group consisting of zinc halide, cobalt halide, bismuth halide, iron halide, titanium halide and aluminum halide, andthe phase-transfer catalyst is a crown ether.5. The method according to claim 3 , wherein R of the acid halide derived from the carboxylic acid (IV) is t-butyl and the halogen atom X of the metal halide MX is a chlorine atom or a bromine atom.6. The method according to claim 2 , whereinthe metal halide MX is lithium bromide or sodium bromide,the Lewis acid catalyst is selected from the group consisting of zinc bromide, cobalt bromide and bismuth bromide, andthe crown ether is 12-crown-4 or 15-crown-5.7. The method according to claim 1 , wherein the method comprises reacting D-glucose or lower alkyl D-glucoside with pivaloyl chloride in the presence of sodium bromide claim 1 , zinc bromide ...

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Номер записи: 23
04-01-2018 дата публикации

Crystal of ammonium n-acetylneuraminate anhydrate, and process for producing same

Номер: US20180002364A1
Автор: Kazunari Fukumoto
Принадлежит: Kyowa Hakko Bio Co Ltd

According to the present invention, a crystal of ammonium N-acetylneuraminate anhydrate, and a process for producing a crystal of ammonium N-acetylneuraminate anhydrate, comprising adding or adding dropwise a solvent selected from the group consisting of alcohols and ketones to an aqueous N-acetylneuraminic acid solution containing an ammonium-containing compound and having a pH of 3.0 to 9.0 to precipitate a crystal of ammonium N-acetylneuraminate anhydrate, and collecting the crystal of ammonium N-acetylneuraminate anhydrate from the aqueous solution, can be provided.

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Номер записи: 24
07-01-2021 дата публикации

TRITERPENE SAPONIN ANALOGUES

Номер: US20210002316A1
Автор: CHEA Eric, FERNANDEZ-TEJADA Alberto, GARDNER Jeffrey, Gin David Y., Lewis Jason, LIVINGSTON Philip, MARTIN J. Tyler, NORDSTROEM Lars, Pillarsetty Naga Vara Kishore, Ragupathi Govind, TAN Derek
Принадлежит:

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases. 3. The pharmaceutical composition according to claim 2 , wherein the antigen is associated with a bacteria or virus.4pertussisBorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. The pharmaceutical composition according to claim 3 , wherein the antigen is associated with a bacterial or virus causing a disease selected from the group consisting of Hepatitis B claim 3 , pneumococcus claim 3 , diphtheria claim 3 , tetanus claim 3 , claim 3 , or Lyme disease including the closely related spirochetes of the genus such as claim 3 , claim 3 , and5. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with Hepatitis B virus.6bacterium.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with pneumococcus7Corynebacterium diphtheria bacterium.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with8Clostridium tetani bacterium.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with9Bordetella pertussis bacterium.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with10bacteriumBorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with a causing Lyme disease or a spirochete of the genus selected from the group consisting of claim 4 , and12. The method according to claim 11 , wherein the antigen is an antigen associated with a bacteria or a virus.13pertussisBorreliaB. burgdorferi, B. ...

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Номер записи: 25
07-01-2021 дата публикации

Method for synthesizing sucrose-6-ester

Номер: US20210002317A1
Автор: JIANG Cai, Kaifeng MA, Xiaoqiao Wei, Yougui Zhou, Yugang Wang, Yunhan YANG
Принадлежит: Shandong Xinhecheng Fine Chemical Technology Co Ltd, Zhejiang NHU Co Ltd

A method for synthesizing sucrose-6-ester includes: (a) in the presence of a polar aprotic solvent, contacting an organic phosphine compound represented by formula I with sucrose and an organic tin compound; (b) removing water to obtain a reaction liquid containing a tin-sucrose adduct; and (c) contacting the reaction liquid containing the tin-sucrose adduct with an acid anhydride compound to prepare a sucrose-6-ester. In formula I, R1, R2, and R3 each are a linear or branched alkyl having 1 to 20 carbon atoms, a cycloalkyl having 3 to 10 carbon atoms, or an aryl having 6 to 10 carbon atoms; moreover, the R1, R2, and R3 are identical groups, partially identical groups, or different groups from each other. According to the method, the reaction conversion rate and selectivity are greatly improved; moreover, it is easy to realize industrial application.

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Номер записи: 26
11-01-2018 дата публикации

Dually Derivatized Chitosan Nanoparticles and Methods of Making and Using the Same for Gene Transfer In Vivo

Номер: US20180008720A1
Автор: CHEUNG Anthony, Gao Jun, Hsu Eric
Принадлежит:

Provided herein is chitosan dually derivatized with arginine and gluconic acid; and methods of making and using the same, e.g., for gene delivery in vivo. 114.-. (canceled)15. A method of treating diabetes comprising administering a therapeutically effective amount of a therapeutic nucleic acid encoding insulin , a glucagon antagonist , GLP-1 or leptin to a target tissue in a patient , wherein said administering comprises contacting said target tissue with a dually derivatized (DD) chitosan nucleic acid polyplex , said DD chitosan nucleic acid polyplex comprising a chitosan-derivative nanoparticle comprising chitosan coupled with gluconic acid and arginine , and said therapeutic nucleic acid.16. A method of treating inflammatory bowel disease comprising administering a therapeutically effective amount of a therapeutic nucleic acid encoding IL-10 , a TNFα antagonist , or an IL-17 antagonist to a target tissue in a patient , wherein said administering comprises contacting said target tissue with a dually derivatized (DD) chitosan nucleic acid polyplex , said DD chitosan nucleic acid polyplex comprising a chitosan-derivative nanoparticle comprising chitosan coupled with gluconic acid and arginine , and said therapeutic nucleic acid.17. A method of treating of obesity comprising administering a therapeutically effective amount of a therapeutic nucleic acid encoding leptin , cholecystokinin , PYY or GLP-1 to a target tissue in a patient , wherein said administering comprises contacting said target tissue with a dually derivatized (DD) chitosan nucleic acid polyplex , said DD chitosan nucleic acid polyplex comprising a chitosan-derivative nanoparticle comprising chitosan coupled with gluconic acid and arginine , and said therapeutic nucleic acid.18. The method according to , , or , wherein said nanoparticle comprises arginine at a concentration of about 10% to about 55%.19. The method according to claim 18 , wherein said nanoparticle comprises gluconic acid at an initial ...

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Номер записи: 27
08-01-2015 дата публикации

Methods for making biocompatible polymerizable acrylate products

Номер: US20150011747A1
Автор: Gregory D. Phelan, Phillip A. Sullivan, William B. Carlson
Принадлежит: EMPIRE TECHNOLOGY DEVELOPMENT LLC

Sugar-acrylic monomers are synthesized to have a carbohydrate moiety linked to an acrylate group. The sugar-acrylic monomers may be polymerized to form polymers, adhesives, hydrogels, and the like. The sugar-acrylic monomers and polymers may be used in tissue engineering, adhesives and sealers, wound healing, and the like.

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Номер записи: 28
10-01-2019 дата публикации

TRITERPENE SAPONIN VARIANTS, METHODS OF SYNTHESIS AND USE THEREOF

Номер: US20190010181A1
Автор: FERNANDEZ-TAJADA Alberto, Gin David Y., Ragupathi Govindaswami, TAN Derek S., WALKOWICZ William E.
Принадлежит:

A number of triterpene saponin variants with different modifications on their central glycosyl ester linkage are described. Also described are methods of making and method of using such triterpene saponin variants. 6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein G is hydrogen.13. A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound of or a pharmaceutically acceptable salt thereof;'}an immunologically effective amount of an antigen; anda pharmaceutically acceptable excipient.14. A method for immunizing a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00013', 'claim 13'}, 'administering to the subject an effective amount of the pharmaceutical composition of .'}15. A method for treating a disorder in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00014', 'claim 14'}, 'administering to the subject an effective amount of the pharmaceutical composition of ,'}wherein the disorder is cancer, an infectious disease or a neurodegenerative disorder. The present application claims priority under 35 U.S. C. § 119(e) to U.S. provisional application U.S. 62/268,837, filed Dec. 17, 2015, the contents of which are incorporated herein by reference.This invention was made with government support under R01 AI085622, R01 GM058833 and P30 CA008748 awarded by National Institutes of Health. The government has certain rights in the invention.The present invention generally relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. More specifically, the invention relates to saponin variants with central glycosidic linkage modifications that exhibit distinct conformations and adjuvant activities.Most of the immunological adjuvants are emulsions that stimulate an immune response, which have shown valuable potentials in the development of vaccines against toxins and viruses such as diphtheria-tetanus-pertussis, ...

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Номер записи: 29
21-01-2016 дата публикации

SHORT-CHAIN FATTY ACID HEXOSAMINE ANALOGS AND THEIR USE IN TISSUE ENGINEERING APPLICATIONS

Номер: US20160016985A1
Автор: Aich Udayanath, Coburn Jeannine, Elisseeff Jennifer H., Yarema Kevin
Принадлежит:

A new class of molecules, C—OH tributanoylated hexosamines, including, for example, GalNAc, GlcNAc and ManNAc, are demonstrated to increase cartilage-like tissue accumulation by IL-1β-stimulated chondrocytes. Furthermore, all three molecules reduced NFKB1 and IκBα driven gene expression, consistent with NFκB inhibitory properties of these analogs. GalNAc-a exposure produced the greatest ECM accumulation by IL-Iβ-stimulated chondrocytes. However, GalNAc-a exposure produced an opposite effect on MSC exposure, where a decrease in ECM accumulation was observed. These findings are in support of the function of NFκB signaling during limb development and growth plate chondrogenesis. The present invention shows the capability of this new class of hexosamine analogs as disease-modifying agents for treating cartilage damage.

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Номер записи: 30
15-01-2015 дата публикации

STABILISATION OF RADIOPHARMACEUTICAL PRECURSORS

Номер: US20150018541A1
Автор: "INT VELD DIRK-JAN", Grigg Julian, Osborn Nigel John, Wickstrom Torild, Wilson Anthony
Принадлежит:

The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed. 1. A method for improving stability of a non fluoridated sugar derivative which comprises storage of said non fluoridated sugar derivative in a solvent in a sealed container.2. A method according to wherein the non fluoridated sugar derivative is a monosaccharide sugar in which one of the OH groups is replaced by a leaving group and the other OH groups of the sugar are each optionally protected with a suitable protecting group.4. A method according to wherein the non fluoridated sugar derivative is 1 claim 1 ,3 claim 1 ,4 claim 1 ,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose.5. A method according to wherein the solvent is an aprotic solvent.6. A method according to wherein the aprotic solvent is acetonitrile.7. A method according to wherein the solvent has a water content of 1000 ppm or less.8. A method according to wherein the solvent has a water content of between 1000 ppm and 50000 ppm.9. A method according to wherein the sealed container is a septum-sealed vial.10. A formulation of a non fluoridated sugar derivative as defined in comprising said non fluoridated sugar derivative claim 1 , and a solvent in a sealed container.11. A formulation according to wherein the solvent is an aprotic solvent claim 10 , suitably acetonitrile.12. A formulation according to wherein the solvent has a water content of 1000 ppm or less.13. A ...

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Номер записи: 31
21-01-2021 дата публикации

DETECTION OF OLIGOSACCHARIDES

Номер: US20210017570A1
Автор: Brown Jillian R., Crawford Brett E., Glass Charles A.
Принадлежит: Biomarin Pharmaceutical Inc.

Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation. 130-. (canceled)31. A method of determining in an individual the presence , identity , and/or severity of an MPS IIIA or MPS IIIB disorder , the method comprising:(a) generating a biomarker comprising one or more saturated non-reducing end oligosaccharides, wherein the biomarker is generated by treating a population of heparan sulfate oligosaccharides, in or isolated from a biological sample from the individual, with at least one digesting glycosaminoglycan lyase, wherein prior to lyase treatment, the biomarker is not present in abundance in samples from individuals with the MPS IIIA or MPS IIIB disorder relative to individuals without the MPS IIIA or MPS IIIB disorder; and(b) using an analytical instrument to detect the presence of and/or measure the amount of the biomarker produced and displaying or recording the presence of or the measure of the biomarker produced;wherein the presence of and/or measure of the amounts of the biomarker are utilized to determine the presence, identity, and/or severity of the MPS III disorder; andwherein the biomarker is selected from a group consisting of{'sub': '3', 'Formula III: [GlcNS-IdoA-GlcN(Ac)0-1](SOR)0-3;'}{'sub': '3', 'Formula IV: [GlcNS-GlcA-GlcN(Ac)0-1](SOR)0-2;'}{'sub': '3', 'Formula V: [GlcNAc-IdoA-GlcN(Ac)0-1](SOR)0-3;'}{'sub': '3', 'Formula VI: [GlcNAc-GlcA-GlcN(Ac)0-1](SOR)0-2;'}{'sub': '3', 'Formula VIII: [GlcN-GlcA-GlcN(Ac)0-1](SOR)0-4;'}{'sub': '3', 'Formula IX: [GlcNAc6S-IdoA-GlcN(Ac)0-1](SOR)0-3;'}{'sub': '3', 'Formula X: [GlcNAc6S-GlcA-GlcN(Ac)0-1](SOR)0-2;'}GlcN-IdoA-GlcNAc;GlcN-IdoA2S-GlcNAc;GlcN-IdoA-GlcNS;GlcN-IdoA-GlcNAc6S;GlcN-IdoA2-GlcNAc6S; andGlcN-IdoA-GlcNS6S.32. The method of claim 31 , wherein the biomarker is of Formula V: [GlcNAc-IdoA-GlcN(Ac)-1](SOR); or ...

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Номер записи: 32
17-04-2014 дата публикации

PHARAMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING HUMAN IMMUNODEFICIENCY VIRUS

Номер: US20140107015A1
Автор: KARADENIZ Fatih, Kim Se-Kwon
Принадлежит: PUKYONG NATIONAL UNIVERSITY INDUSTRY-UNIVERSITY COOPERATION FOUNDATION

There is provided a pharmaceutical composition for preventing or treating human immunodeficiency virus, and more particularly, to a pharmaceutical composition and health functional food for preventing or treating/improving human immunodeficiency virus, the pharmaceutical composition and health functional food including a new compound with chitooligosaccharides conjugated amino acids or dipeptides as an effective component. The new compound has an excellent anti-HIV effect through an activity of inhibiting a HIV initial infection by interrupting an interaction between host-virus membranes, and also activities of inhibiting reverse transcriptase and protease of HIV. The compound according to the present invention is a conjugate synthesized through conjugating chitooligosaccharides derived from a natural material with amino acids or dipeptides. The compound is stable without cytotoxicity. 2. The method of claim 1 , wherein the composition including the compound represented by Chemical Formula 1 (here claim 1 , x is Chemical Structure 1 or 5) as an effective component has an anti-HIV effect through an activity of inhibiting reverse transcriptase of HIV.3. The method of claim 1 , wherein the composition including the compound represented by Chemical Formula 1 (here claim 1 , x is Chemical Structure 3 or 4) as an effective component has an anti-HIV effect through an activity of inhibiting a HIV infection by interrupting an interaction between host-virus membranes.4. The method of claim 1 , wherein the composition including the compound represented by Chemical Formula 1 (here claim 1 , x is Chemical Structure 2) as an effective component has an anti-HIV effect through an activity of inhibiting protease of HIV.5. The method of claim 1 , wherein the composition including the compound represented by Chemical Formula 1 (here claim 1 , x is one selected from Chemical Structures 6 to 8) as an effective component has an anti-HIV effect through activities of inhibiting reverse ...

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Номер записи: 33
28-01-2021 дата публикации

MOFEZOLAC DERIVATIVES AS MULTI-FUNCTIONS SELECTIVE COX-1 INHIBITORS

Номер: US20210023055A1
Автор: PERRONE Maria Grazia, SCILIMATI Antonio, VITALE Paola
Принадлежит:

The invention relates to a new class of compounds targeting COX-1. The invention also relates to the use of some of such compounds as a tool to investigate the structure and function of the enzyme, in the treatment targeting COX-1 or detection of COX-1 in relating disorders or diseases such as cancer and neuroinflammation, in particular in neurological (e.g. autism spectrum disorders) and neurodegenerative diseases (e.g. Alzheimer's diseases, Parkinson's diseases, amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), traumatic brain injury (TBI), HIV dementia and prion diseases), and in gynecological tumor (e.g. ovarian cancer), neck and head tumor, and haematological tumors (e.g. multiple myeloma) and in the detection of COX-1 in “in vitro” (cells and tissues) and in “in vivo”. 2. The compound according to wherein R-G is OH or OCHfor use in the treatment of neuroinflammation.3. The compound according to wherein R-G is OH or OCHfor use in the treatment of a neurological or neurodegenerative disease.4. The compound according to wherein R-G is OH or OCHfor use in the treatment of autism.5. The compound according to wherein R-G is OH or OCHfor use in the treatment of a neurodegenerative disease selected in the group of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , amyotrophic lateral sclerosis (ALS) claim 1 , multiple sclerosis (MS) claim 1 , traumatic brain injury (TBI) claim 1 , HIV dementia and prion diseases.6. The compound according to having the following formula I wherein G is selected from: Galactose claim 1 , Glucose claim 1 , Fructose claim 1 , Glycine claim 1 , Valine claim 1 , Isoleucine claim 1 , Arginine claim 1 , Glutamic acid claim 1 , Glutamine claim 1 , Aspartic acid claim 1 , Asparagine claim 1 , Histidine claim 1 , Alanine claim 1 , Leucine claim 1 , Lysine claim 1 , Methionine claim 1 , Cysteine claim 1 , Phenylalanine claim 1 , Threonine claim 1 , Tryptophan claim 1 , Proline claim 1 , Selenocysteine claim 1 , Serine claim 1 ...

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Номер записи: 34
17-02-2022 дата публикации

Processes and Materials for the Synthesis of Sugar Esters Found in Natural Tobacco

Номер: US20220048938A1
Автор: Chenyue XING
Принадлежит: Myst Labs Inc

A process and materials method for making a glucose tetraester may include reacting glucose with a carboxylic acid to create a glucose pentaester. The glucose pentaester was reacted with a basic reagent to create a glucose tetraester. Glucose was reacted with a carboxylic acid anhydride in the presence of 4-dimethylaminopyridine to create a glucose pentaester product. The glucose pentaester reaction product was separated. The glucose pentaester reaction product was reacted with a basic reagent, wherein the reaction steps may take place at a temperature of about 0° C. to about 60° C. and about ambient pressure, wherein the ratio of the carboxylic acid to the glucose was from about 5:1 to about 50:1, and wherein the ratio of the glucose pentaester to the basic reagent was from about 1:50 to about 1:150.

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Номер записи: 35
30-01-2020 дата публикации

Mobile Rhamnolipid Contamination Response

Номер: US20200031690A1
Автор: DeSanto Keith
Принадлежит:

Our mobile rhamnolipid production vehicles can convert pollutants obtained from contaminated sites into rhamnolipid. Then, our mobile rhamnolipid application units can alter, treat and remove pollutants from soil and water. Our new rhamnolipid application can use various sources for power. All these new components combined are cost efficient. Moreover, the mobile rhamnolipid contamination response vehicles are easy to mobilize and can be deployed and up and running with a short amount of time and effort. 1. An application where , rhamnolipid production tanks for producing rhamnolipid are fixed on a vehicle that is mobile.2. An application as in where the mobile vehicle can be a boat claim 1 , ship claim 1 , train claim 1 , jet claim 1 , airplane or land roaming vehicle.3. An application as in and where each rhamnolipid production tank is short and stacked on top of one another.4. An application as in claim 1 , and where the rhamnolipid production tanks are stacked on top of one another and placed side by side and be made of plastic claim 1 , metal or a combination of both.5. An application in where the rhamnolipid production tanks are connected to other similar mobile vehicle units.6. An application as in through where the rhamnolipid production tanks are connected to each other by metal pipe and or plastic pipe and or electrical power sources.7. An application as in through where the rhamnolipid production tanks are powered by solar power claim 1 , natural gas claim 1 , power from running water claim 1 , wind turbines or electricity.8. An application as in through where the rhamnolipid production tanks are connected and operated wirelessly.9. An application as in through where the rhamnolipid production tanks are monitored and or managed by drones from land claim 1 , from water or from the air.10. An application as in through where the rhamnolipid production tanks are connected wirelessly by drones for communication purposes.11. An application using through to ...

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Номер записи: 36
24-02-2022 дата публикации

ALPHA (1,2) FUCOSYLTRANSFERASE SYNGENES FOR USE IN THE PRODUCTION OF FUCOSYLATED OLIGOSACCHARIDES

Номер: US20220056497A1
Автор: Heidtman Matthew Ian, McCoy John M., Merighi Massimo
Принадлежит:

The invention provides compositions and methods for engineering or other host production bacterial strains to produce fucosylated oligosaccharides, and the use thereof in the prevention or treatment of infection. 1. A method for producing a fucosylated oligosaccharide in a bacterium comprisingproviding bacterium comprising an exogenous lactose-utilizing α(1,2) fucosyltransferase enzyme, wherein said α(1,2) fucosyltransferase enzyme has at least 90% sequence identity to amino acid sequence SEQ ID NO: 17; andculturing said bacterium in the presence of lactose.2. (canceled)3Prevotellaa. The method of claim 1 , wherein said α(1 claim 1 ,2) fucosyltransferase enzyme comprises sp. FutW claim 1 , or a functional variant or fragment thereof.4. (canceled)5. The method of claim 1 , further comprising retrieving the fucosylated oligosaccharide from said bacterium or from a culture supernatant of said bacterium.6. The method of claim 1 , wherein said fucosylated oligosaccharide comprises 2′-fucosyllactose (2′-FL) claim 1 , lactodifucotetraose (LDFT) claim 1 , or lacto-N-difucohexaose I (LDFH I).7. The method of claim 1 , wherein the bacterium further comprises an exogenous lactose-utilizing α(1 claim 1 ,3) fucosyltransferase enzyme and/or an exogenous lactose-utilizing α(1 claim 1 ,4) fucosyltransferase enzyme claim 1 , or wherein said bacterium further comprises a reduced level of β-galactosidase activity claim 1 , a defective colanic acid synthesis pathway claim 1 , an inactivated adenosine-5′-triphosphate (ATP)-dependent intracellular protease claim 1 , or an inactivated endogenous lacA gene claim 1 , or any combination thereof.8Helicobacter pylori. The method of claim 7 , wherein the exogenous lactose-utilizing α(1 claim 7 ,3) fucosyltransferase enzyme comprises a 26695 futA gene.9Helicobacter pyloriHelicobacter pylori. The method of claim 7 , wherein the exogenous lactose-utilizing α(1 claim 7 ,4) fucosyltransferase enzyme comprises a UA948 FucTa gene or a strain DMS6709 ...

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Номер записи: 37
01-05-2014 дата публикации

ANTITUMOR AGENT

Номер: US20140121175A1
Автор: Kita Ayako, Kunoh Tatsuki, Muraoka Osamu, Sugiura Reiko, Tsutsui Nozomi
Принадлежит: KINKI UNIVERSITY

The invention is intended to provide an excellent antitumor agent. An antitumor agent contains a glycolipid glycoside compound represented by Formula (1) or a pharmacologically acceptable salt thereof as an active ingredient: 2. The antitumor agent according to claim 1 ,{'sup': 1', '4, 'wherein in Formula (1), Rto Rare the same as or different from each other and are a lower to higher alkanoyl group or a hydrogen atom, and A is a sugar alcohol residue or a polyol residue.'}3. The antitumor agent according to claim 1 ,{'sup': 1', '4, 'wherein in Formula (1), Rto R, are the same as or different from each other and are an alkanoyl group having 3 to 16 carbon atoms or a hydrogen atom, and A is a sugar alcohol residue having 3 to 7 carbon atoms or a polyol residue having 2 to 3 carbon atoms.'}5. The antitumor agent according to claim 4 ,{'sub': 2', 'k', '2, 'wherein in Formula (1a), f, h, m and n represent an integer of 2 to 8, and —CH(CHOH)CHOH is a sugar alcohol residue having 4 to 7 carbon atoms or a glycerin residue.'} This application is a national stage application under 35 U.S.C. §371 of PCT International Application No. PCT/JP2012/063686 which has an International filing date of May 2012. PCT/JP2012/063868 claims priority under 35 U.S.C. §119 to Japanese Application No. 2011-119797 filed on 27 May 2011 and to Japanese Application No. 2012-097198 filed on 20 Apr. 2012. The contents of each application recited above are incorporated herein by reference in their entirety.The present invention relates to an antitumor agent containing a novel glycolipid glycoside compound or a pharmacologically acceptable salt thereof as an active ingredient.The invention relates to an antitumor agent containing a novel compound discovered by a new screening method that the inventors of the invention have developed, as an active ingredient. The compound, which has a pentitol and a hexitol chain as an aglycone, and in which all hydroxyl groups of a mannose ring which is a mother ...

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Номер записи: 38
14-02-2019 дата публикации

METHOD FOR PRODUCING ALPHA-HALO-TETRAACYL-GLUCOSE

Номер: US20190048034A1
Автор: HATSUDA Masanori, HYODO Isao, TANIMOTO Kouichi, UEDA Keita
Принадлежит: MITSUBISHI TANABE PHARMA CORPORATION

There is provided an efficient and excellent preparation method of an α-halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the α-halo-tetraacyl-glucose represented by the formula (III): 2. The method according to claim 1 , wherein the method comprises using 0.1 to 1 mol of the Lewis acidic metal bromide selected from the group consisting of zinc bromide claim 1 , cobalt bromide claim 1 , and bismuth bromide against 1 mol of unprotected lower alkyl D-glucoside.3. The method according to claim 1 , wherein the method comprises using 0.1 to 0.2 mol of the Lewis acidic metal bromide selected from the group consisting of zinc bromide claim 1 , cobalt bromide claim 1 , and bismuth bromide against 1 mol of unprotected lower alkyl D-glucoside.7. The method according to claim 1 , wherein R is an optionally substituted methyl claim 1 , t-butyl or an optionally substituted phenyl.8. The method according to claim 7 , wherein R is t-butyl.9. The method according to claim 1 , wherein X is a chlorine atom or a bromine atom.10. The method according to claim 1 , wherein the Lewis acidic metal bromide is zinc bromide.11. The method according to claim 1 , wherein the acid halide (V) is pivaloyl bromide.12. The method according to claim 1 , wherein the method comprises using 0.1 to 1 mol of zinc bromide as the Lewis acidic metal bromide against 1 mol of unprotected lower alkyl D-glucoside. This application is a Continuation of copending application Ser. No. 14/770,415, filed on Aug. 25, 2015, which is a national phase of PCT International Application No. PCT/JP2014/054416 on Feb. 25, 2014, which claims the benefit under 35 U.S.C. § 119 (a) to Patent Application No. 2013-036333, filed in Japan on Feb. 26, 2013 and Patent Application No. 2013-268649, filed in Japan on Dec. 26, 2013, all of which are hereby expressly incorporated by ...

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Номер записи: 39
08-05-2014 дата публикации

METHOD FOR DETERMINING THE PRESENCE OR ABSENCE OF A BIOMARKER

Номер: US20140127709A1
Автор: Baird Mark Stephen, Gwenin Christopher David, Gwenin Vanessa Valerie, Pitts Mark
Принадлежит: Bangor University

A method of determining the presence or absence in a sample of a biomarker, the method comprising: (a) linking an antigen to colloidal gold to provide a gold-antigen species; (b) contacting the gold-antigen species with the sample; (c) adding a diagnosis agent to the sample; and (d) observing the colour of the sample. 1. A method of determining the presence or absence in a sample of a biomarker , the method comprising:(a) linking an antigen to colloidal gold to provide a gold-antigen species;(b) contacting the gold-antigen species with the sample;(c) adding a diagnosis agent to the sample; and(d) observing the colour of the sample.2. A method according to wherein the biomarker is a disease antibody indicative of infection with a mycobaterial disease.3. A method according to wherein the biomarker is a disease antibody indicative of the presence of tuberculosis.4. A method according to claim 1 , wherein the antigen is a mycolic acid derived antigen selected from one or more of the following classes of compounds:(i) mycolic acids obtained from natural sources;(ii) synthetically prepared mycolic acids;(iii) salts of mycolic acids;(iv) esters of mycolic acids (i) and/or (ii);(v) sulfur-containing mycolic acids and/or salts or esters thereof;(vi) simple structural analogues of mycotic acids and/or salts or esters thereof.5. A method according to claim 1 , wherein the antigen is linked to the gold by a gold-sulfur bond.6. A method according to wherein the antigen is directly bonded to the colloidal gold by a sulfur atom contained within the antigen molecule.7. A method according to wherein the antigen is linked to the colloidal gold via a sulfur-containing linker compound.8. A method according to claim 1 , wherein the diagnosis agent is an aqueous composition having one or more salts dissolved therein.9. A method according to claim 1 , in which step (d) involves visually observing the presence or absence of a colour change to provide a qualitative assessment.10. A method ...

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Номер записи: 40
13-02-2020 дата публикации

PATTERN FORMING METHOD, UNDER COATING AGENT, AND LAMINATE

Номер: US20200048491A1
Автор: HATTORI Kimiko, MORITA Kazuyo
Принадлежит:

It is an object of the present invention to provide a pattern forming method capable of easily forming a phase-separated structure with high accuracy, even in the case of widening the applicable range of a pattern size. The present invention relates to a pattern forming method comprising: applying an under coating agent onto a substrate, and applying a self-assembly composition for pattern formation to the surface of the substrate, onto which the under coating agent has been applied, and then forming a self-assembly film according to self-assembly phase separation, wherein the self-assembly composition for pattern formation comprises a block copolymer comprising a polymerization unit (a) having at least one selected from a structure represented by a formula () and a structure represented by a formula (), and a polymerization unit (b) having a structure represented by a formula (). 2. The pattern forming method according to claim 1 , wherein the under coating agent comprises a polymer containing at least one selected from a (meth)acrylate-derived unit optionally having a substituent and a styrene-derived unit optionally having a substituent.4. The pattern forming method according to any claim 1 , which further comprises an etching step claim 1 , after completion of the forming the self-assembly film.5. The pattern forming method according to claim 4 , wherein the etching step is a dry etching step.6. The pattern forming method according to claim 4 , wherein the etching step is a wet etching step. The present invention relates to a pattern forming method, an under coating agent, and a laminate.Electronic devices such as semiconductors have been required to be highly integrated as a result of miniaturization thereof. With regard to the patterns of semiconductors, miniaturization and the diversification of the shapes have been studied. As such pattern forming methods, a double patterning method, a lithography method using electron beam, and a pattern forming method ...

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Номер записи: 41
04-03-2021 дата публикации

GLYCOSIDE COMPOUND OF FATTY ACIDS, COMPOSITION COMPRISING IT, PROCESS FOR ITS OBTENTION AND METHODS TO APPLY IT ON PLANTS OR FRUITS OR BOTH AT THE SAME TIME

Номер: US20210059250A1
Автор: Castagnaro Atilio Pedro, Di Peto Pía de los Angeles, Filippone Maria Paula, Grellet Bournonville Carlos Froilan, Mamaní Alicia Ines de Fatima, Viking Welin Bjorn Gunnar
Принадлежит:

A glycoside compound of fatty acids that includes the general formula: GalNAc-GalNAc-Glc-O—R, where GalNAc is α- or β-D-N-acetylgalactosamine, Glc-O—R is a molecule of α- or β-D-glucose esterified to a monounsaturated fatty acid (R), where R is selected from 12:1(n) and where n is an integer between 2 and 11; 11:1(n) and where n is an integer between 2 and 10; 10:1(n), and where n is an integer between 2 and 9; 9:1(n), and where n is an integer between 2 and 8; 8:1(n), and where n is an integer between 2 and 8; 7:1(n) and where n is an integer between 2 and 7; and 6:1(n), and where n is an integer between 2 and 6. The compound has activity against plant pathogens, and induces the defense, and promotes the growth, of plants. 1. A glycoside compound of fatty acids , comprising a general formula:{'br': None, 'GalNAc-GalNAc-Glc-O—R,'}where GalNAc is α- or β-D-N-acetylgalactosamine, Glc-O—R is a molecule of α- or β-D-glucose esterified to a monounsaturated fatty acid (R), where R is selected from 12:1(n) and where n is an integer between 2 and 11; 11:1(n) and where n is an integer between 2 and 10;10:1(n), and where n is an integer between 2 and 9; 9:1(n), and where n is an integer between 2 and 8; 8:1(n), and where n is an integer between 2 and 8; 7:1(n) and where n is an integer between 2 and 7; and 6:1(n), and where n is an integer between 2 and 6.2. A composition for the promotion of plant growth , comprising a fatty acid glycoside having the general formula:{'br': None, 'GalNAc-GalNAc-Glc-O—R,'}where GalNAc is α- or β-D-N-acetylgalactosamine, Glc-O—R is a molecule of α- or β-D-glucose esterified to a monounsaturated fatty acid (R), where R is selected from 12:1(n) and where n is an integer between 2 and 11; 11:1(n) and where n is an integer between 2 and 10; 10:1(n), and where n is an integer between 2 and 9; 9:1(n), and where n is an integer between 2 and 8; 8:1(n), and where n is an integer between 2 and 8; 7:1(n) and where n is an integer between 2 and 7; and 6:1 ...

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Номер записи: 42
01-03-2018 дата публикации

2,3-Fluorinated Glycosides as Neuraminidase Inhibitors and Their Use as Anti-Virals

Номер: US20180057474A1
Автор: Kim Jin Hyo, Watts Andrew Graham, Wennekes Tom, Withers Stephen
Принадлежит:

Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza. 3. The compound of claim 1 , wherein T is COOH or COOR claim 1 ,{'sup': '1', 'sub': '1-10', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO, and'}wherein zero to five backbone carbons of the optionally substituted alkyl group are optionally and independently substituted with O, N or S.4. The compound of claim 1 , wherein T is C(O)OCH claim 1 , C(O)OCHCH claim 1 , C(O)OCHCHCH claim 1 , C(O)OCHCHCHCH claim 1 , C(O)OCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCH claim 1 , C(O)OCHCHCHCHCHCHCHCH claim 1 , or COOH.5. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO.6. The compound of claim 1 , wherein A is selected from the group consisting of: F claim 1 , Cl claim 1 , and OR claim 1 ,{'sup': '3', 'sub': '1-10', 'wherein Ris a Clinear, branched or cyclic, saturated or unsaturated, optionally substituted alkyl group,'}{'sub': 2', '3', '2, 'wherein the optional substituent is selected from one or more of the group consisting of: oxo, OH, F, Cl, Br, I, NH, CN, SH, SOH and NO.'}7. The compound of claim 1 , wherein A is F or Cl.8. The compound of claim 1 , wherein A is F.9. The compound of claim 1 , wherein D is selected from the group consisting of: H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , OH claim 1 , CN claim 1 , and NO claim 1 , provided A and D are not both H.10. The compound of claim 1 , wherein D is selected from the group ...

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Номер записи: 43
20-02-2020 дата публикации

DUALLY DERIVATIZED CHITOSAN NANOPARTICLES AND METHODS OF MAKING AND USING THE SAME FOR GENE TRANSFER IN VIVO

Номер: US20200054759A1
Автор: CHEUNG Anthony, Gao Jun, Hsu Eric
Принадлежит:

Provided herein is chitosan dually derivatized with arginine and gluconic acid; and methods of making and using the same, e.g., for gene delivery in vivo. 114.-. (canceled)15. A method of delivering a nucleic acid to a subject in need thereof comprising administering to the subject a dually derivatized (DD) chitosan nucleic acid polyplex , wherein said DD chitosan nucleic acid polyplex comprises a nucleic acid complexed with a chitosan-derivative nanoparticle comprising chitosan coupled with gluconic acid and arginine.16. The method of claim 15 , wherein said nanoparticle comprises arginine at a concentration of about 10% to about 55%.17. The method of claim 15 , wherein said nanoparticle comprises gluconic acid at an initial concentration of about 8% to about 30%.18. The method of claim 15 , wherein said nanoparticle comprises gluconic acid at a final functionalization of about 3% to about 10%.19. The method of claim 15 , wherein said DD chitosan nucleic acid polyplex has a combined degree of functionalization with said arginine and said gluconic acid of 1-60%.20. The method of claim 19 , wherein said DD chitosan nucleic acid polyplex has a combined degree of functionalization with said arginine and said gluconic acid of 1-30%.21. The method according to claim 15 , wherein the amine to phosphate ratio of said DD-chitosan nucleic acid polyplex is between 2 to 100.22. The method according to claim 21 , wherein the amine to phosphate ratio of said DD-chitosan nucleic acid polyplex is between 2 to 50.23. The method according to claim 22 , wherein the amine to phosphate ratio of said DD-chitosan nucleic acid polyplex is between 2 to 30.24. The method according to claim 23 , wherein the amine to phosphate ratio of said DD-chitosan nucleic acid polyplex is between 2 to 15.25. The method according to claim 15 , wherein said DD-chitosan nucleic acid polyplex has a molar ratio of said arginine to said gluconic acid of between 100:1 and 1:100.26. The method according to claim ...

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Номер записи: 44
01-03-2018 дата публикации

Microorganisms and Methods for Producing Sialylated and N-Acetylglucosamine-Containing Oligosaccharides

Номер: US20180057849A1
Автор: Heidtman Matthew Ian, McCoy John M., Merighi Massimo
Принадлежит:

The invention provides compositions and methods for engineering bacteria to produce sialylated and N-acetylglucosamine-containing oligosaccharides, and the use thereof in the prevention or treatment of infection. 121.-. (canceled)22. A method for producing an N-acetylglucosamine-containing oligosaccharide in a bacterium comprising: 'culturing said bacterium in the presence of lactose.', 'providing a bacterium, said bacterium comprising an exogenous UDP-GlcNAc:Galα/β-R 3-N-acetylglucosaminyltransferase gene and a functional lactose permease gene; and'}23. The method of claim 22 , wherein said bacterium comprises an increased UDP-GlcNAc production capability.24. The method of claim 22 , wherein said increased UDP-GlcNAc production capability comprises overexpression of a nagC gene claim 22 , a glmS gene claim 22 , a glmY gene claim 22 , a glmZ gene or any combination thereof.25E. coli. The method of claim 22 , wherein said increased UDP-GlcNAc production capability comprises overexpression of nagC gene.26. The method of claim 22 , wherein said increased UDP-GlcNAc production capability comprises overexpression of nagC and glmS.27. The method of claim 22 , wherein said increased UDP-GlcNAc production capability comprises overexpression of nagC and glmY.28. The method of claim 22 , wherein said increased UDP-GlcNAc production capability comprises overexpression of nagC and glmZ.29. The method of claim 22 , wherein said N-acetylglucosamine-containing oligosaccharide comprises any one selected from Lacto-N-triose 2 (LNT2) claim 22 , Lacto-N-tetraose (LNT) claim 22 , Lacto-N-neotetraose (LNnT) claim 22 , Lacto-N-fucopentaose I (LNF I) claim 22 , Lacto-N-fucopentaose II (LNF II) claim 22 , Lacto-N-fucopentaose III (LNF III) claim 22 , Lacto-N-fucopentaose V (LNF V) claim 22 , Lacto-N-difucohexaose I (LDFH I) claim 22 , Lacto-N-difucohexaose II (LDFH II) claim 22 , and Lacto-N-neodifucohexaose II (LFNnDFH II).30E. coli.. The method of claim 22 , wherein said bacterium is31. ...

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Номер записи: 45
02-03-2017 дата публикации

Trisaccharide Derivates, and Their Use as Adjuvants

Номер: US20170057987A1
Автор: Hof Robert Patrick, Kriek Maria Aldegonda Jacoba, Schaaper Wilhelmus Martinus Maria, Schenkelaars Everardus Joannes Peter Maria, Turkstra Jouwert Anne, Van Bree Johannes Gernardus Mathias Marie
Принадлежит:

The present invention relates to the use of trisaccharide derivates comprising a substituted trisaccharide core, which trisaccharide core is fully substituted with fatty acid ester groups, and optionally one or more anionic groups as adjuvants, to the trisaccharide derivates as such, to a method for preparing such trisaccharides, to trisaccharides obtained with such method, to adjuvant compositions comprising such trisaccharide derivates and to a vaccine or kit comprising such adjuvant compositions. 110-. (canceled)11. A trisaccharide derivate comprising a substituted trisaccharide core , which trisaccharide core is fully substituted with fatty acid ester groups , and optionally one or more anionic groups as an adjuvant.12. The trisaccharide derivate according to claim 11 , wherein the substituted trisaccharide core is derived from raffinose claim 11 , melezitose claim 11 , maltotriose claim 11 , nigerotriose claim 11 , maltotriulose or kestose.13. The trisaccharide derivate according to claim 11 , wherein the substituted trisaccharide core comprises one or two sulphate ester or phosphate ester groups as anionic groups.14. The trisaccharide derivate according to claim 11 , wherein the anionic group is a sulphate ester.15. The trisaccharide derivate according to claim 11 , wherein the fatty acid ester group is an ester of a straight claim 11 , branched claim 11 , saturated or unsaturated fatty acid with a chain length of 4 to 20 carbon atoms.16. The trisaccharide derivate according to claim 11 , wherein the fatty acid ester is the ester of lauric acid claim 11 , myristic acid claim 11 , palmitic acid claim 11 , stearic acid or arachidic acid.17. The trisaccharide derivate according to claim 11 , wherein the fatty acid ester groups of the substituted trisaccharide core are all identical.18. The trisaccharide derivate according to claim 11 , wherein the substituted trisaccharide core is derived from raffinose claim 11 , melezitose or maltotriose and wherein the ...

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Номер записи: 46
20-02-2020 дата публикации

COMPOUND, RESIST COMPOSITION CONTAINING COMPOUND AND PATTERN FORMATION METHOD USING SAME

Номер: US20200057370A1
Автор: ECHIGO Masatoshi, KUDO Hiroto, Sato Takashi
Принадлежит:

A resist composition comprising one or more tannin compounds selected from the group consisting of a tannin comprising at least one crosslinking reactive group in the structure and a derivative thereof, and a resin obtained using the tannin or the derivative as a monomer. 1. A resist composition comprising one or more tannin compounds selected from the group consisting of a tannin comprising at least one crosslinking reactive group in a structure and a derivative thereof , and a resin obtained using the tannin or the derivative as a monomer.5. The resist composition according to claim 1 , further comprising a solvent.6. The resist composition according to claim 1 , further comprising an acid generating agent.7. The resist composition according to claim 1 , further comprising an acid diffusion controlling agent.8. A method for forming a pattern claim 1 , comprising the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'forming a resist film on a substrate using the resist composition according to ;'}exposing the resist film; anddeveloping the resist film, thereby forming a pattern.10. A resin obtained using the compound according to as a monomer.12. A resin obtained using the compound according to as a monomer.14. A resin obtained using the compound according to as a monomer. The present invention relates to a compound for use mainly as a lithography material, a resist composition comprising the compound, and a pattern formation method using the resist composition.Conventional typical resist materials are polymer based resist materials capable of forming amorphous thin films. Examples include polymer based resist materials such as polymethyl methacrylate, polyhydroxy styrene with an acid dissociation reactive group, and polyalkyl methacrylate. A line pattern of about 45 to 100 nm is formed by irradiating a resist thin film made by coating a substrate with a solution of such a polymer based resist material with ultraviolet, far ultraviolet, electron beam, ...

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Номер записи: 47
28-02-2019 дата публикации

REGIOSELECTIVE SILYL EXCHANGE OF PER-SILYLATED OLIGOSACCHARIDES

Номер: US20190062361A1
Автор: GERVAY-HAGUE Jacquelyn, SCHOMBS Matthew
Принадлежит:

The present invention provides novel, regioselectively-acylated oligosaccharide compounds and methods for preparing them. In another aspect, the. invention provides a method for preparing a selectively-acylated oligosaccharide. The method includes forming a reaction mixture containing a protected oligosaccharide and an acylating agent. The protected oligosaccharide includes at least three hydroxyl moieties and each hydroxyl moiety is protected with a silyl protecting group. The reaction mixture is formed under conditions sufficient to selectively replace at least one silyl protecting group with a —C(0)-C1_6 alkyl group, and the selectively-acylated oligosaccharide comprises at least one —C(0)-C1_6 alkyl group and at least one silyl protecting group. 2. The compound according to claim 1 , wherein{'sup': 1', '2', '3', '4', '6', '7, 'R, R, R, R, and Rare each independently selected from the group consisting of —OR, the α-linked monosaccharide, and the β-linked monosaccharide;'}{'sup': 1a', '2a', '3a', '4a', '6a', '7, 'R, R, R, R, and Rare each independently selected from the group consisting of —ORand the linking moiety —O—;'}{'sup': 7', '8, 'sub': 1-6', '3, 'each Ris independently selected from the group consisting of —C(O)—Calkyl and —Si(R); and'}{'sup': 1', '2', '3', '4', '6', '1a', '2a', '3a', '4a', '6a', '7', '7', '8, 'sub': '3', 'at least one of R, R, R, R, R, R, R, R, R, and Ris —OR, wherein Ris —Si(R).'}3. The compound according to claim 2 , wherein Ris selected from the group consisting of the α-linked monosaccharide and the β-linked monosaccharide.4. The compound according to claim 3 , wherein one of R claim 3 , Rand Ris the linking moiety —O—.5. The compound according to claim 4 , wherein Ris —OR claim 4 , wherein Ris —C(O)—Calkyl.6. The compound according to claim 5 , wherein at least one of R claim 5 , R claim 5 , R claim 5 , R claim 5 , and Ris —OR claim 5 , wherein Ris —C(O)—Calkyl.7. (canceled)10. The compound according to claim 9 , wherein Ris —C(O)— ...

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Номер записи: 48
18-03-2021 дата публикации

CARBOHYDRATE ESTERS AS INDUCERS FOR GENE EXPRESSION

Номер: US20210079438A1
Автор: Huang Tom Tao
Принадлежит:

The invention provides novel carbohydrate esters, in particular disaccharide esters, and the methods of their preparation. These compounds find use as microbial media components for the induction of gene expression in microbial fermentation processes. 2. The method according to claim 1 , wherein an optional conventional inducer is added to the culture.3. The method according to claim 2 , wherein the optional conventional inducer comprises lactose claim 2 , cellobiose claim 2 , sophorose claim 2 , cellulose claim 2 , cellulose hydrolysate claim 2 , maltose claim 2 , isomaltose claim 2 , maltodextrins claim 2 , starch claim 2 , or starch hydrolysate.4. The method according to claim 1 , wherein the protein of interest is cellulase or amylase.5. The method according to claim 1 , wherein the protein of interest is a homologous or heterologous protein.6. The method according to claim 5 , wherein the homologous or heterologous protein is an enzyme claim 5 , a hormone claim 5 , a growth factor claim 5 , a cytokine or an antibody.7. The method according to claim 1 , wherein the fermentation host is capable of producing cellulase or amylase.8Trichoderma, Humicola, Pleurotus, Fusarium, Aspergillus, Streptomyces, Thermomonospora, Bacillus, Cellulomonas, Penicillium, Basidiomycete, Chrysoporium, Pestalotiopsis, Neurospora, Cephalosporium, Achlya, Podospora, Endothia, Mucor, Cochliobolus, Myceliopthora, TalaromycesPyricularia.. The method according to claim 1 , wherein the fermentation host is a filamentous fungus or bacteria or other hosts selected from the genus group consisting of claim 1 , and9Trichoderma reeseiAspergillus niger.. The method according to claim 1 , wherein the fermentation host is the filamentous fungus or10. The method according to claim 1 , wherein the fermentation host is grown in a liquid culture or on a solid substrate without free-flowing liquid.11. The method according to claim 1 , wherein the fermentation host has a promoter operably linked to a gene ...

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Номер записи: 49
22-03-2018 дата публикации

Biosynthesis Of Human Milk Oligosaccharides In Engineered Bacteria

Номер: US20180080034A1
Автор: Heidtman Matthew Ian, McCoy John M., Merighi Massimo
Принадлежит:

The invention provides compositions and methods for engineering bacteria to produce fucosylated oligosaccharides, and the use thereof in the prevention or treatment of infection. 1. A method for producing a fucosylated oligosaccharide in a bacterium , comprisingproviding a bacterium, said bacterium comprising a functional β-galactosidase gene, an exogenous fucosyltransferase gene, a GDP-fucose synthesis pathway, a functional lactose permease gene;culturing said bacterium in the presence of lactose; andretrieving a fucosylated oligosaccharide from said bacterium or from a culture supernatant of said bacterium.2E. coli. The method of claim 1 , wherein said β-galactosidase gene comprises an lacZ gene.3. The method of claim 1 , wherein said β-galactosidase gene is an endogenous β-galactosidase gene or an exogenous β-galactosidase gene.4. The method of claim 1 , wherein said bacterium accumulates an increased intracellular lactose pool claim 1 , and produces a low level of β-galactosidase.5. The method of claim 1 , wherein said exogenous fucosyltransferase gene encodes α(1 claim 1 ,2) fucosyltransferase or α(1 claim 1 ,3) fucosyltransferase.6Bacteroides fragilis. The method of claim 5 , wherein said α(1 claim 5 ,2) fucosyltransferase gene comprises a wcfW gene.7Helicobacter pylori. The method of claim 5 , wherein said α(1 claim 5 ,3) fucosyltransferase gene comprises a 26695 futA gene.8. The method of claim 5 , wherein said bacterium comprises both an exogenous fucosyltransferase gene encoding α(1 claim 5 ,2) fucosyltransferase and an exogenous fucosyltransferase gene encoding α(1 claim 5 ,3) fucosyltransferase.9. The method of claim 1 , wherein said GDP-fucose synthesis pathway comprises endogenous enzymes or exogenous enzymes.10. The method of claim 1 , wherein said lactose permease gene is an endogenous lactose permease gene or an exogenous lactose permease gene.11. A method for producing a fucosylated oligosaccharide in a bacterium claim 1 , comprisingproviding an ...

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Номер записи: 50
22-03-2018 дата публикации

DETECTION OF OLIGOSACCHARIDES

Номер: US20180080059A1
Автор: Brown Jillian R., Crawford Brett E., Glass Charles A.
Принадлежит:

Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation. 130.-. (canceled)31. A method for determining in an individual , the presence , identity , and/or severity of MPS I disorder , the method comprising:a) generating a biomarker comprising of one or more non-reducing end oligosaccharides, wherein the biomarker is generated by treating a population of glycosaminoglycans, in or isolated from a biological sample from the individual, with at least one digesting glycosaminoglycan lyase, wherein prior to lyase treatment, the biomarker is not present in abundance in samples from individuals with the MPS I disorder relative to individuals without the MPS I disorder; andb) using an analytical instrument to detect the presence of and/or measure the amount of the biomarker produced and displaying or recording the presence of or the measure of the biomarker produced;wherein the presence and/or the measure of the amount of the biomarker are utilized to determine the presence, identity, and/or severity of MPS I disorder; andwherein the biomarker is selected from a group consisting ofFormula I-A: IdoA-GlcNAc;Formula I-B: IdoA-GlcNS;Formula I-C: IdoA-GlcNS6S;{'sub': 3', 'n, 'Formula XII: [IdoA-GalNAc](SOR), wherein n is 0-2;'}{'sub': 3', 'n, 'Formula XXI: [IdoA-GlcN(Ac)m-IdoA](SOR), where m is 0-1 and n is 0-4;'}{'sub': 3', 'n, 'Formula XXII: [IdoA-GlcN(Ac)m-GlcA](SOR), where m is 0-1 and n is 0-3; and'}{'sub': 3', 'n, 'Formula XXIII: [GlcA-GlcN(Ac)m-GlcA](SOR), where m is 0-1 and n is 0-3.'}32. The method of claim 31 , wherein the biomarker is selected from the group consisting of: Formula I-A: IdoA-GlcNAc; Formula I-B: IdoA-GlcNS; Formula I-C: IdoA-GlcNS6S; and Formula XII: [IdoA-GalNAc](SO3R)n claim 31 , wherein n is 0-2.33. The method of claim 31 , wherein the biomarker is selected from the ...

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Номер записи: 51
23-03-2017 дата публикации

Alpha (1,2) Fucosyltransferase Syngenes For Use in the Production of Fucosylated Oligosaccharides

Номер: US20170081353A1
Автор: Heidtman Matthew Ian, McCoy John M., Merighi Massimo
Принадлежит:

The invention provides compositions and methods for engineering or other host production bacterial strains to produce fucosylated oligosaccharides, and the use thereof in the prevention or treatment of infection. 1. A method for producing a fucosylated oligosaccharide in a bacterium comprising providing bacterium comprising an exogenous lactose-utilizing α(1 ,2) fucosyltransferase enzyme , wherein the amino acid sequence of said enzyme comprises at least 22% but less than 40% identity to FutC (SEQ ID NO: 1).2. A method for producing a fucosylated oligosaccharide in a bacterium comprising providing bacterium comprising an exogenous lactose-utilizing α(1 ,2) fucosyltransferase enzyme , wherein the amino acid sequence of said enzyme comprises at least 25% identity to FutN (SEQ ID NO: 3).3LachnospiraceaeTannerellaClostridium bolteaeMethanosphaerula palustriesAkkermansia muciniphiliaClostridium bolteae. The method of or , wherein said α(1 ,2) fucosyltransferase enzyme comprises , sp. FutQ , sp. FutS , +13 FutP , FutR , FutY , FutP , or a functional variant or fragment thereof.4. The method of claim 1 , wherein said α(1 claim 1 ,2) fucosyltransferase enzyme comprises any one of amino acid sequences SEQ ID NO: 10-21 and 292 claim 1 , or a functional variant or fragment thereof.5. The method of claim 1 , further comprising retrieving the fucosylated oligosaccharide from said bacterium or from a culture supernatant of said bacterium.6. The method of claim 1 , wherein said fucosylated oligosaccharide comprises 2′-fucosyllactose (2′-FL) claim 1 , lactodifucotetraose (LDFT) claim 1 , Lacto-N-fucopentaose I (LNF I) claim 1 , or lacto-N-difucohexaose I (LDFH I).7. The method of claim 1 , wherein the bacterium further comprises an exogenous lactose-utilizing α(1 claim 1 ,3) fucosyltransferase enzyme and/or an exogenous lactose-utilizing α(1 claim 1 ,4) fucosyltransferase enzyme.8Helicobacter pylori. The method of claim 7 , wherein the exogenous lactose-utilizing α(1 claim 7 ,3) ...

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Номер записи: 52
25-03-2021 дата публикации

THERAPEUTIC DRUG FOR NEURODEGENERATIVE DISEASE AND APPLICATION THEREOF

Номер: US20210087214A1
Автор: AN Yuqian, Cao Xin, HUANG Shichao, Lu Jing, Pei Gang, SHI Fuchun, Yu Biao, Zhou Yue
Принадлежит: SHANGHAI DONGXI ZHIHUI BIOLOGICAL MEDICINE CO., LTD.

The present invention relates to a novel therapeutic drug for a neurodegenerative disease and an application thereof. Provided is a novel compound of formula (I). The compound can effectively facilitate the proliferation of neural stem cells in both in vitro and in vivo experiments and can be used as a treatment approach for facilitating neuroregeneration to fight against cognitive decline associated with aging or a neurodegenerative disease. 2. The compound of formula (I) or an isomer claim 1 , a solvate or a precursor thereof claim 1 , or their pharmaceutically acceptable salts as defined in claim 1 , whereinR1 to R4 are each independently selected from hydrogen, hydroxyl and C1 to C2 alkyl.4. A medicament or a medicine kit comprising the compound of formula (I) or an isomer claim 1 , a solvate or a precursor thereof claim 1 , or their pharmaceutically acceptable salts as defined in for preventing claim 1 , alleviating or treating neurodegenerative diseases claim 1 , depression or stroke.5. A medicament or a medicine kit as defined in claim 4 , wherein the neurodegenerative diseases areneurodegenerative diseases characterized by the occurrence of neuroinflammation in the brain; orneurodegenerative diseases characterized by a significant increase in Aβ production; orneurodegenerative diseases characterized by a significant decline in learning and memory ability; orneurodegenerative diseases characterized by a decline in the function of neural stem cells; orneurodegenerative diseases characterized by a decline in motor coordination ability; orneurodegenerative diseases characterized by a decrease in the number of dopaminergic neurons in substantia nigra; orneurodegenerative diseases characterized by a decrease in the level of striatal dopaminergic nerve fibers.6. A medicament or a medicine kit as defined in claim 5 , wherein the neurodegenerative diseases include Alzheimer's disease claim 5 , Parkinson's disease claim 5 , dementia with Lewy bodies claim 5 , ...

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Номер записи: 53
01-04-2021 дата публикации

N-ACYLETHANOLAMIDE DERIVATIVES AND USES THEREOF

Номер: US20210093589A1
Автор: Levin Andrew D.
Принадлежит: ELIEM THERAPEUTICS, INC.

The present disclosure provides certain N-Acylethanolamide derivatives, and uses relating thereto. 2. The compound of claim 1 , wherein the compound is a salt.3. The compound of claim 2 , wherein the salt is a pharmaceutically acceptable salt.4. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.5. The pharmaceutical composition of claim 4 , comprising one or more additional therapeutic agents.6. The pharmaceutical composition of claim 4 , which is formulated for oral delivery.7. The pharmaceutical composition of claim 6 , which is formulated as a solid formulation.8. The pharmaceutical composition according to claim 7 , wherein the solid formulation is a capsule.9. The pharmaceutical composition according to claim 8 , wherein the capsule encloses a liquid.10. A method of treating pain comprising administering the compound according to or a pharmaceutically acceptable salt thereof to a patient in need thereof.11. A method of treating inflammatory pain comprising administering the compound according to or a pharmaceutically acceptable salt thereof to a patient in need thereof.12. A method of treating neuropathic pain comprising administering the compound according to or a pharmaceutically acceptable salt thereof to a patient in need thereof.13. A method of treating pain comprising administering the pharmaceutical composition according to to a patient in need thereof.14. A method of treating inflammatory pain comprising administering the pharmaceutical composition according to to a patient in need thereof.15. A method of treating neuropathic pain comprising administering the pharmaceutical composition according to to a patient in need thereof. This application is a continuation of U.S. application Ser. No. 16/349,548, which is a U.S. national phase entry under Section 371 of International Application No. PCT/US2017/056353, filed on Oct. 12, 2017, which published as WO/2018/ ...

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Номер записи: 54
05-04-2018 дата публикации

OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE CONSTRUCT USING THE SAME, AND METHODS FOR PRODUCING THEM

Номер: US20180094017A1
Автор: Kitade Yukio, SHIBATA Aya
Принадлежит: GIFU UNIVERSITY

The oligonucleotide derivative of the present invention is represented by Formula (1). This derivative is considered to be introduced into cells by binding of its amino sugar chain moiety to a ligand on cell surfaces, and have selective drug delivery function. The oligonucleotide derivative can be easily synthesized and introduced into cells without using a lipofection reagent. 122-. (canceled)25. The oligonucleotide derivative according to claim 23 , wherein the modified or unmodified oligonucleotides have a partial structure —(CH)n— claim 23 , where n is a natural number of 1 or greater.26. The oligonucleotide derivative according to claim 24 , wherein the modified or unmodified oligonucleotides have a partial structure —(CH)n— claim 24 , where n is a natural number of 1 or greater.27. The oligonucleotide derivative according to claim 23 , wherein Rand Rare H.28. The oligonucleotide derivative according to claim 24 , wherein Rand Rare H.29. The oligonucleotide derivative according to claim 23 , wherein b is 0.30. The oligonucleotide derivative according to claim 24 , wherein b is 0.31. The oligonucleotide derivative according to claim 23 , wherein a and b are both 0.32. The oligonucleotide derivative according to claim 24 , wherein a and b are both 0.33. The oligonucleotide derivative according to claim 23 , wherein c is 1 or more and 5 or less.34. The oligonucleotide derivative according to claim 24 , wherein c is 1 or more and 5 or less.35. The oligonucleotide derivative according to claim 23 , wherein A and B have a partial sequence of mRNA of a predetermined gene or a complementary sequence thereof.36. The oligonucleotide derivative according to claim 24 , wherein A and B have a partial sequence of mRNA of a predetermined gene or a complementary sequence thereof.37. The oligonucleotide derivative according to claim 23 , wherein the total chain length of A and B is 10 or more and 35 or less.38. The oligonucleotide derivative according to claim 24 , wherein the ...

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Номер записи: 55
28-03-2019 дата публикации

METHOD FOR PREPARING SUCRALOSE-6-ACETATE IN BIPHASIC LIQUID-LIQUID SYSTEM

Номер: US20190092801A1
Автор: DENG FUXIANG, Ding Yu, LI Haoran, Xue Wei, YAN WENWU, Yu Ming, Yu Sheng, ZHOU YOUGUI
Принадлежит:

The present invention discloses a method for preparing sucralose-6-acetate in a biphasic liquid-liquid system. The method comprises slowly dropwise adding an inert non-polar solvent containing a chlorinating agent to an N,N-dimethyl formamide (DMF) solution of sucrose-6-acetate; then reacting the biphasic liquid-liquid mixture at a certain temperature for 9-20 hours; cooling the system to room temperature after stopping heating, and settling the solution to form layers, an upper layer being an inert non-polar solvent layer, and a lower layer being a DMF solution layer containing the product; hydrolyzing, neutralizing, and filtering the lower layer to obtain a filtrate, and then concentrating the filtrate to obtain a concentrate; dissolving the concentrate in water, and obtaining the product by extraction using ethyl acetate and crystallization, the inert non-polar solvent being an alkane solvent containing 8-18 carbon atoms that is not mutually soluble with DMF. The method has a high product yield, and can significantly reduce the decomposition of DMF, thereby reducing costs. 1. A method for preparing sucralose-6-acetate in a biphasic liquid-liquid system , characterized in that method comprises the following steps:1) in the biphasic liquid-liquid system formed by an inert non-polar solvent and N,N-dimethylformamide, sucrose-6-acetate and a chlorinating agent engaging in chlorination through heating; cooling, settling the solution to form layers upon completion of reaction, and then taking a DMF (N,N-dimethylformamide) solution layer containing a product;2) conducting hydrolyzed neutralization of the DMF solution layer containing the product as obtained in Step 1) to further obtain a filtrate through filtration;3) proceeding with concentration, extraction and crystallization of the filtrate obtained in Step 2) to further obtain the product, which is sucralose-6-acetate;wherein the inert non-polar solvent as described in Step 1) is an alkane solvent containing 8-18 ...

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Номер записи: 56
12-05-2022 дата публикации

Nutritional supplements and therapeutic compositions comprising (r)-3- hydroxybutyrate derivatives

Номер: US20220145338A1
Автор: Clarke Kieran, King Michael Todd, Veech Richard Lewis
Принадлежит:

Novel compounds and compositions containing (R)-3-hydroxybutyrate derivatives are disclosed. The compounds and compositions can be used as nutritional supplements to increase physical performance and as therapeutics to ameliorate symptoms of medical conditions, particularly neurological conditions, such as Alzheimer's and similar conditions. Novel methods for making R-3-hydroxybutyrate derivatives also are disclosed. Exemplary methods employ a supercritical solvent, such as supercritical carbon dioxide, and employ a lipase catalyzed esterification or transesterification reaction to produce the (R)-3-hydroxybutyrate derivatives. 2. The compound of claim 1 , wherein R is glycerol.3. The compound of claim 2 , wherein:m is 2;n is 3; andx is 3.4. The compound of claim 2 , wherein:m is 3;n is 3; andx is 3.5. The compound of claim 1 , wherein R is glucose.6. The compound of claim 5 , wherein:m is 5;n is 1; andx is 5.7. The compound of claim 1 , wherein R is galactose.8. The compound of claim 7 , wherein:m is 1;n is 5; andx is 5.9. The compound of claim 7 , wherein:m is 4;n is 3; andx is 5.10. The compound of claim 1 , wherein R is mannitol.11. The compound of claim 10 , wherein:m is 6;n is 2; andx is 6.12. The compound of claim 1 , wherein R is sucrose.13. The compound of claim 12 , wherein:m is 7;n is 1; andx is 7.14. The compound of claim 12 , wherein:m is 7;n is 3; andx is 7.15. The compound of claim 12 , wherein:m is 1;n is 6; andx is 7.16. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier. This application claims the benefit of U.S. Provisional Application Nos. 60/485,848 and 60/529,873, filed Jun. 3, 2003 and Dec. 15, 2003, respectively. Both of these prior applications are incorporated herein by reference in their entireties.The disclosure concerns compounds and compositions containing (R)-3-hydroxybutyrate derivatives effective for elevating blood concentrations of ketone bodies and methods for using such compounds and ...

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Номер записи: 57
26-06-2014 дата публикации

METHOD AND COMPOSITIONS

Номер: US20140178434A1
Автор: "Al Dulayymi Jumaa Raheem Najeem", Baird Mark Stephen, Beken Seppe Vander, Grooten Johan Adriaan Marc, Maza-Inglesias Maximilliano
Принадлежит: Bangor University

A method of preparing a compound of formula (III): 2. A method according to claim 1 , wherein x is 1 claim 1 , y is 2 and z is 0 or 1.3. A method according to claim 2 , wherein the compound of formula III comprises a trehalose unit.4. A method according to claim 1 , wherein R is an unsubstituted alkyl chain having 16 to 30 carbon atoms; Ris an alkyl chain having from 12 to 24 carbon atoms; each of R claim 1 , R′ and Ris an alkylene moiety having from 6 to 20 carbon atoms.5. A method according to claim 1 , wherein Rand Rhave a combined total of from 10 to 20 carbon atoms and X includes a cyclopropyl unit.6. The method of claim 1 , wherein the composition further comprises:a pharmaceutically acceptable carrier.7. The method of claim 1 , wherein determining whether the antibody in the body fluid has bound to the compound of formula III includes detecting a second claim 1 , marked antibody bound to the antibody in the body fluid.8. The method of claim 1 , wherein the body fluid is selected from a group consisting of: blood claim 1 , serum claim 1 , plasma claim 1 , pleural effusion claim 1 , ascites fluid claim 1 , and urine.9Mycobacterium tuberculosis.. The method of claim 1 , wherein the pathogen is This application is a divisional of co-pending U.S. patent application Ser. No. 13/146,997 filed on Jul. 29, 2011, which is a 371 National Stage Application of PCT/GB2010/050146 filed Jan. 29, 2010, which claims priority to GB Application No. 0901465.5 filed Jan. 29, 2009. The applications identified above are incorporated herein by reference in their entireties for all that they contain in order to provide continuity of disclosure.The present invention relates to sugar esters of individual mycolic acids, to compositions comprising the same and to methods and uses relating thereto.Mycolic acids are long chain fatty acid compounds typically having 60 to 90 carbon atoms and are found as components of the cells of mycobacteria. An example of such bacteria isTwo moieties can ...

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Номер записи: 58
23-04-2015 дата публикации

Disaccharide Synthetic Lipid Compounds and Uses Thereof

Номер: US20150110854A1
Автор: Burgess Stephen W, Hickman David T, LI Shengrong, Lopez-Deber Maria Pilar, Shaw Walter A
Принадлежит:

Essentially pure compounds of the formulas (I) to (XXV) are provided. Compositions and methods for enhancing or stimulating an immune response are also provided. The compounds, provided are advantageous in that the compounds are essentially pure and free from contaminants encountered when such compounds are purified from natural sources. 3. The essentially pure compound of claim 2 , wherein AA claim 2 , and Aare each independently Cto Cunsubstituted alkyl and Aand Aare each independently are Cto Cunsubstituted alkyl.6. The essentially pure compound of claim 5 , wherein AA claim 5 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.9. The essentially pure compound of claim 8 , wherein A claim 8 , A claim 8 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.11. The essentially pure compound of claim 1 , wherein the compounds is at least 95% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.12. The essentially pure compound of claim 5 , wherein the compounds is at least 99% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.15. The pharmaceutical composition of claim 14 , wherein A claim 14 , A claim 14 , and Aare each independently Cto Cunsubstituted alkyl and Aand Aare each independently are Cto Cunsubstituted alkyl.18. The pharmaceutical composition of claim 17 , wherein AA claim 17 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.21. The pharmaceutical composition of claim 20 , wherein A claim 20 , A claim 20 , and Aare each independently Cto Cunsubstituted alkyl and Ais a Cto Cunsubstituted alkyl.23. The pharmaceutical composition of claim 13 , wherein the compounds is at least 95% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.24. The pharmaceutical composition of claim 13 , wherein the compounds is at least 99% ...

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Номер записи: 59
03-07-2014 дата публикации

PREPARATION OF POLY ALPHA-1,3-GLUCAN ESTERS AND FILMS THEREFROM

Номер: US20140187766A1
Автор: Kasat Rahul B., PAULLIN JAYME L.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Poly alpha-1,3-glucan ester compounds are disclosed herein with a degree of substitution of about 0.05 to about 3.0. Also disclosed are methods of producing poly alpha-1,3-glucan ester compounds and films made therefrom. 1. A film comprising poly alpha-1 ,3-glucan ester having at least one of:(a) a tear resistance of at least about 0.1 gf/mil;{'sup': '2', '(b) a tensile strength of at least about 10 kg/mm; or'}(c) a haze of less than about 20%.2. The film of claim 1 , wherein the poly alpha-1 claim 1 ,3-glucan ester used is poly alpha-1 claim 1 ,3-glucan acetate.3. The film of claim 1 , wherein the film has at least one of:(a) a tear resistance from about 2.0 to about 2.4 gf/mil;{'sup': '2', '(b) a tensile strength of at least about 200 kg/mm; or'}(c) a haze of less than about 10%.4. The film of claim 3 , wherein the poly alpha-1 claim 3 ,3-glucan ester used is poly alpha-1 claim 3 ,3-glucan acetate.5. A method to prepare a poly alpha-1 claim 3 ,3-glucan ester film comprising:(a) providing poly alpha-1,3-glucan ester;(b) contacting the poly alpha-1,3-glucan ester of (a) with a solvent to make a solution of poly alpha-1,3-glucan ester;(c) applying the solution of poly alpha-1,3-glucan ester on a surface; and(d) allowing the solvent to evaporate to provide the poly alpha-1,3-glucan ester film.6. The method of claim 5 , wherein the poly alpha-1 claim 5 ,3-glucan ester used is poly alpha-1 claim 5 ,3-glucan acetate.7. The method of claim 5 , wherein the solvent is acetone. This application claims the benefit of U.S. Provisional Application Nos. 61/746,328; 61/746,335 and 61/746,338; each filed Dec. 27, 2012, all of which are incorporated herein by reference in their entirety.This invention is in the field of poly alpha-1,3-glucan derivatives. Specifically, this invention pertains to poly alpha-1,3-glucan esters, methods of their preparation and films made therefrom.Driven by a desire to find new structural polysaccharides using enzymatic syntheses or genetic engineering ...

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Номер записи: 60
02-04-2020 дата публикации

THIOSCCHARIDE MUCOLYTIC AGENTS

Номер: US20200102340A1
Автор: CARRINGTON Stephen, FAHY John Vincent, Oscarson Stefan, YUAN Shaopeng
Принадлежит:

There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods. 2. The method of claim 1 , wherein said method comprises decreasing mucus viscoelasticity in said subject.396-. (canceled)98. The pulmonary pharmaceutical composition of claim 97 , wherein said pulmonary pharmaceutical carrier is a pulmonary pharmaceutical liquid or pulmonary pharmaceutical powder.99. The pulmonary pharmaceutical composition of claim 98 , wherein said pulmonary pharmaceutical liquid comprises a polar liquid claim 98 , and said thiol saccharide mucolytic agent is dissolved or suspended in said polar liquid.100. The pulmonary pharmaceutical composition of claim 99 , wherein said polar liquid is water.101. The pulmonary pharmaceutical composition of claim 98 , wherein said pulmonary pharmaceutical carrier is lactose claim 98 , mannitol claim 98 , a phospholipid or cholesterol.102. The pulmonary pharmaceutical composition of claim 98 , wherein said pulmonary pharmaceutical carrier is the parent sugar of said thiol saccharide mucolytic agent claim 98 , said parent sugar lacking a thiol moiety.103. The pulmonary pharmaceutical composition of claim 97 , wherein said pulmonary pharmaceutical composition is within a pulmonary pharmaceutical delivery device.104. The pulmonary pharmaceutical composition of claim 103 , wherein said pulmonary pharmaceutical delivery device is a pulmonary pharmaceutical nebulizer claim 103 , a pulmonary pharmaceutical dry powder inhaler claim 103 , or a pulmonary pharmaceutical pressurized metered close inhaler. This application is a divisional of U.S. patent application Ser. No. 15/822,616, filed Nov. 27, 2017, which is a divisional of U.S. patent application Ser. No. 14/847,439, filed Sep. 8, 2015, which is a continuation ...

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Номер записи: 61
02-04-2020 дата публикации

Agricultural Coating Containing Sugar Ester and Methods

Номер: US20200102457A1
Автор: Goldstein Larry, Hayes Melissa C., JR. Arthur R., PEEDEN Gregory S., SHIRLEY
Принадлежит: Renuvix LLC

The invention is a coating for agricultural products, which includes at least 10% of renewably sourced and biodegradable sugar esters. The invention is also a method of making a coated agricultural product, including the steps of providing a coating composition comprising at least 10% of a renewably sourced and biodegradable sugar ester, heating the coating composition to a temperature to reduce its viscosity to below about 100 cP, adding the coating composition to an agricultural product to form a mixture, and cooling the mixture to produce a coated agricultural product. The invention is also a method of reducing dust released from an agricultural product that includes the step of providing a coating composition comprising at least 10% of a renewable sourced and biodegradable sugar ester. Enough of the coating composition is added to the agricultural product to reduce the amount of dust released from the agricultural product by at least half. Finally, the invention is also a method of reducing caking in a granular agricultural product. 1. A coating for agricultural products , the coating comprising at least 10% of renewably sourced and biodegradable sugar esters.2. The invention of wherein the agricultural product is a granular or prilled fertilizer.3. The invention of wherein the agricultural product is seed.4. The invention of wherein the agricultural product is a granular or prilled pesticide.5. The invention of wherein the sugar ester is sucrose ester.6. The invention of wherein the sucrose ester is sucrose octaester.7. The invention of wherein the ester portion of the sucrose ester compound is derived from soybean oil claim 1 , high oleic soybean oil claim 1 , hydrogenated soybean oil claim 1 , high oleic soybean oil claim 1 , sunflower oil claim 1 , safflower oil claim 1 , canola oil claim 1 , corn oil claim 1 , tung oil claim 1 , palm oil claim 1 , cottonseed oil claim 1 , linseed oil claim 1 , rapeseed oil claim 1 , camelina oil claim 1 , jatropha oil claim ...

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Номер записи: 62
26-04-2018 дата публикации

BIOCONJUGATE MOLECULES WITH BIOLOGICAL AND TECHNO-FUNCTIONAL ACTIVITY, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF

Номер: US20180110869A1
Автор: ARRIZON GAVINO Javier Placido, CASAS GODOY Leticia, GONZÁLEZ ÁVILA Marisela, MARTINEZ VELAZQUEZ Moises, PADILLA CAMBEROS Eduardo, SANDOVAL FABIAN Georgina Coral, VILLANUEVA RODRIGUEZ Socorro Josefina
Принадлежит:

The present invention regards the synthesis of bioconjugated molecules, formed between two or more of the following functional groups: sugars, prebiotics, oligosaccharides, polysaccharides, triglycerides, fatty acids, fatty acids esters, anti-inflammatories; with its production process by biocatalyzed synthesis with hydrolases such as esterases, proteases, lipases or cutinases, and its purification with several methods that include washing and drying. In addition, its applications in foods, pharmaceuticals and cosmetics, such as: prebiotic nutraceutical, anti-inflammatory, antitumoral, intestinal vector, techno-functional ingredient for food applications (emulsifier, fat substitute) and cosmetic emollient; which are possible since these are non toxic molecules according to the Ames tests. 1. (canceled)2. (canceled)3. (canceled)4. A process for the production of bioconjugated molecules with biological and techno-functional activities with a weight ratio of 1:1 to 1:10 of sugars , oligosaccharides or branched polysaccharides: carboxylic acid or its derivative , the process including the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. producing a reaction by mixing on a hermetically closed recipient with agitation at 100-1000 r.p.m. and incubation at 40-80° C., two substrates according to in a proportion of 1:1 to 1:10 w/w, in presence of an enzyme in a proportion of 1:1 to 1:10 w/w to the acylating agent; with or without solvent that if it is added is in a ratio of 1:2 to 1:100 w/v;'}b. filtering with Whatman filters numbers 1,3,4, or similar, or centrifuge for separation of the organic solvent and the immobilized enzyme;c. recovering the bioconjugates from the “organic phase” by solvent evaporation at reduced pressure (vacuum) in a rotary evaporator, heating at a temperature where the solvent boils depending on the vacuum used, or by heating at a temperature above the solvent boiling point; and{'b': '4', 'd. recovering the bioconjugates from the “solid ...

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Номер записи: 63
30-04-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF CARDIOVASCULAR AND NEUROLOGICAL DISEASES

Номер: US20150119344A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II or formula III and methods for the treatment of cardiovascular and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, postprandial hyperglycemia, depression, Alzheimer's disease, Parkinson's disease, Huntington's disease, inflammation, Crohn's disease, inflammatory bowel disease and obesity. 4. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.6. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.7. The pharmaceutical composition of claim 4 , which is formulated to treat cardiovascular and neurological diseases the underlying etiology with an effective amount administering the patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration or transdermal administration.8. The pharmaceutical composition of claim 5 , which is formulated to treat cardiovascular and ...

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Номер записи: 64
26-04-2018 дата публикации

THIOSACCHARIDE MUCOLYTIC AGENTS

Номер: US20180111955A1
Автор: CARRINGTON Stephen, FAHY John Vincent, Oscarson Stefan, YUAN Shaopeng
Принадлежит:

There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods. 2. The use of claim 1 , wherein said method comprises decreasing mucus viscoelasticity in said subject.3. (canceled)4. The use of claim 1 , wherein said thiosaccharide mucolytic agent comprises D-glucopyranose claim 1 , D-galactopyranose claim 1 , D-mannopyranose claim 1 , D-glucopyranoside claim 1 , D-galactopyranoside claim 1 , or D-mannopyranoside moieties.5. The use of claim 1 , wherein said thiosaccharide mucolytic agent comprises D-galactopyranose.668.-. (canceled)69. The method of claim 1 , wherein{'sup': 1', '1A, 'Ris —OR; and'}{'sup': 2', '3', '5', '7', '8', '9, 'R, R, R, R, R, and Rare —OH; and'}{'sup': 10', '10A, 'Ris —SH or —OR.'}707. The method of claim claim 1 , wherein{'sup': '1A', 'sub': 1', '10, 'Ris substituted or unsubstituted C-Cthiol-alkyl or substituted or unsubstituted 2 to 10 membered thiol-heteroalkyl.'}71. The method of claim 70 , wherein{'sup': '1A', 'sub': 1', '10, 'Ris unsubstituted C-Cthiol-alkyl; and'}{'sup': '10', 'Ris —OH.'}72. The method of claim 71 , wherein Ris thioethyl.73. The method of claim 69 , wherein{'sup': '1A', 'Ris H; and'}{'sup': '10', 'Ris —SH.'}74. The method of claim 1 , wherein{'sup': '1A', 'sub': 1', '10, 'Ris substituted or unsubstituted C-Cthiol-alkyl or substituted or unsubstituted 2 to 10 membered thiol-heteroalkyl;'}{'sup': 2', '3', '5', '7', '8', '9, 'R, R, R, R, R, and Rare —OH; and'}{'sup': '10', 'Ris —SH.'}75. The method of claim 74 , wherein Ris unsubstituted C-Cthiol-alkyl.76. The method of claim 75 , wherein R1A is thioethyl.77. The method of claim 1 , wherein{'sup': 1', '3', '5', '8', '9', '10, 'R, R, R, R, R, and Rare —OH;'}{'sup': 2', '2B, 'Ris —OH or NR;'}{'sup': '2C', 'sub': 1', '10, 'Ris ...

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Номер записи: 65
10-07-2014 дата публикации

METHODS FOR THE SYNTHESIS OF FUNCTIONALIZED NUCLEIC ACIDS

Номер: US20140194610A1
Автор: Butler David Charles Donnell, IWAMOTO Naoki, Meena Meena, VERDINE Gregory L.
Принадлежит:

Described herein are methods for the synthesis of derivatives of thiosulfonate reagents. Said reagents have utility for the synthesis of phosphorothiotriesters from H-phosphonates in a stereospecific fashion. 3. The process of claim 2 , wherein W is O.5. The process of claim 2 , wherein the silylating reagent is selected from1,1,3,3-tetramethyl-1,3-diphenyldisilazane;1,3-dimethyl-1,1,3,3-tetraphenyldisilazane;1-(trimethylsilyl)imidazole;N-trimethylsilyl-N-methyl trifluoroacetamide;bis(dimethylamino)dimethylsilane;bromotrimethylsilane;chlorodimethyl(pentafluorophenyl)silane;chlorotriethylsilane;chlorotriisopropylsilane;chlorotrimethylsilane;dichlorodimethylsilane;hexamethyldisilazane;N,N′-bis(trimethylsilyl)urea;N,N-bis(trimethylsilyl)methylamine;N,N-dimethyltrimethylsilylamine;N,O-bis(trimethylsilyl)acetamide;N,O-bis(trimethylsilyl)carbamate;N,O-bis(trimethylsilyl)trifluoroacetamide;N-methyl-N-(trimethylsilyl)trifluoroacetamide;N-methyl-N-trimethylsilylacetamide;N-methyl-N-trimethylsilylheptafluorobutyramide;N-tert-butyldimethylsilyl-N-methyltrifluoroacetamide;N-methyl-N-trimethylsilylheptafluorobutyramide;trimethylsilyltriflate;triethylsilyltriflate;triisopropylsilyltriflate; ortert-butyldimethylsilyltriflate.6. The process of claim 5 , wherein the silylating reagent is selected from N claim 5 ,O-bis(trimethylsilyl)trifluoroacetamide claim 5 , trimethylsilyltriflate claim 5 , chlorotrimethylsilane claim 5 , or 1-(trimethylsilyl)imidazole.7. The process of claim 6 , wherein the silylating reagent is selected from N claim 6 ,O-bis(trimethylsilyl)trifluoroacetamide.8. The process of claim 2 , wherein the H-phosphonate is covalently linked to a solid phase.10. The process of claim 8 , wherein the phosphorothiotriesters of structure IIIb comprise non-stereorandom phosphorous linkages and the H-phosphonate of structure Ic comprise non-stereorandom phosphorous linkages; and W is independently selected from O claim 8 , NH claim 8 , or CH.11. The process of claim 10 , ...

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Номер записи: 66
30-04-2015 дата публикации

CHEMOENZYMATIC METHODS FOR SYNTHESIZING MOENOMYCIN ANALOGS

Номер: US20150119561A1
Автор: Doud Emma, Gampe Christian M., Kahne Daniel Evan, Kahne Suzanne Walker, Tsukamoto Hirokazu
Принадлежит:

The present invention provides methods of synthesizing moenomycin analogs of Formula (I). The present invention also provides compositions comprising a compound of Formula (I) and kits for synthesizing compounds of Formula (I). 2. The method of claim 1 , wherein Ris optionally substituted aliphatic.3. The method of claim 1 , wherein Ris —(CH)—C(O)R.45-. (canceled)6. The method of claim 1 , wherein Ris optionally substituted aliphatic.7. The method of claim 6 , wherein Ris methyl or —CH═CH.89-. (canceled)10. The method of claim 6 , wherein Ris substituted with halo A —CN claim 6 , —NC claim 6 , —NCO claim 6 , —OCN claim 6 , —NCS claim 6 , —SCN claim 6 , —NO claim 6 , —N claim 6 , an amino group claim 6 , a hydroxyl group claim 6 , aryl claim 6 , heteroaryl claim 6 , or optionally substituted heterocyclyl.1121-. (canceled)22. The method of claim 1 , wherein Ris —CHaryl or —CHheteroaryl.2348-. (canceled)5051-. (canceled)52. The method of claim 1 , wherein the compound of formula (III) is GalNAz claim 1 , galactosamine claim 1 , GalNAc.5354-. (canceled)55. The method of claim 1 , wherein{'sup': '1', 'sub': '2', 'Ris —C(O)NH;'}{'sup': '2', 'Ris hydrogen;'}{'sup': '3', 'Ris —OH;'}W is —O—;{'sup': '4', 'Ris hydrogen;'}{'sup': '5', 'sub': '3', 'Ris —C(O)CH;'}{'sup': '6', 'Ris —OH;'}{'sup': '7', 'Ris —OH;'}{'sup': 'a', 'Ris hydrogen; and'}{'sup': 'b', 'Ris hydrogen.'}5758-. (canceled)59. The method of claim 1 , wherein Ris C(O)NHor —CHOH.60. (canceled)61. The method of claim 1 , wherein Ris hydrogen; and Ris —OH; or Ris hydrogen; and Ris —OH.62. (canceled)63. The method of claim 1 , wherein —W—Ris —OH claim 1 , —NHC(O)NH claim 1 , —OC(O)NHor —NHC(═NH)NH.6466-. (canceled)67. The method of claim 1 , wherein Ris —C(O)CH.68. (canceled)69. The method of claim 1 , wherein Ris —OH or —OR; wherein Ris a carbohydrate moiety.70. The method of claim 1 , wherein Ris —OH.7183-. (canceled)86. A kit comprising a compound of Formula (III) and a GalT enzyme.8792-. (canceled) The present ...

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Номер записи: 67
13-05-2021 дата публикации

DIARYL TREHALOSE COMPOUNDS AND USES THEREOF

Номер: US20210139521A1
Автор: BURKHART David, Ettenger George, Evans Jay, Ryter Kendal T., SMITH Alyson
Принадлежит:

Disclosed herein are diaryl trehalose compounds and methods of use thereof, for example as vaccine adjuvants. 2. The compound of claim 1 , or a pharmaceutical salt thereof claim 1 , wherein p and q are 0.4. The compound of claim 3 , or a pharmaceutical salt thereof claim 3 , wherein R claim 3 , when present claim 3 , is hydrogen.5. The compound of claim 4 , or a pharmaceutical salt thereof claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , R claim 4 , and Rare each independently selected from hydrogen claim 4 , C-Calkyl claim 4 , hydroxy claim 4 , C-Calkoxy claim 4 , halo claim 4 , C-Chaloalkyl claim 4 , aryl claim 4 , C-Calkoxy-C-Calkoxy claim 4 , C-Calkoxy-C-Calkyl claim 4 , and hydroxy-C-Calkyl;{'sup': 3a', '4a, 'wherein Rand R, together with the carbon atoms to which they are attached, are optionally taken together to form an aryl ring.'}7. The compound of claim 6 , or a pharmaceutical salt thereof claim 6 , wherein R claim 6 , when present claim 6 , is hydrogen.8. The compound of claim 7 , or a pharmaceutical salt thereof claim 7 , wherein R claim 7 , R claim 7 , R claim 7 , R claim 7 , and Rare each independently selected from hydrogen claim 7 , C-Calkyl claim 7 , hydroxy claim 7 , C-Calkoxy claim 7 , halo claim 7 , C-Chaloalkyl claim 7 , aryl claim 7 , C-Calkoxy-C-Calkoxy claim 7 , C-Calkoxy-C-Calkyl claim 7 , and hydroxy-C-Calkyl;{'sup': 3b', '4b, 'wherein Rand R, together with the carbon atoms to which they are attached, are optionally taken together to form an aryl ring.'}1019-. (canceled)20. The compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein m and n are 0.2250-. (canceled)51. The compound of selected from the group consisting of:6,6′-bis(3,5-diethoxybenzoyl)-α,α-D-trehalose,6,6′-bis(2-hydroxy-3,5-di-tert-butylbenzoyl)-α,α-D-trehalose,6,6′-bis(3,5-dipentyloxybenzoyl)-α,α-D-trehalose,6,6′-bis(3,4,5-triethoxybenzoyl)-α,α-D-trehalose, and6,6′-bis(2-hydroxy-3,5-di-tert-butylbenzoylamino)-α,α-D-trehalose, and6,6′-bis(2, ...

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Номер записи: 68
17-07-2014 дата публикации

Polyols, preparation and use thereof

Номер: US20140200327A1
Автор: Christian Koenig, Sebastian Koch
Принадлежит: BASF SE

The present invention relates to polyols and the preparation and use thereof.

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Номер записи: 69
25-08-2022 дата публикации

ESTER COMPOUNDS CONTAINING POLYOL AND SACCHARIDE GROUPS EFFECTIVE IN TREATING HEPATOTOXICITY AND USES THEREOF

Номер: US20220265587A1
Автор: HO Hsin-Tien, HSIONG Cheng-Huei, HU Oliver Yoa-Pu, SHIH Tung-Yuan
Принадлежит: SINEW PHARMA INC.

The present invention relates to compounds effective in treating hepatotoxicity and fatty liver diseases and uses thereof. The present compound is represented by Formula (II), which has the formula: R—O—X—(CH)—X—O—R, wherein: each X is —C(═O)—; Ris a C-Calkyl polyol; Ris a saccharide group of formula (G); G is a monosaccharide residue, where (i) at least one of the —OH groups in (G)is substituted by a halogen atom, and (ii) the saccharide group of formula (G)is linked to —O— through a —CHgroup; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. 2. The compound of claim 1 , wherein two or more of the —OH groups in formula (G)are substituted by halogen atoms.3. The compound of claim 1 , wherein the saccharide group is a hexose.4. The compound of claim 3 , wherein the hexose is an aldohexose or a ketohexose.5. The compound of claim 1 , wherein the saccharide group is represented by -G-O-G claim 1 , wherein Gand Gare the same or different.6. The compound of claim 5 , wherein at least one of the —OH groups in -G-O-Gis substituted by a halogen atom selected from the group consisting of chlorine claim 5 , bromine and iodine.7. The compound of claim 6 , wherein the halogen atom is a chlorine atom.8. The compound of claim 6 , wherein{'sub': '1', 'Gis glucose, wherein one —OH group is substituted by a chlorine atom; and'}{'sub': '2', 'Gis fructose, wherein two —OH groups are substituted by chlorine atoms.'}10. The compound of claim 1 , whereinm is 4; andn is 4.11. The compound of claim 1 , wherein{'sub': '1', 'claim-text': [{'sub': 2', 'p, 'Ris a saccharide group of formula (G)'}, {'sub': 'p', 'wherein G is a monosaccharide residue and p is 1, 2, 3, 4, 5 or 6 in which at least one of the hydroxyl groups in (G)is substituted by a halogen atom; or'}], '(i) Ris hydrogen; and'}{'sub': 1', '2', 'p, 'claim-text': {'sub': 'p', 'wherein G is a monosaccharide residue and p is 1, 2, 3, 4, 5 or 6 in which at least one of the hydroxyl groups in (G)is substituted by a halogen atom, '( ...

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Номер записи: 70
04-05-2017 дата публикации

Hydrolysis Resistant Sialic Acid Derivatives and Methods for Their Use

Номер: US20170121361A1
Автор: BAUMANN Lars, MORLEY Thomas J., WITHERS STEPHEN G.
Принадлежит: The University of British Columbia

This invention provides compound having a structure of Formulas: Furthermore, methods and uses of such compounds for covalently bonding to a sugar acceptor, to form modified protein therapeutics having reduced enzymatic hydrolysis, improved biological stability or an improved pharmacokinetic property. 3. The compound of claim 1 , wherein the ester is independently selected from one or more of the following: a linear or branched acetate claim 1 , a linear or branched propionate claim 1 , a linear or branched butyrate claim 1 , a linear or branched pentanoate claim 1 , a linear or branched hexanoate claim 1 , a linear or branched heptanoate claim 1 , a linear or branched octanoate claim 1 , a linear or branched nonanoate claim 1 , and a linear or branched decanoate.4. The compound of claim 1 , further comprising one or more saccharide groups attached from the 2 carbon position.5. The compound of claim 4 , wherein the one or more saccharide groups is selected from one or more of the following: a sialic acid claim 4 , a modified sialic acid claim 4 , a glucose claim 4 , a galactose claim 4 , a mannose claim 4 , a fucose claim 4 , an acetylgalactosamine claim 4 , an acetylglucosamine claim 4 , an acetylgalactosamine claim 4 , thiazoline an acetylglucosamine thiazoline claim 4 , an acetylneuraminic acid claim 4 , and a xylose.6. The compound of claim 4 , wherein the one or more saccharide groups is selected from one or more of the following: a sialic acid claim 4 , a modified sialic acid claim 4 , a β-D-Glucose claim 4 , a β-D-Galactose claim 4 , a β-D-Mannose claim 4 , an α-L-Fucose claim 4 , a N-Acetylgalactosamine claim 4 , a N-Acetylglucosamine claim 4 , a N-Acetylgalactosamine thiazoline claim 4 , a N-Acetylglucosamine thiazoline claim 4 , a N-Acetylneuraminic acid claim 4 , and a Xylose.7. The compound of claim 3 , wherein the compound is further covalently bound to a protein or a glycolipid.8. The compound of claim 7 , wherein the glycoprotein is mucin-linked or is ...

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Номер записи: 71
25-08-2022 дата публикации

Methods for Glycosylation

Номер: US20220267362A1
Автор: Girish Chandra Sati, John Montgomery, Joshua Lane Martin
Принадлежит: University of Michigan

Provided herein are methods of glycosylation in the formation of disaccharides, trisaccharides, and oligosaccharides using fluoroglycosides, silyl ether glycosides and a triaryl borane catalyst.

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Номер записи: 72
25-04-2019 дата публикации

SEPARATION OF OLIGOSACCHARIDES FROM FERMENTATION BROTH

Номер: US20190119314A1
Автор: Banke Niels, CHASSAGNE Pierre, JONDELIUS HEDEROS Markus, KHANZHIN Nikolay, Matwiejuk Martin
Принадлежит:

The invention relates to a method for obtaining an N-acetylglucosamine containing neutral oligosaccharide from a fermentation broth, wherein said oligosaccharide is produced by culturing a genetically modified microorganism capable of producing said oligosaccharide from an internalized carbohydrate precursor, comprising the steps of: i) ultrafiltration (UF), preferably to separate biomass from the broth, ii) nanofiltration (NF), preferably to concentrate said oligosaccharide in the broth and/or reduce an inorganic salt content of the broth, and iii) treating the broth with an ion exchange resin, preferably to remove charged materials, and/or subjecting the broth to chromatography, preferably to remove hydrophobic impurities. 1. A method for separating an N-acetylglucosamine containing neutral oligosaccharide from dissolved inorganic and organic salts , acids and bases in an aqueous medium from a fermentation or enzymatic process , comprising the step of treating said aqueous medium with a strong cation exchange resin in H-form and a weak anion exchange resin in free base form.2. The method according to claim 1 , wherein the treatment with a strong cation exchange resin in H-form is directly followed by a treatment with a weak anion exchange resin in free base form.3. The method according to which does not comprise electrodialysis.4. The method according to claim 1 , which further comprises ultrafiltration and nanofiltration claim 1 , wherein the treatment with a strong cation exchange resin in H-form and a weak anion exchange resin in free base form is preceded by ultrafiltration followed by nanofiltration.5. (canceled)6. A method for separating an N-acetylglucosamine containing neutral oligosaccharide from a fermentation broth obtained by culturing a genetically modified microorganism capable of producing said N-acetylglucosamine containing neutral oligosaccharide from an internalized carbohydrate precursor claim 1 , wherein the separation comprises the steps of:i) ...

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Номер записи: 73
10-05-2018 дата публикации

OIL-BASED INK COMPOSITION FOR WRITING INSTRUMENTS, AND WRITING INSTRUMENT, MARKING PEN AND BALLPOINT PEN COMPRISING THE SAME

Номер: US20180127609A1
Автор: NAKAMURA Hisashi
Принадлежит: KABUSHIKI KAISHA PILOT CORPORATION

An oil-based ink composition for a writing instrument, comprising a dye, an organic solvent and a phenolic compound of the following general formula (1): 2. The ink composition according to claim 1 , wherein the content of the phenolic compound is 0.5 to 10% by mass based on the total mass of the ink composition.3. The ink composition according to claim 1 , wherein the dye is a solvent dye.4. The ink composition according to claim 1 , wherein a vapor pressure of the organic solvent at 20° C. is 10 to 50 mmHg.5. The ink composition according to claim 1 , wherein a boiling point of the organic solvent is 160 to 250° C.6. The ink composition according to claim 1 , further comprising a resin.7. The ink composition according to claim 6 , wherein the resin is a ketone resin.8. The ink composition according to claim 1 , further comprising a sucrose fatty acid ester.9. A writing instrument claim 1 , comprising the oil-based ink composition for a writing instrument according to .10. The writing instrument according to claim 9 , selected from the group consisting of marking pens and ballpoint pens. The present invention relates to an oil-based ink composition for a writing instrument, and a writing instrument, a marking pen and a ballpoint pen comprising the oil-based ink composition. More particularly, the present invention relates to an oil-based ink composition for a writing instrument which can form handwriting having excellent water resistance, and a writing instrument, a marking pen and a ballpoint pen comprising the oil-based ink composition.A dye is conventionally contained as a coloring agent into an oil-based ink composition because of excellent color development, but an oil-based ink composition including a dye is prone to lower water resistance so that bleeding of handwriting in which the ink composition bleeds from handwriting to spread to the circumference occurs by adhesion of water. Taking this problem into consideration, though a metallized dye is included ...

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Номер записи: 74
23-04-2020 дата публикации

MODIFIED LIPOPOLYSACCHARIDE GLYCOFORM AND METHOD OF USE

Номер: US20200121786A1
Автор: ANDRES Dorothee, Grabowicz Marcin, Kahne Daniel, Lebar Matthew, Silhavy Thomas J.
Принадлежит:

The present disclosure generally relates to genetic engineering of bacteria. More particularly, the present disclosure describes genetic engineering of to create mutant O-antigen ligase, as well as novel lipopolysaccharide molecules resulting from that genetic engineering. Methods for using those novel molecules are also described. 1. A vaccine adjuvant comprising at least one of a lipopolysaccharide isolated from a mutant O-antigen ligase or lipopolysaccharide derivative isolated from the mutant O-antigen ligase , the mutant O-antigen ligase comprising either an isolated protein that has the amino acid sequence SEQ ID NO: 1 , or an isolated protein having at least 90% sequence identity to SEQ ID NO: 2 and having an amino acid substitution of phenylalanine to serine at the phenylalanine homologous to position 332 of SEQ ID NO: 2 ,wherein the isolated protein has at least one of O-antigen ligase activity or the activity to ligate lipid A to disaccharide pentapeptide (DPP).2. A vaccine adjuvant comprising a lipopolysaccharide derivative molecule prepared by the process comprising the steps of:{'i': 'E. coli', 'providing an strain adapted to express a LPS derivative molecule having reduced endotoxicity compared to a LPS molecule that the LPS derivative molecule is derived from;'}{'i': 'E. coli', 'claim-text': a mutant O-antigen ligase comprising an isolated protein that has the amino acid sequence SEQ ID NO: 1, and', 'a mutant O-antigen ligase comprising an isolated protein having at least 90% sequence identity to SEQ ID NO: 2 and having an amino acid substitution of phenylalanine to serine at the phenylalanine homologous to position 332 of SEQ ID NO: 2, wherein the protein has at least one of O-antigen ligase activity or the activity to ligate lipid A to disaccharide pentapeptide (DPP); and, 'modifying the strain by creating a mutant O-antigen ligase selected from the group consisting of{'i': 'E. coli', 'allowing the modified strain to grow under conditions to produce ...

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Номер записи: 75
03-06-2021 дата публикации

MONOESTER SUGAR DERIVATIVES AS FLAVOR MODIFIERS

Номер: US20210161189A1
Автор: CAYEUX Isabelle, DELATTRE Maxime, DI PIETRO Angela, Erni Philipp, Frerot Eric, GAILLARD Maude, LARCINESE-HAFNER Valeria
Принадлежит: FIRMENICH SA

Compositions containing monoester derivatives of the primary alcohol residue of a sugar are generally disclosed herein, as well as their use as sweetness enhancers, bitterness maskers, sourness maskers, or astringency reducers, to improve the taste profile of a flavored article. 1. A flavored article comprising a flavor-enhancing compound , wherein the flavor-enhancing compound is a monoester derivative of a primary alcohol residue of a sugar compound , which comprises a sugar moiety and an acid moiety.2. The flavored article of claim 1 , wherein the sugar moiety of the flavor-enhancing compound is a monosaccharide moiety.3. The flavored article of claim 2 , wherein the sugar moiety of the flavor-enhancing compound is a hexose moiety.4. The flavored article of claim 3 , wherein the sugar moiety of the flavor-enhancing compound is an allose moiety claim 3 , an altrose moiety claim 3 , a glucose moiety claim 3 , a mannose moiety claim 3 , a gulose moiety claim 3 , an idose moiety claim 3 , a galactose moiety claim 3 , a talose moiety claim 3 , a psicose moiety claim 3 , a fructose moiety claim 3 , a sorbose moiety claim 3 , or a tagatose moiety.5. The flavored article of claim 4 , wherein the sugar moiety of the flavor-enhancing compound is a glucose moiety.6. The flavored article of any one of to claim 4 , wherein the acid moiety of the flavor-enhancing compound is a Cfatty acid moiety.7. The flavored article of claim 6 , wherein the acid moiety of the flavor-enhancing compound is a hexanoate moiety claim 6 , an octanoate moiety claim 6 , a decanoate moiety claim 6 , a 9-decenoate moiety claim 6 , a 10-undecenoate moiety claim 6 , a dodecanoate moiety claim 6 , a 9-dodecenoate moiety claim 6 , a tetradecanoate moiety claim 6 , a hexadecanoate moiety claim 6 , an octadecanoate moiety claim 6 , an oleate moiety claim 6 , a linoleate moiety claim 6 , a linolenate moiety claim 6 , an eicosapentaenoate moiet claim 6 , or a docosahexaenoate moiety.8. The flavored article ...

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Номер записи: 76
31-07-2014 дата публикации

VERSATILE NATIVE CHEMICAL LIGATION TECHNOLOGIES

Номер: US20140213758A1
Автор: Garner Philip
Принадлежит: WASHINGTON STATE UNIVERSITY

Novel methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) or glycosylamine under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product containing an aziridinyl ring. Optional subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product. Coupling of a peptide thioacid and glycosylamine yields a glycosylated peptide. 1. A method of forming a glycosylated ligation product , comprisingreacting a thioacid with a compound that comprises a glycosylamine under conditions suitable for forming said ligation product.2. The method of claim 1 , wherein said conditions suitable for forming said ligation product are such that an amide bond is formed by displacement of SH of the thioacid by N of the glycosylamine claim 1 , thereby forming said ligation product.3. The method of claim 1 , wherein said thioacid is a peptide thioacid.4. The method of claim 3 , wherein said peptide thioacid does not contain a protecting group.5. The method of claim 1 , wherein said compound that comprises a glycosylamine is selected from the group consisting of a monosaccharide claim 1 , a disaccharide claim 1 , an oligosaccharide claim 1 , a polysaccharide or a modified saccharide.6. The method of claim 1 , wherein said step of reacting is performed in the presence of Cu(II) ion.7. The method of claim 1 , wherein said step of reacting is carried out at ambient temperature. This application is a continuation-in-part of U.S. patent application Ser. No. 13/657,524 filed on Nov. 13. 2012 and claims benefit of U.S. provisional patent application 61/786,146, filed Mar. 14, 2013, the complete contents of both of which is hereby incorporated by reference.This ...

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Номер записи: 77
02-05-2019 дата публикации

Sialic acid analogs

Номер: US20190127409A1
Автор: Emil Kakkis, He Zhao, Steven Jungles
Принадлежит: Ultragenyx Pharmaceutical Inc

The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.

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Номер записи: 78
19-05-2016 дата публикации

Disaccharide Synthetic Lipid Compounds and Uses Thereof

Номер: US20160136271A1
Автор: Burgess Stephen W., Hickman David T., LI Shengrong, Lopez-Deber Maria Pilar, Shaw Walter A.
Принадлежит:

Essentially pure compounds of the formulas (I) to (XX) are provided. Compositions and methods for enhancing or stimulating an immune response are also provided. The compounds, provided are advantageous in that the compounds are essentially pure and free from contaminants encountered when such compounds are purified from natural sources. 2. The essentially pure compound of claim 1 , wherein AA claim 1 , and Aare each independently Cto Cunsubstituted alkyl.3. The essentially pure compound of claim 1 , wherein Aand Aare each independently are Cto Cunsubstituted alkyl.4. The essentially pure compound of claim 1 , wherein AA claim 1 , and Aare each independently Cto Cunsubstituted alkyl and Aand Aare each independently are Cto Cunsubstituted alkyl.5. The essentially pure compound of claim 1 , wherein AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each Cor AA claim 1 , and Aare each Cand Aand Aare each C.6. The essentially pure compound of claim 1 , wherein AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each C; AA claim 1 , and Aare each Cand Aand Aare each Cor AA claim 1 , and Aare each Cand Aand Aare each C.7. The essentially pure compound of claim 1 , wherein the compounds is at least 95% pure with respect to the synthetic disaccharide lipid compounds as measured on a weight basis.9. The pharmaceutical composition of claim 8 , wherein AA claim 8 , and Aare each independently Cto Cunsubstituted alkyl.10. The pharmaceutical composition of claim 8 , wherein Aand Aare each independently are Cto Cunsubstituted alkyl.11. The pharmaceutical composition of claim 8 , wherein AA claim 8 , and ...

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Номер записи: 79
07-08-2014 дата публикации

HYBRID SCFA-HYDROXYL-DERIVATIZED MONOSACCHARIDES, METHODS OF SYNTHESIS, AND METHODS OF TREATING DISORDERS

Номер: US20140220630A1
Автор: Aich Udayanath, Campbell Christopher T., Choi Sean S., Meledeo Michael A., Sampathkumar Srinivasa-Gopalan, Weier Christopher, Yarema Kevin J.
Принадлежит: THE JOHNS HOPKINS UNIVERSITY

Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof. 3. The compound of claim 2 , wherein each of R claim 2 , Rand Ris independently C(O)(CH)CHwherein each n is independently an integer from 0-18.4. The compound of claim 2 , wherein each of R claim 2 , Rand Ris C(O)(CH)CH.5. The compound of claim 2 , wherein R is alkyl or a substituted alkyl which may be substituted by oxo claim 2 , azido claim 2 , aryl claim 2 , halogen claim 2 , —OC(O)alkyl claim 2 , or —SC(O)alkyl.625-. (canceled)2730-. (canceled)3246-. (canceled)47. The compound of claim 1 , which comprises mix-match substitution.48. The compound of claim 1 , wherein the compound is utilized in metabolic labeling of glycoproteins or glycolipids.49. The compound of claim 1 , wherein the compound is utilized in stem cell differentiation.50. A method for increasing production of a recombinant glycoprotein in a cell claim 1 , the method comprising the step of contacting said cell with a compound of in an amount sufficient to increase recombinant glycoprotein biosynthesis in said cell claim 1 , thereby increasing production of a recombinant glycoprotein in said cell.5162-. (canceled)63. A method of incorporating a compound of in a glycan cell surface or in a glycosylation pathway claim 1 , wherein toxicity is reduced as compared to an appropriate control.64. A method of incorporating a compound of in a glycan cell surface or in a glycosylation pathway claim 1 , wherein toxicity is absent.6576-. (canceled) This application claims benefit of U.S. Application Ser. No. 60/963,966, filed Aug. 8, 2007, which is incorporated by reference in its entirety.Research supporting this application was carried out in part under funding from the NIH/NCI (5R01CA12314-03). The government of the United States may have rights in the inventions.Uncontrolled cell proliferation ...

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Номер записи: 80
07-08-2014 дата публикации

LOW TEMPERATURE CHLORINATION OF CARBOHYDRATES

Номер: US20140221642A1
Автор: Erickson William Randal, Fields Stephen Craig
Принадлежит: LEXINGTON PHARMACEUTICALS LABORATORIES, LLC

Disclosed is a method of chlorinating a carbohydrate or derivative thereof, for example, a sucrose-6-ester at the 4,1′, and 6′ positions, with irreversible removal of HCl formed during the reaction to form the chlorinated carbohydrate or derivative thereof, for example, a 4,1′,6′-trichloro-4,1′,6′-trideoxy-6-O-ester of galactosucrose (TGS-6E). The irreversible removal of HCl can be carried out by an irreversible physical process and/or an irreversible chemical process. Sucralose, an artificial sweetener, can be prepared by deesterification of the TGS-6E. The chlorination reaction takes place at low temperatures and the desired chlorinated product is obtained in high yields and in high purities. 1. A method for chlorinating a carbohydrate or a derivative thereof comprising reacting the carbohydrate or derivative thereof with a chlorinating agent and irreversibly removing during chlorination the hydrogen chloride produced by the reaction of the chlorinating agent with the carbohydrate or derivative thereof.2. The method of claim 1 , wherein the carbohydrate or derivative thereof is a sugar or derivative thereof.3. The method of claim 2 , wherein the sugar derivative is a sugar ester.4. The method of claim 3 , wherein the sugar ester is a sucrose-6-ester.5. The method of claim 4 , wherein the chlorinated product obtained is 4 claim 4 ,1′ claim 4 ,6′-trichloro-4 claim 4 ,1′ claim 4 ,6′-trideoxy-6-O-ester of galactosucrose (TGS-6E).6. The method of claim 1 , wherein the chlorinating agent is an acid chloride or bis(trichloromethyl)carbonate.7. The method of claim 1 , wherein the chlorinating agent is a Vilsmeier Reagent having the formula: [XYC=NR]Cl claim 1 , wherein X is hydrogen claim 1 , aryl claim 1 , or alkyl claim 1 , wherein the aryl or alkyl is optionally substituted with a halogen claim 1 , alkoxy claim 1 , thioalkoxy claim 1 , amido claim 1 , or cyano; Y is a leaving group; and R is hydrogen or alkyl which is optionally substituted with halogen claim 1 , ...

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Номер записи: 81
30-04-2020 дата публикации

SIALIC ACID ANALOGS

Номер: US20200131215A1
Автор: JUNGLES Steven, Kakkis Emil, Zhao He
Принадлежит:

The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies. 177-. (canceled)92. A sustained release pharmaceutical composition comprising a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 , wherein:a) the release of the compound is over a period of about four hours or more; and/orb) the pharmacological effect from the compound lasts about four hours or more upon administration of the composition.93. A sustained release pharmaceutical composition comprising a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 ,wherein the composition, upon administration, provides a therapeutically effective amount of the compound for about 4 hours or more.94. A method for treating a sialic acid deficiency in a patient in need thereof comprising administering an effective amount of a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof.95. A method for treating a sialic acid deficiency in a patient in need thereof comprising administering a compound of claim 78 , or a pharmaceutically acceptable salt or solvate thereof; wherein upon administration claim 78 , the compound claim 78 , or a pharmaceutically acceptable salt or solvate thereof claim 78 , continuously provides a therapeutically effective amount of sialic acid for about 4 hours to about 24 hours.96. The method of claim 94 , wherein the sialic acid deficiency is myopathy associated with sialic acid deficiency.97. The method of claim 96 , wherein the myopathy associated with sialic acid deficiency is Hereditary Inclusion Body Myopathy (HIBM) claim 96 , Nonaka myopathy claim 96 , or Distal Myopathy with Rimmed Vacuoles (DMRV). This application is a continuation of U.S. patent application Ser. No. 16/050,343, filed on Jul. 31, 2018, which is a continuation of U.S. patent application Ser. No. 14/944,779, filed on Nov. 18, 2015, now U.S. Pat. No. 10,065,981, ...

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Номер записи: 82
04-06-2015 дата публикации

POLYMER MONOLITHS FOR SOLVENT EXCHANGE IN CONTINUOUS FLOW MICROFLUIDIC DEVICE

Номер: US20150152206A1
Автор: Ismail Rehana, Keng Pei Yuin, Machness Ariella, Park Kyoung-Joo Jenny
Принадлежит:

The present disclosure relates to the novel multistep procedure for preparation of polymer monoliths for use in solvent exchange, such as methods to exchange and activate fluoride ions on a flow through microfluidic chip for subsequent chemical synthesis. Methods according to the present disclosure include the application of such microfluidic platforms for rapid F18 radiosynthesis on a flow through microfluidic chip with high efficiency, followed by a subsequent nucleophilic fluorination reaction. Various other methods of exchanging and activating fluoride ions on a flow through microfluidic chip are also disclosed. Methods incorporating features of the present invention can be applicable to any flow through microfluidic device in any field, such as radiosyntheses, chemical syntheses, concentration of ions for environmental analyses and sample preparation such as concentrating minute amounts of analyte to improve the downstream detection. 1. A method of exchanging and activating fluoride ions on a flow through microfluidic chip , comprising the steps of:providing a microfluidic chip with one or more channels on or in the chip;vinylizing the microfluidic chip;forming and covalently anchoring polymer monoliths in the one or more channels;{'sup': '18', 'flowing [F] Fluoride ion water through the monoliths in the one or more channels; and'}{'sup': '18', 'eluting the []F fluoride ion via treatment with cryptands and potassium carbonate or potassium bicarbonate, or tetraalkylammonium bicarbonate.'}2. The method of claim 1 , wherein the microfluidic chip comprises glass.3. The method of claim 1 , wherein the one or more channels are serpentine channels formed in the chip.4. The method of claim 3 , wherein the polymer monoliths are within the one or more channels and the volume of the polymer monoliths is at least 13 μL.5. The method of claim 4 , wherein the serpentine channels have a cross section of about 150 μm×150 μm and a length of about 52000 μm.6. The method of claim ...

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Номер записи: 83
02-06-2016 дата публикации

HYBRID SCFA-HYDROXYL-DERIVATIZED MONOSACCHARIDES, METHODS OF SYNTHESIS, AND METHODS OF TREATING DISORDERS

Номер: US20160151400A1
Автор: Aich Udayanath, Campbell Christopher T., Choi Sean S., Meledeo Michael A., Sampathkumar Srinivasa-Gopalan, Weier Christopher, Yarema Kevin J.
Принадлежит:

Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof. 325-. (canceled)2730-. (canceled)3238-. (canceled)42. (canceled)43. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.44. The composition of claim 43 , further comprising an additional therapeutic agent.45. The composition of claim 44 , wherein the additional therapeutic agent is an anticancer agent.4649-. (canceled)50. A method of treating or preventing a subject suffering from or susceptible to a disease or disorder claim 1 , the method comprising the step of administering to the subject a therapeutic amount of a compound of sufficient to treat the disease or disorder or symptoms thereof under conditions such that the disease or disorder is treated.51. A method of treating or preventing a subject suffering from or susceptible to a disease or disorder claim 1 , the method comprising the steps of: (i) identifying the patient as in need of administration of a MUCI claim 1 , MMP9 claim 1 , CXCR4 claim 1 , or NF-κB inhibitor compound; and (ii) administering to the subject a therapeutic amount of a compound of sufficient to treat or prevent the disease or disorder or symptoms thereof.52. The method of claim 51 , wherein the subject is a human.5357-. (canceled)58. A method of sensitizing a cancer cell in a subject to anticancer agents claim 1 , the method comprising the steps of identifying a subject as in need thereof and administering to the subject a therapeutic amount of a compound of sufficient to sensitizing a cancer cell in a subject to anticancer agents.59. A method of treating or preventing cancer in a subject claim 1 , the method comprising the step of administering to the subject a therapeutic amount of a compound of .60. (canceled)61. A method of treating or preventing cancer in a subject claim 1 , with ...

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Номер записи: 84
02-06-2016 дата публикации

BETA-GLYCOLIPIDS FOR USE AS ADJUVANTS

Номер: US20160151483A1
Автор: CUTIGNANO Adele, DE PALMA Raffaele, FONTANA Angelo, MANZO Emiliano
Принадлежит:

The present invention relates to beta-glycolipid derivatives, their preparation and use as adjuvants in vaccines, as being suitable for being co-administered with antigens for vaccine prophylaxis and therapy. In certain embodiments, the beta-glycol-lipid derivatives of the invention also in their salified or complex form, are suitable for being co-administered with antigens for both therapeutic and prophylactic purposes or for vaccine prophylaxis and therapy. 2. The vaccine adjuvant of claim 1 , wherein claim 1 , in the beta-glycolipid derivative claim 1 , Aand Aor Rand Rare claim 1 , independently of each other claim 1 , saturated or monounsaturated linear C-Calkyl.3. The vaccine adjuvant of claim 2 , wherein claim 2 , in the beta-glycolipid derivative claim 2 , Aand Aor Rand Rare claim 2 , independently of each other claim 2 , moieties of lauric acid claim 2 , myristic acid claim 2 , palmitic acid claim 2 , stearic acid claim 2 , arachidic acid claim 2 , behenic acid or lignoceric acid.4. The vaccine adjuvant of claim 2 , wherein claim 2 , in the beta-glycolipid derivative claim 2 , Aand Aor Rand Rare claim 2 , independently of each other claim 2 , saturated or monounsaturated linear C-Calkyl.5. The vaccine adjuvant of claim 1 , wherein claim 1 , in the beta-glycolipid derivative claim 1 , Aand Aare acyl —(CO)Rand acyl —(CO)Rrespectively claim 1 , where Rand Rare claim 1 , independently of each other claim 1 , a moiety of pentadecanoic acid claim 1 , palmitic acid claim 1 , heptadecanoic acid claim 1 , or stearic acid.6. The vaccine adjuvant of claim 1 , wherein the beta-glycolipid derivative of formula (I) is in the form of a salt thereof claim 1 , wherein X is a —SO claim 1 , —OSO claim 1 , —OPO claim 1 , —PO claim 1 , alkali or alkaline-earth metal group.7. The vaccine adjuvant of claim 1 , wherein claim 1 , in the beta-glycolipid derivative claim 1 , X is —SOH claim 1 , —SONa claim 1 , or —SOK.8. The vaccine adjuvant of claim 1 , wherein the beta-glycolipid ...

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Номер записи: 85
15-09-2022 дата публикации

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

Номер: US20220289783A1
Автор: Brimert Thomas, JOHNSSON Richard, Leffler Hakon, Nilsson Ulf, ZETTERBERG Fredrik
Принадлежит: GALECTO BIOTECH AB

An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. 2. The method of wherein said disorder is selected from the group consisting of pulmonary fibrosis claim 1 , liver fibrosis claim 1 , kidney fibrosis claim 1 , cancers claim 1 , autoimmune diseases claim 1 , metabolic disorders claim 1 , heart disease claim 1 , heart failure claim 1 , liver disorders claim 1 , and non-alcoholic steatohepatitis.3. The method of wherein said disorder is selected from the group consisting of carcinomas claim 1 , sarcomas claim 1 , leukemias claim 1 , lymphomas claim 1 , T-cell lymphomas claim 1 , and metastasising cancers.4. The method of wherein said disorder is selected from the group consisting of interstitial lung fibrosis claim 1 , liver cirrhosis claim 1 , autoimmune cirrhosis claim 1 , primary biliary cirrhosis claim 1 , hepatic impairment claim 1 , moderate hepatic impairment claim 1 , cardiovascular disorders claim 1 , cardiac fibrosis claim 1 , cardiac failure claim 1 , aortic stenosis claim 1 , and aortic stiffness.5. The method of wherein the mammal is a human.6. The method of wherein the compound of formula I is in amorphous form.7. The method of wherein the compound of formula I is administered in a pharmaceutical composition selected from tablets or capsules. This application is a continuation of U.S. patent application Ser. No. 17/018,713, filed Sep. 11, 2020, which is a continuation of U.S. patent application Ser. No. 15/535,829, filed Jun. 14, 2017, which is a national phase of International Patent Application No. PCT/EP2016/051836, filed Jan. 28, 2016, which ...

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Номер записи: 86
31-05-2018 дата публикации

USE OF UAP INHIBITORS TO INHIBIT FLUX THROUGH THE HEXOSAMINE BIOSYNTHETIC PATHWAY

Номер: US20180148468A1
Автор: Quinones-Hinojosa Alfredo, Saeui Christopher T., Shah Sagar Ramesh, Yarema Kevin J.
Принадлежит:

Disclosed are UAP inhibitors to inhibit glucose flux in the hexosamine biosynthetic pathway and methods of treating a disease using the inhibitors. 48-. (canceled)10. (canceled)1321-. (canceled)22. A method of treating a disease comprising administering to a subject an effective amount of the pharmaceutical composition of .23. The method of :wherein the compound is a UAP inhibitor;wherein the subject is an animal or human; and/orwherein the disease is selected from cancer, diabetes, neurodegenerative disease, metabolic disorder, cardiovascular disease, ageing, autoimmunity, metabolic syndrome, eye disease and kidney disease, optionally:wherein the cancer is squamous-cell carcinoma, basal cell carcinoma, adenocarcinoma, hepatocellular carcinomas, and renal cell carcinomas, cancer of the bladder, bowel, breast, cervix, colon, esophagus, head, kidney, liver, lung, neck, ovary, pancreas, prostate, and stomach; leukemias; benign and malignant lymphomas, particularly Burkitt's lymphoma and Non-Hodgkin's lymphoma; benign and malignant melanomas; myeloproliferative diseases; sarcomas, including Ewing's sarcoma, hemangiosarcoma, Kaposi's sarcoma, liposarcoma, myosarcomas, peripheral neuroepithelioma, synovial sarcoma, gliomas, astrocytomas, oligodendrogliomas, ependymomas, gliobastomas, neuroblastomas, ganglioneuromas, gangliogliomas, medulloblastomas, pineal cell tumors, meningiomas, meningeal sarcomas, neurofibromas, and Schwannomas; bowel cancer, breast cancer, prostate cancer, cervical cancer, uterine cancer, lung cancer, ovarian cancer, testicular cancer, thyroid cancer, astrocytoma, esophageal cancer, pancreatic cancer, stomach cancer, liver cancer, colon cancer, melanoma; carcinosarcoma, Hodgkin's disease, Wilms' tumor or teratocarcinomas, optionally wherein the disease is pancreatic cancer or liver cancer,wherein the disease is a metabolic disorder, optionally diabetes or obesity, and/orwherein the disease is a neurological disorder, optionally Alzheimer's disease. ...

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Номер записи: 87
21-08-2014 дата публикации

METHOD FOR MAKING A PRECURSOR OF L-FUCOSE FROM D-GLUCOSE

Номер: US20140235848A1
Автор: BONACCORSI Filippo, Boutet Julien, Dekany Gyula, KHANZHIN Nikolay
Принадлежит: GLYCOM A/S

A method that can be used to make a precursor of L-fucose from D-glucose that includes the steps of a) making a compound of formula (1) from D-glucose, formula (1) wherein Ris acyloxy, and Q is a group (a), (b), (c) or (d), formula (a), (b), (c) or (d) or wherein Ris OH, and Q is a group (e), (f) or (g); formula (e), (f) or (g) wherein Ris acyloxy and Ris a sulphonyl leaving group; and b) producing 6-deoxy-L-talose from the compound of formula (1) formed in step a), wherein the moiety is a highly lipophilic protecting group; compounds according to formula (1), and use of a compound according to formula (1) are provided. 13. A method according to claim 1 , wherein Ris mesylate claim 1 , tosylate claim 1 , triflate claim 1 , nosylate claim 1 , brosylate or tresylate claim 1 , and Ris acetoxy or benzoyloxy.14. A compound according to formula 1 of .17. A compound according to claim 14 , wherein Ris mesylate claim 14 , besylate claim 14 , tosylate claim 14 , triflate claim 14 , nosylate claim 14 , brosylate or tresylate claim 14 , and Ris acetoxy or benzoyloxy.18. A compound according to that is isolated in crystalline form.19. (canceled)21. A method according to claim 12 , wherein the two geminal R groups together with the carbon atom to which they are attached form a cyclohexylidene.22. A method according to claim 13 , wherein Ris mesylate or tosylate.23. A compound according to formula 1A of .24. A compound according to formula 1B of .25. A compound according to formula 1C of .26. A compound according to formula 1D of .27. A compound according to formula 1E of .28. A compound according to formula 1F of .29. A compound according to formula 1G of .30. A compound according to claim 16 , wherein the two geminal R groups together with the carbon atom to which they are attached form a cyclohexylidene.31. A compound according to claim 17 , wherein Ris mesylate or tosylate. -Monosaccharides or -sugars, especially -hexoses, are scarce in nature. Nevertheless, some -hexoses are ...

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Номер записи: 88
07-06-2018 дата публикации

METHODS AND COMPOSITIONS FOR MAKING ANTIBODIES AND ANTIBODY DERIVATIVES WITH REDUCED CORE FUCOSYLATION

Номер: US20180155677A1
Автор: ALLEY STEPHEN C., Benjamin Dennis R., Burke Patrick J., Jeffrey Scott C., Sussman Django, Toki Brian
Принадлежит:

The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation. 154-. (canceled)56. The fucose analog of claim 55 , wherein each of R-Ris independently selected from the group consisting of —OH and —OC(O)C-Calkyl.57. The fucose analog of claim 55 , wherein each of R-Ris independently selected from the group consisting of —OH and —OAc.58. The fucose analog of claim 55 , wherein Ris selected from the group consisting of —C≡CH and —C≡CCH.59. The fucose analog of claim 55 , wherein Ris —C(O)OCH.60. The fucose analog of claim 55 , wherein Ris selected from the group consisting of —CN and —CHCN.61. The fucose analog of claim 55 , wherein Ris —CHCN.62. The fucose analog of claim 55 , wherein Ris —CHBr claim 55 , —CHCl claim 55 , or —CHI.63. The fucose analog of claim 55 , wherein Ris —CHBr or —CHI.64. The fucose analog of claim 55 , wherein Ris —CHBr.65. The fucose analog of claim 55 , wherein Ris methoxiran.66. The fucose analog of claim 55 , wherein Ris —CH(OAc)CH.6772-. (canceled)74. A compound of claim 73 , wherein Ris F.75. A compound of claim 73 , wherein Ris F.76. A compound of claim 73 , wherein Ris F.77. A compound of claim 73 , wherein Ris F and Ris F.78. A compound of claim 73 , wherein each of Rand Ris F.79. A compound of claim 73 , wherein R claim 73 , Rand Rare each independently selected from the group consisting of —OH and —OAc; Ris F; and Ris —CH.80. A compound of claim 73 , wherein R claim 73 , Rand Rare each independently selected from the group consisting of —OH and —OAc; Ris F; Rand Rare each H; and Ris —CH.8194-. (canceled)95. (canceled) This application is a continuation of U.S. patent application Ser. No. 14/632,925 filed Feb. 26, 2015, which is a continuation of U.S. patent application Ser. No. 14/043,742 filed Oct. 1, 2013 (now U.S. Pat. No. 8,993,326), which is a divisional of Ser. No. 13/405,143 filed Feb. 24, 2012 (now U.S. Pat. No. 8,574,907), which is a divisional of Ser. No. ...

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Номер записи: 89
28-08-2014 дата публикации

Methods for the Production of 3-O-Deactivated-4'-Monophosphoryl Lipid A (3D-MLA)

Номер: US20140243513A1
Автор: MYERS Kent R., SNYDER D. Scott
Принадлежит: GLAXOSMITHKLINE BIOLOGICALS S.A.

Herein is disclosed a method for producing lipopolysaccharide (LPS), comprising: (a) growing a culture of a deep rough mutant bacterial strain in a medium; (b) maintaining the culture in stationary phase for at least about 5 hr; (c) harvesting, cells from the culture; and (d) extracting LPS from the cells. The method allows for the production of an LPS which can be used to produce a 3-O-deacylated monophosphoryl lipid A (3D-MLA) having at least about 20 mol % of the hexaacyl congener group. 1. A method of extracting lipopolysaccharide (LPS) from a culture of deep rough mutant bacterial strain cells , comprising:a. Extracting the cells with a solution consisting essentially of at least 75 wt % of an aliphatic alcohol having from 1 to 4 carbon atoms and the balance water, thereby producing cells with reduced phospholipid content;b. Extracting the cells with reduced phospholipid content with a solution comprising chloroform and methanol, thereby yielding a solution of LPS in chloroform and methanol,wherein the extracting with aliphatic alcohol is performed at a temperature between 35° C. and 65° C.2SalmonellaEscherichia.. The method of claim 1 , wherein the deep rough mutant bacterial strain is of the genera or3SalmonellaSalmonella minnesota.. The method of claim 2 , wherein the deep rough mutant bacterial strain of genus is of species4Salmonella minnesotaSalmonella minnesota. The method of claim 3 , wherein the deep rough mutant bacterial strain of species is strain R595.5EscherichiaEschenchia coli.. The method of claim 2 , wherein the deep rough mutant bacterial strain of genus is of species6Escherichia coilEscherichia coil. The method of claim 5 , wherein the deep rough mutant bacterial strain of species is of strain D31m4.7. The method of claim 1 , wherein the aliphatic alcohol has from 2 to 4 carbon atoms.8. The method of claim 7 , wherein the aliphatic alcohol is ethanol.9. The method of claim 1 , wherein the solution comprising aliphatic alcohol comprises ...

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Номер записи: 90
04-09-2014 дата публикации

TREHALOSE COMPOUND, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL PRODUCT CONTAINING THE COMPOUND

Номер: US20140248317A1
Автор: Imagawa Hiroshi, Nishizawa Mugio, Oda Masataka, SAKURAI Jun, YAMAMOTO Hirofumi
Принадлежит: GLYTECH, INC.

A trehalose compound having high immunopotentiating activity and low toxicity is represented by formula (1). (In the formula, X and X′ each represents a phenyl, a naphthyl, R—CHR— (wherein Rand Reach represents a C-Calkyl group or the like) or the like; and n and n′ each independently represents an integer of 0-3). The compound exhibits a high activating effect on macrophages and neutrophils. 2. The method according to claim 1 , wherein X represents R—CHR— and X′ represents R—CHR′—.3. The method according to claim 2 , wherein R claim 2 , R′ claim 2 , Rand R′ independently represent a linear C-Calkyl group claim 2 , and n and n′ independently represent 0 or 1.4. The method according to claim 2 , wherein R claim 2 , R′ claim 2 , Rand R′ independently represent a linear C-Calkyl group claim 2 , and n and n′ independently represent 0.5. The method according to claim 2 , wherein R claim 2 , R′ claim 2 , Rand R′ independently represent a linear C-Calkyl group claim 2 , and n and n′ independently represent 1.6. The method according to claim 1 , wherein Ris identical to R′ claim 1 , Ris identical to R′ claim 1 , and n is identical to n′.7. The method according to claim 1 , wherein the compound is selected from the group consisting of:6,6′-bis-O-(2-octyldecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-nonylundecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-decyldodecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-undecyltridecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-dodecyltetradecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-tridecylpentadecanoyl)-α,α′-trehalose,6,6′-bis-O-(2-pentadecylheptadecanoyl)-α,α′-trehalose, and6,6′-bis-O-(2-hexadecyloctadecanoyl)-α,α′-trehalose.8. The method according to claim 1 , wherein the compound is selected from the group consisting of:6,6′-bis-O-(3-nonyldodecanoyl)-α,α′-trehalose,6,6′-bis-O-(3-decyltridecanoyl)-α,α′-trehalose,6,6′-bis-O-(3-undecyltetradecanoyl)-α,α′-trehalose,6,6′-bis-O-(3-dodecylpentadecanoyl)-α,α′-trehalose,6,6′-bis-O-(3-tridecylhexadecanoyl)-α,α′-trehalose, and6,6′- ...

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Номер записи: 91
14-06-2018 дата публикации

CHLORINATION OF SUCROSE-6-ESTERS

Номер: US20180162892A1
Автор: Aktas Halil, EILERS Thomas
Принадлежит: Tate & Lyle Technology Limited

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; (v) quenching said mixture to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane. 1. A method for the chlorination of a sucrose-6-acylate to produce a 4 ,1′ ,6′-trichloro-4 ,1′ ,6′-trideoxy-galactosucrose-6-acylate , wherein said method comprises the following steps (i) to (v):(i) providing a first component comprising sucrose-6-acylate;(ii) providing a second component comprising a chlorinating agent;(iii) combining said first component and said second component to afford a mixture;(iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof;(v) quenching said mixture to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate;wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; andwherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane.2. A method according to claim 1 , wherein both of said first ...

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Номер записи: 92
23-06-2016 дата публикации

REGIOSELECTIVE SILYL EXCHANGE OF PER-SILYLATED OLIGOSACCHARIDES

Номер: US20160176909A1
Автор: GERVAY-HAGUE Jacquelyn, SCHOMBS Matthew
Принадлежит: The Regents of the University of California

The present invention provides novel, regioselectively-acylated oligosaccharide compounds and methods for preparing them. In another aspect, the. invention provides a method for preparing a selectively-acylated oligosaccharide. The method includes forming a reaction mixture containing a protected oligosaccharide and an acylating agent. The protected oligosaccharide includes at least three hydroxyl moieties and each hydroxyl moiety is protected with a silyl protecting group. The reaction mixture is formed under conditions sufficient to selectively replace at least one silyl protecting group with a —C(0)-C1_6 alkyl group, and the selectively-acylated oligosaccharide comprises at least one —C(0)-C1_6 alkyl group and at least one silyl protecting group. 2. The compound according to claim 1 , wherein{'sup': 1', '2', '3', '4', '6', '7, 'R, R, R, R, and Rare each independently selected from the group consisting of —OR, the α-linked monosaccharide, and the β-linked monosaccharide;'}{'sup': 1a', '2a', '3a', '4a', '6a', '7, 'R, R, R, R, and Rare each independently selected from the group consisting of —ORand the linking moiety —O—;'}{'sup': '7', 'sub': 1-6', '3, 'each Ris independently selected from the group consisting of —C(O)—Calkyl and —Si(R); and'}{'sup': 1', '2', '3', '4', '6', '1a', '2a', '3a', '4a', '6a', '7', '7', '8, 'sub': '3', 'at least one of R, R, R, R, R, R, R, R, R, and Ris —OR, wherein Ris —Si(R).'}3. The compound according to claim 2 , wherein Ris selected from the group consisting of the α-linked monosaccharide and the β-linked monosaccharide.46-. (canceled)911-. (canceled)15. (canceled)1720-. (canceled)21. The method according to claim 14 , wherein the reaction mixture further comprises an acid selected from the group consisting of acetic acid claim 14 , formic acid claim 14 , and trichloroacetic acid.22. (canceled)23. The method according to claim 14 , wherein the reaction mixture further comprises at least one base selected from the group consisting of ...

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Номер записи: 93
06-06-2019 дата публикации

Fungal Trisaccharide Ester Compounds and Use Thereof in Preparing Agents for Preventing and Controlling Plant Fungal Diseases

Номер: US20190166835A1
Автор: Jinghua XUE, Liangxiong XU, Linyan Feng, Ping Wu, Xiaoyi Wei, Xuewu Duan
Принадлежит: South China Botanical Garden of CAS

Fungal trisaccharide ester compounds and agents containing the fungal trisaccharide ester compounds as active ingredients for preventing and controlling plant fungal diseases. A Pezicula sp. strain SC1337 was isolated from endophytes of a branch of bald cypress. The strain SC1337 is capable of producing five compounds exhibiting significant inhibitory activities against twelve common plant pathogenic fungi and preservative effect on fruits. Thus, the strain SC1337 can be used to prepare the five compounds exhibiting significant inhibitory activities against twelve common plant pathogenic fungi and preservative effect on fruits and used for preventing and controlling plant pathogenic fungi and fruit preservation.

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Номер записи: 94
22-06-2017 дата публикации

NOVEL MATERIALS DERIVED FROM FERMENTATION-PRODUCED RHAMNOLIPIDS AND METHODS OF PRODUCTION

Номер: US20170175151A1
Автор: Ju Lu-Kwang, Miao Shida
Принадлежит:

A method of preparing a product derived from a rhamnolipid includes the steps of: providing a rhamnolipid, combining the rhamnolipid with a reagent, allowing the rhamnolipid and reagent to react to form a product derived from the rhamnolipid, and collecting the product derived from the rhamnolipid. An exemplary product is dimeric β-hydroxy fatty acid. 2. The compound of claim 1 , where Cand Care each alkyl chains having seven carbon atoms.3. The compound of claim 2 , where Xand Xare each hydroxyl groups.4. A polymer formed from a plurality of the compounds of .6. The compound of claim 5 , where Cand Care each alkyl chains having seven carbon atoms.9. A polymer formed from a plurality of the compounds of .10. A polymer formed from a plurality of the compounds of .11. A method of preparing a product derived from a rhamnolipid comprising the steps of:providing a rhamnolipid,combining the rhamnolipid with a reagent,allowing the rhamnolipid and reagent to react to form a product derived from the rhamnolipid, andcollecting the product derived from the rhamnolipid.12. The method of claim 11 , wherein the reagent is an acid claim 11 , wherein the reaction mixture further comprises an alcohol claim 11 , wherein the rhamnolipid is a rhamnolipid mixture comprising both mono-rhamnolipids and di-rhamnolipids claim 11 , and wherein the product is dimeric β-hydroxy fatty acid.13. The method of claim 12 , wherein the rhamnolipid is a mono-rhamnolipid.14. The method of claim 12 , further comprising the steps of:adding a catalyst to the collected product, andheating the collected product after the adding step,whereby the steps of adding and heating polymerize the dimeric β-hydroxy fatty acid.15. The method of claim 11 , wherein the reagent is a base in solution with an alcohol claim 11 , wherein the rhamnolipid comprises two β-hydroxy fatty acids claim 11 , and wherein the product is a rhamnolipid comprising only one β-hydroxy fatty acid.16. The method of claim 11 , wherein the ...

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Номер записи: 95
28-06-2018 дата публикации

Synthetic Antigen Constructs Against Campylobacter Jejuni

Номер: US20180177857A1
Автор: Guerry Patricia, Jiao Yuening, Monteiro Mario Artur
Принадлежит: United States of America as represented by the Secretary of the Navy

The invention relates to immunogenic synthetic constructs capable of inducing an immune response against () in a subject comprising one or more monosaccharides comprising one or more MeOPN moieties. Specifically, the invention relates to immunogenic synthetic constructs capable of inducing an immune response against () in a subject comprising one or more MeOPN→6 Gal monosaccharides. The invention also relates to compositions comprising the immunogenic synthetic constructs and methods of inducing an immune response against in a subject comprising administering the immunogenic synthetic constructs, and/or compositions comprising the immunogenic synthetic construct, to the subject. 1Campylobacter jejuniC. jejuni. An immunogenic synthetic construct capable of inducing an immune response against () in a subject , wherein said immunogenic synthetic construct comprises one or more MeOPN-6-Gal monosaccharides , and further comprises one or more additional saccharides.2. The immunogenic synthetic construct of wherein the immunogenic synthetic construct is conjugated to a carrier protein.3. The immunogenic synthetic construct of wherein the carrier protein contains at least one T-cell epitope.4. The immunogenic synthetic construct of wherein the carrier protein is an ETEC protein or CRM.5. The immunogenic synthetic construct of wherein the one or more additional saccharides is selected from the group consisting of monosaccharides containing one or more MeOPN moieties claim 1 , galactose claim 1 , fructose claim 1 , glucose claim 1 , heptose claim 1 , N-acetyl galactosamine claim 1 , N-acetyl glucosamine claim 1 , glucitol claim 1 , glucose claim 1 , and modified forms or derivatives thereof.6. The immunogenic synthetic construct of wherein the monosaccharides containing one or more MeOPN moieties is MeOPN-2-Gal monosaccharide.7. The immunogenic synthetic construct of wherein said immunogenic synthetic construct is MeOPN-1-Fru.8C. jejuni. The immunogenic synthetic construct of ...

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Номер записи: 96
13-06-2019 дата публикации

Crocins Compounds and Uses Thereof

Номер: US20190177354A1
Автор: Bao Xiuqi, Gao Hao, Li Lin, NI YANG, Yao Xinsheng, Yu Yang, Zang Caixia, Zhang Dan, Zheng Yuanpeng
Принадлежит: Jinan University

Provided are a series of crocins compounds and related pharmacological applications thereof in prevention and treatment of Alzheimer's disease. The series of crocins compounds are obtained by taking the Chinese herb, namely Ellis, as a raw material and separating same by means of various methods. The compounds playing a role in preventing oxidative injury caused by hydrogen peroxide (HO) and excitatory amino acid injury caused by L-glutamic acid are screened out by in-vitro cell experiments. The results show that the crocins compounds have good effect in preventing cell injury caused by HOand L-glutamic acid. The compounds have good effect in preventing and treating Alzheimer's disease due to the fact that significant rise of oxidative stress and excitatory amino acid is a key factor for nerve injury in Alzheimer's disease, and have broad development and application prospect. 121-. (canceled)23. The compound according to claim 22 , wherein the configuration of the double bound is the trans E configuration claim 22 , Rrepresents glucosyl group claim 22 , and Rrepresents quinic acid group.25. The compound according to claim 22 , wherein the configuration of the double bound is the cis Z configuration claim 22 , Rrepresents H claim 22 , a glucosyl group claim 22 , or a quinic acid group claim 22 , and Rrepresents H claim 22 , a glucosyl group claim 22 , or a quinic acid group.27. The compound according to claim 22 , wherein the configuration of the double bond the trans E configuration claim 22 , Rrepresents a glucosyl group claim 22 , and Rrepresents a glucosyl group or H.29. The compound according to claim 22 , wherein the configuration of the double bond is the trans E configuration claim 22 , Rrepresents a glucosyl group claim 22 , and Rrepresents CHCH.31. The compound according to claim 22 , wherein the configuration of the double bond is the trans E configuration claim 22 , Rrepresents a glucosyl group or a xylosyl group claim 22 , and Rrepresents H.33. A method ...

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Номер записи: 97
09-07-2015 дата публикации

OPTICALLY PURE BENZYL-4-CHLOROPHENYL-C-GLUCOSIDE DERIVATIVE

Номер: US20150191502A1
Автор: Wu Frank
Принадлежит: XUANZHU PHARMA CO., LTD.

The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity) 3. The process for preparing the compound represented by formula (II) according to claim 2 , wherein said organic solvent is selected from N-methylpyrrolidone claim 2 , N claim 2 ,N-dimethylformamide claim 2 , tetrahydrofuran claim 2 , dioxane and acetonitrile claim 2 , preferably N-methylpyrrolidone.6. The process for preparing the compound represented by formula (III) according to claim 5 , wherein said organic solvent is selected from toluene claim 5 , N claim 5 ,N-dimethylformamide claim 5 , tetrahydrofuran claim 5 , dioxane and acetonitrile; preferably toluene.12. A pharmaceutical composition claim 1 , which contains the compound represented by formula (II) and/or the compound represented by formula (III) as defined in or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers and/or diluents claim 1 , and is in any pharmaceutically acceptable dosage form.13. The pharmaceutical composition according to claim 12 , which further contains one or more hypoglycemic agents claim 12 , wherein said hypoglycemic agent is selected from sitagliptin phosphate claim 12 , vildagliptin claim 12 , saxagliptin claim 12 , alogliptin benzoate claim 12 , linagliptin claim 12 , teneligliptin claim 12 ...

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Номер записи: 98
29-06-2017 дата публикации

METHOD FOR PRODUCING SUCROSE FATTY ACID ESTER

Номер: US20170183371A1
Автор: AKIYAMA Koki, KIDANI Keiji, KURIHARA Hideshi, OKUMURA Haruki, Tsukahara Yasunori
Принадлежит: Microwave Chemical Co., Ltd.

The present invention provides a method for producing a sucrose fatty acid ester having high monoester selectivity, the method for producing a sucrose fatty acid ester comprising a step of preparing an aqueous solution containing sucrose and a basic catalyst; and a step of producing a sucrose fatty acid ester, by mixing the aqueous solution obtained in the aforementioned step, a fatty acid alkali metal salt and a melted fatty acid ester, and heating the mixture with stirring under reduced pressure, wherein the step of producing a sucrose fatty acid ester has an earlier step of removing water from the mixture, and a subsequent step of performing transesterification after the earlier step, and, in the subsequent step, heating is performed through microwave irradiation such that the temperature of the mixture is below the sucrose decomposition temperature. 1. A method for producing a sucrose fatty acid ester , comprising:a step of preparing an aqueous solution containing sucrose and a basic catalyst; and wherein the step of producing a sucrose fatty acid ester has an earlier step of removing water from the mixture, and a subsequent step of performing transesterification after the earlier step, and', 'in the subsequent step, heating is performed through microwave irradiation such that the temperature of the mixture is below a decomposition temperature of the sucrose., 'a step of producing a sucrose fatty acid ester, by mixing the aqueous solution obtained in the aforementioned step, a fatty acid alkali metal salt, and a fatty acid ester, and heating the mixture with stirring under reduced pressure,'}2. The method for producing a sucrose fatty acid ester according to claim 1 , wherein a sucrose fatty acid ester with a monoester weight proportion of 60% by weight or more is produced.3. The method for producing a sucrose fatty acid ester according to claim 1 , wherein the fatty acid ester is a fatty acid ester whose constituent fatty acid includes at least one selected ...

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Номер записи: 99
15-07-2021 дата публикации

FLUORINATED N-ACETYL GLUCOSAMINE ANALOGS AND XYLOSE DERIVATIVES

Номер: US20210214384A1
Автор: KEOUGH Michael Bradley, Ling Chang-Chun, RAWJI Khalil Sherali, STEPHENSON Erin Laurel, YONG Voon Wee, Zhang Ping
Принадлежит:

The present disclosure relates to analogs of N-acetyl glucosamine fluorinated at 4- and/or 6-position(s) and derivatives of xylose at anomeric position for the treatment of a neurological disease, inflammation, cancer and a central nervous system injury. 2. A compound of claim 1 , where Rand Rare either an acetyl group or propanoyl claim 1 , and Ris either a H or an acyl group with formula CHCO— (n=2-9) claim 1 , a stereoisomer claim 1 , a racemate claim 1 , a tautomer claim 1 , a pharmaceutically acceptable salt claim 1 , a solvate claim 1 , a prodrug claim 1 , or a functional derivative thereof.4. A compound of claim 3 , where Rand Rare either an acetyl group or propanoyl claim 3 , and Ris either a H or an acyl group with formula CHCO— (n=2-9) claim 3 , a stereoisomer claim 3 , a racemate claim 3 , a tautomer claim 3 , a pharmaceutically acceptable salt claim 3 , a solvate claim 3 , a prodrug claim 3 , or a functional derivative thereof.7. A compound of claim 6 , where Rand Rare either an acetyl group or propanoyl or butanoyl claim 6 , and Ris either a H or an acyl group with formula CHCO— (n=2-9) claim 6 , a stereoisomer claim 6 , a racemate claim 6 , a tautomer claim 6 , a pharmaceutically acceptable salt claim 6 , a solvate claim 6 , a prodrug claim 6 , or a functional derivative thereof.12. A pharmaceutical composition comprising a compound of any one of to claim 6 , or a stereoisomer claim 6 , a racemate claim 6 , a tautomer claim 6 , a pharmaceutically acceptable salt claim 6 , a solvate claim 6 , a prodrug claim 6 , or a functional derivative thereof.13. Use of a compound of any one of to claim 6 , or a composition of claim 6 , for treating a subject claim 6 , or suspected of having a neurological disease or disorder.14. Use of a compound of any one of to claim 6 , or a composition of for treating a subject with claim 6 , or suspected of having multiple sclerosis.15. Use of a compound of any one of to claim 6 , or a composition of for treating a subject ...

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Номер записи: 100