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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 5533. 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
13-12-2012 дата публикации

Aminoglycosides: synthesis and use as antifungals

Номер: US20120316125A1
Автор: Cheng-Wei Tom Chang, Jon Takemoto
Принадлежит: Utah State University USU

The present invention relates to novel aminoglycoside analogs having certain substituents at the 6 position of ring III which exhibit improved antifungal activity but possess minimal antibacterial properties. The compounds of the present invention are analogues of kanamycin A. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating or preventing fungal disease.

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Номер записи: 5
20-12-2012 дата публикации

Inhibition of biofilm formation by 1,2,3,4,6-penta-o-galloyl-d-glucopyranose

Номер: US20120321566A1
Автор: Fang-Rong Chang, Hung-Wei Yang, Mei-Hui Lin, Mu-Yi Hua, Shih-Tung Liu
Принадлежит: Chang Gung University CGU

Disclosed herein are an anti-biofilm composition and a method to inhibit or prevent cell adhesion and/or biofilm formation by a microorganism, in which use of 1,2,3,4,6-penta-O-galloyl-D-glucopyranose (PGG) is involved therein.

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Номер записи: 6
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: 7
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: 8
10-01-2013 дата публикации

Triterpene saponins, methods of synthesis, and uses thereof

Номер: US20130011421A1
Автор: Annie Won, David Gin, Govind Ragupathi, Kai Deng, Michelle Adams, Nicholas Perl, Philip Livingston
Принадлежит: SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

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

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Номер записи: 9
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: 10
25-04-2013 дата публикации

Compositions and methods for treating nephropathy

Номер: US20130101514A1
Автор: Daniel Joseph Cushing
Принадлежит: Complexa Inc

Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.

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Номер записи: 11
27-06-2013 дата публикации

Substituted saccharide compounds and dental compositions

Номер: US20130164709A1
Автор: Afshin Falsafi, Brian A. Shukla, George W. Griesgraber, Jie Yang, Naimul Karim, Paul R. Klaiber, Richard B. Ross, Sumita B. Mitra, Yi He
Принадлежит: 3M Innovative Properties Co

Substituted saccharide compounds, dental compositions comprising substituted saccharide compounds, and methods of using dental compositions are described. In one embodiment, the substituted saccharide amide compound comprises a hydrophobic group and at least one free-radically polymerizable group with the proviso that the hydrophobic group is not bonded to the ethylenically unsaturated carbon atom of the free-radically polymerizable group. The hydrophobic group is typically bonded to a nitrogen atom of a saccharide amine residue or a carbonyl moiety of saccharide amide residue.

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Номер записи: 12
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: 13
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: 14
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: 15
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: 16
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: 17
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: 18
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: 19
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: 20
21-11-2013 дата публикации

Maple tree-derived products and uses thereof

Номер: US20130310332A1
Автор: Genevieve Beland, Julie Barbeau, Navindra P. Seeram, TAO Yuan
Принадлежит: FEDERATION DES PRODUCTEURS ACERICOLES DU QUEBEC, Rhode Island University

The present document describes a neutraceutical, cosmeceuticals, functional food, pharmaceutical, food ingredient, and non-food ingredient compositions comprising sugar maple extract, essential oil compositions comprising oil extracted from an Acer tree, sweetening compositions containing sugar extracted from maple tree leaves, food ingredients comprising maple tree extract, cosmetic composition comprising maple tree extracts, infusion compositions prepared from maple tree leaves, maple roots, maple wood, maple stems of leaves and samara, and stems/twigs as well as compounds isolated from sugar maple biomass and the methods of extracting the same.

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Номер записи: 21
28-11-2013 дата публикации

Compounds and Compositions for the Detection and Treatment of Alzheimer's Disease and Related Disorders

Номер: US20130315827A1
Автор: ELMALEH David R., Fu Hongning, Shoup Timothy M.
Принадлежит:

One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera. 2. The compound of claim 1 , wherein said compound comprises at least one F claim 1 , Br claim 1 , Br claim 1 , I claim 1 , I or I.3. The compound of claim 1 , wherein said compound comprises at least one F.4. The compound of claim 1 , wherein L is —C(═O)Ror —C(═O)[C(R)]C(═O)R.5. The compound of claim 1 , wherein L is —C(═O)R.6. The compound of claim 1 , wherein L is —C(═O)[CH]C(═O)R.7. The compound of claim 1 , wherein L is —C(═O)CHCHC(═O)R.8. The compound of claim 1 , wherein Ris —H claim 1 , —F claim 1 , —Cl claim 1 , —Br claim 1 , —I claim 1 , or —OH.9. The compound of claim 1 , wherein Ris —F or —OH.10. The compound of claim 1 , wherein Ris —F or —OH; provided that only one Ris —F.14. The compound of claim 1 , wherein the compound comprises a radioimaging agent.15. The compound of claim 1 , wherein L is —H claim 1 , one Ris fluoro; and the other Rare hydroxy claim 1 , alkoxy claim 1 , aryloxy claim 1 , heteroaryloxy claim 1 , aralkyloxy claim 1 , or heteroaralkyloxy.16. The compound of claim 1 , wherein the compound is 1-deoxy-1-fluoro-scyllo-inostiol or 1-deoxy-1-fluoro-myo-inositol.17. The compound of claim 14 , wherein R claim 14 , R claim 14 , or Rcomprises the radioimaging agent; and{'sup': '18', 'the radioimaging agent is F.'}18. A pharmaceutical composition comprising a ...

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Номер записи: 22
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: 23
26-12-2013 дата публикации

Photoacid generator, photoresist, coated substrate, and method of forming an electronic device

Номер: US20130344438A1
Автор: Cheng-Bai Xu, Cong Liu, Emad Aqad, Gregory P. Prokopowicz, Irvinder Kaur, Mingqi Li
Принадлежит: Rohm and Haas Electronic Materials LLC

A photoacid generator has the formula (I): wherein R 1 , R 2 , R 3 , L 1 , L 2 , L 3 X, Z + , a, b, c, d, p, q, and r, are defined herein. A photoresist comprises the photoacid generator, and a coated article comprises the photoresist. The photoresist can be used to form an electronic device.

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Номер записи: 24
09-01-2014 дата публикации

Synthetic Lipid A Derivative

Номер: US20140011987A1
Автор: BOONS Geert-Jan
Принадлежит: University of Georgia Research Foundation, Inc.

The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative. 2. The compound of wherein Ris tert-butyldimethylsilyl (TBS) or dimethylthexylsilyl (TDS).3. The compound of wherein Ris azido.4. The compound of wherein Ris an amino protecting group comprising 9-fluorenylmethoxycarbamate (Fmoc).5. The compound of wherein Ris a hydroxyl protecting group comprising allyloxycarbonate (Alloc).6. The compound of wherein Ris an amino protecting group comprising 9-fluorenylmethoxycarbamate (Fmoc).7. The compound of wherein Ris a hydroxyl protecting group comprising allyloxycarbonate (Alloc) or levulinate (Lev).8. The compound of wherein Rand Rtogether form a ring comprising an acetal.10. The method of wherein selectively acylating the functionalized disaccharide comprises selectively acylating the functionalized disaccharide at two claim 9 , three or four of positions C-2 claim 9 , C-3 claim 9 , C-2′ and C-3′ of the functionalized disaccharide.11. The method of further comprising phosphorylating the functionalized disaccharide at either or both of the C-1 or C-4′ positions of the functionalized disaccharide.12. The method of further comprising contacting the functionalized disaccharide with a 3-deoxy-D-manno-oct-2-ulosonic acid (KDO) donor to yield a KDO glycoside at the C-6′ position of the functionalized disaccharide.13. The method of wherein Ris tert-butyldimethylsilyl (TBS) or dimethylthexylsilyl (TDS).14. The method of wherein Ris azido.15. The method of wherein Ris an amino protecting group comprising 9-fluorenylmethoxycarbamate (Fmoc).16. The method of wherein Ris a hydroxyl protecting group comprising allyloxycarbonate (Alloc). This application is a continuation application of U.S. application Ser. No. 12/676,253, filed Apr. 19, 2010, which is national stage application of International Application No. PCT/US2008/010394, filed ...

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Номер записи: 25
09-01-2014 дата публикации

Dibenzo[B,F][1,4]Oxazepin-11-yl-N-Hydroxybenzamides as HDAC Inhibitors

Номер: US20140011988A1
Автор: BEAULIEU Patrick, Chantigny Yves Andre, Chesworth Richard, Deziel Robert, Leit Silvana, Mancuso John, Shapiro Gideon, Smil David, Tessier Pierre
Принадлежит:

This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) 225.-. (canceled) This application claims the benefit of U.S. application Ser. No. 11/925,151, filed Oct. 26, 2007, which claims the benefit of U.S. provisional application 60/884,287, filed Jan. 10, 2007, and U.S. provisional application 60/863,347, filed Oct. 28, 2006.1. Field of the InventionThis invention relates to compounds for the inhibition of histone deacetylase.2. Description of Related ArtIn eukaryotic cells, nuclear DNA associates with histones to form a compact complex called chromatin. The histones constitute a family of basic proteins which are generally highly conserved across eukaryotic species. The core histones, termed H2A, H2B, H3, and H4, associate to form a protein core. DNA winds around this protein core, with the basic amino acids of the histones interacting with the negatively charged phosphate groups of the DNA. Approximately 146 base pairs of DNA wrap around a histone core to make up a nucleosome particle, the repeating structural motif of chromatin.Csordas, 286: 23-38 (1990) teaches that histones are subject to posttranslational acetylation of the N-terminal lysine residues, a reaction that is catalyzed by histone acetyl transferase (HAT1). Acetylation neutralizes the positive charge of the lysine side chain, and is thought to impact chromatin structure. Indeed, Taunton et al., 272: 408-411 (1996), teaches that access of transcription factors to chromatin templates is enhanced by histone hyperacetylation. Taunton et al. further teaches that an enrichment in underacetylated histone H4 has been found in transcriptionally silent regions of the genome.Histone acetylation is a reversible modification, with deacetylation being catalyzed by a family of enzymes termed histone deacetylases (HDACs). The molecular cloning of gene sequences encoding proteins with HDAC activity has established the ...

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Номер записи: 26
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: 27
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: 28
06-02-2014 дата публикации

6"-amino-6"-deoxygalactosylceramides

Номер: US20140037693A1
Автор: Albert Bendelac, Luc Teyton, Paul B. Savage
Принадлежит: BRIGHAM YOUNG UNIVERSITY, Scripps Research Institute, University of Chicago

This invention relates to galactosylceramide compounds.

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Номер записи: 29
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: 30
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: 31
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: 32
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: 33
03-04-2014 дата публикации

FGF RECEPTOR-ACTIVATING 3-O-ALKYL OLIGOSACCHARIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

Номер: US20140094429A1
Автор: DRIGUEZ Pierre Alexandre, DUCHAUSSOY Philippe, Fons Pierre
Принадлежит: SANOFI

The invention relates to the FGF receptor-activating oligosaccharides corresponding to formula (I): 2. The compound according to claim 1 , in which n=1 and m=0 or n=0 and m=1.3. The compound according to claim 1 , in which Rrepresents an —O-alkyl group claim 1 , where said alkyl group contains from 1 to 8 carbon atoms and is optionally substituted with 1 or 2 groups claim 1 , which may be identical or different claim 1 , selected from aryl groups.4. The compound according to claim 1 , in which Rrepresents an —O-methyl or —O-pentyl group and is optionally substituted with 1 or 2 phenyl groups.5. The compound according to claim 1 , in which R claim 1 , R claim 1 , R claim 1 , Rand R claim 1 , which may be identical to or different from one another claim 1 , represent an —OSO group or a hydroxyl group claim 1 , on the condition that at least one group among R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents an —OSO group.6. The compound according to claim 1 , in which R claim 1 , R claim 1 , R claim 1 , Rand Rall represent —OSO groups.7. The compound according to claim 1 , in which at least one of the groups R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents an —OSO group claim 1 , and at least one of the groups R claim 1 , R claim 1 , R claim 1 , Rand Rrepresents a hydroxyl group.8. The compound according to claim 1 , in which R claim 1 , Rand Rrepresent —OSO groups claim 1 , and Rand Rrepresent hydroxyl groups.9. The compound according to claim 1 , in which Rrepresents an —NH—CO-alkyl group claim 1 , where said alkyl group comprises from 1 to 4 carbon atoms.10. The compound according to claim 1 , in which R represents a methoxy group.11. The compound according to claim 1 , selected from the following compounds:{'smallcaps': L', 'D', 'L', 'D', 'L', 'D, 'sub': '2', 'methyl (sodium 3-O-methyl-2-O-sodium sulphonato-α--idopyranosyluronate)-(1→4)-(2-acetamido-2-deoxy-3-O-methyl-6-O-sodium sulphonato-α--glucopyranosyl)-(1→4)-[(sodium 3-O-methyl-2-O-sodium sulphonato-α-- ...

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Номер записи: 34
03-01-2019 дата публикации

Compounds, compositions and methods for protecting brain health in neurodegenerative disorders

Номер: US20190000867A1
Автор: Christopher Rinsch, Philippe V. Dupraz
Принадлежит: AMAZENTIS SA

Aspects of the invention relate to compounds, extracts and compositions thereof, and methods of using of the same, to treat neurodegenerative disorders and/or improve brain health. In certain embodiments, said compounds are pomegranate flavonoids.

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Номер записи: 35
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: 36
07-01-2016 дата публикации

Protected Monomer and Method of Final Deprotection for RNA Synthesis

Номер: US20160002282A1
Автор: Agnieszka Sierzchala, Douglas J. Dellinger, Geraldine F. Dellinger, Joel Myerson, Zoltan Timar
Принадлежит: AGILENT TECHNOLOGIES INC

A method of deprotecting a solid support bound polynucleotide includes the step of contacting the polynucleotide with a composition comprising a diamine under conditions sufficient to deprotect the 2′-protected ribonucleotide residue. The solid support bound polynucleotide has at least one 2′-protected ribonucleotide residue, which has the following structure: wherein B P is a protected or unprotected heterocycle; R 12 is a protecting group selected from a hydrocarbyl, a substituted hydrocarbyl, an aryl, and a substituted aryl; X is O or S; and PG is a thionocarbamate protecting group.

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Номер записи: 37
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: 38
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: 39
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: 40
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: 41
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: 42
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: 43
03-02-2022 дата публикации

Large scale preparation of pseudo-trisaccharide aminoglycosides and of intermediates thereof

Номер: US20220033428A1
Автор: Mani Bushan Kotala, Michael Mizhiritskii, Ravinder PALADI
Принадлежит: Eloxox Pharmaceuticals Ltd, Eloxx Pharmaceuticals Ltd

Synthetic pathways for preparing pseudo-trisaccharide aminoglycoside compounds represented by Formula I or Ia as defined in the specification and donor and acceptor compounds useful for preparing such compounds are provided. A process of stereoselectively preparing compounds represented by Formula III as defined in the specification, while avoiding chromatographic separation of stereoisomers are also provided. Compounds prepared by the described processes and uses thereof are also provided.

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Номер записи: 44
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: 45
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: 46
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: 47
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: 48
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: 49
04-02-2016 дата публикации

Liposomes Useful for Drug Delivery

Номер: US20160030341A1
Автор: Daryl C. Drummond, Dmitri Kirpotin, Keelung Hong
Принадлежит: Merrimack Pharmaceuticals Inc

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

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Номер записи: 50
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: 51
31-01-2019 дата публикации

SEPARATION OF OLIGOSACCHARIDES FROM FERMENTATION BROTH

Номер: US20190031698A1
Автор: CHASSAGNE Pierre, HEDEROS Markus Jondelius, KHANZHIN Nikolay, Matwiejuk Martin
Принадлежит:

The present invention relates to a method for separating sialylated oligosaccharides from a fermentation broth in which they are produced by a genetically modified microorganism The separation comprises the steps of: i) ultrafiltration; ii) nano-filtration; iii) optionally, activated charcoal treatment; and iv) treatment with strong anion and/or cation exchange resin. 1. A method for separating a sialylated oligosaccharide from a fermentation broth obtained by culturing a genetically modified microorganism capable of producing the sialylated oligosaccharide from an internalized carbohydrate precursor , wherein the separation comprises the steps of:i) ultrafiltration,ii) nanofiltration,iii) optionally, activated charcoal treatment, andiv) treatment with strong anion and/or cation exchange resin.2. The method of claim 1 , wherein step i) is conducted before any of the steps ii) claim 1 , iii) or iv).3. The method of claim 1 , wherein step i) comprises two consecutive ultrafiltrations and the molecular weight cut-off of the first ultrafiltration membrane is higher than that of the second membrane.4. The method of any of the claims 1 , wherein step i) further comprises a washing step of the ultrafiltration retentate claims 1 , to obtain a washing filtrate.5. The method of any of the claims 1 , wherein step i) further comprises the dilution of the fermentation broth prior to ultrafiltration.6. The method of claim 4 , wherein the dilution factor of step i) is 1 to 3.5.7. The method of claim 1 , wherein the ultrafiltration step is characterized by a concentration factor of at least 1.25.8. The method of claim 1 , wherein the ultrafiltration permeate is nanofiltered in step ii).9. The method of claim 8 , wherein the molecular weight cut-off of the nanofiltration membrane in step ii) is lower than that of the ultrafiltration membrane in step i).10. The method of claim 9 , wherein the molecular weight cut-off of the nanofiltration membrane in step ii) is around 25-50% of the ...

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Номер записи: 52
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: 53
04-02-2021 дата публикации

GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS

Номер: US20210032250A1
Автор: LONG Daniel D., LOO MANDY M., Wilton Donna A.A.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: 172-. (canceled)74. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is suitable for oral administration.75. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a capsule.76. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a tablet.77. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a pill.78. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a lozenge claim 73 , cachet claim 73 , dragee claim 73 , granules claim 73 , emulsion claim 73 , elixir claim 73 , or syrup.79. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a suspension.80. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a solution.81. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition is in the form of a powder.82. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 95% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.83. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 30% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.84. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.01 to about 10% by weight of the compound of formula VII-1 claim 73 , or a pharmaceutically acceptable salt thereof.85. The pharmaceutical composition of claim 73 , wherein the pharmaceutical composition comprises from about 0.1 to about 10% by weight of the ...

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Номер записи: 54
04-02-2021 дата публикации

CELL LABELING AGENT AND CELL LABELING KIT

Номер: US20210033617A1
Автор: Ishizuka Takumi, Xu Yan, Zhao Pei-Yan
Принадлежит:

The cell labeling agent includes a monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells. Among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives, at least one group that does not change, even when metabolized by the sialic acid biosynthetic pathway, includes a ring structure with a carbon-carbon double bond or triple bond. 16-. (canceled)7. A cell labeling agent , comprising monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells ,wherein at least one group in the monosaccharide derivatives that does not change even when metabolized by the sialic acid biosynthetic pathway, comprises a ring structure with a carbon-carbon double bond or triple bond among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives.14. A cell labeling kit comprising:{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'the cell labeling agent according to , and'}a reporter substance that binds to the sialic acid by reacting with the group presented outside the cell, wherein the group is not changed when metabolized by the sialic acid biosynthetic pathway. The present disclosure relates to a cell labeling agent and a cell labeling kit.Metabolic labeling methods are known to use the metabolism of monosaccharides by the sialic acid biosynthetic pathway to label sugar chains on the cell surface. In the metabolic labeling method, for example, a derivative of N-acetyl mannosamine (ManNAc) with an azide group (peracetylated N-azidoacetyl mannosamine, AcManNAz) is used. AcManNAz taken up into the cell is enzymatically deacetylated in the cytoplasm and is metabolized to the corresponding N-azidoacetylsialic acid (SiaNAz). SiaNAz is incorporated into the sialo sugar complex and then is presented to the cell surface along with ...

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Номер записи: 55
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: 56
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: 57
19-02-2015 дата публикации

Dually Derivatized Chitosan Nanoparticles and Methods of Making and Using the Same

Номер: US20150051265A1
Автор: Anthony Cheung, Eric Hsu, JUN Gao
Принадлежит: Engene Inc

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.

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Номер записи: 58
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: 59
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: 60
25-02-2021 дата публикации

CONJUGATED ANTISENSE COMPOUNDS AND THEIR USE

Номер: US20210054017A1
Автор: Migawa Michael T., Prakash Thazha P., Seth Punit P., Swayze Eric E.
Принадлежит:

Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the gomeric compounds are conjugated to N-Acetylgalactosamine or to N-Acetylgalactosamine anaologues. 1243-. (canceled)247. The compound of claim 245 , wherein Qis CH.248. The compound of claim 244 , wherein Ris CHN.249. The compound of claim 248 , wherein Qis CH.252. The compound of claim 250 , wherein Ris CHOH.254. The compound of wherein L comprises a phosphorus linking group claim 244 , NH claim 244 , or N(CH).256. The compound of claim 244 , wherein the oligomer is a modified oligonucleotide comprising at least one modified nucleoside comprising a modified base and/or a modified sugar moiety.257. The compound of having at least one modified nucleoside comprising a modified sugar moiety selected from a bicyclic sugar moiety and a 2′-substituted sugar moiety.258. The compound of claim 257 , comprising at least one 4′-C(CH)H—O-2′ or 4′-CH—O-2′bridged bicyclic sugar moiety.259. The compound of comprising at least one 2′-O(CH)OCHsubstituted sugar moiety.260. The compound of claim 244 , wherein the conjugate group is attached to the 5′-terminal nucleoside of the oligomer.261. The compound of claim 244 , wherein the conjugate group is attached to the 3′-terminal nucleoside of the oligomer.262. The compound of claim 244 , wherein the oligomer is an oligonucleotide and has a sugar motif comprising:a 5′-region consisting of 2-8 linked 5′-region nucleosides, wherein at least two 5′-region nucleosides are modified nucleosides and wherein the 3′-most 5′-region nucleoside is a modified nucleoside;a 3′-region consisting of 2-8 linked 3′-region nucleosides, wherein at least two 3′-region nucleosides are modified nucleosides and wherein the 5′-most 3′-region nucleoside is a modified nucleoside; anda central region between the 5′-region and the 3′-region consisting of 5-10 linked central region nucleosides, each independently selected from among: a modified nucleoside and an unmodified ...

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Номер записи: 61
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: 62
23-02-2017 дата публикации

REAGENT-CONTROLLED STEREOSELECTIVE GLYCOSYLATION

Номер: US20170051003A1
Автор: Bennett Clay S., Issa John P., Lloyd Dina
Принадлежит:

Provided are methods for the efficient stereoselective formation of glycosidic bonds, without recourse to prosthetic or directing groups. 1. A method of forming a glycosidic bond , comprising:combining a first solvent, a reducing sugar, and a first strong Bronsted base, thereby forming a first reaction mixture;combining a sulfonylating agent and the first reaction mixture, thereby forming a glycosyl sulfonate;combining a second solvent, a glycosyl acceptor, and a second strong Bronsted base, thereby forming a second reaction mixture; andcombining the glycosyl sulfonate and the second reaction mixture, thereby forming a glycosidic bond;wherein the reducing sugar is a pyranose; the sulfonylating agent is a sulfonyl halide; and the glycosidic bond is formed with greater than or equal to 90% stereoselectivity for a particular stereochemical configuration.2. The method of claim 1 , wherein the glycosidic bond is formed with greater than or equal to 95% stereoselectivity for a particular stereochemical configuration.3. (canceled)4. (canceled)5. The method of claim 1 , wherein the reducing sugar is a 2-deoxy-sugar.6. (canceled)7. (canceled)8. The method of claim 1 , wherein the reducing sugar is a -sugar; and the particular stereochemical configuration is a β linkage.9. The method of claim 8 , wherein the reducing sugar is a 2-deoxy--sugar.10. The method of claim 8 , wherein the reducing sugar is a -pyranose.11. (canceled)12. The method of claim 1 , wherein the reducing sugar is an -sugar; and the particular stereochemical configuration is a β linkage.13. The method of claim 12 , wherein the reducing sugar is a 2-deoxy--sugar.14. The method of claim 12 , wherein the reducing sugar is an -pyranose.15. (canceled)16. The method of claim 1 , wherein the reducing sugar is a 2 claim 1 ,6-dideoxy--sugar.18. The method of claim 1 , wherein the first strong Bronsted base is non-nucleophilic.19. The method of claim 1 , wherein the second strong Bronsted base is non-nucleophilic.20. ...

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Номер записи: 63
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: 64
01-03-2018 дата публикации

Derivatives of sobetirome

Номер: US20180057472A1
Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan
Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 65
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: 66
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: 67
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: 68
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: 69
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: 70
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: 71
17-03-2016 дата публикации

Aminoglycosides and uses thereof in treating genetic disorders

Номер: US20160074425A1
Автор: Dana Atia-Glikin, Jeyakumar Kandasamy, Timor Baasov, Valery Belakhov
Принадлежит: Technion Research and Development Foundation Ltd

A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5″ position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

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Номер записи: 72
18-03-2021 дата публикации

IMMUNIGENIC ALPHA-BRANCHED TREHALOSE-DIESTERS

Номер: US20210077618A1
Автор: EVANS Jay T, SMITH Alyson
Принадлежит: GLAXOSMITHKLINE BIOLOGICALS SA

The invention relates to compounds of formula (I) and their use in eliciting a pro-Thl7 immune response. Further provided are methods of production of said compounds. (Formula I) wherein m is an integer between 4 and 13; n is an integer between 4 and 13; x is an integer between 4 and 13; y is an integer between 4 and 13. 257.-. (canceled)58. The compound according to claim 1 , wherein m is 6 and n is 6.59. The compound according to claim 1 , wherein x is 6 and y is 6.60. The compound according to claim 1 , wherein m is 6 claim 1 , n is 6 claim 1 , x is 6 and y is 6 claim 1 , or a pharmaceutically acceptable salt and/or solvate thereof.62. The method according to claim 61 , wherein the pro-Th17 response involves the elicitation of TNF-alpha claim 61 , IL-6 claim 61 , IL-23 and IL-1beta.63. The method according to claim 61 , wherein the pro-Th17 response involves the elicitation of IL-17 cytokine.64. The method according to claim 61 , wherein the pro-Th17 response involves the elicitation of Th17 cells.65. The method of claim 61 , wherein the subject is a human subject.66. The method according to claim 61 , wherein m is 5 claim 61 , 6 claim 61 , or 7; n is 5 claim 61 , 6 claim 61 , or 7; x is 5 claim 61 , 6 claim 61 , or 7; and y is 5 claim 61 , 6 claim 61 , or 7.67. The method according to claim 61 , wherein m is 6 claim 61 , n is 6 claim 61 , x is 6 and y is 6.69. The immunogenic composition according to claim 68 , wherein m is 6 and n is 6.70. The immunogenic composition according to claim 68 , wherein x is 6 and y is 6.71. The immunogenic composition according to claim 68 , wherein m is 6 claim 68 , n is 6 claim 68 , x is 6 and y is 6.72. The immunogenic composition according to claim 68 , wherein antigen is from a human or non-human bacterial claim 68 , viral claim 68 , fungal claim 68 , microorganism or multicellular parasitic pathogen.73Mycobacterium tuberculosis.. The immunogenic composition according to claim 72 , wherein antigen is from74. The immunogenic ...

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Номер записи: 73
05-06-2014 дата публикации

Azacitidine process and polymorphs

Номер: US20140155588A1
Автор: Ganesh Varanasi, Praveen Cherukupally, Satish Kumar Vujjini, Satyanarayana Raju Tirumalaraju, Sreenadha Charyulu Kandala, Srinivas Areveli
Принадлежит: Dr Reddys Laboratories Inc, Dr Reddys Laboratories Ltd

Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form I and mixtures of azacitidine crystalline Forms I and II.

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Номер записи: 74
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: 75
14-03-2019 дата публикации

Brain-Targeting Prodrug for AMPA Receptor Synergist, and Pharmaceutical Applications Thereof

Номер: US20190077821A1
Автор: Li Song, Li Xingzhou, Wang Xiaokui, XIAO Dian, Xiao Junhai, Xie Yunde, Zheng Zhibing, Zhong Wu, Zhou Xinbo
Принадлежит: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA

Disclosed in the present invention is a compound of Formula (I), a geometric or optical isomer, a pharmaceutically acceptable salt, a solvate or a polymorph thereof. Also disclosed in the present invention is a composition comprising the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof. Also disclosed in the present invention is a use of the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof in the treatment of a disease or disorder such as a hypoglutamatergic condition, a neurodegenerative disease or respiratory depression, particularly in the treatment of a disease or disorder associated with AMPA receptor. 11. A pharmaceutical composition claim 1 , comprising an effective amount of the compound claim 1 , the geometric or optical isomer claim 1 , the pharmaceutically acceptable salt claim 1 , the solvate or the polymorph thereof according to claim 1 , and one or more pharmaceutically acceptable carriers claim 1 , additives or excipients.12. A method for treating a disease or disorder or for alleviating the severity of the disease or disorder claim 1 , wherein the method comprises administering to a patient in need of such treatment a therapeutically effective amount of at least one of the compound claim 1 , the geometric or optical isomer claim 1 , the pharmaceutically acceptable salt claim 1 , the solvate or the polymorph thereof according to claim 1 , wherein the disease or disorder is selected from the group consisting of a hypoglutamatergic condition claim 1 , impaired memory or other cognitive functions caused by a deficiency in the number or strength of excitatory synapses claim 1 , or a deficiency in the number of DL-α-amino-3-hydroxy-5-methyl-4-isoxazolyl propionic acid (AMPA) receptors claim 1 , schizophrenia or schizophreniform behavior caused by a cortical/striatal imbalance due to a ...

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Номер записи: 76
22-03-2018 дата публикации

Method for producing glycoside compounds

Номер: US20180079768A1
Автор: Akihiro Itoh, Eriko Aoki, Tadaaki Ohgi, Takashi Kinoshita
Принадлежит: Bonac Corp

The invention provides a production method of a glycoside compound or a salt thereof, which includes subjecting a thioether compound and an alcohol compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid, and then distillation in the presence of at least one kind of additive selected from a sulfur-containing antioxidant and a maleimide group-containing compound to give a thioether compound and a step of subjecting a glycoside compound and a thioether compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid to give a glycoside compound. By this method, a phosphoramidite preferable for the production (synthesis) of a nucleic acid can be produced more efficiently at a high purity.

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Номер записи: 77
23-03-2017 дата публикации

Liposomes Useful for Drug Delivery

Номер: US20170079914A1
Автор: Daryl C. Drummond, Dmitri Kirpotin, Keelung Hong
Принадлежит: Merrimack Pharmaceuticals Inc

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

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Номер записи: 78
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: 79
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: 80
26-03-2015 дата публикации

Triterpene saponins, methods of synthesis and uses thereof

Номер: US20150086585A1
Автор: Annie Won, David Gin, Govind Ragupathi, Kai Deng, Michaelle ADAMS, Nicholas Perl, Philip Livingston
Принадлежит: SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

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

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Номер записи: 81
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: 82
12-03-2020 дата публикации

Aminoglycosides and uses thereof in treating genetic disorders

Номер: US20200078386A1
Автор: Dana Atia-Glikin, Jeyakumar Kandasamy, Timor Baasov, Valery Belakhov
Принадлежит: Technion Research and Development Foundation Ltd

A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5″ position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

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Номер записи: 83
12-03-2020 дата публикации

BIOSYNTHESIS OF HUMAN MILK OLIGOSACCHARIDES IN ENGINEERED BACTERIA

Номер: US20200080119A1
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: 84
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: 85
29-03-2018 дата публикации

Dextrin fatty acid ester and cosmetic

Номер: US20180085299A1
Автор: Daisuke Kato, Takanao Suzuki
Принадлежит: Chiba Flour Milling Co Ltd

A dextrin fatty acid ester is provided in which the dextrin has an average degree of glycopolymerization of 3 or more and 100 or less. The fatty acid comprises one or more linear saturated fatty acids having 14 or more and 18 or less carbon atoms, and one or more branched saturated fatty acids having 14 or more and 18 or less carbon atoms. The molar fraction of the linear saturated fatty acid in the fatty acid is 0.75 or more and 0.95 or less. The average degree of substitution of the fatty acid per glucose unit is 1.5 or more and 2.0 or less.

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Номер записи: 86
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: 87
05-04-2018 дата публикации

Compositions Containing Tannic Acids and Uses Thereof

Номер: US20180092935A1
Автор: Ching-Cheng Wang, Guochuan Emil Tsai, Tien-Lan HSIEH, Yi-Wen Mao
Принадлежит: Syneurx International Taiwan Corp

Compositions (e.g., pharmaceutical compositions, nutraceutical compositions or medical food compositions) comprising tannic acids, particularly tannic acids which are D-amino acid oxidase inhibitor with superior potency, purity and safety profile; and uses thereof for treating CNS disorder and obesity disorders including diabetes, hyperglycemia, hyperlipidemia or hypercholesterolemia.

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Номер записи: 88
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: 89
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: 90
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: 91
12-05-2022 дата публикации

Liquid dispersions for acyl halides

Номер: US20220145541A1
Автор: Jonathan Spender, Michael Albert Bilodeau, Samuel Mikail
Принадлежит: Greentech Global Pte Ltd

The present disclosure describes acyl halide liquid dispersions and tunable methods of treating cellulosic materials with compositions that provide increased hydrophobicity and/or lipophobicity to such materials without sacrificing the biodegradability thereof. The methods as disclosed provide for reacting acyl halides with and binding of saccharide fatty acid esters on cellulosic materials, including that the disclosure provides products made by such methods. The materials thus treated display higher hydrophobicity, lipophobicity, barrier function, and mechanical properties, and may be used in any application where such features are desired.

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Номер записи: 92
06-04-2017 дата публикации

Improved peptide pharmaceuticals for insulin resistance

Номер: US20170096468A1
Автор: John J. Nestor
Принадлежит: Mederis Diabetes LLC, Spitfire Pharma Inc

Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.

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Номер записи: 93
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: 94
14-04-2016 дата публикации

Kinase inhibitors

Номер: US20160102059A1
Автор: Geraint Jones, Matthew Colin Thor Fyfe, Stephen Malcolm Thom, Thomas Matthew BAKER
Принадлежит: Respivert Ltd, TopiVert Pharma Ltd

There are provided compounds of formula I, wherein R 1A to R 1E , R 2 to R 4 , R 5a , L and X 1 to X 3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

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Номер записи: 95
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: 96
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: 97
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: 98
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: 99
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: 100