НЕКОТОРЫЕ СОЕДИНЕНИЯ АМИНОАЛКИЛ ГЛЮКОЗАМИНИД-ФОСФАТА И ИХ ПРИМЕНЕНИЕ

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2007 104 781 (13) A (51) ÌÏÊ C07H 15/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007104781/04, 24.06.2005 (71) Çà âèòåëü(è): ÊÎÐÈÊÑÀ ÊÎÐÏÎÐÅÉØÍ (US) (30) Êîíâåíöèîííûé ïðèîðèòåò: 08.07.2004 US 10/888,683 (43) Äàòà ïóáëèêàöèè çà âêè: 27.08.2008 Áþë. ¹ 24 (72) Àâòîð(û): ÄÆÎÍÑÎÍ Äåéâèä À. (US), ÏÅÐÑÈÍà Äåéâèä Ã. (US) (87) Ïóáëèêàöè PCT: WO 2006/016997 (16.02.2006) Àäðåñ äë ïåðåïèñêè: 103735, Ìîñêâà, óë. Èëüèíêà, 5/2, ÎÎÎ "Ñîþçïàòåíò", ïàò.ïîâ. Ñ.Á.Ôåëèöûíîé (54) ÍÅÊÎÒÎÐÛÅ ÑÎÅÄÈÍÅÍÈß ÀÌÈÍÎÀËÊÈË ÃËÞÊÎÇÀÌÈÍÈÄ-ÔÎÑÔÀÒÀ È ÈÕ A ÏÐÈÌÅÍÅÍÈÅ R U A 2 0 0 7 1 0 4 7 8 1 (57) Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I): ãäå Õ âûáèðàþò èç ãðóïïû, ñîñòî ùåé èç Î è S â àêñèàëüíîì èëè ýêâàòîðèàëüíîì ïîëîæåíèè; Y âûáèðàþò èç ãðóïïû, ñîñòî ùåé èç Î è NH; n, m, p è q âë þòñ öåëûìè ÷èñëàìè îò 0 äî 6; R1, R2 è R3 âë þòñ îäèíàêîâûìè èëè ðàçíûìè è âë þòñ îñòàòêàìè æèðíûõ êèñëîò, âêëþ÷àþùèìè îò 11 äî 14 àòîìîâ óãëåðîäà è ãäå îäèí èç R1, R2 èëè R3 âë åòñ ïðè íåîáõîäèìîñòè âîäîðîäîì; R4 è R5 âë þòñ îäèíàêîâûìè èëè ðàçíûìè è âûáèðàþòñ èç ãðóïïû, ñîñòî ùåé èç Í è ìåòèëà; R6 è R7 âë þòñ îäèíàêîâûìè èëè Ñòðàíèöà: 1 RU 2 0 0 7 1 0 4 7 8 1 (86) Çà âêà PCT: US 2005/022522 (24.06.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 08.02.2007 ðàçíûìè è âûáèðàþòñ èç ãðóïïû, ñîñòî ùåé èç Í, ãèäðîêñè, àëêîêñè, ôîñôîíî, ôîñôîíîêñè, ñóëüôî, ñóëüôîêñè, àìèíî, ìåðêàïòî, öèàíî, íèòðî, ôîðìèë è êàðáîêñè è èõ ñëîæíûõ ýôèðîâ è àìèäîâ; R8 è R9 âë þòñ îäèíàêîâûìè èëè ðàçíûìè è âûáðàíû èç ãðóïïû, ñîñòî ùåé èç ôîñôîíî è Í è õîò áû îäèí èç R8 è R9 âë åòñ ôîñôîíî; R10, R11 è R12 íåçàâèñèìî âûáèðàþò èç ëèíåéíûõ íåçàìåùåííûõ íàñûùåííûõ àëèôàòè÷åñêèõ ãðóïï, âêëþ÷àþùèõ îò 1 äî 10 àòîìîâ óãëåðîäà; èëè èõ ôàðìàöåâòè÷åñêè ïðèåìëåìà ñîëü. 2. Ôàðìàöåâòè÷åñêà êîìïîçèöè , âêëþ÷àþùà : à) ýôôåêòèâíîå êîëè÷åñòâî ñîåäèíåíè ïî ï.1 èëè åãî ôàðìàöåâòè÷åñêè ïðèåìëåìóþ ñîëü è á) ôàðìàöåâòè÷åñêè ...

НЕКОТОРЫЕ АМИНОАЛКИЛГЛЮКОЗАМИНИДФОСФАТНЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ

... 1. Соединение формулы (III) ! ! где X выбирают из группы, состоящей из O и S в аксиальном или экваториальном положении; Y выбирают из группы, состоящей из O и NH; n и m равны 0; ! R1, R2 и R3 являются одинаковыми или различными и представляют собой остатки жирных кислот с 1 и до примерно 20 атомами углерода, и где один из R1, R2 или R3, необязательно, представляет собой необязательно водород; R4 выбран из группы, состоящей из Н и метила; p=1 и R6 представляет собой СООН или p=2 и представляет собой ОРО3Н2; R8 и R9 являются одинаковыми или различными и выбраны из группы, состоящей из H и фосфоно, по меньшей мере, один из R8 и R9 представляет собой фосфоно; R10, R11 и R12 независимо выбраны из группы линейных незамещенных насыщенных алифатических радикалов, содержащих 1-11 атомов углерода; или ! его фармацевтически приемлемая соль. ! 2. Соединение по п.1, где X и Y представляют собой атомы кислорода, R1, R2 и R3 выбирают независимо из числа линейных (С6-С10)-алкильных групп, и R10, R11 и ...

НЕКОТОРЫЕ АМИНОАЛКИЛГЛЮКОЗАМИНИДФОСФАТНЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ

... 1. Соединение формулы (I),где X выбирают из группы, состоящей из О и S в аксиальном или экваториальном положении; Y выбирают из группы, состоящей из О и NH; n, m, р и q равны целым числам от 0 до 6; R, Rи Rявляются одинаковыми или различными и представляют собой остатки жирных кислот с 1 и до примерно 20 атомами углерода, и где один из R, Rили R, необязательно, представляет собой водород; Rи Rявляются одинаковыми или различными и выбраны из группы, состоящей из Н и метила; Rи Rявляются одинаковыми или различными и выбраны из группы, состоящей из Н, гидрокси, алкокси, фосфоно, фосфоноокси, сульфо, сульфоокси, амино, меркапто, циано, нитро, формила и карбокси и их сложных эфиров и амидов; Rи Rявляются одинаковыми или различными и выбраны из группы, состоящей из фосфоно и Н, и, по меньшей мере, один из Rи Rпредставляет собой фосфоно; и R, Rи Rвыбирают, независимо, из числа линейных незамещенных насыщенных алифатических групп с 1-10 атомами углерода;или его фармацевтически приемлемая соль.2 ...

CПOCOБ ПOЛУЧEHИЯ AHAЛOГOB ЛИПИДA A

Способ выделения тринатриевой соли д-фруктоза-1,6-дифосфорной кислоты

PHOSPHOGLYCOLIPID UND VERFAHREN ZU DESSEN VERWENDUNG

ENZYMATIC PRODUCTION OF PHOSPHOLIPID-SACCHARIDE DERIVATIVES

USE OF FRUCTOSE-1,6-DIPHOSPHATE TO PROTECT AGAINST THE TOXIC EFFECTS OF ANTITUMOUR DRUGS

New saccharides,their preparation and pharamceutical compositions containing them.

Compounds of formula III where X and Y independently are oxygen or imino, but not both imino and R1 and R2 independently are acyl of 14 carbons, optionally monosubstituted by hydroxy or acyloxy of 14 carbon atoms except when X is imino and Y is oxygen, R1 and R2 are not both (R)-3-hydroxytetradecanoye are useful as modulators of antimicrobial resistance, for enhancing immune response and unspecific immunity, for preventing endotoxin shock, and for treating malignant tumors and inflammation.

Electrodialysis of Sugar Phosphorylation Reaction Solutions

... 1,195,584. Electro-dialysis of sugar phosphorylation reaction solutions. STAUFFER CHEMICAL CO. July 6, 1967 [Feb. 2, 1967], No. 31179/67. Heading C7B. A solution containing a calcium sugar phosphate, inorganic calcium phosphate and calcium chloride has the CaCl 2 separated from it by electro-dialysis. The calcium sugar phosphate may be derived from sucrose, galactose, arabinose, ribose, xylose, maltose, lactose, raffinose or glucose. The D.C. electro-dialyzing voltage may be continuous, intermittent or pulsed. As shown, the solution is prepared at 20, clarified at 24 (e.g. in a centrifuge), electro-dialyzed at 30, and the product dried at 50 (e.g. by a spray drier). The electro-dialysis zone 30 comprises alternate anion and cation membranes 36, 38 separated by spacer means (not shown). Solution to be purified from CaCl 2 is supplied via line 26 and aqueous dilute CaCl 2 solution is supplied via lines 28 and 32. In operation, Ca and Cl ions pass from the phosphate solution into the CaCl ...

Process for preparing organic phosphates

Phosphates and phosphoramidates are prepared from organic hydroxy compounds and organic amino compounds respectively, by reacting these with organic tertiary phosphites, in the presence of a solvent, and an active methylene compound which is a bromo- or chloro-derivative of N-cyclohexyl cyanoacetamide, cyanoacetamide, malonamide, or a C1 to C4 alkyl cyanoacetate, in accordance with the following equations: (a) wherein R1 is alkyl or aralkyl; R2 and R3 are alkyl, aralkyl or aryl which may be substituted; R4 is an organic radical attached to the oxygen through a carbon atom; and X is -Cl or -Br, A is -CN or -CONH2, Y is -NH2, -NH-cyclohexyl, or OR7 and R7 is C1 to C4 alkyl; and (b) wherein R1, R2, R3, R4, X, A, and Y are as before; R5 is an organic group attached to the nitrogen through a carbon atom, and R6 is hydrogen, alkyl, aralkyl, or aryl. Typical phosphites are tri-alkyl phosphites, where alkyl is C1 to C4, tribenzyl phosphite, and monoethyl ...

USE OF FRUCTOSE-1,6-DIPHOSPHATE

NEW SALTS OF GLUCOSE-1-PHOSPHORIC ACID

... 1,208,270. N-containing organic base salts of glucose-1-phosphoric acid. SPA-SOC. PRODOTTI ANTIBIOTICI S.p.A. 29 Dec., 1967 [3 Jan., 1967], No. 332/67. Heading C2C. [Also in Division A5] Salts of glucose-1-phosphoric acid with mono-, di- or trialkylamines, mono-, di- or tri-(hydroxyalkyl)-amines and heterocyclic nitrogen bases which may be substituted by alkyl or hydroxyalkyl radicals and which may contain hetero atoms other than nitrogen, the alkyl radicals being C 1-4 and the mole ratio of acid to base in the salts being 1 : 1 or 1 : 2 are prepared by first contacting a metallic salt (e.g. Na, K, Ca salt) of glucose-1-phosphoric acid with a cation exchange resin to give the free acid which is then reacted with an appropriate base either as such or as a solution in water, an alcohol or an aqueous alcohol. Specified N-containing organic bases are trimethylamine, mono-, di- and triethylamine, n-butylamine, ethanolamine, triethanolamine, morpholine, pyrrolidine, piperazine and N-(#-hydroxyethyl ...

DERIVATIVES OF EBURNAMONINE

PROCEDURE FOR THE PRODUCTION OF NEW VINCAMONSALZEN

LPS WITH REDUCED TOXICITY OF GENETICALLY MODIFIED GRAM NEGATIVES BACTERIA

USE OF SACCHARIDE KONJUGATEN

PROCEDURE FOR THE CHEMICAL OR ENZYMATIC TRANSFORMATION OF A ALDOSE OR A ALDOSEDERIVATES IN AN APPROPRIATE KETOSE OR AN APPROPRIATE KETOSEDERIVAT

USE FROM FRUCTOSE-1,6-DIPHOSPHAT TO THE TREATMENT OF ACUTES ALCOHOLIC POISONING AND CHRONIC ALCOHOLISM AND USED PHARMACEUTICAL COMPOSITIONS.

2,3-DIAMINO-2,3-DIDESOXYHEXOSE-DERIVATE, PROCEDURE FOR YOUR PRODUCTION AND YOUR USE.

PHOSPHORYLATION MEANS, PROCEDURE FOR ITS PRODUCTION, PROCEDURE FOR THE PHOSPHORYLATION OF AN ORGANIC HYDROXYL OR AMINE CONNECTION.

PHARMACEUTI COMPOSITION

Procedure for the production of a dental care means

Immunogens for meningitidis-A vaccines

Mannose-6-phosphonate compounds for the treatment of inflammatory diseases

Antimicrobial and antiviral compounds and methods for their use

TREATMENT OF CONGENITAL DISORDERS OF GLYCOSYLATION (CDG) USING MANNOSE

Substrate analogs for murg, methods of making same and assays using same

EBURNAMONINE DERIVATIVE

PROCESS AND MATERIALS FOR PRODUCTION OF GLUCOSAMINE

The present invention relates to a method and materials for producing glucosamine by fermentation of a genetically modified microorganism. Included in the present invention are genetically modified microorganisms useful in the present method for producing glucosamine, as well as recombinant nucleic acid molecules and the proteins produced by such recombinant nucleic acid molecules.

NOVEL USES OF D-MANNOPYRANOSE DERIVATIVES

La présente invention est relative à l'utilisation du mannose-6-phosphate (M6P) et de certains de ses dérivés pour le contrôle de l'angiogenèse et la régénération ligamentaire et/ou la reconstruction de cartilage. Le M6P et certains de ses dérivés peuvent notamment être utilisés pour la préparation d'une composition pharmaceutique destinée à la régénération ligamentaire et/ou la reconstruction de cartilages.

CONVERSION OF ALDOSE TO KETOSE IN THE PRESENCE OF A COMPLEXING REAGENT

SYNTHESIS OF OLIGOSACCHARIDES, REAGENTS AND METHODS RELATED THERETO

One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.

IMMUNOSTIMULANT DRUG CONTAINING PHOSPHORYLATED OSE OR POLYOSE DERIVATIVES

INTRAOCULAR IRRIGATING SOLUTION

An intraocular irrigating solution, used during operation performed in the site inside the eyeball, which contains substance (I) and inhibits damage to intraocular tissues, and a method of preventing damage to intraocular tissues due to intraocular irrigating solutions by utilizing said solution. (I) ...

Procédé de préparation d'éthers phosphoriques des alcools polyvalents.

Verfahren zur Herstellung von Glucose-6-phosphat.

UTILISATION DE DERIVES ORGANOPHOSPHORES DANS LES BAINS SULFITIQUES POUR L'ELECTRODEPOSITION DE L'OR ET DES ALLIAGES D'OR.

Verfahren zur Herstellung von Laktose-phosphorsäureestern

Procedimento per la produzione di un nuovo estere fosfo-organico del saccarosio

Procédé de préparation d'un nouveau sel de l'acide glucose-1-phosphorique

Process for recovering calcium phosphate compositions from mixtures ob - td by phosphorylating sucrose

A mixt. of calcium sucrose phosphate and calcium phosphate is recovered from the aq. reaction liquors obtd. by phosphorylating sucrose by drying the liquors in such a manner as to obtain a finely divided powder, sepg. CaCl2 and sucrose by lixiviation with a suitable solvent and drying the lixiviated residue. The Ca-mixt. is used in the prevention of dental caries. The process is more economical than known processes involving removal of CaCl2 by pptn. methods. The product contains less than 0.5% CaCl2 and is non-deliquescent.

Verfahren zur Herstellung von 2-Alkyl-3-hydroxy-4,5-dihydrofuran-4-onen

Sugar diphosphates prepd from monophosphates

Prepn. of hexose-1, 6-& pentose-1, 5-diphosphates. As coenzymes. The sugar 5/6-monophosphate is acylated, pref. with Ac2O & opt. in the presence of a catalyst & solvent, volatiles removed in vacuo at 40-80 deg., & the residue heated in vacuo with excess (3-5 moles) of anhyd. ortho &/or pyrophosphoric acid at 50-80 deg. for 1-2 hr. The product is basified, pref. with MeOH-NaOH, to ppt. a mixt. of di- & monophosphates & inorg. salts. These are filtered or centrifuged, dissd. in hot water, the pH adjusted to 9.0 & the soln. cooled to 0 deg. to ppt. Na2HPO4.12H2O; the rest of the phosphate is removed as the Mg-NH4 salt. Starting material is sepd. by taking the filtrate to pH 7.5, boiling & adding Ba++ & filtering hot to recover the pptd. Ba salt of the product.

Verfahren zur Herstellung einer wasserlöslichen komplexen Assoziation

Cariostatic ca sugar-phosphate preparations

Oral cariostatic compns. in which the active principle is a complex comprising:- (a) one or more Ca sugar-phosphates; (b) an inorg. Ca phosphate such that (1) at least 2% of (b), based on the wt. of (a), is water-sol. under ambient conditions, (2) the total quantity of (a) and (b) dissolving > 5% of the wt. of water. Prefd. as (a) are Ca sucrose- and glucose- phosphates, and as (a + b) complexes the products (X), (Y) and (Z) below.

Procédé de fabrication de phosphate de glucose-6

Verfahren zur Herstellung von Phosphorsäureestern von Kohlehydraten und von mehrwertigen Alkoholen

Verfahren zur Herstellung eines kariostatisch wirkenden Gemisches

Inhibiting dental caries

... (A) The use of soluble, palatable, organic phosphate esters, or their salts, as cariostatic agents for inhibiting dental caries and tooth erosion. In partic., phosphate esters derived from polyhydric alcs., cyclitols, sugars, mono-, oligo- or poly-saccharides. Espec. favoured is Ca sucrose-phosphate, but the glucose, lactose, and glycerol cpds. are also spec. claimed, as well as the use of Na and Mg salts. (B) The incorporation of the prefd. cpd. in such products as:- foodstuffs (up to 6%), dentifrices, mouthwashes, lozenges and drinks. The ability to incorporate a palatable cariostatic agent into foods and drinks, i.e. in the presence possibly of cariogenic substs. such as carbohydrates, is an important point.

Prepn of phosphate esters of carbohydrates - sugar phosphorylation reaction solutions

Process (claimed) for the prepn. of phosphate esters (I) of sugars (II), in which solvent free POCl3 is added to a mixture of (II), H2O, and CaO, Ca(OH)2, or CaCO3 at 0-20 deg. Mixture is clarified (pref. by centrifugation, e.g. in Sharples super solid bowl centrifuge at 24,000 r.p.m. at feed rate 200-300 ml./min.), and supernatant is treated with EtOH, and pptd. (I) is counter-currently leached with EtOH (pref. is not ca 4 stages) to remove CaCl2. (I)- soln. is then spray dried to give pure Ca- (I). (II) may be galactose, arabinose, ribose, xylose, maltose, lactose, raffinose, and glucose etc., partic sucrose. Reaction may be effected with excess of Ca cpd., or pref. with stoichiometric amounts of reagents (mol. ratio II : Ca cpd.: POCl3 = 1:2.5:1). N.B. Original gives flow diagram of suitable process.

Procédé de fabrication de phosphate de glucose-1

Procédé de préparation d'un glucose-phosphate

PROCEDURE FOR THE CONVERSION OF ALDOSEN OR ALDOSE DERIVATIVES FOR KETOSEN OR KETOSE DERIVATIVES.

SUGAR PHOSPHATES AND PROCEDURES FOR YOUR PRODUCTION.

SACCHARIDES AND THESE CONTAINING THERAPEUTIC COMPOSITIONS.

Tieno[ 3.2-and-d]pirimidin, furo[ 3.2-and-d]pirimidin and pirrolo[ 3.2-and-d]pirimidiny, suitable for treatment of infections, caused by respiratory - syncytial virus

DERIVATIVES OF NIKOTINAMIDMONONUKLEOTIDA AND THEIR APPLICATION

Immunogens for meningitidis-a vaccines

An oligosaccharide useful for a Meningitidis A vaccine contains a first mannose unit having a spacer in the alpha configuration at C-1, which spacer is capable of conjugating to a protein, and which is connected to a second mannose unit through a 1,6-linkage which connects C-6 of the first unit to C-1 of the second unit, wherein the 1,6-linkage comprises a phosphonate. Related methods of making such compounds, analogous compounds, or intermediates thereof are also disclosed.

Halogenated dideoxy sugar derivative, preparation method and application thereof

SYNTHESIS OF MOLECULES OF THE TYPE INOSITOLPHOSPHATE GLYCANNE: TREATMENT DESTROUBLES OF THE CELLULAR PROLIFERATION AND DISORDERS METABOLIQUESCARACTERISES BY A RESISTANCE TO INSULIN

Compn. consisting of a complex assocn. of 2 components (a) and (b): (a) consists of is not 1 salt of a sugar phosphate, (b) consists of a phosphat

Method of preparation of organic pyrophosphates

CRYSTALLINE SALT OF RIBOSE-5-PHOSPHORIC ACID

PHOSPHATES DE SUCRE UTILISABLES DANS DES SHAMPOOINGS, RINCAGES ET COSMETIQUES, ET PROCEDE POUR LA PREPARATION DE CES PHOSPHATES

ON PREPARE UN PHOSPHATE DE SUCRE DE FORMULE GENERALE: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN RESTE A HYDROGENE ACTIF D'UN HEXOSE, ET R, R ET R SONT IDENTIQUES OU DIFFERENTS ET REPRESENTENT CHACUN UN GROUPEMENT HYDROCARBONE SATURE OU INSATURE AYANT DE 1 A 4 ATOMES DE CARBONE, EN FAISANT REAGIR UN MONOESTER PHOSPHORIQUE AVEC UN SEL DE GLYCIDYLTRIALKYLAMMONIUM. LES PHOSPHATES DE SUCRE SELON L'INVENTION POSSEDENT UNE BONNE RETENTION DE L'HUMIDITE ET UN BON POUVOIR ABSORBANT SUR LES CHEVEUX, ET ON PEUT LES UTILISER DANS DES SHAMPOOINGS, DES RINCAGES ET DES COSMETIQUES.

GOLD SULFITE BATHS CONTAINING ORGANOPHOSPHORUS COMPOUNDS

PROCESS FOR PREPARING GLUCOSE-1-PHOSPHATE

New saccharide or sugar alcohol derivatives containing O-ortho-salicyloyl group and O-n-alkanoyl group, useful for treating or preventing enterocolitis or intestinal adeno-carcinoma

La présente invention concerne des dérivés de saccharides et d'itols possédant un groupement O-n-alcanoyle et un groupement O-ortho-acétylsalicyloyle et leurs applications comme additifs alimentaires ou médicaments dans le traitement des entérocolites d'étiologies multiples et les adéno-carcinomes intestinaux chez l'Homme et l'animal. L'un des buts de la présente invention est de fournir de nouveaux composés, dérivés de saccharides et d'itols, répondant à la formule générale I : dans laquelle le substrat Sub représente un dérivé saccharidique, R1C(O) représente le groupement ortho-acétlylsalicyloyle, R2C(O) représente un groupement n-alcanoyle dans lequel R2 est un groupement n-alkyle contenant 1 à 17 atomes de carbone, et de préference butyle ; Un autre but de la présente invention est l'utilisation de ces dérivés comme composés pour la préparation d'additifs alimentaires ou de médicaments, notamment dans le traitement d'entérocolites d'étiologies multiples et les adénocarcinomes intestinaux ...

FERRIC SALT OF THE FRUCTOSE-DIPHOSPHATE-1,6, PROCEEDED FOR ITS OBTAINING AND ITS USE IN THE PREPARATION OF ACID FRUCTOSE-DIPHOSPHORIQUE-1,6

DERIVES FROM STABLE ACID L-ASCORBIQUE IN WATER, PROCEEDED FOR SA PREPARATION AND COSMETIC COMPOSITION OF BLEACHING OF the SKIN the CONTAINER

Il est décrit dans ici un dérivé de l'acide L-ascorbique ayant une stabilité dans l'eau améliorée, représenté par la formule générale (I) suivante : (CF DESSIN DANS BOPI) et un procédé pour sa préparation, ainsi qu'une composition cosmétique de blanchiment de la peau contenant ce dérivé comme principe actif.

FERROUS FRUCTOSE-1,6-DIPHOSPHATE, USE, COMPOSITION AND PROCESS FOR THE OBTAINMENT THEREOF

The present invention relates to ferrous fructose-1,6-diphosphate dihydrate, use, composition and a process for the obtainment thereof. The compound of the invention shows a very high Fe2+ titre and an excellent stability in time and is useful for the preparation of a food supplement and/or a medicament for the prevention and/or the treatment of dietetic and/or morbid iron deficiency, in particular of dietary anemia, sideropenia, anemia.

PROCESSES FOR THE PRODUCTION OF AMINOALKYL GLUCOSAMINIDE PHOSPHATE AND DISACCHARIDE IMMUNOEFFECTORS, AND INTERMEDIATES THEREFOR

This invention relates to processes for production of alkylamino glucosaminide phosphate compounds, and of disaccharide compounds, including various novel intermediates and intermediate processes. In one aspect, glycosyl halides are produced by reaction of an O-silyl glycoside with a dihalomethyl alkyl ether.

CERTAIN AMINOALKYL GLUCOSAMINIDE PHOSPHATE COMPOUNDS AND THEIR USE

Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

MOENOMYCIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF

The present invention provides novel moenomycin analogs as well as pharmaceutical compositions thereof, methods of synthesis, and methods of use in treating an infection by administering an inventive compound to a subject in need thereof. The moenomycin analogs may be prepared synthetically, biosynthetically, or semi-synthetically. The analogs are particularly useful in treating or preventing infections caused by Gram-positive organisms. Certain inventive compounds may have a broader spectrum of coverage, which includes Gram-negative organisms.

Use of fructose-1,6-diphosphate for treating myocardial infarction

The invention relates to methods of treatment of patients with heat disorders using fructose-1,6-diphosphate.

PROCESS FOR PREPARING WATER-SOLUBLE SUGAR PHOSPHATE COMPLEXES

SYSTEM AND METHOD FOR QUICK RELEASE

Release assembly for a personal equipment carrier. Release assembly includes securing component, a plurality of first cable assemblies, a plurality of attachment assembly first portions, trigger termination, and trigger activator. Securing component is attachable to a personal equipment carrier. The first cable assemblies, include an outer member and an inner member. A first end of each first cable assembly outer member is anchored to the securing component. Each attachment assembly first portion includes a detachment portion. The detachment portion is attached to a second end of each first cable assembly inner member. The detachment portion is operable, upon tensioning of the attached first cable assembly inner member, for detaching the attachment assembly first portion from an attached attachment assembly second portion. The trigger termination is connected to the first end of each first cable assembly inner member at the securing component. The trigger activator is connected to the trigger ...

Lipid A mimics, methods of preparation, and uses thereof

The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics.

HOMOGENOUS WATER-FREE FORMULATIONS CONTAINING GLYCEROPHOSPHOLIPIDS AND POLAR OR LIPOPHILIC SUBSTANCES, METHOD FOR THE PRODUCTION THEREOF

The invention relates to homogenous, water-free formulations which contain glycerophospholipids and polar or lipophilic substances (e.g. physiological active substances) as constituents in a molar ratio of 1:0.001 to 1:2, in addition to optionally water-free formulations agents, e.g. in the form of glycerin, in a molar ratio of 1:0.001 to 1:1 in relation to glycerophospholipids and which form stable aggregates so that the formulations for the preparation of dispersion emulsions and/or suspensions are most suitable for numerous areas of application, e.g. in food technology, biotechnology or in the pharmaceutical industry. The production of said formulations is carried out with compressed hydrocarbons in an extraction column, whereupon the formulations are obtained in the form of melts.

Novel phosphobetaine and detergent and cosmetic containing the same

LIQUID PREPARATION FOR INTRAOCULAR PERFUSION

Compounds having cardiotrophic activity, a process for the preparation thereof and pharmaceutical compositions therefrom

PRODUCTION OF TUMOR-INHIBITING SACCHARIDE CONJUGATE AND ITS USE

PROBLEM TO BE SOLVED: To obtain the subject tumor-inhibiting saccharide conjugate having a large medicinal activity and reduced toxicity, and useful as an anti-tumor medicine against tumors such as breast cancer, Hodgkin's disease and tumors in gastrointestinal tracts by conjugating a protected brominated sugar with each phosphorous compound and subsequently removing the protecting group. SOLUTION: This method for producing the glycoconjugate of phosphoric acid amide mustard or ifosfamide mustard having formula I [the sugar moiety is a mono-, di- or polysaccharide in any existing isomeric or enantiomeric form, linked to the phosphoric acid amide mustard residue or to the ifosfamide mustard residue; R1 and R2 are each H, a 1-4C(halogeno)alkyl or the like] or formula II and useful as an anti-tumor agent, etc., comprises reacting a 1-O-methyl- pyranoside such as glucose, galactose or mannose with benzyl chloride, removing the 1-methyl group, brominating the product, conjugating the obtained ...

Patent RU2015129468A3

ВИ“? 2015129468” АЗ Дата публикации: 21.01.2019 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2015129468/04(045519) 04.06.2010 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [Х] приоритета 22.12.2011 по первоначальной заявке № 2011152602 из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 61/184,703 05.06.2009 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СИНТЕТИЧЕСКИЕ ГЛЮКОПИРАНОЗИЛЛИПИДНЫЕ АДЪЮВАНТЫ Заявитель: ИНФЕКШЕС ДИЗИЗ РИСЕРЧ ИНСТИТЬЮТ, 05 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 31/7024 (2006.01) С07Н 11/04 (2006.01) Аб1Р 37/02 (2006.01) Аб/1К 31/7028 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1К 31/7024 СО7Н 11/04 АбТР 37/02 Аб1К 31/7028 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): СТРО, РЕРАТБ пес, РУУРТ, ЕАРАТТУ, Езрасепеё, Соое Раеп, /-Р]а( Ра, РАТЕМТЬСОРЕ, Ра еагсЬ, КОРТО, ТРО, Заепсе Оиесё, ОЗРТО 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ...

ГИПЕРСУЛЬФАТИРОВАННЫЕ ГЛЮКОПИРАНОЗИДЫ

1. Фармацевтический состав, подходящий для лечения легочного заболевания или состояния, содержащий соединение формулы I и его фармацевтически приемлемые соли,где R-Rнезависимо выбраны из группы, состоящей из H, SOH или POH, при условии, что по меньшей мере два из R-Rвыбраны из SOH или POH; идобавку, выбранную из группы, состоящей из фармацевтически приемлемого наполнителя или агента для доставки.2. Состав по п.1, отличающийся тем, что по меньшей мере три из R-Rвыбраны из SOH или POH.3. Состав по п.1, отличающийся тем, что по меньшей мере четыре из R-Rвыбраны из SOH или POH.4. Состав по п.1, отличающийся тем, что по меньшей мере пять из R-Rвыбраны из SOH или POH.5. Состав по п.1, отличающийся тем, что R-Rвыбран из SOH.6. Фармацевтический состав, содержащий соединение формулы II и его фармацевтически приемлемые солигде R-Rвыбраны из -SOH, и добавку, выбранную из группы, состоящей из фармацевтически приемлемого наполнителя или полимера.7. Фармацевтический состав по п.6, содержащий соединение формулы II и его фармацевтически приемлемые соли, где фармацевтически приемлемая соль представляет собой натриевую соль.8. Состав по п.7, отличающийся тем, что фармацевтически приемлемый полимер представляет собой гидрофильный полимер.9. Состав по п.8, отличающийся тем, что гидрофильный полимер выбран из поперечно-сшитого полимера акриловой кислоты.10. Состав по п.9, отличающийся тем, что поперечно-сшитый полимер акриловой кислоты выбран из карбопола 934Р (Carbopol 934Р).11. Способ лечения или облегчения воспалительного состояния у млекопитающего, нуждающегося в таком лечении, включающий введение(i) фармацевтически эффективного количества состава, содержащего соединение формулы I или РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A01N 43/16 (13) 2012 140 396 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2012140396/13, 30.03.2011 (71) Заявитель(и): ОПКО ХЕЛС, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы ...

PHOSPHATE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS OF THE SAME

Phosphorus-containing polyols

... 1,127,907. Phosphorus-containing sucrose polyols. MARLES - KUHLMANN - WYANDOTTE. 29 Dec., 1965 [30 Dec., 1964], No. 55059/65. Heading C2C. [Also in Division C3] Phosphorus-containing sucrose polyols are obtained by reacting an oxy-acid of phosphorus with sucrose in the presence of a diluent at a temperature between 0‹ and 50‹ C. and thereafter contacting the sucrose-acid reaction mixture at a temperature between 20‹ and 100‹ C. with an alkylene oxide in such an amount that the resulting phosphorus-containing sucrose polyol is substantially neutral. Specified phosphorus acids are phosphoric acids (85%, 100%, 105% and 115%), phosphorous acid, phosphonic acids, phosphonous acid, phosphinic acids, phosphinous acid, and partial esters of phosphoric, phosphorous, phosphonic and phosphonous acids, and specified diluents, which diluents may also be present during the second step of the process, are water, organic esters, ketones, ethers, aliphatic nitriles, polyhalogenated aliphatic hydrocarbons ...

4-0-phosphono-glycosides

Compounds of formula I wherein R1 represents a sugar residue X and Y are the same or different and stand for oxygen or the imino group, and R2 and R3 are the same or different and represent an optionally substituted acyl group, which process i.a. immuno-modulatory activity.

PROCESS FOR PREPARING GLUCOSE-1-PHOSPHATE

... 1321076 Preparing glucose 1-phosphate HAYASHIBARA CO 23 June 1970 [24 June 1969] 30442/70 Heading C2P Glucose-1-phosphate is obtained by decomposing a raw material selected from glycogen, starch, liquefied starch and soluble starch with 1,6-glucosidase and reacting the decomposed products with phosphorylase. The decomposition and phosphorylation may be carried out simultaneously and the 1,6-glucosidase may be added to the reaction mixture during the phosphorylation of the raw material. The 1,6- glucosidase is suitably produced by culturing at least one strain chosen from the genera Pseudomonas, Escheriohia, Aerobacter, Nocardia, Streptomyces, Actinomyces, Micromonospora, Thermonospora and hactobacillus and several suitable strains of these and other genera are specified. The reaction mixture is suitably worked up to yield the product in the form of its crystalline dipotassium salt ...

Purification of fructose-2 6-diphosphate

A process for the purification and isolation of fructose-2,6-diphosphate produced by cyclization of fructose-1,6-diphosphate and alkaline hydrolysis involves two chromatography steps, treatment with a cationic exchange resin and lyophilisation. Pharmaceutical compositions containing fructose-2,6-diphosphate and a liposome stabiliser are also described.

SALTS OF AMINO GLYCOSIDES

LIPID A MORE SIMILARLY AND YOUR IMMUNOAKTIVIERENDE AND ANTI-TUMOR EFFECT

Procedure for the production of Hexose-1,6-bzw. Pentose-1,5-diphosphaten

Method for Preventing Cancer Metastasis

The present invention relates to the use of a specific family of glycerolipid compounds of formula (I) described in the detailed description or the manufacture of a medicament for the prevention or for the treatment of cancer metastasis.

HEPATITIS C THERAPIES

The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections. 2. The compound of wherein R is OR claim 1 , Cl claim 1 , SR claim 1 , NRR claim 1 , aryl or NRNRR.3. The compound of wherein R is hydroxy claim 1 , chloro claim 1 , methoxy claim 1 , mercapto claim 1 , methylthio claim 1 , methylamino claim 1 , isopropylamino claim 1 , propylamino claim 1 , ethylamino claim 1 , dimethylamino claim 1 , cyclopropylamino claim 1 , 2-aminoethylamino claim 1 , 1-(2-hydroxyethyl)hydrazino claim 1 , hydrazino claim 1 , 1-methylhydrazino claim 1 , azetidino claim 1 , pyrrolidino claim 1 , imidazolylpropylamino claim 1 , pyrrolino claim 1 , morpholino claim 1 , piperazino claim 1 , hydroxyethylamino claim 1 , bis-hydroxyethylamino claim 1 , hydroxypropylamino claim 1 , hydroxyethylpyrrolidino claim 1 , or 1-methyl-2-hydroxyethylamino.4. The compound of wherein R is NRR.6. The compound of which is a prodrug.7. The compound of that comprises one or more mono- claim 1 , di- claim 1 , or tri-phosphate groups.8. The compound of that comprises one or more mono-phosphate groups.9. The compound of wherein the compound is a prodrug.10. The compound of wherein one or more phosphorous atoms of the one or more pendent mono- claim 7 , di- claim 7 , or tri-phosphate groups is bonded to one or more alkoxy or aryloxy groups.11. The compound of wherein one or more phosphorous atoms of the pendent mono- claim 7 , di- claim 7 , or tri-phosphate groups is bonded to one or more groups R—O—; wherein each Ris independently a 1-20 carbon branched or unbranched claim 7 , saturated or unsaturated chain claim 7 , wherein one or more of the carbon atoms is optionally replaced with —O— or —S— and wherein one or more of the carbon atoms is optionally substituted with oxo (═O) or thioxo (═S).12. The compound of wherein one or more phosphorous atoms of the one or more pendent mono- claim ...

NOVEL GLYCOSYL PHOSPHITES

The present invention relates to providing compounds of general formula 1 2. The compound according to claim 1 , wherein A is a protected sialyl or fucosyl moiety claim 1 , and R is optionally substituted aryl.5. A method for producing a compound of general formula 1 as defined in claim 1 , characterized in that a compound of formula A-OH claim 1 , wherein A means a protected glycosyl residue of a mono- claim 1 , di- or oligosaccharide is{'sub': '2', 'a) reacted with a compound (RO)PY wherein R is selected from optionally substituted aryl and optionally substituted heteroaryl, and Y is selected from halogen and dialkylamino, or'}{'sub': '3', 'b) reacted with a compound PXwherein X is halogen, followed by reaction with an alcohol ROH wherein R is defined as above.'}6. The method according to claim 5 , wherein the compound of A-OH is N-acetyl neuraminic acid tetraacetate methyl ester or 2-O-benzyl-3 claim 5 ,4-di-O-(optionally substituted acyl)-L-fucose claim 5 , PXis PCl claim 5 , and the alcohol ROH is phenol optionally substituted with alkyl claim 5 , alkoxy and/or halogen claim 5 , preferably methyl claim 5 , methoxy and/or bromo.7. A process for the synthesis of an oligosaccharide claim 1 , characterized in that the said synthesis comprises at least the step of: coupling a compound of general formula 1 as defined in with an acceptor of the formula B—OH claim 1 , wherein B—OH means a protected mono- claim 1 , di- or oligosaccharide.10. The process according to for the synthesis of a sialylated or fucosylated human milk oligosaccharide claim 1 , wherein a compound of general formula 3A or 3B as defined in is coupled with an acceptor of the formula C—OH claim 1 , wherein C—OH means a protected desialo- or defuco-human milk oligosaccharide claim 1 , followed by deprotection to give the sialylated or fucosylated human milk oligosaccharide.11. The process according to claim 10 , wherein the sialylated or fucosylated human milk oligosaccharide is selected from 6′- ...

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

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.

IMMUNOTHERAPEUTIC POTENTIAL OF MODIFIED LIPOOLIGOSACCHARIDES/LIPID A

Embodiments of the disclosure provide for unique lipooligosaccharide/lipid A-based mimetics for use as adjuvants. Methods of generating lipooligosaccharide/lipid A-based mimetics are provided that utilize recombinantly engineered bacteria to produce the mimetics, including, for example, addition of one or more particular enzymes such as acyltransferases, deacylases, phosphatases, or glycosyltransferases. 1. A method of generating a lipooligosaccharide/lipid A-based mimetic , comprising the steps of: expresses one or more non-endogenous lipid A biosynthesis enzymes;', 'expresses one or more endogenous lipid biosynthesis enzymes, wherein the enzyme is modified; and/or', 'has modified regulation of one or more endogenous lipid biosynthesis enzymes; and, 'obtaining a bacterial strain that has one or more of the following modificationssubjecting the strain to conditions suitable for production of the lipooligosaccharide/lipid A composition.2. The method of claim 1 , wherein the obtaining step is further defined as engineering the bacterial strain to have one or more of the modifications.3. The method of claim 2 , wherein the engineering step comprises one or both of:delivering a vector into the bacteria; orbacterial conjugation.4. The method of claim 2 , wherein the engineering step comprises delivering a vector into the bacteria claim 2 , wherein the vector comprises sequence that encodes one or more non-endogenous lipid A biosynthesis enzymes.5. The method of claim 1 , wherein the lipooligosaccharide/lipid A-based mimetic produced by the method has a modified number of phosphates compared to the endogenous bacterial lipid A molecule or a reference lipid A molecule.6. The method of claim 1 , wherein the lipooligosaccharide/lipid A-based mimetic produced by the method has modified phosphates compared to the endogenous bacterial lipid A molecule or a reference lipid A molecule.7Yersinia pestis, Pseudomonas. The method of claim 1 , wherein the bacterial strain is claim 1 , ...

LIPID A MIMICS, METHODS OF PREPARATION, AND USES THEREOF

The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics. 24-. (canceled)7. (canceled)10. The compound of claim 8 , or pharmaceutically acceptable salt thereof claim 8 , wherein Xis —OP(O)(OH); Yis —NH—R; and Yis —O—R.14. The compound of claim 13 , or pharmaceutically acceptable salt thereof claim 13 , wherein Xis —OP(O)(OH); Yis —NH—R; Yis —O—R; and Yis —OH.16. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein D is —O—.17. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein at least one of A or Land at least one of E or Lindividually comprises one or more lipid chain substituents.26. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , which:has lipid A or lipopolysaccharide (LPS) antagonist activity;has immunostimulatory activity; and/oris capable of binding to toll-like receptor 4 (TLR4).27. (canceled)28. A pharmaceutical composition comprising the compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier claim 1 , diluent or excipient.29. (canceled)30. A vaccine composition comprising the ...

Modification of trehalose-6-phosphate levels in plants

Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.

PHARMACEUTICAL COMPOSITION FOR USE IN INHIBITING RECURRENCE, AGGRAVATION AND METASTASIS OF HEPATOCARCINOMA

The present application provides a pharmaceutical composition for use in inhibiting recurrence, aggravation or metastasis of liver cancer, in which the pharmaceutical composition comprises at least one compound having a structure of formula (I) and a pharmaceutically acceptable vehicle. 2. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having 3n+7 of the R groups as SOH is the primary constituent.3. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n equal to 2 or 3 and 3n+7 of the R groups as SOH is the primary constituent.4. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n equal to 3 and 3n+7 of the R groups as SOH has the highest relative content.5. The pharmaceutical composition of claims 1 , wherein the therapeutically effective amount is between 80 mg to 315 mg per day.6. The pharmaceutical composition of claim 5 , wherein the therapeutically effective amount is 160 mg per day.7. A method for inhibiting recurrence claim 1 , aggravation and/or metastasis of liver cancer claim 1 , comprising administering to a patient in need thereof the pharmaceutical composition of .8. The method of claim 7 , wherein the administration step is performed after liver surgical resection.9. A method of inhibiting recurrence claim 2 , aggravation and/or metastasis of liver cancer claim 2 , comprising administering to a patient in need thereof the pharmaceutical composition of .10. A method of inhibiting recurrence claim 3 , aggravation and/or metastasis of liver cancer claim 3 , comprising administering to a patient in need thereof the pharmaceutical composition of .11. A method of inhibiting recurrence claim 4 , aggravation and/or metastasis of liver cancer claim 4 , comprising administering to a patient in need thereof the pharmaceutical composition of .12. A method of inhibiting recurrence claim 5 , aggravation and/or metastasis of liver cancer claim 5 , comprising ...

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 15-. (canceled)717-. (canceled)21. A compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris F or OH.2328-. (canceled)31. A pharmaceutical composition comprising a compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , and a pharmaceutically acceptable carrier or excipient.32. A pharmaceutical composition comprising a compound of claim 22 , or a pharmaceutically acceptable salt thereof claim 22 , and a pharmaceutically acceptable carrier or excipient.33. A pharmaceutical composition comprising a compound of claim 29 , or a pharmaceutically acceptable salt thereof claim 29 , and a pharmaceutically acceptable carrier or excipient.34. A pharmaceutical composition comprising a compound of claim 30 , or a pharmaceutically acceptable salt thereof claim 30 , and a pharmaceutically acceptable carrier or excipient.35. A method of treating Pneumovirinae virus infection in a human in need thereof claim 6 , the method comprising administering to the human in need thereof a therapeutically effective amount of a compound of claim 6 , or a pharmaceutically acceptable salt thereof.36. The method of claim 35 , wherein the Pneumovirinae virus infection is a respiratory syncytial virus infection.37. A method of treating Pneumovirinae virus infection in a human in need thereof claim 22 , the method comprising administering to the human in need thereof a therapeutically effective amount of a compound of claim 22 , or a pharmaceutically acceptable salt thereof.38. The method of claim 37 , wherein the Pneumovirinae virus infection ...

POLYPHOSPHATE AND PYROPHOSPHATE DERIVATIVE OF SACCHARIDES

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 claim 2 , 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 claim 1 , wherein the compound comprises from 2 to about 10 phosphate or polyphosphate groups or pyrophosphate groups.6. (canceled)7. (canceled)8. The pharmaceutical composition of claim 1 , wherein the pyranose further comprises a derivatized hydroxyl selected from alkoxy (—OR) or acyloxy (—OCOR) claim 1 , where R is selected from alkyl claim 1 , aryl claim 1 , acyl claim 1 , aralkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , heterocyclyl claim 1 , polycyclyl claim 1 , carbocycle claim 1 , amino claim 1 , acylamino claim 1 , amido claim 1 , alkylthio claim 1 , carbonyl claim 1 , sulfonate claim 1 , alkoxyl claim 1 , sulfonyl claim 1 , or sulfoxido.9. (canceled)10. (canceled)11. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)24. (canceled)25. (canceled)26. (canceled)27. (canceled)28. The compound according to claim 12 , ...

LPS EXTRACTION PROCESS

A method of lipopolysaccharide (LPS) extraction from gram negative bacterial cells is provided, said method comprising a step of extracting LPS from the gram negative bacterial cell in a LPS extraction solution comprising a salt, water, an alcohol, and a further organic solvent. Compositions and uses of the extracted LPS are also provided. 2. Use of the LPS extraction solution of for extracting LPS from gram negative bacterial cells claim 1 , wherein the volume of said LPS extraction solution is equal to or greater than a volume selected from the group consisting of: 0.1 claim 1 , 0.2 claim 1 , 0.3 claim 1 , 0.4 claim 1 , 0.5 claim 1 , 0.6 claim 1 , 0.7 claim 1 , 0.8 claim 1 , 0.9 claim 1 , 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 10 claim 1 , 15 claim 1 , and 20 L.3. A method of LPS extraction from gram negative bacterial cells comprising a step of extracting LPS from the gram negative bacterial cells using the extraction solution of claim 1 , wherein the volume of said LPS extraction solution is equal to or greater than a volume selected from the group consisting of: 0.1 claim 1 , 0.2 claim 1 , 0.3 claim 1 , 0.4 claim 1 , 0.5 claim 1 , 0.6 claim 1 , 0.7 claim 1 , 0.8 claim 1 , 0.9 claim 1 , 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 10 claim 1 , 15 claim 1 , and 20 L.4. The LPS extraction solution of claim 1 , wherein the salt is NaOAc.5. The LPS extraction solution of claim 1 , wherein the salt concentration is greater than or equal to 2 mM and less than or equal to 30 mM.6. The LPS extraction solution of claim 1 , wherein the further organic solvent is chloroform.7. The LPS extraction solution of wherein the amount of water in the LPS extraction solution is greater than or equal to 0.1% (v/v) and less than or equal to 3% (v/v).8. The LPS extraction solution of wherein the alcohol is methanol.9. A method of LPS extraction from gram negative bacterial cells comprising the steps:(i) washing gram negative bacterial cells with a ...

LIPID A MIMICS, METHODS OF PREPARATION, AND USES THEREOF

The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics. 1. A compound of formula:{'br': None, 'sub': 1', '2, 'A-L-D-L-E'}wherein:A is a cyclic monosaccharide residue with one or more of the hydroxyl groups optionally substituted or absent, or A is a substituted or unsubstituted aromatic group;{'sub': 1', '2, 'Land Lindependently are present or absent, and if present is independently a substituted or unsubstituted, branched or linear, saturated or unsaturated, carbon chain optionally comprising one or more of O, S or N;'}D is —O—, —S— or —NH—; andE is a cyclic monosaccharide residue with one or more of the hydroxyl groups optionally substituted or absent, or E is a substituted or unsubstituted aromatic group;{'sub': 1', '2, 'wherein at least one of A or E is a substituted or unsubstituted aromatic group and at least one of A, L, Lor E comprises one or more lipid chain substituents;'}or a pharmaceutically acceptable salt thereof.3. The compound of or , or pharmaceutically acceptable salt thereof , wherein at least one of A or E is a substituted or unsubstituted monocyclic carbocyclic aromatic group or a substituted or unsubstituted monocyclic ...

Synthetic Antigen Constructs Against Campylobacter Jejuni

The invention relates to immunogenic synthetic constructs capable of inducing an immune response against Campylobacter jejuni ( C. jejuni ) in a subject comprising one or more monosaccharides comprising one or more MeOPN moieties. Specifically, the invention relates to immunogenic synthetic constructs capable of inducing an immune response against Campylobacter jejuni ( C. jejuni ) in a subject comprising one or more MeOPN→6 Gal monosaccharides. The invention also relates to compositions comprising the immunogenic synthetic constructs and methods of inducing an immune response against C. jejuni in a subject comprising administering the immunogenic synthetic constructs, and/or compositions comprising the immunogenic synthetic construct, to the subject.

METHODS FOR INTRODUCING MANNOSE 6-PHOSPHATE AND OTHER OLIGOSACCHARIDES ONTO GLYCOPROTEINS AND ITS APPLICATION THEREOF

Methods to introduce highly phosphorylated mannopyranosyl oligosaccharide derivatives containing mannose-6-phosphate (M6P), or other oligosaccharides bearing other terminal hexoses, to carbonyl groups on oxidized glycans of glycoproteins while retaining their biological activity are described. The methods are useful for modifying glycoproteins, including those produced by recombinant protein expression systems, to increase uptake by cell surface receptor-mediated mechanisms, thus improving their therapeutic efficacy in a variety of applications. 1: A method for coupling a highly phosphorylated mannopyranosyl oligosaccharide compound to a glycoprotein having at least one glycan , or to chemical compounds with a carbonyl group , said method comprising:derivatizing the highly phosphorylated mannopyranosyl oligosaccharide compound with a chemical compound containing a carbonyl-reactive group;oxidizing the glycoprotein having at least one glycan to generate at least one carbonyl (aldehyde) group on the glycoprotein; andreacting the oxidized glycoprotein having at least one glycan, or a chemical compound with a carbonyl group, with the derivatized highly phosphorylated mannopyranosyl oligosaccharide compound to form a new compound having a hydrazone bond.231-. (canceled)32: A modified acid α-glucosidase composition comprising an acid α-glucosidase and a bis-M6P oligomannose , wherein the acid α-glucosidase and the bis-M6P oligomannose are linked by a hydrazone bond.33: A method of coupling an alpha-N-acetylglucosaminidase to an oligosaccharide comprising a phosphorylated mannose , comprising:(a) derivatizing an oligosaccharide comprising a phosphorylated mannose with a compound containing a carbonyl-reactive group;(b) oxidizing an alpha-N-acetylglucosaminidase having at least one oligosaccharide to generate at least one carbonyl group on the at least one oligosaccharide of the alpha-N-acetylglucosaminidase; and(c) reacting the derivatized oligosaccharide with the oxidized ...

Synthetic Antigen Constructs Against Campylobacter Jejuni

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

Nicotinamide mononucleotide derivatives and their uses

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 14-. (canceled)6. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris Cl.7. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris NH.8. (canceled)9. The compound of claim 5 , or the pharmaceutical acceptable salt thereof wherein Ris H.10. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris H.11. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris F.12. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris F.13. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris Cl.14. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris N.15. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of CN and N.16. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of methyl claim 5 , ethyl claim 5 , and propyl.17. The compound of claim 5 , or the pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of CHF claim 5 , CHF claim 5 , and CHCl.23. A method of treating a Pneumoviridae virus infection in a human in need thereof claim 5 , the method comprising administering to the human a therapeutically effective amount of the compound of claim 5 , or the pharmaceutically acceptable salt thereof. ...

PHARMACEUTICAL COMPOSITION FOR USE IN INHIBITING RECURRENCE, AGGRAVATION AND METASTASIS OF HEPATOCARCINOMA

The present application provides a pharmaceutical composition for use in inhibiting recurrence, aggravation or metastasis of liver cancer, in which the pharmaceutical composition comprises at least one compound having a structure of formula (I) and a pharmaceutically acceptable vehicle. 2. The pharmaceutical composition of claim 1 , wherein the ratio of the compound of formula (I) having n=2 to the compound of formula (I) having n=3 is greater than 0.75 and less than 1.3. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n=2 accounts for at least 35% of the pharmaceutical composition.4. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n=2 accounts for 35%˜40% of the pharmaceutical composition.5. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n=1 accounts for at least 5% of the pharmaceutical composition.6. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n=1 accounts for 5%˜10% of the pharmaceutical composition.7. The pharmaceutical composition of claim 1 , wherein the compound of formula (I) having n=2 and the compound of formula (I) having n=3 with 3n+7 of the R groups being SOH account for at least 80% of the pharmaceutical composition.8. The pharmaceutical composition of claim 1 , wherein the therapeutically effective amount is between 80 mg to 315 mg per day.9. The pharmaceutical composition of claim 1 , wherein the therapeutically effective amount is between 80 mg to 160 mg per day.10. The pharmaceutical composition of claim 1 , wherein the therapeutically effective amount is 160 mg per day.11. A method for inhibiting recurrence claim 1 , aggravation and/or metastasis of liver cancer claim 1 , comprising administering to a patient in need thereof the pharmaceutical composition of .12. The method of claim 11 , further comprising:administering to the patient at least one additional therapy for inhibiting ...

METHOD FOR PREPARING PHOSPHORYLATED KETO POLYOLS, DERIVATIVES THEREOF AND USES THEREOF

The present invention relates to a method for preparing phosphorylated keto polyols by biocatalysis and uses thereof. 118-. (canceled)20. The method of claim 19 , wherein the ketone of formula (III) is characterized in that:{'sup': 1', '2, 'sub': 2', 'p', '2', '1', '10', '1', '3', '1', '3, 'claim-text': [{'sub': 1', '6', '1', '6, 'Ph is a phenyl optionally substituted by one or several substituents selected from halogens, —OH, C-Calkyl, and C-Calkoxy,'}, 'p is an integer from 1 to 6, and', {'sub': 1', '6', '1', '3', '1', '3, 'R is a C-Calkyl optionally substituted by one or several substituents selected from halogens, —OH, C-Calkyl, and C-Calkoxy, or'}], 'Rand Rare independently selected from the group consisting of —(CH)-Ph, —COOH, —C(═O)—R, —CH—C(═O)—R, —C(═O)OR, and C-C, optionally substituted with at least one group selected from —OH, C-Calkoxy, C-Calkyl, —F, —Cl, —Br, —I, wherein{'sup': 1', '2, 'sub': 5', '6', '3, 'Rand Rform together, with the carbonyl group, a C-Cring bearing at least one group selected from —OH, —OCH, —F, —Cl, —Br, —I, at position alpha of the carbonyl group or a second oxo group at position alpha or beta of the carbonyl group.'}21. The method of claim 19 , wherein the ketone of formula (III) is such that:{'sup': 1', '2, 'sub': 2', 'p', '2', '1', '3', '1', '6', '3, 'Rand Rare independently selected from the group consisting of —(CH)-Ph, wherein Ph is a phenyl, and p is 1 or 2; COOH; —CH—C(═O)—R, —C(═O)—R wherein R is a C-Calkyl; C-Calkyl optionally substituted with at least one group selected from —OH, —OCHand —Cl, or'}{'sup': 1', '2, 'sub': 6', '3, 'Rand Rform together, with the carbonyl group, a Cring bearing at least one group selected from —OH, —OCH, and —Cl at position alpha of the carbonyl group or bearing a second oxo group at position alpha or beta of the carbonyl group.'}23. The method of claim 22 , wherein:{'sub': 3', '3, 'X is selected from —OH, —OCH, a halogen, and C(═O)CH,'}{'sup': 1', '5, 'sub': 1', '6', '1', '6', '1', '3', '1 ...

Clostridium difficile lipoteichoic acid and uses thereof

A novel lipoteichoic acid (LTA) was isolated from C. difficile , the structure of which is illustrated below wherein n is an integer between 1 and 20, R3 and R4 are independently selected from C 14:0, C 16:0, C 16:1, C 18:0 or C18:1 fatty acid or any combination thereof wherein one of COR3 or COR4 may be replaced by H. Further described are conjugates comprising the novel LTA and vaccines produced using the isolated LTA and the LTA conjugates. The invention also encompasses methods of conferring immunity against C. difficile comprising administering a vaccine of the invention, and methods of detecting C. difficile using the isolated LTA of the invention.

GLA MONOTHERAPY FOR USE IN CANCER TREATMENT

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen. 2. The method of wherein R claim 1 , R claim 1 , Rand Rare undecyl and Rand Rare tridecyl.3. The method of any of or wherein the mammal is human.43. The method of any of - claims 1 , wherein the composition is an aqueous formulation.53. The method of any of - claims 1 , wherein the composition is in the form of an oil-in-water emulsion claims 1 , a water-in-oil emulsion claims 1 , liposome claims 1 , micellar formulation claims 1 , or a microparticle.65. The method of any of - claims 1 , wherein the cancer comprises a solid tumor.7. The method of claim 6 , wherein the solid tumor is a carcinoma claim 6 , a sarcoma or a lymphoma.8. The method of claim 6 , wherein the solid tumor is a primary solid tumor.9. The method of claim 6 , wherein the solid tumor is a secondary solid tumor.105. The method of any of - claims 1 , wherein the cancer is selected from the group consisting of claims 1 , melanoma claims 1 , Merkel cell carcinoma claims 1 , lung cancer claims 1 , cervical cancer claims 1 , ovarian cancer claims 1 , uterine cancer claims 1 , breast cancer claims 1 , liver cancer claims 1 , gastric cancer claims 1 , prostate cancer claims 1 , colon cancer claims 1 , kidney cancer claims 1 , bladder cancer claims 1 , brain cancer claims 1 , and pancreatic cancer.1110. The method of any of - claims 1 , wherein the composition is administered by subcutaneous claims 1 , intradermal claims 1 , intramuscular claims 1 , intratumoral claims 1 , or intravenous injection.1210. The method of any of - claims 1 , wherein the composition is administered intranasally or intrapulmonary.1312. The method of any of - claims 1 , wherein the composition is administered in conjunction with one or more additional therapeutic agents or treatments.14. The method of claim 13 , wherein the therapeutic agents is an immune checkpoint inhibitor.15. ...

Method for detecting the presence of mycobacterial material in a sample using at least two antigens

Disclosed is a method of detecting the presence of antibodies against mycobacterial material in a sample by detecting binding of antibodies in said sample to at least two types of immobilised antigen, which antigens are capable of binding to an antibody which is indicative for the presence of mycobacterial material in a human or animal. Also disclosed is a solid substrate including a combination of said at least two antigens immobilised to said substrate, and to a biosensor having at least two types of immobilised antigen, which antigens are capable of binding to an antibody which is indicative for the presence of mycobacterial material in a human or animal.

N-GLYCOSYLATION OF PEPTIDES AND PROTEINS

A process for the production of a glycoconjugate by N-glycosylation of a protein or peptide comprising the sequence D/E-X—N—X—S/T, wherein each X is the same or different and is any natural amino acid other than proline, wherein the process comprises reacting the protein or peptide with a polyisoprenyl pyrophosphate of formula (I), or a salt thereof, in the presence of PglB: (I) to produce the glycoconjugate comprising the protein or peptide having a saccharide [SI] linked to the asparagine in the sequence D/E-X—N—X—S/T. Polyisoprenylpyrophosphates used as substrates in the biocatalytic process are also provided, as well as certain glycoconjugates. 2. A process according to claim 1 , wherein the protein or peptide comprising the sequence D/E-X—N—X—S/T is an antibody.3. A process according to claim 1 , wherein n is 1 claim 1 , 2 or 3.4. A process according to claim 1 , wherein [S1] is a mono- or disaccharide.5. A process according to claim 1 , wherein the saccharide [S1] is modified at one or more positions.6. A process according to claim 1 , wherein [S1] is GlcNAc or GlcNAc-GlcNAc claim 1 , and wherein [S1] is optionally further modified at one or more additional positions.7. A process according to claim 1 , wherein [S1] is modified to carry one or more groups R1 claim 1 , wherein R1 comprises a reactive group.8. A process according to claim 7 , wherein the reactive group is an azide claim 7 , alkene or alkyne group.9. A process according to claim 7 , wherein R1 comprises the reactive group and a linker moiety L.10. A process according to claim 9 , wherein L is selected from an alkylene moiety claim 9 , an oxy-alkylene- moiety and a moiety of formula —NH—C(═O)-alkylene-.11. A process according to claim 9 , wherein R1 is a group of formula —(C-Calkylene)-Y claim 9 , —O—(C-Calkylene)-Y claim 9 , —NH—C(═O)—(C-Calkylene)-Y claim 9 , —NH—C(═O)—O—(C-Calkylene)-Y claim 9 , —O—C(═O)—(C-Calkylene)-Y or —O—C(═O)—O—(C-Calkylene)-Y claim 9 , wherein Y is a reactive group.12. A ...

Stable peptide-conjugated ascorbic acid derivative, method for preparing same, and cosmetic composition comprising same

The present invention provides a stable peptide-conjugated, ascorbic acid derivative, a method for preparing the same, and a cosmetic composition comprising the same as an active ingredient. The stable peptide-conjugated ascorbic acid derivative of the present invention has both the effect of whitening the skin by inhibiting melanin production and the effect of reducing skin wrinkles by activating collagen production, and may be used in a cosmetic composition.

GLA Monotherapy for use in Cancer Treatment

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen. 2. The method of wherein R claim 1 , R claim 1 , Rand Rare undecyl and Rand Rare tridecyl.3. The method of any of or wherein the mammal is human.4. The method of any of - claim 1 , wherein the composition is an aqueous formulation.5. The method of any of - claim 1 , wherein the composition is in the form of an oil-in-water emulsion claim 1 , a water-in-oil emulsion claim 1 , liposome claim 1 , micellar formulation claim 1 , or a microparticle.6. The method of any of - claim 1 , wherein the cancer comprises a solid tumor.7. The method of claim 6 , wherein the solid tumor is a carcinoma claim 6 , a sarcoma or a lymphoma.8. The method of claim 6 , wherein the solid tumor is a primary solid tumor.9. The method of claim 6 , wherein the solid tumor is a secondary solid tumor.10. The method of any of - claim 6 , wherein the cancer is selected from the group consisting of claim 6 , melanoma claim 6 , Merkel cell carcinoma claim 6 , lung cancer claim 6 , cervical cancer claim 6 , ovarian cancer claim 6 , uterine cancer claim 6 , breast cancer claim 6 , liver cancer claim 6 , gastric cancer claim 6 , prostate cancer claim 6 , colon cancer claim 6 , kidney cancer claim 6 , bladder cancer claim 6 , brain cancer claim 6 , and pancreatic cancer.11. The method of any of - claim 6 , wherein the composition is administered by subcutaneous claim 6 , intradermal claim 6 , intramuscular claim 6 , intratumoral claim 6 , or intravenous injection.12. The method of any of - claim 6 , wherein the composition is administered intranasally or intrapulmonary.13. The method of any of - claim 6 , wherein the composition is administered in conjunction with one or more additional therapeutic agents or treatments.14. The method of claim 13 , wherein the therapeutic agents is an immune checkpoint inhibitor.15. The method of claim 13 , wherein the ...

IMMUNOTHERAPEUTIC POTENTIAL OF MODIFIED LIPOOLIGOSACCHARIDES/LIPID A

Embodiments of the disclosure provide for unique lipooligosaccharide/lipid A-based mimetics for use as adjuvants. Methods of generating lipooligosaccharide/lipid A-based mimetics are provided that utilize recombinantly engineered bacteria to produce the mimetics, including, for example, addition of one or more particular enzymes such as acyltransferases, deacylases, phosphatases, or glycosyltransferases. 2. A kit claim 1 , comprising one or both of the compounds of .3. The kit of claim 2 , further comprising one or both of an antigen and a pharmaceutically acceptable carrier.4. A method of enhancing an immune response in a subject claim 1 , comprising administering to the subject an effective amount of a compound of . This application is a continuation of U.S. Non-Provisional patent application Ser. No. 16/431,536 filed Jun. 4, 2019, which is a divisional of U.S. Non-Provisional patent application Ser. No. 14/772,282 filed Sep. 2, 2015, granted as U.S. Patent Registration No. 10,358,667 issued Jul. 23, 2019, which is a national phase application under 35 U.S.C. § 371 that claims priority to International Application No. PCT/US2014/022121 filed Mar. 7, 2014 which claims the benefit of priority to U.S. Provisional Patent Application No. 61/773,928, filed Mar. 7, 2013, all of which applications are incorporated by reference herein in their entirety.This invention was made with government support under Grant Number AI101685 awarded by The National Institutes of Health. The government has certain rights in the invention.Embodiments of the disclosure generally relate at least to the fields of immunology, cell biology, molecular biology, and medicine. The present disclosure generally relates to compositions, methods of screening, and methods of use for immunotherapeutic molecules and adjuvants for immunogenic formulations. More specifically, the present invention relates to compositions and methods of screening for immunogenic formulations using bacterial enzymatic ...

NICOTINAMIDE MONONUCLEOTIDE DERIVATIVES AND THEIR USES

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival. 5. The compound of claim 4 , wherein Ris optionally substituted phenyl or naphthyl.6. The compound of claim 4 , wherein R is selected from Calkyl claim 4 , Calkyl claim 4 , and Calkyl.10. The compound of claim 8 , wherein each Ris H and each Ris independently (C-C)alkyl claim 8 , (C-C)alkenyl claim 8 , (C-C)alkynyl claim 8 , (C-C)carbocyclyl claim 8 , (C-C)carbocyclylalkyl claim 8 , aryl(C-C)alkyl claim 8 , heterocyclyl(C-C)alkyl claim 8 , (C-C)aryl claim 8 , (C-C)heterocyclyl or heteroaryl.11. The compound of claim 8 , wherein each Ris H and each Ris independently (C-C)alkyl.12. The compound of claim 8 , wherein each Ris independently (C-C)alkyl.14. The compound of claim 13 , wherein Ris (C-C)aryl claim 13 , (C-C)heterocyclyl or heteroaryl.15. The compound of claim 13 , wherein Ris unsubstituted phenyl.16. The compound of claim 13 , wherein Ris pyridyl.17. The compound of claim 13 , wherein one of Ror Ris H and the other of Ror Ris (C-C)alkyl claim 13 , (C-C)alkenyl claim 13 , (C-C)alkynyl claim 13 , (C-C)carbocyclyl claim 13 , (C-C)carbocyclylalkyl claim 13 , aryl(C-C)alkyl claim 13 , heterocyclyl(C-C)alkyl claim 13 , (C-C)aryl claim 13 , (C-C)heterocyclyl or heteroaryl.18. The compound of claim 13 , wherein one of Ror Ris H and the other of Ror Ris (C-C)alkyl.19. The compound of claim 13 , wherein Ris unsubstituted phenyl claim 13 , one of Ror Ris H and the other of Ror Ris methyl. ...

D-GLYCERO-B-D-HEPTOSE 1-PHOSPHATE (HMP) CONJUGATES AND USE FOR TARGETED IMMUNE MODULATION

Heptose-1-monophosphate-7-derivatives are modifiable immunomodulators that can be used to prepare clinically active conjugate compounds. Such conjugate compounds are useful in modulating an immune response in a subject. 2. The compound of claim 1 , wherein Y is Na.3. The compound of claim 1 , wherein:R is selected from the group consisting of:{'sub': 0-6', '1-6', '0-6', '3', '1-6', '0-6', '1-6', '0-6', '0-6', '0-6', '2-6', '0-6', '2-6, '—C(O)OH, —C(O)H, —Calkyl-C(O)—Calkyl, —Calkyl-N, —Calkyl, —Calkyl —O—Calkyl, —Calkyl-aryl, —Calkyl-O-aryl, —Calkyl-C-allyl groups, and —Calkyl-O—C-allyl,'}{'sub': 0-6', '1-6', '1-6', '0-6', '1-6', '0-6', '0-6', '2-6', '0-6', '2-6, 'wherein said —Calkyl-C(O)—Calkyl, —Calkyl, Calkyl-O—Calkoxy, -aryl, Calkyl-O-aryl, Calkyl-C-allyl groups, and Calkyl-O—C-allyl is optionally substituted with a: amino, acyloxy, alkoxy, carboxyl, carbalkoxyl, hydroxy, trifluoromethyl, cyano, nitro, acyl, or a halo group;'}or{'sub': 1-6', '3', '1-6', '1-6', '3', '1-6', '1-6', '3', '1-6', '1-6', '3', '1-6', '3', '2-6, 'R is selected from the group consisting of: —Calkyl-OPOC(O)—Calkyl, —Calkyl-OPOCalkyl, —Calkyl-OPO—C—O-alkoxy, —Calkyl-OPO-aryl, and —Calkyl-OPO—C-allyl,'}{'sub': 1-6', '3', '1-6', '1-6', '3', '1-6', '1-6', '3', '1-6', '1-6', '3', '1-6', '3', '2-6, 'wherein said —Calkyl-OPOC(O)—Calkyl, —Calkyl-OPOCalkyl, —Calkyl-OPO—C—O-alkoxy, —Calkyl-OPO-aryl, —Calkyl-OPO—C-allyl group is optionally substituted with a: amino, acyloxy, alkoxy, carboxyl, carbalkoxyl, hydroxy, trifluoromethyl, cyano, nitro, acyl, or a halo group;'}orR is selected from the group consisting of:{'sub': 1-6', '3', '1-6', '1-6', '2-6', '2-6, '—C(O)OH, —C(O)H, —C(O)—Calkyl, —N, —Calkyl, —O—Calkyl, -aryl, —O-aryl, —Callyl groups, and —O—C-allyl;'}{'sub': 1-6', '1-6', '1-6', '2-6', '2-6, 'wherein said —C(O)—Calkyl, —Calkyl, —O—Calkoxy, -aryl, —O-aryl, —Callyl groups, and —O—Callyl is optionally substituted with: amino, acyloxy, alkoxy, carboxyl, carbalkoxyl, hydroxy, trifluoromethyl ...

Nicotinamide mononucleotide derivatives and their uses

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

IMMUNOTHERAPEUTIC POTENTIAL OF MODIFIED LIPOOLIGOSACCHARIDES/LIPID A

Embodiments of the disclosure provide for unique lipooligosaccharide/lipid A-based mimetics for use as adjuvants. Methods of generating lipooligosaccharide/lipid A-based mimetics are provided that utilize recombinantly engineered bacteria to produce the mimetics, including, for example, addition of one or more particular enzymes such as acyltransferases, deacylases, phosphatases, or glycosyltransferases. 3. A kit claim 1 , comprising one or more of the compositions of .4. The kit of claim 4 , further comprising one or both of an antigen and a pharmaceutically acceptable carrier. This application is a divisional of U.S. Non-Provisional patent application Ser. No. 14/772,282 filed Sep. 2, 2015, which is a national phase application under 35 U.S.C. § 371 that claims priority to International Application No. PCT/US2014/022121 filed Mar. 7, 2014 which claims the benefit of priority to U.S. Provisional Patent Application No. 61/773,928, filed Mar. 7, 2013, all of which application is are incorporated by reference herein in its their entirety.This invention was made with government support under Grant Number AI101685 awarded by The National Institutes of Health. The government has certain rights in the invention.Embodiments of the disclosure generally relate at least to the fields of immunology, cell biology, molecular biology, and medicine. The present disclosure generally relates to compositions, methods of screening, and methods of use for immunotherapeutic molecules and adjuvants for immunogenic formulations. More specifically, the present invention relates to compositions and methods of screening for immunogenic formulations using bacterial enzymatic combinatorial chemistry.To date, vaccine adjuvants such as complete Freund's adjuvant derived from the cell wall of mycobacteria in a water-in-oil emulsion or aluminum salts have been developed using an empirical trial-and-error approach. This approach has identified compounds that compensate for poor immune ...

USE OF FRUCTOSE-1,6-DIPHOSPHATE FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION FOR PROTECTION AGAINST TOXICITY INDUCED BY THE ADMINISTRATION OF ANTHRACYCLINES AND COMPOSITIONS THEREOF

LA PRESENTE INVENTION CONCERNE UNE UTILISATION DU FRUCTOSE-1,6-DIPHOSPHATE (FDP), POUR LA PREPARATION D'UNE COMPOSITION PHARMACEUTIQUE EN VUE D'UNE ACTION PROTECTRICE CONTRE LA TOXICITE PROVOQUEE SUR LE METABOLISME ET L'INTEGRITE CELLULAIRE PAR L'ADMINISTRATION PROLONGEE DES MEDICAMENTS ANTITUMORAUX ANTHRACYCLINES. L'INVENTION CONCERNE EGALEMENT DES PREPARATIONS A BASE DE FDP AYANT L'ACTION ANTITOXIQUE MENTIONNEE CI-DESSUS. THE PRESENT INVENTION RELATES TO THE USE OF FRUCTOSE-1,6-DIPHOSPHATE (FDP), FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION FOR A PROTECTIVE ACTION AGAINST CELLULAR TOXICITY CAUSED BY LONG-TERM ADMINISTRATION ANTHRACYCLINE ANTI-TUMOR DRUGS. THE INVENTION ALSO RELATES TO FDP-BASED PREPARATIONS HAVING THE ANTITOXIC ACTION MENTIONED ABOVE.

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided:(I) or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 ,Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Cytrabind oxophosphate sodium salt monohydrate having a new crystal form

본 발명은 비흡습성이고 안정성이 우수하며 재현성과 용출성이 탁월한 새로운 결정구조( 형)의 시타라빈 옥포스페이트 나트륨염 일수화물 및 그의 제조법 및 이 화합물을 함유하는 약제학적 조성물에 관한 것이다. 본 발명에 따르는 시타라빈 옥포스페이트 나트륨염 일수화물은 시타라빈 옥포스페이트 나트륨염을 물에 가온하면서 가하여 투명하게 용해시킨 후 여기에 가온한 유기용매를 가한 다음 냉각된 용기에 넣어 급냉시켜 결정을 석출시킨 다음 여과하여 건조시키는 단계를 포함하는 방법에 의해 제조된다. The present invention is a new crystal structure (non-hygroscopic, excellent stability, excellent reproducibility and elution) Cytarabine oxphosphate sodium salt monohydrate and a preparation method thereof and a pharmaceutical composition containing the compound. The cytarabine oxphosphate sodium salt monohydrate according to the present invention is dissolved in a transparent solution by adding the cytarabine oxphosphate sodium salt to warm water, and then added a warm organic solvent and then quenched in a cooled container to precipitate crystals. It is then produced by a method comprising the step of filtration and drying.

Synthetic glucopyranosyllipid adjuvants

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to immune-stimulating compounds of formula: (I), where L 1 , L 2 , L 3 , L 4 , L 5 and L 6 independently represent -O- or -NH-; L 7 , L 8 , L 9 and L 10 is independently absent or represent -C(=O)-; Y 1 represents -OP(O)(OH) 2 ; Y 2 , Y 3 and Y 4 each represents -OH; R 1 , R 3 , R 5 and R 6 independently represent C 8-13 alkyl; and R 2 and R 4 independently represent C 6-11 alkyl. EFFECT: novel compounds, based on them pharmaceutical and vaccine compositions, suitable for immune system stimulation, are claimed. 21 cl, 45 ex, 12 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 560 182 C2 (51) МПК A61K 31/7024 (2006.01) C07H 11/04 (2006.01) A61P 37/02 (2006.01) A61K 31/7028 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011152602/04, 04.06.2010 (24) Дата начала отсчета срока действия патента: 04.06.2010 (72) Автор(ы): РИД Стивен Дж. (US), КАРТЕР Даррик (US) 05.06.2009 US 61/184,703 (43) Дата публикации заявки: 20.07.2013 Бюл. № 20 R U (73) Патентообладатель(и): ИНФЕКШЕС ДИЗИЗ РИСЕРЧ ИНСТИТЬЮТ (US) Приоритет(ы): (30) Конвенционный приоритет: (45) Опубликовано: 20.08.2015 Бюл. № 23 2 5 6 0 1 8 2 (56) Список документов, цитированных в отчете о поиске: US 20080131466 A1, 05.06.2008. US 4912094 A, 27.03.1990. RU 2288723C2, 10.12.2008 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 10.01.2012 (86) Заявка PCT: US 2010/037466 (04.06.2010) 2 5 6 0 1 8 2 WO 2010/141861 (09.12.2010) C 2 C 2 (87) Публикация заявки PCT: Адрес для переписки: 129090, Москва, ул. Большая Спасская, 25, стр. 3, ООО "Юридическая фирма "Городисский и Партнеры" (54) СИНТЕТИЧЕСКИЕ ГЛЮКОПИРАНОЗИЛЛИПИДНЫЕ АДЪЮВАНТЫ (57) Реферат: Изобретение относится к представляют собой -O- или -NH-; L7, L8, L9 и L10 иммуностимулирующим соединениям формулы: независимо отсутствуют или представляют собой -С(=O)-; Y1 представляет собой -OP(O)(OH)2; Y2, Y3 и Y4 каждый представляет R U -ОН ...

Peptide derivative and its preparation

새로운 결정구조의 시타라빈 옥포스페이트 나트륨염 일수화물

본 발명은 비흡습성이고 안정성이 우수하며 재현성과 용출성이 탁월한 새로운 결정구조(∂형)의 시타라빈 옥포스페이트 나트륨염 일수화물 및 그의 제조법 및 이 화합물을 함유하는 약제학적 조성물에 관한 것이다. 본 발명에 따르는 시타라빈 옥포스페이트 나트륨염 일수화물은 시타라빈 옥포스페이트 나트륨염을 물에 가온하면서 가하여 투명하게 용해시킨 후 여기에 가온한 유기용매를 가한 다음 냉각된 용기에 넣어 급냉시켜 결정을 석출시킨 다음 여과하여 건조시키는 단계를 포함하는 방법에 의해 제조된다.

Hormone and growth factor mimetics

Hormone and growth factor phosphoglycokine mimetics from mycobacterium

A hormone or growth factor mimetic second messenger is derived from a microorganism of the genus Mycobacterium, suitably M. vaccae. The mimetic second messenger may mimic the action of insulin, ACTH, NGF, EGF, FGF, TGFβ or HGF. Further, methods of treating type I or type II diabetes mellitus, polycystic ovary syndrome, central nervous system damage, hepatic damage, alcohol abuse, drug sensitivity, tissue damage, adrenal atrophy, etc., are also disclosed. The methods are carried out by administering the mimetic second messenger to a patient in need thereof.

Certain aminoalkyl glucosaminide phosphate compounds and their use

Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Certain aminoalkyl glucosaminidophosphate compounds and their use

Glycosaminoglycan (GAG) MIMETICS

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2006 126 718 (13) A (51) ÌÏÊ C07H 5/10 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006126718/04, 21.12.2004 (71) Çà âèòåëü(è): ÏÐÎÄÆÅÍ ÈÍÄÀÑÒÐÈÇ ËÈÌÈÒÅÄ (AU) (30) Êîíâåíöèîííûé ïðèîðèòåò: 23.12.2003 AU 2003907107 (43) Äàòà ïóáëèêàöèè çà âêè: 27.01.2008 Áþë. ¹ 3 (87) Ïóáëèêàöè PCT: WO 2005/061523 (07.07.2005) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Ã.Á. Åãîðîâîé, ðåã.¹ 513 A (54) ÌÈÌÅÒÈÊÈ ÃËÈÊÎÇÀÌÈÍÎÃËÈÊÀÍΠ(GAG) (57) Ôîðìóëà èçîáðåòåíè R U A 2 0 0 6 1 2 6 7 1 8 1. Ñîåäèíåíèå ôîðìóëû ãäå êàæäûé Õ íåçàâèñèìî îçíà÷àåò ÑÍ2, Ñ(Î), N, O, S, S(O), S(O)2 èëè ñâ çü è êàæäûé R1-R5 íåçàâèñèìî îçíà÷àåò ñâ çü èëè âûáèðàþò èç ãðóïïû, âêëþ÷àþùåé âîäîðîä; ãàëîãåí; àçèä: ãðóïïó R, îïðåäåë åìóþ êàê Ñ1-Ñ8 àëêèë èëè àëêåíèë, àðèë èëè ãåòåðîàðèë, êîòîðà äîïîëíèòåëüíî íåîá çàòåëüíî çàìåùåíà ãðóïïàìè àëêîêñè, àðèëîì, ãåòåðîàðèëîì èëè àðèëîêñè; -ÑÎÎÍ, -S(O)2OH; -S(O)2OH, -S(O)OH, -S(O)R, S(O)2R, -S(O)2NH2, -S(O)2OR, -S(O)OR; -C(O)R; ãåòåðîöèêëè÷åñêóþ ãðóïïó, êîòîðà äàëåå çàìåùåíà àëêèëîì, àðèëîì, -ÑÍ2NHC(O)R, -CH2N(C(O)R)2 èëè -CH2OR; Ñòðàíèöà: 1 RU 2 0 0 6 1 2 6 7 1 8 (86) Çà âêà PCT: AU 2004/001800 (21.12.2004) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 24.07.2006 (72) Àâòîð(û): ÄÎÍ Ðîáåðò Õüþ (AU), ÔÅÐÐÎ Âèòî (AU), ÁÈÒÂÝÉ ßí (AU), ÊÎØÐÀÍ Ñèñêà (AU), ÔÝÉÐÂÅÒÅÐ Äæîí Êðþãåð (AU), ÕÝÌÌÎÍÄ Ýäâàðä Òèìîòè (AU), ÊÀÐÎËÈ Òîìèñëàâ (AU), ËÈ Öàé Ïèí (AU), ËÈÓ Ëèãóí (AU) 2 0 0 6 1 2 6 7 1 8 R U A Ñòðàíèöà: 2 2 0 0 6 1 2 6 7 1 8 ãäå ïî êðàéíåé ìåðå îäíà, íî íå áîëåå äâóõ ãðóïï èç R7-R11 íåçàâèñèìî ïðåäñòàâë åò ñîáîé ñòðóêòóðó ôîðìóëû I; ãäå Y íåçàâèñèìî îçíà÷àåò ñâ çü, Í, R èëè -Ñ(Î)R, êàê îïðåäåëåíî âûøå; è ïî êðàéíåé ìåðå îäíà, íî íå áîëåå ãðóïïà èç R7-R11 íåçàâèñèìî ïðåäñòàâë åò ñîáîé ñòðóêòóðó ôîðìóëû II, ëèáî êàæäà ãðóïïà èç R7-R11 îòñóòñòâóåò íåçàâèñèìî îò äðóãèõ ãðóïï; èëè ...

Phosphate, liposome comprising the phosphate as membrane constituent, and cosmetic and liposome preparation comprising the liposome

A novel monophosphate and a novel diphosphate prepared by a phosphatidyl transfer reaction of a phospholipid and an alcohol in the presence of phospholipase D are disclosed. The phosphates can independently or together form small and stable liposomes which can include active components therein. Cosmetic compositions comprising these phosphates or liposomes penetrate well into the hair and the skin, and exhibit long-lasting excellent moisture-retaining, beauty, skin-activation effects.

Use of fucosylation inhibitor for producing afucosylated antibody

The present invention provides inhibitors of fucosylation during protein expression from mammalian cells. The inhibitors are derived from rhamnose and act by inhibition of GDP-mannose 4,6-dehydratase (GMD). The invention further provides methods of making proteins with reduced level of fucosylation, such as antibodies and antibodies made by the methods of the present invention. Such hypofucosylated or nonfucosylated antibodies may find use, for example, in treatment of human disease in which is it therapeutically beneficial to direct antibody dependent cellular cytotoxicity (ADCC) mediated killing of cells expressing the antibody target on their surface, for example in depletion of Tregs in cancer patients using a hypofucosylated or nonfucosylated anti-CTLA-4 antibody.

Synthetic glucopyranosyl lipoid adjuvants

FIELD: medicine; pharmaceuticals. SUBSTANCE: invention relates to a method for treating an infection caused by Mycobacterium tuberculosis , comprising administering a composition comprising a GLA compound having the following structure (I): (I) or a pharmaceutically acceptable salt thereof, where L 1 , L 2 , L 3 , L 4 , L 5 and L 6 are identical or different and independently represent -O- or -NH-; L 7 , L 8 , L 9 and L 10 are identical or different and independently absent or are -C (= O) -; Y 1 is -OP (O) (OH) 2 ; Y 2 , Y 3 and Y 4 each represent -OH; R 1 , R 3 , R 5 and R 6 are identical or different and independently represent C 8-13 -alkyl; and R 2 and R 4 are identical or different and independently represent C 6-11 -alkyl. EFFECT: novel effective method of treating tuberculosis by enhancing the immune response. 8 cl, 4 dwg, 45 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 732 574 C2 (51) МПК A61K 31/7024 (2006.01) C07H 11/04 (2006.01) A61P 37/02 (2006.01) A61K 31/7028 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/7024 (2018.08); C07H 11/04 (2018.08); A61P 37/02 (2018.08); A61K 31/7028 (2018.08) (21)(22) Заявка: 2015129468, 04.06.2010 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): ИНФЕКШЕС ДИЗИЗ РИСЕРЧ ИНСТИТЬЮТ (US) Дата регистрации: 21.09.2020 05.06.2009 US 61/184,703 Номер и дата приоритета первоначальной заявки, из которой данная заявка выделена: 2011152602 05.06.2009 (56) Список документов, цитированных в отчете о поиске: US 20080131466 A1, 05.06.2008. US 4912094 A, 27.03.1990. RU 2288723 C2, 10.12.2008. (43) Дата публикации заявки: 27.12.2015 Бюл. № 36 C 2 (54) СИНТЕТИЧЕСКИЕ ГЛЮКОПИРАНОЗИЛЛИПИДНЫЕ АДЪЮВАНТЫ (57) Реферат: Изобретение относится к способу лечения или его фармацевтически приемлемую соль, инфекции, вызванной Mycobacterium tuberculosis, где L1, L2, L3, L4, L5 и L6 являются одинаковыми включающему введение композиции, содержащей или различными и ...

Certain aminoalkyl glucosaminide phospahte derivatives and use thereof

FIELD: chemistry. ^ SUBSTANCE: present invention relates to a compound having general structural formula , in which n is equal to 1 or 5 and R6 is COOH or CH2OPO3H2, to a pharmaceutically acceptable salt of the said compound. The invention also pertains to a pharmaceutical composition based on the said compounds or their pharmaceutically acceptable salts, meant for inducing or boosting immunoreaction in a subject. ^ EFFECT: invention relates to a method of inducing or boosting immunoreaction in a subject, as well as to a method of relieving or essentially preventing an infectious disease, involving administration of an effective amount of the said compound to the subject. ^ 7 cl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 389 732 (13) C2 (51) МПК C07H 13/06 (2006.01) A61K 31/7036 (2006.01) A61P 37/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2005125050/04, 06.01.2004 (24) Дата начала отсчета срока действия патента: 06.01.2004 (73) Патентообладатель(и): КОРИКСА КОРПОРЕЙШН (US) R U (30) Конвенционный приоритет: 06.01.2003 US 60/438,585 (72) Автор(ы): ДЖОНСОН Дейвид А. (US) (43) Дата публикации заявки: 27.01.2006 C 2 2 3 8 9 7 3 2 R U C 2 (56) Список документов, цитированных в отчете о поиске: US 6,355,257 B1, 12.03.2002. WO 98/50399 A1, 12.11.1998. US 2003/0092643 A1,15.05.2003. US 2003/0199460 A1, 23.10.2003. WO 98/50399 A1, 12.11.1998. US 6,303,347 В1, 16.10.2001. WO 01/34617 A2, 17.05.2001. US 6,355,257 В1, 12.03.2002. US 5,593,969 А, 14.01.1997. STN БД СА AN 137:57599 (RN 234088-15-4) - US 6,417,172 B1, 09.07.2002. STN БД СА AN 126: 317571 (RN 185954-96-5) - WO 96/39411 A1, 12.12.1996. (85) Дата перевода заявки PCT на национальную фазу: 08.08.2005 (86) Заявка PCT: US 2004/000377 (06.01.2004) (87) Публикация PCT: WO 2004/062599 (29.07.2004) Адрес для переписки: 103735, Москва, ул. Ильинка, 5/2, ООО "Союзпатент", А.П.Агурееву (54) НЕКОТОРЫЕ ...

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided:(I) or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 ,Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Phosphoglycolipid and methods for its use

The invention concerns a novel phosphoglycolipid compound. The compound of the subject invention is 2-Deoxy-6-O-[2-deoxy-4-O-phosphono-3-O-[(R)-3-tetradecanoyloxytetradecanoyl]-2-[(R)-3-octadecanoyloxytetradecanoylamino]-β-D-glucopyranosyl]-2-[(R)-3-hexadecanoyloxytetradecanoylamino]-D-glucopyranose and pharmaceutically acceptable salts thereof. The compound is not immunoreactive, not pyrogenic, not toxic but is active in ameliorating tissue damage due to ischemia/reperfusion injury. Methods for using the subject compound to protect against reversible and irreversible damage due to ischemia/reperfusion injury are also disclosed.

Synthetic glucopyranosyl lipid adjuvants and vaccine compositions containing them

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 , Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Stable peptide-conjugated ascorbic acid derivatives, process for preparing same and cosmetic compositions containing same

本发明提供稳定的肽缀合抗坏血酸衍生物、用于制备其的方法和包含其作为活性成分的化妆品组合物。本发明的稳定的肽缀合抗坏血酸衍生物具有通过抑制黑色素产生来美白皮肤的效果和通过激活胶原蛋白产生来减少皮肤皱纹的效果，并且可以在化妆品组合物中使用。

Stabilized Ascorbic Acid Derivatives with Peptide, its Preparation Method and Cosmetic Composition Comprising the Same

본 발명은 펩타이드가 결합된 안정한 아스코르빈산 유도체, 그의 제조방법 및 그를 유효성분으로 포함하는 화장료 조성물을 제공한다. 본 발명의 펩타이드가 결합된 아스코르빈산 유도체는 멜라닌 생성 억제를 통한 미백 효과 및 콜라겐 생성 활성화를 통한 주름개선 효과를 동시에 나타내는 이중복합 기능을 가지며, 화장료 조성물에 사용될 수 있다. The present invention provides a stable ascorbic acid derivative to which a peptide is bound, a process for producing the same, and a cosmetic composition comprising the same as an active ingredient. The peptide conjugated ascorbic acid derivative of the present invention has a dual complex function simultaneously exhibiting whitening effect through inhibition of melanin production and wrinkle improvement effect through activation of collagen production, and can be used in a cosmetic composition.

Some amino alkyl glucose aminide phosphate derivatives and thereof application

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to immunoeffectors of formula: , where n equals 1 (C 6 alkyl) or 5 (C 10 alkyl), and R 1 represents CO 2 H. EFFECT: claimed novel compounds and pharmaceutical compositions based on them enhance immune response, increase production of antibodies in immunised animals, stimulate production of cytokines and activate macrophages. 7 cl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 544 850 C2 (51) МПК C07H 13/06 (2006.01) C07H 11/04 (2006.01) C07H 15/06 (2006.01) C07H 5/02 (2006.01) C07H 9/02 (2006.01) A61K 31/7036 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61P 37/00 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 31/00 (2006.01) (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2009140730/04, 06.01.2004 (24) Дата начала отсчета срока действия патента: 06.01.2004 (72) Автор(ы): ДЖОНСОН Дейвид А (US) (73) Патентообладатель(и): КОРИКСА КОРПОРЕЙШН (US) R U Приоритет(ы): (22) Дата подачи заявки: 06.01.2004 (30) Конвенционный приоритет: 06.01.2003 US 60/438,585 Номер и дата приоритета первоначальной заявки, из которой данная заявка выделена: 2 5 4 4 8 5 0 2005125050 06.01.2003 (43) Дата публикации заявки: 10.05.2011 Бюл. № 13 (45) Опубликовано: 20.03.2015 Бюл. № 8 2 5 4 4 8 5 0 R U 5593969 A1, 14.01.1997. US 6355257 B1, 12.03.2002. WO 1996039411 A1, 12.12.1996. Baldridge J.R. et al., J Endotoxin Res, 2002; v.8, n.6, p.p.453-458 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: WO 1998050399 A1, 12.11.1998. US Адрес для переписки: 109012, Москва, ул. Ильинка, 5/2, ООО "Союзпатент" (54) НЕКОТОРЫЕ АМИНОАЛКИЛГЛЮКОЗАМИНИДФОСФАТНЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ (57) Реферат: Изобретение относится к иммуноэффекторам где n равно 1 (С6алкил) или 5 (С10 алкил), а R1 формулы: представляет собой CO2H. Предложенные новые соединения и фармацевтические композиции на их основе усиливают иммунную реакцию, увеличивают выработку антител у иммунизированных животных, а также стимулируют выработку цитокинов и активируют макрофаги. 4 н. ...

2'-fluoro substituted carba-nucleoside analogs for antiviral treatment

Provided are select imidazo[1,2-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2′ position of the nucleoside sugar is substituted with halogen and carbon substituents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.

Methods for synthesizing nucleosides, nucleoside derivatives and non-nucleoside derivatives

The present invention provides methods for the chemical synthesis of nucleosides and derivatives thereof, including 2'-amino, 2'-N-phthaloyl, 2'-O-methyl, 2'-O-silyl, 2'-OH nucleosides, C-nucleosides, nucleoside phosphoramidites, C-nucleoside phosphoramidites, and non-nucleoside derivatives.

Phosphoramidate derivatives

Methods for introducing mannose-6-phosphate and other oligosaccharides onto glycoproteins and its application thereof

Methods to introduce highly phosphorylated mannopyranosyl oligosaccharide derivatives containing mannose-6-phosphate (M6P), or other oligosaccharides bearing other terminal hexoses, to carbonyl groups on oxidized glycans of glycoproteins while retaining their biological activity are described. The methods are useful for modifying glycoproteins, including those produced by recombinant protein expression systems, to increase uptake by cell surface receptor-mediated mechanisms, thus improving their therapeutic efficacy in a variety of applications.

Synthetic antigen constructs against campylobacter jejuni

The invention relates to immunogenic synthetic constructs capable of inducing an immune response against Campylobacter jejuni (C. jejuni) in a subject comprising one or more monosaccharides comprising one or more MeOPN moieties. Specifically, the invention relates to immunogenic synthetic constructs capable of inducing an immune response against Campylobacter jejuni (C, jejuni) in a subject comprising one or more MeOPN ⃗ 6 Gal monosaccharides. The invention also relates to compositions comprising the immunogenic synthetic constructs and methods of inducing an immune response against C. jejuni in a subject comprising administering the immunogenic synthetic constructs, and/or compositions comprising the immunogenic synthetic construct, to the subject.

A kind of fructose sodium diphosphate compound and preparation method thereof

本发明涉及医药领域，具体地说，涉及一种果糖二磷酸钠化合物及其制备方法。所述果糖二磷酸钠化合物的X‑射线衍射图谱如图1所示，本发明还提供了该种果糖二磷酸钠化合物的制备方法，采用啤酒酵母、葡萄糖、磷酸、碳酸镁等原料进行发酵，经过滤和离子交换之后，脱色过滤并结晶干燥，得到1,6‑二磷酸果糖三钠八水合物。使用上述方法生产的果糖二磷酸钠化合物吸湿性有所降低，稳定性增加，有利于注射剂的生产应用，并且由于其特有的晶型提高了口服生物利用度，适合于片剂的生产应用。

Production of sphingolipid derivative using enzymic method

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Lipid analogs or their pharmaceutically acceptable salts

FIELD: organic chemistry. SUBSTANCE: product: lipid analogs of the general formula (I): where: R 1 - OH, ; R 2 - where: R 6 and R 7 - H, F; R 8 - H, OH or tetradecanoyloxy; - tetradecanoyl or R 9 where: R 10 - H, F; R 4 - H, OH, tetradecanoyloxy or 2,2-difluorotetradecanoyloxy; - OH, R< and at least one of groups R 4 and - group R 5 ; R 2 - OH, F at condition that exception of case when at least one of R 3 and R 2 - tetradecanoyl substituted with F or at least one substituent of the group: F, OH, tetradecanoyloxy, or at least one of R 3 and R 4 - tetradecanoyl substituted with at least one fluoro-substituted tetradecanoyloxy-group, or their pharmaceutically acceptable salts. Synthesized compounds were used as immunoregulating and immunostimulating preparations. EFFECT: improved method of synthesis. 6 cl, 4 tbl 41019140Сс ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2076 107. (51) МПК 13) Сл С 07Н 5/06 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5052656/04, 09.09.1992 (30) Приоритет: 11.12.1989 УР 1-321153 20.02.1990 УР 2-37339 (46) Дата публикации: 27.03.1997 (56) Ссылки: Сагфопуагае Кезеагсй. спет. 6 (4), 625-638 (1987). Сагропуагае Кезеагсп, 162 (1987), 127-140. (62) Первичная заявка, из которой выделена настоящая: 4830600/04 (71) Заявитель: Санкио Компани Лимитед (.Р) (72) Изобретатель: Масао Сиозаки[Р], Нобору Исида[Р], Томово Кобаяси[/Р], Тетсуо Хираока[/Р], Масами Араи[/Р], Юзуру Акаматсу[/Р], Масахиро Нисидзима[/Р] (73) Патентообладатель: Санкио Компани Лимитед (Р) (54) АНАЛОГИ ЛИПИДА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ (57) Реферат: Использование: В иммунорегулирующих и иммуностимулирующих препаратов. Сущность: продукт: аналоги липида общей формулы |: качестве 1 сн о 5 2 52 = с с 4 2 Е и в \ нк | з ОЕ 6 о Е 1 и 2 | Е -он, 0-Р-ОН к -с-с -Сн-<СН,>, -Сн, | и [3 15 он о Е Е ле Вби В’- НЕ В _Н ОН или тетрадеканоилокси, КЗ - тетрадеканоил или _-С-СН-СН -ССН —_СН и 1з 10 2 10 3 ов Е де В? - Н, Е В - Н; ОН ПРИЕМЛЕМЫЕ СОЛИ ...

Lipidated PSA compositions and methods

The invention provides various isolated and synthetic forms of lipidated PSA as well as isolated or synthetic forms of the glycolipid component of lipidated PSA, and compositions thereof, methods of making including methods of isolating such forms, and methods of use thereof.

Lipoteichoic acid-derived glycolipids, and compositions comprising same

The present invention relates to lipoteichoic acid-derived glycolipids, and to pharmaceutical, food or cosmetic compositions and vaccine adjuvants comprising same. The lipoteichoic acid-derived glycolipids according to the present invention inhibit the production of inflammatory cytokines and thus have anti-inflammatory effects. Therefore, pharmaceutical, food or cosmetic compositions comprising lipoteichoic acid-derived glycolipids of the present invention can be employed for the purpose of preventing and treating inflammatory diseases. The lipoteichoic acid-derived glycolipids of the present invention can be also used as vaccine adjuvants.

GLA monotherapy for use in cancer treatment

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen.

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 , Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L 1 . L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 , Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 , Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L 1 , L 2 , L 3 , L 4 , L 5 , L 6 , L 7 , L 8 , L 9 , L 10 , Y 1 , Y 2 , Y 3 , Y 4 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

GLA monotherapy for use in cancer treatment

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen.

GLA monotherapy for use in cancer treatment

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen.

GLA monotherapy for use in cancer treatment

The present disclosure relates generally to compositions and methods for treating cancer with a glucopyranosyl lipid A (GLA) in the absence of antigen.

Phosphoramidate derivatives

Halogenated dideoxy saccharide derivatives, preparation method and use thereof

본 발명은 활로겐 다이디글루코오스 유도체를 공개하며, 다음 일반식I를 지닌 화합물임: 이중X는 할로겐 원소이고, 이다; R 1 ，R 2 는 각각H또는Br이고; R 3 ，R 4 는 각각OH또는Oac이다. 본 발명의 화합물 1-14을 실험한 결과, 화합물1-14는 인체 비인두암 모계세포 CNE-2Z, 인체 폐암 암세포 A549, 인체 결장암 암세포 HT-29, 인체 간암 암세포 Bel-7402, 인체 대장암 암세포 HCE8693, 인체 위암 암세포 BGC-803, 인체 식도암 암세포 CaEs-17, 인체 유방암 암세포 MCF-7, 인체 난소암 암세포 A2780, 인체 췌장암 암세포 PC-3, 인체 방광암 암세포 EJ, 인체 뇌교질암 암세포 TG-905, 인체 백혈병 세포 K562, 인체 흑색종 암세포 M14, 갑상선 이형성암 암세포 TA-K등 종양세포에 대해 모두 강력한 선장억제작용의 효과가 있다는 것을 보여준다. 항암약물 제조에 사용할 수 있고, 보다 큰 임상 용도 가치가 있다. The present invention discloses an active dideoxyglucose derivative and is a compound having the general formula I: X is a halogen element, to be; R 1 and R 2 are each H or Br; R 3 and R 4 are each OH or Oac. As a result of the test of Compound 1-14 of the present invention, the compound 1-14 was found to be a human body cancer cell line CNE-2Z, a human lung cancer cell A549, a human colorectal cancer cell HT-29, a human liver cancer cell Bel-7402, a human colorectal cancer cell HCE8693 , Human gastric cancer cancer cell BGC-803, human esophageal cancer cell CaEs-17, human breast cancer cancer cell MCF-7, human ovarian cancer cell cancer cell A2780, human pancreatic cancer cell cancer PC-3, human bladder cancer cell EJ, human pancreatic cancer cancer cell TG-905, human leukemia Cell K562, human melanoma cancer cell M14, and thyroid dysplasia cancer cell TA-K. It can be used for the manufacture of anticancer drugs and has a greater clinical use value.

Synthetic glucopyranosyl lipid adjuvants

本申请涉及合成的吡喃葡萄糖脂佐剂。提供具有下述结构(I)的化合物，尤其是吡喃葡萄糖脂佐剂(GLA)化合物，或其药物可接受的盐： 其中L 1 、L 2 、L 3 、L 4 、L 5 、L 6 、L 7 、L 8 、L 9 、L 10 、Y 1 ,Y 2 、Y 3 、Y 4 、R 1 、R 2 、R 3 、R 4 、R 5 、R 6 如本文所定义。还提供诱导或增强免疫反应的药物组合物、疫苗组合物以及相关方法。

GLA monotherapy for use in cancer treatment

본 개시내용은 통상적으로 항원의 부재하에 글루코피라노실 지질 A (GLA)를 포함하는 암을 치료하기 위한 조성물 및 방법에 관한 것이다. The present disclosure is generally directed to compositions and methods for treating cancer comprising glucopyranosyl lipid A (GLA) in the absence of antigen.

Phosphate derivative, its production and antitumor agent containing the same

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Process for the preparation of novel saccharides

Kallikrein inactivator against diseases of the pancreas.

MANOSSYL-1 PHOSPHATES, PROCESS FOR THEIR PREPARATION AND USE IN THERAPEUTICS, IN PARTICULAR WITH RESPECT TO CDG-LA SYNDROME

PROCESS FOR TRANSFORMATION OF AN ALDOSE OR ALDOSE DERIVATIVE INTO A CETOSE OR DERIVATIVE OF CETOSE

Patent FR2316246B1

SUGAR PHOSPHATES FOR USE IN SHAMPOOS, RINSES AND COSMETICS, AND PROCESS FOR THE PREPARATION OF SUCH PHOSPHATES

4,6-0-hydroxyphosphoryl-glucosamine derivatives

A B S T R A C T 4,6-O-hydroxyphosphoryl-glucosamine derivatives as shown in the following formula [I] and its pharmaceutically-acceptable salt: [I] wherein R1 and R2 indicate a hydrogen atom or a hydroxy group; one of R3 and R4 indicates -OCO(CH2)nCH3, -CH2(CH2)nCH3 or -O-CH2(CH2)nCH3, and the other indi-cates a hydrogen atom; 1 is an integer of 4-16; m is an integer of 4-16; and n is an integer of 6-18.

Drug composition, useful as cellular sources of mannose-1-phosphate against carbohydrate deficient glycoprotein type I syndrome, comprises excipient and active ingredient e.g. mono(alpha-D-mannopyranosyl-1) phosphates

Drug composition comprises an excipient and an active ingredient (T) e.g. mono (alpha -D-mannopyranosyl-1) phosphates, in a medium. Drug composition comprises an excipient and an active ingredient (T) e.g. mono (alpha -D-mannopyranosyl-1) phosphate of formula (I), (II) and/or (III), in a medium. R 11-R 14, R 21-R 24H or OH protecting group (preferably 2-6C aliphatic acyl); R, R1a : T 1, OB 1, O-CH(CH 3)-O-CO-(1-5C)alkyl, -O-CH(CH 3)-O-CO-O-(1-5C)alkyl or -O-CH 2-CH(OH)-CH 2OH, preferably OB 1, phenoxy, 1-naphtyloxy, benzyloxy, 1-naphtylmethoxy, -O-CH(Q)-O-CO-O-(1-5C) alkyl, -O-CH 2-CH(OH)-CH 2OH, OH protecting group, -NH-(CH 2) 4-CH(NH 2)COOH, -(p-O)-C 6H 4-CH 2-CH(NH 2)COOH, -O-CH 2-CH(NH 2)COOH or -O-CH(CH 3)- CH(NH 2)COOH, -NH-(CH 2) 3-CH-(NH 2)COOH or -NH-(CH 2) 2-CH(NH 2)COOH (where COOH and NH 2of each group is protected); T 16-10C aryloxy, (6-10C)aryl(1-5C)alkyleneoxy (both optionally substituted by T 2), -O-CH 2-CH(OH)-CH 2OH, OH protecting group (2-6C acyl), -X-A-CH(COOY 1)(NZ 2Z 3)- or -(Z 2)N-CH(Z 4)-COOY 1; T 21-5C alkyl, 1-5C alkoxy, halo, CF 3and/or NO 2; B 1optionally branched 2-21C ethylenic unsaturated hydrocarbon chain or 5-21C cycloaliphatic group, preferably farnesyloxy or geranyloxy group; X : -O-, -S- or -NZ 1; Y 12-5C alkyl; A, Z 41-5C alkylene, phenylene or phenylalkylene group; Z 1-Z 3H, 1-5C alkyl, or N protecting group; R1 : OH protecting group (2-6C acyl), 1-20C alkoxy, -O-CH(Q)-O-CO-alkyl, -O-CH(Q)-O-CO-O-(1-5C)alkyl, OB 1or T 1, phenoxy, 1-naphtyloxy, benzyloxy, 1-naphtylmethoxy, -O-CH(Q)-O-CO-O-(1-5C) alkyl, -O-CH 2-CH(OH)-CH 2OH, OH protecting group, -NH-(CH 2) 4-CH(NH 2)COOH, -(p-O)-C 6H 4-CH 2-CH(NH 2)COOH, -O-CH 2-CH(NH 2)COOH or -O-CH(CH 3)- CH(NH 2)COOH, -NH-(CH 2) 3-CH-(NH 2)COOH or -NH-(CH 2) 2-CH(NH 2)COOH (where COOH and NH 2of each group is protected); Q : H or CH 3; and R 31-R 34H or OH protecting group (preferably 3-6C aliphatic acyl). Independent claims are included for: (1) a mannosyl-1 phosphate derivative of formula (I ...

NOVEL DISACCHARIDES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

L'INVENTION CONCERNE LES COMPOSES DE FORMULE IA ET III: (CF DESSIN DANS BOPI) (CF DESSIN DANS BOPI) ET LEUR PREPARATION. CES COMPOSES PEUVENT ETRE TUILISES COMME MEDICAMENTS EN PARTICULIER COMME MODULATEURS DE LA RESISTANCE ANTI-MICROBIENNE. THE INVENTION CONCERNS THE COMPOUNDS OF FORMULA IA AND III: (CF DRAWING IN BOPI) (CF DRAWING IN BOPI) AND THEIR PREPARATION. THESE COMPOUNDS MAY BE USED AS MEDICINES, IN PARTICULAR AS MODULATORS OF ANTI-MICROBIAL RESISTANCE.

SUGAR PHOSPHATES FOR USE IN SHAMPOO, RINSE AND COSMETICS, AND PROCESS FOR PREPARING THESE PHOSPHATES

ON PREPARE UN PHOSPHATE DE SUCRE DE FORMULE GENERALE: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN RESTE A HYDROGENE ACTIF D'UN HEXOSE, ET R, R ET R SONT IDENTIQUES OU DIFFERENTS ET REPRESENTENT CHACUN UN GROUPEMENT HYDROCARBONE SATURE OU INSATURE AYANT DE 1 A 4 ATOMES DE CARBONE, EN FAISANT REAGIR UN MONOESTER PHOSPHORIQUE AVEC UN SEL DE GLYCIDYLTRIALKYLAMMONIUM. LES PHOSPHATES DE SUCRE SELON L'INVENTION POSSEDENT UNE BONNE RETENTION DE L'HUMIDITE ET UN BON POUVOIR ABSORBANT SUR LES CHEVEUX, ET ON PEUT LES UTILISER DANS DES SHAMPOOINGS, DES RINCAGES ET DES COSMETIQUES. A SUGAR PHOSPHATE OF THE GENERAL FORMULA: (CF DRAWING IN BOPI) IS PREPARED IN WHICH R REPRESENTS AN ACTIVE HYDROGEN REMAINDER OF A HEXOSE, AND R, R AND R ARE THE SAME OR DIFFERENT AND EACH REPRESENT A SATURATED OR INSATURATED HYDROCARBON GROUP. FROM 1 TO 4 CARBON ATOMS, BY REACTING A PHOSPHORIC MONOESTER WITH A GLYCIDYLTRIALKYLAMMONIUM SALT. SUGAR PHOSPHATES ACCORDING TO THE INVENTION HAVE GOOD MOISTURE RETENTION AND ABSORBING POWER ON THE HAIR, AND CAN BE USED IN SHAMPOOS, RINSES AND COSMETICS.

IMMUNOSTIMULANT MEDICINAL PRODUCT CONTAINING OSE DERIVATIVE OR PHOSPHORYL POLYOSE

USE OF FRUCTOSE-1,6-DIPHOSPHATE FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION FOR PROTECTION AGAINST TOXICITY INDUCED BY THE ADMINISTRATION OF ANTHRACYCLINES AND COMPOSITIONS THEREOF

Synthetic antigen constructs against campylobacter jejuni

The invention relates to immunogenic synthetic constructs capable of inducing an immune response against Campylobacter jejuni (C. jejuni) in a subject comprising one or more monosaccharides comprising one or more MeOPN moieties. Specifically, the invention relates to immunogenic synthetic constructs capable of inducing an immune response against C. jejuni in a subject comprising one or more MeOPN-6-Gal monosaccharides, one or more MeQPN-4-Gal monosaccharides, and/or one or more MeOPN-2-Gal monosaccharides. The invention also relates to compositions comprising the immunogenic synthetic constructs, and methods of inducing an immune response against C. jejuni in a subject comprising administering the immunogenic synthetic constructs, and/or compositions comprising the immunogenic synthetic constructs, to the subject. Methods of treating, preventing, or ameliorating a C. jejuni bacterial infection in a subject comprising administering to the subject one or more doses of immunoglobulins directed to one or more of the MeOPN moieties are also contemplated.

New drug in particular for the treatment of states of adynamia.

Fructose 1,6-diphosphate(fdp) as parenteral injection for human prepared by partial freeze-drying

(57)【要約】 【課題】 フルクトース−１，６−ジホスフェート（Ｆ ＤＰ）を虚血または低酸素状態の患者および心臓バイパ ス手術を受ける患者に注射するのに適切な剤型で提供す る。 【解決手段】 ＦＤＰ水溶液、または該塩水溶液を、残 留含水量が１０％から２５％（重量比）である固体物質 を生成するまで凍結乾燥することにより、一部凍結乾燥 ＦＤＰ、または薬理的に許容な該塩を製造する方法を提 供する。残留含水量が１２％から１６％（重量比）の範 囲であることが特に望ましく、確実に総不純物を５％以 下、いずれの単不純物も１％以下とすることが可能であ る。この製剤は、ＦＤＰを凍結乾燥バイアルに詰入し、 凍結乾燥工程を遂行することにより、密閉無菌容器内部 で生成される。高含有水分は製品の安定度及び、貯蔵寿 命を減じたり、限定することはない。純度の実質的欠損 なしに１年以上室温保存が可能である。

Nicotinamide mononucleotide derivatives and their uses

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

Synthetic lipid a glycoconjugate antigens for use in vaccines

31,791-00 SYNTHETIC LIPID A GLYCOCONJUGATE ANTIGENS FOR USE IN VACCINES ABSTRACT Synthetic glycoconjugate antigens of the formula:

SYNTHETIC GLYCONKJJUGATANTIGENER AV LIPID A FOER ATT ANVAENDAS I VACCINER

Phosphoglycan messengers and their medical uses

Phosphoglycan messengers (PGMs) which are carbohydrate derivatised phosphatidyl cyclitols are disclosed, together with the finding that these substances are biologically active, especially in modulating plasma cholesterol, plasma triglycerides and/or high density lipoprotein levels and/or modulating the LDL:HDL ratio, and for the treatment of lipodystrophy or dyslipidemia. These compounds are distinct from GPI-anchors disclosed in the prior art as these GPI-anchors are protein linked and are not biologically active.

NOVEL DISACCHARIDES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

EBURNAMONINE DERIVATIVES, THEIR PREPARATION AND MEDICINAL PRODUCTS CONTAINING SUCH SUBSTANCES

Nouveaux dérivés de la vincamone. Ils sont caractérisés par la formule générale : New derivatives of vincamone. They are characterized by the general formula: