СИНТЕЗ β-L-2'-ДЕЗОКСИНУКЛЕОЗИДОВ

FIELD: chemistry. ^ SUBSTANCE: invention relates to the method of producing 2'-desoxy--L-thymidine, which involves reacting 5'-O-trityl- or 5'-O-dimethoxytrityl- substituted 2,2' -anhydro-1 --L- arabinofuranosylthymine with a reducing agent RedAl and a complexing agent 15-crown-5-ether in a polar solvent 1,2-dimethoxyethane (DME) or tetrahydrofuran, obtaining 5'-O-trityl- or 5'-O-dimethoxytrityl- substituted 2,2'-desoxy--L-thymidine, subjected to protection removal if necessary. The invention also relates to the method of producing 2'-desoxy--L-thymidine, which involves reacting L-arabinose with cyanamide with subsequent reaction of the intermediate product - L-arabinofuranosylaminooxazoline - with a cycling or condensing agent, forming 2,2' -anhydro-1--L-arabinofuranosylthymine; reaction of the latter with a reducing agent RedAl and a complexing agent 15-crown-5-ether in a polar solvent 1,2-dimethoxyethane (DME) or tetrahydrofuran, obtaining 2'-desoxy--L-thymidine, where L-arabinofuranosylaminooxazoline can be protected by trityl or dimethoxytrityl in position 5' before or after reaction with the cycling or condensing agent; and protection removal of optionally protected 2'-desoxy--L-thymidine, if this is necessary or desired. Use in the given methods of such a reducing agent as Red-Al, and such a complexing agent as 15-crown -5-ether, causes a reaction of intramolecular protection and production of the required nucleoside product with good output. ^ EFFECT: compound is of great importance as an antiviral or antineoplastic preparation. ^ 13 cl, 29 dwg, 28 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 361 875 (13) C2 (51) МПК C07H 1/00 (2006.01) C07H 19/073 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2006102518/04, 30.06.2004 (24) Дата начала отсчета срока действия патента: 30.06.2004 (73) Патентообладатель(и): АЙДЕНИКС ( ...

СИНТЕЗ L-2-ДЕЗОКСИНУКЛЕОЗИДОВ

... 1. Способ получения промежуточного продукта формулы (B), включающий восстановление лактона формулы (A) с использованием Red-Al с получением соединения формулы (B) 2. Способ по п.1, в котором защитными группами кислорода являются группы толуоила. 3. Способ получения промежуточного продукта формулы (F), включающий a) взаимодействие необязательно защищенного спирта формулы (C) с мезилхлоридом с получением мезилата формулы (D), где P, P' и P" означают водород, алкил или подходящую защитную группу кислорода, b) восстановление соединения формулы (D), чтобы получить соединение формулы (E), ; и c) при необходимости, удаление защиты с получением соединения формулы (F) 4. Способ получения промежуточного продукта формулы (F), включающий a) взаимодействие необязательно защищенного спирта формулы (C') с мезилатом с получением мезилата формулы (D') где P, P' и P" означают водород, алкил или подходящую защитную группу кислорода, b) восстановление соединения формулы (D') с получением соединения формулы ...

КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ДУБИЛЬНЫЕ КИСЛОТЫ И ИХ ПРИМЕНЕНИЕ

Группа изобретений относится к фармацевтической промышленности, а именно к средствам, ингибирующим активность оксидазы D-аминокислоты. Композиция для ингибирования активности оксидазы D-аминокислоты (DAAO), содержащая (i) дубильную кислоту или ее фармацевтически приемлемую соль и (ii) и фармацевтически приемлемый носитель, где дубильная кислота содержит 4,5,6,7,8,9,10,11 или 12 галлоильных групп и где дубильная кислота составляет по меньшей мере 90% по массе всех дубильных кислот, содержащихся в композиции. Способ лечения заболевания, связанного с активностью оксидазы D-аминокислоты (DAAO), которым является ожирение, гиперлипидемия, диабет или расстройство центральной нервной системы (ЦНС), включающий введение индивидууму, нуждающемуся в этом, эффективного количества композиции. Способ получения композиции дубильной кислоты, включающий: (i) получение чернильных орешков из растения; (ii) измельчение чернильных орешков с получением порошка чернильных орешков; (iii) экстракцию порошка чернильных ...

СОЕДИНЕНИЯ, КОМПОЗИЦИИ И СПОСОБЫ ЗАЩИТЫ ЗДОРОВЬЯ ГОЛОВНОГО МОЗГА ПРИ НЕЙРОДЕГЕНЕРАТИВНЫХ РАССТРОЙСТВАХ

... 1. Способ, включающий этап введения субъекту количества Пуникалина (Punicalin), Пуникалагина (Punicalagin), Педункулагина (Pedunculagin), Теллимаграндина (Tellimagrandin), Корилагина (Corilagin), Гранатина A (Granatine А), Гранатина Б (Granatine В), Терминалина (Terminalin), Галлагилдилактона (Gallagyldilactone), Соединения А или соединения Формулы I:или его фармацевтически приемлемой соли, биологически активного метаболита, сольвата, гидрата, пролекарства, энантиомера или стереоизомера;где независимо для каждого случаяХ представляет собойили; икаждый из R, Rи Rнезависимо представляет собой водород, алкил, аралкил, алкилкарбокси или сахар; илиRпредставляет собой водород, алкил, аралкил, алкилкарбокси,или сахар, Rпредставляет собой водород или, и Rпредставляет собой; илиRпредставляет собой водород, алкил, аралкил, алкилкарбокси или сахар, а Rи Rвместе представляют собой2. Способ по п.1, отличающийся тем, что Х представляет собой3. Способ по п.1, отличающийся тем, что X представляет собой4 ...

Способ получения производных глюкозамина

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДДЫ С ГЛ10КОЗАМИНА общей формулы СНзОН i-о (О V-OH Ho)|-f / ira-co-Ei Бг-сн С о -IJH- CJi- CO-liH- Си- (СНз 12 5 (В) (О)(L) где R, - Cy-Cj-алкил или фенил; RZ - водород или С -С -алкил; R - водород, С -Сд-алкил или оксиметил; R. карбоксил , метоксикарбонил , карбамоил, N-(C -C2-алкил )-карбамоил, К-бензил- или N-карбамоилметилкарбамоил; R- карбоксил , метоксикарбонил , карбамоил или Н-метилкарбамоил , при условии, что алкил R содержит более 1 атома углерода, если Rj метил или водород, а R и Rg карб оксил, отличающийся тем, что соединение общей формулы 0-1 /О i СО G у «(I-Rl Бг-ш в, СО-Ш1-СЫ-СО-1 Н-СН-(СН2) (D) (Ь) (D) где имеют указанные значения; 05 R - С -С -алкилиден или О 00 СJ-C,-циклоалкнлиден, обрабатывают кислым ионообменником или трифторуксусной кислотой в течение 10-25 ч при комнатной температуре в воде, тетрагидрофуране и/или хлористом метилене.

Verfahren zur Wiedergewinnung von Organozinnestern aus diese enthaltenden Reaktionsgemischen und Wiederverwendung der wiedergewonnenen Organozinnverbindungen.

VERFAHREN ZUR VERBESSERUNG DER REINHEIT UND AUSBEUTE VON SUCRALOSE

Pharmaceutical compositions having appetite suppressant activity

PREPARATION OF FLOURO-COMPOUNDS

Sucralose pentaester production

Intermediates in the synthesis of appetite suppressant steroid glycosides

Steroidal glycosides

A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).

3-deoxy-ribofuranosyl derivatives

Compounds of the formula where X is halogen and R is an acyl radical may be obtained by reacting a compound of the formula wherein R11 is an alkyl group, with a halogenating system capable of producing a halogen anion in the presence of a strong acid under anhydrous conditions, suitably in the presence of an inert organic solvent. The halogenating agent may be a hydrogen or thionyl halide (both of which may also function as the strong acid) or a metal halide.

BBM-1675, A new antitumor antibiotic complex

An antibiotic complex designated herein as BBM-1675 complex is produced by fermentation of certain novel strains of Actinomadura verrucosospora. The complex may be separated into two major components, BBM-1675A1 and A2, and four minor components, BBM-1675 A3, A4, B1 and B2, and such components exhibit both antimicrobial activity and antitumor activity.

Low temperature, single solvent process for the production of sucrose-6-ester

Methods and compositions for treating hyperglycemic, hyperlipidemic, or hyperinsulinemic disorders

Process for the production of sucrose-6-ester

ANTHRACYCLINE GLYCOSIDES

... 1529992 Daunorubicin derivatives SOC FARMACEUTICI ITALIA SpA 8 July 1977 [13 July 1976] 28985/76 Heading C2C Compounds of the general formula (R 1,3 = H, R 2 = H, halogen, Me, OMe; R 1 , 2 = H, R 3 = C 1-4 alkoxy; or R 2 = H, R 1 = R 3 = halogen, Me, OMe) and their 14-hydroxy derivatives and hydrochlorides are prepared by reacting the corresponding aglycone with 3,6-dideoxy - 2,4 - bis(p - nitrobenzoyl) - 3 - trifluoroacetamido - - L - talohexopyranosyl bromide, followed by removal of the protecting groups and, optionally, bromination and hydrolysis and/or salt formation. The compounds are antimitotics. The bromosugar is prepared by reacting 3- amino - 3,6 - dideoxy - L - talohexose hydrochloride with trifluoroacetic anhydride, removing the O-trifluoroacetyl groups, esterifying with p-nitrobenzoyl chloride and treating the product with hydrogen bromide.

Novel nitrosourea compounds

Novel nitrosourea compounds are provided which possess a high level of inhibitory activity against leukemia and tumors with a low toxicity and which are therefore useful for pharmaceutical purposes. The compounds have the chemical structure: wherein DIFFERENCE represents a single bond which may be in the alpha - or beta -position and are prepared by nitrosating a urea compound of the formula: with a nitrosating agent in a manner known per se.

Pharmaceutical compositions having appetite suppressant activity comprising an extract from a plant of the genus trichocaulon or hoodia

A pharmaceutical composition for use in suppressing appetite comprising as an active ingredient an extract obtained from a plant of the genus Trichocaulon or Hoodia. The invention further teaches a process for obtaining an extract having appetite suppressant activity. The invention also extends to the use of such extracts for the manufacture of medicaments having appetite suppressant activity and for treating and preventing obesity.

Intermediate and process for preparing of beta-anomer enriched 2'deoxy, 2',2'-difluoro-D-ribofuranosyl nucleosides.

Pharmaceutical compositions having appetite suppressant activity

A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).

Pharmaceutical compositions having appetite suppresant activity

Purine derivatives.

The present invention relates to the compounds of the formula (i)and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, composites containing, and the uses of such compounds as adenosine a2a receptor agonists.

Pharmaceutical compositions having appetie suppressant activity.

A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).

Intermediate and process for prepaing of beta-anomer inriched 21deoxy, 21,21-difluoro-D-ribofuranosyl nucleosides

Purine derivatives.

Sialyl lex analogues as inhibitors of cellular adhesion

Method of preparation of nitrogenized food.

Pharmaceutical compositions having appetite suppressant activity

Process for the preparation of monosaccharide O-esters presenting of the groupings ethers.

Biologically active compositions.

Pharmaceutical compositions having appetite suppressants activity

Pharmaceutical compositions having appetite suppressants activity

Intermediate and process for prepaing of beta-anomer inriched 21deoxy, 21,21-difluoro-D-ribofuranosyl nucleosides

Pharmaceutical compositions having appetite suppresant activity

Pharmaceutical compositions having appetite suppressants activity

Pharmaceutical compositions having appetite suppressants activity

Purine derivatives

Intermediate and process for prepaing of beta-anomer inriched 21deoxy, 21,21-difluoro-D-ribofuranosyl nucleosides

VERFAHREN ZUR HERSTELLUNG DES NEUEN ANTITUMORANTIBIOTIKUM-KOMPLEXES BBM-1675

CONNECTIONS AND PHARMACEUTICAL COMPOSITIONS WITH APPETITE-SUPPRESSING ACTIVITY

VERFAHREN ZUR HERSTELLUNG VON NEUEN KOHLENHYDRAT-ESTERN DER ACETYLSALICYLSAEURE

VERFAHREN ZUR HERSTELLUNG VON NEUEN O-ESTERN VON MONOSACCHARIDEN

PROCEDURE FOR THE PRODUCTION OF NEW PROTEIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW SACCHAROSE AZIDE OF DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW O-ESTERS OF MONO SACCHARIDES

WISHING CASE WITH NATRIUMSULFIT SHIFTING OF PARTIALESTER FROM MULTI-VALUED ALCOHOLS, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS SKIN-FRIENDLY, NOT IONOGENE AND/OR ANION-ACTIVE SURFACE-ACTIVE SUBSTANCES.

PRODUCTION OF NUCLEOSIDES.

Paper carriage switching mechanism with different switching width for typewriters.

PROCEDURE FOR the PRODUCTION OF 2-CHLOR-2-DEOXY-SACCHARIDEN AND SOME 2-CHLOR-2-DEOXY-SACCHARIDE.

PROCEDURE FOR THE SYNTHESIS OF TUBING SUGAR DERIVATIVES BY A REGIOKSELEKTIVE REACTION.

TANNINEXTRAHIERUNG

PURINDERIVATE

POLYCYCLI DERIVATIVES TO THE CHANGE OF THE OPTICAL CHARACTERISTICS AND ÄTZBESTÄNDIGKEITSEIGNENSCHAFTEN

PLANT EXTRACTS WITH APPETITE-SUPPRESSING ACTIVITY

D-PENTOFURANOSE-DERIVATIVES AND PROCEDURES FOR YOUR PRODUCTION

PROCEDURE FOR the PRODUCTION OF WITH ALPHA ANOMEREN ENRICHMENT 1-HALOGEN-2-DEOXY-2,2-DIFLUOR-D RIBOFURANOSYL DERIVATIVES

Process for improving sucralose purity and yield

Chemical derivatives of jasmonate, pharmaceutical compositions and methods of use thereof

Process for improving sucralose purity and yield

Synthesis of decitabine

A method for producing a -enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula (I); and b) quenching the reaction mixture of step a) with a base. The -enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.

Process for improving sucralose purity and yield

PROCESS FOR IMPROVING SUCRALOSE PURITY AND YIELD

METHODS AND COMPOSITIONS FOR TREATING DIABETES MELLITIS

Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics

The invention relates to derivatives of morphine-6-glucuronide having formula (I) wherein R1 is a 5-membered heteroaromatic group optionally substituted by one or more substituents selected from among halogen atoms and (C-C)alkyl, halogen, hydroxyl, halo(C-C)alkyl, halo(C-C)alkyloxy, (C-C)alkyloxy, aryl(C-C)alkyl and aryl groups, said aryl group being optionally substituted by one or more groups selected from among (C-C)alkyl, halo(C-C)alkyl, hydroxyl and (C-C)alkyloxy groups, in the form of a base or acid addition salt, as well as in hydrate or solvate form. The invention also relates to the preparation method thereof and to the use of same in therapeutics.

4-(4-(4-phenylureido-naphthalen-1-yl)oxy-pyridin-2-yl)amino-benzoic acid derivative as p38 kinase inhibitor

There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

4-(4-(4-phenylureido-naphthalen-1-yl)oxy-pyridin-2-yl)amino-benzoic acid derivative as p38 kinase inhibitor

There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Diaryl urea derivatives as p38 kinase inhibitors

There are provided compounds of formula I, wherein R ...

Substituted pyrrolidine-2-carboxamides

There are provided compounds of the formula (I) wherein X, Y, Z, R ...

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

Gallotannins and ellagitannins as regulators of cytokine release

COMPOUND CONTAINED IN BLUE ROSE

Disclosed is a novel compound contained in blue rose. This novel compound, which is contained in blue rose, has a chemical structure represented by general formula (I): [see Chemical Formula 1] [wherein R1 is a group as set forth in claim 1; and R2 represents -OH, or R1 and R2 together form -O-]. Also disclosed are a rose plant containing the aforesaid compound, and a part of the same.

BBM-1675, A NEW ANTITUMOR ANTIBIOTIC COMPLEX

A novel antibiotic complex designated herein as BBM-1675 complex is produced by fermentation of certain novel strains of Actinomadura verrucosospora. The complex may be separated into two major components, BBM-1675 A1 and A2, and four minor components, BBM-1675 A3, A4, B1 and B2, and such components exhibit both antimicrobial activity and antitumor activity.

ANTITUMOR GLYCOSIDES, THEIR PREPARATION, USE AND COMPOSITIONS THEREOF

Anthracycline glycosides of the formula I I wherein R is hydrogen or hydroxy, one of R1 and R2 is methyl and the other of R1 and R2 is hydroxy, and pharmaceutically acceptable acid addition salts thereof, which are useful in treating certain mammalian turmors, are prepared by condensing daunomycinone with certain novel sugars in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form the corresponding protected glycosides from which the protecting groups are removed. This gives the compounds wherein R is hydrogen. The former are converted to the corresponding hydroxyl compounds by treatment with bromine and sodium formate.

PROCESS FOR SYNTHESIZING SUCROSE DERIVATIVES BY REPROCESS FOR SYNTHESIZING SUCROSE DERIVATIVES BY REGIOSELECTIVE REACTION GIOSELECTIVE REACTION

Sucrose is reacted with a 1,3-di(hydrocarbyloxy)-1,1,3,3-tetra(hydrocarbyl)distannoxane to produce a 1,3-di-(6-0-sucrose)-1,1,3,3-tetra(hydrocarbyl)distannoxane, which can be acylated to produce a sucrose-6-ester.

PROCESS FOR IMPROVING SUCRALOSE PURITY AND YIELD

This invention relates to processes for purifying sucralose by the use of an initial non-crystallization purification procedure followed by three or more sequential crystallization steps and recycle of the mother liquor remaining from each crystallization step to the feed of another crystallization or purification step. This invention also relates to sucralose compositions as well as compositions comprising the sucralose compositions of the present invention. These compositions may be highly pure and have a superior taste profile.

CONJUGATES OF A PHARMACEUTICAL AGENT AND A MOIETY CAPABLE OF BINDING TO A GLUCOSE SENSING PROTEIN

The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration.

TRITERPENE SAPONINS, METHODS OF SYNTHESIS, AND USES THEREOF

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

DIARYL UREA DERIVATIVES AS P38 KINASE INHIBITORS

There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

SYNTHETIC HEPARIN PENTASACCHARIDES

Preparation of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.

SYNTHETIC HEPARIN PENTASACCHARIDES

Preparation of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.

PESTICIDAL COMPOSITIONS

The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.

BICYCLIC DERIVATIVES OF MORPHINE-6-GLUCURONIDE, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS

La présente invention a pour objet les composés répondant à la formule (I) dans laquelle : R1 représente un atome d'hydrogène ou un groupe (C1-C4)alkyle, R2 représente un groupe hydroxyle, un groupe thiol, un groupe (C1-C4)alkyloxy ou un groupe thio(C1-C4)alkyle, et n est un nombre entier égal à 1 ou 2, à l'état de base ou de sel d'addition à un acide ainsi qu'à l'état d'hydrate ou de solvate. La présente invention vise également leur procédé de préparation et leur application en thérapeutique.

PROCESS FOR MAKING 5-AZACYTOSINE NUCLEOSIDES AND THEIR DERIVATIVES

A process of efficiently synthesizing a 5-azacytosine nucleoside of formula I: (see formula I) wherein R1 is hydrogen, hydroxy or halogen; R2 is hydrogen or halogen, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose in the presence of a less than one molar equivalent sulfonic acid catalyst with respect to the protected D-ribofuranose. This process is efficient and amenable to manufacturing scale synthesis. It also does not require an aqueous workup or addition of a large amount of catalyst." ...

SUCROSE-6-ESTER PRODUCTION PROCESS

SUCROSE-6-ESTER PRODUCTION PROCESS Process which comprises reacting sucrose with a di(hydrocarbyl)tin oxide in an inert organic reaction vehicle with removal of water for a period of time and at a temperature sufficient to produce a 1,3-di-(6-O-sucrose)-1,1,3,3-tetra(hydrocarbyl)distannoxane. NOR-8 ...

PROCESS FOR RECOVERY OF ORGANOTIN ESTERS FROM REACTION MIXTURES CONTAINING THE SAME AND RE-USE OF THE RECOVERED ORGANOTIN COMPOUNDS

PROCESS FOR RECOVERY OF ORGANOTIN ESTERS FROM REACTION MIXTURES CONTAINING THE SAME AND RE-USE OF THE RECOVERED ORGANOTIN COMPOUNDS A process which comprises extracting 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxane from a mixture containing 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxaane, a sucrose-6-ester, and polar aprotic solvent, which process comprises the steps of: (a) contacting said mixture, in the presence of a small amount of water, with an organic solvent that is substantially immiscible with water to form thereby an extraction mixture, wherein the amount of water employed is sufficient to cause efficient partitioning of said 1,3diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxane from a first phase comprising said polar aprotic solvent into second phase comprising said organic solvent; (b) agitating the extraction mixture for a period of time and at a temperature sufficient to form thereby a twophase mixture wherein the preponderance of the 1,3diacyloxy-1,1,3,3-tetra ...

SIALYL LEX ANALOGUES AS INHIBITORS OF CELLULAR ADHESION

The present invention relates to analogues of Sialyl Lewisx that inhibit cellular adhesion between a selectin receptor and cells that express sialyl Lex on their surfaces, as well as methods and compositions using the same, intermediates and methods for the preparation of the cellular adhesion inhibitor compounds and their intermediates. A contemplated or inhibitor compound has the 2-N-acetyl moiety of the GlcNAc with YR1 wherein Y is C(O), SO2, HNC(O) or SC(O) and R1 is aryl, substituted aryl, or phenyl C1-C3 alkylene moieties.

PROCESS FOR PREPARING ACYLATED GLYCOSYL FLUORIDES

HOE 90/F 196 Process for preparing acylated glycosyl fluorides Process for preparing acylated glycosyl fluorides by fluorination of saccharides, which are at least partially O-acylated, in anhydrous hydrogen fluoride, characterized in that the corresponding carboxylic anhydride is added to the hydrogen fluoride before the reaction and the reaction solution is processed after reaction times of at most 60 minutes.

IMPROVED SUCROSE-6-ESTER PROCESS

There is described a process which comprises passing vapors of a solvent capable of removing water by codistillation through a reaction mixture containing (a) a polar aprotic solvent and (b) sucrose and a 1,3-diacyloxy-1,1,3, 3-tetra-(hydrocarbyl)distannoxane and/or the reaction product of sucrose and a 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxane, in sufficient quantity and for a period of time sufficient to remove substantially all of the water in said reaction mixture by codistillation. In a particular aspect, there is described a process which comprises: (1) preparing a first reaction mixture comprising sucrose and a polar aprotic solvent, and optionally heating said first reaction mixture by passing vapors of a second solvent capable of removing water by codistillation through said first reaction mixture; (2) adding a 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)-distannoxane to said first reaction mixture to form a second reaction mixture; (3) passing vapors of a second solvent ...

Verfahren zur Herstellung eines fettlöslichen Tannin-Abkömmlings.

Verfahren zur Herstellung von Ketosidopurinen

Verfahren zur Herstellung geschmackfreier Antihistaminika

Verfahren zur Herstellung von Estern der Naphthensäuren mit Di- oder Trisacchariden

Verfahren zur Herstellung von Halogenribofuranosiden

Procédé de préparation d'esters d'hydrates de carbone de l'acide salicylique, utilisables comme analgésiques

Verfahren zur Herstellung von 2-C-Methyl-nukleosiden

O-esters of monosaccharides possessing ether - gps

O-esters of monosaccharides with optionally substd. 2-R-O benzoic acid, possessing at least one saccharide OH gp. esterified by a 2-R-O benzoyl radical where R = H, acyl or optionally substd. hydrocarbon, and at least one saccharide gp. etherified by an optionally substd. hydrocarbon radical, wherein further saccharide hydroxy gps. can be free or esterified or etherified, and salts of compds. of this type possessing salt-forming gps.

Verfahren zur Herstellung von Hexafuranoseverbindungen

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

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

Supercooling promoting agent

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

Triterpene saponins, methods of synthesis, and uses thereof

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

TANNIN INHIBITORS OF HIV

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

Maple tree-derived products and uses thereof

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

TREHALOSE DERIVATIVES, PREPARATION METHOD AND USES THEREOF

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

ANTI-CHOLESTEROLEMIC COMPOUNDS AND METHODS OF USE

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

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

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

METHOD FOR PRODUCING a-HALO-TETRAACYL-GLUCOSE

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

TRITERPENE SAPONIN ANALOGUES

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

Method for synthesizing sucrose-6-ester

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

METHOD FOR PRODUCING ALPHA-HALO-TETRAACYL-GLUCOSE

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

CONJUGATED ANTISENSE COMPOUNDS AND THEIR USE

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

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

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

Triterpene saponins, methods of synthesis and uses thereof

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

Compositions Containing Tannic Acids and Uses Thereof

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

Kinase inhibitors

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

DIARYL TREHALOSE COMPOUNDS AND USES THEREOF

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

NOVEL CONJUGATES OF A PHARMACEUTICAL AGENT AND A MOIETY CAPABLE OF BINDING TO A GLUCOSE SENSING PROTEIN

The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration. 1. A conjugate of formula (I){'br': None, 'sub': 1', 'm', '1', 'o', '2', 'p', '2', '3', '3', '4, 'P-[L]-[A]-[L]-[A]-[L]-[A]-[L]-S\u2003\u2003(I)'}wherein P is an insulin or an insulinotropic peptide,{'sub': 1', '2, 'Land Lare independently of each other a linker having a chain length of 1-25 atoms,'}{'sub': '3', 'Lis a linker having a chain length of 2 or 3 atoms,'}{'sub': '4', 'and Lis a linker having a chain length of 1, 2 or 3 atoms,'}{'sub': '1', 'A, is a 5 to 6 membered monocyclic ring or a 9 to 12 membered bicyclic ring, wherein each ring is independently a saturated, unsaturated, or aromatic carbocyclic or heterocyclic ring and wherein each ring may carry at least one substituent,'}{'sub': 2', '3, 'Aand Aare independently of each other a 5 to 6 membered monocyclic ring or a 9 to 12 membered bicyclic ring, wherein each ring is independently an aromatic carbocyclic or aromatic heterocyclic ring and wherein each ring may carry at least one substituent,'}S is a sugar moiety which binds to the insulin independent glucose transporter GLUT1, andm, o, and p are independently of each other 0 or 1,or a pharmaceutically acceptable salt or solvate thereof.2. The conjugate of formula (I) of claim 1 ,{'br': None, 'sub': 1', 'm', '1', 'o', '2', 'p', '2', '3', '3', '4, 'P-[L]-[A]-[L]-[A]-[L]-[A]-[L]-S\u2003\u2003(I)'}wherein P is an insulin or an insulinotropic peptide,{'sub': 1', '2, 'Land Lare independently of each other a linker having a chain length of 1-25 atoms,'}{'sub': '3', 'Lis a linker having a chain length of 2 or 3 atoms,'}{'sub': '4', 'and Lis a linker having a chain length of 1, 2 or 3 atoms,'}{'sub': '1', 'A, is a 5 to 6 membered monocyclic ring or a 9 to 12 membered bicyclic ring, wherein each ring is independently a ...

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

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

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

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

Compounds reducing the production of sorbitol in the eye and methods of using the same

Methods of inhibiting the progression of or treating secondary complications of diabetes, especially a diabetic eye disease, in a mammal by inhibiting the production of sorbitol in the mammal. Small molecule inhibitors of sorbitol production in the eye useful in the methods of the invention and pharmaceutical compositions containing the compounds, and methods of using the same.

COMPOSITIONS CONTAINING TANNIC ACIDS AND USES THEREOF

Compositions (e.g., pharmaceutical compositions, nutraceutical compositions or medical food compositions) comprising tannic acids, particularly tannic acids which are D-amino acid oxidase inhibitor with superior potency, purity and safety profile; and uses thereof for treating CNS disorder and obesity disorders including diabetes, hyperglycemia, hyperlipidemia or hypercholesterolemia. 1. A composition , comprising (i) a mixture of tannic acids or an acceptable salt thereof , and (ii) a carrier , wherein the composition is substantially free of tannic acids having less than four galloyl moieties.2. The composition of claim 1 , wherein ≥98% of the tannic acids in the composition have 4-12 galloyl moieties.3. The composition of claim 1 , wherein ≥97% of the tannic acids in the composition have 5-12 galloyl moieties.4. The composition of claim 1 , wherein ≥90% of the tannic acids in the composition have 6-12 galloyl moieties.5. The composition of claim 1 , wherein ≥60% of the tannic acids in the composition have 8-12 galloyl moieties.6. The composition of claim 1 , wherein in the composition claim 1 , about 10-20% of the tannic acids have 5 galloyl moieties claim 1 , about 15-25% of the tannic acids have 6-7 galloyl moieties claim 1 , and about 55-65% of the tannic acids have 8-12 galloyl moieties.7. The composition of claim 1 , wherein the composition is a pharmaceutical composition claim 1 , a nutraceutical composition claim 1 , a health food claim 1 , or a medical food.8. The composition of claim 7 , wherein the composition is a tablet claim 7 , a capsule claim 7 , a soft chew claim 7 , or gel.9. A method for inhibiting D-amino acid oxidase (DAAO) in a subject claim 1 , comprising administering to a subject in need thereof an effective amount of the composition of .10. The method of claim 9 , wherein the subject is a human patient having claim 9 , suspected of having claim 9 , or at risk for a central nervous system (CNS) disorder or a disorder associated with ...

Phosphorylation of products for flame retardant applications

Disclosed herein are flame retardant materials, and in particular materials and processes for phosphorylating materials for flame retardant applications

Glucose responsive insulin delivery compositions and methods

Disclosed herein is a glucose-responsive insulin delivery system based on the interaction between the glucose-modified insulin and glucose transporters (GLUTs) on erythrocytes (or red blood cells, RBCs). After being conjugated with glucose, insulin can efficiently bind to RBC membranes. The binding is reversible in the setting of hyperglycemia, resulting in fast release of insulin and subsequent drop of blood glucose (BG) level in vivo. In some embodiments, the delivery vehicle can include: 1) intravenously injectable polymeric nanoparticles (˜100 nm in diameter) coated with RBC membrane and loaded with glucose-modified insulin and/or 2) painless microneedle (MN) patches loaded with the complex of GLUT and glucose-modified insulin.

TRITERPENE SAPONIN ANALOGUES

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases. 3. The pharmaceutical composition according to claim 2 , wherein the antigen is associated with a bacteria or virus.4BorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. The pharmaceutical composition according to claim 3 , wherein the antigen is associated with a bacterial or virus causing a disease selected from the group consisting of Hepatitis B claim 3 , pneumococcus claim 3 , diphtheria claim 3 , tetanus claim 3 , pertussis claim 3 , or Lyme disease including the closely related spirochetes of the genus such as claim 3 , claim 3 , and5. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with Hepatitis B virus.6. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with pneumococcus bacterium.7Corynebacterium diphtheria. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with bacterium.8Clostridium tetani. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with bacterium.9Bordetella pertussis. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with bacterium.10BorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. The pharmaceutical composition according to claim 4 , wherein the antigen is an antigen associated with a bacterium causing Lyme disease or a spirochete of the genus selected from the group consisting of claim 4 , and12. The method according to claim 11 , wherein the antigen is an antigen associated with a bacteria or a virus.13BorreliaB. burgdorferi, B. garinii, B. ...

KINASE INHIBITORS

There are provided compounds of formulas III and VIIa: 2. A compound of:{'b': '24', '(a) formula III, or a salt or protected derivative thereof, as claimed in claim , wherein said compound or protected derivative is'}methyl 4-((4-((4-aminonaphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoate ormethyl 4-((4-((4-((tert-butoxycarbonyl)amino)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoate; or{'b': '24', '(b) formula VIIa, or a salt or protected derivative thereof, as claimed in claim , wherein said compound is methyl 4-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)-phenyl)ureido)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoate.'} This invention relates, inter alia, to compounds which are antiinflammatory agents (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), for example the alpha kinase sub-type thereof; Syk kinase; and the Src family of tyrosine kinases). The invention also relates to the use of such compounds in therapy, including in mono- and combination therapies, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung (such as asthma and chronic obstructive pulmonary disease (COPD)), eye (such as uveitis or keratoconjunctivitis sicca (dry eye disease, also known as xerophthalmia)) and gastrointestinal tract (such as Crohn's disease and ulcerative colitis).The listing or discussion of an apparently prior-published document in this specification should not necessarily be taken as an acknowledgement that the document is part of the state of the art or is common general knowledge.Four p38 MAPK isoforms (alpha, beta, gamma and delta respectively) have been identified, each displaying different patterns of tissue expression. The p38 MAPK alpha and beta isoforms are found ubiquitously throughout the body, are present in many different cell types and are inhibited by a number of ...

Triterpene saponin synthesis, intermediates and adjuvant combinations

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases.

TRITERPENE SAPONINS, METHODS OF SYNTHESIS AND USES THEREOF

The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation. 136-. (canceled)39. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.40. The pharmaceutical composition of further comprising an immunologically effective amount of an antigen.41. (canceled) The present application is a continuation of U.S. patent application Ser. No. 13/613,312, filed Sep. 13, 2012, which is a divisional of and claims priority under 35 U.S.C. §120 to U.S. patent application U.S. Ser. No. 12/420,803, filed Apr. 8, 2009, which claims priority under 35 U.S.C. §119(e) to U.S. provisional application U.S. Ser. No. 61/043,197, filed Apr. 8, 2008, each of which is incorporated herein by reference.This invention was made with United States Government support under grant GM58833 awarded by the National Institutes of Health. The United States Government has certain rights in the invention.The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of infectious diseases and cancer.Saponins are glycosidic compounds that are produced as secondary metabolites of steroids and triterpenes. They are widely distributed among plant species and ...

Steviol Glycosides, Their Compositions and Their Purification

The present invention relates generally to steviol glycosides, as well as compositions comprising such steviol glycosides. The present invention further extends to methods of preparing and purifying such steviol glycosides and methods for enhancing the flavor or sweetness of consumables using these steviol glycosides and compositions. The present invention extends to consumables comprising steviol glycosides, where the such steviol glycosides are present in a concentration at or below their sweetness recognition threshold, and wherein such steviol glycosides enhance the sweetness of the consumable. 187.-. (canceled)90steviaStevia rebaudiana. The composition of claim 89 , further comprising steviol glycosides selected from the group consisting of a commercially available extract; steviol glycosides prepared from plant material of the Bertoni plant claim 89 , the by-product of another isolation and purification processes of steviol glycosides claim 89 , stevioside claim 89 , rebaudioside A claim 89 , rebaudioside C claim 89 , dulcoside A claim 89 , rubusoside claim 89 , steviolbioside claim 89 , rebaudioside B claim 89 , rebaudioside D claim 89 , rebaudioside F claim 89 , and combinations thereof.91. The composition of claim 89 , further comprising at least one additional sweetener.92. The composition of claim 91 , wherein the at least one additional sweetener is selected from the group consisting of sucrose claim 91 , fructose claim 91 , glucose claim 91 , high fructose corn syrup claim 91 , xylose claim 91 , arabinose claim 91 , rhamnose claim 91 , erythritol claim 91 , xylitol claim 91 , mannitol claim 91 , sorbitol claim 91 , inositol claim 91 , AceK claim 91 , aspartame claim 91 , neotame claim 91 , sucralose claim 91 , saccharine claim 91 , naringin dihydrochalcone (NarDHC) claim 91 , neohesperidin dihydrochalcone (NDHC) claim 91 , rubusoside claim 91 , mogroside IV claim 91 , siamenoside I claim 91 , mogroside V claim 91 , trilobatin and combinations thereof.93 ...

ALLOSTERIC MODULATORS OF FACTOR XIa AS ANTICOAGULANT AGENTS

Compounds which allosterically modulate and/or inhibit factor XIa activity are provided, as are methods of their use. These compounds include i) sulfated gallolyl glucosides, ii) sulfated quinazolinones, and iii) sulfated inositol analogs. The compounds used as anticoagulant agents.

KINASE INHIBITORS

There are provided compounds of formula IIb, 2. A compound as claimed in claim 1 , wherein LGrepresents phenoxy.4. A compound as claimed in claim 3 , wherein R represents a Calkyl group.5. A compound as claimed in claim 1 , wherein the carboxyl moiety of Ris protected as an ethyl or methyl ester.6. A compound as claimed in claim 1 , wherein the carboxyl moiety of Ris protected as a methyl ester. This invention relates, inter alia, to compounds which are antiinflammatory agents (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), for example the alpha kinase sub-type thereof; Syk kinase; and the Src family of tyrosine kinases). The invention also relates to the use of such compounds in therapy, including in mono- and combination therapies, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung (such as asthma and chronic obstructive pulmonary disease (COPD)), eye (such as uveitis or keratoconjunctivitis sicca (dry eye disease, also known as xerophthalmia)) and gastrointestinal tract (such as Crohn's disease and ulcerative colitis).The listing or discussion of an apparently prior-published document in this specification should not necessarily be taken as an acknowledgement that the document is part of the state of the art or is common general knowledge.Four p38 MAPK isoforms (alpha, beta, gamma and delta respectively) have been identified, each displaying different patterns of tissue expression. The p38 MAPK alpha and beta isoforms are found ubiquitously throughout the body, are present in many different cell types and are inhibited by a number of previously described small molecular weight compounds. Early classes of inhibitors were highly toxic due to the broad tissue distribution of these isoforms which resulted in off-target effects of the compounds. Some of the more recently identified inhibitors show improved ...

SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSYL)CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME

A compound represented by a formula [1D] as shown below (wherein R 1A , R 1B , R 2A , R 2B , R 3A and R 3B represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.

TRITERPENE SAPONIN ANALOGUES

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases. 8. The method according to claim 6 , further comprising:{'sup': '4', '(c) reacting the product of step (b) or a compound obtained after modifying the product of step (b) with R—OH.'}9. The method according to claim 8 , wherein R—OH is HO—C(O)—(CH)—C(O)—OR claim 8 , wherein Ris independently hydrogen or an oxygen protecting group selected from the group consisting of alkyl ethers claim 8 , benzyl ethers claim 8 , silyl ethers claim 8 , acetals claim 8 , ketals claim 8 , esters claim 8 , carbamates claim 8 , and carbonates.10. The method according to claim 9 , wherein Ris H.11. The method according to claim 9 , wherein Ris Bn.13BorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. A pharmaceutical composition comprising the compound according to and an immunologically effective amount of an antigen associated with a bacteria or virus causing a disease selected from the group consisting of Hepatitis B claim 1 , pneumococcus claim 1 , diphtheria claim 1 , tetanus claim 1 , pertussis claim 1 , or Lyme disease including the closely related spirochetes of the genus such as claim 1 , claim 1 , and14BorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. A pharmaceutical composition comprising the compound according to and an immunologically effective amount of an antigen associated with a bacteria or virus causing a disease selected from the group consisting of Hepatitis B claim 2 , pneumococcus claim 2 , diphtheria claim 2 , tetanus claim 2 , pertussis claim 2 , or Lyme disease including the closely related spirochetes of the genus such as claim 2 , claim 2 , and15BorreliaB. burgdorferi, B. garinii, B. afzelliB. japonica.. ...

KINASE INHIBITORS

There are provided compounds of formula I,

METHOD FOR PRODUCING THIOLANE SKELETON-TYPE GLYCOCONJUGATE, AND THIOLANE SKELETON-TYPE GLYCOCONJUGATE

There is provided a production method of a compound represented by the following formula (II) through a step of reacting a compound represented by the following General Formula (I) with a sulfur compound. 3. The production method according to claim 1 ,{'sup': 5', '3', '3a, 'wherein Ris an aryl group, and Ror —O—C(═O)—Ris an arylcarbonyloxy group.'}4. The production method according to claim 1 ,{'sup': 5', '3', '3a, 'wherein Ris a phenyl group, a 4-methylphenyl group, a 4-phenylphenyl group, or a 2-naphthyl group, and Ror —O—C(═O)—Ris a phenylcarbonyloxy group, a 4-methylphenylcarbonyloxy group, a 4-phenylphenylcarbonyloxy group, or a 2-naphthylcarbonyloxy group.'}6. The production method according to claim 1 ,{'sup': 1', '1a, 'wherein Ror Ris an acetyl group or an arylcarbonyl group.'}7. The production method according to claim 1 ,wherein X is a halogen atom, an alkylsulfonyloxy group, or an arylsulfonyloxy group.8. The production method according to claim 1 ,{'sub': '2', 'wherein the sulfur compound is MSH or MS in which M is an alkali metal.'}10. The compound according to claim 9 ,{'sup': 1', '2a', '3a', '5, 'wherein Ris a hydrogen atom, an acetyl group, or an arylcarbonyl group, and each of R, R, and Ris independently an aryl group.'}11. The compound according to claim 9 ,{'sup': 2a', '3a', '5, 'wherein each of R, R, and Ris independently a phenyl group, a 4-methylphenyl group, a 4-phenylphenyl group, or a 2-naphthyl group.'}13. The compound according to claim 12 ,{'sup': 1', '1b', '1c', '2a', '3a', '5', '5b', '5c', '2b', '5d', '5c, 'wherein Ris a hydrogen atom, an acetyl group, a 4-methylbenzoyl group, a 4-phenylbenzoyl group, or a 2-naphthoyl group, each of Rand Ris independently a hydrogen atom, a 4-methylbenzoyl group, a 4-phenylbenzoyl group, or a 2-naphthoyl group, each of R, R, R, R, and Ris independently a 4-methylphenyl group, a 4-phenylphenyl group, or a 2-naphthyl group, Ris a phenylmethyl group, and each of Rand Ris independently a phenyl group, a 4- ...

SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSYL)CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME

A compound represented by a formula [1D] as shown below (wherein R 1A , R 1B , R 2A , R 2B , R 3A and R 3B represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.

CONJUGATED ANTISENSE COMPOUNDS AND THEIR USE

Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the gomeric compounds are conjugated to N-Acetylgalactosamine or to N-Acetylgalactosamine analogues. 13-. (canceled)56-. (canceled)8. The compound of wherein X is selected from substituted aryl and substituted heteroaryl.9. The compound of wherein X is phenyl or substituted phenyl comprising one or more substituent groups selected from F claim 8 , Cl claim 8 , Br claim 8 , COEt claim 8 , OCH claim 8 , CN claim 8 , CH claim 8 , OCH claim 8 , CF claim 8 , N(CH)and O-phenyl.10. (canceled)12. The compound of wherein Ris selected from CHNJJ claim 4 , CHNand CHSJwherein J claim 4 , Jand Jare each independently selected from H and CH.13. The compound of wherein J claim 12 , Jand Jare each H.1417-. (canceled)18. The compound of wherein Ris N(H)C(═O)-Q.19. The compound of wherein Qis selected from C-Calkyl claim 18 , substituted C-Calkyl claim 18 , C-Calkoxy and substituted C-Calkoxy.2022-. (canceled)2441-. (canceled)43. The compound of wherein L comprises a phosphorus linking group claim 4 , NH claim 4 , or N(CH).4446-. (canceled)4888-. (canceled)89. The compound of claim 4 , wherein the oligomer comprises at least one modified nucleoside comprising a modified base and or a modified sugar.9094-. (canceled)95. The compound of having at least one modified nucleoside comprising a modified sugar selected from a bicyclic nucleoside and a 2′-modified nucleoside.9698-. (canceled)99. The compound of claim 95 , comprising at least one 4′-C(CH)H—O-2′- or 4′-CH—O-2′bridged bicyclic nucleoside.100103-. (canceled)104. The compound of claim 95 , comprising at least one 2′ O(CH)OCHsubstituted 2′-modified nucleoside.105124-. (canceled)125. The compound of claim 4 , wherein the conjugate group is attached to the 5′-terminal nucleoside of the oligomer.126. The compound of claim 4 , wherein the conjugate group is attached to the 3′-terminal nucleoside of the oligomer.127131-. (canceled)132. The compound of ...

Compositions containing tannic acids and uses thereof

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

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS

An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. 2. The compound of claim 1 , wherein A is selected from formula 2 wherein R-Rare independently selected from H claim 1 , F claim 1 , methyl optionally substituted with a F claim 1 , and OCHoptionally substituted with a F.3. The compound of claim 1 , wherein A is selected from formula 2 wherein Rand Rare selected from H and R-Rare selected from F or wherein R-Rare all F or wherein Rand Rare F and R claim 1 , Rand Rare H claim 1 , or wherein Rand Rare F and R claim 1 , Rand Rare H claim 1 , or wherein Ris F and R claim 1 , R-Rare H claim 1 , or wherein Rand Rare F claim 1 , Ris OCH claim 1 , and Rand Rare H.4. The compound of claim 1 , wherein A is selected from formula 3 wherein Hetis selected from a six membered heteroaromatic ring claim 1 , optionally substituted with a group selected from Br claim 1 , F claim 1 , and Cl.5. The compound of claim 1 , wherein A is selected from formula 3 wherein Hetis selected from a pyridinyl substituted with a F claim 1 , such as 3 F.6. The compound of claim 1 , wherein A is selected from formula 4 wherein Ris selected from Calkyl optionally substituted with a halogen claim 1 , and branched Calkyl claim 1 , such as CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , isopropyl and CHCF.7. The compound of claim 1 , wherein A is selected from formula 5 wherein Ris selected from phenyl optionally substituted with a group selected from Br claim 1 , F claim 1 , Cl claim 1 , methyl optionally substituted with a F claim 1 , and OCHoptionally substituted with a F.8. The compound of claim 1 , ...

Substituted pyrrolidine-2-carboxamides -2-

BBM-1675, a new antibiotic complex

A novel antibiotic complex designated herein as BBM-1675 complex is produced by fermentation of certain novel strains of Actinomadura verrucosospora. The complex may be separated into two major components, BBM-1675 A1 and A2, and four minor components, BBM-1675 A3, A4, B1 and B2, and such components exhibit antimicrobial activity and also antitumor activity in certain mouse tumor systems.

Procedimiento para preparar derivados de 1-halo-2-desoxi-2,2-difluoro-d-ribofuranosilo enriquecidos en anomero alfa.

UN PROCESO ESTEREOSELECTIVO PARA LA PREPARACION DE DERIVADOS DE 1-(ALFA)-HALO-2-DESOXI2,2-DIFLUORO-D-RIBOFURANOSILOS ENRIQUECIDOS CON ALFA-ANOMEROS QUE CONSISTE EN HACER PONER EN CONTACTO UN 2-DESOXI-2,2-DIFLUORO-D-RIBOFURANOSIL-1-(BETA)-SULFONATO PROTEGIDO CON 3,5-HIDROXI CON UNA FUENTE DE HALURO EN UN SOLVENTE INERTE.

取代的吡咯烷-2-甲酰胺

本申请提供了式(I)化合物、其对映异构体及其药学上可接受的盐和酯、制备这些化合物的方法以及所述化合物作为药物尤其是作为抗癌剂的用途，其中X、Y、Z、R 1 、R 2 和R 3 如申请所述。

1-?-halo-2,2-difluoro-2-deoxy-d-ribofuranose derivatives and process for the preparation thereof

본 발명은 하기 화학식 1로 표시되는 1-α-할로-2,2-다이플루오로-2-데옥시-D-라이보퓨라노스 유도체 및 이의 제조방법에 관한 것으로, 본 발명의 1-α-할로-라이보퓨라노스 유도체는 고체 상태로 수득되어 젬시타빈(gemcitabine)의 제조를 위한 중간체로서 유용하게 사용될 수 있다. The present invention relates to a 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative represented by the following Chemical Formula 1 and a method for preparing the same, and to 1-α-halo of the present invention. Ribofuranose derivatives are obtained in the solid state and can be usefully used as intermediates for the preparation of gemcitabine. 상기 식에서, Where R 1 은 벤조일 또는 이고, R 1 is benzoyl or ego, R 2 는 이고, R 2 is ego, R 3 은 시아노, 할로겐, 카보알콕시, 톨루엔, 니트로, C 1-2 알콕시, C 1-2 알킬 및 다이알킬 아미노로 이루어진 군으로부터 선택된 하나 이상의 기로 치환되거나 치환되지 않은 페닐이며, R 3 is phenyl unsubstituted or substituted with one or more groups selected from the group consisting of cyano, halogen, carboalkoxy, toluene, nitro, C 1-2 alkoxy, C 1-2 alkyl and dialkyl amino, X는 Cl, Br 또는 I이다. X is Cl, Br or I.

Замещенные пирролидин-2-карбоксамиды

1. Соединение формулыгде X выбран из группы, состоящей из H, F, Cl, Br, I, циано, нитро, этинила, циклопропила, метила, этила, изопропила, винила и метокси;Y представляет собой группу(ы) в количестве от одной до четырех, независимо выбранную(ые) из группы, состоящей из H, F, Cl, Br, I, CN, OH, нитро, низшего алкила, циклоалкила, низшего алкокси, низшего алкенила, циклоалкенила и низшего алкинила;Z представляет собой низший алкокси;Rвыбран из группы, состоящей из низшего алкила, замещенного низшего алкила, низшего алкенила, замещенного низшего алкенила, арила, замещенного арила, гетероарила, замещенного гетероарила, гетероцикла, замещенного гетероцикла, циклоалкила, замещенного циклоалкила, циклоалкенила и замещенного циклоалкенила;Rпредставляет собой замещенный фенил, выбранный из:W представляет собой F, Cl или Br;V представляет собой H или F,Rвыбран из группы, состоящей из низшего алкокси, замещенного низшего алкокси, алкиламино, диалкиламино, остатков глюкуроновой кислоты, гексоз, аминогексоз, пираноз, аминогликозидов, природных и неприродных аминокислот, -OCHC(O)N(CH), -(OCHCH)-OH, -(OCHCH)-OCH, -(OCHCH)-OP(O)(OR), -OCHC(O)-(OCHCH)-OH, -OCHC(O)-(OCHCH)-OCH, -NH(CHCHO)-CH, -NH(CHCHO)-H, -OCHC(O)NH(CHCHO)-CH, -O-R, -OCH-R, -OCHCH-R, -OCHC(O)-R, -NH(OCHCH)-NHи -OCHCH-аминокислоты, где n составляет число от 3 до 80;Rпредставляет собой водород или бензил;Rвыбран из группы, состоящей из гетероциклов, замещенных гетероциклов, диалкиламино, алкиламино и аминоалкиловых спиртов; илиего фармацевтически приемлемые соль или сложный эфир.2. Соединение по п. 1, гдеX выбран из H, F или Cl;Y выбран из Н, F или Cl;Rпредставляет собой низший алкил или замещенный низший алкил;Rвыбран из группы, состоящей из низшего алкокси, замещенного низшего алкокси, алкиламино, диалкиламино, остатков глюкуроновой кислоты, гексоз, аминогексоз, пираноз, аминогликозидов, природных и неприродных аминокислот, -OCHC(O)N(CH), -(OCHCH)-OH, -(OCHCH)-OCH, -(OCHCH)-OP РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) ...

Gallotannic compounds in lithographic printing plate coating compositions

FIELD: chemistry. SUBSTANCE: novel gallotannic compounds include gallotannin, wherein at least one hydroxyl group is substituted with a substitute, said substitute including a molecule, an oligomer or polymer, used in lithographic printing plate coatings, gallotannin or another gallotannin compound, wherein the substitutes are attached to gallotannin directly or through a linking group. EFFECT: compounds can be used in a lithographic printing plate coating composition. 15 cl, 33 dwg, 49 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 487 882 (13) C1 (51) МПК C07H C07H C07H C08G B41C 15/18 (2006.01) 1/00 (2006.01) 15/26 (2006.01) 67/00 (2006.01) 1/10 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011151989/04, 11.06.2010 (24) Дата начала отсчета срока действия патента: 11.06.2010 (73) Патентообладатель(и): МАЙЛАН ГРУП (VN) (45) Опубликовано: 20.07.2013 Бюл. № 20 2 4 8 7 8 8 2 (56) Список документов, цитированных в отчете о поиске: US 20020142244 А1, 03.10.2002. US 3862842 В1, 28.01.1975. US 6596464 В2, 22.07.2003. US 3600166 A1, 17.08.1971. ЕА 005016 В1, 28.10.2004. (85) Дата начала рассмотрения заявки PCT на национальной фазе: 19.12.2011 2 4 8 7 8 8 2 R U (87) Публикация заявки РСТ: WO 2011/050442 (05.05.2011) C 1 C 1 (86) Заявка PCT: CA 2010/000862 (11.06.2010) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры" (54) ГАЛЛОТАННИНОВЫЕ СОЕДИНЕНИЯ В КОМПОЗИЦИЯХ ДЛЯ ПОКРЫТИЯ ЛИТОГРАФИЧЕСКИХ ПЕЧАТНЫХ ФОРМ (57) Реферат: Изобретение относится к новым галлотанниновым соединениям, включающим галлотаннин, в котором по меньшей мере одна гидроксильная группа замещена заместителем, причем данный заместитель включает молекулу, олигомер или полимер, которые используют в покрытиях литографических печатных форм, галлотаннин или другое галлотанниновое соединение, при этом заместители связаны с галлотаннином непосредственно или через соединительную группу. Указанные ...

Sucrose derivatives

내용 없음. No content.

Single tin organic compound, preparation method and application thereof

本申请提供一种单锡有机化合物，用于合成蔗糖‑6‑羧酸酯，所述化合物为下述式(1)表示的化合物：式(1) 其中，R 1 、R 2 和R 3 分别独立地表示C1～C8的直链或支链饱和烷基、C2～C8的直链或支链不饱和烷基、C3～C8的取代或未取代的饱和环烷基、C3～C8的取代或未取代的不饱和环烷基、或C6～C12的芳基或取代芳基；R 4 表示C1～C6的直链或支链饱和烷基或C6～C12的芳基或取代芳基。本申请的单锡有机化合物，使得在合成蔗糖‑6‑羧酸酯过程中，能够准确地进行计量加料，同时提高催化剂回收率、减少后续氯化副反应的发生，且反应较快、能耗小、单位体积内收率更高。

Purified pentagalloylglucose and delivery device

本文公开了通过用二甲醚洗涤来生产至少99.9％纯度的高纯度的五没食子酰葡萄糖(PGG)、其类似物或衍生物的方法。PGG可以在试剂盒中提供，所述试剂盒包括用于溶解PGG的水解剂和盐水溶液。本文还公开了用于将治疗溶液递送至血管的装置。所述装置可以是具有上游球囊和下游球囊的导管。上游球囊可以扩张以锚定导管并阻断顺行血流。下游球囊可以扩张以阻断逆行血流，从而在血管内产生密封体积。下游球囊可具有被配置为将治疗性膨胀溶液递送到密封体积或其一部分内的孔。下游球囊可以通过扩张设置在下游球囊内的球囊而扩张。

DERIVATIVES OF 1-α-HALOGEN-2,2-DIFLUORO-2-DEOXY-D-RIBOFURANOSE AND METHOD OF THEIR OBTAINMENT

FIELD: chemistry. SUBSTANCE: invention claims derivatives of 1-α-halogen-2,2-difluoro-2-deoxy-D-ribofuranose of the general formula (I) in solid state, where R 1 is benzoyl or ; R 2 is hydrogen; and X is CI, Br or I; which can be applied as intermediates in stereoselective method of gemcitabine obtainment. In addition, invention claims stereoselective method of obtaining compounds of the general formula (I), including stages of: (i) recovery of 1-oxoribose of formula to obtain lactol of formula ; (ii) interaction of compound of formula (III) with halogen phosphate compound of formula in the presence of a base to obtain 1-phosphatefuranose derivative of formula ; and (iii) interaction of compound of formula (V) (also included in the claim) with halogen source, with further recrystallisation of obtained product; where R 1 , R 2 and X are the same as indicated above while R 3 is phenyl. EFFECT: efficient method of obtaining derivatives of the abovementioned agent. 11 cl, 6 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 346 948 (13) C2 (51) ÌÏÊ C07H 5/02 (2006.01) C07H 1/00 (2006.01) C07H 11/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2007107607/04, 21.06.2005 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 21.06.2005 (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.07.2004 KR 10-2004-0059623 17.05.2005 KR 10-2005-0041278 (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 (45) Îïóáëèêîâàíî: 20.02.2009 Áþë. ¹ 5 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: US 5945547 À, 31.08.1999. US 5453499 À, 26.09.1995. US 5744597 À, 28.04.1998. US 5401861 À, 28.03.1995. RU 2131880 Ñ1, 20.06.1999. 2 3 4 6 9 4 8 R U (86) Çà âêà PCT: KR 2005/001922 (21.06.2005) C 2 C 2 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2007 (87) Ïóáëèêàöè PCT: WO 2006/011713 (02.02.2006) Àäðåñ äë ïåðåïèñêè: 129090, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé ...

Polycarbocyclic derivatives for modification of resist, optical and etch resistance properties

ικτά καρβοκυκλικά παράγωγα, τα οποία περιέχουν τουλάχιστον δύο καρβοκυκλικές ομάδες ανά μόριο από τις κατηγορίες του ανθρακενίου και των παραγώγων του, του αδαμαντανίου και των παραγώγων του και των στεροειδών, με ανθρακικές αλυσίδες που περιέχουν λειτουργικές ομάδες, συντίθενται και χρησιμοποιούνται ως τροποποιητές ιδιοτήτων φωτοπολυμερικών υλικών λιθογραφίας και ειδικότερα για τη βελτίωση τηςαντίσιτασης στην εκχάραξη και των ιδιοτήτων απορρόφησης. Αυτά τα παράγωγα χαρακτηρίζονται από τους τύπους I-V, όπου A και R μπορούν να είναι μια ανθρυλο- ή/και μια αδαμαντυλο- ή/και μια ομάδα στεροειδούς. Περιγράφονται μέθοδοι για την παρασκευή των παραπάνω ενώσεων. ΰ

Gallotannic compounds for lithographic printing plate coating compositions

There is provided a gallotannic compound, a method of producing a gallotannic compound, a lithographic printing plate coating composition, a lithographic printing plate, a method of producing a lithographic printing plate and a method of printing.

Gallotannic compounds for lithographic printing plate coating compositions

There is provided a gallotannic compound, a method of producing a gallotannic compound, a lithographic printing plate coating composition, a lithographic printing plate, a method of producing a lithographic printing plate and a method of printing.

Method for selective acylation of saccharides

Prodrugs, their preparation and use as medicines

SUGAR AMINO SULFURIC ACID ESTERS, THEIR USE, A PROCEDURE TO PREPARE THEM, AND A MEDICINAL PRODUCT CONTAINING THEM

El presente invento se refiere a nuevos ésteres de ácido sulfúrico de amino azúcares de las fórmulas generales (Ia), (Ib) y (Ic), en donde: B es alquilenoinferior o un sistema de anillo aromático opcionalmente sustituido; G1, G2 y y G3 son cada uno, independientemente, un radical de un glicopiranósido,una glicopiranosa o un derivado respectivo, estando por lo menos un grupo hidroxi del radical G1, G2 ó G3 esterificado con ácido sulfúrico, y sus salesfarmacéuticamente utilizables. Los ésteres son apropiados como sustancias terapéuticamente activas para el tratamiento de trastornos que se distinguenpor proliferación excesiva o destructiva de células del músculo liso y cambios arterioescleróticos frente a la pared vascular. Además, el presenteinvento se refiere al uso de dichos ésteres o de sus sales como medicamentos, especialmente para el tratamiento y/o profilaxis de trastornos que sedistinguen por proliferación excesiva o destructiva de células de músculo liso y cambios arterioescleróticos frente a la pared vascular y, respectivamente,para la producción de medicamentos correspondientes. Asimismo, el presente invento se refiere a un procedimiento para preparar dichos ésteres y unmedicamento que loscontiene. The present invention relates to new sulfuric acid esters of amino sugars of the general formulas (Ia), (Ib) and (Ic), wherein: B is lower alkylene or an optionally substituted aromatic ring system; G1, G2 and and G3 are each, independently, a radical of a glycopyranoside, a glycopyranose or a respective derivative, at least one hydroxy group of the radical G1, G2 or G3 being esterified with sulfuric acid, and their pharmaceutically usable salts. Esters are suitable as therapeutically active substances for the treatment of disorders distinguished by excessive or destructive proliferation of smooth muscle cells and arteriosclerotic changes against the vascular wall. Furthermore, the present invention relates to the use of said esters or their salts as medicaments, ...

Preparation method and application of tannin extract in sea buckthorn

本发明公开一种沙棘中鞣质提取物的制备方法及其用途。该提取物将沙棘叶用甲醇浸泡提取浸膏；再将备用浸膏用水分散后,用机溶剂萃取,减压回收溶剂待用；取经过上述步骤的浸膏,用20％甲醇溶解后,进行Sephadex LH‑20柱色谱分离,以甲醇‑水(20:80→100:0)溶剂系统梯度洗脱,得到4个部分Fr.1‑4,Fr.4(20g)经过硅胶、MCI CHP‑20柱色谱和半制备高效液相色谱分离纯化，得到化合物。本发明的鞣质提取物具有抗炎抗肥胖活性，能够用于炎症及肥胖的预防和治疗，本发明通过生物活性测试实验表明，所述沙棘鞣质提取物具有强抗炎抗肥胖作用。

Synthesis of flg

본 발명은, 아노머적으로 상당히 순수한 2,3-디데옥시-3-플루오로-5-0-(4-페닐벤조일)-α-D-에리트로펜토푸라노실 클로라이드를, 상응하는 메틸 글리코시드의 α/β-혼합물로부터 합성하는 방법에 관한 것이다. 본 발명의 방법은 아노머 분리가 필요 없이 순수한 α-클로라이드를 제공한다. 이렇게 수득된 α-클로라이드는 2',3'-디데옥시-3'-플루오로 뉴클레오사이드의 제조에서 글리코실 공여체로서 사용하기에 적합하다. 특히, 아노머 분리가 필요 없이 메틸 글리코시드의 α/β-혼합물을 사용한 2',3'-디데옥시-3'-플루오로 구아노신(FLG)의 제조가 교시된다.

Chitosamine derivative, its composition and its medical usage

本发明提供式(A)化合物及其药学上可接受的盐和酯，以及其药物组合物，所述化合物及其药物组合物在用于制备预防或治疗哺乳动物关节及骨骼疾病如关节炎及骨质疏松症的药物中的用途。

DERIVATIVES 1-α-HALOGEN-2, 2-DIFFOROR-2-DESOXY-D-RIBOFURANOSES AND METHOD FOR PRODUCING THEM

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 107 607 (13) A (51) ÌÏÊ C07H 1/00 (2006.01) C07H 5/02 (2006.01) C07H 11/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007107607/04, 21.06.2005 (71) Çà âèòåëü(è): ÕÀÍÌÈ ÔÀÐÌ. ÊÎ., ËÒÄ. (KR) (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.07.2004 KR 10-2004-0059623 17.05.2005 KR 10-2005-0041278 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2007 (87) Ïóáëèêàöè PCT: WO 2006/011713 (02.02.2006) A Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Ã.Á. Åãîðîâîé, ðåã.N 513 (54) ÏÐÎÈÇÂÎÄÍÛÅ 1-α-ÃÀËÎÃÅÍ-2, 2-ÄÈÔÒÎÐ-2-ÄÅÇÎÊÑÈ-D-ÐÈÁÎÔÓÐÀÍÎÇÛ È ÑÏÎÑÎÁ ÈÕ R U (57) Ôîðìóëà èçîáðåòåíè 1. Ïðîèçâîäíîå 1-α-ãàëîãåí-2,2-äèôòîð-2-äåçîêñè-D-ðèáîôóðàíîçû ôîðìóëû (I) â òâåðäîé ôîðìå: ãäå R 1 âë åòñ áåíçîèëîì èëè R 2 âë åòñ âîäîðîäîì, öèàíî, ãàëîãåíîì, êàðáîàëêîêñè, íèòðî, C1-2 àëêîêñè, Ñ1-2 àëêèëîì èëè äèàëêèëàìèíî; è Ñòðàíèöà: 1 RU A 2 0 0 7 1 0 7 6 0 7 ÏÎËÓ×ÅÍÈß 2 0 0 7 1 0 7 6 0 7 (86) Çà âêà PCT: KR 2005/001922 (21.06.2005) R U (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 Áþë. ¹ 25 (72) Àâòîð(û): ËÈ Äçàåõåîí (KR), ÏÀÐÊ Ãà Ñåóíã (KR), ËÈ Ìîîíñóá (KR), ÊÈÌ Õàí Êèîíã (KR), ÁÀÍà Õèî-Äçåîíã (KR), ×ÀÍà ßíã-Êèë (KR), ËÈ Ãâàí Ñóí (KR) X âë åòñ Cl, Br èëè I. 2. Ïðîèçâîäíîå ïî ï.1, ãäå R 2 âë åòñ âîäîðîäîì. 3. Ïðîèçâîäíîå ïî ï.1, ãäå ñîäåðæàíèå β-àíîìåðà ñîñòàâë åò 0,5% èëè ìåíüøå. 4. Ñïîñîá ïîëó÷åíè ïðîèçâîäíîãî 1-α-ãàëîíåí-2,2-äèôòîð-2-äåçîêñè-D-ðèáîôóðàíîçû ôîðìóëû (I), âêëþ÷àþùèé ñòàäèè: (i) âîññòàíîâëåíè ñîåäèíåíè 1-îêñîðèáîçû ôîðìóëû (II) ñ ïîëó÷åíèåì ñîåäèíåíè ëàêòîëà ôîðìóëû (III); (ii) âçàèìîäåéñòâè ñîåäèíåíè ôîðìóëû (III) ñ ãàëîãåíôîñôàòíûì ñîåäèíåíèåì ôîðìóëû (IV) â ïðèñóòñòâèè îñíîâàíè ñ ïîëó÷åíèåì 1-ôîñôàòôóðàíîçíîãî ïðîèçâîäíîãî ôîðìóëû (V); è (iii) âçàèìîäåéñòâè ñîåäèíåíè ôîðìóëû (V) ñ èñòî÷íèêîì ãàëîãåíà ñ ïîñëåäóþùåé ïåðåêðèñòàëëèçàöèåé ïîëó÷èâøåãîñ ïðîäóêòà ñ ïîëó÷åíèåì ïðîèçâîäíîãî 1 ...

Thiopyranose compound and method for producing same

A method for producing a thiopyranose compound represented by formula (2), which comprises reacting a compound represented by formula (1) with a sulfur compound. X represents a leaving group; A represents an oxygen atom or a sulfur atom; and R 1A to R 4B , R 1B to R 4B and R 5 independently represent a hydrogen atom or a specific substituent.

Method for producing thiolane skeleton-type glycoconjugate, and thiolane skeleton-type glycoconjugate

There is provided a production method of a compound represented by the following formula (II) through a step of reacting a compound represented by the following General Formula (I) with a sulfur compound. In General Formulas (I) and (II), R 1 represents a hydrogen atom or an acyl group, R 2 represents a hydrogen atom, a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R 3 represents a hydrogen atom or an acyloxy group, R 5 represents an alkyl group or an aryl group, and X represents a leaving group. Here, in a case where R 2 is a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R 3 is an acyloxy group.

Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine, synthetic intermediate of thionucleoside, and method for producing the same

A compound represented by a formula [1D] as shown below (wherein R 1A , R 1B , R 2A , R 2B , R 3A and R 3B represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.

Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine, synthetic intermediate of thionucleoside, and method for producing the same

A compound represented by a formula [1D] as shown below (wherein R 1A , R 1B , R 2A , R 2B , R 3A and R 3B represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.

Thiopyranose compound and method for producing same

There is provided a production method of a thiopyranose compound represented by the following Formula (2) by reacting a compound represented by the following Formula (1) with a sulfur compound. X represents a leaving group. A represents an oxygen atom or a sulfur atom. Further, each of R 1A to R 4B , R 1B to R 4B , and R 5 represents a hydrogen atom or a specific substituent.

Triterpenoid saponin analogue

Methods of manufacture of 2′-deoxy-β-L-nucleosides

The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.

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

Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-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 substitutents. 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.

Ribofuranosyl Purine Derivatives

1,163,103. Ribofuranosyl purine derivatives. MERCK & CO. Inc. 8 Nov., 1966 [15 Nov., 1965], No. 49924/66. Heading C2C. Novel nucleosides of the formula where R is a C 1-5 alkyl radical and each of Ra and Rb is a hydrogen or halogen atom or a hydroxy, C 1-5 alkyl, amino, C 1-5 alkylamino, di- (C 1-5 alkyl) amino, mercapto or C 1-5 alkyl mercapto radical, are prepared by treating 2,3,5 - tri - O - acyl - 3 - C 1-5 - alkyl - D - ribofuranosyl halides II with a chloromercuri-2,6- substituted purines of the formula where each of Rc and Rd is a halogen or hydrogen atom or a hydroxy, C 1-5 alkyl, acylamino or acyl C 1-5 alkylamino to produce the corresponding 9 - (2,3,5 - tri - 0 - acyl - 3 - C 1-5 - alkyl- D - ribofuranosyl) - 2,6 - substituted purine derivatives IV and either (a) hydrolysing these by a basic solvolysis reaction to give a compound of Formula I in which each of Ra and/or Rb is a hydrogen or halogen atom or a hydroxy, C 1-5 alkyl, amino or C 1-5 alkylamino radical or (b) when Rc and/or Rd is halogen, reacting compounds IV with primary or secondary amines to give compounds of Formula I in which Ra and/or Rb is a C 1-5 alkylamino or di-(C 1-5 alkyl) amino radical or (c) when Rc and/or Rd is halogen, subjecting compounds IV to mercaptolysis to give compounds of Formula I in which Ra and/or Rb is a mercapto or C 1-5 alkyl mercapto radical or (d) when Rc and/or Rd is halogen, hydrogenating and solvolysing compounds IV to give compounds of Formula I in which Ra and/or Rb is hydrogen. In the mercaptolysis reaction (c), a (tri-acyl-3-C 1-5 alkyl ribosyl) purine thiol may be formed as an intermediate. The 2,3,5 - tri - 0 - acyl - 3 - C 1-5 alkyl - D- ribofuranosyl halides II may be prepared by reacting a 5-0-acyl-1,2-O-isopropylidene-D- erythro-3-pentulofuranose with a Grignard reagent, thereby forming a 5-0-acyl-1,2-0-isopropylidene - 3 - C 1-5 alkyl - D - ribofuranose, subjecting this to acid alcoholysis to produce an alkyl 5 - O - acyl - 3 - C 1-5 alkyl - D - ...

Patent FR1498856A

Substituted purine nucleosides and processes for their preparation

Substituted purine nucleosides

2-c or 3-c-alkylribofuranosyl - 1-substituted compounds and the nucleosides thereof

Composition of matter and process

A process for treating DNA viral diseases in humans and animals which comprises administering a therapeutic amount of a compound of the formula ##STR1## the compounds are formulated with pharmaceutical carriers for systemic or local means of administration. CROSS REFERENCE TO RELATED APPLICATION

Process for separating 2-deoxy-2,2-difluoro-D-ribofuranosyl alkylsulfonate anomers

A process for separating an anomeric mixture of alpha and beta 2-deoxy-2,2-difluoro-D-ribofuranosyl-1-alkylsulfonates by contacting the anomeric mixture with a solvent; heating; adding a countersolvent; and lowering the temperature.

Low temperature process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates

A stereoselective process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates by contacting a lactol with an amine base in an inert solvent, adjusting the temperature and adding a sulfonating reagent.

Methods of manufacture of 2 -deoxy-beta-L-nucleosides

本发明涉及2’－脱氧－β－L－胸苷、2’－脱氧－β－L－尿苷和2’－脱氧－β－L－胞苷及其衍生物的合成，其中所述衍生物例如为3′－O－酰基或3’，5’－O－二酰基前药，包括3’－O－L－氨酰基和3’，5’－O－L－二氨酰基前药，特别是3’－O－L－缬氨酰和3’，5’－O－L－二缬氨酰前药。

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

Provided are pyrrolo[1,2-f][1,2,4] triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-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.

Synthesis of decitabine

一种制备β-富集的受保护的地西他滨(decitabine)的方法，其包含：a)在存在催化剂的情况下使受保护的2-脱氧-呋喃核糖与受保护的5-氮杂胞嘧啶偶合，形成包含式I的受保护的地西他滨的反应混合物；和b)用碱淬灭步骤a)的所述反应混合物。所制备的所述β-富集的受保护的地西他滨可脱除保护基以产生高产率及高纯度的地西他滨产物。

METHODS FOR EXTRACTION AND CLEANING OF THE INTERMEDIATE PRODUCT FOR PRODUCING SUCRALOSE

1. Способ очистки сукралоза-6-сложного эфира, применяемого при получении сукралозы, включающий: ! экстрагирование сукралоза-6-сложного эфира из композиции, содержащей сукралоза-6-сложный эфир, с помощью первого органического растворителя с получением первого раствора сукралоза-6-сложного эфира; ! сушку первого раствора сукралоза-6-сложного эфира с получением неочищенного сукралоза-6-сложного эфира; ! добавление воды к неочищенному сукралоза-6-сложному эфиру с получением второго раствора сукралоза-6-сложного эфира; ! добавление второго органического растворителя ко второму раствору сукралоза-6-сложного эфира для осаждения сукралоза-6-сложного эфира с получением полуочищенного сукралоза-6-сложного эфира; ! нагревание полуочищенного сукралоза-6-сложного эфира в третьем органическом растворителе с получением раствора полуочищенного сукралоза-6-сложного эфира; и ! охлаждение раствора полуочищенного сукралоза-6-сложного эфира с получением очищенного сукралоза-6-сложного эфира. ! 2. Способ по п.1, отличающийся тем, что первый органический растворитель представляет собой этилацетат. ! 3. Способ по п.1, отличающийся тем, что второй органический растворитель представляет собой простой эфир или алкан. ! 4. Способ по п.1, отличающийся тем, что второй органический растворитель представляет собой диэтиловый эфир, петролейный эфир или их комбинацию. ! 5. Способ по п.1, отличающийся тем, что третий органический растворитель представляет собой этилацетат. ! 6. Способ по п.1, отличающийся тем, что первый раствор сукралоза-6-сложного эфира сушат с применением вакуумной сушки. ! 7. Способ по п.1, отличающийся тем, что отношение (об./об.) вто� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2011 106 794 (13) A (51) МПК C07H 1/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): МЭМТЕК ИНТЕРНЭШНЛ ЛИМИТЕД (CN) (21)(22) Заявка: 2011106794/04, 23.07.2009 Приоритет(ы): (30) Конвенционный приоритет: 23.07.2008 US 12/178,510 (85) Дата начала ...

Triterpene saponin analogues

【課題】天然サポニンアジュバントＱＳ－２１に代わる、ＱＳ－２１及びＱＳ－７の類似物であるトリテルペングリコシドサポニン誘導アジュバント、それの合成法、及びそれの中間体を提供する。また、本発明の化合物を含む医薬組成物、並びに感染症の治療及び感染症のための免疫化に上記化合物または組成物を使用する方法も提供する。【解決手段】例えば、図に示される化合物（ＴＱＬ－１０５５）及びその合成法である。【選択図】図１

Prodrugs and methods for their preparation

본 발명은 글라이코실-스페이서-약물 화합물(선구약물), 이의 제조방법 및 약제로서의 이의 용도에 관한 것이다. The present invention relates to glycosyl-spacer-drug compounds (precursor drugs), their preparation and their use as medicaments.

A kind of method of catalytic esterification-separation coupling preparation food-grade rosin xylose ester

本发明公开了一种催化酯化‑分离耦合制备食品级松香木糖酯的方法，操作步骤为(1)将木糖或木糖醇类、松香或氢化松香与绿色溶剂混合，溶解；(2)通入CO 2 进行酯化反应；(3)气相经不断地采出，冷凝分离；(4)酯化反应2.0～16.0h后，从酯化反应器内取出所得反应产物；(5)反应产物经常压蒸馏和减压蒸馏除去绿色溶剂即可得到食品级松香木糖酯。本发明以松香或氢化松香与木糖或木糖醇为原料制备食品级松香木糖酯，因木糖或木糖醇自身为一种天然、健康的甜味剂，作为食品添加剂使用时可不需另外加入甜味剂。本发明方法生产的产品安全可靠，绿色溶剂循环使用，是一种绿色催化松香或氢化松香制备食品级木糖酯的方法和清洁生产过程。

Tannate salt of rasagiline

Conjugated antisense compounds and their use

Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the gomeric compounds are conjugated to N -Acetylgalactosamine or to N -Acetylgalactosamine analogues.

Triterpene saponins, methods of synthesis, and uses thereof

본 발명은 트리테르펜 글리코시드 사포닌-유래의 아주반트, 그의 합성법, 그에 대한 중간체 및 그의 용도에 관한 것이다. QS-7은 항암 및 항-바이러스 백신에서 현재 유리하게 사용되는 아주반트인 관련 사포닌 QS-21보다 유의하게 덜 독성인 강력한 면역-아주반트이다. 지루한 단리 및 정제 프로토콜로 인해 QS-7의 임상 개발이 방해를 받아 왔다. 가수분해된 프로사포게닌 혼합물을 사용하여 QS-7, QS-21 및 관련 유사체를 합성하는 신규한 반합성 방법이 제공되어, 전임상 및 임상 평가를 위한 QS-7 및 QS-21 유사체에 대한 접근을 매우 용이하게 한다. The present invention relates to a triterpene glycoside saponin-derived azbunt, a synthetic method thereof, an intermediate therefor and a use thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than the avant-related saponin QS-21, which is currently advantageously used in anti-cancer and anti-viral vaccines. Clinical development of QS-7 has been hampered by tedious isolation and purification protocols. A novel semisynthetic method of synthesizing QS-7, QS-21 and related analogs using hydrolyzed prosapogenin mixtures has been provided to provide access to QS-7 and QS-21 analogs for preclinical and clinical evaluation .

Process for producing antracycline glycosides

Anthracycline glycosides, which in form of pharmaceun- cal compositions, exhibit antitumoral activity. The anthracycline glycosides are of the general formula I in which R represents a hydrogen atom or a hydroxy group, one of R 1 and R 2 represents a methyl group, and the other of R 1 and R 2 represents a hydroxy group, and their pharmaceutically acceptable acid addition salts, a process for producing said compounds and pharmaceutical compositions containing same.

Glucosamine derivative, composition thereof and medical application thereof

本发明提供式(A)化合物及其药学上可接受的盐和酯，以及其药物组合物，所述化合物及其药物组合物在用于制备预防或治疗哺乳动物关节及骨骼疾病如关节炎及骨质疏松症的药物中的用途。

Pesticide compositions

FIELD: chemistry. SUBSTANCE: invention relates to compounds - tetrahydropyran derivatives of formula , where (a) Ar 1 is a substituted phenyl, wherein said substituted phenyl has one or more substitutes independently selected from H, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C(=O)H, C 1 -C 6 (hydroxy)haloalkyl; (b) E is N, C or CR5;(c) G is a double or triple bond; (d) M is N, C or CR5 (under the condition that when E is a nitrogen atom "N", M is a nitrogen atom "N"; when E is a carbon atom "C", M is a carbon atom "C"; and when E is "CR5", M is "CR5"); (e) Ar 2 is a phenyl; (f) J is NR5 or CR5; (g) L is a single or double bond; (h) K is C=O or N; (i) R1 is C 1 -C 6 alkoxy; (j) R2 is C 1 -C 6 alkoxy; (k) R3 is C 1 -C 6 alkoxy; (l) R4 is C 1 -C 6 alkyl; (m) R5 is H, or to pesticidally acceptable acid addition salts thereof, which have pesticide activity, and to use of said compounds in pest control. EFFECT: obtaining pest control compounds. 8 cl, 4 tbl, 12 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 534 529 C2 (51) МПК C07H 15/02 (2006.01) A01N 43/16 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011137406/04, 11.02.2010 (24) Дата начала отсчета срока действия патента: 11.02.2010 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 20.03.2013 Бюл. № 8 R U 11.02.2009 US 61/151,549 (72) Автор(ы): КРАУЗ Гари (US), СПАРКС Томас (US), МАКЛАУД КаСандра (US), БРАУН Аннетт (US), СИДДАЛЛ Томас (US) (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) (45) Опубликовано: 27.11.2014 Бюл. № 33 2 5 3 4 5 2 9 (56) Список документов, цитированных в отчете о поиске: WO 9847894 A1 29.10.1998. RU 2255934 C2 10.07.2005. RU 2308452 C2 20.10.2007. RU 2336272 C2 20.10.2008 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.09.2011 (86) Заявка PCT: 2 5 3 4 5 2 9 R U (87) Публикация заявки PCT: C 2 C 2 US 2010/023852 (11.02 ...

SYNTHETIC INTERMEDIATE COMPOUND 1-(2-DESOXY-2-FLUORO-4-THIO-β-D-ARABINOFURANOSYL)CYTOSINE, SYNTHETIC INTERMEDIATE THIONUCLEOSIDES COMPOUND AND METHOD FOR THEIR PRODUCTION

FIELD: pharmacology. SUBSTANCE: invention relates to a process for preparation of a compound of the formula and also to a process for the preparation of 1-(2-desoxy-2-halo-4-thio-β-D-arabinofuranosyl) cytosine of the following formula: . In addition, the invention relates to a formula intermediate. EFFECT: new method for preparation of thionucleoside, which is useful as a medicament, is developed. 24 cl, 48 ex

Steviol glycoside isomers

FIELD: chemistry. SUBSTANCE: invention relates to compounds of formula II: where R 1 can be 1-β-D-glucopyranosyl or 2-(1-β-D-glucopyranosyl)-1-β-D-glucopyranosyl, and R 2 can be hydrogen, 1-β-D-glucopyranosyl, 2-(1-β-D-glucopyranosyl)-1-β-D-glucopyranosyl, 2,3-bis(1-β-D-glucopyranosyl)-1-β-D-glucopyranosyl, 2-(1-α-L-rhamnopyranosyl)-1-β-D-glucopyranosyl, 2-(1-α-L-rhamnopyranosyl)-3-(1-β-D-glucopyranosyl)-1-β-D-glucopyranosyl, or 2-(1-β-D-xylopyranosyl)-3-(1-β-D-glucopyranosyl)-1-β-D-glucopyranosyl. EFFECT: compounds can be used as sweetening agents which do not have nutritional qualities in food and drinks. 35 cl, 8 ex, 23 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 430 102 (13) C1 (51) МПК C07H C07H C07C A23L A23L 15/24 13/08 62/32 1/236 2/60 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010107991/04, 04.09.2008 (24) Дата начала отсчета срока действия патента: 04.09.2008 (73) Патентообладатель(и): ПепсиКо, Инк. (US) R U Приоритет(ы): (30) Конвенционный приоритет: 17.09.2007 US 11/856,274 (72) Автор(ы): ЛЕЕ Томас (US) (45) Опубликовано: 27.09.2011 Бюл. № 27 C 1 2 4 3 0 1 0 2 R U C 1 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 05.03.2010 (86) Заявка PCT: US 2008/075192 (04.09.2008) (87) Публикация заявки РСТ: WO 2009/038978 (26.03.2009) Адрес для переписки: 127006, Москва, ул. Долгоруковская, 7, Садовая Плаза, 11 этаж, фирма "Бейкер и Макензи", патентному поверенному Ю.А.Пыльневу (54) ИЗОМЕРЫ СТЕВИОЛ-ГЛИКОЗИДОВ (57) Реферат: Данное изобретение соединениям формулы II относится к Ñòð.: 1 ru 2 4 3 0 1 0 2 (56) Список документов, цитированных в отчете о поиске: М. Kobayashi et al, "Dulcosides A and B, new diterpene glycosides from Stevia Rebaudiana", Phytochemistry, 1977, v.16, pp.1405-1408. Hanson J.R. et al, "The microbiological transformation of steviol derivatives by rhizopus stolinifer and gibberella fujikuroi", ...

Separation method of 2-deoxy-2,2-difluoro-di-ribofuranosyl-alkylsulfonate anomer

아노머 혼합물을 용매와 접촉시키고, 가열하고, 보조용매를 첨가하고, 온도를 낮추는 단계를 포함하는 α및 β2-데옥시-2,2-디플루오로-D-리보푸라노실-1-알킬설포네이트 아노머 혼합물의 분리방법이 제공된다.

Method for producing thiolane skeleton type sugar compound and thiolane skeleton type sugar compound

Method of producing glucosamine or salts thereof

Glucosamine derivatives of the formula <IMAGE> (X, R, R1, R2, R4, R6-R9 have the meaning stated in Claim 1) are prepared by condensation of corresponding 3-O-carboxymethylglucopyranosides with corresponding dipeptides. These glucosamine derivatives have the ability to increase the immunogenicity of an antigen on admixture therewith and, on systemic administration, to enhance the immunological reactivity of the treated organism. They can thus be used as adjuvants to increase the vaccine protection from bacterial, viral or parasitic pathogens.

Triterpene saponins, methods of synthesis, and uses thereof

본 발명은 트리테르펜 글리코시드 사포닌-유래의 아주반트, 그의 합성법, 그에 대한 중간체 및 그의 용도에 관한 것이다. QS-7은 항암 및 항-바이러스 백신에서 현재 유리하게 사용되는 아주반트인 관련 사포닌 QS-21보다 유의하게 덜 독성인 강력한 면역-아주반트이다. 지루한 단리 및 정제 프로토콜로 인해 QS-7의 임상 개발이 방해를 받아 왔다. 가수분해된 프로사포게닌 혼합물을 사용하여 QS-7, QS-21 및 관련 유사체를 합성하는 신규한 반합성 방법이 제공되어, 전임상 및 임상 평가를 위한 QS-7 및 QS-21 유사체에 대한 접근을 매우 용이하게 한다. The present invention relates to triterpene glycoside saponin-derived adjuvants, their synthesis, intermediates thereto, and uses thereof. QS-7 is a potent immune-adjuvant that is significantly less toxic than the related saponin QS-21, an adjuvant currently advantageously used in anti-cancer and anti-viral vaccines. The clinical development of QS-7 has been hampered by tedious isolation and purification protocols. A novel semi-synthetic method for synthesizing QS-7, QS-21 and related analogs using hydrolyzed prosapogenin mixtures has been provided, greatly enhancing the approach to QS-7 and QS-21 analogs for preclinical and clinical evaluation. Make it easier.

SYNTHESIS OF BETA-L-2'-DEXOXINUCLEOSIDE

1. Способ получения 2'-дезокси-β-L-тимидина, включающий ! a) получение 5'-О-тритил- или 5'-О-диметокситритил-защищенного 2,2'-ангидро-1-β-L-арабинофуранозилтимина; ! b) взаимодействие 5'-О-диметокситритил-защищенного 2,2'-ангидро-1-β-L-арабинофуранозилтимина со стадии (a) с восстановителем RedAl и комплексообразующим агентом 15-краун-5-эфиром в полярном растворителе 1,2-диметоксиэтане (DME) или тетрагидрофуране (ТГФ) с получением 5'-О-диметокситритил-защищенного 2'-дезокси-β-L-тимидина или взаимодействие 5'-О-тритил-защищенного 2,2'-ангидро-1-β-L-арабинофуранозилтимина со стадии (a) с восстановителем RedAl в отсутствие комплексообразующего агента 15-краун-5-эфира с получением 5'-О-тритил-защищенного 2'-дезокси-β-L-тимидина и ! c) удаление защиты продукта со стадии (b), если это необходимо или желательно. ! 2. Способ по п.1, в котором на стадии (c) удаление защиты осуществляют посредством добавления кислоты или кислой смолы при температуре примерно 50°C. ! 3. Способ по п.1, в котором на стадии (b) температура реакции составляет примерно 0-5°C. ! 4. Способ по п. 1, в котором указанный 5'-О-тритил- или 5'-О-диметокситритил- защищенный 2,2'-ангидро-1-β-L-арабинофуранозилтимин получают с помощью следующих стадий: ! a) защиты L-рибофуранозы посредством взаимодействия с диметокситритильной или тритильной защитной группой; ! b) конденсации продукта со стадии (a) с тимином с образованием нуклеозида и ! c) взаимодействия нуклеозида со стадии (b) с конденсирующим агентом с образованием 5'-О-тритил- или 5'-О-диметокситритил- защищенного 2,2'-ангидро-1-β-D-арабинофуранозилтимина. ! 5. Способ по п.4, в котором на стадии (b) конденсацию осуществляют в присутствии растворителя и необязательно катал РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2009 115 775 (13) A (51) МПК C07H 1/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: ...

Production equipment and production method of sucrose-6-ester

本申请提供了一种蔗糖‑6‑酯的生产设备及生产方法，其中设备包括罐体、旋转蒸馏装置、冷凝装置；罐体包括分离腔和反应腔，冷凝装置套设在旋转蒸馏装置内，旋转蒸馏装置滑动连接在分离腔内；旋转蒸馏的转盘通过多个连接板固设在所述转筒的顶面，转盘的外壁上设有第一加热装置；冷凝装置包括依次上下连接的冷凝管、接水板以及冷凝水水箱；冷凝装置非接触套设旋转蒸馏装置的转筒内，冷凝管贯穿转盘与罐体的顶面接触设置；旋转蒸馏装置能够沿着转盘的中轴线旋转，以将从反应液进料管进入的反应液分离为水蒸气和蒸余液。本申请的设备使实现了蔗糖‑6‑酯的连续生产，极大程度上缩短了生产周期，提高了生产效率。

Methods of manufacture of 2'-deoxy-beta-L-nucleosides

The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.