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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 11056. Отображено 100.
05-01-2012 дата публикации

Process for production of orally ingestible composition containing arabinofuranosyl vitexin, and use of the composition

Номер: US20120004193A1
Автор: Shuichi Kusano
Принадлежит: Fuji Sangyo Co Ltd

A method for producing an orally ingestible composition containing an arabinofuranosyl vitexin and/or a hydrolysate thereof by using Basella alba as a raw material. The product of such method has a sedative effect and a sleep-inducing effect.

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Номер записи: 1
02-02-2012 дата публикации

Process for the synthesis of cleistanthin

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

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

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Номер записи: 2
08-03-2012 дата публикации

Macrolides with Anti-Inflammatory Activity

Номер: US20120058963A1
Автор: Antun Hutinec, Dubravko Jelic, Goran Kragol, Marija Ribic, Martina Bosnar, Nikola Marjanovic, Ognjen Culic, Sulejman Alihodzic, Vanja Vela, Vesna Erakovic Haber, Zorica Marusic-Istuk
Принадлежит: Glaxo Group Ltd

The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

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Номер записи: 3
03-05-2012 дата публикации

Phosphonate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production

Номер: US20120108531A1
Автор: Christophe Pannecouque, Erik De Clercq, Piet Herdewijn, Tongfei Wu
Принадлежит: KU Leuven Research and Development

Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.

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Номер записи: 4
01-11-2012 дата публикации

Cell surface coating with hyaluronic acid oligomer derivative

Номер: US20120277416A1
Автор: Alexander Tuzikov, Deborah Adella Blake, Eleanor Christine Williams, Elena Yurievna Korchagina, Nicola Lewell Carter, Nicolai Bovin, Stephen Michael Henry
Принадлежит: Kode Biotech Ltd

A method of localising reproduction assisting hyaluronic acid to reproductive cell surfaces by covalently linking it to lipids is disclosed.

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Номер записи: 5
31-01-2013 дата публикации

Nucleoside phosphoramidate prodrugs

Номер: US20130029929A1
Автор: Dhanapalan Nagarathnam, Jinfa Du, Michael Joseph Sofia, Peiyuan Wang
Принадлежит: GILEAD PHARMASSET LLC

Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.

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Номер записи: 6
21-02-2013 дата публикации

Composition comprising an amorphous non-crystalline glass form of roxithromycin

Номер: US20130045936A1
Автор: Marique Aucamp, Melgardt M. De Villiers, Wilna Leibenberg
Принадлежит: NORTH WEST UNIVERSITY

The invention relates to an amorphous non-crystalline glass form (Form-ll) of 3R,4S,5S,6R,7R,9R,11S,12R,13S,14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxa-cyclotetradecan-2-one or roxithromycin having at least one characteristic infra-red spectrum peak at approximately 3580 to 3464 cm −1 . The invention further relates to a preparation method of increasing the solubility of roxithromycin including the steps of selecting anhydrous roxithromycin or monohydrated roxithromycin; elevating the temperature of the roxithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-ll) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.

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Номер записи: 7
21-03-2013 дата публикации

PHOTOCLEAVABLE LABELED NUCLEOTIDES AND NUCLEOSIDES AND METHODS FOR THEIR USE IN IN DNA SEQUENCING

Номер: US20130072388A1
Автор: Litosh Vladislav A., Metzker Michael L., Stupi Brian P., Wu Weidong
Принадлежит:

Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3′-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group. 2. A compound according to claim 1 , wherein the cleavable terminating moiety is attached to the base through a linkage selected from the group consisting of benzyl amine claim 1 , benzyl ether claim 1 , carbamate claim 1 , carbonate claim 1 , 2-(o-nitrophenyl)ethyl carbamate claim 1 , and 2-(o-nitrophenyl)ethyl carbonate.4. A compound according to claim 3 , wherein Rand Rare selected from the group consisting of —CH claim 3 , —CHCH claim 3 , —CHCHCH claim 3 , isopropyl claim 3 , tert-butyl claim 3 , phenyl claim 3 , 2-nitrophenyl claim 3 , and 2 claim 3 ,6-dinitrophenyl.5. A compound according to claim 3 , wherein Rand Rare selected from the group consisting of alkyl and aromatic groups optionally containing at least one heteroatom in the alkyl or aromatic groups claim 3 , and further wherein the aromatic group may optionally be an aryl or polycyclic group.6. A compound according to claim 3 , wherein R claim 3 , R claim 3 , R claim 3 , and Rare selected from an aromatic group consisting of aryl and ...

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Номер записи: 8
04-04-2013 дата публикации

MANUFACTURING METHOD FOR POLYPHENOL COMPOSITION

Номер: US20130085270A1
Автор: Hanaki Keigo, Komatsu Toshiteru, Yamada Yasushi
Принадлежит: KAO CORPORATION

A method for producing a polyphenol composition including a step of subjecting (A) a hardly water-soluble polyphenol and (B) one or more selected from cathechins, chlorogenic acids and methylated compounds of hardly water-soluble polyphenols to a heat treatment at from 100 to 180° C. in the presence of an aqueous medium. 119-. (canceled)20. A method for producing a polyphenol composition comprising subjecting:(A) a hardly water-soluble polyphenol and(B) at least one member selected from the group consisting of cathechins, chlorogenic acids and methylated compounds of hardly water-soluble polyphenols to a heat treatment at from 100 to 180° C. in the presence of an aqueous medium.21. The method for producing the polyphenol composition according to claim 20 , wherein the heat treatment is carried out at a temperature of from 110 to 170° C.22. The method for producing the polyphenol composition according to claim 20 , wherein the log P value of (A) the hardly water-soluble polyphenol is from −1.0 to 4.0.23. The method for producing the polyphenol composition according to claim 20 , wherein (A) the hardly water-soluble polyphenol is at least one member selected from the group consisting of hesperidin claim 20 , quercetin claim 20 , resveratrol claim 20 , naringin claim 20 , curcumin claim 20 , rutin claim 20 , caffeic acid and ferulic acid.24. The method for producing the polyphenol composition according to claim 20 , wherein a mass ratio (A)/(B) of (A) the hardly water-soluble polyphenol to (B) at least one member selected from the group consisting of catechins claim 20 , chlorogenic acids and methylated compounds of hardly water-soluble polyphenols is from 0.005 to 10 in the heat treatment.25. The method for producing the polyphenol composition according to claim 24 , wherein the methylated compound of the hardly water-soluble polyphenol is methylhesperidin.26. The method for producing the polyphenol composition according to claim 20 , further comprising:cooling a ...

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Номер записи: 9
11-04-2013 дата публикации

Thiazole Derivatives as SGLT2 Inhibitors and Pharmaceutical Composition Comprising Same

Номер: US20130090298A1
Автор: Kang Suk Youn, KIM Jeongmin, Kim Jong Yup, Kim Min Ju, Kong Younggyu, Lee Jinhwa, LEE Junwon, Lee Suk Ho, Lee Sung-Han, PARK Eun-Jung, Seo Hee Jeong, Son Eun Jung, Song Kwang-Seop
Принадлежит: GREEN CROSS CORPORATION

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. 4. The compound of claim 1 , wherein the prodrug is carboxylate or aminoacetate of the compound of formula I claim 1 , the carboxylate or aminoacetate being optionally substituted with at least one substituent selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkenyloxy claim 1 , Caryl claim 1 , Caryloxy claim 1 , Caryl-Calkyl claim 1 , Caryl-Calkoxy claim 1 , and Caryl substituted with at least one Calkoxy.5. A compound of claim 1 , which is selected from the group consisting of:(1) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-((5-(thiophen-3-yl)thiazol-2-yl)methyl)phenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol;(2) (2S,3R,4R,5S,6R)-2-(3-((5-(4-Fluorophenyl)thiazol-2-yl)methyl)-4-methoxynaphthalen-1-yl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol;(3) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-(1-(5-(furan-2-yl)thiazol-2-yl)cyclopropyl)phenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol;(4) (2S,3R,4R,5S,6R)-2-(3-((5-(Furan-2-yl)thiazol-2-yl)methyl)-4-(trifluoromethyl)phenyl)-6-(hydroxymethyl-tetrahydro-2H-pyran-3,4,5-triol;(5) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-((5-(furan-2-yl)thiazol-2-yl)methyl)phenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol;(6) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-((5-(furan-3-yl)thiazol-2-yl)methyl)phenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol;(7) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-((5-(thiophen-2-yl)thiazol-2-yl)methyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol;(8) (2S,3R,4R,5S,6R)-2-(4-Chloro-3-((5-(5-chlorothiophen-2-yl)thiazol-2-yl)methyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol;(9) (2S,3R,4R,5S,6R)-2-(3-(2,5 ...

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Номер записи: 10
25-04-2013 дата публикации

AMORPHOUS ROXITHROMYCIN COMPOSITION

Номер: US20130102550A1
Автор: Aucamp Marique, Liebenberg Wilna
Принадлежит: North-West University

This invention relates to a macrolide composition, more particularly an amorphous form (Form-III) of 3R, 4S, 5S, 6R, 7R, 9R, 11S, 12R, 13S, 14R-6-[(2S, 3R, 4S, 6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7, 12, 13-trihydroxy-4-[(2R, 4R, 5S, 6S)-5-hydroxy-4-methoxy-4, 6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxy-imino)-3, 5, 7, 9, 11, 13-hexamethyl-1-oxacyclotetradecan-2-one or roxithromycin characterised by the absence of peaks in the infra-red spectrum of amorphous (Form-III) of roxithromycin at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 relative to the infra-red spectrum of the prior art roxithromycin raw material displaying peaks at 3577.15; 3526.03; 3465.27 and 3276.24 cm-1 and further characterised by an increased solubility of at least 50% over prior art anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5), phosphate buffer (pH 6.8) and water. 1. A composition comprising an amorphous form (Form-III) of roxithromycin.2. A composition according to characterised by the absence of peaks in the infra-red spectrum of the amorphous (Form-III) of roxithromycin at 3577.15; 3526.03; 3465.27 and 3276.24 cmrelative to the infra-red spectrum of the prior art roxithromycin raw material displaying peaks at 3577.15; 3526.03; 3465.27 and 3276.24 cm.3. A composition according to wherein the amorphous form (Form-III) of roxithromycin displays an infra-red pattern substantially as depicted in .4. A composition according to having at least 50% increased solubility over anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5).5. A composition according to having at least 150% increased solubility over anhydrous and monohydrated roxithromycin in acetate buffer (pH 4.5).6. A composition according to having at least 50% increased solubility over anhydrous and monohydrated roxithromycin in phosphate buffer (pH 6.8).7. A composition according to having at least 100% increased solubility over anhydrous and monohydrated roxithromycin in ...

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Номер записи: 11
16-05-2013 дата публикации

Antifungal and Antiparasitic Polyene Macrolides

Номер: US20130123205A1
Автор: Tunac Josefino B.
Принадлежит: ACEA BIOTECH, INC.

In certain aspects, the present disclosure provides for novel, water-soluble polyene macrolides and salts or solvates thereof and methods of making the water-soluble polyene macrolides. Also provided are compositions and methods for inhibiting, preventing, and/or treating fungal and parasitic diseases in a subject. 23-. (canceled)5. The compound of claim 1 , wherein X is a cation of aluminum claim 1 , calcium claim 1 , lithium claim 1 , magnesium claim 1 , or zinc.67.-. (canceled)87. The compound of claim claim 1 , wherein Xis a cation of an amine claim 1 , C-Calkyl claim 1 , halo-C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Csulfinylalkyl claim 1 , C-Csulfonylalkyl claim 1 , C-Cthioalkyl claim 1 , C-Caminoalkyl claim 1 , C-Chydroxyalkyl claim 1 , arylalkyl claim 1 , cycloalkyl claim 1 , heterocycle claim 1 , or heteroaryl.9. The compound of claim 8 , wherein X is a cation of an amine and the amine is tetramethylammonium claim 8 , ammonia claim 8 , ethylenediamine claim 8 , N- methylglucamine claim 8 , lysine claim 8 , arginine claim 8 , orthinine claim 8 , choline claim 8 , N claim 8 ,N′ dibenzylethylenediamine claim 8 , chloroprocaine claim 8 , diethanolamine claim 8 , procaine claim 8 , N-benzylphenethylamine claim 8 , 1-p-chlorobenzyl-2-pyrrolidine-1′-methylbenzimidazole claim 8 , diethylamine claim 8 , piperazine claim 8 , morpholine claim 8 , 2 claim 8 , 4 claim 8 , 4-trimethyl-2-pentamine claim 8 , or tris(hydroxymethyl)aminomethane.1027.-. (canceled)2930.-. (canceled)3129. The method of claim claim 8 , wherein X is sodium.3229. The method of claim claim 8 , wherein X is potassium.3329. The method of claim claim 8 , wherein X is calcium.3436.-. (canceled)37. The method of claim 28 , wherein the parasitic infection is a protozoal infection.38. The method of claim 37 , wherein the parasitic infection is leishmaniasis.39. The method of claim 38 , wherein the parasitic infection is visceral leishmaniasis.40. The method of claim 38 , wherein the ...

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Номер записи: 12
23-05-2013 дата публикации

C-ARYL GLUCOSIDE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF

Номер: US20130130997A1
Автор: Dong Qing, Fan Jiang, Guan Dongliang, Shen Guangyuan, Tang Peng Cho, Tu Wangyang, Wang Yang, Yang Fanglong, Yuan Jijun, Zhang Limin
Принадлежит:

C-aryl glucoside derivatives, preparation processes and pharmaceutical uses thereof are disclosed. In particular, C-aryl glucoside derivatives represented by formula (I), with each substituent defined in the application, pharmaceutically acceptable salts or stereoisomers thereof, their preparation methods, and pharmaceutical compositions containing the derivatives as well as their uses as therapeutic agents, particularly as sodium-dependent glucose cotransporter (SGLT)-1 inhibitors, are disclosed. 3. The compound of formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof according to claim 1 , wherein ring A is aryl claim 1 , wherein the aryl is optionally substituted by one or more groups selected from the group consisting of halogen claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , cycloalkyl claim 1 , heterocyclyl claim 1 , aryl claim 1 , heteroaryl claim 1 , —OR claim 1 , —S(O)R claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , —NRRand —C(O)NRR claim 1 , wherein the alkyl claim 1 , cycloalkyl claim 1 , heterocyclyl claim 1 , aryl and heteroaryl are each independently and optionally substituted by one or more groups selected from the group consisting of deuterium claim 1 , halogen claim 1 , alkenyl claim 1 , alkynyl claim 1 , nitro claim 1 , cyano claim 1 , alkoxyl claim 1 , cycloalkyl claim 1 , —OR claim 1 , —S(O)R claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , —NRRand —C(O)NRR.4. The compound of formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof according to claim 3 , wherein R claim 3 , Rand Rare each independently hydrogen; and Ris halogen.5. The compound of formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof according to claim 3 , wherein ring A is phenyl claim 3 , wherein the phenyl is optionally substituted by 1 to 5 groups independently selected from the group consisting of halogen and —OR; Ris alkyl claim 3 , wherein the alkyl is optionally substituted by 1 to 3 groups independently ...

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Номер записи: 13
23-05-2013 дата публикации

Analogues of Etoposide for the Treatment of Tumours

Номер: US20130130998A1
Автор: Nalan Utku
Принадлежит: Cellact Pharma GMBH

Compounds for treatment of a patient having a tumour that is metastatic and/or that reduces an organ function, wherein the compounds are of the general formula: wherein X is O, NH and S, wherein n is 0, 1 or 2, wherein R 1 and R 2 are H, methyl or ethyl, or together form a group CR 3 R 4 , and wherein R 3 and R 4 are H, methyl or ethyl.

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Номер записи: 14
06-06-2013 дата публикации

PYRAZOLE DERIVATIVES

Номер: US20130142757A1
Автор: FANG Yang, LE Xiaoyong, Li Chenxi, Shen Weisheng
Принадлежит:

Disclosed are compounds of general formula (I), wherein R, R, R, R, R, R, X, Y, Z, A and B are as defined in the application. 2. The compound of claim 1 , wherein A and B together with carbons to which A and B attach represent optionally substituted aryl or optionally substituted cyclohydrocarbyl.3. The compound of claim 1 , wherein X is oxygen.4. The compound of claim 1 , wherein Y and Z are each nitrogen.5. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , optionally substituted alkyl and optionally substituted haloalkyl.6. The compound of claim 1 , wherein R is selected from the group consisting of hydrogen claim 1 , optionally substituted alkyl claim 1 , optionally substituted haloalkyl claim 1 , optionally substituted cyclohydrocarbyl and optionally substituted heterocyclyl.7. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rare independently selected from hydrogen and optionally substituted alkyl.8. The compound of claim 1 , wherein A and B together with carbons to which A and B attach represent phenyl claim 1 , cyclopentyl or cyclohexyl.9. The compound of any one of to claim 1 , wherein R is selected from the group consisting of alkyl claim 1 , phenyl claim 1 , alkylpyrrolidinyl claim 1 , haloalkylpyrrolidinyl claim 1 , cyclohydrocarbyl pyrrolidinyl and alkylpiperidyl.10. The compound of claim 1 , which is selected from the group consisting of(2S,3S,4S,5R,6S)-6-(1,3-dimethyl-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinoline-5-oxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-formic acid;(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(1-isopropyl-3-methyl-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinoline-5-oxy)-tetrahydro-2H-pyran-2-formic acid;(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(1-phenyl-3-methyl-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinoline-5-oxy)-tetrahydro-2H-pyran-2-formic acid;(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(3-methyl-1-((R)-1-propylpyrrolidin-2-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c] ...

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Номер записи: 15
06-06-2013 дата публикации

TANAPROGET DERIVATIVES, METABOLITES, AND USES THEREOF

Номер: US20130143827A1
Автор: Chandrasekaran Appavu, DeMaio William, Keating Kelly, McConnell Oliver J., Shen Li
Принадлежит: WYETH LLC

A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided. 1. A method for detecting metabolites of tanaproget in a sample , said method comprising:(a) isolating said metabolite of tanaproget in said sample;(b) characterizing said metabolite of tanaproget to determine the structure of said metabolite of tanaproget; and(c) comparing said structure to the structures of synthetic N- and S-glucuronide derivatives of tanaproget.2. The method according to claim 1 , wherein said synthetic glucuronide derivative of tanaproget is an S-glucuronide derivative.3. The method according to claim 1 , wherein said synthetic glucuronide derivative of tanaproget is an N-glucuronide derivative.4. An antibody generated using a synthetic glucuronide derivative of tanaproget claim 1 , said antibody being specific for tanaproget or a derivative thereof.5. The antibody according to claim 4 , wherein said synthetic glucuronide derivative of tanaproget is an S-glucuronide derivative.6. The antibody according to claim 4 , wherein said synthetic glucuronide derivative of tanaproget is an N-glucuronide derivative.7. A kit for monitoring therapy with tanaproget claim 6 , said kit comprising an antibody according to .8. A method for detecting metabolites of tanaproget claim 6 , said method comprising detecting binding to an antibody according to .9. A method for detecting metabolites of tanaproget claim 6 , said method comprising comparison of a sample to a tanaproget derivative selected from the group consisting of:(a) an enzymatically derived tanaproget glucuronide derivative;(b) tanaproget having a sulfate moiety located on the thiocarbonyl group;(c) tanaproget having a hydroxy group located on the pyrrole ring;(d) tanaproget having a hydroxy group located on the phenylpyrrole ring; and(e) tanaproget having a carbamate located on the thiocarbonyl ...

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Номер записи: 16
13-06-2013 дата публикации

Process for extracting materials from biological material

Номер: US20130149322A1
Автор: Frank Hollman, Geert-Jan Witkamp, Jacob Van Spronsen, Robert Verpoorte, Young Hae Choi
Принадлежит: UNIVERSITEIT LEIDEN

The invention is directed to a process for extracting materials from biological material, which process is characterized in that the naturally occurring biological material is treated with an extractant consisting of a deep eutectic solvent of natural origin or a an ionic liquid of natural origin to produce a biological extract of natural origin dissolved in the said solvent or ionic liquid.

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Номер записи: 17
13-06-2013 дата публикации

Trioxacarcins and uses thereof

Номер: US20130150314A1
Автор: Andrew G. Myers, Daniel J. Smaltz, Jakub Svenda, Nicholas E. Hill, Robert T. Yu, Thomas Magauer
Принадлежит: Harvard College

The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; and methods of use and treatment.

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Номер записи: 18
20-06-2013 дата публикации

Polyol modified aminoglycoside-lipid conjugates

Номер: US20130157969A1
Автор: Frank Schweizer, George Zhanel, Smritilekha Bera
Принадлежит: University of Manitoba

In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof. Additionally, methods of treating and preventing bacterial infections using the aminoglycoside derivatives are also provided

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Номер записи: 19
27-06-2013 дата публикации

Nucleoside phosphoramidates

Номер: US20130165401A1
Автор: Bruce Ross, Byoung-Kwon Chun, Ganapati REDDY PAMULAPATI, Hai-Ren Zhang, Michael Joseph Sofia, Peiyuan Wang, Suguna Rachakonda
Принадлежит: GILEAD PHARMASSET LLC

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

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Номер записи: 20
27-06-2013 дата публикации

6,11-BRIDGED BIARYL MACROLIDES

Номер: US20130165641A1
Автор: Kim Heejin, Kim In Jong, Liu Tongzhu, Long Jiang, Or Yat Sun, Phan Ly Tam, Qiu Yao-Ling, Wang Guoqiang, Wang Yanchun
Принадлежит: Enanta Pharmaceuticals, Inc.

The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1. A compound represented by the formula (I) or (II):as well as the pharmaceutically acceptable salts, esters and prodrugs thereof, wherein:{'sub': 3', '1', '2', '1', '2, 'claim-text': (a) hydrogen;', {'sub': 3', '3', '1', '6', '2', '6', '2', '6, '(b) —R, wherein Ris substituted or unsubstituted —C-Calkyl, —C-Calkenyl, or —C-Calkynyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N;'}, {'sub': 4', '4, 'claim-text': (i) hydrogen;', '(ii) aryl; substituted aryl; heteroaryl; substituted heteroaryl;', {'sub': '3', '(iii) —R; and'}, {'sub': 5', '5', '3', '12, '(iv) —R, wherein Ris substituted and unsubstituted —C-Ccycloalkyl each containing 0, 1, 2, or 3 heteroatoms selected from O, S or N;'}], '(c) —C(O)R; wherein Ris independently selected from the group consisting of, {'sub': '4', '(d) —C(O)NHR;'}, {'sub': '4', '(e) —C(O)OR; and'}, {'sub': 2', '4, '(f) —S(O)R;'}], 'T is hydrogen, OR, halogen or NRR, wherein Rand Rare each independently selected from{'sub': 1', '2, 'alternatively, Rand Rcan be taken together with the nitrogen they are attached with to form a fused or non-fused, substituted or unsubstituted heterocyclic ring;'}{'sub': '1', 'Yis S or O;'}{'sub': 2', '3', '10', '10', '3', '2', '3, 'Yand Yare each independently selected S, N, O or CR; wherein Ris independently selected from hydrogen, hydroxy, amino, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamino, substituted or unsubstituted dialkylamino, CF, CN, NO, N, sulfonyl, acyl, aliphatic, and substituted aliphatic;'}{'sub': 1', '3', '2, 'provided that when either Yor Yis S and Yis CH or N, T is not hydrogen;'}{'sub': 1', '2', '3', '10, 'X, Xand Xare each independently selected N or CR;'}Cy is substituted or unsubstituted heterocyclic, or substituted or unsubstituted heteroaryl; (a) hydrogen;', {'sub': '3', '(b) —R;'}, {'sub': '4', ...

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Номер записи: 21
04-07-2013 дата публикации

Anthracycline-Antibody Conjugates for Cancer Therapy

Номер: US20130171176A1
Автор: GOLDENBERG David M., Griffiths Gary L., HANSEN Hans J., Qu Zhengxing
Принадлежит: IMMUNOMEDICS, INC.

The invention relates to therapeutic conjugates with the ability to target various antigens. The conjugates contain a targeting antibody or antigen binding fragment thereof and an anthracycline chemotherapeutic drug. The targeting antibody and the chemotherapeutic drug are linked via a linker comprising a hydrazide moiety. 1. A method of treating a CD74-expressing cancer , comprising administering to a human subject a conjugate of an anthracycline drug and a humanized anti-CD74 antibody or antigen-binding fragment thereof comprising human antibody framework (FR) and constant region sequences , wherein the humanized anti-CD74 antibody competes for binding to CD74 with an LL1 antibody comprising the light chain complementarity determining region (CDR) sequences CDR1 (RSSQSLVHRNGNTYLH , SEQ ID NO:1) , CDR2 (TVSNRFS , SEQ ID NO:2) and CDR3 (SQSSHVPPT , SEQ ID NO:3) and heavy chain CDR1 (NYGVN , SEQ ID NO:4) , CDR2 (WINPNTGEPTFDDDFKG , SEQ ID NO:5) , and CDR3 (SRGKNEAWFAY , SEQ ID NO:6).2. The method of claim 1 , wherein the anthracycline drug is conjugated to the antibody or fragment thereof with 4-(N-maleimidomethyl)cyclohexane-1-carboxyl hydrazide claim 1 ,3. The method of claim 1 , wherein the humanized antibody comprises human antibody constant region sequences selected from the group consisting of IgG1 claim 1 , IgG2 claim 1 , IgG3 and IgG4.4. The method of claim 1 , wherein said anthracycline drug is selected from the group consisting of daunorubicin claim 1 , doxorubicin claim 1 , epirubicin claim 1 , 2-pyrrolinodoxorubicin claim 1 , morpholino-doxorubicin claim 1 , and cyanomorpholino-doxorubicin.5. The method of claim 1 , wherein said anthracycline drug is linked to the antibody through the 13-keto moiety.6. The method of claim 1 , wherein the cancer is selected from the group consisting of B-cell lymphoma claim 1 , B-cell leukemia claim 1 , multiple myeloma claim 1 , non-Hodgkin's lymphoma claim 1 , Hodgkin's lymphoma claim 1 , breast cancer claim 1 , lung ...

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Номер записи: 22
04-07-2013 дата публикации

NOVEL THIOPHENE DERIVATIVE AS SGLT2 INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

Номер: US20130172278A1
Автор: Lee Jinhwa, Lee Suk Ho, Song Kwang-Seop
Принадлежит: GREEN CROSS CORPORATION

The present invention relates to a novel compound with thiophene ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The prevention also provides a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating metabolic disorders, particularly diabetes. 2. The compound according to claim 1 , wherein{'sub': 1-7', '1-7', '1-7', '1-7', '2-7', '2-7', '3-10', '1-7', '6-14', '1-7', '2-7', '2-7', '3-10', '5-10', '6-14', '2-8', '2-8', '7-15', '7-15, 'claim-text': in which', 'said alkyl, alkenyl, alkynyl, alkoxy, or acyl is optionally substituted with a substituent selected from the group consisting of halogen, hydroxy, cyano, nitro, amino, and mercapto;', {'sub': 1-4', '1-4, 'said cycloalkyl, cycloalkenyl, aryl, aroyl, heteroaryl, heteroaroyl, or heterocycloalkyl is optionally substituted with a substituent selected from the group consisting of halogen, hydroxy, cyano, nitro, amino, mercapto, Calkyl, and Calkoxy; and'}, 'said heterocycloalkyl, heteroaryl, and heteroaroyl each independently contains at least one heteroatom selected from the group consisting of N, O and S., 'the ring B is thiophene, oxazole, thiazole, oxadiazole, or thiadiazaole, in which said ring B is optionally substituted with at least one substituent selected from the group consisting of halogen, hydroxy, mercapto, cyano, carboxy, amino, mono- or di-Calkylamino, guanidino, ureido, Calkoxy, Calkoxy, Calkoxy, Calkenyloxy, Calkynyloxy, Ccycloalkyloxy, 5 to 10-membered heterocycloalkyloxy, Calkylsulfanyl, Carylsulfanyl, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Ccycloalkenyl, Caryl, 5 to 13-membered heteroaryl, Cacyl, Cacyloxy, 6 to 14-membered heteroaroyloxy, Caroyl, Caroyloxy, or 5 to 10-membered heterocycloalkyl ...

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Номер записи: 23
04-07-2013 дата публикации

HYDROGEN BOND FORMING FLUORO KETOLIDES FOR TREATING DISEASES

Номер: US20130172280A1
Автор: Pereira David E.
Принадлежит: CEMPRA PHARMACEUTICALS, INC.

The invention described herein pertains to a novel macrolide antibacterial agent of formula (I): A-L-Q, as defined herein, and pharmaceutically acceptable salts, solvates, and hydrates thereof. Inter alia, the new macrolide antibacterial agent is active against a number of bacterial species, including resistant species. 2. The compound or salt of wherein A is capable of forming a hydrogen bond interaction selected from the group consisting of hydrogen bond donation to O4′ of A752 claim 1 , hydrogen bond donation to 06 of G748 claim 1 , and hydrogen bond acceptance from N1 of G748.3. The compound or salt of wherein A is capable of forming a hydrogen bond interaction selected from the group consisting of hydrogen bond donation to O4′ of A752 claim 1 , and hydrogen bond donation to 06 of G748.4. The compound or salt of wherein(a) A is capable of forming a hydrogen bond interaction selected from the group consisting of hydrogen bond donation to O4′ of A752, hydrogen bond donation to 06 of G748, and hydrogen bond acceptance from N1 of G748; and(b) the 3-keto group of Q is capable of forming a hydrogen bond interaction with U2609; and(c) the aminosaccharide of Q is capable of forming a hydrogen bond interaction with A2059; and(d) the aminosaccharide of Q is capable of forming a hydrogen bond interaction with G2505.5. The compound or salt of wherein the atom of A involved in hydrogen bond donation or acceptance is connected to 11-N of Q by a chain of at least about 9 atoms claim 1 , where the chain may optionally be included in one or more cyclic groups.68.-. (canceled)9. The compound or salt of wherein the atom of A involved in hydrogen bond donation or acceptance is a nitrogen or an oxygen.10. The compound or salt of wherein A comprises a heterocyclic ring and the atom of A involved in hydrogen bond donation or acceptance is an atom of the heterocyclic ring.1113.-. (canceled)14. The compound or salt of wherein Ris F.15. The compound or salt of wherein the 2-fluoro group ...

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Номер записи: 24
25-07-2013 дата публикации

COMPOUNDS FOR INHIBITION OF CANCER CELL PROLIFERATION

Номер: US20130190258A1
Автор: CASHMAN John, MERCOLA Mark, SCHADE Dennis, TSUDA Masanao
Принадлежит:

Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R, R, R, R, R, R, R, R, R, Rare as described herein. 4. A method for inhibiting cancer cell proliferation claim 1 , the method comprising contacting the cancer cell with a compound of Formula I of .5. The method of claim 1 , wherein the compound of Formula I is in the form of a free base or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate or N-oxide thereof; and wherein A claim 1 , B claim 1 , D claim 1 , E claim 1 , F claim 1 , G claim 1 , I claim 1 , J claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , are as described in .6. The method of claim 4 , wherein contact with the cancer cells and the compound of Formula I lasts for a period of time between about 24 hours and about 192 hours or between about 48 hours and about 144 hours.7. The method of claim 4 , wherein the cancer cells comprise colon cancer claim 4 , prostate cancer claim 4 , breast cancer claim 4 , ovarian cancer claim 4 , uterine cancer claim 4 , liver cancer claim 4 , malignant melanoma claim 4 , pancreatic cancer claim 4 , gastric cancer and glioblastoma or other brain cancers.8. The method of claim 4 , further comprising contacting the cancer cells with a cytotoxic or chemotherapeutic anti-cancer drug by co-administration.9. The method of claim 4 , wherein cancer cell proliferation is inhibited.10. The method of claim 4 , further comprising contacting the cancer cells with a sulfonamide that inhibits a Wnt pathway protein or stimulates HIPK2.11. The method of claim 10 , wherein the Wnt pathway protein is TCF4.12. The method of claim 4 , wherein the cancer cells are cancer stem cells.13. The method of claim 4 , ...

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Номер записи: 25
01-08-2013 дата публикации

Novel process for the preparation of 9-deoxo-9a-aza-9a-homoerythromycin a, modified in the c-44" of the cladinose ring by an epoxide group

Номер: US20130197204A1
Автор: Albert Codony, Oriol Martorell, Rafael Garcia
Принадлежит: Individual

The present invention concerns a process for the preparation of the compound of formula The compound of formula (1) is the key intermediate in the synthesis of some antibacterial agents of the triamilide class, such as Tulathromycin, useful to treat bacterial and protozoa infections.

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Номер записи: 26
08-08-2013 дата публикации

GLYCOSIDE DERIVATIVES AND USES THEREOF

Номер: US20130203975A1
Автор: BEBERNITZ Gregory Raymond, Bock Mark Gary
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; 63. The compound of anyone of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein n is 0.736. The compound of anyone of - and claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein q is 0.8. The compound of anyone of the preceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein V is —OR.9. The compound of anyone of the preceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein R claims 1 , R claims 1 , and Rare hydrogen.10. The compound of anyone of the preceding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Ris halo claims 1 , Calkyl claims 1 , or Ccycloalkyl.11. The compound of anyone of the preceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Ris bromo claims 1 , ethyl or cyclopropyl.12. The compound of anyone of the preceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Ris ethyl.13. The compound of anyone of the proceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein X is O.1412. The compound of anyone of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein X is S.1512. The compound of anyone of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein X is S(O).1612. The compound of anyone of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein X is NR.17. The compound of anyone of the proceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Ris Calkyl claims 1 , haloCalkyl claims 1 , Ccycloalkyl claims 1 , phenyl claims 1 , or a 5- to 6-membered heteroaryl.18. The compound of anyone of the proceeding claims claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Ris methyl.19. The compound of claim 16 , or a ...

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Номер записи: 27
15-08-2013 дата публикации

METALLODRUGS HAVING IMPROVED PHARMACOLOGICAL PROPERTIES AND METHODS OF MANUFACTURE AND USE THEREOF

Номер: US20130210705A1
Автор: COWAN Ada S., COWAN James A.
Принадлежит: METALLOPHARM LLC

It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms. 1. An antimicrobial composition , comprising:a first moiety which is (i) an antimicrobial peptide (“AMP”), or peptide that binds to a pathogenic target, the sequence of which is between 6 and 100 amino acids, is net positively charged, and is amphipathic, (ii) an antibiotic, or (iii) a conjugate comprising an AMP, or peptide that binds to a pathogenic target, and an antibiotic; anda second moiety which is a metal binding moiety,wherein the first moiety and the second moiety are covalently linked to form a complex, andwherein the first moiety promotes uptake of the complex into a target cell or organelle.2. A composition according to claim 1 , wherein the first moiety comprises an antimicrobial peptide claim 1 , or peptide that binds to a pathogenic target claim 1 , that adopts a structure selected from the group consisting of an α-helix claim 1 , a β-hairpin-like beta-sheet claim 1 , a beta-sheet claim 1 , or an α-helix/beta-sheet mixed structure.3. A composition according to claim 2 , wherein the antimicrobial peptide claim 2 , or peptide that binds to a pathogenic target claim 2 , adopts an amphipathic α-helical structure.4. A composition according to claim 2 , wherein the antimicrobial peptide claim 2 , or peptide that binds to a pathogenic target claim 2 , adopts a structure comprising antiparallel β-sheets.5. A composition according to claim 2 , wherein the antimicrobial peptide claim 2 , or peptide that binds to a pathogenic target claim 2 , adopts an extended backbone ...

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Номер записи: 28
05-09-2013 дата публикации

Modified drugs for use in liposomal nanoparticles

Номер: US20130230582A1
Автор: Igor Jigaltsev, Marcel Bally, Marco Ciufolini, Norbert Maurer, Pieter Cullis
Принадлежит: The University of British Columbia

Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.

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Номер записи: 29
05-09-2013 дата публикации

ANTI-BACTERIAL ACTIVITY OF 9-HYDROXY DERIVATIVES OF 6,11-BICYCLOLIDES

Номер: US20130231298A1
Автор: Iyengar Rajesh, Or Yat Sun, Phan Ly Tam, Wang Yanchun
Принадлежит: Enanta Pharmaceuticals, Inc.

The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: 8. A pharmaceutical composition comprising a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , ester or prodrug thereof claim 1 , in combination with a pharmaceutically acceptable carrier.9. A method for treating a bacterial infection in a subject claim 8 , comprising administering to said subject a therapeutically effective amount of a pharmaceutical composition according to .10. A method of treating cystic fibrosis in subject claim 8 , comprising administering to said subject claim 8 , a therapeutically effective amount of a pharmaceutical composition of .11. A method of treating inflammation in a subject comprising administering to said subject claim 8 , therapeutically effective amount of a pharmaceutical composition of . This application is a continuation of U.S. application Ser. No. 12/437,616, filed May 8, 2009, which claims the benefit of U.S. Provisional Application No. 61/051,991, filed on May 9, 2008. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to novel semisynthetic macrolides having antibacterial activity that are useful in the treatment and prevention of bacterial infections. More particularly, the invention relates to spC9 oxygenated compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.The spectrum of activity of macrolides, including erythromycin, covers most relevant bacterial species responsible for upper and lower respiratory tract infections. 14-membered ring macrolides are well known for their overall efficacy, safety and lack of serious side effects. Erythromycin, however, is quickly degraded into inactive products in the acidic medium of the stomach resulting in low bioavailability and gastrointestinal side effects. Improvement of ...

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Номер записи: 30
05-09-2013 дата публикации

POLYETHERESTER POLYOLS AND THE USE THEREOF FOR PRODUCING RIGID POLYURETHANE FOAMS

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

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

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Номер записи: 31
05-09-2013 дата публикации

Method for preparing albiflorin and paeoniflorin

Номер: US20130231469A1
Автор: Zuoguang Zhang
Принадлежит: Individual

The present invention discloses a method for preparing high purity paeoniflorin and albiflorin simultaneously comprising: extraction the raw material Paeonia Lactiflora by percolation or heating reflux to obtain the Paeonia Lactiflora extract solution, then purification by macroporous absorption resin, alumina column and silica gel column in turn to obtain high purity paeoniflorin and albiflorin. The preparation method of the invention can provide high purity paeoniflorin and albiflorin with low price and energy-consumption by the identical procedure. The process is simple. The purification efficacy is high and the purification time is short.

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Номер записи: 32
19-09-2013 дата публикации

STANDARDIZED PLANT EXTRACT, PROCESS FOR OBTAINING THE SAME AND USES THEREOF

Номер: US20130243860A1
Автор: BITTENCOURT Christiane Meire da Silva, BRESOLIM Tania Mari Belle, DE SOUZA Marcia Maria, FILHO Valdir Cechinel, LUCINDA Ruth Meri, MORA Ticiana Camila, NITA Marcelo Eidi, PEDREIRA Marcello Creado, PICOLLI Carlos, QUINTAO Nara Lins Meira, SPRICIGO Rodrigo
Принадлежит:

The present invention refers to a process for obtaining a standardized extract having antinociceptive, anti-inflammatory and antipyretic properties, from at least one part of a plant of genus . Furthermore, the present invention provides a pharmaceutical composition comprising an active ingredient of a pharmaceutically efficient quantity of standardized extract from at least one part of the plant of genus . Finally, the present invention describes a method of treatment and use of the said extract, isolated or in a pharmaceutical composition, for the prevention, control or treatment of painful, inflammatory or febrile affections. 141-. (canceled)42AleuritesAleurites. A standardized extract of at least one part of a plant of the genus , wherein said extract is distinguished by at least one of the aspects selected from the group consisting of: (i) chromatograms by high performance liquid chromatography (HPLC) specific to the soft extract and dry extract of the said plant of genus , (ii) NMR 0spectrums of the 2″-O-rhamnosylswertisin marker measured at 300 MHz in deuterated methanol , (iii) NMR Hspectrums of the 2″-O-rhamnosylswertisin marker measured at 300 MHz in deuterated methanol , (iv) chromatograms by high efficiency liquid chromatography of the 2″-O-rhamnosylswertisin standardized purified by preparative thin-layer chromatography and (v) infra-red spectrum of the 2″-O-rhamnosylswertisin marker.43. The extract according to claim 42 , wherein said HPLC chromatograms specific for soft extract and dry extract are represented in claim 42 , but not limited to claim 42 , .44. The extract according to claim 42 , wherein said NMR Cspectrums are represented in claim 42 , but not limited to claim 42 , .45. The extract according to claim 42 , wherein said NMR Hspectrums are represented in claim 42 , but not limited to claim 42 , .46. The extract according to claim 42 , wherein said HPLC chromatograms of the 2″-O-rhamnosylswertisin standard are represented in claim 42 , but ...

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Номер записи: 33
26-09-2013 дата публикации

Glycomimetic compounds as anti-infectious against pathogens lectins

Номер: US20130252910A1
Автор: Anne Imberty, Benoit Guery, Karine Faure, Samy Cecioni, Sébastien Vidal, Susan Matthews
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite Claude Bernard Lyon 1 UCBL

The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH 2 -group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group, a halogen atom, a —CH 2 R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl) 2 group, a NH(alkyl) group, or E represents a —CO—R′ wherein R′ is a hydrogen atom, a hydroxyl group or an amino, B represents a A-C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH 2 ) i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II). The present invention also relates to a pharmaceutical composition characterized in that it comprises the said calixarene-based glycosylated compound (I), in combination with pharmaceutically acceptable carriers or diluents. The present invention also relates to the use of the said calixarene-based glycosylated compound (I) or the said pharmaceutical composition, for the manufacture of a drug intended to prevent or treat bacterial infections from pathogens that use lectins in the first steps of infection.

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Номер записи: 34
26-09-2013 дата публикации

Macrolide Polymorphs, Compositions Comprising Such Polymorphs, and Methods of Use and Manufacture Thereof

Номер: US20130252914A1
Автор: Che Tessie Mary, Chiu Yu-Hung, Ichikawa Yoshi, Romero Alex, Shue Youe-Kong
Принадлежит: OPTIMER PHARMACEUTICALS, INC.

The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to (“”), (“”), species, for example, methicillin-resistant , or including Vancomycin-resistant enterococci. 1. A crystalline polymorph of tiacumicin comprising a powder x-ray diffraction pattern with at least peaks at diffraction angles 2θ of 7.7° , 15.0° , and 18.8°±0.2.3. The crystalline polymorph of claim 2 , further comprising at least one compound selected from a mixture of tiacumicins.4. The crystalline polymorph of claim 2 , wherein the polymorph of Formula I is present in at least about 75% to about 99.99%.5. The crystalline polymorph of claim 4 , wherein the polymorph of Formula I is present in at least about 85%.6. The crystalline polymorph of claim 4 , wherein the polymorph of Formula I is present in at least about 90%.7. The crystalline polymorph of claim 4 , wherein the polymorph of Formula I is present in at least about 95%.8. The crystalline polymorph of claim 4 , wherein the polymorph of Formula I is present in at least about 99%.10. The crystalline polymorph of claim 9 , further comprising at least one compound selected from a mixture of tiacumicins.11. The crystalline polymorph of claim 9 , wherein the polymorph of Formula I is present from about 75% to about 99.99%.12. The crystalline polymorph of claim 9 , wherein the polymorph of Formula I is present in at least about ...

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Номер записи: 35
26-09-2013 дата публикации

CRYSTALLINE FORMS OF A MACROLIDE, AND USES THEREFOR

Номер: US20130252915A1
Автор: Pereira David E.
Принадлежит: CEMPRA PHARMACEUTICALS, INC.

New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein. 1. The compound CEM-101 in crystalline form.2. The form of which is Form I of CEM-101 having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=6.2 claim 1 , 8.5 claim 1 , 8.8 claim 1 , 10.5 claim 1 , 13.2 claim 1 , and 18.6.3. The form of which is Form I of CEM-101 having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=8.8 claim 1 , 10.5 claim 1 , 13.2 claim 1 , and 18.6.4. The form of which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=6.2 and 8.8.5. The form of which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=8.5 and 8.8.6. The form of which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=6.2 claim 1 , 8.5 claim 1 , and 8.8.7. CEM-101 claim 2 , comprising Form I of CEM-101 according to having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=8.5 claim 2 , 8.8 claim 2 , 10.5 claim 2 , 13.2 claim 2 , and 18.6.8. CEM-101 according to that is substantially free of Form II.9. CEM-101 according to as determined by the X-ray powder diffraction pattern claim 7 , wherein one or more peaks at °2θ=5.6 claim 7 , 7.9 claim 7 , 9.8 claim 7 , or 11.7 are absent or nearly absent.10. CEM-101 according to as determined by the X-ray powder diffraction pattern claim 7 , wherein one or more peaks at °2θ=5.6 or 7.9 are absent or nearly absent.11. The form of which is Form II of CEM-101 having an X-ray powder diffraction ...

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Номер записи: 36
26-09-2013 дата публикации

Uridine diphosphate derivatives, compositions and methods for treating neurodegenerative disorders

Номер: US20130252919A1
Автор: Jinbo Lee, Jinghui DONG, Philip Haydon, Raquel REVILLA-SANCHEZ, Stephen Moss
Принадлежит: TUFTS UNIVERSITY

This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P 2 Y 6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.

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Номер записи: 37
10-10-2013 дата публикации

PROCEDURE FOR THE PURIFICATION OF TIACUMICIN B

Номер: US20130267692A1
Автор: Fonte Piera, Lazzari Giovanni
Принадлежит: OLON S.p.A.

The present invention relates to an improved process for the purification of tiacumicin B. Specifically, the invention relates to a simplified, optimised process for the purification of tiacumicin B from a fermentation broth, using chromatography techniques. In particular, the invention relates to a method for purifying tiacumicin B which comprises subjecting a liquid containing tiacumicin B to at least one hydrophobic interaction chromatography step. 1. A process for purifying tiacumicin B comprising subjecting a liquid containing tiacumicin B to at least one hydrophobic interaction chromatography step.2. The process according to wherein the hydrophobic interaction chromatography uses a styrene-divinylbenzene resin.3. The process according to wherein the hydrophobic interaction chromatography uses a styrene-divinylbenzene resin selected from the group consisting of HP20 claim 2 , HP21 claim 2 , HP20SS claim 2 , SP20 claim 2 , SP2OSS claim 2 , SP825 claim 2 , SP850 claim 2 , SP207 claim 2 , XAD16 claim 2 , XAD1600 and XAD18.4. The process according to wherein the resin is HP20SS.5. The process according to wherein the hydrophobic interaction chromatography comprises the following steps:a) loading the liquid containing tiacumicin B at a pH ranging from 2.0 to 8.0 onto the hydrophobic interaction resin;b) eluting the impurities from the hydrophobic interaction resin with a mixture consisting of water and an organic solvent selected from methanol, ethanol, acetonitrile, acetone, THF or a mixture thereof at a pH ranging from 2.0 to 8.0;c) eluting tiacumicin B from the hydrophobic interaction resin with a mixture consisting of water and an organic solvent selected from methanol, ethanol, acetonitrile, acetone, THF or a mixture thereof at a pH ranging from 2.0 to 8.0;6. The process according to wherein the liquid containing tiacumicin B is loaded at a pH ranging from 2.5 to 6.5 onto the hydrophobic interaction resin.7. The process according to wherein the pH of the eluent ...

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Номер записи: 38
17-10-2013 дата публикации

Sesterterpene Compounds and Use Thereof

Номер: US20130274212A1
Автор: Giri Awadut Gajendra, Kang Heon joong, Kim Eun Oh, Kim Jung Ah, Mallepally Venkat Reddy, Won Dong Hwan, Yang In Ho
Принадлежит: SNU R&DB FOUNDATION

The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed. 3. A pharmaceutical composition for preventing and treating diabetes claim 1 , diabetes complications claim 1 , vascular diseases claim 1 , fatty liver disease claim 1 , or obesity claim 1 , the pharmaceutical composition containing the sesterterpene compound of Chemical Formula I of claim 1 , a stereoisomer thereof claim 1 , an enantiomer thereof claim 1 , an in vivo-hydrolysable precursor thereof claim 1 , or a pharmaceutically acceptable salt thereof.4. The pharmaceutical composition of claim 3 , wherein the diabetes complications foot ulcer and renal failure.5. The pharmaceutical composition of claim 3 , wherein the vascular diseases are hyperlipidemia claim 3 , atherosclerosis claim 3 , and atherosclerotic stroke.6. The pharmaceutical composition of claim 3 , wherein the fatty liver diseases are alcoholic claim 3 , non-alcoholic claim 3 , or viral fatty liver diseases.7. A pharmaceutical composition for preventing and treating vascular diseases claim 1 , the pharmaceutical composition containing the sesterterpene compound of Chemical Formula I of claim 1 , a stereoisomer thereof claim 1 , an enantiomer thereof claim 1 , an in vivo-hydrolysable precursor thereof claim 1 , or a pharmaceutically ...

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Номер записи: 39
17-10-2013 дата публикации

GLYCOSYLATED AMINOCOUMARINS AND METHODS OF PREPARING AND USES OF SAME

Номер: US20130274213A1
Автор: Yang Min
Принадлежит: UNIVERSITY COLLEGE LONDON

There is provided a method of glycosylating an aminocoumarin compound comprising conjugating a sugar to the 4′-OH position of the core of the aminocoumarin compound. Also provided is an aminocoumarin compound glycosylated at the 4′-OH position of the core of the aminocoumarin compound. Further aspects of this invention provide this compound for use in therapy, more particularly for use as an antibiotic, or in anticancer treatment. 1. A method of glycosylating an aminocoumarin compound comprising conjugating a sugar to the 4′-OH position of the core of the aminocoumarin compound.2. A method according to wherein the sugar is chemically conjugated to the 4′-OH position of the aminocoumarin core.3. A method according to wherein the sugar is enzymatically conjugated to the 4′-OH position of the aminocoumarin core.4. A method according to wherein the enzyme is a plant glycosyltransferase or a mutant thereof.5. A method according to wherein the sugar is selected from glucose and galactose.8. A method according to wherein the aminocoumarin is an antibiotic selected from Novobiocin claim 1 , Clorobiocin and Coumermycin.9. An aminocoumarin compound glycosylated at the 4′-OH position of the core of the aminocoumarin compound.10. An aminocoumarin compound according to having a sugar conjugated to the 4′-OH position of the core of the aminocoumarin compound wherein the sugar is selected from glucose and galactose.12. An aminocoumarin compound according to for use in therapy.13. An aminocoumarin compound according to for use as an antibiotic.14. An aminocoumarin compound according to for use in anticancer treatment.15. A pharmaceutical composition comprising an aminocoumarin compound according to and one or more pharmaceutically acceptable excipients.17. An aminocoumarin compound according to claim 9 , wherein the aminocoumarin is an antibiotic selected from Novobiocin claim 9 , Clorobiocin and Coumermycin. The present invention relates to methods of glycosylating aminocoumarins, ...

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Номер записи: 40
07-11-2013 дата публикации

Process for producing a particulate composition comprising anhydrous crystalline 2-o-alpha-d-glucosyl-l-ascorbic acid

Номер: US20130295618A1
Автор: Seisuke Izawa, Shigeharu Fukuda, Takashi Shibuya, Tomoyuki Nishimoto, Toshio Miyake
Принадлежит: Hayashibara Co Ltd

The invention provides a process for enabling the production of a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside that does not significantly cake even when the production yield of ascorbic acid 2-glucoside does not reach 35% by weight. The process for producing a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside, which comprises allowing a CGTase to act on a solution containing either liquefied starch or dextrin and L-ascorbic acid and then allowing a glucoamylase to act on the resulting solution to obtain a solution with an ascorbic acid 2-glucoside production yield of at least 27%, purifying the obtained solution to increase the ascorbic acid 2-glucoside content to a level of over 86% by weight, precipitating anhydrous crystalline ascorbic acid 2-glucoside by a controlled cooling method or pseudo-controlled cooling method, collecting the precipitated anhydrous crystalline ascorbic acid 2-glucoside, and ageing and drying the collected anhydrous crystalline ascorbic acid 2-glucoside.

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Номер записи: 41
14-11-2013 дата публикации

NOVEL PYRAZOLE COMPOUNDS

Номер: US20130303471A1
Автор: MANTLO Nathan Bryan, QU Fucheng
Принадлежит: ELI LILLY AND COMPANY

The present invention provides a compound of Formula II: 4. A method of treating diabetes in a patient comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .5. A method of treating type 1 diabetes in a patient comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .6. A method of treating type 2 diabetes in a patient comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .7. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients.8. The pharmaceutical composition according to claim 7 , further comprising one or more other therapeutic agents. The present invention relates to novel pyrazole compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders, and to intermediates and processes useful in the synthesis of the compounds.The present invention is in the field of treatment of diabetes and other diseases and disorders associated with hyperglycemia. Diabetes is a group of diseases that is characterized by high levels of blood glucose. It affects approximately 25 million people in the United States and is also the 7leading cause of death in U.S. according to the 2011 National Diabetes Fact Sheet (U.S. Department of Health and Human Services, Centers for Disease Control and Prevention). Sodium-coupled glucose cotransporters (SGLT's) are one of the transporters known to be responsible for the absorption of carbohydrates, such as glucose. More specifically, SGLT1 is responsible ...

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Номер записи: 42
14-11-2013 дата публикации

SOLID STATE FORMS OF FIDAXOMYCIN AND PROCESSES FOR PREPARATION THEREOF

Номер: US20130303472A1
Автор: ARVAI Edit Nagyne, FONAGY Tamas, KOVACSNE-MEZEI Adrienne, SZUROS Levente
Принадлежит:

The present invention provides solid state forms of Fidaxomycin, processes for preparing the solid state forms, as well as pharmaceutical compositions and formulations comprising one or more of the solid state forms of Fidaxomycin, and processes for the preparation of the compositions and formulations. The solid state forms of the present invention exhibit advantageous properties such as improved reliability and reproducibility in manufacturing and processing and stability in formulations. 1. A crystalline form of Fidaxomycin , wherein the crystalline form is{'figref': {'@idref': 'DRAWINGS', 'FIG. 4'}, 'crystalline form of Fidaxomycin, designated as Form Z1, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at: 4.3, 8.2 and 11.2 degrees two theta ±0.2 degrees two theta; a powder X-ray diffraction pattern substantially as depicted in ; and by combinations of these data;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 8'}, 'crystalline Form Z of Fidaxomycin characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at: 4.1, 9.7, 10.2, 11.2 and 15.6 degrees two theta ±0.2 degrees two theta; a powder X-ray diffraction pattern substantially as depicted in ; and by combinations of these data; or'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 7'}, 'crystalline form of Fidaxomycin, designated as Form C, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at: 6.8, 7.9, 10.0, 10.2, 12.2, 13.4, 14.6, 15.4, 16.4, 17.5, 18.4 and 23.1 degrees two theta ±0.1 degrees two theta; a powder X-ray diffraction pattern substantially as depicted in ; and by combinations of these data.'}2. The crystalline form of Fidaxomycin of claim 1 , wherein the crystalline form is Form Z1 characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at: 4.3 claim 1 , 8.2 and 11.2 ...

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Номер записи: 43
05-12-2013 дата публикации

5'-END DERIVATIVES

Номер: US20130323836A1
Автор: Lima Walter F., Manoharan Muthiah, Prakash Thazha P., Rajeev Kallanthottathil G., Swayze Eric E., Zlatev Ivan
Принадлежит: Isis Pharmaceuticals, Inc.

The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. 13-. (canceled)68-. (canceled)9. The compound of wherein Y′ and Y″ are independently for each occurrence (CH)OH claim 4 , (CH)SCH claim 4 , (CH)SH claim 4 , COR claim 4 , (CH)COR claim 4 , (CH)NQQ claim 4 , OP(Z)(Y)NQQ claim 4 , OP(Z)(X)Y claim 4 , linear or branched alkyl claim 4 , aryl claim 4 , heteroaryl claim 4 , or heterocyclic.10. The compound of wherein n is 1-4.11. (canceled)12. The compound of wherein Ris OH or alkoxy.1317-. (canceled)18. The compound of wherein Zis oligonucleotide.19. An oligonucleotide comprising at least one compound of .20. (canceled)21. The oligonucleotide of wherein the oligonucleotide comprises:1-20 first-type regions, each first-type region independently comprising 1-20 contiguous nucleosides wherein each nucleoside of each first-type region comprises a first-type modification;0-20 second-type regions, each second-type region independently comprising 1-20 contiguous nucleosides wherein each nucleoside of each second-type region comprises a second-type modification; and0-20 third-type regions, each third-type region independently comprising 1-20 contiguous nucleosides wherein each nucleoside of each third-type region comprises a third-type modification,{'sub': 3', '2', '3, 'wherein the first-type modification, the second-type modification, and the third-type modification are each independently selected from 2′-F, 2′-OCH, 2′-0(CH)2OCH, BNA, F—HNA, 2′-H and 2′-OH.'}22. The oligonucleotide of claim 19 , wherein the oligonucleotide comprises at least one non-phosphodiester internucleoside linkage.23. The oligonucleotide of claim 22 , wherein the non-phosphodiester internucleoside ...

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Номер записи: 44
05-12-2013 дата публикации

SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES

Номер: US20130324531A1
Автор: Bartkovitz David Joseph, Chu Xin-Jie, Ehrlich George Kenneth, Liu Jin-Jun, Michel Hanspeter, Vu Binh Thanh, Zhao Chunlin
Принадлежит: Hoffmann-La Roche Inc.

There are provided compounds of the formula 2. The compound of whereinX is selected from H, F or Cl,{'sub': '1', 'Y is selected from H, F or C,'}{'sub': '1', 'Ris lower alkyl or substituted lower alkyl,'}{'sub': 3', '2', '3', '2', '2', '2', 'n', '2', '2', 'n', '3', '2', '2', 'n', '4', '2', '2', '2', '2', 'n', '2', '2', '2', 'n', '3', '2', '2', 'n', '3', '2', '2', 'n', '2', '2', '2', 'n', '3', '5', '2', '5', '2', '2', '5', '2', '5', '2', '2', 'n', '2', '2', '2, 'Ris selected from the group consisting of lower alkoxy, substituted lower alkoxy, alkylamino, dialkylamino, glucuronic acid, hexoses, aminohexoses, pyranoses, aminoglycosides, natural and unnatural amino acids, —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)—NHand —OCHCH-amino acid, wherein n is from 3 to 60,'}{'sub': '4', 'Ris hydrogen or benzyl,'}{'sub': '5', 'Ris selected from the group consisting of heterocycles, substituted heterocycles, dialkylamino, alkylamino and aminoalkyl alcohols,'}or a pharmaceutically acceptable salt or ester thereof.3. The compound of whereinX is selected from H, F or Cl,Y is selected from H, F or Cl,{'sub': '1', 'Ris lower alkyl or substituted lower alkyl,'}{'sub': 3', '2', '3', '2', '2', '2', 'n', '2', '2', 'n', '3', '2', '2', 'n', '4', '2', '2', '2', '2', 'n', '2', '2', '2', 'n', '3', '2', '2', 'n', '3', '2', '2', 'n', '2', '2', '2', 'n', '3', '5', '2', '5', '2', '2', '5', '2', '5', '2', '2', 'n', '2', '2', '2, 'Ris selected from the group consisting of lower alkoxy, substituted lower alkoxy, alkylamino, dialkylamino, glucuronic acid, hexoses, aminohexoses, pyranoses, aminoglycosides, natural and unnatural amino acids, —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)—NHand — ...

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Номер записи: 45
12-12-2013 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FXR

Номер: US20130331349A1
Автор: Alper Phillip B., Chianelli Donatella, MUTNICK Daniel, RUCKER Paul Vincent, Tully David C.
Принадлежит:

The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR). 2. The compound of claim 1 , wherein Ris cyclopropyl.3. The compound of claim 1 , wherein Z is phenylene claim 1 , pyridylene claim 1 , pyrimidinylene claim 1 , pyrazinylene claim 1 , pyridazinylene claim 1 , thiazolylene claim 1 , benzothiazolyl claim 1 , benzo[d]isothiazolyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , quinolinyl claim 1 , 1H-indolyl claim 1 , pyrrolo[1 claim 1 ,2-b]pyridazinyl claim 1 , benzofuranyl claim 1 , benzo[b]thiophenyl claim 1 , 1H-indazolyl claim 1 , benzo[d]isoxazolyl claim 1 , quinazolinyl claim 1 , 1H-pyrrolo[3 claim 1 ,2-c]pyridinyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyrimidinyl claim 1 , imidazo[1 claim 1 ,2-b]pyridazinyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl; each of which is optionally substituted with 1-2 Rradicals selected from halogen claim 1 , Calkyl claim 1 , haloCalkyl claim 1 , Calkoxy claim 1 , haloCalkoxy claim 1 , or cyclopropyl.7. The compound of claim 1 , wherein Ris phenyl substituted with 1-3 R; and{'sup': '1a', 'sub': 1-6', '1-6', '1-6', '1-6, 'Ris halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy.'}8. The compound of claim 1 , wherein Ris —X—COR; X is a bond and Ris hydrogen or Calkyl.9. The compound of claim 1 ,{'sup': '6', 'wherein Ris methyl, methoxy, fluoro or trifluoromethoxy.'}10. The compound of claim 1 , wherein said compound is selected frommethyl 2-[3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylate;methyl 2-[(1R,3r,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylate;2-[3-({5-cyclopropyl-3-[ ...

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Номер записи: 46
12-12-2013 дата публикации

E-selectin antagonists

Номер: US20130331350A1
Автор: Beat Ernst, Céline E. Weckerle, Jonas K. Egger
Принадлежит: Glycomimetics Inc

Compounds, compositions and methods are provided for inhibiting in vitro and in vivo processes mediated by E-selectin binding. More specifically, particular glycomimetic compounds are described, wherein the compounds are E-selectin antagonists.

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Номер записи: 47
19-12-2013 дата публикации

Novel Compound Isolated from Allium tuberosum and Use Thereof as Antiviral Agent

Номер: US20130338090A1
Автор: Cho Sang Buem, Kim Soo Ki, Lee Jun Hyeong, Moon Hyung In, Paik Hyun Dong, Seo Sang Heui
Принадлежит:

The present invention relates to a novel compound isolated from and the use thereof as an antiviral agent. The compound isolated from shows the ability to inhibit highly pathogenic virus, and thus is a promising candidate for an antiviral agent. 2Allium tuberosumAllium tuberosum. A method of obtaining the compound of from claim 1 , the method comprising the steps of: treating with an organic solvent to obtain an organic solvent extract;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'suspending the organic solvent extract in water; treating the suspension with chloroform to obtain an chloroform fraction; and obtaining the compound of from the chloroform fraction.'}3. The method of claim 2 , wherein the organic solvent is a Cto Calcohol.4. The method of claim 3 , wherein the alcohol is methanol.5. A pharmaceutical composition for preventing or treating viral disease claim 1 , comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof.6. The pharmaceutical composition of claim 5 , wherein the viral disease is avian influenza viral disease.7. The pharmaceutical composition of claim 6 , wherein the avian influenza virus is H5N1-serotype avian influenza virus.8Allium tuberosum.. A feed composition for preventing or treating viral disease claim 1 , comprising the compound of or a methanol fraction of9. The feed composition of claim 8 , wherein the viral disease is avian influenza virus.10. The feed composition of claim 9 , wherein the avian influenza virus is H5N1-serotype avian influenza virus.11. A method for preventing or treating viral disease claim 1 , comprising a step of administering an effective amount of the compound of or a pharmaceutically acceptable salt thereof to a subject in need of prevention or treatment of viral disease.12. The method of claim 11 , wherein the viral disease is avian influenza viral disease.13. The method of claim 12 , wherein the avian influenza virus is H5N1-serotype avian influenza virus.14Allium tuberosum. ...

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Номер записи: 48
26-12-2013 дата публикации

HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE

Номер: US20130345157A1
Автор: Arvanitis Argyrios G., Galya Laurine G., Li Mei, Nedza Frank M., Rodgers James D., Shepard Stacey, Shilling Adam
Принадлежит: INCYTE CORPORATION

The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile. 28-. (canceled)12. A compound of claim 1 , which is:6-(3-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acidor a pharmaceutically acceptable salt of any of the aforementioned.13. A compound of claim 1 , selected from:6-(1-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;6-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyano-1-cyclopentylethoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;6-(2-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;6-(2-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-cyano-2-cyclopentylethoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid; and6-(3-(1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-2-cyanoethyl)cyclopentyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;or a pharmaceutically acceptable salt of any of the aforementioned.14. A compound which is:6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acidor a pharmaceutically acceptable salt of any of the aforementioned.15. A compound selected from:6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-6-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid;6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid; and6-(4-(1-(2-cyano-1-cyclopentylethyl)-1H- ...

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Номер записи: 49
26-12-2013 дата публикации

Novel antibacterial agents

Номер: US20130345410A1
Автор: Alex Romero, Chan-Kou Hwang, Chang-Hsing Liang, David Rabuka, Jonathan Duffield, Kenneth Marby, Steve Sucheck, Sulan Yao, Yoshiaka Ichikawa, Youe-Kong Shue, Yu-Hung Chiu
Принадлежит: Optimer Pharmaceuticals LLC

Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

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Номер записи: 50
02-01-2014 дата публикации

KETOLIDE COMPOUNDS

Номер: US20140005133A1
Автор: Bhagwat Sachin, BHAVSAR Satish, Dekhane Deepak, Deshpande Prasad, Diwakar Santosh, GUPTA Sunil, Jafri Mohammad, Mishra Amit, Patel Mahesh, Patil Vijay, Pawar Shivaji, Solanki Manish, Tadiparthi Ravikumar, TRIVEDI Bharat
Принадлежит:

The invention relates to ketolide compounds of Formula (I) and their pharmaceutically acceptable salts, solvates, hydrates, polymorphs and stereoisomers having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compounds of invention, wherein, T is —C*H(R)—P-Q; Ris hydrogen; unsubstituted or substituted lower alkyl, cycloalkyl or aryl; P is heteroaryl ring; Q is unsubstituted or substituted aryl or heteroaryl ring; and P is attached to Q via carbon-carbon link; and Ris hydrogen or fluorine, With the provision that when Ris hydrogen, Ris fluorine. 2. A compound as claimed in claim 1 , wherein:{'sub': '1', 'T is —C*H(R)—P-Q;'}{'sub': '1', 'Ris hydrogen;'}{'sub': '3', 'Ris fluorine;'}P is 5 or 6-membered heteroaryl ring with up to three heteroatoms;Q is unsubstituted or substituted aryl or 5 or 6-membered heteroaryl ring; andP is attached to Q via carbon-carbon link.312-. (canceled)13. A compound as claimed in claim 1 , wherein:{'sub': '1', 'T is —C*H(R)—P-Q;'}{'sub': '1', 'Ris unsubstituted or substituted lower alkyl, cycloalkyls, or aryl;'}P is heteroaryl ring;Q is unsubstituted or substituted aryl or heteroaryl ring; andP is attached to Q via carbon-carbon link; and{'sub': '3', 'Ris hydrogen or fluorine.'}1416-. (canceled)17. A compound as claimed in claim 1 , wherein:{'sub': '1', 'T is —C*H(R)—P-Q;'}{'sub': '1', 'Ris methyl;'}P is 5-membered heteroaryl ring with up to three heteroatoms;Q is unsubstituted or substituted aryl or heteroaryl ring with up to two nitrogens; andP is attached to Q via carbon-carbon link; and{'sub': '3', 'Ris hydrogen or fluorine.'}18. (canceled)19. A compound as claimed in claim 1 , wherein:{'sub': '1', 'T is —C*H(R)—P-Q;'}{'sub': '1', 'Ris methyl;'}P is 5-membered heteroaryl ring such as isoxazole or thiadiazole;Q is pyridine or pyrimidine; andP is attached to Q via carbon-carbon link; and{'sub': '3', 'Ris ...

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Номер записи: 51
02-01-2014 дата публикации

Method of extracting kaempferol-based antioxidants from solenostemma arghel

Номер: US20140005373A1
Автор: Amani Shafeek Awaad, Reham Moustafa El-Meligy
Принадлежит: KING SAUD UNIVERSITY

The method of extracting kaempferol-based antioxidants from Solenostemma arghel provides a method of producing medicinal antioxidants for usage as anti-inflammatory and analgesic treatments. The kaempferol-based antioxidants are primarily kaempferol-3,4′-diglucoside and kaempferol 3-rutinoside. The method includes the following steps: collecting aerial parts of Solenostemma arghel; drying the aerial parts; powdering the aerial parts; extracting the powdered aerial parts in ethanol and filtering to produce a filtrate; concentrating the filtrate to form a concentrated residue; dissolving the concentrated residue in water; and extracting the kaempferol-based antioxidant from the dissolved residue in ethyl acetate.

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Номер записи: 52
09-01-2014 дата публикации

NOVEL MACROLIDE DERIVATIVE

Номер: US20140011757A1
Автор: Kurihara Kenichi, Mitomi Masaaki
Принадлежит: MEIJI SEIKA PHARMA CO., LTD.

The inventors of the present invention have succeeded in acquiring a compound having excellent antibacterial activities against pathogens of respiratory tract infections in animals through the use of josamycin as a lead scaffold. 2. A drug claim 1 , comprising as an active ingredient the compound or the pharmacologically acceptable salt thereof according to .3. The drug according to claim 2 , which is used as an antibacterial drug.4. A pharmaceutical composition claim 1 , comprising as an active ingredient the compound or the pharmacologically acceptable salt thereof according to claim 1 , and an additive for formulation.5. An animal drug claim 1 , comprising as an active ingredient the compound according to .6. An animal antibacterial drug claim 1 , comprising as an active ingredient the compound according to . The present invention relates to a novel macrolide derivative effective as a therapeutic drug for bacterial infections in animals.Among macrolides as animal antibacterial drugs, erythromycin, tylosin, and tilmicosin are mainly used as injection preparations or oral preparations for treating bacterial respiratory tract infections in cattle and swine. Further, natural products classified as leucomycin-type 16-membered ring macrolides, such as josamycin, kitasamycin, and spiramycin, do not have indications as therapeutic drugs for respiratory tract infections in cattle, but are used as oral antibacterial agents for treating bacterial respiratory tract infections in swine.Meanwhile, among antibacterial drugs for respiratory tract infections in humans, macrolides that are most frequently used in clinical practice at present are clarithromycin, which is obtained by 6-O-methylation of erythromycin, and azithromycin, which is an azalide-type 15-membered ring macrolide obtained by introduction of a nitrogen atom into a lactone ring of erythromycin.Tulathromycin is a recently developed azalide-type 15-membered ring macrolide exclusively for animals. Tulathromycin was ...

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Номер записи: 53
16-01-2014 дата публикации

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

Номер: US20140018309A1
Автор: Kaul Ramesh, McEachern Ernest J., Mu Changwei, Selnick Harold G., Vocadlo David J., Wang Yaode, Wei Zhongyong, Zhou Yuanxi, Zhu Yongbao
Принадлежит:

The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. 2. The compound of wherein:{'sup': 1', '2', '1', '2', '1', '2', '1', '2, 'Rand Rare H, or Ris H and Ris F, or Ris F and Ris H, or Ris OH and Ris H;'}{'sup': '4', 'Ris H;'}{'sup': '5', 'Ris OH;'}{'sup': '6', 'Ris H or OH; and'}{'sup': 8', '8, 'sub': 3', '2', '3', '2', '2', '3', '2', '2', '2', '2, 'each Ris independently selected from the group consisting of: H, CH, CHCH, (CH)CH, CHCH═CH, and CHC≡CH, or NRis azetidin-1-yl,'}{'sup': 6', '7, 'with the proviso that when Ris OH, each Ris H;'}{'sup': 1', '6, 'with the proviso that either Ror Ris other than OH.'}3. The compound of wherein at least one of R claim 1 , R claim 1 , R claim 1 , and Ris F.5. (canceled)6. The compound of wherein the compound is selected from the following group:(3aR,5R,6S,7R,7aR)-2-(ethylamino)-5-methyl-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6S,7aR)-2-(ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6S,7aR)-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6S,7aR)-2-(dimethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6S,7aR)-2-amino-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6S,7aR)-5-(hydroxymethyl)-2-(propylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6R,7R,7aR)-2-(ethylamino)-7-fluoro-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6R,7R,7aR)-2-(dimethylamino)-7-fluoro-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-6-ol;(3aR,5R,6R,7R,7aR)-7-fluoro-5-(hydroxymethyl)-2-(methylamino)-5 ...

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Номер записи: 54
30-01-2014 дата публикации

ANTI-INFLAMMATORY MACROLIDES

Номер: US20140031307A1
Автор: Bauerlein Christiane, Burnet Michael W., Eggers Mary, Guse Jan-Hinrich
Принадлежит: Synovo GmbH

The invention provides novel compounds and compositions and methods for making and using the compounds and compositions. 4. A method for producing a compound of claim 1 , the method comprising the step of oxidizing a descladinosyl macrocyclic compound.5. The method of claim 4 , in which the step of oxidizing comprises oxidizing using the Swern reaction.6. A pharmaceutical composition comprising a compound or salt of and a pharmaceutically acceptable carrier.7. A method of treating an inflammatory disorder claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound or salt of .8. A method of treating an infectious disease claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound or salt of .9. A method of treating allergy claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound or salt of .10. A method of treating an immune disorder claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound or salt of .11. A method of manufacturing a pharmaceutical composition for the treatment of an autoimmune disease claim 1 , the method comprising mixing a compound or salt of with a suitable pharmaceutically acceptable carrier. This application claims priority to U.S. Provisional Application No. 61/391,679, filed Oct. 10, 2010, the contents of which are incorporated herein by reference in their entirety.Macrocyclic lactones, and in particular, the “macrolides” are naturally derived and semi-synthetic compounds with a range of biological activities. Amongst the best known of these activities is antibiotic activity through binding to the bacterial ribosome. Certain of these compounds do, however, have other activities including anti-inflammatory activity (see European patent publication 0283055). In recent years, macrocycles may have been used as drug carriers in which an active ...

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Номер записи: 55
30-01-2014 дата публикации

COMPOUNDS

Номер: US20140031534A1
Автор: BORGOS Sven Even Finn, BRAUTASET Trygve, ELLINGSEN Trond Erling, OLSUFYEVA Evgenia Nikolaevna, PREOBRAZHENSKAYA Maria Nikolaevna, SLETTA Havard, ZOTCHEV Sergey Borisovich
Принадлежит: BIOSERGEN AS

The present invention provides a compound which is a nystatin derivative having an additional double bond present between C28 and C29 and which is further modified relative to nystatin at one or more of positions C5, C7, C9, C10, C11, C16 or at the amino group of mycosamine. 132.-. (canceled)34. A compound as claimed in which is modified at position C5 relative to nystatin.35. A compound as claimed in which is modified at C9 relative to nystatin.36. A compound as claimed in which is modified at C10 relative to nystatin.37. A compound as claimed in which is modified at the amino group of mycosamine.38. A compound as claimed in wherein Rrepresents a hydrogen atom claim 33 , a hydroxyl group or an alkoxy group (e.g. a group —OC) and Ris a hydrogen atom or wherein Rand Rtogether form a carbonyl group.39. A compound as claimed in claims 33 , wherein Rrepresents a hydrogen atom claims 33 , a hydroxyl group or an alkoxy group (e.g. a group —OC) and Ris a hydrogen atom or wherein Rand Rtogether form a carbonyl group.40. A compound as claimed in claim 33 , wherein Rrepresents a hydrogen atom claim 33 , a hydroxyl group or an alkoxy group (e.g. a group —OC) and Ris a hydrogen atom41. A compound as claimed in claim 33 , wherein Rrepresents a hydrogen atom claim 33 , an alkylamino group claim 33 , a sugar or an acyl group and Ris identical to Ror is a hydrogen atom claim 33 , e.g. Ris a hydrogen atom.43. A compound as claimed in wherein Ris methyl claim 42 , CONH(CH)N(CH)or CONH(CH)OH where n is 2 or 3.44. A compound as claimed in claim 33 , wherein Ris an alkylamino group of the formula —(CH)NHor —(CH)N(Calkyl)wherein x is 2 to 6 or is a monosaccharide selected from glucose claim 33 , galactose claim 33 , glucopyranose claim 33 , mannopyranose claim 33 , galactopyranose claim 33 , fructopyranose and tagotopyranose or is an oligosaccharide selected from lactose claim 33 , melibiose claim 33 , sucrose claim 33 , maltose and cellobiose.45. A compound as claimed in claim 33 , ...

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Номер записи: 56
30-01-2014 дата публикации

NOVEL GLYCOSYLTRANSFERASE GENE AND USE THEREOF

Номер: US20140033369A1
Автор: MATSUI Keisuke, Okitsu Naoko, Tanaka Yoshikazu
Принадлежит: SUNTORY HOLDINGS LIMITED

Provided is a polynucleotide encoding a protein having an activity to transfer a sugar to the hydroxy groups at the 4′- and 7-positions of a flavone. The polynucleotide is selected from the group consisting of: (a) a polynucleotide which comprises a base sequence represented by SEQ ID NO: 1, 3, or 12; (b) a polynucleotide which hybridizes to a polynucleotide comprising a base sequence complementary to a base sequence represented by SEQ ID NO: 1, 3, or 12 under high stringency conditions, and encodes a protein having an activity to transfer a sugar to the hydroxy groups at the 4′- and 7-positions of a flavone; (c) a polynucleotide which encodes a protein comprising an amino acid sequence represented by SEQ ID NO: 2, 4, or 13; (d) a polynucleotide which encodes a protein comprising an amino acid sequence in which one or more amino acids have been deleted, substituted, inserted, and/or added in an amino acid sequence represented by SEQ ID NO: 2, 4, or 13 and having an activity to transfer a sugar to the hydroxy groups at the 4′- and 7-positions of a flavone; etc. 1. A polynucleotide selected from the group consisting of:(a) a polynucleotide comprising a base sequence defined in SEQ ID NO: 1, 3 or 12;(b) a polynucleotide which hybridizes with a polynucleotide comprising a base sequence complementary to a base sequence defined in SEQ ID NO: 1, 3 or 12 under a stringent condition and encodes a protein having an activity of transferring a glycosyl to both of the hydroxyl groups at 4′- and 7-positions of a flavone;(c) a polynucleotide which encodes a protein comprising an amino acid sequence defined in SEQ ID NO: 2, 4 or 13;(d) a polynucleotide which encodes a protein comprising an amino acid sequence in which one or several amino acids have been deleted, substituted, inserted, and/or added in an amino acid sequence defined in SEQ ID NO: 2, 4 or 13 and having an activity of transferring a glycosyl to both of the hydroxyl groups at 4′- and 7-positions of a flavone; and(e) a ...

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Номер записи: 57
06-02-2014 дата публикации

NOVEL MACROLIDE INTERMEDIATE AND NOVEL PRODUCTION PROCESS

Номер: US20140039171A1
Автор: Kurihara Kenichi, Minoma Nobuto, Mitomi Masaaki
Принадлежит: MEIJI SEIKA PHARMA CO., LTD.

Provided are: a novel monoalkylamino intermediate (I); and a production method for a compound represented by the formula (III), which is an animal antibacterial agent, via the novel monoalkylamino intermediate. 3. A compound according to claim 2 , wherein Rand Reach represent an ethyl group.4. A compound according to claim 2 , wherein Rrepresents a methyl group claim 2 , and Rrepresents an isobutyl group.7. A production method for the compound represented by the formula (II) as defined in claim 2 , comprising allowing a compound represented by the formula (IV) to react with an organophosphorous reagent and subsequently with paraformaldehyde and subjecting the resultant to a reduction reaction.8. A production method for the compound represented by the formula (II) as defined in claim 3 , comprising allowing a compound represented by the formula (IV) to react with an organophosphorous reagent and subsequently with paraformaldehyde and subjecting the resultant to a reduction reaction.9. A production method for the compound represented by the formula (II) as defined in claim 4 , comprising allowing a compound represented by the formula (IV) to react with an organophosphorous reagent and subsequently with paraformaldehyde and subjecting the resultant to a reduction reaction. The present invention relates to a novel production method for a macrolide derivative effective as a therapeutic drug for bacterial infections in animals.The inventors of the present invention have discovered that derivatives of midecamycin modified at the C-12 and C-13 positions have excellent antibacterial activities (WO 2002/064607 A1). In recent years, the inventors have found that a compound represented by the formula (IIIa) out of the derivatives exhibits remarkably strong antibacterial actions against pathogens of bacterial respiratory tract infections in livestock animals such as cattle and swine. The inventors have also found that a compound represented by the formula (IIIb) using josamycin ...

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Номер записи: 58
13-02-2014 дата публикации

Nucleoside phosphoramidate prodrugs

Номер: US20140045783A1
Автор: Dhanapalan Nagarathnam, Jinfa Du, Michael Joseph Sofia, Peiyuan Wang
Принадлежит: GILEAD PHARMASSET LLC

Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment uses, and processes for preparing each of which utilize the compound represented by formula I.

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Номер записи: 59
13-02-2014 дата публикации

C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE

Номер: US20140046043A1
Автор: HAYASHI Masato, Kanemoto Kenichi, Kashimura Masato, Kumura Kou, Kurosaka Jun, Miura Tomoaki, Ogita Haruhisa, Sasamoto Naoki, Shitara Eiki, Sugimoto Tomohiro, Tamura Keiji, Ushiki Yasunobu, Yamamoto Kanako, YOSHIDA Satoshi
Принадлежит:

A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas). 2. The compound according to or a salt thereof claim 1 , or a hydrate or a solvate thereof claim 1 , wherein Ris hydrogen atom claim 1 , a Calkyl group claim 1 , or a Calkylsulfonyl group claim 1 ,{'sup': '2', 'sub': 7-12', '1-6', '1-6', '1-6', '1-6', '1-6, 'Ris a 4- to 8-membered saturated heterocyclic group (the saturated heterocyclic group may be substituted with one or two substituents selected from a Caralkyl group, and a Calkyl group), a Calkanoyl group (the Calkanoyl group may be substituted with amino group, or a Calkylamino group), or a Calkyl group which may be substituted with 1 to 3 substituents selected from the substituent group 1, or'}{'sup': 1', '2, 'sub': 1-6', '1-6', '1-6', '1-6, 'Rand Rmay combine together to form, together with the nitrogen atom to which they bind, a 4- to 8-membered saturated nitrogen-containing heterocyclic group (the saturated nitrogen-containing heterocyclic group may be substituted with 1 to 3 substituents selected from hydroxy group, amino group, a Calkylamino group, and a Calkyl group (the Calkyl group may be substituted with amino group, or a Calkylamino group)), and'}{'sup': 38', '39, 'sub': 1-6', '1-6', '3-6', '7-12', '7-12', '1-6', '1-6, 'Rand R, which may be the same or different, represent hydrogen atom, a Calkyl group (the Calkyl group may be substituted with a Ccycloalkyl group), a Caralkyl group (the Caralkyl group may be substituted with 1 to 3 substituents selected from a halogen atom, a Calkyl group, and a Calkoxy group) or a heteroaralkyl group.'}3. The compound according to or a salt thereof claim 1 , or a hydrate or a solvate thereof claim 1 , wherein Ris a Calkyl group substituted with 1 to 3 substituents selected from the substituent group 1.4. The compound according to or a salt thereof claim 1 , or a hydrate or a solvate thereof claim 1 ...

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Номер записи: 60
06-03-2014 дата публикации

Purification of biological conjugates by size exclusion chromatography

Номер: US20140066605A1
Автор: Christopher A. Tomas, David K. Schisla, Lou-Hwa J. Sheu, Marcela De Leon Gatti, Yingqing Huang
Принадлежит: ABBOTT LABORATORIES

A method for separating a biological conjugate from an aggregate. The molecular weight of the biological conjugate ranges from about 10 kDa to about 1000 kDa. In one embodiment, the method comprises the steps of: (e) providing a mixture comprising the biological conjugate and the aggregate, wherein the biological conjugate has a molecular weight of from about 10 kDa to about 1000 kDa; (f) providing a chromatography column containing a gel, wherein the gel comprises at least one polysaccharide; (g) introducing the mixture of step (a) into the chromatography column; (h) recovering the biological conjugate from the column.

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Номер записи: 61
13-03-2014 дата публикации

Process for preparation of ketolide intermediates

Номер: US20140073770A1
Автор: Birajdar Satish, DHOND Bharat, PATIL Vijaykumar Jagdishwar, Tribedi Bharat Kalidas
Принадлежит:

The inventions discloses a process for preparation of compounds of Formula (IX), Wherein, R is C-Calkyl, Ris hydrogen or a hydroxyl protecting group, and Ris hydrogen or fluorine. 2. The process according to claim 1 , wherein the base used in step (a) is pyridine claim 1 , dimethylaminopyridine or a mixture of pyridine and dimethylaminopyridine.3. The process according to claim 1 , wherein the base used in step (b) or (c) is one or more of sodium bicarbonate claim 1 , sodium carbonate claim 1 , sodium hydride claim 1 , sodium-t-butoxide potassium hydroxide claim 1 , potassium hydride and potassium t-butoxide.4. The process according to claim 1 , wherein the cyanating agent used in step (b) is sodium cyanide claim 1 , potassium cyanide claim 1 , copper cyanide claim 1 , or tosyl cyanide.7. The process according to claim 6 , wherein the de-protecting agent used in step (e) is selected from one or more of hydrochloric acid claim 6 , sulfuric acid and pyridine hydrofluoride9. The process according to claim 8 , wherein the fluorinating agent is one or more of N-fluorobenzenesulfonimide claim 8 , 1-(chloromethyl)-4-fluoro-1 claim 8 ,4 diazo bicyclo [2.2.2]octane bis[tetrafluoroborate] claim 8 , tetrabutylammonium fluoride and diethyl aminosulfur trifluoride.10. The process according to claim 8 , wherein the base is selected from one or more of potassium-t-butoxide claim 8 , potassium hydride claim 8 , sodium bis(trimethylsilyl)amide claim 8 , sodium hydride and sodium-t-butoxide.11. The process according to claim 8 , wherein the solvent is one or more of dichloromethane claim 8 , tetrahydrofuran claim 8 , N-N-dimethylformamide and ethylene dichloride. The invention relates to a process for preparation of compounds of Formula (IX) useful in the synthesis of 11,12-γ lactone ketolide compounds.Wherein,* indicates a chiral center,R is C-Calkyl,Ris hydrogen or hydroxyl protecting group, andRis hydrogen or fluorine.Macrolide compounds represent a well-known family of ...

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Номер записи: 62
20-03-2014 дата публикации

ARYLALKYLAMINE COMPOUND AND PROCESS FOR PREPARING THE SAME

Номер: US20140080770A1
Автор: HISADA Yutaka, MIYAZAKI Hiroshi, OKABE Junko, SAKURAI Osamu, TAKAMURO Iwao, YANAGIDA Tetsuya, YASUDA Kosuke
Принадлежит: MITSUBISHI TANABE PHARMA CORPORATION

An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof. 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein X is —CO— or —(CH)—CO—.37-. (canceled)8. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ar is a group which may be optionally substituted by group(s) selected from lower alkyl and lower alkoxy.9. (canceled)10. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the ring portion of the group represented by Ris the following (i) claim 1 , (ii) or (iii):(i) phenyl;(ii) monocyclic heterocyclic group, hetero ring of which comprises one saturated or unsaturated 5 to 7-membered ring, and contains 1 to 4 hetero atom(s) selected from nitrogen atom, oxygen atom and sulfur atom; or(iii) bicyclic heterocyclic group, hetero ring of which comprises two saturated or unsaturated 5 to 7-membered rings being fused, and contain 1 to 6 hetero atom(s) selected from nitrogen atom, oxygen atom and sulfur atom.11. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the ring portion of the group represented by Ris the following (i) claim 1 , (ii) or (iii):(i) phenyl;(ii) monocyclic heterocyclic group selected from pyrrolidinyl, imidazolidinyl, pyrazolidinyl, oxolanyl, thiolanyl, pyrrolinyl, imidazolinyl, pyrazolinyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, furyl, oxazolyl, isooxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, piperidyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrimidinyl, pyradinyl, pyridazinyl, pyranyl, perhydroazepinyl, perhydrothiazepinyl, partially or completely saturated group thereof, and a group in which the hetero atom(s) (N or S) thereof is/are oxidized; or(iii) bicyclic heterocyclic group selected from indolinyl, isoindolinyl, indolyl, indazolyl, isoindolyl, benzimidazolyl, benzotriazolyl, ...

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Номер записи: 63
27-03-2014 дата публикации

Esters and Malonates of SATE Prodrugs

Номер: US20140086873A1
Автор: MAYES Benjamin Alexander, MOUSSA Adel M.
Принадлежит:

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein are compounds according to Formula 1001: 2. The compound of claim 1 , wherein A is methyl.3. The compound of claim 1 , wherein A and Y claim 1 , together with the atoms to which they are attached claim 1 , combine to form an oxacyclopropyl ring.4. The compound of claim 1 , wherein Z is —(CRR)C(O)O(CRR)CRRR.5. The compound of claim 1 , wherein Z is —(CRR)OC(O)(CRR)CRRR.6. The compound of claim 1 , wherein Y is fluoro.7. The compound of claim 1 , wherein Y is hydroxyl.8. The compound of claim 1 , wherein Ris —CHPh and Ris hydrogen.9. The compound of claim 1 , wherein each Ris independently hydrogen claim 1 , halo claim 1 , C-Calkyl claim 1 , C-Csubstituted alkyl claim 1 , C-Caryl claim 1 , or C-Cheteroaryl.10. The compound of claim 1 , wherein each Ris independently hydrogen claim 1 , halo claim 1 , C-Calkyl claim 1 , C-Csubstituted alkyl claim 1 , C-Caryl claim 1 , or C-Cheteroaryl.11. (canceled)12. (canceled)13. (canceled)15. (canceled)16. (canceled)18. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient claim 1 , carrier or diluent.19. The pharmaceutical composition of claim 18 , wherein the composition is an oral formulation.21. The method of claim 20 , wherein the host is a human.22. The method of claim 20 , wherein the administration directs a substantial amount of the compound claim 20 , or pharmaceutically acceptable salt or stereoisomer thereof claim 20 , to a liver of the host.23. The method of claim 20 , wherein the compound is administered in combination or alternation with a second anti-viral agent selected from the group consisting of an interferon claim 20 , a ...

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Номер записи: 64
27-03-2014 дата публикации

Water soluble and activable phenolics derivatives with dermocosmetic and therapeutic applications and process for preparing said derivatives

Номер: US20140088030A1
Автор: Daniel Auriol, Fabrice Lefevre, Patrick Robe, Renaud Nalin
Принадлежит: Libragen SA

The invention relates to the preparation of phenolics derivatives by enzymatic condensation of phenolics selected among pyrocatechol or its derivatives with the glucose moiety of sucrose. The production of said phenolics derivatives is achieved with a glucosyltransferase (EC 2.4.1.5). These O-α-glucosides of selected phenolics are new, have a solubility in water higher than that of their parent polyphenol and have useful applications in cosmetic and pharmaceutical compositions, such as antioxidative, antiviral, antibacterial, immune-stimulating, antiallergic, antihypertensive, antiischemic, antiarrythmic, antithrombotic, hypocholesterolemic, antilipoperoxidant, hepatoprotective, anti-inflammatory, anticarcinogenic, antimutagenic, antineoplastic, anti-thrombotic and vasodilatory formulations, or in any other field of application.

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Номер записи: 65
27-03-2014 дата публикации

Triazole Compounds and Methods of Making and Using the Same

Номер: US20140088031A1
Автор: Bhattacharjee Ashoke, Kanyo Zoltan F., Sherer Edward C.
Принадлежит: Rib-X Pharmaceuticals, Inc.

The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. 4. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide or prodrug thereof claim 1 , wherein Ris Calkyl claim 1 , optionally substituted with from 1 to 7 fluorines.5. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide or prodrug thereof claim 1 , wherein Ris selected from —CH claim 1 , —CHF claim 1 , —CHF claim 1 , and —CF.7. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 1 or 2.8. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 1.9. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein Ris F.10. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 0.11. A compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein A is selected from: (a) a Calkyl group claim 1 , (b) a Calkenyl group claim 1 , (c) a Calkynyl group claim 1 , (d) a Csaturated claim 1 , unsaturated claim 1 , or aromatic carbocycle claim 1 , (e) a 3-12 membered saturated claim 1 , unsaturated claim 1 , or aromatic heterocycle containing one or more nitrogen claim 1 , oxygen or sulfur atoms claim 1 , (f) —CF claim 1 , (g) —NR(CRR)R claim 1 , (h) —OR claim 1 , (i) —S(CRR)R claim 1 , —S(O)(CRR)R claim 1 , (j) —S(O)(CRR)R claim 1 , (k) —S(O)((CRR)R claim 1 , (l) —C(O)( ...

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Номер записи: 66
27-03-2014 дата публикации

METHOD OF EXTRACTING PHENOLIC FRACTIONS OF EXTRA VIRGIN OLIVE OIL

Номер: US20140088299A1
Автор: Gutierrez Thomas, Harrell C. Chad, Hillhouse M. Christine, Klapish Timothy A.
Принадлежит: PhytoChem Pharmaceuticals, Inc.

The present invention relates to isolating phenolics from extra virgin olive oil (EVOO) having a low triglyceride and non-polar content. The method includes an ethanol/water extraction with a heptane wash 1. A method for isolating phenolics from EVOO , wherein the isolated phenolics have a low triglyceride and non-polar content comprising:a) selecting a desired quantity of EVOO for extraction;b) extracting the EVOO a plurality of times with an ethanol/water solution;c) isolating the ethanol/water solution after each extraction;d) rinsing the ethanol/water solution with a heptane solution;e) isolate the ethanol/water solution from the heptane; andf) evaporate the ethanol/water solution to remove the phenolics from the solution.2. A method according to wherein the plurality isolated solutions of step c) are combined before step d).3. A method according to wherein the evaporation is carried out by a method selected from the list comprising rotary evaporation and speed vacuum evaporation.4. A method according to wherein the ethanol comprises about 50 to 90 percent of the ethanol/water solution.5. A method according to wherein the ethanol comprises about 80 percent of the ethanol/water solution.6. A method according to which further comprises the addition of further ethanol/water solution to the isolated solution in step e) during the evaporation process.7. A phenolic extract of EVOO manufactured by the method of .8. A polar phenolic extract of EVOO comprising EVOO that has been extracted with an ethanol/water solution than then has been washed with a solution of heptane. This application claims priority of U.S. provisional application No. 61/448,265 filed on Mar. 2, 2011 and included herein in its entirety by reference.A portion of the disclosure of this patent contains material that is subject to copyright protection. The copyright owner has no objection to the reproduction by anyone of the patent document or the patent disclosure as it appears in the Patent and ...

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Номер записи: 67
03-04-2014 дата публикации

Triazole Compounds and Methods of Making and Using the Same

Номер: US20140094422A1
Автор: Ashoke Bhattacharjee, Zoltan F. Kanyo
Принадлежит: Melinta Therapeutics Inc

The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. These compounds are represented by the following formula (I): wherein R 1 , R 2 , etc. are defined as in Claim 1.

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Номер записи: 68
03-04-2014 дата публикации

Process for preparation of ketolide compounds

Номер: US20140094600A1
Автор: DEO Keshav, Diwan Furqan Mohammed, Gangakhedkar Kiran Kumar, Varangaonkar Aniruddha
Принадлежит: WOCKHARD LIMITED

A process for the preparation of compound of Formula (I) is provided. Formula-I 2. The process according to claim 1 , wherein the base used in step (a) is one or more of sodium hydroxide claim 1 , potassium hydroxide claim 1 , lithium hydroxide claim 1 , sodium methoxide claim 1 , potassium tert butoxide and sodium ethoxide.3. The process according to claim 1 , wherein the protic solvent used in step (a) is a C-Calcohol.4. The process according to claim 1 , wherein the protic solvent used in step (a) is iso-propanol.5. The process according to claim 1 , wherein the solvent used in step (b) is a non-polar aprotic solvent claim 1 , or a chlorinated solvent claim 1 , or a mixture of a non-polar aprotic solvent and a chlorinated solvent.6. The process according to claim 5 , wherein the non-polar aprotic solvent is one or more of n-hexane claim 5 , benzene and toluene.7. The process according to claim 5 , wherein the chlorinated solvent is one or more of chloroform claim 5 , methylene dichloride claim 5 , ethylene dichloride claim 5 , and chlorobenzene.8. The process according to claim 1 , wherein the de-protection of silyl protecting group is achieved by using methanol-water-HCl. The invention relates to an improved process for the preparation of ketolide compounds.Macrolides are a well-known family of antimicrobial agents. Erythromycin A, a 14-membered macrolide, was isolated in 1952 from Examples of macrolides being used as therapeutic agents are roxithromycin, clarithromycin and azithromycin (azalide). Ketolides are semisynthetic 14-membered ring macrolide derivatives, characterized by the presence of a keto function at position 3 instead of L-cladinose moiety present in the macrolactone ring. Telithromycin and Cethromycin are examples of ketolides.U.S. Pat. No. 4,331,803 discloses 6-O-methyl derivative of erythromycin i.e. Clarithromycin. U.S. Pat. No. 4,349,545 discloses Roxithromycin. The azalide Azithromycin is disclosed in U.S. Pat. No. 4,517,359. Telithromycin ...

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Номер записи: 69
10-04-2014 дата публикации

NOVEL UREA COMPOUNDS

Номер: US20140100179A1
Автор: QU Fucheng
Принадлежит: ELI LILLY AND COMPANY

The present invention provides a compound of Formula I: 3. A method of treating diabetes in a patient comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .4. A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients. The present invention relates to novel urea compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders, and to intermediates and processes useful in the synthesis of the compounds.The present invention is in the field of treatment of diabetes and other diseases and disorders associated with hyperglycemia. Diabetes is a group of diseases that is characterized by high levels of blood glucose. It affects approximately 25 million people in the United States and is also the 7leading cause of death in U.S. according to the 2011 National Diabetes Fact Sheet (U.S. Department of Health and Human Services, Centers for Disease Control and Prevention). Sodium-coupled glucose cotransporters (SGLT's) are one of the transporters known to be responsible for the absorption of carbohydrates, such as glucose. More specifically, SGLT1 is responsible for the transport of glucose across the brush border membrane of the small intestine Inhibition of SGLT1 may result in reduced absorption of glucose in the small intestine, thus providing a useful approach to treating diabetes.U.S. Pat. No. 7,655,632 discloses certain pyrazole derivatives with human SGLT1 inhibitory activity which are further disclosed as useful for the prevention or treatment of a disease associated with hyperglycemia, such as diabetes. In addition, WO 2011/039338 discloses certain pyrazole derivatives with SGLT1/SGLT2 inhibitor activity which are ...

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Номер записи: 70
06-01-2022 дата публикации

SCUTELLARIN AMIDE DERIVATIVES, AND PREPARATION METHODS AND USES THEREOF

Номер: US20220002332A1
Автор: Han Tong, Hua Huiming, Jiang Chunyu, JIN Chenghao, Li Dahong, Xu Xin, Zhang Xinmiao
Принадлежит: HEILONGJIANG BAYI AGRICULTURAL UNIVERSITY

The present disclosure discloses scutellarin amide derivatives and preparation methods and uses thereof, which belongs to the field of natural drugs and medicinal chemistry. The scutellarin amide derivatives according to the present disclosure and pharmaceutically acceptable salts thereof have a structure as shown in the following general formula I: 2. The compound according to claim 1 , wherein R is a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted benzyl group on the benzene ring claim 1 , and the substituent is a C-Calkyl group claim 1 , a C-Calkoxy group; Ris a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted phenyl group claim 1 , and the substituent is halogen claim 1 , a C-Calkyl group or a C-Calkoxy group.3. The compound according to claim 1 , wherein R is methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl or benzyl; Ris ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , phenyl claim 1 , 4-chlorophenyl claim 1 , 3-chlorophenyl claim 1 , 2-chlorophenyl claim 1 , 4-methylphenyl claim 1 , 3-methylphenyl claim 1 , 2-methylphenyl claim 1 , 4-hydroxyphenyl claim 1 , 3-hydroxyphenyl claim 1 , 2-hydroxyphenyl claim 1 , 4-methoxyphenyl claim 1 , 3-methoxyphenyl claim 1 , 2-methoxyphenyl.5. A pharmaceutical composition comprising the compound according to and a pharmaceutically acceptable salt thereof.6. The pharmaceutical composition according to claim 5 , wherein R is a substituted or unsubstituted C-Calkyl group claim 5 , a substituted or unsubstituted benzyl group on the benzene ring claim 5 , and the substituent is a C-Calkyl group claim 5 , a C-Calkoxy group; Ris a substituted or unsubstituted C-Calkyl group claim 5 , a substituted or unsubstituted phenyl group claim 5 , and the substituent is halogen claim 5 , a C-Calkyl group or a C-Calkoxy group.7. The ...

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Номер записи: 71
07-01-2016 дата публикации

Pharmaceutical Compositions for Rectal Administration

Номер: US20160002278A1
Автор: MALHOTRA Geena, Purandare Shrinivas Madhukar
Принадлежит: CIPLA LIMITED

The present invention relates to pharmaceutical compositions for rectal administration comprising fidaxomicin and to a process for preparing the pharmaceutical compositions for rectal administration. The invention also relates to an aerosol canister comprising a foamable pharmaceutical composition comprising fidaxomicin for rectal administration and to the treatment or maintenance of remission of infections such as diarrhea caused by 1. A pharmaceutical composition for rectal administration in the form of a foam comprising fidaxomicin.2. A foamable pharmaceutical composition for rectal administration comprising fidaxomicin.3. The pharmaceutical composition according to claim 1 , wherein fidaxomicin is in the form of a pharmaceutically acceptable derivative thereof.4. The pharmaceutical composition according to claim 3 , wherein the pharmaceutically acceptable derivative of fidaxomicin is a salt claim 3 , solvate claim 3 , complex claim 3 , hydrate claim 3 , isomer claim 3 , ester claim 3 , tautomer claim 3 , anhydrate claim 3 , enantiomer claim 3 , polymorph or prodrug.5. The pharmaceutical composition according to claim 1 , wherein fidaxomicin is present in an amount of from about 0.01% w/w to about 10% w/w based on the total weight of the composition claim 1 , optionally from about 0.5% w/w to about 8% w/w based on the total weight of the composition.6. The pharmaceutical composition according to claim 1 , further comprising one or more pharmaceutically acceptable excipients which are selected from the group comprising: propellants claim 1 , vehicle claim 1 , emollient and/or humectants claim 1 , pH adjusting agent claim 1 , surfactants claim 1 , emulsifiers claim 1 , foaming agents claim 1 , fatty alcohol claim 1 , preservatives claim 1 , chelating agents claim 1 , antioxidants claim 1 , suspending agents claim 1 , thickening agents claim 1 , lubricants claim 1 , permeation enhancers claim 1 , suspension-forming agents claim 1 , mucoadhesive agents claim 1 , ...

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Номер записи: 72
07-01-2016 дата публикации

COMPOUNDS FROM INVASIVE SALVINIAS AND METHODS OF USING THE SAME

Номер: US20160002279A1
Автор: DENG Guangrui, LI Shiyou, SU Zushang, Wang Ping, Yuan Wei
Принадлежит:

In some embodiments, the compositions and methods relate to compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of using the same. 4. (canceled)611.-. (canceled)12. The compound of claim 1 , wherein the compound is isolated from a plant in the Salviniaceae family.13Salvinia. The compound of claim 12 , wherein the compound is isolated from a plant in the genus.14S. auriculata, S. biloba, S. cucullata, S. cyathiformis, S. hastate, S. herzogii, S. minima, S. molesta, S. natans, S. nymphellula, S. oblongifolia, S. radula, S. rotundifoliaS. sprucei.. The compound of claim 12 , wherein the compound is isolated from claim 12 , or15Azolla. The compound of claim 12 , wherein the compound is isolated from a plant in the genus.16. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) the compound according to or a pharmaceutically acceptable salt thereof; and'}(b) an excipient.17. A method of treating cancer in a patient in need thereof claim 1 , comprising administering to the patient a pharmaceutical composition comprising a compound according to in an amount sufficient to treat the cancer.18. The method of claim 17 , wherein the cancer is melanoma claim 17 , cervical cancer claim 17 , breast cancer claim 17 , ovarian cancer claim 17 , prostate cancer claim 17 , testicular cancer claim 17 , urothelial carcinoma claim 17 , bladder cancer claim 17 , non-small cell lung cancer claim 17 , small cell lung cancer claim 17 , sarcoma claim 17 , colorectal adenocarcinoma claim 17 , gastrointestinal stromal tumors claim 17 , gastroesophageal carcinoma claim 17 , colorectal cancer claim 17 , pancreatic cancer claim 17 , kidney cancer claim 17 , hepatocellular cancer claim 17 , malignant mesothelioma claim 17 , leukemia claim 17 , lymphoma claim 17 , myelodysplastic syndrome claim 17 , multiple myeloma claim 17 , transitional cell carcinoma claim 17 , neuroblastoma claim 17 , ...

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Номер записи: 73
05-01-2017 дата публикации

Cyclic nucleotide analogs

Номер: US20170002037A1
Автор: David Bernard Smith, Jerome Deval, Leonid Beigelman, Vivek Kumar Rajwanshi
Принадлежит: Alios Biopharma Inc

Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.

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Номер записи: 74
02-01-2020 дата публикации

FLUOROGENIC GLYCOSIDASE SUBSTRATE AND ASSOCIATED DETECTION METHOD

Номер: US20200002367A1
Автор: GONDRAND Corentin, HASSERODT Jens, PROST Maxime, TRIQUENEAUX Gérard, YVERT Gaël
Принадлежит:

The invention relates to novel glycosidase substrates of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R′9, V, X, Y and Z are as defined in claim , and a method for detecting the presence of a catalytically active glycosidase by means of one of said substrates. 2. Compounds (I) according to claim 1 , wherein R3 is a hydrogen atom or an (C1-C4) alkyl claim 1 , and R2 and R4 are bonded to each other and form a —(CH2)m- chain with m=3 claim 1 , 4 or 5.3. Compounds (I) according to claim 1 , wherein R3 is a hydrogen atom or an (C1-C4) alkyl claim 1 , and R2 and R4 are bonded to each other and form a —CH2CH2-NR11-CH2- chain in the direction of R2 toward R4 claim 1 , R11 representing a hydrogen atom or -(L)n-GP with n which is equal to 0 or 1 claim 1 , L a linking arm and GP a hydro solubilizing group.4. Compounds (I) according to claim 1 , wherein R2 claim 1 , R3 and R4 claim 1 , identical or different claim 1 , represent an (C1-C4) alkyl group claim 1 , for example claim 1 , methyl or ethyl.5. Compounds (I) according to claim 1 , wherein R1 is an aromatic group comprising one or more aromatic rings claim 1 , substituted or not substituted claim 1 , which rings can comprise one or more hetero-atoms chosen from among the nitrogen claim 1 , oxygen or sulfur atoms and/or one or more carbon atoms in the form of a C═O carbonyl.8. Compounds (I) according to claim 1 , wherein R0 is cleavable from the rest of compound (I) by the catalytic action of a glycosidase.9. Compounds (I) according to claim 1 , wherein R0 is a group that is cleavable under the action of a glycosidase claim 1 , chosen from among N-acetyl-β-galactosaminidase; N-acetyl-β-glucosaminidase; α-amylase; α-arabinofuranosidase claim 1 , α-arabinosidase; β-cellobiosidase; β-chitobiosidase; α-galactosidase; β-galactosidase; α-glucosidase; β-glucosidase; β-glucuronidase; α-maltosidase; α-mannosidase; β-mannosidase; β-xylosidase; β-D-fucosidase; α-L-fucosidase claim 1 , β-L-fucosidase; L-iduronidase or ...

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Номер записи: 75
02-01-2020 дата публикации

Amphotericin b derivatives with improved therapeutic index

Номер: US20200002368A1
Автор: Brice E. Uno, David M. Knapp, Ian DAILEY, Justin Struble, Kaitlyn C. Gray, Martin D. Burke, Nagarjuna Palyam, Pulin Wang, Stephen Davis
Принадлежит: University of Illinois

Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

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Номер записи: 76
20-01-2022 дата публикации

Fluorinated 4'-Alkylumbelliferyl a-D-Glucopyranosides, Biological Sterilization Indicators Including The Same And Methods Of Using The Same

Номер: US20220017939A1
Автор: Bonilla Tonya D., Griesgraber George W., Roscoe Stephen B.
Принадлежит:

A self-contained biological sterilization indicator comprises: a housing; bacterial spores comprising, and/or capable of producing, an enzyme capable of catalyzing cleavage of an enzyme substrate; and a frangible container containing a composition, wherein the composition comprises the enzyme substrate, wherein if the frangible container is broken the composition will contact the bacterial spores to form a mixture having an initial pH in the range from 6.0 to 9.0. The enzyme substrate comprises a fluorinated 4′-alkylumbelliferyl α-D-glucopyranoside represented by the structural formula (I) wherein one of Rand Ris F and the other is H, and Ris an alkyl group having from 1 to 12 carbon atoms. A biological sterilization indicator comprising a kit containing isolated components comprising (i) bacterial spores comprising, and/or capable of producing, an enzyme capable of catalyzing cleavage of the enzyme substrate and a method of assessing efficacy of a sterilization process are also disclosed. 2. The fluorinated 4′-alkylumbelliferyl α-D-glucopyranoside of claim 1 , wherein Ris an alkyl group having 1 to 4 carbon atoms.3. (canceled)4. (canceled)6. The self-contained biological sterilization indicator of claim 5 , wherein the self-contained biological sterilization indicator is disposed inside a process-challenge device.7. The self-contained biological sterilization indicator of claim 5 , wherein Ris an alkyl group having 1 to 4 carbon atoms.8. The self-contained biological sterilization indicator of claim 5 , wherein the self-contained biological sterilization indicator is capable of determining efficacy of two or more cycles chosen from the powerset of 121 gravity claim 5 , 121 pre-vac claim 5 , 121 SFPP claim 5 , 132 gravity claim 5 , 132 pre-vac claim 5 , 132 SFPP claim 5 , 134 pre-vac claim 5 , 134 SFPP claim 5 , 135 gravity claim 5 , 135 pre-vac claim 5 , and 135 SFPP.11. The self-contained biological sterilization indicator of claim 5 , wherein the mixture has an ...

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Номер записи: 77
12-01-2017 дата публикации

Process for the attachment of a galnac moiety comprising a (hetero)aryl group to a glcnac moiety, and product obtained thereby

Номер: US20170009266A1
Автор: Floris Louis Van Delft, Maria Antonia WIJDEVEN, Remon VAN GEEL, Ryan HEESBEEN
Принадлежит: Synaffix BV

The present invention relates to a process for attaching an N-acetylgalactosamine-(hetero)arylmoiety to an N-acetylglucosaminemoiety, the process comprising the step of contacting the N-acetylgalactosamine-(hetero)arylmoiety with the N-acetylglucosaminemoiety in the presence of a mutant galactosyltransferase, wherein the N-acetylglucosaminemoiety is according to Formula (1) the N-acetylgalactosamine-(hetero)arylmoiety is according to Formula (2): In a particularly preferred embodiment of the process according to the invention, the N-acetylgalactosamine-(hetero)arylmoiety comprises a 1,3-dipole functional group, and the N-acetylglucosaminemoiety is a terminal GlcNAc moiety of a glycoprotein glycan. The invention further relates to a product obtainable by the process according to the invention, in particular to glycoproteins. Also, the invention relates to several compounds comprising an N-acetylgalactosamine-(hetero)arylmoiety.

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Номер записи: 78
14-01-2016 дата публикации

PHOSPHONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION

Номер: US20160009750A1
Автор: DE CLERCQ Erik, HERDEWIJN Piet, PANNECOUQUE Christophe, WU Tongfei
Принадлежит:

The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. These compounds can be described by general formula (II) 111.-. (canceled)13. The process of claim 12 , wherein the silylating agent is a chlorine-containing silylating agent.14. The process of claim 12 , wherein the silylating agent is tributyldimethylsilyl chloride.15. The process of claim 12 , wherein the reaction is performed in the presence of an organic solvent.16. The process of claim 15 , wherein the organic solvent is acetonitrile.17. The process of claim 12 , wherein the reaction is performed in the presence of a reactant.18. The process of claim 17 , wherein the reactant is imidazole.19. The process of claim 12 , wherein the reaction is performed at a temperature ranging from 0° C. to room temperature.20. The process of claim 12 , wherein the compound is selected from the group consisting of:2-O-tributyldimethylsilyl-L-threonolactone,2-O-tributyldimethylsilyl-3-O-benzoyl-L-threonolactone,2-O-tributyldimethylsilyl-3-O-benzoyl-L-threose,1α,2-di-O-tributyldimethylsilyl-L-threose,1β,2-di-O-tributyldimethylsilyl-L-threose,1α,2-di-O-tributyldimethylsilyl-3-O-(diisopropylphosphonomethyl)-L-threose, and1β,2-di-O-tributyldimethylsilyl-3-O-(diisopropylphosphonomethyl)-L-threose.21. The process of claim 12 , wherein the process further comprises the step of protecting the free hydroxyl group on position 3 of the 2 claim 12 ,3-dihydroxy-dihydro-furan-1-one by acylation.22. The process of claim 21 , wherein said acylation is benzoylation.23. The process of claim 22 , wherein the benzoylation is performed by means of benzoyl chloride in an organic solvent. The present invention relates to a series of novel phosphonate nucleosides and thiophosphonate nucleosides, more specifically phosphonate nucleosides and ...

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Номер записи: 79
11-01-2018 дата публикации

CRYSTAL STRUCTURE OF THE LARGE RIBOSOMAL SUBUNIT FROM S. AUREUS

Номер: US20180009853A1
Автор: BASHAN Anat, EYAL Zohar, MATZOV Donna, ROZENBERG Haim, YONATH Ada, ZIMMERMAN Ella
Принадлежит:

A composition-of-matter comprising a crystallized form of a large ribosomal (50S) subunit of a pathogenic bacterium, and the atomic coordinates of the three-dimensional structure thereof are provided herein, as well as methods for crystallizing the same, and using the atomic coordinates of the same to design de novo ligands with high specificity thereto. 1. A composition-of-matter comprising a crystallized large ribosomal subunit of a pathogenic bacterium , wherein the pathogenic bacterium is:a pathogenic Gram positive bacterium; and/or{'i': 'Staphylococcus aureus', 'a pathogenic bacterium exhibiting a degree of 23S rRNA sequence identity of at least 80% compared to rRNA of ; and/or'}{'i': 'Escherichia coli', 'a pathogenic bacterium exhibiting a degree of 23S rRNA sequence identity of less than 99.9% compared to rRNA of , and'}the crystallized large ribosomal subunit effectively diffracts X-rays for calculating an electron density map and determination of atomic coordinates to a resolution of at least 4 Å.24-. (canceled)5Staphylococcus aureus. The composition of claim 1 , wherein said Gram positive pathogenic bacterium is a that is capable of developing a resistance to an antibacterial agent.6Staphylococcus aureusStaphylococcus aureusStaphylococcus aureusStaphylococcus aureusStaphylococcus aureus. The composition of claim 5 , wherein said is selected from the group consisting of a methicillin-resistant (MRSA) claim 5 , an oxacillin-resistant (ORSA) claim 5 , a vancomycin-resistant (VRSA) and a vancomycin intermediate (VISA).7. The composition of claim 5 , characterized by the atomic coordinates deposited at the Protein Data Bank under accession number PDB ID: 4WCE.8. The composition of claim 1 , wherein a ligand is bound to said large ribosomal subunit to form a crystallized complex of the subunit and said ligand.9. The composition of claim 8 , wherein said ligand is selected from the group consisting of linezolid claim 8 , BC-3205 claim 8 , telithromycin claim 8 , ...

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Номер записи: 80
14-01-2021 дата публикации

AMINOCOUMARIN COMPOUNDS AND METHODS OF THEIR USE

Номер: US20210009621A1
Автор: Kahne Daniel, Mandler Michael D.
Принадлежит:

Disclosed are aminocoumarin compounds, pharmaceutical compositions containing aminocoumarin compounds, and methods of their use, e.g., in the treatment of a Gram-negative bacterial infection. 2. The compound of claim 1 , wherein Ris heteroaryl substituted by 1 or more substituents claim 1 , wherein at least one substituent is —OR.3. The compound of or claim 1 , wherein Ris pyridyl substituted by 1 or more substituents claim 1 , wherein at least one substituent is —OR.4. The compound of claim 1 , wherein Ris phenyl substituted by 1 or more substituents claim 1 , wherein at least one substituent is —OR.7. The compound of any one of - claim 1 , wherein Ris optionally substituted aryl.8. The compound of claim 7 , wherein Ris aryl substituted by one or more substituents each independently selected from the group consisting of halo claim 7 , nitro claim 7 , cyano claim 7 , hydroxyl claim 7 , optionally substituted alkyl claim 7 , hydroxyalkyl claim 7 , haloalkyl claim 7 , aminoalkyl claim 7 , optionally substituted alkoxy claim 7 , haloalkoxy claim 7 , optionally substituted alkenyl claim 7 , optionally substituted alkynyl claim 7 , optionally substituted aryl claim 7 , optionally substituted heteroaryl claim 7 , optionally substituted cycloalkyl claim 7 , and optionally substituted heterocycloalkyl.9. The compound of any one of - claim 7 , wherein Ris optionally substituted heteroaryl.10. The compound of any one of - claim 7 , wherein L is —CO—.11. The compound of any one of - claim 7 , wherein X is O.13. The compound of any one of - claim 7 , wherein Ris hydroxyl.14. The compound of any one of - claim 7 , wherein Ris —O—CO—NH—R.15. The compound of claim 14 , wherein Ris H.16. The compound of any one of - claim 14 , wherein Ris optionally substituted Calkyl.17. The compound of claim 16 , wherein Ris methyl.18. The compound of any one of to claim 16 , wherein Ris hydroxyl.22. The compound of claim 21 , wherein L is —CO—.23. The compound of or claim 21 , wherein X is O.25. ...

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Номер записи: 81
09-01-2020 дата публикации

PHENAZINE DERIVATIVES AS ANTIMICROBIAL AGENTS

Номер: US20200010432A1
Автор: Abouelhassan Yasmeen, Burch Gena, Garrison Aron, Huigens, III Robert William, Yang Hongfen
Принадлежит: University of Florida Research Foundation, Incorporated

The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II)-(XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is CR.3. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein both X and Y are independently halogen.4. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is chloro.5. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is bromo.6. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is iodo.7. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is chloro.8. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is bromo.9. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is iodo.10. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each of X and Y is independently bromo or iodo ...

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Номер записи: 82
09-01-2020 дата публикации

Novel immune stimulating macrolides

Номер: US20200010498A1
Автор: Emma LINDH, Matt GREGORY, Ola Winqvist, Robert WALLIN, Steven Moss
Принадлежит: ISR Immune System Regulation Holding AB

The present invention provides immune stimulating macrolides of formula (I), wherein the substituents are as defined in the claims. The macrolides have utility in treating viral diseases and cancer.

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Номер записи: 83
09-01-2020 дата публикации

NOVEL IMMUNE STIMULATING COMPOUND

Номер: US20200010499A1
Автор: Gregory Matt, Lindh Emma, Moss Steven, Wallin Robert, Winqvist Ola
Принадлежит:

The present invention provides immune stimulating macrolide of formula (I). The macrolide has utility in treating intracellular bacterial, fungal, and protozoal infections. 2. A pharmaceutical composition comprising the compound according to .3. The pharmaceutical composition according to claim 2 , wherein the pharmaceutical composition comprises one or more pharmaceutically acceptable excipients.4. A method for treating an intracellular infection claim 1 , the method comprising administering to a human or animal subject in need thereof a therapeutically effective amount of the compound according to .5. The method according to claim 4 , wherein the intracellular infection is selected from intracellular bacterial claim 4 , intracellular protozoal claim 4 , and intracellular fungal infections.6Mycobacterium tuberculosisMycobacterium aviumM. intracellulareMycobacterium aviumM kansasii, M. marinum, M. fortuitum, M. gordinae, Mycoplasma pneumoniae, M. genitalium, M. hominis, Ureaplasma urealyticum, U. parvum, Chlamydophila pneumoniae,Salmonella typhimurium.. The method according to claim 5 , wherein the intracellular infection is selected from intracellular bacterial infections caused by claim 5 , Mycobacteria causing atypical disease claim 5 , and (also known as -intracellulare complex claim 5 , or MAC) claim 5 , and7Toxoplasma gondii, Plasmodium falciparum, P. vivax, Trypanosoma cruzi, CryptosporidiumLeishmania.. The method according to claim 5 , wherein the intracellular infection is selected from intracellular protozoal infections caused by claim 5 , and8Histoplasma capsulatum, Cryptococcus neoformans,Encephalitozoon cuniculi.. The method according to claim 5 , wherein the intracellular infection is selected from intracellular fungal infections caused by and9. A method for treating or preventing a disease caused by an intracellular infection comprising administering to a human or animal subject in need thereof a therapeutically effective amount of the compound ...

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Номер записи: 84
21-01-2016 дата публикации

FLAVOR COMPOSITION CONTAINING HMG GLUCOSIDES

Номер: US20160015063A1
Автор: Didzbalis John, Munafo John P.
Принадлежит: MARS, INCORPORATED

A flavor composition containing at least one HMG glucoside compound that can be used to enhance the taste of edible compositions including sweet goods, such as confectionery goods, and savory goods, such as pet foods.

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Номер записи: 85
21-01-2016 дата публикации

Method of isolating blue anthocyanin fractions

Номер: US20160017150A1
Автор: J. Christopher Johnson, M. Monica Giusti, Neda AHMADIANI, Rebecca J. Robbins, Thomas M. Collins
Принадлежит: Mars Inc, Ohio State University

The present invention is directed to a method of isolating fractions of anthocyanin molecules from anthocyanin-containing vegetable and fruit juices and extracts, or combinations thereof, at a select pH based on differences in polarity of the anthocyanin molecules in the anthocyanin-containing vegetable and fruit juices and extracts.

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Номер записи: 86
18-01-2018 дата публикации

PROCESS FOR THE PREPARATION OF DIOSMIN

Номер: US20180016292A1
Автор: LÓPEZ CREMADES Francisco Javier
Принадлежит: INTERQUIM, S.A.

The present invention relates to a process for the preparation of diosmin from hesperidin. The process involves the oxidation of acylated hesperidin with iodine or bromine in a C-Ccarboxylic acid medium and subsequent treatment with an inorganic base to partially neutralize the acidic media. The process allows obtaining diosmin with low iodine or bromine content, avoiding the use of organic solvents. 1. Process for the preparation of diosmin from hesperidin comprising the following steps:a) acylating hesperidin with the anhydride of a C2-C4 carboxylic acid;b) treating the mixture obtained in step a) with a halogen selected from iodine and bromine, in aqueous medium;c) treating the mixture obtained in step b) with an inorganic base to reach a pH value in the range 3.5-6.5;d) deacylating the acylated diosmin obtained in step c) by treatment with an inorganic base;wherein no organic solvent is added throughout the process.2. Process according to claim 1 , wherein in step a) a catalyst is used selected from sodium acetate and potassium acetate.3. Process according to claim 1 , wherein the anhydride of the C2-C4 carboxylic acid of step a) is acetic anhydride.4. Process according to claim 1 , wherein step b) is carried out bya) using the halogen in a stoichiometric amount, orb) using a halide in a stoichiometric amount and an oxidant in a stoichiometric amount, orc) using the halogen in a catalytic amount and an oxidant in a stoichiometric amount.5. Process according to claim 1 , wherein step b) is carried out by using a halide in a catalytic amount and an oxidant in a stoichiometric amount.6. Process according to claim 4 , wherein the oxidant is selected from the group of hydrogen peroxide claim 4 , sodium percarbonate claim 4 , potassium percarbonate claim 4 , sodium perborate claim 4 , potassium perborate claim 4 , sodium permanganate claim 4 , potassium permanganate claim 4 , sodium dichromate claim 4 , potassium dichromate claim 4 , and hydrates thereof.7. Process ...

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Номер записи: 87
18-01-2018 дата публикации

METHOD FOR IMPROVING HETEROLOGOUS SYNTHESIS OF ESCHERICHIA COLI INTO POLYKETIDES AND USE OF SAME

Номер: US20180016585A1
Автор: Liu Qiaoxia, Song Shujie, WANG JIANFENG, Wang Yong, Xiong Zhiqiang
Принадлежит: Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences

The present invention relates to a method for improving the heterologous synthesis of a polyketide by and use thereof. The yield of the polyketide heterologously synthesized by is significantly increased by attenuating the expression of seventy-two genes, such as sucC and talB, in a host strain, wherein the highest yield increase rate can reach 60% or more. Currently, erythromycin is the most clear model compound in the study on the biosynthesis of polyketids. The production strain of the present invention enables massive accumulation of 6-deoxyerythronolide (6-dEB), an erythromycin precursor, in the fermentation process, laying the foundation for the industrial production of the heterologous synthesis of erythromycin by 1. A method for promoting a host strain for synthesizing the polyketide 6-deoxyerythronolide to synthesize the polyketide 6-deoxyerythronolide biologically , wherein the method comprises:(1) attenuating the expression of a target gene in the host strain for synthesizing the polyketide 6-deoxyerythronolide;wherein, the target gene is selected from:(a) a gene for nucleotide synthesis and other metabolism modules: purT, lsrC, hemN, zwf, pgl, gnd, rpe, talA, talB, tktA, tktB, ulaE or yieK;(b) a gene for pentose phosphate and glyoxylate pathway modules: yaeR, rpiA, rpiB, purH, pyrB, pyrI, cysQ, pyrC, gmk, guaA, guaB, ndk, pyrF, pyrE, pyrH or hpt;(c) a gene for TCA cycle and oxidative phosphorylation modules: frdD, frdA, sdhA, sdhB, sdhC, sdhD, sucC, sucD, cyoA or cyoB;(d) a gene for carbohydrate metabolism module: aceF, pgi, lpdA, ppk, ptsH, ptsI, glcF, glcE, fsaA or agaW;(e) a gene for 6-dEB precursor metabolism module: yjiM, scpA, scpB, tdcD, tdcE, pflB, pflD, PaaF, ackA, pta or ybiW;(f) a gene for fatty acid metabolism module: fadJ, fadB, dhaK1, dhaK2 or dhaH;(g) a gene for amino acid and protein synthetic metabolism modules: leuC, leuD, serC, serB, serA, gdhA or tnaA; or(h) the combination of frdD+sucC, the combination of lsrC+frdD, the combination ...

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Номер записи: 88
18-01-2018 дата публикации

ELECTROCHEMICAL DETECTION OF MICROORGANISMS

Номер: US20180016618A1
Автор: Han Jing Ying Evelina, Hinks Jamie, Loo Say Chye Joachim, Wuertz Stefan
Принадлежит:

The present invention provides a method for determining the presence of a microorganism in a sample using an electrochemically active reporter, wherein the method comprises (a) contacting the sample with an electrochemically active reporter, wherein the electrochemically active reporter is a conjugate comprising a sugar moiety and a redox active reporter moiety that are covalently linked such that the covalent bond can be enzymatically cleaved in the presence of the microorganism by an enzyme expressed by the microorganism, wherein the redox active reporter moiety is selected from the group consisting of resorufin and compounds of formula (I) as defined herein, under conditions that allow enzymatic cleavage of the covalent bond between the sugar moiety and the redox active reporter moiety and reduction of the redox active report moiety in the presence of the microorganism; (b) electrochemically determining the released redox active reporter moiety; and (c) determining the presence of the microorganism and, optionally, number of the microorganisms in the sample based on the determined released redox active reporter moiety. Also encompassed are the electrochemically active reporters used in the described methods and their use for determination of the presence of microorganisms in a sample. 2. The method of claim 1 , wherein the method is carried out by a 3-electrode electrochemical system or a 2-electrode self-powering bioelectrochemical system comprising a working electrode and an electrolyte.3. The method of claim 2 , wherein step (a) comprises adding the sample and an effective amount of the electrochemically active reporter to the electrolyte.4. The method of claim 3 , wherein step (b) comprises measuring the electrical current or voltage resulting from the released redox active reporter moiety by chronoamperometry claim 3 , potentiometry or voltammetry or other standard electrochemical techniques using the electrochemical system or by determining the potential ...

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Номер записи: 89
16-01-2020 дата публикации

Seco macrolide compounds

Номер: US20200017522A1
Автор: Andrea Fajdetic, Antun Hutinec, Dijana Pesic, Dinko ZIHER, Goran Kragol, Gordon Saxty, Ivana Ozimec Landek, Ivaylo Jivkov Elenkov, Kristina BUTKOVIC, Maja Matanovic Skugor, Marko DUKSI, Milan Mesic, Mirjana BUKVIC, Renata Rupcic, Sanja Kostrun, Visnja Poljak, Zorica Marusic Istuk
Принадлежит: Fidelta doo

The present invention relates to seco (opened ring) macrolide compounds, to the process for preparation thereof, to the use of said seco macrolide compounds as intermediates for preparation of macrolide based macrocycles, to macrolide based macrocycles obtained from said seco macrolide compounds, to the process for preparation of macrolide based macrocycles, to the pharmaceutical compositions comprising macrolide based macrocycles, and to the use of macrolide based macrocycles as therapeutic agents.

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Номер записи: 90
28-01-2016 дата публикации

PROCESS FOR PRODUCING A PARTICULATE COMPOSITION COMPRISING AN HYDROUS CRYSTALLINE 2-O-ALPHA-D-GLUCOSYL-L-ASCORBIC ACID

Номер: US20160024131A1
Автор: Fukuda Shigeharu, Izawa Seisuke, Miyake Toshio, NISHIMOTO Tomoyuki, Shibuya Takashi
Принадлежит:

The invention provides a process for enabling the production of a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside that does not significantly cake even when the production yield of ascorbic acid 2-glucoside does not reach 35% by weight. The process for producing a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside, which comprises allowing a CGTase to act on a solution containing either liquefied starch or dextrin and L-ascorbic acid and then allowing a glucoamylase to act on the resulting solution to obtain a solution with an ascorbic acid 2-glucoside production yield of at least 27%, purifying the obtained solution to increase the ascorbic acid 2-glucoside content to a level of over 86% by weight, precipitating anhydrous crystalline ascorbic acid 2-glucoside by a controlled cooling method or pseudo-controlled cooling method, collecting the precipitated anhydrous crystalline ascorbic acid 2-glucoside, and ageing and drying the collected anhydrous crystalline ascorbic acid 2-glucoside. 1which comprises 2-O-α-D-glucosyl-L-ascorbic acid in an amount of over 98.0% by weight but 99.8% by weight or lower, on a dry solid basis;which has a degree of crystallinity of 90% or higher for anhydrous crystalline 2-O-α-D-glucosyl-L-ascorbic acid, when calculated based on a profile of powder X-ray diffraction analysis of said composition;which contains particles with a particle size of less than 150 μm in an amount of 70% by weight or higher to the whole particulate composition, and those with a particle size of at least 53 μm but less than 150 μm in an amount of 40 to 60% by weight to the whole composition; andwhich has a reducing power of the whole composition being less than one percent by weight.. A particulate composition comprising anhydrous crystalline 2-O-α-D-glucosyl-L-ascorbic acid, The present invention relates to a process for producing a particulate composition containing anhydrous crystalline 2-O-α-D- ...

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Номер записи: 91
10-02-2022 дата публикации

Methods of treating cancer using platanoside and isomers thereof

Номер: US20220040213A1
Автор: Yehoshua KORCHIA MAOR
Принадлежит: SHARE GAL RESEARCH AND DEVELOPMENT LTD

This invention relates to methods of treating cancer with platanoside and/or isomers thereof or pharmaceutically acceptable salts thereof, particularly treatment of a pancreatic, liver or brain cancer. This invention further relates to methods of treating cancer with platanoside and/or isomers thereof, produced from Ephedra foeminea.

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Номер записи: 92
17-04-2014 дата публикации

ISOFLAVONES FOR TREATING MUCOPOLYSACCHARIDOSES

Номер: US20140107051A1
Автор: BARANSKA Sylwia, CZARTORYSKA Barbara, GRYNKIEWICZ Grzegorz, JAKOBKIEWICZ-BANECKA Joanna, PIOTROWSKA Ewa, SZECHNER Barbara, SZEJA Wieslaw, TYLKI-SZYMANSKA Anna, WEGRZYN Alicja, WEGRZYN Grzegorz
Принадлежит: INSTYTUT FARMACEUTYCZNY

A pharmaceutical composition including a pharmaceutically acceptable excipient; and a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof, the natural isoflavone, the derivative thereof, or the pharmaceutically acceptable salt thereof being in a therapeutically effective amount for the treatment of mucopolysaccharidosis. A method of treatment of mucopolysaccharidosis, the method including administering to a patient in the need of such treatment—a therapeutically effective amount of a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof. 2. The composition of claim 1 , except that the compound of formula (I) is not genistein.4. The method of claim 3 , except that the compound of formula (I) is not genistein.5. The method of claim 3 , wherein said disease is mucopolysaccharidosis type 1.6. The method of claim 3 , wherein said compound is administered at a ratio between 1 and 50 mg of said compound per kg of a patient's body mass.8. The method of claim 7 , wherein said compound inhibits the synthesis of glycosaminoglycans claim 7 , and removes deposits of glycosaminoglycans.10. The composition of claim 9 , wherein said C-acyl is acetyl.11. The composition of claim 9 , wherein said C-alkylcarboxyl is AcO.12. A method for the treatment of mucopolysaccharidosis claim 9 , the method comprising administering to a patient in the need thereof a therapeutically effective amount of the compound of claim 9 , or a pharmaceutically acceptable salt thereof. This application is a continuation-in-part of U.S. application Ser. No. 13/433,492 filed on Mar. 29, 2012, now pending, which is a continuation of U.S. application Ser. No. 12/067,289 with a 371(c) date of Nov. 5, 2008, now issued as U.S. Pat. No. 8,178,609 on May 15, 2012, which is a National Stage Application under 35 U.S.C. §371 of Int'l Pat. Appl. No. PCT/PL2006/000064, filed on Sep. 21, 2006. Pursuant to 35 U.S.C. §119 and ...

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Номер записи: 93
17-04-2014 дата публикации

CHEMOSELECTIVE ENRICHMENT FOR COMPOUND ISOLATION

Номер: US20140107328A1
Автор: CARLSON Erin E., TRADER Darci
Принадлежит:

Chemoselective isolation of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds is accomplished via formation of polymeric siloxyl ethers. Chemoselective release of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds from polymeric siloxyl reagents is described. 1. A process for preparing a second mixture selectively enriched in aromatic-hydroxyl group containing compounds from a first mixture comprising hydroxyl group containing compounds , where the hydroxyl group containing compounds include one or more functional groups selected from aromatic-hydroxyl groups and aliphatic-hydroxyl groups , the method comprising the steps(a) contacting the first mixture with a polymeric reagent{'sub': 2', 'n, 'sup': 1', '2, 'comprising a polymer having one or more functional groups of formula (CH)—O—Si(R)(R)X covalently attached to the polymer, wherein'}the functional group is capable of reacting with hydroxyl group containing compounds when the mixture containing the compounds contacts the reagent;n is 1 to 4;{'sup': 1', '2, 'sub': 1', '8', '3', '8, 'Rand Rare independently selected in each instance from the group consisting of C-Calkyl and C-Ccycloalkyl; and'}{'sub': 2', '3, 'X is selected from the group consisting of Cl, Br, and OS(O)CF.;'}wherein one or more of the functional groups forms a covalent bond with the hydroxyl group of one or more of the hydroxyl group containing compounds;{'sub': 5', '10', '1', '5', '1', '5', '2', '5', '1', '4', '1', '4, '(b) washing the polymer resulting from step (a) with a solvent selected from the group consisting of optionally branched C-Calkanes, optionally-branched C-Calcohols, benzene, toluene, xylenes, C-Calkyl C-Calkanoates, where each of the alkyl or the alkanoate is optionally branched, C-Calkylnitriles, DMF, THF, dioxane, DMSO, C-Chaloalkanes, and combinations thereof; and'}{'sup': 3', '3, 'sub': 2', '1', '8, '(c) contacting the polymer resulting from step (b) with a ...

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Номер записи: 94
10-02-2022 дата публикации

QUINONE METHIDE ANALOG SIGNAL AMPLIFICATION

Номер: US20220041633A1
Автор: Ashworth-Sharpe Julia, Bieniarz Christopher, Kelly Brian D., Polaske Nathan
Принадлежит:

Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step. 1. A method of detecting a first target in a biological sample , comprising:contacting the biological sample with a first detection probe specific to the first target;labeling the first target with a first enzyme through the first detection probe;contacting the biological sample with a first quinone methide analog precursor comprising a first enzyme recognition group and a first detectable label, anddetecting the first target by detecting the first detectable label.2. The method of claim 1 , wherein the first enzyme cleaves the first enzyme recognition group claim 1 , thereby converting the first quinone methide analog precursor into a first reactive quinone methide analog which covalently binds to the biological sample proximally to or directly on the first target.3. The method of claim 1 , wherein the first enzyme is a phosphatase claim 1 , phosphodiesterase claim 1 , esterase claim 1 , lipase claim 1 , amidase claim 1 , protease claim 1 , nitroreductase claim 1 , urease claim 1 , sulfatase claim 1 , cytochrome P450 claim 1 , alpha-glucosidase claim 1 , beta-glucosidase claim 1 , beta-lactamase claim 1 , alpha-glucoronidase claim 1 , beta-glucoronidase claim 1 , alpha-galactosidase claim 1 , beta- ...

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Номер записи: 95
24-01-2019 дата публикации

CONVERGENT PROCESSES FOR PREPARING MACROLIDE ANTIBACTERIAL AGENTS

Номер: US20190023731A1
Автор: PEREIRA David Eugene
Принадлежит:

The invention described herein relates to processes for preparing ketolide antibacterial agents. In particular, the invention relates to intermediates and processes for preparing ketolides that include a 1,2,3-triazole substituted side chain. 125-. (canceled)28. The compound of wherein C is aryl claim 27 , heteroaryl claim 27 , arylalkyl claim 27 , or heteroarylalkyl claim 27 , each of which is optionally substituted.29. The compound of wherein A is CH.30. The compound of wherein B is (CH) claim 27 , and n is an integer from 2-6.33. The compound of wherein Ris hydrogen.35. The intermediate of wherein C is aryl claim 34 , heteroaryl claim 34 , arylalkyl claim 34 , or heteroarylalkyl claim 34 , each of which is optionally substituted.36. The intermediate of wherein A is CH.37. The intermediate of wherein B is (CH) claim 34 , and n is an integer from 2-6.38. The intermediate of wherein B is (CH) claim 34 , and n is 2 claim 34 , 3 claim 34 , or4.39. The intermediate of wherein Ris acyl. The present application claims, under 35 U.S.C. § 119(e), the benefit of and priority to U.S. Provisional Application No. 61/786,914 filed Mar. 15, 2013, which is hereby incorporated herein by reference.The invention described herein relates to processes for preparing ketolide antibacterial agents. In particular, the invention relates to intermediates and processes for preparing ketolides that include a 1,2,3-triazole substituted side chain.The use of macrolides for various infectious diseases is well known. Erythromycin was the first compound of this class to be introduced into clinical practice. Since then, additional macrolides, including ketolides have garnered much attention for their ability to treat a wide range of disease states. In particular, macrolides are an important component of therapies for treating bacterial, protozoal, and viral infections. In addition, macrolides are often used in patients allergic to penicillins.Illustrative of their wide ranging uses, macrolide ...

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Номер записи: 96
28-01-2021 дата публикации

Novel Form of Invermectin and a Process for Making it

Номер: US20210023111A1
Автор: Sergio SILVA
Принадлежит: Hovione Scientia Ltd

Amorphous ivermectin is provided, suitably in isolated solid form, and is suitably free of any additives or a support matrix, such as a solid dispersion. Also provided is a pharmaceutical formulation, for animal including human or veterinary use, comprising the amorphous ivermectin of the invention, and a pharmaceutically-acceptable carrier therefor. Also provided is a medical device incorporating amorphous ivermectin according to the invention, or a medical device incorporating a pharmaceutical formulation according to the invention described herein. A method of preparing amorphous ivermectin comprises the steps of preparing a solution of ivermectin in at least one solvent; removing the solvent by feeding the solution to a spray dryer and collecting particles of ivermectin. Amorphous ivermectin as disclosed herein may be used as a medicament, in particular to treat conditions such as a medical condition caused by internal nematode infections including but not limited to onchocerciasis (river blindness), filariasis (elephantiasis), strongyloidiasis or demodicosis.

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Номер записи: 97
28-01-2021 дата публикации

Analogues of etoposide for the treatment of tumours

Номер: US20210023112A1
Автор: Nalan Utku
Принадлежит: Purdue Pharma LP

Compounds for treatment of a patient having a tumour that is metastatic and/or that reduces an organ function, wherein the compounds are of the general formula: wherein X is O, NH and S, wherein n is 0, 1 or 2, wherein R 1 and R 2 are H, methyl or ethyl, or together form a group CR 3 R 4 , and wherein R 3 and R 4 are H, methyl or ethyl.

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Номер записи: 98
04-02-2016 дата публикации

AZITHROMYCIN ANTIMICROBIAL DERIVATIVES WITH NON-ANTIBIOTIC PHARMACEUTICAL EFFECT

Номер: US20160031925A1
Автор: GARDARSSON Friõrik, GARDARSSON Magnús, GULDBERG Susanne
Принадлежит:

The invention provides molecules, which are based on a modification of azithromycin, removing the antibiotic effect, while retaining other beneficial effects, such as, but not limited to immunomodulatory effects. The compounds of the invention can be described by compounds of Formula (I) as further defined herein. 2. The compound of claim 1 , wherein{'sup': 1', '3', '5, 'sub': '3', 'Ris the group R, where Ris H, OH or CH, and'}{'sup': '2', 'sub': 3', '3, 'Ris OH, CH, or OCH.'}3. The compound of claim 1 , wherein{'sup': 1', '2', '4', '6, 'sub': 3', '3', '3, 'Ris OH, CH, OCH, and Ris the group R, with Rbeing H, OH or CH.'}4. The compound of claim 1 , selected from the group consisting of{'sup': 1', '3', '5', '2', '4', '6, 'sub': '3', 'i) compound of Formula (I) wherein Ris the group R, with Rbeing CH, and Ris the group R, with Rbeing OH;'}{'sup': 1', '3', '5', '2', '4', '6, 'sub': '3', 'ii) compound of Formula (I) wherein Ris the group R, with Rbeing OH and Ris the group R, with Rbeing CH;'}{'sup': 1', '3', '5', '2', '4', '6, 'sub': 3', '3, 'iii) compound of Formula (I) wherein Ris the group R, with Rbeing CHand Ris the group R, with Rbeing CH;'}{'sup': 1', '3', '5', '2', '4', '6, 'iv) compound of Formula (I) wherein Ris the group R, with Rbeing OH and Ris the group R, with Rbeing H;'}{'sup': 1', '3', '5', '2', '4', '6, 'v) compound of Formula (I) wherein Ris the group R, with Rbeing H and Ris the group R, with Rbeing OH;'}{'sup': 1', '3', '5', '2', '4', '6, 'vi) compound of Formula (I) wherein Ris the group R, with Rbeing H and Ris the group R, with Rbeing H;'}{'sup': 1', '3', '5', '2', '4', '6, 'sub': '3', 'vii) compound of Formula (I) wherein Ris the group R, with Rbeing CHand Ris the group R, with Rbeing H;'}{'sup': 1', '3', '5', '2', '4', '6, 'sub': '3', 'viii) compound of Formula (I) wherein Ris the group R, with Rbeing H and Ris the group R, with Rbeing CH;'}{'sup': 1', '2, 'ix) compound of Formula (I) wherein Ris OH and Ris OH;'}{'sup': 1', '2, 'sub': 3', '3, ...

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Номер записи: 99
04-02-2016 дата публикации

Triazole Compounds and Methods of Making and Using the Same

Номер: US20160031926A1
Автор: Bhattacharjee Ashoke, Kanyo Zoltan F., Sherer Edward C.
Принадлежит:

The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. 4. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide or prodrug thereof claim 1 , wherein Ris Calkyl claim 1 , optionally substituted with from 1 to 7 fluorines.5. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide or prodrug thereof claim 1 , wherein Ris selected from —CH claim 1 , —CHF claim 1 , —CHF claim 1 , and —CF.7. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 1 or 2.8. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 1.9. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein Ris F.10. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein n is 0.11. A compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , N-oxide claim 1 , or prodrug thereof claim 1 , wherein A is selected from: (a) a Calkyl group claim 1 , (b) a Calkenyl group claim 1 , (c) a Calkynyl group claim 1 , (d) a Csaturated claim 1 , unsaturated claim 1 , or aromatic carbocycle claim 1 , (e) a 3-12 membered saturated claim 1 , unsaturated claim 1 , or aromatic heterocycle containing one or more nitrogen claim 1 , oxygen or sulfur atoms claim 1 , (f) —CF claim 1 , (g) —NR(CRR)R claim 1 , (h) —OR claim 1 , (i) —S(CRR)R claim 1 , (j) —S(O)(CRR)R claim 1 , (k) —S(O)(CRR)R claim 1 , (l) —C(O)(CRR)R claim 1 , (m) —OC ...

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Номер записи: 100