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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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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 7609. Отображено 100.
21-02-2013 дата публикации

Composition comprising an amorphous non-crystalline glass form of roxithromycin

Номер: US20130045936A1
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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04-04-2013 дата публикации

MANUFACTURING METHOD FOR POLYPHENOL COMPOSITION

Номер: US20130085270A1
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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11-04-2013 дата публикации

METHODS OF ACCELERATING MUSCLE GROWTH, DECREASING FAT DEPOSITS AND IMPROVING FEED EFFICIENCY IN LIVESTOCK ANIMALS

Номер: US20130090295A1
Автор: Aberg A.K. Gunnar
Принадлежит: BRIDGE PHARMA, INC.

A method of promoting or improving the feed efficiency and the muscle to fat ratio in animals by administering to the animals a therapeutically effective amount of a pure or substantially pure RR-isomer of ractopamine is disclosed. Also disclosed are animal feed preparations and compositions and pharmaceutical preparations capable of increasing lean meat deposition in an animal or decreasing body fat, or promoting or improving the growth of an animal or improving the feed efficiency of an animal. Feed preparation, compositions and pharmaceutical preparations including therapeutically effective amounts of a pure or substantially pure RR-isomer of ractopamine are disclosed. 1. A method of minimizing the amount of tissue residue of total ractopamine in a ractopamine-treated animal , which comprises administering to the animal an effective amount of a pure or substantially pure RR-enantiomer of ractopamine or a pharmaceutically acceptable salt , solvate or polymorph thereof.2. The method of claim 1 , wherein the administration of the effective amount of the pure or substantially pure RR-enantiomer of ractopamine or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof claim 1 , reduces the risk for pharmacological side effects and toxic effects in the animal.3. The method of claim 1 , wherein the administration of the effective amount of the pure or substantially pure RR-enantiomer of ractopamine or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof to the animal claim 1 , reduces the risk for pharmacological side effects and toxic effects in a human that consumes meat from the animal.4. The method of claim 1 , wherein the administration of the effective amount of the pure or substantially pure RR-enantiomer of ractopamine or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof claim 1 , reduces the environmental impact of the ractopamine treatment.5. The method of claim 1 , wherein the effective amount of ...

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11-04-2013 дата публикации

Thiazole Derivatives as SGLT2 Inhibitors and Pharmaceutical Composition Comprising Same

Номер: US20130090298A1
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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18-04-2013 дата публикации

AVERMECTIN/METRONIDAZOLE COMPOSITIONS FOR TREATING AFFLICTIONS OF THE SKIN, E.G., ROSACEA

Номер: US20130095051A1
Принадлежит: GALDERMA S.A.

Pharmaceutical/dermatological compositions containing at least one avermectin compound, e.g., ivermectin and metronidazole or salt, ester or derivative thereof, are useful for treating afflictions of the skin, especially rosacea. 1. A pharmaceutical topically applicable composition useful for treating rosacea , comprising anti-rosacea effective amounts of ivermectin and metronidazole , formulated into a topically applicable , physiologically acceptable medium therefor.2. The pharmaceutical composition as defined by claim 1 , comprising from 0.001% to 10% by weight of ivermectin relative to the total weight thereof.3. The pharmaceutical composition as defined by claim 1 , comprising from 0.0001% to 20% by weight of metronidazole relative to the total weight of the composition.4. The pharmaceutical composition as defined by claim 1 , further comprising at least one additive selected from the group consisting of chelating agents claim 1 , antioxidants claim 1 , sunscreens claim 1 , preservatives claim 1 , fillers claim 1 , electrolytes claim 1 , humectants claim 1 , dyes claim 1 , mineral acids claim 1 , organic acids claim 1 , mineral bases claim 1 , organic bases claim 1 , fragrances claim 1 , essential oils claim 1 , cosmetic active agents claim 1 , moisturizers claim 1 , vitamins claim 1 , essential fatty acids claim 1 , sphingolipids claim 1 , self-tanning compounds claim 1 , calmatives claim 1 , skin-protecting agents claim 1 , pro-penetrating agents claim 1 , gelling agents claim 1 , and mixtures thereof.5. The pharmaceutical composition as defined by claim 1 , comprising from 0.01% to 5% by weight of ivermectin relative to the total weight thereof and from 0.01% to 2% by weight of metronidazole relative to the total weight thereof.6. A pharmaceutical topically applicable composition useful for treating rosacea claim 1 , comprising anti-rosacea effective amounts of ivermectin and metronidazole claim 1 , formulated into a topically applicable claim 1 , ...

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18-04-2013 дата публикации

COMPOSITION FOR PREVENTION, AMELIORATION OR TREATMENT OF METABOLIC SYNDROME

Номер: US20130096075A1
Принадлежит: House Wellness Foods Corporation

A composition comprising (a) and (b), and a food or drink or a medicine comprising the composition, wherein 1. A composition for the prevention , amelioration , or treatment of metabolic syndrome , the composition comprising (a) and (b):(a) at least a kind of polyphenols selected from the group consisting of a polyphenol containing 15 mass % or more of proanthocyanidin having a polymerization degree of 1 to 3, hesperidin, a hesperidin derivative, and hesperetin; and(b) at least a kind of xanthine derivatives, the mass ratio of (a):(b) in the composition being 1:(0.001 to 5).2. The composition according to claim 1 , wherein the mass ratio of (a):(b) is 1:(0.01 to 0.5).3. The composition according to claim 1 , wherein the xanthine derivative is caffeine claim 1 , theophylline claim 1 , or theobromine.4. A medicine claim 1 , a food or drink claim 1 , or a feed comprising the composition according to .5. A food or drink comprising the composition according to claim 1 , the food or drink being labeled as at least one selected from the group consisting of improving lipid metabolism; promoting basal metabolism; reducing body weight; reducing visceral fat or subcutaneous fat; having a slimming effect; preventing or treating obesity claim 1 , or ameliorating a symptom thereof; and preventing or treating metabolic syndrome claim 1 , or ameliorating a symptom thereof. The present invention relates to a composition for the prevention, amelioration, or treatment of metabolic syndrome. More specifically, the present invention relates to a composition comprising a polyphenol and a xanthine derivative, for the prevention, amelioration, or treatment of metabolic syndrome.In recent years, with steadily increasing obesity, the World Health Organization (WHO) is warning countries around the world of an increased risk of lifestyle-related diseases, which are associated with obesity and include diabetes, hyperlipidemia, hypertension, arteriosclerosis, and fatty liver. Metabolic syndrome ...

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25-04-2013 дата публикации

AMORPHOUS ROXITHROMYCIN COMPOSITION

Номер: US20130102550A1
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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25-04-2013 дата публикации

ANTIBIOTIC COMPOSITIONS

Номер: US20130102551A1
Принадлежит:

The invention relates to solid pharmaceutical or veterinary compositions comprising substantially pure Tulythromycin A in form of an addition salt with one or more acids, and to methods for preparing them. Following reconstitution with an aqueous solvent, the resulting solutions of Tulathromycin A may be administered to a mammal in order to treat bacterial or protozoal infections. 1. A solid pharmaceutical or veterinary composition comprising essentially pure Tulathromycin A in form of an addition salt with the one or more acids.2. The composition of claim 1 , wherein the essentially pure Tulathromycin A comprises more than 97% Tulathromycin A and less than 3% of Tulathromycin B.3. The composition of claim 1 , wherein the one or more acids are selected from the group consisting of acetic acid claim 1 , benzenesulfonic acid claim 1 , citric acid claim 1 , methanesulfonic acid claim 1 , p-toluenesulfonic acid claim 1 , hydrochloric acid claim 1 , D- and L-lactic acid claim 1 , succinic acid claim 1 , palmitic acid claim 1 , benzoic acid claim 1 , sulfuric acid claim 1 , D- and L. tartraric acid claim 1 , malic acid claim 1 , malonic acid claim 1 , fumaric acid claim 1 , phosphoric acid claim 1 , and mixtures thereof.4. The composition of claim 3 , wherein the one or more acids is citric acid.5. The composition of claim 3 , wherein the one or more acids are citric acid and hydrochloric acid.6. The composition of claim 1 , wherein the addition salt of the essentially pure Tulathromycin A is present in amorphous form.7. A pharmaceutical or veterinary kit for administering substantially pure Tulathromycin A to a mammal claim 1 , comprising a first and a second container claim 1 , whereinthe first container comprises a solid composition of essentially pure Tulathromycin A in form of an addition salt with one or more acids, andthe second container comprises a solvent comprising water and optionally a water-miscible solvent, an antioxidant and/or a preservative.8. The ...

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02-05-2013 дата публикации

COMPOSITION FOR TREATING OR PREVENTING NEURODEGENERATIVE BRAIN DISEASES COMPRISING BLACK BEAN EXTRACT

Номер: US20130109640A1
Автор: Kim Myeong Ok

The present invention relates to a composition for treating or preventing neurodegenerative brain diseases comprising a black bean extract, and more particularly, to a composition for treating or preventing neurodegenerative brain diseases comprising a black bean extract or a fraction thereof, which comprises 15-25 wt % of delphinidin-3-glucoside, 65-80 wt % of cyanidin-3-glucoside and 5-10 wt % of petunidin-3-glucoside, a functional food composition for enhancing brain or cognitive function comprising the black bean extract or a fraction thereof, and a method for preparing the composition. 1. A composition for preventing or treating neurodegenerative brain disease , comprising a black bean extract or a fraction thereof , which comprises 15-25 wt % of delphinidin-3-glucoside , 65-80 wt % of cyanidin-3-glucoside and 5-10 wt % of petunidin-3-glucoside.2. The composition of claim 1 , wherein the black bean extract is prepared by extraction with water claim 1 , an organic solvent or a mixed solvent thereof.3. The composition of claim 1 , further comprising a pharmaceutically acceptable carrier.4. The composition of claim 1 , wherein the black bean is soybean cultivar “Core-Green Geomjeongkong #1”.5. The composition of claim 1 , wherein the black bean extract is used in an amount of 0.01 mg or more.6. The composition of claim 1 , wherein the neurodegenerative brain disease is dementia or Alzheimer's disease.7. The composition of claim 1 , wherein the neurodegenerative brain disease is a disease induced by beta-amyloid protein in brain cells.8. The composition of claim 1 , wherein the black bean extract has an effect of protecting neuronal cells.9. The composition of claim 8 , wherein the effect of protecting neuronal cells is achieved by reducing a cytoxicity on the neuronal cells.10. The composition of claim 8 , wherein the neuronal cells are cerebral cortical or hippocampal neuronal cells.11. The composition of claim 8 , wherein the effect of protecting neuronal cells ...

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02-05-2013 дата публикации

USE OF FLAVONOIDE COMPOUNDS FOR THE PROPHYLAXIS AND THERAPY OF ISCHAEMIC OR INFLAMMATORY HEART AND CARDIOVASCULAR DISEASES

Номер: US20130109641A1
Принадлежит:

The present invention relates to the use of flavonoid compounds, particularly quercetin-3-O-β-D-glucuronide and kaempferol-3-O-β-D-glucuronide and their glucosides, for preventing diseases of the heart. Red vine leaf extract has proved a particularly advantageous source of the flavonoid compounds in question. 1. Use of A method of using quercetin-3-O-β-D-glucuronide , kaempferol-3-O-β-D-glucuronide , or a combination thereof for preventing diseases of the heart induced ischaemically or by inflammation.2. The method according to claim 1 , wherein the quercetin-3-O-β-D-glucuronide claim 1 , kaempferol-3-O-β-D-glucuronide claim 1 , or the combination thereof is administered by intravascular route.3. The method according to claim 1 , wherein the quercetin-3-O-β-D-glucuronide claim 1 , kaempferol-3-O-β-D-glucuronide claim 1 , or the combination thereof is administered by oral route in the form of their corresponding glucosides.4. The method according to claim 1 , wherein quercetin-3-O-β-D-glucoside or kaempferol-3-O-β-D-glucoside is administered by oral route in the form of their corresponding glucosides.5. The method according to claim 3 , wherein the quercetin-3-O-β-D-glucuronide claim 3 , kaempferol-3-O-β-D-glucuronide claim 3 , or the combination thereof is part of a composition.6. The method according to claim 5 , wherein the composition is an extract of red vine leaf.7. The method according to claim 6 , wherein the extract used is the one marketed as AS195.8. The method according to claim 1 , wherein the diseases of the heart are selected from among myocardial infarct and heart failure. The present invention relates to the use of flavonoid compounds, particularly flavonol glucosides and flavonol glucuronides, especially quercetin-3-O-β-D-glucoside, kaempferol-3-O-β-D-glucoside and the corresponding glucuronides, quercetin-3-O-β-D-glucuronide and kaempferol-3-O-β-D-glucuronide, for preventing heart and circulatory disease. Certain vegetable extracts, e.g. endive, ...

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02-05-2013 дата публикации

ADMINISTRATION OF AVERMECTIN/MILBEMYCIN COMPOUNDS FOR THE TREATMENT OF OPHTHALMIC PATHOLOGIES

Номер: US20130109642A1
Принадлежит: GALDERMA S.A.

Administration of at least one compound of the family of the avermectins or of the family of the milbemycins, notably ivermectin, is useful for the treatment of ophthalmic pathologies, including ocular rosacea. 1. A pharmaceutical composition useful for the treatment of symptoms of ocular rosacea in the eye(s) , said composition comprising a thus effective amount of ivermectin , formulated into an eyewash composition with a pharmaceutically acceptable vehicle therefor , wherein ivermectin is the sole active ingredient for treating said symptoms of ocular rosacea in said eyewash composition , said eyewash composition being sterile , non-irritating and compatible with eye tissue , said eyewash composition comprising ivermectin , polysorbate 80 , benzalkonium chloride , EDTA , water and a buffer system to adjust pH , said eyewash composition comprising from 0.001% to 0.10% by weight of ivermectin relative to the total weight of the composition.2. The pharmaceutical composition as defined by claim 1 , comprising from 0.01% to 0.10% by weight of ivermectin relative to the total weight of the composition.3. The pharmaceutical composition as defined by claim 2 , comprising 0.03% by weight of ivermectin relative to the total weight of the composition.4. A pharmaceutical composition useful for the treatment of symptoms of ocular rosacea in the eye(s) claim 2 , said composition comprising a thus effective amount of ivermectin claim 2 , formulated into an eye gel composition with a pharmaceutically acceptable vehicle therefor claim 2 , wherein ivermectin is the sole active ingredient for treating said symptoms of ocular rosacea in said eye gel composition claim 2 , said eye gel composition being sterile claim 2 , non-irritating and compatible with eye tissue claim 2 , said eye gel composition comprising ivermectin claim 2 , polysorbate 80 claim 2 , phenylethyl alcohol claim 2 , hydroxypropylcellulose claim 2 , sorbitol claim 2 , water and a buffer system to adjust pH claim 2 , ...

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09-05-2013 дата публикации

COMPOSITION CONTAINING IRIDOIDS AND USES THEREOF

Номер: US20130116205A1

Composition containing iridoids such as morroniside and loganin, the use thereof in preparing medicaments for preventing and treating neurologic demyelinating diseases, and the method thereof in treating diseases related to neurologic demyelinating lesions are disclosed by the present application. 1. A use of a composition comprising an iridoid compound in the manufacture of a medicament for alleviating or repairing a disease associated with nervous system myelin sheath lesion.2. The use according to claim 1 , wherein the iridoid compound is morroniside or its homolog or analog claim 1 , and/or loganin or its homolog or analog.3. The use according to claim 2 , wherein morroniside is 25-50% w/w of the composition claim 2 , and loganin is 25-40% w/w of the composition.4Fructus corni,. The use according to claim 1 , wherein the composition is an extract of wherein morroniside is 25-50wt % relative to the total weight of the extract claim 1 , and loganin is 25-40wt % relative to the total weight of the extract.5. The use according to claim 1 , wherein the alleviating nervous system myelin sheath lesion is used for the treatment of a disease with myelin sheath lesion caused by various reasons claim 1 , or for the treatment of a demyelinating disease of nervous system.6. The use according to claim 5 , wherein the disease is multiple sclerosis claim 5 , optical neuromyelitis claim 5 , acute disseminated encephalomyelitis claim 5 , diffuse sclerosis claim 5 , concentric circle sclerosis claim 5 , leukodystrophy claim 5 , central pontine myelinolysis claim 5 , acute inflammatory demyelinating polyneuropathy or chronic inflammatory demyelinating polyneuropathy claim 5 , or the disease is leukoencephalopathy caused by an ischemia-anoxia disease claim 5 , subacute combined degeneration caused by a nutrition deficiency disease claim 5 , subacute sclerosing panencephalitis or progressive multifocal leukoencephalopathy caused by a viral infection.7. The use according to claim 5 , ...

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16-05-2013 дата публикации

METHODS AND COMPOSITIONS FOR INHIBITING THE NUCLEAR FACTOR KAPPAB PATHWAY

Номер: US20130122114A1
Принадлежит:

The current invention provides therapeutic methods which include inhibition of nuclear factor κb pathway in a cell based on the discovery of an active fraction of a plant extract termed NUP or a composition which includes NUP. NUP is used in treating and managing different diseases such as cancer, inflammation, and virus infections. 2. The composition of claim 1 , wherein said NUP inhibits a nuclear factor κB pathway in a cell.3Nuphar lutea.. The composition of claim 1 , wherein said Nymphaeaceae is4. A method for treating a subject afflicted with Hodgkin lymphoma claim 1 , melanoma claim 1 , or lung melanoma comprising administering to said subject the composition of .5. A method for enhancing the efficacy of a composition comprising podophyllotoxin drug or a platinum drug claim 1 , comprising the step of combining said composition comprising podophyllotoxin drug or said platinum drug with the composition of .6. The method of claim 5 , wherein said podophyllotoxin drug is etoposide.7. The method of claim 5 , wherein said platinum drug is cisplatin.8. A method for reducing or treating inflammation disease in a subject in need thereof claim 1 , comprising administering to said subject the composition of .9. The method of claim 8 , wherein said reducing or treating inflammation disease is affected by reducing pro-inflammatory cytokines and elevating anti-inflammatory cytokine in the blood of said subject.10. The method of claim 8 , wherein said inflammation disease is inflammatory bowel disease (IBD) claim 8 , ulcerative colitis (UC) or Crohn's disease (CD).11. A method for treating a subject afflicted with Respiratory Syncytial Virus claim 1 , comprising the step of administering to said subject the composition of .12. A method for preventing a cytotoxic effect of a Respiratory Syncytial Virus in a subject claim 1 , comprising the step of administering to said subject the composition of .13. A method of reducing the contagiousness of a subject infected by a ...

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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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23-05-2013 дата публикации

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

Номер: US20130130997A1
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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23-05-2013 дата публикации

METHOD OF DETERMINING ACUTE MYELOID LEUKEMIA RESPONSE TO TREATMENT WITH FARNESYLTRANSFERASE INHIBITORS

Номер: US20130130999A1
Принадлежит: Veridex, LLC

The disclosed method rapidly identifies with desired accuracy AML patients, including elderly AML patients, likely to respond to treatment with a combination of a farnesyltransferase inhibitor and one or more of etoposide, teniposide, tamoxifen, sorafenib, paclitaxel, temozolomide, topotecan, trastuzumab and cisplatinum. In an embodiment, the improvements include the use of whole blood rather than the customary bone marrow sample, thus making the assay more accurate, rapid, less intrusive, less expensive as well as less painful. The method includes evaluation of a two-gene expression ratio (RASGRP1:APTX), which with a corresponding threshold, provides sufficient accuracy for predicting the response to the combination treatment. In the preferred embodiment the combination treatment combines tipifarnib (R115777, ZARNESTRA®) with etoposide. Further, the elderly AML patients identified as being likely responsive to the combination treatment with tipinifarb and etoposide have a complete recovery rate comparable to the best therapy available for younger patients. 1. A method for administering tipinifarb and etoposide to a patient diagnosed with a disorder , the method comprising:determining if a ratio of RASGRP1 and APTX expression, each level computed using the ΔΔCt method, exceeds a ΔΔCt threshold corresponding to a specified sensitivity or specificity or a maximized sum of sensitivity and specificity in a ROC analysis in a test population; andadministering a therapeutically effective amount of tipifarnib if the ratio exceeds the ΔΔCt threshold.3. The method of wherein a level of expression of RASGPR1 is estimated relative to one or more of the group consisting of APTX claim 1 , beta-actin and HMBS.4. The method of wherein the ΔΔCt threshold is about 5.2.5. The method of wherein the ΔΔCt threshold corresponds to an area under the curve of about 70% or more.6. The method of claim 1 , wherein the assay is performed in a single tube in a multiplex format.7. The method of ...

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23-05-2013 дата публикации

Composition Comprising Ligustroflavone, Rhoifolin and Hyperin and Its Pharmaceutical Application

Номер: US20130131000A1
Принадлежит:

Disclosed is a composition comprising ligustroflavone, rhoifolin and hyperin, which is prepared according to rational weight ratio: 40% to 80% ligustroflavone, 5% to 45% rhoifolin and 1% to 40% hyperin. The composition can be used as a neuraminidase inhibitor for preventing and treating influenza, and can be formulated into pharmaceutically acceptable dosage forms. 2. The composition according to claim 1 , wherein the rational weight ratio is 45% to 75% ligustroflavone claim 1 , 10% to 40% rhoifolin and 5% to 35% hyperin.3. The composition according to claim 2 , wherein the rational weight ratio is 50% to 70% ligustroflavone claim 2 , 15% to 35% rhoifolin and 10% to 30% hyperin.4. The composition according to claim 3 , wherein the rational weight ratio is 55% to 65% ligustroflavone claim 3 , 20% to 30% rhoifolin and 15% to 25% hyperin.5. The composition according to claim 4 , wherein the rational weight ratio is 58% ligustroflavone claim 4 , 25% rhoifolin and 17% hyperin.6. A method for preventing claim 4 , treating influenza and its complications comprising administering a composition comprising a ligustroflavone claim 4 , a rhoifolin and a hyperin to a patient claim 4 , a rational weight ratio of the composition is 40% to 80% ligustroflavone claim 4 , 5% to 45% rhoifolin and 1% to 40% hyperin.7. The method according to claim 6 , wherein the composition is used to inhibit the influenza virus.8. The method according to claim 7 , wherein the composition is used to inhibit influenza virus FM1.9. The method according to claim 6 , wherein the composition is used to inhibit the neuraminidase.10. The method according to claim 6 , wherein the complication refers to the kidney failure.11. The method according to claim 6 , wherein the complication refers to the spleen injury or/and lung injury.12. A pharmaceutical composition comprising the composition claimed in the as active components and one or more pharmaceutically acceptable excipients.13. An extraction method of a ...

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06-06-2013 дата публикации

PYRAZOLE DERIVATIVES

Номер: US20130142757A1
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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13-06-2013 дата публикации

Process for extracting materials from biological material

Номер: US20130149322A1
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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13-06-2013 дата публикации

Trioxacarcins and uses thereof

Номер: US20130150314A1
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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20-06-2013 дата публикации

METHOD OF PREVENTING EARLY LAWSONIA INTRACELLULARIS INFECTIONS

Номер: US20130156811A1
Принадлежит: Boehringer Ingelheim Vetmedica, Inc.

The present invention relates inter alia to the use of a combination of a vaccine against and an anti-antibiotic for the prevention or reduction of early, preferably fulminant infections. The present invention relates particularly to the use of a live vaccine in conjunction with an antibiotic that is effective against for the avoidance or reduction of early infections in animals. 1Lawsonia intracellularisLawsonia intracellularisLawsonia intracellularis,Lawsonia intracellularisLawsonia intracellularis. A method of reducing early infections in piglets comprising administering a live vaccine and an antibiotic that is effective against wherein said live vaccine is administered within the first four weeks of life of said piglets and the antibiotic is administered over a period of 12 to 21 days starting at day 3 after the administration of said live vaccine.2. The method according to claim 1 , wherein said early infections is a fulminant infection.3Lawsonia intracellularis. The method according to claim 1 , wherein said vaccine is administered within the first three weeks of life of said piglets.4. The method according to claim 1 , wherein said antibiotic is administered at least until reliable immunity is detected.5Lawsonia intracellularis. The method according to claim 4 , wherein the reliable immunity detection is determined by the detection of -specific antibodies in the vaccinated piglets.6Lawsonia intracellularis. The method according to claim 1 , wherein said antibiotic is administered to the piglets starting on day 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 or 7 after the administration of said vaccine.7Lawsonia intracellularis. The method according to claim 1 , further comprising additionally administering said antibiotic before said vaccine is administered.8Lawsonia intracellularis. The method according to claim 7 , wherein said antibiotic is administered from 1 to 3 days before the administration of said vaccine.9. The method according to claim 1 , wherein said ...

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20-06-2013 дата публикации

NEW USE OF ICARIIN AND EPIMEDIUM FLAVONOIDS CONTAINING ICARIIN

Номер: US20130157966A1

New use of icariin and Epimedium flavaoids containing icariin is provided by the present invention. Specifically, uses of compounds of Formula I or Epimedium containing compounds of formula I, Epimedium flavanoids, or extracts of Epimedium in manufacturing medicaments for treating, preventing, reducing and/or relieving diseases and/or conditoins related to neural myelin sheath impairments, or use of above materials in manufacturing medicaments for relieving demyelination and/or promoting repair of myelin sheath are provided by the present application, wherein, Ris selected from H, halogen, —Calkyl, and —C(O)—Calkyl 3. The process according to claim 1 , further comprising any one or more of the following items a) to e):a) the composition comprises an effective amount of a compound of Formula I, an Epimedium comprising a compound of Formula I, Epimedium flavanoids comprising a compound of Formula I, or an Epimedium extract comprising a compound of Formula I, and optionally a pharmaceutically acceptable carrier;b) the Epimedium, Epimedium flavanoids or Epimedium extract comprises therapeutically, prophylactically, alleviatively and/or relievedly effective amount of icariin;{'sub': 33', '40', '15, 'c) the Epimedium, expressed in dry product, contains icariin (CHO) in an amount of not less than 0.5% (wt/wt), or not less than 1.0%, 2.0%, or 5.0%;'}{'sub': 33', '40', '15, 'd) the Epimedium flavanoids contains icariin (CHO) in an amount of 20-90% (wt/wt), or 25-85%, 30-80%, 35-80%, 40-80%, 45-80%, 50-75%, 50-70%, 30-90%, 40-90%, 50-90%, 55-90%, or 60-90%;'}{'sub': 33', '40', '15, 'e) the Epimedium flavanoids contains icariin (CHO) in an amount of 10-90% (wt/wt), or 15-85%, 20-80%, 25-80%, 30-80%, 35-80%, 40-75%, 40-70%, 20-90%, 30-90%, 40-90%, 50-90%, 55-90%, or 60-90%.'}4. The process according to claim 1 , further comprising any one of the following items a) to d):a) the disease and/or disorder associated with nervous system myelin sheath lesion is a disease and/or ...

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27-06-2013 дата публикации

TELODENDRIMER NANODISCS WITHOUT APOLIPOPROTEIN

Номер: US20130164369A1

The present invention provides a nanodisc without a membrane scaffold protein. The nanodisc includes a telodendrimer and a lipid; the nanodisc does not include a membrane scaffold protein. The telodendrimer has the general formula PEG-L-D-(R), wherein D is a dendritic polymer; L is a bond or a linker linked to the focal point group of the dendritic polymer; each PEG is a poly(ethylene glycol) polymer; each R is and end group of the dendritic polymer, or and end group with a covalently bound hydrophobic group, hydrophilic group, amphiphilic compound, or drug; and subscript n is an integer from 2 to 20. Methods of making the nanodiscs are also provided. 1. A nanodisc without a membrane scaffold protein , the nanodisc comprising:a telodendrimer; anda lipid,wherein the nanodisc does not include a membrane scaffold protein.3. The nanodisc of claim 2 , wherein each branched monomer unit X is lysine.6. The nanodisc of claim 2 , wherein each R is independently selected from the group consisting of cholic acid claim 2 , (3α claim 2 ,5β claim 2 ,7α claim 2 ,12α)-7 claim 2 ,12-dihydroxy-3-(2 claim 2 ,3-dihydroxy-1-propoxy)-cholic acid (CA-4OH) claim 2 , (3α claim 2 ,5β claim 2 ,7α claim 2 ,12α)-7-hydroxy-3 claim 2 ,12-di(2 claim 2 ,3-dihydroxy-1-propoxy)-cholic acid (CA-5OH) claim 2 , (3α claim 2 ,5β claim 2 ,7α claim 2 ,12α)-7 claim 2 ,12-dihydroxy-3-(3-amino-2-hydroxy-1-propoxy)-cholic acid (CA-3OH—NH) claim 2 , cholesterol formate claim 2 , doxorubicin claim 2 , and rhein.7. The nanodisc of claim 2 , wherein each R is cholic acid.8. The nanodisc of claim 2 , wherein the telodendrimer is selected from the group consisting of PEG-D-CAand PEG-D-CA claim 2 , wherein each dendritic polymer D is a poly(lysine) dendritic polymer.9. The nanodisc of claim 1 , wherein the lipid is selected from the group consisting of a phospholipid claim 1 , a lysolipid claim 1 , cholesterol claim 1 , a phosphatidylcholine claim 1 , a phosphatidylethanolamine claim 1 , a phosphatidylglycerol claim 1 ...

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27-06-2013 дата публикации

6,11-BRIDGED BIARYL MACROLIDES

Номер: US20130165641A1
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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04-07-2013 дата публикации

Anthracycline-Antibody Conjugates for Cancer Therapy

Номер: US20130171176A1
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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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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04-07-2013 дата публикации

METHOD OF TREATING HERPES VIRUS INFECTION USING MACROCYCLIC LACTONE COMPOUND

Номер: US20130172282A1
Принадлежит: GALDERMA S.A.

A method of treating herpes simplex virus infection or varicella zoster virus infection is disclosed. The method includes topically applying a composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to the affected area of an individual suffering from herpes simplex virus infection or varicella zoster virus infection. 1. A method of treating herpes virus infection comprising locally applying a composition comprising an effective amount of one or more avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to an affected area of an individual suffering from herpes simplex virus infection or varicella zoster virus infection.2. The method of claim 1 , wherein said virus infections are caused by herpes simplex virus-1 claim 1 , herpes simplex virus-2 claim 1 , or varicella zoster virus.3. The method of claim 1 , wherein said virus infections are herpes simplex including orofacial herpes claim 1 , herpetic gingivostomatitis claim 1 , herpes labialis claim 1 , herpes genitalis claim 1 , herpetic whitlow claim 1 , herpes gladiatorum claim 1 , or herpetic sycosis; or herpes zoster (or shingles) including herpes zoster oticus; or chickenpox.4. The method of claim 1 , wherein said method comprises topically applying said composition on said affected area associated with herpes simplex claim 1 , herpes zoster claim 1 , or chickenpox.5. The method of claim 1 , wherein said method comprises topically applying said composition on lesions associated with herpes simplex claim 1 , herpes zoster or chickenpox.6. The method of claim 1 , wherein said method comprises applying said composition into blisters associated with herpes simplex claim 1 , herpes zoster or chickenpox.7. The method of claim 1 , wherein said topically applying said composition on said affected area includes scratching the surface of the skin of an affected ...

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11-07-2013 дата публикации

METHOD OF TREATING HEMORRHOIDS USING MACROCYCLIC LACTONE COMPOUND

Номер: US20130178433A1
Принадлежит: GALDERMA S.A.

A method of treating hemorrhoids is disclosed. The method includes locally administering a composition including an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds, milbemycin compounds, or mixture thereof and a pharmaceutically acceptable carrier to the affected anorectal region of an individual suffering from hemorrhoid. 1. A method of treating hemorrhoid comprising locally administering a composition comprising an effective amount of one or more avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to affected region of an individual suffering from hemorrhoid.2. The method of claim 1 , wherein said composition is administered intrarectally to said individual.3. The method of claim 1 , wherein said composition is administered topically to the anal verge and the perianal skin to said individual.4. The method of claim 1 , wherein said composition is applied with a gloved finger or using a nozzle.5. The method of claim 1 , wherein said composition is administered one to more times a day to said affected region.6. The method of claim 1 , wherein said hemorrhoid is an internal or external hemorrhoid.7. The method of claim 1 , wherein said avermectin compounds comprise avermectins or avermectin derivatives.8. The method of claim 7 , wherein said avermectin derivatives comprise ivermectin claim 7 , ivermectin derivatives claim 7 , emamectin claim 7 , doramectin claim 7 , selamectin claim 7 , eprinomectin claim 7 , or latidectin.9. The method of claim 7 , wherein said composition comprises one or more said avermectin compounds in a concentration from about 0.001% to about 10% (w/w) in said composition.10. The method of claim 1 , wherein said milbemycin compounds comprise milbemycins or milbemycin derivatives.11. The method of claim 10 , wherein said milbemycin derivatives comprise moxidectin claim 10 , nemadectin claim 10 , milbemycin oxime claim 10 , or lepimectin.12. The method of claim 10 , ...

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11-07-2013 дата публикации

METHOD OF TREATING OTITIS EXTERNA USING MACROCYCLIC LACTONE COMPOUND

Номер: US20130178434A1
Принадлежит: GALDERMA S.A.

A method of treating otitis externa is disclosed. The method includes topically applying an otic composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier into the external auditory canal and the auricle of an affected ear of an individual suffering from otitis externa. 1. A method of treating otitis externa comprising topically applying an otic composition comprising an effective amount of one or more avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to an affected ear of an individual suffering from otitis externa.2. The method of claim 1 , wherein said otic composition is applied into the external auditory canal of said affected ear.3. The method of claim 2 , wherein said otic composition is applied with an applicator claim 2 , dropped claim 2 , or sprayed into the external auditory canal.4. The method of claim 1 , wherein said otic composition is topically applied on the auricle of said affected ear.5. The method of claim 1 , wherein said otic composition is topically applied one or more times to said affected ear.6. The method of claim 1 , wherein said otic composition is applied at early onset of said otitis externa.7. The method of claim 1 , wherein said avermectin compounds comprise avermectins or avermectin derivatives.8. The method of claim 7 , wherein said avermectin derivatives comprise ivermectin claim 7 , ivermectin derivatives claim 7 , emamectin claim 7 , doramectin claim 7 , selamectin claim 7 , eprinomectin claim 7 , or latidectin.9. The method of claim 7 , wherein said otic composition comprises one or more said avermectin compounds in a concentration from about 0.001% to about 10% (w/w) in said composition.10. The method of claim 1 , wherein said milbemycin compounds comprise milbemycins or milbemycin derivatives.11. The method of claim 10 , wherein said milbemycin derivatives ...

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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
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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08-08-2013 дата публикации

CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY

Номер: US20130203700A1
Принадлежит: CERULEAN PHARMA INC.

The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein. 1. A pharmaceutical composition comprising a sugar and a water soluble linear polymer conjugate , wherein the water soluble linear polymer conjugate comprises:a linear polymer comprising beta cyclodextrin moieties and comonomers which do not contain beta cyclodextrin moieties (comonomers); andtaxane moieties covalently linked to the linear polymer via glycine linkers, wherein the taxane moieties are cleaved from the water soluble linear polymer conjugate under biological conditions to release the taxane moieties;wherein the water soluble linear polymer conjugate comprises at least four beta cyclodextrin moieties and at least four comonomers.2. The pharmaceutical composition of claim 1 , wherein the comonomer comprises a polyethylene glycol.3. The pharmaceutical composition of claim 2 , wherein the polyethylene glycol has a molecular weight of 0.2 kDa to 5 kD.4. The pharmaceutical composition of claim 1 , wherein each of the at least four beta cyclodextrin moieties alternates with each of the at least four comonomers in the water soluble linear polymer conjugate.5. The pharmaceutical composition of claim 1 , wherein the taxane moieties are ...

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15-08-2013 дата публикации

TOPICAL APPLICATION OF IVERMECTIN FOR THE TREATMENT OF DERMATOLOGICAL CONDITIONS/AFFLICTIONS

Номер: US20130209381A1
Принадлежит: GALDERMA S.A.

Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin. 1. A method for the treatment of common acne , seborrheic dermatitis , perioral dermatitis , an acneform rash , transient acantholytic dermatosis or acne necrotica milliaris , comprising topically applying onto the affected skin area of an individual in need of such treatment , a topical pharmaceutical composition which comprises a thus effective amount of ivermectin , said topical pharmaceutical composition being formulated as an emulsion , the topical pharmaceutical emulsion comprising:an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax;at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;ivermectin;a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;one or more gelling agents selected from the group consisting of carbomers, cellulose gelling agents, xanthan gums, aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica, guar gums, polyacrylamides and modified starches; andwater;said emulsion being chemically stable over a period of time of 8 weeks.2. The method as defined by claim 1 , wherein the topical pharmaceutical ...

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15-08-2013 дата публикации

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

Номер: US20130210705A1
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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29-08-2013 дата публикации

METHOD FOR ISOLATING SMALL MOLECULES WITH IMPORTANT BIOLOGICAL ACTIVITY USING YEAST

Номер: US20130225515A1

Methods of isolating biologically active molecules from an organism, for example from a fungus, are described. The methods involve isolating an active molecule which possesses a specific biological activity on, in or against wild-type yeast cells, but not on, in or against yeast cells that express a given ABC transporter from a given organism, including but not limited to species such as . In preferred embodiments, the biological activity is antifungal activity. In most preferred embodiments, the antifungal activity is against a human pathogen, including but not limited to . The biologically active molecules can be formulated as pharmaceutical compositions and used to treat fungal infections in a subject, including a human subject. 1. A method of isolating a biologically active molecule from an organism , which comprises:a) preparing total extract from a wild type or ABC transporter-deletion mutant organism;b) testing said total extract for a specific biological activity on wild-type yeast cells;c) expressing said ABC transporter in wild-type yeast cells;d) testing said total extract for said specific biological activity on ABC transporter-expressing yeast cells;e) subjecting said total extract to chromatographic fractionation to obtain one or more fractions;f) testing said fractions to identify one or more specific fraction that exhibits said biological activity only on wild type but not ABC transporter-expressing yeast cells;g) purifying by further chromatography said specific fraction that exhibits said biological activity only on wild type but not ABC transporter-expressing yeast cells to obtain purified fractions;h) testing each of said purified fractions for said biological activity on wild type yeast cells and ABC transporter-expressing yeast cells to identify one or more purified fraction that exhibits said biological activity only on wild type but not ABC transporter-expressing yeast cells;i) pooling said purified fractions that exhibit said biological ...

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05-09-2013 дата публикации

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

Номер: US20130231298A1
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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05-09-2013 дата публикации

POLYETHERESTER POLYOLS AND THE USE THEREOF FOR PRODUCING RIGID POLYURETHANE FOAMS

Номер: US20130231413A1
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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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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12-09-2013 дата публикации

METHODS AND COMPOSITIONS FOR TREATING INFLAMMATORY BOWEL DISEASE

Номер: US20130237488A1
Принадлежит: RED HILL BIOPHARMA LTD.

The present disclosure provides improved compositions comprising rifabutin, clarithromycin, and clofazimine for use in the treatment of Inflammatory Bowel Diseases. In one instance, the compositions may comprise a formulation of rifabutin, clarithromycin, and clofazimine in a single dosage form, such as a capsule, tablet, etc., with one or more specific excipients. 1. A method to treat inflammatory bowel disease comprising: rifabutin;', 'clarithromycin;', 'clofazimine; and', 'wherein the polyethylene glycol (i) has an average molecular weight of between 1000-15000 Daltons, and (ii) is between 300% and 700% w/w relative to the amount of clofazimine; and', 'polyethylene glycol,'}], 'providing a solid oral dosage form comprisingadministering, to a patient, the solid oral dosage form.2. The method of claim 1 , wherein the polyethylene glycol has an average molecular weight of between 5000-12000 Daltons.3. The method of claim 1 , wherein the rifabutin claim 1 , clarithromycin claim 1 , and clofazimine are present in a 9±0.5:19±0.5:2±0.5 w/w/w ratio.4. The method of claim 1 , wherein the solid oral dosage form is administered twice each day for a first period of treatment.5. The method of claim 4 , wherein the first period of treatment is one week.6. The method of claim 4 , wherein following the first period of treatment claim 4 , the solid oral dosage form is administered four times each day for a second period of treatment.7. The method of claim 6 , wherein the second period of treatment is one week.8. The method of claim 6 , wherein following the second period of treatment claim 6 , the solid oral dosage form is administered six times each day for a third period of treatment.9. The method of claim 8 , wherein the third period of treatment is one week.10. The method of claim 8 , wherein following the third period of treatment claim 8 , the solid oral dosage form is administered eight times each day for a fourth period of treatment.11. The method of claim 10 , wherein ...

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19-09-2013 дата публикации

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

Номер: US20130243860A1
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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19-09-2013 дата публикации

ABNORMAL INTRAOCULAR PRESSURE TREATMENT

Номер: US20130244961A1
Принадлежит:

Methods and compositions for reducing intraocular pressure in a patient, particularly a human patient, are described. In particular, compositions are disclosed that contain an anthocyanoside or an extract comprising it, a proanthhocyanidin or an extract comprising it and combinations thereof. The compositions are useful for lowering intraocular pressure. 1. A pharmaceutical composition for the treatment or prevention of high or abnormal intraocular pressure comprising (1) a therapeutically effective amount of at least one of an anthocyanoside , a proanthocyanidin or a combination thereof , and (2) a pharmaceutically acceptable excipient.2. The composition of claim 1 , comprising therapeutically effective amounts of at least one anthocyanoside and at least one proanthocyanidin.3. The composition of claim 2 , wherein said at least one proanthocyanidin is an extract comprising at least one proanthocyanidin.4. The composition of claim 2 , wherein said at least one anthocyanoside is an extract comprising at least one anthocyanoside.5. The composition of claim 3 , wherein said extract comprises a plant extract.6. The composition of claim 5 , wherein said plant extract comprises a pine bark extract claim 5 , a grape seed extract or an extract of apples claim 5 , peanut skin claim 5 , walnuts claim 5 , pomegranates claim 5 , tomatoes claim 5 , almonds claim 5 , tea claim 5 , hawthorn or cocoa.7Pinus pinaster. The composition of claim 6 , wherein said pine bark extract is from a pine of the species.8Vitis vinifera. The composition of claim 6 , wherein said grape seed extract is from species.9. The composition of claim 4 , wherein said extract comprises a plant extract.10. The composition of claim 9 , wherein said plant extract is a red fruit extract.11Vaccinium myrtillus.. The composition of claim 10 , wherein the red fruit extract is from12. The composition of claim 10 , wherein the red fruit extract is from blueberry claim 10 , cherry claim 10 , cranberry claim 10 , red ...

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26-09-2013 дата публикации

Glycomimetic compounds as anti-infectious against pathogens lectins

Номер: US20130252910A1

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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26-09-2013 дата публикации

18-Membered Macrocycles and Analogs Thereof

Номер: US20130252913A1
Принадлежит: OPTIMER PHARMACEUTICALS, INC.

The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specifically infections. 2. The compound of claim 1 , which is greater than 90% stereomeric purity.3. The compound of claim 1 , which is greater than 95% stereomeric purity.4. The compound of claim 1 , which is greater than 99% stereomeric purity.6. The composition of claim 5 , wherein the compound is greater than 90% stereomeric purity.7. The composition of claim 5 , wherein the compound is greater than 95% stereomeric purity.8. The composition of claim 5 , wherein the compound is greater than 99% stereomeric purity.9. The composition of further comprising a pharmaceutically acceptable carrier.10. The composition of further comprising 0-20% of Tiacumicin B related compounds.11. The composition of claim 10 , wherein said Tiacumicin B related compounds is selected from the group consisting of Lipiarmycin A4 and C-19 Ketone.12. The composition of further comprised of an additional agent selected from the group consisting of an antimicrobial agent and an antifungal agent.13. The composition of suitable for oral administration.14. The composition of suitable for parenteral administration.15. The composition of claim 5 , wherein the compound is present in an amount of about 0.015-0.25 μg/mL.16. A method for treating bacterial infections in a mammal claim 5 , which comprises administering to said mammal a composition comprising a therapeutically effective amount of said composition of . The present application is a continuation-in-part application of International Application PCT/US2005/002887, filed Jan. 31, 2005, which is incorporated by reference in its entirety.The present invention relates generally to the 18-membered ...

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26-09-2013 дата публикации

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

Номер: US20130252914A1
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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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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10-10-2013 дата публикации

Compound

Номер: US20130267586A1
Принадлежит: ANTOXIS LIMITED

The present invention provides compounds of the formula Formula I or a salt thereof: and the uses of such compounds for the treatment of a disease or disorder involving oxidative damage, for preventing UV damage to the skin of a mammal and for preventing or reversing the effects of ageing, or for treating or preventing dry skin. 2. A compound as claimed in claim 1 , wherein:{'sub': '20', 'Rrepresents H or a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D);'}{'sub': '21', 'claim-text': i) represents H;', {'sub': '22', 'sup': 1', '2, 'ii) together with Rprovides a second bond between Cand C; or'}, {'sub': 1', '1', '1-6', '21', '1, 'sup': '1', 'iii) when X is —NR— and Ris not H or Calkyl, Rtogether with Rprovides a second bond between Cand N;'}], 'R{'sub': '22', 'claim-text': i) represents H;', {'sub': '23', 'ii) together with Rforms ═O; or'}, {'sub': '21', 'sup': 1', '2, 'iii) together with Rprovides a second bond between Cand C;'}], 'R{'sub': '23', 'claim-text': i) represents H or a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D); or', {'sub': '22', 'ii) together with Rforms ═O;'}, {'sub': 20', '23, 'wherein at least one of Rand Ris a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D).'}], 'R3. (canceled)4. (canceled)5. A compound as claimed in claim 1 , wherein:{'sub': 20', '21', '22', '23, 'sup': 1', '2, 'R, R, R, and Rform part of a 5, 6 or 7 membered unsaturated ring including Cand C, which ring (Ring A) is substituted with at least one group;'}said at least one group being a 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D); and{'sup': '1', 'wherein the 3, 4, 5, 6, 7 or 8 membered saturated or unsaturated ring (Ring D) is at the meta, para or ortho position relative to C.'}6. A compound as claimed in claim 5 , wherein the 3 claim 5 , 4 claim 5 , 5 claim 5 , 6 claim 5 , 7 or 8 membered saturated or unsaturated ring (Ring D) is at the meta position relative to C.7. A compound as claimed in claim ...

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10-10-2013 дата публикации

PROCEDURE FOR THE PURIFICATION OF TIACUMICIN B

Номер: US20130267692A1
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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17-10-2013 дата публикации

PESTICIDAL EAR TAG

Номер: US20130273134A1
Автор: Kellerby Joe D
Принадлежит:

Articles including eartags provide topical application of a mixture of (1) a macrolide of the avermectin/milbemycin class, such as, but not limited to ivermectin, abamectin, or milbemectin, and (2) a synergist of the aryl aliphatic ether-class, such as, but not limited to piperonyl butoxide, present in (3) a weight ratio of synergist:macrolide that is greater than 1:1. The articles are effective against various pests of domestic animals, including horn flies and buffalo flies. 2. The ear tag according to claim 1 , wherein the macrolide component comprises abamectin or ivermectin.3. The ear tag according to claim 1 , wherein the macrolide component comprises abamectin.4. The ear tag according to claim 1 , wherein the synergist component comprises piperonyl butoxide.5. The ear tag according to claim 4 , wherein the piperonyl butyoxide is piperonyl butoxide technical and the weight ratio of piperonyl butoxide technical to avermectin is at least about 2:1.6. The ear tag according to claim 1 , wherein the polymer resin base comprises a polymer selected from the group consisting of polyvinyl chloride claim 1 , acrylonitrile-butadiene copolymer claim 1 , polyurethane claim 1 , chlorinated polyethylene claim 1 , and mixtures thereof.7. The ear tag according to claim 1 , wherein the resin base comprises claim 1 , in addition to a polymer claim 1 , a substance selected from the group consisting of plasticizers claim 1 , stabilizers claim 1 , colorants claim 1 , fluorescents claim 1 , and mixtures thereof.8. An article capable of controlling pests of domestic animals claim 1 , comprising: a) a macrolide component comprising a pesticidal compound of the avermectin-milbemycin class; and', 'b) a synergist component comprising an aryl aliphatic ether-class synergist compound;', 'c) the weight ratio of the synergist component (b) to the macrolide component (a) being greater than 1;, 'a pesticidally effective amount of an active ingredient composition that comprises'}impregnated in ...

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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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14-11-2013 дата публикации

NOVEL PYRAZOLE COMPOUNDS

Номер: US20130303471A1
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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14-11-2013 дата публикации

SOLID STATE FORMS OF FIDAXOMYCIN AND PROCESSES FOR PREPARATION THEREOF

Номер: US20130303472A1
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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28-11-2013 дата публикации

USE OF ALBIFLORIN AND METABOLITES THEREOF

Номер: US20130316966A1
Автор: Zhang Zuoguang
Принадлежит:

Disclosed is a use of albiflorin or a metabolite thereof in preparation of antianxiety and sleep disorder improving drugs or health-care food. Tests prove that albiflorin has significant antianxiety effects and sleep disorder improving effects achieved by prolonging SWS and low the toxic side effects, thus being a safety monomer compound capable of effectively treating anxiety and sleep disorder. 1. A method for preventing , ameliorating and/or treating anxiety or sleep disorder comprising administering a medicament comprising a therapeutically effective amount of albiflorin or a metabolite of albiflorin to a patient in need thereof.2. The method according to claim 1 , wherein said metabolite of albiflorin is paeonilactone A or paeonilactone B.3. The method according to claim 1 , wherein said sleep disorder comprises insomnia sleep disorder associated with anxiety and/or depression.4. The method according to claim 1 , wherein said medicament comprises albiflorin or a metabolites of albiflorin and a pharmaceutically acceptable carrier.5. The method according to claim 1 , wherein said medicament is in the form of a tablet claim 1 , a capsule claim 1 , a pill claim 1 , a powder claim 1 , a granule claim 1 , a syrup claim 1 , a solution claim 1 , an emulsion claim 1 , an injection claim 1 , a spray claim 1 , an aerosol or patch.6. A medicament for preventing claim 1 , ameliorating and/or treating anxiety and sleep disorder claim 1 , wherein said medicament comprises at least one of albiflorin claim 1 , a metabolite of albiflorin claim 1 , a composition of albiflorin claim 1 , a herb comprising albiflorin or a herb extract comprising albiflorin.7. The medicament according to claim 6 , wherein said metabolite of albiflorin is paeonilactone A claim 6 , or paeonilactone B.8. The medicament according to claim 6 , wherein the content of albiflorin in said herb extract comprising albiflorin is between 6% and 100% by weight.9. The medicament according to claim 6 , wherein said ...

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05-12-2013 дата публикации

5'-END DERIVATIVES

Номер: US20130323836A1
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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12-12-2013 дата публикации

Synergistic Combinations of Polyene Fungicides and Non-Ribosomal Peptides and Related Methods of Use

Номер: US20130331311A1
Принадлежит: BAYER CROPSCIENCE LP

The present invention includes compositions comprising a synergistic fungicidal combination of a polyene fungicide and at least one lipopeptide and methods for using such compositions in controlling fungal pathogens. 1. A composition comprising a synergistic fungicidal combination of a polyene fungicide and at least one lipopeptide , wherein the polyene fungicide is natamycin or a derivative of natamycin and wherein the weight to weight ratio of the polyene fungicide and the at least one lipopeptide is from about 500:1 to about 1:500.2. A method for controlling fungal pathogens comprising applying to a locus in need of treatment an effective amount of the composition of . This application claims priority to and is a continuation of U.S. patent application Ser. No. 13/478,989, filed May 23, 2012, which in turn claims priority to U.S. Provisional Application No. 61/615,075, filed on Mar. 23, 2012, and U.S. Provisional Application No. 61/489,640, filed on May 24, 2011. The contents of the aforementioned patent applications are hereby incorporated by reference into the present disclosure.The present invention relates to synergistic combinations of polyene fungicides with antibiotic non-ribosomal peptides, such as amphiphilic cyclic lipopeptides, to improve the fungicidal activity of both components.Fungicides have myriad uses, including for crop protection; as food, feed, and cosmetics preservatives; and as pharmaceuticals for both human and veterinary applications. Crop yield reduction, food-borne diseases and fungal infections of both humans and animals are a problem in both developed and developing countries. Therefore, improvements to the efficacy of existing fungicides, especially those that are environmentally friendly and are not susceptible to development of fungal resistance are highly desirable.Polyene fungicides are antifungal antibiotics that have been used in all of the aforementioned fields. They may be obtained through fermentation of species, such as , ...

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12-12-2013 дата публикации

PUERARIN HYDRATES, PREPARATION METHODS AND USES THEREOF

Номер: US20130331345A1
Автор: Liu Li
Принадлежит:

The present invention pertains to the field of pharmaceutical and chemical engineering, and relates to a puerarin hydrate, the preparation method and use thereof. Specifically, said puerarin hydrate has a molecular formula of CHO.n HO, in which n is a value of 0.8-1.3. The present invention further relates to a pharmaceutical composition comprising said puerarin hydrate, and a method for the treatment of cardiovascular diseases or eye diseases. The puerarin hydrate of the present invention is more stable than puerarin without water of crystallization, convenient for storage and transportation, and has good fluidity at room temperature thereby easy for the manufacture of preparations. 1. A puerarin hydrate , of which the molecular formula is CHO.n HO , wherein n is a value selected from 0.4-1.3 or 0.8-1.3.2. The puerarin hydrate according to claim 1 , wherein n is 0.5 claim 1 , 0.8 claim 1 , 0.85 claim 1 , 1 claim 1 , 1.05 claim 1 , 1.2 claim 1 , 1.25 or 1.3.3. A method for preparing the puerarin hydrate of or claim 1 , which is any one of the following methods A to E:Method A:{'i': 'Puerariae', 'In a reaction container, subjecting Radix powder to cold extraction, ultrasonic extraction, microwave extraction or refluxing extraction one or more times with one or more of water or C1-C6 lower alcohols, combining, filtering, filtering with microporous membrane or ceramic membrane, concentrating filtrate, concentrating to obtain Radix Puerariae extractum, adding water, adjusting pH to 3-5 with an acid, then adjusting pH to 6-9 with one or more of a base or sodium carbonate or sodium hydrogen carbonate, filtering, then extracting with one or more solvents of C3-C6 lower alcohols or C3-C8 lower ketones, such as hexone, or C2-C8 lower esters, drying by evaporation to obtain a solid, adding water, then extracting with one or more solvents of C3-C6 lower alcohols or C3-C8 lower ketones, such as hexone, or C2-C8 lower esters, concentrating, standing, filtering, performing ...

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12-12-2013 дата публикации

Treatment of Clostridium Difficile Infection in Patients Undergoing Antibiotic Therapy

Номер: US20130331347A1
Принадлежит: OPTIMER PHARMACEUTICALS, INC.

The present invention relates to methods of treating infection in a subject receiving antibiotic therapy for a different infection comprising administering to the subject an effective amount of the compounds described herein. 2. The method of wherein the different infection is due to a bacterium claim 1 , fungus or protozoan.3. The method of wherein the different infection is due to a gram-positive bacterium.4. The method of wherein the different infection is due to a gram-negative bacterium.5. The method of wherein the antibiotic therapy for treatment of a different infection comprises administration of an antibiotic selected from the group consisting of aminoglycosides claim 1 , ansamycins claim 1 , carbacephems claim 1 , carbapenems claim 1 , cephalosporins claim 1 , glycopeptides claim 1 , lincosamides claim 1 , macrolides claim 1 , monobactams claim 1 , penicillins claim 1 , polypeptides claim 1 , quinolones claim 1 , rifamycins claim 1 , sulfonamides and tetracyclines.6. The method of wherein the aminoglycoside antibiotic is selected from the group consisting of amikacin claim 5 , gentamycin claim 5 , kanamycin claim 5 , neomycin claim 5 , netilmicin claim 5 , streptomycin claim 5 , tobramycin and paromomycin.7. The method of wherein the ansamycin antibiotic is selected from the group consisting of geldanamycin and herbimycin.8. The method of wherein the carbapenem antibiotic is selected from the group consisting of ertapenem claim 5 , doripenem claim 5 , imipenem/cilastatin and meropenem.9. The method of wherein the cephalosporin antibiotic is selected from the group consisting of cefadroxil claim 5 , cefazolin claim 5 , cefalotin claim 5 , cefalexin claim 5 , cefaclor claim 5 , cefamandole claim 5 , cefoxitin claim 5 , cefprozil claim 5 , cefuroxime claim 5 , cefiximie claim 5 , cefdinir claim 5 , cefditoren claim 5 , cefoperazone claim 5 , cefotaxime claim 5 , cefpodoxime claim 5 , ceftazidime claim 5 , ceftibuten claim 5 , ceftizoxime claim 5 , ceftriaxone ...

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19-12-2013 дата публикации

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

Номер: US20130338090A1
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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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
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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26-12-2013 дата публикации

COMPOSITION FOR PROMOTING HEMATOGENESIS CONTAINING QUERCETIN 3-O-beta-(2''-GALLOYL)-RHAMNOPYRANOSIDE AS ACTIVE INGREDIENT

Номер: US20130345158A1

This invention relates to a composition for promoting hematopoiesis and for treating, preventing or alleviating cytopenia or bone marrow failure comprising quercetin 3-O-β-(2″-galloyl)-rhamnopyranoside (QGR) as active ingredient. The present active compound QGR (i) increases dose dependently the mRNA expression of cytokines involved in hematopoiesis including stem cell factor, granulocyte-macrophage colony stimulating factor and erythropoietin from mouse bone marrow mononuclear cells, (ii) promotes the formation of burst forming unit-erythroid and colony forming unit-fibroblast, (iii) stimulates the generation of cells positive for TER-119, a specific marker of mouse erythroid precursors, (iv) promotes erythropoiesis, leukopoiesis, thrombopoiesis, and hemoglobin production in bone marrow failure mouse model, (v) stimulates the formation of hematopoietic stem/progenitor cells and mesenchymal stem/progenitor cells, (vi) stimulates megakaryocyte formation surrounding the blood system of damaged bone marrow, osteoid formation and bone marrow restoration through a recovery of damaged bone marrow microenvironment. The QGR of the present invention can be used for promoting hematopoiesis and treating cytopenia or bone marrow failure. 111-. (canceled)13. The method according to claim 12 , wherein the promoting of hematopoiesis is a process of promoting hematopoiesis from hematopoietic stem cells.14. The method according to claim 13 , wherein the hematopoiesis is erythropoiesis claim 13 , leukopoiesis claim 13 , or thrombopoiesis.16. The method according to claim 15 , wherein the cytopenia is erythropenia claim 15 , leukopenia claim 15 , granulocytopenia claim 15 , neutropenia claim 15 , thrombocytopenia claim 15 , pancytopenia claim 15 , anemia claim 15 , aplastic anemia claim 15 , myelodysplasia claim 15 , or chemotherapy-induced cytopenia.18. The method according to claim 17 , wherein the quercetin 3-O-β-(2″-galloyl)-rhamnopyranoside stimulates a megakaryocyte formation ...

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26-12-2013 дата публикации

Novel antibacterial agents

Номер: US20130345410A1
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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02-01-2014 дата публикации

KETOLIDE COMPOUNDS

Номер: US20140005133A1
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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02-01-2014 дата публикации

Method of extracting kaempferol-based antioxidants from solenostemma arghel

Номер: US20140005373A1
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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09-01-2014 дата публикации

NOVEL MACROLIDE DERIVATIVE

Номер: US20140011757A1
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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30-01-2014 дата публикации

SINGLE DOSE ORAL FORMULATIONS AND METHODS FOR TREATMENT OF CATS WITH ECTOPARASITICIDAL SPINOSAD

Номер: US20140031306A1
Принадлежит:

This invention provides a single-dose oral formulation of spinosad for the extended control of a infestation on a cat at a predictable dose of spinosad that is suitable for administration once every 30 days (i.e., one month). The invention also provides methods of using the formulation of spinosad. 1C. felis. A single-dose oral formulation for controlling a infestation on a cat comprising an ectoparasiticidal amount of spinosad , microcrystalline cellulose , hydroxypropylcellulose , colloidal silicon (anhydrous) , croscarmellose sodium , and magnesium stearate , and optionally an artificial flavor , wherein the formulation is suitable for oral administration once every 30 days at a dose of at least about 50 mg of spinosad per kg of body weight of the cat.2. The formulation of claim 1 , wherein the dose is at least about 75 mg of spinosad per kg of body weight of the cat.3. The formulation of claim 1 , wherein the dose is at least about 100 mg of spinosad per kg of body weight of the cat.6. The formulation of claim 1 , wherein the formulation has greater than 75% residual efficacy at 30 days post-administration.7. The formulation of claim 1 , wherein the formulation has greater than 90% residual efficacy at 30 days post-administration.8. The formulation of claim 1 , wherein the formulation has greater than 95% residual efficacy at 30 days post-administration.9. The formulation of claim 1 , wherein the formulation is a tablet or capsule.10C. felis. A method of controlling a infestation on a cat claim 1 , the method comprising orally administering a single-dose oral formulation comprising an ectoparasiticidal amount of spinosad claim 1 , microcrystalline cellulose claim 1 , hydroxypropylcellulose claim 1 , colloidal silicon (anhydrous) claim 1 , croscarmellose sodium claim 1 , and magnesium stearate claim 1 , and optionally an artificial flavor claim 1 , wherein the formulation is suitable for oral administration once every 30 days at a dose of at least about 50 mg of ...

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30-01-2014 дата публикации

ANTI-INFLAMMATORY MACROLIDES

Номер: US20140031307A1
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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30-01-2014 дата публикации

COMPOUNDS

Номер: US20140031534A1
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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30-01-2014 дата публикации

NOVEL GLYCOSYLTRANSFERASE GENE AND USE THEREOF

Номер: US20140033369A1
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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06-02-2014 дата публикации

LUTEOLIN AND DIOSMIN/DIOSMETIN AS NOVEL STAT3 INHIBITORS FOR TREATING AUTISM

Номер: US20140038913A1
Автор: LUO Deyan, Tan Jun
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

The present invention includes methods for the treatment of autoimmune disorders such as autism, schizophrenia, and type 1 diabetes. Flavonoids, luteolin, diosmin, and diosmin's aglycone form, diosmetin, were found to inhibit activation/phosphorylation of STAT3 induced by IL-6 in cultured neuronal cells. Furthermore, mice treated with diosmin showed a significant reduction of autistic phenotype induced by IL-6 through inhibition of STAT3 activation. 1. A method of reducing the risk of developing autism in a patient due to exposure of the patient in utero to elevated levels of IL-6 from the patient's mother comprising:inhibiting activation of STAT3 in both the patient and the patient's mother by administering a therapeutically effective amount of a flavonoid selected from the group consisting of luteolin, diosmin, and diosmetin to the patient's mother during pregnancy;wherein STAT3 in the patient and the patient's mother is activated by elevated levels of IL-6 from the patient's mother.2. The method of claim 1 , wherein the flavonoid is administered orally.3. The method of claim 1 , wherein the flavonoid is administered at a dosage of between about 0.81 mg/kg/day and about 2.5 mg/kg/day4. The method of claim 1 , wherein the patient's mother suffered from an infection which resulted in maternal immune activation of IL-6 while pregnant.5. The method of claim 3 , wherein the flavonoid is diosmin.6. A method of treating autism in a patient in utero comprising:obtaining levels of IL-6 in a mother of the patient;comparing the levels of IL-6 from the mother to a control level wherein an elevated level of IL-6 from the mother as compared to the control level is indicative of STAT3 activation; andinhibiting the activation of STAT3 by administering a therapeutically effective amount of a flavonoid selected from the group consisting of luteolin, diosmin, and diosmetin to the mother;wherein inhibiting STAT3 activation in the mother also inhibits STAT3 activation in the patient.7 ...

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06-02-2014 дата публикации

NOVEL MACROLIDE INTERMEDIATE AND NOVEL PRODUCTION PROCESS

Номер: US20140039171A1
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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13-02-2014 дата публикации

C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE

Номер: US20140046043A1
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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06-03-2014 дата публикации

Purification of biological conjugates by size exclusion chromatography

Номер: US20140066605A1
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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13-03-2014 дата публикации

Process for preparation of ketolide intermediates

Номер: US20140073770A1
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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20-03-2014 дата публикации

IDENTIFICATION OF FREE-B-RING FLAVONOIDS AS POTENT COX-2 INHIBITORS

Номер: US20140080774A1
Принадлежит: Unigen, Inc.

The present invention provides a novel method for inhibiting the cyclooxygenase enzyme COX-2. The method is comprised of administering a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 mediated diseases and conditions. The method for preventing and treating COX-2 mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids and a pharmaceutically acceptable carrier. 111.-. (canceled)12Scutellaria. A method for reducing joint dysfunction , comprising administering to a human or animal having joint pain , joint stiffness , or impaired physical function due to joint dysfunction a therapeutically effective amount of a extract enriched for a Free-B-Ring flavonoid or a mixture of Free-B-Ring flavonoids , wherein the method inhibits peroxidase activity which reduces joint dysfunction in the human or animal.14ScutellariaScutellaria baicalensislaterifloraorthocalyx.. The method according to claim 12 , wherein the is claim 12 , Scutellariae claim 12 , Scutellariae radix claim 12 , or Scutellariae15Scutellaria. The method according to claim 12 , wherein the extract enriched for a Free-B-Ring flavonoid or mixture of Free-B-Ring flavonoids is extracted from a plant part selected from stems claim 12 , stem barks claim 12 , twigs claim 12 , tubers claim 12 , roots claim 12 , root barks claim 12 , young shoots claim 12 , seeds claim 12 , rhizomes claim 12 , flowers claim 12 , leaves claim 12 , or other aerial parts.16. The method according to claim 12 , wherein the joint dysfunction is associated with systemic lupus erythematosis claim 12 , rheumatoid arthritis claim 12 , or osteoarthritis.17Scutellaria. The method according to claim 12 , wherein the ...

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20-03-2014 дата публикации

USE OF SECNIDAZOLE IN TREATMENT OF DENTAL INFECTIONS

Номер: US20140080778A1
Автор: Defrance Pierre-Marie
Принадлежит: MADECA

The invention relates to the combination of secnidazole with an antibiotic of the macrolide family, preferably azithromycin 11, for oral treatment of dental infections, which enables a considerable reduction in the length of treatment and the doses administered in comparison with the conventional treatment. 1. Composition for use in the treatment by oral route of dental infections , containing secnidazole in association with an antibiotic of the macrolide family , the secnidazole and the antibiotic being associated in a single medicine or presented as a pair of medicines.2. Composition according to claim 1 , characterized in that the antibiotic is selected between spiramycine and azithromycine.3. Pharmaceutical form for oral administration claim 1 , containing the composition according to or claim 1 , administrable as a single intake and containing from 1500 mg to 2500 mg claim 1 , preferably approximately 2000 mg claim 1 , of secnidazole and a pharmaceutically acceptable excipient or diluent.4. Pharmaceutical form according to claim 3 , characterized in that it contains claim 3 , in addition claim 3 , approximately 750 mg to 1500 mg claim 3 , preferably approximately 1000 mg of azithromycine.5. Composition according to or claim 3 , packed as a single medicine or two medicines claim 3 , containing claim 3 ,in the first case, a pharmaceutical form for oral administration, containing from 1500 mg to 2500 mg, preferably 2000 mg, of secnidazole, and from 750 mg to 1500 mg, preferably 1000 mg, azithromycine, and a pharmaceutically acceptable excipient or diluent, orin the second case, on one hand, a pharmaceutical form for oral administration, containing from 1500 mg to 2500 mg, preferably 2000 mg of secnidazole, and a pharmaceutically acceptable excipient or diluent and, on another hand, either one unit of a pharmaceutical form, adapted to oral administration and containing 1000 mg azithromycine and a pharmaceutically acceptable excipient or diluent, or two units of a ...

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27-03-2014 дата публикации

Esters and Malonates of SATE Prodrugs

Номер: US20140086873A1
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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27-03-2014 дата публикации

PHARMACEUTICAL COMPOSITION COMPRISING AN SGLT2 INHIBITOR AND A PPAR- GAMMA AGONIST AND USES THEREOF

Номер: US20140088027A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to a pharmaceutical composition comprising an SGLT2 inhibitor and a PPARγ agonist which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions. 1. A pharmaceutical composition comprising:(a) an SGLT2 inhibitor, and(b) a PPARγ agonist.2. The pharmaceutical composition according to claim 1 , wherein said PPARγ agonist is a thiazolidindione claim 1 , or a pharmaceutically acceptable salt thereof.3. The pharmaceutical composition according to claim 1 , wherein said thiazolidindione is pioglitazone or rosiglitazone claim 1 , or a pharmaceutically acceptable salt thereof.5. The pharmaceutical composition according to claim 1 , wherein the composition is suitable for combined or simultaneous or sequential use of the SGLT2 inhibitor and the PPARγ agonist.6. Method for preventing claim 1 , slowing the progression of claim 1 , delaying or treating a metabolic disorder selected from the group consisting of type 1 diabetes mellitus claim 1 , type 2 diabetes mellitus claim 1 , impaired glucose tolerance claim 1 , impaired fasting blood glucose claim 1 , hyperglycemia claim 1 , postprandial hyperglycemia claim 1 , overweight claim 1 , obesity claim 1 , metabolic syndrome claim 1 , gestational diabetes claim 1 , new onset diabetes after transplantation (NODAT) and complications associated therewith claim 1 , and post-transplant metabolic syndrome (PTMS) and complications associated therewith in a patient in need thereof characterized in that an SGLT2 inhibitor and a PPARγ agonist according to are administered in combination or alternation to the patient.7. Method for improving glycemic control and/or for reducing of fasting plasma glucose claim 1 , of postprandial plasma glucose and/or of glycosylated hemoglobin ...

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27-03-2014 дата публикации

Triazole Compounds and Methods of Making and Using the Same

Номер: US20140088031A1
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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27-03-2014 дата публикации

METHOD OF EXTRACTING PHENOLIC FRACTIONS OF EXTRA VIRGIN OLIVE OIL

Номер: US20140088299A1
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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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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10-04-2014 дата публикации

TOPICAL PHARMACEUTICAL COMPOSITION CONTAINING A WATER-SENSITIVE ACTIVE PRINCIPLE

Номер: US20140100181A1
Принадлежит: GALDERMA S.A.

A topical pharmaceutical composition including, as a pharmaceutical active agent, a water-sensitive compound in a solubilised form in a physiologically acceptable medium is described. A method for preparing such a composition, and uses thereof in dermatology are also described. 1. A pharmaceutical composition in the form of an oil-in-water emulsion , the composition comprising: a lipophilic solvent/oily phase for the active agent, said active agent being dissolved in and chemically stable in the oily phase,', 'at least one polyol selected from the group consisting of trihydric alcohols, tetrahydric alcohols and hexahydric alcohols,', 'at least 5% water,, 'at least one water-sensitive active agent selected from the group consisting of a macrocyclic lactone and a phenolic derivative, the active agent being in a dissolved form and chemically stable in the oily phase,'}wherein the composition is topical and comprises at least one surfactant selected from the group consisting of a sucroester and a polyglycerol ester.25-. (canceled)6. The composition according to claim 1 , wherein the macrocyclic lactone is ivermectin.7. The composition according to claim 1 , wherein the phenolic derivative is rucinol or hydroquinone.8. The composition according to claim 1 , further comprising at least one gelling agent.9. The composition according to claim 8 , wherein the gelling agent is selected from the group consisting of an acrylamide claim 8 , a carbomer and a polysaccharide.10. The composition according to claim 1 , wherein the lipophilic solvent/oily phase for the active agent comprises at least one fatty substance selected from the group consisting of a capric/caprylic triglyceride and a mineral oil.11. The composition according to claim 1 , wherein the sucroester is selected from the group consisting of sucrose stearate claim 1 , sucrose laurate claim 1 , sucrose palmitate claim 1 , and mixtures thereof.12. The composition according to claim 1 , wherein the polyol is glycerol. ...

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07-01-2016 дата публикации

PHARMACEUTICAL COMPOSITION, METHODS FOR TREATING AND USES THEREOF

Номер: US20160000816A1
Принадлежит:

The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing oxidative stress, for example in patients with type 1 or type 2 diabetes, as well as to the use of such SGLT-2 inhibitors in treatment and/or prevention of cardiovascular diseases in patients, for example type 1 or type 2 diabetes patients. The present invention further relates to certain SGLT-2 inhibitors for treating and/or preventing a metabolic disorder and preventing, reducing the risk of or delaying the occurrence of a cardiovascular event in patients, for example patients with type 1 or type 2 diabetes. 1. A method to reduce the risk of cardiovascular death in a patient with type 2 diabetes mellitus , said method comprising administering empagliflozin to the patient.2. The method according to claim 1 , wherein said patient has or is at risk of a cardiovascular disease.3. The method according to claim 1 , wherein empagliflozin is administered orally in a total daily amount of 10 mg or 25 mg.4. A method to reduce the risk of hospitalization for heart failure in a patient with type 2 diabetes mellitus claim 1 , said method comprising administering empagliflozin to the patient.5. The method according to claim 4 , wherein said patient has or is at risk of a cardiovascular disease.6. The method according to claim 4 , wherein empagliflozin is administered orally in a total daily amount of 10 mg or 25 mg.7. A method to reduce the risk of all-cause mortality in a patient with type 2 diabetes mellitus claim 4 , said method comprising administering empagliflozin to the patient.8. The method according to claim 7 , wherein said patient has or is at risk of a cardiovascular disease.9. The method according to claim 7 , wherein empagliflozin is administered orally in a total daily amount of 10 mg or 25 mg.10. A method to reduce the risk of all-cause mortality by reducing cardiovascular death in a patient with type 2 diabetes mellitus claim 7 , said method comprising administering ...

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06-01-2022 дата публикации

SCUTELLARIN AMIDE DERIVATIVES, AND PREPARATION METHODS AND USES THEREOF

Номер: US20220002332A1

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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02-01-2020 дата публикации

POLYPHENOL GLYCOSIDE-CONTAINING COMPOSITION

Номер: US20200000834A1
Принадлежит: SUNSTAR INC.

The present invention provides a method of efficiently promoting AMPK and/or ACC phosphorylation. Specifically, the present invention provides a composition comprising trifolin and astragalin, wherein the content mass ratio of trifolin and astragalin is 1:0.2 to 3. 1. A composition comprising trifolin and astragalin , wherein the content mass ratio of trifolin and astragalin is 1:0.2 to 3.2. The composition according to claim 1 , wherein the content mass ratio of trifolin and astragalin is 1:0.5 to 2.3. The composition according to claim 1 , further comprising hyperoside and/or isoquercitrin.4. The composition according to for use in foods claim 1 , quasi-drugs claim 1 , or drugs.5. A method of activating AMP-activated protein kinase in a skeletal muscle cell claim 1 , comprising administering the composition according to to a subject in need of sugar metabolism improvement.6. A method of inactivating acetyl-CoA carboxylase in a skeletal muscle cell claim 1 , comprising administering a required amount of the composition according to to a subject in need of sugar metabolism improvement.7. A method of reducing blood sugar levels claim 1 , comprising administering a required amount of the composition according to to a subject in need of reduction in blood sugar levels.8. A method of reducing blood sugar levels claim 2 , comprising administering a required amount of the composition according to to a subject in need of reduction in blood sugar levels.9. A method of reducing blood sugar levels claim 3 , comprising administering a required amount of the composition according to to a subject in need of reduction in blood sugar levels. The present invention relates to a composition comprising polyphenol glycoside (in particular, trifolin and astragalin) etc.AMP-activated protein kinase (AMPK) is one of the serine/threonine kinases (serine/threonine phosphoenzymes) that are highly conserved in eukaryotic cells, and plays an important role as an intracellular energy sensor. ...

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07-01-2016 дата публикации

Pharmaceutical Compositions for Rectal Administration

Номер: US20160002278A1
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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02-01-2020 дата публикации

FLUOROGENIC GLYCOSIDASE SUBSTRATE AND ASSOCIATED DETECTION METHOD

Номер: US20200002367A1
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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02-01-2020 дата публикации

Amphotericin b derivatives with improved therapeutic index

Номер: US20200002368A1
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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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
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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12-01-2017 дата публикации

TREATMENT OF NEURODEGENERATIVE AND NEURODEVELOPMENTAL DISEASES BY INHIBITION OF THE a2-Na/K ATPase/a-ADDUCIN COMPLEX

Номер: US20170007633A1
Принадлежит:

Described herein are methods for the prevention of neurodegeneration and the treatment of neurodegenerative disease (Including amyotrophic lateral sclerosis) ami neurodevelopmental disorders through the administration of an agent that inhibits die a2-Na/K ATPase/a-Adducin Complex. 1. A method of treating a neurodegenerative disease or a neurodevelopmental disorder comprising administering to a subject an agent that inhibits α2-Na/K ATPase and/or α-Adducin.2. The method of claim 1 , wherein the disease is a neurodegenerative disease selected from the group consisting of amyotrophic lateral sclerosis (ALS) claim 1 , Huntington's disease claim 1 , spinocerebellar ataxias claim 1 , Alzheimer's disease claim 1 , traumatic brain injury and Parkinson's disease or a neurodevelopmental disorder selected from the group consisting of fragile X syndrome claim 1 , Down's syndrome claim 1 , Rett syndrome claim 1 , intellectual disability claim 1 , autism claim 1 , an autism spectrum disorder and Asperger syndrome.3. The method of claim 2 , wherein the neurodegenerative disease is ALS.4. The method of claim 1 , wherein the agent is selected from the group consisting of a small molecule claim 1 , an interfering nucleic acid molecule specific for α2-Na/K ATPase claim 1 , an antibody that binds to α2-Na/K ATPase claim 1 , an isolated soluble polypeptide comprising at least 5 consecutive amino acids of the amino acid sequence encoding α-Adducin claim 1 , an interfering nucleic acid molecule specific for α-Adducin claim 1 , and an isolated soluble polypeptide comprising at least 5 consecutive amino acids of the amino acid sequence encoding α2-Na/K ATPase.5. The method of wherein the small molecule is a cardiac glycoside.6. The method of claim 5 , wherein the small molecule is selected from the group consisting of digoxin claim 5 , ouabain claim 5 , digitoxin claim 5 , proscillaridin A claim 5 , digoxigenin claim 5 , gitoxin claim 5 , gitoxigenin claim 5 , oleandrin claim 5 , butalin ...

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14-01-2016 дата публикации

PHARMACEUTICAL COMPOSITIONS FOR INHIBITING ANGIOGENESIS

Номер: US20160008319A1

The disclosure provides a pharmaceutical composition for inhibiting angiogenesis, including an effective amount of a lignan as an effective ingredient. The pharmaceutical composition may further include a pharmaceutically acceptable carrier or salt. The disclosure also provides a method for inhibiting angiogenesis, including administering an effective amount of a lignan as an effective ingredient for inhibiting angiogenesis to a subject in need thereof. 2. The pharmaceutical composition for inhibiting angiogenesis as claimed in claim 1 , wherein the lignin comprises yatein claim 1 , 5′-desmethoxyyatein (bursehernin) claim 1 , 7′ claim 1 , 7′-dihydroxy bursehernin claim 1 , 5 ′-methoxyyatein claim 1 , podorhizol or podorhizol 4′-o-β-D-glucopyranoside.3. The pharmaceutical composition for inhibiting angiogenesis as claimed in claim 1 , further comprising a pharmaceutically acceptable carrier or salt. This application is a Divisional of U.S. patent application Ser. No. 14/133,213 filed on Dec. 18, 2013, which claims priority under 35 U.S.C. §119(a) to Patent Application No. 101148230 filed in Taiwan on Dec. 19, 2012, all of which are hereby expressly incorporated by reference into the present application.The technical field relates to pharmaceutical compositions and method for inhibiting angiogenesis.Angiogenesis means a process for forming a new blood vessel near a pre-existing blood vessel. Under a normal physiological mechanism, during the process of a response which can result from a stimulation of signal transduction for angiogenesis, such as wound healing or the menstrual cycle of women, a controlled angiogenesis will occur and be maintained for about 1-2 weeks. However, pathological angiogenesis is not controlled by a normal physiological mechanism. Regulation of angiogenesis plays a very important balancing role in the human body. Under a strong angiogenesis effect, it may result in diabetic retinopathy, rheumatoid arthritis, or may accelerate aggravation or ...

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08-01-2015 дата публикации

Low Dose Topiramate/Phentermine Composition and Methods of Use Thereof

Номер: US20150010625A1
Принадлежит:

A method for effecting weight loss by administering a combination of topiramate and phentermine is provided. The phentermine is generally administered in immediate release form, in a daily dose in the range of 2 mg to 8 mg, in combination with a daily dose of topiramate selected to prevent the loss of effectiveness of phentermine alone. Methods for treating obesity, conditions associated with obesity, and other indications are also provided, as are compositions and dosage forms containing low doses of phentermine and topiramate, e.g., 3.75 mg phentermine and 23 mg topiramate. 1. A method for effecting weight loss in a subject , comprising administering to the subject continually over a significant period of time a daily dose of phentermine in the range of 2 mg to 8 mg and in combination therewith a daily dose of topiramate selected to prevent the loss of effectiveness of phentermine alone.2. The method of claim 1 , wherein the daily dose of phentermine is in the range of 2 mg to 5 mg.3. The method of claim 1 , wherein the dose of topiramate is in the range of 15 mg to 50 mg.4. The method of claim 3 , wherein the dose of topiramate is in the range of 15 mg to 25 mg.5. The method of claim 4 , wherein the dose of topiramate is in the range of 17 mg to 23 mg.6. A method for effecting weight loss in a subject claim 4 , comprising administering to the subject claim 4 , on a daily basis claim 4 , 3.75 mg phentermine and 23 mg topiramate.7. A method for effecting weight loss in a subject claim 4 , comprising administering to the subject claim 4 , on a daily basis claim 4 , 7.5 mg phentermine and 46 mg topiramate.8. The method of claim 1 , wherein the phentermine and the topiramate are administered orally.9. The method of claim 8 , wherein the phentermine and the topiramate are administered at different times of day.10. The method of claim 9 , wherein the phentermine is administered in the morning and the topiramate is administered in the afternoon or evening.11. The method ...

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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
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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08-01-2015 дата публикации

TREATMENT OF PAPULOPUSTULAR ROSACEA WITH IVERMECTIN

Номер: US20150011491A1
Автор: JACOVELLA Jean
Принадлежит: GALDERMA S.A.

Methods and compositions for safe and effective treatment of papulopustular rosacea in a subject are described. The methods involve topically applying to an affected skin area a topical composition containing ivermectin and a pharmaceutically acceptable carrier. Treatment with ivermectin represents an innovative therapy that is more robust and effective than the conventional treatments. 1. A method of treating papulopustular rosacea in a subject in need thereof , comprising topically administering , once daily , to a skin area affected by the papulopustular rosacea a therapeutically effective amount of a pharmaceutical composition comprising about 0.1% to about 1% by weight ivermectin and a pharmaceutically acceptable carrier to thereby obtain a significant reduction in inflammatory lesion count in the subject , wherein the subject has moderate to severe papulopustular rosacea before the treatment.2. (canceled)3. The method of claim 1 , wherein the subject has 15 or more inflammatory lesions of the papulopustular rosacea before the treatment.4. The method of claim 1 , wherein as early as 2 weeks after the initial administration of the pharmaceutical composition claim 1 , the significant reduction in inflammatory lesion count is observed.5. (canceled)6. The method of claim 1 , wherein the pharmaceutical composition comprises about 0.5% to about 1% by weight ivermectin.7. The method of claim 6 , wherein the pharmaceutical composition comprises about 1% by weight ivermectin.8. The method of claim 6 , wherein the pharmaceutically acceptable carrier comprises one or more ingredients selected from the group consisting of: an oily phase comprising one or more selected from the group consisting of dimethicone claim 6 , cyclomethicone claim 6 , isopropyl palmitate claim 6 , isopropyl myristate claim 6 , and a fatty substance selected from the group consisting of cetyl alcohol claim 6 , cetostearyl alcohol claim 6 , stearyl alcohol claim 6 , palmitostearic acid claim 6 , ...

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11-01-2018 дата публикации

CRYSTAL STRUCTURE OF THE LARGE RIBOSOMAL SUBUNIT FROM S. AUREUS

Номер: US20180009853A1
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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14-01-2021 дата публикации

AMINOCOUMARIN COMPOUNDS AND METHODS OF THEIR USE

Номер: US20210009621A1
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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09-01-2020 дата публикации

NOVEL IMMUNE STIMULATING COMPOUND

Номер: US20200010499A1
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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19-01-2017 дата публикации

FLAVONOID COMPOSITIONS AND USES THEREOF

Номер: US20170014439A1
Принадлежит:

This invention relates to a flavonoid composition that includes eriocitrin. The flavonoid may be included in a complex with other bioflavonoids. The composition may also include neoeriocitrin. This invention also relates to methods of using the composition, including for reducing IL-6 or MCP-1 levels, treating inflammation, and treating symptoms of metabolic syndrome. 1. A composition comprising at least 10% wt/wt eriocitrin.2. The composition of claim 1 , wherein the composition comprises at least 50% wt/wt eriocitrin.3. The composition of claim 1 , wherein the composition comprises at least 0.1% wt/wt of a second flavonoid.4. The composition of claim 3 , wherein the second flavonoid is selected from the group consisting of neoeriocitrin claim 3 , eriodictyol claim 3 , hesperidin claim 3 , and eriodictyol glucoside.5. The composition of claim 4 , wherein the second flavonoid is neoeriocitrin.6. The composition of claim 5 , wherein the composition comprises at least 0.2% neoerioctrin.7. The composition of claim 5 , wherein the composition further comprises eriodictyol and hesperidin.8. The composition of claim 5 , further comprising a polymethoxylated flavone claim 5 , naringen claim 5 , naringenin claim 5 , an omega-3 fatty acid claim 5 , coenzyme Q10 claim 5 , or a green tea extract.9. The composition of claim 8 , wherein the polymethoxylated flavone comprises a hydroxylated polymethoxylated flavone.10. A method for treating inflammation claim 8 , comprising administering a composition comprising eriocitrin and neoeriocitrin to a subject in need thereof.11. A method for treating a disease or condition associated with elevated IL-6 levels claim 8 , comprising administering a composition comprising eriocitrin and neoeriocitrin to a subject in need thereof claim 8 , wherein the IL-6 levels in the subject are elevated relative to a healthy subject.12. The method of claim 11 , wherein the disease or condition is selected from the group consisting of autoimmune disease ...

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21-01-2016 дата публикации

FLAVOR COMPOSITION CONTAINING HMG GLUCOSIDES

Номер: US20160015063A1
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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18-01-2018 дата публикации

RESTORING PHYSIOLOGY WITH SMALL MOLECULE MIMICS OF MISSING PROTEINS

Номер: US20180015115A1
Принадлежит:

Disclosed are methods for treating a disease or condition characterized by decreased expression or reduced function of an ion channel, comprising administering to a subject in need thereof a therapeutically effective amount of a pore-forming polyene macrolide or pore-forming derivative thereof. For example, the pore-forming polyene macrolide may be amphotericin B (AmB), nystatin, or natamycin. The methods can be used to treat cystic fibrosis. 1. A method of treating a disease or condition characterized by decreased expression or reduced function of an ion channel , comprising administering to a subject in need thereof a therapeutically effective amount of a pore-forming polyene macrolide or pore-forming derivative thereof , thereby treating the disease or condition characterized by decreased expression or reduced function of the ion channel.2. The method of claim 1 , wherein the disease or condition characterized by decreased expression or reduced function of an ion channel is selected from the group consisting of cystic fibrosis claim 1 , hyperkalemic periodic paralysis claim 1 , paramyotonia congenita claim 1 , potassium aggravated myotonia claim 1 , generalized epilepsy with febrile seizures plus (GEFS+) claim 1 , episodic ataxia claim 1 , familial hemiplegic migraine claim 1 , spinocerebellar ataxia type 13 claim 1 , long QT syndrome claim 1 , Brugada syndrome claim 1 , and mucolipidosis type IV.3. The method of claim 1 , wherein the disease or condition characterized by decreased expression or reduced function of an ion channel is cystic fibrosis.4. The method of claim 1 , wherein the subject is not receiving the pore-forming polyene macrolide or pore-forming derivative thereof to treat an infection.5. The method of claim 1 , wherein the polyene macrolide is selected from the group consisting of amphotericin B (AmB) claim 1 , nystatin claim 1 , natamycin claim 1 , candicidin claim 1 , and mepartricin claim 1 , and any combination thereof.6. The method of claim ...

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18-01-2018 дата публикации

PROCESS FOR THE PREPARATION OF DIOSMIN

Номер: US20180016292A1
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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18-01-2018 дата публикации

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

Номер: US20180016585A1

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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15-01-2015 дата публикации

PAEONIFLORIN PREPARATIONS AND USES THEREOF FOR FAT REDUCTION

Номер: US20150018906A1
Автор: Rabie Bakr
Принадлежит:

Disclosed are methods and preparations useful for reducing fat at a targeted area(s) on a human. The preparations comprise as an active ingredient an adipolysis enhancing (i.e., fat-melting) amount of an active ingredient, paeoniflorin (PF). The preparations may be provided as an injectable preparation or as a topically applied preparation, such as in the form of a crème or lotion. In topical preparations, the active ingredient paeoniflorin may be contained within nanospheres, such as albumin nanospheres. The PF-containing preparations may also include a permeant, such as azone. The method may be accompanied by the application of ultrasound to the area being treated prior to, during or after, or prior to, during, and after application of the paeoniflorin preparation to an area of the body in which fat reduction is desired. By way of example, the methods and preparations are effective for reducing targeted fat deposits at various anatomical sites of the body, such as the midsection (“love handles”), jowls, hips, arms, thighs and buttocks area. 1. An adipolysis enhancing preparation comprising as an active ingredient an adipolysis enhancing amount of paeoniflorin , wherein glycerol release in a culture of Swiss 3T3 cells in the presence of the adipolysis enhancing amount of paeoniflorin is greater than glycerol release in the absence of the adipolysis enhancing amount of paeoniflorin.2. The adipolysis enhancing preparation of wherein the preparation comprises a creme or lotion.3. The adipolysis enhancing preparation of further comprising a permeant.4. The adipolysis enhancing preparation of comprising paeoniflorin containing albumin nanospheres.5. The adipolysis enhancing preparation of wherein the preparation comprises an injectable preparation.6. The adipolysis enhancing preparation of where the permeant is azone.7. The adipolysis enhancing preparation of comprising a concentration of paeoniflorin of about 0.25 mg/0.5 ml (0.50 mg/ml).8. The adipolysis enhancing ...

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