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

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Применить Всего найдено 22218. Отображено 200.
20-12-2008 дата публикации

КОМБИНАЦИИ, ВКЛЮЧАЮЩИЕ ПРОИЗВОДНЫЕ ЭПОТИЛОНА И АЛКИЛИРУЮЩИЕ АГЕНТЫ

Номер: RU2341260C2

Изобретение относится к фармацевтической комбинации, которая включает (а) алкилирующий агент и (б) производное эпотилона формулы I в которой А представляет собой О или NRN, где RN представляет собой водород или низший алкил, R представляет собой водород или низший алкил и Z представляет собой О или связь. Указанная комбинация может быть полезна для лечения пролиферативного заболевания, особенно опухолевого заболевания, и пролиферативное действие является большим по сравнению с максимальным действием, которое может быть достигнуто каждым из ингредиентов отдельно. 4 н. и 4 з.п. ф-лы.

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13-08-2018 дата публикации

ПИРАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ FSHR И ИХ ПРИМЕНЕНИЕ

Номер: RU2663898C2
Принадлежит: МЕРК ПАТЕНТ ГМБХ (DE)

Изобретение относится к соединению формулы I,или его фармацевтически приемлемой соли, также к фармацевтической композиции, способам лечения и модулирования, обусловленным воздействием на рецептор фолликулостимулирующего гормона. 7 н. и 12 з.п. ф-лы, 50 пр.

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15-04-2019 дата публикации

Применение производного бета-морфолинопропиоамидоксима в качестве противодиабетического средства

Номер: RU2684779C2

Изобретение относится к медицине, а именно к эндокринологии, и касается лечения диабета. Для этого вводят эффективное количество О-пара-толуоил-β-(морфолин-1-ил)пропиоамидоксима. Это обеспечивает эффективное гипогликемическое действие, превышающее гипогликемическое действие препарата сравнения - метформина в 1,2 раза. 1 табл.

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17-02-2020 дата публикации

Номер: RU2018114459A3
Автор:
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21-03-2019 дата публикации

Номер: RU2017122610A3
Автор:
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20-06-2013 дата публикации

МУЛЬТИВИТАМИННАЯ/МИНЕРАЛЬНАЯ КОМПОЗИЦИЯ ДЛЯ БОРЬБЫ С ЭФФЕКТАМИ ЭКОЛОГИЧЕСКОГО СТРЕССА, ПОВЫШЕНИЯ ИММУНИТЕТА И ПОВЫШЕНИЯ АКТИВНОСТИ, НАПРАВЛЕННАЯ НА НЕДОСТАТОЧНОСТИ ВИТАМИНОВ И МИНЕРАЛОВ БЕЗ НЕГАТИВНЫХ ПОБОЧНЫХ ЭФФЕКТОВ МЕГАДОЗОВОЙ ПИЩЕВОЙ ДОБАВКИ

Номер: RU2484824C2
Принадлежит: Вайет ЭлЭлСи (US)

Изобретение относится к фармацевтической промышленности и представляет собой витаминную добавку, содержащую витамин В1, витамин В2, никотиновую кислоту, витамин В6, биотин и пантотеновую кислоту; и где массовое отношение биотина к витамину В1 составляет от 1:20 до 1:25; где массовое отношение биотина к витамину В2 составляет от 1:25 до 1:30; где массовое отношение биотина к никотиновой кислоте составляет от 1:310 до 1:330; где массовое отношение биотина к витамину В6 составляет от 1:30 до 1:35; где массовое отношение биотина к пантотеновой кислоте составляет от 1:110 до 1:130. Изобретение обеспечивает повышение активности, снижение эффектов экологического стресса, улучшение иммунитета субъекта, уменьшение случаев продолжительности и серьезности простудных инфекций. 3 н. и 10 з.п. ф-лы, 1 пр.

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10-06-2006 дата публикации

КОМПОЗИЦИИ ДЛЯ СУПРЕССИИ ЭКСПРЕССИИ ССR5 И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Номер: RU2005139394A
Принадлежит:

... 1. Фармацевтическая композиция для уменьшения экспрессии поверхностных рецепторов CRR5 на мононуклеарных клетках, где композиция содержит терапевтически эффективное количество по меньшей мере одного соединения, блокирующего фазу G1. 2. Фармацевтическая композиция по п.1, дополнительно содержащая по меньшей мере одно противовирусное средство. 3. Фармацевтическая композиция по п.1, где соединение, блокирующее фазу G1, является представителем, выбранным из группы, включающей бутират натрия, афидиколин, гидроксимочевину (HU), оломуцин, росковитин, токоферолы и рапамицин (RAPA). 4. Фармацевтическая композиция по п.2, где противовирусное средство представляет собой противовирусное средство против ВИЧ. 5. Фармацевтическая композиция по п.4, где противовирусное средство против ВИЧ представляет собой ингибитор нуклеозида RT, ингибитор/антагонист CCR5, ингибитор вирусного вхождения и их функциональные эквиваленты. 6. Фармацевтическая композиция по п.2, где противовирусное средство представляет собой ...

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27-06-2008 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 1,4-ДИФЕНИЛАЗЕТИДИНОНА

Номер: RU2006145444A
Принадлежит:

... 1. Способ получения производных 1,4-дифенилазетидинона из подходящим образом защищенных β-замещенных аминоамидов в присутствии агентов силилирования и по меньшей мере одного катализатора циклизации, причем этот катализатор циклизации используют как катион одной из нижеследующих общих формул причем R16, R17, R18, R19 независимо друг от друга означают арил, (C1-C15)алкил, бензил, R41 означает арил, (C1-C15) алкил, бензил, R42 означает (C1-C15)алкил, бензил, (C5-C8)циклоалкил, арил, причем арил может быть замещен F, Cl, Br, I, -OH, -O(C1-C3)алкилом, -NH2, -NH(C1-C3)алкилом, -N[(C1-C3)алкил]2, -C(O)OH, -C(O)O(C1-C3)алкилом, -C(O)NH2, -C(O)NH(C1-C3)алкилом, -C(O)N[(C1-C3)алкил]2, -SO2NH2, -SO2 NH(C1-C3)алкилом, -SO2N[(C1-C3)алкил]2, -CN, (C1-C12)алкилом и (C5-C8)циклоалкилом, и как анион или или или и символы, заместители и индексы имеют следующие значения: Z = C=O, C=S, S=O, SO2 или C=NR20 K = O, S, NR21 или CR22R23 L = NR24 или CR25R26 n = 0 или 1 M = О, C=O, NR27 или CR28R29 Q = О, S, NR30 ...

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18-06-2020 дата публикации

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ПАРЕНТЕРАЛЬНОГО КАПЕЛЬНОГО ВВЕДЕНИЯ

Номер: RU2723950C1

Изобретение относится к области фармацевтической промышленности, а именно к фармацевтической композиции для парентерального капельного введения для применения при перенапряжении в условиях интенсивных нагрузок, характеризующейся тем, что содержит комплекс активных веществ при следующем соотношении компонентов, мг: флавинадениндинуклеотид натрия 40 мг; никотинамидадениндинуклеотидфосфат 500 мг; фолиевая кислота 15 мг; кальция фолинат пентагидрат 50 мг; цианокобаламин 1 мг; метилкобаламин 500 мкг; глутатион 600-1200 мг; α-липоевая (тиоктовая) кислота 50 мг; β-D-фруктозо-1,6-дифосфат 5000-10000 мг; N,N-диметилглицин 300 мг; аскорбиновая кислота 2000 мг; L-таурин 500 мг; L-карнитин 1000 мг; инозин 400 мг; магния аспарагинат 280 мг; калия аспарагинат 320 мг; кальция глюконат 500 мг; декстроза 5% до 500 мл. Изобретение обеспечивает создание высокоэффективной лекарственной формы, которая может быть использована при различных состояниях, связанных с физическими перегрузками и перенапряжением отдельных ...

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27-09-1996 дата публикации

ПРОИЗВОДНЫЕ АМИНОУКСУСНОЙ КИСЛОТЫ В ВИДЕ РАЦЕМАТА ИЛИ D- И L-ЭНАНТИОМЕРОВ И ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ, СПОСОБ ПОЛУЧЕНИЯ D- И L-ЭНАНТИОМЕРОВ ПРОИЗВОДНЫХ АМИНОУКСУСНОЙ КИСЛОТЫ ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ СОЛЕЙ И ПРОМЕЖУТОЧНЫЕ D- И L-ЭНАНТИОМЕРЫ АМИНОУКСУСНОЙ КИСЛОТЫ В ВИДЕ ЦИНХОНИДИНОВОЙ СОЛИ

Номер: RU94046047A
Принадлежит:

Объектом изобретения являются производные аминоуксусной кислоты формулы I, приведенной в описании, в виде рацемической смеси или энантиомера D или L и их фармацевтически приемлемые соли. Дальнейшим объектом изобретения является способ получения энантиомеров D и L производных аминоуксусной кислоты формулы I. Еще одним объектом изобретения являются энантиомеры D и L производных аминоуксусной кислоты формулы III, приведенной в описании, в виде цинхонидиновой соли, которые представляют собой промежуточные соединения для синтеза производных аминоуксусной кислоты формулы I.

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27-02-2013 дата публикации

МУЛЬТИВИТАМИННАЯ/МИНЕРАЛЬНАЯ КОМПОЗИЦИЯ ДЛЯ БОРЬБЫ С ЭФФЕКТАМИ ЭКОЛОГИЧЕСКОГО СТРЕССА; ПОВЫШЕНИЯ ИММУНИТЕТА И ПОВЫШЕНИЯ АКТИВНОСТИ, НАПРАВЛЕННАЯ НА НЕДОСТАТОЧНОСТИ ВИТАМИНОВ И МИНЕРАЛОВ БЕЗ НЕГАТИВНЫХ ПОБОЧНЫХ ЭФФЕКТОВ МЕГАДОЗОВОЙ ПИЩЕВОЙ ДОБАВКИ

Номер: RU2011128131A
Принадлежит:

... 1. Пищевая добавка, содержащая (1) витамин В1, витамин В2, никотиновую кислоту, витамин В6, биотин и пантотеновую кислоту; и (2) где массовое отношение биотина к витамину В1 составляет от 1:20 до 1:25; где массовое отношение биотина к витамину В2 составляет от 1:25 до 1:30; где массовое отношение биотина к никотиновой кислоте составляет от 1:310 до 1:330; где массовое отношение биотина к витамину В6 составляет от 1:30 до 1:35; где массовое отношение биотина к пантотеновой кислоте составляет от 1:110 до 1:130.2. Пищевая добавка по п.1, где массовое отношение биотина к витамину В1 составляет примерно 1:22; массовое отношение биотина к витамину В2 составляет примерно 1:28; массовое отношение биотина к никотиновой кислоте составляет примерно 1:320; массовое отношение биотина к витамину В6 составляет примерно 1:32; массовое отношение биотина к пантотеновой кислоте составляет примерно 1:120.3. Пищевая добавка по п.1, где количество витамина В1 составляет от примерно 1 до примерно 2 мг; количество ...

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27-01-2005 дата публикации

ПРОИЗВОДНЫЕ 5-ЧЛЕННЫХ ГЕТЕРОЦИКЛОВ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Номер: RU2003132471A
Принадлежит:

... 1. Соединение, выбранное из следующих соединений: 2,6-ди-трет-бутил-4-{2-[2-(метиламино)этил]-1,3-тиазол-4-ил}фенола; 2, 6-ди-трет-бутил-4-[4-(гидроксиметил)-1,3-оксазол-2-ил]фенола; 2,6-ди-трет-бутил-4-{2-[1-(метиламино)этил]-1,3-тиазол-4-ил}фенола; 2,6-ди-трет-бутил-4-[2-(метоксиметил)-1, 3-тиазол-4-ил]фенола; 2,6-ди-трет-бутил-4-{4-[(метиламино)метил]-1,3-оксазол-2-ил]фенола; N-{[4-(3,5-ди-трет-бутил-4-гидроксифенил)-1,3-тиазол-2-ил]метил}ацетамида; этил[4-(3,5-ди-трет-бутил-4-гидроксифенил)-1,3-тиазол-2-ил]метилкарбамата; 2,6-ди-трет-бутил-4-[2-(морфолин-4-илметил)-1,3-тиазол-4-ил]фенола; 2, 6-ди-трет-бутил-4-[2-(тиоморфолин-4-илметил)-1,3-тиазол-4-ил]фенола; 4-[2-(анилинометил)-1,3-тиазол-4-ил]-2,6-ди-трет-бутилфенола; 2, 6-ди-трет-бутил-4-(2-{[[2-(диметиламино)этил](метил)амино]метил}-1,3-тиазол-4-ил)фенола; 2,6-ди-трет-бутил-4-{5-метил-2-[(метиламино)метил]-1,3-тиазол-4-ил}фенола; 1-[4-(10Н-фенотиазин-2-ил)-1,3-тиазол-2-ил]метанамина; N-{[4-(3,5-ди-трет-бутил-4-гидроксифенил)-1,3 ...

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16-01-2024 дата публикации

Ингибиторы альдостеронсинтазы (CYP11B2) человека

Номер: RU2811745C1

Изобретение относится к области биотехнологии. Описана группа изобретений, включающая соединение, фармацевтическую композицию для лечения или профилактики заболевания или состояния, которое опосредовано или поддерживается активностью CYP11B2, включающую вышеуказанное соединение, и способ лечения или профилактики заболевания или состояния, которое опосредовано или поддерживается активностью CYP11B2. Изобретение расширяет арсенал средств, характеризующихся высокой эффективностью в ингибировании активности цитохрома 11В2 человека (CYP11B2). 3 н. и 23 з.п. ф-лы, 2 табл., 33 пр.

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29-11-2007 дата публикации

ZUSAMMENSETZUNG AUS EINER BESCHICHTUNG ODER MATRIX MIT VERZÖGERTER FREISETZUNG UND EINEM NMDA-REZEPTORANTAGONISTEN SOWIE VERFAHREN ZUR VERABREICHUNG EINES SOLCHEN NMDA-REZEPTORANTAGONISTEN AN EIN SUBJEKT

Номер: DE0005852057T1

Pharmazeutische Zusammensetzung, die Memantin oder ein pharmazeutisch verträgliches Salz davon und eine Komponente für eine verzögerte Freisetzung umfasst, zur Verwendung bei einer oralen Verabreichung zum Erreichen einer therapeutisch wirksamen Plasma-Gleichgewichtskonzentration von Memantin oder eines pharmazeutisch verträglichen Salzes davon in einem Menschen innerhalb von 15 Tagen ab dem Beginn einer Therapie mit Memantin oder einem pharmazeutisch verträglichen Salz davon.

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04-10-1973 дата публикации

Номер: DE0001618626C3

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01-10-1970 дата публикации

Номер: DE0002006433A1
Автор:
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19-07-2006 дата публикации

Microbe inhibition

Номер: GB0000611144D0
Автор:
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03-09-1987 дата публикации

THERAPEUTIC USE OF SEROTONIN-ANTAGONISTS

Номер: GB0008717768D0
Автор:
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17-02-1988 дата публикации

Therapeutic use of serotonin antagonists

Номер: GB0002193633A
Принадлежит:

Use of a mono or bicyclic carbocylic, or heterocyclic carboxylic, acid ester or amide or an imidazolyl carbazol in the manufacture of a medicament suitable for the treatment of stress-related psychiatric disorders, for increasing vigilance, for the treatment of rhinitis or serotonin-induced disorders and/or coadministration with another active agent to increase the bioavailability thereof, or for nasal administration.

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14-11-1990 дата публикации

THERAPEUTIC USE OF SEROTONIN ANTAGONISTS

Номер: GB0002231264A
Принадлежит:

Use of a mono or bicyclic carbocyclic, or heterocyclic carboxylic, acid ester or amide or an imidazolyl carbazol in the manufacture of a medicament suitable for the treatment of stress-related psychiatric disorders, for increasing vigilance, for the treatment of rhinitis or serotonin-induced disorders and/or coadministration with another active agent to increase the bioavailability thereof, of for nasal administration.

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05-05-1971 дата публикации

Номер: GB0001230528A
Автор:
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21-06-2006 дата публикации

Novel compounds

Номер: GB0000609117D0
Автор:
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17-07-1968 дата публикации

Pharmaceutical compositions containing basic ethers

Номер: GB0001119836A
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Pharmaceutical compositions having analgesic, vasodilator, antihistaminic, antidepressive and vagolytic activity comprise a solid or sterile parenterally acceptable carrier and a compound (or a salt thereof) of the general formula: wherein A represents an alkyl group or a group of the formulae or in which X is H, 1 or 2 halogens, 1 or 2 methyl groups or -CF3; R is alkyl, phenylalkyl, ar-halophenyl alkyl or tetrahydrofurfuryl; B is a morpholino group or a secondary or tertiary amino group of the formula -NHR1 or -NR2R3 wherein R1 is alkyl, cycloalkyl, alkenyl, hydroxyalkyl or aralkyl and R2 and R3 are alkyl, hydroxyalkyl, acyloxyalkyl or aralkyl or a group of the formulae in which M is 4 or 5 and R4 is H, alkyl, aralkyl, diaralkyl, ar-haloaralkyl, haloalkyl, hydroxyalkyl, acyloxyalkyl, diarylalkoxyalkyl or ar-trimethoxybenzyl.

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09-09-1970 дата публикации

IMPROVEMENTS IN OR RELATING TO SULPHON ANILIDES AND THE MANUFACTURE THEREOF

Номер: GB0001204946A
Автор:
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... 1,204,946. Phenoxyalkanesulphonanilides. UPJOHN CO. 12 June, 1968 [18 July, 1967], No. 27979/68. Heading C2C. Novel compounds I (including salts thereof) wherein X is halo, C 1-4 alkyl or C 1-4 alkoxy, Y is halo, R1 is H, C 1-4 alkyl, 3-piperidinopropyl, 2-piperidinoethyl, 3-pyrrolidinopropyl, 2-pyrrolidinoethyl, 3-morpholinopropyl, 2-morpholinoethyl or dialkylaminoalkyl of the formula -(CH 2 ) k .NR3R4, wherein R3 and R4 are the same or different C 1-4 alkyl, R2 is C 1-6 alkyl, k is 2 or 3, m is 0, 1, 2 or 3 and n is 0, 1 or 2, are obtained by the interaction of an alkanesulphonyl halide, halogen-SO 2 -R2, and an appropriate phenoxyaniline or N-alkylated (C 1-4 )-phenoxyaniline; products wherein R1 is a hydrogen atom may optionally be alkylated. Pharmaceutical preparations suitable for lowering cholesterol and triglyceride levels contain as active ingredient compounds I; administration is orally or parenterally.

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14-08-1975 дата публикации

Method of preparation of new dialkylaminoalkyl ethers of the 2-alcoxy-3,5-dihalogenobenzene.

Номер: OA0000003885A
Автор:
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17-12-2004 дата публикации

Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia.

Номер: AP0000001349A
Принадлежит:

This invention relates to a series of arylsubstituted piperazines, of formula (i), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the alpha-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other diseases.

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30-09-1998 дата публикации

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

Номер: AP0009801283A0
Принадлежит:

Derivatives of mutiline of formula (1a)and pharmaceutically acceptable salts and derivatives thereof, in which r1 is ethyl or vinyl, y is a carbamoyloxy group, which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

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31-12-1999 дата публикации

Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia

Номер: AP0009901684A0
Автор:
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24-12-1971 дата публикации

Process for the preparation of amino-alcohols and salts thereof.

Номер: OA0000003659A
Автор:
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15-05-2007 дата публикации

PRENYL TRANSFERASE INHIBITORS

Номер: AT0000359290T
Автор: KIM SUN H, KIM, SUN, H.
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15-06-2010 дата публикации

USE OF CHROMONDERIVATEN

Номер: AT0000469637T
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15-04-1981 дата публикации

INSECTICIDES PREPARATION

Номер: AT0000929178A
Автор:
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10-02-1970 дата публикации

PROCEDURE FOR the PRODUCTION OF NEW ONE 1-ALKYLIDENIMINOADAMANTANEN

Номер: AT0000278744B
Автор:
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10-12-1974 дата публикации

Procedure for the production of new N-1-Adamantyl-2-Carboxyl-1-azacycli connections and their salts

Номер: AT0000319262B
Автор:
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15-01-1978 дата публикации

INSECTICIDES PREPARATION

Номер: AT0000364675B
Автор:
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27-12-1965 дата публикации

Procedure for the production of Dibenzocycloheptaenverbindungen and their salts

Номер: AT0000244323B
Автор:
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10-12-1969 дата публикации

As well as procedures for the production of new Amino dihalogenphenyl äthylaminen from their acid addition salts

Номер: AT0000277210B
Автор:
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10-02-1969 дата публикации

Procedure for the production of new tricyclischen amines and their acid addition salts

Номер: AT0000268236B
Автор:
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10-11-1971 дата публикации

Procedure for the production of new Thiepin and Oxepin derivatives as well as their acid addition salts

Номер: AT0000294104B
Автор:
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10-12-1968 дата публикации

Procedure for the production of new Isoxazolderivaten

Номер: AT0000266831B
Автор:
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16-07-1992 дата публикации

USE OF TELLURIUM COMPOUNDS IN STIMULATING CELLS TO PRODUCE LYMPHOKINES

Номер: AU0000625922B2
Принадлежит:

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22-03-2007 дата публикации

Use of tellurium compounds for protection from ultra-violet radiation

Номер: AU2006290297A1
Принадлежит:

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15-06-2004 дата публикации

COMPOSITIONS AND METHOD FOR TREATING AFFECTIVE, PAINFUL OR ALLERGIC DISORDERS

Номер: AU2003290970A1
Принадлежит:

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23-02-2006 дата публикации

Chemokine combinations to mobilize progenitor/stem cells

Номер: AU2005272653A1
Принадлежит:

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22-01-2015 дата публикации

Fragments of the PA subunit of RNA dependent RNA polymerase from pandemic influenza virus A 2009 H1N1, and their use

Номер: AU2011229469B2
Принадлежит:

The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pandemic HlNl virus or is a variant thereof. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds which are able to modulate, preferably to ...

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18-09-2014 дата публикации

A multivitamin/mineral formulation to combat the effects of environmental stress; improve immunity and improve energy while addressing vitamin and mineral deficiencies without the negative side effects of a mega dose nutritional supplement

Номер: AU2010206791B2
Принадлежит:

A nutritional supplement, and methods of use thereof, are provided that are designed to be most effective in optimizing health, improving energy and appearance, reducing the effects of environmental stress and improving, aiding, assisting a person's immunity, including but not limited to decreasing the instances, duration and severity of cold infections.

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13-12-2018 дата публикации

Heterocyclic compounds and methods of use

Номер: AU2014312245B2
Принадлежит: Spruson & Ferguson

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists. Compounds of the invention may also find use in treating cancer. Presented herein are novel compounds bearing a perhaloalkylsulfonamide moiety. Such compounds, in addition to being highly effective SREBP inhibitors, are also unexpectedly highly bioavailable in vivo. Heteroaromatic compounds bearing sulfonamide groups are prone to several ionic states, based on the inherent pKa values.

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13-11-2014 дата публикации

High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions

Номер: AU2013262320A1
Принадлежит:

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

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26-03-2015 дата публикации

Compounds for the treatment of paramoxyvirus viral infections

Номер: AU2013305759A1
Принадлежит:

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

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28-11-2019 дата публикации

Processes for preparing oxathiazin-like compounds

Номер: AU2015365348B2
Принадлежит: WRAYS PTY LTD

Oxathiazin-like compounds, processes for making new oxathiazin-like compounds, compounds useful for making oxathiazin-like compounds, and their uses are disclosed. Processes of treating patients suffering from cancers, bacterial infections, fungal infections and/or viral infections by administering oxathiazin-like compounds are also disclosed. These compounds were found to have significantly longer half-life compared to taurolidine and taurultam.

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10-10-2019 дата публикации

Selenosugars and therapeutic uses thereof

Номер: AU2014408672B2
Принадлежит: FB Rice Pty Ltd

A topical composition for skin repair comprising selenosugars of formula (1): (Formula (I)) wherein, n is 1, 2 or 3; m is 2, 3, 4; or 5; and each R1 is independent!y-(optionally substituted C ...

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27-09-2018 дата публикации

Gamma-diketones as Wnt/beta -catenin signaling pathway activators

Номер: AU2014218720B2

The present disclosure provides ƴ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

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12-05-2016 дата публикации

Novel 3-azabicyclo[3.1.0]hexane derivative and use thereof for medical purposes

Номер: AU2014354085A1
Принадлежит:

The present invention addresses the problem of providing a compound which has few adverse side effects, high safety and an antagonistic activity to a opioid receptor. A compound represented by general formula (I) [wherein R ...

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05-01-2012 дата публикации

Method of reducing multi-drug resistance using inositol tripyrophosphate

Номер: US20120003327A1
Принадлежит: Individual

Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.

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05-01-2012 дата публикации

Chroman derivatives, medicaments and use in therapy

Номер: US20120004296A1
Принадлежит: Marshall Edwards Inc

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

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09-02-2012 дата публикации

Compositions for potentiating apoposis signals in tumour cells

Номер: US20120034210A1

The present invention concerns a composition for potentiating formation of DISC (Death Inducing Signaling Complex) macro-complex and for inducing apoptotic signal mediated by death receptors in tumour cells comprising a therapeutically effective amount of an active agent selected among a hypocalcemia-inducing agent, a calcium channel inhibitor and a calcium chelator in association with a therapeutically effective amount of an anticancer agent inducing an apoptotic signal via death receptors Fas, TNF-R1, DR4 and/or DR5.

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16-02-2012 дата публикации

Methods of treating pain

Номер: US20120039866A1
Автор: Daniela Salvemini
Принадлежит: St Louis University

The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.

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16-02-2012 дата публикации

Compositions and systems for forming crosslinked biomaterials and associated methods of preparation and use

Номер: US20120039980A1
Принадлежит: AngioDevice International GmbH

Methods of preventing adhesion between issues are provided that utilizes in situ crosslinked biomaterials. The biomaterial contains at least the crosslinked product of two biocompatible, non-immunogenic components having reactive groups thereon, with the functional groups selected so as to enable inter-reaction between the components, i.e., crosslinking. Exemplary uses for the crosslinked compositions include preventing adhesions following surgery or injury, and preventing scar tissue formation.

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15-03-2012 дата публикации

Cyclodextrin-based polymers for therapeutics delivery

Номер: US20120065368A1
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.

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29-03-2012 дата публикации

Methods of enhancing drug delivery and effectiveness of therapeutic agents

Номер: US20120076862A1
Принадлежит: Individual

The present invention in one aspect provides methods of enhancing uptake of a therapeutic agent in a target tissue as well as methods of treating a disease (such as cancer) or enhancing effectiveness of treatment with a therapeutic agent in an individual by co-administering a composition comprising nanoparticles comprising albumin and a poorly water soluble drug such as a taxane with the therapeutic agent. The present invention in another aspect provides a method of treatment or a method of selecting patients for treatment of a disease (such as cancer) with the combination of a therapeutic agent and a composition comprising nanoparticles comprising albumin and a poorly water soluble drug such as a taxane based on one or more characteristics of the target tissue that correlates or indicates the capability of getting enhanced therapeutic agent uptake as a result of the co-administration of the taxane nanoparticle composition in the target tissue (referred to as “the drug uptake capability”). Also provided are pharmaceutical compositions, article of manufacture, and kits useful for methods described herein.

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12-04-2012 дата публикации

Use of inhibitors of bruton's tyrosine kinase (btk)

Номер: US20120087915A1
Принадлежит: Pharmacyclics LLC

Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

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12-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120088762A1
Принадлежит: Onyx Therapeutics Inc

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

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26-04-2012 дата публикации

Solubilisation Method

Номер: US20120100067A1
Принадлежит: MEDIGENE AG

The present invention relates to the solubilisation of an active agent in a lipid dispersion, in particular to the solubilisation of an active agent in a suspension of preformed empty liposomes.

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26-04-2012 дата публикации

Compositions and methods for biological remodeling with frozen particle compositions

Номер: US20120101738A1
Принадлежит: SEARETE LLC

Certain embodiments disclosed herein relate to compositions, methods, devices, systems, and products regarding frozen particles. In certain embodiments, the frozen particles include materials at low temperatures. In certain embodiments, the frozen particles provide vehicles for delivery of particular agents. In certain embodiments, the frozen particles are administered to at least one biological tissue.

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03-05-2012 дата публикации

Films and particles

Номер: US20120107365A1

Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.

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17-05-2012 дата публикации

Localized therapy following breast cancer surgery

Номер: US20120121510A1
Принадлежит: Individual

Particles providing prolonged release of chemotherapy are injected or implanted into surgical sites in the breast following removal of cancerous tissue. In one embodiment, the particles are designed to not release formulation for approximately two to three weeks after surgery so as to not inhibit healing; in another embodiment particles are not administered until two to three weeks after surgery, and release immediately. The particles then release an effective amount of a chemotherapeutic such as a taxane to inhibit proliferation of any remaining cancer cells at or near the surgical site. This may also help prevent overproliferation leading to scarring with the surgical region.

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17-05-2012 дата публикации

Bicyclic compound and use thereof for medical purposes

Номер: US20120122964A1
Принадлежит: Ono Pharmaceutical Co Ltd

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

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24-05-2012 дата публикации

Pentamidine combinations for treating cancer

Номер: US20120128667A1
Принадлежит: Oncozyme Pharma Inc

The present invention relates to the treatment of cancer, e.g., ovarian cancer, breast cancer, pancreatic cancer or colon cancer, with pentamidine and (a) oxaliplatin, (b) gemcitabine, (c) taxol, (d) 5-fluorouracil or (e) CPT 11.

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24-05-2012 дата публикации

Docetaxel formulations with lipoic acid

Номер: US20120129922A1
Автор: Nageswara R. Palepu
Принадлежит: Scidose Llc

Pharmaceutical formulations comprising docetaxel or a pharmaceutically acceptable salt thereof, one or more solubilizers, α-lipoic acid, TPGS, one or more hydrotropes, and optionally one or more agents having a pK a of about 3 to about 6. The pharmaceutical formulations are stable and substantially free of excipients that can cause severe side effects and maintains chemical stability during storage. The pharmaceutical formulations are ready to be combined with an infusion solution for administration to patients in need thereof. Methods of treating patients in need thereof comprise administering the pharmaceutical formulations combined with an infusion solution.

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31-05-2012 дата публикации

Methods to regulate polarization and enhance function of excitable cells

Номер: US20120136296A1
Автор: Gholam A. Peyman
Принадлежит: Individual

Minimally invasive delivery with intercellular and/or intracellular localization of nano- and micro-particle solar cells within and among excitable biological cells to controllably regulate membrane polarization and enhance function of such cells. The cells include retinal and other excitable cells.

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05-07-2012 дата публикации

Chroman derivatives, medicaments and use in therapy

Номер: US20120172424A1
Принадлежит: Marshall Edwards Inc

Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

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19-07-2012 дата публикации

use of inhibitors of bruton's tyrosine kinase (btk)

Номер: US20120183535A1
Принадлежит: Pharmacyclics LLC

Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

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19-07-2012 дата публикации

1,2,4-thiazoloidin-3-one derivatives and their use in the treatment of cancer

Номер: US20120183537A1
Принадлежит: Betagenon Ab

According to the invention there is provided a compound of formula (I) wherein: A represents C(═N—W-D) or S; B represents S or C(—NH—W-D); when: A represents C(═N—W-D) and B represents S then the bond between B and the NH atom is a single bond; or A represents S and B represents C(—NH—W-D) then the bond between B and the NH atom is a double bond; X represents -Q-[CR x R y ] n —; W represents —[CR x R y ] m — or —C(O)—[CR x R y ] p —; Q represents a bond, —N(R a )—, —S—, or —O—; A 1 to A 5 respectively represent C(R 1 ), C(R 2 ), C(R 3 ), C(R 4 ) and C(R 5 ), or, alternatively, up to two of A 1 to A 5 may independently represent N; D represents phenyl, pyridyl or pyrimidinyl optionally substituted by one or more R 6 groups, which compounds are useful in the treatment of cancer.

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02-08-2012 дата публикации

Therapeutic Inhibitor of Vascular Smooth Muscle Cells

Номер: US20120195951A1
Принадлежит: Individual

Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.

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23-08-2012 дата публикации

Methods of treating a subject and related particles, polymers and compositions

Номер: US20120213854A1
Автор: Oliver S. Fetzer
Принадлежит: Individual

Described herein are methods for treating a subject with combinations of polymer-agent particles and cyclodextrin polymer agent conjugates. The methods herein may be used to treat subjects identified with cancer, cardiovascular disorders, autoimmune disorders, or inflammatory disorders. Also described herein are compositions, dosage forms, and kits comprising polymer-agent particles and cyclodextrin polymer agent conjugates.

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13-09-2012 дата публикации

Method and apparatus for implementing control of multiple physically dual homed devices

Номер: US20120230183A1
Принадлежит: ROCKSTAR BIDCO LP

A ring control protocol is used to establish a separate control plane for a plurality of physically dual homed devices to enable collections of dual homed devices to be represented by a single pair of addresses into the attached routed Ethernet network. The gateway devices analyze the passing ring control packets to create direct mappings for data packets to the routed Ethernet network. Thus, although the dual homed devices are treated as a ring from a control perspective, the data path is implemented to be direct so that data packets continue to flow directly from the dual homed devices to each of the attached gateway devices. In one embodiment, each of the gateway devices implements a virtual switch and advertises the MAC address of the virtual switch into the routed Ethernet network rather than the MAC addresses of each of the attached Ethernet Switch Units.

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13-09-2012 дата публикации

Block Copolymer For Intraperitoneal Administration Containing Anti-Cancer Agent, Micelle Preparation Thereof, And Cancer Therapeutic Agent Comprising The Micelle Preparation As Active Ingredient

Номер: US20120231053A1
Принадлежит: Nippon Kayaku Co Ltd

To provide a therapeutic method using a water soluble, high molecular weight block polymer to enable that an intraperitoneally administered anti-cancer agent may maintain for a long-term retention in the abdominal cavity to enoughly exert the effect of the anti-cancer agent and reduce adverse side-effects thereof. A therapeutic agent as a micelle preparation, comprising a copolymer having a hydrophilic polymeric moiety and a polycarboxylic acid derivative moiety; and an anti-cancer agent bonding to or encapsulated in the copolymer, wherein the micelle preparation may exhibit sustained drug release capability, and enables an extension of a retention time period of the anti-cancer agent in an abdominal cavity, is provided. A superior life-prolonging effect was found in an intraperitoneal administration mouse model compared with a case in which only an encapsulated drug is administered, and thus the present invention was completed accordingly.

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20-09-2012 дата публикации

Anti-constipation composition

Номер: US20120237598A1
Автор: Ryuji Ueno
Принадлежит: SUCAMPO AG

An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X 1 and X 2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.

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04-10-2012 дата публикации

Drug delivery from rapid gelling polymer composition

Номер: US20120252905A1
Принадлежит: Angiotech International AG

Compositions are disclosed that afford drug delivery from two-part polymer compositions that rapidly form covalent linkages when mixed together. Such compositions are particularly well suited for use in a variety of tissue related applications when rapid adhesion to the tissue and gel formation is desired along with drug delivery. For example, the compositions are useful as tissue sealants, in promoting hemostasis, in effecting tissue adhesion, in providing tissue augmentation, and in the prevention of surgical adhesions.

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11-10-2012 дата публикации

Anticancer combination of artemisinin-based drugs and other chemotherapeutic agents

Номер: US20120258181A1

The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.

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01-11-2012 дата публикации

Drug Loaded Polymeric Nanoparticles and Methods of Making and Using Same

Номер: US20120276162A1
Принадлежит: Individual

The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

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15-11-2012 дата публикации

Lipase Inhibitors for the Treatment of Pancreatitis and Organ Failure

Номер: US20120289588A1
Автор: Vijay Prem Singh
Принадлежит: Individual

The present invention relates to methods for treating pancreatitis and/or organ failure comprising administering, to a subject in need of such treatment, an effective amount of a lipase inhibitor. It is based, at least in part, on the discoveries that lipotoxicity contributes to inflammation, multisystem organ failure, necrotic pancreatic acinar cell death and in acute pancreatitis, and that inhibition of lipolysis was able to reduce indices associated with these conditions. Accordingly, in various embodiments, the present invention provides for methods and compositions for limiting lipotoxicity and thereby reducing the likelihood of poor outcomes associated with acute pancreatitis and other severe systemic conditions, especially in obese individuals.

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22-11-2012 дата публикации

Treatment of lung cancer

Номер: US20120294957A1
Принадлежит: Ramot at Tel Aviv University Ltd

Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.

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06-12-2012 дата публикации

Submicro emulsion of paclitaxel using steroid complex as intermediate carrier

Номер: US20120308616A1
Принадлежит: Institute of Materia Medica of CAMS

A submicron emulsion of paclitaxel, the preparation method and the use thereof are disclosed. Said paclitaxel submicron emulsion comprises paclitaxel/steroid complex, oil for injection, water for injection, emulsifier, assistant emulsifier and isotonic agent, wherein the mole ratio of paclitaxel to steroid in the complex is 1:0.2˜4; preferably 1:0.25˜2. Said submicron emulsion is useful for the treatment for malignant tumor. The average particle diameter of the submicron emulsion is less than 400 nm and the pH Value is 3.5-6.

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06-12-2012 дата публикации

Micelle composition of polymer and passenger drug

Номер: US20120309780A1
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Hydrophobic drugs become more practical for treatments by being encapsulated in micelle compositions for increasing solubility. Micelle compositions may include an excipient tocopherol and/or prodrug formulations of the drug. Micelles extend the time period the drug remains in the micelles to improve drug circulation time and thereby drug delivery. Hydrophobic drugs for micelle encapsulation may include rapamycin, geldanamycin, and paclitaxel. Administration of these micelle compositions does not require Cremophor EL or Tween 80, avoiding serious side effects associated with these products which would previously accompany such drug administration.

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27-12-2012 дата публикации

Treatment of cancer using benzoic acid derivatives

Номер: US20120329861A1
Принадлежит: New York University NYU

The present invention provides a method of treating cancer using benzoic acid derivatives, alone or in combination with standard treatments such as chemotherapy and radiotherapy. Also provided are methods of screening for benzoic derivatives based on their ability to inhibit the enzyme tyrosinase or to bind to and activate PXR/SXR xenobiotic receptors.

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03-01-2013 дата публикации

Anti-cancer agent delivery vehicles capable of improved loading

Номер: US20130004488A1

There is provided a conjugate of a delivery agent containing a chemical moiety and at least one flavonoid. The flavonoid exists in a monomeric form or dimeric form before conjugation and remains in the monomeric form or dimeric form after conjugation. Preferably, the conjugate comprises two flavonoids. The delivery agent is conjugated at the C6 and/or the C8 position of the A ring of the flavonoid. An anti-cancer agent delivery vehicle comprising an anti-cancer agent and the conjugate is also provided.

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03-01-2013 дата публикации

Inhibitors of brutons tyrosine kinase for the treatment of solid tumors

Номер: US20130005746A1
Принадлежит: Pharmacyclics LLC

Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.

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07-02-2013 дата публикации

Small-molecule inhibitors of dengue and west nile virus proteases

Номер: US20130035284A1
Принадлежит: University of Texas System

The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.

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21-02-2013 дата публикации

Parenteral formulations of macrolide antibiotics

Номер: US20130045937A1
Принадлежит: Cempra Pharmaceuticals Inc

Described herein are pharmaceutical compositions adapted for the parenteral administration of macrolide antibiotics, such as triazole-containing and fluoroketolide antibiotics. Also described herein are methods for their use in the treatment of bacterial, protozoal, and other infections.

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28-02-2013 дата публикации

Non-aqueous taxane pro-emulsion formulations and methods of making and using the same

Номер: US20130052241A1
Автор: Kiichiro Nabeta
Принадлежит: Teikoku Pharma USA Inc

Non-aqueous taxane pro-emulsion formulations are provided. Pro-emulsion formulations of embodiments of the invention include a taxane, an oil component, a surfactant component and, optionally, a non-aqueous solvent component. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations.

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07-03-2013 дата публикации

Treatment of solid tumors with rapamycin derivatives

Номер: US20130059877A1
Принадлежит: Individual

Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.

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21-03-2013 дата публикации

Fascile synthesis of biocompatible polymer capsule nanoparticles for drug encapsulation

Номер: US20130071472A1
Автор: SHIEH Dar-Bin
Принадлежит:

The present invention relates to a method for preparing a capsule nanoparticle used in encapsulating hydrophobic medicines, comprising the following steps: (A) providing a biocompatible polymer and an organic solution containing a hydrophobic medicine; (B) stirring the organic solution at 3-10° C., and titrating with an alcohol solution, so as to make the biocompatible polymer encapsulate hydrophobic medicine to form a capsule nanoparticle; (C) ultrasonic vibrating the capsule nanoparticle at 3-10° C.; (D) filtering the capsule nanoparticle to an average size controllable in the range of 60-450 nm; and (E) lyophilizing the encapsulated particles. 1. A method for preparing capsules encapsulating hydrophobic medicines , comprising the steps of:(A) providing an organic solution having a biocompatible polymer and a hydrophobic medicine;(B) stirring the organic solution at a low temperature of 3 to 10° C., and titrating with a alcohol solution, to make the biocompatible polymer encapsulate the hydrophobic medicine to form a capsule nanoparticle;(C) ultrasonic vibrating the capsule nanoparticle at a low temperature of 3 to 10° C.;(D) filtering the capsule nanoparticle, to make an average capsule nanoparticle diameter of the capsule nanoparticle at 60-450 nm; and(E) lyophilizing the capsule nanoparticle.2. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein claim 1 , the biocompatible polymer is selected from the group consisting of: (poly-(D claim 1 ,L-lactide-co-glycolide)) claim 1 , PLA claim 1 , and PEG-PLA.3. The method for preparing capsules encapsulating hydrophobic medicines according to claim 1 , wherein the hydrophobic medicine is a anti-cancer medicine.4. The method for preparing capsules encapsulating hydrophobic medicines according to claim 3 , wherein claim 3 , the anti-cancer is at least selected from the group consisting of: phyxol claim 3 , J-30 claim 3 , LY 294002 and AG490.5. The method for preparing ...

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21-03-2013 дата публикации

Theranostic and diagnostic methods using sparc and hsp90

Номер: US20130072389A1
Принадлежит: Caris Life Sciences Inc

Provided herein are methods and systems of molecular profiling of diseases, such as cancer. The molecular profiling can be used to provide a diagnosis, prognosis, or theranosis for the disease, such as identifying a candidate treatment. The methods can detect overexpression of SPARC and HSP90. The cancer can be, e.g., a renal cell carcinoma or an interdigitating dendritic cell sarcoma.

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28-03-2013 дата публикации

Method of Treating Cancer

Номер: US20130078288A1
Автор: Yu Chun Ho
Принадлежит:

A method and composition for administering a therapeutic composition to a lesion comprising about 20% to about 50% ethanol and other novel therapeutic agents. 1. A therapeutic composition for treatment of hepatic solid tumors comprising a fatty acid mixture and ethanol wherein the ratio of said fatty acid mixture to ethanol is about 1 to 1 to about 5 to 1 and maybe retained in said tumors from about 15 month to about 51 month.2. The therapeutic composition for treating hepatic solid tumors of wherein the said fatty acid mixture is a combination of fatty acids comprising of linolenic acid claim 1 , linoleic acid claim 1 , and oleic acid.3. The therapeutic composition for treating hepatic solid tumors of further comprising a therapeutic agent which may comprise of cisplatin claim 1 , paclitaxol claim 1 , doxorubicin claim 1 , and/or ethanol.4. The therapeutic composition for treating hepatic solid tumors of further comprising a hyperthermia therapy agent.5. The therapeutic composition for treating hepatic solid tumors of wherein said hyperthermia therapy agent comprise of iron oxide nanoparticles with a diameter of approximately 20 to 30 nanometers.6. The therapeutic composition for treating hepatic solid tumors of wherein said hyperthermia therapy agent comprise of tantalum nanoparticles or microparticles.7. The therapeutic composition for treating hepatic solid tumors of wherein the said composition may be administered to a solid tumor by intra-arterial injection that carries blood to the tumor and is retained in a solid tumor claim 1 , occludes arterial vasculature of said solid tumor and occludes portal venous vessels that supply liver tumors.8. The composition for treating hepatic solid tumors of where in the said therapeutic composition serves as a embolic agent claim 1 , sclerosing agent and a chemical ablative agent.9. A method of treating hepatic solid tumors by administering a therapeutic composition to the solid tumors comprising:combining a therapeutic ...

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28-03-2013 дата публикации

Method of Treating Hair Loss Due to Systemic Chemotherapy

Номер: US20130079312A1
Автор: Joel E. Bernstein
Принадлежит: Elorac Ltd

Methods and composition for preventing and/or treating hair loss associated with the administration of cancer chemotherapy using vasoconstrictors are disclosed. Optionally corticosteroids are also in the formulation.

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04-04-2013 дата публикации

COMBINATORIAL THERAPIES FOR THE TREATMENT OF NEOPLASIAS USING THE OPIOID GROWTH FACTOR RECEPTOR

Номер: US20130084242A1
Принадлежит: THE PENN STATE RESEARCH FOUNDATION

The present invention relates to pharmaceutical compositions for treating neoplasias in an animal or human comprised of a carrier and therapeutically effective amounts of at least one chemotherapeutic agent along with the biotherapeutic endogenous pentapeptide Met-enkephalin, referred to as opioid growth factor. Also provided are methods of treating neoplasias in an animal or human in need of such treatment, comprising the administration to the animal or human therapeutically effective amounts of a pharmaceutical composition comprised of a carrier and therapeutically effective amounts of at least one neoplasia-treating agent, such as a chemotherapeutic agent or radiation, along with opioid growth factor. 1. A pharmaceutical composition for treating neoplasias in an animal or human which are characterized by an opioid growth factor receptor , comprising:therapeutically effective amounts of at least one chemotherapeutic, biotherapeutic, and/or radionuclide agent with between about 20 to 1000 μg/kg body weight of an opioid growth factor; and a carrier.2. The pharmaceutical composition of wherein said agent is a therapeutic agent.3. The pharmaceutical composition of claim 2 , wherein the neoplasias includes not limited to pancreatic cancer claim 2 , squamous cell cancer of the head and neck claim 2 , breast cancer claim 2 , colorectal cancer claim 2 , renal cancer claim 2 , brain cancer claim 2 , prostate cancer claim 2 , bladder cancer claim 2 , bone or joint cancer claim 2 , uterine cancer claim 2 , cervical cancer claim 2 , endometrial cancer claim 2 , multiple myeloma claim 2 , Hodgkin's disease claim 2 , non-Hodgkin's lymphoma claim 2 , melanoma claim 2 , leukemias claim 2 , lung cancer claim 2 , ovarian cancer claim 2 , gastrointestinal cancer claim 2 , Kaposi's sarcoma claim 2 , liver cancer claim 2 , pharyngeal cancer and laryngeal cancer.4. The pharmaceutical composition of claim 3 , wherein the chemotherapeutic agent is selected from but not limited to the ...

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04-04-2013 дата публикации

METHODS OF CARDIOVASCULAR PATIENT TREATMENT USING SUBSTANCES SUFFICIENT TO REDUCE ACTIN DEPOLYMERIZATION

Номер: US20130085109A1
Принадлежит:

Methods of cardiovascular patient treatment using substances sufficient to reduce actin depolymerization. In an exemplary embodiment of a method of treating a patient of the present disclosure, the method comprises the step of administering a therapeutically effective dose of a substance that reduces actin depolymerization within a vasculature of a patient to treat a cardiovascular condition of the patient. In at least one embodiment, the substance the substance is selected from the group consisting of jasplakinolide, Jasplaskinolide V, and Amphidinolide H. 1. A method of treating a patient , the method comprising the step of administering a therapeutically effective dose of a substance that reduces actin depolymerization within a vasculature of a patient to treat a cardiovascular condition of the patient.2. The method of claim 1 , wherein the substance is selected from the group consisting of jasplakinolide claim 1 , Jasplaskinolide V claim 1 , and Amphidinolide H.3. The method of claim 1 , wherein the cardiovascular condition comprises blood flow reversal.4. The method of claim 3 , wherein the therapeutically effective dose of the substance does not inhibit the incidence of blood flow reversal.5. The method of claim 1 , wherein the cardiovascular condition comprises congestive heart failure.6. The method of claim 1 , wherein the therapeutically effective dose is effective to prevent actin depolymerization with the vasculature of the patient.7. The method of claim 1 , wherein the therapeutically effective dose of the substance also inhibits an effect of superoxide within the vasculature of the patient.8. The method of claim 1 , wherein the therapeutically effective dose of the substance also inhibits superoxide production within the vasculature of the patient claim 1 , wherein the superoxide production is induced due to the cardiovascular condition.9. The method of claim 1 , wherein the therapeutically effective dose of the substance also inhibits superoxide ...

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04-04-2013 дата публикации

COMBINATION OF AN IAP INHIBITOR AND A TAXANE FOR THE TREATMENT OF A PROLIFERATIVE DISEASE

Номер: US20130085153A1
Принадлежит:

The invention provides a pharmaceutical combination comprising: 2. A method for treating or preventing a proliferative disease in a subject in need thereof claim 1 , comprising co-administration to said subject of a therapeutically effective amount of at least one taxane and a compound that inhibit the binding of the Smac protein to IAPs of formula (I) or (IV) according to .3. A pharmaceutical combination according to claim 1 , for use in a method according to .4. A pharmaceutical combination according to claim 1 , for use in the preparation of a medicament for use in a method according to .6. A pharmaceutical combination according to claim 1 , wherein agent b) is selected from Paclitaxel claim 1 , docetaxel claim 1 , vinorelbine and the epothilones and combinations thereof.7. A method for treating a proliferative disease comprising administering a combination of a taxane and a compound that inhibit the binding of the Smac protein to IAPs of formula (I) or (IV).8. A method for treating a proliferative disease comprising administering a combination of a taxane and a compound selected from N-[1-cyclohexyl-2-oxo-2-(6-phenethyl-octahydro-pyrrolo[2 claim 1 ,3-c]pyridin-1-yl-ethyl]-2-methylamino-propionamide of formula (III) and pharmaceutically acceptable salts thereof.9. A method for treating a proliferative disease comprising administering a combination of a taxane and a compound that inhibit the binding of the Smac protein to IAPs of formula (I) or (IV) claim 1 , wherein the taxane is selected from paclitaxel and docitaxel claim 1 , and combinations thereof.10. A method for treating a proliferative disease selected from breast claim 1 , ovarian and lung tumors comprising administering a combination of a taxane and a compound that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of formula (I) or (IV).11. A method for treating a proliferative disease selected from breast claim 1 , ovarian and lung tumors comprising administering a ...

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11-04-2013 дата публикации

Macrocyclic Inhibitors Of Hepatitis C Virus

Номер: US20130089520A1
Принадлежит: Medivir AB

Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R 1 is —OR 7 , —NH—SO 2 R 8 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkyl; R 4 is aryl or Het; n is 3, 4, 5, or 6; R 5 is halo, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, phenyl, or Het; R 6 is C 1-6 alkoxy, or dimethylamino; R 7 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 8 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

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11-04-2013 дата публикации

COMPOSITIONS AND METHODS FOR TREATING OBESITY AND OBESITY-RELATED CONDITIONS

Номер: US20130089603A1
Автор: Thompson Ronald
Принадлежит: CHELATEXX LLC

A method to effectively treat the adverse events of ingested lipase inhibitor such as orlistat, and to maintain the effectiveness of ingested orlistat, the method comprising the steps of: ingesting a compound of orlistat to irreversibly bind with lipase enzymes of the gastrointestinal tract; ingesting a compound of simethicone to cause undigested fats to remain in an emulsified state in the bowel; and ingesting an enteric-coated activated charcoal to absorb emulsified fats only in the lower bowel, thus preventing the adverse events associated with the ingestion of orlistat alone. 131-. (canceled)32. A method of treating obesity or an obesity-related condition , comprising the step of administering a therapeutically effective amount of a lipase inhibitor in combination with an effective amount of a surfactant and an effective amount of enteric-coated activated charcoal.33. The method of claim 32 , wherein said lipase inhibitor is orlistat or cetilistat claim 32 , and said surfactant is simethicone.34. The method of claim 33 , wherein said lipase inhibitor is administered separately from said simethicone and enteric-coated charcoal.35. The method of wherein said lipase inhibitor comprises orlistat claim 32 , and said lipase inhibitor claim 32 , simethicone and enteric-coated activated charcoal are administered together in a unit dosage form.36. The method of claim 35 , wherein said enteric coating is configured such that the activated charcoal is primarily released in the lower half of the small intestine.37. The method of claim 35 , wherein said enteric coating is configured such that the activated charcoal is primarily released in the lower third of the small intestine.38. The method of claim 35 , wherein said enteric coating is configured such that the activated charcoal is primarily released in the terminal ileum and ascending colon.39. The method of claim 35 , wherein said unit dosage form comprises from 30 to 240 mg of orlistat.40. The method of claim 39 , ...

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11-04-2013 дата публикации

COMPOSITIONS INCLUDING TRICIRIBINE AND TAXANES AND METHODS OF USE THEREOF

Номер: US20130090304A1
Принадлежит:

This application relates to combination therapies including triciribine and related compounds and taxanes and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation. 127-. (canceled)29. The method of claim 28 , wherein the biological sample is taken from breast claim 28 , pancreas claim 28 , ovary claim 28 , colon claim 28 , or rectum.30. The method of claim 28 , wherein the level of Akt kinase expression is determined by assaying the cancer for the presence of a phosphorylated Akt kinase.31. The method of claim 28 , wherein the level of Akt kinase expression is determined by assaying the cancer for the presence of a phosphorylated Akt kinase with an antibody.32. The method of claim 28 , wherein the administration is repeated at least twice.33. The method of claim 28 , wherein the administration is repeated at least 4 times.34. The method of claim 28 , wherein at least 10 mg/mof the triciribine compound is administered.35. The method of claim 28 , wherein 10 mg/mor less of the triciribine compound is administered.3614. The method of claim claim 28 , wherein the administration is repeated until regression of the cancer is achieved.37. The method of claim 28 , wherein the drug is administered intravenously.38. The method of claim 28 , wherein the subject has been diagnosed with a carcinoma claim 28 , sarcoma claim 28 , lymphoma claim 28 , leukemia claim 28 , or myeloma.39. The method of wherein the subject is mammal.40. The method of wherein the subject is human. This application is a continuation-in-part of U.S. application Ser. No. 11/096,082, filed Mar. 25, 2005, which claims the benefit of U.S. provisional patent application No. 60/557,599 filed Mar. 29, 2004, which is incorporated herein by reference.This application relates to combination therapies including triciribine compounds and one or more taxanes and compositions including such combinations with reduced ...

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18-04-2013 дата публикации

USE OF ISOQUINOLONES FOR PREPARING DRUGS, NOVEL ISOQUINOLONES AND METHOD FOR SYNTHESISING SAME

Номер: US20130096083A1
Принадлежит:

The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer. 136-. (canceled)38) A method for the prevention and treatment of mammals claim 37 , in particular humans claim 37 , suffering from pathological angiogenesis claim 37 , in particular retinopathies claim 37 , or benign or malignant (cancerous) tumours claim 37 , comprising administering to a mammal in need thereof an effective amount of at least one compound of general formula (I) according to .39) A method for the prevention and treatment of mammals claim 37 , in particular humans claim 37 , suffering from pathological angiogenesis claim 37 , in particular retinopathies claim 37 , or benign or malignant (cancerous) tumours claim 37 , comprising administering to a mammal in need thereof an effective amount of at least one compound of general formula (I) according to claim 37 , as a protein phosphatase 1 inhibitor claim 37 , vascular-disrupting agent and antiproliferative agent.40) A method for the prevention and treatment of mammals claim 37 , in particular humans claim 37 , suffering from pathological angiogenesis claim 37 , in particular retinopathies claim 37 , or benign or malignant (cancerous) tumours claim 37 , comprising administering to a mammal in need thereof an effective amount of at least one compound of general formula (I) according to claim 37 , as a tubulin polymerization inhibitor claim 37 , vascular-disrupting agent and antiproliferative agent.41) A method for the prevention and treatment of mammals claim 37 , in particular humans claim 37 , suffering from pathological angiogenesis claim 37 , in particular retinopathies claim 37 , or benign or malignant (cancerous) tumours claim 37 , comprising administering to a mammal in need thereof an effective amount of at least one compound of general formula (I) according to ...

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18-04-2013 дата публикации

DOXEPIN TRANS ISOMERS AND ISOMERIC MIXTURES AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS

Номер: US20130096188A1
Принадлежит:

The invention relates to use of the trans-(E) isomer or isomeric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders 1. A method for the treatment of a patient suffering from insomnia comprising administering to said patient doxepin , a pharmaceutically-acceptable salt or a prodrug thereof in a daily dosage ranging from about 0.0001 to about 499 milligrams , wherein the doxepin , the salt or the prodrug is a geometric isomer mixture containing about 88.3% to about 100.0% of the trans-(E) isomer or is 100% trans-(E) isomer.2. The method of claim 1 , wherein said geometric isomer mixture contains more than 90% of the trans-(E) isomer.3. The method of claim 1 , wherein said geometric isomer mixture contains more than 95% of the trans-(E) isomer.4. The method of claim 1 , wherein said geometric isomer mixture contains more than 98% of the trans-(E) isomer.5. The method of claim 1 , wherein said geometric isomer mixture contains more than 99% of the trans-(E) isomer.6. The method of claim 1 , wherein said geometric isomer mixture contains at least 99.5% or 99.9% of the trans-(E) isomer.7. The method of claim 1 , wherein said geometric isomer mixture contains 100.0% of the trans-(E) isomer.8. The method of claim 1 , wherein said geometric isomer mixture contains about 89% to about 99.9% of the trans-(E) isomer.9. The method of claim 1 , wherein the daily dosage is about 0.01 to about 20 milligrams.10. A composition comprising a pharmaceutically-acceptable carrier and doxepin claim 1 , a pharmaceutically-acceptable salt of doxepin claim 1 , or a prodrug of doxepin in a unit dosage form of about 0.0001 milligrams to about 499 milligrams claim 1 , wherein the doxepin claim 1 , the salt or the prodrug is a geometric isomer mixture containing about 88.3% to about 100.0% of the ...

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25-04-2013 дата публикации

COMPOSITIONS OF BOTANICAL EXTRACTS FOR CANCER THERAPY

Номер: US20130101616A1
Принадлежит:

Methods and compositions for prevention and therapy of cancer are provided. Compositions comprising therapeutically effective amounts of two or more of an extract of , an extract of and an extract of and optionally a therapeutically effective amount of an extract of are provided. Novel synergistic effects of the use of these compounds in combination therapy are disclosed. Embodiments further comprising therapeutically effective amounts of at least one chemotherapeutic agent are also provided. 153-. (canceled)54Ganoderma lucidumSalvia miltiorrhizaScutellaria barbata. An anticancer composition comprising two or more of an organic extract of , an organic extract of and an organic extract of , wherein each extract comprises a therapeutically effective amount.55Ganoderma lucidumScutellaria barbata.. The composition of claim 54 , wherein the composition comprises about 10 to about 50 percent by weight of the composition the extract of and/or about 10 to about 50 percent by weight of the composition the extract of56Ganoderma lucidum, Salvia miltiorrhizaScutellaria barbata. The composition of claim 54 , wherein the organic extract of claim 54 , or is an ethyl acetate extract claim 54 , an alcohol extract claim 54 , a methylene chloride extract claim 54 , or a methanol extract.57. The composition of claim 54 , wherein the composition displays at least one property selected from the group consisting of: anti-inflammatory activity claim 54 , immunoboosting activity claim 54 , inducing lymphocytes to release TNF-alpha claim 54 , and accelerating cell proliferation.58. The composition of claim 54 , wherein the composition selectively inhibits COX-2 over COX-1.59Hippophae rhamnoides.. The composition of further comprising an extract of60. The composition of further comprising a therapeutically effective amount of at least one chemotherapeutic agent.61. The composition of claim 60 , wherein the chemotherapeutic agent perturbs microtubule polymerization.62. The composition of claim ...

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25-04-2013 дата публикации

CHOLESTANOL DERIVATIVE FOR COMBINED USE

Номер: US20130101679A1
Принадлежит:

The invention provides a cancer chemotherapeutic agent which has fewer side effects and excellent efficacy. The cancer chemotherapeutic agent of the invention includes a cholestanol derivative represented by formula (1): 2. A cancer chemotherapeutic agent according to claim 1 , wherein claim 1 , in formula (1) claim 1 , G is GlcNAc-Gal- or GlcNAc-.3. A cancer chemotherapeutic agent according to or claim 1 , wherein the anti-cancer agent is one or more species selected from the group consisting of a taxane anti-cancer agent claim 1 , a platinum complex anti-cancer agent claim 1 , a pemetrexed compound claim 1 , and fluorouracil.4. A cancer chemotherapeutic agent according to claim 3 , wherein the anti-cancer agent is one or more species selected from the group consisting of Paclitaxel claim 3 , Docetaxcel claim 3 , Pemetrexed claim 3 , 5-FU claim 3 , Cisplatin claim 3 , Oxaliplatin claim 3 , Cyclophosphamide claim 3 , and Irinotecan.5. A cancer chemotherapeutic agent according to any of to claim 3 , which is a compounding agent.6. A cancer chemotherapeutic agent according to any of to claim 3 , which is in the form of a kit including a drug containing a cholestanol derivative and a drug containing an anti-cancer agent.7. A cancer chemotherapeutic agent according to claim 6 , wherein the drug containing a cholestanol derivative is a liposomal formulation.10. A cancer chemotherapy according to claim 9 , wherein the cholestanol derivative or a cyclodextrin inclusion compound thereof and the anti-cancer agent are administered to a patient in need thereof simultaneously claim 9 , or separately and intermittently. 1. Field of the InventionThe present invention relates to a chemotherapeutic agent for cancer (hereinafter referred to as a “cancer chemotherapeutic agent”) and, more particularly, to a cancer chemotherapeutic agent employing a cholestanol derivative and an anti-cancer agent in combination.2. Background ArtA variety of anti-cancer agents used in chemotherapy for ...

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25-04-2013 дата публикации

METHODS, COMPOSITIONS AND ARTICLES OF MANUFACTURE FOR CONTRIBUTING TO THE TREATMENT OF CANCERS

Номер: US20130102543A1
Принадлежит:

Methods, compositions and articles of manufacture for contributing to the treatment of cancers, including solid tumors, are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ET) to enhance the delivery and resulting efficacy of a chemotherapeutic agent. 1. A method of selectively increasing delivery of a chemotherapeutic agent to a prostate tumor comprising administering to a mammal in need thereof an IRL-1620 and a chemotherapeutic agent.2. The method according to claim 1 , wherein said IRL-1620 selectively increases blood flow to said prostate tumor thereby increasing said delivery of said chemotherapeutic agent to said prostate tumor.3. The method according to claim 1 , wherein the pharmacokinetic properties of said chemotherapeutic agent are not affected by said IRL-1620.4. The method according to claim 1 , wherein said IRL-1620 enhances the efficacy of said chemotherapeutic agent.5. The method according to claim 1 , wherein said IRL-1620 and said chemotherapeutic agent are administered simultaneously.6. The method according to claim 1 , wherein said IRL-1620 and said chemotherapeutic agent are administered sequentially.7. The method according to claim 6 , wherein said IRL-1620 is administered at least 15 minutes before said chemotherapeutic agent.8. The method according to claim 6 , wherein said IRL-1620 is administered about 15 minutes to about 120 minutes before said chemotherapeutic agent.9. The method according to claim 6 , wherein said IRL-1620 is administered about 15 minutes to about 60 minutes before said chemotherapeutic agent.10. The method according to claim 6 , wherein said IRL-1620 is administered about 15 minutes to about 30 minutes before said chemotherapeutic agent.11. The method according to claim 1 , wherein said chemotherapeutic agent is adriamycin claim 1 , camptothecin claim 1 , carboplatin claim 1 , cisplatin claim 1 , daunorubicin claim 1 , doxorubicin claim 1 , alpha interferon claim 1 ...

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25-04-2013 дата публикации

DOXEPIN ISOMERS AND ISOMERIC MIXTURES AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS

Номер: US20130102658A1
Принадлежит:

The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders 1. A method for the treatment of a patient suffering from insomnia comprising administering to said patient doxepin , a pharmaceutically-acceptable salt or a prodrug thereof in a daily dosage ranging from about 0.0001 to about 499 milligrams , wherein the doxepin , the salt or the prodrug is a geometric isomer mixture containing about 18.2% to about 100.0% of the cis-(Z) isomer or is 100% cis-(Z) isomer.2. The method of claim 1 , wherein said geometric isomer mixture contains more than 20% of the cis-(Z) isomer.3. The method of claim 1 , wherein said geometric isomer mixture contains more than 50% of the cis-(Z) isomer.4. The method of claim 1 , wherein said geometric isomer mixture contains more than 90% of the cis-(Z) isomer.5. The method of claim 1 , wherein said geometric isomer mixture contains more than 95% of the cis-(Z) isomer.6. The method of claim 1 , wherein said geometric isomer mixture contains about 20% to about 99.9% of the cis-(Z) isomer.7. The method of claim 1 , wherein the daily dosage is about 0.01 to about 20 milligrams.8. A composition comprising a pharmaceutically-acceptable carrier and doxepin claim 1 , a pharmaceutically-acceptable salt of doxepin claim 1 , or a prodrug of doxepin in a unit dosage form of about 0.0001 milligrams to about 499 milligrams claim 1 , wherein the doxepin claim 1 , the salt or the prodrug is a geometric isomer mixture containing about 18.2% to about 100.0% of the cis-(Z) isomer or is 100% cis-(Z) isomer.9. The composition of claim 8 , wherein said geometric isomer mixture contains about 20% to about 99.9% of the cis-(Z) isomer.10. The composition of claim 8 , wherein the unit dosage form is about 0.1 to ...

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09-05-2013 дата публикации

METHODS FOR TREATING HEPATOCELLULAR CARCINOMA

Номер: US20130115296A1
Автор: Wong Nathalie, Yeo Winnie
Принадлежит:

The present invention provides methods and compositions for treating hepatocellular carcinoma (HCC) by administering a composition comprising nanoparticles that comprise a taxane and an albumin. The invention also provides combination therapy methods of treating HCC comprising administering to an individual an effective amount of a composition comprising nanoparticles that comprise a taxane and an albumin and another agent, such as an agent that inhibits microtubule disassembly. 1. A method of treating hepatocellular carcinoma (HCC) in an individual in need thereof , comprising administering to the individual an effective amount of a composition comprising nanoparticles comprising a taxane and an albumin.2. The method of claim 1 , further comprising administering to the individual an effective amount of at least one other agent claim 1 , wherein said other agent inhibits microtubule disassembly.3. The method of claim 2 , wherein the nanoparticle composition and the other agent are administered simultaneously or sequentially.4. The method of claim 2 , wherein the nanoparticle composition and the other agent are administered concurrently.5. The method of claim 2 , wherein the other agent inhibits a molecule that promotes microtubule disassembly directly or indirectly.6. The method of claim 2 , wherein the other agent inhibits a molecule selected from the group consisting of ABP1 claim 2 , ARHGAP4 claim 2 , HSPA8 claim 2 , LCP1 claim 2 , PACSIN2 claim 2 , RUNX1T1 claim 2 , STMN1 claim 2 , and Tubulin claim 2 , and TUBB4.7. The method of claim 6 , wherein the other agent is an inhibitor of STMN1.8. The method of claim 7 , wherein the other agent is an siRNA against STMN1.9. The method of claim 7 , wherein the other agent is a gamboge or a derivative thereof.10. The method of claim 2 , wherein the other agent activates a molecule that promotes microtubule assembly directly or indirectly.11. The method of claim 2 , wherein the other agent activates a molecule selected ...

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09-05-2013 дата публикации

COMBINATION THERAPIES FOR TREATING NEUROLOGICAL DISORDERS

Номер: US20130116215A1
Принадлежит:

The invention features novel pharmaceutical combinations useful for the treatment of neurological diseases, specifically neurodegenerative diseases. The novel pharmaceutical combinations of the invention demonstrate additive or synergistic effect in silico and in vivo. The invention also relates to methods of treatment of neurological and neurodegenerative diseases including the pharmaceutical combinations of the invention. 1Ginkgo biloba. A pharmaceutical composition comprising a therapeutically-effective amount of at least two or more compounds or an acceptable salt thereof , selected from the group including L-Glutamine , Biotin , L-Lysine , Vitamin C , L-Leucine , L-Methionine , L-Alanine , L-Isoleucine , Methadone , Methoxyflurane , Tacrolimus , Alfentanil , Aspirin , Halothane , Danazol , Estriol , Acetic Acid , Adenosine monophosphate , Arsenic trioxide , Atropine , Azelaic Acid , Chloroprocaine , Dimethyl sulfoxide , Ethanol , Fludarabine , Fomepizole , Isoflurane , L-Carnitine , Praziquantel , Promethazine , Rifampin , Spermine , Terfenadine , Vitamin E , Acarbose , Acetohydroxamic Acid , Aciclovir , Adenine , Adenosine triphosphate , Alclometasone , Alemtuzumab , Alendronate , Alpha-Linolenic Acid , Amifostine , Amlexanox , Amlodipine , Amodiaquine , Amrinone , Aspartame , Astemizole , Atazanavir , Atorvastatin , Atovaquone , Bacitracin , Balsalazide , Beclomethasone , Buclizine , Calcitriol , Cefadroxil , Cefalotin , Cefazolin , Cefdinir , Cefepime , Cefonicid , Cefoperazone , Cetuximab , Chloramphenicol , Chlorpheniramine , Cinnarizine , Ciprofloxacin , Clofarabine , Clopidogrel , Clotrimazole , Cloxacillin , Cocaine , Cyanocobalamin , Cyclizine , Cycloserine , Cyclosporine , Cyclothiazide , Cyproheptadine , Dapsone , Daunorubicin , Diethylstilbestrol , Dipyridamole , Disulfuram , Dofetilide , Enflurane , Enfuvirtide , Enoxacin , Enprofylline , Epinastine , Ertapenem , Ethchlorvynol , Ezetimibe , Felodipine , Fenofibrate , Flucytosine , Flumethasone ...

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16-05-2013 дата публикации

TRIAZOLOPYRIDINE DERIVATIVES

Номер: US20130121994A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors in which R, R, R, R, and Rare as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds. 5. The compound according to which is selected from the group consisting of:4-{[6-(4-hydroxy-3,5-dimethylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]amino}-3-methoxybenzonitrile;4-{2-[(2,4-dimethoxyphenyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;4-{2-[(2-methoxyphenyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;2,6-dimethyl-4-[2-(pyrimidin-5-ylamino)[1,2,4]triazolo[1,5-a]pyridin-6-yl]phenol;4-{2-[(2,5-dimethoxyphenyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;4-{2-[(5-fluoro-2-methoxyphenyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;2-{[6-(4-hydroxy-3,5-dimethylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]amino}benzonitrile;2,6-dimethyl-4-[2-(pyridin-3-ylamino)[1,2,4]triazolo[1,5-a]pyridin-6-yl]phenol;2,6-dimethyl-4-(2-{[4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenol;2,6-dimethyl-4-(2-{[2-(trifluoromethoxy)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenol;4-{[6-(4-hydroxy-3,5-dimethylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]amino}benzonitrile;4-{2-[(2-ethoxyphenyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;3-{[6-(4-hydroxy-3,5-dimethylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]amino}-4-methoxybenzonitrile;4-{2-[(3-methoxypyridin-2-yl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}-2,6-dimethylphenol;4-{[6-(4-hydroxy-3,5-dimethylphenyl)[1,2,4]triazolo[1,5-a]pyridin-2-yl]amino}-N-methylbenzamide;N,N-Diethyl-4-[6-( ...

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16-05-2013 дата публикации

Prodrug compositions, prodrug nanoparticles, and methods of use thereof

Номер: US20130122100A1
Принадлежит: Washington University in St Louis WUSTL

Nanoparticles comprising a prodrug and prodrugs linked to phospholipids, wherein the linkages facilitate release of the prodrugs from the nanoparticles to sites within a target cell or cell membrane by fusion of the particle and the cell membrane are disclosed. Also disclosed are methods for producing and using the nanoparticles and their constituents.

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16-05-2013 дата публикации

ANTITUMORAL COMBINATION COMPRISING OMBRABULIN, A TAXANE DERIVATIVE AND A PLATINUM DERIVATIVE

Номер: US20130122113A1
Принадлежит: SANOFI

The invention concerns an antitumoral combination comprising ombrabulin, a taxane derivative and a platinum derivative and its use in the treatment of advanced solid tumors. 1. A combination of antitumoral agents , wherein said antitumoral agents comprise ombrabulin , a taxane derivative and a platinum derivative , said ombrabulin , said taxane derivative and said platinum derivative each being in the form of a free base , of an addition salt with a pharmaceutically acceptable acid , of a hydrate , or of a solvate , wherein said combination is well tolerated , does not exacerbate the toxicity of each of the antitumoral agents , and allows the treatment of advanced solid tumors either by stabilizing or a tumor or by inducing a partial or a complete regression of a tumor.2. The combination according to wherein ombrabulin is in the form of the hydrochloride salt.3. The combination according to wherein the taxane derivative is chosen from paclitaxel and docetaxel.4. The combination according to wherein the platinum derivative is chosen from cisplatin and carboplatin.5. The combination according to wherein ombrabulin is in combination with docetaxel and cisplatin or in combination with paclitaxel and carboplatin.6. The combination according to comprising an effective quantity of ombrabulin claim 1 , an effective quantity of a taxane derivative and an effective quantity of a platinum derivative.7. The combination according to wherein ombrabulin is administered at a dose of between 15 and 35 mg/m.8. The combination according to wherein ombrabulin is administered at a dose chosen from 15.5 claim 7 , 20 claim 7 , 25 claim 7 , 30 and 35 mg/m.9. The combination according to wherein the taxane derivative is docetaxel and is administered at a dose of 60 or 75 mg/m.10. The combination according to wherein the taxane derivative is paclitaxel and is administered at a dose of 175 or 200 mg/m.11. The combination according to wherein the platinum derivative is cisplatin and is ...

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16-05-2013 дата публикации

Synergistic Anti-Cancer Activity of SR16388 with Anti-Mitotic Drugs

Номер: US20130123222A1
Автор: Lidia Sambucetti, Wei Zhou
Принадлежит: SRI International Inc

The invention provides methods and compositions for inhibiting tumor growth in a mammal. The methods comprise administering to the mammal a synergistic combination of (E)-3-hydroxy-21-[2′-(N,N-dimethylamino)ethoxy]-19-norpregna-1,3,5(10),17(20)-tetraene and a microtubulin inhibitor like paclitaxel or vincristine. The combination of the compounds more than additively inhibits growth of tumor cells.

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16-05-2013 дата публикации

Tricyclic Compounds and Methods of Making and Using Same

Номер: US20130123235A1
Принадлежит: Individual

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

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16-05-2013 дата публикации

Balloon catheter coated with an anti-restenotic active ingredient and a molecular dispersion agent that promotes transport

Номер: US20130123695A1
Принадлежит: HEMOTEQ AG

The present invention relates to balloon catheters with or without crimped stent, whose surface is coated with at least one antirestenotic agent and at least one transport promoting molecular dispersant, as well as a method for the preparation of these medical devices.

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23-05-2013 дата публикации

Combination Cancer Therapies with Wortmannin Analogs

Номер: US20130129720A1
Принадлежит: Oncothyreon Inc.

Provided herein are combination therapies for the treatment of certain cancers in a subject by administering a combination of a therapeutic and a wortmannin analog to that subject. 2. The method of claim 1 , wherein the cancer is selected from the group consisting of head and neck cancer claim 1 , lung cancer claim 1 , ovarian cancer claim 1 , liver cancer claim 1 , colon cancer claim 1 , breast cancer claim 1 , pancreatic cancer claim 1 , kidney cancer claim 1 , cervical cancer claim 1 , uterine cancer claim 1 , prostate cancer claim 1 , esophageal cancer and gastric cancer.3. The method of claim 1 , wherein the cancer is non-small cell lung cancer or head and neck squamous cell carcinoma.4. The method of further comprising pretreating the subject with a corticosteroid prior to administration of the compound and docetaxel.5. The method of further comprising administering an additional anti-mitotic claim 1 , platinum therapy or both.6. The method of further comprising an anti-emetic claim 1 , anti-diarrheal or both.7. The method of further comprising preselecting the subject having completed first-line anti-cancer therapy.8. The method of further comprising evaluating the treated subject claim 1 , wherein the evaluation comprises determining at least one of: (a) tumor size claim 1 , (b) tumor location claim 1 , (c) nodal stage claim 1 , (d) growth rate of the cancer claim 1 , (e) survival rate of the subject claim 1 , (f) changes in the subject's cancer symptoms claim 1 , (g) changes in the subject's Prostate Specific Antigen (PSA) concentration claim 1 , (h) changes in the subject's PSA concentration doubling rate claim 1 , (i) changes in the subject's biomarkers claim 1 , or (i) changes in the subject's quality of life.10. The method of claim 9 , wherein the compound is administered at a dose and frequency sufficient to result in one or more of the following: 1) 17-hydroxy metabolite between about 500 pg/mL and about 2500 pg/mL (peak) within about 1-3 hours of ...

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23-05-2013 дата публикации

Humanized anti-egfl7 antibodies and methods using same

Номер: US20130129733A1
Принадлежит: Genentech Inc

The present invention concerns antibodies to EGFL7 and the uses of same.

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23-05-2013 дата публикации

HUMANIZED ANTI-EGFL7 ANTIBODIES AND METHODS USING SAME

Номер: US20130129749A1
Принадлежит: Genentech, Inc.

The present invention concerns antibodies to EGFL7 and the uses of same. 1. A method of enhancing efficacy of an anti-angiogenesis agent in a subject having a pathological condition associated with angiogenesis , the method comprising administering to an individual in need of such treatment an effective amount of an anti-EGFL7 antibody , the antibody comprising the following hypervariable region (HVR) sequences:{'sub': 1', '2', '3', '4', '5', '1', '2', '3', '4', '5, '(i) HVR-L1 comprising KXSXSXDYXGDSYXS, wherein Xis A or R; Xis H or Q; Xis G or V; Xis selected from the group consisting of D, L, R, S, and W; and Xis M or V (SEQ ID NO: 210);'}{'sub': 1', '2', '3', '1', '2', '3, '(ii) HVR-L2 comprising GASXXEX, wherein Xis N or Y; Xis selected from the group consisting of L, R and Y; and Xis Q or S (SEQ ID NO: 211);'}{'sub': 1', '2', '1', '2, '(iii) HVR-L3 comprising QQNNEXPXT, wherein Xis D or E; and Xis F or Y (SEQ ID NO: 212);'}{'sub': 1', '2', '3', '4', '5', '1', '2', '3', '4', '5, '(iv) HVR-H1 comprising GXXXXTYGXS, wherein Xis H or V; Xis R or T; Xis selected from the group consisting of F, G, R, and S; Xis selected from the group consisting of D, G, R, and T; and Xis M or Y (SEQ ID NO: 213);'}{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '1', '2', '3', '4', '5', '6', '7', '8, '(v) HVR-H2 comprising GWINXXSGVPTXAXXXXX, wherein Xis selected from the group consisting of I, M, T, and W; Xis H or R; Xis selected from group consisting of I, M, T, and Y; Xis D or H; Xis selected from group consisting of D, M and T; Xis F or Y; Xis K or S; and Xis G or R (SEQ ID NO: 214, and'}{'sub': 1', '2', '3', '1', '2', '3, '(vi) HVR-H3 comprising AXLGSXAVDX, wherein Xis N or R; Xis selected from the group consisting of C, R, H, and Y; and Xis A or Y (SEQ ID NO: 215).'}2. A method of enhancing efficacy of an anti-angiogenesis agent in a subject having a pathological condition associated with angiogenesis , the method comprising administering to an individual in need of such ...

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23-05-2013 дата публикации

COMBINATION THERAPY USING A RUTHENIUM COMPLEX

Номер: US20130129840A1
Принадлежит: Niiki Pharma Inc.

A combination therapy is disclosed for treating cancer. The method comprises administering to a cancer patient a therapeutically effective amount of trans-[tetrachlorobis(1H-indazole)ruthenate(III)] or a pharmaceutically acceptable salt thereof, and administering to the patient a therapeutically effective amount of one or more other anti-cancer agents as disclosed herein. 1. A method of treating cancer , comprising:administering to a patient in need of treatment, simultaneously or sequentially (1) a pharmaceutically acceptable salt of trans-[tetrachlorobis(1H-indazole)ruthenate(III)], and (2) one or more anti-cancer agents chosen from the group consisting of platinum agents, taxane, anthracyclines, 5-FU and prodrugs thereof, nitrosourea compounds, gemcitabine, temozolomide, EGFR inhibitors, mTOR inhibitors, sorafenib, regorafenib, and sunitinib.2. The method of claim 1 , wherein said pharmaceutically acceptable salt of trans-[tetrachlorobis(1H-indazole)ruthenate(III)] is sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)].3. The method of claim 2 , wherein said one or more anti-cancer agents includes a platinum agent.4. The method of claim 3 , wherein said platinum agent is cisplatin claim 3 , carboplatin claim 3 , or oxaliplatin.5. The method of claim 2 , wherein said one or more anti-cancer agents includes an anthracycline.6. The method of claim 5 , wherein said anthracycline is doxorubicin.7. The method of claim 2 , wherein said one or more anti-cancer agents includes 5-FU or a prodrug thereof.8. The method of claim 2 , wherein said one or more anti-cancer agents includes a nitrosourea compound.9. The method of claim 8 , wherein said nitrosourea compound is BCNU.10. The method of claim 2 , wherein said one or more anti-cancer agents includes gemcitabine.11. The method of claim 2 , wherein said one or more anti-cancer agents includes temozolomide.12. The method of claim 2 , wherein said one or more anti-cancer agents includes an EGFR inhibitor.13. The method ...

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23-05-2013 дата публикации

THERAPEUTIC COMBINATION COMPRISING A PARP-1 INHIBITOR AND AN ANTI-NEOPLASTIC AGENT

Номер: US20130129841A1
Принадлежит: NERVIANO MEDICAL SCIENCES S.R.L.

The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an antimitotic agent and radiation wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof. 2. A combination according to claim 1 , wherein the alkylating or alkylating-like agent is selected from the group consisting of Carboplatin claim 1 , Cisplatin claim 1 , Temozolomide claim 1 , Dacarbazine.3. A combination according to claim 1 , wherein the antimetabolite is Gemcitabine.4. A combination according to claim 1 , wherein the topoisomerase I inhibitor is selected from the group consisting of Irinotecan and Topotecan.5. A combination according to claim 1 , wherein the topoisomerase II inhibitor is nemorubicin.6. A combination according to claim 1 , wherein the antimitotic agent is selected from the group consisting of Paclitaxel and Docetaxel.76. A combination according to claim 1 , wherein in formula (I):{'sub': 1', '2', '1', '2, '(i): when R is hydrogen atom, then Rand Rare both fluorine atoms and, when R is fluorine atom, then Rand Rare both chlorine atoms, fluorine atoms or together form an oxo group (=O), or'}{'sub': 1', '2, '(ii): R is hydrogen atom or fluorine atom, and Rand Rare both fluorine atoms, or'}{'sub': 1', '2, '(iii): R, Rand Rare all fluorine atoms.'}87. A combination according to claim 1 , wherein the compound of formula (I) is selected from the group consisting of:2-[1-(4,4-difluorocyclohexyl)piperidin-4-yl]-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide;2-[1-(4,4-difluorocyclohexy)piperidin-4-yl]-6-fluoro-3 -oxo-2,3-dihydro-1H-isoindole-4-carboxamide;6-fluoro-3-oxo-2-[1-(4-oxocyclohexy)piperidin-4-yl]-2,3-dihydro-1H-isoindole-4- ...

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23-05-2013 дата публикации

Cyclodextrin-based polymers for therapeutics delivery

Номер: US20130131013A1
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.

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30-05-2013 дата публикации

NOVEL MUTATED HUMANIZED 12G4 ANTIBODIES AND THE FRAGMENTS THEREOF AGAINST THE HUMAN ANTI-MULLERIAN HORMONE RECEPTOR TYPE II

Номер: US20130136743A1
Принадлежит:

Novel mutated humanized 12G4 antibodies, and fragments thereof, directed against the anti-Müllerian hormone type II receptor. 1. Humanized 12G4 monoclonal antibody comprising or consisting of: a variable region the amino acid sequence of which is represented by SEQ ID NO: 2 or SEQ ID NO: 4, and', 'a constant region the amino acid sequence of which is represented by SEQ ID NO: 6 or by a sequence having at least 80% homology with SEQ ID NO: 6,, 'a) a light chain comprising or consisting of a variable region the amino acid sequence of which is represented by SEQ ID NO: 8, or SEQ ID NO: 10, and', 'a constant region the amino acid sequence of which is represented by SEQ ID NO: 12 or by a sequence having at least 80% homology with SEQ ID NO: 12,, 'b) a heavy chain comprising or consisting of{'sub': 'D', 'claim-text': a variable region the amino acid sequence of which is represented by SEQ ID NO: 14, and', 'a constant region the amino acid sequence of which is represented by SEQ ID NO: 6,, 'said humanized 12G4 monoclonal antibody is mutated, comprises at least one mutation in the light and/or heavy chain, and has a Kfor the human anti-Müllerian hormone type II receptor (AMHRII) at least equal to that of the chimeric 12G4 monoclonal antibody comprising or consisting of a variable region the amino acid sequence of which is represented by SEQ ID NO: 18, or SEQ ID NO: 10, and', 'a constant region the amino acid sequence of which is represented by SEQ ID NO: 12,, 'b) a heavy chain consisting of{'sup': −9', '−8', '−9', '−11, 'for said receptor, preferably below 10M, in particular below 10M, in particular in the range from 10M to 10M.'}2. Mutated humanized 12G4 monoclonal antibody according to claim 1 , comprising at least one mutation in at least one CDR of the variable region of the light chain claim 1 , and having an affinity for said receptor at least equal to that of said chimeric 12G4 monoclonal antibody.3. Mutated humanized 12G4 monoclonal antibody according to claim 1 , ...

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30-05-2013 дата публикации

Crystal Forms of Kinase Inhibitors

Номер: US20130136804A1
Принадлежит: AbbVie Inc.

N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer. 122-. (canceled)24. The method of claim 23 , wherein the solution is administered by a parenteral route.25. The method of claim 23 , further comprising administering 5-azacitidine claim 23 , docetaxel claim 23 , cisplatin claim 23 , or carboplatin.27. The method of claim 26 , wherein the solution is administered by a parenteral route.28. The method of claim 26 , further comprising administering 5-azacitidine claim 26 , docetaxel claim 26 , cisplatin claim 26 , or carboplatin.30. The method of claim 29 , wherein the solid dispersion is administered by an oral route.31. The method of claim 29 , further comprising administering 5-azacitidine claim 29 , docetaxel claim 29 , cisplatin claim 29 , or carboplatin.33. The method of claim 32 , wherein the solid dispersion is administered by an oral route.34. The method of claim 32 , further comprising administering 5-azacitidine claim 32 , docetaxel claim 32 , cisplatin claim 32 , or carboplatin. This application claims priority to U.S. Provisional Application Ser. No. 61/353,058 filed Jun. 9, 2010, which is incorporated by reference in its entirety.The present invention relates to crystalline forms of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea, processes for preparing the crystalline forms, pharmaceutical formulations thereof, and methods of treating cancer.Mitosis is a process by which a complete copy of a duplicated genome is segregated by the microtuble spindle apparatus into two daughter cells. Aurora-kinases, key mitotic regulators required for genome stability, have been found to be overexpressed in human tumors. There is therefore an existing need in the therapeutic arts for ...

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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06-06-2013 дата публикации

METHOD OF TREATING TUMOR RESISTANT TO HERCEPTIN OR PACLITAXEL USING FOXM1 INHIBITORS AND DETECTING SAME

Номер: US20130142784A1

The invention provides methods of treating cancer, especially breast cancer, and in particular HER2/ErbB2 positive breast cancer using a FoxM1 inhibitor in conjunction with trastuzumab and/or paclitaxel. Pharmaceutical compositions comprising a FoxM1 inhibitor in the presence of trastuzumab and/or paclitaxel are also provided. The invention further provides methods of identifying and treating trastuzumab resistant and/or paclitaxel resistant cancer. Also provided are methods of promoting breast tumor cell differentiation. 196-. (canceled)97. A pharmaceutical composition for inhibiting tumor growth comprising a combination of a FoxM1 inhibitor and trastuzumab or paclitaxel or both trastuzumab and paclitaxel , wherein the combination is in a therapeutically effective amount , and a pharmaceutically acceptable excipient , diluent or carrier.98. The pharmaceutical composition of wherein the combination comprises a FoxM1 inhibitor and trastuzumab and paclitaxel.99. The pharmaceutical composition of wherein the FoxM1 inhibitor comprises an inhibitory P19ARF peptide.100. The pharmaceutical composition of wherein the inhibitory P19ARF peptide comprises a peptide having the sequence of SEQ ID NO:6 or SEQ ID NO:7.101. The pharmaceutical composition of wherein the FoxM1 inhibitor comprises a FoxM1-specific siRNA.102. The pharmaceutical composition of claim 101 , wherein the FoxM1-specific siRNA comprises a polynucleotide having the sequence of SEQ ID NO:8 claim 101 , SEQ ID NO:9 claim 101 , SEQ ID NO:10 claim 101 , or SEQ ID NO:11.103. The pharmaceutical composition of wherein the FoxM1 inhibitor comprises a thiazole antibiotic.104. The pharmaceutical composition of claim 103 , wherein the thiazole antibiotic is siomycin A or thiostrepton.105. The pharmaceutical composition of wherein the FoxM1 inhibitor is an antioxidant.106. The pharmaceutical composition of wherein the antioxidant is N-acetyl-L-cysteine (NAC) claim 105 , catalase claim 105 , 4-Hydroxy-2 claim 105 ,2 claim ...

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06-06-2013 дата публикации

FIXED DOSING OF HER ANTIBODIES

Номер: US20130142865A1
Принадлежит: Genentech, Inc.

The present invention concerns fixed dosing of HER antibodies, such as Pertuzumab. 1. A method for treating cancer comprising administering one or more fixed dose(s) of a HER antibody to a human patient in an amount effective to treat the cancer.2. The method of wherein the antibody binds to a HER receptor selected from the group consisting of EGFR claim 1 , HER2 claim 1 , and HER3.3. The method of wherein the antibody binds to HER2.4. The method of wherein the HER2 antibody binds to Domain II of HER2 extracellular domain.5. The method of wherein the antibody binds to a junction between domains I claim 1 , II and III of HER2 extracellular domain.6. The method of wherein the HER antibody inhibits heterodimerization of HER2 with EGFR or HER3.7. The method of wherein the HER antibody comprises the variable light and variable heavy amino acid sequences in SEQ ID Nos. 3 and 4 claim 1 , respectively.8. The method of wherein the HER antibody is pertuzumab.9. The method of wherein the fixed dose is in the range from about 20 mg to about 2000 mg of the HER antibody.10. The method of wherein the fixed dose is selected from the group consisting of approximately 420 mg claim 9 , approximately 525 mg claim 9 , approximately 840 mg claim 9 , and approximately 1050 mg of the HER antibody.11. The method of wherein the fixed dose is 420 mg of the HER antibody.12. The method of wherein the fixed dose is 840 mg of the HER antibody.13. The method of wherein the fixed dose is 1050 mg of the HER antibody.14. The method of wherein the fixed dose is 525 mg of the HER antibody.15. The method of wherein a fixed dose of the HER antibody is administered to the patient approximately every week claim 1 , approximately every 2 weeks claim 1 , approximately every 3 weeks claim 1 , or approximately every 4 weeks.16. The method of wherein a fixed dose of the HER antibody is administered to the patient approximately every 3 weeks.17. The method of comprising administering a loading dose of ...

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06-06-2013 дата публикации

CHEMO- AND RADIATION-SENSITIZATION OF CANCER BY ANTISENSE TRPM-2 OLIGODEOXYNUCLEOTIDES

Номер: US20130143944A1
Принадлежит: The University of British Columbia

Administration of antisense oligodeoxynucleotides (ODN) targeted against the testosterone-repressed prostate message-2 (TRPM-2) gene can reduce the amount of TRPM-2 in renal cell cancer (RCC) cells and other cancer cells, and as a result enhance chemosensitivity of these cells to chemotherapy agents and radiation. Thus, for example, the sensitivity of renal cell cancer cells to a chemotherapeutic agent can be increased by exposing renal cell cancer cells to a chemotherapeutic agent and an agent which reduces the amount of TRPM-2 in the renal cell cancer cells. This provides an improved method for treatment of renal cell cancer, which is generally resistant to treatment with known chemotherapy agents. 142-. (canceled)43. A method for treating an individual suffering from ovarian cancer comprising administering to said individual a therapeutically effective amount of an antisense oligodeoxynucleotide and chemotherapy comprising a taxane , wherein the antisense oligodeoxynucleotide has nucleotides in the sequence set forth in Seq. ID No. 4 and which antisense oligodeoxynucleotide comprises a phosphorothioate modification to increase the stability thereof in vivo , thereby treating said individual.44. A method for enhancing chemosensitivity in an individual suffering from ovarian cancer comprising administering to said individual a therapeutically effective amount of an antisense oligodeoxynucleotide and chemotherapy comprising a taxane , wherein the antisense oligodeoxynucleotide has nucleotides in the sequence set forth in Seq. ID No. 4 and which antisense oligodeoxynucleotide comprises a phosphorothioate modification to increase the stability thereof in vivo , thereby enhancing chemosensitivity in said individual.45. A method for treating an individual suffering from bladder cancer comprising administering to said individual a therapeutically effective amount of an antisense oligodeoxynucleotide and chemotherapy comprising a taxane , wherein the antisense ...

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06-06-2013 дата публикации

Absorbable crystalline copolyester-based bioactive hydroforming luminal liner compositions

Номер: US20130144264A1
Принадлежит: Individual

Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.

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13-06-2013 дата публикации

HUMANIZED ANTI-EGFL7 ANTIBODIES AND METHODS USING SAME

Номер: US20130149307A1
Принадлежит: Genentech, Inc.

The present invention concerns antibodies to EGFL7 and the uses of same. 1. A method for treating a tumor , a cancer , or a cell proliferative disorder , the method comprising administering to an individual in need of such treatment an effective amount of an anti-EGFL7 antibody , the antibody comprising the following hypervariable region (HVR) sequences:{'sub': 1', '2', '3', '4', '5', '1', '2', '3', '4', '5, '(i) HVR-L1 comprising KXSXSXDYXGDSYXS, wherein Xis A or R; Xis H or Q; Xis G or V; Xis selected from the group consisting of D, L, R, S, and W; and Xis M or V (SEQ ID NO: 210);'}{'sub': 1', '2', '3', '1', '2', '3, '(ii) HVR-L2 comprising GASXXEX, wherein Xis N or Y; Xis selected from the group consisting of L, R and Y; and Xis Q or S (SEQ ID NO: 211);'}{'sub': 1', '2', '1', '2, '(iii) HVR-L3 comprising QQNNEXPXT, wherein Xis D or E; and Xis F or Y (SEQ ID NO: 212);'}{'sub': 1', '2', '3', '4', '5', '1', '2', '3', '4', '5, '(iv) HVR-H1 comprising GXXXXTYGXS, wherein Xis H or V; Xis R or T; Xis selected from the group consisting of F, G, R, and S; Xis selected from the group consisting of D, G, R, and T; and Xis M or Y (SEQ ID NO: 213);'}{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '1', '2', '3', '4', '5', '6', '7', '8, '(v) HVR-H2 comprising GWINXXSGVPTXAXXXXX, wherein Xis selected from the group consisting of I, M, T, and W; Xis H or R; Xis selected from group consisting of I, M, T, and Y; Xis D or H; Xis selected from group consisting of D, M and T; Xis F or Y; Xis K or S; and Xis G or R (SEQ ID NO: 214, and'}{'sub': 1', '2', '3', '1', '2', '3, '(vi) HVR-H3 comprising AXLGSXAVDX, wherein Xis N or R; Xis selected from the group consisting of C, R, H, and Y; and Xis A or Y (SEQ ID NO: 215).'}2. A method for treating a tumor , a cancer , or a cell proliferative disorder , the method comprising administering to an individual in need of such treatment an effective amount of an anti-EGFL7 antibody , the antibody comprising the following HVR sequences: HVR-L1 ...

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13-06-2013 дата публикации

Compositions and Methods for Treatment of Cancer

Номер: US20130150310A1
Принадлежит: ArQule, Inc.

The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. 115-. (canceled)1716. The pharmaceutical composition of , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen , raloxifene , anastrozole , exemestane , letrozole , trastuzumab , imatinib , paclitaxel , cyclophosphamide , lovastatin , mimosine , gemcitabine , araC , 5-fluorouracil , methotrexate , docetaxel , goserelin , vinctristine , vinblastine , nocodazole , teniposide , etoposide , gemcitabine , epothilone , navelbine , camptothecin , daunorubicin , dactinomycin , mitoxantrone , amsacrine , doxorubicin , epirubicin or idarubicin.1826-. (canceled)28. The method of claim 27 , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen claim 27 , raloxifene claim 27 , anastrozole claim 27 , exemestane claim 27 , letrozole claim 27 , trastuzumab claim 27 , imatinib claim 27 , paclitaxel claim 27 , cyclophosphamide claim 27 , lovastatin claim 27 , mimosine claim 27 , gemcitabine claim 27 , araC claim 27 , 5-fluorouracil claim 27 , methotrexate claim 27 , docetaxel claim 27 , goserelin claim 27 , vinctristine claim 27 , vinblastine claim 27 , nocodazole claim 27 , teniposide claim 27 , etoposide claim 27 , gemcitabine claim 27 , epothilone claim 27 , navelbine claim 27 , camptothecin claim 27 , daunorubicin claim 27 , dactinomycin claim 27 , mitoxantrone claim 27 , amsacrine claim 27 , doxorubicin claim 27 , epirubicin or idarubicin.29. The method of wherein said treating said cell proliferative ...

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13-06-2013 дата публикации

PACLITAXEL/STEROIDAL COMPLEX

Номер: US20130150335A1

A paclitaxel/steroid complex comprising paclitaxel and steroid is disclosed. The molar ratio of paclitaxel to steroid is 1:0.2˜4, preferably 1:0.25˜2. A process for the preparation thereof and the use thereof in the manufacture of submicron emulsion, dry emulsion, self-microemulsifying system are also disclosed. 1. A paclitaxel steroid complex , wherein the complex is composed of paclitaxel and steroid with molar ratio of 1:0.2˜4.2. The paclitaxel steroid complex according to claim 1 , wherein the molar ratio of paclitaxel and steroid is 1:0.25˜2.3. The paclitaxel steroid complex according to claim 2 , wherein the molar ratio of paclitaxel and steroid is 1:0.33˜1.4. The paclitaxel steroid complex according to claim 1 , wherein said steroid is a natural steroid or a derivative thereof.5. The paclitaxel steroid complex according to claim 4 , wherein said natural steroid is selected from the group consisting of cholesterol claim 4 , 7-dehydrocholesterol claim 4 , lanosterol claim 4 , sitosterol claim 4 , brassicasterol claim 4 , mycosterol claim 4 , oysters steroid claim 4 , stigmasterol claim 4 , sitosterolum and ergosterol; said derivative is selected from the group consisting of cholic acid claim 4 , deoxycholic acid and anthropodesoxycholic acid.6. The paclitaxel steroid complex according to claim 1 , wherein said complex contains an antioxidant stabilizer.7. The paclitaxel steroid complex according to claim 6 , wherein said antioxidant stabilizer is selected from the group consisting of sodium bisulfate claim 6 , sodium metabisulfite claim 6 , vitamin C claim 6 , EDTA and its salts claim 6 , and vitamin E and its derivatives.8. A method for preparing a paclitaxel steroid complex according to said method comprising the following steps:a. mixing paclitaxel and steroid lipid materials in proportion, adding an organic solvent to dissolve, adding an antioxidant stabilizer; andb. stirring at a suitable temperature, removing the organic solvent, and vacuum drying.9. The ...

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13-06-2013 дата публикации

METHODS OF USING LOW-DOSE DOXEPIN FOR THE IMPROVEMENT OF SLEEP

Номер: US20130150434A1
Принадлежит: Somaxon Pharmaceuticals, Inc.

Methods of treating sleep disorders by administration of low doses of doxepin in individuals seeking sustained efficacy or in need of avoiding weight gain, rebound insomnia, or sedative tolerance resulting from doxepin treatment. 1. A method , comprising:identifying a patient in need of pharmaceutical treatment of a sleep disorder,evaluating the importance to that patient of selecting a pharmaceutical agent to minimize rebound insomnia as a side effect of pharmaceutical treatment of said sleep; and selecting doxepin therapy for treating the patient based at least in part on its low incidence of rebound insomnia, and then', 'treating said sleep disorder with doxepin or a pharmaceutically acceptable salt thereof in a daily dosage between about 0.5 milligram and 6 milligrams., 'avoiding rebound insomnia in said patient by2. The method of claim 1 , wherein the dosage of doxepin is about 1 milligram.3. The method of claim 1 , wherein the dosage of doxepin is about 3 milligrams.4. The method of claim 1 , wherein the dosage of doxepin is about 6 milligrams.5. The method of claim 1 , wherein the patient is in need of treatment for transient insomnia or short term insomnia.6. The method of claim 1 , wherein the patient is in need of treatment for chronic insomnia.7. A method for treating a patient claim 1 , comprising:identifying a patient in need of pharmaceutical therapy for a sleep disorder;also identifying a need to avoid rebound insomnia in the patient as a consequence of said pharmaceutical therapy;selecting a doxepin therapy protocol for the patient based at least in part on its low incidence of rebound insomnia; andtreating the patient according to the protocol with daily doses of between 0.5 mg and 6 mg doxepin or a pharmaceutically acceptable salt thereof, thereby providing pharmaceutical therapy for the sleep disorder while avoiding rebound insomnia.8. A method claim 1 , comprising:identifying a patient in need of pharmaceutical treatment of a sleep disorder and ...

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13-06-2013 дата публикации

USE OF BIS [THIOHYDRAZIDE AMIDE] COMPOUNDS SUCH AS ELESCLOMOL FOR TREATING CANCERS

Номер: US20130150440A1
Принадлежит: Synta Pharmaceuticals Corp.

Improved cancer treatments with bis[thiohydrazide amide] compounds such as elesclomol, in particular for identifying patient populations that would benefit from such treatments. 2. The method of claim 1 , wherein the patient has been diagnosed as being at risk of having cancer cells with elevated lactate dehydrogenase levels.5. The method of claim 4 , wherein the LDH inhibitor is oxamic acid or a salt thereof.6. The method of claim 4 , wherein the LDH inhibitor inhibits LDH-A.8. The method of claim 1 , wherein the cancer is selected from the group consisting of renal cancer claim 1 , skin cancer claim 1 , bone marrow cancer claim 1 , blood cell cancer claim 1 , prostate cancer claim 1 , ovarian cancer claim 1 , and breast cancer.9. The method of claim 8 , wherein the blood cell cancer is leukemia claim 8 , lymphoma or myeloma.10. The method of claim 9 , wherein the leukemia is selected from the group consisting of acute lymphocytic leukemia claim 9 , acute myelocytic leukemia claim 9 , chronic leukemia claim 9 , polycythemia vera claim 9 , lymphocytic leukemia claim 9 , large granular lymphocytic leukemia claim 9 , lymphoblastic leukemia claim 9 , T-cell leukemia claim 9 , T-lymphocytic leukemia claim 9 , T-lymphoblastic leukemia claim 9 , B cell leukemia claim 9 , B-lymphocytic leukemia claim 9 , B and T cell leukemia claim 9 , B and T lymphocytic leukemia claim 9 , myeloid leukemias claim 9 , neutrophilic leukemia claim 9 , eosinophilic leukemia claim 9 , monocytic leukemia claim 9 , myelomonocytic leukemia claim 9 , Naegeli-type myeloid leukemia claim 9 , and nonlymphocytic leukemia.11. The method of claim 9 , wherein the lymphoma is selected from the group consisting of Hodgkin's and non-Hodgkin's disease claim 9 , and Waldenström macroglobulinemia.12. The method of claim 1 , wherein the compound is co-administered with an anti-cancer agent that stabilizes microtubules.13. The method of claim 1 , wherein the compound is co-administered with paclitaxel claim 1 , ...

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20-06-2013 дата публикации

Cyclodextrin-based polymers for therapeutics delivery

Номер: US20130156721A1
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.

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20-06-2013 дата публикации

Substituted Triazolopyridines

Номер: US20130156756A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R, R, R, R, and Rare as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds. 2. The compound according to claim 1 , wherein:{'sup': '1', 'claim-text': 'which is substituted, one or more times, identically or differently, with a substituent selected from:', 'Rrepresents an aryl or heteroaryl group'}{'sup': 6', '6', '6', '6', '6', '6', '6', '6', '6', '6', '7', '6', '6', '7', '7', '6', '7', '6', '7', '6', '6', '7', '6', '6', '6', '6', '7', '6', '6', '6', '7', '6', '7', '6', '6', '6', '7', '6', '7', '7', '6', '6', '7, 'sub': 2', 'n', '2', 'm', '1', '6', '2', 'n', '2', 'p', '1', '6', '1', '6', '1', '6', '1', '6', '2', '2', '2', '2', '2, 'claim-text': and', {'sup': 'xy', 'which is optionally substituted, one or more times, identically or differently, with a substituent Rselected from, {'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'sup': 8', '7', '8', '8', '8', '7, 'halo-, hydroxyl-, cyano-, C-C-alkyl-, halo-C-C-alkyl-, C-C-alkoxy-, halo-C-C-alkoxy-, hydroxy-C-C-alkyl-, —N(H)C(═O)R, —N(R)C(═O)R, —C(═O)N(H)R, —C(═O)NRR;'}], 'R—(CH)(CHOH)(CH)—, R—(C-C-alkoxy)-, R—(CH)(CHOH)(CH)—O—, R—(C-C-alkoxy-C-C-alkyl)-, R—(C-C-alkoxy-C-C-alkyl)-O—, R—O—, —C(═O)R, —C(═O)O—R, —OC(═O)—R, —N(H)C(═O)R, —N(R)C(═O)R, —N(H)C(═O)NRR, —N(R)C(═O)NRR, —NRR, —C(═O)N(H)R, —C(═O)NRR, R—S—, R—S(═O)—, R—S(═O)—, —N(H)S(═O)R, —N(R)S(═O)R, —S(═O)N(H)R, —S(═O)NRR, —N(H)S(═O)R, —N(R)S(═O)R, —S(═O)N(H)R, —S(═O)NRR, —S(═O)(═NR)R, —S(═O)(═NR)R, —N═S(═O)(R)R;'}or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a ...

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27-06-2013 дата публикации

NEURONAL CIRCUIT-DEPENDENT NEUROPROTECTION BY INTERACTION BETWEEN NICOTINIC RECEPTORS

Номер: US20130165495A1
Принадлежит:

A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis. 2. A method of wherein Ris α—OH and R claim 1 , R claim 1 , R claim 1 , and Rare H3. A method of wherein Ris OH and R claim 1 , R claim 1 , R claim 1 , and Rare H4. A method of wherein Ris β—OH and R claim 1 , R claim 1 , R claim 1 , and Rare H5. A method of wherein Ris OH and R claim 1 , R claim 1 , R claim 1 , and Rare H12. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.13. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.14. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.15. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.16. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.17. The method of wherein said compound is administered in an amount sufficient to achieve a concentration between about 200 nM to about 40 μM.18. The method of wherein said compound is administered in an amount sufficient to achieve a ...

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04-07-2013 дата публикации

SYNERGISTIC ACTIVITY OF MODULATORS OF THE NO METABOLISM AND OF NADPH OXIDASE IN THE SENSITIZATION OF TUMOR CELLS

Номер: US20130171104A1
Автор: Bauer Georg
Принадлежит: Universitaetsklinikum Freiburg

What is disclosed is pharmaceutical compositions which contain a pharmaceutically active amount of at least one active substance which increases the available NO concentration in the cell, together with at least one active substance which stimulates the NADPH oxidase. 1. A pharmaceutical composition comprising a pharmaceutically active amount of a first active substance that increases available NO concentration in a cell in combination with a pharmaceutically active amount of a second active substance that stimulates NADPH oxidase.2. The pharmaceutical composition according to claim 1 , characterised in that the second active substance is selected from the group consisting of resveratrol claim 1 , transforming growth factor β and angiotensin II.3. The pharmaceutical composition according to claim 1 , characterised in that the first active substance does not have a simultaneous effect on NADPH oxidase.4. The pharmaceutical composition according to claim 1 , characterised in that the first active substance is selected from the group consisting of arginine and arginase inhibitors.5. The pharmaceutical composition according to claim 1 , characterised in that the second active substance is resveratrol claim 1 , combined with the arginase inhibitor nor-NOHA.6. The pharmaceutical composition according to claim 2 , characterised in that the second active substance is resveratrol claim 2 , combined with Taxol or diallyl disulfide.7. The pharmaceutical composition according to claim 2 , characterised in that the second active substance is resveratrol claim 2 , combined with cyanidin chloride.8. The pharmaceutical composition according to claim 2 , characterised in that resveratrol is combined with an azole.9. The pharmaceutical composition according to claim 2 , characterised in that the first and second active substances are in the form of a hybrid molecule.10. The pharmaceutical composition according to claim 1 , characterised in that the first active substance increases ...

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04-07-2013 дата публикации

METHOD TO IDENTIFY A PATIENT WITH AN INCREASED LIKELIHOOD OF RESPONDING TO AN ANTI-CANCER THERAPY

Номер: US20130171135A1
Принадлежит: F. Hoffmann-La Roche AG

The invention provides methods for identifying patient who may benefit from treatment with an anti-cancer therapy comprising a VEGF antagonist. The invention also provides methods for monitoring a patients' response to the anti-cancer therapy. The invention also provides kits and articles of manufacture for use in the methods. 1. A method of identifying a patient who may benefit from treatment with an anti-cancer therapy comprising a VEGF antagonist , the method comprising:determining an expression level of unmodified VEGF in a sample obtained from the patient, wherein a level of unmodified VEGF in the sample obtained from the patient at or above a reference level indicates that the patient may benefit from treatment with the anti-cancer therapy.2. A method of predicting responsiveness of a patient suffering from cancer to treatment with an anti-cancer therapy comprising a VEGF-A antagonist , the method comprising:determining an expression level of unmodified VEGF in a sample obtained from the patient, wherein a level of unmodified VEGF in the sample obtained from the patient at or above a reference level indicates that the patient is more likely to be responsive to treatment with the anti-cancer therapy.3. A method for determining the likelihood that a patient with cancer will exhibit benefit from anti-cancer therapy comprising a VEGF-A antagonist , the method comprising:determining an expression level of unmodified VEGF in a sample obtained from the patient, wherein a level of unmodified VEGF in the sample obtained from the patient at or above a reference level indicates that the patient has increased likelihood of benefit from the anti-cancer therapy.4. A method for optimizing the therapeutic efficacy of an anti-cancer therapy comprising a VEGF-A antagonist , the method comprising:determining an expression level of unmodified VEGF in a sample obtained from the patient, wherein a level of unmodified VEGF in the sample obtained from the patient at or above a ...

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04-07-2013 дата публикации

Micelle encapsulation of a combination of therapeutic agents

Номер: US20130171207A1
Автор: Glen S. Kwon
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

The invention provides active agents, such as paclitaxel, rapamycin, or 17-DMAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) (“PEG-b-PLA”) micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-DMAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.

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11-07-2013 дата публикации

Growth inhibitory effects of nanoparticles containing triterpene glycosides or triterpenes

Номер: US20130177627A1
Принадлежит:

The present invention relates to pharmaceutical composition containing a physiologically effective dose of a nanoparticle triterpene glycoside or nanoparticle triterpene complex, wherein said complex is a liposome encapsulated compound, or exosome-encapsulated compound. 1. A pharmaceutical composition containing a physiologically effective dose of a nanoparticle triterpene glycoside or nanoparticle triterpene complex; wherein said complex is a liposome encapsulated compound , or exosome-encapsulated compound.2. A pharmaceutical composition containing:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) a physiologically effective dose of the composition of ; and'}(b) a physiologically effective dose of another chemotherapeutic agent.3. The composition of wherein the triterpene glycoside compound is selected from the group consisting of actein claim 1 , cimifugoside claim 1 , cimigenol glycoside claim 1 , cimiracemoside A claim 1 , and 23-epi-26-deoxyactein.4. The composition of wherein the triterpene glycoside compound is selected from the group consisting of actein claim 2 , cimifugoside claim 2 , cimigenol glycoside claim 2 , cimiracemoside A claim 2 , and 23-epi-26-deoxyactein.5. The composition of wherein the triterpene compound is cimigenol.6. The composition of wherein the triterpene compound is cimigenol.7. The composition of wherein the triterpene compound is 25-acetyl-7 claim 1 ,8-didehydrocimigenol 3-O-β-D-xylopyranoside.8. The composition of wherein the triterpene compound is 25-acetyl-7 claim 2 ,8-didehydrocimigenol 3-O-β-D-xylopyranoside.9. The composition of wherein the complex is approximately 100 nm to approximately 400 nm in diameter.10. The composition of wherein the liposome is composed of DOPE and DOPC.11. A method of treating cancer comprising systemically administering a pharmaceutical composition containing a physiologically effective dose of a nanoparticle triterpene glycoside or nanoparticle triterpene complex; wherein said complex is a ...

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18-07-2013 дата публикации

BLOOD PLASMA BIOMARKERS FOR BEVACIZUMAB COMBINATION THERAPIES FOR TREATMENT OF BREAST CANCER

Номер: US20130183302A1
Принадлежит: Hoffman-La Roche Inc.

The present invention provides methods for improving the treatment effect of a chemotherapy regimen of a patient suffering from breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer, by adding bevacizumab (Avastin®) to a chemotherapy regimen by determining the expression level, in particular the blood plasma expression level, of one or more of VEGFA, VEGFR2 and PLGF relative to control levels of patients diagnosed with breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer. In particular, the present invention provides methods of improving the treatment effect, wherein the treatment effect is the progression-free survival of the patient. The present invention further provides for methods for assessing the sensitivity or responsiveness of a patient to bevacizumab (Avastin®) in combination with a chemotherapy regimen, by determining the expression level, in particular the blood plasma expression level, of one or more of VEGFA, VEGFR2 and PLGF relative to control levels in patients diagnosed with breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer. 1. A method for the identification of a patient responsive to or sensitive to the addition of bevacizumab treatment to a chemotherapy regimen , said method comprising:(a) determining an expression level of VEGFA and/or VEGFR2 in a patient sample from a patient suspected to suffer from or being prone to suffer from breast cancer, whereby an increased expression level of VEGFA and/or VEGFR2 relative to control expression levels determined in patients suffering from breast cancer identifies the patient as being responsive to or sensitive to the addition of bevacizumab to said chemotherapy regimen; and(b) informing the identified patient that they have an increased likelihood of being responsive to or sensitive to the addition of bevacizumab to said chemotherapy regimen.2. A method of ...

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18-07-2013 дата публикации

BLOOD PLASMA BIOMARKERS FOR BEVACIZUMAB COMBINATION THERAPIES FOR TREATMENT OF BREAST CANCER

Номер: US20130183303A1
Принадлежит: Hoffman-La Roche Inc.

The present invention provides methods for improving the treatment effect of a chemotherapy regimen of a patient suffering from breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer, by adding bevacizumab (Avastin®) to a chemotherapy regimen by determining the expression level, in particular the blood plasma expression level, of one or more of VEGFA, VEGFR2 and PLGF relative to control levels of patients diagnosed with breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer. In particular, the present invention provides methods of improving the treatment effect, wherein the treatment effect is the progression-free survival of the patient. The present invention further provides for methods for assessing the sensitivity or responsiveness of a patient to bevacizumab (Avastin®) in combination with a chemotherapy regimen, by determining the expression level, in particular the blood plasma expression level, of one or more of VEGFA, VEGFR2 and PLGF relative to control levels in patients diagnosed with breast cancer, in particular locally advanced, recurrent or metastatic HER-2 negative breast cancer. 1. A method of selecting a cancer treatment for a patient suffering from breast cancer , said method comprising:(a) determining that a sample obtained from the patient has an increased expression level of VEGFA and/or VEGFR2 relative to control expression levels determined in patients suffering from breast cancer; and(b) providing a recommendation that said cancer treatment selected for the patient comprise an effective amount of bevacizumab in combination with a chemotherapy regimen.2. A method of monitoring patient response to a cancer treatment for a patient suffering from breast cancer , said method comprising:(a) determining that a sample obtained from the patient has an increased expression level of VEGFA and/or VEGFR2 relative to control expression levels determined in patients ...

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18-07-2013 дата публикации

Novel IDO Inhibitors and Methods of Use Thereof

Номер: US20130183388A1
Принадлежит: LANKENAU INSTITUTE FOR MEDICAL RESEARCH

Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed. 1. (canceled)3. (canceled)4. (canceled)5. A pharmaceutical composition for the treatment of cancer comprising a pharmaceutically acceptable carrier and an effective amount at least one indoleamine 2 claim 2 ,3-dioxygenase (IDO) inhibitor claim 2 , wherein at least one of said IDO inhibitors is the compound of .616-. (canceled)17. The pharmaceutical composition of claim 5 , further comprising at least one signal transduction inhibitor (STI).18. (canceled)19. (canceled)20. The pharmaceutical composition of claim 5 , further comprising at least one chemotherapeutic agent.21. (canceled)22. (canceled)23. The pharmaceutical composition of claim 20 , wherein said at least one chemotherapeutic agent is selected from the group consisting of paclitaxel (Taxol®) claim 20 , cisplatin claim 20 , docetaxol claim 20 , carboplatin claim 20 , vincristine claim 20 , vinblastine claim 20 , methotrexate claim 20 , cyclophosphamide claim 20 , CPT-11 claim 20 , 5-fluorouracil (5-FU) claim 20 , gemcitabine claim 20 , estramustine claim 20 , carmustine claim 20 , adriamycin (doxorubicin) claim 20 , etoposide claim 20 , arsenic trioxide claim 20 , irinotecan claim 20 , and epothilone derivatives.2434.-. (canceled)35. A compound which is the hydroquinone form of the compound of .36. (canceled)37. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , and Xare H.38. The compound of claim 2 , wherein Xis R.39. The compound of claim 38 , wherein R is aryl.40. The compound of claim 37 , wherein Xis R.41. The compound of claim 39 , wherein R is aryl. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/918,516, filed on Mar. 16, 2007. The foregoing application is incorporated by reference herein.Pursuant to 35 U.S.C. Section 202(c), it is acknowledged that the United ...

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18-07-2013 дата публикации

Hydrazone modulators of cannabinoid receptors

Номер: US20130184275A1
Принадлежит: Mohamed Naguib Attala, Philippe Diaz

Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.

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25-07-2013 дата публикации

Use of fucoxanthin in the preparation of product for improving memory and having neuroprotective effect associated with neurodegenerative disorder

Номер: US20130189382A1
Автор: Li Liang, Li Yanmei

Use of fucoxanthin in the preparation of a product having neuroprotective effect associated with neurodegenerative disorder and improving memory is disclosed in the disclosure. A product having neuroprotective effect associated with neurodegenerative disorder is also disclosed in the disclosure. Fucoxanthin can inhibit oxidative stress of cells and has the effect of preventing or treating Alzheimer's disease and improving memory. 1. Use of fucoxanthin in the preparation of a product having neuroprotective effect associated with neurodegenerative disorder , wherein the product includes a food , a healthcare product and a drug.2. The use according to claim 1 , wherein the neurodegenerative disorder includes claim 1 , Parkinson's disease claim 1 , and Huntington's disease.3. The use according to claim 2 , wherein the product further has a memory-improving effect.4. The use of fucoxanthin according to claim 1 , wherein the source of fucoxanthin includes a plant source claim 1 , a microorganism source claim 1 , or a synthetic compound source.5. The use of fucoxanthin according to claim 4 , wherein the plant source of fucoxanthin is seaweed claim 4 , selected from a group consisting of laminaria japonica claim 4 , gulfweed claim 4 , wrack claim 4 , myosoton aquaticum claim 4 , colpomenia peregrina claim 4 , chorda filum claim 4 , wakame claim 4 , giant kelp claim 4 , carageen claim 4 , sargassum miyabei yendo claim 4 , hijiki claim 4 , sargassum pallidum claim 4 , and diatom.6. The use of fucoxanthin according to claim 1 , wherein the content of fucoxanthin in the product is 0.0001% to 60%; preferably claim 1 , the content of fucoxanthin in the product is 0.0001% to 10%.7. (canceled)8. The use of fucoxanthin according to claim 1 , wherein the content of fucoxanthin in a fucoxanthin extract is 90% to 100%; preferably claim 1 , the content of fucoxanthin in a fucoxanthin extract is 95% to 100%.9. (canceled)10. The use of fucoxanthin according to claim 1 , wherein 0.001 mg ...

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01-08-2013 дата публикации

FILMS AND PARTICLES

Номер: US20130195954A1
Принадлежит:

Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses. 3. The oligomer or polymer of claim 1 , wherein Ris hydrogen or methyl.4. The oligomer or polymer of claim 1 , wherein Q is oxygen.5. A composition comprising the oligomer or polymer of .6. A polymeric film or particle comprising an oligomer or polymer of .7. A polymeric particle of claim 6 , comprising a microparticle or nanoparticle.8. A polymeric particle of claim 7 , wherein the particle has a diameter between about 2 nm and 1 micron.9. The polymeric particle of comprising a first volume at a first pH claim 7 , and a second volume at a second pH claim 7 , different from the from the first pH.10. The polymeric particle of claim 9 , wherein the second volume is 1× or more greater than the first volume when the second pH is lower than the first pH.11. The polymeric particle of claim 9 , wherein the second volume is 4× or more greater than the first volume when the second pH is lower than the first pH.12. The polymeric particle of claim 9 , wherein the second volume is 8× or more greater than the first volume when the second pH is lower than the first pH.13. The polymeric particle of claim 9 , wherein the second volume is greater than the first volume and the change in volume is sufficient that the particle when within a cell during the volume change ruptures the cell or a cellular compartment.14. The polymeric particle of claim 9 , wherein the second volume is greater than the first volume and the change in volume is sufficient to cause the particle to become lodged claim 9 , embedded claim 9 , or immobilized in an anatomic location claim 9 , such as a lymph node claim 9 , airway claim 9 , cavity claim 9 , capillary claim 9 , or other tissue.15. The polymeric film or particle of claim 6 , further comprising an agent.16. The polymeric film or particle of claim 15 , wherein the ...

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01-08-2013 дата публикации

COMBINATIONS AND MODES OF ADMINISTRATION OF THERAPEUTIC AGENTS AND COMBINATION THERAPY

Номер: US20130195984A1
Принадлежит: ABRAXIS BIOSCIENCE, LLC

The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents (such as an anti-VEGF antibody), or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime. 1. A composition comprising: (a) nanoparticles comprising paclitaxel and albumin and (b) an anti-VEGF antibody.2. The composition of claim 1 , wherein the anti-VEGF antibody is bevacizumab.3. The composition of claim 1 , wherein the weight ratio of the paclitaxel and the anti-VEGF antibody is between about 0.01:1 and about 100:1.4. The composition of claim 1 , wherein the weight ratio of the paclitaxel and the anti-VEGF antibody is less than about 30:1.5. The composition of claim 1 , wherein the weight ratio of the paclitaxel and the anti-VEGF antibody is less than about 10:1.6. The composition of claim 2 , wherein the weight ratio of the paclitaxel and the bevacizumab is less than about 10:1.7. The composition of claim 1 , wherein the weight ratio of the paclitaxel and the anti-VEGF antibody is about 2:1 to about 3:1.8. The composition of claim 2 , wherein the weight ratio of the paclitaxel and the bevacizumab is about 2:1 to about 3:1.9. The composition of claim 1 , wherein the composition further comprises a platinum-based agent.10. The composition of claim 9 , wherein the platinum-based agent is carboplatin.11. The composition of claim 1 , wherein the nanoparticles comprise paclitaxel coated with albumin.12. The composition of claim 8 , wherein the nanoparticles comprise paclitaxel coated with albumin.13. The composition of claim 1 , wherein the average diameter of the nanoparticles in the composition is no greater ...

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08-08-2013 дата публикации

METHODS OF TREATMENT OF PANCREATIC CANCER

Номер: US20130202709A1
Принадлежит:

The present invention provides methods and compositions for treating pancreatic cancer in an individual who has been previously treated for pancreatic cancer (e.g., gemcitabine-based therapy) by administering a composition comprising nanoparticles that comprise a taxane and an albumin. The invention also provides combination therapy methods of treating pancreatic cancer (for example, in an individual who has been previously treated for pancreatic cancer) comprising administering to an individual an effective amount of a composition comprising nanoparticles that comprise a taxane and an albumin and another agent. 1. A method of treating pancreatic cancer in an individual in need thereof , comprising administering to the individual an effective amount of a composition comprising nanoparticles comprising a taxane and an albumin , wherein the individual has progressed on a gemcitabine-based therapy.2. The method of claim 1 , wherein the progression is within less than about 12 months.3. A method of treating resistant or refractory pancreatic cancer in an individual in need thereof claim 1 , comprising administering to the individual an effective amount of a composition comprising nanoparticles comprising a taxane and an albumin.4. A method of treating recurrent pancreatic cancer in an individual in need thereof claim 1 , comprising administering to the individual an effective amount of a composition comprising nanoparticles comprising a taxane and an albumin.5. The method of claim 3 , wherein a prior therapy has stopped for at least 6 months when initiating administration to the individual of an effective amount of a composition comprising nanoparticles comprising a taxane and an albumin.6. The method of claim 5 , wherein the prior therapy is a gemcitabine-based therapy.7. The method of claim 1 , wherein the gemcitabine-based therapy further comprises erlotinib.8. The method of claim 1 , wherein the gemcitabine-based therapy is monotherapy.9. The method of claim 1 , ...

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08-08-2013 дата публикации

Treatment of Cancer Using Hypoxia Activated Prodrugs

Номер: US20130202716A1
Принадлежит:

Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy. 1. A method of treating cancer comprising administering TH-302 and a therapeutically effective dose of an anticancer drug that is not a hypoxia activated prodrug to a patient in need of cancer therapy ,{'sup': 2', '2, 'wherein TH-302 is administered intravenously in an amount in the range of 200 mg/mto 500 mg/mand administration of the anticancer drug that is not a hypoxia activated prodrug begins 30 minutes to 8 hours after administration of TH-302 is completed.'}2. The method of claim 1 , wherein the drug that is not a hypoxia activated prodrug is administered 2 hours to 6 hours after administration of TH-302 is complete.3. The method of claim 1 , wherein the anticancer drug that is not a hypoxia activated prodrug is docetaxel claim 1 , pemetrexed claim 1 , doxorubicin claim 1 , gemcitabine claim 1 , cisplatin claim 1 , carboplatin or 5-fluorouracil.4. The method of wherein the patient is in need of treatment for lung cancer and the anticancer drug that is not a hypoxia activated prodrug is docetaxel claim 3 , paclitaxel claim 3 , pemetrexed claim 3 , doxorubicin claim 3 , gemcitabine claim 3 , 5-fluorouracil claim 3 , cisplatin claim 3 , or carboplatin.5. The method of wherein the patient is in need of treatment for prostate cancer and the anticancer drug that is not a hypoxia activated prodrug is docetaxel.6. The method of wherein the patient is in need of treatment for pancreatic cancer and the anticancer drug that is not a hypoxia activated prodrug is gemcitabine.7. The method of wherein ...

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15-08-2013 дата публикации

Methods and compositions for malic enzyme 2 (me2) as a target for cancer therapy

Номер: US20130209488A1

The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing cancer and other related diseases that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include combination therapy, such as with a combination of two or more ME2 inhibitors or a combination of an ME2 inhibitor and an anticancer agent.

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15-08-2013 дата публикации

Compositions of small molecule therapeutics

Номер: US20130210766A1
Принадлежит: Nexmed Holdings Inc

Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.

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15-08-2013 дата публикации

CANCER THERAPY

Номер: US20130210890A1
Принадлежит: BRANDEIS UNIVERSITY

The present invention provides agents useful in the treatment of cancer, as well as systems for identifying and/or characterizing such agents, and systems for identifying and/or characterizing patient populations responsive to particular agents. 1. A method of treating cancer by administering to a patient in need thereof an agent that inhibits palmitoylation of NRAS.2. The method of claim 1 , wherein the cancer is associated with an oncogene that acts upstream of RAS.3. The method of or claim 1 , wherein the cancer is not associated with a mutation of NRAS.43. The method of any one of - wherein the agent comprises an siRNA.5. The method of wherein the siRNA targets a RAS palmitoyl-acyl transferase.6. The method of wherein the siRNA targets a fatty acid synthase involved in palmitate production7. A method of identifying agents useful in the treatment of cancer claim 4 , the method comprising steps of:providing one or more agents that inhibit RAS palmitoylation; andassessing ability of the agents to inhibit proliferation of cancer cells.8. The method of claim 7 , wherein the cancer cells do not contain NRAS mutations.9. A method of treating cancers associated with activated RAS that requires palmitoylation claim 7 , the method comprising steps of:administering a FASN inhibitor to a subject suffering from a cancer that is associated with activated RAS requiring palmitoylation.10. A method for treating cancer comprising:administering a FASN inhibitor and a RAS palmitoylation inhibitor in combination.11. A method comprising steps of:identifying in a cancer patient suffering from or susceptible to a cancer associated with an activated RAS that requires palmitoylation;determining, based on the identification, that the patient is a good candidate for therapy with a FASN inhibitor and/or a RAS palmitoylation inhibitor. This application claims priority to U.S. Provisional Application No. 61/357,845, entitled Cancer Therapy, filed Jun. 23, 2010, the entire contents of which ...

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