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Изобретение относится к медицине, а именно к психиатрии, неврологии и клинической фармакологии, и может быть использовано для выбора тактики лечения пациентов с антипсихотик-индуцированными экстрапирамидными расстройствами. Определяют особенности генотипа пациентов посредством микрочипов. При выявлении гомозигот GG варианта rs1799732 (4750dup) гена DRD2, гомозигот ТТ варианта rs1045642 гена АВСВ1 и гомозигот АА варианта CYP2D6*4 (rs3892097) гена CYP2D6 определяют фенотип антипсихотик-индуцированного паркинсонизма. При выявлении гомозигот ТТ варианта rs6275 (67525 Т>С) гена DRD2 и гомозигот ТТ варианта CYP3A5*6 (rs10264272 C>Т) гена CYP3A5 определяют фенотип антипсихотик-индуцированной тардивной дискинезии. При выявлении гомозигот СС варианта rs1800498 (59414 Т>С) гена DRD2, гомозигот ТТ варианта rs1128503 гена АВСВ1 и гомозигот ТТ варианта CYP3A5*6 (rs10264272 C>Т) гена CYP3A5 определяют фенотип антипсихотик-индуцированной акатизии. В соответствии с фенотипом пациента осуществляют выбор ...

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... 1. Применение первого соединения - селективного антагониста 5-НТ6-рецептора и второго соединения - селективного антагониста 5-НТ2А-рецептора, где первое соединение имеет сродство к 5-НТб-рецептору с величиной pKi, большей или равной 8, и второе соединение имеет сродство к 5-НТ2А-рецептору с величиной pKi, большей или равной 8, причем каждое из указанных соединений имеет селективность по меньшей мере в 30 раз большую по сравнению с 5-НТ2С рецептором, допаминовым D2-рецептором, гистаминовым Н1-рецептором и мускариновыми М1 и М2 рецепторами, для изготовления лекарственного средства для лечения болезненного состояния, связанного с когнитивным расстройством. 2. Применение по п.1, где когнитивное расстройство выбрано из группы, состоящей из болезни Альцгеймера, дегенеративных расстройств, относящихся к обучаемости, неспособности к обучению, нарушению функции памяти или когнитивной функции, таких как умеренное когнитивное расстройство, возрастное ухудшение когнитивной функции, старческое угасание ...

ПРОИЗВОДНЫЕ ГИАЛУРОНОВОЙ КИСЛОТЫ И СОДЕРЖАЩЕЕ ЕГОЛЕКАРСТВЕННОЕ СРЕДСТВО

... 1. Производное гиалуроновой кислоты, где противовоспалительное лекарственное средство связано с гиалуроновой кислотой посредством ковалентной связи через спейсер, содержащий биодеградируемый участок. 2. Производное гиалуроновой кислоты по п.1, где противовоспалительное лекарственное средство выбрано из нестероидного противовоспалительного лекарственного средства и облегчающего заболевание противоревматического лекарственного средства. 3. Производное гиалуроновой кислоты по п.1 или 2, где противовоспалительное лекарственное средство содержит карбоксильную группу. 4. Производное гиалуроновой кислоты по п.3, где противовоспалительное лекарственное средство представляет собой остаток соединения, выбранного из группы, состоящей из салициловой кислоты, аспирина, мефенамовой кислоты, толфенамовой кислоты, флуфенамовой кислоты, диклофенака, сулиндака, фенбуфена, индометацина, ацеметацина, амфенака, этодолака, фелбинака, ибупрофена, флурбипрофена, кетопрофена, напроксена, пранопрофена, фенопрофена ...

БОЛЕУТОЛЯЮЩИЕ И ПРОТИВОВОСПАЛИТЕЛЬНЫЕ СОСТАВЫ, СОДЕРЖАЩИЕ ИНГИБИТОРЫ ЦИКЛООКСИГЕНАЗЫ-2

... 1. Состав, содержащий по существу (а) по меньшей мере один ингибитор циклооксигеназы-2 и (б) по меньшей мере одно соединение, выбранное из группы, включающей NSAID, ацетаминофен и их смеси. 2. Состав по п.1, отличающийся тем, что ингибитор циклооксигеназы-2 выбран из группы, включающей целекоксиб, мелоксикам, нимесулид и рофекоксиб и их смеси, а компонент (б) представляет собой NSAID. 3. Состав по п.2, отличающийся тем, что NSAID выбран из группы, включающей ибупрофен, кетопрофен, фенопрофен, флубипрофен, напроксен натрия, проксен, оксапрозин, пироксикам и их смеси. 4. Состав по п.1, отличающийся тем, что ингибитор циклооксигеназы-2 является целекоксибом, а компонент (б) - ибупрофеном. 5. Состав по п.4, отличающийся тем, что целекоксиб присутствует в количестве в пределах примерно 25 - 200 мг, предпочтительно примерно 100 - 200 мг, наиболее предпочтительно около 200 мг, а ибупрофен присутствует в количестве в пределах примерно 50 - 800 мг, предпочтительно примерно 200 - 400 мг, и наиболее ...

ФАРМАЦЕВТИЧЕСКАЯ КОМБИНАЦИЯ, ВКЛЮЧАЮЩАЯ 3-(3-ДИМЕТИЛАМИНО-1-ЭТИЛ-2-МЕТИЛПРОПИЛ)ФЕНОЛ Т НЕСТЕРОИДНЫЙ ПРОТИВОВОСПАЛИТЕЛЬНЫЙ ПРЕПАРАТ

... 1. Комбинация, включающая в качестве компонентов: ! (а) по крайней мере один 3-(3-диметиламино-1-этил-2-метилпропил)фенол формулы (I), ! ! необязательно в форме одного из индивидуальных стереоизомеров, прежде всего, ! энантиометра или диастереомера, рацемата или в форме смеси стереоизомеров, прежде всего, энантиомеров и/или диастереомеров, в любом соотношении, или в форме любой кислотно-аддитивной соли, или любых сольватов указанных соединений, и ! (б) один или более нестероидных противовоспалительных препаратов (НПВП). ! 2. Комбинация по п.1, отличающаяся тем, что компонент (а) выбирают из группы, включающей ! (1R,2R)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1S,2S)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1R,2S)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1S,2R)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, или любую смесь указанных соединений. ! 3. Комбинация по п.2, отличающаяся тем, что компонент (а) выбирают из группы, включающей !(1R,2R)-3-(3-диметиламино-1-этил ...

ПРИМЕНЕНИЕ ПРОИЗВОДНОГО ПИРАЗОЛА ДЛЯ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОГО СРЕДСТВА, ПРИГОДНОГО ДЛЯ ПРОФИЛАКТИКИИ ЛЕЧЕНИЯ ДИСЛИПИДЕМИЙ И ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ СДИСЛИПИДЕМИЯМИ И/ИЛИ С ОЖИРЕНИЕМ

... 1. Применение римонабанта для получения лекарственного средства, пригодного при лечении и профилактике заболеваний, связанных с ожирением и/или дислипидемиями, выбранных из метаболического синдрома и стеатоза. 2. Применение по п.1 для профилактики и лечения метаболического синдрома. 3. Применение по п.1 для профилактики и лечения стеатоза. 4. Применение по п.1, в котором римонабант комбинируют с другим действующим началом, выбранным из одного из следующих терапевтических классов: антагонист рецепторов AT1 ангиотензина II, индивидуально или в комбинации с диуретиком или с антагонистом кальция; ингибитор фермента превращения, индивидуально или в комбинации с диуретиком; антагонист кальция; бета-блокатор, индивидуально или в комбинации с диуретиком или антагонистом кальция; антигиперлипемическое или антигиперхолистеринемическое средство; антидиабетическое средство; другой агент против ожирения. 5. Применение по одному из пп.1-4, в котором римонабант используют в дозе от 5 до 50 мг. 6. Фармацевтическая ...

Фармацевтический состав, содержащий алимемазина тартрат

Изобретение относится к области химико-фармацевтической промышленности и медицины. Фармацевтический состав содержит алимемазина тартрат и вспомогательные компоненты. В качестве вспомогательных компонентов выбраны микрокристаллическая целлюлоза, гипромеллоза, кремния диоксид коллоидный и стеарат магния в указанных в формуле изобретения количествах. Фармацевтический состав алимемазина тартрата выполнен в форме таблетки, покрытой пленочной оболочкой. Таблетка по изобретению обеспечивает пролонгированное высвобождение алимемазина тартрата, при этом сохраняя преимущества в виде короткого периода полувыведения; характеризуется удовлетворительной стабильностью, прочностью более чем 70 Н и прочностью на истирание не менее 98,5%. 4 з.п. ф-лы, 4 табл., 5 пр.

Средство, его применение и способ повышения устойчивости организма млекопитающих к переохлаждению

Группа изобретений относится к созданию лекарственного средства для повышения устойчивости млекопитающих к переохлаждению. Средство содержит фармацевтическую композицию препаратов, содержащую 0,78-1,18 мас.% пропранолола, 0,015-0,024 мас.% резерпина, 0,078-0,12 мас.% ивабрадина, 0,098-0,18 мас.% дифенгидрамина, 0,025-0,035 мас.% перициазина, 0,25-0,35 мас.% серотонина гидрохлорид, 0,07-0,12 мас.% пропицила, 0,07-0,16 мас.% сульфата магния, 98-98,61 мас.% фармацевтически приемлемого растворителя. Также предлагается способ повышения устойчивости организма млекопитающих к переохлаждению, заключающийся в введении терапевтически эффективного количества средства. Техническим результатом является повышение резистентности клеток жизненно важных органов и тканей к переохлаждению. 3 н.п. ф-лы, 2 ил., 2 пр.

Препарат для профилактики и лечения воспалительных процессов у животных

Изобретение относится к ветеринарии и фармацевтической промышленности, а именно к препарату для профилактики и лечения воспалительных процессов (заболеваний) у животных, который включает (в мас.%): 0,15-0,25% мелоксикама в качестве нестероидного противовоспалительного средства, 7,5-12,5% этилметилгидроксипиридина сукцината, 5,0-10,0% левамизола основания, 2,5-4,5% поливинлпирролидона и воду для инъекций (остальное). Изобретение обеспечивает повышение противовоспалительного терапевтического эффекта при наличии антиоксидантного и иммуностимулирующего действия, а также снижение токсичности и частоты развития побочных эффектов. 7 пр., 7 ил.

КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПОЛИСАХАРИДНУЮ МАТРИЦУ ДЛЯ КОНТРОЛИРУЕМОГО ВЫСВОБОЖДЕНИЯ АКТИВНЫХ ИНГРЕДИЕНТОВ

СРЕДСТВО В ВИДЕ КАПСУЛЫ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ СУСТАВОВ

ЛЕКАРСТВЕННЫЕ СРЕДСТВА И СПОСОБЫ ЛЕЧЕНИЯ ПРЕСБИОПИИ, УМЕРЕННОЙ ГИПЕРМЕТРОПИИ И НЕПРАВИЛЬНОГО АСТИГМАТИЗМА

... 1. Лекарственное средство для лечения состояния глаз, содержащееагонист мускариновогоацетилхолинового рецептора Ми, по меньшей мере одно из следующего:альфа-стимулирующий агонист, содержащий имидазолиновую группу; илинестероидное противовоспалительное средство (НПВС), обладающее селективностью к ЦОГ-2;отличающееся тем, что состояние глаз включает пресбиопию, умеренную гиперметропию, неправильный астигматизм, гиперметропическую аккомодационную эзотропию или глаукому.2. Лекарственное средство по п. 1, отличающееся тем, что лекарственное средство содержит:от около 0,01 до около 4% мас./мас. агониста мускариновогоацетилхолинового рецептора М; иот около 0,01% до около 0,5% мас./мас. альфа-стимулирующего агониста, содержащего имидазолиновую группу или от около 0,01 до около 2% НПВС, обладающего селективностью к ЦОГ-2 или и то, и другое.3. Лекарственное средство по п. 1, отличающееся тем, что лекарственное средство содержит:от около 0,01 до около 2% мас./мас. агониста мускариновогоацетилхолинового ...

ПЕРОРАЛЬНО ВВОДИМАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ЛЕЧЕНИЯ СИНДРОМА РАЗДРАЖЕННОГО КИШЕЧНИКА, СОДЕРЖАЩАЯ РЕГУЛЯТОР ПЕРИСТАЛЬТИКИ КИШЕЧНИКА, СРЕДСТВО, КОТОРОЕ ПРЕДОТВРАЩАЕТ ЗАДЕРЖКУ ГАЗОВ, И ПИЩЕВАРИТЕЛЬНЫЕ ФЕРМЕНТЫ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

... 1. Фармацевтическая композиция или состав, адаптированный для перорального введения, в форме таблетки, покрытой оболочкой таблетки или капсулы для предотвращения или лечения кишечных нарушений, где состав состоит из регулятора перистальтики кишечника, средства, которое предотвращает задержку газов, пищеварительного фермента, связующего средства, разбавителя, абсорбирующего средства, дезинтегрирующего средства, смазывающего средства и средства, способствующего скольжению.2. Фармацевтический состав по п. 1, где регулятор перистальтики кишечника выбран из группы, которая состоит из тримебутина, феноверина, мебеверина, дицикловерина, этилбромида, алосетрона, тегасерода, лоперамида, флороглюцинола, триметилфлороглюцинола, бутилскополамина и паргеверина.3. Фармацевтический состав по п.2, где регулятор перистальтики кишечника представляет собой тримебутин и его фармацевтически приемлемые соли.4. Фармацевтический состав по п.2, где регулятор перистальтики кишечника представляет собой феноверин ...

КОМБИНИРОВАННОЕ ЛЕЧЕНИЕ, ПРЕДУСМАТРИВАЮЩЕЕ ВВЕДЕНИЕ 2-АМИНО-3,5,5-ТРИФТОР-3,4,5,6-ТЕТРАГИДРОПИРИДИНОВ

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ АНТИПСИХОТИЧЕСКОЕ ЛЕКАРСТВЕННОЕ СРЕДСТВО И ИНГИБИТОР VMAT2, И ИХ ПРИМЕНЕНИЕ

АЗАГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ

... 1. Соединение формулы (I)или его стереоизомеры или таутомеры, или фармацевтически приемлемые соли каждого из вышеуказанных, включая их смеси во всех соотношениях, где2. Соединение по п. 1 или его стереоизомеры или таутомеры, или фармацевтически приемлемые соли каждого из вышеуказанных, включая их смеси во всех соотношениях, в котором остатки, не обозначенные более подробно, имеют значения, указанные для формулы (I), но в которомв Подформуле 1в Подформуле 2в Подформуле 3в Подформуле 4в Подформуле 5в Подформуле 6в Подформуле 7в Подформуле 8в Подформуле 9в Подформуле 10в Подформуле 11в Подформуле 12в Подформуле 13в Подформуле 14в Подформуле 15в Подформуле 16в Подформуле 17в Подформуле 18в Подформуле 19в Подформуле 20в Подформуле 21в Подформуле 223. Соединение по п. 1, где соединение выбирают из группы, включающей:1-(2-{6-[4-(5-Метил-пиридин-2-ил)-фенокси]-пиразин-2-иламино}-этил)-пиперидин-2-он,1-[2-(Метил-{6-[4-(5-метил-пиридин-2-ил)-фенокси]-пиразин-2-ил}-амино)-этил]-пиперидин-2-он,[6-( ...

ПРИМЕНЕНИЕ АННЕЛИРОВАННЫХ СОЕДИНЕНИЙ ПИРРОЛА ПРИ ЛЕЧЕНИИ ДЕГЕНЕРАЦИИ СУСТАВНОГО ХРЯЩА ИЛИ СТРУКТУРНЫХ ИЗМЕНЕНИЙ СУБХОНДРАЛЬНОЙ КОСТИ

... 1. Использование одного или более одного соединения формулы (I) где X представляет собой CR8R9, S, O, NR12 или C(O); A представляет собой CR10R11 или связь между X и атомом, несущим радикалы R6 и R7; первый из радикалов R1, R2, R3 представляют собой арил, необязательно замещенный одним или несколькими заместителями, независимо выбранными из группы, состоящей из галогена, алкила, галогеналкила, алкокси, арилокси, галогеналкокси, алкилтио, гидрокси, нитро, алкилсульфинил, алкилсульфонил, сульфамоил, N-алкилсульфамоил, N, N-диалкилсульфамоил, алкилсульфонамидо и алкилсульфон-N-алкиламидо; или ароматическую или неароматическую, моно- или бициклическую, необязательно бензоаннелированную, гетероциклическую группу с 1, 2 или 3 гетероатомами, независимо выбранными из N, O и S, и, необязательно, замещенную одним или более чем одним заместителями, независимо выбранными из группы, состоящей из галогена, алкила, галогеналкила, алкокси, арилокси, галогеналкокси, алкилтио, гидрокси, нитро, алкилсульфинил ...

ANNELIERTE PYRROL-VERBINDUNGEN ALS PROTONENPUMPENHEMMER ZUR BEHANDLUNG VON GESCHWÜREN

KOMBINIERTE VERWENDUNG VON HYALURONSÄURE UND THERAPEUTISCHEN WIRKSTOFFEN ZUR VERBESSERUNG DES THERAPEUTISCHEN EFFEKTS

PHARMAZEUTISCHE ZUSAMMENSETZUNG ENTHALTEND TENATOPRAZOL UND EINEN ENTZÜNDUNGSHEMMER

Piroxicam enthaltende gastrointestinale Zubereitung aus merheren Einheiten bestehend

CYANOPYRROLE ALS PROGESTERONREZEPTORAGONISTEN

VERBINDUNGEN MIT ENTZUENDUNGSHEMMENDER AKTIVITAET, HERGESTELLT DURCH KOMPLEXIERUNG MIT BETA-CYCLODEXTRIN UND PHARMAZEUTISCHE ZUSAMMENSETZUNGEN WELCHE DIESE ENTHALTEN.

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In the preparation of a medicament for treating psychiatric disorders, cyclooxygenase-2 (COX-2) inhibitor is used. An Independent claim is included for new kit-of-parts comprising a first dosage form containing neuroleptic drug or an antidepressant and a second dosage form containing a COX-2 inhibitor for simultaneous, simultaneously or sequential administration.

Verfahren zum Übertragen eines analogen Datenstroms und Schaltungsanordnung

The invention relates to a method for transmitting an analog data flow (101). According to said method, transients are compensated when the analog data flow is received, by transforming the analog data flow (101) into a digital data flow (103) by scanning the analog data flow (101) in an analog-digital converter (104), the digital data flow is then equalised in the temporal region in an equalisation device (105), the equalised digital data flow (106) is decimated in a decimation device (107) in order to obtain a decimated equalised digital data flow (109), the temporal region is transformed into the frequency region by means of a transformation device (110), transformation signals obtained (111a - 111n) are corrected in a correction device (112), at least one value signal (114) and at least one phase signal (115) are determined in a determination device (116), and the value signals (114) and the phase signals (115) are decoded in a decoding device (117), in order to obtain a decoded data ...

Intranasal analgesic composition comprising buprenorphine, & preferably chitosan or partially esterified pectin

Aqueous formulations suitable for intranasal administration comprise buprenorphine (I) or a physiologically acceptable salt or ester thereof and (a) a pectin having a degree of esterification of less than 50% or (b) chitosan and a polyoxyethylene-polyoxypropylene copolymer (poloxamer) or (c) chitosan and hydroxypropylmethylcellulose. Such formulations can induce rapid and prolonged analgesia when delivered intranasally to a patient. The buprenorphine or buprenorphine salt or ester may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration of buprenorphine, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours. Also claimed are the use of buprenorphine (or a physiologically acceptable salt or ester thereof) and a delivery agent for (i) the manufacture of a medicament for intranasal administration for the treatment of pain and (ii) the manufacture of a nasal delivery device, as well as a composition containing ...

Treatment of protein aggregation diseases

A stable parental formulation of levomepromazine and a method for stabilizing said formulation

Small molecule modulators of human STING

... (I) A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, for use in therapy is provided, wherein X is CR9R10, O, S, S=O or SO2; X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; the or each Z is independently CR11R12 or NR11; n is 1 or 2; Q is C=O, S=O, SO2, C=S or CR4R5; L is optionally substituted C1-C6alkyl, C1-C3polyfluoroalkyl, optionally substituted C3-C6cycloalkyl, optionally substituted C2-C6alkenyl, optionally substituted C2-C6alkynyl, C=O, S=O, SO2, -CH2C(O)-, -CH2CONH- or -CONH-; Y is an optionally substituted C1-C6alkyl, C1-C3polyfluoroalkyl, an optionally substituted C2-C6alkenyl, an optionally substituted C2-C6alkynyl, an optionally substituted C3-C6cycloalkyl, an optionally substituted mono or bicyclic 3 to 8 membered heterocycle; R6 is mono or bicyclic optionally substituted C5-C10aryl, mono or bicyclic optionally substituted 5 to 10 membered heteroaryl, optionally substituted C3-C6cycloalkyl or an optionally substituted mono or bicyclic 3 to ...

Compositions

Pharmaceutical compositions and their use

Pharmaceutical composition

Treatment

A NOVEL FORMULATION OF MELOXICAM

Novel use of antihistamine agents for the preventative or early treatment of inflammatory syndromes,in particular those triggered by togaviruses

PHARMACEUTICAL COMPOSITION AND THE USE THEREOF, AND APPLICATION REGIME OF SAID PHARMACEUTICAL COMPOSITION FOR ON-DEMAND CONTRACEPTION

Stable aqueous suspension

Method for the production of commercial nanoparticle and microparticle powders.

Production of encapsulated nanoparticles at commercial scale.

A novel formulation of meloxicam.

Antiviral compounds.

Methods for improving the dissolution profile of abiologically active material.

A NOVEL FORMULATION OF MELOXICAM

Use and application regimen of a pharmaceutical composition containing levonorgestrel and a cox inhibitor for on-demand contraception

Treatment of disease employing hyaluronic acid and nsaids.

A pharmaceutical composition comprising a plurality ...

Combination and formulations and the administration thereof to a mammal for the treatment of conditions and disease.

A combination for ...

Modulation of cellular activity by administering a form of hyaluronic acid.

A method for the modulation of cellular activity of tissue and cells expressing an adhesion molecule of a human, ...

Use of cox-2 inhibitors for the treatment of schizophrenia, delusional disorders, affective disorders, autism or tic disorders.

The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophre-nia, delusional disorders, affective disorders, autism or tic disorders.

New benzothiazinone derivatives and their use as antibacterial agents

Pharmaceutical formulations containing hyaluronic acid.

Pharmaceutical compositions from which effective non-toxic (to the patient)dosage amounts may be taken and applied to the skin and/or exposed tissue of a human, each effective dosage amount comprising pharmaceutical excipients suitable for topical application, an effective non-toxic dosage amount of a drug to treat and assist to resolve a disease and/or condition of the skin and/or exposed tissue of a human and an effective non-toxic dosage amount of hyaluronic acid and/or salts thereof and/or homologues, analogues, derivatives, complexes, esters, fragments, and/or sub-units of hyaluronic acid sufficient to transport (to facilitate or cause the transport of)the drug, to a site in the skin including epidermis or exposed tissue of a disease or condition for percutaneous transport into the skin and/or exposed tissue to accumulate and remain there for a prolonged period of time and which is systemic independent acting.

Pharmaceutical combinations of COX-2 inhibitors and opiates

A pharmaceutical composition comprises a combination of a selective or specific COX 2 inhibitor or a pharmaceutical!/ acceptable salt or derivative thereof and an opiate or a pharmaceuticafly acceptable salt or derivative thereof, for example a combination of meloxicam and codeine, as active ingredients, and a pharmaceutically acceptable carrier. It may include a centrally-acting cyclo-oxygenase inhibitor such as paracetamol or its pharmaceutically acceptable salts or derivatives. The pharmaceutical compositions are used in methods of providing symptomatic relief or treatment of pain, in an algesic and/or hyperalgesic state, with or without fever, in particular that associated with inflammation such as that associated with trauma, osteoarthritis, rheumatoid arthritis, noninflammatory myalgia or dysmenorrhoea.

Process for preparing diaminophenothiazinium compounds

FORMULATIONS CONTAINING HYALURONIC ACID

METHOD FOR THE PRODUCTION OF COMMERCIAL NANOPARTICLE AND MICROPARTICLE POWDERS

Modulation of cellular activity

Use of cox-2 inhibitors for preventing immunodeficiency

PRODUCTION OF ENCAPSULATED NANOPARTICLES AT COMMERCIAL SCALE

METHOD FOR IMPROVING THE DISSOLUTION PROFILE OF A BIOLOGICALLY ACTIVE MATERIAL

TREATMENT OF DISEASE EMPLOYING HYALURONIC ACID AND NSAIDS

Stable aqueous suspension.

TREATMENT OF CONDITIONS & DISEASES

Methods and compositions for restoring conformational stability of a protein of the p53 family.

The invention is in the field of cancer treatment. In particular, the present invention provides pharmaceutical compounds capable of interacting with mutant and non-mutant forms of cancer-related regulatory proteins such that the mutant protein regains the capacity to properly interact with other macromolecules, thereby restoring or stabilizing all or a portion of its wild type activity. Regulatory proteins include members of the p53 protein family such as for example, p53, p63 and p73. The compounds of the invention are useful for cancer treatment. Methods for screening for such pharmacological compounds are also provided.

Novel use of antihistamine agents for the preventative or early treatment of inflammatory syndromes,in particular those triggered by togaviruses

Stable aqueous suspension

New benzothiazinone derivatives and their use as antibacterial agents

Pharmaceutical combinations of cox-2 inhibitors and opiates

Process for prepaiIrng diaminophenothiazinium compounds

Use of Cox-2 inhibitors for the treatment of schizophrenia, delusional disorders, affective disorders, autism or tic disorders.

OFFSHORE FLUID OFFLOADING SYSTEMS AND METHODS

A NOVEL FORMULATION OF MELOXICAM

Antiviral compounds

Novel use of antihistamine agents for the preventative or early treatment of inflammatory syndromes,in particular those triggered by togaviruses

Use and application regimen of a pharmaceutical composition containing levonorgestrel and a cox inhibitor for on-demand contraception

PHARMACEUTICAL COMPOSITION AND THE USE THEREOF, AND APPLICATION REGIME OF SAID PHARMACEUTICAL COMPOSITION FOR ON-DEMAND CONTRACEPTION

METHOD FOR IMPROVING THE DISSOLUTIONPROFILE OF A BIOLOGICALLY ACTIVE MATERIAL

ANTIVIRAL COMPOUNDS

A NOVEL FORMULATION OF MELOXICAM

A NOVEL FORMULATION OF MELOXICAM

A novel formulation of meloxicam.

Antiviral compounds.

Method for the production of commercial nanoparticle and microparticle powders.

Offshore fluid offloading systems and methods

Methods for improving the dissolution profile of abiologically active material.

Use of cox-2 inhibitors for preventing immunodeficiency.

The present invention provides a method for treating or preventing a disorder typified by an immunodeficiency (e.g. HIV), wherein the patient is administered a COX-2 inhibitor or derivative or pharmaceutically acceptable salt thereof, preferably diisopropylfluophasphaate, L-745337, rofecoxi, NS 398, SC 58125, etodolac, meloxicam, celecoxib flusolide or nimesulide, and compositions and products containing the same or use of the same in preparing medicaments and for treatment.

Anti-Emetic Substance

The present invention provides a therapeutic solution for effective control of symptoms related to nausea and vomiting. The therapeutic solution is a pharmaceutical composition which combines anti-emetics of different classes. These classes include dopamine receptor antagonists, serotonin receptor antagonists, butyrphenones, and neurokinin receptor antagonists. The combination of different anti-emetics mitigates adverse affects of a single anti-emetic alone while increasing drug efficacy and decreasing cost of administration to the individual patient.

5,6-dihydro-1h-pyridin-2-one compounds

The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.

Novel formulation of meloxicam

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.

Aggregates with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin

The invention describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component alternatively, can take the role of a drug. The disclosure further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The disclosure also provides methods and favourable conditions for carrier manufacturing and application.

Pharmaceutical Compositions

Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Production of encapsulated nanoparticles at commercial scale

The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.

Oral lysophilisates containing pvp/va

The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.

4-amino-1,3-thiazine or oxazine derivative

The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-β proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.

Piroxicam-Containing Transdermally Absorbable Preparation

An adhesive patch is provided in which piroxicam is formulated as a non-steroidal anti-inflammatory analgesic. In particular, provided is a piroxicam-containing transdermally absorbable adhesive patch in which an absorption promoter to piroxicam is formulated to achieve high anti-inflammatory and analgesic effects without inhibiting releasing of these drugs. The piroxicam-containing transdermally absorbable adhesive patch contains piroxicam as a medicinal component and oxybuprocaine or a pharmaceutically acceptable salt thereof as an absorption promoter. In the piroxicam-containing transdermally absorbable adhesive patch, the content of piroxicam is from 0.1% to 5% by weight to the total weight of a drug-containing plaster and the content of oxybuprocaine or the pharmaceutically acceptable salt thereof is from 1% to 30% by weight to the total weight of the drug-containing plaster.

Pain Relieving Composition

A pain relieving composition that includes an anesthetic in the range of 0.5%-7.0% by weight (“w/w”), an anti-inflammatory agent in the range of 1.0%-11.0% w/w, a moisturizing agent in the range of 0.5%-12.0% w/w, a humectant in the range of 0.5%-13.0% w/w, a penetration enhancing agent in the range of 0.5%-7.0%, and a carrier solvent in the range of 40.0%-97.0% w/w to be used before and/or after procedures which cause damage to human skin.

Small-molecule inhibitors of dengue and west nile virus proteases

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.

Use of meloxicam for the long-term treatment of musculoskeletal disorders in cats

The invention is directed to the use of a formulation comprising meloxicam or a pharmacologically acceptable meloxicam salt of an organic or inorganic base thereof for the long-term treatment of musculoskeletal disorders in cats. No negative effects on renal function occur following a treatment from 10 to 20 months or more.

Treatment of Cancer with Dopamine Receptor Antagonists

Described are methods of treating a cancer comprising administering to a subject in need thereof an effective amount of a dopamine receptor (DR) antagonist. The DR antagonist may be a phenothiazine derivative, such as thioridazine or chlorpromazine. Optionally, the cancer is acute myeloid leukemia. Also described are methods for identifying subjects with cancer, methods for providing a prognosis for a subjects with cancer and methods for identifying subjects likely to be responsive to therapy with DR receptor antagonists. Methods for identifying cancer stem cells and chemotherapeutic compounds that are DR receptor antagonists as also provided. Also described are methods for the identification and validation of agents that target cancer stem cells. 1. A method for identifying and validating a test agent as a selective anti-cancer stem cell agent , the method comprising:i) contacting one or more variant neoplastic stem cells with the test agent and one or more normal stem cells with the test agent;ii) detecting a change in cell count of the variant neoplastic stem cells in response to the test agent, and detecting a change in cell count of the normal stem cells in response to the test agent;iii) identifying the test agent as a selective anti-cancer stem cell agent if contact with the test agent induces a decrease in cell count of the variant neoplastic stem cells without inducing a comparable decrease in the normal stem cells.2. The method of claim 1 , further comprising claim 1 , contacting the variant neoplastic stem cells and the normal stem cells with the test agent at a plurality of test concentrations and detecting a change in cell count for the one or more variant neoplastic stem cells and for the normal stem cells at the plurality of test concentrations.3. The method of claim 2 , wherein the plurality of test concentrations varies by at least about 3 claim 2 , 4 or 5 orders of magnitude.4. The method of claim 2 , wherein the plurality of concentrations varies ...

Taste masked pharmaceutical composition

This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

Topical antimicrobial compositions and methods of using same

The invention includes a method of treating a mammal comprising topically applying an aqueous composition to a target site on the mammal, wherein the aqueous composition comprises: active ingredients comprising i) a cosmetic dye selected from a violet, blue or green dye, or combinations thereof, and ii) an enhancing ingredient, wherein the relative weight percentage of the cosmetic dye to the enhancing ingredient is about 1:2 to about 40:1, wherein the cosmetic dye interacts with keratinous material thereby i) substantially staining the target site and ii) inhibiting the active ingredients from significantly leaching from the target site. 1. A method of treating a mammal comprising topically applying an aqueous composition to a target site on the mammal , wherein the aqueous composition comprises: active ingredients comprising i) a cosmetic dye selected from a violet , blue or green dye , or combinations thereof , and ii) an enhancing ingredient , wherein the relative weight percentage of the cosmetic dye to the enhancing ingredient is about 1:2 to about 40:1 , wherein the cosmetic dye interacts with keratinous material thereby i) substantially staining the target site and ii) inhibiting the active ingredients from significantly leaching from the target site.2. The method of wherein the relative weight percentage of the cosmetic dye to the enhancing ingredient is about 10:1.3. The method of wherein the relative weight percentage of the active ingredients to water is about 1:5 to about 1:1000.4. The method of wherein the mammal is bovine livestock.5. The method of wherein treating the bovine livestock comprises inhibiting disease claim 4 , preventing disease claim 4 , assisting in healing lesions claim 4 , maintaining or improving hygiene claim 4 , or combinations thereof.6. The method of wherein the target site is the hoof the livestock.7. The method of wherein the livestock is treated for hoof rot claim 6 , foot rot claim 6 , digital dermatitis and/or interdigital ...

Hyaluronic Acid Decomposition-Promoting Factor and Inhibitor Thereof

The present invention is directed to KIAA1199, which is a novel factor involved in decomposition of hyaluronic acid, and to use thereof. More specifically, the invention is directed to a hyaluronic acid decomposition-promoting agent containing the KIAA1199 gene and a protein encoded by the gene; to a hyaluronic acid decomposition-inhibiting agent characterized by inhibiting the activity or expression thereof (including an siRNA or a monoclonal antibody); and to a method for screening a novel hyaluronic acid decomposition-controlling agent, in which the method contains employing the expression of KIAA1199 as an index. 1. A method for screening a hyaluronic acid decomposition-controlling agent , wherein the method comprises assessing a hyaluronic acid decomposition controlling effect of a test substance by use of cells in which a KIAA1199 gene is highly expressed transiently or stably.2. The method according to claim 1 , wherein the hyaluronic acid decomposition controlling effect of the test substance is assessed on the basis of the expression level of the KIAA1199 gene or a protein encoded by the KIAA1199 gene as an index.3. The method according to claim 1 , which comprises the following steps:1) culturing cells in the presence or absence of the test substance;2) determining the expression level of the KIAA1199 gene or a protein encoded by the KIAA1199 gene in the cells; and3) assessing the hyaluronic acid decomposition controlling effect of the test substance on the basis of the difference between the expression level of the KIAA1199 gene or the protein encoded by the KIAA1199 gene in the cells determined in the presence of the test substance and that determined in the absence of the test substance.4. The method according to claim 1 , which comprises the following steps:1) culturing cells in coexistence with a labeled hyaluronic acid in the presence or absence of the test substance;2) recovering a culture supernatant after culturing, and determining a molecular ...

Dual Controlled Release Dosage Form

A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

METHOD OF USING BIOTHIONOL AND BIOTHIONOL-LIKE COMPOUNDS AS ANTI-ANGIOGENIC AGENTS

The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine. 114-. (canceled)17. The method of wherein Alk is an 1 claim 16 ,2-ethanediyl radical.18. The method of wherein the compound of Formula (I) is Ritanserin.19. (canceled)20. (canceled)22. The method of wherein the compound of Formula (III) is Terfenadine.24. The method of wherein the compound of Formula (IV) is Perphenazine.25. (canceled)26. (canceled)28. The method of wherein the compound of Formula (VI) is Clomipramine.31. The method of wherein Alk is an 1 claim 30 ,2-ethanediyl radical.32. The method of wherein the compound of Formula (I) is Ritanserin.33. (canceled)34. (canceled)36. The method of wherein the compound of Formula (III) is Terfenadine.38. The method of wherein the compound of Formula (IV) is Perphenazine.39. (canceled)40. (canceled)42. The method of wherein the compound of Formula (VI) is Clomipramine.44. The method of wherein the compound of Formula (VI) is Clomipramine. The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to the patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect in preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadine, Perphenazine, Bithionol, and Clomipramine.Angiogenesis is the formation of new blood vessels out of pre- ...

METHODS FOR ALLEVIATING CHRONIC PAIN AND IMPROVING PERFORMANCE OF CATTLE UNDERGOING DEHORNING OR CASTRATION

Methods of improving performance, increasing weight gain, and decreasing incidence of disease in ruminant and pre-ruminant animals, such as cattle, after undergoing painful processing procedures, such as castration and dehorning, are provided. Veterinary formulations for use in methods of the invention are also provided. The formulations comprise a compound selected from the group consisting of meloxicam, gabapentin, the pharmaceutically acceptable salts thereof, and combinations thereof. Methods of treating pathological pain in cattle are also provided. 14-. (canceled)5. A method of improving the performance of a ruminant or pre-ruminant animal following processing , comprising:orally administering to said animal an effective amount of meloxicam or a pharmaceutically acceptable salt thereof; andsubjecting said animal to processing, wherein said animal has improved performance after said processing.6. The method of claim 5 , wherein said animal is a bovine.7. The method of claim 5 , wherein said processing is selected from the group consisting of dehorning claim 5 , castration claim 5 , branding claim 5 , and combinations thereof.8. The method of claim 5 , wherein said meloxicam or pharmaceutically acceptable salt thereof is administered to said animal in an amount sufficient to provide a level of meloxicam of from about 0.1 mg/kg body weight to about 5 mg/kg body weight of said animal.9. The method of claim 5 , wherein said meloxicam or pharmaceutically acceptable salt thereof is in the form of a tablet claim 5 , capsule claim 5 , liquid claim 5 , granule claim 5 , top-dress claim 5 , suspension claim 5 , bolus claim 5 , drench claim 5 , solution claim 5 , topical pour-on claim 5 , sustained-release implant claim 5 , or rectal suppository.10. The method of claim 5 , wherein said meloxicam is administered to said animal up to about 72 hours before said processing.11. The method of claim 5 , wherein said improved performance is selected from the group consisting of ...

METHOD OF DRUG DETOXIFICATION

A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state. 1. A method of detoxifying a patient addicted to at least one drug , said method comprising the steps of:administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient;administering an anesthetic component to the patient for putting the patient in a sedated state;administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state;administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state; andterminating administration of the anesthetic component to the patient for reviving the patient from the sedated state;wherein the first-medication component comprises gabapentin, ropinirole, citric acid sodium citrate, famotidine, glycopyrrolate, ondansetron, dexamethasone, midazolam, or combinations thereof.2. A method as set forth in wherein the patient is in the sedated state ...

Aminodihydrothiazine derivatives

A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR′; R 1 is a hydrogen atom or lower alkyl; R 2a , R 2b , R 3a , R 3b , R 4a and R 4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R 5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.

COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES

Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. 2. The method of claim 1 , wherein both of Rand Rare H.3. The method of claim 1 , wherein both of Rand Rare alkyl.4. The method of claim 1 , wherein both of Rand Rare methyl.5. The method of claim 1 , wherein m is 1.6. The method of claim 1 , wherein L is NRSO claim 1 , SONR claim 1 , C(O)NR claim 1 , NRC(O) claim 1 , OC(O)NR claim 1 , NRC(O)O claim 1 , or NRC(O)NR.7. The method of claim 1 , wherein L is C(O)NRor NRC(O).8. The method of claim 1 , wherein Ris thiazolyl.9. The method of claim 1 , wherein Ris phenyl.10. The method of claim 1 , wherein Ris phenyl substituted with 2 R.11. The method of claim 1 , wherein Ris H.12. The method of claim 1 , wherein the compound is administered via intramuscular injection.13. The method of claim 1 , wherein the compound is administered topically.14. The method of claim 1 , wherein the compound is administered by topical ocular administration.15. The method of claim 1 , wherein the compound is administered prior to the exposure to the chemical warfare agent.16. The method of claim 1 , wherein the compound is administered after exposure to the chemical warfare agent.17. The method of claim 1 , wherein the chemical warfare agent is tear gas.18. The method of claim 1 , wherein the chemical warfare agent is chlorine.19. The method of claim 1 , wherein the chemical warfare agent is mustard gas.20. The method of claim 1 , wherein the subject is a human.21. The method of claim 1 , wherein the compound is administered orally. This application claims priority from U.S. Ser. No. 61/127,662, filed May 14, 2008, and U.S. Ser. No. 61/082,809, filed Jul. 22, 2008, both of which are incorporated herein by reference in their entirety.The invention relates to compounds and compositions useful for treating injuries caused by chemical warfare and similar agents.A variety of ion channel proteins exist to mediate ion flux across ...

Composition and method for compounded therapy

The present embodiments relate to topically delivered compounded medications. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include low concentrations of local anesthetics, a NSAID, an anticonvulsant, and/or other active ingredients. For instance, the transdermal cream may include lidocaine, prilocaine, meloxicam, and lamotrigine and/or topiramate. Alternatively, the transdermal cream may include a lidocaine/prilocaine base cream to which is added a fine powder of one or more ground up medications to form a compounded medication. The compounded medication in powder form may be generated from grinding up tablets of NSAIDs, anticonvulsants, nerve depressants, antidepressants, muscle relaxants, NMDA receptor antagonists, opiate or opioid agonists, and/or other agents. The compounded medication in powder form may include meloxicam, lamotrigine, topiramate, and/or other active ingredients. In another aspect, the present embodiments relate to methods of compounding medications and transdermal creams or gels.

HIGHLY CONCENTRATED STABLE MELOXICAM SOLUTIONS

Aqueous cyclodextrin-free solution of meloxicam for administration by oral or parenteral route, containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients, the content of dissolved meloxicam salt being more than 10 mg/mL. The formulation according to the invention has a shelf-life of up to 24 months or more. 1. A treatment method for treating a mammal suffering from one or more of pain , inflammation , fever , acute mastitis , diarrhea , lameness , locomotor deficiency , or respiratory illness , the method comprising administering to the mammal an aqueous , cyclodextrin-free solution comprising a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients , wherein the concentration of dissolved meloxicam salt is more than 10 mg/mL.2. The method according to claim 1 , wherein the method is used in conjunction with antibiotic therapy.3. The method according to claim 1 , wherein the solution is administered in a dosage range of from 0.2 to 1.0 mg of active substance/kg of bodyweight of the mammal.4. The method according to claim 1 , wherein the solution is administered in a dosage range of from 0.4 to 0.8 mg of active substance/kg of bodyweight of the mammal.5. The method according to claim 1 , wherein the solution is administered in a dosage range of from 0.5 to 0.7 mg of active substance/kg of bodyweight of the mammal.6. A treatment method for treating an animal suffering from one or more of pain claim 1 , inflammation claim 1 , fever claim 1 , acute mastitis claim 1 , diarrhea claim 1 , lameness claim 1 , locomotor deficiency claim 1 , or respiratory illness claim 1 , the method comprising administering to the animal an aqueous claim 1 , cyclodextrin-free solution comprising:a pharmacologically acceptable meloxicam salt; andan excipient selected from the group consisting of citric acid, lecithin, gluconic acid, tartaric acid, phosphoric acid, and ...

2-(R2-THIO)-10-[3-(4-R1-PIPERAZIN-1-YL) PROPYL]-10H-PHENOTHIAZINE FOR TREATING A BETA-AMYLOIDOPATHY OR AN ALPHA-SYNUCLEOPATHY, AND METHOD FOR THE DIAGNOSIS OR PREDIAGNOSIS THEREOF

The invention relates to 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to general formula I, for treating a β-amyloidopathy or an α-synucleinopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter. The invention also relates to a method for the diagnosis or prediagnosis of a β-amyloidopathy or an α-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter. 2. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to claim 1 , characterized in that wherein the halogen atom/the halogen atoms are selected from the group consisting of fluorine and chlorine.3. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to claim 1 , wherein Rand Rare the same or different and each independently of one another is a C-Calkyl group.4. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to claim 1 , wherein the residues Rand Rare hydrogen.5. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to claim 1 , wherein the residue Ris a methyl group claim 1 , the residue Ris an ethyl group claim 1 , and the residues Rand Rare hydrogen.6. A composition comprising a 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazine according to claim 1 , further comprising a further active substance.7. A composition according to claim 6 , wherein a 1-benzohydrylpiperazine is a further active substance.8. A composition according to claim 7 , wherein 1-benzohydryl-4-cinnamyl piperazine is the 1-benzohydrylpiperazine.9. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H-phenothiazines according to claim 1 , wherein the β-amyloidopathy is Alzheimer's dementia.10. A 2-(R-thio)-10-[3-(4-R-piperazin-1-yl)propyl]-10H- ...

SUSTAINED RELEASE FORMULATION OF A NON-STEROIDAL ANTI-INFLAMMATORY DRUG

Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided. 1. A formulation of one or more non-steroidal anti-inflammatory drugs , comprising:one or more non-steroidal anti-inflammatory drugs; andmultivesicular liposomes,wherein the one or more non-steroidal anti-inflammatory drugs are encapsulated in the multivesicular liposomes.2. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is chosen from the group consisting of indomethacin claim 1 , sulindac claim 1 , etodolac claim 1 , mefenamic acid claim 1 , meclofenamic acid claim 1 , meclofenamate sodium claim 1 , flufenamic acid claim 1 , tolmetin claim 1 , ketorolac claim 1 , diclofenac claim 1 , diclofenac sodium claim 1 , ibuprofen claim 1 , naproxen claim 1 , naproxen sodium claim 1 , fenoprofen claim 1 , ketoprofen claim 1 , flurbiprofen claim 1 , oxaprozin piroxicam claim 1 , meloxicam claim 1 , ampiroxicam claim 1 , droxicam claim 1 , pivoxicam claim 1 , lornoxicam claim 1 , cinnoxicam claim 1 , sudoxicam claim 1 , and tenoxicam.3. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is diclofenac.4. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is piroxicam.5. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is meloxicam.6. The formula of claim 1 , wherein said non-steroidal anti-inflammatory drug is ketorolac.7. The formulation as in claim 1 , wherein the multivesicular liposomes further comprise cholesterol claim 1 , one or more phospholipids claim 1 , including salts of the phospholipids claim 1 , and one or more ...

SUSTAINED RELEASE FORMULATION OF A NON-STEROIDAL ANTI-INFLAMMATORY DRUG

Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided. 1. A formulation of one or more non-steroidal anti-inflammatory drugs , comprising:one or more non-steroidal anti-inflammatory drugs; andmultivesicular liposomes,wherein the one or more non-steroidal anti-inflammatory drugs are encapsulated in the multivesicular liposomes.2. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is chosen from the group consisting of indomethacin claim 1 , sulindac claim 1 , etodolac claim 1 , mefenamic acid claim 1 , meclofenamic acid claim 1 , meclofenamate sodium claim 1 , flufenamic acid claim 1 , tolmetin claim 1 , ketorolac claim 1 , diclofenac claim 1 , diclofenac sodium claim 1 , ibuprofen claim 1 , naproxen claim 1 , naproxen sodium claim 1 , fenoprofen claim 1 , ketoprofen claim 1 , flurbiprofen claim 1 , oxaprozin piroxicam claim 1 , meloxicam claim 1 , ampiroxicam claim 1 , droxicam claim 1 , pivoxicam claim 1 , lornoxicam claim 1 , cinnoxicam claim 1 , sudoxicam claim 1 , and tenoxicam.3. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is diclofenac.4. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is piroxicam.5. The formulation of claim 1 , wherein said non-steroidal anti-inflammatory drug is meloxicam.6. The formula of claim 1 , wherein said non-steroidal anti-inflammatory drug is ketorolac.7. The formulation as in claim 1 , wherein the multivesicular liposomes further comprise cholesterol claim 1 , one or more phospholipids claim 1 , including salts of the phospholipids claim 1 , and one or more ...

PIROXICAM FOR PROPHYLACTICALLY AND THERAPEUTICALLY TREATING HERPES INFECTIONS

The invention relates to an agent for the prophylactic and therapeutic treatment of virus infections, said agent containing piroxicam in a carrier substance. 1. Agent for the prophylactic and therapeutic treatment of virus infections caused by a virus of the family of herpesviridae , characterized in that said agent contains piroxicam in a carrier substance.2. Agent according to claim 1 , characterized by a content of piroxicam ranging between 0.1 and 10% w/w.3. Agent according to claim 2 , characterized by a content of piroxicam ranging between 1 and 5 w/w.4. (canceled)5. Agent according to characterized in that the virus infection is an infection caused by herpes simplex.6. Agent according to for topical administration.7. Agent according to claim 5 , in the form of a cream claim 5 , ointment claim 5 , tincture or gel.8. Agent according to for infusion or injection.9. Agent according to claim 5 , wherein the virus infection is an infection caused by herpes labialis. The invention relates to an agent for the prophylactic and therapeutic treatment of virus infections, e.g. herpes infections, in particular involving herpes simplex.The treatment of virus infections in humans and animals has always been a great challenge due to the fact that only a limited number of active agents is available and this is also true for the family of herpesviruses.The family of Herpesviridae comprises a great number of viruses having a double-stranded DNA. Widely spread are herpes simplex viruses of type HSV 1 and HSV 2 as well as the herpes varicella zoster virus VZV. All cause painful infections in the form of superficial inflammation. Herpesviruses remain dormant within the human body for a long time so that the outbreaks of the disease will occur repeatedly and may even display serious symptoms.Herpes simplex infections will primarily affect the mouth and manifest themselves in the form of blisters and lesions on mucous membranes and lips. Varicella zoster infections manifest ...

WATER-SOLUBLE MELOXICAM GRANULES

Water soluble meloxicam granules include meloxicam, a salt forming agent which forms the meglumine, sodium, potassium, or ammonium salt of meloxicam, a binder, a sugar or sweetener, and a carrier, and a flavoring agent. 1. A method of treating animals comprising administering water soluble granules to an animal , the water soluble granules comprising meloxicam; a salt forming agent operable to form a meloxicam salt; a binder; and a carrier.2. The method according to further comprising dissolving the water soluble granules in water prior to administration.3. The method according to further comprising mixing the water soluble granules with animal feed prior to administration.4. The method according to claim 1 , wherein the salt forming agent is selected from the group consisting of meglumine claim 1 , sodium claim 1 , potassium claim 1 , or ammonium meloxicam salt.5. The method according to claim 1 , wherein the salt forming agent is meglumine.6. The method according to claim 1 , wherein the binder is selected from hydroxypropylmethylcellulose claim 1 , polyvinylpyrrolidone claim 1 , gelatine claim 1 , starch claim 1 , or polyethylene glycol ether.7. The method according to claim 6 , wherein the binder is present in an amount of 20 mg/g to 150 mg/g.8. The method according to claim 1 , wherein the water soluble granules are administered in conjunction with antibiotic treatment.9. The method according to claim 1 , wherein the animal includes horses claim 1 , pigs claim 1 , cattle claim 1 , dogs claim 1 , or cats.10. The method according to claim 1 , wherein the meloxicam granules comprises meloxicam claim 1 , meglumine claim 1 , hydroxypropylmethylcellulose claim 1 , povidone claim 1 , and glucose monohydrate.11. The method according to claim 1 , wherein the granules possess a particle size distribution of 125 μm to 500 μm.12. The method according to claim 1 , wherein:the salt forming agent is meglumine;the molar ratio of meglumine and meloxicam is 9:8 to 12:8.13. An ...

Low Concentration Meloxicam Tablets

A solid tablet formed through direct compression of powder, the powder comprising meloxicam as an active ingredient and one or more excipients which are homogenously dispersed within the tablet that can be broken into two, three or four units with each unit containing equal amounts of the meloxicam. 1. A method of forming a chewable , solid tablet for administration to companion animals , the method comprising:(a) mixing meloxicam or a pharmaceutically acceptable salt thereof with a first portion of a primary filler to form a first mixture,(b) screening the first mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a first screened mixture;(c) mixing a second portion of the first filler with a second filler to form a second mixture;(d) screening the second mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a second screened mixture;(e) combining the first screened mixture with the second screened mixture to form a final mixture;(f) compressing the final mixture into a tablet having a diameter of 10 mm-20 mm; and(g) scoring the tablet to enable the division of the tablet into individually administered doses,wherein the meloxicam or pharmaceutically is homogenously distributed within the tablet.2. The method of further comprising screening the final mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a final screened mixture before compression.3. The method according to wherein:the first and second fillers are selected from the group consisting of calcium phosphate, lactose, maltodextrin, mannitol, sorbitol, cross-linked polyvinyl pyrrolidone, sodium carboxymethyl cellulose, starch and microcrystalline cellulose; andthe first filler is different from the second mixture.4. The method according to claim 1 , further comprising:mixing a first excipient with a second excipient to form an excipient mixture;screening the excipient mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a screened excipient ...

BUCCAL, POLAR AND NON-POLAR SPRAY OR CAPSULE CONTAINING DRUGS FOR TREATING METABOLIC DISORDERS

Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant. 1111-. (canceled)112. A propellant free buccal spray composition for transmucosal administration of an active compound comprising:(a) meloxicam or a pharmaceutically acceptable salt thereof in an amount of between about 0.001 and about 60 percent by weight of the total composition; and(b) a polar solvent in an amount of about 5 to about 30 percent by weight of the total composition.113. The composition of claim 112 , wherein the polar solvent is present in an amount of about 7.5 to about 20 percent by weight of the total composition.114. The composition of claim 113 , wherein the polar solvent is present in an amount of about 9 to about 15 percent by weight of the total composition.115. The composition of claim 112 , wherein the polar solvent comprises aqueous ethanol.116. A pump spray container comprising:a pump spray formulation comprising a propellant free buccal spray composition for transmucosal administration of an active compound comprising:(a) meloxicam or a pharmaceutically acceptable salt thereof; and(b) a polar solvent.117. The pump spray container of claim 116 , wherein the meloxicam is present in an amount between about 0.001 and about 60 percent by weight of the total composition.118. The pump spray container of claim 116 , wherein the polar solvent is present in an amount of about 5 to about 30 percent by weight of the total ...

Antiviral compound and cox-2 inhibitor combination therapy for functional somatic syndromes, including combination of famciclovir and celecoxib

The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.

VALACICLOVIR AND MELOXICAM COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor meloxicam. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and meloxicam. 1. A combination comprising a therapeutically-effective amount of valaciclovir and a therapeutically-effective amount of meloxicam , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1500 mg , and wherein the amount of meloxicam is present in a unit dosage form from about 15 mg to about 30 mg.2. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1050 mg.3. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 1050 mg to about 1500 mg.4. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form selected from the group consisting of about 750 mg claim 1 , about 1050 mg claim 1 , about 1250 mg and about 1500 mg.5. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg.6. The combination of claim 1 , wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.7. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg claim 1 , and wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache ...

FAMCICLOVIR AND MELOXICAM COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor meloxicam. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and meloxicam. 1. A combination comprising a therapeutically-effective amount of famciclovir and a therapeutically-effective amount of meloxicam , wherein the amount of famciclovir is present in a unit dosage form from about 125 mg to about 1000 mg , and wherein the amount of meloxicam is present in a unit dosage form from about 15 mg to about 30 mg.2. The combination of claim 1 , wherein the amount of famciclovir is present in a unit dosage form from about 125 mg to about 500 mg.3. The combination of claim 1 , wherein the amount of famciclovir is present in a unit dosage form from about 500 mg to about 1000 mg.4. The combination of claim 1 , wherein the amount of famciclovir is present in a unit dosage form selected from the group consisting of about 125 mg claim 1 , about 250 mg claim 1 , about 500 mg and about 1000 mg.5. The combination of claim 1 , wherein the amount of famciclovir is present in a unit dosage form of about 250 mg or about 500 mg.6. The combination of claim 1 , wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.7. The combination of claim 1 , wherein the amount of famciclovir is present in a unit dosage form of about 250 mg or about 500 mg claim 1 , and wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache claim 1 , chronic ...

ACICLOVIR AND MELOXICAM COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound aciclovir and a therapeutically-effective amount of the COX-2 inhibitor meloxicam. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of aciclovir and meloxicam. 1. A combination comprising a therapeutically-effective amount of aciclovir and a therapeutically-effective amount of meloxicam , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 1600 mg , and wherein the amount of meloxicam is present in a unit dosage form from about 15 mg to about 30 mg.2. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 800 mg.3. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 800 mg to about 1600 mg.4. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form selected from the group consisting of about 400 mg claim 1 , about 800 mg claim 1 , about 1200 mg and about 1600 mg.5. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 800 mg.6. The combination of claim 1 , wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.7. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 1200 mg claim 1 , and wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache claim 1 , chronic neck pain claim ...

METHOD AND COMPOSITION FOR TREATING ALZHEIMER'S DISEASE AND DEMENTIAS OF VASCULAR ORIGIN

A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans. 1. A method of treating Alzheimer's disease comprising administering to a mammal in need thereof a therapeutically effective amount of a specific endothelin-A antagonist.2. The method of wherein the specific endothelin-A antagonist is selected from the group consisting of BMS-182874 claim 1 , BQ123 TBC2576 claim 1 , TBC3214 claim 1 , PD180988 claim 1 , RPR118031A claim 1 , SB247083 claim 1 , and mixtures thereof.3. The method of wherein the endothelin antagonist comprises BQ123.4. The method of further comprising administering a therapeutically effective amount of a second therapeutic agent useful in the treatment of Alzheimer's disease.5. The method of wherein the second therapeutic agent comprises a cholinesterase inhibitor.6. The method of wherein the cholinesterase inhibitor is selected from the group consisting of tacrine claim 5 , metrifonate claim 5 , bethanacol claim 5 , physostigmine claim 5 , donepezil claim 5 , rivastigmine claim 5 , galantamine claim 5 , and mixtures thereof.7. The method of wherein the second therapeutic agent comprises a statin.8. The method of wherein the statin is selected from the group consisting of atorvastatin claim 7 , fluvastatin claim 7 , lovastatin claim 7 , pravastatin claim 7 , and mixtures thereof.9. The method of wherein the second therapeutic agent is selected from the group consisting of a nonsteroidal antiinflammatory drug claim 4 , memantine claim 4 , CX516 claim 4 , AN-1792 claim 4 , COSNIShunt claim 4 , and mixtures thereof.10. The method of wherein the endothelin antagonist and second therapeutic agent are administered simultaneously.11. The method of wherein the endothelin antagonist and second therapeutic agent are administered from a single ...

Pharmaceutical Forms and Methods for Designing the Same

Methods for selecting active principles to be used in association within a single pharmaceutical form, the method comprising searching, selecting and analyzing published bibliographic data. The disclosure also relates computer-implemented methods for selecting active principles to be used in association within a single pharmaceutical form, comprising: selecting with a processor-implemented process at least one listing of keywords stored in memory; and submitting the keywords in a query. Further, the specification relates to pharmaceutical oral forms defined by implementing these methods, wherein at least two active principles are brought together in a leak proof water-soluble wrapping or envelop and the active principles cannot come into contact with one another.

TOPICAL COMPOSITIONS

Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn. 1. A composition comprising a non-steroidal anti-inflammatory drug (NSAID) , a solvent system , water , and from zero to about 60% (wt/wt of composition) alkanol , wherein(i) the solvent system comprises at least two solvent alcohols;(ii) one of the at least two solvent alcohols is a polyethylene glycol, a propylene glycol, glycerin, polyether polyol, butylene glycol, or an alkyl glycerol derivative selected from polysorbate, sorbitol, and panthenol;(iii) the solvent system has about a 20% super solvent effect or greater;(iv) the solvent system is present in an amount sufficient to solubilize the NSAID;(v) the NSAID is in an amount of about 12% (wt/wt of composition) to about 30% (wt/wt of composition);(vi) the composition is a single phase composition; and(vii) the water is at least about 20% of the composition.2. The composition of wherein the other one of at least two solvent alcohols is selected from the group consisting of polyethylene glycols claim 1 , propylene glycols claim 1 , glycerin claim 1 , polyether polyols claim 1 , butylene glycols; glycerol derivatives claim 1 , ethanol claim 1 , and isopropanol.3. The composition of wherein the ...

COMPOUND FORMULATIONS

Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods. 1. A pharmaceutical composition in solid dosage form comprising , as active ingredient , MTC , said composition further comprising at least one diluent suitable for direct compression , characterised in that the MTC exists in a substantially pure and stable polymorphic form.2. A composition as claimed in claim 1 , wherein the MTC is in polymorph Form A.3. A composition as claimed in or claim 1 , wherein the amount of MTC in the composition is more than about 10% w/w claim 1 , or more than 20% claim 1 , or more than 30% w/w.4. A composition as claimed in claim 3 , wherein the amount of MTC is less than about 75% w/w claim 3 , or less than 60% or less than 50% w/w.5. A composition as claimed in claim 4 , wherein the amount of MTC in the composition is from about 10% w/w (or 20% or 30%) to about 70% w/w (or 60% or 50%).6. A composition as claimed in any preceding claim claim 4 , which comprises at least 15% w/w claim 4 , at least 20% claim 4 , at least 30% claim 4 , at least 40% or at least 50% w/w of diluent(s).7. A composition as claimed in any preceding claim claim 4 , wherein the diluent(s) are selected from the group consisting of microcrystalline cellulose claim 4 , lactose claim 4 , mannitol claim 4 , calcium salts such as calcium phosphate dibasic claim 4 , calcium sulphate and calcium carbonate claim 4 , and sugars such as lactose claim 4 , sucrose claim 4 , dextrose and maltodextrin.8. A composition as claimed in any preceding claim claim 4 , which further comprises a lubricant.9. A composition as claimed in claim 8 , wherein the lubricant is selected from the group consisting of magnesium stearate claim 8 , calcium stearate claim 8 , sodium stearyl fumarate claim 8 , stearic acid claim 8 , ...

NOVEL USE

The present invention relates to the use of one or more compounds selected from the following classes of biologically active agents: an a-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator and/or a vitamin, or a pharmaceutically acceptable derivative thereof, for use in the treatment of a microbial infection and in particular for killing multiplying, non-multiplying and/or clinically latent microorganisms associated with such an infection. 1. Use of one or more compounds selected from the following: an α-adrenergic antagonist , an anthelmintic agent , an antifungal agent , an antimalarial agent , an antineoplastic agent , an antipsychotic agent , an antioxidant , a vasodilator and/or a vitamin , or a pharmaceutically acceptable derivative thereof , for the treatment of a microbial infection; with the proviso that when the biologically active agent is an antifungal agent , the microbial infection is a bacterial infection.2. Use according to for killing multiplying microorganisms associated with a microbial infection.3. Use according to for killing non-multiplying microorganisms associated with a microbial infection.4. Use according to for killing clinically latent microorganisms associated with a microbial infection.5. Use according to wherein the infection is a bacterial infection.6Staphylococcus aureus, Escherichia coliPseudomonas aeruginosa.. Use according to wherein the infection is caused by or7Staphylococcus aureus.. Use according to wherein the infection is caused by8. Use according to wherein the microbial infection is a fungal infection.9Aspergillus fumigatus, Candida albicans, Cryptococcus neoformans, Histoplasma capsulatumPneumocystis jiroveci.. Use according to wherein the infection is caused by and10gardnerellaStaph. epidermidis, Strept. agalactiae, Strept. pyogenes, Escherichia coli, Klebs. pneumoniae, Klebs. oxytoca, Pr. mirabilis, Pr. ...

Acamprosate formulations, methods of using the same, and combinations comprising the same

Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

BMP-2 Upregulating Compounds For Healing Bone Tissue And Screening Methods For Selecting Such Compounds

The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit. 1. A method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an Hreceptor antagonist , whereby endogenous BMP-2 up-regulation is stimulated in said subject.2. The method of independent claim 1 , wherein said Hreceptor antagonist is one or more antagonists selected from the following: a first a first generation Hreceptor antagonist and a second generation Hreceptor antagonist.3. The method of independent claim 1 , wherein said Hreceptor antagonist is selected from the group consisting of terfenadine claim 1 , promethazine claim 1 , ebastine claim 1 , pheniramine claim 1 , carebastine and astemizole.4. The method of independent claim 1 , wherein said Hreceptor antagonist is terfenadine.5. The method of independent claim 1 , wherein said Hreceptor antagonist is carebastine.6. The method of independent claim 1 , wherein said Hreceptor antagonist is ebastine.7. The method of independent claim 1 , wherein said Hreceptor antagonist is astemizole.8. The method of wherein said subject is characterized by one or more conditions selected from the group consisting of osteoporosis claim 1 , bone fractures claim 1 , osteolytic lesions claim 1 , metastic bone disease claim 1 , segmental bone defects claim 1 , post-plastic surgery that benefits from bone healing.9. The method of further comprising administering to said subject one or more additional agents that promote tissue growth or infiltration.10. The method of claim 7 , wherein said one or more additional agents is ...

Pharmaceutical Kit for Treating Neuronal Damages

A pharmaceutical kit for treating neuronal damages is disclosed. The pharmaceutical composition of the present invention comprises: a first pharmaceutical composition comprising a first effective amount of a Mg-containing compound; and a second pharmaceutical composition comprising a second effective amount of a COX-2 inhibitor. 19-. (canceled)10. A method for treating neuronal damages , which comprises steps of: (A) administering a first pharmaceutical composition comprising a first effective amount of a Mg-containing compound to a subject in need thereof; and (B) administering a second pharmaceutical composition comprising a second effective amount of a COX-2 inhibitor to the subject.11. The method as claimed in claim 10 , wherein the neuronal damages include brain ischemia claim 10 , stroke claim 10 , spinal cord injury claim 10 , traumatic brain injury claim 10 , or peripheral nerve ischemia.12. The method as claimed in claim 10 , wherein the neuronal damages include ischemic stroke.13. The method as claimed in claim 10 , wherein the Mg-containing compound is MgSO.14. The method as claimed in claim 10 , wherein the COX-2 inhibitor is nimesulide or meloxicam.15. The method as claimed in claim 10 , wherein the COX-2 inhibitor is N-(4-Nitro-2-phenoxyphenyl)methane-sulfonamide claim 10 , or 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1 claim 10 ,2-benzothiazine-3-carboxamide-1 claim 10 ,1-dioxide.16. The method as claimed in claim 10 , wherein the first effective amount is 20-60 mg/Kg.17. The method as claimed in claim 16 , wherein the first effective amount is 40-50 mg/Kg.18. The method as claimed in claim 10 , wherein the second effective amount is 2-12 mg/Kg.19. The method as claimed in claim 18 , wherein the second effective amount is 3-7 mg/Kg.20. The method as claimed in claim 12 , wherein the first pharmaceutical composition is administered followed by the occurrence of ischemic stroke and before thrombolysis.21. The method as claimed in claim 12 , wherein ...

COMBINATION THERAPY FOR THE TREATMENT OF CANCER

Described are methods and compositions for treating cancer that include a dopamine receptor (DR) antagonist such as thioridazine and a chemotherapeutic agent. Optionally, the chemotherapeutic agent is a DNA synthesis inhibitor such as cytarabine or a microtubule inhibitor such as paclitaxel or docetaxel. The methods and compositions are useful for the treatment of cancers such as acute myeloid leukemia. 1. A method of treating acute myeloid leukemia in a subject in need thereof comprising administering to the subject thioridazine and cytarabine.2. The method of claim 1 , wherein thioridazine and cytarabine are administered to the subject at the same time.3. The method of claim 1 , wherein thioridazine and cytarabine are administered to the subject at different times.4. The method of claim 1 , wherein cytarabine is administered to the subject such that the plasma concentration of cytarabine in the subject is between 1 nM and 100 nM.5. The method of claim 4 , wherein cytarabine is administered to the subject such that the plasma concentration of cytarabine in the subject is less than 5 nM.6. The method of claim 1 , wherein thoridazine is administered to the subject such that the plasma concentration of thioridazine in the subject is between 5 μM and 15 μM.7. The method of claim 1 , wherein thioridazine is administered to the subject such that the plasma concentration of thioridazine in the subject is about 10 μM.8. The method of claim 1 , wherein cytarabine is administered to the subject such that the plasma concentration of cytarabine in the subject is between 1 nM and 100 nM and thioridazine is administered to the subject such that the plasma concentration of thioridazine in the subject is between 5 μM and 15 μM.9. The method of claim 8 , wherein thioridazine is administered to the subject such that the plasma concentration of thioridazine in the subject is about 10 μM.10. A method for reducing the proliferation of one or more leukemic cells comprising contacting ...

SOX9 INHIBITORS

Methods for treating a condition associated with proteoglycan production in a mammal are provided. The methods comprise the administration of at least one of a calmodulin antagonist, a transient receptor potential (TRP) channel inhibitor and a calmodulin-binding peptide to the mammal. 1. A method of treating a pathological condition associated with proteoglycan production or modulation in a mammal comprising administering to the mammal an agent selected from the group of a calmodulin antagonist and a transient receptor potential (TRP) channel inhibitor.2. The method as defined in claim 1 , wherein the pathological condition is a condition involving inhibition of neuronal growth or neuronal plasticity.3. The method of claim 2 , wherein the condition is selected from the group consisting of spinal cord injury claim 2 , traumatic brain injury claim 2 , neurodegenerative disease claim 2 , Friedreich's ataxia claim 2 , spinocerebellar ataxia claim 2 , Alzheimer's disease claim 2 , Parkinson's Disease claim 2 , Lou Gehrig's Disease (ALS) claim 2 , demyelinative disease claim 2 , multiple sclerosis claim 2 , transverse myelitis resulting from spinal cord injury claim 2 , inflammation claim 2 , and disease associated with retinal neuronal degeneration.4. The method of claim 1 , wherein the calmodulin antagonist is selected from the group consisting of alpha-adrenergic blockers claim 1 , phenothiazines claim 1 , naphthalenesulfonamides claim 1 , ACE inhibitors claim 1 , alkaloids and pharmaceutically acceptable salts thereof.5. The method of claim 1 , wherein the calmodulin antagonist is selected from the group consisting of phenoxybenzamine claim 1 , Prazosin claim 1 , Terazosin claim 1 , Doxazosin claim 1 , Tamsulosin claim 1 , chlorpromazine claim 1 , calmidazolium claim 1 , E6 Berbamine claim 1 , CGS 9343B claim 1 , trifluoperazine claim 1 , fluphenazine claim 1 , cyclosporine claim 1 , rapamycin claim 1 , FK506 claim 1 , A7 claim 1 , J8 claim 1 , W-5 claim 1 , W-7 claim ...

2-(2-PHENYLETHENYL) 1,3-BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER

The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S0; X, X, X, X, X, Yand Yare each independently selected from H, halogen, alkyl, haloalkyl and OR; and Yand Yare each OR, wherein each Ris independently H, C-Calkyl, acyl, —(CHCH0)wherein n is an integer of 1 to 20, or a functional group that gives rise to hydroxyl upon hydrolysis. 150.-. (canceled)52. A compound according to claim 51 , wherein A is H.53. A compound according to claim 51 , wherein A is CN.54. A compound according to claim 51 , wherein Z is S.55. A compound according to claim 51 , wherein Z is SO.56. A compound according to claim 51 , wherein{'sup': 1', '2', '3', '4', '1', '2, 'at least one of X, X, X, X, Yand Yis a halogen: or'}{'sup': 1', '2', '3', '4, 'X, X, X, and Xare each H or a halogen; or'}{'sup': 3', '4, 'Yand Yare each OH; or'}{'sup': 1', '2, 'Yand Yare each OH.'}57. A compound according to claim 51 , wherein{'sup': 3', '4', '1, 'A is H, Z is S, Yand Yare each OH, and Xis a halogen selected from Br and I; or'}{'sup': 3', '4', '1, 'A is CN, Z is S, Yand Yare each OH, and Xis a halogen selected from Br and I; or'}{'sup': 3', '4', '3, 'A is H, Z is S, Yand Yare each OH, and Xis a halogen selected from Br and I; or'}{'sup': 3', '4', '2, 'A is H, Z is S, Yand Yare each OH, and Xis a halogen selected from Br and I; or'}{'sup': 3', '4', '1', '4, 'A is H, Z is S, Yand Yare each OH, and Xand Xare each a halogen selected from Br and I; or'}{'sub': '2', 'sup': 3', '4', '1, 'A is H, Z is SO, Yand Yare each OH, and Xis a halogen selected from Br and I; or'}{'sub': '2', 'sup': 3', '4', '1', '2', '3', ...

Method for improving the dissolution profile of a biologically active material

A method for improving the dissolution profile of a biologically active material

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis. 3. The method according to claim 1 , wherein X is selected from CH and N.4. The method according to claim 1 , wherein the compound of Formula I is selected from:3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-7-(morpholinomethyl)isoquinolin-1(2H)-one;2-(4-(bis(2-hydroxyethyl)amino)phenyl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(2-chloro-6-methylpyridin-4-yl)-5,7-dimethoxyquinazolin-4(3H)-one;3-(4-Hydroxyphenyl)-2H-isoquinolin-1-one;4-(1-Oxo-1,2-dihydroisoquinolin-3-yl)phenyl 2-amino-5-guanidino-pentanoate trihydrochloride;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2-methylisoquinolin-1(2H)-one;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2,7-dimethylisoquinolin-1(2H)-one;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2-methyl-7-(morpholino-methyl)isoquinolin-1(2H)-one;5,7-dimethoxy-2-(pyridin-2-yl)quinazolin-4(3H)-one;5,7-dimethoxy-2-(pyridin-3-yl)quinazolin-4(3H)-one;5,7-dimethoxy-2-(pyridin-4-yl)quinazolin-4(3H)-one;2-(3,5-dimethyl-4-(2-morpholinoethoxy)phenyl)quinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one;2-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)quinazolin-4(3H)-one;2-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenoxy)acetic acid;2-(4-(dimethylamino)pyridinon-1-yl)quinazolin-4(3H)-one;2-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenoxy)acetamide;2-(4-(dimethylamino)pyridinon-1-yl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(4-(bis(2-hydroxyethyl)amino)phenyl)quinazolin-4(3H)-one;2-(4-hydroxy-3,5-dimethylphenyl)-6,7-dimethoxyquinazolin-4(3H)-one;N-(2-(4-hydroxy-3,5- ...

METHOD FOR TREATING BRAIN TUMOR

The preset invention relates to a new method for treating brain tumor with an antipsychotic phenothiazine derivative as a brain tumor cell inhibitor or a brain tumor stem cell inhibitor. In particular, an antipsychotic phenothiazine is accessible to brain via blood-brain barrier, which should be beneficially in treatment of brain tumor. 1. A method for treating a brain tumor in a subject comprising administering to the subject in need thereof a therapeutically effective amount of an antipsychotic phenothiazine derivative.2. The method of claim 1 , wherein the brain tumor is a primary brain tumor.3. The method of claim 1 , wherein the brain tumor is a metastatic brain tumor.4. The method of claim 1 , wherein tire brain tumor is glioblastoma.5. The method of claim 1 , wherein the antipsychotic phenothiazine derivative is selected from the group consisting of thioridazine claim 1 , acepromazine claim 1 , fluphenazine claim 1 , perphenazine claim 1 , prochlorperazine claim 1 , promazine claim 1 , promethazine claim 1 , trifluoperazine claim 1 , triflupromazine and chlorpromazine.6. The method of claim 5 , wherein the antipsychotic phenothiazine derivative is thioridazine claim 5 , fluphenazine claim 5 , trifluoperazine or prochlorperazine.7. The method of claim 1 , wherein the antipsychotic phenothiazine derivative is thioridazine.8. The method of claim 1 , wherein the antipsychotic phenothiazine derivative is fluphenazine.9. The method of claim 1 , wherein die treatment is achieved by inhibiting the growth of brain claim 1 , cancer cells and/or brain cancer stem cells.10. A method claim 1 , for inhibiting the growth claim 1 , of brain cancer stem cells in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an antipsychotic phenothiazine derivative.11. The method of claim 10 , wherein the brain cancer is glioblastoma.12. The method of claim 10 , wherein the antipsychotic phenothiazine derivative is selected from the ...

COMPOSITIONS AND METHODS FOR TREATMENT OF FILOVIRUS-MEDIATED DISEASES

The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal. 1. A method for treating a patient having a filovirus-mediated disease , said method comprising administering to said patient an agent selected from the agents listed in Table 1 in an amount that is effective to treat said patient.2. The method of claim 1 , wherein said filovirus is Ebola virus or Marburg virus.3. The method of claim 1 , said method further comprising administering a second agent selected from the agents listed in Table 1.4. The method of claim 3 , wherein the first agent is aripiprazole.5. The method of claim 4 , wherein the second agent is piperacetazine.6. The method of claim 3 , wherein said agents are administered within twenty-four hours of each other.7. The method of claim 3 , wherein said agents are administered within 1 hour of each other or substantially simultaneously.8. The method of claim 1 , wherein said agent is administered orally claim 1 , parenterally claim 1 , systemically claim 1 , topically claim 1 , or inhalationally.98. The method of any of - claims 6 , wherein said first agent is aripiprazole and said second agent is piperacetazine.10. A composition comprising two or more agents selected from the group consisting of the agents of Table 1.11. The composition of claim 10 , wherein said two or more agents are present in amounts that claim 10 , when administered together to a patient with a filovirus-mediated disease claim 10 , are effective to treat said patient.12. The composition of claim 11 , wherein said filovirus is Ebola virus or Marburg virus.13. The composition of claim 10 , wherein said two or more agents are aripiprazole and piperacetazine.14. A kit comprising:(a) an active agent selected from Table 1 or an analog thereof; and(b) instructions for administering said agent to a patient having a filovirus-mediated disease.15. The kit of claim 14 , ...

QUINOLINE DERIVATIVES AND USES THEREOF

This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQand CQmalaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQreversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQor CQsp. (such as ). 2. The compound of claim 1 , wherein Yis N.3. The compound of claim 1 , wherein Lis from 2 to 6 atoms in length.4. The compound of claim 1 , wherein m is 1 or 2 claim 1 , n is 0 or 1 claim 1 , and each Xand Xindependently is H claim 1 , chloro claim 1 , fluoro claim 1 , or trifluoromethyl.5. The compound of claim 1 , wherein each Xindependently is H claim 1 , chloro claim 1 , or trifluoromethyl claim 1 , and n is 0.6. The compound of claim 5 , wherein m is 1 and (X)is chloro at position C.7. The compound of claim 1 , wherein Rand Rare independently H claim 1 , alkyl having from 1 to 4 carbon atoms claim 1 , or heteroalkyl having from 1 to 4 carbon atoms.8. The compound of claim 7 , wherein Rand Rare independently H claim 7 , methyl claim 7 , trifluoromethyl claim 7 , —CHCHCF claim 7 , —CHCF claim 7 , —CHCHNH claim 7 , —CHNH claim 7 , —CHCHC(O)NH claim 7 , or —CHC(O)NH.9. The compound of claim 1 , wherein Land Lare independently from 1 to 12 atoms in length claim 1 , and each position of Land Lis independently methylene claim 1 , difluoromethylene claim 1 , dichloromethylene claim 1 , di(methylamino) claim 1 , —NH— claim 1 , or —O—.10. The compound of claim 1 , wherein:{'sub': 1', 'm', '7, 'm is 1 and (X)is chloro at position C;'}n is 0;{'sub': 1', '2', '2', '2', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Rand Rare independently H, methyl, trifluoromethyl, —CHCHCF, —CHCF, —CHCHNH, —CHNH, —CHCHC(O)NH, or —CHC(O)NH ...

Compositions and methods for inhibition of the jak pathway

Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Pharmaceutical composition comprising (1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano-[3,4,b]indol]-4-amine and an oxicam

The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient, which is selected from (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient, which is an oxicam selected from the group consisting of meloxicam, piroxicam, tenoxicam, lornoxicam, droxicam and the physiologically acceptable salts thereof. 1. A pharmaceutical composition comprising:a) a first pharmacologically active ingredient, which is selected from (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, andb) a second pharmacologically active ingredient, which is an oxicam selected from the group consisting of meloxicam, piroxicam, tenoxicam, lornoxicam, droxicam and the physiologically acceptable salts thereof.2. The pharmaceutical composition according to claim 1 , wherein the first pharmacologically active ingredient is (1r claim 1 ,4r)-6′-fluoro-N claim 1 ,N-dimethyl-4-phenyl-4′ claim 1 ,9′-dihydro-3′H-spiro[cyclohexane-1 claim 1 ,1′-pyrano[3 claim 1 ,4 claim 1 ,b]indol]-4-amine.3. The pharmaceutical composition according to claim 1 , wherein the second pharmacologically active ingredient is an oxicam selected from the group consisting of meloxicam claim 1 , piroxicam claim 1 , tenoxicam claim 1 , lornoxicam and the physiologically acceptable salts thereof.4. The pharmaceutical composition according to claim 1 , which contains the first and the second pharmacologically active ingredient in such a weight ratio that they will exert a synergistic therapeutic effect upon administration to a patient.5. The pharmaceutical composition according to claim 1 , wherein the relative weight ratio of the first pharmacologically active ingredient to the second pharmacologically active ingredient is within the range ...

PHARMACEUTICAL TRANSDERMAL COMPOSITIONS AND METHOD FOR TREATING INFLAMMATION IN CATTLE

Novel transdermal preparations combining a non-steroidal anti-inflammatory drug (NSAID) selected from groups such as oxicams (for example, meloxicam), propionic acids (for example, ketoprofen) and anthranilic acids (for example, tolfenamic acid), are disclosed. Methods for using and administering such preparation in the treatment of inflammatory conditions in bovines are also disclosed. 124-. (canceled)25. A method for providing a systemic anti-inflammatory activity in a bovine animal , comprising administering an effective amount of a composition to the skin of the animal wherein the composition comprisesa) a non-steroidal anti-inflammatory compound selected from the following groups: oxicams, propionic acids and anthranilic acids, or pharmacologically acceptable salts thereof;b) at least one solvent selected from a pyrrolidone solvent, ethyl lactate, glycol ethers, ethanol, isopropyl alcohol; and benzyl alcohol; andc) at least one dermal penetration enhancer selected from menthol, xylene, D-limonene, isopropyl myrstiate, propylene glycol dicaprylate/dicaprate decanoic acid, decyl alcohol and oleic acid.26. The method of claim 25 , wherein the systemic bioavailability of the non-steroidal anti-inflammatory compound is at least 10%.27. The method of claim 25 , wherein the composition comprises at least 0.5% by wt of the non-steroidal anti-inflammatory compound.28. The method of claim 25 , wherein the non-steroidal anti-inflammatory compound is meloxicam or a pharmacologically acceptable salt thereof.29. The method of claim 25 , wherein the non-steroidal anti-inflammatory compound is ketoprofen or a pharmacologically acceptable salt thereof.30. The method of claim 25 , wherein the non-steroidal anti-inflammatory compound is tolfenamic acid or a pharmacologically acceptable salt thereof.31. The method of claim 25 , wherein the penetration enhancer is a mixture of propylene glycol dicaprylate/dicaprate and menthol.32. The method of claim 25 , wherein the solvent is a ...

Inclusion complexes containing piroxicam, a cyclodextrin and arginine

The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, using the following successive stages: (a) bringing one or several active substances into contact with one or several host molecules; (b) initiating a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in (a) in a static mode in the presence of one or several diffusing agents; (c) recovering the active substance-host molecule molecular complex formed; (d) adding and mixing an interaction agent with the active substance-host molecule molecular complex; (e) recovering the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound obtained by the method, particularly a piroxicam-cyclodextrin-arginine compound.

Treatment of Cancer WIth Dopamine Receptor Antagonists

Described are methods of treating a cancer comprising administering to a subject in need thereof an effective amount of a dopamine receptor (DR) antagonist. The DR antagonist may be a phenothiazine derivative, such as thioridazine or chlorpromazine. Optionally, the cancer is acute myeloid leukemia. Also described are methods for identifying subjects with cancer, methods for providing a prognosis for a subjects with cancer and/or subjects likely to be responsive to therapy with DR receptor antagonists. Methods for identifying cancer stem cells and chemotherapeutic compounds that are DR receptor antagonists as also provided. 1. A method of treating acute myeloid leukemia (AML) in a subject comprising administering to the subject a dopamine receptor antagonist.2. The method of claim 1 , wherein the dopamine receptor antagonist is a Dfamily dopamine receptor antagonist.3. The method of claim 2 , wherein the dopamine receptor antagonist is a phenothiazine derivative or a compound listed in Table 1.4. The method of claim 3 , wherein the phenothiazine derivative is thioridazine.5. The method of claim 1 , wherein the acute myeloid leukemia comprises cells that express one or more dopamine receptors (DR) selected from DR1 claim 1 , DR2 claim 1 , DR3 claim 1 , DR4 and DR5.6. The method of claim 5 , wherein the cells that express one or more dopamine receptors also express CD14.7. The method of claim 1 , wherein the dopamine receptor antagonist preferentially induces the differentiation of cancer stem cells relative to hematopoietic or normal stem cells.8. The method of claim 1 , wherein the subject is in remission.9. A method for reducing the proliferation of a cancer cell comprising contacting the cancer cell with a dopamine receptor antagonist.10. The method of claim 9 , wherein the cancer cell is a cancer stem cell and contacting the cancer stem cell with the dopamine receptor antagonist induces differentiation of the cancer stem cell.11. The method of claim 9 , wherein ...

TOPICAL FORMULATIONS, SYSTEMS AND METHODS

The present disclosure is drawn to topical formulations, transdermal systems, and related methods. In one embodiment, a topical formulation is provided that includes a local anesthetic, a first compound, and a second compound. The first compound and second compound are different and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate. 2. The topical formulation of claim 1 , wherein the local anesthetic is selected from the group consisting of lidocaine claim 1 , tetracaine claim 1 , benzocaine claim 1 , prilocaine claim 1 , bupivacaine claim 1 , dimethocaine claim 1 , mepivacaine claim 1 , procaine claim 1 , ropivacaine claim 1 , trimecaine claim 1 , articaine claim 1 , and combinations thereof.3. The topical formulation of claim 1 , wherein the topical formulation includes lidocaine claim 1 , tetracaine claim 1 , or a combination thereof.4. The topical formulation of claim 1 , wherein the topical formulation includes a eutectic mixture of lidocaine and tetracaine.5. The topical formulation of claim 1 , wherein the local anesthetic is at least one local anesthetic base.6. The topical formulation of claim 1 , wherein the local anesthetic comprises at least about 30 wt % of the topical formulation.7. The topical formulation of claim 1 , wherein the local anesthetic comprises at least about 35 wt % of the topical formulation.8. The topical formulation of claim 1 , wherein the topical formulation further comprises water.9. The topical formulation of claim 8 , wherein the topical formulation has less phase separation after four weeks stored at 25° C. compared to a comparative formulation devoid of the first compound and the second compound and replaced with an equivalent wt % of water.10. The topical formulation of claim 8 , wherein the topical formulation has less phase separation after two weeks when stored at about 40° C. compared to a ...

COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING PHENYLKETONURIA (PKU)

A method of diagnosing Phenylketonuria (PKU) in a subject in need thereof is disclosed. The method comprises detecting phenylalanine fibrils in a tissue of the subject, wherein a presence or level above a predetermined threshold of said phenylalanine fibrils in said tissue, is indicative of PKU in the subject. Antibodies capable of detecting phenylalanine fibrils are also disclosed as well as additional uses. 1. A method of diagnosing Phenylketonuria (PKU) in a subject in need thereof , the method comprising detecting phenylalanine fibrils in a tissue of the subject , wherein a presence or level above a predetermined threshold of said phenylalanine fibrils in said tissue , is indicative of PKU in the subject.2. The method of claim 1 , wherein said detecting is effected using an isolated antibody which specifically binds to fibrils consisting of phenylalanine.3. The method of claim 1 , wherein said detecting is effected with a dye.4. The method of claim 3 , wherein said dye is selected from the group consisting of Congo red and ThT.5. An isolated antibody which specifically binds to fibrils consisting of phenylalanine.6. The isolated antibody of claim 5 , attached to an identifiable moiety.7. The isolated antibody of claim 5 , being a polyclonal antibody.8. The isolated antibody of claim 5 , being a monoclonal antibody.9. A pharmaceutical composition comprising as an active ingredient the isolated antibody of .10. A method of detecting phenylalanine fibrils in a biological sample claim 5 , the method comprising contacting the biological sample with the antibody of under conditions which allow formation of immunocomplexes claim 5 , wherein a presence of immunocomplexes above a predetermined threshold is indicative of phenylalanine fibrils in the biological sample.11. A method of treating PKU in a subject in need thereof claim 5 , the method comprising administering to the subject a therapeutic effective amount of an anti-amyloid agent claim 5 , thereby treating the ...

Drug delivery device

The invention provides an implantable intracranial device for the site-specific delivery of a pharmaceutically active agent to a human or animal for treating a mental or neurological disorder, such as Alzheimer's disease, schizophrenia or other psychoses. The biodegradable device includes a pharmaceutically active agent for treating the disorder, polymeric nano-lipoparticles into or onto which the pharmaceutically active agent is embedded; and a polymeric matrix or scaffold incorporating the nano-lipoparticles. The nano-lipoparticles can be in the form of nano-liposhells or nano-lipobubbles. The nano-liposhells or nano-lipobubbles can include an essential fatty acid or can be conjugated to a peptide ligand which targets the device to a specific cell into which the therapeutic agent can be delivered. The device can be implanted in the sub-arachnoid space in the region of the frontal lobe of the brain.

BRANCHED OXATHIAZINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, USE THEREOF AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND USE THEREOF

The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia. 2. The compound of claim 1 , wherein{'sub': '2', 'A is CH;'}{'sub': 1', '6', '3', '8, 'D is (C-C)-alkylene, (C-C)-cycloalkylene;'}{'sub': 2', 'n', '2', 'n, 'claim-text': {'sub': 3', '2', '2', '2', '3', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '2', '3', '2', '2', '2', '1', '6', '2', '1', '6', '2', '1', '6', '2', '1', '6', '1', '6', '2', '5, 'where the phenyl radical or pyridinyl radical may be mono- to trisubstituted by F, Cl, Br, I, OH, CF, CHF, CHF, NO, CN, OCF, OCHF, O—(C-C)-alkyl, (C-C)-alkyl, NH, NH(C-C)-alkyl, N((C-C)-alkyl), SO—CH, SO—NH, SO—NH(C-C)-alkyl, SO—N((C-C)-alkyl), COOH, COO—(C-C)-alkyl, CONH, CONH(C-C)-alkyl, CON((C-C)-alkyl), SF;'}, 'R1 is —(CH)-phenyl, —(CH)-pyridinyl,'}n is 0, 1, 2;{'sub': 1', '6, 'R2, R3 are each independently H, (C-C)-alkyl;'}{'sub': 2', '2', '2, 'R6 is OH, O—(CO)—NH, SONH;'}and pharmaceutically acceptable salts thereof.3. The compound of claim 1 , wherein{'sub': '2', 'A is CH;'}{'sub': 1', '6, 'D is (C-C)-alkylene;'} {'sub': 3', '2', '2', '2', '3', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '2', '3', '2', '2', '2', '1', '6', '2', '1', '6', '2', '1', '6', '2', '1', '6', '1', '6', '2', '5, 'where the phenyl radical or pyridinyl radical may be mono- to trisubstituted by F, Cl, Br, I, OH, CF, CHF, CHF, NO, CN, OCF, OCHF, O—(C-C)-alkyl, (C-C)-alkyl, NH, NH(C-C)-alkyl, N((C-C)-alkyl), SO—CH, SO—NH, SO—NH(C-C)-alkyl, SO—N((C-C)-alkyl); COOH, COO—(C-C)-alkyl, CONH, CONH(C-C)-alkyl, CON((C-C)-alkyl), SF;'}, 'R1 is phenyl, pyridine'}{'sub': 1', '6, 'R2, R3 are each independently H, (C-C)-alkyl;'}R6 is OH;and pharmaceutically acceptable salts thereof.4. The compound of claim 1 , wherein{'sub': '2', 'A is CH;'}{'sub': 1', '2, 'D is (C-C)-alkylene;'} {'sub': 3', '2', '2', '2', '3', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '2', '3 ...

OXATHIAZINE DERIVATIVES SUBSTITUTED WITH CARBOCYCLES OR HETEROCYCLES, METHOD FOR PRODUCING SAME, DRUGS CONTAINING SAID COMPOUNDS, AND USE THEREOF

The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia. 4. (canceled)5. A pharmaceutical composition comprising the compound of claim 1 , or pharmaceutically acceptable salts thereof claim 1 , and a pharmaceutically acceptable carrier and/or excipient.6. The pharmaceutical composition of claim 5 , further comprising at least one further active ingredient.7. The pharmaceutical composition of claim 6 , wherein said active ingredient is one or more antidiabetics claim 6 , active hypoglycemic ingredients claim 6 , HMG-CoA reductase inhibitors claim 6 , cholesterol absorption inhibitors claim 6 , PPAR gamma agonists claim 6 , PPAR alpha agonists claim 6 , PPAR alpha/gamma agonists claim 6 , PPAR delta agonists claim 6 , fibrates claim 6 , MTP inhibitors claim 6 , bile acid absorption inhibitors claim 6 , CETP inhibitors claim 6 , polymeric bile acid adsorbers claim 6 , LDL receptor inducers claim 6 , ACAT inhibitors claim 6 , antioxidants claim 6 , lipoprotein lipase inhibitors claim 6 , ATP citrate lyase inhibitors claim 6 , squalene synthetase inhibitors claim 6 , lipoprotein(a) antagonists claim 6 , HM74A receptor agonists claim 6 , lipase inhibitors claim 6 , insulins claim 6 , sulfonylureas claim 6 , biguanides claim 6 , meglitinides claim 6 , thiazolidinediones claim 6 , α-glucosidase inhibitors claim 6 , active ingredients which act on the ATP-dependent potassium channel of the beta cells claim 6 , glycogen phosphorylase inhibitors claim 6 , glucagon receptor antagonists claim 6 , activators of glucokinase claim 6 , inhibitors of gluconeogenesis claim 6 , inhibitors of fructose 1 claim 6 ,6-biphosphatase claim 6 , modulators of glucose transporter 4 claim 6 , inhibitors of glutamine-fructose-6-phosphate amidotransferase claim 6 , inhibitors of dipeptidylpeptidase IV claim 6 , inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 claim 6 , inhibitors of protein ...

Compositions and Methods for the Treatment of Catatonia

Compositions and methods for treating psychotic and neurological disorders in a subject are disclosed. The compositions and methods utilize a pharmaceutical compound that reverses or negates the effects of an NMDA receptor antagonist. The compositions and methods are effective in reducing at least catatonic features in the subject.

ORAL PHARMACEUTICAL DISPERSION COMPOSITIONS

The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic. 1. An oral pharmaceutical composition , optionally in dose unit form , comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier , preferably an aqueous gel , wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10 , characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value , said pH being below said pKa where said group is acidic and above said pKa where said group is basic.2. A composition as claimed in wherein said carrier is an aqueous gel.3. A composition as claimed in either of and wherein said drug substance is an NSAID.4. A composition as claimed in wherein said drug substance is ibuprofen.5. A composition as claimed in wherein the pH of said carrier is in the range 4 to 4.5.6. An oral pharmaceutical composition comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion claim 4 , wherein said drug substance is a hydrophilic drug dispersed in the lipid phase or a lipophilic drug substance dispersed in a claim 4 , preferably continuous claim 4 , aqueous phase of the emulsion.7. A pharmaceutical composition claim 4 , comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion claim 4 , wherein said drug substance is a hydrophilic drug dispersed in an oil phase and/or a lipophilic drug dispersed in a claim 4 , preferably continuous claim 4 , aqueous ...

Materials and methods for treating radiation poisoning

Disclosed herein are materials and methods for treating patients that have been exposed to pathological levels on ionizing radiation. These materials and methods include administering to a patient in thereof at least one dose of a compound such as prostaglandin (PGE 2 ) as soon as possible after the patient has been exposed to the radiation. Additional embodiments include treating a patient exposed to radiation with at least one dose of a compound that modulates PGE 2 activity such as non-steroidal anti-inflammatory compound. Some methods include a first step of administering PGE 2 or another compound that binds as soon as possible after exposure to radiation followed by a delayed dosing with at least one compound such as meloxicam that interferes with PGE 2 activity.

PHARMACEUTICAL COMPOSITIONS

Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic. 1138-. (canceled)139. A solid composition comprising: i. one or more opioid analgesics, and', 'ii. one or more antiemetics; and, 'a. an effective amount ofb. a pharmaceutically acceptable carrier or vehicle.140. The solid composition of claim 139 , wherein:the one or more opioid analgesics is hydrocodone, oxycodone, morphine, diamorphine, codeine, pethidine, alfentanil, buprenorphine, butorphanol, dezocine, fentanyl, hydromorphone, levomethadyl acetate, levorphanol, meperidine, methadone, morphine sulfate, nalbuphine, oxycodone, oxymorphone, pentazocine, propoxyphene, remifentanil, sufentanil, tramadol, or a pharmaceutically acceptable salt of each of the foregoing.141. The solid composition of claim 139 , wherein:the one or more antiemetics is aprepitant, dronabinol, perphenazine, palonosetron, trimethyobenzamide, metoclopromide, domperidone, prochlorperazine, promethazine, chlorpromazine, trimethobenzamide, ondansetron, granisetron, hydroxyzine, acetylleucine monoethanolamine, alizapride, azasetron, benzquinamide, bietanautine, bromopride, buclizine, clebopride, cyclizine, dimenhydrinate, diphenidol, dolasetron, meclizine, methallatal, metopimazine, nabilone, oxyperndyl, pipamazine, scopolamine, sulpiride, tetrahydrocannabinol, thiethylperazine, thioproperazine, tropisetron, droperidol, haloperidol, prochloperazine, metoclopramide, diphenhydramine, cannabis, midazolam, lorazepam, hyoscine, dexamethasone, emetrol, propofol, or a pharmaceutically acceptable salt of each of the forgoing.142. The solid composition of claim 139 , wherein the one or more antiemetics comprise promethazine or a pharmaceutically acceptable salt thereof.143. The solid composition of claim 139 , wherein the one or more opioid analgesics comprise hydrocodone or a pharmaceutically acceptable salt thereof or ...

5,6-dihydro-1h-pyridin-2-one compounds

The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR 3 , and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

DRUG THERAPY TO INHIBIT CHEMOTHERAPY-INDUCED ADVERSE EFFECTS AND RELATED PHARMACEUTICAL COMPOSITIONS, DIAGNOSTICS, SCREENING TECHNIQUES AND KITS

The invention provides a method of treatment comprising reducing therapy-induced adverse effects (TIAE), including chemotherapy-induced adverse effects (CIAE), such as chemotherapy-induced peripheral neuropathy (CIPN) and/or chemotherapy-induced cardiovascular adverse effects (CICAE) in a subject being treated with a CIAE-inducing anti-cancer active ingredient by co-administering to the subject a pharmaceutically effective amount of a NCS-1-protective composition. Related pharmaceutical compositions, diagnostics and screening techniques are also provided. 1. A method of treatment comprising inhibiting or preventing the onset of or ameliorating one or more the symptoms of chemotherapy-induced adverse effects peripheral neuropathy (CIPNCIAE) in a subject being treated with a CIPNCIAE-inducing anti-cancer active ingredient by co-administering to the subject a pharmaceutically effective amount of a NCS-1-protective composition , wherein said chemotherapy induced adverse effects include calcium signaling disregulation , neuropathy , peripheral neuropathy , cardiac arrhythmia , cardiac dysfunction , increased and/or decreased cardiovascular calcium signaling and increased spontaneous calcium oscillations , central nervous system effects of reduced cognition/cognitive impairment and adverse effects caused by myelin degradation.2. The method of claim 1 , wherein the CIPNCIAE-inducing anti-cancer active ingredient is selected from the group consisting of a taxane claim 1 , a platinum compound claim 1 , a vinca alkaloid claim 1 , a radiation sensitizing agent or a mixture thereof thalidomide claim 1 , bortezornib (Velcade®) and carfilzomib and the NCS-1-protective composition is selected from the group consisting of AV411 (ibudilast) claim 1 , an AV411(ibudilast) analog claim 1 , a PDE4 inhibitor claim 1 , OCR5638 claim 1 , lithium claim 1 , valproric acid claim 1 , calpastatin claim 1 , chlorpromazine claim 1 , and a calpain inhibitor. and mixtures thereof.3. The method of ...

DIRECTED DIFFERENTIATION OF OLIGODENDROCYTE PRECURSOR CELLS TO A MYELINATING CELL FATE

The present invention provides methods of inducing differentiation of oligodendrocyte progenitor cells to a mature myelinating cell fate with a neurotransmitter receptor modulating agent. The present invention also provides methods of stimulating increased myelination in a subject in need thereof by administering said neurotransmitter receptor modulating agent. Methods of treating a subject having a demyelinating disease using a neurotransmitter receptor modulating agent are also provided. 1. A method of stimulating increased myelination of nerves in a human subject having a demyelinating disease , the method comprising:administering to the subject a therapeutically effective dose of a neurotransmitter receptor modulating agent selected from a muscarinic receptor antagonist, a dopamine receptor antagonist, a histamine receptor antagonist, a beta adrenergic receptor modulator, and an opioid receptor modulator; thereby stimulating increased myelination of nerves in the subject.2. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a muscarinic receptor antagonist.3. (canceled)4. The method of claim 2 , wherein the muscarinic receptor antagonist is selected from benztropine claim 2 , carbetapentane claim 2 , clemastine claim 2 , ipratropium claim 2 , atropine claim 2 , and salts thereof.5. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a dopamine receptor antagonist.6. (canceled)7. The method of claim 5 , wherein the dopamine receptor antagonist is selected from benztropine claim 5 , GBR12935 claim 5 , trifluoperazine claim 5 , and salts thereof.8. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a histamine receptor antagonist.9. (canceled)10. The method of claim 8 , wherein the histamine receptor antagonist is clemastine or a salt thereof.11. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a beta adrenergic receptor antagonist.12. ( ...

PIROXICAM-CONTAINING MATRIX PATCHES AND METHODS FOR THE TOPICAL TREATMENT OF ACUTE AND CHRONIC PAIN AND INFLAMMATION THEREWITH

This invention relates to matrix patches for the topical (i.e., transdermal) delivery of piroxicam and methods for the treatment of acute and chronic pain and inflammation therewith, particularly pain and inflammation caused by sports injuries or other muscle aches or injuries requiring the application of analgesic and/or anti-inflammation medication, in this instance, piroxicam. 190-. (canceled)91. A method of treating a condition associated with acute and chronic pain and/or inflammation , wherein said method comprises applying a matrix patch for topical administration of piroxicam to a subject ,wherein said matrix patch consists of a removable covering layer, a compatible backing layer, and a piroxicam-containing self-adhesive matrix layer in between wherein the self-adhesive matrix layer includes a pharmaceutically effective amount of piroxicam in an acrylic copolymer self-adhesive base, wherein said base further includes petrolatum, polyvinylpyrrolidone, and either dimethyl isosorbide and/or a monoalkyl ether of diethylene glycol.92. The method according to claim 91 , wherein said condition is selected from the group consisting of rheumatoid arthritis claim 91 , osteoarthritis claim 91 , inflammatory arthropathies claim 91 , gout and pseudogout claim 91 , dysmenorrhea claim 91 , metastatic bone pain claim 91 , headache and migraine claim 91 , postoperative pain claim 91 , post-herpetic neuralgia claim 91 , neuropathic pains claim 91 , sports injuries claim 91 , soft-tissue injuries claim 91 , strains claim 91 , sprains claim 91 , contusions claim 91 , tendonitis or bursitis of the shoulder claim 91 , elbow claim 91 , wrist or knee claim 91 , Carpal tunnel syndrome claim 91 , lateral epicondylosis claim 91 , low back pains and injury.93. A method of treating a condition associated with acute and chronic pain and/or inflammation claim 91 , wherein said method comprises applying a matrix patch for topical administration of piroxicam to a subject claim 91 ,wherein ...

Antiviral compounds

The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Modulators of atp-binding cassette transporters

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

DOPAMINE RECEPTOR D2 ANTAGONIST FOR PREVENTION AND TREATMENT OF FLAVIVIRUS INFECTION

Methods for preventing and/or treating flavivirus infection are disclosed. The method comprises administering to a subject in need thereof a composition comprising: a) a dopamine D2 receptor antagonist in an amount effective for preventing and/or treating flavivirus infection; and b) a pharmaceutically acceptable carrier. The dopamine D2 receptor antagonist may be selected from the group consisting of prochlorperazine or a salt thereof, and haloperidol. 1. A method of preventing and/or treating flavivirus infection , comprising:administering to a subject in need thereof a composition comprising:a) a dopamine D2 receptor antagonist in an amount effective for preventing and/or treating flavivirus infection; andb) a pharmaceutically acceptable carrier;wherein the dopamine D2 receptor antagonist exhibits an antiviral activity in inhibiting dengue virus replication and/or inhibiting nonstructural protein 3 (NS 3) production in a host cell.2. The method of claim 1 , wherein the dopamine D2 receptor antagonist is at least one selected from the group consisting of prochlorperazine or a salt thereof claim 1 , and haloperidol.3. The method of claim 1 , wherein the flavivirus is selected from the group consisting of a dengue virus claim 1 , an encephalitis virus claim 1 , and a West Nile virus.4. The method of claim 3 , wherein the encephalitis virus is a Japanese encephalitis virus.5. The method of claim 3 , wherein the dengue virus is serotype 2 or serotype 1.6. The method of claim 1 , wherein the salt of prochlorperazine is selected from the group consisting of prochlorperazine maleate and prochlorperazine dimethanesulfonate.7. The method of claim 1 , wherein the subject is a high-risk human or a patient with fever before dengue diagnosis in epidemic areas during dengue outbreaks.8. The method of claim 1 , wherein the subject is a patient with dengue fever.9. The method of claim 1 , wherein the amount of prochlorperazine claim 1 , or a salt thereof claim 1 , is effective in ...

Osteoclast activity

Described are medicaments and methods of treating or preventing metabolic bone diseases, such as Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppress critical illness enhanced osteoclastogenesis or increased osteoclast differentiation. The methods include administering of an autophagy activating compound to a mammal to: treat or prevent a bone degenerative disorder; slow bone deterioration; restore lost bone; maintain bone mass and/or bone quality or inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. Also described are methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and/or enhanced activation of osteoclasts.

Highly Concentrated Stable Meloxicam Solutions for Needleless Injection

A method for treating pain, inflammation, fever and respiratory complaints in mammals comprising administering by needleless injection to a mammal in need of such treatment an aqueous cyclodextrin-free solution of meloxicam containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base. 1. A method for treating pain , inflammation , fever and respiratory complaints in mammals comprising administering by needleless injection to a mammal in need of such treatment a composition comprising:40 to 80 mg/ml meloxicam;a pharmacologically acceptable organic or inorganic base capable of forming a salt with the meloxicam and selected from the group consisting of meglumine, sodium, potassium and ammonium; anddisodium EDTA;wherein the solution is free of cyclodextrin.2. The method of claim 1 , wherein the administration of the composition is to a large farm animal in need of such treatment.3. The method of claim 1 , wherein the administration of the composition is to a mammal that is at least 50 kg and up to 750 kg.4. The method of claim 3 , wherein the solution is administered in a dosage range of from 0.2 to 1.0 mg of meloxicam/kg of bodyweight of the mammal.5. The method of claim 3 , wherein the mammal is suffering from at least one of acute mastitis claim 3 , diarrhea claim 3 , lameness claim 3 , and oncological indications.6. The method of claim 1 , wherein the solution has a pH of between 8.5 and 9.7. The method of claim 1 , wherein the solution comprises disodium EDTA in an amount such that the weight ratio of meloxicam to disodium EDTA is between 100:1 and 35:1.8. The method of claim 1 , wherein the solution further comprises:a polyethylene glycol;a polyoxyethylene-polypropylene copolymer; andethanol;wherein the solution is free of cyclodextrin, the solution has a pH of between 8.5 and 9, and the solution has a shelf-life after opening of 28 days or more.9. The method according to claim 1 , wherein the pharmacologically acceptable organic or ...

TETRAZOLONES AS INHIBITORS OF FATTY ACID SYNTHASE

Provided herein are tetrazolone FASN inhibitors of the formula (I): 2. The method of claim 1 , wherein L is a covalent bond.3. The method of claim 1 , wherein L is a divalent Chydrocarbon chain claim 1 , wherein one methylene unit of L is optionally and independently replaced with a divalent carbocyclyl claim 1 , divalent heterocyclyl claim 1 , divalent aryl or divalent heteroaryl group.4. The method of claim 1 , wherein Ris selected from —CN claim 1 , —NO claim 1 , —SOH claim 1 , —SOH claim 1 , —C(═O)R claim 1 , —COH claim 1 , —CHO claim 1 , —COR claim 1 , —C(═O)N(R) claim 1 , —C(═NR)OR claim 1 , —C(═NR)N(R) claim 1 , —C(═O)NRSOR claim 1 , —SON(R) claim 1 , —SOR claim 1 , —SOOR claim 1 , —S(═O)R claim 1 , —C(═S)N(R) claim 1 , —C(═O)SR claim 1 , —C(═S)SR claim 1 , —P(═O)R claim 1 , —P(═O)(R) claim 1 , —P(═O)N(R) claim 1 , —P(═O)(NR) claim 1 , —B(OR) claim 1 , —BR(OR) and tetrazolyl.5. The method of claim 4 , wherein Ris selected from —C(═O)R claim 4 , —COH claim 4 , —CHO claim 4 , —COR claim 4 , —C(═O)N(R) claim 4 , —C(═NR)OR claim 4 , —C(═NR)N(R) claim 4 , —C(═O)NRSOR claim 4 , —C(═S)N(R) claim 4 , —C(═O)SRand —C(═S)SR.6. The method of claim 5 , wherein Ris selected from —C(═O)R claim 5 , —COH claim 5 , —CHO claim 5 , and —COR.7. The method of claim 6 , wherein Ris —COH.8. The method of claim 1 , wherein Ris further substituted with the group:{'br': None, 'sup': 'E', '—R'}wherein:{'sup': E', 'B10', 'B11', 'B11', 'B12', 'B12', 'B10', 'B12', 'B10', 'B10', 'B11', 'B11', 'B10', 'B11', 'B10', 'B11', 'B11', 'B11', 'B10', 'B11', 'B10', 'B11', 'B11', 'B11', 'B11', 'B11', 'B11', 'B10', 'B10', 'B101', 'B10', 'B10', 'B10', 'B10', 'B10', 'B12', 'B11', 'B11', 'B11', 'B12', 'B11', 'B11', 'B12', 'B12', 'B12', 'B12, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '3, 'Ris selected from halogen, —OH, —OR, —ON(R), —N(R), —N(OR)R, —SH, —SR, —SSR, —OC(═O)R, —OCOR, —OC(═O)N(R), —NRC(═O)R, —-—NRCOR, —NRC(═O)N(R), — ...

PHARMACEUTICAL PREPARATIONS CONTAINING HIGHLY VOLATILE SILICONES

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions. 1. A transdermal preparation containing a pharmaceutically active ingredient , wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof , and these coated particles are dispersed in a gel or cream base.2. A composition according to claim 1 , characterized in that the active ingredient is acyclovir claim 1 , piroxicam claim 1 , meloxicam claim 1 , ibuprofen claim 1 , diclofenac sodium or diclofenac potassium claim 1 , clotrimazole claim 1 , bifonazole claim 1 , metronidazole claim 1 , nifedipine claim 1 , glycerol trinitrate or cetirizine.3. A composition according to claim 1 , characterized in that the volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclosiloxane.4. A composition according to claim 1 , characterized in that the cream base is carboxyvinyl polymer claim 1 , hydroxypropyl-methylcellulose or mixtures thereof.5. A process for the preparation of the composition according to claim 1 , characterized in that the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof and the obtained mixture is distributed in a gel or cream base claim 1 , thus the particles in the gel or cream base are surrounded with silicone coating. This application claims priority to U.S. patent application Ser. No. 12/672,696, filed Apr. 9, 2010, which claims priority to PCT Application, PCT/HU2008/000083, filed Jul. 10, 2008 ...

NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS

Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R, R, R, R, R, R, R, R, R, R, and Rare defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. 5. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , prodrug or salt thereof claim 1 , of claim 1 , wherein A is a 5- to 6-membered aryl.6. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , prodrug or salt thereof claim 1 , of claim 1 , wherein A is a 5- to 6-membered heteroaryl claim 1 , wherein the heteroaryl contains 1-4 heteroatoms selected from N claim 1 , O claim 1 , and S.12. A pharmaceutical composition comprised of a therapeutically effective amount of at least one compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , prodrug or salt thereof claim 1 , of claim 1 , and a pharmaceutically acceptable carrier.13. The pharmaceutical composition of claim 12 , further comprising a therapeutically effective amount of one or more other therapeutically active agents.14. A method of modulating the activity of the TGR5 receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , prodrug or salt thereof claim 1 , of claim 1 , and optionally an additional therapeutic agent.15. A method for preventing claim 1 , inhibiting ...

Methods and Compositions for the Treatment of Estrogen-Dependent Hyperproliferative Uterine Disorders

The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects. 1. A method for treating a subject for an estrogen-dependent hyperproliferative uterine condition , comprising intravaginally administering to the subject a combination of at least two active agents selected from an aromatase inhibitor , an antiinflammatory agent , and a uterine-selective estrogen receptor antagonist.240.-. (canceled) This application is a continuation of U.S. patent application Ser. No. 12/587,004, filed Sep. 29, 2009, which claims priority under 35 U.S.C. §119(e) to Provisional U.S. Patent Application Ser. No. 61/194,491, filed Sep. 29, 2008, the disclosure of each is incorporated by reference herein.The invention relates generally to pharmaceutical methods and compositions in which two or more active agents, as will be specified, are combined for the treatment of estrogen-dependent hyperproliferative uterine disorders such as endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and related conditions. As such, the invention finds utility in the fields of medicine, pharmaceutical formulation, and drug delivery.Endometriosis is an estrogen-dependent disease that affects about ...

TWO-COMPONENT PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PAIN

The present invention is directed to a pharmaceutical composition that includes a combination of about 2-5 milligrams of a non-steroidal anti-inflammatory drug and from about 2-30 milligrams of an opioid analgesic in a single pharmaceutical dosage unit that can provide effective chronic pain management with the added benefit of reduced side effects such as withdrawal and gastrointestinal disorders. The non-steroidal anti-inflammatory drug may be piroxicam and the opioid analgesic may be buprenorphine. The present invention also provides for a method of managing pain in a patient that includes administering the pharmaceutical composition previously described. The pharmaceutical composition previously described may be administered in a single or multiple dosage regimens. 1. A pharmaceutical dosage unit comprising about 2-5 milligrams of a non-steroidal anti-inflammatory drug and about 2-30 milligrams of an opioid analgesic for heating chronic pain.2. The pharmaceutical dosage unit of claim 1 , wherein the non-steroidal anti-inflammatory drug is present in an amount of about 2-3 milligrams.3. The pharmaceutical dosage unit of claim 1 , wherein the non-steroidal anti-inflammatory drug is present in an amount of about 2 milligrams.4. The pharmaceutical dosage unit of claim 1 , wherein the non-steroidal anti-inflammatory drug is piroxicam.5. The pharmaceutical dosage unit of claim 1 , wherein the opioid analgesic is present in an amount of about 2-15 milligrams.6. The pharmaceutical dosage unit of claim 1 , wherein the opioid analgesic is present in an amount of about 2 milligrams.7. The pharmaceutical dosage unit of claim 1 , wherein the opioid analgesic is buprenorphine.8. The pharmaceutical dosage unit of claim 1 , wherein the pharmaceutical dosage unit is delivered by sublingual claim 1 , mucosal claim 1 , parenteral claim 1 , intravenous claim 1 , intramuscular claim 1 , transdermal administration and combinations thereof.9. The pharmaceutical dosage unit of claim 1 ...

Antiviral compounds

The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.

COMBINATION

The invention provides a combination comprising at least one compound selected from dichlorophen, chlorprothixene, perphenazine, thioridazine, trifluoperazine and edetate or a pharmaceutically acceptable derivative thereof and a carbapenem or a pharmaceutically acceptable derivative thereof. This combination is particularly useful for the treatment of microbial infections. 1. A combination comprising: (i) at least one compound selected from dichlorophen , chlorprothixene , perphenazine , thioridazine , trifluoperazine and edetate or a pharmaceutically acceptable derivative thereof; and (ii) a carbapenem or a pharmaceutically acceptable derivative thereof.2. The combination according to claim 1 , wherein the carbapenem is selected from one or more of imipenem claim 1 , meropenem claim 1 , doripenem and ertapenem or a pharmaceutically acceptable derivative thereof.3. The combination according to claim 1 , wherein the carbapenem is meropenem or a pharmaceutically acceptable derivative thereof.4. (canceled)5. The method according to claim 16 , wherein the microbial infection is a bacterial infection selected from at least one a gram-negative bacterial infection.6E. coliKlebs. pneumoniae.. The method according to claim 5 , wherein the bacterial infection is caused by or7. The method according to claim 17 , wherein the infection is caused by a drug-resistant strain of the bacteria.8. (canceled)9. (canceled)10. The combination according to claim 1 , wherein the combination is used to treat a microbial infection.11E. coliKlebs. pneumoniae.. The combination according to claim 19 , wherein the bacterial infection is a gram-negative bacterial infection caused by or12. The combination according to claim 10 , wherein the microbial infection is caused by a drug-resistant strain.13gardnerellasalmonellosisEscherichia coli, Klebs. pneumoniae, Klebs. oxytoca, Pr. mirabilis, Pr. rettgeri, Pr. vulgaris, Haemophilis influenzae, Enterococcus faecalis, Enterococcus faeciumEnterobacter ...

TREATMENT OF INFLAMMATORY DISORDERS IN NON-HUMAN MAMMALS

The present invention relates to the prevention, reduction, inhibition and reversal of pain and inflammation in a non-human mammal by administration of an inhibitor of soluble epoxide hydrolase, as sole active agent or co-administered with other active agents. 1. A method of preventing , ameliorating , delaying the progression and/or reversing the progression of an inflammatory condition in a non-human mammal , comprising administering to the mammal an inhibitor of soluble epoxide hydrolase (sEH).2. A method of enhancing or maintaining the anti-inflammatory efficacy and/or anti-nociceptive efficacy and reducing undesirable side effects of a non-steroidal anti-inflammatory drug (“NSAID”) in a non-human mammal , comprising co-administering to the non-human mammal in need thereof an inhibitor of soluble epoxide hydrolase and the anti-inflammatory agent.3. A method of preventing , ameliorating , delaying the progression and/or reversing the progression of chronic pain in a non-human mammal , comprising administering to the mammal an inhibitor of soluble epoxide hydrolase (sEH).4. A method of enhancing or maintaining the anti-nociceptive efficacy on chronic or neuropathic pain and reducing undesirable side effects of an active agent selected from the group consisting of NSAIDs , Gamma-aminobutyric Acid (GABA) analogs , phosphodiesterase inhibitors , N-methyl-D-aspartate receptor antagonists , opioids and sodium channel blockers , or analogs or pro-drugs thereof , in a non-human mammal , comprising co-administering to the non-human mammal in need thereof an inhibitor of soluble epoxide hydrolase and the active agent , or an analog or pro-drug thereof.5. The method of any one of to , wherein the non-human mammal is canine , feline , equine , bovine , ovine or porcine.6. The method of any one of to , wherein the non-human mammal is an ungulate.7. The method of claim 6 , wherein the inflammatory condition is laminitis.8. The method of any one of to claim 6 , wherein the ...

USE AND APPLICATION REGIMEN OF A PHARMACEUTICAL COMPOSITION CONTAINING LEVONORGESTREL AND A COX INHIBITOR FOR ON-DEMAND CONTRACEPTION

The invention relates to a method of hormonal female controlled “on demand” contraception, in which a pharmaceutical preparation comprising a COX inhibitor and levonorgestrel is taken on demand prior to expected sexual intercourse. Further subjects of the invention relate to pharmaceutical compositions and application regimes for “on demand” contraception. 1. A method of female controlled “on demand” contraception , comprising administering a pharmaceutical composition comprising levonorgestrel and a COX inhibitor , selected from the group consisting of indomethacin , diclofenac , naproxen , ibuprofen , nimesulide , ketoprofen , and piroxicam , to a female on demand and once in a period of 0-24 hours prior to expected sexual intercourse.2. The method according to claim 1 , characterized in that the pharmaceutical formulation is administered at the earliest 24 hours before expected sexual intercourse.3. The method according to claim 1 , characterized in that the pharmaceutical formulation is administered once 0-6 hours prior to expected sexual intercourse.4. The method according to claim 1 , characterized in that the pharmaceutical formulation is administered once 0-1 hours prior to expected sexual intercourse.5. The method according to claim 1 , characterized in that the COX inhibitor is diclofenac claim 1 , indomethacin claim 1 , ibuprofen claim 1 , naproxen or piroxicam.6. (canceled)7. (canceled)8. The method of claim 1 , characterized in that the COX inhibitor is diclofenac.9. The method of claim 1 , characterized in that the COX inhibitor is indomethacin.10. The method of claim 1 , characterized in that the COX inhibitor is naproxen.11. The method of claim 1 , characterized in that the COX inhibitor is ibuprofen.12. The method of claim 1 , wherein the amount of COX inhibitor administered is selected from the group consisting ofIndomethacin: 50-400 mg/day;Diclofenac: 50-400 mg/day;Naproxen: 500-3000 mg/day;Ibuprofen: 500-5000 mg/day;Nimesulide: 100-500 mg/day; ...

PHARMACEUTICAL COMPOSITION FOR TREATMENT OF EYE PAIN, CONTAINING PGE2 SYNTHESIS INHIBITOR

The present invention relates to a pharmaceutical composition for the treatment of eye pain, containing a PGE2 synthesis inhibitor. The use of the pharmaceutical composition for the prevention or treatment of eye pain according to the present invention, which contains the PGE2 synthesis inhibitor as an active ingredient, makes it possible to alleviate the symptoms of eye pain by selectively inhibiting the PGE2 expression level, and also has the advantages of treating and preventing xerophthalmia and of overcoming and preventing eye discomfort caused by various inflammation-inducing circumstances including following surgery. Also, by using a kit for detecting the amount of PGE2, PGD2 and COX2, the present invention makes it possible to easily diagnose eye-pain symptoms in clinical practice, and can be widely used in checking the state not only of patients having xerophthalmia but also patients following eye surgery. 128-. (canceled)29. A method of preventing or treating ocular pain by administering a PGE2 synthesis inhibitor to a mammal , wherein the PGE2 synthesis inhibitor is selected from the group consisting of 15-deoxy-A12 , 14-PGJ2 , Exisulind , NS-398 , Leukotnene C4 , mk-886 , MF63 , celecoxib , Thienopyrrole , Naphthalene disulphonamide , and γ-hydroxybutenolide.30. A method of preventing or treating ocular pain by administering a COX2 inhibitor to a mammal , wherein the COX2 synthesis inhibitor is selected from the group consisting of Nimesulide , 3 ,5-di-tert-butyl-4-hydroxybenzylidene)-2-ethyl-1 ,2-isothiazolidine-1 ,1 -dioxide , Meloxicam , cis-Stilbenes , and Ibuprofen.31. (canceled)32. (canceled)33. The method of claim 29 , wherein the ocular pain is ocular pain resulting from dry eye syndrome claim 29 , inflammatory ocular disease or the use of a contact lens.34. The method of claim 30 , wherein the ocular pain is ocular pain resulting from dry eye syndrome claim 30 , inflammatory ocular disease or the use of a contact lens. The present invention ...

Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase

This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) 11. The method according to any of claim 10 , wherein J is selected from the group consisting of a —C-Calkyl-C-Cheteroalkyl-C-Calkyl- claim 10 , —C-Calkyl-aryl-C-Calkyl- claim 10 , —C-Calkyl-aryl-C-Cheteroalkyl- claim 10 , —C-Calkyl-cycloalkyl-C-Calkyl- claim 10 , —C-Cheterocyclyl-aryl-C-Calkyl- claim 10 , —C-Cheterocyclyl-aryl-C-Cheteroalkyl- claim 10 , —C-Calkyl-C-Cheterocyclyl-C-Calkyl- claim 10 , —C-Calkyl-heteroaryl-C-Calkyl- claim 10 , —C-Calkyl-heteroaryl-C-Cheteroalkyl- claim 10 , —C-Cheterocyclyl-heteroaryl-C-Calkyl- claim 10 , —C-Calkyl-aryl-C-Calkynyl- claim 10 , —C-Calkyl-heteroaryl-C-Calkynyl- claim 10 , —C-Calkyl-aryl-C-Calkynyl-C-Calkenyl- claim 10 , —C-Calkyl-aryl-C-Calkenyl- claim 10 , —C-Calkyl-heteroaryl-C-Calkenyl- claim 10 , —C-Calkenyl-aryl-C-Calkyl- claim 10 , —C-Calkenyl-heteroaryl-C-Calkyl- claim 10 , —C-Calkylaryl-aryl-C-Calkyl- claim 10 , —C-Calkylaryl-heteroaryl-C-Calkyl- and —C-Calkyl-C-Ccycloalkyl-C-Calkyl- claim 10 , wherein each alkyl claim 10 , alkenyl claim 10 , alkynyl claim 10 , heteroalkyl claim 10 , aryl claim 10 , heteroaryl claim 10 , heterocyclyl claim 10 , and cycloalkyl moiety is optionally substituted.12. The method according to claim 11 , wherein J is —C-Calkyl-heteroaryl-C-Calkyl- or —C-Calkyl-aryl-C-Calkyl-.14. The method according to any of to claim 11 , wherein U and Uare a covalent bond.15. The method according to any of to claim 11 , wherein U and Uare —C(O)—.16. The method according to any of to claim 11 , wherein U is —C(O)—O—C-Calkyl-.17. The method according to any of to claim 11 , wherein Uis —C-Calkyl-O—C(O)—.21. The method according to any of to claim 11 , wherein Z is —NROR claim 11 , Rand Rare H claim 11 , and L is a covalent bond.22. The method according to any of to claim 11 , wherein Z is H and L is —N(OH). ...

Pharmaceutical compositions comprising meloxicam

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a dosage form to the migraine patient , wherein the dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the migraine patient experiences a reduction in photophobia as a result of orally administering the dosage form to the migraine patient.2. The method of claim 1 , wherein the dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , wherein the dosage form is a solid oral dosage form having a shorter Tof meloxicam in the human being than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , and 3) does not contain a ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a dosage form to the migraine patient , wherein the dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the human migraine patient is free of photophobia two hours after the dosage form is orally administered to the human migraine patient.2. The method of claim 1 , wherein the dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , wherein the dosage form is a solid oral dosage form having a shorter Tof meloxicam in the human being than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , and 3) does not contain a ...

LONG-ACTING POLYMERIC DELIVERY SYSTEMS

Compositions comprised of a delivery vehicle or delivery system and an active agent dispersed within the delivery vehicle or system, wherein the delivery vehicle or system contains a polyorthoester polymer and a polar aprotic solvent. Also disclosed are low viscosity delivery systems for administration of active agents. The low viscosity delivery systems have a polyorthoester polymer, a polar aprotic solvent and a solvent containing a triglyceride viscosity reducing agent. Compositions described include an amide- or anilide-type local anesthetic of the “caine” classification, and a non-steroidal anti-inflammatory drug (NSAID), along with related methods, e.g., for treatment of post-operative pain or for prophylactic treatment of pain. The compositions are suitable for delivery via, e.g., direct application and instillation, intradermal injection, subcutaneous injection, and nerve block (perineural). 1. A composition , consisting essentially of: a delivery vehicle , an amide-type local anesthetic , and a non-steroidal anti-inflammatory drug (NSAID) , wherein the ratio of the amide-type local anesthetic to the NSAID ranges from about 15:1 to 50:1 , and wherein the NSAID is present in the composition in an amount between about 0.005-0.75 wt %.2. The composition of claim 1 , wherein the amide-type local anesthetic is present in the composition in an amount ranging from about 0.1 to 8.0 wt % and the NSAID is present in the composition in an amount ranging from about 0.01-0.5 wt %.3. The composition of claim 1 , wherein the delivery vehicle is a sustained-release delivery vehicle.4. The composition of claim 1 , wherein the delivery vehicle is aqueous based.5. The composition of claim 3 , wherein the sustained-release delivery vehicle is a bioerodible or biodegradable polymer.7. The composition of claim 6 , wherein the delivery vehicle comprises the polyorthoester claim 6 , a polar aprotic solvent and a triglyceride viscosity reducing agent.8. The composition of claim 7 , ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a solid dosage form to the migraine patient , wherein the solid oral dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the human migraine patient is free of migraine pain two hours after the solid dosage form is orally administered to the human migraine patient.2. The method of claim 1 , wherein the solid oral dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the solid oral dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the solid oral dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , the solid oral dosage form having a shorter Tof meloxicam in the human being than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a dosage form to the migraine patient , wherein the dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the migraine patient experiences a reduction in nausea as a result of orally administering the dosage form to the migraine patient.2. The method of claim 1 , wherein the dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , wherein the dosage form is a solid oral dosage form having a shorter Tof meloxicam in the human being than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , and 3) does not contain a ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a dosage form to the migraine patient , wherein the dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the human migraine patient is free of nausea two hours after the dosage form is orally administered to the human migraine patient.2. The method of claim 1 , wherein the dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , wherein the dosage form is a solid oral dosage form having a shorter Tof meloxicam in the human migraine patient than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , and 3) does not contain a ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tof meloxicam of 3 hours or less. 1. A method of treating migraine comprising: selecting a human migraine patient with a history of inadequate response to prior migraine treatments , and orally administering a dosage form to the migraine patient , wherein the dosage form comprises a combination of: 1) a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD) , 2) a bicarbonate , and 3) a rizatriptan , wherein the migraine patient experiences a reduction in phonophobia as a result of orally administering the dosage form to the migraine patient.2. The method of claim 1 , wherein the dosage form contains 400 mg to 600 mg of the bicarbonate.3. The method of claim 1 , wherein the dosage form contains about 5 mg to about 50 mg of meloxicam.4. The method of claim 1 , wherein the dosage form contains about 50 mg to about 200 mg of the SBEβCD.5. The method of claim 1 , wherein the dosage form is a solid oral dosage form having a shorter Tof meloxicam in the human being than a reference dosage form that: 1) contains the same amount of meloxicam claim 1 , 2) does not contain an SBEβCD claim 1 , and 3) does not contain a ...

PHARMACEUTICAL COMPOSITIONS COMPRISING MELOXICAM

Disclosed herein are compositions comprising an NSAID such as meloxicam in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of conditions such as pain. 1. A method of treating migraine comprising: orally administering a solid dosage form to a human being suffering from a migraine , wherein the solid dosage form comprises: 1) a complex of meloxicam and a sulfobutyl ether β-cyclodextrin (SBEβCD) , and 2) a bicarbonate , wherein orally administering the solid dosage form to the human being results in a Tof meloxicam that is shorter than a Tof a reference solid dosage form that: 1) contains the same amount of meloxicam , 2) does not contain an SBEβCD , and 3) does not contain a bicarbonate , wherein the solid dosage form has been shown to have a median Tof meloxicam that is less than 1 hour in human subjects.2. The method of claim 1 , wherein the solid dosage form contains about 10 mg to about 20 mg of meloxicam.3. The method of claim 1 , wherein the solid dosage form contains about 15 mg of meloxicam.4. The method of claim 1 , wherein the SBEβCD has about 6 to about 7 sulfobutyl ether groups for each molecule of β-cyclodextrin.5. The method of claim 1 , wherein the solid dosage form contains about 50 mg to about 200 mg of the SBEβCD.6. The method of claim 1 , wherein the solid dosage form contains about 100 mg of the SBEβCD.7. The method of claim 1 , wherein the bicarbonate is sodium bicarbonate.8. The method of claim 1 , wherein the solid dosage form contains about 400 mg to about 600 mg of the bicarbonate.9. The method of claim 7 , wherein the solid dosage form contains about 500 mg of sodium bicarbonate.10. The method of claim 1 , wherein the solid dosage form further comprises an acid inhibitor.11. The method of claim 10 , wherein the acid inhibitor is a proton pump inhibitor.12. The method of claim 11 , ...

NOVEL FORMULATION OF MELOXICAM

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments. 1. A method for producing a composition , comprising the steps of:dry milling a solid biologically active material and a millable grinding matrix in a mill comprising a plurality of milling bodies, for a time period sufficient to produce particles of the biologically active material dispersed in an at least partially milled grinding material,wherein the biologically active material is meloxicam.241.-. (canceled) The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.Poor bioavailability is a significant problem encountered in the development of compositions in the therapeutic, cosmetic, agricultural and food industries, particularly those materials containing a biologically active material that is poorly soluble in water at physiological pH. An active material's bioavailability is the degree to which the active material becomes available to the target tissue in the body or other medium after systemic administration through, for example, oral or intravenous means. Many factors affect bioavailability, including the form of dosage and the solubility and dissolution rate of the active material.In therapeutic applications, poorly and slowly water-soluble materials tend to be eliminated from the gastrointestinal tract before being absorbed into the circulation. In addition, ...

CALMODULIN INHIBITORS, CHK2 INHIBITORS AND RSK INHIBITORS FOR THE TREATMENT OF RIBOSOMAL DISORDERS AND RIBOSOMAPATHIES

The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA. 136-. (canceled)38. The phenothiazine compound of claim 37 , wherein Xis S.39. The phenothiazine compound of claim 38 , wherein Ris a -Calkyl.40. The phenothiazine compound of claim 39 , wherein Ris isopropyl.41. The phenothiazine compound of claim 40 , wherein each R is independently selected from the group consisting of H claim 40 , halo claim 40 , C-Calkyl claim 40 , C-Chaloalkyl claim 40 , OH claim 40 , C-Calkoxy claim 40 , NH claim 40 , NO claim 40 , C-Calkylamino claim 40 , di(C-Calkyl)amino claim 40 , CN or COH.42. The phenothiazine compound of claim 41 , wherein each R independently is selected from the group consisting of H claim 41 , CI claim 41 , F claim 41 , Br claim 41 , methyl claim 41 , trifluoromethyl claim 41 , OH claim 41 , NH claim 41 , NO claim 41 , CN or COH.43. The phenothiazine compound of claim 38 , wherein Ris an optionally substituted alkylaryl.44. The phenothiazine compound of claim 43 , wherein Ris C-Calkylphenyl.45. The phenothiazine compound of claim 43 , wherein Ris benzyl.46. The phenothiazine compound of claim 45 , wherein each R is independently selected from the group consisting of H claim 45 , halo claim 45 , C-Calkyl claim 45 , C-Chaloalkyl claim 45 , OH claim 45 , C-Calkoxy claim 45 , NH claim 45 , NO claim 45 , C-Calkylamino claim 45 , di(C-Calkyl)amino claim 45 , CN or COH.47. The phenothiazine compound of claim 46 , wherein each R independently is selected from the ...

ADMINISTRATION AND DOSAGE OF DIAMINOPHENOTHIAZINES

The invention provides novel regimens for treatment of neurodegenerative disorders utilising methylthioninium (MT)-containing compounds. The regimens are based on novel findings in relation to the dosage of MT compounds, and their interaction with symptomatic treatments based on modulation of acetylcholinesterase levels. 2. (canceled)3. The method as claimed in claim 1 , wherein the total daily dosage is 2 to 15 mg; or 3 to 10 mg.411-. (canceled)1314-. (canceled)16. The method as claimed in claim 1 , wherein the or each protic acid is an inorganic acid.1718-. (canceled)19. The method as claimed in claim 1 , wherein the or each protic acid is an organic acid.20. The method as claimed in claim 19 , wherein the or each protic acid is selected from HCO; CHCOOH; methanesulfonic acid claim 19 , 1 claim 19 ,2-ethanedisulfonic acid claim 19 , ethansulfonic acid claim 19 , naphthalenedisulfonic acid claim 19 , and p-toluenesulfonic acid.22. The method as claimed in claim 21 , wherein the total daily dose of LMTM is around 0.8 to 33 mg/day claim 21 , more preferably 6 to 12 mg/day of LMTM total.23. The method as claimed in wherein the dose of LMTM is around 9 mg/once per day.2537-. (canceled)3940-. (canceled)41. The method as claimed in claim 1 , wherein the subject has not historically received treatment with an acetylcholinesterase inhibitor or an N-methyl-D-aspartate receptor antagonist.42. The method as claimed in claim 1 , wherein the subject has historically received treatment with an acetylcholinesterase inhibitor and\or an N-methyl-D-aspartate receptor antagonist claim 1 , but ceased that medication at least 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , or 8 weeks prior to treatment with the MT containing compound.43. The method as claimed in claim 1 , wherein the subject is selected as one who is receiving treatment with an acetylcholinesterase inhibitor and\or an N-methyl-D-aspartate receptor antagonist claim 1 ,wherein said ...

AZAHETEROCYCLIC COMPOUNDS

The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases. 2. The compound according to claim 1 , or its stereoisomers or tautomers claim 1 , orpharmaceutically acceptable salts of each of the foregoing, including mixtures thereof in all ratios, in which the residues not designated in greater detail have the meaning indicated for Formula (I), but in whichin Subformula 1{'sub': 3', '2, 'Z is H, NCH, CH,'}in Subformula 2{'sup': 5', '4, 'W is —NRCOR,'}in Subformula 3{'sup': 4', '5, 'W is —CON(R)(R),'}in Subformula 4Y is O,in Subformula 5{'sub': 3', '2, 'Z is H, NCH, CH,'}{'sup': 4', '5, 'R, Rare methyl,'}in Subformula 6{'sup': 5', '4, 'W is —NRCOR,'}{'sup': 4', '5, 'R, Rtogether with the atoms they are attached to, form piperidin-2-one or pyrrolidin-2-one,'}{'sup': '6', 'Ris H,'}in Subformula 7{'sup': 4', '5, 'W is —CON(R)(R),'}{'sup': '4', 'Ris methyl,'}{'sup': '5', 'Ris H,'}in Subformula 8X is N,in Subformula 9{'sup': 5', '4, 'W is —NRCOR,'}{'sup': '4', 'Ris methyl, hydroxymethyl, tert-butyloxy, neopentyl,'}{'sup': '5', 'Ris H, methyl, ethyl, isopropyl, fluoromethyl,'}in Subformula 10{'sup': 5', '4, 'W is —NRCOR,'}{'sup': 4', '5, 'R, Rare methyl,'}in Subformula 11X is N,{'sup': '1', 'Ris H,'}in Subformula 12{'sup': '1', 'Cycis indanyl, indolyl, isoquinolinyl, benzoisoxazolyl,'}in Subformula 13{'sup': '1', 'Cycis phenyl, which is independently mono-, di- or tri-substituted by F, Br, CN, O(LA), LA,'}in Subformula 14{'sup': 1', '2, 'Cycis phenyl, which is substituted in 4-position by L-Cyc,'}in Subformula 15{'sup': 1', '2, 'Cycis phenyl, which is substituted in 4-position by L-Cyc, and in 1- and/or 2-position by F,'}in Subformula 16X is N,Y is O,{'sub': 3', '2, 'Z is H, NCH, CH,'}in Subformula 17X is N,Y is O,{'sub': 3', '2, 'Z is NCH, CH,'}{'sup': '1', 'Ris H,'}in Subformula 18{'sup': 5', '4, 'W is ...

FIXED DOSE COMBINATION FOR PAIN RELIEF WITHOUT EDEMA

Methods for individualized therapy of arthritic pain using a non-steroidal anti-inflammatory drug (COX-2 inhibitor). Said methods comprise basing COX-2 inhibitor dose on each patient's pharmacokinetic response to said COX-2 inhibitor. 1. A composition for treating pain without inducing edema comprising a NSAID and a diuretic , wherein the composition is administered in a fixed-dose combination.2. The composition of claim 1 , wherein the NSAID is selected from the group consisting of aspirin claim 1 , diclofenac claim 1 , diflusnisal claim 1 , etodolac claim 1 , fenoprofen claim 1 , flubiprofen claim 1 , ibuprofen claim 1 , indomethacin claim 1 , ketoprofen claim 1 , ketorolac claim 1 , meclofenamate claim 1 , nabumetone claim 1 , naproxen claim 1 , oxaprozin claim 1 , phenylbutazone claim 1 , piroxicam claim 1 , salicylate claim 1 , sulindac claim 1 , tolmetin claim 1 , celecoxib claim 1 , rofecoxib claim 1 , etoricoxib claim 1 , polmacoxib claim 1 , lumiracoxib claim 1 , parecoxib claim 1 , valdecoxib claim 1 , chlorthalidone and combinations thereof and combinations thereof.3. The composition of claim 2 , wherein the NSAID is a COX-2 inhibitor.4. The composition of claim 3 , wherein the COX-2 inhibitor is celecoxib claim 3 , etoricoxib claim 3 , polmacoxib claim 3 , lumiracoxib claim 3 , parecoxib claim 3 , valdecoxib claim 3 , chlorthalidone or a combination thereof.5. The composition of claim 3 , wherein the COX-2 inhibitor is celecoxib.6. The composition of claim 1 , wherein the diuretic is selected from the group consisting of amiloride claim 1 , bumetanide claim 1 , chlorothalidone claim 1 , ethacrynic acid claim 1 , furosemide claim 1 , hydrochlorothiazide claim 1 , indapamide claim 1 , metolazone claim 1 , torsemide claim 1 , triamterene claim 1 , acetazolamide claim 1 , theophylline claim 1 , chlorthalidone claim 1 , spironolactone claim 1 , and combinations thereof.7. The composition of claim of claim 6 , wherein the diuretic is hydrochlorothiazide.8. The ...

ACTIVATED LYMPHOCYTIC CELLS AND METHODS OF USING THE SAME TO TREAT CANCER AND INFECTIOUS CONDITIONS

Provided herein are methods for treating a patient with HIV, cancer, a viral infection, or a bacterial infection, comprising administering an effective amount of activated lymphocytic cellular compositions. Related compositions, kits, and methods for modulating the immune system using the activated lymphocytic cellular compositions are also provided. 1. A method of treating a patient with HIV , cancer , a viral infection , or a bacterial infection , the method comprising administering an effective amount of a lymphocytic cellular composition comprising activated natural killer (NK) cells to the patient.25-. (canceled)6. The method of claim 1 , wherein the cellular composition further comprises activated gamma delta T cells (GDT cells).7. The method of claim 1 , wherein the cellular composition further comprises invariant natural killer T cells (iNKT cells).8. The method of claim 1 , wherein the cellular composition further comprises CD3T cells.9. The method of claim 1 , wherein prior to administration to the patient claim 1 , the lymphocytic cellular composition is activated by mixing/incubating/contacting the cells with at least one cytokine and optionally soluble fibroblast growth factor receptor 1 (sFGFR1).10. The method of claim 9 , wherein the cytokine is selected from the group consisting of IL-2 claim 9 , IL-15 claim 9 , IL-21 claim 9 , Flt3-L claim 9 , stem cell factor (SCF) claim 9 , IL-7 claim 9 , IL-12 claim 9 , and IL18 claim 9 , and any combination thereof.1112-. (canceled)13. The method of claim 1 , wherein the method further comprises pre-conditioning the patient prior to administering the lymphocytic cellular composition by administering at least one lympho-suppressive agent claim 1 , chemotherapeutic agent claim 1 , or immunosuppressive agent for between 3-5 days prior to administering the lymphocytic cellular composition.14. The method of claim 13 , wherein the lympho-suppressive or chemotherapeutic agent comprises any one of 6TG claim 13 , 6-MMP ...