ПРИМЕНЕНИЕ ПРОИЗВОДНЫХ 3,5-ВТОР-4-НОРХОЛЕСТАНА ДЛЯ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОГО СРЕДСТВА - ЦИТОПРОТЕКТОРА

Настоящее изобретение относится к области фармакологии и медицины и касается применения производных 3,5-втор-4-норхолестана для получения лекарственного средства-цитопротектора, обладающего высокой активностью, за исключением нейропротектора. 3 н. и 16 з.п. ф-лы, 2 табл.

СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ, КОМПОЗИЦИЯ ДЛЯ ПРИГОТОВЛЕНИЯ ЛЕКАРСТВЕННОГО СРЕДСТВА

Описан способ получения соединения формулы где В - липид, предпочтительно холестерин, А - представляющий интерес фрагмент (ПИФ), Х - линкер, действием соединения I На соединение (II) в смеси или связанные с нуклеотидной последовательностью или фармацевтически активным агентом, R1-H и R2 - неподеленная пара или Н. Полученные соединения предназначены для лечения генетического нарушения или заболевания. 2 н. и 21 з.п. ф-лы, 1 табл., 6 ил.

ПРОИЗВОДНЫЕ, ПРИМЕНЯЕМЫЕ ДЛЯ ЛЕЧЕНИЯ МЫШЕЧНОЙ АТРОФИИ

Изобретение относится к применению производного общей формулы Iгде Rи Rнезависимо друг от друга представляют собой водород, n представляет собой целое число между 1 и 2, Rпредставляет собой группу -OH или группу -O(C-Cалкил), Rпредставляет собой C-Cалкильную группу, Rи Rпредставляют собой независимо друг от друга атом галогена, или его фармацевтически приемлемой соли в качестве лекарственного средства для лечения и/или предотвращения мышечной атрофии у млекопитающих, и/или для ограничения мышечной атрофии у млекопитающих, и/или для стимуляции мышечного роста у тренирующихся млекопитающих, стремящихся увеличить массу и качество мышц, предотвращая появление симптомов саркопении, связанных с возрастом или реабилитацией после потери мышц, возрастной мышечной атрофии и/или последствий лекарственного лечения, и/или иммобилизации, и/или кахексии. 11 з.п. ф-лы, 1 ил., 3 табл.

ПРИМЕНЕНИЕ СПЕЦИФИЧЕСКОГО АНТАГОНИСТА 5HT2 РЕЦЕПТОРОВ ДЛЯ ПРИГОТОВЛЕНИЯ ЛЕКАРСТВ, ПРИГОДНЫХ ДЛЯ ЛЕЧЕНИЯ СИНДРОМА АПНОЭ ВО СНЕ

Изобретение относится к медицине, в частности к приготовлению лекарств, пригодных для лечения синдрома апноэ во сне. Для этого предлагают использовать специфические антагонисты 5НТ2А рецепторов, такие как 1-(2-фторфенил)-3-(4-гидроксифенил)-проп-2-ен-1-он-О-(2-диметиламиноэтил)-оксим или его фармацевтически приемлемые соли. Способ обеспечивает заметное снижение индекса апноэ-гипноэ у таких больных. 2 с. и 2 з.п.ф-лы.

МЕДЛЕННО ВЫДЕЛЯЮЩЕЕ МЕДИКАМЕНТОЗНОЕ ПОЛИМЕРНОЕ ФОРМОВАННОЕ ИЗДЕЛИЕ И СПОСОБЫ ЕГО ПОЛУЧЕНИЯ, СПОСОБ БОРЬБЫ С ПАРАЗИТАМИ

Изобретение относится к медикаментозным полимерным формованным изделиям, которые удерживают большое количество активнодействующего вещества, и постепенно его выделяют с постоянной скоростью. Активнодействующее вещество содержится в пористом полимерном формованном изделии, выполненном путем растяжения в 1,1 - 10 раз полимерной композиции, включающей в себя 100 вес.ч. термопластичной смолы и 50-400 вес.ч. наполнителя, при этом количество активнодействующего вещества соответствует степени насыщения при растворении для данной термопластичной смолы. Способы получения данных изделий позволяют избежать истечения активнодействующего вещества при обеспечении его высокого содержания в формованном изделии. 5 с. и 13 з.п.ф-лы, 6 табл., 4 ил.

1-ФЕНИЛЭТИЛОВЫЙ ЭФИР 2-(2-(4-НИТРОБЕНЗОИЛ)ГИДРАЗОНО)-4-ОКСО-4-(4-МЕТИЛФЕНИЛ)БУТАНОВОЙ КИСЛОТЫ, ОБЛАДАЮЩИЙ АНАЛЬГЕТИЧЕСКОЙ АКТИВНОСТЬЮ

Изобретение относится к области органической и медицинской химии, а именно к 1-фенилэтиловому эфиру 2-(2-(4-нитробензоил)гидразоно)-4-оксо-4-(4-метилфенил)бутановой кислоты формулы 1. Предложенное соединение обладает выраженной анальгетической активностью и низкой токсичностью и может быть использовано в качестве лекарственного средства с анальгетическими свойствами. 1 табл., 3 пр.

ПРОФИЛАКТИЧЕСКОЕ ИЛИ ТЕРАПЕВТИЧЕСКОЕ СРЕДСТВО ДЛЯЛЕЧЕНИЯ РАССТРОЙСТВА СНА

... 1. Профилактическое или терапевтическое средство для лечения расстройства сна, содержащее комбинацию лекарственного средства для увеличения продолжительности медленноволнового сна и (S)-N-[2-(1,6,7,8-тетрагидро-2Н-индено[5,4-b]фуран-8-ил)этил]пропионамида. 2. Профилактическое или терапевтическое средство для лечения расстройства сна по п. 1, в котором лекарственное средство для увеличения продолжительности медленноволнового сна представляет собой по меньшей мере одно средство, выбранное из антагониста 5-НТ2А рецепторов, антагониста 5-НТ2С рецепторов, антагониста 5-НТ2А/2С рецепторов, ингибитора захвата серотонина, модулятора ГАМК и ингибитора захвата ГАМК. 3. Профилактическое или терапевтическое средство для лечения расстройства сна по п. 1, в котором лекарственное средство для увеличения продолжительности медленноволнового сна представляет собой по меньшей мере одно средство, выбранное из М-100907, ритансерина, тразодона, габапентина, тиагабина, Org-50081 и эпливансерина. 4. Применение ...

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ ПРОФИЛАКТИКИ И/ИЛИ ЛЕЧЕНИЯ ЖЕЛУДОЧНО-КИШЕЧНЫХ ЗАБОЛЕВАНИЙ, ВКЛЮЧАЯ ЯЗВУ

Изобретение относится к фармацевтическим композициям для предотвращения и/или лечения желудочно-кишечных заболеваний, включая язву, и к способу лечения таких заболеваний. Фармацевтические композиции в соответствии с изобретением в качестве активного компонента содержат производные циклического кетона формулы, приведенной в описании, или его стереоизомер или оптический изомер, или их возможные смеси, или его фармацевтически приемлемую кислую аддитивную соль или его четвертичное аммониевое производное в смеси с носителем (носителями), традиционно используемым в фармацевтических композициях.

ИММУНОРЕГУЛИРУЮЩИЕ СРЕДСТВА

АГОНИСТЫ GPR40

... 1. Соединение формулы (I):где кольцо А представляет собой возможно замещенную фенильную группу;кольцо В представляет собой возможно замещенную фенильную группу;Х представляет собой связь или линкерный фрагмент, содержащий от 1 до 8 атомов в линейной цепи;Y представляет собой связь или линкерный фрагмент, содержащий от 1 до 8 атомов в линейной цепи;Z представляет собой связь или выбран из группы, состоящей из возможно замещенного C-Cарила и возможно замещенного C-Cгетероарила, -С(=O)-, -C(=NR)-, -(CRR)-, -(CRR)O-, -(CRR)S-, -(CRR)NR'-, или представляет собой гетероатомную группу, выбранную из группы, состоящей из S, О, Р и NR'', где R'' выбран из группы, состоящей из Н, возможно замещенного C-Cалкила, возможно замещенного С-Сгетероалкила, возможно замещенного С-Сциклоалкила, возможно замещенного С-Cарила и возможно замещенного C-Cгетероарила;L представляет собой группу, способную высвобождать катион, или ее соль;Rвыбран из группы, состоящей из Н, OR, возможно замещенного C-Cалкила, возможно ...

НОВЫЕ ПРЕПАРАТЫ АЛЬФА -2,4-ДИСУЛЬФОФЕНИЛ-N-ТРЕТ-БУТИЛНИТРОНА

... 1. Фармацевтический препарат, содержащий концентрированный водный раствор двунатриевой соли α-(2,4-дисульфофенил)-N-трет-бутилнитрона и отличающийся тем, что концентрация находится в пределах от 50 до 600 мг/мл. 2. Препарат по п.1, где концентрация составляет от 100 до 600 мг/мл. 3. Препарат по п.1, где концентрация составляет от 200 до 400 мг/мл. 4. Препарат по п.1, где концентрация составляет примерно 400 мг/мл. 5. Препарат по любому из пп.1-4, где раствор продувают инертным газом и хранят в атмосфере инертного газа. 6. Препарат по п.5, где инертный газ представляет собой азот. 7. Препарат по любому из пп.1-6, где раствор забуферен с использованием физиологически приемлемого буфера в пределах рН от 7 до 9,5. 8. Препарат по п.7, где раствор забуферен при рН примерно 8,5. 9. Препарат по п.7 или 8, где буфер представляет собой фосфатный буфер. 10. Препарат по любому из пп.1-9, где раствор хранят в герметичном стеклянном сосуде с минимальным объемом свободного пространства, и это свободное ...

ЦИКЛОПЕНТИЛПРОИЗВОДНЫЕ ДИАЗЕНИЙДИОЛАТА

... 1. Соединение, имеющее формулу Iили его фармацевтически приемлемая соль, гдеRпредставляет собой водород, -OH, -O-Cалкил, =О или галоген;Rпредставляет собойводород,-C(О)OR,-CHC(О)OR,-(CH)OH,-CRROH,-C(O)O(CH)арил,-C(O)NRR,-C(O)SONRR,-CHOR,-W-C(О)OR,-W-OR,-Y или-P(О)(OR)(OR);Rпредставляет собой водород или -Cалкил;Rпредставляет собой водород, -OH или -C(О)OR;Rпредставляет собой водород или дейтерий;Rи Rпредставляют собой независимо -Cалкил, фторзамещенный -Cалкил, дейтерийзамещенный -Cалкил или -(CH)R, где любой атом углерода фторзамещенного -Cалкила моно- или дизамещен фтором и любой атом углерода дейтерийзамещенного -Cалкила моно- или дизамещен фтором;Rв каждом случае, в котором он присутствует, представляет собой водород, -Cалкил или -(CH)N(CH);Rи Rв каждом случае, в котором они присутствуют, независимо представляют собой -Cалкил;Rпредставляет собой -OH, -O-Cалкил, -OCD, -OC(О)OCалкил, -NH, -CH, -Nили W;W представляет собой незамещенное 5- или 6-членное гетероарильное кольцо, имеющее 1, ...

ПРОИЗВОДНЫЕ, ПРИМЕНЯЕМЫЕ ДЛЯ ЛЕЧЕНИЯ МЫШЕЧНОЙ АТРОФИИ

RADIKALFÄNGER ("SPIN TRAPS") ZUR BEHANDLUNG VON MIT OXIDATION VON LIPIDEN UND PROTEINEN VERBUNDENEN ERKRANKUNGEN

ENZYMATISCHE ÄNDERUNG DES HAARWUCHSES

NEUE ACETOPHENONOXIMDERIVATE

TRIARYLMETHANVERBINDUNGEN ZUR BEHANDLUNG VON KREBS, AKTINISCHER KERATOSE UND KAPOSISARKOM

N,N'-BIS (SULFONYL) HYDRAZINE DIE ALS ANTINEOPLASTISCHE MITTEL NÜTZLICH SIND

Pharmacologically Active Oximes and Processes for the Preparation thereof

... 1,178,198. Indanone - oxime derivatives. MEAD JOHNSON & CO. 18 Oct., 1968 [20 Oct., 1967], No. 49565/68. Heading C2C. Novel compounds I in which R is H or methyl and their acid addition salts are prepared by reacting the appropriate ketone with hydroxylamine or alternatively reacting the disodium or dipotassium salt of 3- phenylindan-1-one oxime with a 2-methyl- or 2-dimethyl-aminoethyl reactive ester, followed, if desired, by acid addition salt formation. Intermediate 3 - (2 - dimethylaminoethyl)- 3 - phenyl-indan-1-one is prepared by reacting the disodium salt of 3-phenyl-indan-1-one with 2- dimethylaminoethyl chloride. Pharmaceutical compositions comprise a compound I together with a suitable carrier or diluent, are administered orally or parenterally and have an antidepressant effect.

Pharmaceutical combination products for parkinsons disease

Thiocarbamoylhydrazines

The invention comprises hydrazines of the general formula R1NHCSNHNHCSNR2R3 wherein of the symbols R1 R2 and R3, one stands for an alkyl radical of not more than 4 carbon atoms or for an alkenyl radical and, of the remaining two symbols, one stands for hydrogen or for an alkyl radical of not more than 4 carbon atoms, an alkenyl radical, an aralkyl radical optionally substituted by halogen, methyl or methoxy radicals, a cycloalkyl radical, an alkoxyalkyl radical or an alkylthioalkyl radical and the other stands for an alkyl radical of not more than 4 carbon atoms, an alkenyl radical, an aralkyl radical optionally substituted by halogen, methyl or methoxy radicals, a cycloalkyl radical, an alkoxyalkyl radical or an alkylthioalkyl radical or wherein R1 stands for an alkyl or alkenyl radical, R2 stands for hydrogen and R3 stands for a carbethoxy radical, provided that when R2 stands for hydrogen, R1 and R3 do not both stand for the methyl, ethyl or allyl radicals and, when R1 stands for the ...

SUBSTITUTED OXIMES PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS

... 1323453 Analgesic medicines CHOAY SA 7 Aug 1970 [8 Aug 1969] 38147/70 Heading A5B [Also in Division C2] Pharmaceutical compositions having analgesic activity, for oral, parenteral or rectal administration, comprise a compound of formula I: in which R 1 represents one or more substituents each attached at any available position on the phenyl nucleus and selected from -NO 2 , -OH, carbomethoxy, methyl-sulfonyl, halogen and alkyl groups containing one to three carbon atoms, two chlorine or methyl radicals not simultaneously occupying the 2 and 6 positions on the phenyl nucleus, or, except when R 2 is hydrogen and R 3 and R 4 are both ethyl groups, R 1 represents a hydrogen atom; R 2 is hydrogen or a methyl group; R 3 and R 4 are alkyl radicals containing from two to four carbon atoms, or together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heterocyclic group; and Y is an aliphatic divalent hydrocarbon group containing from two to four carbon atoms ...

PHARMACEUTICAL COMPOSITION

Pharmaceutical composition comprising at least one quinone for use in the treatment of cancer and virus infections.

The invention relates to a pharmaceutical composition comprising at least one quinone and to its use in the treatment of disease, especially cancer and virus infections. The composition of the invention comprises at least one quinone dissolved or dispersed in a liquid diluent of carrier at a concentration of about 10-3 moles/litre or below. Preferably down to 10-18 moles/litre.

PHARMACEUTICAL COMPOSITION

New pharmaceuticals combinations for nos inhibitors.

The present invention relates to new pharmaceutical uses for compounds that exhibit activity as nitric oxide synthase (nos)inhibitors. Specifically, it relates to the use of nos inhibitors, particularly selective neuronal nos (nnos)inhibitors, alone or in combination with another active agent, in particular, either an ssri or an nk-1 receptor antagonist, for the treatment of disorders or conditions the treatment which can be effected or facilitated by altering circadian rhythms. Examples of such disorders and conditions are blindness, obesity, seasonal affective disorder, bipolar disorder, jet lag, circadian sleep rhythms disorder, sleep deprivation, parasomnias, rem sleep disorders, hypersomnia, sleep-wake cycle disorders, narcolepsy and sleep disorders associated with shift work or irregular work schedules; nocturnal enuresis, and restless-legs syndrome.

Methods of administering pirfenidone therapy

New pharmaceutical combinations for nos inhibitors

Methods of administering pirfenidone therapy.

Pharmaceutical composition.

Use of trinitrobenzenes or carminic acid in the treatment of cancer or viral diseases

Method of preparation of active derivatives of acétoxime.

New pharmacetical combinations for nos inhibitors

Pharmaceutical composition

Methods of administering pirfenidone therapy.

Methods of administering pirfenidone therapy.

PROCEDURE FOR THE PRODUCTION OF 2 (E) - PHENYLMETHYLEN-CYCLOHEPTAN-1-ON (E) - OXIM

BENZAMIDOXIME AS PRELIMINARY STAGES OF ANTIPNEUMOCYSTI ACTIVE SUBSTANCES

GABOXADOL TO THE TREATMENT OF DEPRESSIONS AND OTHER AFFEKTIVEN DISTURBANCES

POLYAMINE CONNECTIONS TO THE TREATMENT OF CHEMOKIN RECEPTOR OBTAINING DISEASES

Preparation of chemical compounds against liver cancer

Salicylsäure Hydrazid Oxim-Liganden (H2L) und seine Komplexe Mangan (II), Kobalt (II), Nickel (II), Kupfer (II), Zink (II) und Cadmium (II) wurden hergestellt und durch Elementaranalysen, IR-, UV-VIS, IH-NMR und Massenspektren, magnetische Suszeptibilität, Leitfahigkeit, thermische Analyse (DTA und TGA) und ESR-Messungen. Der Ligand und einige Komplexe zeigte eine hohe potentielle zytotoxische Aktivität und starke Wirkungenaufgrund ihrer antiproliferativen Wirkung mit einem IC50 zwischen 0-50 ug Konzentration gegen das Wachstum von Tumorzelllinien (menschliche Leberkrebs HEPG2 und Kolonkarzinom HCT), verglichen mit einem Standard-Medikament.

RESIN MOLDED ARTICLE WITH SLOW DELIVERY AND PROCEDURE FOR YOUR PRODUCTION

CARBOCYCLI HYDRAZINO HEMMER OF CUPREOUS AMINOXIDASEN

Procedure for the production of new 1-Phenyl-3-hydroxy-3-methyl-triazene

USE FROM FUMARIC ACID DERIVATIVES TO THE TREATMENT OF MITOCHONDRIALER DISEASES

SUBSTITUTED CHALKONE AS DRUGS

N, N' TO (SULPHONYL) HYDRAZINE the WHEN of ANTI-EOP READING TABLES MEANS USEFUL ARE

PHARMACEUTICAL COMPOSITION OF SULINDAC AND TROMETHAMINE OR SODIUM BICARBONATE

Pharmaceutical combinations comprising mebendazole and a strong or moderate CYP1A2 inhibitor

The invention relates to a pharmaceutical composition comprising mebendazole and a strong or moderate cytochrome P ...

COMPOSITIONS AND METHODS FOR SELECTIVE DELIVERY OF OLIGONUCLEOTIDE MOLECULES TO SPECIFIC NEURON TYPES

The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or 5 reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a neurotransmitter transporter. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the 10 cells for diagnostic purposes.

MATERIALS AND METHODS FOR CONTROLLING INFECTIONS

The subject invention provides materials methods for reducing infections in subjects. The materials methods utilize chlorhexidine, which has been found to be surprisingly non-toxic. The lack of toxicity facilitates the use of chlorhexidine in contexts that were not previously thought to 5 be possible.

The Combination of a Serotonin Reuptake Inhibitor and a 5-HT2C Antagonist, Inverse Agonist or Partial Agonist

Combination of a long-acting hypnotic agent and a short-acting hypnotic agent and therapeutic use of same

Novel combinations comprising a phosphodiesterase-5 inhibitor and their use

The invention relates generally to novel pharmaceutical compositions and methods for the treatment of various conditions, disorders, and diseases, and more particularly relates to the treatment of such conditions, disorders, and diseases using therapeutic agents that include a phosphodiesterase-5 inhibitor (PI-5) in combination with one or more agents.

Substituted catechols as inhibitors of IL-4 and IL-5 for the treatment bronchial asthma

The present invention relates to compounds of general formula 1 for the treatment of bronchial asthma by inhibition of IL-4 or IL-5 pathway inhibition. The present invention also relates to the use of compound of general formula 1 for the treatment of bronchial by inhibition of IL-4 or IL-5 pathway. The present invention also relates to the method of treating asthma by inhibition of IL-4 or IL-5 pathway by administration of compound or said composition through oral, intranasal, route or by inhalation to a mammal in need thereof. Compound of general formula 1 may be used for reducing perivascular and peribronchial inflammation.

FLUORINATED DIAMINES

Novel formulations of alpha-2,4-disulfophenyl-n-tert-butylnitrone

Use of aryl nitrone compounds in methods for treating neuropathic pain

Lipids comprising an aminoxy group

METHOD OF TREATMENT OF HYPERTENSION USING SELECTIVE SEROTONIN RE-UPTAKE INHIBITORS (SSRIs)

Applications of substituent benzyloxy group containing ether compounds for preparing antitumor drugs

Disclosed are applications of substituent benzyloxy group containing ether compounds represented by general formula I for preparing antitumor drugs. The definitions of the substituent groups in the formula are provided in the specification. The compounds having general formula I have desirable antitumor activity, particularly, and have excellent activity against leukemia strain HL-60, lung cancer A549, H157, H460, H520, bladder cancer T24,J82, prostate cancer LNCap, PC-3, rectal cancer HCT8,HCT116,RkO, and the like.

Treatment of circadian rhythm disorders

Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

PDE10 inhibitors and related compositions and methods

Materials and methods for controlling infections

The subject invention provides materials methods for reducing infections in subjects. The materials methods utilize chlorhexidine, which has been found to be surprisingly non-toxic. The lack of toxicity facilitates the use of chlorhexidine in contexts that were not previously thought to be possible.

Use of nitric oxide-releasing compounds as hypoxic cell radiation sensitizers

Use of spin trapping for the treatment of diseases associated with oxidation of lipids and proteins

FLUORINATED DIAMINES

TREATMENT OF CIRCADIAN RHYTHM DISORDERS

Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Method and compositions for inhibition of disorders associated with oxidative damage

Treatment of mood/affective disorders by glutamatergic upmodulators

I_h-modulators

PROPENONE-THIENYL AND CHALCONE DERIVATIVES

Method and compositions for inhibition of disorders associated with oxidative damage

2-P-NITRO- OR P-CHLOROBENZAMIDOACETOHYDROXAMIC ACID

METHODS FOR ALTERING INSULIN SECRETION

Modulation of the activity of glucocorticoid inducible kinase SGK1 in pancreatic islet cells restores insulin release. Also disclosed are methods and compounds useful for the treatment of glucocorticoid induced diabetes mellitus type-2.

PROCESS FOR PREPARING (3,4-DICHLOROPHENYL-SULPHINYL)- ACETAMIDOXIME AND ITS ADDITION SALTS

HYDROXYLAMINE COMPOUNDS AND METHODS OF THEIR USE

The present disclosure provides compounds that include hydroxylamines of formula (I) or (II), pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical com positions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain o ther ophthalmic conditions, inflammation, arthritis, and related diseases an d for the inhibition of complement activation.

FILM PREPARATION WITH RAPIDLY DISSOLVING PROPERTY AND FLEXIBILITY

A medicinal film preparation which reconciles rapidly dissolving properties with flexibility. The medicinal film preparation is characterized by comprising: an active-ingredient-containing layer comprising an active ingredient, a water-soluble polymer selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methyl cellulose, and a disintegrator; and an active-ingredient-free layer comprising methyl cellulose and/or hydroxypropyl methyl cellulose. It is further characterized in that the amount of the active ingredient is 0.1-75.0 mass% based on the whole medicinal film preparation and the sum of the active ingredient and the water-soluble polymer in the active-ingredient-containing layer is 15.0-95.0 mass% based on the whole active-ingredient-containing layer.

COMPOSITIONS FOR CONTINUOUS ADMINISTRATION OF DOPA DECARBOXYLASE INHIBITORS

Disclosed herein are arginine salts of carbidopa and levodopa and compositions that include for example the argi-nine salt of carbidopa suitable for continuous administration for treating neurological or movement diseases or disorders such as restless leg syndrome, Parkinson's disease, secondary parkinsonism, Huntington's disease, Parkinson's-like syndrome, PSP, MSA, ALS, Shy-Drager syndrome and conditions resulting from brain injury including carbon monoxide or manganese intoxication, to-gether with administration of levodopa ...

TRPA1 ANTAGONISTS

Compounds of formula (I), wherein R1, R2, R3, m, and Y are defined in the specification are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

NOVEL COMPOSITIONS FOR PREVENTING AND/OR TREATING LYSOSOMAL STORAGE DISORDERS

The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.

COMPOSITIONS AND METHODS RELATED TO HEART FAILURE

THERAPEUTIC DRUG FOR DIABETES

A medicine for the prevention of and/or treatments for diabetes or complications of diabetes, which contains as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I): (I) [wherein X represents a connecting group in which the main chain has 2 to 5 atoms (the group has been optionally substituted); A represents hydrogen or acetyl; E represents optionally substituted aryl or optionally substituted heteroaryl; and ring Z represents either arene which may have one or more substituents besides the groups represented by the formula -O-A (wherein A has the same meaning as defined above) and the formula -X-E (wherein X and E have the same meanings as defined above) or heteroarene which may have one or more substituents besides the groups represented by the formula -O-A (wherein A has the same meaning as defined above) and the formula -X-E (wherein X and E have the same meanings as defined above)], pharmacologically acceptable ...

PROPOFOL ANALOGS, PROCESS FOR THEIR PREPARATION, AND METHODS OF USE

The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.

ACETOXIME DERIVATIVES AND PROCESS FOR PREPARING THE SAME

PHARMACEUTICAL COMBINATIONS COMPRISING MEBENDAZOLE AND A STRONG OR MODERATE CYP1A2 INHIBITOR

The invention relates to a pharmaceutical composition comprising mebendazole and a strong or moderate cytochrome P450 1A2isoenzyme (CYP1A2) inhibitor, preferably fluvoxamine, thiabendazole or furafylline.

FORMULATIONS OF TEGAVIVINT AND RELATED COMPOUNDS

Formulations of tegavivint and related compounds, methods of making such formulations and methods of treating various conditions utilizing such formulations.

NEW POLYIMINO KETOALDEHYDES

The compounds with the general formula (I) are disclosed where n1 is the number of carbon atoms connected to nitrogen atom by a double bond and can take on values between 25 and 41, and where n2 is the number of -CH2- groups and can take on values between 15 and 23, as well as their biologically acceptable salts and solvates.

ALCOYLAMINOALCOHOL ETHER-OXIDE AND ETHER-OXIMES USED AS DRUGS, NOVEL PRODUCTS AND PREPARATION PROCESS

METHODS USING HYDRALAZINE COMPOUNDS AND ISOSORBIDE DINITRATE OR ISOSORBIDE MONONITRATE

CCR5 ANTAGONISTS AS PROPHYLACTICS FOR PREVENTING HIV INFECTION AND METHODS OF INHIBITING TRANSMISSION OF SAME

Topical cream, ointment, lotion, gel, foam formulations and slow release formulations or devices are provided including certain CCR5 antagonists as prophylactics for the prevention, retardation or inhibition of transmission of Human Immunodeficiency Virus (HIV) infection from one human to another.

CCR5 ANTAGONISTS AS PROPHYLACTICS FOR PREVENTING HIV INFECTION AND METHODS OF INHIBITING TRANSMISSION OF SAME

Topical cream, ointment, lotion, gel, foam formulations and slow release formulations or devices are provided including certain CCR5 antagonists as prophylactics for the prevention, retardation or inhibition of transmission of Human Immunodeficiency Virus (HIV) infection from one human to another.

TOXICITY-REDUCING NITRONE ADJUVANTS FOR DOXORUBICIN AND USE OF THE SAME

Methods are provided for using doxorubicin active agents in which reduced host toxicity is observed. Aspects of the methods including administering to a subject an effective amount of a doxorubicin active agent in conjunction with a doxorubicin toxicity-reducing adjuvant, e.g., a nitrone compound, or a nitrone compound in combination with a bisdioxopiperazine compound. Also provided are compositions for use in practicing the subject methods. The methods and compositions find use in a variety of different applications, including in the treatment of a variety of different disease conditions. (see above formula) ...

PREVENTIVE OR THERAPEUTIC AGENT FOR PAIN ASSOCIATED WITH HERPES ZOSTER IN ACUTE PHASE

A P2X4 receptor antagonist such as paroxetine, a di-azepinedione derivative having the following formula (IX) is used as an agent for preventing or treating zoster-associated pain in acute phase: wherein R1 is hydrogen, a C1-8 alkyl group, or the like; each of R2 and R3 is hydrogen, a C1-8 alkyl group, or the like; each of R4 and R5 is hydrogen or the like; and W is a five-membered or six-membered heterocyclic ring optionally having one or more substituents and comprising one to four nitrogen atoms as the members of the ring.

SUBSTITUTED CATECHOLS AS INHIBITORS OF IL-4 AND IL-5 FOR THE TREATMENT BRONCHIAL ASTHMA

The present invention relates to compounds of general formula 1 for the treatment of bronchial asthma by inhibition of IL-4 or IL-5 pathway inhibition. The present invention also relates to the use of compound of general formula 1 for the treatment of bronchial by inhibition of IL-4 or IL-5 pathway. The present invention also relates to the method of treating asthma by inhibition of IL-4 or IL-5 pathway by administration of compound or said composition through oral, intranasal, route or by inhalation to a mammal in need thereof. Compound of general formula 1 may be used for reducing perivascular and peribronchial inflammation.

METHODS FOR TREATMENT OF DISEASES AND DISORDERS RELATED TO TRANSDUCIN .BETA.-LIKE PROTEIN 1 (TBL1) ACTIVITY, INCLUDING MYELOPROLIFERATIVE NEOPLASIA AND CHRONIC MYELOID LEUKEMIA.

The present invention discloses utilization of the anthracene-9,10-dione dioxime compound: 2-((3R,5S)-3,5-dimethylpiperdin-1ylsulfonyl)-7-((3S,5R)-3, 5-dimethylpiperidin-1-ylsulfonyl)anthracene-9,10-dione dioxime for the treatment of cancer, including myeloproliferative neoplasia, chronic myeloid leukemia and acute myeloid leukemia. Such an anthracene- 9,10-dione dioxime compound interrupts the Wnt/beta-catenin pathway and inhibits the deregulated activity of this pathway for the treatment, diagnosis and prevention of beta-catenin pathway-related disorders, as well as disrupting transducin beta-like protein 1 (TBL1) interaction with the coactivator molecule beta-catenin.

TREATMENT OF CIRCADIAN RHYTHM DISORDERS

Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

METHODS AND COMP0STIONS FOR TREATMENT OF DEMYELINATING DISEASES

Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.

Tablet formulation

The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.

Modified release formulations containing drug-ion exchange resin complexes

A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

Sphingo-guanidines and their use as inhibitors of sphingosine kinase

The presently disclosed subject matter provides compounds of the formula: (1) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limit cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.

Transdermal Preparation

Provided is a transdermal preparation, which is capable of long-term (1-day to 7-day) release of a basic drug from a preparation, continuously and at a consistent concentration; shows little reduction over time in the drug content, even if multiple drugs are contained in the preparation; and is produced by a simple process. The transdermal preparation comprises a substrate, and an adhesive layer containing a basic drug and a water-soluble polymer.

Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) an antidiabetic compound for use in the treatment of proliferative diseases

The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.

Therapeutic approaches for treating alzheimer disease and related disorders through a modulation of cell stress response

The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate cell stress response for treating said disease.

Method For Improved Bioactivation Of Pharmaceuticals

This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R 1 and R 2 are hydrogen, alkyl, or aryl radicals.

Methods of treating cancer with phenformin

Methods of using phenformin to treat certain types of cancers are described.

Inhibitors of anaphase promoting complex activity

The invention provides an anti-proliferative composition comprising a non-peptide analog of the C-terminal isoleucine-arginine (IR) tail motif of an activator of an anaphase promoting complex (APC). The invention further provides methods of inhibing the ubiquitination activity of the APC by administering compositions of the invention.

Diagnosis of restenosis in patients undergoing percutaneous coronary intervention

The present invention relates to compounds, compositions, methods and/or kits for determining and/or predicting and/or diagnosing and/or treating restenosis in a patient.

Pentamidine combinations for treating cancer

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

Pharmaceutical co-crystals of quercetin

Disclosed herein is synergistic pharmaceutical co-crystals composition comprising Quercetin and an antidiabetic agent(s) as combination drug that have unique physical properties and biological activity which differ from the active agent in pure form. The invention further discloses process for preparation of the same and pharmaceutical compositions comprising these synergistic co-crystals.

Compositions and methods relating to proliferative diseases

Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

Methods and compositions for increasing the anaerobic working capacity in tissues

Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

PREVENTING ISLET INFLAMMATION AND DYSFUNCTION AND MAINTAINING PROPER GLUCOSE LEVELS BY CONTROLLING eIF5A AND ITS HYPUSINATION

Pancreatic islet dysfunction, in both type 1 and type 2 diabetes results, in part, from cytokine-mediated inflammation leading to iNOS generation and the death of pancreatic islets. The production of pro-inflammatory cytokines involved in the generation of iNOS is facilitated by the availability of the hypusine-containing translational factor eIF5A, necessary for the maturation of antigen-presenting cells. Treatment with agents capable of interfering with the mRNA translating iNOS or with agents that can interfere with the hypusination of eIF5A, prevents the death of islets, lowers blood glucose levels, avoids insulin resistance, and generally avoids the inflammatory response in islets associated with type 1 and type 2 diabetes.

Treatment of Psoriasis Using Oral Dosage Forms of Nitrone Spin Traps

Psoriasis is treated by oral administration of a pharmaceutical composition containing a nitrone spin trap such as α-phenyl t-butyl nitrone (PBN) and derivatives thereof. Preferred compositions and method of treatments further comprise at least one adjunct ingredient including fatty acid esters of ascorbic acid such as ascorbyl palmitate and ascorbyl stearate. The pharmaceutical composition can be prepared as an immediate release formulation or controlled released formulations.

Floating microgranules

A floating granule having a solid core, on which an active ingredient is supported, and a compound capable of generating a gas discharge which is constituted by an alkaline agent, characterised in that it does not comprise an acid agent that is capable of generating a gas discharge.

2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations

The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:

Compositions For The Treatment of Central Nervous System Disorders Including Depression Employing Novel Drug Combination Therapy To Reduce Suicidality In Patients

Described herein are novel methods and formulations for reducing suicidality in human subjects. Such formulations and methods are a combination of lithium and one or more other CNS therapeutic agents such as anti-depressant, mood-stabilizing, anxiolytic, anticonvulsant, antipsychotic, anti-addictive, and appetite suppressant drugs.

Lipid depot formulations

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Use of inhibitors of scavenger receptor class proteins for the treatment of infectious diseases

The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.

Methods and compositions for the induction of hypothermia

Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time. Using the two phase delivery method of the invention, the composition may comprise ethanol and, optionally, at least one of a vasoactive compound, an antiarrhythmic compound, a serotonin 5-HT3 receptor antagonist, an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. This two phase delivery method can be used to deliver any of the compositions of the invention and provides significant benefits to a patient.

Bilayer tablet formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Wound dressing

The invention relates to a sterile wound dressing having a backing and a nonabsorbent elastomer wound contact layer, wherein the elastomer matrix is formed by a synthetic three-block elastomer, preferably a copolymer of polystyrene block and polyolefin block (SEPS, SEBS, SEEPS, etc.) or mixtures thereof, wherein the total polymer content is less than 3.2 wt %, in particular 3.0 wt % or less, preferably 2.6 wt % or less, and is plasticized by an apolar oil and/or petroleum jelly.

Antiprotozoal compound derived from coelenterata

The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R 1 represents R 10 — of formula (4) or R 20 — of formula (5); R 2 represents CHO—, etc.; R 3 represents a hydrogen atom, CH 3 —C(═O)—, etc.; R 4 represents a hydrogen atom, CH 3 —C(═O)—, etc.; each of R 11 and R 12 independently represents each a hydrogen atom, a methyl group, etc.; R 13 represents —CH 2 —, —CH(—OH)— or —C(═O)—; each of R 21 and R 22 independently represents eaeh a hydrogen atom, a methyl group, etc.; R 23 represents —CH 2 —, —CH(—OH)— or —C(═0)—; and R 24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.

Pharmaceutical combination for use in inducing weight loss in diabetes type 2 patients or/and for preventing weight gain in diabetes type 2 patients

The present invention refers to a pharmaceutical combination for use in inducing weight loss in diabetes type 2 patients or/and for preventing weight gain in diabetes type 2 patients.

Compositions, uses and methods for treatment of metabolic disorders and diseases

The invention relates to variants and fusions of fibroblast growth factor 19 (FGF19), variants and fusions of fibroblast growth factor 21 (FGF21), fusions of fibroblast growth factor 19 (FGF19) and/or fibroblast growth factor 21 (FGF21), and variants or fusions of fibroblast growth factor 19 (FGF19) and/or fibroblast growth factor 21 (FGF21) proteins and peptide sequences (and peptidomimetics), having one or more activities, such as glucose lowering activity, and methods for and uses in treatment of hyperglycemia and other disorders.

Bile Acid Recycling Inhibitors for Treatment of Pancreatitis

Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.

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.

Calixarene-Based Peptide Conformation Mimetics, Methods of Use, and Methods of Making

A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Cytostatic drug composition

A drug composition containing as a drug substance a polymeric guanidine derivative based on a diamine containing oxyalkylene chains between two amino groups, with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyalkylene chains between two amino groups, as well as the pharmaceutically acceptable salts thereof.

Neuroprotective modulation of nmda receptor subtype activities

In various aspects, the invention provides methods and compositions for modulating NMDA receptor subtype activity, to enhance NR2A-containing NMDA receptor activity relative to NR2B-containing NMDA receptor activity, so as to effect a neuroprotective reduction in excitotoxic NMDA receptor activity

Diazeniumdiolate cyclopentyl derivatives

A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, —OH, —O—C 1-6 alkyl, ═O, or halogen; R 2 is hydrogen, C(O)OR 8 , C 6 H 5 C(O)OR 8 , (CH 2 ) 1-2 OH, CR 9 R 10 OH, C(O)O(CH 2 ) 0-2 aryl, C(O)NR 9 R 10 , C(O)SO 2 NR 9 R 10 , C 6 H 5 OR 9 , W—C(O)OR 8 , W—OR 9 , Y, or P(O)(OR 9 )(ORlO); R 3 is hydrogen or —C 1-6 alkyl; R 4 is hydrogen, —OH or —C(O)OR 9 ; R 5 is hydrogen or deuterium; R 6 and R 7 are independently —C 1-6 alkyl, fluoro-substituted —C 1-6 alkyl, deutero-substituted —C 1-6 alkyl or —(CH 2 ) 1-2 R 11 , wherein any carbon atom of the fluoro-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro; R 8 , in each instance in which it occurs, is independently hydrogen, —C 1-6 alkyl, or —(CH 2 ) 2 N + (CH 3 ) 3 ; R 9 and R 10 , in each instance in which they occur, are independently —C 1-6 alkyl; R 11 is —OH, —O—C 1-6 alkyl, -0CD3, —OC(O)OC 1-6 alkyl, —NH 2 , —C 6 H 5 , —N 3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R 6 or R 7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.

ANTIMICROBIAL COMPOSITIONS

Antimicrobial compositions are provided that include a hydroalcoholic solvent system comprising a lower C-Calcohol and water; a cationic antimicrobial agent such as chlorhexidine gluconate; a fatty component containing at least one free hydroxyl group, such as a C-Cfatty alcohol, a C-Cfatty ester, a C-Cfatty ether, a C-Cfatty amide, and combinations thereof; and optionally an emollient ester such as diesters of bibasic acids and trimesters of citric acid. The compositions described herein display improved antimicrobial efficacy and improved cosmetic elegance. Methods of using the antimicrobial compositions are provided. 1. A method of improving the wet adhesion of medical adhesive article , comprising applying a composition comprising:{'sub': 2', '5, 'a) a C-Clower alcohol present in an amount of at least 35 wt-%;'}{'sub': 12', '21', '12', '21', '12', '21, 'b) a fatty component containing one or more free hydroxyl groups selected from the group consisting of C-Cfatty alcohols, C-Cfatty ethers, C-Cfatty amides, and combinations of all of the foregoing; wherein the fatty component is present in the composition in an amount of at least 2 wt-%; and'}c) a cationic antimicrobial agent present in an amount of at least 0.5 wt-% based upon the total weight of the antimicrobial composition; and wherein the fatty component and the cationic antimicrobial are dissolved in the antimicrobial composition, and the antimicrobial composition is a solution;', 'wherein the antimicrobial composition is free of surfactants with an HLB greater than 6;', 'wherein if any component of the composition is ethoxylated, no more than two moles of ethylene oxide are included; and', 'wherein the antimicrobial composition is essentially free of hydrophilic polymers; and, 'd) water, wherein the lower alcohol to water weight ratio is between 40:60 to 95:5;'}applying a medical adhesive article over the composition;2. A method of improving the wet adhesion of medical adhesive article , comprising ...

Vaccines comprising cholesterol and cpg as sole adjuvant-carrier molecules

Described are vaccines having one or more antigens cholesterol and CpG. Aspects of the invention relate to the use of the vaccines of the invention for the treatment and/or prevention of human and animal disorders.

PREVENTION OF HYPOGLYCEMIA IN DIABETES MELLITUS TYPE 2 PATIENTS

A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering 1. A method for the prevention of hypoglycaemia in diabetes mellitus type 2 comprising administering{'sup': '36', 'sub': 6', '2, '(a) desProExendin-4(1-39)-Lys-NHor/and a pharmaceutically acceptable salt thereof, and'}(b) metformin or/and a pharmaceutically acceptable salt thereof,to a subject in need thereof.2. The method of claim 1 , wherein desProExendin-4(1-39)-Lys-NHor/and a pharmaceutically acceptable salt thereof is administered subcutaneously.3. The method of claim 1 , wherein the metformin is administered orally.4. The method of claim 1 , wherein desProExendin-4(1-39)-Lys-NHor/and a pharmaceutically acceptable salt is administered in an add-on therapy to administration of metformin.5. The method of claim 1 , wherein the subject to be treated is obese.6. The method of claim 5 , wherein the subject has a body mass index of at least 30.7. The method of claim 1 , wherein the subject to be treated is an adult subject.8. The method of claim 1 , wherein diabetes mellitus type 2 is not adequately controlled with metformin alone.9. The method of claim 8 , wherein treatment with a dose of at least 1.5 g/day metformin alone for three months does not adequately control diabetes mellitus type 2.10. The method of claim 1 , wherein the subject to be treated has a HbA1c value in the range of 7% to 10%.11. The method of claim 1 , wherein the hypoglycaemia is associated with a plasma glucose concentration of below 60 mg/dL.12. The method of claim 1 , wherein the hypoglycaemia is a symptomatic hypoglycaemia.13. The method of claim 12 , wherein the symptomatic hypoglycaemia is associated with at least one symptom selected from sweating claim 12 , palpitations claim 12 , hunger claim 12 , restlessness claim 12 , anxiety claim 12 , fatigue claim 12 , irritability claim 12 , headache claim 12 , loss of concentration claim 12 , somnolence claim 12 , psychiatric disorders claim 12 , ...

Novel synergistic pharmaceutical composition for topical applications

A synergistic pharmaceutical composition for the preparation of topical formulations for use in prophylaxis and treatment of wounds, burn wounds, skin grafts, pressure ulcers, diabetic foot ulcers and other skin diseases is provided. The composition may include one or more synergistically active ingredients and one or more inactive ingredients. The synergistically active ingredients may include Recombinant Human Epidermal Growth Factor (rh-EGF) (REGEN-D™ of Bharat Biotech International Limited) and/or Platelet Derived Growth Factor (rh-PDGF-BB), silver sulfadiazine (SSD) and chlorhexidine gluconate (CHG). One or more inactive ingredients may comprise carriers, preservatives, emulsifiers, skin emollients and soothers and one or more other constituents.

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 ...

Methods and compositions comprising ampk activator (metformin/troglitazone) for the treatment of myotonic dystrophy type 1 (dm1)

The present invention relates to methods and compositions for the treatment of Myotonic Dystrophy type 1 (DM1) with an AMPK activator <eq.metformin or troglizazone>.

Biguanide Compositions and Methods of Treating Metabolic Disorders

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 2. A composition according to claim 1 , wherein{'sub': 2', '3', '4', '5', '6', '7, 'R, R, R, R, Rand Rare independently selected from H, methyl, ethyl, propyl or isopropyl; and'}{'sub': '1', 'Ris selected fromH,{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkenyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 1', '12', '2, 'Cto Cstraight chain or branched chain alkynyl optionally hetero substituted with oxygen, silicon, sulphur or optionally substituted with OH, O-alkyl, SH, S-alkyl, NH, NH-alkyl,'}{'sub': 3', '7', '2', '6, 'Cto Ccycloalkyl, Cto Cheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N,'}{'sub': 4', '12, 'Cto Calkylcycloalkyl,'}{'sub': 3', '11, 'Cto Calkylheterocycloalkyl, where the heterocycle comprises one or two hetero atoms selected from O, S, or N and wherein N is present in the heterocyclic ring, the nitrogen atom may be in the form of an amide, carbamate or urea,'}phenyl, substituted phenyl, naphthyl, substituted naphthyl,alkylphenyl, alkylsubstituted phenyl, alkylnaphthyl, alkylsubstituted naphthyl,pyridyl, furanyl, thiophenyl, pyrrollyl, oxazolyl, isoxazolyl, thiazolyl, diazolyl, pyrazolyl ...

Compositions and methods for enhancing drug delivery across and into ocular tissues

This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

USE OF INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS AND NITRIC OXIDE SCAVENGERS TO INHIBIT POST-TRAUMATIC IMMUNODEPRESSION

The present invention relates to methods and compositions that inhibit the effects of nitric oxide for inhibiting post-traumatic immunodepression. It is based, at least in part, on the discovery that, in a murine model system of trauma, genetic or chemical reduction of nitric oxide inhibited the development of immunodepression. Accordingly, the present invention provides for methods and compositions to be administered to subjects, post-trauma, that inhibit the effects of nitric oxide by inhibiting inducible nitric oxide synthase (iNOS) and/or scavenge nitric oxide. 1. A method of inhibiting post-trauma immunodepression in a subject who has suffered a traumatic injury , comprising administering , to the subject , an effective amount of an agent that inhibits the effects of nitric oxide.2. The method of claim 1 , wherein the agent is a nitric oxide scavenger.3. The method of claim 2 , wherein the nitric oxide scavenger comprises a dithiocarbamate compound.4. The method of claim 1 , wherein the agent is NOX-100.5. The method of claim 1 , wherein the agent inhibits inducible nitric oxide synthase.6. The method of claim 1 , wherein the agent is N-(3-(aminomethyl)benzyl)acetamidine.7. A method for inhibiting a decrease in cell-mediated immunity in a subject who has suffered a traumatic injury claim 1 , comprising administering claim 1 , to the subject claim 1 , an effective amount of an agent that inhibits the effects of nitric oxide.8. The method of claim 7 , wherein the agent is a nitric oxide scavenger.9. The method of claim 8 , wherein the nitric oxide scavenger comprises a dithiocarbamate compound.10. The method of claim 7 , wherein the agent is NOX-100.11. The method of claim 7 , wherein the agent inhibits inducible nitric oxide synthase.12. The method of wherein the agent is N-(3-(aminomethyl)benzyl)acetamidine.13. A method for reducing the risk of infection in a subject who has suffered a traumatic injury claim 7 , comprising administering claim 7 , to the subject ...

Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. 1. A method for treating or ameliorating hypercholemia comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the method comprises decreasing at least 20% of serum bile acid or hepatic bile acid levels in the patient.3. The method of claim 1 , wherein less than 10% of the ASBTI is systemically absorbed.5. The method of claim 4 , wherein:q is 1;n is 2;{'sup': 'x', 'sub': 3', '2, 'Ris N(CH);'}{'sup': 7', '8, 'Rand Rare independently H;'}{'sup': 1', '2, 'Rand Ris alkyl;'}{'sup': 3', '4, 'Ris H, and Ris OH;'}{'sup': 5', '6', '9', '9', '9', '9', '9, 'sub': 2', '3', 'Z', 'Z, 'claim-text': wherein z is 1, 2 or 3; each L is independently a substituted or unsubstituted alkyl, a substituted or unsubstituted heteroalkyl, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aminoalkyl group, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted cycloalkyl, or a substituted or unsubstituted heterocycloalkyl; each K is a moiety that prevents systemic absorption;', {'sup': 15', '13', '13', '14', '13', '14', '13', '13', '13', '13', '13', '14', '13', ...

Co-Therapy for Diabetic Conditions

Methods of treating diseases diabetes are disclosed. Methods of modulating elevated fructosamine levels, elevated HbA1c levels, impaired glucose tolerance, and impaired fasting glucose are also disclosed. In some embodiments, methods include co-administration of a biguanide and a bile acid sequestrant. Drug products including a biguanide and bile acid sequestrants in combination are also disclosed. 1. A method for treating diabetes in a human , the method comprising administering to a human in need thereof a pharmaceutically effective amount of a biguanide agent and a pharmaceutically effective amount of a bile acid sequestrant.2. The method of claim 1 , wherein the biguanide agent and the bile acid sequestrant are administered simultaneously.3. The method of claim 2 , wherein the bile acid sequestrant and the biguanide agent are administered in a single dosage form.4. The method of claim 1 , wherein the bile acid sequestrant and the biguanide agent are administered separately.5. The method of claim 4 , wherein the bile acid sequestrant and the biguanide agent are administered within one hour of each other.6. The method of claim 4 , wherein the bile acid sequestrant and the biguanide agent are administered within twelve hours of each other.7. The method of claim 1 , wherein the biguanide agent comprises metformin or a pharmaceutically acceptable salt thereof.8. The method of claim 7 , wherein the bile acid sequestrant comprises colesevelam or a pharmaceutically acceptable salt thereof.9. The method of claim 8 , wherein the salt form of colesevelam comprises colesevelam HCl and the salt form of metformin comprises metformin HCl.10. A method for modulating a condition in a subject claim 8 , the condition selected from the group consisting of elevated fructosamine levels claim 8 , elevated HbA1c levels claim 8 , impaired glucose tolerance claim 8 , and impaired fasting glucose comprising co-administering to a subject a bile acid sequestrant claim 8 , in free or ...

Anti-IL 1- ß Antibody Combination Therapy

The present invention relates to a new combination comprising a therapeutically effective amount of an anti-IL1β antibody or an antigen-binding fragment thereof and at least one anti-diabetic agent. The anti-diabetic agent can be selected from the group consisting of insulin signaling pathway modulators, such as inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), DPP-IV inhibitors, agents influencing a deregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, α-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and α-adrenergic antagonists, for simultaneous, separate or sequential use of the anti-IL-1β antibody or a antigen-binding fragment thereof and the at least one anti-diabetic agent, especially in the prevention, delay of progression or treatment of metabolic conditions mediated by IL1β such as conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis, in particular diabetes and specifically type 1 diabetes or type 2 diabetes mellitus. The invention also relates to pharmaceutical composition comprising the combination of the invention and methods of treatment using the combination for the prevention, delay of progression or treatment of metabolic conditions mediated by IL1β such as diabetes or improving the function of beta cell function. 1. A pharmaceutical combination comprising a therapeutically effective amount of an anti-IL1β monoclonal antibody or antigen binding fragment thereof and at least one anti- ...

Pharmaceutical Formulations Containing An SGLT2 Inhibitor

Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.

Pharmaceutical preparation for controlling water-soluble drug release

A solid formulation comprising a water-soluble drug and a hardly water-soluble pharmaceutically-acceptable solid substance, which comprises silicone as a carrier, wherein the silicone formulation can exhibit an excellent controlled-release of the water-soluble drug.

ACTIVATION OF AMP-PROTEIN ACTIVATED KINASE BY OXALOACETATE COMPOUNDS

The present invention relates to oxaloacetate compounds that activate AMP-activated protein kinase (AMPK), including the preparation of the compounds, compositions containing the compounds, preserving said compounds and the use of the compounds in the prevention or treatment of disorders such as diabetes, metabolic syndrome, obesity, cardiovascular disease, Alzheimer's disease, and cancer. 1. A method of activating AMPK , comprising an effective amount of a compound such as oxaloacetate , oxaloacetic acid , an oxaloacetate salt , alpha-ketoglutarate or aspartate as an active ingredient.2. The method of claim 1 , wherein said compound is administered orally.3. The method of claim 1 , wherein said compound is formulated with a buffer.4. The method of claim 1 , wherein said organism is a mammal.5. The method of claim 4 , wherein said mammal is a human.6. The method of claim 1 , wherein said compound is topically administered.7. The method of claim 1 , wherein said compound is administered parenterally.8. The method of claim 1 , wherein said compound is administered in a biphasic delivery system.9. The method of claim 1 , wherein said AMPK activation also beneficially activates lipid metabolism.10. The method of wherein said AMPK activation is an obesity suppressing agent.11. The method of claim 1 , wherein said AMPK activation is a diabetes preventing/ameliorating agent.12. The method of claim 1 , wherein said AMPK activation is a hepatic hypertrophy suppressing agent.13. The method of wherein said AMPK activation is a fatty liver suppressing agent.14. The method of wherein said AMPK activation increases mitochondrial density.15. The method of wherein said AMPK activation reduces the risk of cancer.16. The method of wherein said AMPK activation has beneficial effect on cancer prevention or treatment.17. The method of wherein said AMPK activation acts as an exercise-substitutive agent.18. The method of wherein said AMPK activation increases athletic performance.19. The ...

ANTI-VIRAL CARBAMIMIDOTHIOIC ACID ESTERS

Carbamimidothioic acid esters of formula (I) and 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide are used for the treatment of influenza, and for the inhibition of a viral RNA-dependent RNA polymerase. Formulae (I), (II). 3. The compound according to claim 1 , consisting of a compound shown in Table 2.4. A pharmaceutical composition comprising the compound of claim 1 , in admixture with a suitable pharmaceutically acceptable diluent or carrier.5. The pharmaceutical composition of claim 4 , in admixture with a medication for the treatment of influenza.6. The pharmaceutical composition of claim 5 , wherein the medication for the treatment of influenza is oseltamivir claim 5 , zanamivir claim 5 , amantadine claim 5 , or rimantadine.7. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering the compound of to a patient.8. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester or a pharmaceutically acceptable salt claim 1 , solvent claim 1 , or hydrate thereof to a patient.9. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester claim 1 , dihydrobromide or 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide to a patient.10. The method according to claim 8 , wherein the influenza is influenza A.11. The method according to claim 8 , wherein the influenza is influenza type B or C.12. The method according to claim 10 , wherein the influenza is type A group-1.13. The method according to claim 10 , wherein the influenza is type A group-2.14. The method according to claim 10 , wherein the influenza is H1N1 claim 10 , H1N2 claim 10 , H3N2 claim 10 , H5N1 claim 10 , H9N2 claim 10 , H7N3 claim 10 , or H7N7.15. The method according to claim 8 , for treatment or prophylaxis ...

COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING METABOLIC SYNDROME AND RELATED DISEASES AND DISORDERS

Disclosed herein are novel compositions and methods for treating or preventing metabolic syndromes. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a combination of at least one antidiabetic agent, at least one proton pump inhibitor and at least one bile acid sequestrant, and, optionally, at least one active agent, including, but not limited to, dyslipidemia agents, histamine Hreceptor blockers, antacids, γ-aminobutyricacid-b (GABA-B) agonists, prodrugs of GABA-B agonists, protease inhibitors and combinations of two or more thereof. 1. A composition comprising a therapeutically effective amount of at least one antidiabetic agent , at least one proton pump inhibitor and at least one bile acid sequestrant.2. A composition according to claim 1 , further comprising a pharmaceutically acceptable excipient claim 1 , diluent claim 1 , or carrier.3. A composition according to claim 1 , wherein the at least one antidiabetic agent is chosen from a thiazolidinedione claim 1 , a sulfonylurea compound claim 1 , a biguanide claim 1 , a meglitinide claim 1 , an alpha-glucosidase inhibitor and a DPP-4 inhibitor.49-. (canceled)10. A composition according to claim 1 , wherein the at least one proton pump inhibitor is chosen from omeprazole claim 1 , esomeprazole claim 1 , lansoprazole claim 1 , pantoprazole claim 1 , rabeprazole claim 1 , tenatoprazole claim 1 , leminoprazole claim 1 , dontoprazole claim 1 , and ransoprazole.11. A composition according to claim 1 , wherein the at least one bile acid sequestrant is chosen from one or more of GT102-279 claim 1 , cholestyramine claim 1 , colesevelam claim 1 , colesevelam hydrochloride claim 1 , ursodeoxycholic acid claim 1 , colestipol claim 1 , colestilan claim 1 , sevelamer claim 1 , polydiallylamine cross-linked with epichlorohydrin claim 1 , dialkylaminoalkyl derivatives of a cross-linked dextran claim 1 , or N-(cycloalkyl) ...

TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE

The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrein, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive. 3. The method of claim 1 , wherein Ris COORpresent once and in meta or para position.4. The method of claim 1 , wherein Ris hydrogen.5. The method of claim 1 , wherein said compound is a salt selected from chloride claim 1 , bromide claim 1 , acetate claim 1 , trifluoroacetate claim 1 , and toluenesulfonate.6. The method of claim 1 , wherein said blood loss occurs in hyperfibrinolytic conditions.7. The method of claim 1 , wherein said compound claim 1 , or salt thereof claim 1 , is administered during a surgical operation.8. The method of claim 7 , wherein said surgical operation is a cardiac surgical procedure or an organ transplant.9. The method of claim 8 , wherein said cardiac surgical procedure includes cardiopulmonary bypass (CPB).11. The method of claim 10 , wherein said blood loss occurs in hyperfibrinolytic conditions.12. The method of claim 10 , wherein said compound claim 10 , or salt thereof claim 10 , is administered during a surgical operation.13. The method of claim 12 , wherein said surgical operation is a cardiac surgical procedure or an organ transplant.14. The method of claim 12 , wherein said cardiac surgical procedure includes cardiopulmonary bypass (CPB). This application is a continuation of U.S. patent application Ser. No. 13/471,007, filed on May 14, 2012, which is a continuation of U.S. patent application Ser. No. 12/429,766, filed on Apr. 24, 2009, now U.S. Pat. No. 8,207,378, which is a continuation-in-part of International Application No. PCT/EP2007/009220, filed Oct. 24, 2007, which claims benefit of German ...

TRANS-CLOMIPHENE FOR METABOLIC SYNDROME

The present invention relates to the administration of compositions comprising an antiestrogen, preferably trans-clomiphene, for treating metabolic syndrome in a subject. The invention is also directed to methods for reducing fasting glucose levels in a subject by administering a composition comprising an antiestrogen, preferably trans-clomiphene. 1. A method for preventing or treating type 2 diabetes in a hypogonadal human male with a body mass index greater than 26 , comprising administering to the male an effective amount of a composition comprising a selective estrogen receptor modulator (SERM).2. The method of claim 1 , wherein the composition comprises about 100% trans-clomiphene and about 0% cis-clomiphene or pharmaceutically acceptable salts thereof.3. The method of claim 2 , wherein the composition comprises about 12.5 to 50 mg trans-clomiphene.4. The method of claim 3 , wherein the composition comprises 12.5 claim 3 , 25 or 50 mg trans-clomiphene.5. The method of claim 2 , wherein the salt of trans-clomiphene is the citrate salt.6. The method of claim 1 , wherein the male has a fasting blood glucose level between 110 mg/dl and 125 mg/dl.7. The method of claim 1 , wherein metformin is simultaneously claim 1 , separately claim 1 , or sequentially co-administered with the composition. The present invention relates to compositions and methods for treating metabolic syndrome and conditions associated therewith. More specifically, the present invention relates to the use of compositions comprising clomiphene enriched for trans-clomiphene for treating metabolic syndrome and conditions associated therewith in subjects with low or low normal testosterone.Metabolic syndrome is characterized by a group of metabolic risk factors in one person including abdominal obesity, insulin resistance or glucose intolerance, atherogenic dyslipidemia, prothrombotic state, proinflammatory state and hypertension. The Adult Treatment Panel defines metabolic syndrome as present if a ...

Compositions and Methods of Treating Metabolic Disorders

Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine. 1. A method of improving the gastrointestinal tolerability of and/or reducing gastrointestinal complications resulting from biguanide administration , comprising administering a therapeutically effective amount of a biguanide compound in a delayed-release formulation to a patient in need thereof.2. A method of treating metabolic disorders in a patient in need thereof , comprising administering a therapeutically effective amount of a biguanide compound to said patient in a delayed-release formulation , wherein said patient has a contraindication for the biguanide compound.3. The method according to claim 2 , wherein the patient has a contraindication selected from the group consisting of a hypoxic condition claim 2 , impaired lactate clearance claim 2 , and impaired clearance of the biguanide compound.4. The method according to claim 3 , wherein the patient has a hypoxic condition.5. The method according to claim 3 , wherein the patient has impaired lactate clearance.6. The method according to claim 3 , wherein the patient has impaired clearance of the biguanide compound.7. The method according to claim 3 , wherein the patient has moderate renal impairment claim 3 , severe renal impairment claim 3 , or endstage renal disease which results in impaired clearance of the biguanide compound.8. The method according to claim 3 , wherein the patient has chronic kidney disease.9. The method according to any one of the preceding claims claim 3 , wherein the patient in need thereof has hyperglycemia.10. The method according to claim 9 , wherein the hyperglycemia is ...

Methods And Compositions For Treatment Of Lipogenic Virus Related Conditions

Disclosed are methods of treatment for adipogenic virus-related conditions. The methods may comprise administering a composition comprising an effective dose of an antiviral agent to a subject having an adipogenic adenovirus-related condition. Administration of the antiviral agent may prevent or reduce viral proliferation in the subject. The method may also include administering a composition comprising an effective dose of a therapeutic agent known to treat the adipogenic adenovirus-related condition in conjunction with the composition comprising an effective dose of an antiviral agent. Administration of the antiviral agent and the therapeutic agent may reduce or eliminate one or more symptoms of the adipogenic adenovirus-related condition more efficiently than administration of either the antiviral agent and the therapeutic agent alone. 1. A method for treating a lipogenic adenovirus-related condition comprising:a) identifying a subject infected with a lipogenic adenovirus and having a lipogenic adenovirus-related condition; andb) administering a composition comprising an effective dose of an antiviral agent to the subject thereby preventing or reducing lipogenic adenovirus proliferation and/or action or thereby reducing or eliminating one or more symptoms of the lipogenic adenovirus-related condition.2. The method of 1 , further comprising administering a composition comprising an effective dose of a therapeutic agent known to treat the lipogenic adenovirus-related condition in conjunction with the composition comprising an effective dose of an antiviral agent , wherein administration of the antiviral agent and the therapeutic agent reduce or eliminate one or more symptoms of the lipogenic adenovirus-related condition more efficiently than administration of either the antiviral agent or the therapeutic agent alone.3. The method of claim 1 , wherein the step of identifying a subject having a lipogenic adenovirus-related condition comprises at least one of:(i) ...

Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions

The present invention relates to substituted quinazolines of formula (I): 2. The compound of formula (I) according to claim 1 , in whichR1 and R2 are the same or different and are independently selected from 3-(R)-amino-piperidin-1-yl, (2-amino-2-methyl-propyl)-methylamino and (2-(S)-amino-propyl)-methylamino;or a tautomer, enantiomer, diastereomer, mixture or salt thereof.3. The compound of formula (I) according to claim 1 , in which X and Y are the same claim 1 , or a tautomer claim 1 , enantiomer claim 1 , diastereomer claim 1 , mixture or salt thereof.6. Physiologically acceptable salt of the compound according to with an inorganic or organic acid or base.7. Pharmaceutical composition containing a compound of formula (I) according to claim 1 , or a physiologically acceptable salt thereof with an inorganic or organic acid or base claim 1 , optionally together with one or more pharmaceutically acceptable excipients.8. Use of a compound according to for preparing a pharmaceutical composition which is suitable for treating type II diabetes mellitus or obesity.9. Process for preparing a pharmaceutical composition according to claim 7 , characterised in that the compound of formula (I) or a physiologically acceptable salt thereof with an inorganic or organic acid or base is incorporated in one or more pharmaceutically acceptable excipients.10. A method of treating or preventing type II diabetes mellitus or obesity claim 1 , the method comprising administering the compound according to claim 1 , and optionally one or more other active substances claim 1 , to a patient.11. The method according to claim 10 , wherein the one or more other active substances is selected from metformin claim 10 , metformin; sulphonylureas claim 10 , nateglinide claim 10 , repaglinide claim 10 , thiazolidinediones (e.g. pioglitazone) claim 10 , PPAR-gamma agonists claim 10 , alpha-glucosidase blockers claim 10 , insulin or insulin analogues claim 10 , and GLP-1 and GLP-1 analogues.12. ...

COMBINATION OF A PYRROLOQUINOLINE COMPOUND AND A BETA-LACTAM ANTIMICROBIAL AGENT, MUPIROCIN OR CHLORHEXIDINE

This invention relates to the use of 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof in combination with another antimicrobial agent selected from the group consisting of a beta-lactam antimicrobial agent, mupirocin and chlorhexidine or a pharmaceutically acceptable derivative thereof, for the prevention and/or treatment of microbial infections. 1. A combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 ,3-dihydro-1H-pyrrolo[3 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof and another antimicrobial agent selected from the group consisting of a beta-lactam antimicrobial agent , mupirocin and chlorhexidine or a pharmaceutically acceptable derivative thereof.2. A combination according to comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 claim 1 ,3-dihydro-1H-pyrrolo[3 claim 1 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof and a beta-lactam antimicrobial agent or a pharmaceutically acceptable derivative thereof.3. A combination according to wherein the beta-lactam antimicrobial agent is co-amoxiclay.4. A combination according to comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 claim 1 ,3-dihydro-1H-pyrrolo[3 claim 1 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof and mupirocin or a pharmaceutically acceptable derivative thereof.5. A combination according to comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 claim 1 ,3-dihydro-1H-pyrrolo[3 claim 1 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof and chlorhexidine or a pharmaceutically acceptable derivative thereof.6. A combination according to further comprising an aminoglycoside antimicrobial agent.7. A combination according to wherein the aminoglycoside is gentamicin claim 6 , neomycin or a pharmaceutically acceptable derivative thereof8. A combination according to for use in the prevention and/or treatment of a microbial infection.9. A combination ...

Novel NIDDM Regimen

The present invention relates to the use of a short-acting oral hypoglycemic agent and to a novel regimen in the treatment of type 2 diabetes in which the endogenous secretion of insulin is stimulated in connection with meals by administering in connection with the meals a short-acting oral hypoglycaemic agent. Also, the present invention relates to a method of achieving significantly improvement in the glycaemic control by a combined use of repaglinide and metformin in NIDDM patients poorly controlled on metformin alone.

METHODS AND USE OF COMPOUNDS THAT BIND TO HER2/NEU RECEPTOR COMPLEX

This application describes pharmaceutical compositions, kits, and methods for inhibiting cell proliferative disorders, especially those disorders characterized by overactivity and/or inappropriate activity of a receptor tyrosine kinase, including Her2 related cancers, and methods for imaging an Her-2 expressing tumor. 5. (canceled)6. The method of wherein the receptor is Her2.79-. (canceled)10. The method of wherein the cell proliferative disorder is cancer.11. The method of wherein the cell proliferative disorder affects a breast claim 1 , prostate claim 1 , lung claim 1 , pancreas claim 1 , ovary or stomach.12. (canceled)13. The method of wherein the patient is a human.14. The method of further comprising administering a pharmaceutically effective amount of an anti-cancer agent or performing a non-drug therapy or both to the patient.15. The method of wherein the compound of Formula (I) and the anti-cancer agent are administered at the same time.16. The method of wherein the non-drug therapy is surgery claim 14 , hypertensive chemotherapy claim 14 , genetherapy claim 14 , thermotherapy claim 14 , cryotherapy claim 14 , photodynamic therapy claim 14 , laser cauterization radiotherapy claim 14 , or a combination thereof.1749-. (canceled)5455-. (canceled)56. The composition of wherein the receptor is Her2.5759-. (canceled)60. The composition of wherein the cell proliferative disorder is cancer.61. The composition of wherein the cell proliferative disorder affects a breast claim 50 , prostate claim 50 , lung claim 50 , pancreas claim 50 , ovary claim 50 , or stomach.62. (canceled)63. The composition of wherein the patient is a human.6466-. (canceled)67. A commercial package comprising the pharmaceutical composition of or a pharmaceutically acceptable salt or prodrug thereof claim 50 , at least one anti-cancer agent claim 50 , and a written matter associated therewith claim 50 , the written matter stating that the pharmaceutical composition can or should be used for the ...

Modulation of nitric oxide signaling to normalize tumor vasculature

The instant invention provides methods for treating a solid tumor in a subject comprising modulating nitric oxide production in the tumor to normalize tumor vasculature and administering an anti-tumor therapy to the subject. The invention further provides methods of treating a solid tumor in a subject comprising selectively increasing cyclic guanosine monophosphate (cGMP) or cGMP dependent protein kinase G production in the tumor vasculature to an amount effective to normalize tumor vasculature and administering an anti-tumor therapy to the subject.

TREATMENT OF GENOTYPED DIABETIC PATIENTS WITH DPP-IV INHIBITORS SUCH AS LINAGLIPTIN

The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups. 113-. (canceled)14. Method for preventing , slowing the progression of , delaying or treating a metabolic disorder selected from the group consisting of type 1 diabetes mellitus , type 2 diabetes mellitus , impaired glucose tolerance , impaired fasting blood glucose , hyperglycemia , postprandial hyperglycemia , overweight , obesity and metabolic syndrome , orfor improving glycemic control and/or for reducing of fasting plasma glucose, of postprandial plasma glucose and/or of glycosylated hemoglobin HbA1c in a patient in need thereof, or for preventing, slowing, delaying or reversing progression from impaired glucose tolerance, impaired fasting blood glucose, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, orfor preventing, slowing the progression of, delaying or treating of a condition or disorder selected from the group consisting of complications of diabetes mellitus such as cataracts and micro- and macrovascular diseases, such as nephropathy, retinopathy, neuropathy, tissue ischaemia, diabetic foot, arteriosclerosis, myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, stroke, peripheral arterial occlusive disease, cardiomyopathy, heart failure, heart rhythm disorders and vascular restenosis, or for reducing body weight or preventing an increase in body weight or facilitating a reduction in body weight, orfor preventing, slowing, delaying or treating the degeneration of pancreatic beta cells and/or the decline of the functionality of pancreatic beta cells and/or for improving and/or restoring the functionality of pancreatic beta cells and/or restoring the functionality of pancreatic insulin secretion, orfor preventing, slowing, delaying or treating diseases or conditions attributed to an abnormal accumulation of liver fat, orfor maintaining ...

Compositions and Methods for Combinations of Oligoamines with 2-Difluoromethylornithine (DFMO)

The present invention is based on the seminal discovery of a synergistic effect for combinations of oligoamines with 2-difluoromethylornithine (DFMO) for treatment of cancer. The invention provides combinations of at least one inhibitor of a histone demethylase enzyme and at least one inhibitor of ornithine decarboxylase (ODC). The invention also provides methods for treatment of cancer using such combinations and methods for altering methylation in a cell using such combinations. The invention provides that certain silenced genes can be re-expressed using combinations disclosed herein.

PHARMACEUTICAL COMBINATION FOR USE IN GLYCEMIC CONTROL IN DIABETES TYPE 2 PATIENTS

The present invention refers to a pharmaceutical combination for use in glycemic control in diabetes type 2 patients. 1. A pharmaceutical combination for use in glycemic control in diabetes type 2 patients , said combination comprising{'sup': '36', 'sub': 6', '2, '(a) desProExendin-4(1-39)-Lys—NHor/and a pharmaceutically acceptable salt thereof, and'}(b) a glitazone or/and a pharmaceutically acceptable salt thereof.2. The combination of claim 1 , further comprising(c) metformin or/and a pharmaceutically acceptable salt thereof.3. The combination of claim 2 , wherein the metformin or/and a pharmaceutically acceptable salt thereof is prepared for oral administration.4. The pharmaceutical combination according to claim 1 , wherein the diabetes type 2 patient is obese.5. The pharmaceutical combination according to claim 1 , wherein the diabetes type 2 patient has a body mass index of at least 30 kg/m.6. The pharmaceutical combination according to claim 1 , wherein the diabetes type 2 patient is an adult patient.7. The pharmaceutical combination according to claim 1 , wherein the diabetes type 2 patient does not receive an antidiabetic treatment.8. The pharmaceutical combination of claim 1 , wherein in the diabetes type 2 patient claim 1 , diabetes mellitus type 2 has been diagnosed at least 1 year or at least 2 years before onset of therapy.9. The pharmaceutical combination of claim 1 , wherein the diabetes type 2 patient has a HbAvalue of about 7% to about 10%.10. The pharmaceutical combination of claim 1 , wherein the diabetes type 2 patient has a fasting plasma glucose concentration of at least 8 mmol/L.11. The pharmaceutical combination of claim 1 , wherein the diabetes type 2 patient has a 2 hours postprandial plasma glucose concentration of at least 10 mmol/L.12. The pharmaceutical combination of claim 1 , wherein the diabetes type 2 patient has a glucose excursion of at least 2 mmol/L claim 1 , A claim 1 , wherein the glucose excursion is the difference of the 2 ...

Biomarkers for Cardiodiabetes

The invention provides compositions and methods for determining cardiodiabetes status in a subject. The invention also provides compositions and methods for treating a subject experiencing cardiodiabetes.

METHODS AND COMPOSITIONS FOR THE IMPROVEMENT OF SKELETAL MUSCLE FUNCTION IN A MAMMAL

The present invention is directed to the treatment of muscular dysfunction or increasing muscle strength and/or decreasing muscle fatigue in a subject using a composition that includes a biguanide or a pharmaceutically acceptable salt thereof, e.g., at a low dosage. 1. A method of treating muscular dysfunction , increasing muscle strength , or decreasing muscle fatigue in a subject in need thereof , said method comprising administering to said subject a therapeutically effective amount of a biguanide or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein said muscular dysfunction is associated with a condition or disease selected from the group consisting of muscular dystrophy claim 1 , sarcopenia claim 1 , cachexia claim 1 , cancer claim 1 , acquired immune deficiency syndrome claim 1 , advanced organ failure claim 1 , chronic obstructive pulmonary disease claim 1 , rhabdomyolysis claim 1 , disuse atrophy claim 1 , incontinence claim 1 , sepsis claim 1 , neuromuscular disease claim 1 , and congenital myopathy.3. The method of claim 2 , wherein said muscular dystrophy is Duchenne muscular dystrophy.420-. (canceled)21. A method of treating or reducing the likelihood of developing cancer in a subject in need thereof or extending the lifespan of said subject claim 2 , said method comprising administering to said subject a low dosage of a biguanide or a pharmaceutically acceptable salt thereof.22. (canceled)23. A pharmaceutical composition comprising a biguanide or a pharmaceutically acceptable salt thereof at a dosage unit of less than 250 milligrams.24. (canceled) This invention was made with government support under grant number NIH R44 NS059098. The government has certain rights in the invention.In general, the invention relates to methods of using a biguanide to treat muscular dysfunction, increase muscle strength, and/or reduce muscle fatigue. The invention also features pharmaceutical compositions formulated with low dosages of a ...

Drug Formulations Using Water Soluble Antioxidants

The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin cross-linking) during the manufacturing process and/or during shelf-life storage. 1. A coated tablet comprising: '(i) optionally at least one antidiabetic agent or a pharmaceutically acceptable salt thereof, wherein the antidiabetic agent is other than saxagliptin;', '(a) a tablet core wherein the tablet core comprises'} (i) a coating material; and', '(ii) optionally at least one water soluble antioxidant;, '(b) a first layer that coats the tablet core, wherein the first layer comprises'} (i) a coating material;', '(ii) at least one water soluble antioxidant; and', '(iii) an active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof, wherein the active pharmaceutical ingredient is a primary amine or a secondary amine; and, '(c) a second layer that coats the first layer wherein the second layer comprises'} (i) a coating material; and', '(ii) optionally at least one water soluble antioxidant., '(d) a third layer that coats the second layer wherein the third layer comprises'}2. The coated tablet according to wherein the active pharmaceutical ingredient is saxagliptin claim 1 , sitagliptin claim 1 , vildagliptin claim 1 , linagliptin claim 1 , dutogliptin claim 1 , or alogliptin.3. The coated tablet according to wherein the active pharmaceutical ingredient is saxagliptin.4. The coated tablet according to wherein the water soluble antioxidant is ascorbic acid claim 1 , propyl gallate claim 1 , sodium sulfite claim 1 , sodium metabisulfite claim 1 , sodium bisulfite claim 1 , thioglycerol claim 1 , thioglycollic acid claim 1 , or a combination thereof.5. The coated tablet according to ...

Compounds and Pharmaceutical Compositions for Uses in Diabetes

New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I, IA, IB and IC, and their pharmaceutical acceptable salts are described for prevention or treatment of diabetes or a diabetes-related disorder in a subject in need thereof. Diabetes and diabetes-related disorder include Type I diabetes, Type II diabetes, maturity-onset diabetes of the young, latent autoimmune diabetes of adults (LADA), gestational diabetes, diabetic nephropathy, proteinuria, ketonuria, obesity, hyperglycemia, glucose intolerance, insulin resistance, hyperinsulinemia, hypercholesterolemia, hypertension, hyperlipoproteinemia, hyperlipidemia, hypertriglyceridemia, dyslipidemia, metabolic syndrome, syndrome X, diabetic neuropathy, diabetic retinopathy, hypoglycemia, cardiovascular disease, atherosclerosis, diabetic kidney disease, ketoacidosis, thrombotic disorders, sexual dysfunction, dermatopathy, edema, metabolic syndrome and renal disorders. The related pharmaceutical compositions and methods are also described. These compounds can be used in combination with comprising a therapeutic agent for lowering or controlling blood glucose level such as metformin or a thiazolidinedione. 128-. (canceled)33. The method of claim 29 , wherein the pharmaceutically acceptable salt is a base addition salt.34. The method of claim 33 , wherein the base addition salt comprises a metal counterion selected from sodium claim 33 , potassium claim 33 , magnesium claim 33 , calcium and lithium.36. The method of claim 35 , wherein the compound is Compound I claim 35 , II claim 35 , V claim 35 , VIII claim 35 , XIV claim 35 , XXIII or XXVI.37. The method of claim 35 , wherein the compound is Compound I.38. The method of claim 35 , wherein the compound is Compound XIV.39. The method of claim 29 , wherein said diabetes or diabetes-related disorder is Type I diabetes claim 29 , Type II diabetes claim 29 , maturity-onset diabetes of the young claim 29 , latent autoimmune ...

METHODS FOR ADMINISTERING HYPOGLYCEMIC AGENTS

The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists. 1. A method for treating a disease selected from the group consisting of Type 1 diabetes , Type II diabetes , obesity and hyperglycemia in a human in need thereof comprising administering a composition comprising at least one polypeptide having GLP-1 activity as a subcutaneous injection to said human via an injection device comprising a tube having a gauge of about 28 or greater once weekly , wherein the composition comprises about 0.01 mg to about 104 mg of at least one polypeptide having GLP-1 activity.2. The method of wherein the disease is Type II diabetes.3. The method of claim 1 , wherein the polypeptide having GLP-1 activity comprises at least one fragment or variant of human GLP-1 genetically fused with human serum albumin.4. The method of wherein the at least one fragment or variant of GLP-1 comprises GLP-1(7-36(A8G)).5. The method of wherein the at least one fragment or variant of GLP-1 is genetically fused to human serum albumin.6. The method of wherein at least one fragment or variant of GLP-1 comprises at least two GLP-1(7-36(A8G)) tandemly and genetically fused to the human serum albumin.7. The method of wherein the at least two GLP-1(7-36(A8G)) are genetically fused at the N-terminus of the human serum albumin.8. The method of wherein at least one polypeptide having GLP-1 activity comprises the amino acid sequence of SEQ ID NO: 1.9. The method of wherein the polypeptide having the amino acid of SEQ ID NO:1 is administered at a dose of about 0.25 mg to about 32 mg weekly.10. The method of claim 1 , wherein said composition comprising at least one polypeptide having GLP-1 activity comprises exendin-4.11. The method of claim 1 , further comprising the step of co-administering a compound selected from the group of: peroxisome proliferating activated receptor ligand claim 1 , thiazolidinedione claim 1 , metformin claim 1 , insulin claim 1 , and sulfonylurea ...

ANTIMICROBIAL SOLUTIONS

The present invention provides antimicrobial solutions that in certain cases comprise a biguanide and a glycol ether and, in some cases, optionally also includes combinations of at least one an alcohol, at least one chelator, glycerol, deoxycholate, and/or at least one alkylpolyglucoside. In certain aspects the invention comprises a biguanide and deoxycholate or a combination of chelator, ethanol, and alkylpolyglucoside. Also provided are methods for rapidly killing and/or reducing bacteria, fungi, or virus from surfaces, for example, including surfaces of indwelling medical devices and organic surfaces such as skin and sutures, and inorganic surfaces such as medical equipment, pipelines etc. 1. An antimicrobial composition comprising at least one biguanide and at least one glycol ether.3. The composition of claim 1 , comprising a biguanide claim 1 , a glycol ether claim 1 , and an alkylpolyglucoside.4. The composition of claim 1 , comprising a biguanide claim 1 , a alkylpolyglucoside claim 1 , a chelator claim 1 , and an alcohol.5. The composition of claim 1 , comprising a biguanide claim 1 , a glycol ether claim 1 , and deoxycholate.6. The composition of claim 1 , comprising a biguanide claim 1 , a glycol ether claim 1 , an alkylpolyglucoside claim 1 , and deoxycholate.7. The composition of claim 2 , wherein R is a C-Calkyl.8. The composition of claim 2 , wherein the alkylpolyglucoside is selected from the group consisting of capryl glucoside claim 2 , decyl glucoside claim 2 , coco-glucoside claim 2 , and lauryl glucoside.9. The composition of claim 1 , wherein the biguanide is selected from the group consisting of chlorhexidine claim 1 , alexidine claim 1 , hexamidine.10. The composition of claim 1 , wherein the glycol ether is dipropylene glycol n-butyl ether.11. The composition of claim 1 , wherein the chelator is selected from the group of chelators consisting of EDTA free acid claim 1 , EDTA 2Na claim 1 , EDTA 3Na claim 1 , EDTA 4Na claim 1 , EDTA 2K claim 1 ...

ANTIMICROBIAL WOUND DRESSING

The invention relates to a wound dressing comprising a polymer substrate and a compound comprising a) at least one antimicrobial active agent and b) an agent that reduces the cytotoxicity, comprising an oil-in-water emulsion that additionally has one or more alkanediol(s) and/or one or more glyceryl ether(s). 1. A wound dressing comprising a polymeric substrate and a composition comprisinga) at least one antimicrobially active substance; andb) a cytotoxicity-reducing agent comprising an oil-in-water emulsion that additionally contains one or more alkanediols and/or one or more glycerol ethers.2. The wound dressing according to claim 1 , wherein said polymeric substrate can absorb liquid claim 1 ,3. The wound dressing according to claim 1 , wherein said polymeric substrate is selected from the group consisting of polyurethanes claim 1 , polyethers claim 1 , cellulose materials claim 1 , cellulose derivatives claim 1 , polyesters claim 1 , polyvinyl alcohol claim 1 , polyvinyl acetate claim 1 , polysulfones claim 1 , polyacrylates claim 1 , polyolefins claim 1 , polyamides claim 1 , alginates claim 1 , chitosan as well as mixtures and combinations thereof.4. The wound dressing according to claim 1 , wherein said polymeric substrate is selected from the group consisting of polyethylene terephthalate claim 1 , polyethylene claim 1 , polypropylene claim 1 , rayon claim 1 , cotton claim 1 , nylon-6 claim 1 ,6 claim 1 , polycaprolactam claim 1 , polyurethane as well as any mixtures and combinations thereof.5. The wound dressing according to claim 1 , wherein said polymeric substrate is polyurethane.6. The wound dressing according to claim 5 , wherein said polyurethane is obtained by reacting a component having at least one isocyanate group with at least one polyol.7. The wound dressing according to claim 1 , wherein said antimicrobially active substance is selected from the group of components having at least one guanide and/or biguanide group claim 1 , iodophors claim 1 , ...

PHARMACEUTICAL COMPOSITION AND USES THEREOF

The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases. 1. A pharmaceutical composition comprising:a) an extended release core comprising metformin (particularly metformin hydrochloride) and one or more excipients;b) an optional seal and/or barrier coating; and a DPP-4 inhibitor, preferably linagliptin, and', 'a SGLT-2 inhibitor, preferably 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene,', 'and one or more excipients., 'c) an immediate release coating comprising at least one active pharmaceutical ingredient selected from'}2. The pharmaceutical composition according to claim 1 , wherein the inner extended release core a) is a formulation comprising metformin hydrochloride claim 1 , a swellable and/or extended release polymer claim 1 , and one or more further excipients.3. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising:the at least one active pharmaceutical ingredient, preferably a stabilizer for stabilizing linagliptin (preferably L-arginine), andone or more film-coating agents selected from hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), ethyl cellulose, hydroxypropyl cellulose, polydextrose, methacrylic and/or acrylic polymer, or a mixture thereof,optionally one or more plasticizers selected from polyethylene glycol, propylene glycol, diethyl phthalate, tributyl sebacate and/or triacetin, or a mixture thereof,optionally a glidant selected from talc, magnesium stearate and fumed silica, andoptionally one or more pigments and/or colorants.4. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising linagliptin claim 1 , L-arginine as stabilizer claim 1 , a film- ...

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.

BICYCLIC GPR119 MODULATORS

The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I). 7. The compound of claim 1 , wherein is double bond.9. The compound of claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , cyano claim 1 , halo claim 1 , cycloalkyl claim 1 , heterocyclyl claim 1 , aryl or heteroaryl.10. The compound of claim 1 , wherein Ris hydrogen claim 1 , halogen or alkyl.11. The compound of claim 1 , wherein Ris hydroxyalkyl claim 1 , —C(O)OR claim 1 , —S(O)R claim 1 , —C(O)NRR claim 1 , —N(R)C(O)R claim 1 , —CHN(R)C(O)R claim 1 , —N(R)C(O)OR claim 1 , —N(R)C(O)NRR claim 1 , —S(O)NRR claim 1 , —N(R)S(O)R claim 1 , heterocyclyl; wherein Rand Rare each independently a hydrogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , cycloalkyl claim 1 , hydroxyalkyl claim 1 , aryl claim 1 , heteroaryl or heterocyclyl; or Rand Rmay join together with the nitrogen atom to which they are attached to form a heterocyclic ring.12. The compound of claim 1 , wherein Ris substituted or unsubstituted heteroaryl or heterocyclyl.13. The compound of claim 12 , wherein heteroaryl is oxazole claim 12 , oxadiazole claim 12 , triazole or tetrazole.14. The compound of claim 12 , wherein heterocyclyl is pyrrolidine claim 12 , pyrrolidine-2-one or oxazolidin-2-one.15. The compound of claim 12 , wherein substituent(s) is alkyl.16. The compound of claim 1 , wherein X is —(CRR)O(CRR)— or —(CRR)NR(CRR)—; ‘q’ is 0 or 1; ‘t’ is 0 or 1; and each of Rand Rare hydrogen.17. The compound of claim 1 , wherein Z is hydrogen ...

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.

PHARMACEUTICAL COMPOSITIONS CONTAINING A BIGUANIDE AND A LOW DOSE ANTIDIABETIC AGENT

The present invention relates to pharmaceutical compositions that include a combination of a biguanide present in an extended-release form and a low dose antidiabetic agent present in an immediate-release form. The present invention further relates to processes for preparing such compositions. 1. A pharmaceutical composition of a biguanide and a low dose antidiabetic agent comprising:(i) a biguanide core comprising a therapeutically effective amount of a biguanide or its pharmaceutically effective salts and one or more pharmaceutically acceptable excipients;(ii) optionally a seal coat;(iii) an extended-release coat comprising one or more rate-controlling materials wherein there is no passageway in the coat;(iv) optionally a second seal coat;(v) a low dose antidiabetic agent coat comprising a therapeutically effective amount of a low dose antidiabetic agent or its pharmaceutically effective salts and one or more pharmaceutically acceptable excipients; and(vi) optionally a film coat.2. The pharmaceutical composition according to claim 1 , wherein the biguanide comprises metformin claim 1 , phenformin claim 1 , buformin claim 1 , and pharmaceutically acceptable salts claim 1 , solvates claim 1 , polymorphs claim 1 , enantiomers claim 1 , isomers claim 1 , or mixtures thereof.3. The pharmaceutical composition according to claim 1 , wherein the low dose antidiabetic agent is selected from DPP-IV inhibitors claim 1 , meglitinides claim 1 , second generation sulphonylureas claim 1 , glucagon-like peptide (GLP-1) analogues claim 1 , other hypoglycemics which are used as an adjunct to metformin therapy claim 1 , or mixtures thereof.4. The pharmaceutical composition according to claim 1 , wherein the biguanide is metformin and the low dose antidiabetic agent is a DPP-IV inhibitor.5. The pharmaceutical composition according to claim 1 , wherein the biguanide is layered onto a pharmaceutically inert core or seed.6. The pharmaceutical composition according to claim 5 , wherein ...

Compositions comprising an aryl pyrazole and/or a formamidine, methods and uses thereof

This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds alone or in combination with formamidine compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to the animal in need thereof.

Methods and compositions for increasing the anaerobic working capacity in tissues

Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

NOVEL PHARMACEUTICAL FORMULATION CONTAINING A BIGUANIDE AND A THIAZOLIDINEDIONE DERIVATIVE

A pharmaceutical dosage form comprising a controlled release component comprising an antihyperglycemic drug in combination with a second component comprising a thiazolidinedione derivative is herein disclosed and described. 134-. (canceled)35. A tablet for the oral administration of metformin hydrochloride and pioglitazone hydrochloride comprising:(a) a controlled release core comprising: i) a core comprising about 500 mg to about 1000 mg of only one drug which is metformin hydrochloride and at least one pharmaceutically acceptable excipient; and ii) a sustained release coating surrounding the core;(b) optionally a first seal coating surrounding the sustained release coating wherein the first seal coating does not contain an active pharmaceutical ingredient and rapidly disperses or dissolves in water; and (i) about 15 mg to about 45 mg of pioglitazone hydrochloride;', '(ii) a binder selected from the group consisting of polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethylcellulose, hydroxypropyl methylcellulose, ethylcellulose, polymethacrylate, polyvinylalcohol, waxes and mixtures thereof;', '(iii) a pore forming agent selected from the group consisting of sodium chloride, potassium chloride, sucrose, sorbitol, mannitol, polyethylene glycols, propylene glycol and mixtures thereof;', '(iv) optionally a pharmaceutical excipient selected from the group consisting of surfactants, absorption enhancers, plasticizers, antifoaming agent and combinations thereof, '(c) an immediate release pioglitazone layer surrounding the sustained release coating of the controlled release core or the first seal coating if present comprising (i) (+/−)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzyl]-5-hydroxy-2,4-thiazolidinedione;', '(ii) (z)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzylidene]-2,4-thiazolidinedione;', '(iii) (+/−)-5-[p-[2-(5-ethyl-2-pyridyl)ethoxy]benzyl]-3-[2-(5-ethyl-2-pyridyl)ethyl]-2,4-thiazolidinedione;', '(iv) (+/−)-ethyl-2-carbamoylthio-3-[4-[2-(5-ethyl-2-pyridyl) ...

TOPICAL PHARMACEUTICAL COMPOSITION COMPRISING NANONIZED SILVER SULFADIAZINE AND CHLORHEXIDINE GLUCONATE

The invention relates to an improved topical pharmaceutical composition for burn treatment and microbial infections on human beings or animals. The pharmaceutical composition comprises 0.1% w/w to 1% w/w of an antimicrobial drug, i.e., silver sulfadiazine and 0.2% w/w antiseptic, i.e., chlorhexidine gluconate; wherein silver sulfadiazine is in nanonized form. 1. A topical pharmaceutical composition comprising 0.1% w/w to 1% w/w silver sulfadiazine , 0.2% w/w chlorhexidine gluconate , and one or more pharmaceutically acceptable excipients; wherein the silver sulfadiazine has a Z-average molar mass between 150 nm to 500 nm.2. The topical pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipients comprise one or more of thickening agents claim 1 , emulsifying agents claim 1 , fragrance/perfumes claim 1 , preservatives claim 1 , chelating agents claim 1 , pH modifiers claim 1 , and antioxidants.3. The topical pharmaceutical composition according to claim 2 , wherein the thickening agents comprises one or more of soft paraffin claim 2 , aluminum stearate claim 2 , cetostearyl alcohol claim 2 , propylene glycol claim 2 , polyethylene glycols claim 2 , povidone claim 2 , wool-fat claim 2 , hydrogenated lanolin and beeswax.4. The topical pharmaceutical composition according to claim 2 , wherein the emulsifying agent comprises one or more of cetomacrogol claim 2 , non-ethoxylated glyceryl monostearate claim 2 , carbopols claim 2 , cetearyl alcohol claim 2 , sodium stearoyl lactylate and lecithin.5. The topical pharmaceutical composition according to claim 2 , wherein the preservative comprises one or more of methylparaben claim 2 , propylparaben claim 2 , benzyl alcohol claim 2 , benzoic acid claim 2 , sodium benzoate claim 2 , chlorocresol claim 2 , sorbic acid and its salt claim 2 , and phenylethyl alcohol.6. The topical pharmaceutical composition according to claim 2 , wherein the chelating agent comprises one or more of ...

Compounds and Methods for Treating Aberrant Adrenocartical Cell Disorders

Methods and compositions are provided for treatment of disorders associated with aberrant adrenal cortex cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC), Cushing's syndrome and/or pituitary ACTH excess (Cushing's Disease). Such methods involve administration of an effective amount N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)-methyl)urea hydrochloride to the patient.

TREATMENT OF MOTOR NEURON DISEASE

Provided herein are methods and compositions for the treatment of motor neuron diseases including, for example, amyotrophic lateral sclerosis. Suitable therapeutic agents include, for example, agents that up-regulate the expression IGF-II or guanine deaminase in a cell. 1. A method for treating a motor neuron disease in a human patient comprising administering to said patient a therapeutically effective amount of an agent that up-regulates IGF-II gene expression.2. The method of claim 1 , wherein the therapeutic agent up-regulates IGF-II by at least 2-fold in said patient.3. The method of or claim 1 , wherein the agent is selected from the group consisting of eletriptan hydrobromide claim 1 , modafinil claim 1 , dicloxacillin sodium claim 1 , thiamphenicol claim 1 , ceftibuten claim 1 , tacrine HCl claim 1 , fluoxetine claim 1 , citalopram claim 1 , fluvoxamine maleate claim 1 , amoxapine claim 1 , atomoxetine HCl claim 1 , olmesartan medoxomil claim 1 , guanabenz acetate claim 1 , hydralazine HCl claim 1 , methyldopate HCl claim 1 , diltiazem HCl claim 1 , glyburide claim 1 , flurbiprofen claim 1 , carprofen claim 1 , meloxicam sodium claim 1 , diclofenac sodium claim 1 , levodopa claim 1 , olanzapine claim 1 , chlorpromazine claim 1 , valacyclovir HCl claim 1 , levocarnitine claim 1 , ropinirole claim 1 , vardenafil HCl claim 1 , guaifenesin claim 1 , omeprazole claim 1 , cetirizine HCl claim 1 , azelastine hydrochloride claim 1 , ramelteon claim 1 , nicotine ditartrate claim 1 , zolpidem claim 1 , aspartame claim 1 , thiamine claim 1 , riboflavin claim 1 , niacinamide claim 1 , sildenafil HCl claim 1 , tadalafil HCl and dexamethasone acetate.4. The method of claim 3 , wherein the agent is vardenafil HCl.5. The method of claim 4 , wherein the therapeutically effective amount is from 1 mg to 50 mg per day.6. The method of claim 3 , wherein the agent is guanabenz acetate.7. The method of claim 6 , wherein the therapeutically effective amount is from 1 mg to 10 mg ...

Soft Elastic Capsules Containing Tablets and Liquid or Semisolid Fills and Methods for Their Manufacture

Disclosed herein is a soft elastic capsule that includes an acid resistant, capsule shell that defines an encapsulated space having a predetermined volume, a liquid or semisolid fill comprising a first active ingredient located within the encapsulated space, and a first compressed tablet a having a minimal dimension of 2 mm, being located within the encapsulated space, unanchored to the capsule shell, and surrounded by the fill, said tablet comprising a second active ingredient that is substantially insoluble in the fill. A method of manufacturing a soft elastic capsule is also disclosed.

COMBINATION OF SYROSINGOPINE AND MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF CANCER AND IMMUNOSUPPRESSION

The invention relates to a combination of syrosingopine and a mitochondrial inhibitor, e.g. metformin or oligomycin, and the use of the combination of syrosingopine and a mitochondrial inhibitor for the treatment of cancer and for achieving immunosuppression. The invention also relates to a fluorescence-based method for predicting syrosingopine sensitivity of a cancer cell. 1. A pharmaceutical composition comprising syrosingopine and a mitochondrial inhibitor.2. The pharmaceutical composition of wherein the mitochondrial inhibitor is metformin or phenformin.3. The pharmaceutical composition of wherein the mitochondrial inhibitor is metformin.4. The pharmaceutical composition of wherein the mitochondrial inhibitor is selected from the group consisting of rotenone claim 1 , piericidin A claim 1 , epiberberine claim 1 , 2-thenoyltrifluoroacetone (TTFA) claim 1 , antimycin A claim 1 , oligomycin claim 1 , carbonyl cyanide-p-trifluoromethoxyphenylhydrazone (FCCP) claim 1 , and stavudine.5. The pharmaceutical composition of wherein the mitochondrial inhibitor is oligomycin.6. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and the mitochondrial inhibitor is between 1 to 10 and 1 to 1′000.7. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and metformin is between 1 to 10 and 1 to 200.8. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and oligomycin is between 1′000 to 1 and 10′000 to 1.9. A combination of syrosingopine and a mitochondrial inhibitor for use in the treatment of cancer or autoimmune diseases.10. The method of wherein the mitochondrial inhibitor is metformin.11. The method of wherein the mitochondrial inhibitor is oligomycin.12. The method of wherein the cancer is selected from the group consisting of carcinoma claim 19 , sarcoma claim 19 , leukemia claim 19 , myeloma claim 19 , lymphoma claim 19 , and cancers ...

LIPID-LOWERING ANTIDIABETIC AGENT

A composition which includes a salt of metformin and the use of the composition for treatment of or use in prediabetes, diabetes, lowering triglycerides and/or other conditions in mammals. 119-. (canceled)2344-. (canceled) The present application claims priority from U.S. provisional patent application 61/461,113 filed on Jan. 12, 2011, the contents of which arc herein incorporated by reference.1. Field of the InventionThe present invention relates to salts of poly unsaturated fatty acids with biguanides.2. Technical BackgroundDiabetes mellitus has become pandemic and according to a forecast by the World Health Organization, there will be a sharp increase in the number of diabetic patients by the year 2030. This is an ominous forecast, because managing the long-term complications of diabetes, which include nephropathy, neuropathy, retinopathy, and cardiovascular complications, will have a serious impact on public health budgets. The hallmark of diabetes is chronically elevated blood glucose levels. It is also known that abnormally elevated glucose levels have an adverse impact on glutathione levels in key diabetic tissues. Furthermore, increased oxidative stress and increased production of reactive oxygen species are implicated under hyperglycemic conditions.In spite of the early discovery of insulin and its subsequent widespread use in the treatment of diabetes, and the later discovery of and use of sulfonylureas, and thiazolidenediones, such as troglitazone, rosiglitazone or pioglitazone, as oral hypoglycemic agents, the treatment of diabetes remains less than satisfactory.The use of insulin requires multiple daily doses, usually by self-injection. Determination of the proper dosage of insulin requires frequent estimations of the sugar in urine or blood. Treatment of non-insulin dependent diabetes mellitus (type 2 diabetes, NIDDM) usually consists of a combination of diet, exercise, oral hypoglycemic agents, e.g., thiazolidenediones, and, in more severe cases, ...

Modulation of histone h2b monoubiquitination and treatment of cancer

Provided are methods and compositions for treatment of cancer. In particular, these methods and compositions may include an inhibitor of a deubiquitinating enzyme. In certain aspects, these methods and compositions may include a modulator of glucose metabolism. Also provided are methods of assaying the glucose content of cells and tissues using detection of uH2B.

Treatment protocol of diabetes type 2

The present invention refers to a treatment protocol for diabetes type 2 patients.

NOVEL COMPOSITIONS COMPRISING A PHOSPHODIESTERASE-5 INHIBITOR AND THEIR USE IN METHODS OF TREATMENT

The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.

ORAL CARE METHOD AND KIT

A method of moisturizing while decolonizing mammalian tissue, comprising applying a multi-valent cationic antiseptic composition to the tissue, and applying a moisturizer composition to at least a portion of the same tissue is provided. An oral care kit comprising a composition comprising the multi-valent cationic antiseptic and the moisturizer composition, and a method of moisturizing oral tissue of a patient requiring intubation using the moisturizer composition and an endotracheal tube coated or impregnated with a cationic antiseptic are also provided. 1. An oral care kit comprising:at least one dose of a multi-valent cationic antiseptic composition comprising a multi-valent cationic antiseptic;a moisturizer composition in an amount sufficient for at least 4 separate applications; anda treatment protocol;wherein each composition is for application to oral tissue of a subject within a specified time period according to the protocol; and wherein at least one application of the moisturizer composition is to be applied within 4 hours before or after applying the multi-valent cationic antiseptic;wherein the moisturizer composition essentially excludes any component which causes a precipitate when combined with the multi-valent cationic antiseptic when tested according to Test Method F;wherein the multi-valent cationic antiseptic is other than a metal ion.2. The oral care kit of claim 1 , wherein the essentially excluded component is selected from the group consisting of polyanions of polycarboxylates claim 1 , polysulfonates claim 1 , polysulfates claim 1 , and organic and inorganic polyphosphates; anions of alkylsulfates claim 1 , arylsulfates claim 1 , alkylsulfonates claim 1 , arylsulfonates claim 1 , alkylcarboxylates claim 1 , arylcarboxylates claim 1 , alkylphosphates claim 1 , arylphosphates; halide salts; and combinations thereof claim 1 , wherein the alkyl groups have a chain length of greater than 6 carbon atoms and the aryl groups have 6 or more carbon ...

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.

Salts of lorcaserin with optically active acids

Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.

LIPOSOMAL DRUG COMPOSITION CONTAINING A POLYMERIC GUANIDINE DERIVATIVE

A liposomal drug composition comprising: a dimeric or polymeric guanidine derivative or a pharmaceutically acceptable salt thereof as drug substance, and a lipid modified by polyethylene glycole (PEG). The drug composition have cytostatic and antimicrobial activity. 1. A liposomal drug composition comprising:a dimeric or polymeric guanidine derivative or a pharmaceutically acceptable salt thereof as drug substance; anda lipid modified by polyethylene glycole (PEG).2. A liposomal drug composition according to claim 1 , wherein the lipid is a phospholipid and said PEG is PEG-PEG.3. A liposomal drug composition according to claim 1 , wherein said polymeric guanidine derivative is one claim 1 , which guanidine derivative is based on a diamine containing oxyalkylene chains between two amino groups claim 1 , with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyoxyalkylene chains between two amino groups.4. A liposomal drug composition according to claim 3 , wherein among the representatives of the family of polyoxyalkylene guanidine salts claim 3 , there are such using triethylene glycol diamine (relative molecular mass: 148) claim 3 , polyoxypropylene diamine (relative molecular mass: 230) as well as polyoxyethylene diamine (relative molecular mass: 600).5. A liposomal drug composition according to claim 1 , wherein poly-[2-(2-ethoxyethoxyethyl)guanidinium hydrochloride] comprising at least 3 guanidinium groups is contained as the drug substance.6. A drug composition according to claim 5 , wherein the average molecular mass of the drug substance ranges from 500 to 3000.7. A method of preparing a cytostatically active liposomal drug composition using the dimeric or polymeric guanidine derivative of .8. A method of preparing an antimicrobial drug composition using the dimeric or polymeric guanidine derivative of .9. A process for therapeutically treating human beings and animals claim 1 ...

USE OF A DPP-4 INHIBITOR IN AUTOIMMUNE DIABETES, PARTICULARLY LADA

The present invention relates to methods for treating and/or preventing autoimmune diabetes, particularly LADA, as well as diseases related or associated therewith, comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for modifying disease trajectory of autoimmune diabetes (particularly LADA). 2. The method according to claim 1 , wherein human patient has or is at risk of a cardiovascular and/or renal disease selected from the group consisting of myocardial infarction claim 1 , stroke claim 1 , peripheral arterial occlusive disease claim 1 , diabetic nephropathy claim 1 , micro- or macroalbuminuria claim 1 , acute or chronic renal impairment claim 1 , hyperuricemia and hypertension.3. The according to claim 1 , wherein the human patient has nephropathy claim 1 , impaired renal function claim 1 , chronic kidney disease claim 1 , and micro- or macroalbuminuria.4. The method of claim 1 , wherein the human patient has mild claim 1 , moderate or severe renal impairment claim 1 , or end stage renal disease.5. The method of claim 1 , wherein the human patient patient has microalbuminuria or diabetic nephropathy.6. The method of claim 1 , wherein the one or more other active agents is selected from the group consisting of metformin claim 1 , thiazolidinediones claim 1 , insulin and insulin analogues.7. A method for modifying the disease trajectory of latent autoimmune diabetes of adults (LADA) in a human patient claim 1 , the method comprising administering to said human patient linagliptin claim 1 , optionally in combination with one more other active agents selected from the group consisting of metformin claim 1 , thiazolidinediones claim 1 , insulin and insulin analogues claim 1 , wherein said human patient has one or more autoantibodies selected from the group consisting of GAD-65 claim 1 , anti-GAD claim 1 , ICA claim 1 , IA-2A claim 1 , ZnT8 (anti-ZnT8) and IAA.8. The method according to ...

Aqueous Pharmaceutical Composition Containing A Biologic Therapeutic Agent And Guanidine Or A Guanidine Derivative And An Injection Including The Composition

The present invention is directed to an aqueous pharmaceutical composition, particularly an aqueous ophthalmic composition, suitable as an injection, particularly an intravitreal injection. The composition includes a biologic therapeutic agent (e.g., an isolated monoclonal antibody that specifically binds to a C5 protein) that tends to raise the viscosity of the composition and a guanidine and/or guanidine derivative (e.g., L-arginine) that tends to lower the viscosity of the composition. 2. A composition as in wherein the composition is an aqueous ophthalmic composition suitable for intravitreal injection.3. A composition as in further comprising a stabilizer.4. A composition as in wherein stabilizer is trehalose.5. A composition as in further comprising a surfactant.6. A composition as in wherein the viscosity of the composition is no greater than 7 centipoise.7. A composition as in wherein the biologic therapeutic agent is an antibody.8. A composition as in wherein the biologic therapeutic agent is an IgG1/lambda isotype antibody.9. A composition as in wherein the biologic therapeutic agent is an isolated monoclonal antibody that specifically binds to a C5 protein.10. A composition as in wherein the guanidine and/or guanidine derivative includes only guanidine derivative and wherein:{'sub': 3', 'n', '2n+1', '2n', 'n', '2−1, 'R1 is nothing, CH, CH, CH, or CH(n=1−10); and'}R2 includes an amine group, an amino group, an amido group, a methoxy group, an alkoxy group, an ester, an ether, a carboxylic acid or a combination thereof.11. A composition as in wherein the guanidine and/or guanidine derivative includes only guanidine derivative and wherein:{'sub': 3', 'n', '2n+1', 'n', '2', 'n', '2n−1, 'R1 is nothing, CH, CH, CHn, or CH(n=1−10); and'}R2 includes an amine group and a carboxylic acid group.12. A composition as in wherein the guanidine and/or guanidine derivative includes only guanidine derivative and wherein:{'sub': 1', '9', '1', '5', '2', '4, 'R1 is a C-Calkyl ...

Bilayer Tablet Formulations

The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Co-Therapy for Diabetic Conditions

Methods of treating diseases such as diabetes are disclosed. Methods of modulating elevated fructosamine levels, elevated HbA1c levels, impaired glucose tolerance, and impaired fasting glucose are also disclosed. In some embodiments, methods include co-administration of a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof. Drug products including a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide, a sulfonylurea and insulin, or pharmaceutically acceptable salts thereof, in combination are also disclosed. 1. A method for treating diabetes in a human in need of such treatment , the method comprising administering to said human therapeutically effective amounts of a bile acid sequestrant and two or more additional compounds selected from the group consisting of a biguanide , a sulfonylurea , insulin , and pharmaceutically acceptable salts thereof.2. The method of claim 1 , wherein the bile acid sequestrant and the two or more compounds are administered substantially simultaneously.3. The method of claim 1 , wherein the bile acid sequestrant and the two or more compounds are administered separately.4. The method of claim 2 , wherein the bile acid sequestrant and the two or more compounds are administered within one hour of each other.5. The method of claim 3 , wherein the bile acid sequestrant and the two or more compounds are administered within twelve hours of each other.6. The method of claim 1 , wherein the bile acid sequestrant is selected from the group consisting of colesevelam claim 1 , cholestyramine claim 1 , and colestipol; the biguanide comprises metformin; and the sulfonylurea is selected from the group consisting of glipizide claim 1 , glyburide glimepiride claim 1 , gliclazide claim 1 , glibenclamide claim 1 , gliquidone claim 1 , acetohexamide claim 1 , ...

INSULIN SENSITISERS AND METHODS OF TREATMENT

The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitisers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes, syndrome X, hyperglycaemia, vascular disease and kidney disease. The present invention further relates to compounds and agents and compositions thereof for use in the treatment methods. 2. (canceled)3. The combination according to wherein the compound of Formula (III) is methazolamide.4. (canceled)6. The method according to wherein the compound of Formula (III) is administered at a dose that does not cause clinically significant inhibition of carbonic anhydrase enzymes.7. The method according to wherein the compound of Formula (III) is methazolamide.8. The method according to wherein the methazolamide is administered at a dose of from 10 to 100 mg per day.912.-. (canceled)14. The method according to wherein claim 13 , the disease or condition is type II diabetes claim 13 , gestational diabetes claim 13 , impaired glucose tolerance claim 13 , impaired fasting tolerance or syndrome X.15. The method according to wherein the compound of Formula (III) is administered at a dose that does not cause clinically significant inhibition of carbonic anhydrase enzymes.16. The method according to wherein the compound of Formula (III) is methazolamide.17. The method according to where the methazolamide is administered at a dose of from 10 to 100 mg per day.1821.-. (canceled) The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitisers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes ...

BRIDGE-HELIX CAP: TARGET AND METHOD FOR INHIBITION OF BACTERIAL RNA POLYMERASE

It has been discovered that the Sal target represents a new and promising target for antibacterial drug discovery. The Sal target is distinct from the rifamycin target and from the CBR703 target. This indicates that antibacterial compounds that function through the Sal target should exhibit no, or minimal, cross-resistance with rifamycins and CBR703. This further implies that it should be possible to co-administer antibacterial compounds that function through the Sal target together with a rifamycin, together with CBR703, or together with both a rifamycin and CBR703, in order to achieve additive or synergistic antibacterial effects and in order to suppress or eliminate the emergence of resistance. 1. A method for identifying an agent that binds to a bacterial RNAP bridge-helix cap target in a first entity , comprising the steps of:(a) preparing a reaction solution including the agent to be tested and a first entity including a bacterial RNAP bridge-helix cap target; and(b) detecting at least one of the presence, extent, concentration-dependence, or kinetics of binding of the agent to the bridge-helix cap target, wherein the agent is not salinamide A.2. The method of claim 1 , wherein the first entity is a bacterial RNAP.3Escherichia coli. The method of claim 1 , wherein the first entity is RNAP.4Bacillus subtilis. The method of claim 1 , wherein the first entity is RNAP.5. The method of claim 1 , further comprising the step of: assessing at least one of the presence claim 1 , extent claim 1 , concentration-dependence claim 1 , or kinetics of binding of the agent to a second entity that contains a derivative of a bacterial RNAP bridge-helix cap target having at least one substitution claim 1 , insertion claim 1 , or deletion.6. The method of claim 5 , wherein the second entity is a derivative of a bacterial RNAP.7Escherichia coli. The method of claim 5 , wherein the second entity is a derivative of RNAP.8Bacillus subtilis. The method of claim 5 , wherein the second ...

Thermo-sensitive, mucoadhesive or dermoadhesive, and penetration-enhancing formulations for topical delivery of therapeutics

The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.

Chemosensory Receptor Ligand-Based Therapies

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use. 1201-. (canceled)202. A method of lowering blood glucose levels in a subject in need thereof , comprising administering a composition comprising metformin or salt thereof , wherein the composition is adapted to release a therapeutically effective amount of the metformin or salt thereof to one or more regions of the intestine.203. A method of treating disorders of glucose metabolism in a subject in need thereof , comprising administering a composition comprising metformin or a salt thereof , wherein the composition is adapted to release a therapeutically effective amount of the metformin or salt thereof to one or more regions of the intestine.204. The method according to claim 203 , wherein said disorder is hyperglycemia.205. A method of treating a condition associated with a chemosensory receptor in a subject in need thereof comprising administering a composition comprising metformin or a salt thereof claim 203 , wherein the composition is adapted to release a therapeutically effective amount of the metformin or salt thereof to one or more regions of the intestine.206205. The method according to any one of - claims 202 , wherein said metformin salt is metformin hydrochloride.207205. The method according to any one of - claims 202 , wherein said one or more regions of the intestine are the duodenum claims 202 , jejunum claims 202 , ileum and/or lower intestine.208205. The method according to ...

Medicine composition containing vitamin d and metformin

A medicine composition contains vitamin D and metformin, wherein vitamin D comprises vitamin D2, vitamin D3, alphacalcidol, calcifediol, calcitriol, and dihydrotachysterol. The composition can be used in the preparation of a medicine for treating and/or preventing a polyp and cancer in large intestine.

ANTI-PARASITIC METHODS AND COMPOSITIONS UTILIZING DIINDOLYLMETHANE-RELATED INDOLES

The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis. 1. A method of treating or reducing the risk of a protozoal disease comprising administering to a subject in need thereof a therapeutically effective amount of one or more DIM-related indoles and one or more anti-protozoal agents.2. The method of claim 1 , wherein said protozoal disease is leishmaniasis or trypanosomiasis.3. The method of claim 1 , wherein said protozoal disease is malaria claim 1 , toxoplasmosis claim 1 , cryptosporidiosis or bebesiosis.4Microsporidia, Trichomonas, Cyclospora, IsosporaBlastocystis.. The method of claim 1 , wherein said protozoal disease results from an infection from or5Neospora.. The method of claim 1 , wherein said protozoal disease results from an infection from6. The method of claim 1 , or claim 1 , wherein said subject is a human.7. The method of claim 6 , wherein said human is immunocompromised.8. The method of claim 3 , wherein said subject is a lamb claim 3 , calf claim 3 , pig claim 3 , rabbit or chicken.9. The method of claim 5 , wherein said subject is a non-human mammal selected from the group consisting of a dog claim 5 , cow claim 5 , sheep claim 5 , goat and horse.11. The method of claim 1 , wherein the one or more DIM-related indoles are selected from the group consisting of diindolylmethane claim 1 , hydroxylated DIMs claim 1 , methoxylated DIMs claim 1 , 2-(Indol-3-ylmethyl)-3 claim 1 ,3′-diindolylmethane (LTR) claim 1 , ...