Abstract: In certain embodiments methods are provided for the therapeutic or prophylactic amelioration of one or more symptoms or disorders associated with metabolic syndrome. In various embodiments the methods involve administering to a subject in need thereof, a GABA receptor agonist, in an amount sufficient to ameliorate said one or more symptoms. In certain embodiments methods are provided for the prophylaxis or treatment of type I diabetes and related pathologies that involve the use of GABA or GABA agonists in combination with certain other compounds (e.g., one more antigens (e.g., GAD) that have a therapeutic effect in type I diabetes and/or an anti-CD3 antibody, an anti-CD20 antibody, exendin-4, and/or or a pro-insulin therapeutic).

Abstract: Disclosed are methods for treating a subject suffering from phenylketonuria and/or phenylalanemia. The methods include, in part, enterally administering to the subject a LNAA supplement in which the weight ratio of Leu to Val is greater than 2:1; in which the weight ratio of Leu to iLeu is greater than 3:1; or which includes one or more LNAAs and which further includes Lys. LNAA supplements are also disclosed. Also disclosed are methods for treating a subject suffering from a condition involving a metabolic disorder involving the metabolism of a first amino acid X. The method includes enterally administering to the subject a composition which (i) is substantially free from the first amino acid X and (ii) which includes a second amino acid Y that competes with amino acid X at a gastrointestinal tract transporter.

Abstract: Methods of treating, ameliorating, or inhibiting the development of autoimmune diseases by modulating the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease. The binding may be modulated by the administration of D-?-methyldopa, or pharmaceutical compositions comprising therapeutically effective amounts of D-?-methyldopa.

Abstract: This invention relates to a biological oil composition, preferably obtained from a copepod, most preferably the copepod Calanus finmarchicus and the use thereof to prevent or treat formation of atherosclerotic plaques and hence development of coronary heart disease. The composition comprises the same marine n-3 polyunsaturated fatty acids (PUFAs) generally regarded as being responsible for the anti-atherosclerotic effect of marine oils, namely EPA (C20:5n-3 eicosapentaenoic acid) and DHA (C22:6n-3 docosahexaenoic acid). However, quite unexpectedly, it has been found that the oil composition of the present invention has a remarkably higher ability to prevent formation of atherosclerotic plaques than what can be attributed to EPA and DHA alone, and moreover, unlike EPA and DHA alone it has a notable blood cholesterol lowering effect.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Described herein are pharmaceutical compositions comprising fumarate esters, methods for making the same, and methods for treating subjects in need thereof. In particular, oral pharmaceutical compositions comprising fumarate esters are described.

Abstract: Described herein are pharmaceutical compositions comprising fumarate esters, methods for making the same, and methods for treating subjects in need thereof. In particular, oral controlled release pharmaceutical compositions comprising fumarate esters suspended in liquid matrices are described. One embodiment described herein is a pharmaceutical composition comprising fumarate esters suspended in a lipid or lipophilic liquid with enhanced bioavailability.

Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Abstract: The present invention relates to a pharmaceutical composition for preventing, ameliorating, or treating cancer. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating cancer including a lignan compound having a specific chemical structure (Chemical Formula 1); a health functional food composition for preventing or ameliorating cancer including the lignan compound; and a method for preventing, ameliorating, or treating cancer using the composition. Further, the present invention relates to a use of the lignan compound in the preparation of a pharmaceutical composition or a health functional food composition for preventing, ameliorating, or treating cancer.

Abstract: This application is in the field of medicinal chemistry and relates to ultrapure ajulemic acid, its synthesis, pharmaceutical compositions and methods of use thereof for the treatment and/or prevention of inflammation, pain, and fibrotic diseases including scleroderma, systemic sclerosis, scleroderma-like disorders, sine scleroderma, liver cirrhosis, interstitial pulmonary fibrosis, idiopathic pulmonary fibrosis, Dupuytren's contracture, keloids, chronic kidney disease, chronic graft rejection, and other scarring-wound healing abnormalities, post-operative adhesions, and reactive fibrosis.

Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.

Abstract: The present invention is directed to statin formulations having improved solubility and/or stability and methods for the same.

Abstract: One aspect of the invention provides a method of inhibiting an efflux pump in a bacteria, the method comprising contacting the bacteria with 3,4-dibromopyrrole-2,5-dione, thereby inhibiting the efflux pump. Another aspect provides a method of inhibiting proliferation of a bacteria, the method comprising contacting the bacteria with 3,4-dibromopyrrole-2,5-dione and an antibiotic, thereby inhibiting the proliferation of the bacteria. Another aspect of the invention provides a method of increasing the efficacy of an antibiotic, the method comprising contacting a bacteria with 3,4-dibromopyrrole-2,5-dione and an antibiotic, thereby increasing the efficacy of the antibiotic. Another aspect provides a method of inhibiting development of antibiotic resistance in a bacteria, the method comprising contacting the bacteria with 3,4-dibromopyrrole-2,5-dione and an antibiotic, thereby inhibiting development of resistance to the antibiotic.

Abstract: The present invention provides the compound Ormeloxifene [3, 4-trans-2,2-dimethyl-3-phenyl-4-p-(beta-pyrrolidinoethoxy) phenyl-7-methoxy chroman] as useful in inducing differentiation in wide range of myeloid leukemias including acute promyelocytic leukemia, acute myeloid leukemia and chronic myeloid leukemia where block in differentiation is common feature. Ormeloxifene induced differentiation that is marked by increase in differentiation marker proteins like C/EBP? and surface proteins such as cd11b and granulocyte colony stimulating factor receptor (GCSFr). Differentiated cells having neutrophil like morphology were observed when treated with 1.0 uM to 7.5 uM ORM which clearly indicates that ORM can induce differentiation in myeloid leukemia cells. At higher doses (5 uM to 7.5 uM) there is early onset of myeloid differentiation (24 to 48 h) with reduced no. of cells which is likely due to apoptotic effects of ORM at higher does.

Abstract: This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).

Abstract: The invention relates to medicine and concerns a method for the prophylaxis or treatment of diseases caused by (+)RNA-containing viruses which involves the use of an effective amount of glutaryl histamine or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition for the prophylaxis or treatment of diseases caused by (+)RNA-containing viruses which contains an effective amount of glutaryl histamine or a pharmaceutically acceptable salt thereof. The present invention solves the problem of providing a novel agent which is effective in the treatment of diseases caused by (+)RNA-containing viruses of the enterovirus genus or of the flavivirus genus.

Abstract: Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.

Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.

Abstract: The invention is a pharmaceutical tablet formulation comprising between about 12.5 mg and 100 mg losartan potassium, between about 6.25 mg and about 50 mg chlorthalidone, and sodium bicarbonate in an amount between about 1.0% and about 10.0% by weight.

Abstract: The present invention is directed to methods of inhibiting LTA4-h in a human patient and method of treating a condition ameliorated by the inhibition of leukotriene A4 hydrolase activity in a human patient comprising administering to said human patient the compound, 4-{5-[4-(4-Oxazol-2-yl-phenoxy)-benzyl]-2,5-diaza-bicyclo[2.2.1]hept-2-ylmethyl}-benzoic acid.

Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.

Abstract: Pharmaceutically acceptable single parasiticidal agent compositions of imidacloprid for oral delivery to mammals to systemically control targeted blood-sucking or blood-consuming parasites, such as fleas, ticks and certain species of helminthes and scabies.

Abstract: The present invention relates to new compositions and methods for protecting neuronal cells from ischemic or hypoxic events. More precisely, this invention provides new combinatorial therapies that efficiently protect neuronal cells from ischemia or hypoxia.

Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

Abstract: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Abstract: Disclosed herein are methods of treating retinopathy of prematurity (ROP) in a premature and/or low birth weight infant in need thereof, comprising administering to the infant an effective amount of a compound represented by Structural Formula I, Structural Formula la or Structural Formula II described herein, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of inhibiting the destruction of retinal blood vessels in a premature and/or low birth weight infant in need thereof, comprising administering to the infant an effective amount of a compound represented by Structural Formula I, Structural Formula la or Structural Formula II, or a pharmaceutically acceptable salt thereof.

Abstract: The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphine which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.

Abstract: The present invention pertains to oral immediate release pharmaceutical compositions suitable for treating patients suffering from pain comprising oxycodone and naloxone or their pharmaceutically acceptable salts.

Abstract: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.

Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

Abstract: The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects.

Abstract: The described invention provides a method of treating a patient with an epithelial cancer comprising administering a composition comprising a therapeutic amount of an inhibitor of a BTK protein and one or more chemotherapeutic agent(s) selected from the group consisting of an antimetabolite, a platinum coordination compound, an alkylating agent and a combination thereof, wherein the composition is effective to reduce one or more of tumor cell growth, tumor cell clonogenicity, tumor cell proliferation, tumor cell viability and tumor volume and the therapeutic amount of the inhibitor of a BTK protein and the one or more chemotherapeutic agent(s) exerts a synergistic effect. The described invention also provides methods of treating a chemotherapy drug-resistant cancer and sensitizing a cancer patient to chemotherapy.

Abstract: The present invention relates to the use of 1-(4-chlorophenyl)-4-(4-morpholinyl)-2.5-dihydro-1H-imidazol-2-one or a physiologically acceptable salt thereof in a method for treatment and/or prevention of one or more epileptic disorders in a feline animal, preferably a cat.

Abstract: The present invention relates to a method of treating ophthalmic diseases and conditions, e.g. diabetic retinopathy, age-related macular degeneration, retinopathy of prematurity, etc., in a subject comprising administering to said subject a therapeutically effective amount of at least one compound of formula I or a prodrug, pharmaceutically acceptable salt, racemic mixtures or enantiomers of said compound. The compounds of formula I are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.

Abstract: The present invention provides an improved novel process of manufacturing a sterile, ophthalmic pharmaceutical suspension comprising an active ingredient(s) such as carbonic anhydrase inhibitors (CAIs) wherein the said process involves solubilization, followed by controlled precipitation of carbonic anhydrase inhibitors of the right particle size, e.g., less than 10 micron, preferably less than 5 micron (D90) by varying pH with a little or no homogenization. Said process further does not require the use of any special equipment such as ball mill, milling bottle and/or jet mill. This newly improved process is simple, cost effective and efficient.

Abstract: A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)n—R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)a—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxy

Abstract: Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid, e.g., oleic acid, that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound or active metabolite thereof to subcutaneous fat under the skin. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject. The present invention also provides kits comprising the composition and instructions for use.

Abstract: Cerclage pessary containing progesterone homogeneously distributed in the pessary body providing a prolonged, sustained and continuous release for a period of at least 6 months, wherein the pessary consists of dimethylsiloxane elastomer with RTV (Room Temperature Vulcanization) mechanism, the progesterone amount is from 20% to 30% w/w, relative to pessary weight and the ratios of the polymers forming the matrix is from 6:1 to 14 1. The cerclage pessary is useful for the prevention of preterm birth. Progesterone diffuses through the polymer continuously, without altering the shape and integrity of the pessary, since the elastomer forming the polymeric matrix used herein is not biodegradable. This guarantees that the form of pessary remains intact until the end of treatment.

Abstract: Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component that includes an Glucocorticoid Derivative which, upon delivery to the posterior segment of a mammalian eye, does not significantly diffuse to the anterior segment of said eye. Methods of making and using the present materials are also described.

Abstract: A preparation method for an antithyroid ointment for external application is provided. The ointment includes the following components by mass percentage: 0.01-10% gluco corticoid, 1-15% antithyroid drug, 0.1-30% percutaneous penetration enhancer, 10-30% oleaginous base and 4-40% water-soluble base. The method includes: mixing the glucocorticoid and a drug carrier material so as to evenly disperse the glucocorticoids on the drug carrier material to obtain a glucocorticoid component; placing and evenly mixing an antithyroid drug and other ingredients in distilled water, and heating to 80° C. and evenly mixing to obtain a water phase; melting an oleaginous base and a percutaneous penetration enhancer at 80° C. and evenly mixing to obtain an oil phase; maintaining at 80° C. and pouring the oil phase into the water phase, and evenly stirring; adding the glucocorticoid component when the temperature drops to 40° C.; and evenly and sufficiently stirring until cooled to obtain an ointment.

Abstract: A method of accelerating remyelination or suppressing demyelination of neurons in a mammal, and a method of treating a disease associated with demyelination of neurons in a mammal.

Abstract: The present invention relates to use of bisphosphonate formulations for the treatment and management of HIV/AIDS. The method of the invention comprises administering a formulation comprising an effective amount of a bisphosphonate that specifically inhibits the activity and/or decreases the number of monocytes and/or macrophages, thereby reducing or eliminating HIV reservoirs. The invention also provides a method of complementing an HIV antiviral therapy, such as the highly active antiretroviral therapy (HAART), with a bisphosphonate formulation to improve clinical outcome.

Abstract: Osteoclast inhibitors, such as neridronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.

Abstract: The present invention relates to the field of medicine. It relates more particularly to the use of compounds to prevent and/or treat lipotoxicity in a subject, especially lipotoxicity by hypoxia. The invention relates more particularly to compositions, especially pharmaceuticals compositions and nutritional supplements or complements comprising such compounds as well as their use to prevent and/or treat lipotoxicity, especially lipotoxicity by hypoxia. The compounds and compositions of the invention can especially be advantageously used to prevent and/or treat a pathology from among pulmonary pathologies, especially cystic fibrosis or a chronic obstructive pulmonary disease.

Abstract: A new class of paromomycin-derived aminoglycosides, which exhibit efficient stop-codon mutation suppression activity, low toxicity and high selectivity towards eukaryotic cells are provided. Also provided are chemical and chemo-enzymatic processes of preparing these paromomycin-derived aminoglycosides and intermediates thereof, as well as pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders.

Abstract: Disclosed herein is a method for alleviating radiation injury, which includes administering to a subject in need thereof a composition containing isorhamnetin-3-O-?-D-glucoside.

Abstract: Methods and devices treating an autonomic nervous system associated disease condition in a subject are provided. Aspects of the invention include inducing one or more physiological response selected from the group consisting of sweating, gastric emptying, enhanced heart rate variability and enhanced quantitative sensory test responsiveness in a manner sufficient to modify the autonomic nervous system so as to treat the subject for the disease condition. The methods and devices find use in a variety of applications, e.g. in the treatment of subjects suffering from conditions arising from disorders of the autonomic nervous system.

Abstract: This disclosure relates to the field of cancer, particularly the field of melanoma. It was found that a particular long non-coding RNA (lncRNA) is specifically up-regulated in melanoma (but not other tumor) cells as compared to melanocytes. Inhibition of this lncRNA in melanoma cells leads to induction of apoptosis and is a novel therapeutic strategy in the treatment of melanoma.