Abstract: The invention relates to a pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the prophylaxis and therapy of Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy. Another object of the invention concerns the use of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the enhancement of insulin sensitivity and the preservation or increase of ?-cell compensation.

Abstract: The use of Kukoamine A and Kukoamine B in the preparation of drugs for the prevention and treatment of sepsis and autoimmune disease is disclosed. Bacterial endotoxin/lipopolysaccaride (LPS) and unmethylated DNA (CpG DNA) of bacteria, the major pathogen-associated molecular patterns in sepsis and autoimmune disease, are specifically targeted, while the disclosed use and directionally isolates lead compounds from traditional Chinese medicine. These measures can overcome the major defects of uncertainty of pharmacological material basis and drug targets of extracts and constituents of traditional Chinese medicine. The disclosed use can help in developing a safe, effective and quality controllable drug for prevention and treatment of sepsis and autoimmune disease so as to help solve the present lack of effective drugs in clinical treatment.

Abstract: Amorphous solid dispersions suitable for oral delivery comprising fenretinide or an analog thereof and at least one matrix polymer, and processes for making the dispersions, are disclosed. Also disclosed are solid oral formulations comprising the amorphous solid dispersions, as well as uses thereof for the prevention and/or treatment of diseases or conditions treatable by fenretinide, including but not limited to cancers, conditions associated with a lipid imbalance, cystic fibrosis, osteoporosis, conditions associated with inflammation or opportunistic infections, and other diseases such as diabetes, obesity, dry-form age-related macular degeneration.

Abstract: Methods of alleviating the symptoms of hemoglobinopathies, including, but not limited to, sickle cell disease, ?-thalassemia, and hemoglobin H disease are provided. In some embodiments, the methods comprise administering an agent to the subject if the subject has increased expression or activation of at least one of ERK, Ras, BRAF, Raf1 MEK, ?-arrest1/2, Syk, P60-c-Src, or GRK2. Methods of determining the likelihood of a complication or vascular endothelial injury and mortality resulting from a hemoglobinopathy in a subject are also provided.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: The present disclosure relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases, the pharmaceutical composition including a graphene nanostructure as an active ingredient.

Abstract: The present invention provides a highly palatable colon cleansing formulation that utilizes a low chloride electrolyte-replenishing base solution. When formulated with polyethylene glycol and a selected sugar alcohol, the formulation offers the advantages of superior palatability without undesirable concomitant side effects or a decrease in cleansing efficacy.

Abstract: The present invention aims to provide an ophthalmic solution for the treatment of dry eye which is used to inhibit apoptosis caused by tear hyperosmolarity. The present invention relates to an ophthalmic solution for the treatment of dry eye, containing diclofenac or a pharmaceutically acceptable salt thereof, the ophthalmic solution being used to inhibit apoptosis caused by tear hyperosmolarity.

Abstract: Compositions and methods for therapeutic delivery are disclosed. More particularly, the present disclosure relates to nanoparticle compositions that sequester the activity of a target molecule while leaving other domains accessible to bind targeted tissues of interest. Methods for thrombus dissolution include administering a nanoparticle reversibly coupled to a target molecule that can dissolve a blood clot. Compositions and methods for inducing blood clotting are also disclosed. Methods for inducing blood clotting include administering a nanoparticle reversibly coupled to a target molecule that can induce the formation of a blood clot. Methods for sequestering a target molecule are also disclosed. The method includes reversibly coupling a target molecule to a nanoparticle having an affinity ligand that reversibly couples the target molecule, and thus, sequesters the target molecule activity until the target molecule interacts with its substrate resulting in the release of the target molecule.

Abstract: Described are methods for oral administration of therapeutic proteins and peptides, more specifically to the oral administration of therapeutic proteins and peptides with gastric acid modulators, and compositions of comprising a gastric acid modulator and a protein or peptide.

Abstract: The present invention relates to use of ornithine in the manufacture of a medicament for use in combination with at least one of phenylacetate and phenylbutyrate for preventing or treating liver decompensation or hepatic encephalopathy. The invention also relates to use of at least one of phenylacetate and phenylbutyrate in the manufacture of a medicament for use in combination with ornithine for preventing or treating liver decompensation or hepatic encephalopathy.

Abstract: The present invention is based on the discovery that parenteral nutrition (PN) induced liver disease, e.g. fatty liver disease, can be prevented and even reversed by administration of primarily omega-3-fatty acid with PN rather than the administration of the standard intravenous lipid emulsions that contain primarily plant derived omega-6 fatty acid. Thus, the present invention provides a method for treating or preventing liver disease in a human patient obtaining nutritional support through PN. The method comprises intravenous administration of an effective amount of an omega-3-fatty acid emulsion to the patient, wherein the patient is not administered phytosterols or plant derived fatty acids, e.g. omega-6 fatty acids derived from a plant source, and wherein the administration of the omega-3-fatty acid emulsion to the patient is for a period greater than three weeks. Preferably, the administration is for a period of greater than six weeks.

Abstract: A method for treating or preventing a complement activated T-cell mediated disorder in a subject includes administering a therapeutically effective amount of a pharmaceutical composition to the subject. The pharmaceutical composition includes at least one amidine compound or pharmaceutically acceptable salt.

Abstract: The present invention relates to new crystals A, B and F of lobaplatin as well as preparation methods therefor and pharmaceutical applications thereof. Lobaplatin crystal A has a melting point Tm.p. of 220±5° C. and is obtained by adding a lobaplatin trihydrate to a suspension crystallization solvent. Lobaplatin crystal B has a melting point Tm.p. of 230±5° C. and is obtained by performing solvent evaporation on a lobaplatin trihydrate or by adding a solvent to a lobaplatin dihydrate, and performing room temperature evaporation or solventing-out crystallization and then drying. Lobaplatin crystal F has a melting point Tm.p. of 229±5° C. and is obtained by adding methanol or ethanol to a lobaplatin dihydrate, stirring at room temperature until solids are dissolved, filtering out insolubles, slowly adding an organic solvent, crystallizing out, separating the crystal and drying the crystal.

Abstract: The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

Abstract: The invention relates to fluorinated compounds and their use in the field of pathological syndromes of the cardiovascular system. Novel fluorinated benzofuran derivatives of amiodarone and pharmaceutically acceptable salts or solvates thereof and their use for the treatment of arrhythmias are described.

Abstract: Provided is a hepatocyte nuclear factor 4 alpha (HNF4-?) antagonist and a use thereof. The HNF4-? antagonist selected in the present invention was confirmed to specifically bind to the ligand binding domain of HNF4-?, thereby inhibiting the activity of HNF4-?. The HNF4-? antagonist of the present invention can significantly reduce the expression of Wnt5a in a specific manner compared to that of the conventional known HNF4-? antagonists, and can also inhibit the growth of gastric cancer cells. Therefore, the HNF4-? antagonist of the present invention can not only be used as a pharmaceutical composition or a health functional food for preventing and treating cancer but can also be applied to a composition for treating or preventing diseases occurring due to the overexpression of HNF4-?.

Abstract: A substituted chroman compound includes R1a and R1b as substituents selected from hydrogen and phenyl optionally substituted with 1-3 substituents. R2a and R2b are hydrogen atoms. R3a and R3b are C1-C4 alkyls, or represent an oxo group, or are C5-C8 alkylene substituents. R3a and R3b with their attached carbon atom form a ring. Nitrogen atoms replace two non-adjacent carbon atoms in the main chain to the C5-8 alkylene, which is optionally substituted by a thioxo group. n is the number of the substituents Rz. z is the sequence number of the substituent Rz. (Rz) is a substituent on the benzene ring attached to a non-nodal carbon atom selected from hydroxyl, halogen, C2-C6 alkenyl, C1-C4 alkoxy, C1-4 alkanoyloxy, heterocyclic C4-C7 alkyloxy having an oxygen atom in the ring and optionally substituted with 1-3 substituents. The compound is used as a tautomer, enantiomer, diastereomer, mixture of enantiomers and/or mixture of diastereomers.

Abstract: The present invention administers a cannabinoid medication to a patient followed by observing one or more physiological responses in the patient during a first period of time when treating a medical condition. The cannabinoid medication may include one or more specific types of cannabinoids at a dosage level or may include a plurality of discrete formulations where each formulation includes masses of specific cannabinoids that may be used for treating one or more ailments.

Abstract: The present invention relates to a novel pharmaceutical composition comprising zaltoprofen or a pharmaceutically acceptable salt thereof in combination with muscle relaxants with anti-inflammatory, analgesic and myorelaxant activity.

Abstract: The present invention relates to the use of 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio-?-D-xylopyranoside in the treatment of a mucopolysaccharidosis such as type I mucopolysaccharidosis.

Abstract: Methods for treating ameliorating, reducing and/or preventing a cutaneous T-cell lymphoma in a subject in need thereof, comprising administration butyroyloxymethyl diethyl phosphate (AN-7) alone or combined with an additional anti-cancer therapy.

Abstract: Degranulation suppressors are provided that are effective against allergic disease and osteoarthritis. The degranulation suppressors contain chlorophyll c.

Abstract: The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a diastereoisomer thereof for use in the treatment of cancers associated with human papillomavirus. The present invention also relates to the pharmaceutical compositions containing the compounds of Formula (I) for the treatment of cancers associated with human papillomavirus.

Abstract: Provided are methods and compositions that relate to, inter alia, CBL0137 for the treatment of various cancers, optionally in combination with various agents.

Abstract: The present disclosure provides compositions that inhibit the SH2-containing inositol 5?-phosphatase (SHIP), as well as methods using such compositions for use in treating or ameliorating the effects of a medical condition in a subject.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: There is provided a compound of formula I or a pharmacologically acceptable salt thereof: for use in the treatment of a brain cancer selected from a MGMT positive astrocytic brain tumor, a metastatic brain cancer and primary CNS lymphoma and a method of treating said brain cancers in a patient in need thereof comprising administering to the patient said compound of formula I or a pharmacologically acceptable salt thereof.

Abstract: The invention relates to the use of a pan-PPAR agonist, or of a pharmaceutical composition containing said agonist, for the treatment of a fibrotic condition.

Abstract: An agent that increases local concentration of retinoic acid (RA) in the intestine through modifying enzymatic pathways involved in RA metabolism is administered in a dose effective to inhibit or reverse production of inflammatory mediators by intestinal dendritic cells and thereby reduce intestinal inflammation and tumor growth associated with intestinal inflammation.

Abstract: The present invention relates to rifaximin compositions comprising amino acids, characterized in that they increase rifaximin solubility in aqueous solutions and are useful in the treatment of disease wherein amino acids and rifaximin are efficacious. The present invention also relates to pharmaceutical compositions comprising rifaximin or one of the pharmaceutically acceptable salts thereof and one or more amino acid(s), wherein the molar ratio between the amino acid(s) and rifaximin is from 1:1 to 10:1, together with pharmaceutically acceptable excipients. The present invention further relates to rifaximin crystals obtained by dissolving rifaximin and amino acids in solutions formed by ethanol/water and evaporating the solution.

Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (1): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.

Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Abstract: A composition suitable for use in nicotine replacement therapy products includes a nicotine product that includes a synthetic nicotine that is substantially free of one or more contaminants and/or impurities normally associated with tobacco-derived nicotine. For example, the synthetic nicotine is substantially free of one or more of nicotine-1?-N-oxide, nicotyrine, nornicotyrine, 2?,3-bipyridyl, cotinine, anabasine, and/or anatabine. The composition further comprises one or more pharmaceutically acceptable excipients, additives and/or carriers. The nicotine replacement therapy products may include any number of such products, including transdermal nicotine delivery patches, nicotine gums, synthetic chewing tobacco, synthetic snuff, and synthetic strips (e.g., dissolvable synthetic tobacco). Additionally, a method of treating nicotine addiction includes administering a nicotine replacement composition, e.g., via a nicotine replacement therapy product, to a user.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

Abstract: Protein kinase C plays important roles in TNBC development and could be a specific target. The in vitro anti-proliferative activity of PKC inhibitor chelerythrine on a panel of breast cancer cell lines was evaluated. Chelerythrine selectively inhibited the growth of TNBC cell lines over non-TNBC cell lines as demonstrated by cell proliferation assay and colony formation assay. The selective anti-proliferative effect of chelerythrine was associated with the differential apoptosis induction ability on breast cancer cell lines and induction of cell cycle arrest in some TNBC cell lines. By analysis of the expression levels of different PKC subtypes, the inventors found multiple PKC isozymes may mediate the selective activity of chelerythrine on TNBC cells. Finally, combination of chelerythrine and chemotherapy reagent taxol showed synergistic/additive effect on TNBC cell lines.

Abstract: A liposome of irinotecan or irinotecan hydrochloride and its preparation method are disclosed. The liposome contains irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, wherein the weight ratio of the cholesterol to the neutral phospholipid is 1:3 to 1:5. The liposome is prepared by an ion gradient method.

Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.

Abstract: The present invention provides polymorphic forms of Vortioxetine of and its pharmaceutically acceptable salts. Specifically the present invention relates to the novel crystalline forms of Vortioxetine or its pharmaceutically acceptable salts. Moreover, the present invention also provides an amorphous form of Vortioxetine hydrobromide and a stable amorphous co-precipitate of Vortioxetine hydrobromide with pharmaceutically acceptable excipients.

Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.

Abstract: The present invention relates to a method for treating a dry eye syndrome using an alpha 2 adrenergic agonist, pharmaceutically acceptable salt thereof or a mixture thereof. In particular, the alpha 2 adrenergic agonist of the invention has a higher alpha 2A agonist activity compared to alpha 2B agonist activity. This invention also relates to an ophthalmic composition comprising a therapeutically effective amount of an alpha 2 adrenergic agonist, a pharmaceutically acceptable salt thereof or a combination thereof as an active ingredient for treating a dry eye syndrome.

Abstract: Disclosed are methods that address providing a subject experiencing, or who has experienced, a headache precursor event and administering dihydroergotamine, or a pharmaceutically acceptable salt or complex thereof, to the subject by oral inhalation, in an amount effective to pre-empt a subsequent headache in the subject. Also disclosed are compositions that are related to those methods.

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.

Abstract: In one aspect, the invention relates to compounds having the formula I: where R1, R2a, R2b, and R3-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.

Abstract: The present invention features solid dosage forms comprising two or more different active ingredients. In one embodiment, the present invention features a tablet dosage form comprising a first layer and a second layer, wherein the first layer comprises (1) 200 mg lopinavir, (2) ritonavir, (3) a pharmaceutically acceptable hydrophilic polymer, (4) a pharmaceutically acceptable surfactant, and (5) no more than 0.2% by weight of one or more lubricants, and the second layer comprises another therapeutic agent.

Abstract: Compositions tor prevention or treatment of non-inflammatory neuronal damage from brain trauma and strokes are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Linalool, Icilin and combinations thereof. Methods for treatment or prevention of non-inflammatory neuronal damage from brain trauma and strokes are also provided, and the methods include administering such compositions.