Abstract: The present invention is directed to a method for treating a neurodegenerative disease such as amyotrophic lateral sclerosis (ALS), Alzheimer disease, Parkinson's disease, Huntington's disease, frontotemporal degeneration, dementia with Lewy bodies, a motor neuron disease, or a demyelinating disease. The method comprises administering to a subject in need thereof a Ppargc1a activator 2-(4-tert-butylphenyl)-1H-benzimidazole, 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole, in an effective amount. A preferred route of administration is oral administration.

Abstract: The present invention relates to active agents or compounds as well as pharmaceutical compositions comprising said compounds, which are capable of reducing or inhibiting or blocking the enzymatic activity of the glutaminyl-peptide cyclotransferase (QPCT) protein, the glutaminyl-peptide cyclotransferase-like protein (QPCTL) protein, or combinations thereof or are capable of reducing or inhibiting the expression of QPCT gene, the QPCTL gene, or combinations thereof. Also provided are methods for screening or selecting for said compounds. The present invention further relates to a pharmaceutical composition comprising a first active agent for use in a method of treating a condition in a subject that would benefit from reducing the signaling or the binding between SIRP? and CD47 in the subject (e.g. cancer), wherein the method of treating comprises reducing expression or enzymatic activity of QPCTL, QPCT, or combinations thereof in the cell with CD47 on the surface.

Abstract: Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.

Abstract: It has been established that exposure to cytotoxic doses of HSP90 inhibitor is broadly immunosuppressive, whereas continuous exposure to low-dosages of the same inhibitor exerts anti-tumor activity. The anti-tumor activity is mediated by the host immune system. Compositions and methods for continuous, low-dose exposure to HSP90 inhibitors in combination with one or more immunostimulatory agents for the treatment of cancer are described. Typically, the HSP90 inhibitor is administered in an amount that is between 1% and 20% of the clinically-determined maximum tolerate dose. The immunostimulatory agent can be administered simultaneously with the HSP90 inhibitor, or at some time before or after the HSP90 inhibitor. Compositions including a sub-toxic dose of HSP90 inhibitor in combination with an immunostimulatory agent in an amount effective to treat cancer are also provided.

Abstract: The present invention discloses novel formulations, reconstitutable solid compositions, pharmaceutical compositions, and aqueous injectable formulations of specific amidine substituted beta-lactam compounds on the basis of modified cyclodextrins and organic and/or inorganic acids, their preparation and use as antimicrobial pharmaceutical compositions that are parenterally or orally administrable.

Abstract: Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodrug comprises a step of coupling the drug molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.

Abstract: Methods of treating a bacterial lung infection are provided and comprise administering an effective amount of rifaximin to a subject in need thereof. The rifaximin can be delivered by inhalation therapy, such as by delivering the rifaximin in aerosol form. The rifaximin is administered alone or in combination with tobramycin, including in multiple doses. Methods of reducing biofilm formation are also provided and comprise contacting a bacteria with an effective amount of rifaximin. Pharmaceutical composition are also included and comprise rifaximin and a pharmaceutically-acceptable vehicle suitable for administering the rifaximin in aerosol form.

Abstract: The invention relates to MKK4 (mitogen-activated protein kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The MKK4 inhibitors selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7.

Abstract: Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Abstract: Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Abstract: Described herein are spiro and cyclic bis-benzylidine proteasome inhibitors, which inhibit the proteasome function through either ubiquitin receptor ADRM1/RPN13 or proteasome DUB enzymes (USP14, UCH37 and RPN11), and which can be used for the treatment of cancers/diabetes/neurological disorders.

Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

Abstract: The present disclosure relates to a pharmaceutical composition comprising as active substance betahistine or a pharmaceutically acceptable salt thereof, for use in the treatment of otological or neurological disorders in a human subject by intranasal application.

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

Abstract: The present invention relates to pharmaceutical compositions for alleviation of pain and/or skin inflammation comprising (i) ropivacaine and (ii) two or more locoregional anesthetics of amide type and optionally hydrocortisone, to methods of preparing such compositions and uses thereof.

Abstract: The present disclosure relates to identification of inhibitors of hepatitis and herpesvirus replication including compounds of the formula: wherein the variables are as defined herein. Also provided are methods of treatment using agents so identified.

Abstract: Provided is a topical pharmaceutical gel composition of an amlodipine salt and methods for its use in the treatment of anorectal disease.

Abstract: Provided are methods for improving cell-based therapies by co-administration with an agent that increases the production and or levels of epoxygenated fatty acids, as well as kits, stents and patches for co-administering stem cells with an agent that increases the production and/or levels of epoxygenated fatty acids.

Abstract: Methods and compositions for producing fetal hemoglobin and treating a hemoglobinopathy or thalassemia are disclosed.

Abstract: A composition for treating varicose veins is provided and has 61.67% Reverse Osmosis Water, 5.5% Glycerin, 5.5% Caprylic Triglycerides, 2.5% Oleic Acid, 2.5% Propylene Glycol, 1.5% Isopropyl Alcohol (or alternatively Ethanol), 1.0% Polysorbate 80, 0.3% Lecithin, 0.8% Xanthan Gum, 0.4% Allantoin, 1.1% Methyl Nicotinate (Nicotinic Acid), 0.3% Pyridoxal-5-Phosphate (P5P), 0.1% Phosphatidylcholine, 5.0% L-Histidine, 5.0% Glycine, 3.0% Gingko Biloba Extract, 0.08% Phytonadione, 0.05% Cholecalciferol, 2.0% Copper Peptides (GHK-Cu), 0.8% Sharon™ Biomix II, 1.0% Herbal Fragrance.

Abstract: The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

Abstract: The present invention relates to a therapeutic agent for an ophthalmic disease comprising a vascular endothelial growth factor (VEGF) receptor inhibitor or an epidermal growth factor (EGF) receptor inhibitor in a nanoparticle form, having a property to be retained in a posterior eye tissue when systemically administered.

Abstract: There is disclosed an amorphous solid dispersion of valbenazine tosylate, and a process for preparation.

Abstract: The present invention provides methods for enhancing transmucosal uptake of a medicament, e.g., fentanyl or buprenorphine, to a subject and related devices. The method includes administering to a subject a transmucosal drug delivery device comprising the medicament. Also provided are devices suitable for transmucosal administration of a medicament to a subject and methods of their administration and use. The devices include a medicament disposed in a mucoadhesive polymeric diffusion environment and a barrier environment.

Abstract: Methods are provided for preventing, reducing, and/or treating contrast-induced acute kidney injury which include administering an inhibitor of fatty acid oxidation to a patient in need thereof. Also provided are methods involving use of trimetazidine or pharmaceutically acceptable salts thereof for the prevention and/or treatment of contrast-induced acute kidney injury. Methods are also provided for preventing and/or treating contrast-induced acute kidney injury which include administration of one or more of trimetazidine, etomoxir, oxfenicine, perhexiline, mildronate, or ranolazine, or pharmaceutically acceptable salts of any of the preceding.

Abstract: The present disclosure relates to pharmaceutical combinations comprising a cyclin dependent kinase 4/6 (CDK4/6) inhibitor compound, (b) a mitogen activated protein kinase (MEK) inhibitor compound, and optionally (c) an alpha-isoform specific phosphatidylinositol 3-kinase (PI3K) inhibitor compound, for the treatment or prevention of cancer, as well as related pharmaceutical compositions, uses, and methods of treatment or prevention of cancer.

Abstract: The present invention concerns methods for managing hepatotoxicity in a subject undergoing treatment with a composition comprising an azole inhibitor of the Hedgehog signaling pathway (azole inhibitor), such as itraconazole or an analogue thereof, comprising suspending, for a period of time, the administration of the composition to the subject exhibiting hepatotoxicity, and re-administering the composition to the subject with a reduced dosage of the azole inhibitor.

Abstract: The present invention concerns methods for treating high-risk basal cell carcinoma (BCC) or high-risk basal cell carcinoma nevus syndrome (BCCNS) in a subject, comprising administering a composition comprising an azole inhibitor of the Hedgehog signaling pathway (azole inhibitor) to the subject.

Abstract: A pharmaceutical composition or kit has at least one CXCR4 inhibitor and a multi-tyrosine kinase inhibitor. The composition has at least one CXCR4 inhibitor for use in the treatment of cancer or idiopathic pulmonary fibrosis in a subject suffering from the cancer or idiopathic pulmonary fibrosis and receiving a multi-tyrosine kinase inhibitor therapy. A method for identifying whether a subject suffering from cancer or idiopathic pulmonary fibrosis and receiving a multi-tyrosine kinase inhibitor therapy is susceptible to a CXCR4 inhibitor therapy by determining a CXCR4 signal intensity in a PET dataset obtained from the subject, comparing the CXCR signal intensity to a reference, and identifying whether the subject is susceptible based on the results of the comparison.

Abstract: The present application is directed to a method of sensitizing homologous recombination (HR)-proficient cancer cells to treatment with poly ADP ribose polymerase (PARP) inhibitors. This method involves providing HR-proficient cancer cells and treating the HR-proficient cancer cells with an Ataxia telangiectasia and Rad3-related (ATR) inhibitor under conditions effective to sensitize the HR-proficient cancer cells to treatment with PARP inhibitors, where the treating is carried out without administering PARP inhibitors. This technique can also be used to treat cancer in a subject. Additional methods of treating HR-proficient cancer cells and methods of treating a cancer patient are also disclosed.

Abstract: The present disclosure relates to the field of pharmacy, particularly to a Wt inhibitor and a PD-1 inhibitor for use in the treatment of cancer. Specifically, the disclosure relates to a pharmaceutical combination comprising a Wnt inhibitor, or a pharmaceutically acceptable salt thereof, and a PD-1 inhibitor, or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer, to a method for the treatment of cancer that involves administering the combination and to the use of the combination for the manufacture of a medicament for the treatment of cancer.

Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract: This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof.

Abstract: Described are methods of reducing pulmonary exacerbations and methods of treating cystic fibrosis, including methods of reducing pulmonary inflammation, comprising administration of an LTA4h inhibitor.

Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

Abstract: The present disclosure provides selective phosphoinositide 3-kinase inhibitors of formula (A), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more P13K isoforms, such as PI3K delta (PI3K?). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase inhibitors using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase activity.

Abstract: The present disclosure relates to the use of negative allosteric modulators (NAMs) of the metabotropic glutamate receptor 5 (mGluR5) in the treatment of a mature brain damage, such as damage after stroke.

Abstract: A method of treating cancer in a subject is disclosed. The method comprises administering to the subject a therapeutically effective amount of a Casein kinase I alpha (CKlalpha) inhibitor, wherein the cancer is not associated with an Adenomatous polyposis coli (APC) mutation. Additional uses of CKI inhibitors are also disclosed.

Abstract: Methods of using substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, or compositions, for the treatment of brain cancers, in particular EGFR-mediated metastatic brain cancer, are disclosed.

Abstract: The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of lung cancer and other respiratory conditions.

Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.

Abstract: A method of treating psychosis, and the underlying antipsychotic formulation. The method includes administering a therapeutically effective amount of synthetic agents that selectively recruit ?-arrestin to D2 receptors and have little-to-no binding to culprit receptors associated with weight gain and Type II diabetes. The synthetic agents can include SYA16263 and SYA16264, and/or derivatives or analogs thereof. The 1-(pyridin-2-yl)piperazine moiety was found to play a significant role in recruiting ?-arrestin to D2 receptors. In other embodiments, the current invention relates to synthetic agents that are selective of D4 receptors for treatment of psychosis and erectile dysfunction. The synthetic agents can include SYA27287 and/or derivatives or analogs thereof. In all embodiments, extrapyramidal side effects are eliminated or minimized.

Abstract: The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.

Abstract: Novel HIF inhibitors having low cytotoxicity and suitable for ophthalmologic treatment and agents for the treatment or prevention of ischemic diseases, glaucoma, optic nerve diseases, retinal degenerative diseases, retinal degenerative diseases, angiogenic retinal diseases, cancer, neurodegenerative or autoimmune diseases are provided. The present invention is a therapeutic or prophylactic agent for ischemic disease, glaucoma, optic nerve disease, retinal degenerative disease, retinal degenerative disease, angiogenic retinal disease, cancer, neurodegenerative disease, or autoimmune disease, which comprises as an active ingredient one or more or an extract thereof selected from the group consisting of plants belonging to the genus Asian, plants belonging to the genus Swiss, plants belonging to the genus Grape, plants belonging to the genus Brassica, fish belonging to the genus Kivinago, and so on.

Abstract: A liquid nutritional composition including 5-methyltetrahydrofolic acid (5-MTHF) is provided. The liquid nutritional composition also includes ascorbic acid and a protein system containing methionine to inhibit or reduce oxidation of the 5-MTHF and provide an active folate level of the liquid nutritional composition that remains stable over the shelf life of the liquid nutritional composition.

Abstract: A pharmaceutical composition for neovascular diseases, a pharmaceutical composition for inhibiting an angiogenic growth factor, and use of these pharmaceutical compositions are provided. In one or more embodiments, a pharmaceutical composition contains as an active ingredient a low molecular weight compound that is able to suppress the expression of VEGF gene in cells or to reduce the production of VEGF protein from cells. In one or more embodiments, a pharmaceutical composition contains as an active ingredient a compound expressed by the following formula (I) or a prodrug thereof or pharmaceutically acceptable salts thereof.

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract: The present application provides methods of treating PI3K? related disorders using pyrazolopyrimidine derivatives.

Abstract: Methods of using serum glucocorticoid induced kinase 1 (SGK1) inhibitors for reducing the development of diseases related to salt and water balance, and in particular, hydrocephalus and/or hypertension, are disclosed herein. Particularly, the present disclosure is directed to the use of SGK1 inhibitors to inhibit transepithelial ion transport, such as in one embodiment, in the choroid plexus of a subject, thereby reducing cerebrospinal fluid (CSF) production or, alternatively, in another embodiment, to inhibit transepithelial sodium transport in the kidney collecting duct thereby reducing sodium reabsorption into the blood.