Abstract: Treatment of intrahepatic cholestatic diseases by therapy with MBX-8025 or an MBX-8025 salt.

Abstract: Methods and compositions for use in treating, attenuating, preventing or improving liver fibrosis in a subject are described. The compounds of the present invention are gamma-ketoaldehyde scavengers.

Abstract: A pharmaceutical gel composition for intra-intestinal administration comprises (i) a dopamine replacement agents, (ii) a dopamine decarboxylase inhibitor (DDI), and (iii) a COMT inhibitor.

Abstract: The present invention relates to the field of medicine, in particular of oncology. Especially, it provides new compounds useful in the treatment of various cancers. The present invention relates more particularly to methods for the treatment of cancer with IL4I1 expressing cells.

Abstract: The present invention relates to a composition for preventing or treating a muscular disease or improving muscle function. The composition includes suberic acid or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: The present invention relates to compositions comprising one or more extracts and/or compounds having retinol-like activity and properties and methods of using the compositions to treat the eye.

Abstract: The present invention relates to compositions comprising one or more extracts and/or compounds having retinol-like activity and properties and methods of using the compositions to treat the eye.

Abstract: A production of a drug, wherein the drug is specific for SH-SY5Y neuroblastoma cancer by loading caffeic acid phenethyl ester (CAPE) to a plurality of microvesicles that a specialized skin cell leaves into a nutrient solution. The objective of the present invention is to provide a cell-specific targeted vesicle development by loading the CAPE to the plurality of microvesicles obtained as a result of culturing and subsequent specialization of a plurality of tissue cells; and to use the CAPE at lower concentrations compared to a state of the art applications to minimize a toxicity of the CAPE to both a plurality of cells other than a plurality of targeted cells and a body.

Abstract: Induced Pluripotent Stem Cell (iPSC) technology enables the generation and study of living brain tissue relevant to Parkinson's disease (PD) ex vivo. Utilizing cell lines from PD patients presents a powerful discovery system that links cellular phenotypes observed in vitro with real clinical data. Differentiating patient derived iPSCs towards a dopaminergic (DA) neural fate revealed that these cells exhibit molecular and functional properties of DA neurons in vitro that are observed to significantly degenerate in the substantia nigra of PD patients. Clinical symptoms that drive the generation of other relevant cell types may also yield novel PD specific phenotypes in vitro that have the potential to lead to new therapeutic avenues for patients with PD.

Abstract: Provided herein are methods of treating multiple sclerosis with a fumarate, wherein the fumarate is a dialkyl fumarate, a monoalkyl fumarate, a combination of a dialkyl fumarate and a monoalkyl fumarate, a prodrug of monoalkyl fumarate, a deuterated form of any of the foregoing, or a pharmaceutically acceptable salt, clathrate, solvate, tautomer, or stereoisomer of any of the foregoing, or a combination of any of the foregoing. The methods provided herein improve the safety of treatment by informing and monitoring patients undergoing treatment regarding progressive multifocal leukoencephalopathy, and/or by monitoring lymphocyte count.

Abstract: This document relates to a composition comprising Docetaxel, human serum albumin, and one or more amino acids selected from aspartic acid, glutamic acid, and cysteine, wherein the human serum albumin and the Docetaxel in the composition have a ratio by weight of no less than 60:1. This document also relates to a composition comprising Docetaxel, human serum albumin, one or more amino acids selected from aspartic acid, glutamic acid, and cysteine, and a sugar alcohol or a sugar, wherein the human serum albumin and the Docetaxel in the composition have a ratio by weight of no less than 60:1.

Abstract: A pharmaceutical composition comprises a taxane (e.g., paclitaxel, docetaxel, cabazitaxel, larotaxel, ortataxel, and/or tesetaxel) in a mixture of first and second surfactants. The absorption of the taxane is increased from the pharmaceutical composition is greater than the sum of the absorption of docetaxel from either the first or the second surfactant. The increase in absorption is especially enhanced when the ratio of the first surfactant to the second surfactant in the pharmaceutical composition is between 60:40 and 85:15 by weight, and the total surfactant weight does not exceed 98% of the total weight. Polysorbate 80, polysorbate 20, and caprylocaproyl polyoxylglycerides serve as suitable first surfactants, and polysorbate 80 or polyethyoxylated castor oil serve as suitable second surfactants. The stability of the pharmaceutical composition may be enhanced by further including a stabilizer (e.g., citric acid and/or ascorbic acid).

Abstract: This application describes compounds and methods that can be used to treat, reverse, or avoid hyperalgesia.

Abstract: The present disclosure relates to cannabinoid-based therapeutics, and their use in treating pain, e.g., chronic pain. The present disclosure also relates to cannabinoid-based therapeutics, and their use in treating opioid addiction.

Abstract: Provided is a method for treating conditions and/or symptoms associated with a stressful event, comprising administering to a subject in need thereof a therapeutically effective amount of a composition comprising at least one cannabinoid; at least one terpene selected from the group consisting of Pinene, Myrcene, Caryophyllene, Humulene, Nerolidol, Bisabolol, Linalool, Fenchol, Limonene, Terpinene, Terpineol, Eucalyptol, geraniol and combinations thereof, wherein said at least two terpenes are present in the composition at a concentration of at least about 40 wt %, based on the weight of the total amount of terpenes in the composition and at least 5% by weight of a non-cannabinoid, non-terpene carrier.

Abstract: A pouch designed for administration of an active ingredient in the oral cavity is disclosed, the pouch containing a matrix composition having a combination of an amount of one or more cannabinoids and a water-insoluble composition. Also, pouches for use as a medicament, for use in alleviation of pain, and for use in mitigation of appetite deficiency are disclosed. Further, a method of alleviation of pain and a method of mitigation of appetite deficiency using the pouch are disclosed.

Abstract: Disclosed herein is a method for treating tumor, comprising administering a liposomal composition comprising eribulin or a pharmaceutically acceptable salt thereof and a PD-1 antagonist to a patient in need thereof

Abstract: Dosing regimens and methods are disclosed for upregulating protein kinase C (PKC) while reducing subsequent downregulation, comprising administering a PKC activator once a week for three consecutive weeks followed by cessation of administration or dosing for three consecutive weeks. Also described are methods for improving or enhancing cognitive ability, preventing or treating cognitive impairment, preventing or treating a neurodegenerative disease or condition, and/or preventing or treating a disease or condition associated with neuronal or synaptic loss according to the disclosed regimens.

Abstract: The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

Abstract: The present invention relates to a controlled release formulation comprising the active compounds tesofensine and a beta blocker, such as metoprolol or carvedilol, or a pharmaceutically accetpable salt thereof. The invention further relates to use of the controlled release formulation in a method of treatment of diabetes, obesity, or an obesity associated disorder.

Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.

Abstract: Disclosed are compositions containing (a) a purified toad secretion tryptamines chosen from the following 5-MeO-DMT, 5-MeO-NMT, 5-Methoxytryptamine, bufobutanoic Acid, bufobutarginine, bufoserotonin A, bufoserotonin B, bufoserotonin C, bufotenidine, bufotenin, bufotenin Oxide, bufotenine-O-Sulphate, bufoviridine, dET, dMT, n-Acetylserotonin, n?-Formylserotonin, n-Methylserotonin, o-Methylbufoviridine, serotonin, tryptamine, and bufopyramide or the salts of these toad secretion tryptamines and (b) a second active compound selected from a serotonergic drug, a purified psilocybin derivative, a purified cannabinoid, or a purified terpene. The disclosure also relates to formulations, including pharmaceutical formulations, of such a composition and an excipient. Also disclosed are methods of regulating the activity of a neurotransmitter receptor and methods of treating a psychological disorder, a compulsive disorder, or a depressive disorder.

Abstract: Compositions and methods for treating a range of Central Nervous System (CNS) disorders and diseases such as amyloidosis, protein folding diseases, tauopathy, and specifically Alzheimer's Disease and Parkinson's Disease, among others, in humans and in veterinary animals, by administering to a subject in need thereof a formulation comprising of melatonin, curcumin and cannabis, specifically THC alone or with CBD.

Abstract: The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract: The invention relates to a new class of compounds targeting COX-1. The invention also relates to the use of some of such compounds as a tool to investigate the structure and function of the enzyme, in the treatment targeting COX-1 or detection of COX-1 in relating disorders or diseases such as cancer and neuroinflammation, in particular in neurological (e.g. autism spectrum disorders) and neurodegenerative diseases (e.g. Alzheimer's diseases, Parkinson's diseases, amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), traumatic brain injury (TBI), HIV dementia and prion diseases), and in gynecological tumor (e.g. ovarian cancer), neck and head tumor, and haematological tumors (e.g. multiple myeloma) and in the detection of COX-1 in “in vitro” (cells and tissues) and in “in vivo”.

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract: The present invention relates to a new use of compounds that are angiotensin II (Ang II) agonists, more particularly agonists of the Ang II type 2 receptor (the AT2 receptor), and especially agonists that bind selectively to the AT2 receptor, for the prevention or treatment of muscular dystrophy or complications associated with muscular dystrophy.

Abstract: Compositions and methods are provided that are useful for diagnosing, treating, and monitoring alcohol dependence and disorders, susceptibility to alcohol dependence disorders, as well as drug related dependence and disorders. The methods include treating patients with an antagonist of the serotonin receptor 5-HT3 for such disorders, wherein the patient's serotonin transporter gene SLC6A4 is known to have particular genotypes.

Abstract: The present invention relates to a liquid pharmaceutical formulation, which is stable at room temperature, being essentially free of water, comprising a) at least one easily degradable active pharmaceutical ingredient, b) at least one pharmaceutically acceptable organic solvent and c) at least one pharmaceutically acceptable alkaline earth metal salt and its use in medicine.

Abstract: In one aspect, the disclosure relates to compositions and methods for dispersing exiting Salmonella biofilms and inhibiting formation of Salmonella biofilms. In various aspects, the disclosed compositions can be used in methods of treating a persistent Salmonella infection, including an asymptomatic infection. Such infections can colonize a variety of tissues, including the gall-bladder. Also disclosed are methods of treating typhoid fever. Also disclosed are methods for mitigating or preventing secondary outbreaks of typhoid fever by treating asymptomatic subjects who had been symptomatic for typhoid fever at a previous time. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Abstract: Disclosed are methods of treating ataxia by administering to a patient in need thereof a riluzole prodrug such as troriluzole. Pharmaceutical compositions and kits including the riluzole prodrugs are also disclosed.

Abstract: The present disclosure provides novel methods for treating or preventing amyotrophic lateral sclerosis (ALS), methods for delaying the onset of neurological symptoms associated with ALS, increasing survival in subjects afflicted with ALS, and attenuating the decline of muscle strength associated with ALS in a subject in need thereof. The present disclosure also provides methods for treating or preventing ?-synucleinopathy or TDP-43 proteinopathy. The methods comprise administering to the subject an effective amount of a mitochondria-targeting peptidomimetic compound, such as (R)-2-amino-N—((S)-1-(((S)-5-amino-1-(3-benzyl-1,2,4-oxadiazol-5-yl)pentyl)amino)-3-(4-hydroxy-2,6-dimethylphenyl)-1-oxopropan-2-yl)-5-guanidinopentanamide, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, and/or solvate thereof.

Abstract: Methods and dosing regimens for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof and at least one or more other therapeutic agent.

Abstract: The present invention includes compositions and methods for treating a subject afflicted with a neurodegenerative disorder or disease by determining that the subject is in need of treatment for the neurodegenerative disorder or disease; and administering to the subject an amount of an effective amount of a compound comprising a flupirtine derivative as disclosed herein.

Abstract: Provided herein are, inter alia, amphiphilic thiol compounds and methods of using the same for the purpose of depalmitoylating proteins in cellular membranes (e.g., plasma membranes). The compounds provided herein include an amphiphilic tail, which enables them to associate with a cellular membrane and depalmitoylate (cleave native S-palmitoyl groups from) a protein in said membrane by native chemical ligation thereby triggering the protein's release from the plasma membrane. The compounds (amphiphilic thiol compounds of formula (I), (II), (III)) are, inter alia, useful for the treatment of diseases caused or associated with aberrant depalmitoylation of certain proteins (e.g., HRas, EGFR).

Abstract: Disclosed are methods and compositions for the treatment of a proliferative disorder characterized by increased expression of the FOXM1 gene. Exemplary disorders include adenocarcinoma, melanoma, rhabdomyosarcoma, non-small cell lung cancer (NSCLC), head and neck squamous carcinoma, hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma, colon carcinoma, basal cell carcinoma, infiltrating ductal breast carcinoma, anaplastic astrocytoma, glioblastoma, pancreatic carcinoma, gastric cancer, acute myeloid leukemia, lung cancer, liver cancer, breast cancer, prostate cancer, a brain cancer. Kits and articles of manufacture comprising compositions for such treatment are also disclosed.

Abstract: The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.

Abstract: A method of inhibiting a rise in intraneuronal calcium concentration includes administering an effective amount of a cyclic amine derivative represented by formula (I) or a pharmacologically acceptable salt thereof to a subject in need thereof: wherein A represents formula (IIa), (IIb) or (IIc):

Abstract: The present invention provides methods for treating onychomycosis. In certain embodiments, the methods comprise comprising applying a pharmaceutically acceptable formulation containing 10% efinaconazole once a day for a treatment period of at least 36 weeks to the treatment area of an onychomycosis patient (a) without debriding the nail or nail-associated tissue initially or during the treatment period and/or (b) without removing the formulation from the treatment area during the treatment period. In certain embodiments, the formulation also comprises, water, cyclomethicone, diisopropyl adipate, alcohol, C12-15 alkyl lactate, butylated hydroxytoluene, citric acid anhydrous, and disodium edetate.

Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

Abstract: The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of elacridar with superior pharmacokinetic properties such that it is now possible to facilitate accumulation and distribution of therapeutic agents to effective levels in cells or compartments protected by efflux transporter proteins such as Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP). Such transporter protected compartments include brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, stem cells, and solid tumors. In other embodiments, the present invention comprises methods of using the instant deuterated analogs.

Abstract: Methods of using glucagon-like peptide 1 receptor (GLP1R) agonists are generally disclosed herein. In certain aspects, the disclosure provides methods of treating type 2 diabetes that include administering a GLP1R agonist according to certain dosage regimens. In certain other aspects, the disclosure provides methods of treating obesity that include administering a GLP1R agonist according to certain dosage regimens. In certain other aspects, the disclosure provides methods of lowering glycated hemoglobin (for example, lowering HbA1c) that include administering a GLP1R agonist according to certain dosage regimens. Compositions containing GLP1R agonists and their manufacture, for example, for use as a medicament are also disclosed herein.

Abstract: The invention is directed to pharmaceutical compositions comprising dextromethorphan and methods of use thereof. Formulations of the present invention include dextromethorphan or a pharmaceutically acceptable salt thereof in a sustained release formulation comprising a controlled release agent. Formulations of the present invention include a core tablet, optionally an active coating and, optionally a film coating. The pharmaceutical compositions may be used as an antitussive, and the invention further relates to the treatment of cough in a patient in need thereof.

Abstract: The present invention relates generally to methods of using nalmefene for treating and/or preventing demyelinating disease in a subject, and in particular for treating and/or preventing multiple sclerosis (MS). Also disclosed is nalmefene for use in treating and/or preventing MS as well as pharmaceutical compositions and unit dosage forms comprising nalmefene for use for treating and/or preventing demyelinating disease in a subject, and in particular for treating and/or preventing MS.

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: Therapeutic treatments for a disease such as a cancer are disclosed, including pharmaceutical compositions and methods of using pharmaceutical compositions for treating the cancer wherein the cancer cells overexpress arginine methyltransferase CARM1. In some embodiments, the therapeutic treatments disclosed include methods comprising the step of administering a therapeutically effective dose of an enhancer of zeste homolog 2 (EZH2) inhibitor to a subject, including a human subject, wherein the cancer cells of the subject overexpress arginine methyltransferase CARM1 and a PARP inhibitor. In some embodiments, the EZH2 inhibitors are CA administered in conjunction with platinum-based antineoplastic drugs.

Abstract: This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.

Abstract: Provided is a pharmaceutical composition comprising an effective amount of itraconazole, and a pharmaceutically acceptable excipient. The use of the pharmaceutical composition for treatment of idiopathic pulmonary fibrosis is also provided.

Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are tyrosine analogues derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).