Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.

Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.

Abstract: The present invention relates to modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of preventing, inducing, causing or increasing weight loss, treating obesity and/or treating metabolic syndrome utilizing the modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of improving insulin sensitivity and glycemic control, reducing insulin levels and/or improving leptin sensitivity utilizing the modified or polymer conjugated MetAP2 inhibitors.

Abstract: The invention relates to inhibitors of EZH2 for use in the treatment of cancers characterised by expression of mutated histone H3 having a mutation of amino acid number 27. The invention also relates to methods for predicting the efficacy of treatment of a cancer with an inhibitor of EZH2 by determining whether the cancer cells contain a gene encoding p16INK4A, wherein the presence of a gene encoding p16INK4A is indicative of efficacy of treatment of the cancer with an inhibitor of EZH2.

Abstract: Provided is a solution suitable for oral administration of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof. A solution for oral administration containing compound (I) or a salt thereof, and at least one compound selected from the group consisting of lactic acid, phosphoric acid, glycolic acid, malic acid, tartaric acid, citric acid, succinic acid and acetic acid and having pH 2.5-4.5.

Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.

Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.

Abstract: The present invention provides a method for treating a tumor comprising administering an effective amount of an antibody which specifically binds to human CC chemokine receptor 4, human epidermal growth factor receptor 2, human CD20, or epidermal growth factor receptor, and an indoleamine 2,3-dioxygenase inhibitor to a human in need thereof, and the like.

Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.

Abstract: Embodiments of the present disclosure pertain to methods of inhibiting cancer cells by exposing the cancer cells to a purinergic receptor antagonist that targets one or more purinergic receptors of the cancer cells. The targeted purinergic receptors can include P2 purinergic receptors, such as P2X purinergic receptor subtypes (e.g., P2X3 or P2X5) and P2Y purinergic receptor subtypes (e.g., P2Y2). In some embodiments, the inhibited cancer cells are associated with hepatocellular carcinoma. In additional embodiments, the present disclosure pertains to methods of treating hepatocellular carcinoma in a subject by administering a purinergic receptor antagonist to the subject such that the antagonist targets one or more purinergic receptors of hepatocellular carcinoma cells in the subject. In some embodiments, the subject is a human being suffering from hepatocellular carcinoma.

Abstract: The present invention provides compositions and methods of inhibiting tyrosine phosphorylation. In one aspect, a composition comprising a low-dosage tyrosine kinase inhibitor, where the low-dosage tyrosine kinase inhibitor decreases tyrosine phosphorylation, is provided. In another aspect, a method for treating cardiovascular disease or condition associated with a RASopathy having aberrant protein tyrosine phosphorylation is described. Methods for treating congenital heart disease associated with Noonan or Noonan syndrome with multiple lentigines and decreasing aberrant levels of Protein Zero-Related (PZR) tyrosyl phosphorylation are also described.

Abstract: The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like.

Abstract: The invention provides 3-deuterium-enriched 3-(6-, 7-, or 8-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.

Abstract: Disclosed herein are compositions and methods for transitioning or converting a white adipocyte to a beige adipocyte. The compositions and methods may be used in the treatment of obesity. In some embodiments, the compositions include a compound selected from DC677 and DC761.

Abstract: The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.

Abstract: Disclosed are methods for treating autism spectrum disorders and/or anxiety disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. Anxiety disorders include agoraphobia (with or without panic disorder), generalized anxiety disorder (GAD), social anxiety disorder (SAD), panic disorder (PD), post-traumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD).

Abstract: Inhibiting Akt1 and Akt2 but not Akt3 in a subject has been found to be an effective immune therapy that delays the exhaustion of CD8 T cells, prolongs CD8 T cell survival, preserves a remarkably high percentage of TCM cells, and significantly increases TCM proliferative potential upon reencountering antigen. In a preferred embodiment, the Akt1 and Akt2 inhibitors do not inhibit Akt3. Preferred small molecule inhibitors include, but are not limited to MK-2206, AZD5363, (1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one trifluoroacetate salt hydrate or combinations thereof.

Abstract: The present disclosure is generally directed to bumped kinase inhibitor (BKI) compositions and methods for treating cancer.

Abstract: The present invention relates to a liquid pharmaceutical composition suitable for parenteral administration comprising: a) pemetrexed diacid; b) at least one organic amine; c) at least one antioxidant; d) 10-200 mg/ml of propylene glycol; and e) one or more parenteral solvents, wherein the preparation thereof is conducted in an atmosphere of inert gas and wherein the organic amine(s) is present in an amount sufficient to reach a pH of the composition in the range from 8.3 to 9.1 The invention further relates to the use of said liquid pharmaceutical composition as medicament in the treatment of malignant pleural mesothelioma and non-small cell lung cancer.

Abstract: Described herein are methods for treating a viral infection comprising administering to an individual in need thereof a therapeutically effective amount of a compound of Formula I: Formula (I).

Abstract: The present invention provides a chromone oxime derivative of formula (I), which is a modulator of nervous system receptors sensitive to the neuroexcitatory amino acid glutamate and presents an advantageously high brain exposure upon oral administration, for the treatment or prevention of levodopa-induced dyskinesia. The present invention also provides an improved therapy of Parkinson's disease, using the chromone oxime derivative of formula (I) in combination with ievodopa.

Abstract: Alkaloid compounds described herein are useful for treating disorders associated with monoamine oxidase (MAO) activity, such as depression, pain, smoking cessation, and substance addictions, and/or for treating disorders associated with chronic or low-level inflammation. In some examples, compounds are effective for treating cancers, autoimmune disorders, and other disorders associated with inducible nitric oxide synthase (iNOS).

Abstract: Tricyclic dibenzothiazepine compounds for use in the treatment of CDKL5 disorder. Specifically, a compound of Formula I, or a pharmaceutically or veterinarily acceptable salt thereof, or a pharmaceutically or veterinarily acceptable solvate of either entity for use in the treatment of CDKL5 disorder in a mammal, wherein a compound of Formula I comprises: or a pharmaceutically or veterinarily acceptable salt thereof, or a pharmaceutically or veterinarily acceptable solvate of either entity, wherein: R1 and R3 each independently represent, at each occurrence when used herein, H or C1 to C5 alkyl; R2 represents halo; R4 and R5 each independently represent H; R6 represents —C(O)OR9; X represents CH2, O or S; R9 represents H or C1 to C5 alkyl; and, m is an integer from 1 to 6 inclusive.

Abstract: Pharmaceutical compositions and methods for inducing conscious sedation using such compositions are described, the compositions comprising a benzodiazepine-based compound, a NMDA antagonist, and optionally a ?-blocker, antiemetic, an NSAID, and/or an antihistamine medication. Methods for fabricating the compositions and using them for anesthesiological applications are also described.

Abstract: Prostamide-containing intraocular implants that biodegrade in the eye and that are effective for reducing intraocular pressure in an eye for a sustained period. The implants generally contain a prostamide, such as bimatoprost, and at least three distinct biodegradable polymers selected from polylactide and poly(lactide-co-glycolide) polymers and are optimized for placement in and compatibility with the anterior chamber of the eye, particularly the anterior chamber angle. Methods for making and using the implants to reduce ocular hypertension and intraocular pressure in a patient are described.

Abstract: The present invention discloses scalarane sesterterpenoids represented by formula (I) and meroditerpenoid represented by formula (II), which are extracted from Carteriospongia sp. sponge: where R1 is —CH3 or —C2H5. The compounds of formula (I) can be used to be an anticancer, act as an inhibitor targeting to topoisomerase II and hsp90 and a pharmaceutical composition for anticancer.

Abstract: Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure: is specifically disclosed for the medical treatment and/or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

Abstract: A self-foaming composition is described that includes clobetasol propionate, for a no-rinse topical application and for application to the skin. The composition can include: at least one intermediate composition B including a gas-generating agent; at least one intermediate composition A including an agent for activating the gas-generating agent; and clobetasol propionate being present in at least one of the intermediate compositions A and B. Also described, is a kit or a single container including a plurality of compartments including such a composition.

Abstract: Assay methods for determining purity of a sample of a sterol are provided. These methods include providing an HPLC eluent including a sterol, other compounds related to the sterol and a mobile volatile phase; generating an aerosol of liquid droplets from the HPLC eluent; drying the liquid droplets to obtain residue particles of the sterol; contacting the residue particles of the sterol with an ion stream which applies a size-dependent electrical charge to each of the residue particles to generate an electrical signal and measuring the electrical signal to determine the purity of the sterol in the sample. The sterol can be OXY133 or OXY133 monohydrate.

Abstract: A pharmaceutical composition comprising a cancer therapeutic that is capable of inhibiting and/or reducing the ability of a cancer cell to take up and utilize glucose or other energy source, a lipid or other building block of a cell membrane or organelle, and/or cholesterol. The pharmaceutical composition can comprise one or more cancer therapeutics that can be administered individually or in combination to an individual.

Abstract: A stabilized formulation for controlled release of a vitamin D compound is disclosed. The formulation comprises one or both of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 and a cellulosic compound. The stabilized formulations exhibit a stable dissolution profile following exposure to storage conditions and demonstrate improved pharmacokinetic parameters compared to unstabilized formulations.

Abstract: A stabilized formulation for controlled release of a vitamin D compound is disclosed. The formulation comprises one or both of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3 and a cellulosic compound. The stabilized formulations exhibit a stable dissolution profile following exposure to storage conditions and demonstrate improved pharmacokinetic parameters compared to unstabilized formulations.

Abstract: Embodiments disclosed herein provide compositions and methods for treating lymphangioleiomyomatosis (LAM) comprising inhibiting COX overexpression and prostaglandin over production by administering at least one COX inhibitor and/or prostaglandin biosynthetic pathway inhibitors.

Abstract: Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions, such as arthritis.

Abstract: This disclosure provides methods for the treatment of one or more of: Parkinson's disease (PD); PD symptoms; movement disorders; neurodegenerative diseases linked to changes in dopamine, dopamine signaling, or dopamine expression, in a subject in need thereof comprising administering to the subject an effective amount of an agent that potentiates dopaminergic neurotransmission. Also provided is a method for selecting a candidate agent for the treatment of Parkinson's disease (PD); PD symptoms; and neurodegenerative diseases linked to changes in dopamine, dopamine signaling, or dopamine expression.

Abstract: Disclosed is a combination of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)]phosphate) (NUC-1031) and a platinum-based anticancer agent selected from carboplatin, dicycloplatin, oxaliplatin, satraplatin and nedaplatin. The combinations are useful in the treatment of cancer and particularly ovarian cancer.

Abstract: A solid pharmaceutical composition comprising a solid composition, wherein the solid com-position comprises sofosbuvir and at least one pharmaceutically acceptable matrix compound, wherein at least 99 weight-% of the sofosbuvir comprised in the solid composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, wherein the solid composition contains the sofosbuvir in an amount of at least 25 weight-%, or at least 30 weight-%, or at least 35 weight-%, or at least 40 weight-% or at least 50 weight-% or at least 55 weight-% or preferably at least 5 weight-% based on the combined weight of the sofosbuvir and the at least one matrix com-pound, wherein in the adsorption-desorption isotherm of the at least one pharmaceutically acceptable matrix compound, the desorption mass difference minus the adsorption mass dif-ference at 75% relative humidity and 25° C. is less than 0.

Abstract: The present invention generally relates to therapeutic inhibition of protein arginine methyltransferase 5 (PRMT5). In particular, cell lines having MTAP loss and increased intracellular MTA concentrations show selective dependence on PRMT5. Thus, the invention also relates to methods of identifying and treating PRMT5-related diseases in subjects or tissues which have an MTAP deficiency, alone or in combination, with a second agent that reduces MTAP activity and/or increases intracellular MTA levels, and/or provides an MTA analogs to the cell or tissue. The invention also relates to the Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)-Cas System and components thereof. More specifically, the present invention relates to the delivery, use and therapeutic applications of the CRISPR-Cas systems and compositions in tumor cells ex vivo and/or in vivo. For example using methods disclosed herein, cells can be sensitized to PRMT5 inhibition.

Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

Abstract: Provided are methods of treatment in subjects having progeroid diseases and related conditions which rely upon LMNA-targeted antisense oligonucleotides for reducing expression of one or more aberrantly spliced LMNA mRNA isoforms that encode progerin.

Abstract: The present disclosure provides pharmaceutical compositions comprising nucleic acids capable of targeting IGF-1R expression in M2 cells. The present disclosure also provides methods for the selective reduction of M2 cells by targeting expression of IGF-1R in these cells. The present disclosure further provides methods for treating cancer and enhancing therapeutic by targeting expression of IGF-1R in M2 cells in patients. The pharmaceutical composition of the present invention is effective when administered systemically to subjects in need thereof. The ease of administration of the pharmaceutical composition facilitates treatment and enhances patient compliance.

Abstract: Tumor growth was found to be significantly suppressed in vivo by inhibiting both miRNA containing 5?-AACACUG-3? as a seed sequence and miRNA containing 5?-AAUACUG-3? as a seed sequence. The inhibition significantly altered the proportion of subpopulations of tumor cells and reduced the tumorigenicity in all subpopulations. The inhibition also exerted a remarkable tumor-shrinking effect on already-formed tumors. The present invention provides novel therapeutic potential against tumor.

Abstract: The present invention discloses an Asarum total polysaccharide extract with antitussive activity, an extraction method thereof and an application in the preparation of a medicine for preventing and treating coughs. The present invention proves that the Asarum total polysaccharide extract has a significant effect of suppressing cough for the first time through a large number of pharmacodynamic tests, has the therapeutic effect approximate to codeine, has the effect of prolonging the cough latent period better than codeine, and also finds that the total Asarum polysaccharide extract has the effects of reducing the cough sensitivity and suppressing the airway inflammation for the first time, has excellent preventive and therapeutic effects on various types of coughs, and can be used for preparing the medicines for preventing and treating cough-related diseases.

Abstract: Provided herein is a novel composition for oral administration and delivery of Noble gas, such as xenon or argon. Methods of treating and preventing neuronal or cardiovascular damage with such compositions are also provided.

Abstract: Compositions that include a clay such as kaolin dispersed in a liquid such as water may be useful for promoting the clotting of blood. The compositions may be in a liquid, gel, paste, foam, or another form. Uses may include treating a traumatic injury such as in injury caused by a bullet, an explosive, a blade etc., or an injury caused during a medical procedure such as surgery.

Abstract: A composition of chlorine-free poly-oxygenated metal hydroxide that comprises a clathrate containing oxygen gas molecules, and which may comprise a nutraceutical. In one embodiment, the poly-oxygenated metal hydroxide composition is soluble, and may have particles having a diameter of 212 ?m or less. The poly-oxygenated metal hydroxide may comprise of a poly-oxygenated aluminum hydroxide. The nutraceutical may include one or more of a protein, vitamin, fiber, mineral and electrolytes. The composition may be in a powder or fluid form, where the poly-oxygenated aluminum hydroxide is soluble in the fluid.

Abstract: A method of treating a mammal, comprising administering a therapeutically effective amount of a poly-oxygenated metal hydroxide composition to a mammal to reduce a proliferation of hypoxic carcinoma cells, wherein the poly-oxygenated metal hydroxide composition comprises a clathrate containing free oxygen gas (O2) molecules. The carcinoma cells may comprise lung carcinoma (A549). The poly-oxygenated metal hydroxide material is configured to provide bioavailable oxygen gas molecules to a mammal when administered to the mammal. The poly-oxygenated metal hydroxide composition can be administered intravenously, directly to carcinoma cells, and orally. The composition may comprise a fluid, where the poly-oxygenated metal hydroxide composition is soluble in the fluid.

Abstract: Methods, compounds, and solutions for neurotransmitter restoration in a mammalian brain. The compound comprises calcium carbonate, pyridoxine hydrochloric acid, magnesium citrate, zinc amino acid chelate, chromium amino acid chelate, and a mixture comprising L-Tryptophan, L-Glutamine, L-Tyrosine, DL-Phenylalanine, and rhodiola. A visual indicator may be included to provide a easily discernable indication of the efficacy of a mixed solution.

Abstract: The present invention relates to novel methods of using microporous zirconium silicate to reduce the risk of hyperkalemia and to lower aldosterone levels in the treatment of chronic kidney disease and/or chronic heart disease with therapies comprising diuretics. The invention provides a safe way to reduce the risk of hyperkalemia and to lower aldosterone. The invention also relates to treatment of other conditions that can occur either alone or in connection with hyperkalemia, chronic kidney disease, and/or chronic heart disease.

Abstract: The present invention pertains to the use of the calcium-sensing receptor (CaSR)-activating nutrients (designated as “CaSR-based nutrients”) for the prevention and/or treatment of diarrheal diseases and inflammation in the gastrointestinal tract. In one embodiment, the current invention is formulated for oral administration. The anti-diarrheal composition of the present invention is useful for treating diarrheal and gastrointestinal inflammatory conditions in infants and young children.