Abstract: The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of leukemia.

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: Methods are provided for the treatment of Parkinson's disease (PD) in patients bearing mutations in the LRRK2 gene. A therapeutically effective amount of piperazine derivative compounds are employed to inhibit the biological activity of ArfGAP1, inhibition that counteracts the deleterious effects of mutations in, or increased expression of, the LRRK2 protein.

Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.

Abstract: Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.

Abstract: The present invention relates to a pharmaceutical composition and a therapeutic combination comprising a novel cholesteryl ester transfer protein (CETP) inhibitor and a HMG CoA Reductase inhibitor, which may be used in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia.

Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

Abstract: Aminothiazole compounds of Formula (I) shown below and pharmaceutical compositions containing one of such compounds: Also disclosed are methods of inhibiting a tyrosine kinase and treating cancer associated with a tyrosine kinase with one of the aminothiazole compounds.

Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.

Abstract: Provided are a composition containing an unstable drug against oxidation like pemetrexed with improved stability and a preparation method thereof, by removing oxygen during the preparation without use of an antioxidant. The method is readily applicable for manufacturing by freezing and degassing in a sealed chamber, and can provide formulations with significantly increased stability for the unstable drug against oxidation.

Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.

Abstract: The present disclosure relates to methods for reducing the rate of cardiovascular death, myocardial infarction, or stroke in a patient in recognized need thereof, comprising administering to the patient a pharmaceutical composition comprising 60 mg ticagrelor twice daily.

Abstract: Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

Abstract: A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof

Abstract: Methods for treating insomnia are disclosed. The methods are directed to administering a pharmaceutically effective amount of phosphodiesterase 5 (PDE5) inhibitor to a male individual suffering from insomnia. In addition, due to the PDE5 inhibitor positive effects on addressing erectile dysfunction (ED) in males, the present methods are directed to treating insomnia in patients that also suffer from ED by administering a pharmaceutically effective amount of a PDE5 inhibitor.

Abstract: Carbon monoxide-releasing organic molecules are described herein. The molecules can be synthesized prior to administration (e.g., ex vivo) or formed in vivo. In those embodiments where the molecules are formed in vivo, reactants are administered under physiological conditions and undergo a cycloaddition reaction to form a product which releases carbon monoxide. In applying such reactions for therapeutic applications in vivo, the cycloaddition and CO release typically occur only under near-physiological or physiological conditions. For example, in some embodiments, the cycloaddition reaction and/or release of carbon monoxide occur at a temperature of about 37 C and pH of about 7.4. Pharmaceutical compositions and methods for release carbon monoxide are also described.

Abstract: Described are combination therapies and metabolically-activated drug conjugates and their use in treating cancer in subjects.

Abstract: A composition comprising a drug selected from the group consisting of an arylphenoxypropionate derivative, an aryloxyphenoxyacetate derivative, an aryloxyphenylacetate derivative, a substituted quinol, or a salt, hydrate, or prodrugs thereof, or a combination thereof, in an amount and formulation sufficient to inhibit a mycobacterium is disclosed.

Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.

Abstract: Provided are methods for the combined use of cyclin-dependent kinase 9 (CDK9) inhibitors and bromodomain containing 4 (BRD4) inhibitors to reduce, inhibit and/or prevent cartilage degradation and systemic traumatic inflammation. A combination of CDK9 inhibitors and BRD4 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. A combination of CDK9 inhibitors and BRD4 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.

Abstract: Provided herein is the use of compounds that modulate the activity of inhibitor of apoptosis proteins (IAPs), alone or in combination with other therapeutic agents, in the treatment of human immunodeficiency virus (HIV). Described herein is the use of IAP antagonists in the treatment of human immunodeficiency virus (HIV) in a mammal, alone or in combination with other therapeutic agents used in HIV therapy. In one aspect, provided herein is a method of treating human immunodeficiency virus (HIV) in an individual in need thereof comprising administering a therapeutically effective amount of at least one inhibitor of apoptosis proteins (IAP) antagonist.

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.

Abstract: The present disclosure is directed to methods, compositions, and kits for treating dementia.

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 compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.

Abstract: Doxycycline formulations with a reduced food effect are disclosed. Particularly disclosed are modified release formulations which can be administered once a day and exhibit a reduced food effect. Methods of treating inflammatory conductions such as rosacea or inflammatory symptoms such as the papules and pustules of rosacea or acne vulgaris are also disclosed.

Abstract: A composition containing a macrophage inhibitor may be administered in an effective amount to prevent, inhibit or reduce restenosis, thrombus or aneurysm formation in implanted polymeric vascular grafts. The composition may be administered prior to vascular graft implantation, at the same time as vascular graft implantation, following vascular graft implantation, or any combination thereof. Examplary macrophage inhibitors include bisphosphonates, anti-folate drugs and antibodies, preferably in a controlled release or liposomal formulation.

Abstract: The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.

Abstract: The present invention relates to methods for treating or preventing pulmonary hypertension, reducing mortality in a subject experiencing pulmonary hypertension, or inhibiting ADP-mediated vasoconstriction of pulmonary arteries in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a reversible P2Y12 receptor antagonist. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments.

Abstract: A nutrient composition, a lipid metabolism-improving agent, and prophylactic and/or therapeutic agents typically for inflammatory bowel diseases, immune disorders, cancers, non-alcoholic steatohepatitis, obesity, diabetes, and hypercholesterolemia each contain a cellulose acetate having a total degree of acetyl substitution of 0.4 to 1.1. The cellulose acetate may be one having a compositional distribution index (CDI) of 2.0 or less, where the CDI is defined by the formula: CDI=(Measured value of half height width of chemical composition)/(Theoretical value of half height width of chemical composition) where the measured value of half height width of chemical composition represents a half height width of chemical composition determined by HPLC analysis of a cellulose acetate propionate prepared by propionylating all residual hydroxy groups of the cellulose acetate (sample), and the theoretical value of half height width of chemical composition =2.

Abstract: This disclosure provides mixtures of beta-cyclodextrin molecules substituted at one or more hydroxyl positions by hydroxypropyl groups, the mixture optionally including unsubstituted beta-cyclodextrin molecules, for use as a pharmaceutically active ingredient; methods of making such mixtures; methods of qualifying such mixtures for use in a pharmaceutical composition suitable for intrathecal or intracerebroventricular administration; pharmaceutical compositions suitable for intrathecal or intracerebroventricular administration comprising such mixtures; and methods of using the pharmaceutical compositions for treatment of Niemann-Pick disease Type C.

Abstract: The present invention relates to zirconium silicate compositions having a lead content that is below 0.6 ppm and methods of manufacturing zirconium silicate at reactor volumes exceeding 200-L with a lead content below 1.1 ppm. The lead content of the zirconium silicate of this invention are within the levels that are considered acceptable for extended use given the dose requirements for zirconium silicate.

Abstract: The invention relates to a method for producing eye drops, the thus obtained eye drops and to a kit which comprises the eye drops.

Abstract: Disclosed are compositions and methods relating to the expansion of memory NK cells.

Abstract: The present disclosure provides distinct therapeutic populations of cells that form a pharmaceutical composition useful in hematopoietic stem/progenitor cell transplant. For example, the present disclosure provides a therapeutic population of cells, comprising an enriched population of hematopoietic stem/progenitor cells, memory T cells, regulatory T cells, and wherein the population of cells is depleted of naïve conventional ??-T cells. The present disclosure further provides methods of treatment using the therapeutic population of cells. In other embodiments, the present disclosure provides methods of producing a therapeutic population of cells.

Abstract: The present disclosure provides compositions including a human placental extract and biodegradable microparticles, sustained release angiogenesis-modulating compositions, compositions and methods for releasing a placental extract to a target over a period of time, and methods for inducing and/or modulating angiogenesis and identifying modulators of angiogenesis. The present disclosure also provides methods of making a composition, including a placental extract that can induce and/or modulate angiogenesis.

Abstract: The present invention relates to purified compositions of bee bloom, methods of preparing the purified compositions of bee bloom and the use of bee bloom in the reducing and treatment of inflammation.

Abstract: Provided are methods and compositions for inhibiting or reducing fungal growth in or on a subject. The methods comprise exposing the subject to a composition comprising one or more enzymes, one or more bacteria, and/or an enzymatic extract, wherein the one or more enzymes, one or more bacteria, and/or the enzymatic extract isolated from one or more bacteria are exposed to the subject in a quantity sufficient to inhibit or reduce fungal growth.

Abstract: A method for inhibiting bacterial adhesion of oral pathogens, comprising administering a heat-inactivated Lactobacillus strain to a subject in need to inhibit bacterial adhesion of oral pathogens is disclosed. The Lactobacillus strain is selected from Lactobacillus paracasei GMNL-143, Lactobacillus helveticus GMNL-164 or Lactobacillus rhamnosus GMNL-464. A composition for inhibiting bacterial adhesion of oral pathogens is also disclosed.

Abstract: The invention relates to a gene transfer-based method to protect a subject from diabetes or obesity. The method comprises administering to a salivary gland of the subject an AAV virion comprising an AAV vector that encodes an exendin-4 protein. Also provided are exendin-4 proteins and nucleic acid molecules that encode such exendin-4 proteins. Also provided are AAV vectors and AAV virions that encode an exendin-4 protein. One embodiment is an exendin-4 protein that is a fusion protein comprising an NGF secretory segment joined to the amino terminus of an exendin-4 protein domain.

Abstract: The present invention is related to the use of a virus, preferably an adenovirus, for the manufacture of a medicament, whereby the virus is replication deficient in cells which do not have YB-1 in the nucleus, and the virus codes for an oncogene or oncogene product, in particular an oncogene protein, which transactivates at least one viral gene, preferably an adenoviral gene, whereby the gene is selected from the group comprising E1B55kDa, E4orf6, E4orf3 and E3ADP.

Abstract: A process for extracting antioxidants from a plant, including contacting a plant material from a guayusa plant for a first time with a solvent, thereby obtaining a first slurry, filtering said first slurry, thereby obtaining a first extract, contacting said plant material for a second time with said solvent, thereby obtaining a second slurry, filtering said second slurry, thereby obtaining a second extract, combining said first extract and said second extract, thereby generating an third extract containing at least antioxidants, xanthines, and amino acids, and substantially drying said third extract.

Abstract: A Chinese medicine composition for treating leukemia bone marrow transplant failure complicated by brain stem stroke after chemotherapy, wherein the composition is prepared by the following steps: (A) providing a mixture; (B) mixing the mixture with water and heating the mixture to obtain a crude extract; and (C) filtering the crude extract to remove a residue and obtain a liquid extract; wherein the mixture comprises Fructus corni, Rehmannia glutinosa, Rhizoma dioscoreae, Angelica sinensis, Cortex eucommiae, Semen cuscutae, Fructus lycii, Cinnamomum cassia, Radix aconiti lateralis preparata, Rhizoma zingiberis, Poria, Cortex phellodendri, Radix achyranthis bidentatae, and Atractylodes lancea.

Abstract: A pharmaceutical composition or dietary supplement is described that is effective in the treatment and prevention of urinary tract infections, comprising a combination of D-mannose, proanthocyanidins, hydroquinone derivatives and zinc.

Abstract: The extract of Vicia faba beans is prepared by soaking beans in distilled water overnight and then boiling in a water bath to reduce the volume of aqueous extract, which is then homogenized and filtered. The filtrate is concentrated to a smaller volume, lyophilized, and powdered. The lyophilized powder is extracted with hexane to remove oils and lipids. The oil-free lyophilized powder is dissolved in ethanol solvent and extracted for eight hours under reflux, and filtered. The volume of ethanol is reduced by a rotary evaporator, and a first off-white precipitate (sample A-1) is collected, washed with ethanol, and dried at 80° C. Mass spectrometry shows a molecular weight of 200.16447 g mol?1, and an empirical formula of C9H16N2O3 is assigned. Intraperitoneal injection of mice with 50 mg/kg of A-1 twenty minutes prior to injection with strychnine protected the mice from strychnine-induced convulsions to the same extent as phenobarbitone (phenobarbital).

Abstract: Embodiments of the invention generally relate to methods and supplements for increasing, enhancing, or maintaining fertility in a human being.