Abstract: The present invention provides methods of treating hematological disorders and solid malignant tumors, using substituted indazole compounds and pharmaceutically acceptable salts thereof. The compounds inhibit IRAK4 and BCL-2 kinases.

Abstract: It is intended to provide a drug, a quasi-drug, a dermatological preparation for external use, or a material to be contained to drugs, quasi-drugs, dermatological preparations for external use, food products, or the like which has an excellent UCP-1 expression-promoting action and promotes conversion of adipose to brown adipose (browning). The present invention provides a UCP-1 expression promoter comprising a PPAR? activator and a Smad3 inhibitor in combination. The present invention also provides a UCP-1 expression promoter comprising a PPAR? activator, a Smad3 inhibitor, and a ?3 adrenaline receptor activator or a TGR5 activator in combination.

Abstract: Nanoparticle based MKT formulation. MKT is encapsulated by poly(ethylene glycol)ylated (PEGylated) poly-(lactide-co-glycolide) (PLGA) to form nanoparticles (NPs). To induce trans-BBB permeability, glutathione (GSH) is coated on the resulting NPs. Newly generated MKT-NPs showed BBB permeability and tau reduction in experimental models. Specifically, brain-targeting MKT NPs were developed with a glutathione coating, characterized, and shown to permeate BBB permeation insert models as a therapeutic for Alzheimer's disease and related tauopathies.

Abstract: The invention relates to a molecule enabling removal of neurotoxicity observed in neuron cells due to various reasons.

Abstract: The invention is directed to a method of inhibiting, within a living cell, the interaction between NF-?B essential modulator (“NEMO”) with I?B kinase-? (IKK-?) at the NEMO binding domain (NBD), comprising exposing the cell to an effective amount or concentration of a compound of the invention, a NEMO-binding domain analog (NBDA). The invention is further directed to a method of treating a condition in a patient, wherein inhibiting the interaction between NF-?B essential modulator (“NEMO”) with I?B kinase-? (IKK-?) at the NEMO binding domain (NBD) is medically indicated, comprising administering to the patient an effective dose of a compound of the invention. Conditions that can be treated by a method of the invention includes muscular dystrophy, asthma, inflammatory bowel disease, multiple sclerosis, Parkinson's Disease, arthritis, diabetes, graft versus host disease, accelerated aging, heart ischemia, cancer, UV-induced skin damage, or an age-related pathology.

Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.

Abstract: The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises piperlongumine (PL) or derivative thereof. The selective killing of senescent cells may delay aging and/or treat age-related disorders.

Abstract: The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

Abstract: The present invention provides, inter alia, methods for treating or ameliorating the effects of a disease, such as cancer in a subject. The methods include: administering to a subject in need thereof (a) a therapeutically effective amount of a molecularly targeted agent; and (b) a therapeutically effective amount of a monoclonal antibody or antigen binding fragment thereof, wherein the monoclonal antibody contains: (i) a heavy chain variable region (VH), which includes an amino acid sequence selected from SEQ ID NO:1, SEQ ID NO:3, SEQ ID NO:5, and SEQ ID NO:7; and (ii) a light chain variable region (VL), which includes an amino acid sequence selected from SEQ ID NO:2, SEQ ID NO:4, SEQ ID NO:6, and SEQ ID NO:8. Compositions, including pharmaceutical compositions, and kits for treating diseases, such as cancer, are also provided herein.

Abstract: The invention relates a composition comprising an opioid agonist and Compound-1:

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprises administering to the subject in need thereof, a therapeutically effective amount of azaquinone or a pharmaceutical composition consisting of clofazimine or a clofazimine analogue, azaquinone, and at least one pharmaceutically acceptable excipient. Pharmaceutical compositions comprising a therapeutically effective amount of azaquinone or consisting of clofazimine or a clofazimine analogue, azaquinone, and at least one pharmaceutically acceptable excipient are provided for treating Clostridium difficile infection and diseases or symptoms associated therewith.

Abstract: Described herein are carboxamide derivatives that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity. Such carboxamide derivatives form bicyclic and tricyclic ring systems and the disease or condition associated with RSK activity in a mammal is cancer.

Abstract: Methods for treating HIV or AIDS in a human are provided using two drug regimens comprising a bictegravir and rilpivirine, as well as compositions containing such compounds.

Abstract: Disclosed herein are pharmaceutical compositions, devices, their combinations, and their uses thereof for example in treating or preventing headaches.

Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

Abstract: The present invention provides a therapeutic drug that is useful for levodopa induced dyskinesia in Parkinson's disease. In particular, the present invention provides a composition and method for treating, improving, suppressing the progression, or preventing motor complications associated with levodopa therapy for Parkinson's disease, especially levodopa induced dyskinesia (PD-LID), comprising tandospirone or a pharmaceutically acceptable salt or prodrug thereof, wherein the tandospirone or a pharmaceutically acceptable salt or prodrug thereof is parenterally administered.

Abstract: The present application discloses a method of treating a Varicella-Zoster Virus (VZV) infection in an individual in need thereof, including the step of administering to said individual an effective Varicella-Zoster Virus antiviral amount of a compound called N-methanocarbathymidine (N-MCT), which has a northern configuration with the structure as follows

Abstract: The invention provides methods and compositions that are useful for treating allergic diseases, bacterial infections, fungal infections, viral infections, mastocytosis, mast cell-mediated inflammation and parasite infections (e.g., helminth infections).

Abstract: The present subject matter relates to a compound represented by the general formula (I) or (I?) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).

Abstract: Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.

Abstract: Provided herein are methods of treating focal segmental glomerulosclerosis, said methods include administering to a subject in need thereof a therapeutically effective amount of a CCR2 antagonist. In some embodiments, the CCR2 antagonist is used in monotherapy. In some embodiments, the CCR2 antagonist is used in combination therapy. In some embodiments, the additional therapeutic agent is a RAAS blocker and/or an endothelin receptor inhibitor. The CCR2 antagonist may have the structure of formula (I).

Abstract: This application relates to methods of treating and/or preventing cancer (e.g., non-small cell lung cancer, renal cell carcinoma, hepatocellular carcinoma, thyroid carcinoma, colorectal cancer, gastrointestinal stromal tumors, breast cancer, prostate cancer, pancreatic cancer, or thymoma) in patients in need thereof comprising administering to the patient a therapeutically effective amount of a CDK inhibitor (e.g., milciclib) in combination with a therapeutically effective amount of another anticancer drug (e.g., sorafenib, lenvatinib, regorafenib, sunitinib, nivolumab, gemcitabine, and palbociclib).

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: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.

Abstract: Provided herein is a pharmaceutical composition comprising two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a ?2-adrenoreceptor agonist. Also provided herein is a method of treating, preventing, or ameliorating a cardiovascular disease in a subject, comprising administering to the subject in need thereof two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a ?2-adrenoreceptor agonist.

Abstract: Disclosed is a method of treating a subject who has a neurological disease. The neurological disease may be associated with altered C9ORF72 protein activity. In one aspect, the method includes a step of administering an effective dose of a pharmaceutical composition to a subject in need thereof, thereby rescuing the defects associated with altered C9ORF72 protein activity. Also described are methods for identifying a compound for inhibiting motor neuron degeneration.

Abstract: The present invention provides a transdermal delivery system, which comprises a drug-containing matrix layer comprising: galantamine or its pharmaceutically acceptable salt as an active ingredient; and a styrene-butadiene-styrene copolymer or a styrene-isoprene-styrene copolymer as an adhesive.

Abstract: Provided are inclusion complexes comprising fulvestrant and a cyclodextrin. The complexes may be useful for treating various conditions, such as cancer and systemic lupus erythematosus. Also provided are methods of producing the inclusion complexes, methods of using the inclusion complexes in therapy, and kits and unit dosages comprising the complexes.

Abstract: The present invention relates to methods and pharmaceutical compositions for treating peripheral demyelinating diseases. In particular the present invention relates to a method of treating a peripheral demyelinating disease in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an inhibitor of VDAC1 activity or expression.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: The present invention relates to a method of treating allergic rhinitis in a subject (e.g., a pediatric human subject) in need thereof comprising nasally administering to the subject an effective amount of a fixed-dose pharmaceutical composition comprising mometasone or its salt and olopatadine or its salt.

Abstract: It was discovered that NF-?B signaling pathway plays a central role in pancreatitis, and inhibition of NF-?B signaling has the potential to reduce the incidence of pancreatitis and protect pancreatic tissues from inflammatory damage. Aspects of the disclosure relate to a method for inhibiting or treating pancreatitis in a subject in need thereof comprising administering a therapeutically effective amount of an NF-?B signaling pathway inhibitor to the subject.

Abstract: The present invention relates to a new pharmaceutical composition containing a combination of 5-aminosalicylic acid and nicotinamide or related compounds. The combination is believed to beneficially influence the intestinal microbiota and/or reduce gastrointestinal inflammation. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.

Abstract: The invention relates to a halogenated salicylanilide selected from closantel, rafoxanide, oxyclozanide and niclosamide and derivatives thereof including salts, hydrates, esters and the like for use in the topical treatment or prevention of infections caused by Gram-positive bacteria such as Staphylococcus, in particular Staphylococcus aureus, and Streptococcus, in particular Streptococcus pyogenes. Grain positive bacteria treated with the halogenated salicylanilides exhibit a very low frequency of appearance of resistant mutants compared to commonly used topical antibiotics.

Abstract: An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

Abstract: The present invention relates to a composition comprising at least one fucosylated oligosaccharide, for use in preventing allergies and/or treating allergies and/or reducing the occurrence or the risk of allergies in an infant or a young child born from a mother deficient in at least one fucosylated oligosaccharide(s) or fed with a mother's milk deficient in at least one fucosylated oligosaccharide(s). The use of said composition in infant formula, milk fortifier or children's food is foreseen.

Abstract: The present invention relates to antibody drug conjugates (ADCs) presenting improved properties of in vivo tolerability.

Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: Provided herein are hybrid oligonucleotides comprising a region that promotes cleavage of a nucleic acid and a region that protects a nucleic acid from exonuclease activity. Such hybrid oligonucleotides are useful for modulating the expression of genes. Related compositions and methods are also provided. In some embodiments, methods are provided for treating a disease, such as by administering a hybrid oligonucleotide.

Abstract: Diabetic wounds have elevated levels of cathepsin K, a protease enzyme, which degrades proteins, such as collagen, causing delayed wound healing. By targeting cathepsin K, diabetic wound healing is ameliorated. Methods and devices for treatment include topical application of pharmacological inhibitors of cathepsin K, for example, in the form of gel, powder, or bandage. Other methods and systems include localized genetic knock out of the cathepsin K gene by topical application of a small interfering RNA (siRNA) or antisense oligonucleotide to aid in wound healing.

Abstract: Neuregulin-1 (NRG1) or a fragment thereof or vitamin B12 for use in maintaining or increasing muscle function and/or mass in an ageing subject, and/or substantially preventing or reducing muscle wasting in an ageing subject.

Abstract: Disclosed are compositions comprising synergic combinations of xyloglucans and plant or animal proteins, which are useful in the treatment of intestinal disorders.

Abstract: A supplement for preventing and/or treating gastrointestinal distress, including ulcer conditions, in animals is disclosed. The supplement is in a gel form and comprises mastic gum and an emulsifying agent such as lecithin. The supplement may also comprise a vegetable oil, B vitamins, one or more prebiotics or probiotics, and one or more minerals as well as, pH buffers and flavoring. The amount of mastic gum is from about 1 to about 6 grams per 10 cubic centimeters of gel.

Abstract: The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a colon release coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: A method for synthesizing high purity montmorillonite is disclosed. According to this synthesis method, bentonite is dissolved in aqua regia to produce a solution and then sodium hydroxide (NaOH) is added to the solution to produce a mixed solution. Then, the mixed solution is kept in a sealed state at a temperature of 90° C. inclusive to 100° C. exclusive to synthesize montmorillonite crystals.

Abstract: The present invention provides compositions comprising amorphous calcium carbonate (ACC), suitable to being administered by inhalation, and methods for their use in treating ACC-responsive diseases and conditions. Further provided are ACC compositions suitable for buccal or sublingual administration.

Abstract: Stabilized amorphous calcium carbonate (ACC) for treatment of several neurological, muscular and infertility diseases and conditions is provided. In particular, the stabilized ACC may be used in the treatment of axonal defects and muscular dystrophy. In addition, provided are improved methods used in assistant reproductive technology. Examples of such methods are in vitro fertilization and improvement of sperm quality. The improved IVF method, for example, comprises addition of the stabilized ACC to the cell culture medium in which the stages of fertilization and embryo development occurs.

Abstract: The disclosure concerns a method for cancer treatment by in vivo priming and activation of natural killer cells for achieving tumor cell lysis. The method includes introducing into a patient a priming tumor cell preparation (PTCP) derived from a first tumor cell line, which is irradiated to inactivate the first tumor cells or a membrane preparation thereof, the first tumor cells having known priming ligands on the membrane surface thereof. The patient's rest NK cells are contacted by the PTCP in vivo, resulting in primed NK cells, which are characterized by upregulation of CD69, shedding of CD16, or a combination of CD69+ and CD16?. These primed NK cells then contact second tumor cells, the cancer, and are configured to lyse and kill the second tumor cells.