Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.

Abstract: The present invention relates to products and methods for treatment of narcotic dependence in a user. The invention more particularly relates to self-supporting dosage forms which provide an active agent for treating narcotic dependence while providing sufficient buccal adhesion of the dosage form.

Abstract: The present invention relates to methods and compositions for the treatment or prevention of diseases and disorder associated with myeloproliferative and lymphoproliferative disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing diseases and disorder associated with myeloproliferative and lymphoproliferative disorders.

Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.

Abstract: Disclosed are methods for treating a meylodysplastic syndrome (MDS) in a subject that involves administering to the subject a therapeutically effective amount of a protein phosphatase 2A (PP2A) inhibitor.

Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

Abstract: Disclosed herein are analogues of itraconazole that are both angiogenesis and hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.

Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.

Abstract: The invention includes compositions comprising NSC59984 or a derivative or analogue thereof and a pharmaceutically acceptable carrier. The invention further includes methods of treating or preventing cancer in a subject, comprising the step of administering to the subject the compositions contemplated within the invention.

Abstract: The present disclosure provides methods and compositions for treating or preventing erythema, including rebound erythema associated with the use of topical alpha-adrenergic agonists. In certain embodiments, an effective amount of a capsaicinoid, such as capsaicin or a pharmaceutically acceptable salt or derivative thereof, is administered to a subject.

Abstract: Certain adjunctive therapies comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent for treating HIV-related disorders are provided herein. These disorders include AIDS dementia complex, AIDS-induced encephalopathy, HIV-associated neurocognitive disorder, asymptomatic neurocognitive impairment, minor neurocognitive disorder, minor cognitive motor disorder, vacuolar myelopathy, peripheral neuropathies, and polymyositis. Also provided are pharmaceutical compositions comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent.

Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegenerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.

Abstract: The present invention provides ligands which bind to MR1, some of which induce MR1 to bind to MAIT cells thereby activating or inhibiting MAIT cell activation.

Abstract: The present invention describes novel pharmaceutical compositions and methods for treatment of diseases, disorders, or conditions characterized by neuroinflammation, particularly, Parkinson's disease. According to the invention, compounds which inhibit the activity or expression of non-receptor Fyn tyrosine kinase can prevent activation of the neural inflammatory pathway and provide protection from and treatment of Parkinson's disease. Particularly preferred is the class of small molecule Fyn kinase inhibitors such as sacaratinib and its prodrugs, derivatives, analogs and the like.

Abstract: Provided herein are methods of using antagonists of G9a, for example, for treating cancer and/or preventing drug resistance in an individual. For example, a method of treating cancer in an individual comprising administering to the individual an antagonist of G9a alone or in combination with a cancer therapy agent is provided. In some embodiments, the antagonist of G9a increases the period of cancer sensitivity and/or delays development of cancer resistance.

Abstract: Compounds of formula I, have anti-inflammatory activity. Exemplary mechanisms of action include inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases. The compounds have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

Abstract: Compositions and methods including at least one PNP inhibitor or at least one PNP inhibitor in combination with guanosine identified as endogenous adjuvant useful to enhance Graft versus Malignancy effects in patients, with relapse of malignancy after hematopoietic stem cell transplantation, to reverse or prevent relapse or progression of malignancy. The compositions may be formulated as pharmaceutical dosage forms and components may be assembled as kits.

Abstract: The present invention provides for methods and pharmaceutical compositions for treating disorders using treatment regimens involving multiple agents. In one aspect, a method of treatment is provided resulting in reduced toxicity and/or synergistic effect by administration according to a described dosing schedule.

Abstract: Disclosed are chemical entities of formula I: wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

Abstract: The present invention relates to MEK inhibitors that are capable of displaying one or more beneficial therapeutic effects. The MEK inhibitors can be used in the prevention and/or treatment of viral infection. MEK inhibitors in combination with neuraminidase inhibitor compounds are capable of displaying one or more beneficial therapeutic effects in the treatment of viral diseases.

Abstract: Disclosed is a composition for inducing the differentiation of neural stem cells into dopaminergic neurons. The composition includes the compound represented by Formula 1 (“AS703026”) as a MEK 1/2 inhibitor. Also disclosed is a method for inducing the differentiation of neural stem cells into dopaminergic neurons by using the composition. Dopaminergic neurons whose differentiation from neural stem cells is induced by the composition and method can be applied to cell replacement therapies and gene therapies for the treatment of neurodegenerative diseases, such as Parkinson's disease, or can be widely used as materials for the examination of drug effects or numerous studies in the development of new drugs.

Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.

Abstract: The solubility of kinetin and/or of zeatin is increased when either or both are combined in a formulation that includes a polyoxyalkylene-n-glycerol dicarboxylate component and a fatty acid component. These two components provide a synergistic increase in the solubility of kinetin and/or zeatin that is greater than that which would be expected based on the solubility of kinetin and zeatin in the individual components.

Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.

Abstract: The application relates to solid pharmaceutical compositions suitable for oral administration, processes for their production and uses of the pharmaceutical compositions.

Abstract: This disclosure pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiaziniumcompounds”) including Methythioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt-formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). Also disclosed resulting (high purity) compounds, compositions comprising them (e.g.

Abstract: The present disclosure relates to pharmaceutical products comprising a combination of (i) a MET inhibitor which is INC280 or a pharmaceutically acceptable salt or hydrate thereof and (ii) an EGFR inhibitor described herein, which are jointly active in the treatment of proliferative diseases, corresponding pharmaceutical formulations, uses, methods, processes, commercial packages and related embodiments.

Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.

Abstract: Described herein are compounds and chemical entities of Formula I, methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.

Abstract: The present disclosure provides methods of treating a flavivirus infection, and compositions for use in the methods.

Abstract: The present invention relates to treatment of a condition associated with hyperinsulinaemia using the compounds described herein.

Abstract: Disclosed herein are pharmaceutical combinations, dosing regimen, and methods of administering a combination of a BTK inhibitor (e.g., ibrutinib), an immunomodulatory agent, and a steroid for the treatment of a hematologic malignancy.

Abstract: This document provides dietary supplements. For example, composition having a combination of ingredients useful in reducing cholesterol and improving overall cardiovascular health as well as methods for reducing cholesterol and improving overall cardiovascular health are provided.

Abstract: This invention provides a fixed-dose composition comprising formoterol or a pharmaceutically acceptable salt thereof and budesonide, for use in the long-term treatment of COPD and the treatment of acute exacerbations of COPD, wherein the composition is administered as a maintenance dose for the long-term treatment of COPD and pro re nata (p.r.n.) as a rescue medication for the treatment of acute exacerbations of COPD.

Abstract: The invention relates to a composition for preventing bearing loss in subject or for at least partially restoring bearing in a subject having a reduced auditory function. The composition comprises at least one sterol compound inducing neuron differentiation. Said composition is placed in contact with at least part of the cochlea.

Abstract: This document provides methods and materials for reducing development of stenosis of arteriovenous fistulas. For example, methods and materials for reducing IEX-1 polypeptide expression or activity within a mammal (e.g., a human) to reduce venous neointimal hyperplasia and/or the development of stenosis of arteriovenous fistulas are provided.

Abstract: Methods for the treatment of solid tumor cancers, specifically ovarian cancer and drug-resistant solid tumors, are disclosed. A method comprises administering a combination therapy including a therapeutically effective amount of an HDAC inhibitor and a therapeutically effective amount of an IKK inhibitor to a subject in need thereof. Pharmaceutical compositions and kits comprising an HDAC inhibitor and an IKK inhibitor are also disclosed.

Abstract: The invention relates to a poly(?-amino ester (PBAE) or a derivative thereof, for use as a vehicle for transporting an agent into cartilage tissue. In particular, PBAE derivatives are combined with agents and in particular therapeutic agents to form complexes. Certain PBAE derivatives and complexes are novel and these are described and claimed, together with pharmaceutical compositions and methods for using them.

Abstract: Oral, parenteral, and intravenous dosage forms of osteoclast inhibitors, such as neridronic acid, can be used to treat or alleviate pain or related conditions, such as knee pain.

Abstract: The use of neridronic acid or a salt thereof in the treatment of osteoarthritis is described. In particular, neridronic acid or a salt thereof has been shown to be able to reduce significantly the symptoms of osteoarthritis, such as pain and physical and mobility disabilities, as well as subchondral bone marrow lesions underlying the onset of such symptoms.

Abstract: Phosphatidylserine powder compositions of the present invention were found to provide more homogeneous dispersion and demonstrate reduced sedimentation, compared to conventional phosphatidylserine powders, when mixed without processing by high pressure homogenization in water or other liquids. The composition of the present invention comprises phosphatidylserine and at least 80% (w/w) of the composition has a particle size of 500 microns or less. Nutritional, nutraceutical, or pharmaceutical compositions including the phosphatidylserine powder compositions of the present invention are also provided. Process for preparing phosphatidylserine powder compositions according to the present invention is also provided and includes sieving.

Abstract: The invention pertains to the use of a non-digestible oligosaccharide in the manufacture of a composition for providing nutrition to an infant suffering from an increased risk of food allergy, preferably whey protein allergy; and/or reducing the risk of occurrence of or preventing whey protein allergy in an infant suffering from an increased risk of food allergy, particularly whey protein allergy. The infant is preferably at increased risk of trichothecene mycotoxin exposure, for instance by eating a lot of cereals.

Abstract: To provide an adiponectin secretion regulator whereby the effect of adiponectin can be efficiently expressed while the adverse effect of appetite increase associated with adiponectin is avoided, and to provide a food/drink product, a functional food product, a cosmetic, a pharmaceutical, and an animal feed having such adiponectin secretion regulating effects. In the present invention, fucose or a precursor thereof is used as an active ingredient of the adiponectin secretion regulator. A food/drink product, a functional food product, a cosmetic, a pharmaceutical, or an animal feed having adiponectin secretion regulating effects is obtained by compounding a specific amount of fucose or a precursor thereof.

Abstract: The invention relates to methods for obtaining liposomes externally modified with a targeting peptide able to selectively drive liposomal doxorubicin on membrane receptors over expressed in tumours. The invention is based on a kit containing a first vial filled with a sterile, translucent, red dispersion of the liposomal doxorubicin drug; a second vial filled with a modified phospholipid with a reactive function such as DSPE—Peg—maleimide in lyophilized form; and a third vial filled with a peptide modified with an appropriate reactive function, in a 1:1 stoichiometric amount respect to modified phospholipid and in lyophilized form. The kit could also contain an additional fourth vial with the targeting peptide modified with a chelating agent able to complex radioactive metal ions for diagnostic and imaging purposes. The patients to be treated with the peptide modified liposomal doxorubicin could be selected on the basis of the over expression of the targeting receptors.

Abstract: This invention is directed to compositions for promoting wound healing and regeneration and methods of use thereof. In one aspect, methods for promoting wound healing in a subject are provided, the methods comprising: administering a therapeutically effective amount of a DNA methyl transferase inhibitors (DNMT) to the subject. In another aspect, methods for reducing scarring during healing of a skin wound are provided, the methods comprising: administering a therapeutically effective amount of a DNMT inhibitor.

Abstract: Uridine triacetate or other uridine prodrugs are used to treat genetic glycosylation disorders by administering them in an amount sufficient to raise plasma uridine in the to a level greater than 30 micromolar. They can be administered alone or in combination with a sugar whose transfer is defective in the glycosylation disorder being treated.

Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.

Abstract: Method of producing nanoparticle of drug and imaging agents are provided. The phosphorylated encapsulated drugs and imaging agents could be encapsulated at therapeutic levels, were encapsulated at higher amounts. The CPSNPs were more effective in treating cancer, in reducing cancer proliferation, arresting cancer cell growth than when not in the form of a CPSNP, and showed efficacious treatment of cancer cells at far lower dosage than free molecules. Calcium phosphosilicate and phosphate nanoparticles are disclosed and their method of use. The methods and nanoparticles are particularly efficacious where CPSNPs were used to encapsulate 5-FU metabolites such as FdUMP and gemcitabine metabolites.

Abstract: The present invention relates to an association of beta-glucans from a first cereal and arabinoxylans from a second cereal different from the first cereal, and their use to improve the microbiota balance in human gut.