Abstract: The present invention relates to storage stable nanoparticulate compositions of piperazine compounds. The pharmaceutical compositions comprising the nanoparticulate compositions that are useful for the treatment and prevention of proliferative diseases including cancer are also described.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.

Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.

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 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: Antihepatotoxic agents include dihydropyrimidinone derivatives with 1,4-benzodioxane. The antihepatotoxic agents are compounds having the structural formula represented by Formula 1: wherein each Z independently represents O, N or S; X represents O or S; R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and pharmaceutically acceptable salts of these compounds.

Abstract: The invention relates to medicine, in particular to gastroenterology, and lies in the field of treatment of liver diseases of various origins. For this purpose, the hepatoprotective agent that is introduced to the patient is embodied as derivatives of bis(2-thio-4,6-dioxo-1,2,3,4,5,6-hexahydropyrimidine-5-yl) arylmethanes. The method provides reduction of the manifestations of cytolysis under the influence of damaging agents and a statistically significant reduction of dysproteinemia, it accelerates restoration of detoxifying processes of the liver, increases induction of endogenic interferon alfa and, consequently, makes the protection of liver cells during hepatitides of various origins more effective.

Abstract: The present invention is generally directed toward therapeutic compositions for treating infections caused by Herpes Simplex Virus (“HSV”). The therapeutic compositions meet a long felt need in the art of providing a treatment for lesions that result from HSV that drastically reduce the duration of a cold sore when vesicles have already appeared and a treatment that will prevent the outbreak of a lesion and formation of vesicles when applied in the prodromal stage. The therapeutic compound comprises a mixture of Acyclovir (“ACV”), Penciclovir (“PCV”), and dimethyl sulfoxide (“DMSO”). The therapeutic compositions of the present invention include multiple formulations of the three active ingredients and may also include inactive ingredients and/or additional active ingredients.

Abstract: The present disclosure provides compositions and methods for the prevention of HSV infection in an HSV seronegative individual.

Abstract: Provided are pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflamation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.

Abstract: The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.

Abstract: The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.

Abstract: Methods for treating neurodegeneration and/or myelination in patients are disclosed comprising treating the patient with a progestin compound which exerts binding to progesterone receptors and elicits progesterone-receptor-induced biological responses without interacting with the androgen receptor and without inducing androgen or glucocorticoid biological responses at a dosage sufficient to prevent or reduce neurodegeneration. The progestin compound preferably comprises 16-methylene-17?-acetoxy-19-norpregn-4-ene-3,20-dione, and the methods include combining the progestin compound with an estrogen compound to provide both contraception and treatment for myelin repair and neurodegeneration.

Abstract: Model and method of treating inflammatory diseases. Traditional treatments for such diseases include administering to the patient toxic anti-inflammatory drugs. Following stabilization of the symptoms, the drug doses are tapered down to minimize side effects, as a result of which inflammation remains high and the disease is rarely cured. A chemistry-based disease model concludes that irrespective of the role that inflammation plays in the disease, inflammation reduction will impede disease initiation and progression. Managing and controlling inflammatory diseases requires reducing inflammation to acceptable normal values. Non-toxic ways such as non-steroidal anti-inflammatory drugs, anti-inflammatory diets, and regular exercise allow such reduction in inflammation to normal values, thereby slowing down or arresting disease progression and allowing the discontinuation or reduction of toxic anti-inflammatory therapy while maintaining low inflammation using non-toxic therapy.

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: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid form or a salt form can be used to treat or alleviate pain or related conditions, such as allodynia associated with complex regional pain syndrome.

Abstract: This invention relates to compositions containing combinations of a balanced phosphatidylcholine composition and one or more cannabinoids, a natural or synthetic derivative thereof, or a salt thereof, and kits containing such combinations and methods of using such combinations to treat subjects suffering from an imbalance of fatty acids and related diseases or disorders. This invention also relates to the synergistic effect of such combination therapies in humans.

Abstract: The present invention relates to the new use of antiparasitic agents, such as ivermectin, abamectin/avermectin, doramectin and so on, and the design method of the derivatives for the new use. The said compounds including macrolide abamectin/avermectin, ivermectin, doramectin and the derivatives thereof, may be used in the manufacture of a medicament for use in treating metabolic related diseases in a mammal, such as hyperglycemia, insulin resistance, hypertriglyceridemia, hypercholesterolemia, diabetes, obesity, etc, and Famesoid X receptor mediated diseases, such as cholestasia, gallstone, non alcohol fatty liver disease, atherosclerosis, inflammation, cancer, etc.

Abstract: The present invention relates to an injectable anthelmintic composition of avermectin and basic albendazole sulfoxide for combatting parasites that infest animals. The invention further contemplates a specific method that allows the stable association of avermectin and basic albendazole sulfoxide.

Abstract: Disclosed herein are nucleosides, nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a Filoviridae virus infection with one or more nucleosides and/or nucleotide analogs.

Abstract: The present invention relates to a composition comprising a phosphorothioate oligonucleotide and at least one fatty acid and/or at least one emulsifying agent, wherein said composition is sterile and wherein said composition comprises at least one agent comprising a thiol group and at least one phosphate compound, preferably said composition is an ophthalmic composition. The present invention also relates to a method for obtaining the same and to the therapeutic use thereof.

Abstract: The present invention relates generally to vitamin B12 nasal spray compositions and methods of using the same in the treatment of vitamin B12 deficiency and various disorders that are related to such deficiency. In particular embodiments, the present invention is directed to treatment methods comprising intranasal administration of a cobalamin composition according to a particular dosing and frequency schedule and to a preservative-free nasal spray composition comprising a cobalamin compound useful in the practice of such treatment methods.

Abstract: Assays, methods and kits for predicting a subject's (e.g., human) risk of primary glomerulopathy, secondary glomerulopathy or recurrence (e.g., post-transplant recurrence) of any glomerular disease include examining cells for the presence or absence of cytoskeletal disruptions or rearrangements and examining cells for modulation of expression and/or activity of markers such as SMPDL-3b. Assays for predicting if a diabetic subject will develop kidney disease or a patient with FSGS will develop recurrent disease after transplant also include examining cells for the presence or absence of cytoskeletal disruptions or rearrangements and examining cells for modulation of expression and/or activity of markers such as SMPDL-3b. Also described herein are compositions and methods for treating and preventing the afore-mentioned disorders.

Abstract: Methods are presented for treating cancers and hematopoietic stem cell disorders, comprising administering to a subject with a cancer or hematopoietic stem cell disorder who is receiving a treatment regimen, a heparin derivative capable of inhibiting, reducing, abrogating or otherwise interfering with the binding of CXCL12 to CXCR4, wherein the cancer or hematopoietic stem cell disorder is one in which interaction of CXCL12 with CXCR4 privileges the cancer or disordered HSCs against therapeutic intervention. In preferred embodiments, the heparin derivative is a substantially 2-O, 3-O-desulfated heparin derivative.

Abstract: The subject of the invention is use of block polymers with a block of poly(3-methacryloylpropyltrimethylammonium chloride) to direct neutralization of heparin, especially unfractionated heparin and low molecular weight heparins in the blood and other body fluids.

Abstract: A topical application of nitric oxide may be provided by two separate containers, each containing an active component media to produce nitric oxide when combined. For example, a nitrite component media may be contained in one dispenser and an acidified component media may be contained in another dispenser. Each dispenser may dispense the respective component media as a foam. The resultant foams are combined to initiate the production of nitric oxide and the mixture of foams is applied topically to treat various skin disorders or wounds.

Abstract: The present invention relates to new plasma or new platelet-rich plasma preparations, new cell dissociation methods, new cell associations or compositions, a method of preparation thereof, a use thereof, devices for the preparation thereof and preparations containing such a platelet-rich plasma preparation and cell associations or compositions. Specifically, the invention provides plasma or platelet-rich plasma alone or in cell composition preparations for use in tissue regeneration and bone regeneration and pain reduction.

Abstract: The invention provides a corneal endothelial composition comprising a transparent hydrogel scaffold and a single layer of cultured corneal endothelial cells on the surface of the scaffold. The hydrogel scaffold I comprised of at least one biopolymer, preferably gelatin. Also provided are methods of making a corneal endothelial scaffold.

Abstract: Disclosed herewith is a method for inducing angiogenesis using modified placental tissue or an extract thereof to treat conditions other than cardiovascular conditions.

Abstract: A method of parenterally administering a composition, the method including parenterally administering to a person a composition including krill oil in an oil-in-water emulsion. A parenterally applicable pharmaceutical composition, including an oil-in-water emulsion including a phospholipid obtained from a marine crustacean.

Abstract: Species of human-derived bacteria belonging to the Clostridia class have been shown to induce accumulation of regulatory T cells (Treg cells) in the colon and suppress immune functions. Pharmaceutical compositions containing these bacteria can be used to prevent and treat immune-mediated diseases such as autoimmune diseases.

Abstract: It is to provide a composition derived from lactic acid bacteria having an anti-allergic effect (an effect of suppressing allergic symptoms such as hay fever) synergistically, and a food product, pet food, etc. containing the composition. It is to prepare a composition having an anti-allergic action, containing Lactobacillus crispatus KT-11 strain, KT-23 strain, or KT-25 strain bacterial cells and viable bacteria, dead bacteria, or a processed product of bacterial cells of other lactic acid bacteria belonging to the genus Lactobacillus, genus Bifidobacterium, genus Leuconostoc, genus Enterococcus, genus Pediococcus, etc. at a biomass-converted ratio of 99:1 to 50:50, preferably 99:1 to 75:25.

Abstract: The invention relates to fungal cells and spores, as well as extracts of either, for use, in particular, in prevention or treatment of Chlamydia, or Helicobacter pylori or other infections, inflammation, inflammatory, lysosomal, acidic, SOD—or IgG or other immunoglobulin—peroxidases or hydrogen peroxide induced or other forms of oxidative damage, atherosclerosis, heart disease, stomach, intestinal and liver inflammatory conditions and their complications, promoting or stimulating regeneration or healing of wounds, burns, ulcers, or other forms of damaged or aged tissues, or in reducing elevated cholesterol and/or triglycerides levels In a preferred instance, the fungal cells or spores are those used in the manufacture of fungal fermented cheeses or other food stuff or beverages, particular fungal blue or white cheeses.

Abstract: Topical medications to treat the physical effects of bruises and burns. For bruises, the topical medication preferably includes therapeutically effective amounts of vasoconstrictor, such as phenylephrine HCL USP, an anti-inflammatory, such as Arica, and compounding agents. In one embodiment, the compounding agents are a Versabase® gel which includes water, ammonium acryloyldimethyltaurate copolymer, aloe barbadensis leaf juice powder, allatoin, disodium EDTA, methylchloroisothiazolinone and methylisothiazolinone. For burns, the topical medication preferably combines therapeutically effective amounts of an active anti-bacterial compound, such as silver sulfadiazine, an anesthetic, such as lidocaine, and a histamine blocker, such as diphenhydramine, with suitable compounding agents, such as Versabase® gel. Both the anti-bruise and anti-burn medications of the present invention can advantageously be formulated in solutions, lotions, creams, ointments, gels, foams or transdermal patches.

Abstract: Topical aqueous compositions are effective in minimizing scar formation and improving the visual appearance of scars. The compositions are also effective in treating numerous skin disorders, including acne, psoriasis, and eczema.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating diabetes or dementia, comprising centipede grass (Eremochloa ophiuroides) extracts as an active ingredient. It has been identified from animal tests that the centipede grass extracts, fractions thereof, and active fractions separated from the said fractions effectively regulate blood glucose levels, and inhibit the activity of amyloid-?(A?) which is involved in the formation of amyloid plaques that might cause dementia. Thus, the extracts, the fractions thereof, and the active fractions separated from the said fractions can be effectively used in a composition for preventing and treating diabetes or dementia, in a functional food for preventing or improving diabetes or dementia, and in a pharmaceutical composition or health food for blood glucose regulation.

Abstract: Compositions, foods, and medicaments for enhancing memory and learning function and/or cognitive function are provided. Compositions, foods, and medicaments for improving brain function and particularly enhancing memory and learning function and/or cognitive function can be provided by including a peptide including an amino acid sequence set forth in any one of SEQ ID NOs 1 to 16 as an active ingredient.

Abstract: The present invention relates to compositions and methods for treating autoimmune diseases by administering to a subject a CTLA4 molecule that block endogenous B7 molecules from binding their ligands.

Abstract: A liquid pharmaceutical composition having a conjugated erythropoietin, buffer, sugar, tonicity modifier and amino acid as an aggregation inhibitor. The liquid pharmaceutical composition provides a stable pharmaceutical composition which encompasses conjugated erythropoietin, acetate buffer, sucrose, arginine and sodium chloride which is maintained at a pH of about 4.9 to 5.3.

Abstract: The disclosure relates to therapeutic methods for regulating weight gain, metabolic syndrome, and insulin resistance. In certain embodiments, the disclosure relates to methods of treating or preventing obesity, metabolic syndrome, or insulin resistance by administering an effective amount of a pharmaceutical composition comprising one or more GDNF receptor agonists to a subject in need thereof.

Abstract: An isolated human cell is disclosed comprising at least one mesenchymal stem cell phenotype and secreting brain-derived neurotrophic factor (BDNF), wherein a basal secretion of the BDNF is at least five times greater than a basal secretion of the BDNF in a mesenchymal stem cell. Methods of generating same and uses of same are also disclosed.

Abstract: Methods and compositions for treating or preventing cognitive disorders in mammals, preferably humans, are provided. The methods generally involve modulation of the OST-PTP signaling pathway or the PTP-1B signaling pathway involving gamma-carboxylase and osteocalcin, e.g., by administration of undercarboxylated/uncarboxylated osteocalcin. Disorders amenable to treatment by the methods include, but are not limited to, cognitive loss due to neurodegeneration associated with aging, anxiety, depression, memory loss, learning difficulties, and cognitive disorders associated with food deprivation during pregnancy.

Abstract: The invention relates to methods and compositions for regulation of GSK3? activity. The invention provides phosphorylated GSK3? polypeptides and antibodies that recognize such polypeptides. The invention further includes methods for treating disorders that are associated with elevated or reduced GSK3? activity.

Abstract: The present invention provides methods, compositions, and kits for the treatment of neurocutaneous syndromes, such as neurofibromatosis type I; disorders associated with overactivation of FGFR3, such as achondroplasia; bone or cartilage disorders; or vascular smooth muscle disorders; or for the elongation of bone. In some embodiments, the present invention provides polypeptides having an alkaline phosphatase peptide fused to an Fc domain of an immunoglobulin or a natriuretic peptide fused to an Fc domain of an immunoglobulin. Such polypeptides can be administered to subjects, e.g., subcutaneously, to treat a neurocutaneous syndrome, a disorder associated with overactivation of FGFR3, a bone or cartilage disorder, or a vascular smooth muscle disorder, or to elongate bone.

Abstract: The present invention includes compositions and methods for treating disease and disorders associated with pathological calcification or pathological ossification by modulating the level or activity of NPP1 or a mutant thereof, or a mutant NPP4 modified to exhibit ATP hydrolase activity similar to the hydrolase activity of NPP1.

Abstract: The present invention relates to polyethylene glycol (PEG) modified protein drugs, and a PEGylated tissue kallikrein, a preparation method and use thereof are disclosed. The tissue kallikrein has a sequence as shown in SEQ ID No. 1 or SEQ ID No. 2, and the tissue kallikrein may be natural or recombinant. The PEG has a molecular weight of 20 to 40 kDa, and is conjugated to the N-terminal primary amino of the tissue kallikrein. In addition to the advantages of significantly extended half-life, significantly reduced immunogenicity and stable and uniform structure, the biological activity of the PEGylated KLK1 provided in the present invention is improved to a higher extent, which is more significant in the treatment of cerebral apoplexy and diabetic nephropathy in particular.

Abstract: A novel method of using an aquaporin protein from Rhipicephalus microplus (RmAQP2), fragments of RmAQP2, and/or the cDNA encoding RmAQP2 and/or the fragments are described. Immunogenic composition containing recombinant RmAQP2 and/or fragments of RmAQP2 are produced and administered to an ungulate which generates an immune response to RmAQP2. After feeding female ticks on the ungulate injected with RmAQP2 and/or fragments of RmAQP2, the female ticks have lower reproductive viability because of a reduced egg mass, reduced hatching percentage, and reduced survival of larvae. Thus, administering RmAQP2 and/or RmAQP2 fragments to an ungulate can reduce the incidence of R. microplus and also reduce the incidence of tick-borne pathogens in ungulates because of the lower number of R. microplus.

Abstract: Protein conjugate comprising a protein antigen for generating an immune response against the HER2/neu protein and an immunogenic carrier covalently bonded to said protein antigen, wherein said protein antigen (i) has a sequence segment of 300 or more contiguous amino acids of the amino acid sequence of SEQ ID NO: 1; or (ii) has a variant sequence segment of 300 or more amino acid residues, wherein the amino acid sequence of said variant sequence segment has at least 85% sequence identity to a sequence portion from SEQ ID: 1; or (iii) has a variant sequence segment of 300 or more amino acid residues and has from 1 to 10 substitutions, deletions or additions in said variant sequence segment compared to a sequence segment of 300 or more amino acid residues of the amino acid sequence of SEQ ID NO: 1 or 2.