Abstract: There is described, inter alia, a coated bead comprising: (a) a granule; (b) a first layer coated over the granule, the first layer comprising a first amount of an active pharmaceutical ingredient comprising a central nervous system stimulant; and (c) a second layer coated over the first layer, the second layer being present in an amount sufficient to substantially delay release of the active pharmaceutical ingredient in the first layer until after the coated bead reaches a distal intestine portion of a subject to whom the coated bead is administered; and (d) the third layer coated over the second layer, the third layer comprising a second amount of the active pharmaceutical ingredient, the third layer being configured to permit substantially immediate release of the active pharmaceutical ingredient comprised therein. Embodiments related to a solid oral pharmaceutical composition are also described.

Abstract: There is described, inter alia, a coated bead comprising: (a) a granule; (b) a first layer coated over the granule, the first layer comprising a first amount of an active pharmaceutical ingredient comprising a central nervous system stimulant; and (c) a second layer coated over the first layer, the second layer being present in an amount sufficient to substantially delay release of the active pharmaceutical ingredient in the first layer until after the coated bead reaches a distal intestine portion of a subject to whom the coated bead is administered; and (d) the third layer coated over the second layer, the third layer comprising a second amount of the active pharmaceutical ingredient, the third layer being configured to permit substantially immediate release of the active pharmaceutical ingredient comprised therein. Embodiments related to a solid oral pharmaceutical composition are also described.

Abstract: Disclosed are a hyaluronic acid-based amphiphilic polymer, preparation method and application thereof. A main chain of the amphiphilic polymer is a hydrophilic hyaluronic acid and can be employed in active targeting, and a side chain thereof is a hydrophobic group represented by Formula (1). The amphiphilic polymer can carry a small molecule anticancer drug. Polymer nanoparticles are obtained via chemical crosslinking, such that the nanoparticles are not readily dissociated outside a cell or in blood, thus ensuring the stability of a drug encapsulated by the nanoparticles. Upon arriving at a tumor tissue, the hyaluronic acid on a surface of the nanoparticle can immediately combine with a CD44 receptor on a surface of a tumor cell, and effectively enter the tumor cell via endocytosis mediated by the receptor, and then quickly de-crosslink to be dissociated.

Abstract: Disclosed is an adhesive patch having a support and an adhesive agent layer laminated on the support, wherein the support consists of spunlace nonwoven fabric, the adhesive agent layer comprises an SIS block copolymer and liquid paraffin, the adhesive patch has a first direction, which is a predetermined reference axis direction, and a second direction, which is orthogonal to the first direction, and a bending resistance in the first direction of the adhesive patch is 18 to 30 mm.

Abstract: The invention relates to a transdermal therapeutic system, preferably a transdermal patch, having an active ingredient-containing matrix formed substantially of a water-insoluble base material, such as rubber and synthetic polymers, into which is incorporated water-soluble and/or water-swellable inclusion bodies, e.g. inclusion bodies formed from polyvinyl alcohol or polyethylene glycol, that further include micronized or nanoscale active ingredient particles.

Abstract: Methods and compositions are disclosed for delivering lutein or other antioxidant to target tissues such as the eye, in bioactive form, while protecting the antioxidant from degradation. The antioxidant is encapsulated in nanoparticles comprising a protein such as zein or a polymer such as poly(lactic-co-glycolic acid) (PLGA). Preferably a surfactant is associated with the nanoparticles as well, further helping to protect the antioxidant. After the nanoparticles are administered to the target tissue, bioactive antioxidant is released to the tissue over time. Optionally, the nanoparticles are admixed with a thermosensitive, bioadhesive gel to promote slow release of antioxidant. The methods and compositions are useful for treating or preventing conditions such as age-related macular degeneration or cataracts.

Abstract: Systems and methods provide sugar alcohol to heat stressed ruminants to improve performance. During periods of high temperature or humidity, heat stressed ruminants may exhibit decreased dry matter intake, and in response, an effective amount of sugar alcohol such as sorbitol may be provided in the ruminant diet to cause performance to increase, which may include increased milk yield, improved feed efficiency or both compared to heat stressed dairy cattle without sugar alcohol in the diet.

Abstract: A dressing for applying to the skin is characterized in that the adhesive mass is applied discontinuously in a strip or wave and contains an active substance.

Abstract: This disclosure provides generally for antimicrobial compositions and methods of use comprising an anthocyanin, an anthocyanidin or metabolites thereof. Methods for promoting healing of a wound using these compositions are also disclosed. These compositions have broad spectrum antimicrobial activity and are safe for human and animal uses. Further, these compositions are safe for medical uses and industrial uses as antiseptic preparations to reduce or prevent microbial growth.

Abstract: The present application relates to a method of treating Parkinson's disease by administering a mouth-dissolving composition of N-propargylamine derivative, such as rasagiline or a pharmaceutically-acceptable salt thereof.

Abstract: Disclosed herein are pharmaceutical compositions for nasal administration comprising tapentadol, their preparation and their use in the treatment of pain.

Abstract: The invention relates to a pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the prophylaxis and therapy of Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy. Another object of the invention concerns the use of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the enhancement of insulin sensitivity and the preservation or increase of ß-cell compensation.

Abstract: Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of diseases such as inflammation and/or pain, comprising the administration of a therapeutically effective amount of a non-steroidal, non-opioid compound having GI-/renal-/platelet-sparing activities, and wide safety margins with no appreciable inhibition of either form of cyclooxygenase.

Abstract: This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

Abstract: Ketogenic compositions including a beta-hydroxybutyrate (BHB) mixed salt are formulated to induce or sustain ketosis in a subject to which the ketogenic compositions are administered. The BHB mixed salt is formulated to provide a biologically balanced set of cationic electrolytes, and is formulated to avoid detrimental health effects associated with imbalanced electrolyte ratios. A ketogenic composition includes BHB salts of at least sodium, potassium, calcium, and magnesium. The BHB salts may also include at least other component such as a BHB compound containing other cations, such as transition metal cations (e.g., zinc or iron), a BHB-amino acid salts, medium chain fatty acid source, vitamin D3, flavorant, or other excipient.

Abstract: The present invention relates to a pharmaceutical composition of ibuprofen and tramadol for ophthalmic use. Said composition is effective and safe for the treatment of ocular inflammation and/or pain associated to different diseases or pathological states which affect the eye area In particular, the ophthalmic composition of the invention is indicated, for example, for the treatment of pain and/or inflammation after eye surgery.

Abstract: The invention provides methods for muscle repair or regeneration comprising administering therapeutically effective amounts of RAR agonists or stem cells that are pretreated with contact with a RAR agonist to a subject at a site of muscle damage. Additionally, the invention provides compositions comprising RAR agonist treated stem cells and methods of use of said cells for muscle repair or regeneration. In one embodiment, the stem cells are mesenchymal stem cells. In one embodiment, the RAR agonist is an RAR? agonist. In one embodiment, administration of the RAR agonist is begun during a period of increased endogenous retinoid signaling in the subject resulting from incurrence of the damaged muscle tissue.

Abstract: Provided is a skin external composition, which includes tranexamic acid or a salt thereof and a skin penetration enhancer, thereby showing remarkably increased skin permeability and improved sense of use, skin irritation, and storage stability.

Abstract: The present invention is a glutamine compound having a high Z element attached via a ligand, which enters the mitochondrion and is subsequently exposed to ionizing radiation. When exposed to ionizing radiation, the present invention damages mitochondrial (as well as other) substructures such as mtDNA, the outer membrane, the inner membrane, cristae, ribosomes, etc., and causes the effective destruction of such mitochondrion. Tumorigenic cells without mitochondria cannot produce the energy they need to subsist and replicate, effectively starving them of energy and causing their destruction.

Abstract: Embodiments of the invention generally relate to supplements for treating fibromyalgia and symptoms associated with fibromyalgia.

Abstract: Lipid compositions comprising nuts, seeds, oils, legumes, fruits, grains, and dairy useful in specified amounts as dietary supplements and diet plans designed around and including the aforementioned for the prophylaxis and treatment of numerous diseases are disclosed. The compositions include omega-6 and omega-3 fatty acids where the ratio of the omega-6 to the omega-3 fatty acids and their amounts are controlled based on one or more factors including age of the subject, sex of the subject, diet of the subject, the body weight of the subject, medical conditions of the subject, and climate of the subject's living area.

Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.

Abstract: The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein R1 is a hydrogen atom, an alkyl group and the like, R2, R3, and R4 are the same or different and each is a hydrogen atom, an alkyl group and the like, R5 and R6 are the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Ar1 is a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is —O—, —S—, —SO2—, or —N(R7)— wherein R7 is a hydrogen atom, a (C1-C6) alkyl group and the like, or a pharmacologically acceptable salt thereof.

Abstract: The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

Abstract: Provided is a novel medicament capable of reducing the side effects of metformin or a pharmaceutically acceptable salt thereof and useful as an anti-malignant tumor agent, in which metformin or a pharmaceutically acceptable salt thereof and dihydroquercetin or a pharmaceutically acceptable salt thereof are combined.

Abstract: Combinations of betaine and vitamin C are used to suppress or prevent malignant tumors or to treat viruses, e.g., by combining the two ingredients in a product consumed by a human, dog, or cat, such as an aqueous liquid such as grape juice, the ingredients being provided in containers with instructions for use, or in finished products, especially with support of tests demonstrating the effectiveness of the treatment for, e.g., preventing tumors in populations known to be at risk of developing tumors, or, treating existing cancers in combination with other cancer drugs such as anastrozole and/or fulvestrant and/or artemisinin either concurrently or sequentially to prevent the cancer from growing when the cancer drug is not being used, or in the treatment of viruses.

Abstract: Embodiments of the invention generally relate to supplements for increasing human growth hormone (hGH) levels in healthy human beings.

Abstract: The present invention relates to a nintedanib diethanesulfonate salt A-type crystal represented by formula (II), and also relates to a crystalline composition and pharmaceutical composition comprising the crystal, and preparation method and use thereof. An X-ray powder diffraction spectrum of the nintedanib diethanesulfonate salt A-type crystal of the present invention has a diffraction peak at about 14.64, 18.79, 19.31, 20.11, 21.20, 22.45 and 26.71° when represented via a 2? value. The nintedanib diethanesulfonate salt A-type crystal of the present invention has a stable property, is non-hygroscopic and difficult to degrade, and is particularly suitable for medicine production.

Abstract: The present invention provides controlled release dosage formulations of compounds having the Formula: or pharmaceutically acceptable salts thereof, and in particular, aplindore. The dosage forms are useful, inter alia, for reducing side effects from administration of such compounds.

Abstract: A composition for opththalmic administration comprising a formaldehyde releasing agent, sodium bicarbonate, and an ophthalmically suitable carrier or excipient is provided.

Abstract: The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).

Abstract: The present invention relates to a composition for prevention or treatment of bronchial asthma comprising a PKR inhibitor as an active ingredient. The PKR inhibitor and derivatives thereof according to the present invention can be used as a pharmaceutical for prevention, amelioration or treatment of bronchial asthma and as a supplementary health food because the PKR inhibitor and derivatives thereof reduce the total counts of inflammatory cells, eosinophils, neutrophils and lymphocytes in bronchoalveolar lavage fluid of neutrophilic severe asthma-induced mice, reduce airway inflammation and airway hyper-responsiveness, and reduce inflammatory mediators.

Abstract: The present application relates to novel heteroaryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.

Abstract: A pharmaceutical composition containing an anticancer compound, named isopicrinine, isolated from the plant Rhazya Stricta. The pharmaceutical composition may contain a salt, an analog, a derivative, and/or the prodrug of isopicrinine. A method of treating cancer with the pharmaceutical composition is disclosed. A method of extracting isopicrinine is also disclosed.

Abstract: Compounds and pharmaceutical compositions for treating cancer by, for example, modulating immune system activity, are provided.

Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like.

Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c

Abstract: The present invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.

Abstract: The present disclosure provides methods and compositions for treating fall-related symptoms in patients with neurodegenerative diseases such as Parkinson's disease or Parkinson-related diseases. In some embodiments, the disclosure utilizes nicotine or a salt thereof in combination of dopaminergic agent treatments for reducing fall-related symptoms such as reducing frequency of fall, reducing injuries related to fall, reducing severity of injuries related to fall, freezing of gait, improving posture stability, improving locomotion ability, improving balance and gait. In some embodiments, the methods predict fall frequency and tendency of recurrent falls in patients with Parkinson's disease, in particular, patients with typical Parkinson's disease.

Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.

Abstract: The present invention relates to the field of molecular biology and cancer biology. Specifically, the present invention relates to methods of treating a subject with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on genotyping and expression profiling of certain immunological genes and RAS mutation status in the subject.

Abstract: In DN-DISC1 mice, a mouse model for major mental illnesses, the model that expresses pathological phenotypes relevant to schizophrenia, mood disorders, and addiction simultaneously, the inventors of the present invention found pronounced levels of oxidative stress in the prefrontal cortex, but not in the striatum. These mice also displayed greater amounts of GAPDH-Siah1 binding, a protein-protein interaction that is activated under exposure to oxidative stress. The present inventors investigated the role of oxidative stress in other organ systems. As detailed herein, the inventors found that GAPDH-Siah1 binding was increased in mouse models of cardiac failure. It was also found, that certain novel analogs of deprenyl, significantly inhibited GAPDH-Siah1 binding in cardiac tissue.

Abstract: The present invention relates to compounds of Formula (I), along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).

Abstract: The present disclosure provides a method of treating a subject that is resistant to one or more drugs by identifying a subject having one or more drug resistant cells; administering to the subject a pharmaceutically effective amount of an inhibitor compound, and contacting one or more drug resistant cells with the inhibitor compound to reduce the export of the inhibitor compound from the one or more drug resistant tumor cells and to block the transport of drug(s) from the one or more drug resistant cells.

Abstract: Use of oxymethylene aryl GPR119 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provided.

Abstract: The present invention provides methods for increasing plasma dUrd levels comprising the administration of 6R-MTHF. The methods of increasing plasma dUrd increase dUrd levels compared to equimolar concentrations of LV. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF.

Abstract: The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: Certain embodiments are directed to methods of treating chronic lung diseases in a subject comprising administering to a subject diagnosed with, exhibiting symptoms of, or at risk of developing a chronic lung disease a therapeutically effective amount of a BRD4 inhibitor or a CDK9 inhibitor to the subject.

Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.