Abstract: The present invention relates to new monoterpene derivatives of chalcone or dihydrochalcone and their use as a depigmenting agent.

Abstract: The invention provides a preparation method of N-acyl acidic amino acid or a salt thereof, comprising subjecting a fatty acyl chloride and an amino acid to an amidation reaction under an alkaline condition. The preparation method is characterized in that in the amidation reaction, water is used as a solvent, an acidic amino acid or a salt thereof is used as a main raw material and a small amount of a neutral amino acid or a salt thereof is used as an auxiliary raw material, and the method comprises the following steps: under a stirring condition, firstly adding the fatty acyl chloride dropwise into an aqueous solution of the acidic amino acid or the salt thereof; adding an alkali to adjust the pH value of the reaction solution; after a certain amount of fatty acyl chloride having been added dropwise, adding an aqueous solution of the neutral amino acid or the salt thereof, and continuing to add the fatty acyl chloride dropwise until the addition is finished and stirring to maintain the reaction.

Abstract: Topical compositions to address menopausal skin conditions include an effective amount of S-acyl glutathione derivative and a carrier. Methods for addressing menopausal skin conditions include applying a composition containing S-acyl glutathione derivative in a dermatologically acceptable carrier to skin tissue. The acyl group is a saturated or unsaturated aliphatic C12-C24 group, preferably an unsaturated C16-C24 group, most preferably an unsaturated C18 group. In particularly preferred embodiments, the acyl group is a linoleoyl group.

Abstract: Described herein are novel methods for the treatment of rosacea which include the step of applying of a composition containing a polymetal complex to an area of the skin afflicted with rosacea and novel regimens using such compounds.

Abstract: A composition of matter is used as an ingredient in cosmetics comprising at least 0.5% by weight and preferably 1-30% by weight of highly refined cellulose fiber in a cosmetic composition. Additionally present in the composition are other conventional cosmetic ingredients as known in the art. This composition may include at least colorants (dyes and pigments), lipophilic materials, aqueous materials (water and aqueous solutions), waxes, binding agents (polymers, thickening agents), emollients, emulsifiers, thickening agents, antioxidants, natural and synthetic oils and extracts, clays, ultraviolet radiation absorbers, and the like.

Abstract: Described are novel polymers and home and personal care compositions incorporating said polymers.

Abstract: A mixable multi-functional composition for application to keratin fibers such as hair, lashes or brows comprising at least one volatile solvent, at least one siloxane resin, at least one montmorillonite mineral, optionally at least one non-volatile oil, and optionally at least one wax; and a method for coloring keratin fibers comprising the steps of sequentially applying to the fibers, in any order, at least one mixable composition and at least one pigmented composition, wherein upon application the mixable composition mixes and combines with the pigmented composition in the wet state to form a final mixed composition that upon drying forms a compatible and homogeneous film.

Abstract: Disclosed is a topical skin composition comprising an aqueous extract from a part of Nymphaea gigantea, wherein said part consists of the flower of Nymphaea gigantea, an aqueous extract from a part of Plumeria alba, wherein said part consists of the flower of Plumeria alba, and a dermatologically acceptable vehicle.

Abstract: The present invention relates to a composition comprising an NF?B-inhibitor and a tropoelastin promoter, and methods of treating signs of skin aging using said compositions.

Abstract: Substance mixtures are proposed, comprising (a) terpenes, (b) propane-1,3-diol, and optionally (c) active substances selected from the group consisting of (c1) rebaudiosides or plant extracts comprising them, (c2) steviosides or plant extracts comprising them, (c3) monatin, (c4) naringin, (c5) chalcones and hydrochalcones, (c6) mogrosides or plant extracts comprising them, (c7) rubusosides or plant extracts comprising them, and (c8) glycyrrhizic acid or plant extracts comprising it.

Abstract: The present invention relates to a method of preparing a colored gloss pigment using a natural dye. According to the present disclosure, the method may include preparing a dye from a dye material of natural dyes; titrating the dye with an inorganic salt solution and subsequently adjusting a pH neutral to prepare a natural pigment containing the dye; dispersing a substrate coated with a metal oxide into a DI water to form a substrate suspension; and introducing a pH adjusting agent and the natural pigment into the substrate suspension to coat a surface of the substrate with the natural pigment.

Abstract: The present invention is directed to a carbamazepine-cyclodextrin inclusion complex useful for the parenteral administration of carbamazepine. The carbamazepine-cyclodextrin inclusion complex is prepared by the admixture of a modified cyclodextrin and carbamazepine in a physiologically acceptable fluid. Modified cyclodextrins include 2-hydroxypropyl-beta-cyclodextrin and sulfoalkyl cyclodextrins. More particularly, the sulfoalkyl cyclodextrins are those described and disclosed in U.S. Pat. Nos. 5,134,127 and 5,376,645. A physiologically acceptable fluid includes sterile isotonic water, Ringer's lactate, D5W (5% dextrose in water), physiological saline, and similar fluids suitable for parenteral administration.

Abstract: Provided herein are hemostatic compositions. In one embodiment, the hemostatic composition includes cross-linked polymer microspheres, such as cross-linked gelatin microspheres with pores. In another embodiment, the hemostatic composition comprises an additive such as a wetting agent, a suspending agent, or both. The hemostatic compositions may also include a hemostatic agent such as thrombin, and may include a high concentration of thrombin. The hemostatic compositions may also include plasma. Also provided herein are devices for dispersing said hemostatic compositions in a diluent, and delivering said dispersed hemostatic composition. The hemostatic compositions may also fabricated with a selected geometry as administration suggests.

Abstract: Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.

Abstract: The present invention concerns gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent and process for manufacturing said formulation.

Abstract: This application discloses a BBB-selective antibody. The BBB-selective antibody comprises a protein encoded by a DNA sequence comprising SEQ ID NO:7 (CDRH1 of scFv 15), SEQ ID NO:8 (CDRH2 of scFv 15), SEQ ID NO:9 (CDRH3 of scFv 15), SEQ ID NO:10 (CDRL1 of scFv 15), SEQ ID NO:11 (CDRL2 of scFv 15) and SEQ ID NO:12 (CDRL3 of scFv 15) or a DNA sequence comprising SEQ ID NO:19 (CDRH1 of scFv 38), SEQ ID NO:20 (CDRH2 of scFv 38), SEQ ID NO:21 (CDRH3 of scFv 38), SEQ ID NO:22 (CDRL1 of scFv 38), SEQ ID NO:23 (CDRL2 of scFv 38) and SEQ ID NO:24 (CDRL3 of scFv 38). Preferably, the BBB-selective antibody comprises a protein encoded by SEQ ID NO:1 or 3.

Abstract: The present invention relates to an enteric coating formulation, as well as methods for preparing and using said enteric coating formulation. In particular, the invention relates to an enteric coating formulation that is made up of foodeous approved materials.

Abstract: The present invention provides, among other things, methods of delivering mRNA in vivo, including administering to a subject in need of delivery a composition comprising an mRNA encoding a protein, encapsulated within a liposome such that the administering of the composition results in the expression of the protein encoded by the mRNA in vivo, wherein the liposome comprises a cationic lipid of formula I-c: or a pharmaceutically acceptable salt thereof.

Abstract: Described are stability-enhancing formulations of drugs that are sensitive to moisture. The formulations comprise co-granulates containing a moisture-sensitive drug and an excipient selected from fructose, xylitol, maltitol, and mixtures thereof. Also described are methods of producing a pharmaceutical tablet. The method comprises forming a blend of a moisture-sensitive drug and a first excipient selected from fructose, xylitol, maltitol, and mixtures thereof; spraying the blend with water to produce granules; drying and milling the granules; mixing a second excipient with the granules; and compressing into tablets.

Abstract: Granules of racemic sodium ibuprofen dihydrate formed from components specified herein have very desirable properties and can be effectively used in conventional rotary press tableting equipment without operational difficulties often encountered in actual practice. Their preparation by a wet granulation process, the wet granule compositions, formulations adapted for preparation of solid dosage forms utilizing a rotary press, solid dosage forms, and methods of preparing solid dosage forms in a rotary press are also described.

Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.

Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release matrix preparation comprising (A) a pharmacologically active drug, (B) a combination of cellulose derivatives, and (C) mannitol.

Abstract: Disclosed is a method for the preparation of easily-swallowed, reliably-dosed, aesthetically-improved tablets of sodium ibuprofen dihydrate, the method comprising the formation of the tablets with punches or presses comprising contact surfaces which are chrome or chrome-plated.

Abstract: The invention relates to a capsule comprising an inlet and an outlet connected by a passage, in which a dissolvable blocking element and a composition to be orally administered are arranged. The blocking element is fluid permeable and, in a non-dissolved condition, is arranged in the passage to block delivery of the composition to an outlet of the passage. The invention further relates to a method for releasable sealing a capsule comprising a composition to be orally administered, comprising the steps of providing the composition chamber in a passage and filling composition into the composition chamber. The passage formed by the capsule is occluded with a blocking element and the blocking element comprises dissolvable material and has a fluid permeable structure.

Abstract: A cell carrying microsphere composition, wherein the microsphere composition comprises a microspheric core comprising a triblock copolymer matrix A-B-A wherein A is selected from poly(lactide-co-glycolide) (PLGA) or polylactide (PLA) and B is poloxamer or poloxamine, wherein the microspheric core is coated with a cell adhesion coating and further comprises whole cells or cell fragments bonded to the cell adhesion coating, a process for the preparation of a cell carrying microsphere composition, and applications thereof.

Abstract: Provided herein are therapeutic nanoparticles having a diameter of between 10 nm to 30 nm, and containing a polymer coating, and a nucleic acid containing a sequence complementary to a sequence within a micro-RNA identified as having a role in cancer cell metastasis or anti-apoptotic activity in a cancer cell (e.g., miR-10b) or a sequence within an mRNA encoding a pro-apoptotic protein that is covalently linked to the nanoparticle. Also provided are pharmaceutical compositions containing these therapeutic nanoparticles. Also provided herein are methods of decreasing cancer cell invasion or metastasis in a subject having a cancer and methods of treating a metastatic cancer in a lymph node in a subject that require the administration of these therapeutic nanoparticles to a subject.

Abstract: Hypotonic formulations were evaluated for delivering water-soluble drugs and for drug delivery with muco-inert (that is, non-adhesive) mucus-penetrating nanoparticles (MPP). Hypotonic formulations markedly increased the rate at which drugs and MPP reached the epithelial surface, including deep into the vaginal folds. Minimally hypotonic formulations, preferably ranging from 20-220 mOsm/kg, provided rapid and uniform delivery of MPP to the entire vaginal surface, with minimal risk of epithelial toxicity. Data also show that there is a higher osmolality in the colon, such that vehicles with an osmolality above that of blood plasma (generally considered isotonic at ˜300 mOsm/kg), still lead to improvements in distribution in the colon due to rapid, osmotically-induced fluid absorption. The range for improved colon distribution with a hypotonic vehicle in the colon is ˜20 mOsm/kg-450 mOsm/kg.

Abstract: A tissue thickness compensator may generally comprise a compressible core comprising a plurality of movable particles, and a wrap surrounding the compressible core. The plurality of movable particles may comprise at least one medicament. A tissue thickness compensator may generally comprise a compressible core comprising a plurality of crushable particles, and a wrap surrounding the compressible core. The plurality of crushable particles may comprise at least one medicament. The compressible core may comprise a material selected from a group consisting of a biocompatible material. The wrap may comprise a material selected from a group consisting of a biocompatible material. Articles of manufacture comprising the tissue thickness compensator and methods of making and using the tissue thickness compensator are also described.

Abstract: Disclosed herein are compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging, or for modulating one or more energy biomarkers, normalizing one or more energy biomarkers, or enhancing one or more energy biomarkers, wherein the compound is a compound of Formula I or Formula II: wherein: R1 and R2 are independently hydrogen, (C1-C6)alkyl or —O(C1-C6)alkyl; or R1 and R2 together represent —CH?CH—CH?CH—; R3 is (C1-C6)alkyl; X is —CH?CH— or —C?C—; m is 1-10; n is 1-5; k is 1-3, with the proviso that when k is an integer of 2 or 3, n is independently 1-5 in each occurrence of the —X—(CH2)n— group; Y is —OR4, —CN, —C(?O)OR5, —C(?O)R5, or —C(?O)N(R6)2; R4 and R5 are independently selected from the group consisting of hydrogen, —(C1-C6)alkyl, —(C1-C6)haloalkyl, —C(?O)—(C1-C6)alkyl, —C(?O)—(C1-C6)haloalkyl, —C(?O)—NH(C1-C6)alkyl, —C(?O)—N((C1-C6)alkyl)2,

Abstract: The invention provides methods of inhibiting the development or progression of a thioesterase deficiency disorder in a mammal by the administration of a compound that functionally mimics the enzymatic activity of all thioesterases in mammals. Such thioesterase deficiency disorders include cancers and adult- or infant-neuronal ceroid lipofuscinoses (NCLs). The invention also provides small molecule mimics of thioesterases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds and methods of using the same.

Abstract: A method and pharmaceutical composition are disclosed for treating, ameliorating and/or preventing one or more myocardial disorders in a mammalian heart caused by a myocardial hypoxic event and/or a loss, reduction or interruption in coronary blood flow such as may happen during or after events such as a heart attack, cardiac surgery including coronary artery bypass graft, or coronary artery or myocardial reperfusion. The myocardial disorders include myocardial arrhythmias, myocardial damage and myocardial cell death, and the subsequent loss of haemodynamic function. The myocardial disorders could be in progress or suspected of being in progress at the time of treatment or could be anticipated disorders being treated prophylactically. The method involves the step of administering an effective amount of the composition. The composition comprises as its active ingredient one or more compounds having myocardial persistent sodium channel blocking activity.

Abstract: The present invention relates to a pharmaceutical composition of tapentadol for parenteral administration which provides prolonged release of tapentadol. Present invention also relates to the process of preparation of pharmaceutical composition of tapentadol for parenteral administration and its use in the treatment of pain.

Abstract: Methods for preconditioning and/or providing neuroprotection to the animal central nervous system against the effects of progressive supranuclear palsy. Therapeutic agents are administered to the upper third of the nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of such therapeutic agents is the iron chelator deferoxamine (DFO). An effective amount of DFO may be administered to the upper third of the nasal cavity of a patient at risk for, or diagnosed with, progressive supranuclear palsy. The effective amount of DFO is delivered directly to the patient's central nervous system for preconditioning, preventing and/or treating the progressive supranuclear palsy.

Abstract: Provided herein are compositions comprising eicosapentaenoic acid (EPA) and polar lipids (e.g., glycolipids and phospholipids), and which do not contain any docosahexaenoic acid (DHA) or esterified fatty acids.

Abstract: The present invention is based on the discovery that parenteral nutrition (PN) induced liver disease, e.g. fatty liver disease, can be prevented and even reversed by administration of primarily omega-3-fatty acid with PN rather than the administration of the standard intravenous lipid emulsions that contain primarily plant derived omega-6 fatty acid. Thus, the present invention provides a method for treating or preventing liver disease in a human patient obtaining nutritional support through PN. The method comprises intravenous administration of an effective amount of an omega-3-fatty acid emulsion to the patient, wherein the patient is not administered phytosterols or plant derived fatty acids, e.g. omega-6 fatty acids derived from a plant source, and wherein the administration of the omega-3-fatty acid emulsion to the patient is for a period greater than three weeks. Preferably, the administration is for a period of greater than six weeks.

Abstract: The present invention relates to novel compounds for modulating US28 receptor activity and methods for their use in preventing or treating US28 receptor-mediated disorders or conditions.

Abstract: The present invention relates to a composition for enhancing collagen production, for enhancing elastin production and/or for enhancing keratinocyte migration, including sesaminol as an active component. The present invention also relates to a method for enhancing collagen production, for enhancing elastin production and/or for enhancing keratinocyte migration, including administering the composition.

Abstract: Substituted indole derivatives of formula (I) wherein the radicals have e.g. the following meaning: R1 is hydrogen, —C1-6-alkyl, R2 is hydrogen, —C1-6-alkyl or cycloC3-12-alkyl; R3 is —OR R4 is hydrogen or halogen, R5 is hydrogen, —C1-6-alkyl R6 is hydrogen, —C1-6-alkyl R is hydrogen or —C1-6-alkyl; X is a group —C(O)CH2— or —CH?CH—; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.

Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from gabapentinoids and the physiologically acceptable salts thereof.

Abstract: This invention relates to the treatment of uveitis, in particular posterior infectious uveitis. In specific embodiments, the invention provides for methods of treating uveitis and/or infectious uveitis comprising administration of a sustained-release system containing 5-amino-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide) and optionally a glucocorticoid. In one embodiment, the glucocorticoid is dexamethasone. In another embodiment, the sustained-release system comprises a polymer such as e.g. polylactic-coglycolic acid.

Abstract: The invention encompasses methods of decreasing the lumenal diameter of a blood vessel by contacting the vessel with a myosin light chain phosphatase inhibitor.

Abstract: Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin.

Abstract: The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin.

Abstract: Provided is the discovery of the role of EphA4 signaling in neurodegenerative disorders involving ?-amyloid induced neurotoxicity such as Alzheimer's Disease. New therapeutic methods, therapeutic agents, and kits for treating diseases caused or exacerbated by overactivated EphA4 signaling are provided. Also provided are methods for identifying additional compounds as therapeutic agents useful for treating conditions involving overly active EphA4 signaling.

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: A nicotine-containing particulate material for release of nicotine, the material comprising a combination of nicotine or a pharmaceutically acceptable salt, complex or solvate thereof and a microcrystalline cellulose, The particulate material is stable upon storage and releases nicotine relatively fast. The particulate material can be used in the manufacture of nicotine-containing pharmaceutical composition, wherein the release of nicotine can be designed to be relatively fast so as to obtain a fast onset of action.

Abstract: The present invention is directed to a composition comprising the following compound: The compound is associated with activity of a muscarinic receptor (e.g. one or more M1, M2, M3, M4 and M5.

Abstract: Provided is a pharmaceutical composition which enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm. The pharmaceutical composition for the inhibition of formation and/or enlargement of cerebral aneurysm or for the regression of cerebral aneurysm of the present invention, which includes a S1P1 receptor agonist as an active ingredient, enables the inhibition of formation and/or enlargement of cerebral aneurysm or the regression of cerebral aneurysm, and enables the prevention and/or treatment of a disease associated with cerebral aneurysm.

Abstract: A method for treating tau-associated disease by administering a pharmaceutical composition comprising a quinoline derivative to a subject in need is disclosed. Particularly, a method for treating Alzheimer's disease by administering a pharmaceutical composition comprising a quinoline derivative to a subject in need is disclosed. The two disclosed quinoline derivatives have the inhibition effect for GSK-3? kinase activity, so as the two disclosed quinoline derivatives have the ability for inhibiting tau hyperphosphorylation or reducing tau aggregation.

Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.