Abstract: Compositions containing 5,6,7-trihydroxyheptanoic acid and analogs and their use for treating posterior segment ocular diseases and diseases characterized by cellular hyperproliferation or angiogenesis, are disclosed.

Abstract: The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among C1-4alkyl, C3-10cycloalkyl, or phenyl, each of which can be substituted by C1-3alkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments.

Abstract: Sodium butyrate was chronically administrated through diet supplementation at 5% w/w in a high fat diet. Supplementation of butyrate prevented development of insulin resistance and obesity in C57BL/6J mice on a high fat diet, and in mice fed on a regular diet of tributyrin. Fasting blood glucose, insulin, and insulin tolerance were all reserved in the butyrate-treated mice. The body fat content was maintained at 10% without a reduction in food intake. Adaptive thermogenesis and fatty acid oxidation were enhanced. An increase in mitochondria function and biogenesis was observed in the skeletal muscle and brown fat, and Type 1 muscle fiber was enriched in the skeletal muscle. In genetically obese mice, supplementation of butyrate led to an increase in insulin sensitivity and reduction in adiposity. Dietary supplementation of butyrate can prevent and treat diet-induced insulin resistance.

Abstract: Methods to cause tissue, such as mucosal cells, to express increased amounts of bactericidal permeability increasing protein (BPI) are described. The BPI inducing agents include, for example, lipoxin compounds.

Abstract: Dietary supplement compositions are disclosed. Methods of making and using dietary supplement compositions are also disclosed.

Abstract: The invention concerns a process for preparing particles, which particles contain one or more spaces in which a gas phase is present which comprises at least one active ingredient, in particular at least one aroma, flavor or precursor for an aroma or flavor, and which space or spaces are at least substantially surrounded by an enveloping phase which at ambient temperature is at least substantially solid and at least substantially impermeable to the active ingredient, comprising allowing the gaseous active ingredient to migrate from or through the enveloping phase into the space or spaces at a temperature at which the enveloping phase is permeable to the gaseous active ingredient; and then cooling the particles to a temperature at which the enveloping phase of the particles is at least substantially impermeable to the active ingredient in the particles.

Abstract: The present invention relates to a method of improving the energy status of an individual by enhancing the usage of lactate. Improved lactate usage is accomplished through a composition comprising lactate precursors, adrenergic receptor agonists and insulinotropic agents.

Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.

Abstract: Described herein are microneedle drug delivery systems comprising a pharmaceutical compositions comprising pharmaceutically active agents (e.g., cannabidiol and prodrugs of cannabidiol) and microneedle arrays suitable for local and systemic delivery of the active agent to a mammal. Also described herein are methods of using a microneedle transdermal or topical drug delivery systems comprising pharmaceutical compositions, comprising cannabidiol and prodrugs of cannabidiol, and microneedle arrays in the treatment disease, including pancreatitis and pancreatic cancer.

Abstract: Medicaments containing shikonin compounds and salts thereof including shikonin and alkannin are used for treatment of virus infections, mycoplasma infections and malignant tumor.

Abstract: Analogs that inhibit the transport of anandamide across cell membranes. The inhibitors are amide and ester analogs of anandamide having a tail portion X that is a fatty acid chain remnant, a central portion Y that is an amide or ester radical and a head portion Z that is selected from a variety of groups including hydrogen, alkyl, hydroxy alkyl, aryl, hydroxy aryl, heterocyclic and hydroxy heterocyclic radicals. The disclosed analogs have potential pharmaceutical uses as drugs for treating a variety of diseases and afflictions, including cardiovascular diseases and blood pressure disorders.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: Methods of retarding formation of a lipofuscin pigment in the retina and of treating or ameliorating the effects of a disease characterized by an accumulation of a lipofuscin pigment in a retina are provided. These methods include the step of administering to a patient in need thereof a substituted C20-retinoid in an amount sufficient to reduce accumulation of a lipofuscin pigment in the retina. Further provided are methods of retarding formation of A2E and/or ATR-dimer by replacing an all-frans-retinal (ATR) substrate with a C20-D3-retinal substrate under conditions sufficient to impede the formation of A2E. Compositions for retarding formation of a lipofuscin pigment in the retina containing a substituted C20-retinoid and a pharmaceutically acceptable carrier are also provided.

Abstract: Disclosed are novel oxylipins, referred to herein as docosanoids, that are derived from C22 polyunsaturated fatty acids, and method of making and using such oxylipins. Also disclosed is the use of docosapentaenoic acid (C22:5n-6) (DPAn-6), docosapentaenoic acid (C22:5n-3) (DPAn-3), and docosatetraenoic acid (DTAn-6: C22:4n-6) as substrates for the production of novel oxylipins, and to the oxylipins produced thereby. Also disclosed is the use of DPAn-6, DPAn-3, DTAn-6, and/or the oxylipins derived therefrom, and/or novel docosanoids derived from the structures of C22 fatty acids, in therapeutic and nutritional or cosmetic applications, and particularly as anti-inflammatory or anti-neurodegenerative compounds. The invention also relates to novel ways of producing long chain polyunsaturated acid (LCPUFA)-rich oils and compositions that contain enhanced and effective amounts of LCPUFA-derived oxylipins, and particularly, docosanoids.

Abstract: An external composition for skin is provided, which gives good warmth without inducing irritation or pain and whose sustainability of warmth is good. The external composition for skin contains (A) an agent for giving warmth and (B) at least one member selected from the group consisting of fatty acid esters of aliphatic polyhydric alcohols and aromatic carboxylic acid esters of lower alcohols or aliphatic polyhydric alcohols.

Abstract: The present invention relates to a novel antimicrobial composition and method comprising any of the C1-C4 monohydric alcohol esters of C8 to C22 fatty acids, and most preferably the C1-C4 monohydric alcohol esters of C8 to C12 fatty acids, namely, caprylic, capric, and lauric fatty acids. Specifically the invention is related to a composition and method to disinfect various surfaces and substrates including the surfaces of food products, animal and human tissue and appendages, inanimate objects of various compositions, and also enclosed spaces. The invention can be incorporated into various media including liquids, gels, powders, paints, sealants, and the like and can be in the form of emulsions including nanoemulsions.

Abstract: Compositions containing 5,6,7-trihydroxyheptanoic acid and analogs and their use for treating posterior segment ocular diseases and diseases characterized by cellular hyperproliferation or angiogenesis, are disclosed.

Abstract: The use of L-carnitine, or one of its pharmaceutically acceptable salts, is described in combination with glucose for the preparation of a medicament useful for diminishing the number of deaths caused by acute myocardial infarction, for reducing the number of days infarction patients spend in intensive care in hospital, and for reducing the number of episodes of post-infarction heart failure, in which the L-carnitine is administered intravenously within only a few hours of the onset of symptoms of acute myocardial infarction at an initial dose of 9 grams a day in combination with 1000-1500 mL of a 5% glucose solution for 5 days, after which the L-carnitine treatment is continued at a dose of 4 grams a day administered orally.

Abstract: Methods for the treatment of CNS disorders using combinations of muscarinic activators and inhibitors, and medicaments comprising muscarinic activators and inhibitors.

Abstract: The present invention relates to methods for preparing liquid valproate compositions comprising solutions of a magnesium valproate and L-carnitine in water and administering said compositions to a subject in need of treatment with valproate and L-carnitine. The compositions of the invention are particularly useful treatments for infants, young children, women of child-bearing age, the aging, institutionalized patients, and patients having dysphagia who are receiving valproate treatment and are at high risk for valproate-related L-carnitine deficiency and cellular dysfunction and hepatotoxicity related thereto.

Abstract: The invention relates to the stimulation of the synthesis and of the activity of an isoform of lysyl oxidase, and more particularly of the LOXL (lysyl oxidase-like) isoform. The invention relates notably to a method of identifying an active principle which stimulates the formation of elastic fibers. The aim of the invention is mainly to provide such a method of identification so as to provide compositions which enable stimulating the formation of elastic fibers.

Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.

Abstract: Novel ester derivatives of ascorbic acid and 2-keto-acid saccharides are provided wherein the ester is introduced by ester bond formation between at least one hydroxy-functionality on the ascorbic acid or 2-keto-acid saccharide and a carboxy-functional organosiloxane, or between a 2-keto-gulonic acid and a hydroxy-functional organosiloxane, as well as methods for their synthesis. Treatment, cosmetic, and personal care formulations comprising the novel esters are also provided, including controlled release forms thereof.

Abstract: This invention relates to methods of using inhibitors of the enzyme acetyl-CoA carboxylase (ACC) for the treatment, prevention, inhibition or alleviation of diseases associated with neuronal hypometabolism and/or loss of cognitive function caused by reduced neuronal metabolism such as, for example, Age Associated Memory Impairment (AAMI), Mild Cognitive Impairment (MCI), Alzheimer's disease, Parkinson's disease, Friedreich's Ataxia (FRDA), GLUT1-deficient Epilepsy, Leprechaunism and Rabson-Mendenhall Syndrome, Coronary Arterial Bypass Graft (CABG) dementia, anesthesia induced memory loss, Huntington's disease and many others.

Abstract: Compounds of the formula (1) in which R1, R2, X, Y and Z are as defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.

Abstract: A skin-sensitizing formulation is provided in an edible, softgel pill. A person engaged in a sexual activity bites down on the pill, thereby effectuating the oral release of the skin-sensitizing formulation. This allows the skin-sensitizing formulation to be spread to a sexual partner, on any part of the skin or sexual region of the body preferably through oral contact with the partner. The skin-sensitizing substance is spread to the partner directly on the skin or through oral contact or beneath a condom worn by the partner. The skin-sensitizing formulation may include an essential mint oil, analog or derivative, and may further includes an enhancer, rubefacient, counterirritant, anesthetic, K-Opoid Receptor activator, or TRPM8 activator. Various inactive ingredients are also disclosed.

Abstract: The invention relates to a medicament containing a compound of general formula (1), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkynyl group, preferably a C11-C15 alkyl, alkylene or alkynyl group, particularly a C11-C13 alkyl, alkylene or alkynyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkynyl group, preferably a C1-C6 alkyl, alkylene or alkynyl group, in particular a C2-C4 alkyl, alkylene or alkynyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m—O]nH group with n=1 to 10, preferably n=1 to 5, m=1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2—(R3)]— group, where R3=independent H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or tu

Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.

Abstract: The current invention provides novel thiotungstate derivatives, methods of making novel thiotungstate derivatives, pharmaceutical compositions of novel thiotungstate derivatives, methods of using novel thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders and obesity and methods of using pharmaceutical compositions of thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-?B dysregulation.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: The onset ratios and pathological conditions of collagen-induced arthritis and adjuvant arthritis in model mice and rats, respectively, were successfully ameliorated by topically expressing the cyclin-dependent kinase inhibitors p161nk4a and p21Cip1 in articular tissues using adenoviral vectors. In the synovial cells of CDKI-transduced mice, expression of inflammatory cytokines was inhibited. Described are the use of the p21Cip1 protein for inhibiting abnormal proliferation of synovial tissues, inflammation in synovial tissues and/or expression of inflammatory cytokines in synovial tissues; the p21Cip1 gene; compounds promoting the activity or expression of the p21Cip1 protein; and pharmaceutical compositions containing these molecules. Also provided are method of screening for compounds participating in the abnormal proliferation of synovial tissues, inflammation in synovial tissues and/or the expression of inflammatory cytokines in synovial tissues targeting the p21Clip1 protein.

Abstract: A method of producing in a composition adapted to be applied to the mucous membranes, the physiological effects of menthol at a reduced menthol concentration, by the partial replacement of menthol by a cooling and flavour blend, including (a) at least one compound selected from the group consisting of lactoyl ethanolamide, nonanoic acid vanillyl amide and menthyl lactate; and (b) at least one compound of the Formula I in which the dotted line represents an optional single bond, the moieties R1, R2, R3, R4 and R5 being independently selected from H, CH3 and OH, three moieties being H, one CH3 and one OH, such that (i) when the optional single bond is absent, one of R1 and R5 is OH only when R3 is H; and (ii) when the optional single bond is present, R3 is CH3 and one of R1 and R5 is OH.

Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.

Abstract: The present invention provides a cooling component or sensate component which does not have undesirable stimulus feeling, bitterness and the like and is excellent in the persistence of refresh-feeling and cool-feeling, a sensate composition which comprises the same, and various products that comprise said sensate composition.

Abstract: Disclosed herein are thiocolchicine derivatives suitable for use as muscle relaxants, methods of making the derivatives, and compositions comprising the derivatives.

Abstract: The present invention provides a novel amorphous form of fesoterodine fumarate, process for preparation, pharmaceutical compositions, and method of treating thereof.

Abstract: In recent years the demand for cosmetic compositions and cosmetic methods for improving the appearance and condition of skin has grown enormously; consumers are seeking topical skin care products that help treat or delay the signs of natural (chronoaging) and environmental aging. The present invention relates to topical compositions for application to human skin and to their use in improving the condition and appearance of skin. It is based on the premise that effective treatment of normal skin conditions due to natural or environmental aging, such as wrinkles, lines, sagging, hyperpigmentation and age spots, and/or of sensitive, dry, rough, flaky, red, itchy, irritated skin may be obtained through the application of cosmetic compositions to the skin which comprise a combination of collagen stimulators, phytoestrogens, plant derived anti-inflammatory agents, fatty acid, antioxidants.

Abstract: The subject disclosure provides compositions for reducing serum cholesterol and/or triglyceride levels in subjects. These compositions can comprise racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, esters of D-?-hydroxybutyrate, oligomers of D-?-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol or R-1,3 butandiol alone and can be, optionally, administered in conjunction with a low fat diet to a subject.

Abstract: A cosmetic or dermatological composition characterized in that it comprises an association between an elastase inhibitor compound of the N-acylaminoamide family and at least one metalloproteinase inhibiting compound.

Abstract: The present invention concerns enhancements in the cooling effects of certain physiological coolant-containing compositions such as topically applied cosmetic, toiletry or pharmaceutical products, wherein the cooling effect of the physiological coolants is enhanced by the addition of a substance according to formula (I) or dermatologically acceptable salts thereof: R1—CR2(OR3)—CO—NR4—CR5R6—X—OR7??(I) It was found that substances represented by formula (I) are capable of bringing about greater cooling effects from reduced concentrations of physiological coolants without behaving as physiological coolants themselves, thereby enabling the preparation of compositions that do not necessarily have the characteristic minty odour of menthol-containing products and/or to allow greater freedom in creating perfumed products.

Abstract: The invention relates to the use of esters of 2-ethylbutanol with C4-36 carboxylic acids or C4-36 dicarboxylic acids in cosmetics and/or pharmaceutical preparations. The compounds are characterised by a particularly light feeling.

Abstract: A composition for hyperuricemia disease or a related disorder, use thereof and method of using thereof are provided.

Abstract: The present application describes an ethyl acetate fraction of Melissa leaf having excellent angiogenesis and MMP inhibitory activities, and a composition comprising the same.

Abstract: The present disclosure relates to lipid compounds of formula (I): wherein: R1 is chosen from a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and are chosen from hydrogen and a C1-C6 alkyl; X is chosen from O, S, SO, SO2, Si, and Se; n=1 or 3; and P1 is chosen from hydrogen; a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; a group of formula (II) or formula (III), wherein P2, P3, and P4 are chosen from hydrogen, an alkyl, an alkenyl, and an alkynyl, optionally substituted; and a group of formula (IV) or formula (V), wherein P5 is chosen from hydrogen and a C1-C6 alkyl; or a pharmaceutically acceptable salt, complex, or solvate thereof.

Abstract: The present invention provides a cooling component or sensate component which has further strong cooling intensity and is excellent in the persistency or refresh-feeling and cool-feeling, a sensate composition comprising the same, and various products comprising the sensate composition.

Abstract: The invention is directed to novel pharmaceutical compositions comprising chemicals agents that are useful in the treatment and prevention of cystic fibrosis and the prevention of signs and symptoms of this disease. These pharmaceutical compositions are surprisingly successful in the treatment disorders related to cystic fibrosis including disorders of blood production. Many of these compositions of the invention are even more effective when administered to a patient in pulses. Pulse therapy is not a form of discontinuous administration of the same amount of a composition over time, but comprises administration of the same dose of the composition at a reduced frequency or administration of reduced doses.

Abstract: Antimicrobial compositions comprising one or more compound components generally recognized as safe for human consumption, and related methods of use, such compositions and methods as can be employed in a wide range of agricultural, industrial, building, pharmaceutical and/or personal care products and applications.

Abstract: A composition for external application to skin, containing a compound represented by formula (I) or a salt thereof, and/or a quaternary ammonium salt represented by formula (II): wherein R1 is a substituted or unsubstituted, linear or branched chain alkyl group having 2 to 25 carbon atoms; X is —CO—NH—, —O—CO—O—, —NH—CO—, —CO—O—, —O—CO— or —O—; Y is a substituted or unsubstituted alkylene group having 1 to 4 carbon atoms; R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R3 is an alkyl group having 1 to 4 carbon atoms; R2 and R3 are the same as or different from each other; R4, R5 and R6, which may the same as or different from each other, each are an alkyl group having 1 to 4 carbon atoms; and A? is a counter ion.

Abstract: The present invention relates to a lipid composition comprising at least omega-3 polyunsaturated alcohols, or pro-drugs thereof, which omega-3 polyunsaturated alcohols, or pro-drugs thereof, comprising at least (all-Z)-5,8,11,14,17-eicosapentaen-1-ol, or pro-drug thereof, and (all-Z)-4,7,10,13,16,19-docosahexaen-1-ol, or pro-drug thereof, and their use as a pharmaceutical, in particular for the treatment of elevated triglyceride levels. The invention also relates to methods for the preparation of these pro-drugs from marine oils.

Abstract: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (TOP) in the eye. In one embodiment, the microspheres are formed from polylactide-co-glycolide (“PLGA”); in another embodiment, the microspheres are formed from a blend PLGA and poly lactic acid (“PLA”).