Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders.

Abstract: The present invention relates to a formulation comprising an endothermic cooling agent selected from the group consisting of xylitol, sorbitol, mannitol and erythritol having a heat of enthalpy between ?10 cal/g and ?100 cal/g, and one or more active agents wherein the endothermic agent is present in the formulation at an amount less than 10% w/w.

Abstract: The invention concerns the use of 2E,4E-decadienoic acid-N-isobutylamide (trans-pellitorin) as flavorant, in particular as salivation inducing flavor substance, preferably in a foodstuff or nutrient, an oral hygienic preparation or a gourmet or snack preparation. Further, the invention concerns preparations, semi-finished preparations as well as fragrance, aroma and taste compositions, containing trans-pelletorin as well as a processes for the production of trans-pelletorin.

Abstract: A system and method to improve sensory functions in the hand or foot by dermal topical application of a local anaesthetic substance to adjacent skin areas, using a tailored application device or kit specially designed to fit the size and anatomical shape of the body part which is to be anaesthetised. The concept is to block sensory input from the anaesthetised skin area hereby inducing a functional reorganisation in sensory brain cortex resulting in enhanced sensory functions in body parts adjacent to the anaesthetised area with focus on the hand and sole of the foot.

Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.

Abstract: Antagonists of S1P3 (Edg-3) receptors are provided for attenuation of Smad signaling in a method of down-regulation of receptor signaling and downstream decreased production of connective tissue growth factor in ocular disorders involving CTGF accumulation. Ocular disorders involving inappropriate CTGF accumulation include ocular hypertension, glaucoma, glaucomatous retinopathy, optic neuropathy, macular degeneration, diabetic retinopathy, choroidal neovascularization, proliferative vitreoretinopathy and ocular wound healing, for example. Such disorders are treated by administering antagonists of the present invention.

Abstract: Pharmaceutical compositions comprising an aptamer and an amino acid ester or amide or an aptamer; a divalent metal cation; and a carboxylic acid, a phospholipid, a phosphatidyl choline, or a sphingomyelin. Methods of treating or preventing a condition in an animal comprising administering to the animal the pharmaceutical compositions.

Abstract: The invention relates to methods of inducing smooth muscle relaxation, for example, a method of inducing relaxation of a vascular or a non-vascular muscle or a method of inducing relaxation of the microvasculature, in a subject in need thereof by promoting the accumulation of protoporphyrin IX in the smooth muscle.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

Abstract: The invention provides methods of treating depressive disorders, in particular major depression but other depressive orders also, with prodrug stimulants or analogs including amphetamine prodrugs, methylphenidate prodrugs, and methylphenidate analogs, Such methods of treatment may utilize the prodrug stimulant or analog as monotherapy or, more commonly, as an adjunct to antidepressant medication treatment to augment their effect. The invention includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered to an individual in need with one or more other active agents, either in separate forms or as a single pharmaceutical formulation. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.

Abstract: The invention relates to compounds, which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, in addition to conjugates from the compounds comprising biomolecules or pharmaceutically active substances. The inventive compounds are highly cross-linked and can be formed in a simple manner by using a central cross-linking module. The invention also relates to the use of conjugates as an improved formulation of pharmaceuticals and to the production thereof.

Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.

Abstract: Implant devices for intravesical administration and local drug delivery. The device has a body which includes a hollow tube formed of a biocompatible material; at least one reservoir in the tube which contains a drug; and one or more apertures through which the drug can be released. The device is configured for minimally invasive insertion into a body cavity, such as the bladder. The hollow tube may be elastomeric to permit the device to be elastically deformed from its initial shape into an elongated shape for passage through a catheter, where following such passage the device can return to or toward its initial shape to facilitate retention of the device in the body cavity. The body may have a narrow, elongated shape effective to permit insertion of the drug delivery device through a catheter without necessarily deforming the body, yet include flexible projections which effect retention within the body cavity.

Abstract: A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.

Abstract: Provided herein are methods of utilizing bile acid transport inhibitors for the treatment of obesity and diabetes.

Abstract: Compositions containing a delivery system including polymeric microparticles capable of undergoing a visual change, such as a color change, after application to a substrate are disclosed. The delivery system informs a consumer that the composition has been properly applied and/or has performed its intended function.

Abstract: The present invention describes compounds, compositions and methods of using the same comprising lysine covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

Abstract: The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.

Abstract: Described herein are polysaccharide gel formulations including at least one inhibitor of polysaccharide degradation and methods of making the same. The methods described herein involve the steps of providing at least one polysaccharide and incorporating at least one inhibitor of degradation into the polysaccharide.

Abstract: A topical opioid paradigm was developed to determine analgesic peripheral effects of morphine. Topical morphine as well as peptides such as [D-Ala2,MePhe4,Gly(ol)5]enkephalin (DAMGO) produced a potent, dose-dependent analgesia using the radiant heat tailflick assay. The topical drugs potentiated systemic agents, similar to the previously established synergy between peripheral and central sites of action. Local tolerance was rapidly produced by repeated daily topical exposure to morphine. Topical morphine tolerance was effectively blocked by the N-Methyl-D-Aspartate (NMDA) receptors antagonist MK801 and ketamine given either systemically or topically. NMDA receptor antagonists reversed pre-existing morphine tolerance. The activity of topical NMDA antagonists to block local morphine tolerance suggests that peripheral NMDA receptors mediate topical morphine tolerance.

Abstract: The invention concerns the use in a cosmetic composition of at least a poly-aminoacid of general formula (1) in which X is —O—, —S— or —NR3; R represents in particular a hydrogen atom or a C1-C10 alkyl radical; R2 represents in particular a hydrogen atom or an optionally substituted alkyl radical; R3 represents a hydrogen atom or an alkyl radical; R4 represents a hydrogen atom or a radical such as NH2, OH, SH, —CHOHCH3, —CONH2; n is a number greater than 1 such that the poly-aminoacid derivative molecular weight ranges between 200 and 200000. The invention also concerns the use of said derivatives for keratinous fibre strengthening and care.

Abstract: The present invention relates to a nanoparticulated anaesthetic composition for topical use in which at least one local anaesthetic agent is encapsulated in polymeric nanoparticles. The present invention also relates to the use of such polymeric nanoparticles comprising at least one local anaesthetic agent in the preparation of an anaesthetic composition for topical application to the skin or mucosa.

Abstract: Self-learning process for automatically adjusting a dosage of a substance administered to a person by a drug delivery device, a drug delivery device, wherein a dosage of a substance is adjusted by such a self-learning process and a drug delivery system comprising such a drug delivery device. Pain is experienced differently at certain times of day due to the origin causing the symptoms. Therefore, the medication providing pain relief should also be adjusted accordingly. The invention is to anticipate the pain experience and to deliver pain relief medication in such a way that Quality of Life is improved by appropriate timing of the right amount of medication and by appropriate timing of turning off the medication to reduce side effects.

Abstract: The present invention relates to anti-viral uses of leflunomide product, alone or in combination with other anti-viral agents, or in combination with a pyrimidine such as uridine.

Abstract: Systems and methods are provided for dispensing compositions comprising sols, sol-forming compounds, or highly viscous compositions into porous substrates. In some embodiments, the porous substrates are elements of transdermal delivery devices. In some embodiments, the highly viscous compositions comprise alkylcellulose ethers, or derivatives thereof, in particular, hydroxypropyl cellulose. Such may be useful in continuous web-based manufacturing processes.

Abstract: Amide compounds, amide polymers, compositions including amide compounds and amide polymers may be used to bind target ions, such as phosphorous-containing compounds in the gastrointestinal tract of animals. In some cases, amide compounds and amide polymers may include a core derived from an amide polyol and an organic polyacid or ester.

Abstract: The present invention provides compounds of formula (I), wherein k, Ar, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention provides unbranched aliphatic polyamines for use in therapy, particularly for use in the treatment of psoriasis and compositions containing polyamines.

Abstract: Methods for disrupting amyloid fibrils in a subject, comprising combining an effective amount of a ?-2 microglobulin fibril disrupting compound with a medium associated with the subject, are disclosed. The invention also relates to combining the ?-2 microglobulin fibril disrupting compound ex vivo with the blood during dialysis treatment of an animal. It also relates to methods for determining which compounds are effective at disrupting amyloid fibrils in a medium.

Abstract: The present invention provides a method for ameliorating cue-induced cravings for an addictive substance in abstinent addicts by administering a compound capable of blockade of GluR2-lacking AMPA receptors.

Abstract: A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.

Abstract: A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general surgical, therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents, including at least one local anesthetic agent, and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents.

Abstract: Disclosed herein are soft tissue fillers, for example, dermal and subdermal fillers, based on hyaluronic acids and pharmaceutically acceptable salts thereof. In one aspect, hyaluronic acid-based compositions described herein include a therapeutically effective amount of at least one anesthetic agent, for example, lidocaine. The present hyaluronic acid-based compositions including lidocaine have an enhanced stability, relative to conventional compositions including lidocaine, for example when subjected to sterilization techniques or when stored for long periods of time. Methods and processes of preparing such hyaluronic acid-based compositions are also provided.

Abstract: Disclosed herein are cohesive soft tissue fillers, for example, dermal and subdermal fillers, based on hyaluronic acids and pharmaceutically acceptable salts thereof. In one aspect, hyaluronic acid-based compositions described herein include a therapeutically effective amount of at least one anesthetic agent, for example, lidocaine. The present hyaluronic acid-based compositions including lidocaine have an enhanced stability and cohesivity, relative to conventional compositions including lidocaine, for example when subjected to sterilization techniques or when stored for long periods of time. Methods and processes of preparing such hyaluronic acid-based compositions are also provided.

Abstract: Composition and method for the inhibition of microbial growth in alkaline aqueous media requiring both rapid decontamination and long term preservation. The composition is a blend of 2,2-dibromo-3-nitrilopropionamide and 2-bromo-2-nitro-1,3-propanediol.

Abstract: The invention relates to a drug delivery system for the topical administration of therapeutic agents.

Abstract: A pharmaceutical anti-inflammatory preparation and method for preparation and treatment of arthritis and related inflammatory conditions used for mild to severe pain for relatively long acting results. This anti-inflammatory preparation comprises anti-inflammatory corticord steroid in aqueous-like suspension, a muscle relaxant in oil-like composition, and amide anesthetic compound in aqueous-like composition and Vitamin B-12 in aqueous-like composition. It is prepared by mixing the anti-inflammatory preparation at a rate and for a time sufficient to create a suspended emulsion. The anti-inflammatory preparation is administered while in suspended emulsion by intramuscular patient injection.

Abstract: Methods and compositions for treating skin conditions, in particular jellyfish stings, are provided.

Abstract: The present invention relates to a method for reducing electrical disturbance of a cell's resting membrane potential comprising administering an effective amount of a composition comprising an effective amount of a local anaesthetic and of one or more of a potassium channel opener, an adenosine receptor agonist, an anti-adrenergic, a calcium antagonist, an opioid, an NO donor and a sodium hydrogen exchange inhibitor.

Abstract: A dual adhesive layer dosage form for delivery of active agent to and across, the mucosa is disclosed. Particularly, bioadhesive tablets for administration at the vaginal mucosa are disclosed as having a central active layer sandwiched between two bioadhesive layers.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).

Abstract: An electrical stimulation method for the treatment of peripheral neuropathy is disclosed. In a preferred embodiment, the method utilizes an electrical stimulation device that includes a plurality of channels of electrodes each of which includes a first and second electrode positioned in electrical contact with tissue of a target region suffering from peripheral neuropathy. Agonist/antagonist muscles involved in abduction/adduction, flexion/extension, supination/pronation, protraction/retraction, and/or eversion/inversion in the peripheral body regions are stimulated with a patterned series of electrical pulses through channels of electrodes in accordance with a procedure for treating peripheral neuropathy.

Abstract: Described herein are transdermal delivery devices composed of at least one resealable injection port and at least one local anesthetic reservoir. The device effectively delivers anesthetic to the skin of the subject prior to puncturing the skin by syringes, needle sticks, or other instruments intended to be inserted into the skin. In addition, this device can be used to deliver various therapeutic agents for either locally or systemically.

Abstract: A method of potentiating the activity of a drug which affects the central nervous system (CNS) comprising systemically administrating to a subject said drug together with an effective amount of a compound which stimulates peripheral chemoreceptors of vagal afferents and, optionally, with an effective amount of a stimulator of peripheral osmoreceptors of vagal afferents. Also disclosed are pharmaceutical compositions for systemic administration comprising a CNS drug together with the aforementioned compounds.

Abstract: The present invention is directed to compositions and methods for the transdermal delivery of a pharmaceutically active compound. In some embodiments, the addition of inert pharmaceutical ingredients in place of a portion of adhesive in a transdermal patch formulation increases the rate of skin permeation of a pharmaceutical compound.

Abstract: The present invention relates to a method for arresting, protecting and/or preserving an organ which includes administering effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) local anaesthetic to a subject in need thereof. The present invention also relates to a method for arresting, protecting and/or preserving an organ which comprises adding a composition which includes effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) a local anaesthetic to the organ. The present invention further provides a pharmaceutical or veterinary composition which includes effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) a local anaesthetic.

Abstract: A coated spherical capsule that comprises a seamless capsule and an edible coating is disclosed. The seamless capsule includes a seamless solid shell surrounding a mononuclear liquid or viscous core and the edible coating surrounding the seamless capsule. The edible coating can include at least one dietary supplement and at least one sugar or sugar alcohol. The liquid or viscous core can include 1-100% of a flavoring, based on total weight of the liquid or viscous core. The edible coating can include an effective amount of the at least one dietary supplement based on the weight of the edible coating. Also disclosed is a method of administering an effective amount of a dietary supplement. The method includes providing a plurality of coated spherical capsule and ingesting at least one coated spherical capsule for two or more days in order to deliver an effective amount of a dietary supplement.