Abstract: Effective implantable medical devices for reducing and treating post-operative pain are provided. The implantable medical device comprises clonidine in an amount from about 1 wt. % to about 30 wt. % of the implantable medical device. At least one biodegradable polymer and a pore forming agent in an amount from about 1 wt. % to about 30 wt. % of the implantable medical device is also provided. The implantable medical device is configured to release the clonidine over a period of at least 48 hours. Methods of use are also disclosed.

Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.

Abstract: The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using ?1-adrenergic receptor (?1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.

Abstract: Disclosed is a pharmaceutical composition for the prevention or treatment of ischemic heart diseases, comprising as an active ingredient an inhibitor which acts to restrain mononuclear phagocyte system cells from synthesizing or releasing AGE-albumin, which induces the apoptosis of cardiomyocytes upon the onset of the ischemic heart disease. Also, a method is provided for screening an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells. Inhibitory or suppressive of AGE-albumin-induced cell death, the pharmaceutical composition comprising as an active ingredient an inhibitor against the AGE-albumin synthesis or release of mononuclear phagocyte system cells can be applied to the prevention or treatment of a wide spectrum of ischemic heart diseases including myocardial infarction.

Abstract: Methods for treating cognitive dysfunction by modulating brain energy metabolism using cyclocreatine or a pharmaceutically acceptable salt thereof are discussed.

Abstract: The present invention relates to tetracaine based anesthetic formulations and methods of use thereof. The invention further relates to topical formulations of tetracaine and methods of topically anesthetizing body tissues. The present invention also relates to tetracaine based dental anesthetic formulations and methods for anesthetizing the maxillary dental arch using these formulations.

Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).

Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Abstract: Biocompatible intraocular implant systems are formulated for discontinuous or intermittent release of therapeutic levels of a therapeutic agent (such as a steroid) to minimize development of side effects associated with continuous or long term use of such agent. The implant system may comprise one or more implant, and preferably, although not necessarily, also contains an auxiliary agent having an activity effective to lessen at least one side effect associated with said therapeutic agent compared to the use of an otherwise identical implant system lacking said auxiliary agent. The implants containing the therapeutic agent and auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the ocular side effects otherwise accompanying the use of such therapeutic agent.

Abstract: The invention provides methods, compositions, and kits containing phentolamine for improving visual performance. In particular, the invention provides improvement in visual performance, such as improvement in visual acuity, by daily ophthalmic administration of a phentolamine solution to an eye of a patient at or near the bedtime of the patient for an extended duration while minimizing the occurrence of adverse side effects, such as eye redness during the patient's waking hours.

Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Abstract: The invention provides aqueous ophthalmic solutions of phentolamine or pharmaceutically acceptable salts thereof, medical kits, and methods for using such ophthalmic solutions to improve visual performance in a patient. Exemplary aqueous ophthalmic solutions include those containing phentolamine mesylate, mannitol, sodium acetate, and water.

Abstract: An implantable drug depot useful for preventing, reducing or treating bleeding at a surgical site beneath the skin in a patient is provided. The implantable drug depot comprises a therapeutically effective amount of clonidine or a pharmaceutically acceptable salt thereof, and at least one biodegradable polymer. The drug depot is capable of releasing clonidine or a pharmaceutically acceptable salt thereof over a period of at least three days.

Abstract: The present disclosure provides novel formulations for treating foot or hand pain by topically administering a sympathomimetic drug, particularly oxymetazoline, to the skin of the foot or hand.

Abstract: This invention relates to a new application of compound Clonidine Hydrochloride in a use of preparation of information intervention agent, a new preparation method of information intervention agent, and a product. The Clonidine Hydrochloride interacts with the human information receptor, therefore realizing the intervention through the Clonidine Hydrochloride information physical method, and treatment was not a chemical treatment. This invention comprises: putting the compound Clonidine Hydrochloride information package filler (3) into a container (4), closing the lid (7), sealing by a glue, attaching a hanging piece to the container (4) to form the Clonidine Hydrochloride information intervention agent (9) for clinical use. The usage of this invention is simple, convenient, safe, reliable and easy to accept. It is especially appropriate for use by senior people, unhealthy people, children, or people with disturbance of consciousness, mental retardation, and behavioral disorders.

Abstract: Formulations have been developed which assist individuals having an addiction such as smoking to reduce or quit engaging in the addictive behavior. Representative behaviors include smoking, excessive alcohol or food ingestion, drug addiction, and ingestion of caffeine or junk food providing quick “highs”. The formulations assist the smoker to become dissatisfied with smoking, until he or she willingly gives up the habit or at least cuts down on the number of cigarettes smoked per day as an initial step towards quitting in the future. The formulations can also be used in conjunction with other known formulations, such as nicotine gum or patch. The formulations contain hydrophilic polymers, for example, polyethylene glycol (PEG) alone or in combination or polyvinyl pyrrolidone (PVP) (also known as povidone or polyvidone alone or in combination.), sweeteners and/or flavorings, viscosity modifiers/binders, and pH or buffering agents.

Abstract: A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Abstract: The invention features topical formulations comprising an osmotically active agent and/or a vasoconstrictor and/or an astringent agent for the treatment and prevention of eyelid swelling, and methods of use thereof.

Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.

Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.

Abstract: The invention relates to the use of antioxidants such as, ascorbic acid (Vitamin C), Tocopherol (Vitamin E), vitamin A and polyphenols, for the treatment of cognitive and behavioural disorders in patients with Fragile X syndrome. Specifically, the invention relates to the use of said antioxidants in a pre-determined concentration in a therapeutic doses, in order to obtain the greatest amount of antioxidants possible in all the tissues of the organism, so as to eliminate the excess free radicals produced in the cells and to treat the aforementioned cognitive and behavioural disorders in patients with Fragile X syndrome.

Abstract: Compositions and methods related to ophthalmic use of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymers and therapeutic uses are described herein.

Abstract: Presented herein inter alia are novel methods of treating heart and brain diseases.

Abstract: An article that is a porous, dissolvable solid structure that dissolves easily due to the shape, product orientation and/or method of manufacturing the porous, dissolvable solid structure. The process of making the Article involves preparing a pre-mixture, aerating the pre-mixture, dosing the pre-mixture into individual cavities in molds, and drying the pre-mixture to an Article having an open celled foam with a % open cell of from about 80% to about 100%.

Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.

Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a therapeutically effective amount of clonidine or pharmaceutically acceptable salt thereof and a polymer; wherein the depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the depot is capable of releasing (i) about 5% to about 45% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a first period of up to 48 hours and (ii) about 55% to about 95% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a subsequent period of at least 3 days.

Abstract: An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours.

Abstract: Methods and products for treating or preventing erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical aqueous gel composition comprising about 0.01% to about 10% by weight of at least one ?-adrenergic receptor agonist and a pharmaceutically acceptable carrier.

Abstract: A nasal delivery device for and method of delivering a substance, preferably comprising oxytocin, non-peptide agonists thereof and antagonists thereof, preferably as one of a liquid, as a suspension or solution, or a powder to the nasal airway of a subject, preferably the posterior region of the nasal airway, and preferably the upper posterior region of the nasal airway which includes the olfactory bulb and the trigeminal nerve, and preferably in the treatment of neurological conditions and disorders.

Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.

Abstract: An alpha2 adrenoreceptor agonist eg. clonidine, brimonidine, monoxidine, lofexidine is useful for the treatment of siaiorrhoea, administered by the paraungual, sublingual or buccal route. The patient to be treated is also given an anti-muscarinic agent eg. oxybutynin, glycopyrrolate, ipratropium.

Abstract: The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid.

Abstract: The present invention is directed to a method for treating a patient suffering from a metabolic disorder such as the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, and the metabolic sequale of these diseases including cardiovascular, cerebrovascular, renal and hepatic diseases, comprising the step of: administering to a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject.

Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.

Abstract: A medicament tablet containing paracetamol (acetaminophen) as the (or an) active ingredient, and an encapsulated flavorant. The tablet may be swallowed in tablet form or may be dissolved or dispersed in water to form a palatable drink.

Abstract: The present invention is directed to a topical ophthalmic composition for a liquid comprised of clear colloidal polar nanolipids delivered in submicron sized particles, aqueous colloidal lubricants, aqueous polymers, emulsifies, and a unique stabilizing buffer system, which undergoes a liquid-gel phase transition in the eye. Said composition is designed to deliver advanced eye lubricants, protect the three (3) layers of corneal film from dryness, and provide a unique system of Dry Eye treatment that addresses and treats all three layers of corneal tear film. Said composition is further designed to provide a superior delivery system of various Active Pharmaceutical Ingredients (APIs), and/or anti-infective/antibiotic/anti-fungal agents, accepted as safe and efficacious for ophthalmic use.

Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

Abstract: A nasal delivery device for and method of delivering a substance, preferably comprising oxytocin, non-peptide agonists thereof and antagonists thereof, preferably as one of a liquid, as a suspension or solution, or a powder, to the nasal airway of a subject, preferably the posterior region of the nasal airway, and preferably the upper posterior region of the nasal airway which includes the olfactory bulb and the trigeminal nerve, and preferably in the treatment of neurological conditions and disorders.

Abstract: A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase II? and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo II? have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.

Abstract: Compositions, products and methods including silicone based excipients are provided. The compositions, products and methods of the present invention are particularly useful for the treatment of ophthalmic diseases.

Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.

Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.

Abstract: The invention is directed to the therapeutic use of arylsulfonamide derivatives.

Abstract: The present invention relates to a process for the preparation and purification of olmesartan medoxomil hydrohalide salts and optionally converting them to olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.

Abstract: Disclosed herein is a method of upregulating regulatory T-cells, and treating diseases that would benefit from such upregulation, by administering an alpha 2 receptor agonist.

Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.

Abstract: The present invention concerns a pharmaceutical composition comprising an alpha-2 adrenergic receptor agonist for preventing or treating inflammatory pain and diseases in mucosa of oral cavity, pharynx and larynx. In another aspect the present invention provides mucosal bioadhesive slow release carriers for the extended and controlled release of alpha-2 adrenergic receptor agonists that can be used on mucosal surfaces for preventing or treating inflammatory pain and diseases in mucosa of oral cavity.

Abstract: The implant design is a drug loaded polymer device, such as a rod, designed to control the release of a biologically active agent, such as clonidine or its derivatives, such as clonidine HCl for a prolonged period of time, such as 2 months, 3 months, 4 months, and even 4.5 months. The polymer is preferably a biodegradable polymer, such as poly(lactide-co-glycolide) or polylactic acid/polylactide. The challenge in using the HCl salt forms of drugs such as clonidine, is controlling the release of the highly water soluble drug for up to 4.5 months. It has been found that by controlling the particle size distribution of the drug powder, the drug distribution within the polymer matrix is more uniform and can be controlled. Therefore, the large aggregates, which cause rapid drug release can be eliminated.

Abstract: In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.