Abstract: The present invention relates to a preventive and/or a therapeutic agent for inflammatory bowel diseases containing a fermentation product of a propionic acid bacterium as an active ingredient.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from resveratrol compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of resveratrol compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the resveratrol compound is concentration dependent, with the amount of resveratrol photostabilization increasing with the concentration of the alkoxycrylene compound.

Abstract: Neurite outgrowth-promoting prostaglandins (NEPPs) and other electrophilic compounds bind to Keap1, a negative regulator of the transcription factor Nrf2, and prevent Keap1-mediated inactivation of Nrf2 and, thus, enhance Nrf2 translocation into the nucleus of neuronal cells. Therefore, neuroprotective compositions and related methods are provided that employ such neuroprotective compounds, and prodrugs of such compounds, to cause dissociation of Nrf2 from a Keap1/Nrf2 complex.

Abstract: One embodiment relates to a method of treating pulmonary hypertension based upon co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension. The benefit of the co-administration of these agents is to eliminate or reduce one or more side effects associated with mono-therapy of either agent, as well as one or more side effects associated with other administration routes such as subcutaneous or intravenous administration.

Abstract: The invention is generally directed to a drug-release composition that contains drug-linker-drug compound that is combined with another therapeutic agent that can be an antirestenotic agent. The therapeutic agent can be partially bound to the drug-linker-drug compound, miscible with the drug-linker-drug compound, combined with the drug-linker-drug compound at various ratios, and tuned to control the release of drugs to a tissue in need thereof.

Abstract: The present invention relates to a method for treating and screening for compounds for the treatment of sepsis. More specifically, the treatment and screening methods are based on the discovery that granzyme B containing platelets (GzmB-platelet) causes apoptosis by direct contact with cells.

Abstract: A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.

Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Examplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative therof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.

Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.

Abstract: Provided herein are methods of treatment of prostate intraepithelial neoplasia (PIN) by administering bexarotene. Also provided are pharmaceutical compositions and dosing regimens.

Abstract: Buffer solutions for pharmaceutical preparations that have bactericidal activity preferentially against gram negative bacteria are provided. The buffers have a pH of greater than about 10 or less than about 4.5 with low buffer capacity. Methods of their use in reducing the occurrence of blood stream infections in a mammal is also provided.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.

Abstract: Provided herein are methods and materials for treating pulmonary hypertension (PH) in a subject. Also provided herein is a method of diagnosing whether a has PH by detecting a PH marker. A PKG pulmonary hypertension marker has been identified and may be useful in predicting PH disease progression and assessing a subject's response to PH therapy.

Abstract: The invention relates to liquid pharmaceutical compositions for oral administration comprising rhein or diacerein, or salts or esters or prodrugs thereof and processes for preparing such compositions.

Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.

Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.

Abstract: The present invention provides a micelle comprising an amphiphilic block copolymer, said amphiphilic block copolymer consisting of (a) a hydrophobic polymer attached to the 5? end of a first nucleic acid molecule, wherein said first nucleic acid molecule is hybridized with a second nucleic acid molecule, wherein a targeting unit capable of selectively binding to a specific cell type and/or tissue is attached to the 5? end of said second nucleic acid molecule; and/or (b) a hydrophobic polymer attached to the 3? end of a first nucleic acid molecule, wherein said first nucleic acid molecule is hybridized with a second nucleic acid molecule, wherein a targeting unit capable of selectively binding to a specific cell type and/or tissue is attached to the 3? end of said second nucleic acid molecule.

Abstract: The unexpected expression of tryptophan 2,3-dioxygenase (TDO2) in cancer cells and tumors has been established. Methods for diagnosing cancer based on the expression of TDO2 are provided, as are methods for treating cancer and inhibiting the growth of cancer cells by inhibiting TDO2, as well as pharmaceutical compositions.

Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.

Abstract: Novel dermatological depigmentation compositions, especially for topical application, contain as pharmaceutical active agents a dissolved phenolic compound and a retinoid, formulated as anhydrous compositions free of petroleum jelly and free of elastomer. The present invention relates to a novel depigmenting composition especially for topical application, comprising as pharmaceutical active agents a dissolved phenolic derivative and a retinoid, in the form of an anhydrous composition free of petroleum jelly and free of elastomer, to the process for preparing it and to its use in dermatology.

Abstract: The present invention relates to compositions and methods for preventing migraines. The migraine prophylaxis composition is a single dosage form comprising at least one form of elemental magnesium and at least one NSAID. The prophylaxis composition, comprising at least one form of elemental magnesium and a therapeutically effective concentration of acetylsalicylic acid may also provide cardiac protection and prevent cardiovascular diseases.

Abstract: Buffer solutions for pharmaceutical preparations that have bactericidal activity preferentially against gram negative bacteria are provided. The buffers have a pH of greater than about 10 or less than about 4.5 with low buffer capacity. Methods of their use in reducing the occurrence of blood stream infections in a mammal is also provided.

Abstract: A novel maintenance therapy regime/regimen for the treatment of acne related diseases includes administering an oral antibiotic with a topical fixed-dose combination of a retinoid, such as adapalene, and an anti-bacterial agent, such as benzoyl peroxide.

Abstract: An active agent delivery composition is provided that allows topical delivery of active agents including vitamin A and its derivatives. A polyhalogenic vehicle such as methoxyonafluorobutane or ethoxyonafluorobutane serves as a coupler for an active agent and a silicone carrier so as to allow solubilization of active agents not normally miscible in silicones and providing a moisture maintaining composition.

Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from retinoid compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of retinoid compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the retinoid compound is concentration dependent, with the amount of retinoid photostabilization increasing with the concentration of the alkoxycrylene compound.

Abstract: A cooling composition comprising at least one compound of the Formula I in which R is selected from the group of moieties consisting of (CH2)nCOOR?; (CH2)nCONMe2; (CH2)nOR?; and CHNH2CH3; where n is 1-3 and R? is independently selected from hydrogen, methyl and ethyl; and R? is selected from the group consisting of the moieties fenchyl, D-bornyl, L-bornyl, exo-norbornyl, 2-methylisobornyl, 2-ethylfenchyl, 2-methylbornyl, cis-pinan-2-yl, verbanyl and isobornyl. The compositions are useful in providing cooling sensations to the skin or mucous membranes of the body.

Abstract: Patients which are treated with stimulants (e.g., CNS stimulants, sympathomimetic amine, or anorectic/anorexigenic), such as patients being treated for attention deficit/hyperactivity disorder or obesity, often are atrisk in developing high blood pressure. Similarly, patients which are treated with analgesics such as non-steroidal anti-inflammatory drugs (NSAIDs) over an extended period of time risk developing high blood pressure. These and other iatrogenic therapies (therapies which inadvertently cause an increase in, e.g., blood pressure) are addressed by providing the patient with one or more antihypertensive drugs, most preferably calcium channel blockers, during the treatment period. The CNS or NSAIDs can be provided separately or together with the antihypertensive drugs or as part of a combined composition. The adjunctive therapy can prevent or reduces cardiovascular disease and other complications of high blood pressure attendant with these iatrogenic therapies.

Abstract: The present invention is directed to a pharmaceutically acceptable taste masking liquid excipient base for administration of a relatively large amount of unpleasant tasting medicines. More particularly, the enhanced sweetness and taste masking effect are produced by the addition of sucralose to the excipient base with maintenance of a pH from about 2 to about 5. The invention is further directed to medicinal compositions comprising such a liquid excipient base and unpleasant tasting medicines. Still further, the invention is directed to a method for taste masking unpleasant tasting medicines through their incorporation into the claimed liquid excipient bases.

Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.

Abstract: A pharmaceutical implant may include a pharmaceutical and at least one excipient, and may be configured to be implanted in a body of a patient. The at least one excipient may dissolve after implantation of the pharmaceutical implant in the body of the patient and release the pharmaceutical. In some examples, the pharmaceutical implant includes at least two pharmaceuticals. The at least one excipient may be selected to provide a desired release profile of the pharmaceutical. For example, the pharmaceutical implant may be configured to dissolve and release the pharmaceutical over a length of time between about one day and about 30 days. In some examples, the pharmaceutical implant may be implanted in the body of the patient proximate to an implantable medical device.

Abstract: A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.

Abstract: The invention provides dosage forms for the delivery of one or more non-steroidal anti-inflammatory drugs to equines. The dosage forms are palatable, desirable, and easy to administer with little or no mess or waste. The dosage form can be a cookie that includes one or more grain products, one or more protein products, one or more flavoring agents, or a combination thereof. The dosage form also includes a therapeutically effective amount of one or more non-steroidal anti-inflammatory drugs, for example, for the treatment of joint deterioration, swelling and inflammation, founder, fever, laminitis, or a combination thereof. The drug can be phenylbutazone or firocoxib and the dosage unit can be conveniently hand-fed to the horse.

Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.

Abstract: A device, a system, or a method is described for treating a disease or condition of one or more joints of articulating bone in a mammalian subject. A device is described which includes one or more substrates configured to contact one or more body contours at one or more joints of articulating bone of a mammalian subject; and an applicator supported by the one or more substrates and configured to inject one or more medicaments to one or more joint tissues of the mammalian subject.

Abstract: A composition suitable for topical application that contains at least two active ingredients, one of these being dapsone and one selected from the group consisting of adapalene, tazarotene and treinion for the effective treatment of acne and other dermatological conditions.

Abstract: A device, a system, or a method is described for treating a disease or a condition of one or more joints of articulating bone in a mammalian subject. The device provides one or more medicaments to one or more joints of the mammalian subject. A device is described that includes one or more substrates configured to contact one or more body contours in proximity to one or more joints of articulating bone of a mammalian subject; one or more sensors configured to monitor movement of the one or more body contours; and one or more applicators supported by the one or more substrates and configured to respond to the movement of the one or more body contours by injecting one or more medicaments to the one or more joint tissues of the mammalian subject.

Abstract: The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: —(CH2)1-4—, (C2-C4)-alkenyl, (C2-C4)alkynyl, —S—(CH2)1-3—#, and —(CH2)1-3—O—#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: —(CH2)2-4—, —S—(CH2)1-3#, and —O—(CH2)1-3—#; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: —OR4. The compounds of formula (I) are useful in the treatment of cancer.

Abstract: The present invention relates to salts of Memantine and COX-INHIBITORs, their crystal form, the processes for preparation of the same and their uses for the treatment of various disorders, including pain.

Abstract: The present invention describes novel methods for using 9-deoxy-2?,9-?-methano-3-oxa-4,5,6-trinor-3,7-(1?,3?-interphenylene)-13,14-dihydro-prostaglandin F1 (also known as Treprostinil) or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of foot ulcers in subjects with diabetic neuropathy. The invention also relates to kits for treatment and/or prevention of foot ulcers, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.

Abstract: An improved excipient comprising substantially homogeneous particles of a compressible, high functionality granular microcrystalline cellulose based excipient is provided. The improved excipient comprises microcrystalline cellulose, a binder and a disintegrant, and is formed by spraying a homogeneous slurry of the components. The excipient provides enhanced flowability/good flow properties, excellent/high compactibility, and increased API loading and blendability as compared to the individual components, and as compared to conventional excipients formed from the same materials. The improved excipient has strong intraparticle bonding bridges between the components, resulting in a unique structural morphology including significant open structures or hollow pores. The presence of these pores provides a surface roughness that is the ideal environment for improved blending with an API.

Abstract: The invention relates to orally disintegrating pharmaceutical compositions comprising rhein or diacerein, or salts or esters or prodrugs thereof, and processes for preparing such compositions.

Abstract: Dermatological disorders having an inflammatory or proliferative component, notably common acne, are treated with topically applicable pharmaceutical compositions containing about 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously formulated into topically applicable gels, preferably aqueous gels, creams, lotions or solutions.

Abstract: Dermatological/cosmetic gel compositions suited for preventing or treating cell differentiation and/or proliferation and/or keratinization disorders, including preventing or treating common acne, comprise (i) at least one retinoid, (ii) dispersed benzoyl peroxide and (iii) at least one pH-independent gelling agent, formulated into (iv) a physiologically acceptable medium therefor.

Abstract: An oral solid dosage form containing nanoparticles is made by (a) reducing the particle size of at least one pharmaceutically active ingredient dispersed in a solution containing fish gelatin to form a nanosuspension and (b) freeze-drying the nanosuspension of step (a) to form the oral solid dosage form.

Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.

Abstract: Compounds that may have anti-inflammatory activity have the general formula (I): Wherein R1, R2, R3 are each independently H or a C1-4 alkyl group or a C2-4 acyl group; R4 and R5 are each independently H or a group of formula —SO3R6, wherein R6 is H or a C1-4 alkyl group or a C2-4 acyl group; with the proviso that at least one of R4 and R5 is a group of formula —SO3R6, or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides a composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt, as well methods of producing such a solid naproxen concentrate.

Abstract: A device is configured to remove a target molecule from a bodily fluid of a subject and to deliver a therapeutic agent to the subject. Such a device may be used for treatment of a disease associated with amyloid beta accumulation in the subject. Agents selected from the group consisting of an ApoE-modulating agent; a RAGE inhibitor; a ?-secretase 1 (BACE1) inhibitor; a ?-secretase inhibitor; a muscarinic receptor subtype 1 (M1) agonists; a growth factor; an enzyme capable of degrading amyloid beta; a mitochondrial antioxidant; insulin; and an inhibitor of tumor necrosis factor (TNF) may be administered directly to the central nervous system of a subject for treatment of a disease associated with amyloid beta accumulation.