Abstract: The present invention relates to a solvent system with improved disintegration degree and dissolution ratio of a hardly soluble drug by highly concentrating the drug through partial ionization, and by establishing optimal conditions for enhancing bioavailability of the drug, such as the co-relation between the acid drug and the accompanied components, ionization degree of a solvent system, use of an appropriate cation acceptor, water content, selection of optimal mixing ratio of the respective components and use of specific surfactants, and to a pharmaceutical preparation comprising the same. The solvent system of the invention has advantages in that it can enhance bioavailability by improving the disintegration degree and dissolution ratio of a hardly soluble drug and also provide a capsule with a sufficiently small volume to permit easy swallowing.

Abstract: A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.

Abstract: The invention relates to the use of derivatives of sulphonic acid (I) or one of the pharmaceutically-acceptable prodrugs or salts thereof in the preparation of a medicament for the treatment of vasoproliferative ocular diseases, said sulphonic acid having formula (I).

Abstract: The present invention provides for compositions and methods for modulating hematopoietic stem cell populations by using HCS modulators, which are agents that either increase HSC numbers or decrease HSC numbers as desired by a particular indication. For example, HSC modulators found to increase HSC numbers include prostaglandin E2 (PGE2) and agents that stimulate the PGE2 pathway. Conversely, HSC modulators that prevent PGE2 synthesis decrease HSC numbers. HCS modulators may be used in vitro, in vivo, or ex vivo.

Abstract: The inventors have found that vitamin K3 and vitamin K5 which may be used in pharmaceuticals and foods or ACNQ, DHNA, or the like which can stimulate the growth of bifidobacteria can inhibit degranulation of basophil-like cells, exhibit a potent degranulation-inhibiting effect, and are useful anti-allergic agents or foods. The present invention provides an anti-allergic agent containing, as an active ingredient, one or more species selected from among 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-dihydroxy-2-naphthoic acid, 1,4-naphthoquinone, 4-amino-2-methyl-1-naphthol, 2-methyl-1,4-naphthoquinone, 2-amino-3-chloro-1,4-naphthoquinone, and a salt thereof.

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: There is provided a stable monohydrate form of treprostinil and pharmaceutical formulation comprising the same, method of making and using the same.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A 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: Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least analgesic and/or at least one anti-inflammatory agent at or near a target site, one can reduce, prevent or treat inflammation and pain.

Abstract: Effective treatments of acute pain and/or inflammation for extended periods of time are provided. Through the administration of an effective amount of sulfasalazine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

Abstract: Effective treatments of pain and/or inflammation for extended periods of time are provided. Through the administration of an effective amount of sulindac or a pharmaceutically acceptable salt thereof at or near a target site, one can relieve pain and/or inflammation caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discongenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days, at least twenty-five days. In some embodiments, the relief can be for at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: The present invention is directed to co-administration of a non-steroidal anti-inflammatory agent (NSAID) and acid blocking agent for the treatment of pain and inflammation with reduced gastrointestinal irritation. A pharmaceutical composition suitable for the co-administration contains a therapeutically effective amount of at least one non-steroidal anti-inflammatory agent, and a therapeutically effective amount of at least one acid blocking agent. A ratio of the non-steroidal anti-inflammatory agent to acid blocking agent in the composition is within a range that provides greater pain relief and reduction of inflammation with less gastrointestinal irritation than that obtainable by the administration of the non-steroidal anti-inflammatory agent or acid blocking agent alone. Examples of pharmaceutical compositions for co-administration of the agents are those containing ibuprofen and ranitidine (“ibudine”), as well as naproxen and ranitidine (“naprodine”).

Abstract: The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, ZP, LP1, LP2 LNP, RP3, RN, and ZNP are defined herein, their preparation, pharmaceutical compositions, and methods of use.

Abstract: The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of SAHA or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of Targretin. The SAHA and Targretin may be administered to comprise therapeutically effective amounts.

Abstract: A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.

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 therefore, advantageously topically applicable gels, creams or lotions.

Abstract: This invention relates to novel compounds that display retinoid like activities, including HB-EGF (Heparin Binding Epidermal Growth Factor) release from keratinocytes, cell proliferation, and epidermal thickening without the irritation potentials, such as release of interleukin 8 and inhibition of terminal differentiation of keratinocytes. This invention also relates to the use of such a compound for both external and non-external applications.

Abstract: Topically applicable, reduced-irritant dermatological/cosmetic compositions useful for the prevention/treatment of a variety of keratinization disorders, for example acne vulgaris, contain at least one naphthoic acid compound and an amount of benzoyl peroxide encapsulated in a polymeric system of porous particles for increasing cutaneous penetration of the at least one naphthoic acid compound, are formulated into topically applicable, physiologically acceptable media therefor.

Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: The invention relates to the use preferably of at least one active ingredient for the prophylaxis or therapy of a viral disease, wherein this active ingredient inhibits at least one component of the cellular signal transduction pathway for the activation of the transcription factor NF-kB such that virus multiplication is inhibited. The present invention relates furthermore to the local, preferably aerogenic, administration of the active ingredient according to the invention for inhibiting virus multiplication. The active ingredient according to the invention may be combined with at least one further antivirally effective substance for the prophylaxis or therapy of a viral disease.

Abstract: A taste-masked liquid composition of docusate includes a docusate salt, povidone, a polyether, and water. Additional ingredients in the composition may include thickeners, sweeteners, flavorants, polyols, preservatives, chelating agents and pH adjusters. Such compositions may be used as taste-masked oral compositions of docusate, and may provide therapeutic effects such as stool-softening.

Abstract: The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof

Abstract: The disclosure provides compounds, compositions, and methods for modulating PPAR? receptor. In one embodiment, the compounds of the disclosure comprise a tri-substituted thiazole group. The substituent at the 2-position of the thiazole group provides steric bulk to the compounds. The compounds, compositions, and methods may be useful, for example, in the treatment of cancer.

Abstract: The present invention discloses methods of application employing B5/B6 vitamins in molecular transport creams or gels to deliver B6 in a high dose to bring about therapeutic ways in human or mammal tissues to reverse a disease process or injury to bring about normal function of the affected tissues. Examples of disease changes to normal include, but are not limited to strokes, cellulitis, facial acne, precancerous lesions, nerve injury like paresthesia, periorbital hematoma, pentathol general anesthesia recovery, headaches, improved sight, hypothyroidism, dental pain, dental gingivitis, insect bites, delayed hypersensitivity states, phlebitis of veins and synergism of steroid activity.

Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.

Abstract: The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of ischemic lesions, such as digital ulcers, in subjects with scleroderma (including systemic sclerosis), Buerger's disease, Raynaud's disease, Raynaud's phenomenon and/or other conditions that cause such lesions. The invention also relates to kits for treatment and/or prevention of ischemic lesions, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.

Abstract: A drug-introduced photo-crosslinked hyaluronic acid derived gel which is a photo-crosslinked hyaluronic acid gel into which a drug is introduced through a covalent bond, and has characteristics that are capable of extruding from an injection device. The drug-introduced photo-cross-linked hyaluronic acid derived gel is capable of extruding, for example, by an injection needle of 20 to 25 gauge with a pressure of 0.5 to 5 kg/cm2.

Abstract: The presently disclosed subject matter provides derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) that are characterized by substantially reduced cyclooxygenase inhibiting activity, yet retain the ability to interact with and modulate the activities of other polypeptides such as the class of peroxisome proliferators-activated receptors (PPARs) and ?-secretase. Also provided are methods of using the derivatives to treat pathological disorders.

Abstract: Certain 2-keto-oxazole compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract: Provided are methods of reducing cell death, attenuating a burst of reactive oxygen species, reducing cytotoxicity, reducing intracellular oxidant stress due species in a population of cells following hypoxia by reoxygenating the cells in the presence of a reversible electron transport chain inhibitor or under hypercarbic conditions. Also provided is a method to determine the effectiveness of a reversible electron transport chain inhibitor for reducing cell death in a population of cells.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Improved methods and compositions for protecting plants or seeds from soil-borne fungal diseases. The composition may include a triterpenoid isolated from Glycyrrhiza glabra and a polymer. The triterpenoid may be Carbenoxolone disodium salt, and the polymer may be a water-insoluble, water-soluble or flowable, seed coating polymer. The methods may comprise the steps of applying the composition to the plant's seeds, roots, tubers and/or foliage, and may also include applying the composition to the soil surround surrounding the plant. The composition may be applied as an aqueous solution or as dry particulates, and may be used for the treatment of soybean plants and seeds.

Abstract: Topically applicable cosmetic/pharmaceutical compositions contain at least one retinoid and at least one anti-irritant compound selected from among is allantoin, divalent strontium salts, divalent zinc salts, monovalent sodium salts and the hydrated derivatives thereof, and are useful for the treatment and/or prevention of a dermatological condition or affliction related to a disorder of keratinization relating to cell differentiation and to cell proliferation, e.g. acne vulgaris.

Abstract: The present invention aims at provision of a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, an agent for the prophylaxis or treatment of diabetes and the like. The compound represented by the formula: wherein each symbol is as defined in the description, a salt thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonistic activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents as agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.

Abstract: Disclosed and claimed herein are e,e,e malonic acid/acetic acid tri-adducts of buckminsterfullerene of the general formula C60R3, wherein each R is independently selected from groups of the formula ?CR1R2 wherein each R1 and R2 is independently selected from the group consisting of —H and —COOH, provided, however, that at least one of the R1's and R2's is a hydrogen. Processes for preparing and uses of the same for treating neuronal injury and for life-extension are also disclosed and claimed herein.

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: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.

Abstract: The present invention relates to a therapeutic agent or prophylactic agent for a disease accompanying an abnormality in an amount of insulin or insulin response, an insulin-mimetic action agent, a food, beverage, or feed, an agent for enhancement of glucose uptake into a cell, and an agent for inducing differentiation into an adipocyte, each comprising as an effective ingredient at least one compound selected from the group consisting of specified compounds having an insulin-mimetic action, derivatives thereof, and pharmacologically acceptable salts thereof.

Abstract: The present invention relates to orally effective ligands of the peripheral cannabinoid receptor CB2, especially (+)-?-pinene derivatives, and to pharmaceutical compositions thereof, which are useful for prevention, alleviation or treatment of autoimmune neurodegenerative disorders, in particular multiple sclerosis and associated symptoms. Methods of the invention are useful when the active ingredient is administered alone or in combination with existing therapeutic modalities. The compositions are administered by oral route.

Abstract: The present invention relates to a composition for the prevention and the treatment of cardiovascular disease containing extracts of T. nucifera or abietane diterpenoid compound or terpenoid compound isolated from the same as an effective ingredient. T. nucifera extracts or abietane diterpenoid compound or terpenoid compound isolated from the same of the present invention not only shows excel lent anti-oxidative activity to LDL but also effectively inhibits ACAT activity. Further, T. nucifera extracts of the present invention reduce blood LDL cholesterol and total cholesterol. Therefore, the composition of the present invention can be effectively used for the prevention and the treatment of cardiovascular diseases including hyperlipidemia and atherosclerosis caused by the LDL oxidation and the synthesis and accumulation of cholesteryl ester.

Abstract: The invention describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDs) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium. A suitably ionised NSAID is one of the two, amongst said three, components that tends to destabilise lipid membranes, the other system component with such activity being typically a surfactant. In contrast, the remaining amongst said at least three amphipatic components typically forms a stable lipid membrane on it's own. An essential characteristics of the resulting, relatively large, aggregates is an improved ability to penetrate pores, in a semi-permeable barrier, at least 30%, and often much smaller than the average diameter of the complex aggregate. This enables said aggregates to mediate NSAID transport through semi-permeable barriers including mammalian skin.

Abstract: [Object] To provide a compound having prostaglandin production-suppressing action and leukotriene production-suppressing action. [Means for Solution] A compound represented by the formula (I): [In the formula, represents a single bond, or a double bond, Link represents a single bond, or a saturated or unsaturated straight hydrocarbon having 1 or 2 carbon atoms, W represents a single bond, oxygen atom, sulfur atom, N(Rw) etc., Rw represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms etc, Rs represents -D-Rx etc., D represents a single bond, oxygen atom, sulfur atom etc., Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms etc., one of V1 and V2 represents Zx, and the other represents AR, Zx represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms etc.

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: Improved treatments of joint diseases, such as, e.g.

Abstract: Methods for treatment of pulmonary hypertension include administration of a first amount of treprostinil and administration of a second amount of a Rho kinase inhibitor such that the first amount and the second amount form together an amount effective for pulmonary hypertension treatment. Kits for treatment pulmonary hypertension are also disclosed.

Abstract: The present invention relates to improved therapeutically active nanocomposite microstructure compositions, including nanoparticle compositions and nanoparticle preparations. Preferred embodiments include nanoparticle compositions comprising nanoparticles of a therapeutically active agent dispersed in a carrier matrix. The invention also relates to a method for preparing said compositions and preparations using solid-state mechanochemical synthesis. Further, it relates to therapeutic products produced using said compositions and to methods of treatment using the compositions.

Abstract: Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.

Abstract: Retinoids with retinoid antagonistic activities, especially Retinoid X Receptor antagonists called RXR antagonists, pharmaceutically acceptable salts and pharmaceutically acceptable esters and amides thereof, have been found to be effective in the treatment of multiple sclerosis, especially by systemic such as oral administration of RXR antagonists.

Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.