Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,

Abstract: The present invention discloses methods of application employing B51B6 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: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: A nutritional supplement for increasing cognitive functioning. The supplement includes a flavonoid such as luteolin and a labdane diterpene such as forskolin. The supplement can also include one or any combination of L-phenylalanine, L-carnitine, acetyl-L-carnitine, and vitamin B6. Artichoke extract can be used as a source of luteolin. Methods of using the nutritional supplements to increase cognitive functioning are also included.

Abstract: Embodiments of the present invention relate to a nutritional sleep supplement having a balanced ratio of nutritional elements to facilitate a healthy lifestyle. In one embodiment, a nutritional sleep supplement has a set of active ingredients, the active ingredients comprising: between 50 mg to 600 mg of 5-Hydroxytryptophan; between 125 mg to 1500 mg of calcium lactate; between 50 mg to 600 mg of citric acid; between 125 mg to 1500 mg of gamma-Aminobutyric acid; between 50 mg to 600 mg of L-theanine; between 25 mg to 300 mg of L-tryptophan; between 45 mg to 540 mg of magnesium glycinate; between 1.25 mg to 15 mg of melatonin; between 8.75 mg to 105 mg of niacin; between 7.5 mg to 90 mg of potassium sorbate; and between 10 mg to 100 mg of pyridoxine.

Abstract: The present invention provides methods of alleviating a sign or a symptom of Fragile X Syndrome and relates disorders such as autism spectrum disorders

Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms or sequelae of disease. Chronic and acute conditions may be due to viral infections such as HIV and AIDS, neoplastic diseases stroke, kidney disease, urinary incontinence, autoimmune disorders, Parkinson's disease, prostate hypertrophy, aging, or the treatment of such diseases. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools against acute and chronic conditions in mammalian subjects.

Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

Abstract: The invention relates to liquid compositions which contain a) from 40 to 99.9% by weight of sorbitan monocaprylate and b) from 0.1 to 60% by weight of one or more antimicrobial substances selected from the group consisting of the components b1) to b5): b1) specific organic acids and the salts thereof, b2) specific formaldehyde donors, b3) specific isothiazolinones, b4) specific paraben esters and the salts thereof, and b5) specific pyridones and the salts thereof. The liquid compositions are suitable for the production of cosmetic, dermatological or pharmaceutical products.

Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.

Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: The invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a compound of formula (I) and at least one further respiratory chain complex in inhibitor (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.

Abstract: The invention relates to agents for the control of parasites on animals, comprising an active substance from the group of the phenylpyrazoles and vitamin E or a derivative thereof, such as particularly vitamin E acetate, as well as optionally a further active substance from the group of the pyrethroids and/or optionally additionally further active and/or auxiliary substances. In particular, the invention relates to the use of such agents for the control of ectoparasites such as, in particular, fleas, ticks and sand flies in pets such as, in particular, in dogs, cats and ferrets.

Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract: Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) in a subject are also provided.

Abstract: The present disclosure provides methods for diagnosis of interstitial lung diseases (ILDs). The present disclosure provides methods for differential diagnosis of idiopathic pulmonary fibrosis from other ILDs. Compositions and kits useful in carrying out a subject method are also provided.

Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.

Abstract: Compositions comprising dihydroavenanthramide D and climbazole; and, cosmetics or pharmaceutical end products comprising the compositions, useful for treating skin and/or hair.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

Abstract: The present invention is directed to anti-fungal compositions comprising an anti-fungal agent, an oil and excipients or additives. The compositions of the present invention are devoid of C-11 or greater fatty acids/esters.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.

Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Abstract: A topical insecticide preparation is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The topical insecticide contains a combination of a first pyrethroid insecticide effective for killing fleas, a second pyrethroid insecticide effective for killing ticks, and an insect growth regulator (IGR). The topical insecticide preparation can be packaged together or packaged so that the first and second pyrethroid insecticides are stored separately prior to administration of the insecticide preparation to the animal. The combination of the first and second pyrethroid insecticides with an insect growth regulator results in an insecticide preparation formulated to have enhanced insecticidal activity against fleas and ticks compared to the effectiveness of the first and second insecticides used alone.

Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.

Abstract: The present invention relates to a powder formulation which reduces side effect risk of a medicine having a side effect of drug-induced photodermatosis and increases therapeutic effect, and relates to the method for producing the same. Said powder formulation makes inhalation therapy possible by carrying out aerosolization easily, and since pharmacological effect in lung local part is increased, it is possible to decrease the dose. Skin transmigration of said medicine is controlled by a lung specific delivery technology, and photodermatosis which is a side effect can be controlled.

Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.

Abstract: The invention exploits the elucidation of a connection between the S-adenosylmethionine one-carbon cycle and MAO-B levels and describes drug efficacy testing methods and the use of compounds of the S-adenosylmethionine one-carbon cycle as MAO-B inhibitors in disease prevention and treatment.

Abstract: The present invention relates to a delayed release pharmaceutical composition containing doxylamine succinate and pyridoxine HCl for treatment of nausea and vomiting during pregnancy. More specifically, the present invention concerns a disintegrant-free delayed release pharmaceutical composition for oral administration comprising a core and an enteric coating, wherein said core comprising: a) at least one pharmaceutically active ingredient, and b) at least one pharmaceutically acceptable excipient, wherein said composition provides an in vitro drug release profile of about 80% of active ingredient dissolved within 20 minutes as measured by USP Type II apparatus and also a manufacturing process of said pharmaceutical composition.

Abstract: A synergistic composition, or the use of that composition in the manufacture of a medicament, or a method of treatment including the use of that composition, for the treatment of hair loss and baldness, for combined, sequential or simultaneous administration, in any form, via any biological route. In its optimal embodiment the composition consists, in the form of a lotion: 1600-2400 IU/mL Vitamin A Palmitate, 0.64%-0.96% Thiamine Hydrochloride, 0.64%-0.96% Pyridoxine Hydrochloride, 4.8%-7.2% Niacinamide, 2.85%-5.2% D-Panthenol, 1.6%-2.4% L-Arginine, 3.6%-4.4% Methyl Sulphonyl Methane (MSM), 0.08%-0.12% Ginger Oil, 0.08%-0.12% Cinnamon Oil, 0.0996%-0.1494% Oleoresin Capsicum, 1.3%-1.95% Magnesium, 2.4%-3.6% Zinc, 0.192%-0.288% Manganese, 2.6%-3.9% Urea, 2.4%-3.6% Sodium Glycerophosphate, 4.8%-7.2% L-Lysine HCl, plus Preservatives, Co-solvent (Propylene Glycol), Fragrances, Anti-Oxidant, Cooling agent (Menthol), Emulsifier, and Vehicle (Purified water).

Abstract: A process for improving the health of a subject, the process comprising orally administering a composition comprising hydroxytyrosol to the subject to provide the subject with a daily dose of about 0.1 to about 750 .mu.g hydroxytyrosol per kg of body weight, and a dietary supplement in dosage unit form for oral administration, the dosage unit form comprising a composition containing about 1 microgram to about 50 milligrams hydroxytyrosol or an ester or salt thereof.

Abstract: Methods for reducing the incidence of flea allergy dermatitis (FAD) in a companion animal are disclosed, the methods directed to inhibiting blood feeding by ectoparasites on a companion animal. The methods of the present invention involve administering a pesticide composition comprising cyphenothrin to a companion animal, specifically dogs and cats, in doses and proportions which are parasiticidally effective against a variety of ectoparasites, and in formulations which are convenient for topical application to the animal's skin, preferably localized over a small surface area. Such methods are useful in preventing and/or reducing the incidence of flea allergy dermatitis.

Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

Abstract: A dual release oral dosage system/dosage form comprising an immediate release component/composition and a delayed release component/composition is described. Each of the immediate release component/composition and delayed release component/composition comprises one or more of doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof, and one or more of pyridoxine, a salt thereof, a metabolite thereof and/or a salt of the metabolite. The dual release oral dosage system/dosage form exhibits an improved pharmacokinetic profile relative to the current Diclectin® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting in pregnancy (NVP).

Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.

Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: A hair care composition comprising from about 0.25% to about 80% of a pre-emulsified emulsion comprising from about 0.005% to about 80% of one or more materials selected from the group comprising metathesized unsaturated polyol esters, sucrose polyesters, fatty esters with a molecular weight greater than or equal to 1500 and mixtures thereof and mixtures thereof or, by weight of said hair care composition; wherein an emulsifier is selected from the group consisting of anionic, non-ionic, cationic, amphoteric and mixtures thereof wherein the average particle size of the pre-emulsified oil in water emulsion is from about 20 nanometers to 20 microns; and a cationic surfactant system wherein the composition is stable with respect to one of the following measures selected from emulsion particle size, viscosity or visual phase separation and mixtures thereof.

Abstract: The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-? and anti-TGF-?1 action for the treatment of hepatic fibrosis.

Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.

Abstract: Thyroid hormone antagonists and their nanoparticle formulations (Nanotetrac™ or Nanotriac™) act at a cell surface receptor to block angiogenesis and tumor cell proliferation. The complex anti-angiogenic performs actions on specific cytokines and chemokines. Thyroid hormone antagonists inhibit expression in tumor cells of cytokine genes, e.g., specific interleukins, and chemokine genes, such as fractalkine (CX3CL1), and chemokine receptor genes (CX3CR1) that are targets in the development of inflammation-suppressant drugs. This application discloses a novel composition of Tetra or Tri-iodothyroacetic acid (tetrac or triac), other thyroid partial agonists or antagonists and their nanoparticle formulations conjugated to polymers and encapsulating non-steroidal anti-inflammatory, anti-inflammatory glucocorticoids, and/or polyphenols for the management of various acute and chronic inflammatory disorders ranging from neurological, vascular, and musculoskeletal disorders.

Abstract: Methods and formulations for treating animal ectoparasites, effective against parasites such as fleas and ticks are provided. The methods comprise topically co-administering a non-mobile insect growth regulator and a mobile insect growth regulator to the animal. Parasiticidal formulations for treating animal ectoparasites are also provided, which can be safe to use and avoid the many common deleterious side effects of conventional topical formulations. The topical formulations comprise a combination of two insect growth regulators, a non-mobile insect growth regulator and a mobile insect growth regulator. The topical formulation can be packaged with the two insect growth regulators together or packaged to prevent mixing of the two insect growth regulators prior to administering the topical insecticide formulation to the animal.

Abstract: The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith.

Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an carboxylic acid compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II): and pyribencarb shows an excellent controlling efficacy on plant diseases.

Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.

Abstract: The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.

Abstract: The present invention is directed to a novel use of pyridone derivatives such as pirfenidone for the prevention and treatment of damages to tissues or organs induced by various cytotoxic agents, such as chemotherapeutic agents, biologics, immunosuppressants and radiation. Such prophylactic and/or therapeutic effects of the pyridone derivatives make it possible to increase therapeutic dosages of the cytotoxic agent, thereby enhancing the therapeutic efficacy of the cytotoxic agent and radiation therapy.