Abstract: Provided are pharmaceutical compositions and methods of treating or preventing edema, using an anti-T cell agent, an anti-TGF-?1 agent, or an anti-angiotensin agent, preferably a combination of at least two such agents. The pharmaceutical compositions can be formulated for systemic or local administration, and are preferably administered topically.

Abstract: Provided, in part, are compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with the activity of sodium channels. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.

Abstract: The present invention relates to the use of natural protectants comprising (i) a cetylpyridinium salt (such as cetylpyridinium chloride) or p-anisic acid or a salt thereof (such as sodium p-anisate) and (ii) piroctone olamine to prevent microbial growth in a product, such as a personal care product.

Abstract: The present invention relates to new extended release pharmaceutical compositions and methods of use thereof for the treatment of disorders.

Abstract: The present invention relates to novel processes for the preparation of substituted pyridyl-methylbenzamide derivatives of formula (I), in particular 2,6-dichloro-N-{[3-chloro-5-(trifluoromethyl)-2-pyridyl]methyl}benzamide (Fluopicolide), and for the catalytic hydrogenation of substituted cyanopyridine derivatives, in particular 3-chloro-2-cyano-5-trifluoromethylpyridine [=Py-CN] to the corresponding substituted 2-methylaminopyridine derivatives, in particular 2-aminomethyl-3-chloro-5-trifluoromethylpyridine [=Py-methylamine] or salts thereof in the presence of metal catalysts such as in particular palladium catalysts, catalytic modifiers and acids.

Abstract: Compounds and pharmaceutically acceptable salts thereof that may be used to treat a disease, for example, Duchenne muscular dystrophy, AIDS, and progeria. The compounds and pharmaceutically acceptable salts thereof may be part of a pharmaceutical composition including a pharmaceutically acceptable support.

Abstract: The present invention relates to novel processes for the preparation of substituted pyridyl-methylbenzamide derivatives of formula (I), in particular 2,6-dichloro-N-{[3-chloro-5-(trifluoromethyl)-2-pyridyl]methyl}benzamide (Fluopicolide), and for the catalytic hydrogenation of substituted cyanopyridine derivatives, in particular 3-chloro-2-cyano-5-trifluoromethylpyridine [=Py-CN] to the corresponding substituted 2-methylaminopyridine derivatives, in particular 2-aminomethyl-3-chloro-5-trifluoromethylpyridine [=Py-methylamine] or salts thereof in the presence of metal catalysts such as in particular palladium catalysts, catalytic modifiers and acids.

Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: 4,5-Substituted Picolinamide and picolinonitrile compounds of formula (I), where R4 is CONH2 or CN and R1 is an optionally substituted aryl or heteroaryl, are negative allosteric modulators of the metabotropic glutamate receptor 2 (mGlu2). The compounds and pharmaceutical compositions including the compounds may be useful for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.

Abstract: The present invention relates to a solid concentrate composition comprising: (a) from 5% to 25% by weight of zinc pyrithione (ZPT); (b) from 8% to 85% by weight of at least one surfactant, preferably, wherein the solid concentrate composition has a penetration hardness of between 20 N and 50 N according to the test method as disclosed herein.

Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.

Abstract: The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug contraindicated for concomitant administration with a strong CYP3A4 inhibitor, wherein the patient is treated with multiple doses of posaconazole, stops posaconazole treatment, and then is treated with the CYP3A4 substrate drug. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-21 after stopping posaconazole. In some embodiments, the patient is treated with or prescribed a reduced dose of the CYP3A4 substrate drug for about 2-21 after stopping posaconazole.

Abstract: The present invention relates to novel fungicidal compositions for the treatment of phytopathogenic diseases of useful plants, especially phytopathogenic fungi, and to a method of controlling such phytopathogenic diseases on useful plants. In particular compositions suitable for control of diseases caused by phytopathogens comprise a mixture of a compound of formula (I) with a compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants using such compositions.

Abstract: The present invention relates to solid pharmaceutical dosage forms comprising the drug substance 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea or any pharmaceutically acceptable salt thereof. It further relates to processes of making said solid pharmaceutical dosage forms.

Abstract: The disclosure relates to granulate formulations of pirfenidone and methods of making such formulations.

Abstract: The present invention relates to methods of preventing or treating skin necroptosis diseases, including administering to subjects receptor-interacting protein kinase-3 (RIP3)-mixed lineage kinase domain-like protein (MLKL) pathway blockers or dabrafenib, and method of diagnosing of skin necroptosis diseases, including detecting phosphorylated MLKL. The RIP3-MLKL pathway blockers according to the present invention directly suppress RIP3 overexpressing in skin necroptosis diseases, or inhibit phosphorylation and translocation to plasma membranes of MLKL, subsequently induced therefrom, thereby effectively preventing skin cell death via necroptosis. Thus, the present invention can prevent or treat a variety of skin diseases caused by necroptosis.

Abstract: Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: wherein X is OH, C1-C6 alkoxyl; Y and Z are independently selected from a C1-C6 alkyl, C1-C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

Abstract: The invention provides, in various embodiments, systems, devices and methods relating to ex-vivo organ care. In certain embodiments, the invention relates to maintaining an organ ex-vivo at near-physiologic conditions. The present application describes a method for using lactate measurement in the arterial and the venous blood lines of the Organ Care System Heart perfusion device to evaluate the: 1) The overall perfusion status of an isolated heart and 2) The metabolic status of an isolated heart and 3) the overall vascular patency of an isolated donor heart. This aspect of the present invention uses the property of myocardial cell's unique ability to produce/generate lactate when they are starved for oxygen and metabolize/utilize lactate for energy production when they are well perfused with oxygen.

Abstract: The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.

Abstract: Disclosed is the use of benzotropolone derivatives of formula wherein R1, R2 and R7 independently from each other are hydrogen; C1-C3alkyl; or COR8; R3 is hydrogen; or COOR9 R4 is hydrogen; or C1-C3alkyl; R5 is hydrogen; hydroxy; C1-C3-alkoxy; or —O—(CO)—R10; R6 is hydrogen; C1-C3alkyl; or COR8; or R5 and R6 together may form a five or six membered ring; or R6 and R7 together form a five or six membered ring; and R8, R9, R10 independently of each other are C1-C30alkyl; for protecting body-care and household products from photolytic and oxidative degradation.

Abstract: A combination of: a first tetracycline (TC) component; and a second component capable of releasing nitric oxide (NO) or a nitrate capable of mimicking NO effects in vivo (NO mimetic). The combinations of the invention advantageously act as more effective MMP modulators with selective reductions in circulating MMP-9 levels in-vivo and inhibitory effects on MMP-2 and MMP-9 levels in-vitro. The combinations of the invention also advantageously act as modulators of inflammation mediators. The co-existence of abnormalities of MMP enzymes and inflammation in many diseases make these characteristics advantageous. Therefore, the various combinations of the invention find utility in medical applications where MMPs and/or inflammation is implicated.

Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

Abstract: The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.

Abstract: A solid oral dosage form comprising a core comprising a doxylamine component and a pyridoxine component coated with an enteric coating is disclosed. The solid oral dosage form further comprises two active ingredient-containing coatings surrounding the enteric coating, the active ingredient-containing coatings being separated from one another by an intermediate coating, and one of the two active ingredient-containing coatings comprising a doxylamine component and being free of a pyridoxine component, and the other of the two active ingredient-containing coatings comprising a pyridoxine component and being free of doxylamine component. Uses of the solid oral dosage form for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP), are also disclosed.

Abstract: Provided are compounds, compositions and methods for treating Toll-like receptor 1/2 complex (TLRI/2) related inflammatory disorders. Small molecules, based on the benzotropolone scaffold, capable of influencing downstream signaling are disclosed as well as methods of making and modifying these molecules. Also provided are methods for treating a subject for a clinical condition associated with Toll-like receptor complex 1/2 activation, comprising administering to the subject an effective amount of a benzotropolone compound.

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: A substituted phenol compound represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof. At least one of X and Y is CH, and the other one of X and Y is N or CH. R1 is C1-C4 alkyl or C1-C4 haloalkyl. R2 is C1-C4 alkyl, or halogen. R3 is H, C1-C4 alkyl, aryl, or —(CH2)n-aryl, in which n is 1, 2, or 3. The compound is useful as anticonvulsant.

Abstract: The invention provides methods and compositions for reducing or inhibiting osteolysis, bone resorption, osteoclast differentiation and stimulation and the loosening of medical prostheses by administering a compound or agent that inhibits the biological activity of an axon guidance protein. The compound or agent my inhibit transcription or translation of or bind to an axon guidance protein, such as, for instance, a netrin like netrin-1. Likewise, the compound or agent may inhibit transcription or translation of or bind to a receptor of an axon guidance protein, such as, for instance, a netrin receptor such as unc5b. In some instances, the compound or agent is an agonist of an adenosine A2A receptor. The invention also extends to pharmaceutical compositions comprising such compounds and agents.

Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more carbamate compound(s) selected from Group (A) shows an excellent controlling activity on a pest. Group (A): a group consisting of alanycarb, aldicarb, aldoxycarb, bendiocarb, benfuracarb, carbaryl, carbofuran, carbosulfan, cloethocarb, ethiofencarb, fenobucarb, fenothiocarb, fenoxycarb, furathiocarb, isoprocarb, metolcarb, methomyl, methiocarb, oxamyl, pirimicarb, propoxur, XMC, thiodicarb and xylylcarb.

Abstract: This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma.

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: The present invention relates to a composition, comprising a microorganism of species Penicillium bilaji and at least one compound (II) in a synergistically effective amount.

Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably fipronil, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.

Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Abstract: The present invention is to provide a composition for preventing plant diseases which comprises at least Component I and Component II, is capable of obtaining a synergic effect that cannot be expected with each single component, is capable of markedly increasing a control effect in a much smaller amount of chemicals against various plant pathogens, and causes no phytotoxicity suffering. A composition for preventing plant diseases comprises Components I and II as active ingredients. The Component I is (RS)—N-[2-(1,3-dimethylbutyl)thiophen-3-yl]-1-methyl-3-tri fluoromethyl-1H-pyrazole-4-carboxamide.

Abstract: The subject matter disclosed in this specification pertains to a method for detecting cells with elastic cell membranes. A plurality of cells are fixed to an impedimetric transducer and osmotic stress is applied. Those cells with elastic membranes, including cancer cells, undergo a volume change which is detected by the impedimetric transducer.

Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably fipronil, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.

Abstract: The instant invention relates to a semi-solid topical composition containing Pirfenidone and an antimicrobial/antiseptic agent such as Modified Diallyl Disulfide Oxide (M-DDO) and its preparation process, offering advantages compared to other pharmaceutical forms of topical administration known in the state of the art, useful as antifibrotic, anti-inflammatory and antiseptic agent in the prevention, treatment and reversion of acne and post acne lesions. Said compositions is also useful for reducing skin redness, detaining the formation of new acne outbreaks, reversing already existing outbreaks and regenerating skin damage caused by acne.

Abstract: Pharmaceutical compositions and methods for the treatment of chronic fatigue in human patients comprising a central nervous system (CNS) stimulant in a daily low-dosage amount in combination with therapeutically effective daily amounts of micronutrients, comprising acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha-lipoic acid. The CNS and micronutrient components may be in an oral dosage composition containing a low dosage amount of CNS stimulant such as about 2.5 mg methylphenidate HCl together with about 60-250 mg acetyl L-carnitine, 50-200 mg L-tyrosine, 60-250 mg N-acetyl cysteine, and 25-100 mg alpha-lipoic acid.

Abstract: The invention relates to a composition which contains at least one N-acyl-amino acid surfactant, a betaine surfactant, an N-methyl-N-acylglucamine, said N-methyl-N-acylglucamine having a C16-C20-acyl group, and further contains a solvent and optionally one or more additives. The invention also relates to a method for producing the composition. The invention further relates to the use of the composition for the treatment or care of skin or hair, or for use as a shampoo, face cleaner, liquid cleaner or shower gel.

Abstract: The invention provides a method for preventing discoloration of pyrithione-containing materials, in particular plastic materials or other material such as paints, coatings, adhesives or textiles which are exposed to an outdoor environment. The method is likewise suited for preventing discoloration of other pyrithione-containing materials such as personal care compositions like shampoos. A discoloration inhibitor that includes dehydroacetic acid or a salt thereof is added to the pyrithione-containing material. The discoloration is prevented without the addition of a cyclic organic phosphoric acid ester or an organic phosphite. Use of the discoloration inhibitor does not interfere with the antimicrobial effect of the pyrithione.

Abstract: The invention provides compositions for the prevention and treatment of the symptoms of alcoholic beverage-induced hangover syndrome, related kits and methods of using the compositions and kits.

Abstract: A method for identifying a kidney transplant recipient at an increased risk of developing interstitial fibrosis or tubular atrophy which comprises obtaining a post-transplant urine sample from the kidney transplant recipient; measuring the level of clusterin in the urine sample; comparing the level of clusterin in the patient sample to the level of clusterin in a control sample from the urine of a non-fibrotic kidney transplant recipient; diagnosing a kidney transplant recipient with a clusterin level that is significantly higher than the clusterin level in the control as being at an increased risk of developing interstitial fibrosis or tubular atrophy.

Abstract: The present invention relates to a method for identifying a drug candidate for enhancing expression of p21cip1/waf1 in a human patient suffering from a medical condition that can be treated by enhancing expression of p21C?1/waf1. The method includes (a) providing a cell line comprising a nucleic acid sequence that comprises a p21cip1/waf1 promoter operationally ligated to a reporter domain; (b) exposing the cell line to a compound; and (c) identifying a compound that induces expression of the reporter domain. The compound that induces expression of the reporter domain is a drug candidate for treating a medical condition that can be treated by enhancing expression of p21cip1/waf1.

Abstract: A pesticidal composition comprising 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether; a hydrophobic organic solvent capable of dissolving 0.1-fold by weight of 4-phenoxyphenyl 2-(2-pyridyloxy)propyl ether at 0° C.; polyvinyl alcohol; a nonionic surfactant selected from the group consisting of alkoxylated castor oil, alkoxylated hydrogenated castor oil and alkoxylated hydrogenated castor oil fatty acid ester; and water, is excellent in storage stability.

Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.

Abstract: Disclosed herein are methods of administering deuterated pirfenidone and kits thereof.

Abstract: The present invention provides a method of treatment of Scedosporium spp.

Abstract: The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking.

Abstract: The present invention relates to a suspoemulsion comprising the following ingredients (1), (2), (3), (4), (5), and (6): an ingredient (1): low water-soluble liquid pesticidal ingredient, an ingredient (2): low water-soluble pesticidal active ingredient which is solid at normal temperature, an ingredient (3): polyoxyalkylene block copolymer, an ingredient (4): phosphate ester salt and/or sulfate ester salt of polyoxyethylene aryl phenyl ether, an ingredient (5): ligninsulfonic acid salt, and an ingredient (6): water. The suspoemulsion of the present invention is a formulation having excellent storage stability, which suppresses the particle growth of dispersoids of an ingredient (1) and an ingredient (2) during storage at high temperature and low temperature, and causes neither aggregation nor separation of dispersoids, nor formation of a hard cake, nor a change in appearance.