Abstract: Provided are manassantin compounds and methods of using the compounds. Provided are methods of treating a disease, the method comprising administering a compound according to Formula I. Further provided are pharmaceutical compositions comprising compounds according to Formula I. Also provided are methods of inhibiting HIF-1 in a cell, the methods comprising administering to the cell a compound according to Formula I.

Abstract: The invention is directed to methods and compositions that can be used in the treatment of headaches. In particular, methods and compositions are described involving the combination of a long-acting NSAID and a 5-HT1B/1D agonist.

Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.

Abstract: The present invention relates to the use of specific compounds related to the indolocarbazole K252a, for the preparation of pharmaceutical compositions for the treatment of various forms of cancer.

Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.

Abstract: 2-cyclopenten-1-one oxime derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof inhibit the production of TNF-? or PDE4, and therefore show therapeutic effect in inflammatory or immunological disorders mediated through TNF-? or PDE4.

Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.

Abstract: Oral dosage forms, and particles used therein, containing salivation inducing agents are disclosed. The salivation agents may be in the core of the dosage form and/or in coatings applied thereto, or alternatively may be within particles and/or the matrix of such dosage forms, in coatings applied to such particles, or on the surface of such coated particles. The particles may be produced into a tablet form, such as a chewable tablet form, that provides for the immediate release of the active ingredient. Other oral dosage forms include thin film strips, gummi, foam tabs, and lozenges.

Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.

Abstract: The present invention refers to the use of a specific indolocarbazole compound of general formula (1) or a pharmaceutically-acceptable a salt thereof for the preparation of a pharmaceutical composition for the prevention or treatment of a neurodegenerative and/or dementing illness driven by the molecular pathology of microtubule-associate tau such as Alzheimer's disease, frontal lobe dementia, Pick's disease, Parkinson disease with dementia, corticobasal degeneration, argyrophilic grains disease, or supranuclear palsy. A method for treating or preventing such illnesses is also disclosed. Furthermore, methods for the identification of efficacious inhibitors of neurofibrillary degeneration, and methods for the determination of an appropriate dosage of an inhibitor of the PHF-type tau hyperphosphorylation for the treatment of a condition characterized by neurofibrillary pathology are described.

Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).

Abstract: The present invention relates to a pharmaceutical composition comprising specific compounds which may be obtained from Leontopodium alpinum Cass. (Edelweiss). A preferred compound is leoligin (=(2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4-dimethoxyphenyl)tetrahydrofuran-3-yl]methyl(2Z)-2-methylbut-2-enoat]). Corresponding means and methods in respect of medical uses of the compounds are described. The present invention also provides a medical device comprising, containing or having been contacted with the compound. The compounds provided herein may particularly be used in the treatment of hyperplastic diseases, in particular intimal hyperplasia, e.g. stenosis, restenosis, atherosclerosis and the like. Also envisaged herein is the use of these compounds in the treatment of proliferative diseases, such as leukemia, prostate cancer and lung cancer.

Abstract: The invention relates to a method of treating with furanone derivatives and the pharmaceutically acceptable salts thereof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treating a number of conditions such as contact dermatitis, skin irritation, rosacea, acne, psoriasis, and preventing and protecting skin tissue against age-related damage or damage resulting from insults such as harmful (UV) radiation or environmental pollution, stress and fatigue.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.

Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: A compound has Formula VIII where, X is —C(O)R, —C(O)OR, —CN, —NO2, —S(O)2R?, —P(O)(OR)2; each R is individually H, alkyl, or alkenyl; R? is alkyl or akenyl; R1 is aryl, alkenyl, arylalkenyl, heterocyclyl, or heteroaryl; and R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are individually H, alkoxy, or hydroxy. In some cases, X is NO2. Pharmaceutical compositions of the compound of Formula VIII with a pharmaceutically acceptable carrier may be prepared. The compounds may be used for inhibition of cyclooxygenase-2.

Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.

Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.

Abstract: There are disclosed skin treatment compositions containing cell signaling compounds, which induce and promote the biosynthesis and/or bioactivity of endogenous chemicals that mediate cell to cell communication in the skin between keratinocytes, fibroblasts and other cell types present in the skin. The cell signaling compound is selected from the group consisting of: andrographolide and its derivatives; adenosine cyclic phosphate and its derivatives; hydrolyzed milk proteins; sunflower seed extract; plankton extract; phytol and its derivatives; and mixtures thereof.

Abstract: Methods of treating chemokine-mediated diseases are disclosed. The methods comprise the administration of CXC-Chemokine receptor antagonists of the formula or pharmaceutically acceptable salts or solvates thereof, in combination with other classes of pharmaceutical compounds. The chemokine-mediated diseases include acute and chronic inflammatory disorders, psoriasis, cystic fibrosis, asthma and cancer. Also disclosed are novel compounds of formula (I).

Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.

Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.

Abstract: The present technology provides a cell based assay for identifying compounds that modulate store-operated ionic calcium levels using itpr mutant cell lines, such as itpr-ku cells, which have abnormal ionic calcium levels.

Abstract: The present invention provides a method of designing a modulator of a myosin, the method comprising molecular modeling of a compound such that the modeled compound interacts with at least three amino acid residues of said myosin, said residues being selected from (a) ranges K265-V268, V411-L441, N588-Q593, D614-T629, and V630-E646 of SEQ ID NO: 2, said myosin comprising or consisting of (i) the sequence of SEQ ID NO: 2; (ii) the sequence encoded by the sequence of SEQ ID NO: 1; (iii) a sequence being at least 40% identical to the sequence of SEQ ID NO: 2 or to the sequence encoded by the sequence of SEQ ID NO: 1; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of SEQ ID NO: 1; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise K265; or (b) ranges of any one of SEQ ID NOs: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 7

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(?O)— or —C(?O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.

Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.

Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.

Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.

Abstract: A range of concentrations exists in which fermentation inhibitors derived from pretreatment of lignocellulosic feed stocks inhibit growth of lactic acid bacteria without affecting fermentive yeast. By optimizing levels of fermentation inhibitors to fall within this range, yeast fermentations of lignocellulosic biomass can be conducted under non-sterile conditions with ethanol yields comparable to those achieved under sterile conditions. Optimised inhibitor levels can be achieved by controlling the water/biomass ratio of a lignocellulosic biomass during and after pretreatment, for example by washing the fiber fraction of a previously pretreated lignocellulosic biomass with a pre-defined amount of fresh water or recycled process solutions. Crude extracts of liquid fraction or process solutions from pretreatment of lignocellulosic biomass can also provide an effective anti-bacterial treatment for first generation starch fermentations.

Abstract: Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-16. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.

Abstract: The present application relates to novel substituted furan derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.

Abstract: The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.

Abstract: Described herein are compounds, compositions, and methods for treating HIV and related diseases.

Abstract: The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.

Abstract: A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective ?, ? unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.

Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.

Abstract: The invention relates to the use of one or several synthetic or natural furan alkyls for cosmetically treating cellulite. Said furan alkyls preferably correspond to formula (I), wherein identical or different R1, R2, R3et R4 are independently of each other a hydrogen atom, a C1-C35alkyl radical, C1-C35 alcenyl radical or a C1-C35 alcynyl radical, preferably C10-C22, wherein said alkyl, alcenyl and alcynyl radicals are substitutable and R1, R2, R3 are preferably a hydrogen atom.

Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radical of formulae (a) to (c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively, into cosmetic compositions.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted alkyl; (iv) tetrazol-5-yl.

Abstract: 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.

Abstract: Disclosed is an agent which has a destructive effect on malignant tumors and contains alpha-ketoglutaric acid, N-acetyl-seleno-L-methionine, N-acetyl-L-methionine, and a compound that is capable of forming azomethine and is selected among the group 5-hydroxymethylfurfural, dehydroascorbic acid, maltol, and vanillin as an active substance, 5-hydroxymethylfurfural being preferred. The inventive agent can be used in the form of an infusion, in an oral or rectal form of administration, or as an irrigation in cancer therapy.

Abstract: The present invention relates to, inter alia, the use of a compound capable of inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) in an animal in the manufacture of a medicament for use in the treatment and/or prevention of depression. The invention also provides for the use of a compound capable of inhibiting HPPD in an animal in the manufacture of a medicament for use in the treatment of the withdrawal symptoms associated with an addictive drug which causes dopamine dependant associative learning disorders in said animal. In a particular embodiment said HPPD inhibitor is selected from the group consisting of the compound depicted as compound 1; 2; and 3.22.

Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.

Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.