Abstract: The present invention generally relates to a process for preparation of 9-halo-3-(2-haloacetyl)-10,11-dihydro-5H-dibenzo[c,g]chromen-8(9H)-one of Formula I, which is an intermediate in the preparation of Hepatitis C Virus (HCV) inhibitors.

Abstract: Compounds including those of the Formula I where X, R1, R2 and subscript t are as defined herein, useful as ?-secretase inhibitors, are provided, as are compositions comprising the compounds, as well as methods for use of the compounds for treating or preventing neurodegenerative diseases, such as, for instance, Alzheimer's disease.

Abstract: A condensed cyclic compound and an organic light-emitting device including the same, the compound being represented by Formula 1, below: Ar1-(L11)b1-(L1)a1-(L12)b2-Ar2.

Abstract: A compound is represented by Formula 1, 2, or 3, and an organic light-emitting device includes the compound. The organic light-emitting device includes a first electrode, a second electrode, and an organic layer. The organic layer includes the compound represented by Formula 1, 2 or 3. A flat display apparatus includes the organic light-emitting device.

Abstract: A condensed cyclic compound of Formula 1 is provided. An organic light-emitting device includes the same.

Abstract: This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed.

Abstract: A novel polyisoprenylated tetracyclic xanthone, named garciesculentone B, isolated from Garcinia esculenta Y. H. Li is disclosed in the present invention. This compound is shown to have significant cytotoxicity against various cancer cells. In addition, garciesculentone B is shown to have antimigration effect on various cancer cells such as human esophageal carcinoma cell. The experimental data supports that this compound is useful for developing into an anticancer drug.

Abstract: Improved processes for the extraction of quassinoids such as quassin and neoquassin from natural substances containing these compounds are described. The process uses compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration. In a first embodiment, the process includes a sonication method using water and no organic solvent. The process is highly efficient and comprises fewer steps than other processes known in the art. In a second embodiment, a method of extracting quassinoids from natural substance comprising bark of a plant of the plant family Simaroubaceae is also disclosed. In a third embodiment, indirect sonication of quassinoids is described using a mixture of polar and non-polar organic solvents.

Abstract: Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

Abstract: Embodiments of near-infrared (NIR) dyes are disclosed, along with methods and kits for detecting analytes with the NIR dyes. The NIR dyes have a structure according to the general structure At least one of R1/R2, R2/R3, R3/R4, R5/R6, R6/R7, and/or R7/R8 together forms a substituted or unsubstituted cycloalkyl or aryl.

Abstract: Methods are provided for forming a xanthone derivative via reacting a 2-substituted benzaldehyde with a phenol derivative to form the xanthone derivative.

Abstract: Disclosed is a method for screening a compound having an activity that selectively modulates an androgen receptor, comprising a step of measuring the mRNA expression level of prostate-specific antigen or the production level of prostate-specific antigen in prostate cancer cells by contacting a test substance with the prostate cancer cells, and a step of measuring the mRNA expression level of uncoupling protein 1 or the production level of uncoupling protein 1 in adipocytes by contacting a test substance with the adipocytes. Additionally disclosed is a selective androgen receptor modulator, comprising as an active ingredient thereof a compound represented by any of structural formulas (I) to (III), and a composition for preventing or treating a lifestyle-related disease, comprising as an active ingredient thereof said selective androgen receptor modulator.

Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.

Abstract: Pharmaceutical or dermo-cosmetic compositions for topical and intravaginal application for treatment of human and veterinary affections caused by anaerobic organisms or parasites are provided comprising quassinoids or plant extracts containing these phytochemicals, in effective amounts. Such compositions can be administered topically or intravaginally to patients in need thereof in various pharmaceutical dosage forms.

Abstract: The present invention relates to photochromic materials that include certain indeno-fused naphthopyrans. The indeno-fused naphthopyrans have an amino group (e.g., a piperidino or morpholino group) bonded to the 6-position and hydrogen or a halo group (e.g., fluoro) bonded to the 11-position thereof. The photochromic materials of the present invention can have a closed-form electromagnetic radiation absorption spectrum that is shifted to longer wavelengths (e.g., wavelengths of greater than 390 nm), relative to comparable photochromic materials. The present invention also relates to optical elements, such as eyeglasses, that include the photochromic materials of the present invention.

Abstract: The invention provides compounds that are A-type procyanidins. The compounds can be prepared by reacting flavylium salts with catechins or analogs thereof, for example, under anhydrous conditions in alcohol.

Abstract: Provided is a pharmaceutical composition for the treatment and/or prevention of disease involving metabolic syndromes, comprising (a) a therapeutically effective amount of a particular compound represented by Formula 1 as defined in the specification, or isomer, prodrug, or solvate or thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.

Abstract: Fluorescent phenyl xanthene dyes are described that comprise any fluorescein, rhodamine or rhodol comprising a particular C9 phenyl ring. One or both of the ortho groups on the lower C9 phenyl ring is ortho substituted with a group selected from alkyl, heteroalkyl, alkoxy, halo, haloalkyl, amino, mercapto, alkylthio, cyano, isocyano, cyanato, mercaptocyanato, nitroso, nitro, azido, sulfeno, sulfinyl, and sulfino. In one embodiment, halo and/or hydroxy groups are used. Optimal dyes contain a lower C9 phenyl ring in which both ortho groups are the same and the lower ring exhibits some form a symmetry relative to an imaginary axis running from the phenyl rings point of attachment to the remainder of the xanthene dye through a point para to the point of attachment. The phenyl xanthene dyes may be activated. Furthermore, the phenyl xanthene dyes may be conjugated to one or more substances including other dyes.

Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.

Abstract: Xanthene compounds are disclosed having fluorescence at multiple wavelengths. Also disclosed are methods for their synthesis and use. Some of the compounds fluoresce at three wavelengths, emitting white light. Uses include the imaging of biological tissues, illumination, and display technologies. Many of the compounds have large Stokes shifts, and are resistant to photobleaching. The fluorescence may be readily distinguished from that of endogenous fluorophores, and from that of most existing, commercially-available fluorescent probes. The compounds are well suited for use in “multiplexing” techniques. They exhibit clear isosbestic and isoemissive points, and have broad absorption and emission ranges.

Abstract: The present invention relates to a composition for treating or preventing hearing loss comprising naphthoquinone-based compounds.

Abstract: The present invention relates to naphthalenetetracarboxylic acid derivates, to a process for their preparation and to their use, especially as an n-type semiconductor.

Abstract: The present invention relates to photochromic materials that include certain indeno-fused naphthopyrans. The indeno-fused naphthopyrans have an amino group (e.g., a piperidino or morpholino group) bonded to the 6-position and an optional halo group (e.g., fluoro) bonded to the 11-position thereof. The photochromic materials of the present invention may have a closed-form electromagnetic radiation absorption spectrum that is shifted to longer wavelengths (e.g., wavelengths of greater than 390 nm), relative to comparable photochromic materials. The present invention also relates to optical elements, such as eyeglasses, that include the photochromic materials of the present invention.

Abstract: The invention provides compounds that are A-type procyanidins. The compounds can be prepared by reacting flavylium salts with catechins or analogs thereof, for example, under anhydrous conditions in alcohol.

Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.

Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Abstract: A new generation of fluorescent ion indicators for measuring cytosolic concentrations of calcium. These new indicators emit in the red portion of the visible spectrum and are ratiometric. The ratiometry consists of shifting in the emission upon binding calcium when exciting with an argon laser at 488 nm. These indicators also show marked increases in red fluorescence when excited with visible light at longer wavelengths. Like all calcium indicators, they comprise the usual chelating portion based on BAPTA (Bis Amino Phenyl Tetraacetic Acid) and a fluorophore portion, either a seminaphthofluorescein/seminaphthorhodamine or dinaphthofluorescein, which enable ratiometry. Unlike other naphthofluoresceins, the pKa has been adjusted on the naphtho moiety to make it suitable for biological calcium measurements. The invention relates to the structures of the indicators and to the method of synthesizing these indicators.

Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.

Abstract: Specific photochromic spirodihydrophenanthropyrans and their use in synthetic resin materials of all kinds, particularly for ophthalmic purposes. The compounds of the invention are photochromic pyran compounds derived from 9,10-dihydrophenanthrene in which at least one of the two carbon atoms at positions 9 and 10 belongs to a further ring system and thus forms a spiro linkage point.

Abstract: The present invention provides zebrafish based methods for the identification of compounds potentially useful in the treatment of motor neuron degenerative diseases (MNDDs), compounds identified by these methods and compositions, methods and medicaments for treating MNDDs.

Abstract: The present invention relates to novel compound of stemphones obtained by culturing microorganism belonging to genus Aspergillus and having ability to produce compound of stemphones selected from the group consisting of stemphone D substance, stemphone E substance, stemphone E1 substance, stemphone E2 substance, stemphone E3 substance and stemphone F substance, accumulating the compound of stemphones in the cultured mass, and isolating the compound of stemphones from the cultured mass. Since the obtained compound has enhancing activity for imipenem and activity for reducing cytotoxicity, it can be expected to be useful as lead compounds for combination remedy for methicillin resistant Staphylococcus aureus (MRSA) infection.

Abstract: The present invention is directed to novel steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.

Abstract: The invention is related to the area of new 6-Oxa-8?-steroid estrogen analogues and the synthesis of these new biological active steroid estrogen analogues, namely, to the preparation of 6-oxa-8?-steroid estrogens and their use as estrogen receptor modulators. These new estrogen analogues are ligands for estrogen receptors and as such may be useful for the treatment and prevention of a variety of conditions related to estrogen functioning. These conditions include bone and cartilage disorders, increased levels of LDL cholesterol, cardiovascular diseases, impairment of cognitive function, cerebral degeneration disorders, endometriosis and other types of inflammation, the metabolic syndrome, and cancer, in particular of the breast, uterus and prostate.

Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Abstract: Disclosed is a method for the screening of a compound having an activity to selectively modulate an androgen receptor. The method comprises the steps of: contacting a substance to be tested with a prostate cancer cell and measuring the level of expression of mRNA for a prostate-specific antigen or the level of production of the prostate-specific antigen in the prostate cancer cell; and contacting the substance with an adipocyte and measuring the level of expression of mRNA for uncoupling protein-1 or the level of production of uncoupling protein-1 in the adipocyte. Also disclosed is a selective androgen receptor modulator comprising a compound represented by any one formula selected from the structural formulae (I) to (III) as an active ingredient. Further disclosed is a composition for preventing or treating lifestyle-related diseases, which comprises the selective androgen receptor modulator.

Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.

Abstract: A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.

Abstract: The present invention relates to methods for the synthesis of morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.

Abstract: Provided is a pharmaceutical composition for the treatment and/or prevention of restenosis including (a) a therapeutically effective amount of a particular compound represented by Formula 1 and 2, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.

Abstract: The present invention is concerned with novel compounds derived from polyquinonic ionic compounds and their use in electrochemical generators.

Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular phenanthrenequinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.

Abstract: The present invention relates to novel stemphones having enhancing effect of ?-lactam antibiotic used as an antibacterial agent, and a process for production thereof. The process is comprised of culturing microorganism belonging to genus Aspergillus and having ability to produce stemphones, the microorganism of which is Aspergillus sp. FKI-2136 NITE BP-83, accumulating the stemphones in the cultured mass, and isolating the stemphones from the cultured mass. Since the obtained stemphones have an action enhancing activity of ?-lactam antibiotic used as an antibacterial agent by combining with ?-lactam antibiotic, the stemphones are expected to be useful as the therapeutic agent for MRSA infection and infectious diseases caused by multi-drug resistant microorganisms including ?-lactam antibiotic resistance.

Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.

Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.

Abstract: Skin lightening additives and skin lightening compositions having an acetylcholinesterase inhibitor are described. The compositions are suitable for topical application and may comprise inhibitors like galanthamine, taspine or both.

Abstract: Provided is a pharmaceutical composition for the treatment and/or prevention of disease involving metabolic syndromes, comprising (a) a therapeutically effective amount of a particular compound represented by Formula 1 as defined in the specification, or isomer, prodrug, or solvate or thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.

Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.