Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunoinflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.

Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.

Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.

Abstract: The invention relates to preparations comprising at least one compound of the formula (I), where the substituents R1 to R4 have a meaning indicated in claim 1, and salts and solvates thereof, and to the use thereof and selected compounds of the formula (I).

Abstract: The invention relates to a pharmaceutical composition for diabetic nephropathy and its preparation, and the application in preparing of medicine for diabetic nephropathy. The pharmaceutical composition is made up of at least one of 7-hydroxycoumarin and 7-hydroxy-6-methoxycoumarin as active ingredient, and the weight percentage of active ingredient is 0.1-99.5%. Moreover, the pharmaceutical composition is mainly used for the prevention and cure of diabetic nephropathy. For the abundant material, remarkable effect on prevention and cure for diabetic nephropathy and convenience for use, it will be a new facultative drug for patients.

Abstract: Methods for assaying ?-L-iduronidase enzymatic activity and methods for screening newborns for Mucopolysaccharidosis Type-I.

Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.

Abstract: Compounds of Formula 5 and prodrug compounds of Formula 5 wherein G1 is H or OH; G2 is H, R?, or CO2R?; G3, G4 and G5, are each independently selected from the group consisting of: H, R?, OH, OR?, F, Cl, Br, I, NH2, NHR?,NR?2, CN, SH, SR?, SO3H, SO3R?, SO2R?, OSO3R?, and NO2; and R? is a one to four carbon alkyl group are provided. Uses of these compounds and methods of medical treatment involving these compounds for the treatment of hepatitis C are also provided.

Abstract: Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided.

Abstract: Novel compounds composition capable of inhibiting TNF? and having anti immunoinflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: There is provided an oligopeptide compound comprising: (a) at least one nitrogen-containing basic group attached to at least one end of the oligopeptide; and (b) two or more heterocyclic monomers, at least one of which is substituted in the heterocyclic part by a branched, cyclic or part cyclic C3-5 alkyl group, or a pharmaceutically acceptable salt or solvate thereof; which compound, salt or solvate binds to the minor groove of DNA.

Abstract: The present invention is directed to novel coumarin derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels

Abstract: Present invention refers to substituted cumarines that are capable to emit fluorescent light when illuminated by wave lengths within ultraviolet range. Present invention also refers to process of production of said substituted cumarines, well as provides compositions containing said substituted cumarines, especially compositions containing said cumarines and volatile solvents and/or adjuvants. Said compositions can be used in objects of great value for its owner, in view of facilitating the identification of such objects.

Abstract: Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.

Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.

Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R5 are selected from the group consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, acetoxy group, phenyl group, naphthyl group, and alkyl group in which a part or all of hydrogen atoms are substituted with fluorine atom; and X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group.

Abstract: This invention provides a method of detecting enzyme activity on a solid medium. The enzyme substrate has a chromogenic portion comprising a catechol residue, in which a derivitising moiety is linked to the aromatic ring of the catechol via a bond, and an enzyme cleavable group which is attached via an ester or ether linkage to the oxygen atom derived from a hydroxyl group of the catechol residue. If the enzyme substrate contacts an enzyme capable of cleaving the enzyme cleavable groups and the cleaved compound contacts a chelatable metal ion, a substantially non-diffusable coloured precipitate is formed.

Abstract: A suppressor of the expression of MCP-1 is provided that is excellent in safety and is widely applicable to, for example, foods. The suppressor of the expression of MCP-1 according to the present invention is characterized by containing auraptene. Auraptene is contained in citrus fruits such as Hassaku, Amanatsu, Natsumikan, and grapefruit. Since these citrus fruits have been eaten for a long time, the present invention has no problem in safety. Furthermore, even when added to, for example, foods, auraptene does not impair the flavor thereof because it is substantially tasteless and odorless. Since auraptene has a low calorific value, for example, an obese person or a diabetic patient can ingest it over a long period of time. Auraptene suppresses the expression of MCP-1 at a genetic level (see FIG. 1) and a protein level.

Abstract: The present invention provides methods and fluorescent compounds that facilitate detecting and labeling of a fusion protein by being capable of selectively binding to an affinity tag. The fluorescent compounds have the general formula A(B)n, wherein A is a fluorophore, B is a binding domain that is a charged chemical moiety, a protein or fragment thereof and n is an integer from 1-6 with the proviso that the protein or fragment thereof not be an antibody or generated from an antibody. The present invention provides specific fluorescent compounds and methods used to detect and label fusion proteins that contain a poly-histidine affinity tag. These compounds have the general formula A(L)m(B)n wherein A is a fluorophore, L is a linker, B is an acetic acid binding domain, m is an integer from 1 to 4 and n is an integer from 1 to 6.

Abstract: There is disclosed a process for performing an isolated Pd(II) mediated oxidation reaction electrochemically. The inventive process is performed on an electrode array device having a plurality of separately addressable electrodes. Preferably, the Pd(II) mediated oxidation is a Wacker reaction.

Abstract: There is described compounds for use in therapy, said compounds being defined by Formula (1): There is also described an anti-proliferative composition comprising one or more compounds according to Formula (1), and a method of treatment of neoplasia comprising the administration of such a compound or composition.

Abstract: A method of detecting platinum group metals in a sample is provided. The method comprises the step of contacting the sample with a fluorophore capable of undergoing allylic ether or allylic ester cleavage. The fluorophore has an oxygen-protected moiety, the protecting group having an allylic functionality. A reducing agent and optionally a solubilizer are also added to the sample. Very low levels of platinum group metals such as palladium and platinum can be detected in a sample.

Abstract: The Indo-Pacific marine sponge Ircinia ramosa has been found to contain two powerful (GI50 0.001 to <0.0001 ?g/ml) murine and human cancer cell growth inhibitors, denominated herein as irciniastatin A and irciniastatin B. Both were isolated (10-3 to 10-4% yields) by cancer cell line bioassay-guided techniques and named irciniastatins A (1) and B (2). Structural elucidation by a combination of spectral analyses, primarily high resolution mass and 2D-NMR (principally APT, HMQC, HMBC and ROESY) revealed unusual structures 1 and 2.

Abstract: A dihydrocoumarin ring-containing compound of the invention is represented by the following formula (1): wherein R represents hydrogen or an alkyl; A1 to A3 each represents 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z3 each represents a single bond, —(CH2)2—, —CH2O—, —OCH2—, —CF2O—, —OCF2—, —CH?CH—, —CF?CF—, —C?C—, —(CH2)4—, —O(CH2)2O—, —(CH2)2CF2O—, —(CH2)2OCF2—, —CF2O(CH2)2—, —OCF2(CH2)2—, —CH?CH—CH2O—, or —OCH2—CH?CH—; X represents hydrogen, fluorine, chlorine, —CN, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, or —OCH2F; G represents oxygen or sulfur; and n and m each represents 0, 1, or 2.

Abstract: Accordingly the present invention describes the anti-inflammatory compound 3-(1,1-dimethyl-allyl)-6-hydroxy-chromen-2-one isolated from the Ruta graveolens L. plant for the inhibition of inos gene thereby reducing nitric oxide level that increases significantly in inflammatory diseases.

Abstract: A class of photo-caged and cell permeable fluorescent molecules having high uncaging cross sections, robust fluorescence enhancement, and flexible chemistry for bioconjugation. Some of the photo-caged fluorescent molecules are derived from 6-chloro-7-hydroxy-coumarin 3-carboxamide. The fluorescent molecules are useful for cellular imaging applications and particularly for tracing the molecular transfer between cellular gap junctions. The fluorescent molecules also have an emission wavelength that spectrally complements with the emission wavelength of other fluorophores, enabling simultaneous multi-color imaging.

Abstract: A compound represented by the general formula (I) below: In the formula, A is as defined in the specification and B denotes where n is an integer of 1 to 4, and a process for producing the above compound includes a reaction between an activated ester and a t-butoxycarbonylaminoethylamine or an ?-amino acid derivative.

Abstract: 4-Substituted coumarin compounds having the general formula of where R is H, CHO, OCH3, X, NO2, an alkyl having C1-10, —OCH2O—, an aryl being mono- or poly-substituted with CN or COOCH3 with the aryl being a phenyl, naphthyl, or azaryl, or a coumarin group that is substituted with R1, R2, R3, R4, with R1, R2, R3, and R4 being H, an alkyl having C1-10, X, NO2, CN, OCH3, COOCH3 or OR5, R5 being H or an alkyl having C1-10, and X being a halogen.

Abstract: A method for treating a disease associated with the estrogen receptor-?, comprising the step of administiering a therapeutically-effective amount of a compound that satifies the equation: Ki?A/Ki?A>25, optionally having general structure (I).

Abstract: Methods and apparatuses for treating fluids to inactivate microorganisms which may be present therein, said fluid containing one or more components selected from the group consisting of protein, blood and blood constituents are provided. The methods comprise adjusting the percentage of plasma in said fluid to a desired value; mixing an inactivation-effective, substantially non-toxic amount of an endogenous photosensitizer or endogenously-based derivative photosensitizer to said fluid; exposing said fluid to photoradiation of sufficient wavelength and energy to activate the photosensitizer, whereby said microorganisms are inactivated.

Abstract: The present invention is directed to a new class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives to their use as androgen antagonists, and to relieve conditions associated with inappropriate activation of the androgen receptor.

Abstract: The present invention is directed to a new class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives to their use as androgen antagonists, and to relieve conditions associated with inappropriate activation of the androgen receptor.

Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunoinflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.

Abstract: A method for enhancing the efficacy of chemotherapy in the treatment of cancer in animals, particularly humans, is provided wherein isocoumarin derivatives that exhibit unique chemopotentiation properties are employed in a combination treatment with chemotherapy.

Abstract: A method of preparing optically active isocoumarin-3-yl-acetic acid derivatives represented by Formula (I): wherein a specific isocoumarin-ketene derivative is subjected to an addition reaction with an optically active alcohol, and then the ester thus obtained is subjected to a hydrolysis reaction. An intermediate for synthesis used therein. A method of preparing isocoumarin-3-yl-acetic acid derivatives represented by Formula (III): wherein a specific isocoumarin derivative is subjected to an addition reaction with carbon monoxide and oxygen in the presence of a transition metal catalyst. An intermediate for synthesis used therein.

Abstract: Novel coumarin derivatives comprising a coumarin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivate crosslinking groups when incorporated into polynucleotides as replacements for one or more of the complementary nucleoside bases present in probes used in procedures involving nucleic acid hybridization reactions.

Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.

Abstract: Disclosed are a color fading/discoloration preventive agent containing as its active ingredient a coumarin analog represented by general formula (1) below, a glycoside of that analog, or a plant extract containing the coumarin analog or its glycoside: (wherein R1 represents a hydrogen atom, a hydroxyl group or a methoxy group, R2 represents a hydrogen atom or a hydroxyl group, and R1 and R2 are not both hydrogen atoms); and a color fading/discoloration preventive agent containing as its active ingredient a coumarin analog mixture obtained from the rind of citrus fruit, and particularly a coumarin analog mixture obtained from citrus cold press oil.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: The present invention relates to a process for preparing substituted coumarins. More particularly, the present invention relates to a process for preparing substituted coumarins using polyaniline salts as catalysts.

Abstract: The new organic electroluminescent display device has a carrier-transporting layer and/or an organic luminous layer composed of a nematic liquid crystal or a liquid crystal dispersing a carrier-transporting low-molecule therein. When the organic luminous layer is to be bestowed with faculty as a liquid crystal, it is made of a nematic liquid crystal. Both the carrier-transporting layer and the organic luminous layer may be bestowed with faculty as a liquid crystal. Since the liquid crystal is incorporated in the carrier-transporting layer and/or the organic luminous layer, the display device can be driven as a liquid crystal display device in a dark place by charging with a voltage lower than a light emission initiating potential. Of course, it is driven as an electroluminescent display device when it is charged with a voltage higher than the light emission initiating potential. Use of an electroluminescent liquid crystal as a organic luminous layer enables omission of a carrier-transporting layer.

Abstract: The present invention relates to compounds and compositions useful in treating or preventing conditions and diseases related to Mycobacterium infection, and methods of use directed thereto.

Abstract: Coumarin derivatives as substrates for cytochrome P450 enzyme.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: This invention relates to determining the three-dimensional structure of the cytosolic domain of phospholamban (PLB) and its active site from NMR data of sufficiently high resolution for the three-dimensional structure determination. The invention also relates to methods for rational drug design enabling the design of phospholamban inhibitors based on using the three-dimensional structure data provided on computer readable media, as analyzed on a computer system having suitable computer algorithms. The invention also relates to phospholamban inhibiting compounds with certain structural, phsicochemical and spatial characteristics that allow for the interaction of said compounds with specific residues of phospholamban.

Abstract: Disclosed are pyran derivatives, which have distinctive sensitivity to visible light and distinctive luminous ability. The derivatives are useful in photopolymerization, electroluminescence, and dye lasers, and are obtainable through a step of reacting a compound having a 4-cyanomethylene-2-methyl-4H-pyran skeleton with a compound having a 3-formylcoumarin skeleton.