Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: The present invention relates to novel compounds which are capable as acting as fluorescent sensors or which are precursors for these and for the use of these for the assay of biological processes such as posttranslational modifications of biological molecules such as phosphorylation, de-phosphorylation, proteolytic cleavage, phosphodiesterase mediated hydrolysis of cyclic nucleotides, methylation, acetylation of proteins peptides, DNA, lipids and the detection of biomolecule interactions (e.g., protein-protein interactions). A small molecule sensor is described which can associate to phosphorylated biological targets via metal ion—phosphate association. The association event can be monitored as fluorescence quench, sensitized emission, fluorescence polarization or a combination thereof.

Abstract: The invention relates to a process for the synthesis of dialkoxyorganoboranes, in particular to a process for the synthesis of dialkoxyorganoboranes by an ester exchange reaction. Moreover, the invention relates to a process for the synthesis of organo-oxazaborolidine catalysts (organo-CBS) and of trialkylboroxins. Furthermore, the invention relates to methods of using dialkoxyorganoboranes for the preparation of organo-CBS catalysts and in Suzuki-type coupling reactions.

Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.

Abstract: The present invention describes novel fluorescent compounds analogous to alkyl phospholipids, containing highly photostable fluorescent groups in the structure thereof and emitting in the visible spectrum wavelength zone. Said compounds are easily introduced to microorganisms, enabling the detection and identification of these organisms by means of fluorescence microscopy. The novel fluorescent compounds can also diagnose, rapidly and easily, the presence of pathogenic microorganisms characterised in that they are resistant to treatment with alkyl phospholipids.

Abstract: The invention relates to oxidized phospholipids having one of the general formulas (I) or (II) wherein A?O, C, NH, or S; B?O, C, NH, or S; and R2 is selected from the group consisting of —CO—(CH2)n—CH3; —CO—(CH2)n—CHO; and —CO—(CH2)n—COOH, with n=3-7, with the proviso that in general formula (I), R1 is selected from the group consisting of —CH2—(CH2)n—X; and —CO—(CH2)n—X with n=5-11, wherein X is a fluorophore; and in general formula (II), R1 is selected from the group consisting of —CH?CH—(CH2)n—CH3 with n=9-15; —(CH2)n—CH3 with n=11-17; and —CO—(CH2)n—CH3 with n=10—16; and R3 is selected from the group consisting of —CO—(CH2)n—X; and —SO2—(CH2)n—X, with n=0-5, wherein X is a fluorophore.

Abstract: The present invention is directed to a method of treatment of a malcondition that can be regulated or normalized via inhibition of DPP-IV. The method involves administration of an effective amount of a pyrrolidine compound of the invention, such as would be present in a pharmaceutical composition of the invention, to mammals, especially humans, to affect a malcondition that can be regulated or normalized via inhibition of DPP-IV.

Abstract: The invention relates to difluoroboradiazaindacene dyes of the formula (1) where R1=fluoro-substituted phenyl residue C6HmFn where n=1 to 5 and m+n=5; or fluoro-substituted naphthyl residue C10HmFn where n=1 to 9 and m+n=9; R2=CH3, C2H5, C3H7, or C4H9; R3=alkyl, aryl, or vinyl aryl; R4, R5=H, F, or an R4 and R5 bridging residue CH?CH—CH?CH; R6, R7=H, F, or an R6 and R7 bridging residue CH?CH—CH?CH; and R8=alkyl or aryl.

Abstract: The invention relates to unsaturated dipyrromethene-boron borocarbons of formula (I) and the use thereof for fluorescence or electroluminescent analysis. The fluorescent properties are provided by the central ring of six atoms comprising the —N—B—N— sequence, R1 to R7 permitting the modification of the compound properties (fluorescence emission wavelength, quantitative fluorescent yield), at least one of the substituents S1 and S2 has a chromophore end group which permits an excitation of the molecule at wavelengths close to those of the substituent chromophore. A preferably selected from the chromophore substituents with a wavelength close to the ultraviolet which significantly increases the Stokes displacement.

Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 independently represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 and X2 represent hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom), provided that R1 and R2 do not simultaneously represent hydrogen atom; R3 and R6 represent an alkyl group; R4 and R7 represent hydrogen atom, an alkyl group, carboxy group, an alkoxycarbonyl group, or sulfo group; and R5 and R8 represents an alkyl group, an aryl group, an alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group], or a salt thereof, which is usable for efficient screening for a chemical substance having applicability as a catalyst of the reaction of Michael addition.

Abstract: This present invention can provide a novel pigment useful in color image displays to form blue pixels capable of providing high-level brightness and saturation, especially a finely-divided pigment which has bright hue and is excellent in pigment physical properties such as light fastness, solvent resistance and heat resistance, and a process for producing the same, a pigment dispersion making use of the pigment, and an ink for a color filters. The novel pigment is produced by forming into a pigment a subphthalocyanine represented by the following formula (1): wherein X is a halogen atom, presents diffraction peaks at diffraction angles (2?) 7.0°, 12.3°, 20.4° and 23.4° in x-ray diffraction, and has an average particle size of 120 to 20 nm.

Abstract: The invention provides a novel compound used as a material for organic light-emitting elements, and an organic light-emitting element which has highly efficient and highly luminescent optical power and is superior in durability. The organic light-emitting element includes an anode and a cathode, and a layer which contains an organic compound and is held between the anode and the cathode.

Abstract: The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

Abstract: The present invention relates to a novel method for preparing atorvastatin. According to the present invention, provided are a novel intermediate of the preparation of atorvastatin and a method of preparing large amounts of atorvastatin in a safe manner using the intermediate.

Abstract: The invention relates to fused bicycloheterocycle substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: Provided herein are compounds or hypochlorous acid probes which can be used as reagents for measuring, detecting and/or screening, directly or indirectly, hypochlorous acid or hypochlorite. Provided also herein are methods that can be used to measure, directly or indirectly, the amount of hypochlorous acid or hypochlorite in chemical samples and biological samples such as cells and tissues in living organisms. Specifically, the methods include the steps of contacting the hypochlorous acid probes disclosed herein with the samples to form one or more fluorescent compounds, and measuring fluorescence properties of the fluorescent compounds. Provided also herein are high-throughput screening fluorescent methods for detecting or screening hypochlorous acid or compounds that can increase or decrease, directly or indirectly, the level of hypochlorous acid or hypochlorite in chemical and biological samples.

Abstract: This invention relates to DPP-IV inhibitory citrate or tartrate salts of pyrrolidinylaminoacetyl pyrrolid acid compounds that are physically and chemically stable, substantially non-deliquescent solids under ambient conditions.

Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.

Abstract: The invention generally relates to novel fluorescent phospholipid compounds, compositions comprising these compounds, and their use in a variety of diagnostic applications, including fluorescence imaging of tumors.

Abstract: The invention relates to novel metal complexes. Said compounds can be used as functional material in a series of different applications which in the broadest sense can be attributed to the electronics industry. The inventive compounds are described by the formula (1) and by compounds (1) to (52).

Abstract: Imaging agents that comprise labeled substrates of the cystine/glutamate antiporter of cells, whereby the methods of use comprise introducing the labeled agents into cells via the cystine/glutamate antiporter, which are then reduced to a labeled cysteine, and subsequently detected in the cell.

Abstract: A light emitting device material containing a pyrromethene compound represented by the general formula (1). It realized a luminescent element having a high luminescent efficiency and excellent color purity. Also provided is a luminescent element employing the materials.

Abstract: The invention relates to novel metal complexes. Said compounds can be used as functional materials in a series of different types of applications that can be attributed in the broadest sense to the electronics industry The inventive compounds are defined by formula (1).

Abstract: The invention is amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate anion wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms, and a cationic counter ion.

Abstract: The invention relates to compositions and methods useful in the labeling and identification of changes in protein levels, changes in enzyme activity, and changes in protein modification. The invention provides for highly soluble optical labeling molecules which are optionally cleavable after separation of mixtures of labeled proteins into components. These optical labeling molecules find utility in a variety of applications, including use in the field of proteomics.

Abstract: Methods for preparing an inhibitor of dipeptidyl peptidase IV, as well as formulations of such inhibitors of dipeptidyl peptidase IV that have a high degree of stability including under warm, humid storage conditions.

Abstract: A phosphoprotein detection reagent that selectively binds phosphoamino acids. Methods of generating and employing the reagent are also provided, as are methods of detecting modulation of protein phosphorylation are disclosed. Methods of detecting a change in state of a cell are also disclosed. Additionally, a kit for the detection of phosphoproteins is also disclosed.

Abstract: Compositions, methods of synthesis and applications of phospholipase A2 (PLA2) specific enzyme substrates which exhibit fluorescence resonance energy transfer (FRET) are described. The compounds generally have the structure: (I) wherein, the variables are described throughout the application. These novel compounds provide a sensitive method to monitor real time PLA2 specific enzyme activities in various cells, tissues and small organisms with fluorescence-ratiometric analysis.

Abstract: The invention provides a crystalline form of a synthetic intermediate useful in the preparation of a DPP-IV inhibitor, a method for preparing the crystalline form of the intermediate, and a method of using the crystalline form of the intermediate in the preparation of the inhibitor.

Abstract: The invention relates to compositions and methods useful in the labeling and identification of proteins. The invention provides for highly soluble zwitterionic dye molecules where the dyes and associated side groups are non-titratable and maintain their net zwitterionic character over a broad pH range, for example, between pH 3 and 12. These dye molecules find utility in a variety of applications, including use in the field of proteomics.

Abstract: The preparation and use of fluorescent cell markers of the structure F—S1-S2-L is described where F is a fluorophore, S1-S2 is a spacer linking F to L, and L is a diacyl lipid.

Abstract: The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

Abstract: Compounds (including polymers) for use in hybrid host materials which can be used in electroluminescent devices. The compounds comprise at least one electron-transporting moiety and at least one hole-transporting moiety which are joined by a flexible linker. Hybrid host materials comprising the compounds exhibit stability against phase separation, elevated glass transition temperature, morphological stability against crystallization, and isolation of the electron transporting moiety and hole transporting moiety ?-systems.

Abstract: The present invention provides a light emitting device material which enables a light emitting device having high efficiency and excellent chromatic purity and durability using a light emitting device material containing a pyrene compound represented by formula (1), wherein any one of R1 to R10 is a group represented by formula (2), or 1 to 4 substituents is/are group(s) represented by formula (3), and a light emitting device using the same.

Abstract: The invention is a system for initiating free radical polymerization comprising: a) in one part, one or more amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms and optionally containing one or more heteroatoms or heteroatom containing functional moieties, and one or more cationic counter ions and b) in a second part, a liberating compound which reacts with the nitrogen atom(s) bound to the boron atom(s) upon contact with the amido-borate to form an organoborane radical.

Abstract: A compound represented by the formula (I) wherein R1 and R2 represent amino groups that substitute at adjacent positions on the benzene ring, wherein one of the amino groups may have one alkyl group; R3 and R4 represent hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group, R9 and R8 independently represent a C1-6 alkyl group, R6 and R9 represent a carboxy-substituted C1-6 alkyl group, an alkoxycarbonyl-substituted C1-6 alkyl group, a sulfo-substituted C1-6 alkyl group, or an alkyl sulfonate-substituted C1-6 alkyl group, and R7 and R10 represent a C1-6 alkyl group, an aryl group, a C1-6 alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group, and an agent for measurement of nitrogen monoxide containing the compound. Said compound can give a fluorescent substance that is free from change in fluorescence intensity in a wide pH range.

Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH2)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.

Abstract: Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: The present invention relates to new compounds of formula I wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

Abstract: Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.

Abstract: To provide a method for producing a wide variety of carbazole derivatives which have a simple and uncomplicated process and in which variations in the yield, purity, etc. of a desired substance which are caused by an aryl group introduced is reduced as much as possible. A method for producing a carbazole derivative represented by General Formula (1) is provided, in which 9-[4-(10-phenyl-9-anthryl)phenyl]-9H-carbazole having an active site at the 3-position of the carbazole skeleton and an aromatic compound having an active site are coupled. In the formula, Ar1 represents an aryl group with 6 to 13 carbon atoms in a ring, and Ar1 may have a substituent.

Abstract: A compound represented by the following general formula (I): wherein R1 represents an amino group which may be substituted with one or two alkyl groups; R2, R3, R4 and R5 independently represent an alkyl group; and R6 and R7 independently represent a monocarboxyalkyl group, a salt thereof, or an ester thereof, which is useful as a pH-sensitive fluorescent probe which emits intense fluorescence in an acidic region.