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(CH3)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: 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: A novel subphthalocyanine derivative having a phosphorus derivative-substituted group as an axially substituted group which has an excellent solubility, a method for producing the same and an optical film containing the same, are provided without impairing excellent properties peculiar to the original subphthalocyanines. The novel subphthalocyanine derivative is represented by the following chemical formula (1), and it is applicable for optical films.

Abstract: Processes are disclosed for the preparation of a compound having the formula: (I) and intermediate compounds wherein M is a single-photon-emission tomography imageable radiometal and/or a paramagnetic metal, R is hydrogen or a halogen provided that at least one R is halogen and Y is selected from ortho, meta or para O(CH2)nC2HB9H10 or O(CH2)nC2HB10H10 wherein n is 0 or an integer from 1 to 20 and O(CH2)nC2HB9H10 is nido ortho-, meta- or para-carborane and O(CH2)nC2HB10H10 is ortho-, meta- or para-carborane.

Abstract: The present invention provides an economically and industrially superior simple process that enables the selective production of an aromatic heterocyclic monoboron compound and aromatic heterocyclic diboron compound at a satisfactory yield and in a desired ratio by reacting an aromatic heterocyclic compound and a boron compound in a single step under mild conditions while changing only the charged ratios of the raw materials. The present invention provides a production process of a heteroaryl mono- or diboron compound comprising an aromatic heterocyclic compound and a boron compound in the form of bis(pinacolate)diboron or pinacolate diborane in the presence of a iridium-containing catalyst and a ligand such as a bipyridyl ligand.

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: 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: The invention provides compounds that inhibit a viral protease enzyme of the hepatitis C virus (HCV). The compounds are adapted for treatment of a HCV infection in a patient with the disease. The compounds include analogs of tripeptides and tetrapeptides that resemble the viral protease substrate. The invention also provides pharmaceutical compositions and combinations, methods of preparation of the compounds, and methods of treatment of patients afflicted with HCV using the compounds.

Abstract: The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.

Abstract: The present invention provides an economically and industrially superior simple process that enables the selective production of an aromatic heterocyclic monoboron compound and aromatic heterocyclic diboron compound at a satisfactory yield and in a desired ratio by reacting an aromatic heterocyclic compound and a boron compound in a single step under mild conditions while changing only the charged ratios of the raw materials. The present invention provides a production process of a heteroaryl mono- or diboron compound comprising an aromatic heterocyclic compound and a boron compound in the form of bis(pinacolate)diboron or pinacolate diborane in the presence of a iridium-containing catalyst and a ligand such as a bipyridyl ligand.

Abstract: A method of making a metal complex comprises combining a 1-monoacyldipyrromethane with a compound of the formula R1R2MX, wherein M is boron, R1 and R2 are each independently organic substituents; and X is an anion leaving group; to produce a metal complex of the formula DMR1R2 wherein DH is a 1-monoacyldipyrromethane. The methods and complexes are useful for the purification and synthesis of dipyrromethanes and porphyrins.

Abstract: A method of measuring the binding activity of a test compound to a splicing factor 3b (SF3b), which comprises the following steps of: (a) contacting a labeled pladienolide compound and a test compound with a cell or a cell fraction; and (b) measuring the distribution of the bound labeled compound. The method enables to screen for a novel active compound capable of acting on (binding to) a pladienolide target molecule or the like.

Abstract: The present invention relates to novel boronic chalcone derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic chalcone derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.

Abstract: Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer.

Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract: The present invention relates to inhibitors of post-proline cleaving enzyme, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention incorporate a lactam ring in the backbone of the inhibitors. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the target protease.

Abstract: The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV (DPP-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: Disclosed are (i) a boron-dipyrrin compound having thienyl groups, (ii) a preparation method thereof and (iii) a chemosensor comprising the boron-dipyrrin compound having thienyl groups. More particularly, the present invention provides a boron-dipyrrin compound having thienyl group, furyl (OC4H3) group or selyl (SeC4H3) group, which is represented by the following formula (1), a preparation method thereof and a chemosensor comprising the above boron-dipyrrin compound having thienyl groups, characterized in that the chemosensor exhibits variations in colors and fluorescent properties caused by reaction of the boron-dipyrrin compound with metal ions, including, but not limited to, Cu2+ and Hg2+: 3-(R)-4,4-di(R)-8-(R)-4-bora-3a,4a-diaza-s-indacene ??formula (1) wherein R is any one selected from 2-thienyl group and 3-thienyl group.

Abstract: The present disclosure relates, according to some embodiments, to compositions, systems, and methods for preparing and using fluorescent through-bond energy transfer cassettes.

Abstract: A novel fluorescent compound having a high light fastness, high fluorescence quantum yield and sharp absorption spectrum, which emits fluorescence having a wavelength in long wavelength region, as well as its use as a labeling agent, is disclosed. In Formula [I] below, by forming a specific hetero ring(s) with R1 and R2, and/or R6 and R7, shift of the wavelength of the fluorescence to longer wavelength and increase in molar extinction coefficient are attained maintaining the high light fastness, high fluorescence quantum yield and sharp absorption spectrum which the fluorescent dyes having the boron dipyrromethene skeleton have.

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

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)b—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; a —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 invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: The present invention discloses conjugated compounds containing heteroatom-centered arylsilane derivatives and their applications as host materials, electron transport materials, or hole transport materials in an organic electroluminescent device. The general structure of the conjugated compounds containing heteroatom-centered arylsilane derivatives is as follows: where X1, X2, X3, and X4 can be identical or different and X1, X2, X3, and X4 are independently selected from the group consisting of the following: H, B, N, P?O, Si—R9; and R1, R2, R3, R4, R5, R6, R7, R8, and R9 can be identical or different and R1, R2, R3, R4, R5, R6, R7, R8, and R9 are independently selected from aryl group or heterocyclic aryl group containing one or more substituents.

Abstract: The present invention provides methods for preparing complexed diaryl boronic acids from alkyl diarylborinates.

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: The present invention is directed to a new crystalline molecular sieve designated SSZ-82, a method for preparing SSZ-82 using a 1,6-bis(N-cyclohexylpyrrolidinium)hexane dication as a structure directing agent, and uses for SSZ-82.

Abstract: A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.

Abstract: In the context of synthesizing heterocyclic boronic acid compounds, a convergent synthetic methodology is particularly efficient for preparing boropyrrolidines and derivatives of boropyrrolidines.

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 relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.

Abstract: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: A new class of pH sensitive fluorescent dyes and assays relating thereto are described. The dyes and assays are particularly suited for biological applications including phagocytosis and monitoring intracellular processes. The pH sensitive fluorescent dyes of the present invention include compounds of Formula I: wherein the variables are described throughout the application.

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: A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.

Abstract: The proteins in a biological sample that is sought to be analyzed for its protein composition by an electrophoretic or chromatographic procedure are coupled to a dye in an unusually efficient manner by combining the sample with a solid dry composition containing the dye, a buffering agent, and in preferred embodiments, a denaturing agent as well. The solid and dry form of the composition prevents the dye from deteriorating or decomposing, and the combination of components in the composition allows the dye to couple to the proteins in a relatively uniform manner with no overstaining of the protein when the composition and the sample are heated together and held at an elevated temperature for a short period of time.

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: A photoelectric conversion element comprises a first photoelectric conversion part, the first photoelectric conversion part comprising: a pair of electrodes; and a photoelectric conversion film between the pair of electrodes, wherein the photoelectric conversion film comprises an organic photoelectric conversion material having an absorption peak in an infrared region of an absorption spectrum within a combined range of a visible region and the infrared region and generating an electric charge according to light absorbed, and the first photoelectric conversion part as a whole transmits 50% or more of light in the visible region.

Abstract: A method of making a metal complex comprises combining a 1-monoacyldipyrromethane with a compound of the formula R1R2MX, wherein M is boron, R1 and R2 are each independently organic substituents; and X is an anion leaving group; to produce a metal complex of the formula DMR1R2 wherein DH is a 1-monoacyldipyrromethane. The methods and complexes are useful for the purification and synthesis of dipyrromethanes and porphyrins.

Abstract: An optical layer comprises ?-oxo-bridged boron subphthalocyanine dimer. The ?-oxo-bridged boron subphthalocyanine dimer is represented by the following chemical formula (1). (In the chemical formula (1), Z1 to Z12 are the same or different to each other and selected from the groups consisting of a hydrogen atom, a hydroxyl group, a mercapto group, an alkyl group, an aralkyl group, an aryl group, an amino group, an alkoxyl group and a thioether group. Z1 to Z12 have one or more substitutional groups or have no substitutional group.

Abstract: This invention relates to a novel process for obtaining a compound of formula I: wherein the values of R1, R2, and R3 and P are as described in the specification.

Abstract: Novel optically active ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, and m are each as defined in the description, a plurality of the processes for preparing these substances and their use for controlling pests.

Abstract: A salt of formula (I) [HEoR13]+[T1T2]? ??(I) wherein Eo is a nitrogen or phosphorous atom; R1 is hydrocarbon radical; T1 is a Lewis acid that forms a complex with T2, and T2 is a substituted pyrrolyl radical of formula (III) These salts can be used as cocatalyst in a process for the polymerization of alpha-olefins in conjunction with a transition metal organometallic compound.

Abstract: The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.

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: Metal hydride materials react with BZ3 compounds in the presence of ligand to form BH3-L compounds. A compound of the formula HBZ2 is prepared from a compound of the formula BZ3 by reacting a first amount of a compound of the formula HBZ2 with a metal hydride material “MH” and a compound “L” to form a material of the formula BH3-L, and then reacting the BH3-L thus formed with a compound of the formula BZ3 to form HBZ2 in a second amount greater than the first amount of HBZ2. Z is selected from alkoxy, aryloxy, amido, arylamido, doubly substituted alkoxy, doubly substituted aryloxy, doubly substituted amido, doubly substituted arylamido, alkoxy-amido, and aryloxy-arylamido. When Z is bidentate, then HBZ2 has a ring structure. “L” is selected from ethers, aromatic ethers, amines, aromatic amines, heterocyclic nitrogen compounds, sulfides, aromatic sulfides, and heterocyclic sulfur compounds. “L” becomes a ligand in the BH3-L material.

Abstract: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: Process for the preparation of 2-substituted-7-boryl indoles and compounds therefrom. The compounds are intermediates to functionalized indoles, both natural and synthetic which are cytotoxic agents, anticancer and antiviral agents.

Abstract: Process for the preparation of N-protected boryl compounds. The compounds are intermediates to functionalized compounds, both natural and synthetic which are cytotoxic, anticancer and antiviral agents.