Abstract: The present invention provides symmetric carbocyanine dyes and dye precursors useful for fluorescence microscopy, and methods of making and using same.

Abstract: A light-emitting element has high luminous efficiency and excellent durability. The light-emitting element includes at least a light-emitting layer between a positive electrode and a negative electrode, and emits light by electrical energy. The light-emitting element is characterized by containing a naphthacene compound that has a specific structure and organic fluorescent substance that has a fluorescence peak wavelength of not less than 500 nm but not more than 690 nm.

Abstract: Indole derivatives of Formula (I+A) having antitumor and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumors.

Abstract: A radioactive isotope-labeled dye compound represented by the following general formula (I): wherein R1 and R2 represent a substituent, R3 to R6 represent a substituted or unsubstituted alkyl group; R7 and R8 represent a substituted or unsubstituted alkyl group; L1 to L3 represent a substituted or unsubstituted methine group; r represents an integer of 0 to 3; P and Q represent 123I, 124I, 125I, 131I or 18F; M represents hydrogen atom, Na, or K; and m and n represent an integer of 0 to 2.

Abstract: This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.

Abstract: A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug.

Abstract: The present disclosure provides compounds that may be used as chromogens, fluorochromes, or as both. Said compounds may further be used as substrate for at least one enzyme, wherein said enzyme is capable of processing an aromatic amine group (—NH2), an aromatic hydroxyl group (—OH), or an aromatic phosphate group (—PO4). Furthermore, the present disclosure also provides methods for precipitating said compounds as well as methods for detecting a target using said compounds. Even further, kits comprising said compounds are disclosed. Said compounds may be used in any method utilizing a fluorochrome, a chromogen, or both.

Abstract: The present invention relates to radiation-curable coating materials comprising new photoinitiators, and to the use thereof.

Abstract: A near-infrared-ray absorbing material which contains a cyanine compound represented by general formula (I), shows a narrow peak of light absorption in the range of wavelengths of 800-1,000 nm, and has excellent light resistance. In formula (I), R1 to R4, Y1, and Y2 each represents a hydrogen atom, a group of formula (II) or (II?), etc., and Anq? represents a q-valent anion, provided that at least R1 is a group of formula (II) or (II') or Anq? is an ion of formula (III); R11 to R13 each represents a hydrogen atom, hydroxy, etc.; and Z1 and Z2 each represents a C1-10 alkyl, etc. In formula (II?), the bond between G? and T? is a double bond or a conjugated double bond; G? represents a carbon atom; T? represents a carbon atom or a nitrogen atom; the ring including G? and T? represents a 6-membered ring, etc.; w? is 0-4; and R01? represents a hydrogen atom, hydroxy, etc. In formula (III), R5 and R6 each represents a C1-8 haloalkyl.

Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.

Abstract: The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.

Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.

Abstract: A new series of HIV-1 fusion inhibitors and methods of use are disclosed. The compounds are based on a substituted indole, benzimidazole, indoline or isoindoline fragment. The compounds find use in inhibiting or preventing HIV fusion from occurring, thus inhibiting or preventing entry of viral RNA into host cells. The compounds may be useful towards other biological targets involving protein-protein interactions.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.

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: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.

Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.

Abstract: A compound having the general formula I or a conjugate thereof, wherein various groups are as defined in the specification. A composition includes: (i) a compound having the general formula I or a conjugate thereof; and (ii) at least one surfactant selected from cationic surfactants and nonionic surfactants. Also disclosed is a preparation method for the composition and a kit comprising the composition. Further disclosed is a method for identifying and differentiating erythroblasts, basophils and lymphocytes simultaneously using the composition according to the present disclosure.

Abstract: Compounds, compositions, and methods for optical, including fluorescence optical, determinations useful in labeling biomolecules such as protein and deoxyribonucleic acid for their detection and quantitation. The compounds are diastereomeric cyanines with high hydrophilicity and other desirable properties.

Abstract: A compound of Formula (1) or a salt thereof, methods for the preparation and use of such a compound, especially as an IAP inhibitor, and related compounds, compositions, and methods.

Abstract: A fluorescent probe comprising a compound represented as (Fluorophore A)-S-(Fluorophore B) (Fluorophore A and Fluorophore B are fluorophores which emit fluorescence when they are irradiated with an excitation light of a wavelength of 600 to 950 nm, Fluorophore A has a property that it shows change of fluorescence characteristic before and after a specific reaction with an substance to be measured, and S represents a spacer which connects Fluorophore A and Fluorophore B), which compound shows substantial change in efficiency of fluorescence resonance energy transfer between Fluorophore A and Fluorophore B before and after the specific reaction with the objective substance, wherein Fluorophore A is represented by the following formula (AI): which uses and shows an excitation light wavelength/fluorescence wavelength in the near infrared region, lights of which region show superior biological tissue permeability, and enables measurement of an substance to be measured by the ratio method.

Abstract: Cyanine-type fluorescent dyes modified with an alkynyl linker arm of formula (I), suitable for the conjugation of biomolecules, such as for example nucleosides, nucleotides, oligonucleotides, nucleic acids, proteins, peptides, vitamins and hormones. A method and intermediates for the synthesis of the alkynyl cyanines of the invention are also described, as well as alkynyl cyanine-biomolecule conjugates and methods for preparing thereof. The alkynyl cyanines can be advantageously used as markers for biomolecules or as quenchers.

Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.

Abstract: A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole2), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.

Abstract: A reagent for measurement of reactive oxygen, which can be used with a light of the near infrared region showing superior biological tissue permeability, wherein (i) a first cyanine compound residue and a second cyanine compound residue are bound to each other, (ii) the first cyanine compound residue has a property that it easily reacts with a reactive oxygen species and is thereby decomposed, and (iii) the second cyanine compound residue either equals or surpasses the first cyanine compound residue in its stability to the reactive oxygen species, and the first cyanine compound residue acts as a quenching group for the second cyanine compound residue.

Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.

Abstract: A fluorescent probe which specifically and efficiently traps nitrogen monoxide, zinc ion etc. to emit fluorescence is provided. A compound represented by the following general formula (I): [wherein R1 and R2 represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 to X4 represent hydrogen atom, an alkyl group, or a protective group for amino group, and m and n represent 0 or 1); R3 and R4 represent hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R5 to R12 represent hydrogen atom, sulfo group, phospho group, a halogen atom, or a C1-6 alkyl group; R13 and R14 represent a C1-18 alkyl group; Z1 represents oxygen atom, sulfur atom, or —N(R15)— (wherein R15 represents hydrogen atom, or a C1-6 alkyl group); Y1 and Y2 represent —C(?O)—, —C(?S)—, or —C(R16)(R17) (wherein R16 and R17 represent a C1-6 alkyl group); and M? represents a counter ion in a number required for neutralizing the charge].

Abstract: The present invention provides compositions and methods for imaging tumor resections.

Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.

Abstract: This invention relates to oligomeric compounds that are prepared by the reaction of a dianhydride with an amino-alcohol to yield an imide-diol intermediate, which is then esterified with a carboxylic acid to form a reactive oligomer.

Abstract: The present invention describes small molecule ligand-drug conjugates and methods of using the small molecule ligand-drug conjugates for targeted treatment of cancer in a patient in need thereof. Further described are methods of sterilizing circulating tumor cells and determining drug concentration in cancer tissue.

Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.

Abstract: Reduced dyes, such as hydrocyanines, deuterocyanines, and/or other deuterated dyes capable of detecting one or more reactive oxygen species are described herein. The reduced dyes exhibit little or no fluorescence due to the disrupted ? conjugation. However, upon reaction with ROS, the reduced dyes are oxidized, regenerating the extended ? conjugation and causing a substantial increase in fluorescence intensity. In many case, the oxidized dye is generally membrane impermeable. However, upon reduction, many of the reduced dyes are membrane permeable. Thus, reduced dyes can accumulate in cells and/or tissue to amplify the signal. Once inside the cell or tissue, the reduced dye is reoxidized upon reaction with ROS, and the oxidized dye again becomes membrane impermeable, trapping the dye within the cell. The reduced dyes can be used to image ROS, such as hydroxide radical and superoxide, in serum, cell cultures, tissue explants, and in vivo.

Abstract: Subject of the present invention are polyether polyol dendron conjugates comprising a specific polyether polyol dendron moiety, at least one certain fluorescent effector molecule (E). Such polyether polyol dendron conjugates may be used for diagnostic and therapeutic purposes, whereby the optical properties of the at least one certain fluorescent effector molecule are enhanced due to the attachment to the polyether polyol dendron conjugate.

Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of use compounds of Formula I in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.

Abstract: The present invention relates to molecular probes of the formula (I) L1-R1-L-A-X??(I) as defined herein that allow for the observation of the catalytic activity of a selected caspase, cathepsin, MMP and carboxypeptidase in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.

Abstract: Embodiments of the present invention are directed to heteroarylamine compounds and organic light-emitting devices including the heteroarylamine compounds. The organic light-emitting devices using the heteroarylamine compounds have high-efficiency, low driving voltages, high luminance and long lifespans.

Abstract: A compound represented by general formula (I) below, or a pharmacologically acceptable salt thereof: wherein X represents sulfonic acid group; R1 and R2 represent substituents; R3 to R6 represent optionally substituted alkyl groups; R7 and R8 represent an optionally substituted alkyl groups; L1 to L3 represent optionally substituted methine groups, with at least one of L1 to L3 being a methine group having a substituent with the bulkiness of an ethyl group or greater; r represents an integer of from 0 to 3, and when r is 2 or more, the plural L2 and the plural L3 may be the same or different, respectively; each of m and n independently represents an integer of 0 to 3; and at least one of the substituents is sulfonic acid group or a group comprising sulfonic acid group, which is useful as an imaging component in a near infrared fluorescence imaging agent.

Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect c-Jun NH2-terminal kinase; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a c-Jun NH2-terminal kinase in a reaction system in which the c-Jun NH2-terminal kinase contacts with a test substance, and the like.

Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris

Abstract: A compound represented by general formula (I) below, or a pharmacologically acceptable salt thereof: wherein X represents sulfonic acid group or phosphoric acid group; R1 and R2 represent substituents; R3 to R6 represent optionally substituted alkyl groups; R7 and R8 represent optionally substituted alkyl groups; L1 to L3 represent optionally substituted methine groups; r represents an integer of from 0 to 3, and when r is 2 or more, the plural L2 and the plural L3 may be the same or different, respectively; each of m and n represent integers of 0 to 3; at least one of the substituents is an acid group selected from sulfonic acid group, carboxylic acid group, and phosphonic acid group or a group comprising the acid group; and two or more of the acid groups and X are selected from carboxylic acid group and phosphonic acid group.

Abstract: Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decreasing the activity of a protein kinase and for treating a protein kinase-related disease, such as cancer, with these compounds.

Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.

Abstract: A color-forming photosensitive composition contains: a cyanine dye having at least two polymerizable groups selected from an acryloyl group, a methacryloyl group and a vinyl group; a radical generator; and a monomer having an ethylenically unsaturated group.

Abstract: The presently disclosed subject matter provides dyes having an improved photostability, biosensors comprising such dyes, and methods of use thereof, including methods for detecting target molecules in a sample under test and for live-cell imaging. The dyes can include a binding member, including a biomolecule or fragments thereof, which can interact with target molecules of interest and can be specific to a given conformational state or covalent modification, e.g., phosphorylation, of the target molecule. The presently disclosed dyes can be used for detecting changes in the binding, conformational change, or posttranslational modification of the target molecule.

Abstract: Cyanine-type fluorescent dyes modified with an alkynyl linker arm of formula (I), suitable for the conjugation of biomolecules, such as for example nucleosides, nucleotides, oligonucleotides, nucleic acids, proteins, peptides, vitamins and hormones. A method and intermediates for the synthesis of the alkynyl cyanines of the invention are also described, as well as alkynyl cyanine-biomolecule conjugates and methods for preparing thereof. The alkynyl cyanines can be advantageously used as markers for biomolecules or as quenchers.

Abstract: A fluorescent probe which specifically and efficiently traps nitrogen monoxide, zinc ion etc. to emit fluorescence is provided. A compound represented by the following general formula (I): [wherein R1 and R2 represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 to X4 represent hydrogen atom, an alkyl group, or a protective group for amino group, and m and n represent 0 or 1); R3 and R4 represent hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R5 to R12 represent hydrogen atom, sulfo group, phospho group, a halogen atom, or a C1-6 alkyl group; R13 and R14 represent a C1-18 alkyl group; Z1 represents oxygen atom, sulfur atom, or —N(R15)— (wherein R15 represents hydrogen atom, or a C1-6 alkyl group); Y1 and Y2 represent —C(?O)—, —C(?S)—, or —C(R16)(R17) (wherein R16 and R17 represent a C1-6 alkyl group); and M? represents a counter ion in a number required for neutralizing the charge].

Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

Abstract: The present invention relates to trifunctional imaging agents that include an antibody for cell targeting, as well as a chelating moiety for sequestering radioisotopes and a fluorescing moiety for imaging. The invention also provides methods using the conjugates for medical diagnostic imaging.