Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.

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

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: The invention provides a near-infrared-absorbing material comprising at least one first compound selected from the group consisting of a singlet oxygen scavenger, a radical trapping agent and an antioxidant and at least one second compound represented by the following formula (II-1) or (II-2).

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.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

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: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.

Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge selected from the group consisting of: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.

Abstract: A method of forming a CBI CC-1065 analog utilizes NH2 as a starting material, where R3 is H or alkyl and R6 is H, substituted or unsubstituted lower alkyl, cyano, or alkoxy. Intermediates (I) are used and are claimed.

Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In general formula (I), ring A is a benzene ring, etc.; R1 is a group of general formula (II), etc.; R2 is a C1-C30 organic group, etc.; Y1 is a C1-C10 alkyl group, etc.; Z1 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; Z2 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq- is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.

Abstract: An object is to provide a novel anthracene derivative. Another object is to provide a light-emitting element with high luminous efficiency. Yet another object is to provide a light-emitting element with a long lifetime. Still another object is to provide a light-emitting device and an electronic device having a long lifetime by using the light-emitting elements of the present invention. The anthracene derivative represented by General Formula (1) is provided. The ability of the anthracene derivative represented by General Formula (1) to exhibit high luminous efficiency allows the production of a light-emitting element with high luminous efficiency and a long lifetime.

Abstract: A method of effecting a one-pot conversion of a tetrahydronaphthalic anhydride to a benzisoindolenine salt is provided. The method comprises heating the tetrahydronaphthalic anhydride with a reagent mixture comprising ammonium nitrate.

Abstract: The present invention provides new intermediate compounds enabling the preparation of N-meso substituted cyanine, merocyanine or oxonole dyes wherein the N-meso substituent comprises electron withdrawing groups and wherein such N-meso substituents are introduced at the intermediate level. These intermediates enable the formation of dyes having in the meso-position N-substituents comprising electron withdrawing groups without the need for further derivatization of the meso-substituent at the dye level.

Abstract: Disclosed are cyanine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which at least one of groups R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 R11, R12, R13 and R14 is -L-M or -L-P, where L is a linking group, M is a target bonding group and P is a conjugated component, and at least one of groups R3, R4, R5, R6, R7, R8, R9 and R19 comprises fluorine. The use of cyanine dyes substituted by fluorine and having additional substitution with three or more sulphonic acid groups for labelling biological target molecules results in a labelled product in which there is reduced dye-dye aggregation and improved photostability, compared with cyanine dyes having no such substitutions.

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: The invention relates to a method for purification of synthetically-produced compounds, comprising a betaine structure in the molecule, for example, indocyan green, characterized in that reaction by-products, starting materials and/or other impurities such as NaI used during production are separated by extraction.

Abstract: The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.

Abstract: A compound represented by Formula (1) below, where n is 2 or 3; a is an integer of 1 to 4 and b is an integer of 3 and 5 to 10, or a is 5 and b is an integer of 1 to 10; R1 to R8 each independently represent a hydrogen atom or a sulfonate that is any one of sodium sulfonate, potassium sulfonate, ammonium sulfonate, triethylammonium sulfonate, pyridinium sulfonate, lysine sulfonate, and arginine sulfonate; and R9 to R12 each independently represent a substituted or unsubstituted C1-C3 alkyl group.

Abstract: Disclosed are cyanine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which at least one of groups R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 R11, R12, R13 and R14 is -L-M or -L-P, where L is a linking group, M is a target bonding group and P is a conjugated component, and at least one of groups R3, R4, R5, R6, R7, R8, R9 and R10 comprises fluorine. The use of cyanine dyes substituted by fluorine and having additional substitution with three or more sulphonic acid groups for labelling biological target molecules results in a labelled product in which there is reduced dye-dye aggregation and improved photostability, compared with cyanine dyes having no such substitutions.

Abstract: Norbornene monomers with fluorene group and polymer material thereof are disclosed. The norbornene monomers with fluorene group are prepared by Diels-Alder reation. The Norbornene monomers containing fluorene groups are highly active for ring-opening-metathesis polymerization (ROMP), and the molecular weight and PDI value of the obtained polymers are controllable.

Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?0)NH(C1-3alkyl), -L-C(?O)N(C1-3alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3alkyl)2, -L-S(?O)2NH(C1-3alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.

Abstract: Compounds of the formula (I), wherein R1, R2 and R10 independently of one another are C1-C20alkyl, phenyl, C1-C12alkylphenyl or phenyl-C1-C6alkyl; R3 and R4 independently of one another are hydrogen, C1-C20alkyl, NR6R7 or SR8, provided that at least one of R3 or R4 is NR6R7 or SR8; R5 is hydrogen or C1-C20alkyl; R6 and R7 independently of one another are C1-C20alkyl, or R6 and R7 together with the N-atom to which they are attached form a 5 or 6 membered ring, which optionally is interrupted by O, S or NR9 and which optionally additionally is substituted by one or more C1-C4alkyl; R8 is phenyl, biphenylyl, naphthyl, anthryl or phenanthryl, all of which optionally are substituted by one or more C1-C4alkyl; and R9 is hydrogen, C1-C20alkyl, C2-C4hydroxyalkyl or phenyl; exhibit an unexpectedly good performance in photopolymerization reactions.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and the 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 derivate compounds having one or more benzo nitrogens.

Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.

Abstract: A method of effecting a one-pot conversion of a tetrahydronaphthalic anhydride of formula (I): to a nitrate salt of a benzisoindolenine of formula (II): The method comprises heating the tetrahydronaphthalic anhydride of formula (I) with a reagent mixture comprising ammonium nitrate so as to effecting concomitant dehydrogenation during the conversion.

Abstract: The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: A novel stilbene derivative is provided with motivation of providing a blue emissive material showing excellent color purity. The use of the stilbene derivative of the present invention allows the fabrication of a blue-emissive light-emitting element with excellent color purity. The invention also includes an electronic device equipped with a display portion in which the stilbene derivative is employed. The stilbene derivative of the present invention is represented by formula (1), in which Ar1 and Ar2 may form a 5-membered ring by being directly bonded to each other. In formula (1), A11 represents any one of substituents represented by general formulas (1-1) to (1-3). The variables shown in formula (1) and (1-1) to (1-3) are as defined in the specification.

Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.

Abstract: The present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.

Abstract: The present invention discloses synthesis of 2,2?-disubstituted 9,9?-spirobifluorene-based triaryldiamine. First, 2,2?-diamino-9,9?-spirobifluorene, a Pd-catalyst as auxiliary and aryl halide BX are provided, wherein X is selected from the group consisting of: Cl, Br and I, B comprises one of the following group: aryl moiety, hetero cycle, multiple fused ring, multiple fused ring with hetero atom(s). Next, a substitution reaction is performed to react the 2,2?-diamino-9,9?-spirobifluorene with the aryl halide BX to produce the 2,2?-disubstituted 9,9?-spirobifluorene-based triaryldiamines. In addition, the present invention discloses organic light emitting devices comprising hole transporting material comprising 2,2?-bis(N,N-disubstituted amino)-9,9?-spirobifluorenes.

Abstract: The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates, and to methods of treatment using them.

Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium.

Abstract: The indolium compounds of the present invention are represented by general formula (I) below and exhibit thermal decomposition behavior further suitable for optical recording materials used in an optical recording layer of an optical recording medium for high-speed recording.

Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared (NIR) spectral range. The NIR is highly sensitive for tumor detection and tracking. The application discloses targeting a tumor-enriched cell surface receptor with a ligand-conjugated fluorescent probe, which specifically allows detection of the tumor relative to the negligible animal autofluorescence.

Abstract: The present disclosure provides contrast photoacoustic probes, and compositions comprising such probes, designed to non-invasively detect and monitor various disease states, or targets within a subject human or animal. The probes are designed to be optically excited in tissue, ultimately generating thermal energy, which is transformed into acoustic energy by the response of the aqueous environment in the subject to the thermal emissions. The acoustic energy (sound) can then be detected by suitably applied transducers and digitally transformed into images indicating the location of the probe in the subject. One aspect of the disclosure encompasses photoacoustic probes that comprise: a carbon nanotube and a plurality of dye molecules bound to the carbon nanotube. The probes may further comprise a targeting moiety for localizing the probe at the site of a specific target.

Abstract: The present invention relates to a trimethine cyanine represented by the formula (1): wherein each symbols are defined in the specification. The present invention also relates to a use of the above dimeric trimethine cyanine compound for as a dye, which is used in optic element, particularly a high density recordable optical media.

Abstract: A novel anthracene derivative represented by General Formula (1) is provided, which enables the production of a light-emitting element with high luminous efficiency and a long lifetime. A high-performance light-emitting device and electronic device in which the anthracene derivative is employed are also disclosed. The anthracene derivative of the present invention is represented by General Formula (1), in which the unit A represents any one of substituents represented by General Formulae (1-1) to (1-3). The variables shown in Formulae (1) and (1-1) to (1-3) are defined in the specification.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor.

Abstract: Novel dyes, precursors to novel dyes, and conjugates of the novel dyes are disclosed, as well as methods of making and using the same.

Abstract: The present invention provides methods for preparing compounds having activity as dopamine autoreceptor agonists and partial agonists at the postsynaptic dopamine D2 receptor. These compounds are useful for treating dopaminergic disorders, such as schizophrenia, schizoaffective disorder, Parkinson's disease, Tourette's syndrome, hyperprolactinemia, and drug addiction.

Abstract: The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

Abstract: The invention relates to a family of cyanine dyes which fluoresce in the far red and near infra red wavelengths of the spectrum and preferably possess lipophilic side chains. The dyes of the invention are soluble in commercially available membrane staining vehicles, are useful as probes for rapidly staining lipophilic structures such as membranes in cells or isolated from cells, and are well retained therein. Methods of using the dyes to detect stained cells both in vivo and in vitro are also disclosed.

Abstract: Disclosed is a cyanine compound represented by general formula (I) below. Also disclosed are an optical filter using the compound and an optical recording material.

Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

Abstract: An electron transport material based on fused aromatic electron-deficient compounds. The accumulation of aromatic rings with an electron deficiency allows free-radical anions to be stabilized very efficiently in these systems.

Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.