Abstract: The present invention relates to compounds of formula I: methods of their use, processes for their preparation and isolated actinomycetes strains capable of preparing pyrrolo[4,3,2-de]quinolin-8-amine compounds.

Abstract: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on.

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.

Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: Disclosed is an organic electroluminescence element comprising an anode, a cathode and a plurality of organic compound layers between the anode and the cathode, provided that one of the organic compound layers is a light emitting layer containing a phosphorescence emitting compound, wherein at least one of the organic compound layers contains a compound represented by Formula (1), wherein, X represents O or S; Y1 to Y3 each represents a hydrogen atom, a substituent or a group represented by Formula (A) disclosed un the specification, provided that at least two of Y1 to Y3 are groups represented by Formula (A), not all of Y1 to Y3 are the same group, and at least one of the groups represented by Formula (A) has Ar of a carbazolyl group, or an azacarbazolyl group containing 2 to 5 nitrogen atoms.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in the variety of therapeutic application, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or neuronal disorder.

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.

Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.

Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.

Abstract: Disclosed is an organic electroluminescence element comprising an anode, a cathode and a plurality of organic compound layers between the anode and the cathode, provided that one of the organic compound layers is a light emitting layer containing a phosphorescence emitting compound, wherein at least one of the organic compound layers contains a compound represented by Formula (1), wherein, X represents O or S; Y1 to Y3 each represents a hydrogen atom, a substituent or a group represented by Formula (A) disclosed in the specification, provided that at least two of Y1 to Y3 are groups represented by Formula (A), not all of Y1 to Y3 are the same group, and at least one of the groups represented by Formula (A) has Ar of a carbazolyl group, or an azacarbazolyl group containing 2 to 5 nitrogen atoms.

Abstract: The present invention is directed at ?-carbolines, preferred 9-alkyl-?-carbolines (9-alkyl-?-BC), their manufacture as well as their use in prophylaxis and treatment of hearing damages, tinnitus, acute acoustic trauma, vertigo and vestibular disorder as well as pharmaceutical compositions containing theses ?-carbolines.

Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Abstract: A material for an organic photoelectric device, the material including a compound including a pyridine ( ) moiety, the compound being a bipolar organic compound including both a hole transporting unit and an electron transporting unit, the compound being represented by the following Formula 1:

Abstract: We have found that exposure of an aqueous tryptophan solution to window sunlight results in the production of multiple tryptophan photoproducts that have the capability of activating the aryl hydrocarbon receptor and increasing the production of AhR target genes and proteins in hepatocytes. We have isolated three of those photoproducts not previously identified as AhR activators, their chemical identification and synthesis and the demonstration that all three have biologic activities as novel AhR activators. Further, one of the three is a completely novel, not previously described, chemical compound.

Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin sub-type receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.

Abstract: The invention relates to compounds which have an affinity for the ? opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.

Abstract: Novel compounds containing substituted oligoazacarbazole chains are provided. These compounds are useful in organic light emitting devices, in particular as hosts in the emissive layer of such devices.

Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

Abstract: The present invention relates to new tetrahydro-?-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically acceptable salts or corresponding solvates. These compounds are suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to 5-HT6 receptors. The invention also relates to two different methods for obtaining the mentioned compounds and to pharmaceutical compositions containing them.

Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.

Abstract: [Problem] An organic compound of excellent characteristics is provided that exhibits excellent hole-injecting/transporting performance with electron blocking ability, and that has high stability in the thin-film state and high luminous efficiency, the organic compound being provided as material for an organic electroluminescent device having high efficiency and high durability. The invention also provides a high-efficient, high-durable organic electroluminescent device using the compound. [Means for Resolution] The compound is of the following general formula having a carbazole ring structure. The organic electroluminescent device includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes, and the compound is used as a constituent material of at least one organic layer.

Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

Abstract: The present invention provides, e.g., compounds having the structure of formula (I): The present invention also provides pharmaceutical compositions that include such compounds, and methods for modulating murine double minute 2 protein (Mdm2) E3 ligase activity, particularly the Mdm2-MdmX hetero-complex E3 ligase activity, using such compounds.

Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract: The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia.

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: A phosphorescent compound is represented by following Formula:

Abstract: Compositions based on hydrogenated pyrido[4,3-b]indoles (variants) of formula (1) or formula (2): are provided, as are methods and kits using those compositions for the treatment of anxiety or mood disorders characterized by stresses, anxiety, neuroses, obsessive fears and their consequences.

Abstract: Disclosed is an organic electroluminescent element which is characterized in that constituent layers including at least a phosphorescent light-emitting layer are provided between a pair of electrodes, and at least one of the constituent layers contains a compound represented by general formula (1). (In the formula, A1, A2 and A3 each represents a substituent; n1 and n2 each represents an integer of 0-3; X1 and X2 each represents an oxygen atom, a sulfur atom, an alkylene group, an imino group, a carbonyl group, a sulfoxide group or a sulfonyl group, or alternatively X2 represents a bonding hand; and Z1, Z2, Z3 and Z4 each represents an optionally substituted aromatic heterocyclic ring or an aromatic hydrocarbon ring, provided that all of the Z1, Z2, Z3 and Z4 are not aromatic hydrocarbon rings at the same time.

Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: substances and the nasal administration thereof, in particular as one of a liquid, as a suspension or solution, or a powder, to the nasal airway of a subject, in particular the posterior region of the nasal airway, and in particular the upper posterior region of the nasal airway, which includes the olfactory bulb, in particular in the treatment of neurological conditions and disorders.

Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders in which orexin pathways are involved, like sleep disorders.

Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

Abstract: The present invention provides a novel diazafluorene compound for manufacturing a 4,5-diazafluorene derivative. The diazafluorene compound is represented by the general formula (1): wherein R1 and R2 each represent a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group, and may be the same or different from each other; and X1 and X2 each represent a halogen atom, and may be the same or different from each other.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).

Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The present invention pertains generally to methods of preparing certain 9-(arylalkyl)-1,2,3,4-tetrahydro-?-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-?-carboline compounds.

Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.

Abstract: The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.

Abstract: Provided is a method for producing a nitrogen-containing condensed heterocyclic compound containing the step of: reacting a compound represented by Formula (1a) or Formula (1b) with a compound represented by Formula (2) under existence of cupper or a cupper ion, and a ligand to produce a nitrogen-containing condensed heterocyclic compound represented by Formula (3a) or Formula (3b):