Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

Abstract: An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

Abstract: Disclosed are fused heterocyclic compounds of Formula (I) or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

Abstract: Provided is a photopolymerizable composition that is highly sensitive to light having wavelengths of 365 nm and 405 nm, and is capable of forming a curable film that can suppress deterioration in physical properties of the film due to heat-aging. The photopolymerizable composition include: (A) an oxime polymerization initiator which includes a condensed ring formed by containing two or more rings selected from an aromatic ring and a heterocyclic ring, and a cyclic structure which is connected to the condensed ring, the cyclic structure containing a carbonyl group and having an oxime group directly connected to the carbonyl group; and (B) a polymerizable compound.

Abstract: The invention relates to pyrrolo[2,3-a]carbazole derivatives, to a method for preparing the same, and to the use thereof as PIM kinase inhibitors. The invention can particularly be used in the pharmaceutical field.

Abstract: A condensation compound of a fluorinated cyclopentane ring and an aromatic ring, which is useful, for example, for electronic materials, and a process for producing the same are provided. For instance, according to Scheme 1 below, a compound (68) containing a condensed structure formed of a hexafluorocyclopentane ring and an aromatic ring is synthesized. The aromatic ring is not limited to a thiophene ring but can be any ring and any substituent can be used. Thus a compound containing a condensed ring structure formed of a hexafluorocyclopentane ring and an aromatic ring, particularly, for instance, a thiophene ring, which was impossible to produce conventionally, can be produced easily with high yield. The compound of the present invention is particularly suitable to be applied to, for example, electronic materials or semiconductors.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.

Abstract: Compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed: wherein R1-R8, G, N and A? are as defined in the written description.

Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

Abstract: The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.

Abstract: Embodiments of the present invention are directed to a heterocyclic compound and an organic light-emitting device including the heterocyclic compound. The organic light-emitting devices using the heterocyclic compounds have high-efficiency, low driving voltage, high luminance and long lifespan.

Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.

Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).

Abstract: The invention provides a process for production of trans-dibenzoxenopyrrole compounds, in which reduction, leaving group conversion, hydrogenation and methylation are carried out in that order. The process of the invention allows trans-dibenzoxenopyrrole compounds to be produced by a simpler procedure than conventional processes. The invention further provides novel compounds obtained as intermediates in the process, and a process for their production.

Abstract: Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs.

Abstract: The object of the present invention is to provide a potassium channel opener having benzofuroindole skeleton representing the following formula (I) wherein, R1 is hydrogen, R2 is CF3, R3 is COOH, R4 is hydrogen, R5 is hydrogen or chloride and R6 is hydrogen or chloride.

Abstract: The invention provides epoxy and oxetane compositions including the novel acyloxy and N-acyl curing agents described herein. Use of invention curing agents result in cured adhesive compositions with remarkably increased adhesion and reduced hydrophilicity when compared to resins cured with other types of curing agents. Furthermore, the curatives of this invention do not interfere with free-radical cure and are thus suited for use in hybrid cure thermoset compositions.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

Abstract: Compounds of Formulas I-II are described, along with methods of using such compounds for the treatment of cancer and pharmaceutical formulations thereof.

Abstract: Tetracyclic 3-substituted indoles having serotonin receptor affinity and pharmaceutically acceptable salts thereof.

Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: Disclosed are compounds, compositions and methods for the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation. Such compounds are represented by Formula I as follows: wherein R1, R2, a, R3, b, R6, A, Z, and Y are defined herein.

Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.

Abstract: A fused tricyclic compound having aldose reductase inhibitory activity and shown by the following formula, wherein R1 represents 1 to 3 atoms or substituents selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylene, or alkoxy group, and a protected or unprotected hydroxyl or carboxyl group, R2 represents a protected or unprotected carboxyl group, R3 represents 1 or 2 atoms or substituents selected from a hydrogen atom, a halogen atom, an oxo group, a substituted or unsubstituted alkyl or alkoxy group, and a protected or unprotected carboxyl group, A represents an alkylene group, and B represents an oxygen atom, a sulfur atom, or a group shown by the following formula, wherein R4 represents an alkyl or aryl group substituted by an aryl, cycloalkyl, or heterocyclic group, and X represents an oxygen atom or a sulfur atom, provided that, when B represents a group shown by the following formula: wherein R4 represents an alkyl or aryl group substituted wi

Abstract: The present invention relates to methods of inducing expression of an epigenetically silenced gene, RASSF1A, in cells, particularly human cells, such as cancer cells. It also relates to methods of treating an individual, prophylactically or therapeutically, for cancer in which RASSF1A is epigenetically silenced.

Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of 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 a neurodegenerative disease.

Abstract: There is provided an oligopeptide compound comprising: (a) at least one nitrogen-containing basic group attached to at least one end of the oligopeptide; and (b) two or more heterocyclic monomers, at least one of which is substituted in the heterocyclic part by a branched, cyclic or part cyclic C3-5 alkyl group, or a pharmaceutically acceptable salt or solvate thereof; which compound, salt or solvate binds to the minor groove of DNA.

Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I).

Abstract: The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

Abstract: The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided.

Abstract: The present application describes deuterium-enriched asenapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.

Abstract: This invention provides a method of synthesizing enantioenriched merrilactone A and enantiopure merrilactone A, as well as an improved method of synthesizing racemic merrilactone.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.