Abstract: It is intended to provide a benzoxazole derivative or a pharmaceutically acceptable salt or solvate thereof which is useful in the early diagnosis of a conformation disease; a composition or a kit containing the same for diagnosing a conformation disease; a medical composition for treating and/or preventing a conformation disease; and so on.

Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

Abstract: A process for producing a thiazole compound of the formula (3): wherein X1 is a hydrogen atom or a halogen atom, which comprises reacting a compound of the formula (1): wherein X1 is as defined above, and X2 represents a halogen atom, with ammonia and formaldehyde to obtain a hexahydrotriazine compound of the formula (2): wherein X1 is as defined above, and reacting the resulting hexahydrotriazine compound with hydroxylamine under acidic conditions. According to this process, the thiazole compound of the formula (3) can be industrially advantageously produced using inexpensive ammonia with suppressing the formation of a byproduct of the formula (4): wherein X1 is as defined above.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: A compound for an organic thin film transistor having a structure shown by the following formula (1): X1-L-Ar-L-X2??(1) wherein L is —C?C—, or —CH?CH— in a trans configuration, X1 and X2 are independently a substituted or unsubstituted aromatic heterocyclic group having 5 to 60 ring atoms, and their bonding positions to L are in heterocycles, Ar is a substituted or unsubstituted aromatic hydrocarbon group having 6 to 60 ring carbon atoms, or a substituted or unsubstituted aromatic heterocyclic group having 5 to 60 ring atoms, and at least one of X1, X2 and Ar is a bi- or higher-fused ring.

Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.

Abstract: The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.

Abstract: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(?O)—, —C(?O)—C(?O)—, —OC(?O)—, —N(R11)C(?O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or subst

Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: The present invention provides kinase inhibitors of Formula I:

Abstract: A method for producing a compound having a deuterated aromatic ring or heterocyclic ring according to the invention includes heating a compound having an aromatic ring or heterocyclic ring in the presence of heavy water, a transition metal and a metal which generates deuterium. As the metal which generates deuterium, at least one metal selected from the group consisting of aluminum, magnesium, zinc, iron, lead and tin is preferred. As the transition metal, at least one metal selected from the group consisting of platinum, palladium, ruthenium and rhodium is preferred. The heating is preferably carried out by microwave irradiation.

Abstract: The present disclosure relates to a method for inhibiting brassinin oxidase comprising treating a pathogen that is producing BO with an effective amount of selected Paldoxin compounds.

Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.

Abstract: The present invention provides a process for purifying 2-chloro-5-chloromethyl-1,3-thiazole represented by the formula (I): characterized in that a crude 2-chloro-5-chloromethyl-1,3-thiazole represented by the formula (I) is treated with a lower alcohol before the distillation, and then is distilled. The present purification process is a new one for purifying 2-chloro-5-chloromethyl-1,3-thiazole, suitable for industrial practice.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.

Abstract: Provided are a compound represented by the following general formula (1): A1-B1-X1-C1-D1 wherein A1 and D1 each represent an unsubstituted or substituted anthracene ring; B1 and C1 each represent an unsubstituted or substituted thiazole ring; and X1 represents a single bond or a divalent group, and an organic thin film transistor using the compound.

Abstract: The invention relates to a process for the preparation of onium alkylsulfates by reaction of an onium halide with a symmetrically substituted dialkyl sulfate, in which the alkyl group can have 1 to 14 C atoms, with an asymmetrically substituted dialkyl sulfate, in which one alkyl group can have 4 to 20 C atoms and the second alkyl group denotes methyl or ethyl, with an alkyl trialkylsilyl sulfate, with an alkyl acyl sulfate or with an alkyl sulfonyl sulfate, where the reaction with a dialkyl sulfate is carried out at room temperature.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.

Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.

Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.

Abstract: A composite having electro-optic activity including a chromophore compound dispersed in a host material comprising a dendronized chromophore compound, methods for making the composite, and electro-optic devices including the composite.

Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.

Abstract: The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.

Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract: The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

Abstract: Disclosed herein are NPN-type low molecular aromatic ring compounds, organic semiconductor layers formed from such compounds that exhibit improved electrical stability and methods of forming such layers using solution-based processes, for example, spin coating processes performed at or near room temperature. These NPN-type compounds may be used, either singly or in combination, for fabricating organic semiconductor layers in electronic devices. The NPN-type aromatic ring compounds according to example embodiments may be deposited as a solution on a range of substrates to form a coating film that is then subjected to a thermal treatment to form a semiconductor thin film across large substrate surfaces that exhibits reduced leakage currents relative to conventional PNP-type organic semiconductor materials, thus improving the electrical properties of the resulting devices.

Abstract: The present invention provides a novel phenylpropionic acid derivative and a PPAR-? modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-? and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.

Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 20 (GPR20), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR20.

Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.

Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.

Abstract: The invention provides compounds of formula (IA) or (IB) and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120.

Abstract: Compounds of the following structure are described: wherein R1-R6, R10, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.

Abstract: Disclosed is light-driven actuator element characterized in that, inter alia, it can be reduced to micrometer size, is rapidly responsive, and reversibly changes to enable repeated use. The light-driven actuator element includes a crystal of diarylethene compound which changes shape upon photoisomerization (e.g., the compound of Structural Formula (I) below, where R1 represents a hydrogen atom or methyl group and R2 represents a methyl group). The element can be a rod-shaped or plate-like microcrystal having a size on the order of micrometer. The element bends (or contracts) on irradiation with ultraviolet light and expands to return to the original size on irradiation with visible light.

Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Abstract: Compounds of the following structure are described: wherein R1-R6, m, V, W, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and wherein either the bond between the C1 and C2 carbon atoms is a double bond or the bond between the C2 and C3 carbon atoms is a double bond, R2 being absent when the bond between the C1 and C2 carbon atoms is a double bond.

Abstract: The present invention provides a heterocyclic compound of the following general formula (I): wherein X and Y are different from each other and represent a halogen atom selected from among a chlorine atom, bromine atom and iodine atom, or CF3SO3?, CH3SO3?, C6H5SO3? or CH3C6H4SO3?; R1 represents an optionally substituted monovalent aliphatic hydrocarbon group having two or more carbon atoms; one of A1 and A2 represents —S—, —O—, —Se— or Te—, while the other represents —N?, —P? or —Si(R2)?, wherein R2 represents a hydrogen atom, an optionally substituted monovalent hydrocarbon group, a halogen atom, an amino group or a carbonyl group; and one of two linkages each represented by a solid line and a dashed line is a single bond, while the other is a double bond.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.