Abstract: The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.

Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-aminated methylene or 2-esterified methylene tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When X is nitrogen, formula I indicates 2-aminated methylene tanshinone I; when X is oxygen, formula I indicates 2-esterified methylene tanshinone I.

Abstract: Nitrogen-containing biphenyl compounds as represented by formula (I), pharmaceutically acceptable salts or derivatives thereof, pharmaceutical compositions, and preparation methods therefore, and anti-HIV-1 use of the compound. Each substituent group in formula (I) is as defined in the description.

Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells is provided, containing a compound represented by the formula (I): (wherein X, Y, Z, Ar1 , R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, amide, ester, or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.

Abstract: Optionally substituted bipyridine compounds, optionally substituted phenylbipyridine compounds, or optionally substituted bis-phenylbipyridine compounds may be useful in light-emitting devices.

Abstract: Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.

Abstract: The present invention relates to organic compounds, usable as ligands in the preparation of lanthanide complexes or of certain water-soluble transition metals, a method for preparation thereof, and the use of said organic compounds as fluorescent probes.

Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.

Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, which is optionally substituted by 1-2 halogen atoms; selected from fluorine or chlorine; or to a pharmaceutically acceptable acid addition salt in enantiomerically pure form. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: The present invention relates to novel acrylamide compounds of formula (I): wherein A, X, R1, and Y are as defined herein, and their pharmaceutically acceptable salts and process of their preparation. The compounds of formula (I) are useful in the treatment of various disorders that related to Histamine H3 receptors.

Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.

Abstract: Some substituted biaryl ring systems may be useful in light-emitting devices, such as those comprising a light-emitting diode. For example, substituted bipyridinyl or substituted phenylpyridinyl may be useful in these devices. The substituted biaryl ring system may have at least two different substituents, including one on each ring on the biaryl system. The first substituent may include optionally substituted carbazolyl, optionally substituted diphenylamine, optionally substituted diphenylaminophenyl, and optionally substituted carbazolylphenyl. The second substituent may include optionally substituted benzimidazol-2-yl, optionally substituted benzoxazol-2-yl, and an optionally substituted benzothiazol-2-yl.

Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.

Abstract: The present invention relates to compounds of Formula I and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as TrkA antagonists.

Abstract: The present invention provides a thermally activated delayed fluorescence material, a method of synthesizing the same and an OLED device using the same. The thermally activated delayed fluorescence material includes a structure formula 1 as Ar—(Ar1)m-(Ar2)n, wherein the number of m is in 1˜4, the number of n is in 1˜8, the group Ar is an electron withdrawing group, the group Ar1 is an electron donating group and the group Ar2 is an aggregation induced emission group. The thermally activated delayed fluorescence material has a higher glass transition temperature, high thermal stability and excellent luminous efficiency. The method of synthesizing the same has simplified steps, easily purified product, high yield, and luminous and thermal properties of the product can be adjusted by connecting to differentiated functional groups.

Abstract: To provide a new bipolar organic compound. In particular, to provide a bipolar organic compound having excellent heat resistance and to provide a bipolar organic compound which is electrochemically stable. Further, to provide a light emitting element and a light emitting device of which a driving voltage and power consumption are reduced by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have excellent heat resistance by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have a long life by using a new bipolar organic compound.

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract: The present application discloses a stereoselective process for the preparation of ?-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups. In one embodiment, the stereoselective process comprises the preparation of the compound of formula I: the process comprising: a) contacting 1,6-anhydro-?-D-glucopyranose with a compound of formula II, R1R2R3Al, in a solvent to form a first reaction mixture; b) contacting the first reaction mixture of step a) with a second reaction mixture to form a third reaction mixture, wherein the second reaction mixture is prepared by contacting an organoaluminum compound of formula III, R4aR5bAlXc, with a compound of formula IV, ArM; and c) contacting the third reaction mixture with a reagent to form the compound of the formula I.

Abstract: The present invention relates to a novel crystalline form B of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione The invention also relates to a process for the production of this crystalline form and formulations for plant protection which contains the novel crystalline form of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione.

Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.

Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.

Abstract: A method of treating inflammation, by administering an effective amount of a ?2 integrin agonist to a patient, and reducing inflammation. A method of treating cancer, by administering an effective amount of a ?2 integrin agonist to a patient, and reducing tumor growth. A method of treating a patient exposed to radiation, by administering an effective amount of a ?2 integrin agonist to the patient after radiation exposure, and mitigating the effects of radiation exposure in the patient. A method of preventing effects of radiation, by administering an effective amount of a ?2 integrin agonist to the patient prior to radiation exposure, and preventing the effects of radiation exposure on the patient. A method of treating acquired bone marrow failure (BMF), by administering an effective amount of a ?2 integrin agonist to a patient. Methods of improving the health of damaged vasculature in a patient and activating ?2 integrins.

Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,12aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-(1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.

Abstract: Process for the preparation of a benzohetero-[1,3]diazole compound disubstituted with brominated heteroaryl groups which comprises reacting at least one dihalogenated benzohetero[1,3]diazole compound with at least one brominated heteroaryl compound. Said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of compounds useful in the construction of solar concentrators (LSCs—“Luminescent Solar Concentrators”). Furthermore, said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of photoactive polymers useful in the construction of photovoltaic devices (or solar devices) such as, for example, photovoltaic cells (or solar cells), photovoltaic modules (or solar modules), on both rigid or flexible supports.

Abstract: Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: The present invention provides a compound of Formula (I): wherein the variables Z, n, Y and p are as defined herein, and pharmaceutically acceptable salts thereof, which can inhibit the activity of poly (ADP-ribose)polymerases, and pharmaceutical compositions comprising the same.

Abstract: Disclosed are compounds of Formula (Ia), and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3A, R3B, and R4 are as described herein. The compounds may be used as agents in the treatment of diseases, including cancer. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (Ia).

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentifylline and related compounds are beneficial.

Abstract: The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.

Abstract: Provided is a process for the preparation of meropenem trihydrate in high purity and high yield, including using a dry methanol solvate of meropenem, which can remarkably reduce the amount of residual solvents in the resulting product, thereby obtain meropenem trihydrate in high purity.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.

Abstract: The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.

Abstract: The fused heterocyclic compound represented by formula (1) has excellent effectiveness in pest control. In the formula (1), J represents formula J1, J2, J3, J4, J5 or J6; A1; A2; A3; A4; A5; B1; B2; B4; B5; and B6 each represent a nitrogen atom, etc.; B3 represents NR15, etc.; R1 represents a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group X; the pairs R2 and R3 and R5 and R6 are the same or different, and represent a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group X; R4 represents a C1-C6 chain hydrocarbon group, etc., optionally substituted with one or more atoms or groups selected from group W; and n represents 0, 1, or 2.

Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 7-substituted fangchinoline derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.

Abstract: The present invention relates to rotenone derivatives and a use of the same. Particularly, the present inventors identified rotenoisin A and B which are compounds with no toxicity and which are prepared by irradiation with gamma rays onto rotenone as represented by the following formula 1. It was further confirmed that the rotenone derivatives significantly inhibited pancreatic lipase activity and preadipocyte differentiation. The rotenone derivatives of the present invention can be effectively used as a composition for the prevention and treatment of obesity and as a composition for health functional food for the prevention and improvement of obesity: (In formula 1, R1 and R2 are as defined in this description).

Abstract: The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease: wherein A is selected from the group consisting of; of; R1 is H or F; R2 is H, —OCH3, C1-C3 alkyl; R3 is H, —CH3, or —OCH3; and R4 is H or F; or a pharmaceutically acceptable salt thereof.

Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.

Abstract: Embodiments of norbornenylhydrocarbylene dihydrocarbylboranes represented by the Formula (I), and methods of forming such norbornenylhydrocarbylene dihydrocarbylboranes are provided, where m is 0, 1 or 2, A is a C2 to C12 hydrocarbylene group; R1 and R2 are independently selected from a substituted or unsubstituted C1 to C12 hydrocarbyl, substituted or unsubstituted, monocyclic or bicyclic C5 to C7 rings, and R1 and R2, taken together with the boron atom to which they are attached, can form a monocyclic or bicyclic ring; wherein the norbornenylhydrocarbylene dihydrocarbylboranes of Formula (I) are subject to the proviso that 9-norbornenylethyl-9-borabicyclo[3.3.1]nonane is not included.

Abstract: A protected organoboronic acid includes a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sp3 hybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.

Abstract: The present invention is directed to fluorophosphates, and pharmaceutical compositions thereof, which are inhibitors of intestinal apical sodium/phosphate co-transport and are useful in the treatment of hyperphosphatemia, in reducing blood phosphate levels, and in treating hypertension.

Abstract: Compounds of the formulae, (I), wherein each variable is as defined herein are provided which are useful in (i) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable carrier, excipient, and/or diluent; (3) methods for inhibiting or treating prostrate cancer; and (4) methods for blocking or destabilizing neovasculature of a tumor.

Abstract: This invention relates to biology and medicine and, in particular, can be used in medicine to make a pharmaceutical composition for targeted delivery of biologically active substances into mitochondria, driven by proton electro-chemical potential in the mitochondria. This invention also relates to the method to affect an organism by the targeted delivery of biologically active compounds to mitochondria. The invention can be useful in treatment of diseases or disorders associated with not normal functioning of mitochondria, in particular diseases associated with increased production of free radicals and reactive oxygen species.

Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.