Abstract: The invention relates to a pharmaceutical composition comprising a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and at least one second agent selected from the group consisting of signal transduction pathway inhibitors, tumour immunotherapeutics, agents inhibiting the BCL2 family of proteins, agents inhibiting Mcl-1, proteasome Inhibitors, poly (ADP-ribose) polymerase (PARP) Inhibitors, aromatase inhibitors, conventional cytotoxic agents or a miscellaneous agent selected from abiraterone, ARN-509 and MYC inhibitors.

Abstract: A polycyclic compound and an organic electroluminescence device including the same. The polycyclic compound according to an example embodiment is represented by the following Formula 1. wherein in Formula 1, Cy1 is carbonyl-containing five- or six-membered and substituted or unsubstituted cyclic hydrocarbon or substituted or unsubstituted heterocycle, and R1 to R4 are each independently a hydrogen atom or a group represented by the following Formula 2 or 3.

Abstract: A bis(benzoxazinyl)phthalimidine has the structure wherein R1, R2, R3, R4, j, and k are defined herein. The bis(benzoxazinyl)phthalimidine is useful as a component of a curable composition. It exhibits a high melting temperature and a high exotherm onset temperature. Also described is a composite that includes a reinforcing filler and the curing product of the bis(benzoxazinyl)phthalimidine.

Abstract: The present invention relates to fluorescent compounds with large Stokes-shift and a process for their preparation. More particularly, the present invention relates to fluorescent compounds that are colorless. The compounds may be used in compositions for inks, paints and plastics, especially in a wide variety of printing systems and are particularly well-suited for security applications.

Abstract: Disclosed are fluorescent compounds with large Stokes-shift and a process for their preparation. More particularly, disclosed are fluorescent compounds that are colorless. The compounds can be used in compositions for inks, paints and plastics, especially in a wide variety of printing systems and are particularly well-suited for security applications.

Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: Polytetrahydrobenzoxazines and bistetrahydrobenzoxazines, obtainable by (A) reacting at least one diamine of the formula H2N-A-NH2 with a C1- to C12-aldehyde and a C1- to C8-alkanol at 20 to 80° C. with elimination and removal of water, (B) reacting the condensation product from (A) with a phenol which bears a long-chain substituent at 30 to 120° C., and optionally (C) heating the reaction product from (B) to 125 to 280° C. The resulting polytetrahydrobenzoxazines and bistetrahydrobenzoxazines are suitable as fuel or lubricant additives, especially as detergent additives for diesel fuels.

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.

Abstract: An organic light-emitting device comprises an anode, a cathode and a light-emitting layer between the anode and the cathode. The light-emitting layer comprises a compound of formula (I): wherein Ar1, Ar2, Ar3, Ar6 and Ar7 in each occurrence independently represent an unsubstituted or substituted aryl or heteroaryl group; X independently in each occurrence represents S or O; R independently in each occurrence represents H or a substituent; p is 0 or 1; q is 0 or 1; f is 1, 2 or 3; g is 1, 2 or 3; and adjacent groups Ar3 or adjacent groups Ar2 may be linked by a divalent group to form a ring. This compound can provide a bluer emitter that can be blended into current host formulations (deep blue, CIEy<0.08) suitable for solution processing.

Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: The present invention provides benzoxazine containing propargyl group as formula (I): wherein and The present invention provides a method of preparing a compound of formula (I). The present invention also provides a flame resistant resin.

Abstract: The present invention relates to a benzoxazine intermediate and a preparation method thereof. The structural formula of the benzoxazine intermediate is shown by formula (1), R1 in formula represents o, C?O, S, SO2, alicyclic hydrocarbon with 3 to 30 carbon atoms and derivatives thereof, aliphatic hydrocarbon with 1 to 20 carbon atoms and derivatives thereof, or unsaturated aliphatic hydrocarbon with 2 to 20 carbon atoms and derivatives thereof; R2 is alicyclic hydrocarbon with 3 to 20 carbon atoms and derivatives thereof, aliphatic hydrocarbon with 1 to 20 carbon atoms and derivatives thereof, or unsaturated aliphatic hydrocarbon with 2 to 20 carbon atoms and derivatives thereof. The benzoxazine intermediate of the present invention contains a naphthalene ring structure segment, has desirable heat resistance performance and flame retarding performance, and can be widely applied in composite materials.

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob

Abstract: The use of tetrahydrobenzoxazines I where R1 is a hydrocarbyl radical and R2, R3, R4 and R5 are each independently hydrogen atoms, hydroxyl groups or hydrocarbyl radicals, and where R2 to R5 may also form a second and a third tetrahydrooxazine ring, with the proviso that at least one of the substituents has from 4 to 3000 carbon atoms and the remaining substituents, when they are hydrocarbyl radicals, each have from 1 to 20 carbon atoms, as stabilizers for stabilizing inanimate organic material, especially turbine fuels, against the action of light, oxygen and heat.

Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.

Abstract: The compounds represented fey the following general formula is is thermally stable and has excellent characteristics as a charge transport material [Ar1 represents a single bond, a benzene ring, etc.; X1 represents a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; either one of L1 and L2, and L3 and L4 bond to each other to represent a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; the other of L1 and L2, and L3 and L4 represent a hydrogen atom or a substituent; Y1 represents a linking group that links via a nitrogen atom, a boron atom or a phosphorus atom; R1, R2, R5 to R7 and R10 to R12 represent a hydrogen atom or a substituent; and n1 indicates an integer of 2 or more.].

Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.

Abstract: Disclosed is a method for making a low-k, flame-retardant, bi-functional benzoxazine. The method includes the steps of dissolving phosphoric diamine with various functional groups, phenolic adamantane and paraformaldehyde in a solvent at 72° C. to 88° C. for 7 to 9 hours, and cooling and introducing the solution in n-hexane to separate the low-k, flame-retardant, phosphoric, bi-functional benzoxazine.

Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I) and (II): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Abstract: A curable polymer composition containing: (A) a thermoset benzoxazine resin precursor component; (B) optionally, an arylsulphone-containing benzoxazine component, and (C) a polyarylsulphone thermoplastic toughening agent, wherein in the absence of component (B), component (C) contains one or more benzoxazine pendant-and/or end-groups.

Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

Abstract: A monomer having the general formula: in which R1 is any substitution; R2 is any substitution; R1 and R2 may be linked to form a saturated or unsaturated ring; L represents a reactive leaving group; X and Y each independently represent CR2, O, BR, NR, SiR2, S, S?O, SO2, PR or P?O(R) wherein R in each occurrence is independently selected from H or a substituent; Z represents a single bond or a divalent atom or group, wherein X—Z—Y forms an unconjugated ring or chain, with the proviso that at least one of R1 and R2 is an aryl or heteroaryl group if Z is a single bond.

Abstract: Disclosed are fluorescent compounds with large Stokes-shift and a process for their preparation. More particularly, disclosed are fluorescent compounds that are colourless. The compounds can be used in compositions for inks, paints and plastics, especially in a wide variety of printing systems and are particularly well-suited for security applications.

Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract: Provided is an excellent organic light emitting element having high emission efficiency and a low drive voltage. The organic light emitting element includes an anode, a cathode, and an organic compound layer disposed between the anode and the cathode, in which the organic compound layer includes a quinolino[3,2,1-kl]phenoxazine compound represented by the following general formula [1]: where R1 to R4 each represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R1 to R4 may be identical to or different from each other, and Ar represents a single bond or an oligophenylene group having 6 to 18 carbon atoms.

Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.

Abstract: Disclosed is a method for making a low-k, flame-retardant, bi-functional benzoxazine. The method includes the steps of dissolving phosphoric diamine with various functional groups, phenolic adamantane and paraformaldehyde in a solvent at 72° C. to 88° C. for 7 to 9 hours, and cooling and introducing the solution in n-hexane to separate the low-k, flame-retardant, phosphoric, bi-functional benzoxazine.

Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).

Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.

Abstract: The present invention provides novel phosphinated compounds of monofunctional, bifunctional, multifunctional phenols represented by the following formulae and their derivatives, and preparation methods thereof:

Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Abstract: The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors.

Abstract: A phosphorous containing benzoxazine-based monomer, a polymer thereof, an electrode for a fuel cell including the same and an electrolyte membrane for a fuel cell, and a fuel cell including the same.

Abstract: This invention relates to syntheses for the preparation of benzoxazine, including benzoxazine monomers and benzoxazime oligomers, from phenolic compounds, aldehyde compounds, and either primary diamine compounds, such as diamino alkylene compounds, e.g., methylene diamine, or diamino arylene compounds, e.g., phenylene diamine, using water, and optionally an organic solvent, as the reaction solvent.

Abstract: A phosphorus containing monomer, a polymer thereof, an electrode for a fuel cell including the polymer, an electrolyte membrane for a fuel cell including the polymer, and a fuel cell including the electrode.