Abstract: The invention provides boronic esters of Formula I wherein R1, R2, R3, and R4 are as described herein, and methods for the preparation and purification thereof.

Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.

Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.

Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.

Abstract: The present invention relates to FTY720 analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the alkyl side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy and in chromatography using fluorescence detection.

Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.

Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of ?-amino boronic acid derivatives.

Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.

Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.

Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.

Abstract: Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.

Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.

Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: 6-Amino-2-substituted-5-vinylsilylpyrimidine-4-carboxylates and 4-amino-6-substituted-3-vinylsilylpyridine-picolinates and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control

Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.

Abstract: A kind of new compounds, and their pharmaceutically acceptable salts, and hydrates are disclosed. The pharmaceutical composition thereof is also provided. And also are the medical uses of the compounds, pharmaceutically acceptable salts, hydrates and the pharmaceutical composition for treating the TRPV1-mediate diseases.

Abstract: An organic electroluminescence device includes: a pair of electrodes; and at least one organic layer including a light emitting layer, the light emitting layer being provided between the pair of electrodes, wherein at least one layer of the at least one organic layer contains a compound represented by formula (1): wherein each of Z11 and Z12 independently represents an aromatic heterocyclic ring or an aromatic hydrocarbon ring; R11 represents a hydrogen atom or a substituent, provided that a plurality of R11s are the same or different; m represents an integer of 1 or more; and L1 represents a single bond or an m-valent linking group and is linked to any one of C atoms in R11, Z11 and Z12, provided that when m is 1, L1 does not exist.

Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.

Abstract: Novel fluorescent markers of Formula I: are disclosed herein, wherein X and Y are independently or together absent or are independently selected from R and R1 are independently selected from H and alkyl; Ar is phenyl or heteroaryl; L is absent or a spacer selected from the group consisting of —NH—; —(CH2)nNH—; —NHSO2—; —(CH2)nNHCO—; -(cycloalkyl)NHCO—; —(CH2)nNHSO2—; -(cycloalkyl)NHSO2—; —CONH(CH2)nNHCO—; —CONH(cycloalkyl)NHCO—; —NHCO(CH2)nNHCO—; —NHCO(cycloalkyl)NHCO—; —(CH2)nSO2NH—; -(cycloalkyl)SO2NH—; —(CH2)nNHCSNH—; -(cycloalkyl)NHCSNH—; —CR?CR1—; —C?C—; —(CH2)nN?CH—; -(cycloalkyl)N?CH—; —N?CH(CH2)—; —N?CH(cycloalkyl)-; n is an integer ranging from 1 to 5; F is a fluorophore selected from the group consisting of fluorescein, rhodamine, eosin, thionine, safranin, coumarin, methoxycoumarin, dansyl, BODIPY and BODIPY derivatives; and wherein X, Y and L may be positioned in a 1,3,5; 1,2,3; 1,3,4 or in a 3,4,5 configuration respectively.

Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).

Abstract: A novel fluorescent compound having a high light fastness, high fluorescence quantum yield and sharp absorption spectrum, which emits fluorescence having a wavelength in long wavelength region, as well as its use as a labeling agent, is disclosed. In Formula [I] below, by forming a specific hetero ring(s) with R1 and R2, and/or R6 and R7, shift of the wavelength of the fluorescence to longer wavelength and increase in molar extinction coefficient are attained maintaining the high light fastness, high fluorescence quantum yield and sharp absorption spectrum which the fluorescent dyes having the boron dipyrromethene skeleton have.

Abstract: The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —

Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

Abstract: Compounds according to Formula I are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, D, W, X, Y, and Z are defined in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use in treating or preventing a disease or a condition associated with arginase activity.

Abstract: A charge-transporting material contains a compound represented by the following formula (1) in an organic layer, in which the contents of specific halogen-containing compounds are 0.1% or less to the compound represented by formula (1). In formula (1), each of A1 and A2 independently represents N, —CH or —CR; R represents a substituent; L represents a single bond, an arylene group, a cycloalkylene group or an aromatic heterocyclic group; each of R1 to R5 independently represents a substituent; each of n1, n2 and n3 independently represents an integer of 0 to 4; each of n4 and n5 independently represents an integer of 0 to 5; and each of p and q independently represents an integer of 1 to 4.

Abstract: A compound represented by the following general formula (I): {R1, R3, R6 and R8 are methyl groups and the like, R2 and R7 are cyano groups and the like, R4 and R5 are fluorine atoms and the like, and X is a group represented by the formula (A) [R11 is a monocarboxy-substituted C1-8 alkoxy group and the like, R12, R14 and R15 are hydrogen atoms and the like, and R13 is hydroxy group and the like], provided that the combination of the aforementioned substituents is such a combination that the compound represented by the formula (I) can be substantially non-fluorescent before reacting with peroxynitrite, and the compound represented by the formula (I) in which the group represented by the formula (A) is nitrated after reacting with peroxynitrite can be substantially highly fluorescent}, or a salt thereof, which is useful as a fluorescent probe for peroxynitrite measurement.

Abstract: The present invention relates to novel compounds of the formula (I) wherein R1 and R1? independently of each other are H or a substituent, halogen or SiR6R4R5; R2 and R2? may be the same or different and are selected from C1-C25alkyl, C3-C12-cycloalkyl, C2-C25alkenyl, C2-C25alkynyl, C4-C25aryl, C5-C25alkylaryl or C5-C25aralkyl, each of which is unsubstituted or substituted, and under conditions as defined in claim 1, R2 and/or R2? may also be halogen or hydrogen; X is a divalent linking group selected from formula (Ia) and formula (Ib); Y and Y? independently are selected from formula (Ic), formula (Id), formula (Ie), formula (If), formula (Ig); n and p independently range from 0 to 6; where further symbols are as defined in claim 1, and to corresponding oligomers and (co)polymers. The compounds according to the invention are useful as semiconductors and have excellent solubility in organic solvents and excellent film-forming properties.

Abstract: Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating FAAH-mediated disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.

Abstract: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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: A cationic compatible metal oxide and oral care compositions containing the metal oxide are disclosed. Preferably, the oral care compositions contain a cationic compatable metal oxide and a cationic ingredient, such as for example, a cationic antibacterial agent such as cetyl pyridinium chloride (“CPC”). The cationic compatible metal oxide, e.g. silica, comprise metal oxide particles having a subtantially negative surface charge and a vitamin deposited onto or reacted with the surface of the metal oxide particles in an amount sufficient to provide a substantially positive surface charge on the metal oxide particle. Processes for making and using the vitamin modified metal oxide in oral care compositions are also disclosed.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?xHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1, 2 or 3, or anions selected from the group of [(Rf1SO2)2N]? anions or anions selected from the group of [BFWRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.

Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Abstract: Macrocyclization of amino acids or linear peptides upon reaction with amphoteric amino aldehydes and isocyanides is provided.

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.

Abstract: Disclosed herein are vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives useful as synthetic intermediates for the preparation of therapeutic agents. Also disclosed are methods of synthesis of vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives.

Abstract: piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:

Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: A method for generating a recombinant clonal cell line expressing a target cell surface receptor at a specific level of expression from a cell population comprising cells transfected with a plasmid encoding the cDNA sequence of the target receptor and expressing the target cell surface receptor, the method comprising (c) incubating the cell population with a receptor specific fluorescent ligand (d) selecting single cells from step (c) expressing the target cell surface receptor by monitoring the specific binding of the fluorescent ligand using flow cytometry; and novel fluorescent ligands.

Abstract: This invention relates to organometallic precursor compounds represented by the formula (H)mM(R)n wherein M is a metal or metalloid, R is the same or different and is a substituted or unsubstituted, saturated or unsaturated, heterocyclic radical containing at least one nitrogen atom, m is from 0 to a value less than the oxidation state of M, n is from 1 to a value equal to the oxidation state of M, and m+n is a value equal to the oxidation state of M, a process for producing the organometallic precursor compounds, and a method for producing a film or coating from the organometallic precursor compounds.