Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q, Z, R2, R3 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.

Abstract: The present invention relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.

Abstract: Premature termination codon readthrough prodrug compounds, compositions thereof, and methods of making and using the same are provided. In certain embodiments, the compounds are of Formula Ia or a pharmaceutically acceptable salt, solvate, polymorph, hydrate, ester, isomer, stereoisomer, or tautomer thereof, wherein R, A and W are as described herein.

Abstract: The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.

Abstract: The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: The present invention provides a compound of formula I: wherein R1, X1, X2, R2, R3, R4, R5, n, and m are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: The present disclosure relates to heterocyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of the TAM protein kinases and are useful in the treatment of TAM-associated diseases such as cancer.

Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.

Abstract: A compound of Formula I, enantiomers, diastereomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

Abstract: The present invention is directed to tricyclic compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.

Abstract: The invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system diseases, and tumor. The 4-substituted pyrrolo[2,3-d]pyrimidine compound of the invention is as shown in chemical formula I. The activity experimental results of the invention show that the new compound has obvious effect and activity in inhibition of Janus kinases, JAK-STAT, cell proliferation of human lymphocytoma, and rheumatoid arthritis.

Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

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 Lympho

Abstract: The present invention relates to compounds of formula I, wherein A, B, R1, R2, and Z are as defined hereinbefore.

Abstract: Provided herein, inter alia, are methods of synthesizing and formulating porphyrins, including manganese containing porphyrins. Also provided herein are pharmaceutical compositions and crystals of porphyrins achieved using the methods described herein.

Abstract: The application is directed to compounds of Formula I (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R1a, R1b, X, Y, Z, G, Q, W1 and W2 are defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

Abstract: The present invention relates to compounds of formula (I) that are metallo-?-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with ?-lactam antibiotics for overcoming resistance.

Abstract: The present invention relates to 4-azapodophyllotoxin analogs of formula (I) in which X, R1, R2, R3, R4 and Ar are as defined in claim 1, preferably a pharmaceutically acceptable salt thereof, optionally in the form of a solvate, a composition comprising said analogs, their use as medicament, in particular for the treatment of cancer, and a process for their preparation.

Abstract: The present disclosure concerns harringtonines salts at the crystalline state exhibiting a protonated nitrogen seen in solid state analysis and having general formula 1, comprising solvates, made by reacting a cephalotaxine ester alkaloid base having formula 2, in which R1 is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, and R2 is, independently, but not limited to H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, with an acid having general formula AH in a non-aqueous crystallization solvent, wherein the said salt has a large water solubility. The disclosure is also related to a process for preparing and purifying these salts and their use as chemotherapeutic drugs.

Abstract: The present invention provides a compound having the structure:

Abstract: The present invention relates to a curable bicyclic compound derived from biomass, solvent-free curable composition and a method for preparing thereof. The curable compound derived from biomass according to the invention comprises a bicycle structure, to which one of two epoxide functional groups are bonded.

Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.

Abstract: The present invention discloses a probe useful for the selective detection of metallo-beta-lactamases, in particular carbapenemases, thereby distinguishing those species of bacteria that are carbapenem-resistant from bacterial strains that are sensitive. Cephalospori based probes that have the 6,7 R,R configuration are susceptible to cleavage by beta-lactamases but cannot distinguish between cleavage by metallo-beta-lactamases and other beta-lactamases.

Abstract: A lanthanide complex, method of forming and method of using the lanthanide complex as a near-infrared luminescent material are described. The complex includes at least one lanthanide ion and at least one polydentate ligand derived from a molecule having the general formula of Structure 2: where: E represents a heteroatom or heteroatom-containing group and R1-R8 are independently selected from H, —OH, —NH2, —SO3H, —CO2H, halides, optionally substituted organic groups; and conjugated linking groups which link two of the polydentate ligands of Structure 2 together.

Abstract: The invention provides compositions and methods for mass spectrometric (MS), organic synthesis, and applications of organo-trifluoroborate, for example, as mass tags for use in negative ion mode. When subject to MS fragmentation, organo-trifluoroborates preferentially undergo neutral losses of hydrogen fluoride (HF) or boron trifluoride (BF3) molecules, transferring the negative charge to the rest of the molecule. Such a fragmentation pattern is used to detect and quantitate analytes of interest after derivatization with organo-trifluoroborates.

Abstract: Provided are a novel trisilyl amine derivative, a method for preparing the same, and a silicon-containing thin film using the same, wherein the trisilyl amine derivative, which is a compound having thermal stability, high volatility, and high reactivity and being present in a liquid state at room temperature and under pressure where handling is possible, may form a high purity silicon-containing thin film having excellent physical and electrical properties by various deposition methods.

Abstract: The present invention is directed to compounds having the Formula (I), (II), (III), (IV), and (V), compositions thereof, and methods for the treatment of a condition associated with a dysfunction in proteostasis.

Abstract: The present invention relates to a complexing agent and preparation method and use thereof, the complexing agent has a general formula MxHyPnO3n+1Rz, wherein M is any one or more of alkali metal ions and NH4+; R is acyl; x, n and z are positive integers, y is 0 or a positive integer and x+y+z=n+2. A preparing method of a complexing agent comprises: mixing alkali, carbonate or bicarbonate containing M, phosphoric acid and an acidic salt of monoprotic organic acids or polybasic organic acids containing an R group for reacting according to a molar ratio, then carrying one step polymerization on a reaction solution at 100-800° C. for 0.5-10h to obtain a finished product of the complexing agent; or drying the reaction solution firstly, and then polymerizing at 100-800° C. for 0.5-10h to obtain a finished product of the complexing agent.

Abstract: Disclosed are an o-phenyl chalcone compounds and preparation methods and uses thereof. The o-phenyl chalcone compounds are capable of inhibiting the aggregation of microtubules in tumor cells and influencing the mitosis of the cells, and have a high antitumor activity. The compounds also have inhibitory activity against proliferation on various tumor cells, such as a human ovary cancer cell A2780, a human colon cancer cell HCT8, a human breast cancer cell MCF7, a human lung cancer cell A549, a human colon cancer cell SW480, a human nasopharyngeal carcinoma cell CNE2, a human liver cancer cell HepG2 and the like at nanomole concentrations.

Abstract: The instant invention relates to a method of phosphorodiamidite production that comprises: (E1) preparing a purified solution of a dialkylamine in a polar solvent as follows:—the dialkylamine dissolved in a polar solvent is contacted with a quantity of phosphorus trihalide that is sufficient to react with the alcohol impurities contained in the dialkylamine but sufficiently low to leave a major part of the dialkylamine unreacted, whereby a mixture is obtained that contains the dialkylamine in the polar solvent and reaction products of the impurities with the phosphorous trihalide;—the unreacted dialkylamine and polar solvent present in the mixture obtained in step (E1.1.

Abstract: The present invention relates to compounds which can be used to control plant development. Indeed, the present invention discloses a new class of pyrabactin analogues which have a physiological effect on—for example—seed germination, and/or stomatal closure, and/or have developmental effects on root and shoot development and organogenesis. Hence, the latter compounds can be used to control plant development such as—for example—increasing the tolerance of plants to drought stress or to control physiological phenomena such as pre-harvest sprouting, tolerance to pathogens etc.

Abstract: Provided are a novel polyketone polymerization catalyst and a method of preparing a ligand, which can reduce production costs and can enable commercial mass synthesis by using ((2,2-dimethyl-1,3-dioxane-5,5-diyl)bis(methylene))bis(bis(2-methoxyphenyl)phosphine) as a ligand constituting the polykeytone polymerization catalyst, the ligand having a simple structure and a small molecular weight while having high activity.

Abstract: The following formula is an example of a phosphole compound of the present invention. The phosphole compound of the present invention has the characteristic of maintaining a high fluorescence quantum yield in a wide range of solvents from low-polarity solvents to high-polarity solvents, as well as the characteristic in which the fluorescence wavelength shifts to the longer wavelength side as the polarity of the solvent increases. Because of these characteristics, the phosphole compound of the present invention is expected to be used, for example, for quantitatively determining the polarity in the environment therearound by using the absorption wavelength and fluorescence wavelength thereof, or used as a new fluorescent probe dye or a highly efficient luminescent material in organic electronic devices.

Abstract: The present invention relates to novel derivatives of oxazaphosphorines that are pre-activated, to the methods for preparing same, to the pharmaceutical compositions containing same and to the therapeutic use thereof, in particular for treating cancer.

Abstract: This invention relates to a process for producing compounds derived from 9,10-Dihydro-9-Oxa-10-Phosphaphenantrene-10-oxide (DOPO). In particular, the invention relates to producing DOPO-derived compounds by reacting DOPO with diol compounds in the presence of a catalyst. This invention also relates to DOPO derived composition containing a high melting point diastereomer. The DOPO derived compounds may be useful as flame-retardants.

Abstract: There is provided an improved method for the recovery of residual, unseparated ?-ACF from reaction mixtures remaining from an initial synthesis of ACF, which is in particular usable on a large industrial scale, more particularly in the production of capecitabine.

Abstract: The present invention discloses a method for purifying ?-nicotinamide mononucleotide, comprising the steps of: a. sequentially microfiltrating and nanofiltrating a pretreated ?-nicotinamide mononucleotide solution with membrane concentration devices, to collect a concentrated crude product solution; b. adjusting the obtained crude product solution to pH 3-7, loading it onto a preparative reverse phase high performance liquid chromatographic column, and purifying by gradient elution using an octadecylsilane-bonded silica gel as a stationary phase, a hydrochloric acid solution at pH 3-7 as a mobile phase A, and ethanol as a mobile phase B, to obtain a purified sample solution; and c. nanofiltrating the purified sample solution with a membrane concentration device, and freeze drying it in a vacuum freeze drier, to obtain purified ?-nicotinamide mononucleotide.

Abstract: The present application discloses a simple process for the purification of neutral human milk oligosaccharides (HMOs) produced by microbial fermentation. The process uses a combination of a cationic ion exchanger treatment, an anionic ion exchanger treatment, and a nanofiltration and/or electrodialysis step, which allows efficient purification of large quantities of neutral HMOs at high purity. Contrary to the purification currently used in fermentative production of neutral HMOs, the presented process allows the provision of HMOs without the need of a chromatographic separation. The so purified HMOs may be obtained in solid form by spray drying, as crystalline material or as sterile filtered concentrate. The provided HMOs are free of proteins and recombinant material originating from the used recombinant microbial strains and thus very well-suited for use in food, medical food and feed (e.g. pet food) applications.

Abstract: Provided herein are glycomimetic E-selectin antagonist compounds of formula (I)) and pharmaceutical compositions comprising at least one of the same. The compounds of the present disclosure include trisaccharide domain mimics comprising at least one macrocycle created through the 2nd and 3rd positions on a galactose within the mimic. Methods are also provided comprising using at least one of such compounds and compositions comprising at least one of the same to treat and/or prevent diseases and disorders treatable by inhibiting binding of an E-selectin to an E-selectin ligand.

Abstract: Cells incorporating a synthetic molecule construct of the structure F—S1—S2-L where: F—S1 is an aminoalkylglycoside where F is a mono-, di-, tri- or oligo-saccharide and S1 is 2-aminoethyl, 3-aminopropyl, 4-aminobutyl, or 5-aminopentyl; S2 is —CO(CH2)2CO—, —CO(CH2)3CO—, —CO(CH2)4CO— or —CO(CH2)5CO—; and L is phosphatidylethanolamine.

Abstract: Conjugated molecules are prepared that comprise a predetermined number of oligo conjugation components. The conjugated molecules also may comprise one or more detectable labels. Preparation of these molecules can be implemented according to an asymmetric or a symmetric conjugation strategy.

Abstract: The invention provides for methods of inactivating virus in product feedstream in a manufacturing process of a therapeutic polypeptide using an environmentally compatible detergent. The environmentally compatible detergent does not adversely affect product quality while effectively inactivating virus in the feedstream.

Abstract: We disclose novel peptidomimetics with antiangiogenic activity and their uses, particularly in the treatment of neoplasms and chronic inflammation (in particular of: rheumatoid arthritis, colitis), in eczema, diabetes, age-related macular degeneration (ARMD), nephropathy and neuropathy, in particular for use in the form of intravenous infusions or injections, or implants releasing the active ingredient.

Abstract: The present invention relates to peptidomimetics of the formula (I) or (I)c wherein L1, L2, L3, R1, R2, R3, R4, R5, R6, n, m, Q, X, Z1 and Z2 are defined as mentioned in the description and to salts and solvates of each of these compounds and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as meticillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations.