Abstract: The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Abstract: The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, wherein A is a bond, alkyl or alkoxy optionally substituted with one or more R? as defined herein, *—N(R??)CO—, *—CON(R??)—, *—N(R??)CON(R??)—, —S—, —SO—, *—N(R??)—, *—N(R??)CO—, *—CON(R??)—, —CO—, *—COO—, *—OOC—, *—SO2N(R??)—, —SO2, or *—N(R??)—SO2—, wherein R?? is as defined herein and * specifies the point of attachment to X; X is aryl, cycloalkyl, aralkyl, heterocyclyl or heteroaryl, which may be substituted with one or more RX further described herein; L is a bond or *—N(RN)CO—, *—CON(RN)—, *—N(RN)—, *—C?N(RN)—, *—N(RN)-alkyl-, *-alkyl-N(RN)—, *—N(RN)CON(RN)—, *—CO—, *—CO2—, alkyl, *-alkyl-O-alkyl-, *—NCO—CH?CH—, *—CH?CH—CONH—, *—SO2N(RN)—, *—N(RN)SO2—, or heterocyclyl, wherein * specifies the point of attachment to X; Y is H, alkyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heteroaryl, which may be substituted with one or more RY further described herein; and R and RN

Abstract: The present invention relates to a compound for detecting phosgene and DCP (diethyl chlorophosphate) and a composition for detecting phosgene and DCP (diethyl chlorophosphate) comprising the said compound. More precisely, the compound for detecting phosgene and DCP of the present invention can selectively detect phosgene and DCP either in the liquid phase of gas phase by detecting the changes of fluorescence and color development very quickly within a few seconds with nM sensitivity. Therefore, the compound can also be effectively used as an ingredient for the composition and kit for the detection of one or more materials selected from the group consisting of phosgene and DCP.

Abstract: Sanguinarine analogs as PP2C inhibitors are disclosed for the treatment of various cancers, as well as methods of synthesizing such analogs.

Abstract: The present invention relates to a method of producing anhydrosugar alcohol by dehydrating sugar alcohol at high pressure in the presence of a catalyst which is less acidic than a conventional sulfuric acid catalyst and which can suppress side reactions at high temperature. According to the present invention, anhydrosugar alcohol can be produced in a yield similar to that in a vacuum reaction.

Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

Abstract: The present invention discloses a novel process for the preparation of macrocyclic ketone analogs of halichondrin B or pharmaceutically acceptable salts thereof and to novel intermediates which are produced during the course of carrying out the novel process.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents —CH?, —C(—R7)?, or —N?, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.

Abstract: The present invention encompasses the use of compounds for a novel approach to treat and prevent diseases, conditions, and disorders such as diabetes and ischemic reperfusion injury. Compounds of the invention, including but not limited to BAM15 ((2-fluorophenyl){6-[(2-fluorophenyl)amino](1,2,5-oxadiazolo[3,4-e]pyrazin-5-yl)}amine), a mitochondrial uncoupler, can improve glucose tolerance, increases cellular oxygen consumption, treat or prevent kidney ischemia reperfusion injury reverse insulin resistance, reverse or treat hyperinsulinemia, and reverse or treat hyperlipidemia. The present invention further provides novel compounds as well as methods for identifying compounds with the same or similar properties as BAM15.

Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].

Abstract: The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

Abstract: The present application relates to novel amino-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

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. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.

Abstract: The Invention relates to a novel receptor molecule for estimation of amino acids based on florescence enhancements. Particularly, the invention relates to a novel Cu (II)-complex as a turn-on luminescence probe for selective detection of cysteine and histidine in pure aqueous environment and in biological sample as well as for detection of cyanide ions among various anions under physiological conditions.

Abstract: A catalyst includes a bis(2-pyridylmethyl)amine-based ligand. A method of forming a catalyst, may include: reacting bis(2-pyridylmethyl)amine-based compound with a terminal azide and/or a terminal alkyne in the presence of Cu(I) to form a bis(2-pyridylmethyl)amine-based ligand. A method of using such catalysts may include neutralizing toxicity of at least one organophosphorus-based compound by reacting the organophosphorus-based compound with a bis(2-pyridylmethyl)amine-based ligand-metal complex.

Abstract: The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.

Abstract: The present invention is directed to compositions for silylating organic substrates containing C—H or O—H bonds, especially heteroaromatic substrates. The compositions are derived from the preconditioning of mixtures of hydrosilanes or organodisilanes with bases, including metal hydroxide and metal alkoxide bases. In some embodiments, the preconditioning results in the formation of reactive silicon hydride species.

Abstract: Provided is a method of preparing a silylative-reduced N-heterocyclic compound by reducing an N-heteroaromatic compound including a sp2 hybridized nitrogen atom while simultaneously introducing a silyl group into a beta-position with respect to a nitrogen atom of the N-heteroaromatic compound, using a silane compound, in the presence of an organoboron catalyst.

Abstract: A cyclic organosilicon compound having a (meth)acrylic group and a urea structure on a silicon atom cures into a product having improved flexibility, surface hardness, and evaporation amenability.

Abstract: The invention relates to alkenyl(perfluoroalkyl)phosphinic acids, to the preparation and intermediates thereof, to the use thereof as monomers for the preparation of oligomers and/or polymers, to the corresponding oligomers/polymers, to the corresponding support materials comprising the oligomers/polymers, and to the use thereof as ion exchangers, as catalysts or extraction medium and corresponding salts thereof.

Abstract: The present discovery pertains to the discovery of certain amphiphilic compounds that may be useful for the management of sebum secretion in subjects with acne, oily skin, or seborrheic dermatitis. These compounds are 1-dialkylphosphorylalkanes with the longest alkyl group being seven or more carbons. Preferably, a compound is dissolved in a dermatologically acceptable vehicle, and delivered to the skin in a solution, gel, lotion, cream, or ointment. The method of application may be with the surface of the finger, or via an applicator. The decrease is sebum secretion in certain subjects may result in skin conditions that enhance cosmetic appearance and ameliorate skin disorders.

Abstract: [Object] To provide a phosphorylcholine group-containing compound capable of producing a phosphorylcholine complex, and the phosphorylcholine complex, the phosphorylcholine complex being easily manufactured and suitable for use as a phosphorylcholine antigen. [Solving Means] There are provided a phosphorylcholine group-containing compound having a structure represented by the following formula (1), and a phosphorylcholine-protein complex having a structure in which the phosphorylcholine group-containing compound and an amino acid amine site of a protein are amide bonded.

Abstract: The present invention relates to an antioxidant compound having anti atherosclerotic effect and preparation thereof. The present invention more particularly relates to the synthesis of TPP+ coupled esculetin (mitochondria-targeted esculetin [Mito-Esc]) followed by the biological evaluation of Mito-Esc for its ability to attenuate Angiotensin-II-induced atherosclerosis in apolipoproteinE knockout (ApoE?/? mice along with the endothelial cell age-delaying effects of Mito-Esc.

Abstract: A hydroformylation process wherein the hydrolyzable organophosphorous ligand component of the catalyst is supplied as a stabilized ligand composition comprising a hydrolyzable organophosphorous ligand and, per 100 moles compound, from 0.05 to 13 acid-neutralizing equivalents of an acid scavenger.

Abstract: Novel phosphorescent tetradentate platinum compounds of Formula I are provided. The complexes contain a dibenzo moiety, which allows for the creation of OLED devices with improved properties when compounds of Formula I are incorporated into such devices. Compounds of Formula I? that comprise two ligands that contain a 5-membered carbocyclic or heterocyclic ring, one of which contains an imidazole ring with a twisted aryl group attached to N?1 and a second aromatic ring that is attached to the platinum via a carbon atom. These compounds may be advantageously used in OLEDs.

Abstract: Phosphorescent metal complexes comprising a pendant redox-active metallocene are disclosed. These complexes are useful as emitters for phosphorescent OLEDs.

Abstract: [Object] An anticancer agent capable of continuously killing cancer cells in a plurality of phases is provided. [Solution] An anticancer agent contains a complex produced by making a metal-salen complex compound, which includes a central metal and (N, N, O, O) as a quadridentate ligand and is magnetic, bind to taxane molecules which are anticancerous; and the anticancer agent is to kill cancer cells regarding which phase transition of its cell cycle occurs between phases including Gap1, Synthesis, Gap2, and Mitosis and Cytokinesis. The present disclosure is suited for use to kill cancer cells of breast cancer and, particularly, cancer cells of triple-negative breast cancer. The present disclosure is designed to make the anticancer agent contact the cancer cells in two or more continuous phases selected from a group consisting of Gap1, Synthesis, Gap2, and Mitosis and Cytokinesis and kill the cancer cells.

Abstract: The present invention relates to new compounds comprising a siderophore moiety as well as a core structure able to chelate a metal ion. Optionally, the compounds may have additionally a moiety with a functional element including a marker molecule, a bioactive agent, an activity based probe suitable to monitor the aberrant expression or activity of proteins involved in the initiation and progression of bacterial infection, or a compound useful for bacterial inhibition. In a further aspect, the present invention provides a pharmaceutical composition containing said compound, for example, said pharmaceutical composition is an antibiotic. Additionally, the present invention relates to the use of said compounds in diagnostic methods, in particular, imaging methods including SPEC, PET or MRI. In an embodiment of the present invention, the compound is part of a theranostic composition having both, therapeutic as well as diagnostic activities.

Abstract: The invention relates to bola-amphiphilic compounds and their uses for biomedical application. The invention particularly relates to the use of bola-amphiphilic compounds for providing low molecular weight gels (LMWG), useful, in particular, as culture media for animal or human cells, or as biocompatible material for biomedical applications.

Abstract: The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.

Abstract: The present invention provides compounds of Formula (I) or Formula (II): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Abstract: The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

Abstract: A Gadd45?/MKK7 inhibitor for use in a method of treating a resistant haematological malignancy, combinations of said inhibitor with a further anti-cancer agent and related methods of use.

Abstract: The present disclosure provides aromatic-cationic peptide compositions and methods of using the same. The methods comprise use of the peptides in electron transport and electrical conductance.

Abstract: A method is provided for treatment of a condition mediated by Nox2 in a patient. The method comprises administering to the patient by inhalation a polypeptide as described herein, able to inhibit superoxide production by Nox2.

Abstract: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

Abstract: Described herein is the discovery of novel PSMA-specific peptides, which were identified through a novel combinatorial biopanning method. One of the novel PSMA-specific peptides discovered, GTIQPYPFSWGY (or GTI) (SEQ ID NO: 2), exhibits high binding affinity and selectivity to PSMA and PSMA-positive prostate cancer cells. It was found that GTI can mediate internalization of the apoptotic KLA peptide to PSMA-positive LNCaP cells and induce cell death. Moreover, a FAM-labeled GTI peptide shows a high and specific tumor uptake in nude mice bearing human prostate cancer xenografts. It was demonstrated that the GTI peptide can be employed as a PSMA-specific ligand for prostate cancer diagnosis and/or for targeted drug delivery to prostate cancer cells.

Abstract: Functional-lipid constructs of the structure F-S-L are disclosed, wherein F comprises a tyrosine or histidine residue, S is a spacer covalently linking F to L and L is a lipid. The functional residue may be iodinated and used to radiolabel a biological entity with 1251 and the iodinated constructs are used in a non-invasive method of monitoring the distribution of a biological entity in vivo.

Abstract: The present invention is to execute macromolecule intracellular transduction technology (MITT) for delivering biologically active macromolecules into the cells; specifically, by exploiting well-enhanced hydrophobic cell penetrating peptide (CPP)—advanced macromolecule transduction domain (aMTD)—to effectively transduce biologically active molecules into the plasma membrane, polynucleotides encoding the same, methods of identifying the same, systems of genetically engineering a biologically active molecule with much enhanced cell-permeability by using the same, methods of importing a biologically active molecule into a cell by using the same, and uses thereof.

Abstract: The present invention relates to a process for the preparation of Linaclotide by oxidizing linear Linaclotide of formula (II) using combination of air and oxidizing agent followed by purification using RP-HPLC.

Abstract: The present invention relates to methods and uses for screening anti-hepadnaviral substances, wherein the substances are screened for the capacity to inhibit covalently closed circular (ccc) DNA of a hepadnavirus, like hepatitis B virus. The methods and uses take advantage of cells comprising a nucleic sequence encoding a tagged hepadnavirus e antigen, like Hepatitis B virus e antigen (HBeAg). Furthermore, the present invention provides nucleic acid sequences encoding a tagged hepadnavirus e antigen and proteins encoded thereby. Also kits for use in the screening methods are provided.

Abstract: The invention provides a recombinant polypeptide comprising the EDIII domain of each of Dengue virus serotype DENV-1, DENV-2, DENV-3, and DENV-4 linked to the N-terminal of HBsAg.

Abstract: The invention relates to the treatment of bacterial respiratory infections using the bacterially-originating antibiotics known as pyocins. In particular, the invention provides the use of S-type pyocins, administered by pulmonary administration, for the treatment of such infections.

Abstract: The disclosure provides nucleic acids, and variants and fragments thereof, obtained from strains of Bacillus thuringiensis encoding polypeptides having pesticidal activity against insect pests, including Lepidopteran and Coleopteran. Particular embodiments of the disclosure provide isolated nucleic acids encoding pesticidal proteins, pesticidal compositions, DNA constructs, and transformed microorganisms and plants comprising a nucleic acid of the embodiments. These compositions find use in methods for controlling pests, especially plant pests.

Abstract: The present invention provides peptides comprising a sequence of X-6X-5X-4X-3X-2X-1X1PX3X4PX6X7P-GX10X11AX13X14X15X16LX18X19X20X21X22X23LX25X26YLX29X30X31X32 wherein the amino acids X-6, X-5, X-4X-3, X-2, X-1, X1, X3, X4, X6, X7, X10, X11, X13, X14, X15, X16, X18, X19, X20, X21, X22, X25, X26, X29, X30, X31, and X32 are as defined herein. The present invention further provides pharmaceutical compositions comprising the peptides and methods of using the peptides. Also provided are methods of screening a library of peptide dimers using a peptide dimer display technology.