Abstract: Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds.

Abstract: Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds.

Abstract: The present disclosure provides compounds comprising a tetrapyrrole (e.g., a tetrapyrrole group) linked via a linker to one or more ligands and uses of the compounds. The compounds may be used as imaging agents (e.g., MRI contrast agents) or as both imaging and therapeutic agents. The compounds may be used to treat individuals in need of treatment for a hyperproliferative disorder, such as, for example, malignancy. The present disclosure also provides kits comprising pharmaceutical preparations containing any one or any combination of the compounds described herein.

Abstract: The present invention related to novel morphinans, compositions comprising the novel morphinans, and their uses as agonists of the kappa opioid receptor.

Abstract: The present invention discloses a composition comprising at least one or more stereoisomers of a compound represented by the following Formula (1), wherein, in a gas chromatogram obtained by analyzing the composition by gas chromatography, the ratio of the area of the maximum peak with respect to the total area of peaks derived from the stereoisomers is 90% or more. The present invention also discloses: a curable composition comprising the above described composition, and one selected from the group consisting of a thermal cationic polymerization initiator, an acid anhydride-based curing agent and a curing accelerator, and a photo-cationic polymerization initiator; as well as a cured product therefrom. The above described curable composition is useful in that it allows for the production of a cured product having a high heat resistance. (In the Formula (1), R1 to R18 are each independently selected from the group consisting of a hydrogen atom, an alkyl group and an alkoxy group.

Abstract: The present invention relates to a crystalline form of a salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide, and a pharmaceutical composition containing the same. The crystalline form of the salt of the compound can be easily used for preparing a pharmaceutical composition containing the same as an active ingredient.

Abstract: The present invention relates to a compound, 4-amino-N-(1-((3-chloro-2-fluoro-4-hydroxyphenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide, and pharmaceutically acceptable salts thereof having inhibitory activity for protein kinases.

Abstract: Compounds of Formula I, pharmaceutically acceptable salts thereof, tautomers thereof, pharmaceutically acceptable salts of the tautomers, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.

Abstract: The invention provides new heterocyclic compounds having the general formula wherein A, L, X, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Abstract: This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahy-dro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base hydrate (Form 24). This invention also relates to pharmaceutical compositions comprising Form 24, and to methods of using Form 24 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.

Abstract: The present invention refers to novel thiazolo[5,4-d]pyrimidine derivatives that are inverse agonists of the adenosine A2A receptor, to a process for their preparation, to the pharmaceutical compositions containing them and to their use in the medical field, in particular in the therapeutic treatment of diseases or disorders associated to an activity of the adenosine A2A receptor, and more in particular in the therapeutic treatment of neurological diseases, of pain, of cancer, and of dermal fibrosis and scarring.

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).

Abstract: In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, X, Y, Z, R1, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The present disclosure provides a compound of Formula I wherein M is a metal selected from the group consisting of Cu, Ag, and Au; T is a five-membered or six-membered heterocyclic ring, which is optionally substituted, wherein T includes a carbene carbon coordinated to M, or T is aromatic and includes a sp2 nitrogen coordinated to M; L is a group comprising a coordinating member selected from the group consisting of C, N, O, S, and P, wherein the coordinating member coordinates L to M; and Q1 and Q2 are each independently a linker, wherein the linker connects T to the coordinating member of L to form a macrocyclic ligand coordinated to M.

Abstract: Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.

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: A methylsilicic acid hydrogel is produced by reacting a solution of sodium methyl siliconate with a gaseous acid agent. The resulting product is vacuumised to remove residual gas, and washed with water. A significant OH-group content in the hydrogel, which results from bubbling the gaseous acid agent through the solution of sodium methyl siliconate, makes it possible to increase the selectivity of the adsorption properties when the hydrogel is used in medicine and veterinary science.

Abstract: Guanidinium-rich oligophosphotriesters transporter compounds and methods of making and using the same are provided. Also provided are pharmaceutical compositions that include the subject transporter compounds, where the transporter can be joined to a cargo of interest, and is formulated with a pharmaceutically acceptable excipient. Formulations may be provided in a unit dose, where the dose provides an amount of the compound effective to afford a desired therapeutic effect. Methods of using the subject transporter compounds to deliver a cargo moiety to a cell are provided, where the method can include contacting a target cell with the transporter compound. The subject methods can be performed in vitro or in vivo.

Abstract: A composition including a first compound including a compound represented by Formula 1, a second compound including a compound represented by Formula 2, and a third compound including a compound represented by Formula 3, and an organic light-emitting device including the composition: wherein the description of Formulae 1 to 3 are the same as described in the specification.

Abstract: An organometallic compound represented by Formula 1, an organic light-emitting device including the organometallic compound, and a diagnostic composition including the organometallic compound: wherein, in Formula 1, Y2, a ring CY2, R1 to R8, R20, A1 to A7 and d2 may be each independently the same as described in the specification.

Abstract: Disclosed are an organometallic compound represented by Formula 1, an organic light-emitting device including the same, and an electronic device including the organic light-emitting device: The detailed description of Formula 1 is the same as described in the present specification.

Abstract: A compound comprising a first bidentate ligand LA, wherein LA comprises a structure of Formula I; wherein Z is selected from the group consisting of O, S, NR, BR, CRKRL, SiRKRL, —CRKRLCRMRN—, —SiRKRLSiRMRN—, —CRKRLO—, —SiRKRLO—, and —CRK?CRL—; wherein ring A, ring B, and ring C are each independently a 5-membered carbocyclic ring, 5-membered heterocyclic ring, 6-membered carbocyclic ring or 6-membered heterocyclic ring; wherein LA is coordinated to a metal M forming a 5-membered chelate ring; wherein M is selected from the group consisting of Ir, Pt, Pd, Ru, Rh, Os, Re, Cu, Ag, and Au; wherein RA, RB, and RC each represent mono to the maximum allowable substitution, or no substitution; wherein each R, RK, RL, RM, RN, RA, RB, and RC is independently a hydrogen or a substituent selected from the group consisting of deuterium, halogen, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, boryl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, car

Abstract: Provided are an organometallic compound represented by Formula 1, an organic light-emitting device including the same, and an electronic apparatus including the organic light-emitting device: wherein, in Formula 1, Y2, ring CY1, ring CY2, T1, T2, A1 to A7, a1, and a2 are as defined in the specification.

Abstract: The present invention relates to the technical field of chiral synthesis, and specifically provides a new type of oxa-spirodiphosphine ligands. The bisphosphine ligand is prepared with oxa-spirobisphenol as a starting material after triflation, palladium catalyzed coupling with diaryl phosphine oxide, reduction of trichlorosilane, further palladium catalyzed coupling with diaryl phosphine oxide, and further reduction of trichlorosilane. The oxa-spiro compound has central chirality, and thus includes L-oxa-spirodiphosphine ligand and R-oxa-spirodiphosphine ligand. The racemic spirodiphosphine ligand is capable of being synthesized from racemic oxa-spirobisphenol as a raw material. The present invention can be used as a chiral ligand in the asymmetric hydrogenation of unsaturated carboxylic adds. The complex of the ligand with ruthenium can achieve an enantioselectivity of greater than 99% in the asymmetric hydrogenation of methyl-cinnamic acid.

Abstract: An organometallic compound represented by Formula I, an organic light-emitting device including the same, and a diagnostic composition including the organometallic compound.

Abstract: The invention provides a compound of formula (Ia) or (Ib): or a salt thereof, wherein A, B, C, D, E, F, J, K, L, M, Q, V, X, Y, W and Z have any of the values described in the specification, as well as compositions comprising a compound of formula (Ia) or (Ib) or a salt thereof, and methods of use thereof.

Abstract: An organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, wherein the organic layer includes an emission layer, the emission layer includes a first host, a first dopant, and a second dopant, and the first dopant is an organometallic compound the first dopant represented by one of Formulae 40 and 50 and including metal having an atomic weight of 40 or greater:

Abstract: The present invention relates to methods of manufacturing multiple metal propionates in a single reaction using sodium hydroxide as initiator and propionic acid as solvent. The method provides up to 95% conversion with greater than 60% yield. In addition, the method significantly reduces the cost or production by shortening reaction time, eliminating secondary mixing process, and providing simultaneous drying and micronization steps.

Abstract: Disclosed is a method for purifying sialylated oligosaccharides from a fermentation broth, cell-lysate or biocatalytic reaction mixture for obtaining high amounts of desired sialylated oligosaccharides in high purity. The method is particular suitable for the large-scale economic purification of sialylated human milk oligosaccharides (such as 3?-sialyllactose, 6?-sialyllactose or sialylated lacto-N-tetraose derivatives) from microbial fermentation, using recombinant bacterial cells or yeast cells. The obtained material is of high purity and can be used for food or medical application such like medical nutrition products, infant formula, dietary supplements, general nutrition products (e.g. dairy drinks).

Abstract: The present invention related to an arabinoxylo-oligosaccharide composition comprising at least one arabinose unit linked to one of the xylose units of the backbone, per molecule, wherein the at least one arabinose unit is an ?-L-arabinofuranosyl, wherein said composition has an xylo-oligosaccharide backbone with a degree of polymerization of 1-10.

Abstract: The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

Abstract: Provided in the present invention are a compound of Formula (I), a pharmaceutical composition comprising the same, a method for preparing the same, and use thereof as a NS5B polymerase inhibitor, a DNA polymerase inhibitor or a reverse transcriptase inhibitor for the prevention or treatment of viral diseases or cancers.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: Cyclic-GMP-AMP synthase (cGAS) and cyclic-GMP-AMP (cGAMP), including 2?3-cGAMP, 2?2-cGAMP, 3?2?-cGAMP and 3?3?-GAMP, are used in pharmaceutical formulations (including vaccine adjuvants), drug screens, therapies, and diagnostics.

Abstract: The present invention relates to a process for the purification of methylcobalamin, namely from iron cyanide impurities, comprising contacting a solution comprising methylcobalamin and iron cyanide anions with a strongly basic anion exchange resin. This purification process can advantageously be used for removing iron cyanide impurities from methylcobalamin obtained by reductive methylation of cyanocobalamin and wherein iron (II) salts are used as cyanide scavengers, thus providing methylcobalamin with a reduced iron content. Methylcobalamin (R is methyl).

Abstract: The present invention provides improved processes for purifying liraglutide. Liraglutide is purified via two sequential RP-HPLC purifications followed by a salt-exchange step, where a pH is kept constant in the first and second purification steps. In particular, the processes utilize a halogenated solvent in a sample preparation step, which provides better solubility and an environment suitable for decarboxylation for crude liraglutide prior to a RP-HPLC purification.

Abstract: Provided herein are methods for the production of native and reconstituted hyaluronan (HA) complexes containing pentraxin-3 (PTX3) and heavy chain 1 (HC1) of inter alpha inhibitor (I?I). Compositions containing the complexes and therapeutic methods using the complexes are provided. Combinations and kits for use in practicing the methods also are provided.

Abstract: Compositions comprising an antioxidant directed or indirectly conjugated to an aromatic-cationic peptide are provide. Said antioxidants are selected from TEMPO, Tro, PBN, AHDP, DBHP, Caf and Hem and may be conjugated to the aromatic-cationic peptide directly or indirectly via a linker to the N-terminus, C-terminus or a side chain of an amino acid residue of the aromatic-cationic peptide. In some embodiments, the aromatic-cationic peptide is 2?,6?-Dmt-D-Arg-Phe-Lys-NH2, Phe-D-Arg-Phe-Lys-NH2 or D-Arg-2?,6?-Dmt-Lys-Phe-NH2. These conjugates have increased antioxidant activity as compared to the unconjugated aromatic-cationic peptide and have utility in treating complex regional pain syndrome.

Abstract: The present technology provides methods of generating the peptides, and pharmaceutically acceptable salts of the peptides and intermediates thereof. In some embodiments, the peptide is D-Arg-2?6?-Dmt-Lys-Phe-NH2.

Abstract: The present invention relates to novel tetrapeptides as well as the use thereof as antimicrobial agents.

Abstract: Disclosed herein are composite polypeptide. According to various embodiments, the composite polypeptide includes a parent polypeptide and a metal binding motif capable of forming a complex with a metal cation. The composite polypeptide may be conjugated with a linker unit having a plurality of functional elements to form a multi-functional molecular construct. Alternatively, multiple composite polypeptides may be conjugated to a linker unit to form a molecular construct, or a polypeptide bundle. Linker units suitable for conjugating with the composite polypeptide having the metal binding motif are also disclosed.

Abstract: The present invention provides DEPDC1-derived epitope peptides having the ability to induce cytotoxic T cells. The present invention further provides polynucleotides encoding the peptides, antigen-presenting cells presenting the peptides, and cytotoxic T cells targeting the peptides, as well as methods of inducing the antigen-presenting cells or CTLs. The present invention also provides compositions and pharmaceutical compositions containing them as an active ingredient. Further, the present invention provides methods of treating and/or preventing cancer, and/or preventing postoperative recurrence thereof, using the peptides, polynucleotides, antigen-presenting cells, cytotoxic T cells or pharmaceutical compositions of the present invention. Methods of inducing an immune response against cancer are also provided.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer, in particular myeloma. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer, in particular myeloma. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer, in particular myeloma. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: Peptide inhibitors of activation of hepatitis C virus (HCV) NS3 protease are disclosed. They are analogs of the activation peptide HCV NS4 of residues 21-33 of SEQ ID NO: 2 and contain non-proteinogenic amino acids. Competitive binding studies showed the peptide analogs bind HCV NS3 protease at the activation site.

Abstract: The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of ?4?7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, possess high selectivity against ?4?1 binding, and have high stability under gastrointestinal conditions.

Abstract: Synthetic cyclic peptide modulators of the AgrC quorum sensing system of S. epidermidis. Synthetic agonists and antagonist of AgrC-I are described. Compounds capable of either pan-group or group-selective AgrC receptor inhibition in S. epidermidis were identified. Additionally, compounds that are species selective, and could be applied to selectively modulate either S. epidermidis or S. aureus AgrC receptors were identified. An AgrC-I agonist was found which strongly inhibits S. epidermidis biofilm growth, with a higher potency and efficacy than that of native AIP-I. Methods of modulating virulence in S. epidermidis and related Staphylococcus by contacting a bacterium or a bacterial environment, such as a biofilm, with a modulator of the disclosure are provided. Methods are provided for treating infections of S. epidermidis and related Staphylococcus by administering a therapeutically effective amount of one or more compounds herein to an individual in need thereof.

Abstract: The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., KD of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly).