Abstract: The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for tau imaging, and preparations of tau imaging formulations.

Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

Abstract: The present invention provides quenchers of excited state energy, probes and other conjugates comprising these quenchers, and methods of their use.

Abstract: The present invention provides novel neuromodulatory compounds and compositions thereof. The invention also relates to methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; as well as intermediates for the preparation compounds.

Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.

Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Abstract: The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.

Abstract: The present invention relates to compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

Abstract: New amorphous solid phases of sitagliptin with derivatives of hydroxybenzoic acids, dihydroxybenzoic acids and trihydroxybenzoic acids as coformers; the obtained new solid phases possess enhanced pharmaceutical properties such as enhanced solubility and higher dissolution rate, as compared to the sitagliptin phosphate monohydrate, and they are also stable under ambient conditions.

Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as ERK (MAPK). Also provided are methods of using such compounds or compositions, and methods of using these compositions to modulate the activities of one or more of these kinases, especially for therapeutic applications such as the treatment disorders such as cancer.

Abstract: The invention described herein relates generally to neuroactive compounds and compositions for the treatment psychotic disorders, methods for treating psychosis using these neuroactive compounds, and methods for screening for novel neuroactive compounds. Certain aspects are directed to a family of compounds called “finazines.” Certain aspects are directed to in vivo screening methods using high-through-put behavioral assays in zebrafish.

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

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 provides processes for the preparation of Edoxaban (1) and salts thereof, as well as intermediates thereof. In particular, intermediate compounds and/or salts of the Formulae (3), (4), (6-A), (7-A), (8-A), (9-A) and (10-AS) are provided.

Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Abstract: The disclosure is directed to compounds and compositions that inhibit Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase and methods of their use.

Abstract: Disclosed are a quinoline derivative, and a pharmaceutical composition, a preparation method and a use thereof. The quinoline derivative of the present invention has a c-Met inhibitory activity and can be used for the treatment, relieving and/or prevention of cancers or similar diseases.

Abstract: The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilizing the radiolabelled compounds of the invention.

Abstract: A method for preparing an anionic polymerization initiator, a device for manufacturing the same, and an anionic polymerization initiator prepared therefrom is provided. And the method for preparing an anionic polymerization initiator according to the present invention is characterized in that in a continuous reactor an amine compound of Formula 1 and/or Formula 2; an organometallic compound; and/or a conjugated diene compound are introduced in the form of a solution and reacted.

Abstract: The invention provides organoboron precursors and facile photoirradiation and/or heating methods of making corresponding elimination products. Some elimination products are polycyclic aromatic molecules wherein a number of aromatic C—C moieties have been replaced by a B—N moiety to form azaborine compounds with interesting properties such as electronic, photophysical, luminescent, as well as chemical properties. Examples of polymer films that were doped with such compounds are shown wherein irradiated portions of the polymer film luminesce. The invention further provides methods of producing photoluminescence and electroluminescence, and uses of the compounds of the invention in luminescent probes, sensors, electroluminescent devices, hydrogen storage materials, optoelectronic materials, and bioactive molecules.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: The present invention relates to novel full-color tunable light emitter based on N,C-chelate four-coordinate organoborons having excellent Quantum yield, stokes shift and solvate chromism of Formula (I);

Abstract: A method of separating a metal organic framework (MOF) from a solution and associated apparatus. The method comprises: providing a MOF containing solution; contacting the MOF containing solution with an acoustic reflector surface such that, any high frequency ultrasound applied within the MOF containing solution reflects off the acoustic reflector surface; and applying a high frequency ultrasound of at least 20 kHz to the MOF containing solution. The MOF material is substantially separated from solution as aggregated sediment that settles out of solution.

Abstract: Provided is a method of controlling release of nitric oxide, and more particularly, to a method of selectively releasing nitric oxide depending on a change in pH using calcium phosphate. The method of selectively releasing nitric oxide according to the present invention may stably deliver nitric oxide to a desired site, and induce release of nitric oxide by a change in pH, thereby making it possible to improve a therapeutic effect while preventing a loss of nitric oxide.

Abstract: A method for preparing a stabilizer containing phosphate ester, including following steps: (1) distributing a compound containing phosphorous and oxide in polar aprotic solvent to obtain a mixture; (2) adding bis(2-hydroxyethyl) terephthalate (BHET) into the mixture to carry out a reaction so as to obtain a solution; and (3) hydrolyzing the solution to obtain a stabilizer containing phosphate ester, where the stabilizer includes compounds represented by the following formulas (I) and (II): where X1, X2 and X3 are independently selected from the moiety represented by following formula (III), and R1 and R2 are independently selected from one of the linear or branched alkylene radicals comprising 2 to 4 carbon atoms The method yields a phosphate ester containing a phosphate monoester and a phosphate diester of a high content and only a minor amount of phosphoric acid in the absence of phosphate triester without the step of extraction.

Abstract: Gold(I) complex with mixed ligands as an anticancer agent. The gold(I) ion is coordinated to a dithiocarbamate ligand and a phosphorus-containing ligand (e.g. phosphines). Also described are a pharmaceutical composition incorporating the gold(I) complex, a methods of synthesizing the gold(I) complex, and a method for treating cancer.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: The present invention relates to improved processes for the preparation of ruthenium or osmium complexes comprising P and N donor ligands, in particular, ruthenium complexes.

Abstract: Tetradentate ligand based on strapped phenenthradine-imidazole (SIP) based Pt or Pd complexes useful as emitters in PHOLEDs is disclosed.

Abstract: A method of enhancing the growth of an animal, as well as treating or preventing antimicrobial infections is provided. The method includes causing the animal to ingest or absorb an effective amount of one or more Fe III complex compounds, including but not limited to Fe III complexes comprising ligands bound to the iron center such as amino acids or ?-hydroxy acids. The compounds are also useful for inhibiting, reducing, or preventing biofilm formation or buildup on a surface; the treatment of, inhibition of growth of, and inhibition of colonization by, bacteria, both in biological and non-biological environments; disinfecting surfaces, potentiating the effects of antibiotics and other anti-microbial agents, and increasing the sensitivity of bacteria and other microorganisms, to anti-microbial agents are also provided.

Abstract: Nickel nanoparticles can be synthesized using a variety of precursors (e.g., nickel amides [Ni(NR2)2], alkyls [NR2], and alkoxides [Ni(OR)2]).

Abstract: The present invention discloses a process for preparing high-purity raffinose from defatted wheat germ comprising the steps of percolate extraction of raffinose from defatted wheat germ, decoloration by extraction from the abstraction liquid, electrodialysis desalination, impurity removal by simulated moving bed, concentration and crystallization, with the absolute purity of raffinose as high as 98% and the recovery up to 75%. The process is not only reliable and easy to operate, but also easy to realize industrial production and control the parameters.

Abstract: A process for enabling the production of a particulate composition containing crystalline trehalose dihydrate is provided. Including allowing an ?-glycosyltrehalose-forming enzyme to act on liquefied starch derived from a microorganism of the genus Arthrobacter and a trehalose-releasing enzyme derived from a microorganism of the genus Arthrobacter along with a starch debranching enzyme and a cyclomaltodextrin glucanotransferase; allowing glucoamylase to act on the resulting mixture to obtain a saccharide solution containing ?,?-trehalose; precipitating crystalline ?,?-trehalose dihydrate from the above saccharide solution; collecting the precipitated crystalline ?,?-trehalose dihydrate by a centrifuge; and ageing and drying the collected crystals. Cyclomaltodextrin glucanotransferase derived from a microorganism of the genus Paenibacillus or a mutant enzyme thereof is used to increase the ?,?-trehalose content in the saccharide solution to over 86.

Abstract: According to the present invention, it is possible to efficiently remove 13-dihydroepi-daunorubicin and 4?-epi-feudomycin, which are typical impurities possibly contained in 4?-epi-daunorubicin as a starting material, by using an organic acid salt of 4?-epi-daunorubicin or a hydrate or solvate thereof as a novel production intermediate, thus making it possible to produce high-purity epirubicin.

Abstract: Provided are an L-proline complex of a sodium-glucose cotransporter 2 inhibitor, and a monohydrate and a crystal of the L-proline complex. Specifically, provided are 1,6-dehydrated-1-C{4-chloro-3-[(3-fluoro-4-ethoxyphenyl)methyl]phenyl}-5-C-(hydroxymethyl)-?-L-idopyranose L-proline (a compound of formula (I)), a monohydrate and a type A crystal thereof, and a preparation method therefor. The obtained type A crystal of the compound of formula (I) has good chemical stability and crystal stability, and the crystallization solvent used has low toxicity and low residue, so the type A crystal can be better used in clinical treatment.

Abstract: Phosphoramidate esters and related nucleotide analogs useful in polynucleotide sequencing techniques, and synthetic methods for preparing those compounds, are disclosed, including compounds having the following structure: wherein R1, R2, R3 and R4 are as defined herein.

Abstract: The present invention provides methods, compositions, mixtures and kits utilizing deoxynucleoside triphosphates comprising a 3?-O position capped by a group comprising methylenedisulfide as a cleavable protecting group and a detectable label reversibly connected to the nucleobase of said deoxynucleoside. Such compounds provide new possibilities for future sequencing technologies, including but not limited to Sequencing by Synthesis.

Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.

Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.

Abstract: The present invention provides a family of dark quenchers, termed Black Hole Quenchers (“BHQs”), that are efficient quenchers of excited state energy but which are themselves substantially non-fluorescent. Also provided are methods of using the BHQs, probes incorporating the BHQs and methods of using the probes.

Abstract: The invention relates to compounds of formula (I) and related methods, wherein R1, R2, Y, R4 and R5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids with pharmacological activity. The invention futher provides intermediated in the systhesis of obeticholic acid and its analogues. The invention also provides methods related to the synthesizing of these intermediates and methods of preparing obeticholic acid and obeticholic acid analogues from the compound of the invention.

Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

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: Aspects of the present application relates to co-crystal of carfilzomib with maleic acid, process for the preparation of co-crystal of carfilzomib with maleic acid, process for the preparation of pure carfilzomib from co-crystal of carfilzomib with maleic acid and process for the preparation of amorphous carfilzomib.

Abstract: The present invention relates to an antibacterial and fungicidal peptide in which a lysine and tryptophan dipeptide is repeated. More specifically, the antibacterial and fungicidal peptide of the present invention, in which lysine and tryptophan dipeptide is repeated four times, shows excellent antibacterial activities with respect to gram-positive bacteria, gram-negative bacteria and antibiotic-resistant strains by affecting the inner membrane of harmful microorganisms, has remarkable fungicidal activities with respect to pathogenic fungi and antibiotic-resistant fungi, and shows little cytotoxicity, and thus can be useful for a pharmaceutical composition, a cosmetic composition, agricultural chemicals, a food preservative, a cosmetic preservative, and a pharmaceutical preservative.

Abstract: Short tri- and tetrapeptides according to the following Formula I Ar(CH2)mX1—X2—CO—X3—X4—X5-(Trp)n-NX6R are potent, selective agonists of melanocortin 1 receptor (MC1R). Provided herein are pharmaceutical compositions including Formula I peptide agonists of MC1R and methods of treating skin diseases and disorders that include administering to an individual in need thereof a therapeutic amount of a Formula I peptide. The peptides, pharmaceutical compositions, and methods described herein are useful in the treatment of diseases and disorders that benefit from agonism of MC1R, including melanoma, basal cell carcinoma, squamous cell carcinoma, porphyria, polymorphous light eruption, vitiligo, and solar urticaria.

Abstract: The present invention described herein relates to the composition that interact with molecules that suppress the immune system.

Abstract: The present disclosure provides agents capable of promoting endogenous steroid production (such as endogenous testosterone production) without altering the endogenous luteinizing hormone. The present disclosure also provides associated therapeutic methods as well as screening assays for identifying further therapeutic agents for the prevention, treatment and/or alleviations of symptoms associated with hypogonadism.

Abstract: Compounds and methods for imaging and/or assessing collagen are described. The compounds can include collagen binding peptides.