Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat diseases, such as cancer.

Abstract: Indazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: The present invention provides compounds that modulate biological metals and to pharmaceutical compositions containing such compounds. The invention particularly relates to imidazo[1,5-a]pyridine compounds that modulate iron and are useful for the treatment of diseases, particularly neurological diseases such as Parkinson's disease (PD), Alzheimer's disease (AD), Alzheimer-type dementia, Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), frontotemporal dementia (FTD) and multiple system atrophy (MSA).

Abstract: A crystalline form of an avibactam derivative, pharmaceutical compositions thereof, and the use of the crystalline avibactam derivative for treating bacterial infections are provided.

Abstract: Provided herein are spirocyclic and fused bicyclic carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

Abstract: Disclosed herein are methods and compounds of augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, the compounds disclosed herein are ENPP-1 inhibitors, pharmaceutical compositions, and methods for the treatment of cancer or a viral infection.

Abstract: The present invention provides the compound represented by the following formula (I): wherein a moiety represented by formula: or the like. The symbols are defined in the specification. The compounds of the present invention have MGAT2 inhibitory activity, and are useful as a medicine for treatment of MGAT2-associated diseases including obesity, metabolic syndrome, hyperlipidemia, hypertriglyceridemia, hyper-VLDL-triglyceridemia, hyperfattyacidemia, diabetes mellitus, and arteriosclerosis.

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, Y3, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

Abstract: Compounds having a structure according to formula (I) where R1, R2, and R3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Abstract: This invention relates to carbapenem compounds, their stereoisomers, pharmaceutically acceptable salts or N-oxides thereof, which may be useful for the treatment of bacterial infections, particularly drug-resistant bacterial infections, as well as the processes for the preparation of compounds, the pharmaceutical compositions of these compounds and their use in the treatment of bacterial infection.

Abstract: Disclosed herein, inter alia, are compositions and methods for treating parasitic diseases.

Abstract: A crystal form of PARP-1 inhibitor and a preparation method therefor are described. Specifically, a crystal form A of 4-[[3-[[2-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-?]pyrazine-7-yl]carbonyl]-4-fluorophenyl]methyl-1(2H)-phthalazinone (formula I) and a preparation method therefor are described.

Abstract: The invention provides new pyrimidine compounds having the general formula (I), wherein R1, R2, R3, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Abstract: The present invention relates to compounds of formula I wherein L is a bond, a triple bond, —C(O)NH— or —NHC(O)—; R1 is phenyl or a five or six-membered heteroaryl group, optionally substituted by lower alkyl, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R2 is fluoro; R3 is fluoro or chloro; R4 is hydrogen, lower alkyl, halogen, lower alkyl substituted by hydroxy, S(O)2CH3, or is a five or six-membered heteroaryl group or a heterocycloalkyl group, which are optionally substituted by lower alkyl, hydroxy or ?O; R5 and R6 are both methyl and the dotted line is a bond, or R5 and R6 are both methyl and the dotted line is nothing, or one of R5 and R6 is hydrogen and the other is methyl, and the dotted line is nothing; or to a pharmaceutically acceptable salt or acid addition salt, to all possible tautomeric forms, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

Abstract: The present invention relates to a compound of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, —CH2—C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n=2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

Abstract: Solid forms of the compound, 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine, and solid forms of salts or co-crystals of Compound I, were prepared and characterized: Also provided are processes of making the solid forms and methods of use thereof.

Abstract: The present disclosure may disclose a new crystal form D of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one ((1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl) methanesulfonic acid salt, preparation method therefor and a medicinal use. Compared to the existing crystalline forms, this new crystalline form has clear advantages with respect to solubility, stability, and the preparation process.

Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R9, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The invention relates to novel heteroaryl compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.

Abstract: The present application relates to a macrocycle containing aminopyrazole and pyrimidine, which is represented by formula (1), a pharmaceutical composition thereof, and a use thereof in inhibiting tropornyosin receptor kinase (Trk) activity and in treating diseases in mammals that are mediated by Trk.

Abstract: The invention relates to novel compounds of the formula (I) in which Aa, Ab, R1, R2, R3, R4, R5 and n have the meanings mentioned above, to the use thereof as acaricides and/or insecticides for controlling animal pests and to methods and intermediates for the preparation thereof.

Abstract: A sensor and a method of using the sensor are disclosed. The sensor includes a conductive region in electrical communication with two electrodes, the conductive region including single-walled carbon nanotubes, nanosized particles of a metal dichalcogenide, and a mercaptoimidazolyl metal-ligand complex. The sensor can be used to detect volatile compounds that have a double or triple bond.

Abstract: A method for enhancing the conductivity of MOF-5 by the development of an MOF-5 polymer composite material. The composite material incorporates a conductive polymer, preferably polyaniline, in the solvo-thermal synthesis pathway of MOF-5. The electrically conductive MOF-5 composite exhibits electric conductivity three orders of magnitude higher than that of MOF-5 while maintaining the crystallinity, robustness, and thermal stability of MOF-5.

Abstract: The present invention provides a preparation method for zeolitic imidazolate frameworks. The preparation method comprises: adding a metal carbonate or oxide, an organic ligand to a hydrophilic liquid to obtain a mixture; introducing an acidic gas to reach a reaction pressure of 0.1 MPa to 2.0 MPa, and reacting for a predetermined time; heating to 30° C.-60° C. and vacuuming to obtain the zeolitic imidazolate framework. The present invention also provides a zeolitic imidazolate framework obtained by the above preparation method. The preparation method according to the present invention is environmentally friendly and has a high yield.

Abstract: Described herein are complexes comprising a cationic antibacterial agent and a metal salt; oral care compositions comprising same; along with methods of making and using these complexes and compositions.

Abstract: A method for the production of phosphoethanolamine is disclosed. Phosphoric acid and monoethanolamine are mixed at a sufficient ratio using a doser to form a solution. The solution is then esterified by heating the solution to about 200° C., followed by cooling the solution to 40° C. A sufficient amount of distilled water is added to the solution to produce the desired viscosity. Excess ethanol is then filtered from the solution via a suction element. The solution is then subjected to centrifugal action for up to four hours at 1800 RPM to separate the phosphoethanolamine until a moisture content below 20% is reached. The remainder is then air dried to further isolate the phosphoethanolamine.

Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: R1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.

Abstract: Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.

Abstract: Disclosed are to metallocyclopropene complexes, methods of making same, methods for ring expansion metathesis polymerization, and polymers prepared by the methods for ring expansion metathesis polymerization.

Abstract: Disclosed are compounds, compositions, and methods useful for the oxygen reduction reaction (ORR) and capable of operating efficiently at low overpotentials.

Abstract: A sensor compound and sensor composition comprising the sensor compound are disclosed. The sensor compound includes a metal atom and a mercaptoimidazolyl multidentate ligand. The sensor composition comprises the sensor compound and a metal dichalcogenide.

Abstract: The present invention provides purified compounds extracted from seaweeds having the formula (I): wherein R1 and R2 is each independently H or a fatty acid and their use for inhibiting the growth of cancer cells.

Abstract: Methods of preparing nicotinamide riboside and derivatives thereof.

Abstract: The present invention relates to the field of stereodefined phosphorothioate oligonucleotidess and to nucleoside monomers and methods of synthesis thereof. Herein are disclosed acyl protected L-LNA-G monomers which have improved solubility and stability characteristics, and result in improved efficacy in oligonucleotide synthesis.

Abstract: The present invention is related to a method for the preparation of a modified nucleic acid molecule comprising a nucleic acid moiety and a non-nucleic acid moiety by reacting a first reactant and a second reactant, wherein the first reactant comprises the non-nucleic acid moiety and a carboxyl group, and wherein the second reactant is an amino-modified nucleic acid molecule comprising the nucleic acid moiety and an amino modification comprising an amino group which is attached to the nucleic acid moiety, wherein the method comprises the following steps: a) activating the first reactant, preferably the carboxyl group of the first reactant, by a condensation reagent in a water miscible organic solvent, and b) reacting the activated first reactant, preferably the activated carboxyl group of the first reactant, of step a) and the second reactant, preferably the amino group of the amino modification of the amino-modified nucleic acid molecule which has been dissolved in water or a mixture of a water miscible orga

Abstract: The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

Abstract: Provided herein is a deuterated compound of Formula (I) Formula (I) or a pharmaceutically acceptable salt thereof, wherein R3a, R5, R6a, R6b, R17, R21a, R21b, Rm, Rn, R16a, R16b, R7a, R7b, R12a, R12b, R11a, R11b, R2a, R2b, R19, R4a, and R4b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Abstract: The present invention provides, in certain aspects, novel 7-dehydrocholesterol (7DHC) derivatives that are useful in treating or preventing cancer, as well as in treating or preventing uncontrolled angiogenesis, in a subject. In certain embodiments of the present invention, the subject is a human. In other aspects, the present invention provides a method of preparing compounds of the invention, or a salt or solvate thereof.

Abstract: A method for producing a peptide by conducting steps (1) condensing an N-protected amino acid or an N-protected peptide to an N-terminus of a C-protected amino acid or a C-protected peptide represented by formula (II): wherein Y represents an amino acid or a peptide with an unprotected N-terminus; R1, R2 and R3 each independently represent an optionally substituted aliphatic hydrocarbon group, an optionally substituted aromatic hydrocarbon group, or —OR4 (wherein R4 represents an optionally substituted aliphatic or aromatic hydrocarbon group; two of R1, R2 and R3 may form a 5- to 7-membered ring together with the Si atom to which they are bonded; and the R1R2R3Si group has 8 or more carbon atoms and is bonded to a C-terminus of an amino acid or a peptide in Y, and (2) removing the protective group at the N-terminus of the peptide obtained in step (1).

Abstract: Described herein is a method of maintaining corn protein yield during extraction, comprising obtaining a corn gluten material, washing the corn gluten material to remove non-protein components with an ethanol-water solvent comprising at least 85 wt % ethanol to obtain a corn protein concentrate product, wherein the loss of corn protein content during extraction is less than 25% of total corn protein.

Abstract: Herein is reported a method for obtaining a polypeptide in monomeric form comprising the steps of a) providing a solution comprising the polypeptide in monomeric form and in aggregated form, wherein the ratio of monomeric to aggregated form is 4:1 or less as determined by size exclusion chromatography, b) performing a mixed-mode chromatography in bind-and-elute mode, or a hydrophobic interaction chromatography in flow-through mode, or a size-exclusion chromatography, and c) performing a weak cation exchange chromatography in bind-and-elute mode or flow-through mode, and thereby obtaining the polypeptide in monomeric form.

Abstract: The present invention is directed to methods for the separation of a molecule of interest from a solution containing the molecule using dual stage tangential-flow ultrafiltration (“TFF”). In particular, the methods of the invention are directed to the processing of crude feed streams such as conditioned cell culture supernatant to dramatically reduce contaminant and/or impurity levels prior to subsequent, i.e., downstream, refining unit operations. The methods of the invention may be used in the processing of a crude feed stream from biological production systems such as fermentation or other cell culture process, and may further eliminate the need for time consuming impurity precipitation (e.g., pH driven) and/or precipitate filtration processes prior to downstream processes that are sensitive to high impurity loads such as chromatographic unit operations.

Abstract: Compositions and methods are described in which a primary detergent or surfactant in an aqueous solution is removed by the addition of a secondary detergent or surfactant in concentrations that exceed the critical micellar concentration (CMC) of the secondary detergent or surfactant. These compositions and methods are particularly applicable to protein-containing solutions. Typical primary detergents/surfactants include polysorbate 20, polysorbate 80, and Triton X-100. Suitable secondary detergents or surfactants can be ionic, nonionic, or zwitterionic. Typical secondary detergents/surfactants include, but are not limited to, galactoside detergents (e.g. octyl-?-galactoside), glucamide detergents (e.g. MEGA 8, MEGA 9, MEGA 10), cholamide detergents (e.g. CHAPS, CHAPSO, BIGCHAPS), and sulfobetaine detergents (such as sulfobetaine 3-10).

Abstract: IL-2R? ligands and IL-2R?c ligands and compounds comprising the ligands are disclosed. The ligands and compounds such as heterodimers and fusion proteins comprising the IL-2R? ligands and/or the IL-2R?c ligands can be IL-2 receptor agonists.

Abstract: IL-2R? ligands and IL-2R?c ligands and compounds comprising the ligands are disclosed. The ligands and compounds such as heterodimers and fusion proteins comprising the IL-2R? ligands and/or the IL-2R?c ligands can be IL-2 receptor agonists.