Abstract: The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.

Abstract: The embodiments relate to improved vitamin supplement compositions formulated for administration to patients, particularly improved vitamin compositions formulated for use in cosmetic or therapeutic applications. The compositions may be used to slow aging process and promote wellness including treating a vitamin deficiency, skin conditions, improving skin appearance, wound healing and scar prevention and hair loss.

Abstract: The embodiments of present invention provide processes and an intermediate for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms, such as tablets, made by these processes. Additionally, embodiments of the present invention provide tablets including 25 mg, 50 mg, 100 mg, or 200 mg free base equivalent of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide hemisuccinate.

Abstract: Provided are crystal forms A, B, C and D of a compound of formula (I), and application of the crystal forms in the preparation of drugs for treating ASK1-related diseases.

Abstract: This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.

Abstract: This application describes methods of inhibiting APOL1 and treating APOL1-mediated kidney diseases comprising administering Compound I and/or a pharmaceutically acceptable salt thereof. The application also describes pharmaceutical compositions comprising Compound I and/or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of formula (I?), wherein A, R1, R2, T1, T2, T3, T4, L, W, Z, R??, m and n have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Abstract: Disclosed herein are compounds of Formula I?: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.

Abstract: Provided herein are processes for purifying TCH in a feed stream, such as an adiponitrile process stream. The processes include a first separating step of separating the adiponitrile process stream to form a first overhead stream comprising low-boiling components and high-boiling components and a first bottoms stream comprising high-boiling components. The processes also include a second separating step of separating the first overhead stream in one or more distillation columns to form a lights stream comprising low-boiling components, a heavies stream comprising high-boiling components, and a TCH stream.

Abstract: Disclosed are alkynyl (hetero) aromatic ring compounds that inhibit protein tyrosine kinases, pharmaceutical compositions comprising same, preparations therefor and uses thereof. Specifically, disclosed are an alkynyl (hetero) aromatic ring compound represented by formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotope variant thereof. The disclosed compounds may be used in the treatment and/or prevention of diseases associated with protein tyrosine kinase, such as in preventing tumors.

Abstract: Methods for treating or preventing kidney diseases and fibrosis, such as chronic kidney disease (CKD), kidney fibrosis, heart fibrosis, uterine fibrosis, and cystic fibrosis, with compounds of Formulae (I), (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof.

Abstract: HM30181 (shown below) can be used to improve absorption of cancer chemotherapy drugs, such as paclitaxel. Herein are described various polymorphisms of HM30181, in particular polymorphism C, as well as their physical properties and methods for their preparation and characterization.

Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.

Abstract: Provided herein are materials that can achieve up to 14% hydrogen absorption by weight in ambient conditions, which is a marked improvement over the hydrogen absorption values found in the prior art. Further provided are experimental conditions necessary to produce these materials. In order to produce the hydrogen storage material, a transition metal (or Lithium) is vaporized in a pi bond gas in conditions that permit only a few bonding collisions to occur between the vaporized transition metal atoms and pi bond gas molecules before the resulting bonded material is collected.

Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.

Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.

Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.

Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.

Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aryl; R3-R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.

Abstract: The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form.