Abstract: A method of treating prostate cancer in a patient comprising administering to the patient a pharmaceutical composition including a first therapeutic including a TLK1B inhibitor, or a pharmaceutically acceptable salt, solvate, ester, amide, clathrate, stereoisomer, enantiomer, prodrug or analog thereof, and a second therapeutic including an antiandrogen or a pharmaceutically acceptable salt, solvate, ester, amide, clathrate, stereoisomer, enantiomer, prodrug or analog thereof.

Abstract: Described herein are crystalline forms of (R)-3-(2-(trans-4-(2-aminoethylamino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylic acid. In some embodiments, the crystalline forms are formulated for treating a subject in need thereof with a bacterial infection.

Abstract: Described herein are compounds of the formulae (I)-(III) and (Ia)-(IIIa) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods using compounds of the formulae (I)-(III) and (Ia)-(IIIa) to, among other things, treat cancer.

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.

Abstract: An object of the invention is to provide a photoelectric conversion element exhibiting an excellent production suitability. Also, the other object of the invention is to provide an optical sensor and an imaging element comprising the photoelectric conversion element. The photoelectric conversion element of the invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1) below.

Abstract: Compounds, compositions and methods are provided for the inhibition of GBP1. The subject inhibitor compounds can act by inhibiting GBP1 alone and/or GBP1: pro-survival kinase (e.g. serine/threonine-protein kinase pim-1 (PIM1)) interactions. Aspects of the subject methods include contacting a cellular sample with a GBP 1 inhibitor to inhibit the GBP 1 alone and/or GBP 1: PIM 1 interactions. Also provided are compositions and methods for treating cancer. In certain cases the cancer is resistant towards chemotherapy and radiation therapy.

Abstract: Provided is a bismaleimide compound having a favorable compatibility with other resins and contributing to a higher Tg. The compound is represented by the following formula wherein A independently represents a tetravalent organic group having a cyclic structure, B independently represents a divalent hydrocarbon group having 6 to 200 carbon atoms, Q independently represents a cyclohexane backbone-containing divalent alicyclic hydrocarbon group having 6 to 60 carbon atoms, W represents B or Q, n represents 1 to 100, m represents 0 to 100, repeating units identified by n and m whose bonding pattern may be alternate, block or random are present in any order, and wherein Q is independently represented by the following formula (2): wherein each of R1, R2, R3 and R4 independently represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, each of x1 and x2 represents a number of 0 to 4.

Abstract: A hypergolic co-crystal material for producing a hypergol when combined with an oxidizer; it has co-crystals composed at least of a hypergolic trigger component and an energetic coformer.

Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

Abstract: The present disclosure provides pharmaceutical combinations of orally administered irinotecan and a P-gp inhibitor. The pharmaceutical combinations are suitable for the treatment of cancer in a subject and for reducing or preventing toxicity, hypersensitivity-type infusion reactions, and other negative outcomes resulting from or associated with intravenously administered irinotecan (e.g., Camptosar®) therapy in a subject suffering from cancer.

Abstract: A process for forming 2-hydroxypyridine-1-oxide or derivatives thereof, the process comprising inter alia providing a solution comprising at least one compound according to Formula (1) and recovering a compound according to Formula (2) Also related products, uses, methods and compositions.

Abstract: The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2?. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The present invention relates to a derivative of 13-oxidized ingenol, use thereof in the prevention and/or treatment of a disease associated with proliferation or tumor in a subject, or a cosmetic indication, and use thereof in the prevention and/or treatment of a disease responsive to neutrophil oxidative burst, a disease responsive to a release of IL-8 by keratinocyte, or a disease responsive to induction of necrosis.

Abstract: The present disclosure relates to new therapeutic uses of MPO inhibitors and methods of treatment involving the same.

Abstract: K13-propeller polymorphism is a useful molecular marker for tracking the emergence and spread of ART-resistant P. falciparum. The invention encompasses methods, compositions, and kits for detecting and genotyping Plasmodium, for example, Plasmodium falciparum. The methods, compositions, and kits can be used to detect the presence or absence of a mutated K-13 propeller nucleic acid or protein in the sample.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating solid cancer and blood cancers such as acute leukemia and chronic leukemia, comprising a derivative compound of 1,2-naphthoquinone or a pharmaceutically acceptable salt thereof as an effective component. The derivative compound of 1,2-naphthoquinone is highly effective in killing cancer cells of various solid cancers, acute leukemia, and chronic leukemia, and thus can be beneficially used as a pharmaceutical composition for preventing or treating cancers, especially solid cancers, acute leukemia, and chronic leukemia.

Abstract: A method for producing a cyclic carbonate represented by the following formula (1): wherein X1 and X2 are the same as or different from each other, and are each a hydrogen atom, a fluorine atom, or a monovalent organic group; and R is an organic group containing one or more carbon-carbon unsaturated bonds. The method includes reacting an unsaturated cyclic carbonate represented by the following formula (A): wherein X1 and X2 are defined as described above, and an alcohol represented by the formula (B): R—OH, wherein R is defined as described above, or an alkoxide thereof in the presence of a base, or reacting the unsaturated cyclic carbonate and the alkoxide. Also disclosed is a method for producing a cyclic carbonate.

Abstract: An N-benzenesulfonylbenzamide compound represented by the formula (I), or a crystal form, a prodrug, pharmaceutically acceptable salts, a stereoisomer, a solvate or a hydrate thereof, a pharmaceutical composition containing same, and a use thereof as a Bcl-2 protein inhibitor for preparing a medicament for treatment of leukemia or a cancer.

Abstract: The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

Abstract: The invention relates to functionalized quinazoline compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as heparanase inhibitors for the treatment of diseases or conditions related to heparanse activity.