Abstract: Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection. The compositions may be administered intact, or may be crushed prior to administration.

Abstract: A N?-(2-naphthoyloxy)-2-(benzo[d]oxazol-2-yl)acetimidamide compound, its synthesis, and its use as an anti-microbial agent.

Abstract: Synthesis of a compound 1,3-bis(naphthalen-1-yloxy)propan-2-one and its use as an insecticidal agent.

Abstract: A method for treating a viral infection of a mammalian subject that comprises administering a virus-inhibiting amount of a halogenated xanthene, a pharmaceutically acceptable salt, an alkyl ester or amide or aromatic ester or amide derivative thereof as disclosed within, to that mammalian subject. A method of inducing a type I interferon response in a mammalian subject that presents with a microbial infection, cancerous tumor or hematological malignancy that comprises administering an amount of a halogenated xanthene as discussed above, effective to induce the type I interferon response. A method of enhancing a mammalian immunogen-specific immune response that comprises contacting mammalian cells, in vivo or present in a mammalian cell growth supporting medium, with an adjuvant-effective amount of a halogenated xanthene as discussed above, and an immunogen to which that response is to be enhanced.

Abstract: This invention relates to novel compounds according to Formula (I) which are antagonists of MrgX2, to pharmaceutical compositions containing them, and to their use in therapy for the treatment of MrgX2-mediated diseases and disorders.

Abstract: Compositions comprising an active oxygen-responsive antioxidant crystal, methods of making them, and methods for controlling the dissolution rate and/or altering the crystallization behavior of an antioxidant are disclosed. The crystals comprise an antioxidant and a disulfide- or diselenide-crosslinked polymer that is adsorbed onto a surface of the antioxidant. Upon exposure to an active-oxygen stimulus, the polymer de-crosslinks to release the antioxidant from the composition in an amount effective to counteract the stimulus. While prior approaches to altering dissolution rates have relied on passive zero- or first-order kinetics that are independent of ROS levels, the inventive compositions actively respond by releasing antioxidant in an amount proportional to the concentration of active-oxygen species present. The crystallization methods are simple and scalable.

Abstract: The present invention relates to a process for the preparation of crystalline Bortezomib of formula (I) and its pharmaceutical acceptable salts thereof. The present invention relates to a process for the preparation of highly pure crystalline Bortezomib (I).

Abstract: Systems, compositions, and methods are disclosed for developing and delivering therapeutically effective 14,15-epoxyeicosatrienoic acid (14,15-EET) analogs, for example for pain management or treatment. Of particular interest are intermediate salts.

Abstract: A method of inducing a Type I interferon response in a mammalian subject that presents with a microbial infection, cancerous tumor or hematological malignancy that comprises administering an amount of a halogenated xanthene as discussed above, effective to induce the Type I interferon response. A method of enhancing a mammalian immunogen-specific immune response that comprises contacting mammalian cells, in vivo or present in a mammalian cell growth supporting medium, with an adjuvant-effective amount of a halogenated xanthene, and an immunogen to which that response is to be enhanced. A mammalian HX compound-adjuvanted vaccine composition that contains an immunogen present in a vaccine-effective amount along with an adjuvant-effective amount of a halogenated xanthene (HX) compound and one or more excipients present at about 0.001% by weight to 10% by weight of the vaccine composition dissolved or dispersed in a pharmaceutically acceptable diluent.

Abstract: A 3,3?-(piperazine-1,4-diyl)bis(1-(naphthalen-2-yloxy)propan-2-ol) compound, its synthesis, and its use as an insecticidal agent.

Abstract: The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.

Abstract: The present application relates to compositions comprising vitamins and/or minerals and a polyphenolic matrix having increased stability and bioavailability. The polyphenolic matrix may comprise a polyphenolic extract, an emulsifier and a binder. The polyphenolic extract may be a fruit peel extract. The present application further relates to uses and methods using the compositions of the application.

Abstract: Provided herein are combinations comprising difluoromethylornithine (DFMO), or an ionic form thereof, and a compound of the following structural formula: or a protonated form thereof, wherein values for the variables (e.g., a, b, c, d, e, n, R1, R2, X) are described herein. The combinations can provide combination drug therapy in a single pharmaceutical dosage form, and be used, for example, for the treatment of cancer.

Abstract: Provided herein are polymorphs of (2E)-3-fluoro-2-({[2-(4-methoxypiperidin-1-yl)pyrimidin-5-yl]oxy}methyl)prop-2-en-1-aminium 4-methylbenzenesulfonate, compositions thereof, methods of preparation thereof, and methods of use thereof.

Abstract: The invention relates to crystalline forms of Alpha-1062 gluconate. In one aspect, the invention relates to a crystalline solid form of Alpha-1062 gluconate (Form A), wherein said crystalline form has prominent peaks at 3.61, 10.98, 14.41 and 18.44 degrees 2-theta (±0.2) in a powder X-ray diffraction pattern. The invention further relates to methods for manufacturing crystalline forms and compositions comprising said crystalline forms.

Abstract: Described herein are PHD inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of anemia.

Abstract: The present invention provides novel methods of using nitric oxide donor compounds for treating infectious diseases, for example, COVID-19.

Abstract: The present invention relates to the technical field of disease treatment, and more specifically, it relates to a pharmaceutical composition, having arginine metabolite dimethylguanidino valeric acid (DMGV) or plant flavonoids to treat chronic inflammatory and cancers. Disclosed in the present invention are plant flavonoids including kaempferol, daidzein, and quercetin. Treated chronic inflammatory diseases include rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and cancer further including hematological cancers as well as solid tumor.

Abstract: The present technology is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods. Diseases and conditions that can be treated with the compounds and compositions of the present technology include, but are not limited to, antibacterial infection, antiviral infection, cancer and neurodegenerative disorders susceptible to treatment by modulation of p97.

Abstract: Disclosed are means of stimulating systemic immunity and reduction of post-surgery tumor metastasis through the concurrent intralymphatic inhibition of NR2F6 and treatment with cannabidiol. In some embodiments NR2F6 is inhibited by high pressure transient delivery of short interfering RNA into tumor draining lymph nodes concurrent with systemic administration of cannabidiol. This combination may be performed together with means that induce immunogenic tumor cell death. Through the combination of immunogenic cell death and immune stimulation, the invention provides a means of enhancing the abscopal effect and in some embodiments to cause immunological mediated destruction primary and secondary neoplasia.