Abstract: A delivery system using materials that form a liquogel or nanocarrier are described. The delivery system comprises hyperbranched polyglycerols (HPGs). The delivery system can include a drug or therapeutic agent and this system can be used to administer the drug or therapeutic agent locally. The delivery system provides for controlled release of the drug or therapeutic agent.

Abstract: The technology described herein is directed to methods and compositions for inhibition of ClbP and the treatment and/or prevention of cancer, e.g., colorectal cancer, a urinary tract cancer, a squamous cell carcinoma, an oral squamous cell carcinoma, or a head-and-neck cancer.

Abstract: Disclosed are methods of treating cancers and enhancing efficacy of T cell redirecting therapeutics.

Abstract: A multifunctional immunity-targeted micromolecule anti-cancer medicine Citrate Bestazomib and preparation method and application thereof. The structure of the multifunctional immunity-targeted micromolecule anti-cancer medicine Bestazomib Citrate is shown as follows: The multifunctional immunity-targeted micromolecule anti-cancer medicine Citrate Bestazomib has an activity-inhibiting effect on APN/CD13, also has an activity-inhibiting effect on tumor proteasome, and can be applied to the development of medicines for treating malignant tumors.

Abstract: A solid dispersion of amorphous efinaconazole and a method for preparing the same are proposed. The solid dispersion includes an amorphous form of efinaconazole and at least one stabilization carrier selected from hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), ethyl cellulose (EC), hydroxypropyl methylcellulose acetate succinate (HPMC-AS), polyvinylpyrrolidone (PVP), polyacrylic acid (PAA), saccharin, and malonic acid. The solid dispersion undergoes minimal thermodynamic deformation when exposed to ambient temperature and humidity, achieving improved stability, while maintaining the inherent improved stability and bioavailability of amorphous efinaconazole.

Abstract: The present disclosure relates to ready-to-use liquid aqueous bortezomib compositions bortezomib and pharmaceutical excipients. Other aspects include methods of preparing such ready-to-use liquid aqueous bortezomib compositions, and methods of using such ready-to-use liquid bortezomib compositions in therapeutic applications.

Abstract: Disclosed include crystalline (S)-2-amino-N-((3R,5R)-8-hydroxy-6-oxo-7-oxa-1-aza-8-boraspiro[4.7]dodecan-3-yl)-3-methylbutanamide in Form D and in Form E: (3R,5R)-8-hydroxy-3-((S)-4-isopropyl-2,2-dimethyl-5-oxoimidazolidin-1-yl)-7-oxa-1-aza-8-boraspiro[4.7]dodecan-6-one or a pharmaceutically acceptable salt thereof or the crystalline Form 1 thereof: and pharmaceutical compositions and methods of using the same.

Abstract: ?-Amino boronic acid derivatives are useful for inhibiting the activity of immunoproteasome (LMP7) and for the treatment and/or prevention of medical conditions affected by immunoproteasome activity such as inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases, and cancer.

Abstract: A benzoxaborole formulation composition including a benzoxaborole, a non-ionic surfactant, or a non-ionic and ionic surfactant mixture, and a carrier is described herein. At least one of the non-ionic surfactant, the non-ionic and ionic surfactant mixture, and the carrier comprise a Lewis base or a N—H or O—H bond. The carrier is a solid or a liquid. Benzoxaborole compounds and methods of using the compounds and formulations of the compounds are described. For example, a method for reducing, preventing, ameliorating, or inhibiting an infestation by a pathogen by applying a compound or a formulation of a compound, wherein the pathogen is selected from insects, nematodes, bacteria, microbes, fungi, protozoa, viruses, and parasites, or any combinations thereof is described.

Abstract: A method to treat a patient with a Clostridium difficile infection comprising administering a therapeutically effective amount of diiodohydroxyquinoline, with or without one or more anti-infective agents.

Abstract: The invention provides novel pyridinamine-pyridone and pyrimidinamine-pyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders, autoimmune diseases and viral infections; wherein R1, R2, R3 and Z are as defined in the specification.

Abstract: The present application relates to large-scale methods of uniformly coating packaging surfaces with a benzoxaborole compound.

Abstract: The present invention relates to four crystal forms of crisaborole in free form and the preparation method thereof. The present invention also relates to the pharmaceutical composition containing the crystal forms and the use thereof.

Abstract: The present disclosure relates to ready-to-use liquid aqueous bortezomib compositions bortezomib and pharmaceutical excipients. Other aspects include methods of preparing such ready-to-use liquid aqueous bortezomib compositions, and methods of using such ready-to-use liquid bortezomib compositions in therapeutic applications.

Abstract: Disclosed are compounds for medical uses, for example, compounds of formula Ia, wherein A1, A2, A3, A4, A5, A6, A7, R6, R7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: Heterocyclic compounds are provided as arginase inhibitors, in particular to a compound represented by Formula (I), or a pharmaceutically acceptable salt, stereoisomer or tautomer, or prodrug thereof and a pharmaceutical composition including the compound.

Abstract: Compounds for use in the textile field, and more particularly the use of compounds of the 4-bora-3a,4a-diaza-s-indacene family for the manufacture of fluorescent fibers, the fluorescent compound being chosen from those of formula I: Also, processes for producing the fluorescent fibers and also to the uses thereof, notably for the provision of security to products.

Abstract: The invention relates to a method for in vitro predicting the outcome of an individual having a multiple myeloma, comprising the steps of: a. measuring the expression level of genes coding for kinases, b. calculating a score value for each genes; and c. classifying the individual as having a good or a bad outcome.

Abstract: Disclosed herein are methods of treating a subject having a cancer characterized by a modification at biomarker 1q21, which comprises administering to the subject a therapeutically effective amount of an anti-CD46 antibody.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: Useful chiral specific boron-containing compounds, such as boronate, boronate esters, boranamines, borane diamines, boranamine thioesters, and boronic mono/di-thioesters, have been prepared. These compounds and compositions containing them are useful as anti-cancer or anti-amyloidosis agents.

Abstract: The disclosure relates to the field of pharmaceutical technology, in particular, to a compound pharmaceutical composition for treating skin inflammatory diseases, which is characterized in that an active ingredient of the compound pharmaceutical of the disclosure is composed of tofacitinib and crisaborole, and the composition has a stronger therapeutic effect and a lower dosage with a significant synergistic therapeutic effect. The pharmaceutical composition of the disclosure can be used to treat skin inflammatory diseases.

Abstract: ?-amino boronic acid derivatives are useful for inhibiting the activity of immunoproteasome (LMP7) and for the treatment and/or prevention of medical conditions affected by immunoproteasome activity such as inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.

Abstract: The present invention provides compositions and methods for treating hypertension and obstructive sleep apnea utilizing hydrogel compositions comprising drug amphiphiles with TRPM 7 antagonists for use in a subject, including use on the carotid body of a subject.

Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.

Abstract: The invention provides novel pyridinamine-pyridone and pyrimidinamine-pyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders, autoimmune diseases and viral infections; (I) wherein R1, R2, R3 and Z are as defined in the specification.

Abstract: The present invention relates to methods for identifying candidate therapeutics for a disease caused by a viral envelope protein. In particular, the method can include contacting a test envelope protein with the candidate and determining its activity.

Abstract: Disclosed are compounds for medical uses, for example, compounds of formula (Ia), wherein A1, A2, A3, A4, A5, A6, A7, R6, R7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: Provided herein are compounds, such as a compound of Formula (I), as described herein, or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: Provided are a substituted oxadiazole chemical compound and composition containing said chemical compound and use thereof; said substituted oxadiazole chemical compound is the oxadiazole chemical compound as represented by formula (I), or its crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvent compound. The disclosed substituted oxadiazole chemical compound and composition containing said chemical compound are capable of inhibiting indoleamine 2,3-dioxygenase; it also has better pharmacokinetic parameter attributes and is capable of improving the drug concentration of the chemical compound in an animal body, thus improving the therapeutic efficacy and safety of the drug.

Abstract: The present disclosure relates to methods for predicting and/or determining responsiveness to an activator of JNK kinase activity. The present disclosure further relates to improved methods for treating a cancer patient with an activator of JNK kinase activity. The present disclosure also relates to methods for screening for a modulator of XBP1s protein phosphorylation.

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: Provided is a novel compound that has an excellent ?-lactamase inhibitory effect. More specifically, provided is a compound represented by formula (1a), (1b) or (11) having an excellent ?-lactamase inhibitory effect or a pharmaceutically acceptable salt thereof. By using this compound either in combination with a ?-lactam drug or alone, a useful preventive or therapeutic agent for bacterial infections is provided. Also provided are useful preventive or therapeutic agents for treating various diseases with the combined use of the aforesaid compound and ?-lactam drugs.

Abstract: The present disclosure relates to boronic derivatives of hydroxamate compounds, methods for making the same, methods for use as a monotherapy or in combination with one or more other therapeutic agents, for treatment of proliferative diseases such as cancer. The present disclosure also teaches the utilization of said boronic derivatives of hydroxamates as epigenetic therapy medications with enhanced bioavailability, lower-toxicity, and longer-lasting efficacy.

Abstract: Provided herein are free base crystalline forms and crystalline salts of Compound 1.

Abstract: Method of treating or ameliorating a bacterial infection comprising administering a composition comprising a cyclic boronic acid ester compound in combination with a carbapenem antibacterial agent such as Biapenem, and the pharmacokinetics studies thereof are provided.

Abstract: A method is disclosed for altering the redox equilibrium of a transmembrane receptor-like protein tyrosine phosphatase (RPTP), particularly a type IIa RPTP, by chemically modulating the activity through contact of such an enzyme with a diaryl boron compound that preferentially reacts with an RPTP in an oxidized state (CyS-OH). This redox modulation is most readily observed and put to use by assaying the inhibition of the phosphatase activity of the RPTP. Such an assay can be carried out on an enzyme in vitro or by contacting the enzyme in a living organism (in vivo). A useful diaryl boron compound corresponds in structure to Formula I in which Ar-1, Ar-2, R1, R2, R3 and R4 are defined within. A pharmaceutical composition containing a useful diaryl boron compound is also disclosed, as are particularly preferred diaryl boron compounds.

Abstract: The present invention is directed to a combination therapy involving a selective Bcl-2 inhibitor and a MEK inhibitor for the treatment of a patient in need of such a therapy. The patient in need of the combination therapy is suffering from cancer, such as acute myeloid leukemia.

Abstract: The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.

Abstract: The present invention relates to a method for preparing a four-coordinated organic boron compound, and more specifically, to a method for preparing various and widespread four-coordinated organic boron compounds by directly using an aryl, heteroaryl, or vinyl-functional boronic acid, boroxine, or borate compound as a starting material and adding the compound to any bidentate N,O-ligand, O,O-ligand, or N,N-ligand.

Abstract: Compositions and methods for enriching glycocompounds are disclosed which can comprise a glycocompound bound to a boronic acid compound which can be conjugated to a dendrimer.

Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: The present invention relates to a method for skin-whitening using a composition containing resveratryl triglycolate as an active ingredient, and more specifically, relates to a composition for skin-whitening containing resveratryl triglycolate or a cosmetically or pharmaceutically acceptable salt thereof as an active ingredient, a method for skin-whitening including applying or administering a composition containing resveratryl triglycolate or an acceptable salt thereof as an active ingredient to a subject, and a resveratryl triglycolate compound which has a skin-whitening effect, since the resveratryl triglycolate can inhibit melanin synthesis and brighten skin tone.

Abstract: What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.

Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.

Abstract: Disclosed are functionalized aminobenzoboroxoles compounds, method for preparing these compounds, and methods for treating cancers.

Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.

Abstract: Disclosed herein are antimicrobial compounds having the structure of the formula III? pharmaceutical compositions, the use and preparation thereof. The compounds are of the class of boronic acid derivatives, useful for antimicrobial treatment.

Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.