Abstract: A process for producing ethylene oxide by gas-phase oxidation of ethylene, comprising: directing a feed comprising gaseous ethylene and gaseous oxygen through a packing of individual shaped catalyst bodies, under conditions conducive to obtain a reaction mixture containing at least 2.7 vol.-% of ethylene oxide, wherein each shaped catalyst body comprises silver deposited on a refractory support and is characterized by a content of at least 20 wt.-% of silver, relative to the total weight of the shaped catalyst body; a BET surface area in the range of 1.6 to 3.0 m2/g; a first face side surface, a second face side surface and a circumferential surface with a plurality of passageways extending from the first face side surface to the second face side surface; and a uniform multilobed cross-section; and a longest direct diffusion pathway d, with 2d being in the range of 0.7 to 2.

Abstract: Provided is a salt of an Syk inhibitor and a crystalline form thereof, and more specifically, provided are 5-fluoro-1-methyl-3-((5-(4-(oxetan-3-yl)piperazine-1)-yl)pyridin-2-yl)amino)-6-(1H-pyrazol-3-yl)quinoline-2(1H)-ketamine hydrochloride, a crystalline form thereof, a preparation method therefor, a pharmaceutical composition thereof and a use thereof. The hydrochloride of the compound represented by formula I and the crystalline form thereof have good salt-forming properties, high stability and low hygroscopicity, have advantages in terms of physical properties, safety and metabolic stability, and have value in prepared medicines.

Abstract: The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation.

Abstract: Novel pyrazolo[1,5-c]pyrido[3,4-e]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrazolo[1,5-c]pyrido[3,4-e]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Compositions for intranasal delivery of olanzapine and methods for their use to treat various symptoms of schizophrenia, schizoaffective disorder, and bipolar disorder, such as acute agitation, mania, and mixed episodes. Intranasal olanzapine compositions comprise dodecyl maltoside to improve bioavailability of olanzapine and is administered via nasal mucosa to avoid direct systemic administration.

Abstract: The discovery of mutant or fusion kinases that drive oncogenesis, and the subsequent approval of specific inhibitors for these enzymes, has been instrumental in the management of some cancers. However, acquired resistance remains a significant problem in the clinic, limiting the long-term effectiveness of most of these drugs. Herein is demonstrated a strategy to overcome this resistance through drug-induced MEK cleavage (via direct procaspase-3 activation) combined with targeted kinase inhibition. This combination effect is shown to be general across diverse tumor histologies (melanoma, lung cancer, and leukemia) and driver mutations (mutant BRAF or EGFR, fusion kinases EML4-ALK and BCR-ABL). Caspase-3-mediated degradation of MEK kinases results in sustained pathway inhibition and substantially delayed or eliminated resistance in cancer cells in a manner superior to combinations with MEK inhibitors.

Abstract: The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

Abstract: The present invention relates to a process for producing a sterile liquid pharmaceutical composition suitable for administration by inhalation comprising ensifentrine particles, wherein the process comprises: (a) heating ensifentrine particles at a temperature of from 100° C. to 220° C. to obtain sterile ensifentrine particles; and (b) combining the sterile ensifentrine particles with a sterile liquid vehicle to produce the sterile liquid pharmaceutical composition suitable for administration by inhalation. A process for producing an ampule comprising the sterile liquid pharmaceutical composition is also described.

Abstract: Provided are methods of using a MYC gene as a biomarker for predicting therapeutic efficacy of survivin inhibitors such as YM155 monobromide in cancer therapy, and related kits, compositions, and methods for diagnosing and treating cancer in a subject in need thereof.

Abstract: The present invention relates to a compound of the Formula: or a pharmaceutically acceptable salt thereof. The compound of the present invention inhibits Pol?. This novel therapeutic compound is therefore useful for the treatment and/or prevention of diseases and conditions in which Pol? activity is implicated, such as, for example but not limited to, the treatment and/or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compound defined herein, to processes for synthesising the compound and to their use for the treatment of diseases and/or conditions in which Pol? activity is implicated.

Abstract: The subject invention provides compounds as Drp1 inhibitors, compositions comprising a Drp1 inhibitor, and methods for inhibiting Drp1 protein using the Drp1 inhibitors. Further provided are methods for treating and/or preventing a disease or condition associated with mitochondrial dysfunction, oxidative stress, inflammation and/or autophagy. Advantageously, the compounds and compositions of the subject invention can also be used to treat a variety of other conditions including, for example, autoimmune disorders, disorders of the nervous system, and cardiovascular disorders.

Abstract: The present disclosure relates to a crystalline salt selected from crystalline N-ethyl-2-(5-fluoro-1H-indol-3-yl)-N-methylethan-1-amine fumarate and crystalline N-ethyl-2-(5-fluoro-1H-indol-3-yl)-N-methylethan-1-amine hydrochloride, methods of preparing them, and uses thereof for treating mood disorders. In addition, the present disclosure relates to polymorphs of the aforementioned salts.

Abstract: Disclosed are macrocyclic compounds that possess inhibitory activity against DYRK, TRK, TLK, and/or RET. Also disclosed are pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to treat diseases and disorders that are characterized or mediated by aberrant DYRK, TRK, TLK, and/or RET activity such as cancer, neurodegenerative disorders and genetic disorders.

Abstract: Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis.

Abstract: Compositions and methods for treating multiple myeloma (MM), acute myeloid lymphoma (AML) or a myeloproliferative disease (MPD) in a human patient in need thereof. The methods entail administering to the patient an effective amount of cerdulatinib.

Abstract: The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).

Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.

Abstract: In certain embodiments, this disclosure relates to KRAS agonists, pharmaceutical composition, and uses in managing cancer. In certain embodiments, the KRAS agonist is 4-(4-(2-bromoacetamido)butyl)benzoic acid, salt, prodrug, or derivative thereof. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering an effective amount of a compound of Formula I, salt, prodrug, or derivative thereof, to a subject in need thereof, wherein, substituents are reported herein.

Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a novel compound and a pharmaceutical composition for enhancing anticancer activity, which includes the same, and more particularly, to a pharmaceutical composition, which includes a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, thereby enhancing anticancer activity of an anticancer agent or radiation, and inducing proliferation inhibition and death of cancer cells, resulting in effectively treating cancer: