Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1 X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substitu

Abstract: The invention relates to dipeptidyl peptidase-4 inhibitors, including saxagliptin and sitagliptin, for use in the topical eye treatment and/or prevention of retinal neurodegenerative diseases, in particular diabetic retinopathy and its associated microvascular impairment. The invention also encompasses pharmaceutical topical eye compositions for use in the topical treatment and/or prevention of these diseases.

Abstract: The present invention relates generally to intranasal pharmaceutical compositions. In particular, the present invention is directed to sustained, enhanced delivery of pharmaceutical agents across the nasal mucosa for systemic drug delivery.

Abstract: Provided herein are methods for treating pancreatic cancer using a combination of radiotherapy and an agent that inhibits binding of PD-L1 to PD1 (e.g., durvalumab).

Abstract: An ethyl 3-(5-(3-fluorophenyl)-4-phenyl-4H-1,2,4-triazol-3-ylthio)propanoate compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The disclosure discloses a fatty acid synthase inhibitor and application thereof and belongs to the technical field of medical biology. The fatty acid synthase inhibitor of the disclosure can significantly inhibit the activity of fatty acid synthase without affecting normal expression, and adjust the ratio of fatty acids in cells. The fatty acid synthase inhibitor of the disclosure has a good tumor proliferation inhibitory effect, can arrest the growth cycle of tumor cells in the interphase, prevent tumor cell division, inhibit tumor cell proliferation, promote tumor cell apoptosis and exert a tumor treatment effect, can be used to treat tumors and metabolism related diseases, and has an important clinical application prospect.

Abstract: The present invention is generally directed to substantially pure cannabidiol, stable cannabinoid pharmaceutical formulations, and methods of their use.

Abstract: The present disclosure provides a method for treating hypertension by using a compound, wherein the compound is selected from the group consisting of: (E)-4-(3-(3-methyl benzyloxy)benzylidene)-1-phenylpyrazolidine-3,5-dione, (2R)-2-amino-3-(2,3-dihydro-1H-inden-1-yl)-N?-((E)-quinolin-7-ylmethylene)propane hydrazide, and a combination thereof. The present disclosure uses a small molecule compound (E)-4-(3-(3-methyl benzyloxy)benzylidene)-1-phenylpyrazolidine-3,5-dione, (2R)-2-amino-3-(2,3-dihydro-1H-inden-1-yl)-N?-((E)-quinolin-7-ylmethylene)propane hydrazide or a combination thereof, which can be developed as a therapeutic drug for lowering blood pressure, whether it is taken orally or injected.

Abstract: Compositions and methods of treating a subject for a coronavirus infection are provided. The methods typically include administering the subject an effective amount of probenecid, a metabolite or analog thereof, or a pharmaceutically acceptable salt thereof. The methods can by therapeutic and/or prophylactic. The amount of probenecid or a pharmaceutically acceptable salt thereof can be effective to, for example, reduce viral replication, reduce one or more symptoms of disease, disorder, or illness associated with virus, or a combination thereof. In preferred embodiments, the virus is a Severe acute respiratory syndrome-related coronavirus such as SARS-CoV-2 or SARS-CoV, a Middle East respiratory syndrome-related coronavirus such as MERS-CoV, or a coronavirus that causes the common cold.

Abstract: Provided is a composition for the prevention and treatment of one or more cancers selected from the group consisting of breast cancer, liver cancer, and gastric cancer, the composition comprising selenopsammaplin A as active ingredients. The selenopsammaplin A and derivatives thereof of the present invention have been confirmed to exhibit excellent anticancer activity against breast cancer, liver cancer, and gastric cancer cells, and exhibit not only a strong effect of suppressing breast cancer growth compared to existing psammaplin A but also an excellent effect of suppressing the metastasis of breast cancer cells, and thus the selenopsammaplin A and derivatives thereof are expected to be effectively usable as a pharmaceutical composition for the prevention and treatment of breast cancer, liver cancer, and/or gastric cancer, and for the suppression of breast cancer metastasis.

Abstract: The present disclosure provides methods of treating inflammation of the upper gastrointestinal tract, especially the esophagus, by administering an oral corticosteroid. In some cases, the methods include treating eosinophilic esophagitis (EoE) by administering an oral corticosteroid in an induction phase and a maintenance phase to improve peak eosinophilic counts and symptoms. In embodiments, the methods include treating EoE by administering the oral corticosteroid at nighttime and/or while the patient is lying down.

Abstract: Compositions and methods for lightening skin are provided. A method for lightening skin may include the step of identifying skin where lightening or whitening is desired and topically applying to the skin a composition including (a) a skin lightening agent comprising a canola extract and (b) a cosmetically acceptable carrier. A method for treating hyperpigmentation may include the step of identifying skin containing areas of hyperpigmentation and topically applying to the skin a composition including (a) a canola extract and (b) a cosmetically acceptable carrier.

Abstract: Provided herein are compositions, systems, and methods for treating wounds with the combination of statins and cholesterol to help prevent and reduce scar formation.

Abstract: The present disclosure provides liquid formulations comprising polypeptides and surfactants. In particular, it discloses a liquid formulation comprising a polypeptide and a surfactant, wherein at least about 70% (wt %) of the surfactant are isosorbide polyoxyethylene (POE) fatty acid esters. The invention also provides methods for making such liquid formulations, articles of manufacture comprising such liquid formulations and methods of treating a patient with such liquid formulations.

Abstract: The subject invention provides oligo(carbamoylated guanidine)s (OCGs) having fast and selective mycobactericidal effects via disruption of the mycobacterial membrane potential. OCGs also potentiates bedaquiline, an oxidative phosphorylation-targeting anti-TB drug. The combination of OCG and anti-TB drug can be used as an effective therapy for treating tuberculosis.

Abstract: Healthcare formulations, including, inventive surfactants, Active ingredient formulated as solids, liquids, or emulsions. The present disclosure provides formulations of healthcare products, such as: prescription drugs, over the counter drugs; minerals, herbal, and/or vitamin supplements; drugs administered in hospitals, clinics, physician's office, and places of palliative care; vaccines, tissue, organ, and cell transplants and/or grafts and/or infusions; and wound care formulations including topical ointments, lotions, cleaners, wipes, bandages, and dressings. The Active may be included in the formulations as a solute, a solvent, a particle, or an oil immiscible component of the formulation. The Active may be included in tablets, capsules, tinctures, liquids, or emulsions. Inventive healthcare formulations include formulations suitable for administration orally, topically, and/or by injection.

Abstract: The present invention provides diagnostic and therapeutic methods and compositions for cancer. The invention provides methods of determining whether an individual having a cancer is likely to respond to treatment comprising a pan-RAF dimer inhibitor and a MEK or PI3K inhibitor, methods of predicting responsiveness of an individual having a cancer to treatment comprising a pan-RAF dimer inhibitor and a MEK or PI3K inhibitor, methods of selecting a therapy for an individual having a cancer, and methods of treating an individual having cancer based on the presence of a biomarker of the invention (e.g., a KRAS activating mutation, e.g., a KRAS-G13D mutation, or an NRAS activating mutation).

Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.

Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.

Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.