Abstract: The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists.

Abstract: A 6-(6-bromo-2-oxo-2H-chromen-3-yl)-4-(4-chlorophenyl)-2-alkoxynicotinonitrile compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The present invention relates to the technical field of photosensitizers, and particularly to a near-infrared nano-photosensitizer and a preparation method and use thereof. The near-infrared nano-photosensitizer in the present invention is modified by conjugation extension of the boron dipyrromethene core, achieving absorption and emission spectra close to the near-infrared region. A polyfluoroalkyl group and a polyethylene glycol group are introduced to the boron dipyrromethene structure to obtain an amphiphilic photosensitizer. By means of the strong fluorine-fluorine interaction between the polyfluoroalkyl group and the hydrophilic interaction of the polyethylene glycol group, a nano-photosensitive micelle with an ultra-low CMC value is ultimately constructed. Boron dipyrromethene is induced by fluorine-fluorine interaction to undergo J-aggregation, causing the maximum absorption peak to red-shift to the near-infrared region, beneficial to the deep phototherapy of tumors.

Abstract: The present technology is related to reducing or treating neurological swelling and related conditions with SUR1-TRPM4 channel inhibitors. In some embodiments, the methods include: reducing late neurological deterioration or preventing death, reducing cerebral midline shift, reducing the degree of disability in a subject, counteracting blood glucose levels in a subject receiving a SUR1-TRPM4 channel inhibitor, preventing brain swelling, monitoring liver enzyme activity along with treating injury or conditions related to CNS edema, or monitoring cardiac activity along with treating injury or conditions related to CNS edema.

Abstract: Compositions comprising fatty acid analogs are provided for treating metabolic syndrome, anemia, cancer, cardiovascular disease, diabetes, dyslipidemia, hypertension, inflammation, insulin resistance, prediabetes, fatty liver disease, steatohepatitis, iron overload, neurodegenerative diseases, including Alzheimer's disease and other forms of dementia, and other related conditions. Methods for the diagnosis and monitoring of metabolic syndrome and other conditions are also provided.

Abstract: Disclosed herein is a complex, a contrast agent and the method for treating a disease related to CXCR4 receptor. The complex is configured to bind the CXCR4 receptor, and is used as a medicament for diagnosis and treatment of cancers and other indications related to the CXCR4 receptor.

Abstract: An 2-benzo-[3,4-b]quinolino-[b,g]indeno[1?,2?:3,4]fluoreno-[1,2-d]oxonine-24-flouro-5,11,16,21-tetraone compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Provided are aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.

Abstract: Provided herein are pharmaceutical compositions comprising a phosphatidylinositol 3-kinase inhibitor or a pharmaceutically acceptable form thereof, and a Bcl-2 inhibitor or a pharmaceutically acceptable form thereof. Also provided herein are methods for treating cancer comprising administration the compositions, and uses of the compositions, e.g., for the treatment of cancer.

Abstract: Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml.

Abstract: Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).

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

Abstract: The present disclosure relates to derivatized agelastatin compounds and methods for the treatment, prevention, or delay of cancer, comprising administering a therapeutically effect amount of the derivatized agelastatin compounds, a pharmaceutically acceptable salt thereof, or a composition thereof to a subject in need thereof. Methods for making the derivatized agelastatin compounds are also provided.

Abstract: The present disclosure provides a method for preparing a nicotinamide mononucleotide cocrystal, and aims to solve the technical problems of larger content/weight difference and inconsistent quality of nicotinamide mononucleotide (NMN) medicines or health care products due to poor fluidity of existing nicotinamide mononucleotide crystals. The method includes the steps of mixing nicotinamide mononucleotide as an active pharmaceutical ingredient with isonicotine as a cocrystal former by adopting solution synthesis and then performing crystal precipitation. The method has the advantages of simple operation and wide application range.

Abstract: The present disclosure is concerned with substituted N-(5-chloro-4-((4-chlorophenyl)(cyano)methyl)-2-methylphenyl)benzamide compounds, and methods of treating and/or preventing neurodegenerative or neurocognitive disorders including, but not limited to, Alzheimer's disease, cerebral autosomal dominant arteriopathy with sub-cortical infarcts and leukoencephalopathy (CADASIL), Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis (ALS/Lou Gehrig's disease), Multiple Sclerosis, spinal muscular atrophy, spinal and bulbar muscular atrophy, familial spastic paraparesis, Machado Joseph disease, Friedreich's ataxia, Lewy body disease, and dementia (e.g., vascular dementia, Lewy body dementia, frontotemporal dementia, mixed dementia, dementia induced by Alzheimer's disease or Parkinson's disease). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Provided is a drug superior for preventing and/or treating dementia. It contains a carbostyril derivative of the following formula (1) (wherein R is a cycloalkyl group, A is a lower alkyl group, and a single bond or a double bond is present between the 3-position and the 4-position of the carbostyril nucleus) and dihydroquercetin.

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: 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.