Abstract: The present invention relates to 1,2,3-triazoles of formula: useful for improving or restoring the intracellular calcium homeostasis and RyR-calstabin binding function in human and animal cells. The present invention also relates to methods for synthesizing said compounds, to pharmaceutical compositions containing them, and to the use thereof for preventing or treating skeletal muscle, heart and nervous system disorders.

Abstract: Methods of treating bacterial infection in immunocompromised subjects and subjects with one or more underlying malignancies include administering a combination of meropenem and vaborbactam to the subject. Suitable subjects to be treated can include a subject with a history of ongoing leukemia or lymphoma, a subject that has had an organ transplant, stem cell transplant, bone marrow transplant, or splenectomy, a subject receiving immunosuppressive medications, a subject receiving bone marrow ablative chemotherapy, a subject with neutropenia and subject suffering from or having suffered from a malignancy.

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: Novel compounds useful for treating and/or preventing HCMV infections are provided.

Abstract: An efficient blue-green to orange-red thermally activated delayed fluorescence material, a manufacture method, and an application thereof are provided. This disclosure solves the technical problems in the art by cleverly synthesizing a series of thermally activated delayed fluorescence materials, which have lower singlet-triplet energy difference, high luminous efficiency, and fast reverse intersystem crossing constant, and simultaneously fine-tuning the structure to cover the spectrum from blue-green light to orange-red light. Further, their structures are confirmed by nuclear magnetic resonance and mass spectroscopy, and their photophysical properties are also determined. Therefore, these luminescent thermally activated delayed fluorescence (TADF) materials are applied to light-emitting layer for manufacturing a series of organic light-emitting diodes (OLEDs) having high performance, which have great application prospects and economic value.

Abstract: Chemical compounds are provided that are useful in the treatment of diseases associated with an activity of a 5,10-methylenyltetrahydrofolate cyclohydrolase/5,10-methylene tetrahydrofolate dehydrogenase enzyme in pathological eukaryotic cells. In particular, compounds that exhibit inhibitory activity upon 5,10-methylenyltetrahydrofolate cyclohydrolase/5,10-methylene tetrahydrofolate dehydrogenase enzymes and their use in the treatment of cancer and/or parasitic diseases are provided.

Abstract: The present disclosure describes novel compounds of the general Formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds can inhibit both LSD and HDAC and are useful as therpeautic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, parkinson's disease and the like.

Abstract: A method for preparing phthalocyanine nanospheres is provided, including: synthesizing an ionic phthalocyanine molecule of formula I according to a following chemical scheme: wherein M is Cu or Zn, X is Br or Cl, R1, R2, R3, and R4 are aromatic substituent groups; dissolving at least one ionic phthalocyanine molecule selected from the formula I in a solvent to form a solution; preparing a two-dimensional layer crystalline material with an opposite charge to the ionic phthalocyanine molecule; adding the two-dimensional layer crystalline material to the solution; heating the solution to evaporate a portion of the solvent to aggregate the ionic phthalocyanine molecule into phthalocyanine nanospheres between a film layer of the two-dimensional layer crystalline material; and separating the phthalocyanine nanospheres from the film layer of the two-dimensional layer crystalline material.

Abstract: The present disclosure relates to chemical compounds that modulate proteasome activity, pharmaceutical compositions containing such compounds, and use of these compounds and compositions for the treatment of disorders of uncontrolled cellular proliferation such as, for example, a cancer. 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: Disclosed are a novel tumor microenvironment-related target TAK1 and an application thereof in inhibition of a tumor. TAK1, as a research target for SASP regulation, can be used as a marker in tumor diagnosis and prognosis, and can also be used as a tumor microenvironment specific target to develop tumor inhibitory drugs.

Abstract: The present invention relates to Fms-like tyrosine kinase (FLT3) inhibitors. The present invention provides novel 4-quinolinone derivatives used as FLT3 inhibitors and for treatment and/or prevention of tumors.

Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX or Formula X and, the methods for the treatment of fungal infections may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of fungal infections.

Abstract: The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the use thereof.

Abstract: Chemical compounds are provided belonging to the group of nucleotide analogues. More specifically, acylnucleoside phosphonate compounds are disclosed and also their method of preparation and their use as medicaments, in particular for the prevention and/or the treatment of diseases caused by infection by an organism that is auxotrophic for purines, such as Plasmodium falciparum. Also disclosed are pharmaceutical compositions containing such compounds.

Abstract: Disclosed herein are a preparation method and an application of an isoxazinone compound (I), where the preparation method includes: reacting compound (II) with a carboxylic acid (III) in the presence of a dehydrating agent and a base to produce the isoxazinone compound (I); and subjecting the isoxazinone compound (I) and a protonic acid salt of an amino compound (IV) or R3OH (VII) to ring-opening reaction in the presence of a base to produce a bisamide compound (V) or an N-acyl benzoate compound (VI).

Abstract: The invention relates to Pro-drugs, comprising red-ox-sensitive cleavage sites. The compounds may be utilized in medical practice for targeting of si RNA, antisense oligonucleotides or protein-based therapeutics to the cytoplasmatic compartment of cells both in vitro or in vivo, in a subject in need.

Abstract: The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.

Abstract: This invention relates to compounds useful for inhibiting telomere elongation. More specifically, the invention provides nucleotide analogs that are incorporated into telomeres by telomerase thereby inhibiting elongation of telomeres. The compounds are use in treating cancer and other cell proliferative diseases.

Abstract: The present application relates to treatment of myeloproliferative neoplasms using the JAK1/JAK2 inhibitor, ruxolitinib, in combination with a low dose of a Pim inhibitor, N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, wherein the combination is unexpectedly synergistic at a very low dose of the Pim inhibitor.

Abstract: The present invention relates to compounds of Formula (I) as defined herein, and salts, hydrates and solvates thereof. The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to the use of compounds of Formula (I) in the treatment or prevention of PRMT5-mediated disorders, such as cancer.