Abstract: Disclosed are compounds of Formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1, R3, X, Y, Z, and W are as defined herein. The compounds are, for example, inhibitors of WRN helicase and useful in treating a proliferative disease, such as cancer.

Abstract: The present invention relates to a method of treating a cancer including administering a pharmaceutical composition to an individual suspected to have the cancer excluding humans in a pharmaceutically effective amount, where the pharmaceutical composition comprises an agent capable of inhibiting expression of kinesin spindle protein (KSP) and a mitosis inhibitor.

Abstract: The disclosure provides human toll-like receptor modulators of general Formula (II), wherein R1, R2, R3, R4, R5, R6, R7, R8 are defined herein.

Abstract: The invention provides methods of treating cancer characterized by the presence of one or both of wild type isocitrate dehydrogenase 1 (IDH1) gene and wild type IDH1 enzyme, by administering compounds that inhibit mutant IDH1 enzyme, such as Ivosidenib (AG-120, IVOSIDENIB®). The invention also provides cell-based methods for determining anti-cancer activity of test compounds under in vitro conditions of low concentrations of magnesium ion and/or glucose.

Abstract: This disclosure provides cyanine dye compounds having linked hydrogen bond-forming groups that can be used for detecting nucleic acids, particularly for fluorescent staining of DNA, in a biological sample. We found that the simultaneous incorporation of at least two hydrogen bond-forming groups (HBGs) into such a nucleic acid stain can provide for crosslinking interactions between the stain and the target nucleic acid, and lead to a significant increase in the detection sensitivity without substantially increasing undesirable cytotoxicity or mutagenicity properties of the dye compounds. The cyanine dye compounds can have a cyanine structure that connects two particular fused heterocycle ring systems, where at least two HBGs are connected to the core structure through linkers. Also provided are nucleic acid complexes including the cyanine dye compounds, and methods of using the compounds to detect nucleic acids in a biological sample.

Abstract: The present disclosure provides compounds and compositions thereof which are useful as inhibitors of JAK2 and which exhibit desirable characteristics for the same.

Abstract: Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R3, R4, R5, L1, L2, L3, G1, G2, and G3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

Abstract: Provided herein are compounds, compositions, pharmaceutical compositions, kits, and methods relating to novel sulfono-?-AA peptides. Novel sulfono-?-AA peptides as described herein can have the structure according to Formula 1: In embodiments according to the present disclosure, novel sulfono-?-AA peptides as described herein have minimal toxicity, can repair neuronal damage, inhibit Amyloid beta aggregation, and promote cellular growth and viability.

Abstract: Provided herein are lipidoid compounds of Formulae (I) and (II), and pharmaceutically acceptable salts, co-crystals, tautomers, stereoisomers, solvates, hydrates, polymorphs, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive lipidoid compounds, compositions, or formulations for treating and/or preventing diseases (e.g., genetic disease, proliferative disease, hematological disease, neurological disease, painful condition, psychiatric disorder, metabolic disorder, long-term medical condition, inflammatory disease, autoinflammatory disease, liver disease, lung disease, spleen disease, familial amyloid neuropathy, cardiovascular disease, viral infection, infectious disease, fibrotic condition, or autoimmune disease) in a subject, methods for synthesizing the compounds described herein, and compounds described herein synthesized by the synthetic methods described herein.

Abstract: The present disclosure relates to a method for preparing a compound of formula (I). In the compound of formula (I), n may be 0 to 5 and each of R1, R2, R3, and R4 may be independently selected from the group consisting of H, —O-Alkyl, halo, alkyl, —CN, or —NO3.

Abstract: The present technology relates to compounds that inhibit human Ly6K and homologs thereof. Also disclosed are methods of using such compounds to: inhibit activity of a Ly6K protein in a cell; decrease migration, colony formation, and/or proliferation of a cell; modulate expression of a gene in a cell, reduce suppression of the immune response to cancer in a subject, decrease tumorigenic growth of a cancer in a subject, and treat or prevent in a subject a disorder mediated by Ly6K protein.

Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition.

Abstract: The subject invention provides compositions and methods for inhibiting the growth and/or proliferation of cancer cells. The subject invention also provides methods for treating cancer in a subject in need of such treatment by administering a composition described herein. The subject invention can be used to inhibit cancer cell growth by exposing the cells to a composition. The subject invention further provides cancer treatments that may be used in combination with surgery, chemotherapy, and/or radiation therapy.

Abstract: Compounds, compositions, and method useful for treating a viral infection, such as human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, are disclosed. In particular, prodrugs of phosphonamide nucleotide analogues and methods for their preparation and use as therapeutic or prophylactic agents are disclosed.

Abstract: Compounds and compositions having antifungal activity, and methods of using the antifungal compounds and compositions, are described for use in treating fungal infections.

Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating diseases, such as cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Abstract: The disclosure relates to compounds of formula (I) and pharmaceutically acceptable salts, and compositions thereof, wherein the substituents are as defined herein. Also provided are methods of making compounds of formula (I), and methods involving the compounds or compositions for treating disorders and diseases described herein.

Abstract: The synthesis of a range of pentylbezene-1,3-diol compounds of formula I is disclosed. These compounds bind to cannabinoid 1 and 2 receptors (CB1 and CB2), and are thus presumed to be useful in modulating the activity of such receptors. Accordingly, the use of such synthetic cannabinoids in the treatment of various disorders mediated by CB1 and CB2 is contemplated.

Abstract: The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.