Abstract: The present disclosure provides androgen receptor (AR) and phosphodiesterase 5 (PDE-5) inhibitor compounds of the formula (I): and compositions including said compounds. The compounds can provide dual functionality for inhibiting AR and inhibiting PDE-5. The present disclosure also provides methods of using said compounds and compositions for inhibiting AR and PDE-5 in a biological system or biological sample. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.

Abstract: The present disclosure provides adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including said compounds. The present disclosure also provides methods of using said compounds and compositions for modulating (e.g., inhibiting or antagonizing) A2A and/or A1 receptor in a biological system. The compounds and compositions find use in various therapeutic applications including the treatment of cancer and in immuno-oncology. The compounds and compositions find use in various therapeutic applications including the treatment of central nervous system or neurodegenerative diseases, such as Parkinson’s disease.

Abstract: Provided herein is an immunocytokine comprising (i) an antigen binding protein (ABP) specific to a target protein; (ii) an IL-21 domain; and (iii) an IL-21R? mutein, wherein the IL-21R? mutein has a reduced binding affinity to the IL-21 domain compared to a wild-type IL-21R?. Further provided includes a method of using the immunocytokine to selectively activate an IL-21R? on a target cell, thereby enhance immune response or treat cancer.

Abstract: The present disclosure provides phosphodiesterase 5 (PDE-5) and/or phosphodiesterase 6 (PDE-6) inhibitor compounds and compositions including said compounds. In some embodiments, said compounds are nitrogen oxide (NO) donating PDE-5 and/or -6 inhibitor compounds that include a nitrogen oxide-containing donor substituent attached to a benzenesulfonamide group. The compounds can provide dual functionality for increasing protein kinase G (PKG) activity by inhibiting PDE-5 and PDE-6, and/or stimulating guanylate cyclase (sGC) via donation of nitrogen oxide (NO) from the donor substituent of the compound. The present disclosure also provides methods of using said compounds and compositions for inhibiting PDE-5 and/or -6 and increasing activity of protein kinase G (PKG). The compounds and compositions find use in therapeutic applications including in the treatment of a variety of eye diseases.

Abstract: The present disclosure provides androgen receptor (AR) and phosphodiesterase 5 (PDE-5) inhibitor compounds and compositions including said compounds. The compounds can provide dual functionality for inhibiting AR and inhibiting PDE-5. The present disclosure also provides methods of using said compounds and compositions for inhibiting AR and PDE-5 in a biological system or sample. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.

Abstract: The present disclosure provides autotaxin (ATX) inhibitor compounds and compositions including said compounds. The present disclosure also provides methods of using said compounds and compositions for inhibiting ATX. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.