Abstract: Adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including the adenosine receptor antagonist compounds are disclosed. Methods of using the compounds and compositions for modulating (e.g., inhibiting or antagonizing) A2A and/or A1 receptor in a biological system are also disclosed. 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: 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.

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.

Abstract: Adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including said compounds are disclosed. 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 central nervous system or neurodegenerative diseases, such as Parkinson's disease. The compounds and compositions may also find use in various therapeutic applications including the treatment of cancer and in immuno-oncology.

Abstract: Adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including said compounds are disclosed. 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 central nervous system or neurodegenerative diseases, such as Parkinson's disease. The compounds and compositions may also find use in various therapeutic applications including the treatment of cancer and in immuno-oncology.

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: 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: Adenosine receptor (e.g., A2A and/or A1 receptor) antagonist compounds and compositions including said compounds are disclosed. 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 central nervous system or neurodegenerative diseases, such as Parkinson's disease. The compounds and compositions may also find use in various therapeutic applications including the treatment of cancer and in immuno-oncology.

Abstract: The present disclosure provides uses of phosphodiesterase 5 (PDE-5) and/or phosphodiesterase 6 (PDE-6) inhibitor compounds and uses of 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 via donation of 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 PKG. The compounds and compositions find use in the treatment of a variety of eye diseases.

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.

Abstract: Disclosed are a novel 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and a pharmaceutical use thereof. The 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and compositions containing them are useful for treating a tumor.