Abstract: This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF?) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Abstract: The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: Aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.

Abstract: Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: Compounds as inhibitors of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.

Abstract: Heterocyclic compounds of Formula (I): as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.

Abstract: Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.

Abstract: 1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.

Abstract: The present invention discloses compounds useful in treatment of conditions associated with excessive activity of transforming growth factor beta (TGF-?), particularly type I or activin-like kinase 5 (ALK 5). Specifically, the present invention discloses compound of formula (I) which exhibit inhibitory activity against ALK 5. Method of treating conditions associated with excessive activity (ALK 5) with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: The present disclosure relates generally to compounds useful in treatment of conditions associated with mutant isocitrate dehydrogenase (mt-IDH), particularly mutant IDH1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against mutant IDH1 enzymes. Method of treating conditions associated with excessive activity of mutant IDH1 enzymes with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: The present disclosure generally relates to the compounds that exhibits protein kinase inhibitory activity. Specifically, the present disclosure provides compounds of formula (I) that exhibits dual inhibitory activity against ALK5 and P38A MAP kinase. The present disclosure also provides process(es) for preparation of such compounds, pharmaceutical compositions containing one or a combination of these compounds, and methods of treatment of conditions associated with excessive activity of any or a combination of transforming growth factor-beta (TGF?) and p38 mitogen-activated protein kinase (MAPK) utilizing these compounds. An aspect of the present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salt, polymorph, solvate or stereoisomer thereof that exhibit dual inhibitory activity against ALK5 and P38 alpha.

Abstract: Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

Abstract: The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.

Abstract: This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF?) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Abstract: This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF?) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Abstract: Compounds as inhibitors of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.