C07D209/14

ANTICANCER COMPOUNDS
20230025178 · 2023-01-26 ·

Disclosed are compounds of formula (I):

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and pharmaceutically acceptable salts thereof. The compounds of the invention are BDII-selective inhibitors of BET proteins, and have therapeutic potential for treating cancer, acute kidney disease, and viral infections, among other diseases.

ANTICANCER COMPOUNDS
20230025178 · 2023-01-26 ·

Disclosed are compounds of formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof. The compounds of the invention are BDII-selective inhibitors of BET proteins, and have therapeutic potential for treating cancer, acute kidney disease, and viral infections, among other diseases.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

##STR00001##

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

##STR00001##

USES OF P53 X-RAY CO-CRYSTAL STRUCTURES
20230024905 · 2023-01-26 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. Disclosed herein are compounds and methods to recover wild-type function of p53 mutants using x-ray co-crystal structures of mutant p53 and compounds of the disclosure. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

COMPOUND AND USE THEREOF IN TREATING AUTOIMMUNE DISEASES

A compound according to an embodiment is represented by Formula 1. The compound may be used for treatment of autoimmune diseases. A composition for treatment or prevention of autoimmune diseases includes the compound and is expected to not only control inflammation but also recover immune balance as well as damaged tissues, thereby restoring bowel tissue homeostasis.

COMPOUND AND USE THEREOF IN TREATING AUTOIMMUNE DISEASES

A compound according to an embodiment is represented by Formula 1. The compound may be used for treatment of autoimmune diseases. A composition for treatment or prevention of autoimmune diseases includes the compound and is expected to not only control inflammation but also recover immune balance as well as damaged tissues, thereby restoring bowel tissue homeostasis.

INHIBITORS OF APOL1 AND METHODS OF USING SAME

The disclosure provides compounds of Formula I,

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deuterated derivatives of those compounds, and pharmaceutically acceptable salts of those compounds and derivatives, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.

Inhibitors of NLRP3 inflammasome

The present disclosure relates to compounds of Formula I: ##STR00001##
that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.