C07D491/107

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
20230002403 · 2023-01-05 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure 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.

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
20230002403 · 2023-01-05 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure 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.

METHODS AND COMPOSITIONS FOR TARGETING PD-L1

The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-L1 or the PD-1/PD-L1 interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and uses of or methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.

METHODS AND COMPOSITIONS FOR TARGETING PD-L1

The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-L1 or the PD-1/PD-L1 interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and uses of or methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.

Crystalline forms of therapeutic compounds and uses thereof

Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.

Crystalline forms of therapeutic compounds and uses thereof

Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.

QUINOLIN-2-ONE DERIVATIVES

Compounds of the formula I

##STR00001##

in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, Q and Y have the meanings indicated in claim 1,
are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

QUINOLIN-2-ONE DERIVATIVES

Compounds of the formula I

##STR00001##

in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, Q and Y have the meanings indicated in claim 1,
are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

ISOXAZOLE DERIVATIVES TARGETING TACC3 AS ANTICANCER AGENTS

In one aspect, the present disclosure relates to compounds and compositions capable of inhibiting TACC3. In another aspect, the present disclosure relates to methods of treating TACC3 mediated diseases and disorders.

ISOXAZOLE DERIVATIVES TARGETING TACC3 AS ANTICANCER AGENTS

In one aspect, the present disclosure relates to compounds and compositions capable of inhibiting TACC3. In another aspect, the present disclosure relates to methods of treating TACC3 mediated diseases and disorders.