C07D487/10

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
20230046427 · 2023-02-16 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of 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
20230046427 · 2023-02-16 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of 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.

New compounds for treatment of diseases related to DUX4 expression

The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.

New compounds for treatment of diseases related to DUX4 expression

The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.

COCRYSTALS OF PTEROSTILBENE AND COMPOSITIONS COMPRISING THEM

The present disclosure relates to a cocrystal of pterostilbene and a coformer capable to form hydrogen bond interactions, to a process for the preparation thereof, and to its use as a medicament or a dietary supplement. The present disclosure also relates to a composition comprising the cocrystal.

Spiro-lactam NMDA receptor modulators and uses thereof
11578072 · 2023-02-14 · ·

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders as well as other disorders.

UNNATURAL AMINO ACIDS AND USES THEREOF
20230042042 · 2023-02-09 ·

This invention provides unnatural amino acids as well as amino acid sequences, foldamers, macrocycles, and formulations comprising said unnatural amino acids. In one aspect of the invention, the unnatural amino acids or the formulation thereof are used to mimic natural amino acids or the formulations thereof in a subject in need thereof.

UNNATURAL AMINO ACIDS AND USES THEREOF
20230042042 · 2023-02-09 ·

This invention provides unnatural amino acids as well as amino acid sequences, foldamers, macrocycles, and formulations comprising said unnatural amino acids. In one aspect of the invention, the unnatural amino acids or the formulation thereof are used to mimic natural amino acids or the formulations thereof in a subject in need thereof.

COMPOUND COMPRISING EZH2 INHIBITOR AND E3 LIGASE BINDER AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING EZH2-ASSOCIATED DISEASE COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a compound comprising an EZH2 inhibitor and an E3 ligase binder, and a pharmaceutical composition for preventing or treating EZH2-associated disease and a pharmaceutical composition for selective protein degradation containing the same as an active ingredient. Since the compound of the present invention can selectively degrade EZH2, it can be effectively used for the treatment of EZH2-related diseases and cancers, particularly, cancers in which EZH2 is overexpressed, and can be usefully used for the selective degradation of EZH2.

NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

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