C07D223/04

SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

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ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

##STR00001##

3-DIARYLMETHYLENES AND USES THEREOF
20230146127 · 2023-05-11 ·

3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

3-DIARYLMETHYLENES AND USES THEREOF
20230146127 · 2023-05-11 ·

3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

Process for the synthesis of n-substituted lactams and amides

A process for the synthesis of N-alkylated lactams via reductive alkylation. The process of the present disclosure may be conducted by the addition of an aldehyde to a lactam in the presence of a catalyst under a reducing atmosphere.

Process for the synthesis of n-substituted lactams and amides

A process for the synthesis of N-alkylated lactams via reductive alkylation. The process of the present disclosure may be conducted by the addition of an aldehyde to a lactam in the presence of a catalyst under a reducing atmosphere.

Ester substituted ion channel blockers and methods for use

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001## The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

Ester substituted ion channel blockers and methods for use

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001## The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

MYST family histone acetyltransferase inhibitors

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.