C07D209/34

Ion Channel Antagonists/Blockers and Uses Thereof

Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.

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Ion Channel Antagonists/Blockers and Uses Thereof

Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.

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COMPOUNDS AND THEIR METHODS OF USE

The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.

INHIBITORS OF CYSTEINE PROTEASES AND METHODS OF USE THEREOF
20230212152 · 2023-07-06 ·

The disclosure provides compounds of formula II with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.

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SMALL MOLECULE INHIBITORS OF GRK5 AND GRK5 SUBFAMILY MEMBERS AND USES THEREOF
20230212120 · 2023-07-06 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having an indolinone structure which function as inhibitors of GRK5, and their use as therapeutics for the treatment of heart conditions and cancer.

SMALL MOLECULE INHIBITORS OF GRK5 AND GRK5 SUBFAMILY MEMBERS AND USES THEREOF
20230212120 · 2023-07-06 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having an indolinone structure which function as inhibitors of GRK5, and their use as therapeutics for the treatment of heart conditions and cancer.

Therapeutic compounds and methods of use thereof

There are provided new heterobifunctional agents designed to mediated formation of protein-protein dimers and promote ubiquitination of a protein of the dimer. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by protein over-expression or malfunction.

Compound of 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based phosphine ligand, and preparation method thereof

The present application discloses a 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based phosphine ligand, an intermediate, a preparation method and uses thereof. The compound of phosphine ligand is a compound having a structure represented by formula I or formula II, or an enantiomer, a raceme, or diastereomer thereof. The phosphine ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6′-dihydroxyl-3,3,3′,3′-tetramethyl-1,1′-spirobiindane is used as a raw material and the compound represented by formula III serves as the key intermediate. The new phosphine ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral phosphine ligand that is widely used in many asymmetric catalytic reactions including asymmetric hydrogenation and asymmetric allyl alkylation, and thus it has economic practicability and industrial application prospect. ##STR00001##

ANTI-FIBROTIC COMPOUNDS AND USE THEREOF
20220371990 · 2022-11-24 ·

The present invention relates to compounds, compositions and methods for treating fibrosis. In particular, compounds that inhibit or downregulate Sirtuin 1 (SIRT1) activity, which are particularly useful in the treatment of Idiopathic Pulmonary Fibrosis (IPF) are provided.

ANTI-FIBROTIC COMPOUNDS AND USE THEREOF
20220371990 · 2022-11-24 ·

The present invention relates to compounds, compositions and methods for treating fibrosis. In particular, compounds that inhibit or downregulate Sirtuin 1 (SIRT1) activity, which are particularly useful in the treatment of Idiopathic Pulmonary Fibrosis (IPF) are provided.