C07D235/14

ASPARAGINE DERIVATIVES AND METHODS OF USING SAME

The present disclosure relates to compounds of formulas (A) and (I), pharmaceutically acceptable salts thereof, and solvates of any of the foregoing, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer, such as colorectal cancer, using the same.

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INHIBITORS OF PROTEIN ARGININE DEIMINASE 1 AND METHODS OF PREPARATION AND USE THEREOF
20230002328 · 2023-01-05 ·

The invention provides novel inhibitors or inactivators of protein arginine deiminase 1, pharmaceutical compositions and methods of use thereof. The invention also relates to molecular probes based on such compounds and methods of use thereof.

GLP-1 Receptor Agonist and Use Thereof

The present invention provides novel compounds of chemical formula 1, optical isomers of the compounds, or a pharmaceutically acceptable salts of the compounds, or the optical isomers. The compounds, isomers, and salts exhibits excellent activity as GLP-1 receptor agonists. Particularly, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used therapeutic agents for metabolic diseases. In addition, they exhibits excellent pharmacological safety for cardiovascular systems.

Substituted Benzimidazole Derivative And Use Thereof

The present invention relates to a substituted benzimidazole derivative as represented by formula (I) and a pharmaceutically acceptable salt, a polymorph, a tautomer, a stereoisomer, a hydrate, a solvate or an isotopic variant of the derivative. The compound is a PPAR α and/or PPAR δ agonist, therefore the compound can be used for treating and/or preventing diseases associated with by PPAR α and/or PPAR δ, such as non-alcoholic steatohepatitis, Duchenne muscular dystrophy syndrome, Alzheimer's disease, tumors and PBC (primary biliary cholangitis)

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Substituted Benzimidazole Derivative And Use Thereof

The present invention relates to a substituted benzimidazole derivative as represented by formula (I) and a pharmaceutically acceptable salt, a polymorph, a tautomer, a stereoisomer, a hydrate, a solvate or an isotopic variant of the derivative. The compound is a PPAR α and/or PPAR δ agonist, therefore the compound can be used for treating and/or preventing diseases associated with by PPAR α and/or PPAR δ, such as non-alcoholic steatohepatitis, Duchenne muscular dystrophy syndrome, Alzheimer's disease, tumors and PBC (primary biliary cholangitis)

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GLP-1 RECEPTOR AGONIST AND USE THEREOF

Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.

CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS WITH ENHANCED EFFICACY

The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS WITH ENHANCED EFFICACY

The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORγ) and pharmaceutical uses thereof

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders. ##STR00001##

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORγ) and pharmaceutical uses thereof

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders. ##STR00001##