C07D311/30

COMPOSITION FOR PREVENTING OR TREATING TNF-RELATED DISEASES, CONTAINING NOVEL DERIVATIVE AS ACTIVE INGREDIENT, AND METHOD FOR INHIBITING TNF ACTIVITY BY USING SAME
20230099574 · 2023-03-30 · ·

The present invention relates to: a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate, or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF, and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit a TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.

SCUTELLARIAE RADIX COMPOUNDS AND USE THEREOF FOR INHIBITING OXIDATIVE PHOSPHORYLATION PATHWAY OF MITOCHONDRIA

Provided are scutellariae radix compounds and the use thereof for inhibiting the oxidative phosphorylation pathway of mitochondria. Specifically provided is the use of a compound of formula I, or an optical isomer thereof, or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof in the preparation of a composition or a preparation. The composition or the preparation is used for one or more uses selected from the group consisting of: (a) inhibiting the oxidative phosphorylation pathway of mitochondria; (b) preventing and/or treating diseases associated with the oxidative phosphorylation pathway of mitochondria; and (c) preventing and/or treating cancers. The compounds can be used for inhibiting the oxidative phosphorylation pathway of mitochondria and preventing and/or treating diseases associated with the oxidative phosphorylation pathway of mitochondria, and especially have a significant inhibitory effect on the upregulation of the oxidative phosphorylation pathway of mitochondria or tumor cells with a low mPTP activity.

Amylase inhibitor compounds, methods of their use and compositions thereof

There are provided compounds of Formula I: ##STR00001##
various compositions thereof and methods for their use in the inhibition of α-amylase.

Amylase inhibitor compounds, methods of their use and compositions thereof

There are provided compounds of Formula I: ##STR00001##
various compositions thereof and methods for their use in the inhibition of α-amylase.

Compound containing fused ring, use thereof and pharmaceutical composition containing same

Disclosed are a compound containing a fused ring, a use thereof and a pharmaceutical composition containing same. Provided are a compound as shown in formula I-A, a pharmaceutically acceptable salt thereof, a solvate thereof, a solvate of the pharmaceutically acceptable salt thereof or a crystal form thereof. The compound can significantly reduce the levels of HBsAg, HBeAg and HBV DNA, and can be used for preparing a drug for treating hepatitis B, and has good market prospects. (I-A)

PRODRUGS, ANALOGS OR DERIVATIVES OF KAEMPFEROL AS ANTIVIRAL AGENTS
20230064951 · 2023-03-02 ·

The present invention relates to compounds which can inhibit host cell ACE2 receptor, viral spike S protein, Spike protein-ACE2 receptor interface, RNA-dependent RNA polymerase (RdRp), helicase and exoribonuclease activity. Particularly the invention relates to kaempferol analogs, derivatives and prodrugs as antiviral agents specific to Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) or SARS-CoV-2 and SARS (Severe, acute respiratory syndrome coronavirus).

PRODRUGS, ANALOGS OR DERIVATIVES OF KAEMPFEROL AS ANTIVIRAL AGENTS
20230064951 · 2023-03-02 ·

The present invention relates to compounds which can inhibit host cell ACE2 receptor, viral spike S protein, Spike protein-ACE2 receptor interface, RNA-dependent RNA polymerase (RdRp), helicase and exoribonuclease activity. Particularly the invention relates to kaempferol analogs, derivatives and prodrugs as antiviral agents specific to Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) or SARS-CoV-2 and SARS (Severe, acute respiratory syndrome coronavirus).

PROCESSES FOR THE PREPARATION OF ORTHO-ALLYLATED HYDROXY ARYL COMPOUNDS

The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

##STR00001##

PROCESSES FOR THE PREPARATION OF ORTHO-ALLYLATED HYDROXY ARYL COMPOUNDS

The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

##STR00001##

COMPOSITIONS AND METHODS OF SUPPRESSING AVERSIVENESS OF PHARMACEUTICALS AND INGESTIBLE MATERIALS

Provided herein are compositions and methods of ameliorating the pharmaceutical aversiveness of active pharmaceutical ingredient (API) by administering the API after or substantially simultaneously with a flavone compound.