C07D495/04

APTAMER NUCLEIC ACID MOLECULE, AND COMPLEX AND APPLICATION THEREOF
20230002769 · 2023-01-05 ·

The present application relates to an aptamer nucleic acid molecule, a complex containing the aptamer nucleic acid molecules, a method of detecting intracellular or extracellular RNA, DNA or other target molecules, and a kit containing the aptamer. The aptamer of the present application is capable of specifically binding a kind of fluorophore micromolecules, and can significantly enhance fluorescence intensity under excitation light of appropriate wavelength.

RAS PROTEIN DEGRADERS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS

Provided herein are RAS protein degraders, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RAS-mediated disorder, disease, or condition.


R.sup.Hct—L.sup.2—X—L.sup.1—R.sup.1  (1)

RAS PROTEIN DEGRADERS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS

Provided herein are RAS protein degraders, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RAS-mediated disorder, disease, or condition.


R.sup.Hct—L.sup.2—X—L.sup.1—R.sup.1  (1)

OXA-AZASPIRO DERIVATIVE, AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
20230234962 · 2023-07-27 ·

Disclosed are an oxa-azasipro derivative, a preparation method therefor and a pharmaceutical use thereof. In particular, disclosed are an oxa-azasipro derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, especially the use thereof as a PI3Kδ inhibitor and the use thereof in the preparation of a drug for treating diseases or conditions improved by means of inhibiting PI3Kδ.

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OXA-AZASPIRO DERIVATIVE, AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
20230234962 · 2023-07-27 ·

Disclosed are an oxa-azasipro derivative, a preparation method therefor and a pharmaceutical use thereof. In particular, disclosed are an oxa-azasipro derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, especially the use thereof as a PI3Kδ inhibitor and the use thereof in the preparation of a drug for treating diseases or conditions improved by means of inhibiting PI3Kδ.

##STR00001##

HETEROBICYCLIC CARBOXAMIDES AND USES THEREOF

Provided herein are heterobicyclic cyclopropanecarboxamide and heterobicyclic carboxamide compounds. In particular, provided herein are compounds that affect the function of kinases in a cell, and that are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers. Also provided herein are compositions comprising heterobicyclic cyclopropanecarboxamide or heterobicyclic carboxamide compounds.

HETEROBICYCLIC CARBOXAMIDES AND USES THEREOF

Provided herein are heterobicyclic cyclopropanecarboxamide and heterobicyclic carboxamide compounds. In particular, provided herein are compounds that affect the function of kinases in a cell, and that are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers. Also provided herein are compositions comprising heterobicyclic cyclopropanecarboxamide or heterobicyclic carboxamide compounds.

TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF

A compound of the present invention, which is a tricyclic derivative represented by chemical formula 1 or a pharmaceutically acceptable salt thereof, has an excellent inhibitory effect on serotonin activity and a pharmaceutical composition comprising same can be thus advantageously used for preventing or treating a metabolic disease associated with serotonin activation, etc.

ACC INHIBITOR AND USE THEREOF

The present invention provides a compound suitable for use as an acetyl CoA carboxylase (ACC) inhibitor, specifically, a thienopyridine derivative, and use of the compound in the preparation of drugs for treating metabolic disorders, cancers or other proliferative disorders, and nonalcoholic steatohepatitis (NASH).

ACC INHIBITOR AND USE THEREOF

The present invention provides a compound suitable for use as an acetyl CoA carboxylase (ACC) inhibitor, specifically, a thienopyridine derivative, and use of the compound in the preparation of drugs for treating metabolic disorders, cancers or other proliferative disorders, and nonalcoholic steatohepatitis (NASH).