206265-94-3Relevant academic research and scientific papers
Small molecule compound based on EZH2 protein degradation, and application thereof
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, (2021/08/07)
The invention discloses a series of small molecule compounds capable of selectively degrading EZH2 protein, and application thereof. The compounds can be prepared into proper pharmaceutical dosage forms for EZH2-mediated related tumor treatment.
Heterocyclic compound and application thereof
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, (2021/08/07)
The invention discloses a heterocyclic compound and application thereof. The invention provides a heterocyclic compound as shown in a formula I, or pharmaceutically acceptable salt thereof. The heterocyclic compound can be used for degrading ALK, c-Met and ROS proteins.
Neem PROTAC compound with STAT3 degradation activity and preparation method and application thereof
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, (2022/01/10)
A NEEM PROTAC compound with STAT3 degradation activity, the structure of which is generally formula (I): Y is a specific protein ligand in the E3 ubiquitin ligase complex, a Cereblon protein ligand or A VHL protein ligand; X is a linking group between nee
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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Page/Page column 262, (2021/09/04)
This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.
Compound for targeted degradation of ALK, c-Met and ROS1 proteins, and preparation method thereof
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, (2020/07/07)
The invention provides a novel compound for targeted degradation of ALK, c-Met and ROS1 proteins, wherein the compound is represented by a formula A, is formed by linking an ubiquitin ligase E3 recognition ligand and an ALK, c-Met and ROS1 protein inhibitor compound through a linking arm, and can selectively induce degradation of ALK, c-Met and ROS1 proteins and mutant proteins of the ALK, c-Met and ROS1 proteins. According to the invention, a bifunctional small molecule is obtained; and in-vitro anti-tumor activity data of the compound show that the compound has high-efficiency anti-tumor activity on conventional tumor cells, has strong inhibition activity on mutant cell strains (BaF3/EML4-ALKG1202R, BaF3/EML4-ALKL1196M and BaF3-TEL-ALK-C1156Y) causing the drug resistance, provides a effective antitumor drug for clinical application, has great application value, brings good news for tumor treatment, especially for some drug-resistant patients, and has important social benefits.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 001134; 001135, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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Page/Page column 173, (2020/03/15)
Bivalent compounds, compositions comprising one or more of the bivalent compounds, and methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof are provided. Methods for identifying such bivalent compounds are provided, either.
PROTEIN DEGRADERS AND USES THEREOF
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, (2019/04/16)
The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.
IRAK DEGRADERS AND USES THEREOF
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, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
MYELOPEROXIDASE IMAGING AGENTS
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, (2018/06/06)
Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using positron emission tomography or fluorescence imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using radiolabeled and unlabeled compounds are also provided.
