68819-84-1Relevant academic research and scientific papers
Synthesis and structure activity relationship of the first class of LXR inverse agonists
Elgendy, Bahaa,Griffett, Kristine,Hegazy, Lamees,Di Fruscia, Paolo,Sample, Kirby,Schoepke, Emmalie,Kamenecka, Theodore M.,Burris, Thomas P.
, (2021/12/14)
Liver X Receptors (LXRs) are members of the nuclear receptor family, and they play significant role in lipid and cholesterol metabolism. Moreover, they are key regulators of several inflammatory pathways. Pharmacological modulation of LXRs holds great pot
Small molecule compound based on EZH2 protein degradation, and application thereof
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Paragraph 0031; 0042-0045, (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.
Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma
Tu, Yalin,Sun, Yameng,Qiao, Shuang,Luo, Yao,Liu, Panpan,Jiang, Zhong-Xing,Hu, Yumin,Wang, Zifeng,Huang, Peng,Wen, Shijun
, p. 10167 - 10184 (2021/07/26)
Traditional EZH2 inhibitors are developed to suppress the enzymatic methylation activity, and they may have therapeutic limitations due to the nonenzymatic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation. Two best degraders, YM181 and YM281, induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.
COMPOUNDS AND USES THEREOF
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Page/Page column 120-121, (2021/08/06)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
BIFUNCTIONAL DEGRADERS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASES AND THERAPEUTIC USE THEREOF
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Page/Page column 125, (2021/08/27)
The present disclosure provides bifunctional compounds as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.
PROCESS FOR THE PREPARATION OF PANOBINOSTAT
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Page/Page column 10-11, (2021/09/03)
The present invention relates to a new process for the preparation of Panobinostat and intermediates thereof.
Compound targeting to I-type PRMT and preparation method and application of compound
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Paragraph 0097-0101, (2020/03/11)
The invention relates to the technical field of chemical drugs, in particular to a compound targeting to I-type PRMT, and a preparation method and application thereof. The compound A and a pharmaceutically acceptable salt thereof belong to covalent inhibi
ANDROGEN RECEPTOR PROTEIN DEGRADERS
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Paragraph 0172; 0296, (2020/07/21)
The present disclosure provides compounds represented by Formula (I): A—L—B (I), and the salts or solvates thereof, wherein A, L, and B are as defined in the specification. Compounds having Formula (I) are androgen receptor degraders useful for the treatment of cancer.
QUINAZOLINE DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
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Paragraph 0241, (2020/07/15)
The present disclosure provides certain quinazoline compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Atorvastatin Derived HMG-CoA Reductase Degradation Inducing Compound
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Paragraph 0461-0465, (2020/12/01)
The present invention relates to a HMG-CoA reductase degradation-inducing compound and, more specifically, to a bifunctional compound in which atorvastatin and E3 ubiquitin ligase binding moiety are chemically linked as HMG-CoA reductase binding moiety, to a production method thereof, to a HMG-CoA reductase degradation method using the same, and to a pharmaceutical composition for preventing or treating HMG-CoA reductase-related diseases, comprising the same.
