171663-13-1Relevant articles and documents
COMPOUNDS AND USES THEREOF
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Page/Page column 115, (2021/08/06)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
COMPOUNDS AND USES THEREOF
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Page/Page column 231; 232, (2021/08/06)
The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.
Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy
Zhang, Zhuqing,Guo, Zuhao,Xu, Xiaowei,Cao, Danyan,Yang, Hong,Li, Yanlian,Shi, Qiongyu,Du, Zhiyan,Guo, Xiaobin,Wang, Xin,Chen, Danqi,Zhang, Ying,Chen, Lin,Zhou, Kaixin,Li, Jian,Geng, Meiyu,Huang, Xun,Xiong, Bing
, p. 16650 - 16674 (2021/12/02)
CARM1 is a protein arginine methyltransferase and acts as a transcriptional coactivator regulating multiple biological processes. Aberrant expression of CARM1 has been related to the progression of multiple types of cancers, and therefore CARM1 was consid
COMPOUNDS AND USES THEREOF
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Page/Page column 162, (2020/08/22)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
COUMARIN-LIKE CYCLIC COMPOUND AS MEK INHIBITOR AND USE THEREOF
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Paragraph 0137-0139, (2020/05/30)
Disclosed are a class of coumarin-like cyclic compounds as MEK inhibitors and pharmaceutical compositions comprising the compounds, and the use of same in the preparation of a drug for treating MEK-related diseases. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof or tautomers thereof.
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate
Cinelli, Maris A.,Reidl, Cory T.,Li, Huiying,Chreifi, Georges,Poulos, Thomas L.,Silverman, Richard B.
, p. 4528 - 4554 (2020/05/05)
Inhibition of neuronal nitric oxide synthase (nNOS), an enzyme implicated in neurodegenerative disorders, is an attractive strategy for treating or preventing these diseases. We previously developed several classes of 2-aminoquinoline-based nNOS inhibitor
CHEMICAL COMPOUNDS
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Page/Page column 106; 107, (2019/04/11)
The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to FormμLa (I): wherein R, R1,P, X, Y, and Z are as defined herein; or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be usefμL in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Arginine methyltransferase inhibitor and pharmaceutical composition and application thereof
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Paragraph 0345; 0347-0350, (2019/10/29)
The invention relates to an arginine methyltransferase inhibitor and a pharmaceutical composition and application thereof, in particular to a compound represented by a formula (I), a pharmaceuticallyacceptable salt, isomer, racemate, prodrug, co-crystal c
K-RAS MODULATORS WITH A VINYL SULFONAMIDE MOIETY
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Paragraph 0414, (2019/11/12)
Provided herein are compounds comprising a vinyl sulfonamide moiety. Also provided herein are pharmaceutical compositions comprising such compounds, and methods of using such compounds and pharmaceutical compositions for inhibiting the post-translational
Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1)
Chien, Huan-Chieh,Colas, Claire,Finke, Karissa,Springer, Seth,Stoner, Laura,Zur, Arik A.,Venteicher, Brooklynn,Campbell, Jerome,Hall, Colton,Flint, Andrew,Augustyn, Evan,Hernandez, Christopher,Heeren, Nathan,Hansen, Logan,Anthony, Abby,Bauer, Justine,Fotiadis, Dimitrios,Schlessinger, Avner,Giacomini, Kathleen M.,Thomas, Allen A.
supporting information, p. 7358 - 7373 (2018/08/06)
The L-type amino acid transporter 1 (LAT1, SLC7A5) transports essential amino acids across the blood-brain barrier (BBB) and into cancer cells. To utilize LAT1 for drug delivery, potent amino acid promoieties are desired, as prodrugs must compete with millimolar concentrations of endogenous amino acids. To better understand ligand-transporter interactions that could improve potency, we developed structural LAT1 models to guide the design of substituted analogues of phenylalanine and histidine. Furthermore, we evaluated the structure-activity relationship (SAR) for both enantiomers of naturally occurring LAT1 substrates. Analogues were tested in cis-inhibition and trans-stimulation cell assays to determine potency and uptake rate. Surprisingly, LAT1 can transport amino acid-like substrates with wide-ranging polarities including those containing ionizable substituents. Additionally, the rate of LAT1 transport was generally nonstereoselective even though enantiomers likely exhibit different binding modes. Our findings have broad implications to the development of new treatments for brain disorders and cancer.