cas 509093-74-7, 1-(4-fluoro-3-nitrobenzyl)piperidine | Articles data ｜lookchem

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509093-74-7

Articles about 509093-74-7Total 3 be found

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COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 1606-1607

(2019/06/07)

Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4
In this Letter, we report the continued optimization of the N-acyl-2-aminobenzimidazole series, focusing in particular on the N-alkyl substituent and 5-position of the benzimidazole based on the binding mode and the early SAR. These efforts led to the discovery of 16, a highly potent, selective, and orally bioavailable inhibitor of IRAK-4.
Wang, Zhulun,Sun, Daqing,Johnstone, Sheree,Cao, Zhaodan,Gao, Xiong,Jaen, Juan C.,Liu, Jingqian,Lively, Sarah,Miao, Shichang,Sudom, Athena,Tomooka, Craig,Walker, Nigel P.C.,Wright, Matthew,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
p. 5546 - 5550
(2015/11/17)

Benzimidazole derivatives
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.
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(2008/06/13)

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Chemical Properties

Boiling Point: 346.64oC at 760 mmHg
Flash Point:163.442oC
Density: 1.242g/cm3
Storage Temp.:2-8°C
Vapor Pressure: 0mmHg at 25°C
PKA: 7.69±0.10(Predicted)
PSA: 49.06000
LogP: 3.18090

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