59227-80-4Relevant academic research and scientific papers
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
Yang, Bowen,Wu, Qian,Huan, Xiajuan,Wang, Yingqing,Sun, Yin,Yang, Yueyue,Liu, Tongchao,Wang, Xin,Chen, Lin,Xiong, Bing,Zhao, Dongmei,Miao, Zehong,Chen, Danqi
supporting information, (2020/12/28)
In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target.
Palladium-Catalyzed Germylation of Aryl Bromides and Aryl Triflates Using Hexamethyldigermane
Komami, Narumi,Matsuoka, Keitaro,Yoshino, Tatsuhiko,Matsunaga, Shigeki
, p. 2067 - 2075 (2018/02/26)
Palladium-catalyzed germylation of aryl bromides and aryl triflates using commercially available hexamethyldigermane is described. Optimized reaction conditions afforded various functionalized aryltrimethylgermanes, including drug-like molecules, in moderate to good yields, demonstrating the versatility of the presented protocols.
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety
Dow, Robert L.,Ammirati, Mark,Bagley, Scott W.,Bhattacharya, Samit K.,Buckbinder, Leonard,Cortes, Christian,El-Kattan, Ayman F.,Ford, Kristen,Freeman, Gary B.,Guimar?es, Cristiano R. W.,Liu, Shenping,Niosi, Mark,Skoura, Athanasia,Tess, David
, p. 3114 - 3125 (2018/04/23)
Studies have linked the serine-threonine kinase MAP4K4 to the regulation of a number of biological processes and/or diseases, including diabetes, cancer, inflammation, and angiogenesis. With a majority of the members of our lead series (e.g., 1) suffering from time-dependent inhibition (TDI) of CYP3A4, we sought design avenues that would eliminate this risk. One such approach arose from the observation that carboxylic acid-based intermediates employed in our discovery efforts retained high MAP4K4 inhibitory potency and were devoid of the TDI risk. The medicinal chemistry effort that led to the discovery of this central nervous system-impaired inhibitor together with its preclinical safety profile is described.
SUBSTITUTED IMIDAZOLONE DERIVATIVES, PREPARATIONS AND USES
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Page/Page column 45, (2010/02/16)
The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.
CCR10 ANTAGONISTS
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Page/Page column 66, (2009/05/28)
The invention relates to a compound of formula (I) or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy
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Page/Page column 16, (2008/12/06)
The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1/s
Treatment of skin conditions by use of PPAR alpha activators
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, (2008/06/13)
Disorders of the skin and mucous membrane that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of compounds that are either activators of the farnesoid X receptor, activators of the peroxisome proliferator-activated receptor alpha , and oxysterol activators of the LXR alpha receptor. The same compounds are also effective in treating disorders of epidermal differentiation and proliferation.
