29786-38-7Relevant academic research and scientific papers
Synthesis method of arylcyclobutane compound
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Paragraph 0033-0037; 0062-0065, (2022/01/10)
The present invention discloses a method for synthesizing an arylcyclobutane compound to 1eq phenylacetonitrile and 1.1eq 1-bromo-3-chloropropane as raw material, N,N- dimethylacetamide as a solvent, plus 2.5eq sodium hydride, under the protection of iner
Discovery of selective, orally bioavailable pyrazolopyridine inhibitors of protein kinase cθ (pkcθ) that ameliorate symptoms of experimental autoimmune encephalomyelitis
Collier, Philip N.,Twin, Heather C.,Knegtel, Ronald M. A.,Boyall, Dean,Brenchley, Guy,Davis, Christopher J.,Keily, Shazia,Mak, Chau,Miller, Andrew,Pierard, Fran?oise,Settimo, Luca,Bolton, Clare M.,Chiu, Peter,Curnock, Adam,Doyle, Elisabeth,Tanner, Adam J.,Jimenez, Juan-Miguel
supporting information, p. 1134 - 1139 (2019/08/27)
PKCθ plays an important role in T cell biology and is a validated target for a number of disease states. A series of potent and selective PKCθ inhibitors were designed and synthesized starting from a HTS hit compound. Cell activity, while initially a challenge to achieve, was built into the series by transforming the nitrile unit of the scaffold into a primary amine, the latter predicted to form a new hydrogen bond to Asp508 near the entrance of the ATP binding site of PKCθ. Significant improvements in physiochemical parameters were observed on introduction of an oxetane group proximal to a primary amine leading to compound 22, which demonstrated a reduction of symptoms in a mouse model of multiple sclerosis.
Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)
He, Wu,Zhou, Bin,Liu, Weijia,Zhang, Meizi,Shen, Zhenhua,Han, Zhifu,Jiang, Qingwei,Yang, Qinghua,Song, Chuanjun,Wang, Ruiyong,Niu, Tianhui,Han, Shengna,Zhang, Lirong,Wu, Jie,Guo, Feima,Zhao, Renbin,Yu, Wenquan,Chai, Jijie,Chang, Junbiao
, p. 7341 - 7348 (2015/10/05)
N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide (N-CDPCB, 1a) is found to be an inhibitor of the fat mass and obesity associated protein (FTO). The crystal structure of human FTO with 1a reveals a novel binding site for the FTO inhibitor and defines the molecular basis for recognition by FTO of the inhibitor. The identification of the new binding site offers new opportunities for further development of selective and potent inhibitors of FTO, which is expected to provide information concerning novel therapeutic targets for treatment of obesity or obesity-associated diseases.
UREA COMPOUNDS AS GAMMA SECRETASE MODULATORS
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Page/Page column 75, (2010/01/29)
The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
