178035-47-7Relevant academic research and scientific papers
Asymmetric synthesis of cis-(-)-(2R4S)-4-(phosphonomethyl)-2-piperidinecarboxylic acid, a potent NMDA receptor antagonist
Skiles, Jerry W.,Giannousis, Peter P.,Fales, Kevin R.
, p. 963 - 966 (1996)
The asymmetric synthesis of cis-(-)-(2R4S)-4-(phosphononomethyl)-2-piperidinecarboxylic acid (1), a potent and specific NMDA receptor antagonist, via an olefin-iminium cyclization is described.
Preparation method of griseine key intermediate
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Paragraph 0023-0024; 0033-0038, (2021/09/29)
The preparation method comprises S1, sequentially adding 4A molecular sieve, acetonitrile and a compound shown in structural formula 1 into acrylic acid, performing a Diels - Alder reaction, and obtaining an intermediate product. TLC A neutralization reag
Structure guided design of a series of sphingosine kinase (SphK) inhibitors
Gustin, Darin J.,Li, Yihong,Brown, Matthew L.,Min, Xiaoshan,Schmitt, Mike J.,Wanska, Malgorzata,Wang, Xiaodong,Connors, Richard,Johnstone, Sheere,Cardozo, Mario,Cheng, Alan C.,Jeffries, Shawn,Franks, Brendon,Li, Shyun,Shen, Shanling,Wong, Mariwil,Wesche, Holger,Xu, Guifen,Carlson, Timothy J.,Plant, Matthew,Morgenstern, Kurt,Rex, Karen,Schmitt, Joanna,Coxon, Angela,Walker, Nigel,Kayser, Frank,Wang, Zhulun
, p. 4608 - 4616 (2013/08/15)
Sphingosine-1-phosphate (S1P) signaling plays a vital role in mitogenesis, cell migration and angiogenesis. Sphingosine kinases (SphKs) catalyze a key step in sphingomyelin metabolism that leads to the production of S1P. There are two isoforms of SphK and observations made with SphK deficient mice show the two isoforms can compensate for each other's loss. Thus, inhibition of both isoforms is likely required to block SphK dependent angiogenesis. A structure based approach was used to design and synthesize a series of SphK inhibitors resulting in the identification of the first potent inhibitors of both isoforms of human SphK. Additionally, to our knowledge, this series of inhibitors contains the only sufficiently potent inhibitors of murine SphK1 with suitable physico-chemical properties to pharmacologically interrogate the role of SphK1 in rodent models and to reproduce the phenotype of SphK1 (-/-) mice.
ISOQUINOLINONE DERIVATIVES
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Page/Page column 139, (2010/04/27)
The present invention relates to isoquinolinone derivatives of formula (I): wherein are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
