2387-08-8Relevant academic research and scientific papers
PYRROLOPYRAZINE KINASE INHIBITORS
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Page/Page column 187; 188, (2013/03/28)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists
Shimada, Itsuro,Maeno, Kyoichi,Kazuta, Ken-ichi,Kubota, Hideki,Kimizuka, Tetsuya,Kimura, Yasuharu,Hatanaka, Ken-ichi,Naitou, Yuki,Wanibuchi, Fumikazu,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
, p. 1966 - 1982 (2008/09/21)
A series of novel indazole derivatives were synthesized, and their structure-activity relationships examined in order to identify potent and selective 5-HT2C receptor agonists. Among these compounds, (S)-2-(7-ethyl-1H-furo[2,3-g]indazol-1-yl)-1-methylethylamine (YM348) had a good in vitro profile, that is, high agonistic activity to the human 5-HT2C receptor subtype (EC50 = 1.0 nM) and high selectivity over 5-HT2A receptors. This compound was also effective in a rat penile erection model when administered po.
CYCLIC AMIDINES USEFUL AS NMDA NR2B ANTAGONISTS
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, (2008/06/13)
The invention encompasses novel compounds of Formula I as well as a method of treating NMDA mediated diseases comprising administration to a patient in need of such treatment a non-toxic amount of a compound of Formula I effective to block the NMDA NR2B r
Transition metal catalysed cross-coupling between benzylic halides and aryl nucleophiles. Synthesis of some toxicologically interesting tetrachlorobenzyltoluenes
De Lang, Robbert-Jan,Van Hooijdonk, Marcel J.C.M.,Brandsma, Lambert,Kramer, Hester,Seinen, Willem
, p. 2953 - 2966 (2007/10/03)
The aryl-benzyl cross-coupling in the presence of copper-, nickel- and palladium-catalysts has been investigated with a number of chlorine- and methyl-substituted arylmetal compounds ArM (M = MgBr, ZnCl) and (substituted) benzylic halides ArCH2X. The results have been applied in the selective synthesis of some toxicologically interesting tetrachlorobenzyltoluenes.
