61779-03-1Relevant academic research and scientific papers
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
Sun, Daqing,Wang, Zhulun,Caille, Seb,Degraffenreid, Michael,Gonzalez-Lopez De Turiso, Felix,Hungate, Randall,Jaen, Juan C.,Jiang, Ben,Julian, Lisa D.,Kelly, Ron,McMinn, Dustin L.,Kaizerman, Jacob,Rew, Yosup,Sudom, Athena,Tu, Hua,Ursu, Stefania,Walker, Nigel,Willcockson, Maren,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 405 - 410 (2011/02/27)
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
Benzamide derivatives and uses related thereto
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Page/Page column 63-64, (2008/06/13)
Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
Butyrophenones as hypotensive agents. Derivatives of 4 aryl 4 (hydroxymethyl)cyclohexylamine
Lednicer,Emmert,Rudzik,Graham
, p. 593 - 599 (2007/10/06)
The preparation of butyrophenone derivatives of 4 aryl 4 (hydroxymethyl) cyclohex 1 ylamines starting from the corresponding 4 cyano 4 phenylcyclohexan 1 ones is described. Substitution was varied in both rings; both isomers of 4 phenyl 4 (hydroxymethyl)cyclohex 1 ylamine were characterized. Those derivatives which carried p fluoro substitution on the butyrophenone exhibited hypotensive activity in the rat with diminished CNS activity compared to compounds lacking the hydroxymethyl group. The effect of substitution on the 4 aryl ring is discussed.
