- Novel method for synthesis of compound 1-cyclopropyl-1-cyano-4-cyclohexanone
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The invention discloses a novel method for synthesis of a compound 1-cyclopropyl-1-cyano-4-cyclohexanone. The method comprises that p-toluenesulfonylmethyl isocyanide and a compound 1, 4-dioxospiro[4, 5]decane-8-one shown in the formula 1 undergo a reacti
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Paragraph 0028; 0029; 0030
(2017/05/19)
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- Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
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Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 were optimized to account for liabilities relating to in vitro pharmacokinetics, cytotoxicity and protein-related shifts in potency. A representative compound showing favorable in vivo pharmacokinetics was found to be an efficacious inhibitor of 11β-HSD1 in a rat pharmacodynamic model (ED50 = 10 mg/kg).
- McMinn, Dustin L.,Rew, Yosup,Sudom, Athena,Caille, Seb,DeGraffenreid, Michael,He, Xiao,Hungate, Randall,Jiang, Ben,Jaen, Juan,Julian, Lisa D.,Kaizerman, Jacob,Novak, Perry,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Wang, Zhulun,Powers, Jay P.
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scheme or table
p. 1446 - 1450
(2010/01/16)
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- Benzamide derivatives and uses related thereto
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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.
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Page/Page column 43
(2008/06/13)
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