887950-87-0Relevant articles and documents
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
supporting information; experimental part, p. 5577 - 5582 (2011/10/09)
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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Page/Page column 51, (2010/11/03)
The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists
Xu, Ruo,Li, Shengjian,Paruchova, Jaroslava,McBriar, Mark D.,Guzik, Henry,Palani, Anandan,Clader, John W.,Cox, Kathleen,Greenlee, William J.,Hawes, Brian E.,Kowalski, Timothy J.,O'Neill, Kim,Spar, Brian D.,Weig, Blair,Weston, Daniel J.
, p. 3285 - 3299 (2007/10/03)
Melanin concentrating hormone (MCH) receptor antagonists have been proposed as potential treatments of obesity. MCH receptor antagonists with a biphenylamine subunit have been reported previously at Schering-Plough. Herein, we report the discovery of bicy