784181-24-4Relevant academic research and scientific papers
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity
Smith, Roger A.,Fathi, Zahra,Achebe, Furahi,Akuche, Christiana,Brown, Su-Ellen,Choi, Soongyu,Fan, Jianmei,Jenkins, Susan,Kluender, Harold C.E.,Konkar, Anish,Lavoie, Rico,Mays, Ronald,Natoli, Jennifer,O'Connor, Stephen J.,Ortiz, Astrid A.,Su, Ning,Taing, Christy,Tomlinson, Susan,Tritto, Theresa,Wang, Gan,Wirtz, Stephan-Nicholas,Wong, Wai,Yang, Xiao-Fan,Ying, Shihong,Zhang, Zhonghua
, p. 2706 - 2711 (2008/12/20)
Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provided the imidazole 2-hydroxy-cyclohexyl amide 45, which exhibited hCB-1 Ki = 3.7 nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models.
IMIDAZOLE COMPOUNDS AND USES THEREOF
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Page/Page column 49, (2010/02/10)
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the activation of the cannabinoid receptors in animals are described herein.
BICYCLIC PYRIDAZINONE CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
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Page/Page column 54-55, (2010/02/12)
Compounds of Formula (I) and (II) are described herein, as well as their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors (in particular, the CB-1 receptor) in animals.
BICYCLIC IMIDAZOLYL PYRIMIDIN-4-ONE CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
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Page/Page column 50-51, (2010/02/12)
Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.
Cannabinoid receptor ligands and uses thereof
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Page 23, (2008/06/13)
Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
Cannabinoid receptor ligands and uses thereof
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Page 28, (2010/02/09)
Compounds of Formula (I) or (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
