- SUBSTITUTED IMIDAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS
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Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
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Paragraph 0313-0315
(2015/02/25)
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- C-H functionalization/C-N bond formation: Copper-catalyzed synthesis of benzimidazoles from amidines
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(Chemical Equation Presented) Copper closes the ring: Benzimidazoles are synthesized from amidines through a copper-catalyzed C-H functionalization/ C-N bond-forming process. The method tolerates a broad range of functional groups and provides the benzimidazoles in up to 89% yield. Best results are obtained by using 15 mol% Cu(OAc)2, 2-5 equivalents of HOAc as additive, and oxygen as the stoichiometric reoxidant (see scheme).
- Brasche, Gordon,Buchwald, Stephen L.
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p. 1932 - 1934
(2008/12/22)
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- Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity
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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.
- 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
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p. 2706 - 2711
(2008/12/20)
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- Ion Channel Modulators
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The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
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Page/Page column 54
(2010/11/29)
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- ION CHANNEL MODULATORS
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The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel fu
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Page/Page column 52-53
(2010/02/14)
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- 2,3-Diaryl-5-anilino[1,2,4]thiadiazoles as melanocortin MC4 receptor agonists and their effects on feeding behavior in rats
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The melanocortin-4 receptor (MC4) modulates physiological functions such as feeding behavior, nerve regeneration, and drug addiction. Using a high throughput screen based on 125I-NDP-MSH binding to the human MC4 receptor, we discovered 2,3-diar
- Pan, Kevin,Scott, Malcolm K.,Lee, Daniel H. S.,Fitzpatrick, Louis J.,Crooke, Jeffery J.,Rivero, Ralph A.,Rosenthal, Daniel I.,Vaidya, Anil H.,Zhao, Boyu,Reitz, Allen B.
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p. 185 - 192
(2007/10/03)
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