- Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays
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A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identification process, leading us to focus on a 6,5,7-tricyclic scaffold. A subsequent early SAR investigation provided potent agonists of the 5-HT2C receptor that were highly selective in both functional and binding assays, had good rat PK properties and that significantly reduced acute food intake in the rat.
- Dang, Huong,Feichtinger, Konrad,Frazer, John,Grottick, Andrew J.,Kasem, Michelle,Le, Minh,Lehman, Juerg,Morgan, Michael E.,Ren, Albert,Sage, Carleton R.,Schrader, Thomas O.,Semple, Graeme,Unett, David J.,Whelan, Kevin T.,Wong, Amy,Zhu, Xiuwen
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supporting information
(2020/01/22)
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- Microwave-assisted synthesis of benzo-[1,4]-oxazinones using MeO-PEG-OMe as solvent
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Efficient one-pot microwave-assisted synthesis of various benzo-[1,4]-oxazinones via Smiles rearrangement is described. Treatment of 2-chloroacetamide, substituted 2-chlorophenols and cesium carbonate in MeO-PEG-OMe (2,000) as solvent afforded the corresp
- Lim, Jae-Min,Gam, Gyunghee,Kim, Shin-Hyuong,Shin, Dong-Soo,Jang, Kiwan
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p. 468 - 472,5
(2020/08/31)
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- Morpholine derivatives
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The disclosure relates to new morpholine derivatives which possess antidepressant activity, to processes for the manufacture of said derivatives and to pharmaceutical compositions containing them. Typical of the morpholine derivatives disclosed is 2-(4H-2
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