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4-Bicyclic heteroaryl-piperidine derivatives as potent,orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs |
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| Authors: | Shyh-Ming Yang Yuting Tang Rui Zhang Huajun Lu Gee-Hong Kuo Michael D. Gaul Yaxin Li George Ho James G. Conway Yin Liang James M. Lenhard Keith T. Demarest William V. Murray |
| Affiliation: | Cardiovascular and Metabolism Research, Janssen Research and Development, LLC, Welsh & McKean Roads, Spring House, PA 19477, USA |
| Abstract: | A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure–activity relationships focused on bicyclic heteroarenes and aminothiazole–urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated. |
| Keywords: | Stearoyl-CoA desaturase SCD1 inhibitors Desaturation index Obesity |
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