- Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists
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TGR5 is emerging as an important and promising target for the treatment of non-alcoholic steatohepatitis, type 2 diabetes mellitus (T2DM), and obesity. A series of novel 3-phenoxypyrazine-2-carboxamide derivatives were designed, synthesized and evaluated
- Chen, Wei-Dong,Fu, Yajie,Hou, Ruifang,Li, Yunfu,Wang, Chenwei,Wang, Jie,Wang, Le,Wang, Yan-Dong,Yang, Dongbin,Zhao, Shizhen,Zheng, Shaowei
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p. 3618 - 3629
(2022/02/11)
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- Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists
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TGR5 is emerging as an important and promising target for the treatment of diabetes, obesity and other metabolic syndromes. A series of novel 1-benzyl-1H-imidazole-5-carboxamide derivatives was designed, synthesized and evaluated in vitro and in vivo. The
- Zhao, Shizhen,Li, Xinping,Wang, Le,Peng, Wenjing,Ye, Wenling,Li, Weiguo,Wang, Yan-Dong,Chen, Wei-Dong
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- NON-SYSTEMIC TGR5 AGONISTS
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Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
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Page/Page column 90
(2013/07/05)
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- 2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)
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Potency with potential: 2-Phenoxy- nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type2 diabetes and metabolic syndrome. Extensive structure-activity relationship studies supported by homolog
- Martin, Rainer E.,Bissantz, Caterina,Gavelle, Olivier,Kuratli, Christoph,Dehmlow, Henrietta,Richter, Hans G. F.,ObstSander, Ulrike,Erickson, Shawn D.,Kim, Kyungjin,Pietranico-Cole, Sherrie Lynn,Alvarez-Sanchez, Ruben,Ullmer, Christoph
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supporting information
p. 569 - 576
(2013/08/22)
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- 4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS
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This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
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Page/Page column 24
(2011/08/04)
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- 4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS
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This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula (I), wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
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Page/Page column 53
(2011/08/08)
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- NOVEL PHENYL AMIDE OR PYRIDYL AMIDE DERIVATIVES
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This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
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Page/Page column 48
(2010/05/13)
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