1224640-13-4Relevant articles and documents
Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists
Chen, Wei-Dong,Fu, Yajie,Hou, Ruifang,Li, Yunfu,Wang, Chenwei,Wang, Jie,Wang, Le,Wang, Yan-Dong,Yang, Dongbin,Zhao, Shizhen,Zheng, Shaowei
, p. 3618 - 3629 (2022/02/11)
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
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists
Zhao, Shizhen,Li, Xinping,Wang, Le,Peng, Wenjing,Ye, Wenling,Li, Weiguo,Wang, Yan-Dong,Chen, Wei-Dong
, (2021/01/18)
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
2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)
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
, p. 569 - 576 (2013/08/22)
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
NON-SYSTEMIC TGR5 AGONISTS
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, (2013/07/05)
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.
4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS
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, (2011/08/04)
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.
4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS
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, (2011/08/08)
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.
NOVEL PHENYL AMIDE OR PYRIDYL AMIDE DERIVATIVES
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Page/Page column 48, (2010/05/13)
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.