55432-23-0Relevant academic research and scientific papers
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
METALLOENZYME INHIBITOR COMPOUNDS
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Paragraph 1590; 1591; 1592; 1593, (2018/07/29)
Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
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Paragraph 0476, (2017/01/23)
This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
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Paragraph 0549-0550, (2017/09/19)
The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
QUINAZOLINE BASED RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
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Page/Page column 49; 50, (2015/05/19)
Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.
RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
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Page/Page column 18, (2015/05/19)
Compounds of Formula (I): wherein R1, R2 and R3 are defined herein, are useful as inhibitors of RSV.
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
supporting information, 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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Page/Page column 89, (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.
Identification of novel HDAC inhibitors through cell based screening and their evaluation as potential anticancer agents
Wang, Tong,Sepulveda, Mario,Gonzales, Paul,Gately, Stephen
, p. 4790 - 4793 (2013/09/02)
A series of benzimidazole based HDAC inhibitors have been rationally designed, synthesized and screened. The SAR of this new chemotype is described. The lead compound, 11e, showed strong activity in several cellular assays and demonstrated in vivo efficacy in mouse xenograft pancreatic cancer models.
4-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS
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Page/Page column 25, (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.
