- Practical and Efficient Synthesis of 2-Thio-imidazole Derivative - ZY12201: A Potent TGR5 Agonist
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Early scalable process development for the synthesis of ZY12201, a novel TGR5 receptor agonist, as a potential clinical candidate is described. A practical, efficient, and scalable synthetic route provided ZY12201 in seven steps and 32% overall yield. The
- Agarwal, Sameer,Chaubey, Vipin,Chauhan, Rakesh,Jain, Sarika,Joshi, Vivek M.,Mande, Hemant,Pamidimukkala, Padmaja Sudhakar,Pandey, Bipin,Sasane, Santosh,Shah, Kalpesh,Shah, Shailesh R.,Shukla, Mrigendra,Singh, Kumar K.,Sojitra, Chandrakant,Soman, Shubhangi
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p. 1508 - 1514
(2020/11/23)
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- Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist
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TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (hTGR5
- Agarwal, Sameer,Patil, Amit,Aware, Umesh,Deshmukh, Prashant,Darji, Brijesh,Sasane, Santosh,Sairam, Kalapatapu V. V. M.,Priyadarsiny, Priyanka,Giri, Poonam,Patel, Harilal,Giri, Suresh,Jain, Mukul,Desai, Ranjit C.
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supporting information
p. 51 - 55
(2016/02/03)
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- 2-THIO-IMIDAZOLE DERIVATIVES AS TGR5 MODULATORS
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The present invention relates to compounds of the general Formula I their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, their N-oxide, metabolites, polymorphs, use of these compounds in medicine for treating diabetes (TGR5 modulators) and the intermediates involved in their preparation.
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Page/Page column 63
(2013/04/25)
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