1354810-75-5

Upstream product

• 1354817-59-6 C₂₂H₂₀BrNO₂ 
• 1354817-60-9 C₂₂H₂₁BrN₂O₂ 
• 14047-29-1 4-carboxyphenylboronic acid 
• 1354817-58-5 C₂₁H₁₈BrNO₂ 
• 1354817-57-4 C₂₂H₂₀BrNO₂ 
• 1354810-20-0 (S)-3-(4-bromo-phenyl)-N-methoxy-N-methyl-3-o-tolyl-propionamide 
• 1354808-43-7 3-(4-bromophenyl)-3-o-tolylpropanoic acid 
• 1354808-42-6 ethyl 3-(4-bromophenyl)-2-cyano-3-o-tolylpropanoate 
• 42205-33-4 ethyl 3-(4-bromophenyl)-2-cyanoacrylate 
• 1122-91-4 4-bromo-benzaldehyde 
• 1354810-74-4 4'-[3-[(E)-hydroxyimino]-3-(1-methyl-6-oxo-1,6-dihydro-pyridin-3-yl)-1-o-tolyl-propyl]-biphenyl-4-carboxylic acid 

Relevant academic research and scientific papers

Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists

A series of non-steroidal GPBAR1 (TGR5) agonists was developed from a hit in a high-throughput screening campaign. Lead identification efforts produced biphenyl-4-carboxylic acid derivative (R)-22, which displayed a robust secretion of PYY after oral administration in a degree that can be correlated with the unbound plasma concentration. Further optimisation work focusing on reduction of the lipophilicity provided the 1-phenylpiperidine-4-carboxylic acid derivative (R)-29 (RO5527239), which showed an improved secretion of PYY and GLP-1, translating into a significant reduction of postprandial blood glucose excursion in an oral glucose tolerance test in DIO mice.

1-HYDROXYIMINO-3-PHENYL-PROPANES

This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBA