915296-75-2

Upstream product

• 14205-39-1 methyl 3-aminocrotonate 
• 874-42-0 2,4-dichlorobenzaldeyhde 
• 915296-73-0 ethyl 2-(chloromethyl)-4-(2,4-dichlorophenyl)-5-(2-methoxy-2-oxoethyl)-6-methyl-1,4-dihydropyridine-3-carboxylate 
• 915296-74-1 3-ethyl 5-methyl 2-(chloromethyl)-4-(2,4-dichlorophenyl)-6-methylpyridine-3,5-dicarboxylate 
• 62-53-3 aniline 

Downstream Products

• 915296-76-3 3-(chloromethyl)-4-(2,4-dichlorophenyl)-2,7-dimethyl-6-phenyl-6,7-dihydropyrrolo[3,4-b]pyridin-5-one 
• 915297-28-8 C₂₁H₁₆Cl₂N₂O₂ 
• 915297-29-9 C₂₁H₁₄Cl₂N₂O₃ 

Relevant academic research and scientific papers

Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b] pyridin-6(7H)-yl)-N, N-dimethylacetamide (BMS-767778)

Optimization of a 5-oxopyrrolopyridine series based upon structure-activity relationships (SARs) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series and characterization of 2s are described.

Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods

Compounds are provided having the formula (I) wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.