778646-95-0

Upstream product

• 1095173-08-2 (2R,4R)-1-tert-butyl 2-methyl 4-azidopiperidine-1,2-dicarboxylate 
• 405229-64-3 (2R,4S)-1-tert-butyl 2-methyl 4-(methylsulfonyloxy)piperidine-1,2-dicarboxylate 
• 321744-26-7 N-Boc-4-hydroxy-2-piperidine carboxylic acid methyl ester 

Downstream Products

• 1095173-19-5 (2R,4R)-1-tert-butyl 2-methyl 4-(3-(4-cyanophenyl)ureido)piperidine-1,2-dicarboxylate 
• 1352568-39-8 (2R,4R)-tert-butyl 2-((2-aminophenyl)carbamoyl)-4-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)piperidine-1-carboxylate 
• 1352568-41-2 C₁₉H₂₆N₂O₆ 
• 1352568-42-3 C₂₅H₃₂N₄O₅ 
• 1352568-43-4 C₂₁H₂₄N₄O₂ 
• 1095173-20-8 (2R,4R)-1-(tert-butoxycarbonyl)-4-(3-(4-cyanophenyl)ureido)piperidine-2-carboxylic acid 
• 1095173-26-4 (2R,4R)-tert-butyl 2-((2-aminophenyl)carbamoyl)-4-(3-(4-cyanophenyl)ureido)piperidine-1-carboxylate 
• 1095173-27-5 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea 
• 1352568-40-1 C₂₀H₂₈N₂O₆ 

Relevant academic research and scientific papers

Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened

Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we describe the discovery strategy to overcome the issues inherent in lead structure 1 that resulted in the identification of Smoothened inhibitor 1-((2R,4R)-2-(1H-benzo[d] imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea (PF-04449913, 26), which has been advanced to human clinical studies.

BENZIMIDAZOLE DERIVATIVES

The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.