618385-83-4

Upstream product

• 618386-45-1 (3R,3aS,4S,4aR,7R,8aS,9aR)-4-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-7-(hydroxymethyl)-3-methyldecahydronaphtho[2,3-c]furan-1(3H)-one 
• 618385-72-1 (3R,3aS,4S,4aR,7R,8aS,9aR)-7-(aminomethyl)-4-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-3-methyldecahydronaphtho[2,3-c]furan-1(3H)-one 
• 109-90-0 ethyl isocyanate 
• 618386-48-4 C₂₇H₂₉FN₄O₂ 
• 618386-47-3 C₂₈H₃₂FNO₅S 
• 618386-46-2 (1R,3aR,4aS,6R,8aR,9S,9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-carbaldehyde 
• 618386-44-0 C₂₈H₃₀FNO₃ 
• 618386-13-3 C₂₆H₂₆FNO₃ 

Relevant academic research and scientific papers

Himbacine-derived thrombin receptor antagonists: C7-aminomethyl and C9a-hydroxy analogues of vorapaxar

We have synthesized several C7-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a from this series showed excellent PAR-1 activity (Ki = 5 nM). We have also synthesized a C9a-hydroxy analogue of vorapaxar, which showed very good PAR-1 affinity (Ki = 19.5 nM) along with excellent rat pharmacokinetic profile and ex vivo efficacy in the cynomolgus monkey.