1021435-06-2

Upstream product

• 924271-88-5 ethyl (4R)-4-[(7-bromo-6-methoxyisoquinolin-1-yl)oxy]-1-[(2S)-2-cyclohexyl-2-({[(2,2-dimethylpent-4-en-1-yl)oxy]carbonyl}amino)acetyl]-L-prolinate 
• 914841-18-2 (2S)-cyclohexyl({[(2,2-dimethylpent-4-en-1-yl)oxy]carbonyl}amino)acetic acid 
• 924365-09-3 C₁₇H₁₉BrN₂O₄ 
• 1021435-05-1 ethyl (2R,4S,7S,14E)-7-cyclohexyl-23-methoxy-12,12-dimethyl-6,9-dioxo-3,4,6,7,8,9,12,13-octahydro-2H,11H-16,18-(ethanediylidene)-2,5-methanopyrido[2,3-k][1,10,3,6]dioxadiazacyclononadecine-4-carboxylate 

Downstream Products

• 1021435-07-3 (3R,5S,8S)-8-cyclohexyl-18-methoxy-13,13-dimethyl-7,10-dioxo-2,11-dioxa-6,9,23-triazatetracyclo[15.6.2.1~3,6~.0~20,24~]hexacosa-1⁽²³⁾,17,19,21,24-pentaene-5-carboxylic acid 
• 924270-31-5 C₄₀H₅₃N₅O₉S 

Relevant academic research and scientific papers

Discovery of MK-1220: A macrocyclic inhibitor of hepatitis C virus NS3/4A Protease with Improved Preclinical Plasma Exposure

The discovery of MK-1220 is reported along with the development of a series of HCV NS3/4A protease inhibitors containing a P2 to P4 macrocyclic constraint with improved preclinical pharmacokinetics. Optimization of the P2 heterocycle substitution pattern as well as the P3 amino acid led to compounds with greatly improved plasma exposure following oral dosing in both rats and dogs while maintaining excellent enzyme potency and cellular activity. These studies led to the identification of MK-1220.

HCV NS3 PROTEASE INHIBITORS

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.