| 摘要 |
Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including α-thiomonophosphates, α-thiodiphosphates, and α-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates. |
| 主权项 |
1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: B1 is an optionally substituted purine base or an optionally substituted pyrimidine base; R1 is an optionally substituted N-linked α-amino acid or an optionally substituted N-linked α-amino acid ester derivative; R2 is an optionally substituted aryl; R3a and R3b are independently hydrogen, deuterium or methyl; R4 is hydrogen; R5 is hydrogen; R6 is selected from the group consisting of hydrogen, halogen, —OR12 and —OC(═O)R13; R7 is selected from the group consisting of hydrogen, halogen, —OR14 and —OC(═O)R15;
or R6 and R7 are both oxygen atoms and linked together by a carbonyl group; R8 is selected from the group consisting of hydrogen, halogen and an unsubstituted C1-6 alkyl; R9 is hydrogen; R12 and R14 are independently hydrogen or an unsubstituted C1-6 alkyl; and R13 and R15 are independently an unsubstituted C1-6 alkyl or an unsubstituted C3-6 cycloalkyl; and wherein when a substituent is substituted, the substituent is substituted with a group individually and independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, cycloalkenyl, C6-C10 aryl, 4 to 14 atom heteroaryl, 3 to 18 atom heteroalicyclyl, (aryl)C1-4 alkyl, (heteroaryl)C1-4 alkyl, (heteroalicyclyl) C1-4 alkyl, hydroxy, alkoxy, aryloxy, acyl, cyano, halogen, O-carbamyl, N-carbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, nitro, sulfonyl, haloalkyl, haloalkoxy, an amino, a mono-substituted amino group and a di-substituted amino group. |
