Anti-influenza compositions and methods

摘要

Disclosed are novel compounds comprising an imino-ribose derivative covalently linked to a carbocycle or heterocycle. Pharmaceutical compositions comprising the compounds of the invention are also described. Methods of inhibition, treatment and/or suppression of viral infections with the compounds of the invention are also described. The compositions or methods may optionally comprise one or more additional anti-viral agents.

主权项

1. A compound of formula I: wherein R1 is selected from R2 is a bond, O, or S; R3 is a bond, C(═O), C(═S), C(═NR10), OC(═O), OC(═S), OC(═NR10), N(R11)C(═O), N(R11)C(═S), or N(R11)C(═NR10); R4 is OH or N(R15)2; R5 is H or N(R15)2; R6 is R11, C(═O)—R11, or SO2—R11; R7 is H or R12, wherein R12 is optionally substituted with one or more groups selected from lower alkyl, OR11, O—C(═O)—R11, O—C(═O)O—R11, O—C(═O)N(R11)2, O—C(═S)—R11, O—C(═S)O—R11, and O—C(═S)N(R11)2; R8 is OR11, O—C(═O)—R11, O—C(═O)O—R11, O—C(═O)N(R11)2, O—C(═S)—R11, O—C(═S)O—R11, O—C(═S)N(R11)2, N(R11)2, N(R11)C(═O)—R11, N(R11)C(═O)O(R11)2, N(R11)C(═O)N(R11)2, N(R11)C(═S)—R11, N(R11)C(═S)O—R11, N(R11)C(═S)N(R11)2, or N(R11)C(═NR10)N(R11)2; R9 is H, OH, O—C(═O)O—R11, O—C(═O)N(R11)2, O—C(═S)—R11, O—C(═S)O—R11, O—C(═S)N(R11)2; B is a bond, R12, R12—R13, R12—R13—R14, R12—O—R13, R12—S—R13, R12—N(R11)2—R13, R12—C(═O)—R13, R12—C(═S)—R13, R12—C(═NR10)—R13, R12—OC(═O)—R13, R12—OC(═S)—R13, R12—OC(═NR10)—R13, R12—SC(═O)—R13, R12—SC(═S)—R13, R12—SC(═NR10)—R13, R12—N(R11)C(═O)—R13, R12—N(R11)C(═S)—R13, R12—N(R11)C(═NR10)—R13, R12—OC(═O)—OR13, R12—OC(═S)—OR13, R12—OC(═NR10)—OR13, R12—OC(═O)—N(R11)R13, R12—OC(═S)—N(R11)R13, R12—OC(═NR10)—N(R11)R13, R12—OC(═O)—SR13, R12—OC(═S)—SR13, R12—OC(═NR10)—SR13, R12—N(R11)C(═O)—OR13, R12—N(R11)C(═S)—OR13, R12—N(R11)C(═NR10)—OR13, R12—N(R11)C(═O)—N(R11)R13, R12—N(R11)C(═S)—N(R11)R13, R12—N(R11)C(═NR10)—N(R11)R13, R12—N(R11)C(═O)—SR13, R12—N(R11)C(═S)—SR13, R12—N(R11)C(═NR10)—SR13, R12—SC(═O)—OR13, R12—SC(═S)—OR13, R12—SC(═NR10)—OR13, R12—SC(═O)—SR13, R12—SC(═S)—SR13, R12—SC(═NR10)—SR13, R12—SC(═O)—N(R11)R13, R12—SC(═S)—N(R11)R13, or R12—SC(═NR10)—N(R11)R13; wherein each R12, R13, and R14 are optionally substituted with one or more R15; R10 is independently H, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl, OR11, or N(R11)2; R11 is independently H, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, or heteroaryl; R12 is independently lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, or heteroaryl; R13 is independently lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, or heteroaryl; R14 is independently lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, or heteroaryl; and R15 is independently halogen, R10, OC(═O)R11, OC(═S)R11, OC(═NR10)R11, OC(═O)OR11, OC(═S)OR11, OC(═NR10)OR11, OC(═O)N(R11)2, OC(═S)N(R11)2, OC(═NR10)N(R11)2, N(R11)C(═O)R11, N(R11)C(═S)R11, N(R11)C(═NR10)R11, N(R11)C(═O)OR11, N(R11)C(═S)OR11, N(R11)C(═NR10)OR11, N(R11)C(═O)N(R11)2, N(R11)C(═S)N(R11)2, or N(R11)C(═NR10)N(R11)2; or a pharmaceutically acceptable salt thereof.