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US 2015/0307443 A1Published application
Functionalized benzamide derivatives as antiviral agents against hbv infection
AssigneesBaruch S. Blumberg Institute, Drexel University
InventorsXIAODONG XU, TIMOTHY M. BLOCK, JU-TAO GUO, YANMING DU
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Abstract
Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, and are useful for the treatment of Hepatitis B virus (HBV) infection.
Claims21
A compound of formula (I), or a hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof:
- , wherein in (I):
- X is selected from the group consisting of CH and S;
- A is selected from the group consisting of hydrogen and C1-4 alkyl;
- R1 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, optionally substituted C1-4 alkenyl, CO2R8, CONHR9, NHCOR10, and OR11;
- or R1 and A are taken together with the atom to which they are bound to form an optionally substituted ring having 5-7 ring atoms;
- R2 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, optionally substituted C1-4 alkenyl, NHCOR10, and OR11;
- or R1 and R2 are taken together with the atom to which they are bound to form an optionally substituted ring having 5-7 ring atoms optionally containing one or two atoms independently selected from the group consisting of oxygen, sulfur and nitrogen;
- R3 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, and optionally substituted C1-4 alkenyl;
- or R2 and R3 are taken together with the atom to which they are bound to form an optionally substituted ring having 5-7 ring atoms;
- R4 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, and OR11;
- R5 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, and OR11;
- R6 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, and OR11;
- R7 is selected from the group consisting of hydrogen, halogen, optionally substituted C1-4 alkyl, and OR11;
- R8 is selected from the group consisting of hydrogen, optionally substituted C1-4 alkyl, and optionally substituted C3-7 cycloalkyl;
- R9 is selected from the group consisting of hydrogen, optionally substituted C1-4 alkyl, and optionally substituted C3-7 cycloalkyl;
- R10 is selected from the group consisting of hydrogen, optionally substituted C1-4 alkyl, and optionally substituted C3-7 cycloalkyl;
- R11 is selected from the group consisting of hydrogen, optionally substituted C1-4 alkyl, and optionally substituted C3-7 cycloalkyl;
- m is 0 or 1;
- and
- n is 0 or 1.
17 more elements
Dependencies are inferred from the claim text.