Back to results
US 11,629,125 B2Granted
Elimination of hepatitis b virus with antiviral agents
AssigneeEmory University
InventorsRaymond F. Schinazi, Sebastien Boucle, Franck Amblard, Ozkan Sari, Leda Bassit
Life of this patent
Estimating the term…
Abstract
The present invention is directed to compounds, compositions and methods for preventing, treating or curing Hepatitis B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV infection.
Claims9
A compound of the following formula:
- or a pharmaceutically acceptable salt thereof, wherein
- when R1 and R1′ are attached to a carbon, they are, independently, hydrogen, halogen, SF5, CF3, hydroxy, N(R′)S(O)2R′, S(O)2R′, S(O)2N(R′)2, C1-6 alkoxy, C1-6 haloalkoxy, C2-6 alkenyl, cyano, C2-6 alkynyl, C3-6 alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, C1-6 alkyl, arylalkoxycarbonyl, carboxy, C1-6 haloalkyl, heterocyclylalkyl, or C1-6 hydroxyalkyl;
- when R1 and R1′ are attached to a nitrogen, they are, independently, hydrogen, C2-6 alkoxy, C3-6 alkoxyalkyl, C2-6 alkenyl, alkoxycarbonyl, carbonylalkyl, carbonyl aryl, C1-6 alkyl, heterocyclylalkyl, C2-6 hydroxyalkyl, or S(O)2R′;
- each R′ is independently H, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, aryl, heteroaryl, alkylaryl, or arylalkyl, or if two R′ reside on the same nitrogen atom, they can come together to form a C3-6 ring optionally containing a N, O, or S heteroatom;
- the R′ groups, other than H, can optionally be substituted with one or more substituents, which substituents are, independently, halo, C1-6 haloalkyl, C1-6 hydroxyalkyl, hydroxyl, carboxyl, acyl, aryl, acyloxy, amino, amido, carboxyl derivatives, alkylamino, dialkylamino, arylamino, alkoxy, alkoxyalkyl, aryloxy, nitro, cyano, sulfonic acid, thiol, imine, sulfonyl, sulfanyl, sulfinyl, sulfamonyl, ester, carboxylic acid, amide, phosphonyl, phosphinyl, phosphoryl, phosphine, thioester, thioether, acid halide, anhydride, oxime, hydrazine, carbamate, phosphonic acid, or phosphonate;
- u and v are independently 0, 1, 2, 3, 4 or 5;
- K is a six-membered heteroaromatic ring containing one, two, or three nitrogen atoms, a five-membered heteroaromatic ring containing one, two, or three heteroatoms which are, independently, N, O, or S;
- or a C4-14 bicyclic ring;
- L is a five-membered heteroaromatic ring containing one, two, or three heteroatoms which are, independently, N, O, or S,
- W is
- R14 is H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, or C2-6 alkynyl,
- R15 is C1-6 alkyl, C1-6 haloalkyl, C2-8 alkoxyalkyl, a six-membered ring or a six-membered bridged or spiro-fused ring containing zero, one, or two heteroatoms which are, independently, N, O, or S, a seven-membered bridged or spiro-fused ring containing zero, one, or two heteroatoms which are, independently, N, O, S, or Se, a five-membered ring containing zero, one, or two heteroatoms which are, independently, N, O, S or Se;
- a four-membered ring containing zero, one, or two heteroatoms which are, independently, N, O, S, or Se;
- R15 is optionally substituted with one or more substituents which are, independently, halogen, SF5, CF3, hydroxy, N(R′)S(O)2R′, S(O)2R′, S(O)2N(R′)2, C1-6 alkoxy, C1-6 haloalkoxy, cyano, azido, C2-6 alkynyl, C3-6 alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, C1-6 alkyl, cycloalkyl, arylalkoxycarbonyl, carboxy, C1-6 haloalkyl, heterocyclylalkyl, or C1-6 hydroxyalkyl;
- or is optionally substituted with aryl, substituted aryl, heteroaryl, or substituted heteroaryl, where substituents on the substituted aryl and substituted heteroaryl are selected from the group consisting of halogen, SF5, CF3, hydroxy, N(R′)S(O)2R′, S(O)2R′, S(O)2N(R′)2, C(O)R′, C1-6 alkoxy, cyano, azido, C2-6 alkynyl, C3-6 alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, and C1-6 alkyl, or
- R14 and R15 can come together with the nitrogen to which they are attached form a 6-10 membered bicyclic or bridged ring or a 3 to 8 membered saturated ring;
- such bicyclic, bridged and saturated ring moiety optionally containing one or more additional heteroatoms which are, independently, O, S or N, and optionally being substituted with one or more substituents each independently selected from the group consisting of halogen, CF3, hydroxy, N(R′)S(O)2R′, S(O)2R′, S(O)2N(R′)2, C1-6 alkoxy, cyano, azido, C2-6 alkynyl, C3-6 alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, C1-6 alkyl, arylalkoxycarbonyl, carboxy, C1-6 haloalkyl, heterocyclylalkyl, and C1-6 hydroxyalkyl.
14 more elements
Dependencies are inferred from the claim text.