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Publication Number
US-8629274-B2
Publication Date
2014-01-14
Expiration Date
Abstract
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Core Innovation
The invention concerns compounds of Formula IVc, or pharmaceutically acceptable salts thereof. The compounds are defined by structural constraints in which X is halo, G1 is halo, G2 is C1-C4 alkyl, or halo, and G4 is H, halo, C1-C4 alkyl, or OH. The disclosed structures include substituted sulfonamide-containing aromatic amide compounds with halogen substitution patterns and, in some embodiments, an OH-bearing cyclic amine or cycloalkyl ring.
The disclosure provides specific chemical structures within the Formula IVc scaffold, including examples with F, Cl, and Br substituents on aromatic rings and a sulfonyl or sulfonamide motif linked through an NH-containing amide or anilide-type connection. Representative structures are shown with varying ring substitution patterns, including hydroxyl substituents and other allowed forms within the Formula IVc framework. Some entries are accompanied by 1H NMR characterization data.
The compound examples are presented as labeled GA or numbered compounds consistent with the Formula IVc structural definition. The disclosure maintains the common Formula IVc core while varying halo and alkyl substituents and permitting pharmaceutically acceptable salt forms. The overall subject matter centers on concrete embodiments of the defined scaffold rather than a separate biological or therapeutic system.
Claims Coverage
The claim coverage centers on one independent claim directed to compounds of Formula IVc, or pharmaceutically acceptable salts thereof. The independent claim contains four principal inventive structural features, defined by the allowed values of X, G1, G2, and G4.
Formula IVc compound with defined substituent constraints
A compound of Formula IVc or a pharmaceutically acceptable salt thereof, wherein X is halo; G1 is halo; G2 is C1-C4 alkyl, or halo; and G4 is H, halo, C1-C4 alkyl, or OH.
Specific depicted Formula IVc embodiment
The compound is the specific compound of Formula IVc (or a pharmaceutically acceptable salt thereof) as shown in the depicted chemical structure.
Pharmaceutical composition with carrier
A pharmaceutical composition including a compound according to the claim (or its salt, solvate, or N-oxide) together with at least one pharmaceutically acceptable carrier.
Overall, the claims are directed to Formula IVc compounds defined by halo, alkyl, and hydroxyl substitution constraints at X, G1, G2, and G4, with dependent coverage tied to depicted Formula IVc structures. The claim set also extends to pharmaceutically acceptable salts and, in at least one dependent claim, to pharmaceutical compositions including carriers and additional salt, solvate, or N-oxide forms.
Stated Advantages
Suitability for monotherapy.
Potential effectiveness against drug-resistant HBV strains.
Rationale for cross-class combination regimens involving polymerase inhibitors, interferon including pegylated interferon, viral entry inhibitors, and TLR agonists.
Documented Applications
Inhibiting, suppressing, or preventing hepatitis B virus (HBV) infection by administering therapeutically effective amounts of compounds of the invention.
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