Functionalized heterocycles as antiviral agents
Inventors
Panarese, Joseph D. • Davis, Dexter • Bartlett, Samuel • Chong, Katherine • Kenton, Nathaniel Thomas • Or, Yat Sun
Assignees
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Abstract
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Core Innovation
The invention relates to a pharmaceutical composition comprising a compound selected from a group of depicted compounds, or a pharmaceutically acceptable salt or ester thereof, together with a pharmaceutically acceptable carrier or excipient. The depicted compounds are represented by multiple chemical structure depictions and associated structure files, and include heteroaromatic, heterocyclic, bicyclic, and fused ring scaffold variants with variable substituents, heteroatoms such as nitrogen, oxygen, and sulfur, and wavy bond attachment points.
The disclosure includes substituted pyrazolo[1,5-a]pyrido[2,2-c]pyrazine-12-carboxylic acid derivatives, pyrazolo[1,5-a]pyrido[2,1-c]pyrazine-9-carboxylic acid derivatives, Formula (X-1), Formula (I), Formula (X-4), Formula (XI-1), Formula (XI-2), Formula (XI-3), Formula (XI-4), Formula (XI-5), Formula (XI-6), Formula (XI-7), Formula (XI-8), Formula (X-3), Formula (X-5), Formula (X-6), Formula (X-7), Formula (X-8), and related compound groups. Across the examples, the structures include halogen and fluorinated substituents such as fluorine, chlorine, CF3, difluoro, trifluoromethoxy, CN, OH, amino, ether, amide-like motifs, aryl, and heteroaryl groups.
The claim context links the selected compound compositions to therapeutic use in treating hepatitis B virus infection. The compositions are described for administration of a therapeutically effective amount to a subject, and some content also states uses for treating and preventing HBV infection or HBV life-cycle inhibition.
Claims Coverage
The consolidated claim coverage centers on one independent pharmaceutical composition claim, with dependent claims that refine the selected depicted compound and add hepatitis B virus treatment language. In total, the claim set covers a selected compound from a depicted group, its pharmaceutically acceptable salt or ester, and a pharmaceutically acceptable carrier or excipient, with method claims directed to administration for hepatitis B virus infection. The consolidated inventive features reduce to 3 main elements.
Pharmaceutical composition with selected depicted compound and carrier or excipient
A pharmaceutical composition comprising a compound selected from a depicted group, or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier or excipient.
Specific depicted compound selection with salt or ester
The pharmaceutical composition includes a specified depicted compound and its pharmaceutically acceptable salt or ester.
Treatment of hepatitis B virus infection by administering a therapeutically effective amount
A method for treating hepatitis B virus infection in a subject by administering a therapeutically effective amount of the pharmaceutical composition.
Overall, the claims cover a pharmaceutical composition defined by selection from depicted compound groups, including pharmaceutically acceptable salts or esters, formulated with a pharmaceutically acceptable carrier or excipient. Dependent claims further narrow the specific depicted compound and recite treatment of hepatitis B virus infection by administering a therapeutically effective amount of the composition.
Stated Advantages
Provides a composition and method for treating hepatitis B virus infection in a subject by administering a therapeutically effective amount.
Antiviral activity by inhibiting and/or interfering with hepatitis B virus (HBV) proteins or HBV life-cycle processes.
Provides pharmaceutical composition forms suitable for treating and preventing HBV infection.
Documented Applications
Treating hepatitis B virus infection in a subject by administering a therapeutically effective amount of the pharmaceutical composition.
Preventing HBV infection.
HepG2 antiviral activity assay with HBsAg and HBeAg readouts, with activity summarized using EC50 and CC50.
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