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Publication Number
US-9676747-B2
Publication Date
2017-06-13
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 is directed to compounds of Formula V, including pharmaceutically acceptable salts thereof, defined by substituent-selection rules for R4, G1, R5, and R2, together with integers n, x, and y. The structure scope allows R4 and G1 to be H or C1-C6 alkyl, and provides independently selected groups for R5 and R2 from specified substituent sets including hydroxyl, halo, cyano, nitro, alkyl, alkoxy, fluoroalkyl, heteroalkyl, and C(O)-C1-C6 alkyl.
The disclosed compounds are illustrated by multiple specific GA-labeled chemical structures that share a sulfonamide-containing core with an aryl amide linkage and substituted cyclic amine or cycloalkyl moieties bearing hydroxyl substituents. The examples include fluorinated and chloro-substituted aryl rings, with halogen substitution patterns such as F, Cl, and Br, and some entries are accompanied by 1H NMR characterization data.
The claim family also extends to compositions including salt, solvate, and N-oxide forms, and to HBV treatment methods using the claimed Formula V compounds. Dependent claims further define combination administration with additional therapeutic agents and include a comparative limitation in which administering the specified compound reduces viral load to a greater extent than administering listed HBV and antiviral agents or combinations thereof.
Claims Coverage
The independent claim is directed to a compound of Formula V (or a pharmaceutically acceptable salt thereof) defined by substituent-selection rules for R4, G1, R5, R2, and the integers n, x, and y. Dependent claims narrow the substituent choices, extend coverage to salt, solvate, and N-oxide forms, and add HBV treatment-related limitations including combination administration and comparative viral-load reduction. The claim set centers on one broad chemical genus with three major claim groups: compound scope, composition forms, and HBV method scope.
Formula V compound with defined substituent-selection rules
A compound of Formula V or a pharmaceutically acceptable salt thereof, wherein R4 is H or C1-C6 alkyl, G1 is H or C1-C6 alkyl, each R5 is independently selected from OH, C1-C6 alkyl, halo, —CN, —NO2, C1-C6 chloroalkyl, —C1-C6 dichloroalkyl, —C1-C6 trichloroalkyl, —C1-C6 fluoroalkyl, —C1-C6 difluoroalkyl, and —C1-C6 trifluoroalkyl, R2 is independently selected from halo, —OH, —CN, —NO2, —C1-C6 alkyl, —C1-C6 alkoxy, —C1-C6 fluoroalkyl, —C1-C6 heteroalkyl, and C(O)—C1-C6 alkyl, n is 1, 2, 3, 4, 5, or 6, x is 0, 1, 2, 3, or 4, and y is 1, 2, or 3.
Composition including salt, solvate, or N-oxide forms
A composition that includes a compound as defined in claim 1 or one of its salt, solvate, or N-oxide forms.
HBV treatment with additional therapeutic agents
A method of treating HBV by administering the Formula V compound, optionally together with one or more additional therapeutic agents selected from specified categories and named HBV-related agents, including BAY 41-4109, AT-61, and AT-130.
Comparative viral-load reduction versus listed alternatives
A method limited so that administering the specified compound reduces an individual's viral load to a greater extent than administering any compound selected from a listed set of HBV and antiviral agents, or any combination thereof.
The inventive coverage is a Formula V compound genus defined by explicit substituent-selection rules, together with compositions covering salt, solvate, and N-oxide forms and HBV treatment methods. The method claims further include combination administration with specified additional therapeutic agents and a comparative viral-load reduction limitation versus listed alternatives.
Stated Advantages
Greater viral-load reduction than administering any compound selected from a listed set of HBV and antiviral agents, or any combination thereof.
Lower mutation/resistance incidence versus specified alternatives.
Reduces viral load.
May modulate cccDNA activity.
Improves seroconversion.
May reduce drug resistance.
Remission of hepatic injury.
Reduced adverse impact of long-term therapy.
Documented Applications
HBV treatment by administering the claimed Formula V compound, including treatment of chronic HBV infection.
HBV combination treatment with additional therapeutic agents selected from specified categories and named agents, including BAY 41-4109, AT-61, and AT-130.
Prophylaxis in the context of HBV infection.
A method aimed at remission of hepatic injury and reduced adverse impact of long-term therapy.
In vitro HBV capsid assembly evaluation using a fluorescence quenching assay readout.
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