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US 11,078,170 B2Granted
Cyclic sulfamide compounds and methods of using same
AssigneeAssembly Biosciences, Inc.
InventorsWilliam W. Turner, Jr., Leping Li, Simon Nicolas Haydar, Mark G. Bures, Roopa Rai, Samson Francis, Lee D. Arnold
Life of this patent
Estimating the term…
Abstract
The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
Claims35
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- w is 2;
- R1 is of phenyl or pyridyl, each or which is optionally substituted with one, two, or three substituents independently selected from the group consisting of halo, —OH, —CN, —NO2, oxo, hydrazino, formyl, azido, silyl, siloxy, —S(O)q—C1-6alkyl, —NRc—S(O)t—C1-6alkyl, —S(O)t—NRaRb, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, haloC1-6alkyl, hydroxyC1-6alkyl, RaRbN—C1-6alkyl-, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy-, RaRbN—C1-6alkoxy-, C1-6alkoxyC1-6alkyl, —C(O)NRaRb, —C(O)—C1-6alkyl, —C(O)OH, and —C(O)O—C1-6alkyl;
- R2 is hydrogen;
- R3 is selected from the group consisting of:
- wherein:
- R4 is hydrogen or C1-6alkyl optionally substituted with one, two, or three substituents independently selected from the group consisting of:
- halogen, —OH, —CN, —S(O)q—C1-6alkyl, —NRaRb—NRc—S(O)t—C1-6alkyl, —S(O)t—NRaRb, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, —C(O)NRaRb, —C(O)—C1-6alkyl, formyl, —C(O)OH, —C(O)O—C1-6alkyl, benzyloxy, C1-4 alkoxyphenyl, pyrrolidinyl, morpholinyl, tetrahydrofuranyl and triazolyl;
- R5 is hydrogen or C1-6alkyl optionally substituted with a substituent selected from the group consisting of halogen, —OH, C1-6alkoxy, —NRaRb, and RaRbN—C1-4alkyl;
- R6 is hydrogen or C1-6alkyl;
- R33 is independently selected for each occurrence from the group consisting of:
- halo, —OH, —CN, —NO2, oxo, hydrazino, formyl, azido, silyl, siloxy, —S(O)q—C1-6alkyl, —NRaRb, —NRc—S(O)t—C1-6alkyl, —S(O)t—NRaRb, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, haloC1-6alkyl, hydroxyC1-6alkyl, RaRbN—C1-6alkyl-, C1-6 alkoxy, haloC1-6 alkoxy, hydroxyC1-6alkoxy-, RaRbN—C1-6alkoxy-, C1-6alkoxyC1-6alkyl, —C(O)NRaRb, —C(O)—C1-6alkyl, —C(O)OH, and —C(O)O—C1-6alkyl phenyl, and a 5-6 membered monocyclic heteroaryl having one, two, or three heteroatoms selected from the group consisting of O, N, and S, wherein the phenyl and 5-6 membered monocyclic heteroaryl is optionally substituted with one, two or three substituents independently selected from the group consisting of:
- halo, —OH, —CN, —NO2, oxo, hydrazino, formyl, azido, silyl, siloxy, —S(O)q—C1-6alkyl, —NRaRb, —NRc—S(O)t—C1-6alkyl, —S(O)t—NRaRb, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, haloC1-6alkyl, hydroxyC1-6alkyl, RaRbN—C1-6alkyl-, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy-, RaRbN—C1-6alkoxy-, C1-6alkoxyC1-6alkyl, —C(O)NRaRb, —C(O)—C1-6alkyl, —C(O)OH, and —C(O)O—C1-6alkyl;
- R34 is selected from the group consisting of hydrogen, C1-4alkyl and hydroxyC1-4alkyl;
- Ra and Rb are independently hydrogen or C1-6alkyl;
- or
- Ra and Rb may be taken together with the nitrogen to which Ra and Rb are attached to form:
- Rc is hydrogen or C1-6alkyl;
- for each occurrence, q is 0, 1, or 2,
- for each occurrence, t is 1 or 2;
- r is 0, 1 or 2;
- r2 is 0, 1, 2 or 3;
- with the provisos that:
- when R3 is thiophen-2-yl or furan-2-yl, r2 is 1, 2 or 3;
- when R3 is pyrazol-4-yl, in at least one instance, R33 is other than C1-6alkyl;
- and
- when R3 is phenyl, at least one of R35, R36 and R37 is other than halo and C1-6 alkoxy.
24 more elements
Dependencies are inferred from the claim text.