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US 2026/0274823 A1Published application
5-membered heteroaryl carboxamide compounds for treatment of hbv
AssigneeAssembly Biosciences, Inc.
InventorsThilo HECKRODT, Michael WALKER, Min ZHONG
Life of this patent
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Abstract
The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.
Claims19
A compound of Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- L is C1-4alkylene or haloC1-4alkylene;
- L′ and L2 are independently a bond, C1-6alkylene, O, NRc, C(O), C(O)O, C(O)NRc, S(O)t or S(O)tNR0;
- X1 is NRx1;
- X3 is CR4R8;
- X4 and X6 are independently O or S;
- X5 is O, S or NR0;
- Ra, Rb and Rc are independently selected for each occurrence from the group consisting of hydrogen, C1-6 alkyl, haloC1-6 alkyl and C3-6 monocycloalkyl;
- Rd is hydrogen, OH, C1-6 alkyl or C1-6 alkoxy;
- Rx1 is hydrogen, C1-4 alkyl, C1-4 alkenyl, C1-4 alkynyl, haloC1-4 alkyl, or C3-6 monocycloalkyl;
- or Rx1 and R2 together form a —CH2CH2CH2—, —CH2CH2CH2CH2—, —CH2CH2O—, —CH2OCH2—, —CH2CH2CH2O—CH2CH2OCH2—, —CH2CH2—NH—CH2NHCH2—, —CH2CH2CH2NH— or —CH2CH2NHCH2— group;
- R0a is independently selected for each occurrence from the group consisting of hydrogen, halogen, OH, CN, NO2, RaRbN—, C1-4alkyl and haloC1-4alkyl;
- R4a and R6a are independently hydrogen or C1-4 alkyl;
- R0, R6 and R11 are independently selected for each occurrence from the group consisting of hydrogen, halogen, OH, CN, NO2, oxo, RdN═, hydrazino, formyl, azido, silyl, siloxy, HOC(O)—, RaRbN—, RaRbNS(O)t—, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl-, RaRbNC1-6alkyl-, HOC(O) C1-6alkyl-, RaRbNC1-6alkylNRc-, C1-6alkylNRaC1-6alkylNRc-, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy-, RaRbNC1-6alkoxy-, C1-6alkoxyC1-6alkyl-, haloC1-6alkoxyC1-6alkyl-, RaRbNC(O)—, C1-6alkylC(O)—, C1-6alkoxyC(O)—, C1-6alkylC(O)O—, C1-6alkylS(O)q—, C1-6alkylS(O)tNRc—, C1-6alkylS(O)tC1-6alkyl-, C1-6alkylS(O)tNRC1-6alkyl-, C3-6cycloalkylS(O)tC1-6alkyl-, C1-6alkylC(O) C1-6alkyl-, and C1-6alkylC(O) OC1-6alkyl-;
- R1 is a phenyl or 5-6 membered monocyclic heteroaryl, wherein the phenyl or 5-6 membered monocyclic heteroaryl is optionally substituted with one, two, or three independently selected R11 groups;
- R2 and R8 are independently selected from the group consisting of hydrogen, halo, CN, OH, RaRbN, C1-4alkyl, haloC1-4alkyl, C3-5monocycloalkyl, C1-4alkoxy, and haloC1-4alkoxy;
- R3 is
- R4 is R5-L1, R6 or R9;
- R5 is
- R9 is R14S(O)q-L-, R14S(O)qNH-L-, or R14C(O)NH-L-;
- R14 is RaRbN—, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy, or R5-L1-;
- q, r, t, and w are independently selected for each occurrence from 0, 1 and 2;
- and
- v is independently selected for each occurrence from 0, 1, 2 and 3.
21 more elements
Dependencies are inferred from the claim text.