Bromodomain and extra-terminal (bet) subfamily bromodomain 1 (bd1) selective inhibitors and methods using same

A compound of formula (I), or a salt, solvate, prodrug, isotopologue, tautomer, or stereoisomer thereof:

• wherein:
• R1 is
• R2a and R2b are each independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, and C(═O)N(Ra)(R),
• wherein at least one of R2a and R2b is H;
• R3a and R3b are each independently selected from the group consisting of H and C1-C6 alkyl;
• R4 is
• R5a, R5b, R5c, R5d, and R5e, if present, are each independently selected from the group consisting of H, halogen, CN, NO2, ORa, N(Ra)(Rb), C(═O)Ra, C(═O)ORa, C(═O)N(Ra)(Rb), N(Ra)C(═O)Ra, OC(═O)Ra, C(═O)H, S(═O)Ra, S(═O)2ORa, S(═O)2Ra, S(═O)2N(Ra)(R), optionally substituted C1-C6 alkyl, optionally substituted C1-C6 haloalkyl, optionally substituted C1-C6 alkoxy, optionally substituted C1-C6 haloalkoxy, optionally substituted phenyl, optionally substituted naphthyl, and optionally substituted C2-C8 heterocyclyl;
• wherein two vicinal substituents selected from the group consisting of R5a, R5b, R5c, R5d, and R5e, if present, may combine to form an optionally substituted phenyl or optionally substituted C2-C8 heteroaryl;
• R6a, R6b, R6c, R6d, R6e, R6f, R6g, R6h, and R6i, if present, are each independently selected from the group consisting of H, halogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, optionally substituted C3-C8 cycloalkyl, and optionally substituted C2-C8 heterocyclyl;
• R7 is
• R8a, R8b, R8c, R8d, and R8e are each independently selected from the group consisting of H, halogen, CN, NO2, ORa, N(Ra)(Rb), C(═O)Ra, C(═O)ORa, C(═O)N(Ra)(Rb), N(Ra)C(═O)Ra, OC(═O)Ra, C(═O)H, S(═O)Ra, S(═O)2ORa, S(═O)2Ra, S(═O)2N(Ra)(Rb), optionally substituted C1-C6 alkyl, optionally substituted C1-C6 haloalkyl, optionally substituted C1-C6 alkoxy, optionally substituted C1-C6 haloalkoxy, optionally substituted phenyl, optionally substituted naphthyl, and optionally substituted C2-C8 heterocyclyl;
• X is selected from the group consisting of N and C(R5e);
• L is selected from the group consisting of —C(═O)(optionally substituted C1-C3 alkylene)-*, —(C═O)—*, and -(optionally substituted C1-C3 alkylene)C(═O)—*,
• wherein * indicates the bond between L and R7;
• RA and RB are each independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 haloalkyl, C2-C8 heterocyclyl, optionally substituted benzyl, and optionally substituted phenyl;
• and
• Ra and Rb are each independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 haloalkyl, C2-C8 heterocyclyl, optionally substituted benzyl, and optionally substituted phenyl.