Prodrugs of Neurosteroid Analogs and Uses Thereof

A compound of Formula II or a pharmaceutically acceptable salt, hydrate, or hydrated salt thereof,

• wherein n is 0 or 1;
• and
• wherein:
• (1) X is OH or NR1R2,
• Y is O or NR3,
• RA, RB, RC, RD, RE, and RF are independently selected from the group consisting of hydrogen, halogen, cyano, nitro, carboxyl, carbonate, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, acyl, sulfinyl, sulfonyl, sulfonate, sulfonamide, amide, optionally Si-substituted silyl, ester, thioester, carbonate ester, and carbamate, and
• R1, R2, and R3 are independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, with the proviso that at least one of R1 and R2 is hydrogen;
• (2) X is NR1R2,
• Y is O or NR3,
• R1 joins RC or RE to form a 4-7 membered, optionally substituted heterocycle,
• R2 is hydrogen,
• RA, RB, RC, RD, RE, and RF, on each occurrence when not joined by R1 to form the heterocycle, are independently selected from the group consisting of hydrogen, halogen, cyano, nitro, carboxyl, carbonate, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, acyl, sulfinyl, sulfonyl, sulfonate, sulfonamide, amide, optionally Si-substituted silyl, ester, thioester, carbonate ester, and carbamate, and
• R3 is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl;
• or
• (3) X is OH or NR1R2,
• Y is NR3,
• R3 joins RA to form a 4-7 membered, optionally substituted heterocycle,
• RB, RC, RD, RE, and RF are independently selected from the group consisting of hydrogen, halogen, cyano, nitro, carboxyl, carbonate, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, acyl, sulfinyl, sulfonyl, sulfonate, sulfonamide, amide, optionally Si-substituted silyl, ester, thioester, carbonate ester, and carbamate, and
• R1 and R2 are independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, with the proviso that at least one of R1 and R2 is hydrogen.