| 摘要 |
In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to novel isotoplogues of 3α-hydroxy-3β-methyl-5α-pregnan-20-one (ganaxolone). In accordance with one aspect of the invention there is disclosed an isotopologue compound of the general Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are hydrogen or deuterium (2H); provided that at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 is deuterium (2H); or an ester, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof. The isotopologue compounds disclosed are effective in modulating the GABA receptor chloride ionophore complex (GR complex) in vitro and exhibit useful therapeutic effects in animal models of human central nervous system (CNS) disorders. |
