| 摘要 |
In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. |
| 主权项 |
1. A compound having a structure represented by a formula (I)or a formula (II) wherein m is 0 or 1; n is an integer from 0 to 3; X is selected from the group consisting of OH, NO2 and F; Z is selected from the group consisting of N and CH; R1 is selected from the group consisting of halo, C1-C3 haloalkyl, and C1-C3 polyhaloalkyl; each of R2, R3, and R4 is independently selected from the group consisting of hydrogen, halo, hydroxyl, cyano, amino, C2-C6 alkalkoxy, C1-C6 alkoxy, C1-C6 alkyl, C1-C6 polyhaloalkyl, and C1-C6 haloalkyl; R5 is selected from the group consisting of NR6 R7, C1-C6 alkyl, C3-C6 cycloalkyl, and Cy, and substituted with 0-3 groups independently selected from halo, hydroxyl, amino, C2-C6 alkalkoxy, C1-C6 alkylalcohol, C1-C6 alkoxy, C1-C6 alkyl, C1-C6 polyhaloalkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, and Cy; Cy is a heterocycloalkyl selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, azepanyl, oxazolidinyl, imidazolidinyl, pyrazolidinyl, piperazinyl, oxazinanyl, morpholinyl, hexahydrophyrimidinyl, and hexahydropyridazinyl; and each of R6 and R7 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, and C3-C6 heterocycloalkyl; or a pharmaceutically acceptable salt thereof.
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