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1. (WO2018200041) METHODS, AGENTS, AND COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA

Pub. No.:    WO/2018/200041    International Application No.:    PCT/US2018/000111
Publication Date: Fri Nov 02 00:59:59 CET 2018 International Filing Date: Fri Apr 27 01:59:59 CEST 2018
IPC: A61K 31/36
C07D 317/46
C07D 317/48
C07D 405/06
Applicants: UNIVERSITY OF CINCINNATI
Inventors: JIANG, Xi
CHEN, Jianjun
Title: METHODS, AGENTS, AND COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
Abstract:
A method of treating a subject suffering from a condition characterized by over- expression of Ten-eleven translocation 1 (TET1) is provided, the method including administering to the subject an effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the Formula I: (formula I) wherein: R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, hydroxyl, alkyl, alkoxy, amine, halo, and trifluoromethyl, and wherein any two adjacent moieties of R1, R2, R3, R4, and R5 may come together to form a heterocyclic ring; R6 is H or hydroxyl; and R7 is selected from H, (formula 2), and (formula 3), wherein R8 is C or O. Also provided are methods for selectively suppressing transcription of TET1 and/or reducing a level of 5-hydroxymethylcytosine in a subject by administering an effective amount of a Formula (I) compound and pharmaceutical compositions comprising Formula (I) compounds.