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US 10,118,903 B2Granted
Aminotriazole-based KDM1A inhibitors as epigenetic modulators
AssigneeMUSC Foundation for Research Development
InventorsPatrick M. Woster, Craig J. Kutz
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Abstract
In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease.
Claims18
A compound of the formula:
- wherein:
- R1 is halo, hydroxy, amino, nitro, cyano, alkyl(C≤12), or substituted alkyl(C≤12);
- Y1 is alkanediyl(C≤12), alkylaminodiyl(C≤12), alkoxydiyl(C≤12), or a substituted version of any of these groups;
- X1 is —O—, —S—, or —NR3—, wherein R3 is hydrogen or alkyl(C≤6);
- and
- R2 is aryl(C≤12), aralkyl(C≤12), heteroaryl(C≤12), heteroaralkyl(C≤12), or a substituted version of any of these groups;
- provided that R2 is not phenyl when X1 is —O—;
- or a pharmaceutically acceptable salt or tautomer thereof.
5 more elements
A compound of the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.