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US 12,545,649 B2Granted
WDR5-MYC inhibitors
AssigneeVanderbilt University
InventorsSelena Chacon Simon, Alex Waterson, Jonathan D. MacDonald, Stephen Fesik, Shaun R. Stauffer, William P. Tansey
Life of this patent
Estimating the term…
Abstract
Substituted N-heteroaryl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject such as cancer cell proliferation.
Claims17
A compound of formula (I), or a pharmaceutically acceptable salt thereof,
- wherein
- G is
- R1a is G1, hydrogen, C1-8alkyl, C1-8haloalkyl, —C(O)Rb, —C1-6alkylene-G1, or —CH(G1)2;
- R1b is—SO2Ra, hydrogen, C1-8alkyl, C1-8haloalkyl, —C(O)Rb, —C(O)ORb, —C(O)N(Rb)2, or G1;
- R1c is hydrogen or C1-4alkyl;
- Q is
- Ra, at each occurrence, is independently C1-8alkyl, C1-8haloalkyl, G1, —C1-6alkylene-G1, —CH(G1)2, or -G1-G2,
- Rb, at each occurrence, is independently hydrogen, C1-8alkyl, C1-8haloalkyl, G1, —C1-6alkylene-G1, —CH(G1)2, or -G1-G2,
- G1 and G2, at each occurrence, are independently a C3-12carbocyclyl, a 6- to 12-membered aryl, a 4- to 12-membered heterocyclyl, or a 5- to 12-membered heteroaryl, wherein G1 and G2 are independently unsubstituted or substituted with 1-5 substituents independently selected from the group consisting of halogen, C1-4alkyl, C1-4haloalkyl, oxo, X2, and —C1-6alkylene-X2;
- X2 is cyano, —OR10, —N(R10)2, —C(O)R10, —SR10, —SOR10, —SO2R10, —C(O)OR10, —C(O)N(R10)2, —SO2N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)OR10, —N(R10)C(O)N(R10)2, or —N(R10) SO2R10,
- R10 is hydrogen, C1-4alkyl, —C1-4haloalkyl, C3-6cycloalkyl, or —C1-3alkylene-C3-6cycloalkyl, wherein alternatvely two R10, together with a common nitrogen to which they attach, form a 4- to 8-membered heterocyclyl optionally substituted with 1-4 substituents independently selected from the group consisting of halogen, C1-4alkyl, C1-4haloalkyl, and oxo;
- R6 is halogen, hydrogen, cyano, C(O)OH, SF5, NO2, C1-4alkyl, C1-4haloalkyl, —OC1-4alkyl, —OC1-4haloalkyl, —C1-6alkylene-OH, —C1-6alkylene-OC1-4alkyl, C3-6cycloalkyl, or a 4- to 7-membered heterocyclyl, wherein the cycloalkyl and heterocyclyl are optionally substituted with 1-4 substituents independently selected from the group consisting of halogen, cyano, C1-4alkyl, and C1-4haloalkyl;
- R8 is halogen, hydrogen, cyano, SF5, NO2, C1-4alkyl, C1-4haloalkyl, —OC1-4alkyl, —OC1-4haloalkyl, or C3-6cycloalkyl;
- and
- R7 and R9 are independently hydrogen, halogen, cyano, SF5, NO2, C1-4alkyl, C1-4haloalkyl, —OC1-4alkyl, —OC1-4haloalkyl, or C3-6cycloalkyl.
12 more elements
Dependencies are inferred from the claim text.