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US 2018/0155279 A1Published application
Aryl ethers and uses thereof
AssigneePeloton Therapeutics, Inc.
InventorsDarryl David Dixon, Jonas Grina, John A. Josey, James P. Rizzi, Stephen T. Schlachter, Eli M. Wallace, Bin Wang, Paul Wehn, Rui Xu, Hanbiao Yang
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Abstract
The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
Claims21
-64. (canceled)
A method of treating cancer, comprising administering to a subject in need thereof a compound of Formula III:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is aryl or heteroaryl;
- R4 is nitro, halo, cyano, alkyl, sulfinyl, sulfonamide, sulfonyl or sulfoximinyl;
- R5 is hydrogen, halo or alkyl;
- R8 is hydrogen, hydroxy, alkylamino, alkoxy or amino;
- R9 is hydrogen, alkyl, alkenyl or alkynyl, or R8 and R9 in combination form oxo or oxime;
- each of R10 is independently selected from the group consisting of fluoro, chloro, hydroxy and alkyl, or two R10 groups and the carbon atom(s) to which they are attached form 3- to 8-membered cycloalkyl or heterocycloalkyl;
- and
- n is 1, 2, 3 or 4;
- in conjunction with a radiation therapy.
7 more elements
Dependencies are inferred from the claim text.