Peloton Therapeutics, Inc.

Darryl David Dixon

Eli M Wallace

Stephen T Schlachter

James P Rizzi

Bin Wang

John A Josey

Hanbiao Yang

Paul Wehn

Jonas Grina

Rui Xu

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.

Aryl ethers and uses thereof

Disclosed herein are substituted indane derivatives useful as HIF-2&#x3b1; inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2&#x3b1; activity are also disclosed.

Aromatic compounds and uses thereof

The present disclosure relates to HIF-2&#x3b1; inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2&#x3b1; 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.

Benzimidazole derivatives of Formula I, that modulate the activity of ACSS2 are disclosed for therapeutic use. The fused imidazole ring of the compounds disclosed has a diarylmethyl or diarylmethanol moiety attached at the 2-position and the as compounds have at least one other substituent at the 5 or 6 position of the benzimidazole. Also disclosed are methods of using the benzimidazole compounds for the treatment of diseases or disorders, such as cancer.

Benzimidazole derivatives and uses thereof

The present disclosure relates to cyclic sulfones and sulfoximines that are HIF-2a inhibitors and methods of making and using them for treating cancers. In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound described herein and a pharmaceutically acceptable carrier or excipient. The compound may exist in an amorphous form, a crystalline form, or as a salt, solvate, or hydrate. In another aspect, the present disclosure provides a method of treating renal cell carcinoma by administrating a therapeutically effective amount of a compound described herein or a pharmaceutical composition thereof to a subject in need of such treatment.

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Somerset, NJ, United States of America

Darryl David Dixon