Peloton Therapeutics, Inc.

Paul Wehn

Hanbiao Yang

James P Rizzi

Bin Wang

Eli M Wallace

Stephen T Schlachter

Rui Xu

John A Josey

Jonas Grina

Darryl David Dixon

Karl Bedke

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

The present disclosure provides compounds of Formula (II)  wherein R, R, R, R, R, W, W, W, X, Y, and A are as described herein. The disclosed compounds modulate CD73 activity. The present disclosure also provides, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity.

CD73 inhibitors 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.

Substituted pyridines that modulate HIF-2a activity, pharmaceutical compositions containing the substituted pyridines, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2a activity are described herein.

Substituted pyridines and uses thereof

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.

Cyclic sulfone and sulfoximine analogs and uses thereof

Compounds comprising a fused tricylic core that modulate HIF-2&#x3b1; activity, pharmaceutical compositions containing these chemical entities, and methods of using these chemical entities for treating diseases associated with HIF-2&#x3b1; activity are described herein.

Growing community of inventors

Dallas, TX, United States of America

Paul Wehn