Peloton Therapeutics, Inc.

Amgen Inc.

Array Biopharma Inc.

Genentech, Inc.

John A Josey

Eli M Wallace

Stephen T Schlachter

Rui Xu

James P Rizzi

Bin Wang

Hanbiao Yang

Paul Wehn

Jonas Grina

Darryl David Dixon

Kevin Koch

Andreas Peter Termin

Nathan B Mantlo

Guangzhou Han

James F Blake

Steven Wade Andrews

Kevin Ronald Condroski

Ian S Mitchell

George T Topalov

Mark C Munson

Dengming Xiao

John Peter Fischer

Anthony D Piscopio

Martha E Rodriguez

Keith Lee Spencer

Jay Bradford Fell

Nicholas C Kallan

Peter J Stengel

Chang Rao

Yvan Le Huerou

April L Kennedy

Guy P A Vigers

Gregory F Miknis

Scott Miller

Yongxin Han

Lisa A De Meese

April L Bernacki

Bing Wang

Barry Goggin

Xinlin Du

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 invention provides methods and pharmaceutical compositions for treating proliferative disorders.

Combination therapy of a HIF-2-&#x3b1; inhibitor and an immunotherapeutic agent 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.

The present disclosure provides methods of treating glioblastoma multiform (GBM) in a subject in need thereof. Compositions for use in these methods are also provided.

Compositions for use in treating glioblastoma

The present invention provides methods and pharmaceutical compositions for treating proliferative disorders. The method involves step of administering to said subject a HIF-2alpha inhibitor and an immunotherapeutic agent.

Combination therapy of a HIF-2-alpha inhibitor and an immunotherapeutic agent and uses thereof

The present disclosure provides methods of treating pulmonary arterial hypertension (PAH) in a subject in need thereof. Compositions for use in these methods are also provided.

Compositions for use in treating pulmonary arterial hypertension

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 of Formula I: and salts thereof in which R, R, R, R, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers. 

Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula:A-L-CRwhere CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

AKT protein kinase inhibitors

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Dallas, TX, United States of America

John A Josey