The University of British Columbia

British Columbia Cancer Agency Branch

Provincial Health Services Authority

Essa Pharma, Inc.

Columbia University

Kunzhong Jian

Raymond John Andersen

Marianne Dorothy Sadar

Nasrin R Mawji

Carmen Adriana Banuelos

Han-Jie Zhou

Peter Virsik

Jun Wang

Javier Garcia Fernandez

Yu-Chi Yang

Daniel Andrew Golec

Hsing Chen Tien

Yusuke Imamura

The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.

Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, R, R, R, R, R, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Bisphenol derivatives and their use as androgen receptor activity modulators

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, L, L, L, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Bisphenol ether derivatives and methods for using the same

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

Androgen receptor modulators and methods for their use

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, R, R, R, R, R, X, n, n, and nare as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Heterocyclic compounds for cancer imaging and treatment and methods for their use

Compounds having a structure of Formula I or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, R, R, R, R, R, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, R, R, R, R, R, X, n, n, and nare as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided. 

Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R, L, L, L, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided. 

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Surrey, Canada

Kunzhong Jian