Bisphenol derivatives and their use as androgen receptor activity modulators
AssigneesThe University of British Columbia, Provincial Health Services Authority
InventorsRaymond J. Andersen, Marianne Dorothy Sadar, Kunzhong Jian, Nasrin R. Mawji, Jun Wang, Carmen Adriana Banuelos, Yu-Chi Yang
Life of this patent
Estimating the term…
Abstract
Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, 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.
Claims19
A method for prostate cancer comprising administering a compound having the following structure (I):
- or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof to a subject in need thereof,
- wherein:
- X is —S(O)n— or —C(R8R9)—;
- R1 is H, hydroxyl or —OC(═O)R13;
- R2 is hydroxyl or —OC(═O)R13;
- R3 is —NH2, —NHC(═O)R13, —N(C(═O)R13)2, —NHS(O)nR5, —N(C(═O)R13)(S(O)nR5), —N(C1-C6 alkyl)(S(O)nR5), or —S(O),R5, which are optionally substituted with one or more R6;
- R5 is each independently C1-C6 alkyl which is optionally substituted with one or more R6;
- R6is each independently selected from the group consisting of H, F, Cl, Br, I, 123I, hydroxyl, oxo, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C6-C12 aryl, wherein each R6is optionally substituted with one or more of halogen, 123I, 18F, hydroxyl, —OS(O)2-aryl, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl;
- R8 and R9 are each independently H or C1-C6 alkyl;
- R11a, R11b, R11c and R11d are each independently H, methyl, F, Cl, Br, I, or 123I;
- R13 is C1-C6 alkyl;
- and
- n is 0, 1, or 2;
- wherein at least one of R11a, R11b, R11c and R11d is methyl F, Cl, Br, I, or 123I.
Dependencies are inferred from the claim text.