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1. US20170298033 - BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Office United States of America
Application Number 15489162
Application Date 17.04.2017
Publication Number 20170298033
Publication Date 19.10.2017
Publication Kind A1
IPC
C07D 295/088
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
08substituted by singly bound oxygen or sulfur atoms
084with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
088to an acyclic saturated chain
C07C 317/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
26having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
28with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 317/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
22with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 317/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
18with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/09
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
075Ethers or acetals
085having an ether linkage to aromatic ring nuclear carbon
09having two or more such linkages
CPC
C07D 295/088
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
08substituted by singly bound oxygen or sulfur atoms
084with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
088to an acyclic saturated chain
C07D 233/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
60with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
C07C 317/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
26having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
28with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 317/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
22with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 317/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
16having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
18with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 43/23
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
43Ethers; Compounds having groups, groups or groups
02Ethers
20having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
23containing hydroxy or O-metal groups
Applicants THE UNIVERSITY OF BRITISH COLUMBIA
British Columbia Cancer Agency Branch
Inventors Raymond ANDERSEN
Marianne Dorothy SADAR
Kunzhong JIAN
Nasrin R. MAWJI
Jun WANG
Carmen Adriana BANUELOS
Yu-Chi YANG
Title
(EN) BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS
Abstract
(EN)

Compounds having a structure of Formula I:

embedded image

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.