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1. EP3442942 - BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Office European Patent Office
Application Number 17781660
Application Date 18.04.2017
Publication Number 3442942
Publication Date 20.02.2019
Publication Kind A4
IPC
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
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
A61K 31/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
095Sulfur, selenium or tellurium compounds, e.g. thiols
10Sulfides; Sulfoxides; Sulfones
A61K 31/165
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
165having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/222
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
22of acyclic acids, e.g. pravastatin
222with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/4164
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
CPC
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 A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 13/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 17/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
14for baldness or alopecia
Applicants BRITISH COLUMBIA CANCER AGENCY BRANCH
THE UNIV OF BRITISH COLUMBIA UNIV INDUSTRY LIAISON OFFICE
Inventors ANDERSEN RAYMOND
SADAR MARIANNE DOROTHY
JLAN KUNZHONG
MAWJL NASRIN R
WANG JUN
BANUELOS CARMEN ADRIANA
YANG YU-CHI
Designated States
Priority Data 201662323196 15.04.2016 US
Title
(DE) BISPHENOLDERIVATE UND DEREN VERWENDUNG ALS ANDROGENREZEPTORAKTIVITÄTSMODULATOREN
(EN) BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS
(FR) DÉRIVÉS DE BISPHÉNOL ET LEUR UTILISATION EN TANT QUE MODULATEURS DE L'ACTIVITÉ DU RÉCEPTEUR DES ANDROGÈNES
Abstract
(EN)
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.

(FR)
Cette invention concerne des composés ayant une structure de Formule I ou un sel pharmaceutiquement acceptable, un tautomère ou un stéréoisomère de ceux-ci, où R1, R2, R3, R11a, R11b, R11c, R11d, et X, étant tels que définis dans la présente invention. Les utilisations de ces composés pour moduler l'activité du récepteur des androgènes, imager des diagnostics dans le domaine du cancer et des substances thérapeutiques, et des méthodes destinées à traiter des sujets en ayant besoin, dont des sujets atteints du cancer de la prostate sont en outre décrits.