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1. CN109311807 - BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Office China
Application Number 201780034942.3
Application Date 18.04.2017
Publication Number 109311807
Publication Date 05.02.2019
Publication Kind A
IPC
C07C 317/16
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
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
不列颠哥伦比亚癌症局分支机构
THE UNIVERSITY OF BRITISH COLUMBIA UNIVERSITY-INDUSTRY LIAISON OFFICE
加拿大不列颠哥伦比亚大学
Inventors ANDERSEN RAYMOND
R·安徒生
SADAR MARIANNE DOROTHY
M·D·萨达尔
JLAN KUNZHONG
K·简
MAWJL NASRIN R.
N·R·马瓦尔
WANG JUN
J·王
BANUELOS CARMEN ADRIANA
C·A·巴努埃洛斯
YANG YU-CHI
Y-C·杨
Agents 北京坤瑞律师事务所 11494
Priority Data 62/323,196 15.04.2016 US
Title
(EN) BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS
(ZH) 双酚衍生物和其作为雄激素受体活性调节剂的用途
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.

(ZH)
提供了具有式I的结构的化合物或其药学上可接受的盐、互变异构体或立体异构体,其中R1、R2、R3、R11a、R11b、R11c、R11d和X如本文所定义。还提供了这类化合物用于调节雄激素受体活性、癌症的成像诊断和治疗的用途,并且还提供了用于治疗有需要的受试者(包括前列腺癌)的方法。