IP Library Granted Patent US 9,475,791
Granted Patent B2
US 9,475,791 · App. 14/438,326 · Granted Oct 25, 2016

Compositions and methods for treating estrogen-related medical disorders

Inventors: Gregory R. Thatcher (Chicago, IL); Debra Tonetti (Westchester, IL); Mary Ellen Molloy (Chicago, IL); Bradley Michalsen (Grayslake, IL); Zihui Qin (Mundelein, IL)
Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
C07D333/64A61K31/381G01N33/57496G01N2333/91205G01N2800/52
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Quick Facts
Patent No.
US 9,475,791
App. No.
14/438,326
Granted
Oct 25, 2016
Kind
B2
Abstract

Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I) or a pharmaceutically acceptable salt thereof.

Claims (19)

1. A compound having formula (I-vii)

wherein

R 1 is selected from the group consisting of hydrogen, alkyl, —SO 3 R x1 , —PO 3 R y1 R z1 , and —C(═O)R a ;

R 2 is selected from the group consisting of halo and —OR 3 ;

R 3 is selected from the group consisting of hydrogen, alkyl, —SO 3 R x1 , —PO 3 R y1 R z1 , and —C(═O)R a ;

R 4 is selected from the group consisting of hydrogen, alkyl, —SO 3 R x1 , —PO 3 R y1 R z1 , and —C(═O)R a ;

R a , at each occurrence, is independently selected from the group consisting of —OH and alkyl; and

R x1 , R y1 and R z1 are, at each occurrence, independently selected from the group consisting of hydrogen and a pharmaceutically acceptable cation.

2. The compound of claim 1 , having formula (I-viii),

wherein R 1 and R 4 are as defined in claim 1 .

3. The compound of claim 1 , having formula (I-ix),

wherein R 1 is as defined in claim 1 .

4. The compound of claim 1 , having formula (I-x),

5. A pharmaceutical composition comprising a compound of formula (I-vii) according to claim 1 , and a pharmaceutically acceptable carrier.

6. A compound selected from the group consisting of:

3-(4-fluorophenyl)-2-(4-hydroxyphenoxyl)benzo[b]thiophen-6-ol; and

4-((3-(4-fluorophenyl)-6-methoxybenzo[b]thiophen-2-yl)oxy)phenol;

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition, comprising a compound according to claim 6 , and a pharmaceutically acceptable carrier.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2017
From: XIONG, RUI
To: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Reel/Frame 042308/0294 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 12, 2016
From: THATCHER, GREGORY R.; TONETTI, DEBRA; MOLLOY, MARY ELLEN; MICHALSEN, BRADLEY; QIN, ZIHUI
To: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Reel/Frame 038567/0151 →
CONFIRMATORY LICENSE Recorded Jun 8, 2015
From: UNIVERSITY OF ILLINOIS AT CHICAGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035858/0960 →
Continuity (3)
Provisional Application 61808971 · Apr 5, 2013
Provisional Application 61718035 · Oct 24, 2012
Related Publication 20150291552A1 · Oct 15, 2015