IP Library Granted Patent US 9,938,240
Granted Patent B2
US 9,938,240 · App. 15/372,497 · Granted Apr 10, 2018

Fluorinated derivatives of 3-hydroxypyridin-4-ones

Inventors: Tim Fat Tam (Vaughan, CA); Regis Leung-Toung (Mississauga, CA); Yingsheng Wang (Richmond Hill, CA); Yanqing Zhao (Richmond Hill, CA); Tao Xin (Woodbridge, CA); Birenkumar Shah (Brampton, CA)
Assignee: Apotex Inc.
C07D213/26A61K31/4412A61K31/4545A61K31/496C07D211/86C07D213/69C07D213/74C07D401/06
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Quick Facts
Patent No.
US 9,938,240
App. No.
15/372,497
Granted
Apr 10, 2018
Kind
B2
Abstract

Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Friedreich's ataxia.

Claims (35)

1. A morpholinyl-containing fluorinated 3-hydroxy pyridine-4(1H)-one compound of Formula I:

or a pharmaceutically acceptable salt thereof,

wherein:

G 1 is CH 2 NR 1 R 2 , where NR 1 R 2 is morpholinyl;

G 2 is CH 2 CF 2 R 3 ; wherein R 3 is F or H;

G 3 is H or C 1 -C 4 alkyl; and

G 4 is H or C 1 -C 4 alkyl.

2. A morpholinyl-containing fluorinated 3-hydroxy pyridine-4(1H)-one compound of Formula I:

or a pharmaceutically acceptable salt thereof,

wherein

G 1 is C 1 -C 4 alkyl;

G 2 is H, C 1 -C 4 alkyl or cyclopropyl;

G 3 is H or C 1 -C 4 alkyl; and

G 4 is CH(R 8 )CF 3 , wherein R 8 is morpholinyl.

3. A morpholinyl-containing fluorinated 3-hydroxy pyridine-4(1H)-one compound of Formula I:

or a pharmaceutically acceptable salt thereof,

wherein

G 1 is CH(R 4 )CF 3 , wherein R 4 is morpholinyl;

G 2 is H, C 1 -C 4 alkyl or cyclopropyl;

G 3 is H or C 1 -C 4 alkyl; and

G 4 is H or C 1 -C 4 alkyl.

4. A morpholinyl-containing fluorinated 3-hydroxy pyridine-4(1H)-one compound of Formula I:

or a pharmaceutically acceptable salt thereof,

wherein

G 1 is CH(R 7 )CF 2 H, wherein R 7 is morpholinyl;

G 2 is H, C 1 -C 4 alkyl or cyclopropyl;

G 3 is H or C 1 -C 4 alkyl; and

G 4 is H or C 1 -C 4 alkyl.

5. The compound of claim 2 , wherein G 1 is methyl, G 2 is H, and G 3 is H.

6. The compound of claim 2 , wherein G 1 is methyl, G 2 is methyl, and G 3 is H.

7. The compound of claim 1 , wherein R 3 is F, G 3 is methyl and G 4 is H.

8. The compound of claim 1 , wherein R 3 is F, G 3 is H and G 4 is H.

9. The compound of claim 3 , wherein G 2 is methyl, G 3 is methyl, and G 4 is H.

10. The compound of claim 3 , wherein G 2 is methyl, G 3 is H, and G 4 is H.

11. The compound of claim 4 , wherein G 2 is methyl, G 3 is H, and G 4 is H.

Assignments (3)
SECURITY INTEREST Recorded Apr 15, 2023
From: APOTEX INC.
To: THE BANK OF NOVA SCOTIA
Reel/Frame 063364/0710 →
MERGER Recorded Nov 19, 2019
From: APOTEX TECHNOLOGIES INC.
To: APOTEX INC.
Reel/Frame 051057/0015 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 14, 2016
From: TAM, TIM FAT; LEUNG-TOUNG, REGIS; WANG, YINGSHENG; ZHAO, YANQING; XIN, TAO; SHAH, BIRENKUMAR
To: APOTEX TECHNOLOGIES INC.
Reel/Frame 040731/0767 →
Continuity (4)
Continuation In Part 14735718 · Jun 10, 2015
Division 13382130
Provisional Application 61222979 · Jul 3, 2009
Related Publication 20170088518A1 · Mar 30, 2017