IP Library Granted Patent US 9,969,728
Granted Patent B2
US 9,969,728 · App. 15/038,239 · Granted May 15, 2018

Tetrahydroimidazopyridine derivatives as modulators of TNF activity

Inventors: Sabine Defays (Brussels, BE); Jag Paul Heer (Brussels, BE); Victoria Elizabeth Jackson (Slough, GB); James Andrew Johnson (Slough, GB); Boris Kroeplien (Slough, GB); John Robert Porter (Slough, GB)
Assignee: UCB BIOPHARMA SPRL
C07D471/04A61K31/4184A61K31/437
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,969,728
App. No.
15/038,239
Granted
May 15, 2018
Kind
B2
Abstract

A series of substituted 5,6,7,8-tetrahydroimidazo[1,2-α]pyridine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Claims (17)

1. A compound represented by formula (IIA) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, or a glucuronide derivative thereof, or a co-crystal thereof:

wherein

R 11 represents hydrogen or halogen;

R 12 represents hydrogen or halogen; and

R 15 represents C 1-6 alkyl or difluoromethoxy;

R 16 represents hydrogen or C 1-6 alkyl;

E represents —CH 2 ;

Q represents —CH 2 — or —CH 2 O—;

Z represents (oxo)oxazolidinylphenyl.

2. The compound as claimed in claim 1 wherein R 11 represents hydrogen.

3. The compound as claimed in claim 1 wherein R 12 represents hydrogen or fluoro.

4. The compound as claimed in claim 1 wherein R 15 represents difluoromethoxy.

5. The compound of claim 1 that is

3-{3-[(3-{[2-(Difluoromethoxy)phenyl]methyl}-5,6,7,8-tetrahydroimidazo[1,2-α]pyridin-2-yl)methoxy]phenyl}oxazolidin-2-one; or

3-{3-[(3-{[2-(Difluoromethoxy)phenyl]methyl}-7-floro-5,6,7,8-tetrahydroimidazo[1,2-α]pyridin-2-yl)methoxy]phenyl}oxazolidin-2-one.

6. A pharmaceutical composition comprising a compound according to claim 1 or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, or a glucuronide derivative thereof, or a co-crystal thereof, in association with a pharmaceutically acceptable carrier.

7. The pharmaceutical composition as claimed in claim 6 further comprising an additional pharmaceutically active ingredient.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 2, 2017
From: UCB PHARMA S.A.
To: UCB BIOPHARMA SPRL
Reel/Frame 042572/0783 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2017
From: DEFAYS, SABINE; HEER, JAG PAUL
To: UCB BIOPHARMA SPRL
Reel/Frame 042242/0230 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: JACKSON, VICTORIA ELIZABETH; JOHNSON, JAMES ANDREW; KROEPLIEN, BORIS; PORTER, JOHN ROBERT
To: CELLTECH R&D LIMITED
Reel/Frame 041810/0043 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: CELLTECH R&D LIMITED
To: UCB S.A.
Reel/Frame 041808/0570 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 31, 2017
From: UCB S.A.
To: UCB PHARMA S.A.
Reel/Frame 041809/0918 →
Priority Claims (1)
GB 1321743.5 · Dec 9, 2013 · national
Continuity (1)
Related Publication 20160289228A1 · Oct 6, 2016