IP Library Granted Patent US 10,584,111
Granted Patent B2
US 10,584,111 · App. 16/280,512 · Granted Mar 10, 2020

4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators

Inventors: John Andrew Christopher (Cambridge, GB); Miles Stuart Congreve (Cambridge, GB); Sarah Joanne Aves (Cambridge, GB); Benjamin Gerald Tehan (Cambridge, GB)
Assignee: Heptares Therapeutics Limited
C07D401/04C07D239/26C07D403/04
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 10,584,111
App. No.
16/280,512
Granted
Mar 10, 2020
Kind
B2
Abstract

The disclosures herein relate to novel compounds of formula wherein R 1 , R 2 , R 3 and R 4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.

Claims (34)

1. A compound of formula (4):

or a pharmaceutically acceptable salt thereof, wherein

R 1 is F, Cl, OMe, CH 2 OMe, Me, fluoromethyl or cyano;

R 2 is H or F;

and

R 3 is H, Me, F, Cl or cyano.

2. The compound according to claim 1 , wherein R 1 is F, Cl or cyano.

3. The compound according to claim 1 , wherein R 3 is H or F.

4. The compound according to claim 1 which is selected from the group consisting of:

3-chloro-4-fluoro-5-[6-(pyridin-2-yl)pyrimidin-4-yl]benzonitrile,

3-chloro-5-[6-(pyridin-2-yl)pyrimidin-4-yl]benzonitrile,

6-[6-(3-chloro-5-cyanophenyl)pyrimidin-4-yl]pyridine-3-carbonitrile,

3-methyl-5-[6-(pyridin-2-yl)pyrimidin-4-yl]benzonitrile,

3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile,

5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzene-1,3-dicarbonitrile,

3-chloro-5-[6-(5-methylpyridin-2-yl)pyrimidin-4-yl]benzonitrile,

3-chloro-5-[6-(5-chloropyridin-2-yl)pyrimidin-4-yl]benzonitrile,

5-[6-(pyridin-2-yl)pyrimidin-4-yl]benzene-1,3-dicarbonitrile,

3-chloro-4-fluoro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile,

3-methyl-5-[6-(5-methylpyridin-2-yl)pyrimidin-4-yl]benzonitrile,

3-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]-5-(methoxymethyl)benzonitrile,

3-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]-5-methoxybenzonitrile,

or a pharmaceutically acceptable salt thereof.

5. The compound according to claim 1 which is 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile or a pharmaceutically acceptable salt thereof.

6. The compound according to claim 1 which is 5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzene-1,3-dicarbonitrile or a pharmaceutically acceptable salt thereof.

7. The compound according to claim 1 which is 3-chloro-5-[6-(5-methylpyridin-2-yl)pyrimidin-4-yl]benzonitrile or a pharmaceutically acceptable salt thereof.

8. The compound according to claim 1 which is 3-chloro-5-[6-(5-chloropyridin-2-yl)pyrimidin-4-yl]benzonitrile or a pharmaceutically acceptable salt thereof.

9. A method for the treatment of migraine, dystonia, depression, anxiety or amyotrophic lateral sclerosis (ALS) comprising administering an effective amount of a compound according to claim 1 to a subject in need thereof.

10. The method according to claim 9 , wherein the disorder is migraine.

11. The method according to claim 9 , wherein the disorder is dystonia.

12. The method according to claim 9 , wherein the disorder is depression.

13. The method according to claim 9 , wherein the disorder is anxiety.

14. The method according to claim 9 , wherein the disorder is amyotrophic lateral sclerosis (ALS).

15. The method according to claim 12 , wherein the depression is treatment-resistant depression.

Assignments (3)
CHANGE OF NAME Recorded Aug 8, 2024
From: HEPTARES THERAPEUTICS LIMITED
To: NXERA PHARMA UK LIMITED
Reel/Frame 068230/0394 →
CHANGE OF ADDRESS Recorded Mar 21, 2019
From: HEPTARES THERAPEUTICS LIMITED
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 048661/0096 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 15, 2019
From: CHRISTOPHER, JOHN ANDREW; CONGREVE, MILES STUART; AVES, SARAH JOANNE; TEHAN, BENJAMIN GERALD
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 048613/0723 →
Priority Claims (1)
GB 1312800.4 · Jul 17, 2013 · national
Continuity (3)
Continuation 15618504 · Jun 9, 2017
Continuation 14904907
Related Publication 20190177297A1 · Jun 13, 2019
Cited By (1)
US 12,415,795