IP Library Granted Patent US 10,246,432
Granted Patent B2
US 10,246,432 · App. 15/618,504 · Granted Apr 2, 2019

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

Inventors: John Andrew Christopher (Welwyn Garden City, GB); Miles Stuart Congreve (Welwyn Garden City, GB); Sarah Joanne Aves (Welwyn Garden City, GB); Benjamin Gerald Tehan (Welwyn Garden City, 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 10,246,432
App. No.
15/618,504
Granted
Apr 2, 2019
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 (35)

1. A method for the treatment of a disorder, comprising administering an effective amount of a compound to a subject in need thereof, wherein the compound is selected from the group consisting of the compounds represented by the following formulae:

or a pharmaceutically acceptable salt thereof, wherein

R 1 is halogen, optionally substituted C 1 -C 3 alkyl, cyclopropyl, optionally substituted C 1 -C 3 alkoxy, cyano, hydroxyl, nitro or NH 2 ;

R 2 is H or F;

R 3 is H, halogen, optionally substituted C 1 -C 3 alkyl, optionally substituted C 1 -C 3 alkoxy or cyano;

R 4 is H, halogen, optionally substituted C 1 -C 3 alkyl, optionally substituted C 1 -C 3 alkoxy, or cyano; and

n is 0-3,

wherein the disorder is migraine, dystonia, depression, anxiety or amyotrophic lateral sclerosis (ALS).

2. The method of claim 1 , wherein the disorder is migraine.

3. The method of claim 1 , wherein the disorder is dystonia.

4. The method of claim 1 , wherein the disorder is depression.

5. The method of claim 1 , wherein the disorder is anxiety.

6. The method of claim 1 , wherein the disorder is amyotrophic lateral sclerosis (ALS).

7. The method according to claim 1 wherein R 1 is F, Cl, OMe, CH 2 OMe, Me, fluoromethyl or cyano.

8. The method according to claim 1 wherein R 1 is F, Cl or cyano.

9. The method according to claim 1 wherein R 3 is H, Me, F, Cl or cyano.

10. The method according to claim 1 wherein R 3 is H or F.

11. The method according to claim 1 wherein n is 0 or 1.

12. The method according to claim 1 wherein the compound 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-(pyridazin-3-yl)pyrimidin-4-yl]benzonitrile,

3-(4,4′-bipyrimidin-6-yl)-5-chlorobenzonitrile,

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, and

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

or a pharmaceutically acceptable salt thereof.

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 Jun 12, 2017
From: CHRISTOPHER, JOHN ANDREW; CONGREVE, MILES STUART; AVES, SARAH JOANNE; TEHAN, BENJAMIN GERALD
To: HEPTARES THERAPEUTICS LIMITED
Reel/Frame 042675/0653 →
Priority Claims (1)
GB 1312800.4 · Jul 17, 2013 · national
Continuity (2)
Continuation 14904907
Related Publication 20170275265A1 · Sep 28, 2017
Cited By (1)
US 12,415,795