Substituted 3-phenoxyazetidin-1-yl-pyrazines

Patent metadata

Field	Value
Publication number	US-11780827-B2
Application number	US-202117215759-A
Country	US
Kind code	B2
Filing date	Mar 29, 2021
Priority date	Mar 30, 2020
Publication date	Oct 10, 2023
Grant date	Oct 10, 2023

Abstract

The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

First claim

The invention claimed is:

1. A compound of formula (I)

wherein
A is selected from the group A a consisting of

R is selected from the group R 1a consisting of H— and F—;
R 2 is selected from the group R 2a consisting of H— and F—;
R 3 is selected from the group R 3a consisting of halogen, F 2 HCO—, F 3 CO—, F 2 HC— and F 3 C—;
R 4 is selected from the group R 4a consisting of
H— and C 1-3 -alkyl-,
wherein the above mentioned C 1-3 -alkyl-group may optionally be substituted with 1 to 5 substituents independently selected from the group consisting of fluorine;

or a salt thereof.

2. A compound, or a salt thereof, according to claim 1 , wherein
A is selected from

or a salt thereof.

3. The compound, or a salt thereof, of claim 1 , wherein
R 3 is selected from the group R 3b consisting of
F—, Cl—, and F 2 HC—

or a salt thereof.

4. The compound, or a salt thereof, of claim 1 , wherein
R 3 is selected from
F—,

or a salt thereof.

5. The compound, or a salt thereof, of claim 1 , wherein
R 4 is selected from the group R 4b consisting of
H—, C 1-2 -alkyl- and F 3 C—,

or a salt thereof.

6. The compound, or a salt thereof, of claim 1 , wherein
R 4 is selected from
C 1-2 -alkyl-,

or a salt thereof.

7. A compound selected from the group consisting of

No.
Structure

I

II

III

IV

V

VI

VII

VIII

IX

X

XI

XII

XIII

XIV

XV

XVI

XVII

XVIII

XIX

Assignees

• Boehringer Ingelheim Int
• Arena Pharm Inc

Inventors

• Gerlach Kai
• Semple Graeme
• Xiong Yifeng
• Bertani Barbara
• Ferrara Marco
• Fossati Giacomo
• Hobson Scott
• Lessel Uta Friederike
• Runge Frank
• Mueller-Vieira Ursula
• Wippich Julian

Classifications

• C07D403/14 Primary

  containing three or more hetero rings · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61K31/501

  not condensed and containing further heterocyclic rings · CPC title

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title