Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)

Patent metadata

Field	Value
Publication number	US-9902710-B2
Application number	US-201514885740-A
Country	US
Kind code	B2
Filing date	Oct 16, 2015
Priority date	Dec 5, 2013
Publication date	Feb 27, 2018
Grant date	Feb 27, 2018

Abstract

The invention relates to compounds of the formula

or a pharmaceutically acceptable salt thereof, wherein R′, R 1 through R 7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.

First claim

What is claimed is:

1. A compound of Formula (I)

or a pharmaceutically acceptable salt, thereof, wherein:
R 1 is selected from the group of H, optionally substituted (C 1 -C 6 )alkyl, and optionally substituted (C 3 -C 6 )cycloalkyl;
R 2 is H;
R 3 and R 4 independently represent a (C 1 -C 3 )alkyl group;
R 5 is H;
R 6 and R 7 are independently H;
R′ is H;
Ar is selected from the group consisting of:

2. The compound according to claim 1 , selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

4. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising at least one compound of claim 4 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

Assignees

• Allergan Inc
• Exonhit Therapeutics Sa

Inventors

• Leblond Bertrand
• Taverne Thierry
• Chauvignac Cedric
• Beausoleil Eric
• Casagrande Anne Sophie
• Desire Laurent
• Pando Matthew P
• Donello John E
• Yang Rong

Classifications

• C07D217/04

  with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom · CPC title

• C07F9/62

  Isoquinoline or hydrogenated isoquinoline ring systems · CPC title

• C07D491/056

  with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring · CPC title

• C07D217/02

  with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines · CPC title

• C07D401/14

  containing three or more hetero rings · CPC title