Ethynyl derivatives

Patent metadata

Field	Value
Publication number	US-9682959-B2
Application number	US-201614991748-A
Country	US
Kind code	B2
Filing date	Jan 8, 2016
Priority date	Jul 8, 2013
Publication date	Jun 20, 2017
Grant date	Jun 20, 2017

Abstract

The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

First claim

The invention claimed is:

1. A compound of formula I

wherein
Y is CH;
R 1 is hydrogen, fluoro or chloro; and
R 2 is hydrogen or lower alkyl;
or a pharmaceutically acceptable acid addition salt thereof.

2. A compound of formula I according to claim 1 , selected from the group consisting of
2-[5-[2-(3-Fluorophenyl)ethynyl]-2-pyridyl]-3,5,5-trimethyl-imidazol-4-one
3,5,5-Trimethyl-2-[5-(2-phenylethynyl)-2-pyridyl]imidazol-4-one and
2-[5-[2-(3-Chlorophenyl)ethynyl]-2-pyridyl]-3,5,5-trimethyl-imidazol-4-one

and, if desired, alkylating the compound obtained to form a compound of formula

wherein the substituents are as described in claim 1 .

3. A pharmaceutical composition comprising a compound of formula I according to claim 1 and a therapeutically active carrier.

Assignees

• Hoffmann La Roche

Inventors

• Jaeschke Georg
• Lindemann Lothar
• Martin Rainer E
• Ricci Antonio
• Rueher Daniel
• Stadler Heinz
• Vieira Eric

Classifications

• A61P25/24

  Antidepressants · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61P25/22

  Anxiolytics · CPC title

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title