# US 9,751,856 B2 · Ethynyl derivatives

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- Number: US 9,751,856 B2
- Document ID: US9751856B2
- Status: Granted
- Kind: B2
- Application number: 15/489,295
- Filed: 2017-04-17
- Published: 2017-08-03
- Granted: 2017-09-05
- Earliest claimed: 2013-07-08
- Assignees: Hoffmann-La Roche Inc.
- Applicants: Hoffmann-La Roche Inc.
- Inventors: Georg Jaeschke; Lothar Lindemann; Rainer E. Martin; Antonio Ricci; Daniel Rueher; Heinz Stadler; Eric Vieira
- Web page: https://patentgrep.com/patent/US9751856B2

## CPC

- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D 403/04: directly linked by a ring-member-to-ring-member bond
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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).

## Claims

### Claim 1

A compound of formula I
wherein
Y is N;
R1 is hydrogen, fluoro or chloro; and
R2 is hydrogen or lower alkyl;
or a pharmaceutically acceptable acid addition salt thereof.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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