# US 7,745,452 B2 · Quinazolinone T-type calcium channel antagonists

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- Number: US 7,745,452 B2
- Document ID: US7745452B2
- Status: Granted
- Kind: B2
- Application number: 11/886,053
- Filed: 2006-03-08
- Published: 2008-07-10
- Granted: 2010-06-29
- Earliest claimed: 2006-03-08
- Assignees: Merck Sharp & Dohme Corp.
- Inventors: James C. Barrow; Rowena V. Cube; Phung Le Ngo; Kenneth E. Rittle; Zhiqiang Yang; Steven D. Young
- Web page: https://patentgrep.com/patent/US7745452B2

## CPC

- C07D 239/82: with an aryl radical attached in position 4
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 25/30: for treating abuse or dependence
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 405/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention is directed to quinazolinone compounds of the formula I: wherein R1, R2, R3, X1, X2 X3 are defined herein. These compounds are antagonists of T-type calcium channels, and are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

## Claims

### Claim 1

A compound which is selected from the group consisting of:
4-(2,2-Difluoroethyl)-5,6-difluoro-4-(4-fluorophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one;
6-Chloro-4-ethyl-4-(4-fluorophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one;
6-Chloro-4-(4-fluorophenyl)-4-propyl-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one; and
6-Chloro-4-cyclopropyl-4-(4-cyanophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one;
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1 which is 4-(2,2-Difluoroethyl) -5,6-difluoro-4-(4-fluorophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The compound of claim 1 which is 6-Chloro-4-ethyl-4-(4-fluorophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The compound of claim 1 which is 6-Chloro-4-(4-fluoro-phenyl)-4-propyl-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

### Claim 5

A compound which is 6-Chloro-4-cyclopropyl-4-(4-cyanophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one, or a pharmaceutically acceptable salt thereof.

### Claim 6

A compound which is 6-Chloro-4-cyclopropyl-4-(4-cyanophenyl)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinazolin-2(1H)-one.

### Claim 7 (depends on 1)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 1, or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 2)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 2, or a pharmaceutically acceptable salt thereof.

### Claim 9 (depends on 3)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 3, or a pharmaceutically acceptable salt thereof.

### Claim 10 (depends on 4)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 4, or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 5)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 5, or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 6)

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and the compound of claim 6.