# US 9,751,877 B2 · Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders

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- Number: US 9,751,877 B2
- Document ID: US9751877B2
- Status: Granted
- Kind: B2
- Application number: 14/877,118
- Filed: 2015-10-07
- Published: 2016-01-28
- Granted: 2017-09-05
- Earliest claimed: 2012-09-21
- Assignees: Pfizer Inc.
- Applicants: Pfizer Inc.
- Inventors: Martin Youngjin Pettersson; Douglas Scott Johnson; Chakrapani Subramanyam; Christopher John O'Donnell; Christopher William am Ende; Michael Eric Green; Nandini Chaturbhai Patel; Cory Michael Stiff; Tuan Phong Tran; Gregory Wayne Kauffman; Antonia Friederike Stepan; Patrick Robert Verhoest
- Web page: https://patentgrep.com/patent/US9751877B2

## CPC

- C07D 471/04: Ortho-condensed systems
- A61P 25/00: Drugs for disorders of the nervous system
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

## Claims

### Claim 1

The compound 2-[(1S)-1-{(2S,5R)-5-[4-chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydrofuran-2-yl}ethyl]-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising the compound according to claim 1 in admixture with at least one pharmaceutically acceptable excipient.

### Claim 3 (depends on 1)

A method for reducing the production of amyloid beta proteins in a human in need thereof comprising administering a therapeutically effective amount of the compound according to claim 1 to said human.

### Claim 4 (depends on 1)

A method for treating Alzheimer's disease in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound according to claim 1.

### Claim 5

A pharmaceutically acceptable salt of the compound 2-[(1S)-1-{(2S,5R)-5-[4-chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydrofuran-2-yl}ethyl]-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione.

### Claim 6 (depends on 5)

A pharmaceutical composition comprising the compound according to claim 5 in admixture with at least one pharmaceutically acceptable excipient.

### Claim 7 (depends on 5)

A method for reducing the production of amyloid beta proteins in a human in need thereof comprising administering a therapeutically effective amount of the compound according to claim 5 to said human.

### Claim 8 (depends on 5)

A method for treating Alzheimer's disease in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound according to claim 5.
