# US 8,772,282 B2 · Tetrahydropyrrolothiazine compounds

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- Number: US 8,772,282 B2
- Document ID: US8772282B2
- Status: Granted
- Kind: B2
- Application number: 14/096,443
- Filed: 2013-12-04
- Published: 2014-04-03
- Granted: 2014-07-08
- Earliest claimed: 2012-04-03
- Assignees: Eli Lilly and Company
- Applicants: Eli Lilly and Company
- Inventors: James Peter Beck; Steven James Green; Jose Eduardo Lopez; Brian Michael Mathes; Dustin James Mergott; Warren Jaye Porter; Zoran Rankovic; Yuan Shi; Brian Morgan Watson; Leonard Larry Winneroski, Jr.
- Web page: https://patentgrep.com/patent/US8772282B2

## CPC

- C07D 513/04: 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

The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound of the formula:
wherein A is selected from the group consisting of;
R1 is H or F;
R2 is H, —CH2OH, C1-C3 alkyl,
R3 is H, F, or CN;
R4 is H, F; or CN; and
R5 is H, —CH3, or —OCH3;
or a pharmaceutically acceptable salt thereof, in combination with one or more pharmaceutically acceptable carriers, diluents, or excipients.

### Claim 2 (depends on 1)

A pharmaceutical composition according to claim 1 wherein A is selected from the group consisting of:

### Claim 3 (depends on 2)

A pharmaceutical composition according to claim 2 wherein A is selected from the group consisting of:

### Claim 4 (depends on 1)

A pharmaceutical composition according to claim 1 wherein R1 is F.

### Claim 5 (depends on 4)

A pharmaceutical composition according to claim 4 wherein R2 is H.

### Claim 6 (depends on 4)

A pharmaceutical composition according to claim 4 wherein R2 is

### Claim 7 (depends on 5)

A pharmaceutical composition according to claim 5 wherein R5 is H.

### Claim 8 (depends on 6)

A pharmaceutical composition according to claim 6 wherein R5 is H.

### Claim 9 (depends on 7)

A pharmaceutical composition according to claim 7 wherein A is selected from the group consisting of:

### Claim 10 (depends on 8)

A pharmaceutical composition according to claim 8 wherein A is selected from the group consisting of:

### Claim 11

A pharmaceutical composition comprising a compound which is (4aR,7aR)-6-(5-fluoropyrimidin-2-yl)-7a-isothiazol-5-yl-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-2-amine:
or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable carriers, diluents, or excipients.

### Claim 12 (depends on 11)

A pharmaceutical composition comprising a compound according to claim 11 which is (4aR,7aR)-6-(5-fluoropyrimidin-2-yl)-7a-isothiazol-5-yl-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-2-amine:
in combination with one or more pharmaceutically acceptable carriers, diluents, or excipients.