# US 10,117,876 B2 · Pharmaceutical composition of fused aminodihydrothiazine derivative

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,117,876 B2
- Document ID: US10117876B2
- Status: Granted
- Kind: B2
- Application number: 15/516,567
- Filed: 2015-10-08
- Published: 2018-09-20
- Granted: 2018-11-06
- Earliest claimed: 2014-10-10
- Assignees: Eisai R&D Management Co., Ltd.
- Applicants: Eisai R&D Management Co., Ltd.
- Inventors: Yasuhiro Zaima; Kazuo Kazama; Shuntaro Arase; Kentaro Nagane; Kanta Horie; Yosuke Ueki
- Web page: https://patentgrep.com/patent/US10117876B2

## CPC

- A61K 31/542: ortho- or peri-condensed with heterocyclic ring systems
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- 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
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound represented by formula (1):
or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and
a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the salt of a compound having a C12-22 saturated aliphatic hydrocarbon group is at least one selected from the group consisting of a metal salt of a C12-22 saturated aliphatic organic acid, a mono alkaline metal salt of a mono C12-22 alkyl fumarate, and a mono alkaline earth metal salt of a mono C12-22 alkyl fumarate.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the salt of a compound having a C12-22 saturated aliphatic hydrocarbon group is at least one selected from the group consisting of sodium stearyl fumarate, sodium lauryl sulfate, calcium stearate and magnesium stearate.

### Claim 4

A pharmaceutical composition comprising a compound represented by formula (1):
or N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d] [1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide, or a pharmaceutically acceptable salt of the foregoing, and
means that does not cause a substantial change in the dissolution profile even after storage for a certain period of time.