# US 11,304,928 B2 · Tablet comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salt thereof

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- Number: US 11,304,928 B2
- Document ID: US11304928B2
- Status: Granted
- Kind: B2
- Application number: 16/063,833
- Filed: 2016-12-22
- Published: 2018-12-27
- Granted: 2022-04-19
- Earliest claimed: 2015-12-25
- Assignees: FUJIFILM Toyama Chemical Co., Ltd.
- Applicants: FUJIFILM Toyama Chemical Co., Ltd.
- Inventors: Atsushi Kano; Hiroyuki Inaba; Tai Oura
- Web page: https://patentgrep.com/patent/US11304928B2

## CPC

- A61K 31/397: having four-membered rings, e.g. azetidine
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 25/02: for peripheral neuropathies
- 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

A tablet which comprises (1) 1-(3-(2-(1-benzothiophen-5- yl)ethoxy)propyl)azetidin-3-ol or a salt thereof and (2) ethyl cellulose, said tablet having excellent elution properties and good moldability, remaining stable during prolonged storage, and exhibiting high impact resistance.

## Claims

### Claim 1

A tablet having improved impact strength comprising:
(1) 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof;
(2) 2-5% based on the mass of the tablets ethyl cellulose
(3) 0.5 to 3% based on the mass of the tablets of microcrystalline cellulose;
(4) mannitol; and
(5) from 0.1 to 10% based on the tablet mass of a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone and mixtures thereof; and
the tablet's impact strength is greater than that of a tablet of the same composition except not comprising ethyl cellulose when measured in the falling impact test.

### Claim 2 (depends on 1)

The tablet according to claim 1, further comprising magnesium stearate.

### Claim 3 (depends on 1)

The tablet according to claim 1, wherein the tablet is a film coated tablet.

### Claim 4 (depends on 1)

A method for therapy of a disease of the central nerve or the peripheral nerve, comprising administering the tablet according to claim 1 to a subject in need thereof.

### Claim 5 (depends on 1)

A method for treating a disease in which neurogenesis induction is effective for therapy, comprising administering the tablet according to claim 1 to a subject in need thereof.

### Claim 6 (depends on 1)

A method for enhancing an effect of post-nerve injury rehabilitation, comprising administering the tablet according to claim 1 to a subject in need thereof.

### Claim 7 (depends on 1)

The tablet according to claim 1, wherein the tablet is an uncoated tablet.