Post nerve injury rehabilitation effect-enhancing agent comprising alkyl ether derivative or salt thereof

Patent metadata

Field	Value
Publication number	US-10471044-B2
Application number	US-201816005774-A
Country	US
Kind code	B2
Filing date	Jun 12, 2018
Priority date	Jan 31, 2014
Publication date	Nov 12, 2019
Grant date	Nov 12, 2019

Abstract

Provided is a medicinal composition characterized by comprising an alkyl ether derivative represented by general formula [1]

[wherein: R 1 and R 2 are the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted C 1-6 alkyl group, an optionally substituted aryl group, etc.; R 3 represents an optionally protected hydroxyl group, etc.; and m and n are the same or different and represent an integer of 1 to 6] or a salt thereof. The medicinal composition according to the present invention is useful as a post nerve injury rehabilitation effect-enhancing agent.

First claim

The invention claimed is:

1. A method for enhancing recovery from or alleviation of functional disorder, comprising:
administering to a patient having a nerve injury and undergoing rehabilitation 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof such that the rehabilitation and 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt exhibit a synergistic effect or a statistically significant effect.

2. The method of claim 1 , wherein the salt of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol is a salt with a mineral acid, a salt with an organic carboxylic acid, a salt with a sulfonic acid, a salt with an alkali metal, a salt with an alkaline earth metal, an ammonium salt, or a salt with a nitrogen-containing organic base.

3. The method of claim 1 , wherein 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt is administered to the patient such that the patient exhibits statistically significant recovery from the functional disorder as compared to a patient undergoing the rehabilitation and not administered with 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt, and a patient administered with 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt and not undergoing the rehabilitation.

4. The method of claim 1 , wherein the functional disorder is motor dysfunction.

5. The method of claim 4 , wherein the motor dysfunction is at least one selected from the group consisting of a disturbances in skilled movements, Babinski's sign, spastic paralysis, chronic phase spasticity, chronic phase exaggerated deep tendon reflex, muscular rigidity, bradypragia, tremor, chorea, athetosis, dystonia, ataxia, gait dysfunction, upper limb dysfunction, language dysfunction, an eating disorder, and a swallowing disorder.

6. The method of claim 4 , wherein the motor dysfunction is at least one selected from the group consisting of gait dysfunction and upper limb dysfunction.

7. The method of claim 1 , wherein the nerve injury is at least one selected from the group consisting of a stroke, a brain injury, a spinal cord injury, a neurodegenerative disease, and a demyelinating disease.

8. The method of claim 1 , wherein the nerve injury is at least one selected from the group consisting of a stroke, a brain injury, and a spinal cord injury.

9. The method of claim 1 , wherein the rehabilitation includes motor dysfunction recovery training.

10. The method of claim 1 , wherein 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt is administered to the patient for at least 28 days.

11. The method of claim 1 , wherein 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt is administered to the patient for at least 49 days.

12. The method of claim 1 , wherein the patient is an adult human and 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt is administered to the patient in an amount of from 0.1 to 1,000 mg per day in a single dose or divided doses.

13. The method of claim 1 , wherein the patient is an adult human and 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt is administered to the patient in an amount of from 40 to 500 mg per day in a single dose or divided doses.

Assignees

• Fujifilm Toyama Chemical Co Ltd

Inventors

• Takahashi Takuya
• Okuda Tomohiro

Classifications

• A61P25/28

  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 · CPC title

• A61K31/397 Primary

  having four-membered rings, e.g. azetidine · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/381

  having five-membered rings · CPC title