# US 5,707,649 A · Agent for treating neuronal diseases

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- Number: US 5,707,649 A
- Document ID: US5707649A
- Status: Granted
- Kind: A
- Application number: 08/464,683
- Filed: 1995-08-05
- Granted: 1998-01-13
- Earliest claimed: 1993-08-13
- Assignees: Seikagaku Corporation
- Inventors: Jinichi Inokuchi; Seigou Usuki
- Web page: https://patentgrep.com/patent/US5707649A

## CPC

- C07D 295/13: to an acyclic saturated chain
- A61K 31/5375: 1,4-Oxazines, e.g. morpholine
- A61P 25/16: Anti-Parkinson drugs
- 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
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 295/125: with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

Disclosed is an agent for curing neuronal diseases caused by disorders of peripheral nervous system or central nervous system, which comprises a 2-acylaminopropanol derivative represented by the formula (I): ##STR1## ›wherein R.sup.1 represents a phenyl group or cyclohexyl group each of which may be substituted by 1 to 3 same or different substituents selected from the group consisting of alkyl, alkoxy, hydroxy and nitro, or represents an alkyl group, and n represents an integer of 0 to 16! or a pharmaceutically acceptable salt thereof as an effective ingredient. It accelerates neurite extension and synapse formation by elevating biosynthesis of endogenous sphingoglycolipid of neurocytes, particularly ganglioside, whereby it can be used for curing various diseases of central nervous system and peripheral nervous system.

## Claims

### Claim 1

A liposome preparation composition for treating neuronal diseases treatable by elevating biosynthesis of endogenous glycosphingolipids (GSLs) of neurocytes comprising at least one 2-acylaminopropanol derivative of the formula ##STR4## wherein R.sup.1 is phenyl or cyclohexyl, each of which may be substituted by 1 to 3 members selected from the group consisting of alkyl, alkoxy, hydroxy and nitro, or R.sup.1 is alkyl and n is an integer of 0 to 16 and said derivative has efficacy for accelerating biosynthesis of glycosphingolipids, accelerating neurite extension and/or accelerating synapse formation, or a pharmaceutically acceptable salt thereof and a phospholipid.

### Claim 2 (depends on 1)

The liposome preparation composition according to claim 1, wherein n of the formula (I) is 6 to 16.

### Claim 3 (depends on 1)

The liposome preparation composition according to claim 1, wherein R.sup.1 of the formula (I) is phenyl.

### Claim 4 (depends on 1)

The liposome preparation composition according to claim 1, wherein the 2-acylaminopropanol derivative represented by the formula (I) is a L-threo isomer.

### Claim 5 (depends on 4)

The liposome preparation composition according to claim 4, wherein the 2-acylaminopropanol derivative is a L-threo isomer of 1-phenyl-2-decanoylamino-3-morpholino-1-propanol, or a salt thereof.

### Claim 6 (depends on 1)

The liposome preparation composition according to claim 1 wherein the liposome is capable of maintaining an effective concentration for exhibiting a pharmaceutical effect in brain when intravenously administered.

### Claim 7 (depends on 1)

The liposome preparation composition according to claim 1 wherein the liposome is a nanosphere liposome.

### Claim 8

A method of treating neuronal diseases treatable by elevating biosynthesis of endogenous glycosphingolipids (GLSs) of neurocytes in warm-blooded animals comprising administering to warm-blooded animals an amount of a liposome composition comprising at least one 2-acylaminopropanol derivative of the formula ##STR5## wherein R.sup.1 is phenyl or cyclohexyl, each of which may be substituted by 1 to 3 members selected from the group consisting of alkyl, alkoxy, hydroxy and nitro, or R.sup.1 is alkyl and n is an integer of 0 to 16 and said derivative has efficacy for accelerating biosynthesis of glycospyhingolipids, accelerating neurite extension and/or accelerating synapse formation, or a pharmaceutically acceptable salt thereof and a phospholipid sufficient to treat said neuronal diseases.

### Claim 9 (depends on 8)

The method of claim 8 wherein the compound of Formula I is a L-threo isomer.

### Claim 10 (depends on 8)

The method of claim 8 wherein the compound of Formula I is the L-threo isomer of 1-phenyl-2-decanoylamino-3-morpholino-1-propanol or a non-toxic, pharmaceutical acceptable acid addition salt thereof.