# US 2013/0158124 A1 · 1-amino-alkylcyclohexane derivatives for the treatment of mast cell mediated diseases

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- Number: US 2013/0158124 A1
- Document ID: US20130158124A1
- Status: Published application
- Kind: A1
- Application number: 13/766,145
- Filed: 2013-02-13
- Published: 2013-06-20
- Earliest claimed: 2008-12-19
- Assignees: MERZ PHARMA GmbH & CO. KGaA
- Inventors: Hjalmar KURZEN
- Web page: https://patentgrep.com/patent/US20130158124A1

## CPC

- A61K 31/13: Amines {(A61K31/04 takes precedence)}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/06: Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 27/02: Ophthalmic agents
- A61P 27/14: Decongestants or antiallergics
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- 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 relates to the treatment of an individual afflicted with mast cell mediated diseases comprising administering to the individual an effective amount of a 1-amino-alkylcyclohexane derivative.

## Claims

### Claim 1

A method of treating or preventing mast cell mediated diseases in a subject in need thereof, comprising administering an effective amount of a 1-amino-alkylcyclohexane derivative selected from neramexane and pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the 1-amino-alkylcyclohexane derivative is neramexane mesylate.

### Claim 3 (depends on 2)

The method according to claim 2, wherein neramexane mesylate is administered in a range from about 5 mg to about 150 mg/day.

### Claim 4 (depends on 2)

The method according to claim 2, wherein neramexane mesylate is administered in a range from about 5 mg to about 100 mg/day.

### Claim 5 (depends on 2)

The method according to claim 2, wherein neramexane mesylate is administered at about 5 mg to about 75 mg/day.

### Claim 6 (depends on 2)

The method according to claim 2, wherein neramexane mesylate is administered at about 50 mg/day.

### Claim 7 (depends on 2)

The method according to claim 2, wherein neramexane mesylate is administered at about 75 mg/day.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the 1-amino-alkylcyclohexane derivative is administered once a day, twice a day (b.i.d.), or three times a day.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the 1-amino-alkylcyclohexane derivative is administered in a topical formulation.

### Claim 10 (depends on 9)

The method according to claim 9, wherein the 1-amino-alkylcyclohexane derivative is administered between 0.1 and 99% by weight of the formulation.

### Claim 11 (depends on 1)

The method according to claim 1, wherein the 1-amino-alkylcyclohexane derivative is administered in an oral formulation.

### Claim 12 (depends on 1)

The method according to claim 1, wherein the mast cell mediated disease is not psoriasis.

### Claim 13

A pharmaceutical composition comprising a therapeutically effective amount of a 1-amino-alkylcyclohexane derivative selected from neramexane and pharmaceutically acceptable salts thereof, in combination with an additional pharmaceutical agent which has been shown to be effective for the treatment or the prevention of mast cell mediated diseases and, optionally, at least one pharmaceutically acceptable carrier or excipient.

### Claim 14 (depends on 13)

The pharmaceutical composition according claim 13, wherein the 1-amino-alkylcyclohexane derivative is neramexane mesylate.