# US 10,245,253 B2 · Pharmaceutical combination comprising a selective S1P1 receptor agonist

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- Number: US 10,245,253 B2
- Document ID: US10245253B2
- Status: Granted
- Kind: B2
- Application number: 15/534,951
- Filed: 2015-12-10
- Published: 2017-12-07
- Granted: 2019-04-02
- Earliest claimed: 2014-12-11
- Assignees: Actelion Pharmaceuticals Ltd.
- Applicants: Actelion Pharmaceuticals Ltd
- Inventors: Martine Clozel; Luca Piali
- Web page: https://patentgrep.com/patent/US10245253B2

## CPC

- A61K 31/426: 1,3-Thiazoles
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/22: of acyclic acids, e.g. pravastatin
- A61K 31/225: Polycarboxylic acids
- A61K 31/27: of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
- A61K 31/4015: having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- 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 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is dimethyl fumarate.

### Claim 2 (depends on 1)

A pharmaceutical combination according to claim 1, wherein the first and the second active ingredient are comprised in a single pharmaceutical composition.

### Claim 3 (depends on 1)

A pharmaceutical combination according to claim 1, wherein the first and the second active ingredient are comprised in separated pharmaceutical compositions.

### Claim 4 (depends on 1)

A method of treatment for multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 1 to a subject in need thereof.

### Claim 5 (depends on 1)

A method of treatment for relapsing multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 1 to a subject in need thereof.

### Claim 6 (depends on 1)

A method of treatment for relapsing-remitting multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 1 to a subject in need thereof.

### Claim 7 (depends on 2)

A method of treatment for multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 2 to a subject in need thereof.

### Claim 8 (depends on 2)

A method of treatment for relapsing multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 2 to a subject in need thereof.

### Claim 9 (depends on 2)

A method of treatment for relapsing-remitting multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 2 to a subject in need thereof.

### Claim 10 (depends on 3)

A method of treatment for multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 3 to a subject in need thereof.

### Claim 11 (depends on 3)

A method of treatment for relapsing multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 3 to a subject in need thereof.

### Claim 12 (depends on 3)

A method of treatment for relapsing-remitting multiple sclerosis, the method comprising administering the pharmaceutical combination according to claim 3 to a subject in need thereof.