# US 8,541,456 B2 · Roflumilast for the treatment of diabetes mellitus type 2

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- Number: US 8,541,456 B2
- Document ID: US8541456B2
- Status: Granted
- Kind: B2
- Application number: 13/179,895
- Filed: 2011-07-11
- Published: 2011-11-03
- Granted: 2013-09-24
- Earliest claimed: 2005-08-03
- Assignees: Takeda GmbH
- Applicants: Hans-Peter Kley; Guido Hanauer; Daniela Hauser; Beate Schmidt; Dirk Bredenbröker; Wilhelm Wurst; Jörg Kemkowski
- Inventors: Hans-Peter Kley; Guido Hanauer; Daniela Hauser; Beate Schmidt; Dirk Bredenbröker; Wilhelm Wurst; Jörg Kemkowski
- Web page: https://patentgrep.com/patent/US8541456B2

## CPC

- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- 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 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 13/12: of the kidneys
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 27/02: Ophthalmic agents
- 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 application relates to specific combinations of Roflumilast and/or Roflumilast N-Oxide and a PPAR-agonist, as well as their use in the treatment of diabetes mellitus type 2.

## Claims

### Claim 1

A pharmaceutical composition comprising a pharmaceutical formulation including a first amount of a compound of formula 1.1
or a pharmaceutically acceptable salt thereof and/or a compound of formula 1.2
or a pharmaceutically acceptable salt thereof, a second amount of a PPAR-agonist selected from the group consisting of MURAGLITAZAR, ROSIGLITAZONE, PIOGLITAZONE, RAGAGLITAZAR, FARGLITAZAR, TESAGLITAZAR, NAVEGLITAZAR, NETOGLITAZONE, RIVOGLITAZONE, K-111, GW-677954, FK-614, (−)-Halofenate and the pharmaceutically acceptable salts of these compounds, wherein the first amount and the second amount together comprise an effective amount for the treatment of diabetes mellitus type 2, and at least one pharmaceutically acceptable auxiliary.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the PPAR-agonist is selected from the group consisting of PIOGLITAZONE and the pharmaceutically acceptable salts thereof.

### Claim 3 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the pharmaceutical formulation is a combination of Roflumilast and PIOGLITAZONE.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the pharmaceutical formulation is a combination of Roflumilast and a pharmaceutically acceptable salt of PIOGLITAZONE.

### Claim 5

A method for treating diabetes mellitus type 2 comprising administering to a patient in need thereof a pharmaceutical composition comprising a pharmaceutical formulation including a first amount of a compound of formula 1.1
or a pharmaceutically acceptable salt thereof and/or a compound of formula 1.2
or a pharmaceutically acceptable salt thereof, a second amount of a PPAR-agonist selected from the group consisting of MURAGLITAZAR, ROSIGLITAZONE, PIOGLITAZONE, RAGAGLITAZAR, FARGLITAZAR, TESAGLITAZAR, NAVEGLITAZAR, NETOGLITAZONE, RIVOGLITAZONE, K-111, GW-677954, FK-614, (−)-Halofenate and the pharmaceutically acceptable salts of these compounds, wherein the first amount and the second amount together comprise an effective amount for the treatment of diabetes mellitus type 2, and at least one pharmaceutically acceptable auxiliary.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the PPAR-agonist is selected from the group consisting of PIOGLITAZONE and the pharmaceutically acceptable salts thereof.

### Claim 7 (depends on 5)

The method according to claim 5, wherein the pharmaceutical formulation is a combination of Roflumilast and PIOGLITAZONE.

### Claim 8 (depends on 5)

The method according to claim 5, wherein the pharmaceutical formulation is a combination of Roflumilast and a pharmaceutically acceptable salt of PIOGLITAZONE.