# US 2013/0156720 A1 · Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders

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- Number: US 2013/0156720 A1
- Document ID: US20130156720A1
- Status: Published application
- Kind: A1
- Application number: 13/819,243
- Filed: 2011-08-23
- Published: 2013-06-20
- Earliest claimed: 2010-08-27
- Assignees: Ironwood Pharmaceuticals, Inc.
- Inventors: Mark G. Currie
- Web page: https://patentgrep.com/patent/US20130156720A1

## CPC

- A61K 31/785: Polymers containing nitrogen
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/403: condensed with carbocyclic rings, e.g. carbazole
- A61K 31/426: 1,3-Thiazoles
- A61K 31/427: not condensed and containing further heterocyclic rings
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/4453: only substituted in position 1, e.g. propipocaine, diperodon
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 31/64: Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
- A61K 31/702: Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
- A61K 31/721: Dextrans
- A61K 31/787: containing heterocyclic rings having nitrogen as a ring hetero atom
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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)

## Abstract

Disclosed herein are novel compositions and methods for treating or preventing metabolic syndromes. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a combination of at least one antidiabetic agent, at least one proton pump inhibitor and at least one bile acid sequestrant, and, optionally, at least one active agent, including, but not limited to, dyslipidemia agents, histamine H2 receptor blockers, antacids, γ-aminobutyricacid-b (GABA-B) agonists, prodrugs of GABA-B agonists, protease inhibitors and combinations of two or more thereof.

## Claims

### Claim 1

A composition comprising a therapeutically effective amount of at least one antidiabetic agent, at least one proton pump inhibitor and at least one bile acid sequestrant.

### Claim 2 (depends on 1)

A composition according to claim 1, further comprising a pharmaceutically acceptable excipient, diluent, or carrier.

### Claim 3 (depends on 1)

A composition according to claim 1, wherein the at least one antidiabetic agent is chosen from a thiazolidinedione, a sulfonylurea compound, a biguanide, a meglitinide, an alpha-glucosidase inhibitor and a DPP-4 inhibitor.

### Claim at position 4

4-9. (canceled)

### Claim 10 (depends on 1)

A composition according to claim 1, wherein the at least one proton pump inhibitor is chosen from omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole, tenatoprazole, leminoprazole, dontoprazole, and ransoprazole.

### Claim 11 (depends on 1)

A composition according to claim 1, wherein the at least one bile acid sequestrant is chosen from one or more of GT102-279, cholestyramine, colesevelam, colesevelam hydrochloride, ursodeoxycholic acid, colestipol, colestilan, sevelamer, polydiallylamine cross-linked with epichlorohydrin, dialkylaminoalkyl derivatives of a cross-linked dextran, or N-(cycloalkyl)alkylamines.

### Claim 12 (depends on 1)

A composition according to claim 1, wherein the at least one bile acid sequestrant is chosen from one or more of those represented by Structural formulae AAA-1 to AAA-64, Sephadex (DEAE), Cholacrylamine resin (MK-325), or SK&F97426-A.

### Claim 13

(canceled)

### Claim 14 (depends on 1)

A composition according to claim 1, further comprising a therapeutically effective amount of at least one agent chosen from a dyslipidemic agent or an anti-hypertensive agent.

### Claim 15 (depends on 14)

A composition according to claim 14, wherein the dyslipidemic agent is chosen from one or more of a statin, a HMG-CoA synthase inhibitor, a cholesterol absorption inhibitor or an ACAT inhibitor.

### Claim 16 (depends on 14)

A composition according to claim 14, wherein the anti-hypertensive agent is chosen from one or more of a thiazide derivative, a β-adrenergic blocker, a calcium-channel blocker, an angiotensin-converting-enzyme (ACE) inhibitor, and an angiotensin II receptor antagonist.

### Claim at position 12

17-19. (canceled)

### Claim 20 (depends on 1)

A pharmaceutical dosage form comprising a composition according to claim 1, wherein the therapeutically effective amount of said at least one antidiabetic agent is in a range from about 1 mg to about 1000 mg, the therapeutically effective amount of said at least one proton pump inhibitor is in a range from about 5 mg to about 100 mg, and the therapeutically effective amount of said at least one bile acid sequestrant is in a range from about 500 mg to about 10 g.

### Claim at position 14

21-22. (canceled)

### Claim 23 (depends on 1)

A method for treating a disorder selected from metabolic syndrome, type 2 diabetes, or a condition associated with type 2 diabetes or metabolic syndrome, the method comprising administering to a patient having or at risk of developing said disorder or condition a therapeutically effective amount of a composition according to claim 1.

### Claim 24

A method for treating a disorder selected from metabolic syndrome, type 2 diabetes, or a condition associated with type 2 diabetes or metabolic syndrome, the method comprising administering to a patient having or at risk of developing said disorder or condition a therapeutically effective amount of at least one proton pump inhibitor and at least one bile acid sequestrant.

### Claim 25 (depends on 24)

The method according to claim 24, further comprising administering to the patient a therapeutically effective amount of at least one antidiabetic agent.

### Claim at position 18

26-34. (canceled)

### Claim 35 (depends on 24)

A method according to claim 24, wherein the at least one proton pump inhibitor, the at least one bile acid sequestrant, and the least one antidiabetic agent, if present, are administered simultaneously, separately, or sequentially.

### Claim 36 (depends on 24)

A method according to claim 24, further comprising administering simultaneously, separately, or sequentially a therapeutically effective amount of at least one agent chosen from a dyslipidemic agent or an anti-hypertensive agent.

### Claim at position 21

37-38. (canceled)

### Claim 39 (depends on 24)

A method according to claim 24, wherein the disorder is selected from metabolic syndrome, type 2 diabetes, hyperglycemia, hyperinsulinaemia, hyperlipidemia, insulin resistance, impaired glucose metabolism, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, diabetic neuropathy, erectile dysfunction, premenstrual syndrome, vascular restenosis, ulcerative colitis, coronary heart disease, hypertension, angina pectoris, myocardial infarction, stroke, skin and connective tissue disorders, foot ulcerations, metabolic acidosis, arthritis or osteoporosis.

### Claim 40

(canceled)

### Claim 41 (depends on 40)

The method according to claim 40, wherein the disorder is metabolic syndrome, type 2 diabetes or insulin resistance.

### Claim 42 (depends on 23)

The method according to claim 23, comprising administering the composition or the pharmaceutical dosage form parenterally, orally, by inhalation, nasally, buccally, or via an implanted reservoir.

### Claim 43

A method for treating GERD in a diabetic patient, the method comprising administering to the diabetic patient having or at risk of developing GERD a therapeutically effective amount of at least one antidiabetic agent, at least one proton pump inhibitor and at least one bile acid sequestrant.

### Claim 44 (depends on 43)

The method according to claim 43, further comprising administering to the patient a therapeutically effective amount of at least one agent chosen from an dyslipidemic agent, an anti-hypertensive agent, a histamine H2 receptor blocker, an antacid, a GABA-B agonist, a γ-aminobutyricacid-b (GABA-B) agonist, a prodrug of a GABA-B agonist or a protease inhibitor.

### Claim 45

(canceled)