# US 7,612,058 B2 · Methods for inhibiting sterol absorption

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- Number: US 7,612,058 B2
- Document ID: US7612058B2
- Status: Granted
- Kind: B2
- Application number: 10/998,400
- Filed: 2004-11-29
- Published: 2005-07-14
- Granted: 2009-11-03
- Earliest claimed: 2001-01-26
- Assignees: Schering Corporation
- Inventors: Wing-Kee Philip Cho
- Web page: https://patentgrep.com/patent/US7612058B2

## CPC

- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/397: having four-membered rings, e.g. azetidine
- 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 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- 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 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 provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.

## Claims

### Claim 1

A method of treating a vascular condition associated with elevated sterol and/or stanol levels, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting of:
Weight
percent of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 2 (depends on 1)

The method according to claim 1, wherein the vascular condition is atherosclerosis.

### Claim 3

A method of treating diabetes in a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting of:
Weight
percent of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 4

A method of treating obesity in a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting of:
Weight
percent of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 5

A method of lowering a plasma sterol concentration of a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting of:
Weight
percent of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 6

A method of treating a vascular condition associated with elevated sterol and/or stanol levels, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting essentially of:
milligrams
of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 7 (depends on 6)

The method according to claim 6, wherein the vascular condition is atherosclerosis.

### Claim 8

A method of treating diabetes in a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting essentially of:
milligrams
of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 9

A method of treating obesity in a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting essentially of:
milligrams
of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is:

### Claim 10

A method of lowering a plasma sterol concentration of a mammal, comprising the step of administering to a mammal in need of such treatment a pharmaceutical composition consisting essentially of:
milligrams
of
Ingredient
ingredient
Compound of Formula (II)
10
Lactose monohydrate
55
Microcrystalline cellulose
20
Povidone
4
Croscarmellose sodium
8
Sodium lauryl sulfate
2
Magnesium stearate
1
Total
100
wherein the compound represented by Formula (II) below is: