IP Library Granted Patent US 7,612,058
Granted Patent B2
US 7,612,058 · App. 10/998,400 · Granted Nov 3, 2009

Methods for inhibiting sterol absorption

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Quick Facts
Patent No.
US 7,612,058
App. No.
10/998,400
Granted
Nov 3, 2009
Kind
B2
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 (178)

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:

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

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:

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:

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:

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:

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

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:

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:

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:

Assignments (6)
SECURITY INTEREST Recorded May 29, 2024
From: ORGANON LLC
To: U.S. BANK TRUST COMPANY, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 067545/0934 →
SECURITY INTEREST Recorded Mar 12, 2024
From: ORGANON LLC
To: U.S. BANK TRUST COMPANY, NATIONAL ASSOCIATION
Reel/Frame 066729/0749 →
SECURITY INTEREST Recorded Mar 12, 2024
From: ORGANON LLC
To: U.S. BANK TRUST COMPANY, NATIONAL ASSOCIATION
Reel/Frame 066729/0759 →
SECURITY INTEREST Recorded Mar 12, 2024
From: ORGANON LLC
To: JP MORGAN CHASE BANK, N.A.
Reel/Frame 066729/0769 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 19, 2021
From: MERCK SHARP & DOHME CORP.
To: ORGANON LLC
Reel/Frame 057223/0821 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →