# US 5,348,974 A · Tocotrienols in the treatment of hypercholesterolemia, hyperlipidemia and thromboembolic disorders

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- Number: US 5,348,974 A
- Document ID: US5348974A
- Status: Granted
- Kind: A
- Application number: 08/015,778
- Filed: 1993-02-10
- Granted: 1994-09-20
- Earliest claimed: 1989-10-04
- Assignees: Bristol-Myers Squibb Company
- Inventors: John J. Wright; Bradley C. Pearce; Rex Parker; Asaf A. Qureshi
- Web page: https://patentgrep.com/patent/US5348974A

## CPC

- A61K 31/355: Tocopherols, e.g. vitamin E
- A61P 3/06: Antihyperlipidemics
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 311/72: 3,4-Dihydro derivatives having in position 2 at least one methyl radical and in position 6 one oxygen atom, e.g. tocopherols
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

This invention relates to the use of tocotrienol, gamma-tocotrienol and delta-tocotrienol in reducing hypercholesterolemia, hyperlipidemia and thromboembolic disorders in mammals. The isolation of these tocotrienols from natural sources and their chemical synthesis is disclosed. The present invention also relates to prodrugs and pharmaceutical compositions of gamma-tocotrienol, delta-tocotrienol and tocotrienol and uses thereof.

## Claims

### Claim 1

A method of reducing, in a bird or a mammal, the platelet aggregation to adenosine diphosphate, epinephrine or Collagen in platelet rich plasma and whole blood which comprises administering to such bird or mammal a safe and effective amount of substantially pure gamma-tocotrienol, substantially pure delta-tocotrienol, substantially pure tocotrienol, or mixtures thereof.

### Claim 2

A method of reducing, in a bird or mammal, thromboxane A.sub.2 and platelet factor 4 levels providing antithrombotic effectiveness which comprises administering to such bird or mammal a safe and effective amount of substantially pure gamma-tocotrienol, substantially pure delta-tocotrienol, substantially pure tocotrienol, or mixtures thereof.

### Claim 3

A method of reducing, in a bird or a mammal, the platelet aggregation to adenosine diphosphate, epinephrine or Collagen in platelet rich plasma and whole blood which comprises administering to such bird or mammal a safe and effective amount of the prodrug of gamma-tocotrienol, delta-tocotrienol or tocotrienol, or mixtures thereof.

### Claim 4

A method of reducing, in a bird or a mammal, thromboxane A.sub.2 and platelet factor 4 levels providing antithrombotic effectiveness which comprises administering to such bird or mammal a safe and effective amount of the prodrug of gamma-tocotrienol, delta-tocotrienol or tocotrienol, or mixtures thereof.

### Claim 5 (depends on 1, 2, 3, 4)

The method of any one of claims 1, 2, 3 and 4 wherein the tocotrienol is the d-isomer.

### Claim 6 (depends on 1, 2, 3, 4)

The method of any one of claims 1, 2, 3 and 4 wherein the tocotrienol is the d, l racemic mixture.