IP Library Patent Application 12921083
Patent Application
App. No. 12/921,083

METHOD FOR INHIBITING THE BUILD-UP OF ARTERIAL PLAQUE BY ADMINISTERING FULLERENES

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Patent No.
US None
App. No.
12/921,083
Abstract

Disclosed herein are methods of inhibiting the build-up of arterial plaque in a subject in need thereof. These methods comprise administering to the subject in need thereof a therapeutically effective amount of fullerenes.

Claims (81)

1 . A method of inhibiting the build-up of arterial plaque, comprising:

administering a therapeutically effective amount of one or more fullerenes to a subject in need thereof.

2 . The method of claim 1 , wherein said fullerenes inhibit accumulation of LDL in foam cells of the subject.

3 . The method of claim 1 , wherein said fullerenes are delivered directly to the foam cells of the subject.

4 . The method of claim 1 , wherein said fullerenes are administered as cholesterol modified fullerenes.

5 . The method of claim 1 , wherein said fullerenes are administered orally or intravenously.

6 . The method of claim 1 , wherein said fullerenes are administered as a pharmaceutical composition which comprises at least one carrier and/or at least one excipient.

7 . The method of claim 1 , wherein said fullerenes are administered to the subject in combination with at least one other active ingredient.

8 . The method of claim 1 , wherein said subject is a human.

9 . The method of claim 1 , wherein at least one of said one or more fullerenes is a synthetically modified fullerene of the formula

Z m -F-Y n

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage.

Z and Y are positioned near respective opposite poles of C p ;

m=1-5 and Z is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y is a lipophilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms.

10 . The method of claim 9 , wherein p is 60 or 70.

11 . The method of claim 10 , wherein p is 70.

12 . The method of claim 1 , wherein at least one of said one or more fullerenes is a synthetically modified fullerene of the formula

Z(C p )Y

wherein p=60-200 carbons, preferably p=60 or 70; Y is a lipophilic moiety covalently connected to C p , optionally through a linking group, at or near a pole thereof, and wherein Z is a lipophilic moiety, amphiphilic moiety, or a hydrophilic moiety covalently connected to C p , optionally through a linking group, at or near a pole opposite to said Y.

13 . The method of claim 12 , wherein C p is C 70 .

14 . The method of claim 1 , wherein at least one of said one or more fullerenes is a synthetically modified fullerene of the formula

Z′ m -F-Y′ n ;

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage;

Z′ and Y′ are positioned near respective opposite poles of C p ;

m=1-5 and Z′ is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y′ is a hydrophilic or amphiphilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms.

15 . The method of claim 14 , wherein p is 60 or 70.

16 . The method of claim 15 , wherein p is 70.

17 . The method of claim 1 , wherein at least one of said one or more fullerenes is a synthetically modified fullerene of the formula

Z′(C p )Y′

wherein: p=60-200 carbons, preferably p=60 or 70; Y′ is a hydrophilic or amphiphilic moiety covalently connected to C p , optionally through a linking group, at or near a pole thereof, and wherein Z′ is a hydrophilic or amphiphilic moiety covalently connected to C p , optionally through a linking group, at or near a pole opposite to said Y′.

18 . The method of claim 17 , wherein C p =C 70 .

19 . The method of claim 1 , wherein at least one of said one or more fullerenes is a compound shown in the present figures.

20 . The method of claim 1 , wherein at least one of said one or more fullerenes is selected from the group consisting of compound 5, compound 7, and combinations thereof.

21 . A synthetically modified fullerene of the formula

Z m -F-Y n

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage.

Z and Y are positioned near respective opposite poles of C p ;

m=1-5 and Z is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y is a lipophilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms,

for use in inhibiting the build-up of arterial plaque.

22 . A synthetically modified fullerene of the formula

Z m -F-Y n

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage.

Z and Y are positioned near respective opposite poles of C p ;

m=1-5 and Z is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y is a lipophilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms,

for preparation of a medicament for inhibiting the build-up of arterial plaque.

23 . A synthetically modified fullerene of the formula

Z′ m -F-Y′ n ;

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage;

Z′ and Y′ are positioned near respective opposite poles of C p ;

m=1-5 and Z′ is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y′ is a hydrophilic or amphiphilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms,

for use in inhibiting the build-up of arterial plaque.

24 . A synthetically modified fullerene of the formula

Z′ m -F-Y′ n ;

wherein F is a fullerene of formula C p or X@C p , the fullerene having two opposing poles and an equatorial region;

C p represents a fullerene cage having p carbon atoms, and X@C p represents such a fullerene cage having a chemical group X within the cage;

Z′ and Y′ are positioned near respective opposite poles of C p ;

m=1-5 and Z′ is a hydrophilic, lipophilic, or amphiphilic chemical moiety;

n=1-5 and Y′ is a hydrophilic or amphiphilic chemical moiety;

p=60-200 and p is an even number; and

X, if present, represents one or more metal atoms within the fullerene (F), optionally in the form of a trinitride of formula G i=1-3 H k=3-i N in which G and H are metal atoms,

for preparation of a medicament for inhibiting the build-up of arterial plaque.

Assignments (1)
RELEASE OF SECURITY INTEREST Recorded Feb 6, 2015
From: HANSEN MEDICAL, INC.
To: LUNA INNOVATIONS INCORPORATED
Reel/Frame 034914/0407 →