IP Library Patent Application 12921106
Patent Application
App. No. 12/921,106

USING FULLERENES TO ENHANCE AND STIMULATE HAIR GROWTH

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Quick Facts
Patent No.
US None
App. No.
12/921,106
Abstract

Described herein are methods for treating lack of hair growth or a reduction or loss of existing hair by stimulating and/or restoring hair growth, or preventing hair loss. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a fullerene.

Claims (101)

1 . A method for preventing hair loss and/or promoting hair growth, comprising administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene of the formula

Z m —F—Y n

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

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

Z and Y are positioned near respective opposite poles of Cp;

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 Gi=1-3Hk=3-iN in which G and H are metal atoms.

2 . The method of claim 1 , wherein p is an even number between 60 and 120.

3 . The method of claim 2 , wherein p is an even number between 60 and 96.

4 . The method of claim 3 , wherein p is 60 or 70.

5 . The method of claim 4 , wherein p is 70.

6 . The method of claim 1 , wherein said synthetically modified fullerene is a prolate ellipsoid shaped fullerene having a major axis such that said poles are located at opposing ends of the major axis of the prolate ellipsoid fullerene.

7 . The method of claim 1 , wherein said synthetically modified fullerene is spheroid with opposing poles defined by an axis through opposing carbon rings.

8 . A method for preventing hair loss and/or promoting hair growth, comprising administering to a subject in need thereof a therapeutically effective amount of 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.

9 . The method of claim 8 , wherein C p is C 70 .

10 . The method of claim 8 , wherein Z is a hydrophilic moiety.

11 . The method of claim 10 , wherein the synthetically modified fullerene is compound 5.

12 . A method for preventing hair loss and/or promoting hair growth, comprising administering to a subject in need thereof a therapeutically effective amount of 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 3-i N in which G and H are metal atoms.

13 . The method of claim 12 , wherein p is an even number between 60 and 120.

14 . The method of claim 13 , wherein p is an even number between 60 and 96.

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 12 , wherein said synthetically modified fullerene is a prolate ellipsoid shaped fullerene having a major axis such that said poles are located at opposing ends of the major axis of the prolate ellipsoid fullerene.

18 . The method of claim 12 , wherein said synthetically modified fullerene is spheroid with opposing poles defined by an axis through opposing carbon rings.

19 . The method of claim 12 , wherein

Z′ comprises the formula A′ r B wherein A′ is a hydrophilic, lipophilic or amphiphilic chemical moiety, r=1-4, and B is a chemical linker connecting said A′ to the fullerene;

Y′ comprises the formula DE′ v wherein E′ is a hydrophilic or amphiphilic chemical moiety and, v=1-4, and D is a chemical linker connecting the chemical moiety Y′ to the fullerene.

20 . A method for preventing hair loss and/or promoting hair growth, comprising administering to a subject in need thereof a therapeutically effective amount of 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′.

21 . The method of claim 20 , wherein

(a) Z′ and Y′ are both amphiphilic;

(b) Z′ and Y′ are both hydrophilic;

(c) one of Z′ and Y′ is amphiphilic while the other is hydrophilic;

(d) Z′ is lipophilic and Y′ is hydrophilic; or

(e) Z′ is lipophilic and Y′ is amphiphilic.

22 . The method of claim 21 , wherein Z′ and Y′ are both hydrophilic.

23 . The method of claim 22 , wherein C p =C 70 .

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 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 preventing hair loss and/or promoting hair growth.

25 . 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 preventing hair loss and/or promoting hair growth.

26 . 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 preventing hair loss and/or promoting hair growth.

27 . 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 preventing hair loss and/or promoting hair growth.

28 . A method of preventing hair loss and/or promoting hair growth, comprising administering a therapeutically effective amount of a fullerene to a subject in need thereof.

29 . The method of claim 28 wherein said fullerene is derivatized.

30 . The method of claim 29 , wherein said fullerene is water soluble.

31 . The method of claim 30 , wherein said fullerene is Polyhydroxy-C60.

32 . A method for preventing hair loss and/or promoting hair growth, comprising administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene, wherein the synthetically modified fullerene is any one or more of the compounds shown in the present figures.

33 . The method of claim 32 , wherein the synthetically modified fullerene is selected from the group consisting of compound 5, compound 7, compound 10, compound 12, compound 13, compound 21, and compound 23.

34 . The method of claim 1 , wherein said fullerene is administered to an area of skin exhibiting or suspected of hair growth reduction or hair loss.

35 . The method of claim 34 , wherein said fullerene is injected at said area.

36 . The method of claim 34 , wherein said fullerene is administered topically.

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

38 . The method of claim 1 , wherein said hair loss is related to androgenetic alopecia (AGA), alopecia areata, and/or chemotherapy or radiation therapy.

39 . A compound selected from the group consisting of C 70 -ALM-PC (compound 21) and compound C 70 -ALM-inositol (compound 23).