Method of treating or preventing alopecia

Details Method of treating or preventing alopecia Method of treating or preventing alopecia

1996-11-29

2003-04-22

Padmanabhan, Sreeni (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Sulfur, selenium or tellurium compound

C514S467000, C514S450000, C514S457000, C514S025000, C514S105000, C514S880000, C424S600000

Reexamination Certificate

active

06552089

ABSTRACT:

BACKGROUND OF THE INVENTION
Alopecia which is the partial or complete loss of hair may result from genetic factors, aging, antineoplastic chemotherapy or other causes. Noncicatricial alopecia occurs without scarring or gross atrophic changes. These types of alopecia include males pattern baldness, toxic alopecia, alopecia areata and trichotillomania. In recent years toxic alopecia which is by antineoplastic chemotherapy has become a more common problem as the use of chemotherapy for neoplastic diseases has expanded. This is one of the toxic effects that is seen frequently with alkylating agents, anti-metabolites, plant alkaloids, anti-tumor antibiotics and interferons is alopecia. This problem is particularly distressing to patients who are recovering from chemotherapy because it persists being after any period of hospitalization is required and causes many patients deep psychological difficulties.
Male pattern baldness and other types of alopecia have been resistant to treatment and at the present time, minoxidil is the only recognized therapy for male pattern baldness.
A composition obtained from the bacteria
Serratia marcescens
has been used to protect against the alopecia which is associated with the use of cytosine arabinoside and doxorubicin. This composition had no effect on alopecia which was induced by cyclophosphamide.
The applicants have discovered that noncicatricial or nonscarring alopecia including the alopecia associated with the therapeutic doses of antineoplastic agents may be avoided or reduced by the prior concomitant or subsequent administration of an effective amount of an effective tellurium compound.
It is therefore a primary object of the invention to provide a method for preventing and/or treating alopecia.
It is also an object of the invention to provide a method for preventing alopecia which is induced by antineoplastic agents.
SUMMARY OF THE INVENTION
The invention comprises a method for preventing or treating nonscarring alopecia, said method comprising administering an effective amount of a tellurium compound.
DETAILED DESCRIPTION OF THE INVENTION
The tellurium compounds for use in the invention include those of the formula:
or
TeO
2
or complexes of TeO
2
  (C)
or
PhTeCl
3
  (D)
or
TeX
4
, when X is Cl, Br or F
or
(C
6
H
5
)
4
P+(TeCl
3
(O
2
C
2
H
4
))—  (E)
wherein Q is Te or Se; t is 1 or 0; u is 1 or 0; v is 1 or 0; R, R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, and R
9
are the same or different and are independently selected from the group consisting of hydrogen, hydroxyalkyl of 1 to 5 carbons, hydroxy, alkyl or from 1 to 5 carbon atoms, halogen, haloalkyl of 1 to 5 carbon atoms, carboxy, alkylcarbonylalkyl of 2 to 10 carbons, alkanoyloxy of 1 to 5 carbon atoms, carboxyalkyl of 1 to 5 carbons atoms, acyl, amido, cyano, amidoalkyl of 1 to 5 carbons, N-monoalkylamidoalkyl of 2 to 10 carbons, N,N-dialkylamidoalkyl of 4 to 10 carbons, cyanoalkyl of 1 to 5 carbons alkoxy of 1 to 5 carbon atoms, alkoxyalkyl of 2 to 10 carbon atoms and —COR
10
wherein R
10
is alkyl of 1 to 5 carbons; and X is halogen; while the ammonium salt is illustrated, it is understood that other pharmaceutically acceptable salts such as K+ are within the scope of the invention. The compounds with the five membered rings are preferred.
As used herein and in the appended claims, the term alkyl of 1 to 5 carbon atoms includes straight and branched chain alkyl groups such as methyl; ethyl; n-propyl; n-butyl, and the like; the term hydroxyalkyl of 1 to 5 carbon atoms includes hydroxymethyl; hydroxyethyl; hydroxy-n-butyl; the term halkoakyl of 1 to 5 carbon atoms includes chloromethyl; 2-iodoethyl; 4-bromo-n-butyl; iodoethyl; 4-bromo-n-pentyl and the like; the term alkanoyloxy of 1 to 5 carbon atoms includes acetyl, propionyl, butanoyl and the like; the term carboxyalkyl includes carboxymethyl, carboxyethyl, ethylenecarboxy and the like; the term alkylcarbonylalkyl includes methanoylmethyl, ethanoylethyl and the like; the term amidoalkyl includes —CH
2
CONH
2
; —CH
2
CH
2
CONH
2
; —CH
2
CH
2
CH
2
CONH
2
and the like; the term cyanoalkyl includes —CH
2
CN; —CH
2
CH
2
CN; —CH
2
CH
2
CH
2
CN and the like; the alkoxy, of 1 to 5 carbon atoms includes methoxy, ethoxy, n-propoxy, n-pentoxy and the like; the terms halo and halogen are used to signify chloro, bromo, iodo and fluoro; the term acyl includes R
16
CO wherein R
16
is H or alkyl of 1 to 5 carbons such as methanoyl, ethanoyl and the like; the term aryl includes phenyl, alkylphenyl and naphthyl; the term N-monoalkylamidoalkyl includes —CH
2
CH
2
CONHCH
3
, —CH—
2
CONHCH
2
CH
3
; the term N,N-dialkylamidoalkyl includes —CH
2
CON(CH
3
)
2
; CH
2
CH
2
CON(CH
2
—CH
3
)
2
. Compounds which are based on tellurium are the presently preferred compounds of the invention. The tellurium based compounds that are preferred include those of the formula:
wherein X is halogen. The preferred halogen species is chloro.
Other compounds which are based on tellurium and may be used in the practice of the invention include PhTeCl
3
, TeO
2
and TeX
4
(C
6
H
5
)
4
P+(TeCl
3
(O
2
C
2
H
4
))—(Z. Naturforsh, 36, 307-312 (1981). Compounds of the following structure are also included:
Other compounds useful for the practice of invention include:
wherein R
11
, R
12
, R
13
and R
14
are independently selected from the group consisting of hydrogen, hydroxy-alkyl of 1-5 carbons atoms, hydroxy and alkyl of 1-5 carbons atoms.
Useful dihydroxy compounds for use in the preparation of compounds of structure A or B, include those of formula I wherein R, R
1
, R
4
and R
5
are as shown in the Table:
TABLE
(I)

R
R
1
R
4
R
5
H
H
H
H
H
Cl
H
H
H
OCH
3
H
H
H
COOCH
3
H
H
H
H
CN
H
H
CHO
H
H
H
H
COOH
H
H
CH
2
COOH
H
H
H
H
CH
2
COOCH
3
H
H
I
H
H
H
H
Br
H
H
H
CONH
2
H
H
H
CH
2
OH
H
H
COOH
H
H
Other dihydroxy compounds for use in the preparation of compounds A and B include those of formula II wherein R, R
1
, R
2
, R
3
, R
4
and R
5
are as shown in the Table:
(II)

R
R
1
R
2
R
3
R
4
R
5
H
H
H
H
H
H
H
H
Cl
H
H
H
H
CH
2
OH
H
H
H
H
H
H
OH
H
H
H
H
H
H
CH
3
H
H
H
H
H
CH
2
Cl
H
H
H
H
H
COOH
H
H
H
H
H
CH
2
COOH
H
H
H
H
H
CHO
H
H
H
H
H
H
H
CH
2
CHO
H
H
CONH
2
H
H
2
CH
3
H
H
H
CN
H
H
H
H
H
H
CH
2
COHN
2
H
H
H
H
COOCH
3
H
3
H
H
H
3
OCH
3
H
H
H
Other dihydroxy compounds for use in making compound of formula A and B include those of formula III wherein R, R
1
, R
2
, R
3
, R
4
and R
5
are as shown in the Table.
(III)

R
R
1
R
2
R
3
R
4
R
5
R
8
R
9
H
H
H
H
H
H
H
H
H
H
Cl
H
H
H
H
H
H
H
H
H
Br
H
H
H
H
H
OCH
3
H
H
H
H
H
H
H
CONH
2
H
H
H
H
H
H
Br
H
H
H
H
H
H
H
H
H
H
CH
2
COOH
H
H
H
H
H
Cl
Cl
H
H
H
H
H
CH
2
COOH
H
H
H
H
H
H
H
H
CH
3
H
H
H
H
H
H
CH
3
H
H
H
H
H
H
H
CH
2
Cl
H
H
H
H
H
H
H
H
H
I
H
H
H
H
H
CH
2
CN
H
H
H
H
H
H
H
H
H
H
CH
2
CH
2
OH
H
H
H
Additional dihydroxy compounds include those of formula IV wherein R, R
1
, R
2
, R
3
, R
4
and R
5
are as shown in the Table.
(IV)

R
R
1
R
2
R
3
R
4
R
5
R
6
R
7
R
8
R
9
H
H
H
H
H
H
H
H
H
H
H
H
Cl
H
H
H
Cl
H
H
H
H
H
Cl
Cl
H
H
H
H
H
H
H
H
CONCH
3
H
H
H
Br
H
H
H
H
H
Br
H
H
H
CON(CH
3
)
2
H
H
H
H
H
H
OCH
3
H
H
H
H
H
H
H
H
H
H
OCH
3
H
H
H
H
H
H
H
H
H
CH
2
COOH
H
H
H
H
H
H
H
COOH
H
H
H
H
H
H
H
H
CH
3
H
H
H
H
H
H
H
H
CH
3
H
H
H
H
CH
3
H
H
H
H
H
CH
2
CH
3
H
H
H
H
H
Cl
H
H
H
CH
2
CN
H
H
CH
2
OH
H
H
H
H
H
H
H
H
I
H
H
H
H
CN
H
H
CH
2
CH
2
COOH
H
H
H
H
H
H
H
H
H
H
CHO
H
H
H
H
H
H
H
H
H
H
F
H
H
H
H
H
H
Compounds of the following formula are also included:
herein R
15
, R
16
, R
17
and R
18
are independently selected from halogen, alkyl of 1-5 carbons; aryl, acyl of 1-5 carbon hydroxyalkyl of 1-5 carbons and aminoalkyl of 1-5 carbons may be made by reacting the appropriate di, tri or tetrahaloselenide or telluride with the appropriate hydroxy compound which may be of the formula: HO—R
19
; wherein R
19
; is alkyl of 1 to 5 carbons, haloalkyl of 1 to 5 carbons, aryl, alkylaryl, alkylamido of 1 to 5 carbons, alkylcarbonyl of 1 to 5 carbons, cyanoalkyl of 1 to 5 carbons, cyanoalkyl of 1 to 5 carbons, and an alkoxyalkyl of 2 to 10 carbons. Specific examples of R
16
include methyl, ethyl, n-pr

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