Use of pyrethroid compounds to promote hair growth

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

Reexamination Certificate

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Details

C514S880000

Reexamination Certificate

active

06288112

ABSTRACT:

BACKGROUND OF THE INVENTION
Unwanted hair loss can plague both men and women of all ages. It can arise as the result of a variety of underlying causes, including hormonal imbalance, genetic redisposition and exposure to toxic substances. Alopecia areata is a non-scarring inflammatory hair loss disease that can affect men, women, and even children. The factors that activate the onset of alopecia and the mechanisms of its development are not well understood. It is characterized clinically by the sudden appearance of a round or oval patch of non-scarring and painless hair loss with spontaneous remissions and exacerbations (Weitzer,
Am. Fam. Physician
41(4):1197-1201 (1990)). The annual incidence of alopecia areata is approximately 2 per 10,000 population. 5% to 10% of patients, especially children, result in a total loss of all of the scalp hair (alopecia totalis). Although the disease itself is non-life threatening, the cosmetic and psychological impact on both patients and parents is tremendous. Patients usually suffer from a higher than normal rate of major depression and/or other anxiety disorder (Colon et al.,
Comprehensive Psychiatry
32(3): 245-251 (1991); Beard,
J. Am. Acad. Dermatol.
14(4):697-700 (1986)).
SUMMARY OF THE INVENTION
In general, the invention features, a method of promoting hair growth. The method includes administering to a subject, e.g., a human with an insufficient amount of hair or an insufficient rate of hair growth, an effective amount of a pyrethroid, e.g., a type I pyrethroid or, preferably, a type II pyrethroid, e.g., cypermethrin, deltamethrin, or fenvalerate. In a preferred embodiment, the pyrethroid is administered topically. The pyrethroid can be administered to the scalp, face, chest, legs, and other regions of the body. In a preferred embodiment, the pyrethroid is provided in a composition, e.g., a pharmaceutically acceptable composition. In a preferred embodiment, the weight percent of the pyrethroid ranges from 0.005% to 5%; the weight percent of the pyrethroid ranges from 0.01% to 2%. In a preferred embodiment, the compound is administered at any point in a hair cycle, e.g., in the anagen (growth) phase of hair growth; in the telogen (resting) phase of hair growth; in the catagen (the period between the telogen phase and the anagen phase) phase of hair growth.
In a preferred embodiment, the method includes: identifying a subject in need of hair growth promoting treatment; after administration of a pyrethroid compound, evaluating the effect of the administration on hair growth; the treatment can involve more than one administration, e.g., at least two, three, or four administrations, of the pyrethroid compound.
In a preferred embodiment, the subject can be male or female that suffers from genetic pattern baldness; suffers from a hormonal disorder which decreases hair growth; has received a treatment, e.g., radiation, or chemotherapy, or a drug which inhibits hair growth; or has had a surgical procedure, e.g., skin graft, which is in need of hair growth.
In another aspect, the invention features, a method of promoting hair growth. The method includes administering to a subject, e.g., a human with an insufficient amount of hair or an insufficient rate of hair growth, an effective amount of a compound of the formula:
wherein R
1
is
in which each of R
a
, R
b
, R
c
, and R
d
, independently, is H, fluoro, chloro, bromo, iodo, or C
1-4
alkyl. Alkyl can be either a straight or branched group. Some examples of alkyl groups are methyl, ethyl, propyl, isopropyl, butyl, isobutyl, and tert-butyl. R
2
is CN or C≡CH; and R
3
is
in which X is O, S, NH, or CH
2
; and each of R′ and R″, independently, is H, fluoro, chloro, bromo, iodo, or C
1-4
alkyl. The compound can exist as a salt, e.g., a hydrochloride salt. There can be more than one substituents on each aromatic ring, e.g., more than one R
d
, R′, or R″ on each ring.
In a preferred embodiment, the compound is administered topically. The compound can be administered to the scalp, face, chest, legs, and other regions of the body. In a preferred embodiment, the compound is provided in a composition, e.g., a pharmaceutically acceptable composition. In a preferred embodiment, the compound is administered at any point in a hair cycle, e.g., in the anagen (growth) phase of hair growth; in the telogen (resting) phase of hair growth; in the catagen (the period between the telogen phase and the anagen phase) phase of hair growth.
In a preferred embodiment, R
2
is CN. In a preferred embodiment, R
1
is
in which each of R
a
, R
b
and R
c
, independently, is H, fluoro, chloro, bromo, iodo, or C
1-4
alkyl. In a preferred embodiment, each of R
a
and R
b
, independently, is chloro or bromo; and R
c
is H. In a preferred embodiment, each of R
a
and R
b
, independently, is chloro; X is O; and each of R′ and R″, independently, is H. In a preferred embodiment, each of R
a
and R
b
, independently, is bromo; X is O; and each of R′ and R″, independently, is H. In a preferred embodiment, R
1
is
in which R
d
is H, fluoro, chloro, bromo, iodo, or C
1-4
alkyl. In a preferred embodiment, R
d
is chloro; X is O; and each of R′ and R″, independently, is H. In a preferred embodiment, X is O; each of R′ and R″, independently, is H.
In a preferred embodiment, the method includes: identifying a subject in need of hair growth promoting treatment; after administration of an effective amount of the compound, evaluating the effect of the administration on hair growth; the treatment can involve more than one administration, e.g., at least two, three, or four administrations, of the compound.
In a preferred embodiment, the subject can be male or female that suffers from genetic pattern baldness; suffers from a hormonal disorder which decreases hair growth; has received a treatment, e.g., radiation, or chemotherapy, or a drug which inhibits hair growth; or has had a surgical procedure, e.g., skin graft, which is in need of hair growth.
The invention also includes composition of the compound described herein. Accordingly, in another aspect, the invention features, a composition for promoting hair growth. The preparation can include a pyrethroid, e.g., a type I pyrethroid or, preferably, a type II pyrethroid (e.g., cypermethrin, deltamethrin, or fenvalerate), and a pharmaceutically acceptable carrier. In a preferred embodiment, the composition is sterile. In a preferred embodiment, the composition includes a fragrance. In a preferred embodiment, the weight percent of the pyrethroid in the composition ranges from 0.005% to 5%; the weight percent of the compound in the composition ranges from 0.01% to 2%. In a preferred embodiment, the compound is administered at any point in a hair cycle, e.g., in the anagen (growth) phase of hair growth; in the telogen (resting) phase of hair growth; in the catagen (the period between the telogen phase and the anagen phase) phase of hair growth.
In another aspect, the invention features, a kit for promoting hair growth. The kit includes, a compound described herein and instruction for use of the compound to promote hair growth.
In another aspect, the invention features, a container which includes a compound described herein, wherein the container has one ore more of the following properties: it contains less than 5.0, 1.0, 0.5, or 0.1 g of the compound described herein; it is air tight; it is waterproof; or in addition to the compound described herein, it contains a fragrance or other cosmetic ingredient.
By promoting hair growth is meant an increase in the total mass of hair or the total length of the hairs, in a unit area, e.g., per cm
2
, as compared to nontreated tissue. It can include one or more of: an increase in the length or growth rate of a hair shaft, an increase in the number of hairs, or an increase in the thickness of a hair. In a preferred embodiment, the growth rate is increased.
Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly underst

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