Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2000-10-26
2003-04-29
Cook, Rebecca (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S324000, C514S422000, C514S651000, C514S880000
Reexamination Certificate
active
06555532
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to methods of treating hair loss and promoting hair growth, and more particularly to a method of using estrogen receptor antagonists to promote hair growth in a subject in need of such treatment.
BACKGROUND OF THE INVENTION
Alopecia (baldness) is a deficiency of hair, either normal or abnormal, and is primarily a cosmetic problem in humans, although the negative psychological impact of hair loss is well known. See C. H. Mortimer et al.,
Clin. Exp. Dermatol.
9, 342-350 (1984). Dermatologists recognize many different types of alopecia, with androgenic alopecia being the most common cause of hair loss in both men and women. As this type of hair loss is more common and more severe in males, it is typically referred to as “male pattern baldness.” However, it is thought that androgenic alopecia affects more that one third of individuals of either sex who have a strong family history of hair loss. See W. F. Bergfield,
Clin. Dermatol.
6, 102-107 (1988).
One traditional treatment for alopecia is the method of hair transplantation. Typically, this method involves transplanting plugs of natural hair from areas of the scalp where hair is growing to bald areas. This procedure is costly, time-consuming, painful, and meets with only limited success.
Another common treatment for hair loss is the application of a chemical or drug for the purpose of stimulating hair growth. For example, U.S. Pat. No. 5,177,061 to Pickart proposes the topical application of glycyl-L-histidyl-L-lycine:copper(II) (GHL-Cu) and its derivatives to promote hair growth in warm-blooded animals (applicant specifically intends the disclosure of this and all other patent references cited herein to be incorporated herein by reference in their entirety). U.S. Pat. No. 4,832,946 to Green proposes a composition for topical application to mammalian hair or skin, comprising an amount of the cell-free supernatant from a culture of dermal papilla fibroblasts, which is said to increase hair growth in the rat. U.S. Pat. No. 5,358,714 to Green proposes the use of diacylglycerol activators of protein kinase C in order to increase or maintain hair growth in mammals, while U.S. Pat. No. 5,068,315 to Buultjens et al. proposes the application of purified hair growth regulating peptides (HGRP) to stimulate hair growth. It has also been suggested that retinoids, substituted pyrimidines, and immunosuppressants be used as possible treatments for hair loss, although methods utilizing these compounds have not been entirely successful in producing a reliable and safe method of inducing hair growth. See G. Bazzano et al.,
J. Invest. Dermatol.
101 (1 Supplement), 138S-142S (1993); H. Jiang et al.,
J. Invest. Dermatol.
104(4), 523-525 (1995).
In recent years, the topical application of minoxidil has been a widely-used method for treating androgenic alopecia. See A. R. Zapacosta,
N. Eng. J. Med.
303, 1480-81 (1980). U.S. Pat. No. 4,139,619 to Chidsey, proposes a topical composition of minoxidil and related iminopyrimidines to stimulate the conversion of vellus hair to terminal hair and increase the rate of growth of terminal hair. However, despite its popularity, minoxidil has not performed in a completely satisfactory fashion in promoting hair growth in all target populations.
SUMMARY OF THE INVENTION
A first aspect of the present invention is a method of treating alopecia in a subject in need thereof. The method comprises topically applying to the skin of the subject an estrogen receptor antagonist or a pharmaceutically acceptable salt thereof (an “active compound”) in an amount sufficient to treat alopecia.
A more general aspect of the present invention is a method of promoting hair growth in a subject in need thereof. The method comprises topically applying to the skin of the subject an active compound as given above in an amount sufficient to promote hair growth.
A second aspect of the present invention is a topical pharmaceutical formulation comprising an active compound as given above in an amount effective to treat alopecia or promote hair growth, in a pharmaceutically acceptable topical carrier.
A third aspect of the present invention is the use of an active compound as given above for the preparation of a medicament useful for carrying out a method as given above.
REFERENCES:
patent: 4139619 (1979-02-01), Chidsey, III
patent: 4596812 (1986-06-01), Chidsey, III et al.
patent: 4828837 (1989-05-01), Uster et al.
patent: 5026691 (1991-06-01), Kligman
patent: 5068315 (1991-11-01), Buultjens et al.
patent: 5177061 (1993-01-01), Pickart
patent: 5183814 (1993-02-01), Dukes
patent: 5225189 (1993-07-01), Pena
patent: 5358714 (1994-10-01), Green
patent: 5395842 (1995-03-01), Labrie et al.
patent: 5407944 (1995-04-01), Goldman
patent: 5574048 (1996-11-01), Cullinan
patent: 5643942 (1997-07-01), Hester, Jr. et al.
patent: 659414 (1995-06-01), None
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A.E. Wakeling et al.; A Potent Specific Antiestrogen with Clinical Potential,Cancer Res.51:3867-3873 (1991).
J. Bowler et al.; Novel Steroidal Pure Antiestrogens,ICI Pharmaceuticals, Research Dept.(1988).
H. Jiang et al.; Induction of Anagen in Telogen Mouse Skin by Topical Application of FK506, a Potent Immunosuppressant,J. of Invest. Derm.104:523-525 (1995).
J.P. Jacobs et al.; Use of Topical Minoxidil Therapy for Androgentic Alopecia in Women,Int'l J. of Derm. 32:758-762 (1993).
D.H. Rushton; Management of Hair Loss in Women,Derm. Therapy11 No. 1:47-53 (1993).
G. Bazzano et al.; Effect of Retinoids on Follicular Cells,J. of Invest. Derm., 101 No. 1 (Supp):138S-142S (1993).
H. Uno et al.; Chemical Agents and Peptides Affect Hair Growth,J. of Invest. Derm.101 No. 1 (Supp) 138S-142S (1993).
W.S. Branham et al.; ICI 182,780 Inhibits Endogenous Estrogen-Dependent Rat Uterine Growth and Tamoxifen-Induced Development Toxicity,Bio of Reproduct54:160-167 (1996).
C. Levesque et al.; Synthesis and Biological Activity of New Halo-Steroidal Antiestrogens,J. Med. Chem.34:1624-1630 (1991).
A. Claussner et al.; 11&bgr;-Amidoalkyl Estradiols, A New Series of Pure Antiestrogens,J. Steroid Biochem. Molec. Biol.41 No. 3-8:609-614 (1992).
D. Poirier et al.; Synthesis and Antiestrogenic Activity of Diaryl Thioether Derivatives,J. Med. Chem.37:1115-1125 (1994).
V.C. Jordan; Hydroxylated Antioestrogens: New Pharmacological Probes to Investigate Oestrogen and Antioestrogen Action,Hormone Antagonists110-111 (1982).
J. Rosen et al.; Intracellular Receptors and Signal Transducers and Activators of Transcription Superfamilies: Novel Targets for Small-Molecule Drug Discovery,J. Med. Chem.38 No. 25:4855-4874 (1995).
Archer, C.B., et al.,Alopecia neoplastica responsive to tamoxifen;The Royal Society of Medicine, vol. 83, No. 10, pp. 647-648 (1990).
Oh Hye-Sun
Smart Robert C.
Cook Rebecca
Myers Bigel & Sibley & Sajovec
North Carolina State University
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