Patent US4684635A successfully refreshed from Google Patents.
US4684635A
Expired / Lapsed
US
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Compositions and methods for inhibiting the action of androgens
Assignee: Individual
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Filing: 1986-03-27
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Granted: 1987-08-04
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Expires: 2006-03-27
Abstract
Abstract Synergistic compositions for inhibiting the action of androgens comprise the combination in a single topical preparation of a 5α-reductase enzyme inhibitor and an androgen receptor blocking agent in a pharmaceutically and dermatologically acceptable vehicle. The compositions may be topically applied to affected areas of the skin in the treatment or prevention of sebaceous gland hypertrophy, hirsutism and male-pattern baldness in mammals. The inhibitor and blocking agent are present in the composition in a weight ratio of about 1:20 to 5:1, with the inhibitor comprising up to about 0.1% w/v of the composition and the blocking agent comprising up to about 1% w/v of the composition.
Inventors
- 👤 Norman Orentreich
- 👤 Jonathan R. Matias
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 17:05
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/56; A61K31/57; A61K31/58; A61K31/585
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
64 words
A topical composition for the treatment of sebaceous gland hypertrophy and hirsutism comprising therapeutically and synergistically effective amounts of (a) an inhibitor of the conversion of testosterone to dihydrotestosterone by the 5α-reductase enzyme and (b) a blocking agent which blocks the binding of dihydrotestosterone to receptor protein in cell cytoplasm and a pharmaceutically and dermatologically acceptable vehicle for said inhibitor and said blocking agent.
Claim 2
Dependent Claim
64 words
A topical composition for the treatment of sebaceous gland hypertrophy and hirsutism comprising therapeutically and synergistically effective amounts of (a) an inhibitor of the conversion of testosterone to dihydrotestosterone by the 5α-reductase enzyme and (b) a blocking agent which blocks the binding of dihydrotestosterone to receptor protein in cell cytoplasm and a pharmaceutically and dermatologically acceptable vehicle for said inhibitor and said blocking agent.
Claim 3
Dependent Claim
24 words
A composition according to claim 1 wherein said inhibitor and said blocking agent are present in the weight ratio of about 1:20 to 5:1.
Claim 4
Dependent Claim
24 words
A composition according to claim 1 wherein said inhibitor and said blocking agent are present in the weight ratio of about 1:1 to 1:2.
Claim 5
Dependent Claim
34 words
A composition according to claim 1 wherein said inhibitor comprises up to about 0.1% and said blocking agent comprises up to about 1.0% of the composition, said percentages being on the basis of weight/volume.
Claim 6
Dependent Claim
29 words
A composition according to claim 1 wherein said inhibitor is selected from the group consisting of progesterone, 17β-carboxylic acid derivatives of testosterone, desoxycorticosterone, desoxycorticosterone acetate, 19-nor-testosterone, 4-pregnen-20β-ol-3-one and 17α-hydroxyprogesterone.
Claim 7
Dependent Claim
11 words
A composition according to claim 1 wherein said inhibitor is progesterone.
Claim 8
Dependent Claim
31 words
A composition according to claim 1 wherein said blocking agent is selected from the group consisting of spironolactone, cyproterone acetate, flutamide, trimethyltrienolone, hydroxy-flutamide, canrenone, canrenoic acid, 5,5-dimethyl-3-[4-nitro-3(trifluoromethyl)phenyl]-2,4-imidazolidinedione and 5,6-dihydro-2-methyl-4-[4- nitro-3-(trifluromethyl)phenyl]-2H-1,2,4-oxadiozin-3-(4H)- one.
Claim 9
Dependent Claim
17 words
A composition according to claim 1 wherein said vehicle comprises water, alcohol, acetone or a combination thereof.
Claim 10
Dependent Claim
25 words
A composition according to claim 1 wherein said vehicle is selected from the group consisting of solutions, tinctures, creams, ointments, gels, lotions and aerosol sprays.
Claim 11
Dependent Claim
19 words
A method of inhibiting the action of androgens comprising topically applying the composition of claim 1 to the skin.
Claim 12
Dependent Claim
13 words
A method according to claim 10 wherein said androgens are testosterone and dihydrotestosterone.
Claim 13
Dependent Claim
26 words
A method for treating sebaceous gland hypertrophy and hirsutism in mammals comprising topically applying the composition of claim 1 to the affected areas of the skin.
References Cited (Backward Citations)
US4347245A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-08-03 | 1991-02-02 | 1991-08-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-08-03 | 1995-02-02 | 1995-08-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-08-03 | 1999-02-02 | 1999-08-04 | $7700.00 | Window Closed / Lapsed |