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US4344941A
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Antiandrogenic 17α-substituted steroids
Assignee: Bayer Pharma AG
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Filing: 1980-10-20
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Granted: 1982-08-17
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Expires: 2000-10-20
Abstract
Abstract 17α-substituted steroids of the formula ##STR1## wherein R 1 is hydrogen, acyl, alkyl, alkenyl, alkyl or alkenyl interrupted by an oxygen atom, cyclopentyl, or tetrahydropyranyl, R 2 is alkyl or alkenyl of 2-6 carbon atoms, X is oxygen or the grouping H(OR 3 ) wherein R 3 is hydrogen, acyl, alkyl, alkenyl, alkyl or alkenyl interrupted by an oxygen atom, cyclopentyl, or tetrahydropyranyl, upon topical application, display antiandrogenic properties and can be utilized for the treatment of acne, seborrhea, alopecia and hirsutism.
Inventors
- 👤 Rudolf Wiechert
- 👤 Dieter Bittler
- 👤 Annerose Schleusener
- 👤 Manfred Albring
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 05:53
CPC Classifications
C; C07; C07J; C07J21/00; C07J21/005; C07J21/006; C07J1/00; C07J1/0003; C07J1/0033; C07J1/0037; C07J1/004; C07J1/0044; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
100 words
A 17α-substituted steroid of the formula ##STR4## wherein R 1 is hydrogen, an acyl group of a C 1-17 optionally substituted, hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 -alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl, R 2 is C 2-6 -alkenyl, X is oxygen or H(OR 3 ) wherein R 3 is hydrogen, an acyl group of a C 1-17 optionally substituted, hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl.
Claim 2
Dependent Claim
100 words
A 17α-substituted steroid of the formula ##STR4## wherein R 1 is hydrogen, an acyl group of a C 1-17 optionally substituted, hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 -alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl, R 2 is C 2-6 -alkenyl, X is oxygen or H(OR 3 ) wherein R 3 is hydrogen, an acyl group of a C 1-17 optionally substituted, hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl.
Claim 3
Dependent Claim
6 words
17β-Hydroxy-1α-methyl-17α-(1-methyl-2-propenyl)-5.alpha.-androstan-3-one, a compound of claim 1.
Claim 4
Dependent Claim
6 words
17β-Hydroxy-1α-methyl-17α-(2-propenyl)-5α-androstan-3-one, a compound of claim 1.
Claim 5
Dependent Claim
23 words
A pharmaceutical composition comprising an antiandrogenically topically effective amount of a composition of claim 1 and a pharmaceutically acceptable carrier for topical formulations.
Claim 6
Dependent Claim
41 words
A method of achieving a topical antiandrogenic effect in a patient suffering from a disease treatable by topical administration of an antiandrogenically active agent, which comprises topically administering to the patient an antiandrogenically effective amount of a compound of claim 1.
Claim 7
Dependent Claim
30 words
A compound of claim 1 wherein R 1 is C 1-5 alkyl, C 1-5 alkenyl, C 1-5 -alkyl or C 1-5 -alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl.
Claim 8
Dependent Claim
23 words
A compound of claim 1 wherein R 1 is an acyl group of a C 1-17 optionally substituted, hydrocarbon carboxylic or sulfonic acid.
Claim 9
Dependent Claim
20 words
A compound of claim 7 wherein R 1 is chloroacetyl, glycoloyl, trifluoroacetyl, succinyl, glutaryl, adipoyl, benzoyl, dimethylaminopropionyl, nicotinoyl or isonicotinoyl.
Claim 10
Dependent Claim
49 words
A compound of claim 7 wherein X is OR 3 wherein R 3 is an acyl group of a C 1-17 optionally substituted hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl.
Claim 11
Dependent Claim
10 words
A compound of claim 1 wherein R 1 is H.
Claim 12
Dependent Claim
49 words
A compound of claim 10 wherein X is OR 3 wherein R 3 is an acyl group of a C 1-17 optionally substituted hydrocarbon carboxylic or sulfonic acid, C 1-5 alkyl, C 1-5 -alkenyl, C 1-5 -alkyl or C 1-5 alkenyl interrupted by an oxa atom, cyclopentyl or tetrahydropyranyl.
References Cited (Backward Citations)
US3391168A
Cited
US3705180A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-08-16 | 1986-02-15 | 1986-08-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-08-16 | 1990-02-15 | 1990-08-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-08-16 | 1994-02-15 | 1994-08-17 | $7700.00 | Window Closed / Lapsed |