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Patent US4310523A successfully refreshed from Google Patents.
US4310523A
Expired / Lapsed
US
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Combined antiestrogens and antigonadotropically effective antiandrogens for the prophylaxis and therapy of hyperplasia of the prostate
Assignee: Bayer Pharma AG
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Filing: 1980-10-10
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Granted: 1982-01-12
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Expires: 2000-10-10
Abstract
Abstract A pharmaceutical composition comprising an anti-estrogen and an antigonadotropically effective anti-androgen, e.g., in a weight ratio of anti-estrogen to anti-androgen of essentially 2:1 to 1:10 is effective for the prophylaxis and therapy of prostate hyperplasia. Suitable anti-estrogens include, for example, tamoxifen. Antigonadotropically active anti-androgens preferably are steroids having anti-androgenic and progestational properties, e.g., cyproterone acetate.
Inventors
- 👤 Friedmund Neumann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 12:00
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K31/00; A61K31/56; A61K31/565; A61K31/57; A61P; A61P13/00; A61P13/02; A61P15/00; A61P3/00; A61P3/04
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
47 words
A pharmaceutical composition for the prophylaxis or treatment of prostate hyperplasia comprising an antiestrogen which is (Z)-2-[p-(1,2-diphenyl-1-butenyl)-phenoxy]-N,N-dimethylethylamine, 1-(2-[4-(6-methoxy-2-phenyl-3,4-dihydro-1-naphthyl)-phenoxy]-ethyl)-pyrrolidone hydrochloride, 1-[p-(2-diethylaminoethoxy)-phenyl]-2-(p-methoxyphenyl)-1-phenylethanol, tri-(p-anisolyl)-chloroethylene, 1-[p-(β-diethylaminoethoxy)phenyl]-1,2-diphenylchloroethylene, bis(p-acetoxyphenyl)cyclohexylidenemethane, 1-[2-(p-[α-(p-methoxyphenyl)-β-nitrostyryl]-phenoxy)-ethyl]-pyrrolidine, or 11α-methoxy-17α-ethynyl-1,3,5(10)-estratriene-3,17β-diol, and a antigonadotropically effective anti-androgen, in respective amounts such that the combination is effective for prophylaxis or treatment of prostate hyperplasia.
Claim 2
Dependent Claim
47 words
A pharmaceutical composition for the prophylaxis or treatment of prostate hyperplasia comprising an antiestrogen which is (Z)-2-[p-(1,2-diphenyl-1-butenyl)-phenoxy]-N,N-dimethylethylamine, 1-(2-[4-(6-methoxy-2-phenyl-3,4-dihydro-1-naphthyl)-phenoxy]-ethyl)-pyrrolidone hydrochloride, 1-[p-(2-diethylaminoethoxy)-phenyl]-2-(p-methoxyphenyl)-1-phenylethanol, tri-(p-anisolyl)-chloroethylene, 1-[p-(β-diethylaminoethoxy)phenyl]-1,2-diphenylchloroethylene, bis(p-acetoxyphenyl)cyclohexylidenemethane, 1-[2-(p-[α-(p-methoxyphenyl)-β-nitrostyryl]-phenoxy)-ethyl]-pyrrolidine, or 11α-methoxy-17α-ethynyl-1,3,5(10)-estratriene-3,17β-diol, and a antigonadotropically effective anti-androgen, in respective amounts such that the combination is effective for prophylaxis or treatment of prostate hyperplasia.
Claim 3
Dependent Claim
11 words
The composition of claim 1, further comprising a pharmaceutically acceptable carrier.
Claim 4
Dependent Claim
16 words
The composition of claim 1, wherein the weight ratio of anti-estrogen to anti-androgen is about 2:1-1:10.
Claim 5
Dependent Claim
14 words
The composition of claim 1, wherein the anti-estrogen is (Z)-2-[p-(1,2-diphenyl-1-butenyl)-phenoxy]-N,N-dimethylethylamine, 1-(2-[4-(6-methoxy-2-phenyl-3,4-dihydro-1-naphthyl)-phenoxy]-ethyl)-pyrrolidine hydrochloride, or 1-[p-(2-diethylaminoethoxy)-phenyl]-2-(p-methoxyphenyl)-1-phenylethanol.
Claim 6
Dependent Claim
10 words
The composition of claim 1 wherein (Z)-2-[p-(1,2-diphenyl-1-butenyl)-phenoxy]-N,N-dimethylethylamine is the anti-estrogen.
Claim 7
Dependent Claim
10 words
The composition of claim 1, wherein the anti-estrogen is 11α-methoxy-17α-ethynyl-1,3,5(10)-estratriene-3,17β-diol.
Claim 8
Dependent Claim
114 words
The composition of claim 1, wherein the antigonadotropically effective anti-androgen is a compound of the formula ##STR6## wherein R 1 and R 2 are hydrogen or together form an additional carbon-to-carbon bond or methylene; R 3 is C 1-8 alkanoyl; Y is oxygen or the grouping (H, OR 4 ) wherein R 4 is hydrogen, C 1-8 alkanoyl or C 1-5 alkyl; X 1 is hydrogen or chlorine; and X 2 is hydrogen, fluorine, chlorine or C 1-5 alkyl; or ##STR7## wherein R 5 and R 6 are hydrogen or together are methylene; X is hydrogen, fluorine or chlorine, and A-B is ##STR8## wherein R 7 and R 8 are each C 1-8 alkanoyl.
Claim 9
Dependent Claim
13 words
The composition of claim 7, wherein the antigonadtropically effective anti-androgen is 6-chloro-17-hydroxy-1α,2α-methylenepregna-4,6-diene-3,20-dione acetate.
Claim 10
Dependent Claim
13 words
The composition of claim 7, wherein the antigonadotropically effective anti-androgen is 6-chloro-17-hydroxypregna-4,6-diene-3,20-dione acetate.
Claim 11
Dependent Claim
13 words
The composition of claim 4, wherein the antigonadotropically effective anti-androgen is 6-chloro-17-hydroxy-1α,2α-methylenepregna-4,6-diene-3,20-dione acetate.
Claim 12
Dependent Claim
13 words
The composition of claim 4, wherein the antigonadotropically effective anti-androgen is 6-chloro-17-hydroxy-pregna-4,6-diene-3,20-dione acetate.
Claim 13
Dependent Claim
13 words
The compound of claim 5, wherein the antigonadotropically effective anti-androgen is 6-chloro-17-hydroxy-1α,2α-methylenepregna-4,6-diene-3,20-dione acetate.
Claim 14
Dependent Claim
30 words
A pharmaceutical composition of claim 2, comprising 5-50 mg of (Z)-2-[p-(1,2-diphenyl-1-butenyl)-phenoxy]-N,N-dimethylethylamine and 5-50 mg of 6-chloro-17-hydroxy-1α,2α-methylenepregna-4,6-diene-3,20-dione acetate, and the weight ratio of anti-estrogen to anti-androgen is about 2:1 to 1:10.
Claim 15
Dependent Claim
29 words
A method for prophylaxis or treatment of prostate hyperplasia which comprises administering an amount of a composition of claim 1 effective for the prophylaxis or treatment of prostate hyperplasia.
Claim 16
Dependent Claim
29 words
A method for prophylaxis or treatment of prostate hyperplasia which comprises administering an amount of a composition of claim 3 effective for the prophylaxis or treatment of prostate hyperplasia.
Claim 17
Dependent Claim
27 words
The method of claim 15, wherein the daily dosage of the anti-estrogen is 5-100 mg and the daily dosage of the anti-gonadotropically effective anti-androgen is 5-100 mg.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-01-11 | 1985-07-13 | 1986-01-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-01-11 | 1989-07-13 | 1990-01-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-01-11 | 1993-07-13 | 1994-01-12 | $7700.00 | Window Closed / Lapsed |