Patent US4145416A successfully refreshed from Google Patents.
US4145416A
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Novel agents and novel methods for treatment of climacteric disturbances
Assignee: Bayer Pharma AG
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Filing: 1977-09-27
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Granted: 1979-03-20
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Expires: 1997-09-27
Abstract
Abstract Relief from climacteric disturbances is achieved by administration of first a combination of an estrogen of type 1 and an estrogen of type 2, approximately in a ratio of 2:1 to 1:8, daily over 10-12 days; then a combination of an estrogen of type 1 and an estrogen of type 2, approximately in a ratio of 2:1 to 1:8, and a progestogen, daily over 9-11 days; and thereafter an estrogen of type 2, or a placebo, daily over 6-8 days.
Inventors
- 👤 Ursula Lachnit-Fixson
- 👤 Friedmund Neumann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 00:56
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/56; A61K31/565
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
92 words
A pharmaceutical composition for the treatment of climacteric disturbances, to be administered in three phases, which comprises: for the first phase, 10-12 dosage units of a combination of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of from 2:1 to 1:8, for the second phase, 9-11 dosage units of a combination of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of from 2:1 to 1:8 and a progestational agent; and for the third phase, 6-8 dosage units of an estriol estrogen or a placebo.
Claim 2
Dependent Claim
92 words
A pharmaceutical composition for the treatment of climacteric disturbances, to be administered in three phases, which comprises: for the first phase, 10-12 dosage units of a combination of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of from 2:1 to 1:8, for the second phase, 9-11 dosage units of a combination of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of from 2:1 to 1:8 and a progestational agent; and for the third phase, 6-8 dosage units of an estriol estrogen or a placebo.
Claim 3
Dependent Claim
26 words
The composition of claim 1 wherein the ratio of estradiol estrogen to that of estriol estrogen for both the first and second phases is about 1:2.
Claim 4
Dependent Claim
13 words
The composition of claim 1 wherein the dosage units are in tablet form.
Claim 5
Dependent Claim
12 words
The composition of claim 1 wherein the estriol estrogen is estradiol valerate.
Claim 6
Dependent Claim
11 words
The composition of claim 1 wherein the estriol estrogen is estriol.
Claim 7
Dependent Claim
10 words
The composition of claim 1 wherein the progestogen is D-norgestrel.
Claim 8
Dependent Claim
14 words
The composition of claim 1 wherein the progestogen is norethisterone acetate or cyproterone acetate.
Claim 9
Dependent Claim
26 words
The composition of claim 1 wherein the amount of progestational agent in a daily dosage is equivalent in activity to 0.1 - 0.5 mg. of D-norgestrel.
Claim 10
Dependent Claim
24 words
The composition of claim 1 wherein the daily dosage of estradiol estrogen is equivalent in activity to 0.5 - 4 mg. of estradiol valerate.
Claim 11
Dependent Claim
22 words
The composition of claim 1 wherein the amount of estriol estrogen is equivalent in activity to 0.5 - 8 mg. of estriol.
Claim 12
Dependent Claim
12 words
The composition of claim 9 wherein the estradiol estrogen is estradiol valerate.
Claim 13
Dependent Claim
11 words
The composition of claim 10 wherein the estriol estrogen is estriol.
Claim 14
Dependent Claim
11 words
The composition of claim 8 wherein D-norgestrel is the progestational agent.
Claim 15
Dependent Claim
15 words
The composition of claim 8 wherein noretheristerone acetate or cyproterone acetate is the progestational agent.
Claim 16
Dependent Claim
88 words
In a method of alleviating the physiological and psychological disturbances of menopause comprising administrating to a female afflicted therewith an amount effective to alleviate those disturbances of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of 2:1 to 1:8 daily for a first 10-12 days and then daily for the next 9-11 days and thereafter an estriol estrogen or a placebo daily for the next 6-8 days, the improvement which comprises administering a progestogen daily concurrently with the estrogens during said next 9-11 days.
Claim 17
Dependent Claim
88 words
In a method of alleviating the physiological and psychological disturbances of menopause comprising administrating to a female afflicted therewith an amount effective to alleviate those disturbances of an estradiol estrogen and an estriol estrogen, approximately in a weight ratio of 2:1 to 1:8 daily for a first 10-12 days and then daily for the next 9-11 days and thereafter an estriol estrogen or a placebo daily for the next 6-8 days, the improvement which comprises administering a progestogen daily concurrently with the estrogens during said next 9-11 days.
Claim 18
Dependent Claim
27 words
The method of claim 15 wherein the ratio of estradiol estrogen to that of estriol estrogen in both the first and second administration phases is about 1:2.
Claim 19
Dependent Claim
44 words
The method of claim 15 wherein the amount of estradiol estrogen administered daily is equivalent in activity to 0.5 - 4 mg. of estradiol valerate and the amount of estriol estrogen administered daily is equivalent in activity to 0.5 - 8 mg. of estriol.
Claim 20
Dependent Claim
24 words
The method of claim 15 wherein the amount of progestational agent administered daily is equivalent in activity to 0.1 - 0.5 mg. of D-norgestrel.
Claim 21
Dependent Claim
12 words
The method of claim 18 wherein the hormone-active agents are administered orally.
Claim 22
Dependent Claim
18 words
The method of claim 19 wherein estradiol valerate is the estradiol estrogen and estriol is the estriol estrogen.
Claim 23
Dependent Claim
15 words
The method of claim 20 wherein D-norgestrel, norethisterone acetate or cyproterone acetate is the progestogen.
Claim 24
Dependent Claim
21 words
A composition comprising an estradiol estrogen and an estriol estrogen in a ratio from 2:1 to 1:8 and a progestational agent.
Claim 25
Dependent Claim
21 words
A composition comprising an estradiol estrogen and an estriol estrogen in a ratio from 2:1 to 1:8 and a progestational agent.
Claim 26
Dependent Claim
19 words
The composition of claim 22 wherein the ratio of estradiol estrogen to that of estriol estrogen is about 1:2.
References Cited (Backward Citations)
US3639599A
Cited
US3932635A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-19 | 1982-09-18 | 1983-03-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-19 | 1986-09-18 | 1987-03-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-19 | 1990-09-18 | 1991-03-20 | $7700.00 | Window Closed / Lapsed |