DE60309895T2 - Estrogenersatztherapie - Google Patents
Estrogenersatztherapie Download PDFInfo
- Publication number
- DE60309895T2 DE60309895T2 DE60309895T DE60309895T DE60309895T2 DE 60309895 T2 DE60309895 T2 DE 60309895T2 DE 60309895 T DE60309895 T DE 60309895T DE 60309895 T DE60309895 T DE 60309895T DE 60309895 T2 DE60309895 T2 DE 60309895T2
- Authority
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- Germany
- Prior art keywords
- estrogen
- dose
- phases
- substance
- activity
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US40633102P | 2002-08-28 | 2002-08-28 | |
| US406331P | 2002-08-28 | ||
| PCT/CA2003/001325 WO2004019954A1 (en) | 2002-08-28 | 2003-08-28 | Estrogen replacement regimen |
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| DE60309895D1 DE60309895D1 (de) | 2007-01-04 |
| DE60309895T2 true DE60309895T2 (de) | 2007-10-18 |
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| US8617597B2 (en) | 2006-07-06 | 2013-12-31 | Bayer Intellectual Property Gmbh | Pharmaceutical composition containing a tetrahydrofolic acid |
| DE102009007771B4 (de) | 2009-02-05 | 2012-02-16 | Bayer Schering Pharma Aktiengesellschaft | Bukkales Applikationssystem, 17α-Estradiol enthaltend |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| US8951996B2 (en) | 2011-07-28 | 2015-02-10 | Lipocine Inc. | 17-hydroxyprogesterone ester-containing oral compositions and related methods |
| US8633178B2 (en) | 2011-11-23 | 2014-01-21 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| MX2016011801A (es) * | 2014-03-12 | 2017-07-14 | Warner Chilcott Co Llc | Crema de estradiol de dosis baja. |
| EP3145489A1 (en) | 2014-05-22 | 2017-03-29 | TherapeuticsMD, Inc. | Natural combination hormone replacement formulations and therapies |
| LT3310345T (lt) | 2015-06-18 | 2021-06-25 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| CR20180042A (es) | 2015-06-18 | 2018-05-03 | Mithra Pharmaceuticals S A | Unidad de dosificación orodispersable que contiene un componente estetrol. |
| DK3701944T3 (da) | 2015-06-18 | 2022-03-14 | Estetra Srl | Oro-dispergerbar doseringsenhed indeholdende en estetrolkomponent |
| LT3310346T (lt) | 2015-06-18 | 2021-06-10 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| AU2016284459B2 (en) | 2015-06-22 | 2021-12-23 | Lipocine Inc. | 17-hydroxyprogesterone ester-containing oral compositions and related methods |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| WO2017173071A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
| WO2017173044A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd Inc. | Steroid hormone compositions in medium chain oils |
| KR102712911B1 (ko) | 2016-08-05 | 2024-10-04 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
| CN111989105B (zh) | 2018-04-19 | 2024-07-19 | 埃斯特拉私人有限责任公司 | 化合物以及它们在缓解绝经相关症状中的用途 |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
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| US4826831A (en) * | 1983-08-05 | 1989-05-02 | Pre Jay Holdings Limited | Method of hormonal treatment for menopausal or post-menopausal disorders involving continuous administration of progestogens and estrogens |
| EP0303306B1 (en) * | 1987-08-08 | 1993-03-10 | Akzo N.V. | Contraceptive implant |
| US4900734A (en) * | 1987-08-27 | 1990-02-13 | Maxson Wayne S | Novel pharmaceutical composition containing estradiol and progesterone for oral administration |
| US5108995A (en) * | 1987-09-24 | 1992-04-28 | Jencap Research Ltd. | Hormone preparation and method |
| US5256421A (en) * | 1987-09-24 | 1993-10-26 | Jencap Research Ltd. | Hormone preparation and method |
| US5422119A (en) * | 1987-09-24 | 1995-06-06 | Jencap Research Ltd. | Transdermal hormone replacement therapy |
| US5276022A (en) * | 1987-09-24 | 1994-01-04 | Jencap Research Ltd. | Hormone preparation and method |
| DE3888269T2 (de) * | 1987-09-24 | 1994-07-07 | Jencap Research Ltd | Hormon-Zusammensetzung und -Anwendung. |
| US5382873A (en) * | 1991-12-04 | 1995-01-17 | U.S. Philips Corporation | High-pressure discharge lamp with incandescing metal droplets |
| US5521166A (en) * | 1994-12-19 | 1996-05-28 | Ortho Pharmaceitical Corporation | Antiprogestin cyclophasic hormonal regimen |
| DE19513662A1 (de) * | 1995-04-08 | 1996-10-10 | Schering Ag | Pharmazeutisches Kombinationspräparat zur hormonalen Kontrazeption |
| CN1188189C (zh) * | 1995-06-07 | 2005-02-09 | 奥瑟－麦内尔制药公司 | 基质层含有17－脱乙酰基诺孕酯的经皮贴片及基质的用途 |
| US6506390B2 (en) * | 1996-06-25 | 2003-01-14 | Akzo Nobel | Progestogen-anti-progestogen regimens |
| CA2267743C (en) * | 1999-03-30 | 2011-07-26 | Robert F. Casper | Low dose estrogen interrupted hormone replacement therapy |
| US6653298B2 (en) * | 2000-01-14 | 2003-11-25 | Sterix Limited | Composition |
| DE10100911A1 (de) * | 2001-01-11 | 2002-08-01 | Schering Ag | Verfahren zur Hormonersatztherapie und dessen Darreichungsform |
-
2003
- 2003-08-28 AU AU2003264203A patent/AU2003264203A1/en not_active Abandoned
- 2003-08-28 PL PL03374762A patent/PL374762A1/xx not_active Application Discontinuation
- 2003-08-28 HR HR20050291A patent/HRP20050291A2/xx not_active Application Discontinuation
- 2003-08-28 DE DE60309895T patent/DE60309895T2/de not_active Expired - Lifetime
- 2003-08-28 US US10/526,064 patent/US8946198B2/en active Active
- 2003-08-28 UA UAA200502488A patent/UA82851C2/uk unknown
- 2003-08-28 WO PCT/CA2003/001325 patent/WO2004019954A1/en not_active Ceased
- 2003-08-28 NZ NZ538342A patent/NZ538342A/en unknown
- 2003-08-28 ES ES03790602T patent/ES2277139T3/es not_active Expired - Lifetime
- 2003-08-28 AT AT03790602T patent/ATE345804T1/de not_active IP Right Cessation
- 2003-08-28 KR KR1020057003209A patent/KR20050059092A/ko not_active Withdrawn
- 2003-08-28 PT PT03790602T patent/PT1539184E/pt unknown
- 2003-08-28 CN CNA038205157A patent/CN1678324A/zh active Pending
- 2003-08-28 BR BR0313921-2A patent/BR0313921A/pt not_active IP Right Cessation
- 2003-08-28 DK DK03790602T patent/DK1539184T3/da active
- 2003-08-28 RU RU2005108977/15A patent/RU2340345C2/ru not_active IP Right Cessation
- 2003-08-28 RS YUP-2005/0184A patent/RS20050184A/sr unknown
- 2003-08-28 MX MXPA05002294A patent/MXPA05002294A/es active IP Right Grant
- 2003-08-28 CA CA002495330A patent/CA2495330A1/en not_active Abandoned
- 2003-08-28 JP JP2004531341A patent/JP2005538150A/ja active Pending
- 2003-08-28 IL IL16658503A patent/IL166585A0/xx unknown
- 2003-08-28 EP EP03790602A patent/EP1539184B1/en not_active Expired - Lifetime
-
2005
- 2005-02-11 ZA ZA200501274A patent/ZA200501274B/en unknown
- 2005-03-23 NO NO20051545A patent/NO20051545L/no not_active Application Discontinuation
-
2007
- 2007-02-14 CY CY20071100200T patent/CY1106019T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003264203A1 (en) | 2004-03-19 |
| MXPA05002294A (es) | 2005-09-12 |
| JP2005538150A (ja) | 2005-12-15 |
| NZ538342A (en) | 2007-08-31 |
| RS20050184A (sr) | 2007-11-15 |
| DE60309895D1 (de) | 2007-01-04 |
| ATE345804T1 (de) | 2006-12-15 |
| US8946198B2 (en) | 2015-02-03 |
| HRP20050291A2 (en) | 2005-10-31 |
| WO2004019954A1 (en) | 2004-03-11 |
| EP1539184B1 (en) | 2006-11-22 |
| UA82851C2 (en) | 2008-05-26 |
| PT1539184E (pt) | 2007-02-28 |
| RU2340345C2 (ru) | 2008-12-10 |
| US20060089337A1 (en) | 2006-04-27 |
| ES2277139T3 (es) | 2007-07-01 |
| NO20051545L (no) | 2005-03-23 |
| RU2005108977A (ru) | 2005-10-10 |
| IL166585A0 (en) | 2006-01-15 |
| DK1539184T3 (da) | 2007-03-19 |
| CN1678324A (zh) | 2005-10-05 |
| CY1106019T1 (el) | 2011-04-06 |
| BR0313921A (pt) | 2005-07-19 |
| EP1539184A1 (en) | 2005-06-15 |
| CA2495330A1 (en) | 2004-03-11 |
| ZA200501274B (en) | 2006-08-30 |
| KR20050059092A (ko) | 2005-06-17 |
| PL374762A1 (en) | 2005-10-31 |
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