JP2005538150A5 - - Google Patents
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- Publication number
- JP2005538150A5 JP2005538150A5 JP2004531341A JP2004531341A JP2005538150A5 JP 2005538150 A5 JP2005538150 A5 JP 2005538150A5 JP 2004531341 A JP2004531341 A JP 2004531341A JP 2004531341 A JP2004531341 A JP 2004531341A JP 2005538150 A5 JP2005538150 A5 JP 2005538150A5
- Authority
- JP
- Japan
- Prior art keywords
- activity
- estrogen
- dose
- phase
- amount
- 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.)
- Pending
Links
- 229940011871 estrogen Drugs 0.000 claims 98
- 239000000262 estrogen Substances 0.000 claims 98
- 239000000126 substance Substances 0.000 claims 70
- 230000001747 exhibiting effect Effects 0.000 claims 59
- 230000001076 estrogenic effect Effects 0.000 claims 45
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims 42
- 230000000694 effects Effects 0.000 claims 37
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 26
- 229930182833 estradiol Natural products 0.000 claims 26
- 229960005309 estradiol Drugs 0.000 claims 26
- 239000000825 pharmaceutical preparation Substances 0.000 claims 24
- 229960001207 micronized progesterone Drugs 0.000 claims 12
- 239000000583 progesterone congener Substances 0.000 claims 12
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims 9
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical group OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims 9
- 229960003387 progesterone Drugs 0.000 claims 9
- 239000000186 progesterone Substances 0.000 claims 9
- 230000009469 supplementation Effects 0.000 claims 8
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims 6
- 150000002148 esters Chemical class 0.000 claims 6
- IMSSROKUHAOUJS-MJCUULBUSA-N mestranol Chemical compound C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(OC)=CC=C3[C@H]21 IMSSROKUHAOUJS-MJCUULBUSA-N 0.000 claims 6
- JKKFKPJIXZFSSB-UHFFFAOYSA-N 1,3,5(10)-estratrien-17-one 3-sulfate Natural products OS(=O)(=O)OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 JKKFKPJIXZFSSB-UHFFFAOYSA-N 0.000 claims 5
- JKKFKPJIXZFSSB-CBZIJGRNSA-N estrone 3-sulfate Chemical compound OS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 JKKFKPJIXZFSSB-CBZIJGRNSA-N 0.000 claims 5
- 229960000417 norgestimate Drugs 0.000 claims 4
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims 3
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 3
- QMBJSIBWORFWQT-DFXBJWIESA-N Chlormadinone acetate Chemical compound C1=C(Cl)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 QMBJSIBWORFWQT-DFXBJWIESA-N 0.000 claims 3
- 241000283073 Equus caballus Species 0.000 claims 3
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims 3
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 claims 3
- ICTXHFFSOAJUMG-SLHNCBLASA-N Norethynodrel Chemical compound C1CC(=O)CC2=C1[C@H]1CC[C@](C)([C@](CC3)(O)C#C)[C@@H]3[C@@H]1CC2 ICTXHFFSOAJUMG-SLHNCBLASA-N 0.000 claims 3
- 102000001307 androgen receptors Human genes 0.000 claims 3
- 108010080146 androgen receptors Proteins 0.000 claims 3
- 229960001616 chlormadinone acetate Drugs 0.000 claims 3
- 239000000470 constituent Substances 0.000 claims 3
- 229960000978 cyproterone acetate Drugs 0.000 claims 3
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims 3
- 239000002552 dosage form Substances 0.000 claims 3
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims 3
- 229960001348 estriol Drugs 0.000 claims 3
- 229960003399 estrone Drugs 0.000 claims 3
- 150000002170 ethers Chemical class 0.000 claims 3
- 229960004400 levonorgestrel Drugs 0.000 claims 3
- 229960002985 medroxyprogesterone acetate Drugs 0.000 claims 3
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 claims 3
- 229960001390 mestranol Drugs 0.000 claims 3
- 229940053934 norethindrone Drugs 0.000 claims 3
- 229960001652 norethindrone acetate Drugs 0.000 claims 3
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 claims 3
- 229960001858 norethynodrel Drugs 0.000 claims 3
- 230000001072 progestational effect Effects 0.000 claims 3
- 102000003998 progesterone receptors Human genes 0.000 claims 3
- 108090000468 progesterone receptors Proteins 0.000 claims 3
- PWZUUYSISTUNDW-VAFBSOEGSA-N quinestrol Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@]4(O)C#C)C)CC2=CC=3OC1CCCC1 PWZUUYSISTUNDW-VAFBSOEGSA-N 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- 102000034755 Sex Hormone-Binding Globulin Human genes 0.000 claims 2
- 108010089417 Sex Hormone-Binding Globulin Proteins 0.000 claims 2
- 229960004976 desogestrel Drugs 0.000 claims 2
- RPLCPCMSCLEKRS-BPIQYHPVSA-N desogestrel Chemical group C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 RPLCPCMSCLEKRS-BPIQYHPVSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- JGMOKGBVKVMRFX-HQZYFCCVSA-N dydrogesterone Chemical compound C1=CC2=CC(=O)CC[C@@]2(C)[C@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 JGMOKGBVKVMRFX-HQZYFCCVSA-N 0.000 claims 2
- 102000006395 Globulins Human genes 0.000 claims 1
- 108010044091 Globulins Proteins 0.000 claims 1
- 229940083546 estradiol 0.5 mg Drugs 0.000 claims 1
- HZEQBCVBILBTEP-ZFINNJDLSA-N estropipate Chemical compound C1CNCCN1.OS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 HZEQBCVBILBTEP-ZFINNJDLSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- KIQQMECNKUGGKA-NMYWJIRASA-N norgestimate Chemical compound O/N=C/1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(OC(C)=O)C#C)[C@@H]4[C@@H]3CCC2=C\1 KIQQMECNKUGGKA-NMYWJIRASA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40633102P | 2002-08-28 | 2002-08-28 | |
| PCT/CA2003/001325 WO2004019954A1 (en) | 2002-08-28 | 2003-08-28 | Estrogen replacement regimen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005538150A JP2005538150A (ja) | 2005-12-15 |
| JP2005538150A5 true JP2005538150A5 (https=) | 2006-10-12 |
Family
ID=31978284
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004531341A Pending JP2005538150A (ja) | 2002-08-28 | 2003-08-28 | エストロゲン補充療法 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8946198B2 (https=) |
| EP (1) | EP1539184B1 (https=) |
| JP (1) | JP2005538150A (https=) |
| KR (1) | KR20050059092A (https=) |
| CN (1) | CN1678324A (https=) |
| AT (1) | ATE345804T1 (https=) |
| AU (1) | AU2003264203A1 (https=) |
| BR (1) | BR0313921A (https=) |
| CA (1) | CA2495330A1 (https=) |
| CY (1) | CY1106019T1 (https=) |
| DE (1) | DE60309895T2 (https=) |
| DK (1) | DK1539184T3 (https=) |
| ES (1) | ES2277139T3 (https=) |
| HR (1) | HRP20050291A2 (https=) |
| IL (1) | IL166585A0 (https=) |
| MX (1) | MXPA05002294A (https=) |
| NO (1) | NO20051545L (https=) |
| NZ (1) | NZ538342A (https=) |
| PL (1) | PL374762A1 (https=) |
| PT (1) | PT1539184E (https=) |
| RS (1) | RS20050184A (https=) |
| RU (1) | RU2340345C2 (https=) |
| UA (1) | UA82851C2 (https=) |
| WO (1) | WO2004019954A1 (https=) |
| ZA (1) | ZA200501274B (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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
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