PE20000261A1 - Preparacion combinada de estrogeno y antiestrogeno y su empleo - Google Patents
Preparacion combinada de estrogeno y antiestrogeno y su empleoInfo
- Publication number
- PE20000261A1 PE20000261A1 PE1999000143A PE00014399A PE20000261A1 PE 20000261 A1 PE20000261 A1 PE 20000261A1 PE 1999000143 A PE1999000143 A PE 1999000143A PE 00014399 A PE00014399 A PE 00014399A PE 20000261 A1 PE20000261 A1 PE 20000261A1
- Authority
- PE
- Peru
- Prior art keywords
- estrogen
- methylene
- halogen
- hydrocarbon
- antiestrogen
- Prior art date
Links
- 229940011871 estrogen Drugs 0.000 title abstract 3
- 239000000262 estrogen Substances 0.000 title abstract 3
- 229940046836 anti-estrogen Drugs 0.000 title abstract 2
- 230000001833 anti-estrogenic effect Effects 0.000 title abstract 2
- 239000000328 estrogen antagonist Substances 0.000 title abstract 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 11
- 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 abstract 4
- 239000004215 Carbon black (E152) Substances 0.000 abstract 3
- 229930195733 hydrocarbon Natural products 0.000 abstract 3
- 150000002430 hydrocarbons Chemical class 0.000 abstract 3
- -1 17-O-ETHYNYLESTRADIOL Chemical compound 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 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 abstract 1
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 abstract 1
- OTMSDBZUPAUEDD-UHFFFAOYSA-N Ethane Chemical compound CC OTMSDBZUPAUEDD-UHFFFAOYSA-N 0.000 abstract 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 229940035811 conjugated estrogen Drugs 0.000 abstract 1
- 229960004766 estradiol valerate Drugs 0.000 abstract 1
- 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 abstract 1
- 229960001348 estriol Drugs 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229940088597 hormone Drugs 0.000 abstract 1
- 239000005556 hormone Substances 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 abstract 1
- 229910021653 sulphate ion Inorganic materials 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/567—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 substituted in position 17 alpha, e.g. mestranol, norethandrolone
-
- 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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
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)
- Endocrinology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A UNA COMPOSICION QUE COMPRENDE a)ESTROGENO TAL COMO 17-ß-ESTRADIOL, 17-O-ETINILESTRADIOL, ESTRIOL, ESTRIONA, SULFATO DE ESTRIONA, SULFAMATO DE ESTROGENO, 17-O-ESTRADIOL, MESTRANOL, ESTILBESTROL, ESTROGENOESTERES DE 17-ß-ESTRADIOL (VALERATO DE ESTRADIOL, ESTROGENOS CONJUGADOS NATURALES); b)ANTIESTROGENO TAL COMO 7O-( -AMINOALQUIL)-ESTRATRIENO DE FORMULA I; 11ß-HALOGENO-7O-ESTRATRIENO, SK ES -(CH2)m-N(-A)-C(H)(-B)-C(H)(-D)-(CH2)n-SOx-(CH2)3-E; m ES 4-6; n ES 0-2; x ES 0-2; A ES H, ALQUILO C1-C5; B Y D SON H; A Y B SON ALQUILENO -(CH2)p-, p ES 2-5; D ES H; A Y D SON ALQUILENO -(CH2)q-; q ES 2-4; B ES H; E ES ETILO, -(CH2)3-E; R3 ES H, HIDROCARBURO C1-C8, R3`-C(O)-; R3' ES H, HIDROCARBURO C1-C8, FENILO; R11 ES H, HALOGENO, -O-NO2-; R14, R15O, R15ß, R16O, R16ß SON H; R14 Y R15O SON UN ENLACE, METILENO; R15ß ES METILENO; R15O ES H; R15ß Y R16ß JUNTOS SON METILENO; R16O o R16ß ES HALOGENO, R16O Y R16ß SON METILIDENO; R17' ES H, ALQUILO C1-C5; ALQUENILO C2-C5, ENTRE OTROS; R17'' ES H, R17'''-CO-; R17''' ES H, HIDROCARBURO C1-C8; R17' ESTA EN O; R17' Y R14 SON ETANO; CUANDO A Y B NO SON (CH2)p; A Y D NO SON (CH2)q UNO DE R14, R15O o ß, R16O o ß NO SON H. LA RELACION DE LOS COMPONENTES a/b ES DE 1:5 A 1:500. LA COMPOSICION PUEDE SER EMPLEADA EN TERAPIA DE SUSTITUCION DE HORMONAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19807791A DE19807791A1 (de) | 1998-02-19 | 1998-02-19 | Kombinationspräparat aus Östrogen und Antiöstrogen |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20000261A1 true PE20000261A1 (es) | 2000-05-22 |
Family
ID=7858786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1999000143A PE20000261A1 (es) | 1998-02-19 | 1999-02-17 | Preparacion combinada de estrogeno y antiestrogeno y su empleo |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6677324B1 (es) |
| EP (1) | EP1054676A1 (es) |
| JP (1) | JP2002503695A (es) |
| AR (1) | AR017982A1 (es) |
| AU (1) | AU2834799A (es) |
| BR (1) | BR9908094A (es) |
| CA (1) | CA2321427A1 (es) |
| DE (1) | DE19807791A1 (es) |
| IL (1) | IL137491A0 (es) |
| PE (1) | PE20000261A1 (es) |
| WO (1) | WO1999042109A1 (es) |
| ZA (1) | ZA991370B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6653298B2 (en) | 2000-01-14 | 2003-11-25 | Sterix Limited | Composition |
| US7335650B2 (en) | 2000-01-14 | 2008-02-26 | Sterix Limited | Composition |
| DE10039199A1 (de) * | 2000-08-10 | 2002-02-21 | Schering Ag | Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen |
| DE10159217A1 (de) | 2001-11-27 | 2003-06-05 | Schering Ag | 17alpha-Alkyl-17ß-oxy-estratriene und Zwischenprodukte zu deren Herstellung, Verwendung der 17alpha-Alkyl-17ß-oxy-estratriene zur Herstellung von Arzneimitteln sowie pharmazeutische Präparate |
| US20040242551A1 (en) * | 2003-05-28 | 2004-12-02 | Schering Ag | Composition comprising antiprogestins and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases |
| EP1749017A2 (en) * | 2004-05-27 | 2007-02-07 | MIGENIX Corp. | Compounds and methods for cytoprotection |
| US7790910B2 (en) | 2004-07-27 | 2010-09-07 | Sicor Inc. | Process for the preparation of 7α-alkylated 19-norsteroids |
| CN101014610B (zh) * | 2004-09-08 | 2012-08-22 | Msd欧斯股份有限公司 | 具有选择性雌激素活性的15β-取代的类固醇 |
| AU2006317486B9 (en) | 2005-11-22 | 2011-08-04 | Sumitomo Chemical Company, Limited | Organic sulfur compounds and use thereof as arthropodicides |
| JP2009001551A (ja) | 2007-05-18 | 2009-01-08 | Sumitomo Chemical Co Ltd | 有機硫黄化合物及びその有害節足動物防除用途 |
| TW200904329A (en) | 2007-05-18 | 2009-02-01 | Sumitomo Chemical Co | Organic sulfur compound and its use for controlling harmful arthropod |
| JP5298631B2 (ja) | 2007-05-18 | 2013-09-25 | 住友化学株式会社 | 有機硫黄化合物及びその有害節足動物防除用途 |
| US8153846B2 (en) * | 2007-12-03 | 2012-04-10 | E.I. Du Pont De Nemours And Company | Sulfur containing fluoroalkyl amines and isocyanates |
| EP2070941A1 (en) | 2007-12-14 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Stereoselective synthesis of selective estrogen receptor down-regulators |
| ES2885523T3 (es) | 2011-11-23 | 2021-12-14 | Therapeuticsmd Inc | Formulaciones y terapias de reposición hormonal de combinación naturales |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| 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 |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | 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 |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | 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 |
| AR100562A1 (es) | 2014-05-22 | 2016-10-12 | Therapeuticsmd Inc | Composición farmacéutica de estradiol y progesterona para terapia de reemplazo hormonal |
| CN104387435B (zh) * | 2014-12-10 | 2017-05-10 | 天津孚音生物科技发展有限公司 | 一种化合物及其制备方法与应用 |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| CA3020153A1 (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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8327256D0 (en) * | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| GB8813353D0 (en) * | 1988-06-06 | 1988-07-13 | Ici Plc | Therapeutic product |
| DE3925507A1 (de) * | 1989-07-28 | 1991-01-31 | Schering Ag | 14,17(alpha)-etheno- und ethanoestratriene, verfahren zur herstellung dieser verbindungen, sowie ihre verwendung zur herstellung von arzneimitteln |
| DE19622457A1 (de) * | 1996-05-24 | 1997-11-27 | Schering Ag | 7alpha-(5-Methylaminopentyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha-(5-Methylaminopentyl)-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| US5866560A (en) * | 1996-08-20 | 1999-02-02 | Schering Ag | 7α-(ξ-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7α-(ξ-aminoalkyl)-estratrienes as well as their use for the production of pharmaceutical agents |
| DE19635525A1 (de) | 1996-08-20 | 1998-02-26 | Schering Ag | 7alpha-(xi-Aminoalkyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha(xi-Aminoalkyl-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
-
1998
- 1998-02-19 DE DE19807791A patent/DE19807791A1/de not_active Ceased
-
1999
- 1999-02-17 PE PE1999000143A patent/PE20000261A1/es not_active Application Discontinuation
- 1999-02-18 US US09/622,532 patent/US6677324B1/en not_active Expired - Fee Related
- 1999-02-18 CA CA002321427A patent/CA2321427A1/en not_active Abandoned
- 1999-02-18 IL IL13749199A patent/IL137491A0/xx unknown
- 1999-02-18 AU AU28347/99A patent/AU2834799A/en not_active Abandoned
- 1999-02-18 WO PCT/EP1999/001023 patent/WO1999042109A1/de not_active Ceased
- 1999-02-18 EP EP99908916A patent/EP1054676A1/de not_active Withdrawn
- 1999-02-18 BR BR9908094-0A patent/BR9908094A/pt not_active IP Right Cessation
- 1999-02-18 JP JP2000532124A patent/JP2002503695A/ja not_active Withdrawn
- 1999-02-19 ZA ZA9901370A patent/ZA991370B/xx unknown
- 1999-02-23 AR ARP990100693A patent/AR017982A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999042109A1 (de) | 1999-08-26 |
| AR017982A1 (es) | 2001-10-24 |
| IL137491A0 (en) | 2001-07-24 |
| CA2321427A1 (en) | 1999-08-26 |
| AU2834799A (en) | 1999-09-06 |
| JP2002503695A (ja) | 2002-02-05 |
| BR9908094A (pt) | 2000-10-31 |
| ZA991370B (en) | 1999-11-24 |
| DE19807791A1 (de) | 1999-08-26 |
| EP1054676A1 (de) | 2000-11-29 |
| US6677324B1 (en) | 2004-01-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |