DK2714712T3 - Fremgangsmåde til fremstilling af estetrol-mellemprodukter - Google Patents
Fremgangsmåde til fremstilling af estetrol-mellemprodukter Download PDFInfo
- Publication number
- DK2714712T3 DK2714712T3 DK12729053.4T DK12729053T DK2714712T3 DK 2714712 T3 DK2714712 T3 DK 2714712T3 DK 12729053 T DK12729053 T DK 12729053T DK 2714712 T3 DK2714712 T3 DK 2714712T3
- Authority
- DK
- Denmark
- Prior art keywords
- group
- formula
- compound
- sulfinylation
- alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
-
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
-
- 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
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (14)
1. Fremgangsmåde til fremstilling af en forbindelse med formlen (I)
(l) omfattende følgende trin a) omsætning af en forbindelse med formlen (II) med et silylerings- eller et acy-leringsmiddel til fremstilling af en forbindelse med formlen (III), hvor P1 er en beskyttelsesgruppe, som er valgt blandt R2-Si-R3R4 eller R1CO-, R1 er en gruppe, som er valgt blandt Ci_6alkyl eller C3.6cycloalkyl, idet hver gruppe eventuelt er substitueret med én eller flere substituenter, som uafhængigt er valgt blandt fluor eller C-|.4alkyl; R2, R3 og R4 hver især uafhængigt er en gruppe, som er valgt blandt Ci_6alkyl eller phenyl, idet hver gruppe eventuelt er substitueret med én eller flere substituenter, som uafhængigt er valgt blandt fluor eller Ci_4alkyl;
(II) (III) b) halogenering eller sulfinylering af forbindelsen med formlen (III) til fremstilling af en forbindelse med formlen (IV); hvor X is halogen eller -SO-R5, og R5 er en gruppe, som er valgt blandt C6-ioaryl eller heteroaryl, idet hver gruppe eventuelt er substitueret med én eller flere substituenter, som uafhængigt er valgt blandt chlor eller Ci_4alkyl;
(iv) c) dehalogenering eller desulfinylering af forbindelsen med formlen (IV) til fremstilling af en forbindelse med formlen (V); og
(V) d) omsætning af forbindelsen med formlen (V) med et reduktionsmiddel til fremstilling af en forbindelse med formlen (I), og hvor C6-io aryl også skal omfatte partielt hydrogenerede derivater.
2. Fremgangsmåde ifølge krav 1, hvor trin (b) er en sulfinylering, og sulfinyleringen udføres ved omsætning af forbindelsen med formlen (III) med en base og med et sulfi-nyleringsreagens.
3. Fremgangsmåde ifølge krav 1 eller 2, hvor trin (b) er en sulfinylering, og sulfinyle-ringsreagenset er methyl 2-pyridinsulfinat, methylbenzensulfinat, methyl 4-methyl-benzensulfinat, methyl 4-chlor-benzensulfinat.
4. Fremgangsmåde ifølge krav 2 eller 3, hvor den base, der anvendes i sulfinyle-ringstrinnet, er valgt fra gruppen omfattende kaliumhydrid, kalium-terbutylat, natrium-hydrid, natrium-terbutylat og en blanding deraf.
5. Fremgangsmåde ifølge krav 1, hvor trin (b) er en halogenering, og halogeneringen udføres ved omsætning af forbindelsen med formlen (III) med et halogeneringsrea-gens.
6. Fremgangsmåde ifølge krav 1 eller 5, hvor trin (b) er en brominering, og bromineringsreagenset er valgt fra gruppen omfattende kobber(ll)bromid, brom og pyridinbrom-perbrom.
7. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 4, hvor desulfinylerings-trinnet udføres med varme, eventuelt i nærværelse af cuprisulfat.
8. Fremgangsmåde ifølge et hvilket som helst af kravene 1,5-6, hvor dehalogenerings-trinnet udføres i nærværelse af en base.
9. Fremgangsmåde ifølge krav 8, hvor basen er valgt fra gruppen omfattende imidazol, collidin, 2,6-lutidin, triethylamin eller 1,8-diazabicyclo[5.4.0]undec-7-en.
10. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 9, hvor trin (c) udføres under anvendelse af et reduktionsmiddel, som er valgt fra gruppen af metal hydridfor-bindelser.
11. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 10, hvor trin (c) udføres under anvendelse af et reduktionsmiddel, som er valgt fra gruppen omfattende NaBH4/CeCI3, LiAIH4, NaBH4, NaBH(OAc)3 og ZnBH4.
12. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 11, hvor silyleringsmid-let er valgt fra gruppen omfattende Ci.6alkylsilylchlorid, Ci.6alkylsilyltriflat, phenylsilyl-chlorid, phenylsilyltriflat, Ci.6alkylphenylsilylchlorid, Ci-6alkylphenylsilyltriflat, idet hver gruppe eventuelt er substitueret med én eller flere substituenter, som uafhængigt er valgt blandt fluor eller C-|.4alkyl.
13. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 11, hvor acyleringsmid-let er valgt fra gruppen omfattende C2-6alkenylCi.6alkanoater, C2-6alkenylC3-6cycloalka-noat, acylchlorider og anhydrider.
14. Fremgangsmåde til fremstilling af estetrol, hvilken fremgangsmåde omfatter fremstilling af en forbindelse med formlen (I) ved en fremgangsmåde ifølge et hvilket som helst af kravene 1 til 13 og yderligere omsætning af forbindelsen med formlen (I) til fremstilling af estetrol.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161492297P | 2011-06-01 | 2011-06-01 | |
| EP11168560 | 2011-06-01 | ||
| PCT/EP2012/060446 WO2012164095A1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2714712T3 true DK2714712T3 (da) | 2016-12-05 |
Family
ID=44588329
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12729053.4T DK2714712T3 (da) | 2011-06-01 | 2012-06-01 | Fremgangsmåde til fremstilling af estetrol-mellemprodukter |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US11053273B2 (da) |
| EP (1) | EP2714712B1 (da) |
| JP (1) | JP6116550B2 (da) |
| KR (1) | KR101957937B1 (da) |
| CN (1) | CN103619867B (da) |
| AU (1) | AU2012264601C1 (da) |
| BR (1) | BR112013030833B1 (da) |
| CA (1) | CA2835979C (da) |
| CY (1) | CY1118164T1 (da) |
| DK (1) | DK2714712T3 (da) |
| EA (1) | EA025511B1 (da) |
| ES (1) | ES2600703T3 (da) |
| HR (1) | HRP20161369T1 (da) |
| HU (1) | HUE031809T2 (da) |
| LT (1) | LT2714712T (da) |
| ME (1) | ME02585B (da) |
| MX (1) | MX342537B (da) |
| PL (1) | PL2714712T3 (da) |
| PT (1) | PT2714712T (da) |
| RS (1) | RS55293B1 (da) |
| SG (1) | SG195121A1 (da) |
| SI (1) | SI2714712T1 (da) |
| SM (1) | SMT201600408B (da) |
| WO (1) | WO2012164095A1 (da) |
| ZA (1) | ZA201308445B (da) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2714710B1 (en) | 2011-06-01 | 2016-04-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| ES2600703T3 (es) | 2011-06-01 | 2017-02-10 | Estetra S.P.R.L. | Proceso para la producción de intermediarios de estetrol |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| DK2764008T3 (da) | 2011-10-07 | 2016-11-07 | Estetra Sprl | Fremgangsmåde til fremstilling af estetrol |
| TN2017000499A1 (en) | 2015-06-18 | 2019-04-12 | Mithra Pharmaceuticals S A | Orodispersible dosage unit containing an estetrol component |
| GEP20217243B (en) | 2015-06-18 | 2021-04-26 | Sprl Estetra | Orodispersible dosage unit containing an estetrol component |
| ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
| LT3310346T (lt) | 2015-06-18 | 2021-06-10 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| KR20220144885A (ko) | 2016-08-05 | 2022-10-27 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
| JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
| 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 |
| WO2023021026A1 (en) | 2021-08-17 | 2023-02-23 | Aspen Oss B.V. | A synthetic pathway to estra-1,3,5(10)-triene-3,15a,16a,17b-tetrol |
Family Cites Families (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE144266C (da) | ||||
| US3138588A (en) | 1962-08-24 | 1964-06-23 | American Home Prod | 17-ketals of estrone and derivatives thereof |
| US3177206A (en) | 1963-03-07 | 1965-04-06 | American Home Prod | Selective bromination of a-ring aromatic 17-ketalized steroids |
| US3433785A (en) | 1966-07-11 | 1969-03-18 | Sterling Drug Inc | 15,16-disubstituted aromatic steroids,intermediates and processes |
| US3673180A (en) | 1970-06-18 | 1972-06-27 | Merck & Co Inc | 19-nor-6,6-ethylene-20-spiroxenes |
| US4792620A (en) | 1983-10-14 | 1988-12-20 | Bp Chemicals Limited | Carbonylation catalysts |
| US4739078A (en) | 1984-02-17 | 1988-04-19 | The Upjohn Company | Use of borohydride-salt lanthanide salt reagents for stereo selective reduction of C-15-keto prostaglandin precursors |
| IE60780B1 (en) * | 1987-01-23 | 1994-08-10 | Akzo Nv | New 11-aryl steroid derivatives |
| DE3710728A1 (de) | 1987-03-31 | 1988-10-13 | Schering Ag | Verfahren zur herstellung von 17(alpha)-ethinyl-17ss-hydroxy-18-methyl-4,15-estradien-3-on und die neuen zwischenprodukte fuer dieses verfahren |
| US5073374A (en) | 1988-11-30 | 1991-12-17 | Schering Corporation | Fast dissolving buccal tablet |
| US5340586A (en) | 1991-04-12 | 1994-08-23 | University Of Southern California | Methods and formulations for use in treating oophorectomized women |
| JPH07101977A (ja) | 1993-10-05 | 1995-04-18 | Kureha Chem Ind Co Ltd | ホルモン作用を軽減した新規なエストラジオール誘導体及びその増殖因子阻害剤 |
| WO1997004752A1 (en) | 1995-07-26 | 1997-02-13 | Duramed Pharmaceuticals, Inc. | Pharmaceutical compositions of conjugated estrogens and methods for their use |
| US6117446A (en) | 1999-01-26 | 2000-09-12 | Place; Virgil A. | Drug dosage unit for buccal administration of steroidal active agents |
| TW548277B (en) * | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| US20020132801A1 (en) | 2001-01-11 | 2002-09-19 | Schering Aktiengesellschaft | Drospirenone for hormone replacement therapy |
| DK1390040T3 (da) | 2001-05-18 | 2007-04-23 | Pantarhei Bioscience Bv | Farmaceutisk præparat til anvendelse i hormonerstatningsterapi |
| EP1260225A1 (en) | 2001-05-18 | 2002-11-27 | Pantarhei Bioscience B.V. | A pharmaceutical composition for use in hormone replacement therapy |
| EP1390041B1 (en) | 2001-05-23 | 2009-11-25 | Pantarhei Bioscience B.V. | Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception |
| US7732430B2 (en) | 2001-05-23 | 2010-06-08 | Pantarhei Bioscience B.V. | Drug delivery system comprising a tetrahydroxilated estrogen for use in hormonal contraception |
| WO2003018026A1 (en) | 2001-08-31 | 2003-03-06 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| EP1446128B1 (en) | 2001-11-15 | 2006-12-06 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| US6723348B2 (en) | 2001-11-16 | 2004-04-20 | Ethypharm | Orodispersible tablets containing fexofenadine |
| HU227198B1 (en) | 2001-11-27 | 2010-10-28 | Richter Gedeon Nyrt | Pharmaceutical composition for emergency contraception containing levonorgestrel |
| MXPA04008185A (es) | 2002-02-21 | 2004-11-26 | Schering Ag | Composiciones farmaceuticas que comprenden uno o mas esteroides, uno o mas componentes de tetrahidrofolato y vitamina b12. |
| US20050147670A1 (en) | 2002-05-29 | 2005-07-07 | Impax Laboratories Inc. | Oral disintegrating dosage forms |
| WO2003103685A1 (en) | 2002-06-11 | 2003-12-18 | Pantarhei Bioscience B.V. | A method of treating human skin and a skin care composition for use in such a method |
| ATE340579T1 (de) | 2002-06-11 | 2006-10-15 | Pantarhei Bioscience Bv | Methode zur behandlung oder prävention immunologischer erkrankungen und pharmazeutische zusammensetzung zur solchen anwendung |
| AU2003253506A1 (en) | 2002-07-12 | 2004-02-02 | Pantarhei Biosciences B.V. | Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy |
| CN100528167C (zh) | 2002-10-23 | 2009-08-19 | 潘塔希生物科学股份有限公司 | 用于治疗癌症的包含雌四醇衍生物的药物组合物 |
| WO2004041839A2 (en) | 2002-11-08 | 2004-05-21 | Pantarhei Bioscience B.V. | Synthesis of estetrol via estrone derived steroids |
| US20060276414A1 (en) | 2003-05-22 | 2006-12-07 | Coelingh Bennink Herman Jan Ti | Use of compositions comprising an estrogenic component for the treatment and prevention of musculoskeletal pain |
| CA2609726C (en) | 2005-05-26 | 2013-10-01 | Solvay Pharmaceuticals Gmbh | 17.beta.-hsd1 and sts inhibitors |
| DE502006007749D1 (de) | 2005-07-25 | 2010-10-07 | Riboxx Gmbh | Verfahren und Kit zur Amplifikation von heteropolymerer oder poly(C)- RNA |
| US20070048369A1 (en) | 2005-08-26 | 2007-03-01 | National Starch And Chemical Investment Holding Corporation | Mucosal delivery tablet |
| WO2007081206A1 (en) | 2006-01-09 | 2007-07-19 | Pantarhei Bioscience B.V. | A method of treating an acute vascular disorder |
| SG174785A1 (en) | 2006-06-08 | 2011-10-28 | Warner Chilcott Co Llc | Methods to administer solid dosage forms of ethinyl estradiol and prodrugs thereof with improved bioavailabilty |
| US20070286819A1 (en) | 2006-06-08 | 2007-12-13 | Warner Chilcott Company, Inc. | Methods to administer ethinyl estradiol and prodrugs thereof with improved bioavailability |
| US20080113953A1 (en) | 2006-06-08 | 2008-05-15 | Warner Chilcott Company, Inc. | Methods to administer solid dosage forms of ethinyl estradiol and prodrugs thereof with improved bioavailability |
| GB0621926D0 (en) | 2006-11-03 | 2006-12-13 | Medlock Medical Ltd | Multi directional stretch tubular bandages |
| CL2007003429A1 (es) | 2006-11-29 | 2008-04-11 | Wyeth Corp | Tableta bi-capa que comprende una primera capa con al menos un estrogeno y una segunda capa con uno o mas agentes terapeuticos seleccionados entre un modulador selectivo del receptor de estrogeno y un agente progestacional; proceso de produccion, uti |
| MX2009006823A (es) | 2006-12-20 | 2009-07-03 | Duramed Pharmaceuticals Inc | Formas de dosificacion solidas de desintegracion oral que comprenden progestina y metodos para hacer y usar las mismas. |
| CN101583363B (zh) | 2007-01-08 | 2013-08-21 | 潘塔希生物科学股份有限公司 | 治疗或预防雌性哺乳动物不育症的方法和此类方法中使用的药物试剂盒 |
| AR064875A1 (es) | 2007-01-12 | 2009-04-29 | Wyeth Corp | Composiciones de tableta en tableta |
| EP2155205B1 (en) | 2007-06-21 | 2011-12-21 | Pantarhei Bioscience B.V. | Treatment of meconium aspiration syndrome with estrogens |
| ATE533492T1 (de) | 2007-07-19 | 2011-12-15 | Pantarhei Bioscience Bv | Behandlung oder prävention von hypertensiven erkrankungen in der schwangerschaft oder von wachstumsverzögerung des foeten |
| CN101541725B (zh) | 2007-08-31 | 2013-08-28 | 国立大学法人名古屋大学 | 羰基化合物的制造方法和用于制造羰基化合物的氧化促进剂 |
| EP2077272A1 (en) | 2007-12-21 | 2009-07-08 | Affibody AB | Polypeptide libraries with a predetermined scaffold |
| EP2077273B1 (en) | 2007-12-31 | 2011-09-14 | Animal Technology Institute Taiwan | Methods for separating casein from soluble proteins in a composition |
| CN101318983A (zh) * | 2008-04-21 | 2008-12-10 | 上海大学 | 螺[(5β,6β,15β,16β-二亚甲基-雄甾-14β-氢-5,7-二烯-3-酮)-17α-2′-(1′-氧-环戊烷-5′-酮)]及其合成方法 |
| US20110250274A1 (en) | 2008-09-19 | 2011-10-13 | Shaked Ze Ev | Estriol formulations |
| DE102009007771B4 (de) | 2009-02-05 | 2012-02-16 | Bayer Schering Pharma Aktiengesellschaft | Bukkales Applikationssystem, 17α-Estradiol enthaltend |
| CN101560237A (zh) * | 2009-05-26 | 2009-10-21 | 上海大学 | 14β-氢-6β,7β,15β,16β-二亚甲基-3-氧代-17β-孕甾-4-烯-21,17-羧内酯及其合成方法 |
| CN102058604A (zh) | 2009-11-17 | 2011-05-18 | 北京万全阳光医学技术有限公司 | 一种含有地诺孕素和戊酸雌二醇的药物组合物及其制备方法 |
| US9603860B2 (en) | 2010-07-28 | 2017-03-28 | Laboratorios Leon Farma Sa | Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same |
| ES2600703T3 (es) | 2011-06-01 | 2017-02-10 | Estetra S.P.R.L. | Proceso para la producción de intermediarios de estetrol |
| EP2714710B1 (en) | 2011-06-01 | 2016-04-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| KR102033187B1 (ko) | 2011-07-19 | 2019-10-16 | 판타레이 바이오사이언스 비.브이. | 디하이드로에피안드로스테론(ｄｈｅａ)을 함유하는 정제 |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| US9579329B2 (en) | 2011-08-11 | 2017-02-28 | Estetra S.P.R.L. | Use of estetrol as emergency contraceptive |
| US9731018B2 (en) | 2011-09-16 | 2017-08-15 | Ferring B.V. | Fast dissolving pharmaceutical composition |
| DK2764008T3 (da) | 2011-10-07 | 2016-11-07 | Estetra Sprl | Fremgangsmåde til fremstilling af estetrol |
| EP2653163A1 (en) | 2012-04-19 | 2013-10-23 | Université de Liège | Estrogenic components for use in the treatment of neurological disorders |
| US9808470B2 (en) | 2012-04-19 | 2017-11-07 | Universite De Liege | Estrogenic components for use in the treatment of neurological disorders |
| WO2014159377A1 (en) | 2013-03-14 | 2014-10-02 | Teva Women's Health, Inc. | Compositions containing tanaproget and natural estrogens |
| CA2924255C (en) | 2013-09-18 | 2022-11-22 | Crystal Pharma, S.A.U. | Process for the preparation of estetrol |
| CA2932855C (en) | 2013-12-12 | 2022-07-19 | Donesta Bioscience B.V. | Orally disintegrating solid dosage unit containing an estetrol component |
| ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
| GEP20217243B (en) | 2015-06-18 | 2021-04-26 | Sprl Estetra | Orodispersible dosage unit containing an estetrol component |
| TN2017000499A1 (en) | 2015-06-18 | 2019-04-12 | Mithra Pharmaceuticals S A | Orodispersible dosage unit containing an estetrol component |
| LT3310346T (lt) | 2015-06-18 | 2021-06-10 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
-
2012
- 2012-06-01 ES ES12729053.4T patent/ES2600703T3/es active Active
- 2012-06-01 CN CN201280026131.6A patent/CN103619867B/zh active Active
- 2012-06-01 LT LTEP12729053.4T patent/LT2714712T/lt unknown
- 2012-06-01 RS RS20160946A patent/RS55293B1/sr unknown
- 2012-06-01 MX MX2013014044A patent/MX342537B/es active IP Right Grant
- 2012-06-01 DK DK12729053.4T patent/DK2714712T3/da active
- 2012-06-01 AU AU2012264601A patent/AU2012264601C1/en active Active
- 2012-06-01 KR KR1020137031484A patent/KR101957937B1/ko active IP Right Grant
- 2012-06-01 ME MEP-2016-253A patent/ME02585B/me unknown
- 2012-06-01 PL PL12729053T patent/PL2714712T3/pl unknown
- 2012-06-01 EP EP12729053.4A patent/EP2714712B1/en active Active
- 2012-06-01 EA EA201301315A patent/EA025511B1/ru unknown
- 2012-06-01 PT PT127290534T patent/PT2714712T/pt unknown
- 2012-06-01 JP JP2014513213A patent/JP6116550B2/ja active Active
- 2012-06-01 CA CA2835979A patent/CA2835979C/en active Active
- 2012-06-01 HU HUE12729053A patent/HUE031809T2/en unknown
- 2012-06-01 WO PCT/EP2012/060446 patent/WO2012164095A1/en active Application Filing
- 2012-06-01 SI SI201230746A patent/SI2714712T1/sl unknown
- 2012-06-01 US US14/122,892 patent/US11053273B2/en active Active
- 2012-06-01 SG SG2013086715A patent/SG195121A1/en unknown
- 2012-06-01 BR BR112013030833A patent/BR112013030833B1/pt active IP Right Grant
-
2013
- 2013-11-11 ZA ZA2013/08445A patent/ZA201308445B/en unknown
-
2016
- 2016-10-20 HR HRP20161369TT patent/HRP20161369T1/hr unknown
- 2016-10-26 CY CY20161101090T patent/CY1118164T1/el unknown
- 2016-11-10 SM SM201600408T patent/SMT201600408B/it unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK2714712T3 (da) | Fremgangsmåde til fremstilling af estetrol-mellemprodukter | |
| DK2764008T3 (da) | Fremgangsmåde til fremstilling af estetrol | |
| DK2714710T3 (da) | Fremgangsmåde til fremstilling af estetrol-mellemprodukter | |
| AU2012264602A1 (en) | Process for the production of estetrol intermediates | |
| EP2607371A1 (en) | Processes for the preparation of abiraterone and related compouds | |
| NZ617591B2 (en) | Process for the production of estetrol intermediates | |
| NZ621973B2 (en) | Process for the production of estetrol |