HRP20170797T1 - Primjena estetrola kao hitnog kontraceptiva - Google Patents
Primjena estetrola kao hitnog kontraceptiva Download PDFInfo
- Publication number
- HRP20170797T1 HRP20170797T1 HRP20170797TT HRP20170797T HRP20170797T1 HR P20170797 T1 HRP20170797 T1 HR P20170797T1 HR P20170797T T HRP20170797T T HR P20170797TT HR P20170797 T HRP20170797 T HR P20170797T HR P20170797 T1 HRP20170797 T1 HR P20170797T1
- Authority
- HR
- Croatia
- Prior art keywords
- hours
- tetra
- carried out
- application
- hydroxyl group
- Prior art date
Links
- 239000003433 contraceptive agent Substances 0.000 title claims 7
- 230000002254 contraceptive effect Effects 0.000 title claims 7
- AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title claims 3
- 229950009589 estetrol Drugs 0.000 title claims 3
- 229940011871 estrogen Drugs 0.000 claims 7
- 239000000262 estrogen Substances 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- 230000035935 pregnancy Effects 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 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
- A61K31/565—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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Orthopedics, Nursing, And Contraception (AREA)
Claims (12)
1. Postupak hitne kontracepcije kod žena sisavaca obuhvaća primjenu hitnog kontraceptiva koji sadrži tetra-hidroksilirani estrogen predstavljen općom formulom (I):
[image]
gdje svaki od R1, R2, R3, R4 neovisno predstavlja atom vodika, hidroksilnu skupinu, alkoksi skupinu sa 1-5 atoma ugljika, ili keto skupinu;
poželjno gdje svaki od R1, R2, R3, R4 neovisno predstavlja atom vodika, hidroksilnu skupinu ili alkoksi skupinu sa 1-5 atoma ugljika;
gdje svaki od R5, R6, R7 predstavlja hidroksilnu skupinu; i
gdje najviše 3 od R1, R2, R3, R4 predstavljaju atome vodika,
u količini koja je dovoljna za sprječavanje trudnoće kod ženskih sisavaca, pri čemu se navedena primjena provodi nevaginalnim putem.
2. Postupak prema bilo kojem u zahtjevu 1, pri čemu se navedena primjena provodi oralnim, parenteralnim, rektalnim, transkutnim ili lokalnim putem.
3. Postupak prema bilo kojem od zahtjeva 1 ili 2, pri čemu navedeni hitni kontraceptiv dodatno sadrži farmaceutski prihvatljive soli ili ekscipijense.
4. Postupak prema bilo kojem od zahtjeva 1 do 3 pri čemu navedeni hitni kontraceptiv dodatno sadrži dodatni aktivni sastojak prikladan za sprečavanje trudnoće.
5. Postupak prema bilo kojem od zahtjeva 1 do 4, pri čemu navedeni tetra-hidroksilirani estrogen je estetrol (1,3,5 (10)-estratrien-3, 15α, 16α, 17β-tetrol).
6. Postupak prema bilo kojem od zahtjeva 1 do 5, pri čemu navedeni hitni kontraceptiv sadrži tetra-hidroksilirani estrogen u dozi između 0,5 i 7 mg/kg, između 1,0 do 5,0 mg/kg, između 1,5 do 2,5 mg/kg, ili oko 2,0 mg/kg.
7. Postupak prema bilo kojem od zahtjeva 1 do 5, pri čemu navedeni hitni kontraceptiv sadrži tetra-hidroksilirani estrogen u dozi između 30 mg i 400 mg, između 40 mg i 250 mg, između 40 mg i 200 mg, između 40 mg i 150 mg, između 40 mg i 100 mg, između 50 mg i 100 mg, ili oko 100 mg estetrola.
8. Postupak prema bilo kojem od zahtjeva 1 do 7, pri čemu se primjena provodi jednom dozom.
9. Postupak prema zahtjevu 1 do 7, pri čemu se primjena provodi dvostrukom dozom, npr. u intervalu od 6, 12, 18 ili 24 sata.
10. Postupak prema bilo kojem od zahtjeva 1 do 9, pri čemu se navedena primjena provodi unutar 120 sati nakon spolnog odnosa, po mogućnosti unutar 96 sati, unutar 72 sata, unutar 48 sati, unutar 24 sata, unutar 12 sati ili manje.
11. Primjena tetra-hidroksiliranog estrogena predstavljenog općom formulom (I):
[image]
gdje svaki od R1, R2, R3, R4 neovisno predstavlja atom vodika, hidroksilnu skupinu, alkoksi skupinu sa 1-5 atoma ugljika, ili keto skupinu;
poželjno gdje svaki od R1, R2, R3, R4 neovisno predstavlja atom vodika, hidroksilnu skupinu ili alkoksi skupinu sa 1-5 atoma ugljika;
gdje svaki od R5, R6, R7 predstavlja hidroksilnu skupinu; i
gdje najviše 3 od R1, R2, R3, R4 predstavljaju atome vodika,
kao hitni kontraceptiv,
pri čemu se navedena primjena spomenutog tetra-hidroksiliranog estrogena provodi nevaginalnim putem.
12. Primjena prema zahtjevu 11, pri čemu se navedena primjena spomenutog tetra-hidroksiliranog estrogena provodi oralnim, parenteralnim, rektalnim, transkutnim ili lokalnim putem.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161522480P | 2011-08-11 | 2011-08-11 | |
| EP11177266 | 2011-08-11 | ||
| PCT/EP2012/065572 WO2013021025A1 (en) | 2011-08-11 | 2012-08-09 | Use of estetrol as emergency contraceptive |
| EP12753086.3A EP2741824B1 (en) | 2011-08-11 | 2012-08-09 | Use of estetrol as emergency contraceptive |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170797T1 true HRP20170797T1 (hr) | 2017-08-11 |
Family
ID=47667911
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170797TT HRP20170797T1 (hr) | 2011-08-11 | 2017-05-26 | Primjena estetrola kao hitnog kontraceptiva |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US9579329B2 (hr) |
| EP (1) | EP2741824B1 (hr) |
| AU (2) | AU2012293593B2 (hr) |
| BR (1) | BR112014003113A2 (hr) |
| CA (1) | CA2843951C (hr) |
| CY (1) | CY1118996T1 (hr) |
| DK (1) | DK2741824T3 (hr) |
| EA (1) | EA028780B1 (hr) |
| ES (1) | ES2631359T3 (hr) |
| HK (1) | HK1197027A1 (hr) |
| HR (1) | HRP20170797T1 (hr) |
| HU (1) | HUE033590T2 (hr) |
| LT (1) | LT2741824T (hr) |
| ME (1) | ME02723B (hr) |
| PL (1) | PL2741824T3 (hr) |
| PT (1) | PT2741824T (hr) |
| RS (1) | RS55974B1 (hr) |
| SI (1) | SI2741824T1 (hr) |
| WO (1) | WO2013021025A1 (hr) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11053274B2 (en) | 2011-06-01 | 2021-07-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| PT2741824T (pt) * | 2011-08-11 | 2017-07-06 | Estetra Sprl | Utilização de estetrol como contracetivo de emergência |
| TW201613576A (en) | 2014-06-26 | 2016-04-16 | Novartis Ag | Intermittent dosing of MDM2 inhibitor |
| DK3310346T3 (da) | 2015-06-18 | 2021-05-25 | Estetra Sprl | Orodispersibel tablet indeholdende estetrol |
| PL3310333T3 (pl) | 2015-06-18 | 2020-07-13 | Estetra Sprl | Ulegająca rozpadowi w jamie ustnej jednostka dawkowana zawierająca składnik estetrolowy |
| MA44205B1 (fr) * | 2015-06-18 | 2021-04-30 | Estetra Sprl | Comprimé orodispersible comprenant estetrol |
| GEP20217308B (en) | 2015-06-18 | 2021-10-25 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
| 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 |
| JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
| HU231240B1 (hu) | 2019-09-03 | 2022-04-28 | Richter Gedeon Nyrt. | Ipari eljárás nagytisztaságú ösztetrol hatóanyag előállítására |
| US20230338355A1 (en) * | 2020-07-30 | 2023-10-26 | Acer Therapeutics Inc. | Nk antagonists for contraception |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2297273A1 (en) * | 2000-01-26 | 2001-07-26 | Michael D. Perelgut | 3 dimensional imaging of hard structure without the use of ionizing radiation |
| ES2296943T3 (es) * | 2001-05-23 | 2008-05-01 | Pantarhei Bioscience B.V. | Sistema de administracion de un medicamento estrogeno tetrahidroxilado destinado a la contracepcion hormonal. |
| CA2448273C (en) * | 2001-05-23 | 2010-06-29 | Christian Franz Holinka | Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception |
| HU227198B1 (en) * | 2001-11-27 | 2010-10-28 | Richter Gedeon Nyrt | Pharmaceutical composition for emergency contraception containing levonorgestrel |
| SI1562976T1 (sl) * | 2002-11-08 | 2010-08-31 | Pantarhei Bioscience Bv | Sinteza estetrola preko steroidov, izvedenih iz estrona |
| JP2004235111A (ja) * | 2003-01-31 | 2004-08-19 | Ebara Corp | イオン伝導体及びその製造方法 |
| PT2741824T (pt) * | 2011-08-11 | 2017-07-06 | Estetra Sprl | Utilização de estetrol como contracetivo de emergência |
| EA032306B1 (ru) * | 2013-12-12 | 2019-05-31 | Донеста Байосайенс Б.В. | Орально распадающаяся твердая фармацевтическая единица дозирования, содержащая эстетрольный компонент, ее применение и способ получения |
-
2012
- 2012-08-09 PT PT127530863T patent/PT2741824T/pt unknown
- 2012-08-09 WO PCT/EP2012/065572 patent/WO2013021025A1/en active Application Filing
- 2012-08-09 CA CA2843951A patent/CA2843951C/en active Active
- 2012-08-09 LT LTEP12753086.3T patent/LT2741824T/lt unknown
- 2012-08-09 DK DK12753086.3T patent/DK2741824T3/en active
- 2012-08-09 PL PL12753086T patent/PL2741824T3/pl unknown
- 2012-08-09 ES ES12753086.3T patent/ES2631359T3/es active Active
- 2012-08-09 RS RS20170497A patent/RS55974B1/sr unknown
- 2012-08-09 HU HUE12753086A patent/HUE033590T2/hu unknown
- 2012-08-09 EA EA201400202A patent/EA028780B1/ru unknown
- 2012-08-09 US US14/238,310 patent/US9579329B2/en active Active
- 2012-08-09 AU AU2012293593A patent/AU2012293593B2/en active Active
- 2012-08-09 SI SI201230961A patent/SI2741824T1/sl unknown
- 2012-08-09 BR BR112014003113A patent/BR112014003113A2/pt not_active Application Discontinuation
- 2012-08-09 EP EP12753086.3A patent/EP2741824B1/en active Active
- 2012-08-09 ME MEP-2017-111A patent/ME02723B/me unknown
-
2014
- 2014-10-21 HK HK14110473.9A patent/HK1197027A1/xx unknown
-
2017
- 2017-01-13 US US15/405,968 patent/US20170196886A1/en not_active Abandoned
- 2017-05-26 HR HRP20170797TT patent/HRP20170797T1/hr unknown
- 2017-06-14 AU AU2017203991A patent/AU2017203991B2/en active Active
- 2017-06-20 CY CY20171100646T patent/CY1118996T1/el unknown
-
2021
- 2021-02-24 US US17/183,676 patent/US20210290636A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HK1197027A1 (en) | 2015-01-02 |
| RS55974B1 (sr) | 2017-09-29 |
| US20210290636A1 (en) | 2021-09-23 |
| DK2741824T3 (en) | 2017-07-10 |
| AU2012293593A1 (en) | 2014-03-06 |
| BR112014003113A2 (pt) | 2017-03-14 |
| US20140200202A1 (en) | 2014-07-17 |
| CA2843951C (en) | 2019-08-06 |
| CA2843951A1 (en) | 2013-02-14 |
| CY1118996T1 (el) | 2018-01-10 |
| EA028780B1 (ru) | 2017-12-29 |
| PT2741824T (pt) | 2017-07-06 |
| US9579329B2 (en) | 2017-02-28 |
| EP2741824B1 (en) | 2017-05-03 |
| EP2741824A1 (en) | 2014-06-18 |
| EA201400202A1 (ru) | 2014-06-30 |
| US20170196886A1 (en) | 2017-07-13 |
| AU2012293593A8 (en) | 2014-05-29 |
| SI2741824T1 (sl) | 2017-06-30 |
| HUE033590T2 (hu) | 2017-12-28 |
| AU2017203991A1 (en) | 2017-07-06 |
| ME02723B (me) | 2017-10-20 |
| PL2741824T3 (pl) | 2018-03-30 |
| AU2012293593B2 (en) | 2017-03-23 |
| LT2741824T (lt) | 2017-06-26 |
| AU2017203991B2 (en) | 2019-03-14 |
| WO2013021025A1 (en) | 2013-02-14 |
| ES2631359T3 (es) | 2017-08-30 |
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