PE20210155A1 - Anticonceptivos de profarmacos de progestina de accion mas prolongada - Google Patents
Anticonceptivos de profarmacos de progestina de accion mas prolongadaInfo
- Publication number
- PE20210155A1 PE20210155A1 PE2020000487A PE2020000487A PE20210155A1 PE 20210155 A1 PE20210155 A1 PE 20210155A1 PE 2020000487 A PE2020000487 A PE 2020000487A PE 2020000487 A PE2020000487 A PE 2020000487A PE 20210155 A1 PE20210155 A1 PE 20210155A1
- Authority
- PE
- Peru
- Prior art keywords
- progestin
- alkyl
- contraceptives
- drugs
- etonogestrel
- Prior art date
Links
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
- 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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/34—Gestagens
-
- 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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Dispersion Chemistry (AREA)
- Toxicology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invencion se refiere se refiere a compuestos de progestina que tienen tasas de liberacion prolongada y que se pueden usar sin un estrogeno para producir un estado anticonceptivo. Estos compuestos presentan la formula I (Figura 1) donde la progestina es levonorgestrel o etonogestrel; y R1, R2 se combinan para formar un anillo de 3 a 7 miembros fusionado con hasta dos heteroatomos, o cada R1, R2 es H, alquilo, cicloalquilo, fenilo, arilo, heteroarilo, acilo, ciano, halogeno, OH, alcoxi, alquil-sulfonilo o sulfonamida; y presenta la formula II (Figura 2) en donde la progestina es levonorgestrel o etonogestrel; hAr es piridina, pirimidina, pirazina u oxazol; R1, R2 se combinan para formar un anillo de 3 a 7 miembros fusionado con hasta dos heteroatomos, o cada R1, R2 es H, alquilo, cicloalquilo, fenilo, arilo, heteroarilo, acilo, ciano, halogeno, OH, alcoxi, alquilsulfonilo o sulfonamida.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762574445P | 2017-10-19 | 2017-10-19 | |
PCT/US2018/051026 WO2019078983A1 (en) | 2017-10-19 | 2018-09-14 | CONTRACEPTIVES OF PROGESTINE PRODRANT WITH EXTENDED ACTION |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20210155A1 true PE20210155A1 (es) | 2021-01-26 |
Family
ID=66169066
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2020000487A PE20210155A1 (es) | 2017-10-19 | 2018-09-14 | Anticonceptivos de profarmacos de progestina de accion mas prolongada |
Country Status (10)
Country | Link |
---|---|
US (1) | US10624903B2 (es) |
EP (1) | EP3697421B1 (es) |
AU (1) | AU2018353858A1 (es) |
BR (1) | BR112020007673A2 (es) |
CL (1) | CL2020001028A1 (es) |
CO (1) | CO2020003537A2 (es) |
EC (1) | ECSP20026239A (es) |
MX (1) | MX2020003470A (es) |
PE (1) | PE20210155A1 (es) |
WO (1) | WO2019078983A1 (es) |
Family Cites Families (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB753793A (en) * | 1953-07-17 | 1956-08-01 | Schering Corp | Aryloxy esters of testosterone, and therapeutic compositions thereof |
DE1018416B (de) * | 1953-07-17 | 1957-10-31 | Schering Corp | Verfahren zur Herstellung von Aryloxyestern des Testosterons |
US3051731A (en) * | 1960-04-11 | 1962-08-28 | Parke Davis & Co | 5, 6, 7, 8-tetrahydro-1-methyl-2-naphthoxy-acetic acid esters of hydroxy steroids |
GB1069779A (en) * | 1965-05-05 | 1967-05-24 | Schering Ag | 17ª-ethynyl-18-methyl-19-nor-testosterone esters and process for their manufacture |
US3461118A (en) | 1966-10-17 | 1969-08-12 | Syntex Corp | 3beta-tetrahydrofuranyloxy - and 3beta-tetrahydropyranyloxyestra - 4,9(10) - dienes and -4,9(10),11-trienes,their preparation and intermediates thereof |
GB1355663A (en) * | 1970-06-17 | 1974-06-05 | Theramex | 19-nortestosterone 17- -p-substituted phenoxy-acetates |
US4507290A (en) * | 1981-04-07 | 1985-03-26 | World Health Organization | Esters of 17 α-ethynyl 19-nor-testosterone and 17 α-ethynyl-18-homo-19-nor-testosterone and pharmaceutical compositions containing the same |
GB8313921D0 (en) * | 1983-05-19 | 1983-06-22 | World Health Org | Contraceptive compositions |
US4615835A (en) | 1983-11-17 | 1986-10-07 | Stiftung Deutsches Krebsforschungs Zentrum | Steroid esters of N-(2-halogenethyl)-N-nitroso-carbamoylamino and acids and peptides therefore, as well as method for preparing them |
DE3511588A1 (de) * | 1985-03-27 | 1986-10-02 | Schering AG, Berlin und Bergkamen, 1000 Berlin | Waessrige kristallsuspension von steroidglykoestern |
SE8802402D0 (sv) | 1988-06-28 | 1988-06-28 | Pharmacia Ab | Novel esters |
DE4029499A1 (de) | 1990-09-18 | 1992-03-19 | Boehringer Mannheim Gmbh | Neue 17-(beta)-oestradiolderivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
DE4429397C2 (de) | 1994-08-09 | 2003-11-20 | Jenapharm Gmbh | Estra-1,3,5(10)-trien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
DE4447714C2 (de) | 1994-08-09 | 1998-02-05 | Jenapharm Gmbh | Verwendung von Estra-1,3,5(10)-trien-Derivaten zur Hormonsubstitutions-Therapie |
US5705495A (en) | 1995-10-19 | 1998-01-06 | Jenapharm Gmbh & Co. Kg. | Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for their production and pharmaceuticals containing these compounds |
FR2774989B1 (fr) | 1998-02-18 | 2000-03-17 | Adir | Nouveaux cytotoxiques derives de l'oestradiol |
US6958327B1 (en) | 1999-11-02 | 2005-10-25 | Schering, Ag | 18 Norsteroids as selectively active estrogens |
FR2801218B1 (fr) | 1999-11-23 | 2001-12-28 | Hoechst Marion Roussel Inc | Compositions pharmaceutiques comprenant de la trimegestone, leurs procedes de preparation ainsi que le conditionnement primaire les renfermant |
DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
US6956031B2 (en) | 2002-03-27 | 2005-10-18 | Schering Aktiengesellschaft | 11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring |
TW200400041A (en) * | 2002-05-30 | 2004-01-01 | Akzo Nobel Nv | Use of new etonogestrel esters |
US7414043B2 (en) | 2002-06-11 | 2008-08-19 | Schering Ag | 9-α-substituted estratrienes as selectively active estrogens |
US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
US20050277625A1 (en) * | 2004-05-21 | 2005-12-15 | Ralf Wyrwa | Estriol and estetrol prodrugs |
US10137135B2 (en) * | 2005-08-15 | 2018-11-27 | Allergan Sales, Llc | Formulations and methods for providing progestin-only contraception while minimizing adverse side effects associated therewith |
US20070197488A1 (en) * | 2005-11-29 | 2007-08-23 | Olaf Peters | Prodrugs of ERbeta-selective substances, process for their production, and pharmaceutical compositions that contain these compounds |
US20070135375A1 (en) | 2005-11-30 | 2007-06-14 | Ralf Wyrwa | Sulfamoyl sulfonate prodrugs |
US20070135399A1 (en) * | 2005-11-30 | 2007-06-14 | Ralf Wyrwa | Heteroaromatic sulphonamide prodrugs |
EP2162432A2 (en) | 2007-06-29 | 2010-03-17 | Gilead Sciences, Inc. | Antiviral compounds |
US20100061976A1 (en) | 2008-07-24 | 2010-03-11 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Method for treating or preventing osteoporosis by reducing follicle stimulating hormone to cyclic physiological levels in a mammalian subject |
EP2419398A4 (en) * | 2009-04-14 | 2012-11-28 | Infiniton Ab | PRO-BET WITH BETA-KETO-CARBOXYLIC ACID, BETA-KETO-CARBOXYLIC ACID SALT OR BETA-KETO-CARBOXYLIC ACID ESTERS FOR ACTIVE INHIBITION |
CN104130172B (zh) | 2009-12-14 | 2016-05-18 | 罗门哈斯电子材料有限公司 | 磺酰光酸产生剂和包含该磺酰光酸产生剂的光刻胶 |
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CN102127137A (zh) | 2010-12-10 | 2011-07-20 | 郑州大学 | 制备雌甾氨基酸酯的中间体化合物及其合成方法 |
WO2015006691A1 (en) * | 2013-07-11 | 2015-01-15 | Evestra, Inc. | Pro-drug forming compounds |
-
2018
- 2018-09-14 PE PE2020000487A patent/PE20210155A1/es unknown
- 2018-09-14 AU AU2018353858A patent/AU2018353858A1/en active Pending
- 2018-09-14 US US16/131,640 patent/US10624903B2/en active Active
- 2018-09-14 WO PCT/US2018/051026 patent/WO2019078983A1/en unknown
- 2018-09-14 EP EP18868866.7A patent/EP3697421B1/en active Active
- 2018-09-14 MX MX2020003470A patent/MX2020003470A/es unknown
- 2018-09-14 BR BR112020007673-2A patent/BR112020007673A2/pt unknown
-
2020
- 2020-03-26 CO CONC2020/0003537A patent/CO2020003537A2/es unknown
- 2020-04-16 CL CL2020001028A patent/CL2020001028A1/es unknown
- 2020-05-19 EC ECSENADI202026239A patent/ECSP20026239A/es unknown
Also Published As
Publication number | Publication date |
---|---|
CO2020003537A2 (es) | 2020-06-19 |
AU2018353858A1 (en) | 2020-04-02 |
WO2019078983A1 (en) | 2019-04-25 |
CL2020001028A1 (es) | 2020-10-23 |
US20190117670A1 (en) | 2019-04-25 |
BR112020007673A2 (pt) | 2020-10-13 |
MX2020003470A (es) | 2020-10-01 |
EP3697421A1 (en) | 2020-08-26 |
ECSP20026239A (es) | 2020-10-30 |
EP3697421C0 (en) | 2024-04-17 |
US10624903B2 (en) | 2020-04-21 |
EP3697421A4 (en) | 2021-06-16 |
EP3697421B1 (en) | 2024-04-17 |
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