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CL2022000492A1 - Proceso para la preparación de estetrol de alta pureza. - Google Patents

Proceso para la preparación de estetrol de alta pureza.

Info

Publication number
CL2022000492A1
CL2022000492A1 CL2022000492A CL2022000492A CL2022000492A1 CL 2022000492 A1 CL2022000492 A1 CL 2022000492A1 CL 2022000492 A CL2022000492 A CL 2022000492A CL 2022000492 A CL2022000492 A CL 2022000492A CL 2022000492 A1 CL2022000492 A1 CL 2022000492A1
Authority
CL
Chile
Prior art keywords
estetrol
preparation
high purity
intermediate compounds
purity
Prior art date
Application number
CL2022000492A
Other languages
English (en)
Inventor
Róbert Lovas
Sándor Mahó
Ildikó Bacsa
Beatrix Mayer
Original Assignee
Richter Gedeon Nyrt
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Richter Gedeon Nyrt filed Critical Richter Gedeon Nyrt
Publication of CL2022000492A1 publication Critical patent/CL2022000492A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/566Compounds 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 having an oxo group in position 17, e.g. estrone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J75/00Processes for the preparation of steroids in general
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Diabetes (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PROCESO PARA LA PREPARACIÓN DE ESTETROL DE ALTA PUREZA; SU USO Y COMPUESTOS INTERMEDIARIOS.
CL2022000492A 2019-09-03 2022-02-28 Proceso para la preparación de estetrol de alta pureza. CL2022000492A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU1900315A HU231240B1 (hu) 2019-09-03 2019-09-03 Ipari eljárás nagytisztaságú ösztetrol hatóanyag előállítására

Publications (1)

Publication Number Publication Date
CL2022000492A1 true CL2022000492A1 (es) 2023-03-10

Family

ID=89992977

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2022000492A CL2022000492A1 (es) 2019-09-03 2022-02-28 Proceso para la preparación de estetrol de alta pureza.

Country Status (30)

Country Link
US (1) US11633406B2 (es)
EP (1) EP3877395B1 (es)
JP (1) JP7265087B2 (es)
KR (1) KR20220071206A (es)
CN (1) CN114302889B (es)
AU (1) AU2020343497B2 (es)
CA (1) CA3147815C (es)
CL (1) CL2022000492A1 (es)
CO (1) CO2022003769A2 (es)
CU (1) CU24692B1 (es)
DK (1) DK3877395T3 (es)
EC (1) ECSP22022403A (es)
ES (1) ES2855923T3 (es)
FI (1) FI3877395T3 (es)
GE (1) GEP20247626B (es)
HR (1) HRP20230230T1 (es)
HU (2) HU231240B1 (es)
IL (1) IL290973B2 (es)
JO (1) JOP20220041A1 (es)
LT (1) LT3877395T (es)
MA (1) MA54200B1 (es)
MD (1) MD3877395T2 (es)
MX (1) MX2022002603A (es)
PE (1) PE20221418A1 (es)
PL (1) PL3877395T3 (es)
PT (1) PT3877395T (es)
RS (1) RS63966B1 (es)
SI (1) SI3877395T1 (es)
WO (1) WO2021044302A1 (es)
ZA (1) ZA202203557B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020355615B2 (en) * 2019-09-27 2023-12-14 Industriale Chimica S.R.L. Process for preparing (15α,16α,17β)-Estra-1,3,5(10)-Triene-3,15,16,17-Tetrol (Estetrol) and intermediates of said process
WO2023051937A1 (en) * 2021-10-01 2023-04-06 Industriale Chimica S.R.L. Process for preparing (15alpha,16alpha,17 eta)-estra-1,3,5(10)-triene-3,15,16,17-tetrol (estetrol) monohydrate
WO2024160373A1 (en) 2023-02-02 2024-08-08 Industriale Chimica S.R.L. PROCESS FOR PREPARING (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL (ESTETROL) MONOHYDRATE

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60217324T2 (de) 2001-05-18 2007-04-26 Pantarhei Bioscience B.V. Pharmazeutische zusammensetzung für die hormonersatztherapie
EP1260225A1 (en) 2001-05-18 2002-11-27 Pantarhei Bioscience B.V. A pharmaceutical composition for use in hormone replacement therapy
EP1390042B1 (en) 2001-05-23 2007-11-28 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
WO2002094278A1 (en) 2001-05-23 2002-11-28 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
PT1446128E (pt) 2001-11-15 2007-03-30 Pantarhei Bioscience Bv Utilização de compostos estrogénicos combinados com compostos progestagénicos na terapia hormonal de substituição
CA2489271C (en) 2002-06-11 2011-12-06 Pantarhei Bioscience B.V. Method of treating or preventing immune mediated disorders and pharmaceutical formulation for use therein
CA2489270C (en) 2002-06-11 2012-08-07 Pantarhei Bioscience B.V. A method of treating human skin and a skin care composition for use in such a method
CA2492287C (en) 2002-07-12 2011-12-13 Pantarhei Bioscience B.V. Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
AU2003274823A1 (en) 2002-10-23 2004-05-13 Pantarhei Bioscience B.V. Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy
US20060211669A1 (en) * 2002-11-08 2006-09-21 Verhaar Mark T Synthesis of estetrol via estrone derived steroids
EP1971344B1 (en) 2006-01-09 2010-09-22 Pantarhei Bioscience B.V. A method of treating an acute vascular disorder
EP2114412B1 (en) 2007-01-08 2010-07-14 Pantarhei Bioscience B.V. Method of treating or preventing infertility in a female mammal and pharmaceutical kit for use in such method
EP2383279A1 (en) * 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
BR112014003113A2 (pt) 2011-08-11 2017-03-14 Estetra Sprl método de contracepção de emergência em uma fêmea mamífero
EP2764008B1 (en) 2011-10-07 2016-08-17 Estetra S.P.R.L. Process for the production of estetrol
EP2653163A1 (en) 2012-04-19 2013-10-23 Université de Liège Estrogenic components for use in the treatment of neurological disorders
WO2013034780A2 (en) 2012-12-20 2013-03-14 Crystal Pharma, S.A.U. Process for the preparation of estetrol and related compounds
WO2015040051A1 (en) 2013-09-18 2015-03-26 Crystal Pharma, S.A.U. Process for the preparation of estetrol
CN105979935B (zh) 2013-12-12 2019-07-26 多内斯塔生物科学股份有限公司 包含雌四醇组分的口崩固体剂量单位
RS61777B1 (sr) 2015-06-18 2021-06-30 Estetra Sprl Oralno-disperzibilna tableta koja sadrži estetrol
HRP20211968T1 (hr) 2015-06-18 2022-03-18 Estetra Srl Orodisperzibilna jedinica za doziranje koja sadrži komponentu estetrola
ES2877186T3 (es) 2015-06-18 2021-11-16 Estetra Sprl Comprimido orodispersable que contiene estetrol
CA3041016C (en) 2016-10-28 2023-09-05 Estetra Sprl Method for the management of dysmenorrhea and menstrual pain
KR102712911B1 (ko) 2016-08-05 2024-10-04 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
BR112020002094A2 (pt) 2017-08-01 2020-07-28 Fund Sa terapia adjuvante para o uso em tratamento de câncer de próstata
MA51733A (fr) 2018-02-07 2020-12-16 Estetra Sprl Composition contraceptive présentant des effets cardiovasculaires réduits
AU2020355615B2 (en) 2019-09-27 2023-12-14 Industriale Chimica S.R.L. Process for preparing (15α,16α,17β)-Estra-1,3,5(10)-Triene-3,15,16,17-Tetrol (Estetrol) and intermediates of said process

Also Published As

Publication number Publication date
HRP20230230T1 (hr) 2023-04-14
PL3877395T3 (pl) 2023-05-08
JP2022546016A (ja) 2022-11-02
HU231240B1 (hu) 2022-04-28
CU24692B1 (es) 2024-01-10
ECSP22022403A (es) 2022-04-29
KR20220071206A (ko) 2022-05-31
JP7265087B2 (ja) 2023-04-25
CA3147815C (en) 2023-03-28
CO2022003769A2 (es) 2022-04-19
BR112022003254A2 (pt) 2022-05-17
EP3877395A1 (en) 2021-09-15
ES2855923T1 (es) 2021-09-24
SI3877395T1 (sl) 2023-03-31
CN114302889A (zh) 2022-04-08
HUE061427T2 (hu) 2023-07-28
MA54200A (fr) 2022-04-27
CN114302889B (zh) 2023-08-29
US11633406B2 (en) 2023-04-25
MX2022002603A (es) 2022-03-25
CU20220013A7 (es) 2022-10-11
MD3877395T2 (ro) 2023-05-31
AU2020343497A1 (en) 2022-04-14
AU2020343497B2 (en) 2023-02-02
US20220296609A1 (en) 2022-09-22
MA54200B1 (fr) 2023-02-28
JOP20220041A1 (ar) 2023-01-30
HUP1900315A1 (hu) 2021-03-29
PE20221418A1 (es) 2022-09-20
RS63966B1 (sr) 2023-03-31
LT3877395T (lt) 2023-02-27
IL290973B2 (en) 2023-11-01
PT3877395T (pt) 2023-02-02
IL290973B1 (en) 2023-07-01
EP3877395B1 (en) 2022-12-07
DK3877395T3 (da) 2023-03-06
GEP20247626B (en) 2024-05-27
IL290973A (en) 2022-05-01
WO2021044302A1 (en) 2021-03-11
FI3877395T3 (fi) 2023-03-18
ZA202203557B (en) 2022-11-30
CA3147815A1 (en) 2021-03-11
ES2855923T3 (es) 2023-04-28

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