AU2005281705B2 - 15beta-substituted steroids having selective estrogenic activity - Google Patents

15beta-substituted steroids having selective estrogenic activity Download PDF

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Publication number
AU2005281705B2
AU2005281705B2 AU2005281705A AU2005281705A AU2005281705B2 AU 2005281705 B2 AU2005281705 B2 AU 2005281705B2 AU 2005281705 A AU2005281705 A AU 2005281705A AU 2005281705 A AU2005281705 A AU 2005281705A AU 2005281705 B2 AU2005281705 B2 AU 2005281705B2
Authority
AU
Australia
Prior art keywords
alkyl
compound
compound according
estrogen
treatment
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2005281705A
Other languages
English (en)
Other versions
AU2005281705A1 (en
Inventor
Fredericus Antonius Dijcks
Antonius Gerardus Hendrikus Ederveen
Hubert Jan Jozef Loozen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme BV
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme BV
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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme BV filed Critical Merck Sharp and Dohme Ltd
Publication of AU2005281705A1 publication Critical patent/AU2005281705A1/en
Application granted granted Critical
Publication of AU2005281705B2 publication Critical patent/AU2005281705B2/en
Assigned to MSD OSS B.V. reassignment MSD OSS B.V. Request to Amend Deed and Register Assignors: N.V ORGANON
Assigned to MERCK SHARP & DOHME B.V. reassignment MERCK SHARP & DOHME B.V. Request to Amend Deed and Register Assignors: MSD OSS B.V.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • 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
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • 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

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2005281705A 2004-09-08 2005-09-05 15beta-substituted steroids having selective estrogenic activity Ceased AU2005281705B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US60850104P 2004-09-08 2004-09-08
US60/608,501 2004-09-08
EP04104334 2004-09-08
EP04104334.0 2004-09-08
PCT/EP2005/054368 WO2006027347A1 (en) 2004-09-08 2005-09-05 15β-SUBSTITUTED STEROIDS HAVING SELECTIVE ESTROGENIC ACTIVITY

Publications (2)

Publication Number Publication Date
AU2005281705A1 AU2005281705A1 (en) 2006-03-16
AU2005281705B2 true AU2005281705B2 (en) 2011-03-10

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005281705A Ceased AU2005281705B2 (en) 2004-09-08 2005-09-05 15beta-substituted steroids having selective estrogenic activity

Country Status (20)

Country Link
US (1) US7838516B2 (OSRAM)
EP (1) EP1805201B1 (OSRAM)
JP (1) JP4889644B2 (OSRAM)
AR (1) AR050732A1 (OSRAM)
AT (1) ATE414710T1 (OSRAM)
AU (1) AU2005281705B2 (OSRAM)
BR (1) BRPI0514976A (OSRAM)
CA (1) CA2577497C (OSRAM)
DK (1) DK1805201T3 (OSRAM)
ES (1) ES2317312T3 (OSRAM)
NZ (1) NZ553266A (OSRAM)
PE (1) PE20060590A1 (OSRAM)
PL (1) PL1805201T3 (OSRAM)
PT (1) PT1805201E (OSRAM)
RS (1) RS51640B (OSRAM)
RU (1) RU2386637C2 (OSRAM)
SI (1) SI1805201T1 (OSRAM)
TW (1) TW200621795A (OSRAM)
UA (1) UA89964C2 (OSRAM)
WO (1) WO2006027347A1 (OSRAM)

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US8030298B2 (en) 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
CA2765609A1 (en) * 2009-06-29 2011-01-06 Merz Pharma Gmbh & Co. Kgaa Method of preparing neramexane
BRPI1012669A2 (pt) * 2009-06-29 2016-04-05 Merz Pharma Gmbh & Co Kgaa metodo de preparacao de 3,3,5,5-tetrametliciclohexanona, método de preparção de 1-amino-1,3,3,5,5,-pentametilciclohexano ou um sal farmaceuticamente aceitável do mesmo e composto
DK2448910T3 (da) * 2009-06-29 2013-06-03 Merz Pharma Gmbh & Co Kgaa Fremgangsmåde til fremstilling af neramexan
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
PL2764008T3 (pl) * 2011-10-07 2017-04-28 Estetra S.P.R.L. Sposób wytwarzania estetrolu
AR096728A1 (es) 2013-06-25 2016-01-27 Forendo Pharma Ltd Derivados de estratrieno-tiazol terapéuticamente activos
JP6456373B2 (ja) 2013-06-25 2019-01-23 フォレンド ファーマ リミテッド 17β−ヒドロキシステロイドデヒドロゲナーゼ タイプ1の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体
AR096729A1 (es) 2013-06-25 2016-01-27 Forendo Pharma Ltd Derivados terapéuticamente activos de estratien-tiazol
JP6523461B2 (ja) 2014-12-23 2019-06-05 フォレンド ファーマ リミテッド 17β−HSD1−阻害剤のプロドラッグ
WO2016102775A1 (en) 2014-12-23 2016-06-30 Forendo Pharma Ltd PRODRUGS OF 17β-HSD1 -INHIBITORS
HUE054551T2 (hu) 2015-06-18 2021-09-28 Estetra Sprl Ösztetrolt tartalmazó, szájban diszpergálódó tabletta
EP3106148B1 (en) 2015-06-18 2018-03-14 Mithra Pharmaceuticals S.A. Orodispersible dosage unit containing an estetrol component
HRP20200850T1 (hr) 2015-06-18 2020-10-02 Estetra Sprl Orodisperzibilna jedinica za doziranje koja sadrži komponentu estetrola
JP6866561B2 (ja) 2015-06-18 2021-04-28 エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ エステトロールを含有する口腔内崩壊錠
KR102712911B1 (ko) 2016-08-05 2024-10-04 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
DK3634975T3 (da) 2017-06-08 2024-05-27 Organon R&D Finland Ltd 17-oximer af 15.beta.-[3-propanamido]-substituerede estra-1,3,5(10)-trien-17-oner til anvendelse i inhibition af 17.beta.-hydroxysteroid-dehydrogenaser
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
CA3122049C (en) 2018-12-05 2023-10-17 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1
TWI893101B (zh) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 具有降低之副作用之避孕組成物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5686437A (en) * 1988-10-31 1997-11-11 Endorecherche Inc. Estrogen nucleus derivatives for use in the inhibition of sex steroid activity

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US3257429A (en) * 1957-11-12 1966-06-21 Syntex Corp 16-methylene derivatives of estrone and estradiol
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FR2377419A1 (fr) 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament
DE2757157C3 (de) 1977-12-19 1980-10-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von 16 a -alkylierten Steroiden
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Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5686437A (en) * 1988-10-31 1997-11-11 Endorecherche Inc. Estrogen nucleus derivatives for use in the inhibition of sex steroid activity

Also Published As

Publication number Publication date
DK1805201T3 (da) 2009-01-12
CA2577497C (en) 2012-03-20
RU2386637C2 (ru) 2010-04-20
JP2008512426A (ja) 2008-04-24
ES2317312T3 (es) 2009-04-16
US7838516B2 (en) 2010-11-23
ATE414710T1 (de) 2008-12-15
WO2006027347A1 (en) 2006-03-16
NZ553266A (en) 2009-06-26
JP4889644B2 (ja) 2012-03-07
US20070254860A1 (en) 2007-11-01
RS51640B (sr) 2011-10-31
RS20070075A (sr) 2008-09-29
AR050732A1 (es) 2006-11-15
TW200621795A (en) 2006-07-01
PT1805201E (pt) 2008-12-31
AU2005281705A1 (en) 2006-03-16
CA2577497A1 (en) 2006-03-16
UA89964C2 (ru) 2010-03-25
PL1805201T3 (pl) 2009-04-30
SI1805201T1 (sl) 2009-04-30
EP1805201A1 (en) 2007-07-11
BRPI0514976A (pt) 2008-07-01
RU2007112939A (ru) 2008-11-10
PE20060590A1 (es) 2006-07-14
EP1805201B1 (en) 2008-11-19

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired