CA2577497C - 15.beta.-substituted steroids having selective estrogenic activity - Google Patents

15.beta.-substituted steroids having selective estrogenic activity Download PDF

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Publication number
CA2577497C
CA2577497C CA2577497A CA2577497A CA2577497C CA 2577497 C CA2577497 C CA 2577497C CA 2577497 A CA2577497 A CA 2577497A CA 2577497 A CA2577497 A CA 2577497A CA 2577497 C CA2577497 C CA 2577497C
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CA
Canada
Prior art keywords
treatment
prevention
estrogen receptor
estrogen
alkyl
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.)
Expired - Fee Related
Application number
CA2577497A
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English (en)
French (fr)
Other versions
CA2577497A1 (en
Inventor
Hubert Jan Jozef Loozen
Antonius Gerardus Hendrikus Ederveen
Fredericus Antonius Dijcks
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
MSD Oss 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 MSD Oss BV filed Critical MSD Oss BV
Publication of CA2577497A1 publication Critical patent/CA2577497A1/en
Application granted granted Critical
Publication of CA2577497C publication Critical patent/CA2577497C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (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)
CA2577497A 2004-09-08 2005-09-05 15.beta.-substituted steroids having selective estrogenic activity Expired - Fee Related CA2577497C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US60850104P 2004-09-08 2004-09-08
EP04104334.0 2004-09-08
EP04104334 2004-09-08
US60/608,501 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
CA2577497A1 CA2577497A1 (en) 2006-03-16
CA2577497C true CA2577497C (en) 2012-03-20

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2577497A Expired - Fee Related CA2577497C (en) 2004-09-08 2005-09-05 15.beta.-substituted steroids having selective estrogenic activity

Country Status (20)

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

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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
HRP20130486T1 (en) * 2009-06-29 2013-06-30 Merz Pharma Gmbh & Co. Kgaa Method of preparing neramexane
JP5749260B2 (ja) * 2009-06-29 2015-07-15 メルツ・ファルマ・ゲーエムベーハー・ウント・コ・カーゲーアーアー ネラメキサンの製造方法
WO2011000540A1 (en) * 2009-06-29 2011-01-06 Merz Pharma Gmbh & Co. Kgaa Method of preparing 3,3,5,5-tetramethylcyclohexanone
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
RS55231B1 (sr) * 2011-10-07 2017-02-28 Estetra Sprl Postupak proizvodnje estetrola
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
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
JP6556125B2 (ja) 2013-06-25 2019-08-07 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の阻害剤としての治療的に活性な１７−窒素置換エストラトリエンチアゾール誘導体
CN107207561B (zh) 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
JP6545266B2 (ja) 2014-12-23 2019-07-17 フォレンド ファーマ リミテッド １７β‐ＨＳＤ１抑制剤のプロドラッグ
DK3701944T3 (da) 2015-06-18 2022-03-14 Estetra Srl Oro-dispergerbar doseringsenhed indeholdende en estetrolkomponent
CR20180042A (es) 2015-06-18 2018-05-03 Mithra Pharmaceuticals S A Unidad de dosificación orodispersable que contiene un componente estetrol.
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
LT3310346T (lt) 2015-06-18 2021-06-10 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
KR102712911B1 (ko) 2016-08-05 2024-10-04 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
HRP20240679T1 (hr) 2017-06-08 2024-08-16 Organon R&D Finland Ltd 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza
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
CN111989105B (zh) 2018-04-19 2024-07-19 埃斯特拉私人有限责任公司 化合物以及它们在缓解绝经相关症状中的用途
JP7417608B2 (ja) 2018-12-05 2024-01-18 フォレンド ファーマ リミテッド １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物
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

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DE1084261B (de) 1957-04-11 1960-06-30 Syntex Sa Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
NL226738A (https=) 1957-04-11
US3257429A (en) * 1957-11-12 1966-06-21 Syntex Corp 16-methylene derivatives of estrone and estradiol
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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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Also Published As

Publication number Publication date
RS20070075A (sr) 2008-09-29
EP1805201A1 (en) 2007-07-11
PT1805201E (pt) 2008-12-31
BRPI0514976A (pt) 2008-07-01
PL1805201T3 (pl) 2009-04-30
PE20060590A1 (es) 2006-07-14
ATE414710T1 (de) 2008-12-15
TW200621795A (en) 2006-07-01
ES2317312T3 (es) 2009-04-16
US7838516B2 (en) 2010-11-23
RU2007112939A (ru) 2008-11-10
UA89964C2 (ru) 2010-03-25
RU2386637C2 (ru) 2010-04-20
EP1805201B1 (en) 2008-11-19
SI1805201T1 (sl) 2009-04-30
AU2005281705A1 (en) 2006-03-16
DK1805201T3 (da) 2009-01-12
RS51640B (sr) 2011-10-31
WO2006027347A1 (en) 2006-03-16
JP2008512426A (ja) 2008-04-24
US20070254860A1 (en) 2007-11-01
AR050732A1 (es) 2006-11-15
JP4889644B2 (ja) 2012-03-07
NZ553266A (en) 2009-06-26
AU2005281705B2 (en) 2011-03-10
CA2577497A1 (en) 2006-03-16

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Effective date: 20150908