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
Other languages
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 & 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)
  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (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
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
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 (enExample)
EP (1) EP1805201B1 (enExample)
JP (1) JP4889644B2 (enExample)
AR (1) AR050732A1 (enExample)
AT (1) ATE414710T1 (enExample)
AU (1) AU2005281705B2 (enExample)
BR (1) BRPI0514976A (enExample)
CA (1) CA2577497C (enExample)
DK (1) DK1805201T3 (enExample)
ES (1) ES2317312T3 (enExample)
NZ (1) NZ553266A (enExample)
PE (1) PE20060590A1 (enExample)
PL (1) PL1805201T3 (enExample)
PT (1) PT1805201E (enExample)
RS (1) RS51640B (enExample)
RU (1) RU2386637C2 (enExample)
SI (1) SI1805201T1 (enExample)
TW (1) TW200621795A (enExample)
UA (1) UA89964C2 (enExample)
WO (1) WO2006027347A1 (enExample)

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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
EP2448901A1 (en) * 2009-06-29 2012-05-09 Merz Pharma GmbH & Co. KGaA Method of preparing 3,3,5,5-tetramethylcyclohexanone
ES2416462T3 (es) * 2009-06-29 2013-08-01 Merz Pharma Gmbh & Co. Kgaa Método de preparación de neramexane.
EP2448908B1 (en) * 2009-06-29 2013-09-18 Merz Pharma GmbH & Co. KGaA Method of preparing neramexane
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
AU2012320423C1 (en) * 2011-10-07 2018-01-25 Estetra Srl Process for the production of estetrol
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
AU2014300894A1 (en) 2013-06-25 2016-01-28 Forendo Pharma Ltd Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase
US10413557B2 (en) 2014-12-23 2019-09-17 Forendo Pharma Ltd. Prodrugs of 17.BETA.-HSD1-inhibitors
WO2016102775A1 (en) 2014-12-23 2016-06-30 Forendo Pharma Ltd PRODRUGS OF 17β-HSD1 -INHIBITORS
MA44206B1 (fr) 2015-06-18 2021-04-30 Estetra Sprl Comprimé orodispersible comprenant estetrol
CU24523B1 (es) 2015-06-18 2021-06-08 Estetra Sprl Unidad de dosificación orodispersable que contiene un componente estetrol
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
EP3701944B1 (en) 2015-06-18 2021-12-08 Estetra SRL 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
SG11201911776PA (en) 2017-06-08 2020-01-30 Forendo Pharma Ltd 15.beta.-[3-propanamido]-substituted estra-1,3,5(10)-trien-17-one compounds and their 17-oximes for use in inhibition of 17.beta.-hydroxysteroid dehydrogenases
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
EP3781171B1 (en) 2018-04-19 2022-02-09 Estetra SRL Compounds and their uses for alleviating menopause-associated symptoms
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

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DE1084261B (de) 1957-04-11 1960-06-30 Syntex Sa Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
US3257429A (en) * 1957-11-12 1966-06-21 Syntex Corp 16-methylene derivatives of estrone and estradiol
US3007946A (en) 1958-11-06 1961-11-07 Searle & Co 3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones
US3049555A (en) 1959-12-22 1962-08-14 Searle & Co 3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones
US3092645A (en) 1961-12-28 1963-06-04 Searle & Co Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols
GB1110792A (en) 1964-04-07 1968-04-24 Res Inst Medicine Chem Novel 5(10)-dehydro-steroids
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US3465010A (en) 1966-11-22 1969-09-02 Searle & Co 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof
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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
AU572589B2 (en) 1983-12-14 1988-05-12 Upjohn Company, The 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids
US5116830A (en) 1984-08-17 1992-05-26 Sri International Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses
US5204337A (en) * 1988-10-31 1993-04-20 Endorecherche Inc. Estrogen nucleus derivatives for use in inhibition of sex steroid activity
ZA94715B (en) 1993-02-08 1994-10-24 Akzo Nv Steroids for treating menopausal complaints
EP0613687B1 (en) 1993-03-05 1999-06-02 Akzo Nobel N.V. Use of a pregnane derivatives for the treatment of tumours
CA2200423C (en) 1996-03-26 2006-12-19 Sietse Mosselman Novel estrogen receptor
TW403736B (en) 1997-02-21 2000-09-01 Akzo Nobel Nv Steroid compounds having contraceptive and anti-osteoporosis activity
CA2319765A1 (en) 1998-03-09 1999-09-16 Akzo Nobel Nv New contraceptive kit
TR200003743T2 (tr) 1998-06-19 2001-07-23 Akzo Nobel N.V. Testosteron türevi.
WO2000031112A1 (en) 1998-11-20 2000-06-02 Akzo Nobel N.V. Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11
TW548277B (en) 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens
NZ517281A (en) 1999-09-06 2003-09-26 Akzo Nobel Nv Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11
PT1226155E (pt) * 1999-11-02 2007-07-26 Bayer Schering Pharma Ag 18-nor-esteróides como estrogénios selectivamente activos
US7696190B2 (en) * 2000-07-28 2010-04-13 N.V. Organon 16Alpha-methyl or ethyl substituted estrogens

Also Published As

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

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Effective date: 20150908