ES2317312T3 - Esteroides 15beta-sustituidos que tienen actividad estrogenica selectiva. - Google Patents

Esteroides 15beta-sustituidos que tienen actividad estrogenica selectiva. Download PDF

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Publication number
ES2317312T3
ES2317312T3 ES05794597T ES05794597T ES2317312T3 ES 2317312 T3 ES2317312 T3 ES 2317312T3 ES 05794597 T ES05794597 T ES 05794597T ES 05794597 T ES05794597 T ES 05794597T ES 2317312 T3 ES2317312 T3 ES 2317312T3
Authority
ES
Spain
Prior art keywords
alkyl
compound
estrogen
compound according
acyl
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 - Lifetime
Application number
ES05794597T
Other languages
English (en)
Spanish (es)
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.)
Organon NV
Original Assignee
Organon NV
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 Organon NV filed Critical Organon NV
Application granted granted Critical
Publication of ES2317312T3 publication Critical patent/ES2317312T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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)
  • 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)
ES05794597T 2004-09-08 2005-09-05 Esteroides 15beta-sustituidos que tienen actividad estrogenica selectiva. Expired - Lifetime ES2317312T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US60850104P 2004-09-08 2004-09-08
EP04104334 2004-09-08
EP04104334 2004-09-08
US608501P 2004-09-08

Publications (1)

Publication Number Publication Date
ES2317312T3 true ES2317312T3 (es) 2009-04-16

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
ES05794597T Expired - Lifetime ES2317312T3 (es) 2004-09-08 2005-09-05 Esteroides 15beta-sustituidos que tienen actividad estrogenica selectiva.

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)

Families Citing this family (23)

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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

Family Cites Families (31)

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DE1084261B (de) 1957-04-11 1960-06-30 Syntex Sa Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
NL226738A (OSRAM) 1957-04-11
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
US3299108A (en) 1965-10-18 1967-01-17 Searle & Co 17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto
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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US3766224A (en) * 1971-06-03 1973-10-16 Sandoz Ag 15-methyl-substituted steroids
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
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
DE69418744T2 (de) 1993-03-05 1999-11-11 Akzo Nobel N.V., Arnheim/Arnhem Verwendung von Pregnanderivaten zur Behandlung von Tumoren
CA2200423C (en) 1996-03-26 2006-12-19 Sietse Mosselman Novel estrogen receptor
IL123195A (en) 1997-02-21 2002-11-10 Akzo Nobel Nv Steroid compounds with anti-pregnancy activity and against bone thinning, preparation and pharmaceutical preparations containing them
RU2225714C2 (ru) 1998-03-09 2004-03-20 Акцо Нобель Н.В. Новый набор противозачаточных средств
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DE69902684T2 (de) 1998-11-20 2003-04-24 Akzo Nobel N.V., Arnheim/Arnhem Estrogenische estra-1,3,5(10)-trien verbindungen mit verschiedenen wirkungen auf estrogenrezeptor alpha und beta mit einer unverzweigten kohlenwasserstoffkette von 5-9 kohlenstoffatomen in position 11
TW548277B (en) 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens
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EP1226155B1 (de) * 1999-11-02 2007-05-02 Bayer Schering Pharma AG 18-nor-steroide als selektiv wirksame estrogene
HRP20030060A2 (en) * 2000-07-28 2004-06-30 Akzo Nobel Nv 16alpha-methyl or ethyl substituted estrogens

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
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
AU2005281705B2 (en) 2011-03-10
EP1805201B1 (en) 2008-11-19

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