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)
  • 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)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (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
US608501P 2004-09-08
EP04104334 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 (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
JP5749261B2 (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 ３，３，５，５−テトラメチルシクロヘキサノンを調製する方法
JP5738854B2 (ja) * 2009-06-29 2015-06-24 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
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
EP2764008B1 (en) * 2011-10-07 2016-08-17 Estetra S.P.R.L. Process for the production of estetrol
WO2014207311A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1
US10377791B2 (en) 2013-06-25 2019-08-13 Forendo Pharma Ltd. Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1
KR20160042873A (ko) 2013-06-25 2016-04-20 포렌도 파마 리미티드 17.베타.-하이드록시스테로이드 탈수소효소의 억제제로서 치료적 활성 17-질소 치환된 에스트라트리엔티아졸 유도체
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
US10626140B2 (en) 2014-12-23 2020-04-21 Forendo Pharma Ltd Prodrugs of 17β-HSD1-inhibitors
MD3310333T2 (ro) 2015-06-18 2020-06-30 Estetra Sprl Unitate de dozare orodispersabilă care conține un component estetrol
CN116077454A (zh) 2015-06-18 2023-05-09 埃斯特拉有限责任公司 含雌四醇组分的口腔分散剂量单位
RS61777B1 (sr) 2015-06-18 2021-06-30 Estetra Sprl Oralno-disperzibilna tableta koja sadrži estetrol
HUE054589T2 (hu) 2015-06-18 2021-09-28 Estetra Sprl Szájban diszpergálódó esztetrol tartalmú tabletta
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
FI3634975T3 (fi) 2017-06-08 2024-05-03 Organon R&D Finland Ltd 15-beeta-[3-propanamido]substituoitujen estra-1,3,5(10)-trien-17-onien 17-oksiimeja käytettäväksi 17-beeta-hydroksisteroididehydrogenaasien inhiboimisessa
DK3781171T3 (da) 2018-04-19 2022-05-02 Estetra Srl Sammensætninger og deres anvendelser til lindring af menopause-associerede symptomer
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
BR112021010598A2 (pt) 2018-12-05 2021-08-24 Forendo Pharma Ltd Compostos, método para preparação de um composto e composição farmacêutica
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 (https=) 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
GB1112840A (en) 1964-04-07 1968-05-08 Res Inst Medicine Chem Steroids having pro-oestrogenic activity
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
ES2134313T3 (es) 1993-03-05 1999-10-01 Akzo Nobel Nv Utilizacion de derivados de pregnano para el tratamiento de tumores.
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
WO1999045886A2 (en) 1998-03-09 1999-09-16 Akzo Nobel N.V. New contraceptive kit for monotherapy
NZ508299A (en) 1998-06-19 2003-04-29 Akzo Nobel Nv Testosterone derivative
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
US6677329B1 (en) 1999-09-06 2004-01-13 Akzo Nobel N V. Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11
DE50014299D1 (de) * 1999-11-02 2007-06-14 Bayer Schering Pharma Ag 18-nor-steroide als selektiv wirksame estrogene
AU8201601A (en) * 2000-07-28 2002-02-13 Akzo Nobel Nv 16alpha-methyl or ethyl substituted estrogens

Also Published As

Publication number Publication date
US7838516B2 (en) 2010-11-23
UA89964C2 (ru) 2010-03-25
JP2008512426A (ja) 2008-04-24
DK1805201T3 (da) 2009-01-12
PL1805201T3 (pl) 2009-04-30
TW200621795A (en) 2006-07-01
US20070254860A1 (en) 2007-11-01
EP1805201B1 (en) 2008-11-19
RS51640B (sr) 2011-10-31
RU2386637C2 (ru) 2010-04-20
WO2006027347A1 (en) 2006-03-16
EP1805201A1 (en) 2007-07-11
PE20060590A1 (es) 2006-07-14
AR050732A1 (es) 2006-11-15
ATE414710T1 (de) 2008-12-15
SI1805201T1 (sl) 2009-04-30
AU2005281705B2 (en) 2011-03-10
PT1805201E (pt) 2008-12-31
RS20070075A (sr) 2008-09-29
CA2577497C (en) 2012-03-20
BRPI0514976A (pt) 2008-07-01
RU2007112939A (ru) 2008-11-10
NZ553266A (en) 2009-06-26
JP4889644B2 (ja) 2012-03-07
CA2577497A1 (en) 2006-03-16
AU2005281705A1 (en) 2006-03-16

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