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PE20060590A1 - COMPUESTOS ESTEROIDALES 15ß-SUSTITUIDOS CON ACTIVIDAD SELECTIVA DEL RECEPTOR DE ESTROGENOS - Google Patents

COMPUESTOS ESTEROIDALES 15ß-SUSTITUIDOS CON ACTIVIDAD SELECTIVA DEL RECEPTOR DE ESTROGENOS

Info

Publication number
PE20060590A1
PE20060590A1 PE2005001026A PE2005001026A PE20060590A1 PE 20060590 A1 PE20060590 A1 PE 20060590A1 PE 2005001026 A PE2005001026 A PE 2005001026A PE 2005001026 A PE2005001026 A PE 2005001026A PE 20060590 A1 PE20060590 A1 PE 20060590A1
Authority
PE
Peru
Prior art keywords
alkyl
estrogen receptor
15beta
substituted steroidal
steroidal compounds
Prior art date
Application number
PE2005001026A
Other languages
English (en)
Inventor
Hubert Jan Jozef Loozen
Antonius Gerardus Hendrikus Ederveen
Fredericus Antonius Dijcks
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
Publication of PE20060590A1 publication Critical patent/PE20060590A1/es

Links

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)
  • Orthopedic Medicine & Surgery (AREA)
  • Reproductive Health (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)

Abstract

SE REFIERE A UN COMPUESTO ESTEROIDAL 15BETA-SUSTIUTIDO DE FORMULA I, DONDE R1 ES H, ALQUILO C1-C5, ACILO C1-C12, OXICARBONIL- (ALQUILO C1-C5), ENTRE OTROS; R2 ES H, ALQUILO C1-C3, ALQUENIL C2-C3, ALQUINIL C2-C3, ENTRE OTROS; R3 ES ALQUILO C1-C2, ETENIL O ETINIL OPCIONALMENTE SUSTITUIDOS POR HALOGENO; R4 ES H, ACILO C1-C12. SON COMPUESTOS PREFERIDOS: 7ALFA-ETIL-15BETA-METIL-19-NOR-17ALFA-PREGNA-1.3.5(10)-TRIEN-20-INE-3.17BETA-DIOL; 3-PIVALOILOXI-7ALFA-ETIL-15BETA-METIL-19-NOR-17ALFA-PREGNA-1.3.5(10)-TRIEN-20-INE-17BETA-OL. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS POSEEN NIVELES DE SELECTIVIDAD FUNCIONAL PARA EL ALFA-SUBTIPO DEL RECEPTOR DE ESTROGENOS UTILES EN EL TRATAMIENTO DE LA ANTICONCEPCION
PE2005001026A 2004-09-08 2005-09-06 COMPUESTOS ESTEROIDALES 15ß-SUSTITUIDOS CON ACTIVIDAD SELECTIVA DEL RECEPTOR DE ESTROGENOS PE20060590A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20060590A1 true PE20060590A1 (es) 2006-07-14

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001026A PE20060590A1 (es) 2004-09-08 2005-09-06 COMPUESTOS ESTEROIDALES 15ß-SUSTITUIDOS CON ACTIVIDAD SELECTIVA DEL RECEPTOR DE ESTROGENOS

Country Status (20)

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

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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
PL2448910T3 (pl) * 2009-06-29 2013-10-31 Merz Pharma Gmbh & Co Kgaa Sposób wytwarzania nerameksanu
ES2446365T3 (es) * 2009-06-29 2014-03-07 Merz Pharma Gmbh & Co. Kgaa Procedimiento de preparación de neramexane
EP2448901A1 (en) * 2009-06-29 2012-05-09 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
PT2764008T (pt) * 2011-10-07 2016-11-10 Estetra Sprl Processo para a produção de estetrol
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
TW201522359A (zh) 2013-06-25 2015-06-16 Forendo Pharma Ltd 治療用活性雌三烯噻唑衍生物
CN105518016B (zh) 2013-06-25 2020-10-23 佛恩多制药有限公司 治疗活性的作为1型17β-羟基类固醇脱氢酶抑制剂的雌三烯噻唑衍生物
WO2016102775A1 (en) 2014-12-23 2016-06-30 Forendo Pharma Ltd PRODRUGS OF 17β-HSD1 -INHIBITORS
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
SMT202200102T1 (it) 2015-06-18 2022-05-12 Estetra Srl Unità di dosaggio orodispersibile contenente un componente di estetrolo
DK3106148T3 (en) 2015-06-18 2018-05-07 Mithra Pharmaceuticals S A Orodispersible dosing unit containing an estetrol component
JP6813150B2 (ja) 2015-06-18 2021-01-13 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
SI3310345T1 (sl) 2015-06-18 2021-05-31 Estetra Sprl Orodisperzibilna tableta, ki vsebuje estetrol
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
IL294140B2 (en) 2017-06-08 2024-09-01 Forendo Pharma Ltd 15beta-(3-PROPANAMIDO)-SUBSTITUTED ESTRA-1,3,5(10)-TRIEN-17-OXIMES FOR USE IN INHIBITION OF 17beta-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
JOP20200260A1 (ar) 2018-04-19 2019-10-19 Estetra Sprl مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث
AU2019393005B2 (en) 2018-12-05 2022-12-15 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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Also Published As

Publication number Publication date
ES2317312T3 (es) 2009-04-16
NZ553266A (en) 2009-06-26
UA89964C2 (ru) 2010-03-25
DK1805201T3 (da) 2009-01-12
AR050732A1 (es) 2006-11-15
RS51640B (sr) 2011-10-31
CA2577497A1 (en) 2006-03-16
TW200621795A (en) 2006-07-01
ATE414710T1 (de) 2008-12-15
EP1805201B1 (en) 2008-11-19
WO2006027347A1 (en) 2006-03-16
RU2386637C2 (ru) 2010-04-20
US20070254860A1 (en) 2007-11-01
AU2005281705B2 (en) 2011-03-10
PT1805201E (pt) 2008-12-31
CA2577497C (en) 2012-03-20
PL1805201T3 (pl) 2009-04-30
RU2007112939A (ru) 2008-11-10
JP4889644B2 (ja) 2012-03-07
JP2008512426A (ja) 2008-04-24
EP1805201A1 (en) 2007-07-11
US7838516B2 (en) 2010-11-23
BRPI0514976A (pt) 2008-07-01
AU2005281705A1 (en) 2006-03-16
RS20070075A (sr) 2008-09-29
SI1805201T1 (sl) 2009-04-30

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