AR050732A1 - 15 beta-sustituidos esteroides con actividad estrogenica selectiva - Google Patents

15 beta-sustituidos esteroides con actividad estrogenica selectiva

Info

Publication number
AR050732A1
AR050732A1 ARP050103745A ARP050103745A AR050732A1 AR 050732 A1 AR050732 A1 AR 050732A1 AR P050103745 A ARP050103745 A AR P050103745A AR P050103745 A ARP050103745 A AR P050103745A AR 050732 A1 AR050732 A1 AR 050732A1
Authority
AR
Argentina
Prior art keywords
alkyl
beta
selective
activity
strogen
Prior art date
Application number
ARP050103745A
Other languages
English (en)
Inventor
Hubert Jan Jozef Loozen
Antonius Gerardus Hen Ederveen
Fredericus Antonius Dijcks
Original Assignee
Akso Nobel N V
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 Akso Nobel N V filed Critical Akso Nobel N V
Publication of AR050732A1 publication Critical patent/AR050732A1/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)
  • 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)

Abstract

La presente proporciona compuestos esteroidales 15b-substituidos con actividad selectiva del receptor de estrogenos. Reivindicacion 1: Un compuesto esteroidal 15beta-sustituido de formula (1) caracterizado porque: R1 es H, C1-5 alquil, C1-12 acil, di-(C1-5 alquil)aminocarbonil, (C1-5 alquil)oxicarbonil o sulfamoil; R2 es H, C1-3 alquil, C2-3 alquenil o C2-3 alquinil, cada uno de los cuales se puede sustituir opcionalmente con un halogeno; R3 es C1-2 alquil, etenil o etinil, cada uno de los cuales se puede sustituir opcionalmente con un halogeno, y R4 es H o C1-12 acil.
ARP050103745A 2004-09-08 2005-09-08 15 beta-sustituidos esteroides con actividad estrogenica selectiva AR050732A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR050732A1 true AR050732A1 (es) 2006-11-15

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050103745A AR050732A1 (es) 2004-09-08 2005-09-08 15 beta-sustituidos esteroides con actividad estrogenica selectiva

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
US20120116125A1 (en) * 2009-06-29 2012-05-10 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
SI2448910T1 (sl) * 2009-06-29 2013-07-31 Merz Pharma Gmbh & Co. Kgaa Postopek za pripravo nerameksana
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
SG11201401282PA (en) * 2011-10-07 2014-05-29 Estetra Sprl Process for the production of estetrol
CN105518017B (zh) 2013-06-25 2020-07-14 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
US9663549B2 (en) 2013-06-25 2017-05-30 Forendo Pharma Ltd. Therapeutically active 17-nitrogen substituted estratreinthiazole derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase
JP6461127B2 (ja) 2013-06-25 2019-01-30 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脱水素酵素、タイプＩの阻害剤としての治療活性エストラトリエンチアゾール誘導体
WO2016102776A1 (en) 2014-12-23 2016-06-30 Forendo Pharma Ltd Prodrugs of 17.beta.-hsd1 -inhibitors
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
UA123098C2 (uk) 2015-06-18 2021-02-17 Естетра Спрл Диспергована у порожнині рота одиниця дозування, що містить естетрольний компонент
US10894014B2 (en) 2015-06-18 2021-01-19 Estetra Sprl Orodispersible tablet containing Estetrol
SI3310346T1 (sl) 2015-06-18 2021-07-30 Estetra Sprl Orodisperzibilna tableta, ki vsebuje estetrol
PE20231714A1 (es) 2015-06-18 2023-10-23 Estetra Sprl Unidad de dosificacion orodispersable que contiene un componente estetrol
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
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
EP3891167A1 (en) 2018-12-05 2021-10-13 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

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Also Published As

Publication number Publication date
US7838516B2 (en) 2010-11-23
WO2006027347A1 (en) 2006-03-16
SI1805201T1 (sl) 2009-04-30
RU2386637C2 (ru) 2010-04-20
AU2005281705A1 (en) 2006-03-16
CA2577497C (en) 2012-03-20
RS20070075A (en) 2008-09-29
EP1805201B1 (en) 2008-11-19
RU2007112939A (ru) 2008-11-10
JP4889644B2 (ja) 2012-03-07
ES2317312T3 (es) 2009-04-16
JP2008512426A (ja) 2008-04-24
TW200621795A (en) 2006-07-01
US20070254860A1 (en) 2007-11-01
PL1805201T3 (pl) 2009-04-30
UA89964C2 (ru) 2010-03-25
EP1805201A1 (en) 2007-07-11
NZ553266A (en) 2009-06-26
DK1805201T3 (da) 2009-01-12
CA2577497A1 (en) 2006-03-16
BRPI0514976A (pt) 2008-07-01
AU2005281705B2 (en) 2011-03-10
ATE414710T1 (de) 2008-12-15
PT1805201E (pt) 2008-12-31
RS51640B (en) 2011-10-31
PE20060590A1 (es) 2006-07-14

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