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WO2006003013A3 - NEUE 2-SUBSTITUIERTE ESTRA-1,3,5(10)-TRIEN-17-ONE ALS INHIBITOREN DER 17β-HYDROXYSTEROIDDEHYDROGENASE TYP 1 - Google Patents

NEUE 2-SUBSTITUIERTE ESTRA-1,3,5(10)-TRIEN-17-ONE ALS INHIBITOREN DER 17β-HYDROXYSTEROIDDEHYDROGENASE TYP 1 Download PDF

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Publication number
WO2006003013A3
WO2006003013A3 PCT/EP2005/007315 EP2005007315W WO2006003013A3 WO 2006003013 A3 WO2006003013 A3 WO 2006003013A3 EP 2005007315 W EP2005007315 W EP 2005007315W WO 2006003013 A3 WO2006003013 A3 WO 2006003013A3
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WO
WIPO (PCT)
Prior art keywords
atom
group
rest
oxygen
hydroxysteroiddehydrogenase
Prior art date
Application number
PCT/EP2005/007315
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English (en)
French (fr)
Other versions
WO2006003013A2 (de
WO2006003013B1 (de
Inventor
Alexander Hillisch
Wilko Regenhardt
Christian Gege
Olaf Peters
Ulrich Bothe
Jerzy Adamski
Gabriele Moeller
Andrea Rosinus
Walter Elger
Birgitt Schneider
Original Assignee
Schering Ag
Alexander Hillisch
Wilko Regenhardt
Christian Gege
Olaf Peters
Ulrich Bothe
Jerzy Adamski
Gabriele Moeller
Andrea Rosinus
Walter Elger
Birgitt Schneider
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 Schering Ag, Alexander Hillisch, Wilko Regenhardt, Christian Gege, Olaf Peters, Ulrich Bothe, Jerzy Adamski, Gabriele Moeller, Andrea Rosinus, Walter Elger, Birgitt Schneider filed Critical Schering Ag
Priority to JP2007518558A priority Critical patent/JP2008504338A/ja
Priority to EP05767936A priority patent/EP1771461A2/de
Publication of WO2006003013A2 publication Critical patent/WO2006003013A2/de
Publication of WO2006003013A3 publication Critical patent/WO2006003013A3/de
Publication of WO2006003013B1 publication Critical patent/WO2006003013B1/de

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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
    • A61P5/32—Antioestrogens
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals

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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Die Erfindung betrifft neue 2-substituierte Estra-1,3,5(10)-trien-17-one der allgemeinen Formel (I), worin R2 eine gesättigte oder ungesättigte C1-C8-Alkylgruppe, eine C1-C5-Alkyloxygruppe, ein Aralkyl- oder Alkylarylrest, ein Rest -O-CnFmHo, wobei n = 1,2,3,4,5 oder 6, m≥1 und m = 2n+1 ist, oder eine Gruppe CH2XY, in der X für ein Sauerstoffatom und Y für einen Alkylrest mit 1 bis 4 Kohlenstoffatomen steht, sowie ein Halogenatom oder eine Nitrilgruppe, R13 ein Wasserstoffatom oder eine Methylgruppe, R16 ein Wasserstoff- oder ein Fluoratom, Z ein Sauerstoff- oder ein Schwefelatom R3 und R5 jeweils unabhängig voneinander ein α- oder β-ständiges Wasserstoffatom, R4 und R6 jeweils unabhängig voneinander ein α- oder β-ständiges Wasserstoffatom, eine C1-C5-Alkyl-, eine C1-C5-Alkyloxy-, eine C1-C5-Acyl- oder eine Hydroxygruppe oder ein Aralkyl- oder Alkylarylrest, R3 und R4 zusammen ein Sauerstoffatom, R5 und R6 zusammen ein Sauerstoffatom, R7 und R8 jeweils ein Wasserstoffatom oder zusammen eine CH2-Gruppe bedeuten, sowie ihre pharmazeutisch annehmbaren Salze, deren Herstellung und Verwendung als Arzneimittel zur Prophylaxe und Therapie estrogen-abhängiger Erkrankungen, die sich durch Hemmung der 17β-Hydroxysteroiddehydro-genase Typ 1 beeinflussen lassen.
PCT/EP2005/007315 2004-07-02 2005-07-04 NEUE 2-SUBSTITUIERTE ESTRA-1,3,5(10)-TRIEN-17-ONE ALS INHIBITOREN DER 17β-HYDROXYSTEROIDDEHYDROGENASE TYP 1 WO2006003013A2 (de)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2007518558A JP2008504338A (ja) 2004-07-02 2005-07-04 １７β−ヒドロキシステロイドデヒドロゲナーゼタイプ１のインヒビターとしての新規２−置換されたエストラ−１，３，５（１０）−トリエン−１７−オン
EP05767936A EP1771461A2 (de) 2004-07-02 2005-07-04 Neue 2-substituierte estra-1,3,5(10)-trien-17-one als inhibitoren der 17beta-hydroxy-steroiddehydrogenase typ 1

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004032674A DE102004032674A1 (de) 2004-07-02 2004-07-02 Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1
DE102004032674.6 2004-07-02

Publications (3)

Publication Number Publication Date
WO2006003013A2 WO2006003013A2 (de) 2006-01-12
WO2006003013A3 true WO2006003013A3 (de) 2006-06-22
WO2006003013B1 WO2006003013B1 (de) 2006-08-31

Family

ID=35207898

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PCT/EP2005/007315 WO2006003013A2 (de) 2004-07-02 2005-07-04 NEUE 2-SUBSTITUIERTE ESTRA-1,3,5(10)-TRIEN-17-ONE ALS INHIBITOREN DER 17β-HYDROXYSTEROIDDEHYDROGENASE TYP 1

Country Status (4)

Country Link
EP (1) EP1771461A2 (de)
JP (1) JP2008504338A (de)
DE (1) DE102004032674A1 (de)
WO (1) WO2006003013A2 (de)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102004032673A1 (de) * 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1
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
CN105518015B (zh) 2013-06-25 2017-09-15 佛恩多制药有限公司 治疗活性的作为17β‑羟基类固醇脱氢酶抑制剂的17‑氮取代雌三烯噻唑衍生物
AR096728A1 (es) 2013-06-25 2016-01-27 Forendo Pharma Ltd Derivados de estratrieno-tiazol terapéuticamente activos
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
EP3237431B1 (de) 2014-12-23 2019-03-20 Forendo Pharma Ltd Prodrugs von 17.beta.-hsd1-inhibitoren
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
CZ307437B6 (cs) 2016-06-07 2018-08-22 Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz
PT3634975T (pt) 2017-06-08 2024-05-20 Organon R&D Finland Ltd 17-oximas de estra-1,3,5(10)-trien-17-onas 15.beta.-[3- propanamido]-substituídas para utilização na inibição de 17.beta.-hidroxiesteroide desidrogenases
CN113412269A (zh) 2018-12-05 2021-09-17 佛恩多制药有限公司 作为17-hsd1抑制剂的在位置16(17)具有缩合的吡唑环的雌甾-1,3,5(10)-三烯化合物

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Also Published As

Publication number Publication date
WO2006003013A2 (de) 2006-01-12
DE102004032674A1 (de) 2006-01-26
EP1771461A2 (de) 2007-04-11
WO2006003013B1 (de) 2006-08-31
JP2008504338A (ja) 2008-02-14

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