BRPI0511394A - d-homo-estra-1,3,5(10)-trienos 2-substituìdos como inibidores de 17-hidróxi esteróide desidrogenase tipo 1 - Google Patents

d-homo-estra-1,3,5(10)-trienos 2-substituìdos como inibidores de 17-hidróxi esteróide desidrogenase tipo 1

Info

Publication number
BRPI0511394A
BRPI0511394A BRPI0511394-6A BRPI0511394A BRPI0511394A BR PI0511394 A BRPI0511394 A BR PI0511394A BR PI0511394 A BRPI0511394 A BR PI0511394A BR PI0511394 A BRPI0511394 A BR PI0511394A
Authority
BR
Brazil
Prior art keywords
sub
sup
trienes
estra
homo
Prior art date
Application number
BRPI0511394-6A
Other languages
English (en)
Inventor
Christian Gege
Wilko Regenhardt
Olaf Peters
Alexander Hillisch
Jerzy Adamski
Gabriele Moeler
Dominga Deluca
Walter Elger
Birgitt Schneider
Original Assignee
Schering Ag
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 filed Critical Schering Ag
Publication of BRPI0511394A publication Critical patent/BRPI0511394A/pt

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

D-HOMO-ESTRA-1,3,5(10)-TRIENOS 2-SUBSTITUìDOS COMO INIBIDORES DE I7B-HIDRóXI ESTERóIDE DESIDROGENASE TIPO 1. A invenção se refere a novos D-homo-estra-1 ,3,5(10)-trienos 2-substituídos de fórmula geral (I) em que R¬ 2¬ representa um grupo C~ 1~-C~ 8~ alquil, C~ 1~-C~ 8~ alquiloxi ou um átomo de halogênio, R¬ 13¬ representa um átomo de hidrogênio ou um grupo metil, e R¬ 17¬ representa um átomo de hidrogênio ou um átomo de flúor. A invenção também se refere a sais farmaceuticamente aceitáveis dos ditos compostos, a produção desses e ao uso dos mesmos como medicamentos para a profilaxia e tratamento de doenças dependentes de estrogênio, que podem ser influenciadas pela inibição de 17<225>-hidróxi esteróide desidrogenase tipo 1.
BRPI0511394-6A 2004-07-02 2005-07-04 d-homo-estra-1,3,5(10)-trienos 2-substituìdos como inibidores de 17-hidróxi esteróide desidrogenase tipo 1 BRPI0511394A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004032673A DE102004032673A1 (de) 2004-07-02 2004-07-02 Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1
PCT/EP2005/007314 WO2006003012A1 (de) 2004-07-02 2005-07-04 NEUE 2-SUBSTITUIERTE D-HOMO ESTRA-1,3,5(10)-TRIENE ALS INHIBITOREN DER 17ß-HYDROXYSTEROIDDEHYDROGENASE TYP 1

Publications (1)

Publication Number Publication Date
BRPI0511394A true BRPI0511394A (pt) 2007-12-04

Family

ID=35106828

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0511394-6A BRPI0511394A (pt) 2004-07-02 2005-07-04 d-homo-estra-1,3,5(10)-trienos 2-substituìdos como inibidores de 17-hidróxi esteróide desidrogenase tipo 1

Country Status (25)

Country Link
EP (1) EP1763534B1 (pt)
JP (1) JP4871274B2 (pt)
KR (1) KR20070035059A (pt)
CN (1) CN1980949B (pt)
AT (1) ATE458744T1 (pt)
AU (1) AU2005259329B8 (pt)
BR (1) BRPI0511394A (pt)
CA (1) CA2571760C (pt)
CR (1) CR8854A (pt)
DE (2) DE102004032673A1 (pt)
DK (1) DK1763534T3 (pt)
EA (1) EA011455B1 (pt)
EC (1) ECSP077160A (pt)
ES (1) ES2340401T3 (pt)
HK (1) HK1103745A1 (pt)
HR (1) HRP20100230T1 (pt)
IL (1) IL180171A0 (pt)
MX (1) MX2007000108A (pt)
NO (1) NO20070605L (pt)
NZ (1) NZ552515A (pt)
PL (1) PL1763534T3 (pt)
PT (1) PT1763534E (pt)
UA (1) UA92324C2 (pt)
WO (1) WO2006003012A1 (pt)
ZA (1) ZA200700958B (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE102007015169A1 (de) 2007-03-27 2008-10-02 Universität des Saarlandes Campus Saarbrücken 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
DE102007040243A1 (de) 2007-08-25 2009-02-26 Universität des Saarlandes 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
US9850272B2 (en) 2013-06-25 2017-12-26 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
US9663549B2 (en) 2013-06-25 2017-05-30 Forendo Pharma Ltd. Therapeutically active 17-nitrogen substituted estratreinthiazole derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase
CN107207562B (zh) 2014-12-23 2020-03-06 佛恩多制药有限公司 17β-HSD1抑制剂的前药
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
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
UA126342C2 (uk) 2017-06-08 2022-09-21 Форендо Фарма Лтд 15-бета-[3-пропанамідо]-заміщені естра-1,3,5(10)-трієн-17-он-сполуки і їх 17-оксими для використання в інгібуванні 17-бета-гідроксистероїддегідрогеназ
SG11202105795XA (en) 2018-12-05 2021-06-29 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3005835A (en) * 1960-09-13 1961-10-24 Searle & Co D-homo-18-norestra-1, 3, 5(10)-trien-17alpha-ones and intermediates thereto
GB1346691A (en) * 1970-06-12 1974-02-13 Inst Khim Prirodnykh Soedineny Stereospecific method for preparing estrane compounds of natural configuration
JPH06279488A (ja) * 1993-03-29 1994-10-04 Kuraray Co Ltd 新規なステロイド誘導体および骨粗鬆症治療剤
PL343862A1 (en) * 1998-03-11 2001-09-10 Endorech Inhibitors of type 5 and type 3 17β−hydroxysteroid dehydrogenase and methods for their use
DE10151365A1 (de) * 2001-10-17 2003-04-30 Schering Ag 17-Chlor-D-Homosteroide als selektive Estrogenrezeptorantagonisten
WO2003017974A1 (en) * 2001-08-31 2003-03-06 Pantarhei Bioscience B.V. Method of treating benign gynaecological disorders and a pharmaceutical kit for use in such method
DE10307103A1 (de) * 2003-02-19 2004-09-09 Schering Ag Antitumor wirksame 2-substituierte D-Homostra-1,3,5(10)-trien-3-yl sulfamate
DE102004032674A1 (de) * 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1

Also Published As

Publication number Publication date
ES2340401T3 (es) 2010-06-02
CA2571760A1 (en) 2006-01-12
AU2005259329B8 (en) 2011-11-24
AU2005259329A1 (en) 2006-01-12
MX2007000108A (es) 2007-03-09
DK1763534T3 (da) 2010-05-17
CN1980949B (zh) 2010-05-05
PT1763534E (pt) 2010-04-27
EP1763534B1 (de) 2010-02-24
ZA200700958B (en) 2008-07-30
CN1980949A (zh) 2007-06-13
EP1763534A1 (de) 2007-03-21
WO2006003012A1 (de) 2006-01-12
KR20070035059A (ko) 2007-03-29
PL1763534T3 (pl) 2010-07-30
CR8854A (es) 2007-08-28
HRP20100230T1 (hr) 2010-06-30
UA92324C2 (en) 2010-10-25
ATE458744T1 (de) 2010-03-15
DE102004032673A1 (de) 2006-01-26
JP2008504337A (ja) 2008-02-14
JP4871274B2 (ja) 2012-02-08
IL180171A0 (en) 2007-06-03
EA200700103A1 (ru) 2007-08-31
CA2571760C (en) 2011-11-22
EA011455B1 (ru) 2009-04-28
NO20070605L (no) 2007-02-01
NZ552515A (en) 2010-07-30
HK1103745A1 (en) 2007-12-28
DE502005009091D1 (de) 2010-04-08
AU2005259329B2 (en) 2011-11-10
ECSP077160A (es) 2007-02-28

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AO NAO RECOLHIMENTO DA 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2204 DE 02/04/2013.