WO2004094451A3 - 8beta-vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene - Google Patents

8beta-vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene Download PDF

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Publication number
WO2004094451A3
WO2004094451A3 PCT/EP2004/004086 EP2004004086W WO2004094451A3 WO 2004094451 A3 WO2004094451 A3 WO 2004094451A3 EP 2004004086 W EP2004004086 W EP 2004004086W WO 2004094451 A3 WO2004094451 A3 WO 2004094451A3
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WO
WIPO (PCT)
Prior art keywords
dollar
trienes
estra
vinyl
substituted
Prior art date
Application number
PCT/EP2004/004086
Other languages
English (en)
French (fr)
Other versions
WO2004094451A2 (de
Inventor
Nico Braeuer
Olaf Peters
Alexander Hillisch
Rolf Bohlmann
Margit Richter
Hans Peter Muhn
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
Priority to AU2004232462A priority Critical patent/AU2004232462A1/en
Priority to EP04727876A priority patent/EP1622924A2/de
Priority to JP2006505174A priority patent/JP2006524202A/ja
Priority to YUP-2005/0793A priority patent/RS20050793A/sr
Priority to BRPI0409794-7A priority patent/BRPI0409794A/pt
Priority to EA200501568A priority patent/EA009606B1/ru
Priority to MXPA05011386A priority patent/MXPA05011386A/es
Priority to CA002522354A priority patent/CA2522354A1/en
Publication of WO2004094451A2 publication Critical patent/WO2004094451A2/de
Publication of WO2004094451A3 publication Critical patent/WO2004094451A3/de
Priority to NO20055493A priority patent/NO20055493L/no

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general

Landscapes

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

Abstract

Die vorliegende Erfindung betrifft 8β-Vinyl-11β-(w-substituierte)alkyl-estra-1,3,5(10)-triene der allgemeinen Formel (I) mit ERβ-antagonistischer Aktivität, Verfahren zu deren Herstellung, deren Zwischenprodukte, pharmazeutische Präparate enthaltend die erfindungsgemäßen Verbindungen, sowie deren Verwendung zur Herstellung von Arzneimitteln. Die neuen Verbindungen sind zur Kontrazeption beim Mann und der Frau einsetzbar, ohne daß sie andere Östrogen-sensitive Organe wie den Uterus oder die Leber beeinflußen. Sie sind auch zur Behandlung von gutartigen oder bösartigen proliferativen Erkrankungen des Ovars, wie Ovarialcarcinomen und Granulosazelltumoren geeignet.
PCT/EP2004/004086 2003-04-22 2004-04-16 8beta-vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene WO2004094451A2 (de)

Priority Applications (9)

Application Number Priority Date Filing Date Title
AU2004232462A AU2004232462A1 (en) 2003-04-22 2004-04-16 8$g(b)-vinyl-11$g(b)-($g(v)-substituted)alkyl-estra-1,3,5(10)-trienes
EP04727876A EP1622924A2 (de) 2003-04-22 2004-04-16 8beta-vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene
JP2006505174A JP2006524202A (ja) 2003-04-22 2004-04-16 ８β−ビニル−１１β（ω−置換された）アルキル−エストラ−１，３，５（１０）−トリエン
YUP-2005/0793A RS20050793A (sr) 2003-04-22 2004-04-16 8beta-vinil-11beta-(omega- supstituisani)alkil-estra-1,3,5 (10)- trieni
BRPI0409794-7A BRPI0409794A (pt) 2003-04-22 2004-04-16 8beta-vinil-11beta-(Èmega-substituìdo)alquil-estra-1 ,3,5(10)-trienos
EA200501568A EA009606B1 (ru) 2003-04-22 2004-04-16 8β-ВИНИЛ-11β-(ω-ЗАМЕЩЕННЫЕ)АЛКИЛЭСТРА-1,3,5(10)-ТРИЕНЫ
MXPA05011386A MXPA05011386A (es) 2003-04-22 2004-04-16 Alquil-estra-1, 3, 5(10)-trienos 8??-vinil- 11??(?- sustituidos.
CA002522354A CA2522354A1 (en) 2003-04-22 2004-04-16 8beta-vinyl-11beta-(alpha-substituted)alkyl-estra-1,3,5(10)-trienes
NO20055493A NO20055493L (no) 2003-04-22 2005-11-21 8β-vinyl-11β-(w-substituerte)alkyl-ostra-1,3,5(10)-triener

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10318896.7 2003-04-22
DE10318896A DE10318896A1 (de) 2003-04-22 2003-04-22 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene

Publications (2)

Publication Number Publication Date
WO2004094451A2 WO2004094451A2 (de) 2004-11-04
WO2004094451A3 true WO2004094451A3 (de) 2004-12-23

Family

ID=33304956

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/004086 WO2004094451A2 (de) 2003-04-22 2004-04-16 8beta-vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene

Country Status (21)

Country Link
US (1) US7375098B2 (de)
EP (1) EP1622924A2 (de)
JP (1) JP2006524202A (de)
KR (1) KR20060005386A (de)
CN (1) CN100381457C (de)
AR (1) AR044056A1 (de)
AU (1) AU2004232462A1 (de)
BR (1) BRPI0409794A (de)
CA (1) CA2522354A1 (de)
CL (1) CL2004000856A1 (de)
CR (1) CR8053A (de)
DE (1) DE10318896A1 (de)
EA (1) EA009606B1 (de)
EC (1) ECSP056180A (de)
MX (1) MXPA05011386A (de)
NO (1) NO20055493L (de)
PE (1) PE20050423A1 (de)
RS (1) RS20050793A (de)
UY (1) UY28284A1 (de)
WO (1) WO2004094451A2 (de)
ZA (1) ZA200509447B (de)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20023382A3 (cs) * 2000-04-12 2003-02-12 Schering Aktiengesellschaft Substituované estratrieny jako selektivně účinné estrogeny
EP1789420A2 (de) 2004-09-07 2007-05-30 Wyeth, A Corporation of the State of Delaware 6H-[1]BENZOPYRANO[4,3-b]CHINOLINE UND IHRE VERWENDUNG ALS OESTROGENE MITTEL
BRPI0606168A2 (pt) * 2005-10-05 2009-06-02 Sicor Inc separação de isÈmeros de fulvestrant

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001077138A1 (de) * 2000-04-12 2001-10-18 Schering Aktiengesellschaft 8β-SUBSTITUIERTE-11β-PENTYL-UND 11β-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
DE10151114A1 (de) * 2001-10-15 2003-04-17 Schering Ag 8ß-Substituierte-11ß-aryl-estra-2,3,5(10)-trienderivate

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1226155T3 (da) * 1999-11-02 2007-09-10 Bayer Schering Pharma Ag 18-nor-steroider som selektivt virksomme östrogener

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001077138A1 (de) * 2000-04-12 2001-10-18 Schering Aktiengesellschaft 8β-SUBSTITUIERTE-11β-PENTYL-UND 11β-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
DE10151114A1 (de) * 2001-10-15 2003-04-17 Schering Ag 8ß-Substituierte-11ß-aryl-estra-2,3,5(10)-trienderivate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LOBACCARO C ET AL: "Steroidal Affinity Labels of the Estrogen Receptor. 3. Estradiol 11.beta.-n-Alkyl Derivatives Bearing a Terminal Electrophilic Group: Anti-estrogenic and Cytotoxic Properties", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 40, no. 14, 4 July 1997 (1997-07-04), pages 2217 - 2227, XP002100729, ISSN: 0022-2623 *

Also Published As

Publication number Publication date
ZA200509447B (en) 2009-08-26
BRPI0409794A (pt) 2006-05-30
ECSP056180A (es) 2006-04-19
US7375098B2 (en) 2008-05-20
UY28284A1 (es) 2004-11-30
AR044056A1 (es) 2005-08-24
EP1622924A2 (de) 2006-02-08
MXPA05011386A (es) 2006-04-18
WO2004094451A2 (de) 2004-11-04
KR20060005386A (ko) 2006-01-17
CL2004000856A1 (es) 2005-03-28
CN1777618A (zh) 2006-05-24
AU2004232462A1 (en) 2004-11-04
CN100381457C (zh) 2008-04-16
CR8053A (es) 2006-05-29
NO20055493D0 (no) 2005-11-21
US20050065135A1 (en) 2005-03-24
EA009606B1 (ru) 2008-02-28
PE20050423A1 (es) 2005-08-13
JP2006524202A (ja) 2006-10-26
CA2522354A1 (en) 2004-11-04
NO20055493L (no) 2006-01-18
RS20050793A (sr) 2008-04-04
EA200501568A1 (ru) 2006-06-30
DE10318896A1 (de) 2004-11-25

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