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WO2008152112A3 - 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL - Google Patents

17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL Download PDF

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Publication number
WO2008152112A3
WO2008152112A3 PCT/EP2008/057427 EP2008057427W WO2008152112A3 WO 2008152112 A3 WO2008152112 A3 WO 2008152112A3 EP 2008057427 W EP2008057427 W EP 2008057427W WO 2008152112 A3 WO2008152112 A3 WO 2008152112A3
Authority
WO
WIPO (PCT)
Prior art keywords
hydrogen
derivative
group
together form
androst
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2008/057427
Other languages
English (en)
French (fr)
Other versions
WO2008152112A2 (de
Inventor
Joachim Kuhnke
Jan Huebner
Rolf Bohlmann
Thomas Frenzel
Ulrich Klar
Frederik Menges
Sven Ring
Steffen Borden
Hans-Peter Muhn
Katja Prelle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Bayer Schering Pharma 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
Priority to EP08760962A priority Critical patent/EP2167525A2/de
Priority to JP2010511650A priority patent/JP2010529174A/ja
Priority to US12/664,099 priority patent/US20100292184A1/en
Priority to CA 2692997 priority patent/CA2692997A1/en
Priority to BRPI0812535A priority patent/BRPI0812535A2/pt
Priority to CN200880020030A priority patent/CN101679479A/zh
Priority to AU2008263857A priority patent/AU2008263857A1/en
Priority to MX2009013631A priority patent/MX2009013631A/es
Application filed by Bayer Schering Pharma AG filed Critical Bayer Schering Pharma AG
Publication of WO2008152112A2 publication Critical patent/WO2008152112A2/de
Publication of WO2008152112A3 publication Critical patent/WO2008152112A3/de
Priority to IL202325A priority patent/IL202325A0/en
Anticipated expiration legal-status Critical
Priority to ZA2010/00186A priority patent/ZA201000186B/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61P15/12—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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P5/34—Gestagens
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • 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
    • C07J53/007—3 membered carbocyclic rings in position 6-7
    • 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
    • C07J53/008—3 membered carbocyclic rings in position 15/16

Landscapes

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

Abstract

Die 17ß-Cyano-19-androst-4-en-Derivate der vorliegenden Erfindung besitzen gestagene Wirksamkeit. Sie haben die allgemeine chemische Formel (1), in der Z ausgewählt ist aus der Gruppe, umfassend O, zwei Wasserstoffatome, NOR und NNHSO2R, worin R Wasserstoff oder C1-C4-Alkyl ist, R1, R2 unabhängig voneinander Wasserstoff oder Methyl sind oder R1 und R2 gemeinsam Methylen bilden oder unter Bildung einer Doppelbindung zwischen C1 und C2 entfallen, R4 Wasserstoff oder Halogen ist, ferner entweder: R6a, R6b gemeinsam Methylen oder 1,2-Ethandiyl bilden oder R6a Wasserstoff und R6b aus der Gruppe ausgewählt ist, umfassend Wasserstoff, Methyl und Hydroxymethylen, und R7 ausgewählt ist aus der Gruppe, umfassend Wasserstoff, C1-C4-Alkyl, C2-C3-Alkenyl und Cyclopropyl, oder: R6a Wasserstoff und R6b und R7 gemeinsam Methylen bilden oder unter Bildung einer Doppelbindung zwischen C6 und C7 entfallen oder R6a Methyl ist und R6b und R7 unter Bildung einer Doppelbindung zwischen C6 und C7 entfallen, R15, R16 Wasserstoff sind oder gemeinsam Methylen bilden, R17 ausgewählt ist aus der Gruppe, umfassend Wasserstoff, C1-C4-Alkyl und AIIyI, und umfassen außerdem deren Solvate, Hydrate, Stereoisomere, Diastereomere, Enantiomere und Salze, mit der Maßgabe, dass bestimmte Verbindungen ausgenommen sind.
PCT/EP2008/057427 2007-06-12 2008-06-12 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL Ceased WO2008152112A2 (de)

Priority Applications (10)

Application Number Priority Date Filing Date Title
AU2008263857A AU2008263857A1 (en) 2007-06-12 2008-06-12 17beta-cyano-19-androst-4-ene derivative, use thereof and medicaments containing said derivative
US12/664,099 US20100292184A1 (en) 2007-06-12 2008-06-12 17beta-cyano-19-androst-4-ene derivative, its use and medicaments comprising the derivative
CA 2692997 CA2692997A1 (en) 2007-06-12 2008-06-12 17.beta.-cyano-19-androst-4-ene derivative, its use and medicaments comprising the derivative
BRPI0812535A BRPI0812535A2 (pt) 2007-06-12 2008-06-12 derivado de 17beta-ciano-19-androst-4-eno, seu uso e medicamentos compreendendo o derivado
CN200880020030A CN101679479A (zh) 2007-06-12 2008-06-12 17β-氰基-19-雄甾-4-烯衍生物、其用途以及含有该衍生物的药物
EP08760962A EP2167525A2 (de) 2007-06-12 2008-06-12 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL
JP2010511650A JP2010529174A (ja) 2007-06-12 2008-06-12 １７β−シアノ−１９−アンドロスト−４−エン誘導体、その使用、及び前記誘導体を含んで成る薬剤
MX2009013631A MX2009013631A (es) 2007-06-12 2008-06-12 DERIVADO DE 17ß-CIANO-19-ANDROST-4-ENO, SU USO Y MEDICAMENTOS QUE COMPRENDEN AL DERIVADO.
IL202325A IL202325A0 (en) 2007-06-12 2009-11-25 17??-cyano-19-androst-4-ene derivative, use thereof and medicaments containing said derivative
ZA2010/00186A ZA201000186B (en) 2007-06-12 2010-01-11 17b-cyano-19-androst-4-ene derivative,use thereof and medicaments containing said derivative

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE102007027635A DE102007027635A1 (de) 2007-06-12 2007-06-12 17ß-Cyano-19-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel
DE102007027635.6 2007-06-12
US94365107P 2007-06-13 2007-06-13
US60/943,651 2007-06-13

Publications (2)

Publication Number Publication Date
WO2008152112A2 WO2008152112A2 (de) 2008-12-18
WO2008152112A3 true WO2008152112A3 (de) 2009-04-30

Family

ID=39986162

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/057427 Ceased WO2008152112A2 (de) 2007-06-12 2008-06-12 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL

Country Status (15)

Country Link
US (1) US20100292184A1 (de)
EP (1) EP2167525A2 (de)
JP (1) JP2010529174A (de)
KR (1) KR20100037596A (de)
CN (1) CN101679479A (de)
AU (1) AU2008263857A1 (de)
BR (1) BRPI0812535A2 (de)
CA (1) CA2692997A1 (de)
CL (1) CL2008001720A1 (de)
DE (1) DE102007027635A1 (de)
IL (1) IL202325A0 (de)
MX (1) MX2009013631A (de)
RU (1) RU2010100337A (de)
WO (1) WO2008152112A2 (de)
ZA (1) ZA201000186B (de)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010066349A1 (de) * 2008-12-12 2010-06-17 Bayer Schering Pharma Aktiengesellschaft Verwendung von 17beta-cyano-19-androst-4-en-derivaten zur herstellung eines arzneimittels in depot-form zur parenteralen anwendung sowie depot-arzneimittel enthaltend 17beta-cyano-19-androst-4-en-derivate zur parenteralen anwendung
WO2012059594A1 (en) 2010-11-04 2012-05-10 Bayer Pharma Aktiengesellschaft Mineralcorticoid receptor antagonists for the treatment of corticoid-induced obesity
CN105085596A (zh) * 2015-08-18 2015-11-25 湖北竹溪人福药业有限责任公司 一种羧酸黄体酮的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3705179A (en) * 1971-03-15 1972-12-05 American Home Prod Antiandrogenic steroids
DE2226552A1 (de) * 1971-06-01 1973-01-04 Roussel Uclaf Ungesaettigte, eine cyanogruppe enthaltende steroidderivate und verfahren zu deren herstellung
WO2006072467A1 (de) * 2004-12-30 2006-07-13 Schering Aktiengesellschaft 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactone, sowie diese enthaltende pharmazeutische präparate

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1183500B (de) 1962-10-12 1964-12-17 Schering Ag Verfahren zur Herstellung von alpha, beta-Methylenketonen der Steroidreihe
GB1089945A (en) * 1965-09-23 1967-11-08 British Drug Houses Ltd Steroidal-6-spirocyclopropyl-4-en-3-ones
DE1593516C3 (de) * 1966-08-25 1975-05-15 Schering Ag, 1000 Berlin Und 4619 Bergkamen 4-Halogen-1,2 alpha; 6,7 betabismethylen-delta hoch 4-3-ketosteroide, Verfahren zu ihrer Herstellung sowie diese Steroide enthaltende Mittel
DE2109555C3 (de) 1971-02-24 1980-10-30 Schering Ag Neue 15 a , 16 a -Methylensteroide, diese enthaltende Arzneimittel sowie Verfahren zu ihrei Herstellung
NL7701384A (nl) 1977-02-10 1978-08-14 Akzo Nv Werkwijze voor het bereiden van nieuwe steroiden van de oestraanreeks.
DE2922500A1 (de) 1979-05-31 1980-12-04 Schering Ag 6 beta .7 beta
US4512986A (en) * 1983-07-26 1985-04-23 Research Triangle Institute Progrestationally active steroids
DE3402329A1 (de) 1984-01-20 1985-08-01 Schering AG, 1000 Berlin und 4709 Bergkamen 6,6-ethylen-15,16-methylen-3-oxo-17(alpha)-pregn-4-en-21,17-carbolactone, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate
US5352809A (en) * 1986-10-10 1994-10-04 Gist-Brocades N.V. 9-alpha-hydroxy steroids, process for their preparation, process for the preparation of the corresponding 9(11)-dehydro derivatives and pharmaceutical preparations containing such steroids
DE19651000A1 (de) 1996-12-01 1998-06-04 Schering Ag Oxyiminopregnancarbolactone
EP1359154A1 (de) * 2002-04-29 2003-11-05 BOEHRINGER INGELHEIM INTERNATIONAL GmbH Weitere Verfahren zur Herstellung von Cyproteron Azetat
ITMI20042338A1 (it) * 2004-12-06 2005-03-06 Ind Chimica Srl Processo per la preparazione di drospirenone
DE102007027637A1 (de) * 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17ß-Cyano-19-nor-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3705179A (en) * 1971-03-15 1972-12-05 American Home Prod Antiandrogenic steroids
DE2226552A1 (de) * 1971-06-01 1973-01-04 Roussel Uclaf Ungesaettigte, eine cyanogruppe enthaltende steroidderivate und verfahren zu deren herstellung
WO2006072467A1 (de) * 2004-12-30 2006-07-13 Schering Aktiengesellschaft 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactone, sowie diese enthaltende pharmazeutische präparate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
OLDENZIEL, OTTO H. ET AL: "Chemistry of sulfonylmethyl isocyanides. 13. A general one-step synthesis of nitriles from ketones using tosylmethyl isocyanide. Introduction of a one-carbon unit", JOURNAL OF ORGANIC CHEMISTRY, ISSN: 0022-3263, vol. 42, no. 19, 1977, pages 3114 - 3118, XP002509341 *

Also Published As

Publication number Publication date
CL2008001720A1 (es) 2008-12-19
RU2010100337A (ru) 2011-07-20
MX2009013631A (es) 2010-01-20
ZA201000186B (en) 2011-03-30
JP2010529174A (ja) 2010-08-26
DE102007027635A1 (de) 2008-12-18
EP2167525A2 (de) 2010-03-31
IL202325A0 (en) 2010-06-30
CN101679479A (zh) 2010-03-24
KR20100037596A (ko) 2010-04-09
US20100292184A1 (en) 2010-11-18
CA2692997A1 (en) 2008-12-18
BRPI0812535A2 (pt) 2017-05-16
WO2008152112A2 (de) 2008-12-18
AU2008263857A1 (en) 2008-12-18

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