CN101541823B - 孕酮受体拮抗剂 - Google Patents

孕酮受体拮抗剂 Download PDF

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Publication number
CN101541823B
CN101541823B CN200780042476XA CN200780042476A CN101541823B CN 101541823 B CN101541823 B CN 101541823B CN 200780042476X A CN200780042476X A CN 200780042476XA CN 200780042476 A CN200780042476 A CN 200780042476A CN 101541823 B CN101541823 B CN 101541823B
Authority
CN
China
Prior art keywords
ketone
pregnant
fluoro
phenyl
receptor antagonists
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.)
Expired - Fee Related
Application number
CN200780042476XA
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English (en)
Chinese (zh)
Other versions
CN101541823A (zh
Inventor
U·富尔曼
A·施密特
A·克利夫
O·彼得罗夫
G·加尔克
S·普吕斯
M·布鲁德尼-克勒佩尔
A·罗特曼
R·哈赛尔曼
M·舒尔策-摩斯高
C·莫勒
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
Bayer Intellectual Property GmbH
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
Application filed by Bayer Schering Pharma AG filed Critical Bayer Schering Pharma AG
Publication of CN101541823A publication Critical patent/CN101541823A/zh
Application granted granted Critical
Publication of CN101541823B publication Critical patent/CN101541823B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • 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
    • A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • 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
    • A61P15/18—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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

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)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oncology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN200780042476XA 2006-11-15 2007-11-14 孕酮受体拮抗剂 Expired - Fee Related CN101541823B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102006054535.4 2006-11-15
DE102006054535A DE102006054535A1 (de) 2006-11-15 2006-11-15 Progesteronrezeptorantagonisten
PCT/EP2007/009997 WO2008058767A1 (en) 2006-11-15 2007-11-14 Progesterone receptor antagonists

Publications (2)

Publication Number Publication Date
CN101541823A CN101541823A (zh) 2009-09-23
CN101541823B true CN101541823B (zh) 2012-10-03

Family

ID=39243738

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200780042476XA Expired - Fee Related CN101541823B (zh) 2006-11-15 2007-11-14 孕酮受体拮抗剂

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US (1) US8053426B2 (enExample)
EP (1) EP2081951B1 (enExample)
JP (1) JP5260537B2 (enExample)
KR (1) KR101494914B1 (enExample)
CN (1) CN101541823B (enExample)
AR (1) AR063813A1 (enExample)
AT (1) ATE465169T1 (enExample)
AU (1) AU2007321848B2 (enExample)
BR (1) BRPI0718409A2 (enExample)
CA (1) CA2669767C (enExample)
CL (1) CL2007003266A1 (enExample)
CO (1) CO6180443A2 (enExample)
CY (1) CY1110671T1 (enExample)
DE (2) DE102006054535A1 (enExample)
DK (1) DK2081951T3 (enExample)
EA (1) EA017038B1 (enExample)
EC (1) ECSP099337A (enExample)
ES (1) ES2343915T3 (enExample)
GT (1) GT200900128A (enExample)
HN (1) HN2009000997A (enExample)
HR (1) HRP20100366T1 (enExample)
IL (1) IL198650A (enExample)
JO (1) JO2672B1 (enExample)
MA (1) MA30990B1 (enExample)
MX (1) MX2009005212A (enExample)
NO (1) NO20092284L (enExample)
NZ (1) NZ576927A (enExample)
PA (1) PA8755801A1 (enExample)
PE (1) PE20081409A1 (enExample)
PL (1) PL2081951T3 (enExample)
PT (1) PT2081951E (enExample)
RS (1) RS51369B (enExample)
SI (1) SI2081951T1 (enExample)
SV (1) SV2009003260A (enExample)
TN (1) TN2009000185A1 (enExample)
TW (1) TW200831109A (enExample)
UA (1) UA98312C2 (enExample)
UY (1) UY30718A1 (enExample)
WO (1) WO2008058767A1 (enExample)
ZA (1) ZA200904150B (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102006054535A1 (de) 2006-11-15 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Progesteronrezeptorantagonisten
EP2123279A1 (de) * 2008-05-14 2009-11-25 Bayer Schering Pharma Aktiengesellschaft Sequentielle Verabreichung von 20,20,21,21,21-Pentafluor-17-hydroxy-1 1beta-[4-(hydroxyacetyl) phenyl]-19-nor-17alpha-pregna-4,9-dien-3-on und einem oder mehreren Gestagenen zur Behandlung gynäkologischer Erkrankungen
DE102009034362A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034368A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylenphenyl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034366A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-methylenoxyalkylenaryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034367A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-benzyliden-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
DE102009034525A1 (de) 2009-07-21 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034526A1 (de) * 2009-07-21 2011-02-10 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-ethinylphenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
DE102010007722A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
DE102010007719A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
DE102010030538A1 (de) 2010-06-25 2011-12-29 Bayer Schering Pharma Aktiengesellschaft 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
DE102011004899A1 (de) 2011-03-01 2012-09-06 Bayer Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
US20130029953A1 (en) * 2011-07-28 2013-01-31 Klaus Nickisch Progesterone antagonists
DE102011087987A1 (de) 2011-12-08 2013-06-13 Bayer Intellectual Property Gmbh 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
US9096641B2 (en) 2013-06-05 2015-08-04 Evestra, Inc. Imidazolyl progesterone antagonists
EP2868320A1 (en) 2013-11-03 2015-05-06 Flamina Holding AG A composition or group of compositions for the treatment of human cells
CA2966753A1 (en) 2014-11-17 2016-05-26 Arno Therapeutics, Inc. Onapristone extended-release compositions and methods
AU2016326657B2 (en) 2015-09-25 2019-10-24 Context Biopharma, Inc. Methods of making onapristone intermediates
CA3008422A1 (en) 2015-12-15 2017-06-22 Context Biopharma Inc. Amorphous onapristone compositions and methods of making the same
EP3214092A1 (en) 2016-03-04 2017-09-06 Bayer Pharma Aktiengesellschaft Prodrugs of the selective progesterone receptor modulator (sprm) (11.beta.,17.beta.)-17-hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one
WO2017165315A1 (en) * 2016-03-21 2017-09-28 Arno Therapeutics, Inc. Onapristone metabolite compositions and methods
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection

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US5693628A (en) * 1993-09-20 1997-12-02 Jenapharm Gmbh 11-benzaldoxime-estra-diene derivatives, methods for their production and pharmaceuticals containing these compounds
CN1246865A (zh) * 1997-02-07 2000-03-08 舍林股份公司 具氟化17α－烷基链的抗孕激素活性类固醇

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FR2596395B1 (fr) * 1986-03-26 1989-05-26 Roussel Uclaf Nouveaux steroides comportant un cycle spirannique en position 17, leur procede de preparation, leur application comme medicaments et les compositions les renfermant
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US20020143000A1 (en) * 2001-01-09 2002-10-03 Christa Hegele-Hartung Use of antigestagens for inhibiting accelerated endometrial maturation during infertility treatment
WO2003093292A1 (de) 2002-05-03 2003-11-13 Schering Ag 17α-FLUORALKYL-11β-BENZALDOXIM-STEROIDE, VERFAHREN ZU DEREN HERSTELLUNG, DIESE STEROIDE ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
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US5693628A (en) * 1993-09-20 1997-12-02 Jenapharm Gmbh 11-benzaldoxime-estra-diene derivatives, methods for their production and pharmaceuticals containing these compounds
CN1246865A (zh) * 1997-02-07 2000-03-08 舍林股份公司 具氟化17α－烷基链的抗孕激素活性类固醇

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Ulrike Fuhrmann,et al..Synthesis and Biological Activity of a Novel, Highly Potent Progesterone Receptor Antagonist.《J. Med. Chem.》.2000,第43卷(第26期),5010-5016. *
UlrikeFuhrmann et al..Synthesis and Biological Activity of a Novel

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Publication number Publication date
TW200831109A (en) 2008-08-01
ECSP099337A (es) 2009-06-30
GT200900128A (es) 2012-02-01
RS51369B (sr) 2011-02-28
AU2007321848A1 (en) 2008-05-22
KR101494914B1 (ko) 2015-02-23
IL198650A (en) 2012-05-31
CA2669767A1 (en) 2008-05-22
CA2669767C (en) 2014-04-01
NZ576927A (en) 2012-01-12
SV2009003260A (es) 2009-12-14
CL2007003266A1 (es) 2008-07-04
ES2343915T3 (es) 2010-08-12
US20080200440A1 (en) 2008-08-21
EP2081951B1 (en) 2010-04-21
EA200900635A1 (ru) 2009-12-30
UA98312C2 (en) 2012-05-10
DE102006054535A1 (de) 2008-05-21
BRPI0718409A2 (pt) 2013-12-17
US8053426B2 (en) 2011-11-08
EA017038B1 (ru) 2012-09-28
JP2010509386A (ja) 2010-03-25
NO20092284L (no) 2009-08-13
JP5260537B2 (ja) 2013-08-14
CY1110671T1 (el) 2015-06-10
MA30990B1 (fr) 2009-12-01
PE20081409A1 (es) 2008-12-05
HK1136302A1 (en) 2010-06-25
HRP20100366T1 (hr) 2010-07-31
PL2081951T3 (pl) 2010-09-30
ATE465169T1 (de) 2010-05-15
MX2009005212A (es) 2009-05-27
HN2009000997A (es) 2011-10-19
JO2672B1 (en) 2012-06-17
TN2009000185A1 (en) 2010-10-18
KR20090079995A (ko) 2009-07-22
CN101541823A (zh) 2009-09-23
PA8755801A1 (es) 2009-08-26
AU2007321848B2 (en) 2013-09-19
SI2081951T1 (sl) 2010-08-31
DK2081951T3 (da) 2010-08-09
EP2081951A1 (en) 2009-07-29
IL198650A0 (en) 2010-02-17
UY30718A1 (es) 2008-07-03
WO2008058767A1 (en) 2008-05-22
CO6180443A2 (es) 2010-07-19
ZA200904150B (en) 2010-11-24
PT2081951E (pt) 2010-07-01
DE602007006040D1 (de) 2010-06-02
AR063813A1 (es) 2009-02-18

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