KR101494914B1 - 프로게스테론 수용체 길항제 - Google Patents

프로게스테론 수용체 길항제 Download PDF

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Publication number
KR101494914B1
KR101494914B1 KR1020097012215A KR20097012215A KR101494914B1 KR 101494914 B1 KR101494914 B1 KR 101494914B1 KR 1020097012215 A KR1020097012215 A KR 1020097012215A KR 20097012215 A KR20097012215 A KR 20097012215A KR 101494914 B1 KR101494914 B1 KR 101494914B1
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KR
South Korea
Prior art keywords
pentafluoro
phenyl
hydroxy
dien
dihydroxyethyl
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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
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KR1020097012215A
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English (en)
Korean (ko)
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KR20090079995A (ko
Inventor
울리케 푸르만
안야 슈미트
아르베트 클레페
올린 페트로프
군나르 가르케
스테판 프루에스
마르가레트 브루드니-클로에펠
안톄 로트만
라이너 하셀만
마르쿠스 슐체-모스가우
카르스텐 묄러
Original Assignee
바이엘 인텔렉쳐 프로퍼티 게엠베하
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Publication of KR20090079995A publication Critical patent/KR20090079995A/ko
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    • 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

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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)
  • 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)
KR1020097012215A 2006-11-15 2007-11-14 프로게스테론 수용체 길항제 Expired - Fee Related KR101494914B1 (ko)

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
KR20090079995A KR20090079995A (ko) 2009-07-22
KR101494914B1 true KR101494914B1 (ko) 2015-02-23

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KR1020097012215A Expired - Fee Related KR101494914B1 (ko) 2006-11-15 2007-11-14 프로게스테론 수용체 길항제

Country Status (40)

Country Link
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
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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

Citations (1)

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US6316432B1 (en) 1997-02-07 2001-11-13 Schering Aktiengesellschaft Antigestagenically active steroids with a flourinated 17 α-alkyl chain

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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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DE102006054535A1 (de) 2006-11-15 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Progesteronrezeptorantagonisten

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6316432B1 (en) 1997-02-07 2001-11-13 Schering Aktiengesellschaft Antigestagenically active steroids with a flourinated 17 α-alkyl chain

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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
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
CN101541823B (zh) 2012-10-03
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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