EA200900635A1 - Антагонисты прогестеронового рецептора - Google Patents

Антагонисты прогестеронового рецептора

Info

Publication number
EA200900635A1
EA200900635A1 EA200900635A EA200900635A EA200900635A1 EA 200900635 A1 EA200900635 A1 EA 200900635A1 EA 200900635 A EA200900635 A EA 200900635A EA 200900635 A EA200900635 A EA 200900635A EA 200900635 A1 EA200900635 A1 EA 200900635A1
Authority
EA
Eurasian Patent Office
Prior art keywords
receptor antagonists
protesteron
general formula
hydrogen atom
relates
Prior art date
Application number
EA200900635A
Other languages
English (en)
Other versions
EA017038B1 (ru
Inventor
Ульрике Фурманн
Аня Шмидт
Арвед Клеве
Орлин Петров
Гуннар Гарке
Штефан Прюс
Маргарете Брудни-Клёппель
Антье Роттманн
Райнер Хассельманн
Маркус Шултце-Мосгау
Карстен Мёллер
Original Assignee
Байер Шеринг Фарма Акциенгезельшафт
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 Байер Шеринг Фарма Акциенгезельшафт filed Critical Байер Шеринг Фарма Акциенгезельшафт
Publication of EA200900635A1 publication Critical patent/EA200900635A1/ru
Publication of EA017038B1 publication Critical patent/EA017038B1/ru

Links

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)
  • Pregnancy & Childbirth (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Настоящее изобретение относится к антагонистам прогестеронового рецептора общей формулы Iв которой R1 может быть атомом водорода и R2 гидроксильной группой или R1 и R2 вместе могут быть оксогруппой.
EA200900635A 2006-11-15 2007-11-14 Антагонисты прогестеронового рецептора EA017038B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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
EA200900635A1 true EA200900635A1 (ru) 2009-12-30
EA017038B1 EA017038B1 (ru) 2012-09-28

Family

ID=39243738

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200900635A EA017038B1 (ru) 2006-11-15 2007-11-14 Антагонисты прогестеронового рецептора

Country Status (41)

Country Link
US (1) US8053426B2 (ru)
EP (1) EP2081951B1 (ru)
JP (1) JP5260537B2 (ru)
KR (1) KR101494914B1 (ru)
CN (1) CN101541823B (ru)
AR (1) AR063813A1 (ru)
AT (1) ATE465169T1 (ru)
AU (1) AU2007321848B2 (ru)
BR (1) BRPI0718409A2 (ru)
CA (1) CA2669767C (ru)
CL (1) CL2007003266A1 (ru)
CO (1) CO6180443A2 (ru)
CY (1) CY1110671T1 (ru)
DE (2) DE102006054535A1 (ru)
DK (1) DK2081951T3 (ru)
EA (1) EA017038B1 (ru)
EC (1) ECSP099337A (ru)
ES (1) ES2343915T3 (ru)
GT (1) GT200900128A (ru)
HK (1) HK1136302A1 (ru)
HN (1) HN2009000997A (ru)
HR (1) HRP20100366T1 (ru)
IL (1) IL198650A (ru)
JO (1) JO2672B1 (ru)
MA (1) MA30990B1 (ru)
MX (1) MX2009005212A (ru)
NO (1) NO20092284L (ru)
NZ (1) NZ576927A (ru)
PA (1) PA8755801A1 (ru)
PE (1) PE20081409A1 (ru)
PL (1) PL2081951T3 (ru)
PT (1) PT2081951E (ru)
RS (1) RS51369B (ru)
SI (1) SI2081951T1 (ru)
SV (1) SV2009003260A (ru)
TN (1) TN2009000185A1 (ru)
TW (1) TW200831109A (ru)
UA (1) UA98312C2 (ru)
UY (1) UY30718A1 (ru)
WO (1) WO2008058767A1 (ru)
ZA (1) ZA200904150B (ru)

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
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
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
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
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
US10786461B2 (en) 2014-11-17 2020-09-29 Context Biopharma Inc. Onapristone extended-release compositions and methods
BR112018005999A2 (pt) 2015-09-25 2019-01-08 Context Biopharma Inc métodos para a produção de intermediários de onapristona
KR20180113988A (ko) 2015-12-15 2018-10-17 컨텍스트 바이오파마 인코포레이티드 비정질 오나프리스톤 조성물 및 그 제조방법
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
JP2019513706A (ja) * 2016-03-21 2019-05-30 コンテキスト・バイオファーマ・インコーポレイテッド オナプリストン代謝物質組成物及び方法
US20180148471A1 (en) 2016-11-30 2018-05-31 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection

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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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JP4335525B2 (ja) * 2000-10-18 2009-09-30 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト 腫瘍細胞の増殖因子依存性の阻害
US20020143000A1 (en) 2001-01-09 2002-10-03 Christa Hegele-Hartung Use of antigestagens for inhibiting accelerated endometrial maturation during infertility treatment
DE10221034A1 (de) 2002-05-03 2003-11-20 Schering Ag 17alpha-Fluoralkyl-11ß-benzaldoxim-Steroide, Verfahren zu deren Herstellung, diese Steroide enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
ES2252670T3 (es) 2002-05-03 2006-05-16 Schering Ag Esteroides con fluoroalquilo en 17a y benzaldoxima en 11beta, procedimiento para su preparacion, formulaciones farmaceuticas que contienen estos esteroides, asi como su utilizacion para la produccion de medicamentos.
EP1862468A1 (de) * 2006-06-02 2007-12-05 Bayer Schering Pharma Aktiengesellschaft Kristallines 11beta-(4-Acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-on
DE102006054535A1 (de) 2006-11-15 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Progesteronrezeptorantagonisten

Also Published As

Publication number Publication date
WO2008058767A1 (en) 2008-05-22
KR20090079995A (ko) 2009-07-22
CN101541823B (zh) 2012-10-03
EP2081951B1 (en) 2010-04-21
HK1136302A1 (en) 2010-06-25
CY1110671T1 (el) 2015-06-10
IL198650A0 (en) 2010-02-17
RS51369B (en) 2011-02-28
MX2009005212A (es) 2009-05-27
GT200900128A (es) 2012-02-01
PT2081951E (pt) 2010-07-01
PE20081409A1 (es) 2008-12-05
PL2081951T3 (pl) 2010-09-30
ECSP099337A (es) 2009-06-30
ES2343915T3 (es) 2010-08-12
BRPI0718409A2 (pt) 2013-12-17
CA2669767C (en) 2014-04-01
US20080200440A1 (en) 2008-08-21
ZA200904150B (en) 2010-11-24
CN101541823A (zh) 2009-09-23
TW200831109A (en) 2008-08-01
EP2081951A1 (en) 2009-07-29
HRP20100366T1 (hr) 2010-07-31
SV2009003260A (es) 2009-12-14
UA98312C2 (en) 2012-05-10
PA8755801A1 (es) 2009-08-26
CL2007003266A1 (es) 2008-07-04
US8053426B2 (en) 2011-11-08
AU2007321848A1 (en) 2008-05-22
HN2009000997A (es) 2011-10-19
ATE465169T1 (de) 2010-05-15
AU2007321848B2 (en) 2013-09-19
JP2010509386A (ja) 2010-03-25
SI2081951T1 (sl) 2010-08-31
CA2669767A1 (en) 2008-05-22
TN2009000185A1 (en) 2010-10-18
DK2081951T3 (da) 2010-08-09
UY30718A1 (es) 2008-07-03
EA017038B1 (ru) 2012-09-28
IL198650A (en) 2012-05-31
NO20092284L (no) 2009-08-13
JO2672B1 (en) 2012-06-17
JP5260537B2 (ja) 2013-08-14
CO6180443A2 (es) 2010-07-19
MA30990B1 (fr) 2009-12-01
NZ576927A (en) 2012-01-12
DE102006054535A1 (de) 2008-05-21
KR101494914B1 (ko) 2015-02-23
AR063813A1 (es) 2009-02-18
DE602007006040D1 (de) 2010-06-02

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