CO6180443A2 - Antagonistas del receptor de progesterona - Google Patents
Antagonistas del receptor de progesteronaInfo
- Publication number
- CO6180443A2 CO6180443A2 CO09050000A CO09050000A CO6180443A2 CO 6180443 A2 CO6180443 A2 CO 6180443A2 CO 09050000 A CO09050000 A CO 09050000A CO 09050000 A CO09050000 A CO 09050000A CO 6180443 A2 CO6180443 A2 CO 6180443A2
- Authority
- CO
- Colombia
- Prior art keywords
- pregna
- pentafluoro
- hydroxy
- phenyl
- dien
- Prior art date
Links
Classifications
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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
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- 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
1.- Un antagonista de receptor de progesterona de la fórmula general I:en la que R1 puede ser un átomo de hidrógeno y R2 puede ser un grupo hidroxilo o R1 y R2 pueden ser juntos un grupo oxo. 2.- 11ß-[4-(1,2-Dihidroxietil)fenil]-20,20,21,21,21- pentafluoro-17-hidroxi-19-nor-17a -pregna-4,9-dien-3-ona. 3.- 11ß-[4-[(1R) -1,2-Dihidroxietil]fenil] -20, 20, 21, 21, 21-pentafluoro-17-hidroxi-19-nor-17a -pregna-4,9-dien-3-ona. 4.- 11ß-[4-[(1S)-1,2-Dihidroxietil]fenil]-20,20,21,21, 21-pentafluoro-17-hidroxi-19-nor-17a-pregna-4,9-dien-3-ona. 5.- 20,20,21,21,21-Pentafluoro-17-hidroxi-11ß-[4-(hidroxiacetil) fenil]-19-nor-17a-pregna-4,9-dien--3-ona. 6.- Un fármaco que contiene antagonistas del receptor de progesterona de acuerdo con la reivindicación 1. 7.- El fármaco de acuerdo con la reivindicación 6 que contiene 11ß-[4-(1,2-dihidroxietil) fenil] -20, 20, 21, 21, 21- pentafluoro-17-hidroxi-19-nor-17a-pregna-4,9-dien-3-ona. 8.- El fármaco de acuerdo con la reivindicación 7 que contiene 11ß-[4-[(1R)-1,2-dihidroxietil]fenil]-20, 20, 21, 21, 21-pentafluoro-17-hidroxi-19-nor-17a-pregna-4,9-dien-3-ona. 9.- El fármaco de acuerdo con la reivindicación 7 que contiene 11ß-[4-[(1S)-1,2-dihidroxietil]fenil]-20,20,21,21, 21-pentafluoro-17-hidroxi-19-nor-17a-pregna-4,9-dien-3-ona. 10.- El fármaco de acuerdo con la reivindicación 6 que contiene 20, 20, 21, 21, 21-pentafluoro-17-hidroxi-11ß-[4- hidroxiacetil)fenil]-19-nor-17a -pregna-4,9-dien-3-ona.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102006054535A DE102006054535A1 (de) | 2006-11-15 | 2006-11-15 | Progesteronrezeptorantagonisten |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6180443A2 true CO6180443A2 (es) | 2010-07-19 |
Family
ID=39243738
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO09050000A CO6180443A2 (es) | 2006-11-15 | 2009-05-15 | Antagonistas del receptor de progesterona |
Country Status (41)
Families Citing this family (22)
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 |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3347126A1 (de) | 1983-12-22 | 1985-07-11 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
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 |
CN86102502B (zh) * | 1986-08-29 | 1988-06-22 | 上海市计划生育科学研究所 | 11,17位双取代δ4,9-雌甾二烯化合物的合成方法 |
CA2100514C (en) | 1992-07-29 | 2005-03-29 | Johannes A. M. Hamersma | 17-spiromethylene steroids |
DE4332283A1 (de) * | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
DE19535572B4 (de) * | 1994-09-14 | 2007-02-01 | Schering Ag | Verfahren zur Herstellung von 17 α-Fluor-steroid-ketonen |
ES2218556T3 (es) | 1994-11-22 | 2004-11-16 | Balance Pharmaceuticals, Inc. | Metodos de contracepcion. |
WO1998005679A2 (en) | 1996-08-05 | 1998-02-12 | Duke University | Mixed agonists of the progesterone receptor and assays therefor |
DE19706061A1 (de) * | 1997-02-07 | 1998-08-13 | Schering Ag | Antigestagen wirksame Steroide mit fluorierter 17alpha-Alkylkette |
US20010016578A1 (en) | 1997-06-18 | 2001-08-23 | Balance Pharmaceuticals, Inc. | Compositions and methods for contraception and for treatment of benign gynecological disorders |
DE19929715A1 (de) * | 1999-06-24 | 2000-12-28 | Schering Ag | 11ß-langkettig-substituierte Estratriene, Verfahren zur Herstellung , pharmazeutische Präparate, die diese 11ß-langkettig-substituierten Estratriene enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
DE10049736A1 (de) * | 2000-09-29 | 2002-04-18 | Jenapharm Gmbh | 17alpha-Fluoralkylsteroide, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
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 |
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2006
- 2006-11-15 DE DE102006054535A patent/DE102006054535A1/de not_active Withdrawn
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2007
- 2007-11-11 JO JO2007469A patent/JO2672B1/en active
- 2007-11-13 CL CL200703266A patent/CL2007003266A1/es unknown
- 2007-11-14 EA EA200900635A patent/EA017038B1/ru not_active IP Right Cessation
- 2007-11-14 ES ES07819866T patent/ES2343915T3/es active Active
- 2007-11-14 CA CA2669767A patent/CA2669767C/en not_active Expired - Fee Related
- 2007-11-14 PA PA20078755801A patent/PA8755801A1/es unknown
- 2007-11-14 BR BRPI0718409-3A patent/BRPI0718409A2/pt not_active IP Right Cessation
- 2007-11-14 DK DK07819866.0T patent/DK2081951T3/da active
- 2007-11-14 CN CN200780042476XA patent/CN101541823B/zh not_active Expired - Fee Related
- 2007-11-14 NZ NZ576927A patent/NZ576927A/en not_active IP Right Cessation
- 2007-11-14 PE PE2007001568A patent/PE20081409A1/es not_active Application Discontinuation
- 2007-11-14 WO PCT/EP2007/009997 patent/WO2008058767A1/en active Application Filing
- 2007-11-14 JP JP2009536670A patent/JP5260537B2/ja not_active Expired - Fee Related
- 2007-11-14 RS RSP-2010/0290A patent/RS51369B/en unknown
- 2007-11-14 MX MX2009005212A patent/MX2009005212A/es active IP Right Grant
- 2007-11-14 PL PL07819866T patent/PL2081951T3/pl unknown
- 2007-11-14 KR KR1020097012215A patent/KR101494914B1/ko not_active IP Right Cessation
- 2007-11-14 SI SI200730275T patent/SI2081951T1/sl unknown
- 2007-11-14 UA UAA200906032A patent/UA98312C2/ru unknown
- 2007-11-14 AT AT07819866T patent/ATE465169T1/de active
- 2007-11-14 EP EP07819866A patent/EP2081951B1/en active Active
- 2007-11-14 DE DE602007006040T patent/DE602007006040D1/de active Active
- 2007-11-14 PT PT07819866T patent/PT2081951E/pt unknown
- 2007-11-14 AU AU2007321848A patent/AU2007321848B2/en not_active Ceased
- 2007-11-14 AR ARP070105061A patent/AR063813A1/es unknown
- 2007-11-15 TW TW096143300A patent/TW200831109A/zh unknown
- 2007-11-15 US US11/984,331 patent/US8053426B2/en not_active Expired - Fee Related
- 2007-11-15 UY UY30718A patent/UY30718A1/es not_active Application Discontinuation
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2009
- 2009-05-07 IL IL198650A patent/IL198650A/en not_active IP Right Cessation
- 2009-05-08 TN TNP2009000185A patent/TN2009000185A1/fr unknown
- 2009-05-15 HN HN2009000997A patent/HN2009000997A/es unknown
- 2009-05-15 GT GT200900128A patent/GT200900128A/es unknown
- 2009-05-15 EC EC2009009337A patent/ECSP099337A/es unknown
- 2009-05-15 SV SV2009003260A patent/SV2009003260A/es active IP Right Grant
- 2009-05-15 CO CO09050000A patent/CO6180443A2/es active IP Right Grant
- 2009-06-12 ZA ZA2009/04150A patent/ZA200904150B/en unknown
- 2009-06-12 NO NO20092284A patent/NO20092284L/no not_active Application Discontinuation
- 2009-06-12 MA MA31988A patent/MA30990B1/fr unknown
-
2010
- 2010-03-22 HK HK10102964.6A patent/HK1136302A1/xx not_active IP Right Cessation
- 2010-06-29 HR HR20100366T patent/HRP20100366T1/hr unknown
- 2010-07-21 CY CY20101100681T patent/CY1110671T1/el unknown
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