ES2108371T3 - Nuevos derivados de estradieno de 11-benzaldoxima, procedimientos para su produccion y farmacos conteniendo estos compuestos. - Google Patents
Nuevos derivados de estradieno de 11-benzaldoxima, procedimientos para su produccion y farmacos conteniendo estos compuestos.Info
- Publication number
- ES2108371T3 ES2108371T3 ES94250178T ES94250178T ES2108371T3 ES 2108371 T3 ES2108371 T3 ES 2108371T3 ES 94250178 T ES94250178 T ES 94250178T ES 94250178 T ES94250178 T ES 94250178T ES 2108371 T3 ES2108371 T3 ES 2108371T3
- Authority
- ES
- Spain
- Prior art keywords
- compounds
- new derivatives
- benzaldoxima
- estradiene
- procedures
- 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 - Lifetime
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 229940079593 drug Drugs 0.000 title 1
- 150000002158 estradienes Chemical class 0.000 title 1
- 230000000694 effects Effects 0.000 abstract 2
- 239000003418 antiprogestin Substances 0.000 abstract 1
- 230000003247 decreasing effect Effects 0.000 abstract 1
- 239000003862 glucocorticoid Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P5/32—Antioestrogens
-
- 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
- C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
- C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Toxicology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE DESCRIBEN NUEVOS DERIVADOS 11 DE LA FORMULA GENERAL I Y SUS SALES EXTRAIBLES FARMACEUTICAMENTE, UN PROCESO PARA SU ELABORACION Y LOS MEDICAMENTOS QUE CONTIENEN ESTOS COMPUESTOS. LOS COMPUESTOS DESCRITOS MUESTRAN EFECTOS ANTIGESTAGENOS FUERTES CON ACTIVIDAD DISMINUIDA GLUCOCORTICOIDE.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4332283A DE4332283A1 (de) | 1993-09-20 | 1993-09-20 | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US08/309,175 US5693628A (en) | 1993-09-20 | 1994-09-20 | 11-benzaldoxime-estra-diene derivatives, methods for their production and pharmaceuticals containing these compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2108371T3 true ES2108371T3 (es) | 1997-12-16 |
Family
ID=25929786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES94250178T Expired - Lifetime ES2108371T3 (es) | 1993-09-20 | 1994-07-07 | Nuevos derivados de estradieno de 11-benzaldoxima, procedimientos para su produccion y farmacos conteniendo estos compuestos. |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US5693628A (es) |
| EP (1) | EP0648778B1 (es) |
| JP (1) | JP2753562B2 (es) |
| AT (1) | ATE156835T1 (es) |
| AU (1) | AU682195B2 (es) |
| CA (1) | CA2130516C (es) |
| CZ (1) | CZ292298B6 (es) |
| DE (2) | DE4332283A1 (es) |
| DK (1) | DK0648778T3 (es) |
| ES (1) | ES2108371T3 (es) |
| FI (1) | FI113657B (es) |
| HU (1) | HU223339B1 (es) |
| NO (1) | NO304989B1 (es) |
| NZ (1) | NZ264229A (es) |
| PL (1) | PL183181B1 (es) |
| SK (1) | SK280137B6 (es) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4332284C2 (de) * | 1993-09-20 | 1997-05-28 | Jenapharm Gmbh | 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE4332283A1 (de) * | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US5576310A (en) * | 1994-09-20 | 1996-11-19 | Jenapharm Gmbh | 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds |
| DE19548450A1 (de) * | 1995-12-22 | 1997-06-26 | Jenapharm Gmbh | 17alpha-Cyanomethylestra-4,9-dien-3-on-17beta-yl- derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| DE19745085A1 (de) * | 1997-10-11 | 1999-04-15 | Jenapharm Gmbh | 11ß-Benzaldoxim-9alpha,10alpha-epoxy-estr-4-en-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Präparate |
| DE19809845A1 (de) * | 1998-03-03 | 1999-09-09 | Jenapharm Gmbh | S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen |
| DE19906152B4 (de) | 1999-02-10 | 2005-02-10 | Jenapharm Gmbh & Co. Kg | Wirkstoffhaltige Laminate für Transdermalsysteme |
| PE20010581A1 (es) | 1999-08-31 | 2001-06-04 | Schering Ag | Mesoprogestinas (modulares de receptores de progesterona) como componentes de composiciones utilizadas para la terapia de sustitucion hormonal (hrt) |
| US7629334B1 (en) | 1999-08-31 | 2009-12-08 | Bayer Schering Pharma Aktiengesellschaft | Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT) |
| US8193252B1 (en) | 1999-08-31 | 2012-06-05 | Bayer Pharma AG | Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders |
| CO5200772A1 (es) * | 1999-08-31 | 2002-09-27 | Jenapharm Gmbh And Co Kg | Mesoprogestinas (moduladores de receptores de progesterona) para el trataiento y la prevencion de transtornos ginecolo- gicos benignos hormona-dependientes |
| CN1384748A (zh) * | 1999-08-31 | 2002-12-11 | 耶拿制药两合公司 | 作为女性避孕药成分的中孕酮(孕酮受体调节剂) |
| DE19961219A1 (de) * | 1999-12-15 | 2001-07-19 | Jenapharm Gmbh | 11beta-Phenylestratrien-Derivate mit Fluoralkylgruppen in der aromatischen Seitenkette, deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| EP1157996A1 (de) * | 2000-05-23 | 2001-11-28 | JENAPHARM GmbH | Neue Festkörperformen des Mesoprogestins 11Beta-[4E-(Hydroxyiminomethyl)-phenyl]-17Alpha-methoxymethyl-17Beta-methoxy-estra-4,9-dien-3-on |
| JP4593754B2 (ja) * | 2000-10-13 | 2010-12-08 | 一般財団法人 化学物質評価研究機構 | 化学物質の50%阻害濃度決定方法 |
| DE10056675A1 (de) | 2000-11-10 | 2002-05-16 | Jenapharm Gmbh | Verfahren zur Herstellung von 4-(17alpha-Methylsubstituierten 3-Oxoestra-4,9-dien-11ß-yl)-benzaldehyd-(1E oder 1Z)-oximen |
| DE10056676A1 (de) * | 2000-11-10 | 2002-05-16 | Jenapharm Gmbh | Verfahren zur Herstellung von 4-/17alpha-substituierten-3-oxoestra-4,9-dien-11beta-yl)benzaldehyd-(1E oder 1Z)-oximen |
| EP1285927A3 (de) * | 2001-08-16 | 2005-06-29 | Schering Aktiengesellschaft | Verwendung von Glucocorticoid-Rezeptorantagonisten zur Vorbeugung und Behandlung von Erkrankungen des männlichen Reproduktionssystems |
| DE10218109A1 (de) * | 2002-04-23 | 2003-11-20 | Jenapharm Gmbh | Verfahren zum Herstellen von Kristallen, danach erhältliche Kristalle und deren Verwendung in pharmazeutischen Formulierungen |
| DE10218107A1 (de) * | 2002-04-23 | 2003-11-20 | Jenapharm Gmbh | Verfahren zum Herstellen von Kristallen von Steroiden, danach erhältliche Kristalle und deren Verwendung in pharmazeutischen Formulierungen |
| 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 |
| ES2273061T3 (es) * | 2002-08-02 | 2007-05-01 | Schering Aktiengesellschaft | Agentes moduladores de receptores de progesterona con actividad antigonadotropa elevada para el control de fertilidad femenina y para la terapia por reemplazo hormonal. |
| DE10236405A1 (de) * | 2002-08-02 | 2004-02-19 | Schering Ag | Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie |
| US20050215535A1 (en) * | 2004-03-24 | 2005-09-29 | Kristof Chwalisz | Sequential SPRM/progestin treatment |
| US20050215536A1 (en) * | 2004-03-24 | 2005-09-29 | Kristof Chwalisz | Sequential SPRM/ progestin treatment |
| DE102005059222B4 (de) * | 2005-12-08 | 2007-10-11 | Bayer Schering Pharma Ag | 11ß-Benzaldoximderivate von D-Homoestra-4,9-dien-3-onen |
| DE102006018888A1 (de) * | 2006-04-18 | 2007-10-25 | Bayer Schering Pharma Ag | Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil) |
| EP2078032B1 (en) | 2006-10-24 | 2017-08-02 | Repros Therapeutics Inc. | Compositions and methods for suppressing endometrial proliferation |
| DE102006054535A1 (de) * | 2006-11-15 | 2008-05-21 | Bayer Schering Pharma Aktiengesellschaft | Progesteronrezeptorantagonisten |
| TWI539953B (zh) | 2008-04-28 | 2016-07-01 | 瑞波若斯治療學公司 | 用於治療乳癌之組成物和方法 |
| 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 |
| 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 |
| 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 |
| PH12012501812A1 (en) | 2010-03-22 | 2012-12-10 | Allergan Pharmaceuticals Int Ltd | Compositions and methods for non-toxic delivery of antiprogestins |
| 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 |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU580843B2 (en) * | 1985-02-07 | 1989-02-02 | Schering Aktiengesellschaft | 11``-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them |
| DE3506785A1 (de) * | 1985-02-22 | 1986-08-28 | Schering AG, Berlin und Bergkamen, 1000 Berlin | 11ss-n,n-dimethylaminophenyl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| FR2598421B1 (fr) * | 1986-05-06 | 1988-08-19 | Roussel Uclaf | Nouveaux produits 19-nor ou 19-nor d-homo steroides substitues en position 11b par un radical phenyle portant un radical alkynyle, leur procede de preparation, leur application comme medicaments et les compositions les renfermant |
| US5272140A (en) * | 1987-01-23 | 1993-12-21 | Akzo N.V. | 11-aryl steroid derivatives |
| DE3866410D1 (de) * | 1987-04-24 | 1992-01-09 | Akzo Nv | 11-arylestranderivate und 11-arylpregnanderivate. |
| DD287510A5 (de) * | 1989-04-19 | 1991-02-28 | Adw,Zi Fuer Mikrobiologie Und Experimentelle Therapie,De | Verfahren zur herstellung von 17 alpha-ch tief 2x-substituierten 11 beta-aryl-4,9-diensteroiden |
| DK0411733T3 (da) * | 1989-08-04 | 1999-06-28 | Schering Ag | 11-beta-aryl-gona-4,9-dien-3-oner |
| US5276023A (en) * | 1989-08-08 | 1994-01-04 | Roussel Uclaf | 19-nor-steroid esters |
| DD289539A5 (de) * | 1989-10-12 | 1991-05-02 | Zi F. Mikrobiologie U. Experimentelle Therapie,De | Verfahren zur herstellung von 11 beta-(4-acetylphenyl)-17alpha-alkoxy-methyl-estra-4,9-dien-3-onen |
| US5407928A (en) * | 1990-08-15 | 1995-04-18 | Schering Aktiengesellschaft | 11β-aryl-gona-4,9-dien-3-ones |
| DE4332283A1 (de) * | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE4332284C2 (de) * | 1993-09-20 | 1997-05-28 | Jenapharm Gmbh | 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US5576310A (en) * | 1994-09-20 | 1996-11-19 | Jenapharm Gmbh | 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds |
-
1993
- 1993-09-20 DE DE4332283A patent/DE4332283A1/de not_active Withdrawn
-
1994
- 1994-07-07 EP EP94250178A patent/EP0648778B1/de not_active Expired - Lifetime
- 1994-07-07 ES ES94250178T patent/ES2108371T3/es not_active Expired - Lifetime
- 1994-07-07 DK DK94250178.4T patent/DK0648778T3/da active
- 1994-07-07 DE DE59403717T patent/DE59403717D1/de not_active Expired - Fee Related
- 1994-07-07 AT AT94250178T patent/ATE156835T1/de not_active IP Right Cessation
- 1994-08-09 FI FI943687A patent/FI113657B/fi active
- 1994-08-09 NO NO942953A patent/NO304989B1/no not_active IP Right Cessation
- 1994-08-10 SK SK957-94A patent/SK280137B6/sk not_active IP Right Cessation
- 1994-08-12 NZ NZ264229A patent/NZ264229A/en not_active IP Right Cessation
- 1994-08-15 CZ CZ19941970A patent/CZ292298B6/cs not_active IP Right Cessation
- 1994-08-18 AU AU70350/94A patent/AU682195B2/en not_active Ceased
- 1994-08-19 CA CA002130516A patent/CA2130516C/en not_active Expired - Lifetime
- 1994-09-19 HU HU9402694A patent/HU223339B1/hu not_active IP Right Cessation
- 1994-09-19 PL PL94305092A patent/PL183181B1/pl not_active IP Right Cessation
- 1994-09-20 JP JP6224379A patent/JP2753562B2/ja not_active Expired - Fee Related
- 1994-09-20 US US08/309,175 patent/US5693628A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU7035094A (en) | 1995-03-30 |
| AU682195B2 (en) | 1997-09-25 |
| PL305092A1 (en) | 1995-04-03 |
| CA2130516C (en) | 2003-04-15 |
| DE4332283A1 (de) | 1995-04-13 |
| CA2130516A1 (en) | 1995-03-21 |
| CZ197094A3 (en) | 1995-04-12 |
| NO304989B1 (no) | 1999-03-15 |
| ATE156835T1 (de) | 1997-08-15 |
| FI943687L (fi) | 1995-03-21 |
| JP2753562B2 (ja) | 1998-05-20 |
| CZ292298B6 (cs) | 2003-09-17 |
| EP0648778A3 (de) | 1995-08-09 |
| FI113657B (fi) | 2004-05-31 |
| FI943687A0 (fi) | 1994-08-09 |
| DE59403717D1 (de) | 1997-09-18 |
| EP0648778B1 (de) | 1997-08-13 |
| HU9402694D0 (en) | 1994-11-28 |
| DK0648778T3 (da) | 1998-03-30 |
| HUT68029A (en) | 1995-05-29 |
| NZ264229A (en) | 1995-04-27 |
| SK280137B6 (sk) | 1999-08-06 |
| NO942953L (no) | 1995-03-21 |
| NO942953D0 (no) | 1994-08-09 |
| HU223339B1 (hu) | 2004-06-28 |
| US5693628A (en) | 1997-12-02 |
| SK95794A3 (en) | 1995-04-12 |
| JPH07149789A (ja) | 1995-06-13 |
| EP0648778A2 (de) | 1995-04-19 |
| PL183181B1 (pl) | 2002-06-28 |
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