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WO1991001958A3 - 11β-ARYL-GONA-4,9-DIENE-3-ONES - Google Patents

11β-ARYL-GONA-4,9-DIENE-3-ONES Download PDF

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Publication number
WO1991001958A3
WO1991001958A3 PCT/DE1990/000614 DE9000614W WO9101958A3 WO 1991001958 A3 WO1991001958 A3 WO 1991001958A3 DE 9000614 W DE9000614 W DE 9000614W WO 9101958 A3 WO9101958 A3 WO 9101958A3
Authority
WO
WIPO (PCT)
Prior art keywords
gona
aryl
dien
ones
derscription
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.)
Ceased
Application number
PCT/DE1990/000614
Other languages
German (de)
English (en)
Other versions
WO1991001958A2 (fr
Inventor
Helmut Kasch
Gudrun Bertram
Kurt Ponsold
Gerd Schubert
Heidemarie Roehrig
Anatoli Kurischko
Bernd Menzenbach
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
Original Assignee
Schering 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
Priority claimed from DD33147989A external-priority patent/DD290893A5/de
Priority claimed from DD33181889A external-priority patent/DD289537A5/de
Priority claimed from DD33340989A external-priority patent/DD299068A5/de
Application filed by Schering AG filed Critical Schering AG
Priority to JP51117490A priority Critical patent/JP3202224B2/ja
Publication of WO1991001958A2 publication Critical patent/WO1991001958A2/fr
Publication of WO1991001958A3 publication Critical patent/WO1991001958A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P5/36—Antigestagens
    • 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
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0092—Alkenyl derivatives
    • 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
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Luminescent Compositions (AREA)
  • Die Bonding (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Powder Metallurgy (AREA)
  • Holo Graphy (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Carbon And Carbon Compounds (AREA)

Abstract

De nouveaux 11β-aryl-gona-4,9-diènes de formule générale (I), dans laquelle R?1, R2, R3, R4 et R5¿ ont la notation donnée dans la description, possèdent une activité antigestagénique marquée et se prêtent à la fabrication de médicaments.
PCT/DE1990/000614 1989-08-04 1990-08-06 11β-ARYL-GONA-4,9-DIENE-3-ONES Ceased WO1991001958A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP51117490A JP3202224B2 (ja) 1989-08-04 1990-08-06 １１β―アリール―ゴナ―４，９―ジエン―３―オン、その製造方法及びそれを含有する調剤学的調製剤

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DDWPC07J/331479/0 1989-08-04
DD33147989A DD290893A5 (de) 1989-08-04 1989-08-04 Verfahren zur herstellung von 11 beta-aryl-estra-4,9-dien-3-onen
DD33181889A DD289537A5 (de) 1989-08-16 1989-08-16 Verfahren zur herstellung von 11 beta-aryl-gona-4,9-dienen
DDWPCO7J/331818/3 1989-08-16
DD33340989A DD299068A5 (de) 1989-10-09 1989-10-09 Verfahren zur herstellung von 11 beta-arylsubstituierten 17 beta-alkoxy-17 alpha -alkoxymethyl-estra-4,9-dien-3-onen
DDWPC07J/333409/5 1989-10-09

Publications (2)

Publication Number Publication Date
WO1991001958A2 WO1991001958A2 (fr) 1991-02-21
WO1991001958A3 true WO1991001958A3 (fr) 1991-12-12

Family

ID=27179934

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE1990/000614 Ceased WO1991001958A2 (fr) 1989-08-04 1990-08-06 11β-ARYL-GONA-4,9-DIENE-3-ONES

Country Status (7)

Country Link
EP (1) EP0411733B1 (fr)
JP (1) JP3202224B2 (fr)
AT (1) ATE172469T1 (fr)
DE (1) DE59010853D1 (fr)
DK (1) DK0411733T3 (fr)
ES (1) ES2127181T3 (fr)
WO (1) WO1991001958A2 (fr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL118974A (en) * 1995-08-17 2001-09-13 Akzo Nobel Nv History 11 - (Transformed Phenyl) - Astra - 4, 9 - Diane, their preparation and pharmaceutical preparations containing them
TW403736B (en) * 1997-02-21 2000-09-01 Akzo Nobel Nv Steroid compounds having contraceptive and anti-osteoporosis activity
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US5962444A (en) * 1998-05-29 1999-10-05 Research Triangle Institute 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6262042B1 (en) 1998-05-29 2001-07-17 Research Triangle Institute 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6172052B1 (en) 1998-12-04 2001-01-09 Research Triangle Institute 17β-acyl-17α-propynyl-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
DE102006018869A1 (de) * 2006-04-13 2007-10-18 Bayer Schering Pharma Ag 17alpha-substituierte 4-(3-Oxoestra-4,9-dien-11beta-yl)-benzoesäure, deren Derivate und Verfahren zu ihrer Herstellung
EP1862468A1 (fr) 2006-06-02 2007-12-05 Bayer Schering Pharma Aktiengesellschaft 11beta-(4-Acetylphenyle)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-one crystalline
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
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

Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1983003099A1 (fr) * 1982-03-01 1983-09-15 Roussel Uclaf 3-ceto-delta 4,9-19-norsteroides
EP0097572A1 (fr) * 1982-06-11 1984-01-04 Roussel-Uclaf Nouveaux 19-nor stéroides substitués en 11 et éventuellement en 2,leur préparation, leur application comme médicaments, les compositions les renfermant et les nouveaux intermédiaires obtenus
EP0104387A1 (fr) * 1982-08-24 1984-04-04 Schering Aktiengesellschaft Dérivés du 11-bêta-aryle-17-alpha-alcynyle-17-bêta-hydroxy-4,9(10)-estradiène-3-one, leur préparation et compositions pharmaceutiques les contenant
EP0110434A1 (fr) * 1981-01-09 1984-06-13 Roussel-Uclaf Nouveaux produits intermédiaires stéroides substitués en 11-beta et procédé de préparation de ces produits
EP0129499A2 (fr) * 1983-06-15 1984-12-27 Schering Aktiengesellschaft 13-Alpha alcoyle-gonanes, leur préparation et préparations pharmaceutiques les contenant
EP0135400A2 (fr) * 1983-06-14 1985-03-27 Roussel-Uclaf Dérivés estradiéniques radioactifs marqués au tritium, leur procédé et leurs intermédiaires de préparation et leur application pour l'étude et le dosage radioimmunologique de stéroides dans les fluides biologiques
EP0147361A2 (fr) * 1983-12-22 1985-07-03 Schering Aktiengesellschaft 11-Bêta-aryl-estradiènes, leur préparation et compositions pharmaceutiques les contenant
GB2160873A (en) * 1984-06-29 1986-01-02 Roussel Uclaf 11B-(4-Aminophenyl) estra-4,9-dienes
EP0184471A1 (fr) * 1984-11-29 1986-06-11 Roussel-Uclaf Produit comprenant une substance antiprogestomimétique et une substance utérotonique
EP0190759A2 (fr) * 1985-02-07 1986-08-13 Schering Aktiengesellschaft 11 Bêta-phényl gonanes, leur préparation et compositions pharmaceutiques les contenant
FR2586021A1 (fr) * 1985-08-09 1987-02-13 Roussel Uclaf Nouveaux produits derives de la structure 5a-oh d 9(10) 19-nor steroides
EP0254670A1 (fr) * 1986-07-25 1988-01-27 Schering Aktiengesellschaft 11-Bêta-(4-isopropenylphényl)-estra-4,9-diène, leur préparation et compositions pharmaceutiques les contenant
EP0277676A1 (fr) * 1987-01-23 1988-08-10 Akzo N.V. Dérivés de 11-aryl stéroides
EP0289073A1 (fr) * 1987-04-24 1988-11-02 Akzo N.V. Dérivés de 11-arylestranes et 11-arylprégnanes
EP0299913A1 (fr) * 1987-07-16 1989-01-18 Schering Aktiengesellschaft 11 Bêta-phényl-estra-4,9-15-triènes, leur préparation et compositions pharmaceutiques les contenant
EP0305242A1 (fr) * 1987-07-30 1989-03-01 Roussel-Uclaf Nouveaux 17-aryle stéroides, leur procédé et intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant
EP0308345A1 (fr) * 1987-09-18 1989-03-22 Roussel-Uclaf Nouveaux stéroides comportant un cycle spirannique à 3, 4 ou 6 chaînons en position 17, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant
EP0321010A1 (fr) * 1987-12-12 1989-06-21 Akzo N.V. Dérivés de 11-aryl stéroides
WO1989012448A1 (fr) * 1988-06-23 1989-12-28 Research Triangle Institute ANALOGUES DE PROGESTERONE A SUBSTITUTION 11beta

Patent Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110434A1 (fr) * 1981-01-09 1984-06-13 Roussel-Uclaf Nouveaux produits intermédiaires stéroides substitués en 11-beta et procédé de préparation de ces produits
WO1983003099A1 (fr) * 1982-03-01 1983-09-15 Roussel Uclaf 3-ceto-delta 4,9-19-norsteroides
EP0097572A1 (fr) * 1982-06-11 1984-01-04 Roussel-Uclaf Nouveaux 19-nor stéroides substitués en 11 et éventuellement en 2,leur préparation, leur application comme médicaments, les compositions les renfermant et les nouveaux intermédiaires obtenus
EP0104387A1 (fr) * 1982-08-24 1984-04-04 Schering Aktiengesellschaft Dérivés du 11-bêta-aryle-17-alpha-alcynyle-17-bêta-hydroxy-4,9(10)-estradiène-3-one, leur préparation et compositions pharmaceutiques les contenant
EP0135400A2 (fr) * 1983-06-14 1985-03-27 Roussel-Uclaf Dérivés estradiéniques radioactifs marqués au tritium, leur procédé et leurs intermédiaires de préparation et leur application pour l'étude et le dosage radioimmunologique de stéroides dans les fluides biologiques
EP0129499A2 (fr) * 1983-06-15 1984-12-27 Schering Aktiengesellschaft 13-Alpha alcoyle-gonanes, leur préparation et préparations pharmaceutiques les contenant
EP0147361A2 (fr) * 1983-12-22 1985-07-03 Schering Aktiengesellschaft 11-Bêta-aryl-estradiènes, leur préparation et compositions pharmaceutiques les contenant
GB2160873A (en) * 1984-06-29 1986-01-02 Roussel Uclaf 11B-(4-Aminophenyl) estra-4,9-dienes
EP0184471A1 (fr) * 1984-11-29 1986-06-11 Roussel-Uclaf Produit comprenant une substance antiprogestomimétique et une substance utérotonique
EP0190759A2 (fr) * 1985-02-07 1986-08-13 Schering Aktiengesellschaft 11 Bêta-phényl gonanes, leur préparation et compositions pharmaceutiques les contenant
FR2586021A1 (fr) * 1985-08-09 1987-02-13 Roussel Uclaf Nouveaux produits derives de la structure 5a-oh d 9(10) 19-nor steroides
EP0254670A1 (fr) * 1986-07-25 1988-01-27 Schering Aktiengesellschaft 11-Bêta-(4-isopropenylphényl)-estra-4,9-diène, leur préparation et compositions pharmaceutiques les contenant
EP0277676A1 (fr) * 1987-01-23 1988-08-10 Akzo N.V. Dérivés de 11-aryl stéroides
EP0289073A1 (fr) * 1987-04-24 1988-11-02 Akzo N.V. Dérivés de 11-arylestranes et 11-arylprégnanes
EP0299913A1 (fr) * 1987-07-16 1989-01-18 Schering Aktiengesellschaft 11 Bêta-phényl-estra-4,9-15-triènes, leur préparation et compositions pharmaceutiques les contenant
EP0305242A1 (fr) * 1987-07-30 1989-03-01 Roussel-Uclaf Nouveaux 17-aryle stéroides, leur procédé et intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant
EP0308345A1 (fr) * 1987-09-18 1989-03-22 Roussel-Uclaf Nouveaux stéroides comportant un cycle spirannique à 3, 4 ou 6 chaînons en position 17, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant
EP0321010A1 (fr) * 1987-12-12 1989-06-21 Akzo N.V. Dérivés de 11-aryl stéroides
WO1989012448A1 (fr) * 1988-06-23 1989-12-28 Research Triangle Institute ANALOGUES DE PROGESTERONE A SUBSTITUTION 11beta

Also Published As

Publication number Publication date
EP0411733A3 (en) 1992-01-22
WO1991001958A2 (fr) 1991-02-21
ATE172469T1 (de) 1998-11-15
EP0411733B1 (fr) 1998-10-21
DE59010853D1 (de) 1998-12-03
ES2127181T3 (es) 1999-04-16
DK0411733T3 (da) 1999-06-28
JP3202224B2 (ja) 2001-08-27
EP0411733A2 (fr) 1991-02-06
JPH05504759A (ja) 1993-07-22

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