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

11β-ARYL-GONA-4,9-DIEN-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
Application number
PCT/DE1990/000614
Other languages
German (de)
French (fr)
Other versions
WO1991001958A2 (en
Inventor
Helmut Kasch
Gudrun Bertram
Kurt Ponsold
Gerd Schubert
Heidemarie Roehrig
Anatoli Kurischko
Bernd Menzenbach
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/en
Priority claimed from DD33181889A external-priority patent/DD289537A5/en
Priority claimed from DD33340989A external-priority patent/DD299068A5/en
Application filed by Schering Ag filed Critical Schering Ag
Priority to JP51117490A priority Critical patent/JP3202224B2/en
Publication of WO1991001958A2 publication Critical patent/WO1991001958A2/en
Publication of WO1991001958A3 publication Critical patent/WO1991001958A3/en

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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (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)
  • Carbon And Carbon Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)

Abstract

New 11 beta -aryl-gona-4,9-dienes of general formula (I), in which R<1>, R<2>, R<3>, R<4> and R<5> have the meaning given in the derscription, possess a marked antigestagenic activity and are suitable for the manufacture of drugs.
PCT/DE1990/000614 1989-08-04 1990-08-06 11β-ARYL-GONA-4,9-DIEN-3-ONES WO1991001958A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP51117490A JP3202224B2 (en) 1989-08-04 1990-08-06 11β-aryl-gon-4,9-dien-3-ones, process for their preparation and pharmaceutical preparations containing them

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DD33147989A DD290893A5 (en) 1989-08-04 1989-08-04 PROCESS FOR THE PREPARATION OF 11 BETA-ARYL-ESTRA-4,9-DIEN-3-ONES
DDWPC07J/331479/0 1989-08-04
DD33181889A DD289537A5 (en) 1989-08-16 1989-08-16 PROCESS FOR THE PREPARATION OF 11 BETA-ARYL-GONA-4,9-DIENES
DDWPCO7J/331818/3 1989-08-16
DD33340989A DD299068A5 (en) 1989-10-09 1989-10-09 PROCESS FOR PREPARING 11 BETA-ARYL SUBSITUTED 17 BETA-ALKOXY-17 ALPHA -ALKOXYMETHYL-ESTRA-4,9-DIEN-3-ONES
DDWPC07J/333409/5 1989-10-09

Publications (2)

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

Family

ID=27179934

Family Applications (1)

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

Country Status (7)

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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4332284C2 (en) * 1993-09-20 1997-05-28 Jenapharm Gmbh 11-Benzaldoxime-17beta-methoxy-17alpha-methoxymethyl-estradiene derivatives, process for their preparation and medicaments containing these compounds
DE4332283A1 (en) * 1993-09-20 1995-04-13 Jenapharm Gmbh Novel 11-benzaldoximestradiene derivatives, processes for their preparation and medicaments containing these compounds
IL123195A (en) * 1997-02-21 2002-11-10 Akzo Nobel Nv Steroid compounds having contraceptive and anti-osteoporosis activity, their preparation and pharmaceutical compositions containing them
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 (en) * 2006-04-13 2007-10-18 Bayer Schering Pharma Ag 17alpha-substituted 4- (3-oxoestra-4,9-diene-11beta-yl) -benzoic acid, its derivatives and processes for their preparation
EP1862468A1 (en) 2006-06-02 2007-12-05 Bayer Schering Pharma Aktiengesellschaft Crystalline 11beta-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-one
DE102009034362A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-aryl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034367A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-benzylidene derivatives, process for their preparation and their use for the treatment of diseases
DE102009034366A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-methyleneoxyalkylene aryl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034368A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-acyloxyalkylenephenyl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034526A1 (en) 2009-07-21 2011-02-10 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-ethynylphenyl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034525A1 (en) 2009-07-21 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-aryl derivatives, process for their preparation and their use for the treatment of diseases
DE102010007722A1 (en) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesterone receptor antagonist
DE102010007719A1 (en) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesterone receptor antagonist

Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1983003099A1 (en) * 1982-03-01 1983-09-15 Roussel Uclaf 3-keto-delta 4,9-19-norsteroids
EP0097572A1 (en) * 1982-06-11 1984-01-04 Roussel-Uclaf 19-Nor steroids substituted at position 11 and optionally at position 2, their preparation, their utilization as medicaments, compositions containing them and intermediates obtained
EP0104387A1 (en) * 1982-08-24 1984-04-04 Schering Aktiengesellschaft 11-Beta-aryl-17-alpha-alkynyl-17-beta-hydroxy-4,9(10)-estradien-3-one derivatives, their preparation and pharmaceutical compositions containing them
EP0110434A1 (en) * 1981-01-09 1984-06-13 Roussel-Uclaf Steroid intermediates substituted at position 11, and process for their preparation
EP0129499A2 (en) * 1983-06-15 1984-12-27 Schering Aktiengesellschaft 13-Alpha-alkyl gonanes, their preparation and pharmaceutical compositions containing them
EP0135400A2 (en) * 1983-06-14 1985-03-27 Roussel-Uclaf Estradiene derivatives labelled with tritium, their preparation and intermediates for their preparation, and their utilization in the study and in the determination of steroids in biological fluids
EP0147361A2 (en) * 1983-12-22 1985-07-03 Schering Aktiengesellschaft 11-Beta-aryl-estradienes, their preparation and pharmaceutical compositions containing them
GB2160873A (en) * 1984-06-29 1986-01-02 Roussel Uclaf 11B-(4-Aminophenyl) estra-4,9-dienes
EP0184471A1 (en) * 1984-11-29 1986-06-11 Roussel-Uclaf Product containing an antiprogestomimetic and a uterotonic substance
EP0190759A2 (en) * 1985-02-07 1986-08-13 Schering Aktiengesellschaft 11-Beta phenyl gonanes, their preparation and pharmaceutical compositions containing them
FR2586021A1 (en) * 1985-08-09 1987-02-13 Roussel Uclaf New products derived from the structure 5 alpha -OH- DELTA <9(10)>-19-norsteroids
EP0254670A1 (en) * 1986-07-25 1988-01-27 Schering Aktiengesellschaft 11-beta-(4-isopropenylphenyl)-estra-4,9-diene, their preparation and pharmaceutical compositions containing them
EP0277676A1 (en) * 1987-01-23 1988-08-10 Akzo N.V. New ll-aryl steroid derivatives
EP0289073A1 (en) * 1987-04-24 1988-11-02 Akzo N.V. Novel 11-aryloestrane and 11-arylpregnane derivatives
EP0299913A1 (en) * 1987-07-16 1989-01-18 Schering Aktiengesellschaft 11-Beta-phenyl-4,9-15-estratrienes, their preparation and pharmaceutical compositions containing them
EP0305242A1 (en) * 1987-07-30 1989-03-01 Roussel-Uclaf 17-Aryl steroids, their preparation and intermediates for their preparation, their use as medicines and pharmaceutical compositions containing them
EP0308345A1 (en) * 1987-09-18 1989-03-22 Roussel-Uclaf Steroids with a 3,4 or 6 ring members spiro ring at position 17, their preparation, intermediates for their preparation, their use as medicaments and pharmaceutical compositions containing them
EP0321010A1 (en) * 1987-12-12 1989-06-21 Akzo N.V. New 11-arylsteroid compounds
WO1989012448A1 (en) * 1988-06-23 1989-12-28 Research Triangle Institute 11beta-SUBSTITUTED PROGESTERONE ANALOGS

Patent Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110434A1 (en) * 1981-01-09 1984-06-13 Roussel-Uclaf Steroid intermediates substituted at position 11, and process for their preparation
WO1983003099A1 (en) * 1982-03-01 1983-09-15 Roussel Uclaf 3-keto-delta 4,9-19-norsteroids
EP0097572A1 (en) * 1982-06-11 1984-01-04 Roussel-Uclaf 19-Nor steroids substituted at position 11 and optionally at position 2, their preparation, their utilization as medicaments, compositions containing them and intermediates obtained
EP0104387A1 (en) * 1982-08-24 1984-04-04 Schering Aktiengesellschaft 11-Beta-aryl-17-alpha-alkynyl-17-beta-hydroxy-4,9(10)-estradien-3-one derivatives, their preparation and pharmaceutical compositions containing them
EP0135400A2 (en) * 1983-06-14 1985-03-27 Roussel-Uclaf Estradiene derivatives labelled with tritium, their preparation and intermediates for their preparation, and their utilization in the study and in the determination of steroids in biological fluids
EP0129499A2 (en) * 1983-06-15 1984-12-27 Schering Aktiengesellschaft 13-Alpha-alkyl gonanes, their preparation and pharmaceutical compositions containing them
EP0147361A2 (en) * 1983-12-22 1985-07-03 Schering Aktiengesellschaft 11-Beta-aryl-estradienes, their preparation and pharmaceutical compositions containing them
GB2160873A (en) * 1984-06-29 1986-01-02 Roussel Uclaf 11B-(4-Aminophenyl) estra-4,9-dienes
EP0184471A1 (en) * 1984-11-29 1986-06-11 Roussel-Uclaf Product containing an antiprogestomimetic and a uterotonic substance
EP0190759A2 (en) * 1985-02-07 1986-08-13 Schering Aktiengesellschaft 11-Beta phenyl gonanes, their preparation and pharmaceutical compositions containing them
FR2586021A1 (en) * 1985-08-09 1987-02-13 Roussel Uclaf New products derived from the structure 5 alpha -OH- DELTA <9(10)>-19-norsteroids
EP0254670A1 (en) * 1986-07-25 1988-01-27 Schering Aktiengesellschaft 11-beta-(4-isopropenylphenyl)-estra-4,9-diene, their preparation and pharmaceutical compositions containing them
EP0277676A1 (en) * 1987-01-23 1988-08-10 Akzo N.V. New ll-aryl steroid derivatives
EP0289073A1 (en) * 1987-04-24 1988-11-02 Akzo N.V. Novel 11-aryloestrane and 11-arylpregnane derivatives
EP0299913A1 (en) * 1987-07-16 1989-01-18 Schering Aktiengesellschaft 11-Beta-phenyl-4,9-15-estratrienes, their preparation and pharmaceutical compositions containing them
EP0305242A1 (en) * 1987-07-30 1989-03-01 Roussel-Uclaf 17-Aryl steroids, their preparation and intermediates for their preparation, their use as medicines and pharmaceutical compositions containing them
EP0308345A1 (en) * 1987-09-18 1989-03-22 Roussel-Uclaf Steroids with a 3,4 or 6 ring members spiro ring at position 17, their preparation, intermediates for their preparation, their use as medicaments and pharmaceutical compositions containing them
EP0321010A1 (en) * 1987-12-12 1989-06-21 Akzo N.V. New 11-arylsteroid compounds
WO1989012448A1 (en) * 1988-06-23 1989-12-28 Research Triangle Institute 11beta-SUBSTITUTED PROGESTERONE ANALOGS

Also Published As

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

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