DK1272505T3 - 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater - Google Patents

8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater

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Publication number
DK1272505T3
DK1272505T3 DK01940331T DK01940331T DK1272505T3 DK 1272505 T3 DK1272505 T3 DK 1272505T3 DK 01940331 T DK01940331 T DK 01940331T DK 01940331 T DK01940331 T DK 01940331T DK 1272505 T3 DK1272505 T3 DK 1272505T3
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Prior art keywords
sup
8beta
11beta
substituted
compounds
Prior art date
Application number
DK01940331T
Other languages
English (en)
Inventor
Alexander Hillisch
Karl-Heinrich Fritzemeier
Olaf Peters
Nico Braeuer
Christa Hegele-Hartung
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 DE10019167A external-priority patent/DE10019167A1/de
Application filed by Schering Ag filed Critical Schering Ag
Application granted granted Critical
Publication of DK1272505T3 publication Critical patent/DK1272505T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P13/08Drugs for disorders of the urinary system of the prostate
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0062Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic

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  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DK01940331T 2000-04-12 2001-04-12 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater DK1272505T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10019167A DE10019167A1 (de) 2000-04-12 2000-04-12 Substituierte Estratriene als selektiv wirksame Estrogene
US20737000P 2000-05-26 2000-05-26

Publications (1)

Publication Number Publication Date
DK1272505T3 true DK1272505T3 (da) 2005-11-07

Family

ID=26005365

Family Applications (2)

Application Number Title Priority Date Filing Date
DK01931609T DK1272504T3 (da) 2000-04-12 2001-04-12 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener
DK01940331T DK1272505T3 (da) 2000-04-12 2001-04-12 8beta-substituerede-11beta-pentyl- og 11beta-hexyl-estra-1,3,5(10)-trienderivater

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DK01931609T DK1272504T3 (da) 2000-04-12 2001-04-12 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener

Country Status (25)

Country Link
US (3) US7378404B2 (da)
EP (2) EP1272504B1 (da)
JP (2) JP3828423B2 (da)
CN (1) CN100453549C (da)
AT (2) ATE363487T1 (da)
AU (3) AU5834101A (da)
BG (1) BG107173A (da)
BR (1) BR0109983A (da)
CA (1) CA2406177C (da)
CZ (1) CZ20023382A3 (da)
DE (1) DE50112561D1 (da)
DK (2) DK1272504T3 (da)
EA (1) EA006299B1 (da)
EE (1) EE200200589A (da)
ES (2) ES2287127T3 (da)
HR (1) HRP20020892B1 (da)
HU (1) HUP0300335A2 (da)
IL (2) IL152248A0 (da)
MX (1) MXPA02010066A (da)
NO (2) NO325337B1 (da)
NZ (1) NZ543724A (da)
PL (1) PL207488B1 (da)
PT (1) PT1272504E (da)
SK (1) SK14632002A3 (da)
WO (2) WO2001077138A1 (da)

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DE10039199A1 (de) * 2000-08-10 2002-02-21 Schering Ag Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen
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DE10226326A1 (de) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
DE60323938D1 (de) * 2003-03-27 2008-11-20 Pantarhei Bioscience Bv Verwendung von Estrogenen zur Behandlung von Männerunfruchtbarkeit
DE10318896A1 (de) 2003-04-22 2004-11-25 Schering Ag 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene
ES2307064T3 (es) * 2003-11-26 2008-11-16 Bayer Schering Pharma Aktiengesellschaft Prevencion y tratamiento de enfermedades cardiacas hipertensivas por los estrogenos selectivos 8beta-vinil-estra-1,3,5(10)-trien-3,17beta-diol y 17beta-fluor-9alfa-vinil-estra-1,3,5(10)-trien-3,16alfa-diol.
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057225A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
DE102005057224A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
EP2014672A1 (en) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft 8-beta-substituted estratrienes as selectively active estrogens
NZ586666A (en) * 2008-02-13 2012-04-27 Bayer Schering Pharma Ag Estradiol-containing drug delivery system
EA018330B1 (ru) * 2008-02-13 2013-07-30 Байер Интеллекчуал Проперти Гмбх Система доставки лекарственного средства со стабилизирующим эффектом
EP2143432A1 (en) 2008-07-11 2010-01-13 Bayer Schering Pharma AG 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer
WO2010057594A1 (en) * 2008-11-21 2010-05-27 Bayer Schering Pharma Aktiengesellschaft Drug delivery system
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
BR112014012444B1 (pt) 2011-11-23 2021-12-14 Therapeuticsmd, Inc Composição farmacêutica compreendendo estradiol solubilizado, progesterona e um agente de solubilização, bem como usos desta para tratar um sintoma relacionado à menopausa em uma mulher
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US20130338122A1 (en) 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
RU2016143081A (ru) 2014-05-22 2018-06-26 Терапьютиксмд, Инк. Натуральные комбинированные гормонозаместительные составы и терапии
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
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ES2287127T3 (es) 2007-12-16
EP1272504A1 (de) 2003-01-08
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ES2245694T3 (es) 2006-01-16
NO325337B1 (no) 2008-03-31
WO2001077139A1 (de) 2001-10-18
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ATE302790T1 (de) 2005-09-15
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