DE60121928T2 - Verfahren zur herstellung von den trans-4-n-butylcyclohexanoicsaüre- und undecanoicsaüreestern von (7-alpha,11-beta)-dimethyl-17 beta -hydroxy-4-estren-3-one und deren medizynische anwendung - Google Patents

Verfahren zur herstellung von den trans-4-n-butylcyclohexanoicsaüre- und undecanoicsaüreestern von (7-alpha,11-beta)-dimethyl-17 beta -hydroxy-4-estren-3-one und deren medizynische anwendung Download PDF

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Publication number
DE60121928T2
DE60121928T2 DE60121928T DE60121928T DE60121928T2 DE 60121928 T2 DE60121928 T2 DE 60121928T2 DE 60121928 T DE60121928 T DE 60121928T DE 60121928 T DE60121928 T DE 60121928T DE 60121928 T2 DE60121928 T2 DE 60121928T2
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dimethyl
bucyclate
compound
hydroxy
estrene
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Expired - Lifetime
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DE60121928T
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German (de)
English (en)
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DE60121928D1 (de
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P. Richard Highland BLYE
K. Hyun Bethesda KIM
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US Department of Health and Human Services
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US Department of Health and Human Services
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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06Anabolic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P5/30Oestrogens
    • 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
    • C07J1/0066Estrane 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
    • 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
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/006Ketals at position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
DE60121928T 2000-03-31 2001-03-30 Verfahren zur herstellung von den trans-4-n-butylcyclohexanoicsaüre- und undecanoicsaüreestern von (7-alpha,11-beta)-dimethyl-17 beta -hydroxy-4-estren-3-one und deren medizynische anwendung Expired - Lifetime DE60121928T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US19353000P 2000-03-31 2000-03-31
US193530P 2000-03-31
US19444000P 2000-04-04 2000-04-04
US194440P 2000-04-04
PCT/US2001/010293 WO2001074839A2 (en) 2000-03-31 2001-03-30 Methods of making the 4-n-butylcyclohexanoic and the undecanoic acid esters of (7 alpha, 11 beta)-dimethyl-17 beta-hydroxy-4-estren-3-one and their medical use

Publications (2)

Publication Number Publication Date
DE60121928D1 DE60121928D1 (de) 2006-09-14
DE60121928T2 true DE60121928T2 (de) 2007-03-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
DE60121928T Expired - Lifetime DE60121928T2 (de) 2000-03-31 2001-03-30 Verfahren zur herstellung von den trans-4-n-butylcyclohexanoicsaüre- und undecanoicsaüreestern von (7-alpha,11-beta)-dimethyl-17 beta -hydroxy-4-estren-3-one und deren medizynische anwendung

Country Status (8)

Country Link
US (1) US7196074B2 (https=)
EP (1) EP1272196B1 (https=)
JP (1) JP4845320B2 (https=)
AT (1) ATE334682T1 (https=)
AU (2) AU2001249661B2 (https=)
CA (1) CA2402524C (https=)
DE (1) DE60121928T2 (https=)
WO (1) WO2001074839A2 (https=)

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* Cited by examiner, † Cited by third party
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US5952319A (en) 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
US20030069215A1 (en) * 2001-03-30 2003-04-10 The Government Of The United States Of America, Methods of making and using 7a,11b-dimethyl-17b-hydroxy-4-estren-3-one 17b-trans-4-n-butylcyclohexane carboxylate and 7a,11b-dimethyl-17b-hydroxyestr-4-en-3-one 17-undecanoate
GB0025221D0 (en) * 2000-10-14 2000-11-29 Astrazeneca Ab New process
AU2006211907B2 (en) * 2005-02-04 2011-09-08 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Nandrolone 17beta-carbonates
WO2008039482A2 (en) * 2006-09-26 2008-04-03 The Regents Of The University Of California Methods and compositions for cancer prevention and treatment
US9517240B2 (en) 2006-09-26 2016-12-13 The Regents Of The University Of California Methods and compositions for cancer prevention and treatment
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
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
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
US10806697B2 (en) 2012-12-21 2020-10-20 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
US10568891B2 (en) 2012-12-21 2020-02-25 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
US10537581B2 (en) 2012-12-21 2020-01-21 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
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10050658B2 (en) 2014-02-24 2018-08-14 National Products, Inc. Docking sleeve with electrical adapter
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
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
US9931349B2 (en) 2016-04-01 2018-04-03 Therapeuticsmd, Inc. Steroid hormone pharmaceutical composition
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations
US20230227492A1 (en) * 2020-06-11 2023-07-20 The Usa As Represented By The Secretary, Department Of Health And Human Services Monomeric and oligomeric compound embodiments as contraceptives and therapies and methods of making and using the same

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US2837517A (en) * 1955-08-08 1958-06-03 Upjohn Co 9, 11beta-epoxy-17-alkyltestosterones
US3160644A (en) * 1955-08-08 1964-12-08 Upjohn Co 1-dehydro-11-keto-9alpha-fluoro-17alpha-methyl testosterones
US2806863A (en) * 1956-03-19 1957-09-17 Upjohn Co 9alpha-halo-11beta, 17beta-dihydroxy-17alpha-methylandrostane-3-ones
US3438783A (en) * 1965-08-16 1969-04-15 Monsanto Co Improving egg quality in poultry by orally administering androgens
US3577410A (en) 1968-07-30 1971-05-04 American Home Prod 13beta-alkyl-17-hydroxygona-4,14-dien-3-ones
DE2031849C3 (de) 1970-06-27 1978-11-16 Bosch Gmbh Robert Flüssigkeitsdichte Verbindung eines Deckels aus thermoplastischem Material mit einem Kasten aus thermoplastischem Material
ZA712312B (en) 1970-04-28 1972-01-26 Ochsner Med Found Alton 4,14-estradiene compounds
IL36628A (en) 1970-04-28 1978-08-31 Ochsner Med Found Alton 4, 14-estradiene compounds and processes for their preparation
ES2053714T3 (es) * 1987-12-12 1994-08-01 Akzo Nv Proceso para la preparacion de 11-arilesteroides.
FR2747680B1 (fr) * 1996-04-18 1998-07-03 Roussel Uclaf Nouveaux steroides, leur application a titre de medicaments, leur procede de preparation, les intermediaires de ce procede et les compositions pharmaceutiques les renfermant
DE19619045C1 (de) 1996-05-02 1997-11-13 Jenapharm Gmbh Verwendung von Kombinationspräparaten zur Behandlung hypogonadaler Männer sowie Männern mit Hypophysenerkrankungen
US5952319A (en) * 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
TW548277B (en) 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens

Also Published As

Publication number Publication date
AU2001249661B2 (en) 2005-02-17
WO2001074839A2 (en) 2001-10-11
EP1272196A2 (en) 2003-01-08
CA2402524A1 (en) 2001-10-11
JP4845320B2 (ja) 2011-12-28
WO2001074839A3 (en) 2002-06-13
CA2402524C (en) 2009-11-17
US20030130243A1 (en) 2003-07-10
JP2003531119A (ja) 2003-10-21
ATE334682T1 (de) 2006-08-15
DE60121928D1 (de) 2006-09-14
AU4966101A (en) 2001-10-15
US7196074B2 (en) 2007-03-27
EP1272196B1 (en) 2006-08-02

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