JP4845320B2 - (7α,11β)−ジメチル−17β−ヒドロキシ−4−エストレン−3−オンの4−N−ブチルシクロヘキサン酸エステル及びウンデカン酸エステルの製造方法及びそれらの医学用途 - Google Patents

(7α,11β)−ジメチル−17β−ヒドロキシ−4−エストレン−3−オンの4−N−ブチルシクロヘキサン酸エステル及びウンデカン酸エステルの製造方法及びそれらの医学用途 Download PDF

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JP4845320B2
JP4845320B2 JP2001572528A JP2001572528A JP4845320B2 JP 4845320 B2 JP4845320 B2 JP 4845320B2 JP 2001572528 A JP2001572528 A JP 2001572528A JP 2001572528 A JP2001572528 A JP 2001572528A JP 4845320 B2 JP4845320 B2 JP 4845320B2
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compound
dimethyl
bucyclate
undecanoate
hydroxy
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JP2003531119A5 (enExample
JP2003531119A (ja
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ピー. ブライ、リチャード
ケイ. キム、ヒュン
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Government of the United States of America
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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)
  • Veterinary Medicine (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)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2001572528A 2000-03-31 2001-03-30 (7α,11β)−ジメチル−17β−ヒドロキシ−4−エストレン−3−オンの4−N−ブチルシクロヘキサン酸エステル及びウンデカン酸エステルの製造方法及びそれらの医学用途 Expired - Fee Related JP4845320B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US19353000P 2000-03-31 2000-03-31
US60/193,530 2000-03-31
US19444000P 2000-04-04 2000-04-04
US60/194,440 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 (3)

Publication Number Publication Date
JP2003531119A JP2003531119A (ja) 2003-10-21
JP2003531119A5 JP2003531119A5 (enExample) 2008-05-01
JP4845320B2 true JP4845320B2 (ja) 2011-12-28

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JP2001572528A Expired - Fee Related JP4845320B2 (ja) 2000-03-31 2001-03-30 (7α,11β)−ジメチル−17β−ヒドロキシ−4−エストレン−3−オンの4−N−ブチルシクロヘキサン酸エステル及びウンデカン酸エステルの製造方法及びそれらの医学用途

Country Status (8)

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

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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
CA2596884C (en) * 2005-02-04 2013-11-12 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Nandrolone 17.beta.-carbonates
US9517240B2 (en) 2006-09-26 2016-12-13 The Regents Of The University Of California Methods and compositions for cancer prevention and treatment
US20100160275A1 (en) * 2006-09-26 2010-06-24 Lee Eva Y H P 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
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
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
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US11266661B2 (en) 2012-12-21 2022-03-08 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
US11246875B2 (en) 2012-12-21 2022-02-15 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
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
KR20180126582A (ko) 2016-04-01 2018-11-27 쎄러퓨틱스엠디, 인코퍼레이티드 스테로이드 호르몬 약제학적 조성물
WO2017173044A1 (en) 2016-04-01 2017-10-05 Therapeuticsmd Inc. Steroid hormone compositions in medium chain oils
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations
EP4164743A2 (en) * 2020-06-11 2023-04-19 The United States of America, 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

Citations (2)

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JPH01211597A (ja) * 1987-12-12 1989-08-24 Akzo Nv 新規の11−アリールステロイド化合物
WO1999026962A1 (en) * 1997-11-26 1999-06-03 Research Triangle Institute Androgenic steroid compounds and a method 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
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
TW548277B (en) * 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01211597A (ja) * 1987-12-12 1989-08-24 Akzo Nv 新規の11−アリールステロイド化合物
WO1999026962A1 (en) * 1997-11-26 1999-06-03 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same

Also Published As

Publication number Publication date
CA2402524C (en) 2009-11-17
EP1272196B1 (en) 2006-08-02
WO2001074839A2 (en) 2001-10-11
DE60121928D1 (de) 2006-09-14
CA2402524A1 (en) 2001-10-11
AU4966101A (en) 2001-10-15
EP1272196A2 (en) 2003-01-08
ATE334682T1 (de) 2006-08-15
AU2001249661B2 (en) 2005-02-17
US7196074B2 (en) 2007-03-27
DE60121928T2 (de) 2007-03-01
WO2001074839A3 (en) 2002-06-13
US20030130243A1 (en) 2003-07-10
JP2003531119A (ja) 2003-10-21

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