KR20120095461A - 6-치환된 에스트라디올 유도체 및 사용 방법 - Google Patents

6-치환된 에스트라디올 유도체 및 사용 방법 Download PDF

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Publication number
KR20120095461A
KR20120095461A KR1020127017044A KR20127017044A KR20120095461A KR 20120095461 A KR20120095461 A KR 20120095461A KR 1020127017044 A KR1020127017044 A KR 1020127017044A KR 20127017044 A KR20127017044 A KR 20127017044A KR 20120095461 A KR20120095461 A KR 20120095461A
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South Korea
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methyl
hydrogen
alkyl
cyclopenta
alkenyl
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KR1020127017044A
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English (en)
Korean (ko)
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제임스 지. 야거
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엔디씨, 엘엘씨
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Publication of KR20120095461A publication Critical patent/KR20120095461A/ko
Ceased legal-status Critical Current

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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
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07J41/0044Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/06Animal cells or tissues; Human cells or tissues
    • C12N5/0602Vertebrate cells
    • C12N5/0693Tumour cells; Cancer cells
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2501/00Active agents used in cell culture processes, e.g. differentation
    • C12N2501/30Hormones
    • C12N2501/38Hormones with nuclear receptors
    • C12N2501/39Steroid hormones
    • C12N2501/392Sexual steroids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020127017044A 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법 Ceased KR20120095461A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12/627,874 2009-11-30
US12/627,874 US10174070B2 (en) 2005-09-30 2009-11-30 6-substituted estradiol derivatives and methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020187023922A Division KR102048457B1 (ko) 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법

Publications (1)

Publication Number Publication Date
KR20120095461A true KR20120095461A (ko) 2012-08-28

Family

ID=44067274

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020187023922A Expired - Fee Related KR102048457B1 (ko) 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법
KR1020127017044A Ceased KR20120095461A (ko) 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법

Family Applications Before (1)

Application Number Title Priority Date Filing Date
KR1020187023922A Expired - Fee Related KR102048457B1 (ko) 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법

Country Status (12)

Country Link
US (2) US10174070B2 (enExample)
EP (1) EP2507253B1 (enExample)
JP (1) JP5898625B2 (enExample)
KR (2) KR102048457B1 (enExample)
CN (1) CN102753564B (enExample)
AU (3) AU2010324632A1 (enExample)
CA (1) CA2781627C (enExample)
DK (1) DK2507253T3 (enExample)
ES (1) ES2568941T3 (enExample)
MX (1) MX342436B (enExample)
SG (1) SG181126A1 (enExample)
WO (1) WO2011066542A2 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
WO2012037261A2 (en) * 2010-09-14 2012-03-22 Endece, Llc 6-substituted demethyl-estradiol derivatives as er-beta agonists
SG193380A1 (en) * 2011-03-21 2013-10-30 Endece Llc 6-substituted estradiol derivatives for use in remyelination of nerve axons
EP2688901B1 (en) * 2011-03-25 2019-05-08 Université Laval INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10
CA2909418A1 (en) * 2013-04-18 2014-10-23 Xi'an Libang Pharmaceutical Technology Co., Ltd. Ester derivative of 7-.alpha.-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)n onyl]-estra-1,3,5(10)-triene-3,17.beta.-diol having anticancer activity and preparation method thereof
MX2016012045A (es) * 2014-03-19 2017-01-19 Endece Llc Derivados de estradiol 6-sustituido para el tratamiento de la enfermedad de alzheimer.
CN114644673B (zh) * 2020-12-19 2023-12-26 上海喀露蓝科技有限公司 一种雌二醇衍生物、其制备方法及其在医药上的用途
CN113956321B (zh) * 2021-10-22 2023-11-03 郑州安图生物工程股份有限公司 雌二醇6位葡萄糖醛酸苷及其制备方法和应用
CN117264008A (zh) * 2022-06-15 2023-12-22 中国科学院大连化学物理研究所 一种化合物及应用和抑制剂与药物
CN115505019B (zh) * 2022-11-07 2024-01-26 南宁师范大学 7-酰胺取代雌甾类化合物及其制备方法和应用

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GB853012A (en) 1958-06-26 1960-11-02 British Drug Houses Ltd 1:6-dimethyl aromatic steroids and the preparation thereof
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NL122154C (enExample) 1963-10-18
US3377363A (en) 1966-04-13 1968-04-09 Abbott Lab delta5(10)-6-hydroxymethyl-estrene compounds
DE1906716A1 (de) 1969-02-06 1970-08-20 Schering Ag 6,7-Disubstituierte OEstratriene
DK290774A (enExample) 1973-06-08 1975-02-03 Schering Ag
DE2832606A1 (de) 1978-07-21 1980-01-31 Schering Ag Verfahren zur herstellung von 7 alpha -methyl-oestrogenen
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GB8517360D0 (en) 1985-07-09 1985-08-14 Erba Farmitalia Substituted androsta-1,4-diene-3,17-diones
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GB8615092D0 (en) 1986-06-20 1986-07-23 Erba Farmitalia Androst-4-ene-317-diones
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DE19633349A1 (de) 1996-08-19 1998-02-26 Sigma Tau Ind Farmaceuti Neue 6-Hydroxy- und 6-Oxo-androstan-Derivate, die auf das kardiovaskuläre System wirken und pharmazeutische Zusammensetzungen, die diese enthalten
KR20010074814A (ko) 1998-08-11 2001-08-09 추후제출 항진균제로서 에스트로겐 화합물의 용도
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WO2012037261A2 (en) 2010-09-14 2012-03-22 Endece, Llc 6-substituted demethyl-estradiol derivatives as er-beta agonists

Also Published As

Publication number Publication date
AU2010324632A1 (en) 2012-06-14
US20100130463A1 (en) 2010-05-27
ES2568941T3 (es) 2016-05-05
US10723757B2 (en) 2020-07-28
EP2507253B1 (en) 2016-03-30
US10174070B2 (en) 2019-01-08
JP5898625B2 (ja) 2016-04-06
US20190135853A1 (en) 2019-05-09
CA2781627A1 (en) 2011-06-03
AU2018203658A1 (en) 2018-06-14
DK2507253T3 (en) 2016-07-04
CN102753564B (zh) 2017-04-05
MX342436B (es) 2016-09-29
EP2507253A2 (en) 2012-10-10
SG181126A1 (en) 2012-07-30
CA2781627C (en) 2017-02-28
WO2011066542A2 (en) 2011-06-03
JP2013512260A (ja) 2013-04-11
CN102753564A (zh) 2012-10-24
AU2016238850A1 (en) 2016-10-20
KR102048457B1 (ko) 2019-11-25
KR20180095742A (ko) 2018-08-27
MX2012006169A (es) 2012-11-12
EP2507253A4 (en) 2013-05-22
WO2011066542A3 (en) 2011-10-20

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