KR102048457B1 - 6-치환된 에스트라디올 유도체 및 사용 방법 - Google Patents

6-치환된 에스트라디올 유도체 및 사용 방법 Download PDF

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Publication number
KR102048457B1
KR102048457B1 KR1020187023922A KR20187023922A KR102048457B1 KR 102048457 B1 KR102048457 B1 KR 102048457B1 KR 1020187023922 A KR1020187023922 A KR 1020187023922A KR 20187023922 A KR20187023922 A KR 20187023922A KR 102048457 B1 KR102048457 B1 KR 102048457B1
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hydrogen
alkyl
compounds
halo
compound
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KR20180095742A (ko
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제임스 지. 야거
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엔디씨, 엘엘씨
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    • 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
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • 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
    • C07J41/0044—Normal 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/06—Animal cells or tissues; Human cells or tissues
    • C12N5/0602—Vertebrate cells
    • C12N5/0693—Tumour cells; Cancer cells
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2501/00—Active agents used in cell culture processes, e.g. differentation
    • C12N2501/30—Hormones
    • C12N2501/38—Hormones with nuclear receptors
    • C12N2501/39—Steroid hormones
    • C12N2501/392—Sexual 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)
KR1020187023922A 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법 Expired - Fee Related KR102048457B1 (ko)

Applications Claiming Priority (3)

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
PCT/US2010/058342 WO2011066542A2 (en) 2009-11-30 2010-11-30 6-substituted estradiol derivatives and methods of use

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020127017044A Division KR20120095461A (ko) 2009-11-30 2010-11-30 6-치환된 에스트라디올 유도체 및 사용 방법

Publications (2)

Publication Number Publication Date
KR20180095742A KR20180095742A (ko) 2018-08-27
KR102048457B1 true KR102048457B1 (ko) 2019-11-25

Family

ID=44067274

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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 After (1)

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KR1020127017044A Ceased KR20120095461A (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
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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

Citations (1)

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Publication number Priority date Publication date Assignee Title
US20080312202A1 (en) * 2005-09-30 2008-12-18 James Yarger 6-substituted estradiol derivatives and methods of use

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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
KR20120095461A (ko) 2012-08-28
AU2016238850A1 (en) 2016-10-20
KR20180095742A (ko) 2018-08-27
MX2012006169A (es) 2012-11-12
EP2507253A4 (en) 2013-05-22
WO2011066542A3 (en) 2011-10-20

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