CN102753564B - 6‑取代的雌二醇衍生物及其使用方法 - Google Patents

6‑取代的雌二醇衍生物及其使用方法 Download PDF

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Publication number
CN102753564B
CN102753564B CN201080059521.4A CN201080059521A CN102753564B CN 102753564 B CN102753564 B CN 102753564B CN 201080059521 A CN201080059521 A CN 201080059521A CN 102753564 B CN102753564 B CN 102753564B
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cancer
compound
compounds
methyl
phenanthrene
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Expired - Fee Related
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Chinese (zh)
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CN102753564A (zh
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J·G·雅格尔
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Endece LLC
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Endece LLC
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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)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • General Engineering & Computer Science (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201080059521.4A 2009-11-30 2010-11-30 6‑取代的雌二醇衍生物及其使用方法 Expired - Fee Related CN102753564B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/627,874 US10174070B2 (en) 2005-09-30 2009-11-30 6-substituted estradiol derivatives and methods of use
US12/627,874 2009-11-30
PCT/US2010/058342 WO2011066542A2 (en) 2009-11-30 2010-11-30 6-substituted estradiol derivatives and methods of use

Publications (2)

Publication Number Publication Date
CN102753564A CN102753564A (zh) 2012-10-24
CN102753564B true CN102753564B (zh) 2017-04-05

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CN201080059521.4A Expired - Fee Related CN102753564B (zh) 2009-11-30 2010-11-30 6‑取代的雌二醇衍生物及其使用方法

Country Status (12)

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

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
BR112013005843A2 (pt) * 2010-09-14 2019-12-10 Endece Llc derivativos de er-beta 6-substituído por desmetil-estradiol
CN106420767A (zh) * 2011-03-21 2017-02-22 安德斯有限责任公司 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物
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
SG11201607693WA (en) * 2014-03-19 2016-10-28 Endece Llc 6-substituted estradiol derivatives for the treatment of alzheimer's disease
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3130210A (en) * 1962-11-14 1964-04-21 Olin Mathieson Estradiol derivatives
US20080119447A1 (en) * 2005-09-30 2008-05-22 James Yarger 6-alkoxyalkyl estradiol derivatives and methods of use
WO2008067450A2 (en) * 2006-11-30 2008-06-05 Endece, Llc 6-alkoxyalkyl estradiol derivatives and methods of use
US20080312202A1 (en) * 2005-09-30 2008-12-18 James Yarger 6-substituted estradiol derivatives and methods of use

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE258820C (https=)
US2867630A (en) 1958-06-09 1959-01-06 Upjohn Co 6-fluoro androstenes
GB853012A (en) 1958-06-26 1960-11-02 British Drug Houses Ltd 1:6-dimethyl aromatic steroids and the preparation thereof
NL122154C (https=) 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 (https=) 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
US4732904A (en) 1984-12-24 1988-03-22 Morgan Lee R Antiestrogenic hydrazones
GB8517360D0 (en) 1985-07-09 1985-08-14 Erba Farmitalia Substituted androsta-1,4-diene-3,17-diones
DD258820A1 (de) 1986-06-13 1988-08-03 Adw Ddr Verfahren zur herstellung von 6beta-hydroxy-methyl-androsta-1,4-dien-3,17-dion
GB8615092D0 (en) 1986-06-20 1986-07-23 Erba Farmitalia Androst-4-ene-317-diones
GB8721383D0 (en) 1987-09-11 1987-10-21 Erba Farmitalia Preparation of methylene derivatives
GB8801697D0 (en) 1988-01-26 1988-02-24 Erba Farmitalia Improvements in synthesis of 6-methylene derivatives of androsta-1 4-diene-3 17-dione
US4938763B1 (en) 1988-10-03 1995-07-04 Atrix Lab Inc Biodegradable in-situ forming implants and method of producing the same
US5504074A (en) 1993-08-06 1996-04-02 Children's Medical Center Corporation Estrogenic compounds as anti-angiogenic agents
JPH07215992A (ja) 1993-12-07 1995-08-15 Teikoku Hormone Mfg Co Ltd ６−又は７−置換アンドロスタ−１，４−ジエン誘導体
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
ATE284682T1 (de) 1998-08-11 2005-01-15 Entremed Inc Verwendung von 2-methoxyestradiol als fungizide
WO2001058919A2 (en) 2000-02-11 2001-08-16 Sri International Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one
IT1317031B1 (it) 2000-05-17 2003-05-26 Sigma Tau Ind Farmaceuti Procedimento migliorato per la preparazione di (e,z)3-(2-amminoetossimmino)-androstano-6, 17-dione e di suoi analoghi.
WO2002022645A2 (en) 2000-09-14 2002-03-21 Accelerated Pharmaceuticals, Inc. Method of making 7alpha-methyl-11beta-methoxy estradiol and related compounds with estrogenic activity
JP2006526025A (ja) 2003-05-28 2006-11-16 エントレメッド インコーポレイテッド 抗血管新生剤
US8088758B2 (en) 2003-11-12 2012-01-03 Abbott Products Gmbh 17β-hydroxysteroid dehydrogenase type I inhibitors
ATE548375T1 (de) 2004-01-16 2012-03-15 Cedarburg Pharmaceuticals Inc Exemestan und zwischenprodukte davon und verfahren zu dessen herstellung
US7498322B2 (en) 2004-03-12 2009-03-03 Entremed, Inc. Antiangiogenic agents
US7419972B2 (en) 2004-07-02 2008-09-02 Schering Ag 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
BRPI0616639A2 (pt) 2005-09-30 2011-06-28 Endece Llc compostos de exemestano de (s)-6-metiloxaalquila e métodos de uso relacionados
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
TWI392682B (zh) 2006-04-13 2013-04-11 Sigma Tau Ind Farmaceuti 作為心血管疾病的治療藥物之雄甾烷和雄甾烯的胺基衍生物
BR112013005843A2 (pt) 2010-09-14 2019-12-10 Endece Llc derivativos de er-beta 6-substituído por desmetil-estradiol

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3130210A (en) * 1962-11-14 1964-04-21 Olin Mathieson Estradiol derivatives
US20080119447A1 (en) * 2005-09-30 2008-05-22 James Yarger 6-alkoxyalkyl estradiol derivatives and methods of use
US20080312202A1 (en) * 2005-09-30 2008-12-18 James Yarger 6-substituted estradiol derivatives and methods of use
WO2008067450A2 (en) * 2006-11-30 2008-06-05 Endece, Llc 6-alkoxyalkyl estradiol derivatives and methods of use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Structure–activity relationships of 2-, 4-, or 6-substituted estrogens as aromatase inhibitors;Mitsuteru Numazawa et al.;《Journal of Steroid Biochemistry & Molecular Biology》;20050721;第96卷;51-58 *

Also Published As

Publication number Publication date
DK2507253T3 (en) 2016-07-04
MX2012006169A (es) 2012-11-12
KR20120095461A (ko) 2012-08-28
CA2781627A1 (en) 2011-06-03
MX342436B (es) 2016-09-29
AU2010324632A1 (en) 2012-06-14
US20100130463A1 (en) 2010-05-27
EP2507253B1 (en) 2016-03-30
WO2011066542A2 (en) 2011-06-03
SG181126A1 (en) 2012-07-30
AU2018203658A1 (en) 2018-06-14
US20190135853A1 (en) 2019-05-09
CN102753564A (zh) 2012-10-24
ES2568941T3 (es) 2016-05-05
KR20180095742A (ko) 2018-08-27
EP2507253A2 (en) 2012-10-10
EP2507253A4 (en) 2013-05-22
CA2781627C (en) 2017-02-28
US10174070B2 (en) 2019-01-08
JP5898625B2 (ja) 2016-04-06
KR102048457B1 (ko) 2019-11-25
WO2011066542A3 (en) 2011-10-20
US10723757B2 (en) 2020-07-28
AU2016238850A1 (en) 2016-10-20
JP2013512260A (ja) 2013-04-11

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Termination date: 20211130