ES2568941T3 - Derivados de estradiol sustituidos en la posición 6 y métodos de uso - Google Patents

Derivados de estradiol sustituidos en la posición 6 y métodos de uso Download PDF

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Publication number
ES2568941T3
ES2568941T3 ES10834033.2T ES10834033T ES2568941T3 ES 2568941 T3 ES2568941 T3 ES 2568941T3 ES 10834033 T ES10834033 T ES 10834033T ES 2568941 T3 ES2568941 T3 ES 2568941T3
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Spain
Prior art keywords
compound
compounds
mmol
comparative
methods
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Active
Application number
ES10834033.2T
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English (en)
Spanish (es)
Inventor
James G. Yarger
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Endece LLC
Original Assignee
Endece LLC
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Publication date
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Publication of ES2568941T3 publication Critical patent/ES2568941T3/es
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Classifications

    • 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

Landscapes

  • 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)
ES10834033.2T 2009-11-30 2010-11-30 Derivados de estradiol sustituidos en la posición 6 y métodos de uso Active ES2568941T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US627874 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

Publications (1)

Publication Number Publication Date
ES2568941T3 true ES2568941T3 (es) 2016-05-05

Family

ID=44067274

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10834033.2T Active ES2568941T3 (es) 2009-11-30 2010-11-30 Derivados de estradiol sustituidos en la posición 6 y métodos de uso

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
MX343059B (es) * 2010-09-14 2016-10-24 Endece Llc Derivados de desmetil-estradiol sustituido en 6 como agonistas de er-beta selectivos.
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
WO2012129673A1 (en) * 2011-03-25 2012-10-04 Universite Laval INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10
US20160060288A1 (en) * 2013-04-18 2016-03-03 Xi'anlibang Pharmaceutical Technology Co., Ltd. Ester derivatives of 7-alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-estra-1,3,5(10)-triene-3,17beta-diol having anticancer activity and preparation method thereof
WO2015143201A2 (en) * 2014-03-19 2015-09-24 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

Family Cites Families (35)

* Cited by examiner, † Cited by third party
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DE258820C (enExample)
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
US3130210A (en) 1962-11-14 1964-04-21 Olin Mathieson Estradiol derivatives
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
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
CA2339835C (en) 1998-08-11 2008-12-16 Entremed, Inc. Use of estrogenic compounds as anti-fungal agents
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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.
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ATE548375T1 (de) 2004-01-16 2012-03-15 Cedarburg Pharmaceuticals Inc Exemestan und zwischenprodukte davon und verfahren zu dessen herstellung
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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
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
US20080119447A1 (en) 2005-09-30 2008-05-22 James Yarger 6-alkoxyalkyl estradiol derivatives and methods of use
US8168621B2 (en) 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use
CN101312743A (zh) 2005-09-30 2008-11-26 安德西有限公司 (s)-6-甲基氧杂烷基依西美坦化合物及相关使用方法
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
JP5290189B2 (ja) 2006-11-30 2013-09-18 エンディース エルエルシー ６−アルコキシアルキルエストラジオール誘導体およびその使用
MX343059B (es) 2010-09-14 2016-10-24 Endece Llc Derivados de desmetil-estradiol sustituido en 6 como agonistas de er-beta selectivos.

Also Published As

Publication number Publication date
KR102048457B1 (ko) 2019-11-25
KR20120095461A (ko) 2012-08-28
AU2018203658A1 (en) 2018-06-14
WO2011066542A3 (en) 2011-10-20
US10174070B2 (en) 2019-01-08
MX2012006169A (es) 2012-11-12
AU2010324632A1 (en) 2012-06-14
KR20180095742A (ko) 2018-08-27
CN102753564B (zh) 2017-04-05
CA2781627C (en) 2017-02-28
SG181126A1 (en) 2012-07-30
CN102753564A (zh) 2012-10-24
DK2507253T3 (en) 2016-07-04
US10723757B2 (en) 2020-07-28
CA2781627A1 (en) 2011-06-03
EP2507253A2 (en) 2012-10-10
EP2507253B1 (en) 2016-03-30
WO2011066542A2 (en) 2011-06-03
JP5898625B2 (ja) 2016-04-06
JP2013512260A (ja) 2013-04-11
AU2016238850A1 (en) 2016-10-20
MX342436B (es) 2016-09-29
US20190135853A1 (en) 2019-05-09
US20100130463A1 (en) 2010-05-27
EP2507253A4 (en) 2013-05-22

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