DK2507253T3 - 6-substituerede estradiolderivater samt anvendelsesmåder - Google Patents

6-substituerede estradiolderivater samt anvendelsesmåder Download PDF

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Publication number
DK2507253T3
DK2507253T3 DK10834033.2T DK10834033T DK2507253T3 DK 2507253 T3 DK2507253 T3 DK 2507253T3 DK 10834033 T DK10834033 T DK 10834033T DK 2507253 T3 DK2507253 T3 DK 2507253T3
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DK
Denmark
Prior art keywords
compounds
compound
estrogen
mmol
methyl
Prior art date
Application number
DK10834033.2T
Other languages
English (en)
Inventor
James G Yarger
Original Assignee
Endece Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Endece Llc filed Critical Endece Llc
Application granted granted Critical
Publication of DK2507253T3 publication Critical patent/DK2507253T3/da

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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

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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)

Claims (2)

1. Forbindelse med formlen:
hvori Ru R2, R3 og R4 er brint; m er et heltal fra 2 til 8; n er et heltal fra 0 til 3; Z er -0-; hvori både C-13 metyl og C-17 hydroxyl er (S)-konfigureret; og symbolet vww repræsenterer enhver type binding uanset stereokemi; og de respektive hydrater, solvater og farmaceutisk acceptable salte deraf.
2. Farmaceutisk sammensætning omfattende en forbindelse ifølge krav 1 og en farmaceutisk acceptabel bærer.
DK10834033.2T 2009-11-30 2010-11-30 6-substituerede estradiolderivater samt anvendelsesmåder DK2507253T3 (da)

Applications Claiming Priority (2)

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
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
DK2507253T3 true DK2507253T3 (da) 2016-07-04

Family

ID=44067274

Family Applications (1)

Application Number Title Priority Date Filing Date
DK10834033.2T DK2507253T3 (da) 2009-11-30 2010-11-30 6-substituerede estradiolderivater samt anvendelsesmåder

Country Status (12)

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

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
ES2605960T3 (es) * 2010-09-14 2017-03-17 Endece, Llc Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta
BR112013024168A2 (pt) * 2011-03-21 2017-07-11 Endece Llc derivados 6-substituídos de estradiol para aplicação na remielinização de axônios de nervos
EP2688901B1 (en) * 2011-03-25 2019-05-08 Université Laval INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10
WO2014169462A1 (zh) * 2013-04-18 2014-10-23 西安力邦医药科技有限责任公司 具有抗癌活性的7-α-[9-(4,4,5,5,-五氟戊基亚硫酰基)壬基]-雌甾-1,3,5(10)-三烯-3,17β-二醇的酯类衍生物及其制备方法
BR112016021408A2 (pt) * 2014-03-19 2017-12-19 Endece Llc métodos para o tratamento da doença de alzheimer utilizando compostos derivados de 6-estradiol substituído
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
Publication number Priority date Publication date Assignee Title
DE258820C (da)
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 (da) * 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 (da) * 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
WO2000009101A2 (en) * 1998-08-11 2000-02-24 Entremed, Inc. Use of estrogenic compounds as anti-fungal agents
US6784170B2 (en) * 2000-02-11 2004-08-31 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
ES2382609T3 (es) 2004-01-16 2012-06-11 Cedarburg Pharmaceuticals, Inc. Exemestano y sus productos intermedios y métodos de preparación de los mismos
JP2007529426A (ja) 2004-03-12 2007-10-25 エントレメッド インコーポレイテッド 抗血管新生薬
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
US8168621B2 (en) 2005-09-30 2012-05-01 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
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
CA2624269C (en) 2005-09-30 2016-03-22 Endece, Llc Exemestane compounds, compositions and related uses thereof
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
WO2008067450A2 (en) 2006-11-30 2008-06-05 Endece, Llc 6-alkoxyalkyl estradiol derivatives and methods of use
ES2605960T3 (es) 2010-09-14 2017-03-17 Endece, Llc Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta

Also Published As

Publication number Publication date
CN102753564B (zh) 2017-04-05
CN102753564A (zh) 2012-10-24
EP2507253A2 (en) 2012-10-10
SG181126A1 (en) 2012-07-30
JP2013512260A (ja) 2013-04-11
MX342436B (es) 2016-09-29
ES2568941T3 (es) 2016-05-05
US20190135853A1 (en) 2019-05-09
KR20120095461A (ko) 2012-08-28
EP2507253A4 (en) 2013-05-22
US10723757B2 (en) 2020-07-28
US10174070B2 (en) 2019-01-08
CA2781627C (en) 2017-02-28
CA2781627A1 (en) 2011-06-03
WO2011066542A3 (en) 2011-10-20
AU2016238850A1 (en) 2016-10-20
WO2011066542A2 (en) 2011-06-03
AU2018203658A1 (en) 2018-06-14
KR20180095742A (ko) 2018-08-27
AU2010324632A1 (en) 2012-06-14
KR102048457B1 (ko) 2019-11-25
US20100130463A1 (en) 2010-05-27
MX2012006169A (es) 2012-11-12
EP2507253B1 (en) 2016-03-30
JP5898625B2 (ja) 2016-04-06

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