AU2010324632A1 - 6-substituted estradiol derivatives and methods of use - Google Patents

6-substituted estradiol derivatives and methods of use Download PDF

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Publication number
AU2010324632A1
AU2010324632A1 AU2010324632A AU2010324632A AU2010324632A1 AU 2010324632 A1 AU2010324632 A1 AU 2010324632A1 AU 2010324632 A AU2010324632 A AU 2010324632A AU 2010324632 A AU2010324632 A AU 2010324632A AU 2010324632 A1 AU2010324632 A1 AU 2010324632A1
Authority
AU
Australia
Prior art keywords
nch
methyl
hydrogen
cyclopenta
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU2010324632A
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English (en)
Inventor
James G. Yarger
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Endece LLC
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
Publication of AU2010324632A1 publication Critical patent/AU2010324632A1/en
Assigned to ENDECE, LLC reassignment ENDECE, LLC Amend patent request/document other than specification (104) Assignors: ENDECE INC.
Priority to AU2016238850A priority Critical patent/AU2016238850A1/en
Priority to AU2018203658A priority patent/AU2018203658A1/en
Abandoned legal-status Critical Current

Links

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)
AU2010324632A 2009-11-30 2010-11-30 6-substituted estradiol derivatives and methods of use Abandoned AU2010324632A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2016238850A AU2016238850A1 (en) 2009-11-30 2016-10-05 6-substituted estradiol derivatives and methods of use
AU2018203658A AU2018203658A1 (en) 2009-11-30 2018-05-24 6-substituted estradiol derivatives and methods of use

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 Child Applications (1)

Application Number Title Priority Date Filing Date
AU2016238850A Division AU2016238850A1 (en) 2009-11-30 2016-10-05 6-substituted estradiol derivatives and methods of use

Publications (1)

Publication Number Publication Date
AU2010324632A1 true AU2010324632A1 (en) 2012-06-14

Family

ID=44067274

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2010324632A Abandoned AU2010324632A1 (en) 2009-11-30 2010-11-30 6-substituted estradiol derivatives and methods of use
AU2016238850A Abandoned AU2016238850A1 (en) 2009-11-30 2016-10-05 6-substituted estradiol derivatives and methods of use
AU2018203658A Abandoned AU2018203658A1 (en) 2009-11-30 2018-05-24 6-substituted estradiol derivatives and methods of use

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2016238850A Abandoned AU2016238850A1 (en) 2009-11-30 2016-10-05 6-substituted estradiol derivatives and methods of use
AU2018203658A Abandoned AU2018203658A1 (en) 2009-11-30 2018-05-24 6-substituted estradiol derivatives and methods of use

Country Status (12)

Country Link
US (2) US10174070B2 (enExample)
EP (1) EP2507253B1 (enExample)
JP (1) JP5898625B2 (enExample)
KR (2) KR20120095461A (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
ES2605960T3 (es) * 2010-09-14 2017-03-17 Endece, Llc Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta
MX354409B (es) * 2011-03-21 2018-03-05 Endece Llc Derivados de estradiol sustituidos en 6 para uso en remielinización de axones nerviosos.
US11072632B2 (en) * 2011-03-25 2021-07-27 UNIVERSITé LAVAL Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10
KR102046415B1 (ko) * 2013-04-18 2019-12-02 시안 리방 파마슈티컬 테크놀로지 컴퍼니 리미티드 항암 활성을 갖는 7-α-[9-(4,4,5,5,5-펜타플루오로펜틸설피닐)노닐]-에스트라-1,3,5(10)-트리엔-3,17β-디올의 에스테르 유도체 및 그의 제조 방법
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

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DE258820C (enExample)
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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
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
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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
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Also Published As

Publication number Publication date
WO2011066542A2 (en) 2011-06-03
SG181126A1 (en) 2012-07-30
KR102048457B1 (ko) 2019-11-25
CN102753564A (zh) 2012-10-24
US20190135853A1 (en) 2019-05-09
US20100130463A1 (en) 2010-05-27
CA2781627C (en) 2017-02-28
JP5898625B2 (ja) 2016-04-06
CA2781627A1 (en) 2011-06-03
CN102753564B (zh) 2017-04-05
DK2507253T3 (en) 2016-07-04
WO2011066542A3 (en) 2011-10-20
MX2012006169A (es) 2012-11-12
KR20120095461A (ko) 2012-08-28
EP2507253A4 (en) 2013-05-22
KR20180095742A (ko) 2018-08-27
MX342436B (es) 2016-09-29
JP2013512260A (ja) 2013-04-11
ES2568941T3 (es) 2016-05-05
AU2018203658A1 (en) 2018-06-14
US10174070B2 (en) 2019-01-08
EP2507253A2 (en) 2012-10-10
US10723757B2 (en) 2020-07-28
AU2016238850A1 (en) 2016-10-20
EP2507253B1 (en) 2016-03-30

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Legal Events

Date Code Title Description
MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted