CA2726364C - 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
CA2726364C
CA2726364C CA2726364A CA2726364A CA2726364C CA 2726364 C CA2726364 C CA 2726364C CA 2726364 A CA2726364 A CA 2726364A CA 2726364 A CA2726364 A CA 2726364A CA 2726364 C CA2726364 C CA 2726364C
Authority
CA
Canada
Prior art keywords
group
alkyl
compound
halogen
glucoronide
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.)
Expired - Fee Related
Application number
CA2726364A
Other languages
English (en)
French (fr)
Other versions
CA2726364A1 (en
Inventor
James 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 CA2726364A1 publication Critical patent/CA2726364A1/en
Application granted granted Critical
Publication of CA2726364C publication Critical patent/CA2726364C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Medicinal Chemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Wood Science & Technology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cell Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CA2726364A 2008-06-04 2009-06-03 6-substituted estradiol derivatives and methods of use Expired - Fee Related CA2726364C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/132,857 US8168621B2 (en) 2005-09-30 2008-06-04 6-substituted estradiol derivatives and methods of use
US12/132,857 2008-06-04
PCT/US2009/046120 WO2009149176A1 (en) 2008-06-04 2009-06-03 6-substituted estradiol derivatives and methods of use

Publications (2)

Publication Number Publication Date
CA2726364A1 CA2726364A1 (en) 2009-12-10
CA2726364C true CA2726364C (en) 2016-10-11

Family

ID=41398499

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2726364A Expired - Fee Related CA2726364C (en) 2008-06-04 2009-06-03 6-substituted estradiol derivatives and methods of use

Country Status (13)

Country Link
US (2) US8168621B2 (enExample)
EP (1) EP2300016B1 (enExample)
JP (1) JP5727370B2 (enExample)
KR (1) KR101769152B1 (enExample)
CN (1) CN102076343B (enExample)
AU (1) AU2009256237B2 (enExample)
BR (1) BRPI0913632A2 (enExample)
CA (1) CA2726364C (enExample)
DK (1) DK2300016T3 (enExample)
ES (1) ES2641779T3 (enExample)
MX (1) MX2010013288A (enExample)
NO (1) NO2300016T3 (enExample)
WO (1) WO2009149176A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002342335B2 (en) * 2001-05-16 2006-02-02 Novartis Ag Combination comprising N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent
US10174070B2 (en) * 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
US20090028895A1 (en) * 2007-07-27 2009-01-29 Smith Walter P Methods and compositions for reducing facial lines and wrinkles
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
US11624095B2 (en) 2017-09-27 2023-04-11 Case Western Reserve University Method of quantifying HIV reservoirs by induced transcription based sequencing
US20210024568A1 (en) * 2019-07-23 2021-01-28 Endece Llc Methods for modulation of lipoprotein lipase and apolipoprotein c2 expression and/or activity in the treatment of peripheral and central nervous system tissue disease states

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL122154C (enExample) 1963-10-18
GB8517360D0 (en) 1985-07-09 1985-08-14 Erba Farmitalia Substituted androsta-1,4-diene-3,17-diones
GB8615092D0 (en) * 1986-06-20 1986-07-23 Erba Farmitalia Androst-4-ene-317-diones
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
US4904950A (en) 1988-11-04 1990-02-27 Medical Data Electronics, Inc. Telemetry digital subcarrier demodulator
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
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
WO2005030120A2 (en) 2003-05-28 2005-04-07 Entremed, Inc. Antiangiogenic agents
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
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
US20080119447A1 (en) * 2005-09-30 2008-05-22 James Yarger 6-alkoxyalkyl 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

Also Published As

Publication number Publication date
US20120270817A1 (en) 2012-10-25
US8168621B2 (en) 2012-05-01
JP5727370B2 (ja) 2015-06-03
EP2300016B1 (en) 2017-08-09
KR20110019767A (ko) 2011-02-28
WO2009149176A1 (en) 2009-12-10
AU2009256237B2 (en) 2015-11-26
DK2300016T3 (en) 2017-09-18
EP2300016A1 (en) 2011-03-30
JP2011522825A (ja) 2011-08-04
US20080312202A1 (en) 2008-12-18
CN102076343B (zh) 2015-04-01
US8629130B2 (en) 2014-01-14
ES2641779T3 (es) 2017-11-13
AU2009256237A1 (en) 2009-12-10
MX2010013288A (es) 2010-12-21
EP2300016A4 (en) 2012-01-18
CA2726364A1 (en) 2009-12-10
NO2300016T3 (enExample) 2018-01-06
KR101769152B1 (ko) 2017-08-17
BRPI0913632A2 (pt) 2017-01-24
CN102076343A (zh) 2011-05-25

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US20080119447A1 (en) 6-alkoxyalkyl estradiol derivatives and methods of use
AU2007325092B2 (en) 6-alkoxyalkyl estradiol derivatives and methods of use
HK1139315A (en) 6-alkoxyalkyl estradiol derivatives and its use
HK1139315B (en) 6-alkoxyalkyl estradiol derivatives and its use

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Effective date: 20210603