AU2012230974B2 - 6-substituted estradiol derivatives for use in remyelination of nerve axons - Google Patents

6-substituted estradiol derivatives for use in remyelination of nerve axons Download PDF

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Publication number
AU2012230974B2
AU2012230974B2 AU2012230974A AU2012230974A AU2012230974B2 AU 2012230974 B2 AU2012230974 B2 AU 2012230974B2 AU 2012230974 A AU2012230974 A AU 2012230974A AU 2012230974 A AU2012230974 A AU 2012230974A AU 2012230974 B2 AU2012230974 B2 AU 2012230974B2
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AU
Australia
Prior art keywords
methyl
cyclopenta
decahydro
phenanthrene
diol
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.)
Ceased
Application number
AU2012230974A
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English (en)
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AU2012230974A1 (en
Inventor
Steve NYE
James G. Yarger
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Endece LLC
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Endece LLC
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Publication of AU2012230974A1 publication Critical patent/AU2012230974A1/en
Application granted granted Critical
Publication of AU2012230974B2 publication Critical patent/AU2012230974B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/566Compounds 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 having an oxo group in position 17, e.g. estrone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2012230974A 2011-03-21 2012-03-21 6-substituted estradiol derivatives for use in remyelination of nerve axons Ceased AU2012230974B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161454873P 2011-03-21 2011-03-21
US61/454,873 2011-03-21
PCT/US2012/029973 WO2012129324A2 (en) 2011-03-21 2012-03-21 6-substituted estradiol derivatives for use in remyelination of nerve axons

Publications (2)

Publication Number Publication Date
AU2012230974A1 AU2012230974A1 (en) 2013-09-26
AU2012230974B2 true AU2012230974B2 (en) 2016-05-12

Family

ID=46877849

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012230974A Ceased AU2012230974B2 (en) 2011-03-21 2012-03-21 6-substituted estradiol derivatives for use in remyelination of nerve axons

Country Status (13)

Country Link
US (2) US9364486B2 (enExample)
EP (1) EP2688570B1 (enExample)
JP (1) JP6174563B2 (enExample)
KR (1) KR102080151B1 (enExample)
CN (2) CN103501790B (enExample)
AU (1) AU2012230974B2 (enExample)
BR (1) BR112013024168A2 (enExample)
CA (1) CA2830515C (enExample)
DK (1) DK2688570T3 (enExample)
ES (1) ES2561536T3 (enExample)
MX (1) MX354409B (enExample)
SG (1) SG193380A1 (enExample)
WO (1) WO2012129324A2 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2688570T3 (en) * 2011-03-21 2015-12-21 Endece Llc 6-substituted estradiol for use in the remyelination of nerve axons
WO2014064712A2 (en) * 2012-10-22 2014-05-01 Intas Pharmaceuticals Limited An improved process for the preparation of fulvestrant
US20150265630A1 (en) * 2014-03-19 2015-09-24 Endece Llc 6-Substituted Estradiol Derivatives for the Treatment of Alzheimer's Disease
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100130463A1 (en) * 2005-09-30 2010-05-27 Yarger James G 6-substituted estradiol derivatives and methods of use

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4136160A (en) * 1977-08-17 1979-01-23 Cohen Steven R Specific assay for active demyelinization
JPH0193529A (ja) * 1987-10-05 1989-04-12 Mect Corp シアロシルコレステロールの脱髄性疾患治療剤
JPH01193529A (ja) 1988-01-27 1989-08-03 Yoshitsugu Takano 液体循環装置
KR101484134B1 (ko) * 2005-09-30 2015-01-21 엔디씨, 엘엘씨 (s)-6-메틸옥사알킬 엑스메스탄 화합물 및 관련 사용방법
US8168621B2 (en) * 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use
ES2604079T3 (es) * 2006-11-30 2017-03-02 Endece, Llc Derivados de 6-alcoxialquil estradiol y métodos de uso
AU2011302065B2 (en) 2010-09-14 2016-12-01 Endece, Llc 6-substituted demethyl-estradiol derivatives as ER-beta agonists
DK2688570T3 (en) * 2011-03-21 2015-12-21 Endece Llc 6-substituted estradiol for use in the remyelination of nerve axons

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100130463A1 (en) * 2005-09-30 2010-05-27 Yarger James G 6-substituted estradiol derivatives and methods of use

Also Published As

Publication number Publication date
JP2014508807A (ja) 2014-04-10
CA2830515A1 (en) 2012-09-27
EP2688570A4 (en) 2014-09-10
US20160279144A1 (en) 2016-09-29
WO2012129324A9 (en) 2012-11-15
KR20140074253A (ko) 2014-06-17
EP2688570B1 (en) 2015-11-18
DK2688570T3 (en) 2015-12-21
BR112013024168A2 (pt) 2017-07-11
US9636348B2 (en) 2017-05-02
CA2830515C (en) 2015-09-15
US20120245131A1 (en) 2012-09-27
MX2013010650A (es) 2013-10-07
WO2012129324A2 (en) 2012-09-27
AU2012230974A1 (en) 2013-09-26
KR102080151B1 (ko) 2020-02-21
ES2561536T3 (es) 2016-02-26
EP2688570A2 (en) 2014-01-29
JP6174563B2 (ja) 2017-08-02
US9364486B2 (en) 2016-06-14
CN103501790A (zh) 2014-01-08
CN106420767A (zh) 2017-02-22
CN103501790B (zh) 2016-08-17
MX354409B (es) 2018-03-05
SG193380A1 (en) 2013-10-30

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired