CN103501790B - 用于神经轴突的髓鞘再生的6-取代的雌二醇衍生物 - Google Patents

用于神经轴突的髓鞘再生的6-取代的雌二醇衍生物 Download PDF

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Publication number
CN103501790B
CN103501790B CN201280014512.2A CN201280014512A CN103501790B CN 103501790 B CN103501790 B CN 103501790B CN 201280014512 A CN201280014512 A CN 201280014512A CN 103501790 B CN103501790 B CN 103501790B
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methyl
phenanthrene
diol
decahydro
cyclopenta
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Expired - Fee Related
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CN201280014512.2A
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Chinese (zh)
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CN103501790A (zh
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J·G·雅格尔
S·奈
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Endece LLC
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Endece LLC
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    • 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
    • A61K31/566—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 having an oxo group in position 17, e.g. estrone
    • 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
    • A61K31/565—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
    • 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
    • A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • 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
    • A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—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 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
    • 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
    • A61K31/57—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators

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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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201280014512.2A 2011-03-21 2012-03-21 用于神经轴突的髓鞘再生的6-取代的雌二醇衍生物 Expired - Fee Related CN103501790B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610455383.0A CN106420767A (zh) 2011-03-21 2012-03-21 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610455383.0A Division CN106420767A (zh) 2011-03-21 2012-03-21 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物

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CN103501790A CN103501790A (zh) 2014-01-08
CN103501790B true CN103501790B (zh) 2016-08-17

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CN201610455383.0A Pending CN106420767A (zh) 2011-03-21 2012-03-21 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物

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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
SG193380A1 (en) * 2011-03-21 2013-10-30 Endece Llc 6-substituted estradiol derivatives for use in remyelination of nerve axons
CA2884806A1 (en) * 2012-10-22 2014-05-01 Intas Pharmaceuticals Limited An improved process for the preparation of fulvestrant
MX2016012045A (es) * 2014-03-19 2017-01-19 Endece Llc Derivados de estradiol 6-sustituido para el tratamiento de la enfermedad de alzheimer.
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 (9)

* 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
CA2624269C (en) * 2005-09-30 2016-03-22 Endece, Llc Exemestane compounds, compositions and related uses thereof
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
US8168621B2 (en) * 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use
EP2099460B1 (en) * 2006-11-30 2016-09-07 Endece, LLC 6-alkoxyalkyl estradiol derivatives and methods of use
WO2012037261A2 (en) 2010-09-14 2012-03-22 Endece, Llc 6-substituted demethyl-estradiol derivatives as er-beta agonists
SG193380A1 (en) * 2011-03-21 2013-10-30 Endece Llc 6-substituted estradiol derivatives for use in remyelination of nerve axons

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Oestrogen receptor ligand: a novel treatment to enhance endogenous functional remyelination;D.K.CRAWFORD等;《BRAIN》;20100921;第133卷(第10期);2999-3016 *

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Publication number Publication date
CA2830515A1 (en) 2012-09-27
EP2688570A4 (en) 2014-09-10
WO2012129324A2 (en) 2012-09-27
US9364486B2 (en) 2016-06-14
CN106420767A (zh) 2017-02-22
DK2688570T3 (en) 2015-12-21
KR20140074253A (ko) 2014-06-17
EP2688570B1 (en) 2015-11-18
BR112013024168A2 (pt) 2017-07-11
MX354409B (es) 2018-03-05
AU2012230974B2 (en) 2016-05-12
KR102080151B1 (ko) 2020-02-21
US9636348B2 (en) 2017-05-02
AU2012230974A1 (en) 2013-09-26
WO2012129324A9 (en) 2012-11-15
EP2688570A2 (en) 2014-01-29
CN103501790A (zh) 2014-01-08
US20120245131A1 (en) 2012-09-27
CA2830515C (en) 2015-09-15
US20160279144A1 (en) 2016-09-29
MX2013010650A (es) 2013-10-07
SG193380A1 (en) 2013-10-30
JP6174563B2 (ja) 2017-08-02
ES2561536T3 (es) 2016-02-26
JP2014508807A (ja) 2014-04-10

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Granted publication date: 20160817