CN106420767A - 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
CN106420767A
CN106420767A CN201610455383.0A CN201610455383A CN106420767A CN 106420767 A CN106420767 A CN 106420767A CN 201610455383 A CN201610455383 A CN 201610455383A CN 106420767 A CN106420767 A CN 106420767A
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methyl
cyclopenta
phenanthrene
glycol
methoxy
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CN201610455383.0A
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Chinese (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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    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychology (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)
CN201610455383.0A 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 Pending CN106420767A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161454873P 2011-03-21 2011-03-21
US61/454,873 2011-03-21
CN201280014512.2A CN103501790B (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

Related Parent Applications (1)

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CN201280014512.2A Division CN103501790B (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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CN106420767A true CN106420767A (zh) 2017-02-22

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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
CN201280014512.2A Expired - Fee Related CN103501790B (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) CN106420767A (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
MX354409B (es) * 2011-03-21 2018-03-05 Endece Llc Derivados de estradiol sustituidos en 6 para uso en remielinización de axones nerviosos.
US9315540B2 (en) 2012-10-22 2016-04-19 Intas Pharmaceuticals Ltd. Process for the preparation of fulvestrant
AU2015231172A1 (en) * 2014-03-19 2016-09-08 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 (2)

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

Family Cites Families (7)

* 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
US8168621B2 (en) * 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use
WO2008067450A2 (en) * 2006-11-30 2008-06-05 Endece, Llc 6-alkoxyalkyl estradiol derivatives and methods of use
BR112013005843A2 (pt) 2010-09-14 2019-12-10 Endece Llc derivativos de er-beta 6-substituído por desmetil-estradiol
MX354409B (es) * 2011-03-21 2018-03-05 Endece Llc Derivados de estradiol sustituidos en 6 para uso en remielinización de axones nerviosos.

Patent Citations (2)

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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
D.K.CRAWFORD等: "Oestrogen receptor beta ligand: a novel treatment to enhance endogenous functional remyelination", 《BRAIN》 *

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Publication number Publication date
EP2688570A2 (en) 2014-01-29
CA2830515C (en) 2015-09-15
JP2014508807A (ja) 2014-04-10
EP2688570A4 (en) 2014-09-10
AU2012230974B2 (en) 2016-05-12
AU2012230974A1 (en) 2013-09-26
US20160279144A1 (en) 2016-09-29
US9636348B2 (en) 2017-05-02
US9364486B2 (en) 2016-06-14
BR112013024168A2 (pt) 2017-07-11
KR102080151B1 (ko) 2020-02-21
DK2688570T3 (en) 2015-12-21
MX354409B (es) 2018-03-05
MX2013010650A (es) 2013-10-07
SG193380A1 (en) 2013-10-30
JP6174563B2 (ja) 2017-08-02
EP2688570B1 (en) 2015-11-18
CN103501790B (zh) 2016-08-17
WO2012129324A2 (en) 2012-09-27
KR20140074253A (ko) 2014-06-17
ES2561536T3 (es) 2016-02-26
US20120245131A1 (en) 2012-09-27
CN103501790A (zh) 2014-01-08
WO2012129324A9 (en) 2012-11-15
CA2830515A1 (en) 2012-09-27

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Application publication date: 20170222