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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CN
China
Prior art keywords
methyl
phenanthrene
diol
methoxymethyl
decahydro
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Pending
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CN201610455383.0A
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English (en)
Chinese (zh)
Inventor
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
    • 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
    • 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
    • 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)
  • 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)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (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)

Application Number Title Priority Date Filing Date
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

Publications (1)

Publication Number Publication Date
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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Country Status (13)

Country Link
US (2) US9364486B2 (https=)
EP (1) EP2688570B1 (https=)
JP (1) JP6174563B2 (https=)
KR (1) KR102080151B1 (https=)
CN (2) CN106420767A (https=)
AU (1) AU2012230974B2 (https=)
BR (1) BR112013024168A2 (https=)
CA (1) CA2830515C (https=)
DK (1) DK2688570T3 (https=)
ES (1) ES2561536T3 (https=)
MX (1) MX354409B (https=)
SG (1) SG193380A1 (https=)
WO (1) WO2012129324A2 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2014064712A2 (en) * 2012-10-22 2014-05-01 Intas Pharmaceuticals Limited An improved process for the preparation of fulvestrant
SG11201607693WA (en) * 2014-03-19 2016-10-28 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)

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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
JP5290189B2 (ja) * 2006-11-30 2013-09-18 エンディース エルエルシー ６−アルコキシアルキルエストラジオール誘導体およびその使用
BR112013005843A2 (pt) 2010-09-14 2019-12-10 Endece Llc derivativos de er-beta 6-substituído por desmetil-estradiol
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

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》 *

Also Published As

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

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