CA2830515C - 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

Info

Publication number
CA2830515C
CA2830515C CA2830515A CA2830515A CA2830515C CA 2830515 C CA2830515 C CA 2830515C CA 2830515 A CA2830515 A CA 2830515A CA 2830515 A CA2830515 A CA 2830515A CA 2830515 C CA2830515 C CA 2830515C
Authority
CA
Canada
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.)
Expired - Fee Related
Application number
CA2830515A
Other languages
English (en)
French (fr)
Other versions
CA2830515A1 (en
Inventor
James G. Yarger
Steve NYE
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.)
Individual
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 CA2830515A1 publication Critical patent/CA2830515A1/en
Application granted granted Critical
Publication of CA2830515C publication Critical patent/CA2830515C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/566—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

Landscapes

  • 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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2830515A 2011-03-21 2012-03-21 6-substituted estradiol derivatives for use in remyelination of nerve axons Expired - Fee Related CA2830515C (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
CA2830515A1 CA2830515A1 (en) 2012-09-27
CA2830515C true CA2830515C (en) 2015-09-15

Family

ID=46877849

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2830515A Expired - Fee Related CA2830515C (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) 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
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
EP2909224B1 (en) * 2012-10-22 2020-03-18 Intas Pharmaceuticals Limited An improved process for the preparation of fulvestrant
WO2015143201A2 (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

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
US8168621B2 (en) * 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use
US10174070B2 (en) * 2005-09-30 2019-01-08 Endece Llc 6-substituted 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
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
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

Also Published As

Publication number Publication date
AU2012230974B2 (en) 2016-05-12
US9364486B2 (en) 2016-06-14
KR102080151B1 (ko) 2020-02-21
JP2014508807A (ja) 2014-04-10
JP6174563B2 (ja) 2017-08-02
CN103501790A (zh) 2014-01-08
AU2012230974A1 (en) 2013-09-26
US20120245131A1 (en) 2012-09-27
EP2688570B1 (en) 2015-11-18
MX2013010650A (es) 2013-10-07
EP2688570A4 (en) 2014-09-10
EP2688570A2 (en) 2014-01-29
CA2830515A1 (en) 2012-09-27
CN106420767A (zh) 2017-02-22
ES2561536T3 (es) 2016-02-26
CN103501790B (zh) 2016-08-17
WO2012129324A9 (en) 2012-11-15
US9636348B2 (en) 2017-05-02
BR112013024168A2 (pt) 2017-07-11
WO2012129324A2 (en) 2012-09-27
SG193380A1 (en) 2013-10-30
US20160279144A1 (en) 2016-09-29
DK2688570T3 (en) 2015-12-21
KR20140074253A (ko) 2014-06-17
MX354409B (es) 2018-03-05

Similar Documents

Publication Publication Date Title
CA2781627C (en) 6-substituted estradiol derivatives and methods of use
EP2616477B1 (en) 6-substituted demethyl-estradiol derivatives as er-beta agonists
US9636348B2 (en) 6-substituted estradiol derivatives for use in remyelination of nerve axons
TWI910261B (zh) Ｒｐｓ２５基因之表現及／或功能調節劑
JP5727370B2 (ja) ６−置換エストラジオール誘導体および使用方法
CA2085819A1 (en) Novel tricyclic steroid analogs
AU2018201003A1 (en) 6-substituted estradiol derivatives for the treatment of alzheimer's disease
AU2007325092B2 (en) 6-alkoxyalkyl estradiol derivatives and methods of use
US20230097440A1 (en) 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
WO2014091020A1 (en) Phenanthrene derivatives for use as medicaments

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20130917

MKLA Lapsed

Effective date: 20220301

MKLA Lapsed

Effective date: 20200831