CN113330020B - 用于治疗神经变性疾病的2-氟代的胆汁酸 - Google Patents

用于治疗神经变性疾病的2-氟代的胆汁酸 Download PDF

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Publication number
CN113330020B
CN113330020B CN201980085276.5A CN201980085276A CN113330020B CN 113330020 B CN113330020 B CN 113330020B CN 201980085276 A CN201980085276 A CN 201980085276A CN 113330020 B CN113330020 B CN 113330020B
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China
Prior art keywords
compound
dihydroxy
difluoro
formula
acid
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CN201980085276.5A
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English (en)
Chinese (zh)
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CN113330020A (zh
Inventor
A·C·韦茅斯-威尔逊
B·J·P·林克劳
G·帕克尔
J·瓦茨
H·莫蒂博伊斯
O·班德曼
C·黑斯廷斯
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University of Southampton
Nzp Uk Ltd
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University of Southampton
Nzp Uk Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • 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
    • 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
    • A61P25/16Anti-Parkinson drugs
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J33/00Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C07J41/0061Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J11/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980085276.5A 2018-12-20 2019-12-20 用于治疗神经变性疾病的2-氟代的胆汁酸 Active CN113330020B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1820887.6 2018-12-20
GBGB1820887.6A GB201820887D0 (en) 2018-12-20 2018-12-20 Compounds
PCT/GB2019/053665 WO2020128514A1 (en) 2018-12-20 2019-12-20 2-fluorinated bile acids for the treatment of neurodegenerative diseases

Publications (2)

Publication Number Publication Date
CN113330020A CN113330020A (zh) 2021-08-31
CN113330020B true CN113330020B (zh) 2024-04-05

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Country Link
US (1) US20220073557A1 (https=)
EP (1) EP3898645B1 (https=)
JP (1) JP7503063B2 (https=)
KR (1) KR102856276B1 (https=)
CN (1) CN113330020B (https=)
AU (1) AU2019411556B2 (https=)
BR (1) BR112021011189A2 (https=)
CA (1) CA3123333A1 (https=)
EA (1) EA202191521A1 (https=)
ES (1) ES3036094T3 (https=)
GB (1) GB201820887D0 (https=)
IL (1) IL284093B2 (https=)
MX (1) MX2021007551A (https=)
SG (1) SG11202105465WA (https=)
WO (1) WO2020128514A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4486318A4 (en) * 2022-03-02 2026-02-25 Boyce Thompson Institute For Plant Res Inc Cysteamides, related therapeutic compositions and associated processes
GB202208151D0 (en) 2022-06-01 2022-07-13 Nzp Uk Ltd Compounds
GB202314563D0 (en) 2023-09-22 2023-11-08 Nzp Uk Ltd Compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014036379A2 (en) * 2012-08-31 2014-03-06 Metselex Bile acids prevent or abolish progression of parkinson's and related neurodegenerative diseases
CN107531741A (zh) * 2015-03-10 2018-01-02 美莱斯股份有限公司 氟化和烷基化胆酸

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ298567A (en) * 1994-11-23 2000-01-28 Cocensys Inc Androstane and pregnane derivatives, pharmaceutical compositions and methods of treatment
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
FR2934596B1 (fr) * 2008-07-30 2015-04-10 Trophos Nouveaux derives de l'oxime de cholest-4-en-3-one, compositions pharmaceutiques les renfermant, et procede de preparation
ITMI20121344A1 (it) * 2012-07-31 2014-02-01 Erregierre Spa Processo di preparazione di acido ursodesossicolico ad elevata purezza
CN103333216A (zh) * 2013-06-04 2013-10-02 苏州大学 5α-6-酮-胆甾烷类似物及其应用
US20150112089A1 (en) 2013-10-22 2015-04-23 Metselex, Inc. Deuterated bile acids
GB201812382D0 (en) * 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014036379A2 (en) * 2012-08-31 2014-03-06 Metselex Bile acids prevent or abolish progression of parkinson's and related neurodegenerative diseases
CN107531741A (zh) * 2015-03-10 2018-01-02 美莱斯股份有限公司 氟化和烷基化胆酸

Also Published As

Publication number Publication date
IL284093B1 (en) 2025-03-01
EP3898645C0 (en) 2025-06-25
AU2019411556A1 (en) 2021-06-10
WO2020128514A1 (en) 2020-06-25
IL284093A (en) 2021-08-31
EP3898645B1 (en) 2025-06-25
GB201820887D0 (en) 2019-02-06
KR20210125982A (ko) 2021-10-19
EP3898645A1 (en) 2021-10-27
CN113330020A (zh) 2021-08-31
ES3036094T3 (en) 2025-09-12
BR112021011189A2 (pt) 2021-08-31
JP2022514401A (ja) 2022-02-10
AU2019411556B2 (en) 2025-04-03
MX2021007551A (es) 2021-10-13
EA202191521A1 (ru) 2021-09-10
IL284093B2 (en) 2025-07-01
CA3123333A1 (en) 2020-06-25
US20220073557A1 (en) 2022-03-10
JP7503063B2 (ja) 2024-06-19
SG11202105465WA (en) 2021-06-29
KR102856276B1 (ko) 2025-09-05

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