IL284093B2 - Bile acids modified at position 2 with fluorine for the treatment of neurodegenerative diseases - Google Patents

Bile acids modified at position 2 with fluorine for the treatment of neurodegenerative diseases

Info

Publication number
IL284093B2
IL284093B2 IL284093A IL28409321A IL284093B2 IL 284093 B2 IL284093 B2 IL 284093B2 IL 284093 A IL284093 A IL 284093A IL 28409321 A IL28409321 A IL 28409321A IL 284093 B2 IL284093 B2 IL 284093B2
Authority
IL
Israel
Prior art keywords
compound
general formula
dihydroxy
difluoro
acid
Prior art date
Application number
IL284093A
Other languages
English (en)
Hebrew (he)
Other versions
IL284093B1 (en
IL284093A (en
Original Assignee
Nzp Uk Ltd
The Univ Of Southampton
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 Nzp Uk Ltd, The Univ Of Southampton filed Critical Nzp Uk Ltd
Publication of IL284093A publication Critical patent/IL284093A/en
Publication of IL284093B1 publication Critical patent/IL284093B1/en
Publication of IL284093B2 publication Critical patent/IL284093B2/en

Links

Classifications

    • 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
    • C07J11/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • 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
    • 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

Landscapes

  • 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)
IL284093A 2018-12-20 2019-12-20 Bile acids modified at position 2 with fluorine for the treatment of neurodegenerative diseases IL284093B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (3)

Publication Number Publication Date
IL284093A IL284093A (en) 2021-08-31
IL284093B1 IL284093B1 (en) 2025-03-01
IL284093B2 true IL284093B2 (en) 2025-07-01

Family

ID=65364420

Family Applications (1)

Application Number Title Priority Date Filing Date
IL284093A IL284093B2 (en) 2018-12-20 2019-12-20 Bile acids modified at position 2 with fluorine for the treatment of neurodegenerative diseases

Country Status (15)

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

Family Cites Families (9)

* 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
WO2014036377A1 (en) 2012-08-31 2014-03-06 Metselex Methods of promoting cell viability
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
US11072630B2 (en) * 2015-03-10 2021-07-27 Metselex, Inc. Fluorinated and alkylated bile acids
GB201812382D0 (en) * 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds

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
CN113330020B (zh) 2024-04-05
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

Similar Documents

Publication Publication Date Title
KR101892768B1 (ko) Metap-2 저해제의 결정질 고체 및 그의 제조 및 이용 방법
EP1728793B1 (en) 9-substituted 8-oxoadenine compound
JP6896113B2 (ja) ジアザ二環式置換イミダゾピリミジンおよび呼吸障害を治療するためのその使用
JP7733937B2 (ja) グアイアン系セスキテルペン誘導体及びその使用
EP3898645B1 (en) 2-fluorinated bile acids for the treatment of neurodegenerative diseases
CN114805478A (zh) 氘代拟肽类化合物及其用途
CN111620815B (zh) 手性氯喹、羟氯喹和其衍生物及其制备方法与用途
WO2023125535A1 (zh) 氘代拟肽类化合物及其用途
US20250320246A1 (en) 3-azasteroid compounds for the treatment of diseases related to mitrochondrial function
HK40062202B (en) 2-fluorinated bile acids for the treatment of neurodegenerative diseases
HK40062202A (en) 2-fluorinated bile acids for the treatment of neurodegenerative diseases
US20250034194A1 (en) Inhibitors of abnormal phosphorylation and tau protein aggregation
CN112218878A (zh) Ntcp抑制剂
EA046372B1 (ru) 2-фторированные желчные кислоты для лечения нейродегенеративных заболеваний
CN117015548A (zh) 合成的熊果酸衍生物和其使用方法
EP4043447B1 (en) Halogenated tetracyclic triterpene derivative, preparation and application thereof
US5516921A (en) Thiono-lactone inhibitors of protein trafficking and uses therefor
WO2025062143A1 (en) 7-difluorinated steroids for use in the treatment of neurological or mitochondrial diseases
WO2023077977A1 (zh) 秋水仙碱衍生物的制备方法及其用途
CN113620967A (zh) 一种α-倒捻子素衍生物及其制备方法和应用
HK1098140B (en) 9-substituted 8-oxoadenine compound