EA201100267A1 - Новые бензофураны, подходящие в качестве предшественников соединений, которые являются полезными для визуализации амилоидных отложений - Google Patents

Новые бензофураны, подходящие в качестве предшественников соединений, которые являются полезными для визуализации амилоидных отложений

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Publication number
EA201100267A1
EA201100267A1 EA201100267A EA201100267A EA201100267A1 EA 201100267 A1 EA201100267 A1 EA 201100267A1 EA 201100267 A EA201100267 A EA 201100267A EA 201100267 A EA201100267 A EA 201100267A EA 201100267 A1 EA201100267 A1 EA 201100267A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
useful
new
benzofuranes
sediments
Prior art date
Application number
EA201100267A
Other languages
English (en)
Other versions
EA019093B1 (ru
Inventor
Сет Бьёрк
Верн Делиссер
Петер Йохнстрём
Нильс Андерс Нильссон
Катинка Руда
Пер Магнус Скоу
Бритт-Марие Свахн
Original Assignee
Астразенека Аб
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.)
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Publication date
Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of EA201100267A1 publication Critical patent/EA201100267A1/ru
Publication of EA019093B1 publication Critical patent/EA019093B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/76—Nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hospice & Palliative Care (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

Настоящее изобретение относится к новым производным, которые являются подходящими в качестве предшественников соединений, которые являются полезными для визуализации амилоидных отложений у живых пациентов, к их композициям, способам применения и способам получения таких соединений. Соединения, происходящие от этих предшественников, являются полезными в способах визуализации амилоидных отложений в мозге in vivo для обеспечения прижизненной диагностики болезни Альцгеймера позитронно-эмиссионной томографией (ПЭТ), а также измерения клинической эффективности терапевтических агентов против болезни Альцгеймера. Кроме того, настоящее изобретение также раскрывает данные соединения-предшественники в кристаллической форме.
EA201100267A 2008-08-29 2009-08-28 Новые бензофураны, подходящие в качестве предшественников соединений, которые являются полезными для визуализации амилоидных отложений EA019093B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9285108P 2008-08-29 2008-08-29
PCT/SE2009/050972 WO2010024769A1 (en) 2008-08-29 2009-08-28 New benzofurans suitable as precursors to compounds that are useful for imaging amyloid deposits

Publications (2)

Publication Number Publication Date
EA201100267A1 true EA201100267A1 (ru) 2011-10-31
EA019093B1 EA019093B1 (ru) 2014-01-30

Family

ID=41721733

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100267A EA019093B1 (ru) 2008-08-29 2009-08-28 Новые бензофураны, подходящие в качестве предшественников соединений, которые являются полезными для визуализации амилоидных отложений

Country Status (22)

Country Link
US (3) US8193363B2 (ru)
EP (1) EP2328891B1 (ru)
JP (1) JP5613669B2 (ru)
KR (1) KR101648848B1 (ru)
CN (3) CN104447710A (ru)
AR (2) AR073230A1 (ru)
AU (1) AU2009286176B2 (ru)
BR (1) BRPI0917147B8 (ru)
CA (1) CA2735497C (ru)
CL (1) CL2011000420A1 (ru)
CO (1) CO6341628A2 (ru)
EA (1) EA019093B1 (ru)
EC (1) ECSP11010850A (ru)
ES (1) ES2627769T3 (ru)
IL (1) IL211188A0 (ru)
MX (1) MX2011001918A (ru)
NZ (1) NZ591446A (ru)
PE (1) PE20110393A1 (ru)
TW (1) TW201014848A (ru)
UY (1) UY32076A (ru)
WO (1) WO2010024769A1 (ru)
ZA (1) ZA201102284B (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8193363B2 (en) 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits
JP5825608B2 (ja) * 2010-08-06 2015-12-02 国立大学法人京都大学 ピリジルベンゾフラン誘導体
US10098859B2 (en) 2012-09-05 2018-10-16 Amri Ssci, Llc Cocrystals of p-coumaric acid
EP2767532B1 (en) 2012-12-21 2016-07-13 National Institutes for Quantum and Radiological Science and Technology Novel compound for imaging tau protein accumulated in the brain
WO2016029146A1 (en) * 2014-08-22 2016-02-25 University Of Washington Specific inhibitors of methionyl-trna synthetase
CA3006054A1 (en) * 2015-11-20 2017-05-26 Navidea Biopharmaceuticals, Inc. Formulations for 2-heteroaryl substituted benzofurans
TWI759962B (zh) 2019-11-13 2022-04-01 香港商新旭生技股份有限公司 用於降解tau蛋白聚集體的化合物及其用途

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EP0735821A4 (en) 1993-12-21 1998-04-01 Lilly Co Eli METHODS FOR TREATING OR PREVENTING CONDITIONS ASSOCIATED WITH AMYLO DOGEN PEPTIDES
HUP0203294A3 (en) * 1999-10-15 2003-03-28 Hoffmann La Roche Benzodiazepine derivatives, process for their preparation, pharmaceutical compositions containing them and their use
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US8193363B2 (en) 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits

Also Published As

Publication number Publication date
PE20110393A1 (es) 2011-07-15
JP5613669B2 (ja) 2014-10-29
ES2627769T3 (es) 2017-07-31
US20100056796A1 (en) 2010-03-04
EA019093B1 (ru) 2014-01-30
JP2012501324A (ja) 2012-01-19
CL2011000420A1 (es) 2011-07-15
KR20110045023A (ko) 2011-05-03
TW201014848A (en) 2010-04-16
AR073230A1 (es) 2010-10-20
EP2328891A1 (en) 2011-06-08
CA2735497C (en) 2016-07-19
CN104478862B (zh) 2017-05-24
US9309267B2 (en) 2016-04-12
BRPI0917147B1 (pt) 2020-09-15
CO6341628A2 (es) 2011-11-21
NZ591446A (en) 2012-08-31
MX2011001918A (es) 2011-03-24
UY32076A (es) 2010-03-26
AU2009286176A1 (en) 2010-03-04
AU2009286176B2 (en) 2012-04-26
CN102197036A (zh) 2011-09-21
EP2328891A4 (en) 2012-07-04
US20140296534A1 (en) 2014-10-02
EP2328891B1 (en) 2017-04-05
IL211188A0 (en) 2011-04-28
US8193363B2 (en) 2012-06-05
US8653274B2 (en) 2014-02-18
KR101648848B1 (ko) 2016-08-17
CA2735497A1 (en) 2010-03-04
ECSP11010850A (es) 2011-03-31
CN104447710A (zh) 2015-03-25
WO2010024769A1 (en) 2010-03-04
AR114029A2 (es) 2020-07-15
BRPI0917147B8 (pt) 2021-05-25
BRPI0917147A2 (pt) 2015-11-17
US20120264943A1 (en) 2012-10-18
CN102197036B (zh) 2014-12-10
CN104478862A (zh) 2015-04-01
ZA201102284B (en) 2012-09-26

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