EA200970551A1 - Производные ацетилена и их применение для связывания и визуализации бляшек амилоида - Google Patents

Производные ацетилена и их применение для связывания и визуализации бляшек амилоида

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Publication number
EA200970551A1
EA200970551A1 EA200970551A EA200970551A EA200970551A1 EA 200970551 A1 EA200970551 A1 EA 200970551A1 EA 200970551 A EA200970551 A EA 200970551A EA 200970551 A EA200970551 A EA 200970551A EA 200970551 A1 EA200970551 A1 EA 200970551A1
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EA
Eurasian Patent Office
Prior art keywords
amyloid
methods
acetylene
visualization
derivatives
Prior art date
Application number
EA200970551A
Other languages
English (en)
Inventor
Ханк Ф. Кунг
Мей Пинг Кунг
Original Assignee
Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания
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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Application filed by Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания filed Critical Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания
Publication of EA200970551A1 publication Critical patent/EA200970551A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/78—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C217/80—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/34—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having amino groups and esterified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Настоящее изобретение относится к меченным радиоактивным изотопом соединениям и их использованию в способах визуализации (получения изображения) отложений амилоида, а также к способам их получения. Кроме того, настоящее изобретение относится к соединениям для ингибирования агрегации амилоидных белков, которые образуют отложения амилоида, способам доставки терапевтических средств к отложениям амилоида, а также способам получения соединений, которые ингибируют агрегацию амилоидных белков.
EA200970551A 2006-12-07 2007-12-07 Производные ацетилена и их применение для связывания и визуализации бляшек амилоида EA200970551A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87324906P 2006-12-07 2006-12-07
US11/951,612 US7678819B2 (en) 2006-12-07 2007-12-06 Acetylene derivatives and their use for binding and imaging amyloid plaques
PCT/US2007/025177 WO2008073350A2 (en) 2006-12-07 2007-12-07 Acetylene derivatives and their use for binding and imaging amyloid plaques

Publications (1)

Publication Number Publication Date
EA200970551A1 true EA200970551A1 (ru) 2009-12-30

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ID=39512287

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EA200970551A EA200970551A1 (ru) 2006-12-07 2007-12-07 Производные ацетилена и их применение для связывания и визуализации бляшек амилоида

Country Status (16)

Country Link
US (1) US7678819B2 (ru)
EP (1) EP2089110A2 (ru)
JP (1) JP2010512325A (ru)
KR (1) KR20090090370A (ru)
AU (1) AU2007332818A1 (ru)
BR (1) BRPI0720590A2 (ru)
CA (1) CA2672187A1 (ru)
CO (1) CO6190627A2 (ru)
CR (1) CR10842A (ru)
EA (1) EA200970551A1 (ru)
IL (1) IL199201A (ru)
MX (1) MX2009006075A (ru)
NO (1) NO20092567L (ru)
NZ (1) NZ577458A (ru)
SV (1) SV2009003289A (ru)
WO (1) WO2008073350A2 (ru)

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LT2247558T (lt) 2008-02-14 2022-04-11 Eli Lilly And Company Nauji vizualizavimo agentai neurologinės disfunkcijos aptikimui
US8932557B2 (en) 2008-02-14 2015-01-13 Eli Lilly And Company Imaging agents for detecting neurological dysfunction
JP2011529086A (ja) 2008-07-24 2011-12-01 シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド Ａｄ病変を同定するために有用な造影剤
EP2323696B1 (en) 2008-09-18 2018-09-05 Cedars-Sinai Medical Center Optical method for the detection of alzheimer's disease
CN102438660A (zh) * 2009-03-23 2012-05-02 美国西门子医疗解决公司 用于检测神经障碍的显像剂
US8691187B2 (en) * 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
WO2011045415A2 (en) 2009-10-15 2011-04-21 Guerbet New imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases
US9259495B2 (en) * 2010-10-12 2016-02-16 Mayo Foundation For Medical Education And Research Imaging of meningiomas using phenylbenzothiazole, stilbene, or biphenylalkyne derivatives
CN107412788B (zh) * 2012-12-21 2021-06-18 国立研究开发法人量子科学技术研究开发机构 用于对脑内所蓄积的Tau蛋白质进行成像的新的化合物
US9895324B2 (en) 2014-03-26 2018-02-20 University Of Kentucky Research Foundation Halogenated diarylacetylenes and methods of treating cancer
CN107847466B (zh) 2015-04-08 2024-02-06 贝欧曼蒂克丝公司 用于调节创伤愈合的配制物和方法
JP7456621B2 (ja) * 2018-08-07 2024-03-27 慶應義塾 神経機能調節物質の動態の検出剤、及び神経機能調節物質の検出方法

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Also Published As

Publication number Publication date
AU2007332818A1 (en) 2008-06-19
CA2672187A1 (en) 2008-06-19
BRPI0720590A2 (pt) 2014-04-08
SV2009003289A (es) 2009-10-02
KR20090090370A (ko) 2009-08-25
NZ577458A (en) 2012-01-12
JP2010512325A (ja) 2010-04-22
CO6190627A2 (es) 2010-08-19
WO2008073350A2 (en) 2008-06-19
US20080166299A1 (en) 2008-07-10
US7678819B2 (en) 2010-03-16
EP2089110A2 (en) 2009-08-19
CR10842A (es) 2009-10-13
IL199201A (en) 2013-05-30
WO2008073350A3 (en) 2008-08-14
MX2009006075A (es) 2009-06-30
NO20092567L (no) 2009-09-04

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