JP2010523599A - クリックケミストリーを使用した炭酸脱水酵素−ｉｘのための分子イメージングプローブの開発 - Google Patents

クリックケミストリーを使用した炭酸脱水酵素−ｉｘのための分子イメージングプローブの開発 Download PDF

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Publication number
JP2010523599A
JP2010523599A JP2010502352A JP2010502352A JP2010523599A JP 2010523599 A JP2010523599 A JP 2010523599A JP 2010502352 A JP2010502352 A JP 2010502352A JP 2010502352 A JP2010502352 A JP 2010502352A JP 2010523599 A JP2010523599 A JP 2010523599A
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Prior art keywords
methyl
alkyl
triazol
yloxy
phenyl
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Pending
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JP2010502352A
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Japanese (ja)
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JP2010523599A5 (enExample
Inventor
シー コルプ、ハルトムート
シー ウォルシュ、ジョセフ
カシ、ダーナラクシュミ
モカルラ、ヴァニ
ワン、ビン
ビー ガンガドハルマト、ウメシュ
エイ ダクロス、ブライアン
チェン、カイ
ツァン、ウェイ
チェン、ガン
クリフトン パジェット、ヘンリー
カリミ、ファルハド
ジェイ エイチ スコット、ペーター
ガオ、ツィヤン
リン、キアンワ
リー カリアー、トーマス
ツァオ、ティミン
クシャ、チュンファン
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Siemens Medical Solutions USA Inc
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Siemens Medical Solutions USA Inc
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Publication of JP2010523599A publication Critical patent/JP2010523599A/ja
Publication of JP2010523599A5 publication Critical patent/JP2010523599A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
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    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
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    • G01N2500/00—Screening for compounds of potential therapeutic value
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Analytical Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Radiology & Medical Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2010502352A 2007-04-05 2008-04-07 クリックケミストリーを使用した炭酸脱水酵素−ｉｘのための分子イメージングプローブの開発 Pending JP2010523599A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92206507P 2007-04-05 2007-04-05
PCT/US2008/059599 WO2008124703A2 (en) 2007-04-05 2008-04-07 Development of molecular imaging probes for carbonic anhydrase-ix using click chemistry

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JP2010523599A true JP2010523599A (ja) 2010-07-15
JP2010523599A5 JP2010523599A5 (enExample) 2010-12-02

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US (2) US7829063B2 (enExample)
EP (2) EP2129666A2 (enExample)
JP (1) JP2010523599A (enExample)
KR (2) KR20120003499A (enExample)
CN (1) CN101679318A (enExample)
CA (1) CA2683434A1 (enExample)
WO (1) WO2008124703A2 (enExample)

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JP2011509304A (ja) * 2008-01-09 2011-03-24 モレキュラ インサイト ファーマシューティカルズ インコーポレイテッド 炭酸脱水酵素ｉｘの阻害剤
WO2012161177A1 (ja) * 2011-05-24 2012-11-29 アステラス製薬株式会社 腫瘍の画像診断用標識誘導体
US8840865B2 (en) 2008-01-09 2014-09-23 Molecular Insight Pharmaceuticals, Inc. Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof
US9120837B2 (en) 2012-01-06 2015-09-01 Molecular Insight Pharmaceuticals Metal complexes of poly(carboxyl)amine-containing ligands having an affinity for carbonic anhydrase IX
US9149547B2 (en) 2009-06-15 2015-10-06 Molecular Insight Pharmaceuticals, Inc. Process for production of heterodimers of glutamic acid
US10086096B2 (en) 2013-01-14 2018-10-02 Molecular Insight Pharmaceuticals, Inc. Triazine based radiopharmaceuticals and radioimaging agents
JP2019514984A (ja) * 2016-05-13 2019-06-06 ザ・ジョンズ・ホプキンス・ユニバーシティ 炭酸脱水酵素ｉｘを標的にする核造影および放射性治療剤ならびにそれらの使用
JP2019214626A (ja) * 2014-09-16 2019-12-19 ギリアード サイエンシーズ， インコーポレイテッド Ｔｏｌｌ様受容体モジュレーターを調製する方法
CN110785414A (zh) * 2017-04-20 2020-02-11 加利福尼亚大学董事会 K-Ras调节剂

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EA026557B1 (ru) 2008-12-09 2017-04-28 Джилид Сайэнс, Инк. Промежуточные соединения для получения модуляторов толл-подобных рецепторов
WO2011018798A2 (en) * 2009-08-14 2011-02-17 Indian Association For The Cultivation Of Science Morpholino-based antisense agent
EP2491014A1 (en) * 2009-10-21 2012-08-29 Bayer Pharma Aktiengesellschaft Substituted halophenoxybenzamide derivatives
JP6245981B2 (ja) * 2010-04-08 2017-12-13 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Ｓｉｅｍｅｎｓ Ｍｅｄｉｃａｌ Ｓｏｌｕｔｉｏｎｓ ＵＳＡ，Ｉｎｃ． 含水有機溶媒中の１８ｆ−標識化トレーサーの合成
US10639608B2 (en) 2010-04-08 2020-05-05 Siemens Medical Solutions Usa, Inc. System, device and method for preparing tracers and transferring materials during radiosynthesis
DK2634177T3 (en) * 2010-10-29 2016-08-15 Clino Ltd TAU IMAGE SOUND
CA2817691C (en) * 2010-11-13 2020-09-01 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
US9180209B2 (en) * 2011-02-28 2015-11-10 The Board Of Trustees Of The Leland Stanford Junior University Non-peptidic quenched fluorescent imaging probes
CN102219753B (zh) * 2011-04-21 2012-10-31 山东大学 一种三氮唑类化合物及其制备方法与应用
WO2012154885A2 (en) 2011-05-09 2012-11-15 Visen Medical, Inc. Carbonic anhydrase targeting agents and methods of using same
WO2013148319A1 (en) 2012-03-30 2013-10-03 Visen Medical, Inc. Bacterial imaging agents and methods of using same
CA2929401A1 (en) 2013-11-05 2015-05-14 Bayer Cropscience Aktiengesellschaft Novel compounds for combating arthropods
PT3166607T (pt) 2014-07-11 2022-12-07 Gilead Sciences Inc Moduladores de receptores de tipo toll para o tratamento do vih
CN104212440B (zh) * 2014-09-03 2016-03-30 无锡艾德美特生物科技有限公司 一类喹唑啉类荧光探针及其制备和应用
AU2015318061B2 (en) 2014-09-16 2018-05-17 Gilead Sciences, Inc. Solid forms of a toll-like receptor modulator
CN107428776B (zh) 2015-03-24 2020-10-23 H.隆德贝克有限公司 制造4,5,6,7-四氢异噁唑并[5,4-c]吡啶-3-醇
LT6401B (lt) 2015-07-28 2017-06-12 Vilniaus Universitetas Karboanhidrazės selektyvūs inhibitoriai
CN105541825A (zh) * 2015-12-28 2016-05-04 中国药科大学 三氮唑衍生物制备方法及其作为药物的用途
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DK3668856T3 (da) 2017-08-17 2021-09-20 Glaxosmithkline Ip Dev Ltd Hidtil ukendte tetrazolforbindelser og anvendelse deraf til behandling af tuberkulose
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WO2025113696A1 (zh) * 2023-11-30 2025-06-05 赣州和美药业股份有限公司 一种化合物及其应用

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Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011509304A (ja) * 2008-01-09 2011-03-24 モレキュラ インサイト ファーマシューティカルズ インコーポレイテッド 炭酸脱水酵素ｉｘの阻害剤
US8840865B2 (en) 2008-01-09 2014-09-23 Molecular Insight Pharmaceuticals, Inc. Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof
US8877970B2 (en) 2008-01-09 2014-11-04 Molecular Insight Pharmaceuticals, Inc. Inhibitors of carbonic anhydrase IX
US8962799B2 (en) 2008-01-09 2015-02-24 Molecular Insight Pharmaceuticals, Inc. Technetium—and rhenium-bis(heteroaryl) complexes and methods of use thereof
US9433594B2 (en) 2008-01-09 2016-09-06 Molecular Insight Pharmaceuticals, Inc. Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof
US9149547B2 (en) 2009-06-15 2015-10-06 Molecular Insight Pharmaceuticals, Inc. Process for production of heterodimers of glutamic acid
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