JP2011505363A - α−フルオロアルキルテトラベナジン及びジヒドロテトラベナジンイメージング剤並びにプローブ - Google Patents

α−フルオロアルキルテトラベナジン及びジヒドロテトラベナジンイメージング剤並びにプローブ Download PDF

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Publication number
JP2011505363A
JP2011505363A JP2010536109A JP2010536109A JP2011505363A JP 2011505363 A JP2011505363 A JP 2011505363A JP 2010536109 A JP2010536109 A JP 2010536109A JP 2010536109 A JP2010536109 A JP 2010536109A JP 2011505363 A JP2011505363 A JP 2011505363A
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Prior art keywords
group
compound
aliphatic group
hydrogen
enantiomer
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JP2010536109A
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English (en)
Japanese (ja)
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JP2011505363A5 (enExample
Inventor
リシェル，マイケル・ジェームズ
ジョンソン，ブルース・フレッチャー
アマラシンゲ，カンデ・カンカナナマラゲ・ダヤラスナ
ディン，ショーン・リチャード
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General Electric Co
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General Electric Co
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Publication date
Priority claimed from US11/947,275 external-priority patent/US7910738B2/en
Priority claimed from US11/947,215 external-priority patent/US7902364B2/en
Application filed by General Electric Co filed Critical General Electric Co
Publication of JP2011505363A publication Critical patent/JP2011505363A/ja
Publication of JP2011505363A5 publication Critical patent/JP2011505363A5/ja
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2010536109A 2007-11-29 2008-11-25 α−フルオロアルキルテトラベナジン及びジヒドロテトラベナジンイメージング剤並びにプローブ Ceased JP2011505363A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US11/947,275 US7910738B2 (en) 2007-11-29 2007-11-29 Intermediates for alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
US11/947,215 US7902364B2 (en) 2007-11-29 2007-11-29 Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
US12/174,167 US8053578B2 (en) 2007-11-29 2008-07-16 Alpha-fluoroalkyl dihydrotetrabenazine imaging agents and probes
PCT/US2008/084601 WO2009070552A1 (en) 2007-11-29 2008-11-25 Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes

Publications (2)

Publication Number Publication Date
JP2011505363A true JP2011505363A (ja) 2011-02-24
JP2011505363A5 JP2011505363A5 (enExample) 2014-01-09

Family

ID=40297912

Family Applications (1)

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JP2010536109A Ceased JP2011505363A (ja) 2007-11-29 2008-11-25 α−フルオロアルキルテトラベナジン及びジヒドロテトラベナジンイメージング剤並びにプローブ

Country Status (5)

Country Link
US (1) US8053578B2 (enExample)
EP (2) EP2217599A1 (enExample)
JP (1) JP2011505363A (enExample)
CN (1) CN101878213B (enExample)
WO (1) WO2009070552A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016506957A (ja) * 2013-01-31 2016-03-07 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｖｍａｔ２のベンゾキノロン阻害剤

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120003330A1 (en) * 2010-06-01 2012-01-05 Auspex Pharmaceuticals, Inc. Benzoquinolone inhibitors of vmat2
EP2758041B1 (de) * 2011-09-20 2021-01-13 Basf Se Niedermolekulare modulatoren des kälte-menthol-rezeptors trpm8 und deren verwendung
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
JP6362601B2 (ja) 2012-09-18 2018-07-25 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 小胞モノアミン輸送体２の重水素化ベンゾキノリン阻害剤の製剤薬物動態
CA2925562A1 (en) * 2013-09-27 2015-04-02 Auspex Pharmaceuticals, Inc. Benzoquinolone inhibitors of vmat2
WO2015077521A1 (en) * 2013-11-22 2015-05-28 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
AU2014357518A1 (en) 2013-12-03 2016-06-09 Auspex Pharmaceuticals, Inc. Methods of manufacturing benzoquinoline compounds
KR20160111999A (ko) * 2014-01-27 2016-09-27 오스펙스 파마슈티칼스, 인코포레이티드 소포성 모노아민 수송체 2의 벤조퀴놀린 억제제
PL3265085T3 (pl) 2015-03-06 2022-11-07 Auspex Pharmaceuticals, Inc. Sposoby leczenia zaburzeń związanych z nieprawidłowymi ruchami mimowolnymi
PE20240822A1 (es) * 2021-03-22 2024-04-18 Neurocrine Biosciences Inc Inhibidores de vmat2 y metodos de uso
WO2026050236A1 (en) 2024-08-27 2026-03-05 Neurocrine Biosciences, Inc. Muscarinic receptor agonist in combination with a vesicular monoamine transporter 2 inhibitor, for use in the treatment of a neurological or psychiatric disorder

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2843591A (en) * 1958-07-15 Method for preparing same
DE1068261B (de) * 1959-11-05 F. Hoffmann-La Roche £v Co. Aktiengesellschaft, Basel (Schweiz) Verfahren zur Herstellung von substituierten 2-Oxobenzo-chinollizinen
JPS545999A (en) * 1977-06-15 1979-01-17 Chinoin Gyogyszer Es Vegyeszet Novel benzoquinolidine derivative and its preparation
WO1993016730A1 (en) * 1992-02-28 1993-09-02 The Trustees Of The University Of Pennsylvania Iodine derivatives of tetrabenazyne
WO2007130365A2 (en) * 2006-05-02 2007-11-15 The Trustees Of The University Of Pennsylvania Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2410947B (en) 2004-02-11 2008-09-17 Cambridge Lab Ltd Pharmaceutical compounds
CA2623794A1 (en) 2005-06-29 2007-01-11 The Trustees Of Columbia University In The City Of New York Use of dtbz for imaging endocrine pancreas and beta cell mass in type 1 diabetes
ES2318771T3 (es) 2005-08-06 2009-05-01 Cambridge Laboratories (Ireland) Limited 3,11b-cis-dihidrotetrabenazinas para el tratamiento de la esquizofrenia y otras psicosis.
US8008500B2 (en) 2007-06-08 2011-08-30 General Electric Company Intermediates useful for making tetrabenazine compounds
US7902364B2 (en) * 2007-11-29 2011-03-08 General Electric Company Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2843591A (en) * 1958-07-15 Method for preparing same
DE1068261B (de) * 1959-11-05 F. Hoffmann-La Roche £v Co. Aktiengesellschaft, Basel (Schweiz) Verfahren zur Herstellung von substituierten 2-Oxobenzo-chinollizinen
JPS545999A (en) * 1977-06-15 1979-01-17 Chinoin Gyogyszer Es Vegyeszet Novel benzoquinolidine derivative and its preparation
WO1993016730A1 (en) * 1992-02-28 1993-09-02 The Trustees Of The University Of Pennsylvania Iodine derivatives of tetrabenazyne
WO2007130365A2 (en) * 2006-05-02 2007-11-15 The Trustees Of The University Of Pennsylvania Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JPN6013034074; Ｎｕｃｌｅａｒ　Ｍｅｄｉｃｉｎｅ　ａｎｄ　Ｂｉｏｌｏｇｙ Ｖｏｌ．３３, 2006, Ｐ．６８５-６９４ *
JPN6013034076; Ｎｕｃｌｅａｒ　Ｍｅｄｉｃｉｎｅ　ａｎｄ　Ｂｉｏｌｏｇｙ Ｖｏｌ．３４, 200704, Ｐ．２３９-２４６ *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016506957A (ja) * 2013-01-31 2016-03-07 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｖｍａｔ２のベンゾキノロン阻害剤
JP2019048829A (ja) * 2013-01-31 2019-03-28 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｖｍａｔ２のベンゾキノロン阻害剤

Also Published As

Publication number Publication date
EP2594568A1 (en) 2013-05-22
WO2009070552A1 (en) 2009-06-04
US20090142276A1 (en) 2009-06-04
US8053578B2 (en) 2011-11-08
CN101878213A (zh) 2010-11-03
EP2217599A1 (en) 2010-08-18
CN101878213B (zh) 2013-05-29

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