DK2012833T3 - Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler - Google Patents

Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler Download PDF

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Publication number
DK2012833T3
DK2012833T3 DK07776522.0T DK07776522T DK2012833T3 DK 2012833 T3 DK2012833 T3 DK 2012833T3 DK 07776522 T DK07776522 T DK 07776522T DK 2012833 T3 DK2012833 T3 DK 2012833T3
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DK
Denmark
Prior art keywords
compounds
imaging
binding
compound
dtbz
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DK07776522.0T
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English (en)
Inventor
Mei-Ping Kung
Michael Kilbourn
Hank F Kung
Daniel M Skovronsky
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Univ Pennsylvania
Avid Radiopharmaceuticals Inc
Univ Michigan
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Application filed by Univ Pennsylvania, Avid Radiopharmaceuticals Inc, Univ Michigan filed Critical Univ Pennsylvania
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Publication of DK2012833T3 publication Critical patent/DK2012833T3/da

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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C07D455/06—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (6)

  1. )ATENTKRAV Forbindelse med formlen
    eller et farmaceutisk acceptabelt salt deraf.
  2. Forbindelse ifølge krav 1, der er
    oprenset fra dens stereoisomerer.
  3. 3. Forbindelse med formlen
    hvor Ms er methansulfonyl; og n er 2 eller 3.
  4. 4. Forbindelse ifølge krav 3, der er
  5. 5. Fremgangsmåde til fremstilling af en forbindelse med følgende struktur:
    hvilken fremgangsmåde omfatter omsætning af en forbindelse med formlen
    hvor MsO er mesylat; med 18F anion.
  6. 6. Diagnostisk sammensætning til billeddannelse af vesikulære monoamintransportere, hvilken sammensætning omfatter:
    eller et farmaceutisk acceptabelt salt deraf, og et farmaceutisk acceptabelt bærestof eller fortyndingsmiddel. Fremgangsmåde til billeddannelse af vesikulære monoamintransportere, hvilken fremgangsmåde omfatter: a. introduktion i et pattedyr af en detekterbar mængde af en diagnostisk sammensætning ifølge krav 6; b. tildeling af tilstrækkelig tid, til at den mærkede forbindelse forbindes med transporterne og c. detektering af den mærkede forbindelse forbundet med én eller flere af transporterne.
DK07776522.0T 2006-05-02 2007-05-01 Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler DK2012833T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US79651806P 2006-05-02 2006-05-02
US90811607P 2007-03-26 2007-03-26
PCT/US2007/010478 WO2007130365A2 (en) 2006-05-02 2007-05-01 Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents

Publications (1)

Publication Number Publication Date
DK2012833T3 true DK2012833T3 (da) 2015-01-19

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DK07776522.0T DK2012833T3 (da) 2006-05-02 2007-05-01 Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler

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Country Link
US (1) US8562949B2 (da)
EP (2) EP2012833B1 (da)
JP (1) JP5392622B2 (da)
KR (1) KR101429302B1 (da)
CN (1) CN101484190B (da)
AU (1) AU2007248764B2 (da)
BR (1) BRPI0711481A8 (da)
CA (1) CA2650904C (da)
DK (1) DK2012833T3 (da)
ES (1) ES2525932T3 (da)
IL (1) IL195044A (da)
MX (1) MX2008014064A (da)
NO (1) NO341065B1 (da)
PL (1) PL2012833T3 (da)
PT (1) PT2012833E (da)
SI (1) SI2012833T1 (da)
TW (1) TWI432214B (da)
WO (1) WO2007130365A2 (da)
ZA (1) ZA200810200B (da)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8008500B2 (en) 2007-06-08 2011-08-30 General Electric Company Intermediates useful for making tetrabenazine compounds
JP5663309B2 (ja) * 2007-10-25 2015-02-04 ゼネラル・エレクトリック・カンパニイ フッ素化ジヒドロテトラベナジンエーテルイメージング剤及びプローブ
US7897770B2 (en) 2007-10-25 2011-03-01 General Electric Company Fluorinated dihydrotetrabenazine ether imaging agents and probes
US7897769B2 (en) 2007-10-25 2011-03-01 General Electric Company Intermediates for fluorinated dihydrotetrabenazine ether imaging agents and probes
JP2011502966A (ja) * 2007-10-31 2011-01-27 アルセレス ファーマシューティカルズ， インコーポレイテッド ドーパミントランスポーターレベルを評価することによるレビー小体型認知症の診断およびレビー小体型認知症の処置のモニタリングのための方法
US7910738B2 (en) 2007-11-29 2011-03-22 General Electric Company Intermediates for alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
US8053578B2 (en) 2007-11-29 2011-11-08 General Electric Company Alpha-fluoroalkyl dihydrotetrabenazine imaging agents and probes
US7902364B2 (en) 2007-11-29 2011-03-08 General Electric Company Alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
US7919622B2 (en) 2007-12-07 2011-04-05 Kande Kankanamalage Dayarathna Amarasinghe Intermediates for fluorinated tetrabenazine carbinol compounds imaging agents and probes
US8013161B1 (en) 2007-12-07 2011-09-06 General Electric Company Fluoroalkyl tetrabenazine carbinol compounds as imaging agents and probes
GB2463452A (en) * 2008-09-08 2010-03-17 Cambridge Lab Desmethyl derivatives of tetrabenazine and pharmaceutical compositions thereof
US8524733B2 (en) * 2008-09-18 2013-09-03 Auspex Pharmaceuticals Benzoquinoline inhibitors of vesicular monoamine transporter 2
WO2010107029A1 (ja) * 2009-03-19 2010-09-23 国立大学法人京都大学 膵島イメージング用分子プローブ前駆体及びその使用
CN102120742B (zh) * 2010-01-08 2013-03-13 中国药科大学 一种丁苯那嗪的制备方法
US20120003330A1 (en) 2010-06-01 2012-01-05 Auspex Pharmaceuticals, Inc. Benzoquinolone inhibitors of vmat2
EP2394668A1 (en) * 2010-06-01 2011-12-14 Julius-Maximilians-Universität Würzburg PET radiopharmaceuticals for differential diagnosis between bilateral and unilateral conditions of primary hyperaldosteronism
CN101985446B (zh) * 2010-06-10 2012-05-30 江苏省原子医学研究所 一种(±)-9-O-去甲基-α-二氢丁苯那嗪合成方法
WO2012121746A2 (en) * 2011-03-09 2012-09-13 The General Hospital Corporation Imaging beta cell mass
CN102260255B (zh) * 2011-07-07 2013-07-10 江苏省原子医学研究所 一种9,10-二甲氧基-1,3,4,6,7,11b-六氢-3-异丁基-2H-苯并[a]喹嗪-2-酮的简便合成方法
BR112015005894B1 (pt) 2012-09-18 2022-03-29 Auspex Pharmaceuticals, Inc Composto, composição farmacêutica, método para tratar um distúrbio mediado por vmat2 e formulação farmacêutica de liberação prolongada
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
CN102936246A (zh) * 2012-11-08 2013-02-20 江苏暨明医药科技有限公司 丁苯那嗪的合成方法
EA201500801A1 (ru) 2013-01-31 2016-01-29 Ауспекс Фармацетикалс, Инк. Бензохинолоновые ингибиторы vmat2
EP3049087A4 (en) * 2013-09-27 2017-05-24 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
MX2016006622A (es) * 2013-11-22 2016-12-09 Auspex Pharmaceuticals Inc Metodos para tratar actividad muscular anormal.
AU2014357518A1 (en) 2013-12-03 2016-06-09 Auspex Pharmaceuticals, Inc. Methods of manufacturing benzoquinoline compounds
EP3099299A4 (en) 2014-01-27 2017-10-04 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
CA2938244A1 (en) 2014-02-07 2015-08-13 Auspex Pharamaceuticals, Inc. Novel pharmaceutical formulations
KR102528845B1 (ko) 2015-03-06 2023-05-08 오스펙스 파마슈티칼스, 인코포레이티드 비정상적 불수의 운동 장애의 치료 방법
JP2018530612A (ja) 2015-10-09 2018-10-18 テバ、ファーマスーティカルズ、インターナショナル、ゲゼルシャフト、ミット、ベシュレンクテル、ハフツングＴｅｖａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｔｅｒｎａｔｉｏｎａｌ Ｇｍｂｈ パーキンソン病の治療のための重水素化レボドパとカルビドパおよびオピカポンとの組合せ
TW201906818A (zh) * 2017-05-31 2019-02-16 美商５１１製藥公司 新穎氘取代之正子發射斷層掃描（ｐｅｔ）顯影劑及其藥理應用
CN108912118A (zh) * 2018-07-12 2018-11-30 新乡学院 一种四氢异喹啉并三嗪骨架化合物及其制备方法
CN114302883B (zh) * 2019-08-12 2022-09-06 山东绿叶制药有限公司 Vmat2抑制剂及其制备方法和应用
CN111320620A (zh) * 2020-03-17 2020-06-23 四川大学华西医院 一种异喹啉并哒嗪酮类化合物及其合成方法和应用
PE20240822A1 (es) 2021-03-22 2024-04-18 Neurocrine Biosciences Inc Inhibidores de vmat2 y metodos de uso
CN114288419B (zh) * 2021-12-30 2023-08-18 中山大学附属第八医院（深圳福田） 一种利福平纳米递药系统的制备及其在防治帕金森病方面的应用
CN115536705A (zh) * 2022-09-23 2022-12-30 江苏省原子医学研究所 靶向ii型囊泡单胺转运体分子探针及其制备方法和应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3053845A (en) 1962-09-11 Benzofykedocolines
DE1470074C3 (de) * 1964-07-25 1974-01-24 Merck Patent Gmbh, 6100 Darmstadt 1,2,3,4,6,7-Hexahydro-l lbH-benzo eckige Klammer auf a eckige Klammer zu chinolizine sowie deren Acetate und/oder phsiologisch verträgliche Säureadditionssalze sowie Verfahren zu ihrer Herstellung
GB1513824A (en) * 1975-05-22 1978-06-14 Wyeth John & Brother Ltd 1,3,4,6,7,11b-hexahydro-2h-benzo(a)quinolizine derivative
US5278308A (en) 1992-02-28 1994-01-11 The Trustees Of The University Of Pennsylvania Iodine derivatives of tetrabenazine
FR2770215B1 (fr) * 1997-10-28 2000-01-14 Pf Medicament Derives d'aminomethyl-benzo[a]quinolizidine, leur preparation et leur application en therapeutique pour les maladies neurodegeneratives
GB2410947B (en) * 2004-02-11 2008-09-17 Cambridge Lab Ltd Pharmaceutical compounds

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US8562949B2 (en) 2013-10-22
IL195044A (en) 2013-08-29
EP2012833A4 (en) 2011-06-29
ES2525932T3 (es) 2015-01-02
SI2012833T1 (sl) 2015-03-31
EP2604290A3 (en) 2013-07-10
WO2007130365A2 (en) 2007-11-15
CN101484190B (zh) 2011-07-20
EP2604290A2 (en) 2013-06-19
IL195044A0 (en) 2011-08-01
MX2008014064A (es) 2009-06-12
BRPI0711481A8 (pt) 2017-11-28
KR101429302B1 (ko) 2014-08-11
ZA200810200B (en) 2012-02-29
JP2009535403A (ja) 2009-10-01
CN101484190A (zh) 2009-07-15
CA2650904A1 (en) 2007-11-15
BRPI0711481A2 (pt) 2011-11-16
US20080050312A1 (en) 2008-02-28
NO20085004L (no) 2009-02-02
AU2007248764A1 (en) 2007-11-15
CA2650904C (en) 2015-07-07
JP5392622B2 (ja) 2014-01-22
EP2012833B1 (en) 2014-10-29
NO341065B1 (no) 2017-08-14
TWI432214B (zh) 2014-04-01
AU2007248764B2 (en) 2013-08-01
KR20090007781A (ko) 2009-01-20
WO2007130365A3 (en) 2008-11-27
PT2012833E (pt) 2014-12-23
EP2012833A2 (en) 2009-01-14
PL2012833T3 (pl) 2015-05-29
TW200810783A (en) 2008-03-01

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