DK2012833T3 - Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler - Google Patents
Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler Download PDFInfo
- 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
- Authority
- DK
- Denmark
- Prior art keywords
- compounds
- imaging
- binding
- compound
- dtbz
- Prior art date
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Classifications
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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
Landscapes
- 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)
- )ATENTKRAV Forbindelse med formleneller et farmaceutisk acceptabelt salt deraf.
- Forbindelse ifølge krav 1, der eroprenset fra dens stereoisomerer.
- 3. Forbindelse med formlenhvor Ms er methansulfonyl; og n er 2 eller 3.
- 4. Forbindelse ifølge krav 3, der er
- 5. Fremgangsmåde til fremstilling af en forbindelse med følgende struktur:hvilken fremgangsmåde omfatter omsætning af en forbindelse med formlenhvor MsO er mesylat; med 18F anion.
- 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.
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 |
Family
ID=38668238
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK07776522.0T DK2012833T3 (da) | 2006-05-02 | 2007-05-01 | Radioaktivt mærkrede dihydrotetrabenazinderivater og anvendelse heraf som billeddannelsesmidler |
Country Status (19)
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)
Publication number | Priority date | Publication date | Assignee | Title |
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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)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
-
2007
- 2007-05-01 EP EP07776522.0A patent/EP2012833B1/en active Active
- 2007-05-01 TW TW096115465A patent/TWI432214B/zh not_active IP Right Cessation
- 2007-05-01 ES ES07776522.0T patent/ES2525932T3/es active Active
- 2007-05-01 KR KR1020087029358A patent/KR101429302B1/ko active IP Right Grant
- 2007-05-01 PL PL07776522T patent/PL2012833T3/pl unknown
- 2007-05-01 EP EP13152239.3A patent/EP2604290A3/en not_active Withdrawn
- 2007-05-01 MX MX2008014064A patent/MX2008014064A/es active IP Right Grant
- 2007-05-01 WO PCT/US2007/010478 patent/WO2007130365A2/en active Application Filing
- 2007-05-01 DK DK07776522.0T patent/DK2012833T3/da active
- 2007-05-01 AU AU2007248764A patent/AU2007248764B2/en active Active
- 2007-05-01 BR BRPI0711481A patent/BRPI0711481A8/pt not_active Application Discontinuation
- 2007-05-01 SI SI200731600T patent/SI2012833T1/sl unknown
- 2007-05-01 PT PT77765220T patent/PT2012833E/pt unknown
- 2007-05-01 CN CN2007800251116A patent/CN101484190B/zh active Active
- 2007-05-01 JP JP2009509647A patent/JP5392622B2/ja active Active
- 2007-05-01 CA CA2650904A patent/CA2650904C/en active Active
- 2007-05-02 US US11/797,341 patent/US8562949B2/en active Active
-
2008
- 2008-11-02 IL IL195044A patent/IL195044A/en active IP Right Grant
- 2008-12-01 NO NO20085004A patent/NO341065B1/no unknown
- 2008-12-01 ZA ZA2008/10200A patent/ZA200810200B/en unknown
Also Published As
Publication number | Publication date |
---|---|
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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