JP4937144B2 - 診断用イメージングのための脂肪酸アナログの立体異性体 - Google Patents
診断用イメージングのための脂肪酸アナログの立体異性体 Download PDFInfo
- Publication number
- JP4937144B2 JP4937144B2 JP2008006447A JP2008006447A JP4937144B2 JP 4937144 B2 JP4937144 B2 JP 4937144B2 JP 2008006447 A JP2008006447 A JP 2008006447A JP 2008006447 A JP2008006447 A JP 2008006447A JP 4937144 B2 JP4937144 B2 JP 4937144B2
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- Prior art keywords
- group
- fatty acid
- imaging
- stereoisomer
- hydrogen
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- Expired - Fee Related
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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
- A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
-
- 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
-
- 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
- A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2123/00—Preparations for testing in vivo
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Optics & Photonics (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physics & Mathematics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Fats And Perfumes (AREA)
- Nuclear Medicine (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Description
臨床におけるイメージング技術は、障害及び疾患の進行を診断する際に重要な役割を果たしている。動物の身体のいかなる部分も現在では、さまざまなイメージング技術を用いて診断目的で視覚的に検査することができる。x線写真は、外部より発生したx線が透過する身体の部分を画像化するために長い間用いられてきた。コンピュータ処理される軸方向の断層撮影法(CAT)は、身体の平面の断面x線画像を提供する。特定の組織や器官は、ポジトロン放出断層撮影法(PET)、一光子放出コンピュータ処理断層撮影法(SPECT)、及びシンチグラム造影法で標的とすることができる。PET、SPECT、及びシンチグラム造影法では、標的となる組織または器官においてある程度になるまでとどめておく能力のある放射性医薬品を患者に体内投与し、留まった放射性医薬品から生じる放射活性の放出線を検出することによって画像を形成する。放射性医薬品には、例えば201Tl、99mTc、133Xeなどのような核種、核種のキレート、例えば11C−デオキシ−D−グルコース、18F−2−フルオロデオキシ−D−グルコース、[1−11C]−及び[123I]−β−メチル脂肪酸アナログ、13N−アンモニアなどのような核種で標識した代謝性薬剤、例えば99mTc−テトラサイクリン、99mTc−ピロリン酸塩、203Hg−水銀製剤、67Ga−クエン酸塩などのような梗塞親和性薬剤、それに核種で標識したモノクローナル抗体が含まれる。赤血球や白血球のような完全細胞もまた、放射性核種で標識することができ、放射性医薬品として機能する。
本発明は、障害及び疾患の状態について診断用イメージングを行うための改良された新規な放射性医薬品(試薬)を提供する。本発明のイメージング試薬は放射性核種含有の脂肪酸のアナログであり、特に心臓血管及び脳をイメージングするのに適当である。本発明のイメージング試薬は実質的に、脂肪酸アナログの純粋な立体異性体である。
本明細書で言及する特許及び科学文献によって、当業者は利用可能な知識を確立する。本明細書に引用した発行された米国特許及び認められた出願は、参考文献として本明細書に組み入れられる。
R=H、ハロゲン、アルキル、アリール、アシル、アルコキシ、
アリル、ハロアリル
*Tc=99mTc
他のN2S2脂肪酸の配置には、例えば次の式のものがありうる。
Claims (2)
- 次の化学式を持つ脂肪酸アナログの立体異性体に空間的に近接する放射性核種を含み、該放射性核種が、123I、99mTc、18F、68Ga、62Cu、及び111Inからなる群より選択される、イメージング試薬:
該立体異性体がR−立体異性体またはS−立体異性体である、イメージング試薬。 - 請求項1記載のイメージング試薬と薬学的に許容される担体とを含むキット。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US786395P | 1995-12-01 | 1995-12-01 | |
US60/007,863 | 1995-12-01 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52066997A Division JP4272259B2 (ja) | 1995-12-01 | 1996-11-25 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2011232673A Division JP2012036215A (ja) | 1995-12-01 | 2011-10-24 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2008201774A JP2008201774A (ja) | 2008-09-04 |
JP2008201774A5 JP2008201774A5 (ja) | 2009-04-09 |
JP4937144B2 true JP4937144B2 (ja) | 2012-05-23 |
Family
ID=21728502
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52066997A Expired - Fee Related JP4272259B2 (ja) | 1995-12-01 | 1996-11-25 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
JP2008006447A Expired - Fee Related JP4937144B2 (ja) | 1995-12-01 | 2008-01-16 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
JP2011232673A Withdrawn JP2012036215A (ja) | 1995-12-01 | 2011-10-24 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP52066997A Expired - Fee Related JP4272259B2 (ja) | 1995-12-01 | 1996-11-25 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2011232673A Withdrawn JP2012036215A (ja) | 1995-12-01 | 2011-10-24 | 診断用イメージングのための脂肪酸アナログの立体異性体 |
Country Status (9)
Country | Link |
---|---|
US (4) | US7005119B2 (ja) |
EP (2) | EP0869821B1 (ja) |
JP (3) | JP4272259B2 (ja) |
AT (2) | ATE526995T1 (ja) |
CA (1) | CA2238860C (ja) |
DE (1) | DE69636881T2 (ja) |
ES (2) | ES2281906T3 (ja) |
HK (2) | HK1016494A1 (ja) |
WO (1) | WO1997019705A1 (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997019705A1 (en) * | 1995-12-01 | 1997-06-05 | Elmaleh David R | Stereoisomers of fatty acid analogs for diagnostic imaging |
US20090117032A1 (en) * | 1998-09-08 | 2009-05-07 | The General Hospital Corporation | Imaging Agents for Early Detection and Monitoring of Cardiovascular Plaque |
EP0992245A1 (en) * | 1998-09-16 | 2000-04-12 | Goldham Bioglan Pharma GmbH | Radio-contrast agents |
EP1040825A1 (en) * | 1999-03-11 | 2000-10-04 | K.U. Leuven Research & Development | Means for diagnosing bladder carcinoma |
CA2366789C (en) | 1999-04-14 | 2010-09-28 | Biostream, Inc. | Fatty acid analogs for diagnosis of coronary artery disease |
WO2003084575A1 (en) * | 2002-04-01 | 2003-10-16 | Biostream, Inc. | Pendant fatty acid imaging agents |
US7494642B2 (en) | 2003-04-17 | 2009-02-24 | The General Hospital Corporation | Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid |
JP2012526129A (ja) * | 2009-05-04 | 2012-10-25 | ワシントン・ユニバーシティ | 脂肪酸代謝および貯蔵を画像化するためのpet放射性追跡子 |
DE102010010666A1 (de) * | 2010-03-01 | 2011-09-01 | Sven Reske | Diagnose und Therapie von Krebserkrankungen mittels Fettsäuren |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NL6802651A (ja) * | 1968-02-23 | 1969-08-26 | ||
DE2828623C2 (de) * | 1978-06-29 | 1983-11-17 | Kernforschungsanlage Jülich GmbH, 5170 Jülich | Mit radioaktivem Flour markierte C↓1↓↓6↓-bis C↓1↓↓8↓- Fettsäuren, ein Verfahren zu ihrer Herstellung sowie deren Verwendung |
DE2947500C2 (de) * | 1979-11-24 | 1984-05-10 | Dutschka, Klaus, 4300 Essen | Radiojodierte ω -Phenylfettsäuren, ihre Herstellung und deren Verwendung zur szintigraphischen Untersuchung des Herzmuskels und der Leber |
FR2508902B1 (fr) * | 1981-07-02 | 1985-09-06 | Commissariat Energie Atomique | Procede de preparation extemporanee d'un acide gras injectable, marque a l'iode radioactif et preparation de derives iodes utilisables pour la mise en oeuvre de ce procede |
US4524059A (en) * | 1983-01-28 | 1985-06-18 | The General Hospital Corporation | Fatty acid analogs |
US4942231A (en) * | 1984-05-24 | 1990-07-17 | Mallinckrodt, Inc. | Method of preparing a chlorinated, brominated, radio-brominated, iodinated and/or radioiodinated aromatic or heteroaromatic compound |
CA1243329A (en) * | 1985-03-11 | 1988-10-18 | Amersham Int Plc | TECHNETIUM COMPLEXES WITH PROPYLENE-AMINE-OXIMES |
US4746505A (en) * | 1985-04-26 | 1988-05-24 | President And Fellows Of Harvard College | Technetium radiodiagnostic fatty acids derived from bisamide bisthiol ligands |
US4764358A (en) * | 1985-04-30 | 1988-08-16 | The United States Of America As Represented By The United States Department Of Energy | Radiolabeled dimethyl branched long chain fatty acid for heart imaging |
US4877599A (en) * | 1986-11-10 | 1989-10-31 | New England Deaconess Hospital Corporation | Detection of vascular disease with labelled antibodies |
EP0317873B1 (en) * | 1987-11-19 | 1993-05-12 | The Vanderbilt University | Radioiodinated benzamides and method of their use as radioimaging agents |
US5242681A (en) * | 1990-03-12 | 1993-09-07 | Research Corporation Technologies, Inc. | Lipophilic contrast agents for diagnostic image analysis |
US7238340B1 (en) * | 1991-11-27 | 2007-07-03 | Cis Bio International | Monoamine, diamide, thiol-containing metal chelating agents |
WO1997019705A1 (en) * | 1995-12-01 | 1997-06-05 | Elmaleh David R | Stereoisomers of fatty acid analogs for diagnostic imaging |
EP1011738A1 (en) * | 1997-09-08 | 2000-06-28 | The General Hospital Corporation | Imaging agents for early detection of cardiovascular plaque |
US7060251B1 (en) * | 1997-09-08 | 2006-06-13 | The General Hospital Corporation | Imaging agents for early detection and monitoring of cardiovascular plaque |
CA2366789C (en) * | 1999-04-14 | 2010-09-28 | Biostream, Inc. | Fatty acid analogs for diagnosis of coronary artery disease |
IL151250A0 (en) * | 2000-03-21 | 2003-04-10 | Procter & Gamble | Difluorobutyric acid metalloprotease inhibitors |
US7494642B2 (en) * | 2003-04-17 | 2009-02-24 | The General Hospital Corporation | Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid |
-
1996
- 1996-11-25 WO PCT/US1996/019024 patent/WO1997019705A1/en active IP Right Grant
- 1996-11-25 DE DE69636881T patent/DE69636881T2/de not_active Expired - Lifetime
- 1996-11-25 ES ES96941503T patent/ES2281906T3/es not_active Expired - Lifetime
- 1996-11-25 JP JP52066997A patent/JP4272259B2/ja not_active Expired - Fee Related
- 1996-11-25 AT AT06025944T patent/ATE526995T1/de not_active IP Right Cessation
- 1996-11-25 EP EP96941503A patent/EP0869821B1/en not_active Expired - Lifetime
- 1996-11-25 CA CA002238860A patent/CA2238860C/en not_active Expired - Fee Related
- 1996-11-25 EP EP06025944A patent/EP1767224B1/en not_active Expired - Lifetime
- 1996-11-25 ES ES06025944T patent/ES2374743T3/es not_active Expired - Lifetime
- 1996-11-25 AT AT96941503T patent/ATE353019T1/de not_active IP Right Cessation
-
1999
- 1999-04-14 HK HK99101613A patent/HK1016494A1/xx not_active IP Right Cessation
-
2003
- 2003-05-05 US US10/429,416 patent/US7005119B2/en not_active Expired - Fee Related
-
2005
- 2005-11-16 US US11/274,505 patent/US7314609B2/en not_active Expired - Fee Related
-
2007
- 2007-01-09 US US11/621,241 patent/US20070128110A1/en not_active Abandoned
- 2007-09-21 HK HK07110322.1A patent/HK1102262A1/xx not_active IP Right Cessation
-
2008
- 2008-01-16 JP JP2008006447A patent/JP4937144B2/ja not_active Expired - Fee Related
- 2008-04-02 US US12/061,528 patent/US20080247948A1/en not_active Abandoned
-
2011
- 2011-10-24 JP JP2011232673A patent/JP2012036215A/ja not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
ATE353019T1 (de) | 2007-02-15 |
WO1997019705A1 (en) | 1997-06-05 |
JP4272259B2 (ja) | 2009-06-03 |
HK1102262A1 (en) | 2007-11-09 |
JP2008201774A (ja) | 2008-09-04 |
US7314609B2 (en) | 2008-01-01 |
US20030215386A1 (en) | 2003-11-20 |
US7005119B2 (en) | 2006-02-28 |
EP1767224A3 (en) | 2007-11-28 |
EP0869821A1 (en) | 1998-10-14 |
DE69636881D1 (de) | 2007-03-22 |
ATE526995T1 (de) | 2011-10-15 |
CA2238860C (en) | 2009-01-13 |
CA2238860A1 (en) | 1997-06-05 |
ES2374743T3 (es) | 2012-02-21 |
EP0869821A4 (en) | 2002-08-28 |
HK1016494A1 (en) | 1999-11-05 |
DE69636881T2 (de) | 2007-09-20 |
US20060078495A1 (en) | 2006-04-13 |
US20080247948A1 (en) | 2008-10-09 |
ES2281906T3 (es) | 2007-10-01 |
EP1767224B1 (en) | 2011-10-05 |
US20070128110A1 (en) | 2007-06-07 |
EP0869821B1 (en) | 2007-01-31 |
EP1767224A2 (en) | 2007-03-28 |
JP2012036215A (ja) | 2012-02-23 |
JP2000502059A (ja) | 2000-02-22 |
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CHAPTER | THE SOCIETY OF NUCLEAR MEDICINE 29thAnnualMeeting |
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