AR036182A1 - Conjugados de biomoleculas y 1,4,7,10-tetraazaciclododecanos, un procedimiento para su preparacion, su uso para la preparacion de medios de diagnostico por resonancia magnetica nuclear o radiodiagnostico o para la radioterapia, los agentes farmaceuticos que los contienen, y los conjuntos o kits para - Google Patents
Conjugados de biomoleculas y 1,4,7,10-tetraazaciclododecanos, un procedimiento para su preparacion, su uso para la preparacion de medios de diagnostico por resonancia magnetica nuclear o radiodiagnostico o para la radioterapia, los agentes farmaceuticos que los contienen, y los conjuntos o kits paraInfo
- Publication number
- AR036182A1 AR036182A1 ARP020102718A ARP020102718A AR036182A1 AR 036182 A1 AR036182 A1 AR 036182A1 AR P020102718 A ARP020102718 A AR P020102718A AR P020102718 A ARP020102718 A AR P020102718A AR 036182 A1 AR036182 A1 AR 036182A1
- Authority
- AR
- Argentina
- Prior art keywords
- conjugates
- preparation
- hydrogen atom
- atoms
- chain
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 238000001959 radiotherapy Methods 0.000 title abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 238000005481 NMR spectroscopy Methods 0.000 abstract 2
- 229910018828 PO3H2 Inorganic materials 0.000 abstract 2
- 229910006069 SO3H Inorganic materials 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- QBPPRVHXOZRESW-UHFFFAOYSA-N 1,4,7,10-tetraazacyclododecane Chemical class C1CNCCNCCNCCN1 QBPPRVHXOZRESW-UHFFFAOYSA-N 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 239000002872 contrast media Substances 0.000 abstract 1
- 229940039231 contrast media Drugs 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 150000002678 macrocyclic compounds Chemical class 0.000 abstract 1
- 229910021645 metal ion Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008177 pharmaceutical agent Substances 0.000 abstract 1
- 239000012217 radiopharmaceutical Substances 0.000 abstract 1
- 229940121896 radiopharmaceutical Drugs 0.000 abstract 1
- 230000002799 radiopharmaceutical effect Effects 0.000 abstract 1
- 230000003439 radiotherapeutic effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
-
- 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
- A61K49/14—Peptides, e.g. proteins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/0002—General or multifunctional contrast agents, e.g. chelated agents
-
- 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
- A61K49/085—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
-
- 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
- A61K49/14—Peptides, e.g. proteins
- A61K49/143—Peptides, e.g. proteins the protein being an albumin, e.g. HSA, BSA, ovalbumin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Radiology & Medical Imaging (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
Abstract
Conjugados de biomoléculas y 1,4,7,10-tetraazaciclododecanos, de fórmula (1), donde Z representa un átomo de hidrógeno o al menos dos Z representan un equivalente de un ión metálico; B representa un átomo de hidrógeno o un radical alquilo C1-4; R representa un átomo de hidrógeno o un radical alquilo C1-10 lineal , o arilo ramificado o cíclico, saturado o insaturado, que está sustituido opcionalmente por un grupo carboxilo, -SO3H ó -PO3H2, y donde la cadena de alquilo del radical alquilo C1-10 contiene opcionalmente un grupo arilo y/o 1-2 átomos de oxígeno, con la condición de que los radicales B y R no representen al mismo tiempo átomos de oxígeno; A representa una cadena de hidrocarburos C1-30 lineal o ramificada, saturada o insaturada, que contiene opcionalmente 1-5 átomos de oxígeno, 1-5 átomos de nitrógeno y/o 1-5 radicales -NR', donde R' está definido como R, pero que puede seleccionarse de modo independiente, que está opcionalmente sustituido con 1-3 grupos carboxilo, 1-3 -SO3H, 1-3 -PO3H2 y/o 1-3 átomos de halógeno, donde están presentes opcionalmente 1-3 átomos de carbono como grupos carbonilo, donde la cadena o una parte de la cadena puede estar dispuesta en forma de anillo, y que está conformada de modo tal que X' está enlazado al menos a través de 3 átomos con el átomo de nitrógeno al que está unido A; X' representa el radical de un grupo X que reaccionó con una biomolécula, y Bio representa el radical de una biomolécula, sus sales, con la condición de que, cuando B es un átomo de hidrógeno y R es un radical alquilo C1-4, A no es el radical -CHR3-C(O)-NH-(CH2)1-6-NH-D- donde R3 es un átomo de hidrógeno o un radical alquilo C1-4; D es un grupo alquileno C1-4, de cadena lineal o ramificada, saturado o insaturado, que opcionalmente puede estar interrumpido o sustituido por un grupo carbonilo y D está unido a X. Estos conjugados son aptos como medios de contraste en el diagnóstico por RMN y radiodiagnóstico y como sustancia radioterapéutica. Con los ligandos especiales de los macrociclos se logra una elevada relajación y se posibilita un ajuste fino de la relajación. Un procedimiento para la preparación de los conjugados de fórmula (1), uso de estos últimos para la preparación de medios de diagnóstico por resonancia magnética nuclear o radiodiagnóstico o para la radioterapia, los agentes farmacéuticos que los contienen, y los conjuntos o kits para preparar radiofármacos que comprenden dichos conjugados.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10135355A DE10135355C1 (de) | 2001-07-20 | 2001-07-20 | Konjugate makrocyclischer Metallkomplexe mit Biomolekülen und deren Verwendung zur Herstellung von Mitteln für die NMR- und Radiodiagnostik sowie die Radiotherapie |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036182A1 true AR036182A1 (es) | 2004-08-18 |
Family
ID=7692470
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020102718A AR036182A1 (es) | 2001-07-20 | 2002-07-19 | Conjugados de biomoleculas y 1,4,7,10-tetraazaciclododecanos, un procedimiento para su preparacion, su uso para la preparacion de medios de diagnostico por resonancia magnetica nuclear o radiodiagnostico o para la radioterapia, los agentes farmaceuticos que los contienen, y los conjuntos o kits para |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20030206865A1 (es) |
| EP (1) | EP1450864A2 (es) |
| JP (1) | JP2004536889A (es) |
| KR (1) | KR20040030825A (es) |
| CN (1) | CN1301750C (es) |
| AR (1) | AR036182A1 (es) |
| AU (1) | AU2002355333B2 (es) |
| BR (1) | BR0211150A (es) |
| CA (1) | CA2453214A1 (es) |
| DE (1) | DE10135355C1 (es) |
| IL (1) | IL159291A0 (es) |
| MX (1) | MXPA04000400A (es) |
| NO (1) | NO20040239L (es) |
| PE (1) | PE20030190A1 (es) |
| PL (1) | PL366421A1 (es) |
| RU (1) | RU2004105262A (es) |
| TW (1) | TWI238722B (es) |
| UY (1) | UY27389A1 (es) |
| WO (1) | WO2003013617A2 (es) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7632651B2 (en) | 1997-09-15 | 2009-12-15 | Mds Analytical Technologies (Us) Inc. | Molecular modification assays |
| US7067111B1 (en) | 1999-10-25 | 2006-06-27 | Board Of Regents, University Of Texas System | Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging |
| KR100784120B1 (ko) * | 2000-06-02 | 2007-12-12 | 보드 오브 리전츠, 더 유니버시티 오브 텍사스 시스템 | 에틸렌디시스테인(ｅｃ)-약물 접합체 |
| DE10135356C1 (de) * | 2001-07-20 | 2003-04-17 | Schering Ag | Makrocyclische Metallkomplexe und deren Verwendung zur Herstellung von Konjugaten mit Biomolekülen |
| EP1466629A1 (en) * | 2003-04-11 | 2004-10-13 | BRACCO IMAGING S.p.A. | Adducts between magnetic resonance shift reagents and substrates containing exchangeable protons for "CEST" applications |
| DE10325752A1 (de) * | 2003-06-06 | 2004-12-30 | Faustus Forschungs Cie. Translational Cancer Research Gmbh | Lektin-Konjugate |
| FR2856689A1 (fr) * | 2003-06-25 | 2004-12-31 | Guerbet Sa | Composes specifiques a forte relaxivite |
| JP2007521254A (ja) * | 2003-06-25 | 2007-08-02 | ゲルベ | 診断画像用化合物 |
| EP1687034A1 (en) * | 2003-11-17 | 2006-08-09 | Philips Intellectual Property & Standards GmbH | Contrast agent for medical imaging techniques and usage thereof |
| US9050378B2 (en) * | 2003-12-10 | 2015-06-09 | Board Of Regents, The University Of Texas System | N2S2 chelate-targeting ligand conjugates |
| FR2868320B1 (fr) * | 2004-03-31 | 2007-11-02 | Centre Nat Rech Scient Cnrse | Agent de contraste pour l'imagerie par resonance magnetique |
| WO2006039505A2 (en) | 2004-09-30 | 2006-04-13 | Molecular Devices Corporation | Luminescent lanthanide complexes |
| CN101166547B (zh) * | 2005-04-26 | 2013-02-06 | 皇家飞利浦电子股份有限公司 | 包含cest活性的顺磁性配合物的mri造影剂 |
| FI20055712A0 (fi) * | 2005-12-29 | 2005-12-29 | Wallac Oy | Makrosykliset oligonukleotiidien leimausreagenssit ja niistä johdetut konjugaatit |
| US8758723B2 (en) * | 2006-04-19 | 2014-06-24 | The Board Of Regents Of The University Of Texas System | Compositions and methods for cellular imaging and therapy |
| US10925977B2 (en) | 2006-10-05 | 2021-02-23 | Ceil>Point, LLC | Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications |
| US8562945B2 (en) | 2008-01-09 | 2013-10-22 | Molecular Insight Pharmaceuticals, Inc. | Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof |
| 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 |
| AU2009322171A1 (en) | 2008-12-05 | 2011-06-30 | Molecular Insight Pharmaceuticals, Inc. | CA-IX specific radiopharmaceuticals for the treatment and imaging of cancer |
| US8211402B2 (en) | 2008-12-05 | 2012-07-03 | Molecular Insight Pharmaceuticals, Inc. | CA-IX specific radiopharmaceuticals for the treatment and imaging of cancer |
| US8465725B2 (en) | 2009-06-15 | 2013-06-18 | Molecular Insight Pharmaceuticlas, Inc. | Process for production of heterodimers of glutamic acid |
| CN101912623B (zh) * | 2010-08-24 | 2012-06-06 | 上海师范大学 | 具有靶向功能铁-钆双模式磁共振造影剂的制备及应用 |
| CN102136339B (zh) * | 2011-01-24 | 2012-05-23 | 南开大学 | 一种具有铁磁、铁电双功能的镝单分子磁体及其制备方法 |
| CA2860504A1 (en) | 2012-01-06 | 2013-07-11 | Molecular Insight Pharmaceuticals | Metal complexes of poly(carboxyl)amine-containing ligands having an affinity for carbonic anhydrase ix |
| ES2738474T3 (es) | 2013-01-14 | 2020-01-23 | Molecular Insight Pharm Inc | Radiofármacos a base de triazina y agentes radioimagenológicos |
| EP3074388A1 (en) * | 2013-11-25 | 2016-10-05 | Sanofi | Dotam derivatives for therapeutic use |
| EP3101012A1 (en) | 2015-06-04 | 2016-12-07 | Bayer Pharma Aktiengesellschaft | New gadolinium chelate compounds for use in magnetic resonance imaging |
| WO2018096082A1 (en) | 2016-11-28 | 2018-05-31 | Bayer Pharma Aktiengesellschaft | High relaxivity gadolinium chelate compounds for use in magnetic resonance imaging |
| US11191854B2 (en) | 2017-05-05 | 2021-12-07 | Centre For Probe Development And Commercialization | Pharmacokinetic enhancements of bifunctional chelates and uses thereof |
| IL313115A (en) | 2017-05-05 | 2024-07-01 | Centre For Probe Dev And Commercialization | R1–IGF monoclonal antibodies and their use |
| US10093741B1 (en) | 2017-05-05 | 2018-10-09 | Fusion Pharmaceuticals Inc. | IGF-1R monoclonal antibodies and uses thereof |
| AU2019382881B2 (en) | 2018-11-23 | 2025-06-12 | Bayer Aktiengesellschaft | Formulation of contrast media and process of preparation thereof |
| FR3092580B1 (fr) * | 2019-02-08 | 2021-03-19 | Centre Nat Rech Scient | Nouveaux dérivés azobenzènes, leur procédé de préparation et leur utilisation pour le traitement thérapeutique associé à des radiations ionisantes |
| EP3757098A1 (en) * | 2019-06-25 | 2020-12-30 | Ustav Organicke Chemie a Biochemie AV CR, v.v.i. | Cyclen based compounds, coordination compounds, peptides, pharmaceutical preparation, and use thereof |
| KR102203368B1 (ko) * | 2020-10-30 | 2021-01-14 | 경북대학교 산학협력단 | 신규한 화합물 및 이를 함유하는 mri 조영제 |
| US20250154159A1 (en) * | 2022-03-16 | 2025-05-15 | Wenzhou Institute University of Chinese Academy of Sciences | CYCLIC Gd (III) COMPLEX AND PREPARATION METHOD AND USE THEREOF |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5049667A (en) * | 1987-04-14 | 1991-09-17 | Guerbet S.A. | Nitrogen-containing cyclic ligands |
| JPH04154729A (ja) * | 1990-10-16 | 1992-05-27 | Nippon Mejifuijitsukusu Kk | 磁気共鳴造影剤 |
| DE4115789A1 (de) * | 1991-05-10 | 1992-11-12 | Schering Ag | Makrocyclische polymer-komplexbildner, deren komplexe, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische mittel |
| CA2092596A1 (en) * | 1992-03-27 | 1993-09-28 | Kan Kubomura | Tetraazacyclododecane derivative and its use |
| DE69324161T2 (de) * | 1992-12-09 | 1999-10-28 | Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield | Stabilisierte medizinische aerosollösungen |
| US6693190B1 (en) * | 1994-05-11 | 2004-02-17 | Bracco International B.V. | Enhanced relaxivity monomeric and multimeric compounds |
| US6045776A (en) * | 1996-12-04 | 2000-04-04 | Schering Aktiengesellschaft | Process for the production of metal-complex carboxylic acid amides |
| US6113880A (en) * | 1997-12-17 | 2000-09-05 | Schering Aktiengesellschaft | Polyrotaxane derivatives for x-ray and nuclear magnetic resonance imaging |
| DE19905094C1 (de) * | 1999-02-01 | 2000-10-12 | Schering Ag | Gadolinium (III)-Komplexe sowie ihre Verwendung für Zweischritt Strahlentherapieformen und diese enthaltende pharmazeutische Mittel |
-
2001
- 2001-07-20 DE DE10135355A patent/DE10135355C1/de not_active Expired - Fee Related
-
2002
- 2002-07-17 UY UY27389A patent/UY27389A1/es not_active Application Discontinuation
- 2002-07-18 JP JP2003518619A patent/JP2004536889A/ja active Pending
- 2002-07-18 EP EP02794507A patent/EP1450864A2/de not_active Withdrawn
- 2002-07-18 WO PCT/EP2002/008000 patent/WO2003013617A2/de not_active Ceased
- 2002-07-18 RU RU2004105262/04A patent/RU2004105262A/ru not_active Application Discontinuation
- 2002-07-18 IL IL15929102A patent/IL159291A0/xx unknown
- 2002-07-18 AU AU2002355333A patent/AU2002355333B2/en not_active Ceased
- 2002-07-18 PL PL02366421A patent/PL366421A1/xx not_active Application Discontinuation
- 2002-07-18 MX MXPA04000400A patent/MXPA04000400A/es not_active Application Discontinuation
- 2002-07-18 BR BR0211150-0A patent/BR0211150A/pt not_active IP Right Cessation
- 2002-07-18 KR KR10-2004-7000905A patent/KR20040030825A/ko not_active Ceased
- 2002-07-18 CN CNB028145690A patent/CN1301750C/zh not_active Expired - Fee Related
- 2002-07-18 CA CA002453214A patent/CA2453214A1/en not_active Abandoned
- 2002-07-19 PE PE2002000641A patent/PE20030190A1/es not_active Application Discontinuation
- 2002-07-19 TW TW091116146A patent/TWI238722B/zh not_active IP Right Cessation
- 2002-07-19 AR ARP020102718A patent/AR036182A1/es unknown
- 2002-07-19 US US10/198,048 patent/US20030206865A1/en not_active Abandoned
-
2004
- 2004-01-19 NO NO20040239A patent/NO20040239L/no not_active Application Discontinuation
-
2006
- 2006-03-28 US US11/390,414 patent/US20070014725A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2002355333B2 (en) | 2007-01-04 |
| UY27389A1 (es) | 2003-02-28 |
| WO2003013617A3 (de) | 2004-06-10 |
| PL366421A1 (en) | 2005-01-24 |
| NO20040239L (no) | 2004-01-19 |
| MXPA04000400A (es) | 2004-03-18 |
| US20030206865A1 (en) | 2003-11-06 |
| RU2004105262A (ru) | 2005-07-10 |
| US20070014725A1 (en) | 2007-01-18 |
| DE10135355C1 (de) | 2003-04-17 |
| WO2003013617A2 (de) | 2003-02-20 |
| EP1450864A2 (de) | 2004-09-01 |
| CA2453214A1 (en) | 2003-02-20 |
| IL159291A0 (en) | 2004-06-01 |
| PE20030190A1 (es) | 2003-03-22 |
| CN1541114A (zh) | 2004-10-27 |
| KR20040030825A (ko) | 2004-04-09 |
| JP2004536889A (ja) | 2004-12-09 |
| BR0211150A (pt) | 2004-06-29 |
| TWI238722B (en) | 2005-09-01 |
| CN1301750C (zh) | 2007-02-28 |
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