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PE20030322A1 - Complejos metalicos y macrociclicos - Google Patents

Complejos metalicos y macrociclicos

Info

Publication number
PE20030322A1
PE20030322A1 PE2002000642A PE2002000642A PE20030322A1 PE 20030322 A1 PE20030322 A1 PE 20030322A1 PE 2002000642 A PE2002000642 A PE 2002000642A PE 2002000642 A PE2002000642 A PE 2002000642A PE 20030322 A1 PE20030322 A1 PE 20030322A1
Authority
PE
Peru
Prior art keywords
alkyl
atoms
carboxyl
oxygen
oxygen atoms
Prior art date
Application number
PE2002000642A
Other languages
English (en)
Inventor
Johannes Platzek
Heribert Schmitt-Willich
Detlev Sulzle
Heiko Schirmer
Gunther Michl
Thomas Frenzel
Hans Bauer
Bernd Raduchel
Original Assignee
Schering Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20030322A1 publication Critical patent/PE20030322A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/547—Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Radiology & Medical Imaging (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

DE FORMULA (I), DONDE Z ES H O AL MENOS DOS Z SON UN EQUIVALENTE DE UN ION METALICO; B ES H O ALQUILO C1-4; R ES H O ALQUILO C1-10 QUE CONTIENE ARILO Y/O 1 A 2 ATOMOS DE OXIGENO, o ARILO SUSTITUIDO POR CARBOXILO, -S03H o -PO3H2, CON LA CONDICION DE QUE B Y R NO SEAN AL MISMO TIEMPO ATOMOS DE OXIGENO; A ES HIDROCARBURO C1-30 QUE CONTIENE OPCIONALMENTE 1 A 5 ATOMOS DE OXIGENO, NITROGENO Y/O RADICALES -NR', DONDE R' ES R, PERO PUEDE SELECCIONARSE INDEPENDIENTEMENTE Y ESTA OPCIONALMENTE SUSTITUIDO CON 1 A 3 GRUPOS CARBOXILO, 1 A 3 -SO3H, 1 A 3 -PO3H2 Y 1 A 3 ATOMOS DE HALOGENO, DONDE LA CADENA O UNA PARTE DE ELLA PUEDE ESTAR DISPUESTA EN FORMA DE ANILLO Y ESTA CONFORMADA DE MODO TAL QUE X ESTA ENLAZADO AL MENOS A TRAVES DE 3 ATOMOS CON EL ATOMO DE NITROGENO AL QUE ESTA UNIDO A; X ES UN GRUPO QUE PUEDE REACCIONAR CON UNA BIOMOLECULA Y SUS SALES, CON LA CONDICION DE QUE: a)CUANDO B ES UN ATOMO DE H Y R ES -CH2CH2CO2H, A-X JUNTOS NO SON -CH(CO2H)CH2CH2CO2H; b)CUANDO B ES H Y R ES METILO O ETILO SUSTITUIDO POR CARBOXILO, A NO ES -CH(R4)-CO-NR2-U6, DONDE R2 ES H, METILO O ETILO SUSTITUIDO POR CARBOXILO, R4 ES ALQUILO C1-30 Y QUE PUEDE ESTAR INTERRUMPIDAPOR 1 A 10 ATOMOS DE OXIGENO, FENILENO, ENTRE OTROS Y U6 ES ALQUILENO C1-20; c)SI B ES H Y R ES ALQUILO C1-4, A NO ES EL RADICAL (II), DONDE R3 ES H O ALQUILO C1-4, D ES UN GRUPO ALQUILENO C1-4 OPCIONALMENTE SUSTITUIDO POR CARBONILO Y D ESTA UNIDO A X. DICHOS CONJUGADOS SON APROPIADOS PARA OBTENER MEDIOS DE CONTRASTE PARA DIAGNOSTICO
PE2002000642A 2001-07-20 2002-07-19 Complejos metalicos y macrociclicos PE20030322A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10135356A DE10135356C1 (de) 2001-07-20 2001-07-20 Makrocyclische Metallkomplexe und deren Verwendung zur Herstellung von Konjugaten mit Biomolekülen

Publications (1)

Publication Number Publication Date
PE20030322A1 true PE20030322A1 (es) 2003-04-13

Family

ID=7692471

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000642A PE20030322A1 (es) 2001-07-20 2002-07-19 Complejos metalicos y macrociclicos

Country Status (19)

Country Link
US (2) US7164016B2 (es)
EP (1) EP1409024B1 (es)
JP (1) JP2005504745A (es)
KR (1) KR20040030826A (es)
CN (1) CN1533286A (es)
AR (1) AR036183A1 (es)
AT (1) ATE403442T1 (es)
AU (1) AU2002321236B2 (es)
BR (1) BR0211273A (es)
CA (1) CA2453106A1 (es)
DE (2) DE10135356C1 (es)
IL (1) IL159290A0 (es)
MX (1) MXPA04000401A (es)
NO (1) NO20040238L (es)
PE (1) PE20030322A1 (es)
PL (1) PL366426A1 (es)
RU (1) RU2305096C2 (es)
UY (1) UY27390A1 (es)
WO (1) WO2003009874A1 (es)

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KR100784120B1 (ko) 2000-06-02 2007-12-12 보드 오브 리전츠, 더 유니버시티 오브 텍사스 시스템 에틸렌디시스테인(ｅｃ)-약물 접합체
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DE10325752A1 (de) * 2003-06-06 2004-12-30 Faustus Forschungs Cie. Translational Cancer Research Gmbh Lektin-Konjugate
US9050378B2 (en) 2003-12-10 2015-06-09 Board Of Regents, The University Of Texas System N2S2 chelate-targeting ligand conjugates
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
CN101516899B (zh) * 2006-04-19 2016-07-06 得克萨斯大学体系董事会 细胞成像和治疗的组合物和方法
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US10189803B2 (en) 2008-02-22 2019-01-29 Illinois Institute Of Technology Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
US10556873B2 (en) 2008-02-22 2020-02-11 Illinois Institute Of Technology Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
US9446995B2 (en) 2012-05-21 2016-09-20 Illinois Institute Of Technology Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
WO2010011367A2 (en) * 2008-02-22 2010-01-28 Illinois Institute Of Technology Bimodal ligands with macrocyclic and acyclic binding moieties, complexes and compositions thereof, and methods of using
KR101253100B1 (ko) * 2010-02-16 2013-04-10 경북대학교 산학협력단 폴리아자마크로사이클릭 화합물, 그 제조 방법 및 생의학적 적용
KR101236142B1 (ko) * 2010-09-30 2013-02-21 경북대학교 산학협력단 가돌리늄 착물을 함유하는 ｍｒｉ조영제
US10441669B2 (en) 2013-10-04 2019-10-15 Illinois Institute Of Technology Multifunctional chelators, complexes, and compositions thereof, and methods of using same
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
US10093741B1 (en) 2017-05-05 2018-10-09 Fusion Pharmaceuticals Inc. IGF-1R monoclonal antibodies and uses thereof
IL313115A (en) 2017-05-05 2024-07-01 Centre For Probe Dev And Commercialization R1–IGF monoclonal antibodies and their use
US11191854B2 (en) 2017-05-05 2021-12-07 Centre For Probe Development And Commercialization Pharmacokinetic enhancements of bifunctional chelates and uses thereof
FR3069245B1 (fr) * 2017-07-21 2019-07-26 Guerbet Ligands macrocycliques lipophiles, leurs complexes ainsi que leurs utilisations medicales
CN109810140B (zh) * 2017-11-22 2021-06-29 湖南科技大学 一种血红素配体模拟物及其合成方法
AU2019382881B2 (en) 2018-11-23 2025-06-12 Bayer Aktiengesellschaft Formulation of contrast media and process of preparation thereof
CN110396122B (zh) * 2019-08-13 2020-10-27 牡丹江医学院 一种核磁共振造影剂、制备方法及其用于肿瘤诊断中的用途
KR102203368B1 (ko) * 2020-10-30 2021-01-14 경북대학교 산학협력단 신규한 화합물 및 이를 함유하는 mri 조영제
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Also Published As

Publication number Publication date
NO20040238L (no) 2004-01-19
IL159290A0 (en) 2004-06-01
WO2003009874A1 (de) 2003-02-06
BR0211273A (pt) 2004-08-03
US7164016B2 (en) 2007-01-16
US20070009442A1 (en) 2007-01-11
DE10135356C1 (de) 2003-04-17
CN1533286A (zh) 2004-09-29
EP1409024A1 (de) 2004-04-21
EP1409024B1 (de) 2008-08-06
ATE403442T1 (de) 2008-08-15
UY27390A1 (es) 2003-02-28
AU2002321236B2 (en) 2006-11-02
MXPA04000401A (es) 2004-03-18
JP2005504745A (ja) 2005-02-17
DE50212604D1 (de) 2008-09-18
RU2004105261A (ru) 2005-07-10
AR036183A1 (es) 2004-08-18
PL366426A1 (en) 2005-01-24
CA2453106A1 (en) 2003-02-06
KR20040030826A (ko) 2004-04-09
RU2305096C2 (ru) 2007-08-27
US20030108486A1 (en) 2003-06-12

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