ES2091865T3 - Tetraaza-compuestos macrociclicos que contienen 6 anillos, procedimiento para su preparacion y agentes farmaceuticos que los contienen. - Google Patents

Tetraaza-compuestos macrociclicos que contienen 6 anillos, procedimiento para su preparacion y agentes farmaceuticos que los contienen.

Info

Publication number
ES2091865T3
ES2091865T3 ES91250008T ES91250008T ES2091865T3 ES 2091865 T3 ES2091865 T3 ES 2091865T3 ES 91250008 T ES91250008 T ES 91250008T ES 91250008 T ES91250008 T ES 91250008T ES 2091865 T3 ES2091865 T3 ES 2091865T3
Authority
ES
Spain
Prior art keywords
denotes
group
hydrogen atom
figures
represent
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES91250008T
Other languages
English (en)
Inventor
Heinz Dr Gries
Bernd Dr Raduchel
Johannes Dr Platzek
Hanns-Joachim Dr Weinmann
Wolf-Rudiger Press
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
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
Application granted granted Critical
Publication of ES2091865T3 publication Critical patent/ES2091865T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/003—Compounds containing elements of Groups 3 or 13 of the Periodic System without C-Metal linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo

Abstract

COMBINACIONES DE TETRAAZA MACROCICLICAS QUE CONTIENEN 6-ANILLOS DE LA FORMULA GENERAL I DONDE ... PARA UN ENLACE SIMPLE O DOBLE Q PARA UN ATOMO DE NITROGENO O EL RESTO NH, X ELEVADO A 1 PARA UN ATOMO DE HIDROGENO, UNA -(CH SUB 2) SUB N-R SUB 1O N EN LA SIGNIFICACION DE LAS CIFRAS 1 HASTA 5, M EN LA SIGNIFICACION DE LAS CIFRAS 0 HASTA 2, Y R ELEVADO A 1 EN LA SIGNIFICACION DE UN ATOMO DE HIDROGENO O DE UN GRUPO HIDROXI, X (AL CUADRADO) PARA X ELEVADO A 1 O UN GRUPO -(CH SUB 2) SUB N-(O) SUB 1-(CH SUB 2) SUB K-(C SUB 6 H SUB 4) SUB Q-R (AL CUADRADO) CON K EN LA SIGNIFICACION DE LAS CIFRAS 0 O 1, Y R (AL CUADRADO) EN LA SIGNIFICACION DE UN ATOMO DE HIDROGENO, DE UN GRUPO ALCOXI C SUB 1-C SUB 4, DE UN GRUPO FUNCIONAL O UNIDO SOBRE ESTE GRUPO FUNCIONAL DE UNA BIO O MACROMOLECULA, A ELEVADO A 1, A (AL CUADRADO) , B ELEVADO A 1, B (AL CUADRADO) , C ELEVADO A 1, C (AL CUADRADO) , D ELEVADO A 1, D (AL CUADRADO) , E ELEVADO A 1, E (AL CUADRADO) , F ELEVADO A 1 Y F (AL CUADRADO) , INDEPENDIENTES ENTRESI, EN CADA CASO PARA X (AL CUADRADO) G PARA R (AL CUADRADO) O UN SEGUNDO MACROCICLO UNIDO SOBRE K DE LA FORMULA GENERAL II CON K EN LA SIGNIFICACION DE UN ENLACE DIRECTO DE UN GRUPO DE BIS (CARBONILOAMINO) (-NH-CO-CO-NH-) O DE UN GRUPO DE ALQUILENOS C SUB 1-C SUB 14, QUE SI SE DIERA EL CASO LLEVA EN LOS EXTREMOS, LOS GRUPOS DE CARBONILO (CO) O DE CARBONILOAMINO (-NH-CO-) O ATOMOS DE OXIGENO Y SI SE DIERA EL CASO UNO O MAS ATOMOS DE OXIGENO, GRUPOS IMINOS SUSTITUTOS DE HIDROXIMETILENO (-CH-OH-), CH(X (AL CUADRADO) )COOZ O CONTIENE DE UNA HASTA DOS C-C COMBINACIONES DOBLES Y/O TRIPLES, Z PARA UN ATOMO DE HIDROGENO Y/O UN EQUIVALENTE DE ION METALICO DE UN ELEMENTO DE NUMERO ATOMICO 21-29, 31, 32, 37-39, 42-44, 49 O 57-83 ESTAN EN LA MEDIDA EN QUE LOS 12 SUSTITUTOS DE ANILLO DE A ELEVADO A 1 HASTA F (AL CUADRADO) ESTAN COMO MINIMO PARA 8 ATOMOS DE HIDROGENO, EN QUE X ELEVADO A 1 Y X (AL CUADRADO) ESTAN SOLO SIMULTANEAMENTE PARA ATOMOS DE HIDROGENO , SIEMPRE Y CUANDO AL MENOS UNO DE LOS SUSTITUTOS DE ANILLO A ELEVADO A 1 A F (AL CUADRADO) NO ESTE PARA UN ATOMO DE HIDROGENO Y EN QUE EL MACROCICLO DE LA FORMULA GENERAL I NO CONTENGA MAS DE UNA BIO O MACROMOLECULA Y EN QUE EL RESTO DE LOS GRUPOS CO SUB 2H SE PRESENTE COMO ESTER O AMIDA ASI COMO SUS SALES CON BASES ORGANICAS E INORGANICAS, AMINOACIDOS O AMIDAS AMINOACIDAS. SON VALIOSOS MEDIOS DIAGNOSTICOS Y TERAPEUTICOS.
ES91250008T 1990-01-18 1991-01-16 Tetraaza-compuestos macrociclicos que contienen 6 anillos, procedimiento para su preparacion y agentes farmaceuticos que los contienen. Expired - Lifetime ES2091865T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE4001655A DE4001655A1 (de) 1990-01-18 1990-01-18 6-ring enthaltende makrocyclische tetraaza-verbindungen, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische mittel

Publications (1)

Publication Number Publication Date
ES2091865T3 true ES2091865T3 (es) 1996-11-16

Family

ID=6398485

Family Applications (1)

Application Number Title Priority Date Filing Date
ES91250008T Expired - Lifetime ES2091865T3 (es) 1990-01-18 1991-01-16 Tetraaza-compuestos macrociclicos que contienen 6 anillos, procedimiento para su preparacion y agentes farmaceuticos que los contienen.

Country Status (19)

Country Link
EP (1) EP0438206B1 (es)
JP (1) JPH05112567A (es)
KR (1) KR910014377A (es)
AT (1) ATE141602T1 (es)
AU (1) AU6981291A (es)
CA (1) CA2034242A1 (es)
DE (2) DE4001655A1 (es)
DK (1) DK0438206T3 (es)
ES (1) ES2091865T3 (es)
FI (1) FI94758C (es)
GR (1) GR3020973T3 (es)
HU (1) HUT56569A (es)
IE (1) IE75898B1 (es)
IL (1) IL96840A0 (es)
NO (1) NO910191L (es)
NZ (1) NZ236803A (es)
PT (1) PT96505B (es)
TW (1) TW233298B (es)
ZA (1) ZA91389B (es)

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AU3246893A (en) * 1991-12-10 1993-07-19 Dow Chemical Company, The Bicycloazamacrocyclophosphonic acid, conjugates, contrast agents and preparation
US5428139A (en) * 1991-12-10 1995-06-27 The Dow Chemical Company Bicyclopolyazamacrocyclophosphonic acid complexes for use as radiopharmaceuticals
MX9207165A (es) * 1991-12-10 1993-06-01 Dow Chemical Co Complejos de acido biciclopoliazamacrociclocarboxilico, sus conjugados, procedimientos para su preparacion y su uso como radiofarmaceuticos.
US5480990A (en) * 1991-12-10 1996-01-02 The Dow Chemical Company Bicyclopolyazamacrocyclocarboxylic acid complexes for use as contrast agents
DE69230970T2 (de) * 1991-12-10 2001-01-04 Dow Chemical Co Bicylclische, polyazamakrocyclocarbonsäure-komplexe, konjugate, herstellung und verwendung als kontraststoffe
WO1994026313A1 (en) * 1993-05-06 1994-11-24 The Dow Chemical Company Bicyclopolyazamacrocyclocarboxylic acid complexes, their conjugates, processes for their preparation, and use as contrast agents
US5739294A (en) * 1991-12-10 1998-04-14 The Dow Chemical Company Bicyclopol yazamacrocyclophosphonic acid complexes for use as contrast agents
AU4237493A (en) * 1993-05-06 1994-12-12 Dow Chemical Company, The Bicyclopolyazamacrocyclocarboxylic acid complexes, their conjugates, processes for their preparation, and use as radiopharmaceuticals
US5358704A (en) * 1993-09-30 1994-10-25 Bristol-Myers Squibb Hepatobiliary tetraazamacrocyclic magnetic resonance contrast agents
US5417959A (en) * 1993-10-04 1995-05-23 Mallinckrodt Medical, Inc. Functionalized aza-crytand ligands for diagnostic imaging applications
DE69504220T2 (de) * 1994-02-21 1999-04-29 Pliva Pharm & Chem Works Sulfonamidodioxepane mit hypoglykämischen Eigenschaften, Methoden zu ihrer Herstellung, ihre Zwischenprodukte und Salze
US6207826B1 (en) 1995-03-27 2001-03-27 Isis Pharmaceuticals, Inc. Macrocyclic compounds having nitrogen-containing linkages
WO1996030377A1 (en) 1995-03-27 1996-10-03 Isis Pharmaceuticals, Inc. Nitrogenous macrocyclic compounds
AU719002B2 (en) * 1996-04-19 2000-05-04 Dow Chemical Company, The Fluorescent chelates as visual tissue specific imaging agents
IT1291624B1 (it) * 1997-04-18 1999-01-11 Bracco Spa Chelati complessi di metalli paramagnetici a bassa tossicita'
WO1998047539A1 (en) * 1997-04-22 1998-10-29 Nycomed Imaging As Nmr image compounds
FR2794744B1 (fr) * 1999-06-09 2001-09-21 Guerbet Sa Complexes metalliques de polyaminoacides bicycliques, leur procede de preparation et leur application en imagerie medicale
US8986650B2 (en) 2005-10-07 2015-03-24 Guerbet Complex folate-NOTA-Ga68
FR2891830B1 (fr) 2005-10-07 2011-06-24 Guerbet Sa Composes a chaines aminoalcools courtes et complexes metalliques pour l'imagerie medicale
US8926945B2 (en) 2005-10-07 2015-01-06 Guerbet Compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium
EP2004642B1 (en) 2006-03-10 2017-07-26 Nordion (Canada) Inc. Bifunctional polyazamacrocyclic chelating agents
JP6608805B2 (ja) 2013-04-26 2019-11-20 ゲルベ 造影製剤および関連する調製方法
EP3544964B1 (en) 2016-11-28 2020-06-17 Bayer Pharma Aktiengesellschaft High relaxivity gadolinium chelate compounds for use in magnetic resonance imaging
JOP20210114A1 (ar) 2018-11-23 2023-01-30 Bayer Ag تركيبة وسط تباين وعملية لتحضيرها
FR3091873B1 (fr) 2019-01-17 2020-12-25 Guerbet Sa Complexe de gadolinium et d’un ligand chelateur derive de pcta diastereoisomeriquement enrichi et procede de preparation et de purification
FR3091872B1 (fr) 2019-01-17 2020-12-25 Guerbet Sa Complexe de gadolinium et d’un ligand chelateur derive de pcta diastereoisomeriquement enrichi et procede de synthese
US20230339945A1 (en) 2020-07-17 2023-10-26 Guerbet Method for preparing a chelating ligand derived from pcta
CN114105983B (zh) * 2021-11-09 2023-08-11 国科温州研究院(温州生物材料与工程研究所) 手性1,4,7,10-四氮杂-2,6-吡啶环蕃衍生物及其金属螯合物的制备和应用

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DE3129906C3 (de) * 1981-07-24 1996-12-19 Schering Ag Paramagnetische Komplexsalze, deren Herstellung und Mittel zur Verwendung bei der NMR-Diagnostik
DE3150917A1 (de) 1981-12-18 1983-06-30 Schering Ag, 1000 Berlin Und 4619 Bergkamen "2-amino-1-(1,3-dioxolan-4-yl)-ethanol-verbindungen, deren herstellung und verwendung zur weiterverarbeitung"
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DE3825040A1 (de) * 1988-07-20 1990-01-25 Schering Ag 5- oder 6-ring- enthaltende makrocyclische polyaza-verbindungen, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische mittel
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Also Published As

Publication number Publication date
JPH05112567A (ja) 1993-05-07
NO910191L (no) 1991-07-19
EP0438206B1 (de) 1996-08-21
DE4001655A1 (de) 1991-07-25
FI94758B (fi) 1995-07-14
GR3020973T3 (en) 1996-12-31
DE59108091D1 (de) 1996-09-26
NZ236803A (en) 1993-08-26
HU910156D0 (en) 1991-08-28
IE75898B1 (en) 1997-09-24
KR910014377A (ko) 1991-08-31
IL96840A0 (en) 1991-09-16
ATE141602T1 (de) 1996-09-15
HUT56569A (en) 1991-09-30
CA2034242A1 (en) 1991-07-19
ZA91389B (en) 1991-10-30
FI94758C (fi) 1995-10-25
FI910276A (fi) 1991-07-19
PT96505B (pt) 1998-07-31
AU6981291A (en) 1991-08-22
FI910276A0 (fi) 1991-01-18
EP0438206A1 (de) 1991-07-24
DK0438206T3 (es) 1997-01-20
NO910191D0 (no) 1991-01-17
TW233298B (es) 1994-11-01
PT96505A (pt) 1991-10-15
IE910162A1 (en) 1991-07-31

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