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1. WO1986000897 - NOVEL RADIOPHARMACEUTICALS AND CHELATING AGENTS USEFUL IN THEIR PREPARATION

Publication Number WO/1986/000897
Publication Date 13.02.1986
International Application No. PCT/US1985/001333
International Filing Date 15.07.1985
IPC
C07D 213/53 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
53Nitrogen atoms
C07D 213/82 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81Amides; Imides
82in position 3
C07D 277/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
C07D 285/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
285Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
C07F 13/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
13Compounds containing elements of Groups 7 or 17 of the Periodic System
C07K 5/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
CPC
C07C 323/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
C07D 213/53
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
53Nitrogen atoms
C07D 213/82
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
81Amides; Imides
82in position 3
C07D 277/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
C07D 285/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
285Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
C07F 13/005
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
13Compounds containing elements of Groups 7 or 17 of the Periodic System
005Compounds without a metal-carbon linkage
Applicants
  • UNIVERSITY OF FLORIDA [US]/[US] (AllExceptUS)
  • BODOR, Nicholas, S. [US]/[US] (UsOnly)
Inventors
  • BODOR, Nicholas, S.
Agents
  • BAUMEISTER, Mary, Katherine
Priority Data
632,38319.07.1984US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL RADIOPHARMACEUTICALS AND CHELATING AGENTS USEFUL IN THEIR PREPARATION
(FR) PRODUITS RADIOPHARMACEUTIQUES ORIGINAUX, ET AGENTS DE CHELATION UTILES POUR LEUR PREPARATION
Abstract
(EN) A dihydropyridine$(1,7)$pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radio-nuclide to the brain. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine$(1,7)$pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety $i(in vivo) to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.
(FR) On propose un type de système de distribution du rédox ou de produits chimiques, du type à sel dihydropyridine$(1,7)$pyridinium pour l'envoi au cerveau et à d'autres organes d'un radionucléide, spécifique au site et/ou à site préférentiel. Un agent de chélation, capable d'effectuer la chélation avec un radionucléide et possédant une fonction amino primaire, secondaire ou tertiaire, peut être transformé dans un agent analogue correspondant dans lequel ladite fonction est remplacée par un système rédox à sel dihydropyridine$(1,7)$pyridinium et ensuite complexée avec un radionucléide pour créer un nouveau produit radiopharmaceutique qui sous sa forme dihydropyridine lipoïdale pénètre la barrière BBB (barrière sang-cerveau) et autorise des concentrations de radionucléides plus élevées dans le cerveau, en particulier étant donné que l'oxydation de la moitié dihydropyridine $i(in vivo) en sel pyridinium ionique ralentit son élimination du cerveu, tout en accélérant son élimination de la circulation générale. Ce système d'envoi de radionucléides est bien adapté à des utilisations en scintigraphie et dans des techniques radiographiques semblables.
Related patent documents
NO19860980This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
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