C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 255/00 (2006.01) A01N 33/04 (2006.01) A01N 43/64 (2006.01) A01N 43/713 (2006.01) A01N 43/90 (2006.01) A01N 57/18 (2006.01) A61K 31/13 (2006.01) A61K 31/131 (2006.01) A61K 31/135 (2006.01) A61K 31/136 (2006.01) A61K 31/137 (2006.01) A61K 31/28 (2006.01) A61K 31/395 (2006.01) A61K 31/4025 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/555 (2006.01) A61K 31/66 (2006.01) A61K 31/675 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 49/04 (2006.01) A61K 49/06 (2006.01) A61K 51/04 (2006.
Patent
CA 2225453
This invention involves synthesis and use of a class of compounds having fomula (I) wherein: p and q are each independently integers of from 2 to 3; r is an integer of from 0 to 4; R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkenyl, aryl, arylalkyl, alkoxy, alkylthio, alkenoxy, alkenylthio, aryloxy, arylthio, alkyl interrupted by one or more oxa, alkenyl interrupted by one or more oxa, alkyl interrupted by thia, alkenyl interrupted by thia, aryloxyalkyl, alkoxyaryl, aminoalkyl, aminoalkenyl, aminoaryl, aminoarylalkyl, hydroxyalkyl, hydroxyalkenyl, hydroxyaryl, hydroxyarylalkyl, halogen substituted versions therof; R1 is a member selected from the group consisting of R2, R3, R4, and radicals of formula (V) and wherein, optionally, any two of R1, R2, R3 and R4 are combined to form a ring structure; said dimers therof, said dimers being formed by the covalent attachment of two complexing agents of formula (I) through a linking group having from 1 to 6 carbon atom;- and physiological salts thereof with the proviso that the molecular weight of said complexing agent does not exceed 2000, which chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy. Since these compounds are capable of decreasing the in vivo availability of tissue iron they are useful in management of free redical mediated tissue damage, and oxidation mediated tissue damage. When combined with radioisotopic or paramagnetic cations of first transition series elements, or elements with chemical properties similar to those of first transition series elements, prior to their administration, the resulting complexes are useful as diagnostic agents in nuclear medicine and magnetic resonance imaging (MRI).
L'invention se rapporte à la synthèse et à l'utilisation d'une classe de composés avec une affinité et une sélectivité de chélation vis-à-vis d'éléments de la première série de transition. L'administration d'un composé libre ou conjugué ou de sels physiologiques du composé libre ou conjugué a pour résultat une diminution de la biodisponibilité in vivo des éléments de la première série de transition et/ou une élimination hors du corps des éléments de la première série de transition ainsi que d'éléments possédant des propriétés chimiques similaires. Ces caractérisitiques rendent de tels composés utiles dans la gestion de maladies associées à un excès dans le corps d'éléments de la première série de transition ainsi que d'éléments possédant des propriétés chimiques similaires. Cette invention démontre que de tels composés inhibent la réplication des cellules mammifères, bactériennes et fongiques et sont donc utiles pour le traitement de néoplasies, infections, inflammations, de la réponse immunitaire et de l'interruption de grossesse. Puisque ces composés sont capables de diminuer la disponibilité in vivo du fer dans les tissus, ils sont utiles dans la gestion d'une détérioration tissulaire induite par les radicaux libres et par l'oxydation. Lorsqu'ils sont combinés avec des cations radioisotopiques ou paramagnétiques des éléments de la première série de transition ou avec des éléments possédant des propriétés chimiques similaires, avant leur administration, les complexes résultants sont utiles en tant qu'agents de diagnostic en médecine nucléaire et dans l'imagerie par résonance magnétiques (IRM).
Cyjon Rosa L.
Klein Joseph Y.
Klein Ofer
Simhon Elliot D.
Winchell Harry S.
Chelator Llc
Concat Ltd.
Fetherstonhaugh & Co.
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