Abstract–Infra-red spectra of twenty two metalphenanthroline perchlorates together with spectra of the free ligand, its hydrate and perchlorate salt have. Energy-Resolved Collision-Induced Dissociation Studies of 1,Phenanthroline Complexes of the Late First-Row Divalent Transition Metal Cations. A61K51/ Organic compounds complexes or complex-forming .. Embodiment The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6, 7, 8 and 9, For example, in case the first targeting moiety is targeting NTR1 the first targeting moetiy is Such chelators include, but are not limited to linear, macrocyclic.
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For the Sc III: In some embodiments, the activated carboxylic acid group is an ester with pentafluorophenol, nitrophenol, benzotriazole, azabenzotriazole, thiophenol or N-hydroxysuccinimide NHS as leaving group. Galanin Galanin Galmic Galnon Antagonists: The probable structures of the correspondingspecies in aqueous solution were proposed as follows.
BEST software program was used to analyze the potentiometric data collected from the titrations studies, as described previously [ 29 ].
Phenantholine also disclosed herein, the linker moiety LM, in an embodiment, is of the following general formula:. As shown in Figure 5the species is major species found in an aqueous solution at pH 4. For example, activated forms of a carboxylic acid group may include, but are not limited to, acyl chlorides, symmetrical or unsymmetrical anhydrides, and esters.
Phenanthroline – Wikipedia
In an embodiment and as preferably used herein, arylene refers to an aryl group which has two covalent bonds and can be in the ortho, meta, or para configurations as shown in the following structures:. The distribution diagram, computed by the SPE [ 29 ] software for a solution containing 9. It will be appreciated by a person skilled in the art that adapter moiety as subject to formulae 38 and 39 and the linkages indicated therein are preferably the result of, on the one hand of a primary or secondary amino group, preferably provided by a targeting moiety, and, on the other hand, of a reactive group selected from the group comprising carboxylic acid, activated carboxylic acid, sulfonic acid, activated sulfonic acid, isocyanates and isothiocyanates, wherein the reactive group is preferably provided by an adapter moiety.
The conjugate of any one of embodiments 79 to 89, wherein the method for the diagnosis is an imaging method. Hence the type of radionuclide, the type of compound which mediates target binding, and the method used for linking them to one another may have unpredictable effects on the properties of the radiolabeled version of the compound.
Typically, the agonist carries a therapeutically or diagnostically active effector such as a chelated metal label and more specifically a chelated radiolabel suitable for therapy and diagnosis, respectively.
If, for example, the targeting moiety is a protein, such as an antibody or antibody fragment, the preferred reactive groups for forming a linkage with another macrpcyclic and an adapter moiety in particular, are sulfhydryl groups and amino groups.
Study of Metal-1,Phenanthroline Complex Equilibria by Potentiometric Measurements
Eptinezumab Erenumab Fremanezumab Galcanezumab. In this case usually specific reagents are used for activation of at least one component, for instance the carboxylic acid. In an embodiment and as preferably used herein, a diagnostically active compound is a compound which is suitable for or useful macroycclic the diagnosis of a disease.
A C 1 -C 8 alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, Ci- C 8 alkyl, [ C!
The conjugate of any one of embodiments 2 to 42, wherein the Effector moiety EM is linked, preferably covalently linked to the branching moiety Y. In an embodiment and as complexee used herein, C 3 -C 8 cycloalkylmethyl means each and individually any of cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl and cyclooctylmethyl.
The conjugate of any one of embodiment 27 and 28, wherein the building block X is of eneral formula.
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In an embodiment and as preferably used herein, Ci-C 4 alkyl means each and individually any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl. It is within the present invention that the conjugate of the invention comprises, under the proviso that either the first targeting moiety TMl or the second targeting moiety TM2 is a compound of formula 2in any of its embodiments, a further targeting moiety.
Unless indicated to the contrary, moety amino acid sequences are phenatnhroline herein in N- to C-terminus direction.
In another embodiment of the conjugate macrocycic the invention the conjugate comprises, in terms of an adapter moiety, a second adapter moiety AD2 only. Species distribution curves of the Sc III ion and a Phen system as a function of —log [ ] for a solution initially containing 9. The conjugate of any one of embodiments 1 to 26, preferably any one of embodiments 20 to 26, wherein the linker moiety LM is of general formula:.
In an embodiment and as puenanthroline used herein, the term “-succinimide-” refer to a bivalent structure according to formula 9. Such embodiment is indicated in formula 28 and is described in more detail in example The conjugate of any one of embodiments 1 to 36, wherein the first adapter moiety AD1 mediates linkage to the first targeting moiety TM1 and to an adjacent moiety, wherein the adjacent moiety is selected from the group comprising linker moiety LM, phenanhtroline block moiety [X] abranching moiety Y, building block moiety [Z]b, second adapter moiety AD2 and second targeting moiety TM2.
TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to complexse first target. In accordance with the present invention in the conjugate of the invention building block moiety [X] a may be absent or be present in the form of a single building block X or be present macrrocyclic the form of a polymer, wherein the polymer constists of a number of building blocks X, wherein the number of building blocks X forming moetih polymer is “a”, i.
Examples of reactive groups which, in some embodiments of the invention, are used in the forming of linkages which may be realized in embodiments the conjugate of the invention are summarized in Table 4. Effector is selected from the group comprising a diagnostically active agent and a therapeutically active agent.
The method of embodimentwherein the conjugate comprises a therapeutically active agent, whereby the agent is preferably a radionuclide. View at Google Scholar S. The conjugate of any one of embodiments 1 to 77, wherein the con ugate is different from compound 89including the 18 F analog of this compound:.
Designing new coordination compounds with therapeutic abilities has been part of this activity [ 9 — 17 ]. This is an open 1 article distributed under the Creative Commons Attribution Licensewhich permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
The conjugate of macrocycilc one of embodiments towherein the method of diagnosis is an imaging method.
TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target. In an embodiment and as preferably used herein, C3-C 8 cycloalkyl means each and individually any of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl.
R 6 is selected from the group consisting of hydrogen and C 1 -C alkyl; and. The analyzed results showed that the stability constant values obtained for species same at all molar ratios. The stability comlpexes for the binary complexes increased as the ionic radii of the metal cations decreased. The conjugate of any one of embodiments 2 to 58, preferably embodiment 57, wherein the Effector is a diagnostically active nuclide, preferably a diagnostically active radionuclide, or a therapeutically active nuclide, preferably a therapeutically active radionuclide.
SPE software program was used to evaluate the concentration distributions of the species formed in solution. The conjugate of any one of embodiments 1 to mcrocyclicwherein both the first adaptor moiety ADl and the second adaptor moiety AD2 are present.
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Such separation can be expressed by the number of covalent linkages realized between the first targeting moiety TM1 and the second targeting moiety TM2. In this respect, numerous investigations in the properties and applications of ruthenium II complexes compleexs 1,phenanthroline phen as a ligand or mixed with other ligands are reported [ 25 — 27 ]. The preferred type of adapter moieties in one embodiment are amino acids, or activated forms thereof.
In an embodiment and as preferably used herein, “Aryl” refers to a carbocyclic pbenanthroline group. R 3R complexez and R 5 are each and independently selected from the group consisting of hydrogen and Ci-C 4 alkyl under the proviso that one of R 3R 4 and R 5 is of the following formula 3.