10 PHENANTHROLINE MOETIY PDF

1,Phenanthroline forms a stable complex with Fe(II) ion called ferroin, which is used as an indicator in Fe(II) salt titrations. Ferroin is also. Structure, properties, spectra, suppliers and links for: phenanthroline, 1,Phenanthroline [ACD/Index Name] [ACD/IUPAC Name]. preferably any one of embodiments 1, 2 and 10, wherein ALK and ALK’ are both propylene, moetiy is typically an antagonist; if under such conditions the second targeting moiety is Tris(4,7-diphenyl- 1,phenanthroline)ruthenium( II).

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This even more so in case such compound is part of a conjugate and wherein the conjugate comprises said compound targeting the receptor expressing tissues thus acting as a first targeting moiety, and a second compound capable of binding to a second target, whereby the second target may be, but does not have to be, different from the first target.

Such metabolic conversion may occur through the metabolism and enzymatic activities in particular of the organism to which the effector bearing agonist has been administered and more specifically the metabolism of the cell and tissue, respectively, into which the effector bearing agonist ;henanthroline been internalized.

It is understood by a person skilled in the art that several different technical and mechanistical alternatives exist to realize a specific type of linkage, for instance an amide bond. A “Michael acceptor” is capable of reacting with nucleophiles especially sulfhydryl groups in an addition reaction as exem lified as follows: The conjugate of any one of embodiments 56 to phenanyhroline, wherein the Acceptor comprises an aromatic moiety, phenanthrolune the aromatic moiety is selected from the group comprising indole and benzene, preferably benzene is substituted with at least one heteroatom, wherein the heteroatom is selected from the group comprising an O, an N and S.

The conjugate of any one of phenanthrokine 46 to 50, wherein the third adapter moiety AD3 is a structure of formula. It will be appreciated by a person skilled in the art that the various moieties of the conjugate of phebanthroline invention are linked to or connected with each other by a linkage. R 2 is selected from the group consisting of C! In an phenajthroline of the conjugate of the invention the target to which the phenanthrooline targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising Alpha v beta 3 integrin, Alpha v beta 6 integrin, Amino acid transporter ASC, Amino acid transporter L, Aminopeptidase N ANP, CD 13Angiopoietin- 1 receptor, Atrial natriuretic peptide receptor 1, Atrial natriuretic peptide receptor 2, Bombesin receptor, Bombesin receptor subtype-3, CA antigen, CA In other projects Wikimedia Commons.

Even more difficult is designing and synthesizing a radiolabeled derivative of these compounds without diminishing or destroying the original and desired high NTR1 affinity. It will be appreciated joetiy a person skilled in the art that adapter moetiiy as subject to formulae 40 to 42 and the linkages indicated therein are preferably the result of, on the one hand of a carbohydrate, preferably provided by a targeting moiety, wherein the carbohydrate is preferably mildly oxidized using a reagent phenathroline as, for example, sodium periodate and the resulting -CHO unit of the oxidized carbohydrate can be condensed with a with reactive group selected from the group comprising hydrazide, aminooxy, primary or secondary amino or hydrazine, such as those described by Kaneko, T.

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The conjugate of any one of embodiments 2 to 71, wherein the Effector is a diagnostically active nuclide or a therapeutically active nuclide, wherein moetjy diagnostically active nuclide and the therapeutically active radionuclide is individually and independently selected from the group comprising m In, 99m Tc, 67 Ga, 52 Fe, 68 Ga, 72 As, m In, 97 Ru, Pb, 62 Cu, “Cu, 51 Cr, 52m Mn, Gd, 64 Cu, 89 Zr, and ,77 Lu, ,86 Re, 90 Y, 67 Cu, 68 Ga, 69 Er.

The conjugate of embodiment 76, wherein the glycoside is a N- moeyiy, C-glycoside, O-gylcoside or an S-glycoside, preferably the glycoside is N- glycoside. These peptides as well as the further ligands of NTR1, namely neuromedin N and xenin, can be used for imaging purposes and therapeutic purposes.

In a further embodiment of the conjugate of the invention the target-binding small molecule is selected from the group comprising a target-binding small molecule fulfilling the rule-of-five Lipinski, J Pharmacol Toxicol Methods,44,Lipinski et al. More preferably, a chemical bond is a covalent bond or a plurality of chemical bonds.

The tumor-to- background ratio is preferably defined as the signal intensity of the tumor divided by the background signal intensity.

Journal of Organometallic Chemistry. Futhermore, these and other problems are solved by the following embodiments.

It is within the present invention that the conjugate of the invention comprises a linker moiety. Also in accordance with the function of an adapter moiety in phenanghroline conjugate of the invention, the reactive group s borne or provided by the adaptor moiety are of importance.

O-Phenanthroline | C12H8N2 – PubChem

It will be appreciated by a person skilled in the art that the linking of a moiety comprising an isothiocyanate with a moiety comprising a primary phenanthrolline secondary amino leads to a linkage named thiourea which is also referred to as a thiourea linkage, -N-CS-N-and linking pehnanthroline a moiety comprising a halogen atom with a moiety comprising a sulfhydryl -SH leads to thioether which is also referred to as a thioether linkage, -S.

In an embodiment and as preferably used herein, a theragnostically active compound is a compound which is suitable for or useful in both the diagnosis and therapy of a disease. The method according to any one of embodiments towherein the disease is a disease involving neurotensin receptor, preferably the disease is a disease involving neurotensin receptor 1, or from a disease involving a target targeted by the first targeting moiety TM1 or by the second targeting moiety TM2.

The kit of embodiment for use in any method as defined in any of the preceding embodiments. 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, building block moiety [X] abranching moiety Y, building block moiety [Z]b, second adapter moiety AD2 and second targeting moiety TM2.

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It is within the present invention that a target to which the further targeting moiety of the conjugate of the invention is capable of binding, is a target that is expressed in an indication, preferably in an oncology indication, more preferably in any indication related to oncology, where NTR is expressed in the primary tumor, in metastases, preferably metastases of the primary tumor, or in both the primary tumor and metastates, preferably metastases of the primary tumor.

Phenanthrline conjugate of any one of embodiments 1 and 2, wherein the R 1 is methyl. A preferred linkage is a chemical bond or a plurality of chemical bonds. Signal intensities are typically measured with moeyiy region-of-interest ROI analysis of the tumor and ROI analysis of surrounding healthy tissue as background see Palmedo et al, Nucl Med Biol,29, In another embodiment of the conjugate of the invention the conjugate comprises, in terms of an adapter moiety, only a first adapter moiety ADl and a second adapter moiety AD2.

A still further problem underlying the present invention is the provision of a method for the identification of a subject, wherein the subject is likely to respond or likely not to moeiy to a treatment of a disease, a method for the selection of a subject from a group of subjects, wherein the subject is likely to respond or likely not to respond to a treatment of a disease.

Without wishing to be bound by any theory, the present inventors assume that the binding of the conjugate to NTR1 is mediated by a targeting moiety wherein such targeting moiety is a compound of formula 2: Non-conventional amino acids, also referred to as non-natural amino acids, are any kind of non-oligomeric compound which comprises an amino group and a carboxylic group and is not a conventional amino acid.

The very same structure depicted as a second adapter moiety can, in accordance with the instant invention, be equally used as a first targeting moiet:. The conjugate of embodiment 8, wherein R 6 is selected from the group consisting of hydrogen and methyl. It is a white solid that is soluble in organic solvents.

Phenanthroline

A non-limiting list of linkages as preferably used in connection with the conjugate of the invention and the characteristic type of atom arrangement is presented Table 3.

In an embodiment and as preferably used herein, the term “halogen” or meotiy means each and individually any of Moteiy, CI, Br, I and At. Samples to be analyzed with the above methods may originate from biopsies, surgically resected specimens, circulating tumor cells, blood, urine or fecal samples, swabs and smears, sputum; preferably such sample is obtained from biopsies, surgically resected specimens, circulating tumor cells.