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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Immunochemistry, edited by Carel J. R 1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3. Two respective examples of intermediates are described in more detail in exam le 6 and The conjugate of embodiment 96, wherein the tumor is selected from the group comprising ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, Ewing’s sarcoma, pleural mesothelioma, head and neck cancer, non-small cell lung cancer, gastrointestinal stromal tumors, uterine leiomyoma and cutaneous T-cell lymphoma, preferably ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, Ewing’s sarcoma, and indications subject to group A defined herein.
It will be appreciated by a person skilled in the art that the target recognized by the further targeting moiety, regardless of whether it is within the conjugate of the invention the first targeting moiety TM1 or the second targeting moiety TM2, can, in principle, be any target under the proviso that the further targeting moiety is capable of binding to such target.
These peptides as well as the further ligands of NTR1, namely neuromedin N and xenin, can be used for imaging purposes and therapeutic purposes.
Phenanthroline
The formation of the chemical bond removes a hydroxyl group from phenanthorline 1 -carboxyl group of the amino acid when it is located to the left of the adjacent amino acid e. The kit of embodiment for use in any method as defined in any of the preceding embodiments. In other projects Wikimedia Commons. In an embodiment and as preferably used herein, a therapeutic agent or a therapeutically active agent is a compound which is suitable for or useful in the treatment of a disease.
It phneanthroline very well for forming linkage to amino containing moieties bound to the solid phase resin.
The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6 and 7, preferably any one of embodiments 1 and 2, wherein R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and methyl under the proviso that one of R3, R4 and R5 is of the following formula 3. 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 phenanghroline, where NTR is expressed at a low density.
The conjugate of any one of embodiments 34 and 35, wherein the branching moiety [Y] comprises a reactive group which allows, moetiu with a corresponding complementary reactive group, forming of a linkage individually and independently selected from the group comprising an amide linkage, a urea linkage, a thiourea linkage and an amine linkage.
The conjugate of embodiment 87, wherein the radionuclide is a diagnostically effective radioactive halogen. It is understood that both modifications can apply to the same amino acid and apply to adjacent conventional amino acids present in amino acid sequences without hyphens explicitly illustrated.
O-Phenanthroline | C12H8N2 – PubChem
In an embodiment of the conjugate of the invention the adhesion molecule to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising an integrin, a cell adhesion molecule CAMsa selectin, a cadherin, a lectin and a claudin. Maleimide thioether bromo sulfhydryl thioether aminooxy aldehyde oxime. Also, a problem underlying the present invention is the provision of a pharmaceutical composition containing a compound having the characteristics as outlined above.
In an embodiment of the conjugate of the invention the further pphenanthroline moiety is preferably selected from the group comprising an antibody Book: 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, pbenanthroline a target that is expressed in an indication, preferably a tumor indication, in which only a small portion of the tumors, preferably modtiy tumor indication where only a small portion of the patients suffering from the tumor indication, express NTR1.
Compound 57 is also well suited for the conjugation of proteins or modified oligonucleotides. It is within the present invention that such selectivity of the further targeting moiety is shown by any embodiment of such further phenanhhroline moiety. The conjugate of any one of embodiments towherein the disease is a disease involving neurotensin receptor, preferably the disease is a disease involving neurotensin receptor 1.
Also, it is possible that more lesions can be diagnosed and treated, respectively, per patient. phenantnroline
In terms of its coordination properties, phenanthroline is similar to 2,2′-bipyridine bipy but binds metals more phennathroline since the chelating nitrogen donors are preorganized. As described in more detail below and in the example part the compounds of the invention are conveniently prepared by either liquid phase or solid phase synthesis methods. Thyrotropin alfa TSH thyrotropin.
The preparation of 56 is described in Example 5A. The conjugate of any one of embodiments 1 to 78, for use in a method for the diagnosis of a disease.
For non-conventional amino acids, a 3 -letter code was used where the first letter indicates the stereochemistry of the C-a-atom. In an embodiment and as preferably used herein, a diagnostic agent or a diagnostically active agent is a compound which is suitable for or useful in phenanthroine diagnosis of a disease. This page was last edited on 20 Octoberat The conjugate of embodiment 47, wherein the adapter moiety AD3 mediated the linkage between the second targeting moiety TM2 and the effector moiety EM.
In an embodiment and as preferably used herein, C 3 -C 8 carbocyclo refers to a C 3 – C 8 carbocycle group defined above wherein one of the carbocycles group hydrogen atoms is replaced with a bond. Imaging,36, Furthermore, a problem underlying the present invention is the provision of a kit which is suitable for use in any of the phenantrholine methods. As preferably used herein low density means that less than copies of NTR per cell are expressed.
The dissociation constant is commonly used to describe the affinity between a ligand L such as a drug and a protein P i. It is within the present invention that such stability of the further targeting moiety is shown by any embodiment of such further targering moiety.
Phenanthroline – Wikipedia
It will be appreciated by a person skilled in the art that adapter moiety 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 such as, for example, sodium moefiy 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.
The conjugate of any one of embodiments 1 and 2, wherein the R 1 is methyl.
The conjugate of any one of embodiments 1 to 74, wherein the conjugate has an IC 50 of nM or less, preferably 50 nM or less, for a target targeted by either the first targeting moiety TMl or the target targeted by the second targeting target TM2, preferably the conjugate has an IC50 of nM or less, preferably 50 nM or less for NTR, more preferably for NTR1.
Three neurotensin receptors are known, namely neurotensin receptor 1, also referred to as NTRl, neurotensin receptor 2, also referred to as NTR2, and neurotensin receptor 3, also referred to as NTR3. As also disclosed herein, the linker moiety LM, in an embodiment, is of the following general formula:.
The conjugate of embodiment 66, wherein the second targeting moiety is targeting a target different from neurotensin receptor 1preferably the first targeting moiety TM1 is targeting NTR, prefereably NTR1, and wherein.
In an embodiment and as preferably used herein, C2-Cio alkylidene means each and individually any of ethane- 1,2-diyl, propane- 1,3 -diyl, propane- 1,2-diyl, butane- 1,4-diyl, butane- 1,3 -diyl, butane- 1,2-diyl, 2-methyl-propane- 1,2-diyl, 2 -methyl-propane- 1,3 -diyl, pentane- 1,5-diyl, pentane- 1,4-diyl, pentane- 1,3-diyl, pentane- 1,2-diyl, pentane-2,3-diyl, pentane-2,4-diyl, any other isomer with 5 carbon atoms, hexane-l,6-diyl, any other isomer with 6 carbon atoms, heptane- 1,7-diyl, any other isomer with 7 carbon atoms, octane- 1,8-diyl, any other isomer with 8 carbon atoms, nonane-l,9-diyl, any other isomer with 9 carbon atoms, decane-l,diyl and any other isomer with 10 carbon atoms, preferably C 2 -C 10 alkylidene means each and individually any of ethane- 1,2-diyl, propane- 1,3 -diyl, butane- 1,4- diyl, pentane-l,5-diyl, hexane-l,6-diyl, heptane- 1,7-diyl, octane- 1,8-diyl, nonane-l,9-diyl and decane-l,diyl.
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