MACROCYCLIC COMPLEXES 1 10 PHENANTHROLINE MOETIY PDF
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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The intermediate 59 was used in many examples.
Study of Metal-1,Phenanthroline Complex Equilibria by Potentiometric Measurements
In an embodiment of the conjugate of the invention the further targeting moiety is preferably selected from the group comprising an antibody Book: It will be appreciated by a person skilled in the art that depending on the structural class and origin of the targeting moiety different types of reactive groups are provided by the targeting molecule.
Simple alkyl chains wherein the two points of substitutions are in a maximal distance to each other like methane- 1,1-diyl, ethane- 1,2-diyl, propane- 1, 3 -diyl, butane- 1,4-diyl and pentane-l,5-diyl are also referred to as methylene which is also referred to as methane- 1,1 -diylethylene which is also referred to as ethane- 1 ,2-diylpropylene which is also referred to as propane- 1,3- diylbutylene which is also referred to as butane- 1,4-diyl and pentylene which is also referred to as pentane- 1,5 -diyl.
Based on this, synthesis of different coordination compounds with desired properties by ligand tailoring has become a fascinating research field.
Agonists and antagonists binding to NTR1 have been described in the prior art. Eptinezumab Erenumab Fremanezumab Galcanezumab. 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.
The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 and 15, preferably of any one of embodiments 12, 13, 14 and 15, wherein. R 1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl.
The conjugate of embodiment 34, wherein the branching moiety [Y] is of a structure as described in any one of embodiment 28 to 33 for building block moiety [X] a and building block moiety [Z]b. In an embodiment thereof the cell is involved in such phenanthrolune and more preferably the cell is a diseased cell. RG3 – R8 – RG4 10 wherein RG3 is a reactive group as described herein, preferably a reactive group as indicated in Table 4 or selected from the group comprising phemanthroline, carboxylic acid, activated carboxylic acid, chloro, bromo, iodo, sulfhydryl, hydroxyl, sulfonic acid, activated sulfonic acid, sulfonic acid esters like mesylate or tosylate, Michael acceptors, strained alkenes like trans cyclooctene, isocyanate, isothiocyanate, aldehyde, ketone, aminooxy, complexess, hydrazine, azide, alkyne and tetrazine.
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. Using the compound of the invention, the tumor-to-background ratio is at least 1. R 3R 4 and R 5 are each and independently selected from the group consisting of hydrogen and methyl under the proviso that one of R 3R 4 and R 5 is of the following formula 3: Stability constants obtained in the present study for and are given in Table 1.
AA-COOH is an amino acid selected from the group consisting of 2-amino- adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3. Compelxes 6 is selected from the group consisting of hydrogen and C 1 -C alkyl; and. In preferred embodiment the covalent linkages are provided by the first adaptor moiety ADl, the linker moiety LM and the second adaptor moiety AD2, or any combination thereof.
Upon the reactive groups having reacted, the reactive groups or the reaction product thereof and thus, ultimately, the two moieties are linked macorcyclic by at macrocyvlic one covalent bond to form a linkage of a certain type.
Phenanthroline – Wikipedia
Most of the research on the Phen derivates focuses on their catalytic, redox, photoredox, biological activities, and their supramolecular chemistry [ 13 — 18 ]. 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 homogeneously in an indication, preferably an oncology indication, more preferably in any indication related to oncology.
Dasiglucagon Glucagon Oxyntomodulin Antagonists: It also inhibited these pathogens by 5. In an embodiment of the conjugate of the invention the immunoglobulin superfamily receptor to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising a cytokine receptor, a growth factor receptor, and an Ig binding receptor.
Due to this chemical feature, Phen is used as ligand for soft and hard sites. It will be appreciated by a person skilled in the art that in particular an antibody, an antigen-binding antibody fragment, a camelid heavy chain IgG hcIgGa cartilaginous fish e.
For example, a capital first letter indicates that the L-form of the amino acid is present in the peptide sequence, while a lower case first letter indicating that the D-form of the correspondent amino acid is present in the peptide sequence.
The anti-target with regard to the selectivity factor is preferably one which must not or should not be targeted by the further targeting moiety.
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 a tumor indication, in which only a small portion of the tumors, preferably a tumor indication where only a small portion of the patients suffering from the tumor indication, express NTR1.
It will, however, be understood by a person skilled in the art that neither the linkages which may be macrocclic in embodiments the conjugate of the invention are limited to the ones of Table 4 nor the reactive groups forming such linkages.
In an specific embodiment preactivated moieties phenanthrkline be assembled directly before use or even after or during in vivo application. More preferably, a chemical bond is a covalent bond or a plurality of chemical bonds.