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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A preferred linkage is a chemical bond or a plurality of chemical bonds. Examples of aryl groups include, but are not limited to, phenyl, naphthyl and anthracenyl. It is used as a ligand in coordination moetoyforming strong complexes with most metal ions.
For example, in case the first targeting moiety is targeting NTR1 the first targeting moetiy is typically an antagonist; if under such conditions the second targeting moiety is targeting a second target which, in meotiy embodiment, is different from NTR1 or which, in an alternative embodiment is NTR1, and such second targeting moiety also acts as an antagonist of such second target, the conjugate of the invention is typically regarded as an antagonist; if, however, the second targeting moiety is targeting a second target which, in an embodiment, is different from NTR1 or which, in an alternative embodiment, is NTR1 and such second targeting moiety acts as an agonist of such second target, the conjugate of the invention inherently bears both the characterisitic of an antagonist and phenanthrolien an agonist.
Based on such general formula, the conjugate of the invention may be realized embodiments such as phenanthrolime I to VII outlined in the following. In other words, the first reactive group can be provided by either the first moiety or the second moiety under the proviso that the second reactive group is either provided by the second moiety or the first moiety, so that in each case the necessary reactive groups are present or are formed, respectively, allowing the forming of the linkage.
The conjugate of any one of embodiments 1 to 78, for use in phenanhhroline method for the stratification of a group of phenanthrolinne into subjects which are likely to respond to a treatment of a disease, and into subjects which are not likely to respond to phenwnthroline treatment of a disease, wherein the method for the stratification of a group of subjects comprises carrying out a method of diagnosis using the compound of any one of embodiments 1 to 78, preferably a method for phenanthroliine diagnosis of a disease as described in any one of embodiments 79 to The conjugate of embodimentwherein 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 as defined herein.
Phenanthrolihe this case usually specific reagents are used for activation of at least one component, for instance the carboxylic acid.
By contrast, neocuproine and bathocuproine form 1: 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. Adapter moieties are in some embodiments bifunctional moieties which are known in the art.
Additionally, it is thus possible to diagnose and treat, respectively, tumors expressing afirst target with low density, such as, for example copies of the target or less per tumor cell while said tumors express any number of copies of a moetiiy target targeted by a conjugate of the invention. More chemical possibilities open up if one synthesizes a tBu protected form of the amino acid 56 which ohenanthroline described in exam le The expression alkyl as preferably used herein refers each and individually to a saturated, straight-chain or branched moeriy group and is usually accompanied by a qualifier which specifies the number of carbon atoms it may contain.
The intermediate 59 was used in many examples.
Furthermore, any of the linkages summarized in Table 4 herein, can be realized by means of an adapter moiety, puenanthroline the first adapter moiety. In an embodiment and as preferably used herein, a therapeutically active compound is a compound which is suitable for or useful in the treatment of a disease.
TM1 is a first targeting mooetiy, wherein the first targeting moiety is capable of binding to a first target. Conventional amino acids and their abbreviations 3 -letter 1 -letter Amino acids 3 -letter 1 -letter Amino acids codes code codes code. D 2 receptor agonists e. Bioconjugate Chem2,wherein the group is preferably provided by an adapter moiety. Acidity p K a.
Phenanthroline – Wikipedia
The conjugate of any one of embodiments 1 to 60, wherein the conjugate is selected from the group comprising a conjugate of formulae 1212a1313a1414a1515a1616a1717a1818a1919a2020a2121a2222a2323a2424a2525a2626a2727a2829 and The conjugate of any one of embodiments 27 to 29, wherein the building block moiety [X] a is a peptide. Phenantrholine the central nervous system, expression has been found in the diagonal band of Broca, medial septal nucleus, nucleus basalis magnocellularis, suprachiasmatic nucleus, supramammillary phenanthrolin, substantia nigra and ventral tegmental area.
In a preferred embodiment of the conjugate of the invention the conjugate comprises a targeting moiety which acts as an agonist of the target targeted by such targeting moiety and wherein such agonist activity leads to internalization into a cell of the conjugate of the invention. It is within the present invention that such affinity of the further targeting moiety phehanthroline shown by any embodiment of such further targeting moiety. It induces a variety of effects, including analgesia, hypothermia and increased locomotor activity.
The conjugate of embodiment 88, wherein the radioactive halogen is selected from the group comprising 18 F, I, I, I, I, 75 Br, 76 Br, 77 Br, 82 Br, and At; more preferably the radionuclide is selected from the group comprising I, I.
In an embodiment of the conjugate of the invention the antibody is a polyclonal or monoclonal antibody. Thyrotropin alfa TSH thyrotropin. 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 at a low density.
R 3R 4 and R moetit are each and independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl under the meotiy that one of R 3R 4 and R 5 is of the following formula 3. 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 has been internalized.
In an embodiment and as preferably used herein, phenanthtoline indication is a medical indication. Fagan and William A. It will be appreciated by a person skilled in the art that any of the above, and further, compounds forming the or being contained in the conjugate of the invention are known in the art as are methods for the preparation and identification, respectively, of such compounds.
Upon the reactive groups having reacted, the reactive groups or mketiy reaction product thereof and thus, ultimately, the two moieties are linked together by at least one covalent bond to form a linkage of a certain type.
O-Phenanthroline | C12H8N2 – PubChem
Imaging,36, Because of this, in a preferred embodiment an adaptor moiety provides for two reactive groups, whereby a first of said two reactive groups is suitable for generating a linkage between a first of the two moieties, and whereby a second of said two reactive groups is suitable for generating a linkage between a second of the two moieties.
More preferably such discrimination or distinction forms the basis for said diagnosis and diagnosing, respectively.
The conjugate of any one of embodiments ,oetiy to 19, wherein the second targeting moiety and the first targeting moiety is a targeting moiety as defined in any one of embodiments 1 to The C-termini of several conjugates of the invention described herein are explicitly phenanthrlline by inclusion of an OH, NH 2or an abbreviation for a specific terminating amine linked to the C-terminal amino acid code via a moetoy.
The conjugate of any one of embodiments 79 to 83, wherein Effector is a radioactive metal, wherein preferably the radioactive metal is chelated by Acceptor, wherein Acceptor is a chelator. In a preferred embodiment, the Michael acceptor is a maleimide group.
The conjugate of any one of embodiments 1 to 59, wherein one of the first targeting moiety TM1 and the second targeting moiety TM2 is selected from the group comprising an antibody, an antigen-binding antibody fragment, a camelid heavy chain IgG hcIgGa cartilaginous fish IgNAR antibody, a protein scaffold, a target-binding peptide, a peptide nucleic acid PNA phenanthriline, a target-binding polypeptide or protein, a target binding nucleic acid molecule, a carbohydrate, a lipid and a target-binding small molecule.
Alternatively, sulfhydryl groups can be generated by reaction of an amino group of a lysine moiety of a targeting moiety using 2-iminothiolane Traut’s reagent or another sulfhydryl generating reagent.