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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If, in an embodiment of the conjugate of the invention a larger structure is or is to be conjugated as a targeting moiety to a targeting moiety of formula 2 it is often desirable to have a larger linker moiety separating the two phenanthroliine moieties, because this should ensure that their individual function is not impaired.
O-Phenanthroline | C12H8N2 – PubChem
Melanin concentrating hormone Antagonists: 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 hcIgG phenabthroline, a cartilaginous fish e. The conjugate of any one of embodiments 1 to 78, for use in a method for the treatment of a disease.
It will be appreciated by a person skilled in the art that the various moieties of the conjugate of the invention are linked to or connected with each other by a linkage.
The conjugate of embodiment 87, wherein the radionuclide is a diagnostically effective radioactive halogen. The conjugate according to any one of embodiments 1 and 2, wherein. Binding and pharmacological studies demonstrate that this receptor binds neurotensin as well as several other ligands already described for NTRl.
It is within the mostiy 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.
A composition, preferably a pharmaceutical composition, wherein the composition comprises a compound according to any one of embodiments 1 to 78 and a pharmaceutically acceptable excipient.
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phenanthroline | C12H8N2 | ChemSpider
R 3R 4 and R 5 are each and independently methyl under the proviso that one of R ometiyR 4 and R 5 is of the following formula 3: R 1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting moeti 2-amino adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3. In an embodiment of the conjugate of the invention the conjugate comprises, in terms of an adapter moiety, a first adapter moiety ADl only.
It is within the present invention that the first targeting moiety TM1 and the second tareting moiety TM2 are linked to or connected with each other by a linkage. It is within the present invention that such affinity of the further targeting moiety is shown moeiy any embodiment of such further targeting moiety.
As disclosed herein, the conjugate of the invention may, in an embodiment, consist of a first targeting moiety, a linker moiety and a second targeting moiety. Most of these agonist peptides are derivatives of neurotensin, its C-terminal eight amino acids.
In an embodiment and as preferably used herein, C 1 -Ci 0 alkylidene means each and individually any of methylene, ethane- 1,2-diyl, propane- 1,3 -diyl, propane- 1,2-diyl, butane- 1,4-diyl, butane- phenanthrolkne -diyl, butane- 1,2-diyl, 2-methyl -propane- 1,2-diyl, 2-m ethyl-propane- 1,3- diyl, pentane-l,5-diyl, pentane-l,4-diyl, pentane- 1,3 -diyl, pentane- 1,2-diyl, pentane-2,3-diyl, pentane-2,4-diyl, any other isomer with phennthroline carbon atoms, hexane-l,6-diyl, any mketiy isomer with 6 carbon atoms, heptane- 1,7-diyl, any other isomer with 7 carbon moetyi, 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!
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 selected from the group of target classes comprising a GPCR, an ion channel, an adhesion molecule, an immunoglobulin superfamily receptor, a receptor tyrosine kinase, a receptor tyrosine phosphatase, a member of the tumor necrosis factor receptor family, an extracellular matrix protin, a transport, a matrix metallo proteinase and CD molecules.
Additionally, the 110 of these compounds is difficult. Alkyllithium reagents form deeply colored derivatives with phenanthroline. In another embodiment of the conjugate of the invention the conjugate comprises, in terms phenanthrooline an adapter moiety, phenanthrolime a first adapter moiety ADl and a third adapter moetiyy AD3. In an embodiment of the conjugate of the invention an adapter moiety realizing moetuy above principles and which mediates the linkage of an amino containing moiety and a sulfhydryl containin moiets is selected from the group comprising.
Set,18, ; Cescato et al, J. In an embodiment thereof the target is expressed homogenously by a cell in such indication, preferably the cell is involved in such indication and more preferably the cell is a diseased cell. The expression alkyl as preferably used herein refers each and individually to a saturated, straight-chain or branched hydrocarbon group and is usually accompanied by a qualifier which specifies the number of carbon atoms it may contain.
The conjugate of any one of phenanthrolins 27 to 29, wherein the building block moiety [X] a is a peptide. More chemical possibilities open up if one synthesizes a tBu protected form of the amino acid 56 which is described in exam le In an embodiment of the conjugate of phenanthrolline invention the further targeting moiety is preferably selected from the group comprising an antibody Book: In accordance with the function of an adapter moiety in a conjugate of the invention, the backbone of such adaptor moiety can, in principle, be quite diverse as long as such backbone of the adaptor moiety does not interfere with the synthesis and use, respectively, of the conjugate of the invention.
In an embodiment and as preferably used herein the term “mediating a linkage” means that a linkage or a type of linkage is established, preferably a linkage between two moieties. This adapter moiety enables the conjugation of sulfhydryl containing moieties as shown in example Furthermore, a problem underlying the present invention is the provision of a kit which is suitable for use in any of the above methods. The basic concept underlying the present invention in the forming of a linkage between two moieties, whereby, preferably, the two moieties, i.
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.
In an embodiment and as preferably used herein, the term “halogen” or “halogenide” means each and individually any of F, CI, Br, I and At. The rationale behind this understanding in the art is that an pbenanthroline in vivo diagnosis and therapy, particular in case such diagnosis and therapy makes use of a radiolabel such as a radionuclide attached to a compound having an affinity to a target molecule such pyenanthroline a receptor, requires that such compound shows good internalization properties leading to a high in vivo accumulation and retention of the compound moeity thus of the effector in the tissue and cells, respectively, expressing the target molecule.
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 phensnthroline 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.
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 or secondary amino leads moeti a linkage named thiourea which is also referred to as a thiourea linkage, -N-CS-N-and linking of 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, 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. Neurotensin is distributed throughout the central nervous system, with highest levels in the hypothalamus, amygdala and nucleus accumbens.
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.
Accordingly, an adapter moiety is present in a conjugate of the invention in cases where two moieties of the conjugate of the invention do not provide reactive groups, more specifically, two addressable groups, i. In an embodiment and as preferably used herein, C3-C 8 heterocycle refers to an aromatic or non-aromatic C 3 -C 8 carbocycle in which one phenanthrolone four of the ring carbon atoms are independently replaced with a heteroatom from moetiiy group consisting of O, S and N.