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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The linkage of the targeting moiety Biotin, targeting avidin or streptavidin, to the targeting moiety 4 is mediated by a single amino acid Ttds as linker moiety without the use of any adapter moieties. US discloses metabolically protected analogs of neurotensin.
In a further embodiment of the conjugate of the invention the protein scaffold is selected from the group comprising a protein scaffold for molecular recognition; a protein scaffold derived from naturally occurring protein domains; a protein scaffold derived from a venomous animal, preferably such venomous animal is one selected from the group comprising a spider, a scorpion, a see anemonea, an insect, a frog, a snail, a snake and fish; a genetically engineered protein scaffold; an affibody, wherein the affibody is preferably based on the Z-domain of staphylococcal protein A Nord et al.
Also, it is possible that more lesions can be diagnosed and treated, respectively, per patient. The conjugate of any one of embodiments 1 to 78, for use in a method for the treatment of a disease.
The conjugate of any one of embodiments 27 to 32, wherein the building block moiety [Z] b is a peptide. 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. Neurotensin is distributed throughout the central nervous system, with highest levels in the hypothalamus, amygdala and nucleus accumbens.
O-Phenanthroline | C12H8N2 – PubChem
The conjugate of embodiment 8, wherein R 6 is selected from the group consisting of hydrogen and methyl. In some embodiments, the activated carboxylic acid group is an ester with pentafluorophenol, nitrophenol, benzotriazole, azabenzotriazole, thiophenol or N-hydroxysuccinimide NHS as leaving group.
The conjugate of any one of embodiments 1 to 54, wherein the conjugate further comprises a third adaptor moiety [AD3], wherein the third adaptor moiety is mediating the linkage of the Effector moiety to the conjugate. The conjugate of any one of embodiments 40 to 31, wherein the second adapter moiety AD2, preferably prior to forming any linkage, is of the following structure:.
Pancreatic cancer Ehlers et al. The conjugate of embodimentwherein the radionuclide is a radioactive halogen. More speficially, such stability of the further targeting moiety can also be realized in those embodiments of the conjugate of the invention where the further targeting moiety is preferably selected from the group comprising an antibody, an antigen-binding antibody fragments, camelid heavy chain IgG hcIgGa cartilaginous fish e.
R 6 is selected from the group consisting of hydrogen and methyl; and. The conjugate of embodiment 87, wherein the modtiy is a diagnostically effective radioactive halogen. The conjugate of any one of embodiments 1 to 45, wherein the conjugate comprises a third adapter moiety AD3. Insofar, the range is actually an individualized disclosure of said integer. The conjugate of embodiment 46, wherein the adapter moiety AD3 mediates the linkage between branching moiety [Y] and the effector phenanthrolin EM.
The conjugate of any one of embodiments 20 and 21, wherein the first targeting moiety is a com ound of formula 4.
More chemical possibilities open up if one synthesizes a tBu protected form of the amino acid 56 which is described in exam le The expression alkylidene as preferably used herein refers to a saturated straight chain or branched hydrocarbon group wherein two points of substitution are specified.
The conjugate of embodiment 27, wherein building block moiety [X] a is linked to an adjacent moiety through a linkage, wherein the linkage is individually and independently selected from the group comprising an amide linkage, a urea linkage, a carbamate linkage, an ester linkage, an ether linkage, a thioether linkage and a disulfide linkage, and wherein the adjacent moiety is selected from the group comprising branching moiety [Y], building block moiety [Z] bsecond adapter moiety AD2, second targeting moiety TM2, first adapter moiety AD1 and first targeting moiety TM1.
In another embodiment of the conjugate of the invention the conjugate comprises, in terms of an adapter moiety, a first adapter moiety ADl, a second adapter moiety AD2 and a third adapter moiety AD3.
In an embodiment and as preferably used herein, a theragnostical agent or a theragnostically active agent is a compound which is suitable for or useful in both the diagnosis and therapy of a disease.
It was found that most neurotensin-derived metal labeled peptides have a very short circulation half-life due to rapid renal clearance as often observed for peptidic molecules. The conjugate of any one of embodiments 93 to 97, wherein Effector is a phenanthroilne metal, wherein preferably the radioactive metal mooetiy chelated by Acceptor, wherein Acceptor is a chelator.
A “Michael acceptor” is capable of reacting with nucleophiles especially sulfhydryl groups in an moefiy reaction as exem lified as follows: From Wikipedia, the free encyclopedia. Alkyllithium reagents form deeply colored derivatives with phenanthroline. 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.
phenanthroline | C12H8N2 | ChemSpider
Melanin concentrating hormone Antagonists: R 3R 4 and R 5 are each and independently methyl under the proviso that one of R 3R 4 and R 5 is of the following formula 3: The neurotensin receptor 1 NTRl was cloned in from rat brain and found to act as a high affinity, levocabastine insensitive receptor for neurotensin Tanaka et al, Neuron,4, Acidity p K a. In light of these surprising characteristics it is possible that, without wishing to be bound by any theory, because of the two targeting moieties more patients can be positively diagnosed and treated, respectively, within an indication.
The conjugate of any one of embodiments 1 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