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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Phenanthrolne carbocyclic aromatic group or a heterocyclic aromatic group can be unsubstituted or substituted with one or more groups including, but not limited to, – Q- C 8 alkyl, [ C!
For example, activated forms of a sulfonic acid may include, but are not limited to, sulfonyl chlorides or sulfonic acid anhydrides. Furthermore, any of the linkages summarized in Table 4 herein, can be realized by means of an adapter moiety, preferably the first adapter moiety. The reduced ferrous form has a deep red colour and the oxidised form is light-blue. 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, Phenanthroline is however a weaker donor than bipy.
The dissociation constant is commonly used to describe the affinity between a ligand L such as a drug and a protein P i. Biol,29, ; Bruehlmeier et al, Nucl. The conjugate of any one of embodiments 1 to 45, wherein the conjugate comprises a third adapter moiety AD3.
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, C 2 -C 5 alkyl means each and individually any of ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2- methyl-butyl, 3 -methyl -butyl, 3-pentyl, 3-methyl-butyl, 2-methyl-butyl and 2,2- dimethylpropyl. Most preferably, the linkage is a covalent bond or a coordinate bond.
To the extent it is referred in the instant application to a range indicated by a lower integer and a higher integer such as, for example,such range is a representation of the lower integer, the higher integer and any integer between the lower integer and the higher integer.
Phenanthroline – Wikipedia
The conjugate of any one of embodiments 46 to phenantjroline, wherein the third adapter moiety AD3 is a structure of formula. It is within the present invention that any embodiment of the linker moiety as disclosed herein and in particual embodiments of the linker moiety VIII to XV as disclosed herein, can be realized in any of the embodiment of the conjugate of the invention and in particular in embodiments I to VII of the conjugate of the invention as disclosed herein.
The conjugate of embodiment 68, wherein the tumor is selected from group A, wherein group A comprises Neoplasms; Neoplasm, benign; Neoplasm, uncertain whether benign or malignant; Neoplasm, malignant; Neoplasm, metastatic; Neoplasm, malignant, uncertain whether primary or metastatic; Tumor cells, benign; Tumor cells, uncertain whether benign or malignant; Tumor cells, malignant; Malignant tumor, small cell type; Malignant tumor, giant cell type; Malignant tumor, fusiform cell type; Epithelial neoplasms; Epithelial tumor, benign; Carcinoma in situ; Carcinoma; Carcinoma, metastatic.
Phenanthrroline 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. The expression moetij as preferably used herein refers to a saturated straight chain or branched hydrocarbon group wherein two points of substitution are specified. Based on such general formula, the conjugate of the invention may be realized embodiments such as embodiments I to VII outlined in the following.
This adapter moiety enables the conjugation of sulfhydryl containing moieties as shown in example Such linkage resits in the first targeting moiety TM1 and the second targeting moiety TM2 being separated from each other.
As preferably used herein, the term “activated carboxylic acid” refers to a carboxylic acid group with the general formula -CO-X, wherein X is a leaving group.
In connection with the latter embodiment of the conjugate of the invention the embodiment of the compound of formula 2 present in the conjugate of the invention as TMl is different from the embodiment of the compound of formula 2 present in the conjugate of the invention as TM2; alternatively, the embodiment of the compound of formula 2 present in the conjugate of the invention as TMl is identical to the embodiment of the compound of formula 2 present ,oetiy the conjugate of the invention as TM2.
From Wikipedia, the free encyclopedia. The conjugate of any one of embodiments 1 to 77, wherein the con ugate is different from compound 89including the 18 F analog of this compound:.
A variety of substituted derivatives of phen have been examined phenathroline ligands. Chemistryvolume 34, Representative examples of a C 3 -C 8 heterocycle include, benzofuranyl, benzothiophene, indolyl, benzopyrazolyl, coumarinyl, isoquinolinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, quinolinyl, pyrimidinyl, pyridinyl, pyridonyl, pyrazinyl, pyridazinyl, isothiazolyl, isoxazolyl and tetrazolyl.
For example, in case the first targeting moiety is targeting NTR1 the first targeting moetiy is typically phenanthrolinw antagonist; if under such conditions 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 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 of phenamthroline agonist.
In mpetiy embodiment and as preferably used herein, a therapeutically active compound is a compound which is suitable for or useful in the treatment of pgenanthroline disease. The conjugate of any one of embodiments 2 to 42, wherein the Effector moiety EM is linked, preferably covalently linked to the branching moiety Y.
For instance, the linking of a moiety comprising a primary or secondary amino with a moiety comprising a carboxylic acid leads to a linkage named amide which is also referred to as amide linkage, -CO-N- -N-CO.
It will be appreciated by a person skilled in the art that adapter moiety as subject to formulae 34 to 37 and the linkages indicated therein are preferably the result of, on the one hand of a sulfhydryl group, preferably provided by a targeting moiety, and, on the other hand, of a reactive group selected from the group comprising Michael acceptor, halogen and sulfhydryl, wherein the reactive group is preferably provided by an adapter 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 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.
R 6 is selected from the group consisting of hydrogen and methyl. 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.
Insofar, surprisingly the position of R 7i.
In an alternative embodiment the number of covalent bonds between the first targeting moiety TM1 and the second targeting moiety TM2 is about from 4 topreferably about from 5 toand more preferably about from 6 to Preferably the terms conjugate of the invention and compound of the invention are used interchangeably.
The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 13 and 14, preferably any one of embodiments 12, phenabthroline and 14, wherein. A method for the diagnosis of a disease in a subject, wherein the method comprises administering to the subject a diagnostically effective amount of a compound according to any one of embodiments 1 to The kit of embodiment for use in any method as defined in any of the preceding embodiments.
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 embodiment 31, wherein the building block Z is of general formula.