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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As preferably used herein, an embodiment of a coordinate bond is a bond or group of bonds as realized when a metal is bound by a chelator. The conjugate of embodimentwherein the tumor is selected from the group comprising ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal phhenanthroline, breast cancer, meningioma, E wing’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.

phenathroline

Phenanthroline

Consequently, also due to avidity and re-binding effets a longer retention time is achieved which goes along with a higher effective dose and thus improvement in diagnosis and therapy of the respective disease. In an embodiment and as preferably used herein, C 3 -C 8 heterocyclo refers to a C 3 – C heterocycle group defined above wherein one of the carbocycles group hydrogen atoms is replaced with a bond. Acceptor is a moiety which mediates linking of an Effector to the third adapter moiety AD3, if present, or Acceptor is a moiety which mediates linking of an Effector to the branching moiety [Y], and.

R 6 is selected from the group consisting of hydrogen and C! R 6 is selected from the group consisting of hydrogen and and. A method for the treatment of a disease in a subject, wherein the method comprises administering to the subject a therapeutically effective amount of a conjugate according to any one of embodiments 1 to Two respective examples of intermediates are described in more detail in exam le 6 and The conjugate of any one of embodiments towherein the disease is a disease involving neurotensin receptor, preferably the disease is a disease involving neurotensin receptor 1.

R 6 is selected from the group consisting of hydrogen and methyl. Depending on the type of atoms linked and their atomic environment different types of linkages are created. 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. These small molecule compounds and SR in particular, however, cross the blood-brain barrier and are thus suitable neither for the radionuclide therapy of tumors nor for the radioactive diagnosis of tumors and imaging in particular, whereby the tumors are preferably those expressing NTR1, since irradiation of the central nervous system or any other non-radioactive cell-killing effect may have detrimental effects on the patient.

Examples of non-natural amino acids, preferably used for the construction of the conjugates of the invention are identified according to their abbreviation or name found in Table 2. As preferably used herein, the term “activated sulfonic acid” refers to a sulfonic acid group with the general formula -S0 2 -X, wherein X is a leaving group. Silverman, Academic Press Ltd. 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.

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The conjugate of any one of embodiments 1 to 18, wherein the first targeting moiety is selected from the group consisting of a compound of formula 4a compound of formula 5 and a compound of formula 6wherein. 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 at least 20, or more copies of NTR or at least 10, or more copies of NTR or at least 5, or more copies of NTR or at least 1, or more copies of NTR are expressed per cell.

Preferred linkages established between two moieties by means of an adapter moiety are the linkages indicated in Table 3 herein. In an embodiment and as preferably used herein, a theragnostically active compound is a compound which is suitable for or useful in both the diagnosis and therapy of a disease.

Attempts to find new antimalarials. 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.

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.

Only for colon weak or moderate expression under physiological conditions is described. It is within the present invention that such affinity of the further targeting moiety is shown by any embodiment of such further targeting moiety. Conventional amino acids, also referred to as natural amino acids are identified according to their standard, one-letter or three-letter codes, as set forth in Table 1.

It is, however, well known that the radionuclide chemistry and associated linkages are crucial particularly with respect to the attachment to the compound of an effector which provides the signal needed for diagnosis or which provides the therapeutically effective activity. It is within the present invention that the conjugate of the invention comprises a linker moiety.

O-Phenanthroline | C12H8N2 – PubChem

The kit of embodiment for use in any method as defined in any of the preceding embodiments. In an embodiment of the conjugate of the invention an adapter moiety realizing the above principles and which mediates the linkage of an amino containing moiety and a carboxylic acid containing moiety forms linkages to these moieties wherein the first linkage to the amino group is selected from the group comprising amide, urea, thiourea, alkylamine and sulfonamide and the corresponding reactive group as provided by the adapter moiety is independently selected from the group of carboxylic acid, activated carboxylic acid, sulfonic acid, activated sulfonic acid, aldehyde, ketone, isocyanate and isothiocyanate.

More preferably such discrimination or distinction forms the basis for said diagnosis and diagnosing, respectively.

The conjugate of any one of embodiments 1 to 26, preferably any one of embodiments 20 to 26, wherein the linker moiety LM is of general formula:. Moetly of these agonist peptides phenanthrolime derivatives of neurotensin, its C-terminal eight amino acids. 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.

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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 phenanthriline 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 of the conjugate of the invention the transporter to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising an ATP -binding cassette phenatnhroline family, an F-type ATPase, a V-type ATPase, a P-type ATPase, a member of the major facilitator superfamily MFS of transporters, and a member of the SLC superfamily of solute carriers.

The conjugate of embodiment 1, wherein the conjugate comprises an Effector moiety, wherein the Effector moiety comprises or is capable of comprising an Effector, wherein the Effector is selected from the group comprising a diagnostically active agent, a therapeutically active agent and a combination thereof. The conjugate of embodiment 8, wherein R 6 is selected from the group consisting of hydrogen and methyl.

The receptor can also stimulate cAMP formation, MAP kinase activation and the induction of growth related genes, such as krox Vincent et al. The following table summarizes the expression of NTR1 as described in the prior art indicating the tissue, degree of expression, detection method and the respective references. The present invention is based on the surprising finding of the present inventors that the conjugate of the invention is not only binding to NTR1 with a high affinity, but is also not crossing the blood-brain barrier.

In a preferred embodiment the linkage and the type of linkage is as defined herein.

The preferred type of adapter moieties in one embodiment are dicarboxylic acids, or activated forms thereof. 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.

In an embodiment of the conjugate of the invention the target to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected phenanthrooine groupB as defined hereinb. The conjugate of koetiy one of embodiments 1 to 78, for use in a method for the selection of a subject from a group of subjects, wherein the subject is likely to respond or likely not to respond to a treatment of a disease, wherein the method for phrnanthroline selection of a subject from 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 the diagnosis of a disease as described in any one of embodiments 79 to The conjugate of any one of embodiments 93 to 94, wherein the disease is selected from the group comprising tumors and hematological malignancies.

In an embodiment thereof the target is expressed heterogenously phenanrhroline a cell in such indication, preferably the cell is involved in such indication and more preferably the cell is a diseased cell. The conjugate pnenanthroline any one mietiy embodiments 1 to 77, wherein the con ugate is different from compound 89including the 18 F analog of this compound:. The receptor is also expressed in the dorsal root ganglion neurones of the spinal cord.

A generic formula of a preferred embodiment of an adapter moiety is as follows:.